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Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade

a technology of coagulation cascade and polycyclic compounds, which is applied in the direction of drug compositions, biocides, extracellular fluid disorders, etc., can solve the problems of ischemic necrosis of tissue supplied by the artery, myocardial infarction or heart attack, and reduce blood flow, so as to prevent and treat thrombotic conditions in mammals

Inactive Publication Date: 2005-10-27
PHARMACIA CORP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0011] Among the several aspects of the present invention, therefore, is the provision of compounds useful for selective inhibition of certain enzymes that act upon the coagulation cascade thereby preventing and treating thrombotic conditions in mammals.

Problems solved by technology

Unregulated activation of the of the hemostatic system, however, may cause thrombosis, which can reduce blood flow to critical organs like the brain and myocardium.
Arterial thrombosis may result in ischemic necrosis of the tissue supplied by the artery.
When the thrombosis occurs in a coronary artery, a myocardial infarction or heart attack can result.
A thrombosis occurring in a vein may cause tissues drained by the vein to become edematous and inflamed.
Thrombosis of a deep vein may be complicated by a pulmonary embolism.
The ionic nature of such protonated species hinders their permeability across lipophilic membranes, which can reduce bioavailability when the pharmaceutical agent is administered orally.

Method used

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  • Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
  • Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade
  • Substituted 5-membered polycyclic compounds useful for selective inhibition of the coagulation cascade

Examples

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Embodiment Construction

[0049] One aspect of the invention embraces compounds that correspond to formula (I)

wherein:

[0050] X comprises a 5-membered heterocyclic or carbocyclic ring, the ring atoms being X1, X2, X3, X4, and X5, wherein X1, X3, and X4, are independently carbon or nitrogen and X2 and X5 are independently carbon, nitrogen, oxygen or sulfur;

[0051] L1, L3 and L4 are linkages through which Z1, Z3, and Z4, respectively, are covalently bonded to different ring atoms of the 5-membered heterocyclic or carbocyclic ring of X, wherein Z1 is covalently bonded to X1, Z3 is covalently bonded to X3, and Z4 is covalently bonded to X4, each of L1, L3 and L4 independently being a covalent bond or comprising one or more atoms through which Z1, Z3, and Z4 are covalently bonded to X1, X3 and X4, respectively;

[0052] Z1 is hydrocarbyl or substituted hydrocarbyl;

[0053] Z3 comprises a 5- or 6-membered heterocyclic or aromatic ring substituted with an amidine group, the ring atoms of the 5- or 6-membered hetero...

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Abstract

The present invention relates to compounds, and prodrugs thereof, compositions and methods useful for preventing and treating thrombotic conditions in mammals. The compounds of the present invention, and prodrugs thereof, selectively inhibit certain proteases of the coagulation cascade.

Description

CROSS REFERENCE TO RELATED APPLICATIONS [0001] This application claims priority from Provisional Application Ser. Nos. 60 / 326,721 filed Oct. 3, 2001, 60 / 338,623 filed Oct. 24, 2001, 60 / 332,857 filed Nov. 6, 2001, 60 / 344,957 filed on Nov. 7, 2001, 60 / 332,107 and from 60 / 332,104 both filed on Nov. 21, 2001, which are all hereby incorporated by reference in their entirety.FIELD OF THE INVENTION [0002] The present invention relates to compounds, compositions and methods for preventing and treating thrombotic conditions such as coronary artery and cerebrovascular disease. More particularly, the invention relates to 5-membered polycyclic compounds, and prodrugs thereof that inhibit serine proteases of the coagulation cascade. BACKGROUND OF THE INVENTION [0003] Hemorrhage, intravascular thrombosis, and embolism are common clinical manifestations of many diseases (see R. I. Handin in Harrison's Principles of Internal Medicine (J. D. Wilson, et al. eds., 12th ed. 1991) New York, McGraw-Hill ...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/166A61K31/341A61K31/381A61K31/40A61K31/415A61K31/4152A61K31/4168A61K31/4196A61K31/421A61K31/426A61P7/02A61P9/00A61P11/00A61P35/00A61P43/00C07C257/18C07D207/14C07D207/32C07D207/34C07D207/46C07D211/56C07D211/98C07D213/74C07D231/12C07D231/38C07D231/46C07D231/48C07D233/88C07D237/04C07D239/10C07D239/22C07D241/04C07D241/20C07D249/08C07D249/14C07D253/06C07D253/075C07D263/48C07D265/02C07D277/20C07D277/42C07D307/22C07D333/36C07D401/12C07D403/10C07D413/12C07D471/04
CPCC07C257/18C07D471/04C07C2101/10C07D207/32C07D207/46C07D211/56C07D211/98C07D213/74C07D231/38C07D231/48C07D237/04C07D239/10C07D239/22C07D241/04C07D241/20C07D249/14C07D253/06C07D253/075C07D263/48C07D265/02C07D277/42C07D307/22C07D333/36C07D401/12C07D403/10C07D413/12C07C2101/04C07C2601/04C07C2601/10A61P11/00A61P35/00A61P43/00A61P7/02A61P9/00
Inventor SOUTH, MICHAEL S.WEBBER, RONALD K.HUANG, HORNG-CHIHTOTH, MIHALY V.MOORMANN, ALAN E.SNYDER, JEFFERY S.SCHOLTEN, JEFFREY A.GARLAND, DANNY J.RUEPPEL, MELVIN L.NEUMANN, WILLIAM L.LONG, SCOTTHUANG, WEITRUJILLO, JOHNPARLOW, JOHN J.JONES, DARIN E.CASE, BRENDAHAYES, MICHAEL J.
Owner PHARMACIA CORP
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