JP2021518413A - 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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JP2021518413A
JP2021518413A JP2020550798A JP2020550798A JP2021518413A JP 2021518413 A JP2021518413 A JP 2021518413A JP 2020550798 A JP2020550798 A JP 2020550798A JP 2020550798 A JP2020550798 A JP 2020550798A JP 2021518413 A JP2021518413 A JP 2021518413A
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methyl
compound according
compound
carboline
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JP2021518413A5 (https=
Inventor
クナル クマール
クナル クマール
ペン ワン
ペン ワン
ロベルト サンチェス
ロベルト サンチェス
アドルフォ ガルシア オカーニャ
アドルフォ ガルシア オカーニャ
アンドリュー スチュアート
アンドリュー スチュアート
ロバート デヴィータ
ロバート デヴィータ
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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
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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Publication of JP2021518413A publication Critical patent/JP2021518413A/ja
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    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2020550798A 2018-03-20 2019-03-20 キナーゼ阻害剤化合物及び組成物ならびに使用方法 Pending JP2021518413A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201862645560P 2018-03-20 2018-03-20
US62/645,560 2018-03-20
PCT/US2019/023206 WO2019183245A1 (en) 2018-03-20 2019-03-20 Kinase inhibitor compounds and compositions and methods of use

Publications (2)

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JP2021518413A true JP2021518413A (ja) 2021-08-02
JP2021518413A5 JP2021518413A5 (https=) 2022-03-25

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US (2) US11866427B2 (https=)
EP (1) EP3768267B1 (https=)
JP (1) JP2021518413A (https=)
CN (1) CN112135613A (https=)
AU (1) AU2019240065A1 (https=)
CA (1) CA3093340A1 (https=)
ES (1) ES3038913T3 (https=)
WO (1) WO2019183245A1 (https=)

Families Citing this family (13)

* 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
CN115466312B (zh) * 2021-06-10 2025-10-31 首都医科大学 抑制侵袭和迁移的1-咪唑-β-咔啉-3-甲酰-RGDV、其制备和应用
CN114288291B (zh) * 2021-12-28 2023-04-28 大连医科大学附属第一医院 Norharman在制备预防或治疗急性胰腺炎药物中的应用
CN114984195B (zh) * 2022-04-29 2025-12-16 上海中医药大学 脂肪膜相关蛋白及其相关编码基因和片段的新用途
CN114907346B (zh) * 2022-05-19 2023-03-31 暨南大学 一种生物碱类化合物、提取物及其在制备具有抗呼吸道合胞病毒作用的产品中的应用
CN115322089B (zh) * 2022-07-18 2023-10-03 中国农业科学院烟草研究所(中国烟草总公司青州烟草研究所) 一种覆盆子酮半抗原、人工抗原及其制备方法、抗体和应用
WO2024178504A1 (en) * 2023-02-27 2024-09-06 Enveric Biosciences Canada Inc. Tri-halo-alkoxy-substituted tryptamine derivatives and methods of using
US11802129B1 (en) 2023-03-20 2023-10-31 King Faisal University Pyrido[3,4-b]indol-1-one compounds as anticancer agents
US11773092B1 (en) 2023-03-27 2023-10-03 King Faisal University Pyrido[3,4-b]indol-1-one compounds as antibacterial agents
CN116509853B (zh) * 2023-06-12 2025-01-28 新疆医科大学第一附属医院 去氢骆驼蓬碱衍生物在改善器官纤维化中的应用
WO2025122509A1 (en) * 2023-12-04 2025-06-12 Poviva Corp Compositions and methods for treating diabetes

