NO328578B1 - Forbindelse samt anvendelse derav, og farmasoytisk preparat - Google Patents

Forbindelse samt anvendelse derav, og farmasoytisk preparat Download PDF

Info

Publication number
NO328578B1
NO328578B1 NO20035201A NO20035201A NO328578B1 NO 328578 B1 NO328578 B1 NO 328578B1 NO 20035201 A NO20035201 A NO 20035201A NO 20035201 A NO20035201 A NO 20035201A NO 328578 B1 NO328578 B1 NO 328578B1
Authority
NO
Norway
Prior art keywords
pharmaceutically acceptable
methyl
mammal
acceptable salt
compound according
Prior art date
Application number
NO20035201A
Other languages
English (en)
Norwegian (no)
Other versions
NO20035201L (no
NO20035201D0 (no
Inventor
Mark Edward Flanagan
Michael John Munchhof
Glenn Ernest Wilcox
Christian Koecher
Ton Rene Vries
Original Assignee
Pfizer Prod Inc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26968730&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NO328578(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of NO20035201L publication Critical patent/NO20035201L/no
Publication of NO20035201D0 publication Critical patent/NO20035201D0/no
Publication of NO328578B1 publication Critical patent/NO328578B1/no

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
    • 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
    • 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
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • 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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D211/36Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D211/56Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Pulmonology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Hydrogenated Pyridines (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
NO20035201A 2001-05-31 2003-11-24 Forbindelse samt anvendelse derav, og farmasoytisk preparat NO328578B1 (no)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US29477501P 2001-05-31 2001-05-31
US34104801P 2001-12-06 2001-12-06
PCT/IB2002/001905 WO2002096909A1 (en) 2001-05-31 2002-05-29 Optical resolution of (1-benzyl-4-methylpiperidin-3-yl) -methylamine and the use thereof for the preparation of pyrrolo 2,3-pyrimidine derivatives as protein kinases inhibitors

Publications (3)

Publication Number Publication Date
NO20035201L NO20035201L (no) 2003-11-24
NO20035201D0 NO20035201D0 (no) 2003-11-24
NO328578B1 true NO328578B1 (no) 2010-03-22

Family

ID=26968730

Family Applications (3)

Application Number Title Priority Date Filing Date
NO20035201A NO328578B1 (no) 2001-05-31 2003-11-24 Forbindelse samt anvendelse derav, og farmasoytisk preparat
NO20093135A NO20093135L (no) 2001-05-31 2009-10-13 Optisk opplosning av (1-benzyl-4-metylpiperidin-3-yl) -metylamin og anvendelse derav for fremstilling av pyrrolo 2,3-pyrimidinderivater som protein kinase inhibitorer
NO2017047C NO2017047I1 (no) 2001-05-31 2017-09-08 Tofacitinib, evt. i form av et farmasøytisk akseptabelt salt, inkludert citratsalt

Family Applications After (2)

Application Number Title Priority Date Filing Date
NO20093135A NO20093135L (no) 2001-05-31 2009-10-13 Optisk opplosning av (1-benzyl-4-metylpiperidin-3-yl) -metylamin og anvendelse derav for fremstilling av pyrrolo 2,3-pyrimidinderivater som protein kinase inhibitorer
NO2017047C NO2017047I1 (no) 2001-05-31 2017-09-08 Tofacitinib, evt. i form av et farmasøytisk akseptabelt salt, inkludert citratsalt

Country Status (52)

