JP4681302B2 - チアジアゾールまたはオキサジアゾール、およびこれらの、ｊａｋプロテインキナーゼのインヒビターとしての使用 - Google Patents

チアジアゾールまたはオキサジアゾール、およびこれらの、ｊａｋプロテインキナーゼのインヒビターとしての使用 Download PDF

Info

Publication number
JP4681302B2
JP4681302B2 JP2004563181A JP2004563181A JP4681302B2 JP 4681302 B2 JP4681302 B2 JP 4681302B2 JP 2004563181 A JP2004563181 A JP 2004563181A JP 2004563181 A JP2004563181 A JP 2004563181A JP 4681302 B2 JP4681302 B2 JP 4681302B2
Authority
JP
Japan
Prior art keywords
compounds
compound
aliphatic
jak
mmol
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.)
Expired - Fee Related
Application number
JP2004563181A
Other languages
English (en)
Japanese (ja)
Other versions
JP2006513192A (ja
JP2006513192A5 (enExample
Inventor
ガイ ダブリュ． ベミス，
スコット エル． ハーブソン，
マーク リーデボー，
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.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex 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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of JP2006513192A publication Critical patent/JP2006513192A/ja
Publication of JP2006513192A5 publication Critical patent/JP2006513192A5/ja
Application granted granted Critical
Publication of JP4681302B2 publication Critical patent/JP4681302B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • A61P25/28—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
    • 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
    • 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
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2004563181A 2002-05-06 2003-05-06 チアジアゾールまたはオキサジアゾール、およびこれらの、ｊａｋプロテインキナーゼのインヒビターとしての使用 Expired - Fee Related JP4681302B2 (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37818502P 2002-05-06 2002-05-06
PCT/US2003/014223 WO2004058753A1 (en) 2002-05-06 2003-05-06 Thiadiazoles or oxadiazoles and their use as inhibitors of jak protein kinase

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2010101525A Division JP2010159306A (ja) 2002-05-06 2010-04-26 チアジアゾールまたはオキサジアゾール、およびこれらの、ｊａｋプロテインキナーゼのインヒビターとしての使用

Publications (3)

Publication Number Publication Date
JP2006513192A JP2006513192A (ja) 2006-04-20
JP2006513192A5 JP2006513192A5 (enExample) 2006-07-06
JP4681302B2 true JP4681302B2 (ja) 2011-05-11

Family

ID=32681783

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2004563181A Expired - Fee Related JP4681302B2 (ja) 2002-05-06 2003-05-06 チアジアゾールまたはオキサジアゾール、およびこれらの、ｊａｋプロテインキナーゼのインヒビターとしての使用
JP2010101525A Pending JP2010159306A (ja) 2002-05-06 2010-04-26 チアジアゾールまたはオキサジアゾール、およびこれらの、ｊａｋプロテインキナーゼのインヒビターとしての使用

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2010101525A Pending JP2010159306A (ja) 2002-05-06 2010-04-26 チアジアゾールまたはオキサジアゾール、およびこれらの、ｊａｋプロテインキナーゼのインヒビターとしての使用

Country Status (14)

Country Link
US (1) US7271179B2 (enExample)
EP (2) EP2316834A1 (enExample)
JP (2) JP4681302B2 (enExample)
KR (1) KR20050006237A (enExample)
CN (1) CN1665808A (enExample)
AT (1) ATE489384T1 (enExample)
AU (1) AU2003299472A1 (enExample)
CA (1) CA2485429A1 (enExample)
DE (1) DE60335099D1 (enExample)
IL (1) IL165067A0 (enExample)
MX (1) MXPA04011048A (enExample)
NO (1) NO20045282L (enExample)
RU (1) RU2004135386A (enExample)
WO (1) WO2004058753A1 (enExample)

