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公开(公告)号:US06177454B1
公开(公告)日:2001-01-23
申请号:US09514637
申请日:2000-02-29
申请人: Tatsuya Maruyama , Kenichi Onda , Masahiko Hayakawa , Takumi Takahashi , Takayuki Suzuki , Tetsuo Matsui
发明人: Tatsuya Maruyama , Kenichi Onda , Masahiko Hayakawa , Takumi Takahashi , Takayuki Suzuki , Tetsuo Matsui
IPC分类号: A61K314184
CPC分类号: C07D233/64 , C07C217/16 , C07C271/16 , C07C271/20 , C07D235/16 , C07D249/12 , C07D277/30 , C07D277/40 , C07D277/42 , C07D285/12 , C07D471/04
摘要: An amide derivative represented by the following general formula (I) or a salt thereof and a pharmaceutical composition containing the amide derivative and a pharmaceutically acceptable vehicle. The symbols in the formula have the following meanings wherein A: heteroarylene; X: bond, O, S, —NR5—, —NR5CO—, —NR5CONH—, —NR5SO2— or —NR5C(═NH)NH—; R1: —H, -optionally substituted lower alkyl, -optionally substituted aryl, -optionally substituted heteroaryl or -optionally substituted cycloalkyl; R2a, R2b: —H or -lower alkyl, which may be the same or different; R3: —H or -lower alkyl; R4a, R4b: —H or —OH, which may be the same different, or R4a and R4b are taken together to form ═O or ═N—O—lower alkyl; and R5: —H or -lower alkyl.
摘要翻译: 由以下通式(I)表示的酰胺衍生物或其盐和含有酰胺衍生物和药学上可接受的载体的药物组合物。式中的符号具有以下含义:A:亚杂芳基; X:键,O,S, -NR5-,-NR5CO-,-NR5CONH-,-NR5SO2-或-NR5C(= NH)NH-; R1:-H,可选取代的低级烷基, - 取代的芳基, - 取代的杂芳基或 - 取代的环烷基 ; R 2a,R 2b:-H或 - 低级烷基,其可以相同或不同; R 3:-H或 - 低级烷基; R 4a,R 4b:-H或-OH,其可以相同,或者R 4a和R 4b 一起形成= O或= NO-低级烷基; 和R5:-H或 - 低级烷基。
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公开(公告)号:US6048884A
公开(公告)日:2000-04-11
申请号:US297762
申请日:1999-05-07
申请人: Tatsuya Maruyama , Kenichi Onda , Masahiko Hayakawa , Takumi Takahashi , Takayuki Suzuki , Tetsuo Matsui
发明人: Tatsuya Maruyama , Kenichi Onda , Masahiko Hayakawa , Takumi Takahashi , Takayuki Suzuki , Tetsuo Matsui
IPC分类号: A61K31/41 , A61K31/415 , A61K31/425 , A61P3/10 , A61P5/50 , C07C217/16 , C07C271/16 , C07C271/20 , C07D233/54 , C07D233/61 , C07D233/64 , C07D235/16 , C07D249/08 , C07D249/12 , C07D257/04 , C07D277/30 , C07D277/38 , C07D277/40 , C07D277/42 , C07D277/46 , C07D285/12 , C07D471/04 , A61K31/426 , A61K31/4436
CPC分类号: C07D233/64 , C07C217/16 , C07C271/16 , C07C271/20 , C07D235/16 , C07D249/12 , C07D277/30 , C07D277/40 , C07D277/42 , C07D285/12 , C07D471/04
摘要: An amide derivative represented by the following general formula (I) or a salt thereof and a pharmaceutical composition containing the amide derivative and a pharmaceutically acceptable vehicle. ##STR1## (The symbols in the formula have the following meanings. (whereinA: heteroarylene;X: bond, O, S, --NR.sup.5 --, --NR.sup.5 CO--, --NR.sup.5 CONH--, --NR.sup.5 SO.sub.2 -- or --NR.sup.5 C(.dbd.NH)NH--;R.sup.1 : --H, -optionally substituted lower alkyl, -optionally substituted aryl, -optionally substituted heteroaryl or -optionally substituted cycloalkyl;R.sup.2a, R.sup.2b : --H or -lower alkyl, which may be the same or different;R.sup.3 : --H or -lower alkyl;R.sup.4a, R.sup.4b : --H or --OH, which may be the same different, or R.sup.4a and R.sup.4b are taken together to form .dbd.O or .dbd.N.about.O-lower alkyl; andR.sup.5 : --H or -lower alkyl.)
