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51. 发明公开

EP0103390A2 Guanidine-containing esters as histamine H2 receptor blockers 失效
标题翻译： Guanidin enthaltende Ester mit Histamin-H-2-Empfängerblockierender Wirkung。
公开(公告)号：EP0103390A2
公开(公告)日：1984-03-21
申请号：EP83304506.5
申请日：1983-08-04
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC
发明人： Wardleworth, James Michael
IPC分类号： A61K31/425 , A61K31/41 , A61K31/415 , A61K31/505
CPC分类号： C07D231/38 , A61K31/41 , A61K31/415 , A61K31/425 , A61K31/505 , C07D231/16 , C07D231/40 , C07D239/47 , C07D249/06 , C07D277/48
摘要： Pharmaceutical compositions of ester intermediates of the formula I:
described in European Patent Publication 60094. The compositions have histamine H-2 receptor blocking activity.
摘要翻译：欧洲专利公开60094中描述的式I的酯中间体的药物组合物：。组合物具有组胺H-2受体阻断活性。

52. 发明授权

EP0010418B1 Antisecretory guanidine derivatives, processes for their manufacture and pharmaceutical compositions containing them 失效
标题翻译：抗菌药物衍生物及其制备方法及含有它们的药物组合物
公开(公告)号：EP0010418B1
公开(公告)日：1984-03-07
申请号：EP79302210.4
申请日：1979-10-15
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC , ICI AMERICAS INC.
发明人： Yellin, Tobias Oregon , Gilman, David John
IPC分类号： C07D277/48 , C07D417/12 , A61K31/34 , A61K31/425 , A61K31/44
CPC分类号： C07D271/07 , C07D233/88 , C07D263/48 , C07D277/48 , C07D285/08

53. 发明公开

EP0100190A2 Fungicidal N-phenylcarbamate 失效
标题翻译： N-苯基氨基甲酸乙酯mit fungizider Wirkung。
公开(公告)号：EP0100190A2
公开(公告)日：1984-02-08
申请号：EP83304163.5
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.
摘要翻译：使用下式的N-苯基氨基甲酸酯作为杀真菌剂，特别是其对苯并咪唑，甲基托布津和/或环状酰亚胺杀真菌剂有抗性的菌株。

54. 发明公开

EP0086647A3 Pyrimidone compounds, their preparation, and pharmaceutical compositions containing them 失效
标题翻译： PYRIMIDONE化合物，其制备和含有它们的药物组合物
公开(公告)号：EP0086647A3
公开(公告)日：1983-11-30
申请号：EP83300710
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： C07D239/36 , C07D405/12 , C07D417/12 , A61K31/505 , C07D417/14 , C07C123/00 , C07C69/716 , C07C69/738
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： Novel pyrimidones of the formula I and salts thereof are gastric acid secretion inhibitors and some have other medical utility:
wherein R 1 represents a hydrogen atom, a C 1 to C 10 alkyl group, a C 1 to C 5 alkenyl group, a C 1 to C 5 alkinyl group, a phenyl group, a cycloalkylmethyl group, an unsubstituted or R 3 substituted aralkyl group, or the group -A-N wherein A R 4 represents a C 1 to C 5 alkylene group and R 3 and R 4 are the same or different C 1 to C 5 alkyl groups or combine to form with the adjacent nitrogen atom a piperidine or pyrrolidine ring; R 2 represents a hydrogen atom, a C 1 to C 5 alkyl group or a trifluoromethyl group; Y represents a heterocyclic group of the formula:
or
wherein R represents a hydrogen atom or a C 1 to C 5 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. Methods and novel intermediates for their preparation are disclosed, as well as medicaments containing them and medical treatments using them.