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP20050089B1 (hr) 2002-07-29 2015-06-19 Rigel Pharmaceuticals Upotreba 2,4 pirimidindiaminskog spoja za proizvodnju lijeka za lijeäśenje ili sprjeäśavanje autoimunosne bolesti
DE102004009933A1 (de) * 2004-02-26 2005-09-15 Merck Patent Gmbh Verwendung von Thiadiazolharnstoffderivaten
US7550499B2 (en) 2004-05-12 2009-06-23 Bristol-Myers Squibb Company Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
AU2005245389A1 (en) * 2004-05-12 2005-12-01 Bristol-Myers Squibb Company Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
US7977345B2 (en) * 2004-07-02 2011-07-12 Exelixis, Inc. c-MET modulators and method of use
CN101039933B (zh) * 2004-09-17 2012-06-06 沃泰克斯药物股份有限公司 可用作蛋白激酶抑制剂的二氨基三唑化合物
EP1809282B1 (en) * 2004-10-18 2013-01-09 Amgen, Inc Thiadiazole compounds and methods of use
US7767687B2 (en) * 2004-12-13 2010-08-03 Biogen Idec Ma Inc. Pyrido pyrimidinones, dihydro pyrimido pyrimidinones and pteridinones useful as RAF kinase inhibitors
WO2006078621A2 (en) * 2005-01-19 2006-07-27 Bristol-Myers Squibb Company 2-phenoxy-n- (1, 3 , 4-thiadizol-2-yl) pyridin-3-amine derivatives and related compounds as p2y1 receptor inhibitors for the treatment of thromboembolic disorders
BRPI0610876B8 (pt) 2005-06-08 2021-05-25 Rigel Pharmaceuticals Inc composto, formulação farmacêutica, e métodos de inibir uma atividade de uma jak cinase, e de inibir uma cascata de transdução de sinal em que jak3 cinase desempenha um papel
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
DE602006017694D1 (de) * 2005-06-27 2010-12-02 Bristol Myers Squibb Co C-verknüpfte zyklische antagonisten des p2y1-rezeptors mit eignung bei der behandlung thrombotischer leiden
ATE502924T1 (de) 2005-06-27 2011-04-15 Bristol Myers Squibb Co Lineare harnstoffmimetika-antagonisten des p2y1- rezeptors zur behandlung von thromboseleiden
TW200726764A (en) * 2005-06-27 2007-07-16 Bristol Myers Squibb Co N-linked heterocyclic antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
WO2007002634A1 (en) * 2005-06-27 2007-01-04 Bristol-Myers Squibb Company Carbocycle and heterocycle antagonists of p2y1 receptor useful in the treatment of thrombotic conditions
JP2009510132A (ja) * 2005-10-05 2009-03-12 メルク フロスト カナダ リミテツド ロイコトリエン生合成の阻害剤としての置換キノリン
ES2622493T3 (es) 2006-02-24 2017-07-06 Rigel Pharmaceuticals, Inc. Composiciones y métodos para la inhibición de la ruta de JAK
US20070213378A1 (en) * 2006-03-10 2007-09-13 Lymphosign Inc. Compounds for modulating cell proliferation, compositions and methods related thereto
EP2079739A2 (en) 2006-10-04 2009-07-22 Pfizer Products Inc. Pyrido[4,3-d]pyrimidin-4(3h)-one derivatives as calcium receptor antagonists
US7960569B2 (en) * 2006-10-17 2011-06-14 Bristol-Myers Squibb Company Indole antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
WO2008139845A1 (ja) * 2007-04-24 2008-11-20 Daiichi Sankyo Company, Limited 新規アミド誘導体
HUE030912T2 (en) 2008-02-15 2017-06-28 Rigel Pharmaceuticals Inc Pyrimidine-2-amine compounds and their use as inhibitors of yak kinases
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
US8063058B2 (en) 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
AU2009238590A1 (en) 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
US8466290B2 (en) 2008-07-10 2013-06-18 Pharma Ip General Incorporated Association STAT3 inhibitor containing quinolinecarboxamide derivative as active ingredient
MY159327A (en) * 2009-02-27 2016-12-25 Ambit Biosciences Corp Jak kinase modulating quinazoline derivatives and methods of use thereof
US8361962B2 (en) * 2009-07-27 2013-01-29 Roche Palo Alto Llc Tricyclic inhibitors of JAK
PL2520575T3 (pl) 2009-12-28 2017-05-31 General Incorporated Association Pharma Valley Project Supporting Organization Związek 1,3,4-oksadiazolo-2-karboksyamidowy
KR101483215B1 (ko) * 2010-01-29 2015-01-16 한미약품 주식회사 단백질 키나아제 저해활성을 갖는 비시클릭 헤테로아릴 유도체
JP5855095B2 (ja) 2010-06-07 2016-02-09 ノボメディックス, エルエルシーNovomedix, Llc フラニル化合物およびその使用
EP2397482A1 (en) * 2010-06-15 2011-12-21 Almirall, S.A. Heteroaryl imidazolone derivatives as jak inhibitors
CN101891697B (zh) * 2010-07-02 2011-08-31 山东大学 含1，2，4-噁二唑杂环α，β-不饱和酮类化合物
EP2975027A1 (en) 2010-11-01 2016-01-20 Portola Pharmaceuticals, Inc. Nicotinamides as jak kinase modulators
MX363551B (es) 2011-11-23 2019-03-27 Portola Pharmaceuticals Inc Star Compuestos derivados de pirazina como inhibidores de cinasa.
KR101328126B1 (ko) * 2012-04-10 2013-11-08 연세대학교 원주산학협력단 신규한 옥사디아졸 유도체 및 이의 알레르기 질환의 예방, 개선 또는 치료적 용도
MX371331B (es) 2012-04-24 2020-01-27 Vertex Pharma Inhibidores de la proteina cinasa dependiente de acido desoxirribonucleico(adn-pk).
CN103382206B (zh) * 2012-05-04 2016-09-28 上海恒瑞医药有限公司 喹啉或喹唑啉类衍生物、其制备方法及其在医药上的应用
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
JP6218848B2 (ja) * 2012-11-20 2017-10-25 プロキナーゼ ゲゼルシャフト ミット ベシュレンクテル ハフツング プロテインキナーゼ阻害剤としてのチオエーテル誘導体
CL2012003253A1 (es) * 2012-11-22 2013-01-11 Univ Concepcion Compuestos derivados de 1,3,4-tiadiazol alquilamidas y de chalconas, antagonistas del receptor trpv-1; uso de los compuestos para tratar el dolor cronico.
ME03336B (me) 2013-03-12 2019-10-20 Vertex Pharma Inhibitori dnk-pk
JP6408569B2 (ja) 2013-10-17 2018-10-17 バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ Ｄｎａ−ｐｋ阻害剤としての（ｓ）−ｎ−メチル−８−（１−（（２’−メチル−［４，５’−ビピリミジン］−６−イル）アミノ）プロパン−２−イル）キノリン−４−カルボキサミドおよびその重水素化誘導体の共結晶
AU2014353006B2 (en) 2013-11-20 2019-04-04 Signalchem Life Sciences Corp. Quinazoline derivatives as TAM family kinase inhibitors
JP6269942B2 (ja) * 2014-02-20 2018-01-31 国立研究開発法人理化学研究所 ｐ３８ＭＡＰキナーゼγおよび／またはδ阻害剤
KR102894264B1 (ko) * 2015-03-10 2025-12-02 오리진 온콜로지 리미티드 면역조절제로서의 1,2,4-옥사다이아졸 및 티아다이아졸 화합물
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
EP3518931A4 (en) 2016-09-27 2020-05-13 Vertex Pharmaceuticals Incorporated METHOD FOR TREATING CANCER WITH A COMBINATION OF DNA-DAMAGING SUBSTANCES AND DNA-PK INHIBITORS
WO2018160944A1 (en) * 2017-03-03 2018-09-07 Progenra, Inc. Azole compounds as ubiquitin-specific protease usp7 inhibitors
CN108148058B (zh) * 2018-02-08 2021-03-16 中国人民解放军第四军医大学 一种4-(2-巯基噻二唑)取代的嘧啶衍生物其制备方法及应用
EA202192575A1 (ru) 2019-03-21 2022-01-14 Онксео Соединения dbait в сочетании с ингибиторами киназ для лечения рака
EP3947737A2 (en) 2019-04-02 2022-02-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods of predicting and preventing cancer in patients having premalignant lesions
EP3955920A1 (en) 2019-04-16 2022-02-23 Institut National de la Santé et de la Recherche Médicale (INSERM) Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
CN114380817B (zh) * 2020-10-21 2024-06-21 中国医学科学院药物研究所 苯并咪唑并2-氨基-1,3,4-噻二唑化合物及其制法和药物用途
CA3236877A1 (en) * 2021-11-08 2023-05-11 Ventus Therapeutics U.S., Inc. Heterocyclic compounds and uses thereof
WO2023222565A1 (en) 2022-05-16 2023-11-23 Institut National de la Santé et de la Recherche Médicale Methods for assessing the exhaustion of hematopoietic stems cells induced by chronic inflammation

