ATE519741T1 - Racemattrennung von (1-benzyl-4-methylpiperidin-3-yl)-methylamin - Google Patents

Racemattrennung von (1-benzyl-4-methylpiperidin-3-yl)-methylamin

Info

Publication number
ATE519741T1
ATE519741T1 AT05015461T AT05015461T ATE519741T1 AT E519741 T1 ATE519741 T1 AT E519741T1 AT 05015461 T AT05015461 T AT 05015461T AT 05015461 T AT05015461 T AT 05015461T AT E519741 T1 ATE519741 T1 AT E519741T1
Authority
AT
Austria
Prior art keywords
racemat
methylpiperidine
methylamine
benzyl
separation
Prior art date
Application number
AT05015461T
Other languages
German (de)
English (en)
Inventor
Glenn Ernest Wilcox
Christian Koecher
Ton Vries
Mark Edwards Flanagan
Michael John Munchhof
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=ATE519741(T1) "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
Application granted granted Critical
Publication of ATE519741T1 publication Critical patent/ATE519741T1/de

Links

Classifications

    • 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
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic 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
    • C07D211/36—Heterocyclic 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
    • C07D211/56—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Emergency Medicine (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (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)
AT05015461T 2001-05-31 2002-05-29 Racemattrennung von (1-benzyl-4-methylpiperidin-3-yl)-methylamin ATE519741T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US29477501P 2001-05-31 2001-05-31
US34104801P 2001-12-06 2001-12-06

Publications (1)

Publication Number Publication Date
ATE519741T1 true ATE519741T1 (de) 2011-08-15

Family

ID=26968730

Family Applications (1)

Application Number Title Priority Date Filing Date
AT05015461T ATE519741T1 (de) 2001-05-31 2002-05-29 Racemattrennung von (1-benzyl-4-methylpiperidin-3-yl)-methylamin

Country Status (52)

Country Link
US (2) US7301023B2 (index.php)
EP (3) EP1666481B9 (index.php)
JP (1) JP4381137B2 (index.php)
KR (5) KR100926875B1 (index.php)
CN (1) CN1729192A (index.php)
AP (1) AP1859A (index.php)
AR (2) AR037321A1 (index.php)
AT (1) ATE519741T1 (index.php)
AU (2) AU2002304401C1 (index.php)
BE (1) BE2017C032I2 (index.php)
BG (1) BG66489B1 (index.php)
BR (1) BR0209246A (index.php)
CA (1) CA2448281C (index.php)
CL (1) CL2008000762A1 (index.php)
CR (1) CR10177A (index.php)
CU (1) CU23337B7 (index.php)
CY (2) CY1113322T1 (index.php)
CZ (1) CZ304366B6 (index.php)
DK (1) DK1666481T3 (index.php)
EA (2) EA007251B1 (index.php)
EC (1) ECSP034865A (index.php)
EE (1) EE05332B1 (index.php)
ES (2) ES2369226T3 (index.php)
FR (1) FR17C1031I2 (index.php)
GE (1) GEP20063784B (index.php)
GT (2) GT200200100AA (index.php)
HR (1) HRP20030943B1 (index.php)
HU (2) HU230876B1 (index.php)
IL (1) IL158588A0 (index.php)
IS (1) IS3023B (index.php)
LT (1) LTC1666481I2 (index.php)
LU (1) LUC00031I2 (index.php)
MA (1) MA27029A1 (index.php)
MX (1) MXPA03011062A (index.php)
MY (1) MY129649A (index.php)
NL (1) NL300887I2 (index.php)
NO (3) NO328578B1 (index.php)
NZ (2) NZ530380A (index.php)
OA (1) OA12612A (index.php)
PA (1) PA8546301A1 (index.php)
PE (1) PE20030561A1 (index.php)
PL (2) PL367945A1 (index.php)
PT (1) PT1666481E (index.php)
RS (1) RS52144B (index.php)
SI (1) SI1666481T1 (index.php)
SK (2) SK288192B6 (index.php)
TN (1) TNSN03128A1 (index.php)
TW (2) TWI316061B (index.php)
UA (1) UA80093C2 (index.php)
UY (1) UY27317A1 (index.php)
WO (1) WO2002096909A1 (index.php)
ZA (1) ZA200307982B (index.php)

