AR052315A1 - Derivados de quinazolina utiles para el tratamiento de cancer - Google Patents
Derivados de quinazolina utiles para el tratamiento de cancerInfo
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- AR052315A1 AR052315A1 ARP050104278A ARP050104278A AR052315A1 AR 052315 A1 AR052315 A1 AR 052315A1 AR P050104278 A ARP050104278 A AR P050104278A AR P050104278 A ARP050104278 A AR P050104278A AR 052315 A1 AR052315 A1 AR 052315A1
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- alkyl
- ureido
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- amino
- alkanoylamino
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- A—HUMAN NECESSITIES
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
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- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- Chemical & Material Sciences (AREA)
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Procesos para su preparacion, composiciones farmacéuticas que los contienen y su uso en la elaboracion de un medicamento para usar en el tratamiento de los trastornos de proliferacion celular o en el tratamiento de estados de enfermedad asociados con la angiogénesis y/o la permeabilidad vascular. Reivindicacion 1: Un derivado de quinazolina caracterizado porque responde a la formula (1) en donde p es 0, 1, 2 o 3; cada grupo R1, que pueden ser iguales o diferentes, se selecciona entre halogeno, trifluorometilo, ciano, hidroxi, mercapto, amino, (C1-8) alquilo, (C2-8) alquenilo, (C2-8) alquinilo, (C1-6) alcoxi, (C2-6) alqueniloxi, (C2-6) alquiniloxi, (C1-6) alquiltio, (C1-6) alquilsulfinilo, (C1-6) alquilsulfonilo, (C1-6) alquilamino y di-[(C1-6)alquil]amino, o ente un grupo de la formula Q1-X2- en donde X2 es un enlace directo o se selecciona entre O, S, SO, SO, N(R8), CO, CON(R8), N(R8)CO, OC(R8)2 y N(R8)C(R8)2, en donde cada R8 es H o (C1-8) alquilo, y Q1 es arilo, aril-(C1-6) alquilo, (C3-8) cicloalquilo, (C3-8) cicloalquil-(C1-6) alquilo, (C3-8) cicloalquenilo, (C3-8) cicloalquenil-(C1-6) alquilo, heteroarilo, heteroaril-(C1-6) alquilo, heterociclilo o heterociclil-(C1-6) alquilo, y en done cualquier grupo arilo, (C3-8) cicloalquilo, (C3-8) cicloalquenilo, heteroarilo o heterociclilo dentro de un sustituyente R1 tiene opcionalmente 1, 2 o 3 sustituyentes, que pueden ser iguales o diferentes, seleccionados entre halogeno, trifluorometilo, ciano, nitro, hidroxi, amino, carboxi, carbamoilo, ureido, (C1-8) alquilo, (C2-8) alquenilo, (C2-8) alquinilo, (C1-6) alcoxi, (C2-6) alqueniloxi, (C2-6) alquiniloxi, (C1-6) alquiltio, (C1-6) alquilsulfinilo, (C1-6) alquilsulfonilo, (C1-6) alquilamino, di- [(C1-6)alquilamino, N-(C1-6)alquilcarbamoilo, N,N-di-[(C1-6)alquil]carbamoilo, (C2-6)alcanoilamino, N-(C1-6) alquil-(C2-6)alcanoilamino, N-(C1-6)alquilureido, N'-(C1-6)alquilureido, N',N'-di-[(C1-6)alquil]ureido, N,N'-di[(C1-6)alquil]ureido, N,N',N'- tri-[C1-6)alquil]ureido, N-(C1-6)alquilsulfamoilo, N,N-di-[(C1-6)alquil]sulfamoilo, (C1-6)alcansulfonilamino