Novel fibrinogen receptor antagonists

Claim 1

A compound of the formula and the pharmaceutically acceptable salts thereof, wherein R¹ is a four to eight member heterocyclic ring containing 1, 2, 3 or 4 hetero atoms wherein said heteroatoms are N, O or S and wherein said heterocyclic ring is optionally substituted at any atom by H, R⁶ or R⁷; NR⁶R⁷ wherein R⁶ and R⁷ are independently hydrogen, C₁₋₁₀ alkoxycarbonyl or unsubstituted or substituted C₁₋₁₀ alkyl and cycloalkyl wherein said substituents are C₁₋₁₀ alkoxy, C₁₋₁₀ alkoxyalkyl, C₁₋₁₀ alkoxyalkyloxy, C₁₋₁₀ alkoxycarbonyl, C₁₋₁₀ alkylcarbonyl, C₀₋₆ alkylaminocarbonyl, C₁₋₁₀ aralkylcarbonyl, C₁₋₁₀ alkylthiocarbonyl, C₄₋₁₀ aralkylthiocarbonyl, thiocarbonyl, C₁₋₁₀ alkoxythiocarbonyl, aryl, 5 to 6 membered saturated heterocyclic rings of 1, 2, 3 or 4 hetero atoms wherein said hetero atoms are taken from the group consisting of N, O and S, C₁₋₄ alkanoylamino, C₁₋₆ alkoxycarbonyl-C₀₋₆ alkylamino, C₁₋₁₀ alkylsulfonylamino, C₄₋₁₀ aralkylsulfonylamino, C₄₋₁₀ aralkyl, C₁₋₁₀ alkaryl, C₁₋₁₀ alkylthio, C₄₋₁₀ aralkylthio, C₁₋₁₀ alkylsulfinyl, C₄₋₁₀ aralkylsulfinyl, C₁₋₁₀ alkylsulfonyl, C₄₋₁₀ aralkylsulfonyl, aminosulfonyl, C₁₋₁₀ alkylaminosulfonyl, C₄₋₁₀ aralkylsulfonylamino, oxo, thio, unsubstituted or mono- or di-substituted 1-ethenyl, 2-ethenyl or 3-propenyl wherein said substituents are selected from the group consisting of hydrogen, C₁₋₁₀ alkyl and C₇₋₁₀ aralkyl, carboxy, hydroxy, amino, C₁₋₆ alkylamino, C₁₋₆ dialkylamino, halogen, where halogen is defined as Cl, F, Br, or I, nitro, or cyano, and further wherein said N can additionally be substituted to form a quaternary ammonium ion wherein said substituent is as previously defined for R⁶ and R⁷; R² and R³ are independently hydrogen, aryl or unsubstituted or substituted C₀₋₁₀ alkyl or cycloalkyl wherein said substituent is C₁₋₁₀ alkoxyalkyl, aryl, a 4 to 8 membered heterocyclic ring containing 1, 2, 3 or 4 hetero atoms, wherein said hetero atoms are taken from the group consisting of N, O and S, C₄₋₁₀ aralkyl, C₁₋₁₀ alkaryl, carboxy, C₁₋₁₀ alkylcarbonyl, C₁₋₁₀ alkylthiocarbonyl, C₄₋₁₀ aralkylcarbonyl, C₄₋₁₀ aralkylthiocarbonyl, C₁₋₆ alkoxycarbonyl, C₄₋₁₀ aralkoxycarbonyl, C₁₋₆ alkoxy, C₄₋₁₀ aralkoxy, C₁₋₆ alkylamino, C₁₋₁₂ dialkylamino, C₁₋₆ alkanoylamino, C₄₋₁₂ aralkanoylamino, C₄₋₁₀ aralkylamino; R⁴ is hydrogen, aryl, C₁₋₁₀ alkyl or cycloalkyl C₄₋₁₀ aralkyl, arylcarbonyl, aminocarbonyl, C₁₋₁₀ alkylcarbonyl, C₁₋₆alkylaminocarbonyl, C₁₋₁₀ alkylthiocarbonyl, C₁₋₆dialkylaminocarbonyl, C₁₋₁₀ alkoxythiocarbonyl, arylC₁₋₆alkylaminocarbonyl, C₁₋₁₀ alkoxycarbonyl, C₄₋₁₀ aralkylcarbonyl, C₄₋₁₀ aralkoxycarbonyl, C₁₋₁₀ carboxylalkyl and further wherein any of the substitutents for R⁴ may be substituted by one or more substituents selected from the group as defined for R⁶, or an L- or D-amino acid joined by an amide linkage; R⁵ is a four to eight membered saturated or unsaturated heterocyclic ring containing 1, 2, 3 or 4 hetero atoms wherein said hetero atoms are N, O, or S or, wherein R⁸ is hydroxy, C₁₋₁₀ alkyloxy, C₁₋₁₀ alkaryloxy, C₄₋₁₀ aralkyloxy, C₄₋₁₀ aralkylcarbonyloxy, C₁₋₁₀ alkoxyalkyloxy, C₁₋₁₀ alkoxyalkylcarbonyloxy, C₁₋₁₀ alkoxycarbonyloxyalkyl, C₁₋₁₀ alkylcarbonyloxyalkyloxy, an L- or D-amino acid joined by an amide linkage, and wherein the carboxylic acid moiety of said amino acid is as the free acid or is esterified by C₁₋₆alkyl. wherein R⁹ and R¹⁰ are selected from the group consisting of hydrogen, C₁₋₁₀ alkyl and C₄₋₁₀ aralkyl; X and Y are optional substituents that, when present, are NR⁶, O, S, SO, SO₂, oxo, aryl, thiono, unsubstituted or substituted C₁₋₁₅ alkyl or cycloalkyl wherein said substituents are independently R⁶ and R⁷, -NR⁶-SO₂-,   -SO₂-NR⁶-, or a 4- to 8- membered heterocyclic ring containing 1, 2, 3, or 4 heteroatoms wherein said atoms are N, 0, or S and wherein said ring is independently substituted at any atom with R⁶; Z is an optional substituent that, when present, is independently chosen as defined by X and Y; m is an integer of from zero to ten; n is an integer of from zero to ten; and p is an integer of from zero to three.