Patent ID: 6030985
Filing Date: 2000-02-29
Classification: A61P,C07C,C07D

Abstract:
A method of treatment or prophylaxis of diseases or conditions in which inhibition of NOS is beneficial which comprises administering to a person in need thereof a therapeutically effective amount of a compound of formula (I) ##STR24## wherein D represents phenyl, pyridinyl or a 5-membered heterocyclic aromatic ring containing 1 to 4 heteroatoms selected from O, S or N, which three groups are optionally substituted by one or more groups selected from alkyl C1 to 6, alkoxy C1 to 6, halogen and perfluoroalkyl C1 to 6; or perfluoroalkyl C1 to 6;R.sup.1 represents hydrogen, alkyl C1 to 6 or halogenR.sup.2 represents --X(CH.sub.2).sub.n ZCONR.sup.3 R.sup.4, --X(CH.sub.2).sub.n NHCO(CH.sub.2).sub.s NR.sup.3 R.sup.4,--X(CH.sub.2).sub.p NR.sup.3 R.sup.4, --X(CH.sub.2).sub.n NHCOR.sup.5 or --(CH.sub.2).sub.q NHC(NH)R.sup.6 ;R.sup.3 and R.sup.4 independently represent hydrogen, alkyl C1 to 6, --(CH.sub.2).sub.r A, --(CH.sub.2).sub.m OA or --CH(CH.sub.3)(CH.sub.2).sub.1 A;or --NR.sup.3 R.sup.4 together represent 1-indanyl, piperonylamino-, piperdinyl, morpholinyl, pyrrolidinyl, 1,2,3,4-tetrahydroisoquinolinyl; or piperazinyl optionally 4-substituted by alkyl C1 to C6;R.sup.5 represents alkyl C1 to 6, perfluoroalkyl C1 to 6, --(CH.sub.2).sub.r A or --O(CH.sub.2).sub.w A;A represents phenyl, pyridinyl, pyrimidinyl, or a 5 membered heterocyclic aromatic ring containing 1 to 4 heteroatoms selected from O, S and N, which four groups are optionally substituted by one or more groups selected from alkyl C1 to 6, halogen, nitro, cyano and trifluoromethyl;R.sup.6 represents phenyl, pyridinyl or a 5 membered heterocyclic aromatic ring containing 1 to 4 heteroatoms selected from O, S and N, which three groups are optionally substituted by one or more groups selected from alkyl C1 to 6, alkoxy C1 to 6, halogen and perfluoroalkyl C1 to 6; or perfluoroalkyl C1 to 6;n and r independently represent an integer in the range 0 to 6 inclusive;p and w independently represent an integer in the range 1 to 5 inclusive;m represents an integer in the range 2 to 5 inclusive;q and t independently represent an integer in the range 0 to 5 inclusive;s represents an integer in the range 1 to 3 inclusive;X represents O or a bond;Z represents O, NR.sup.7 or a bond;R.sup.7 represents hydrogen or alkyl C1 to 6;provided that:(a) when D contains a heteratom, it is not connected to the remainder of the compound of formula I through the heteroatom;(b) when R.sup.2 represents --X(CH.sub.2).sub.n ZCONR.sup.3 R.sup.4, and neither X nor Z represent a bond, then n represents an integer in the range 2 to 6 inclusive;(c) when R.sup.2 represent --X(CH.sub.2).sub.n NHCO(CH.sub.2).sub.s NR.sup.3 R.sup.4, or --X(CH.sub.2).sub.n NHCOR.sup.5, and X represents O, then n represents an integer in the range 2 to 6 inclusive;(d) when R.sup.2 represents --X(CH.sub.2).sub.p N.sup.3 R.sup.4 and X represents O, then p represents an integer in the range 2 to 5 inclusive; or a pharmaceutically acceptable salt thereof.