Claims for Patent: 10,273,252

Summary for Patent: 10,273,252

Title:	Substituted dihydropyrrolopyrazole derivative
Abstract:	The present invention provides a compound represented by the general formula (Ia) or a pharmacologically acceptable salt thereof. In the general formula (Ia), two R moieties each independently represent a C.sub.1-3 alkyl group or the like; and R.sup.1, R.sup.2 and R.sup.3 each independently represent an optionally substituted linear or branched C.sub.1-4 alkyl group. ##STR00001##
Inventor(s):	Iwase; Noriaki (Ube, JP), Aga; Yasuhiro (Ube, JP), Ushiyama; Shigeru (Ube, JP), Kono; Shigeyuki (Ube, JP), Sunamoto; Hidetoshi (Ube, JP), Matsushita; Takashi (Ube, JP), Ogi; Sayaka (Ube, JP), Umezaki; Satoshi (Ube, JP), Kojima; Masahiro (Ube, JP), Onuma; Kazuhiro (Ube, JP), Shiraishi; Yusuke (Ube, JP), Okudo; Makoto (Ube, JP), Kimura; Tomio (Tokyo, JP)
Assignee:	UBE INDUSTRIES, LTD. (Yamaguchi, JP)
Application Number:	15/736,677
Patent Claims:	1. A compound represented by the formula (Ia) or a pharmacologically acceptable salt thereof: ##STR00264## wherein two R moieties each independently are a C.sub.1-3 alkyl group or are groups bonded to each other to form a C.sub.2-5 alkylene group; A is an optionally substituted C.sub.6-10 aryl group or an optionally substituted heteroaryl group, and Z is a hydrogen atom or an optionally substituted C.sub.1-6 alkyl group, or a group represented by Z--N-A forms an optionally substituted bicyclic fused heterocyclic group through the bonding between A and Z; and R.sup.1, R.sup.2 and R.sup.3 each independently are an optionally substituted linear or branched C.sub.1-4 alkyl group. 2. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is a compound represented by the formula(I) or a pharmacologically acceptable salt thereof: ##STR00265## wherein two R moieties each independently are a C.sub.1-3 alkyl group or are groups bonded to each other to form a C.sub.2-5 alkylene group; A is an optionally substituted C.sub.6-10 aryl group or an optionally substituted heteroaryl group; and R.sup.1, R.sup.2 and R.sup.3 each independently are an optionally substituted linear or branched C.sub.1-4 alkyl group. 3. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is a compound represented by the formula (IIa) or a pharmacologically acceptable salt thereof: ##STR00266## wherein A is an optionally substituted C.sub.6-10 aryl group or an optionally substituted heteroaryl group, and Z is a hydrogen atom or an optionally substituted C.sub.1-6 alkyl group, or a group represented by Z--N-A forms an optionally substituted bicyclic fused heterocyclic group through the bonding between A and Z; and R.sup.1, R.sup.2 and R.sup.3 each independently are an optionally substituted linear or branched C.sub.1-4 alkyl group. 4. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is a compound represented by the formula (II) or a pharmacologically acceptable salt thereof: ##STR00267## wherein A is an optionally substituted C.sub.6-10 aryl group or an optionally substituted heteroaryl group; and R.sup.1, R.sup.2 and R.sup.3 each independently are an optionally substituted linear or branched C.sub.1-4 alkyl group. 5. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is a compound represented by the formula (IIIa) or a pharmacologically acceptable salt thereof: ##STR00268## wherein A is an optionally substituted C.sub.6-10 aryl group or an optionally substituted heteroaryl group, and Z is a hydrogen atom or an optionally substituted C.sub.1-6 alkyl group, or a group represented by Z--N-A forms an optionally substituted bicyclic fused heterocyclic group through the bonding between A and Z; and R.sup.1, R.sup.2 and R.sup.3 each independently are an optionally substituted linear or branched C.sub.1-4 alkyl group. 6. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is a compound represented by the formula (III) or a pharmacologically acceptable salt thereof: ##STR00269## wherein A is an optionally substituted C.sub.6-10 aryl group or an optionally substituted heteroaryl group; and R.sup.1, R.sup.2 and R.sup.3 each independently are an optionally substituted linear or branched C.sub.1-4 alkyl group. 7. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is a compound represented by the formula (IVa) or a pharmacologically acceptable salt thereof: ##STR00270## wherein A is an optionally substituted C.sub.6-10 aryl group or an optionally substituted heteroaryl group, and Z is a hydrogen atom or an optionally substituted C.sub.1-6 alkyl group, or a group represented by Z--N-A forms an optionally substituted bicyclic fused heterocyclic group through the bonding between A and Z; and R.sup.1, R.sup.2 and R.sup.3 each independently are an optionally substituted linear or branched C.sub.1-4 alkyl group. 8. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is a compound represented by the formula (IV) or a pharmacologically acceptable salt thereof: ##STR00271## wherein A is an optionally substituted C.sub.6-10 aryl group or an optionally substituted heteroaryl group; and R.sup.1, R.sup.2 and R.sup.3 each independently are an optionally substituted linear or branched C.sub.14 alkyl group. 9. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is a compound selected from the compound group consisting of 6,6-Dimethyl-N-phenyl-3-[1-(trimethylsilyl)cyclobutanecarboxamido]-4,6-di- hydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, 6,6-Dimethyl-N-(p-tolyl)-3-[1-(trimethylsilyl)cyclobutanecarboxamido]-4,6- -dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(4-methoxyphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarboxam- ido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(4-fluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarboxami- do]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, 6,6-Dimethyl-N-(pyridin-3-yl)-3-[1-(trimethylsilyl)cyclobutanecarboxamido- ]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-fluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarboxami- do]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, 6,6-Dimethyl-N-(o-tolyl)-3-[1-(trimethylsilyl)cyclobutanecarboxamido]-4,6- -dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, 