CA2792278C - 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses - Google Patents

2,4-pyrimidinediamine compounds and prodrugs thereof and their uses Download PDF

Info

Publication number
CA2792278C
CA2792278C CA2792278A CA2792278A CA2792278C CA 2792278 C CA2792278 C CA 2792278C CA 2792278 A CA2792278 A CA 2792278A CA 2792278 A CA2792278 A CA 2792278A CA 2792278 C CA2792278 C CA 2792278C
Authority
CA
Canada
Prior art keywords
alkyl
fluoro
oxo
pyrimidinediamine
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
Application number
CA2792278A
Other languages
English (en)
French (fr)
Other versions
CA2792278A1 (en
Inventor
Jiaxin Yu
Jeffrey Clough
Rajinder Singh
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Rigel Pharmaceuticals Inc
Original Assignee
Rigel Pharmaceuticals Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Rigel Pharmaceuticals Inc filed Critical Rigel Pharmaceuticals Inc
Publication of CA2792278A1 publication Critical patent/CA2792278A1/en
Application granted granted Critical
Publication of CA2792278C publication Critical patent/CA2792278C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CA2792278A 2010-04-13 2011-04-13 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses Active CA2792278C (en)

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

Publications (2)

Publication Number Publication Date
CA2792278A1 CA2792278A1 (en) 2011-10-20
CA2792278C true CA2792278C (en) 2019-05-14

Family

ID=44583348

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2792278A Active CA2792278C (en) 2010-04-13 2011-04-13 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses

Country Status (6)

Country Link
US (1) US8618095B2 (https=)
EP (1) EP2558474B1 (https=)
JP (2) JP6067550B2 (https=)
CA (1) CA2792278C (https=)
ES (1) ES2562419T3 (https=)
WO (1) WO2011130390A1 (https=)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2792278C (en) * 2010-04-13 2019-05-14 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
PT2736487T (pt) 2011-07-28 2019-02-13 Rigel Pharmaceuticals Inc Novas formulações de (trimetoxifenilamino) pirimidinilo
WO2013020132A1 (en) * 2011-08-04 2013-02-07 The Brigham And Women's Hospital, Inc. Methods of treating cardiovascular and metabolic diseases
ES2704744T3 (es) 2012-06-13 2019-03-19 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
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
MX361157B (es) * 2012-08-30 2018-11-28 Hoffmann La Roche Compuestos inhibidores de pi3k de dioxino- y oxazin-[2,3-d]pirimid ina y métodos de uso.
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
US10130609B2 (en) 2013-03-13 2018-11-20 University Health Network Pyrazole derivatives and their uses thereof
EA035095B1 (ru) 2013-04-19 2020-04-27 Инсайт Холдингс Корпорейшн Бициклические гетероциклы в качестве ингибиторов fgfr
FI3177281T3 (fi) * 2014-08-08 2024-03-13 Ali Res S R L Rasvahappojen ja palmitoyylietanoliamidin seos käytettäväksi tulehduksellisten ja allergisten patologioiden hoitoon
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MX373169B (es) 2015-02-20 2020-04-24 Incyte Holdings Corp Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr).
WO2016134294A1 (en) 2015-02-20 2016-08-25 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
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
MA52493A (fr) 2018-05-04 2021-03-10 Incyte Corp Sels d'un inhibiteur de fgfr
CR20200590A (es) 2018-05-04 2021-04-26 Incyte Corp Formas sólidas de un inhibidor de fgfr y procesos para prepararlas
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
TWI891666B (zh) 2019-10-14 2025-08-01 美商英塞特公司 作為ｆｇｆｒ抑制劑之雙環雜環
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
EP4069696A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2022206797A1 (zh) * 2021-03-30 2022-10-06 贝达药业股份有限公司 Egfr抑制剂及其组合物和用途
TW202304459A (zh) 2021-04-12 2023-02-01 美商英塞特公司 包含ｆｇｆｒ抑制劑及ｎｅｃｔｉｎ－４靶向劑之組合療法
WO2022236255A2 (en) * 2021-05-03 2022-11-10 Nuvation Bio Inc. Heterocyclic compounds as kinase inhibitors
EP4352059A1 (en) 2021-06-09 2024-04-17 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2022261159A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
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)

