NO329228B1 - Indoliziner som kinaseinhibitorer - Google Patents

Indoliziner som kinaseinhibitorer Download PDF

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Publication number
NO329228B1
NO329228B1 NO20041493A NO20041493A NO329228B1 NO 329228 B1 NO329228 B1 NO 329228B1 NO 20041493 A NO20041493 A NO 20041493A NO 20041493 A NO20041493 A NO 20041493A NO 329228 B1 NO329228 B1 NO 329228B1
Authority
NO
Norway
Prior art keywords
phenyl
amide
pyrazine
optionally substituted
dihydro
Prior art date
Application number
NO20041493A
Other languages
English (en)
Norwegian (no)
Other versions
NO20041493L (no
Inventor
Andrew James Ratcliffe
Tahir Nadeem Majid
David John Aldous
Sukanthini Thurairatnam
Roger John Aitchison Walsh
Conception Nemecek
Shelly Amendola
John Edward Souness
Sylvie Wentzler
Corinne Venot
Original Assignee
Aventis Pharma Sa
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB0122560.6A external-priority patent/GB0122560D0/en
Application filed by Aventis Pharma Sa filed Critical Aventis Pharma Sa
Publication of NO20041493L publication Critical patent/NO20041493L/no
Publication of NO329228B1 publication Critical patent/NO329228B1/no

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Classifications

    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Epidemiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Steroid Compounds (AREA)
NO20041493A 2001-09-19 2004-04-13 Indoliziner som kinaseinhibitorer NO329228B1 (no)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB0122560.6A GB0122560D0 (en) 2001-09-19 2001-09-19 Chemical compounds
US35586002P 2002-02-11 2002-02-11
PCT/EP2002/011131 WO2003024967A2 (en) 2001-09-19 2002-09-17 Indolizines as kinase protein inhibitors

Publications (2)

Publication Number Publication Date
NO20041493L NO20041493L (no) 2004-04-13
NO329228B1 true NO329228B1 (no) 2010-09-20

Family

ID=26246563

Family Applications (1)

Application Number Title Priority Date Filing Date
NO20041493A NO329228B1 (no) 2001-09-19 2004-04-13 Indoliziner som kinaseinhibitorer

Country Status (19)

Country Link
US (1) US7148215B2 (enExample)
EP (1) EP1436291B1 (enExample)
JP (1) JP4456365B2 (enExample)
CN (1) CN100391958C (enExample)
AT (1) ATE420879T1 (enExample)
AU (1) AU2002337142B2 (enExample)
BR (1) BR0212760A (enExample)
CA (1) CA2466243A1 (enExample)
CO (1) CO5640127A2 (enExample)
DE (1) DE60230890D1 (enExample)
EA (1) EA007983B1 (enExample)
HR (1) HRP20040267A2 (enExample)
HU (1) HUP0401982A3 (enExample)
IL (1) IL160915A0 (enExample)
MX (1) MXPA04002243A (enExample)
NO (1) NO329228B1 (enExample)
NZ (1) NZ531378A (enExample)
PL (1) PL369530A1 (enExample)
WO (1) WO2003024967A2 (enExample)

