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1. 发明申请

WO2007039885A1 A PROCESS FOR THE PREPARATION OF FAROPENEM 审中-公开
标题翻译：一种制备农药的方法
公开(公告)号：WO2007039885A1
公开(公告)日：2007-04-12
申请号：PCT/IB2006/053651
申请日：2006-10-05
申请人： RANBAXY LABORATORIES LIMITED , KUMAR, Neela, Praveen , PRASAD, Mohan
发明人： KUMAR, Neela, Praveen , PRASAD, Mohan
IPC分类号： C07D499/88
CPC分类号： C07D499/893
摘要： The present invention is related to processes for the preparation of faropenem.
摘要翻译：本发明涉及制备法罗培南的方法。

2. 发明申请

WO1993007154A1 PROCESS FOR MAKING ANTIMICROBIAL QUINOLONYL LACTAMS 审中-公开
标题翻译：制备抗微生物喹诺酮类药物的方法
公开(公告)号：WO1993007154A1
公开(公告)日：1993-04-15
申请号：PCT/US1992008246
申请日：1992-09-28
申请人： PROCTER & GAMBLE PHARMACEUTICALS, INC.
发明人： PROCTER & GAMBLE PHARMACEUTICALS, INC. , WHITE, Ronald, Eugene , DEMUTH, Thomas, Prosser, Jr.
IPC分类号： C07D499/88
CPC分类号： C07D505/00 , C07D477/02 , C07D499/88 , Y02P20/55
摘要： The present invention provides methods of making compounds of the structure [Q - L ] - L - [L - B], wherein Q is a quinolone moiety; B is a beta-lactam moiety; L, L , and L together comprise a carbamate-containing linking moiety, comprising the steps of: 1) reacting a lactam compound of the formula B-L -H with phosgene to form an intermediate compound of the formula B-L -C(=O)-Cl, where L is oxygen; and 2) coupling said intermediate compound with a quinolone compound of the formula Q-l -R , wherein L is nitrogen; R is hydrogen, Si(R )3, or Sn(R )3; and R is lower alkyl. Preferably, the process additionally comprises steps prior to the reacting and coupling steps where esters of the lactam and quinolone compounds are made. Also preferably, the coupling step comprises adding a solution containing the quinolone compound to a solution containing the intermediate compound. The process steps are also preferably performed at a temperature of from about -80 DEG C to about 0 DEG C. Preferred antimicrobial compounds made by these processes are those where the beta-lactam moiety is a penem.
摘要翻译：本发明提供了制备[Q-L 1] -L- [L 2 -B]结构的化合物的方法，其中Q是喹诺酮部分; B是β-内酰胺部分; L，L 1和L 2一起包含含氨基甲酸酯的连接部分，包括以下步骤：1）将式BL 4 -H的内酰胺化合物与光气反应以形成中间体化合物式（4）-C（= O）-Cl，其中L 4为氧; 和2）将所述中间体化合物与式Q-l 3-R 44的喹诺酮化合物偶联，其中L 3是氮; R 44是氢，Si（R 45）3或Sn（R 45）3; R 45为低级烷基。优选地，该方法还包括在制备内酰胺和喹诺酮化合物的酯的反应和偶联步骤之前的步骤。还优选地，偶联步骤包括将含有喹诺酮化合物的溶液加入到含有中间体化合物的溶液中。方法步骤还优选在约-80℃至约0℃的温度下进行。通过这些方法制备的优选的抗微生物化合物是其中β-内酰胺部分是青铜的那些。

