Deeper Knowledge, Faster

  • Identify first generic entrants
  • Uncover prior art in expired and abandoned patents
  • Obtain formulation and manufacturing information
➤ Start Trial

or, See Plans & Pricing

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

Serving leading biopharmaceutical companies globally:

Deloitte
Covington
Mallinckrodt
Daiichi Sankyo
Chubb
AstraZeneca
McKinsey
Novartis
Baxter
Express Scripts

Generated: January 22, 2018

DrugPatentWatch Database Preview

Claims for Patent: 5,292,756

« Back to Dashboard

Summary for Patent: 5,292,756
Title: Novel sulfonamide fibrinogen receptor antagonists
Abstract:A series of non-peptide derivatives of the formula ##STR1## that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
Inventor(s): Duggan; Mark E. (Narberth, PA), Egbertson; Melissa S. (Ambler, PA), Halczenko; Wasyl (Hatfield, PA), Hartman; George D. (Lansdale, PA)
Assignee: Merck & Co., Inc. (Rahway, NJ)
Application Number:07/860,747
Patent Claims: 1. A compound of the structural formula ##STR216## and the pharmaceutically acceptable salts thereof, wherein R.sup.4 is

aryl,

C.sub.1-10 alkyl, or

C.sub.4-10 aralkyl,

wherein aryl is phenyl, pyridyl, thienyl, tetrazole or oxazale;

R.sup.5 is ##STR217## wherein R.sup.8 is hydroxy or C.sub.1-10 alkyloxy, ##STR218## wherein R.sup.9 and R.sup.10 are selected from the group consisting of hydrogen, C.sub.1-10 alkyl and phenyl C.sub.1-4 alkyl;

Z is ##STR219## p is zero or one; and m is an integer from two to six.

2. A compound of claim 1, ##STR220## and the pharmaceutically acceptable salts thereof, wherein R.sup.4 is

aryl,

C.sub.1-10 alkyl, or

C.sub.4-10 aralkyl,

wherein aryl is phenyl, pyridyl, thiophenyl, tetrazole, or oxazole;

R.sup.5 is ##STR221## wherein R.sup.8 is hydroxy or C.sub.1-10 alkyloxy, ##STR222## wherein R.sup.9 and R.sup.10 are selected from the group consisting of hydrogen, C.sub.1-10 alkyl and phenyl C.sub.1-4 alkyl;

Z is O;

p is zero or one; and

m is an integer from two to six.

3. A compound as claimed in claim 2, of the structural formula ##STR223##

4. A compound as claimed in claim 2, of the structural formula ##STR224##

5. A compound as claimed in claim 2, of the structural formula ##STR225##

6. A compound of claim 1 selected from the group consisting of

2-S-(2-Styrylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]propionic acid hydrochloride;

2-S-(Phenylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]propionic acid hydrochloride;

2-S-(2-Phenethylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]propioni c acid hydrochloride;

2-S-(2-Thienylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]propionic acid hydrochloride;

{2-[4-[4-Piperidin-4-yl)butyloxyphenyl]1-n-butylsulfonylamino)}ethanephosph onic acid ethyl ester;

{2-[4-[4-Piperidin-4-yl)butyloxyphenyl]1n-butylsulfonylamino)}ethanephospho nic acid; and

Ethyl-2-S-Benzylsulfonylamino-3-[4-(piperidin-4-yl)butyloxyphenyl]propionat e;

2-S-(Butylsulfonylamino)-3-[4-(piperidin-4-yl)-1,1-dimethyl-butyloxyphenyl] propionic acid; and

3-S-(Butylsulfonylamino)-4-[4-piperidin-4-yl)butyloxyphenyl]butanoic acid.

7. A pharmaceutical composition, comprising a compound as claimed in claim 2, and a pharmaceutically acceptable carrier.

8. A pharmaceutical composition, comprising the compound as claimed in claim 3, and a pharmaceutically acceptable carrier.

9. A pharmaceutical composition, comprising the compound as claimed in claim 4, and a pharmaceutically acceptable carrier.

10. A pharmaceutical composition, comprising the compound as claimed in claim 5, and a pharmaceutically acceptable carrier.

11. A pharmaceutical composition, comprising a compound as claimed in claim 6, and a pharmaceutically acceptable carrier.

12. A method of blocking fibrinogen from acting at its platelet receptor site in a mannal, comprising the step of administering to said mammal a pharmacologically effective amount of a compound as claimed in claim 2.

13. The method as claimed in claim 12, wherein said compound is ##STR226##

14. The method as claimed in claim 12, wherein said compound is ##STR227##

15. The method as claimed in claim 12, wherein said compound is ##STR228##

16. The method as claimed in claim 12, wherein said compound is selected from

2-S-(2-Styrylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]propionic acid hydrochloride;

2-S-(Phenylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]-propionic acid hydrochloride;

2-S-(2-Phenethylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]propioni c acid hydrochloride;

2-S-(2-Thienylsulfonylamino)-3-[4-(piperidin-4-yl)butyloxyphenyl]propionic acid hydrochloride;

{2-[4-[4-Piperidin-4-yl)butyloxyphenyl]-1-n-butylsulfonylamino)}ethanephosp honic acid ethyl ester;

{2-[4-[4-Piperidin-4-yl)butyloxyphenyl]-1-n-butylsulfonylamino)}ethanephosp honic acid; and

Ethyl-2-S-Benzylsulfonylamino-3-[4-(piperidin-4-yl)butyloxyphenyl]propionat e;

2-S-(Butylsulfonylamino)-3-[4-(piperidin-4-yl)-1,1-dimethyl-butyloxphenyl]p ropionic acid; and

3-S-(Butylsulfonylamino)-4-[4-piperidin-4-yl)butyloxyphenyl]butanoic acid.

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

Serving leading biopharmaceutical companies globally:

Daiichi Sankyo
Julphar
Fuji
Argus Health
Express Scripts
Chinese Patent Office
Medtronic
Baxter
Queensland Health

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.

botpot