JP2022515652A - キナーゼ阻害剤化合物及び組成物ならびに使用方法 - Google Patents

キナーゼ阻害剤化合物及び組成物ならびに使用方法 Download PDF

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JP2022515652A
JP2022515652A JP2021538213A JP2021538213A JP2022515652A JP 2022515652 A JP2022515652 A JP 2022515652A JP 2021538213 A JP2021538213 A JP 2021538213A JP 2021538213 A JP2021538213 A JP 2021538213A JP 2022515652 A JP2022515652 A JP 2022515652A
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compound
purified
silica gel
column chromatography
gel column
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JP2022515652A5 (https=
Inventor
ロバート ジェイ． デヴィータ
アンドリュー エフ． スチュアート
チャラダ スプスウォン
クナル クマール
ペン ワン
ロベルト ジェイ． サンチェス
フイ ワン
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アイカーン スクール オブ メディシン アット マウント サイナイ
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • C07—ORGANIC CHEMISTRY
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • 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
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    • 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
    • A61K31/403—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 carbocyclic rings, e.g. carbazole
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • 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
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    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2021538213A 2018-12-31 2019-12-31 キナーゼ阻害剤化合物及び組成物ならびに使用方法 Pending JP2022515652A (ja)

Applications Claiming Priority (3)

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US201862786966P 2018-12-31 2018-12-31
US62/786,966 2018-12-31
PCT/US2019/069057 WO2020142485A1 (en) 2018-12-31 2019-12-31 Kinase inhibitor compounds and compositions and methods of use

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JP2022515652A true JP2022515652A (ja) 2022-02-21
JP2022515652A5 JP2022515652A5 (https=) 2023-01-11

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US (1) US20220162182A1 (https=)
EP (1) EP3906233B1 (https=)
JP (1) JP2022515652A (https=)
CN (1) CN113508111A (https=)
AU (1) AU2019419414A1 (https=)
CA (1) CA3124700A1 (https=)
WO (1) WO2020142485A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019100062A1 (en) 2017-11-20 2019-05-23 Ichan School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
WO2019136320A1 (en) 2018-01-05 2019-07-11 Icahn School Of Medicine At Mount Sinai Method of increasing proliferation of pancreatic beta cells, treatment method, and composition
CN112135613A (zh) 2018-03-20 2020-12-25 西奈山伊坎医学院 激酶抑制剂化合物和组合物及使用方法
US20250236613A1 (en) * 2021-10-25 2025-07-24 Sironax Ltd. Sarm1 modulators, preparations, and uses thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007516196A (ja) * 2003-07-02 2007-06-21 ガラパゴス エヌブイ Ｒｈｏキナーゼ阻害剤としてのピラジン及びピラリジン誘導体
WO2013052394A1 (en) * 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
JP2016501251A (ja) * 2012-12-10 2016-01-18 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト がんの治療のための新規二環フェニル−ピリジン／ピラジン
JP2018526452A (ja) * 2015-09-03 2018-09-13 アリゾナ ボード オブ リージェンツ オン ビハーフ オブ ザ ユニバーシティー オブ アリゾナ Ｄｙｒｋ１ａの小分子抑制剤およびその使用

