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1. 发明授权

EP1521747B1 RECEPTOR-TYPE KINASE MODULATORS AND METHODS OF USE 有权转让
公开(公告)号：EP1521747B1
公开(公告)日：2018-09-05
申请号：EP03764599.1
申请日：2003-07-14
申请人： Symphony Evolution, Inc.
发明人： RICE, Kenneth, D. , ANAND, Neel, Kumar , BUSSENIUS, Joerg , COSTANZO, Simona , KENNEDY, Abigail, R. , KIM, Angie, I. , PETO, Csaba, J. , TSANG, Tsze, H. , BLAZEY, Charles, M.
IPC分类号： C07D239/93 , C07D239/94 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , A61K31/517 , A61P35/00
CPC分类号： C07D403/12 , A61K31/517 , A61K31/5377 , A61K31/5383 , A61K31/5513 , A61K31/553 , A61K31/7064 , C07D239/94 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D451/06 , C07D471/04 , C07D487/04 , C07D493/04
摘要： The present invention provides compounds which can modulate receptor kinase activity, particularly ephrin and EGFR, pharmaceutical compositions thereof and such compounds for use in treating cancer. The compounds comprise N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,5r,6aS)-2-methyloctahydrocyclopenta [c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine and N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,5s,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine.

2. 发明授权

EP2947072B1 1-(3-(6,7-DIMETHOXYQUINAZOLIN-4-YLOXY)PHENYL)-3-(5-(1,1,1-TRIFLUORO-2-METHYLPROPAN-2-YL)ISOXAZOL-3-YL)UREA AS RAF KINASE MODULATOR IN THE TREATMENT OF CANCER DISEASES 有权
标题翻译： 1-（3-（6,7-二甲氧基喹啉-4-基氧基）苯基）-3-（5-（1,1,1-三氟-2-甲基丙烷-2-基）异恶唑-3-基）脲，为RAF 激酶调制器用于治疗癌症
公开(公告)号：EP2947072B1
公开(公告)日：2016-11-09
申请号：EP15166141.0
申请日：2009-03-17
申请人： Ambit Biosciences Corporation
发明人： Abraham, Sunny , Bhagwat, Shripad, S. , Campbell, Brian, T. , Chao, Qi , Faraoni, Raffaella , Holladay, Mark, W. , Lai, Andiliy, G. , Rowbottom, Martin, W. , Setti, Eduardo , Sprankle, Kelly, G.
IPC分类号： C07D239/88 , C07D239/93 , A61K31/517 , A61P35/00
CPC分类号： C07D239/88 , A61K9/20 , A61K9/48 , A61K31/517 , A61K45/06 , C07D239/93 , C07D261/14 , C07D413/12
摘要： Compounds, compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. The compound is 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea, having the structure or a pharmaceutically acceptable salt, solvate, clathrate or hydrate thereof.

3. 发明公开

EP2947072A1 1-(3-(6,7-DIMETHOXYQUINAZOLIN-4-YLOXY)PHENYL)-3-(5-(1,1,1-TRIFLUORO-2-METHYLPROPAN-2-YL)ISOXAZOL-3-YL)UREA AS RAF KINASE MODULATOR IN THE TREATMENT OF CANCER DISEASES 有权
标题翻译： 1-（3-（6,7-二甲氧基环己烷-4-基）苯基）-3-（5-（1,1,1-三氟-2-甲基丙-2-炔基）异辛基-3-基）乙烯基）激光调制器ZUR BEHANDLUNG VON KREBSERKRANKUNGEN
公开(公告)号：EP2947072A1
公开(公告)日：2015-11-25
申请号：EP15166141.0
申请日：2009-03-17
申请人： Ambit Biosciences Corporation
发明人： Abraham, Sunny , Bhagwat, Shripad, S. , Campbell, Brian, T. , Chao, Qi , Faraoni, Raffaella , Holladay, Mark, W. , Lai, Andiliy, G. , Rowbottom, Martin, W. , Setti, Eduardo , Sprankle, Kelly, G.
IPC分类号： C07D239/88 , C07D239/93 , A61K31/517 , A61P35/00
CPC分类号： C07D239/88 , A61K9/20 , A61K9/48 , A61K31/517 , A61K45/06 , C07D239/93 , C07D261/14 , C07D413/12
摘要： Compounds, compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases.
The compound is 1-(3-(6,7-dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea, having the structure

or a pharmaceutically acceptable salt, solvate, clathrate or hydrate thereof.
摘要翻译：提供化合物，组合物和方法用于调节RAF激酶（包括BRAF激酶）的活性，并用于治疗，预防或改善由RAF激酶介导的疾病或病症的一种或多种症状。化合物是1-（3-（6,7-二甲氧基喹唑啉-4-基氧基）苯基）-3-（5-（1,1,1-三氟-2-甲基丙-2-基）异恶唑-3-基）尿素，具有结构或其药学上可接受的盐，溶剂合物，包合物或水合物。