* Cited by examiner, † Cited by third party
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
ES2445208T3 (es) * 2002-07-29 2014-02-28 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para uso en métodos para tratar o prevenir enfermedades autoinmunitarias
WO2004110368A2 (en) 2003-06-06 2004-12-23 Merck & Co., Inc. Combination therapy for the treatment of hypertension
BRPI0413018B8 (pt) 2003-07-30 2021-05-25 Rigel Pharmaceuticals Inc composto, e, uso de um composto
WO2005013996A2 (en) 2003-08-07 2005-02-17 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
EP1814878B1 (en) * 2004-11-24 2012-01-04 Rigel Pharmaceuticals, Inc. Spiro-2, 4-pyrimidinediamine compounds and their uses
DE602006010979D1 (de) * 2005-01-19 2010-01-21 Rigel Pharmaceuticals Inc Prodrugs aus 2,4-pyrimidindiamin-verbindungen und ihre verwendungen
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
EP2420505A1 (en) 2006-11-21 2012-02-22 Rigel Pharmaceuticals, Inc. Prodrug salts of 2, 4- pyrimidinediamine compounds and their uses
WO2008118823A2 (en) 2007-03-26 2008-10-02 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
TWI546290B (zh) * 2008-06-27 2016-08-21 賽基艾維洛米斯研究股份有限公司 雜芳基化合物及其用途
ES2542884T3 (es) * 2008-09-23 2015-08-12 Rigel Pharmaceuticals, Inc. Inhibidores de JAK de carbamato tricíclico
ES2624622T3 (es) 2008-12-30 2017-07-17 Rigel Pharmaceuticals, Inc. Inhibidores de pirimidindiamina cinasa
ES2524127T3 (es) 2009-11-20 2014-12-04 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidinodiamina y sus profármacos y sus usos
CA2792278C (en) * 2010-04-13 2019-05-14 Rigel Pharmaceuticals, Inc. 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses

Also Published As

Publication number Publication date
US8618095B2 (en) 2013-12-31
CA2792278A1 (en) 2011-10-20
EP2558474A1 (en) 2013-02-20
EP2558474B1 (en) 2015-11-25
JP6067550B2 (ja) 2017-01-25
WO2011130390A1 (en) 2011-10-20
ES2562419T3 (es) 2016-03-04
JP2016041700A (ja) 2016-03-31
JP2013523891A (ja) 2013-06-17
US20110251177A1 (en) 2011-10-13

Similar Documents

Publication Publication Date Title
CA2792278C (en) 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses
CA2780777C (en) 2,4-pyrimidinediamine compounds and prodrugs thereof and their uses
EP3277689B1 (en) Heterocyclic compounds as lsd1 inhibitors
TWI789381B (zh) 雜環化合物
CA2867760C (en) Indolizinyl derivatives as protein kinase c inhibitors and uses thereof
TW202515555A (zh) 作為pi3k抑制劑的苯并吡啶酮及苯并嘧啶酮
EP3392252B1 (en) Pyrimido- pyridazinone compounds and use thereof
US20100316649A1 (en) Small molecule inhibitors of spleen tyrosine kinase (syk)
UA119229C2 (uk) Циклічні ефіри піразол-4-ілгетероциклілкарбоксамідних сполук та способи їх застосування
ES2914686T3 (es) Sales de un inhibidor de Pim quinasa
EP4161927B1 (en) Spiro compounds as melanocortin 4 receptor antagonists and uses thereof
KR20250023362A (ko) Smarca2의 표적화된 분해를 위한 화합물
AU2018297592B2 (en) New substituted azaindoline derivatives as NIK inhibitors
AU2017389818A1 (en) Quinazoline compound and preparation method, application, and pharmaceutical compostion thereof
EP4720038A1 (en) (hetero)aryl-carbonyl-heterobicyclic compounds as inhibitors of pms2 for cancer and degenerative illnesses
WO2023154905A1 (en) Antiviral pyrazolopyridinone compounds
RU2780577C2 (ru) Новые замещенные производные азаиндолина в качестве ингибиторов nik
EA048136B1 (ru) Спиросоединения в качестве антагонистов рецептора меланокортина 4 и их применения

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20160413

MPN Maintenance fee for patent paid

Free format text: FEE DESCRIPTION TEXT: MF (PATENT, 14TH ANNIV.) - STANDARD

Year of fee payment: 14

U00 Fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U00-U101 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE REQUEST RECEIVED

Effective date: 20250404

U11 Full renewal or maintenance fee paid

Free format text: ST27 STATUS EVENT CODE: A-4-4-U10-U11-U102 (AS PROVIDED BY THE NATIONAL OFFICE); EVENT TEXT: MAINTENANCE FEE PAYMENT PAID IN FULL

Effective date: 20250404