Families Citing this family (202)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20040082509A1 (en) 1999-10-12 2004-04-29 Christophe Bonny Cell-permeable peptide inhibitors of the JNK signal transduction pathway
US20090118139A1 (en) * 2000-11-07 2009-05-07 Caliper Life Sciences, Inc. Microfluidic method and system for enzyme inhibition activity screening
MXPA04002243A (es) 2001-09-19 2004-06-29 Aventis Pharma Sa Compuestos quimicos.
US20040087642A1 (en) * 2002-10-24 2004-05-06 Zeldis Jerome B. Methods of using and compositions comprising a JNK inhibitor for the treatment, prevention, management and/or modification of pain
FR2857362B1 (fr) * 2003-07-10 2005-09-23 Aventis Pharma Sa Tetrahydro-1h-pyrazolo[3,4-c] pyridines substituees, compositions les contenant et utilisation
AR045037A1 (es) 2003-07-10 2005-10-12 Aventis Pharma Sa Tetrahidro-1h-pirazolo [3,4-c] piridinas sustituidas, composiciones que las contienen y su utilizacion.
GB0324159D0 (en) * 2003-10-15 2003-11-19 Glaxo Group Ltd Novel compounds
DE602005014964D1 (de) 2004-04-02 2009-07-30 Osi Pharm Inc Mit einem 6,6-bicyclischen ring substituierte heterobicyclische proteinkinaseinhibitoren
AR053090A1 (es) 2004-07-20 2007-04-25 Osi Pharm Inc Imidazotriazinas como inhibidores de proteina quinasas y su uso para la preparacion de medicamentos
US7803824B2 (en) 2004-10-29 2010-09-28 Alcon, Inc. Use of inhibitors of Jun N-terminal kinases to treat glaucoma
US20060094753A1 (en) 2004-10-29 2006-05-04 Alcon, Inc. Use of inhibitors of Jun N-terminal kinases for the treatment of glaucomatous retinopathy and ocular diseases
RS52711B (sr) 2005-05-10 2013-08-30 Incyte Corporation Modulatori indolamin 2,3-dioksigenaze i postupci upotrebe istih
WO2007031098A1 (en) 2005-09-12 2007-03-22 Xigen S.A. Cell-permeable peptide inhibitors of the jnk signal transduction pathway
EP1926996B1 (en) 2005-09-20 2011-11-09 OSI Pharmaceuticals, Inc. Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
JP5119154B2 (ja) 2005-09-22 2013-01-16 インサイト・コーポレイション Ｊａｎｕｓキナーゼの四環系阻害剤
AR057960A1 (es) 2005-12-02 2007-12-26 Osi Pharm Inc Inhibidores de proteina quinasa biciclicos
TWI630207B (zh) 2005-12-13 2018-07-21 英塞特控股公司 作為傑納斯激酶（ＪＡＮＵＳ ＫＩＮＡＳＥ）抑制劑之經雜芳基取代之吡咯并〔２，３-ｂ〕吡啶及吡咯并〔２，３-ｂ〕嘧啶
DE102006049452A1 (de) 2006-10-17 2008-05-08 Grünenthal GmbH Substituierte Tetrahydropyrolopiperazin-Verbindungen und deren Verwendung in Arzneimitteln
EP2121692B1 (en) 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
EP3070090B1 (en) 2007-06-13 2018-12-12 Incyte Holdings Corporation Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
CN101848903A (zh) * 2007-09-06 2010-09-29 葛兰素集团有限公司 对组胺h3受体具有亲和性的哌嗪衍生物
ES2569528T3 (es) 2007-11-16 2016-05-11 Incyte Holdings Corporation 4-pirazolil-N-arilpirimidin-2-aminas y 4-pirazolil-N-heteroarilpirimidin-2-aminas como inhibidores de quinasas Janus
NZ586575A (en) 2007-12-21 2012-03-30 Genentech Inc Azaindolizines and methods of use
PL2288610T3 (pl) 2008-03-11 2017-12-29 Incyte Holdings Corporation Azetydynowe i cyklobutanowe pochodne jako inhibitory jak
US8871753B2 (en) 2008-04-24 2014-10-28 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
DE102008022657A1 (de) * 2008-05-07 2009-11-19 Knorr-Bremse Systeme für Nutzfahrzeuge GmbH Achsaggregat und Lenker
WO2009143865A1 (en) * 2008-05-30 2009-12-03 Xigen S.A. Use of cell-permeable peptide inhibitors of the jnk signal transduction pathway for the treatment of various diseases
