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1. 发明授权

US4970305A Crystalline dihydrochloride of cephalosporin derivative and a method for preparation thereof 失效
标题翻译：头孢菌素衍生物的结晶二盐酸盐及其制备方法
公开(公告)号：US4970305A
公开(公告)日：1990-11-13
申请号：US413915
申请日：1989-09-28
申请人： Tsuneo Okonogi , Yasushi Murai , Masahiro Onodera , Toshio Nishizuka , Yasuhiko Abat , Seiji Shibahara , Shigeharu Inouye
发明人： Tsuneo Okonogi , Yasushi Murai , Masahiro Onodera , Toshio Nishizuka , Yasuhiko Abat , Seiji Shibahara , Shigeharu Inouye
IPC分类号： C07D501/00 , A61K31/545 , C07D501/36
CPC分类号： C07D501/36 , Y02P20/55
摘要： The crystalline dihydrochloride of a specific cephalosporin derivative is stable to heat and retains its antibacterial activity even after storage over long periods at high temperature. The crystalline dihydrochloride can be obtained by removing protective groups from the cephalosporin derivative wherein the amino group and carboxy groups are protected and then crystallizing the cephalosporin derivative from a hydrochloric acid aqueous solution. The crystalline dihydrochloride is useful for pharmaceutical preparations.

2. 发明授权

US5334723A 2-piperidinecarboxylic acid derivative, oncogene suppressor and agent for obtaining revertants 失效
标题翻译： 2-哌啶羧酸衍生物，癌基因抑制剂和获得回复体的试剂
公开(公告)号：US5334723A
公开(公告)日：1994-08-02
申请号：US937112
申请日：1992-08-31
申请人： Tsuneo Okonogi , Osamu Makabe , Yuichi Yamamoto , Osamu Itoh , Tsutomu Tsuruoka , Takayuki Usui , Seiji Shibahara , Kozo Nagaoka , Shigeharu Inouye , Nobuko Okada , Susumu Nishimura
发明人： Tsuneo Okonogi , Osamu Makabe , Yuichi Yamamoto , Osamu Itoh , Tsutomu Tsuruoka , Takayuki Usui , Seiji Shibahara , Kozo Nagaoka , Shigeharu Inouye , Nobuko Okada , Susumu Nishimura
IPC分类号： C07D211/90 , C07D211/76 , C07D211/86 , C07D211/88
CPC分类号： C07D211/90
摘要： A novel 2-piperidinecarboxylic acid derivative represented by the formula: ##STR1## wherein X represents an oxygen atom, a sulfur atom or a nitrogen atom to which a hydrogen atom is bound; and * represents that the configuration of the carbon atom binding to the carboxyl group is (S), (R) or a mixture of (S) and (R); and a pharmaceutically acceptable salt thereof which exerts an antitumor effect over a wide range of tumor cells.
摘要翻译：由下式表示的新颖的2-哌啶羧酸衍生物：其中X表示与氢原子结合的氧原子，硫原子或氮原子; 和*表示与羧基结合的碳原子的构型是（S），（R）或（S）和（R）的混合物。和其药学上可接受的盐在广泛的肿瘤细胞上发挥抗肿瘤作用。

