EA036448B1 - Производные бипиразола в качестве ингибиторов jak - Google Patents

Производные бипиразола в качестве ингибиторов jak Download PDF

Info

Publication number
EA036448B1
EA036448B1 EA201592199A EA201592199A EA036448B1 EA 036448 B1 EA036448 B1 EA 036448B1 EA 201592199 A EA201592199 A EA 201592199A EA 201592199 A EA201592199 A EA 201592199A EA 036448 B1 EA036448 B1 EA 036448B1
Authority
EA
Eurasian Patent Office
Prior art keywords
compound
cyanomethyl
azetidin
bipyrazol
trifluoro
Prior art date
Application number
EA201592199A
Other languages
English (en)
Russian (ru)
Other versions
EA201592199A1 (ru
Inventor
Юнь-Лун Ли
Цзиньцун Чжо
Дин-Цюань Цянь
Сун Мей
Ганьфэн Цао
Юнчунь Пань
Цюнь Ли
Чжунцзян Цзя
Original Assignee
Инсайт 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 Инсайт Корпорейшн filed Critical Инсайт Корпорейшн
Publication of EA201592199A1 publication Critical patent/EA201592199A1/ru
Publication of EA036448B1 publication Critical patent/EA036448B1/ru

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
    • A61K31/495Heterocyclic 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/20Antivirals for DNA viruses
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Transplantation (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Biotechnology (AREA)
  • Dermatology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
EA201592199A 2013-05-17 2014-05-16 Производные бипиразола в качестве ингибиторов jak EA036448B1 (ru)

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 (2)

Publication Number Publication Date
EA201592199A1 EA201592199A1 (ru) 2016-05-31
EA036448B1 true EA036448B1 (ru) 2020-11-11

Family

ID=50983151

Family Applications (2)

Application Number Title Priority Date Filing Date
EA202090291A EA039660B1 (ru) 2013-05-17 2014-05-16 Твердая форма производного бипиразола
EA201592199A EA036448B1 (ru) 2013-05-17 2014-05-16 Производные бипиразола в качестве ингибиторов jak

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EA202090291A EA039660B1 (ru) 2013-05-17 2014-05-16 Твердая форма производного бипиразола

Country Status (36)

Country Link
US (8) US9382231B2 (enExample)
EP (6) EP2997023B9 (enExample)
JP (5) JP6415543B2 (enExample)
KR (4) KR102442747B1 (enExample)
CN (2) CN107698569B (enExample)
AR (2) AR096330A1 (enExample)
AU (5) AU2014265279B2 (enExample)
BR (1) BR112015028501B8 (enExample)
CA (1) CA2911536C (enExample)
CL (1) CL2015003355A1 (enExample)
CR (2) CR20190156A (enExample)
CY (3) CY1119105T1 (enExample)
DK (4) DK4275756T3 (enExample)
EA (2) EA039660B1 (enExample)
ES (5) ES2960731T3 (enExample)
FI (2) FI4275756T3 (enExample)
HK (1) HK1245769B (enExample)
HR (5) HRP20170795T1 (enExample)
HU (4) HUE053122T2 (enExample)
IL (4) IL242453B (enExample)
LT (5) LT4275756T (enExample)
ME (2) ME03355B (enExample)
MX (2) MX373238B (enExample)
MY (1) MY174788A (enExample)
PE (2) PE20200527A1 (enExample)
PH (2) PH12015502563B1 (enExample)
PL (4) PL3527263T3 (enExample)
PT (5) PT2997023T (enExample)
RS (5) RS61482B1 (enExample)
SG (2) SG11201509180WA (enExample)
SI (4) SI3231801T1 (enExample)
SM (5) SMT202300352T1 (enExample)
TR (1) TR201905814T4 (enExample)
TW (4) TWI840646B (enExample)
UA (1) UA117830C2 (enExample)
WO (1) WO2014186706A1 (enExample)

