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1. 发明申请

WO2008107478A8 QUINOLINONE DERIVATIVES AS PARP AND TANK INHIBITORS 审中-公开
标题翻译：喹诺酮衍生物作为PARP和油墨抑制剂
公开(公告)号：WO2008107478A8
公开(公告)日：2008-10-23
申请号：PCT/EP2008052764
申请日：2008-03-07
申请人： JANSSEN PHARMACEUTICA NV , VIALARD JORGE EDUARDO , ANGIBAUD PATRICK RENE , MEVELLEC LAURENCE ANNE , MEYER CHRISTOPHE , FREYNE EDDY JEAN EDGARD , PILATTE ISABELLE NOELLE CONSTANCE , ROUX BRUNO , PASQUIER ELISABETH THERESE JEANNE , BOURDREZ XAVIER MARC , ADELINET CHRISTOPHE DENIS , MARCONNET-DECRANE LAURENCE FRANCOISE BERNADETTE , MACRITCHIE JACQUELINE ANNE , DUFFY JAMES EDWARD STEWART , OWENS ANDREW PATE , STORCK PIERRE-HENRI , PONCELET VIRGINIE SOPHIE
发明人： VIALARD JORGE EDUARDO , ANGIBAUD PATRICK RENE , MEVELLEC LAURENCE ANNE , MEYER CHRISTOPHE , FREYNE EDDY JEAN EDGARD , PILATTE ISABELLE NOELLE CONSTANCE , ROUX BRUNO , PASQUIER ELISABETH THERESE JEANNE , BOURDREZ XAVIER MARC , ADELINET CHRISTOPHE DENIS , MARCONNET-DECRANE LAURENCE FRACOISE BERNADETTE , MACRITCHIE JACQUELINE ANNE , DUFFY JAMES EDWARD STEWART , OWENS ANDREW PATE , STORCK PIERRE-HENRI , PONCELET VIRGINIE SOPHIE
IPC分类号： C07D215/22 , A61K31/4704
CPC分类号： C07D215/227 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： The present invention provides compounds of Formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , n, m and X have defined meanings.
摘要翻译：本发明提供式（I）化合物，其作为PARP抑制剂的用途以及包含所述化合物的药物组合物，其中R 1，R 2，R 2， R 4，R 4，R 5，R 6，R 7，n，m和 X已经定义了含义。

2. 发明专利

CA2678248C QUINOLINONE DERIVATIVES AS PARP AND TANK INHIBITORS 未知
公开(公告)号：CA2678248C
公开(公告)日：2016-06-28
申请号：CA2678248
申请日：2008-03-07
申请人： JANSSEN PHARMACEUTICA NV
发明人： VIALARD JORGE EDUARDO , ANGIBAUD PATRICK RENE , MEVELLEC LAURENCE ANNE , MEYER CHRISTOPHE , FREYNE EDDY JEAN EDGARD , PILATTE ISABELLE NOELLE CONSTANCE , ROUX BRUNO , PASQUIER ELISABETH THERESE JEANNE , BOURDREZ XAVIER MARC , ADELINET CHRISTOPHE DENIS , MARCONNET-DECRANE LAURENCE FRANCOISE BERNADETTE , MACRITCHIE JACQUELINE ANNE , DUFFY JAMES EDWARD STEWART , OWENS ANDREW PATE , STORCK PIERRE-HENRI , PONCELET VIRGINIE SOPHIE
IPC分类号： C07D215/22 , A61K31/4704
摘要： The present invention provides compounds of Formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds, wherein R1, R2, R3, R4, R5, R6, R7, n, m and X have defined meanings.

5. 发明专利

PT1037880E 未知
公开(公告)号：PT1037880E
公开(公告)日：2004-11-30
申请号：PT98965820
申请日：1998-12-08
申请人： JANSSEN PHARMACEUTICA NV
发明人： VENET MARC GASTON , MABIRE DOMINIQUE , ADELINET CHRISTOPHE DENIS , CSOKA IMRE CHRISTIAN
IPC分类号： A61K31/4164 , A61K31/4196 , A61K31/427 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61P17/00 , A61P43/00 , C07D207/335 , C07D207/337 , C07D213/40 , C07D233/56 , C07D233/61 , C07D249/08 , C07D257/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D521/00
摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or -NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het is triazolyl; and Het1 represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.

6. 发明专利

SI1037880T1 RETINOIC ACID MIMETIC ANILIDES 未知
公开(公告)号：SI1037880T1
公开(公告)日：2004-10-31
申请号：SI9830681
申请日：1998-12-08
申请人： JANSSEN PHARMACEUTICA NV
发明人： MABIRE DOMINIQUE , ADELINET CHRISTOPHE DENIS , CSOKA IMRE CHRISTIAN , VENET MARC GASTON
IPC分类号： A61K31/4164 , A61K31/4196 , A61K31/427 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61P17/00 , A61P43/00 , C07D207/335 , C07D207/337 , C07D213/40 , C07D233/56 , C07D233/61 , C07D249/08 , C07D257/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D521/00
摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or -NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het is triazolyl; and Het1 represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.

