Piperidine derivatives useful as ccr5 antagonists

a technology of ccr5 and derivatives, applied in the field ofpiperidine derivatives, can solve problems such as multi-drug resistance, and achieve the effect of preventing or ameliorating one or mor

Inactive Publication Date: 2008-04-24
SCHERING CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The piperidine derivatives effectively inhibit HIV entry and treat conditions like HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, and multiple sclerosis by targeting the CCR5 receptor, offering a potential solution to the limitations of existing treatments.

Problems solved by technology

However, these multidrug therapies do not eliminate HIV-1 and long-term treatment usually results in multidrug resistance.

Method used

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  • Piperidine derivatives useful as ccr5 antagonists
  • Piperidine derivatives useful as ccr5 antagonists
  • Piperidine derivatives useful as ccr5 antagonists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0035] In one embodiment, the present invention discloses compounds represented by structural formula I,

or a pharmaceutically acceptable salt or solvate thereof; wherein the various moieties are defined as above.

[0036] The compounds of formula I can be administered as racemic mixtures or enantiomerically pure compounds.

[0037] In an embodiment of the compounds of formula I, X is CH.

[0038] In another embodiment, Z is N.

[0039] In another embodiment, t is 2 and s is 1.

[0040] In another embodiment, R2, R5 and R7 are hydrogen.

[0041] In another embodiment, R4 and R7 are alkyl,

[0042] In an additional embodiment, R4 and R7 are methyl.

[0043] In an additional embodiment, R1 is H, —S(O2)alkyl, —S(O2)aryl or —S(O2)cycloalkyl.

[0044] In a still additional embodiment, R1 is H,

[0045] In a still additional embodiment, R3 is aryl or aralkyl,

[0046] In a still another additional embodiment, R3 is benzyl or phenyl and R8 is heteroaryl.

[0047] In yet an additional preferred embodiment R8 is...

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Abstract

The present invention provides a compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein the various moieties are as defined in the specification. The present invention also provides pharmaceutical compositions containing the compound of this invention, and methods of treatment using the compound of this invention. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.

Description

PRIORITY APPLICATION [0001] This application is a divisional of U.S. application Ser. No. 10 / 738,907, filed Dec. 17, 2003, which claims the benefit of U.S. provisional Application Ser. No. 60 / 434,306, filed Dec. 18, 2002, both of which are incorporated herein by reference in their entirety.FIELD OF THE INVENTION [0002] The present invention relates to piperidine derivatives useful as selective CCR5 antagonists, pharmaceutical compositions containing the compound of this invention, and methods of treatment using the inventive compounds. The invention also relates to the use of a combination of the compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of the compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, ato...

Claims

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Application Information

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Patent Type & AuthorityApplications(United States)
IPC IPC(8): A61K31/506A61K31/538A61K31/551A61K31/675A61K31/7056A61K31/7068A61K31/7072A61K31/708A61K38/20A61P31/18A61P37/00C07D401/14
CPCC07D401/14A61P1/00A61P11/06A61P17/00A61P17/04A61P17/06A61P19/00A61P19/02A61P19/04A61P25/00A61P29/00A61P31/12A61P31/18A61P37/00A61P37/02A61P37/06A61P37/08A61P43/00A61K31/506
InventorMILLER, MICHAEL W.SCOTT, JACK D.
OwnerSCHERING CORP