CA2469350A1 - 3-{4-methyl-3[methyl-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile mono citrate salt - Google Patents

3-{4-methyl-3[methyl-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile mono citrate salt Download PDF

Info

Publication number
CA2469350A1
CA2469350A1 CA002469350A CA2469350A CA2469350A1 CA 2469350 A1 CA2469350 A1 CA 2469350A1 CA 002469350 A CA002469350 A CA 002469350A CA 2469350 A CA2469350 A CA 2469350A CA 2469350 A1 CA2469350 A1 CA 2469350A1
Authority
CA
Canada
Prior art keywords
methyl
pyrrolo
pyrimidin
piperidin
oxo
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
CA002469350A
Other languages
French (fr)
Other versions
CA2469350C (en
Inventor
Mark Edward Flanagan
Zheng Jane Li
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Pfizer Products Inc
Original Assignee
Individual
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=23326961&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2469350(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Individual filed Critical Individual
Publication of CA2469350A1 publication Critical patent/CA2469350A1/en
Application granted granted Critical
Publication of CA2469350C publication Critical patent/CA2469350C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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
    • 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
    • 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
    • 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

Abstract

This invention relates to a novel amorphous and crystallline forms of 3-{(3R,4R)-4-methyl-3-[methyl-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile mono citrate salt, useful as inhibitors of protein kinases, and to their methods of preparation.
CA002469350A 2001-12-06 2002-11-25 3-{4-methyl-3[methyl-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile mono citrate salt Expired - Lifetime CA2469350C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US33898401P 2001-12-06 2001-12-06
US60/338,984 2001-12-06
PCT/IB2002/004948 WO2003048162A1 (en) 2001-12-06 2002-11-25 Novel crystalline compound

Publications (2)

Publication Number Publication Date
CA2469350A1 true CA2469350A1 (en) 2003-06-12
CA2469350C CA2469350C (en) 2009-09-29

Family

ID=23326961

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002469350A Expired - Lifetime CA2469350C (en) 2001-12-06 2002-11-25 3-{4-methyl-3[methyl-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile mono citrate salt

Country Status (30)

Country Link
US (2) US6965027B2 (en)
EP (1) EP1451192B1 (en)
JP (1) JP4201135B2 (en)
KR (1) KR100691590B1 (en)
CN (1) CN1325498C (en)
AR (1) AR037635A1 (en)
AT (1) ATE497962T1 (en)
AU (1) AU2002348857B2 (en)
BR (1) BR0214761A (en)
CA (1) CA2469350C (en)
CO (1) CO5580780A2 (en)
CY (1) CY1111311T1 (en)
DE (1) DE60239146D1 (en)
DK (1) DK1451192T3 (en)
ES (1) ES2357942T3 (en)
GT (1) GT200200234A (en)
HK (1) HK1070653A1 (en)
HN (1) HN2002000349A (en)
IL (1) IL161914A0 (en)
MX (1) MXPA04005401A (en)
NO (1) NO20042721L (en)
NZ (1) NZ532366A (en)
PA (1) PA8560201A1 (en)
PE (1) PE20030807A1 (en)
PL (1) PL221493B1 (en)
RU (1) RU2315052C2 (en)
TW (1) TW200300690A (en)
UY (1) UY27567A1 (en)
WO (1) WO2003048162A1 (en)
ZA (1) ZA200404270B (en)