3. 发明申请

WO1993000345A1 PENEM DERIVATIVES 审中-公开
标题翻译：笔式衍生物
公开(公告)号：WO1993000345A1
公开(公告)日：1993-01-07
申请号：PCT/EP1992001396
申请日：1992-06-22
申请人： FARMITALIA CARLO ERBA S.R.L. , VISENTIN, Giuseppina , ZARINI, Franco , JABES, Daniela , PERRONE, Ettore , DELLA BRUNA, Costantino , ALPEGIANI, Marco
发明人： FARMITALIA CARLO ERBA S.R.L.
IPC分类号： C07D499/88
CPC分类号： C07D499/88
摘要： The invention provides compounds of general formula (I) wherein R1 is a hydrogen atom, a negative charge or an ester residue; R is: a) -(CH2)n-A-CO2H, -(CH2)n-A-SO3H or -(CH2)n-A-PO3H2, wherein n is either zero, one or two and A is a group -CH=CH- (either E or Z), -OCH2-, -SCH2- or -CHOH-; b) -(CH2)n-PO3H2, -(CH2)nSO2NHCN, -(CH2)nNHSO3H, -(CH2)nCONHSO2CH3 or -(CH2)nCONHSO2CF3, wherein n is as defined above; c) -(CH2S)m-W-(CH2)nZ, wherein W is an arylene group or a heterocyclediyl group, m is 0 or 1, n is as above defined, and Z represents CO2H, PO3H2, SO2NHCN, NHSO3H, CONHSO2CH3 or CONHSO2CF3; d) -Y-CH2 formula (II), wherein Y is O or NH and X is NH, N-OH or N-O-(CH2)n+1COOH wherein n is as defined above; or e) -(CH2S)m-W', wherein W' is a heterocyclyl group convertible into an anion at physiological pH and m is as defined above. Compounds (I), their salts and ester prodrugs have antibacterial activity.

4. 发明申请

WO2018030840A1 연조직 경화용 조성물 审中-公开
标题翻译：用于硬化软组织的组合物
公开(公告)号：WO2018030840A1
公开(公告)日：2018-02-15
申请号：PCT/KR2017/008743
申请日：2017-08-11
申请人： 가톨릭대학교 산학협력단 , 한국화학연구원
发明人： 이상철 , 김세준 , 정관령 , 김옥희 , 조석준 , 유민진
IPC分类号： C07D499/88 , A61K31/43 , A61K31/47 , A61K31/4709 , G01N33/50 , G01N33/483
摘要： 본 발명은 연조직의 봉합 수술을 위하여 연조직을 일시적으로 단단하게 경화시킬 수 있는 다양한 화합물에 관한 것이다. 본 발명에 따른 화합물은 연조직의 경도 또는 인장력을 일시적으로 높여 연조직에 대한 봉합 시술 시 봉합 효율을 높여 문합이 제대로 이루어지지 않음에 따른 후유증 등을 예방할 수 있다. 또한, 본 발명에 따른 화합물은 연조직 중에서도 특히 췌장의 경도 또는 인장력을 일시적으로 높여 췌십이지장절제술(pancreaticoduodenectomy) 시 봉합 효율을 높여 췌장루를 효과적으로 예방할 수 있다.
摘要翻译：＆lt; p num =“0000”＆gt;本发明涉及能够暂时硬化用于软组织缝合操作的硬组织的各种化合物。根据本发明，能够防止副作用，例如根据所述吻合缝合增加了治疗软组织的增加软组织的硬度或张力暂时不能正常工作的密封效率的化合物。此外，这些化合物根据本发明能够特别胰暂时提高胰腺的硬度或张力以增加十二指肠切除术（胰十二指肠切除术）的密封的软组织中的效率有效地防止胰腺路。

