-
公开(公告)号:US5744487A
公开(公告)日:1998-04-28
申请号:US378615
申请日:1995-01-26
申请人: Masahiro Ohshima , Norimichi Iwase , Shigeo Sugiyama , Koichi Sugawara , Misao Okitsu , Yoshikuni Tamao , Yasuhiro Morinaka
发明人: Masahiro Ohshima , Norimichi Iwase , Shigeo Sugiyama , Koichi Sugawara , Misao Okitsu , Yoshikuni Tamao , Yasuhiro Morinaka
IPC分类号: A61K38/00 , C07D207/16 , C07D211/60 , C07D401/12 , C07D405/12 , C07D409/06 , C07K5/06 , C07K5/062 , C07K5/065 , C07K5/072 , A61K31/40 , C07D207/09
CPC分类号: C07D401/12 , C07D207/16 , C07D211/60 , C07D405/12 , C07D409/06 , C07K5/0606 , C07K5/06069 , C07K5/06078 , C07K5/06113 , C07K5/06191 , A61K38/00
摘要: A prolineamide derivative represented by the formula (I): ##STR1## or a salt or hydrate thereof or a pharmaceutically acceptable salt thereof, which has a protease inhibition activity and is useful as an active ingredient of pharmaceutical compositions is provided.
摘要翻译: 提供了具有蛋白酶抑制活性并可用作药物组合物的活性成分的由式(I)表示的脯氨酰胺衍生物:其中(I)或其盐或水合物或其药学上可接受的盐。
-
公开(公告)号:US5462941A
公开(公告)日:1995-10-31
申请号:US215426
申请日:1994-03-21
IPC分类号: A61K31/50 , A61K31/502 , A61P7/02 , A61P9/00 , A61P9/10 , C07D237/34 , C07D241/44 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/04 , C07D417/14 , C07D491/04 , C07D491/048 , C07D495/04 , C07D521/00 , C07D247/02
CPC分类号: C07D231/12 , C07D233/56 , C07D237/34 , C07D249/08 , C07D403/04 , C07D405/04 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/04 , C07D491/04 , C07D495/04
摘要: A 3,6-disubstituted pyridazine derivative having excellent platelet agglutination inhibitory effects. It is useful for a preventive medicine or a therapeutic medicine for a cerebrovascular disorder such as cerebral thrombosis and cerebral embolism, an ischemic heart disease such as myocardial infarction, and a circulation disorder such as peripheral circulation disorder. A pharmaceutical composition containing a compound of the present invention as an effective ingredient and a process for preparing the same are also disclosed. The compound has the formula (I) ##STR1## wherein A represents an alkyl group having 3 to 6 carbon atoms; a cycloalkyl group having 5 to 7 carbon atoms; a phenyl group, a thienyl group, a furyl group, a thiazolyl group, a phenoxy group, a phenylalkyl group having 7 to 9 carbon atoms, a phenylthio group, a 5-6 membered saturated heterocyclic group containing one or more nitrogen atoms, a pyridyl group or an imidazolyl group each of which may have at least one substituent selected from the group consisting of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms and a halogen atom; B represents (a) --NH--D wherein D represents ##STR2## (4) --CH.sup.3 R.sup.4 ; or (5) an alkyl group having 3 to 8 carbon atoms; or ##STR3## and the ring C represents a benzene ring.