Families Citing this family (99)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PA8474101A1 (en) * 1998-06-19 2000-09-29 Pfizer Prod Inc PYROLEUM [2,3-D] PIRIMIDINE COMPOUNDS
CA2393640C (en) * 1999-12-10 2006-09-05 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidine compounds
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
GT200200234A (en) * 2001-12-06 2003-06-27 NEW CRYSTAL COMPOUNDS
TWI329105B (en) 2002-02-01 2010-08-21 Rigel Pharmaceuticals Inc 2,4-pyrimidinediamine compounds and their uses
ES2337782T3 (en) 2002-07-29 2010-04-29 Rigel Pharmaceuticals, Inc. METHODS TO TREAT OR PREVENT AUTOIMMUNITY DISEASES WITH 2,4-PYRIMIDINDIAMINE COMPOUNDS.
KR20050086784A (en) * 2002-11-26 2005-08-30 화이자 프로덕츠 인크. Method of treatment of transplant rejection
NZ545270A (en) 2003-07-30 2010-04-30 Rigel Pharmaceuticals Inc 2,4-Pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases
CN101106983A (en) * 2004-11-24 2008-01-16 诺瓦提斯公司 Combinations comprising JAK inhibitors and at least one of Bcr-Abl, Flt-3, FAK or RAF kinase inhibitors
AR054416A1 (en) 2004-12-22 2007-06-27 Incyte Corp PIRROLO [2,3-B] PIRIDIN-4-IL-AMINAS AND PIRROLO [2,3-B] PIRIMIDIN-4-IL-AMINAS AS INHIBITORS OF THE JANUS KINASES. PHARMACEUTICAL COMPOSITIONS.
ES2651349T3 (en) 2005-06-08 2018-01-25 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibiting the JAK route
US20070203161A1 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
EP1910358A2 (en) 2005-07-14 2008-04-16 Astellas Pharma Inc. Heterocyclic janus kinase 3 inhibitors
CN102127078A (en) 2005-07-14 2011-07-20 安斯泰来制药株式会社 Heterocyclic janus kinase 3 inhibitors
PT1913000E (en) 2005-07-29 2012-02-28 Pfizer Prod Inc Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis
EP2270014A1 (en) 2005-09-22 2011-01-05 Incyte Corporation Azepine inhibitors of janus kinases
TW201434835A (en) 2005-12-13 2014-09-16 Incyte Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
JP2009528295A (en) 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 Compositions and methods for inhibition of the JAK pathway
GB0605691D0 (en) * 2006-03-21 2006-05-03 Novartis Ag Organic Compounds
ES2415863T3 (en) 2006-12-22 2013-07-29 Incyte Corporation Substituted heterocycles as Janus Kinase inhibitors
CL2008001709A1 (en) 2007-06-13 2008-11-03 Incyte Corp Compounds derived from pyrrolo [2,3-b] pyrimidine, jak kinase modulators; pharmaceutical composition; and use in the treatment of diseases such as cancer, psoriasis, rheumatoid arthritis, among others.
LT3070090T (en) 2007-06-13 2019-06-25 Incyte Holdings Corporation Use of salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h- pyrazol-1-yl)-3- cyclopentylpropanenitrile
ES2523303T3 (en) 2007-07-11 2014-11-24 Pfizer Inc. Pharmaceutical compositions and procedures for treating dry eye disorders
US20100267720A1 (en) * 2007-07-30 2010-10-21 Astrazeneca Ab Crystalline Forms of 2-Hydroxy-3- [5- (Morpholin- 4- Ylmethyl) Pyridin-2-YL] IH- Indole- 5 -Carbonitrile Citrate
KR101700454B1 (en) 2008-02-15 2017-01-26 리겔 파마슈티칼스, 인크. Pyrimidine-2-amine compounds and their use as inhibitors of jak kinases
PT2288610T (en) 2008-03-11 2016-10-17 Incyte Holdings Corp Azetidine and cyclobutane derivatives as jak inhibitors
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
US8063058B2 (en) 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
BRPI0910668A2 (en) 2008-04-22 2019-09-24 Portola Pharmaceutiacals Inc protein kinase inhibitors
PT2384326E (en) 2008-08-20 2014-06-09 Zoetis Llc Pyrrolo[2,3-d]pyrimidine compounds
US8385364B2 (en) * 2008-09-24 2013-02-26 Nec Laboratories America, Inc. Distributed message-passing based resource allocation in wireless systems
US9145396B2 (en) * 2008-12-01 2015-09-29 Targacept, Inc. Synthesis and novel salt forms of (R)-5-((E)-2-pyrrolidin-3ylvinyl)pyrimidine
US20100189791A1 (en) 2009-01-23 2010-07-29 Teva Pharmaceutical Industries, Ltd. Delayed release rasagiline malate formulation
JP5709276B2 (en) 2009-04-20 2015-04-30 オースペックス ファーマシューティカルズ，エルエルシー Piperidine inhibitor of Janus kinase 3
