JP2014518266A - ジペプチジルペプチダーゼ−ｉｖ阻害剤の新規結晶形 - Google Patents

ジペプチジルペプチダーゼ−ｉｖ阻害剤の新規結晶形 Download PDF

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JP2014518266A
JP2014518266A JP2014518879A JP2014518879A JP2014518266A JP 2014518266 A JP2014518266 A JP 2014518266A JP 2014518879 A JP2014518879 A JP 2014518879A JP 2014518879 A JP2014518879 A JP 2014518879A JP 2014518266 A JP2014518266 A JP 2014518266A
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difluorophenyl
crystalline
pyran
methylsulfonyl
dihydropyrrolo
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JP2014518879A
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Japanese (ja)
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JP2014518266A5 (enExample
Inventor
アローヨ，イツツイア
クルーガー，ダビダ
チエン，ピーン
モーメント，アーロン
ビフツ，テスフエイ
シーン，フエイ
ジヤーン，ヤンフェーン
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
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Publication of JP2014518266A publication Critical patent/JP2014518266A/ja
Publication of JP2014518266A5 publication Critical patent/JP2014518266A5/ja
Pending legal-status Critical Current

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    • 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
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/12—Antihypertensives
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4162—1,2-Diazoles condensed with heterocyclic ring 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2014518879A 2011-06-29 2012-06-25 ジペプチジルペプチダーゼ−ｉｖ阻害剤の新規結晶形 Pending JP2014518266A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161502497P 2011-06-29 2011-06-29
US61/502,497 2011-06-29
PCT/US2012/043922 WO2013003249A1 (en) 2011-06-29 2012-06-25 Novel crystalline forms of a dipeptidyl peptidase-iv inhibitor

Related Child Applications (1)

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JP2016198829A Division JP2017039752A (ja) 2011-06-29 2016-10-07 ジペプチジルペプチダーゼ−ｉｖ阻害剤の新規結晶形

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JP2014518266A true JP2014518266A (ja) 2014-07-28
JP2014518266A5 JP2014518266A5 (enExample) 2015-05-21

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JP2014518879A Pending JP2014518266A (ja) 2011-06-29 2012-06-25 ジペプチジルペプチダーゼ−ｉｖ阻害剤の新規結晶形
JP2014518880A Active JP5873554B2 (ja) 2011-06-29 2012-06-25 キラルジペプチジルペプチダーゼ−ｉｖ阻害剤の調製プロセス
JP2016198829A Pending JP2017039752A (ja) 2011-06-29 2016-10-07 ジペプチジルペプチダーゼ−ｉｖ阻害剤の新規結晶形
JP2018055962A Withdrawn JP2018115191A (ja) 2011-06-29 2018-03-23 ジペプチジルペプチダーゼ−ｉｖ阻害剤の新規結晶形

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JP2014518880A Active JP5873554B2 (ja) 2011-06-29 2012-06-25 キラルジペプチジルペプチダーゼ−ｉｖ阻害剤の調製プロセス
JP2016198829A Pending JP2017039752A (ja) 2011-06-29 2016-10-07 ジペプチジルペプチダーゼ−ｉｖ阻害剤の新規結晶形
JP2018055962A Withdrawn JP2018115191A (ja) 2011-06-29 2018-03-23 ジペプチジルペプチダーゼ−ｉｖ阻害剤の新規結晶形

Country Status (12)

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US (4) US8895603B2 (enExample)
EP (2) EP2725905A4 (enExample)
JP (4) JP2014518266A (enExample)
KR (2) KR20140034862A (enExample)
CN (3) CN103987388A (enExample)
AR (1) AR089554A1 (enExample)
AU (2) AU2012275638A1 (enExample)
CA (2) CA2838738A1 (enExample)
MX (2) MX341299B (enExample)
RU (2) RU2598072C2 (enExample)
TW (1) TWI574965B (enExample)
WO (2) WO2013003250A1 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
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JP2019500371A (ja) * 2015-12-25 2019-01-10 スーチュアン ハイスーク ファーマシューティカル カンパニー リミテッド 置換アミノピラン誘導体の結晶形
JP2019527708A (ja) * 2016-08-12 2019-10-03 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッドChia Tai Tianqing Pharmaceutical Group Co., Ltd. Ｄｐｐ−ｉｖ長時間作用型阻害剤の結晶及びその塩
JP2019529480A (ja) * 2016-09-28 2019-10-17 アモーレパシフィック コーポレーションＡｍｏｒｅｐａｃｉｆｉｃ Ｃｏｒｐｏｒａｔｉｏｎ （ｒ）−ｎ−［４−（１−アミノ−エチル）−２，６−ジフルオロ−フェニル］−メタンスルホンアミドの製造方法

