AR040971A1 - Compuestos pirimido que tienen actividad antiproliferativa - Google Patents
Compuestos pirimido que tienen actividad antiproliferativaInfo
- Publication number
- AR040971A1 AR040971A1 ARP030102914A ARP030102914A AR040971A1 AR 040971 A1 AR040971 A1 AR 040971A1 AR P030102914 A ARP030102914 A AR P030102914A AR P030102914 A ARP030102914 A AR P030102914A AR 040971 A1 AR040971 A1 AR 040971A1
- Authority
- AR
- Argentina
- Prior art keywords
- compounds
- alkyl
- independently selected
- nr5r6
- atoms
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 230000001028 anti-proliverative effect Effects 0.000 title abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 208000026310 Breast neoplasm Diseases 0.000 abstract 1
- 108091008794 FGF receptors Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 229940124639 Selective inhibitor Drugs 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 210000000481 breast Anatomy 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 210000001072 colon Anatomy 0.000 abstract 1
- 208000029742 colonic neoplasm Diseases 0.000 abstract 1
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 210000004072 lung Anatomy 0.000 abstract 1
- 208000037841 lung tumor Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000023958 prostate neoplasm Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Se presentan compuestos que son inhibidores selectivos de ambas KDR y FGFR quinasas y son selectivas contra LCK. Estos compuestos y sus sales farmacéuticamente aceptables son agentes antiproliferativos útiles en el tratamiento o control de tumores sólidos, en particular tumores de mama, colon, pulmón y próstata. También se revelan composiciones farmacéuticas que contienen estos compuestos y un proceso para su preparación. Reivindicación 1: Un compuesto de fórmula (1) o sales farmacéuticamente aceptables del mismo, en donde R1 se selecciona del grupo, -H, -COR4, y -COOCHR5OCOR4; R2 y R3 se seleccionan independientemente de -H, y -OR5; R4 se selecciona del grupo -C1-6 alquilo; C1-6 alquilo sustituido por hasta 4 grupos seleccionados independientemente de -NR5R6, -SR5, -OR5, arilo, arilo sustituido por hasta 2 grupos seleccionados independientemente de -OR5 y C1-4 alquilo, y heteroarilo, y heterociclo; R5 y R6 se seleccionan independientemente de -H y C1-5 alquilo, o, alternativamente, -NR5R6 puede formar un anillo que tiene de 3 a 7 átomos, dicho anillo que incluye opcionalmente uno o más átomos de O o N adicionales.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US40351902P | 2002-08-14 | 2002-08-14 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR040971A1 true AR040971A1 (es) | 2005-04-27 |
Family
ID=31946709
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030102914A AR040971A1 (es) | 2002-08-14 | 2003-08-12 | Compuestos pirimido que tienen actividad antiproliferativa |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US7084270B2 (es) |
| EP (1) | EP1556384B1 (es) |
| JP (1) | JP2005538141A (es) |
| KR (1) | KR20070087687A (es) |
| CN (1) | CN1323080C (es) |
| AR (1) | AR040971A1 (es) |
| AT (1) | ATE386743T1 (es) |
| AU (1) | AU2003255389A1 (es) |
| BR (1) | BR0313732A (es) |
| CA (1) | CA2494127A1 (es) |
| DE (1) | DE60319255T2 (es) |
| ES (1) | ES2300644T3 (es) |
| MX (1) | MXPA05001629A (es) |
| PA (1) | PA8580001A1 (es) |
| PL (1) | PL375588A1 (es) |
| RU (1) | RU2336275C2 (es) |
| TW (1) | TW200407326A (es) |
| UY (1) | UY27937A1 (es) |
| WO (1) | WO2004018472A2 (es) |
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006024487A1 (en) | 2004-08-31 | 2006-03-09 | F. Hoffmann-La Roche Ag | AMIDE DERIVATIVES OF 7-AMINO-3-PHENYL-DIHYDROPYRIMIDO [4,5-d]PYRIMIDINONES, THEIR MANUFACTURE AND USE AS PHARMACEUTICAL AGENTS |
