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101. 发明授权

US4452985A 2-Guanyl-4-(substituted phenyl) thiazole derivatives 失效
标题翻译： 2-鸟苷基-4-（取代苯基）噻唑衍生物
公开(公告)号：US4452985A
公开(公告)日：1984-06-05
申请号：US466239
申请日：1983-02-14
申请人： Arthur A. Santilli , Anthony C. Scotese , Robert L. Morris , Stanley C. Bell
发明人： Arthur A. Santilli , Anthony C. Scotese , Robert L. Morris , Stanley C. Bell
IPC分类号： C07D277/48 , C07D417/10 , C07D277/46 , A61K31/425
CPC分类号： C07D417/10 , C07D277/48
摘要： Compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, cyano or cyano(lower)alkyl;R.sup.2 is hydrogen, cyano, carboxy, carbamoyl, guanyl, (lower)alkoxyimino, hydrazinocarbonyl, (lower)alkylaminoimino, ##STR2## with the proviso that one but never both of R.sup.1 and R.sup.2 is hydrogen; and the pharmacologically acceptable salts thereof exhibit H.sub.2 -receptor antagonist and gastric secretion inhibition activity.
摘要翻译：下式的化合物：其中R 1是氢，氰基或氰基（低级）烷基; R2是氢，氰基，羧基，氨基甲酰基，脒基，（低级）烷氧基亚氨基，肼基羰基，（低级）烷基氨基亚氨基，条件是R1和R2之间的一个但不是二者都是氢; 其药理学上可接受的盐显示出H 2受体拮抗剂和胃分泌抑制活性。

102. 发明授权

US4431643A Syn-isomer of 3-substituted-7-[2-cyclopentyloxyimino-2-(2-aminothiazol-4-yl)-acetamido]- 3 失效
标题翻译： 3-取代-7- [2-环戊氧基亚氨基-2-（2-氨基噻唑-4-基） - 乙酰氨基] -3-头孢烯-4-羧酸化合物的异构体
公开(公告)号：US4431643A
公开(公告)日：1984-02-14
申请号：US353879
申请日：1982-03-01
申请人： Takao Takaya , Takashi Masugi , Hisashi Takasugi , Hiromu Kochi
发明人： Takao Takaya , Takashi Masugi , Hisashi Takasugi , Hiromu Kochi
IPC分类号： C07D277/20 , C07D277/48 , C07D333/16 , C07D501/24 , A61K31/545 , C07D501/56
CPC分类号： C07D277/20 , C07D277/48 , C07D277/587 , C07D333/16
摘要： The present invention relates to new syn-isomers of 3,7-disubstituted-3-cephem-4-carboxylic acid compounds, pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising the same, which have antibacterial activities in the treatment of infectious diseases in human beings and animals.
摘要翻译：本发明涉及3,7-二取代-3-头孢烯-4-羧酸化合物的新的同分异构体，其药学上可接受的盐，以及包含它们的药物组合物，其在人类感染性疾病的治疗中具有抗菌活性生物和动物。

