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1. 发明授权

US07557123B2 Heterocyclic compound and medicinal use thereof 失效
标题翻译：杂环化合物及其医药用途
公开(公告)号：US07557123B2
公开(公告)日：2009-07-07
申请号：US10478862
申请日：2002-05-27
申请人： Hiroshi Matsui , Hideo Kobayashi , Satoru Azukizawa , Masayasu Kasai , Akihisa Yoshimi , Hiroaki Shirahase
发明人： Hiroshi Matsui , Hideo Kobayashi , Satoru Azukizawa , Masayasu Kasai , Akihisa Yoshimi , Hiroaki Shirahase
IPC分类号： A61K31/47 , C07D217/02 , C07D401/02
CPC分类号： C07D413/12 , C07D217/26 , C07D417/12
摘要： The novel heterocyclic compound of the present invention is a novel heterocyclic compound having the formula (I) Y: R15—C(R14)═N—O— wherein R1 is H or C1-6 alkyl, R2 is H, —CO—C(R4)═C(R4)—R5 wherein R4 is H or C1-4 alkyl, and R5 is C4-8 alkyl, C2-8 alkenyl and the like, and the like, Y is the following group wherein X is O or S, R7 is the same as R4, R8 is R10—C(R9)═C(R9)— wherein R9 is the same as R4, R10 is C3-6 alkyl and the like, and the like, R14 is the same as R4, and R15 is aryl and the like, Y—(CH2)n-O— is bonded to the 6- or 7-position of the tetrahydroisoquinoline skeleton, and n is an integer of 1 to 4, or a pharmaceutically acceptable salt thereof. The compound (I) of the present invention is useful as a hypoglycemic agent, a hypolipidemic agent, an insulin resistance improver, a therapeutic agent of diabetes, a therapeutic agent of diabetic complications, a glucose tolerance improver, an anti-arteriosclerosis agent, an anti-obesity agent, an antiinflammatory agent, an agent for the prophylaxis or treatment of PPAR-mediated diseases or an agent for the prophylaxis or treatment of syndrome X.
摘要翻译：本发明的新型杂环化合物是具有式（I）Y：R 15 -C（R 14）-NO-的新型杂环化合物，其中R 1为H或C 1-6烷基，R 2为H，-CO-C（R 4 ）-C（R4）-R5，其中R4是H或C1-4烷基，R5是C4-8烷基，C2-8链烯基等，Y是下列基团，其中X是O或S， R 7与R 4相同，R 8是R 10 -C（R 9）-C（R 9） - ，其中R 9与R 4相同，R 10是C 3-6烷基等，R 14与R 4相同， R 15为芳基等，Y-（CH 2）n O-键合于四氢异喹啉骨架的6-位或7-位，n为1〜4的整数，或其药学上可接受的盐。本发明的化合物（I）可用作降血糖药，降血脂药，胰岛素抵抗改善剂，糖尿病治疗剂，糖尿病并发症治疗剂，葡萄糖耐量改善剂，抗动脉硬化药，抗肥胖剂，抗炎剂，预防或治疗PPAR介导的疾病的药物或用于预防或治疗综合征X的药剂。

