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WO2016063294A3 - Process for the preparation of (r)-3-(4-(7h-pyrrolo[2,3-d], pyrimidin-4-yl)-1 h-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate and its polymorphs thereof - Google Patents

Process for the preparation of (r)-3-(4-(7h-pyrrolo[2,3-d], pyrimidin-4-yl)-1 h-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate and its polymorphs thereof Download PDF

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Publication number
WO2016063294A3
WO2016063294A3 PCT/IN2015/000398 IN2015000398W WO2016063294A3 WO 2016063294 A3 WO2016063294 A3 WO 2016063294A3 IN 2015000398 W IN2015000398 W IN 2015000398W WO 2016063294 A3 WO2016063294 A3 WO 2016063294A3
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WO
WIPO (PCT)
Prior art keywords
pyrrolo
pyrazol
pyrimidin
preparation
polymorphs
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.)
Ceased
Application number
PCT/IN2015/000398
Other languages
French (fr)
Other versions
WO2016063294A2 (en
Inventor
Srinivasan Thirumalai Rajan
Sajja Eswaraiah
Gogulapati VENKATA PANAKALA RAI
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.)
MSN Laboratories Pvt Ltd
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MSN Laboratories Pvt Ltd
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Publication date
Application filed by MSN Laboratories Pvt Ltd filed Critical MSN Laboratories Pvt Ltd
Publication of WO2016063294A2 publication Critical patent/WO2016063294A2/en
Publication of WO2016063294A3 publication Critical patent/WO2016063294A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/0803—Compounds with Si-C or Si-Si linkages
    • C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
    • C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention provides an improved process for the preparation of (R)-3-(4-(7H- pyrrolo[2,3d-]pyrimidin-4-yl)-lH-pyrazol-l-yl)-3-cyclopentylpropanenitrile phosphate compound of formula- la and its novel polymorphs thereof, which is represented by the following structural formula:
PCT/IN2015/000398 2014-10-20 2015-10-20 Process for the preparation of (r)-3-(4-(7h-pyrrolo[2,3-d], pyrimidin-4-yl)-1 h-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate and its polymorphs thereof Ceased WO2016063294A2 (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
IN5225/CHE/2014 2014-10-20
IN5225CH2014 2014-10-20
IN270/CHE/2015 2015-01-19
IN270CH2015 2015-01-19
IN2369CH2015 2015-05-11
IN2369/CHE/2015 2015-05-11

Publications (2)

Publication Number Publication Date
WO2016063294A2 WO2016063294A2 (en) 2016-04-28
WO2016063294A3 true WO2016063294A3 (en) 2016-07-07

Family

ID=55761709

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2015/000398 Ceased WO2016063294A2 (en) 2014-10-20 2015-10-20 Process for the preparation of (r)-3-(4-(7h-pyrrolo[2,3-d], pyrimidin-4-yl)-1 h-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate and its polymorphs thereof

Country Status (1)

Country Link
WO (1) WO2016063294A2 (en)

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CN111763209B (en) * 2015-12-31 2021-12-03 正大天晴药业集团股份有限公司 Synthesis process of luccotinib
CZ201629A3 (en) * 2016-01-22 2017-08-02 Zentiva, K.S. Crystalline modifications of the (3R)-3-cyclopentyl-3- [4-(7H-pyrrolo [2,3-d] pyrimidin-4yl) pyrazol-1yl] propanenitrile salts and the method of their preparation
WO2022040180A1 (en) 2020-08-18 2022-02-24 Incyte Corporation Process and intermediates for preparing a jak inhibitor
PE20231308A1 (en) 2020-08-18 2023-08-24 Incyte Corp PROCESS AND INTERMEDIATE TO PREPARE A JAK1 INHIBITOR
CN114853760A (en) * 2021-02-03 2022-08-05 南京正大天晴制药有限公司 Preparation method of luccotinib intermediate
CN113292569A (en) * 2021-05-25 2021-08-24 常州制药厂有限公司 Preparation method of JAK inhibitor
WO2023288197A1 (en) 2021-07-12 2023-01-19 Incyte Corporation Process and intermediates for preparing baricitinib
CA3139457A1 (en) * 2021-11-19 2023-05-19 Apotex Inc. Novel salts of ruxolitinib and crystalline forms thereof
CN114044777B (en) * 2022-01-10 2022-04-19 南京佰麦生物技术有限公司 Preparation method of tricitabinib phosphate
US20230399331A1 (en) * 2022-06-14 2023-12-14 Incyte Corporation Solid forms of jak inhibitor and process of preparing the same
CN115124537A (en) * 2022-07-13 2022-09-30 山东大学 A kind of preparation method of JAK inhibitor baricitinib
EP4565213A1 (en) 2022-08-03 2025-06-11 Medichem, S.A. Stable oral pharmaceutical formulation containing ruxolitinib hemifumarate
CN118255768A (en) * 2022-12-26 2024-06-28 上海科胜药物研发有限公司 Preparation method of JAK inhibitor and intermediate thereof
AU2024335978A1 (en) * 2023-09-04 2025-10-30 Granules India Limited Improved process for the preparation of ruxolitinib and novel crystalline form thereof
CN118047782A (en) * 2024-02-06 2024-05-17 南京道尔医药研究院有限公司 Process for preparing intermediate of ponatinib
US12247034B1 (en) 2024-04-19 2025-03-11 Sun Pharmaceutical Industries, Inc. Crystalline form of deuruxolitinib phosphate
CN118994172A (en) * 2024-09-12 2024-11-22 广州科锐特生物科技有限公司 Preparation method of poncirtinib phosphate

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7598257B2 (en) * 2005-12-13 2009-10-06 Incyte Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
US8722693B2 (en) * 2007-06-13 2014-05-13 Incyte Corporation Salts of the Janus kinase inhibitor (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7598257B2 (en) * 2005-12-13 2009-10-06 Incyte Corporation Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
US8722693B2 (en) * 2007-06-13 2014-05-13 Incyte Corporation Salts of the Janus kinase inhibitor (R)-3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile

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