MX2012004180A - Derivados de hidroxil, ceto y glucuronido de 3-(4-7h-pirrolo[2,3-d ]pirimidin-a-il)-1h-pirazol-1-il)-3-ciclopentilpropanonitrilo. - Google Patents

Derivados de hidroxil, ceto y glucuronido de 3-(4-7h-pirrolo[2,3-d ]pirimidin-a-il)-1h-pirazol-1-il)-3-ciclopentilpropanonitrilo.

Info

Publication number
MX2012004180A
MX2012004180A MX2012004180A MX2012004180A MX2012004180A MX 2012004180 A MX2012004180 A MX 2012004180A MX 2012004180 A MX2012004180 A MX 2012004180A MX 2012004180 A MX2012004180 A MX 2012004180A MX 2012004180 A MX2012004180 A MX 2012004180A
Authority
MX
Mexico
Prior art keywords
pentylpropanenitrile
pyrrolo
pyrazol
pyrimidin
keto
Prior art date
Application number
MX2012004180A
Other languages
English (en)
Spanish (es)
Inventor
James D Rodgers
Argyrios G Arvanitis
Stacey Shepard
Mei Li
Adam Shilling
Laurine G Galya
Frank M Nedza
Original Assignee
Incyte 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 filed Critical Incyte Corp
Publication of MX2012004180A publication Critical patent/MX2012004180A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
    • C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H15/00—Compounds containing hydrocarbon or substituted hydrocarbon radicals directly attached to hetero atoms of saccharide radicals
    • C07H15/26—Acyclic or carbocyclic radicals, substituted by hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Psychiatry (AREA)
  • Reproductive Health (AREA)
  • Heart & Thoracic Surgery (AREA)
MX2012004180A 2009-10-09 2010-10-08 Derivados de hidroxil, ceto y glucuronido de 3-(4-7h-pirrolo[2,3-d ]pirimidin-a-il)-1h-pirazol-1-il)-3-ciclopentilpropanonitrilo. MX2012004180A (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US25038709P 2009-10-09 2009-10-09
US31621810P 2010-03-22 2010-03-22
PCT/US2010/052011 WO2011044481A1 (en) 2009-10-09 2010-10-08 Hydroxyl, keto, and glucuronide derivatives of 3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile

Publications (1)

Publication Number Publication Date
MX2012004180A true MX2012004180A (es) 2012-07-17

Family

ID=43037845

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2012004180A MX2012004180A (es) 2009-10-09 2010-10-08 Derivados de hidroxil, ceto y glucuronido de 3-(4-7h-pirrolo[2,3-d ]pirimidin-a-il)-1h-pirazol-1-il)-3-ciclopentilpropanonitrilo.

Country Status (13)

Country Link
US (3) US8486902B2 (enExample)
EP (1) EP2486041B1 (enExample)
JP (3) JP5946768B2 (enExample)
KR (3) KR20180126619A (enExample)
CN (2) CN105541847B (enExample)
BR (1) BR112012008267B1 (enExample)
CA (1) CA2777114C (enExample)
EA (1) EA021478B1 (enExample)
ES (1) ES2435491T3 (enExample)
MX (1) MX2012004180A (enExample)
PL (1) PL2486041T3 (enExample)
PT (1) PT2486041E (enExample)
WO (1) WO2011044481A1 (enExample)

