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公开(公告)号:US09290515B2
公开(公告)日:2016-03-22
申请号:US14349227
申请日:2012-10-03
申请人: SHIONOGI & CO., LTD.
发明人: Kenji Yamawaki , Masayuki Sano , Jun Sato
IPC分类号: C07D501/56 , C07D501/46
CPC分类号: C07D501/56 , C07D501/46
摘要: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof wherein A represents a group represented by one of formulae (i)-(iii); B represents a group represented by formula (v) or (vi); and E represents a substituted or unsubstituted heterocyclic group having a cationic nitrogen atom.
摘要翻译: 由式(I)表示的化合物或其药学上可接受的盐,其中A表示由式(i) - (iii)之一表示的基团; B表示由式(v)或(vi)表示的基团; E表示具有阳离子氮原子的取代或未取代的杂环基。
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公开(公告)号:US09085589B2
公开(公告)日:2015-07-21
申请号:US13642959
申请日:2011-04-27
申请人: Hiroki Kusano , Kenji Yamawaki
发明人: Hiroki Kusano , Kenji Yamawaki
IPC分类号: A61K31/546 , C07D501/56 , C07D501/42 , C07D501/44 , C07D501/46 , C07D519/00 , C07D519/06 , C07D501/54
CPC分类号: C07D501/56 , C07D501/42 , C07D501/44 , C07D501/46 , C07D501/54 , C07D519/00 , C07D519/06
摘要: Provided is a cephem compound which has a wide antimicrobial spectrum, and in particular exhibits potent antimicrobial activity against beta-lactamase producing Gram negative bacteria, and a pharmaceutical composition comprising the same. The cephem compound has the formula (I): where W and U are as defined in the specification; R1 is as defined in the specification; R2A and R2B are as defined in the specification, provided that R2A and R2B are not taken together to form an optionally substituted oxime group when R1 is aminothiazole or aminothiadiazole optionally protected at the amino group; ring A is a benzene ring or a 6-membered aromatic heterocyclic group having 1-3 nitrogen atoms; R3 is a hydrogen atom, —OCH3 or —NH—CH(═O); k is an integer from 0 to 2; R4 is as defined in the specification; and D and E are as defined in accordance with a) or b) described in the specification.
摘要翻译: 本发明提供一种具有广谱抗菌谱的头孢烯化合物,特别是对产生β-内酰胺酶的革兰氏阴性细菌表现出有效的抗微生物活性,以及包含其的药物组合物。 头孢烯化合物具有式(I):其中W和U如说明书中所定义; R1如规范中所定义; R2A和R2B如说明书中所定义,条件是当R 1为氨基噻唑或氨基噻二唑任选在该氨基保护时,R2A和R2B不一起形成任选取代的肟基; 环A是苯环或具有1-3个氮原子的6元芳族杂环基; R3是氢原子,-OCH3或-NH-CH(= O); k是0至2的整数; R4如规范中所定义; 和D和E如在说明书中描述的a)或b)所定义。
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公开(公告)号:US20150025053A1
公开(公告)日:2015-01-22
申请号:US14333966
申请日:2014-07-17
IPC分类号: C07D501/60 , C07D501/04
CPC分类号: C07D501/60 , C07D501/04 , C07D501/56
摘要: The cephalosporin compound of formula (I) is disclosed, which exhibits antibiotic activity against Gram-negative (e.g., Pseudomonas aeruginosa) and Gram-positive (e.g., methicillin-resistant Staphylococcus aureus) bacteria. Methods of manufacturing the compound of formula (I), and uses of the compound in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
摘要翻译: 公开了式(I)的头孢菌素化合物,其表现出抗革兰氏阴性(例如铜绿假单胞菌)和革兰氏阳性(例如耐甲氧西林金黄色葡萄球菌)细菌的抗生素活性。 还公开了制备式(I)化合物的方法,以及该化合物在制备药物组合物和抗菌应用中的用途。
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公开(公告)号:US20140274999A1
公开(公告)日:2014-09-18
申请号:US14211465
申请日:2014-03-14
发明人: Jan-Ji Lai , Pradip M. Pathare , Laxma Kolla , Adrien F. Soret
IPC分类号: C07D501/06 , A61K31/433 , A61K31/546
CPC分类号: C07D501/59 , A61K31/41 , A61K31/426 , A61K31/433 , A61K31/545 , A61K31/546 , A61K31/675 , C07D501/04 , C07D501/06 , C07D501/22 , C07D501/34 , C07D501/36 , C07D501/56 , C07D501/57 , C07F9/65613
摘要: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step.
