IP Library Granted Patent US 10,730,889
Granted Patent B2
US 10,730,889 · App. 15/936,086 · Granted Aug 4, 2020

Amido spirocyclic amide and sulfonamide derivatives

Inventors: Kenneth W. Bair (Wellesley, MA); Timm R. Baumeister (Watertown, MA); Peter Dragovich (South San Francisco, CA); Xiongcai Liu (Beijing, CN); Snahel Patel (South San Francisco, CA); Po-Wai Yuen (Beijing, CN); Mark Zak (South San Francisco, CA); Guiling Zhao (South San Francisco, CA); Yamin Zhang (Beijing, CN); Xiaozhang Zheng (Lexington, MA)
Assignees: FORMA TM, LLC; Genentech, Inc.
C07D519/00A61K31/438A61K31/444A61K31/4545A61K31/496A61K31/497A61K31/501A61K31/506A61K31/513A61K31/519A61K31/5377A61K31/541A61K45/06C07D471/04C07D487/04C07D491/048C07D495/04
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Quick Facts
Patent No.
US 10,730,889
App. No.
15/936,086
Granted
Aug 4, 2020
Kind
B2
Abstract

Provided are amido spirocyclic amide and sulfonamide compounds, pharmaceutical compositions comprising such compounds, and methods of treatment using such compounds.

Claims (23)

1. A compound of Formula I-a:

or a pharmaceutically acceptable salt thereof, wherein:

R is

R 1 is —C(O)R a or —CO 2 R a ;

wherein each R a is independently

(1) alkyl; or

(2) heteroaryl or heterocycloalkyl, each substituted with one or more alkyl; and

R 2 and R 3 are each H.

2. The compound of claim 1 , wherein R 1 is —C(O)R a .

3. The compound of claim 2 , wherein R a is alkyl.

4. The compound of claim 3 , wherein R a is isobutyl.

5. The compound of claim 2 , wherein R a is heteroaryl or heterocycloalkyl, each substituted with one or more alkyl.

6. The compound of claim 5 , wherein R a is 2,4-dimethyloxazolyl.

7. The compound of claim 1 , wherein R 1 is —CO 2 R a .

8. The compound of claim 7 , wherein R a is alkyl.

9. The compound of claim 8 , wherein R a is tert-butyl.

10. The compound of claim 8 , wherein R a is isopropyl.

11. The compound of claim 7 , wherein R a is heteroaryl or heterocycloalkyl, each substituted with one or more alkyl.

12. The compound of claim 11 , wherein R a is 3-methyloxetan-3-yl.

13. The compound of claim 1 , wherein the compound is tert-butyl 2-[(1,3-dihydropyrrolo[3,4-c]pyridine-2-carbonylamino)methyl]-6-azaspiro[2.5]octane-6-carboxylate.

14. The compound of claim 1 , wherein the compound is isopropyl 2-[(1,3-dihydropyrrolo[3,4-c]pyridine-2-carbonylamino)methyl]-6-azaspiro[2.5]octane-6-carboxylate.

15. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.

16. The pharmaceutical composition of claim 15 , comprising the compound of claim 1 as a pharmaceutically acceptable salt.

Assignments (12)
RELEASE OF SECURITY INTEREST Recorded Oct 17, 2023
From: FIRST-CITIZENS BANK & TRUST COMPANY, AS AGENT
To: VALO HEALTH, INC.; VALO HEALTH, LLC
Reel/Frame 065255/0660 →
SECURITY INTEREST Recorded Jul 6, 2023
From: VALO HEALTH, LLC; VALO HEALTH, INC.
To: FIRST-CITIZENS BANK & TRUST COMPANY, AS AGENT
Reel/Frame 064207/0957 →
MERGER Recorded Sep 8, 2021
From: VALO EARLY DISCOVERY, INC.
To: VALO HEALTH, INC.
Reel/Frame 057438/0025 →
CHANGE OF NAME Recorded Sep 16, 2020
From: INTEGRAL EARLY DISCOVERY, INC.
To: VALO EARLY DISCOVERY, INC.
Reel/Frame 053787/0138 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 5, 2020
From: FORMA THERAPEUTICS, INC.
To: INTEGRAL EARLY DISCOVERY, INC.
Reel/Frame 053402/0298 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 3, 2020
From: FORMA TM, LLC
To: FORMA THERAPEUTICS, INC.
Reel/Frame 053387/0440 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 31, 2018
From: FORMA THERAPEUTICS, INC.
To: FORMA TM, LLC
Reel/Frame 046513/0563 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 31, 2018
From: BAIR, KENNETH W.; BAUMEISTER, TIMM R.; ZHENG, XIAOZHANG
To: FORMA THERAPEUTICS, INC.
Reel/Frame 046513/0359 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 31, 2018
From: DRAGOVICH, PETER; PATEL, SNAHEL; ZAK, MARK; ZHAO, GUILING
To: GENENTECH, INC.
Reel/Frame 046513/0389 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 31, 2018
From: LIU, XIONGCAI; YUEN, PO-WAI; ZHANG, YAMIN
To: PHARMARON BEIJING, CO., LTD.
Reel/Frame 046513/0447 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 31, 2018
From: PHARMARON BEIJING, CO., LTD.
To: PHARMARON, INC.
Reel/Frame 046513/0496 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 31, 2018
From: PHARMARON, INC.
To: GENENTECH, INC.
Reel/Frame 046513/0512 →
Continuity (4)
Continuation 15473110 · Mar 29, 2017
Continuation 14382210
Provisional Application 61606291 · Mar 2, 2012
Related Publication 20180339998A1 · Nov 29, 2018
Cited By (1)
US 12,336,981