JP2010508307A - Mapk/erkキナーゼ阻害剤 - Google Patents

Mapk/erkキナーゼ阻害剤 Download PDF

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Publication number
JP2010508307A
JP2010508307A JP2009534950A JP2009534950A JP2010508307A JP 2010508307 A JP2010508307 A JP 2010508307A JP 2009534950 A JP2009534950 A JP 2009534950A JP 2009534950 A JP2009534950 A JP 2009534950A JP 2010508307 A JP2010508307 A JP 2010508307A
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Japan
Prior art keywords
alkyl
hetero
cycloalkyl
bicycloaryl
aryl
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JP2009534950A
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English (en)
Japanese (ja)
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JP2010508307A5 (enExample
Inventor
アダムス、マーク、イー.
ドン、キン
カルドー、ステファン、ダヴリュ.
カヌーニ、トゥーフィク
ウォレス、マイケル、ビー.
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Takeda Pharmaceutical Co Ltd
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Takeda Pharmaceutical Co Ltd
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Publication of JP2010508307A publication Critical patent/JP2010508307A/ja
Publication of JP2010508307A5 publication Critical patent/JP2010508307A5/ja
Withdrawn legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • 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
    • 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
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • 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
    • 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
    • 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
    • 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
    • A61P9/10—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
    • 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
    • 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
    • C07D403/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
JP2009534950A 2006-10-31 2007-10-31 Mapk/erkキナーゼ阻害剤 Withdrawn JP2010508307A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US86374806P 2006-10-31 2006-10-31
PCT/US2007/083240 WO2008055236A2 (en) 2006-10-31 2007-10-31 Mapk/erk kinase inhibitors

Publications (2)

Publication Number Publication Date
JP2010508307A true JP2010508307A (ja) 2010-03-18
JP2010508307A5 JP2010508307A5 (enExample) 2010-12-16

Family

ID=39227092

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2009534950A Withdrawn JP2010508307A (ja) 2006-10-31 2007-10-31 Mapk/erkキナーゼ阻害剤

Country Status (5)

Country Link
US (1) US7943659B2 (enExample)
EP (2) EP2113500A1 (enExample)
JP (1) JP2010508307A (enExample)
CA (1) CA2667961A1 (enExample)
WO (1) WO2008055236A2 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013525324A (ja) * 2010-04-23 2013-06-20 バイエル・インテレクチユアル・プロパテイー・ゲー・エム・ベー・ハー 5−フルオロ−1−アルキル−3−フルオロアルキル−1h−ピラゾール−4−カルボニルクロリドおよびフルオリドの調製方法
JP2022510586A (ja) * 2018-11-20 2022-01-27 エヌフレクション セラピューティクス インコーポレイテッド 皮膚障害の処置のためのチエニル-アニリン化合物
JP2022513089A (ja) * 2018-11-20 2022-02-07 エヌフレクション セラピューティクス インコーポレイテッド 皮膚癌の処置のためのアリールアニリンおよびヘテロアリールアニリン化合物

Families Citing this family (26)

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US8022057B2 (en) * 2007-11-12 2011-09-20 Takeda Pharmaceutical Company Limited MAPK/ERK kinase inhibitors
EP2370568B1 (en) 2008-12-10 2017-07-19 Dana-Farber Cancer Institute, Inc. Mek mutations conferring resistance to mek inhibitors
KR20120117905A (ko) 2010-01-28 2012-10-24 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 프로테아좀 활성을 향상시키는 조성물 및 방법
CA2789696C (en) 2010-02-25 2017-11-07 Dana-Farber Cancer Institute, Inc. Braf mutations conferring resistance to braf inhibitors
EP2545187B1 (en) 2010-03-09 2018-09-05 Dana-Farber Cancer Institute, Inc. Methods of diagnosing and treating cancer in patients having or developing resistance to a first cancer therapy
TR201906779T4 (tr) 2011-05-12 2019-05-21 Proteostasis Therapeutics Inc Proteostaz regülatörleri.
WO2013109142A1 (en) 2012-01-16 2013-07-25 Stichting Het Nederlands Kanker Instituut Combined pdk and mapk/erk pathway inhibition in neoplasia
WO2013169858A1 (en) 2012-05-08 2013-11-14 The Broad Institute, Inc. Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy
WO2014071183A1 (en) 2012-11-02 2014-05-08 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Method of reducing adverse effects in a cancer patient undergoing treatment with a mek inhibitor
WO2014116228A1 (en) 2013-01-25 2014-07-31 President And Fellows Of Harvard College Usp14 inhibitors for treating or preventing viral infections
WO2015041534A1 (en) 2013-09-20 2015-03-26 Stichting Het Nederlands Kanker Instituut P90rsk in combination with raf/erk/mek
US9629851B2 (en) 2013-09-20 2017-04-25 Stitching Het Nederlands Kanker Institut—Antoni Van Leeuwenhoek Ziekenhuis ROCK in combination with MAPK pathway
WO2015073528A1 (en) 2013-11-12 2015-05-21 Proteostasis Therapeutics, Inc. Proteasome activity enhancing compounds
US20170027940A1 (en) 2014-04-10 2017-02-02 Stichting Het Nederlands Kanker Instituut Method for treating cancer
WO2015178770A1 (en) 2014-05-19 2015-11-26 Stichting Het Nederlands Kanker Instituut Compositions for cancer treatment
US20170114323A1 (en) 2014-06-19 2017-04-27 Whitehead Institute For Biomedical Research Uses of kinase inhibitors for inducing and maintaining pluripotency
WO2016187028A1 (en) * 2015-05-15 2016-11-24 Celgene Avilomics Research, Inc. Heteroaryl compounds, synthesis thereof, and intermediates thereto
WO2017058007A1 (en) 2015-10-01 2017-04-06 Stichting Het Nederlands Kanker Instituut-Antoni van Leeuwenhoek Ziekenhuis Histone deacetylase inhibitors for the use in the treatment of drug resistant melanoma
WO2017099591A1 (en) 2015-12-07 2017-06-15 Stichting Het Nederlands Kanker Instituut-Antoni van Leeuwenhoek Ziekenhuis Treatment of inhibitor resistant braf-mutant cancers
WO2017204626A1 (en) 2016-05-24 2017-11-30 Stichting Het Nederlands Kanker Instituut-Antoni van Leeuwenhoek Ziekenhuis Combination therapy - combined map2k4/map3k1 and mek/erk inhibition
ES2913213T3 (es) 2017-05-19 2022-06-01 Nflection Therapeutics Inc Compuestos heteroaromáticos de anilina condensados para el tratamiento de trastornos dérmicos
JP7212956B2 (ja) 2017-05-19 2023-01-26 エヌフレクション セラピューティクス インコーポレイテッド 皮膚障害の処置用のピロロピリジン-アニリン化合物
EP3883552B1 (en) 2018-11-20 2025-04-09 NFlection Therapeutics, Inc. Cyanoaryl-aniline compounds for treatment of dermal disorders
CN113473986B (zh) 2018-11-20 2024-10-11 恩福莱克逊治疗有限公司 用于治疗皮肤疾病萘啶酮苯胺化合物
CN117157065A (zh) 2021-01-21 2023-12-01 恩福莱克逊治疗有限公司 吡咯并吡啶-苯胺化合物的晶型
US12371667B2 (en) 2021-05-13 2025-07-29 Washington University Enhanced methods for inducing and maintaining naive human pluripotent stem cells

