JP6067550B2 - 2,4−ピリミジンジアミン化合物およびそのプロドラッグならびにそれらの使用 - Google Patents
2,4−ピリミジンジアミン化合物およびそのプロドラッグならびにそれらの使用 Download PDFInfo
- Publication number
- JP6067550B2 JP6067550B2 JP2013505087A JP2013505087A JP6067550B2 JP 6067550 B2 JP6067550 B2 JP 6067550B2 JP 2013505087 A JP2013505087 A JP 2013505087A JP 2013505087 A JP2013505087 A JP 2013505087A JP 6067550 B2 JP6067550 B2 JP 6067550B2
- Authority
- JP
- Japan
- Prior art keywords
- fluoro
- oxo
- pyrimidinediamine
- pyrido
- dihydro
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
- 0 CC1C*=CC1 Chemical compound CC1C*=CC1 0.000 description 14
- RUKYTDSSQUANDC-VOTSOKGWSA-N C=CC(/C(/N)=C\C=C)P=C Chemical compound C=CC(/C(/N)=C\C=C)P=C RUKYTDSSQUANDC-VOTSOKGWSA-N 0.000 description 1
- PQXAPVOKLYINEI-GVHYBUMESA-N CCC1C[C@H](C)CC1 Chemical compound CCC1C[C@H](C)CC1 PQXAPVOKLYINEI-GVHYBUMESA-N 0.000 description 1
- XWKFPIODWVPXLX-UHFFFAOYSA-N Cc1ccc(C)nc1 Chemical compound Cc1ccc(C)nc1 XWKFPIODWVPXLX-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32369910P | 2010-04-13 | 2010-04-13 | |
| US61/323,699 | 2010-04-13 | ||
| PCT/US2011/032291 WO2011130390A1 (en) | 2010-04-13 | 2011-04-13 | 2, 4-pyrimidinediamine compounds and prodrugs thereof and their uses |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015193022A Division JP2016041700A (ja) | 2010-04-13 | 2015-09-30 | 2,4−ピリミジンジアミン化合物およびそのプロドラッグならびにそれらの使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013523891A JP2013523891A (ja) | 2013-06-17 |
| JP2013523891A5 JP2013523891A5 (enExample) | 2014-05-29 |
| JP6067550B2 true JP6067550B2 (ja) | 2017-01-25 |
Family
ID=44583348
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013505087A Active JP6067550B2 (ja) | 2010-04-13 | 2011-04-13 | 2,4−ピリミジンジアミン化合物およびそのプロドラッグならびにそれらの使用 |
| JP2015193022A Pending JP2016041700A (ja) | 2010-04-13 | 2015-09-30 | 2,4−ピリミジンジアミン化合物およびそのプロドラッグならびにそれらの使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015193022A Pending JP2016041700A (ja) | 2010-04-13 | 2015-09-30 | 2,4−ピリミジンジアミン化合物およびそのプロドラッグならびにそれらの使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US8618095B2 (enExample) |
| EP (1) | EP2558474B1 (enExample) |
| JP (2) | JP6067550B2 (enExample) |
| CA (1) | CA2792278C (enExample) |
| ES (1) | ES2562419T3 (enExample) |
| WO (1) | WO2011130390A1 (enExample) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2562419T3 (es) * | 2010-04-13 | 2016-03-04 | Rigel Pharmaceuticals, Inc. | Compuestos de 2,4-pirimidinodiamina y sus profármacos y sus usos |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| HRP20190186T4 (hr) | 2011-07-28 | 2024-12-20 | Rigel Pharmaceuticals, Inc. | Nove formulacije (trimetoksifenilamino)pirimidinila |
| WO2013020132A1 (en) * | 2011-08-04 | 2013-02-07 | The Brigham And Women's Hospital, Inc. | Methods of treating cardiovascular and metabolic diseases |
| ES2984771T3 (es) | 2012-06-13 | 2024-10-31 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| WO2013189241A1 (zh) * | 2012-06-20 | 2013-12-27 | 上海恒瑞医药有限公司 | 嘧啶二胺类衍生物、其制备方法及其在医药上的应用 |
| CN102746337B (zh) * | 2012-06-21 | 2014-12-17 | 成都苑东药业有限公司 | 一种2,4-嘧啶二胺类化合物及其制备方法 |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| BR112015002493A8 (pt) * | 2012-08-30 | 2019-07-30 | Hoffmann La Roche | composto, composição farmacêutica, processo para a preparação de uma composição farmacêutica, kit e uso de um composto” |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| EP2970138B1 (en) | 2013-03-13 | 2019-01-16 | Canadian Blood Services | Pyrazole derivatives and their uses thereof |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| JP7118642B2 (ja) * | 2014-08-08 | 2022-08-16 | アリ リサーチ ソシエタ ア レスポンサビリタ リミタータ センプリフィカタ | 炎症性およびアレルギー性病変の治療に用いるための脂肪酸とパルミトイルエタノールアミドの混合物 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | 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 |
| EA038045B1 (ru) | 2015-02-20 | 2021-06-28 | Инсайт Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| US11174257B2 (en) | 2018-05-04 | 2021-11-16 | Incyte Corporation | Salts of an FGFR inhibitor |
| RS66310B1 (sr) | 2018-05-04 | 2025-01-31 | Incyte Corp | Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | 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 |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| PH12022550892A1 (en) | 2019-10-14 | 2023-05-03 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| AU2020395185A1 (en) | 2019-12-04 | 2022-06-02 | Incyte Corporation | Derivatives of an FGFR inhibitor |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CN116670127A (zh) * | 2021-03-30 | 2023-08-29 | 贝达药业股份有限公司 | Egfr抑制剂及其组合物和用途 |
