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61. 发明授权

US4649142A 3,4-dihydro-1,3-disubstituted-6-(substituted phenylimino)-2(1H)-pyrimidinone useful as cardiotonic agent and anti-allergic agent 失效
标题翻译：可用作强心剂和抗过敏剂的3,4-二氢-1,3-二取代-6-（取代苯基亚氨基）-2（1H） - 嘧啶酮
公开(公告)号：US4649142A
公开(公告)日：1987-03-10
申请号：US743525
申请日：1985-06-07
申请人： Takao Takaya , Masayoshi Murata , Kiyotaka Ito
发明人： Takao Takaya , Masayoshi Murata , Kiyotaka Ito
IPC分类号： C07D239/46 , C07D239/54 , C07D239/56 , C07D405/04 , A61K31/505 , C07D239/02
CPC分类号： C07D239/47 , C07D239/54 , C07D239/56 , C07D405/04
摘要： The invention relates to novel pyrimidinone compounds of anti-allergic and cardiotonic activity of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl, lower alkoxycarbonyl(lower)alkyl, carboxy(lower)alkyl or di(lower)alkylamino(lower)alkyl,R.sup.3 is hydroxy, lower alkoxy, halo(lower)alkoxy, lower alkylthio, lower alkanesulfinyl, lower alkanesulfonyl, nitro, amino or di(lower)alkanesulfonylamino,R.sup.4 is hydroxy, lower alkoxy, halo(lower)alkoxy, lower alkoxycarbonyl(lower)alkoxy or carboxy(lower)alkoxy, orR.sup.3 and R.sup.4 are taken together to form lower alkylenedioxy or lower alkylidenedioxy,R.sup.5 is phenyl substituted with 1 to 4 substituents selected from the group consisting of lower alkyl and sulfamyl,R.sup.10 is hydrogen or sulfamyl, provided that when both of R.sup.1 and R.sup.2 are lower alkyl and R.sup.3 and R.sup.4 are lower alkoxy, then R.sup.10 is sulfamoyl, and that when R.sup.3 is hydroxy, then R.sup.4 is hydroxy, and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及具有下式的抗过敏和强心活性的新型嘧啶酮化合物：其中R 1和R 2各自为低级烷基，低级烷氧基羰基（低级）烷基，羧基（低级）烷基或二（低级）烷基氨基）烷基，R 3是羟基，低级烷氧基，卤代（低级）烷氧基，低级烷硫基，低级链烷亚磺酰基，低级烷磺酰基，硝基，氨基或二（低级）烷磺酰氨基，R4是羟基，低级烷氧基，卤代（低级）（低级）烷氧基或羧基（低级）烷氧基，或者R 3和R 4一起形成低级亚烷基二氧基或低级亚烷基二氧基，R 5是被1至4个选自低级烷基和氨磺酰基的取代基取代的苯基，R 10是氢或氨基磺酰基，条件是当R 1和R 2均为低级烷基且R 3和R 4均为低级烷氧基时，则R 10为氨磺酰基，当R 3为羟基时，R 4为羟基及其药学上可接受的盐。

62. 发明授权

US4631274A Halovinyl cephem compounds 失效
标题翻译：卤乙烯基头孢烯化合物
公开(公告)号：US4631274A
公开(公告)日：1986-12-23
申请号：US704776
申请日：1985-02-25
申请人： Takao Takaya , Kazuo Sakane , Hideaki Yamanaka , Kenzi Miyai
发明人： Takao Takaya , Kazuo Sakane , Hideaki Yamanaka , Kenzi Miyai
IPC分类号： C07D501/18 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/24
CPC分类号： C07D501/24
摘要： The invention relates to novel halovinyl cephem derivatives of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is a group of the formula:R.sup.4 --A--CONH--in which R.sup.4 is cyano(lower)alkenylthio or a group of the formula: ##STR2## in which R.sup.6 is hydrogen, amino or a protected amino group, andA is carbonyl, lower alkylene, hydroxy(lower)alkylene or a group of the formula: ##STR3## in which R.sup.5 is hydrogen, carboxy(lower)alkyl or protected carboxy(lower)alkyl;R.sup.2 is carboxy or a protected carboxy group; andX is halogen, and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及具有下式的高抗微生物活性的新的卤代乙烯基头孢烯衍生物：其中R 1是下式的基团：其中R 4是氰基（低级）烯硫基或下式的基团：R 4 -A-CONH- 其中R 6是氢，氨基或保护的氨基，A是羰基，低级亚烷基，羟基（低级）亚烷基或下式的基团：其中R 5是氢，羧基（低级）烷基或保护的羧基（低级）烷基; R2是羧基或被保护的羧基; 和X是卤素，及其药学上可接受的盐。