5. 发明申请

WO99036098A1 ANTIBACTERIAL COMPOSITION FOR TOPICAL ADMINISTRATION CONTAINING ANTIBIOTICS 审中-公开
标题翻译：用于含有抗生素的局部管理的抗菌组合物
公开(公告)号：WO99036098A1
公开(公告)日：1999-07-22
申请号：PCT/JP1999/000068
申请日：1999-01-12
IPC分类号： A61K9/00 , A61K31/43 , A61K47/06 , A61K47/32 , A61K47/36 , C07D499/88 , A61K47/30 , C07D499/00
CPC分类号： C07D499/88 , A61K9/0014 , A61K9/0063 , A61K31/43 , A61K47/06 , A61K47/32 , A61K47/36
摘要： An antibacterial composition for topical administration having a potent antibacterial effect over a broad range and a high safety and containing in a stable state penem antibiotics which are chemically unstable to hydrolysis, oxidation, photoisomerization, etc. The composition comprises a non-aqueous base blended with a penem antibiotic or a pharmaceutically acceptable salt thereof.
摘要翻译：一种用于局部给药的抗菌组合物，其在宽范围和高安全性下具有强效的抗菌作用，并且在稳定状态下含有对水解，氧化，光异构化等化学不稳定的青霉烯抗生素。该组合物包含与青霉素抗生素或其药学上可接受的盐。

6. 发明申请

WO1994006803A1 PENEM DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：派宁衍生物，其制剂和含有它们的药物组合物
公开(公告)号：WO1994006803A1
公开(公告)日：1994-03-31
申请号：PCT/EP1993002493
申请日：1993-09-15
申请人： A. MENARINI INDUSTRIE FARMACEUTICHE RIUNITE ... , ISTITUTO LUSOFARMACO D'ITALIA S.P.A. , ALTAMURA, Maria , ARCAMONE, Federico, Maria , PERROTTA, Enzo , PESTELLINI, Vittorio , SBRACI, Piero , CASCIO, Giuseppe
发明人： A. MENARINI INDUSTRIE FARMACEUTICHE RIUNITE ... , ISTITUTO LUSOFARMACO D'ITALIA S.P.A.
IPC分类号： C07D499/88
CPC分类号： C07D499/88
摘要： Described are penems derivatives of general formula (I) wherein R1 is chosen in the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy, C3-C7 cycloalkyl, optionally protected C1-C6 hydroxyalkyle; R2 is chosen in the group consisting of carboxyl group free or esterified with a group easily activated "in vivo", carboxylate anion; R3 is chosen in the group consisting of H, C1-C4 alkyl optionally substituted; R4 is chosen in the group consisting of: H, C1-C6 alkyl optionally substituted, C1-C6 hydroxyalkyl optionally substituted, C1-C6 mercaptoalkyl optionally substituted, C1-C6 aminoalkyl optionally substituted, C1-C6 alkyl substituted by a quaternary ammonium group, C1-C6 carboxyalkyl optionally substituted, cycloalkyl, aryl, arylalkyl, heterocyclyl-alkyl optionally substituted, saturated or unsaturated heterocycle wherein the heteroatoms in the heterocyclic ring can be N, O, S, or R3 and R4 linked together form a heterocyclic ring having 3-7 atoms, optionally substituted, saturated or unsaturated which can contain other heteroatoms as O, N, S. R5 and R6 independently from one another are chosen in the group consisting of: H, C1-C6 alkyl, C1-C6 hydroxyalkyl, C1-C6 mercaptoalkyl, C1-C6 aminoalkyl, alkenyl, cycloalkyl, aryl, arylalkyl, alkylaryl, heterocyclyl-alkyl, C1-C6 alkyl carboxyamide wherein the alkyl group can be linear or branched (all these groups optionally substituted), or R5 and R6 taken together form an heterocyclic ring having 3-7 atoms optionally substituted, n is chosen in the group consisting of: 1, 2, 3; and their pharmaceutically acceptable salts.
摘要翻译：描述的是通式（I）的青蒿衍生物，其中R 1选自H，C 1 -C 6烷基，C 1 -C 6烷氧基，C 3 -C 7环烷基，任选保护的C 1 -C 6羟基烯烃; R2选自无羧基或酯基化，易于活化的“体内”，羧酸根阴离子; R3选自H，任选取代的C 1 -C 4烷基; R4选自：任选取代的H，任选取代的C 1 -C 6烷基，任选取代的C 1 -C 6羟基烷基，任选取代的C 1 -C 6巯基烷基，任选取代的C 1 -C 6氨基烷基，被季铵基团取代的C 1 -C 6烷基， C 1 -C 6羧基烷基任选取代的，环烷基，芳基，芳基烷基，杂环基 - 烷基任选取代的饱和或不饱和杂环，其中杂环中的杂原子可以是N，O，S或R 3和R 4连接在一起形成具有3 -7个原子，任选取代的，饱和或不饱和的，其可以含有其它杂原子作为O，N，S。R5和R6彼此独立地选自：H，C1-C6烷基，C1-C6羟基烷基，C1 -C 6巯基烷基，C 1 -C 6氨基烷基，烯基，环烷基，芳基，芳基烷基，烷基芳基，杂环基 - 烷基，C 1 -C 6烷基羧酰胺，其中烷基可以是直链或支链（所有这些基团任选取代） d R6一起形成任选取代的具有3-7个原子的杂环，n选自：1,2,3; 及其药学上可接受的盐。