7. 发明专利

ID21498A 未知
公开(公告)号：ID21498A
公开(公告)日：1999-06-17
申请号：ID981606
申请日：1998-12-10
申请人： JANSSEN PHARMACEUTICA NV
发明人： MABIRE DOMINIQUE , ADELINET CHRISTOPHE DENIS , CSOKA IMRE CHRISTIAN , VENET MARC GASTON
IPC分类号： A61K31/4164 , A61K31/4196 , A61K31/427 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61P17/00 , A61P43/00 , C07D207/335 , C07D207/337 , C07D213/40 , C07D233/56 , C07D233/61 , C07D249/08 , C07D257/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D521/00 , C07C303/40
摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or -NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het is triazolyl; and Het1 represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.

8. 发明专利

ES2224462T3 ANILIDAS MIMETICAS DEL ACIDO RETINOICO. 未知
公开(公告)号：ES2224462T3
公开(公告)日：2005-03-01
申请号：ES98965820
申请日：1998-12-08
申请人： JANSSEN PHARMACEUTICA NV
发明人： MABIRE DOMINIQUE , ADELINET CHRISTOPHE DENIS , CSOKA IMRE CHRISTIAN , VENET MARC GASTON
IPC分类号： A61K31/4164 , A61K31/4196 , A61K31/427 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61P17/00 , A61P43/00 , C07D207/335 , C07D207/337 , C07D213/40 , C07D233/56 , C07D233/61 , C07D249/08 , C07D257/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D521/00
摘要： Un compuesto que tiene la fórmula **(Fórmula)** un N-óxido, una sal de adición farmacéuticamente aceptable o una forma estereoquímicamente isómera del mismo, en el cual: X representa -O-, S-o NR3-; R1 representa hidrógeno, hidroxi, C1-6alquilo o arilo; R2 representa hidrógeno; C1-12alquilo; C3-7cicloalquilo; C2-8alquenilo; arilo; Het1; o C1-12alquilo sustituido con uno o dos sustituyentes seleccionados de C3-7cicloalquilo, hidroxi, C1-4alquiloxi, ciano, amino, mono- y y di(C1-4alquil)amino, mono- o o ddi(aril-C1, 4alquil)amino, di(aril-C1-4alquil)aminocarboniloxi, (C1-4alquil)(aril-C1-4 alquil)amino, mono- y di(aril)-amino, (C1-4alquil)(di(C1-4alquil)amino-C1-4alquil)-amino, pirrolidinilo, piperidinilo, piperazinilo sustituido opcionalmente con C1, 4alquilo, morfolinilo, perhidro-azepinilo, carboxilo, C C1-4 alquiloxi-carbonilo, aminocarbonilo, mono- y di(C1-4alquil)-aminocarbonilo, arilo, ariloxi y ariltio; o R1 y R2, considerados juntos, pueden formar un radical bivalente de fórmula -R1-R2- en donde -R1-R2- representa-(CH2)n- en donde n es 2, 3, 4, 5 ó 6; R3 representa hidrógeno, C1-6alquilo, arilo, Het1 o C1-6alquilo sustituido con arilo o Het1; R4 representa hidrógeno; hidroxi; mercapto; C1-6alquil-oxi; C C1-6alquiltio; ariloxi; ariltio; Het1-oxi; Het1-tio; C C1-12 alquilosustituido opcionalmente con uno, dos o tres sustituyentes seleccionados cada uno independientemente de halo, hidroxi, mercapto, C1-6alquiloxi, C1-6alquiltio, ariloxi, ariltio, Het1-oxi, , Het1-tio, C3-7cicloalquilo sustituido opcionalmente con hidroxicarbonil-C1-6alquilo, carboxilo, C1-6alquiloxicarbonilo, aril-C1-6alquiloxi, arilC1-6alquiltio, arilo, Het1; C2-8alquenilo sustituido opcionalmente con uno, dos o tres sustituyentes seleccionados de halo, C3-7cicloalquilo, arilo, Het1; C2-8alquinilosustituido opcionalmente con halo, C3-7cicloalquilo, arilo; C3-7cicloalquilo sustituido opcionalmente con C1-6alquilo o arilo; C5-7ciclo-alquenilo sustituido opcionalmente con C1-6alquilo o arilo; arilo; Het1; o-Alk - NR3R5 (i) o -NR3R5 (ii) en donde Alk representa C1-6alcanodiílo; y R5 representa hidrógeno, C1-6alquilo, arilo, Het1, (aril o Het1)C1-6alquilo, (aril o Het1)-carbonilo o o (aril o o Het1) C1-6alquiloxicarbonilo; arilo representa indanilo, indenilo, naftilo, 5, 6, 7, 8-tetrahidro-2-naftalenilo; fenilo; donde dicho indanilo, indenilo, naftilo o fenilo puede estar sustituido con uno, dos, tres, cuatro o cinco sustituyentes seleccionados cada uno independientemente de hidroxi, halo, nitro, ciano, amino, azido, mono- o o di(C1-6alquil)amino, C1-6alquilcarbonilamino, C1-6alquilo, polihalo-C1-6alquilo, hidroxi-C1-6alquilo, fenilo, feniloxi, fenil-C1-6alquiloxi, piridinil-C1-6 alquiloxi, C1-6alquiloxi, formilo, carboxilo, y C1-6alquilcarbonilo; o dos átomos de carbono adyacentes en dicho fenilo pueden estar sustituidos por un solo radical bivalente que tiene la fórmula C1-12alcanodiílo o polihalo C1-12alcanodiílo; Het representa un heterociclo insaturado seleccionado de pirrolilo, pirazolilo, imidazolilo, triazolilo, tetrazolilo y piridinilo; pudiendo estar cada uno de dichos heterociclos insaturados sustituido opcionalmente con amino, mercapto, C1-6alquilo, C1-6alquiltio o arilo; y Het1 representa un heterociclo monocíclico seleccionado de pirrolidinilo, pirrolilo, pirazolilo, imidazolilo, 1, 3, 4-tria -zolilo, 1, 2, 4-triazolilo, tetrahidro-furanilo, furanilo, tiolanilo, tienilo, dioxolanilo, isoxazolilo, oxazolilo, isotiazolilo, tiazolilo, isoxazolidinilo, oxazolidinilo, isotiazolidinilo, tiazolidinilo, piperidinilo, piridinilo, piperazinilo, piridazinilo, pirimidinilo, pirazinilo, 1, 2, 3-triazinilo, 1, 2, 4-triazinilo, tetrahidropiranilo, piranilo, morfolinilo y dioxanilo; pudiendo estar cada uno de dichos heterociclos monocíclicos sustituido opcionalmente con uno o dos sustituyentes seleccionados cada uno independientemente de C1, 4alquilo, hidroxi, amino, halo, arilo, arilcar.

