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1. 发明专利

BR112014004504B1 Inibidor de c-kit cinase, seu uso, e composição farmacêutica 未知
公开(公告)号：BR112014004504B1
公开(公告)日：2022-03-22
申请号：BR112014004504
申请日：2012-08-28
申请人： IRM LLC , NOVARTIS AG , NOVARTIS INT PHARMACEUTICAL LTD
发明人： NGUYEN BAO , HANK MICHAEL JAMES PETRASSI , LOREN JON , NABAKKA JULIET , MOLTENI VALENTINA , YEH VINCE , LIU XIAODONG , LI XIAOLIN
IPC分类号： C07D471/04 , A61K31/437 , A61P3/00 , A61P11/00 , A61P17/00 , A61P29/00
摘要： composto como inibidor de c-kit cinase, seu uso, composição farmacêutica, e medicamento para o tratamento de uma doença mediada por uma cinase. a presente invenção refere-se a compostos de fórmula (i) e (ii) e a composições farmacêuticas dos mesmos, que são úteis como inibidores de proteína cinase, bem como métodos para uso de tais compostos para tratar, melhorar ou prevenir uma condição associada com atividade cinase anormal ou desregulada. em algumas modalidades, a invenção fornece métodos para uso de compostos para tratar, melhorar ou impeder doenças ou distúrbios que envolvem a ativação anormal de c-kit ou c-kit e pdgfr (pdgfr(alfa), pdgfr(beta)) cinases.

2. 发明申请

WO2007038669A3 DIARYLAMINE-CONTAINING COMPOUNDS AND COMPOSITIONS, AND THEIR USE AS MODULATORS OF C-KIT RECEPTORS 审中-公开
标题翻译：含二氨基苯胺的化合物和组合物及其作为C-kit接受体的调节剂
公开(公告)号：WO2007038669A3
公开(公告)日：2007-11-22
申请号：PCT/US2006037820
申请日：2006-09-26
申请人： IRM LLC , NOVARTIS AG , MOLTENI VALENTINA , LI XIAOLIN , CHIANELLI DONATELLA , LOREN JON , LIU YI , KARANEWSKY DONALD S , FURET PASCAL , GUAGNANO VITO , YOU SHULI , NABAKKA JULIET , LIU XIAODONG , PAN SHIFENG
发明人： MOLTENI VALENTINA , LI XIAOLIN , CHIANELLI DONATELLA , LOREN JON , LIU YI , KARANEWSKY DONALD S , FURET PASCAL , GUAGNANO VITO , YOU SHULI , NABAKKA JULIET , LIU XIAODONG , PAN SHIFENG
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D403/04 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/10
摘要： Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.
摘要翻译：本文描述的是包括二芳基胺结构特征的化合物。本文还描述了制备这种化合物的方法，使用这些化合物调节c-kit受体的活性的方法，以及包含这些化合物的药物组合物和药物。本文还描述了使用这些化合物，药物组合物和药物来治疗和/或预防和/或抑制和/或改善与c-kit受体活性相关的病理学和/或症状学疾病或病症的方法。

3. 发明申请

WO2007038669A9 DIARYLAMINE-CONTAINING COMPOUNDS AND COMPOSITIONS, AND THEIR USE AS MODULATORS OF C-KIT RECEPTORS 审中-公开
标题翻译：含二氨基苯胺的化合物和组合物及其作为C-kit接受体的调节剂
公开(公告)号：WO2007038669A9
公开(公告)日：2008-05-29
申请号：PCT/US2006037820
申请日：2006-09-26
申请人： IRM LLC , NOVARTIS AG , MOLTENI VALENTINA , LI XIAOLIN , CHIANELLI DONATELLA , LOREN JON , LIU YI , KARANEWSKY DONALD S , FURET PASCAL , GUAGNANO VITO , YOU SHULI , NABAKKA JULIET , LIU XIAODONG , PAN SHIFENG
发明人： MOLTENI VALENTINA , LI XIAOLIN , CHIANELLI DONATELLA , LOREN JON , LIU YI , KARANEWSKY DONALD S , FURET PASCAL , GUAGNANO VITO , YOU SHULI , NABAKKA JULIET , LIU XIAODONG , PAN SHIFENG
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D403/04 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/10
摘要： Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.
摘要翻译：本文描述的是包括二芳基胺结构特征的化合物。本文还描述了制备这些化合物的方法，使用这些化合物调节c-kit受体的活性的方法，以及包含这些化合物的药物组合物和药物。本文还描述了使用这些化合物，药物组合物和药物来治疗和/或预防和/或抑制和/或改善与c-kit受体活性相关的病理学和/或症状学疾病或病症的方法。