103. 发明授权

US4409216A Method of treating diabetes using oxazoline or thiazoline compounds 失效
标题翻译：使用恶唑啉或噻唑啉化合物治疗糖尿病的方法
公开(公告)号：US4409216A
公开(公告)日：1983-10-11
申请号：US139284
申请日：1980-04-11
申请人： Barrie C. C. Cantello
发明人： Barrie C. C. Cantello
IPC分类号： C07D277/20 , A61K31/42 , A61K31/421 , A61P3/08 , A61P3/10 , C07D263/48 , C07D277/48 , C07D277/82 , A61K31/425 , A61K31/535 , A61K31/54
CPC分类号： C07D263/48 , C07D277/48 , C07D277/82
摘要： A compound, with hypoglycaemic activity, having formula (II) or a pharmaceutically acceptable acid addition salt thereof: ##STR1## wherein X represents oxygen or sulphur;R.sup.1 R.sup.2 are the same or different and represent hydrogen, halogen, C.sub.1-6 alkyl, phenyl, benzyl,C.sub.3-6 cycloalkyl, carbo-C.sub.1-6 alkoxy or C.sub.1-6 carboxy or R.sup.1 and R.sup.2 represent the remaining members of a benzene ring;R.sup.3 represents hydrogen, C.sub.1-6 alkyl, phenyl or benzyl;R.sup.4 represents hydrogen or C.sub.1-6 alkyl;R.sup.5 represents C.sub.1-6 alkyl, phenyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl, and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or R.sup.4 and R.sup.5 together represent the remaining members of a 5- or 6- membered ring optionally containing an oxygen, sulphur or additional nitrogen atom and being optionally substituted with C.sub.1-6 alkyl; andR.sup.6 represents C.sub.1-6 alkyl, phenyl, optionally substituted with up to 3 groups selected from halogen, nitro-, amino-, trifluoromethyl, C.sub.1-6 alkyl and C.sub.1-6 alkoxy; or benzyl optionally substituted with up to 3 groups selected from halogen, C.sub.1-6 alkyl and C.sub.1-6 al
摘要翻译：具有低血糖活性的化合物，具有式（II）或其药学上可接受的酸加成盐：其中X表示氧或硫; R1 R2相同或不同，代表氢，卤素，C 1-6烷基，苯基，苄基，C 3-6环烷基，碳-C 1-6烷氧基或C 1-6羧基或R 1和R 2表示苯环的剩余成员 ; R3代表氢，C1-6烷基，苯基或苄基; R4表示氢或C1-6烷基; R5表示C1-6烷基，任选被至多3个选自卤素，C 1-6烷基和C 1-6烷氧基的基团取代的苯基; 或任选被至多3个选自卤素，C 1-6烷基和C 1-6烷氧基的基团取代的苄基; 或R 4和R 5一起代表5-或6-元环的任选含有氧，硫或另外的氮原子并且任选地被C 1-6烷基取代的剩余成员; R 6表示C 1-6烷基，苯基，任选被至多3个选自卤素，硝基，氨基 - ，三氟甲基，C 1-6烷基和C 1-6烷氧基的基团取代; 或任选被至多3个选自卤素，C 1-6烷基和C 1-6的基团取代的苄基

104. 发明授权

US4386089A .beta.-Lactam antibiotics and their medicinal use 失效
标题翻译： β-内酰胺抗生素及其药用
公开(公告)号：US4386089A
公开(公告)日：1983-05-31
申请号：US276762
申请日：1981-06-24
申请人： Hans-Bodo Konig , Karl G. Metzger , Michael Preiss
发明人： Hans-Bodo Konig , Karl G. Metzger , Michael Preiss
IPC分类号： C07D499/70 , A61K31/43 , A61P31/04 , C07D233/38 , C07D277/20 , C07D277/48 , C07D499/00 , C07D499/46 , C07D499/64 , C07D501/20 , C07D501/34 , C07D501/36 , A61K31/545
CPC分类号： C07D277/20 , C07D233/38 , C07D277/48 , C07D499/00
摘要： .beta.-Lactam compounds of the formula ##STR1## in which B denotes an optionally substituted heterocyclic 5-membered or 6-membered ring or an optionally substituted phenyl ring,Z denotes a hydrogen atom or a C.sub.1 to C.sub.4 alkoxy group, ##STR2## Y, E.sub.1 and E.sub.2 independently of one another denote a divalent organic radical andR.sub.1, R.sub.2, R.sub.3 and R.sub.4 independently of one another denote a hydrogen atom or an alkyl, alkenyl, alkinyl, alkadienyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, aryl or heterocyclyl radical, it also being possible for the above-mentioned radicals, with the exception of hydrogen, to be substituted, or an acyl radical,are antibacterial agents with a broad antibacterial spectrum and are useful as agents for promoting growth and for improving feed utilization in animals and as antioxidants.
摘要翻译：式（I）的β-内酰胺化合物，其中B表示任选取代的杂环5元或6元环或任选取代的苯环，Z表示氢原子或C1至C4烷氧基， Y，E1和E2彼此独立地表示二价有机基团，R 1，R 2，R 3和R 4彼此独立地表示氢原子或烷基，烯基，炔基，链烯基，环烷基，环烯基，环链二烯基，芳基或杂环基，除了氢被取代以外，上述基团也可以是酰基，是具有广谱抗菌谱的抗菌剂，并且可用作促进生长的试剂并提高动物和抗氧化剂的饲料利用率。

