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31. 发明公开

EP0923557A1 STEREOSELECTIVE DEOXYGENATION REACTION 失效
标题翻译：立体选择性脱氧反应
公开(公告)号：EP0923557A1
公开(公告)日：1999-06-23
申请号：EP97937187.0
申请日：1997-08-08
申请人： MERCK & CO., INC. , BANYU PHARMACEUTICAL CO., LTD.
发明人： DEVINE, Paul, N. , DOLLING, Ulf, H. , FREY, Lisa, F. , TILLYER, Richard, D. , TSCHAEN, David, M. , KATO, Yoshiaki
IPC分类号： C07D221 , A61K31 , A61P43 , C07D263 , C07D405 , C07D413
CPC分类号： C07D405/04
摘要： This invention relates to a key intermediate in the synthesis of an endothelin antagonist, the synthesis of this key intermediate and the synthesis of an endothelin antagonist using this intermediate in a stereoselective deoxygenation reaction.
摘要翻译：本发明涉及内皮素拮抗剂合成中的关键中间体，该关键中间体的合成以及使用该中间体在立体选择性脱氧反应中合成内皮素拮抗剂。

32. 发明公开

EP0882701A1 SUBSTITUTED AMIDE DERIVATIVES 失效
标题翻译：替代氨基酸
公开(公告)号：EP0882701A1
公开(公告)日：1998-12-09
申请号：EP97902606.9
申请日：1997-02-07
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： IWASAWA, Yoshikazu, Banyu Pharmaceutical Co. Ltd., , AOYAMA, Tetsuya, Banyu Pharmaceutical Co., Ltd., , KAWAKAMI, Kumiko, Banyu Pharmaceutical Co., Ltd., , ARAI, Sachie, Banyu Pharmaceutical Co., Ltd., , SATOH, Toshihiko, Banyu Pharmaceutical Co., Ltd., , MONDEN, Yoshiaki, Banyu Pharmaceutical Co., Ltd.,
IPC分类号： C07C233/01 , C07D307/68 , A61K31/27 , A61K31/34
CPC分类号： C07C233/01 , C07D307/68
摘要： Compounds represented by general formula (I), pharmacologically acceptable salts or esters thereof, and antitumor agents comprising
these as the active ingredients, wherein Ar 1 , Ar 2 , and Ar 3 each represents aryl or heteroaryl; A 1 represents C 1-6 hydrocarbyl or a group represented by -A 1a -W 1 -A 1b - (where W 1 represents oxygen, sulfur, ethynylene, cyclopropylene, or a group represented by -NR w -); A 2 represents C 1-8 hydrocarbyl group; R 1 represents lower alkyl, lower alkenyl, lower alkoxy, carboxy, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, a group represented by R a COO- (where R a represents hydrogen, amino, lower alkyl, lower alkoxy, or lower alkylamino) or by R b CONR c - (where R b represents hydrogen, amino, lower alkyl, lower alkoxy, or lower alkylamino), or an alicyclic group; R 2 represents lower alkyl; and X and Y each represents oxygen, sulfur, carbonyl, or a group represented by -CHR d - or -NR c -, or X and Y are bonded to each other to thereby form vinylene or ethynylene, provided that when one of X and Y represents oxygen, sulfur, or a group represented by -NR c -, then the other represents carbonyl or a group represented by -CHR d -.
摘要翻译：由通式（I）表示的化合物，其药理学上可接受的盐或酯，以及包含它们作为活性成分的抗肿瘤剂，其中Ar 1，Ar 2和Ar 3各自表示芳基或杂芳基; A 1表示C 1-6烃基或由-A 1 a -W 1 -A 1b表示的基团 - （其中W 1表示氧，硫，亚乙炔基，亚环丙基或由 -NR在 - ）; A 2表示C 1-8烃基; R 1表示低级烷基，低级烯基，低级烷氧基，羧基，低级烷氧基羰基，氨基甲酰基，低级烷基氨基甲酰基，由R aCOO-表示的基团（其中R a表示氢，氨基，低级烷基，低级烷氧基或低级烷基氨基）或通过R CONR c - （其中R b表示氢，氨基，低级烷基，低级烷氧基或低级烷基氨基）或脂环族基团; R 2表示低级烷基; 并且X和Y各自表示氧，硫，羰基或由-CHR d - 或-NR c表示的基团，或X和Y彼此键合，从而形成亚乙烯基或亚乙炔基，条件是当 X和Y中的一个表示氧，硫或-NR c表示的基团，则另一个表示羰基或由-CHR d - 表示的基团。

