公开(公告)号：US20090036431A1

公开(公告)日：2009-02-05

申请号：US12174195

申请日：2008-07-16

Applicant: Laurence GAUZY ,  Herve BOUCHARD ,  Ravi V.J. CHARI ,  Alain COMMERCON ,  Robert ZHAO ,  Yonghong DENG ,  Wei LI

Inventor： Laurence GAUZY ,  Herve BOUCHARD ,  Ravi V.J. CHARI ,  Alain COMMERCON ,  Robert ZHAO ,  Yonghong DENG ,  Wei LI

IPC: A61K31/551 ,  C07D487/14 ,  C07K16/00 ,  C12N5/02 ,  A61P35/04 ,  C07K14/54 ,  C07K2/00

CPC classification number: C07D487/04

Abstract: The present invention is related to new tomaymycin derivatives, their process of preparation and their therapeutic uses.

Abstract translation: 本发明涉及新的茅屋霉素衍生物，其制备方法及其治疗用途。

公开(公告)号：US20080108654A1

公开(公告)日：2008-05-08

申请号：US11972314

申请日：2008-01-10

Applicant: Marcel PATEK ,  Anil NAIR ,  Augustin HITTINGER ,  Conception NEMECEK ,  Daniel BOND ,  Greg HARLOW ,  Herve BOUCHARD ,  Jacques MAUGER ,  Jean-Luc MALLERON ,  Mark PALERMO ,  Fahad AL-OBEIDI ,  Thomas FAITG ,  Hartmut STROBEL ,  Sven RUF ,  Kurt RITTER ,  Youssef EL-AHMAD ,  Dominique LESUISSE

Inventor： Marcel PATEK ,  Anil NAIR ,  Augustin HITTINGER ,  Conception NEMECEK ,  Daniel BOND ,  Greg HARLOW ,  Herve BOUCHARD ,  Jacques MAUGER ,  Jean-Luc MALLERON ,  Mark PALERMO ,  Fahad AL-OBEIDI ,  Thomas FAITG ,  Hartmut STROBEL ,  Sven RUF ,  Kurt RITTER ,  Youssef EL-AHMAD ,  Dominique LESUISSE

IPC: A61K31/47 ,  C07D401/02 ,  C07D401/14 ,  A61K31/444 ,  A61P11/06 ,  A61P25/00 ,  A61P35/00 ,  C12N9/99 ,  A61K31/4439

CPC classification number: C07D401/06 ,  C07D401/14

Abstract: The disclosure relates to a cyclic urea compound of formula I: as defined herein, to the process for its preparation, pharmaceutical composition comprising it and its pharmaceutical use as an inhibitor on a protein kinase. Thus, the compound of formula I is useful for preventing or treating a physiological disorder capable of being modulated by inhibiting the activity of a protein kinase, such as a solid tumor.

Abstract translation: 本公开涉及式I的环脲化合物：如本文所定义，其制备方法，包含其的药物组合物及其作为蛋白激酶上的抑制剂的药物用途。 因此，式I化合物可用于预防或治疗能够通过抑制蛋白激酶如实体瘤的活性而被调节的生理障碍。

公开(公告)号：US20070232572A1

公开(公告)日：2007-10-04

申请号：US10773806

申请日：2004-02-06

Applicant: Augustin Hittinger ,  Thomas Caulfield ,  Patrick Mailliet ,  Herve Bouchard ,  Eliane Mandine ,  Jean-Louis Mergny ,  Lionel Guittat ,  Jean-Francois Riou ,  Dennis Gomez ,  Chafke Belmokhtar

Inventor： Augustin Hittinger ,  Thomas Caulfield ,  Patrick Mailliet ,  Herve Bouchard ,  Eliane Mandine ,  Jean-Louis Mergny ,  Lionel Guittat ,  Jean-Francois Riou ,  Dennis Gomez ,  Chafke Belmokhtar

IPC: A61K31/47 ,  A61K31/497 ,  A61K31/56 ,  A61K31/66 ,  C07D215/00

CPC classification number: C07D401/14 ,  C07D215/38

Abstract: The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which is quite specific. It also relates to novel chemical compounds and their therapeutic application in humans.

Abstract translation: 本发明涉及癌症治疗和具有非常特异性的作用机制的新型抗癌剂。 它还涉及新型化合物及其在人体中的治疗应用。

公开(公告)号：US20060199840A1

公开(公告)日：2006-09-07

申请号：US11222322

申请日：2005-09-08

Applicant: Herve Bouchard ,  Augustin Hittinger

Inventor： Herve Bouchard ,  Augustin Hittinger

IPC: C07D215/12 ,  A61K31/47

CPC classification number: C07D401/14 ,  C07D215/38 ,  C07D215/42 ,  C07D409/14

Abstract: The present invention relates to cancer therapy and to novel anticancer agents having a mechanism of action which is quite specific. It also relates to novel chemical compounds as well as their therapeutic application in humans.