KR101771401B1 (en) 2009-05-22 2017-08-25 인사이트 홀딩스 코포레이션 N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
PT2432472T (en) 2009-05-22 2019-12-09 Incyte Holdings Corp 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
JP5946768B2 (en) 2009-10-09 2016-07-06 インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ Hydroxyl, keto and glucuronide derivatives of 3- (4- (7H-pyrrolo [2,3-d] pyrimidin-4-yl) -1H-pyrazol-1-yl) -3-cyclopentylpropanenitrile
EP2545045B1 (en) 2010-03-10 2016-01-06 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
EA035981B1 (en) 2010-05-21 2020-09-09 Инсайт Холдингс Корпорейшн Jak inhibitor formulation for topical application
EP2635557A2 (en) 2010-11-01 2013-09-11 Portola Pharmaceuticals, Inc. Nicotinamides as jak kinase modulators
TW201249845A (en) 2010-11-19 2012-12-16 Incyte Corp 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
EP2481397A1 (en) 2011-01-27 2012-08-01 Ratiopharm GmbH Pharmaceutical compositions comprising tasocitinib
EP2481411A1 (en) * 2011-01-27 2012-08-01 Ratiopharm GmbH Oral dosage forms for modified release comprising the JAK3 inhibitor tasocitinib
ES2547916T3 (en) 2011-02-18 2015-10-09 Novartis Pharma Ag MTOR / JAK inhibitor combination therapy
WO2012135338A1 (en) 2011-03-28 2012-10-04 Ratiopharm Gmbh Processes for preparing tofacitinib salts
CN104610264A (en) 2011-04-08 2015-05-13 辉瑞大药厂 Crystalline and non- crystalline forms of tofacitinib, and a pharmaceutical composition comprising tofacitinib and a penetration enhancer
ES2560611T3 (en) 2011-06-20 2016-02-22 Incyte Holdings Corporation Phenyl azetidinyl, 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 (en) 2011-08-18 2013-04-01 Incyte Corp Cyclohexyl azetidine derivatives as JAK inhibitors
UA111854C2 (en) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн METHODS AND INTERMEDIATE COMPOUNDS FOR JAK INHIBITORS
KR102019530B1 (en) 2011-11-23 2019-09-06 포톨라 파마슈티컬스, 인코포레이티드 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
EP3170827A1 (en) 2011-12-15 2017-05-24 ratiopharm GmbH Tofacitinib mono-oxalate salt
US20130310340A1 (en) 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
TW201406761A (en) 2012-05-18 2014-02-16 Incyte Corp Piperidinylcyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as JAK inhibitors
EP2903970A4 (en) 2012-10-08 2016-11-30 Portola Pharm Inc Substituted pyrimidinyl kinase inhibitors
CN105007901A (en) 2012-11-15 2015-10-28 因赛特公司 Sustained-release dosage forms of ruxolitinib
US9481679B2 (en) 2012-12-17 2016-11-01 Sun Pharmaceutical Industries Limited Process for the preparation of tofacitinib and intermediates thereof
US9670160B2 (en) 2012-12-28 2017-06-06 Glenmark Pharmaceuticals Limited Process for the preparation of tofacitinib and intermediates thereof
CN103073552B (en) * 2013-02-05 2015-08-12 华润赛科药业有限责任公司 A kind of unformed Citric Acid holder method is for the preparation method of Buddhist nun
TWI634121B (en) 2013-03-06 2018-09-01 英塞特控股公司 Processes and intermediates for making a jak inhibitor
JP6041823B2 (en) 2013-03-16 2016-12-14 ファイザー・インク Tofacitinib oral sustained release dosage form
WO2014174073A1 (en) 2013-04-26 2014-10-30 Sandoz Ag Sustained release formulations of tofacitinib
US20160122354A1 (en) * 2013-06-05 2016-05-05 Srinivasan Thirumalai Rajan PROCESS FOR THE PREPARATION OF (3R,4R)-4-METHYL-3-(METHYL-7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL-AMINO)-ß-OXO-1-PIPERIDINEPROPANENITRILE AND ITS SALTS
CN104341422A (en) * 2013-07-26 2015-02-11 重庆医药工业研究院有限责任公司 Tofacitinib intermediate and preparation method thereof
TWI822248B (en) 2013-08-07 2023-11-11 美商英塞特控股公司 Sustained release dosage forms for a jak1 inhibitor
CN104447752A (en) * 2013-09-16 2015-03-25 天津市汉康医药生物技术有限公司 Tofacitinib hydrate and preparation method thereof
CN104447751A (en) * 2013-09-16 2015-03-25 天津市汉康医药生物技术有限公司 Tofacitinib compound
CN104292231B (en) * 2013-09-17 2016-11-30 广东东阳光药业有限公司 A kind of citric acid expelling pathogens by strengthening vital QI is for the preparation method of Buddhist nun
CN105873931B (en) * 2013-10-08 2018-10-16 广东东阳光药业有限公司 Support method replaces cloth citrate
