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1. 发明申请

WO2006043090A1 IMIDAZO[4,5-B]PYRIDIN-2-ONE AND OXAZOLO[4,5-B]PYRIDIN-2-ONE COMPOUNDS AND ANALOGS THEREOF AS THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：咪唑并[4,5-B]吡啶-2-酮和氧杂唑[4,5-B]吡啶-2-酮化合物及其类似物作为治疗化合物
公开(公告)号：WO2006043090A1
公开(公告)日：2006-04-27
申请号：PCT/GB2005/004081
申请日：2005-10-21
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE) , ASTEX THERAPEUTICS LIMITED , NICULESCU-DUVAZ, Dan , SPRINGER, Caroline, Joy , GILL, Adrian, Liam , TAYLOR, Richard, David , MARAIS, Richard, Malcolm , DIJKSTRA, Harmen , GAULON, Catherine , MENARD, Delphine , ROMAN VELA, Esteban
发明人： NICULESCU-DUVAZ, Dan , SPRINGER, Caroline, Joy , GILL, Adrian, Liam , TAYLOR, Richard, David , MARAIS, Richard, Malcolm , DIJKSTRA, Harmen , GAULON, Catherine , MENARD, Delphine , ROMAN VELA, Esteban
IPC分类号： C07D471/04 , C07D498/04 , A61K31/4353 , A61P35/00
CPC分类号： C07D471/04
摘要： The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof, which, inter alia , inhibit RAF (e.g., B-RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formula (I): wherein: J is independently -O- or -NR N1 -; R N1 , if present, is independently -H or a substituent; R N2 is independently -H or a substituent; Y is independently -CH= or -N=; Q is independently -(CH 2 ) j -M-(CH 2 ) k - wherein: j is independently 0, 1 or 2; k is independently 0, 1, or 2; j+k is 0, 1, or 2; M is independently -O-, -S-, -NH-, -NMe-, or -CH 2 -; each of R P1 , R P2 , R P3 , and R P4 is independently -H or a substituent; and additionally R P1 and R P2 taken together may be -CH=CH-CH=CH-; L is independently: a linker group formed by a chain of 2, 3, or 4 linker moieties; each linker moiety is independently -CH 2 -,-NR N -, -C(=X)-, or -S(=O) 2 -; exactly one linker moiety is -NR N -, or: exactly two linker moieties are -NR N -; exactly one linker moiety is -C(=X)-, and no linker moiety is -S(=O) 2 -; or: exactly one linker moiety is -S(=O) 2 -, and no linker moiety is -C(=X)-; no two adjacent linker moieties are -NR N -; X is independently =O or =S; each R N is independently -H or a substituent; A is independently: C 6-14 carboaryl, C 5-14 heteroaryl, C 3-12 carbocyclic, C 3-12 heterocyclic; and is independently unsubstituted or substituted; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.
摘要翻译：本发明涉及某些咪唑并[4,5-b]吡啶-2-酮和恶唑并[4,5-b]吡啶-2-酮化合物及其类似物，其中i

2. 发明申请

WO2011092469A1 1-(5-TERT-BUTYL-2-PHENYL-2H-PYRAZOL-3-YL)-3-[2-FLUORO-4-(1-METHYL-2-OXO-2,3-DIHYDRO-1H-IMIDAZO[4,5-B]PYRIDIN-7-YLOXY)-PHENYL]-UREA AND RELATED COMPOUNDS AND THEIR USE IN THERAPY 审中-公开
标题翻译： 1-（5-叔丁基-2-苯基-2H-吡唑-3-基）-3- [2-氟-4-（1-甲基-2-氧代-2,3-二氢-1H-咪唑并[ 4,5-B]吡啶-7-YLOXY） - 苯基] - 及其相关化合物及其在治疗中的用途
公开(公告)号：WO2011092469A1
公开(公告)日：2011-08-04
申请号：PCT/GB2011/000106
申请日：2011-01-27
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE) , SPRINGER, Caroline , NICULESCU-DUVAZ, Ion , MARAIS, Richard , NICULESCU-DUVAZ, Dan , ZAMBON, Alfonso , MENARD, Delphine
发明人： SPRINGER, Caroline , NICULESCU-DUVAZ, Ion , MARAIS, Richard , NICULESCU-DUVAZ, Dan , ZAMBON, Alfonso , MENARD, Delphine
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： A61K31/437 , A61K31/4353 , C07D401/02 , C07D471/04
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain compounds of the following formula (I) (for convenience, collectively referred to herein as "IP compounds"), which, inter alia , are useful in the treatment of cancer, e.g., cancer characterised by (e.g., driven by) mutant RAS ("mutant RAS cancer"). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions in the treatment of cancer, e.g., mutant RAS cancer.
摘要翻译：本发明一般涉及治疗化合物领域，更具体地涉及下列通式（I）的某些化合物（为了方便起见，统称为“IP化合物”），其特别可用于治疗癌症，例如以突变RAS（“突变RAS癌症”）为特征的癌症。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在治疗癌症中的用途，例如突变RAS癌症。

