JP5555620B2 - オキサゾールチロシンキナーゼ阻害剤 - Google Patents

オキサゾールチロシンキナーゼ阻害剤 Download PDF

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JP5555620B2
JP5555620B2 JP2010506999A JP2010506999A JP5555620B2 JP 5555620 B2 JP5555620 B2 JP 5555620B2 JP 2010506999 A JP2010506999 A JP 2010506999A JP 2010506999 A JP2010506999 A JP 2010506999A JP 5555620 B2 JP5555620 B2 JP 5555620B2
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optionally substituted
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alkyl
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phenyl
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JP2010526800A (ja
JP2010526800A5 (OSRAM
Inventor
ジョン・チャールズ・リーダー
ジョン・マーク・エラード
ヘレン・ボフィー
スザンヌ・テイラー
アンドリュー・デイビッド・カー
マイケル・チェリー
ミシェル・ウィルソン
リチャード・ボーキェ・オウォーア
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Sareum Ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/48—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
JP2010506999A 2007-05-10 2008-05-09 オキサゾールチロシンキナーゼ阻害剤 Active JP5555620B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US91719107P 2007-05-10 2007-05-10
GBGB0709031.9A GB0709031D0 (en) 2007-05-10 2007-05-10 Pharmaceutical compounds
US60/917,191 2007-05-10
GB0709031.9 2007-05-10
US98727307P 2007-11-12 2007-11-12
US60/987,273 2007-11-12
PCT/GB2008/001612 WO2008139161A1 (en) 2007-05-10 2008-05-09 Oxazole tyrosine kinase inhibitors

Publications (3)

Publication Number Publication Date
JP2010526800A JP2010526800A (ja) 2010-08-05
JP2010526800A5 JP2010526800A5 (OSRAM) 2011-06-23
JP5555620B2 true JP5555620B2 (ja) 2014-07-23

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ID=38219198

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JP2010506999A Active JP5555620B2 (ja) 2007-05-10 2008-05-09 オキサゾールチロシンキナーゼ阻害剤

Country Status (6)

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US (4) US8378095B2 (OSRAM)
EP (1) EP2170849B1 (OSRAM)
JP (1) JP5555620B2 (OSRAM)
CN (1) CN101796038B (OSRAM)
GB (1) GB0709031D0 (OSRAM)
WO (1) WO2008139161A1 (OSRAM)