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US8895603B2 (en) 2011-06-29 2014-11-25 Merck Sharp & Dohme Corp. Crystalline forms of a dipeptidyl peptidase-IV inhibitor
US9073930B2 (en) 2012-02-17 2015-07-07 Merck Sharp & Dohme Dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
WO2014018355A1 (en) 2012-07-23 2014-01-30 Merck Sharp & Dohme Corp. Treating diabetes with dipeptidyl peptidase-iv inhibitors
EP2874622A4 (en) 2012-07-23 2015-12-30 Merck Sharp & Dohme TREATMENT OF DIABETES WITH DIPEPTIDYLPEPTIDASE IV INHIBITORS
TWI500613B (zh) 2012-10-17 2015-09-21 Cadila Healthcare Ltd 新穎之雜環化合物
US9937153B2 (en) 2013-08-30 2018-04-10 Merck Sharp & Dohme Ltd. Oral pharmaceutical formulation of omarigliptin
ES2587585T3 (es) * 2014-03-20 2016-10-25 F.I.S.- Fabbrica Italiana Sintetici S.P.A. Procedimiento para la preparación de intermedios clave de omarigliptina
CN105037367A (zh) * 2014-04-18 2015-11-11 四川海思科制药有限公司 氨基六元环类衍生物及其在医药上的应用
CN105085528A (zh) * 2014-05-15 2015-11-25 成都贝斯凯瑞生物科技有限公司 作为二肽基肽酶-iv抑制剂的氨基四氢吡喃衍生物
JP6574474B2 (ja) * 2014-07-21 2019-09-11 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． キラルジペプチジルペプチダーゼ−ｉｖ阻害剤の製造方法
WO2016015596A1 (en) * 2014-07-29 2016-02-04 Sunshine Lake Pharma Co., Ltd. Process for preparing 2, 3-disubstituted-5-oxopyran compound
CN106316888B (zh) * 2015-06-29 2018-05-18 深圳翰宇药业股份有限公司 一种手性氨基吡喃酮类化合物的合成方法
WO2017032705A1 (en) 2015-08-25 2017-03-02 Sandoz Ag Crystalline form of omarigliptin
CN105130995B (zh) * 2015-09-09 2017-08-11 杭州成邦医药科技有限公司 吡咯酮类化合物及其制备方法和应用
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CN105348286B (zh) * 2015-11-25 2018-12-18 中山奕安泰医药科技有限公司 一种2-甲基磺酰基-2,4,5,6-四氢吡咯[3，4-c]吡唑苯磺酸盐的制备方法
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CN105399744B (zh) * 2015-12-17 2017-07-18 黄燕鸽 一种奥格列汀的合成方法
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CN106928228B (zh) * 2015-12-29 2019-08-30 杭州普晒医药科技有限公司 奥格列汀盐及其晶型、它们的制备方法和药物组合物
CN107652291B (zh) * 2016-07-26 2020-07-14 中国科学院上海药物研究所 一种制备手性四氢吡喃衍生物的方法
CN107793389B (zh) * 2016-09-05 2021-06-29 中国科学院上海药物研究所 手性四氢吡喃衍生物及其制备与用途
CN106674227B (zh) * 2016-12-06 2019-03-19 上海博志研新药物技术有限公司 一种奥格列汀及其中间体的制备方法
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EP3335701A1 (en) 2016-12-16 2018-06-20 Hexal AG Pharmaceutical composition comprising omarigliptin
EP3335703A1 (en) 2016-12-16 2018-06-20 Hexal AG Pharmaceutical composition comprising omarigliptin
SMT201900517T1 (it) 2017-03-20 2019-11-13 Forma Therapeutics Inc Composizioni di pirrolopirrolo come attivatori di piruvato chinasi (pkr)
US11001588B2 (en) 2018-09-19 2021-05-11 Forma Therapeutics, Inc. Activating pyruvate kinase R and mutants thereof
US12053458B2 (en) 2018-09-19 2024-08-06 Novo Nordisk Health Care Ag Treating sickle cell disease with a pyruvate kinase R activating compound
CN109651203B (zh) * 2019-01-22 2021-10-15 河南医学高等专科学校 Dp-iv抑制剂奥格列汀中间体的制备方法
CN110453177A (zh) * 2019-08-06 2019-11-15 太仓碧奇新材料研发有限公司 一种柔性有机整流器的制备方法
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