4. 发明专利

JP2014177486A Compounds including 5-(4-(halo-alkoxy)phenyl)pyrimidine-2-amine and composition as kinase inhibitor 审中-公开
标题翻译：包括5-（4-（HALO-烷氧基）苯基）吡嗪-2-胺和作为激酶抑制剂的组合物的化合物
公开(公告)号：JP2014177486A
公开(公告)日：2014-09-25
申请号：JP2014110269
申请日：2014-05-28
申请人： Irm Llc , アイアールエム・リミテッド・ライアビリティ・カンパニーIrm,Llc
发明人： VALENTINA MOLTENI , LI XIAOLIN , LIU XIAODONG , DONATELLA CHIANELLI , JULIET NABAKKA , JON LOREN , YOU SHULI
IPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P11/00 , A61P13/12 , A61P19/02 , A61P21/02 , A61P27/02 , A61P29/00 , A61P35/00 , A61P35/02 , A61P37/02 , A61P37/08 , A61P43/00 , C07D401/12 , C07D403/12
CPC分类号： C07D239/42 , C07D401/12 , C07D403/12 , C07D413/12
摘要： PROBLEM TO BE SOLVED: To provide compounds useful as a protein kinase inhibitor and their pharmaceutical compositions.SOLUTION: Compounds of formula (1), their medically permissible salts and pharmaceutical compositions containing them are provided. In the formula, Ris a haloalkyl group having 1-6 F; Ris alkyl optionally substituted with halo, amino or hydroxyl, etc.; and any adjacent Rgroups may form a substituted 5- to 8-membered carbocyclic, heterocyclic, aryl or heteroaryl ring.
摘要翻译：要解决的问题：提供可用作蛋白激酶抑制剂的化合物及其药物组合物。解决方案：提供式（1）化合物，其医药上允许的盐和含有它们的药物组合物。在该式中，R 1为1-6 F的卤代烷基; 任选被卤素，氨基或羟基取代的Ris烷基等; 并且任何相邻的R基团可以形成取代的5-至8-元碳环，杂环，芳基或杂芳基环。

5. 发明公开

EP1928236A4 DIARYLAMINE-CONTAINING COMPOUNDS AND COMPOSITIONS, AND THEIR USE AS MODULATORS OF C-KIT RECEPTORS 有权
标题翻译： DIARYLAMINHALTIGE化合物和组合物及其作为C-KIT受体调节剂
公开(公告)号：EP1928236A4
公开(公告)日：2010-07-07
申请号：EP06815653
申请日：2006-09-26
申请人： IRM LLC , NOVARTIS AG
发明人： MOLTENI VALENTINA , LI XIAOLIN , CHIANELLI DONATELLA , LOREN JON , LIU YI , KARANEWSKY DONALD S , FURET PASCAL , GUAGNANO VITO , YOU SHULI , NABAKKA JULIET , LIU XIAODONG , PAN SHIFENG
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D403/04 , C07D239/42 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D413/12 , C07D417/12 , C07D471/04 , C07D491/10

6. 发明专利

AU2007317349A1 Compounds and compositions as protein kinase inhibitors 未知
公开(公告)号：AU2007317349A1
公开(公告)日：2008-05-15
申请号：AU2007317349
申请日：2007-11-02
申请人： NOVARTIS AG , IRM LLC
发明人： PEREZ LAWRENCE B , NABAKKA JULIET , MANLEY PAUL W , WRONA WOJCIECH , LI XIAOLIN , LIU XIAODONG , BREITENSTEIN WERNER , BROOKS CLINTON , MOLTENI VALENTINA , REVESZ LASZLO , CHIANELLI DONATELLA , LOREN JON
IPC分类号： C07D401/14 , A61K31/506 , A61P25/00 , A61P33/06 , A61P35/00 , C07D403/12 , C07D405/14 , C07D407/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to beat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFRα and PDGFR&bgr; kinases. Formula (I).