Families Citing this family (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101391900B1 (ko) 2005-12-13 2014-05-02 인사이트 코포레이션 야누스 키나아제 억제제로서의 헤테로아릴 치환된 피롤로［2,3-ｂ］피리딘 및 피롤로［2,3-ｂ］피리미딘
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds
WO2008157208A2 (en) 2007-06-13 2008-12-24 Incyte Corporation Salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
US9029411B2 (en) 2008-01-25 2015-05-12 Millennium Pharmaceuticals, Inc. Thiophenes and uses thereof
WO2010005841A1 (en) * 2008-07-09 2010-01-14 Merck & Co., Inc. Inhibitors of janus kinases
GB0820819D0 (en) * 2008-11-13 2008-12-24 Sareum Ltd Pharmaceutical compounds
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9139589B2 (en) 2009-01-30 2015-09-22 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
JP5656880B2 (ja) 2009-03-09 2015-01-21 グラクソ グループ リミテッドＧｌａｘｏ Ｇｒｏｕｐ Ｌｉｍｉｔｅｄ Ｐｉ３キナーゼの阻害剤としての４−オキサジアゾール−２−イル−インダゾール
WO2010127152A2 (en) * 2009-04-29 2010-11-04 Irm Llc Compounds and compositions as microsomal prostaglandin e synthase-1 inhibitors
MY160454A (en) 2009-04-30 2017-03-15 Glaxo Group Ltd Oxazole substituted indazoles as pi3-kinase inhibitors
TW201100429A (en) 2009-05-22 2011-01-01 Incyte Corp N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
DK2432472T3 (da) 2009-05-22 2019-11-18 Incyte Holdings Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octan- eller heptan-nitril som jak-inhibitorer
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
PH12015502575A1 (en) 2010-03-10 2017-04-24 Incyte Corp Piperidin-4-yl azetidine derivatives as jak1 inhibitors
EP3087972A1 (en) 2010-05-21 2016-11-02 Incyte Holdings Corporation Topical formulation for a jak inhibitor
EP2575815A4 (en) 2010-06-04 2013-12-25 Albany Molecular Res Inc GLYCIN TRANSPORTER 1 INHIBITORS, METHODS OF MAKING THE SAME, AND USES THEREOF
JP2013533318A (ja) * 2010-08-11 2013-08-22 ミレニアム ファーマシューティカルズ， インコーポレイテッド ヘテロアリールおよびその使用
US9062038B2 (en) 2010-08-11 2015-06-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
MA34797B1 (fr) 2010-08-11 2014-01-02 Millennium Pharm Inc Hétéroaryles et leurs utilisations
US9326987B2 (en) 2010-09-08 2016-05-03 Glaxo Group Limited Indazole derivatives for use in the treatment of influenza virus infection
PH12013500723A1 (en) 2010-10-13 2017-08-23 Millennium Pharm Inc Heteroaryls and uses thereof
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
CA2818545C (en) 2010-11-19 2019-04-16 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
EP2712290A4 (en) 2011-05-19 2014-11-19 Univ Leland Stanford Junior ANTIPROLIFERATIVE COMPOUNDS AND METHOD FOR THEIR USE
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
EP2727920B1 (en) 2011-07-29 2016-11-02 FUJIFILM Corporation 1,5-naphthyridine derivative or salt thereof
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
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
US20130165472A1 (en) * 2011-12-23 2013-06-27 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
GB201202027D0 (en) * 2012-02-06 2012-03-21 Sareum Ltd Pharmaceutical compounds
DK3040336T3 (da) * 2012-03-02 2020-06-22 Sareum Ltd Forbindelser til brug i behandling af TYK2 Kinase-medierede tilstande
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
EP3949953A1 (en) 2012-11-15 2022-02-09 Incyte Holdings Corporation Sustained-release dosage forms of ruxolitinib
BR112015021458B1 (pt) 2013-03-06 2022-06-07 Incyte Holdings Corporation "processos e intermediários para preparar {1-{1-[3-flúor2-(trifluormetil)isonicotinoil] piperidin-4-il}-3-[4-(7hpirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]azetidin-3-il}acetonitrila, útil no tratamento de doenças relacionadas com a atividade de janus quinases
WO2015021153A1 (en) 2013-08-07 2015-02-12 Incyte Corporation Sustained release dosage forms for a jak1 inhibitor
