Claims
- 1. A compound of the formula or a pharmaceutically acceptable salt thereof, wherein A is hydrogen or R1 is hydrogen or C1-10 alkyl;Ar is X isOH, OCH3, OC(O)C(CH3)3, OC(O)CH3, OCH2CH3;R2 is CH(CH3)2, C(CH3)3, CH3, CH2CH3, CH2CH2CH3,CH(CH3)2CH2CH3, CH(CH3)CH2CH3, CH(CH2CH3)2, CH(CH3)CH2OCH3, CH(CH3)CH2CH2CH3, CH(CH3)CH2F, or CH(CH3)CH2SCH3; A1 is hydrogen, Cl, F, CH3, or CN; A2 is hydrogen, F, or OCH3; A3 and A4 are hydrogen; m is 0, 1, or 2; B is hydrogen; R6 is CH(CH3)2, CH2CH3, CH3,C(CH3)3, CH2Ph, Ph, C(CH3)2NC(O)OC(CH3)3, C(NH2)(CH3)2,
- 2. A compound of claim 1, or a pharmaceutically acceptable salt thereof, selected from the group consisting of
- 3. A pharmaceutical composition comprising a therapeutically effective amount of a compound of claim 1 and a pharmaceutically acceptable carrier.
- 4. A method for inhibiting the aggregation of blood platelets in a mammal, comprising treating the mammal with a composition of claim 2.
- 5. A method for inhibiting the aggregation of blood platelets in a mammal, by blocking thrombin from acting at its receptor site, comprising treating the mammal with a composition of claim 3.
- 6. A composition for inhibiting the aggregation of blood platelets in a mammal comprising a therapeutically effective amount of a compound of claim 1 in combination with two or more agents selected from a thrombolytic agent, an anticoagulant agent, and an antiplatelet agent and a pharmaceutically acceptable carrier.
- 7. A composition for inhibiting the aggregation of blood platelets in a mammal comprising a therapeutically effective amount of a compound of claim 1 in combination with a thrombolytic agent and a pharmaceutically acceptable carrier.
- 8. A composition for inhibiting the aggregation of blood platelets in a mammal comprising a therapeutically effective amount of a compound of claim 1 in combination with an anticoagulant agent and pharmaceutically acceptable carrier.
Parent Case Info
This application claims the benfit of provisional application 60,179,184 filed Jan. 31, 2000.
US Referenced Citations (9)
Number |
Name |
Date |
Kind |
5446131 |
Maraganore |
Aug 1995 |
A |
5457177 |
Veber et al. |
Oct 1995 |
A |
5516889 |
Hollenberg et al. |
May 1996 |
A |
5773459 |
Tang et al. |
Jun 1998 |
A |
5866681 |
Scarborough |
Feb 1999 |
A |
6017890 |
Hoekstra et al. |
Jan 2000 |
A |
6063847 |
Chackalamannil et al. |
May 2000 |
A |
6093742 |
Salituro et al. |
Jul 2000 |
A |
6156732 |
Hoekstra et al. |
Dec 2000 |
A |
Foreign Referenced Citations (1)
Number |
Date |
Country |
WO 9403479 |
Feb 1997 |
WO |
Non-Patent Literature Citations (3)
Entry |
Tiers, Chem. Abst. 110:66645 (1989).* |
Bernatowicz, Michael, S. et al., “Development of Potent Thrombin Receptor Antagonict Peptides”, J. Med. Chem., pp. 4879-4887; 39: 1996. |
Alexopoulos, K. et al., “A comparative SAR study of thrombin receptor derived non peptied mimetics: Importance of phenyl/guanidino proximity for activity”, Amino Acids, pp. 211-220; 15: 1998. |
Provisional Applications (1)
|
Number |
Date |
Country |
|
60/179184 |
Jan 2000 |
US |