63. 发明授权

US4594446A 2-alkoxyimino-3,3-dialkoxy-butyrates and derivatives 失效
标题翻译： 2-烷氧基亚氨基-3,3-二烷氧基 - 丁酸酯及其衍生物
公开(公告)号：US4594446A
公开(公告)日：1986-06-10
申请号：US690989
申请日：1985-01-14
申请人： Ikuo Ueda , Takao Takaya , Masakazu Kobayashi , Takashi Masugi , Hisashi Takasugi , Hiromu Kochi , Tadashi Kitaguchi
发明人： Ikuo Ueda , Takao Takaya , Masakazu Kobayashi , Takashi Masugi , Hisashi Takasugi , Hiromu Kochi , Tadashi Kitaguchi
IPC分类号： C07D317/30 , C07D319/06 , C07D501/04 , C07D501/14 , C07D501/20 , C07C131/00 , C07D317/14 , C07D321/00 , C07F7/04
CPC分类号： C07D317/30 , C07D319/06
摘要： The invention relates to new antimicrobially active 3-cephem compounds, processes for preparing such compounds, new intermediate compounds comprising alkoxyimino dioxy butyric acid derivatives useful in said processes, and processes for preparation of said intermediates.

64. 发明授权

US4584290A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4584290A
公开(公告)日：1986-04-22
申请号：US556413
申请日：1983-11-30
申请人： Takao Takaya , Takashi Masugi , Takashi Ogino , Hisashi Takasugi , Hideaki Yamanaka
发明人： Takao Takaya , Takashi Masugi , Takashi Ogino , Hisashi Takasugi , Hideaki Yamanaka
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D213/20 , C07D401/06 , C07D501/18 , C07D501/24 , C07D501/38
CPC分类号： C07D213/20 , C07D401/06
摘要： The invention relates to novel compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sup.1 is amino or acylamino; andR.sup.9 is a group of the formula: ##STR2## wherein R.sup.2 is organic group,X is CH or N,Z is acid residueY is CH or N and n is O; orY is N.sup..sym. --R.sup.2 wherein R.sup.2 is as defined above and n is 1,or a group of the formula:--A--N.sup..sym. (R.sup.10).sub.3whereinR.sup.10 is lower alkyl andA is lower alkylene.
摘要翻译：本发明涉及具有下式的高抗微生物活性的新化合物：其中R1是氨基或酰氨基; 并且R 9是下式的基团：其中R 2是有机基团，X是CH或N，Z是酸残基，Y是CH或N，n是0; 或Y是N（+） - R 2，其中R 2如上定义并且n是1，或下式基团-A-N（+）（R 10）3，其中R 10是低级烷基，A是低级亚烷基。

65. 发明授权

US4563450A Cephem compounds 失效
公开(公告)号：US4563450A
公开(公告)日：1986-01-07
申请号：US515184
申请日：1983-07-19
申请人： Takao Takaya , Yoshikazu Inoue , Masayoshi Murata , Hisashi Takasugi
发明人： Takao Takaya , Yoshikazu Inoue , Masayoshi Murata , Hisashi Takasugi
IPC分类号： C07D257/04 , C07D501/36 , A61K31/545
CPC分类号： C07D257/04 , Y02P20/55
摘要： This invention relates to a new cephem compound of the formula: ##STR1## wherein R.sup.1 is amino or a substituted amino group;R.sup.2 is carboxy or a protected carboxy group;R.sup.3 is a tetrazolyl group having a lower alkynyl group; andX is --S-- or ##STR2## and pharmaceutically acceptable salts thereof, of high antimicrobial activity.

