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51. 发明公开

EP0180745A1 Acylacetate and amidine intermediates for pyrimidone compounds, and their preparation 失效
标题翻译： Acylessigsäureesterund AmidinzwischenproduktefürPyrimidinonverbindungen und deren Herstellung。
公开(公告)号：EP0180745A1
公开(公告)日：1986-05-14
申请号：EP85111879.4
申请日：1983-02-11
申请人： YAMANOUCHI PHARMACEUTICAL CO. LTD.
发明人： Yanagisawa, Isao , Ohta, Mitsuaki , Takagi, Tokuichi
IPC分类号： C07C123/00 , C07C101/34 , C07C69/716 , C07C69/738 , C07D239/36 , C07D213/55 , C07D231/12 , C07D235/16 , C07D215/14 , C07D317/60 , C07D317/62
CPC分类号： C07D231/12 , C07D213/55 , C07D215/14 , C07D235/16 , C07D239/36 , C07D277/48 , C07D295/096 , C07D295/15 , C07D317/60 , C07D317/62 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/12 , C07D405/14 , C07D417/12 , C07D417/14
摘要： Compounds of formulae II and III below are useful as intermediates for the preparation of pyrimidones of formula I below which are gastric acid secretion inhibitors and have other medical utilitv:
wherein R, represents a hydrogen atom, an alkyl group, a lower alkenyl group, a lower alkinyl group, a phenyl group, a cycloalkylmethyl group, an unsubstituted or substituted aralkyl group, or the group
wherein A represents a lower alkylene group and R 3 and R. are the same or different lower alkyl groups or combine to form with the adjacent nitrogen atom a piperidine or pyrrolidine ring; R 2 represents a hydrogen atom, a lower alkyl group or a trifluoromethyl group; Y represents a heterocyclic group of the formula:
or
wherein R represents a hydrogen atom or a lower alkyl group; B represents an oxygen atom or a sulfur atom; m represents zero or an integer of 1 to 3; and n represents an integer of 1 to 3.
摘要翻译：以下式II和III的化合物可用作制备下式I嘧啶酮的中间体，其为胃酸分泌抑制剂，并具有其它医疗效用：其中R 1表示氢原子，烷基，低级烯基，低级炔基，苯基，环烷基甲基，未取代或取代的芳烷基或基团CHEM，其中A表示低级亚烷基，R3和R4是相同或不同的低级烷基或结合形成与相邻的氮原子一起是哌啶或吡咯烷环; R2表示氢原子，低级烷基或三氟甲基; Y表示下式的杂环基：其中R表示氢原子或低级烷基; B表示氧原子或硫原子; m表示0或1〜3的整数， n表示1〜3的整数。

52. 发明公开

EP0168025A1 Process for producing aminothiazolylpropendicarboxylic acid monoesters 有权转让
标题翻译：一种用于Aminothiazolylpropendicarbonsäure的单酯的制备方法。
公开(公告)号：EP0168025A1
公开(公告)日：1986-01-15
申请号：EP85108491.3
申请日：1985-07-09
申请人： SHIONOGI & CO., LTD.
发明人： Matsumura, Hiromu , Yano, Toshisada
IPC分类号： C07D277/38 , C07D277/40 , C07D277/42
CPC分类号： C07D277/20 , C07D277/40 , C07D277/42 , C07D277/46 , C07D277/48 , Y02P20/55
摘要： A useful intermediate for synthesizing antibacterials (i.e., 1-(2-protected amino-4-thiazolyl)propene-1,3-dicarboxylic acid half ester (VI)) is prepared by a process comprising 1) treating haloacetylmalonic acid ester (i) with thiourea to give 2-(2-amino-4-thiazolyl)malonic acid ester (II), 2) protecting the amino group of the latter to give 2-(2-protected amino-4-thiazolyl)malonic acid ester (III), 3) treating the product with haloalkenoic acid ester to give 1-(2-protected amino-4-thiazolyl)-2-propene-(1,1,3-tri or 1,1,3,3-tetra)carboxylic acid ester (IV), 4) hydrolyzing and decarboxylating the latter to give 1-(2-protected amino-4-thiazolyl)propene-1,3-dicarboxylic acid (V), and 5) treating the product with alcohol and a hemi-esterifying reagent to give the objective 1-(2- protected amino-4-thiazoly)propene-1,3-dicarboxylic acid half ester (VI).