Country Link
US (2) US7301023B2 (cs)
EP (3) EP1666481B9 (cs)
JP (1) JP4381137B2 (cs)
KR (5) KR100926875B1 (cs)
CN (1) CN1729192A (cs)
AP (1) AP1859A (cs)
AR (2) AR037321A1 (cs)
AT (1) ATE519741T1 (cs)
AU (2) AU2002304401C1 (cs)
BE (1) BE2017C032I2 (cs)
BG (1) BG66489B1 (cs)
BR (1) BR0209246A (cs)
CA (1) CA2448281C (cs)
CL (1) CL2008000762A1 (cs)
CR (1) CR10177A (cs)
CU (1) CU23337B7 (cs)
CY (2) CY1113322T1 (cs)
CZ (1) CZ304366B6 (cs)
DK (1) DK1666481T3 (cs)
EA (2) EA007251B1 (cs)
EC (1) ECSP034865A (cs)
EE (1) EE05332B1 (cs)
ES (2) ES2369226T3 (cs)
FR (1) FR17C1031I2 (cs)
GE (1) GEP20063784B (cs)
GT (2) GT200200100AA (cs)
HR (1) HRP20030943B1 (cs)
HU (2) HU230876B1 (cs)
IL (1) IL158588A0 (cs)
IS (1) IS3023B (cs)
LT (1) LTC1666481I2 (cs)
LU (1) LUC00031I2 (cs)
MA (1) MA27029A1 (cs)
MX (1) MXPA03011062A (cs)
MY (1) MY129649A (cs)
NL (1) NL300887I2 (cs)
NO (3) NO328578B1 (cs)
NZ (2) NZ540332A (cs)
OA (1) OA12612A (cs)
PA (1) PA8546301A1 (cs)
PE (1) PE20030561A1 (cs)
PL (2) PL367945A1 (cs)
PT (1) PT1666481E (cs)
RS (1) RS52144B (cs)
SI (1) SI1666481T1 (cs)
SK (2) SK288192B6 (cs)
TN (1) TNSN03128A1 (cs)
TW (2) TWI316061B (cs)
UA (1) UA80093C2 (cs)
UY (1) UY27317A1 (cs)
WO (1) WO2002096909A1 (cs)
ZA (1) ZA200307982B (cs)

