IP Library Granted Patent US 9,655,903
Granted Patent B2
US 9,655,903 · App. 14/658,736 · Granted May 23, 2017

Compositions and methods of treating cell proliferation disorders

Inventor: David G. Hangauer, Jr. (Lancaster, NY)
Assignee: Athenex, Inc.
A61K31/5377A61K31/4418A61K31/4425A61K31/4545A61K31/496A61K31/506C07C233/13C07C233/22C07D213/56C07D213/61C07D213/64C07D213/74C07D213/89C07D239/26C07D239/30C07D239/34C07D401/12C07D403/04
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Quick Facts
Patent No.
US 9,655,903
App. No.
14/658,736
Granted
May 23, 2017
Kind
B2
Abstract

The invention relates to compounds and methods for treating cell proliferation disorders.

Claims (49)

1. A method of lessening a disease or disorder that is modulated by tyrosine kinase inhibition selected from the group consisting of: diabetic retinopathy, macular degeneration, psoriasis, solid tumors, lung cancer, breast cancer, colon cancer, ovarian cancer, brain cancer, liver cancer, pancreatic cancer, prostate cancer, malignant melanoma, non-melanoma skin cancer, hematologic tumors, childhood leukemia, lymphoma, multiple myeloma, Hodgkin's disease, lymphomas of lymphocytic or cutaneous origin, acute or chronic leukemia, acute lymphoblastic leukemia, acute myelocytic leukemia, chronic myelocytic leukemia, plasma cell neoplasm, lymphoid neoplasm, epidermic or dermoid cysts, lipomas, adenomas, capillary or cutaneous hemangiomas, lymphangiomas, nevi lesions, teratomas, nephromas, myofibromatosis, osteoplastic tumors, dysplastic masses, and dysplasias, wherein the lessening results in the improvement of the disease or disorder;

comprising administering a pharmaceutical composition comprising a compound according to Formula I:

or a pharmaceutically acceptable salt, tautomer, or prodrug thereof, and at least one pharmaceutically acceptable excipient to a subject in need thereof, wherein:

T is a bond;

X y is CY, N, or N—O;

X z is CZ;

Y is 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, or O-benzyl;

X a is CR a , N, or N—O;

X b is CR b , N, or N—O;

X c is CR c , N, or N—O;

X d is CR d , N, or N—O;

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, 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, C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl-O-lower (C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 ) alkyl, 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,

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

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 —;

R 7 , R 8 , R 9 , R 10 , and R 11 are, independently, hydrogen, hydroxyl, halogen, unsubstituted C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl, unsubstituted 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, unsubstituted C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl-OH, C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl-O—C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl,

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 1,

wherein at least one of X a , X b , X c , X d , and X e is N; provided that when X a is N, X e is not N.

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

3. The method of claim 1 , wherein Y is hydrogen.

4. The method of claim 1 , wherein Z is

5. The method of claim 1 , wherein R b is C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkoxy.

6. The method of claim 1 , wherein R b is

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

7. The method of claim 6 , wherein V is a bond.

8. The method of claim 1 , wherein X a is N, X b is CR b , X e is CR c , X d is CR a and X e is CR e .

9. The method of claim 1 , wherein said compound is a pharmaceutically acceptable salt.

10. The method of claim 1 , wherein said compound is selected from the group consisting of

11. The method of claim 1 , wherein said compound has the formula:

or a pharmaceutically acceptable salt, tautomer or prodrug thereof.

12. The method of claim 1 , wherein said compound has the formula:

13. A method of lessening a disease or disorder that is modulated by tyrosine kinase inhibition selected from the group consisting of: diabetic retinopathy, macular degeneration, psoriasis, solid tumors, lung cancer, breast cancer, colon cancer, ovarian cancer, brain cancer, liver cancer, pancreatic cancer, prostate cancer, malignant melanoma, non-melanoma skin cancer, hematologic tumors, childhood leukemia, lymphoma, multiple myeloma, Hodgkin's disease, lymphomas of lymphocytic or cutaneous origin, acute or chronic leukemia, acute lymphoblastic leukemia, acute myelocytic leukemia, chronic myelocytic leukemia, plasma cell neoplasm, lymphoid neoplasm, epidermic or dermoid cysts, lipomas, adenomas, capillary or cutaneous hemangiomas, lymphangiomas, nevi lesions, teratomas, nephromas, myofibromatosis, osteoplastic tumors, dysplastic masses, and dysplasias, wherein the lessening results in the improvement of the disease or disorder;

comprising administering a pharmaceutical composition comprising a compound that is

or a pharmaceutically acceptable salt, tautomer, or prodrug thereof, and at least one pharmaceutically acceptable excipient to a subject in need thereof.

