IP Library Granted Patent US 11,427,558
Granted Patent B1
US 11,427,558 · App. 16/925,398 · Granted Aug 30, 2022

Indazoles and azaindazoles as LRRK2 inhibitors

Inventors: Albert W. Garofalo (South San Francisco, CA); Stéphane De Lombaert (Brisbane, CA); Jacob Bradley Schwarz (South San Francisco, CA); Daniele Andreotti (San Giovanni Lupatoto, IT); Fabio Maria Sabbatini (Verona, IT); Elena Serra (Lecce, IT); Silvia Bernardi (Verona, IT); Marco Migliore (Verona, IT); Federica Budassi (Urbino, IT); Claudia Beato (Verona, IT)
Assignee: ESCAPE Bio, Inc.
C07D401/12C07D401/14C07D403/12C07D405/04C07D405/12C07D405/14C07D413/14C07D417/14C07D471/04
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Quick Facts
Patent No.
US 11,427,558
App. No.
16/925,398
Granted
Aug 30, 2022
Kind
B1
Abstract

The present invention is directed to indazole and azaindazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.

Claims (18)

1. A compound which is 5-cyano-N-(3-(1-(difluoromethyl)-1H-pyrazol-4-yl)-1H-indazol-5-yl)-3,4-dimethylpicolinamide, or a pharmaceutically acceptable salt thereof.

2. The compound of claim 1 , wherein the compound is 5-cyano-N-(3-(1-(difluoromethyl)-1H-pyrazol-4-yl)-1H-indazol-5-yl)-3,4-dimethylpicolinamide.

3. A pharmaceutical composition comprising a compound of claim 1 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

4. A method for treating a neurodegenerative disease in a patient, said method comprising: administering to the patient a therapeutically effective amount of the compound of claim 1 , or a pharmaceutically acceptable salt thereof.

5. The method of claim 4 , wherein said neurodegenerative disease is selected from Parkinson's disease, Parkinson disease with dementia, Parkinson's associated risk syndrome, dementia with Lewy bodies, Lewy body variant of Alzheimer's disease, combined Parkinson's disease and Alzheimer's disease, multiple system atrophy, striatonigral degeneration, olivopontocerebellar atrophy, and Shy-Drager syndrome.

6. The method of claim 4 , wherein said neurodegenerative disease is Parkinson's disease.

7. A compound which is 5-cyano-3,4-dimethyl-N-(3-(oxazol-5-yl)-1H-indazol-5-yl)picolinamide, or a pharmaceutically acceptable salt thereof.

8. The compound of claim 7 , wherein the compound is 5-cyano-3,4-dimethyl-N-(3-(oxazol-5-yl)-1H-indazol-5-yl)picolinamide.

9. A pharmaceutical composition comprising a compound of claim 7 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

10. A method for treating a neurodegenerative disease in a patient, said method comprising: administering to the patient a therapeutically effective amount of the compound of claim 7 , or a pharmaceutically acceptable salt thereof.

11. The method of claim 10 , wherein said neurodegenerative disease is selected from Parkinson's disease, Parkinson disease with dementia, Parkinson's associated risk syndrome, dementia with Lewy bodies, Lewy body variant of Alzheimer's disease, combined Parkinson's disease and Alzheimer's disease, multiple system atrophy, striatonigral degeneration, olivopontocerebellar atrophy, and Shy-Drager syndrome.

12. The method of claim 10 , wherein said neurodegenerative disease is Parkinson's disease.

13. A compound which is 6-chloro-5-cyano-N-(3-methoxy-1H-indazol-5-yl)-3,4-dimethylpicolinamide, or a pharmaceutically acceptable salt thereof.

14. The compound of claim 13 , wherein the compound is 6-chloro-5-cyano-N-(3-methoxy-1H-indazol-5-yl)-3,4-dimethylpicolinamide.

15. A pharmaceutical composition comprising a compound of claim 13 , or a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable carrier.

16. A method for treating a neurodegenerative disease in a patient, said method comprising: administering to the patient a therapeutically effective amount of the compound of claim 13 , or a pharmaceutically acceptable salt thereof.

17. The method of claim 16 , wherein said neurodegenerative disease is selected from Parkinson's disease, Parkinson disease with dementia, Parkinson's associated risk syndrome, dementia with Lewy bodies, Lewy body variant of Alzheimer's disease, combined Parkinson's disease and Alzheimer's disease, multiple system atrophy, striatonigral degeneration, olivopontocerebellar atrophy, and Shy-Drager syndrome.

18. The method of claim 16 , wherein said neurodegenerative disease is Parkinson's disease.

Assignments (4)
CHANGE OF NAME Recorded Nov 25, 2020
From: E-SCAPE BIO, INC.
To: ESCAPE BIO, INC.
Reel/Frame 054516/0098 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 18, 2020
From: GAROFALO, ALBERT W.; LOMBAERT, STÉPHANE DE; SCHWARZ, JACOB BRADLEY
To: E-SCAPE BIO, INC.
Reel/Frame 053520/0001 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 18, 2020
From: ANDREOTTI, DANIELE; SABBATINI, FABIO MARIA; SERRA, ELENA; BERNARDI, SILVIA; MIGLIORE, MARCO; BUDASSI, FEDERICA; BEATO, CLAUDIA
To: APTUIT (VERONA) SRL, AN EVOTEC COMPANY
Reel/Frame 053520/0052 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 18, 2020
From: APTUIT (VERONA) SRL, AN EVOTEC COMPANY
To: E-SCAPE BIO, INC.
Reel/Frame 053520/0111 →
Continuity (2)
Provisional Application 62937979 · Nov 20, 2019
Provisional Application 62872891 · Jul 11, 2019