3. 发明授权

US5602106A 16-membered macrolide derivatives 失效
标题翻译： 16元大环内酯衍生物
公开(公告)号：US5602106A
公开(公告)日：1997-02-11
申请号：US271996
申请日：1994-07-08
申请人： Keiichi Ajito , Osamu Hara , Ken-ichi Kurihara , Nobue Kikuchi , Minako Araake , Akira Shimizu , Tsuneo Okonogi , Shigeharu Inouye , Seiji Shibahara
发明人： Keiichi Ajito , Osamu Hara , Ken-ichi Kurihara , Nobue Kikuchi , Minako Araake , Akira Shimizu , Tsuneo Okonogi , Shigeharu Inouye , Seiji Shibahara
IPC分类号： C07H17/08 , A61K31/70
CPC分类号： C07H17/08
摘要： 16-membered macrolide derivatives represented by the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a substituent group which protects a hydroxyl group; R.sup.2 represents a hydrogen atom or a substituent group which protects a hydroxyl group; R.sup.3 represents a hydrogen atom or a straight-chain aliphatic acyl group having 2 to 4 carbon atoms; and R.sup.4 represents a hydrogen atom or a straight-chain aliphatic or aromatic acyl group having 1 to 10 carbon atoms;or a pharmaceutically acceptable salt thereof are disclosed.A novel process for producing these 16-membered macrolide derivatives is also disclosed.
摘要翻译：由式（I）表示的16元大环内酯衍生物：其中R 1表示氢原子或保护羟基的取代基; R2表示氢原子或保护羟基的取代基; R3表示氢原子或碳原子数2〜4的直链脂肪族酰基， R 4表示氢原子或碳原子数1〜10的直链脂肪族或芳香族酰基，或其药学上可接受的盐。还公开了一种制备这些16元大环内酯衍生物的新方法。

4. 发明授权

US5200407A Azole derivatives and anti-ulcerative composition containing same 失效
标题翻译：唑衍生物和含有其的抗溃疡组合物
公开(公告)号：US5200407A
公开(公告)日：1993-04-06
申请号：US716621
申请日：1991-06-14
申请人： Kiyoaki Katano , Tamako Tomomoto , Hiroko Ogino , Naoki Yamazaki , Fumiya Hirano , Yasukatsu Yuda , Fukio Konno , Motohiro Nishio , Tomoya Machinami , Seiji Shibahara , Takashi Tsuruoka , Shigeharu Inouye
发明人： Kiyoaki Katano , Tamako Tomomoto , Hiroko Ogino , Naoki Yamazaki , Fumiya Hirano , Yasukatsu Yuda , Fukio Konno , Motohiro Nishio , Tomoya Machinami , Seiji Shibahara , Takashi Tsuruoka , Shigeharu Inouye
IPC分类号： C07D471/04 , C07D498/04 , C07D513/04
CPC分类号： C07D471/04 , C07D513/04
摘要： Compounds of the general formula (I): ##STR1## and pharmaceutically acceptable salts thereof, in which A, B, C and D each represent --CH.dbd. or --N.dbd., with the proviso that at least one of them is --N.dbd.;X represents --NH--, --O-- or --S--;Y represents --(CH.sub.2).sub.p -- wherein p is an integer from 0 to 4, --C(CH.sub.3).sub.2 --, --CH.sub.2 CH.dbd.CH--, --CH.sub.2 CO--, --CF.sub.2 -- or --CH.sub.2 COCH.sub.2 --;R.sup.1 represents a hydrogen atom, a C.sub.1-4 alkyl group, a halogen atom or a C.sub.1-4 alkoxy group;R.sup.2 represents a hydrogen atom, a hydroxyl group, a saturated or unsaturated C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a carboxyl group, a saturated or unsaturated C.sub.1-12 alkoxycarbonyl group which may be optionally substituted, a cycloalkoxycarbonyl group, a saturated or unsaturated five- or six-membered heterocyclic group containing at least one nitrogen atom optionally with one or more nitrogen and/or oxygen atoms, which may be optionally condensed and/or substituted, --CONR.sup.3 R.sup.4, --NR.sup.3 R.sup.4, --OCOR.sup.3 or --NHCONHR.sup.3 wherein R.sup.3 and R.sup.4, which may be the same or different, represent a C.sub.1-6 alkyl group which may be optionally substituted or a cycloalkyl group, andm and n each represent an integer from 0 to 2.
摘要翻译：通式（I）的化合物：其中A，B，C和D各自表示-CH =或-N =，条件是其中至少一个为 -N =; X表示-NH-，-O-或-S-; Y表示 - （CH 2）p - ，其中p是0至4的整数，-C（CH 3）2 - ， - CH 2 CH = CH - ， - CH 2 CO - ， - CF 2 - 或-CH 2 COCH 2 - R1表示氢原子，C1-4烷基，卤素原子或C1-4烷氧基; R2表示氢原子，羟基，饱和或不饱和的C1-6烷基，C1-6烷氧基，羧基，可以任意取代的饱和或不饱和的C 1-12烷氧基羰基，环烷氧基羰基，含有至少一个氮原子的饱和或不饱和五元或六元杂环基，任选具有一个或多个氮和/或氧原子，其可以任选地被缩合和/或取代，-CONR 3 R 4，-NR 3 R 4，-OCOR 3或 - NHCONHR 3其中R3和R4可以相同或不同，表示可以被任意取代的C 1-6烷基或环烷基，m和n各自表示0〜2的整数。