Families Citing this family (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2455382T1 (sl) 2005-12-13 2017-03-31 Incyte Holdings Corporation S heteroarilom substituirani pirolo(2,3b)piridini in pirolo(2,3-b)pirimidini kot zaviralci janus kinaze
ES2467665T5 (es) 2007-06-13 2022-11-03 Incyte Holdings Corp Sales del inhibidor de cinasas Janus (R)-3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo
MY156727A (en) 2009-05-22 2016-03-15 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
PT2432472T (pt) 2009-05-22 2019-12-09 Incyte Holdings Corp 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]octano- ou heptano-nitrilo como inibidores de jak
TW201602113A (zh) 2009-06-29 2016-01-16 英塞特公司 作為pi3k抑制劑之嘧啶酮
WO2011028685A1 (en) 2009-09-01 2011-03-10 Incyte Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
MX354212B (es) 2010-03-10 2018-02-19 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
US20110288107A1 (en) 2010-05-21 2011-11-24 Bhavnish Parikh Topical formulation for a jak inhibitor
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
CA2822070C (en) 2010-12-20 2019-09-17 Incyte Corporation N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors
WO2012177606A1 (en) 2011-06-20 2012-12-27 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
SG10201912484RA (en) 2011-09-02 2020-02-27 Incyte Corp Heterocyclylamines as pi3k inhibitors
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
WO2013173720A1 (en) 2012-05-18 2013-11-21 Incyte 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
ES2880814T3 (es) 2012-11-15 2021-11-25 Incyte Holdings Corp Formas de dosificación de liberación sostenida de ruxolitinib
EP3489239B1 (en) 2013-03-06 2021-09-15 Incyte Holdings Corporation Processes and intermediates for making a jak inhibitor
PT2997023T (pt) * 2013-05-17 2017-05-31 Incyte Corp Derivados de bipirazole como inibidores da jak
TWI789516B (zh) 2013-08-07 2023-01-11 美商英塞特公司 Jak1抑制劑之持續釋放劑型
RS57723B1 (sr) * 2014-02-28 2018-12-31 Incyte Corp Jak1 inhibitori za lečenje mijelodisplastičnog sindroma
JP6537527B2 (ja) 2014-04-08 2019-07-03 インサイト・コーポレイションIncyte Corporation Jak及びpi3k阻害剤併用によるb細胞悪性腫瘍の処置
TW201625643A (zh) 2014-04-30 2016-07-16 英塞特公司 製備jak1抑制劑之方法及其新形式
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
US10077277B2 (en) 2014-06-11 2018-09-18 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
US9586949B2 (en) 2015-02-09 2017-03-07 Incyte Corporation Aza-heteroaryl compounds as PI3K-gamma inhibitors
EP4183789A1 (en) 2015-02-27 2023-05-24 Incyte Holdings Corporation 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
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
US11052094B2 (en) * 2015-05-29 2021-07-06 Sydnexis, Inc. D2O stabilized pharmaceutical formulations
PT3371190T (pt) 2015-11-06 2022-07-08 Incyte Corp Compostos heterocíclicos como inibidores de pi3k-gamma
ES2833955T3 (es) 2016-01-05 2021-06-16 Incyte Corp Piridinas sustituidas con pirazol/imidazol como inhibidores de PI3K-Gamma
WO2017223414A1 (en) 2016-06-24 2017-12-28 Incyte Corporation HETEROCYCLIC COMPOUNDS 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
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
MD3697789T2 (ro) 2017-10-18 2022-02-28 Incyte Corp Derivați imidazol condensați substituiți cu grupări hidroxi terțiare ca inhibitori PI3K-GAMA
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
HRP20220510T1 (hr) 2018-01-30 2022-05-27 Incyte Corporation Postupci za pripravu (1-(3-fluoro-2-(trifluorometil)izonikotinil) piperidin-4-ona)
