BR112015028501B8 - Compostos derivados de bipirazol, seus sais, composição compreendendo o composto ou o sal, método de inibição in vitro de uma atividade de jak1, e processo de preparação de sal de ácido fosfórico - Google Patents

Compostos derivados de bipirazol, seus sais, composição compreendendo o composto ou o sal, método de inibição in vitro de uma atividade de jak1, e processo de preparação de sal de ácido fosfórico

Info

Publication number
BR112015028501B8
BR112015028501B8 BR112015028501A BR112015028501A BR112015028501B8 BR 112015028501 B8 BR112015028501 B8 BR 112015028501B8 BR 112015028501 A BR112015028501 A BR 112015028501A BR 112015028501 A BR112015028501 A BR 112015028501A BR 112015028501 B8 BR112015028501 B8 BR 112015028501B8
Authority
BR
Brazil
Prior art keywords
salt
activity
salts
compound
composition
Prior art date
Application number
BR112015028501A
Other languages
English (en)
Other versions
BR112015028501B1 (pt
BR112015028501A2 (pt
Inventor
Li Yun-Long
Mei Song
Zhuo Jincong
Qian Ding-Quan
Cao Ganfeng
Pan Yongchun
Li Qun
Jia Zhongjiang
Original Assignee
Incyte Corp
Incyte Holdings Corp
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 Incyte Corp, Incyte Holdings Corp filed Critical Incyte Corp
Publication of BR112015028501A2 publication Critical patent/BR112015028501A2/pt
Publication of BR112015028501B1 publication Critical patent/BR112015028501B1/pt
Publication of BR112015028501B8 publication Critical patent/BR112015028501B8/pt

Links

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

ABSTRACT The present invention provides compounds of Formula I: I or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that inhibit the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases. TRADUÇÃO DO RESUMO RESUMO "DERIVADOS DE BIPIRAZOL COMO INIBIDORES DE JAK" A presente invenção fornece Compostos de Fórmula I: I ou os seus sais aceitáveis, bem como as suas composições e métodos de utilização, que inibem a atividade da Quinase Janus (JAK) e são úteis no tratamento de doenças relacionadas com a atividade de JAK, incluindo, por exemplo, distúrbios inflamatórios, distúrbios farmaceuticamente autoimunes, câncer, e outras doenças.
BR112015028501A 2013-05-17 2014-05-16 Compostos derivados de bipirazol, seus sais, composição compreendendo o composto ou o sal, método de inibição in vitro de uma atividade de jak1, e processo de preparação de sal de ácido fosfórico BR112015028501B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361824683P 2013-05-17 2013-05-17
US61/824,683 2013-05-17
PCT/US2014/038388 WO2014186706A1 (en) 2013-05-17 2014-05-16 Bipyrazole derivatives as jak inhibitors

Publications (3)

Publication Number Publication Date
BR112015028501A2 BR112015028501A2 (pt) 2017-07-25
BR112015028501B1 BR112015028501B1 (pt) 2022-11-01
BR112015028501B8 true BR112015028501B8 (pt) 2023-01-24

Family

ID=50983151

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015028501A BR112015028501B8 (pt) 2013-05-17 2014-05-16 Compostos derivados de bipirazol, seus sais, composição compreendendo o composto ou o sal, método de inibição in vitro de uma atividade de jak1, e processo de preparação de sal de ácido fosfórico

Country Status (35)

Country Link
US (6) US9382231B2 (pt)
EP (5) EP3527263B1 (pt)
JP (4) JP6415543B2 (pt)
KR (3) KR102442747B1 (pt)
CN (2) CN105452239B (pt)
AR (2) AR096330A1 (pt)
AU (5) AU2014265279B2 (pt)
BR (1) BR112015028501B8 (pt)
CA (1) CA2911536C (pt)
CL (1) CL2015003355A1 (pt)
CR (2) CR20190156A (pt)
CY (3) CY1119105T1 (pt)
DK (3) DK3527263T3 (pt)
EA (2) EA039660B1 (pt)
ES (4) ES2626793T3 (pt)
FI (1) FI3786162T3 (pt)
HK (2) HK1221466A1 (pt)
HR (4) HRP20231048T1 (pt)
HU (4) HUE063817T2 (pt)
IL (4) IL242453B (pt)
LT (4) LT3786162T (pt)
ME (2) ME02763B (pt)
MX (2) MX2020004506A (pt)
MY (1) MY174788A (pt)
PE (2) PE20160126A1 (pt)
PH (2) PH12015502563B1 (pt)
PL (4) PL3786162T3 (pt)
PT (4) PT3231801T (pt)
RS (4) RS58743B1 (pt)
SG (2) SG10201709469SA (pt)
SI (4) SI3231801T1 (pt)
TR (1) TR201905814T4 (pt)
TW (2) TWI719401B (pt)
UA (1) UA117830C2 (pt)
WO (1) WO2014186706A1 (pt)

