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61. 发明授权

US4804761A Process for making 6-aryl-2-methylpyridines 失效
标题翻译：制备6-芳基-2-甲基吡啶的方法
公开(公告)号：US4804761A
公开(公告)日：1989-02-14
申请号：US69809
申请日：1987-07-01
申请人： Alan E. Barton
发明人： Alan E. Barton
IPC分类号： C07D213/08 , C07D213/09 , C07D213/26 , C07D213/30 , C07D213/32 , C07D405/10 , C07D213/14
CPC分类号： C07D213/08 , C07D213/26 , C07D213/30 , C07D213/32 , C07D405/10
摘要： This invention relates to a process for making 6-aryl-2-methylpyridines from substituted benzaldehydes by way of 1-aryl-1,5-diketones. The 6-aryl-2-methyl-pyridines made by this process can be used in preparing biologically active 6-aryl-pyridine thiosemicarbazones.
摘要翻译：本发明涉及通过1-芳基-1,5-二酮从取代的苯甲醛制备6-芳基-2-甲基吡啶的方法。通过该方法制备的6-芳基-2-甲基 - 吡啶可用于制备生物活性6-芳基 - 吡啶缩氨基硫脲。

62. 发明授权

US4753947A Certain fungicidal alphabenzyl-3-pyridylmethanol, the corresponding chloro derivatives thereof or the N-oxides thereof 失效
标题翻译：某些杀真菌α-花椒基-3-吡啶基甲醇，其相应的氯代衍生物或其N-氧化物
公开(公告)号：US4753947A
公开(公告)日：1988-06-28
申请号：US769535
申请日：1985-08-26
申请人： Franz Dorn , Francois Montavon , Milos Suchy
发明人： Franz Dorn , Francois Montavon , Milos Suchy
IPC分类号： A01N43/40 , A01N43/60 , C07D213/26 , C07D213/30 , C07D213/32 , C07D213/50 , C07D213/57 , C07D213/89 , C07D241/12
CPC分类号： C07D213/30 , A01N43/40 , A01N43/60 , C07D213/26 , C07D213/32 , C07D213/50 , C07D213/57 , C07D213/89 , C07D241/12
摘要： Novel pyridine and pyrazine derivatives of the formula ##STR1## wherein R.sup.4 is 3-pyridyl, 3-pyridyl-1-oxide, 2-pyrazinyl, 2-pyrazinyl-1-oxide, 2-pyrazinyl-4-oxide or 2-pyrazinyl-1,4-dioxide, and R, R.sup.1, R.sup.2 and R.sup.3 are as hereinafter set forth, processes for their preparation, fungicidal compositions containing said compounds, and methods for the use of such compounds or compositions for combatting fungi in agriculture and in horticulture are disclosed. Novel starting materials and fungicidal active substances of the formula ##STR2## wherein R.sup.4' is 3-pyridyl or 2-pyrazinyl, and R and R.sup.1" as hereinafter set forth, which are used for the preparation of the compounds of formula I, and their N-oxides, as well as fungicidal compositions containing these compounds as the active substance, are also described.
摘要翻译：新的吡啶和吡嗪衍生物，其中R 4是3-吡啶基，3-吡啶基-1-氧化物，2-吡嗪基，2-吡嗪基-1-氧化物，2-吡嗪基-4-氧化物或2-吡嗪基 -1,4-二氧化物，R，R 1，R 2和R 3如下文所述，其制备方法，含有所述化合物的杀真菌组合物，以及使用这些化合物或组合物在农业和园艺中对抗真菌的方法被披露。其中R 4'是3-吡啶基或2-吡嗪基的新颖起始物质和杀真菌活性物质，其中R 4'是下文阐述的R和R 1'，其用于制备式I化合物，还描述了它们的N-氧化物，以及含有这些化合物作为活性物质的杀真菌组合物。

