.

Deeper Knowledge, Faster

  • Analyze global market entry opportunities
  • Identify first generic entrants
  • Obtain formulation and manufacturing information

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

Serving leading biopharmaceutical companies globally:

US Department of Justice
Express Scripts
Moodys
Citi
Fish and Richardson
Argus Health
Teva
Merck
QuintilesIMS
Cantor Fitzgerald

Generated: February 23, 2018

DrugPatentWatch Database Preview

Details for Patent: ➤ Sign Up

« Back to Dashboard

Details for Patent: ➤ Sign Up

Title:Compounds and compositions as protein kinase inhibitors
Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.
Inventor(s): Michellys; Pierre-Yves (San Marcos, CA), Pei; Wei (San Diego, CA), Marsilje; Thomas H. (San Diego, CA), Chen; Bei (San Diego, CA), Uno; Tetsuo (San Diego, CA), Jin; Yunho (San Diego, CA), Jiang; Tao (San Diego, CA)
Assignee: IRM LLC (Hamilton, BM)
Filing Date:Mar 15, 2011
Application Number:13/048,636
Claims:1. A compound having Formula (1): ##STR00363## or pharmaceutically acceptable salts thereof; wherein W is ##STR00364## A.sup.1 and A.sup.4 are independently C; each A.sup.2 and A.sup.3 is C; R.sup.1 and R.sup.2 together form an optionally substituted 5-6 membered aryl, or heteroaryl or heterocyclic ring comprising 1-3 nitrogen atoms; R.sup.3 is (CR.sub.2).sub.0-2SO.sub.2R.sup.12, (CR.sub.2).sub.0-2SO.sub.2NRR.sup.12, (CR.sub.2).sub.0-2C(O)O.sub.0-1R.sup.12, (CR.sub.2).sub.0-2CONRR.sup.12, CO.sub.2NH.sub.2, or cyano; R.sup.4, R.sup.7 and R.sup.10 are independently H; R, R.sup.5 and R.sup.5' are independently H or C.sub.1-6 alkyl; R.sup.6 is halo or O(C.sub.1-6 alkyl); R.sup.8 and R.sup.9 are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, halo or X, or one of R.sup.8 and R.sup.9 is H; and provided one of R.sup.8 and R.sup.9 is X; X is (CR.sub.2).sub.qY, cyano, C(O)O.sub.0-1R.sup.12, CONR(R.sup.12), CONR(CR.sub.2).sub.pNR(R.sup.12), CONR(CR.sub.2).sub.pOR.sup.12, CONR(CR.sub.2).sub.pSR.sup.12, CONR(CR.sub.2).sub.pS(O).sub.1-2R.sup.12 or (CR.sub.2).sub.1-6NR(CR.sub.2).sub.pOR.sup.12; Y is an optionally substituted 3-12 membered carbocyclic ring, a 5-12 membered aryl, or a 5-12 membered heteroaryl or heterocyclic ring comprising N, O and/or S and attached to A.sup.2 or A.sup.3 or both via a carbon atom of said heteroaryl or heterocyclic ring when q in (CR.sub.2).sub.qY is 0; R.sup.12 is an optionally substituted 3-7 membered saturated or partially unsaturated carbocyclic ring, or a 5-7 membered heterocyclic ring comprising N, O and/or S; aryl or heteroaryl; or R.sup.12 is H, C.sub.1-6 alkyl; and n is 0; and p and q are independently 0-4.

2. The compound of claim 1, wherein R.sup.3 is SO.sub.2R.sup.12, SO.sub.2NH.sub.2, SO.sub.2NRR.sup.12, CO.sub.2NH.sub.2, CONRR.sup.12, C(O)O.sub.0-1R.sup.12, or cyano; and R.sup.12 is C.sub.1-6 alkyl, an optionally substituted C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkenyl, pyrrolidinyl, piperazinyl, piperidinyl or morpholinyl.

3. The compound of claim 1, wherein said compound is selected from the group consisting of ##STR00365## ##STR00366## ##STR00367## ##STR00368## ##STR00369## ##STR00370## ##STR00371## ##STR00372## or pharmaceutically acceptable salts thereof.

4. The compound of claim 1, wherein said compound is selected from the group consisting of: ##STR00373## ##STR00374## ##STR00375## ##STR00376## or pharmaceutically acceptable salts thereof.

5. The compound of claim 1, wherein said compound is selected from the group consisting of ##STR00377## ##STR00378## ##STR00379## or pharmaceutically acceptable salts thereof.

6. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.

7. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 3 and a pharmaceutically acceptable carrier.

8. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 4 and a pharmaceutically acceptable carrier.

9. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 5 and a pharmaceutically acceptable carrier.

10. The compound of claim 1, wherein said compound is N6-(4-(1-ethylpiperidin-4-yl)-2-isopropoxy-5-methylphenyl)-N4-(2-(isoprop- ylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidine-4,6-diamine, or pharmaceutically acceptable salts thereof.

11. The compound of claim 1, wherein said compound is N6-(2-isopropoxy-5-methyl-4-(1-methylpiperidin-4-yl)phenyl)-N4-(2-(isopro- pylsulfonyl)phenyl)-1H-pyrazolo[3,4-d]pyrimidine-4,6-diamine, or pharmaceutically acceptable salts thereof.

12. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 10 and a pharmaceutically acceptable carrier.

13. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 10 and a pharmaceutically acceptable carrier.
« Back to Dashboard

For more information try a trial or see the plans and pricing

Serving leading biopharmaceutical companies globally:

Cipla
Novartis
Farmers Insurance
Fish and Richardson
Fuji
Cerilliant
Medtronic
McKinsey
AstraZeneca
Healthtrust

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

Copyright 2002-2018 thinkBiotech LLC
ISSN: 2162-2639

Secure SSL Encrypted
Privacy and Cookies
Terms & Conditions

Follow DrugPatentWatch:

botpot