IP Library Granted Patent US 8,598,169
Granted Patent B2
US 8,598,169 · App. 13/540,940 · Granted Dec 3, 2013

Biaryl compositions and methods for modulating a kinase cascade

Inventor: David G. Hangauer, Jr. (Lancaster, NY)
Assignee: Kinex Pharmaceuticals, LLC
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Quick Facts
Patent No.
US 8,598,169
App. No.
13/540,940
Granted
Dec 3, 2013
Kind
B2
Abstract

The invention relates to compounds and methods for modulating one or more components of a kinase cascade. The invention relates to compounds of the formula I: or a pharmaceutically acceptable salt thereof. The compounds of the invention are useful for methods of protecting against or treating hearing loss, osteoporosis, cell proliferative disorders, obesity, diabetes, eye disease, stroke, atherosclerosis, neuropathic pain or hepatitis B.

Claims (46)

1. A method of inhibiting or relieving a disease selected from colon cancer, lung cancer, psoriasis, hearing loss, osteoporosis, type II diabetes, obesity, transplant rejection, stroke, atherosclerosis, chronic neuropathic pain, and hepatitis B, comprising administering to a subject in need thereof a compound of the formula IA:

or a salt, solvate, hydrate, or prodrug thereof, wherein

T is a bond;

X y is CY, N, or N—O;

X z is CZ;

Y is selected from hydrogen, hydroxyl, halogen, lower (C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 ) alkyl, C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkoxy, O-lower (C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 ) alkyl-aryl, and O-benzyl;

X a is CR a , N, or N—O;

X b is CR b ;

X c is CR c ;

X d is CR d ;

X e is CR e , N, or N—O;

R a , R b , R c , R d , R e , R 4 , R 5 , and R 6 are, independently, hydrogen, hydroxyl, halogen, P, C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl, C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkoxy, O-lower (C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 ) alkyl-aryl, O-benzyl, C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl-OH, COOH, COO-lower (C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 ) alkyl, SO 2 H, SO 2 -lower (C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 ) alkyl,

 wherein W is H, or C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl, C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl-aryl;

P is SO 3 H, OSO 3 H, PO 3 H 2 , OPO 3 H 2 , NH 2 , NHR 19 , NR 20 R 21 ,

 tetrazole, O-lower (C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 ) alkyl-K, O—C(O)-lower (C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 ) alkyl-L, NH-lower (C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 ) alkyl-M, or O-aryl-Q, further wherein lower (C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 ) alkyl is linear or branched alkyl;

K is aryl, C(O)NH 2 , COOH, SO 3 H, OSO 3 H, PO 3 H 2 , OPO 3 H 2 , NH 2 , NHR 19 , NR 19 R 20 , SO 2 R 21 , glycoside, lower C 1 , C 2 , C 3 , C 4 , C 5 , C 6 alkoxy, or

L is aryl, OH, C(O)NH 2 , COOH, SO 3 H, OSO 3 H, PO 3 H 2 , OPO 3 H 2 , NH 2 , NHR 19 , NR 19 R 20 , SO 2 R 21 , glycoside, lower C 1 , C 2 , C 3 , C 4 , C 5 , C 6 alkoxy, or

M is aryl, OH, C(O)NH 2 , COOH, SO 3 H, OSO 3 H, PO 3 H 2 , OPO 3 H 2 , NH 2 , NHR 19 , NR 19 R 20 , SO 2 R 21 , glycoside, lower C 1 , C 2 , C 3 , C 4 , C 5 , C 6 alkoxy, or

Q is aryl, OH, C(O)NH 2 , COOH, SO 3 H, OSO 3 H, PO 3 H 2 , OPO 3 H 2 , NH 2 , NHR 19 , NR 19 R 20 , SO 2 R 21 , glycoside, lower C 1 , C 2 , C 3 , C 4 , C 5 , C 6 alkoxy, or

R 19 , R 20 and R 21 are independently C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl or R 19 and R 20 taken together with the attached nitrogen atom form a five membered ring;

V is a bond, —CH 2 —, —CH 2 CH 2 —, —CH 2 CH 2 CH 2 —, —O—CH 2 —, —OCH 2 CH 2 — or —OCH 2 CH 2 CH 2 —;

Z is (CHR 1 ) n —C(O)—NR 2 (CHR 3 ) m —Ar, where Ar is a substituted or unsubstituted aryl or nitrogen-containing heteroaryl group, R 1 , R 2 , and R 3 are independently H or C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl;

n is 1 or 2; and

m is 0, 1, or 2;

provided that at least one of R a , R b , R c , R d , R e , R 4 , R 5 , and R 6 is P and wherein only one of X a , X e , and X y is N or N—O.