5. 发明授权

US5079255A Thiazolo [4,5-6] pyridine derivatives and anti-ulcerative composition containing same 失效
标题翻译：噻唑（4,5-6）吡啶衍生物和含有其的抗 - 组合物
公开(公告)号：US5079255A
公开(公告)日：1992-01-07
申请号：US544671
申请日：1990-06-27
申请人： Kiyoaki Katano , Tamako Tomomoto , Hiroko Ogino , Yamazaki Naoki , Fumiya Hirano , Yasukatsu Yuda , Fukio Konno , Motohiro Nishio , Tomoya Machinami , Seiji Shibahara , Takashi Tsuruoka , Shigeharu Inouye
发明人： Kiyoaki Katano , Tamako Tomomoto , Hiroko Ogino , Yamazaki Naoki , Fumiya Hirano , Yasukatsu Yuda , Fukio Konno , Motohiro Nishio , Tomoya Machinami , Seiji Shibahara , Takashi Tsuruoka , Shigeharu Inouye
IPC分类号： C07D487/04 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61P1/04 , C07D471/04 , C07D498/04 , C07D513/04
CPC分类号： C07D471/04 , C07D513/04
摘要： Compounds of the general formula (I): ##STR1## and pharmaceutically acceptable salts thereof, in which A, B, C and D each represent --CH.dbd. or --N.dbd., with the proviso that at least one of them is --N.dbd.;X represents --NH--, --O-- or --S--;Y represents --(CH.sub.2).sub.p -- wherein p is an integer from 0 to 4, --C(CH.sub.3).sub.2 --, --CH.sub.2 CH.dbd.CH--, --CH.sub.2 CO--, --CF.sub.2 -- or --CH.sub.2 COCH.sub.2 --;R.sup.1 represents a hydrogen atom, a C.sub.1-4 alkyl group, a halogen atom or a C.sub.1-4 alkoxy group;R.sup.2 represents a hydrogen atom, a hydroxyl group, a saturated or unsaturated C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a carboxyl group, a saturated or unsaturated C.sub.1-12 alkoxycarbonyl group which may be optionally substituted, a cycloalkoxycarbonyl group, a saturated or unsaturated five- or six-membered heterocyclic group containing at least one nitrogen atom optionally with one or more nitrogen and/or oxygen atoms, which may be optionally condensed and/or substituted, --CONR.sup.3 R.sup.4, --NR.sup.3 R.sup.4, --OCOR.sup.3 or --NHCONHR.sup.3 wherein R.sup.3 and R.sup.4, which may be the same or different, represent a C.sub.1-6 alkyl group which may be optionally substituted or a cycloalkyl group, andm and n each represent an integer from 0 to 2.

6. 发明授权

US5061702A Cephem compound as an antimicrobial agent 失效
标题翻译： CEPHEM化合物作为抗微生物剂
公开(公告)号：US5061702A
公开(公告)日：1991-10-29
申请号：US402814
申请日：1989-09-05
申请人： Kunio Atsumi , Katsuyoshi Iwamatsu , Kenji Sakagami , Takashi Yoshida , Haruo Yamamoto , Seiji Shibahara , Shigeharu Inouye
发明人： Kunio Atsumi , Katsuyoshi Iwamatsu , Kenji Sakagami , Takashi Yoshida , Haruo Yamamoto , Seiji Shibahara , Shigeharu Inouye
IPC分类号： C07D501/22 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/04 , C07D501/06 , C07D501/24
CPC分类号： C07D501/24 , Y02P20/55
摘要： A novel cephem compound which has antimicrobial activity is disclosed. The cephem compound is represented by the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom or a carboxyl group; R.sup.2 and R.sup.3, which may be the same or different, each represent a hydrogen atom or a lower alkyl group of 1-3 carbon atoms; and R.sup.4 and R.sup.5, which may be the same or different, each represent a hydrogen atom or an acyl group; and pharmaceutically acceptable salts thereof.

