JP5873554B2 - 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 - Google Patents

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 Download PDF

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Publication number
JP5873554B2
JP5873554B2 JP2014518880A JP2014518880A JP5873554B2 JP 5873554 B2 JP5873554 B2 JP 5873554B2 JP 2014518880 A JP2014518880 A JP 2014518880A JP 2014518880 A JP2014518880 A JP 2014518880A JP 5873554 B2 JP5873554 B2 JP 5873554B2
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JP
Japan
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compound
formula
formula iii
added
pyrazolopyrrolidine
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JP2014518880A
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English (en)
Japanese (ja)
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JP2014520802A (ja
Inventor
ザクト，マイケル，ジエイ
ダン，ロバート，エフ
モーメント，アーロン，ジエイ
ジエイニー，ジエイコブ，エム
リーバーマン，デイビツド
シーン，フエイ
ブレマイヤー，ナデイン
スコツト，ジエレミー
クーテ，ジエフリー，テイー
タン，ルシ
チエン，チンハオ
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
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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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (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)
JP2014518880A 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 Active JP5873554B2 (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/US2012/043924 WO2013003250A1 (en) 2011-06-29 2012-06-25 Process for preparing chiral dipeptidyl peptidase-iv inhibitors

Publications (2)

Publication Number Publication Date
JP2014520802A JP2014520802A (ja) 2014-08-25
JP5873554B2 true JP5873554B2 (ja) 2016-03-01

Family

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Family Applications (4)

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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
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
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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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
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)

Country Link
US (4) US8895603B2 (enExample)
EP (2) EP2725905A4 (enExample)
JP (4) JP5873554B2 (enExample)
KR (2) KR20140034861A (enExample)
CN (3) CN103987388A (enExample)
AR (1) AR089554A1 (enExample)
AU (2) AU2012275637B2 (enExample)
CA (2) CA2838748A1 (enExample)
MX (2) MX2013014892A (enExample)
RU (2) RU2014102764A (enExample)
TW (1) TWI574965B (enExample)
WO (2) WO2013003249A1 (enExample)

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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
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CN106660981B (zh) * 2014-07-29 2019-06-25 广东东阳光药业有限公司 2,3-二取代-5-氧代吡喃化合物的制备方法
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
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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
CN109874304B (zh) * 2016-08-12 2021-06-25 正大天晴药业集团股份有限公司 Dpp-iv长效抑制剂的结晶及其盐
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
KR102599958B1 (ko) * 2016-09-28 2023-11-09 (주)아모레퍼시픽 (r)-n-[4-(1-아미노-에틸)-2,6-다이플루오로-페닐]-메테인설폰아마이드의 제조방법
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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US12122778B2 (en) 2018-09-19 2024-10-22 Novo Nordisk Health Care Ag Activating pyruvate kinase R
CN113166060B (zh) 2018-09-19 2024-01-09 诺沃挪第克健康护理股份公司 用丙酮酸激酶激活化合物治疗镰状细胞病
CN113831266B (zh) * 2019-01-22 2024-04-05 河南医学高等专科学校 1-(2,5-二氟苯基)-1-氧代戊-4-炔-2-基氨基甲酸烷基酯的合成
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