Families Citing this family (123)

* 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
SK287188B6 (sk) 1999-12-10 2010-02-08 Pfizer Products Inc. Pyrolo [2,3-d]pyrimidínová zlúčenina, jej použitie a farmaceutická kompozícia alebo kombinácia s jej obsahom
JP4068958B2 (ja) * 2000-06-26 2008-03-26 ファイザー・プロダクツ・インク 免疫抑制剤としてのピロロ（２，３−ｄ）ピリミジン化合物
GT200200234A (es) 2001-12-06 2003-06-27 Compuestos cristalinos novedosos
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
MXPA05001096A (es) 2002-07-29 2005-11-23 Rigel Pharmaceuticals Inc Metodos para tratamiento o prevencion de enfermedades autoinmunes con compuestos de 2,4-diamino-pirimidina.
EP1531817B1 (en) * 2002-08-27 2008-07-30 MERCK PATENT GmbH Glycinamide derivatives as raf-kinase inhibitors
WO2004047843A1 (en) 2002-11-26 2004-06-10 Pfizer Products Inc. Method of treatment of transplant rejection
DK1656372T3 (da) 2003-07-30 2013-07-01 Rigel Pharmaceuticals Inc 2,4-pyrimidindiaminforbindelser til anvendelse til behandling eller forebyggelse af autoimmunsygdomme
EP1755680A1 (en) * 2004-05-03 2007-02-28 Novartis AG Combinations comprising a s1p receptor agonist and a jak3 kinase inhibitor
AU2005260032A1 (en) 2004-06-29 2006-01-12 Amgen Inc. Pyrrolo[2,3-d]pyrimidines that modulate ACK1 and LCK activity
CA2575808A1 (en) 2004-08-02 2006-02-16 Osi Pharmaceuticals, Inc. Aryl-amino substituted pyrrolopyrimidine multi-kinase inhibiting compounds
WO2006056399A2 (en) * 2004-11-24 2006-06-01 Novartis Ag Combinations of jak inhibitors and at least one of bcr-abl, flt-3, fak or raf kinase inhibitors
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
CA2615291A1 (en) 2005-07-14 2007-01-18 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
EP2251341A1 (en) 2005-07-14 2010-11-17 Astellas Pharma Inc. Heterocyclic Janus kinase 3 inhibitors
PT1913000E (pt) 2005-07-29 2012-02-28 Pfizer Prod Inc Derivados de pirrolo[2,3-d]pirimidina, suas substâncias intermédias e processo de síntese
US20070149506A1 (en) 2005-09-22 2007-06-28 Arvanitis Argyrios G Azepine inhibitors of Janus kinases
SI1966202T1 (sl) 2005-12-13 2012-01-31 Incyte Corp S heteroarilom substituirani pirolo (2,3-b)piridini in pirolo (2,3-b)pirimidini kot zaviralci janus kinaze
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
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.
EP4606378A3 (en) 2007-06-13 2025-11-05 Incyte Holdings Corporation Salts of the janus kinase inhibitor (r)-3-( 4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3- cyclopentylprop anenitrile
BRPI0813553A2 (pt) * 2007-07-11 2017-05-09 Pfizer composições farmacêuticas e métodos para tratamento de distúrbios do olho seco
PT2265607T (pt) 2008-02-15 2017-03-08 Rigel Pharmaceuticals Inc Compostos de pirimidina-2-amina e sua utilização como inibidores de jak cinases
SG191660A1 (en) 2008-03-11 2013-07-31 Incyte Corp Azetidine and cyclobutane derivatives as jak inhibitors
ES2546502T3 (es) 2008-04-16 2015-09-24 Portola Pharmaceuticals, Inc. 2,6-Diamino-pirimidin-5-il-carboxamidas como inhibidores de syk o JAK quinasas
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
