JP2004528295A - キナーゼ阻害方法 - Google Patents

キナーゼ阻害方法 Download PDF

Info

Publication number
JP2004528295A
JP2004528295A JP2002560683A JP2002560683A JP2004528295A JP 2004528295 A JP2004528295 A JP 2004528295A JP 2002560683 A JP2002560683 A JP 2002560683A JP 2002560683 A JP2002560683 A JP 2002560683A JP 2004528295 A JP2004528295 A JP 2004528295A
Authority
JP
Japan
Prior art keywords
heterocycle
alkyl
halo
amino
arylamide
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.)
Pending
Application number
JP2002560683A
Other languages
English (en)
Japanese (ja)
Other versions
JP2004528295A5 (enExample
Inventor
バーンズ，クリストファー，ジョン
ウイルクス，アンドリュー，フレデリック
Original Assignee
サイトピア ピーティワイ リミテッド
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
Priority claimed from AUPR2792A external-priority patent/AUPR279201A0/en
Priority claimed from AUPR2793A external-priority patent/AUPR279301A0/en
Application filed by サイトピア ピーティワイ リミテッド filed Critical サイトピア ピーティワイ リミテッド
Publication of JP2004528295A publication Critical patent/JP2004528295A/ja
Publication of JP2004528295A5 publication Critical patent/JP2004528295A5/ja
Pending legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • 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
    • 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
    • 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
    • A61P27/14—Decongestants or antiallergics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/12—Antidiuretics, e.g. drugs for diabetes insipidus

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Virology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Psychiatry (AREA)
  • Dermatology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Otolaryngology (AREA)
JP2002560683A 2001-01-30 2002-01-30 キナーゼ阻害方法 Pending JP2004528295A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
AUPR2792A AUPR279201A0 (en) 2001-01-30 2001-01-30 Jak inhibitors
AUPR2793A AUPR279301A0 (en) 2001-01-30 2001-01-30 Method of inhibiting jak
PCT/AU2002/000089 WO2002060492A1 (en) 2001-01-30 2002-01-30 Methods of inhibiting kinases

Publications (2)

Publication Number Publication Date
JP2004528295A true JP2004528295A (ja) 2004-09-16
JP2004528295A5 JP2004528295A5 (enExample) 2005-12-22

Family

ID=25646570

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2002560683A Pending JP2004528295A (ja) 2001-01-30 2002-01-30 キナーゼ阻害方法

Country Status (5)

Country Link
US (2) US20040102455A1 (enExample)
EP (1) EP1363702A4 (enExample)
JP (1) JP2004528295A (enExample)
CA (1) CA2436487A1 (enExample)
WO (1) WO2002060492A1 (enExample)

Cited By (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006514685A (ja) * 2002-12-11 2006-05-11 サイトピア・リサーチ・ピーティーワイ・リミテッド ピラジン系チューブリン阻害剤
JP2009515888A (ja) * 2005-11-10 2009-04-16 シェーリング コーポレイション プロテインキナーゼインヒビターとしてのイミダゾピラジン
JP2010501003A (ja) * 2006-08-16 2010-01-14 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ピラジン化合物、その使用及び調製方法
JP2010532772A (ja) * 2007-07-11 2010-10-14 バイエル・シェーリング・ファルマ・アクチェンゲゼルシャフト イミダゾ−、ピラゾロピラジン類およびイミダゾトリアジン類およびそれらの使用
KR20100116599A (ko) * 2008-02-01 2010-11-01 어키니언 파마슈티칼스 아베 피라진 유도체 및 단백질 키나아제 억제제로서의 이의 용도
JP2012510997A (ja) * 2008-12-08 2012-05-17 ギリアード コネチカット， インコーポレイテッド イミダゾピラジンＳｙｋ阻害剤
JP2012510998A (ja) * 2008-12-08 2012-05-17 ギリアード コネチカット， インコーポレイテッド イミダゾピラジンｓｙｋ阻害剤
JP2012524053A (ja) * 2009-04-16 2012-10-11 セントロ ナシオナル デ インベスティガシオネス オンコロヒカス（セエネイオ） キナーゼ阻害剤として使用するためのイミダゾピラジン類
JP2014074057A (ja) * 2007-06-08 2014-04-24 Abbvie Inc キナーゼ阻害薬としての５−ヘテロアリール置換インダゾール類
JP2014520767A (ja) * 2011-07-07 2014-08-25 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング がんの処置のための置換されたアザ複素環
US9382256B2 (en) 2013-07-30 2016-07-05 Gilead Connecticut, Inc. Formulation of Syk inhibitors
US9562056B2 (en) 2010-03-11 2017-02-07 Gilead Connecticut, Inc. Imidazopyridines Syk inhibitors
US9657023B2 (en) 2013-07-30 2017-05-23 Gilead Connecticut, Inc. Polymorph of Syk inhibitors
US9687492B2 (en) 2013-12-04 2017-06-27 Gilead Sciences, Inc. Methods for treating cancers
US9707236B2 (en) 2014-07-14 2017-07-18 Gilead Sciences, Inc. Combination methods for treating cancers
US9968601B2 (en) 2013-12-23 2018-05-15 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
US11339168B2 (en) 2019-02-22 2022-05-24 Kronos Bio, Inc. Crystalline forms of 6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine as Syk inhibitors