63. 发明授权

US4727078A 7-phenyl-7-(3-pyridyl)-6-heptenoic acid or derivatives thereof which inhibit the activity of thromboxanes synthetase 失效
标题翻译： 7-苯基-7-（3-吡啶基）-6-庚烯酸或其抑制血栓素合成酶活性的其衍生物
公开(公告)号：US4727078A
公开(公告)日：1988-02-23
申请号：US502603
申请日：1983-06-09
申请人： Shinji Terao , Kohei Nishikawa
发明人： Shinji Terao , Kohei Nishikawa
IPC分类号： C07C51/363 , C07D201/08 , C07D213/26 , C07D213/30 , C07D213/32 , C07D213/50 , C07D213/55 , C07D213/57 , C07D405/06 , C07D409/04 , C07D409/06 , C07F9/54
CPC分类号： C07D213/30 , C07C51/363 , C07D201/08 , C07D213/26 , C07D213/32 , C07D213/50 , C07D213/55 , C07D213/57 , C07D405/06 , C07D409/04 , C07D409/06 , C07F9/5407
摘要： Novel compound of the formula: ##STR1## wherein R.sup.1 is pyridyl group, R.sup.2 is a phenyl group, a thienyl group, a furyl group, a naphthyl group, a benzothienyl group or pyridyl group, which may optionally have a lower alkoxy group, a lower alkyl group, a halogen atom, trifluoromethyl group, a lower alkenyl group or methylenedioxy group, R.sup.3 is hydrogen atom or a lower alkyl group, and n is an integer of 0 to 6, Y is sulphur atom, methylene group or a group of the formula: ##STR2## wherein R.sup.4 is hydrogen atom or acetyl group, and m is 0 or 1, and their pharmaceutically acceptable salts have an inhibitory action on bio-synthesis of thromboxane A.sub.2 (TXA.sub.2) and an effect of accelerating the productivility of prostaglandin I.sub.2 (PGI.sub.2), and can be used for mammals to the prophylaxis or therapy of thrombosis caused by platelet aggregation or ischemic diseases caused by vasospasms in cardiac, cerebral and peripheral circulatory system (e.g. cardiac infarction, apoplexy, infarct of blood vessels in kidney, lung and other organs, pectic ulcer, etc.).
摘要翻译：下式的新型化合物：其中R 1为吡啶基，R 2为可任选具有低级烷氧基的苯基，噻吩基，呋喃基，萘基，苯并噻吩基或吡啶基，低级烷基，卤原子，三氟甲基，低级烯基或亚甲二氧基，R3为氢原子或低级烷基，n为0〜6的整数，Y为硫原子，亚甲基或其中R4为氢原子或乙酰基，m为0或1，其药学上可接受的盐对凝血恶烷A2（TXA2）的生物合成具有抑制作用，并且增加前列腺素的生产性的作用 I2（PGI2），可用于哺乳动物预防或治疗由心脏，脑和周围循环系统（例如心脏梗塞，中风，肾脏血管梗死）引起的血小板聚集或血管痉挛引起的血栓形成，肺等器官，果胶性溃疡等）。

64. 发明授权

US4556661A Pyridine derivatives 失效
标题翻译：吡啶衍生物
公开(公告)号：US4556661A
公开(公告)日：1985-12-03
申请号：US412360
申请日：1982-08-27
申请人： Franz Dorn , Francois Montavon , Milos Suchy
发明人： Franz Dorn , Francois Montavon , Milos Suchy
IPC分类号： A01N43/40 , A01N43/60 , C07D213/26 , C07D213/30 , C07D213/32 , C07D213/50 , C07D213/57 , C07D213/89 , C07D241/12
CPC分类号： C07D213/30 , A01N43/40 , A01N43/60 , C07D213/26 , C07D213/32 , C07D213/50 , C07D213/57 , C07D213/89 , C07D241/12
摘要： Novel pyridine and pyrazine derivatives of the formula ##STR1## wherein R.sup.4 is 3-pyridyl, 3-pyridyl-1-oxide, 2-pyrazinyl, 2-pyrazinyl-1-oxide, 2-pyrazinyl-4-oxide or 2-pyrazinyl-1,4-dioxide, and R, R.sup.1, R.sup.2 and R.sup.3 are as hereinafter set forth, processes for their preparation, fungicidal compositions containing said compounds, and methods for the use of such compounds or compositions for combatting fungi in agriculture and in horticulture are disclosed. Novel starting materials and fungicidal active substances of the formula ##STR2## wherein R.sup.4' is 3-pyridyl or 2-pyrazinyl, and R and R.sup.1" as hereinafter set forth, which are used for the preparation of the compounds of formula I, and their N-oxides, as well as fungicidal compositions containing these compounds as the active substance, are also described.
摘要翻译：新的吡啶和吡嗪衍生物，其中R 4是3-吡啶基，3-吡啶基-1-氧化物，2-吡嗪基，2-吡嗪基-1-氧化物，2-吡嗪基-4-氧化物或2-吡嗪基 -1,4-二氧化物，R，R 1，R 2和R 3如下文所述，其制备方法，含有所述化合物的杀真菌组合物，以及使用这些化合物或组合物在农业和园艺中对抗真菌的方法被披露。其中R 4'是3-吡啶基或2-吡嗪基的新颖起始物质和杀真菌活性物质，其中R 4'是下文阐述的R和R 1'，其用于制备式I化合物，还描述了它们的N-氧化物，以及含有这些化合物作为活性物质的杀真菌组合物。

