AR040770A1 - Benzimidazoles y benzotiazoles como inhibidores de quinasas - Google Patents
Benzimidazoles y benzotiazoles como inhibidores de quinasasInfo
- Publication number
- AR040770A1 AR040770A1 AR20030102781A ARP030102781A AR040770A1 AR 040770 A1 AR040770 A1 AR 040770A1 AR 20030102781 A AR20030102781 A AR 20030102781A AR P030102781 A ARP030102781 A AR P030102781A AR 040770 A1 AR040770 A1 AR 040770A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- optionally substituted
- halo
- alkoxy
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Reivindicación 1: Un compuesto de fórmula (1) en la que: W es como se muestra en el grupo de restos de fórmulas 2 a 11; X es N(R4) o S; R0 es (a) seleccionado entre el grupo compuesto por H, alquilo C1-6, ciano, (alquileno C1-4)-R11, 3-hidroxiprop-2-ilo, (1-fenil)-2-hidroxiet-1-ilo, (1-ciclohexil)-3-hidroxiprop-2-ilo, 4-metoxibencilo, 1,4-dioxoespiro[4,5]dec-8-ilo, tetrahidropirano, 2,2,6,6-tetrametilpiperidin-4-ilo y ciclohexan-1-on-4-ilo, (b) fenilo opcionalmente sustituido con un sustituyente seleccionado entre el grupo compuesto por nitro y amino; (c) piperidin-4-ilo opcionalmente sustituido con un sustituyente seleccionado entre el grupo compuesto por alquilo C1-4, alcoxi C1-4 carbonilo y bencilo, o (d) cicloalquilo C3-6 opcionalmente sustituido con un sustituyente seleccionado entre el grupo compuesto por alcoxi C1-4 carbonilamino, amino, hidroxi y alquileno C1-4-OH; R1 es (a) seleccionado entre el grupo compuesto por H, alquilo C1-6, alquinilo C2-4, halo, amino, azido, formilo, 1-(alcoxi C1-4carbonil)eten-2-ilo, 1-(alcoxi C1-4 carbonil)etilo, 1-(carboxi C1-4)etilo, (alquileno C1-4)benciloxi, trifluorometilo, trimetilsililetinilo, but-3-in-1-ol, cicloalquilo C3-6, tetrahidropiran-4-ilo, hidroximetilo, 2-(piperidin-1-il)metilo, N,N`,N`-[trimetil]-2-(aminoetilamino)metilo, (morfolin-4-il)metilo, dimetilaminoetilo, N-[2-(piperidin-1-il)et-1-il]aminometilo, N´,N´-dimetil-2-(aminoetilamino)metilo, piridinilo, tiazolilo, triazolilo, benzo(1,3)dioxolan-5-ilo e imidazol-2-ilo, (b) fenilo opcionalmente sustituido con uno a tres sustituyentes seleccionados independientemente entre el grupo compuesto por alquilo C1-4, halo, nitro, amino, alcoxi C1-4, trifluorometilo, trifluorometoxi, trifluorometilsulfanilo, metilsulfonilo, metilsulfonamidilo, pirrolidin-1-ilo, morfolin-4-ilo, 4-(alquil C1-4)piperazin-1-ilo, -NR6R7 y alcoxi C1-4 opcionalmente sustituido con un sustituyente seleccionado entre el grupo compuesto por piperidin-1-ilo, pirrolidin-1-ilo, morfolin-4-ilo, azepin-4-ilo y di(alquil C1-4)amino, (c) tienilo opcionalmente sustituido con un sustituyente seleccionado entre el grupo compuesto por halo, nitro, amino y alquilo C1-4, o (d) piperidin-4-ilo opcionalmente sustituido en la posición 1 del grupo compuesto por alquilo C1-4, alcoxi C1-4 carbonilo, benciloxicarbonilo y (alquileno C1-4)-R8; Como alternativa R0 y R1 pueden tomarse conjuntamente para formar una cadena de C C3-4 totalmente saturada o una cadena de C C3-4 totalmente insaturada opcionalmente sustituida con halo o alquilo C1-4; R2 es H, alquilo C1-4 o bencilo; R3 es tienilo o fenilo opcionalmente sustituido con de uno a dos sustituyentes seleccionados independientemente entre el grupo compuesto por halo, alquilo C1-4, alcoxi C1-4 y trifluorometilo; R4 es H, (alquil C1-4)sulfonilo o (cicloalquil C3-6)sulfonilo; o (alquil C1-4)2N-sulfonilo; R5 es halo, H o -NR9R10; R6 y R7 se seleccionan individualmente en cada caso entre H, carbonilo o alquilo C1-4 con la condición de que al menos uno de R6 y R7 es H; R8 es hidroxi, trifluorometilo, dimetilamino, fenilo, piridinilo o 1-metilimidazol-2-ilo; R9 es independientemente en cada caso H o alquilo C1-*4; R10 es H, alquilo C1-4 o bencilo; R11 es alcoxi C1-4, hidroxi, alcoxi C1-4carbonilo, alcoxi C1-4 carbonilamino, cicloalquilo C3-6, fenilo opcionalmente sustituido con de uno a dos sustituyentes seleccionados independientemente entre el grupo compuesto por alcoxi C1-4 y halo, morfolin-4-ilo o piridinilo; con la condición de que cuando W es como se muestra en el resto de fórmula (3) entonces (a) al menos uno de R0 y R1 es H o alquilo C1-6; o (b) R0 y R1 pueden tomarse juntos para formar una cadena de C C3-4 totalmente saturada o una cadena de C C3-4 totalmente insaturada opcionalmente sustituida con halo o alquilo C1-4; con la condición adicional de que cuando X es S, W es como se muestra en el resto de fórmula (3); o una sal farmacéuticamente aceptable o un solvato farmacéuticamente aceptable del mismo.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02380178 | 2002-08-09 | ||
| US42193902P | 2002-10-28 | 2002-10-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR040770A1 true AR040770A1 (es) | 2005-04-20 |
Family
ID=31716856
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AR20030102781A AR040770A1 (es) | 2002-08-09 | 2003-08-01 | Benzimidazoles y benzotiazoles como inhibidores de quinasas |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US7320995B2 (es) |
| EP (1) | EP1554272B1 (es) |
| AR (1) | AR040770A1 (es) |
| AT (1) | ATE343572T1 (es) |
| AU (1) | AU2003256297A1 (es) |
| DE (1) | DE60309342T2 (es) |
| ES (1) | ES2274302T3 (es) |
| TW (1) | TW200404799A (es) |
| WO (1) | WO2004014900A1 (es) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20060063065A1 (en) * | 2001-08-10 | 2006-03-23 | Clarke Robert L | Battery with bifunctional electrolyte |
| EP1720862A1 (en) * | 2004-02-03 | 2006-11-15 | Eli Lilly And Company | Kinase inhibitors |
| US7253200B2 (en) * | 2004-03-25 | 2007-08-07 | Janssen Pharmaceutica, N.V. | Imidazole compounds |
| TW200639163A (en) * | 2005-02-04 | 2006-11-16 | Genentech Inc | RAF inhibitor compounds and methods |
| US7473784B2 (en) | 2005-08-01 | 2009-01-06 | Bristol-Myers Squibb Company | Benzothiazole and azabenzothiazole compounds useful as kinase inhibitors |
| ES2301380B1 (es) | 2006-08-09 | 2009-06-08 | Laboratorios Almirall S.A. | Nuevos derivados de 1,7-naftiridina. |
| MX2009003650A (es) * | 2006-10-06 | 2009-04-22 | Abbott Lab | Nuevos imidazotiazoles e imidazoxazoles. |
| ES2320955B1 (es) | 2007-03-02 | 2010-03-16 | Laboratorios Almirall S.A. | Nuevos derivados de 3-((1,2,4)triazolo(4,3-a)piridin-7-il)benzamida. |
| ES2329639B1 (es) | 2007-04-26 | 2010-09-23 | Laboratorios Almirall S.A. | Nuevos derivados de 4,8-difenilpoliazanaftaleno. |
| EP1992344A1 (en) | 2007-05-18 | 2008-11-19 | Institut Curie | P38 alpha as a therapeutic target in pathologies linked to FGFR3 mutation |
| US20090156594A1 (en) * | 2007-05-21 | 2009-06-18 | Sgx Pharmaceuticals, Inc. | Heterocyclic kinase modulators |
| WO2009005675A1 (en) | 2007-06-28 | 2009-01-08 | Abbott Laboratories | Novel triazolopyridazines |
| EP2108641A1 (en) | 2008-04-11 | 2009-10-14 | Laboratorios Almirall, S.A. | New substituted spiro[cycloalkyl-1,3'-indo]-2'(1'H)-one derivatives and their use as p38 mitogen-activated kinase inhibitors |
| EP2113503A1 (en) | 2008-04-28 | 2009-11-04 | Laboratorios Almirall, S.A. | New substituted indolin-2-one derivatives and their use as p39 mitogen-activated kinase inhibitors |
| EP2623101B1 (en) * | 2009-04-02 | 2021-04-21 | Merck Patent GmbH | Piperidine and piperazine derivatives as autotaxin inhibitors |
| BR112012010041A2 (pt) | 2009-10-30 | 2016-05-24 | Janssen Pharmaceutica Nv | derivados de imidazo [1,2-b] piridazina e seu uso como inibidores de pde10 |
| EP2322176A1 (en) | 2009-11-11 | 2011-05-18 | Almirall, S.A. | New 7-phenyl-[1,2,4]triazolo[4,3-a]pyridin-3(2H)-one derivatives |
| AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
| AR083868A1 (es) | 2010-12-03 | 2013-03-27 | Lilly Co Eli | Compuestos de oxazol[5,4-b]piridin-5-ilo |
| WO2013000924A1 (en) | 2011-06-27 | 2013-01-03 | Janssen Pharmaceutica Nv | 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES |
| EA028626B1 (ru) * | 2012-06-11 | 2017-12-29 | Юсб Байофарма Спрл | БЕНЗИМИДАЗОЛЫ, МОДУЛИРУЮЩИЕ TNF-α |
| ES2855575T3 (es) | 2012-06-26 | 2021-09-23 | Janssen Pharmaceutica Nv | Combinaciones que comprenden compuestos de 4-metil-[1,2,4]triazolo[4,3-a]quinoxalina como inhibidores de PDE2 e inhibidores de PDE10 para su uso en el tratamiento de trastornos neurológicos o metabólicos |
| EP2869822B1 (en) | 2012-07-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | Inhibitors of phosphodiesterase 10 enzyme |
| GB201321729D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| GB201321743D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| GB201321738D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic Agents |
| GB201321730D0 (en) * | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| WO2016081364A1 (en) | 2014-11-21 | 2016-05-26 | Rigel Pharmaceuticals, Inc. | Fused imidazole derivatives as tgf-beta inhibitors |
| EP3954685B1 (en) | 2014-12-29 | 2025-08-27 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Small molecule inhibitors of lactate dehydrogenase and methods of use thereof |
| ES2789331T3 (es) | 2015-03-02 | 2020-10-26 | Rigel Pharmaceuticals Inc | Inhibidores de TGF-beta |
| ES2918924T3 (es) * | 2015-04-01 | 2022-07-21 | Rigel Pharmaceuticals Inc | Inhibidores de TGF-beta |
