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1. 发明申请

WO2017140073A1 一种采用粒子过程晶体产品分子组装与形态优化技术的头孢硫脒新晶型化合物及制剂审中-公开
公开(公告)号：WO2017140073A1
公开(公告)日：2017-08-24
申请号：PCT/CN2016/085303
申请日：2016-06-08
申请人：海南灵康制药有限公司 , 天津大学 , 陶灵刚 , 王静康 , 尹秋响 , 郝红勋
发明人：陶灵刚 , 王静康 , 尹秋响 , 郝红勋
IPC分类号： C07D501/28 , C07D501/04 , C07D501/12 , A61K31/545 , A61P31/04
CPC分类号： A61K31/545 , C07D501/04 , C07D501/12 , C07D501/28
摘要：本发明公开了一种头孢硫脒新晶型化合物及其结晶制备方法，所述头孢硫脒新晶型化合物采用粒子过程晶体产品分子组装与形态优化技术制备而成。本新晶型化合物具有纯度高、杂质含量低、流动性好、稳定性好的特点。同时，本发明还公开了一种采用上述头孢硫脒制备的制剂—注射用头孢硫脒。

2. 发明申请

WO1991016327A1 ANTIMICROBIAL QUINOLONYL LACTAMS 审中-公开
标题翻译：抗微生物喹诺酮类LACTAMS
公开(公告)号：WO1991016327A1
公开(公告)日：1991-10-31
申请号：PCT/US1991002476
申请日：1991-04-12
申请人： NORWICH EATON PHARMACEUTICALS, INC.
发明人： NORWICH EATON PHARMACEUTICALS, INC. , DEMUTH, Thomas, Prosser, Jr. , WHITE, Ronald, Eugene
IPC分类号： C07D501/28
CPC分类号： C07D477/14 , C07D477/20 , C07D499/00 , C07D499/88 , C07D501/00
摘要： Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked to a quinolone moiety, of formula (I), wherein (1) A , A , A , R , and R generally form any of a variety of quinolone, naphthyridine or related cyclic moieties known in the art to have antimicrobial activity; and (2) R is part of a linking moiety, linking hte quinolone moiety to a lactam-containing moiety having formula (II), wherein (3) R , R , R , R , and R , together with bonds ''a'' and ''b'', form any of a variety of lactam-containing moieties known in the art to have antimicrobial activity; and (4) the linking moiety includes (for example) carbamate, dithiocarbamate, urea, thiourea, isouronium, isothiouronium, guanidine, carbonate, trithiocarbonate, reversed carbamate, xanthate, reversed isouronium, reversed dithiocarbamate, reversed isothiouronium, amine, imine, ammonium, heteroarylium, ether, thioether, ester, thioester, amide, and hydrazide groups.
摘要翻译：包含与式（I）的喹诺酮部分连接的含内酰胺部分的抗微生物喹诺酮内酰胺化合物，其中（1）A 1，A 2，A 3，R 1和R 4 >通常形成本领域已知的各种喹诺酮，萘啶或相关的环状部分以具有抗微生物活性; 和（2）R 6是连接部分的一部分，将喹诺酮部分与具有式（II）的含内酰胺部分连接，其中（3）R 10，R 11，R 12， R 13和R 14与键“a”和“b”一起形成本领域已知的具有抗微生物活性的各种含内酰胺的部分; 连接部分包括（例如）氨基甲酸酯，二硫代氨基甲酸酯，脲，硫脲，异脲，异硫脲，胍，碳酸酯，三硫代碳酸酯，反相氨基甲酸酯，黄原酸酯，反式异卤素，反式二硫代氨基甲酸酯，反式异硫脲，胺，亚胺，杂芳基，醚，硫醚，酯，硫酯，酰胺和酰肼基团。

3. 发明申请

WO2016107331A1 一种头孢硫脒化合物新晶型及其制备方法审中-公开
公开(公告)号：WO2016107331A1
公开(公告)日：2016-07-07
申请号：PCT/CN2015/095233
申请日：2015-11-20
申请人：天津大学 , 海南灵康制药有限公司
发明人：郝红勋 , 陶灵刚 , 孙志红 , 侯宝红 , 吕军 , 尹秋响 , 王永莉 , 龚俊波 , 谢闯 , 鲍颖
IPC分类号： C07D501/12 , C07D501/28
CPC分类号： C07D501/60 , C07B2200/13 , C07D501/12 , C07D501/28
摘要：一种头孢硫脒化合物的新晶型及其如下制备方法：将纯度大于等于98％的头孢硫脒化合物溶解在选自甲醇等的溶剂中形成浓度为0.05～0.2g/mL的溶液，再向溶液中滴加选自正丙醇等的溶析剂；随后以0.2～1℃/min降温速率将溶液降温至0～10℃；继续搅拌1～3h，将所得的固液悬浮液分离，干燥，得到该晶型产品。

