公开(公告)号：WO2014165107A3

公开(公告)日：2014-10-09

申请号：PCT/US2014/024411

申请日：2014-03-12

Applicant: VERTEX PHARMACEUTICALS INCORPORATED

Inventor： DIETRICH, Evelyne ,  POISSON, Carl ,  GALLANT, Michel ,  LESSARD, Stephanie ,  LIU, Bingcan ,  DAS, Sanjoy, Kumar ,  RAMTOHUL, Yeeman ,  REDDY, Thumkunta, Jagadeeswar ,  MARTEL, Julien ,  VALLEE, Frederic ,  LEVESQUE, Jean-francois

IPC: C07H15/18 ,  C07H15/20 ,  C07H15/207 ,  C07H15/22 ,  C07H15/26 ,  C07D493/10 ,  A61K31/7034

Abstract: The present invention relates to compounds useful for the treatment or prevention of bacteria infections. These compounds have formula (I) The invention also provides processes for making the compounds described herein. Furthermore, the present invention provides a composition comprising the compounds described herein, and a pharmaceutically acceptable carrier, adjuvant, or vehicle. The present invention also provides methods of treating or preventing bacteria infection in a subject, comprising administering to the subject an effective amount of the compound or the composition described herein.

公开(公告)号：WO2011085544A1

公开(公告)日：2011-07-21

申请号：PCT/CN2010/070148

申请日：2010-01-13

Applicant: 安徽辉克药业有限公司 ,  美国升阳制药公司 ,  朱作霖 ,  孙萌 ,  叶红平

Inventor： 朱作霖 ,  孙萌 ,  叶红平

IPC: C07D487/22 ,  C07D493/20 ,  C07H15/20 ,  A61K31/7042 ,  A61P35/00

CPC classification number: C07H15/203 ,  A61K31/7042

公开(公告)号：WO2005092877A8

公开(公告)日：2006-01-26

申请号：PCT/EP2005002618

申请日：2005-03-11

Applicant: BOEHRINGER INGELHEIM INT ,  BOEHRINGER INGELHEIM PHARMA ,  HIMMELSBACH FRANK ,  ECKHARDT MATTHIAS ,  EICKELMANN PETER ,  BARSOUMIAN EDWARD LEON ,  THOMAS LEO

Inventor： HIMMELSBACH FRANK ,  ECKHARDT MATTHIAS ,  EICKELMANN PETER ,  BARSOUMIAN EDWARD LEON ,  THOMAS LEO

IPC: A61K31/70 ,  A61K31/7004 ,  A61P3/00 ,  C07D309/10 ,  C07H15/04 ,  C07H15/20 ,  C07H15/26 ,  A61K31/351

CPC classification number: C07H23/00 ,  A61K9/0019 ,  A61K9/02 ,  A61K9/2018 ,  A61K9/4866 ,  C07D309/10 ,  C07H15/04 ,  C07H15/20 ,  C07H15/26

Abstract: The invention relates to glucopyranosyl-substitutedted benzol derivatives of general formula (I), wherein rests R 1 to R 6 and R 7a , R 7b , R 7c are such as defined in the claim 1, including the tautomers, stereoisomers, mixtures and the salts thereof. The inventive compounds are useful for treating metabolic diseases.

Abstract translation: 吡喃葡萄糖基取代的（I），其中基团R ^{1 至R 6 和R 7 ，R 通式的苯衍生物 图7b ，R 7C 如根据权利要求1，包括互变异构体，立体异构体，混合物和其盐定义。 本发明的化合物可用于代谢性疾病的治疗中是有用的。}

公开(公告)号：WO2004014930A1

公开(公告)日：2004-02-19

申请号：PCT/JP2003/010159

申请日：2003-08-08

Applicant: 大正製薬株式会社 ,  佐藤 正和 ,  柿沼 浩行 ,  浅沼 肇

Inventor： 佐藤 正和 ,  柿沼 浩行 ,  浅沼 肇

IPC: C07H15/20

CPC classification number: C07H15/203 ,  C07H15/20

Abstract: A process for the production of aryl 5-thio-beta-D- aldohexopyranoside derivatives represented by the general formula (||||||) by reacting, according to the following scheme, a 5-thio-D-aldohexopyranose derivative of the general formula (||) with Ar-OH (||||) in the presence of a phosphine represented by the general formula: PR R R and an azo reagent represented by the general formula: R -N=N-R .

