JP7229257B2 - Ｇｃｎ２阻害剤およびその使用 - Google Patents

Ｇｃｎ２阻害剤およびその使用 Download PDF

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JP7229257B2
JP7229257B2 JP2020541383A JP2020541383A JP7229257B2 JP 7229257 B2 JP7229257 B2 JP 7229257B2 JP 2020541383 A JP2020541383 A JP 2020541383A JP 2020541383 A JP2020541383 A JP 2020541383A JP 7229257 B2 JP7229257 B2 JP 7229257B2
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ring
compound
pharmaceutically acceptable
compounds
acceptable salt
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JP2021512079A5 (OSRAM
JP2021512079A (ja
Inventor
アンドリュー ベイリー，
マシュー ブライク，
ジーン－ダミアン シャリエ，
ジェイムズ ドッド，
スティーブン デュラント，
メレディス スザンヌ イーノ，
イ ハリディ， ゴルカ エチェバリア
サイモン エバリット，
ダミアン フレイス，
シャジア ケリー，
ロナルド ネグテル，
イゴール モシャルキン，
マイケル モルティモア，
キリ ノース，
フィリポス ポリシス，
ロバート プリン，
アリステア ラザフォード，
ピエール－アンリ ストーク，
ヘザー クレア ツウィン，
ユファン シャオ，
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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Publication of JP2021512079A publication Critical patent/JP2021512079A/ja
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Priority to JP2023020523A priority Critical patent/JP7703586B2/ja
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Publication of JP7229257B2 publication Critical patent/JP7229257B2/ja
Priority to JP2025107210A priority patent/JP2025129210A/ja
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed 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
    • A61K31/495—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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines 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
    • A61K31/495—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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed 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
    • A61K31/535—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
    • 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
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • 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
    • 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
    • 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
    • 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
    • A61P9/10—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
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2020541383A 2018-01-29 2019-01-28 Ｇｃｎ２阻害剤およびその使用 Active JP7229257B2 (ja)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2023020523A JP7703586B2 (ja) 2018-01-29 2023-02-14 Ｇｃｎ２阻害剤およびその使用
JP2025107210A JP2025129210A (ja) 2018-01-29 2025-06-25 Ｇｃｎ２阻害剤およびその使用

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862623299P 2018-01-29 2018-01-29
US62/623,299 2018-01-29
PCT/US2019/015469 WO2019148132A1 (en) 2018-01-29 2019-01-28 Gcn2 inhibitors and uses thereof

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JP2023020523A Division JP7703586B2 (ja) 2018-01-29 2023-02-14 Ｇｃｎ２阻害剤およびその使用

Publications (3)

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JP2021512079A JP2021512079A (ja) 2021-05-13
JP2021512079A5 JP2021512079A5 (OSRAM) 2022-02-07
JP7229257B2 true JP7229257B2 (ja) 2023-02-28

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JP2020541383A Active JP7229257B2 (ja) 2018-01-29 2019-01-28 Ｇｃｎ２阻害剤およびその使用
JP2023020523A Active JP7703586B2 (ja) 2018-01-29 2023-02-14 Ｇｃｎ２阻害剤およびその使用
JP2025107210A Pending JP2025129210A (ja) 2018-01-29 2025-06-25 Ｇｃｎ２阻害剤およびその使用

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JP2025107210A Pending JP2025129210A (ja) 2018-01-29 2025-06-25 Ｇｃｎ２阻害剤およびその使用

Country Status (15)

