.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

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

DrugPatentWatch Database Preview

Details for Patent: 7,754,739

« Back to Dashboard

Details for Patent: 7,754,739

Title:Modulators of CFTR
Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette ("ABC") transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator ("CFTR"). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
Inventor(s): Hadida Ruah; Sara S. (La Jolla, CA), Miller; Mark (San Diego, CA), Bear; Brian (Oceanside, CA), Zhou; Jinglan (San Diego, CA), McCartney; Jason (Cardiff by the Sea, CA), Grootenhuis; Peter (San Diego, CA)
Assignee: Vertex Pharmaceuticals Incorporated (Cambridge, MA)
Filing Date:May 09, 2008
Application Number:12/117,948
Claims:1. A compound of formula I: ##STR00023## or a pharmaceutically acceptable salt thereof, wherein independently for each occurrence: m is 0-4; R.sub.M is Z.sup.MR.sub.11, wherein each Z.sup.M is a bond or an optionally substituted branched or straight C.sub.1-6 aliphatic chain wherein up to two carbon units of Z.sup.M are optionally replaced by --CO--, --CS--, --CONR.sup.N--, --CO.sub.2--, --OCO--, --NR.sup.NCO.sub.2--, --O--, --OCONR.sup.N--, --NR.sup.NCO--, --S--, --SO--, --SO.sub.2--, or --NR.sup.N--; R.sub.11 is R.sup.N, halo, --OH, --NH.sub.2, --NO.sub.2, --CN, --CF.sub.3, or --OCF.sub.3; R.sup.N is H or an optionally substituted C1-C8 aliphatic; R.sub.1 is a C1-C6 aliphatic; R.sub.2 is H or an optionally substituted C1-C6 aliphatic; R.sub.3 and R'.sub.3 together with the carbon atom to which they are attached form an unsubstituted C.sub.3-7 cycloalkyl ring; and R4 is: ##STR00024##

2. The compound of claim 1, wherein R.sub.1 is an optionally substituted C1-C4 aliphatic.

3. The compound of claim 1, wherein R.sub.1 is an optionally substituted C1-C4 alkyl.

4. The compound of claim 1, wherein R.sub.1 is methyl, ethyl, propyl, or butyl.

5. The compound of claim 1, wherein R.sub.2 is H.

6. The compound of claim 1, wherein R.sub.2 is a C1-C6 aliphatic.

7. The compound of claim 1, wherein R.sub.2 is a C1-C6 alkyl.

8. The compound of claim 1, wherein R.sub.2 is methyl, ethyl, propyl, butyl, pentyl, or hexyl.

9. The compound of claim 1, wherein R.sub.3 and R'.sub.3 taken together form a cyclopropyl ring.

10. The compound of claim 1, wherein R.sub.3 and R'.sub.3 taken together form a cyclopentyl ring.

11. The compound of claim 1, wherein R.sub.4 is ##STR00025##

12. The compound of claim 1, wherein R.sub.4 is ##STR00026##

13. The compound of claim 1, wherein m is 0.

14. The compound of claim 1, having formula II: ##STR00027##

15. The compound of claim 14, wherein R.sub.1 is methyl.

16. The compound of claim 14, wherein m is 0.

17. The compound of claim 1, having formula III: ##STR00028##

18. The compound of claim 17, wherein R.sub.1 is methyl.

19. The compound of claim 17, wherein m is 0.

20. The compound of claim 1, wherein the compound is ##STR00029##

21. A pharmaceutical composition comprising: (i) a compound according to claim 1; and (ii) a pharmaceutically acceptable carrier.

22. The composition according to claim 21, further comprising a mucolytic agent, a bronchodialator, an antibiotic, an anti-infective agent, an anti-inflammatory agent, a CFTR modulator, or a nutritional agent.

23. A method of modulating CFTR activity comprising the step of contacting said CFTR with a compound according to claim 1.

24. A method of treating or lessening the severity of a disease in a patient, wherein said disease is selected from cystic fibrosis, hereditary emphysema, or COPD, said method comprising the step of administering to said patient an effective amount of a compound according to claim 1.

25. A kit for use in measuring the activity of CFTR or a fragment thereof in a biological sample in vitro or in vivo, comprising: (i) a compound according claim 1; and (ii) instructions for: a) contacting the compound with the biological sample; and b) measuring activity of said CFTR or a fragment thereof.

26. The kit according to claim 25, further comprising instructions for a) contacting an additional compound with the biological sample; b) measuring the activity of said CFTR or a fragment thereof in the presence of said additional compound, and c) comparing the activity of said CFTR in the presence of the additional compound with the activity of said CFTR in the presence of a compound of claim 1.

27. The method of claim 24, wherein the disease is cystic fibrosis.
« Back to Dashboard

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

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.

`abc