| DE602005013248D1 (de) | 2004-08-31 | 2009-04-23 | Hoffmann La Roche | Amidderivate von 3-phenyldihydropyrimidoä4,5-düpyrimidinonen, deren herstellung und verwendung als pharmazeutische mittel |
| US20120189641A1 (en) | 2009-02-25 | 2012-07-26 | OSI Pharmaceuticals, LLC | Combination anti-cancer therapy |
| US8465912B2 (en) | 2009-02-27 | 2013-06-18 | OSI Pharmaceuticals, LLC | Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation |
| WO2010099138A2 (en) | 2009-02-27 | 2010-09-02 | Osi Pharmaceuticals, Inc. | Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation |
| EP2401614A1 (en) | 2009-02-27 | 2012-01-04 | OSI Pharmaceuticals, LLC | Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| US9896730B2 (en) | 2011-04-25 | 2018-02-20 | OSI Pharmaceuticals, LLC | Use of EMT gene signatures in cancer drug discovery, diagnostics, and treatment |
| CN102816162B (zh) * | 2011-06-10 | 2016-04-27 | 中国科学院广州生物医药与健康研究院 | 嘧啶并嘧啶酮类化合物及其药用组合物和应用 |
| WO2013152252A1 (en) | 2012-04-06 | 2013-10-10 | OSI Pharmaceuticals, LLC | Combination anti-cancer therapy |
| CN107652289B (zh) | 2012-06-13 | 2020-07-21 | 因塞特控股公司 | 作为fgfr抑制剂的取代的三环化合物 |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| CN104968664A (zh) * | 2012-12-12 | 2015-10-07 | 山东亨利医药科技有限责任公司 | 作为酪氨酸激酶抑制剂的并环化合物 |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| EA036160B1 (ru) | 2013-03-15 | 2020-10-08 | Селджен Кар Ллс | Гетероарильные соединения и их применение |
| KR102350704B1 (ko) | 2013-03-15 | 2022-01-13 | 셀젠 카르 엘엘씨 | 헤테로아릴 화합물 및 이의 용도 |
| AR095464A1 (es) | 2013-03-15 | 2015-10-21 | Celgene Avilomics Res Inc | Compuestos de heteroarilo y usos de los mismos |
| JP6449244B2 (ja) | 2013-04-19 | 2019-01-09 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｆｇｆｒ抑制剤としての二環式複素環 |
| CN104418860B (zh) * | 2013-08-20 | 2016-09-07 | 中国科学院广州生物医药与健康研究院 | 嘧啶并杂环类化合物及其药用组合物和应用 |
| US10287268B2 (en) | 2014-07-21 | 2019-05-14 | Dana-Farber Cancer Institute, Inc. | Imidazolyl kinase inhibitors and uses thereof |
| DK3172213T3 (da) | 2014-07-21 | 2021-12-13 | Dana Farber Cancer Inst Inc | Makrocykliske kinasehæmmere og anvendelser deraf |
| WO2016023014A2 (en) | 2014-08-08 | 2016-02-11 | Dana-Farber Cancer Institute, Inc. | Uses of salt-inducible kinase (sik) inhibitors |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016134320A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US10954242B2 (en) | 2016-07-05 | 2021-03-23 | The Broad Institute, Inc. | Bicyclic urea kinase inhibitors and uses thereof |
| US11241435B2 (en) | 2016-09-16 | 2022-02-08 | The General Hospital Corporation | Uses of salt-inducible kinase (SIK) inhibitors for treating osteoporosis |
| BR112019017741A2 (pt) * | 2017-02-28 | 2020-04-07 | Dana Farber Cancer Inst Inc | usos de pirimidopirimidinonas como inibidores de sik |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| SG11202010882XA (en) | 2018-05-04 | 2020-11-27 | Incyte Corp | Salts of an fgfr inhibitor |
| DK3788047T3 (da) | 2018-05-04 | 2024-09-16 | Incyte Corp | Faste former af en FGFR-inhibitor og fremgangsmåder til fremstilling deraf |
| CN113474347A (zh) * | 2018-12-27 | 2021-10-01 | 法国施维雅药厂 | Mat2a的aza杂双环抑制剂和用于治疗癌症的方法 |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| MX2022004513A (es) | 2019-10-14 | 2022-07-19 | Incyte Corp | Heterociclos biciclicos como inhibidores de los receptores del factor de crecimiento de fibroblastos (fgfr). |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| JP2023505258A (ja) | 2019-12-04 | 2023-02-08 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤としての三環式複素環 |
| BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2949466A (en) | 1958-03-04 | 1960-08-16 | Parke Davis & Co | Pyrimidine compounds and means of producing the same |
| ES338687A1 (es) | 1966-04-06 | 1968-04-01 | Monsanto Co | Procedimiento para obtener composiciones de fluidos funcio-nales. |