IL276725B2 (en) 2018-02-16 2024-09-01 Incyte Corp Jak1 pathway inhibitors for the treatment of cytokine-related disorders
WO2019191679A1 (en) 2018-03-30 2019-10-03 Incyte Corporation Biomarkers for inflammatory skin disease
HUE067471T2 (hu) * 2018-03-30 2024-10-28 Incyte Corp Gennyes verejtékmirigy-gyulladás kezelése jak inhibitorok alkalmazásával
AU2019252259A1 (en) 2018-04-13 2020-12-03 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
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
CR20250050A (es) 2018-09-05 2025-03-19 Incyte Corp Formas cristalinas de un inhibidor de fosfoinositida 3–quinasa (pi3k) (divisional 2021-0165)
SG11202104321PA (en) 2018-10-31 2021-05-28 Incyte Corp Combination therapy for treatment of hematological diseases
KR20210116487A (ko) 2018-12-19 2021-09-27 인사이트 코포레이션 위장 질환의 치료를 위한 jak1 경로 억제제
KR20210137087A (ko) 2019-03-05 2021-11-17 인사이트 코포레이션 만성 폐 동종이식 기능장애의 치료를 위한 jak1 경로 억제제
WO2020191041A2 (en) 2019-03-19 2020-09-24 Incyte Corporation Biomarkers for vitiligo
BR112021018168B1 (pt) 2019-03-21 2023-11-28 Onxeo Composição farmacêutica, combinação e kit compreendendo uma molécula dbait e um inibidor de quinase para o tratamento de câncer
JP2022549506A (ja) 2019-09-27 2022-11-25 ディスク・メディシン・インコーポレイテッド 骨髄線維症および関連状態を処置するための方法
WO2021072098A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
CA3157499A1 (en) 2019-10-10 2021-04-15 Incyte Corporation Biomarkers for graft-versus-host disease
WO2021076124A1 (en) 2019-10-16 2021-04-22 Incyte Corporation Use of jak1 inhibitors for the treatment of cutaneous lupus erythematosus and lichen planus (lp)
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)
KR20220098759A (ko) 2019-11-08 2022-07-12 인쎄름 (엥스띠뛰 나씨오날 드 라 쌍떼 에 드 라 흐쉐르슈 메디깔) 키나제 억제제에 대해 내성을 획득한 암의 치료 방법
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
EP4149548A4 (en) 2020-05-13 2024-05-08 Disc Medicine, Inc. ANTI-HEMOJUVELIN ANTIBODIES (HJV) FOR THE TREATMENT OF MYELOFIBROSIS
ES2998487T3 (en) * 2020-06-02 2025-02-20 Incyte Corp Processes of preparing a jak1 inhibitor
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
AU2021329301A1 (en) 2020-08-18 2023-04-13 Incyte Corporation Process and intermediates for preparing a JAK1 inhibitor
AU2021329303A1 (en) 2020-08-18 2023-04-06 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
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
MX2023006638A (es) 2020-12-04 2023-08-22 Incyte Corp Inhibidor de la cinasa janus (jak) con un análogo de la vitamina d para el tratamiento de enfermedades de la piel.
US11957661B2 (en) * 2020-12-08 2024-04-16 Incyte Corporation JAK1 pathway inhibitors for the treatment of vitiligo
CN114081889A (zh) * 2020-12-29 2022-02-25 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
AU2022206313A1 (en) 2021-01-11 2023-08-31 Incyte Corporation Combination therapy comprising jak pathway inhibitor and rock inhibitor
IL308216A (en) 2021-05-03 2024-01-01 Incyte Corp Jak1 pathway inhibitors for the treatment of prurigo nodularis
US12071439B2 (en) 2021-07-12 2024-08-27 Incyte Corporation Process and intermediates for preparing a JAK inhibitor
TW202419088A (zh) 2022-08-05 2024-05-16 美商英塞特公司 使用jak抑制劑之蕁麻疹治療
US20240307353A1 (en) 2023-03-16 2024-09-19 Incyte Corporation Jak1 pathway inhibitors for the treatment of asthma
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
US20250325664A1 (en) 2024-04-22 2025-10-23 Incyte Corporation Combination therapy with an anti-colony stimulating factor 1 receptor antibody and a jak inhibitor