摘要翻译: 具有优异的血小板凝集抑制作用的3,6-二取代哒嗪衍生物。 对脑血栓形成和脑栓塞,心肌梗死等缺血性心脏病,周围循环障碍等循环障碍的脑血管障碍的预防药或治疗药有用。 还公开了含有本发明化合物作为有效成分的药物组合物及其制备方法。 该化合物具有式(I)其中A表示具有3至6个碳原子的烷基; 具有5至7个碳原子的环烷基; 苯基,噻吩基,呋喃基,噻唑基,苯氧基,具有7〜9个碳原子的苯基烷基,苯硫基,含有一个或多个氮原子的5-6元饱和杂环基, 吡啶基或咪唑基,其各自可具有至少一个选自具有1至4个碳原子的烷基,具有1至4个碳原子的烷氧基和卤素原子的取代基; (A)-NH-D其中D表示(1)图像(2)图像(3)(4)-CH 3 R 4; 或(5)碳原子数为3〜8的烷基; 或(B),环C表示苯环。
-
公开(公告)号:US5089494A
公开(公告)日:1992-02-18
申请号:US675259
申请日:1991-03-27
IPC分类号: C07D237/34
CPC分类号: C07D237/34
摘要: 4-Phenylphthalazine derivatives having platelet aggregation inhibitory activity of the formula: ##STR1## wherein R.sup.1 is an alkyl or hydroxyalkyl group of 1-5 carbon atoms; R.sup.2 is a hydrogen atom or an alkyl group of 1-5 carbon atoms; or R.sup.1 and R.sup.2, when taken together, may represent an alkylene group of 2-6 carbon atoms, said group optionally containing one or more oxygen atoms; R.sup.3 and R.sup.4 are independently a hydrogen or halogen atom, an alkyl or alkoxy group of 1-4 carbon atoms, or when two of R.sup.3 are adjacently positioned, (R.sup.3)l may represent a --O--(CH.sub.2).sub.p --O-- group and/or when two of R.sup.4 are adjacently positioned, (R.sup.4).sub.m may represent a --O--(CH.sub.2).sub.p --O-- group; R.sup.5 is a hydrogen or halogen atom, an alkyl or alkoxy group of 1-4 carbon atoms, a trifluoromethyl group or a hydroxy group, or when two of R.sup.5 are adjacently positioned, (R.sup.5).sub.n may represent a --O--(CH.sub.2).sub.p --O-- group; p is an integer of 1-3; l and m are independently an integer of 1-2; and n is an integer of 1-3, and optical isomers and pharmaceutically acceptable acid addition salts thereof.
-
公开(公告)号:US5422359A
公开(公告)日:1995-06-06
申请号:US171692
申请日:1993-12-22
IPC分类号: A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/443 , A61K31/4433 , A61P1/16 , A61P3/00 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P13/02 , A61P15/00 , A61P19/10 , A61P25/28 , A61P27/02 , A61P27/14 , A61P29/00 , A61P35/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07D207/32 , C07D207/335 , C07D263/32 , C07D277/22 , C07D277/28 , C07D307/52 , C07D333/22 , C07D333/28 , C07D405/12 , C07D407/12 , C07D409/12 , C07D213/30 , C07D213/32
CPC分类号: C07D207/335 , C07D263/32 , C07D277/28 , C07D307/52 , C07D333/22 , C07D333/28 , C07D405/12 , C07D409/12
摘要: Alpha-aminoketone derivatives of the present invention strongly inhibit thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L and calpain or the like and have excellent properties in absorbance on oral administration, tissue distribution and cell membrane permeability. The alpha-aminoketone derivatives can thus be used as therapeutic agents for treating muscular dystrophy, amyotrophy, cardiac infarction, stroke, Alzheimer's disease, disturbance of consciousness or dyskinesia caused upon brain trauma, multiple sclerosis, peripheral nervous neuropathy, cataract, inflammation, allergosis, fulminant hepatitis, osteoporosis, hypercalcemia, breast carcinoma, prostatic carcinoma or prostatomegaly. They may also be used as therapeutic agents for suppressing growth of cancer cells, preventing metastasis of cancer or suppressing aggregation of plaques.
