Patent ID: 6812231
Filing Date: 2004-11-02
Classification: C07C,C07D,C07F

Abstract:
A composition comprising:a) one or more benzamidine compounds of the following formula (1-1) or a pharmaceutically acceptable salt thereof: wherein L represents an organic group of any of the following formulae (2) to (5): wherein W in formulae (2), (3) and (5) represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an aryl group having 4 to 10 carbon atoms or an aralkyl group having 5 to 12 carbon atoms, one of D and Dâ€² in formula (3) represents a bond to Y in general formula (1-1) and the other represents a hydrogen atom, X in formula (2) represents a hydrogen atom, carboxyl group, an alkoxycarbonyl group having 1 to 3 carbon atoms, an alkyl group having 1 to 3 carbon atoms, which optionally has a substituent(s), or a benzyl group which optionally has a substituent(s); wherein the substituent(s) is selected from the group consisting of a carboxyl group, alkoxycarbonyl groups having 2 to 8 carbon atoms, alkylsulfonyloxy groups having 1 to 6 carbon atoms, piperidyloxy group, iminoalkylpiperidyloxy groups having 6 to 10 carbon atoms, alkoxycarbonylpiperidyloxy groups having 7 to 14 carbon atoms, piperidylalkyl groups having 6 to 8 carbon atoms, iminoalkylpiperidylalkyl groups having 7 to 11 carbon atoms, alkoxycarbonylpiperidylalkyl groups having 8 to 15 carbon atoms, pyrrolidinyloxy group, iminoalkylpyrrolidinyloxy groups having 5 to 9 carbon atoms, alkoxycarbonylpyrrolidinyloxy groups having 7 to 13 carbon atoms, amidino group, mono- or dialkylamidino groups having 2 to 7 carbon atoms, hydroxyl group, halogeno groups, indolyl group and alkyl groups having 1 to 3 carbon atoms, X and W in formula (2) may be bonded together to form a ring and, in this case, â€”Wâ€”Xâ€” represents an ethylene group, trimethylene group or tetramethylene group, when L is an organic group of any of formulae (2) to (4), V1 represents a hydrogen atom, benzoyl, benzenesulfonyl, 2-naphthalenesulfonyl, piperazinecarbonyl, cinnamoyl, piperidinecarbonyl, 4-methylthiazole-5-carbonyl phenylacetyl, phenylthiocarbonyl or benzimidoyl group, which optionally has a substituent(s), or an alkanesulfonyl group having 1 to 6 carbon atoms, which optionally has a substituent(s), and when L is an organic group of formula (5), V1 represents an aryl group having 4 to 10 carbon atoms, which optionally has a substituent(s), when L is an organic group of any of formulae (2) to (5) and V1 has a substituent(s); wherein the substituent is selected from the group consisting of carboxyl group, alkoxycarbonyl groups having 2 to 7 carbon atoms, carbamoyl group, mono- or dialkylcarbamoyl groups having 2 to 7 carbon atoms, amidino group, mono- or dialkylamidino groups having 2 to 7 carbon atoms, acyl groups having 1 to 8 carbon atoms, halogeno groups, amino group, mono- or dialkylamino groups having 1 to 6 carbon atoms, arylamino groups having 4 to 6 carbon atoms, alkoxycarbonylamino groups having 2 to 7 carbon atoms, aminoalkyl groups having 1 to 3 carbon atoms, mono- or dialkylaminoalkyl groups having 2 to 7 carbon atoms, N-alkyl-N-alkoxycarbonylaminoalkyl groups having 4 to 10 carbon atoms, piperidyloxy group, iminoalkylpiperidyloxy groups having 6 to 10 carbon atoms, alkoxycarbonylpiperidyloxy groups having 8 to 14 carbon atoms, pyrrolidinyloxy group, iminoalkylpyrrolidinyloxy groups having 5 to 9 carbon atoms, alkoxycarbonylpyrrolidinyloxy groups having 7 to 13 carbon atoms, hydroxycarbonylalkyl groups having 2 to 7 carbon atoms, alkoxycarbonylalkyl groups having 3 to 8 carbon atoms, hydroxycarbonylalkenyl groups having 3 to 7 carbon atoms, alkoxycarbonylalkenyl groups having 4 to 8 carbon atoms, aryl groups having 4 to 10 carbon atoms, arylalkenyl groups having 6 to 12 carbon atoms, alkoxyl groups having 1 to 10 carbon atoms, nitro group, trifluoromethyl group, alkyl groups having 3 to 8 carbon atoms, arylsulfonyl groups having 4 to 10 carbon atoms, arylalkyl groups having 5 to 12 carbon atoms, piperazinecarbonyl group, iminoalkylpiperazinecarbonyl groups having 7 to 10 carbon atoms, piperazinesulfonyl group, iminoalkylpiperazinesulfonyl groups having 6 to 9 carbon atoms, piperidylalkyl groups having 6 to 9 carbon atoms, iminoalkylpiperidylalkyl groups having 8 to 12 carbon atoms, piperidylidenealkyl groups having 6 to 9 carbon atoms, iminoalkylpiperidylalkyl groups having 8 to 12 carbon atoms, guanidino group, dialkylguanidino groups having 3 to 5 carbon atoms, phosphono group, dialkoxyphosphoryl groups having 2 to 9 carbon atoms, monoalkoxyhydroxyphosphoryl groups having 1 to 4 carbon atoms, trialkylamidino groups having 4 to 7 carbon atoms, dialkoxybenzoyl groups having 9 to 13 carbon atoms, 1-alkylpyridinio groups having 6 to 9 carbon atoms and groups of the following formulae: wherein A in formulae (6) and (7) represents a halogeno group, and B in formulae (8) and (9) represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, a halogeno group or amino group, Y represents any of following formulae (10) to (16): wherein n in formulae (10) and (11) represents an integer of 0 to 2, R1 in formula (16) represents a hydrogen atom, a hydroxycarbonylalkyl group having 2 to 7 carbon atoms, an alkoxycarbonylalkyl group having 3 to 8 carbon atoms or a hydroxycarbonylalkenyl group having 3 to 7 carbon atoms, Z1 represents a group of any of following formulae (17) to (24): wherein m in formulae (17), (19), (21) and (23) represents an integer of 0 to 3, R2 in formulae (17), (18) and (24) represents a hydroxyl group, an alkoxyl group having 1 to 5 carbon atoms, trifluoromethyl group, amino group or a mono- or dialkylamino group having 1 to 6 carbon atoms, R3 in formula (19) represents a hydrogen atom, an alkyl group having 1 to 6 carbon atoms or acetyl group, R4 in formulae (20) to (23) represents hydrogen atom or an alkyl group having 1 to 6 carbon atoms, R5 in formulae (22) and (23) represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, and R6 in formula (24) represents a halogeno group; and b) a pharmaceutically acceptable carrier.