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11. 发明授权

US5444174A 16-membered macrolide derivative having sustained antibacterial activity in plasma, synthesis intermediate thereof and process for producing the same 失效
标题翻译：在血浆中具有持续抗菌活性的16元大环内酯衍生物及其合成中间体及其制备方法
公开(公告)号：US5444174A
公开(公告)日：1995-08-22
申请号：US22165
申请日：1993-02-25
申请人： Keiichi Ajito , Kenichi Kurihara , Tsuneo Ishizuka , Tetsuro Hara , Takayuki Usui , Seiji Shibahara
发明人： Keiichi Ajito , Kenichi Kurihara , Tsuneo Ishizuka , Tetsuro Hara , Takayuki Usui , Seiji Shibahara
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7048 , A61P31/04 , C07H17/08 , C07D313/06
CPC分类号： C07H17/08
摘要： 16-membered macrolide compounds wherein both of hydroxyl groups at the 3"- and 4"-positions form ether bonds together with two alkyl groups which are either the same or different from each other is useful as an antibacterial agent. The macrolide compounds represented by formula (I) are prepared by chemically modifying midecamycin A.sub.3 to obtain a synthesis intermediate of the formula (II), which is further chemically modified. ##STR1##
摘要翻译： 3“和4”位上的两个羟基与其彼此相同或不同的两个烷基形成醚键的16元大环内酯化合物可用作抗菌剂。由式（I）表示的大环内酯化合物通过化学修饰麦地卡霉素A3制备得到式（II）的合成中间体，其进一步化学修饰。（一）

12. 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。

13. 发明授权

US5607927A Cephalosporin derivative 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5607927A
公开(公告)日：1997-03-04
申请号：US385363
申请日：1995-02-07
申请人： Masaki Tsushima , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
发明人： Masaki Tsushima , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/59 , C07D519/00 , C07D519/06 , C07D501/36
CPC分类号： C07D501/00 , Y02P20/55
摘要： An aminothiazolyl- or aminothiadiazolyl-cephalosporin derivative represented by the following general formula (I) which has a condensed-ring thio group as a 3-positioned substituent group that contains a thiazolylthio group, an oxazolylthio group or a heterocyclic ring thereof as one of the ring components. The compound according to the present invention has excellent activities to inhibit growth of various bacteria, especially Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA), and therefore, the antibacterial agent comprising, as an active ingredient, the inventive compound can be used as a therapeutic drug for the treatment of various bacterial infections. ##STR1##
摘要翻译：作为下述通式（I）表示的氨基噻唑基 - 或氨基噻二唑基 - 头孢菌素衍生物，其具有稠环硫基作为含有噻唑基硫基，恶唑基硫基或其杂环的3位取代基环组件。根据本发明的化合物具有优异的抑制各种细菌，特别是耐甲氧西林金黄色葡萄球菌（MRSA）的革兰氏阳性菌生长的活性，因此作为本发明化合物作为活性成分的抗菌剂可以是用作治疗各种细菌感染的治疗药物。

