US 6,333,320 B1Granted

Hexahydro-1,4-diazepine derivatives or salts thereof

AssigneeYamanouchi Pharmaceutical Co., Ltd.

InventorsHiroyuki Koshio, Fukushi Hirayama, Tsukasa Ishihara, Masashi Funatsu, Tomihisa Kawasaki, Yuzo Matsumoto

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Abstract

Hexahydro-1,4-diazepine derivatives represented by general formula (I); pharmaceutically acceptable salts thereof; and drugs containing the same as the active ingredient, such as activated blood coagulation factor X inhibitor, wherein A: phenylene, pyridylene, or the like; B: a 5- or 6-membered aryl or heteroaryl ring; X: —CO—, —CONH—, —CSNH—, —SO2—, —SO2NH—, or the like; Y: a bond or alkylene; R1: hydrogen, alkyl, —Y—(hetero) aryl, or the like; R2: hydrogen, alkoxy, —COOH, or the like; R3: amidino or a group capable of being converted into amidino; and R4, R5: each independently hydrogen or lower alkyl.

Claims8

Dependent claims

A hexahydro-1,4-diazepine compound represented by the following formula (I) or its pharmaceutically acceptable salt:

wherein the symbols have the following meanings:
A:
a phenylene or pyridylene group (which may be substituted),
B:
forming a 5- or 6-membered aryl or heteroaryl,
X:
a group of formula, —CO—, —CONH—, —CSNH—, —SO2—, —SO2NH—, or —SO2N(-lower alkyl)-,
Y:
a bond or a lower alkylene group,
R1:
a hydrogen atom, or a lower alkyl, —L-aryl, —L-heteroaryl, —L—COO-R6, —L—CON(—R6)—R7, —C(═NH)—NH2, or —C(═NH)-lower alkyl group,
R2:
a hydrogen atom, an —O-lower alkyl, —COOH, —COO-lower alkyl, —CONH2, —CONH-lower alkyl, or —CON—di-lower alkyl group, or an aryl or heteroaryl group (which may be substituted),
R3 an amidino group or a group capable of being converted into an amidino group in a living body,
R4, R5:
a hydrogen atom or a lower alkyl group, which may be the same or different,
R6, R7:
a hydrogen atom or a lower alkyl group, which may be the same or different, and
L:
a bond or a lower alkylene group.

17 more elements

Dependencies are inferred from the claim text.