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US (2) US10988477B2 (OSRAM)
EP (2) EP4616913A3 (OSRAM)
JP (3) JP7229257B2 (OSRAM)
KR (1) KR20200116481A (OSRAM)
CN (2) CN111918651B (OSRAM)
AR (1) AR114235A1 (OSRAM)
AU (2) AU2019211485B2 (OSRAM)
BR (1) BR112020015328A2 (OSRAM)
CA (1) CA3089762A1 (OSRAM)
ES (1) ES3055657T3 (OSRAM)
IL (2) IL276095B2 (OSRAM)
MX (1) MX2020007799A (OSRAM)
SG (1) SG11202006701TA (OSRAM)
TW (1) TWI816742B (OSRAM)
WO (1) WO2019148132A1 (OSRAM)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA202092442A3 (ru) 2016-06-07 2021-08-31 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
WO2018172984A1 (en) 2017-03-23 2018-09-27 Jacobio Pharmaceuticals Co., Ltd. Novel heterocyclic derivatives useful as shp2 inhibitors
EP4616913A3 (en) 2018-01-29 2025-12-10 Merck Patent GmbH Gcn2 inhibitors and uses thereof
JP7377207B2 (ja) 2018-01-29 2023-11-09 メルク パテント ゲーエムベーハー Ｇｃｎ２阻害剤およびその使用
MX2021000293A (es) 2018-07-09 2021-07-15 Boehringer Ingelheim Animal Health Usa Inc Compuestos heterociclicos antihelminticos.
WO2020010451A1 (en) * 2018-07-10 2020-01-16 Trillium Therapeutics Inc. Heteroaromatic-fused imidazolyl amides, compositions and uses thereof as sting agonists
CN112839935A (zh) 2018-09-26 2021-05-25 北京加科思新药研发有限公司 可用作shp2抑制剂的新型杂环衍生物
JP7637630B2 (ja) 2019-03-19 2025-02-28 ベーリンガー インゲルハイム フェトメディカ ゲーエムベーハー 駆虫性アザベンゾチオフェンおよびアザベンゾフラン化合物
US11116737B1 (en) 2020-04-10 2021-09-14 University Of Georgia Research Foundation, Inc. Methods of using probenecid for treatment of coronavirus infections
CN111548356B (zh) * 2020-05-20 2022-05-17 无锡合全药业有限公司 叔丁基-1,8-二氧杂-4,11-二氮杂螺[5.6]十二烷-11-甲酸基酯制法
PH12022553222A1 (en) 2020-05-29 2024-02-12 Boehringer Ingelheim Animal Health Usa Inc Anthelmintic heterocyclic compounds
GB202008749D0 (en) 2020-06-09 2020-07-22 Ip2Ipo Innovations Ltd Novel compounds
WO2022020114A2 (en) 2020-07-10 2022-01-27 Ting Therapeutics Llc Methods for the prevention and treatment of hearing loss
JP2023546768A (ja) * 2020-07-20 2023-11-08 ザ トラスティース オブ コロンビア ユニバーシティ イン ザ シティ オブ ニューヨーク トランスサイレチン四量体を安定化するレチノール結合タンパク質４の二重特異性アンタゴニスト、その調製、および一般的な加齢関連合併症の治療における使用
US20240083897A1 (en) * 2021-01-22 2024-03-14 Hibercell, Inc. Gcn2 modulating compounds and uses thereof
GB202104635D0 (en) 2021-03-31 2021-05-12 Imperial College Innovations Ltd Methods and compositions for identifying and treating GCN2-dependent cancers
AR127495A1 (es) 2021-11-01 2024-01-31 Boehringer Ingelheim Vetmedica Gmbh Compuestos de pirrolopiridazina como antihelmínticos
GB202118096D0 (en) 2021-12-14 2022-01-26 Ip2Ipo Innovations Ltd Novel compounds
CA3252213A1 (en) 2022-05-11 2023-11-16 Ip2Ipo Innovations Limited GCN2 INHIBITOR
US20240124450A1 (en) 2022-09-21 2024-04-18 Pfizer Inc. Novel SIK Inhibitors
CN116768868B (zh) * 2023-08-15 2023-12-08 云南省药物研究所 一种哒嗪酮硫代衍生物及其制备方法和应用
WO2025070690A1 (ja) 2023-09-29 2025-04-03 第一三共株式会社 ３－フェニルプロピルアミン誘導体
KR20250122240A (ko) 2024-02-06 2025-08-13 한미약품 주식회사 신규한 함질소 헤테로고리 유도체 및 이의 용도

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006528983A (ja) 2003-05-15 2006-12-28 アークル インコーポレイテッド ｐ３８の阻害物質としてのイミダゾチアゾール類およびイミダゾオキサゾール誘導体
JP2007519662A (ja) 2004-01-22 2007-07-19 ノバルティス アクチエンゲゼルシャフト タンパク質キナーゼ依存性疾患の処置に使用するためのピラゾロ［１，５−ａ］ピリミジン−７−イル−アミン誘導体
JP2008519059A (ja) 2004-11-04 2008-06-05 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 プロテインキナーゼのインヒビターとして有用なピラゾロ［１，５−α］ピリミジン
JP2009502734A (ja) 2005-07-29 2009-01-29 アステラス製薬株式会社 Ｌｃｋ阻害剤としての縮合複素環
JP2010502716A (ja) 2006-09-07 2010-01-28 バイオジェン・アイデック・エムエイ・インコーポレイテッド インターロイキン１受容体関連キナーゼの調節物質
JP2010504927A (ja) 2006-09-28 2010-02-18 ノバルティス アーゲー ピラゾロ［１，５−ａ］ピリミジン誘導体およびそれらの治療的使用
JP2010526120A (ja) 2007-05-09 2010-07-29 ノバルティス アーゲー Ｐｉ３ｋ脂質キナーゼ阻害剤としての置換イミダゾピリダジン
JP2011520887A (ja) 2008-05-13 2011-07-21 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縮合窒素含有ヘテロ環およびその組成物