4. 发明申请

WO1995004740A1 7alpha-AMINO-1,1-DIOXOCEFEM L-VALYLAMIDES 审中-公开
标题翻译： 7α-AMINO-1,1-DIOXOCEFEM L-VALYLAMIDES
公开(公告)号：WO1995004740A1
公开(公告)日：1995-02-16
申请号：PCT/IB1994000235
申请日：1994-08-04
申请人： DOMPE' S.P.A. , MACCHIA, Bruno , OMINI, Claudio , GANDOLFI, Carmelo , MANTOVANINI, Marco
发明人： DOMPE' S.P.A.
IPC分类号： C07D501/28
CPC分类号： C07D501/00
摘要： L-valylamides and L-homovalylamides of 7 alpha -amino-1,1-dioxo-3-cefem of formula (I), the process for obtaining them and the pharmaceutical compositions which contain them are described. The above-mentioned compounds are active in chronic bronchitis, in emphysema, in ARDS, in cystic fibrosis and in rheumatoid arthritis.
摘要翻译：描述了式（I）的7α-氨基-1,1-二氧代-3-头孢的L-缬氨酰胺和L-高戊酰胺，获得它们的方法和含有它们的药物组合物。上述化合物在慢性支气管炎，肺气肿，ARDS，囊性纤维化和类风湿性关节炎中均有活性。

5. 发明申请

WO2013109927A2 METALLODRUGS HAVING IMPROVED PHARMACOLOGICAL PROPERTIES AND METHODS OF MANUFACTURE AND USE THEREOF 审中-公开
标题翻译：具有改进的药理学特性的METALLODRUGS及其制造和使用方法
公开(公告)号：WO2013109927A2
公开(公告)日：2013-07-25
申请号：PCT/US2013/022198
申请日：2013-01-18
申请人： METALLOPHARM LLC
发明人： COWAN, James A. , COWAN, Ada S.
IPC分类号： C07D501/28 , C07D499/68 , C07H17/04 , C07D401/10 , C07K19/00
CPC分类号： C07D501/28 , A61K31/33 , A61K47/547 , A61K47/6811 , A61K47/6835 , C07K14/43563 , C07K14/463 , C07K14/4723 , C07K2319/00 , C07K2319/20
摘要： It is an object of the present invention to provide antimicrobial metallodrugs comprising an antimicrobial peptide ("AMP") and/or an antibiotic covalently bound to a metal binding moiety. These metallodrugs combine a metal binding domain which typically catalyzes oxido-reductase chemistry or acts as a Lewis-Acid catalyst, with a member of a diverse class of antimicrobial agents currently validated in preclinical and clinical settings for the treatment of a broad spectrum of pathogenic organisms.
摘要翻译：本发明的目的是提供包含与金属结合部分共价结合的抗微生物肽（“AMP”）和/或抗生素的抗微生物金属药物。这些金属药物组合了金属结合结构域，其通常催化氧化还原酶化学或作为路易斯酸催化剂，与目前在临床前和临床环境下验证的各种类型的抗微生物剂的成员用于治疗广谱的致病生物。