Families Citing this family (70)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2348023B9 (en) 2005-12-13 2017-03-08 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
CN101932582B (zh) 2007-06-13 2013-09-25 因塞特公司 詹纳斯激酶抑制剂(R)-3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的盐
SG176111A1 (en) 2009-05-22 2011-12-29 Incyte Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
CN102458581B (zh) 2009-05-22 2016-03-30 因塞特控股公司 作为JANUS激酶抑制剂的吡唑-4-基-吡咯并[2,3-d]嘧啶和吡咯-3-基-吡咯并[2,3-d]嘧啶的N-(杂)芳基-吡咯烷衍生物
ME01838B (me) 2009-06-29 2014-12-20 Lncyte Holdings Corp Pirimidinoni kao inhibitori pi3k
US9249145B2 (en) 2009-09-01 2016-02-02 Incyte Holdings Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
ME02386B (me) 2010-03-10 2016-09-20 Incyte Holdings Corp Derivati piperidin-4-il azetidina kao inhibitori jak1
KR102303885B1 (ko) 2010-05-21 2021-09-24 인사이트 홀딩스 코포레이션 Jak 저해제에 대한 국소 제형
EP2640723A1 (en) 2010-11-19 2013-09-25 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
EP2655374B1 (en) 2010-12-20 2019-10-23 Incyte Holdings Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte 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
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
PE20151141A1 (es) 2012-11-01 2015-08-06 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de jak
EA201590930A1 (ru) 2012-11-15 2015-08-31 Инсайт Корпорейшн Лекарственные формы руксолитиниба с замедленным высвобождением
JP6397831B2 (ja) 2013-03-06 2018-09-26 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阻害剤の製造方法及びその中間体
ME02763B (me) 2013-05-17 2018-01-20 Incyte Corp Derivati bipirazola kao inhibitori jak
MY195091A (en) 2013-08-07 2023-01-10 Incyte Corp Sustained Release Dosage Forms for a JAK1 Inhibitor
SI3110409T1 (sl) * 2014-02-28 2018-11-30 Incyte Corporation Inhibitorji JAK1 za zdravljenje mielodisplastičnih sindromov
KR20230044320A (ko) 2014-04-08 2023-04-03 인사이트 코포레이션 Jak 및 pi3k 억제제 조합에 의한 b-세포 악성종양의 치료
SG10201809518QA (en) 2014-04-30 2018-11-29 Incyte Corp 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
CR20170389A (es) 2015-02-27 2018-01-26 Incyte Corp Sales de inhibidor de p13k y procesos de preparación
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
JP2018521000A (ja) * 2015-05-29 2018-08-02 シドネキシス,インク. D2oで安定化された医薬製剤
MD3371190T2 (ro) 2015-11-06 2022-09-30 Incyte Corp Compuși heterociclici ca inhibitori PI3K-gamma
EP3400221B1 (en) 2016-01-05 2020-08-26 Incyte Corporation Pyrazol / imidazol substituted pyridines as pi3k-gamma inhibitors
AR108875A1 (es) 2016-06-24 2018-10-03 Incyte Corp COMPUESTOS HETEROCÍCLICOS COMO INHIBIDORES DE PI3K-g
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
AU2017324281A1 (en) * 2016-09-06 2019-03-21 F. Hoffmann-La Roche Ag 8-(azetidin-1-yl)-[1,2,4]triazolo[1,5-A]pyridinyl compounds, compositions and methods of use thereof
PE20210169A1 (es) 2017-10-18 2021-01-29 Incyte Corp Derivados de imidazol condensados sustituidos por grupos de hidroxia terciaria como inhibidores de pi3k-y gamma
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
