Claims
- 1. Compound formula (I) or (II): whereinG is O or L is selected from the group consisting of the group L1 consisting of and each member of said group can have 0, 1, 2 or 3 pendant groups selected from the group J1; wherein each J1 is individually selected from the group consisting of H, halogen CF3 alkyl groups, straight or branched chain, of 1-5 carbon atoms, alkoxy groups having 1-5 carbon atoms, aryl, and heterocyclic; Q1 is, C(═NH)NH2; X1, X2 and X3 are each C; Y is C(J2); Z1 is O or S; each J2 is individually selected from the group consisting of H, halogen, CF3, and lower alkyl, straight or branched chain, of 1-5 carbon atoms; each J3 is individually selected from the group consisting of H, and lower alkyl, straight or branched, of 1-5 carbon atoms; and pharmaceutically acceptable salts thereof.
- 2. The compound of claim 1 wherein Q1 is C(═NH)NH2.
- 3. The compound of claim 1 being selected from the group consisting of:2-amidino-5 or 6-benzofuranyl 2-furanyl carboxylate, 2-amidino-5 or 6-benzofuranyl 2-thiophene carboxylate, 2-amidino-5-benzofuranyl 3-furanyl carboxylate, 2-amidino-6-benzothiazolyl 2- or 3-furanyl carboxylate, 2-amidino-6-benzothiazolyl 2-thiophene carboxylate, 2-amidino-6-benzothiazolyl benzoate, 2-amidino-5-benzofuranyl 3-thiophene carboxylate, 2-amidino-benzo[b]thien-6-yl benzoate, 2-amidino-benzo[b]thien-6-yl 2-furancarboxylate, 2-amidino-benzo[b]thien-6-yl 3-thiophenecarboxylate, 2-amidino-benzo[b]thien-6-yl 3-furancarboxylate, 2-amidino-benzo[b]thien-6-yl 3-thiophenecarboxylate, 2-amidino-6-benzothiazolyl 3-thiophenecarboxylate, 2-amidino-6-benzothiazolyl 2-(5-chlorothiophene carboxylate, 3-amidino-7-(3-furancarboxy)-2H-1-benzopyran, 3-amidino-7-(2-thiophenecarboxy)-2H-1-benzopyran, 3-amidino-7-(3-thiophenecarboxy)-2H-1-benzopyran, trans-2-amidino-6-benzo[b]thienyl 2-pentenoate, or pharmaceutically acceptable salts thereof.
- 4. The compound of claim 1 being 2-amidino-5- or 6-benzofuranyl 2-furanyl carboxylate or a pharmaceutically acceptable acid condition salt thereof.
- 5. The compound of claim 1 being 2-amidino-5 or 6-benzofuranyl 2-thiophene-carboxylate or a pharmaceutically acceptable salt thereof.
- 6. The compound of claim 1 being 2-amidino-5-benzofuranyl 3-furanylcarboxylate or a pharmaceutically acceptable salt thereof.
- 7. The compound of claim 1 being 2-amidino-6-benzothiazolyl 2- or 3-furancarboxylate or a pharmaceutically acceptable salt thereof.
- 8. The compound of claim 1 being 2-amidino-6-benzothiazolyl 2-thiophenecarboxylate or a pharmaceutically acceptable salt thereof.
- 9. The compound of claim 1 being 2-amidino-6-benzothiazolyl benzoate or a pharmaceutically acceptable salt thereof.
- 10. The compound of claim 1 being 2-Amidino-5-benzofuranyl 3-thiophenecarboxylate methanesulfonate.
- 11. The compound claim 1 being 2-Amidino benzo[b]thien-6-yl benzoate methanesulfonate.
- 12. The compound of claim 1 being 2-Amidino benzo[b]thien-6-yl 2-furancarboxylate methanesulfonate.
- 13. The compound of claim 1 being 2-Amidino benzo[b]thien-6-yl 2-thiophenecarboxylate methanesulfonate.
- 14. The compound of claim 1 being 2-Amidino benzo[b]thien-6-yl 3-furancarboxylate methanesulfonate.
- 15. The compound of claim 1 being 2-Amidino benzo[b]thien-6-yl 3-thiophenecarboxylate methanesulfonate.
- 16. The compound of claim 1 being 2-Amidino-6-benzothiazolyl 3-thiophenecarboxylate methanesulfonate.
- 17. The compound of claim 1 being 2-Amidino-6-benzothiazolyl 2-(5-chlorothiophene)carboxylate methanesulfonate.
- 18. A pharmaceutically composition for use in the complement, coagulation and kallikrein pathways comprising a compound according to claim 1 or pharmaceutically acceptable addition salt thereof that inhibits a broad spectrum of serine proteases; and a pharmaceutical carrier.
- 19. A pharmaceutically composition for the induction of “blood anesthesia” comprising a compound according to claim 1 or pharmaceutically acceptable addition salt thereof that acts at multiple sites of the coargulation and complement components; and a pharmaceutical carriers.
DESCRIPTION
This Appn. is a 371 of PCT/US98/11255 filed Jun. 3, 1998 which claims the benefit of Prov. Applns. 60/079,669, filed Mar. 27, 1998 and 60/048,122, filed Jun. 3, 1997.
PCT Information
Filing Document |
Filing Date |
Country |
Kind |
PCT/US98/11255 |
|
WO |
00 |
Publishing Document |
Publishing Date |
Country |
Kind |
WO98/55471 |
12/10/1998 |
WO |
A |
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Provisional Applications (2)
|
Number |
Date |
Country |
|
60/079669 |
Mar 1998 |
US |
|
60/048122 |
Jun 1997 |
US |