7. 发明申请

WO1992003444A1 PENEM COMPOUNDS 审中-公开
标题翻译： PENEM化合物
公开(公告)号：WO1992003444A1
公开(公告)日：1992-03-05
申请号：PCT/JP1991001100
申请日：1991-08-16
申请人： SUNTORY LIMITED , IWATA, Hiromitsu , NAKATSUKA, Takashi , TANAKA, Rie , ISHIGURO, Masaji
发明人： SUNTORY LIMITED
IPC分类号： C07D499/88
CPC分类号： C07D499/88
摘要： Antibiotic penem compounds are represented by formula (I), wherein R represents a group of formulae (II) or (III) in which R1 is a linear or branched, C1-C6 alkyl group, R2 is a particular substituted or unsubstituted alkyl, aryl or aralkyl group, n is an integer of 1 or 2, and R3 represents a specific substituted or unsubstituted alkyl, aryl or aralkyl group. Antibiotic compositions for oral administration are also described.
摘要翻译：抗生素penem化合物由式（I）表示，其中R表示式（II）或（III）的基团，其中R 1是直链或支链的C 1 -C 6烷基，R 2是特定的取代或未取代的烷基，芳基或芳烷基，n为1或2的整数，R 3表示特定的取代或未取代的烷基，芳基或芳烷基。还描述了用于口服给药的抗生素组合物。

8. 发明申请

WO1992003442A1 ANTIBACTERIAL PENEM ESTERS DERIVATIVES 审中-公开
标题翻译：抗真菌药剂衍生物
公开(公告)号：WO1992003442A1
公开(公告)日：1992-03-05
申请号：PCT/JP1991001098
申请日：1991-08-16
申请人： SUNTORY LIMITED , IWATA, Hiromitsu , NAKATSUKA, Takashi , TANAKA, Rie , ISHIGURO, Masaji
发明人： SUNTORY LIMITED
IPC分类号： C07D499/88
CPC分类号： C07D499/88
摘要： Antibiotic penem compounds are represented by formula (I), wherein R represents a group of general formulae (II), (III), or -CH2-Z, in which R1 is a linear or branched C1-C6 alkyl group, R2 is a particular substituted or unsubstituted alkyl, aryl or aralkyl group, n is an integer of 1-6, Y is a 5- or 6-membered heterocyclic aliphatic group having 1 or 2 oxygen atoms in the ring thereof, and Z is a specific 5-substituted 2-oxo-1,3-dioxolen-4-yl group. Antibiotic compositions for oral administration are also described.
摘要翻译：抗生素penem化合物由式（I）表示，其中R表示通式（II），（III）或-CH 2 -Z的基团，其中R 1是直链或支链C 1 -C 6烷基，R 2是特定的取代或未取代的烷基，芳基或芳烷基，n为1-6的整数，Y为其环中具有1或2个氧原子的5或6元杂环脂族基团，Z为特定的5- 取代的2-氧代-1,3-二氧杂环戊烯-4-基。还描述了用于口服给药的抗生素组合物。

