IP Library Granted Patent US 10,660,897
Granted Patent B2
US 10,660,897 · App. 16/030,729 · Granted May 26, 2020

C5aR antagonists

Inventors: Pingchen Fan (Fremont, CA); Kevin Lloyd Greenman (Sunnyvale, CA); Manmohan Reddy Leleti (Dublin, CA); Yandong Li (San Diego, CA); Jay Powers (Pacifica, CA); Hiroko Tanaka (Mountain View, CA); Ju Yang (Palo Alto, CA); Yibin Zeng (Foster City, CA)
Assignee: ChemoCentryx, Inc.
A61K31/5377A61K31/445A61K31/451A61K31/454A61K31/4545C07D211/60C07D401/06C07D401/10C07D401/12C07D401/14C07D405/10C07D413/12C07D413/14
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Quick Facts
Patent No.
US 10,660,897
App. No.
16/030,729
Granted
May 26, 2020
Kind
B2
Abstract

Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.

Claims (15)

1. A method for treating a human suffering from a disease or disorder selected from the group consisting of tissue graft rejection, hyperacute rejection of transplanted organs, rheumatoid arthritis, lupus nephritis, and autoimmune hemolytic and thrombocytopenic states, comprising administering to the human an effective amount of a compound having the formula:

and pharmaceutically acceptable salts, hydrates and rotomers thereof; wherein

X 1 is selected from the group consisting of N, CH and CR 1 ;

each R 1 is independently selected from the group consisting of

halogen, —CN, —R c , —CO 2 R a , —CONR a R b , and —C(O)R a ; wherein each R a and R b is independently selected from hydrogen, C 1-8 alkyl, and C 1-8 haloalkyl, each R c is independently selected from the group consisting of C 1-8 alkyl, C 1-8 haloalkyl, and C 3-6 cycloalkyl;

the subscript n is an integer of from 0 to 2;

X 2 is selected from the group consisting of N, CH and CR 2 ;

each R 2 is independently selected from the group consisting of

halogen, —CN, —R f , —CO 2 R d , —CONR d R e , and —C(O)R d ; wherein each R d and R e is independently selected from hydrogen, C 1-8 alkyl, and C 1-8 haloalkyl; each R f is independently selected from the group consisting of C 1-8 alkyl, C 1-8 haloalkyl, and C 3-6 cycloalkyl;

the subscript m is an integer of from 0 to 2; and

C 3 is selected from the group consisting of:

2. The method of claim 1 , wherein the disease or disorder is lupus nephritis.

3. The method of claim 1 , wherein the disease or disorder is tissue graft rejection or hyperacute rejection of transplanted organs.

4. The method of claim 1 , wherein the disease or disorder is autoimmune hemolytic and thrombocytopenic states.

5. The method of claim 1 , wherein the disease or disorder is rheumatoid arthritis.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 17, 2019
From: FAN, PINGCHEN; GREENMAN, KEVIN LLOYD; LELETI, MANMOHAN REDDY; LI, YANDONG; POWERS, JAY; TANAKA, HIROKO; YANG, JU; ZENG, YIBIN
To: CHEMOCENTRYX, INC.
Reel/Frame 049214/0935 →
Continuity (6)
Continuation 15354878 · Nov 17, 2016
Continuation 14531385 · Nov 3, 2014
Division 13894209 · May 14, 2013
Division 12643229 · Dec 21, 2009
Provisional Application 61139919 · Dec 22, 2008
Related Publication 20190060321A1 · Feb 28, 2019