66. 发明授权

US4499088A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4499088A
公开(公告)日：1985-02-12
申请号：US455573
申请日：1983-01-04
申请人： Takao Takaya , Hisashi Takasugi , Hideaki Yamanaka
发明人： Takao Takaya , Hisashi Takasugi , Hideaki Yamanaka
IPC分类号： C07D501/36 , A61K31/545 , A61K31/546 , A61P31/04 , C07D277/20 , C07D501/24 , C07D501/34 , C07D501/46 , C07D501/56
CPC分类号： C07D277/587
摘要： This invention relates to novel cephem compounds, of antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 is carboxy (C.sub.1 -C.sub.6) alkyl or esterified carboxy (C.sub.1 -C.sub.6) alkyl,R.sup.2 is carboxy or an esterified carboxy group, andR.sup.3 is (C.sub.1 -C.sub.6) alkanoylamino, (C.sub.1 -C.sub.6) alkanesulfonyl, triazolylthio, tetrazolylthio having (C.sub.1 -C.sub.6) alkyl, pyridazinylthio having (C.sub.1 -C.sub.6) alkyl, thiadiazolylthio having (C.sub.1 -C.sub.6) alkyl, triazolopyridazinylthio or tetrazolopyridazinylthio, and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及下列化学式的抗微生物活性的新型头孢烯化合物：其中R 1是羧基（C 1 -C 6）烷基或酯化的羧基（C 1 -C 6）烷基，R 2是羧基或被酯化的羧基，R 3 是具有（C1-C6）烷基的（C1-C6）烷酰基氨基，（C1-C6）烷基磺酰基，三唑基硫基，具有（C1-C6）烷基的哒嗪硫基，具有（C1-C6）烷基的噻二唑基硫基，（C1-C6）烷基，三氮代哒嗪基硫代或四唑并哒嗪基硫基）其可接受的盐。

67. 发明授权

US4463003A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4463003A
公开(公告)日：1984-07-31
申请号：US452302
申请日：1982-12-22
申请人： Takao Takaya , Hisashi Takasugi , Hideaki Yamanaka
发明人： Takao Takaya , Hisashi Takasugi , Hideaki Yamanaka
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/20 , C07D501/34 , C07D501/36 , C07D501/56 , C07D519/06
CPC分类号： C07D501/20
摘要： The invention relates to novel cephem compounds, of antimicrobial activity, of the formula: ##STR1## wherein R.sup.1 is carboxy (C.sub.1 -C.sub.6) alkyl or esterified carboxy (C.sub.1 -C.sub.6) alkyl, R.sup.2 is carboxy or esterified carboxy, and R.sup.3 is (C.sub.1 -C.sub.6) alkanoyloxy (C.sub.1 -C.sub.6) alkyl, tetrazolopyridazinylthio (C.sub.1 -C.sub.6) alkyl, tetrazolothio (C.sub.1 -C.sub.6) alkyl, or (C.sub.1 -C.sub.6) alkyl tetrazolothio (C.sub.1 -C.sub.6) alkyl, and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及抗微生物活性的新型头孢烯化合物，其具有下式：其中R1是羧基（C1-C6）烷基或酯化的羧基（C1-C6）烷基，R2是羧基或酯化的羧基，R3是（ C1-C6）烷酰氧基（C1-C6）烷基，四唑并哒嗪硫基（C1-C6）烷基，四唑硫基（C1-C6）烷基或（C1-C6）烷基四唑硫基（C1-C6）烷基）及其药学上可接受的盐。

