IP Library Granted Patent US 8,372,849
Granted Patent B2
US 8,372,849 · App. 12/263,671 · Granted Feb 12, 2013

Heterocyclic compounds

Inventors: Chi-Feng Yen (Taipei County, TW); Cheng-Kung Hu (Hsinchu, TW); Chang-Pin Huang (Sanchong, TW); Ying-Huey Huang (Changhua, TW); Gholam Hossein Hakimelahi (Richmond Hill, CA); Chi-Hsin Richard King (Holladay, UT)
Assignee: Taigen Biotechnology Co., Ltd.
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Quick Facts
Patent No.
US 8,372,849
App. No.
12/263,671
Granted
Feb 12, 2013
Kind
B2
Abstract

This invention relates to heterocyclic compounds of the formulas shown in the specification. It also relates to methods for treating inflammatory diseases or immune diseases, developmental or degenerative diseases, and tissue injuries with one of the heterocyclic compounds.

Claims (22)

1. A compound of the following formula:

wherein

each Q and U is CH or N, provided that one of Q and U is N;

each of X, Y, and Z, independently, is C 1-5 alkylene or deleted;

m is 0, 1, 2, 3, 4, or 5;

n is 1;

p is 1 or 2;

R 1 is H, C 1 -C 10 alkyl, C 3 -C 20 cycloalkyl, C 1 -C 20 heterocycloalkyl, aryl, heteroaryl, halo, CN, OR a , COOR a , OC(O)R a , C(O)R a , C(O)NR a R b , or NR a R b ;

R 2 is C 1 -C 10 alkyl, C 3 -C 20 cycloalkyl, C 1 -C 20 heterocycloalkyl, aryl, heteroaryl, or C 1 -C 10 alkyl, optionally substituted with C 1 -C 10 alkyl, C 3 -C 20 cycloalkyl, C 1 -C 20 heterocycloalkyl, or N(R c R d );

R 3 , independently, is C 1 -C 10 alkyl, C 3 -C 20 cycloalkyl, C 1 -C 20 heterocycloalkyl, aryl, heteroaryl, halo, CN, OR e , COOR e , OC(O)R e , C(O)R e , C(O)NR e R f , or NR e R f ; or R 3 is C 1-5 alkylene bonded to two carbon atoms of the ring to which it is attached or C 2-8 alkylene bonded to one carbon atom of the ring to which it is attached; and

R 4 is P(═O)(OR g )(OR i ), P(═O)(NHR g )(OR i ), P(═O)(NR g )(NR i ), S(═O) 2 OR g , or S(═O) 2 R g ;

in which each of R a , R b , R c , R d , R e , R f , R g and R i , independently, is H, C 1 -C 10 alkyl, C 3 -C 20 cycloalkyl, C 1 -C 20 heterocycloalkyl, aryl, heteroaryl, or —C(O)R, R being H, C 1 -C 10 alkyl, C 3 -C 20 cycloalkyl, C 1 -C 20 heterocycloalkyl, aryl, or heteroaryl; or R a and R b are linked and together form C 2-8 alkylene, R c and R d are linked and together form C 2-8 alkylene, R e and R f are linked and together form C 2-8 alkylene, or R g and R i are linked and together form C 1-5 alkylene.

2. The compound of claim 1 , wherein Q is CH and U is N.

3. The compound of claim 1 , wherein X is —CH 2 —, —CH 2 CH 2 — or —CH 2 CH 2 CH 2 — and p is 1.

4. The compound of claim 1 , wherein Y is —CH 2 or deleted and Z is —CH 2 —.

5. The compound of claim 1 , wherein R 2 is C 1-5 alkyl substituted N(R c R d ).

6. The compound of claim 5 , wherein R 2 is —CH 2 CH 2 CH 2 —N(R c R d ), in which R c is H and R d is C 1 -C 10 alkyl, C 3 -C 20 cycloalkyl, C 1 -C 20 heterocycloalkyl, aryl, or heteroaryl, or R c and R d are linked and together form C 4-6 alkylene.

7. The compound of claim 1 , wherein m is 0, 1, or 2; R 1 is NH 2 ; and R 3 is C 1 -C 3 alkyl, C 3 -C 8 cycloalkyl, C 1 -C 8 heterocycloalkyl, aryl, heteroaryl, halo, CN, OR e , or C(O)NR c R f ; or R 3 is C 1-2 alkylene bonded to two carbon atoms of the ring to which it is attached or C 2-5 alkylene bonded to one carbon atom of the ring to which it is attached.

8. The compound of claim 1 , wherein R 4 is P(═O)(OH) 2 , P(═O)(OH)(OCH 2 CH 3 ), P(═O)(OCH 2 CH 3 ) 2 ,

S(═O) 2 OH, S(═O) 2 CH 3 , or S(═O) 2 Ph.

9. The compound of claim 8 , wherein m is 0, 1, or 2; p is 1; X is —CH 2 CH 2 — or —CH 2 CH 2 CH 2 —; Y is —CH 2 or deleted and Z is —CH 2 —; R 1 is NH 2 ; R 2 is C 1-5 alkyl substituted N(R c R d ); and R 3 is C 1 -C 3 alkyl, C 3 -C 8 cycloalkyl, C 1 -C 8 ttbonded to two carbon atoms of the ring to which it is attached or C 2-5 alkylene bonded to one carbon atom of the ring to which it is attached.

10. The compound of claim 1 , wherein the compound is selected from the groups consisting of the following compounds:

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 18, 2021
From: TAIGEN BIOTECHNOLOGY CO., LTD.
To: GPCR THERAPEUTICS, INC
Reel/Frame 055302/0312 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 2, 2008
From: YEN, CHI-FENG; HU, CHENG-KUNG; HUANG, CHANG-PIN; HUANG, YING-HUEY; HAKIMELAHI, GHOLAM HOSSEIN; KING, CHI-HSIN RICHARD
To: TAIGEN BIOTECHNOLOGY CO., LTD.
Reel/Frame 021911/0844 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 4, 2008
From: YEN, CHI-FENG; HU, CHENG-KUNG; HUANG, CHANG-PIN; HUANG, YING-HUEY; HAKIMELAHI, GHOLAM HOSSEIN; KING, CHI-HSIN RICHARD
To: TAIGEN BIOTECHNOLOGY CO., LTD.
Reel/Frame 021781/0647 →
Continuity (2)
Provisional Application 61046496 · Apr 21, 2008
Related Publication 20090264339A1 · Oct 22, 2009