WO2009143864A1 (en) 2008-05-30 2009-12-03 Xigen S.A. Use of cell-permeable peptide inhibitors of the jnk signal transduction pathway for the treatment of chronic or non-chronic inflammatory digestive diseases
PL2315756T3 (pl) 2008-07-08 2015-02-27 Incyte Holdings Corp 1,2,5-oksadiazole jako inhibitory 2,3-dioksygenazy indoloaminy
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
MX2011004824A (es) 2008-11-07 2012-01-12 Triact Therapeutics Inc Uso de derivados de butano catecólico en terapia contra el cáncer.
US8835422B2 (en) * 2008-12-11 2014-09-16 Cara Therapeutics, Inc. Substituted imidazoheterocycle derivatives
WO2010072228A1 (en) 2008-12-22 2010-07-01 Xigen S.A. Novel transporter constructs and transporter cargo conjugate molecules
WO2010085597A1 (en) 2009-01-23 2010-07-29 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
EP2400985A2 (en) 2009-02-25 2012-01-04 OSI Pharmaceuticals, LLC Combination of an either an anti-igf-1r antibody or an igf binding protein and a small molecule igf-1r kinase inhibitor
JP2012519170A (ja) 2009-02-26 2012-08-23 オーエスアイ・ファーマシューティカルズ，エルエルシー 生体内の腫瘍細胞のｅｍｔステータスをモニターするためのｉｎｓｉｔｕ法
WO2010099138A2 (en) 2009-02-27 2010-09-02 Osi Pharmaceuticals, Inc. Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
EP2401614A1 (en) 2009-02-27 2012-01-04 OSI Pharmaceuticals, LLC Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation
JP2012519282A (ja) 2009-02-27 2012-08-23 オーエスアイ・ファーマシューティカルズ，エルエルシー 間葉様腫瘍細胞またはその生成を阻害する薬剤を同定するための方法
JP2012524119A (ja) 2009-04-20 2012-10-11 オーエスアイ・ファーマシューティカルズ，エルエルシー Ｃ−ピラジン−メチルアミンの調製
EP3643312A1 (en) 2009-05-22 2020-04-29 Incyte Holdings Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
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
EP2448938B9 (en) 2009-06-29 2015-06-10 Incyte Corporation Pyrimidinones as pi3k inhibitors
AR078012A1 (es) 2009-09-01 2011-10-05 Incyte Corp Derivados heterociclicos de las pirazol-4-il- pirrolo (2,3-d) pirimidinas como inhibidores de la quinasa janus
CN105541847B (zh) 2009-10-09 2019-08-16 因西特控股公司 3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的羟基衍生物、酮基衍生物和葡糖苷酸衍生物
AR079529A1 (es) 2009-12-18 2012-02-01 Incyte Corp Derivados arilo y heteroarilo sustituidos y fundidos como inhibidores de la pi3k
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
CN102844317B (zh) 2010-02-18 2015-06-03 因西特公司 作为Janus激酶抑制剂的环丁烷和甲基环丁烷衍生物
EP2519826A2 (en) 2010-03-03 2012-11-07 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
AU2011223655A1 (en) 2010-03-03 2012-06-28 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors
EP2544672A1 (en) 2010-03-09 2013-01-16 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
EP3050882B1 (en) 2010-03-10 2018-01-31 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
SG10201503983QA (en) 2010-05-21 2015-06-29 Incyte Corp Topical Formulation for a JAK Inhibitor
FR2960876B1 (fr) * 2010-06-03 2012-07-27 Sanofi Aventis Derives de 3,4-dihydropyrrolo[1,2-a]pyrazine-2,8(1h)-dicarboxamide leur preparation et leur application en therapeutique.
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
WO2011160653A1 (en) 2010-06-21 2011-12-29 Xigen S.A. Novel jnk inhibitor molecules
CA2807036C (en) 2010-10-14 2018-01-16 Xigen S.A. Use of cell-permeable peptide inhibitors of the jnk signal transduction pathway for the treatment of chronic or non-chronic inflammatory eye diseases
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
CN103415515B (zh) 2010-11-19 2015-08-26 因塞特公司 作为jak抑制剂的环丁基取代的吡咯并吡啶和吡咯并嘧啶衍生物
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
