UA117830C2 - Похідні біпіразолу як інгібітори jak - Google Patents

Похідні біпіразолу як інгібітори jak

Info

Publication number
UA117830C2
UA117830C2 UAA201512465A UAA201512465A UA117830C2 UA 117830 C2 UA117830 C2 UA 117830C2 UA A201512465 A UAA201512465 A UA A201512465A UA A201512465 A UAA201512465 A UA A201512465A UA 117830 C2 UA117830 C2 UA 117830C2
Authority
UA
Ukraine
Prior art keywords
jak inhibitors
jak
activity
bipyrazole derivatives
bipyrazole
Prior art date
Application number
UAA201512465A
Other languages
English (en)
Inventor
Юнь-Лун Лі
Цзіньцун Чжо
Дін-Цюань Цянь
Сун Мей
Ганьфен Цао
Юнчунь Пань
Цюнь Лі
Чжунцзян Цзя
Original Assignee
Інсайт Корпорейшн
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
Application filed by Інсайт Корпорейшн filed Critical Інсайт Корпорейшн
Publication of UA117830C2 publication Critical patent/UA117830C2/uk

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

Abstract

У даному винаході запропоновані сполуки Формули І EMBED ISISServer I або їхні фармацевтично прийнятні солі, а також їхні композиції та способи їхнього застосування, які інгібують активність Янус-кінази (JAK) і придатні для застосування для лікування захворювань, пов'язаних з активністю JAK, включаючи, наприклад, запальні захворювання, автоімунні захворювання, ракові захворювання й інші захворювання.
UAA201512465A 2013-05-17 2014-05-16 Похідні біпіразолу як інгібітори jak UA117830C2 (uk)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361824683P 2013-05-17 2013-05-17
PCT/US2014/038388 WO2014186706A1 (en) 2013-05-17 2014-05-16 Bipyrazole derivatives as jak inhibitors

Publications (1)

Publication Number Publication Date
UA117830C2 true UA117830C2 (uk) 2018-10-10

Family

ID=50983151

Family Applications (1)

Application Number Title Priority Date Filing Date
UAA201512465A UA117830C2 (uk) 2013-05-17 2014-05-16 Похідні біпіразолу як інгібітори jak

Country Status (35)

Country Link
US (6) US9382231B2 (uk)
EP (5) EP2997023B9 (uk)
JP (4) JP6415543B2 (uk)
KR (3) KR102442747B1 (uk)
CN (2) CN105452239B (uk)
AR (2) AR096330A1 (uk)
AU (5) AU2014265279B2 (uk)
BR (1) BR112015028501B8 (uk)
CA (1) CA2911536C (uk)
CL (1) CL2015003355A1 (uk)
CR (2) CR20190156A (uk)
CY (3) CY1119105T1 (uk)
DK (3) DK3527263T3 (uk)
EA (2) EA039660B1 (uk)
ES (4) ES2960731T3 (uk)
FI (1) FI3786162T3 (uk)
HK (2) HK1221466A1 (uk)
HR (4) HRP20231048T1 (uk)
HU (4) HUE033587T2 (uk)
IL (4) IL242453B (uk)
LT (4) LT2997023T (uk)
ME (2) ME02763B (uk)
MX (2) MX2015015738A (uk)
MY (1) MY174788A (uk)
PE (2) PE20160126A1 (uk)
PH (2) PH12015502563A1 (uk)
PL (4) PL3786162T3 (uk)
PT (4) PT3231801T (uk)
RS (4) RS64591B1 (uk)
SG (2) SG10201709469SA (uk)
SI (4) SI3527263T1 (uk)
TR (1) TR201905814T4 (uk)
TW (3) TW202116320A (uk)
UA (1) UA117830C2 (uk)
WO (1) WO2014186706A1 (uk)

Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103214484B (zh) 2005-12-13 2016-07-06 因塞特控股公司 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶
EP2740731B1 (en) 2007-06-13 2016-03-23 Incyte Holdings Corporation Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
US8716303B2 (en) 2009-05-22 2014-05-06 Incyte Corporation 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
HUE046493T2 (hu) 2009-05-22 2020-03-30 Incyte Holdings Corp 3-[4-(7H-Pirrolo[2,3-d]pirimidin-4-il)-lH-pirazol-l-il]oktán- vagy heptán-nitril JAK inhibitorokként
SG177384A1 (en) 2009-06-29 2012-02-28 Incyte Corp Pyrimidinones as pi3k inhibitors
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
MY175156A (en) 2010-03-10 2020-06-11 Incyte Corp Piperidin-4-yl azetidine derivatives as jak1 inhibitors
TWI499421B (zh) 2010-05-21 2015-09-11 Incyte Corp Jak抑制劑的局部製劑
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
AU2012273164B2 (en) 2011-06-20 2015-05-28 Incyte Holdings Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
MX2020004502A (es) 2011-09-02 2022-01-20 Incyte Holdings Corp Heterociclilaminas como inhibidores de fosfoinositida 3-cinasas (pi3k).
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
UA117572C2 (uk) 2012-11-01 2018-08-27 Інсайт Холдинґс Корпорейшн Трициклічні конденсовані похідні тіофену як інгібітори jak
WO2014078486A1 (en) 2012-11-15 2014-05-22 Incyte Corporation Sustained-release dosage forms of ruxolitinib
ES2707355T3 (es) 2013-03-06 2019-04-03 Incyte Holdings Corp Procesos y productos intermedios para elaborar un inhibidor de JAK
ME02763B (me) 2013-05-17 2018-01-20 Incyte Corp Derivati bipirazola kao inhibitori jak
CA3155500A1 (en) 2013-08-07 2015-02-12 Incyte Corporation Sustained release dosage forms for a jak1 inhibitor
PE20161388A1 (es) * 2014-02-28 2016-12-28 Incyte Corp Inhibidores de la jak1 para el tratamiento de sindromes mielodisplasicos
PL3129021T3 (pl) 2014-04-08 2021-05-31 Incyte Corporation Leczenie nowotworów złośliwych z komórek b za pomocą skojarzenia inhibitora jak i pi3k
CA2947418A1 (en) 2014-04-30 2015-11-05 Incyte Corporation Processes of preparing a jak1 inhibitor and new forms thereto
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
US9421199B2 (en) 2014-06-24 2016-08-23 Sydnexis, Inc. Ophthalmic composition
WO2016172712A2 (en) 2015-04-23 2016-10-27 Sydnexis, Inc. Ophthalmic composition
US11382909B2 (en) 2014-09-05 2022-07-12 Sydnexis, Inc. Ophthalmic composition
US9586949B2 (en) 2015-02-09 2017-03-07 Incyte Corporation Aza-heteroaryl compounds as PI3K-gamma inhibitors
NZ734993A (en) 2015-02-27 2024-03-22 Incyte Holdings Corp Salts of pi3k inhibitor and processes for their preparation
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
EP3302426A4 (en) * 2015-05-29 2018-12-05 Sydnexis, Inc. D2o stabilized pharmaceutical formulations
MA43169B1 (fr) 2015-11-06 2022-05-31 Incyte Corp Composés héterocycliques en tant qu' inhibiteurs pi3k-gamma
TW201734003A (zh) 2016-01-05 2017-10-01 英塞特公司 作為PI3K-γ抑制劑之吡啶及嘧啶化合物
US10138248B2 (en) 2016-06-24 2018-11-27 Incyte Corporation Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines, substituted imidazo[1,2-b]pyridazines and substituted imidazo[1,2-a]pyrazines as PI3K-γ inhibitors
CN107759623B (zh) * 2016-08-23 2020-08-14 苏州旺山旺水生物医药有限公司 Jak抑制剂的中间体及其制备方法
