Substituted amide derivatives of piperizinylcamphorsulfonyl...

C - Chemistry – Metallurgy – 07 – D

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C07D 295/26 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) A61K 31/55 (2006.01) C07B 59/00 (2006.01) C07D 207/16 (2006.01) C07D 207/277 (2006.01) C07D 211/58 (2006.01) C07D 211/60 (2006.01) C07D 211/62 (2006.01) C07D 213/38 (2006.01) C07D 213/74 (2006.01) C07D 233/54 (2006.01) C07D 241/08 (2006.01) C07D 303/34 (2006.01) C07D 309/14 (2006.01) C07D 335/02 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07D 45

Patent

CA 2077922

18215Y TITLE OF THE INVENTION SUBSTITUTED AMIDE DERIVATIVES OF PIPERAZINYLCAMPHORSULFONYL OXYTOCIN ANTAGONISTS ABSTRACT OF THE INVENTION Compounds of the formula: Image Compounds according to the structural formula, wherein R1 is (1) hydrogen, (2) alkoxycarbonyl or (3) unsubstituted or substituted alkyl wherein said substituent is hydroxyl, alkoxyl, carboxyl, carboxyalkyl., alkylsulfonyl or alkoxycarbonyl; and R2 is (1) hydrogen, -ii- 18215IA (2) alkoxyl, (3) aralkoxyl, (4) alkoxycarbonyl, (5) alkoxycarbonylamino, (6) unsubstituted or substituted cycloalkyl, wherein said substituent is carboxyl, (7) unsubstituted or substituted phenyl wherein said substituent is one or more of carboxyl, carboxyalkyl or S03H, (8) unsubstituted or substituted amino, wherein said substituent is unsubstituted or substituted alkyl where said substituent is one or more of carboxyl, alkylsulfonyl or unsubstituted 5-membered heterocyclic rings having 1 or 2 heteroatoms, where said heteroatom is N, (9) unsubstituted or substituted rings of the formulae Image where said substituents are one or more of alkyl, carboxyl, carboxyalkyl, carboxyaralkyl, aralkylcarbonyl, aralkoxycarbonyl, alkoxycarbonyl, alkoxycarbonylalkyl, alkoxycarbonylaminoalkylcarbonyl, oxo or unsubstituted or substituted amino wherein said substituent is one or more of alkyl, carboxylalkyl, alkoxycarbonyl or alkoxycarbonylalkyl or (10) unsubstituted or substituted alkyl, wherein said substituent is one or more of hydroxyl, carboxyl, carboxyalkylphenyl, alkylsulfonyl, aminocarbonyl, alkylaminocarbonyl, aralkyl, aralkoxycarbonyl, halogen, alkoxycarbonyl, alkoxycarbonylalkyl, Het or unsubstituted or substituted amino, wherein said substituent is one or more of alkyl, alkylcarbonyl, alkylsulfonyl, carboxyalkyl, Cyc, alkoxycarbonyl, alkoxycarbonylalkyl, aralkoxycarbonyl, aminocarbonylalkyl, alkylaminocarbonyl, phenalkyl or unsubstituted or substituted alkylcarbonyl, where said substituent is a 5- membered heterocyclic ring having 1 or 2 heteroatoms and where said -iii- 18215IA hetero atom is N, where Het is defined as for the above heterocyclic rings and where Cyc is defined as substituted or unsubstituted cycloalkyl wherein said substituent is selected from the group consisting of alkoxycarbonyl, carboxyl, hydroxyl, oxo or spiro-dioxolinyl . Such compounds are oxytocin antagonists useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery.

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