JP7504791B2 - Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩 - Google Patents

Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩 Download PDF

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JP7504791B2
JP7504791B2 JP2020517516A JP2020517516A JP7504791B2 JP 7504791 B2 JP7504791 B2 JP 7504791B2 JP 2020517516 A JP2020517516 A JP 2020517516A JP 2020517516 A JP2020517516 A JP 2020517516A JP 7504791 B2 JP7504791 B2 JP 7504791B2
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compound
salt
phenyl
cancer
formula
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JP2020535168A5 (https=
JP2020535168A (ja
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ジョンジアン・ジア
ヨンジョン・ウー
ヨンチュン・パン
ジアチェン・チョウ
リー・チュン
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Incyte Corp
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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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C57/00—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms
    • C07C57/02—Unsaturated compounds having carboxyl groups bound to acyclic carbon atoms with only carbon-to-carbon double bonds as unsaturation
    • C07C57/13—Dicarboxylic acids
    • C07C57/145—Maleic acid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2020517516A 2017-09-27 2018-09-26 Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩 Active JP7504791B2 (ja)

Priority Applications (2)

Application Number Priority Date Filing Date Title
JP2024014546A JP7639195B2 (ja) 2017-09-27 2024-02-02 Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩
JP2025025024A JP2025093936A (ja) 2017-09-27 2025-02-19 Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201762564070P 2017-09-27 2017-09-27
US62/564,070 2017-09-27
US201862714196P 2018-08-03 2018-08-03
US62/714,196 2018-08-03
PCT/US2018/052925 WO2019067594A1 (en) 2017-09-27 2018-09-26 Salts of pyrrolotriazine derivatives useful as tam inhibitors

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JP2024014546A Division JP7639195B2 (ja) 2017-09-27 2024-02-02 Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩

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JP2020535168A JP2020535168A (ja) 2020-12-03
JP2020535168A5 JP2020535168A5 (https=) 2021-10-28
JP7504791B2 true JP7504791B2 (ja) 2024-06-24

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JP2020517516A Active JP7504791B2 (ja) 2017-09-27 2018-09-26 Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩
JP2024014546A Active JP7639195B2 (ja) 2017-09-27 2024-02-02 Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩
JP2025025024A Pending JP2025093936A (ja) 2017-09-27 2025-02-19 Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩

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JP2024014546A Active JP7639195B2 (ja) 2017-09-27 2024-02-02 Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩
JP2025025024A Pending JP2025093936A (ja) 2017-09-27 2025-02-19 Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩

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US (4) US10633387B2 (https=)
EP (2) EP3988552A1 (https=)
JP (3) JP7504791B2 (https=)
KR (1) KR102739325B1 (https=)
CN (2) CN111386273B (https=)
AU (2) AU2018342471B2 (https=)
CA (1) CA3077308A1 (https=)
CL (2) CL2020000791A1 (https=)
CO (1) CO2020005009A2 (https=)
CR (1) CR20200179A (https=)
CY (1) CY1124952T1 (https=)
DK (1) DK3687996T3 (https=)
EC (1) ECSP20021655A (https=)
ES (1) ES2904458T3 (https=)
GE (2) GEAP202215322A (https=)
HU (1) HUE057190T2 (https=)
IL (1) IL273579B2 (https=)
JO (1) JOP20200081B1 (https=)
LT (1) LT3687996T (https=)
MA (1) MA50655B1 (https=)
MD (1) MD3687996T2 (https=)
MX (1) MX2020003375A (https=)
MY (1) MY208007A (https=)
PE (1) PE20210002A1 (https=)
PH (1) PH12020550143A1 (https=)
PL (1) PL3687996T3 (https=)
PT (1) PT3687996T (https=)
RS (1) RS62872B1 (https=)
SA (1) SA520411638B1 (https=)