RU2652795C2 (ru) * 2013-09-03 2018-05-03 Сареум Лимитед Производные 2-фенил-оксазол-4-карбоксамида, модулирующие активность jak и tyk2 киназ
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
US10000474B2 (en) 2014-11-11 2018-06-19 Musc Foundation For Research Development Histone deacetylase inhibitors and uses thereof
ES2796276T3 (es) * 2015-02-05 2020-11-26 Ab Science Compuestos con actividad antitumoral
CN104974095B (zh) * 2015-06-30 2017-09-15 浙江大学 2,4,5‑多取代咪唑类化合物及制备方法
CN105601580B (zh) * 2015-11-29 2017-11-14 陈玉玲 一种噁唑类医药中间体化合物的合成方法
GB201617871D0 (en) 2016-10-21 2016-12-07 Sareum Limited Pharmaceutical compounds
WO2018217766A1 (en) 2017-05-22 2018-11-29 Whitehead Institute For Biomedical Research Kcc2 expression enhancing compounds and uses thereof
TW201924683A (zh) 2017-12-08 2019-07-01 美商英塞特公司 用於治療骨髓增生性贅瘤的低劑量組合療法
DK3746429T3 (da) 2018-01-30 2022-05-02 Incyte Corp Fremgangsmåder til fremstilling af (1-(3-fluor-2-(trifluormethyl)isonicotinyl)piperidin-4-on)
EP3749697A4 (en) 2018-02-05 2021-11-03 Bio-Rad Laboratories, Inc. CHROMATOGRAPHY RESIN WITH LIGAND MIXED MODE ANIONIC / HYDROPHOBIC EXCHANGE
US11472781B2 (en) 2018-02-21 2022-10-18 Southern Research Institute 2-aminoaryl-5-aryloxazole analogs for the treatment of neurodegenerative diseases
CN112423759A (zh) 2018-03-30 2021-02-26 因赛特公司 使用jak抑制剂治疗化脓性汗腺炎
WO2019222497A1 (en) 2018-05-17 2019-11-21 Southern Research Institute 2,5-aryl-thiazole analogs for the treatment of neurodegenerative diseases
GB201816369D0 (en) 2018-10-08 2018-11-28 Sareum Ltd Pharmaceutical compounds
KR20220002488A (ko) 2019-04-30 2022-01-06 셀진 코포레이션 아프레밀라스트 및 tyk2 억제제를 포함하는 조합 요법
GB202005114D0 (en) 2020-04-07 2020-05-20 Sareum Ltd Crystalline Forms of a Pharmaceutical Compound
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE794096A (fr) 1972-08-07 1973-05-16 Lepetit Spa Oxazoles 2,4,5-trisubstitues et leur preparation
JPS6155456A (ja) 1984-08-24 1986-03-19 Toyota Motor Corp 車輌用自動変速機のアイドル運転時制御方法
JPH0753716B2 (ja) 1986-07-02 1995-06-07 吉富製薬株式会社 イミダゾ−ルカルボキサミド誘導体
JPH0770133B2 (ja) 1986-12-19 1995-07-31 三菱電機株式会社 ヘツド支持機構
JPH06310767A (ja) 1993-04-26 1994-11-04 Nec Corp 寒剤容器の断熱支持構造
DE19653355A1 (de) 1996-12-20 1998-06-25 Dresden Arzneimittel Neue, antikonvulsiv wirkende Aminoimidazole und Verfahren zu ihrer Herstellung
GB0003154D0 (en) 2000-02-12 2000-04-05 Astrazeneca Uk Ltd Novel compounds
IL153246A0 (en) * 2000-06-28 2003-07-06 Astrazeneca Ab Substituted quinazoline derivatives and their use as inhibitors
JP2004512365A (ja) * 2000-10-30 2004-04-22 ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ トリペプチジルペプチダーゼ阻害剤
CA2491895C (en) 2002-07-09 2011-01-18 Vertex Pharmaceuticals Incorporated Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases
EP1651209A4 (en) * 2003-07-24 2009-03-04 Merck & Co Inc TYROSINE KINASE INHIBITORS
ATE465731T1 (de) 2003-10-23 2010-05-15 Ab Science 2-aminoaryloxazol-verbindungen als tyrosinkinase- hemmer
GB0504753D0 (en) 2005-03-08 2005-04-13 Astrazeneca Ab Chemical compounds
EP1932833B1 (en) * 2005-10-07 2012-08-01 Kissei Pharmaceutical Co., Ltd. Nitrogenated heterocyclic compound and pharmaceutical composition comprising the same
DK200600313A (da) 2006-03-03 2006-03-13 Novo Nordisk As Treating type 2 diabetes or metabolic syndrome with an interleukin 1beta inhibitor or an interleukin 1beta synthesis or release inhibitor
DE602007009085D1 (de) 2006-05-12 2010-10-21 Ab Science Neues verfahren zur synthese von 2-aminooxazolverbindungen
WO2008024980A2 (en) 2006-08-24 2008-02-28 Serenex, Inc. Pyrrole, thiophene, furan, imidazole, oxazole, and thiazole derivatives
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds

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US8921544B2 (en) 2014-12-30
CN101796038A (zh) 2010-08-04
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