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012024433A2 (en) * 2010-08-17 2012-02-23 Translational Genomics Research Institute Compounds that inhibit tau phosphorylation
CN102977096A (zh) * 2012-12-07 2013-03-20 中国药科大学 具有靶向特性的去氢骆驼蓬碱衍生物的抗肿瘤前药
JP2013525471A (ja) * 2010-05-05 2013-06-20 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 併用療法
WO2014063477A1 (zh) * 2011-10-25 2014-05-01 新疆华世丹药物研究有限责任公司 去氢骆驼蓬碱衍生物在制备抗菌药物中的应用
WO2015011331A1 (es) * 2013-07-25 2015-01-29 Fundación Para La Investigación Biomédica Del Hospital Universitario La Paz (Fibhulp) Uso de compuestos derivados de sales de piridazino[1',6':1,2]pirido[3,4-b]indolinio y piridazino[3,2-b]benzimidazolio como agentes antiinflamatorios
JP2016519082A (ja) * 2013-03-14 2016-06-30 オステオーク インコーポレイティド 骨の成長を促進するためのアルキルアミンハルミン誘導体
CN105884767A (zh) * 2015-11-24 2016-08-24 西华大学 9-位取代的吡啶并[3,4-b]吲哚衍生物及其制备方法和作为SIRT蛋白抑制剂的用途
WO2016161410A2 (en) * 2015-04-03 2016-10-06 Xoma Technology Ltd. Treatment of cancer using inhibitors of tgf-beta and pd-1

Family Cites Families (141)