6,6-Dimethyl-N-(m-tolyl)-3-[1-(trimethylsilyl)cyclobutanecarboxamido]-4,6- -dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-([1,1'-biphenyl]-3-yl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecar- boxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(3-fluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarboxami- do]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(3-chlorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarboxami- do]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-methoxyphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarboxam- ido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-chlorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarboxami- do]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-([1,1'-biphenyl]-2-yl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecar- boxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, 6,6-Dimethyl-N-(pyridin-2-yl)-3-[1-(trimethylsilyl)cyclobutanecarboxamido- ]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-ethylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarboxamid- o]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2,6-dimethylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarbo- xamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2,3-difluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarbo- xamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2,3-dimethylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarbo- xamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-fluoro-6-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-[2-(difluoromethoxy)phenyl]-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobuta- necarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-ethoxyphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarboxami- do]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, 6,6-Dimethyl-N-[2-(trifluoromethoxy)phenyl]-3-[1-(trimethylsilyl)cyclobut- anecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-fluoro-4-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2,6-difluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarbo- xamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-[2-(tert-butyl)phenyl]-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecar- boxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, 6,6-Dimethyl-N-[2-(trifluoromethyl)phenyl]-3-[1-(trimethylsilyl)cyclobuta- necarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(3-fluoro-2-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-cyanophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarboxamid- o]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(4-fluoro-2-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-chloro-6-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-fluoro-3-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-fluoro-5-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(5-fluoro-2-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2,4-difluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarbo- xamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2,5-difluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarbo- xamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2,5-dimethylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarbo- xamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-chloro-6-fluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2,4-dimethylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarbo- xamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, 3-[1-(Ethyldimethylsilyl)cyclobutanecarboxamido]-N-(2-fluorophenyl)-6,6-d- imethyl-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, 6,6-Dimethyl-N-(3-methylisothiazol-4-yl)-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, 6,6-Dimethyl-N-(thiophen-2-yl)-3-[1-(trimethylsilyl)cyclobutanecarboxamid- o]-2,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, 6,6-Dimethyl-N-(thiophen-3-yl)-3-[1-(trimethylsilyl)cyclobutanecarboxamid- o]-2,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2,6-difluoro-4-methoxyphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclob- utanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-fluoro-6-methoxyphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutan- ecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-[2-fluoro-6-(trifluoromethyl)phenyl]-6,6-dimethyl-3-[1-(trimethylsilyl)- cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamid- e, N-(5-chloro-2-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobuta- necarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2,5-dichlorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarbo- xamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-cyclopropylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarb- oxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2,6-dichlorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarbo- xamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, 6,6-Dimethyl-N-(2,4,6-trifluorophenyl)-3-[1-(trimethylsilyl)cyclobutaneca- rboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-ethyl-6-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanec- arboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-bromophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarboxamid- o]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-chloro-5-fluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(5-chloro-2-fluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, 6,6-Dimethyl-N-(2,3,6-trifluorophenyl)-3-[1-(trimethylsilyl)cyclobutaneca- rboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-chloro-6-methoxyphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutan- ecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-[2-(1,1-difluoroethyl)phenyl]-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobu- tanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(6-chloro-2-fluoro-3-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cy- clobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-fluoro-6-(methoxy-d3)phenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclo- butanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-[2-chloro-6-(trifluoromethyl)phenyl]-6,6-dimethyl-3-[1-(trimethylsilyl)- cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamid- e, N-(2-fluoro-6-methoxy-3-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl- )cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxami- de, N-(2,6-difluoro-3-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cycl- obutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-[2-(difluoromethoxy)-6-fluorophenyl]-6,6-dimethyl-3-[1-(trimethylsilyl)- cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamid- e, N-(2-bromo-6-chlorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutan- ecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-chloro-6-fluoro-3-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cy- clobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-ethyl-6-fluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanec- arboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-bromo-6-fluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanec- arboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-bromo-6-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanec- arboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-chloro-5-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(6-fluoro-2,3-dihydrobenzofuran-7-yl)-6,6-dimethyl-3-[1-(trimethylsilyl- )cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxami- de, N-(2-cyano-6-fluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobuta- necarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-chloro-6-cyclopropylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclob- utanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-fluoro-3,6-dimethylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobu- tanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(6-fluorobenzofuran-7-yl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-chloro-3-fluoro-6-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cy- clobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-[2-(difluoromethoxy)-6-fluorophenyl]-6,6-dimethyl-3-[1-(trimethylsilyl)- cyclopropanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxami- de, N-(2,6-dichlorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclopropanec- arboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2,6-dichlorophenyl)-6,6-dimethyl-3-[2-methyl-2-(trimethylsilyl)propane- amido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-[2-(difluoromethoxy)-6-fluorophenyl]-6,6-dimethyl-3-[2-methyl-2-(trimet- hylsilyl)propaneamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide- , N-(2,6-dichloro-4-fluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclob- utanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-ethyl-6-fluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclopropane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-bromo-6-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclopropane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-chloro-5-methoxyphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutan- ecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-ethyl-6-fluorophenyl)-6,6-dimethyl-3-[2-methyl-2-(trimethylsilyl)pro- paneamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-bromo-6-methylphenyl)-6,6-dimethyl-3-[2-methyl-2-(trimethylsilyl)pro- paneamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(6-fluorobenzofuran-7-yl)-6,6-dimethyl-3-[2-methyl-2-(trimethylsilyl)pr- opaneamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(6-fluorobenzofuran-7-yl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclopropan- ecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N,6,6-trimethyl-N-phenyl-3-[1-(trimethylsilyl)cyclobutanecarboxamido]-4,6- -dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(6-fluoro-3-methylbenzofuran-7-yl)-6,6-dimethyl-3-[1-(trimethylsilyl)cy- clobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-(2-chloro-6-fluorobenzofuran-7-yl)-6,6-dimethyl-3-[1-(trimethylsilyl)cy- clobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide, N-[5-(indoline-1-carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]p- yrazol-3-yl]-1-(trimethylsilyl)cyclobutanecarboxamide, N-[5-(3,4-dihydro-2H-benzo[b][1,4]oxazine-4-carbonyl)-6,6-dimethyl-1,4,5,- 6-tetrahydropyrrolo[3,4-c]pyrazol-3-yl]-1-(trimethylsilyl)cyclobutanecarbo- xamide, N-(6-fluoro-2-methylbenzofuran-7-yl)-6,6-dimethyl-3-[1-(trimethyls- ilyl)cyclobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carbo- xamide, and N-[5-(1H-indole-1-carbonyl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]- pyrazol-3-yl]-1-(trimethylsilyl)cyclobutanecarboxamide or a pharmacologically acceptable salt thereof. 10. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is N-(2-fluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarboxami- do]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide or a pharmacologically acceptable salt thereof. 11. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is 6,6-Dimethyl-N-(o-tolyl)-3-[1-(trimethylsilyl)cyclobutanecarboxamido]-4,6- -dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide or a pharmacologically acceptable salt thereof. 12. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is N-(2-chloro-6-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide or a pharmacologically acceptable salt thereof. 13. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is N-(5-fluoro-2-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide or a pharmacologically acceptable salt thereof. 14. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is N-(2,5-dimethylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanecarbo- xamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide or a pharmacologically acceptable salt thereof. 15. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is N-(2-chloro-6-fluorophenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide or a pharmacologically acceptable salt thereof. 16. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is N-(2-bromo-6-methylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutanec- arboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide or a pharmacologically acceptable salt thereof. 17. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is N-(2-fluoro-3,6-dimethylphenyl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobu- tanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide or a pharmacologically acceptable salt thereof. 18. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is N-(6-fluorobenzofuran-7-yl)-6,6-dimethyl-3-[1-(trimethylsilyl)cyclobutane- carboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide or a pharmacologically acceptable salt thereof. 19. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is N-(2-chloro-6-fluorobenzofuran-7-yl)-6,6-dimethyl-3-[1-(trimethylsilyl)cy- clobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide or a pharmacologically acceptable salt thereof. 