53. 发明公开

EP0099121A3 Pharmaceutical compositions 有权
标题翻译：药物组合物
公开(公告)号：EP0099121A3
公开(公告)日：1985-07-03
申请号：EP83106846
申请日：1983-07-12
申请人： Bristol-Myers Company
发明人： Buyniski, Joseph P. , Cavanagh, Robert L. , Gordon, Maxwell
IPC分类号： A61K37/64 , A61K45/06 , A61K31/41
CPC分类号： C07D209/48 , A61K38/04 , C07D271/08 , C07D271/10 , C07D277/42 , C07D277/48 , C07D277/56 , C07D285/10 , C07D307/52 , C07D417/12 , C07D417/14 , C07D471/14 , A61K31/41 , A61K38/005 , A61K2300/00
摘要： Enhanced antiulcer activity is obtained in warm-blooded animals by the concomitant administration of the pepsin complexing agent, pepstatin, and an histamine H 2 -receptor antagonist of the formula
wherein A, m, Z, n, p and R 1 are as defined herein. Concomitant administration of the two entities reduces the amount of histamine H 2 -receptor antagonist necessary for treatment, thereby decreasing its side-effect liability.
摘要翻译：通过伴随施用胃蛋白酶络合剂，胃酶抑素和下式的组胺H2-受体拮抗剂，在温血动物中获得增强的抗溃疡活性，其中A，m，Z，n，p和R 1如本文所定义。两个实体的同时给药减少了治疗所需的组胺H2受体拮抗剂的量，从而降低了它的副作用。

54. 发明公开

EP0123024A3 7-Acylamino-3-vinylcephalosporanic acid derivatives, processes for their preparation, pharmaceutical compositions containing them; their starting compounds and their preparation 有权
标题翻译： 7-乙酰氨基-3-乙酰胆碱多糖衍生物，其制备方法，含有它们的药物组合物; 他们的起始化合物及其制备
公开(公告)号：EP0123024A3
公开(公告)日：1985-03-13
申请号：EP84100915
申请日：1980-11-15
申请人： FUJISAWA PHARMACEUTICAL CO., LTD.
发明人： Takaya, Takao , Takasugi, Hisashi , Masugi, Takashi , Yamanaka, Hideaki , Kawabata, Kohji
IPC分类号： C07D501/22 , C07D501/24 , A61K31/545 , C07D277/46 , C07D277/48 , C07D277/56 , C07D209/48 , C07D271/06 , C07D213/75 , C07D285/08 , C07D257/06 , C07D239/42
CPC分类号： C07D209/48 , C07D213/75 , C07D239/42 , C07D257/06 , C07D271/06 , C07D271/07 , C07D277/20 , C07D277/46 , C07D277/48 , C07D277/56 , C07D277/587 , C07D285/08 , C07D417/12
摘要： 7-Acylamino-3-vinylcephalosporanic acid derivatives of the formula:
in which R' is aminothiazolyl, aminothiadiazolyl, aminooxadiazolyl, aminopyridyl, aminopyrimidinyl, aminotetrazolyl. protected aminothiazolyl, protected aminothiadiazolyl, protected aminooxadiazolyl, protected aminopyridyl, protected aminotetrazolyl,.or
a group of the formula:
wherein R 3 IS C 1 -C 7 alkyl, R 2 is carboxy or a protected carboxy group, and A is methylene which may have certain substituents, processes for their preparation, pharmaceutically acceptable saits thereof, and also a pharmaceutically composition comprising, as an effective ingredient, the above compound in association with pharmaceutically acceptable carriers. The invention further relates to starting and intermediate compounds, which are useful for the preparation of the title compounds.

