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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。
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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。
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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。
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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。
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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。
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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。
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公开(公告)号：US5506243A
公开(公告)日：1996-04-09
申请号：US233963
申请日：1994-04-28
IPC分类号： A61K31/195 , A61K31/198 , A61K31/44 , A61K31/4406 , A61P3/14 , A61P9/00 , A61P9/08 , A61P9/10 , A61P19/10 , A61P21/04 , A61P25/28 , A61P27/02 , A61P27/12 , A61P43/00 , C07C311/19 , C07D209/48 , C07D213/71 , C07D233/02 , C07D233/42 , C07D233/84 , C07D237/18 , C07D237/34 , C07D249/12 , C07D257/04 , C07D309/28 , C07D311/58 , C07D311/76 , C07D333/10 , C07D403/12 , C07D473/00 , C07D475/00 , C07K5/06 , C12N9/99 , A61K31/47 , A61K31/50 , A61K31/505 , C07D213/70
CPC分类号： C07K5/06043 , C07C311/19 , C07D213/71
摘要： Since sulfonamide derivatives of the present invention show strong inhibitory activity against cysteine protease such as calpain papain, cathepsin B, cathepsin H, cathepsin L, they can be used as remedies for muscular dystrophy, cataract, myocardial infarction, stroke, Alzheimer's disease, amyotrophia, osteoporosis, hypercalcemia or the like.
摘要翻译： 由于本发明的磺酰胺衍生物显示出对半胱氨酸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的强抑制活性，因此它们可用作肌营养不良症，白内障，心肌梗塞，中风，阿尔茨海默病，肌萎缩症， 骨质疏松症，高钙血症等。
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公开(公告)号：US20060211680A1
公开(公告)日：2006-09-21
申请号：US10572483
申请日：2004-09-16
IPC分类号： A61K31/55 , A61K31/4545 , A61K31/4439 , C07D401/02 , C07D403/02
CPC分类号： C07D213/69 , C07C47/55 , C07C235/84 , C07D211/74 , C07D215/22
摘要： The present invention relates to a cinnamoyl compound represented by the formula (I):
摘要翻译： 本发明涉及由式（I）表示的肉桂酰基化合物：
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公开(公告)号：US5807860A
公开(公告)日：1998-09-15
申请号：US748612
申请日：1996-11-13
申请人： Shinya Inoue , Masao Taniguchi , Yoshihiro Tarao , Kazuo Suzuki , Chizuko Takahashi , Mizue Kawai , Masayuki Mitsuka
发明人： Shinya Inoue , Masao Taniguchi , Yoshihiro Tarao , Kazuo Suzuki , Chizuko Takahashi , Mizue Kawai , Masayuki Mitsuka
IPC分类号： C07D207/32 , C07D207/325 , C07D213/30 , C07D295/092 , C07D521/00 , A61K31/495 , A61K31/53 , C07D241/02 , C07D403/02
CPC分类号： C07D207/325 , C07D213/30 , C07D231/12 , C07D233/56 , C07D249/08 , C07D295/088
摘要： A compound represented by formula (I) and a salt thereof, and a hydrate and solvate thereof: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 represent independently, for example, hydrogen atom, hydroxyl group, or C.sub.1-3 alkoxy group; R.sub.4 represents, for example, C.sub.1-7 alkyl group or C.sub.3-7 cycloalkyl group; R.sub.5 and R.sub.6 represent independently, for example, hydrogen atom or C.sub.1-3 alkyl group; Y represents C.sub.1-3 alkyl group, a heterocyclic group containing 1 to 4 nitrogen atoms and 5 or 6 ring-membered atoms, or C.sub.6-10 aryl group; k represents an integer of 1 to 3; and l represents an integer of 2 to 4. These urea compounds have excellent inhibitory activities against ACAT and are useful as active ingredients of medicines for preventive and/or therapeutic treatment of hyperlipemia and atherosclerosis.
摘要翻译： 由式（I）表示的化合物及其盐及其水合物和溶剂合物：其中R 1，R 2和R 3独立地表示例如氢原子，羟基或C 1-3烷氧基 ; R4表示例如C 1-7烷基或C 3-7环烷基; R5和R6独立地表示例如氢原子或C1-3烷基; Y表示C1-3烷基，含有1至4个氮原子和5或6个环原子的杂环基或C6-10芳基; k表示1〜3的整数， l表示2〜4的整数。这些脲化合物对ACAT具有优异的抑制活性，可用作预防和/或治疗高脂血症和动脉粥样硬化的药物的活性成分。
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公开(公告)号：US07691883B2
公开(公告)日：2010-04-06
申请号：US10572639
申请日：2004-09-16
IPC分类号： A61K31/44 , A61K31/366 , C07D309/38 , C07D405/12
CPC分类号： C07C47/55 , C07C235/16 , C07D309/26
摘要： The present invention relates to a cinnamoyl compound represented by the formula (I):
摘要翻译： 本发明涉及由式（I）表示的肉桂酰基化合物：
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