y N-(C1-6)alquilo-(C1-6) alcansulfonilamino, o entre un grupo de la formula: -X3-R9 en donde X3 es un enlace directo o se selecciona entre O y N(R10), en donde R10 es H o (C1-8) alquilo, y R9 es halogeno-(C1-6)alquilo, hidroxi-(C1-6)alquilo, mercapto-(C1-6)alquilo, (C1-6)alcoxi-(C1-6)alquilo, (C1-6)alquiltio-(C1-6)alquilo, (C1-6)alquilsulfinil-(C1-6)alquilo, (C1-6)alquilsulfonil- (C16)alquilo, ciano-(C1-6)alquilo, amino-(C1-6)alquilo, (C1-6)alquilamino-(C1-6)alquilo, di-[(1-6)alquil]amino-(C1-6)alquilo, (C2-6)alcanoilamino-(C1-6)alquilo, N-(C1-6)alquil-(C2-6) alcanoilamino-(C1-6)alquilo, (C1-6)alcoxicarbonilamino-(C1- 6)alquilo, ureido-(C1-6)alquilo, N-(C1-6)alquilureido-(C1-6)alquilo, N'-(C1-6) alquilureido-(C1-6)alquilo, N',N'-di-[(C1-6)alquil]ureido-(C1-6)alquilo, N,N'-di-[(C1-6)alquil]ureido-(C1-6)alquilo o N,N',N'-tri-[(C1-6)alquil] ureido-(C1-6)alquilo, o entre un grupo de la formula -X4-Q2 en donde X4 es un enlace directo o se selecciona entre O, CO y N(R11), en donde R11 es H o (C1-8)alquilo, y Q2 es arilo, aril-(C1-6)alquilo, heteroarilo, heteroaril-(C1-6)alquilo, heterociclilo o heterociclil-(C1- 6) alquilo que tiene opcionalmente 1 o 2 sustituyentes, que pueden ser iguales o diferentes, seleccionados entre halogeno, hidroxi, (C1-8) alquilo y (C1-6)alcoxi, y en donde cualquier grupo arilo, heteroarilo o heterociclilo dentro de un sustituyente sobre R1 tiene opcionalmente un grupo (C1-3) alquilendioxi, y en donde cualquier grupo heterociclilo dentro de un sustituyente R1 tiene opcionalmente 1 o 2 sustituyentes oxo o tioxo, y en donde cualquier grupo CH, CH2 o CH3 dentro de un sustituyente R1 tiene opcionalmente en cada uno de dichos grupos CH, CH2 o CH3 uno o más sustituyentes halogeno o (C1-8)alquilo y/o un sustituyente seleccionado entre hidroxi, mercapto, amino, ciano, carboxi, carbamoilo, ureido, (C1-6)alcoxi, (C1-6)alquiltio, (C1-6)alquilsulfinilo, (C1-6)alquilsulfonilo, (C1-6)alquilamino, di-[(C1-6)alquil]amino, (C1-6)alcoxicarbonilo, N-(C1-6)alquilcarbamoilo, N,N-di-[(C1-6)alquil]carbamoilo, (C2-6)alcanoilo, (C2-6) alcanoiloxi, (C2-6)alcanoilamino, N-(C1-6)alquil-(C2- 6)alcanoilamino, N-(C1-6)alquilureido, N'-(C1-6)alquilureido, N',N',-di-[(C1-6)alquil] ureido, N,N'-di-[(C1-6)alquil]ureido, N,N'N'-tri-[(C1-6)alquil]ureido, N-(C1-6)alquilsulfamoilo, N,N-di-[(C1-6)alquil]sulfamoilo, (C1-6) alcansulfonilamino y N-(C1- 6)alquil-(C1-6)alcansulfonilamino, y en donde los C adyacentes en cualquier cadena (C2-6)alquileno dentro de un sustituyente R1 están opcionalmente separados por la insercion en la cadena de un grupo seleccionado entre O, S, SO, SO2, N(R12), CO, CH(OR12), CON(R12), N(R12)CO, N(R12)CON(R12), SO2N(R12), N(R12)SO2, CH=CH y C:::C en donde R12 es H o (C1-8) alquilo, o cuando el grupo insertado es N(R12), R12 también puede ser (C2-6) alcanoilo; q es 0, 1 o 2; cada grupo R2, que pueden ser iguales o diferentes, se selecciona entre