摘要:
A process for the preparation of 4-[4-[4-[4-[[(3R,5R)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)-3-furanyl]methoxy]phenyl]-1-piperazinyl]phenyl]-2-[(1S,2S)-1-ethyl-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazol-3-one compound of formula-1, its intermediates and polymorphs thereof. (I).
摘要:
The invention relates to compounds of formula (II) for use as drugs that selectively inhibit the proliferation of SMCs in comparison with the proliferation of ECs: formula (II), wherein R 1 to R 6 are selected from -H, -F, -CH 3 , -CF 3 , -CF 2 CH 3 , -OCH 3 , -COCH 3 , -C 4 H 9 , -COOC 2 H 5 , and -C 6 H 5 or two vicinal groups from R 1 to R 6 are of such a nature and are connected to each other in such a way that said vicinal groups form a saturated or unsaturated carbocyclic ring together with the two carbon atoms to which said vicinal groups are bonded; R 7 is selected from OH, allyloxy, propargyloxy, 2,2-dimethylpropanoyloxy (pivaloyloxy), butanoyloxy, 3-methylbutanoyloxy, 2-butenoyloxy, 2-methyl-2-butenoyloxy, 3-methyl-2-butenoyloxy, isopentanoyloxy, 2-ethylbutanoyloxy, 3,3-dimethyl-butanoyloxy, cyclopropylcarbonyloxy, cyclobutylcarbonyloxy, cyclopentylcarbonyloxy, cyclopentenylcarbonyloxy, cyclohexylcarbonyloxy, cyclohexenylcarbonyloxy, adamantylethanoyloxy, 3-phenylpropenoyloxy (cinnamyloyloxy), 2-methylbenzoyloxy, and naphthoyloxy; and one or more ring carbon atoms are possibly replaced by heteroatoms in ring A and/or ring B; wherein the compounds of formula (II) are selected from compounds that are obtained by corresponding combination of groups R 1 to R 7 and that inhibit the proliferation of SMCs at least 50% more strongly than the proliferation of ECs; and a new production method for such compounds of formula (II).
摘要翻译:其中:R 1至R 6为-H,-F,-CH 3,-CF 3,-CF 2 CH 3,-OCH 3,-COCH 3,-C 4 H 9,-COOC 2 H 5或-C 6 H 5,或者R 1至R 6的两个连位残基形成饱和或不饱和的 碳环与它们所连接的两个碳原子一起; R7是OH,烯丙氧基,炔丙氧基,2,2-二甲基丙酰氧基(新戊酰氧基),丁酰氧基,3-甲基丁酰氧基,2-丁烯氧基,2-甲基-2-丁烯酰氧基,3-甲基-2-丁酰氧基,异戊酰氧基, - 乙基丁酰氧基,3,3-二甲基丁酰氧基,环丙基羰基氧基,环丁基羰基氧基,环戊基羰基氧基,环戊烯基羰基氧基,环己基羰氧基,环己烯基羰基氧基,金刚烷基乙酰氧基,3-苯基丙酰氧基(肉桂酰氧基),2-甲基苯甲酰氧基或萘氧基。 其中在环A和/或B中,一个或多个碳环原子任选被杂原子取代; 其中式(II)化合物通过组合残基R 1至R 7而获得,其抑制SMC增殖比EC增殖更有效地至少50%。
摘要:
The present invention relates to tetrahydrofuran derivatives, a plasticizer composition containing said tetrahydrofuran derivatives, molding materials containing a thermoplastic polymer and such a tetrahydrofuran derivative, to a process for the production of these tetrahydrofuran derivatives and their use.
摘要:
The present invention relates to a process for the preparation of 4-[4-[4-[4-[[(3R,5R)-5-(2,4-difluorophenyl) tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)-3-furanyl]methoxy]phenyl]-1-piperazinyl] phenyl]-2-[(1S,2S)-1-ethyl-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazol-3-one compound of formula-1, its intermediates and polymorphs thereof.
摘要:
The present invention relates to new substituted triazoles and imidazoles compounds of formula I as defined in the description, and the N-oxides, and salts thereof, their preparation and intermediates for preparing them. The invention also relates to the use of these compounds for combating harmful fungi and seed coated with at least one such compound and also to compositions comprising at least one such compound.
摘要:
The present invention relates to new substituted triazoles and imidazoles compounds of formula I as defined in the description, and the N-oxides, and salts thereof, their preparation and intermediates for preparing them. The invention also relates to the use of these compounds for combating harmful fungi and seed coated with at least one such compound and also to compositions comprising at least one such compound.
摘要:
This disclosure relates to sphingosine-1 -phosphate (SlP) receptor antagonists, compositions comprising the SlP receptor antagonists and methods for using and processes for making the SlP receptor antagonists. In particularly, this disclosure relates to sphingosine-1 -phosphate 1 (SlPl) receptor antagonists, compositions comprising the SlPl receptor antagonist and methods for using the SlPl receptor antagonist, such as in the treatment of cancer, and processes for making the SlPl receptor antagonists.