摘要:
A process for preparing sulfone derivatives of the formula: wherein R¹ and R² are each a hydrogen atom, a lower alkyl group or a substituted or unsubstituted cyclo(lower)alkyl, cyclo(lower)alkylmethyl, lower alkenyl, heterocyclic, aryl or ar(lower)alkyl group, R⁴, R⁵, R⁶ and R⁷ are each a hydrogen atom, a lower alkyl group, a lower alkenyl group or a substituted or unsubstituted aryl grcup and Az is a 1,2,4- or 1,3,4-triazole or imidazole ring, which comprises subjecting a sulfide or sulfoxide compound of the formula: wherein R¹, R², R⁴, R⁵, R⁶, R⁷ and Az are each as defined above and n is an integer of 0 or 1 to oxidation with an oxidizing agent in the presence of a metal catalyst.
摘要:
A novel thiazole derivative of formula [1] or a pharmaceutically acceptable salt thereof:
wherein A is a singe bond, straight-chained or branched-chained lower alkylene or straight-chained or branched lower alkenylene, B is a single bond or -CO-; R¹ is carboxy or -CON(R⁷)OR⁸ (R⁷ and R⁸ are the same or different and each is hydrogen or lower alkyl); R² is lower alkyl; R³ and R⁴ are the same or different and each is hydrogen, lower alkyl or lower alkoxycarbonyl; R⁵ is hydrogen or halogen; and R⁶ is hydrogen, halogen, lower alkyl, hydroxy, lower alkoxy, thiol, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, nitro, amino, substituted amino, cyano, carboxy or acyl. The compounds of the present invention are useful as therapeutic or preventive drugs for autoimmune diseases and inflammatory diseases.
摘要翻译:式[1]的新型噻唑衍生物或其药学上可接受的盐:其中A为单键,直链或支链低级亚烷基或直链或支链低级亚烯基,B为单键或 -CO-; R 1是羧基或-CON(R 7)OR 8(R 7和R 8相同或不同,各自为氢或低级烷基)。 R 2是低级烷基; R 3和R 4相同或不同,各自为氢,低级烷基或低级烷氧基羰基; R 5是氢或卤素; R 6为氢,卤素,低级烷基,羟基,低级烷氧基,硫醇,低级烷硫基,低级烷基亚磺酰基,低级烷基磺酰基,硝基,氨基,取代氨基,氰基,羧基或酰基。 本发明的化合物可用作自身免疫疾病和炎性疾病的治疗或预防药物。
wherein Ar¹ and Ar² are carbocyclic or heterocyclic single ring or fused ring aromatic groups, R¹, R² and R³ are hydrogen, lower alkyl, aryl aryl-alkyl, aryl-alkyloxycarbonyl, alkyloxycarbonyl or acyl, and A¹ a nd A² are lower alkylene groups optionally substituted by oxo, exhibits a high N-methyl-D-aspartic acid (NMDA) receptor antagonistic effect and are therefore useful as a medicine for nerve degeneration diseases.
摘要:
An N-substituted triazole compound of the formula: wherein Ph is a phenyl group or a phenyl group substituted with one or two halogen atoms, R' is a C 1 -C 3 alkyl group, R 2 is a hydrogen atom or a C 1 -C 3 alkyl group, R 3 is a C 1 -C 8 alkyl group, a C 1 -C 8 cycloalkylalkyl group or a C 3 -C 6 cycloalkyl group and n is 0,1 or 2, or an acid addition salt thereof, which is useful as an antifungal agent.
in which B is a carbonyl group or a sulfonyl group, R¹, R², R³ and R⁴ are each a hydrogen atom or a lower alkyl group, or R¹ and R² or R¹ and R³ may be combined together to make a non-aromatic hydrocarbon ring or R¹ and R³ may be combined together to make an aromatic ring, said non-aromatic hydrocarbon ring being optionally bridged with a lower alkylene group or an oxygen atom therein and said aromatic ring, said non-aromatic hydrocarbon ring and said lower alkylene group being each optionally substituted with at least one lower alkyl, and n is an integer of 0 or 1; D is a group of the formula:
-(CH₂) p -A-(CH₂) q -
in which A is a non-aromatic hydrocarbon ring optionally bridged with a lower alkylene group or an oxygen atom, said non-aromatic hydrocarbon ring and said lower alkylene group being each optionally substituted with at least one lower alkyl, and p and q are each an integer of 0, 1 or 2; and Ar is an aromatic group, a heterocyclic aromatic group, a benzoyl group, a phenoxy group or a phenylthio group and G is
or Ar is a biphenylmethylidene group and G is
all of the above groups being each optionally substituted with at least one of lower alkyl, lower alkoxy and halogen; and its acid addition salts, useful as an antipsycotic agent.