14. 发明授权

US5827845A Cephalosporin derivative 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5827845A
公开(公告)日：1998-10-27
申请号：US617870
申请日：1996-07-31
申请人： Sohjiro Shiokawa , Kunio Atsumi , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
发明人： Sohjiro Shiokawa , Kunio Atsumi , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
IPC分类号： C07D501/00 , C07D501/24 , C07D501/56 , A61K31/545
CPC分类号： C07D501/00 , Y02P20/55
摘要： A cephalosporin derivative which has a substituted or unsubstituted 2-(5-thiazolyl)vinyl group at the 3-position and is represented by the following formula (I) ##STR1## wherein X is CH or N, R.sup.1 is an amino group or a protected amino group, R.sup.2 is a hydrogen atom or a hydroxyimino-protecting group, R.sup.3 is a hydrogen atom, a salt-forming cation or a carboxyl-protecting group, R.sup.4 is a hydrogen atom, and R.sup.5 is a hydrogen atom, a lower alkyl group, a halo-(lower)alkyl group or a halogen atom, is now synthetised as a cephem compound which exhibits excellent antibacterial activities and is useful as a therapeutic agent for various bacterial infections.
摘要翻译： PCT No.PCT / JP94 / 01618 Sec。 371日期：1996年7月31日 102（e）日期1996年7月31日PCT 1994年9月29日PCT PCT。公开号WO95 / 09171 日期：1995年4月6日，头孢菌素衍生物，其3-位具有取代或未取代的2-（5-噻唑基）乙烯基，由下式（I）表示：其中X为CH或N R1为氨基或被保护的氨基，R2为氢原子或羟基亚氨基保护基，R3为氢原子，成盐阳离子或羧基保护基，R4为氢原子，R5为作为氢原子，低级烷基，卤代（低级）烷基或卤素原子，现在被合成为具有优异抗菌活性的头孢烯化合物，可用作各种细菌感染的治疗剂。

15. 发明授权

US5464829A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5464829A
公开(公告)日：1995-11-07
申请号：US167204
申请日：1993-12-16
申请人： Masaki Tsushima , Yuko Kano , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
发明人： Masaki Tsushima , Yuko Kano , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D519/06 , C07D501/36
CPC分类号： C07D501/00 , Y02P20/55
摘要： A cephalosporin derivative having a quaternary salt type substituent group at the 3-position, represented by formula (I): ##STR1## wherein X is a carbon atom or a nitrogen atom; Y is a sulfur atom, an oxygen atom or a nitrogen atom substituted with a substituted or unsubstituted lower alkyl group; R.sup.1 is a hydrogen atom, a lower alkyl group or a substituted lower alkyl group; R.sup.2 is a lower alkyl group, a substituted lower alkyl group, a lower alkylene group or a substituted lower alkylene group; and A is an unsaturated six-membered heterocyclic ring containing at least one nitrogen atom, or a pharmaceutically acceptable salt thereof is disclosed. The derivatives have excellent antibacterial activities and can be used as a drug for the treatment of various bacterial infections.
摘要翻译：由式（I）表示的3-位具有季盐型取代基的头孢菌素衍生物：其中X为碳原子或氮原子; Y是硫原子，氧原子或被取代或未取代的低级烷基取代的氮原子; R1是氢原子，低级烷基或取代的低级烷基; R2是低级烷基，取代的低级烷基，低级亚烷基或取代的低级亚烷基; 并且A是含有至少一个氮原子的不饱和六元杂环，或其药学上可接受的盐。该衍生物具有优异的抗菌活性，可用作治疗各种细菌感染的药物。

16. 发明授权

US5461044A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5461044A
公开(公告)日：1995-10-24
申请号：US369274
申请日：1995-01-05
申请人： Masaki Tsushima , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
发明人： Masaki Tsushima , Katsuyoshi Iwamatsu , Atsushi Tamura , Seiji Shibahara
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/59
CPC分类号： C07D501/00 , Y02P20/55
摘要： As new antibacterial agent are provided cephalosporin derivatives having a general formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group or a substituted lower alkyl group, R.sup.2 is a hydrogen atom or an ester-forming group easily cleavable by an esterase present in the digestive tracts, R.sup.3 and R.sup.4 may be the same and each is independently a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkenyl group, hydroxyl group, amino group or a lower alkoxy group, and a pharmaceutically acceptable salt thereof.The cephalosporin derivative of formula (I) is useful as an orally or injectably administrable cephalosporin derivative which exhibits in combination a high antibacterial activity and a favorable characteristic capable of giving a high concentration of this compound in blood when administered.
摘要翻译：作为新的抗菌剂，提供具有通式（I）的头孢菌素衍生物：其中R 1为氢原子，低级烷基或取代的低级烷基，R 2为氢原子或酯形成可以通过存在于消化道中的酯酶容易地切割，R3和R4可以相同，各自独立地为氢原子，卤素原子，低级烷基，低级烯基，羟基，氨基或低级烷氧基基团及其药学上可接受的盐。式（I）的头孢菌素衍生物可用作口服或可注射给药的头孢菌素衍生物，其组合具有高的抗菌活性和在给药时能够在血液中给予高浓度该化合物的有利特征。