3. 发明申请

WO2009130487A1 ARYL-QUINOLYL COMPOUNDS AND THEIR USE 审中-公开
标题翻译： ARYL-QUINOLYL化合物及其用途
公开(公告)号：WO2009130487A1
公开(公告)日：2009-10-29
申请号：PCT/GB2009/001077
申请日：2009-04-27
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE) , NICULESCU-DUVAZ, Ion , ZAMBON, Alfonso , NICULESCU-DUVAZ, Dan , WHITTAKER Steven , MARAIS, Richard , SPRINGER, Caroline Joy
发明人： NICULESCU-DUVAZ, Ion , ZAMBON, Alfonso , NICULESCU-DUVAZ, Dan , WHITTAKER Steven , MARAIS, Richard , SPRINGER, Caroline Joy
IPC分类号： C07D471/04 , A61K31/4985 , A61P35/00
CPC分类号： C07D471/04
摘要： The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain aryl-quinolyl compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.
摘要翻译：本发明一般涉及用于治疗增殖性疾病，癌症等的治疗化合物领域，更具体地涉及本文所述的某些芳基 - 喹啉基化合物，其特别地抑制RAF（例如，B-RAF）活性。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制RAF（例如BRAF）活性，抑制受体酪氨酸激酶（RTK）活性抑制细胞增殖，以及通过抑制RAF，RTK等改善的增殖性疾病如癌症（例如结肠直肠癌，黑素瘤）等疾病和病症的治疗。

4. 发明申请

WO2009077766A1 PYRIDO[2,3-B]PYRAZINE-8-SUBSTITUTED COMPOUNDS AND THEIR USE 审中-公开
标题翻译：吡咯并[2,3-B]吡嗪-8-取代的化合物及其用途
公开(公告)号：WO2009077766A1
公开(公告)日：2009-06-25
申请号：PCT/GB2008/004208
申请日：2008-12-19
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE) , SPRINGER, Caroline, Joy , NICULESCU-DUVAZ, Dan , NICULESCU-DUVAZ, Ion , MARAIS, Richard , SUIJKERBUIJK, Bartholomeus, Marinus, Josephus, Marie , ZAMBON, Alfonso , NOURRY, Arnaud , MENARD, Delphine
发明人： SPRINGER, Caroline, Joy , NICULESCU-DUVAZ, Dan , NICULESCU-DUVAZ, Ion , MARAIS, Richard , SUIJKERBUIJK, Bartholomeus, Marinus, Josephus, Marie , ZAMBON, Alfonso , NOURRY, Arnaud , MENARD, Delphine
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K31/4985
摘要： The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia , inhibit RAF (e.g., B RAF) activity. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc.
摘要翻译：本发明一般涉及用于治疗增殖性疾病，癌症等的治疗化合物领域，更具体地涉及本文所述的某些吡啶并[2,3-b]吡嗪-8-取代的化合物，其特别地，抑制RAF（例如，B RAF）活性。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制RAF（例如BRAF）活性，抑制受体酪氨酸激酶（RTK）活性抑制细胞增殖，以及通过抑制RAF，RTK等改善的增殖性疾病如癌症（例如结肠直肠癌，黑素瘤）等疾病和病症的治疗。