Families Citing this family (124)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
EA006227B1 (ru) * 1999-12-10 2005-10-27 Пфайзер Продактс Инк. СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА
EA006153B1 (ru) * 2000-06-26 2005-10-27 Пфайзер Продактс Инк. СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ИММУНОДЕПРЕССАНТОВ
PY0228255A (es) 2001-12-06 2004-06-01 Pfizer Prod Inc Compuestos cristalinos novedosos
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
BR0313059B8 (pt) 2002-07-29 2021-07-27 Rigel Pharmaceuticals composto, e, composição farmacêutica
ATE402700T1 (de) * 2002-08-27 2008-08-15 Merck Patent Gmbh Glycinamid-derivate als raf-kinase-hemmer
AU2003276591A1 (en) 2002-11-26 2004-06-18 Pfizer Products Inc. Method of treatment of transplant rejection
CN102358738A (zh) 2003-07-30 2012-02-22 里格尔药品股份有限公司 2,4-嘧啶二胺化合物及其预防和治疗自体免疫疾病的用途
MXPA06012663A (es) * 2004-05-03 2007-01-16 Novartis Ag Combinaciones que comprenden un agonista del receptor s1p y un inhibidor de quinasa jak3.
MXPA06015237A (es) 2004-06-29 2007-12-10 Amgen Inc Pirrolo[2-3-d]pirimidinas que modulan la actividad de ack1 y lck.
US7465726B2 (en) 2004-08-02 2008-12-16 Osi Pharmaceuticals, Inc. Substituted pyrrolo[2.3-B]pyridines
KR20070085433A (ko) * 2004-11-24 2007-08-27 노파르티스 아게 Jak 저해제들과 bcr-abl, flt-3, fak 또는raf 키나제 저해제들 중 하나 이상의 조합물
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.
EP1904457B1 (en) 2005-06-08 2017-09-06 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
KR20080026654A (ko) 2005-07-14 2008-03-25 아스텔라스세이야쿠 가부시키가이샤 헤테로시클릭 야누스 키나제 3 억제제
CN102127078A (zh) 2005-07-14 2011-07-20 安斯泰来制药株式会社 Janus激酶3的杂环类抑制剂
CN101233138A (zh) * 2005-07-29 2008-07-30 辉瑞产品公司 吡咯并[2,3-d]嘧啶衍生物、其中间体和合成方法
EP2270014A1 (en) 2005-09-22 2011-01-05 Incyte Corporation Azepine inhibitors of janus kinases
CN103214484B (zh) 2005-12-13 2016-07-06 因塞特控股公司 作为两面神激酶抑制剂的杂芳基取代的吡咯并[2,3-b]吡啶和吡咯并[2,3-b]嘧啶
JP2009528295A (ja) 2006-02-24 2009-08-06 ライジェル ファーマシューティカルズ, インコーポレイテッド Jak経路の阻害のための組成物および方法
GB0605691D0 (en) * 2006-03-21 2006-05-03 Novartis Ag Organic Compounds
ES2415863T3 (es) 2006-12-22 2013-07-29 Incyte Corporation Heterociclos sustituidos como inhibidores de Janus Quinasas
HUE029236T2 (en) 2007-06-13 2017-02-28 Incyte Holdings Corp (R) -3- (4- (7H-Pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-cyclopentylpropanenitrile Crystalline salts of Janus kinase inhibitor
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.
CA2691914C (en) * 2007-07-11 2012-06-26 Pfizer Inc. Pharmaceutical compositions and methods of treating dry eye disorders
HUE030912T2 (en) 2008-02-15 2017-06-28 Rigel Pharmaceuticals Inc Pyrimidine-2-amine compounds and their use as inhibitors of yak kinases
TWI444382B (zh) 2008-03-11 2014-07-11 Incyte Corp 作為jak抑制劑之氮雜環丁烷及環丁烷衍生物
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
MX2010011463A (es) 2008-04-16 2011-06-03 Portola Pharm Inc 2,6-diamino-pirimidin-5-il-carboxamidas como inhibidores de syk o jak quinasas.
JP2011518219A (ja) 2008-04-22 2011-06-23 ポートラ ファーマシューティカルズ, インコーポレイテッド タンパク質キナーゼの阻害剤