Family Cites Families (91)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ221411A (en) 1986-08-11 1989-10-27 Innovata Biomed Ltd Pharmaceutical compositions containing microcapsules and a surfactant
US5179079A (en) 1986-12-16 1993-01-12 Novo Nordisk A/S Nasal formulation and intranasal administration therewith
GB8723846D0 (en) 1987-10-10 1987-11-11 Danbiosyst Ltd Bioadhesive microsphere drug delivery system
US5571714A (en) 1988-12-22 1996-11-05 Celtrix Pharmaceuticals, Inc. Monoclonal antibodies which bind both transforming growth factors β1 and β2 and methods of use
US4994439A (en) 1989-01-19 1991-02-19 California Biotechnology Inc. Transmembrane formulations for drug administration
FI913899A7 (fi) 1989-02-23 1991-08-19 Rorer Int Holdings Inc Terapeuttiset aerosoliseokset
GB8921222D0 (en) 1989-09-20 1989-11-08 Riker Laboratories Inc Medicinal aerosol formulations
US5731144A (en) 1990-06-11 1998-03-24 Nexstar Pharmaceuticals, Inc. High affinity TGFβ nucleic acid ligands
US5731424A (en) 1990-06-11 1998-03-24 Nexstar Pharmaceuticals, Inc. High affinity TGFβ nucleic acid ligands and inhibitors
US5292499A (en) 1990-09-11 1994-03-08 University Of Wales College Of Cardiff Method of preparing medical aerosol formulations including drug dissolved in reverse micelles
US5230884A (en) 1990-09-11 1993-07-27 University Of Wales College Of Cardiff Aerosol formulations including proteins and peptides solubilized in reverse micelles and process for making the aerosol formulations
US6632456B1 (en) 1993-06-24 2003-10-14 Astrazeneca Ab Compositions for inhalation
US6524557B1 (en) 1994-12-22 2003-02-25 Astrazeneca Ab Aerosol formulations of peptides and proteins
CH689139A5 (de) 1995-04-03 1998-10-30 Cerbios Pharma Sa Verfahren zur Herstellung einer liposomalen, in Wasser dispergierbaren, oral zu verabreichenden, festen, trockenen therapeutischen Formulierung.
US6309671B1 (en) 1995-04-14 2001-10-30 Inhale Therapeutic Systems Stable glassy state powder formulations
US5635161A (en) 1995-06-07 1997-06-03 Abbott Laboratories Aerosol drug formulations containing vegetable oils
US6120794A (en) 1995-09-26 2000-09-19 University Of Pittsburgh Emulsion and micellar formulations for the delivery of biologically active substances to cells
JPH10508322A (ja) 1995-10-12 1998-08-18 スーパーゲン，インコーポレイティド ５βステロイドのリポソーム配合物
US6806358B1 (en) 1997-12-16 2004-10-19 University Of California San Diego Peptide inhibitor of TGF-β growth factors
US6943191B1 (en) 1998-02-27 2005-09-13 The United States Of America As Represented By The Department Of Health And Human Services Disubstituted lavendustin A analogs and pharmaceutical composition comprising the analogs
GB9809869D0 (en) 1998-05-09 1998-07-08 Medical Res Council Inhibition of protein kinases
SK17422000A3 (sk) 1998-05-20 2001-09-11 The Liposome Company, Inc. Kompozöcie ¬astöc
GB9814172D0 (en) 1998-06-30 1998-08-26 Andaris Ltd Formulation for inhalation
US6451349B1 (en) 1998-08-19 2002-09-17 Quadrant Healthcare (Uk) Limited Spray-drying process for the preparation of microparticles
AUPP494798A0 (en) 1998-07-29 1998-08-20 Pacific Biolink Pty Limited Protective protein formulation
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
US6290987B1 (en) 1998-09-27 2001-09-18 Generex Pharmaceuticals, Inc. Mixed liposome pharmaceutical formulation with amphiphiles and phospholipids
ES2146552B1 (es) 1998-11-24 2001-04-16 Inst Cientifico Tecnol Navarra Peptidos inhibidores de tgf/31
US6436367B1 (en) 1998-12-21 2002-08-20 Generex Pharmaceuticals Inc. Aerosol formulations for buccal and pulmonary application
EP1338272A1 (en) 1998-12-21 2003-08-27 Generex Pharmaceuticals Inc. Aerosol formulations for buccal and pulmonary application comprising chenodeoxycholate or deoxycholate
US6294153B1 (en) 1998-12-21 2001-09-25 Generex Pharmaceuticals, Inc. Aerosol pharmaceutical formulation for pulmonary and nasal delivery