5. 发明申请

WO2015075483A1 1 -(5-TERT-BUTYL-2-ARYL-PYRAZOL-3-YL)-3-[2-FLUORO-4-[(3-OXO-4H-PYRIDO[2, 3-B]PYRAZIN-8-YL)OXY]PHENYL]UREA DERIVATIVES AS RAF INHIBITORS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译： 1-（5-叔丁基-2-亚氨基 - 吡咯-3-基）-3- [2-氟-4 - [（3-氧代-4H-吡啶并[2,3-b]吡嗪-8-基））OXY]苯胺]尿素衍生物作为RAF抑制剂治疗癌症
公开(公告)号：WO2015075483A1
公开(公告)日：2015-05-28
申请号：PCT/GB2014/053490
申请日：2014-11-25
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)
发明人： SPRINGER, Caroline Joy , MARAIS, Richard , GIROTTI, Romina , NICULESCU-DUVAZ, Dan , NICULESCU-DUVAZ, Ion , ZAMBON, Alfonso
IPC分类号： C07D471/04 , A61K31/4985 , A61P35/00
CPC分类号： C07D471/04
摘要： The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 1-(5-tert-butyl-2-aryl-pyrazol-3-yl)- 3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea compounds (referred herein as "TBAP compounds") that, inter alia, inhibit RAF (e.g., BRAF, CRAF, etc.). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., BRAF, CRAF, etc.); and to treat disorders including: proliferative disorders; cancer (including, e.g., malignant melanoma, colorectal carcinoma, pancreatic adenocarcinoma); inflammation; immunological disorders; viral infections; fibrotic disorders; disorders associated with a mutated form of RAF (e.g., BRAF, CRAF, etc.); disorders ameliorated by the inhibition of RAF (e.g., BRAF, CRAF, etc.); disorders ameliorated by the inhibition of mutant BRAF; disorders ameliorated by the inhibition of BRAF and CRAF; disorders associated with RAS mutations and/or MAPK pathway activation; disorders ameliorated by the inhibition of SRC, p38, FGFRA, VEGFR-2 (KDR), and/or LCK; etc.
摘要翻译：本发明一般涉及治疗化合物领域。更具体地说，本发明涉及某些1-（5-叔丁基-2-芳基 - 吡唑-3-基）-3- [2-氟-4 - [（3-氧代-4H-吡啶并[2,3 -b]吡嗪-8-基）氧基]苯基]脲化合物（在本文中称为“TBAP化合物”），特别是抑制RAF（例如BRAF，CRAF等）。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内都用于抑制RAF（例如BRAF，CRAF等）的用途; 并治疗疾病，包括：增殖性疾病; 癌症（包括例如恶性黑素瘤，结肠直肠癌，胰腺癌）; 炎; 免疫学障碍; 病毒感染; 纤维化疾病; 与突变形式的RAF（例如BRAF，CRAF等）相关的疾病; 通过抑制RAF（例如BRAF，CRAF等）改善的疾病; 通过突变BRAF的抑制改善的疾病; 通过抑制BRAF和CRAF而改善的疾病; 与RAS突变和/或MAPK通路活化相关的疾病; 通过抑制SRC，p38，FGFRA，VEGFR-2（KDR）和/或LCK而改善的疾病; 等等

6. 发明申请

WO2015075482A1 PROCESS FOR THE PREPARATION OF 8-(4-AMINOPHENOXY)-4H-PYRIDO[2,3-B]PYRAZIN-3-ONE DERIVATIVES 审中-公开
标题翻译：制备8-（4-氨基苯氧基）-4H-吡啶并[2,3-b]吡嗪-3-酮衍生物的方法
公开(公告)号：WO2015075482A1
公开(公告)日：2015-05-28
申请号：PCT/GB2014/053489
申请日：2014-11-25
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)
发明人： ZAMBON, Alfonso , NICULESCU-DUVAZ, Dan , CHUBB, Richard , SPRINGER, Caroline Joy
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The present invention pertains generally to the field of organic chemical synthesis, and in particular to certain methods for the synthesis of 8-(4-aminophenyoxy)- 4H-pyrido[2,3-b]pyrazin-3-one and related compounds (denoted herein as (3)) from 4-(4-aminophenyoxy)pyridine-2,3-diamine and related compounds (denoted herein as (1)), by reaction with glyoxylic acid (denoted herein as (2)). The compounds (3) are useful in the synthesis of known anti-cancer agents, such as 1-(5-tert-butyl-2-(4-methyl- phenyl)-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4H-pyrido[2,3-b]pyrazin-8-yl)oxy]phenyl]urea.
摘要翻译：本发明一般涉及有机化学合成领域，特别涉及合成8-（4-氨基苯氧基）-4H-吡啶并[2,3-b]吡嗪-3-酮和相关化合物的某些方法（由4-（4-氨基苯氧基）吡啶-2,3-二胺和相关化合物（在本文中表示为（1）），通过与乙醛酸（本文表示为（2））反应）表示为（3））。化合物（3）可用于合成已知的抗癌剂，例如1-（5-叔丁基-2-（4-甲基 - 苯基） - 吡唑-3-基）-3- [2- 氟-4 - [（3-氧代-4H-吡啶并[2,3-b]吡嗪-8-基）氧基]苯基]脲。