68. 发明授权

US4427677A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4427677A
公开(公告)日：1984-01-24
申请号：US332830
申请日：1981-12-21
申请人： Takao Takaya , Hisashi Takasugi , Masayoshi Murata , Akiteru Yoshioka
发明人： Takao Takaya , Hisashi Takasugi , Masayoshi Murata , Akiteru Yoshioka
IPC分类号： C07D277/20 , C07D277/40 , C07D501/46 , A61K31/545
CPC分类号： C07D277/587
摘要： This invention relates to novel cephem compounds of high antimicrobial activity of the formula: ##STR1## wherein R.sub.1 is amino, lower alkanoylamino or halo(lower)alkanoylamino,R.sub.2 is lower alkyl, lower alkylthio(lower)alkyl, lower alkenyl, lower alkynyl, carboxy(lower)alkyl or esterified carboxy(lower)alkyl, andX is halogen;and pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及具有下式的高抗微生物活性的新型头孢烯化合物：其中R1是氨基，低级烷酰基氨基或卤代（低级）烷酰基氨基，R2是低级烷基，低级烷硫基（低级）烷基，低级烯基，低级炔基，羧基（低级）烷基或酯化羧基（低级）烷基，X为卤素; 及其药学上可接受的盐。

69. 发明授权

US4393059A Cephem compounds 失效
标题翻译：头孢烯化合物
公开(公告)号：US4393059A
公开(公告)日：1983-07-12
申请号：US302639
申请日：1981-09-15
申请人： Takao Takaya , Hisashi Takasugi , Kiyoshi Tsuji , Toshiyuki Chiba
发明人： Takao Takaya , Hisashi Takasugi , Kiyoshi Tsuji , Toshiyuki Chiba
IPC分类号： C07D277/20 , C07D285/06 , C07D501/59 , C07D501/20 , A61K31/545
CPC分类号： C07D277/20 , C07D285/06 , C07D501/20
摘要： The invention relates particularly to syn compounds of the formula: ##STR1## wherein R.sup.2 is hydrogen or an aliphatic hydrocarbon which may be substituted with halogen, carboxy or pharmaceutically acceptable esterified carboxy,R.sup.5 is carboxy or pharmaceutically acceptable esterified carboxy,R.sup.6 is amino or protected amino andR.sup.7 is lower alkanesulfonyl or arenesulfonyl and pharmaceutically acceptable salt thereof, processes for making them, pharmaceutical compositions containing them and their use in treating infectious diseases.
摘要翻译：本发明特别涉及下式的顺式化合物：其中R 2为氢或可被卤素，羧基或药学上可接受的酯化羧基取代的脂族烃基，R 5为羧基或药学上可接受的酯化羧基，R6为氨基或保护基氨基和R7是低级烷基磺酰基或芳烃磺酰基及其药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗感染性疾病中的用途。

70. 发明授权

US4316019A Preparation of syn-isomer of 3-alkanoyloxymethyl-7-(2-alkoxyimino-2-thiazolylacetamido-3-cephem-4-car boxylic acid compounds 失效
标题翻译： 3-烷酰氧基甲基-7-（2-烷氧基亚氨基-2-噻唑基乙酰氨基-3-头孢烯-4-羧酸化合物）的顺式异构体的制备
公开(公告)号：US4316019A
公开(公告)日：1982-02-16
申请号：US916952
申请日：1978-06-19
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 , C07D277/38 , C07D277/46 , C07D277/48 , C07D333/16 , C07D501/32 , C07D501/34 , C07D501/36 , C07D501/06
CPC分类号： C07D277/20 , C07D277/38 , C07D277/46 , C07D277/48 , C07D277/587 , C07D333/16 , C07D501/18
摘要： New syn-isomers of 3-cephem-4-carboxylic acids having anti-bacterial activities, processes for preparation thereof, pharmaceutical compositions thereof, with the acids being substituted at the 3 position with acyloxymethyl, hydroxymethyl, formyl or heterocyclic thiomethyl groups and at the 7 position with alkoxyiminoacetamido substituted with substituted phenyl or substituted thiazolyl.
摘要翻译：具有抗菌活性的3-头孢烯-4-羧酸的新同分异构体，其制备方法，其药物组合物，其酸在3位被酰氧基甲基，羟甲基，甲酰基或杂环硫代甲基取代，并且在 7位与烷氧基亚氨基乙酰胺基被取代的苯基或取代的噻唑基取代。

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