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Azaindazole compounds and methods of use

a technology of azaindazole and compounds, applied in the field of azaindazole compounds and methods of use, can solve the problems of short half-lives once administered, and inability to meet the needs of patients,

Inactive Publication Date: 2007-01-11
CHEMOCENTRYX INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010] In addition to the compounds provided herein, the present invention further provides pharmaceutical compositions containing one or more of these compounds, as well as methods for the use of these compounds in therapeutic methods, primarily to treat diseases associated with CCR1 signaling activity.

Problems solved by technology

While function-blocking antibody and small peptide therapies are promising, they suffer from the perils of degradation, extremely short half-lives once administered, and prohibitive expense to develop and manufacture, characteristic of most proteins.

Method used

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  • Azaindazole compounds and methods of use
  • Azaindazole compounds and methods of use
  • Azaindazole compounds and methods of use

Examples

Experimental program
Comparison scheme
Effect test

example 1

Synthesis of 1-[4-(4-Chloro-3-methoxy-phenyl)-piperazin-1-yl]-2-pyrazolo[3,4-d]pyrimidin-1-yl-ethanone.

[0057]

[0058] Preparation of 4-Chloro-1H-pyrazolo[3,4-d]pyrimidine: 4,6-Dichloro-pyrimidine-5-carbaldehyde hydrazine (10 mL, excess), and dioxane (90 mL) are combined at −78° C. in THF. The reaction solution is warmed to rt and stirred for 16 hr. The solvent is evaporated in vacuo to provide a crude residue which is diluted with dichloromethane (600 mL). The organic solution is washed with water (50 mL), brine (50 mL) and dried over anhydrous sodium sulfate. The solvent is removed in vacuo to provide 4-Chloro-1H-pyrazolo[3,4-d]pyrimidine as a yellow powder which is used without further purification.

[0059] Preparation of 1H-Pyrazolo[3,4-d]pyrimidine: 4-Chloro-1H-pyrazolo[3,4-d]pyrimidine Pd(OH)2 and are combined in methanol in a reaction vessel. The reaction vessel is evacuated and backfilled with hydrogen gas and the resultant mixture is stirred at rt for several hours. The result...

example 2

[0061] This example illustrates the method in which compounds of interest (candidate compounds) of the invention can be evaluated for biological activity.

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Abstract

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Description

CROSS-REFERENCES TO RELATED APPLICATIONS [0001] This application claims priority to U.S. Provisional Application Ser. No. 60 / 693,525 filed on Jun. 22, 2005, the contents of which is incorporated herein in its entirety for all purposes.STATEMENT AS TO RIGHTS TO INVENTIONS MADE UNDER FEDERALLY SPONSORED RESEARCH OR DEVELOPMENT [0002] NOT APPLICABLE REFERENCE TO A “SEQUENCE LISTING,” A TABLE, OR A COMPUTER PROGRAM LISTING APPENDIX SUBMITTED ON A COMPACT DISK. [0003] NOT APPLICABLE BACKGROUND OF THE INVENTION [0004] The present invention provides compounds, pharmaceutical compositions containing one or more of those compounds or their pharmaceutically acceptable salts, which are effective in inhibiting the binding of various chemokines, such as MIP-1α, leukotactin, MPIF-1 and RANTES, to the CCR1 receptor. As antagonists or modulators for the CCR1 receptor, the compounds and compositions have utility in treating inflammatory and immune disorder conditions and diseases. [0005] Human healt...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/519C07D487/02
CPCC07D487/04C07D471/04A61P1/04A61P11/06A61P17/00A61P17/06A61P19/02A61P25/00A61P25/16A61P25/28A61P29/00A61P37/00A61P37/06A61P37/08A61P43/00A61P9/00A61P9/10C07D487/02C07D403/08A61K31/519A61K31/496
Inventor ZHANG, PENGLIEPENNELL, ANDREW M.K.WRIGHT, JOHN J. KIMCHEN, WEILELETI, MANMOHAN R.RONSHEIM, MATTHEW
Owner CHEMOCENTRYX INC
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