公开(公告)号：JP2002265448A

公开(公告)日：2002-09-18

申请号：JP2002009645

申请日：2002-01-18

Applicant: SERVIER LAB

Inventor： CASARA PATRICK ,  LE DIGUARHER THIERRY ,  DOREY GILBERT ,  HICKMAN JOHN ,  PIERRE ALAIN ,  TUCKER GORDON ,  GUILBAUD NICOLAS

IPC: C07C317/00 ,  A61K31/4164 ,  A61K31/417 ,  A61K31/4178 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/454 ,  A61P9/00 ,  A61P9/10 ,  A61P25/00 ,  A61P35/00 ,  C07D213/36 ,  C07D213/38 ,  C07D213/57 ,  C07D233/54 ,  C07D233/58 ,  C07D233/61 ,  C07D233/64 ,  C07D401/06

Abstract: PROBLEM TO BE SOLVED: To provide a compound having a specific structure, selectively inhibiting FTase with respect to GGTase and useful for the treatment of diseases relating to the intracellular signal transduction through Ras protein, etc., and the investigation of pathology relating to angiogenetic amplification. SOLUTION: The objective compound is expressed by formula (I) [X is a bond, an alkylene, S(O)n or the like; Y is an aryl, a heteroaryl or the like; R1 to R4 are each independently H, an aryl or the like or together form a bond, a condensed benzene ring or the like; T is CH(R5 ) (R5 is H or the like) or the like; V is H, a substituted aryl or the like; A2 is [C(R6 ) (R'6 )] (R6 and R'6 are each H or the like; and (p) is 0-4); and R7 and R8 are each H or the like]. The invention further relates to its isomer, diastereomer, pharmacologically permissible acid or base and its addition salt.

公开(公告)号：WO02057223A3

公开(公告)日：2002-11-28

申请号：PCT/FR0200147

申请日：2002-01-16

Applicant: SERVIER LAB ,  CASARA PATRICK ,  LE DIGUARHER THIERRY ,  DOREY GILBERT ,  HICKMAN JOHN ,  PIERRE ALAIN ,  TUCKER GORDON ,  GUILBAUD NICOLAS ,  ORTUNO JEAN-CLAUDE ,  FAUCHERE JEAN-LUC

Inventor： CASARA PATRICK ,  LE DIGUARHER THIERRY ,  DOREY GILBERT ,  HICKMAN JOHN ,  PIERRE ALAIN ,  TUCKER GORDON ,  GUILBAUD NICOLAS ,  ORTUNO JEAN-CLAUDE ,  FAUCHERE JEAN-LUC

IPC: A61P35/00 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  A61K31/415 ,  C07D401/12

CPC classification number: C07D401/14 ,  C07D403/12 ,  C07D413/12

Abstract: A compound having formula (I), wherein X denotes an alkylene group or chain, CO, S(O)n, -S(O)n-A1-, -CO-A1-, -A1-S(O)n-A'1, or A1-CO-A'1-; Y denotes a substituted or non-substituted aryl, heteroaryl, cycloalkyl or heterocyclalkyl group; W denotes a CO or CH2 group; T denotes a N(R1)- or N(R1)CO- group; V denotes a hydrogen atom or a substituted or non-substituted aryl or heteroaryl group; A2 denotes a [C(R2)(R'2)]p group; R1 and R2 are as defined in the description. Medicaments.

Abstract translation: 具有式（I）的化合物，其中X表示亚烷基或链，CO，S（O）n，-S（O）n -A1，-CO-A1-，-A1-S（O） A'1或A1-CO-A'1-; Y表示取代或未取代的芳基，杂芳基，环烷基或杂环烷基; W表示CO或CH 2基团; T表示N（R1） - 或N（R1）CO-基团; V表示氢原子或取代或未取代的芳基或杂芳基; A2表示[C（R2）（R'2）] p基团; R1和R2如说明书中所定义。 药物。

公开(公告)号：WO2010007248A3

公开(公告)日：2010-04-08

申请号：PCT/FR2009000855

申请日：2009-07-10

Applicant: SERVIER LAB ,  CASARA PATRICK ,  LE DIGUARHER THIERRY ,  DURAND DIDIER ,  GENESTE OLIVIER ,  HICKMAN JOHN

Inventor： CASARA PATRICK ,  LE DIGUARHER THIERRY ,  DURAND DIDIER ,  GENESTE OLIVIER ,  HICKMAN JOHN

IPC: C07D471/04 ,  A61K31/498 ,  A61K31/4985 ,  A61P35/00 ,  C07D207/20 ,  C07D211/70 ,  C07D213/36 ,  C07D241/04 ,  C07D471/14 ,  C07D487/04

CPC classification number: C07D471/04 ,  C07D487/04

Abstract: Compounds of formula (I) in which: A is a (hetero)aromatic or non-(hetero)aromatic ring containing 5, 6 or 7 ring members, Z1, Z2 and Z3 are, independently of one another, a CH group or a nitrogen atom, with at least one of these three groups being a nitrogen atom, X is an alkylene chain as defined in the description, R2 is an aryl or heteroaryl group, and the R1 group is a group of formula (II) as defined in the description.