摘要翻译: PCT No.PCT / JP98 / 00237 Sec。 371日期1999年5月7日 102(e)日期1999年5月7日PCT提交1998年1月22日PCT公布。 第WO98 / 32742号公报 日期:1998年7月30日由以下通式(I)表示的酰胺衍生物或其盐和含有酰胺衍生物和药学上可接受的载体的药物组合物。 (其中A:亚杂芳基; X:键,O,S,-NR5-,-NR5CO-,-NR5CONH-,-NR5SO2-或-NR5C(= NH)NH-; R 1:-H, - 取代的低级烷基, - 取代的芳基, - 被取代的杂芳基或 - 取代的环烷基; R 2a,R 2b:-H或 - 低级烷基,其可以相同或不同; R 3:-H或 - 低级烷基; R4a,R4b:-H或-OH,其可以相同,或者R4a和R4b一起形成= O或= N差异O-低级烷基;以及R5:-H或 - 低级烷基 。
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公开(公告)号:US06346532B1
公开(公告)日:2002-02-12
申请号:US09529096
申请日:2000-04-07
申请人: Tatsuya Maruyama , Takayuki Suzuki , Kenichi Onda , Masahiko Hayakawa , Hiroyuki Moritomo , Tetsuya Kimizuka , Tetsuo Matsui
发明人: Tatsuya Maruyama , Takayuki Suzuki , Kenichi Onda , Masahiko Hayakawa , Hiroyuki Moritomo , Tetsuya Kimizuka , Tetsuo Matsui
IPC分类号: A61K31495
CPC分类号: C07D231/12 , C07D213/30 , C07D213/56 , C07D213/81 , C07D215/48 , C07D233/26 , C07D235/16 , C07D235/30 , C07D239/26 , C07D241/12 , C07D257/04 , C07D277/36 , C07D277/82 , C07D401/04 , C07D513/04
摘要: Amide derivatives represented by general formula (I) or salts thereof wherein each symbol has the following meaning: ring B: an optionally substituted heteroaryl optionally fused with a benzene ring; X: a bond, lower alkylene or lower alkenylene optionally substituted by hydroxy or lower alkyl, carbonyl, or a group represented by —NH— (when X is lower alkylene optionally substituted by lower alkyl which may be bonded to the hydrogen atom bonded to a constituent carbon atom of ring B to form lower alkylene to thereby form a ring); A: a lower alkylene or a group represented by -(lower alkylene)—O—; R1a and R1b: the same or different and each hydrogen or lower alkyl; R2: hydrogen or halogeno; and Z: nitrogen or a group represented by ═CH—. The compounds are useful as a diabetes remedy which not only functions to both accelerate the secretion of insulin and enhance insulin sensitivity but has an antiobestic action and an antihyperlipemic action based on its selective stimulative action on a &bgr;3 receptor.
摘要翻译: 由通式(I)表示的酰胺衍生物或其盐,其中每个符号具有以下含义:环B:任选地与苯环稠合的任选取代的杂芳基; X:任选被羟基或低级烷基取代的低级亚烷基或低级亚烯基,羰基或由-NH-表示的基团(当X为任选被低级烷基取代的低级烷基时,该低级烷基可以键合到与 环B的构成碳原子形成低级亚烷基,从而形成环); A:低级亚烷基或由 - (低级亚烷基)-O-表示的基团。 R1a和R1b:相同或不同,各个氢或低级烷基; R2:氢或卤素; 和Z:氮或由= CH-表示的基团。 该化合物可用作糖尿病药物,其不仅可以加速胰岛素的分泌并增强胰岛素敏感性,而且具有基于其对β3受体的选择性刺激作用的抗胆碱作用和抗高脂血症作用。
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公开(公告)号:US5643931A
公开(公告)日:1997-07-01
申请号:US537907
申请日:1995-10-26
申请人: Kunihiro Niigata , Takumi Takahashi , Tatsuya Maruyama , Takayuki Suzuki , Kyoichi Maeno , Kenichi Onda , Toru Kontani , Osamu Noshiro , Reiko Koike , Akiyoshi Shimaya , Jun Irie
发明人: Kunihiro Niigata , Takumi Takahashi , Tatsuya Maruyama , Takayuki Suzuki , Kyoichi Maeno , Kenichi Onda , Toru Kontani , Osamu Noshiro , Reiko Koike , Akiyoshi Shimaya , Jun Irie
IPC分类号: C07D271/06 , A61K31/4166 , A61K31/44 , A61P3/10 , C07D271/07 , C07D413/14 , A61K31/41
CPC分类号: C07D271/07 , C07D413/14
摘要: A bisoxadiazolidine dione derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof, which is useful as an insulin sensitivity-increasing drug, and a pharmaceutical composition thereof. ##STR1## each represents a phenylene groupL:(1) an oxygen,(2) a ##STR2## (3) a --S(O).sub.n --, (4) a --CO--,(5) a ##STR3## (6) an alkylene group or an alkenylene group which may respectively be interrupted with an oxygen atom and/or a sulfur atom.