105. 发明授权

US4362728A Haloguanidine compounds, pharmaceutical compositions and methods of use 失效
标题翻译：卤代胍化合物，药物组合物和使用方法
公开(公告)号：US4362728A
公开(公告)日：1982-12-07
申请号：US206005
申请日：1980-11-12
申请人： Tobias O. Yellin , Philip N. Edwards , Michael S. Large
发明人： Tobias O. Yellin , Philip N. Edwards , Michael S. Large
IPC分类号： C07D251/16 , C07C279/18 , C07C323/44 , C07C335/28 , C07D209/48 , C07D213/74 , C07D213/75 , C07D231/38 , C07D231/40 , C07D239/42 , C07D239/46 , C07D239/47 , C07D239/48 , C07D241/20 , C07D251/18 , C07D277/20 , C07D277/42 , C07D277/48 , C07D285/08 , C07D403/12 , C07D417/12 , G09F13/04 , C07D239/24 , A61K31/495 , A61K31/505
CPC分类号： C07D209/48 , C07C323/44 , C07C335/28 , C07D213/75 , C07D231/40 , C07D239/42 , C07D239/47 , C07D239/48 , C07D241/20 , C07D251/18 , C07D277/48 , C07D285/08
摘要： Compounds useful for inhibiting gastric acid secretion and for the treatment of peptic ulcers caused or exacerbated by gastric acidity having the following formula (I): ##STR1## in which R.sup.1 and R.sup.2, are H, C.sub.1-10 alkyl, C.sub.3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C.sub.1-6 and the cycloalkyl part is C.sub.3-8, each of the alkyl, cycloalkyl and cycloalkylalkyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R.sup.1 and R.sup.2 is a halogen substituted alkyl, cycloalkyl or cycloalkylalkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen; and X, m, Y, n and R.sup.3 are as described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof. Processes for producing compounds of formula (I), pharmaceutical compositions containing them, methods of utilizing such compositions and intermediates useful for synthesizing compounds of formula (I) are also described.
摘要翻译：可用于抑制胃酸分泌和治疗由胃酸引起或加重的具有下式（I）的消化性溃疡的化合物：其中R 1和R 2为H，C 1-10烷基，C 3-8环烷基或烷基部分为C 1-6且环烷基部分为C 3-8的环烷基烷基，烷基，环烷基和环烷基烷基中的每一个任选被一个或多个选自F，Cl和Br的卤素取代，条件是至少一个 R1和R2是卤素取代的烷基，环烷基或环烷基烷基，条件是在直接与氮连接的碳上不存在卤素取代基; X，m，Y，n和R3如说明书所述; 及其药学上可接受的酸加成盐。还描述了制备式（I）化合物，含有它们的药物组合物，利用这些组合物的方法和用于合成式（I）化合物的中间体的方法。

106. 发明授权

US4355160A Thiazolylacetamido cephalosporin type compounds 失效
标题翻译：噻唑基乙酰胺基头孢菌素型化合物
公开(公告)号：US4355160A
公开(公告)日：1982-10-19
申请号：US240466
申请日：1981-03-04
申请人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
发明人： Michihiko Ochiai , Taiiti Okada , Osami Aki , Akira Morimoto , Kenji Kawakita , Yoshihiro Matsushita
IPC分类号： C07D277/20 , C07D277/32 , C07D277/34 , C07D277/38 , C07D277/40 , C07D277/42 , C07D277/46 , C07D277/48 , C07D501/36 , A61K31/545
CPC分类号： C07D277/20 , C07D277/34 , C07D277/40 , C07D277/46 , C07D277/48
摘要： The present invention is directed to a compound having antibacterial activity of the formula ##STR1## wherein R.sup.1 represents amino, protected amino, hydroxy or protected hydroxy;R.sup.4 represents heterocyclic thio wherein heterocyclic is a 5 to 6 membered hetero ring containing 1 to 4 hetero atoms from the group of oxygen, sulfur and nitrogen; andR.sup.5 is hydroxy or protected hydroxy, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明涉及具有下式的抗菌活性的化合物：其中R 1表示氨基，被保护的氨基，羟基或被保护的羟基; R4表示杂环硫基，其中杂环是含有1至4个来自氧，硫和氮的杂原子的5至6元杂环; R5是羟基或被保护的羟基，或其药学上可接受的盐。

107. 发明授权

US4353902A Livestock feed and method for improving food utilization 失效
标题翻译：家畜饲料和提高食品利用的方法
公开(公告)号：US4353902A
公开(公告)日：1982-10-12
申请号：US189540
申请日：1980-09-22
申请人： Richard D. Hedde , Roger C. Parish
发明人： Richard D. Hedde , Roger C. Parish
IPC分类号： C07D233/64 , A23K1/16 , A23K1/18 , A61K31/34 , A61K31/341 , A61K31/415 , A61P3/00 , C07D277/20 , C07D277/48 , C07D307/52 , C07D401/14 , C07D405/14 , C07D417/12
CPC分类号： A23K50/30 , A23K20/116 , A23K20/121 , A23K20/137 , Y10S426/807
摘要： Supplemented livestock feedstuffs and methods of feeding using as active ingredient a chemical compound having histamine H.sub.2 antagonist activity improve the utilization of food by meat producing animals. A specific compound of use as the active ingredient is metiamide.
摘要翻译：补充的家畜饲料和使用作为活性成分的具有组胺H 2拮抗剂活性的化合物的饲养方法改善了肉类生产动物对食物的利用。作为活性成分的具体化合物是甲胺。

108. 发明授权

US4342765A Guanidine derivatives and pharmaceutical compositions containing them 失效
标题翻译：胍衍生物和含有它们的药物组合物
公开(公告)号：US4342765A
公开(公告)日：1982-08-03
申请号：US112608
申请日：1980-01-16
申请人： Derrick F. Jones , Keith Oldham
发明人： Derrick F. Jones , Keith Oldham
IPC分类号： C07D277/20 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/505 , A61P1/00 , A61P1/04 , A61P43/00 , C07D263/48 , C07D271/06 , C07D271/07 , C07D277/48 , C07D285/08 , C07D417/12 , C07D263/30
CPC分类号： C07D271/07 , C07D263/48 , C07D277/48 , C07D285/08
摘要： Guanidine derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. These derivatives have the formula: ##STR1## in which X is oxygen or sulphur;Y is nitrogen or a CH radical;n is 1, 2, 3 or 4;m is 0 or 1;R.sup.1 is, for example, hydrogen or alkyl of 1-6 carbons; andR.sup.2 is, for example, ##STR2## and are characterized by the guanidino and cycloalkyl substituents which are attached directly to the heterocyclic ring.
摘要翻译：作为组胺H-2拮抗剂的胍衍生物，其抑制胃酸分泌。这些衍生物具有下式：其中X是氧或硫的 Y是氮或CH基; n为1,2,3或4; m为0或1; R1是例如氢或1-6个碳的烷基; 并且R 2是例如，其特征在于直接连接到杂环上的胍基和环烷基取代基。