20. The compound or a pharmacologically acceptable salt thereof according to claim 1, wherein the compound or a pharmacologically acceptable salt thereof is N-(6-fluoro-2-methylbenzofuran-7-yl)-6,6-dimethyl-3-[1-(trimethylsilyl)cy- clobutanecarboxamido]-4,6-dihydropyrrolo[3,4-c]pyrazole-5(1H)-carboxamide or a pharmacologically acceptable salt thereof. 21. A pharmaceutical composition comprising a compound or a pharmacologically acceptable salt thereof according to claim 1. 22. The pharmaceutical composition according to claim 21, wherein the pharmaceutical composition is a CDK7 inhibitor. 23. The pharmaceutical composition according to claim 21, wherein the pharmaceutical composition is the treatment of a CDK7-related disease, wherein the disease is selected from a cancer, an inflammatory disease, an allergic disease or a chronic respiratory disease, wherein treatment is achieved by inhibiting CDK7. 24. The pharmaceutical composition according to claim 23, wherein the cancer is selected from the group consisting of urinary bladder cancer, breast cancer, large intestine cancer, kidney cancer, liver cancer, lung cancer, esophageal cancer, gallbladder cancer, ovary cancer, pancreatic cancer, gastric cancer, cervical cancer, thyroid gland cancer, head and neck cancer, prostate cancer, skin cancer, hematopoietic organ tumors of the lymphatic system, hematopoietic organ tumors of the myeloid system, mesenchymal tumors, tumors of the central or peripheral nervous system, teratoma, osteosarcoma, and Kaposi's sarcoma. 25. The pharmaceutical composition according to claim 21, wherein the pharmaceutical composition is for administering in combination with one or more additional drug(s) selected from the group consisting of anticancer agents, antirheumatic agents, drugs for the treatment of psoriasis, drugs for the treatment of multiple sclerosis, drugs for the treatment of inflammatory bowel disease, drugs for the treatment of chronic obstructive pulmonary disease and drugs for the treatment of atopic dermatitis. 26. The pharmaceutical composition according to claim 21, wherein the pharmaceutical composition is for administering at the same time with or at a different time from a composition comprising, as an active ingredient, one or more additional drug(s) selected from the group consisting of anticancer agents, antirheumatic agents, drugs for the treatment of psoriasis, drugs for the treatment of multiple sclerosis, drugs for the treatment of inflammatory bowel disease, drugs for the treatment of chronic obstructive pulmonary disease and drugs for the treatment of atopic dermatitis. 27. The pharmaceutical composition according to claim 21, further comprising, as an active ingredient, one or more additional drug(s) selected from the group consisting of anticancer agents, antirheumatic agents, drugs for the treatment of psoriasis, drugs for the treatment of multiple sclerosis, drugs for the treatment of inflammatory bowel disease, drugs for the treatment of chronic obstructive pulmonary disease and drugs for the treatment of atopic dermatitis. 28. The pharmaceutical composition according to claim 21, wherein the pharmaceutical composition is for administering in combination with one or more additional drug(s) selected from the group consisting of tyrosine kinase inhibitors, immune checkpoint inhibitors, DNA alkylating agents, DNA synthesis inhibitors, platinum-containing drugs, antimetabolites, topoisomerase I inhibitors, topoisomerase II inhibitors, tubulin activator, hormone antagonists, aromatase inhibitors, differentiation inducers, proteosome inhibitors, phospholipid kinase inhibitors, adenosine deaminase inhibitors, antiangiogenic agents, histone deacetylase (HDAC) inhibitors, BET bromodomain inhibitors, histone demethylase inhibitors, histone methyltransferase inhibitors, matrix metalloprotease inhibitors, farnesyltransferase inhibitors, bisphosphonate preparations, Hsp90 inhibitors, kinesin Eg5 inhibitors, serine threonine kinase inhibitors, anticytokine agents, immunosuppressants, immunomodulators, active form of vitamin D3 external agent, S1P1 receptor antagonists, interferon preparations, anticholinergic drugs, leukotriene antagonists, PDE4 inhibitors, PGD2 receptor antagonists, neutrophil elastase inhibitors, antihistamine agents, classical non-steroidal anti-inflammatory drugs, cyclooxygenase inhibitors, nitric oxide-releasing non-steroidal anti-inflammatory drugs, gold preparations, penicillamine, aminosalicylic acid preparations, antimalarial drugs, pyrimidine synthesis inhibitors, TNF inhibitors, interleukin inhibitors, interleukin receptor antagonists, interleukin drugs, B-cell activation inhibitors, costimulatory molecule-related protein preparations, MAPK inhibitors, gene regulation drugs, cytokine production inhibitors, TNF-.alpha.-converting enzyme inhibitors, interleukin-1.beta.-converting enzyme inhibitors, chemokine antagonists, therapeutic vaccine, gene therapy, antisense compounds, proteasome inhibitors, JAK inhibitors, T cell inhibitors, inosine monophosphate dehydrogenase (IMPDH) inhibitors, adhesion molecule inhibitors, thalidomide, cathepsin inhibitors, glucose-6-phosphate dehydrogenase inhibitors, dihydroorotate dehydrogenase (DHODH) inhibitors, phospholipase A2 inhibitors, iNOS inhibitors, microtubule stimulants, anti-microtubule agents, MHC class II antagonists, CD4 antagonists, CD23 antagonists, leukotriene B4 receptor antagonists, 5-lipoxygenase inhibitors, cathepsin B inhibitors, osteogenesis stimulators, dipeptidyl peptidase inhibitors, collagen agonists, capsaicin creams, sulfa drugs, hyaluronic acid derivatives, glucosamine sulfate, amiprilose, CD20 inhibitors, CD52 inhibitors, anti-asthmatic drugs, drugs for the treatment of atopic dermatitis, drugs for the treatment of allergic rhinitis, opioid receptor agonists, immunoglobulins, glatiramer acetate, T cell receptor vaccines, adhesion molecule inhibitors, muscle relaxants, local anesthetics, ketamine, short-acting or long-acting muscarine receptor antagonists, short-acting and long-acting .beta. receptor agonists, inhaled steroids, oral steroids, combination drugs of .beta. receptor agonists and inhaled steroids, vitamin derivatives and adrenocortical steroids. 