33. 发明公开

EP0863141A1 SUBSTITUTED HETEROAROMATIC DERIVATIVES 失效
标题翻译：替代异位异构体
公开(公告)号：EP0863141A1
公开(公告)日：1998-09-09
申请号：EP96932827.7
申请日：1996-10-07
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： MASE, Toshiaki, Banyu Pharmaceutical Co., Ltd. , MITSUYA, Morihiro, Banyu Pharmaceutical Co., Ltd. , KOBAYASHI, Kensuke, Banyu Pharmaceutical Co., Ltd. , NOGUCHI, Kazuhito, Banyu Pharmaceutical Co., Ltd.
IPC分类号： C07D401/06 , C07D405/06 , C07D409/06 , A61K31/445 , A61K31/47
CPC分类号： C07D401/06 , C07D405/06 , C07D409/06
摘要： This invention provides substituted heteroaromatic ring derivatives which are represented by a general formula [I] below:
[in the formula, R 1 and R 2 may be same or different and each signifies hydrogen, halogen or lower alkyl; R 3 signifies C 3 -C 6 cycloalkyl or cycloalkenyl; R 4 signifies a heteroaromatic ring group which may be condensed with a benzene ring and which has 1 or 2 hetero atoms selected from a group consisting of nitrogen, oxygen and sulfur atoms (said heteroaromatic ring group being optionally substituted with lower alkyl, halogen, lower alkoxy, amino or hydroxymethyl); and X stands for O or NH]
or their pharmaceutically acceptable salts.
The substituted heteroaromatic ring derivatives of the present invention have selective M 3 muscarinic receptor antagonist activity, and hence they are useful as therapeutic or prophylactic agents which are safe and efficacious with little side effects, of respiratory diseases such as asthma, chronic airway obstruction and pulmonary fibrosis, etc.; urinary diseases which induce such urination disorders as pollakiurea, urgency and urinary incontinence, etc.; and gastrointestinal diseases such as irritable bowel syndrome, spasm of gastrointestinal tract and gastrointestinal hyperkinesis.
摘要翻译：本发明提供了由下式通式表示的取代杂芳环衍生物：式中R 1和R 2可以相同或不同，表示氢，卤素或低级烷基; R 3表示C 3 -C 6环烷基或环烯基; R 4表示可以与苯环稠合并且具有1或2个选自氮，氧和硫原子的杂原子的杂芳环（所述杂芳环任选被低级烷基，卤素取代，低级烷氧基，氨基或羟甲基）; X代表O或NH或其药学上可接受的盐。本发明的取代杂芳环衍生物具有选择性M3毒蕈碱受体拮抗剂活性，因此它们可用作安全有效的副作用少，呼吸系统疾病如哮喘，慢性气道阻塞和肺纤维化的治疗或预防剂等等诱发排尿障碍的尿路疾病，尿潴留，尿失禁等; 胃肠道疾病如肠易激综合征，胃肠道痉挛和胃肠蠕动过多。

34. 发明授权

EP0528030B1 ANTITUMOR BE-13793C DERIVATIVE 失效
标题翻译：具有抗肿瘤效果-13793C衍生物
公开(公告)号：EP0528030B1
公开(公告)日：1997-09-17
申请号：EP91904336.4
申请日：1991-02-20
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： OKANISHI, Masanori, Banyu Pharmaceutical Co.,Ltd. , UEMURA, Daisuke, 1316-2, Ikeda , TANAKA, Seiichi, Banyu Pharmaceutical Co., Ltd. , KOJIRI, Katsuhisa, Banyu Pharmaceutical Co., Ltd. , OKURA, Akira, Banyu Pharmaceutical Co., Ltd. , FUNAISHI, Kohtaro, Banyu Pharmaceutical Co., Ltd. , SUDA, Hiroyuki, Banyu Pharmaceutical Co., Ltd.
IPC分类号： C07H19/23 , A61K31/70
CPC分类号： C07H19/044 , C07H19/23
摘要： A 12,13-dihydro-6H-indolo[2,3-a]pyrrolo[3,4-C]-carbazole-5,7(6H)-dione derivative of general formula (I), pharmaceutically acceptable salt thereof, production thereof, and uses thereof, wherein R1 represents a monosaccharide group with 5 to 7 carbon atoms, and the hydroxyl group(s) of the monosaccharide group may be substituted with one to three groups which may be the same or different from each other and are selected from among hydrogen, lower alkyl, lower alkylcarbonyloxy and lower alkoxy.