65. 发明授权

US4521413A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4521413A
公开(公告)日：1985-06-04
申请号：US414471
申请日：1982-09-02
申请人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
发明人： Tsutomu Teraji , Kazuo Sakane , Jiro Goto
IPC分类号： C07C257/14 , C07D213/30 , C07D213/32 , C07D213/68 , C07D213/70 , C07D213/74 , C07D285/08 , C07D401/12 , C07D501/20 , C07D501/46 , C07D501/38 , A61K31/545
CPC分类号： C07D213/30 , C07D213/32 , C07D213/68 , C07D213/70 , C07D213/74 , C07D285/08 , C07D401/12 , Y02P20/55
摘要： The invention relates to cephem compounds of high antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 is amino or a protected amino group;R.sup.2 is lower alkyl which may be substituted with one carboxy, lower alkenyl, lower alkynyl, cyclo (lower) alkyl or cyclo (lower) alkenyl;R.sup.3 is lower alkylamino, N-(lower) alkanoyl (lower) alkylamino, di (lower) alkylamino, sulfo (lower) alkylamino, hydroxy (lower) alkylamino, N-(lower) alkanoylhydroxy (lower) alkylamino, alkanoyloxy (lower) alkyl, alkenoyloxy (lower) alkyl, lower alkoxy (lower) alkoxy (lower) alkyl, di (lower) alkylamino (lower) alkyl, lower alkylthio (lower) alkyl, lower alkylthio, lower alkoxy, lower alkoxy (lower) alkoxy, hydroxy (lower) alkoxy, lower alkanesulfonyl (lower) alkyl, hydroxy (lower) alkylthio, di (lower) alkylamino (lower) alkylthio, tetrazolyl, tetrazolylthio, tetrazolylthio (lower) alkyl or dihydrotriazinylthio (lower) alkyl substituted with oxo, hydroxy and lower alkyl; andR.sup.4 is hydrogen or lower alkyl; and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及高抗微生物活性的头孢烯化合物，其具有下式：其中R1是氨基或被保护的氨基; R2是可被一个羧基，低级烯基，低级炔基，环（低级）烷基或环（低级）烯基取代的低级烷基; R3是低级烷基氨基，N-（低级）烷酰基（低级）烷基氨基，二（低级）烷基氨基，磺基（低级）烷基氨基，羟基（低级）烷基氨基，N-（低级）烷酰基羟基（低级）烷基氨基，烷酰氧基（低级）烷基，低级烷氧基（低级）烷基，低级烷氧基（低级）烷基，低级烷基氨基（低级）烷基，低级烷硫基（低级）烷基，低级烷硫基，低级烷氧基，低级烷氧基低级烷基磺酰基（低级）烷基，羟基（低级）烷硫基，二（低级）烷基氨基（低级）烷硫基，四唑基，四唑基硫代，被氧代取代的四唑基硫基（低级）烷基或二氢三嗪基硫代（低级） ; R4为氢或低级烷基; 及其药学上可接受的盐。

