Amine salts of an integrin receptor antagonist
US6444680B1 · kind B1 · utility
Assignee
Inventors
Key dates
| Filing date | Nov 29, 2001 |
| Grant date | Sep 3, 2002 |
| Priority date | — |
| Expiry date | Nov 29, 2021 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D487/04
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Amine salts of 3-(2-methyl-pyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-nonanoic acid are potent antagonists of the integrin &agr;v&bgr;3 receptor and are useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salts as well as pharmaceutical compositions containing the salts and methods of using the salts. Also disclosed are 3(R)- and 3(S)-(2-methylpyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-nonanoic acid in the form of a zwitterion trihydrate.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.