SG (1) SG11202002821UA (https=)
SI (1) SI3687996T1 (https=)
SM (1) SMT202200011T1 (https=)
TW (1) TWI821200B (https=)
WO (1) WO2019067594A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2025093936A (ja) * 2017-09-27 2025-06-24 インサイト・コーポレイション Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2017035366A1 (en) 2015-08-26 2017-03-02 Incyte Corporation Pyrrolopyrimidine derivatives as tam inhibitors
JP7071917B2 (ja) 2015-12-09 2022-05-19 カデント セラピューティクス，インコーポレーテッド ヘテロ芳香族ｎｍｄａ受容体モジュレーターおよびその使用
KR102483020B1 (ko) 2016-03-28 2023-01-04 인사이트 코포레이션 Tam 저해제로서의 피롤로트리아진 화합물
US11274107B2 (en) 2016-12-22 2022-03-15 Cadent Therapeutics, Inc. NMDA receptor modulators and uses thereof
AR117600A1 (es) 2018-06-29 2021-08-18 Incyte Corp Formulaciones de un inhibidor de axl / mer
AR115905A1 (es) 2018-08-03 2021-03-10 Cadent Therapeutics Inc 5-(3-cloro-4-fluorofenil)-7-ciclopropil-3-(2-(3-fluoro-3-metilazetidin-1-il)-2-oxoetil)-3,7-dihidro-4h-pirrolo[2,3-d]pirimidin-4-ona como modulador de los receptores de nmda
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
WO2021178779A1 (en) * 2020-03-06 2021-09-10 Incyte Corporation Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors
WO2022007921A1 (zh) * 2020-07-10 2022-01-13 北京范恩柯尔生物科技有限公司 三嗪类化合物及其组合物和用途
CN115028648B (zh) * 2021-03-03 2024-08-30 武汉誉祥医药科技有限公司 三并环化合物及其药物组合物和应用
JP7802077B2 (ja) * 2021-07-13 2026-01-19 日本曹達株式会社 ウラシル化合物の製造方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019510043A (ja) 2016-03-28 2019-04-11 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｔａｍ阻害剤としてのピロロトリアジン化合物
JP2021529765A (ja) 2018-06-29 2021-11-04 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ａｘｌ／ｍｅｒ阻害剤の製剤

Family Cites Families (135)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5179017A (en) 1980-02-25 1993-01-12 The Trustees Of Columbia University In The City Of New York Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
US4399216A (en) 1980-02-25 1983-08-16 The Trustees Of Columbia University Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
US4634665A (en) 1980-02-25 1987-01-06 The Trustees Of Columbia University In The City Of New York Processes for inserting DNA into eucaryotic cells and for producing proteinaceous materials
US5156840A (en) 1982-03-09 1992-10-20 Cytogen Corporation Amine-containing porphyrin derivatives
US5057313A (en) 1986-02-25 1991-10-15 The Center For Molecular Medicine And Immunology Diagnostic and therapeutic antibody conjugates
JP3101690B2 (ja) 1987-03-18 2000-10-23 エス・ビィ・２・インコーポレイテッド 変性抗体の、または変性抗体に関する改良
US5530101A (en) 1988-12-28 1996-06-25 Protein Design Labs, Inc. Humanized immunoglobulins
IL162181A (en) 1988-12-28 2006-04-10 Pdl Biopharma Inc A method of producing humanized immunoglubulin, and polynucleotides encoding the same
DE3920358A1 (de) 1989-06-22 1991-01-17 Behringwerke Ag Bispezifische und oligospezifische, mono- und oligovalente antikoerperkonstrukte, ihre herstellung und verwendung
JPH0395163A (ja) 1989-09-08 1991-04-19 Daicel Chem Ind Ltd ２．２．４．４．６―ペンタメチル―２．３．４．５―テトラヒドロピリミジンの製造法
US5859205A (en) 1989-12-21 1999-01-12 Celltech Limited Humanised antibodies
EP1400536A1 (en) 1991-06-14 2004-03-24 Genentech Inc. Method for making humanized antibodies
ATE207080T1 (de) 1991-11-25 2001-11-15 Enzon Inc Multivalente antigen-bindende proteine
US5714350A (en) 1992-03-09 1998-02-03 Protein Design Labs, Inc. Increasing antibody affinity by altering glycosylation in the immunoglobulin variable region
US5827690A (en) 1993-12-20 1998-10-27 Genzyme Transgenics Corporatiion Transgenic production of antibodies in milk
US5731168A (en) 1995-03-01 1998-03-24 Genentech, Inc. Method for making heteromultimeric polypeptides
US5869046A (en) 1995-04-14 1999-02-09 Genentech, Inc. Altered polypeptides with increased half-life
ES2176484T3 (es) 1995-08-18 2002-12-01 Morphosys Ag Bancos de proteinas/(poli)peptidos.