29. The pharmaceutical composition according to claim 21, wherein the pharmaceutical composition is for administering in combination with one or more additional drug(s) selected from the group consisting of cisplatin, doxorubicin, Taxotere, Taxol, etoposide, irinotecan, topotecan, paclitaxel, docetaxel, epothilone, tamoxifen, 5-fluorouracil, fingolimod, methotrexate, temozolomide, cyclophosphamide, SCH 66336, R115777, L778,123, BMS 214662, gefitinib, erlotinib, panitumumab, afatinib, dasatinib, bosutinib, vandetanib, sunitinib, axitinib, pazopanib, lenvatinib, lapatinib, nintedanib, nilotinib, crizotinib, ceritinib, alectinib, ibrutinib, imatinib, sorafenib, vemurafenib, dabrafenib, trametinib, palbociclib, interferon alpha-2b, cytarabine, adriamycin, Cytoxan, gemcitabine, uracil mustard, chlormethine, ifosfamide, melphalan, chlorambucil, pipobroman, triethylenemelamine, triethylenethiophosphoramine, ofatumumab, busulfan, carmustine, lomustine, streptozocin, dacarbazine, floxuridine, 6-mercaptopurine, 6-thioguanine, regorafenib, ramucirumab, fludarabine phosphate, oxaliplatin, folinate, pentostatin, vinblastine, vincristine, vindesine, bleomycin, dactinomycin, daunorubicin, doxorubicin, epirubicin, idarubicin, mithramycin, deoxycoformycin, mitomycin-C, L-asparaginase, teniposide, 17.alpha.-ethinylestradiol, diethylstilbestrol, testosterone, prednisone, fluoxymesterone, drostanolone propionate, testolactone, megestrol acetate, methylprednisolone, methyltestosterone, prednisolone, chlorotrianisene, hydroxyprogesterone, aminoglutethimide, estramustine, medroxyprogesterone acetate, leuprolide acetate, flutamide, toremifene, goserelin, carboplatin, hydroxyurea, amsacrine, procarbazine, mitotane, mitoxantrone, levamisole, Navelbine, anastrozole, letrozole, capecitabine, reloxafine, droloxifene, hexamethylmelamine, bevacizumab, omalizumab, mepolizumab, gemtuzumab ozogamicin, mogamulizumab, pertuzumab, ocrelizumab, alemtuzumab, inotuzumab, tositumomab, bortezomib, ibritumomab tiuxetan, diarsenic trioxide, vinorelbine, porfimer sodium, thiotepa, altretamine, trastuzumab, letrozole, fulvestrant, exemestane, rituximab, cetuximab, basiliximab, nivolumab, ipilimumab, pembrolizumab, durvalumab, atezolizumab, avelumab, alcofenac, aceclofenac, sulindac, tolmetin, etodolac, fenoprofen, tiaprofenic acid, meclofenamic acid, meloxicam, tenoxicam, lornoxicam, nabumetone, acetaminophen, phenacetin, ethenzamide, sulpyrine, antipyrine, migrenin, aspirin, mefenamic acid, flufenamic acid, phenylbutazone, indomethacin, ibuprofen, ketoprofen, naproxen, oxaprozin, flurbiprofen, fenbufen, pranoprofen, floctafenine, piroxicam, epirizole, tiaramide hydrochloride, zaltoprofen, gabexate mesilate, camostat mesilate, ulinastatin, colchicine, probenecid, sulfinpyrazone, benzbromarone, allopurinol, brentuximab vedotin, gold sodium thiomalate, sodium hyaluronate, atropine, scopolamine, morphine or salts thereof, pethidine, levorphanol, oxymorphone, celecoxib, etoricoxib, valdecoxib, loxoprofen, auranofin, D-penicillamine, sulfasalazine, mesalazine, olsalazine, balsalazide, chloroquine, leflunomide, tacrolimus, infliximab, etanercept, adalimumab, certolizumab pegol, golimumab, PASSTNF-.alpha., soluble TNF-.alpha. receptor, TNF-.alpha.-binding protein, anti-TNF-.alpha. antibodies, denosumab, anakinra, antibodies against soluble interleukin-1 receptor, tocilizumab, anti-interleukin-6 antibodies, interleukin-10, ustekinumab, briakinumab, secukinumab (AIN-457), ixekizumab (LY-2439821), AMG827, Rituxan, belimumab, abatacept, BMS-582949, inhibitors of molecules involved in signal transduction, MAPK inhibitors, salicylic acid ointments, urea ointments, iguratimod, tetomilast, belnacasan, HMPL-004, IL-8 antagonists, CXCR1-CXCR2 dual antagonists, reparixin, CCR9 antagonists, denileukin diftitox, CCX025, N-{4-chloro-2-[(1-oxidopyridin-4-yl)carbonyl]phenyl}-4-(propan-2-yloxy)be- nzenesulfonamide, MCP-1 antagonists, irbesartan, TNF-.alpha. vaccines, ISIS-104838, natalizumab, vedolizumab, AJM300, TRK-170, E6007, MX-68, BMS-188667, CKD-461, rimexolone, cyclosporine A, mizoribine, gusperimus, sirolimus, temsirolimus, everolimus, antilymphocyte serum, freeze-dried sulfonated normal immunoglobulin, erythropoietin, colony-stimulating factors, atiprimod dihydrochloride, azathioprine, interferon .alpha., interferon .beta.-1b, interferon .beta.-1a, tofacitinib, baricitinib, carfilzomib, ruxolitinib, dexamethasone, hexestrol, methimazole, betamethasone, triamcinolone acetonide, fluocinonide, fluocinolone acetonide, cortisone acetate, hydrocortisone, fluorometholone, beclomethasone propionate, estriol, mycophenolate mofetil, alicaforsen sodium, selectin inhibitors, ELAM-1 inhibitors, VCAM-1 inhibitors, ICAM-1 inhibitors, V-85546, roflumilast, apremilast, VAS203, reumacon, zanolimumab, DW-1350, zileuton, Tyk2 inhibitors, Synvisc (hylan G-F 20), Orthovisc, atacicept, blisibimod, tizanidine, eperisone, afloqualone, baclofen, diazepam, dantrolene sodium, vitamin D3 derivatives, vitamin D2 derivatives, isoprenaline hydrochloride, salbutamol sulfate, procaterol hydrochloride, terbutaline sulfate, trimetoquinol hydrochloride, tulobuterol hydrochloride, orciprenaline sulfate, fenoterol hydrobromide, ephedrine hydrochloride, ipratropium bromide, oxitropium bromide, flutropium bromide, theophylline, aminophylline, sodium cromoglicate, tranilast, repirinast, amlexanox, ibudilast, ketotifen, terfenadine, mequitazine, azelastine, ozagrel hydrochloride, pranlukast hydrate, seratrodast, ciclesonide, chlorpheniramine maleate, alimemazine tartrate, clemastine fumarate, homochlorcyclizine hydrochloride, fexofenadine, ketotifen fumarate, cetirizine hydrochloride, oxatomide, ebastine, epinastine hydrochloride, loratadine, tramadol, promethazine, hydroxyzine, homochlorcyclizine, cyproheptadine, mequitazine, emedastine fumarate, pseudoephedrine, bepotastine besilate, levocetirizine, olopatadine hydrochloride, mycophenolate mofetil, daclizumab, galiximab, metformin hydrochloride, visilizumab, aminopterin, pazopanib hydrochloride, fezakinumab, ruxolitinib phosphate, ixekizumab, guselkumab, SLx-2119, PRX-167700, lidocaine, tiotropium bromide, salmeterol xinafoate, formoterol fumarate, fluticasone propionate, beclometasone propionate, budesonide, and combination drugs of salmeterol xinafoate and fluticasone propionate. 