WO2000047203A1 (en) 1999-02-12 2000-08-17 Mqs, Inc. Formulation and system for intra-oral delivery of pharmaceutical agents
JP2002542183A (ja) 1999-04-16 2002-12-10 ノボ ノルディスク アクティーゼルスカブ 成形可能な乾燥した医薬製剤
US6492497B1 (en) 1999-04-30 2002-12-10 Cambridge Antibody Technology Limited Specific binding members for TGFbeta1
US6485706B1 (en) 1999-06-04 2002-11-26 Delrx Pharmaceutical Corp. Formulations comprising dehydrated particles of pharma-ceutical agents and process for preparing the same
US20010036481A1 (en) 1999-08-25 2001-11-01 Advanced Inhalation Research, Inc. Modulation of release from dry powder formulations
EP1210067A2 (en) 1999-08-25 2002-06-05 Advanced Inhalation Research, Inc. Modulation of release from dry powder formulations
ATE267582T1 (de) 2000-01-20 2004-06-15 Basilea Pharmaceutica Ag Nasal verabreichbare cyclische antimykotische peptidzusammensetzungen
EP1129705A1 (en) 2000-02-17 2001-09-05 Rijksuniversiteit te Groningen Powder formulation for inhalation
GB0009468D0 (en) 2000-04-17 2000-06-07 Vectura Ltd Improvements in or relating to formulations for use in inhaler devices
CA2406206C (en) 2000-04-17 2012-03-20 Vectura Limited Improvements in or relating to formulations for use in inhaler devices
US20020155084A1 (en) 2000-06-02 2002-10-24 The Regents Of The University Of The Michigan Nanoemulsion formulations
US6509318B1 (en) 2000-09-29 2003-01-21 The Regents Of The University Of California TGF-B inhibitors and methods
FI20002768L (fi) 2000-12-18 2002-06-19 Licentia Oy Enteropäällysteisiä lääkekoostumuksia ja niiden valmistus
US20030134836A1 (en) * 2001-01-12 2003-07-17 Amgen Inc. Substituted arylamine derivatives and methods of use
GB0107106D0 (en) 2001-03-21 2001-05-09 Boehringer Ingelheim Pharma Powder inhaler formulations
SK287857B6 (sk) 2001-05-24 2012-01-04 Eli Lilly And Company Novel pyrrole derivatives as pharmaceutical agents
US20030019437A1 (en) 2001-07-26 2003-01-30 John Fore Ungulate game animal feed system and method
US20030028905A1 (en) 2001-07-31 2003-02-06 Petra Knaus Mutant forms of the TGF-beta type II receptor which bind all TGF-beta isoforms
US20030064033A1 (en) 2001-08-16 2003-04-03 Brown Larry R. Propellant-based microparticle formulations
AU2003215334A1 (en) 2002-02-22 2003-09-09 Advanced Inhalation Research, Inc. Inhalable formulations for sustained release
WO2003079885A2 (en) 2002-03-20 2003-10-02 Advanced Inhalation Research, Inc. Inhalable sustained therapeutic formulations
HRP20041152B1 (hr) 2002-05-07 2008-01-31 Ferring B.V. Farmaceutske formulacije
EP1506191A1 (en) 2002-05-15 2005-02-16 Smithkline Beecham Corporation Benzoxazine and benzoxazinone substituted triazoles
AU2003229305A1 (en) 2002-05-17 2003-12-02 Scios, Inc. TREATMENT OF FIBROPROLIFERATIVE DISORDERS USING TGF-Beta INHIBITORS
US7190468B2 (en) 2002-07-17 2007-03-13 Hewlett-Packard Development Company, L.P. Background document rendering system and method
EP1539748A1 (en) 2002-07-31 2005-06-15 Smithkline Beecham Corporation 2-phenylpyridin-4-yl derivatives as alk5 inhibitors
UA80296C2 (en) 2002-09-06 2007-09-10 Biogen Inc Imidazolopyridines and methods of making and using the same
EP1543001B1 (en) 2002-09-17 2007-08-15 Eli Lilly And Company Pyrazolopyridine derivatives as tgf beta signal transduction inhibitors for the treatment of cancer
CA2497971A1 (en) 2002-09-18 2004-04-01 Pfizer Products Inc. Triazole derivatives as transforming growth factor (tgf) inhibitors
EP1542995A1 (en) 2002-09-18 2005-06-22 Pfizer Products Inc. Novel isothiazole and isoxazole compounds as transforming growth factor (tgf) inhibitors
WO2004047818A2 (en) 2002-11-22 2004-06-10 Scios, Inc. USE OF TFG-β INHIBITORSTO COUNTERACT PATHOLOGIC CHANGES IN THE LEVEL OR FUNCTION OF STEROID/THYROID RECEPTORS
US8030336B2 (en) * 2002-12-13 2011-10-04 Ym Biosciences Australia Pty Ltd Nicotinamide-based kinase inhibitors
BRPI0407055A (pt) 2003-01-27 2006-01-17 Pfizer Prod Inc Derivados de isotiazol