ES2547916T3 (es) 2011-02-18 2015-10-09 Novartis Pharma Ag Terapia de combinación de inhibidores de mTOR/JAK
WO2012116040A1 (en) 2011-02-22 2012-08-30 OSI Pharmaceuticals, LLC Biological markers predictive of anti-cancer response to insulin-like growth factor-1 receptor kinase inhibitors in hepatocellular carcinoma
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
US9896730B2 (en) 2011-04-25 2018-02-20 OSI Pharmaceuticals, LLC Use of EMT gene signatures in cancer drug discovery, diagnostics, and treatment
PE20140832A1 (es) 2011-06-20 2014-07-14 Incyte Corp Derivados de azetidinil fenil, piridil o pirazinil carboxamida como inhibidores de jak
HK1198579A1 (en) 2011-08-10 2015-04-30 Novartis Pharma Ag Jak p13k/mtor combination therapy
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
KR102030609B1 (ko) 2011-09-02 2019-10-11 인사이트 홀딩스 코포레이션 Ｐｉ３ｋ 억제제로서 헤테로시클릴아민
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
WO2013091670A1 (en) 2011-12-21 2013-06-27 Xigen S.A. Novel jnk inhibitor molecules for treatment of various diseases
FR2986002B1 (fr) * 2012-01-24 2014-02-21 Servier Lab Nouveaux derives d'indolizine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
WO2013152252A1 (en) 2012-04-06 2013-10-10 OSI Pharmaceuticals, LLC Combination anti-cancer therapy
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
US9611267B2 (en) 2012-06-13 2017-04-04 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
AU2013337824B2 (en) 2012-11-01 2018-03-08 Incyte Holdings Corporation Tricyclic fused thiophene derivatives as JAK inhibitors
PL2919766T3 (pl) 2012-11-15 2021-10-04 Incyte Holdings Corporation Postacie dawkowania ruksolitynibu o przedłużonym uwalnianiu
US9834575B2 (en) 2013-02-26 2017-12-05 Triact Therapeutics, Inc. Cancer therapy
TWI736135B (zh) 2013-03-01 2021-08-11 美商英塞特控股公司 吡唑并嘧啶衍生物治療PI3Kδ相關病症之用途
CN105189509B (zh) 2013-03-06 2017-12-19 因赛特公司 用于制备jak抑制剂的方法及中间体
TWI649318B (zh) 2013-04-19 2019-02-01 英塞特控股公司 作為ｆｇｆｒ抑制劑之雙環雜環
SMT202100040T1 (it) 2013-05-17 2021-03-15 Incyte Corp Derivati di bipirazolo come inibitori di jak
WO2014206427A1 (en) 2013-06-26 2014-12-31 Xigen Inflammation Ltd. New use of cell-permeable peptide inhibitors of the jnk signal transduction pathway for the treatment of various diseases
WO2015197097A1 (en) 2014-06-26 2015-12-30 Xigen Inflammation Ltd. New use for jnk inhibitor molecules for treatment of various diseases
CN105307670A (zh) 2013-06-26 2016-02-03 埃克西金炎症有限公司 Jnk信号转导途径的细胞渗透肽抑制剂用于治疗多种疾病的新用途
FR3008976A1 (fr) * 2013-07-23 2015-01-30 Servier Lab "nouveaux derives d'indolizine, leur procede de preparation et les compositions pharmaceutiques qui les contiennent"
SG10201912203XA (en) 2013-08-07 2020-02-27 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
EP3035966A1 (en) 2013-08-20 2016-06-29 Incyte Corporation Survival benefit in patients with solid tumors with elevated c-reactive protein levels
CA2923667A1 (en) 2013-09-09 2015-03-12 Triact Therapeutics, Inc. Cancer therapy
UY35834A (es) * 2013-11-14 2015-05-29 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Piperazinas de pirazolo sustituido como inhibidores de caseína quinasa 1 delta y epsilon
US10787410B2 (en) 2013-12-16 2020-09-29 The Johns Hopkins University Treating and preventing diseases by modulating cell mechanics
CA2940659C (en) 2014-02-28 2023-01-03 Incyte Corporation Jak1 inhibitors for the treatment of myelodysplastic syndromes
CN106132963B (zh) * 2014-04-07 2019-08-06 荷兰转化研究中心有限责任公司 (5,6-二氢)嘧啶并[4,5-e]吲嗪
KR20240153401A (ko) 2014-04-08 2024-10-22 인사이트 홀딩스 코포레이션 Ｊａｋ 및 ｐｉ3ｋ 억제제 조합에 의한 ｂ-세포 악성종양의 치료