2. 发明授权

US06342494B1 Carbapenem compounds, use thereof, and intermediate compounds of the same 失效
标题翻译：碳青霉烯化合物及其中间体化合物
公开(公告)号：US06342494B1
公开(公告)日：2002-01-29
申请号：US09355757
申请日：1999-08-04
申请人： Hiroshi Matsui , Masayasu Kasai
发明人： Hiroshi Matsui , Masayasu Kasai
IPC分类号： C07D47720
CPC分类号： C07D477/20 , A61K31/407 , Y02P20/55
摘要： A carbapenem compound of the formula (I) wherein R1 is a group hydrolyzable in the body, R2 is selected from the group consisting of aryl groups optionally substituted by 1-3 alkyl groups having 1-4 carbon atoms, 1-alkanoyloxyalkyl, 1-alkoxycarbonyloxyalkyl, phthalidyl and 5-methyl-2-oxo-1,3-dioxolen-4-ylmethyl, R3 and R4 are lower alkyl groups which may be the same or different or instead form a 4- to 6-membered cyclic amino with the adjacent nitrogen selected from the group consisting of azetidinyl, pyrrolidinyl and piperidinyl or a pharmaceutically acceptable salt thereof The carbapenem compound (I) and a pharmaceutically acceptable salt thereof of the present invention show superior absorption from digestive tract by oral administration, and sufficient antibacterial activity against a wide variety of bacterial species. Thus, they are extremely useful as agents for the prophylaxis and treatment of infectious diseases, particularly bacterial infectious diseases. Said agents for the prophylaxis and treatment of infectious diseases can be used as agents for the prophylaxis and treatment of the diseases caused by bacteria (e.g., suppurative diseases, respiratory infectious diseases, inflammatory diseases of biliary tract, urinary tract infection and the like) in warm-blooded animals inclusive of human (e.g., dog, cat, cow, horse, rat, mouse and the like).
摘要翻译：式（I）的碳青霉烯化合物，其中R 1是在体内可水解的基团，R 2选自任选被1-3个具有1-4个碳原子的烷基取代的芳基，1-烷酰氧基烷基，烷氧基羰基氧基烷基，邻苯二甲酰基和5-甲基-2-氧代-1,3-二氧杂环戊烯-4-基甲基，R 3和R 4是可以相同或不同的低级烷基，或者形成4-至6-元环状氨基，选自氮杂环丁烷基，吡咯烷基和哌啶基的相邻氮或其药学上可接受的盐本发明的碳青霉烯化合物（I）及其药学上可接受的盐通过口服给药对消化道具有优异的吸收性，并且具有足够的抗细菌活性各种细菌种类。因此，它们作为用于预防和治疗感染性疾病，特别是细菌感染性疾病的药剂是非常有用的。所述用于预防和治疗感染性疾病的药剂可用作预防和治疗由细菌引起的疾病（例如，化脓性疾病，呼吸道感染性疾病，胆道炎性疾病，尿路感染等）的药物包括人类（例如狗，猫，牛，马，老鼠，老鼠等）的温血动物。

3. 发明授权

US07429612B2 Indoline compound and medicinal use thereof 失效
标题翻译：二氢吲哚化合物及其药用
公开(公告)号：US07429612B2
公开(公告)日：2008-09-30
申请号：US10521175
申请日：2003-07-16
申请人： Shouji Kamiya , Miho Ikai , Kenji Takahash , Tadatsugu Tarumi , Masayasu Kasai , Akihisa Yoshimi , Hiroaki Shirahase
发明人： Shouji Kamiya , Miho Ikai , Kenji Takahash , Tadatsugu Tarumi , Masayasu Kasai , Akihisa Yoshimi , Hiroaki Shirahase
IPC分类号： A61K31/404 , C07D209/04
CPC分类号： C07D209/08 , A61K31/404 , C07D209/10 , C07D209/12 , C07D209/48
摘要： The present invention provides an indoline compound represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing this indoline compound or a pharmaceutically acceptable salt thereof. The compound of the present invention shows superior ACAT inhibitory effect and superior lipoperoxidation inhibitory effect and is useful as an ACAT inhibitor or a lipoperoxidation inhibitor.
摘要翻译：本发明提供由式（I）表示的二氢吲哚化合物，其中每个符号如说明书中所定义，或其药学上可接受的盐，以及含有该二氢吲哚化合物或其药学上可接受的盐的药物组合物。本发明的化合物显示优异的ACAT抑制作用和优异的脂过氧化抑制作用，可用作ACAT抑制剂或脂质过氧化抑制剂。

