CN1729192A - ( 1－苄基－4－甲基哌啶－3－基)－甲基胺的旋光拆分及其用于制备作为蛋白激酶抑制剂的吡咯并[2 , 3－d ]嘧啶衍生物的应用 - Google Patents

( 1－苄基－4－甲基哌啶－3－基)－甲基胺的旋光拆分及其用于制备作为蛋白激酶抑制剂的吡咯并[2 , 3－d ]嘧啶衍生物的应用 Download PDF

Info

Publication number
CN1729192A
CN1729192A CNA028108175A CN02810817A CN1729192A CN 1729192 A CN1729192 A CN 1729192A CN A028108175 A CNA028108175 A CN A028108175A CN 02810817 A CN02810817 A CN 02810817A CN 1729192 A CN1729192 A CN 1729192A
Authority
CN
China
Prior art keywords
alkyl
amino
alkoxy
alkylamino
group
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.)
Pending
Application number
CNA028108175A
Other languages
English (en)
Chinese (zh)
Inventor
G·E·威尔科克斯
C·克歇尔
T·弗里斯
M·E·弗兰纳根
M·J·芒奇霍夫
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
Pfizer Products 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=CN1729192(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer Products Inc filed Critical Pfizer Products Inc
Publication of CN1729192A publication Critical patent/CN1729192A/zh
Pending 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
    • 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Psychiatry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Emergency Medicine (AREA)
  • Transplantation (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pain & Pain Management (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)
CNA028108175A 2001-05-31 2002-05-29 ( 1－苄基－4－甲基哌啶－3－基)－甲基胺的旋光拆分及其用于制备作为蛋白激酶抑制剂的吡咯并[2 , 3－d ]嘧啶衍生物的应用 Pending CN1729192A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US29477501P 2001-05-31 2001-05-31
US60/294,775 2001-05-31
US34104801P 2001-12-06 2001-12-06
US60/341,048 2001-12-06

Publications (1)

Publication Number Publication Date
CN1729192A true CN1729192A (zh) 2006-02-01

Family

ID=26968730

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA028108175A Pending CN1729192A (zh) 2001-05-31 2002-05-29 ( 1－苄基－4－甲基哌啶－3－基)－甲基胺的旋光拆分及其用于制备作为蛋白激酶抑制剂的吡咯并[2 , 3－d ]嘧啶衍生物的应用

Country Status (52)

Country Link
US (2) US7301023B2 (enExample)
EP (3) EP1392694A1 (enExample)
JP (1) JP4381137B2 (enExample)
KR (5) KR100926875B1 (enExample)
CN (1) CN1729192A (enExample)
AP (1) AP1859A (enExample)
AR (2) AR037321A1 (enExample)
AT (1) ATE519741T1 (enExample)
AU (2) AU2002304401C1 (enExample)
BE (1) BE2017C032I2 (enExample)
BG (1) BG66489B1 (enExample)
BR (1) BR0209246A (enExample)
CA (1) CA2448281C (enExample)
CL (1) CL2008000762A1 (enExample)
CR (1) CR10177A (enExample)
CU (1) CU23337B7 (enExample)
CY (2) CY1113322T1 (enExample)
CZ (1) CZ304366B6 (enExample)
DK (1) DK1666481T3 (enExample)
EA (2) EA012666B1 (enExample)
EC (1) ECSP034865A (enExample)
EE (1) EE05332B1 (enExample)
ES (2) ES2393385T3 (enExample)
FR (1) FR17C1031I2 (enExample)
GE (1) GEP20063784B (enExample)
GT (2) GT200200100A (enExample)
HR (1) HRP20030943B1 (enExample)
HU (2) HU230876B1 (enExample)
IL (1) IL158588A0 (enExample)
IS (1) IS3023B (enExample)
LT (1) LTC1666481I2 (enExample)
LU (1) LUC00031I2 (enExample)
MA (1) MA27029A1 (enExample)
MX (1) MXPA03011062A (enExample)
MY (1) MY129649A (enExample)
NL (1) NL300887I2 (enExample)
NO (3) NO328578B1 (enExample)
NZ (2) NZ530380A (enExample)
OA (1) OA12612A (enExample)
PA (1) PA8546301A1 (enExample)
PE (1) PE20030561A1 (enExample)
PL (2) PL228155B1 (enExample)
PT (1) PT1666481E (enExample)
RS (1) RS52144B (enExample)
SI (1) SI1666481T1 (enExample)
SK (2) SK288192B6 (enExample)
TN (1) TNSN03128A1 (enExample)
TW (2) TWI310384B (enExample)
UA (1) UA80093C2 (enExample)
UY (1) UY27317A1 (enExample)
WO (1) WO2002096909A1 (enExample)
ZA (1) ZA200307982B (enExample)