AU2009238590A1 (en) 2008-04-22 2009-10-29 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
MX2011001259A (es) * 2008-08-01 2011-03-15 Biocryst Pharm Inc Derivados de piperidina como inhibidores jak3.
ES2467109T3 (es) 2008-08-20 2014-06-11 Zoetis Llc Compuestos de pirrolo[2,3-d]pirimidina
EP2396004A4 (en) * 2009-02-11 2012-07-25 Reaction Biology Corp SELECTIVE KINASE HEMMER
ES2552805T3 (es) 2009-04-20 2015-12-02 Auspex Pharmaceuticals, Llc Inhibidores piperidínicos de la cinasa Janus 3
UA106078C2 (uk) 2009-05-22 2014-07-25 Інсайт Корпорейшн 3-[4-(7H-ПІРОЛО[2,3-d]ПІРИМІДИН-4-ІЛ)-1H-ПІРАЗОЛ-1-ІЛ]ОКТАН- АБО ГЕПТАННІТРИЛ ЯК JAK-ІНГІБІТОРИ
AU2010249380B2 (en) 2009-05-22 2015-08-20 Incyte Holdings Corporation 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
BR112012005382A2 (pt) * 2009-09-10 2016-03-29 Hoffmann La Roche inibidores de jak
CN105541847B (zh) 2009-10-09 2019-08-16 因西特控股公司 3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的羟基衍生物、酮基衍生物和葡糖苷酸衍生物
MX2012004379A (es) 2009-10-15 2012-06-01 Pfizer Compuestos de pirrolo[2,3-d]pirimidina.
EP2513114B1 (en) 2009-12-18 2014-04-02 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine compounds
CN102712640A (zh) * 2010-01-12 2012-10-03 弗·哈夫曼-拉罗切有限公司 三环杂环化合物、其组合物和应用方法
WO2011097087A1 (en) 2010-02-05 2011-08-11 Pfizer Inc. Pyrrolo [ 2, 3 - d] pyrimidine urea compounds as jak inhibitors
SI2545045T1 (sl) 2010-03-10 2016-05-31 Incyte Holdings Corporation Derivati piperidin-4-ila kot zaviralci JAK1
MX338228B (es) 2010-05-21 2016-04-08 Incyte Corp Formulacion topica para inhibidor de cinasas janus (jak).
US9102625B2 (en) 2010-11-01 2015-08-11 Portola Pharmaceuticals, Inc. Nicotinamides as JAK kinase modulators
US8933085B2 (en) 2010-11-19 2015-01-13 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
US9034884B2 (en) 2010-11-19 2015-05-19 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
PT2675451E (pt) 2011-02-18 2015-10-16 Incyte Corp Terapia de combinação com inibidores mtor/jak
EP2691395B1 (en) 2011-03-28 2017-08-30 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
WO2012177606A1 (en) 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors
US9358229B2 (en) 2011-08-10 2016-06-07 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
CA2856301C (en) 2011-11-23 2020-10-06 Portola Pharmaceuticals, Inc. Pyrazine kinase inhibitors
CN107898790B (zh) 2011-11-30 2024-06-21 埃默里大学 用于治疗或预防逆转录病毒和其它病毒感染的抗病毒jak抑制剂
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
US9193733B2 (en) 2012-05-18 2015-11-24 Incyte Holdings Corporation Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
WO2014016338A1 (en) 2012-07-25 2014-01-30 Lek Pharmaceuticals D.D. New synthetic route for the preparation of 3-amino-piperidine compounds
US9676756B2 (en) 2012-10-08 2017-06-13 Portola Pharmaceuticals, Inc. Substituted pyrimidinyl kinase inhibitors
IL297429A (en) 2012-11-15 2022-12-01 Incyte Holdings Corp Sustained release dosage forms of roxolitinib
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
EP2935216B1 (en) 2012-12-17 2018-06-27 Sun Pharmaceutical Industries Limited Process for the preparation of tofacitinib and intermediates thereof
