IP Library Granted Patent US 7,625,893
Granted Patent B2
US 7,625,893 · App. 12/224,440 · Granted Dec 1, 2009

Substituted 4-phenyl piperidines for use as renin inhibitors

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Quick Facts
Patent No.
US 7,625,893
App. No.
12/224,440
Granted
Dec 1, 2009
Kind
B2
Abstract

Compounds of the general formula (I) and the salts thereof, preferably the pharmaceutically acceptable salts thereof; in which R 1 is straight-chain C 1-8 -alkanoyloxy, straight-chain C 1-8 -alkoxy, straight-chain C 1-8 -alkoxy-straight-chain-C 1-8 -alkoxy, straight-chain C 1-8 -alkoxycarbonylamino, straight-chain C 0-8 -alkylcarbonylamino, optionally N-mono- or N,N-di-C 1-8 -alkylated amino or hydroxy or straight-chain omega-hydroxy-C 1-8 -alkyl.

Claims (17)

1. A compound of the formula

or its pharmaceutically acceptable salt, in which

R 1 is straight-chain C 1-8 -alkanoyloxy, straight-chain C 1-8 -alkoxy, straight-chain C 1-8 -alkoxy-straight-chain-C 1-8 -alkoxy, straight-chain C 1-8 -alkoxycarbonylamino, straight-chain C 0-8 -alkylcarbonylamino, optionally N-mono- or N,N-di-C 1-8 -alkylated amino or hydroxy or straight-chain omega-hydroxy-C 1-8 -alkyl.

2. A compound or its pharmaceutically acceptable salt according to claim 1 1 , in which

R 1 is hydroxy or straight-chain omega-hydroxy-C 1-8 -alkyl.

3. A compound or its pharmaceutically acceptable salt according to claim 1 , in which

R 1 is straight-chain C 1-8 -alkoxy or straight-chain C 1-8 -alkoxy-straight-chain-C 1-8 -alkoxy.

4. A compound or its pharmaceutically acceptable salt according to claim 1 , in which

R 1 is straight-chain C 1-8 -alkanoyloxy.

5. A compound or its pharmaceutically acceptable salt according to claim 1 , in which

R 1 is straight-chain C 0-8 -alkylcarbonylamino.

6. A compound or its pharmaceutically acceptable salt according to claim 1 , in which

R 1 is optionally N-mono- or N,N-di-straight-chain-C 1-8 -alkylated amino.

7. A compound or its pharmaceutically acceptable salt according to claim 1 , in which

R 1 is hydroxy, methoxy, 2-methoxy-ethoxy, acetyloxy, formamido, methylcarbonylamino or ethylcarbonylamino.

8. A pharmaceutical composition comprising a compound or its pharmaceutically acceptable salt according to claim 1 and a pharmaceutically inert inorganic or organic excipient.

9. A method for the treatment of high blood pressure, glaucoma, and myocardial infarction, which comprises administering a therapeutically effective amount of a compound or its pharmaceutically acceptable salt according to claim 1 to a person in need thereof.

Assignments (2)
MERGER Recorded Feb 9, 2010
From: SPEEDEL EXPERIMENTA AG
To: NOVARTIS AG
Reel/Frame 023920/0239 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 27, 2008
From: HEROLD, PETER; MAH, ROBERT; STUTZ, STEFAN; TSCHINKE, VINCEZO; STOJANOVIC, ALEKSANDAR; BEHNKE, DIRK; JOTTERAND, NATHALIE; JELAKOVIC, STJEPAN
To: SPEEDEL EXPERIMENTA AG
Reel/Frame 021479/0497 →