Cited By (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102596962A (zh) * 2009-09-10 2012-07-18 弗·哈夫曼-拉罗切有限公司 Jak抑制剂
CN103459394A (zh) * 2011-04-08 2013-12-18 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
CN104185420A (zh) * 2011-11-30 2014-12-03 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
CN104513248A (zh) * 2013-09-30 2015-04-15 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
CN104761556A (zh) * 2015-03-21 2015-07-08 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
CN104955803A (zh) * 2012-11-30 2015-09-30 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
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
WO2016116025A1 (zh) * 2015-01-20 2016-07-28 南京明德新药研发股份有限公司 Jak抑制剂
CN106660949A (zh) * 2015-02-17 2017-05-10 株式会社爱茉莉太平洋 N‑[4‑(1‑氨基乙基)‑苯基]‑磺酰胺衍生物的手性拆分方法
CN106831538A (zh) * 2017-01-22 2017-06-13 苏州楚凯药业有限公司 托法替尼中间体的制备方法
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
US10174056B2 (en) 2015-05-29 2019-01-08 Wuxi Fortune Pharmaceutical Co., Ltd Substituted pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
US10174036B2 (en) 2015-04-29 2019-01-08 Wuxi Fortune Pharmaceutical Co., Ltd Substituted pyrazoles as JAK inhibitors
US10821111B2 (en) 2011-11-30 2020-11-03 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
CN113549075A (zh) * 2021-06-23 2021-10-26 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
CN113614069A (zh) * 2019-04-05 2021-11-05 柳韩洋行 用于制备(3r,4r)-1-苄基-n,4-二甲基哌啶-3-胺或其盐的方法以及使用其制备托法替尼的方法

Families Citing this family (110)