| US4425346A (en) | 1980-08-01 | 1984-01-10 | Smith And Nephew Associated Companies Limited | Pharmaceutical compositions |
| JPS60226882A (ja) | 1984-04-24 | 1985-11-12 | Nippon Zoki Pharmaceut Co Ltd | 新規ピリミドピリミジン誘導体 |
| WO1998024432A2 (en) | 1996-12-05 | 1998-06-11 | Sugen, Inc. | Use of indolinone compounds as modulators of protein kinases |
| BR9911590A (pt) | 1998-05-26 | 2001-02-13 | Warner Lambert Co | Pirimidinas bicìclicas e 3,4-diidropirimidinas bicìclicas como inibidores da proliferação celular |
| CZ20011394A3 (cs) | 1998-10-23 | 2001-12-12 | F. Hoffmann-La Roche Ag | Derivát bicyklických, dusík obsahujících heterocyklických sloučenin, způsob jeho přípravy a farmaceutický prostředek, který ho obsahuje |
| TR200201058T2 (tr) | 1999-10-21 | 2002-07-22 | F.Hoffmann-La Roche Ag | P38 protein kinaz inhibitörleri olarak, alkilaminoyla ornatılmış bisiklik, azotlu heterosikller |
| JP3961830B2 (ja) | 1999-10-21 | 2007-08-22 | エフ．ホフマン−ラ ロシュ アーゲー | ｐ３８プロテインキナーゼのインヒビターとしてのヘテロアルキルアミノ置換二環式窒素複素環 |
| AR030053A1 (es) | 2000-03-02 | 2003-08-13 | Smithkline Beecham Corp | 1h-pirimido [4,5-d] pirimidin-2-onas y sales, composiciones farmaceuticas, uso para la fabricacion de un medicamento y procedimiento para producirlas |
| CN1275964C (zh) | 2000-08-31 | 2006-09-20 | 霍夫曼-拉罗奇有限公司 | 作为细胞增殖抑制剂的7－氧代吡啶并嘧啶 |
| PA8577501A1 (es) | 2002-07-25 | 2004-02-07 | Warner Lambert Co | Inhibidores de quinasas |
-
2003
- 2003-07-21 US US10/623,972 patent/US7084270B2/en not_active Expired - Fee Related
- 2003-08-07 BR BR0313732-5A patent/BR0313732A/pt not_active IP Right Cessation
- 2003-08-07 RU RU2005107314/04A patent/RU2336275C2/ru not_active IP Right Cessation
- 2003-08-07 PL PL03375588A patent/PL375588A1/xx not_active Application Discontinuation
- 2003-08-07 AT AT03792269T patent/ATE386743T1/de not_active IP Right Cessation
- 2003-08-07 DE DE60319255T patent/DE60319255T2/de not_active Expired - Fee Related
- 2003-08-07 AU AU2003255389A patent/AU2003255389A1/en not_active Abandoned
- 2003-08-07 CN CNB038191601A patent/CN1323080C/zh not_active Expired - Fee Related
- 2003-08-07 MX MXPA05001629A patent/MXPA05001629A/es active IP Right Grant
- 2003-08-07 KR KR1020077017079A patent/KR20070087687A/ko not_active Application Discontinuation
- 2003-08-07 EP EP03792269A patent/EP1556384B1/en not_active Expired - Lifetime
- 2003-08-07 WO PCT/EP2003/008744 patent/WO2004018472A2/en active IP Right Grant
- 2003-08-07 CA CA002494127A patent/CA2494127A1/en not_active Abandoned
- 2003-08-07 ES ES03792269T patent/ES2300644T3/es not_active Expired - Lifetime
- 2003-08-07 JP JP2004530098A patent/JP2005538141A/ja active Pending
- 2003-08-11 PA PA20038580001A patent/PA8580001A1/es unknown
- 2003-08-12 UY UY27937A patent/UY27937A1/es not_active Application Discontinuation
- 2003-08-12 AR ARP030102914A patent/AR040971A1/es not_active Application Discontinuation
- 2003-08-13 TW TW092122274A patent/TW200407326A/zh unknown
Also Published As
| Publication number | Publication date |
|---|---|
| BR0313732A (pt) | 2005-09-27 |
| ES2300644T3 (es) | 2008-06-16 |
| ATE386743T1 (de) | 2008-03-15 |
| AU2003255389A1 (en) | 2004-03-11 |
| PL375588A1 (en) | 2005-11-28 |
| WO2004018472A3 (en) | 2004-04-29 |
| CA2494127A1 (en) | 2004-03-04 |
| TW200407326A (en) | 2004-05-16 |
| DE60319255T2 (de) | 2009-03-05 |
| US20040038995A1 (en) | 2004-02-26 |
| JP2005538141A (ja) | 2005-12-15 |
| RU2336275C2 (ru) | 2008-10-20 |
| CN1675214A (zh) | 2005-09-28 |
| WO2004018472A2 (en) | 2004-03-04 |
| DE60319255D1 (de) | 2008-04-03 |
| UY27937A1 (es) | 2004-02-27 |
| MXPA05001629A (es) | 2005-04-25 |
| US7084270B2 (en) | 2006-08-01 |
| EP1556384A2 (en) | 2005-07-27 |
| CN1323080C (zh) | 2007-06-27 |
| KR20070087687A (ko) | 2007-08-28 |
| RU2005107314A (ru) | 2005-11-20 |
| EP1556384B1 (en) | 2008-02-20 |
| PA8580001A1 (es) | 2004-03-10 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |