AR045811A1 - 5- arilpirimidinas como agentes ainticancerigenos - Google Patents
5- arilpirimidinas como agentes ainticancerigenosInfo
- Publication number
- AR045811A1 AR045811A1 ARP040103441A ARP040103441A AR045811A1 AR 045811 A1 AR045811 A1 AR 045811A1 AR P040103441 A ARP040103441 A AR P040103441A AR P040103441 A ARP040103441 A AR P040103441A AR 045811 A1 AR045811 A1 AR 045811A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- mammal
- compounds
- pharmaceutically acceptable
- acceptable salt
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/48—Two nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—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
- C07D405/02—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 two hetero rings
- C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Compuestos de 5-arilpirimidinas o su sal farmacéuticamente aceptable, y composiciones que contienen dichos compuestos o su sal farmacéuticamente aceptable, en donde dichos compuestos son agentes anticancerígenos útiles para el tratamiento del cáncer en mamíferos. Proceso para la preparación de los compuestos. Método para tratar o inhibir el crecimiento de células tumorales cancerosas y enfermedades asociadas en un mamífero y provee además un método para el tratamiento o prevención de tumores cancerosos que expresan resistencia a fármacos múltiples (MDR) o son resistentes debido a MDR, en un mamífero que lo necesita cuyo método comprende administrar a dicho mamífero una cantidad efectiva de dichos compuestos o su sal farmacéuticamente aceptable. Más específicamente, método para tratar o inhibir el crecimiento de células de tumores cancerosos y enfermedades asociadas en un mamífero que lo necesita mediante promoción de polimerización de microtúbulos la cual comprende administrar a dicho mamífero una cantidad efectiva de dichos compuestos y sus sales farmacéuticamente aceptables. Reivindicación 1: Un método para tratar o inhibir el crecimiento de células tumorales cancerosas y enfermedades asociadas en un mamífero que lo necesita administrando una cantidad efectiva de un compuesto de fórmula (1), en donde: Z ase selecciona de la fórmula (2), y cicloalquilo C6-8; R es una porción de fórmula (3); X es Cl o Br; L1, L2, L3, y L4 son cada uno independientemente H, F, Cl o Br; A es H, F, Cl, Br o Y(CH2)nQ; Y es O, S o NR2; n es un número entero de 2, 3 ó 4; Q es OH o -NR3R4; R1 es H o alquilo C1-3; R2 es H o alquilo C1-3; R3 y R4 son cada uno independientemente H o alquilo C1-3; o R3 y R4 cuando opcionalmente son tomados en forma conjunta con el átomo de nitrógeno al cual cada uno está unido forman un anillo heterocíclico de 4 a 6 átomos en el anillo opcionalmente sustituido con R7; R5 es CF3 o C2F5; W' es -NHR6, -N(CN)R6, arilo C6-12 sustituido opcionalmente con 1-3 grupos seleccionados independientemente de los grupos halógeno, azido, nitro, ciano, hidroxi, alquilo C1-3, alcoxi C1-3, amino, alquilamino C1-3, dialquilamino C1-3, formilo, alcoxicarbonilo C1-3, carboxilo, alcanoilo C1-3, alquiltio C1-3, alquilamido