* 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
OA12118A (en) 1999-12-10 2006-05-04 Pfizer Prod Inc PyrroloÄ2,3-dÜpyrimidine compounds.
OA12292A (en) * 2000-06-26 2003-11-11 Pfizer Prod Inc PyrroloÄ2,3-dÜpyrimidine compounds as immunosuppressive agents.
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
IL166241A0 (en) 2002-07-29 2006-01-15 Rigel Pharmaceuticals Inc Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds
ATE402700T1 (de) * 2002-08-27 2008-08-15 Merck Patent Gmbh Glycinamid-derivate als raf-kinase-hemmer
WO2004047843A1 (en) 2002-11-26 2004-06-10 Pfizer Products Inc. Method of treatment of transplant rejection
ES2421139T3 (es) 2003-07-30 2013-08-29 Rigel Pharmaceuticals, Inc. Compuestos de 2,4-pirimidindiamina para su uso en el tratamiento o la prevención de enfermedades autoinmunitarias
WO2005105146A1 (en) * 2004-05-03 2005-11-10 Novartis Ag Combinations comprising a s1p receptor agonist and a jak3 kinase inhibitor
MXPA06015237A (es) 2004-06-29 2007-12-10 Amgen Inc Pirrolo[2-3-d]pirimidinas que modulan la actividad de ack1 y lck.
MX2007001399A (es) 2004-08-02 2007-04-18 Osi Pharm Inc Compuestos que inhiben pirrolopirimidina multi-cinasa aril-amino sustituidas.
RU2007123675A (ru) * 2004-11-24 2008-12-27 Новартис АГ (CH) Комбинации ингибиторов jak
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.
WO2006133426A2 (en) 2005-06-08 2006-12-14 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
JP5071374B2 (ja) 2005-07-14 2012-11-14 アステラス製薬株式会社 ヘテロ環ヤヌスキナーゼ３阻害剤
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
WO2007012953A2 (en) 2005-07-29 2007-02-01 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis
WO2007038215A1 (en) 2005-09-22 2007-04-05 Incyte Corporation Tetracyclic inhibitors of janus kinases
HUE028588T2 (hu) 2005-12-13 2016-12-28 Incyte Holdings Corp Heteroaril-szubsztituált pirrolo[2,3-b]piridinek és pirrolo[2,3-b]pirimidinek mint Janus-kináz inhibitorok
WO2007098507A2 (en) 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
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.
EP2740731B1 (en) 2007-06-13 2016-03-23 Incyte Holdings Corporation Crystalline salts of the janus kinase inhibitor (r)-3-(4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl)-3-cyclopentylpropanenitrile
WO2009007839A1 (en) * 2007-07-11 2009-01-15 Pfizer Inc. Pharmaceutical compositions and methods of treating dry eye disorders
HRP20170317T1 (hr) 2008-02-15 2017-04-21 Rigel Pharmaceuticals, Inc. Spojevi pirimidin-2-amina i njihova uporaba kao inhibitora jak kinaza
MY165582A (en) 2008-03-11 2018-04-05 Incyte Holdings Corp Azetidine and cyclobutane derivatives as jak inhibitors
US8063058B2 (en) 2008-04-16 2011-11-22 Portola Pharmaceuticals, Inc. Inhibitors of syk and JAK protein kinases
US8138339B2 (en) 2008-04-16 2012-03-20 Portola Pharmaceuticals, Inc. Inhibitors of protein kinases
BRPI0910668A2 (pt) 2008-04-22 2019-09-24 Portola Pharmaceutiacals Inc inibidores de proteína quinases
RU2011105768A (ru) * 2008-08-01 2012-09-10 Биокрист Фармасьютикалз, Инк. (Us) Производные пиперидина в качестве ингибиторов jakз
RS53382B (sr) * 2008-08-20 2014-10-31 Zoetis Llc Jedinjenja pirol [2,3-d]pirimidina
EP2396004A4 (en) * 2009-02-11 2012-07-25 Reaction Biology Corp SELECTIVE KINASE HEMMER