US20020077461A1 (en) 1996-04-24 2002-06-20 Soren Bjorn Pharmaceutical formulation
MXPA02002938A (es) 1999-09-17 2004-12-06 Abbott Gmbh & Co Kg Inhibidores de cinasa como agentes agentes terapeuticos.
KR100786927B1 (ko) 2000-06-28 2007-12-17 스미스클라인비이참피이엘시이 습식 분쇄방법
EA010184B1 (ru) 2001-04-06 2008-06-30 Уайт Применение противоопухолевых комбинаций рапамицина с гемцитабином или 5-фторурацилом
GB0221697D0 (en) 2002-09-18 2002-10-30 Unilever Plc Novel compouds and their uses
AU2003272175A1 (en) 2002-10-21 2004-05-04 Aprea Ab Reactivation of wild type p53 in human tumour cells by a low molecular weight compound
CA2512729C (en) 2003-01-09 2014-09-16 Macrogenics, Inc. Identification and engineering of antibodies with variant fc regions and methods of using same
WO2004065416A2 (en) 2003-01-16 2004-08-05 Genentech, Inc. Synthetic antibody phage libraries
WO2004072266A2 (en) 2003-02-13 2004-08-26 Kalobios Inc. Antibody affinity engineering by serial epitope-guided complementarity replacement
ATE454886T1 (de) 2003-03-26 2010-01-15 Egalet As Matrixzubereitungen für die kontrollierte darreichung von arzneistoffen
EP1639014B1 (en) 2003-06-13 2010-09-22 Biogen Idec MA Inc. Aglycosyl anti-cd154 (cd40 ligand) antibodies and uses thereof
AU2004266159A1 (en) 2003-08-22 2005-03-03 Biogen Idec Ma Inc. Improved antibodies having altered effector function and methods for making the same
WO2005025515A2 (en) 2003-09-12 2005-03-24 California Institute Of Technology Proteasome pathway inhibitors and related methods
EP2168968B1 (en) 2004-04-02 2017-08-23 OSI Pharmaceuticals, LLC 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors
UY28931A1 (es) 2004-06-03 2005-12-30 Bayer Pharmaceuticals Corp Derivados de pirrolotriazina utiles para tratar trastornos hiper-proliferativos y enfermedades asociadas con angiogenesis
TW200613306A (en) 2004-07-20 2006-05-01 Osi Pharm Inc Imidazotriazines as protein kinase inhibitors
UY29177A1 (es) 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
AU2005309019A1 (en) 2004-11-24 2006-06-01 Novartis Ag Combinations of JAK inhibitors and at least one of Bcr-Abl, Flt-3, FAK or RAF kinase inhibitors
ES2365869T3 (es) 2005-11-17 2011-10-11 OSI Pharmaceuticals, LLC COMPUESTOS BICÍCLICOS FUSIONADOS INHIBIDORES DE LA mTOR.
