Organic compounds

Patent metadata

Field	Value
Publication number	US-9403836-B2
Application number	US-201414461132-A
Country	US
Kind code	B2
Filing date	Aug 15, 2014
Priority date	Dec 6, 2007
Publication date	Aug 2, 2016
Grant date	Aug 2, 2016

Abstract

1- or 2-substituted (6aR,9aS)-3-(phenylamino)-5-6a,7,8,9,9a-hexahydro-5-methyl-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(1H or, 2H)-one compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.

First claim

What is claimed is:

1. A Compound of formula Q

wherein
(i) —X—Y—Z is 4-(6-fluoropyrid-2-yl)benzyl; or
(ii) —X is methylene; —Y— is phenylene; and —Z is —C(O)—R 1 wherein R 1 is methyl; or
(iii) —X is methylene; —Y— is phenylene; and —Z is trifluoromethyl; and
(iv) R 4 is H and R 5 phenyl substituted with one or more halo, hydroxy or C 1-6 alkoxy;

in free or salt form.

2. The compound according to claim 1 , in free or salt form, wherein —X—Y—Z is 4-(6-fluoropyrid-2-yl)benzyl.

3. The compound according to claim 2 , in free or salt form, wherein —X—Y—Z is substituted on the 2-position of Formula Q.

4. The compound according to claim 2 , in free or salt form, wherein R 5 is phenyl substituted with fluoro.

5. The compound according to claim 2 , in free or salt form, wherein R 5 is phenyl substituted with hydroxy.

6. The compound according to claim 2 , in free or salt form, wherein R 5 is 4-hydroxyphenyl.

7. The compound according to claim 2 , in free or salt form, wherein R 5 is 4-fluorophenyl.

8. The compound according to claim 3 , in free or salt form, wherein R 5 is phenyl substituted with fluoro.

9. The compound according to claim 3 , in free or salt form, wherein R 5 is phenyl substituted with hydroxy.

10. The compound according to claim 3 , in free or salt form, wherein R 5 is 4-fluorophenyl.

11. The compound according to claim 1 , wherein said compound is:

in free or salt form.

12. The compound according to claim 1 , wherein said compound is:

in free or salt form.

13. A pharmaceutical composition comprising a compound according to claim 1 , in free or pharmaceutically acceptable salt form, in combination or association with a pharmaceutically acceptable diluent or carrier.

14. A pharmaceutical composition comprising a compound according to claim 4 , in free or pharmaceutically acceptable salt form, in combination or association with a pharmaceutically acceptable diluent or carrier.

15. A pharmaceutical composition comprising a compound according to claim 5 , in free or pharmaceutically acceptable salt form, in combination or association with a pharmaceutically acceptable diluent or carrier.

Assignees

• Intra Cellular Therapies Inc

Inventors

• Li Peng

Classifications

• A61P37/02

  Immunomodulators · CPC title

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P5/14

  of the thyroid hormones, e.g. T3, T4 · CPC title