4. 发明授权

EP2277867B1 Compounds, pharmaceutical compositions thereof and their use in treating cancer 无效
标题翻译：含有它们以及它们用于治疗癌症的化合物，药物组合物
公开(公告)号：EP2277867B1
公开(公告)日：2012-12-05
申请号：EP10183590.8
申请日：2003-07-14
申请人： Symphony Evolution, Inc.
发明人： Rice, Kenneth D. , Peto, Csabe J.
IPC分类号： C07D239/93 , C07D239/94 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , A61K31/517 , A61P35/00
CPC分类号： C07D403/12 , A61K31/517 , A61K31/5377 , A61K31/5383 , A61K31/5513 , A61K31/553 , A61K31/7064 , C07D239/94 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D451/06 , C07D471/04 , C07D487/04 , C07D493/04
摘要： The present invention provides compounds which can modulate receptor kinase activity, particularly ephrin and EGFR, pharmaceutical compositions thereof and such compounds for use in treating cancer. The compounds comprise N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,5r,6aS)-2-methyloctahydrocyclopenta [c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine and N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,5s,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine.

5. 发明公开

EP2277867A2 Compounds, pharmaceutical compositions thereof and their use in treating cancer 无效
标题翻译：含有它们以及它们用于治疗癌症的化合物，药物组合物
公开(公告)号：EP2277867A2
公开(公告)日：2011-01-26
申请号：EP10183590.8
申请日：2003-07-14
申请人： Symphony Evolution, Inc.
发明人： Rice, Kenneth D. , Peto, Csabe J.
IPC分类号： C07D239/93 , C07D239/94 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , A61K31/517 , A61P35/00
CPC分类号： C07D403/12 , A61K31/517 , A61K31/5377 , A61K31/5383 , A61K31/5513 , A61K31/553 , A61K31/7064 , C07D239/94 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D451/06 , C07D471/04 , C07D487/04 , C07D493/04
摘要： The present invention provides compounds which can modulate receptor kinase activity, particularly ephrin and EGFR, pharmaceutical compositions thereof and such compounds for use in treating cancer. The compounds comprise N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,5r,6aS)-2-methyloctahydrocyclopenta [c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine and N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,5s,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine.
摘要翻译：本发明提供了用于治疗癌症中的用途，其可调控受体激酶活性，特别是肝配蛋白和EGFR的化合物，其药物组合物以及这些化合物。化合物包含N-（3,4-二氯-2-氟苯基）-7 - （{[（3AR，5R，6AS）-2-甲基八氢环戊烷并[c]吡咯-5-基]甲基}氧基）-6-（甲氧基）喹唑啉-4-胺和N-（3,4-二氯-2-氟苯基）-7 - （{[（3AR，5S，6AS）-2-甲基八氢环戊烷并[c]吡咯-5-基]甲基}氧基基）-6-（甲氧基）喹唑啉-4-胺。

6. 发明公开

EP1521747A2 RECEPTOR-TYPE KINASE MODULATORS AND METHODS OF USE 有权转让
标题翻译：型受体激酶调制器和使用方法
公开(公告)号：EP1521747A2
公开(公告)日：2005-04-13
申请号：EP03764599.1
申请日：2003-07-14
申请人： Exelixis, Inc.
发明人： RICE, Kenneth, D. , ANAND, Neel, Kumar , BUSSENIUS, Joerg , COSTANZO, Simona , KENNEDY, Abigail, R. , KIM, Angie, I. , PETO, Csaba, J. , TSANG, Tsze, H. , BLAZEY, Charles, M.
IPC分类号： C07D239/93 , C07D239/94 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , A61K31/517 , A61P35/00
CPC分类号： C07D403/12 , A61K31/517 , A61K31/5377 , A61K31/5383 , A61K31/5513 , A61K31/553 , A61K31/7064 , C07D239/94 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D451/06 , C07D471/04 , C07D487/04 , C07D493/04
摘要： The present invention provides compounds which can modulate receptor kinase activity, particularly ephrin and EGFR, pharmaceutical compositions thereof and such compounds for use in treating cancer. The compounds comprise N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,5r,6aS)-2-methyloctahydrocyclopenta [c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine and N-(3,4-dichloro-2-fluorophenyl)-7-({[(3aR,5s,6aS)-2-methyloctahydrocyclopenta[c]pyrrol-5-yl]methyl}oxy)-6-(methyloxy)quinazolin-4-amine.