Families Citing this family (123)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003027295A2 (en) * 2001-09-24 2003-04-03 University Of Aarhus Methods for diagnosis and treatment of diseases associated with altered expression of jak1
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
BR0309398A (pt) * 2002-04-19 2005-02-01 Cellular Genomics Inc Composto ou um seu sal, hidrato, solvato, forma cristalina, diastereÈmero, prodroga farmaceuticamente aceitável, ou misturas deles, composição farmacêutica, e, métodos para tratar uma condição envolvida com a cinase em um mamìfero, para tratar câncer, e para identificar uma cinase
CA2486183C (en) 2002-05-23 2012-01-10 Cytopia Pty Ltd. Protein kinase inhibitors
ATE457025T1 (de) 2002-05-23 2010-02-15 Cytopia Res Pty Ltd Kinaseinhibitoren
AU2003249369A1 (en) 2002-06-21 2004-01-06 Cellular Genomics, Inc. Certain amino-substituted monocycles as kinase modulators
GB0215775D0 (en) * 2002-07-06 2002-08-14 Astex Technology Ltd Pharmaceutical compounds
IL166241A0 (en) * 2002-07-29 2006-01-15 Rigel Pharmaceuticals Inc Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds
US7205308B2 (en) 2002-09-04 2007-04-17 Schering Corporation Trisubstituted 7-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors
DE60313872T2 (de) 2002-09-04 2008-01-17 Schering Corp. Pyrazoloä1,5-aüpyrimidine als hemmstoffe cyclin-abhängiger kinasen
AU2003270489A1 (en) * 2002-09-09 2004-03-29 Cellular Genomics, Inc. 6-ARYL-IMIDAZO(1,2-a)PYRAZIN-8-YLAMINES, METHOD OF MAKING, AND METHOD OF USE THEREOF
KR20060010709A (ko) * 2002-09-23 2006-02-02 쉐링 코포레이션 사이클린 의존성 키나제 억제제로서의 신규한 이미다조피라진
JP4799864B2 (ja) 2002-09-23 2011-10-26 シェーリング コーポレイション サイクリン依存性キナーゼインヒビターとしてのイミダゾピラジン
JP2006505571A (ja) * 2002-10-15 2006-02-16 リゲル ファーマシューテイカルズ、インコーポレイテッド 置換されたインドール及びｈｃｖ阻害剤としてのその使用
US7189723B2 (en) 2003-02-10 2007-03-13 Cgi Pharmaceuticals, Inc. Certain 8-heteroaryl-6-phenyl-imidazo[1,2-a]pyrazines as modulators of kinase activity
AR043002A1 (es) * 2003-02-18 2005-07-13 Altana Pharma Ag Imidazopirazinas 6-substituidos
US7186832B2 (en) 2003-02-20 2007-03-06 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
US7157460B2 (en) 2003-02-20 2007-01-02 Sugen Inc. Use of 8-amino-aryl-substituted imidazopyrazines as kinase inhibitors
CA2517291C (en) * 2003-03-19 2012-05-08 Exelixis, Inc. Ortho-substituted aryl and heteroaryl tie-2 modulators and methods of use
WO2004084813A2 (en) * 2003-03-21 2004-10-07 Smithkline Beecham Corporation Chemical compounds
JP4895806B2 (ja) * 2003-04-09 2012-03-14 エクセリクシス， インク． Ｔｉｅ−２モジュレータと使用方法
US7405295B2 (en) 2003-06-04 2008-07-29 Cgi Pharmaceuticals, Inc. Certain imidazo[1,2-a]pyrazin-8-ylamines and method of inhibition of Bruton's tyrosine kinase by such compounds
US7393848B2 (en) 2003-06-30 2008-07-01 Cgi Pharmaceuticals, Inc. Certain heterocyclic substituted imidazo[1,2-A]pyrazin-8-ylamines and methods of inhibition of Bruton's tyrosine kinase by such compounds
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
WO2005019220A2 (en) * 2003-08-11 2005-03-03 Cellular Genomics Inc. Substituted imidazo[1,2-a]pyrazines as modulators of kinase activity
US7390907B2 (en) 2003-09-30 2008-06-24 Amgen Inc. Vanilloid receptor ligands and their use in treatments
ES2372694T3 (es) 2003-10-15 2012-01-25 OSI Pharmaceuticals, LLC Inhibidores de tirosina cinasa de imidazo[1,5-a]pirazina.