EP2938616A4 (en) 2012-12-28 2016-06-15 Glenmark Pharmaceuticals Ltd PROCESSING METHOD FOR THE PRODUCTION OF TOFACITINIB AND INTERMEDIATE PRODUCTS THEREOF
SI2958921T1 (sl) 2013-02-22 2017-12-29 Pfizer Inc. Derivati pirolo(2,3-d)pirimidina kot inhibitorji Janus kinaz (JAK)
PT3489239T (pt) 2013-03-06 2021-12-17 Incyte Holdings Corp Processos e intermediários para a preparação de um inibidor 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
CN114010611B (zh) 2013-08-07 2023-11-28 因赛特控股公司 Jak1抑制剂的持续释放剂型
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
EP3318565B1 (en) 2013-12-05 2021-04-14 Pfizer Inc. Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides
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.
US9260438B2 (en) 2014-02-06 2016-02-16 Apotex Inc. 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
JP6585158B2 (ja) 2014-08-12 2019-10-02 ファイザー・インク ヤヌスキナーゼの阻害に有用なピロロ［２，３−ｄ］ピリミジン誘導体
CN108349977B (zh) * 2015-01-20 2021-05-25 无锡福祈制药有限公司 Jak抑制剂
EP3162793B1 (en) * 2015-02-17 2019-04-10 Amorepacific Corporation Chiral resolution method of n-[4-(1-aminoethyl)-phenyl]-sulfonamide derivatives
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
WO2016173484A1 (zh) 2015-04-29 2016-11-03 南京明德新药研发股份有限公司 Jak抑制剂
US10703756B2 (en) 2015-05-01 2020-07-07 Pfizer Inc. Pyrrolo[2,3-D]pyrimidinyl, pyrrolo[2,3-B]pyrazinyl, pyrrolo[2,3-B]pyridinyl acrylamides and epoxides thereof
MX381994B (es) 2015-05-29 2025-03-13 Wuxi Fortune Pharmaceutical Co Ltd Inhibidor de janus quinasa.
US10034882B2 (en) * 2015-07-27 2018-07-31 Unichem Laboratories Limited Tofacitinib orally disintegrating tablets
KR101771219B1 (ko) * 2015-08-21 2017-09-05 양지화학 주식회사 야누스 키나제 1 선택적 억제제 및 그 의약 용도
WO2017091681A1 (en) 2015-11-24 2017-06-01 Aclaris Therapeutics, Inc. 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
WO2017125417A1 (en) 2016-01-18 2017-07-27 Helmholtz Zentrum München - Deutsches Forschungszentrum für Gesundheit und Umwelt (GmbH) Tofacitinib as vaccination immune modulator
AU2017287762C1 (en) 2016-06-30 2020-04-23 Daewoong Pharmaceutical Co., Ltd. Pyrazolopyrimidine derivatives as kinase inhibitor
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
WO2019132562A1 (ko) 2017-12-28 2019-07-04 주식회사 대웅제약 카이네이즈 저해제로서의 옥시-플루오로피페리딘 유도체
KR102577241B1 (ko) 2017-12-28 2023-09-11 주식회사 대웅제약 카이네이즈 저해제로서의 아미노-플루오로피페리딘 유도체
UA127488C2 (uk) 2018-01-30 2023-09-06 Інсайт Корпорейшн Способи одержання (1-(3-фтор-2-(трифторметил)ізонікотиноїл)піперидин-4-ону)
US12161748B2 (en) 2018-01-31 2024-12-10 Twi Biotechnology, Inc. Topical formulations comprising tofacitinib
WO2019152232A1 (en) * 2018-01-31 2019-08-08 Twi Pharmaceuticals, Inc. Topical formulations comprising tofacitinib
PT3773593T (pt) 2018-03-30 2024-06-25 Incyte Corp Tratamento da hidradenite supurativa com inibidores de jak
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
US12269830B2 (en) 2019-03-13 2025-04-08 Intas Pharmaceuticals Ltd. Process for preparation of tofacitinib and pharmaceutically acceptable salt thereof
CN113993585B (zh) 2019-03-27 2024-10-01 英矽智能科技知识产权有限公司 双环jak抑制剂及其用途
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