7. 发明专利

CA2686382C PHENYLAMINOPYRIMIDINE DERIVATIVES AND COMPOSITIONS THEREOF AS C-KIT AND PDGFR KINASE INHIBITORS 未知
公开(公告)号：CA2686382C
公开(公告)日：2013-09-17
申请号：CA2686382
申请日：2008-05-02
申请人： IRM LLC , NOVARTIS AG
发明人： LI XIAOLIN , LIU XIAODONG , MOLTENI VALENTINA , CHIANELLI DONATELLA , LOREN JON , NABAKKA JULIET , RAMSEY TIMOTHY , BREITENSTEIN WERNER
IPC分类号： C07D401/04 , A61K31/506 , A61P35/00 , A61P37/00 , C07D417/14
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFR.alpha. and PDGFR.beta. kinases. Compounds of this invention have the following Formula in which L is -NHC(O)-, -NHC(O)NH- or -C(O)NH-. (see above formula)

8. 发明专利

AU2008247442B2 Compounds and compositions as c-kit and PDGFR kinase inhibitors 未知
公开(公告)号：AU2008247442B2
公开(公告)日：2013-01-10
申请号：AU2008247442
申请日：2008-05-02
申请人： IRM LLC , NOVARTIS AG
发明人： MOLTENI VALENTINA , RAMSEY TIMOTHY , LOREN JON , LIU XIAODONG , BREITENSTEIN WERNER , NABAKKA JULIET , CHIANELLI DONATELLA , LI XIAOLIN
IPC分类号： C07D401/04 , A61K31/506 , A61P35/00 , A61P37/00 , C07D417/14
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of c-kit, PDGFR and PDGFR kinases.