Family Cites Families (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5650270A (en) 1982-02-01 1997-07-22 Northeastern University Molecular analytical release tags and their use in chemical analysis
US4709016A (en) 1982-02-01 1987-11-24 Northeastern University Molecular analytical release tags and their use in chemical analysis
US4650750A (en) 1982-02-01 1987-03-17 Giese Roger W Method of chemical analysis employing molecular release tag compounds
US5516931A (en) 1982-02-01 1996-05-14 Northeastern University Release tag compounds producing ketone signal groups
EA006227B1 (ru) 1999-12-10 2005-10-27 Пфайзер Продактс Инк. СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА
PE20020354A1 (es) 2000-09-01 2002-06-12 Novartis Ag Compuestos de hidroxamato como inhibidores de histona-desacetilasa (hda)
US7071189B2 (en) 2001-04-27 2006-07-04 Zenyaku Kogyo Kabushiki Kaisha Heterocyclic compound and antitumor agent containing the same as active ingredient
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
GB0212049D0 (en) 2002-05-24 2002-07-03 Merck Sharp & Dohme Therapeutic agents
WO2004019973A1 (en) 2002-08-14 2004-03-11 Atugen Ag Use of protein kinase n beta
JP2006523237A (ja) 2003-04-03 2006-10-12 セマフォア ファーマシューティカルズ， インコーポレイテッド Ｐｉ−３キナーゼインヒビタープロドラッグ
US7425553B2 (en) 2003-05-30 2008-09-16 Gemin X Pharmaceuticals Canada Inc. Triheterocyclic compounds, compositions, and methods for treating cancer or viral diseases
CA2531069A1 (en) 2003-07-03 2005-01-27 The Trustees Of The University Of Pennsylvania Inhibition of syk kinase expression
ES2372694T3 (es) 2003-10-15 2012-01-25 OSI Pharmaceuticals, LLC Inhibidores de tirosina cinasa de imidazo[1,5-a]pirazina.
EP1761540B1 (en) 2004-05-13 2016-09-28 Icos Corporation Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta
TWI309240B (en) 2004-09-17 2009-05-01 Hoffmann La Roche Anti-ox40l antibodies
WO2006070943A1 (ja) * 2004-12-28 2006-07-06 Takeda Pharmaceutical Company Limited 縮合イミダゾール化合物およびその用途
JP4801096B2 (ja) 2005-01-19 2011-10-26 ライジェル ファーマシューティカルズ， インコーポレイテッド ２，４−ピリミジンジアミン化合物のプロドラッグおよびそれらの使用
AU2006230099B2 (en) 2005-03-25 2012-04-19 Gitr, Inc. GITR binding molecules and uses therefor
EP2757099B1 (en) 2005-05-12 2017-08-23 AbbVie Bahamas Limited Apoptosis promoters
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
CA2612241C (en) 2005-07-01 2018-11-06 Medarex, Inc. Human monoclonal antibodies to programmed death ligand 1 (pd-l1)
US7402325B2 (en) 2005-07-28 2008-07-22 Phoenix Biotechnology, Inc. Supercritical carbon dioxide extract of pharmacologically active components from Nerium oleander
AU2006302179C1 (en) 2005-10-07 2013-06-20 Exelixis, Inc. N- (3-amino-quinoxalin-2-yl) -sulfonamide derivatives and their use as phosphatidylinositol 3-kinase inhibitors
US7528143B2 (en) 2005-11-01 2009-05-05 Targegen, Inc. Bi-aryl meta-pyrimidine inhibitors of kinases
CN103214484B (zh) 2005-12-13 2016-07-06 因塞特控股公司 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
RU2439074C2 (ru) 2006-04-26 2012-01-10 Ф. Хоффманн-Ля Рош Аг ПРОИЗВОДНОЕ ТИЕНО[3,2-d]ПИРИМИДИНА В КАЧЕСТВЕ ИНГИБИТОРА ФОСФАТИДИЛИНОЗИТОЛ-3-КИНАЗЫ (РI3К)
PL2526933T3 (pl) 2006-09-22 2015-08-31 Pharmacyclics Llc Inhibitory kinazy tyrozynowej Brutona
KR20090075714A (ko) * 2006-10-30 2009-07-08 노파르티스 아게 소염제로서의 헤테로시클릭 화합물
EP2114941B1 (en) * 2006-12-22 2015-03-25 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
JP5442449B2 (ja) 2006-12-22 2014-03-12 アステックス、セラピューティックス、リミテッド 新規化合物
US8486941B2 (en) 2007-03-12 2013-07-16 Ym Biosciences Australia Pty Ltd Phenyl amino pyrimidine compounds and uses thereof
US8394794B2 (en) 2007-03-23 2013-03-12 Regents Of The University Of Minnesota Therapeutic compounds
EP1987839A1 (en) 2007-04-30 2008-11-05 I.N.S.E.R.M. Institut National de la Sante et de la Recherche Medicale Cytotoxic anti-LAG-3 monoclonal antibody and its use in the treatment or prevention of organ transplant rejection and autoimmune disease
PE20090717A1 (es) 2007-05-18 2009-07-18 Smithkline Beecham Corp Derivados de quinolina como inhibidores de la pi3 quinasa
CN101801413A (zh) 2007-07-12 2010-08-11 托勒克斯股份有限公司 采用gitr结合分子的联合疗法
PE20090506A1 (es) * 2007-07-26 2009-05-28 Novartis Ag DERIVADOS DE IMIDAZO-[1,2-b]-PIRIDAZIN COMO INHIBIDORES DE ALK5 Y/O ALK4
EP2044949A1 (en) 2007-10-05 2009-04-08 Immutep Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response
CN101932325B (zh) 2007-11-30 2014-05-28 新联基因公司 Ido抑制剂
TWI444382B (zh) 2008-03-11 2014-07-11 Incyte Corp 作為ｊａｋ抑制劑之氮雜環丁烷及環丁烷衍生物
US20110176972A1 (en) 2008-05-29 2011-07-21 Saint-Gobain Centre De Recherches et D'Etudes Eur Cellular structure containing aluminium titanate
US8338439B2 (en) 2008-06-27 2012-12-25 Celgene Avilomics Research, Inc. 2,4-disubstituted pyrimidines useful as kinase inhibitors
AR072999A1 (es) 2008-08-11 2010-10-06 Medarex Inc Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos
EP4209510B1 (en) 2008-12-09 2024-01-31 F. Hoffmann-La Roche AG Anti-pd-l1 antibodies and their use to enhance t-cell function
CA2755285C (en) 2009-03-20 2014-02-11 Yunxin Y. Bo Inhibitors of pi3 kinase
PT3023438T (pt) 2009-09-03 2020-05-08 Merck Sharp & Dohme Anticorpos anti-gitr
US8722720B2 (en) 2009-10-28 2014-05-13 Newlink Genetics Corporation Imidazole derivatives as IDO inhibitors
CA2778949C (en) * 2009-10-30 2018-02-27 Janssen Pharmaceutica Nv Imidazo[1,2-b]pyridazine derivatives and their use as pde10 inhibitors
EP2949670B1 (en) 2009-12-10 2019-02-27 F. Hoffmann-La Roche AG Antibodies binding preferentially human csf1r extracellular domain 4 and their use
PH12018501083A1 (en) 2010-03-04 2019-02-18 Macrogenics Inc Antibodies reactive with b7-h3, immunologically active fragments thereof and uses thereof
JP5989547B2 (ja) 2010-03-05 2016-09-07 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト ヒトｃｓｆ−１ｒに対する抗体及びその使用
KR101656548B1 (ko) 2010-03-05 2016-09-09 에프. 호프만-라 로슈 아게 인간 ｃｓｆ-1ｒ에 대한 항체 및 이의 용도
SMT201900074T1 (it) 2010-05-04 2019-02-28 Five Prime Therapeutics Inc Anticorpi che legano csf1r
SG10201912092VA (en) 2010-09-09 2020-02-27 Pfizer 4-1bb binding molecules
PH12013501201A1 (en) 2010-12-09 2013-07-29 Univ Pennsylvania Use of chimeric antigen receptor-modified t cells to treat cancer
US8673905B2 (en) * 2011-03-17 2014-03-18 Hoffmann-La Roche Inc. Imidazo pyrazines
NO2694640T3 (OSRAM) 2011-04-15 2018-03-17
SI2699264T1 (en) 2011-04-20 2018-08-31 Medimmune Llc Antibodies and other molecules that bind b7-h1 and pd-1
US9624298B2 (en) 2011-11-28 2017-04-18 Merck Patent Gmbh Anti-PD-L1 antibodies and uses thereof
EP2791174B1 (en) 2011-12-15 2018-02-28 F. Hoffmann-La Roche AG Antibodies against human csf-1r and uses thereof
RU2548363C2 (ru) * 2012-01-25 2015-04-20 Общество с ограниченной ответственностью "Асинэкс Медхим." СЕЛЕКТИВНЫЕ ИНГИБИТОРЫ Haspin киназы
CN104093740B (zh) 2012-02-06 2018-01-09 弗·哈夫曼-拉罗切有限公司 使用csf1r抑制剂的组合物和方法
CN104114558B (zh) * 2012-02-21 2016-10-26 默克专利股份公司 呋喃并吡啶衍生物
ES2674451T3 (es) * 2012-02-21 2018-06-29 Merck Patent Gmbh 2-amino-[1,2,4]triazolo[1,5-a] pirazinas 8-sustituidos como inhibidores de la SYK tirosina quinasa e inhibidores de la serina quinasa GCN2
JP6049768B2 (ja) * 2012-03-07 2016-12-21 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Ｍｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ トリアゾロピラジン誘導体
AR090263A1 (es) 2012-03-08 2014-10-29 Hoffmann La Roche Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma
KR20150018533A (ko) 2012-05-11 2015-02-23 파이브 프라임 테라퓨틱스, 인크. 콜로니 자극 인자 1 수용체(csf1r)에 결속하는 항체들에 의한 질병 상태의 치료 방법
UY34887A (es) 2012-07-02 2013-12-31 Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware Optimización de anticuerpos que se fijan al gen de activación de linfocitos 3 (lag-3) y sus usos
CN104684582A (zh) 2012-08-31 2015-06-03 戊瑞治疗有限公司 用结合群落刺激因子1受体(csf1r)的抗体治疗病状的方法
US9617266B2 (en) * 2013-03-05 2017-04-11 Merck Patent Gmbh Imidazopyrimidine derivatives
WO2014200882A1 (en) * 2013-06-11 2014-12-18 Janssen Pharmaceutica Nv PDE10a INHIBITORS FOR THE TREATMENT OF TYPE II DIABETES
CA2965741C (en) 2014-11-03 2022-05-17 Iomet Pharma Ltd Pharmaceutical compound
EP3307728A4 (en) * 2015-06-12 2019-07-17 Dana Farber Cancer Institute, Inc. COMBINATION THERAPY OF TRANSCRIPTION INHIBITORS AND CHINESE INHIBITORS
EP3565817B1 (en) * 2017-01-06 2023-06-07 The Johns Hopkins University Small molecule inhibitors of neutral sphingomyelinase 2 (nsmase2) for the treatment of neurodegenerative diseases
EP4616913A3 (en) 2018-01-29 2025-12-10 Merck Patent GmbH Gcn2 inhibitors and uses thereof
JP7377207B2 (ja) 2018-01-29 2023-11-09 メルク パテント ゲーエムベーハー Ｇｃｎ２阻害剤およびその使用

