公开(公告)号：WO2017136642A1

公开(公告)日：2017-08-10

申请号：PCT/US2017/016378

申请日：2017-02-03

Applicant: THE TRUSTEES OF DARTMOUTH COLLEGE

Inventor： CHEUNG, Ambrose Lin Yau ,  NAIR-SCHAEF, Dhanalakshmi R. ,  WU, Jimmy ,  CHEN, Ji

IPC: A61K31/496 ,  A61K31/545 ,  A61K45/06 ,  C07D501/00 ,  C07D501/04 ,  C07D501/06

CPC classification number: A61K31/4706 ,  A61K31/47 ,  C07D215/233 ,  C07D215/26 ,  C07D215/44 ,  C07D413/12 ,  A61K2300/00

Abstract: The present disclosure relates to compounds having antimicrobial activity, compositions comprising said compounds in combination with β-lactam antibiotics, and methods of using the compounds and compositions.

Abstract translation: 本公开涉及具有抗微生物活性的化合物，包含所述化合物与β-内酰胺抗生素组合的组合物，以及使用所述化合物和组合物的方法。

公开(公告)号：WO2014012849A1

公开(公告)日：2014-01-23

申请号：PCT/EP2013/064727

申请日：2013-07-11

Applicant: DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.

Inventor： MAO, Chang-Long ,  XU, Jian-Jun ,  SONG, Bo

IPC: C07D501/00 ,  A61K31/546 ,  A61P31/04 ,  C07D501/56

CPC classification number: C07D501/56

Abstract: The present invention relates to a new crystal form of cefoperazone sodium and the method for making said crystal form. The new crystal form has the following characteristics: orthorhombic crystal, space group F222, unit cell dimensions a=52.15Å, b=51.87Å and c=4.95 Å.

Abstract translation: 本发明涉及一种头孢哌酮钠的新晶体形式及其制备方法。 新晶体具有以下特征：正交晶体，空间群F222，晶胞尺寸a =52.15Å，b =51.87Å，c = 4.95。

公开(公告)号：WO2006018807A8

公开(公告)日：2006-08-10

申请号：PCT/IB2005052691

申请日：2005-08-15

Applicant: RANBAXY LAB LTD ,  MAHENDRU MANU ,  ARYAN RAM CHANDER ,  KUMAR SATISH ,  PANDYA BHARGAV ,  DUGGAL SANJAM ,  GADE SANJAY ,  KUMAR YATENDRA

Inventor： MAHENDRU MANU ,  ARYAN RAM CHANDER ,  KUMAR SATISH ,  PANDYA BHARGAV ,  DUGGAL SANJAM ,  GADE SANJAY ,  KUMAR YATENDRA

IPC: C07D501/00 ,  A61K31/546 ,  A61P31/04

CPC classification number: C07D501/00

Abstract: The invention relates to processes for the preparation of crystalline polymorphic forms of cefdinir of formula I. More particularly, it relates to the preparation of crystalline polymorphic forms of cefdinir designated as Forms B and C. The invention also relates to pharmaceutical compositions that include the polymorphic forms B and C, and the use of the compositions for treating bacterial infections.

Abstract translation: 本发明涉及用于制备式I的头孢地尼的结晶多晶形式的方法。更具体地说，本发明涉及被称为形式B和C的头孢地尼的结晶多晶形式的制备。本发明还涉及药物组合物，其包括多晶型物 形式B和C，以及组合物用于治疗细菌感染的用途。

公开(公告)号：WO2006018807A1

公开(公告)日：2006-02-23

申请号：PCT/IB2005/052691

申请日：2005-08-15

Applicant: RANBAXY LABORATORIES LIMITED ,  MAHENDRU, Manu ,  ARYAN, Ram, Chander ,  KUMAR, Satish ,  PANDYA, Bhargav ,  DUGGAL, Sanjam ,  GADE, Sanjay ,  KUMAR, Yatendra

Inventor： MAHENDRU, Manu ,  ARYAN, Ram, Chander ,  KUMAR, Satish ,  PANDYA, Bhargav ,  DUGGAL, Sanjam ,  GADE, Sanjay ,  KUMAR, Yatendra

IPC: C07D501/00 ,  A61K31/546 ,  A61P31/04

CPC classification number: C07D501/00

Abstract: The invention relates to processes for the preparation of crystalline polymorphic forms of cefdinir of formula (I). More particularly, it relates to the preparation of crystalline polymorphic forms of cefdinir designated as Forms B and C. The invention also relates to pharmaceutical compositions that include the polymorphic forms B and C, and the use of the compositions for treating bacterial infections.