* 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
US5731424A (en) 1990-06-11 1998-03-24 Nexstar Pharmaceuticals, Inc. High affinity TGFβ nucleic acid ligands and inhibitors
US5731144A (en) 1990-06-11 1998-03-24 Nexstar Pharmaceuticals, Inc. High affinity TGFβ nucleic acid ligands
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
US6451349B1 (en) 1998-08-19 2002-09-17 Quadrant Healthcare (Uk) Limited Spray-drying process for the preparation of microparticles
GB9814172D0 (en) 1998-06-30 1998-08-26 Andaris Ltd Formulation for inhalation
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
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
TW200301123A (en) 2001-12-21 2003-07-01 Astrazeneca Uk Ltd New use
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
EP1542995A1 (en) 2002-09-18 2005-06-22 Pfizer Products Inc. Novel isothiazole and isoxazole compounds as transforming growth factor (tgf) inhibitors
CA2496295C (en) 2002-09-18 2010-11-23 Michael John Munchhof Novels pyrazole compounds as transforming growth factor (tgf) inhibitors
CA2497971A1 (en) 2002-09-18 2004-04-01 Pfizer Products Inc. Triazole derivatives 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
AU2003297460A1 (en) 2002-12-19 2004-07-14 Scios, Inc. TREATMENT OF OBESITY AND ASSOCIATED CONDITIONS WITH TGF-Beta 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
WO2005003101A2 (en) 2003-07-02 2005-01-13 Biofocus Discovery Limited Pyrazine and pyridine derivatives as rho kinase inhibitors
US20050032869A1 (en) 2003-07-08 2005-02-10 Pharmacia Italia S.P.A. Pyrazolyl-indole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
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
WO2006027348A1 (en) 2004-09-06 2006-03-16 Basilea Pharmaceutica Ag Phenylaminopyridines
GT200500284A (es) 2004-10-15 2006-03-27 Aventis Pharma Inc Pirimidinas como antagonistas del receptor de prostaglandina d2
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.
GB0705566D0 (en) 2007-03-23 2007-05-02 Univ Dundee Method of treating learning impairment in down's syndrome subjects
EP2178537A4 (en) 2007-07-19 2011-08-17 Merck Sharp & Dohme BETA-CARBOLIN DERIVATIVES AS ANTIDIBLE COMPOUNDS
WO2009032667A1 (en) 2007-08-29 2009-03-12 Smithkline Beecham Corporation Thiazole and oxazole kinase inhibitors
JP5638961B2 (ja) 2008-03-13 2014-12-10 ザ ジェネラル ホスピタル コーポレイション Ｂｍｐシグナル伝達経路のインヒビター
US8298825B1 (en) 2008-08-25 2012-10-30 The General Hospital Corporation TGF-beta receptor inhibitors to enhance direct reprogramming
WO2010080756A2 (en) 2009-01-06 2010-07-15 Osteogenex, Inc. Harmine derivatives for reducing body weight
US8329723B2 (en) * 2009-04-24 2012-12-11 John K Buolamwini 1-aryl- or 1-heteroaryl-pyrido[B]indoles and uses thereof in treating cancers
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.
WO2010135589A2 (en) 2009-05-20 2010-11-25 Sakura Properties, Llc Dietary supplement drink for delivery of resveratrol and other polyphenols
JP2011006408A (ja) 2009-05-29 2011-01-13 Sumitomo Chemical Co Ltd 神経栄養因子の活性が関与する疾患の治療または予防剤
WO2011069051A1 (en) 2009-12-04 2011-06-09 Caliper Life Sciences, Inc. Method of using dopamine reuptake inhibitors and their analogs for treating diabetes symptoms and delaying or preventing diabetes-associated pathologic conditions
KR20120113228A (ko) 2009-12-18 2012-10-12 프레지던트 앤드 펠로우즈 오브 하바드 칼리지 베타 세포 복제 촉진 화합물 및 그 사용 방법
US20130102627A1 (en) 2010-04-09 2013-04-25 The Brigham And Women's Hospital, Inc. Acridines As Inhibitors Of Haspin And DYRK Kinases
WO2011133795A2 (en) 2010-04-22 2011-10-27 The Brigham And Women's Hospital, Inc. Beta-carbolines as inhibitors of haspin and dyrk kinases
AR081626A1 (es) 2010-04-23 2012-10-10 Cytokinetics Inc Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos
AR081331A1 (es) 2010-04-23 2012-08-08 Cytokinetics Inc Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos
CA2803697A1 (en) * 2010-06-25 2011-12-29 Facultes Universitaires Notre Dame De La Paix Beta carboline derivatives useful in the treatment of proliferative disorders
KR101877077B1 (ko) 2010-08-09 2018-07-10 다케다 야쿠힌 고교 가부시키가이샤 췌호르몬-생성 세포의 제조 방법
US9446044B2 (en) 2011-08-19 2016-09-20 Diaxonhit DYRK1 inhibitors and uses thereof
US9216173B2 (en) 2011-10-05 2015-12-22 Merck Sharp & Dohme Corp. 2-Pyridyl carboxamide-containing spleen tyrosine kinase (SYK) inhibitors
WO2013119518A1 (en) 2012-02-06 2013-08-15 The Regents Of The University Of California Small molecules for islet expansion
MX371331B (es) 2012-04-24 2020-01-27 Vertex Pharma Inhibidores de la proteina cinasa dependiente de acido desoxirribonucleico(adn-pk).
KR20150033703A (ko) 2012-06-27 2015-04-01 오르반 바이오테크 엘엘씨 당뇨병 치료를 위한 ctla4 융합 단백질
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
JP2016500080A (ja) 2012-11-26 2016-01-07 新疆華世丹薬物研究有限責任公司 ビスβ−カルボリン系化合物、その製造方法、医薬組成物および用途
JPWO2014058080A1 (ja) 2012-11-30 2016-09-05 国立研究開発法人理化学研究所 体細胞のリプログラミングを亢進させる方法、及び細胞作製キット
HK1213544A1 (zh) 2012-12-10 2016-07-08 霍夫曼-拉罗奇有限公司 新型二环苯基-吡啶/吡嗪用於治疗癌症
US20150174034A1 (en) 2013-03-13 2015-06-25 Avon Products, Inc. Tyrosinase inhibitors
US9815847B2 (en) 2013-03-14 2017-11-14 Icahn School Of Medicine At Mount Sinai Pyrimidine compounds as kinase inhibitors
AU2014283378B2 (en) 2013-06-18 2018-09-27 4Sc Ag 2,3-dihydrobenzofuran-5-yl compounds as DYRK kinase inhibitors
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
HRP20180804T1 (hr) 2013-10-17 2018-08-10 Vertex Pharmaceuticals Incorporated Inhibitori dnk-pk
CN106536507B (zh) 2014-04-08 2020-04-07 里格尔药品股份有限公司 作为TGF-β抑制剂的2,3-二取代的吡啶化合物及其使用方法
US20170280720A1 (en) 2014-09-17 2017-10-05 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP3188721B1 (en) 2014-10-21 2019-06-12 Ankh Life Sciences Limited Human therapeutic agents
EP3234110B1 (en) 2014-12-18 2024-02-28 President and Fellows of Harvard College METHODS FOR GENERATING STEM CELL-DERIVED ß CELLS 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
US10730842B2 (en) 2015-09-03 2020-08-04 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of DYRK1A and uses thereof
CR20180323A (es) 2015-11-20 2018-08-06 Idorsia Pharmaceuticals Ltd Derivados de indol n-sustituídos como moduladores de los receptores de pge2
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
US20170281607A1 (en) 2016-04-01 2017-10-05 University Of Limerick Pharmaceutical compositions and methods for the treatment of diabetes
US10947225B2 (en) 2016-05-11 2021-03-16 Emory University Phosphotidylinositol 3-kinase inhibitors
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
US11266647B2 (en) 2016-10-26 2022-03-08 Icahn School Of Medicine At Mount Sinai Method for increasing cell proliferation in pancreatic beta cells, treatment method, and composition
EP3318563A1 (en) 2016-11-07 2018-05-09 Sanofi Substituted pyrido[3,4-b]indoles for the treatment of cartilage disorders
CN110691782A (zh) 2016-12-01 2020-01-14 艾普托斯生物科学公司 作为brd4和jak2双重抑制剂的稠合的嘧啶化合物及其使用方法
PE20191814A1 (es) 2017-05-18 2019-12-27 Idorsia Pharmaceuticals Ltd Derivados de pirimidina como moduladores del receptor de pge2
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
JP2022515650A (ja) 2018-12-31 2022-02-21 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 キナーゼ阻害剤化合物及び組成物ならびに使用方法
WO2020142485A1 (en) 2018-12-31 2020-07-09 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use
US20230234935A1 (en) 2020-06-26 2023-07-27 Icahn School Of Medicine At Mount Sinai Kinase inhibitor compounds and compositions and methods of use