CN103585126A (en) * 2013-11-18 2014-02-19 南京艾德凯腾生物医药有限责任公司 Tofacitinib composition and preparation method thereof
PT2994454T (en) * 2013-12-09 2019-04-02 Unichem Lab Ltd An improved process for the preparation of (3r,4r)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine
CN104774206A (en) * 2014-01-14 2015-07-15 江苏柯菲平医药股份有限公司 New method for preparing tofacitinib citrate crystal-form A
US9260438B2 (en) * 2014-02-06 2016-02-16 Apotex Inc. Solid forms of tofacitinib salts
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
CN104387392B (en) * 2014-08-22 2016-09-28 中孚药业股份有限公司 Prepare the expelling pathogens by strengthening vital QI method for cloth
US10034882B2 (en) * 2015-07-27 2018-07-31 Unichem Laboratories Limited Tofacitinib orally disintegrating tablets
CN105348287A (en) * 2015-11-30 2016-02-24 宁波立华制药有限公司 Novel synthesis process of tofacitinib citrate
WO2017125417A1 (en) 2016-01-18 2017-07-27 Helmholtz Zentrum München - Deutsches Forschungszentrum für Gesundheit und Umwelt (GmbH) Tofacitinib as vaccination immune modulator
EP3511333B1 (en) * 2016-11-23 2021-05-12 Wuxi Fortune Pharmaceutical Co., Ltd Crystal form and salt form of 7h-pyrrolo[2,3-d]pyrimidine compound and preparation method therefor
WO2018172821A1 (en) * 2017-03-23 2018-09-27 Phalanx Labs Private Limited Novel tofacitinib addition salts and process for the preparation thereof
CN106967072B (en) * 2017-04-12 2019-05-03 山东裕欣药业有限公司 Tofacitinib citrate crystal form compound and preparation method thereof
CN109293682A (en) * 2017-07-25 2019-02-01 重庆医药工业研究院有限责任公司 A kind of support method is for cloth impurity and preparation method thereof
US10596161B2 (en) 2017-12-08 2020-03-24 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
MD3746429T2 (en) 2018-01-30 2022-08-31 Incyte Corp Processes for preparing (1-(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
KR20190110459A (en) * 2018-03-20 2019-09-30 삼진제약주식회사 Novel Salt, Preparation Methods thereof and Pharmaceutical Compositions Comprising thereof
CN108484607A (en) * 2018-03-26 2018-09-04 山东科兴生物制品有限公司 Novel preparation method of tofacitinib citrate
CN113768927A (en) 2018-03-30 2021-12-10 因赛特公司 Treatment of hidradenitis suppurativa with JAK inhibitors
US20220016250A1 (en) 2018-05-03 2022-01-20 Joel Schneider Peptide hydrogels for delivery of immunosuppressive drugs and uses thereof
US20190381046A1 (en) * 2018-06-14 2019-12-19 Andrew HANNA Tofacitinib and baclofen compositions and applications
CN109516991B (en) * 2018-12-29 2020-08-07 山东罗欣药业集团股份有限公司 Tofacitinib citrate crystal form compound and preparation method thereof
KR20230031981A (en) 2019-05-14 2023-03-07 프로벤션 바이오, 인코포레이티드 Methods and compositions for preventing type 1 diabetes
KR102209701B1 (en) 2019-08-16 2021-01-29 유니셀랩 주식회사 A novel crystalline form of tofacitinib, method for prepating thereof
EP4057989A1 (en) 2019-11-14 2022-09-21 Pfizer Inc. 1-(((2s,3s,4s)-3-ethyl-4-fluoro-5-oxopyrrolidin-2-yl)methoxy)-7-methoxyisoquinoline-6-carboxamide combinations and oral dosage forms
WO2021198980A1 (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
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 (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
ATE159257T1 (en) * 1994-05-03 1997-11-15 Ciba Geigy Ag PYRROLOPYRIMIDE DERIVATIVES WITH ANTIPROLIFERATIVE EFFECT
CA2262421C (en) * 1996-08-23 2007-10-02 Novartis Ag Substituted pyrrolopyrimidines and processes for their preparation
EP0972197A1 (en) * 1997-03-24 2000-01-19 PHARMACIA & UPJOHN COMPANY Method for identifying inhibitors of jak2/cytokine receptor binding
PA8474101A1 (en) 1998-06-19 2000-09-29 Pfizer Prod Inc PYROLEUM [2,3-D] PIRIMIDINE COMPOUNDS
BR9911365A (en) 1998-06-19 2001-03-13 Pfizer Prod Inc Pyrrolo [2,3-d] pyrimidine compounds
US6080747A (en) * 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
CA2393640C (en) * 1999-12-10 2006-09-05 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidine compounds
US7301023B2 (en) 2001-05-31 2007-11-27 Pfizer Inc. Chiral salt resolution
GT200200234A (en) * 2001-12-06 2003-06-27 NEW CRYSTAL COMPOUNDS