17. 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。

18. 发明授权

US08318684B2 Antibiotics, bispolides A1, A2, and A3 as well as bispolides B1, B2a, B2b and B3 and processes for producing said antibiotics 有权
标题翻译：抗生素，双酚A，A2和A3以及双酚B1，B2a，B2b和B3以及生产所述抗生素的方法
公开(公告)号：US08318684B2
公开(公告)日：2012-11-27
申请号：US12300468
申请日：2007-05-15
申请人： Keiichi Numata , Noriyuki Okujo , Siew Eim Khor , Lee Li Tan , Annie George , Szu Ting Ng , Chin Jye Tan , Hironobu Iinuma , Yasuo Fukagawa , Kunimoto Hotta , Seiji Shibahara , Shinichi Kondo , Satoshi Nimura
发明人： Keiichi Numata , Noriyuki Okujo , Siew Eim Khor , Lee Li Tan , Annie George , Szu Ting Ng , Chin Jye Tan , Hironobu Iinuma , Yasuo Fukagawa , Kunimoto Hotta , Seiji Shibahara , Shinichi Kondo , Satoshi Nimura
IPC分类号： A61K31/70 , C07H17/08 , C12P19/62
CPC分类号： C07H17/04 , A61K31/04 , A61K31/7048 , C12P17/08 , A61K2300/00
摘要： Seven novel antibiotic substances can be produced by cultivation of a microbial strain which has been isolated from a soil sample and which is designated as Microbispora sp. A 34030 (deposited under an access number FERM BP-10505 in terms of Budapest Treaty). These seven antibiotic substances are named as bispolide A1, bispolide A2, bispolide A3, bispolide B1, bispolide B2a, bispolide B2b and bispolide B3, respectively. These bispolides are each novel compounds which have a chemical structure as collectively represented by the general formula (III) shown below: These bispolides have each a high antibacterial activity against a variety of bacteria, particularly Gram-positive bacteria and their antibiotic-resistant strains, and hence these bispolides each are effective and useful for therapeutically treating bacterial infections of Gram-positive bacteria in humans and animals.
摘要翻译：可以通过培养已经从土壤样品中分离并被称为微双歧杆菌（Microbispora sp。）的微生物菌株来生产七种新型抗生素物质。 A 34030（根据布达佩斯条约保存在访问号FERM BP-10505）。这七种抗生素物质分别被称为双吡啶A1，双吡啶B2，双吡哆醛A3，双吡啶B1，双吡啶B2a，双吡啶B2b和双吡啶B3。这些双吡啶衍生物是具有如以下通式（III）统称为化学结构的新型化合物：这些双酚化物对各种细菌，特别是革兰氏阳性菌及其抗生素抗性菌株具有高抗菌活性，因此这些双吡哆醇各自对于治疗性地治疗人和动物中革兰氏阳性菌的细菌感染是有效和有用的。