CR20200379A (es) 2018-01-30 2021-03-05 Incyte Corp Procesos e intermedio para elaborar un inhibidor de jak campo técnico
KR20200128043A (ko) 2018-02-16 2020-11-11 인사이트 코포레이션 사이토카인-관련 장애의 치료를 위한 jak1 경로 억제제
MA52655A (fr) 2018-03-30 2021-02-17 Incyte Corp Biomarqueurs pour maladie cutanée inflammatoire
CA3095487A1 (en) * 2018-03-30 2019-10-03 Incyte Corporation Treatment of hidradenitis suppurativa using jak inhibitors
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
MX2021004946A (es) 2018-10-31 2021-07-15 Incyte Corp Terapia combinada para tratamiento de enfermedades hematológicas.
CN113692278A (zh) 2018-12-19 2021-11-23 因赛特公司 用于治疗胃肠道疾病的jak1途径抑制剂
SG11202109563WA (en) 2019-03-05 2021-09-29 Incyte Corp Jak1 pathway inhibitors for the treatment of chronic lung allograft dysfunction
US11624751B2 (en) 2019-03-19 2023-04-11 Incyte Corporation Biomarkers for vitiligo
CA3129665A1 (en) 2019-03-21 2020-09-24 Onxeo A dbait molecule in combination with kinase inhibitor for the treatment of cancer
US20210123931A1 (en) 2019-10-10 2021-04-29 Incyte Corporation Biomarkers for graft-versus-host disease
CA3157499A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
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
EP4157831A1 (en) 2020-06-02 2023-04-05 Incyte Corporation Processes of preparing a jak1 inhibitor
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
KR20230096973A (ko) 2020-08-18 2023-06-30 인사이트 코포레이션 Jak 저해제를 제조하기 위한 방법 및 중간체
PE20231308A1 (es) 2020-08-18 2023-08-24 Incyte Corp Proceso e intermedios para preparar un inhibidor de jak1
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
TW202237125A (zh) 2020-12-04 2022-10-01 美商英塞特公司 用於治療皮膚疾病之jak抑制劑與維生素d類似物
CA3204374A1 (en) 2020-12-08 2022-06-16 Incyte Corporation Jak1 pathway inhibitors for the treatment of vitiligo
CN112933095A (zh) * 2020-12-29 2021-06-11 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
KR20230157307A (ko) 2021-01-11 2023-11-16 인사이트 코포레이션 Jak 경로 억제제 및 rock 억제제를 포함하는 병용 요법
JP2024516302A (ja) 2021-05-03 2024-04-12 インサイト・コーポレイション 結節性痒疹を治療するためのjak1経路阻害薬
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
CN1152031C (zh) 1998-08-11 2004-06-02 诺瓦提斯公司 具有血管生成抑制活性的异喹啉衍生物
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
CA2413330A1 (en) 2000-06-28 2002-01-03 Smithkline Beecham P.L.C. Wet milling process
AU2002337142B2 (en) 2001-09-19 2007-10-11 Aventis Pharma S.A. Indolizines as kinase protein inhibitors
CA2462657C (en) 2001-10-30 2011-04-26 Novartis Ag Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity
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
TWI335913B (en) 2002-11-15 2011-01-11 Vertex Pharma Diaminotriazoles useful as inhibitors of protein kinases
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
PE20050952A1 (es) 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
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
EP2348023B9 (en) 2005-12-13 2017-03-08 Incyte Holdings Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as Janus kinase inhibitors