Abstract translation: 式（I）化合物，其中：A是含有5,6或7个环成员的（杂）芳族或非（杂）芳族环，Z 1，Z 2和Z 3彼此独立地是CH基团或 氮原子，并且这三个基团中的至少一个是氮原子，X是如说明书中所定义的亚烷基链，R 2是芳基或杂芳基，并且R 1基团是如上定义的式（II）的基团 说明。

公开(公告)号：MD4793C1

公开(公告)日：2022-09-30

申请号：MD20160018

申请日：2014-07-22

Applicant: SERVIER LAB ,  VERNALIS R&D LTD

Inventor： DAVIDSON JAMES EDWARD PAUL ,  MURRAY JAMES BROOKE ,  CHEN I-JEN ,  WALMSLEY CLAIRE ,  DODSWORTH MARK ,  MEISSNER JOHANNES W G ,  BROUGH PAUL ,  FEJES IMRE ,  TATAI JANOS ,  NYERGES MIKLOS ,  KOTSCHY ANDRAS ,  SZLAVIK ZOLTAN ,  GENESTE OLIVIER ,  LE TIRAN ARNAUD ,  LE DIGUARHER THIERRY ,  HENLIN JEAN-MICHEL ,  STARCK JÉRÔME-BENOÎT ,  GUILLOUZIC ANNE-FRANÇOISE ,  DE NANTEUIL GUILLAUME

IPC: C07D401/14 ,  A61K31/4709 ,  A61K31/4725 ,  A61P35/00 ,  A61P37/00 ,  C07D401/10 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04

Abstract: Invenţia se referă la compuşi noi de izoindolină sau izochinolină, la un procedeu de obţinere a lor şi la compoziţii farmaceutice care le conţin. Prezenta invenţie se referă, în special, la compuşii cu formula (I):unde substituenţii sunt definiţi în descrierea invenţiei. Compuşii, conform invenţiei, au proprietăţi pro-apoptotice, fapt ce permite utilizarea lor în patologii care implică un defect în apoptoză, cum ar fi, de exemplu, în tratamentul cancerului, bolilor autoimune şi bolilor sistemului imunitar.Revendicări: 35

公开(公告)号：MD4643C1

公开(公告)日：2020-03-31

申请号：MD20160016

申请日：2014-07-22

Applicant: SERVIER LAB ,  VERNALIS R&D LTD

Inventor： LE TIRAN ARNAUD ,  LE DIGUARHER THIERRY ,  STARCK JÉRÔME-BENOÎT ,  HENLIN JEAN-MICHEL ,  DE NANTEUIL GUILLAUME ,  GENESTE OLIVIER ,  DAVIDSON JAMES EDWARD PAUL ,  MURRAY JAMES BROOKE ,  CHEN I-JEN

IPC: C07D471/04 ,  A61K31/4709 ,  A61K31/4985 ,  A61P35/00 ,  A61P37/00 ,  C07D487/04 ,  C07D519/00

Abstract: Invenţia se referă la compuşi cu formula (I):Compuşii, conform invenţiei, pot fi utili în tratamentul formelor de cancer rezistente la chimio- sau radioterapie, în hemopatiile maligne şi cancerul pulmonar cu celule mici.Invenţia se referă, de asemenea, la un procedeu de obţinere a compuşilor cu formula (I) şi la compoziţii farmaceutice care cuprind, cel puţin, un compus cu formula (I) în combinaţie cu unul sau mai mulţi excipienţi acceptabili farmaceutic.

公开(公告)号：NZ716156A

公开(公告)日：2019-05-31

申请号：NZ71615614

申请日：2014-07-22

Applicant: SERVIER LAB ,  VERNALIS R&D LTD

Inventor： STARCK JÉRÔME-BENOÎT ,  HENLIN JEAN-MICHEL ,  DAVIDSON JAMES EDWARD PAUL ,  MURRAY JAMES BROOKE ,  LE TIRAN ARNAUD ,  DE NANTEUIL GUILLAUME ,  LE DIGUARHER THIERRY ,  GENESTE OLIVIER ,  CHEN I-JEN

IPC: C07D487/04 ,  A61K31/435 ,  A61P35/00 ,  A61P37/00 ,  C07D498/04

Abstract: The invention provides indolizine derivatives of formula (I): wherein Ra, Rb, Rc, Rd, T, R3, R4, R5, X, Y and Het are as defined in the description, useful as Bcl-2 inhibitors, method for the production thereof and pharmaceutical compositions containing same for the treatment of cancers, auto-immune diseases and diseases of the immune system.