DE602004014347D1 (de) 2003-03-12 2008-07-24 Millennium Pharm Inc Chinazolin-derivate als tgf-beta-inhibitoren
US7223766B2 (en) 2003-03-28 2007-05-29 Scios, Inc. Bi-cyclic pyrimidine inhibitors of TGFβ
ES2389258T3 (es) 2003-06-17 2012-10-24 Millennium Pharmaceuticals, Inc. Composiciones y métodos para inhibir TGF-s
WO2005039570A1 (ja) 2003-10-28 2005-05-06 Riken ＴＧＦ－β情報伝達経路阻害剤
MXPA06008157A (es) 2003-12-24 2007-09-07 Johnson & Johnson Tratamiento de gliomas malignos con inhibidores de factor de crecimiento transformante-beta.
EP1723146A1 (en) 2004-03-01 2006-11-22 Eli Lilly And Company Fused pyrazole derivatives as tgf-beta signal transduction inhibitors for the treatment of fibrosis and neoplasms
WO2006010637A2 (en) * 2004-07-30 2006-02-02 Gpc Biotech Ag Pyridinylamines
JP2007176795A (ja) 2004-08-18 2007-07-12 Univ Nihon ＴＧＦ−β遺伝子発現抑制剤
CN101189234B (zh) 2005-03-25 2011-08-17 泰博特克药品有限公司 Hcv的杂二环抑制剂
PT1910370E (pt) 2005-07-22 2015-06-30 Lilly Co Eli Um pirrolo[1,2-b]pirazole mono-hidratado substituído com piridina e quinolina como inibidor do tgf-beta
EP1974740A4 (en) 2005-10-24 2010-09-01 Proyecto Biomedicina Cima Sl USE OF TGF-BETA1 INHIBITORY PEPTIDES IN THE PREPARATION OF AN IMMUNE RESPONSE MODULATING AGENT
WO2007084667A2 (en) * 2006-01-19 2007-07-26 Osi Pharmaceutical, Inc. Fused heterobicyclic kinase inhibitors
ITMI20060181A1 (it) 2006-02-03 2007-08-04 Univ Padova Modulatori del tgf-b e loro uso
BRPI0807961A2 (pt) * 2007-02-13 2017-05-16 Pharmacopeia Llc agonista de alfa2c adrenorreceptor funcionalmente seletivos.
WO2009032667A1 (en) 2007-08-29 2009-03-12 Smithkline Beecham Corporation Thiazole and oxazole kinase inhibitors
US8298825B1 (en) 2008-08-25 2012-10-30 The General Hospital Corporation TGF-beta receptor inhibitors to enhance direct reprogramming
MX2011012202A (es) * 2009-05-15 2011-12-08 Novartis Ag Derivados de 5-piridin-3-il-1,3-dihidro-indol-2-ona y su uso como moduladores de a sintanasa de aldosterona y/o de cyp11b1.
US9988606B2 (en) 2012-07-24 2018-06-05 The Trustees Of Columbia University In The City Of New York Generation of airway and lung progenitors and epithelial cells and three-dimensional anterior foregut spheres
US20150297573A1 (en) * 2012-10-24 2015-10-22 INSERM (Institut National de la Santé et de la Recherche Médicale) TPL2 KINASE INHIBITORS FOR PREVENTING OR TREATING DIABETES AND FOR PROMOTING Beta-CELL SURVIVAL
CA2854542A1 (en) * 2013-06-18 2014-12-18 4Sc Discovery Gmbh Method of inhibiting dyrk1b
WO2014203217A1 (en) * 2013-06-21 2014-12-24 Lupin Limited Substituted heterocyclic compounds as crac modulators
US20170280720A1 (en) * 2014-09-17 2017-10-05 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
DE112016002687T5 (de) 2015-07-11 2018-03-01 Changzhou Create Electric Appliance Co., Ltd. Gleichstrom-Vertikutierer
EP3328404A4 (en) * 2015-07-27 2018-12-26 The Regents of The University of California Methods and compositions for producing pancreatic beta cells
WO2017106630A1 (en) * 2015-12-18 2017-06-22 The General Hospital Corporation Polyacetal polymers, conjugates, particles and uses thereof
US10487087B2 (en) 2015-12-30 2019-11-26 Vanderbilt University Positive allosteric modulators of the GLP-1 receptor
JP6596390B2 (ja) 2016-06-29 2019-10-23 株式会社沖データ 現像剤収容器、現像装置、画像形成装置、及び基板支持構造

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007516196A (ja) * 2003-07-02 2007-06-21 ガラパゴス エヌブイ Ｒｈｏキナーゼ阻害剤としてのピラジン及びピラリジン誘導体
WO2013052394A1 (en) * 2011-10-05 2013-04-11 Merck Sharp & Dohme Corp. 2-pyridyl carboxamide-containing spleen tyrosine kinase (syk) inhibitors
JP2016501251A (ja) * 2012-12-10 2016-01-18 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト がんの治療のための新規二環フェニル−ピリジン／ピラジン
JP2018526452A (ja) * 2015-09-03 2018-09-13 アリゾナ ボード オブ リージェンツ オン ビハーフ オブ ザ ユニバーシティー オブ アリゾナ Ｄｙｒｋ１ａの小分子抑制剤およびその使用

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 27, JPN6024004274, 2017, pages 4150 - 4155, ISSN: 0005399925 *

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