摘要翻译: PCT No.PCT / JP94 / 00696 Sec。 371 1995年10月26日第 102(e)日期1995年10月26日PCT 1994年4月26日PCT PCT。 公开号WO94 / 25448 日期:1994年11月10日由以下通式(I)表示的双恶唑烷二酮衍生物或其药学上可接受的盐,其可用作胰岛素敏感性增加药物及其药物组合物。 (I)
各自表示亚苯基L:(1)氧,(2)a(S)a -S(O)n - ,(4)-CO-,( (5)可以分别用氧原子和/或硫原子间隔的亚烷基或亚烯基。 -
公开(公告)号:US07982049B2
公开(公告)日:2011-07-19
申请号:US12007653
申请日:2008-01-14
申请人: Souichirou Kawazoe , Kenichirou Sakamoto , Yuji Awamura , Tatsuya Maruyama , Takayuki Suzuki , Kenichi Onda , Toshiyuki Takasu
发明人: Souichirou Kawazoe , Kenichirou Sakamoto , Yuji Awamura , Tatsuya Maruyama , Takayuki Suzuki , Kenichi Onda , Toshiyuki Takasu
IPC分类号: A61K31/426 , C07D277/40
CPC分类号: C07D277/40
摘要: To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with α-form crystal and β-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide. The α-form crystal does not exhibit hygroscopicity and has stability such that it can be used as a medicine, and is useful for mass synthesis in the industrial production. The β-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the α-form crystal.
摘要翻译: 提供可用作糖尿病药物生产成分的新型晶体。 本发明涉及(R)-2-(2-氨基噻唑-4-基)-4' - [2 - [(2-羟基-2-苯基乙基)氨基] 乙基]乙酰苯胺。 α型结晶不具有吸湿性,稳定性高,可用作药物,可用于工业生产中的大规模合成。 该晶体不相对显示吸湿性,也可用作α型晶体的生产中间体。
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公开(公告)号:US20080214633A1
公开(公告)日:2008-09-04
申请号:US12007653
申请日:2008-01-14
申请人: Souichirou Kawazoe , Kenichirou Sakamoto , Yuji Awamura , Tatsuya Maruyama , Takayuki Suzuki , Kenichi Onda , Toshiyuki Takasu
发明人: Souichirou Kawazoe , Kenichirou Sakamoto , Yuji Awamura , Tatsuya Maruyama , Takayuki Suzuki , Kenichi Onda , Toshiyuki Takasu
IPC分类号: A61K31/426 , A61P3/10
CPC分类号: C07D277/40
摘要: To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with α-form crystal and β-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetanilide. The α-form crystal does not exhibit hygroscopicity and has stability such that it can be used as a medicine, and is useful for mass synthesis in the industrial production. The β-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the α-form crystal.
摘要翻译: 提供可用作糖尿病药物生产成分的新型晶体。 本发明涉及(R)-2-(2-氨基噻唑-4-基)-4' - [2 - [(2-羟基-2-苯基乙基)氨基]乙基的α-晶型和β型晶体 ]乙酰苯胺。 α型晶体不具有吸湿性并且具有稳定性,使得其可以用作药物,并且可用于工业生产中的大量合成。 β型晶体不具有吸湿性,也可用作α型晶体的生产中间体。
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公开(公告)号:US07342117B2
公开(公告)日:2008-03-11
申请号:US10494018
申请日:2002-10-20
申请人: Souichirou Kawazoe , Kenichirou Sakamoto , Yuji Awamura , Tatsuya Maruyama , Takayuki Suzuki , Kenichi Onda , Toshiyuki Takasu
发明人: Souichirou Kawazoe , Kenichirou Sakamoto , Yuji Awamura , Tatsuya Maruyama , Takayuki Suzuki , Kenichi Onda , Toshiyuki Takasu
IPC分类号: C07D277/40
CPC分类号: C07D277/40
摘要: To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with α-form crystal and β-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenyleth-yl)amino]ethyl]acetanilide. The α-form crystal does not exhibit hygroscopicity and has stability such that it can be used as a medicine, and is useful for mass synthesis in the industrial production. The β-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the α-form crystal.
摘要翻译: 提供可用作糖尿病药物生产成分的新型晶体。 本发明涉及(R)-2-(2-氨基噻唑-4-基)-4' - [2 - [(2-羟基-2-苯基] - 基)氨基的α-晶型和β型晶体 乙基]乙酰苯胺。 α型晶体不具有吸湿性并且具有稳定性,使得其可以用作药物,并且可用于工业生产中的大量合成。 β型晶体不具有吸湿性,也可用作α型晶体的生产中间体。
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公开(公告)号:US20050004190A1
公开(公告)日:2005-01-06
申请号:US10494018
申请日:2002-10-20
申请人: Souichirou Kawazoe , Kenichirou Sakamoto , Yuji Awamura , Tatsuya Maruyama , Takayuki Suzuki , Kenichi Onda , Toshiyuki Takasu
发明人: Souichirou Kawazoe , Kenichirou Sakamoto , Yuji Awamura , Tatsuya Maruyama , Takayuki Suzuki , Kenichi Onda , Toshiyuki Takasu
IPC分类号: A61P3/10 , C07D277/40 , C07D277/44 , A61K31/426
CPC分类号: C07D277/40
摘要: To provide novel crystals useful as an ingredient for the production of a diabetes remedy. The invention is concerned with α-form crystal and β-form crystal of (R)-2-(2-aminothiazol-4-yl)-4′-[2-[(2-hydroxy-2-phenyleth-yl)amino]ethyl]acetanilide. The α-form crystal does not exhibit hygroscopicity and has stability such that it can be used as a medicine, and is useful for mass synthesis in the industrial production. The β-form crystal does not relatively exhibit hygroscopicity and is also useful as a production intermediate of the α-form crystal.
摘要翻译: 提供可用作糖尿病药物生产成分的新型晶体。 本发明涉及(R)-2-(2-氨基噻唑-4-基)-4' - [2 - [(2-羟基-2-苯基] - 基)氨基的α-晶型和β型晶体 乙基]乙酰苯胺。 α型晶体不具有吸湿性并且具有稳定性,使得其可以用作药物,并且可用于工业生产中的大量合成。 β型晶体不具有吸湿性,也可用作α型晶体的生产中间体。
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公开(公告)号:US20050176771A1
公开(公告)日:2005-08-11
申请号:US10492347
申请日:2003-07-18
申请人: Masahiko Hayakawa , Kenji Negoro , Satoshi Miyamoto , Takayuki Suzuki , Tatsuya Maruyama , Ryosuke Nakano
发明人: Masahiko Hayakawa , Kenji Negoro , Satoshi Miyamoto , Takayuki Suzuki , Tatsuya Maruyama , Ryosuke Nakano
IPC分类号: A61P3/10 , A61P43/00 , C07D207/16 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D451/04 , C07D471/06 , A61K31/454 , A61K31/416 , A61K31/422
CPC分类号: C07D401/12 , C07D207/16 , C07D401/14 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D451/04
摘要: Provided is a compound having excellent dipeptidyl peptidase IV-inhibiting activity, and a remedy based on the activity for insulin-dependent diabetes (type 1 diabetes), especially for non insulin-dependent diabetes (type 2 diabetes), insulin-resistant disorders, and obesity.
摘要翻译: 提供了具有优异的二肽基肽酶IV抑制活性的化合物,以及基于胰岛素依赖性糖尿病(1型糖尿病)的活性,特别是对于非胰岛素依赖性糖尿病(2型糖尿病),胰岛素抵抗障碍和 肥胖。
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公开(公告)号:US07268150B2
公开(公告)日:2007-09-11
申请号:US10492347
申请日:2003-07-18
申请人: Masahiko Hayakawa , Kenji Negoro , Satoshi Miyamoto , Takayuki Suzuki , Tatsuya Maruyama , Ryosuke Nakano
发明人: Masahiko Hayakawa , Kenji Negoro , Satoshi Miyamoto , Takayuki Suzuki , Tatsuya Maruyama , Ryosuke Nakano
IPC分类号: A61K31/445 , C07D207/16
CPC分类号: C07D401/12 , C07D207/16 , C07D401/14 , C07D403/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D451/04
摘要: Provided is a compound having excellent dipeptidyl peptidase IV-inhibiting activity, and a remedy based on the activity for insulin-dependent diabetes (type 1 diabetes), especially for non insulin-dependent diabetes (type 2 diabetes), insulin-resistant disorders, and obesity.
摘要翻译: 提供了具有优异的二肽基肽酶IV抑制活性的化合物,以及基于胰岛素依赖性糖尿病(1型糖尿病)的活性,特别是对于非胰岛素依赖性糖尿病(2型糖尿病),胰岛素抵抗障碍和 肥胖。
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