Claims
- 1. 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.
- 2. The hexahydro-1,4-diazepine compound or its pharmaceutically acceptable salt as claimed in claim 1, wherein the ring is naphthalene or benzofuran.
- 3. The hexahydro-1,4-diazepine compound or, its pharmaceutically acceptable salt as claimed in claim 2, wherein R4 and R5 are each a hydrogen atom.
- 4. The hexahydro-1,4-diazepine compound or its pharmaceutically acceptable salt as claimed in claim 3, wherein the ring is naphthalene; A is a phenylene group (the phenylene group may be substituted with a substituent selected from a halogen atom, or an amino, cyano, nitro, —OH, —COOH, lower alkyl, —O-lower alkyl, or —COO-lower alkyl group), or a pyridylene group; and R3 is an amidino group.
- 5. The hexahydro-1,4-diazepine compound or its pharmaceutically acceptable salt as claimed in claim 4, wherein A is a phenylene or pyridylene group; X is a group of formula, —CO—, —CSNH—, —SO2—, or —SO2NH—; R1 is a hydrogen atom, or a lower alkyl, pyridyl, or —C(═NH)—CH3 group; and R2 is a hydrogen atom or a —COOH, —COO-lower alkyl, or tetrazolyl group.
- 6. A hexahydro-1,4-diazepine compound which is:N-[4-(4-Acetimidoylhexahydro-1H-1,4-diazepin-1-yl)-phenyl]-N-[(7-amidino-2-naphthyl)methyl]acetamide, ethyl [N-[4-(4-acetimidoylhexahydro-1H-1,4-diazepin-1-yl)phenyl]-N-[(7-amidino-2-naphthyl)methyl]-sulfamoyl]acetate, ethyl N-[N-[4-(4-acetimidoylhexahydro-1H-1,4-diazepin-1-yl)phenyl]-N-[(7-amidino-2-naphthyl)methyl]-sulfamoyl]glycinate, ethyl N-[4-(4-acetimidoylhexahydro-1H-1,4-diazepin-1-yl)phenyl]-N-[(7-amidino-2-naphthyl)methyl]malonamate, [N-[6-(4-acetimidoylhexahydro-1H-1,4-diazepin-1-yl)-3-pyridyl]-N-[(7-amidino-2-naphthyl)methyl]sulfamoyl]acetic acid, [N-[4-(4-acetimidoylhexahydro-1H-1,4-diazepin-1-yl)phenyl]-N-[(7-amidino-2-naphthyl)methyl]sulfamoyl]-acetic acid, N-[4-(4-acetimidoylhexahydro-1H-1,4-diazepin-1-yl)phenyl]-N-[(7-amidino-2-naphthyl)methyl]succinamic acid, ethyl N-[4-(4-acetimidoylhexahydro-1H-1,4-diazepin-1-yl)-3-pyridyl]-N-[(7-amidino-2-naphthyl)methyl]-malonamate, ethyl N-[4-(4-acetimidoylhexahydro-1H-1,4-diazepin-1-yl)-3-pyridyl]-N-[(7-amidino-2-naphthyl)methyl]-succinamate, N-[4-(4-acetimidoylhexahydro-1H-1,4-diazepin-1-yl)phenyl]-N-[(7-amidino-2-naphthyl)methyl]thioamido-acetic acid, N-[4-(4-acetimidoylhexahydro-1H-1,4-diazepin-1-yl)-3-pyridyl]-N-[(7-amidino-2-naphthyl)methyl]succinamic acid, or pharmaceutically acceptable salts thereof.
- 7. A pharmaceutical composition containing the hexahydro-1,4-diazepine compound or its pharmaceutically acceptable salt as claimed in claim 1 and a pharmaceutically acceptable carrier.
- 8. The pharmaceutical composition as claimed in claim 7, which is an activated blood coagulation factor X inhibitor.
Priority Claims (1)
Number |
Date |
Country |
Kind |
9-197587 |
Jul 1997 |
JP |
|
Parent Case Info
This application is a national stage entry under 35 U.S.C. § 371 of PCT/JP 98/03267 filed Jul. 22, 1998.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
102e Date |
371c Date |
PCT/JP98/03267 |
|
WO |
00 |
1/19/2000 |
1/19/2000 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO99/05124 |
2/4/1999 |
WO |
A |
US Referenced Citations (3)
Number |
Name |
Date |
Kind |
4634783 |
Fujii et al. |
Jan 1987 |
|
5478945 |
Sato et al. |
Dec 1995 |
|
5576343 |
Nagahara et al. |
Nov 1996 |
|
Foreign Referenced Citations (1)
Number |
Date |
Country |
10-17549 |
Jan 1988 |
JP |