CA2759026C (en) 2009-04-20 2019-01-15 Auspex Pharmaceuticals, Inc. Piperidine inhibitors of janus kinase 3
BRPI1012108B8 (pt) 2009-05-22 2021-05-25 Incyte Corp composto 3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il]octa no- ou heptano-nitrila, sua composição, seus usos e processo para preparar um sal de ácido fosfórico
NZ596479A (en) 2009-05-22 2014-01-31 Incyte Corp N-(hetero)aryl-pyrrolidine derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines and pyrrol-3-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EA021478B1 (ru) 2009-10-09 2015-06-30 Инсайт Корпорейшн ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА
AU2010308028A1 (en) 2009-10-15 2012-04-19 Pfizer Inc. Pyrrolo[2,3-d] pyrimidine compounds
CA2782720A1 (en) 2009-12-18 2011-06-23 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
AU2011213198B2 (en) 2010-02-05 2014-04-24 Zoetis Llc Pyrrolo [ 2,3-d] pyrimidine urea compounds as JAK inhibitors
CA2792508C (en) 2010-03-10 2018-01-16 Incyte Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
EA202091303A3 (ru) 2010-05-21 2021-05-31 Инсайт Холдингс Корпорейшн Композиция ингибитора jak для местного применения
EP2975027A1 (en) 2010-11-01 2016-01-20 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
ES2536415T3 (es) 2010-11-19 2015-05-25 Incyte Corporation Pirrolopiridinas y pirrolopirimidinas sustituidas heterocíclicas como inhibidores de JAK
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
WO2012112847A1 (en) 2011-02-18 2012-08-23 Novartis Pharma Ag mTOR/JAK INHIBITOR COMBINATION THERAPY
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
ES2414384T3 (es) 2011-05-11 2013-07-19 Ratiopharm Gmbh Composición de liberación modificada que comprende ranolazina
US8691807B2 (en) 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
WO2013023119A1 (en) 2011-08-10 2013-02-14 Novartis Pharma Ag JAK P13K/mTOR COMBINATION THERAPY
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為ｊａｋ抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
EP2782579B1 (en) 2011-11-23 2019-01-02 Portola Pharmaceuticals, Inc. Pyrazine kinase inhibitors
WO2013090490A1 (en) 2011-12-15 2013-06-20 Ratiopharm Gmbh Tofacitinib salts
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
WO2014016338A1 (en) 2012-07-25 2014-01-30 Lek Pharmaceuticals D.D. New synthetic route for the preparation of 3-amino-piperidine compounds
WO2014058921A2 (en) 2012-10-08 2014-04-17 Portola Pharmaceuticals, Inc. Substituted pyrimidinyl kinase inhibitors
KR102242077B1 (ko) 2012-11-15 2021-04-20 인사이트 홀딩스 코포레이션 룩솔리티니브의 서방성 제형
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
EA027879B1 (ru) 2013-02-22 2017-09-29 Пфайзер Инк. ПРОИЗВОДНЫЕ ПИРРОЛО[2,3-d]ПИРИМИДИНА В КАЧЕСТВЕ ИНГИБИТОРОВ ЯНУС-РОДСТВЕННЫХ КИНАЗ (JAK)
EP3489239B1 (en) 2013-03-06 2021-09-15 Incyte Holdings Corporation Processes and intermediates for making a jak inhibitor
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
MX376856B (es) 2013-08-07 2025-03-07 Incyte Holdings Corp Formas de dosificacion de liberacion prolongada para un inhibidor de jak 1 (cinasa de janus 1).
LT3077395T (lt) 2013-12-05 2018-02-12 Pfizer Inc. Pirolo[2,3-d]pirimidinilo, pirolo[2,3-b]pirazinilo ir pirolo[2,3-d]piridinilo akrilamidai
ES2865058T3 (es) 2013-12-09 2021-10-14 Unichem Lab Ltd Un proceso mejorado para la preparación de (3R,4R)-(1-bencil-4-metilpiperidin-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
