EA023444B1 - Циклобутановые и метилциклобутановые производные, композиции на их основе и способы их применения - Google Patents

Циклобутановые и метилциклобутановые производные, композиции на их основе и способы их применения Download PDF

Info

Publication number
EA023444B1
EA023444B1 EA201290807A EA201290807A EA023444B1 EA 023444 B1 EA023444 B1 EA 023444B1 EA 201290807 A EA201290807 A EA 201290807A EA 201290807 A EA201290807 A EA 201290807A EA 023444 B1 EA023444 B1 EA 023444B1
Authority
EA
Eurasian Patent Office
Prior art keywords
pyrrolo
pyrimidin
propannitrile
pyrazol
pharmaceutically acceptable
Prior art date
Application number
EA201290807A
Other languages
English (en)
Russian (ru)
Other versions
EA201290807A1 (ru
Inventor
Юнь-Лун Ли
Джеймс Д. Роджерс
Original Assignee
Инсайт Холдингс 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 Холдингс Корпорейшн filed Critical Инсайт Холдингс Корпорейшн
Publication of EA201290807A1 publication Critical patent/EA201290807A1/ru
Publication of EA023444B1 publication Critical patent/EA023444B1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • 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
    • 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • 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
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
EA201290807A 2010-02-18 2011-02-18 Циклобутановые и метилциклобутановые производные, композиции на их основе и способы их применения EA023444B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US30563010P 2010-02-18 2010-02-18
PCT/US2011/025433 WO2011103423A1 (en) 2010-02-18 2011-02-18 Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors

Publications (2)

Publication Number Publication Date
EA201290807A1 EA201290807A1 (ru) 2013-03-29
EA023444B1 true EA023444B1 (ru) 2016-06-30

Family

ID=44227587

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201290807A EA023444B1 (ru) 2010-02-18 2011-02-18 Циклобутановые и метилциклобутановые производные, композиции на их основе и способы их применения

Country Status (11)

Country Link
US (2) US20110207754A1 (enExample)
EP (1) EP2536729A1 (enExample)
JP (1) JP5858434B2 (enExample)
KR (1) KR101836538B1 (enExample)
CN (1) CN102844317B (enExample)
AU (1) AU2011217961B2 (enExample)
BR (1) BR112012020693B1 (enExample)
CA (1) CA2790070C (enExample)
EA (1) EA023444B1 (enExample)
MX (1) MX2012009541A (enExample)
WO (1) WO2011103423A1 (enExample)