Abstract translation: 本发明涉及制备式（I）的头孢地尼的结晶多晶形式的方法。 更具体地说，本发明涉及被称为形式B和C的头孢地尼的晶体多晶形式的制备。本发明还涉及包含多晶型B和C的药物组合物，以及该组合物用于治疗细菌感染的用途。

公开(公告)号：WO2005100368A3

公开(公告)日：2005-10-27

申请号：PCT/US2005/012439

申请日：2005-04-11

Applicant: ABBOTT LABORATORIES ,  SERVER, Nancy, E. ,  LAW, Devalina

Inventor： SERVER, Nancy, E. ,  LAW, Devalina

IPC: C07D501/00

Abstract: The present invention relates to stable amorphous 7-[2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamide]-3-vinyl-3-cephem-4-carboxylic acid (syn isomer), methods for its preparation, and pharmaceutical compositions comprising stable amorphous 7-[2-(2-aminothiazol-4-yl)-2-hydroxyiminoacetamide]-3-vinyl-3-cephem-4-carboxylic acid (syn isomer).

公开(公告)号：WO2005044824A2

公开(公告)日：2005-05-19

申请号：PCT/IB2004/003571

申请日：2004-11-01

Applicant: RANBAXY LABORATORIES LIMITED ,  KUMAR, Yatendra ,  PRASAD, Mohan ,  SINGH, Kaptan ,  PRASAD, Ashok ,  RICHHARIYA, Santosh

Inventor： KUMAR, Yatendra ,  PRASAD, Mohan ,  SINGH, Kaptan ,  PRASAD, Ashok ,  RICHHARIYA, Santosh

IPC: C07D501/00

CPC classification number: C07D501/24

Abstract: The present invention relates to a process for preparation of highly pure amorphous and crystalline forms of cefditoren pivoxil and pharmaceutical compositions comprising highly pure amorphous and crystalline forms of cefditoren pivoxil. The present invention also relates to a method of treating infections using highly pure amorphous and crystalline forms of cefditoren pivoxil. The highly pure cefditoren pivoxil has a purity greater than 98.5% and contains less than 1.0% of the E-isomer impurity and less than 1 % of the Δ 2 ­isomer impurity.

Abstract translation: 本发明涉及一种制备高纯度无定形和结晶形式的头孢托仑匹酯的方法和包含高纯度无定形和结晶形式的头孢托仑匹酯的药物组合物。 本发明还涉及使用高纯度无定形和结晶形式的头孢托仑匹酯治疗感染的方法。 高纯度的头孢托仑匹酯具有大于98.5％的纯度，并含有小于1.0％的E-异构体杂质和小于1％的Δ2异构体杂质。

公开(公告)号：WO2005005436A3

公开(公告)日：2005-03-10

申请号：PCT/US2004022319

申请日：2004-07-09

Applicant: THERAVANCE INC ,  FATHEREE PAUL R ,  LINSELL MARTIN S ,  MARQUESS DANIEL ,  TRAPP SEAN G ,  MORAN EDMUND J ,  AGGEN JAMES B

Inventor： FATHEREE PAUL R ,  LINSELL MARTIN S ,  MARQUESS DANIEL ,  TRAPP SEAN G ,  MORAN EDMUND J ,  AGGEN JAMES B

IPC: A61K38/14 ,  A61P31/04 ,  C07D501/00 ,  C07K7/64 ,  C07K9/00 ,  A61K31/545

CPC classification number: C07K7/64 ,  C07D501/00 ,  C07K9/008

Abstract: This invention provides cross-linked glycopeptide - cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明提供了可用作抗生素的交联糖肽 - 头孢菌素化合物及其药学上可接受的盐。 本发明还提供含有这些化合物的药物组合物; 用这种化合物治疗哺乳动物细菌感染的方法; 和用于制备这些化合物的方法和中间体。