halogeno, trifluorometilo, ciano, hidroxi, amino, (C1-8)alquilo, (C2-8) alquenilo, (C2-8) alquinilo, (C1-6) alcoxi, (C1-6) alquilamino y di[(C1-6) alquil]amino; R3 es H, (C1-8)alquilo, (C2-8) alquenilo, (C2-8) alquinilo, R4 es H, (C1-8) alquilo, (C2-8) alquenilo, (C2-8) alquinilo, halogeno-(C1-6)alquilo, hidroxi-(C1-6)alquilo, (C1-6)alcoxi-(C1-6)alquilo, ciano-(C1-6)alquilo, carboxi-(C1-6)alquilo, amino-(C1-6)alquilo, (C1-6)alquilamino-(C1-6)alquilo, di- [(C1-6)alquil]amino-(C1-6)alquilo, carbamoil-(C1-6) alquilo, N-(C1-6)alquilcarbamoil-(C1-6)alquilo, N,N-di-[(C1-6)alquil]carbamoil-(C1-6)alquilo, (C1-6)alcoxicarbonil-(C1-6)alquilo, (C2-6) alcanoilamino-(C1-6)alquilo o N-(C1-6)alquil-(C2- 6)alcanoilamino-(C1-6)alquilo; o R3 y R4 junto con el átomo de C al cual están unidos forman un grupo (C3-8) cicloalquilo; R5 es H, (C1-8)alquilo, (C2-8) alquenilo o (C2-8) alquinilo o un grupo de la formula -X5-R13 en donde X5 es un enlace directo o se selecciona entre O y N(R14), en donde R14 es H o (C1-8) alquilo, y R13 es halogeno-(C1-6)alquilo, hidroxi-(C1-6)alquilo, (C1-6)alcoxi-(C1-6)alquilo o ciano-(C1-6)alquilo; el anillo A es un anillo arilo bicíclico de 10m miembros o monocíclico de 6 miembros o un anillo heteroarilo bicíclico de 9-10 miembros o monocíclico de 5 o 6 miembros con hasta tres heteroátomos en el anillo seleccionados entre O, N y S; X1 es un enlace directo o se selecciona entre O, S, SO, SO2, N(R15), CO, CH(OR15), CON(R15), N(R15)CO, N(R15)CON(R15), SO2N(R15), N(R15)SO2, C(R15)2O, C(R15)2S, C(R15)2N(R15) y C(R15)2C(R15) 2N(R15), en donde cada R15 es H o (C1-8) alquilo; R6 es halogeno-(C1-6)alquilo, hidroxi-(C1-6)alquilo, mercapto-(C1-6)alquilo, (C1-6) alcoxi- (C1-6)alquilo, (C1-6)alquiltio-(C1-6)alquilo, (C1-6)alquilsulfinil-(C1-6)alquilo, (C1-6)alquilsulfonil-(C16)alquilo, ciano-(C1-6)alquilo, amino-(C1-6)alquilo, (C1-6)alquilamino-(C1-6)alquilo, di-[(1-6)alquil]amino-(C1-6)alquilo, (C2-6)alcanoilamino- (C1-6)alquilo, N-(C1-6) alquil-(C2-6)alcanoilamino-(C1-6)alquilo, carboxi-(C1-6)alquilo, (C1-6)alcoxicarbonil-(C1-6)alquilo, carbamoil-(C1-6)alquilo, N-(C1-6) alquilcarbamoil-(C1-6)alquilo, N,N-di-[(C1-6)alquil]carbamoil-(C1-6)alquilo, sulfamoil-(C1- 6)alquilo, N-(C1-6)alquilsulfamoil-(C1-6)alquilo, N,N-di-[(C1-6)alquil]sulfamoil-(C1-6)alquilo, ureido-(C1-6)alquilo, N-(C1-6)alquilureido-(C1-6)alquilo, N'-(C1-6)alquilureido-(C1-6)alquilo, N',N',-di-[(C1-6)alquil]ureido-(C1-6)alquilo, N,N'-di-[(C1- 6)alquil]ureido-(C1-6)alquilo, N,N'N'-tri-[(C1-6)alquil]ureido-(C1-6)alquilo, (C1-6)alcansulfonilamino-(C1-6)alquilo o N-(C1-6)alquil-(C1-6)alcansulfonilamino-(C1-6)alquilo, o R6 es arilo, aril-(C1-6)alquilo, (C3-8) cicloalquilo (C3-8)cicloalquil- (C1-6)alquilo, (C3-8)cicloalquenilo, (C3-8)cicloalquenil-(C1-6)alquilo, heteroarilo, heteroaril-(C1-6)alquilo, heterociclilo o heterociclil-(C1-6)alquilo, o, cuando X1 es un enlace directo, R6 puede ser carboxi, (C1-6)alcoxicarbonilo, sulfamoilo, N- (C1-6)alquilsulfamoilo o