BR112022007826A2 (pt) 2019-11-14 2022-07-05 Pfizer Combinações de 1-(((2s,3s,4s)-3-etil-4-fluoro-5-oxopirrolidin-2-il)metóxi)-7-metóxi-isoquino¬lina-6-carboxamida e formas de dosagem oral
US20220389010A1 (en) * 2019-11-25 2022-12-08 Daewoong Pharmaceutical Co., Ltd. Novel Triazolopyridine Derivatives and Pharmaceutical Composition Comprising Same
EP4125900A1 (en) 2020-04-04 2023-02-08 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
ATE159257T1 (de) 1994-05-03 1997-11-15 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
CA2223081C (en) 1995-06-07 2001-03-06 Pfizer Inc. Heterocyclic ring-fused pyrimidine derivatives
WO1997002262A1 (en) 1995-07-05 1997-01-23 E.I. Du Pont De Nemours And Company Fungicidal pyrimidinones
WO1997002266A1 (en) 1995-07-06 1997-01-23 Novartis Ag Pyrrolopyrimidines and processes for the preparation thereof
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
DE69613211T2 (de) 1995-11-14 2001-11-15 Pharmacia & Upjohn S.P.A., Mailand/Milano Aryl- und heteroaryl- purin- und pyridopyrimidin- derivate
ES2177925T3 (es) 1996-01-23 2002-12-16 Novartis Ag Pirrolopirimidinas y procedimientos para su preparacion.
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
WO1997032879A1 (de) 1996-03-06 1997-09-12 Novartis Ag 7-ALKYL-PYRROLO[2,3-d]PYRIMIDINE
WO1997049706A1 (en) 1996-06-25 1997-12-31 Novartis Ag SUBSTITUTED 7-AMINO-PYRROLO[3,2-d]PYRIMIDINES AND THE USE THEREOF
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
AU3693697A (en) 1996-07-13 1998-02-09 Glaxo Group Limited Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors
DK0938486T3 (da) 1996-08-23 2008-07-07 Novartis Ag Substituerede pyrrolopyrimidiner og fremgangsmåder til deres fremstilling
CN1237177A (zh) 1996-11-27 1999-12-01 辉瑞大药厂 稠合的二环嘧啶衍生物
WO1998033798A2 (en) 1997-02-05 1998-08-06 Warner Lambert Company Pyrido[2,3-d]pyrimidines and 4-amino-pyrimidines as inhibitors of cell proliferation
WO1998043087A1 (en) 1997-03-24 1998-10-01 Pharmacia & Upjohn Company Method for identifying inhibitors of jak2/cytokine receptor binding
JP2002510687A (ja) 1998-04-02 2002-04-09 ニューロゲン コーポレイション アミノアルキル置換ピロロ［２，３−ｂ］ピリジンおよびピロロ［２，３−ｄ］ピリミジン誘導体：ｃｒｆ１レセプタのモジュレータ
JP2002516823A (ja) 1998-05-28 2002-06-11 パーカー ヒューズ インスティテュート 脳腫瘍の治療のためのキナゾリン
DE69916833T2 (de) 1998-06-19 2005-04-14 Pfizer Products Inc., Groton Pyrrolo(2,3-d)pyrimidin-verbindungen
PA8474101A1 (es) * 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
JP2004504259A (ja) 1998-06-30 2004-02-12 パーカー　ヒューズ　インスティテュート Ｊａｋ−３インヒビターを用いたｃ−ｊｕｎ発現の阻害方法
DE69924500T2 (de) 1998-08-21 2006-02-09 Parker Hughes Institute, St. Paul Chinazolinderivate
US6080747A (en) 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
SK287188B6 (sk) * 1999-12-10 2010-02-08 Pfizer Products Inc. Pyrolo [2,3-d]pyrimidínová zlúčenina, jej použitie a farmaceutická kompozícia alebo kombinácia s jej obsahom
JP4068958B2 (ja) * 2000-06-26 2008-03-26 ファイザー・プロダクツ・インク 免疫抑制剤としてのピロロ（２，３−ｄ）ピリミジン化合物
GT200200234A (es) * 2001-12-06 2003-06-27 Compuestos cristalinos novedosos
AU2005260032A1 (en) * 2004-06-29 2006-01-12 Amgen Inc. Pyrrolo[2,3-d]pyrimidines that modulate ACK1 and LCK activity