14. A method of lessening a disease or disorder that is modulated by tyrosine kinase inhibition selected from the group consisting of: diabetic retinopathy, macular degeneration, psoriasis, solid tumors, lung cancer, breast cancer, colon cancer, ovarian cancer, brain cancer, liver cancer, pancreatic cancer, prostate cancer, malignant melanoma, non-melanoma skin cancer, hematologic tumors, childhood leukemia, lymphoma, multiple myeloma, Hodgkin's disease, lymphomas of lymphocytic or cutaneous origin, acute or chronic leukemia, acute lymphoblastic leukemia, acute myelocytic leukemia, chronic myelocytic leukemia, plasma cell neoplasm, lymphoid neoplasm, epidermic or dermoid cysts, lipomas, adenomas, capillary or cutaneous hemangiomas, lymphangiomas, nevi lesions, teratomas, nephromas, myofibromatosis, osteoplastic tumors, dysplastic masses, and dysplasias, wherein the lessening results in the improvement of the disease or disorder;

comprising administering a pharmaceutical composition comprising a compound according to Formula II:

or a pharmaceutically acceptable salt, tautomer, or prodrug thereof, and at least one pharmaceutically acceptable excipient to a subject in need thereof, wherein:

R b , R 4 , R 5 , R 8 , and R 10 are, independently, 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 , or C 6 alkyl-OH, C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 alkyl-O-lower (C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 ) alkyl, COOH, COO-lower (C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 ) alkyl, SO 2 H, or SO 2 -lower (C 1 , C 2 , C 3 , C 4 , C 5 , or C 6 ) alkyl,

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

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 —.

15. A method of lessening a disease or disorder that is modulated by tyrosine kinase inhibition selected from the group consisting of: diabetic retinopathy, macular degeneration, psoriasis, solid tumors, lung cancer, breast cancer, colon cancer, ovarian cancer, brain cancer, liver cancer, pancreatic cancer, prostate cancer, malignant melanoma, non-melanoma skin cancer, hematologic tumors, childhood leukemia, lymphoma, multiple myeloma, Hodgkin's disease, lymphomas of lymphocytic or cutaneous origin, acute or chronic leukemia, acute lymphoblastic leukemia, acute myelocytic leukemia, chronic myelocytic leukemia, plasma cell neoplasm, lymphoid neoplasm, epidermic or dermoid cysts, lipomas, adenomas, capillary or cutaneous hemangiomas, lymphangiomas, nevi lesions, teratomas, nephromas, myofibromatosis, osteoplastic tumors, dysplastic masses, and dysplasias, wherein the lessening results in the improvement of the disease or disorder;

comprising administering a pharmaceutical composition comprising a compound selected from the group consisting of

or a pharmaceutically acceptable salt, tautomer, or prodrug thereof, and at least one pharmaceutically acceptable excipient to a subject in need thereof.

16. The method of claim 1 , wherein the disease or disorder that is modulated by tyrosine kinase inhibition is psoriasis.

17. The method of claim 13 , wherein the disease or disorder that is modulated by tyrosine kinase inhibition is psoriasis.

18. The method of claim 14 , wherein the disease or disorder that is modulated by tyrosine kinase inhibition is psoriasis.

19. The method of claim 15 , wherein the disease or disorder that is modulated by tyrosine kinase inhibition is psoriasis.

Assignments (8)
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 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 11, 2015
From: HANGAUER, DAVID G., JR
To: KINEX PHARMACEUTICALS, INC.
Reel/Frame 036301/0040 →
Continuity (7)
Division 12950764 · Nov 19, 2010
Continuation 11796200 · Apr 26, 2007
Continuation 11321419 · Dec 28, 2005
Provisional Application 60704551 · Aug 1, 2005
Provisional Application 60639834 · Dec 28, 2004
Provisional Application 60727341 · Oct 17, 2005
Related Publication 20150182532A1 · Jul 2, 2015