Families Citing this family (69)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK3184526T3 (en) 2005-12-13 2019-01-14 Incyte Holdings Corp PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR
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
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.
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
ES2487542T3 (es) * 2009-05-22 2014-08-21 Incyte Corporation Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus
WO2010135621A1 (en) * 2009-05-22 2010-11-25 Incyte Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
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
AU2011217961B2 (en) * 2010-02-18 2016-05-05 Incyte Holdings Corporation Cyclobutane and methylcyclobutane derivatives as Janus kinase inhibitors
SMT201800137T1 (it) 2010-03-10 2018-07-17 Incyte Holdings Corp Derivati di piperidin-4-il azetidina come inibitori di jak1
PH12012502296B1 (en) 2010-05-21 2017-10-06 Incyte Holdings Corp Topical formulation for a jak inhibitor
SG190839A1 (en) 2010-11-19 2013-07-31 Incyte Corp Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
ES2547916T3 (es) 2011-02-18 2015-10-09 Novartis Pharma Ag Terapia de combinación de inhibidores de mTOR/JAK
WO2012177606A1 (en) 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
JP2014521725A (ja) * 2011-08-10 2014-08-28 ノバルティス・ファルマ・アクチェンゲゼルシャフト ＪＡＫＰＩ３Ｋ／ｍＴＯＲ併用療法
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
EP4556010A3 (en) 2011-11-30 2025-07-23 Emory University Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae
WO2013173720A1 (en) 2012-05-18 2013-11-21 Incyte Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
CA2879603A1 (en) 2012-07-27 2014-01-30 Ratiopharm Gmbh Oral dosage forms for modified release comprising ruxolitinib
US9181271B2 (en) 2012-11-01 2015-11-10 Incyte Holdings Corporation Tricyclic fused thiophene derivatives as JAK inhibitors
PE20151157A1 (es) 2012-11-15 2015-08-19 Incyte Corp Formas de dosificacion de ruxolitinib de liberacion sostenida
EP2951590A1 (en) 2013-02-04 2015-12-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for assaying jak2 activity in red blood cells and uses thereof
LT3489239T (lt) 2013-03-06 2022-03-10 Incyte Holdings Corporation Jak inhibitoriaus gamybos būdai ir tarpiniai junginiai
HRP20231048T1 (hr) 2013-05-17 2023-12-22 Incyte Holdings Corporation Derivati bipirazola kao jak inhibitori
UA120499C2 (uk) 2013-08-07 2019-12-26 Інсайт Корпорейшн Лікування захворювань із застосуванням лікарських форм з уповільненим вивільненням для інгібітора jak1
MA39987A (fr) 2014-04-30 2017-03-08 Incyte Corp Procédés de préparation d'un inhibiteur de jak1 et nouvelles formes associées
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
JP6149810B2 (ja) * 2014-06-13 2017-06-21 株式会社島津製作所 代謝物解析システム及び代謝物解析方法
US20170231986A1 (en) 2014-08-11 2017-08-17 Acerta Pharma B.V. Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor, and/or a BCL-2 Inhibitor
US20170224819A1 (en) 2014-08-11 2017-08-10 Acerta Pharma B.V. Therapeutic Combinations of a BTK Inhibitor, a PI3K Inhibitor, a JAK-2 Inhibitor, and/or a CDK 4/6 Inhibitor
EP3179992B1 (en) 2014-08-11 2022-05-11 Acerta Pharma B.V. Therapeutic combinations of a btk inhibitor, a pd-1 inhibitor and/or a pd-l1 inhibitor
