[go: up one dir, main page]

PE20060398A1 - Compuestos derivados de pirimidina como inhibidores de quinasa de proteina - Google Patents

Compuestos derivados de pirimidina como inhibidores de quinasa de proteina

Info

Publication number
PE20060398A1
PE20060398A1 PE2005000667A PE2005000667A PE20060398A1 PE 20060398 A1 PE20060398 A1 PE 20060398A1 PE 2005000667 A PE2005000667 A PE 2005000667A PE 2005000667 A PE2005000667 A PE 2005000667A PE 20060398 A1 PE20060398 A1 PE 20060398A1
Authority
PE
Peru
Prior art keywords
methyl
phenyl
alkyl
benzamide
imidazol
Prior art date
Application number
PE2005000667A
Other languages
English (en)
Inventor
Pamela A Albaugh
Greg Chopiuk
Nathanael Schiander Gray
Taebo Sim
Shuli You
Qiong Zhang
Guobao Zhang
Xia Wang
Pingda Ren
Qiang Ding
Original Assignee
Irm Llc
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 Irm Llc filed Critical Irm Llc
Publication of PE20060398A1 publication Critical patent/PE20060398A1/es

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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • 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
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • 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
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D405/14—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 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
    • C07D417/14—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 three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Dermatology (AREA)
  • Vascular Medicine (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)

Abstract

REFERIDA A UN COMPUESTO DE FORMULA I, DONDE m Y n SON 0, 1 O 2; R1 ES -XOR5, -XNR5R6, -XR5, ENTRE OTROS; R5 ES H, ALQUILO C1-C6, ARILO C1-C6, ENTRE OTROS; R6 ES H, ALQUILO C1-C6, ENTRE OTROS; R2 Y R4 SON HALOGENO, OH, ALQUILO C1-C4, ENTRE OTROS; R3 ES NR10R11, NR10C(O)R11, ENTRE OTROS; R10 ES H Y ALQUILO C1-C6; R11 ES ARILO C6-C10, CICLOALQUILO C3-C10, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: N[4-METIL-3-(1-{6-[4-(2-MORFOLIN-4-IL-ETIL)-FENIL-AMINO]-PIRIMIDIN-4-IL}-1H-IMIDAZOL-2-ILAMINO)-FENIL]-3-TRIFLUORO-METIL-BENZAMIDA, N-{3-[1-(6-CICLOPROPIL-AMINO-PIRIMIDIN-4-IL)-1H-IMIDAZOL-2-ILAMINO]-4-METIL-FENIL}-3-(4-ETIL-PIPERAZIN-1-IL)-5-TRIFLUORO-METIL-BENZAMIDA, N-(4-METIL-3-{1-[6-(2-MORFOLIN-4-IL-ETIL-AMINO)-PIRIMIDIN-4-IL]-1H-IMIDAZOL-2-ILAMINO}-FENIL)-3-TRIFLUORO-METIL-BENZAMIDA, ENTRE OTROS. TAMBIEN ESTA REFERIDA A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON UTILES EN EL TRATAMIENTO DE ENFERMEDADES O DESORDENES QUE INVOLUCREN LA ACTIVACION ANORMAL DE LAS QUINASAS Abl, BCR-Abl, PDGF-R, trkB, c-SRC, BMX, FGFR3, b-RAF, SGK, Tie2, Lck, JNK2a2, MKK4, c-RAF, MKK6, SAPKa Y SAPK2b
PE2005000667A 2004-06-10 2005-06-10 Compuestos derivados de pirimidina como inhibidores de quinasa de proteina PE20060398A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US57849104P 2004-06-10 2004-06-10

Publications (1)

Publication Number Publication Date
PE20060398A1 true PE20060398A1 (es) 2006-06-05

Family

ID=35509612

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2005000667A PE20060398A1 (es) 2004-06-10 2005-06-10 Compuestos derivados de pirimidina como inhibidores de quinasa de proteina

Country Status (21)

