专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 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。

2. 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。

3. 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.

4. 发明授权

US5294705A Process for the preparation of a 3-substituted thio-3-cephem compound 失效
标题翻译： 3-取代的硫代-3-头孢烯化合物的制备方法
公开(公告)号：US5294705A
公开(公告)日：1994-03-15
申请号：US853730
申请日：1992-06-03
申请人： Yuichi Yamamoto , Tsuneo Okonogi , Seiji Shibahara , Shigeharu Inoue
发明人： Yuichi Yamamoto , Tsuneo Okonogi , Seiji Shibahara , Shigeharu Inoue
IPC分类号： C07D501/00 , C07D501/04 , C07D501/59
CPC分类号： C07D501/00 , Y02P20/55
摘要： An ester of 7-acylamido-3-acylthio-3- or -2-cephem-4-carboxylic acid represented by general formula (1) ##STR1## wherein R.sup.1 is an acyl group, R.sup.2 is a carboxyl-protecting group, R.sup.3 is a lower alkyl group, an aryl group or a substituted aryl group, or a mixture of two or more of said ester is used as the starting compound and is reacted wit a tertiary amine and also a secondary amine. Then the tertiary amine salt compound as formed as the reaction product is reacted with a compound of formula (4)R.sup.4 --X (4)wherein R.sup.4 is a lower alkyl group, a cycloalkyl group or a heterocyclic group or a heterocyclic group-substituted methyl group and X is a leaving group, whereby the desired ester of 7-acylamido-3-substituted thio-3-cephem-4-carboxylic acid of formula (5) ##STR2## can be produced preferentially, conveniently and efficiently.
摘要翻译： PCT No.PCT / JP90 / 01599 Sec。 371日期：1992年6月3日 102（e）日期1992年6月3日PCT 1990年12月7日PCT PCT。公开号WO91 / 09037 1991年6月27日，由通式（1）表示的7-酰基氨基-3-酰硫基-3-或2-头孢烯-4-羧酸酯（*化学结构*）（1）其中R1为酰基，R2为羧基保护基，R3为低级烷基，芳基或取代芳基，或两种或多种所述酯的混合物用作起始化合物，并与叔胺以及仲胺。然后将作为反应产物形成的叔胺盐化合物与式（4）R4-X（4）的化合物反应，其中R4是低级烷基，环烷基或杂环基或杂环基取代的甲基并且X是离去基团，由此可以优选地，方便地制备所需的式（5）的7-酰基酰胺基-3-取代的硫代-3-头孢烯-4-羧酸的酯（*化学结构*）（5）并有效地。

5. 发明授权

US5332731A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5332731A
公开(公告)日：1994-07-26
申请号：US623215
申请日：1990-12-06
申请人： Yuichi Yamamoto , Tsuneo Okonogi , Seiji Shibahara , Shigeharu Inoue
发明人： Yuichi Yamamoto , Tsuneo Okonogi , Seiji Shibahara , Shigeharu Inoue
IPC分类号： C07D501/00 , C07D501/59 , C07D501/36
CPC分类号： C07D501/00
摘要： A new class of cephalosporin derivatives is provided, which is useful as antibacterial agent to be particularly suitable for oral administrations in mammals including man, and which is represented by general formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkyl group; R.sup.2 is a hydrogen atom or an ester-forming group capable of being cleaved easily with an esterase existing in the digestive tracts; n is an integer of zero or 1; Z is a saturated heterocyclic group containing one or two oxygen atoms as the hetero-atoms with or without one or more lower alkyl substituents, or a pharmaceutically acceptable salt thereof.
摘要翻译：提供了一类新的头孢菌素衍生物，其可用作特别适合于包括人在内的哺乳动物的口服给药的抗菌剂，其由通式（I）表示，其中R 1是氢原子或低级烷基; R2是能够容易地与存在于消化道中的酯酶裂解的氢原子或成酯基团; n是0或1的整数; Z是含有一个或两个氧原子作为具有或不具有一个或多个低级烷基取代基的杂原子的饱和杂环基，或其药学上可接受的盐。

