Indazole bioisostere replacement of catechol in therapeutically active compounds
US6391872B1 · kind B1 · utility
Assignee
Inventor
Key dates
| Filing date | Sep 20, 1999 |
| Grant date | May 21, 2002 |
| Priority date | — |
| Expiry date | Sep 20, 2019 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P43/00
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Therapeutically active compositions of matter and member species thereof are described which comprise indazole-containing compounds, said compounds and their therapeutic activity resulting directly from an indazole-for-catechol bioisostere replacement of a catechol-containing compound having the same therapeutic activity, where non-catechol substituents are the same or homologous before and after said replacement, and wherein said compositions of matter comprise a compound of Formula (I1) or (I2): or a pharmaceutically acceptable salt thereof, wherein in a preferred embodiment RC is hydrogen; RA is cyclohexyl; and RB is ethyl. Ra and Rb are each individually and independently hydrogen or non-catechol substituents of said compounds resulting directly from an indazole-for-catechol bioisostere replacement of said catechol-containing compound having said therapeutic activity, where said non-catechol substituents are the same or homologous before and after said replacement, provided that both of Ra and Rb cannot be hydrogen at the same time. The therapeutic activity involved may comprise cholinesterase inhibitory activity, adrenergic &agr;1-antagonist and &bgr;1-agonist activity, calciu…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.