JP2017514832A (ja) 2014-04-30 2017-06-08 インサイト・コーポレイションＩｎｃｙｔｅ Ｃｏｒｐｏｒａｔｉｏｎ Ｊａｋ１抑制剤を調製する方法及びその新しい形態
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
US9586949B2 (en) 2015-02-09 2017-03-07 Incyte Corporation Aza-heteroaryl compounds as PI3K-gamma inhibitors
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
AU2016219822B2 (en) 2015-02-20 2020-07-09 Incyte Holdings Corporation Bicyclic heterocycles as FGFR inhibitors
DK3831833T3 (da) 2015-02-27 2022-11-14 Incyte Holdings Corp Fremgangsmåder til fremstillingen af en pi3k-inhibitor
WO2016183062A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Salts of (s)-7-(1-(9h-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5h-thiazolo[3,2-a]pyrimidin-5-one
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
EP4086259A1 (en) 2015-11-06 2022-11-09 Incyte Corporation Heterocyclic compounds as pi3k-gamma inhibitors
WO2017120194A1 (en) 2016-01-05 2017-07-13 Incyte Corporation Pyridine and pyridimine compounds as pi3k-gamma inhibitors
CN105646495A (zh) * 2016-01-06 2016-06-08 中山大学 一种吡咯并[2,3-b]吡嗪衍生物及其制备方法和应用
EP3203509B1 (en) 2016-02-04 2021-01-20 Services Pétroliers Schlumberger Double-sided hermetic multichip module
WO2017223414A1 (en) 2016-06-24 2017-12-28 Incyte Corporation HETEROCYCLIC COMPOUNDS AS PI3K-γ INHIBITORS
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
WO2019020070A1 (zh) * 2017-07-27 2019-01-31 江苏恒瑞医药股份有限公司 哌嗪并杂芳基类衍生物、其制备方法及其在医药上的应用
IL295978B2 (en) 2017-10-18 2024-01-01 Incyte Corp Condensed imidazole derivatives substituted by tertiary hydroxy groups as pi3k-gamma inhibitors
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
WO2019126505A1 (en) 2017-12-21 2019-06-27 Incyte Corporation 3-(5-amino-pyrazin-2-yl)-benzenesulfonamide derivatives and related compounds as pi3k-gamma kinase inhibitors for treating e.g. cancer
EP3746429B1 (en) 2018-01-30 2022-03-09 Incyte Corporation Processes for preparing (1-(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
KR102830476B1 (ko) 2018-02-16 2025-07-08 인사이트 코포레이션 사이토카인-관련 장애의 치료를 위한 jak1 경로 억제제
US20190292188A1 (en) 2018-02-27 2019-09-26 Incyte Corporation Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors
TWI903299B (zh) 2018-03-08 2025-11-01 美商英塞特公司 作為PI3K-γ抑制劑之胺基吡嗪二醇化合物
PT3773593T (pt) 2018-03-30 2024-06-25 Incyte Corp Tratamento da hidradenite supurativa com inibidores de jak
US11220510B2 (en) 2018-04-09 2022-01-11 Incyte Corporation Pyrrole tricyclic compounds as A2A / A2B inhibitors
ES2991427T3 (es) 2018-05-04 2024-12-03 Incyte Corp Formas sólidas de un inhibidor de FGFR y procedimientos para preparar las mismas
TW201946630A (zh) 2018-05-04 2019-12-16 美商英塞特公司 Fgfr抑制劑之鹽
MA52940A (fr) 2018-05-18 2021-04-28 Incyte Corp Dérivés de pyrimidine fusionnés utilisés en tant qu'inhibiteurs de a2a/a2b
US10947227B2 (en) 2018-05-25 2021-03-16 Incyte Corporation Tricyclic heterocyclic compounds as sting activators
CN119258070A (zh) 2018-06-01 2025-01-07 因赛特公司 治疗pi3k相关病症的给药方案
WO2020010003A1 (en) 2018-07-02 2020-01-09 Incyte Corporation AMINOPYRAZINE DERIVATIVES AS PI3K-γ INHIBITORS
CN113166153B (zh) 2018-07-05 2024-11-01 因赛特公司 作为a2a/a2b抑制剂的稠合吡嗪衍生物
US10875872B2 (en) 2018-07-31 2020-12-29 Incyte Corporation Heteroaryl amide compounds as sting activators
US11008344B2 (en) 2018-07-31 2021-05-18 Incyte Corporation Tricyclic heteroaryl compounds as STING activators
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
US11066404B2 (en) 2018-10-11 2021-07-20 Incyte Corporation Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors
WO2020102216A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Substituted heterocyclic derivatives as pi3k inhibitors
WO2020102150A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
WO2020102198A1 (en) 2018-11-13 2020-05-22 Incyte Corporation Heterocyclic derivatives as pi3k inhibitors
US11596692B1 (en) 2018-11-21 2023-03-07 Incyte Corporation PD-L1/STING conjugates and methods of use
WO2020146237A1 (en) 2019-01-07 2020-07-16 Incyte Corporation Heteroaryl amide compounds as sting activators
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
US11384083B2 (en) 2019-02-15 2022-07-12 Incyte Corporation Substituted spiro[cyclopropane-1,5′-pyrrolo[2,3-d]pyrimidin]-6′(7′h)-ones as CDK2 inhibitors
MA54947A (fr) 2019-02-15 2021-12-22 Incyte Corp Biomarqueurs de kinase 2 dépendant de la cycline et leurs utilisations
US11472791B2 (en) 2019-03-05 2022-10-18 Incyte Corporation Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2020205560A1 (en) 2019-03-29 2020-10-08 Incyte Corporation Sulfonylamide compounds as cdk2 inhibitors
US11447494B2 (en) 2019-05-01 2022-09-20 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
US11440914B2 (en) 2019-05-01 2022-09-13 Incyte Corporation Tricyclic amine compounds as CDK2 inhibitors
WO2020252012A1 (en) 2019-06-10 2020-12-17 Incyte Corporation Topical treatment of vitiligo by a jak inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
WO2021022172A1 (en) 2019-08-01 2021-02-04 Incyte Corporation A dosing regimen for an ido inhibitor
MX2022001940A (es) 2019-08-14 2022-05-10 Incyte Corp Compuestos de imidazolil pirimidinilamina como inhibidores de cdk2.
CA3150766A1 (en) 2019-08-26 2021-03-04 Incyte Corporation Triazolopyrimidines as a2a / a2b inhibitors
WO2021067374A1 (en) 2019-10-01 2021-04-08 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN119930610A (zh) 2019-10-11 2025-05-06 因赛特公司 作为cdk2抑制剂的双环胺
GEAP202415945A (en) 2019-10-14 2024-04-25 Incyte Corp Bicyclic heterocycles as fgfr inhibitors
WO2021076728A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
US11992490B2 (en) 2019-10-16 2024-05-28 Incyte Corporation Use of JAK1 inhibitors for the treatment of cutaneous lupus erythematosus and Lichen planus (LP)
JP7518900B2 (ja) 2019-10-16 2024-07-18 インサイト・コーポレイション 皮膚エリテマトーデス及び扁平苔癬（ｌｐ）の治療のためのｊａｋ１阻害剤の使用
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
AU2020395185A1 (en) 2019-12-04 2022-06-02 Incyte Corporation Derivatives of an FGFR inhibitor
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
EP4114401A1 (en) 2020-03-06 2023-01-11 Incyte Corporation Combination therapy comprising axl/mer and pd-1/pd-l1 inhibitors
BR112022018976A2 (pt) * 2020-03-26 2022-11-01 Univ Leland Stanford Junior Métodos para regeneração de tecido e kits para os mesmos
IL297165A (en) 2020-04-16 2022-12-01 Incyte Corp Soysag tricyclic CRS inhibitors
US11739102B2 (en) 2020-05-13 2023-08-29 Incyte Corporation Fused pyrimidine compounds as KRAS inhibitors
CN115836065B (zh) 2020-06-02 2025-07-01 因赛特公司 制备jak1抑制剂的方法
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022047093A1 (en) 2020-08-28 2022-03-03 Incyte Corporation Vinyl imidazole compounds as inhibitors of kras
WO2022061351A1 (en) 2020-09-16 2022-03-24 Incyte Corporation Topical treatment of vitiligo
US11767320B2 (en) 2020-10-02 2023-09-26 Incyte Corporation Bicyclic dione compounds as inhibitors of KRAS
AU2021396231A1 (en) 2020-12-08 2023-06-22 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
WO2022155941A1 (en) 2021-01-25 2022-07-28 Qilu Regor Therapeutics Inc. Cdk2 inhibitors