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012177606A1 (en) * 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors

Family Cites Families (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
JPH0515775Y2 (enExample) 1987-07-13 1993-04-26
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
ES2342240T3 (es) 1998-08-11 2010-07-02 Novartis Ag Derivados de isoquinolina con actividad que inhibe la angiogenia.
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
DE60230890D1 (de) 2001-09-19 2009-03-05 Aventis Pharma Sa Indolizine als kinaseproteinhemmer
IL161156A0 (en) 2001-10-30 2004-08-31 Novartis Ag Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity
AR037647A1 (es) 2002-05-29 2004-12-01 Novartis Ag Derivados de diarilurea utiles para el tratamiento de enfermedades 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
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
SI2455382T1 (sl) 2005-12-13 2017-03-31 Incyte Holdings Corporation S heteroarilom substituirani pirolo(2,3b)piridini in pirolo(2,3-b)pirimidini kot zaviralci janus kinaze
ES2467665T5 (es) 2007-06-13 2022-11-03 Incyte Holdings Corp Sales del inhibidor de cinasas Janus (R)-3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo
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.
US8309718B2 (en) * 2007-11-16 2012-11-13 Incyte Corporation 4-pyrazolyl-N-arylpyrimidin-2-amines and 4-pyrazolyl-N-heteroarylpyrimidin-2-amines as janus kinase inhibitors
EP2288610B8 (en) * 2008-03-11 2016-10-12 Incyte Holdings Corporation Azetidine and cyclobutane derivatives as jak inhibitors
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.
JOP20190230A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
MY156727A (en) * 2009-05-22 2016-03-15 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
PT2432472T (pt) 2009-05-22 2019-12-09 Incyte Holdings Corp 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]octano- ou heptano-nitrilo como inibidores de jak
WO2011028685A1 (en) * 2009-09-01 2011-03-10 Incyte Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
CA2777114C (en) 2009-10-09 2018-10-23 Incyte Corporation Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
MX2012009541A (es) 2010-02-18 2012-10-01 Incyte Corp Derivados de ciclobutano y metilciclobutano como inhibidores de janus cinasa.
MX354212B (es) 2010-03-10 2018-02-19 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
CN102985424B (zh) * 2010-04-14 2015-03-11 阵列生物制药公司 5,7-取代的-咪唑并[1,2-c]嘧啶
US20110288107A1 (en) 2010-05-21 2011-11-24 Bhavnish Parikh Topical formulation for a jak inhibitor
CA2818542A1 (en) * 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
EP2640725B1 (en) 2010-11-19 2015-01-07 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
EP2649061B1 (en) * 2010-12-10 2015-05-13 Rottapharm Biotech S.r.l. Pyridine amide derivatives as ep4 receptor antagonists
EP2678686B1 (en) 2011-02-24 2017-10-11 Massachusetts Institute of Technology ALTERNATIVELY SPLICED mRNA ISOFORMS AS PROGNOSTIC INDICATORS FOR METASTATIC CANCER
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
WO2013173720A1 (en) * 2012-05-18 2013-11-21 Incyte 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
ES2880814T3 (es) 2012-11-15 2021-11-25 Incyte Holdings Corp Formas de dosificación de liberación sostenida de ruxolitinib
EP3489239B1 (en) 2013-03-06 2021-09-15 Incyte Holdings Corporation Processes and intermediates for making a jak inhibitor
US9371282B2 (en) 2013-05-17 2016-06-21 Centrexion Therapeutics Corporation Somatostatin receptor subtype 4 (SSTR4) agonists
JO3603B1 (ar) 2013-05-17 2020-07-05 Janssen Sciences Ireland Uc مشتقات سلفامويل بيرولاميد واستخدامها كادوية لمعالجة التهاب الكبد نوع بي
PE20151951A1 (es) 2013-05-17 2015-12-26 Hoffmann La Roche Heteroarildihidropirimidinas unidas por puentes en 6 para el tratamiento y la profilaxis de infeccion por el virus de la hepatitis b
PT2997023T (pt) 2013-05-17 2017-05-31 Incyte Corp Derivados de bipirazole como inibidores da jak
EP2803668A1 (en) 2013-05-17 2014-11-19 Boehringer Ingelheim International Gmbh Novel (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles
TWI789516B (zh) 2013-08-07 2023-01-11 美商英塞特公司 Jak1抑制劑之持續釋放劑型
RS57723B1 (sr) 2014-02-28 2018-12-31 Incyte Corp Jak1 inhibitori za lečenje mijelodisplastičnog sindroma
TW201625643A (zh) 2014-04-30 2016-07-16 英塞特公司 製備jak1抑制劑之方法及其新形式
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
TN2017000207A1 (en) 2014-12-16 2018-10-19 Novartis Ag Isoxazole hydroxamic acid compounds as lpxc inhibitors
IL276725B2 (en) 2018-02-16 2024-09-01 Incyte Corp Jak1 pathway inhibitors for the treatment of cytokine-related disorders
ES2998487T3 (en) 2020-06-02 2025-02-20 Incyte Corp Processes of preparing a jak1 inhibitor
MX2023006638A (es) 2020-12-04 2023-08-22 Incyte Corp Inhibidor de la cinasa janus (jak) con un análogo de la vitamina d para el tratamiento de enfermedades de la piel.
US11957661B2 (en) 2020-12-08 2024-04-16 Incyte Corporation JAK1 pathway inhibitors for the treatment of vitiligo