摘要翻译: 本发明的α-氨基酮衍生物强烈地抑制木瓜蛋白酶,组织蛋白酶B,组织蛋白酶H,组织蛋白酶L和钙蛋白酶等硫醇蛋白酶,并且在口服给药,组织分布和细胞膜通透性方面的吸光度具有优异的性质。 因此,α-氨基酮衍生物因此可用作治疗肌营养不良症,肌萎缩症,心肌梗死,中风,阿尔茨海默病,意识障碍或脑外伤引起的运动障碍,多发性硬化,周围神经神经病变,白内障,炎症,过敏原, 暴发性肝炎,骨质疏松症,高钙血症,乳腺癌,前列腺癌或前列腺肥大。 它们也可以用作抑制癌细胞生长,预防癌转移或抑制斑块聚集的治疗剂。
-
公开(公告)号:US5416117A
公开(公告)日:1995-05-16
申请号:US202555
申请日:1994-02-28
IPC分类号: A61K31/165 , A61K31/18 , A61K31/19 , A61K31/195 , A61K31/27 , A61K31/415 , A61K31/47 , A61K38/00 , A61P1/16 , A61P3/00 , A61P5/00 , A61P7/02 , A61P9/00 , A61P9/10 , A61P19/10 , A61P25/00 , A61P25/02 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07C237/06 , C07C237/08 , C07C237/20 , C07C237/22 , C07C271/18 , C07C271/22 , C07C271/24 , C07C271/34 , C07C271/54 , C07C275/16 , C07C275/24 , C07C275/28 , C07C275/30 , C07C311/03 , C07C311/06 , C07C311/14 , C07C311/16 , C07C311/19 , C07C311/29 , C07C317/24 , C07C317/44 , C07C323/49 , C07C323/60 , C07C333/04 , C07D211/62 , C07D211/64 , C07D213/30 , C07D213/34 , C07D213/55 , C07D213/81 , C07D213/82 , C07D215/36 , C07D215/48 , C07D215/54 , C07D231/14 , C07D233/90 , C07D239/28 , C07D307/68 , C07D333/38 , C07K5/06 , C07K5/065 , C07K14/81 , C07C311/18
CPC分类号: C07D213/30 , C07C237/08 , C07C237/22 , C07C271/22 , C07C271/24 , C07C271/34 , C07C271/54 , C07C275/16 , C07C275/28 , C07C275/30 , C07C311/06 , C07C311/14 , C07C311/19 , C07C311/29 , C07C317/44 , C07C323/49 , C07C323/60 , C07D211/62 , C07D213/34 , C07D213/81 , C07D213/82 , C07D215/36 , C07D215/48 , C07D231/14 , C07D307/68 , C07D333/38 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/06078 , A61K38/00 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2101/18
摘要: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.
摘要翻译: 一种新颖的环丙烯酮衍生物(I),其对口服吸光度,组织转移和细胞膜通透性具有优异的性质,具有对硫醇蛋白酶如木瓜蛋白酶,组织蛋白酶B,组织蛋白酶H,组织蛋白酶L,钙蛋白酶等的有效抑制活性, 可用于治疗各种疾病如肌营养不良症,肌萎缩症。 还提供了制备化合物(I)的方法和含有该化合物的药物组合物。
-
公开(公告)号:US5424325A
公开(公告)日:1995-06-13
申请号:US171695
申请日:1993-12-22
申请人: Ryoichi Ando , Naoko Ando , Hirokazu Masuda , Toshiro Sasaki , Yasuhiro Morinaka , Chizuko Takahashi , Yoshikuni Tamao , Akihiro Tobe
发明人: Ryoichi Ando , Naoko Ando , Hirokazu Masuda , Toshiro Sasaki , Yasuhiro Morinaka , Chizuko Takahashi , Yoshikuni Tamao , Akihiro Tobe
IPC分类号: C07D213/32 , C07D213/38 , C07D263/20 , C07D277/26 , C07D307/38 , C07D307/42 , C07D307/46 , C07D307/85 , C07D333/16 , C07D333/18 , C07D333/22 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12 , A61K31/34 , A61K31/425 , C07D213/30
CPC分类号: C07D263/20 , C07D213/32 , C07D213/38 , C07D277/26 , C07D307/38 , C07D307/42 , C07D307/46 , C07D307/85 , C07D333/16 , C07D333/18 , C07D333/22 , C07D405/12 , C07D407/12 , C07D409/12 , C07D417/12
摘要: Aminoketone derivatives according to the present invention strongly inhibit thiol protease such as calpain, papain, cathepsin B, cathepsin H, cathepsin L or the like and have excellent properties concerning absorbance on oral administration, tissue distribution and cell membrane permeability. The aminoketone derivatives cart thus be used as therapeutic agents for treating muscular dystrophy, cataract, cardiac infarction, stroke, Alzheimer's disease, amyotrophy, osteoporosis and hypercalcemia and so on. It may also be used as therapeutic agents for preventing metastasis of cancer. In addition, the present derivatives are also applicable as intermediates for the preparation of ketone derivatives, which have inhibitory activity against thiol protease.