35. 发明公开

EP0769555A1 GENE CODING FOR GLYCOSYLTRANSFERASE AND USE THEREOF 失效
标题翻译： GLYCOSYLTRANSFERASE KODIERENDES GEN UND SEINE VERWENDUNG
公开(公告)号：EP0769555A1
公开(公告)日：1997-04-23
申请号：EP95920228.4
申请日：1995-05-31
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： KOJIRI, Katsuhisa Banyu Pharmaceutical Co., Ltd. , SUZUKI, Hajime Banyu Pharmaceutical Co., Ltd. , KONDO, Hisao Banyu Pharmaceutical Co., Ltd. , SUDA, Hiroyuki Banyu Pharmaceutical Co., Ltd.
IPC分类号： C12N15/56 , C12N9/24 , C07H19/23 , C12P19/60
CPC分类号： C12P19/28 , C12N9/1048 , C12P17/182
摘要： This invention relates to glycosyltransferase, genes encoding glycosyltransferase, recombinant vectors having such a gene, host cells transformed with such a recombinant vector, and uses thereof.
This invention makes it possible to glycosylate indolopyrrolocarbazole derivatives conveniently and economically.
摘要翻译：本发明涉及糖基转移酶，编码糖基转移酶的基因，具有这种基因的重组载体，用这种重组载体转化的宿主细胞及其应用。本发明使得可以方便和经济地对吲哚吡咯并咔唑衍生物进行糖基化。

36. 发明公开

EP0747381A1 CARBAPENEM DERIVATIVE 失效
标题翻译：碳青霉烯衍生物
公开(公告)号：EP0747381A1
公开(公告)日：1996-12-11
申请号：EP95909978.9
申请日：1995-02-24
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： NAKAGAWA, Susumu, Banyu Pharmaceutical Co., Ltd. , FUKATSU, Hiroshi, Banyu Pharmaceutical Co., Ltd. , USHIJIMA, Ryosuke, Banyu Pharmaceutical Co., Ltd.
IPC分类号： C07D477/00
CPC分类号： C07D477/20
摘要： A compound of the formula:
wherein R 1 is a hydrogen atom or a lower alkyl group, R 2 is a hydrogen atom or a negative charge, R 3 is a hydrogen atom or a lower alkyl group, Ar is a phenyl group, a naphthyl group or a group of:
(wherein each of A 4 and A 5 is a single bond, -NHSO 2 - or the like, and Het is a pyrrolinyl group, a 1,4-diazabicyclo[2.2.2]octanyl group or the like which may be substituted with a hydroxyl group, a carbamoyl lower alkyl group or the like) which may be substituted with a lower alkyl group, a lower alkylsulfamoyl group or the like which may be substituted with a hydroxyl group, a di-lower alkylsulfonyl group or the like; a hydroxyl group; a di-lower alkylsulfamoyl group or the like, each of A 1 , A 2 and A 3 is a single bond or a lower alkylene group which may be substituted with a lower alkyl group, a lower alkylsulfamoyl group or the like which may be substituted with a hydroxyl group, a di-lower alkylsulfamoyl group or the like; a pyridyl group or a pyridinio group or the like which may be substituted with a lower alkyl group, a carbamoyl lower alkyl group or the like, and W is a sulfur atom, a single bond or the like; or a pharmaceutically acceptable salt or ester thereof, a process for its production and an antibacterial agent containing it as an active ingredient.
摘要翻译：下式化合物：其中R 1为氢原子或低级烷基，R 2为氢原子或负电荷，R 3为氢原子或低级烷基中，Ar为苯基，萘基或下述基团：其中A4和A5各自为单键，-NHSO2-等，Het为吡咯啉基，1,4-二氮杂双环[ 可以被可被羟基取代的低级烷基，低级烷基氨磺酰基等取代的可以被羟基，氨基甲酰基低级烷基等取代的2-辛基或其类似物），二低级烷基磺酰基等; 羟基; 二低级烷基氨磺酰基等，A1，A2和A3各自为可以被羟基取代的低级烷基，低级烷基氨磺酰基等取代的单键或低级亚烷基基，二低级烷基氨磺酰基等; 可以被低级烷基，氨基甲酰基低级烷基等取代的吡啶基或吡啶基等，W是硫原子，单键等; 或其药学上可接受的盐或酯，其生产方法和含有它作为活性成分的抗菌剂。

37. 发明授权

EP0347840B1 Phosphinic acid derivates 失效
标题翻译： Phosphinsäure衍
公开(公告)号：EP0347840B1
公开(公告)日：1995-12-27
申请号：EP89111208.8
申请日：1989-06-20
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： Ishikawa, Kiyofumi , Fukami, Takehiro , Takezawa, Hiroshi , Nakamichi, Kyoko
IPC分类号： C07F9/30 , C07F9/32 , A61K31/66
CPC分类号： C07F9/65182 , C07F9/302 , C07F9/303 , C07F9/3217 , C07F9/3223 , C07F9/582 , C07F9/65062