CN105777754B (zh) * 2014-12-16 2019-07-26 北京赛林泰医药技术有限公司 吡咯并嘧啶化合物
EA035816B1 (ru) 2015-11-24 2020-08-14 ТЕРЕВАНС БАЙОФАРМА Ар энд Ди АйПи, ЭлЭлСи Пролекарства jak-ингибирующего соединения для лечения воспалительного заболевания желудочно-кишечного тракта
CN107513067A (zh) * 2016-06-16 2017-12-26 北京赛林泰医药技术有限公司 含有取代环戊基的吡咯并嘧啶化合物
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
US10472366B2 (en) 2017-03-08 2019-11-12 Theravance Biopharma R&D Ip, Llc Glucuronide prodrugs of tofacitinib
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
CN108794480A (zh) * 2017-04-28 2018-11-13 天津药物研究院有限公司 吡咯并嘧啶类化合物、其制备方法和用途
JP2020520955A (ja) 2017-05-23 2020-07-16 セラヴァンス バイオファーマ アール＆ディー アイピー， エルエルシー ヤヌスキナーゼ阻害剤のグルクロニドプロドラッグ
WO2018217699A1 (en) 2017-05-23 2018-11-29 Theravance Biopharma R&D Ip, Llc Thiocarbamate prodrugs of tofacitinib
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
IL276302B2 (en) 2018-01-30 2023-11-01 Incyte Corp Procedures for preparing [1-(3-fluoro-2-(trifluoromethyl(isonicotinyl}piperidine-4-one)
CN118490690A (zh) 2018-02-16 2024-08-16 因赛特公司 用于治疗细胞因子相关的病症的jak1通路抑制剂
SMT202400306T1 (it) 2018-03-30 2024-09-16 Incyte Corp Trattamento dell'idrosadenite suppurativa utilizzando inibitori di jak.
US11584961B2 (en) 2018-03-30 2023-02-21 Incyte Corporation Biomarkers for inflammatory skin disease
AU2019252259A1 (en) 2018-04-13 2020-12-03 Incyte Corporation Biomarkers for graft-versus-host disease
CA3224985A1 (en) 2018-07-31 2020-02-06 Loxo Oncology, Inc. Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide
CN119751336A (zh) * 2018-09-06 2025-04-04 艾尼纳制药公司 可用于治疗自身免疫性病症和炎性病症的化合物
CN113490484B (zh) 2018-10-31 2024-08-23 因赛特公司 治疗血液疾病的组合疗法
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
EP3898615A1 (en) 2018-12-19 2021-10-27 Array Biopharma, Inc. 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer
CN113490666A (zh) 2018-12-19 2021-10-08 奥瑞生物药品公司 作为fgfr酪氨酸激酶的抑制剂的取代的吡唑并[1,5-a]吡啶化合物
US20220372135A1 (en) 2019-09-27 2022-11-24 Disc Medicine, Inc. Methods for treating myelofibrosis and related conditions
CN110538183B (zh) * 2019-10-09 2021-05-04 吉林大学 一种预防和治疗小儿湿疹的组合物及其制备方法
US12203942B2 (en) 2019-10-10 2025-01-21 Incyte Corporation Biomarkers for graft-versus-host disease
US12360120B2 (en) 2019-10-10 2025-07-15 Incyte Corporation Biomarkers for graft-versus-host disease
CR20220280A (es) 2019-11-22 2022-09-02 Incyte Corp Terapia de combinación que comprende un inhibidor de alk2 y un inhibidor de jak2
IL297437A (en) 2020-05-13 2022-12-01 Disc Medicine Inc Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis
PE20231102A1 (es) 2020-06-02 2023-07-19 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
KR20230096973A (ko) 2020-08-18 2023-06-30 인사이트 코포레이션 Jak 저해제를 제조하기 위한 방법 및 중간체
AU2021329301A1 (en) 2020-08-18 2023-04-13 Incyte Corporation Process and intermediates for preparing a JAK1 inhibitor
US11957661B2 (en) 2020-12-08 2024-04-16 Incyte Corporation JAK1 pathway inhibitors for the treatment of vitiligo
IL308216A (en) 2021-05-03 2024-01-01 Incyte Corp Jak1 pathway inhibitors for the treatment of prurigo nodularis
CN118317946A (zh) 2021-07-12 2024-07-09 因赛特公司 用于制备巴瑞替尼的方法和中间体