30. The pharmaceutical composition according to claim 21, wherein the pharmaceutical composition is for administering at the same time with or at a different time from a composition comprising, as an active ingredient, one or more additional drug(s) selected from the group consisting of tyrosine kinase inhibitors, immune checkpoint inhibitors, DNA alkylating agents, DNA synthesis inhibitors, platinum-containing drugs, antimetabolites, topoisomerase I inhibitors, topoisomerase II inhibitors, tubulin activator, hormone antagonists, aromatase inhibitors, differentiation inducers, proteosome inhibitors, phospholipid kinase inhibitors, adenosine deaminase inhibitors, antiangiogenic agents, histone deacetylase (HDAC) inhibitors, BET bromodomain inhibitors, histone demethylase inhibitors, histone methyltransferase inhibitors, matrix metalloprotease inhibitors, farnesyltransferase inhibitors, bisphosphonate preparations, Hsp90 inhibitors, kinesin Eg5 inhibitors, serine threonine kinase inhibitors, anticytokine agents, immunosuppressants, immunomodulators, active form of vitamin D3 external agent, S1P1 receptor antagonists, interferon preparations, anticholinergic drugs, leukotriene antagonists, PDE4 inhibitors, PGD2 receptor antagonists, neutrophil elastase inhibitors, antihistamine agents, classical non-steroidal anti-inflammatory drugs, cyclooxygenase inhibitors, nitric oxide-releasing non-steroidal anti-inflammatory drugs, gold preparations, penicillamine, aminosalicylic acid preparations, antimalarial drugs, pyrimidine synthesis inhibitors, TNF inhibitors, interleukin inhibitors, interleukin receptor antagonists, interleukin drugs, B-cell activation inhibitors, costimulatory molecule-related protein preparations, MAPK inhibitors, gene regulation drugs, cytokine production inhibitors, TNF-.alpha.-converting enzyme inhibitors, interleukin-1.beta.-converting enzyme inhibitors, chemokine antagonists, therapeutic vaccine, gene therapy, antisense compounds, proteasome inhibitors, JAK inhibitors, T cell inhibitors, inosine monophosphate dehydrogenase (IMPDH) inhibitors, adhesion molecule inhibitors, thalidomide, cathepsin inhibitors, glucose-6-phosphate dehydrogenase inhibitors, dihydroorotate dehydrogenase (DHODH) inhibitors, phospholipase A2 inhibitors, iNOS inhibitors, microtubule stimulants, anti-microtubule agents, MHC class II antagonists, CD4 antagonists, CD23 antagonists, leukotriene B4 receptor antagonists, 5-lipoxygenase inhibitors, cathepsin B inhibitors, osteogenesis stimulators, dipeptidyl peptidase inhibitors, collagen agonists, capsaicin creams, sulfa drugs, hyaluronic acid derivatives, glucosamine sulfate, amiprilose, CD20 inhibitors, CD52 inhibitors, anti-asthmatic drugs, drugs for the treatment of atopic dermatitis, drugs for the treatment of allergic rhinitis, opioid receptor agonists, immunoglobulins, glatiramer acetate, T cell receptor vaccines, adhesion molecule inhibitors, muscle relaxants, local anesthetics, ketamine, short-acting or long-acting muscarine receptor antagonists, short-acting and long-acting .beta. receptor agonists, inhaled steroids, oral steroids, combination drugs of .beta. receptor agonists and inhaled steroids, vitamin derivatives and adrenocortical steroids. 31. The pharmaceutical composition according to claim 21, wherein the pharmaceutical composition is for administering at the same time with or at a different time from a composition comprising, as an active ingredient, one or more additional drug(s) selected from the group consisting of cisplatin, doxorubicin, Taxotere, Taxol, etoposide, irinotecan, topotecan, paclitaxel, docetaxel, epothilone, tamoxifen, 5-fluorouracil, fingolimod, methotrexate, temozolomide, cyclophosphamide, SCH 66336, R115777, L778,123, BMS 214662, gefitinib, erlotinib, panitumumab, afatinib, dasatinib, bosutinib, vandetanib, sunitinib, axitinib, pazopanib, lenvatinib, lapatinib, nintedanib, nilotinib, crizotinib, ceritinib, alectinib, ibrutinib, imatinib, sorafenib, vemurafenib, dabrafenib, trametinib, palbociclib, interferon alpha-2b, cytarabine, adriamycin, Cytoxan, gemcitabine, uracil mustard, chlormethine, ifosfamide, melphalan, chlorambucil, pipobroman, triethylenemelamine, triethylenethiophosphoramine, ofatumumab, busulfan, carmustine, lomustine, streptozocin, dacarbazine, floxuridine, 6-mercaptopurine, 6-thioguanine,regorafenib, ramucirumab, fludarabine phosphate, oxaliplatin, folinate, pentostatin, vinblastine, vincristine, vindesine, bleomycin, dactinomycin, daunorubicin, doxorubicin, epirubicin, idarubicin, mithramycin, deoxycoformycin, mitomycin-C, L-asparaginase, teniposide, 17.alpha.-ethinylestradiol, diethylstilbestrol, testosterone, prednisone, fluoxymesterone, drostanolone propionate, testolactone, megestrol acetate, methylprednisolone, methyltestosterone, prednisolone, chlorotrianisene, hydroxyprogesterone, aminoglutethimide, estramustine, medroxyprogesterone acetate, leuprolide acetate, flutamide, toremifene, goserelin, carboplatin, hydroxyurea, amsacrine, procarbazine, mitotane, mitoxantrone, levamisole, Navelbine, anastrozole, letrozole, capecitabine, reloxafine, droloxifene, hexamethylmelamine, bevacizumab, omalizumab, mepolizumab, gemtuzumab ozogamicin, mogamulizumab, pertuzumab, ocrelizumab, alemtuzumab, inotuzumab, tositumomab, bortezomib, ibritumomab tiuxetan, diarsenic trioxide, vinorelbine, porfimer sodium, thiotepa, altretamine, trastuzumab, letrozole, fulvestrant, exemestane, rituximab, cetuximab, basiliximab, nivolumab, ipilimumab, pembrolizumab, durvalumab, atezolizumab, avelumab, alcofenac, aceclofenac, sulindac, tolmetin, etodolac, fenoprofen, tiaprofenic acid, meclofenamic acid, meloxicam, tenoxicam, lornoxicam, nabumetone, acetaminophen, phenacetin, ethenzamide, sulpyrine, antipyrine, migrenin, aspirin, mefenamic acid, flufenamic acid, phenylbutazone, indomethacin, ibuprofen, ketoprofen, naproxen, oxaprozin, flurbiprofen, fenbufen, pranoprofen, floctafenine, piroxicam, epirizole, tiaramide hydrochloride, zaltoprofen, gabexate mesilate, camostat mesilate, ulinastatin, colchicine, probenecid, sulfinpyrazone, benzbromarone, allopurinol, brentuximab vedotin, gold sodium thiomalate, sodium hyaluronate, atropine, scopolamine, morphine or salts thereof, pethidine, levorphanol, oxymorphone, celecoxib, etoricoxib, valdecoxib, loxoprofen, auranofin, D-penicillamine, sulfasalazine, mesalazine, olsalazine, balsalazide, chloroquine, leflunomide, tacrolimus, infliximab, etanercept, adalimumab, certolizumab pegol, golimumab, PASSTNF-.alpha., soluble TNF-.alpha. receptor, TNF-.alpha.