55. 发明公开

EP0086647A2 Pyrimidone compounds, their preparation, and pharmaceutical compositions containing them 失效
标题翻译： Pyrimidin-Verbindungen，ihre Herstellung und diese enthaltende pharmazeutische Zusammenstellungen。
公开(公告)号：EP0086647A2
公开(公告)日：1983-08-24
申请号：EP83300710.7
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： C07D239/36 , C07D405/12 , C07D417/12 , A61K31/505 , C07D417/14 , C07C123/00 , C07C69/716 , C07C69/738
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： Novel pyrimidones of the formula I and salts thereof are gastric acid secretion inhibitors and some have other medical utility:
wherein R 1 represents a hydrogen atom, a C 1 to C 10 alkyl group, a C 1 to C 5 alkenyl group, a C 1 to C 5 alkinyl group, a phenyl group, a cycloalkylmethyl group, an unsubstituted or R 3 substituted aralkyl group, or the group -A-N wherein A R 4 represents a C 1 to C 5 alkylene group and R 3 and R 4 are the same or different C 1 to C 5 alkyl groups or combine to form with the adjacent nitrogen atom a piperidine or pyrrolidine ring; R 2 represents a hydrogen atom, a C 1 to C 5 alkyl group or a trifluoromethyl group; Y represents a heterocyclic group of the formula:

or
wherein R represents a hydrogen atom or a C 1 to C 5 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. Methods and novel intermediates for their preparation are disclosed, as well as medicaments containing them and medical treatments using them.
摘要翻译：式I的新型嘧啶酮及其盐是胃酸分泌抑制剂，一些具有其它医疗效用：其中R 1表示氢原子，C 1至C 10烷基，C 1至C 5链烯基，C 1至C 5炔基基团，苯基，环烷基甲基，未取代或取代的芳烷基或基团其中A表示C1至C5亚烷基，R3和R4是相同或不同的C1至C5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，C1〜C5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C1至C5烷基：B表示氧原子或硫原子; m表示0或1〜3的整数，并且n表示1〜3的整数。公开了其制备方法和新型中间体，以及含有它们的药物和使用它们的医疗处理。

56. 发明公开

EP0067436A2 Diamino isothiazole -1-oxides and -1,1-dioxides as gastric secretion inhibitors 失效
标题翻译：二氨基噻唑-1-氧化物和-1,1-二氧杂环己烷抑制剂。
公开(公告)号：EP0067436A2
公开(公告)日：1982-12-22
申请号：EP82105169.5
申请日：1982-06-14
申请人： Merck & Co., Inc.
发明人： Britcher, Susan F. , Lumma, William C., Jr. , Habecker, Charles N. , Baldwin, John J. , Hoffman, Jacob M.
IPC分类号： C07D275/02 , C07D417/12 , A61K31/425
CPC分类号： C07D275/03 , C07C255/00 , C07D277/48 , C07F7/10 , C07F7/1896
摘要： Novel diamino isothiazote-1-oxides and -1,1-dioxides having the formulae:
and
are disclosed wherein:

R is e.g. hydrogen, loweralkyl;
p is 1 or 2;
n is 0 or 1;
m is 2 to 4;
X is oxygen, sulfur or methylene;
R 2 is e.g. hydrogen, halogen or loweralkyl;
R 3 and R 4 are e.g. independently hydrogen or loweralkyl; and
Ⓐ is phenylene or a 5- or 6-membered heterocycle containing one to three heteroatoms selected from oxygen, sulfur or nitrogen, which may optionally have a benzo ring fused thereon; and, a substituted 5-membered heterocycle wherein the substituents are loweralkyl, loweralkoxy, carbonyl, halo, carbamoyl, substituted carbamoyl;

provided that when Ⓐ in Formulae la and Ib above is a 5-membered heterocycle, or a benzo fused 5-membered heterocycle containing one heteroatom, n is 1; and, the physiologically acceptable salts and N-oxides thereof. Processes for preparing such compounds are also disclosed. The compounds are useful for suppressing gastric acid secretions in mammals.
摘要翻译：公开了具有下式的新型二氨基异噻唑-1-氧化物和-1,1-二氧化物：其中：R为例如氢，低级烷基; p为1或2; n为0或1; m为2〜4; X是氧，硫或亚甲基; R 2是例如。氢，卤素或低级烷基; R 3和R 4是例如。独立地是氢或低级烷基; 并且芳基是亚苯基或含有一至三个选自氧，硫或氮的杂原子的5-或6-元杂环，其可任选地具有稠合在其上的苯并环; 和取代的5元杂环，其中取代基是低级烷基，低级烷氧基，羰基，卤素，氨基甲酰基，取代的氨基甲酰基; 条件是当上述式Ⅰa和Ib为5元杂环或含有一个杂原子的苯并稠合的5元杂环时，n为1; 及其生理上可接受的盐和N-氧化物。还公开了制备这些化合物的方法。该化合物可用于抑制哺乳动物中的胃酸分泌。