公开(公告)号：US20050009894A1

公开(公告)日：2005-01-13

申请号：US10828012

申请日：2004-04-20

Applicant: Didier Babin ,  Alain Le Brun ,  Laurence Gauzy-Lazo ,  Herve Bouchard

Inventor： Didier Babin ,  Alain Le Brun ,  Laurence Gauzy-Lazo ,  Herve Bouchard

IPC: C07D491/056 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  A61P3/00 ,  A61P3/10 ,  A61P7/02 ,  A61P9/10 ,  A61P11/06 ,  A61P17/06 ,  A61P19/02 ,  A61P21/00 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D487/04 ,  C07D491/04 ,  C07D491/052 ,  C07D521/00 ,  A61K31/4196 ,  C07D471/02

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D487/04 ,  C07D491/04

Abstract: The invention discloses and claims benzimidazole compounds of formula (I): wherein X is C—R2; Y is C—R2 or C—R3; W and Z are each C—R3; R1 is an optionally substituted aryl, heteroaryl or a saturated 5- or 6-membered monocyclic heterocyclic radical or a bicyclic heterocyclic radical; and A5 is H or alkyl; or a stereoisomer, a racemate, an enantiomer or a diastereoisomer of said compound of formula (I) or a pharmaceutically acceptable salt thereof; the use of compounds of formula (I) for the treatment of a disorder of proliferation of blood vessels, uncontrolled angiogenesis, a fibrotic disorder, a disorder of proliferation of mesangial cells, a metabolic disorder, allergy, asthma, thrombosis, a disease of the nervous system, retinopathy, psoriasis, rheumatoid arthritis, diabetes, muscle degeneration, solid tumors and cancers, pharmaceutical compositions comprising a compound of formula (I) and one or more pharmaceutically acceptable adjuvants or diluents and pharmaceutical compositions comprising a compound of formula (I) and one or more. antimitiotic agents.

Abstract translation: 本发明公开并要求式（I）的苯并咪唑化合物：其中X是C-R2; Y为C-R2或C-R3; W和Z各自为C-R3; R 1是任选取代的芳基，杂芳基或饱和的5-或6-元单环杂环基或双环杂环基; A5是H或烷基; 或所述式（I）化合物的立体异构体，外消旋物，对映异构体或非对映异构体或其药学上可接受的盐; 使用式（I）化合物治疗血管增生障碍，不受控制的血管生成，纤维化病症，肾小球膜细胞增殖障碍，代谢紊乱，过敏，哮喘，血栓形成，疾病 神经系统，视网膜病变，银屑病，类风湿性关节炎，糖尿病，肌肉变性，实体瘤和癌症，包含式（I）化合物和一种或多种药学上可接受的佐剂或稀释剂的药物组合物和包含式（I）化合物的药物组合物， 和一个或多个。 抗菌剂。

公开(公告)号：US6040466A

公开(公告)日：2000-03-21

申请号：US271300

申请日：1999-03-17

Applicant: Herve Bouchard ,  Jean-Dominique Bourzat ,  Alain Commer.cedilla.on

Inventor： Herve Bouchard ,  Jean-Dominique Bourzat ,  Alain Commer.cedilla.on

IPC: C07D305/14

CPC classification number: C07D305/14

Abstract: New taxoids and methods of preparing new taxoids of general formula (I): ##STR1## in which: R.sub.4 represents an alkanoyloxy radical in which the alkanoyl portion contains 2 to 6 carbon atoms in an unbranched or branched chain, this radical unsubstituted or substituted with one or more halogen atoms, an alkoxy radical containing 1 to 4 carbon atoms, or alternatively R.sub.4 represents a cycloalkanoyloxy radical in which the cycloalkanoyl portion contains 4 to 8 carbon atoms, or alternatively R.sub.4 represents a benzoyloxy radical;R.sub.5 represents an alkoxy radical containing 1 to 4 carbon atoms, substituted by an alkylthio radical containing 1 to 4 carbon atoms; andZ represents a hydrogen atom or a radical of general formula: ##STR2## wherein such new taxoids display noteworthy anti-tumor and anti-leukemic properties.

Abstract translation: 新的紫杉烷类和通式（I）的新紫杉烷类的制备方法：其中：R4表示烷酰氧基，其中链烷酰基部分在无支链或支链上含有2-6个碳原子，该未取代的基团或被一个或多个 卤原子，含有1至4个碳原子的烷氧基，或者R4表示环烷酰氧基，其中环烷酰基部分含有4至8个碳原子，或者R4表示苯并氧基; R5代表含有1至4个碳原子的烷氧基，被含有1至4个碳原子的烷硫基取代; Z表示氢原子或通式的基团：其中这种新的紫杉醇显示出显着的抗肿瘤和抗白血病性质。

公开(公告)号：US5906990A

公开(公告)日：1999-05-25

申请号：US930814

申请日：1997-10-10

Applicant: Herve Bouchard ,  Alain Commercon

Inventor： Herve Bouchard ,  Alain Commercon

IPC: A61K31/335 ,  A61K31/337 ,  A61P35/00 ,  C07D305/14 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12

CPC classification number: C07D407/12 ,  C07D305/14 ,  C07D409/12 ,  C07D417/12

Abstract: The present invention relates to novel taxoids of general formula: ##STR1## in which: Z represents a hydrogen atom or a radical of general formula: ##STR2##