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US3710795A (en) 1970-09-29 1973-01-16 Alza Corp Drug-delivery device with stretched, rate-controlling membrane
US4044126A (en) 1972-04-20 1977-08-23 Allen & Hanburys Limited Steroidal aerosol compositions and process for the preparation thereof
GB1429184A (en) 1972-04-20 1976-03-24 Allen & Hanburys Ltd Physically anti-inflammatory steroids for use in aerosols
USRE28819E (en) 1972-12-08 1976-05-18 Syntex (U.S.A.) Inc. Dialkylated glycol compositions and medicament preparations containing same
US4328245A (en) 1981-02-13 1982-05-04 Syntex (U.S.A.) Inc. Carbonate diester solutions of PGE-type compounds
US4410545A (en) 1981-02-13 1983-10-18 Syntex (U.S.A.) Inc. Carbonate diester solutions of PGE-type compounds
US4358603A (en) 1981-04-16 1982-11-09 Syntex (U.S.A.) Inc. Acetal stabilized prostaglandin compositions
US4409239A (en) 1982-01-21 1983-10-11 Syntex (U.S.A.) Inc. Propylene glycol diester solutions of PGE-type compounds
AU2004272457A1 (en) 2003-09-16 2005-03-24 Banyu Pharmaceutical Co., Ltd. Novel indolopyrrolocarbazole derivative with antitumor activity
MXPA06013250A (es) 2004-05-14 2007-02-28 Abbott Lab Inhibidores de quinasa como agentes terapeuticos.
ES2330872T3 (es) 2004-12-01 2009-12-16 Merck Serono Sa Derivados de (1,2,4)triazolo(4,3-a)piridina para el tratamiento de enfermedades hiperproliferativas.
US7429667B2 (en) 2005-01-20 2008-09-30 Ardea Biosciences, Inc. Phenylamino isothiazole carboxamidines as MEK inhibitors
NZ567140A (en) 2005-10-07 2011-09-30 Exelixis Inc Azetidines as MEK inhibitors for the treatment of proliferative diseases

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013525324A (ja) * 2010-04-23 2013-06-20 バイエル・インテレクチユアル・プロパテイー・ゲー・エム・ベー・ハー 5−フルオロ−1−アルキル−3−フルオロアルキル−1h−ピラゾール−4−カルボニルクロリドおよびフルオリドの調製方法
JP2022510586A (ja) * 2018-11-20 2022-01-27 エヌフレクション セラピューティクス インコーポレイテッド 皮膚障害の処置のためのチエニル-アニリン化合物
JP2022513089A (ja) * 2018-11-20 2022-02-07 エヌフレクション セラピューティクス インコーポレイテッド 皮膚癌の処置のためのアリールアニリンおよびヘテロアリールアニリン化合物
JP7546297B2 (ja) 2018-11-20 2024-09-06 エヌフレクション セラピューティクス インコーポレイテッド 皮膚障害の処置のためのチエニル-アニリン化合物
JP7576799B2 (ja) 2018-11-20 2024-11-01 エヌフレクション セラピューティクス インコーポレイテッド 皮膚癌の処置のためのアリールアニリンおよびヘテロアリールアニリン化合物

Also Published As

Publication number Publication date
EP2113500A1 (en) 2009-11-04
WO2008055236A3 (en) 2008-10-09
WO2008055236A2 (en) 2008-05-08
US20080188453A1 (en) 2008-08-07
US7943659B2 (en) 2011-05-17
EP2089359A2 (en) 2009-08-19
CA2667961A1 (en) 2008-05-08

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