WO2016024185A1 (en) 2014-08-12 2016-02-18 Pfizer Inc. Pyrrolo[2,3-d]pyrimidine derivatives useful for inhibiting janus kinase
EP3078665A1 (en) 2015-04-10 2016-10-12 OLON S.p.A. Efficient method for the preparation of tofacitinib citrate
CA2984183C (en) 2015-05-01 2021-11-09 Pfizer Inc. Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl, pyrrolo[2,3-b]pyridinyl acrylamides and epoxides thereof
BR112017013253A2 (pt) * 2015-07-27 2018-02-27 Unichem Laboratories Limited comprimidos de desintegração oral, processo para produzir comprimido de desintegração oral contendo tofacitinibe ou seus sais farmaceuticamente aceitáveis, processo para produzir comprimido de desintegração oral, desintegrante, e edulcorantes
KR101771219B1 (ko) * 2015-08-21 2017-09-05 양지화학 주식회사 야누스 키나제 1 선택적 억제제 및 그 의약 용도
CN108472298B (zh) 2015-11-24 2021-04-20 深圳阿拉丁医疗科技有限公司 选择性激酶抑制剂
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
RU2714206C1 (ru) 2016-06-30 2020-02-13 Даевунг Фармасьютикал Ко., Лтд. Пиразолопиримидиновые производные в качестве ингибитора киназы
KR102398659B1 (ko) 2017-03-17 2022-05-16 주식회사 대웅제약 카이네이즈 저해제로서의 피롤로트리아진 유도체
KR102078805B1 (ko) 2017-11-30 2020-02-19 보령제약 주식회사 토파시티닙을 포함하는 약제학적 조성물
TW201924683A (zh) 2017-12-08 2019-07-01 美商英塞特公司 用於治療骨髓增生性贅瘤的低劑量組合療法
MA51431B1 (fr) 2017-12-28 2022-08-31 Daewoong Pharmaceutical Co Ltd Dérivés d'oxy-fluoropipéridine utilisés en tant qu'inhibiteur de kinase
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
MD3746429T2 (ro) 2018-01-30 2022-08-31 Incyte Corp Procedee pentru prepararea de (1-(3-fluoro-2-(trifluorometil)izonicotinil)piperidin-4-onă)
US12161748B2 (en) 2018-01-31 2024-12-10 Twi Biotechnology, Inc. Topical formulations comprising tofacitinib
JP7324210B2 (ja) * 2018-01-31 2023-08-09 ティダブリューアイ・バイオテクノロジー・インコーポレイテッド トファシチニブを含む局所製剤
KR20260080448A (ko) 2018-03-30 2026-06-02 인사이트 코포레이션 Jak 억제제를 사용하는 화농성 한선염의 치료
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
GB2596942B (en) 2019-02-27 2023-05-10 Samson Clinical Pty Ltd Tofacitinib via oral mucosa for use in treatment of autoimmune hair loss or excessing hair shedding
CA3132109A1 (en) 2019-03-13 2020-09-17 Intas Pharmaceuticals Ltd. Process for preparation of tofacitinib and pharmaceutically acceptable salt thereof
EP3946606B1 (en) 2019-03-27 2025-01-01 Insilico Medicine IP Limited Bicyclic jak inhibitors and uses thereof
KR102897231B1 (ko) 2019-10-31 2025-12-05 아르티 인더스트리스 리미티드 토파시티닙 및 그 중간체의 제조방법
EP4054527A4 (en) 2019-11-08 2023-12-06 Cage Bio Inc. TOPICAL ADMINISTRATION OF TOFACITINIB USING IONIC LIQUID
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
KR102877132B1 (ko) * 2019-11-25 2025-10-27 주식회사 대웅제약 신규한 트리아졸로피리딘 유도체 및 이를 포함하는 약학 조성물
BR112022020020A2 (pt) 2020-04-04 2022-11-22 Pfizer Métodos de tratamento da doença do coronavírus 2019
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
WO2022194782A1 (en) * 2021-03-15 2022-09-22 Chiesi Farmaceutici S.P.A. Heterocyclic derivatives as janus kinase inhibitors
EP4180042A1 (en) 2021-11-15 2023-05-17 Sanovel Ilac Sanayi Ve Ticaret A.S. A film coated tablet comprising micronized tofacitinib
CN122341609A (zh) 2023-12-05 2026-07-03 株式会社大熊制药 1-((3S,4R)-3-((2-((1-乙基-1H-吡唑-4-基)氨基)-7H-吡咯并[2,3-d]嘧啶-4-基)氧基)-4-氟哌啶-1-基)丙-2-烯-1-酮的制备方法及其中间体化合物

