Claims for Patent: 8,486,947

Summary for Patent: 8,486,947

Title:	Treatment of Parkinson's disease, obstructive sleep apnea, dementia with Lewy bodies, vascular dementia with non-imidazole alkylamines histamine H.sub.3-receptor ligands
Abstract:	The present invention provides new method of treatment of Parkinson's disease, obstructive sleep apnea, narcolepsy, dementia with Lewy bodies, vascular dementia with non-imidazole alkylamine derivatives that constitute antagonists of the H.sub.3-receptors of histamine.
Inventor(s):	Schwartz; Jean-Charles (Paris, FR), Lecomte; Jeanne-Marie (Paris, FR)
Assignee:	Bioprojet (Paris, FR)
Application Number:	11/909,778
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,486,947
Patent Claims:	1. A method for treating excessive daytime sleepiness comprising administering to a patient in need thereof a compound of formula (IIa): ##STR00065## wherein: R.sup.1 and R.sup.2 form together with the nitrogen atom to which they are attached a saturated nitrogen-containing ring ##STR00066## with m ranging from 2 to 8, or R.sup.a-b being independently a hydrogen atom or a linear or branched alkyl group containing 1 to 6 carbon atoms, and the chain A.sup.II selected from an unbranched alkyl group --(CH.sub.2).sub.nII-- where n.sub.II is 3 ; the group X'' is --O--; the chain B.sup.II is an unbranched alkyl comprising 3 carbon atoms; and the group Y.sup.II represents a phenyl group, unsubstituted or mono- or polysubstituted with one or more identical or different substituents selected from halogen atoms, OCF.sub.3, CHO, CF.sub.3, SO.sub.2N(alkyl).sub.2, NO.sub.2, S(aryl), SCH.sub.2(phenyl), an unbranched or branched alkene, an unbranched or branched alkyne optionally substituted with a trialkylsilyl radical, --O (alkyl), --O(aryl), --CH.sub.2CN, a ketone, an aldehyde, a sulphone, an acetal, an alcohol, a linear or branched alkyl group containing 1 to 6 carbon atoms, --CH.dbd.CH--CHO, --C(alkyl)=N--OH, --C(alkyl)=N--O(alkyl), --CH.dbd.NOH, --CH.dbd.NO(alkyl), --C(alkyl)=NH--NH--CONH.sub.2, an O-phenyl or --OCH.sub.2(phenyl) group, --C(cycloalkyl)=NOH, --C(cycloalkyl)=N--O(alkyl); or its pharmaceutically acceptable salts, hydrates, or hydrated salts, or the polymorphic crystalline structures of these compounds or their optical isomers, racemates, diastereoisomers or enantiomers, wherein said patient is suffering from Parkinson's disease, narcolepsy, or sleep apnea. 2. The method according to claim 1 wherein --NR.sup.1R.sup.2 is a saturated nitrogen-containing ring: ##STR00067## R.sup.a and m being as defined in claim 1. 3. The method according to claim 1, wherein m is 4 or 5. 4. The method according to claim 1, wherein --NR.sup.1R.sup.2 is selected from the group consisting in piperidyl, pyrrolidinyl. 5. The method according to claim 1, wherein R.sup.a is a hydrogen atom. 6. The method according to claim 1, wherein the nitrogen-containing ring i) is one of mono- and di-substituted. 7. The method according to claim 1 , wherein the nitrogen-containing ring i) is mono-substituted with an alkyl group. 8. The method according to claim 1, wherein the nitrogen-containing ring is mono-substituted with a methyl group. 9. The method according to claim 1, wherein the substituent(s) is(are) in beta-position with respect to the nitrogen atom. 10. The method according to claim 1, wherein Y.sup.II represents a phenyl group at least mono-substituted with a halogen atom, keto-substituent which may include a linear or branched chain aliphatic ketone comprising from 1 to 8 carbon atoms and optionally bearing a hydroxyl group, a cycloalkylketone, an arylalkylketone or arylalkenylketone in which the aryl group is optionally substituted, or a heteroaryl ketone. 11. The method according to claim 1, wherein Y.sup.II is a phenyl group at least mono-substituted with a halogen atom, --CHO, a ketone, an aldehyde, --CH.dbd.CH--CHO, --C(alkyl)=N--OH, --C(alkyl)=N--O(alkyl), --CH.dbd.NO(alkyl), -(cycloalkyl)=NOH, --C(cycloalkyl)=N--O (alkyl). 12. The method according to claim 1, wherein the compound is selected from: -3-Phenylpropyl 3-piperidinopropyl ether -3-(4-Chlorophenyl)propyl 3 -piperidinopropyl ether -3-Phenylpropyl 3-(4.about.methylpiperidino)propyl ether -3-Phenylpropyl 3-(3,5-cis-dimethylpiperidino)propyl ether -3-Phenylpropyl 3-(3,5-trans-dimethylpiperidino)propyl ether -3-Phenylpropyl 3-(3-methylpiperidino)propyl ether -3-Phenylpropyl 3-pyrrolidinopropyl ether -3-(4-Chlorophenyl)propyl 3-(4-methylpiperidino)propyl ether -3-(4-Chlorophenyl) propyl 3-(3,5-cis-dimethyl piperidino)propyl ether -3-(4-Chlorophenyl) propyl 3-(3,5-trans-dimethyl piperidino)propyl ether, or its pharmaceutically acceptable salts, hydrates, or hydrated salts, or the polymorphic crystalline structures of these compounds or their optical isomers, racemates, diastereoisomers or enantiomers. 13. The method according to claim 1, wherein the compound is selected from 3-(4-chlorophenyl)propyl-3-piperidino- propylether, or its pharmaceutically acceptable salts, hydrates, or hydrated salts, or the polymorphic crystalline structures of this compound or its optical isomers, racemates, diastereoisomers or enantiomers. 14. The method according to claim 1, wherein the compound is in the form of a pharmaceutically acceptable salt and said salt is chosen from the group consisting in hydrochloride, hydrobromide, hydrogen maleate or hydrogen oxalate. 15. A method according to claim 1 further comprising administering a ligand of the H3 receptor in combination with a medicament for treating of Parkinson's disease, obstructive sleep apnea, narcolepsy, dementia with Lewy bodies and/or vascular dementia, respectively. 16. The method according to claim 1 in which said treatment is intended for treating symptoms of Parkinson's disease, obstructive sleep apnea, dementia with Lewy bodies and/or vascular dementia. 17. The method according to claim 16, in which said symptoms are chosen from sleep and vigilance disorders. 18. The method according to claim 15 wherein the anti-parkinson drug is chosen from levodopa, ropinorole, lisuride, bromocriptine, pramixepole.