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2013525471A (ja) * 2010-05-05 2013-06-20 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 併用療法
WO2012024433A2 (en) * 2010-08-17 2012-02-23 Translational Genomics Research Institute Compounds that inhibit tau phosphorylation
WO2014063477A1 (zh) * 2011-10-25 2014-05-01 新疆华世丹药物研究有限责任公司 去氢骆驼蓬碱衍生物在制备抗菌药物中的应用
CN102977096A (zh) * 2012-12-07 2013-03-20 中国药科大学 具有靶向特性的去氢骆驼蓬碱衍生物的抗肿瘤前药
JP2016519082A (ja) * 2013-03-14 2016-06-30 オステオーク インコーポレイティド 骨の成長を促進するためのアルキルアミンハルミン誘導体
WO2015011331A1 (es) * 2013-07-25 2015-01-29 Fundación Para La Investigación Biomédica Del Hospital Universitario La Paz (Fibhulp) Uso de compuestos derivados de sales de piridazino[1',6':1,2]pirido[3,4-b]indolinio y piridazino[3,2-b]benzimidazolio como agentes antiinflamatorios
WO2016161410A2 (en) * 2015-04-03 2016-10-06 Xoma Technology Ltd. Treatment of cancer using inhibitors of tgf-beta and pd-1
CN105884767A (zh) * 2015-11-24 2016-08-24 西华大学 9-位取代的吡啶并[3,4-b]吲哚衍生物及其制备方法和作为SIRT蛋白抑制剂的用途

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
BALINT, BALAZS ET AL.: "Structure-Based Design and Synthesis of Harmine Derivatives with Different Selectivity Profiles in K", CHEMMEDCHEM, vol. 12, no. 12, JPN7023000649, 2017, pages 932 - 939, ISSN: 0005172355 *
FILALI, INSAF ET AL.: "Synthesis of New Harmine Isoxazoles and Evaluation of their Potential Anti-Alzheimer, Anti-inflammat", MEDICINAL CHEMISTRY (SHARJAH, UNITED ARAB EMIRATES), vol. 12, no. 2, JPN7023000650, 2016, pages 184 - 190, ISSN: 0005172356 *
FILALI, INSAF ET AL.: "Synthesis of new isoxazoline derivatives from harmine and evaluation of their anti-Alzheimer, anti-c", JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol. 30, no. 3, JPN7023000651, 2015, pages 371 - 376, ISSN: 0005172357 *

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