55. 发明公开

EP0100190A3 Fungicidal N-phenylcarbamate 有权转让
标题翻译：杀真菌N-苯甲酰胺
公开(公告)号：EP0100190A3
公开(公告)日：1985-02-06
申请号：EP83304163
申请日：1983-07-18
申请人： SUMITOMO CHEMICAL COMPANY, LIMITED
发明人： Noguchi, Hiroshi , Takahashi, Junya , Yamamoto, Shiego , Kato, Toshiro , Oguri, Yukio , Hirata, Naonori
IPC分类号： C07C125/065 , C07C155/02 , A01N47/20
CPC分类号： C07D213/40 , A01N47/20 , A01N53/00 , C07D263/56 , C07D277/48 , C07D307/52 , C07F7/10
摘要： Use of an N-phenylcarbamate of the formula:
as a fungicidal agent against phytophatogenic fungi, particularly their strains resistant to benzimidazole, thiophanate and or cyclic imide fungicides.

56. 发明公开

EP0099121A2 Pharmaceutical compositions 有权
标题翻译： Pharmazeutische Zusammensetzungen。
公开(公告)号：EP0099121A2
公开(公告)日：1984-01-25
申请号：EP83106846.5
申请日：1983-07-12
申请人： Bristol-Myers Company
发明人： Buyniski, Joseph P. , Cavanagh, Robert L. , Gordon, Maxwell
IPC分类号： A61K37/64 , A61K45/06
CPC分类号： C07D209/48 , A61K38/04 , C07D271/08 , C07D271/10 , C07D277/42 , C07D277/48 , C07D277/56 , C07D285/10 , C07D307/52 , C07D417/12 , C07D417/14 , C07D471/14 , A61K31/41 , A61K38/005 , A61K2300/00
摘要： Enhanced antiulcer activity is obtained in warm-blooded animals by the concomitant administration of the pepsin complexing agent, pepstatin, and an histamine H 2 -receptor antagonist of the formula
wherein A, m, Z, n, p and R 1 are as defined herein. Concomitant administration of the two entities reduces the amount of histamine H 2 -receptor antagonist necessary for treatment, thereby decreasing its side-effect liability.
摘要翻译：通过伴随施用胃蛋白酶络合剂，胃酶抑素和式CHEM的组胺H2受体拮抗剂（其中A，m，Z，n，p和R 1）可以在温血动物中获得增强的抗溃疡活性，如本文所定义。两个实体的同时给药减少了治疗所需的组胺H2受体拮抗剂的量，从而降低其副作用负担。

57. 发明公开

EP0095640A1 Alkylenverbrückte Guanidinothiazolderivate, Verfahren zu ihrer Herstellung sowie ihre Verwendung als Arzneimittel 有权
标题翻译：亚烷基Guanidinothiazolderivate，其制备方法以及它们作为药物的用途。
公开(公告)号：EP0095640A1
公开(公告)日：1983-12-07
申请号：EP83104793.1
申请日：1983-05-16
申请人： BAYER AG
发明人： Ippen, Joachim, Dr. , Perzborn, Elisabeth, Dr. , Puls, Walter, Dr. , Schaller, Klaus, Dr. , Seuter, Friedel, Dr.
IPC分类号： C07D417/12 , C07D417/14 , A61K31/425
CPC分类号： C07D417/12 , C07D239/16 , C07D277/48 , C07D417/14
摘要： Die vorliegende Erfindung betrifft neue alkylenverbrückte Guanidinothiazolderivate, ein Verfahren zu ihrer Herstellung sowie ihre Verwendung als Arzneimittel, insbesondere zur Beeinflussung des Fettstoffwechsels, als Antithrombotika sowie als Antimykotika.
摘要翻译：本发明涉及新的亚烷基Guanidinothiazolderivate，其制备方法以及它们作为药物的使用过程中，特别是用于影响脂质代谢，如抗血栓形成剂和作为抗真菌剂。