7. 发明申请

WO2007125330A1 IMIDAZO[4, 5-B]PYRIDIN-2-ONE AND OXAZOLO[4, 5-B]PYRIDIN-2-ONE COMPOUNDS AND ANALOGS THEREOF AS CANCER THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：咪唑并[4,5-B]吡啶-2-酮和氧杂唑[4,5-B]吡啶-2-酮化合物及其作为癌症治疗化合物的模拟物
公开(公告)号：WO2007125330A1
公开(公告)日：2007-11-08
申请号：PCT/GB2007/001534
申请日：2007-04-26
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE) , ASTEX THERAPEUTICS LIMITED , NICULESCU-DUVAZ, Dan , SPRINGER, Caroline, Joy , MARAIS, Richard, Malcolm , DIJKSTRA, Harmen , MENARD, Delphine , NICULESCU-DUVAZ, Ion , DAVIES, Lawrence , NOURRY, Arnaud
发明人： NICULESCU-DUVAZ, Dan , SPRINGER, Caroline, Joy , MARAIS, Richard, Malcolm , DIJKSTRA, Harmen , MENARD, Delphine , NICULESCU-DUVAZ, Ion , DAVIES, Lawrence , NOURRY, Arnaud
IPC分类号： C07D471/04 , A61K31/437 , A61K31/5377 , A61K31/44 , A61P35/00
CPC分类号： C07D471/04
摘要： The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5 b]pyridin-2-one compounds and analogs thereof, which, inter alia , inhibit RAF (e.g., B RAF) activity, inhibit cell proliferation, treat cancer, etc., and more particularly to compounds of the formulae: wherein: J is independently -O- or -NR N1 - ; R N1 , if present, is independently -H or a substituent; R N2 is independently -H or a substituent; Y is independently -CH= or -N=; Q is independently -(CH 2 ) j -M-(CH 2 ) k - wherein: j is independently 0, 1 or 2; k is independently 0, 1, or 2; j+k is 0, 1, or 2; M is independently O-, -S-, -NH-, -NMe-, or -CH 2 -; each of R P1 , R P2 , R P5 , and R P4 is independently -H or a substituent; and additionally R P1 and R P2 taken together may be CH=CH-CH=CH-; and additionally R P1 and R P5 taken together may be CH=CH-CH=CH-; L is independently: a linker group formed by a chain of 2, 3, or 4 linker moieties; each linker moiety is independently CH 2 -, -NR N -, -C(=X)-, or -S(=O) 2 -; either: exactly one linker moiety is -NR N -, or: exactly two linker moieties are -NR N -; either: exactly one linker moiety is -C(=X)-, and no linker moiety is -S(=O) 2 -, or: exactly one linker moiety is -S(=O) 2 -, and no linker moiety is -C(=X)-; no two adjacent linker moieties are -NR N -; X is independently =O or =S; each R N is independently -H or a substituent; A is independently: C 6-14 carboaryl, C 5-14 heteroaryl, C 3-12 carbocyclic, C 3-12 heterocyclic; and is independently unsubstituted or substituted; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit RAF (e.g., B-RAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and conditions that are ameliorated by the inhibition of RAF, RTK, etc., proliferative conditions such as cancer (e.g., colorectal cancer, melanoma), etc.
摘要翻译：本发明涉及特定的抑制RAF（例如B RAF）的咪唑并[4,5-b]吡啶-2-酮和恶唑并[4,5-b]吡啶-2-酮化合物及其类似物，活性，抑制细胞增殖，治疗癌症等，更具体地涉及下式的化合物：其中：J独立地为-O-或-NR N1。

8. 发明申请

WO2015036759A1 3-ARYL-5-SUBSTITUTED-ISOQUINOLIN-1-ONE COMPOUNDS AND THEIR THERAPEUTIC USE 审中-公开
标题翻译： 3-氨基-5-取代的异喹啉-1-酮化合物及其治疗用途
公开(公告)号：WO2015036759A1
公开(公告)日：2015-03-19
申请号：PCT/GB2014/052752
申请日：2014-09-11
申请人： INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)
发明人： ASHWORTH, Alan , LORD, Christopher, James , ELLIOTT, Richard, James, Rowland , NICULESCU-DUVAZ, Dan , PORTER, Roderick, Alan , AQIL, Rehan , BOFFEY, Raymond, John , BAYFORD, Melanie, Jayne , FIRTH-CLARK, Stuart , HOPKINS, Anna , JARVIS, Ashley, Nicholas , PERRIOR, Trevor, Robert , SKONE, Philip, Alan , KEY, Rebekah, Elisabeth
IPC分类号： C07D401/14 , C07D413/14 , C07D217/24 , C07D401/10 , C07D413/10 , C07D471/08 , A61K31/4725 , A61K31/472 , A61P35/00
CPC分类号： C07D217/24 , C07C53/06 , C07C53/18 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D413/10 , C07D413/12 , C07D413/14 , C07D471/08 , C07D487/08 , C07F7/186
摘要： The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted- 2/-/-isoquinolin-1-one compounds that, inter alia , inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc. Formula (I)
摘要翻译：本发明一般涉及治疗化合物领域。更具体地说，本发明涉及特别是抑制PARP（例如PARP1，TNKS1，TNKS2等）和/或Wnt的某些3-芳基-5-取代-2 - 异喹啉-1-酮化合物信号。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内都用于抑制PARP（例如PARP1，TNKS1，TNKS2等）的用途; 抑制Wnt信号; 治疗通过抑制PARP而改善的疾病（例如PARP1，TNKS1，TNKS2等）; 治疗通过抑制Wnt信号传导而改善的病症; 治疗癌症等增殖性状况。式（I）