9. 发明专利

AT270277T 未知
公开(公告)号：AT270277T
公开(公告)日：2004-07-15
申请号：AT98965820
申请日：1998-12-08
申请人： JANSSEN PHARMACEUTICA NV
发明人： MABIRE DOMINIQUE , ADELINET CHRISTOPHE DENIS , CSOKA IMRE CHRISTIAN , VENET MARC GASTON
IPC分类号： A61K31/4164 , A61K31/4196 , A61K31/427 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61P17/00 , A61P43/00 , C07D207/335 , C07D207/337 , C07D213/40 , C07D233/56 , C07D233/61 , C07D249/08 , C07D257/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D521/00
摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or -NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het is triazolyl; and Het1 represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.

10. 发明专利

PL341059A1 MIMETIC ANILIDES OF RETINOIC ACID 未知
公开(公告)号：PL341059A1
公开(公告)日：2001-03-26
申请号：PL34105998
申请日：1998-12-08
申请人： JANSSEN PHARMACEUTICA NV
发明人： MABIRE DOMINIQUE , ADELINET CHRISTOPHE DENIS , CSOKA IMRE CHRISTIAN , VENET MARC GASTON
IPC分类号： A61K31/4164 , A61K31/4196 , A61K31/427 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61P17/00 , A61P43/00 , C07D207/335 , C07D207/337 , C07D213/40 , C07D233/56 , C07D233/61 , C07D249/08 , C07D257/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D521/00
摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein X represents O, S or NR3; R1 represents hydrogen, hydroxy, C1-6alkyl or aryl; R2 represents hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl; aryl; Het1; R3 represents hydrogen, optionally substituted C1-6alkyl, aryl, Het1; R4 represents hydrogen; hydroxy; mercapto; C1-6alkyloxy; C1-6alkylthio; aryloxy; arylthio; Het1-oxy; Het1-thio; optionally substituted C1-12alkyl; optionally substituted C2-8alkenyl; optionally substituted C2-8alkynyl; optionally substituted C3-7cycloalkyl; optionally substituted C5-7cycloalkenyl; aryl; Het1; or -Alk-NR3R5 (i) or -NR3R5 (ii) wherein Alk represents C1-6alkanediyl; and R5 represents hydrogen, C1-6alkyl, aryl, Het1, (aryl or Het1)C1-6alkyl, (aryl or Het1)carbonyl or (aryl or Het1)C1-6alkyloxycarbonyl; aryl represents optionally substituted indanyl, indenyl, naphtyl, 5,6,7,8-tetrahydro-2-naphtalenyl or phenyl; Het is triazolyl; and Het1 represents an optionally substituted monocyclic or bicyclic heterocycle; having retinoic mimetic activity; their preparation, compositions containing them and their use as a medicine.

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