6. 发明授权

US4785090A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4785090A
公开(公告)日：1988-11-15
申请号：US704077
申请日：1985-02-21
申请人： Takashi Tsuruoka , Seiji Shibahara , Katsuyoshi Iwamatsu , Tsuneo Okonogi , Satoru Nakabayashi , Yasushi Murai , Hiroko Ogino , Kiyoaki Katano , Takashi Yoshida , Shigeharu Inoue , Shunzo Fukatsu , Shinichi Kondo
发明人： Takashi Tsuruoka , Seiji Shibahara , Katsuyoshi Iwamatsu , Tsuneo Okonogi , Satoru Nakabayashi , Yasushi Murai , Hiroko Ogino , Kiyoaki Katano , Takashi Yoshida , Shigeharu Inoue , Shunzo Fukatsu , Shinichi Kondo
IPC分类号： C07D213/64 , C07D213/68 , C07D221/04 , C07D501/36 , C07D501/38 , A61K31/545
CPC分类号： C07D221/04 , C07D213/64 , C07D213/68
摘要： This is a class of antibacterial compounds of the formula: ##STR1## wherein Y is straight or branched alkyl or alkenyl chain, cycloalkanomethyl of 3-6 carbon atoms, each group being optionally substituted by halogen, or a group ##STR2## wherein n is 0 or an integer of 1-3, A is a group --COR.sup.3 wherein R.sup.3 is hydroxy, a group ##STR3## wherein R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or alkyl of 1-5 carbon atoms, a group ##STR4## or a 5- or 6-membered heterocyclic group containing nitrogen and/or sulfur, and R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, alkyl of 1-5 carbon atoms, or R.sup.1 and R.sup.2 may be combined together to form cycloalkylidene of 3-5 carbon atoms, and Z is a group of the formula: ##STR5## wherein m is 0 or an integer of 3-5, R.sup.6 is hydrogen or alkyl of 1-3 carbon atoms, and R.sup.7, when m is an integer of 3-5, is alkyl of 1-5 carbon atoms, alkenyl, cyclopropyl, a group --(CH.sub.2).sub.p B wherein p is 0 or an integer of 1-3 and B is amino, alkyl-substituted amino, hydroxy, carboxy, carbamoyl, trifluoromethyl, sulfonic acid, sulfonic acid amide, alkylthio or cyano or, when m is 0, is alkyl of 1-5 carbon atoms, which may optionally be substituted by halogen, alkenyl, a group ##STR6## wherein R.sup.8 is hydrogen, alkyl of 1-4 carbon atoms or phenyl, or cyclopropyl, and a salt thereof.
摘要翻译：这是一类具有下式的抗菌化合物：其中Y是直链或支链烷基或烯基链，3-6个碳原子的环烷基甲基，每个基团任选被卤素取代，或基团< 其中n为0或1-3的整数，A为基团-COR 3，其中R 3为羟基，其中R 4和R 5可以相同或不同，为氢或1-5碳的烷基原子，基团或含有氮和/或硫的5-或6-元杂环基，R 1和R 2可以相同或不同，为氢，1-5个碳原子的烷基或R1 并且R 2可以组合在一起形成3-5个碳原子的亚烷基，Z是下式的基团：其中m是0或3-5的整数，R6是氢或1-3个碳的烷基原子和R 7，当m是3-5的整数时，是1-5个碳原子的烷基，烯基，环丙基，基团 - （CH 2）pB，其中p是0或1-3的整数，B是氨基，烷基取代的氨基羟基，羧基，氨基甲酰基，三氟甲基，磺酸，磺酸酰胺，烷硫基或氰基，或当m为0时，其为1-5个碳原子的烷基，其可任选被卤素，链烯基，基团其中R8是氢，1-4个碳原子的烷基或苯基，或环丙基及其盐。

7. 发明授权

US4534898A 1-Oxa-1-dethia-cephalosporin derivatives 失效
标题翻译： 1-氧杂-1-脱氢头孢菌素衍生物
公开(公告)号：US4534898A
公开(公告)日：1985-08-13
申请号：US515422
申请日：1983-07-20
申请人： Seiji Shibahara , Tsuneo Okonogi , Yasushi Murai , Shunzo Fukatsu , Tadashi Wakazawa , Taro Niida , Burton G. Christensen
发明人： Seiji Shibahara , Tsuneo Okonogi , Yasushi Murai , Shunzo Fukatsu , Tadashi Wakazawa , Taro Niida , Burton G. Christensen
IPC分类号： C07D498/04 , C07D205/085 , C07D403/12 , C07D505/00 , C07F9/568 , C07D419/14
CPC分类号： C07D403/12 , C07D205/085 , C07D505/00 , C07F9/5683
摘要： This invention relates to 1-oxa-1-dethia-cephalosporins which are useful as anti-biotics.
摘要翻译：本发明涉及可用作抗生物素的1-氧杂-1-脱氢头孢菌素。