摘要翻译: 根据本发明的氨基酮衍生物强烈地抑制硫蛋白酶如钙蛋白酶,木瓜蛋白酶,组织蛋白酶B,组织蛋白酶H,组织蛋白酶L等,并且对于口服给药,组织分布和细胞膜通透性的吸光度具有优异的性质。 因此,氨基酮衍生物载体可用作治疗肌营养不良症,白内障,心肌梗塞,中风,阿尔茨海默病,肌萎缩,骨质疏松症和高钙血症等的治疗剂。 它也可以用作预防癌转移的治疗剂。 此外,本发明的衍生物也可用作制备对硫醇蛋白酶具有抑制活性的酮衍生物的中间体。
-
公开(公告)号:US5328909A
公开(公告)日:1994-07-12
申请号:US905544
申请日:1992-06-25
IPC分类号: A61K31/165 , A61K31/18 , A61K31/19 , A61K31/195 , A61K31/27 , A61K31/415 , A61K31/47 , A61K38/00 , A61P1/16 , A61P3/00 , A61P5/00 , A61P7/02 , A61P9/00 , A61P9/10 , A61P19/10 , A61P25/00 , A61P25/02 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07C237/06 , C07C237/08 , C07C237/20 , C07C237/22 , C07C271/18 , C07C271/22 , C07C271/24 , C07C271/34 , C07C271/54 , C07C275/16 , C07C275/24 , C07C275/28 , C07C275/30 , C07C311/03 , C07C311/06 , C07C311/14 , C07C311/16 , C07C311/19 , C07C311/29 , C07C317/24 , C07C317/44 , C07C323/49 , C07C323/60 , C07C333/04 , C07D211/62 , C07D211/64 , C07D213/30 , C07D213/34 , C07D213/55 , C07D213/81 , C07D213/82 , C07D215/36 , C07D215/48 , C07D215/54 , C07D231/14 , C07D233/90 , C07D239/28 , C07D307/68 , C07D333/38 , C07K5/06 , C07K5/065 , C07K14/81 , A61K31/16
CPC分类号: C07D213/30 , C07C237/08 , C07C237/22 , C07C271/22 , C07C271/24 , C07C271/34 , C07C271/54 , C07C275/16 , C07C275/28 , C07C275/30 , C07C311/06 , C07C311/14 , C07C311/19 , C07C311/29 , C07C317/44 , C07C323/49 , C07C323/60 , C07D211/62 , C07D213/34 , C07D213/81 , C07D213/82 , C07D215/36 , C07D215/48 , C07D231/14 , C07D307/68 , C07D333/38 , C07K5/06026 , C07K5/06043 , C07K5/06052 , C07K5/06078 , A61K38/00 , C07C2101/02 , C07C2101/04 , C07C2101/08 , C07C2101/14 , C07C2101/18
摘要: A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.