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
ES2109796T3 (es) 1994-05-03 1998-01-16 Ciba Geigy Ag Derivados de pirrolopirimidilo con efecto antiproliferante.
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
MX9800136A (es) 1995-07-05 1998-03-29 Du Pont Pirimidinonas fungicidas.
PL188959B1 (pl) 1995-07-06 2005-05-31 Novartis Ag Pirolopirymidyny i sposoby ich wytwarzania
AR004010A1 (es) 1995-10-11 1998-09-30 Glaxo Group Ltd Compuestos heterociclicos
HUP9801177A3 (en) 1995-11-14 1998-11-30 Pharmacia & Upjohn Spa Tetrahydronaphthyl, indanyl and indolyl substituted pyrido[2,3-d]pyrimidine and purine derivatives, process for their preparation and pharmaceutical compositions containing them
US6140317A (en) 1996-01-23 2000-10-31 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
WO1997032879A1 (de) 1996-03-06 1997-09-12 Novartis Ag 7-ALKYL-PYRROLO[2,3-d]PYRIMIDINE
AU3176297A (en) 1996-06-25 1998-01-14 Novartis Ag Substituted 7-amino-pyrrolo{3,2-d}pyrimidines and the use thereof
AR007855A1 (es) 1996-07-13 1999-11-24 Glaxo Group Ltd Compuestos heterociclicos fusionados como inhibidores de proteina tirosina quinasa, sus metodos de preparacion, intermediarios, uso en medicinay composiciones farmaceuticas que los contienen
HRP970371A2 (en) 1996-07-13 1998-08-31 Kathryn Jane Smith Heterocyclic compounds
PT938486E (pt) 1996-08-23 2008-03-27 Novartis Ag Pirrolopirimidinas substituídas e processos para a sua preparação
IL129825A0 (en) 1996-11-27 2000-02-29 Pfizer Fused bicyclic pyrimidine derivatives
ES2301194T3 (es) 1997-02-05 2008-06-16 Warner-Lambert Company Llc Pirido 2,3-d pirimidinas y 4-aminopirimidinas como inhibidores de la proliferacion celular.
WO1998043087A1 (en) * 1997-03-24 1998-10-01 Pharmacia & Upjohn Company Method for identifying inhibitors of jak2/cytokine receptor binding
US6310063B1 (en) 1998-04-02 2001-10-30 Neurogen Corporation Aminoalkyl substituted pyrrolo [3,2-E]pyridine and pyrollo [2,3-b]pyrimidine derivatives: modulators of CRF1 receptors
HUP0102793A3 (en) 1998-05-28 2002-07-29 Parker Hughes Inst St Paul Quinazolines for treating brain tumor and medicaments containing them
AU3951899A (en) * 1998-06-19 2000-01-05 Pfizer Products Inc. Pyrrolo(2,3-d)pyrimidine compounds
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
AU5682799A (en) 1998-08-21 2000-03-14 Parker Hughes Institute Quinazoline derivatives
US6080747A (en) * 1999-03-05 2000-06-27 Hughes Institute JAK-3 inhibitors for treating allergic disorders
OA12118A (en) * 1999-12-10 2006-05-04 Pfizer Prod Inc PyrroloÄ2,3-dÜpyrimidine compounds.
OA12292A (en) * 2000-06-26 2003-11-11 Pfizer Prod Inc PyrroloÄ2,3-dÜpyrimidine compounds as immunosuppressive agents.
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.

