CN115916781A - 1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(r)-氨基-哌啶-1-基)-黄嘌呤的晶型 - Google Patents

1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(r)-氨基-哌啶-1-基)-黄嘌呤的晶型 Download PDF

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Publication number
CN115916781A
CN115916781A CN202180042237.4A CN202180042237A CN115916781A CN 115916781 A CN115916781 A CN 115916781A CN 202180042237 A CN202180042237 A CN 202180042237A CN 115916781 A CN115916781 A CN 115916781A
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CN
China
Prior art keywords
methyl
crystalline form
powder
linagliptin
ray diffraction
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Pending
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CN202180042237.4A
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English (en)
Chinese (zh)
Inventor
田中祐未子
清水柚美华
翁长朝典
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Yuki Gosei Kogyo Co Ltd
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Yuki Gosei Kogyo Co Ltd
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Publication of CN115916781A publication Critical patent/CN115916781A/zh
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    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Diabetes (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Endocrinology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN202180042237.4A 2020-06-10 2021-06-10 1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(r)-氨基-哌啶-1-基)-黄嘌呤的晶型 Pending CN115916781A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
JP2020-101161 2020-06-10
JP2020101161 2020-06-10
JPPCT/JP2021/015338 2021-04-13
PCT/JP2021/015338 WO2021250995A1 (ja) 2020-06-10 2021-04-13 １－［（４－メチル－キナゾリン－２－イル）メチル］－３－メチル－７－（２－ブチン－１－イル）－８－（３－（ｒ）－アミノ－ピペリジン－１－イル）－キサンチンの結晶形態
PCT/JP2021/022157 WO2021251467A1 (ja) 2020-06-10 2021-06-10 １－［（４－メチル－キナゾリン－２－イル）メチル］－３－メチル－７－（２－ブチン－１－イル）－８－（３－（ｒ）－アミノ－ピペリジン－１－イル）－キサンチンの結晶形態

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Publication Number Publication Date
CN115916781A true CN115916781A (zh) 2023-04-04

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CN202180042237.4A Pending CN115916781A (zh) 2020-06-10 2021-06-10 1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(r)-氨基-哌啶-1-基)-黄嘌呤的晶型

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JP (2) JPWO2021251467A1 (https=)
CN (1) CN115916781A (https=)
WO (2) WO2021250995A1 (https=)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021250995A1 (ja) * 2020-06-10 2021-12-16 有機合成薬品工業株式会社 １－［（４－メチル－キナゾリン－２－イル）メチル］－３－メチル－７－（２－ブチン－１－イル）－８－（３－（ｒ）－アミノ－ピペリジン－１－イル）－キサンチンの結晶形態

Citations (13)

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CN101437823A (zh) * 2006-05-04 2009-05-20 贝林格尔.英格海姆国际有限公司 多晶型
US20130123282A1 (en) * 2011-11-16 2013-05-16 Leonid Metsger Solid state forms of linagliptin
WO2013128379A2 (en) * 2012-02-27 2013-09-06 Dr. Reddy's Laboratories Limited Crystalline polymorphic forms of linagliptin
CN103319483A (zh) * 2012-10-19 2013-09-25 药源药物化学（上海）有限公司 一种利拉列汀重要中间体的制备方法
CN105272982A (zh) * 2015-11-23 2016-01-27 齐鲁制药有限公司 利格列汀新晶型及其制备方法
CN106554354A (zh) * 2015-09-28 2017-04-05 四川科伦药物研究院有限公司 利格列汀或其类似物的中间体与利格列汀或其类似物的制备方法
CN108017638A (zh) * 2016-10-31 2018-05-11 江苏艾立康药业股份有限公司 一种利格列汀晶型的制备方法
CN108290891A (zh) * 2015-09-17 2018-07-17 韩美精密化学株式会社 一种利格列汀晶型及其制备方法
JP2018177769A (ja) * 2017-04-07 2018-11-15 イルドン ファーマシューティカル カンパニー リミテッド １−［（４−メチル−キナゾリン−２−イル）メチル］−３−メチル−７−（２−ブチン−１−イル）−８−（３−（ｒ）−アミノ−ピペリジン−１−イル）−キサンチンの新規結晶形及びその製造方法
CN109761983A (zh) * 2019-02-11 2019-05-17 深圳市第二人民医院 一种利格列汀的制备方法
CN110305131A (zh) * 2019-07-03 2019-10-08 山东百诺医药股份有限公司 利格列汀新晶型及其制备方法
CN110964013A (zh) * 2018-09-29 2020-04-07 甘李药业江苏有限公司 利格列汀及其中间体的制备方法
JP2020070296A (ja) * 2018-10-31 2020-05-07 ヤマサ醤油株式会社 リナグリプチンの製造法