Abstract translation: PCT No.PCT / FR96 / 00559 Sec。 371日期：1997年10月10日 102（e）日期1997年10月10日PCT提交1996年4月12日PCT公布。 公开号WO96 / 32387 日期：1996年10月17日本发明涉及通式的新型紫杉烷类：其中：Z表示氢原子或通式如下的基团：

公开(公告)号：US08668910B2

公开(公告)日：2014-03-11

申请号：US13499459

申请日：2010-09-30

Applicant: Herve Bouchard ,  Alain Commercon ,  Claudia Fromond ,  Vincent Mikol ,  Fabienne Parker ,  Ingrid Sassoon ,  Daniel Tavares

Inventor： Herve Bouchard ,  Alain Commercon ,  Claudia Fromond ,  Vincent Mikol ,  Fabienne Parker ,  Ingrid Sassoon ,  Daniel Tavares

IPC: A61K39/395 ,  C07K16/18 ,  C07K16/28

CPC classification number: C07K16/30 ,  A61K47/6803 ,  A61K47/6809 ,  A61K47/6849 ,  A61K2039/505 ,  C07K16/2866 ,  C07K2317/24 ,  C07K2317/34 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/73 ,  C07K2317/76 ,  C07K2317/92

Abstract: The present disclosure relates to an antibody or an epitope-binding fragment thereof that specifically binds to an EphA2 receptor. It further relates to a conjugate comprising a cytotoxic agent which is covalently bound to the antibody and a method for preparing such a conjugate.

Abstract translation: 本公开涉及特异性结合EphA2受体的抗体或其表位结合片段。 它还涉及包含与抗体共价结合的细胞毒性剂的缀合物和制备这种缀合物的方法。

公开(公告)号：US08288425B2

公开(公告)日：2012-10-16

申请号：US11029064

申请日：2005-01-04

Applicant: Michael L. Edwards ,  Paul J. Cox ,  Shelley Amendola ,  Stephanie D. Deprets ,  Timothy A. Gillespy ,  Christopher D. Edlin ,  Andrew D. Morley ,  Charles J. Gardner ,  Brian Pedgrift ,  Herve Bouchard ,  Didier Babin ,  Laurence Gauzy ,  Alain Le-Brun ,  Tahir N. Majid ,  John C. Reader ,  Lloyd J. Payne ,  Nawaz M. Khan ,  Michael Cherry

Inventor： Michael L. Edwards ,  Paul J. Cox ,  Shelley Amendola ,  Stephanie D. Deprets ,  Timothy A. Gillespy ,  Christopher D. Edlin ,  Andrew D. Morley ,  Charles J. Gardner ,  Brian Pedgrift ,  Herve Bouchard ,  Didier Babin ,  Laurence Gauzy ,  Alain Le-Brun ,  Tahir N. Majid ,  John C. Reader ,  Lloyd J. Payne ,  Nawaz M. Khan ,  Michael Cherry

IPC: A61K31/4184 ,  C07D235/18

CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04

Abstract: The invention is directed to physiologically active compounds of the general formula (Ix) and compositions containing such compounds, and their prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their prodrugs, as well as to novel compounds within the scope of formula (Ix), and to processes for their preparation. Such compounds and compositions have valuable pharmaceutical properties, in particular the ability to inhibit kinases.

Abstract translation: 本发明涉及通式（Ix）的生理活性化合物和含有这些化合物及其前药以及这些化合物及其前药的药学上可接受的盐和溶剂合物的组合物，以及式（Ix）范围内的新化合物 Ix），以及它们的制备过程。 这些化合物和组合物具有有价值的药物特性，特别是抑制激酶的能力。

公开(公告)号：US20120201828A1

公开(公告)日：2012-08-09

申请号：US13499459

申请日：2010-09-30

Applicant: Herve Bouchard ,  Alain Commercon ,  Claudia Fromond ,  Vincent Mikol ,  Fabienne Parker ,  Ingrid Sassoon ,  Daniel Tavares

Inventor： Herve Bouchard ,  Alain Commercon ,  Claudia Fromond ,  Vincent Mikol ,  Fabienne Parker ,  Ingrid Sassoon ,  Daniel Tavares

IPC: A61K39/395 ,  A61J1/00 ,  A61P35/02 ,  C07K16/28 ,  A61P35/00

CPC classification number: C07K16/30 ,  A61K47/6803 ,  A61K47/6809 ,  A61K47/6849 ,  A61K2039/505 ,  C07K16/2866 ,  C07K2317/24 ,  C07K2317/34 ,  C07K2317/56 ,  C07K2317/565 ,  C07K2317/73 ,  C07K2317/76 ,  C07K2317/92

Abstract: The present disclosure relates to an antibody or an epitope-binding fragment thereof that specifically binds to an EphA2 receptor. It further relates to a conjugate comprising a cytotoxic agent which is co-valently bound to the antibody and a method for preparing such a conjugate.

Abstract translation: 本公开涉及特异性结合EphA2受体的抗体或其表位结合片段。 它还涉及包含与抗体共价结合的细胞毒性剂的缀合物和制备这种缀合物的方法。