摘要翻译: 本文提供了一种合成头孢菌素抗生素化合物的方法,包括在单一步骤中将受保护的7-氨基转化为7-甲酰胺部分。
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公开(公告)号:US20130096299A1
公开(公告)日:2013-04-18
申请号:US13642959
申请日:2011-04-27
申请人: Hiroki Kusano , Kenji Yamawaki
发明人: Hiroki Kusano , Kenji Yamawaki
IPC分类号: C07D501/56 , C07D519/06 , C07D501/54
CPC分类号: C07D501/56 , C07D501/42 , C07D501/44 , C07D501/46 , C07D501/54 , C07D519/00 , C07D519/06
摘要: Provided is a cephem compound which has a wide antimicrobial spectrum, and in particular exhibit potent antimicrobial activity against beta-lactamase producing Gram negative bacteria, and pharmaceutical composition comprising the same.A Compound of the formula (I): wherein W and U are as defined in the specification; R1 is as defined in the specification; R2A and R2B are as defined in the specification, provided that R2A and R2B are not taken together to form an optionally substituted oxime group when R1 is aminothiazole or aminothiadiazole optionally protected at the amino group; ring A is a benzene ring or a 6-membered aromatic heterocyclic group having 1-3 nitrogen atoms; R3 is a hydrogen atom, —OCH3 or —NH—CH(═O); k is an integer from 0 to 2; R4 is as defined in the specification; and D and E are as defined in accordance with a) or b) described in the specification.
摘要翻译: 提供了具有广谱抗菌谱的头孢烯化合物,并且特别表现出对产生β-内酰胺酶的革兰氏阴性细菌具有强力的抗微生物活性,以及包含其的药物组合物。 式(I)的化合物:其中W和U如说明书中所定义; R1如规范中所定义; R2A和R2B如说明书中所定义,条件是当R 1为氨基噻唑或氨基噻二唑任选在该氨基保护时,R2A和R2B不一起形成任选取代的肟基; 环A是苯环或具有1-3个氮原子的6元芳族杂环基; R3是氢原子,-OCH3或-NH-CH(= O); k是0至2的整数; R4如规范中所定义; 和D和E如在说明书中描述的a)或b)所定义。
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公开(公告)号:US07384928B2
公开(公告)日:2008-06-10
申请号:US10507502
申请日:2003-03-18
IPC分类号: C07D501/46 , A61K31/546 , A61P31/04 , C07D277/593
CPC分类号: C07D501/56 , A61K31/546 , C07D501/00
摘要: A compound of the formula: (wherein, T is S, SO or O; X is halogen, CN, carbamoyl optionally substituted with lower alkyl, lower alkyl, lower alkoxy, or lower alkylthio; A is substituted lower alkylene (wherein the substituent is optionally substituted mono lower alkyl, optionally substituted lower alkylidene, or optionally substituted lower alkylene); Z+ is an optionally substituted, a cation and an N atom-containing heterocyclic group), ester, amino-protected compound wherein the amino bonds to a thiazole ring at the 7-position, or pharmaceutically acceptable salt or solvate thereof.
摘要翻译: 下式的化合物:其中T是S,SO或O; X是卤素,CN,任选被低级烷基,低级烷基,低级烷氧基或低级烷硫基取代的氨基甲酰基; A是取代的低级亚烷基(其中取代基是 任选取代的单低级烷基,任选取代的低级亚烷基或任选取代的低级亚烷基); Z +是任选取代的阳离子和含N原子的杂环基),酯,氨基保护的化合物 其中氨基与7-位的噻唑环或其药学上可接受的盐或溶剂化物的键合。
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公开(公告)号:US20060287244A1
公开(公告)日:2006-12-21
申请号:US11442027
申请日:2006-05-26
申请人: V. Chandran
发明人: V. Chandran
IPC分类号: A61K38/10 , A61K38/08 , A61K38/05 , A61K38/04 , A61K31/7056 , A61K31/7048 , A61K31/704 , A61K31/337 , A61K31/522 , A61K31/573 , A61K31/496 , A61K31/4745 , A61K31/401 , A61K31/473
CPC分类号: A61K38/12 , A61K38/10 , A61K45/06 , A61K47/542 , C07C229/08 , C07C229/22 , C07C229/26 , C07C229/36 , C07C233/47 , C07C2602/22 , C07D207/33 , C07D209/10 , C07D209/14 , C07D211/34 , C07D211/90 , C07D215/38 , C07D217/26 , C07D223/16 , C07D239/10 , C07D261/20 , C07D265/18 , C07D275/04 , C07D295/185 , C07D311/24 , C07D311/32 , C07D333/58 , C07D401/06 , C07D401/12 , C07D403/10 , C07D405/14 , C07D409/06 , C07D413/06 , C07D473/18 , C07D473/34 , C07D493/04 , C07D493/10 , C07D495/04 , C07D498/06 , C07D498/14 , C07D499/14 , C07D501/22 , C07D501/34 , C07D501/46 , C07D501/56 , C07F9/572 , C07F9/65616
摘要: The present invention is directed to a derivative comprised of an L-Threonine bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. The derivative has the same utility as the drug from which it is made, but it has enhanced therapeutic properties. In fact, the derivatives of the present invention enhance at least one or more therapeutic qualities, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.