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5304121A (en) 1990-12-28 1994-04-19 Boston Scientific Corporation Drug delivery system making use of a hydrogel polymer coating
US5886026A (en) 1993-07-19 1999-03-23 Angiotech Pharmaceuticals Inc. Anti-angiogenic compositions and methods of use
US6099562A (en) 1996-06-13 2000-08-08 Schneider (Usa) Inc. Drug coating with topcoat
AU1924099A (en) * 1997-12-18 1999-07-05 Lyonnaise Industrielle Pharmaceutique (Lipha) Piperazine derivatives useful as hypoglycemic agents
US6232320B1 (en) * 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
AU4231299A (en) 1998-06-04 1999-12-20 Abbott Laboratories Cell adhesion-inhibiting antinflammatory compounds
US6486158B1 (en) * 1998-08-14 2002-11-26 Cell Pathways, Inc. [4,5]-fused-3,6-disubstituted-pyridazines with sulfur-containing substituents in position three for the treatment of neoplasia
US6080747A (en) 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
WO2000075145A1 (en) * 1999-06-03 2000-12-14 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
JP2001354658A (ja) * 2000-06-15 2001-12-25 Taisho Pharmaceut Co Ltd ヒドロキシホルムアミジン化合物及びその塩並びにそれらを含む医薬
IL153246A0 (en) * 2000-06-28 2003-07-06 Astrazeneca Ab Substituted quinazoline derivatives and their use as inhibitors