EP2324020A2 (en) * 2008-08-01 2011-05-25 Biocryst Pharmaceuticals, Inc. Piperidine derivatives as jak3 inhibitors
HRP20140395T1 (hr) 2008-08-20 2014-06-06 Zoetis Llc SPOJEVI PIROLO[2,3-d]PIRIMIDINA
JP2012517448A (ja) * 2009-02-11 2012-08-02 リアクション バイオロジー コープ. 選択的キナーゼ阻害剤
EP3026052A1 (en) 2009-04-20 2016-06-01 Auspex Pharmaceuticals, Inc. Preparation of deuterated piperidine inhibitors of janus kinase 3
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
EP2432472B1 (en) 2009-05-22 2019-10-02 Incyte Holdings Corporation 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak 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
CA2773182A1 (en) * 2009-09-10 2011-03-17 F. Hoffmann-La Roche Ag Inhibitors of jak
MX2012004180A (es) 2009-10-09 2012-07-17 Incyte Corp Derivados de hidroxil, ceto y glucuronido de 3-(4-7h-pirrolo[2,3-d ]pirimidin-a-il)-1h-pirazol-1-il)-3-ciclopentilpropanonitrilo.
IN2012DN02577A (cs) 2009-10-15 2015-08-28 Pfizer
ES2461967T3 (es) 2009-12-18 2014-05-21 Pfizer Inc. Compuestos de pirrolo[2,3-d]pirimidina
WO2011086053A1 (en) * 2010-01-12 2011-07-21 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof
EP2531508A1 (en) 2010-02-05 2012-12-12 Pfizer Inc. Pyrrolo [ 2, 3 - d]pyrimidine urea compounds as jak inhibitors
EP3354652B1 (en) 2010-03-10 2020-05-06 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
AR084691A1 (es) 2010-05-21 2013-06-05 Incyte Corp Formulacion de uso topico para un inhibidor de jak y metodo para tratar trastorno de la piel
EP2635557A2 (en) 2010-11-01 2013-09-11 Portola Pharmaceuticals, Inc. Nicotinamides as jak kinase modulators
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
EP2481411A1 (en) 2011-01-27 2012-08-01 Ratiopharm GmbH Oral dosage forms for modified release comprising the JAK3 inhibitor tasocitinib
EP2481397A1 (en) 2011-01-27 2012-08-01 Ratiopharm GmbH Pharmaceutical compositions comprising tasocitinib
WO2012112847A1 (en) 2011-02-18 2012-08-23 Novartis Pharma Ag mTOR/JAK INHIBITOR COMBINATION THERAPY
WO2012135338A1 (en) 2011-03-28 2012-10-04 Ratiopharm Gmbh Processes for preparing tofacitinib salts
US9050342B2 (en) 2011-03-29 2015-06-09 Pfizer Inc. Beneficial effects of combination therapy on cholesterol
CN104610264A (zh) * 2011-04-08 2015-05-13 辉瑞大药厂 结晶和非结晶形式的托法替尼,以及包含托法替尼和渗透增强剂的药物组合物
EP2524688B1 (en) 2011-05-11 2013-05-01 ratiopharm GmbH Composition for modified release comprising ranolazine
MY165963A (en) 2011-06-20 2018-05-18 Incyte Holdings Corp Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
CA2844507A1 (en) 2011-08-10 2013-02-14 Novartis Pharma Ag Jak pi3k/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
SG11201402570QA (en) 2011-11-23 2014-06-27 Portola Pharm Inc Pyrazine kinase inhibitors
CA3131037A1 (en) 2011-11-30 2013-06-06 Emory University Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections
US10821111B2 (en) 2011-11-30 2020-11-03 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
EP2791141B1 (en) 2011-12-15 2017-02-08 ratiopharm GmbH Tofacitinib mono-tartrate salt