Families Citing this family (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1966202E (pt) 2005-12-13 2012-01-03 Incyte Corp Pirrolo[2,3-b] pirimidinas e pirrolo[2,3-b]piridinas substituídas com heteroarilo como inibidores de janus quinase
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.
RS53245B2 (sr) 2007-06-13 2022-10-31 Incyte Holdings Corp Soli inhibitora janus kinaze (r)-3-(4-(7h-pirolo(2,3-d) pirimidin-4-il)-1h-pirazol-1-il)-3-ciklopentilpropan-nitrila
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
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
PL2432472T3 (pl) 2009-05-22 2020-03-31 Incyte Holdings Corporation 3-[4-(7H-Pirolo[2,3-d]pirymidyn-4-ylo)-1H-pirazol-1-ilo]oktano- lub heptano-nitryle jako inhibitory JAK
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
ES2435491T3 (es) 2009-10-09 2013-12-19 Incyte Corporation Derivados de hidroxilo, ceto y glucurónido de 3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo
MX354212B (es) 2010-03-10 2018-02-19 Incyte Corp Derivados de piperidin-4-il azetidina como inhibidores de janus cinasa 1 (jak1).
EA202091303A3 (ru) 2010-05-21 2021-05-31 Инсайт Холдингс Корпорейшн Композиция ингибитора jak для местного применения
CA2818542A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
WO2012068440A1 (en) 2010-11-19 2012-05-24 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as jak inhibitors
EP2675451B9 (en) 2011-02-18 2017-07-26 Novartis Pharma AG mTOR/JAK INHIBITOR COMBINATION THERAPY
CN103797010B (zh) 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
HK1198579A1 (en) 2011-08-10 2015-04-30 Novartis Pharma Ag Jak p13k/mtor combination therapy
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
US9394282B2 (en) * 2011-09-22 2016-07-19 Merck Sharp & Dohme Corp. Pyrazole carboxamides as Janus kinase inhibitors
CA2856722C (en) 2011-11-30 2022-11-22 Emory University Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
BR112015009942A2 (pt) 2012-11-01 2017-07-11 Incyte Corp derivados de tiofeno fundidos tricíclicos como inibidores de jak
NZ708157A (en) 2012-11-15 2019-07-26 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
US20160123982A1 (en) 2013-02-04 2016-05-05 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for assaying jak2 activity in red blood cells and uses thereof
TWI634121B (zh) 2013-03-06 2018-09-01 英塞特控股公司 用於製備jak抑制劑之方法及中間物
US20140343034A1 (en) * 2013-04-25 2014-11-20 Japan Tobacco Inc. Skin barrier function improving agent
WO2014186706A1 (en) 2013-05-17 2014-11-20 Incyte Corporation Bipyrazole derivatives as jak inhibitors
MX394928B (es) 2013-08-07 2025-03-24 Incyte Holdings Corp Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1).
CN105555313A (zh) 2013-08-20 2016-05-04 因赛特公司 在c-反应蛋白水平较高的实体肿瘤患者中的存活益处
HRP20201887T1 (hr) 2014-04-08 2021-02-05 Incyte Corporation LIJEČENJE B-STANIČNIH MALIGNITETA S KOMBINACIJOM INHIBITORA JAK i PI3K
SG11201609016VA (en) 2014-04-30 2016-11-29 Incyte Corp Processes of preparing a jak1 inhibitor and new forms thereto
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
WO2018167283A1 (en) 2017-03-17 2018-09-20 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma associated neural remodeling
US20200088732A1 (en) 2017-04-13 2020-03-19 INSERM (Institut National de la Santé et de la Recherche Mèdicale) Methods for the diagnosis and treatment of pancreatic ductal adenocarcinoma
AR113922A1 (es) 2017-12-08 2020-07-01 Incyte Corp Terapia de combinación de dosis baja para el tratamiento de neoplasias mieloproliferativas
WO2019152374A1 (en) 2018-01-30 2019-08-08 Incyte Corporation Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
WO2019161098A1 (en) 2018-02-16 2019-08-22 Incyte Corporation Jak1 pathway inhibitors for the treatment of cytokine-related disorders
HUE067471T2 (hu) 2018-03-30 2024-10-28 Incyte Corp Gennyes verejtékmirigy-gyulladás kezelése jak inhibitorok alkalmazásával
US11584961B2 (en) 2018-03-30 2023-02-21 Incyte Corporation Biomarkers for inflammatory skin disease
US11372003B2 (en) 2018-04-13 2022-06-28 Incyte Corporation Biomarkers for graft-versus-host disease
BR112020024427A2 (pt) 2018-06-01 2021-03-23 Incyte Corporation regime de dosagem para o tratamento de distúrbios relacionados a pi3k
KR20210109522A (ko) 2018-10-31 2021-09-06 인사이트 코포레이션 혈액 질환의 치료를 위한 병용 요법
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
KR20220088699A (ko) 2019-09-27 2022-06-28 디스크 메디슨, 인크. 골수섬유증 및 관련 상태의 치료 방법
EP4041204A1 (en) 2019-10-10 2022-08-17 Incyte Corporation Biomarkers for graft-versus-host disease
US12360120B2 (en) 2019-10-10 2025-07-15 Incyte Corporation Biomarkers for graft-versus-host disease
CA3160312A1 (en) 2019-11-22 2021-05-27 Incyte Corporation Combination therapy comprising an alk2 inhibitor and a jak2 inhibitor
JP2023528868A (ja) 2020-06-02 2023-07-06 インサイト・コーポレイション Jak1阻害剤の調製プロセス
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
BR112023002939A2 (pt) 2020-08-18 2023-04-25 Incyte Corp Processo e intermediários para preparar um inibidor de jak1
WO2022040180A1 (en) 2020-08-18 2022-02-24 Incyte Corporation Process and intermediates for preparing a jak inhibitor
JP2023552452A (ja) 2020-12-08 2023-12-15 インサイト・コーポレイション 白斑治療用のjak1経路阻害薬
US12268667B2 (en) 2021-05-03 2025-04-08 Incyte Corporation JAK1 pathway inhibitors for the treatment of prurigo nodularis
JP2024526762A (ja) 2021-07-12 2024-07-19 インサイト・コーポレイション Jak阻害剤を調製するためのプロセス及び中間体