Also Published As

Publication number Publication date
RU2004117088A (en) 2005-03-27
CN1325498C (en) 2007-07-11
RU2315052C2 (en) 2008-01-20
CN1596257A (en) 2005-03-16
TW200300690A (en) 2003-06-16
EP1451192B1 (en) 2011-02-09
CY1111311T1 (en) 2015-08-05
AR037635A1 (en) 2004-11-17
AU2002348857B2 (en) 2008-12-04
ATE497962T1 (en) 2011-02-15
DK1451192T3 (en) 2011-04-04
BR0214761A (en) 2004-11-09
IL161914A0 (en) 2005-11-20
JP2005511696A (en) 2005-04-28
KR20050044691A (en) 2005-05-12
PE20030807A1 (en) 2003-09-22
CA2469350C (en) 2009-09-29
WO2003048162A1 (en) 2003-06-12
EP1451192A1 (en) 2004-09-01
PL221493B1 (en) 2016-04-29
NZ532366A (en) 2006-11-30
KR100691590B1 (en) 2007-03-09
US7803805B2 (en) 2010-09-28
CO5580780A2 (en) 2005-11-30
US20030130292A1 (en) 2003-07-10
PL370297A1 (en) 2005-05-16
HN2002000349A (en) 2003-08-20
ES2357942T3 (en) 2011-05-04
US20050159434A1 (en) 2005-07-21
NO20042721L (en) 2004-06-28
UY27567A1 (en) 2003-07-31
PA8560201A1 (en) 2003-12-10
HK1070653A1 (en) 2005-06-24
MXPA04005401A (en) 2004-10-11
DE60239146D1 (en) 2011-03-24
JP4201135B2 (en) 2008-12-24
GT200200234A (en) 2003-06-27
ZA200404270B (en) 2005-10-26
AU2002348857A1 (en) 2003-06-17
US6965027B2 (en) 2005-11-15

Similar Documents

Publication Publication Date Title
CA2469350A1 (en) 3-{4-methyl-3[methyl-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile mono citrate salt
HUS1900008I1 (en) 3-{(3r,4r)-4-methyl-3-[methyl-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-amino]-piperidin-1-yl}-3-oxo-propionitrile as protein kinase inhibitor
WO2007012953A3 (en) Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis
WO2007044407A3 (en) Pyrazolo (1 , 5a) pyrimidines as protein kinase inhibitors
WO2005037198A3 (en) Preparation of 1,7-disubstituted azabenzimidazoles as kinase inhibitors
ZA200704476B (en) Pyrazolo[1,5-a]pyrimidines useful as inhibitors of protein kinases
WO2007044426A3 (en) Pyrazolopyrimidines as protein kinase inhibitors
WO2007065664A3 (en) Pyrazolo[1,5-a]pyridine-3-carboxylic acids as ephb and vegfr2 kinase inhibitors
HUP0400300A3 (en) Pyrrolopyrimidines as protein kinase inhibitors
SG156521A1 (en) 4-amino-6-phenyl-pyrrolo[2,3-d] pyrimidine derivatives
WO2007025540A3 (en) Substituted imidazo[1,2b]pyridazines as kinase inhibitors, the production thereof, and use of the same as medicaments
HK1068134A1 (en) Pyrrolopyrimidines as protein kinase inhibitors
WO2006105372A3 (en) Alkynyl pyrrolopyrimidines and related analogs as hsp90-inhibitors
WO2004043379A3 (en) Chemical compounds
EP1421031A4 (en) Process of producing magnesium ammonium phosphate in monohydrate form (dittmarite)
CA2443820A1 (en) Process for the preparation of alkyl-n-(3-dimethylamino)alkylcarbamates
AU2002318904A1 (en) Process of producing magnesium ammonium phosphate in monohydrate form (dittmarite)
DOP2002000513A (en) NEW CRYSTAL COMPOUNDS.
AU2002216957A1 (en) Method of producing evaporator boards
CA2535742A1 (en) Preparation of risperidone

Legal Events

Date Code Title Description
EEER Examination request
MKEX Expiry

Effective date: 20221125