CN106946886A - 二肽基肽酶‑iv抑制剂的新晶形 - Google Patents

二肽基肽酶‑iv抑制剂的新晶形 Download PDF

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Publication number
CN106946886A
CN106946886A CN201610882581.5A CN201610882581A CN106946886A CN 106946886 A CN106946886 A CN 106946886A CN 201610882581 A CN201610882581 A CN 201610882581A CN 106946886 A CN106946886 A CN 106946886A
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CN
China
Prior art keywords
crystalline form
difluorophenyl
pyran
methylsulfonyl
dihydropyrrolo
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.)
Pending
Application number
CN201610882581.5A
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English (en)
Chinese (zh)
Inventor
I.阿罗由
D.克吕格尔
P.陈
A.莫门特
T.比夫图
F.希恩
Y.张
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.)
Organon Pharma UK Ltd
Merck Sharp and Dohme LLC
Original Assignee
Merck Sharp and Dohme Ltd
Schering Corp
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Filing date
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Application filed by Merck Sharp and Dohme Ltd, Schering Corp filed Critical Merck Sharp and Dohme Ltd
Publication of CN106946886A publication Critical patent/CN106946886A/zh
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)
  • 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)
CN201610882581.5A 2011-06-29 2012-06-25 二肽基肽酶‑iv抑制剂的新晶形 Pending CN106946886A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161502497P 2011-06-29 2011-06-29
US61/502497 2011-06-29
CN201280032077.6A CN103987388A (zh) 2011-06-29 2012-06-25 二肽基肽酶-iv抑制剂的新晶形

Related Parent Applications (1)

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Publications (1)

Publication Number Publication Date
CN106946886A true CN106946886A (zh) 2017-07-14

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CN201610882581.5A Pending CN106946886A (zh) 2011-06-29 2012-06-25 二肽基肽酶‑iv抑制剂的新晶形
CN201280032077.6A Pending CN103987388A (zh) 2011-06-29 2012-06-25 二肽基肽酶-iv抑制剂的新晶形
CN201280032105.4A Pending CN103702562A (zh) 2011-06-29 2012-06-25 用于制备手性二肽基肽酶-iv抑制剂的方法

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CN201280032077.6A Pending CN103987388A (zh) 2011-06-29 2012-06-25 二肽基肽酶-iv抑制剂的新晶形
CN201280032105.4A Pending CN103702562A (zh) 2011-06-29 2012-06-25 用于制备手性二肽基肽酶-iv抑制剂的方法

Country Status (12)

Country Link
US (4) US8895603B2 (enExample)
EP (2) EP2726075A4 (enExample)
JP (4) JP5873554B2 (enExample)
KR (2) KR20140034862A (enExample)
CN (3) CN106946886A (enExample)
AR (1) AR089554A1 (enExample)
AU (2) AU2012275638A1 (enExample)
CA (2) CA2838738A1 (enExample)
MX (2) MX2013014892A (enExample)
RU (2) RU2014102764A (enExample)
TW (1) TWI574965B (enExample)
WO (2) WO2013003249A1 (enExample)

Cited By (2)

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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
CN111793071A (zh) * 2020-07-06 2020-10-20 四川凯科医药科技有限公司 奥格列汀的合成工艺

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WO2013122920A1 (en) 2012-02-17 2013-08-22 Merck Sharp & Dohme Corp. Dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
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WO2014018355A1 (en) 2012-07-23 2014-01-30 Merck Sharp & Dohme Corp. Treating diabetes with dipeptidyl peptidase-iv inhibitors
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US9937153B2 (en) 2013-08-30 2018-04-10 Merck Sharp & Dohme Ltd. Oral pharmaceutical formulation of omarigliptin
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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
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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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
EP3181565A1 (en) 2015-12-18 2017-06-21 Sandoz Ag Crystalline omarigliptin salts
EP3395819B1 (en) * 2015-12-25 2023-05-31 Sichuan Haisco Pharmaceutical Co., Ltd. Crystal form of substituted aminopyran derivative
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
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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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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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