57. 发明公开

EP0061318A2 Guanidinoheterocyclic derivatives as histamine H-2 antagonists 失效
标题翻译：拮抗剂Guanidinoheterocyclische衍生物作为组胺H-2。
公开(公告)号：EP0061318A2
公开(公告)日：1982-09-29
申请号：EP82301420.4
申请日：1982-03-19
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC
发明人： Large, Michael Stewart
IPC分类号： C07D239/46 , C07D239/42 , C07D239/48 , C07D213/76 , C07D231/40 , C07D249/04 , C07D249/06 , C07D249/14 , C07D241/20 , C07D277/48 , A61K31/395
CPC分类号： C07D213/76 , C07D231/40 , C07D239/42 , C07D239/47 , C07D239/48 , C07D241/20 , C07D249/04 , C07D249/06 , C07D249/14 , C07D277/48
摘要： This invention relates to alcohol derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I:-
in which R 1 and R 2 , same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R 1 and R 2 is halogen-substituted, or R 2 is hydrogen and R 1 is R S- E-W- in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyl, E is 0, S, SO, S0 2 or NR 6 in which R 6 is H or 1-6C alkyl, R 5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R 5 and R 6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R 2 is hydrogen and R 1 is hydrogen or 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C aralkyl or 7-11C aroyl, the aryl, arylalkyl and aroyl radicals being optionally substituted; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene or a 1-8C alkylene into which is optionally inserted one or two groups; D is oxygen or sulphur; R 3 , R 4 and R 5 are hydrogen or a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.

58. 发明授权

EP0004956B1 Beta-Lactamantibiotika, Verfahren zu ihrer Herstellung, Futterzusatzmittel, Arzneimittel sowie Verfahren zu deren Herstellung 失效
标题翻译： BETA-LACTAM抗生素，其制备方法，FODDER添加剂，药物及其制备方法
公开(公告)号：EP0004956B1
公开(公告)日：1981-10-14
申请号：EP79101153.9
申请日：1979-04-17
申请人： BAYER AG
发明人： König, Hans-Bodo, Dr. , Metzger, Karl Georg, Dr. , Preiss, Michael, Dr.
IPC分类号： C07D501/20 , C07D499/64 , A61K31/545 , A61K31/43 , A23K1/17
CPC分类号： C07D277/20 , C07D233/38 , C07D277/48 , C07D499/00

59. 发明公开

EP0032058A1 Thiazole derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same 失效
标题翻译：噻唑衍生物，它们的制备方法和含有它们的药物组合物。
公开(公告)号：EP0032058A1
公开(公告)日：1981-07-15
申请号：EP80304740.6
申请日：1980-12-29
申请人： FUJISAWA PHARMACEUTICAL CO., LTD.
发明人： Ueda, Ikuo , Morino, Daizou , Takimoto, Koichi Daiichishinkitano Corp.
IPC分类号： C07D277/22 , C07D277/40 , C07D277/42 , C07D277/46 , C07D417/06 , C07D417/12 , A61K31/425 , A61K31/495 , A61K31/55
CPC分类号： C07D277/22 , C07C45/00 , C07D277/28 , C07D277/40 , C07D277/42 , C07D277/46 , C07D277/48 , C07D277/50 , C07C49/16
摘要： The thiazole derivatives have the general formula:-
wherein R 1 is hydrogen, amino, or mono-or di-substituted amino, in which the substituent is selected from lower alkyl, acyl and di (lower) alkylaminomethylene,