2. The method of claim 1 , wherein X y is N.

3. The method of claim 1 , wherein Z is

and R 7 , R 8 , R 9 , R 10 , and R 11 are selected from hydrogen, hydroxyl, halogen, C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl, C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkoxy, O-lower (C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 ) alkyl-aryl, O-benzyl, C 1 , C 2 , C 3 , C 4 , C 5 , C 6 alkyl-OH, C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl

where W is H, or C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl, C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl-aryl.

4. The method of claim 3 , wherein at least one of R 7 , R 8 , R 9 , R 10 , and R 11 is halogen, C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkoxy, or O-benzyl.

5. The method of claim 3 , wherein m and n are each 1 and R 2 and R 3 are each H.

6. The method of claim 1 , wherein the compound is selected from

7. The method of claim 1 , wherein the disease is colon cancer.

8. The method of claim 1 , wherein the disease is lung cancer.

9. The method of claim 1 , wherein the disease is psoriasis.

10. A method of inhibiting or relieving a disease or disorder selected from selected from colon cancer, lung cancer, psoriasis, hearing loss, osteoporosis, type II diabetes, obesity, transplant rejection, stroke, atherosclerosis, chronic neuropathic pain, and hepatitis B, comprising administering to a subject in need thereof a compound selected from

11. The method of claim 10 , wherein the disease is colon cancer.

12. The method of claim 10 , wherein the disease is lung cancer.

13. The method of claim 10 , wherein the disease is psoriasis.

14. A method of inhibiting or relieving a disease or disorder selected from selected from colon cancer, lung cancer, psoriasis, hearing loss, osteoporosis, type II diabetes, obesity, transplant rejection, stroke, atherosclerosis, chronic neuropathic pain, and hepatitis B, comprising administering to a subject in need thereof a compound selected from

15. The method of claim 14 , wherein the disease is colon cancer.

16. The method of claim 14 , wherein the disease is lung cancer.

17. The method of claim 14 , wherein the disease is psoriasis.

18. The method of claim 1 , wherein m is 1.

19. The method of claim 1 , wherein n is 1.

20. The method of claim 1 , wherein P is O-lower (C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 ) alkyl-K.

Assignments (11)
SECURITY INTEREST Recorded Sep 16, 2022
From: ATHENEX, INC.
To: SAGARD HEALTHCARE ROYALTY PARTNERS, LP, AS ADMINISTRATIVE AGENT
Reel/Frame 061119/0681 →
SECURITY INTEREST Recorded Sep 16, 2022
From: ATNX SPV, LLC
To: SAGARD HEALTHCARE ROYALTY PARTNERS, LP, AS ADMINISTRATIVE AGENT
Reel/Frame 061119/0920 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 13, 2022
From: ATHENEX, INC.
To: ATNX SPV, LLC
Reel/Frame 061071/0086 →
SECURITY INTEREST Recorded Jun 22, 2020
From: ATHENEX, INC.
To: OAKTREE FUND ADMINISTRATION, LLC
Reel/Frame 053005/0657 →
RELEASE OF SECURITY INTEREST Recorded Jun 19, 2020
From: PERCEPTIVE CREDIT HOLDINGS II, LP
To: ATHENEX, INC.
Reel/Frame 052990/0677 →
PATENT SECURITY AGREEMENT Recorded Jul 3, 2018
From: ATHENEX, INC.
To: PERCEPTIVE CREDIT HOLDINGS II, LP
Reel/Frame 047247/0812 →
CHANGE OF NAME Recorded Sep 21, 2015
From: KINEX PHARMACEUTICALS, INC.
To: ATHENEX, INC.
Reel/Frame 036644/0296 →
CHANGE OF NAME Recorded Sep 10, 2015
From: KINEX PHARMACEUTICALS, LLC
To: KINEX PHARMACEUTICALS, INC.
Reel/Frame 036585/0786 →
CONFIRMATORY LICENSE Recorded Feb 24, 2015
From: UNIVERSITY OF KANSAS LAWRENCE
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 035072/0377 →
CONFIRMATORY LICENSE Recorded Mar 31, 2014
From: UNIVERSITY OF KANSAS LAWRENCE
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 032568/0507 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 25, 2013
From: HANGAUER, DAVID G., JR.
To: KINEX PHARMACEUTICALS, LLC
Reel/Frame 030874/0034 →
Continuity (7)
Continuation 13152949 · Jun 3, 2011
Continuation 11480174 · Jun 29, 2006
Continuation In Part 11321419 · Dec 28, 2005
Provisional Application 60639834 · Dec 28, 2004
Provisional Application 60704551 · Aug 1, 2005
Provisional Application 60727341 · Oct 17, 2005
Related Publication 20120270874A1 · Oct 25, 2012