WO2005047290A2 (en) * 2003-11-11 2005-05-26 Cellular Genomics Inc. Imidazo[1,2-a] pyrazin-8-ylamines as kinase inhibitors
PT1689715E (pt) * 2003-12-03 2011-05-16 Ym Biosciences Australia Pty Inibidores da tubulina
GB2423083B (en) 2003-12-03 2007-07-11 Cytopia Res Pty Ltd Azole-based kinase inhibitors
WO2005058876A1 (en) * 2003-12-16 2005-06-30 Gpc Biotech Ag Pyrazine derivatives as effective compounds against infectious diseases
WO2005085252A1 (en) * 2004-03-04 2005-09-15 Biofocus Discovery Limited Imidazo ‘1,2-a’ pyrazine compounds which interact with protein kinases
MXPA06011423A (es) 2004-04-02 2007-01-23 Osi Pharm Inc Inhibidores de proteina cinasa heterobiciclica sustituida en el anillo 6,6-biciclico.
US7642354B2 (en) 2004-04-13 2010-01-05 Icagen, Inc. Polycyclic pyrazines as potassium ion channel modulators
AU2005310979A1 (en) * 2004-11-16 2006-06-08 Bellus Health (International) Limited Compounds for the treatment of CNS and amyloid associated diseases
RU2007123675A (ru) * 2004-11-24 2008-12-27 Новартис АГ (CH) Комбинации ингибиторов jak
GB0428082D0 (en) 2004-12-22 2005-01-26 Welcome Trust The Ltd Therapeutic compounds
AR054416A1 (es) 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
US7777040B2 (en) 2005-05-03 2010-08-17 Cgi Pharmaceuticals, Inc. Certain substituted ureas, as modulators of kinase activity
WO2006133426A2 (en) 2005-06-08 2006-12-14 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
EP1928237A4 (en) 2005-09-02 2011-03-09 Abbott Lab NEW HETEROCYCLES BASED ON IMIDAZO
WO2007038215A1 (en) 2005-09-22 2007-04-05 Incyte Corporation Tetracyclic inhibitors of janus kinases
HUE028588T2 (hu) 2005-12-13 2016-12-28 Incyte Holdings Corp Heteroaril-szubsztituált pirrolo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok
US8575164B2 (en) * 2005-12-19 2013-11-05 OSI Pharmaceuticals, LLC Combination cancer therapy
WO2007098507A2 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2007126964A2 (en) * 2006-03-31 2007-11-08 Schering Corporation Kinase inhibitors
US7893058B2 (en) * 2006-05-15 2011-02-22 Janssen Pharmaceutica Nv Imidazolopyrazine compounds useful for the treatment of degenerative and inflammatory diseases
HRP20100378T1 (hr) * 2006-05-31 2010-08-31 Galapagos N.V. Spojevi triazolopirazina učinkoviti za tretman degenerativnih i upalnih bolesti
US20090175852A1 (en) 2006-06-06 2009-07-09 Schering Corporation Imidazopyrazines as protein kinase inhibitors
ES2415863T3 (es) 2006-12-22 2013-07-29 Incyte Corporation Heterociclos sustituidos como inhibidores de Janus Quinasas
HUE029188T2 (en) 2007-03-12 2017-03-28 Ym Biosciences Australia Pty Phenylamino-pyrimidine compounds and their use
US8148369B2 (en) 2007-05-10 2012-04-03 Janssen Pharmaceutica Nv Fused pyrazine compounds useful for the treatment of degenerative and inflammatory diseases
EP2740731B1 (en) 2007-06-13 2016-03-23 Incyte Holdings Corporation Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
GB0716292D0 (en) * 2007-08-21 2007-09-26 Biofocus Dpi Ltd Imidazopyrazine compounds
EP2250173A1 (en) * 2008-01-18 2010-11-17 OSI Pharmaceuticals, Inc. Imidazopyrazinol derivatives for the treatment of cancers
JP5496915B2 (ja) * 2008-02-13 2014-05-21 シージーアイ ファーマシューティカルズ，インコーポレーテッド ６−アリール−イミダゾ［１，２−ａ］ピラジン誘導体、その製造方法、及びその使用方法
