IP Library Granted Patent US 10,226,459
Granted Patent B2
US 10,226,459 · App. 15/719,949 · Granted Mar 12, 2019

Aza spiro alkane derivatives as inhibitors of metalloproteases

Inventors: Wenqing Yao (Chadds Ford, PA); Jincong Zhuo (Garnet Valley, PA); Meizhong Xu (Hockessin, DE); Fenglei Zhang (Berwyn, PA); Brian W. Metcalf (Moraga, CA)
Assignees: Incyte Holdings Corporation; Incyte Corporation
A61K31/496A61K31/40A61K31/454A61K31/4545A61K31/4709A61K31/4725A61K31/495A61K31/4985A61K31/55A61K31/551C07D221/20C07D401/06C07D401/12C07D401/14C07D405/12C07D405/14C07D409/14C07D417/14C07D471/04C07D487/04C07D495/04
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Quick Facts
Patent No.
US 10,226,459
App. No.
15/719,949
Granted
Mar 12, 2019
Kind
B2
Abstract

The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.

Claims (10)

1. A method for treating a disease associated with unwanted ADAM10, ADAM15, or ADAM17 activity in a mammalian subject, the method comprising administering to said mammal in need thereof a therapeutically effective amount of a compound which is methyl (6S,7S)-7-[(hydroxyamino)carbonyl]-6-[(4-phenylpiperazin-1-yl)carbonyl]-5-azaspiro[2.5]octane-5-carboxylate, or a pharmaceutically acceptable salt thereof, wherein the disease is selected from breast cancer, ovarian cancer, prostate cancer, non-small cell lung cancer, colon cancer, gastric cancer, pancreatic cancer, and glioma.

2. The method of claim 1 , wherein the disease is associated with unwanted ADAM10 activity.

3. The method of claim 1 , wherein the disease is associated with unwanted ADAM15 activity.

4. The method of claim 1 , wherein the disease is associated with unwanted ADAM17 activity.

5. The method of claim 1 , wherein the disease is glioma.

6. The method of claim 1 , wherein the compound methyl (6S,7S)-7-[(hydroxyamino)carbonyl]-6-[(4-phenylpiperazin-1-yl)carbonyl]-5-azaspiro[2.5]octane-5-carboxylate is administered.

7. The method of claim 2 , wherein the compound methyl (6S,7S)-7-[(hydroxyamino)carbonyl]-6-[(4-phenylpiperazin-1-yl)carbonyl]-5-azaspiro[2.5]octane-5-carboxylate is administered.

8. The method of claim 3 , wherein the compound methyl (6S,7S)-7-[(hydroxyamino)carbonyl]-6-[(4-phenylpiperazin-1-yl)carbonyl]-5-azaspiro[2.5]octane-5-carboxylate is administered.

9. The method of claim 4 , wherein the compound methyl (6S,7S)-7-[(hydroxyamino)carbonyl]-6-[(4-phenylpiperazin-1-yl)carbonyl]-5-azaspiro[2.5]octane-5-carboxylate is administered.

10. The method of claim 5 , wherein the compound methyl (6S,7S)-7-[(hydroxyamino)carbonyl]-6-[(4-phenylpiperazin-1-yl)carbonyl]-5-azaspiro[2.5]octane-5-carboxylate is administered.

Assignments (3)
CORRECTIVE ASSIGNMENT TO CORRECT THE OMITTED ASSIGNEE PREVIOUSLY RECORDED AT REEL: 045897 FRAME: 0681. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Jan 17, 2019
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION; INCYTE CORPORATION
Reel/Frame 048085/0168 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 24, 2018
From: YAO, WENQING; ZHUO, JINCONG; XU, MEIZHONG; ZHANG, FENGLEI; METCALF, BRIAN W.
To: INCYTE CORPORATION
Reel/Frame 045897/0627 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 24, 2018
From: INCYTE CORPORATION
To: INCYTE HOLDINGS CORPORATION
Reel/Frame 045897/0681 →
Continuity (8)
Continuation 15204423 · Jul 7, 2016
Continuation 14092351 · Nov 27, 2013
Continuation 13184860 · Jul 18, 2011
Continuation 12327313 · Dec 3, 2008
Continuation 10831265 · Apr 23, 2004
Provisional Application 60534501 · Jan 6, 2004
Provisional Application 60466159 · Apr 24, 2003
Related Publication 20180153882A1 · Jun 7, 2018