6. 发明申请

WO1987005297A1 CEPHALOSPORIN DERIVATIVES 审中-公开
标题翻译： CEPHALOSPORIN衍生物
公开(公告)号：WO1987005297A1
公开(公告)日：1987-09-11
申请号：PCT/US1987000399
申请日：1987-02-27
申请人： THE UNIVERSITY OF CHICAGO
发明人： THE UNIVERSITY OF CHICAGO , JOHNSTON, Michael, Adair , MOBASHERY, Shahrair
IPC分类号： C07D501/28
CPC分类号： C07D501/36 , C07D501/26 , C07D501/34 , Y02P20/55
摘要： Antibacterial cephalosporin compounds of formula (I), wherein W is a pharmaceutically acceptable salt or ester radical, or a carboxyl-protecting group; n is an integer from 0 to 5; -X- is -X1- or -X2- where the X1 moieties are the same or different and selected from the group consisting of (D) or (L) (II), and the -X2- moieties are the same or different and selected from the group consisting of (D) or (L) (III); with the proviso that (a) when X is X1, n is an integer from 1 to 5, is Z1 and Y is either -O- or (IV), (b) when X is X2, n is an integer from 1 to 5, Z is Z2 and Y is either (V) or (VI) and (c) when n is O, Y is (VII); wherein R1 is a functional group which does not substantially prevent hydrolysis of the cephalosporin by endogenous bacterial enzymes, Y1 is -O- or -S-; R2 is H, -CH2R4, -CHR52 or -CR53 where R4 is H, F, Cl, Br, -OH, -CN, (VIII), -CH(CH3)2, (IX), (X), or -C CH; Q1, Q2 and Q3 are the same or different and selected from the group consisting of H, F, Cl or Br; R5 is F, Cl or Br; R3 is H or -CH3; Z1 is H or an amino protecting group; and Z2 is OR6 or -NR7R8 where R6 is H, a pharmaceutically acceptable cation or a pharmaceutically acceptable ester, R7 and R8 are the same or different and selected from the group consisting of H or lower alkyl, or wherein R7 and R8 together with the nitrogen atom form a heterocyclic ring.

7. 发明申请

WO02068678A2 BETA-LACTAMASE SUBSTRATES HAVING PHENOLIC ETHERS 审中-公开
标题翻译：具有酚醛树脂的BETA-LACTAMASE底物
公开(公告)号：WO02068678A2
公开(公告)日：2002-09-06
申请号：PCT/US0200769
申请日：2002-01-11
申请人： UNIV CALIFORNIA , TSIEN ROGER Y , RAO JIANGHONG
发明人： TSIEN ROGER Y , RAO JIANGHONG
IPC分类号： C07D463/00 , C07D501/00 , C07D501/14 , C07D501/24 , C07D501/28 , C07D501/30 , C07D501/34 , C07D501/36 , C07D501/40 , C07D501/42 , C07D501/46 , C07D505/00 , C07F9/6561 , C12Q1/18 , C12Q1/34 , C12Q1/37 , C12Q1/68 , C12Q
CPC分类号： C12Q1/6897 , C07D463/18 , C07D501/00 , C07D505/00 , C07F9/65613 , C12Q1/34
摘要： Provided are fluorescent substrates for β-lactamases having general formula (I), in which R is a benzyl, 2-thienylmethyl, or cyanomethyl group; R' is selected from the group consisting of H, physiologically acceptable salts or metal, ester groups, ammonium cations, --CHR2OCO(CH2)nCH3, --CHR2OCOC(CH3)3, acylthiomethyl, acyloxy-alpha-benzyl, deltabutyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, β-morpholinoethyl, dialkylaminoethyl, and dislkylaminocarbonyloxymethyl, in which R2 is selected from the group consisting of H and lower alkyl; A is selected from the group consisting of S, O, SO, SO2 and CH2; and Z is a donor fluorescent moiety. Also provided are methods of use of the compound of general formula (I).
摘要翻译：提供具有通式（I）的β-内酰胺酶的荧光底物，其中R是苄基，2-噻吩基甲基或氰基甲基; R'选自H，生理上可接受的盐或金属，酯基，铵阳离子，-CHR2OCO（CH2）nCH3，-CH2OCOC（CH3）3，酰基硫代甲基，酰氧基-α-苄基，脱乙酰丁酰基，甲氧羰基氧甲基，苯基，甲基亚磺酰基甲基，β-吗啉代乙基，二烷基氨基乙基和二烷基氨基羰氧基甲基，其中R2选自H和低级烷基; A选自S，O，SO，SO 2和CH 2; Z是供体荧光部分。还提供了通式（I）的化合物的使用方法。