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012177606A1 (en) * 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors

Also Published As

Publication number Publication date
US20250206726A1 (en) 2025-06-26
NZ753636A (en) 2020-11-27
AU2022263454A1 (en) 2022-12-08
SI3527263T1 (sl) 2021-05-31
CL2015003355A1 (es) 2016-05-27
PE20160126A1 (es) 2016-02-24
HUE053122T2 (hu) 2021-06-28
US11905275B2 (en) 2024-02-20
HUE063817T2 (hu) 2024-01-28
JP7126741B2 (ja) 2022-08-29
DK4275756T3 (da) 2025-09-29
RS61482B1 (sr) 2021-03-31
JP2016519147A (ja) 2016-06-30
CN107698569A (zh) 2018-02-16
PL3527263T3 (pl) 2021-05-17
TWI885650B (zh) 2025-06-01
TR201905814T4 (tr) 2019-05-21
AU2018223058A1 (en) 2018-09-20
MY174788A (en) 2020-05-14
RS58743B1 (sr) 2019-06-28
AU2021202685B2 (en) 2022-11-17
CN107698569B (zh) 2020-11-27
ES2845210T3 (es) 2021-07-26
JP2024105557A (ja) 2024-08-06
CN105452239A (zh) 2016-03-30
IL242453B (en) 2019-11-28
JP2022163162A (ja) 2022-10-25
LT3231801T (lt) 2019-08-12
CY1123756T1 (el) 2022-05-27
SMT202100040T1 (it) 2021-03-15
US20160289215A1 (en) 2016-10-06
ME02763B (me) 2018-01-20
NZ713999A (en) 2020-11-27
PT3527263T (pt) 2021-02-01
KR20160019905A (ko) 2016-02-22
HK1245769B (en) 2020-02-07
MX2015015738A (es) 2016-03-16
EP4620528A3 (en) 2025-11-26
JP2021008493A (ja) 2021-01-28
CY1119105T1 (el) 2018-02-14
HRP20231048T1 (hr) 2023-12-22
TWI664176B (zh) 2019-07-01
SI2997023T1 (sl) 2017-07-31
BR112015028501A2 (pt) 2017-07-25
SMT202300352T1 (it) 2024-01-10
LT4275756T (lt) 2025-11-10
JP6775560B2 (ja) 2020-10-28
KR20210120120A (ko) 2021-10-06
TW202116320A (zh) 2021-05-01
CA2911536A1 (en) 2014-11-20
AU2020202000B2 (en) 2021-03-11
LT3527263T (lt) 2021-05-10
ES3047826T3 (en) 2025-12-05
FI4275756T3 (fi) 2025-10-20
HRP20190713T1 (hr) 2019-06-14
US20240150327A1 (en) 2024-05-09
NZ753637A (en) 2020-11-27
US9926301B2 (en) 2018-03-27
DK3527263T3 (da) 2021-01-25
EP2997023A1 (en) 2016-03-23
LT3786162T (lt) 2023-11-27
PL3231801T3 (pl) 2019-07-31
TWI840646B (zh) 2024-05-01
BR112015028501B1 (pt) 2022-11-01
HRP20251220T1 (hr) 2025-12-05
SI3786162T1 (sl) 2024-02-29
EP4275756B1 (en) 2025-09-03
US11001571B2 (en) 2021-05-11
PH12015502563A1 (en) 2016-02-22
DK3231801T3 (en) 2019-04-15
PT3786162T (pt) 2023-10-20
PL2997023T3 (pl) 2017-08-31
TW201512191A (zh) 2015-04-01
EA201592199A1 (ru) 2016-05-31
FI3786162T3 (fi) 2023-10-02
JP6415543B2 (ja) 2018-10-31
AR096330A1 (es) 2015-12-23
KR20220127371A (ko) 2022-09-19
HUE033587T2 (hu) 2017-12-28
PL3786162T3 (pl) 2024-04-08
PT4275756T (pt) 2025-10-31
EP2997023B1 (en) 2017-03-22
HUE043573T2 (hu) 2019-08-28
IL264409B (en) 2021-05-31
DK3786162T3 (da) 2023-10-09
US12247020B2 (en) 2025-03-11