PE20070855A1 (es) 2005-12-02 2007-10-14 Bayer Pharmaceuticals Corp Derivados de 4-amino-pirrolotriazina sustituida como inhibidores de quinasas
WO2007064931A2 (en) 2005-12-02 2007-06-07 Bayer Healthcare Llc Substituted 4-amino-pyrrolotriazine derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis
SG10202003901UA (en) 2005-12-13 2020-05-28 Incyte Holdings Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
WO2007070872A1 (en) 2005-12-15 2007-06-21 Rigel Pharmaceuticals, Inc. Kinase inhibitors and their uses
AU2007238690B2 (en) 2006-04-12 2013-05-02 Vertex Pharmaceuticals Incorporated 4, 5-dihydro- [1, 2, 4] triazolo [4, 3-f] pteridines as protein kinase PLK1 inhibitors for the treatment of proliferative disorders
CA2649288C (en) 2006-04-19 2015-11-24 Novartis Ag 6-o-substituted benzoxazole and benzothiazole compounds and methods of inhibiting csf-1r signaling
WO2007125315A2 (en) 2006-04-25 2007-11-08 Astex Therapeutics Limited Pharmaceutical compounds
JP2009537632A (ja) 2006-05-19 2009-10-29 バイエル・ヘルスケア・アクチェンゲゼルシャフト 過剰増殖性障害および血管新生障害の処置に有用なピリドンカルボキサミド誘導体
WO2008045978A1 (en) 2006-10-10 2008-04-17 Rigel Pharmaceuticals, Inc. Pinane-substituted pyrimidinediamine derivatives useful as axl inhibitors
RS54510B1 (sr) 2006-11-22 2016-06-30 Incyte Holdings Corporation Imidazotriazini i imidazopirimidini kao inhibitori kinaze
CN101646671A (zh) 2006-12-14 2010-02-10 弗特克斯药品有限公司 用作蛋白激酶抑制剂的化合物
CA2710046C (en) 2006-12-29 2016-02-09 Rigel Pharmaceuticals, Inc. N3-heteroaryl substituted triazoles and n5-heteroaryl substituted triazoles useful as axl inhibitors
WO2008083353A1 (en) 2006-12-29 2008-07-10 Rigel Pharmaceuticals, Inc. Bicyclic aryl and bicyclic heteroaryl substituted triazoles useful as axl inhibitors
EP2078010B1 (en) 2006-12-29 2014-01-29 Rigel Pharmaceuticals, Inc. Polycyclic heteroaryl substituted triazoles useful as axl inhibitors
WO2008098139A2 (en) 2007-02-07 2008-08-14 The Regents Of The University Of Colorado Axl tyrosine kinase inhibitors and methods of making and using the same
MX2009010556A (es) 2007-03-29 2009-10-22 Panacea Biotec Ltd Formas de dosificacion modificada de tacrolimus.
EP2116532B1 (en) 2007-06-12 2011-12-07 Concert Pharmaceuticals, Inc. Azapeptide derivatives as HIV protease inhibitors
AU2008287339A1 (en) 2007-08-15 2009-02-19 Vertex Pharmaceuticals Incorporated 4-(9-(3, 3-difluorocyclopentyl) -5, 7, 7-trimethyl-6-oxo-6, 7, 8, 9-tetrahydro-5H-pyrimido [4, 5-b][1, 4] diazepin-2-ylamino)-3-methoxybenzamide Derivatives as Inhibitors of the Human Protein Kinases PLK1 to PLK4 for the Treatment of Proliferative Diseases
GB0719803D0 (en) 2007-10-10 2007-11-21 Cancer Rec Tech Ltd Therapeutic compounds and their use
JP2011500778A (ja) 2007-10-25 2011-01-06 アストラゼネカ・アクチエボラーグ ピリジン及びピラジン誘導体−０８３
EP2205592B1 (en) 2007-10-26 2013-05-08 Rigel Pharmaceuticals, Inc. Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors
EA201001030A1 (ru) 2007-12-19 2011-02-28 Амген Инк. Конденсированные соединения пиридина, пиримидина и триазина в качестве ингибиторов клеточного цикла
AR070127A1 (es) 2008-01-11 2010-03-17 Novartis Ag Pirrolo - pirimidinas y pirrolo -piridinas
RU2010146474A (ru) 2008-04-16 2012-05-27 Макс-Планк-Гезелльшафт Цур Фердерунг Дер Виссеншафтен Е.Ф. (De) Производные хинолина в качестве ингибиторов axl киназ
TWI539953B (zh) 2008-04-28 2016-07-01 瑞波若斯治療學公司 用於治療乳癌之組成物和方法
AU2009271658B2 (en) 2008-06-23 2014-04-10 Vertex Pharmaceuticals Incorporated Protein kinase inhibitors
JP5613156B2 (ja) 2008-07-09 2014-10-22 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 Ａｘｌ阻害剤として有用な架橋二環ヘテロアリール置換トリアゾール
ES2537480T3 (es) 2008-07-09 2015-06-08 Rigel Pharmaceuticals, Inc. Triazoles sustituidos con heteroarilo policíclicos útiles como inhibidores de Axl
US20120230991A1 (en) 2008-07-29 2012-09-13 Douglas Kim Graham Methods and compounds for enhancing anti-cancer therapy
EP2158913A1 (en) 2008-08-25 2010-03-03 Ratiopharm GmbH Pharmaceutical composition comprising N-[3-chhloro-4-[(3-fluorophenyl)methoxy]phenyl]6-(5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine
WO2010025073A1 (en) 2008-08-28 2010-03-04 Takeda Pharmaceutical Company Limited Dihydroimidazo [ 1, 5-f] pteridines as polo-like kinase inhibitors
ES2539620T3 (es) 2008-12-19 2015-07-02 Cephalon, Inc. Pirrolotriazina como inhibidor de ALK y de JAK2
TW201041892A (en) 2009-02-09 2010-12-01 Supergen Inc Pyrrolopyrimidinyl Axl kinase inhibitors
US8765754B2 (en) 2009-04-29 2014-07-01 Locus Pharmaceuticals, Inc. Pyrrolotriazine compounds
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
KR101763656B1 (ko) 2009-06-29 2017-08-01 인사이트 홀딩스 코포레이션 Ｐｉ3ｋ 저해물질로서의 피리미디논
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
CN103492391A (zh) 2009-09-25 2014-01-01 沃泰克斯药物股份有限公司 用于制备用作蛋白激酶抑制剂的嘧啶衍生物的方法
EP2311809A1 (en) 2009-10-16 2011-04-20 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Quinolinyloxyphenylsulfonamides
US8604217B2 (en) 2009-11-12 2013-12-10 Selvita S.A. Compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent
TW201130842A (en) 2009-12-18 2011-09-16 Incyte Corp Substituted fused aryl and heteroaryl derivatives as PI3K inhibitors
EP3354652B1 (en) 2010-03-10 2020-05-06 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
WO2011123493A1 (en) 2010-03-31 2011-10-06 Bristol-Myers Squibb Company Substituted pyrrolotriazines as protein kinase inhibitors
CN102471342A (zh) 2010-05-05 2012-05-23 沃泰克斯药物股份有限公司 用作PKC-θ抑制剂的4取代的吡唑并吡啶类
US9290499B2 (en) 2010-05-19 2016-03-22 The University Of North Carolina At Chapel Hill Pyrazolopyrimidine compounds for the treatment of cancer
EP2423208A1 (en) 2010-08-28 2012-02-29 Lead Discovery Center GmbH Pharmaceutically active compounds as Axl inhibitors
CN103403010A (zh) 2010-10-08 2013-11-20 依兰制药公司 Polo样激酶的抑制剂