Abstract translation: 一种通过下列方案制备由通式（|||||）表示的芳基5-硫代-β-D-羟基己吡喃糖苷衍生物的方法， 在由通式：PR 11 R 12 R 13表示的膦和由以下通式表示的偶氮试剂存在下，通式（||）与Ar-OH（|||） [R <21> -N = NR <22>。

公开(公告)号：WO03028646A3

公开(公告)日：2003-05-22

申请号：PCT/US0231212

申请日：2002-10-01

Applicant: UNIV ILLINOIS ,  HERGENROTHER PAUL J ,  MUSK DINTY J JR ,  DENAP JOHNA C B

Inventor： HERGENROTHER PAUL J ,  MUSK DINTY J JR ,  DENAP JOHNA C B

IPC: A61K31/4709 ,  A61K31/496 ,  A61K31/702 ,  A61K31/704 ,  A61K31/7048 ,  A61K38/14 ,  A61K38/17 ,  A61K45/06 ,  C07H15/00 ,  C07G11/00 ,  C07H15/20 ,  C07H17/00 ,  C12Q1/18

CPC classification number: A61K45/06 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/702 ,  A61K31/704 ,  A61K31/7048 ,  A61K38/14 ,  A61K38/17 ,  A61K2300/00

Abstract: Methods for treatment of antibiotic-resistant and multi-drug resistant bacterial infections are provided. The methods comprise administration of compositions which mimic plasmid incompatibility in bacteria, resulting in their sensitization to previously resistant drugs. Also provided herein are methods for screening compositions for the ability to mimic plasmid incompatibility by inhibiting Rep protein or by destabilizing RNA/RNA stem loop "kissing" structures. The invention also encompasses compositions identified by the screening methods disclosed herein.

Abstract translation: 提供了治疗抗生素耐药性和多重耐药性细菌感染的方法。 该方法包括施用模拟细菌中的质粒不相容性的组合物，导致其对先前的抗药性敏感。 本文还提供了用于通过抑制Rep蛋白或通过使RNA / RNA茎环“接吻”结构不稳定来筛选组合物以模拟质粒不相容性的能力的方法。 本发明还包括通过本文公开的筛选方法鉴定的组合物。

公开(公告)号：WO01054702A1

公开(公告)日：2001-08-02

申请号：PCT/SE2001/000167

申请日：2001-01-30

IPC: C07H15/203 ,  A61K31/7034 ,  A61K45/00 ,  A61P35/00 ,  A61P43/00 ,  C07H15/04 ,  C07H15/20 ,  A61K31/7028 ,  C07H19/04

CPC classification number: A61K31/7004 ,  C07H15/04 ,  C07H15/20 ,  A61K31/535 ,  A61K31/38 ,  A61K31/35 ,  A61K31/195 ,  A61K2300/00

Abstract: The present invention relates to combinations of xylose compounds with other pharmaceutically active compounds, to pharmaceutical compositions comprising said combinations, as well as to use of these combinations for the manufacture of a medicament for the treatment of proliferative disorders. In another aspect, the present invention relates to novel xylose compounds, to pharmaceutical compositions comprising said compounds, and to use of these compounds for the manufacture of a medicament for the treatment of proliferative disorders.

Abstract translation: 本发明涉及木糖化合物与其它药学活性化合物的组合，包括所述组合的药物组合物，以及这些组合用于制备用于治疗增殖性疾病的药物的用途。 另一方面，本发明涉及新颖的木糖化合物，包含所述化合物的药物组合物，以及这些化合物用于制备用于治疗增殖性疾病的药物的用途。

公开(公告)号：WO99058540A2

公开(公告)日：1999-11-18

申请号：PCT/CA1999/000399

申请日：1999-04-29

IPC: C07H7/02 ,  A61K31/351 ,  A61K31/70 ,  A61K31/7004 ,  A61K31/7008 ,  A61P1/00 ,  A61P1/06 ,  A61P1/12 ,  A61P31/04 ,  C07D309/10 ,  C07H7/04 ,  C07H15/20 ,  C07H15/26 ,  C07H

CPC classification number: C07H15/20 ,  C07H15/26

Abstract: Disclosed are novel 1-galactose derivatives having a carbon- or nitrogen-containing aglycon linkage. The disclosed compounds inhibit binding of toxins, such as heat-labile enterotoxin or cholera toxin, to their receptors either in vitro or in vivo. The disclosed compounds also inhibit binding of enterovirulent organisms (e.g., bacteria, virus, fungi, and the like), such as Vibrio cholerae and enterotoxigenic strains of Escherichia coli, to their cell surface receptors.

Abstract translation: 公开了具有含碳或含氮糖苷配基键的新颖的1-半乳糖衍生物。 所公开的化合物在体外或体内抑制毒素如热不稳定肠毒素或霍乱毒素与其受体的结合。 所公开的化合物还抑制肠病毒生物体（例如细菌，病毒，真菌等）与其大肠杆菌的结合，例如霍乱弧菌和肠毒素致病菌株对其细胞表面受体的结合。

公开(公告)号：WO9850049A9

公开(公告)日：1999-03-25

申请号：PCT/US9809255

申请日：1998-05-06

Applicant: CORNELL RES FOUNDATION INC

Inventor： OBENDORF RALPH L ,  HORBOWICZ MARCIN

IPC: C07H15/207 ,  A61K31/70 ,  A61K31/715 ,  C07C31/18 ,  C07H15/20

CPC classification number: C07H15/207 ,  Y10S514/866

Abstract: The present invention describes isolated Fagopyritol A1, isolated Fagopyritol A2, and isolated Fagopyritol B3. Compositions which include two or more of Fagopyritol A1, Fagopyritol A2, Fagopyritol B1, Fagopyritol B2, Fagopyritol B3, and D-chiro-inositol, at least one of which is an isolated Fagopyritol A1, isolated Fagopyritol A2, or isolated Fagopyritol B3, are also disclosed. Methods for preparing substantially pure Fagopyritol A1, Fagopyritol A2, Fagopyritol B1, Fagopyritol B2, Fagopyritol B3, or mixtures thereof from buckwheat are also described. The fagopyritols can be used to prepare pharmaceutical compositions, the administration of which can be used to treat diabetes.

