CN103596954B - 苯甲酸利拉利汀的多晶型物 - Google Patents

苯甲酸利拉利汀的多晶型物 Download PDF

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Publication number
CN103596954B
CN103596954B CN201280028478.4A CN201280028478A CN103596954B CN 103596954 B CN103596954 B CN 103596954B CN 201280028478 A CN201280028478 A CN 201280028478A CN 103596954 B CN103596954 B CN 103596954B
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CN
China
Prior art keywords
linagliptin benzoate
linagliptin
pharmaceutical composition
benzoate
crystalline form
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.)
Expired - Fee Related
Application number
CN201280028478.4A
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English (en)
Chinese (zh)
Other versions
CN103596954A (zh
Inventor
A·霍特
A·皮希勒
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.)
Sandoz AG
Original Assignee
Sandoz AG
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Filing date
Publication date
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Publication of CN103596954A publication Critical patent/CN103596954A/zh
Application granted granted Critical
Publication of CN103596954B publication Critical patent/CN103596954B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • 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
    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN201280028478.4A 2011-05-10 2012-05-09 苯甲酸利拉利汀的多晶型物 Expired - Fee Related CN103596954B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11165597.3 2011-05-10
EP11165597 2011-05-10
PCT/EP2012/058556 WO2012152837A1 (en) 2011-05-10 2012-05-09 Polymorph of linagliptin benzoate

Publications (2)

Publication Number Publication Date
CN103596954A CN103596954A (zh) 2014-02-19
CN103596954B true CN103596954B (zh) 2016-10-26

Family

ID=44227877

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201280028478.4A Expired - Fee Related CN103596954B (zh) 2011-05-10 2012-05-09 苯甲酸利拉利汀的多晶型物

Country Status (9)

Country Link
US (1) US8785455B2 (https=)
EP (1) EP2707368B1 (https=)
JP (1) JP6028016B2 (https=)
CN (1) CN103596954B (https=)
AU (1) AU2012252380B2 (https=)
CA (1) CA2835332C (https=)
EA (1) EA023330B1 (https=)
SI (1) SI2707368T1 (https=)
WO (1) WO2012152837A1 (https=)

Families Citing this family (25)

* 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
DE102004054054A1 (de) 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine
KR101452915B1 (ko) 2006-05-04 2014-10-21 베링거 인겔하임 인터내셔날 게엠베하 다형태
PE20110235A1 (es) 2006-05-04 2011-04-14 Boehringer Ingelheim Int Combinaciones farmaceuticas que comprenden linagliptina y metmorfina
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
PE20091730A1 (es) 2008-04-03 2009-12-10 Boehringer Ingelheim Int Formulaciones que comprenden un inhibidor de dpp4
KR20190016601A (ko) 2008-08-06 2019-02-18 베링거 인겔하임 인터내셔날 게엠베하 메트포르민 요법이 부적합한 환자에서의 당뇨병 치료
US20200155558A1 (en) 2018-11-20 2020-05-21 Boehringer Ingelheim International Gmbh Treatment for diabetes in patients with insufficient glycemic control despite therapy with an oral antidiabetic drug
JP2012512848A (ja) 2008-12-23 2012-06-07 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 有機化合物の塩の形態
KR20240090632A (ko) 2009-11-27 2024-06-21 베링거 인겔하임 인터내셔날 게엠베하 리나글립틴과 같은 ｄｐｐ－ｉｖ 억제제를 사용한 유전자형 검사된 당뇨병 환자의 치료
CA3070513C (en) 2010-05-05 2023-01-03 Boehringer Ingelheim International Gmbh A dpp-4 inhibitor for use in treatment of skin-alterations or necrosis
KR20130093012A (ko) 2010-06-24 2013-08-21 베링거 인겔하임 인터내셔날 게엠베하 당뇨병 요법
AR083878A1 (es) 2010-11-15 2013-03-27 Boehringer Ingelheim Int Terapia antidiabetica vasoprotectora y cardioprotectora, linagliptina, metodo de tratamiento
DK2731947T3 (en) 2011-07-15 2019-04-23 Boehringer Ingelheim Int SUBSTITUTED DIMERIC QUINAZOLINE DERIVATIVE, PREPARATION AND USE thereof IN PHARMACEUTICAL COMPOSITIONS FOR TREATMENT OF TYPE I AND TYPE II DIABETES
US9555001B2 (en) 2012-03-07 2017-01-31 Boehringer Ingelheim International Gmbh Pharmaceutical composition and uses thereof
WO2013171167A1 (en) 2012-05-14 2013-11-21 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in the treatment of podocytes related disorders and/or nephrotic syndrome
WO2013171166A1 (en) 2012-05-14 2013-11-21 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp-4 inhibitor for use in the treatment of sirs and/or sepsis
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
EP3110449B1 (en) 2014-02-28 2023-06-28 Boehringer Ingelheim International GmbH Medical use of a dpp-4 inhibitor
CN105712995B (zh) * 2014-12-05 2017-11-03 浙江京新药业股份有限公司 一种利格列汀的纯化方法
KR102442536B1 (ko) * 2015-09-17 2022-09-13 한미정밀화학주식회사 리나글립틴 결정형 및 이의 제조방법
AU2016335082A1 (en) 2015-10-09 2018-04-12 Hexal Ag Pharmaceutical composition containing 8-[(3R)-3-amino-1-piperidinyl]-7-(2-butyn-1-yl)-3,7-dihydro-3-methyl-1-[4-methyl-2-quinazolinyl)methyl]-1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof
EP4233840A3 (en) 2016-06-10 2023-10-18 Boehringer Ingelheim International GmbH Combinations of linagliptin and metformin
CN106543180B (zh) * 2016-10-28 2018-03-30 南京正大天晴制药有限公司 苯甲酸利格列汀晶型及其制备方法
US20210313015A1 (en) * 2018-08-21 2021-10-07 Towa Pharmaceutical Co., Ltd. Specifically-shaped crystal of compound and method for producing same