Family Cites Families (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3036390A1 (de) 1980-09-26 1982-05-13 Troponwerke GmbH & Co KG, 5000 Köln Neue pyrrolo-pyrimidine, verfahren zu ihrer herstellung und ihre verwendung bei der herstellung von biologischen wirkstoffen
US5521184A (en) 1992-04-03 1996-05-28 Ciba-Geigy Corporation Pyrimidine derivatives and processes for the preparation thereof
JP4010563B2 (ja) 1995-07-05 2007-11-21 イー・アイ・デユポン・ドウ・ヌムール・アンド・カンパニー 殺菌・殺カビ性のピリミジノン類
ATE212993T1 (de) 1995-07-06 2002-02-15 Novartis Erfind Verwalt Gmbh Pyrolopyrimidine und verfahren zu ihrer herstellung
US6232320B1 (en) 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
EP1090009A2 (en) 1998-06-04 2001-04-11 Abbott Laboratories Cell adhesion-inhibiting antinflammatory compounds
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
CZ20004727A3 (cs) 1998-06-19 2002-03-13 Pfizer Products Inc. Deriváty pyrrolo[2,3-d] pyrimidinu
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
AU777911B2 (en) * 1999-12-10 2004-11-04 Pfizer Products Inc. Pyrrolo(2,3-d)pyrimidine compounds
WO2001047922A2 (en) 1999-12-24 2001-07-05 Aventis Pharma Limited 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
EP1295607B9 (en) 2000-06-23 2011-10-05 Mitsubishi Tanabe Pharma Corporation Antitumor effect potentiators
UA74370C2 (uk) 2000-06-26 2005-12-15 Пфайзер Продактс Інк. Піроло(2,3-d)піримідинові сполуки як імуносупресори
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
GB0100622D0 (en) 2001-01-10 2001-02-21 Vernalis Res Ltd Chemical compounds V111
WO2002060492A1 (en) 2001-01-30 2002-08-08 Cytopia Pty Ltd Methods of inhibiting kinases
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
US6852727B2 (en) 2001-08-01 2005-02-08 Merck & Co., Inc. Benzimisazo[4,5-f]isoquinolinone derivatives
AU2002337142B2 (en) 2001-09-19 2007-10-11 Aventis Pharma S.A. Indolizines as kinase protein inhibitors
TWI302836B (en) 2001-10-30 2008-11-11 Novartis Ag Staurosporine derivatives as inhibitors of flt3 receptor tyrosine kinase activity
GT200200234A (es) 2001-12-06 2003-06-27 Compuestos cristalinos novedosos
TW200403058A (en) 2002-04-19 2004-03-01 Bristol Myers Squibb Co Heterocyclo inhibitors of potassium channel function
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
ATE371656T1 (de) 2002-11-04 2007-09-15 Vertex Pharma Heteroaryl-pyrimidinderivate als jak-inhibitoren
AR042052A1 (es) 2002-11-15 2005-06-08 Vertex Pharma Diaminotriazoles utiles como inhibidores de proteinquinasas
BR0316487A (pt) 2002-11-26 2005-10-11 Pfizer Prod Inc Método todo de tratamento da rejeição de transplantes
UA80767C2 (en) 2002-12-20 2007-10-25 Pfizer Prod Inc Pyrimidine derivatives for the treatment of abnormal cell growth
WO2004072063A1 (en) 2003-02-07 2004-08-26 Vertex Pharmaceuticals Incorporated Heteroaryl substituted pyrolls useful as inhibitors of protein kinases
GB0305929D0 (en) 2003-03-14 2003-04-23 Novartis Ag Organic compounds
SE0301373D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
SE0301372D0 (sv) 2003-05-09 2003-05-09 Astrazeneca Ab Novel compounds
US20050043346A1 (en) 2003-08-08 2005-02-24 Pharmacia Italia S.P.A. Pyridylpyrrole derivatives active as kinase inhibitors
PE20050952A1 (es) 2003-09-24 2005-12-19 Novartis Ag Derivados de isoquinolina como inhibidores de b-raf
BRPI0416909A (pt) 2003-11-25 2007-01-16 Pfizer Prod Inc método de tratamento de aterosclerose
SG133602A1 (en) 2003-12-17 2007-07-30 Pfizer Prod Inc Pyrrolo [2,3-d] pyrimidine compounds for treating transplant rejection