-binding protein, anti-TNF-.alpha. antibodies, denosumab, anakinra, antibodies against soluble interleukin-1 receptor, tocilizumab, anti-interleukin-6 antibodies, interleukin-10, ustekinumab, briakinumab, secukinumab (AIN-457), ixekizumab (LY-2439821), AMG827, Rituxan, belimumab, abatacept, BMS-582949, inhibitors of molecules involved in signal transduction, MAPK inhibitors, salicylic acid ointments, urea ointments, iguratimod, tetomilast, belnacasan, HMPL-004, IL-8 antagonists, CXCR1-CXCR2 dual antagonists, reparixin, CCR9 antagonists, denileukin diftitox, CCX025, N-{4-chloro-2-[(1-oxidopyridin-4-yl)carbonyl]phenyl}-4-(propan-2-yloxy)be- nzenesulfonamide, MCP-1 antagonists, irbesartan, TNF-.alpha. vaccines, ISIS-104838, natalizumab, vedolizumab, AJM300, TRK-170, E6007, MX-68, BMS-188667, CKD-461, rimexolone, cyclosporine A, mizoribine, gusperimus, sirolimus, temsirolimus, everolimus, antilymphocyte serum, freeze-dried sulfonated normal immunoglobulin, erythropoietin, colony-stimulating factors, atiprimod dihydrochloride, azathioprine, interferon .alpha., interferon .beta.-1b, interferon .beta.-1a, tofacitinib, baricitinib, carfilzomib, ruxolitinib, dexamethasone, hexestrol, methimazole, betamethasone, triamcinolone acetonide, fluocinonide, fluocinolone acetonide, cortisone acetate, hydrocortisone, fluorometholone, beclomethasone propionate, estriol, mycophenolate mofetil, alicaforsen sodium, selectin inhibitors, ELAM-1 inhibitors, VCAM-1 inhibitors, ICAM-1 inhibitors, V-85546, roflumilast, apremilast, VAS203, reumacon, zanolimumab, DW-1350, zileuton, Tyk2 inhibitors, Synvisc (hylan G-F 20), Orthovisc, atacicept, blisibimod, tizanidine, eperisone, afloqualone, baclofen, diazepam, dantrolene sodium, vitamin D3 derivatives, vitamin D2 derivatives, isoprenaline hydrochloride, salbutamol sulfate, procaterol hydrochloride, terbutaline sulfate, trimetoquinol hydrochloride, tulobuterol hydrochloride, orciprenaline sulfate, fenoterol hydrobromide, ephedrine hydrochloride, ipratropium bromide, oxitropium bromide, flutropium bromide, theophylline, aminophylline, sodium cromoglicate, tranilast, repirinast, amlexanox, ibudilast, ketotifen, terfenadine, mequitazine, azelastine, ozagrel hydrochloride, pranlukast hydrate, seratrodast, ciclesonide, chlorpheniramine maleate, alimemazine tartrate, clemastine fumarate, homochlorcyclizine hydrochloride, fexofenadine, ketotifen fumarate, cetirizine hydrochloride, oxatomide, ebastine, epinastine hydrochloride, loratadine, tramadol, promethazine, hydroxyzine, homochlorcyclizine, cyproheptadine, mequitazine, emedastine fumarate, pseudoephedrine, bepotastine besilate, levocetirizine, olopatadine hydrochloride, mycophenolate mofetil, daclizumab, galiximab, metformin hydrochloride, visilizumab, aminopterin, pazopanib hydrochloride, fezakinumab, ruxolitinib phosphate, ixekizumab, guselkumab, SLx-2119, PRX-167700, lidocaine, tiotropium bromide, salmeterol xinafoate, formoterol fumarate, fluticasone propionate, beclometasone propionate, budesonide, and combination drugs of salmeterol xinafoate and fluticasone propionate. 32. The pharmaceutical composition according to claim 21, further comprising, as an active ingredient, one or more additional drug(s) selected from the group consisting of tyrosine kinase inhibitors, immune checkpoint inhibitors, DNA alkylating agents, DNA synthesis inhibitors, platinum-containing drugs, antimetabolites, topoisomerase I inhibitors, topoisomerase II inhibitors, tubulin activator, hormone antagonists, aromatase inhibitors, differentiation inducers, proteosome inhibitors, phospholipid kinase inhibitors, adenosine deaminase inhibitors, antiangiogenic agents, histone deacetylase (HDAC) inhibitors, BET bromodomain inhibitors, histone demethylase inhibitors, histone methyltransferase inhibitors, matrix metalloprotease inhibitors, farnesyltransferase inhibitors, bisphosphonate preparations, Hsp90 inhibitors, kinesin Eg5 inhibitors, serine threonine kinase inhibitors, anticytokine agents, immunosuppressants, immunomodulators, active form of vitamin D3 external agent, S1P1 receptor antagonists, interferon preparations, anticholinergic drugs, leukotriene antagonists, PDE4 inhibitors, PGD2 receptor antagonists, neutrophil elastase inhibitors, antihistamine agents, classical non-steroidal anti-inflammatory drugs, cyclooxygenase inhibitors, nitric oxide-releasing non-steroidal anti-inflammatory drugs, gold preparations, penicillamine, aminosalicylic acid preparations, antimalarial drugs, pyrimidine synthesis inhibitors, TNF inhibitors, interleukin inhibitors, interleukin receptor antagonists, interleukin drugs, B-cell activation inhibitors, costimulatory molecule-related protein preparations, MAPK inhibitors, gene regulation drugs, cytokine production inhibitors, TNF-.alpha.-converting enzyme inhibitors, interleukin-1.beta.-converting enzyme inhibitors, chemokine antagonists, therapeutic vaccine, gene therapy, antisense compounds, proteasome inhibitors, JAK inhibitors, T cell inhibitors, inosine monophosphate dehydrogenase (IMPDH) inhibitors, adhesion molecule inhibitors, thalidomide, cathepsin inhibitors, glucose-6-phosphate dehydrogenase inhibitors, dihydroorotate dehydrogenase (DHODH) inhibitors, phospholipase A2 inhibitors, iNOS inhibitors, microtubule stimulants, anti-microtubule agents, MHC class II antagonists, CD4 antagonists, CD23 antagonists, leukotriene B4 receptor antagonists, 5-lipoxygenase inhibitors, cathepsin B inhibitors, osteogenesis stimulators, dipeptidyl peptidase inhibitors, collagen agonists, capsaicin creams, sulfa drugs, hyaluronic acid derivatives, glucosamine sulfate, amiprilose, CD20 inhibitors, CD52 inhibitors, anti-asthmatic drugs, drugs for the treatment of atopic dermatitis, drugs for the treatment of allergic rhinitis, opioid receptor agonists, immunoglobulins, glatiramer acetate, T cell receptor vaccines, adhesion molecule inhibitors, muscle relaxants, local anesthetics, ketamine, short-acting or long-acting muscarine receptor antagonists, short-acting and long-acting .beta. receptor agonists, inhaled steroids, oral steroids, combination drugs of .beta. receptor agonists and inhaled steroids, vitamin derivatives and adrenocortical steroids. 