4. 发明申请

US20060128787A1 Novel indoline compound and medicinal use thereof 失效
标题翻译：新型二氢吲哚化合物及其医药用途
公开(公告)号：US20060128787A1
公开(公告)日：2006-06-15
申请号：US10521175
申请日：2003-07-16
申请人： Shouji Kamiya , Miho Ikai , Kenji Takahash , Tadatsugu Tarumi , Masayasu Kasai , Akihisa Yoshimi , Hiroaki Shirahase
发明人： Shouji Kamiya , Miho Ikai , Kenji Takahash , Tadatsugu Tarumi , Masayasu Kasai , Akihisa Yoshimi , Hiroaki Shirahase
IPC分类号： A61K31/405 , C07D209/14
CPC分类号： C07D209/08 , A61K31/404 , C07D209/10 , C07D209/12 , C07D209/48
摘要： The present invention provides an indoline compound represented by the formula (I) wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing this indoline compound or a pharmaceutically acceptable salt thereof. The compound of the present invention shows superior ACAT inhibitory effect and superior lipoperoxidation inhibitory effect and is useful as an ACAT inhibitor or a lipoperoxidation inhibitor.
摘要翻译：本发明提供由式（I）表示的二氢吲哚化合物，其中每个符号如说明书中所定义，或其药学上可接受的盐，以及含有该二氢吲哚化合物或其药学上可接受的盐的药物组合物。本发明的化合物表现出优异的ACAT抑制作用和优异的脂过氧化抑制作用，可用作ACAT抑制剂或脂质过氧化抑制剂。

5. 发明授权

US06589963B2 Heterocyclic compounds and salts thereof and medicinal use of the same 失效
标题翻译：杂环化合物及其盐及其药用
公开(公告)号：US06589963B2
公开(公告)日：2003-07-08
申请号：US10148386
申请日：2002-05-31
申请人： Hiroshi Matsui , Hideo Kobayashi , Satoru Azukizawa , Masayasu Kasai , Akihisa Yoshimi , Hiroaki Shirahase
发明人： Hiroshi Matsui , Hideo Kobayashi , Satoru Azukizawa , Masayasu Kasai , Akihisa Yoshimi , Hiroaki Shirahase
IPC分类号： C07D40112
CPC分类号： C07D217/22
摘要： A heterocyclic compound of the formula [I] wherein R1 is hydrogen atom or lower alkyl, R2 is hydrogen atom, alkyl optionally having a substituent and the like, R3 is hydrogen atom, lower alkyl and the like, A is a single bond or >N—R5 wherein R5 is hydrogen atom or lower alkyl, B is lower alkylene, and Y is aryl optionally having a substituent and the like, and a pharmaceutically acceptable salt thereof show a hypoglycemic action, a blood hypolipidemic action, an insulin resistance-improving action and a PPAR activating action, and are useful as a hypoglycemic agent, a hypolipidemic agent, an insulin resistance improver, a therapeutic agent of diabetes, a therapeutic agent of diabetic complication, a glucose tolerance improver, an anti-atherosclerosis agent, an anti-obesity agent, an antiinflammatory agent, an agent for the prophylaxis or treatment of PPAR-mediated disease and an agent for the prophylaxis or treatment of syndrome X.
摘要翻译：式[I]的杂环化合物，其中R 1为氢原子或低级烷基，R 2为氢原子，任选具有取代基的烷基等，R 3为氢原子，低级烷基等，A为单键或> N-R5其中R5为氢原子或低级烷基，B为低级亚烷基，Y为任选具有取代基的芳基等，其药学上可接受的盐呈低血糖作用，降血脂作用，胰岛素抵抗改善作用和PPAR活化作用，并且可用作降血糖药，降血脂药，胰岛素抵抗改善剂，糖尿病治疗剂，糖尿病并发症治疗剂，葡萄糖耐量改善剂，抗动脉粥样硬化剂，抗 - - 促肥剂，抗炎剂，预防或治疗PPAR介导的疾病的药剂和用于预防或治疗综合症的药剂。