ITRM20100537A1 (it) 2010-10-12 2012-04-12 Consiglio Nazionale Ricerche Aptamero inibitore del recettore tirosina chinasi axl per uso in terapia
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
EP3660016A1 (en) 2010-12-20 2020-06-03 Incyte Holdings Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
RU2568258C2 (ru) 2011-02-28 2015-11-20 Саншайн Лейк Фарма Ко., Лтд Замещенные соединения хинолина и способы их использования
EP2937349B1 (en) 2011-03-23 2016-12-28 Amgen Inc. Fused tricyclic dual inhibitors of cdk 4/6 and flt3
ES2759615T3 (es) 2011-04-01 2020-05-11 Univ Utah Res Found Análogos de N-fenilpirimidina-2-amina sustituidos como inhibidores de la quinasa AXL
AR086913A1 (es) 2011-06-14 2014-01-29 Novartis Ag 4-metil-3-[[4-(3-piridinil)-2-pirimidinil]-amino]-n-[5-(4-metil-1h-imidazol-1-il)-3-(trifluoro-metil)-fenil]-benzamida amorfa, forma de dosificacion que la contiene y metodo para prepararlas
CN103797010B (zh) 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
SG195100A1 (en) 2011-07-01 2013-12-30 Bayer Ip Gmbh Hydroxymethylaryl-substituted pyrrolotriazines as alk1 inhibitors
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
PT3513793T (pt) 2011-09-02 2021-05-10 Incyte Holdings Corp Heterociclilaminas como inibidores de pi3k
DK2758052T3 (en) 2011-09-18 2018-05-28 Euro Celtique Sa Pharmaceutical composition comprising an HDAC inhibitor and a cyclopolysaccharide
CN102408411B (zh) 2011-09-19 2014-10-22 北京康辰药业股份有限公司 一种含喹啉基的羟肟酸类化合物及其制备方法、以及含有该化合物的药物组合物及其应用
MX2014004086A (es) 2011-10-03 2014-09-22 Univ North Carolina Compuestos de pirrolopirimidina para el tratamiento del cancer.
SG11201402004YA (en) 2011-11-14 2014-05-29 Cephalon Inc Uracil derivatives as axl and c-met kinase inhibitors
US9522892B2 (en) 2011-11-29 2016-12-20 Perosphere Inc. Anticoagulant reversal agents
EP2788000B1 (en) 2011-12-06 2018-05-30 Merck Sharp & Dohme Corp. Pyrrolopyrimidines as janus kinase inhibitors
UY34484A (es) 2011-12-15 2013-07-31 Bayer Ip Gmbh Benzotienilo-pirrolotriazinas disustituidas y sus usos
DK2810937T3 (en) 2012-01-31 2017-03-13 Daiichi Sankyo Co Ltd PYRIDONE DERIVATIVES
JP6082033B2 (ja) 2012-02-23 2017-02-15 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 置換ベンゾチエニル−ピロロトリアジンおよびその使用
WO2013162061A1 (ja) 2012-04-26 2013-10-31 第一三共株式会社 二環性ピリミジン化合物
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
EP2892534B8 (en) 2012-09-06 2021-09-15 Plexxikon Inc. Compounds and methods for kinase modulation, and indications therefor
JP2015532287A (ja) 2012-09-26 2015-11-09 ザ・リージエンツ・オブ・ザ・ユニバーシテイー・オブ・カリフオルニア Ｉｒｅ１の調節
EP2909211A4 (en) 2012-10-17 2016-06-22 Univ North Carolina PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT
TWI646099B (zh) 2012-11-01 2019-01-01 英塞特控股公司 作爲ｊａｋ抑制劑之三環稠合噻吩衍生物
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