摘要翻译: 一种新颖的环丙烯酮衍生物(I),其对口服吸光度,组织转移和细胞膜通透性具有优异的性质,具有对硫醇蛋白酶如木瓜蛋白酶,组织蛋白酶B,组织蛋白酶H,组织蛋白酶L,钙蛋白酶等的有效抑制活性, 可用于治疗各种疾病如肌营养不良症,肌萎缩症。 还提供了制备化合物(I)的方法和含有该化合物的药物组合物。
-
公开(公告)号:US5834508A
公开(公告)日:1998-11-10
申请号:US798036
申请日:1997-02-06
申请人: Ryoichi Ando , Naoko Ando , Hirokazu Masuda , Yasuhiro Morinaka , Chizuko Takahashi , Yoshikuni Tamao , Akihiro Tobe
发明人: Ryoichi Ando , Naoko Ando , Hirokazu Masuda , Yasuhiro Morinaka , Chizuko Takahashi , Yoshikuni Tamao , Akihiro Tobe
IPC分类号: A61K31/16 , A61K31/18 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/35 , A61K31/351 , A61K31/352 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/472 , A61K38/00 , A61K38/55 , A61P1/16 , A61P3/00 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P19/10 , A61P25/02 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07C233/78 , C07C237/22 , C07C271/20 , C07C271/22 , C07C311/06 , C07C311/19 , C07C317/24 , C07C317/28 , C07C323/22 , C07C323/24 , C07C323/41 , C07C323/59 , C07D207/333 , C07D213/30 , C07D213/32 , C07D217/06 , C07D235/06 , C07D261/08 , C07D263/20 , C07D263/32 , C07D277/22 , C07D277/24 , C07D277/26 , C07D295/10 , C07D295/13 , C07D307/12 , C07D307/38 , C07D307/42 , C07D307/52 , C07D307/54 , C07D307/56 , C07D307/68 , C07D307/84 , C07D309/06 , C07D311/22 , C07D333/24 , C07D333/28 , C07D333/38 , C07D333/60 , C07D405/12 , C07D407/12 , C07D407/14 , C07D409/12 , C07D409/14 , C07K5/06 , C07K14/81 , C07D263/04 , C07D307/02 , C07D335/60
CPC分类号: C07D263/20 , C07C271/22 , C07C311/06 , C07C311/19 , C07C317/28 , C07C323/41 , C07C323/59 , C07D213/32 , C07D235/06 , C07D261/08 , C07D277/26 , C07D295/13 , C07D307/38 , C07D307/42 , C07D307/52 , C07D307/56 , C07D307/84 , C07D333/28 , C07D405/12 , C07D407/12 , C07D409/12 , C07K5/06043 , A61K38/00 , C07C2101/02 , C07C2101/08 , C07C2101/14
摘要: A novel ketone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.
摘要翻译: 一种对口服吸光度,组织转移和细胞膜通透性具有优异性质的对硫醇蛋白酶如木瓜蛋白酶,组织蛋白酶B,组织蛋白酶H,组织蛋白酶L,钙蛋白酶等具有有效抑制活性的新型酮衍生物(I) 可用于治疗各种疾病如肌营养不良症,肌萎缩症。 还提供了制备化合物(I)的方法和含有该化合物的药物组合物。
-
公开(公告)号:US5639783A
公开(公告)日:1997-06-17
申请号:US451720
申请日:1995-05-26
申请人: Ryoichi Ando , Naoko Ando , Hirokazu Masuda , Yasuhiro Morinaka , Chizuko Takahashi , Yoshikuni Tamao , Akihiro Tobe
发明人: Ryoichi Ando , Naoko Ando , Hirokazu Masuda , Yasuhiro Morinaka , Chizuko Takahashi , Yoshikuni Tamao , Akihiro Tobe
