Claims
- 1. A compound of the formula: in whichR1 is hydrogen, optionally substituted lower alkylcarbamoyl(lower)alkylidene, lower alkylidene, lower alkyl, optionally substituted ar(lower)alkyl, cyclo(lower)alkyl(lower)alkyl, protected carboxy(lower)alkyl, carboxy(lower)alkyl, hydroxy(lower)alkyl, optionally substituted lower alkylcarbamoyl(lower)alkyl, lower alkylthio(lower)alkyl, carboxy(lower)alkanoyl, protected carboxy(lower)alkanoyl, aroyl, lower alkanoyl, or optionally substituted arylcarbamoyl(lower)alkyl, R2 is hydrogen, carboxy, protected carboxy, formyl or N-(lower)alkyl-N-(lower)alkoxycarbamoyl, R3 is hydrogen or amidino-protective group, A is lower alkylene or carbonyl, X is Y is lower alkylene, Z is —S— or —O—, and the line: is a single bond or a double bond, or pharmaceutically acceptable salts thereof.
- 2. The compound of claim 1, whereinR1 is hydrogen; lower alkylcarbamoyl(lower)alkylidene optionally substituted by halogen; lower alkylidene; lower alkyl; ar(lower)alkyl optionally substituted by the group consisting of lower alkyl, lower alkoxy and lower alkylenedioxy; cyclo(lower)alkyl(lower)alkyl; lower alkoxycarbonyl(lower)alkyl; carboxy(lower)alkyl; hydroxy(lower)alkyl; lower alkylcarbamoyl(lower)alkyl optionally substituted by halogen; lower alkylthio(lower)alkyl; carboxy(lower)alkanoyl; lower alkoxycarbonyl(lower)alkanoyl; aroyl; lower alkanoyl; or arylcarbamoyl(lower)alkyl optionally substituted by the group consisting of lower alkyl, lower alkoxy and lower alkylenedioxy; R2 is hydrogen, carboxy, lower alkoxycarbonyl, formyl, or N-(lower)alkyl-N-(lower)alkoxycarbamoyl, and R3 is hydrogen or lower alkoxycarbonyl.
- 3. The compound of claim 1, whereinX is and Y is lower alkylene.
- 4. A process for the preparation of a compound of the formula: in which R1, R2, R3, A, X, Y, Z and the line: are each as defined in claim 1, or salts thereof, which comprises(a) reducing a compound of the formula: or a salt thereof to give a compound of the formula: or a salt thereof; or(b) reacting a compound of the formula: or a salt thereof with ammonia or a salt thereof to give a compound of the formula (I-a), or a salt thereof; or(c) subjecting a compound of the formula: or a salt thereof to a removal reaction of the carboxy-protective group in Rc1 to give a compound of the formula: or a salt thereof; or(d) subjecting a compound of the formula: or a salt thereof to a removal of the carboxy-protective group in Ra2 to give a compound of the formula: or a salt thereof(e) introducing an amidino-protective group into a compound of the formula: or a salt thereof, to give a compound of the formula: or a salt thereof; or(f) reacting a compound of the formula: or its reactive derivative at the carboxy group, or a salt thereof, with N-(lower)alkyl-N-(lower)alkoxyamine or a salt thereof, to give a compound of the formula: or a salt thereof; or(g) subjecting a compound of the formula: or a salt thereof; orto a removal reaction of the amidino-protective group of Ra3, to give a compound of the formula (I-a) or a salt thereof; or(h) reducing a compound of the formula: or a salt thereof, to give a compound of the formula or a salt thereof;in whichR1, R2, R3, A, X, Y, Z and the line: are each as defined above, Ra1 is optionally substituted lower alkylcarbamoyl(lower)alkylidene or lower alkylidene, Rb1 is optionally substituted lower alkylcarbamoyl(lower)alkyl or lower alkyl, Rc1 is protected carboxy(lower)alkyl, Rd1 is carboxy(lower)alkyl, Ra2 is protected carboxy, Rb2 is N-(lower)alkyl-N-(lower)alkoxycarbamoyl, Ra3 is amidino-protective group, R4 is ester residue, Xa is
- 5. A pharmaceutical composition which comprises, as an active ingredient, a compound of claim 1 or a pharmaceutically acceptable salt thereof in admixture with pharmaceutically acceptable carriers or excipients.
- 6. A method for treatment of diseases initiated by urokinase which comprises administering an effective amount of a compound of claim 1 or a pharmaceutically acceptable salt thereof to a human being or an animal.
Priority Claims (1)
Number |
Date |
Country |
Kind |
PO2278 |
Sep 1996 |
AU |
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Parent Case Info
This application is a divisional of U.S. Ser. No. 09/147,812 file Mar. 12, 1999 now U.S. Pat. No. 6,093,710, which is a national stage application filed under 35 U.S.C. 371 of PCT/JP97/03215 filed Sep. 12, 1997.
US Referenced Citations (6)
Number |
Name |
Date |
Kind |
4465851 |
Muramatsu et al. |
Aug 1984 |
|
5089634 |
Powers et al. |
Feb 1992 |
|
5093332 |
Shepard et al. |
Mar 1992 |
|
5240923 |
Dean et al. |
Aug 1993 |
|
5723458 |
Brieaddy et al. |
Mar 1998 |
|
5889002 |
Nielsen et al. |
Mar 1999 |
|
Foreign Referenced Citations (3)
Number |
Date |
Country |
568289 |
Nov 1993 |
EP |
618206 |
Oct 1994 |
EP |
2279951 |
Jan 1995 |
GB |
Continuations (1)
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Number |
Date |
Country |
Parent |
09/147812 |
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US |
Child |
09/584136 |
|
US |