公开(公告)号：CU24380B1

公开(公告)日：2019-02-04

申请号：CU20160011

申请日：2014-07-22

Applicant: SERVIER LAB ,  VERNALIS R&D LTD

Inventor： CHEN I-JEN ,  DAVIDSON JAMES EDWARD PAUL ,  DE NANTEUIL GUILLAUME ,  GENESTE OLIVIER ,  HENLIN JEAN- MICHEL ,  LE DIGUARHER THIERRY ,  LE TIRAN ARNAUD ,  MURRAY JAMES BROOKE ,  STARCK JÉRÔME-BENOÎT

IPC: A61K31/4709 ,  A61K31/4985 ,  A61P35/00 ,  A61P37/00 ,  C07D471/04 ,  C07D487/04 ,  C07D519/00

Abstract: La invención se refiere a compuestos de fórmula I como inhibidores selectivos de las proteínas de la familia Bcl-2 y composiciones farmaceúticas que los contienen, que pueden ser útiles en la fabricación de medicamentos destinados al tratamientos de cánceres , enfermedades autoinmunes y enfermedades del sistema inmune: ESPACIO PARA FÓRMULA I en el que Ra, Rb, Rc, Rd, T, R3, R4, R5, y G son como se definen en la descripción.

公开(公告)号：MD4551C1

公开(公告)日：2018-09-30

申请号：MD20140073

申请日：2014-07-15

Applicant: SERVIER LAB ,  VERNALIS R&D LTD

Inventor： LE TIRAN ARNAUD ,  LE DIGUARHER THIERRY ,  STARCK JÉRÔME-BENOÎT ,  HENLIN JEAN-MICHEL ,  GUILLOUZIC ANNE-FRANÇOISE ,  DE NANTEUIL GUILLAUME ,  GENESTE OLIVIER ,  DAVIDSON JAMES EDWARD PAUL ,  MURRAY JAMES BROOKE ,  CHEN I-JEN

IPC: C07D471/00 ,  A61K31/675 ,  A61P35/00 ,  C07F9/09 ,  C07F9/6558 ,  C07F9/6561

Abstract: Invenţia se referă la compuşii cu formula (I):unde X, Y, A1, A2, Ra, Rb, Rc, Rd, R3, R4, T şi R5 sunt definiţi în descrierea invenţiei, totodată R4 reprezintă un fenil sau piridin-5-il, substituit în poziţia para cu o grupare fosfat, preferabil cu gruparea -OPO(O-Na+)(O-Na+).Invenţia se referă, de asemenea, la un procedeu de obţinere a compuşilor cu formula (I), la compoziţii farmaceutice, care conţin un compus cu formula (I) sau o sare de adiţie a acestuia cu un acid sau o bază acceptabilă farmaceutic, şi la utilizarea compoziţiilor farmaceutice în fabricarea medicamentelor pentru tratarea cancerului, maladiilor autoimune şi ale sistemului imunitar.

公开(公告)号：AU2014294866B2

公开(公告)日：2018-09-27

申请号：AU2014294866

申请日：2014-07-22

Applicant: SERVIER LAB ,  VERNALIS R&D LTD

Inventor： CASARA PATRICK ,  LE DIGUARHER THIERRY ,  HENLIN JEAN-MICHEL ,  STARCK JEROME-BENOIT ,  LE TIRAN ARNAUD ,  DE NANTEUIL GUILLAUME ,  GENESTE OLIVIER ,  DAVIDSON JAMES EDWARD PAUL ,  MURRAY JAMES BROOKE ,  CHEN I-JEN ,  WALMSLEY CLAIRE ,  GRAHAM CHRISTOPHER JOHN ,  RAY STUART ,  MADDOX DANIEL ,  BEDFORD SIMON

IPC: C07D401/14 ,  A61K31/4709 ,  A61P35/00 ,  A61P37/00 ,  C07D401/10 ,  C07D405/14 ,  C07D471/04

Abstract: The invention relates to compounds of formula (I), wherein R

公开(公告)号：AU2014203808B2

公开(公告)日：2018-09-20

申请号：AU2014203808

申请日：2014-07-11

Applicant: SERVIER LAB ,  VERNALIS R&D LTD

Inventor： LE TIRAN ARNAUD ,  LE DIGUARHER THIERRY ,  STARCK JÉRÔME-BENOÎT ,  HENLIN JEAN-MICHEL ,  GUILLOUZIC ANNE-FRANÇOISE ,  DE NANTEUIL GUILLAUME ,  GENESTE OLIVIER ,  DAVIDSON JAMES EDWARD PAUL ,  MURRAY JAMES BROOKE ,  CHEN I-JEN

IPC: C07D217/16 ,  A61K31/4725 ,  A61K31/675 ,  A61P35/00 ,  A61P35/02 ,  A61P37/00 ,  C07D231/40 ,  C07D471/04

Abstract: Abstract Disclosed herein are substituted 1,2,3,4-tetrahydroisoquinoline compounds including a phosphate moiety. Also disclosed are pharmaceuticals comprising the said compounds and methods and uses of the compounds or pharmaceuticals in therapy. Such methods or uses including in the treatment of cancers or disorders of the immune system. The compounds being of general formula (I): N. N NY_ ) Y-A2