| JP2024513575A (ja) | 2021-04-12 | 2024-03-26 | インサイト・コーポレイション | Fgfr阻害剤及びネクチン-4標的化剤を含む併用療法 |
| WO2022236255A2 (en) * | 2021-05-03 | 2022-11-10 | Nuvation Bio Inc. | Heterocyclic compounds as kinase inhibitors |
| WO2022261160A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| TW202313610A (zh) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | 作為fgfr抑制劑之三環雜環 |
| EP4653444A1 (en) * | 2023-01-19 | 2025-11-26 | Hangzhou Innogate Pharma Co., Ltd. | Fused tricyclic compound as kinase inhibitor |
| CN119431398A (zh) * | 2023-07-31 | 2025-02-14 | 中国科学院上海有机化学研究所 | R406及其衍生物协同trail的抗肿瘤应用 |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6573256B2 (en) | 1996-12-30 | 2003-06-03 | Bone Care International, Inc. | Method of inhibiting angiogenesis using active vitamin D analogues |
| FR2785284B1 (fr) | 1998-11-02 | 2000-12-01 | Galderma Res & Dev | Analogues de la vitamine d |
| US6358939B1 (en) | 1999-12-21 | 2002-03-19 | Northern Lights Pharmaceuticals, Llc | Use of biologically active vitamin D compounds for the prevention and treatment of inflammatory bowel disease |
| US6924400B2 (en) | 2001-12-10 | 2005-08-02 | Galderma Research & Development, Snc | Triaromatic vitamin D analogues |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| ATE451104T1 (de) | 2002-07-29 | 2009-12-15 | Rigel Pharmaceuticals Inc | Verfahren zur behandlung oder pruvention von autoimmunkrankheiten mit 2,4-pyrimidindiamin- verbindungen |
| US20060160834A1 (en) | 2003-06-06 | 2006-07-20 | Fong Tung M | Combination therapy for the treatment of hypertension |
| ES2421139T3 (es) | 2003-07-30 | 2013-08-29 | Rigel Pharmaceuticals, Inc. | Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias |
| EP1663242B1 (en) | 2003-08-07 | 2011-04-27 | Rigel Pharmaceuticals, Inc. | 2,4-pyrimidinediamine compounds and uses as anti-proliferative agents |
| US20070092888A1 (en) | 2003-09-23 | 2007-04-26 | Cornelius Diamond | Diagnostic markers of hypertension and methods of use thereof |
| WO2006068770A1 (en) * | 2004-11-24 | 2006-06-29 | Rigel Pharmaceuticals, Inc. | Spiro-2, 4-pyrimidinediamine compounds and their uses |
| EP2161275A1 (en) | 2005-01-19 | 2010-03-10 | Rigel Pharmaceuticals, Inc. | Prodrugs of 2,4-pyrimidinediamine compounds and their uses |
| US8227455B2 (en) | 2005-04-18 | 2012-07-24 | Rigel Pharmaceuticals, Inc. | Methods of treating cell proliferative disorders |
| US7713987B2 (en) | 2005-12-06 | 2010-05-11 | Rigel Pharmaceuticals, Inc. | Pyrimidine-2,4-diamines and their uses |
| US8163902B2 (en) | 2006-11-21 | 2012-04-24 | Rigel Pharmaceuticals, Inc. | Prodrugs of 2,4-pyrimidinediamine compounds and their uses |
| US7834024B2 (en) * | 2007-03-26 | 2010-11-16 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
| US20090012045A1 (en) * | 2007-06-26 | 2009-01-08 | Rigel Pharmaceuticals, Inc. | Methods of Treating Cell Proliferative Disorders |
| TWI458721B (zh) * | 2008-06-27 | 2014-11-01 | Celgene Avilomics Res Inc | 雜芳基化合物及其用途 |
| CA2736258C (en) * | 2008-09-23 | 2016-11-29 | Rigel Pharmaceuticals, Inc. | Tricyclic carbamate jak inhibitors |
| WO2010078369A2 (en) * | 2008-12-30 | 2010-07-08 | Rigel Pharmaceuticals, Inc. | Pyrimidinediamine kinase inhibitors |
| WO2011063241A1 (en) * | 2009-11-20 | 2011-05-26 | Rigel Pharmaceuticals, Inc. | 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses |
| ES2562419T3 (es) * | 2010-04-13 | 2016-03-04 | Rigel Pharmaceuticals, Inc. | Compuestos de 2,4-pirimidinodiamina y sus profármacos y sus usos |
-
2011
- 2011-04-13 ES ES11730116.8T patent/ES2562419T3/es active Active
- 2011-04-13 CA CA2792278A patent/CA2792278C/en active Active
- 2011-04-13 US US13/086,081 patent/US8618095B2/en active Active
- 2011-04-13 WO PCT/US2011/032291 patent/WO2011130390A1/en not_active Ceased
- 2011-04-13 JP JP2013505087A patent/JP6067550B2/ja active Active
- 2011-04-13 EP EP11730116.8A patent/EP2558474B1/en active Active
-
2015
- 2015-09-30 JP JP2015193022A patent/JP2016041700A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CA2792278A1 (en) | 2011-10-20 |
| EP2558474B1 (en) | 2015-11-25 |
| US20110251177A1 (en) | 2011-10-13 |
| US8618095B2 (en) | 2013-12-31 |
| ES2562419T3 (es) | 2016-03-04 |
| WO2011130390A1 (en) | 2011-10-20 |
| CA2792278C (en) | 2019-05-14 |
| EP2558474A1 (en) | 2013-02-20 |
| JP2016041700A (ja) | 2016-03-31 |
| JP2013523891A (ja) | 2013-06-17 |
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