C1-3, fenilo, fenoxi, bencilo, benzoxi, furilo y ciclopropilo; o heteroarilo de 5 a 10 átomos en el anillo que tienen 1 a 4 heteroátomos seleccionados de S, O y N y opcionalmente sustituidos con 1-3 grupos seleccionados independientemente de grupos halógeno, azido, nitro, ciano, hidroxi, alquilo C1-3, alcoxi C1-3, amino, alquilamino C1-3, dialquilamino C1-3, formilo, alcoxicarbonilo C1-3, carboxilo, alcanoilo C1-3, alquiltio C1-3, alquilamido C1-3, fenilo, fenoxi, bencilo, benzoxi, furilo y ciclopropilo; R6 es alquilo C1-3, R7 es alquilo C1-3; o su sal farmacéuticamente aceptable.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US50548703P | 2003-09-24 | 2003-09-24 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR045811A1 true AR045811A1 (es) | 2005-11-16 |
Family
ID=34393022
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040103441A AR045811A1 (es) | 2003-09-24 | 2004-09-23 | 5- arilpirimidinas como agentes ainticancerigenos |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US7524849B2 (es) |
| EP (1) | EP1663241B1 (es) |
| JP (1) | JP2007506746A (es) |
| KR (1) | KR20060089215A (es) |
| CN (1) | CN1871009A (es) |
| AR (1) | AR045811A1 (es) |
| AT (1) | ATE432077T1 (es) |
| AU (1) | AU2004275733A1 (es) |
| BR (1) | BRPI0414736A (es) |
| CA (1) | CA2539235A1 (es) |
| CO (1) | CO5690592A2 (es) |
| DE (1) | DE602004021269D1 (es) |
| EC (1) | ECSP066457A (es) |
| GT (1) | GT200400188A (es) |
| IL (1) | IL174305A0 (es) |
| MX (1) | MXPA06003207A (es) |
| NO (1) | NO20061319L (es) |
| PA (1) | PA8613201A1 (es) |
| PE (1) | PE20050470A1 (es) |
| RU (1) | RU2006107578A (es) |
| SA (1) | SA04250303A (es) |
| TW (1) | TW200512198A (es) |
| WO (1) | WO2005030216A1 (es) |
| ZA (1) | ZA200602386B (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200637556A (en) * | 2005-01-31 | 2006-11-01 | Basf Ag | Substituted 5-phenyl pyrimidines I in therapy |
| CN101193884A (zh) | 2005-06-13 | 2008-06-04 | 惠氏公司 | 微管蛋白抑制剂和其制备方法 |
| BRPI0612145A2 (pt) * | 2005-06-13 | 2010-10-19 | Wyeth Corp | inibidor de tubulina e processo para sua preparação |
| CN101453893A (zh) * | 2006-03-27 | 2009-06-10 | 巴斯夫欧洲公司 | 取代的5-杂芳基-4-氨基嘧啶 |
| CL2007002231A1 (es) * | 2006-08-02 | 2008-04-11 | Basf Ag | Uso de compuestos derivados de 5-(het) arilpirimidina para combatir hongos daninos; compuestos derivados de 5-(het) arilpirimidina; agente fungicida; y agente farmaceutico. |
| TW200836741A (en) * | 2007-01-11 | 2008-09-16 | Basf Ag | 2-substituted pyrimidines I in therapy |
| WO2009007187A1 (de) * | 2007-07-09 | 2009-01-15 | Basf Se | Substituierte 5-hetarylpyrimidine |
| RU2625309C2 (ru) | 2011-04-22 | 2017-07-13 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Замещенные диаминокарбоксамидные и диаминокарбонитрильные производные пиримидинов, их композиции и способы лечения с их помощью |
| EP2903436B1 (en) | 2012-09-19 | 2019-07-17 | The Trustees Of The University Of Pennsylvania | Heterocyclic compounds and their use for the treatment of neurodegenerative tauopathies |
| NZ715903A (en) | 2014-01-30 | 2017-06-30 | Signal Pharm Llc | Solid forms of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide, compositions thereof and methods of their use |
| US9513297B2 (en) | 2014-12-16 | 2016-12-06 | Signal Pharmaceuticals, Llc | Methods for measurement of inhibition of c-Jun N-terminal kinase in skin |
| ES2877642T3 (es) | 2014-12-16 | 2021-11-17 | Signal Pharm Llc | Formulaciones de 2-(terc-butilamino)-4-((1R,3R,4R)-3-hidroxi-4-metilciclohexilamino)-pirimidin-5-carboxamida |
| CA2975260C (en) | 2015-01-29 | 2024-05-21 | Signal Pharmaceuticals Llc | Isotopologues of 2-(tert-butylamino)-4-((1r,3r,4r)-3-hydroxy-4-methylcyclohexylamino)-pyrimidine-5-carboxamide |
| EP3325432B1 (en) | 2015-07-24 | 2020-09-02 | Celgene Corporation | Methods of synthesis of (1r,2r,5r)-5-amino-2-methylcyclohexanol hydrochloride and intermediates useful therein |
| US11623927B2 (en) | 2018-03-02 | 2023-04-11 | The Trustees Of The University Of Pennsylvania | Substituted [1,2,4]triazolo[1,5-a]pyrimidines for stabilizing microtubules |
| WO2021085540A1 (ja) * | 2019-11-01 | 2021-05-06 | ユニマテック株式会社 | 含フッ素ピリミジン化合物およびその製造方法 |
| TW202132285A (zh) * | 2019-11-13 | 2021-09-01 | 美商愛彼特生物製藥股份有限公司 | 經取代異吲哚啉基2,2’-聯嘧啶基化合物、其類似物及使用其之方法 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US61889A (en) * | 1867-02-05 | Improvement in animal teaps | ||
| US88096A (en) * | 1869-03-23 | t h a y e r | ||
| US116429A (en) * | 1871-06-27 | Improvement in dial-telegraph apparatus | ||
| US147744A (en) * | 1874-02-24 | Improvement in locomotive-furnaces | ||
| US69242A (en) * | 1867-09-24 | Calvin pepper | ||
| GB9700664D0 (en) | 1997-01-14 | 1997-03-05 | British Tech Group | Anti-cancer agents |
| US6117876A (en) | 1997-04-14 | 2000-09-12 | American Cyanamid Company | Fungicidal trifluorophenyl-triazolopyrimidines |
| US6509354B1 (en) | 1998-04-27 | 2003-01-21 | Kumiai Chemical Industry Co., Ltd. | 3-arylphenyl sulfide derivative and insecticide and miticide |
| US6156925A (en) | 1998-09-25 | 2000-12-05 | American Cyanamid Company | Process for the preparation of halogenated phenylmaloates |
| US5986135A (en) | 1998-09-25 | 1999-11-16 | American Cyanamid Company | Fungicidal trifluoromethylalkylamino-triazolopyrimidines |
| EA005927B1 (ru) | 2000-06-13 | 2005-08-25 | Басф Акциенгезельшафт | Фунгицидные 5-фенил-замещенные 2-(цианоамино)пиримидины |
| US6670362B2 (en) | 2000-09-20 | 2003-12-30 | Pfizer Inc. | Pyridazine endothelin antagonists |
| MXPA03008121A (es) | 2001-03-15 | 2003-12-12 | Basf Ag | 5-fenilpirimidinas, metodos y productos intermedios para su produccion y uso de las mismas para controlar hongos patogenicos. |
| ATE297390T1 (de) | 2001-04-20 | 2005-06-15 | Ciba Sc Holding Ag | 4-amino-2-(2-pyridinyl)pyrimidine als mikrobizide wirksubstanzen |
| NZ533265A (en) | 2001-11-19 | 2006-05-26 | Basf Ag | 5-Phenylpyrimidines, their preparation, compositions comprising them and their use |
| EP1504001B1 (de) | 2002-02-21 | 2009-04-15 | Basf Se | 2-(2-pyridyl)-5-phenyl-6-aminopyrimidine, verfahren und zwischenprodukte zu ihrer herstellung und ihre verwendung zur bekämpfung von schadpilzen |