9. 发明申请

WO1991017995A1 NEW PENEM DITHIOCARBAMATES, THEIR USE AND PRODUCTION METHODS 审中-公开
标题翻译：新型二氢碳酸钠，其使用和生产方法
公开(公告)号：WO1991017995A1
公开(公告)日：1991-11-28
申请号：PCT/IT1991000041
申请日：1991-05-14
申请人： A. MENARINI INDUSTRIE FARMACEUTICHE RIUNITE ... , ALTAMURA, Maria , ARCAMONE, Federico , GIANNOTTI, Danilo , PESTELLINI, Vittorio , SBRACI, Piero
发明人： A. MENARINI INDUSTRIE FARMACEUTICHE RIUNITE ...
IPC分类号： C07D499/88
CPC分类号： C07D499/88
摘要： A compound of general formula (I), wherein R1 is a hydrogen atom, C1-C6 alkyl, C1-C6 alkoxy, cycloakyl or hydroxyalkyl, the alcoholic function of the hydroxyalkyl being free or protected; R2 is a free or esterified carboxy group or a carboxylate anion; R3 and R4 are each independently either hydrogen or C1-C6 alkyl, C1-C6 hydroxyalkyl or mercaptoalkyl, aminoalkyl or alkyl substituted with a quaternary ammonium group; cycloalkyl, arylalkyl or heterocyclyl-alkyl; a 5-6 membered, saturated or unsaturated heterocyclic ring, which can contain supplementary heteroatoms, such as oxygen, sulfur and nitrogen; an aryl group, or R3 and R4 form together a 3-7 membered, saturated or unsaturated heterocyclic ring, which can contain supplementary heteroatoms, such as oxygen, sulfur or nitrogen.
摘要翻译：通式（I）的化合物，其中R 1为氢原子，C 1 -C 6烷基，C 1 -C 6烷氧基，环烷基或羟基烷基，羟基烷基的醇官能团为游离或保护的; R2是游离的或酯化的羧基或羧酸根阴离子; R 3和R 4各自独立地为氢或C 1 -C 6烷基，C 1 -C 6羟烷基或巯基烷基，氨基烷基或被季铵基取代的烷基; 环烷基，芳基烷基或杂环基 - 烷基; 5-6元饱和或不饱和的杂环，其可以含有辅助杂原子，例如氧，硫和氮; 芳基或R 3和R 4一起形成3-7元饱和或不饱和的杂环，其可以含有辅助杂原子，例如氧，硫或氮。

10. 发明申请

WO2003093277A1 PROCESS FOR PREPARING 6-ALKYLIDENE PENEM DERIVATIVES 审中-公开
标题翻译：制备6-烷基苯胺衍生物的方法
公开(公告)号：WO2003093277A1
公开(公告)日：2003-11-13
申请号：PCT/US2003/013429
申请日：2003-04-30
申请人： WYETH , ABE, Takao , MATSUNAGA, Hiroshi , MIHIRA, Ado , SATO, Chisato , USHIROGOCHI, Hideki , SATO, Koichi , TAKASAKI, Tsuyoshi , VENKATESAN, Aranapakam, Mudumbai , MANSOUR, Tarek, Suhayl
发明人： ABE, Takao , MATSUNAGA, Hiroshi , MIHIRA, Ado , SATO, Chisato , USHIROGOCHI, Hideki , SATO, Koichi , TAKASAKI, Tsuyoshi , VENKATESAN, Aranapakam, Mudumbai , MANSOUR, Tarek, Suhayl
IPC分类号： C07D499/88
CPC分类号： C07D499/88
摘要： The present invention provides a process of making compounds of Formula (I), which are useful for the treatment of bacterial infection or disease.
摘要翻译：本发明提供制备式（I）化合物的方法，其可用于治疗细菌感染或疾病。

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