Abstract translation: 本发明描述了分离的Fagopyritol A1，分离的Fagopyritol A2和分离的Fagopyritol B3。 包含Fagopyritol A1，Fagopyritol A2，Fagopyritol B1，Fagopyritol B2，Fagopyritol B3和D-手性肌醇两种或更多种的组合物，其中至少一种是分离的Fagopyritol A1，分离的Fagopyritol A2或分离的Fagopyritol B3 也披露。 还描述了从荞麦制备基本上纯的Fagopyritol A1，Fagopyritol A2，Fagopyritol B1，Fagopyritol B2，Fagopyritol B3或其混合物的方法。 吡咯并吡喃可用于制备药物组合物，其施用可用于治疗糖尿病。

公开(公告)号：WO9821222A3

公开(公告)日：1998-07-16

申请号：PCT/CA9700864

申请日：1997-11-14

Applicant: SYNSORB BIOTECH INC ,  HINDSGAUL OLE

Inventor： HINDSGAUL OLE

IPC: C07H15/14 ,  A61K31/7028 ,  A61K31/7034 ,  A61P31/04 ,  A61P43/00 ,  C07H5/10 ,  C07H15/18 ,  C07H15/20 ,  C07H15/203 ,  C07H15/22 ,  C40B40/12 ,  C07H15/00

CPC classification number: C07H5/10 ,  B01J2219/00731 ,  C07H15/18 ,  C07H15/203 ,  C40B40/12

Abstract: Disclosed are novel 1-galactose derivatives which inhibit binding of toxins, such as heat-labile enterotoxin or cholera toxin, to their receptors either in vitro or in vivo. Additionally disclosed are compounds which inhibit binding of enterovirulent organisms (e.g., bacteria, virus, fungi, and the like), such as Vibrio cholerae and enterotoxigenic strains of Escherichia coli, to their cell surface receptors. 00000

Abstract translation: 公开了新颖的1-半乳糖衍生物，其在体外或体内抑制毒素如热不稳定肠毒素或霍乱毒素与其受体的结合。 另外公开了抑制肠病毒生物体（例如细菌，病毒，真菌等）如霍乱弧菌和大肠杆菌肠毒素毒株与其细胞表面受体的结合的化合物。 00000

公开(公告)号：WO9816184A3

公开(公告)日：1998-05-28

申请号：PCT/US9718387

申请日：1997-10-15

Applicant: ICN PHARMACEUTICALS ,  WANG GUANGYI ,  TAM ROBERT ,  AVERTT DEVERON

Inventor： WANG GUANGYI ,  TAM ROBERT ,  AVERTT DEVERON

IPC: C07H15/20 ,  A61K31/519 ,  A61K31/52 ,  A61K31/522 ,  A61K31/70 ,  A61K31/7042 ,  A61K31/7052 ,  A61K31/7056 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7072 ,  A61K31/7076 ,  A61K31/708 ,  A61K31/7115 ,  A61K45/06 ,  A61P1/04 ,  A61P3/10 ,  A61P11/06 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/06 ,  A61P29/00 ,  A61P31/00 ,  A61P33/00 ,  A61P35/00 ,  A61P37/02 ,  A61P37/06 ,  A61P43/00 ,  C07H19/02 ,  C07H19/04 ,  C07H19/14 ,  C07H19/16 ,  C07H19/23 ,  C07H19/24 ,  A61K

CPC classification number: C07H19/16 ,  A61K31/519 ,  A61K31/52 ,  A61K31/522 ,  A61K31/70 ,  A61K31/7056 ,  A61K31/7076 ,  A61K31/7115 ,  A61K45/06 ,  C07H19/04

Abstract: Novel purine L-nucleoside compounds are disclosed, in which both the purine rings and the sugar are either modified, functionalized or both. The novel compounds or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, and infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Th1 and Th2. 00000

Abstract translation: 公开了新型嘌呤L-核苷化合物，其中嘌呤环和糖都被修饰，官能化或两者都是。 新化合物或其药学上可接受的酯或其盐可以用于药物组合物中，并且这种组合物可用于治疗感染，感染肿瘤或自身免疫性疾病。 新化合物也可用于调节免疫系统的方面，包括Th1和Th2的调节。 00000