19. 发明申请

US20100144658A1 NOVEL ANTIBIOTICS, BISPOLIDES A1, A2, AND A3 AS WELL AS BISPOLIDES B1, B2A, B2B AND B3 AND PROCESSES FOR PRODUCING SAID ANTIBIOTICS 有权
标题翻译：新型抗生素，BISPOLIDES A1，A2和A3作为双酚A B1，B2A，B2B和B3以及生产抗生素的方法
公开(公告)号：US20100144658A1
公开(公告)日：2010-06-10
申请号：US12300468
申请日：2007-05-15
申请人： Keiichi Numata , Noriyuki Okujo , Siew Eim Khor , Lee Li Tan , Annie George , Szu Ting Ng , Chin Jye Tan , Hironobu Iinuma , Yasuo Fukagawa , Kunimoto Hotta , Seiji Shibahara , Shinichi Kondo , Satoshi Nimura
发明人： Keiichi Numata , Noriyuki Okujo , Siew Eim Khor , Lee Li Tan , Annie George , Szu Ting Ng , Chin Jye Tan , Hironobu Iinuma , Yasuo Fukagawa , Kunimoto Hotta , Seiji Shibahara , Shinichi Kondo , Satoshi Nimura
IPC分类号： A61K31/7048 , A61P31/04 , C07H17/08 , C12P19/60 , C12N1/20
CPC分类号： C07H17/04 , A61K31/04 , A61K31/7048 , C12P17/08 , A61K2300/00
摘要： Seven novel antibiotic substances could be produced by cultivation of a microbial strain which has been isolated from a soil sample and which is designated as Microbispora sp. A 34030 (deposited under an access number FERM BP-10505 in terms of Budapest Treaty). These seven antibiotic substances are named as bispolide A1, bispolide A2, bispolide A3, bispolide B1, bispolide B2a, bispolide B2b and bispolide B3, respectively. These bispolides are each novel compounds which have a chemical structure as collectively represented by the general formula (III) shown below. These bispolides have each a high antibacterial activity against a variety of bacteria, particularly Gram-positive bacteria and their antibiotic-resistant strains, and hence these bispolides each are effective and useful for therapeutically treating bacterial infections of Gram-positive bacteria in human and animals.The general formula (III):
摘要翻译：可以通过培养已经从土壤样品中分离并被称为微双歧杆菌（Microbispora sp。）的微生物菌株产生七种新型抗生素物质。 A 34030（根据布达佩斯条约保存在访问号FERM BP-10505）。这七种抗生素物质分别被称为双吡啶A1，双吡啶B2，双吡哆醛A3，双吡啶B1，双吡啶B2a，双吡啶B2b和双吡啶B3。这些双吡啶衍生物是具有如以下通式（III）统称的化学结构的新化合物。这些双糖苷酸各自对各种细菌，特别是革兰氏阳性菌及其抗生素抗性菌株具有高的抗菌活性，因此这些双吡啶苷各自对于治疗性地治疗人和动物中革兰氏阳性菌的细菌感染是有效和有用的。通式（III）：

20. 发明授权

US4971961A Cephalosporin compounds and antibacterial agents 失效
标题翻译：头孢菌素化合物和抗菌剂
公开(公告)号：US4971961A
公开(公告)日：1990-11-20
申请号：US266050
申请日：1988-11-02
申请人： Kaysuyoshi Iwamatsu , Kenji Sakagami , Kunio Atsumi , Takashi Yoshida , Seiji Shibahara , Takashi Tsuruoka , Shinichi Kondo
发明人： Kaysuyoshi Iwamatsu , Kenji Sakagami , Kunio Atsumi , Takashi Yoshida , Seiji Shibahara , Takashi Tsuruoka , Shinichi Kondo
IPC分类号： A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/20 , C07D501/22 , C07D501/24 , C07D501/34 , C07D501/36
CPC分类号： C07D501/00 , Y02P20/55
摘要： This invention provides cephalosporin compounds represented by the following general formula: ##STR1## wherein R.sup.1 and R.sup.2 are same or different hydrogen atom or a lower alkyl group of 1 to 5 carbon atoms; R.sup.3 is a lower alkyl group which may optionally be substituted with a halogen atome (or atoms), an alkenyl group, or a cycloalkylmethyl group of 3 to 6 carbon atoms; and A is hydrogen atom or residue of a nucleophilic compound and pharmacologically acceptable salts thereof. These compounds have broad-spectrum antibacterial activity against Gram-positive and -negative bacteria including Pseudomonas aeruginosa, as well as against a great variety of .beta.-lactamase-producing strains.

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