HRP20170317T1 (hr) 2008-02-15 2017-04-21 Rigel Pharmaceuticals, Inc. Spojevi pirimidin-2-amina i njihova uporaba kao inhibitora jak kinaza
MY165582A (en) 2008-03-11 2018-04-05 Incyte Holdings Corp Azetidine and cyclobutane derivatives as jak inhibitors
US8063058B2 (en) 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
BRPI0910668A2 (pt) 2008-04-22 2019-09-24 Portola Pharmaceutiacals Inc inibidores de proteína quinases
CA2723358A1 (en) * 2008-05-05 2009-11-12 Allison B. Reiss Method for improving cardiovascular risk profile of cox inhibitors
ES2396613T3 (es) * 2008-05-19 2013-02-22 OSI Pharmaceuticals, LLC Imidazopirazinas e imidazotriazinas sustituidas
US8450321B2 (en) 2008-12-08 2013-05-28 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
GB0822981D0 (en) * 2008-12-17 2009-01-21 Summit Corp Plc Compounds for treatment of duchenne muscular dystrophy
EP2421837A1 (en) 2009-04-20 2012-02-29 OSI Pharmaceuticals, LLC Preparation of c-pyrazine-methylamines
WO2010129740A1 (en) * 2009-05-07 2010-11-11 Osi Pharmaceuticals, Inc. Use of osi-906 for treating adrenocortical carcinoma
NZ596479A (en) 2009-05-22 2014-01-31 Incyte Corp N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
BRPI1012108B8 (pt) 2009-05-22 2021-05-25 Incyte Corp composto 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]octa no- ou heptano-nitrila, sua composição, seus usos e processo para preparar um sal de ácido fosfórico
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EA021478B1 (ru) 2009-10-09 2015-06-30 Инсайт Корпорейшн ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА
CA2779681A1 (en) * 2009-11-05 2011-05-12 Lexicon Pharmaceuticals, Inc. Tryptophan hydroxylase inhibitors for the treatment of cancer
PH12012501361A1 (en) * 2009-12-31 2012-10-22 Centro Nac De Investigaciones Oncologicas Cnio Tricyclic compounds for use as kinase inhibitors
US20120277244A1 (en) * 2009-12-31 2012-11-01 Novartis Ag Pyrazine derivatives and their use in the treatment of neurological disorders
CA2787714C (en) 2010-01-22 2019-04-09 Joaquin Pastor Fernandez Inhibitors of pi3 kinase
CA2792508C (en) 2010-03-10 2018-01-16 Incyte Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
US20130131057A1 (en) * 2010-05-13 2013-05-23 Centro Nacional De Investigaciones Oncologicas (Cnio New bicyclic compounds as pi3-k and mtor inhibitors
EA202091303A3 (ru) 2010-05-21 2021-05-31 Инсайт Холдингс Корпорейшн Композиция ингибитора jak для местного применения
EP2441755A1 (en) * 2010-09-30 2012-04-18 Almirall, S.A. Pyridine- and isoquinoline-derivatives as Syk and JAK kinase inhibitors
WO2012052745A1 (en) 2010-10-21 2012-04-26 Centro Nacional De Investigaciones Oncológicas (Cnio) Combinations of pi3k inhibitors with a second anti -tumor agent
EP2444084A1 (en) 2010-10-21 2012-04-25 Centro Nacional de Investigaciones Oncológicas (CNIO) Use of PI3K inibitors for the treatment of obesity
EP2975027A1 (en) 2010-11-01 2016-01-20 Portola Pharmaceuticals, Inc. Nicotinamides as jak kinase modulators
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
WO2012112847A1 (en) 2011-02-18 2012-08-23 Novartis Pharma Ag mTOR/JAK INHIBITOR COMBINATION THERAPY
JO3363B1 (ar) 2011-04-13 2019-03-13 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
WO2012154518A1 (en) 2011-05-10 2012-11-15 Merck Sharp & Dohme Corp. Bipyridylaminopyridines as syk inhibitors
