摘要:
The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
摘要:
The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (κ) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
摘要:
Pharmaceutical formulations comprising a combination of niacin and an oxicam NSAID, for oral administration, and methods of preparing the formulations.
摘要:
The present invention relates to a class of compounds represented by the Formula I Wherein A1 is a pyridinyl of the formula optionally substituted by one or more Rk selected from the group consisting of hydroxy, alkyl, alkoxy, alkoxyalkyl, thioalkyl, haloalkyl, cyano, amino alkylamino, halogen, acylamino, sulfonamide and —COR; and R is hydroxy, alkoxy, alkyl or amino; and pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the αvβ3 and/or αvβ5 integrin.
摘要:
The present invention relates to a class of compounds represented by the Formula I. or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the &agr;V&bgr;3 and/or the &agr;V&bgr;5 integrin.
摘要:
Novel bicyclic compounds of the formula (I), stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided. Additionally, methods of forming novel bicyclic compounds, stereoisomers, and/or pharmaceutically acceptable salts of the novel bicyclic compounds, and/or pharmaceutically acceptable salts of the stereoisomers of the novel bicyclic compounds are provided: wherein R1, R2, m, and n are defined herein.
摘要:
The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively antagonizing the αVβ3 and/or the αVβ5 integrin without significantly antagonizing the IIb/IIIa or αVβ6 integrin.
摘要:
The present invention relates to a class of compounds represented by the Formula 1. or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula 1, and methods of selectively inhibiting or antagonizing the &agr;v&bgr;3 and/or the &agr;v&bgr;5 integrin.
摘要:
The present invention relates to compounds of the formula ##STR1## wherein HET is ##STR2## m is an integer from 1 to 4; R.sup.1 and R.sup.2 are independently selected from the group consisting of linear or branched alkyl of 1 to 6 carbon atoms; and cycloalkyl or cycloalkylalkyl having 3 to 7 ring carbon atoms, the ring carbon atoms optionally substituted with one or more alkyl groups having 1 to about 4 carbon atoms each;X is a substituent selected from the group consisting of hydrogen, halogen, alkyl, alkoxy, alkoxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkylthio, and alkylthioalkyl, wherein each of said alkyl moieties has from 1 to about 6 carbon atoms; andY and Z are independently selected from the group consisting of hydrogen, alkoxy of about 1 to 6 carbon atoms and halogen;and pharmaceutical compositions containing a therapeutically effective amount of the compounds in combination with a pharmaceutically acceptable carrier and a method for treating diseases mediated by platelet activating factor.
摘要翻译:本发明涉及下式的化合物,其中HET是(i)图像(ii)和(iii)m是1至4的整数; R 1和R 2独立地选自具有1至6个碳原子的直链或支链烷基; 和环碳原子数为3〜7的环烷基或环烷基烷基,环碳原子任选被一个或多个具有1至约4个碳原子的烷基取代; X是选自氢,卤素,烷基,烷氧基,烷氧基烷基,氨基烷基,烷基氨基烷基,二烷基氨基烷基,烷硫基和烷硫基烷基的取代基,其中每个所述烷基部分具有1至约6个碳原子; Y和Z独立地选自氢,约1至6个碳原子的烷氧基和卤素; 以及含有治疗有效量的化合物与药学上可接受的载体组合的药物组合物和用于治疗由血小板活化因子介导的疾病的方法。
摘要:
The invention is directed to novel substituted benzylamino quinolines, compounds comprising substituted benzylamino quinolines, methods of making substituted benzylamino quinolines, the use of substituted benzylamino quinolines for treating or preventing a variety of conditions or diseases associated with lipoprotein metabolism, and the use of substituted benzylamino quinolines as cholesterol ester-transfer protein inhibitors.