58. 发明公开

EP0087274A2 Pyrimidone derivatives 失效
标题翻译： Pyrimidonderivate。
公开(公告)号：EP0087274A2
公开(公告)日：1983-08-31
申请号：EP83300822.0
申请日：1983-02-17
申请人： SMITH KLINE & FRENCH LABORATORIES LIMITED
发明人： Brown, Thomas Henry
IPC分类号： C07D417/14 , C07D405/14 , C07D401/14 , C07D401/06 , A61K31/505 , A61K31/425
CPC分类号： C07D213/64 , C07D213/38 , C07D213/61 , C07D233/64 , C07D239/36 , C07D277/48 , C07D295/096 , C07D307/38 , C07D307/52 , C07D403/06 , C07D403/14 , C07D417/14
摘要： The invention provides histamine H 2 -antaponist compounds of formula (1):-
and pharmaceutically acceptable salts thereof, where

W is a 2-furanyl or 2-thienyl group optionally substituted in the 5-position with a group R 1 R 2 N(CH 2 ) a -; a 2-pyridyl group optionally substituted in the 4- or 6-position with a group R 1 R 2 N(CH 2 ) a -; a phenyl group substituted in the 3-or 4-position with a group R 1 R 2 N(CH 2 ) a -; a 4-imidazolyl group optionally substituted in the 5-position with methyl or bromine; a 2-pyridyl group optionally substituted in the 3-position with C 1-4 alkyl, C 1-4 , alkoxy, halogen, amino or hydroxy; a 2-thiazolyl group or a 2-guanidino-4-thiazolyl group;
X is (CH 2 ) b in which b is from 3 to 6, or (CH 2 ) d S(CH 2 ) e in which dand e are the same or different and are from 1 to 3 or, when W is substituted phenyl or 2-pyridyl substituted in the 4- or 6- position with a group R 1 R 2 N(CH 2 ) a -, O(CH 2 ) t in which f is from 2 to 5;
Z is hydrogen or C 1-4 alkyl;
A is C 1 -C 5 alkylene or (CH 2 ) p A 1 (CH 2 ) q - where A' is oxygen or sulphur and p and q are such that their sum is from 1 to 4;
B is an optionally substituted pyridyl, where the optional substituent is one or more C 1-4 alkyl, or C 1-4 alkoxy or hydroxy groups or halogen atoms or an N-oxo group or a phenyl group optionally substituted with one or more C 1-4 alkyl or C 1-4 alkoxy groups or halogen atoms or B is a 6-(2,3-dihydro-1,4-benzodioxinyl) or a 5-(1,3-benzodioxolyl) group or B is a 2-furanyl or 2-thienyl group optionally substituted in the 5-position with a group R 1 R 2 N(CH 2 ) a -; a phenyl group substituted in the 3- of 4-position with a group R 1 R 2 N(CH 2 ) a - or a 3-pyridyl group substituted in the 5- or 6-position or a 4-pyridyl group substituted in the 2-position by a group R 1 R 2 N(CH 2 ) a -;
R' and R 2 can be the same or different and are hydrogen or C 1-4 alkyl or together form a 1,4-butanediyl, 1,5-pentanediyl, 1,6-hexanediyl or 1,7-heptanediyl group; and a is 1 to 4.
摘要翻译：本发明提供了式（I）的组胺H2拮抗剂化合物：其... ...其药学上可接受的盐，其中W是在5-位上任选被一个R基团取代的2-呋喃基或2-噻吩基 <1> [R <2> N（CH 2）A-; 任选在4-或6-位被R 1 R 2 N（CH 2）a - 取代的2-吡啶基; 在3-或4-位被R 1 R 2 N（CH 2）a - 取代的苯基; 任选在5-位被甲基或溴取代的4-咪唑基; 任选在3-位被C 1-4烷基，C 1-4烷氧基，卤素，氨基或羟基取代的2-吡啶基; 2-噻唑基或2-胍基-4-噻唑基; X为（CH 2）b，其中b为3至6，或（CH 2）d S（CH 2）e，其中d和e为相同或不同且为1至3，或当W为4-或6-位取代的苯基或2-吡啶基时，R 1，R 2，N（CH 2）a - ，O（CH 2）其中f为2至5; Z为氢或C1-4烷基; A为C1-C5亚烷基或（CH2）pA 1（CH2）q-，其中A 1为氧或硫，p为和q是它们的总和为1至4; ... B是任选取代的吡啶基，其中任选的取代基是一个或多个C 1-4烷基。或C 1-4烷氧基或羟基或卤素原子或任选被一个或多个C 1-4烷基或C 1-4烷氧基或卤素原子取代的N-氧代基或苯基，或B是6-（2,3 - 二氢-1,4-苯并二恶英基）或5-（1,3-苯并多恶唑基）基团，或B是任选在5位被R 1 R 2取代的2-呋喃基或2-噻吩基 > N（CH 2）A-; 在3-位的4-位上被基团R 1，R 2，N（CH 2）a - 取代的苯基或在5-或6-位取代的3-吡啶基或4-吡啶基在2位被基团取代R 1 R 2 N（CH 2）a - ; ... R 1和R 2可以相同或不同，为氢或C 1-4烷基或一起形成1,4-丁二基，1,5-戊二基，1,6-己二基或1,7-庚二基; a是1到4。