7. 发明授权

EP0748219B1 COMPOUNDS FOR THE TREATMENT OF DISORDERS RELATED TO VASCULOGENESIS AND/OR ANGIOGENESIS 失效
标题翻译：化合物与血管生成和/或血管相关疾病的治疗。
公开(公告)号：EP0748219B1
公开(公告)日：2005-04-06
申请号：EP95910239.3
申请日：1995-02-09
申请人： Sugen, Inc. , YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM
发明人： GAZIT, Aviv , LEVITZKI, Alexander , APP, Harald , TANG, Cho, Peng , MCMAHON, Gerald, M.
IPC分类号： A61K31/24 , A61K31/42 , A61K31/275 , A61K31/415 , A61K31/495 , C07C211/45 , C07C255/01 , C07D209/18 , C07D231/38 , C07D241/36 , C07C255/41 , C07D239/93
CPC分类号： C07D487/04 , A61K31/235 , A61K31/275 , A61K31/277 , A61K31/38 , A61K31/40 , A61K31/415 , A61K31/42 , A61K31/495 , A61K31/502 , A61K31/505 , A61K31/517 , A61K31/535 , A61K38/00 , C07C229/60 , C07C255/36 , C07C255/40 , C07C255/41 , C07C255/66 , C07C317/46 , C07C327/44 , C07D209/18 , C07D239/93 , C07D239/94 , C07D241/42 , C07D241/44 , C07K14/71 , C07K16/2863 , C07K2319/32 , G01N33/5008 , G01N33/5011 , G01N33/502 , G01N33/5064 , G01N33/5091 , G01N33/6893 , G01N2333/71 , G01N2500/04
摘要： The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLK-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described. The invention also relates to the use of the disclosed compounds in the treatment of disorders, including cancer, diabetes, hemangioma and Kaposi's sarcoma, which are related to vasculogenesis and angiogenesis.

8. 发明公开

EP0860433A4 QUINOLINE DERIVATIVES AND QUINAZOLINE DERIVATIVES INHIBITING AUTOPHOSPHORYLATION OF GROWTH FACTOR RECEPTOR ORIGINATING IN PLATELET AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 失效
标题翻译：喹啉衍生物含有和喹唑啉衍生物的WHAT血小板衍生生长因子受体INHIBIREN的自磷酸化和YOU药物组合物
公开(公告)号：EP0860433A4
公开(公告)日：1999-01-07
申请号：EP96935541
申请日：1996-11-05
申请人： KIRIN BREWERY
发明人： KUBO KAZUO , OHYAMA SHINICHI , SHIMIZU TOSHIYUKI , NISHITOBA TSUYOSHI , KATO SHINICHIRO , MUROOKA HIDEKO , KOBAYASHI YOSHIKO
IPC分类号： C07D215/20 , C07D215/22 , C07D215/233 , C07D215/36 , C07D239/88 , C07D401/12 , C07D405/10 , C07D405/12 , C07D409/12 , C07D491/056 , A61K31/47 , C07D239/74 , C07D239/93
CPC分类号： C07D215/233 , C07D215/20 , C07D215/36 , C07D239/88 , C07D401/12 , C07D405/10 , C07D405/12 , C07D409/12
摘要： Novel quinoline derivatives and quinazoline derivatives represented by general formula (I) which have an inhibitory effect on the autophosphorylation of growth factor receptors originating in platelets and pharmaceutically acceptable salts thereof; pharmaceutical compositions containing these compounds; and a method for treating diseases relating to the abnormal proliferation of cells such as the proliferation of tumors, wherein R1 and R2 represent each H or C1-4 alkyl, or R1 and R2 together form C1-3 alkylene; X represents O, S or CH2; W represents CH or N; and Q represents substituted aryl or substituted heteroaryl.