6. 发明授权

US4943567A Cephalosporin compound and pharmaceutical composition thereof 失效
标题翻译：头孢菌素化合物及其药物组合物
公开(公告)号：US4943567A
公开(公告)日：1990-07-24
申请号：US228714
申请日：1988-05-27
申请人： Susumu Nishizawa , Hiroyuki Muro , Masayasu Kasai , Satoru Hatano , Syouzi Kamiya , Nobuharu Kakeya , Kazuhiko Kitao
发明人： Susumu Nishizawa , Hiroyuki Muro , Masayasu Kasai , Satoru Hatano , Syouzi Kamiya , Nobuharu Kakeya , Kazuhiko Kitao
IPC分类号： C07D277/20 , C07D277/38 , C07D285/08 , C07D501/20 , C07D501/34 , C07D501/36
CPC分类号： C07D277/587 , C07D285/08 , Y02P20/55
摘要： Cephalosporin compounds represented by the general formula (I): ##STR1## wherein R.sup.1 and R.sup.5 independently represent a hydrogen atom or a protective group for an amino group; R.sup.2 represents an alkyl group or a cycloalkyl group; R.sup.3 represents a hydrogen atom, a lower alkenyl group, an alkanoyloxymethyl group, a carbamoyloxymethyl group, a heterocyclic thiomethyl group or a heterocyclic methyl group; R.sup.4 represents a hydrogen atom or an ester residue; and X represents CH or a nitrogen atom and pharmacologically acceptable addition salts thereof, intermediate compounds used in the synthesis process of these compounds, production methods of these compounds and pharmaceutical compositions containing these compounds.Said compounds or addition salts thereof exhibit noticeable antibacterial activities even on Pseudomonas aeruginosa, on which known cephalosporin compounds do not exhibit antibacterial activities, and moreover, work well against ordinary Gram-positive bacteria and Gram-negative bacteria.

7. 发明申请

US20100022582A1 Tetrahydroisoquinoline Compound and Medicinal Use Thereof 审中-公开
标题翻译：四氢异喹啉化合物及其药物用途
公开(公告)号：US20100022582A1
公开(公告)日：2010-01-28
申请号：US11885965
申请日：2006-03-10
申请人： Kenji Takahashi , Hiroaki Shirahase , Kazuyoshi Kunishiro , Masayasu Kasai
发明人： Kenji Takahashi , Hiroaki Shirahase , Kazuyoshi Kunishiro , Masayasu Kasai
IPC分类号： A61K31/472 , C07D217/16 , A61P29/00 , A61P9/10 , A61P3/06
CPC分类号： C07D401/12 , C07D217/26 , C07D401/06
摘要： The present invention provide a tetrahydroisoquinoline compound having a superior ACAT-inhibitory activity and/or anti-oxidation action, particularly, novel compound represented by the formula (I) (wherein each symbol is as described in the specification) and a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有优异的ACAT抑制活性和/或抗氧化作用的四氢异喹啉化合物，特别是由式（I）表示的新化合物（其中各符号如说明书所述）及其药学上可接受的盐。

