Claims for Patent: 10,730,873
✉ Email this page to a colleague
Summary for Patent: 10,730,873
| Title: | Salts and crystalline forms of an apoptosis-inducing agent |
| Abstract: | Salts and crystalline forms of 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin- -1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}-sulfon- yl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide are suitable active pharmaceutical ingredients for pharmaceutical compositions useful in treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer. |
| Inventor(s): | Catron; Nathaniel (Vernon Hills, IL), Chen; Shuang (Gurnee, IL), Gong; Yuchuan (Waukegan, IL), Zhang; Geoff G. (Vernon Hills, IL) |
| Assignee: | AbbVie Inc. (Chicago, IL) |
| Application Number: | 15/806,964 |
| Patent Claims: |
1. A compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin- -1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl}sulfony-
l)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide (Compound 1) in a crystalline form, wherein the crystalline form is Compound 1free base hydrate, characterized by a powder X-ray diffraction pattern having five or more peaks selected from those at 3.3,
6.4, 7.1, 7.3, 10.1, 11.4, 13.2, 14.4, 14.6, 15.1, 15.8, 16.2, 17.2, 17.6, 18.0, 18.6, 19.0, 19.5, 19.8, 20.2, 20.7, 21.0, 22.5, 23.0, 26.0, 28.9, and 29.2 degrees 2.theta.(pattern D), each peak being .+-.0.2 degrees 2.theta., when measured at about
25.degree. C. with Cu K.sub..alpha.radiation at 1.54178 .ANG..
2. A pharmaceutical composition comprising the compound of claim 1 and one or more pharmaceutically acceptable excipients. 3. A process for preparing a pharmaceutical solution of Compound 1 comprising dissolving the compound of claim 1 in a pharmaceutically acceptable solvent or mixture of solvents. 4. A compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin- -1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl)amino]phenyl sulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide (Compound 1) in a crystalline form, characterized by a powder X-ray diffraction pattern having peaks at 7.1, 14.4, and 19.0 degrees 2.theta., each peak being .+-.0.2 degrees 2.theta., when measured at about 25.degree. C. with Cu K.sub..alpha.radiation at 1.54178 .ANG.. 5. A pharmaceutical composition comprising the compound of claim 4 and one or more pharmaceutically acceptable excipients. 6. A process for preparing a pharmaceutical solution of Compound 1comprising dissolving the compound of claim 4 in a pharmaceutically acceptable solvent or mixture of solvents. 7. A compound 4-(4-{[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl}piperazin- -1-yl)-N-({3-nitro-4-[(tetrahydro-2H-pyran-4-ylmethyl) amino]phenylsulfonyl)-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide (Compound 1) in a crystalline form, characterized by a powder X-ray diffraction pattern having peaks at 19.8, 20.7, and 22.5 degrees 2.theta., each peak being .+-.0.2 degrees 2.theta., when measured at about 25.degree. C. with Cu K.sub..alpha.radiation at 1.54178 .ANG.. 8. A pharmaceutical composition comprising the compound of claim 7 and one or more pharmaceutically acceptable excipients. 9. A process for preparing a pharmaceutical solution of Compound 1comprising dissolving the compound of claim 7 in a pharmaceutically acceptable solvent or mixture of solvents. |