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010072776A1 (en) * 2008-12-23 2010-07-01 Boehringer Ingelheim International Gmbh Salt forms of organic compound

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1532149B9 (de) 2002-08-21 2011-04-20 Boehringer Ingelheim Pharma GmbH & Co. KG 8-[3-amino-piperidin-1-yl] -xanthine, deren herstellung und deren verwendung als arzneimittel
DE102004054054A1 (de) * 2004-11-05 2006-05-11 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verfahren zur Herstellung chiraler 8-(3-Amino-piperidin-1-yl)-xanthine
EP1852108A1 (en) 2006-05-04 2007-11-07 Boehringer Ingelheim Pharma GmbH & Co.KG DPP IV inhibitor formulations
KR101452915B1 (ko) 2006-05-04 2014-10-21 베링거 인겔하임 인터내셔날 게엠베하 다형태
PE20090938A1 (es) * 2007-08-16 2009-08-08 Boehringer Ingelheim Int Composicion farmaceutica que comprende un derivado de benceno sustituido con glucopiranosilo
US8835472B2 (en) * 2010-09-02 2014-09-16 Boehringer Ingelheim International Gmbh Compounds, pharmaceutical compositions and uses thereof

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010072776A1 (en) * 2008-12-23 2010-07-01 Boehringer Ingelheim International Gmbh Salt forms of organic compound

Also Published As

Publication number Publication date
CA2835332A1 (en) 2012-11-15
US20140121225A1 (en) 2014-05-01
EA201301240A1 (ru) 2014-04-30
AU2012252380A1 (en) 2013-11-28
WO2012152837A1 (en) 2012-11-15
EA023330B1 (ru) 2016-05-31
CA2835332C (en) 2019-03-26
JP2014513143A (ja) 2014-05-29
AU2012252380B2 (en) 2016-09-08
US8785455B2 (en) 2014-07-22
CN103596954A (zh) 2014-02-19
SI2707368T1 (sl) 2016-04-29
JP6028016B2 (ja) 2016-11-16
EP2707368A1 (en) 2014-03-19
EP2707368B1 (en) 2016-02-03

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Granted publication date: 20161026

CF01 Termination of patent right due to non-payment of annual fee