33. The pharmaceutical composition according to claim 21, further comprising, as an active ingredient, one or more additional drug(s) selected from the group consisting of cisplatin, doxorubicin, Taxotere, Taxol, etoposide, irinotecan, topotecan, paclitaxel, docetaxel, epothilone, tamoxifen, 5-fluorouracil, fingolimod, methotrexate, temozolomide, cyclophosphamide, SCH 66336, R115777, L778,123, BMS 214662, gefitinib, erlotinib, panitumumab, afatinib, dasatinib, bosutinib, vandetanib, sunitinib, axitinib, pazopanib, lenvatinib, lapatinib, nintedanib, nilotinib, crizotinib, ceritinib, alectinib, ibrutinib, imatinib, sorafenib, vemurafenib, dabrafenib, trametinib, palbociclib, interferon alpha-2b, cytarabine, adriamycin, Cytoxan, gemcitabine, uracil mustard, chlormethine, ifosfamide, melphalan, chlorambucil, pipobroman, triethylenemelamine, triethylenethiophosphoramine, ofatumumab, busulfan, carmustine, lomustine, streptozocin, dacarbazine, floxuridine, 6-mercaptopurine, 6-thioguanine, regorafenib, ramucirumab, fludarabine phosphate, oxaliplatin, folinate, pentostatin, vinblastine, vincristine, vindesine, bleomycin, dactinomycin, daunorubicin, doxorubicin, epirubicin, idarubicin, mithramycin, deoxycoformycin, mitomycin-C, L-asparaginase, teniposide, 17.alpha.-ethinylestradiol, diethylstilbestrol, testosterone, prednisone, fluoxymesterone, drostanolone propionate, testolactone, megestrol acetate, methylprednisolone, methyltestosterone, prednisolone, chlorotrianisene, hydroxyprogesterone, aminoglutethimide, estramustine, medroxyprogesterone acetate, leuprolide acetate, flutamide, toremifene, goserelin, carboplatin, hydroxyurea, amsacrine, procarbazine, mitotane, mitoxantrone, levamisole, Navelbine, anastrozole, letrozole, capecitabine, reloxafine, droloxifene, hexamethylmelamine, bevacizumab, omalizumab, mepolizumab, gemtuzumab ozogamicin, mogamulizumab, pertuzumab, ocrelizumab, alemtuzumab, inotuzumab, tositumomab, bortezomib, ibritumomab tiuxetan, diarsenic trioxide, vinorelbine, porfimer sodium, thiotepa, altretamine, trastuzumab, letrozole, fulvestrant, exemestane, rituximab, cetuximab, basiliximab, nivolumab, ipilimumab, pembrolizumab, durvalumab, atezolizumab, avelumab, alcofenac, aceclofenac, sulindac, tolmetin, etodolac, fenoprofen, tiaprofenic acid, meclofenamic acid, meloxicam, tenoxicam, lornoxicam, nabumetone, acetaminophen, phenacetin, ethenzamide, sulpyrine, antipyrine, migrenin, aspirin, mefenamic acid, flufenamic acid, phenylbutazone, indomethacin, ibuprofen, ketoprofen, naproxen, oxaprozin, flurbiprofen, fenbufen, pranoprofen, floctafenine, piroxicam, epirizole, tiaramide hydrochloride, zaltoprofen, gabexate mesilate, camostat mesilate, ulinastatin, colchicine, probenecid, sulfinpyrazone, benzbromarone, allopurinol, brentuximab vedotin, gold sodium thiomalate, sodium hyaluronate, atropine, scopolamine, morphine or salts thereof, pethidine, levorphanol, oxymorphone, celecoxib, etoricoxib, valdecoxib, loxoprofen, auranofin, D-penicillamine, sulfasalazine, mesalazine, olsalazine, balsalazide, chloroquine, leflunomide, tacrolimus, infliximab, etanercept, adalimumab, certolizumab pegol, golimumab, PASSTNF-.alpha., soluble TNF-.alpha. receptor, TNF-.alpha.-binding protein, anti-TNF-.alpha. antibodies, denosumab, anakinra, antibodies against soluble interleukin-1 receptor, tocilizumab, anti-interleukin-6 antibodies, interleukin-10, ustekinumab, briakinumab, secukinumab (AIN-457), ixekizumab (LY-2439821), AMG827, Rituxan, belimumab, abatacept, BMS-582949, inhibitors of molecules involved in signal transduction, MAPK inhibitors, salicylic acid ointments, urea ointments, iguratimod, tetomilast, belnacasan, HMPL-004, IL-8 antagonists, CXCR1-CXCR2 dual antagonists, reparixin, CCR9 antagonists, denileukin diftitox, CCX025, N-{4-chloro-2-[(1-oxidopyridin-4-yl)carbonyl]phenyl}-4-(propan-2-yloxy)be- nzenesulfonamide, MCP-1 antagonists, irbesartan, TNF-.alpha. vaccines, ISIS-104838, natalizumab, vedolizumab, AJM300, TRK-170, E6007, MX-68, BMS-188667, CKD-461, rimexolone, cyclosporine A, mizoribine, gusperimus, sirolimus, temsirolimus, everolimus, antilymphocyte serum, freeze-dried sulfonated normal immunoglobulin, erythropoietin, colony-stimulating factors, atiprimod dihydrochloride, azathioprine, interferon .alpha., interferon .beta.-1b, interferon .beta.-1a, tofacitinib, baricitinib, carfilzomib, ruxolitinib, dexamethasone, hexestrol, methimazole, betamethasone, triamcinolone acetonide, fluocinonide, fluocinolone acetonide, cortisone acetate, hydrocortisone, fluorometholone, beclomethasone propionate, estriol, mycophenolate mofetil, alicaforsen sodium, selectin inhibitors, ELAM-1 inhibitors, VCAM-1 inhibitors, ICAM-1 inhibitors, V-85546, roflumilast, apremilast, VAS203, reumacon, zanolimumab, DW-1350, zileuton, Tyk2 inhibitors, Synvisc (hylan G-F 20), Orthovisc, atacicept, blisibimod, tizanidine, eperisone, afloqualone, baclofen, diazepam, dantrolene sodium, vitamin D3 derivatives, vitamin D2 derivatives, isoprenaline hydrochloride, salbutamol sulfate, procaterol hydrochloride, terbutaline sulfate, trimetoquinol hydrochloride, tulobuterol hydrochloride, orciprenaline sulfate, fenoterol hydrobromide, ephedrine hydrochloride, ipratropium bromide, oxitropium bromide, flutropium bromide, theophylline, aminophylline, sodium cromoglicate, tranilast, repirinast, amlexanox, ibudilast, ketotifen, terfenadine, mequitazine, azelastine, ozagrel hydrochloride, pranlukast hydrate, seratrodast, ciclesonide, chlorpheniramine maleate, alimemazine tartrate, clemastine fumarate, homochlorcyclizine hydrochloride, fexofenadine, ketotifen fumarate, cetirizine hydrochloride, oxatomide, ebastine, epinastine hydrochloride, loratadine, tramadol, promethazine, hydroxyzine, homochlorcyclizine, cyproheptadine, mequitazine, emedastine fumarate, pseudoephedrine, bepotastine besilate, levocetirizine, olopatadine hydrochloride, mycophenolate mofetil, daclizumab, galiximab, metformin hydrochloride, visilizumab, aminopterin, pazopanib hydrochloride, fezakinumab, ruxolitinib phosphate, ixekizumab, guselkumab, SLx-2119, PRX-167700, lidocaine, tiotropium bromide, salmeterol xinafoate, formoterol fumarate, fluticasone propionate, beclometasone propionate, budesonide, and combination drugs of salmeterol xinafoate and fluticasone propionate.

Details for Patent 10,273,252

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Recordati Rare Diseases, Inc.	ELSPAR	asparaginase	For Injection	101063	January 10, 1978	10,273,252	2036-04-28
Bayer Healthcare Pharmaceuticals Inc.	BETASERON	interferon beta-1b	For Injection	103471	July 23, 1993	10,273,252	2036-04-28
Biogen Inc.	AVONEX	interferon beta-1a	For Injection	103628	May 17, 1996	10,273,252	2036-04-28
Biogen Inc.	AVONEX	interferon beta-1a	Injection	103628	May 28, 2003	10,273,252	2036-04-28
Biogen Inc.	AVONEX	interferon beta-1a	Injection	103628	February 27, 2012	10,273,252	2036-04-28