59. 发明公开

EP0068033A1 N-(4-PHENYL-2-THIAZOLYL)CARBAMATE DERIVATIVES, PROCESS FOR THEIR PREPARATION, AND MEDICINAL COMPOSITION CONTAINING SAME 失效
标题翻译： N-（4-苯基-2-噻唑基）氨基甲酸酯衍生物及其制备方法和含有该组合物的药物组合物
公开(公告)号：EP0068033A1
公开(公告)日：1983-01-05
申请号：EP82900226.0
申请日：1982-01-08
申请人： MITSUI TOATSU KAGAKU KABUSHIKI KAISHA
发明人： SAKANO, Isao , YOKOYAMA, Tatsuro , KAJIYA, Seitaro , OKAZAKI, Yutaka , TOKUDA, Hiroshi , KAWAZURA, Hiroshi , KUMAKURA, Mikio , NAKANO, Takuo , AWAYA, Akira
IPC分类号： C07D277/48 , A61K31/425
CPC分类号： C07D277/48 , Y10S514/885
摘要： N-(4-Phenyl-2-thiazolyl)carbamate derivatives represented by the general formula (1):
(wherein R, represents a lower alkylthio group, a lower alkylsulfinyl group, a lower alkylsulfonyl group, a nitro group or an amino group, and R 2 represents a lower alkyl group or a halogenated lower alkyl group), a process for their preparation, and an immunity-controlling medicinal composition containing same, effective for chronic articular rheumatism, viral diseases, cancer, etc.
摘要翻译：（1）表示的N-（4-苯基-2-噻唑基）氨基甲酸酯衍生物：（式中，R 1表示低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，硝基或氨基， R2代表低级烷基或卤代低级烷基），其制备方法和含有它们的免疫控制药物组合物，对慢性关节风湿病，病毒性疾病，癌症等有效。

60. 发明公开

EP0049538A3 Use of thioureum derivatives as medicaments in the treatment of lipoid metabolism diseases 失效
标题翻译：作为治疗LIPOID代谢疾病的药物使用衍生物
公开(公告)号：EP0049538A3
公开(公告)日：1982-10-13
申请号：EP81109562
申请日：1980-07-02
申请人： BAYER AG
发明人： Kabbe, Hans-Joachim, Dr. , Klauke, Erich, Dr. , Krause, Hans Peter, Dr. , Mardin, Mithat, Dr. , Sitt, Rüdiger, Dr.
IPC分类号： A61K31/17 , A61K31/18 , A61K31/275 , A61K31/19 , A61K31/47
CPC分类号： C07D213/75 , A61K31/17 , C07C275/30 , C07D215/38 , C07D215/42 , C07D239/42 , C07D249/06 , C07D251/22 , C07D277/48 , C07D277/82 , C07D279/02 , C07D279/08 , C07D295/12 , C07D295/155 , C07D307/91 , C07D317/46
摘要： Die vorliegende Erfindung betrifft die Verwendung von Thioharnstoffderivaten der allgemeinen Formel I

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