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Biaryl pde4 inhibitors for treating pulmonary and cardiovascular disorders

Inactive Publication Date: 2009-05-28
DECODE GENETICS EHF
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0012]Selective PDE4 inhibitors of the invention are also useful for treating asthma and Chronic Obstructive Pulmonary Disease (COPD). Compounds of the invention, which inhibit tumor growth and metastases, also find utility in the treatment and prevention of cancer, including esophageal cancer, brain cancer, pancreatic cancer, and colon cancer. Compounds of the invention may also find utility in the treatment and prevention of bone loss, bladder inflammation, bladder overactivity or pain arising from bladder inflammation.
[0013]These and other embodiments of the present invention will become apparent in conjunction with the description and claims that follow.

Problems solved by technology

Despite initial optimism, none have yet reached the market.
. . has been discontinued due to lack of efficacy.
A primary problem is the low therapeutic ratio of these compounds, which severely limits the dose that can be given.
Many of the PDE4 inhibitors of the prior art have not reached the market because of the adverse side effect of emesis (Giembycz 2005.

Method used

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  • Biaryl pde4 inhibitors for treating pulmonary and cardiovascular disorders
  • Biaryl pde4 inhibitors for treating pulmonary and cardiovascular disorders
  • Biaryl pde4 inhibitors for treating pulmonary and cardiovascular disorders

Examples

Experimental program
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Embodiment Construction

[0014]Throughout this specification the substituents are defined when introduced and retain their definitions.

[0015]Unless otherwise specified, alkyl is intended to include linear, branched, or cyclic hydrocarbon structures and combinations thereof. A combination would be, for example, cyclopropylmethyl. Lower alkyl refers to alkyl groups of from 1 to 6 carbon atoms. Examples of lower alkyl groups include methyl, ethyl, propyl, isopropyl, butyl, s- and t-butyl and the like. Preferred alkyl groups are those of C20 or below; C1 to C8 are more preferred. Cycloalkyl is a subset of alkyl and includes cyclic hydrocarbon groups of from 3 to 8 carbon atoms. Examples of cycloalkyl groups include c-propyl, c-butyl, c-pentyl, norbornyl and the like.

[0016]C1 to C20 hydrocarbon includes alkyl, cycloalkyl, polycycloalkyl, alkenyl, alkynyl, aryl and combinations thereof. Examples include benzyl, phenethyl, cyclohexylmethyl, camphoryl and naphthylethyl. Hydrocarbon refers to any substituent compris...

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Abstract

The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders. The compounds have general formula Ia, Ib, Ic or Id:A particular embodiment is

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application claims priority from U.S. provisional application 60 / 989,551, filed Nov. 21, 2007, the entire disclosure of which is incorporated herein by reference. The application is related to, but does not claim priority from, four other US non-provisional applications filed of even date herewith and having Jasbir Singh as a common inventor. The applications are titled “BIARYL PDE4 INHIBITORS FOR TREATING INFLAMMATORY, CARDIOVASCULAR AND CNS DISORDERS”, “SUBSTITUTED BENZOAZOLE PDE4 INHIBITORS FOR TREATING INFLAMMATORY, CARDIOVASCULAR AND CNS DISORDERS”, “SUBSTITUTED BENZOAZOLE PDE4 INHIBITORS FOR TREATING PULMONARY AND CARDIOVASCULAR DISORDERS” and “4- (OR5-) SUBSTITUTED CATECHOL DERIVATIVES”. Their disclosures are incorporated herein by reference.FIELD OF THE INVENTION[0002]The present invention relates to a chemical genus of biaryl inhibitors of phosphodiesterase-4 (PDE4) useful for the treatment and prevention of stroke, myocardi...

Claims

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Application Information

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IPC IPC(8): A61K31/44C07D231/12C07D213/64C07D239/42C07D213/79C07C275/28C07D285/135A61K31/433A61K31/4439A61P1/00A61P11/00A61P35/00A61P9/00A61K31/122A61K31/4353A61K31/435A61K31/4427A61K31/437A61K31/4545C07D401/06C07D471/04C07D213/72A61K31/415A61K31/4412A61K31/495
CPCC07B2200/05C07C217/84C07C69/94C07C275/32C07C275/62C07C305/24C07C307/10C07D207/16C07D213/38C07D213/40C07D213/64C07D213/74C07D213/75C07D213/76C07D213/79C07D213/81C07D213/84C07D213/89C07D231/12C07D233/90C07D239/42C07D257/04C07D275/06C07D285/12C07D285/135C07D401/04C07D401/06C07D403/04C07D471/04C07D473/18C07D473/40C07D205/04C07D277/42A61K45/06A61K31/5377A61K31/4427A61K31/4418A61K31/44A61K31/437A61K31/426A61K31/41A61K31/397A61K31/136C07D213/73C07D213/65C07C65/40A61P1/00A61P11/00A61P11/06A61P13/10A61P19/00A61P19/08A61P19/10A61P25/00A61P25/14A61P25/22A61P25/24A61P25/28A61P29/00A61P35/00A61P43/00A61P9/00A61P9/10C07D213/62
Inventor SINGH, JASBIRGURNEY, MARK E.BURGIN, ALEXKISELYOV, ALEXANDERRAO, MUNAGALAHAGEN, TIMOTHY
Owner DECODE GENETICS EHF
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