摘要:
Methods of treating Factor VIIa-associated conditions in a mammal are described, comprising administering to the mammal in need of treatment thereof an effective amount of at least one compound having the formula (I), or a pharmaceutically-acceptable salt, hydrate or prodrug thereof.
摘要:
Compounds having the formula (I), are effective as inhibitors of IMPDH enzyme and/or serine protease Factor VIIa, wherein B is a monocyclic or bicyclic carbocyclic or heterocyclic ring, D is a monocyclic or bicyclic carbocyclic or heterocyclic ring except when A is a heterocyclic ring, then D is a heterocyclic ring system, R is hydrogen or C1-4alkyl, and A, R1, R2 and R4 are as defined in the specification.
摘要:
Compounds having the formula (I), or a stereoisomer or pharmaceutically-acceptable salt, or hydrate thereof, are useful as factor VIIa inhibitors, wherein X is —NR6S(O)pR16; W is hydrogen or —(CR7R8)q—W1; W1 is hydrogen or a bond with R6; Z is a 5-membered heteroaryl group, a five to six membered heterocyclo or cycloalkyl group, a 9 to 10 membered bicyclic aryl or heteroaryl, or a six membered aryl or heteroaryl, and R1, R2, R3, R6, R7, and R16 are as defined in the specification.
摘要翻译:具有式(I)的化合物或其立体异构体或药学上可接受的盐或其水合物可用作因子VIIa抑制剂,其中X为-NR 6 S(O) 16< 16> W是氢或 - (CR 7 R 8)。 W 1是氢或与R 6的键; Z是5元杂芳基,5至6元杂环基或环烷基,9至10元双环芳基或杂芳基,或6元芳基或杂芳基,R 1,R 2, R 2,R 3,R 6,R 7和R 16均为 在规范中定义。
摘要:
Compounds of formula I and II, or pharmaceutically-acceptable salts thereof, are useful as inhibitors of Factor VIIa, Factor IXa, Factor Xa, Factor FXIa, tryptase, and urokinase, wherein ring B is phenyl or pyridyl, L is a linker, and R1-R27, W, Z1, and Z2 are as defined in the specification.
摘要:
Compounds of the formula ##STR1## wherein R.sub.1 is an amino substituted pyrimidinone or a pyrimidinedione including pharmaceutically acceptable salts are useful as antiviral agents.
摘要:
Novel intermediates useful in the preparation of the optically active antiviral compound [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobutyl]-1,9-dihydro-6H-purin-6-one are described.
摘要:
The present invention provides a method for treating a thrombotic or an inflammatory disorder administering to a patient in need thereof a therapeutically effective amount of at least one compound of Formula (I) or Formula (V): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L, Z, R3, R4, R6, R11, X1, X2, and X3 are as defined herein. The compounds of Formula (I) are useful as selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors. This invention also provides compounds within the scope of Formula I and relates to pharmaceutical compositions comprising these compounds.
摘要:
Compounds having the formula (I), and pharmaceutically-acceptable salts, hydrates, or prodrugs thereof, are useful as serine protease inhibitors, wherein X is —OH, —O(alkyl), —O(aryl), —O(arylalkyl), —NR5(aryl), or —NR5(arylalkyl); W is hydrogen or —(CR7R8)q—W1; W1 is hydrogen or a bond with R6; Z is a 5-membered heteroaryl group, a five to six membered heterocyclo or cycloalkyl group, a 9 to 10 membered bicyclic aryl or heteroaryl, or a six membered aryl or heteroaryl, and R1, R2, R3, R5, R6, R7, and R16 are as defined in the specification.
摘要翻译:具有式(I)化合物及其药学上可接受的盐,水合物或前药可用作丝氨酸蛋白酶抑制剂,其中X为-OH,-O(烷基), - (芳基), - (芳基烷基) ,-NR 5(芳基)或-NR 5(芳基烷基); W是氢或 - (CR 7 R 8)其中W是氢或 - (CR 7 R 8) W 1是氢或与R 6的键; Z是5元杂芳基,5至6元杂环基或环烷基,9至10元双环芳基或杂芳基,或6元芳基或杂芳基,R 1, R 3,R 3,R 5,R 6,R 7和R 7, 16 SUB>如说明书中所定义。
摘要:
A purine salt of the formula ##STR1## wherein Y.sub.1 is chloro, bromo, or iodo, and R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are independently selected from alkyl and substituted alkyl.