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公开(公告)号:US09751894B2
公开(公告)日:2017-09-05
申请号:US15369181
申请日:2016-12-05
发明人: Samarendra Nath Maiti , Dai Quoc Nguyen , Andhe V. N. Reddy , Judy Yip , Chan Minh Ha , Rong Ling , Rudong Shan , Madhava Reddy Madala
IPC分类号: C07D501/46 , C07D501/56 , A61K31/546 , C07D501/04
CPC分类号: C07D501/56 , A61K31/546 , C07D501/04
摘要: Cephem compounds, pharmaceutically acceptable salts thereof, and methods of using same, wherein the compound has a bicyclic nitrogen-containing aromatic heterocyclic ring as the quaternary ammoniomethyl group at the 3-position and one or both of a terminal amidine residue (substituted or unsubstituted) attached to an aryl or a 5- or 6-membered heteroaryl group (substituted or unsubstituted) which is further attached through a spacer to the free N-atom of the quaternary nitrogen-containing bicyclic ring at the 3-side chain, or a terminal guanidine residue attached to an aryl or a 5- or 6-membered heteroaryl group (substituted or unsubstituted) which is further attached through a spacer to the free N-atom of the quaternary nitrogen-containing bicyclic ring at the 3-side chain.
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公开(公告)号:US09006421B2
公开(公告)日:2015-04-14
申请号:US14211526
申请日:2014-03-14
发明人: Jan-Ji Lai , Pradip M. Pathare , Laxma Kolla , Adrien F. Soret
IPC分类号: C07D501/06 , C07D501/04 , C07F9/6561 , A61K31/546 , A61K31/433 , A61K31/426 , A61K31/41 , A61K31/545
CPC分类号: C07D501/59 , A61K31/41 , A61K31/426 , A61K31/433 , A61K31/545 , A61K31/546 , A61K31/675 , C07D501/04 , C07D501/06 , C07D501/22 , C07D501/34 , C07D501/36 , C07D501/56 , C07D501/57 , C07F9/65613
摘要: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step.
摘要翻译: 本文提供了一种合成头孢菌素抗生素化合物的方法,包括在单一步骤中将受保护的7-氨基转化为7-甲酰胺部分。
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公开(公告)号:US20130102583A1
公开(公告)日:2013-04-25
申请号:US13639412
申请日:2011-04-04
申请人: Shinya Hisakawa , Yasushi Hasegawa , Toshiaki Aoki , Hiroki Kusano , Masayuki Sano , Jun Sato , Kenji Yamawaki
发明人: Shinya Hisakawa , Yasushi Hasegawa , Toshiaki Aoki , Hiroki Kusano , Masayuki Sano , Jun Sato , Kenji Yamawaki
IPC分类号: C07D505/24 , C07D471/08 , C07D501/56
CPC分类号: C07D505/24 , C07D471/08 , C07D501/46 , C07D501/56 , C07D519/06
摘要: A compound of the formula: wherein X is —N═, —CH═, or the like; W is —CH2— or the like; U is —S— or the like; R1 and R2 are each independently hydrogen, halogen, optionally substituted lower alkyl, or the like; R3 is hydrogen or the like; each R4 is independently hydrogen, halogen, or the like; m is an integer from 0 to 2; Q is a single bond, or the like; G is —C(═O)—, or the like; D is a single bond, —NH—, or the like; and E is a cyclic quaternary ammonium group, or an ester, a protected compound at the amino on the ring in the 7-side chain, a pharmaceutically acceptable salt, or a solvate thereof.
摘要翻译: 下式的化合物:其中X为-N =, - CH =等; W是-CH 2 - 等; U是-S-等; R 1和R 2各自独立地为氢,卤素,任选取代的低级烷基等; R3是氢等; 每个R 4独立地是氢,卤素等; m为0〜2的整数; Q是单键等; G是-C(= O) - 等; D是单键-NH-等; 并且E是环状季铵基团,或酯,在7-侧链上的环上的氨基上的受保护化合物,其药学上可接受的盐或溶剂合物。
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