公开(公告)号：WO2005003141A3

公开(公告)日：2005-03-10

申请号：PCT/IB2004002203

申请日：2004-07-03

Applicant: ORCHID CHEMICALS & PHARM LTD ,  PRABHAT KUMAR SAHOO ,  VEMPALI ANANDAM ,  SUNDARAVADIVELAN SIVAKUMARAN ,  PRAVEEN NAGESH GANESH ,  VITTAL MANIKRAO WAGHDARE ,  PANDURANG BALAWANT DESHPANDE ,  PARVEN KUMAR LUTHRA ,  PRATIK RAMESH SATHE

Inventor： PRABHAT KUMAR SAHOO ,  VEMPALI ANANDAM ,  SUNDARAVADIVELAN SIVAKUMARAN ,  PRAVEEN NAGESH GANESH ,  VITTAL MANIKRAO WAGHDARE ,  PANDURANG BALAWANT DESHPANDE ,  PARVEN KUMAR LUTHRA ,  PRATIK RAMESH SATHE

IPC: C07D501/00 ,  C07D501/04

CPC classification number: C07D501/04

Abstract: The present invention relates to an improved process for the preparation of Cefditoren of formula (I), the said process comprising the steps of: i) converting the compound of formula (II) to a compound of the formula (III) using TPP and sodium iodide in the presence of THF, water, and base; ii) reacting the compound of formula (III) with 4-methyl-5-formyl-thiazole to produce a compound of formula (IV); iii) deesterifying the compound of the formula (IV) to yield compound of formula (V); iv) converting the compound of formula (V) to compound of formula (VI) in the presence of a base and solvent; v) converting the compound of formula (VI) into compound of formula (VII) by enzymatic hydrolysis; and vi) reacting compound of formula (VII) with compound of formula (VIII) in the presence of solvent and base to produce compound of formula (I).

Abstract translation: 本发明涉及制备式（I）的头孢托仑的改进方法，所述方法包括以下步骤：i）使用TPP和钠将式（II）化合物转化为式（III）化合物 碘化物在THF，水和碱的存在下反应; ii）使式（III）化合物与4-甲基-5-甲酰基 - 噻唑反应以制备式（IV）化合物; iii）将式（Ⅳ）化合物酯化，得到式（Ⅴ）化合物; iv）在碱和溶剂的存在下将式（Ⅴ）化合物转化成式（Ⅵ）化合物; v）通过酶水解将式（Ⅵ）化合物转化成式（Ⅶ）化合物; 和vi）使式（VII）的化合物与式（VIII）的化合物在溶剂和碱的存在下反应，得到式（I）的化合物。

公开(公告)号：WO2004067536A3

公开(公告)日：2004-08-12

申请号：PCT/EP2004/000683

申请日：2004-01-27

Applicant: SANDOZ AG ,  ASCHER, Gerd ,  THIRRING, Klaus

Inventor： ASCHER, Gerd ,  THIRRING, Klaus

IPC: C07D501/00

Abstract: A pharmaceutically active compound having a carboxylic acid group-COOH as a part of its chemical structure which -COOH group is in form of a carboxylic acid ester.

公开(公告)号：WO2004067536A2

公开(公告)日：2004-08-12

申请号：PCT/EP2004000683

申请日：2004-01-27

Applicant: SANDOZ AG ,  ASCHER GERD ,  THIRRING KLAUS

Inventor： ASCHER GERD ,  THIRRING KLAUS

IPC: C07D477/20 ,  C07D499/00 ,  C07D501/00

CPC classification number: C07D477/20 ,  C07D499/00 ,  C07D501/00

Abstract: A pharmaceutically active compound having a carboxylic acid group-COOH as a part of its chemical structure which -COOH group is in form of a carboxylic acid ester.

Abstract translation: 具有羧酸基-COOH作为其化学结构的一部分的药物活性化合物，-COOH基团是羧酸酯形式。