Country Link
US (1) US7745437B2 (es)
EP (1) EP1758892B1 (es)
JP (1) JP4688876B2 (es)
CN (1) CN1960988B (es)
AR (1) AR049511A1 (es)
AU (1) AU2005254982B2 (es)
BR (1) BRPI0511978A (es)
CA (1) CA2567662C (es)
EC (1) ECSP067070A (es)
ES (1) ES2396135T3 (es)
IL (1) IL179613A0 (es)
MA (1) MA28679B1 (es)
MX (1) MXPA06014247A (es)
MY (1) MY144044A (es)
NO (1) NO20070160L (es)
PE (1) PE20060398A1 (es)
RU (1) RU2401265C2 (es)
TN (1) TNSN06406A1 (es)
TW (1) TW200610762A (es)
WO (1) WO2005123719A1 (es)
ZA (1) ZA200609450B (es)

Families Citing this family (124)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR045047A1 (es) * 2003-07-11 2005-10-12 Arena Pharm Inc Derivados arilo y heteroarilo trisustituidos como moduladores del metabolismo y de la profilaxis y tratamiento de desordenes relacionados con los mismos
TW200533357A (en) 2004-01-08 2005-10-16 Millennium Pharm Inc 2-(amino-substituted)-4-aryl pyrimidines and related compounds useful for treating inflammatory diseases
US20080194606A1 (en) * 2005-05-05 2008-08-14 Astrazeneca Pyrazolyl-Amino-Substituted Pyrimidines and Their Use in the Treatment of Cancer
ES2401482T3 (es) 2005-05-10 2013-04-22 Incyte Corporation Moduladores de la indolamina 2,3-dioxigenasa y métodos de uso de los mismos
SI2426129T1 (sl) 2005-12-13 2017-02-28 Incyte Holdings Corporation Heteroarilno substituirani pirolo(2,3-b)piridini in pirolo(2,3-b)pirimidini kot zaviralci janusove kinaze
EP2007391B8 (en) * 2006-04-07 2013-05-29 Novartis AG Combination comprising a) a pyrimidylaminobenzamide compound, and b) a thr315ile kinase inhibitor
JP5325783B2 (ja) 2006-09-08 2013-10-23 エフ．ホフマン−ラ ロシュ アーゲー ベンゾトリアゾールキナーゼモジュレーター
DK2068938T3 (da) 2006-09-22 2011-04-04 Novartis Ag Optimering af behandlingen af Philadelphia-positiv leukæmi med ABL-tyrosinkinaseinhibitor imatinib
KR101101675B1 (ko) 2006-10-02 2011-12-30 노파르티스 아게 단백질 키나제 억제제로서의 화합물 및 조성물
JP2010512405A (ja) * 2006-12-11 2010-04-22 アイアールエム・リミテッド・ライアビリティ・カンパニー キナーゼ阻害剤としての化合物および組成物
MX342814B (es) 2007-06-13 2016-10-13 Incyte Holdings Corp Sales de inhibidor de janus cinasa (r)-3-(4-7h-pirrolo[2,3-d]pirim idin-4-il)-1h-pirazol-1-il)-3-ciclopentilpropanitrilo.
BRPI0908637B8 (pt) 2008-05-21 2021-05-25 Ariad Pharma Inc composto e composição farmacêutica do mesmo
US9273077B2 (en) 2008-05-21 2016-03-01 Ariad Pharmaceuticals, Inc. Phosphorus derivatives as kinase inhibitors
EP2307456B1 (en) 2008-06-27 2014-10-15 Amgen Inc. Ang-2 inhibition to treat multiple sclerosis
HRP20141094T1 (hr) 2008-07-08 2015-01-16 Incyte Corporation 1,2,5-oksadiazoli kao inhibitori indolamin 2,3-dioksigenaze
WO2010100127A1 (en) * 2009-03-04 2010-09-10 Novartis Ag Disubstituted imidazole derivatives as modulators of raf kinase
CN102458581B (zh) 2009-05-22 2016-03-30 因塞特控股公司 作为JANUS激酶抑制剂的吡唑-4-基-吡咯并[2，3-d]嘧啶和吡咯-3-基-吡咯并[2，3-d]嘧啶的N-(杂)芳基-吡咯烷衍生物
HUE046493T2 (hu) 2009-05-22 2020-03-30 Incyte Holdings Corp 3-[4-(7H-Pirrolo[2,3-d]pirimidin-4-il)-lH-pirazol-l-il]oktán- vagy heptán-nitril JAK inhibitorokként
JP6073677B2 (ja) 2009-06-12 2017-02-01 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド 縮合複素環式化合物およびそれらの使用
AR077975A1 (es) 2009-08-28 2011-10-05 Irm Llc Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina
WO2011028685A1 (en) 2009-09-01 2011-03-10 Incyte Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EP2937345B1 (en) 2009-12-29 2018-03-21 Dana-Farber Cancer Institute, Inc. Type ii raf kinase inhibitors