66. 发明授权

US4499101A Pharmacologically active isoxazole and triazole compounds 失效
标题翻译：药理活性异恶唑和三唑化合物
公开(公告)号：US4499101A
公开(公告)日：1985-02-12
申请号：US463768
申请日：1983-02-04
申请人： Graham J. Durant , Charon R. Ganellin
发明人： Graham J. Durant , Charon R. Ganellin
IPC分类号： C07D213/02 , A61K31/415 , A61K31/433 , A61P1/04 , A61P43/00 , C07D213/32 , C07D213/61 , C07D213/65 , C07D233/54 , C07D233/64 , C07D233/68 , C07D233/88 , C07D249/08 , C07D249/12 , C07D261/08 , C07D263/46 , C07D275/02 , C07D277/20 , C07D277/26 , C07D285/12 , C07D285/135 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , A61K31/41 , A61K31/42
CPC分类号： C07D233/64 , C07D213/32 , C07D213/65 , C07D233/68 , C07D249/08 , C07D261/08 , C07D263/46 , C07D275/02 , C07D277/26 , C07D285/135
摘要： The compounds are N,N'-substituted thioureas, ureas and guanidines which are H-2 histamine receptor inhibitors. Two compounds of this invention are N,N'-bis[2-((4-methyl-5-imidazolyl)methylthio)ethyl]thiourea and N,N'-bis[2-((4-methyl-5-imidazolyl)methylthio)ethyl]-N"-cyanoguanidine.
摘要翻译：这些化合物是N，N'-取代的硫脲，脲和胍，它们是H-2组胺受体抑制剂。本发明的两种化合物是N，N'-双[2 - （（4-甲基-5-咪唑基）甲硫基）乙基]硫脲和N，N'-双[2 - （（4-甲基-5-咪唑基）甲硫基）乙基] -N“ - 氰基胍

67. 发明授权

US4415579A Pyridine derivatives 失效
公开(公告)号：US4415579A
公开(公告)日：1983-11-15
申请号：US353556
申请日：1982-03-01
申请人： Roger Crossley
发明人： Roger Crossley
IPC分类号： C07D213/32 , A61K31/44 , C07D213/28 , C07D213/44 , C07D213/62
CPC分类号： C07D213/32 , Y10S514/926 , Y10S514/927
摘要： The invention relates to a pharmaceutical composition comprising an anti-ulcer effective amount of a compound of formula I ##STR1## wherein R represents hydrogen, lower alkyl, phenyl, halophenyl, loweralkylphenyl, loweralkoxyphenyl, or aralkyl of 7 to 12 carbon atoms, R.sup.1 represents hydrogen or lower alkoxy, R.sup.2 represents hydrogen, chlorine or trifluoromethyl and n is 1 or 2, or a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutically acceptable carrier.A method of treating ulcers or hypersecretion in a mammal which comprises administering a compound of formula I is also disclosed. Some compounds of formula I are novel and within the scope of the invention.

68. 发明授权

US4388319A N-Heterocyclic alkyl-N'-thiadiazolyl, thiazolyl and isothiazolyl alkylthioureas, ureas and guanidines 失效
标题翻译： N-杂环烷基-N'-噻二唑基，噻唑基和异噻唑烷基硫脲，脲和胍
公开(公告)号：US4388319A
公开(公告)日：1983-06-14
申请号：US215293
申请日：1980-12-11
申请人： Graham J. Durant , Charon R. Ganellin
发明人： Graham J. Durant , Charon R. Ganellin
IPC分类号： C07D213/32 , C07D213/65 , C07D233/54 , C07D233/68 , C07D249/08 , C07D261/08 , C07D263/46 , C07D275/02 , C07D277/26 , C07D285/12 , C07D285/135 , A61K31/425 , A61K31/41 , A61K31/415 , A61K31/42 , C07D403/12 , C07D413/12 , C07D417/12
CPC分类号： C07D233/64 , C07D213/32 , C07D213/65 , C07D233/68 , C07D249/08 , C07D261/08 , C07D263/46 , C07D275/02 , C07D277/26 , C07D285/135 , Y10S514/926 , Y10S514/927
摘要： The compounds are N,N'-substituted thioureas, ureas and guanidines which are H-2 histamine receptor inhibitors. A compound of this invention is N-cyano-N'-[2-((4-methyl-5-imidazolyl)methylthio)ethyl]-N"-[2-(2-thiazolylmethylthio)ethyl]guanidine.
摘要翻译：这些化合物是N，N'-取代的硫脲，脲和胍，它们是H-2组胺受体抑制剂。本发明化合物是N-氰基-N' - [2 - （（4-甲基-5-咪唑基）甲硫基）乙基] -N“ - [2-（2-噻唑基甲硫基）乙基]胍。

