摘要:
A compound represented by the formula (I) or a salt thereof, which is useful as an active ingredient of a pharmaceutical for the prevention and/or treatment of a disease induced by the activation of STAT6 and/or NF-?B. (I) wherein R 1 , R 2 , R 3 and R 4 independently represent a hydrogen atom, a halogen atom, a cyano group, a nitro group, a C 1-4 alkyl group, a halogenated C 1-4 alkyl group, or a C 1-4 alkoxy group; R 5 represents a halogen atom, a cyano group, a C 1-4 alkyl group, a halogenated C 1-4 alkyl group, or a C 1-4 alkoxy group; R 6 represents a C 5-7 cycloalkyl group, a substituted C 5-7 cycloalkyl group, a completely saturated 5- to 7-membered heterocyclic group or a substituted, completely saturated 5- to 7-membered heterocyclic group; X represents a single bond, an oxygen atom, a sulfur atom, NR 7 , -O-CH 2 or -N(R 8 )-CH 2 -; R 7 represents a hydrogen atom or a C 1-4 alkyl group, or together with a substituent in R 6 forms a single bond, a methylene group or an ethylene group; and R 8 represents a hydrogen atom, a C 1-4 alkyl group, or a C 7-12 aralkyl group.
摘要翻译:由式(I)表示的化合物或其盐,其可用作预防和/或治疗由STAT6和/或NF-κB活化引起的疾病的药物的活性成分。 (I)其中R 1,R 2,R 3和R 4独立地表示氢原子, 卤素原子,氰基,硝基,C 1-4烷基,卤代C 1-4烷基或C 1〜 4个烷氧基; R 5表示卤素原子,氰基,C 1-4烷基,卤代C 1-4烷基,或 C 1-4烷氧基; R 6表示C 5至5环烷基,取代的C 5至5环烷基,完全饱和的5-至7-元环 杂环基或取代的完全饱和的5-至7-元杂环基; X表示单键,氧原子,硫原子,NR 7,-O-CH 2或-N(R 8) -CH 2 SUB> - ; R 7表示氢原子或C 1-4烷基,或与R 6中的取代基一起形成单键, 亚甲基或亚乙基; R 8表示氢原子,C 1-4烷基或C 7-12芳烷基。
摘要:
The invention relates to a new and useful process for preparing N,N-substituted carbamoyl halides from secondary amines, carbon dioxide, trialkylsilyl chloride and a halogenating agent.
摘要:
A compound of Formula (A), wherein R 1 is C 1 -C 5 alkyl, C 3 -C 6 branched alkyl, C 4 -C 7 cycloalkyl, C 8 -C 12 fused or bridged polycycloalkyl, or heterocyclic ring, where any of the preceding alkyl, cycloalkyl or heterocyclic ring groups may be singly or multiply substituted with X; R 2 is H or R 1 ; and X is halo, carbonyl, carboxylic acid, carboxylic ester, carboxamide, substituted carboxamide, hydroxy, alkoxy, thioalkyl, sulphoxide, sulphone, sulphonamide, substituted sulphonamide, phenoxy, substituted phenoxy, phenyl, substituted phenyl, amino, substituted amino (including quaternary ammonium salts), N-oxide, imino, 5-7 membered heterocycle, or substituted heterocycle.
摘要:
A compound represented by the general formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug of any of these; and a drug containing any of these. (I) (In the formula, all the symbols are as defined in the description.) The compound represented by the general formula (I) has the ability to combine with an S1P receptor (especially EDG-1, EDG-6, and/or EDG-8). It is useful for the prevention and/or treatment of rejection reactions to transplantation, graft versus host diseases, autoimmune diseases, allergic diseases, neurodegenerative diseases, etc.
摘要:
Chimeric compounds are disclosed which are covalent conjugates of reversible or irreversible cholinergic up-regulators and non-steroidal anti-inflammatory drugs (NSAIDs), methods for their synthesis and use thereof for treatment and/or prevention of central nervous system (CNS) disorders and diseases.
摘要:
A process for the synthesis of 2,2,6,6-tetramethyl-4-oxopiperidine is disclosed wherein the process comprises reacting in a liquid phase reaction mixture: (A) at least one acetone compound, and (B) at least one ammonia donor compound, in the presence of a catalytically effective amount of a crystalline aluminosilicate containing calcium.
摘要:
The present invention is directed to pyrrolidine compounds of formula (I) wherein R , R , R , R , R , R and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
摘要:
The present invention relates to a compound of formula (Ia) or (Ib), wherein the R1, are each independently of one another hydrogen, halogen, NO2, cyano, -CONR5R6, -(R9)COOR4, -C(O)-R7, -OR8, -SR8, NHR8, -N(R8)2, carbamoyl, di(C1-C18alkyl)carbamoyl, -C(=NR5)(NHR6); unsubstituted C1-C18alkyl, C2-C18alkenyl, C2-C18alkynyl, C7-C9phenylalkyl, C3-C12cycloalkyl or C2-C12heterocycloalkyl; or C1-C18alkyl, C2-C18alkenyl, C2-C18alkynyl, C7-C9phenylalkyl, C3-C12cycloalkyl or C2-C12heterocycloalkyl, which are substituted by NO2, halogen, amino, hydroxy, cyano, carboxy, C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylamino or di(C1-C4alkyl)amino; or phenyl, naphthyl, which are unsubstituted or substituted by C1-C4alkyl, C1-C4alkoxy, C1-C4alkylthio, halogen, cyano, hydroxy, carboxy, C1-C4alkylamino or di(C1-C4alkyl)amino; R4 is hydrogen, C1-C18alkyl, phenyl, an alkali metal cation or a tetraalkylammonium cation; R5 and R6 are hydrogen, C1-C18alkyl, C2-C18alkyl which is substituted by at least one hydroxy group or, taken together, form a C2-C12alkylene bridge or a C2-C12alkylene bridge interrupted by at least one O or/and NR8 atom; R7 is hydrogen, C1-C18alkyl or phenyl; R8 is hydrogen, C1-C18alkyl or C2-C18alkyl which is substituted by at least one hydroxy group; R9 is C1-C12alkylene or a direct bond; or all R1 form together the residue of a polycyclic cycloaliphatic ring system or a polycyclic heterocycloaliphatic ring system with at least one di- or trivalent nitrogen atom; the R2 are independently of each other phenyl or C1-C6alkyl or two together with the linking carbon atom form a C5-C6cycloalkyl group; A is a divalent group required to form a cyclic 5-, 6- or 7-membered ring and R3 is a radical of formula (II), wherein X is phenyl, naphthyl or biphenyl, which are unsubstituted or substituted by NO2, halogen, amino, hydroxy, cyano, carboxy, C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylamino or di(C1-C4alkyl)amino; the R12 are independently of each other H or CH3; D is a group (A), a group C(O)-R13 or a group C(O)-R9-C(O)-R13; R13 is C1-C18alkyl and m is a number from 1 to 4. Further subjects of the invention are a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) a glycidyl or alkylcarbonyl functional nitroxide initiator compound of formula (Ia) or (Ib), a process for polymerizing ethylenically unsaturated monomers, and the use of glycidyl and alkylcarbonyl functional nitroxide initiators for radical polymerization.