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070135461A1 (en) * 2005-12-13 2007-06-14 Rodgers James D Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
US20080312259A1 (en) * 2007-06-13 2008-12-18 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
WO2009064835A1 (en) * 2007-11-16 2009-05-22 Incyte Corporation 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors
WO2009114512A1 (en) * 2008-03-11 2009-09-17 Incyte Corporation Azetidine and cyclobutane derivatives as jak inhibitors

Family Cites Families (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
US6232320B1 (en) * 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
PA8474101A1 (es) * 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
BR9912938B1 (pt) 1998-08-11 2011-06-28 derivados de isoquinolina, composição que os compreende, processo para preparação e uso dos mesmos.
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
MXPA02006338A (es) * 1999-12-24 2002-12-13 Aventis Pharma Ltd Azaindoles.
GB0004890D0 (en) 2000-03-01 2000-04-19 Astrazeneca Uk Ltd Chemical compounds
US6335342B1 (en) * 2000-06-19 2002-01-01 Pharmacia & Upjohn S.P.A. Azaindole derivatives, process for their preparation, and their use as antitumor agents
DE60141963D1 (de) * 2000-06-23 2010-06-10 Mitsubishi Tanabe Pharma Corp Antitumoreffekt-verstärker
ES2225624T3 (es) 2000-06-28 2005-03-16 Smithkline Beecham Plc Procedimiento de molienda por via humeda.
CA2446864C (en) * 2001-05-16 2011-02-15 Vertex Pharmaceuticals Incorporated Inhibitors of src and other protein kinases
ES2274986T3 (es) * 2001-08-01 2007-06-01 MERCK & CO., INC. Derivados de benzimidazo 4,5-f/isoquinolinona.
ATE420879T1 (de) 2001-09-19 2009-01-15 Aventis Pharma Sa Indolizine als kinaseproteinhemmer
US7973031B2 (en) 2001-10-30 2011-07-05 Novartis Ag Staurosporine derivatives as inhibitors of FLT3 receptor tyrosine kinase activity
TW200403058A (en) * 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
EP1506189A1 (en) * 2002-04-26 2005-02-16 Vertex Pharmaceuticals Incorporated Pyrrole derivatives as inhibitors of erk2 and uses thereof
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
EP1541563A4 (en) * 2002-07-10 2007-11-07 Ono Pharmaceutical Co ANTAGONIST OF CCR4 AND CORRESPONDING MEDICINAL USE
CL2003002353A1 (es) 2002-11-15 2005-02-04 Vertex Pharma Compuestos derivados de diaminotriazoles, inhibidores d ela proteina quinasa; composicion farmaceutica; procedimiento de preparacion; y su uso del compuesto en el tratamiento de enfermedades de desordenes alergicos, proliferacion, autoinmunes, condic
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
WO2005067546A2 (en) * 2004-01-13 2005-07-28 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
US20060106020A1 (en) * 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
BRPI0511978A (pt) 2004-06-10 2008-01-22 Irm Llc compostos e composições como inibidores de proteìnas quinases
WO2006001463A1 (ja) * 2004-06-23 2006-01-05 Ono Pharmaceutical Co., Ltd. S1p受容体結合能を有する化合物およびその用途
JP2008520612A (ja) 2004-11-24 2008-06-19 ノバルティス アクチエンゲゼルシャフト JAK阻害剤およびBcr−Abl、Flt−3、FAKまたはRAFキナーゼ阻害剤のうち少なくとも1個の組合せ
AR054416A1 (es) * 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
KR20070104641A (ko) * 2005-02-03 2007-10-26 버텍스 파마슈티칼스 인코포레이티드 단백질 키나제의 억제제로 유용한 피롤로피리미딘
NZ564065A (en) * 2005-05-20 2011-03-31 Vertex Pharma Pyrrolopyridines useful as inhibitors of protein kinase
EP1926735A1 (en) * 2005-09-22 2008-06-04 Incyte Corporation Tetracyclic inhibitors of janus kinases
US20070208053A1 (en) * 2006-01-19 2007-09-06 Arnold Lee D Fused heterobicyclic kinase inhibitors
EP1981887A2 (en) * 2006-02-01 2008-10-22 SmithKline Beecham Corporation Pyrrolo[2,3,b]pyridine derivatives useful as raf kinase inhibitors
CA2648250A1 (en) * 2006-04-05 2007-10-18 Vertex Pharmaceuticals Incorporated Deazapurines useful as inhibitors of janus kinases
US8111686B2 (en) * 2006-08-07 2012-02-07 Microsoft Corporation Aggregating endpoint capabilities for a user
EP1918291A1 (en) * 2006-10-30 2008-05-07 Novartis AG 3-Aminocarbonyl-substituted fused pyrazolo-derivatives as protein kinase modulators
EP2121692B1 (en) * 2006-12-22 2013-04-10 Incyte Corporation Substituted heterocycles as janus kinase inhibitors
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.
WO2009073575A2 (en) * 2007-11-30 2009-06-11 Oregon Health & Science University Methods for treating induced cellular proliferative disorders
JOP20190231A1 (ar) * 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
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
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
ES2435491T3 (es) * 2009-10-09 2013-12-19 Incyte Corporation Derivados de hidroxilo, ceto y glucurónido de 3-(4-(7H-pirrolo[2,3-d]pirimidin-4-il)-1H-pirazol-1-il)-3-ciclopentilpropanonitrilo