69. 发明授权

US4379154A Thiocarboxamide derivatives and their use as pharmaceuticals 失效
标题翻译：硫代羧酰胺衍生物及其作为药物的用途
公开(公告)号：US4379154A
公开(公告)日：1983-04-05
申请号：US264550
申请日：1981-05-18
申请人： Jean-Claude Aloup , Jean Bouchaudon , Daniel Farge , Claude James
发明人： Jean-Claude Aloup , Jean Bouchaudon , Daniel Farge , Claude James
IPC分类号： C07D409/04 , A61K31/357 , A61K31/382 , A61K31/385 , A61K31/39 , A61K31/44 , A61K31/4412 , A61K31/443 , A61K31/4433 , A61K31/47 , A61K31/495 , A61K31/50 , A61P1/04 , A61P9/12 , C07D213/32 , C07D215/12 , C07D237/08 , C07D241/12 , C07D405/04 , C07D411/04
CPC分类号： C07D241/12 , C07D213/32 , C07D215/12 , C07D237/08
摘要： Thioformamide derivatives of the formula: ##STR1## wherein R represents hydrogen or alkyl of 1 through 4 carbon atoms, and (i) Het represents a heterocyclic radical selected from pyrid-3-yl, pyrid-4-yl, pyridazinyl, pyrazinyl, pyrimidinyl, quinolyl, imidazolyl, naphthyridinyl, quinoxalinyl and quinazolinyl, X represents sulphur or oxygen and Y represents sulphur or oxygen, a valency bond or methylene, or (ii) Het represents pyrid-2-yl, X represents sulphur or oxygen and Y represents sulphur or oxygen or methylene, or (iii) Het represents pyrid-2-yl, X represents oxygen and Y represents a valency bond, are new compounds possessing useful pharmacological properties. They are particularly useful in the treatment of gastrointestinal ulcers and in the treatment of hypertension, depending on the definition of the symbol Het.
摘要翻译：下式的硫代甲酰胺衍生物：其中R表示氢或1至4个碳原子的烷基，和（i）Het表示选自吡啶-3-基，吡啶-4-基，哒嗪基，吡嗪基，嘧啶基的杂环基喹啉基，咪唑基，萘啶基，喹喔啉基和喹唑啉基，X表示硫或氧，Y表示硫或氧，价键或亚甲基，或（ii）Het表示吡啶-2-基，X表示硫或氧，Y表示硫或氧或亚甲基，或（iii）Het表示吡啶-2-基，X表示氧，Y表示价键，是具有有用药理特性的新化合物。它们在治疗胃肠溃疡和治疗高血压方面特别有用，取决于符号Het的定义。

70. 发明授权

US4375472A Amidinosulphonic acid derivatives 失效
标题翻译：脒基磺酸衍生物
公开(公告)号：US4375472A
公开(公告)日：1983-03-01
申请号：US209449
申请日：1980-11-24
申请人： Graham J. Durant , Rodney C. Young , Zev Tashma
发明人： Graham J. Durant , Rodney C. Young , Zev Tashma
IPC分类号： A61K31/42 , A61K31/44 , A61K31/4402 , A61K31/4418 , A61P37/08 , C07D213/32 , C07D213/61 , C07D213/65 , C07D233/54 , C07D233/64 , C07D233/68 , C07D249/08 , C07D261/08 , C07D263/32 , C07D275/02 , C07D275/03 , C07D277/26 , C07D285/12 , C07D285/135 , A61K31/425
CPC分类号： C07D233/64 , C07D213/32 , C07D213/61 , C07D213/65 , C07D249/08 , C07D261/08 , C07D263/32 , C07D275/02 , C07D275/03 , C07D277/26 , C07D285/135
摘要： Amidinosulphonic acid derivatives carrying an unsaturated nitrogen heterocycle-containing substituent, representative of which are N-methyl-N'[2-(5-methyl-4-imidazolylmethylthio)- ethyl] amidinosulphonic acid and N-methyl-N'-[2-(3-chloropyrid-2-ylmethylthio) ethyl] amidinosulphonic acid, are histamine H.sub.2 -receptor antagonists.

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