IP Library Granted Patent US 9,150,527
Granted Patent B2
US 9,150,527 · App. 14/342,323 · Granted Oct 6, 2015

Metalloenzyme inhibitor compounds

Inventors: William J. Hoekstra (Durham, NC); Robert J. Schotzinger (Raleigh, NC)
Assignee: Innocrin Pharmaceuticals, Inc.
C07D277/24A01N43/78A01N43/84A01N43/90A61K31/427A61K31/542A61K45/06C07D277/22C07D277/28C07D277/32C07D277/56C07D417/06C07D417/12C07D417/14C07D513/04
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Quick Facts
Patent No.
US 9,150,527
App. No.
14/342,323
Granted
Oct 6, 2015
Kind
B2
Abstract

The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

Claims (18)

1. A compound of formula (II):

wherein R 2 is optionally substituted aryl, optionally substituted naphthyl, optionally substituted heteroaryl, optionally substituted alkyl, optionally substituted aralkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, or optionally substituted heteroaryl-alkyl;

R 3 is H, OH, alkoxy, amino, alkylamino, or dialkylamino;

R 4 is chloro;

R 5 is halogen, alkoxy, fluoroalkoxy containing 1-5 fluorines, cyano, carboxamido, optionally substituted aryl, or optionally substituted heteroaryl; and

R 6 is H, halogen, alkoxy, fluoroalkoxy containing 1-5 fluorines, cyano, carboxamido, optionally substituted aryl, or optionally substituted heteroaryl.

2. A compound that is:

1-(2-Chloro-thiazol-5-yl)-1-(6,7-dimethoxynaphthalen-2-yl)-2-methylpropan-1-ol  (1); or

1-(6,7-dimethoxynaphthalen-2-yl)-2-methyl-1-(thiazol-5-yl)propan-1-ol  (2).

3. A method of treating a subject suffering from a metalloenzyme-related disorder or disease, wherein the subject has been identified as in need of treatment for a metalloenzyme-related disorder or disease, comprising administering to said subject in need thereof, an effective amount of a compound of claim 1 , such that said subject is treated for said disorder;

wherein the disease or disorder is prostate cancer, breast cancer, testicular cancer, uterine cancer, or ovarian cancer.

4. The method of claim 3 , wherein the disease or disorder is prostate cancer.

5. A composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.

6. The composition of claim 5 further comprising an additional therapeutic agent.

7. The composition of claim 6 further comprising an additional therapeutic agent that is an anti-cancer agent, antifungal agent, cardiovascular agent, antiinflammatory agent, chemotherapeutic agent, an anti-angiogenesis agent, cytotoxic agent, an anti-proliferation agent, metabolic disease agent, opthalmologic disease agent, central nervous system (CNS) disease agent, urologic disease agent, or gastrointestinal disease agent.

8. The compound of claim 1 , wherein R 3 is OH.

9. The compound of claim 1 , wherein R 2 is optionally substituted alkyl and R 3 is OH.

10. The compound of claim 1 , wherein R 2 is alkyl and R 3 is OH.

Assignments (2)
CHANGE OF NAME Recorded Nov 6, 2014
From: VIAMET PHARMACEUTICALS, INC.
To: INNOCRIN PHARMACEUTICALS, INC.
Reel/Frame 034181/0572 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 23, 2014
From: HOEKSTRA, WILLIAM J.; SCHOTZINGER, ROBERT J.
To: VIAMET PHARMACEUTICALS, INC.
Reel/Frame 032734/0861 →
Continuity (2)
Provisional Application 61528953 · Aug 30, 2011
Related Publication 20140303157A1 · Oct 9, 2014