CN101932582B (zh) 2007-06-13 2013-09-25 因塞特公司 詹纳斯激酶抑制剂(R)-3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的盐
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.
EP2220068B1 (en) * 2007-11-16 2016-01-27 Incyte Holdings Corporation 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors
UA101493C2 (ru) * 2008-03-11 2013-04-10 Инсайт Корпорейшн Производные азетидина и циклобутана как ингибиторы 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
CN102458581B (zh) * 2009-05-22 2016-03-30 因塞特控股公司 作为JANUS激酶抑制剂的吡唑-4-基-吡咯并[2,3-d]嘧啶和吡咯-3-基-吡咯并[2,3-d]嘧啶的N-(杂)芳基-吡咯烷衍生物
SG176111A1 (en) 2009-05-22 2011-12-29 Incyte Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
US9249145B2 (en) 2009-09-01 2016-02-02 Incyte Holdings Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
KR20180126619A (ko) 2009-10-09 2018-11-27 인사이트 홀딩스 코포레이션 3-(4-(7H-피롤로〔2,3-d〕피리미딘-4-일)-1H-피라졸-1-일)-3-사이클로펜틸프로판니트릴의 하이드록실, 케토 및 글루쿠로나이드 유도체
BR112012020693B1 (pt) 2010-02-18 2020-05-12 Incyte Holdings Corporation Derivados de ciclobutano e metilciclobutano como inibidores de janus quinase e composição que os compreende
ME02386B (me) 2010-03-10 2016-09-20 Incyte Holdings Corp Derivati piperidin-4-il azetidina kao inhibitori jak1
JP2013523884A (ja) * 2010-04-14 2013-06-17 アレイ バイオファーマ、インコーポレイテッド JAKキナーゼの阻害剤としての5,7置換イミダゾ[1,2−c]ピリミジン
KR102303885B1 (ko) 2010-05-21 2021-09-24 인사이트 홀딩스 코포레이션 Jak 저해제에 대한 국소 제형
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
EP2640723A1 (en) * 2010-11-19 2013-09-25 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
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
US8691807B2 (en) * 2011-06-20 2014-04-08 Incyte 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
AU2012312305B2 (en) 2011-09-22 2016-11-17 Merck Sharp & Dohme Corp. Acyclic cyanoethylpyrazoles as janus kinase inhibitors
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
PE20151141A1 (es) 2012-11-01 2015-08-06 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de jak
EA201590930A1 (ru) 2012-11-15 2015-08-31 Инсайт Корпорейшн Лекарственные формы руксолитиниба с замедленным высвобождением
JP6397831B2 (ja) 2013-03-06 2018-09-26 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阻害剤の製造方法及びその中間体
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
AU2014267198A1 (en) 2013-05-17 2015-11-05 F. Hoffmann-La Roche Ag 6-bridged heteroaryldihydropyrimidines for the treatment and prophylaxis of Hepatitis B virus infection
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
MY195091A (en) 2013-08-07 2023-01-10 Incyte Corp Sustained Release Dosage Forms for a JAK1 Inhibitor
SI3110409T1 (sl) 2014-02-28 2018-11-30 Incyte Corporation Inhibitorji JAK1 za zdravljenje mielodisplastičnih sindromov
SG10201809518QA (en) 2014-04-30 2018-11-29 Incyte Corp 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
AU2015365455B2 (en) 2014-12-16 2019-01-17 Novartis Ag Isoxazole hydroxamic acid compounds as LpxC inhibitors
EP4157831A1 (en) 2020-06-02 2023-04-05 Incyte Corporation Processes of preparing a jak1 inhibitor
TW202237125A (zh) 2020-12-04 2022-10-01 美商英塞特公司 用於治療皮膚疾病之jak抑制劑與維生素d類似物