Also Published As

Publication number Publication date
WO2004058753A8 (en) 2005-06-16
CN1665808A (zh) 2005-09-07
JP2006513192A (ja) 2006-04-20
CA2485429A1 (en) 2004-07-15
WO2004058753A1 (en) 2004-07-15
AU2003299472A1 (en) 2004-07-22
DE60335099D1 (de) 2011-01-05
IL165067A0 (en) 2005-12-18
US20040038992A1 (en) 2004-02-26
KR20050006237A (ko) 2005-01-15
EP2316834A1 (en) 2011-05-04
NO20045282L (no) 2005-02-07
EP1501829B1 (en) 2010-11-24
ATE489384T1 (de) 2010-12-15
MXPA04011048A (es) 2005-02-17
US7271179B2 (en) 2007-09-18
EP1501829A1 (en) 2005-02-02
RU2004135386A (ru) 2005-07-20
JP2010159306A (ja) 2010-07-22

Similar Documents

Publication Publication Date Title
JP4681302B2 (ja) チアジアゾールまたはオキサジアゾール、およびこれらの、ｊａｋプロテインキナーゼのインヒビターとしての使用
US7122552B2 (en) Inhibitors of JAK and CDK2 protein kinases
RU2403252C2 (ru) Азаиндолы, полезные в качестве ингибиторов jak и других протеинкиназ
JP5019612B2 (ja) Ｒｏｃｋの阻害剤として有用なアザインドールおよび他のプロテインキナーゼ
KR101075812B1 (ko) 단백질 키나제 억제제로서의 트리아졸로피리다진
US7855214B2 (en) Fused cyclic systems useful as inhibitors of TEC family protein kinases
JP2010195838A (ja) Ｊａｋおよび他のプロテインキナーゼのインヒビターとして有用な化合物
EP2325184A1 (en) Azaindoles useful as inhibitors of protein kinases
JP2007513172A (ja) 複素環式プロテインキナーゼインヒビターおよびその使用
KR20070090172A (ko) 단백질 키나아제의 억제제로서 유용한피라졸로[1,5-ａ]피리미딘
JP2012012417A (ja) タンパク質キナーゼのインヒビターとして有用なアザインドール
EP1603886B1 (en) 4-substituted-5-cyano-1h-pyrimidin-6-(thi)ones as gsk-3 inhibitors
JP2013064015A (ja) タンパク質キナーゼのインヒビターとして有用なアザインドール
EP2243781A1 (en) Pyrazolopyridine derivatives as inhibitors of JAK and CDK2 protein kinases
KR20070043813A (ko) 단백질 키나제의 억제제로서 유용한 아자인돌

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20060419

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20060419

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20091026

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20100122

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20100129

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20100426

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20100520

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20100921

A911 Transfer to examiner for re-examination before appeal (zenchi)

Free format text: JAPANESE INTERMEDIATE CODE: A911

Effective date: 20101208

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20110105

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20110204

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20140210

Year of fee payment: 3

LAPS Cancellation because of no payment of annual fees