Cited By (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102596962A (zh) * 2009-09-10 2012-07-18 弗·哈夫曼-拉罗切有限公司 Jak抑制剂
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
CN103459394A (zh) * 2011-04-08 2013-12-18 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
CN103459394B (zh) * 2011-04-08 2016-04-27 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
CN107898790A (zh) * 2011-11-30 2018-04-13 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
CN104185420A (zh) * 2011-11-30 2014-12-03 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
US11065254B2 (en) 2011-11-30 2021-07-20 The United States Government As Represented By The Department Of Veterans Affairs Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
US11045474B2 (en) 2011-11-30 2021-06-29 Emory University Antiviral JAK inhibitors useful in treating or preventing coronaviridae infections
US10821111B2 (en) 2011-11-30 2020-11-03 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
US9662332B2 (en) 2011-11-30 2017-05-30 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
CN104185420B (zh) * 2011-11-30 2017-06-09 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
US10022378B2 (en) 2011-11-30 2018-07-17 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
CN104955803A (zh) * 2012-11-30 2015-09-30 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
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
CN104513248A (zh) * 2013-09-30 2015-04-15 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
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
CN108349977A (zh) * 2015-01-20 2018-07-31 无锡福祈制药有限公司 Jak抑制剂
WO2016116025A1 (zh) * 2015-01-20 2016-07-28 南京明德新药研发股份有限公司 Jak抑制剂
AU2016208906B2 (en) * 2015-01-20 2018-07-12 Wuxi Fortune Pharmaceutical Co., Ltd JAK inhibitor
CN108349977B (zh) * 2015-01-20 2021-05-25 无锡福祈制药有限公司 Jak抑制剂
EA036122B1 (ru) * 2015-01-20 2020-09-30 Уси Форчун Фармасьютикал Ко., Лтд Ингибитор jak
US10617690B2 (en) 2015-01-20 2020-04-14 Wuxi Fortune Pharmaceutical Co., Ltd JAK inhibitor
TWI690531B (zh) * 2015-01-20 2020-04-11 大陸商無錫福祈製藥有限公司 Ｊａｋ抑制劑
CN106660949A (zh) * 2015-02-17 2017-05-10 株式会社爱茉莉太平洋 N‑[4‑(1‑氨基乙基)‑苯基]‑磺酰胺衍生物的手性拆分方法
CN104761556A (zh) * 2015-03-21 2015-07-08 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
US10174036B2 (en) 2015-04-29 2019-01-08 Wuxi Fortune Pharmaceutical Co., Ltd Substituted pyrazoles as JAK inhibitors
US10174056B2 (en) 2015-05-29 2019-01-08 Wuxi Fortune Pharmaceutical Co., Ltd Substituted pyrrolo[2,3-d]pyrimidines as janus 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
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
CN106831538A (zh) * 2017-01-22 2017-06-13 苏州楚凯药业有限公司 托法替尼中间体的制备方法
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
CN113614069A (zh) * 2019-04-05 2021-11-05 柳韩洋行 用于制备(3r,4r)-1-苄基-n,4-二甲基哌啶-3-胺或其盐的方法以及使用其制备托法替尼的方法
CN113614069B (zh) * 2019-04-05 2024-05-28 柳韩洋行 用于制备(3r,4r)-1-苄基-n,4-二甲基哌啶-3-胺或其盐的方法以及使用其制备托法替尼的方法
CN113549075A (zh) * 2021-06-23 2021-10-26 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