MX2012009541A (es) 2010-02-18 2012-10-01 Incyte Corp Derivados de ciclobutano y metilciclobutano como inhibidores de janus cinasa.
RS57219B1 (sr) 2010-03-10 2018-07-31 Incyte Holdings Corp Piperidin-4-il azetidin derivati kao inhibitori jak1
EP3087972A1 (en) 2010-05-21 2016-11-02 Incyte Holdings Corporation Topical formulation for a jak inhibitor
JP2012102090A (ja) * 2010-10-15 2012-05-31 Sumitomo Chemical Co Ltd ピリミジン化合物およびその有害生物防除用途
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
SG190839A1 (en) 2010-11-19 2013-07-31 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
AU2012250517B2 (en) 2011-05-04 2016-05-19 Takeda Pharmaceutical Company Limited Compounds for inhibiting cell proliferation in EGFR-driven cancers
RU2477723C2 (ru) 2011-06-16 2013-03-20 Общество С Ограниченной Ответственностью "Фьюжн Фарма" Ингибиторы протеинкиназ (варианты), их применение для лечения онкологических заболеваний и фармацевтическая композиция на их основе
PH12013502612A1 (en) 2011-06-20 2014-04-28 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
CA2855243C (en) 2011-11-11 2020-04-14 Novartis Ag Method of treating a proliferative disease
JP6106685B2 (ja) 2011-11-17 2017-04-05 ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド Ｃ−ｊｕｎ−ｎ−末端キナーゼ（ｊｎｋ）の阻害剤
PT2782557T (pt) 2011-11-23 2018-11-26 Array Biopharma Inc Formulações farmacêuticas
GB201204384D0 (en) 2012-03-13 2012-04-25 Univ Dundee Anti-flammatory agents
WO2013169401A1 (en) 2012-05-05 2013-11-14 Ariad Pharmaceuticals, Inc. Compounds for inhibiting cell proliferation in egfr-driven cancers
WO2013173720A1 (en) 2012-05-18 2013-11-21 Incyte Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
UA125503C2 (uk) 2012-06-13 2022-04-13 Інсайт Холдинґс Корпорейшн Заміщені трициклічні сполуки як інгібітори fgfr
EP2902489B9 (en) * 2012-09-27 2018-02-07 Chugai Seiyaku Kabushiki Kaisha Fgfr3 fusion gene and pharmaceutical drug targeting same
US10112927B2 (en) 2012-10-18 2018-10-30 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
WO2014063054A1 (en) 2012-10-19 2014-04-24 Dana-Farber Cancer Institute, Inc. Bone marrow on x chromosome kinase (bmx) inhibitors and uses thereof
US9758522B2 (en) 2012-10-19 2017-09-12 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged small molecules as inducers of protein degradation
TWI646099B (zh) 2012-11-01 2019-01-01 英塞特控股公司 作爲ｊａｋ抑制劑之三環稠合噻吩衍生物
TW202228704A (zh) 2012-11-15 2022-08-01 美商英塞特控股公司 盧梭利替尼之緩釋性劑型
TWI687220B (zh) 2013-03-01 2020-03-11 美商英塞特控股公司 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途
BR122021015061B1 (pt) 2013-03-06 2022-10-18 Incyte Holdings Corporation Processos e intermediários para preparar um inibidor de jak
US9611283B1 (en) 2013-04-10 2017-04-04 Ariad Pharmaceuticals, Inc. Methods for inhibiting cell proliferation in ALK-driven cancers
WO2014172644A2 (en) 2013-04-19 2014-10-23 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
DK3030227T3 (da) 2013-08-07 2020-04-20 Incyte Corp Vedvarende frigivelses-doseringsformer for en jak1-inhibitor
EP3057956B1 (en) 2013-10-18 2021-05-05 Dana-Farber Cancer Institute, Inc. Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7)
CA2927917C (en) 2013-10-18 2022-08-09 Syros Pharmaceuticals, Inc. Heteroaromatic compounds useful for the treatment of proliferative diseases