8. 发明授权

US5547978A Derivatives of pyrrolidin-2-ylcarbonylheterocyclic compounds 失效
标题翻译：吡咯烷-2-基羰基杂环化合物的衍生物
公开(公告)号：US5547978A
公开(公告)日：1996-08-20
申请号：US346240
申请日：1994-11-23
申请人： Burton G. Christensen , Takashi Egawa , Yasuyuki Ichimaru , Shokichi Ohuchi , Tsuneo Okonogi , Arthur A. Patchett , Seiji Shibahara , Seiji Tsutsumni
发明人： Burton G. Christensen , Takashi Egawa , Yasuyuki Ichimaru , Shokichi Ohuchi , Tsuneo Okonogi , Arthur A. Patchett , Seiji Shibahara , Seiji Tsutsumni
IPC分类号： A61K31/40 , A61K31/401 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/505 , A61P25/00 , A61P25/28 , C07D401/14 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D498/04 , C07D207/06 , C07D209/08 , C07D277/06
CPC分类号： C07D401/14 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention relates to derivatives of pyrrolidin-2-ylcarbonylheterocyclic compound of the general formula ##STR1## in which R.sup.1 represents C.sub.1-6 alkyl, C.sub.1-20 cycloalkyl, aryl or heteroaryl,R.sup.2 represents a heterocyclic compound selected from the group consisting of 2-thiazole, 2-oxazole, 2-imidazole, 2-pyrrole, 2-thiophene, 2-benzothiazole, 2-benzoxazole, 2-benzimidazole, 2-indole, 2-thiazolo[5,4-b]pyridine, 2-oxazolo[4,5-b]pyridine, 2-imidazo[4,5-b]pyridine, 5-thiazole, 2-thiazoline, 2-pyridine, 3-pyridine, 5-pyrimidine, 2-pyrazine, 2-triazole or 2-pyrazole wherein the heterocyclic compound may be unsubstituted or substituted independently with R.sup.4 or R.sup.5 wherein R.sup.4 and R.sup.5 are H, C.sub.1-5 alkyl, aryl or R.sup.4 and R.sup.5 may be ortho substituents on the heterocyclic compounds and connected to form an aryl or heteroaryl ring,A represents a cyclic amino acid, X is oxygen atom, thiomethlene or methylene residue, m is an integer from 1 to 5, to a process for the preparation thereof, to composition containing them, and to the use thereof.
摘要翻译：本发明涉及通式“IMAGE”的吡咯烷-2-基羰基杂环化合物的衍生物，其中R 1表示C 1-6烷基，C 1-20的环烷基，芳基或杂芳基，R 2表示选自下列的杂环化合物：2- 噻唑，2-恶唑，2-咪唑，2-吡咯，2-噻吩，2-苯并噻唑，2-苯并恶唑，2-苯并咪唑，2-吲哚，2-噻唑并[5,4-b]吡啶，2-恶唑并[ 4,5-b]吡啶，2-咪唑并[4,5-b]吡啶，5-噻唑，2-噻唑啉，2-吡啶，3-吡啶，5-嘧啶，2-吡嗪，2-三唑或2- 吡唑，其中杂环化合物可以是未取代的或独立地被R4或R5取代，其中R4和R5是H，C1-5烷基，芳基或R4和R5可以是杂环化合物上的邻位取代基并且连接形成芳基或杂芳基环， A表示环状氨基酸，X为氧原子，巯基或亚甲基残基，m为1〜5的整数，其制备方法为组合物cont 指导他们，以及使用它们。

9. 发明授权

US4810702A Antibacterial agent for mammal use comprising cephalosporin derivatives as an effective ingredient 失效
标题翻译：哺乳动物用抗菌剂包括头孢菌素衍生物作为有效成分
公开(公告)号：US4810702A
公开(公告)日：1989-03-07
申请号：US131779
申请日：1987-12-11
申请人： Seiji Shibahara , Tsuneo Okonogi , Yasushi Murai , Toshiaki Kudo , Takashi Yoshida , Ken Nishihata , Shinichi Kondo
发明人： Seiji Shibahara , Tsuneo Okonogi , Yasushi Murai , Toshiaki Kudo , Takashi Yoshida , Ken Nishihata , Shinichi Kondo
IPC分类号： A61K31/435 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/36
CPC分类号： C07D501/36
摘要： Cephalosporin compounds having 2-(2-aminothiazol-4-yl)-2{(1S)-carboxyethoxyimino}acetyl group on the side chain at the 7-position thereof and 1-ethylpyridinium-4-ylthiomethyl group on the side chain at the 3-position thereof or non-toxic salts thereof are excellent antibacterial agents for mammals including human. The cephalosporin derivatives have low toxicity.

10. 发明授权

US4472576A Processes for the production of antibiotic 1-oxadethiacephalosporins 失效
标题翻译：用于生产抗生素1-恶二硫醚类的方法
公开(公告)号：US4472576A
公开(公告)日：1984-09-18
申请号：US446534
申请日：1982-12-03
申请人： Tadashi Wakazawa , Taro Niida , Shunzo Fukatsu , Yasushi Murai , Tsuneo Okonogi , Seiji Shibahara
发明人： Tadashi Wakazawa , Taro Niida , Shunzo Fukatsu , Yasushi Murai , Tsuneo Okonogi , Seiji Shibahara
IPC分类号： C07D205/085 , C07D505/00 , C07D498/04
CPC分类号： C07D505/00 , C07D205/085 , Y02P20/55
摘要： Disclosed is a process for preparing antibiotic 1-oxadethiacephalosporins via diazo-species I: ##STR1## wherein: A is acyl; R.sup.1 is H or OCH.sub.3 ; and R.sup.2 is a protecting group.
摘要翻译：本发明公开了一种通过重氮种I制备抗生素1-恶二硫醚类的方法：其中：A为酰基; R1是H或OCH3; R2是保护基。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式