AU2022263454B2 (en) 2024-01-18
LT2997023T (lt) 2017-06-26
US11591318B2 (en) 2023-02-28
PH12018502125A1 (en) 2019-03-25
AU2020202000A1 (en) 2020-04-09
JP2019011364A (ja) 2019-01-24
ES2626793T3 (es) 2017-07-26
EP3527263B1 (en) 2020-10-28
RS56012B1 (sr) 2017-09-29
US10435392B2 (en) 2019-10-08
EA039660B1 (ru) 2022-02-24
UA117830C2 (uk) 2018-10-10
CA2911536C (en) 2021-07-20
AR118120A2 (es) 2021-09-22
EP3231801A1 (en) 2017-10-18
CN105452239B (zh) 2017-11-21
EP4275756A2 (en) 2023-11-15
US20230159501A1 (en) 2023-05-25
NZ753638A (en) 2020-11-27
EP4275756A3 (en) 2024-02-07
RS64591B1 (sr) 2023-10-31
CY1121763T1 (el) 2020-07-31
MX373238B (es) 2020-05-08
US20210238168A1 (en) 2021-08-05
AU2014265279B2 (en) 2018-09-27
US20180312492A1 (en) 2018-11-01
SG10201709469SA (en) 2017-12-28
AU2018223058B2 (en) 2020-01-02
IL282644A (en) 2021-06-30
EP3231801B1 (en) 2019-02-13
AU2021202685A1 (en) 2021-05-27
SG11201509180WA (en) 2015-12-30
IL264409A (en) 2019-02-28
HK1221466A1 (en) 2017-06-02
CR20150633A (es) 2016-04-05
MX385187B (es) 2025-03-14
KR102729910B1 (ko) 2024-11-15
SMT202500397T1 (it) 2025-11-10
BR112015028501B8 (pt) 2023-01-24
ME03355B (me) 2019-10-20
CR20190156A (es) 2019-05-16
PH12015502563B1 (en) 2019-04-26
SI3231801T1 (sl) 2019-05-31
US9382231B2 (en) 2016-07-05
AU2014265279A1 (en) 2015-11-26
MX2020004506A (es) 2021-08-09
HRP20210119T1 (hr) 2021-03-05
US20140343030A1 (en) 2014-11-20
RS67392B1 (sr) 2025-11-28
SMT201700258T1 (it) 2017-07-18
EA202090291A3 (ru) 2020-06-30
EP3527263A1 (en) 2019-08-21
IL282644B (en) 2021-10-31
IL287313A (en) 2021-12-01
NZ753639A (en) 2020-11-27
KR20240063187A (ko) 2024-05-10
WO2014186706A1 (en) 2014-11-20
US20200010456A1 (en) 2020-01-09
KR102442747B1 (ko) 2022-09-14
PE20200527A1 (es) 2020-03-09
IL287313B (en) 2022-03-01
EP3786162B1 (en) 2023-08-09
EP2997023B9 (en) 2018-06-13
ES2960731T3 (es) 2024-03-06
KR102341908B1 (ko) 2021-12-23
TWI719401B (zh) 2021-02-21
HRP20170795T1 (hr) 2017-08-25
EA202090291A2 (ru) 2020-05-31
TW202432140A (zh) 2024-08-16
EP4620528A2 (en) 2025-09-24
SMT201900223T1 (it) 2019-07-11
ES2720073T3 (es) 2019-07-17
EP3786162A1 (en) 2021-03-03
TW201940479A (zh) 2019-10-16
KR102663357B1 (ko) 2024-05-14
PT2997023T (pt) 2017-05-31
PT3231801T (pt) 2019-05-24

Similar Documents

Publication Publication Date Title
US12247020B2 (en) Bipyrazole derivatives as JAK inhibitors
HK40103736A (en) Bipyrazole derivatives as jak inhibitors
HK40049209B (en) Bipyrazole derivatives as jak inhibitors
NZ753637B2 (en) Bipyrazole derivatives as jak inhibitors
NZ753639B2 (en) Bipyrazole derivatives as jak inhibitors
NZ753636B2 (en) Bipyrazole derivatives as jak inhibitors
NZ753638B2 (en) Bipyrazole derivatives as jak inhibitors