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲jak抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
CN104837817B (zh) 2012-07-25 2017-03-22 力奇制药公司 制备3‑氨基‑哌啶化合物的合成路线
US9676756B2 (en) 2012-10-08 2017-06-13 Portola Pharmaceuticals, Inc. Substituted pyrimidinyl kinase inhibitors
TWI761825B (zh) 2012-11-15 2022-04-21 美商英塞特控股公司 盧梭利替尼之緩釋性劑型
CN104955803B (zh) * 2012-11-30 2017-11-28 斯洛文尼亚莱柯制药股份有限公司 通过硝基‑四氢吡啶前体制备3‑氨基‑哌啶化合物
WO2014097150A1 (en) 2012-12-17 2014-06-26 Ranbaxy Laboratories Limited Process for the preparation of tofacitinib and intermediates thereof
WO2014102826A1 (en) 2012-12-28 2014-07-03 Glenmark Pharmaceuticals Limited; The present invention relates to process for the preparation of tofacitinib and intermediates thereof.
EP3290421B1 (en) 2013-02-22 2019-01-02 Pfizer Inc Combination of pyrrolo [2, 3 -d]pyrimidine derivatives with one or more additional agents as inhibitors of janus- related kinases (jak)
MX384910B (es) 2013-03-06 2025-03-14 Incyte Holdings Corp Procesos e intermedios para hacer un inhibidor de jak.
JP6041823B2 (ja) 2013-03-16 2016-12-14 ファイザー・インク トファシチニブの経口持続放出剤形
US20140343034A1 (en) 2013-04-25 2014-11-20 Japan Tobacco Inc. Skin barrier function improving agent
WO2014174073A1 (en) 2013-04-26 2014-10-30 Sandoz Ag Sustained release formulations of tofacitinib
SG11201600815WA (en) 2013-08-07 2016-03-30 Incyte Corp Sustained release dosage forms for a jak1 inhibitor
CN104513248B (zh) * 2013-09-30 2019-05-24 重庆医药工业研究院有限责任公司 一种托法替尼中间体的纯化方法
ES2654051T3 (es) 2013-12-05 2018-02-12 Pfizer Inc. Pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinilo y pirrolo[2,3-d]piridinil acrilamidas
MX362290B (es) * 2013-12-09 2019-01-10 Unichem Lab Ltd Un proceso mejorado para la preparacion de (3r,4r)-(1-bencilo-4-me tilpiperidina-3-il)-metilamina.
CA2881262A1 (en) 2014-02-06 2015-08-06 Prabhudas Bodhuri Solid forms of tofacitinib salts
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
EP3180344B1 (en) 2014-08-12 2019-09-18 Pfizer Inc Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase
AU2016208906B2 (en) * 2015-01-20 2018-07-12 Wuxi Fortune Pharmaceutical Co., Ltd JAK inhibitor
JP6687596B2 (ja) 2015-02-17 2020-04-22 アモーレパシフィック コーポレーションAmorepacific Corporation N−[4−(1−アミノエチル)−フェニル]−スルホンアミド誘導体のキラル分割方法
CN104761556B (zh) * 2015-03-21 2017-06-23 河北国龙制药有限公司 托法替布中间体杂质、托法替布杂质及其合成方法,以及托法替布的质量监控方法
EP3078665A1 (en) * 2015-04-10 2016-10-12 OLON S.p.A. Efficient method for the preparation of tofacitinib citrate
UA119701C2 (uk) 2015-04-29 2019-07-25 Вуксі Фортуне Фармасьютікал Ко., Лтд Піримідинові сполуки як jak-інгібітори
ES2928757T3 (es) 2015-05-01 2022-11-22 Pfizer Acrilamidas de pirrolo[2,3-b]pirazinilo y epóxidos de las mismas como inhibidores de la Janus Quinasa
DK3305788T3 (da) 2015-05-29 2020-09-28 Wuxi Fortune Pharmaceutical Co Ltd Janus-kinase-hæmmer
JP6507272B2 (ja) * 2015-07-27 2019-04-24 ユニケム ラボラトリーズ リミテッド トファシチニブ口腔内崩壊錠
KR101771219B1 (ko) * 2015-08-21 2017-09-05 양지화학 주식회사 야누스 키나제 1 선택적 억제제 및 그 의약 용도
US10045981B2 (en) 2015-11-24 2018-08-14 Jakpharm, Llc Selective kinase inhibitors
CN105348287A (zh) * 2015-11-30 2016-02-24 宁波立华制药有限公司 一种枸橼酸托法替布的新型合成工艺