| US20190060286A1 (en) | 2016-02-29 | 2019-02-28 | University Of Florida Research Foundation, Incorpo | Chemotherapeutic Methods |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| KR20200067170A (ko) | 2017-10-05 | 2020-06-11 | 풀크럼 쎄러퓨틱스, 인코포레이티드 | FSHD의 치료를 위하여 DUX4 및 하류 유전자 발현을 저감시키는 p38 키나제 저해제 |
| CN109467535B (zh) * | 2018-11-14 | 2022-07-12 | 江苏宝众宝达药业有限公司 | 一种芬苯达唑的制备方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX9300141A (es) * | 1992-01-13 | 1994-07-29 | Smithkline Beecham Corp | Compuestos de imidazol novedosos, procedimiento para su preparacion y composiciones farmaceuticas que lo contienen. |
| US6426360B1 (en) * | 1994-07-28 | 2002-07-30 | G D Searle & Co. | 4,5-substituted imidazolyl compounds for the treatment of inflammation |
| IL118544A (en) | 1995-06-07 | 2001-08-08 | Smithkline Beecham Corp | History of imidazole, the process for their preparation and the pharmaceutical preparations containing them |
| US5717100A (en) * | 1995-10-06 | 1998-02-10 | Merck & Co., Inc. | Substituted imidazoles having anti-cancer and cytokine inhibitory activity |
| KR19990077164A (ko) * | 1996-01-11 | 1999-10-25 | 스티븐 베네티아너 | 신규 치환된 이미다졸 화합물 |
| US6087496A (en) * | 1998-05-22 | 2000-07-11 | G. D. Searle & Co. | Substituted pyrazoles suitable as p38 kinase inhibitors |
| EP1037639A4 (en) * | 1997-12-19 | 2002-04-17 | Smithkline Beecham Corp | HETEROARYL-SUBSTITUTED IMIDAZOLE COMPOUNDS, THEIR PHARMACEUTICAL COMPOSITIONS AND USES |
| ATE266399T1 (de) | 1998-08-20 | 2004-05-15 | Smithkline Beecham Corp | Neue substituierte triazolverbindungen |
| US6465493B1 (en) | 1999-04-09 | 2002-10-15 | Smithkline Beecham Corporation | Triarylimidazoles |
| GB0007405D0 (en) | 2000-03-27 | 2000-05-17 | Smithkline Beecham Corp | Compounds |
| AP2002002460A0 (en) * | 2001-03-09 | 2002-06-30 | Pfizer Prod Inc | Novel benzimidazole anti-inflammatory compounds. |
| GB0127430D0 (en) * | 2001-11-15 | 2002-01-09 | Smithkline Beecham Corp | Compounds |
-
2003
- 2003-07-31 ES ES03784749T patent/ES2274302T3/es not_active Expired - Lifetime
- 2003-07-31 AU AU2003256297A patent/AU2003256297A1/en not_active Abandoned
- 2003-07-31 EP EP03784749A patent/EP1554272B1/en not_active Expired - Lifetime
- 2003-07-31 DE DE60309342T patent/DE60309342T2/de not_active Expired - Fee Related
- 2003-07-31 AT AT03784749T patent/ATE343572T1/de not_active IP Right Cessation
- 2003-07-31 US US10/522,227 patent/US7320995B2/en not_active Expired - Fee Related
- 2003-07-31 WO PCT/US2003/019890 patent/WO2004014900A1/en not_active Ceased
- 2003-08-01 TW TW092121140A patent/TW200404799A/zh unknown
- 2003-08-01 AR AR20030102781A patent/AR040770A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| ATE343572T1 (de) | 2006-11-15 |
| EP1554272A1 (en) | 2005-07-20 |
| TW200404799A (en) | 2004-04-01 |
| AU2003256297A1 (en) | 2004-02-25 |
| US20050272791A1 (en) | 2005-12-08 |
| WO2004014900A1 (en) | 2004-02-19 |
| US7320995B2 (en) | 2008-01-22 |
| EP1554272B1 (en) | 2006-10-25 |
| ES2274302T3 (es) | 2007-05-16 |
| DE60309342T2 (de) | 2007-05-16 |
| DE60309342D1 (de) | 2006-12-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |