IP Library Granted Patent US 8,741,896
Granted Patent B2
US 8,741,896 · App. 13/502,554 · Granted Jun 3, 2014

Pyrazolopyrimidine derivatives

Inventors: Hans Peter Buchstaller (Griesheim, DE); Ulrich Emde (Darmstadt, DE); Markus Klein (Darmstadt, DE); Christina Esdar (Mainz, DE); Joerg Bomke (Heidelberg, DE)
Assignee: Merck Patent GmbH
A61K31/5377A61K31/4985C07D413/14C07D487/02
View Patent ↗
Loading inventors, assignments & file history…
Monitor This Case
Get email alerts when status or documents change.
Order Certified Copies
Most orders are placed with the USPTO same day — all within 24 business hours.
Order via The Patent Place →
Pre-filled with this patent's details
Quick Facts
Patent No.
US 8,741,896
App. No.
13/502,554
Granted
Jun 3, 2014
Kind
B2
Abstract

Compounds of the formula (I), in which X, R 1 and R 2 have the meanings indicated in claim 1 , are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumors.

Claims (48)

1. A compound selected from the following compounds:

Compound No.

Name and/or structure

“A65” 

4-(1H-Indol-6-yl)-1-methyl-6-morpholin-4-yl-1H-

pyrazolo[3,4-d]pyrimidine

“A97” 

4-(1H-Indol-4-yl)-1-methyl-6-morpholin-4-yl-1H-

pyrazolo[3,4-d]pyrimidine

“A129”

4-(1H-Benzimidazol-5-yl)-1-methyl-6-morpholin-4-yl-

1H-pyrazolo[3,4-d]pyrimidine

“A161”

4-(1H-Indazol-4-yl)-1-methyl-6-morpholin-4-yl-1H-

pyrazolo[3,4-d]pyrimidine

“A193”

5-(1-Methyl-6-morpholin-4-yl-1H-pyrazolo[3,4-d]-

pyrimidin-4-yl)pyridin-2-ylamine

“A196”

“A228”

“A229”

“A257”

Ethyl [4-(6-aminopyridin-3-yl)-6-morpholin-4-yl-

pyrazolo[3,4-d]pyrimidin-1-yl]acetate

“A258”

2-[4-(6-Aminopyridin-3-yl)-6-morpholin-4-yl-

pyrazolo[3,4-d]pyrimidin-1-yl]-1-pyrrolidin-1-yl-

ethanone

“A259”

Ethyl [4-(2-aminopyrimidin-5-yl)-6-morpholin-4-yl-

pyrazolo[3,4-d]pyrimidin-1-yl]acetate

“A260”

2-[4-(2-Aminopyrimidin-5-yl)-6-morpholin-4-yl-

pyrazolo[3,4-d]pyrimidin-1-yl]-1-pyrrolidin-1-yl-

ethanone

“A261”

2-[4-(2-Aminopyrimidin-5-yl)-6-morpholin-4-yl-

pyrazolo[3,4-d]pyrimidin-1-yl]-1-morpholin-4-yl-

ethanone

“A262”

2-[4-(2-Aminopyrimidin-5-yl)-6-morpholin-4-yl-

pyrazolo[3,4-d]pyrimidin-1-yl]-1-(4-methyl-piperazin-

1-yl)ethanone

or a pharmaceutically usable salt, tautomer or stereoisomer thereof, including mixtures thereof in all ratios.

2. A medicament composition comprising at least one compound according to claim 1 or a pharmaceutically usable salt, tautomer or stereoisomer thereof, including mixtures thereof in all ratios, and at least one excipient or adjuvant.

3. A kit consisting of separate packs of

(a) an effective amount of a compound according to claim 1 or a pharmaceutically usable salt, tautomer or stereoisomer thereof, including mixtures thereof in all ratios, and

(b) an effective amount of a further medicament active compound.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 18, 2012
From: BUCHSTALLER, HANS PETER; EMDE, ULRICH; KLEIN, MARKUS; ESDAR, CHRISTINA; BOMKE, JOERG
To: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
Reel/Frame 028063/0807 →
Priority Claims (1)
DE 10 2009 049 679 · Oct 19, 2009 · national
Continuity (1)
Related Publication 20120208808A1 · Aug 16, 2012