8. 发明申请

WO9535020A3 GLUTARYL 7-ACA DERIVATIVES AND PROCESSES FOR OBTAINING THEM 审中-公开
标题翻译： GLUTARYL 7-ACA衍生物及其制备方法
公开(公告)号：WO9535020A3
公开(公告)日：1996-02-01
申请号：PCT/EP9502802
申请日：1995-07-17
申请人： ANTIBIOTICOS SPA , SOGLI LORIS , LONGONI DAVIDE , POZZI GIOVANNI , SIVIERO ENRICO , TERRASSAN DANIELE MARIO , BERNASCONI ERMANNO , SALTO FRANCISCO
发明人： SOGLI LORIS , LONGONI DAVIDE , POZZI GIOVANNI , SIVIERO ENRICO , TERRASSAN DANIELE MARIO , BERNASCONI ERMANNO , SALTO FRANCISCO
IPC分类号： C07D501/04 , C07D501/00 , C07D501/14 , C07D501/16 , C07D501/20 , C07D501/24 , C07D501/26 , C07D501/28 , C07D501/59
CPC分类号： C07D501/00
摘要： There are disclosed new compounds of formula (I), wherein R is: a hydrogen atom; a linear or branched C1-C4 alkyl group, unsubstituted or substituted by at least a phenyl group or at least a hydrogen atom; a benzyl group substituted by at least a linear or branched C1-C4 alkyl or alkoxy group or a nitro group; a silyl substituted by at least a linear or branched, unsubstituted or substituted C1-C4 alkyl group; n is 0 or 1; and Y is a radical of formula (II), wherein A is H, OH, Cl, CH2, CH2X, where X is F, Cl, Br, I, OH or OR' and R' is COCH3 or a linear or branched, unsubstituted or substituted C1-C4 alkyl group and ... represents a single or a double bond, with the proviso that when n=0 and R is H, R' is not a methyl group; and processes for obtaining them.

9. 发明申请

WO2022239872A1 メタロβラクタマーゼ阻害剤审中-公开
公开(公告)号：WO2022239872A1
公开(公告)日：2022-11-17
申请号：PCT/JP2022/020285
申请日：2022-05-13
申请人：国立大学法人　熊本大学
发明人：澤　智裕 , 山口　佳宏 , 荒川　宜親
IPC分类号： C07D499/68 , A61K31/407 , A61K31/43 , A61K31/545 , A61P31/04 , C07D477/24 , C07D501/28 , C07D501/30
摘要：本発明により、式（Ｉ）、式（ＩＩ）または式（ＩＶ）で表される化合物、または医薬として許容なその塩、および該化合物または医薬として許容なその塩を含むメタロβラクタマーゼ阻害に使用するための医薬組成物が提供される。

10. 发明申请

WO00053207A1 BIOLOGICALLY ACTIVE COMPOUNDS OF DOLLAR I(GANODERMA PFEIFFERI) DMS 13239 审中-公开
标题翻译：生物活性化合物灵芝pfeifferi DMS 13239
公开(公告)号：WO00053207A1
公开(公告)日：2000-09-14
申请号：PCT/EP2000/002026
申请日：2000-03-08
IPC分类号： A61K8/97 , A61K36/06 , A61Q17/00 , A61Q19/00 , C07C69/732 , C07D498/06 , C07D499/36 , C07D501/28 , C07F9/40 , C07F9/655 , C07H19/067 , A61K35/84 , C07C59/52 , C07C59/64 , C07C59/84 , C07C69/734 , C07C69/738 , C07C69/80 , C07J13/00
CPC分类号： A61Q17/005 , A61K8/9706 , A61K36/074 , A61K2800/524 , A61Q19/00 , C07F9/4078 , C07F9/65505
摘要： The invention relates to novel biologically active compounds of fungi of the species Ganoderma pfeifferi DMS 13239, to methods of preparing same and to their use. From the fruit-body and mycelium of Ganoderma pfeifferi DMS 13239 extracts having an antimicrobial action and suitable as preservatives, for pharmaceutical and cosmetic preparations, as antiinfective agents and in fish-farming can be obtained. Antimicrobial active substances called ganomycines which are effective against multi-resistant germs are isolated from the extracts. The total synthesis of the ganomycines and their derivatization permits their use as antibiotics.
摘要翻译：本发明涉及新的从种真菌灵芝pfeifferi DMS 13239的生物活性化合物，它们的制备和它们的用途。从物种的子实体和菌丝体灵芝pfeifferi DMS 13239提取物可具有抗菌作用，可作为防腐剂用于医药和化妆品制剂防治感染，在鱼类养殖中使用。 Ganomycins称为抗微生物剂是针对来自提取物中分离多抗细菌有效。 ganomycins及其衍生的全合成使得能够使用作为抗生素。

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