Also Published As

Publication number Publication date
EP1666481B9 (en) 2013-05-01
CA2448281C (en) 2009-05-05
GT200200100AA (es) 2007-07-06
HRP20030943A2 (en) 2005-08-31
NZ530380A (en) 2005-08-26
FR17C1031I1 (fr) 2017-10-13
EA200301193A1 (ru) 2004-04-29
OA12612A (en) 2006-06-09
PE20030561A1 (es) 2003-06-23
FR17C1031I2 (fr) 2018-11-02
KR100869409B1 (ko) 2008-11-21
AU2002304401B2 (en) 2008-04-17
DK1666481T3 (da) 2012-10-15
AU2008203170A1 (en) 2008-08-07
EP1609781B1 (en) 2011-08-10
CU23337B7 (es) 2009-01-20
EP1392694A1 (en) 2004-03-03
TWI310384B (en) 2009-06-01
ES2393385T3 (es) 2012-12-20
CY2017028I1 (el) 2018-02-14
HRP20030943B1 (hr) 2011-11-30
CY2017028I2 (el) 2018-02-14
MY129649A (en) 2007-04-30
PL228155B1 (pl) 2018-02-28
KR20060133117A (ko) 2006-12-22
KR20040003037A (ko) 2004-01-07
US7432370B2 (en) 2008-10-07
KR100868814B1 (ko) 2008-11-14
NO328578B1 (no) 2010-03-22
ZA200307982B (en) 2004-10-14
EA200600575A1 (ru) 2006-08-25
JP4381137B2 (ja) 2009-12-09
HUS1900008I1 (hu) 2020-02-28
US7301023B2 (en) 2007-11-27
EP1666481A3 (en) 2006-11-29
US20040229923A1 (en) 2004-11-18
BG66489B1 (bg) 2015-05-29
LUC00031I1 (index.php) 2017-08-10
CZ20033260A3 (en) 2004-03-17
EP1609781A1 (en) 2005-12-28
KR20080002931A (ko) 2008-01-04
TW200413370A (en) 2004-08-01
NL300887I2 (nl) 2017-08-31
PT1666481E (pt) 2012-12-03
CN1729192A (zh) 2006-02-01
NO2017047I1 (no) 2017-09-08
MA27029A1 (fr) 2004-12-20
EE05332B1 (et) 2010-08-16
AR037321A1 (es) 2004-11-03
EP1666481A2 (en) 2006-06-07
EP1666481B1 (en) 2012-09-19
NZ540332A (en) 2007-05-31
US20030073719A1 (en) 2003-04-17
HUP0400152A2 (en) 2007-07-30
SK288192B6 (sk) 2014-06-03
HUP0400152A3 (en) 2012-12-28
AU2002304401C1 (en) 2009-03-05
CA2448281A1 (en) 2002-12-05
IS3023B (is) 2020-08-15
WO2002096909A1 (en) 2002-12-05
SI1666481T1 (sl) 2012-11-30
CZ304366B6 (cs) 2014-04-02
MXPA03011062A (es) 2004-03-19
NO20035201L (no) 2003-11-24
TWI316061B (en) 2009-10-21
LUC00031I2 (index.php) 2017-10-11
CR10177A (es) 2008-08-19
AU2008203170B2 (en) 2009-06-18
IL158588A0 (en) 2004-05-12
PA8546301A1 (es) 2003-05-14
IS6993A (is) 2003-10-13
YU92303A (sh) 2006-08-17
BG108389A (bg) 2005-01-31
SK14652003A3 (sk) 2004-05-04
GEP20063784B (en) 2006-04-10
NO20093135L (no) 2003-11-24
UA80093C2 (uk) 2007-08-27
KR20080083028A (ko) 2008-09-12
SK288199B6 (sk) 2014-06-03
PL367945A1 (en) 2005-03-07
EA007251B1 (ru) 2006-08-25
JP2004534047A (ja) 2004-11-11
UY27317A1 (es) 2003-02-28
HU230876B1 (hu) 2018-11-29
PL409305A1 (pl) 2014-12-22
LTC1666481I2 (lt) 2018-06-25
LTPA2017025I1 (lt) 2017-09-11
ECSP034865A (es) 2004-01-28
RS52144B (sr) 2012-08-31
EE200300594A (et) 2004-04-15
ES2369226T3 (es) 2011-11-28
KR20060014459A (ko) 2006-02-15
AP1859A (en) 2008-07-02
CY1113322T1 (el) 2016-06-22
NO20035201D0 (no) 2003-11-24
AP2002002550A0 (en) 2002-06-30
AR045680A2 (es) 2005-11-09
EA012666B1 (ru) 2009-12-30
CL2008000762A1 (es) 2008-07-04
KR100926875B1 (ko) 2009-11-16
TNSN03128A1 (fr) 2005-12-23
BR0209246A (pt) 2004-06-15
GT200200100A (es) 2003-02-11
BE2017C032I2 (index.php) 2021-07-19

