Pyrrolopyrimidine comprising cyclopentyl substituent

Patent metadata

Field	Value
Publication number	US-10617692-B2
Application number	US-201716310221-A
Country	US
Kind code	B2
Filing date	Jun 15, 2017
Priority date	Jun 16, 2016
Publication date	Apr 14, 2020
Grant date	Apr 14, 2020

Abstract

A pyrrolopyrimidine comprising a cyclopentyi substituent. The present invention specifically relates to a compound represented by formula. A and a stereoisomer and pharmaceutically acceptable salt thereof. The invention further relates to a method for manufacturing the pyrrolopyrimidine comprising the cyclopentyl substituent represented by formula A, a pharmaceutical composition, and an application of the compound in treating a disease induced by Janus kinase.

First claim

What is claimed is:

1. A compound represented by formula A, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof:

wherein R 1 and R 4 are each independently selected from the group consisting of H, hydroxyl, and oxo; and R 2 and R 3 are each independently selected from the group consisting of H, and oxo; with the proviso that R 1 , R 2 , R 3 , and R 4 are not all H.

2. The compound represented by formula A according to claim 1 , wherein R 1 and R 2 are both H.

3. The compound represented by formula A according to claim 1 , wherein one of R 3 and R 4 is H, and the other is hydroxyl or oxo.

4. The compound according to claim 1 , wherein the compound is selected from the group consisting of:

5. A pharmaceutical composition, comprising the compound according to claim 1 , a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable carriers or excipients.

6. A pharmaceutical composition, comprising the compound according to claim 4 , a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable carriers or excipients.

7. A method for treating a disease mediated by Janus kinase, comprising administering to a patient a therapeutically effective amount of the compound according to claim 1 , a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, wherein the disease mediated by Janus kinase is lymphoma or leukemia.

8. The method according to claim 7 , further comprising administering to a patient one or more pharmaceutically acceptable carriers or excipients.

9. A method according to claim 7 , wherein the compound is selected from the group consisting of:

or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof.

10. The method according to claim 9 , further comprising administering one or more pharmaceutically acceptable carriers or excipients.

11. A method for inhibiting Janus kinase, comprising administering an effective amount of the compound according to claim 1 .

12. The method according to claim 11 , further comprising administering one or more pharmaceutically acceptable carriers or excipients.

13. The method according to claim 11 , wherein the compound is selected from the group consisting of:

or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof.

14. The method of claim 13 , further comprising administering one or more pharmaceutically acceptable carriers or excipients.

Assignees

• Centaurus Biopharma Co Ltd
• Chia Tai Tianqing Pharmaceutical Group Co Ltd
• Lianyungang Runzhong Pharmaceutical Co Ltd
• Centaurus Biopharma Co
• Chia Tai Tianqing Pharmaceutical Group Co

Inventors

• Zhu Li
• Liu Yangjian
• Zhang Chuanyu
• Wang He
• Luo Hong
• Sun Yinghui
• Han Yongxin

Classifications

• A61K31/519 Primary

  ortho- or peri-condensed with heterocyclic rings · CPC title

• C07D487/04 Primary

  Ortho-condensed systems · CPC title

• A61P35/00

  Antineoplastic agents · CPC title