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070135461A1 (en) * 2005-12-13 2007-06-14 Rodgers James D Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
US20080312259A1 (en) * 2007-06-13 2008-12-18 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
WO2009064835A1 (en) * 2007-11-16 2009-05-22 Incyte Corporation 4-pyrazolyl-n-arylpyrimidin-2-amines and 4-pyrazolyl-n-heteroarylpyrimidin-2-amines as janus kinase inhibitors
WO2009114512A1 (en) * 2008-03-11 2009-09-17 Incyte Corporation Azetidine and cyclobutane derivatives as jak inhibitors

Also Published As

Publication number Publication date
BR112012020693B1 (pt) 2020-05-12
BR112012020693A2 (pt) 2016-07-26
AU2011217961B2 (en) 2016-05-05
MX2012009541A (es) 2012-10-01
WO2011103423A1 (en) 2011-08-25
CN102844317B (zh) 2015-06-03
US20110207754A1 (en) 2011-08-25
CN102844317A (zh) 2012-12-26
JP2013520436A (ja) 2013-06-06
KR20130009763A (ko) 2013-01-23
CA2790070A1 (en) 2011-08-25
CA2790070C (en) 2018-03-06
EA201290807A1 (ru) 2013-03-29
KR101836538B1 (ko) 2018-03-08
US20150087662A1 (en) 2015-03-26
AU2011217961A1 (en) 2012-09-06
EP2536729A1 (en) 2012-12-26
BR112012020693A8 (pt) 2017-07-11
JP5858434B2 (ja) 2016-02-10

Similar Documents

Publication Publication Date Title
EA023444B1 (ru) Циклобутановые и метилциклобутановые производные, композиции на их основе и способы их применения
JP5048514B2 (ja) JANUSキナーゼ阻害剤としてのピロロ[2,3−b]ピリジン−4−イル−アミンおよびピロロ[2,3−b]ピリミジン−4−イル−アミン
JP6302442B2 (ja) Jak阻害薬としての3−[4−(7h−ピロロ[2,3−d]ピリミジン−4−イル)−1h−ピラゾール−1−イル]オクタン−またはヘプタン−ニトリル
JP5711813B2 (ja) βセクレターゼ(BACE)の阻害剤として有用な5,6−ジヒドロ−2H−[1,4]オキサジン−3−イル−アミン誘導体
JP5917544B2 (ja) 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
WO2019134539A1 (zh) 二氢吡唑酮并嘧啶类化合物及其制备方法和用途
JP2010518080A (ja) 治療薬
JP2021193149A (ja) 末梢セロトニンと関連する疾患または障害を処置するためのトリプトファンヒドロキシラーゼ1(tph1)の結晶性スピロ環式化合物インヒビター
WO2015058661A1 (zh) Bcr-abl激酶抑制剂及其应用
JP2002532503A (ja) プロテインキナーゼ阻害剤としての4,5−ピラジノオキシンドール
EP1885725B1 (en) Tricyclic azole derivatives, their manufacture and use as pharmaceutical agents
CN101965349A (zh) 用作抗增殖剂的吡唑并[3,4-d]-嘧啶衍生物
KR20130093140A (ko) 옥사졸로[5,4-b]피리딘-5-일 화합물 및 암의 치료를 위한 그의 용도
HK1168773A (en) 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
HK1168773B (en) 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
AU2015255289A1 (en) 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors