CA2838748A1 - Process for preparing chiral dipeptidyl peptidase-iv inhibitors - Google Patents

Process for preparing chiral dipeptidyl peptidase-iv inhibitors Download PDF

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Publication number
CA2838748A1
CA2838748A1 CA2838748A CA2838748A CA2838748A1 CA 2838748 A1 CA2838748 A1 CA 2838748A1 CA 2838748 A CA2838748 A CA 2838748A CA 2838748 A CA2838748 A CA 2838748A CA 2838748 A1 CA2838748 A1 CA 2838748A1
Authority
CA
Canada
Prior art keywords
formula
compound
formula iii
solvent
base
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.)
Abandoned
Application number
CA2838748A
Other languages
English (en)
French (fr)
Inventor
Michael Zacuto
Robert F. Dunn
Aaron J. Moment
Jacob M. Janey
David Lieberman
Faye SHEEN
Nadine Bremeyer
Jeremy Scott
Jeffrey T. Kuethe
Lushi Tan
Qinghao Chen
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
Merck Sharp and Dohme LLC
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Merck Sharp and Dohme Ltd, Merck Sharp and Dohme LLC filed Critical Merck Sharp and Dohme Ltd
Publication of CA2838748A1 publication Critical patent/CA2838748A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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

Landscapes

  • 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)
CA2838748A 2011-06-29 2012-06-25 Process for preparing chiral dipeptidyl peptidase-iv inhibitors Abandoned CA2838748A1 (en)

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 (1)

Publication Number Publication Date
CA2838748A1 true CA2838748A1 (en) 2013-01-03

Family

ID=47424494

Family Applications (2)

Application Number Title Priority Date Filing Date
CA2838748A Abandoned CA2838748A1 (en) 2011-06-29 2012-06-25 Process for preparing chiral dipeptidyl peptidase-iv inhibitors
CA2838738A Abandoned CA2838738A1 (en) 2011-06-29 2012-06-25 Novel crystalline forms of a dipeptidyl peptidase-iv inhibitor

Family Applications After (1)

Application Number Title Priority Date Filing Date
CA2838738A Abandoned CA2838738A1 (en) 2011-06-29 2012-06-25 Novel crystalline forms of a dipeptidyl peptidase-iv inhibitor

Country Status (12)

Country Link
US (4) US8895603B2 (enExample)
EP (2) EP2726075A4 (enExample)
JP (4) JP5873554B2 (enExample)
KR (2) KR20140034861A (enExample)
CN (3) CN106946886A (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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EP2726075A4 (en) * 2011-06-29 2014-11-19 Merck Sharp & Dohme NEW CRYSTALLINE FORMS OF A DIPEPTIDYL-PEPTIDASE IV HEMMER
US9073930B2 (en) 2012-02-17 2015-07-07 Merck Sharp & Dohme Dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
US9315508B2 (en) 2012-07-23 2016-04-19 Merck Sharp & Dohme Corp. Treating diabetes with dipeptidyl peptidase-IV inhibitors
WO2014018355A1 (en) 2012-07-23 2014-01-30 Merck Sharp & Dohme Corp. Treating diabetes with dipeptidyl peptidase-iv inhibitors
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CN105392772B (zh) * 2014-03-20 2017-09-15 意大利合成制造有限公司 奥格列汀的关键中间体的制备方法
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
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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
WO2017081590A1 (en) * 2015-11-09 2017-05-18 Sun Pharmaceutical Industries Limited Process for the preparation of omarigliptin
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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CN106916157A (zh) * 2015-12-25 2017-07-04 四川海思科制药有限公司 取代的氨基吡喃衍生物的晶型
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
RU2753335C9 (ru) * 2016-08-12 2021-09-20 Чиа Тай Тянцин Фармасьютикал Груп Ко., Лтд. Кристалл ингибитора DPP-IV длительного действия и его соли
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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