109. 发明授权

US4287207A Pharmaceutical composition containing 1,3,5-substituted biuret compound 失效
标题翻译：含有1,3,5-取代缩二脲化合物的药物组合物
公开(公告)号：US4287207A
公开(公告)日：1981-09-01
申请号：US134411
申请日：1980-03-27
申请人： Hajime Fujmura , Yasuzo Hiramatsu , Takahiro Yabuuchi , Masakatu Hisaki , Katsuo Takikawa , Takaji Honna , Hidekazu Miyake , Makoto Kajitani
发明人： Hajime Fujmura , Yasuzo Hiramatsu , Takahiro Yabuuchi , Masakatu Hisaki , Katsuo Takikawa , Takaji Honna , Hidekazu Miyake , Makoto Kajitani
IPC分类号： A61K31/17 , C07C273/18 , C07C275/62 , C07D213/40 , C07D213/75 , C07D239/42 , C07D277/48 , C07D317/66 , C07D333/36 , A61K31/145 , A61K31/22 , A61K31/275
CPC分类号： C07D213/40 , A61K31/17 , C07C273/1863 , C07C273/1872 , C07D213/75 , C07D239/42 , C07D277/48 , C07D317/66 , C07D333/36 , Y10S514/825 , Y10S514/916
摘要： An analgesic, anti-inflammatory or anti-pyretic composition containing 1,3,5-substituted biuret compound of the formula, ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group, a substituted lower alkyl group having chlorine atom(s), cyano group(s), dimethylamino group(s), hydroxy group(s), methoxy group(s) or carboxy group(s) as the substituent(s), a lower alkenyl group, a hydroxy group, a methoxy group, an acetyl group or a phenyl group; R.sup.2 is a hydrogen atom, a lower alkyl group or a phenyl group; R.sup.3 is a phenyl group, a substituted phenyl group having halogen atom(s), trifluoromethyl group(s), methyl group(s), methoxy group(s), methylenedioxy group(s), hydroxy group(s), dimethylamino group(s), carboxy group(s) or carboxymethyl group(s) as the substituent(s), a benzyl group, a pyridyl group, a substituted pyridyl group having methyl group(s) as the substituent(s), a pyridylmethyl group, pyrimidinyl group, a thiazolyl group or a thienyl group, as the active ingredient.
摘要翻译：含有下式的1,3,5-取代缩二脲化合物的镇痛，抗炎或抗裂解组合物，其中R1是氢原子，低级烷基，具有氯原子的取代的低级烷基（s ），氰基，二甲基氨基，羟基，甲氧基或羧基作为取代基，低级烯基，羟基，甲氧基，乙酰基或苯基; R2是氢原子，低级烷基或苯基; R3为苯基，具有卤素原子的取代苯基，三氟甲基，甲基，甲氧基，亚甲二氧基，羟基，二甲基氨基（二甲基氨基） s），作为取代基的羧基或羧甲基，苄基，吡啶基，具有甲基取代基的取代的吡啶基，吡啶基甲基，嘧啶基，噻唑基或噻吩基作为有效成分。

110. 发明授权

US4283408A Guanidinothiazole compounds, process for preparation and gastric inhibiting compositions containing them 失效
标题翻译：胍基噻唑化合物，制备方法和含有它们的胃抑制组合物
公开(公告)号：US4283408A
公开(公告)日：1981-08-11
申请号：US107629
申请日：1979-12-27
申请人： Yasufumi Hirata , Isao Yanagisawa , Yoshio Ishii , Shinichi Tsukamoto , Noriki Ito , Yasuo Isomura , Masaaki Takeda
发明人： Yasufumi Hirata , Isao Yanagisawa , Yoshio Ishii , Shinichi Tsukamoto , Noriki Ito , Yasuo Isomura , Masaaki Takeda
IPC分类号： C07D277/20 , A61K31/425 , A61K31/426 , A61P1/00 , A61P1/04 , A61P43/00 , C07D277/40 , C07D277/48 , C07D277/38
CPC分类号： C07D277/48 , C07D277/40
摘要： Novel guanidinothiazole compounds of the general formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, R.sub.1 represents an amino group, a lower alkyl group, a halogeno lower alkyl group, a substituted- or unsubstituted-aryl group, a mono- or di-lower alkylamino group, an arylamino group or an aralkylamino group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, Y represents a sulfur atom or a methylene group, m and n, each represents an integer of 1-3, and the pharmacologically acceptable acid addition salts thereof, they are useful as gastric acid secretion inhibitors.
摘要翻译：新型的胍基噻唑化合物，其通式为：其中R表示氢原子或低级烷基，R1表示氨基，低级烷基，卤代低级烷基，取代或未取代的芳基，单 - 或二 - 低级烷基氨基，芳基氨基或芳烷基氨基，R 2表示氢原子，低级烷基，低级烯基或低级炔基，Y表示硫原子或亚甲基，m和n 各自表示1-3的整数，其药理学上可接受的酸加成盐可用作胃酸分泌抑制剂。

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