摘要:
This invention relates generally to methods for the treatment of myosin heavy chain (MyHC)-mediated conditions, and in particular, cardiovascular conditions.
摘要:
This invention relates generally to compounds and pharmaceutical compositions for the treatment of myosin heavy chain (MyHC)-mediated conditions, and in particular, cardiovascular conditions.
摘要:
Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.
摘要:
The invention relates to the 2-amino-7-(1-substituted-2-hydroxyethyl)-3, 5-dihydro-pyrrolo[3,2-d] pyrimidin-4-ones of formula I and tautomers thereof, wherein Ar represents biaryl, carbocyclic or heterocyclic aryl; pharmaceutically acceptable prodrug ester derivatives; and pharmaceutically acceptable salts thereof, which are particularly useful as potent purine nucleoside phosphorylase (PNP) inhibitors.
摘要:
Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.
摘要:
Compounds of formula (I) wherein R is hydrogen, lower alkyl, (C3–C6)cycloalkyl, hydroxy, halo, lower alkoxy, trifluoromethoxy, trifluoromethyl or cyano; and A is biaryl, optionally substituted β-naphthyl, bicyclic heterocyclic aryl, (C3–C6)cycloalkyl-monocyclic carbocyclic aryl, or (C5 or C6)cycloalkane fused-monocyclic carbocyclic aryl; pharmaceutically acceptable salts thereof; and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.
摘要:
Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.
摘要翻译:公开了式I的化合物,其中R是甲基或乙基; R 1是氯或氟; R 2是氢或氟; R 3是氢,氟,氯,甲基,乙基,甲氧基,乙氧基或羟基; R 4是氢或氟; 和R 5是氯,氟,三氟甲基或甲基; 作为选择性COX-2环加氧酶抑制剂; 及其药学上可接受的前药酯。
摘要:
Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.
摘要:
Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.
摘要:
The compounds of formula I ##STR1## wherein Ar represents biaryl, carbocyclic or heterocyclic aryl, are prepared, as substantially pure enantiomers, by(a) condensing a compound of the formula ##STR2## as a substantially pure enantiomer, wherein Ar has meaning as defined above and R.sub.6 is on O-protecting group with a lower alkyl ester of formic acid;(b) then condensing the compound so obtained with a compound of the formula ##STR3## wherein R.sub.8 is hydrogen or COOR.sub.3 and R.sub.3 is lower alkyl; (c) then cyclizing the compound so obtained to a compound of the formula ##STR4## as a substantially pure enantiomer; (d) and then condensing the compound so obtained(1) with a carbocyclic aroyl isothiocyanate and treatment of the product so obtained with an alkyl halide followed by anhydrous ammonia; or(2) with cyanamide in acid, optionally followed by treatment with a base.