| CN1642422A (zh) | 2002-03-15 | 2005-07-20 | 西巴特殊化学品控股有限公司 | 4－氨基嘧啶及其在表面抗菌处理中的应用 |
| EP2316831B1 (en) | 2002-11-21 | 2013-03-06 | Novartis AG | 2-(morpholin-4-yl)pyrimidines as phosphotidylinositol (PI) 3-kinase inhibitors and their use in the treatment of cancer |
-
2004
- 2004-09-17 MX MXPA06003207A patent/MXPA06003207A/es unknown
- 2004-09-17 DE DE602004021269T patent/DE602004021269D1/de not_active Expired - Fee Related
- 2004-09-17 CN CNA200480031581XA patent/CN1871009A/zh active Pending
- 2004-09-17 JP JP2006528086A patent/JP2007506746A/ja not_active Withdrawn
- 2004-09-17 BR BRPI0414736-7A patent/BRPI0414736A/pt not_active IP Right Cessation
- 2004-09-17 RU RU2006107578/04A patent/RU2006107578A/ru not_active Application Discontinuation
- 2004-09-17 WO PCT/US2004/030682 patent/WO2005030216A1/en not_active Ceased
- 2004-09-17 EP EP04784529A patent/EP1663241B1/en not_active Expired - Lifetime
- 2004-09-17 CA CA002539235A patent/CA2539235A1/en not_active Abandoned
- 2004-09-17 KR KR1020067005903A patent/KR20060089215A/ko not_active Withdrawn
- 2004-09-17 AT AT04784529T patent/ATE432077T1/de not_active IP Right Cessation
- 2004-09-17 AU AU2004275733A patent/AU2004275733A1/en not_active Withdrawn
- 2004-09-21 TW TW093128501A patent/TW200512198A/zh unknown
- 2004-09-22 PE PE2004000922A patent/PE20050470A1/es not_active Application Discontinuation
- 2004-09-22 SA SA04250303A patent/SA04250303A/ar unknown
- 2004-09-23 GT GT200400188A patent/GT200400188A/es unknown
- 2004-09-23 AR ARP040103441A patent/AR045811A1/es not_active Application Discontinuation
- 2004-09-24 PA PA20048613201A patent/PA8613201A1/es unknown
- 2004-09-24 US US10/950,375 patent/US7524849B2/en not_active Expired - Fee Related
-
2006
- 2006-03-13 IL IL174305A patent/IL174305A0/en unknown
- 2006-03-23 NO NO20061319A patent/NO20061319L/no not_active Application Discontinuation
- 2006-03-23 ZA ZA200602386A patent/ZA200602386B/xx unknown
- 2006-03-24 EC EC2006006457A patent/ECSP066457A/es unknown
- 2006-04-21 CO CO06038135A patent/CO5690592A2/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI0414736A (pt) | 2006-11-21 |
| CA2539235A1 (en) | 2005-04-07 |
| GT200400188A (es) | 2005-05-02 |
| RU2006107578A (ru) | 2007-10-27 |
| IL174305A0 (en) | 2008-02-09 |
| JP2007506746A (ja) | 2007-03-22 |
| EP1663241B1 (en) | 2009-05-27 |
| ECSP066457A (es) | 2006-09-18 |
| DE602004021269D1 (de) | 2009-07-09 |
| ATE432077T1 (de) | 2009-06-15 |
| TW200512198A (en) | 2005-04-01 |
| KR20060089215A (ko) | 2006-08-08 |
| NO20061319L (no) | 2006-04-20 |
| CO5690592A2 (es) | 2006-10-31 |
| AU2004275733A1 (en) | 2005-04-07 |
| US20050075357A1 (en) | 2005-04-07 |
| EP1663241A1 (en) | 2006-06-07 |
| PE20050470A1 (es) | 2005-10-03 |
| MXPA06003207A (es) | 2006-06-23 |
| SA04250303A (ar) | 2005-12-03 |
| CN1871009A (zh) | 2006-11-29 |
| PA8613201A1 (es) | 2005-11-25 |
| US7524849B2 (en) | 2009-04-28 |
| ZA200602386B (en) | 2009-03-25 |
| WO2005030216A1 (en) | 2005-04-07 |
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