IPC分类号: A61K31/16 , A61K31/18 , A61K31/27 , A61K31/34 , A61K31/341 , A61K31/35 , A61K31/351 , A61K31/352 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/415 , A61K31/4184 , A61K31/42 , A61K31/421 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/472 , A61K38/00 , A61K38/55 , A61P1/16 , A61P3/00 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P19/10 , A61P25/02 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/08 , A61P43/00 , C07C233/78 , C07C237/22 , C07C271/20 , C07C271/22 , C07C311/06 , C07C311/19 , C07C317/24 , C07C317/28 , C07C323/22 , C07C323/24 , C07C323/41 , C07C323/59 , C07D207/333 , C07D213/30 , C07D213/32 , C07D217/06 , C07D235/06 , C07D261/08 , C07D263/20 , C07D263/32 , C07D277/22 , C07D277/24 , C07D277/26 , C07D295/10 , C07D295/13 , C07D307/12 , C07D307/38 , C07D307/42 , C07D307/52 , C07D307/54 , C07D307/56 , C07D307/68 , C07D307/84 , C07D309/06 , C07D311/22 , C07D333/24 , C07D333/28 , C07D333/38 , C07D333/60 , C07D405/12 , C07D407/12 , C07D407/14 , C07D409/12 , C07D409/14 , C07K5/06 , C07K14/81 , C07D311/24
CPC分类号: C07D263/20 , C07C271/22 , C07C311/06 , C07C311/19 , C07C317/28 , C07C323/41 , C07C323/59 , C07D213/32 , C07D235/06 , C07D261/08 , C07D277/26 , C07D295/13 , C07D307/38 , C07D307/42 , C07D307/52 , C07D307/56 , C07D307/84 , C07D333/28 , C07D405/12 , C07D407/12 , C07D409/12 , C07K5/06043 , A61K38/00 , C07C2101/02 , C07C2101/08 , C07C2101/14
摘要: A novel ketone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.
摘要翻译: 一种对口服吸光度,组织转移和细胞膜通透性具有优异性质的对硫醇蛋白酶如木瓜蛋白酶,组织蛋白酶B,组织蛋白酶H,组织蛋白酶L,钙蛋白酶等具有有效抑制活性的新型酮衍生物(I) 可用于治疗各种疾病如肌营养不良症,肌萎缩症。 还提供了制备化合物(I)的方法和含有该化合物的药物组合物。
-
公开(公告)号:US5783564A
公开(公告)日:1998-07-21
申请号:US669219
申请日:1996-06-24
申请人: Haruyuki Chaki , Naoko Ando , Yasuhiro Morinaka , Ken-ichi Saito , Tomoko Yugami , Rie Yoshida
发明人: Haruyuki Chaki , Naoko Ando , Yasuhiro Morinaka , Ken-ichi Saito , Tomoko Yugami , Rie Yoshida
CPC分类号: C07J41/0005 , C07J17/005
摘要: Sialic acid derivatives represented by the general formula (I): wherein R.sup.1 is a steroidal compound residue; R.sup.2 is H or alkyl; R.sup.3 is alkyl; ##STR1## wherein each of R.sup.6 and R.sup.7 is H, alkyl or the like and I is an integer of 0 to 6; or the like; X is O or S; R.sup.4 is H or acyl; and R.sup.5 is R.sup.14 O--(R.sup.14 is H or acyl) or R.sup.15 NH--(R.sup.15 is acyl or the like); their salts, hydrates or solvates are provided. Sialic acid derivatives of the present invention are expected to be effective medicines for the prevention and therapy of senile dementia including Alzheimer's disease and the like, because they increase ChAT activity in cholinergic neurons.
摘要翻译: 由通式(I)表示的唾液酸衍生物:其中R1是甾族化合物残基; R2是H或烷基; R3是烷基; 其中R6和R7各自为H,烷基等,I为0-6的整数; 或类似物; X是O或S; R4是H或酰基; R5为R14O-(R14为H或酰基)或R15NH-(R15为酰基等); 提供它们的盐,水合物或溶剂合物。 预期本发明的唾液酸衍生物是预防和治疗老年性痴呆(包括阿尔茨海默氏病等)的有效药物,因为它们增加胆碱能神经元中的ChAT活性。
-
-
-
-
-
-
-
-
-