WO2015164614A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Janus kinase inhibitors and uses thereof
WO2015164604A1 (en) 2014-04-23 2015-10-29 Dana-Farber Cancer Institute, Inc. Hydrophobically tagged janus kinase inhibitors and uses thereof
PE20170300A1 (es) 2014-04-30 2017-04-19 Incyte Corp Procesos para preparar un inhibidor de jak 1 y nuevas formas de este
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
DK3172213T3 (da) 2014-07-21 2021-12-13 Dana Farber Cancer Inst Inc Makrocykliske kinasehæmmere og anvendelser deraf
CA2954186A1 (en) * 2014-07-21 2016-01-28 Dana-Farber Cancer Institute, Inc. Imidazolyl kinase inhibitors and uses thereof
CA2955082A1 (en) 2014-08-08 2016-02-11 Dana-Farber Cancer Institute, Inc. Uses of salt-inducible kinase (sik) inhibitors
US10870651B2 (en) 2014-12-23 2020-12-22 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinase 7 (CDK7)
UA121669C2 (uk) 2015-02-20 2020-07-10 Інсайт Корпорейшн Біциклічні гетероцикли як інгібітори fgfr
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
AU2016243529B2 (en) 2015-03-27 2021-03-25 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
WO2016201370A1 (en) 2015-06-12 2016-12-15 Dana-Farber Cancer Institute, Inc. Combination therapy of transcription inhibitors and kinase inhibitors
EP4019515A1 (en) 2015-09-09 2022-06-29 Dana-Farber Cancer Institute, Inc. Inhibitors of cyclin-dependent kinases
KR101894096B1 (ko) * 2016-01-29 2018-09-05 삼진제약주식회사 Jnk 저해 활성을 갖는 신규한 이미다졸 유도체 및 이의 용도
CA3015417A1 (en) 2016-03-01 2017-09-08 Propellon Therapeutics Inc. Inhibitors of wdr5 protein-protein binding
DK3423451T3 (da) 2016-03-01 2022-11-28 Propellon Therapeutics Inc Inhibitorer af wdr5-protein-proteinbinding
KR20190075043A (ko) 2016-07-05 2019-06-28 더 브로드 인스티튜트, 인코퍼레이티드 비시클릭 우레아 키나제 억제제 및 그의 용도
US11241435B2 (en) 2016-09-16 2022-02-08 The General Hospital Corporation Uses of salt-inducible kinase (SIK) inhibitors for treating osteoporosis
AU2018226771B2 (en) 2017-02-28 2023-11-23 Dana-Farber Cancer Institute, Inc. Uses of pyrimidopyrimidinones as SIK inhibitors
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
SMT202100656T1 (it) 2017-10-18 2022-01-10 Incyte Corp Derivati di imidazolo condensati sostituiti con gruppi ossidrile terziari come inibitori di pi3k-gamma
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
US11306079B2 (en) 2017-12-21 2022-04-19 Incyte Corporation 3-(5-amino-pyrazin-2-yl)-benzenesulfonamide derivatives and related compounds as PI3K-gamma kinase inhibitors
CA3089832A1 (en) 2018-01-30 2019-08-08 Incyte Corporation Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
SMT202200134T1 (it) 2018-03-08 2022-05-12 Incyte Corp Composti di amminopirazindiolo come inibitori di pi3k-y
IL318069A (en) 2018-03-30 2025-02-01 Incyte Corp Using JAK inhibitors to treat hidradenitis suppurativa
US11220510B2 (en) 2018-04-09 2022-01-11 Incyte Corporation Pyrrole tricyclic compounds as A2A / A2B inhibitors
CN112566912A (zh) 2018-05-04 2021-03-26 因赛特公司 Fgfr抑制剂的盐
SI3788047T1 (sl) 2018-05-04 2024-11-29 Incyte Corporation Trdne oblike inhibitorja fgfr in postopki priprave le-teh
MX2020012376A (es) 2018-05-18 2021-03-09 Incyte Corp Derivados de pirimidina fusionados como inhibidores de los receptores de adenosina a2a/a2b.