Also Published As

Publication number Publication date
NO2017047I1 (no) 2017-09-08
LTPA2017025I1 (lt) 2017-09-11
KR100869409B1 (ko) 2008-11-21
GT200200100A (es) 2003-02-11
AU2002304401C1 (en) 2009-03-05
TWI316061B (en) 2009-10-21
MXPA03011062A (es) 2004-03-19
KR20080083028A (ko) 2008-09-12
NO328578B1 (no) 2010-03-22
CA2448281A1 (en) 2002-12-05
EP1666481A2 (en) 2006-06-07
CU23337B7 (es) 2009-01-20
HU230876B1 (hu) 2018-11-29
US7301023B2 (en) 2007-11-27
PT1666481E (pt) 2012-12-03
CR10177A (es) 2008-08-19
AP1859A (en) 2008-07-02
IS6993A (is) 2003-10-13
MY129649A (en) 2007-04-30
NZ530380A (en) 2005-08-26
PA8546301A1 (es) 2003-05-14
SI1666481T1 (sl) 2012-11-30
CZ20033260A3 (en) 2004-03-17
IL158588A0 (en) 2004-05-12
SK288192B6 (sk) 2014-06-03
HUP0400152A3 (en) 2012-12-28
ZA200307982B (en) 2004-10-14
TW200413370A (en) 2004-08-01
NZ540332A (en) 2007-05-31
GT200200100AA (es) 2007-07-06
EE05332B1 (et) 2010-08-16
CZ304366B6 (cs) 2014-04-02
HUS1900008I1 (hu) 2020-02-28
EA007251B1 (ru) 2006-08-25
KR100868814B1 (ko) 2008-11-14
FR17C1031I2 (fr) 2018-11-02
TWI310384B (en) 2009-06-01
UY27317A1 (es) 2003-02-28
NO20035201L (no) 2003-11-24
EP1666481B1 (en) 2012-09-19
BR0209246A (pt) 2004-06-15
KR20060014459A (ko) 2006-02-15
OA12612A (en) 2006-06-09
CA2448281C (en) 2009-05-05
EA200600575A1 (ru) 2006-08-25
RS52144B (sr) 2012-08-31
BE2017C032I2 (enExample) 2021-07-19
CL2008000762A1 (es) 2008-07-04
IS3023B (is) 2020-08-15
LTC1666481I2 (lt) 2018-06-25
HRP20030943B1 (hr) 2011-11-30
PE20030561A1 (es) 2003-06-23
AU2002304401B2 (en) 2008-04-17
KR20080002931A (ko) 2008-01-04
AP2002002550A0 (en) 2002-06-30
AR045680A2 (es) 2005-11-09
US20040229923A1 (en) 2004-11-18
HRP20030943A2 (en) 2005-08-31
WO2002096909A1 (en) 2002-12-05
KR20060133117A (ko) 2006-12-22
YU92303A (sh) 2006-08-17
KR100926875B1 (ko) 2009-11-16
TNSN03128A1 (fr) 2005-12-23
LUC00031I2 (enExample) 2017-10-11
ES2369226T3 (es) 2011-11-28
US20030073719A1 (en) 2003-04-17
EE200300594A (et) 2004-04-15
PL367945A1 (en) 2005-03-07
EP1666481B9 (en) 2013-05-01
PL409305A1 (pl) 2014-12-22
JP4381137B2 (ja) 2009-12-09
EP1609781A1 (en) 2005-12-28
NO20093135L (no) 2003-11-24
FR17C1031I1 (fr) 2017-10-13
ATE519741T1 (de) 2011-08-15
NL300887I2 (nl) 2017-08-31
UA80093C2 (uk) 2007-08-27
AU2008203170B2 (en) 2009-06-18
EA012666B1 (ru) 2009-12-30
DK1666481T3 (da) 2012-10-15
ES2393385T3 (es) 2012-12-20
CY2017028I2 (el) 2018-02-14
CY1113322T1 (el) 2016-06-22
EP1666481A3 (en) 2006-11-29
GEP20063784B (en) 2006-04-10
US7432370B2 (en) 2008-10-07
EA200301193A1 (ru) 2004-04-29
AU2008203170A1 (en) 2008-08-07
EP1609781B1 (en) 2011-08-10
BG66489B1 (bg) 2015-05-29
NO20035201D0 (no) 2003-11-24
ECSP034865A (es) 2004-01-28
KR20040003037A (ko) 2004-01-07
EP1392694A1 (en) 2004-03-03
PL228155B1 (pl) 2018-02-28
SK288199B6 (sk) 2014-06-03
JP2004534047A (ja) 2004-11-11
AR037321A1 (es) 2004-11-03
SK14652003A3 (sk) 2004-05-04
MA27029A1 (fr) 2004-12-20
CY2017028I1 (el) 2018-02-14
BG108389A (bg) 2005-01-31
HUP0400152A2 (en) 2007-07-30
LUC00031I1 (enExample) 2017-08-10

Similar Documents

Publication Publication Date Title
CN1195755C (zh) 吡咯并[2,3－d]嘧啶化合物
CN1717236A (zh) 治疗移植排斥的方法
US7432370B2 (en) Chiral salt resolution
AU784297C (en) Pyrrolo(2,3-d)pyrimidine compounds as immunosuppressive agents
CN1726192A (zh) 3－氨基－哌啶衍生物及其制备方法
CN1893952A (zh) 用于治疗移植排斥的吡咯并[2,3－d]嘧啶化合物
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
US20050113395A1 (en) Method of treatment of atherosclerosis
CN1596257A (zh) 新型结晶化合物
CN1929737A (zh) Hiv整合酶抑制剂
CN1668592A (zh) 哌啶衍生物和它们用作MIP－1α与受体CCR1结合的选择性抑制剂的应用
HK1082501A (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
HK1051195B (en) Pyrrolo(2,3-d)pyrimidine compounds
HK1081440A (en) Method of treatment of transplant rejection
HK1084107A (en) 3-amino-piperidine derivatives and processes for their preparation
HK1097740A (en) Pyrrolo (2,3-d) pyrimidine compounds for treating transplant rejection

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 1082501

Country of ref document: HK

C12 Rejection of a patent application after its publication
RJ01 Rejection of invention patent application after publication

Open date: 20060201

REG Reference to a national code

Ref country code: HK

Ref legal event code: WD

Ref document number: 1082501

Country of ref document: HK