R 2 is hydrogen, halogen, lower alkyl or aryl,
R 3 is ar(lower)alkyl optionally substituted by halogen,
A is lower alkylene optionally interrupted by a sulfur atom, and
Y is C 1 -C 3 alkylene, and their pharmaceutically - acceptable
salts, are useful as antiallergic agents.
摘要翻译：的噻唑衍生物具有以下通式： - ... ... worin - [R <1>是氢，氨基，或其中取代基选自低级烷基，酰基和二选择的单 - 或二 - substituiertem氨基，alkylaminomethylene（低级） ... [R <2>是氢，卤素，低级烷基或芳基，... - [R <3>是芳（低级）烷基，其任选被卤素substituiertem，... A是任选的硫原子中断的低级亚烷基，和Y为C 1 ... C3亚烷基，和它们的药学上 - 可接受的盐，可用作抗过敏剂有用。

60. 发明公开

EP0016296A1 Cephalosporinderivate, Verfahren zu ihrer Herstellung, diese enthaltende Präparate und Zwischenprodukte sowie deren Herstellung 失效
标题翻译：头孢菌素衍生物，它们的制备，制剂和中间体以及它们的制备方法。
公开(公告)号：EP0016296A1
公开(公告)日：1980-10-01
申请号：EP79810157.2
申请日：1979-11-19
申请人： CIBA-GEIGY AG
发明人： Wiederkehr, René, Dr. , Scartazzini, Riccardo, Dr.
IPC分类号： C07D501/20 , A61K31/545 , C07D277/48
CPC分类号： C07D277/20 , C07D277/48 , C07D501/00
摘要： Die Erfindung betrifft Aminothiazolacetamido-3-cephem-4-carbonsäureverbindungen der Formel
worin der Index n eine ganze Zahl von 1 bis 4, X Sauerstoff, Schwefel, die Gruppe -NH-, oder die direkte Bindung, Y Sauerstoff oder Schwefel, A Methylen oder durch Amino, Hydroxy, Carboxyl, Sulfo, Oxo, oder die Gruppe =N-O-R". worin R"Wasserstoff oder gegebenenfalls substituiertes Niederalkyl darstellt, substituiertes Methylen, R, Wasserstoff. Niederalkyl, eine veresterte oder verätherte Hydroxy- oder Mercaptogruppe, Halogen, Formyl oder eine Gruppe der Formel -CH 2 -R 2 , worin R z eine veresterte oder verätherte Hydroxy- oder Mercaptogruppe oder eine quaternäre Ammoniogruppe darstellt, und R 3 Wasserstoff oder Methoxy bedeuten, worin funktionelle Gruppen gegebenenfalls in geschützter Form vorliegen, Salze von solchen Verbindungen mit sauren und/oder basischen Gruppen, Verfahren zur Herstellung dieser Verbindungen, solche Stoffe enthaltende pharmazeutische Mittel und deren therapeutische Verwen- . dung.
Die Verbindungen. haben antibiotische Wirksamkeit und können zur Bekämpfung von Infektionen verwendet werden.
Die Erfindung betrifft ferner neue Z wischenprodukte zur Herstellung vorstehender Verbindungen. Verfahren zu ihrer Herstellung und ihrer Verwendung.
摘要翻译：本发明涉及Aminothiazolacetamido -3-头孢烯-4-羧酸式其中指数n为1〜4的整数的酸化合物中，X是氧，硫，基团-NH-或直接键，Y是氧或硫，一个是亚甲基或由氨基，羟基，羧基，磺基，氧代，或基团= NOR“其中R”为氢或任选取代的低级烷基，取代的亚甲基，R 1是氢，低级烷基，酯化或醚化的羟基或巯基，卤素，甲酰基或下式基团-CH 2 R 2，其中R 2代表酯化的或醚化的羟基或巯基或季铵基，并且R 3是氢或甲氧基，其中的官能团是任选地被保护的形式，具有酸性和这些化合物的盐 /或碱性基团，制备这些化合物，含有这些化合物和它们的治疗的药物组合物使用。该化合物具有抗菌活性，可用于抗感染。本发明还涉及一种用于上述化合物的制备的新的中间体，它们的制备方法以及它们的用途。

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