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
WO2013023119A1 (en) 2011-08-10 2013-02-14 Novartis Pharma Ag JAK P13K/mTOR COMBINATION THERAPY
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
EP2782579B1 (en) 2011-11-23 2019-01-02 Portola Pharmaceuticals, Inc. Pyrazine kinase inhibitors
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲ｊａｋ抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
WO2014013014A1 (en) 2012-07-18 2014-01-23 Fundació Privada Centre De Regulació Genòmica (Crg) Jak inhibitors for activation of epidermal stem cell populations
WO2014058921A2 (en) 2012-10-08 2014-04-17 Portola Pharmaceuticals, Inc. Substituted pyrimidinyl kinase inhibitors
BR112015008480A2 (pt) 2012-10-15 2017-07-04 Epizyme Inc compostos de benzeno substituído
US20150299125A1 (en) * 2012-11-07 2015-10-22 Merck Sharp & Dohme Corp. Prodrug bipyridylaminopyridines as syk inhibitors
KR102242077B1 (ko) 2012-11-15 2021-04-20 인사이트 홀딩스 코포레이션 룩솔리티니브의 서방성 제형
WO2014106606A1 (en) * 2013-01-05 2014-07-10 F. Hoffmann-La Roche Ag Nove phenyl/pyridine series substitued by hydroxyethylamino for the treatment of cancer
WO2014110200A1 (en) 2013-01-10 2014-07-17 Zisman Lawrence S Non-selective kinase inhibitors
EP3489239B1 (en) 2013-03-06 2021-09-15 Incyte Holdings Corporation Processes and intermediates for making a jak inhibitor
MX376856B (es) 2013-08-07 2025-03-07 Incyte Holdings Corp Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1).
ES2959419T3 (es) 2013-10-11 2024-02-26 Pulmokine Inc Formulaciones secas por aspersión
US9290505B2 (en) 2013-12-23 2016-03-22 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
WO2015157955A1 (en) * 2014-04-17 2015-10-22 Abbvie Inc. Heterocyclic btk inhibit ors
EP3137454A1 (en) 2014-04-28 2017-03-08 Pfizer Inc. Heteroaromatic compounds and their use as dopamine d1 ligands
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
TWI681954B (zh) 2014-06-12 2020-01-11 美商西爾拉癌症醫學公司 Ｎ-（氰基甲基）-４-（２-（４-𠰌啉基苯基胺基）嘧啶-４-基）苯甲醯胺
WO2018041989A1 (en) 2016-09-02 2018-03-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for diagnosing and treating refractory celiac disease type 2
RU2763525C2 (ru) 2016-10-27 2021-12-30 Пульмокин, Инк. Комбинированная терапия для лечения легочной гипертензии
KR20220070056A (ko) 2017-08-25 2022-05-27 길리애드 사이언시즈, 인코포레이티드 Syk 억제제의 다형체
TW201924683A (zh) 2017-12-08 2019-07-01 美商英塞特公司 用於治療骨髓增生性贅瘤的低劑量組合療法
MD3746429T2 (ro) 2018-01-30 2022-08-31 Incyte Corp Procedee pentru prepararea de (1-(3-fluoro-2-(trifluorometil)izonicotinil)piperidin-4-onă)
KR20260080448A (ko) 2018-03-30 2026-06-02 인사이트 코포레이션 Jak 억제제를 사용하는 화농성 한선염의 치료
WO2020201362A2 (en) 2019-04-02 2020-10-08 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
WO2020212395A1 (en) 2019-04-16 2020-10-22 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
TW202214634A (zh) * 2020-06-09 2022-04-16 大陸商賽諾哈勃藥業（成都）有限公司 雜環化合物及其衍生物
US20250283174A1 (en) 2022-05-16 2025-09-11 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stem cells induced by chronic inflammation
CN119630668A (zh) * 2022-07-25 2025-03-14 细胞基因公司 取代的咪唑并吡嗪化合物作为irak3结合剂
WO2026093435A1 (en) 2024-10-31 2026-05-07 Institut National de la Santé et de la Recherche Médicale Use of jak inhibitors for enhancing the potency of immunotherapy in the treament of cancer

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1345449A (en) * 1971-05-14 1974-01-30 Science Union & Cie Pyridylpiperazines and process for their preparation
US4876256A (en) * 1988-04-29 1989-10-24 Merck & Co., Inc. Alkylpiperazinylpyridines as hypoglycemic agents
US5494908A (en) * 1992-11-23 1996-02-27 Hoechst-Roussel Pharmaceutical Incorporated Substituted 3-(aminoalkylamino)-1,2-benzisoxazoles and related compounds
US5654307A (en) * 1994-01-25 1997-08-05 Warner-Lambert Company Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
US6231833B1 (en) * 1999-08-05 2001-05-15 Pfizer Inc 2,7-substituted octahydro-1H-pyrido[1,2-A]pyrazine derivatives as ligands for serotonin receptors
JPH09132529A (ja) * 1995-11-09 1997-05-20 Ono Pharmaceut Co Ltd 一酸化窒素合成酵素阻害剤
US5958919A (en) * 1996-09-20 1999-09-28 Washington University Treatment of presymptomatic alzheimer's disease to prevent neuronal degeneration
DE69940808D1 (de) * 1998-03-04 2009-06-10 Bristol Myers Squibb Co Heterocyclen substituierte imidazopyrazine als protein- tyrosin-kinase-inhibitoren
AU3951899A (en) * 1998-06-19 2000-01-05 Pfizer Products Inc. Pyrrolo(2,3-d)pyrimidine compounds
EP0982030A3 (en) * 1998-08-17 2000-05-10 Pfizer Products Inc. 2,7-substituted octahydro-pyrrolo 1,2-a]pyrazine derivatives as 5ht 1a ligands
US6548503B1 (en) * 1998-11-04 2003-04-15 Smithkline Beecham Corporation Pyridin-4-yl or pyrimidin-4-yl substituted pyrazines
ATE329596T1 (de) * 1999-03-30 2006-07-15 Novartis Pharma Gmbh Phthalazinderivate zur behandlung von entzündlicher erkrankungen
MXPA02002559A (es) * 1999-09-10 2002-07-30 Merck & Co Inc Inhibidores de tirosina cinasa.
CN1272328C (zh) * 1999-12-17 2006-08-30 希龙公司 糖元合成酶激酶3的基于吡嗪的抑制剂
US6335342B1 (en) * 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
AU2001278206A1 (en) * 2000-08-08 2002-02-18 Ortho-Mcneil Pharmaceutical, Inc. Neuroprotective 2-pyridinamine compositions and related methods
JP2004513953A (ja) * 2000-10-24 2004-05-13 メルク　エンド　カムパニー　インコーポレーテッド ジベンズオキサゼピンαＶインテグリン受容体アンタゴニスト
CA2450769A1 (en) * 2001-06-15 2002-12-27 Vertex Pharmaceuticals Incorporated 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors

Cited By (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4777065B2 (ja) * 2002-12-11 2011-09-21 ワイエム・バイオサイエンシズ・オーストラリア・ピーティーワイ・リミテッド ピラジン系チューブリン阻害剤
JP2006514685A (ja) * 2002-12-11 2006-05-11 サイトピア・リサーチ・ピーティーワイ・リミテッド ピラジン系チューブリン阻害剤
JP2009515888A (ja) * 2005-11-10 2009-04-16 シェーリング コーポレイション プロテインキナーゼインヒビターとしてのイミダゾピラジン
JP2010501003A (ja) * 2006-08-16 2010-01-14 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ピラジン化合物、その使用及び調製方法
JP2014074057A (ja) * 2007-06-08 2014-04-24 Abbvie Inc キナーゼ阻害薬としての５−ヘテロアリール置換インダゾール類
JP2010532772A (ja) * 2007-07-11 2010-10-14 バイエル・シェーリング・ファルマ・アクチェンゲゼルシャフト イミダゾ−、ピラゾロピラジン類およびイミダゾトリアジン類およびそれらの使用
KR20100116599A (ko) * 2008-02-01 2010-11-01 어키니언 파마슈티칼스 아베 피라진 유도체 및 단백질 키나아제 억제제로서의 이의 용도
JP2011510948A (ja) * 2008-02-01 2011-04-07 アチニオン・ファーマスーティカルズ・アクチエボラーグ 新規化合物、その使用及び製造
KR101599082B1 (ko) * 2008-02-01 2016-03-02 어키니언 파마슈티칼스 아베 피라진 유도체 및 단백질 키나아제 억제제로서의 이의 용도
JP2014148522A (ja) * 2008-02-01 2014-08-21 Akinion Pharmaceuticals Ab 新規化合物、その使用及び製造
US8765761B2 (en) 2008-12-08 2014-07-01 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-{4-[2-methyl-1-(morpholin-4-yl)propan-2-yl]phenyl}imidazo[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a syk inhibitor
JP2012510998A (ja) * 2008-12-08 2012-05-17 ギリアード コネチカット， インコーポレイテッド イミダゾピラジンｓｙｋ阻害剤
US9796718B2 (en) 2008-12-08 2017-10-24 Gilead Connecticut, Inc. 6-(benzo[d]thiazol-5-yl)-n-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine
US10093684B2 (en) 2008-12-08 2018-10-09 Gilead Connecticut, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
JP2017101090A (ja) * 2008-12-08 2017-06-08 ギリアード コネチカット， インコーポレイテッド イミダゾピラジンＳｙｋ阻害剤
US8962835B2 (en) 2008-12-08 2015-02-24 Gilead Connecticut, Inc. Imidazopyrazine Syk inhibitors
US9120811B2 (en) 2008-12-08 2015-09-01 Gilead Connecticut, Inc. 6-(1H-indazol-6-YL)-N-(4-morpholinophenyl)imidazo[1,4-A]pyrazin-8-amine for treating leukemia or lymphoma
JP2015205935A (ja) * 2008-12-08 2015-11-19 ギリアード コネチカット， インコーポレイテッド イミダゾピラジンＳｙｋ阻害剤
US9212191B2 (en) 2008-12-08 2015-12-15 Gilead Connecticut, Inc. 6-(2,3-dihydro-1H-pyrido-[2,3-b][1,4]oxazin-7-yl)-N-(4-morpholinophenyl)imidazo[1,2-a] pyrazin-8-amine as a spleen tyrosine kinase inhibitor
US8748607B2 (en) 2008-12-08 2014-06-10 Gilead Connecticut, Inc. Imidazopyrizine syk inhibitors
JP2012510997A (ja) * 2008-12-08 2012-05-17 ギリアード コネチカット， インコーポレイテッド イミダゾピラジンＳｙｋ阻害剤
US9567348B2 (en) 2008-12-08 2017-02-14 Gilead Connecticut, Inc. Substituted pyrazolo[1,5-a]pyrimidines as Syk inhibitors
JP2012524053A (ja) * 2009-04-16 2012-10-11 セントロ ナシオナル デ インベスティガシオネス オンコロヒカス（セエネイオ） キナーゼ阻害剤として使用するためのイミダゾピラジン類
US9562056B2 (en) 2010-03-11 2017-02-07 Gilead Connecticut, Inc. Imidazopyridines Syk inhibitors
US10842803B2 (en) 2010-03-11 2020-11-24 Kronos Bio, Inc. Imidazopyridines Syk inhibitors
US10092583B2 (en) 2010-03-11 2018-10-09 Gilead Connecticut, Inc. Imidazopyridines Syk inhibitors
JP2014520767A (ja) * 2011-07-07 2014-08-25 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング がんの処置のための置換されたアザ複素環
US9382256B2 (en) 2013-07-30 2016-07-05 Gilead Connecticut, Inc. Formulation of Syk inhibitors
US9918939B2 (en) 2013-07-30 2018-03-20 Gilead Connecticut, Inc. Formulation of Syk inhibitors
US9949932B2 (en) 2013-07-30 2018-04-24 Gilead Connecticut, Inc. Formulation of syk inhibitors
US9657023B2 (en) 2013-07-30 2017-05-23 Gilead Connecticut, Inc. Polymorph of Syk inhibitors
US10266539B2 (en) 2013-07-30 2019-04-23 Gilead Connecticut, Inc. Polymorph of Syk inhibitors
US9687492B2 (en) 2013-12-04 2017-06-27 Gilead Sciences, Inc. Methods for treating cancers
US9974792B2 (en) 2013-12-04 2018-05-22 Gilead Sciences, Inc. Methods for treating cancers
US10342794B2 (en) 2013-12-23 2019-07-09 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
US10828299B2 (en) 2013-12-23 2020-11-10 Kronos Bio, Inc. Crystalline monomesylate salt of 6-(6-aminopyrazin-2-yl)-n-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine
US9968601B2 (en) 2013-12-23 2018-05-15 Gilead Sciences, Inc. Substituted imidazo[1,2-a]pyrazines as Syk inhibitors
US11517570B2 (en) 2013-12-23 2022-12-06 Kronos Bio, Inc. Crystalline succinate salt of 6-(6-aminopyrazin-2-yl)-n-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine
US12263163B2 (en) 2013-12-23 2025-04-01 Kronos Bio, Inc. Crystalline succinate salt of 6-(6-aminopyrazin-2-yl)-n-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine as a Syk inhibitor
US9707236B2 (en) 2014-07-14 2017-07-18 Gilead Sciences, Inc. Combination methods for treating cancers
US10080756B2 (en) 2014-07-14 2018-09-25 Gilead Sciences, Inc. Combination methods for treating cancers
US11339168B2 (en) 2019-02-22 2022-05-24 Kronos Bio, Inc. Crystalline forms of 6-(6-aminopyrazin-2-yl)-N-(4-(4-(oxetan-3-yl)piperazin-1-yl)phenyl)imidazo[1,2-a]pyrazin-8-amine as Syk inhibitors

