Claims
- 1. A compound represented by the general formula (I): wherein M is CH═CH or C≡C; A is selected from any of piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, piperazin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, NHR2 or wherein R9 is selected from any of H, alkyl, CH(NH), CMe(NH) or acyl;R10 is H or C(O)N(R1)YZ, wherein R1 is selected from H or cycloalkyl; R2 is selected from any of H, alkyl or acyl; R5 is H or C(O)NHQ(CHW)rCO2R8; wherein Q is selected from CH-heteroaryl, or CH-substituted-heteroaryl, wherein the heteroaryl is selected from pyridyl, thienyl, furanyl or quinolinyl; W is selected from H or N(R6)T—R7; wherein R6 is selected from any of H, alkyl or acyl; T is selected from C(O), C(N—CN) or SO2; R7 is selected from any of alkyl, aryl, aralkyl, alkoxy, or aminoalkyl; and R8 is H or CH2C(O)NR11R12, wherein R11 and R12 are selected from H, alkyl, or cycloalkyl; m is the integer 1, 2, or 3; X is selected from any of C(O), C(O)O, C(O)NH, CH2, or SO2; n is the integer 1, 2, or 3; r is 0 or 1; Y is selected from any of (CH2)p, CH(R3)(CH2)q, (CH2)qCH(R3), (CH(CO2R4)CH2)q, (CH2)qCHOH or piperidine-3-carboxylic acid; with the proviso that when Y is (CH2)p and p is 2, X is other than C(O) or when X is C(O) then either R1 is other than H or R2 is other than H, and with the proviso that when Y is (CH(CO2R4)CH2)q X is other than C(O) or CH2; p is 2or3; q is 1, 2, or 3; R3 is alkyl, C2-C8 alkenyl, C2-C8 alkynyl, aryl, aralkyl or heteroaryl; R4 is H or alkyl or cycloalkyl; Z is CO2CH2C(O)NR11R12; provided that at least one of R5 and R10 is hydrogen and R5 and R10 are not hydrogen at the same time; provided that when R5 is C(O)NHQ(CHW)rCO2R8 and Q is CH-heteroaryl or CH-substituted-heteroaryl, and R8 is H, then M is CH═CH; or the enantiomer or the pharmaceutically acceptable salt thereof.
- 2. The compound of claim 1, whereinR5 is C(O)NHQ(CHW)rCO2R8; wherein Q is selected from CH-heteroaryl, or CH-substituted-heteroaryl, wherein the heteroaryl is pyridyl; or the enantiomer or the pharmaceutically acceptable salt thereof.
- 3. A composition for treating platelet-mediated thrombic disorders comprising the compound of claim 1 in an effective amount for treating such disorders in combination with a pharmaceutically acceptable carrier.
- 4. A method of making the composition of claim 3 comprising mixing an effective amount of the compound with a pharmaceutically acceptable carrier.
- 5. A method of treating platelet-mediated thrombic disorders comprising administering to a patient afflicted with such disorder an effective amount of the compound of claim 1 to treat such disorder.
- 6. The method of claim 5, wherein the amount is 0.1-300 mg/kg/day.
- 7. A method of treating platelet-mediated thrombic disorders comprising administering to a patient afflicted with such disorder an effective amount of the composition of claim 3 to treat such disorder.
- 8. A method of inhibiting platelet aggregation in a patient in need thereof comprising administering to the patient an effective amount of the compound of claim 1.
- 9. The method of claim 8, wherein the amount is 0.1-300 mg/kg/day.
CROSS-REFERENCE TO RELATED APPLICATION
This application is a continuation of U.S. Ser. No. 09/175,166, filed Oct. 20, 1998, allowed U.S. Pat. No. 6,066,651, which claims priority from U.S. Ser. No. 60/063,366, filed Oct. 29, 1997, the contents of both of which are hereby incorporated by reference.
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Provisional Applications (1)
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Number |
Date |
Country |
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60/063366 |
Oct 1997 |
US |
Continuations (1)
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Number |
Date |
Country |
Parent |
09/175166 |
Oct 1998 |
US |
Child |
09/430472 |
|
US |