US20050165029A1 (en) 2004-01-13 2005-07-28 Ambit Biosciences Corporation Pyrrolopyrimidine derivatives and analogs and their use in the treatment and prevention of diseases
CA2560454C (en) 2004-03-30 2013-05-21 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of jak and other protein kinases
US20060106020A1 (en) 2004-04-28 2006-05-18 Rodgers James D Tetracyclic inhibitors of Janus kinases
WO2005105988A2 (en) 2004-04-28 2005-11-10 Vertex Pharmaceuticals Incorporated Crystal structure of human jak3 kinase domain complex and binding pockets thereof
EP2363149A1 (en) 2004-05-03 2011-09-07 Novartis AG Combinations comprising a S1P receptor agonist and a JAK3 kinase inhibitor
CA2566158A1 (en) 2004-05-14 2005-11-24 Abbott Laboratories Kinase inhibitors as therapeutic agents
PE20060426A1 (es) 2004-06-02 2006-06-28 Schering Corp DERIVADOS DE ACIDO TARTARICO COMO INHIBIDORES DE MMPs, ADAMs, TACE Y TNF-alfa
WO2006013114A1 (en) 2004-08-06 2006-02-09 Develogen Aktiengesellschaft Use of a timp-2 secreted protein product for preventing and treating pancreatic diseases and/or obesity and/or metabolic syndrome
UY29177A1 (es) 2004-10-25 2006-05-31 Astex Therapeutics Ltd Derivados sustituidos de purina, purinona y deazapurina, composiciones que los contienen métodos para su preparación y sus usos
MY179032A (en) 2004-10-25 2020-10-26 Cancer Research Tech Ltd Ortho-condensed pyridine and pyrimidine derivatives (e.g.purines) as protein kinase inhibitors
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.
WO2006083780A2 (en) * 2005-01-31 2006-08-10 Mylan Laboratories, Inc. Glucuronidated nebivolol
ES2320487T3 (es) * 2005-02-03 2009-05-22 Vertex Pharmaceuticals, Inc. Pirrolopirimidinas utiles como inhibidores de proteina quinasas.
US7019626B1 (en) * 2005-03-03 2006-03-28 Omnitek Engineering, Inc. Multi-fuel engine conversion system and method
ES2380795T3 (es) 2005-05-20 2012-05-18 Vertex Pharmaceuticals, Inc. Pirrolopiridinas útiles como inhibidores de proteínas quinasas
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
EP2270014A1 (en) 2005-09-22 2011-01-05 Incyte Corporation Azepine inhibitors of janus kinases
ES2401192T3 (es) 2005-09-30 2013-04-17 Vertex Pharmceuticals Incorporated Deazapurinas útiles como inhibidores de janus cinasas
DK3184526T3 (en) * 2005-12-13 2019-01-14 Incyte Holdings Corp PYRROLO [2,3-D] PYRIMIDINE DERIVATIVES AS A JANUS-KINASE INHIBITOR
EP1968568A4 (en) 2005-12-22 2011-04-13 Glaxosmithkline Llc HEMMER OF NUTS ACTIVITY
EP2537849A3 (en) 2006-01-17 2013-04-03 Vertex Pharmaceuticals, Inc. Azaindoles useful as inhibitors of janus kinases
RU2008143361A (ru) 2006-04-05 2010-05-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Деазапурины в качестве ингибиторов янус-киназ
US8513270B2 (en) 2006-12-22 2013-08-20 Incyte Corporation Substituted heterocycles as Janus kinase inhibitors
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
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.
ES2602577T3 (es) 2008-03-11 2017-02-21 Incyte Holdings Corporation Derivados de azetidina y ciclobutano como inhibidores de 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
ES2487542T3 (es) 2009-05-22 2014-08-21 Incyte Corporation Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus
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
AU2011217961B2 (en) 2010-02-18 2016-05-05 Incyte Holdings Corporation Cyclobutane and methylcyclobutane derivatives as Janus kinase inhibitors