US20150353542A1 (en) 2013-01-14 2015-12-10 Amgen Inc. Methods of using cell-cycle inhibitors to modulate one or more properties of a cell culture
TW201522337A (zh) 2013-03-12 2015-06-16 Arqule Inc 經取代之三環吡唑並－嘧啶化合物類
TWI649308B (zh) 2013-07-24 2019-02-01 小野藥品工業股份有限公司 喹啉衍生物
JP6493218B2 (ja) 2013-11-08 2019-04-03 小野薬品工業株式会社 ピロロピリミジン誘導体
WO2015081783A1 (zh) 2013-12-06 2015-06-11 江苏奥赛康药业股份有限公司 吡咯并[2,1-f][1,2,4]三嗪类衍生物及其制备方法和用途
WO2015132799A2 (en) 2014-02-03 2015-09-11 Cadila Healthcare Limited Novel heterocyclic compounds
GB201420285D0 (en) 2014-11-14 2014-12-31 Bergenbio As Process
JP6621477B2 (ja) 2014-12-18 2019-12-18 ファイザー・インク ピリミジンおよびトリアジン誘導体ならびにａｘｌ阻害薬としてのそれらの使用
US9840503B2 (en) 2015-05-11 2017-12-12 Incyte Corporation Heterocyclic compounds and uses thereof
HUE068868T2 (hu) 2015-07-30 2025-02-28 Macrogenics Inc PD-1-hez kötõdõ molekulák és alkalmazásukra szolgáló eljárások
US9708333B2 (en) 2015-08-12 2017-07-18 Incyte Corporation Fused bicyclic 1,2,4-triazine compounds as TAM inhibitors
WO2017035366A1 (en) 2015-08-26 2017-03-02 Incyte Corporation Pyrrolopyrimidine derivatives as tam inhibitors
US20180296561A1 (en) 2015-10-07 2018-10-18 The University Of North Carolina At Chapel Hill The Methods For Treatment Of Tumors
WO2017065183A1 (ja) 2015-10-13 2017-04-20 日本農薬株式会社 オキシム基を有する縮合複素環化合物又はその塩類及び該化合物を含有する農園芸用殺虫剤並びにその使用方法
JP6905662B2 (ja) 2015-11-14 2021-07-21 サンシャイン・レイク・ファーマ・カンパニー・リミテッドＳｕｎｓｈｉｎｅ Ｌａｋｅ Ｐｈａｒｍａ Ｃｏ．，Ｌｔｄ． 置換キノリン化合物の結晶形およびその医薬組成物
EP3373932B1 (en) 2015-11-14 2022-03-30 Sunshine Lake Pharma Co., Ltd. Crystalline form of a substituted quinoline compound and pharmaceutical compositions thereof
TWI833686B (zh) 2016-04-22 2024-03-01 美商英塞特公司 Lsd1 抑制劑之調配物
US10138248B2 (en) * 2016-06-24 2018-11-27 Incyte Corporation Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-b]pyridazines and substituted imidazo[1,2-a]pyrazines as PI3K-γ inhibitors
EP3484524B1 (en) 2016-07-15 2022-11-09 Ionis Pharmaceuticals, Inc. Compounds and methods for modulation of smn2
JOP20170153A1 (ar) 2016-07-15 2019-01-30 Lilly Co Eli نظائر urocortin-2 جديدة معدلة بحمض دهني لعلاج داء السكري وأمراض الكلى المزمنة
JOP20190257A1 (ar) 2017-04-28 2019-10-28 Novartis Ag مركبات أريل غير متجانسة ثنائية الحلقة مندمجة 6-6 واستخدامها كمثبطات lats
MA50655B1 (fr) 2017-09-27 2021-11-30 Incyte Corp Sels de dérivés de pyrrolotriazine utiles en tant qu'inhibiteurs de tam
WO2021178779A1 (en) 2020-03-06 2021-09-10 Incyte Corporation Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019510043A (ja) 2016-03-28 2019-04-11 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｔａｍ阻害剤としてのピロロトリアジン化合物
JP2021529765A (ja) 2018-06-29 2021-11-04 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ａｘｌ／ｍｅｒ阻害剤の製剤

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2025093936A (ja) * 2017-09-27 2025-06-24 インサイト・コーポレイション Ｔａｍ阻害剤として有用なピロロトリアジン誘導体の塩

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