N,N-di-[(C1-6)alquil]sulfamoilo, o el grupo -X1-R6 y un grupo R7 forman juntos un grupo bivalente que se extiende sobre posiciones adyacentes en el anillo Ha seleccionado entre OC(R20)2O, OC(R20)2C(R20)2O, OC(R20)2C(R20)2, C(R20) 2OC(R20)2, C(R20)2C(R20)2C(R20)2, C(R20)2C(R20)2C(R20)2C(R20)2, OC(R20)2N(R21), OC(R20)2C(R20)2(NR21), N(R21)C(R20) 2N(R21), N(R21)C(R20)2C(R20)2, N(R21)C(R20)2C(R20)2C(R20)2, C(R20)2N(R21)C (R20)2, CO.N(R21)C(R20)2, N(R21)CO.C(R20)2, N(R21)C(R20)2CO, CO.N(R21)CO, N(R21)N(R21)CO, N(R21)CO.N(R21), O.CO.N(R21), O.CO.C(R20)2 y CO.OC(R20)2 en donde cada R20 es H, (C1-8) alquilo, (C2-8) alquenilo o (C2-8)alquinilo, y en donde R21 es H, (C1-8) alquilo, (C2-8) alquenilo, (C2- 8)alquinilo o (C2-8) alcanoilo, y en donde cualquier grupo arilo, (C3-8)cicloalquilo, (C3-8)cicloalquenilo, heteroarilo o heterociclilo dentro del grupo R6 tiene opcionalmente 1, 2 o 3 sustituyentes, que pueden ser iguales o diferentes, seleccionados entre halogeno, trifluorometilo, ciano, nitro, hidroxi., amino, carboxi, carbamoilo, ureido, (C1-8) alquilo, (C2-8) alquenilo, (C2-8) alquinilo, (C1-6) alcoxi, (C2-6) alqueniloxi, (C2-6) alquiniloxi, (C1-6) alquiltio, (C1-6) alquilsulfinilo, (C1-6) alquilsulfonilo, (C1-6) alquilamino, di-[(C1-6)alquil]amino, (C1-6)alcoxicarbonilo, (C2-6)alcanoilo, (C2-6)alcanoiloxi, N-(C1-6)alquilcarbamoilo, N,N-di-[(C1-6)alquil]carbamoilo, (C2-6)alcanoilamino, N-(C1-6)alquil-(C2- 6) alcanoilamino, N'-(C1-6)alquilureido, N',N',-di-[(C1-6)alquil]ureido, N-(C1-6)alquilureido, N,N'-di-[(C1-6)alquil]ureido, N,N'N'-tri-[(C1-6) alquil]ureido, N-(C1-6)alquilsulfamoilo, N,N-di[(C1-6)alquil]sulfamoilo, (C1-6)alcansulfonilamino y N-(C1- 6)alquil-(C1-6) alcansulfonilamino, o entre un grupo de la formula: -X6-R16 en donde X6 es un enlace directo o se selecciona entre O y N(R17), en donde R17 es H o (C1-8) alquilo, y R16 es halogeno-(C1-6)alquilo, hidroxi-(1-6)alquilo, mercapto-(C1- 6)alquilo, (C1-6)alcoxi-(C1-6) alquilo, (C1-6)alquiltio-(C1-6)alquilo, (C1-6)alquilsulfinil-(C1-6)alquilo, (C1-6)alquilsulfo
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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EP04292418 | 2004-10-12 |
Publications (1)
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AR052315A1 true AR052315A1 (es) | 2007-03-14 |
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Family Applications (1)
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ARP050104278A AR052315A1 (es) | 2004-10-12 | 2005-10-12 | Derivados de quinazolina utiles para el tratamiento de cancer |
Country Status (6)
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US (1) | US20090036474A1 (es) |
EP (1) | EP1802608A1 (es) |
JP (1) | JP2008515961A (es) |
AR (1) | AR052315A1 (es) |
TW (1) | TW200628466A (es) |
WO (1) | WO2006040526A1 (es) |
Families Citing this family (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
SI1463506T1 (sl) * | 2001-12-24 | 2010-01-29 | Astrazeneca Ab | Substituirani kinazolinski derivati kot inhibitorji kinaz Aurora |
KR20070084172A (ko) | 2004-10-12 | 2007-08-24 | 아스트라제네카 아베 | 퀴나졸린 유도체 |
WO2007099323A2 (en) * | 2006-03-02 | 2007-09-07 | Astrazeneca Ab | Quinoline derivatives |
UY30183A1 (es) * | 2006-03-02 | 2007-10-31 | Astrazeneca Ab | Derivados de quinolina |
CN102964256B (zh) * | 2012-11-28 | 2014-05-07 | 浙江海翔药业股份有限公司 | 一种4-氨基-n,n-二甲基苄胺的制备方法 |
AU2014219024B2 (en) * | 2013-02-20 | 2018-04-05 | KALA BIO, Inc. | Therapeutic compounds and uses thereof |
CN103159685A (zh) * | 2013-04-11 | 2013-06-19 | 苏州立新制药有限公司 | 4-氯-6,7-二(2-甲氧基乙氧基)喹唑啉的制备方法 |
AU2014342042B2 (en) * | 2013-11-01 | 2017-08-17 | KALA BIO, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
CA3109285A1 (en) * | 2013-11-01 | 2015-05-07 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
AU2014353006B2 (en) | 2013-11-20 | 2019-04-04 | Signalchem Life Sciences Corp. | Quinazoline derivatives as TAM family kinase inhibitors |
WO2016055786A1 (en) | 2014-10-08 | 2016-04-14 | Redx Pharma Plc | N-pyridinyl acetamide derivatives as inhibitors of the wnt signalling pathway |
AU2015329788B2 (en) | 2014-10-08 | 2019-10-10 | Redx Pharma Plc | N-pyridinyl acetamide derivatives as Wnt signalling pathway inhibitors |
CA3036336A1 (en) | 2016-09-08 | 2018-03-15 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
BR112019004463A2 (pt) | 2016-09-08 | 2019-05-28 | Kala Pharmaceuticals Inc | formas cristalinas de compostos terapêuticos, seus processos de obtenção e seus métodos de uso |
US10392399B2 (en) | 2016-09-08 | 2019-08-27 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
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US5476851A (en) * | 1994-09-08 | 1995-12-19 | Rhone-Poulenc Rorer Pharmaceuticals, Inc. | Pyrazolo[3,4-g]quinoxaline compounds which inhibit PDGF receptor protein tyrosine kinase |
SI1578755T1 (sl) * | 2002-12-24 | 2007-12-31 | Astrazeneca Ab | Fosfonooksi kinazolinski derivati in njihova farmacevtska uporaba |
CN1809557B (zh) * | 2003-04-16 | 2012-07-04 | 阿斯利康(瑞典)有限公司 | 化合物 |
JP2008515960A (ja) * | 2004-10-12 | 2008-05-15 | アストラゼネカ アクチボラグ | キノリン誘導体 |
US7652041B2 (en) * | 2005-01-14 | 2010-01-26 | Millennium Pharmaceuticals, Inc. | Cinnamide and hydrocinnamide derivatives with kinase inhibitory activity |
-
2005
- 2005-10-07 JP JP2007536246A patent/JP2008515961A/ja not_active Withdrawn
- 2005-10-07 EP EP05790971A patent/EP1802608A1/en not_active Withdrawn
- 2005-10-07 US US11/665,115 patent/US20090036474A1/en not_active Abandoned
- 2005-10-07 WO PCT/GB2005/003881 patent/WO2006040526A1/en active Application Filing
- 2005-10-12 TW TW094135557A patent/TW200628466A/zh unknown
- 2005-10-12 AR ARP050104278A patent/AR052315A1/es not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
TW200628466A (en) | 2006-08-16 |
JP2008515961A (ja) | 2008-05-15 |
WO2006040526A1 (en) | 2006-04-20 |
US20090036474A1 (en) | 2009-02-05 |
EP1802608A1 (en) | 2007-07-04 |
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