CN111511743A - 结晶的利拉利汀中间体及利拉利汀的制备方法 - Google Patents

结晶的利拉利汀中间体及利拉利汀的制备方法 Download PDF

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Publication number
CN111511743A
CN111511743A CN201880076836.6A CN201880076836A CN111511743A CN 111511743 A CN111511743 A CN 111511743A CN 201880076836 A CN201880076836 A CN 201880076836A CN 111511743 A CN111511743 A CN 111511743A
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China
Prior art keywords
formula
linagliptin
crystalline form
reaction mass
linagliptin intermediate
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Pending
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CN201880076836.6A
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English (en)
Chinese (zh)
Inventor
文卡塔·拉加文德拉查玉鲁·帕勒
山姆哈萨米·拉杰马亨德拉
达尔山·贾卡利·昌德雷古瓦达
唐加拉苏·蓬努萨米
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Biocon Ltd
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Biocon Ltd
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Publication date
Application filed by Biocon Ltd filed Critical Biocon Ltd
Publication of CN111511743A publication Critical patent/CN111511743A/zh
Pending legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
    • C07D473/06—Heterocyclic 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
    • 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
    • A61K31/52—Purines, e.g. adenine
    • A61K31/522—Purines, e.g. adenine having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
    • 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
    • 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)
  • 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)
CN201880076836.6A 2017-09-27 2018-09-27 结晶的利拉利汀中间体及利拉利汀的制备方法 Pending CN111511743A (zh)

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 (1)

Publication Number Publication Date
CN111511743A true CN111511743A (zh) 2020-08-07

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ID=65903063

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880076836.6A Pending CN111511743A (zh) 2017-09-27 2018-09-27 结晶的利拉利汀中间体及利拉利汀的制备方法

Country Status (10)

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

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
KR101452915B1 (ko) 2006-05-04 2014-10-21 베링거 인겔하임 인터내셔날 게엠베하 다형태
IN2013MU02055A (https=) * 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
KR20200092946A (ko) 2020-08-04
AU2018343236A1 (en) 2020-05-14
JP2020535193A (ja) 2020-12-03
RU2020114890A (ru) 2021-10-27
WO2019064214A1 (en) 2019-04-04
US20200354363A1 (en) 2020-11-12
CA3076980A1 (en) 2019-04-04
MX2020004050A (es) 2020-11-06
US11040974B2 (en) 2021-06-22
BR112020005964A2 (pt) 2020-10-06

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Application publication date: 20200807