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006528983A (ja) 2003-05-15 2006-12-28 アークル インコーポレイテッド ｐ３８の阻害物質としてのイミダゾチアゾール類およびイミダゾオキサゾール誘導体
JP2007519662A (ja) 2004-01-22 2007-07-19 ノバルティス アクチエンゲゼルシャフト タンパク質キナーゼ依存性疾患の処置に使用するためのピラゾロ［１，５−ａ］ピリミジン−７−イル−アミン誘導体
JP2008519059A (ja) 2004-11-04 2008-06-05 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 プロテインキナーゼのインヒビターとして有用なピラゾロ［１，５−α］ピリミジン
JP2009502734A (ja) 2005-07-29 2009-01-29 アステラス製薬株式会社 Ｌｃｋ阻害剤としての縮合複素環
JP2010502716A (ja) 2006-09-07 2010-01-28 バイオジェン・アイデック・エムエイ・インコーポレイテッド インターロイキン１受容体関連キナーゼの調節物質
JP2010504927A (ja) 2006-09-28 2010-02-18 ノバルティス アーゲー ピラゾロ［１，５−ａ］ピリミジン誘導体およびそれらの治療的使用
JP2010526120A (ja) 2007-05-09 2010-07-29 ノバルティス アーゲー Ｐｉ３ｋ脂質キナーゼ阻害剤としての置換イミダゾピリダジン
JP2011520887A (ja) 2008-05-13 2011-07-21 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縮合窒素含有ヘテロ環およびその組成物

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