KR102565407B1 (ko) * 2016-01-04 2023-08-10 (주)아모레퍼시픽 극성 비양자성 용매를 이용한 n-[4-(1-아미노에틸)-페닐]-술폰아미드 유도체의 카이랄 분할 방법
US20190083609A1 (en) 2016-01-18 2019-03-21 Helmoltz Zentrum München - Deutsches Forschungszentrum Für Gesundheit And Umwelt (Gmbh) Tofacitinib as vaccination immune modulator
KR102329162B1 (ko) 2016-06-30 2021-11-22 주식회사 대웅제약 카이네이즈 저해제로서의 피라졸로피리미딘 유도체
CN106831538B (zh) * 2017-01-22 2019-06-25 苏州楚凯药业有限公司 托法替尼中间体的制备方法
KR102398659B1 (ko) 2017-03-17 2022-05-16 주식회사 대웅제약 카이네이즈 저해제로서의 피롤로트리아진 유도체
CN107602569A (zh) * 2017-10-23 2018-01-19 上海博悦生物科技有限公司 一种新型吡咯并[2,3‑d]嘧啶化合物及其合成方法和用途
KR102078805B1 (ko) 2017-11-30 2020-02-19 보령제약 주식회사 토파시티닙을 포함하는 약제학적 조성물
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
KR102577242B1 (ko) 2017-12-28 2023-09-11 주식회사 대웅제약 카이네이즈 저해제로서의 아미노-메틸피페리딘 유도체
KR102577241B1 (ko) 2017-12-28 2023-09-11 주식회사 대웅제약 카이네이즈 저해제로서의 아미노-플루오로피페리딘 유도체
PL3733673T3 (pl) 2017-12-28 2022-09-26 Daewoong Pharmaceutical Co., Ltd. Pochodna oksyfluoropiperydyny jako inhibitor kinazy
JP7393348B2 (ja) 2018-01-30 2023-12-06 インサイト・コーポレイション (1-(3-フルオロ-2(トリフルオロメチル)イソニコチニル)ピぺリジン―4-オン)を作製するためのプロセス及び中間体
US12161748B2 (en) 2018-01-31 2024-12-10 Twi Biotechnology, Inc. Topical formulations comprising tofacitinib
SG11202006782YA (en) * 2018-01-31 2020-08-28 Twi Pharmaceuticals Inc Topical formulations comprising tofacitinib
CN113768934A (zh) 2018-03-30 2021-12-10 因赛特公司 使用jak抑制剂治疗化脓性汗腺炎
KR102131107B1 (ko) 2019-01-15 2020-07-07 주식회사 다산제약 3-아미노-피페리딘 화합물의 신규한 제조 방법
NL2022471B1 (en) 2019-01-29 2020-08-18 Vationpharma B V Solid state forms of oclacitinib
US12364696B2 (en) 2019-02-27 2025-07-22 Jak Slave Pty Ltd Treatment of autoimmune disease
EP3938370A4 (en) 2019-03-13 2022-12-21 Intas Pharmaceuticals Ltd. PROCESS FOR THE PREPARATION OF TOFACITINIB AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
WO2020198583A1 (en) 2019-03-27 2020-10-01 Insilico Medicine Ip Limited Bicyclic jak inhibitors and uses thereof
US12227478B2 (en) 2019-04-05 2025-02-18 Yuhan Corporation Processes for preparing (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine or a salt thereof and processes for preparing tofacitinib using the same
AU2020378151A1 (en) 2019-11-08 2022-05-26 Cage Bio, Inc. Topical delivery of tofacitinib using ionic liquid
KR20220101150A (ko) 2019-11-14 2022-07-19 화이자 인코포레이티드 1-(((2s,3s,4s)-3-에틸-4-플루오로-5-옥소피롤리딘-2-일)메톡시)-7-메톡시이소퀴놀린-6-카복사마이드 조합물 및 경구 투여 형태
EP4067354B1 (en) 2019-11-25 2025-10-22 Daewoong Pharmaceutical Co., Ltd. Novel triazolopyridine derivative and pharmaceutical composition comprising same
CA3177852A1 (en) 2020-04-04 2021-10-07 Pfizer Inc. Methods of treating coronavirus disease 2019
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
EP4308568A1 (en) * 2021-03-15 2024-01-24 Chiesi Farmaceutici S.p.A. Heterocyclic derivatives as janus kinase inhibitors
CN113549075B (zh) * 2021-06-23 2025-09-23 合肥华方医药科技有限公司 一种枸橼酸托法替布非对映异构体杂质的合成方法
EP4180042A1 (en) 2021-11-15 2023-05-17 Sanovel Ilac Sanayi Ve Ticaret A.S. A film coated tablet comprising micronized tofacitinib

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NL8403224A (nl) 1984-10-24 1986-05-16 Oce Andeno Bv Dioxafosforinanen, de bereiding ervan en de toepassing voor het splitsen van optisch actieve verbindingen.
US6136595A (en) 1993-07-29 2000-10-24 St. Jude Children's Research Hospital Jak kinases and regulations of cytokine signal transduction
US5389509A (en) 1993-10-04 1995-02-14 Eastman Kodak Company Ultrathin high chloride tabular grain emulsions
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
DE59500788D1 (de) 1994-05-03 1997-11-20 Ciba Geigy Ag Pyrrolopyrimidinderivate mit antiproliferativer Wirkung
JPH07330732A (ja) * 1994-06-10 1995-12-19 Kyorin Pharmaceut Co Ltd 光学活性な3−アミノ−1−ベンジルピペリジン誘導体
US6136596A (en) * 1995-05-19 2000-10-24 University Of Massachusetts Cytokine-, stress-, and oncoprotein-activated human protein kinase kinases
EP0831829B1 (en) 1995-06-07 2003-08-20 Pfizer Inc. Heterocyclic ring-fused pyrimidine derivatives
DE69618959T2 (de) 1995-07-05 2002-08-29 E.I. Du Pont De Nemours And Co., Wilmington Pyrimidone und ihre verwendug als fungizide
EP0836605B1 (en) 1995-07-06 2002-02-06 Novartis AG Pyrrolopyrimidines and processes for the preparation thereof
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
JPH10512896A (ja) 1995-11-14 1998-12-08 フアルマシア・エ・アツプジヨン・エツセ・ピー・アー アリールおよびヘテロアリールプリン化合物
AU1441497A (en) 1996-01-23 1997-08-20 Novartis Ag Pyrrolopyrimidines and processes for their preparation
CH690773A5 (de) 1996-02-01 2001-01-15 Novartis Ag Pyrrolo(2,3-d)pyrimide und ihre Verwendung.
GB9604361D0 (en) 1996-02-29 1996-05-01 Pharmacia Spa 4-Substituted pyrrolopyrimidine compounds as tyrosine kinase inhibitors
AU1794697A (en) 1996-03-06 1997-09-22 Novartis Ag 7-alkyl-pyrrolo{2,3-d}pyrimidines
AU3176297A (en) 1996-06-25 1998-01-14 Novartis Ag Substituted 7-amino-pyrrolo{3,2-d}pyrimidines and the use thereof
EA199900021A1 (ru) 1996-07-13 1999-08-26 Глаксо, Груп Лимитед Бициклические гетероароматические соединения в качестве ингибиторов протеинтирозинкиназы
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
AU720429B2 (en) 1996-08-23 2000-06-01 Novartis Ag Substituted pyrrolopyrimidines and processes for their preparation
CA2272705C (en) 1996-11-27 2003-03-18 Pfizer Inc. Fused bicyclic pyrimidine derivatives
KR20000070751A (ko) 1997-02-05 2000-11-25 로즈 암스트롱, 크리스틴 에이. 트러트웨인 세포 증식 억제제로서의 피리도[2,3-d]피리미딘 및 4-아미노피리미딘
JP2001520748A (ja) 1997-03-24 2001-10-30 ファルマシア・アンド・アップジョン・カンパニー Jak2/サイトカイン受容体結合の阻害剤を同定する方法
CA2326383A1 (en) 1998-04-02 1999-10-14 Neurogen Corporation Aminoalkyl substituted pyrrolo[2,3-b]pyridine and pyrrolo[2,3-d]pyrimidine derivatives: modulators of crf1 receptors
AU4317399A (en) 1998-05-28 1999-12-13 Parker Hughes Institute Quinazolines for treating brain tumor
PA8474101A1 (es) * 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
PL198640B1 (pl) * 1998-06-19 2008-07-31 Pfizer Prod Inc Związki pirolo[2,3-d]pirymidynowe, środek farmaceutyczny i zastosowanie tych związków
EP1091739A1 (en) 1998-06-30 2001-04-18 Parker Hughes Institute Method for inhibiting c-jun expression using jak-3 inhibitors
EP1105378B1 (en) 1998-08-21 2005-03-30 Parker Hughes Institute Quinazoline derivatives
US6080747A (en) 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
EA006227B1 (ru) * 1999-12-10 2005-10-27 Пфайзер Продактс Инк. СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА
EA006153B1 (ru) * 2000-06-26 2005-10-27 Пфайзер Продактс Инк. СОЕДИНЕНИЯ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ИММУНОДЕПРЕССАНТОВ
PY0228255A (es) * 2001-12-06 2004-06-01 Pfizer Prod Inc Compuestos cristalinos novedosos
MXPA06015237A (es) * 2004-06-29 2007-12-10 Amgen Inc Pirrolo[2-3-d]pirimidinas que modulan la actividad de ack1 y lck.