BR112019004486A2 (pt) * 2016-09-06 2019-05-28 Hoffmann La Roche compostos de 8-(azetidin-1-il)-[1,2,4] triazolo [1,5a] piridinil, composições e métodos de uso dos mesmos
WO2019079469A1 (en) 2017-10-18 2019-04-25 Incyte Corporation CONDENSED IMIDAZOLE DERIVATIVES SUBSTITUTED WITH HYDROXY TERTIARY GROUPS AS INHIBITORS OF PI3K-GAMMA
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
MA51771B1 (fr) 2018-01-30 2022-03-31 Incyte Corp Procédés de préparation de (1-(3-fluoro-2-(trifluorométhyl)isonicotinyl)pipéridine-4-one)
MX2020008521A (es) 2018-02-16 2020-12-03 Incyte Corp Inhibidores de la vía de cinasa janus 1 (jak1) para el tratamiento de trastornos relacionados con citocinas.
EP3775284A1 (en) 2018-03-30 2021-02-17 Incyte Corporation Biomarkers for inflammatory skin disease
PE20210402A1 (es) * 2018-03-30 2021-03-02 Incyte Corp Tratamiento de la hidradenitis supurativa mediante el uso de inhibidores de jak
WO2019200030A1 (en) * 2018-04-13 2019-10-17 Incyte Corporation Biomarkers for graft-versus-host disease
CN108484468A (zh) * 2018-05-11 2018-09-04 南京大学 芳基氮杂环丁烷类化合物的制备方法
DK3847175T3 (da) 2018-09-05 2024-03-18 Incyte Corp Krystallinske former af en phosphoinositid-3-kinase- (pi3k) inhibitor
SG11202104321PA (en) 2018-10-31 2021-05-28 Incyte Corp Combination therapy for treatment of hematological diseases
US11596632B2 (en) 2018-12-19 2023-03-07 Incyte Corporation JAK1 pathway inhibitors for the treatment of gastrointestinal disease
CA3132371A1 (en) 2019-03-05 2020-09-10 Incyte Corporation Jak1 pathway inhibitors for the treatment of chronic lung allograft dysfunction
TW202102222A (zh) 2019-03-19 2021-01-16 美商英塞特公司 白斑病之生物標記物
WO2020188015A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
WO2021072098A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
JP2022551649A (ja) 2019-10-10 2022-12-12 インサイト・コーポレイション 移植片対宿主病のバイオマーカー
JP2023506118A (ja) * 2019-10-16 2023-02-15 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
WO2021089791A1 (en) 2019-11-08 2021-05-14 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the treatment of cancers that have acquired resistance to kinase inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
AR122505A1 (es) 2020-06-02 2022-09-14 Incyte Corp Procesos para preparar un inhibidor de jak1
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN117043152A (zh) 2020-08-18 2023-11-10 因赛特公司 用于制备jak1抑制剂的方法和中间体
CR20230129A (es) 2020-08-18 2023-07-13 Incyte Corp Proceso e intermediarios para preparar un inhibidor de jak
CN112159394B (zh) * 2020-10-09 2021-10-22 嘉兴特科罗生物科技有限公司 一种作为jak激酶抑制剂的小分子化合物及其用途
US20220202834A1 (en) 2020-12-04 2022-06-30 Incyte Corporation Jak inhibitor with a vitamin d analog for treatment of skin diseases
TW202237089A (zh) 2020-12-08 2022-10-01 美商英塞特公司 用於治療白斑病之jak1途徑抑制劑
CN114099514A (zh) * 2020-12-29 2022-03-01 上海岸阔医药科技有限公司 预防或治疗egfr功能异常相关的副作用的方法
WO2022150676A1 (en) 2021-01-11 2022-07-14 Incyte Corporation Combination therapy comprising jak pathway inhibitor and rock inhibitor
US20220378746A1 (en) 2021-05-03 2022-12-01 Incyte Corporation Jak1 pathway inhibitors for the treatment of prurigo nodularis
WO2024030600A1 (en) 2022-08-05 2024-02-08 Incyte Corporation Treatment of urticaria using jak inhibitors
CN117186078A (zh) * 2023-11-06 2023-12-08 药康众拓(北京)医药科技有限公司 氘代氮杂环丁烷类jak抑制剂药物及用途

Family Cites Families (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5646749A (en) * 1979-09-26 1981-04-28 Mitsui Toatsu Chemicals Protective sheet for surface
JPS60106847U (ja) 1983-12-27 1985-07-20 富士重工業株式会社 室外後写鏡
JP2650681B2 (ja) 1987-07-10 1997-09-03 株式会社ブリヂストン 空気ばね
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
AU5620299A (en) 1998-08-11 2000-03-06 Novartis Ag Isoquinoline derivatives with angiogenesis inhibiting activity
US6133031A (en) 1999-08-19 2000-10-17 Isis Pharmaceuticals Inc. Antisense inhibition of focal adhesion kinase expression
GB9905075D0 (en) 1999-03-06 1999-04-28 Zeneca Ltd Chemical compounds
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
PL202623B1 (pl) 2000-06-28 2009-07-31 Smithkline Beecham Plc Sposób wytwarzania drobno zmielonego preparatu substancji leczniczej, drobno zmielona substancja lecznicza wytworzona tym sposobem i zawierająca ją kompozycja farmaceutyczna
MXPA04002243A (es) 2001-09-19 2004-06-29 Aventis Pharma Sa Compuestos quimicos.
DE60213842T2 (de) 2001-10-30 2007-09-06 Novartis Ag Staurosporin-derivate als hemmer der flt3-rezeptor-tyrosinkinase-wirkung
PE20040522A1 (es) 2002-05-29 2004-09-28 Novartis Ag Derivados de diarilurea dependientes de la cinasa de proteina
GB0215676D0 (en) 2002-07-05 2002-08-14 Novartis Ag Organic compounds
AR042052A1 (es) 2002-11-15 2005-06-08 Vertex Pharma Diaminotriazoles utiles como inhibidores de proteinquinasas
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
AR045944A1 (es) 2003-09-24 2005-11-16 Novartis Ag Derivados de isoquinolina 1.4-disustituidas
CN101106983A (zh) 2004-11-24 2008-01-16 诺瓦提斯公司 JAK抑制剂与至少一种Bcr-Abl、Flt-3、FAK或RAF激酶抑制剂的组合
CN103214484B (zh) 2005-12-13 2016-07-06 因塞特控股公司 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶
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.
EP2740731B1 (en) 2007-06-13 2016-03-23 Incyte Holdings Corporation Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
EA020777B1 (ru) * 2007-11-16 2015-01-30 Инсайт Корпорейшн 4-пиразолил-n-арилпиримидин-2-амины, 4-пиразолил-n-пиразолилпиримидин-2-амины и 4-пиразолил-n-пиридилпиримидин-2-амины в качестве ингибиторов киназ janus
SI2288610T1 (sl) * 2008-03-11 2016-11-30 Incyte Holdings Corporation Derivati azetidina in ciklobutana kot inhibitorji jak
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.
JOP20190231A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
HUE046493T2 (hu) 2009-05-22 2020-03-30 Incyte Holdings Corp 3-[4-(7H-Pirrolo[2,3-d]pirimidin-4-il)-lH-pirazol-l-il]oktán- vagy heptán-nitril JAK inhibitorokként
US8716303B2 (en) 2009-05-22 2014-05-06 Incyte Corporation 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
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
PL2486041T3 (pl) 2009-10-09 2014-01-31 Incyte Holdings Corp Pochodne hydroksylowe, keto i glukuronidowe 3-(4-(7H-pirolo[2,3-d]pirymidyn-4-ylo)-1H-pirazol-1-ilo)-3-cyklopentylopropanonitrylu
EA023444B1 (ru) 2010-02-18 2016-06-30 Инсайт Холдингс Корпорейшн Циклобутановые и метилциклобутановые производные, композиции на их основе и способы их применения
MY175156A (en) 2010-03-10 2020-06-11 Incyte Corp Piperidin-4-yl azetidine derivatives as jak1 inhibitors
NZ603446A (en) 2010-04-14 2014-05-30 Array Biopharma Inc 5, 7-substituted-imidazo [1, 2-c] pyrimidines as inhibitors of jak kinases
TWI499421B (zh) 2010-05-21 2015-09-11 Incyte Corp Jak抑制劑的局部製劑
JP5917544B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Jak阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン
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
US8828987B2 (en) 2010-12-10 2014-09-09 Rottapharm Biotech S.R.L. Pyridine amide derivatives as EP4 receptor antagonists
US9926601B2 (en) 2011-02-24 2018-03-27 Massachusetts Institute Of Technology Alternatively spliced mRNA isoforms as prognostic indicators for metastatic cancer
AU2012273164B2 (en) 2011-06-20 2015-05-28 Incyte Holdings Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
JP6110859B2 (ja) 2011-09-22 2017-04-05 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. ヤヌスキナーゼ阻害剤としてのピラゾールカルボキサミド
US9193733B2 (en) * 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
UA117572C2 (uk) 2012-11-01 2018-08-27 Інсайт Холдинґс Корпорейшн Трициклічні конденсовані похідні тіофену як інгібітори jak
WO2014078486A1 (en) 2012-11-15 2014-05-22 Incyte Corporation Sustained-release dosage forms of ruxolitinib
ES2707355T3 (es) 2013-03-06 2019-04-03 Incyte Holdings Corp Procesos y productos intermedios para elaborar un inhibidor de JAK
EP2803668A1 (en) 2013-05-17 2014-11-19 Boehringer Ingelheim International Gmbh Novel (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles
US9371282B2 (en) 2013-05-17 2016-06-21 Centrexion Therapeutics Corporation Somatostatin receptor subtype 4 (SSTR4) agonists
JP6533217B2 (ja) 2013-05-17 2019-06-19 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft B型肝炎ウイルス感染症の治療および予防のための6−架橋ヘテロアリールジヒドロピリミジン類
JO3603B1 (ar) 2013-05-17 2020-07-05 Janssen Sciences Ireland Uc مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي
ME02763B (me) 2013-05-17 2018-01-20 Incyte Corp Derivati bipirazola kao inhibitori jak
CA3155500A1 (en) 2013-08-07 2015-02-12 Incyte Corporation Sustained release dosage forms for a jak1 inhibitor
PE20161388A1 (es) 2014-02-28 2016-12-28 Incyte Corp Inhibidores de la jak1 para el tratamiento de sindromes mielodisplasicos
CA2947418A1 (en) 2014-04-30 2015-11-05 Incyte Corporation Processes of preparing a jak1 inhibitor and new forms thereto
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
RS59507B1 (sr) 2014-12-16 2019-12-31 Novartis Ag Jedinjenja izoksazol hidroksamske kiseline kao inhibitori lpxc
AR122505A1 (es) 2020-06-02 2022-09-14 Incyte Corp Procesos para preparar un inhibidor de jak1
US20220202834A1 (en) 2020-12-04 2022-06-30 Incyte Corporation Jak inhibitor with a vitamin d analog for treatment of skin diseases

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