9. 发明申请

WO2013132253A1 3-ARYL-5-SUBSTITUTED-ISOQUINOLIN-1-ONE COMPOUNDS AND THEIR THERAPEUTIC USE 审中-公开
标题翻译： 3-氨基-5-取代的异喹啉-1-酮化合物及其治疗用途
公开(公告)号：WO2013132253A1
公开(公告)日：2013-09-12
申请号：PCT/GB2013/050561
申请日：2013-03-07
申请人： INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL (THE)
发明人： ASHWORTH, Alan , LORD, Christopher James , ELLIOTT, Richard James Rowland , NICULESCU-DUVAZ, Dan , PORTER, Roderick , BOFFEY, Raymond John , BAYFORD, Melanie Jayne , FIRTH-CLARK, Stuart , JARVIS, Ashley Nicholas , PERRIOR, Trevor Robert , KEY, Rebekah Elisabeth
IPC分类号： A61P35/00 , A61K31/472 , C07D401/14 , C07D217/14 , C07D217/16 , C07D401/04 , C07D401/10 , C07D401/12 , C07D405/12 , C07D487/04 , C07D487/08 , C07D487/10 , A61K31/4725 , A61K31/496 , A61K31/506
CPC分类号： C07D217/24 , C07D217/14 , C07D217/16 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/12 , C07D487/04 , C07D487/08 , C07D487/10
摘要： The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain 3-aryl-5-substituted- 2H-isoquinolin-1-one compounds that, inter alia, inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.) and/or Wnt signalling. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to inhibit Wnt signalling; to treat disorders that are ameliorated by the inhibition of PARP (e.g., PARP1, TNKS1, TNKS2, etc.); to treat disorders that are ameliorated by the inhibition of Wnt signalling; to treat proliferative conditions such as cancer, etc.
摘要翻译：本发明一般涉及治疗化合物领域。更具体地，本发明涉及特别是抑制PARP（例如PARP1，TNKS1，TNKS2等）和/或Wnt信号传导的某些3-芳基-5-取代-2H-异喹啉-1-酮化合物。本发明还涉及包含这种化合物的药物组合物，以及这些化合物和组合物在体外和体内都用于抑制PARP（例如PARP1，TNKS1，TNKS2等）的用途; 抑制Wnt信号; 治疗通过抑制PARP而改善的疾病（例如PARP1，TNKS1，TNKS2等）; 治疗通过抑制Wnt信号传导而改善的病症; 治疗癌症等增殖性疾病

10. 发明申请

WO2022123039A1 ALDEHYDE DEHYDROGENASE INHIBITORS AND THEIR THERAPEUTIC USE 审中-公开
公开(公告)号：WO2022123039A1
公开(公告)日：2022-06-16
申请号：PCT/EP2021/085260
申请日：2021-12-10
申请人： CANCER RESEARCH TECHNOLOGY LIMITED [GB]/[GB]
发明人： KERSHAW, Christopher Stephen , ALJARAH, Mohammed , NICULESCU-DUVAZ, Dan , DODSWORTH, Mark Philip , BORDONI, Cinzia , SPRINGER, Caroline
IPC分类号： C07D401/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , A61K31/4725 , A61P35/00
摘要： The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain aldehyde dehydrogenase inhibitor compounds (also referred to herein as "ALDHI compounds"), that, inter alia, inhibit aldehyde dehydrogenase enzyme ALDH1A3. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit ALDH1A3 enzyme; to treat disorder (e.g., diseases) that are ameliorated by the inhibition of ALDH1A3 enzyme; to treat a proliferative disorder, cancer, obesity, diabetes, a cardiovascular disorder, etc.

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