10. 发明公开

EP0326328A3 Quinoline, quinazoline, and cinnoline derivatives 失效
标题翻译：喹啉，喹喔啉和辛醇衍生物
公开(公告)号：EP0326328A3
公开(公告)日：1990-08-22
申请号：EP89300656.9
申请日：1989-01-25
申请人： DowElanco
发明人： Coghlan, Michael Joseph , Dreikorn, Barry Allen , Suhr, Robert George , Jourdan, Glen Phil
IPC分类号： C07D215/22 , C07D215/42 , C07D215/04 , C07D239/94 , C07D215/18 , C07D409/06 , C07D405/06 , C07D239/88 , C07D239/74 , C07D239/93 , C07D215/36
CPC分类号： C07D215/04 , C07D215/18 , C07D215/233 , C07D215/36 , C07D215/42 , C07D215/60 , C07D239/88 , C07D239/93 , C07D239/94 , C07D405/12 , C07D409/12
摘要： Compounds of formula (1)
wherein
R¹ to R⁴ are independently:
H, halo, I, (C₁-C₄) alkyl, branched (C₃-C₄) alkyl, halo (C₁-C₄) alkyl, (C₁-C₄) alkoxy, halo (C₁-C₄) alkoxy, NO₂, or NH₂, at least two of R¹ to R⁴ being H,
one of X and Y is N and the other is CR⁵, or both X and Y are CR⁵,
R⁵ is H, CH₃, or Cl;
Z is O, NR⁶, S, SO, SO₂, or CR⁷R⁸;
R⁶ is H, (C₁-C₄) alkyl, or (C₂-C₄) acyl;
R⁷ and R⁸ are independently H, (C₁-C₄) alkyl, branched (C₃-C₄) alkyl, or (C₁-C₄) acyl, or R⁷ and R⁸ combine to form a saturated or unsaturated carbocyclic ring containing three to seven carbon atoms or one of R⁷ and R⁸ can combine with one of R⁹ and R¹⁰ to form a double bond;
R⁹ and R¹⁰ are independently H, (C₁-C₃) alkyl, phenyl, substituted phenyl, (C₃-C₈) cycloalkyl, hydroxy, halo, I, or acetyl, or R⁹ and R¹⁰ combine to form a saturated or unsaturated carbocyclic ring containing three to seven carbon atoms; and Ar is (C₃-C₈) cycloalkyl,
substituted (C₃-C₈) cycloalkyl,
(C₃-C₈) cycloalkenyl,
naphthyl,
dihydronaphthyl,
tetrahydronaphthyl,
decahydronaphthyl,
1,3-benzodioxolyl,
fluorenyl,
pyridyl,
2,3-dihydro-1,4-benzodioxin-2-yl,
furyl optionally substituted with halo, I, CF₃, CN, NO₂, (C₁-C₄) alkyl, branched (C₃-C₄) alkyl, phenyl, or (C₁-C₄) alkoxy,
thienyl optionally substituted with halo, I, CF₃, CN, NO₂, (C₁-C₄) alkyl, branched (C₃-C₄) alkyl, phenyl, or (C₁-C₄) alkoxy,
a group of the formula (2) or (2a)
wherein R¹¹ is H, halo, I, CF₃, CN, NO₂, (C₁-C₄) alkyl, branched (C₃-C₄) alkyl, phenyl, or (C₁-C₄) alkoxy, F is N or CH and G is O, NR²⁰, or CH₂, provided that F is N or G is NR²⁰, where R²⁰ is H, (C₁-C₄) alkyl, (C₁-C₄) acyl, phenylsulfonyl, or substituted phenylsulfonyl; a group of the formula (3)
wherein
R¹² to R¹⁶ are independently H, halo, I, (C₁-C₁₀) alkyl, branched (C₃-C₆) alkyl, halo (C₁-C₄) alkyl, (C₁-C₄) alkoxy, halo (C₁-C₄) alkoxy, phenoxy, substituted phenoxy, phenyl, substituted phenyl, phenylthio, or substituted phenylthio, NO₂, NH₂, acetoxy, OH, CN, or SiR¹⁷R¹⁸R¹⁹, or OSiR¹⁷R¹⁸R¹⁹, where R¹⁷, R¹⁸, and R¹⁹ are independently C₁-C₄ alkyl, C₁-C₄ branched alkyl, phenyl, or substituted phenyl, provided that unless each of R¹² to R¹⁶ is F, CH₃, or H, then at least two of R¹² to R¹⁶ are H;
or an acid addition salt of a compound of formula (1), or an N-oxide of a compound of formula (1) where Y is CR⁵;
provided that
if R¹ to R⁴ are all H, X is CR⁵, Y is N, and Z is NR⁶, then Ar is naphthyl or a group of formula (3) wherein one of R¹² to R¹⁶ is phenyl, substituted phenyl, phenoxy, substituted phenoxy, phenylthio, or substituted phenylthio, halo (C₁-C₄) alkyl, or halo (C₁-C₄) alkoxy, are plant fungicides, insecticides, and miticides.

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