Invention Grant
- Patent Title: Substituted isoindolines as aspartyl protease inhibitors
- Patent Title (中): 取代的异吲哚啉作为天冬氨酰蛋白酶抑制剂
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Application No.: US11451065Application Date: 2006-06-12
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Publication No.: US08722708B2Publication Date: 2014-05-13
- Inventor: Andrew Stamford , Guoqing Li , William Greenlee , Zhaoning Zhu , Brian McKittrick , Robert Mazzola , Ying Huang , Tao Guo , Thuy X. H. Le , Gang Qian , Yuefei Shao
- Applicant: Andrew Stamford , Guoqing Li , William Greenlee , Zhaoning Zhu , Brian McKittrick , Robert Mazzola , Ying Huang , Tao Guo , Thuy X. H. Le , Gang Qian , Yuefei Shao
- Applicant Address: US NJ Rahway US NJ Princeton
- Assignee: Merck Sharp & Dohme Inc.,Pharmacopeia Drug Discovery, Inc.
- Current Assignee: Merck Sharp & Dohme Inc.,Pharmacopeia Drug Discovery, Inc.
- Current Assignee Address: US NJ Rahway US NJ Princeton
- Agent Keith D. MacMillan; John C. Todaro
- Main IPC: C07D487/04
- IPC: C07D487/04 ; A61K31/519 ; A61K31/4035 ; A61K31/4406 ; C07D487/14 ; A61K31/437 ; A61P25/28 ; A61P9/00 ; A61P31/14

Abstract:
Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6′R7′); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7′ are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.
Public/Granted literature
- US20080176868A1 Preparation and use of compounds as protease inhibitors Public/Granted day:2008-07-24
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