MA52761A (fr) 2018-06-01 2021-04-14 Incyte Corp Schéma posologique destiné au traitement de troubles liés à la pi3k
WO2020005807A1 (en) 2018-06-25 2020-01-02 Dana-Farber Cancer Institute, Inc. Taire family kinase inhibitors and uses thereof
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
IL279829B2 (en) 2018-07-05 2025-05-01 Incyte Holdings Corp Fused pyrazine derivatives as A2A/A2B inhibitors
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
US11161838B2 (en) 2018-11-13 2021-11-02 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
US11078204B2 (en) 2018-11-13 2021-08-03 Incyte Corporation Heterocyclic derivatives as PI3K inhibitors
US11396502B2 (en) 2018-11-13 2022-07-26 Incyte Corporation Substituted heterocyclic derivatives as PI3K inhibitors
US11596692B1 (en) 2018-11-21 2023-03-07 Incyte Corporation PD-L1/STING conjugates and methods of use
JP7660063B2 (ja) 2018-12-28 2025-04-10 ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド サイクリン依存性キナーゼ７のインヒビターおよびそれらの使用
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
WO2020168197A1 (en) 2019-02-15 2020-08-20 Incyte Corporation Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors
WO2020180959A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as cdk2 inhibitors
WO2020185532A1 (en) 2019-03-08 2020-09-17 Incyte Corporation Methods of treating cancer with an fgfr inhibitor
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2020223469A1 (en) 2019-05-01 2020-11-05 Incyte Corporation N-(1-(methylsulfonyl)piperidin-4-yl)-4,5-di hydro-1h-imidazo[4,5-h]quinazolin-8-amine derivatives and related compounds as cyclin-dependent kinase 2 (cdk2) inhibitors for treating cancer
US11591329B2 (en) 2019-07-09 2023-02-28 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CA3150681A1 (en) 2019-08-14 2021-02-18 Incyte Corporation Imidazolyl pyrimidinylamine compounds as cdk2 inhibitors
US12122767B2 (en) 2019-10-01 2024-10-22 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CR20220170A (es) 2019-10-11 2022-10-10 Incyte Corp Aminas bicíclicas como inhibidoras de la cdk2
EP4045151A1 (en) 2019-10-14 2022-08-24 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
US11992490B2 (en) 2019-10-16 2024-05-28 Incyte Corporation Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
EP4069695A1 (en) 2019-12-04 2022-10-12 Incyte Corporation Derivatives of an fgfr inhibitor
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
US12065494B2 (en) 2021-04-12 2024-08-20 Incyte Corporation Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent
WO2022261160A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
CA3220155A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
US12084453B2 (en) 2021-12-10 2024-09-10 Incyte Corporation Bicyclic amines as CDK12 inhibitors
US20230399331A1 (en) 2022-06-14 2023-12-14 Incyte Corporation Solid forms of jak inhibitor and process of preparing the same
US20240101557A1 (en) 2022-07-11 2024-03-28 Incyte Corporation Fused tricyclic compounds as inhibitors of kras g12v mutants
TW202446371A (zh) 2023-04-18 2024-12-01 美商英塞特公司 ２－氮雜雙環［２．２．１］庚烷ｋｒａｓ抑制劑
WO2024220532A1 (en) 2023-04-18 2024-10-24 Incyte Corporation Pyrrolidine kras inhibitors
WO2025096738A1 (en) 2023-11-01 2025-05-08 Incyte Corporation Kras inhibitors
US20250195536A1 (en) 2023-12-13 2025-06-19 Incyte Corporation Bicyclooctane kras inhibitors