Also Published As

Publication number Publication date
US20060069084A1 (en) 2006-03-30
US20040102455A1 (en) 2004-05-27
CA2436487A1 (en) 2002-08-08
EP1363702A4 (en) 2007-08-22
EP1363702A1 (en) 2003-11-26
WO2002060492A1 (en) 2002-08-08

Similar Documents

Publication Publication Date Title
US20040102455A1 (en) Method of inhibiting kinases
RU2632900C2 (ru) Гетероциклические амины и их применение
KR101164541B1 (ko) 선택적 키나제 저해제
AU2003229370B2 (en) Kinase inhibitors
KR102835667B1 (ko) Parp14 억제제로서의 퀴나졸리논
JP2023503052A (ja) Ｈｅｌｉｏｓタンパク質の阻害剤として有用な化合物
JP4831907B2 (ja) ＦａｂＩ阻害剤
CN104603106B (zh) 吲哚甲酰胺衍生物及其用途
KR20210086674A (ko) Il-12, il-23 및/또는 ifn-알파의 조정과 관련된 상태의 치료를 위한 아미드-치환된 헤테로시클릭 화합물
EP1689739B1 (en) Azole-based kinase inhibitors
US12421238B2 (en) Selective dihydropyrrolopyrimidine JAK2 inhibitors
JP2005531584A (ja) ピラゾロピリミジンアニリン化合物
WO2006070943A1 (ja) 縮合イミダゾール化合物およびその用途
CN102015717A (zh) 趋化因子受体调节剂
CN1409711A (zh) 用作hiv逆转录酶抑制剂的稠合的二氮萘化合物
JPH09505055A (ja) サイトカイン媒介疾患治療用オキサゾール
WO2014082578A1 (zh) 杂芳基炔烃化合物及其应用
WO2024020221A1 (en) Modulators of tyk2 proteolysis and associated methods of use
CN115768761A (zh) 新颖苯并咪唑衍生物
EP1857442A2 (en) Novel antimycobacterial compounds
EP3801525A1 (en) Inhibitors of prolyl-trna-synthetase
WO2005118543A1 (ja) キナーゼ阻害薬およびその用途
JP2011510967A (ja) 新規複素環化合物
AU2002226197B2 (en) Methods of inhibiting kinases
JP5893155B2 (ja) Ｃｒｔｈ２受容体拮抗薬としての窒素含有縮合環式化合物

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20041217

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20041217

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20080910

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20080916

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20081210

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20081217

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20090602