摘要:
Disclosed herein are compounds of formula (I) that may be specific to PPAR and/or EGF receptors, and methods of making and using same.
wherein X is C 1 -C 3 alkylene, optionally substituted with one, two or three substituents selected from halogen or hydroxyl; R 1 is selected from the group consisting of C 1 -C 6 alkyl, C 3 -C 6 cycloalkyl, C 2 -C 6 alkenyl, and C 2 -C 6 alkynyl; R 2 is selected from the group consisting of hydrogen and C 1 -C 6 alkyl; R 3 is independently selected, for each occurrence from the group consisting of hydrogen, C 1 -C 6 alkoxy, C 1 -C 6 alkyl, cyano, C 3 -C 6 cycloalkyl, halogen, hydroxyl, and nitro; R 4 is selected from the group consisting of hydrogen and C 1 -C 6 alkyl; R 5 is hydrogen C 1 -C 6 alkyl; or pharmaceutically acceptable salts or N-oxides thereof.
摘要翻译:本文公开了可以对PPAR和/或EGF受体特异的式(I)化合物及其制备和使用方法。 其中X是任选被1,2或3个选自卤素或羟基的取代基取代的C 1 -C 3亚烷基; R 1选自C 1 -C 6烷基,C 3 -C 6环烷基,C 2 -C 6烯基和C 2 -C 6炔基; R 2选自氢和C 1 -C 6烷基; R 3各自独立地选自氢,C 1 -C 6烷氧基,C 1 -C 6烷基,氰基,C 3 -C 6环烷基,卤素,羟基和硝基; R 4选自氢和C 1 -C 6烷基; R 5是氢C 1 -C 6烷基; 或其药学上可接受的盐或N-氧化物。
摘要:
Disclosed are an N-benzylaniline derivative and uses thereof. The derivative is a compound represented by formula I or a pharmaceutically acceptable salt thereof. The compound has an action of protecting against cerebral ischemia/reperfusion injury and an analgesic action for chronic pathologic pains, and may be used to prepare drugs for cerebral apoplexy, neuropathic pain, and inflammatory pain. Moreover, because of the unique mechanism of action of the compound, the compound can be used to prepare drugs for epilepsy, affective disorder, and neurodegenerative diseases.
摘要:
The present invention is related to alkynyl aryl carboxamides of Formula (I’) and use thereof for the treatment and/or prevention of an inflammatory disorder, obesity and/or metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type I and/or II, inadequate glucose tolerance. insulin resistance, hyperlipidemia, hypertriglyceridemia- hypercholesterolemia, polycystic ovary syndrome (PCOS). In particular, the present invention is related to the use of alkynyl aryl carboxamides of Formula (I’) to modulate, notably to inhibit the activity of PTPs. (I’) A is a C2-C15 alkynyl, C2-C6-alkynyl aryl, C2-C6-alkynyl heteroaryl. Cy is an aryl, heteroaryl, cycloalkyl or heterocycle group; n is either 0 or 1. Cy' is an aryl., which may optionally be fused by a 3-8 membered cycloalkyl. R1and R2 are independently from each other is selected from the group consisting of hydrogen or (CI-C6)alkyl. R4and R5 are each independently from each other selected from the group consisting of H, hydroxy. C1 -C6 alkyl, carboxy, C1-C6 alkoxy, C1 -C3 alkyl carboxy, C2-C3 alkenyl carboxy, C2-C3 alkynyl carboxy, amino or R4 and R5 may form an unsaturated or saturated heterocyclic ring, whereby at least one of R4 or R5 is not a hydrogen or C1-C6 alkyl.
摘要:
A compound of formula (I) wherein X is CH=CH, CH 2O wherein the oxygen atom is bound to ring B or OCH 2wherein the oxygen atom is bound to ring A; Y is hydrogen, straight or branched C1-C6 alkyl or a pharmaceutically acceptable inorganic cation; R1 is ethyl or cyclopropyl; and R2 and R3 are the same or different and are selected from F, Cl, Br, CF 3and OCF 3. The compound is useful for the treatment of autoimmune diseases, inflammatory diseases, organ transplant rejection and malignant neoplasia. A pharmaceutical composition. A method for preparing the compound.