7. 发明授权

US5194617A 2,3-disubstituted-4-hydroxyquinoline derivatives 失效
标题翻译： 2,3-二取代-4-羟基喹啉衍生物
公开(公告)号：US5194617A
公开(公告)日：1993-03-16
申请号：US807946
申请日：1991-12-10
申请人： Nobuto Minowa , Tomoya Machinami , Takashi Shomura , Masaji Sezaki , Toru Sasaki , Seiji Shibahara , Shigeharu Inouye
发明人： Nobuto Minowa , Tomoya Machinami , Takashi Shomura , Masaji Sezaki , Toru Sasaki , Seiji Shibahara , Shigeharu Inouye
IPC分类号： C07D215/22 , C07D215/233
CPC分类号： C07D215/233
摘要： 2,3-disubstituted-4-hydroxyquinoline derivatives of the general formula (I): ##STR1## [wherein R.sup.1 represents a hydrogen atom or R.sup.3 CO-- (wherein R.sup.3 is a lower alkyl group); R.sup.2 represents a hydrogen atom, --CH.sub.3 or --C.sub.2 H.sub.5 ; A represents ##STR2## and W represents a hydrogen atom, or 1- 4 halogen atoms or alkyl groups which are substituted at the nucleus and may be the same or different] have a strong antagonistic action on leukotriene D.sub.4.
摘要翻译：（I）的2,3-二取代-4-羟基喹啉衍生物：其中R1表示氢原子或R3CO-（其中R3是低级烷基）; R 2表示氢原子，-CH 3或-C 2 H 5; A表示，W表示氢原子或1-4个卤原子或在核上被取代且可相同或不同的烷基对白三烯D4具有强拮抗作用。

