JP2020535193A - 結晶のリナグリプチン中間体およびリナグリプチンの調製のためのプロセス - Google Patents

結晶のリナグリプチン中間体およびリナグリプチンの調製のためのプロセス Download PDF

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Publication number
JP2020535193A
JP2020535193A JP2020517938A JP2020517938A JP2020535193A JP 2020535193 A JP2020535193 A JP 2020535193A JP 2020517938 A JP2020517938 A JP 2020517938A JP 2020517938 A JP2020517938 A JP 2020517938A JP 2020535193 A JP2020535193 A JP 2020535193A
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Prior art keywords
formula
linagliptin
reaction mass
linagliptin intermediate
intermediate represented
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Pending
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JP2020517938A
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English (en)
Japanese (ja)
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JP2020535193A5 (enExample
Inventor
パレ,ヴェンカタ,ラガヴェンドラチャリュル
ラジマヘンドラ,シャンムガサミー
チャンドレゴウダ,ダルシャン,ジャッカリ
ポンヌサミー,タンガラス
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Biocon Ltd
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Biocon Ltd
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Publication of JP2020535193A publication Critical patent/JP2020535193A/ja
Publication of JP2020535193A5 publication Critical patent/JP2020535193A5/ja
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/02Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • A61K31/522Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Emergency Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Endocrinology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2020517938A 2017-09-27 2018-09-27 結晶のリナグリプチン中間体およびリナグリプチンの調製のためのプロセス Pending JP2020535193A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN201741034292 2017-09-27
IN201741034292 2017-09-27
PCT/IB2018/057484 WO2019064214A1 (en) 2017-09-27 2018-09-27 INTERMEDIATE OF CRYSTALLINE LINAGLIPTIN AND PROCESS FOR THE PREPARATION OF LINAGLIPTIN

Publications (2)

Publication Number Publication Date
JP2020535193A true JP2020535193A (ja) 2020-12-03
JP2020535193A5 JP2020535193A5 (enExample) 2021-10-28

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JP2020517938A Pending JP2020535193A (ja) 2017-09-27 2018-09-27 結晶のリナグリプチン中間体およびリナグリプチンの調製のためのプロセス

Country Status (10)

Country Link
US (1) US11040974B2 (enExample)
JP (1) JP2020535193A (enExample)
KR (1) KR20200092946A (enExample)
CN (1) CN111511743A (enExample)
AU (1) AU2018343236A1 (enExample)
BR (1) BR112020005964A2 (enExample)
CA (1) CA3076980A1 (enExample)
MX (1) MX2020004050A (enExample)
RU (1) RU2020114890A (enExample)
WO (1) WO2019064214A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110684026A (zh) * 2019-10-24 2020-01-14 扬子江药业集团上海海尼药业有限公司 一种利格列汀的工业化制备方法
CN110872292B (zh) * 2019-11-30 2022-01-25 江苏君若药业有限公司 一条合成糖尿病药物利拉利汀的路线
EP4349837A1 (en) 2022-10-05 2024-04-10 Zaklady Farmaceutyczne "Polpharma" S.A. A pharmaceutical intermediate

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015011609A1 (en) * 2013-07-23 2015-01-29 Ranbaxy Laboratories Limited Process for the preparation of linagliptin and an intermediate thereof

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7407955B2 (en) 2002-08-21 2008-08-05 Boehringer Ingelheim Pharma Gmbh & Co., Kg 8-[3-amino-piperidin-1-yl]-xanthines, the preparation thereof and their use as pharmaceutical compositions
BRPI0711558A2 (pt) 2006-05-04 2011-11-08 Boeringer Ingelheim Internat Gmbh polimorfos
IN2013MU02055A (enExample) * 2013-06-18 2015-07-03 Cadila Healthcare Ltd

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015011609A1 (en) * 2013-07-23 2015-01-29 Ranbaxy Laboratories Limited Process for the preparation of linagliptin and an intermediate thereof

Also Published As

Publication number Publication date
CA3076980A1 (en) 2019-04-04
US11040974B2 (en) 2021-06-22
KR20200092946A (ko) 2020-08-04
AU2018343236A1 (en) 2020-05-14
MX2020004050A (es) 2020-11-06
RU2020114890A (ru) 2021-10-27
US20200354363A1 (en) 2020-11-12
WO2019064214A1 (en) 2019-04-04
BR112020005964A2 (pt) 2020-10-06
CN111511743A (zh) 2020-08-07

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