Similar Documents

Publication Publication Date Title
ATE519741T1 (de) Racemattrennung von (1-benzyl-4-methylpiperidin-3-yl)-methylamin
ATA5552001A (de) Verbindung von plattenförmigen bauteilen
DE60211601D1 (de) Bereitstellung von positionsabhängigen Inhalten
EP1294513A4 (en) COVALENT BIOCONJUGATION, RESTRICTION, PROTEINS
FI20010977L (fi) Kromatografinen erotusmenetelmä
DK1360169T3 (da) Succinatsalt af O-desmethyl-venlafaxin
DE60236581D1 (de) Ng von mosaikeffekten
DE02784674T1 (de) Quantifizierung von polypeptiden
DE50212455D1 (de) Verwendung von Dimerdiolen
NO20042742L (no) Pyrimidinforbindelser
NO20020741D0 (no) Separatoranordning
DE60210864D1 (de) Modifiziertes fluoreszentes Protein
DE60126814D1 (de) Inhalation von stickoxid
DE60239357D1 (de) Entsorgung von fluoroform (hfc-23)
DE60215133D1 (de) Abscheidung von löslichen materialien
DE60227828D1 (de) E von schmelzkleber
DE60007360D1 (de) Amorphe modifikation von torasemid
NO20022722D0 (no) Pseudo-offset migrering
EP1366056A4 (en) PREPARATION OF DESOXYNUCLEOSIDES
DE60208437D1 (de) Trennmodul
EP1284989A4 (en) Separation of avian antibodies
FI20010286L (fi) Erotuslaite
ATE326465T1 (de) Racematspaltung von trans 7-
DE60233601D1 (de) Verwendung von bestimmten Cyclolignanen
ATA1152001A (de) Zentrifugalkraft-windsichter

Legal Events

Date Code Title Description
RER Ceased as to paragraph 5 lit. 3 law introducing patent treaties