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5593992A (en) * 1993-07-16 1997-01-14 Smithkline Beecham Corporation Compounds
US6432947B1 (en) * 1997-02-19 2002-08-13 Berlex Laboratories, Inc. N-heterocyclic derivatives as NOS inhibitors
JP2002302445A (ja) * 2001-02-02 2002-10-18 Takeda Chem Ind Ltd Ｊｎｋ阻害剤
CA2443234A1 (en) * 2001-04-10 2002-10-24 Vertex Pharmaceuticals Incorporated Isoxaxole derivatives as inhibitors of src and other protein kinases
CA2443487A1 (en) * 2001-04-13 2002-10-24 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
CA2446864C (en) * 2001-05-16 2011-02-15 Vertex Pharmaceuticals Incorporated Inhibitors of src and other protein kinases

Also Published As

Publication number Publication date
AU2005254982A1 (en) 2005-12-29
US7745437B2 (en) 2010-06-29
JP2008502729A (ja) 2008-01-31
CN1960988B (zh) 2012-01-25
CA2567662A1 (en) 2005-12-29
US20070225286A1 (en) 2007-09-27
EP1758892A1 (en) 2007-03-07
BRPI0511978A (pt) 2008-01-22
IL179613A0 (en) 2007-05-15
AR049511A1 (es) 2006-08-09
NO20070160L (no) 2007-01-09
ECSP067070A (es) 2007-01-26
EP1758892B1 (en) 2012-10-17
WO2005123719A1 (en) 2005-12-29
TW200610762A (en) 2006-04-01
JP4688876B2 (ja) 2011-05-25
EP1758892A4 (en) 2010-07-28
RU2007100136A (ru) 2008-07-20
CN1960988A (zh) 2007-05-09
ZA200609450B (en) 2008-05-28
ES2396135T3 (es) 2013-02-19
RU2401265C2 (ru) 2010-10-10
MY144044A (en) 2011-07-29
MA28679B1 (fr) 2007-06-01
MXPA06014247A (es) 2007-03-12
AU2005254982B2 (en) 2008-11-27
CA2567662C (en) 2012-11-27
TNSN06406A1 (en) 2008-02-22

Similar Documents

Publication Publication Date Title
PE20060398A1 (es) Compuestos derivados de pirimidina como inhibidores de quinasa de proteina
PL2099797T3 (pl) Związki i kompozycje jako inhibitory kinaz białkowych
BRPI0815715A8 (pt) Compostos 5-(-4-(haloalcóxi)fenil)pirimidina-2-amina e composições como inibidores de quinases.
EA200970347A1 (ru) Соединения и композиции в качестве ингибиторов протеинкиназ
NO20091949L (no) Sammensetninger og fremgangsmater for modulering av C-kit og PDGFR-reseptorer
WO2006124731A3 (en) Compounds and compositions as protein kinase inhibitors
EA201000003A1 (ru) Ингибиторы протеинкиназ и способы их применения
WO2006101783A8 (en) Compounds and compositions as protein kinase inhibitors
MX2009003649A (es) Inhibidores de cinasa de proteina y metodos para utilizarlos.
ATE499374T1 (de) Verbindungen und zusammensetzungen als proteinkinase-hemmer
ATE474835T1 (de) Als inhibitoren von proteinkinasen geeignete aminopyrimidine
TNSN07176A1 (en) Compounds and compositions as protein kinase inhibitors
ECSP066365A (es) Anilino purinas sustituidas en la posición 6 útiles como inhibidores de rtk
NO20071915L (no) Diaminotriazolforbindelser nyttige som proteinkinaseinhibitorer
ATE508126T1 (de) Als kinaseinhibitoren geeignete aminopyrimidine
AR056346A1 (es) Compuestos y composiciones como inhibidores de quinasa de proteina
NO20074431L (no) Pyrrolopyrimidiner nyttige som proteinkinaseinhibitorer
AR059027A1 (es) Administracion de inhibidores de dipeptidil peptidasa
NO20080967L (no) Benzimidazoler nyttige som inhibitorer av proteinkinaser
NO20072567L (no) Triazoler nyttige som proteinkinase-inhibitorer
MX2009013782A (es) Inhibidores de cinasa de proteina y metodos para el uso de los mismos.
PT1940844E (pt) Compostos e composições como inibidores de proteína-quinase
WO2005039486A3 (en) Compounds and compositions as protein kinase inhibitors
MX2008001605A (es) Compuestos y composiciones de tiazol-2-il amino 5-substituido como inhibidores de cinasa proteica.
BRPI0512422A (pt) compostos e composições como inobidores da proteìna quinase

Legal Events

Date Code Title Description
FG Grant, registration
FD Application declared void or lapsed