8. 发明授权

US5141946A Azole derivatives and anti-ulcerative composition containing same 失效
标题翻译：唑衍生物和含有其的抗溃疡组合物
公开(公告)号：US5141946A
公开(公告)日：1992-08-25
申请号：US716622
申请日：1991-06-14
申请人： Kiyoaki Katano , Tamako Tomomoto , Hiroko Ogino , Naoki Yamazaki , Fumiya Hirano , Yasukatsu Yuda , Fukio Konno , Motohiro Nishio , Tomoya Machinami , Seiji Shibahara , Takashi Tsuruoka , Shigeharu Inouye
发明人： Kiyoaki Katano , Tamako Tomomoto , Hiroko Ogino , Naoki Yamazaki , Fumiya Hirano , Yasukatsu Yuda , Fukio Konno , Motohiro Nishio , Tomoya Machinami , Seiji Shibahara , Takashi Tsuruoka , Shigeharu Inouye
IPC分类号： C07D487/04 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61P1/04 , C07D471/04 , C07D498/04 , C07D513/04
CPC分类号： C07D471/04 , C07D513/04
摘要： Compounds of the general formula (I): ##STR1## and pharmaceutically acceptable salts thereof, in whichA, B, C and D each represent --CH.dbd. or --N.dbd., with the proviso that at least one of them is --N.dbd.;X represents --NH--, --O-- or --S--;Y represents --(CH.sub.2).sub.p -- wherein p is an integer from 0 to 4, --C(CH.sub.3).sub.2 --, --CH.sub.2 CH.dbd.CH--, --CH.sub.2 CO--, --CF.sub.2 -- or --CH.sub.2 COCH.sub.2 --;R.sup.1 represents a hydrogen atom, a C.sub.1-4 alkyl group, a halogen atom or a C.sub.1-4 alkoxy group;R.sup.2 represnts a hydrogen atom, a hydroxyl group, a saturated or unsaturated C.sub.1-6 alkyl group, a C.sub.1-6 alkoxy group, a carboxyl group, a saturated or unsaturated C.sub.1-12 alkoxycarbonyl group which may be optionally substituted, a cycloalkoxycarbonyl group, a saturated or unsaturated five- or six-memebered heterocyclic group containing at least one nitrogen atom optionally with one or more nitrogen and/or oxygen atoms, which may be optionally condensed and/or substituted, --CONR.sup.3 R.sup.4, --NR.sup.3 R.sup.4, --OCOR.sup.3 or --NHCONHR.sup.3 wherein R.sup.3 and R.sup.4, which may be the same or different, represent a C.sub.1-6 alkyl group which may be optionally substituted or a cycloalkyl group, andm and n each represent an integrer from 0 to 2.The compounds are useful in treating ulcers.
摘要翻译：通式（I）的化合物：其中A，B，C和D各自表示-CH =或-N =，条件是其中至少一个为 -N =; X表示-NH-，-O-或-S-; Y表示 - （CH 2）p - ，其中p是0至4的整数，-C（CH 3）2 - ， - CH 2 CH = CH - ， - CH 2 CO - ， - CF 2 - 或-CH 2 COCH 2 - R1表示氢原子，C1-4烷基，卤素原子或C1-4烷氧基; R2表示氢原子，羟基，饱和或不饱和的C1-6烷基，C1-6烷氧基，羧基，可以任意取代的饱和或不饱和的C 1-12烷氧基羰基，环烷氧基羰基，含有至少一个氮原子的饱和或不饱和五元或六元杂环基团，任选具有一个或多个氮原子和/或氧原子，其可以任选地被缩合和/或取代，-CONR 3 R 4，-NR 3 R 4，-OCOR 3或 - NHCONHR 3其中R3和R4可以相同或不同，表示可以任选被取代的C 1-6烷基或环烷基，m和n各自表示0至2的整数。该化合物可用于处理溃疡

9. 发明授权

US5190952A 4-acyloxyquinoline derivatives and insecticidal or acaricidal compositions containing same 失效
标题翻译： 4-氰基喹啉衍生物和含有它的杀虫剂或杀胡萝卜素组合物
公开(公告)号：US5190952A
公开(公告)日：1993-03-02
申请号：US549136
申请日：1990-07-05
申请人： Nobuto Minowa , Tomoya Machinami , Seiji Shibahara , Keiichi Imamura , Michiaki Iwata , Masaru Shimura , Shigeharu Inouye
发明人： Nobuto Minowa , Tomoya Machinami , Seiji Shibahara , Keiichi Imamura , Michiaki Iwata , Masaru Shimura , Shigeharu Inouye
IPC分类号： C07D215/22 , A01N43/42 , A01N47/06 , A01N53/00 , C07D215/233 , C07D215/56 , C07D219/06 , C07D405/12 , C07D409/12
CPC分类号： C07D215/233 , A01N43/42 , A01N47/06 , A01N53/00 , C07D215/56 , C07D219/06 , C07D405/12 , C07D409/12
摘要： A 4-acyloxyquinoline derivative represented by the general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.18 alkyl, C.sub.2 -C.sub.18 alkenyl, C.sub.3 -C.sub.10 cycloalkyl which may be optionally substituted, phenylloweralkyl, phenoxyloweralkyl, aryl group, a group OR.sup.4, where R.sup.4 represents a lower alkyl or aryl group, or a group ##STR2## where X represents an oxygen or a sulphur atom; R.sup.2 represents a hydrogen atom, a lower alkyl alkyl group or a group --COOR.sup.5 where R.sup.5 represents a hydrogen atom or a lower alkyl group; R.sup.3 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl or C.sub.2 -C.sub.10 alkenyl group, provided that R.sup.1 does not represent OR.sup.4 when R.sup.2 is a hydrogen atom and R.sup.3 is methyl; R.sup.2 and R.sup.3 together represent a group (CH.sub.2).sub.m, wherein m is 3 or 4, and W represents a hydrogen atom, 1 to 4 halogen atoms, a lower alkyl or lower alkoxy group which may be the same or different and with which the left-hand nucleus is substituted, provided that the compound wherein R.sup.1 represents methyl, R.sup.2, R.sup.3 and W each represent a hydrogen atom is excluded.

10. 发明授权

US4229448A 5-Substituted picolinic acid derivatives and an anti-hypertensive composition containing the same 失效
标题翻译： 5-取代的吡啶甲酸衍生物和含有它们的抗高血压组合物
公开(公告)号：US4229448A
公开(公告)日：1980-10-21
申请号：US23504
申请日：1979-03-23
申请人： Yasuharu Sekizawa , Takashi Tsuruoka , Mitsugu Hachisu , Masaji Sezaki , Masashi Miyamoto , Uichi Shibata , Kazuko Mizutani , Shigeharu Inouye , Takemi Koeda , Keizo Shimomura , Taro Niida
发明人： Yasuharu Sekizawa , Takashi Tsuruoka , Mitsugu Hachisu , Masaji Sezaki , Masashi Miyamoto , Uichi Shibata , Kazuko Mizutani , Shigeharu Inouye , Takemi Koeda , Keizo Shimomura , Taro Niida
IPC分类号： C07D213/65 , C07D213/79 , C07D213/81 , A61K31/455
CPC分类号： C07D213/79 , C07D213/65 , C07D213/81
摘要： 5-Substituted picolinic acid derivatives represented by the formula (I): ##STR1## wherein R.sub.1 represents a straight or branched chain halogen-substituted alkyl group having 2 to 6 carbon atoms or a substituted phenyl group having the formula ##STR2## wherein R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, an amino group, an N-alkyl-substituted amino group, an acylamino group, an acetyl group, an acyloxy group, a hydroxy group or a halogen-substituted alkyl group or R.sub.3 and R.sub.4, when taken together, represent a polymethylene chain; and R.sub.2 represents an --OM group wherein M represents a hydrogen, sodium, potassium, calcium, aluminium or magnesium atom, a straight or branched chain or cyclic alkoxy group having 1 to 6 carbon atoms, an aminoalkoxy group, a phenoxy group, a substituted phenoxy group, a 5-indanyloxy group, an acyloxyalkyloxy group having the formula ##STR3## wherein R.sub.5 represents a hydrogen atom or a methyl group and R.sub.6 represents a lower alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group, or an amino group represented by the formula ##STR4## wherein R.sub.7 and R.sub.8, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a phenyl group which are useful as anti-hypertensive agents, a process for preparing the above 5-substituted picolinic acid derivatives, and anti-hypertensive compositions containing the same.
摘要翻译：由式（I）表示的5-取代的吡啶甲酸衍生物：其中R 1表示具有2至6个碳原子的直链或支链卤素取代的烷基或具有下式的取代苯基：其中可以相同或不同的R 3和R 4各自表示氢原子，卤素原子，低级烷基，低级烷氧基，硝基，氨基，N-烷基取代的氨基，酰氨基，乙酰基，酰氧基，羟基或卤素取代的烷基，或者R 3和R 4一起表示聚亚甲基链; R 2表示-OM基，其中M表示氢，钠，钾，钙，铝或镁原子，具有1至6个碳原子的直链或支链或环状烷氧基，氨基烷氧基，苯氧基，取代的苯氧基，5-茚满氧基，具有式“IMAGE”的酰氧基烷氧基，其中R5表示氢原子或甲基，R6表示碳原子数1〜6的低级烷基，苯基或取代苯基或由式“IMAGE”表示的氨基，其中R7和R8可以相同或不同，表示可用作抗高血压剂的氢原子，低级烷基或苯基，制备上述5-取代的吡啶甲酸衍生物的方法和含有它们的抗高血压组合物。

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