38. 发明公开

EP0587430A1 Substituted acetamide derivatives for treatment of hypocholesterolaemia, hyperlipaemia and arteriosclerosis 失效
标题翻译：替代物乙酰胺衍生自身高胆固醇血症，高血压和动脉粥样硬化。
公开(公告)号：EP0587430A1
公开(公告)日：1994-03-16
申请号：EP93307115.1
申请日：1993-09-09
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： Iwasawa, Yoshikazu, c/o Tsukuba Research Lab. , Hattori, Hiromi, c/o Tsukuba Research Lab. , Nagata, Yasufumi, c/o Tsukuba Research Lab. , Shimizu, Akiko, c/o Tsukuba Research Lab. , Sawasaki, Yoshio, c/o Tsukuba Research Lab.
IPC分类号： C07C323/60 , C07C317/44 , C07D333/18 , C07D239/38 , C07D215/36 , C07D233/84 , C07D307/91
CPC分类号： C07D307/91 , C07C317/44 , C07C323/60 , C07D215/36 , C07D233/28 , C07D239/38 , C07D333/18 , Y10S514/824
摘要： There are provided substituted acetamide derivatives represented by general formula (I):

wherein R¹, R², R³, R⁴, R⁵, R⁶, R⁷, R⁸, R⁹, R¹⁰, R¹¹, R¹², R¹³, n and Z are defined in the specification. The substituted acetamide derivatives strongly inhibit acylcoenzyme A cholesterol acyltransferase (ACAT) and are expected to be effective for the treatment and prevention of hypercholesterolemia, hyperlipemia and arteriosclerosis.
摘要翻译：提供由通式（I）表示的取代的乙酰胺衍生物：其中R 1，R 2，R 3，R 4，R 5，R 6， R 7，R 8，R 9，R 1，O，R 1，R 1，R 1，R 3，在规范中。取代的乙酰胺衍生物强烈地抑制酰基辅酶A胆固醇酰基转移酶（ACAT），并且预期对于治疗和预防高胆固醇血症，高脂血症和动脉硬化是有效的。

39. 发明授权

EP0346465B1 1-CARBOXY-1-VYNILOXYIMINOAMINOTHIAZOLE CEPHALOSPORING DERIVATIVES AND PROCESS FOR THEIR PREPARATION 失效
标题翻译： 1-羧氧基-1-戊酰氧基氨基苯并噻唑类化合物衍生物及其制备方法
公开(公告)号：EP0346465B1
公开(公告)日：1993-08-11
申请号：EP87902727.4
申请日：1987-04-14
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： NAKAGAWA, Susumu , MITOMO, Ryuji , YAMADA, Koji , OTAKE, Norikazu , NAKANO, Fumio , ASAI, Akira , KUROYANAGI, Satoru , TANAKA, Yoshiharu , ISHIKAWA, Moriaki , USHIJIMA, Ryosuke
IPC分类号： C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36 , C07D501/46 , C07D277/40 , A61K31/545
CPC分类号： C07D263/58 , C07D235/28 , C07D263/46 , C07D271/113 , C07D277/36 , C07D277/56 , C07D277/587 , C07D285/125 , Y02P20/55
摘要： Compounds represented by general formula (I), [wherein R represents a hydrogen atom, a carboxyl protective group or an anionic charge, Q represents a hydrogen atom, a halogen atom, a hydroxy group, an acetoxy group, a carbamoyloxy group, an azido group, an optionally substituted quaternary ammonio group, or an optionally substituted 5- or 6-membered aromatic heterocyclic thio group containing at least one hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom, and a sulfur atom (additionally, the aromatic hetero ring being optionally bound to a benzene ring or a hetero cyclic ring)], nontoxic salts thereof or nontoxic esters thereof capable of being physiologically hydrolized, process for their preparation, and antibacterial agent containing the compound as an effective ingredient. Further, compounds represented by general formula (III), (wherein R3 represents a hydrogen atom or an amino protective group, and R4 and R5, which may be the same or different, each represents a hydrogen atom or a carboxyl protective group) or their salts and process for their preparation.

40. 发明公开

EP0453574A4 CEPHALOSPORIN DERIVATIVE 失效
标题翻译：头孢吡肟衍生物
公开(公告)号：EP0453574A4
公开(公告)日：1993-03-10
申请号：EP90916366
申请日：1990-11-13
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： NAKAGAWA, SUSUMU, BANYU PHARMACEUTICAL CO., LTD. , MITOMO, RYUJI , USHIJIMA, RYOSUKE, BANYU PHARMACEUTICAL CO., LTD. , ASAI, AKIRA , KUROYANAGI, SATORU, BANYU PHARMACEUTICAL CO., LTD.
IPC分类号： C07D501/00 , C07D501/36 , A61K31/545
CPC分类号： C07D501/00
摘要： A novel, optically active compound of formula (I) which is useful as a remedy for bacterial infection, a pharmaceutically acceptable salt or ester thereof, a crystal thereof, and production and uses thereof.
摘要翻译：用作细菌感染治疗药物的新型旋光化合物，其药学上可接受的盐或酯，其晶体及其生产和用途。

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