9. 发明专利

ES2378153T3 Conpuestos y composiciones que contienen diarilamina, y su uso como moduladores de receptores c-kit 未知
公开(公告)号：ES2378153T3
公开(公告)日：2012-04-09
申请号：ES06815653
申请日：2006-09-26
申请人： IRM LLC , NOVARTIS AG
发明人： MOLTENI VALENTINA , LI XIAOLIN , CHIANELLI DONATELLA , LOREN JON , LIU YI , KARANEWSKY DONALD , FURET PASCAL , GUAGNANO VITO , YOU SHULI , NABAKKA JULIET , LIU XIAODONG , PAN SHIFENG
IPC分类号： A01N43/42 , A61K31/44
摘要： Caja de reloj (1) con una parte de la cubierta (7) que contiene una tapa de la caja (2), con una parte de la base (8) que contiene una base de la caja (3) y una pared circunferencial de la caja (4) entre la tapa de la caja (2) y la base de la caja (3), estando rodeada en al menos parte de su circunferencia, por al menos un elemento decorativo (11), caracterizada porque la parte de la cubierta (7) está unida a la parte de la base (8) por al menos dos puentes de conexión (12) distribuidos sobre todo el perímetro del elemento decorativo (11). **Fórmula** en las que, cuando Ar es un heterociclo aromático de cinco miembros opcionalmente sustituido o un carbociclo aromático de cinco miembros opcionalmente sustituido, Ar está opcionalmente sustituido con uno o más grupos R2 y/o uno o más sustituyentes opcionales; cuando Ar es un heterociclo aromático de seis miembros opcionalmente sustituido, Ar está opcionalmente sustituido con M, uno o más grupos R2 y/o uno o más sustituyentes opcionales; cuando Ar es un fenilo sustituido, opcionalmente sustituido adicionalmente, Ar está sustituido con M y opcionalmente sustituido con uno o más grupos R2 y/o uno o más sustituyentes opcionales; en el que M se selecciona entre el grupo que consiste en H, OH, SH, NO2, CN, NR"2 y un resto opcionalmente sustituido seleccionado entre -L7-alquilo, -L7-alquenilo, -L7-alquinilo, -L7-cicloalquilo, -L7-cicloalquenilo, -L7- cicloalquinilo, -L7-heteroalquilo, -L7-heteroalquenilo, -L7-heteroalquinilo, -L7-haloalquilo, -L7-haloalquenilo, -L15 7- haloalquinilo, -L7-arilo, -L7-heterocicloalquenilo, -L7-heterocicloalquinilo, -L7-heterocicloalquilo y -L7-heteroarilo; en el que L7 se selecciona entre un enlace, -O-, -NH-, -S-, -C(O)-, -C(S)-, -C(O)O-, -C(O)NH-, -S(O)-, -S(O)2-, -OC(O)-, -C(O)NR"(CR"2)1-6C(O)O-, -CR"2NR"CR"2C(O)O-, -C(O)NR"Y1C(O)O-, -C(O)NR"NR"C(O)O-, - S(O)NH-, -C(O)NR"CR"2C(O)W-, -CR"2NR"WO-, -CR"2NR"Y1C(O)O- y -C(O)NR"O-; W es alquileno C1-6; Y1 20 es arileno opcionalmente sustituido o heteroarileno opcionalmente sustituido; en el que dichos sustituyentes opcionales se seleccionan entre halógeno, OH, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, haloalquilo C1-6,haloalquenilo C2-6, haloalquinilo C2-6 y haloalcoxi C1-6; con la condición de que M no sea H en la Fórmula (2); cada R" es independientemente H, OH, halógeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilo C1-6 sustituido, alquenilo C2-6 sustituido, alquinilo C2-6 sustituido, alcoxi C1-6, haloalquilo C1-6, haloalquenilo C2-625 , haloalquinilo C2-6, haloalcoxi C1-6, arilo, haloarilo o heteroarilo; R2 se selecciona independientemente entre el grupo que consiste en H, OH, halógeno y un resto opcionalmente sustituido seleccionado entre -L2-alquilo, -L2-alquenilo, -L2-alquinilo, -L2-cicloalquilo, -L2- cicloalquenilo, -L2-cicloalquinilo, -L2-heteroalquilo, -L2-heteroalquenilo, -L2-heteroalquinilo, -L2-haloalquilo, -L2- haloalquenilo, -L2-haloalquinilo, -L2-arilo, -L2-heterocicloalquilo, -L2-heterocicloalquenilo, -L2- heterocicloalquinilo y -L2-heteroarilo; en el que L2 se selecciona entre un enlace, -O-, -NH-, -S-, -C(O)-, -C(S)-, -C(O)O-, -C(O)NH-, -S(O)-, -S(O)2-, -C(O)NR"(CR"2)1-6C(O)O-, -OC(O)-, -CR"2NR"CR"2C(O)O-, - C(O)NR"NR"C(O)O- y -S(O)NH-; en el que dichos sustituyentes opcionales se seleccionan entre halógeno, OH, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, haloalquilo C1-6, haloalquenilo C2-6, haloalquinilo C2-6 y haloalcoxi C1-6 ; o dos grupos R2 adyacentes cualesquiera pueden formar juntos un anillo arilo, cicloalquinilo, cicloalquenilo, cicloalquilo o heterocíclico de 5 a 8 miembros opcionalmente sustituido; o Ar se selecciona entre el grupo que consiste en y en el que dichos sustituyentes opcionales se seleccionan entre alquenilo sin sustituir, alquilo, alcoxi, alquilamina, alquiltio, alquinilo, amida, amino, arilo, ariloxi, ariltio, carbocíclico, ciano, cicloalquilo, halógeno, heteroalquilo, heteroalquenilo, heteroalquinilo, heteroarilo, heterocíclico, hidroxi, isocianato, isotiocianato, mercapto, nitro, O- carbamilo, N-carbamilo, O-tiocarbamilo, N-tiocarbamilo, C-amido, S-sulfonamido, C-carboxi, perhaloalquilo, perfluoroalquilo, tiocianato y trihalometanosulfonilo; y en el que el término "aromático" o "arilo" se refiere a una estructura de anillo cerrada que tiene al menos un anillo que tiene un sistema de electrones pi conjugados; o una sal farmacéuticamente aceptable, N-óxido farmacéuticamente aceptable o solvato farmacéuticamente aceptable de los mismos.

10. 发明专利

AT534293T 未知
公开(公告)号：AT534293T
公开(公告)日：2011-12-15
申请号：AT06815653
申请日：2006-09-26
申请人： IRM LLC , NOVARTIS AG
发明人： MOLTENI VALENTINA , LI XIAOLIN , CHIANELLI DONATELLA , LOREN JON , LIU YI , KARANEWSKY DONALD , FURET PASCAL , GUAGNANO VITO , YOU SHULI , NABAKKA JULIET , LIU XIAODONG , PAN SHIFENG
IPC分类号： A01N43/42 , A61K31/44
摘要： Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.

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