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Publication number Priority date Publication date Assignee Title
EP1248869A2 (en) * 2000-01-07 2002-10-16 Transform Pharmaceuticals, Inc. High-throughput formation, identification, and analysis of diverse solid-forms
KR101804207B1 (ko) * 2015-12-29 2017-12-04 (주) 에프엔지리서치 무정형 리나글립틴의 제조 방법
CN107043376A (zh) * 2017-05-15 2017-08-15 珠海联邦制药股份有限公司 一种利格列汀新晶型及其制备方法
WO2021250995A1 (ja) * 2020-06-10 2021-12-16 有機合成薬品工業株式会社 １－［（４－メチル－キナゾリン－２－イル）メチル］－３－メチル－７－（２－ブチン－１－イル）－８－（３－（ｒ）－アミノ－ピペリジン－１－イル）－キサンチンの結晶形態

Patent Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101437823A (zh) * 2006-05-04 2009-05-20 贝林格尔.英格海姆国际有限公司 多晶型
US20130123282A1 (en) * 2011-11-16 2013-05-16 Leonid Metsger Solid state forms of linagliptin
WO2013128379A2 (en) * 2012-02-27 2013-09-06 Dr. Reddy's Laboratories Limited Crystalline polymorphic forms of linagliptin
CN103319483A (zh) * 2012-10-19 2013-09-25 药源药物化学（上海）有限公司 一种利拉列汀重要中间体的制备方法
CN108290891A (zh) * 2015-09-17 2018-07-17 韩美精密化学株式会社 一种利格列汀晶型及其制备方法
CN106554354A (zh) * 2015-09-28 2017-04-05 四川科伦药物研究院有限公司 利格列汀或其类似物的中间体与利格列汀或其类似物的制备方法
CN105272982A (zh) * 2015-11-23 2016-01-27 齐鲁制药有限公司 利格列汀新晶型及其制备方法
CN108017638A (zh) * 2016-10-31 2018-05-11 江苏艾立康药业股份有限公司 一种利格列汀晶型的制备方法
JP2018177769A (ja) * 2017-04-07 2018-11-15 イルドン ファーマシューティカル カンパニー リミテッド １−［（４−メチル−キナゾリン−２−イル）メチル］−３−メチル−７−（２−ブチン−１−イル）−８−（３−（ｒ）−アミノ−ピペリジン−１−イル）−キサンチンの新規結晶形及びその製造方法
CN110964013A (zh) * 2018-09-29 2020-04-07 甘李药业江苏有限公司 利格列汀及其中间体的制备方法
JP2020070296A (ja) * 2018-10-31 2020-05-07 ヤマサ醤油株式会社 リナグリプチンの製造法
CN109761983A (zh) * 2019-02-11 2019-05-17 深圳市第二人民医院 一种利格列汀的制备方法
CN110305131A (zh) * 2019-07-03 2019-10-08 山东百诺医药股份有限公司 利格列汀新晶型及其制备方法

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WO2021251467A1 (ja) 2021-12-16
JPWO2021251467A1 (https=) 2021-12-16
JP2025069332A (ja) 2025-04-30

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