Patent ID: 6620811
Filing Date: 2003-09-16
Classification: A61P,C07D

Abstract:
A compound of the formula whereinR1 is phenyl, piperidin-1-yl or morpholinyl; A is â€”Oâ€” and R is â€”(CH2)nâ€”N(Râ€³)â€”C(O)-lower alkyl, â€”(CH2)nâ€”O-lower alkyl, â€”(CH2)nâ€”Oâ€”(CH2)nâ€”O-lower alkyl, lower alkyl, â€”(CH2)n-morpholinyl, â€”(CH2)n-phenyl, â€”(CH2)nâ€”N(Râ€³)2, â€”(CH2)n-pyridinyl, â€”(CH2)nâ€”CF3, â€”(CH2)n-2-oxo-pyrrolidinyl or C4-6-cycloalkyl; each Râ€³ is independently selected from hydrogen or lower alkyl; and n is 1 or 2; or A is â€”N(Râ€²)â€” and R is lower alkyl, C4-6-cycloalkyl, â€”(CH2)nâ€”O-lower alkyl, â€”(CH2)n-pyridinyl, â€”(CH2)n-piperidinyl, â€”(CH2)n-phenyl, â€”(CH2)nâ€”N(Râ€³)â€”C(O)-lower alkyl, â€”(CH2)n-morpholinyl, or â€”(CH2)nâ€”N(Râ€³)2; Râ€² and Râ€³ are independently selected from hydrogen or lower alkyl; and n is 1 or 2; or A is â€”CH2â€” and R is â€”N(Râ€³)â€”(CH2)mâ€”O-lower alkyl, â€”N(Râ€³)2, â€”S-lower alkyl or is acetidinyl, pyrrolidinyl or piperidinyl, which are optionally substituted by hydroxy or lower alkoxy or is morpholinyl, â€”N(Râ€³)â€”(CH2)mâ€”C4-6-cycloalkyl, â€”N(Râ€³)â€”(CH2)mâ€”C(O)O-lower alkyl, â€”N(Râ€³)â€”(CH2)mâ€”C(O)OH, -2-oxo-pyrrolidinyl, â€”N(Râ€³)â€”C(O)O-lower alkyl, â€”O(CH2)mâ€”O-lower alkyl or alkoxy; each Râ€³ is independently selected from hydrogen or lower alkyl; and m is 1, 2 or 3; or A is â€”Sâ€” and R is lower alkyl; or Aâ€”R are together p2 -piperazinyl, substituted by lower alkyl, â€”C(O)-lower alkyl or an oxo group, or is piperidinyl, substituted by lower alkoxy or hydroxy, or is morpholinyl, substituted by lower alkyl, or is â€”C4-6-cycloalkyl, -azetidin-1-yl, optionally substituted by hydroxy or lower alkoxy, thiomorpholine-1,1-dioxo, -tetrahydopyran or 2-oxa-5-aza-bicyclo[2.2.1]hept-5-yl; and pharmaceutically acceptable acid addition salts thereof.