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    • 3. 发明申请
    • THIAZOLIDINE DERIVATIVES
    • 噻唑烷衍生物
    • WO1997031896A1
    • 1997-09-04
    • PCT/JP1997000581
    • 1997-02-27
    • SANKYO COMPANY, LIMITEDISHIHARA, SadaoSAITO, FujioMASUKO, HidekazuOHHATA, YasuoMIYAKE, ShigekiYORIKANE, RyosukeFUKUDA, Norio
    • SANKYO COMPANY, LIMITED
    • C07D207/16
    • C07D277/06
    • Thiazolidine derivatives represented by general formula (I), or pharmacologically acceptable salts thereof. In said formula, X represents methylene, oxygen, or sulfur; R represents an alkanoyl group having one or more substituents [wherein essential substituents comprise groups represented by the formula: -S-R (where R represents hydrogen, aliphatic acyl, alkoxycarbonyl, arylcarbonyl optionally substituted by alkyl, alkoxy, or halogeno, or aromatic heterocyclic carbonyl which contains a heteroatom selected from the group consisting of nitrogen, oxygen, and sulfur and which may be optionally substituted by alkyl, alkoxy, or halogeno), while desirable substituents represent amino, mono- or dialkylamino, protected amino, or protected monoalkylamino]; and "A" represents alkylene or a group represented by the formula: -B-D-E- (where B and E may be the same or different and each represents a single bond or alkylene, and D represents cycloalkylene optionally substituted by alkyl). The compounds have excellent collateral vasodilating and antianginal actions, and are useful for the treatment or prevention of angina pectoris.
    • 由通式(I)表示的噻唑烷衍生物或其药理学上可接受的盐。 在所述式中,X表示亚甲基,氧或硫; R 1表示具有一个或多个取代基的烷酰基[其中基本取代基包括由下式表示的基团-SR 2(其中R 2表示氢,脂族酰基,烷氧基羰基,任选被烷基,烷氧基取代的芳基羰基 ,或卤素,或芳族杂环羰基,其含有选自氮,氧和硫的杂原子,并且其可任选被烷基,烷氧基或卤素取代),而所需的取代基表示氨基,单或二烷基氨基, 保护的氨基或受保护的单烷基氨基]; 和“A”表示亚烷基或由下式表示的基团:-B-D-E-(其中B和E可以相同或不同,各自表示单键或亚烷基,D表示任选被烷基取代的亚环烷基)。 该化合物具有优异的侧支血管扩张和抗心绞痛作用,可用于治疗或预防心绞痛。
    • 7. 发明申请
    • N-PHENYLATED AMIDE AND UREA DERIVATIVES
    • N-苯基酰胺和尿素衍生物
    • WO1996003378A1
    • 1996-02-08
    • PCT/JP1995001481
    • 1995-07-26
    • SANKYO COMPANY, LIMITEDYOSHIDA, AkiraKOGEN, HiroshiHAYAKAWA, IchiroODA, KozoKASAI, TakashiSIMADA, KouseiYOSHIDA, YumiISHIHARA, SadaoSAITO, FujioOHHATA, YasuoKOGA, TeiichiroKITAZAWA, EiichiTOKUI, Taro
    • SANKYO COMPANY, LIMITED
    • C07D213/40
    • C07D231/12C07D233/64C07D295/135C07D317/58C07D405/12
    • Novel N-phenylated amide and urea derivatives represented by general formula (I) and salts thereof, which have excellent ACAT inhibitory activity and peroral absorbability and are useful as a remedy and/or a preventive for arteriosclerosis, wherein R represents C1-C12 alkyl or cycloalkyl-alkyl; R represents H or any of the groups defined above with respect to R ; R , R and R represent each independently H, optionally protected OH, nitro, C1-C12 alkyl, optionally mono- to pentafluorinated C1-C4 alkyl, alkoxy, halogeno, optionally C1-C4-alkylated mono- or dialkylamino, or five- or six-membered nitrogenous saturated heterocycle, or alternatively adjacent groups R and R are combined together to form -O-(CH2)m-O- (m being an integer of 1 to 3); R represents C1-C6 alkyl; R represents A -R (A being C1-C6 alkylene or C3-C5 alkenylene; and R being a heterocyclic group selected from among those belonging to the following group alpha and optionally substituted by halogeno, C1-C4 alkyl or C1-C4 hydroxyalkyl) or A -X-A -R (A being C1-C6 alkylene or C3-C5 alkenylene; X being O, S, NH, C1-C4 alkylimino, sulfinyl or sulfonyl; A being a single bond, C1-C6 alkylene or C3-C5 alkenylene; and R being as defined above, provided that the total number of the carbon atoms of A and A is 1 to 8 and that when A represents a single bond, the heterocyclic group R is bonded to X at the ring carbon atom); and n represents 0 or 1. Group alpha : imidazolyl, pyrazolyl, pyrazolidinyl, 1,2,4-triazolyl, tetrazolyl, morpholino, piperazinyl,2-pyridon-1-yl, 2-pyrimidinyl, pyridyl, pyrazinyl, 1,3,5-triazin-2-yl, benzimidazolyl, piperidinyl, pyrrolidinyl and azetidinyl groups.
    • 具有优异的ACAT抑制活性和口服吸收性的由通式(I)表示的新型N-苯基酰胺和脲衍生物及其盐,可用作动脉硬化的补救剂和/或预防药物,其中R 1a表示C1- C12烷基或环烷基 - 烷基; R 16表示H或上述关于R 1a定义的任何基团; R 2a,R 2b和R 2c各自独立地表示H,任选保护的OH,硝基,C 1 -C 12烷基,任选一至五氟化的C 1 -C 4烷基,烷氧基,卤代,任选被C 1 -C 4烷基化 单 - 或二烷基氨基或五或六元含氮饱和杂环,或者相邻基团R 2a和R 2b组合在一起形成-O-(CH 2)m O-(m是1〜 3); R 3表示C 1 -C 6烷基; R 4表示A 1 -R 5(A 1)是C 1 -C 6亚烷基或C 3 -C 5亚烯基; R 5是选自以下组中的α和 任选被卤代,C 1 -C 4烷基或C 1 -C 4羟烷基取代)或A 2 -XA 3 -R 5(A 2是C 1 -C 6亚烷基或C 3 -C 5亚烯基; X是O, S,NH,C 1 -C 4烷基亚氨基,亚磺酰基或磺酰基; A 3为单键,C 1 -C 6亚烷基或C 3 -C 5亚烯基; R 5如上所定义,条件是碳 A 2和A 3的原子为1〜8,当A 3表示单键时,杂环基R 5在环碳原子上与X键合); 组α:咪唑基,吡唑基,吡唑烷基,1,2,4-三唑基,四唑基,吗啉代,哌嗪基,2-吡啶酮-1-基,2-嘧啶基,吡啶基,吡嗪基,1,3, 5-三嗪-2-基,苯并咪唑基,哌啶基,吡咯烷基和氮杂环丁烷基。