摘要:
The invention provides pharmaceutically useful thieno[2,3-d]pyrimidinediones, processes for their production, pharmaceutical compositions containing them and methods of treatment involving their use.
摘要:
The present invention provides an intermediate for producing a thienopyridine derivative useful as a GnRH antagonist as well as an efficient and safe method for producing the same in an industrial scale at a high yield.
摘要:
There is disclosed a process for producing hexahydro-2-oxo-1H-thieno[3,4-d]imidazole-4-pentanoic acid of the formula (2): which is characterized by contacting a compound of the formula (1): wherein R1 and R2 represent a hydrogen atom or a benzyl group, but R1 and R2do not simultaneously represent a hydrogen atom, and R3 represents a hydrogen atom or a carboxyl group, with sulfuric acid in the presence of an aromatic hydrocarbon.
摘要:
This invention concerns a bicyclic compound of Formula (I), wherein: G is N, CH or C(CN); ring X is a 5- or 6-membered fused heteroaryl ring which contains 1, 2, or 3 heteroatoms selected from oxygen, sulphur and nitrogen; m is 0-2; R1 is a group such as hydroxy, halo, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; each of R2 and R3 is hydrogen, halo, C1-6alkyl, C2-6alkenyl or C2-6 alkynyl; R4 is a group such as hydrogen, hydroxy, C1-6alkyl, C1-6alkoxy, amino and N-C1-6alkylamino; R5 is a group such as hydrogen, halo, trifluoromethyl, cyano, nitro, amino and hydroxy, and q is 0-4; or a pharmaceutically acceptable salt or an in vivo cleavable ester thereof; processes for its preparation, a pharmaceutical composition containing it and its use in the treatment of diseases or medical conditions mediated by cytokines.
摘要翻译:本发明涉及式(I)的双环化合物,其中:G为N,CH或C(CN); 环X是含有1,2或3个选自氧,硫和氮的杂原子的5-或6-元稠合杂芳环; m为0-2; R 1是羟基,卤素,三氟甲基,氰基,巯基,硝基,氨基,羧基和氨基甲酰基等基团。 R 2和R 3各自为氢,卤素,C 1-6烷基,C 2-6烯基或C 2-6炔基; R 4是氢,羟基,C 1-6烷基,C 1-6烷氧基,氨基和N-C 1-6烷基氨基; R 5为氢,卤素,三氟甲基,氰基,硝基,氨基和羟基的基团,q为0-4; 或其药学上可接受的盐或其体内可裂解的酯; 其制备方法,含有它的药物组合物及其在治疗由细胞因子介导的疾病或医学病症中的用途。
摘要:
The invention relates to a process for preparing compounds of the formula I In this process a 2-aminobenzothiophene-3-carboxylic ester of the formula II is reacted with a nitrile of the formula III N≡C—R1 III in solution or suspension in a solvent in the presence of an acid.
摘要:
The invention provides the use in combating fungi of compounds of general formula I wherein R1 is hydrogen, hydroxy, acyl, acyloxy, optionally substituted amino, Ra, Ra3Si, RaS or RaO, where Ra is optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted cycloalkenyl, optionally substituted aryl or optionally substituted heterocyclyl; Z is oxygen or sulfur; M is a thiophene ring; and R3 and R4, which may be the same or different, have the same meaning as Ra or can be optionally substituted amino, hydrogen, halogen, cyano, nitro or a group ORc or S(O)mRc, where Rc has the same meaning as Ra or is hydrogen or acyl and m is 0, 1 or 2; or R3 and R4 together with the atoms to which they are attached form an optionally substituted carbocyclic or heterocyclic ring; together with tautomers of compounds where R1 is hydrogen.
摘要:
The present invention concerns the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; Alk is C1-6alkanediyl; n is 1 or 2; p is 0, 1 or 2; D is an optionally substituted mono-, bi- or tricyclic nitrogen containing heterocycle having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, compositions comprising them and their use as a medicine.
摘要:
Novel orthorombic polymorph of clopidogrel hydrogen sulfate or hydrogen sulfate of methyl (+)-(S)-&agr;-(2-chlorophenyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine-5-acetate and a process for its preparation
摘要:
The invention provides certain pyrrolo-, thieno-, furano- and pyrazolo-[3,4-d]pyridazinones, processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and methods of treatment involving their use.