WO2022206888A1 (en) 2021-03-31 2022-10-06 Qilu Regor Therapeutics Inc. Cdk2 inhibitors and use thereof
EP4323405A1 (en) 2021-04-12 2024-02-21 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
SI4333840T1 (sl) 2021-05-03 2026-01-30 Incyte Corporation Zaviralci poti jak1 za zdravljenje pruriga nodularisa
AR126101A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
US11981671B2 (en) 2021-06-21 2024-05-14 Incyte Corporation Bicyclic pyrazolyl amines as CDK2 inhibitors
CA3224674A1 (en) 2021-07-07 2023-01-12 Pei Gan Tricyclic compounds as inhibitors of kras
EP4370515A1 (en) 2021-07-14 2024-05-22 Incyte Corporation Tricyclic compounds as inhibitors of kras
CA3229855A1 (en) 2021-08-31 2023-03-09 Incyte Corporation Naphthyridine compounds as inhibitors of kras
US12030883B2 (en) 2021-09-21 2024-07-09 Incyte Corporation Hetero-tricyclic compounds as inhibitors of KRAS
WO2023056421A1 (en) 2021-10-01 2023-04-06 Incyte Corporation Pyrazoloquinoline kras inhibitors
IL312114A (en) 2021-10-14 2024-06-01 Incyte Corp Quinoline compounds as Kras inhibitors
JP2024542248A (ja) 2021-11-22 2024-11-13 インサイト・コーポレイション Ｆｇｆｒ阻害剤とｋｒａｓ阻害剤を含む併用療法
US20230203010A1 (en) 2021-12-03 2023-06-29 Incyte Corporation Bicyclic amine cdk12 inhibitors
US11976073B2 (en) 2021-12-10 2024-05-07 Incyte Corporation Bicyclic amines as CDK2 inhibitors
WO2023107705A1 (en) 2021-12-10 2023-06-15 Incyte Corporation Bicyclic amines as cdk12 inhibitors
TW202340215A (zh) 2021-12-22 2023-10-16 美商英塞特公司 Ｆｇｆｒ抑制劑之鹽及固體形式以及其製備方法
WO2023116884A1 (en) 2021-12-24 2023-06-29 Qilu Regor Therapeutics Inc. Cdk2 inhibitors and use thereof
WO2023168686A1 (en) 2022-03-11 2023-09-14 Qilu Regor Therapeutics Inc. Substituted cyclopentanes as cdk2 inhibitors
CR20240408A (es) 2022-03-07 2024-11-22 Incyte Corp Formas sólidas, sales y procesos de preparación de un inhibidor de cdk2.
EP4540252A1 (en) 2022-06-14 2025-04-23 Incyte Corporation Solid forms of a jak inhibitor and process of preparing the same
WO2023250430A1 (en) 2022-06-22 2023-12-28 Incyte Corporation Bicyclic amine cdk12 inhibitors
WO2024015731A1 (en) 2022-07-11 2024-01-18 Incyte Corporation Fused tricyclic compounds as inhibitors of kras g12v mutants
EP4565229A1 (en) 2022-08-05 2025-06-11 Incyte Corporation Treatment of urticaria using jak inhibitors
WO2024220532A1 (en) 2023-04-18 2024-10-24 Incyte Corporation Pyrrolidine kras inhibitors
EP4698542A1 (en) 2023-04-18 2026-02-25 Incyte Corporation 2-azabicyclo[2.2.1]heptane kras inhibitors
WO2024254245A1 (en) 2023-06-09 2024-12-12 Incyte Corporation Bicyclic amines as cdk2 inhibitors
WO2025096738A1 (en) 2023-11-01 2025-05-08 Incyte Corporation Kras inhibitors
US20250195536A1 (en) 2023-12-13 2025-06-19 Incyte Corporation Bicyclooctane kras inhibitors
KR20260035991A (ko) 2024-08-26 2026-03-13 인사이트 코포레이션 룩소리티닙의 약학적으로 허용 가능한 염의 국소 피부 제형

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS57123183A (en) * 1981-01-24 1982-07-31 Yoshitomi Pharmaceut Ind Ltd Pyrroloimidazole derivative and its preparation
IT1214644B (it) * 1985-12-10 1990-01-18 Consiglio Nazionale Ricerche Composti eterociclici dotati di attivita' terapeutica.
JPH0753511A (ja) * 1993-08-11 1995-02-28 Fuji Photo Film Co Ltd β−アルコキシカルボニルピロール化合物の製造方法
AU2001243163B2 (en) * 2000-03-14 2004-11-04 Pharmacia & Upjohn Company Novel 2,3,4,5-tetrahydro-1H-(1,4)diazepino(1,7a)indole compounds
MXPA04002243A (es) 2001-09-19 2004-06-29 Aventis Pharma Sa Compuestos quimicos.

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