Also Published As

Publication number Publication date
KR20180126619A (ko) 2018-11-27
KR20120102604A (ko) 2012-09-18
US9512161B2 (en) 2016-12-06
EA201200565A1 (ru) 2012-09-28
CN102596960B (zh) 2016-01-20
US8748401B2 (en) 2014-06-10
AU2010303245A1 (en) 2012-05-10
JP2017226695A (ja) 2017-12-28
JP5946768B2 (ja) 2016-07-06
CA2777114A1 (en) 2011-04-14
KR20170098334A (ko) 2017-08-29
EA021478B1 (ru) 2015-06-30
BR112012008267B1 (pt) 2022-10-04
CN102596960A (zh) 2012-07-18
CA2777114C (en) 2018-10-23
PL2486041T3 (pl) 2014-01-31
EP2486041A1 (en) 2012-08-15
CN105541847A (zh) 2016-05-04
WO2011044481A1 (en) 2011-04-14
JP2013507390A (ja) 2013-03-04
BR112012008267A2 (enExample) 2021-11-03
JP2016056183A (ja) 2016-04-21
JP6251232B2 (ja) 2017-12-20
US20140378400A1 (en) 2014-12-25
US20110086810A1 (en) 2011-04-14
ES2435491T3 (es) 2013-12-19
KR101921850B1 (ko) 2018-11-23
US20130345157A1 (en) 2013-12-26
US8486902B2 (en) 2013-07-16
CN105541847B (zh) 2019-08-16
HK1174899A1 (en) 2013-06-21
PT2486041E (pt) 2013-11-14
KR101805936B1 (ko) 2017-12-07
EP2486041B1 (en) 2013-08-14

Similar Documents

Publication Publication Date Title
MX2012004180A (es) Derivados de hidroxil, ceto y glucuronido de 3-(4-7h-pirrolo[2,3-d ]pirimidin-a-il)-1h-pirazol-1-il)-3-ciclopentilpropanonitrilo.
SI2432472T1 (sl) 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK
MX2009009773A (es) Sintesis de gamma-carbolinas fusionadas con heterociclo substituido.
PH12012501346A1 (en) Heteroaryl compounds and uses thereof
SG179085A1 (en) Pi3 kinase inhibitors and uses thereof
TN2009000446A1 (en) P70 s6 kinase inhibitors
WO2010077740A3 (en) Novel antiviral compounds, compositions, and methods of use
AP2012006166A0 (en) Pyrimidine derivatives as protein tyrosine kinase 2 inhibitors.
PH12013500870A1 (en) Heterocyclic compounds and uses thereof
MX2009008430A (es) Anticuerpos anti-robo4 y sus usos.
WO2008144223A3 (en) Triazolyl aminopyrimidine compounds
WO2010120994A3 (en) Ureidoaryl-and carbamoylaryl-morpholino- pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their synthesis
IL192948A0 (en) Novel pyridine derivatives
JO2822B1 (en) Inhibitors of the enzyme kinase P70 S6 and AKT
WO2009015037A3 (en) 5-pyridinone substituted indazoles
WO2010054107A3 (en) Kinase knockdown via electrophilically enhanced inhibitors
AU2007329728A1 (en) 3-(dihydro-1H-pyrazolo (4,3-d) pyrimidin-5-yl)-4-propoxybenzenesulfonamide derivatives and methods of use
TW200942530A (en) Pyridine compounds
MX2009013515A (es) Derivados de 7-alquinil-1,8-naftiridonas, su preparacion y su aplicacion en terapeutica.
MY185134A (en) 6-substituted phenoxychroman carboxylic acis derivatives
WO2011005554A3 (en) Recombinant ethanologenic bacteria
IL208262A0 (en) Hydroxyquinoxalinecar boxamide derivatives, compositions comprising the same and uses thereof
WO2008144222A3 (en) Triazolyl aminopyrimidine compounds
AU2009235634A8 (en) Substituted sulfonamide derivatives
WO2010077734A3 (en) Novel antiviral compounds, compositions, and methods of use

Legal Events

Date Code Title Description
FG Grant or registration