Also Published As

Publication number Publication date
CY1123756T1 (el) 2022-05-27
EP4275756A2 (en) 2023-11-15
IL282644B (en) 2021-10-31
JP7126741B2 (ja) 2022-08-29
CN107698569A (zh) 2018-02-16
DK3231801T3 (en) 2019-04-15
EP3786162A1 (en) 2021-03-03
WO2014186706A1 (en) 2014-11-20
EP4275756A3 (en) 2024-02-07
IL242453B (en) 2019-11-28
EP2997023B9 (en) 2018-06-13
SG10201709469SA (en) 2017-12-28
PL3786162T3 (pl) 2024-04-08
AU2018223058B2 (en) 2020-01-02
NZ753637A (en) 2020-11-27
CA2911536A1 (en) 2014-11-20
US20200010456A1 (en) 2020-01-09
CN105452239B (zh) 2017-11-21
AU2021202685A1 (en) 2021-05-27
IL287313A (en) 2021-12-01
TW201512191A (zh) 2015-04-01
RS58743B1 (sr) 2019-06-28
AR096330A1 (es) 2015-12-23
US9382231B2 (en) 2016-07-05
CY1119105T1 (el) 2018-02-14
BR112015028501B1 (pt) 2022-11-01
US11905275B2 (en) 2024-02-20
PE20200527A1 (es) 2020-03-09
CR20150633A (es) 2016-04-05
EA202090291A2 (ru) 2020-05-31
US20210238168A1 (en) 2021-08-05
EP3786162B1 (en) 2023-08-09
LT3231801T (lt) 2019-08-12
PH12015502563A1 (en) 2016-02-22
US20180312492A1 (en) 2018-11-01
AU2021202685B2 (en) 2022-11-17
TWI719401B (zh) 2021-02-21
AU2014265279B2 (en) 2018-09-27
MX2020004506A (es) 2021-08-09
ES2720073T3 (es) 2019-07-17
CN107698569B (zh) 2020-11-27
SI3231801T1 (sl) 2019-05-31
NZ753639A (en) 2020-11-27
RS64591B1 (sr) 2023-10-31
CL2015003355A1 (es) 2016-05-27
IL264409B (en) 2021-05-31
NZ713999A (en) 2020-11-27
EA036448B1 (ru) 2020-11-11
PT3527263T (pt) 2021-02-01
TW201940479A (zh) 2019-10-16
FI3786162T3 (fi) 2023-10-02
AU2018223058A1 (en) 2018-09-20
LT3786162T (lt) 2023-11-27
PL3231801T3 (pl) 2019-07-31
EP2997023B1 (en) 2017-03-22
HUE043573T2 (hu) 2019-08-28
JP6415543B2 (ja) 2018-10-31
MY174788A (en) 2020-05-14
AU2014265279A1 (en) 2015-11-26
EP3231801B1 (en) 2019-02-13
PT2997023T (pt) 2017-05-31
UA117830C2 (uk) 2018-10-10
HUE033587T2 (hu) 2017-12-28
SI3786162T1 (sl) 2024-02-29
JP2022163162A (ja) 2022-10-25
TR201905814T4 (tr) 2019-05-21
DK3527263T3 (da) 2021-01-25
NZ753636A (en) 2020-11-27
ES2626793T3 (es) 2017-07-26
PH12018502125A1 (en) 2019-03-25
PT3786162T (pt) 2023-10-20
EA039660B1 (ru) 2022-02-24
SG11201509180WA (en) 2015-12-30
HK1221466A1 (zh) 2017-06-02
CN105452239A (zh) 2016-03-30
US20140343030A1 (en) 2014-11-20
KR20220127371A (ko) 2022-09-19
EP2997023A1 (en) 2016-03-23
KR102442747B1 (ko) 2022-09-14
SI2997023T1 (sl) 2017-07-31
AR118120A2 (es) 2021-09-22
US11001571B2 (en) 2021-05-11
ME02763B (me) 2018-01-20
HRP20190713T1 (hr) 2019-06-14
JP6775560B2 (ja) 2020-10-28
TW202116320A (zh) 2021-05-01
EA202090291A3 (ru) 2020-06-30
LT2997023T (lt) 2017-06-26
RS61482B1 (sr) 2021-03-31
US11591318B2 (en) 2023-02-28
EP3231801A1 (en) 2017-10-18
JP2016519147A (ja) 2016-06-30
EP3527263A1 (en) 2019-08-21
IL282644A (en) 2021-06-30
PH12015502563B1 (en) 2016-02-22
JP2019011364A (ja) 2019-01-24
PL2997023T3 (pl) 2017-08-31
CR20190156A (es) 2019-05-16
EA201592199A1 (ru) 2016-05-31
HK1245769B (zh) 2020-02-07
KR102341908B1 (ko) 2021-12-23
MX2015015738A (es) 2016-03-16
ME03355B (me) 2019-10-20
LT3527263T (lt) 2021-05-10
HUE053122T2 (hu) 2021-06-28
HRP20231048T1 (hr) 2023-12-22
RS56012B1 (sr) 2017-09-29
CY1121763T1 (el) 2020-07-31
AU2022263454B2 (en) 2024-01-18
PL3527263T3 (pl) 2021-05-17
SI3527263T1 (sl) 2021-05-31
CA2911536C (en) 2021-07-20
PE20160126A1 (es) 2016-02-24
TWI664176B (zh) 2019-07-01
EP3527263B1 (en) 2020-10-28
ES2845210T3 (es) 2021-07-26
IL264409A (en) 2019-02-28
ES2960731T3 (es) 2024-03-06
HUE063817T2 (hu) 2024-01-28
AU2020202000B2 (en) 2021-03-11
HRP20210119T1 (hr) 2021-03-05
AU2020202000A1 (en) 2020-04-09
US20160289215A1 (en) 2016-10-06
HRP20170795T1 (hr) 2017-08-25
US20230159501A1 (en) 2023-05-25
US10435392B2 (en) 2019-10-08
KR20160019905A (ko) 2016-02-22
IL287313B (en) 2022-03-01
AU2022263454A1 (en) 2022-12-08
JP2021008493A (ja) 2021-01-28
BR112015028501A2 (pt) 2017-07-25
DK3786162T3 (da) 2023-10-09
PT3231801T (pt) 2019-05-24
KR20210120120A (ko) 2021-10-06
NZ753638A (en) 2020-11-27
US9926301B2 (en) 2018-03-27

Similar Documents

Publication Publication Date Title
BR112015028501B8 (pt) Compostos derivados de bipirazol, seus sais, composição compreendendo o composto ou o sal, método de inibição in vitro de uma atividade de jak1, e processo de preparação de sal de ácido fosfórico
BR112015015635A8 (pt) composto, método de preparação dos compostos, composição farmacêutica e método in vitro de previsão
GEP20207105B (en) 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2yl carbamate derivatives as magl inhibitors
BR112015022643A2 (pt) inibidores diidro-pirrolpiridinona
BR112013032720A2 (pt) "derivados de azetidinil fenil, piridil ou pirazinil carboxamida como inibidores de jak, composição e uso dos referidos derivados"
BR112015002118A2 (pt) 4-metil-2,3,5,9,9b-pentaaza-ciclopenta[a]naftalenos
PL415078A1 (pl) Podstawione aminotriazole przydatne jako inhibitory kwaśnej chitynazy ssaków
BR112012020693A2 (pt) derivados de ciclobutano e metilciclobutano como inibidores de janus quinase
BR112013025387A2 (pt) análogos substituídos da n-fenilpirimidin-2-amina como inibidores da quinase axl
BR112014008045A2 (pt) benzilindazóis substituídos para uso como inibidores de bub1 cinase no tratamento de doenças hiperproliferativas
BR112013012502A2 (pt) pirrolopiridina ciclobutil substituída e derivados de pirrolopirimidina derivativos como inibidores de jak
BR112013001088A2 (pt) "derivados substituídos como inibidores a quinase de imidazoquinolina"
BR112015020350A2 (pt) derivados de 6-(5-hidroxi-1h-pirazol-1-il)nicotinamida e seu uso como inibidores de phd
BR112014005226A2 (pt) derivados de benzonitrila como inibidores de cinase
BR112015015653A8 (pt) composto, método de preparação dos compostos, composto para uso, composição farmacêutica e métodos in vitro
BR112014004504A2 (pt) "composto como inibidor de c-kit cinase, seu uso, composição farmacêutica, e medicamento para o tratamento de uma doença mediada por uma cinase"
BR112017011798A2 (pt) 4,6-substituído-pirazolo[1,5-a] pirazinas como inibidores janus cinase
AU2012258977A8 (en) Inhibitors of LRRK2 kinase activity
BR112015021701A2 (pt) novos compostos inibidores da fosfoestearase tipo 10a
BR112015001502A2 (pt) derivados de tipo azaindazol ou diazaindazol para tratamento de dor
EA201590183A1 (ru) Производные азаиндола, выступающие в качестве ингибиторов pi3k
BR112014029708A2 (pt) composto de pirrolo[2,1-f][1,2,4]triazina, método de preparação de compostos de pirrolo[2,1-f][1,2,4]triazina e uso do composto de pirrolo[2,1-f][1,2,4]triazina
BR112013030264A2 (pt) ácidos acéticos de benzociclohepteno
NZ706591A (en) Oxazolidin-2-one-pyrimidine derivatives
CO6331433A2 (es) 2,6-diamino-pirimidin-5-ilcarboxamidas como inhibidores de syk p jak quinasas

Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 16/05/2014, OBSERVADAS AS CONDICOES LEGAIS

B25A Requested transfer of rights approved

Owner name: INCYTE HOLDINGS CORPORATION (US)