Also Published As

Publication number Publication date
EA200301193A1 (ru) 2004-04-29
BG108389A (bg) 2005-01-31
EE200300594A (et) 2004-04-15
BG66489B1 (bg) 2015-05-29
CA2448281A1 (en) 2002-12-05
AU2008203170A1 (en) 2008-08-07
JP4381137B2 (ja) 2009-12-09
CN1729192A (zh) 2006-02-01
ES2393385T3 (es) 2012-12-20
CY1113322T1 (el) 2016-06-22
EP1666481A2 (en) 2006-06-07
IS3023B (is) 2020-08-15
EA200600575A1 (ru) 2006-08-25
WO2002096909A1 (en) 2002-12-05
KR100868814B1 (ko) 2008-11-14
JP2004534047A (ja) 2004-11-11
NL300887I2 (nl) 2017-08-31
UA80093C2 (uk) 2007-08-27
PL367945A1 (en) 2005-03-07
HRP20030943B1 (hr) 2011-11-30
BR0209246A (pt) 2004-06-15
OA12612A (en) 2006-06-09
CY2017028I2 (el) 2018-02-14
NO20035201L (no) 2003-11-24
GT200200100A (es) 2003-02-11
CL2008000762A1 (es) 2008-07-04
KR100926875B1 (ko) 2009-11-16
LUC00031I1 (cs) 2017-08-10
CU23337B7 (es) 2009-01-20
UY27317A1 (es) 2003-02-28
KR20040003037A (ko) 2004-01-07
ATE519741T1 (de) 2011-08-15
CR10177A (es) 2008-08-19
PL409305A1 (pl) 2014-12-22
SI1666481T1 (sl) 2012-11-30
GEP20063784B (en) 2006-04-10
HUS1900008I1 (hu) 2020-02-28
KR20080083028A (ko) 2008-09-12
KR20060133117A (ko) 2006-12-22
US7301023B2 (en) 2007-11-27
PL228155B1 (pl) 2018-02-28
YU92303A (sh) 2006-08-17
RS52144B (sr) 2012-08-31
LUC00031I2 (cs) 2017-10-11
FR17C1031I1 (fr) 2017-10-13
LTPA2017025I1 (lt) 2017-09-11
NZ540332A (en) 2007-05-31
BE2017C032I2 (cs) 2021-07-19
US7432370B2 (en) 2008-10-07
HUP0400152A3 (en) 2012-12-28
KR100869409B1 (ko) 2008-11-21
PE20030561A1 (es) 2003-06-23
HU230876B1 (hu) 2018-11-29
TWI310384B (en) 2009-06-01
CY2017028I1 (el) 2018-02-14
EP1666481B9 (en) 2013-05-01
DK1666481T3 (da) 2012-10-15
GT200200100AA (es) 2007-07-06
ES2369226T3 (es) 2011-11-28
FR17C1031I2 (fr) 2018-11-02
IL158588A0 (en) 2004-05-12
NO2017047I1 (no) 2017-09-08
AR037321A1 (es) 2004-11-03
SK288199B6 (sk) 2014-06-03
EP1666481B1 (en) 2012-09-19
AU2002304401C1 (en) 2009-03-05
MXPA03011062A (es) 2004-03-19
IS6993A (is) 2003-10-13
CZ304366B6 (cs) 2014-04-02
AU2002304401B2 (en) 2008-04-17
EA012666B1 (ru) 2009-12-30
NO20093135L (no) 2003-11-24
US20040229923A1 (en) 2004-11-18
EP1609781A1 (en) 2005-12-28
ZA200307982B (en) 2004-10-14
HUP0400152A2 (en) 2007-07-30
NZ530380A (en) 2005-08-26
TW200413370A (en) 2004-08-01
AU2008203170B2 (en) 2009-06-18
MA27029A1 (fr) 2004-12-20
AP2002002550A0 (en) 2002-06-30
AR045680A2 (es) 2005-11-09
EA007251B1 (ru) 2006-08-25
AP1859A (en) 2008-07-02
MY129649A (en) 2007-04-30
EP1392694A1 (en) 2004-03-03
NO20035201D0 (no) 2003-11-24
HRP20030943A2 (en) 2005-08-31
TWI316061B (en) 2009-10-21
CZ20033260A3 (en) 2004-03-17
SK288192B6 (sk) 2014-06-03
EP1609781B1 (en) 2011-08-10
TNSN03128A1 (fr) 2005-12-23
KR20060014459A (ko) 2006-02-15
CA2448281C (en) 2009-05-05
ECSP034865A (es) 2004-01-28
EE05332B1 (et) 2010-08-16
KR20080002931A (ko) 2008-01-04
EP1666481A3 (en) 2006-11-29
PA8546301A1 (es) 2003-05-14
SK14652003A3 (sk) 2004-05-04
PT1666481E (pt) 2012-12-03
LTC1666481I2 (lt) 2018-06-25
US20030073719A1 (en) 2003-04-17

Similar Documents

Publication Publication Date Title
KR100869409B1 (ko) (1-벤질-4-메틸피페리딘-3-일)-메틸아민의 광학 분할, 및단백질 키나아제 억제제로서의 피롤로 2,3-피리미딘유도체의 제조를 위한 이들의 용도
US6965027B2 (en) Crystalline 3-{4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile citrate
SK7562002A3 (en) Pyrrolo[2,3-d]pyrimidine compounds
AU2002304401A1 (en) Optical resolution of (1-benzyl-4-methylpiperidin-3-yl) -methylamine and the use thereof for the preparation of pyrrolo 2,3-pyrimidine derivatives as protein kinases inhibitors

Legal Events

Date Code Title Description
SPCF Filing of supplementary protection certificate

Free format text: PRODUCT NAME: TOFACITINIB, EVENTUELT I FORM AV ET FARMASOEYTISK AKSEPTABELT SALT; REG. NO/DATE: EU/1/17/1178 20170322

Spc suppl protection certif: 2017047

Filing date: 20170908

SPCG Granted supplementary protection certificate

Free format text: PRODUCT NAME: TOFACITINIB, EVENTUELT I FORM AV ET FARMASOEYTISK AKSEPTABELT SALT; REG. NO/DATE: EU/1/17/1178 20170322

Spc suppl protection certif: 2017047

Filing date: 20170908

Extension date: 20270529

MK1K Patent expired