8. 发明授权

US06872732B2 Heterocyclic derivatives and medicinal use thereof 失效
标题翻译：杂环衍生物及其医药用途
公开(公告)号：US06872732B2
公开(公告)日：2005-03-29
申请号：US10478863
申请日：2002-05-27
申请人： Hiroshi Matsui , Hideo Kobayashi , Satoru Azukizawa , Masayasu Kasai , Akihisa Yoshimi , Hiroaki Shirahase
发明人： Hiroshi Matsui , Hideo Kobayashi , Satoru Azukizawa , Masayasu Kasai , Akihisa Yoshimi , Hiroaki Shirahase
IPC分类号： A61P3/04 , A61P3/06 , A61P3/10 , A61P9/10 , A61P9/12 , A61P29/00 , A61P43/00 , C07D413/12 , C07D413/14 , C07D417/12 , A61K31/47 , C07D401/12
CPC分类号： C07D413/12 , C07D413/14 , C07D417/12
摘要： The novel heterocyclic derivative of the present invention is a novel heterocyclic derivative having the formula (I′) wherein R1 is a hydrogen atom or C1-6 alkyl, R2 is —CO—C(R4)═C(R4)—R5 wherein R4 is a hydrogen atom or C1-4 alkyl, and R5 is C4-8 alkyl, C2-8 alkenyl, aryl or aromatic heterocycle, —CO—C≡C—R6 wherein R6 is C1-8 alkyl and the like, R3 is a hydrogen atom or C1-4 alkyl, X is an oxygen atom or a sulfur atom, R20 is optionally substituted phenyl, and n is an integer of 1 to 4, or a pharmaceutically acceptable salt thereof. The compound (I′) of the present invention is useful as a hypoglycemic agent, a hypolipidemic agent, an insulin resistance improver, a therapeutic agent of diabetes, a therapeutic agent of diabetic complications, a glucose tolerance improver, an anti-arteriosclerosis agent, an anti-obesity agent, an antiinflammatory agent, an agent for the prophylaxis or treatment of PPAR-mediated diseases and an agent for the prophylaxis or treatment of syndrome X.
摘要翻译：本发明的新型杂环衍生物是具有式（I'）的新型杂环衍生物，其中R 1是氢原子或C 1-6烷基，R 2是-CO-C（R 4） = C（R 4）-R 5其中R 4是氢原子或C 1-4烷基，R 5是C 4-8烷基，C 2-8烯基，芳基或芳族杂环， CO-C = CR 6其中R 6为C 1-8烷基等，R 3为氢原子或C 1-4烷基，X为氧原子或硫原子，R 20为氢原子，为任选取代的苯基，n为1〜4的整数，或其药学上可接受的盐。本发明的化合物（I'）可用作降血糖剂，降血脂药，胰岛素抵抗改善剂，糖尿病治疗剂，糖尿病并发症治疗剂，葡萄糖耐量改善剂，抗动脉硬化剂，抗肥胖剂，抗炎剂，预防或治疗PPAR介导的疾病的药剂和用于预防或治疗症状X的药剂。

9. 发明授权

US5389625A Cephalosporin compounds 失效
标题翻译：头孢菌素化合物
公开(公告)号：US5389625A
公开(公告)日：1995-02-14
申请号：US849019
申请日：1992-06-08
申请人： Hiroyuki Muro , Masayasu Kasai , Satoru Hatano , Ken-ichi Nishimura , Susumu Nishizawa , Nobuharu Kakeya
发明人： Hiroyuki Muro , Masayasu Kasai , Satoru Hatano , Ken-ichi Nishimura , Susumu Nishizawa , Nobuharu Kakeya
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/20 , C07D501/22
CPC分类号： C07D501/00 , Y02P20/55
摘要： Cephalosporin compounds of the formula (I) ##STR1## wherein R.sup.1 is hydrogen atom or lower alkyl, and R.sup.2 is 1-alkanoyloxyalkyl or 1-alkoxycarbonyloxyalkyl, their pharmaceutically acceptable salts, methods for producing them, and pharmaceutical use thereof.The cephalosporin compounds and their salts are superior in absorption from digestive tract, and upon absorption from the digestive tract, show a wide range of antimicrobial activities in the body as hydrolysis products, and in addition, they have 10-400 times greater sweetness than sucrose. Thus, said compounds are useful as agents to be administered orally for the prophylaxis and treatment of bacterial infectious diseases.
摘要翻译： PCT No.PCT / JP90 / 01370 Sec。 371日期：1992年6月8日 102（e）日期1992年6月8日PCT 1990年10月24日PCT PCT。出版物WO91 / 06549 日本1991年5月16日。式（I）r烷基和R 2的头孢菌素化合物是1-烷酰氧基烷基或1-烷氧基羰氧基烷基，其药学上可接受的盐，其制备方法及其药物用途。头孢菌素化合物及其盐在消化道吸收方面优越，并且在消化道吸收时，作为水解产物在体内表现出广泛的抗微生物活性，此外，它们的甜度比蔗糖高10-400倍。因此，所述化合物可用作口服给药以预防和治疗细菌感染性疾病的药剂。

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