摘要:
Compounds of the formula (I), in which M is a central building block selected from the group below in which A1, A2, K1 and K2 are as defined in the description, are novel effective tryptase inhibitors.
摘要:
The invention relates to compounds of formula (I), wherein M, A1, A2, A3, A4, A5, A6, B1, B2, B3, B4, B5, B6, K1 and K2 have the meanings given in the description. Said compounds are novel, effective tryptase inhibitors.
摘要:
The invention relates to bifunctional inhibitors of human tryptase of formula (I), to human tryptase in crystalline form, to a method for producing human tryptase in crystalline form, to pharmaceutical compositions comprising a bifunctional inhibitor of human tryptase, and to a method for developing and identifying tryptase inhibitors. The tryptase inhibitors are characterized in that both head groups K1 and K2 are the same or different and each comprises a group Q which can interact with a carboxylate group. The linker L can assume a conformation such that the groups Q of both head groups are situated at a distance ranging from 20 to 45 Å, such that the dimension of the head groups and of the linker permit the inhibitor to penetrate into a cavity with the dimensions 52 Å X 32 Å X 40 Å, and such that L represents formula (II) wherein A1 and A2 are the same or different, and represent -C(O)-, NH-, -O- (oxygen), -S- (sulfur), -S(O)2-, -S(O)2-NH-, -NH-S(O)2-, -C(O)-NH-, -NH-C(O)-, -O-C(O)-, -C(O)-O- or a bond. A3 and A4 are the same or different and represent -C(O)-, -C(S)-, -O-, -S-, -NH-, -O-C(O)-, -C(O)-O-, -C(O)-NH-, -NH-C(O)- or a bond, or are selected from the group A5, A6, M, B1-B6 as stated in the description.
摘要:
The invention concerns the compounds 8,9-Diethoxy-2-methyl-6- [4(p-toluenesulfonamido)phenyl] -1,2,3,4,4a,10b-hexahydrobenzo[c] [1,6]naphthyridine and 9-Ethoxy-8-methoxy-2- methyl-6-[4-(p-toluenesulfonamido) phenyl]-1,2,3,4,4a,10b-hexahydrobenzo [c][1,6]naphthyridine and their therapeutic application.
摘要:
Compounds of formula (I) in which R4 is a phenyl radical substituted by R5, where R5 is a tetrazole-5-yl radical optionally substituted by a radical R6, are novel efficacious PDE3/4 inhibitors.
摘要:
Compounds of formula (I), in which M, B1, B2, B3, B4, B5, B6, A1, A2, A3, A4, A5, A6, K1 and K2 have the meanings as indicated in the description are novel effective tryptase inhibitors.
摘要:
The invention relates to compounds of formula (I) wherein R1, R2, R3, R4 and Y have the meanings given in the description. Said compounds are novel active bronchial therapeutic agents.
摘要:
Compounds having the formula (I), in which R1, R2, R3, R4 and n have the meanings given in the description, are new effective bronchotherapeutic agents (phosphodiesterase IV inhibitors).