RU2014102764A - Способ получения хиральных ингибиторов дипептидилпептидазы iv - Google Patents

Способ получения хиральных ингибиторов дипептидилпептидазы iv Download PDF

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RU2014102764A
RU2014102764A RU2014102764/04A RU2014102764A RU2014102764A RU 2014102764 A RU2014102764 A RU 2014102764A RU 2014102764/04 A RU2014102764/04 A RU 2014102764/04A RU 2014102764 A RU2014102764 A RU 2014102764A RU 2014102764 A RU2014102764 A RU 2014102764A
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compound
formula
formula iii
base
solvent
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RU2014102764/04A
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English (en)
Russian (ru)
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Майкл Дж. ЗАКУТО
Роберт Ф. ДАНН
Аарон Дж. МОМЕНТ
Джейкоб М. ДЖЕЙНИ
Дэвид ЛИБЕРМАН
Фэй ШИН
Надин Бремейер
Джереми СКОТТ
Джеффри Т. КУТ
Луши ТАНЬ
Цинхао ЧЭНЬ
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Мерк Шарп И Доум Корп.
Мерк Шарп И Доум Лтд.
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Publication of RU2014102764A publication Critical patent/RU2014102764A/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles condensed with heterocyclic ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design 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)
RU2014102764/04A 2011-06-29 2012-06-25 Способ получения хиральных ингибиторов дипептидилпептидазы iv RU2014102764A (ru)

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

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RU2014102764A true RU2014102764A (ru) 2015-08-10

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RU2014102764/04A RU2014102764A (ru) 2011-06-29 2012-06-25 Способ получения хиральных ингибиторов дипептидилпептидазы iv
RU2014102773/04A RU2598072C2 (ru) 2011-06-29 2012-06-25 Новые кристаллические формы ингибиторов дипептидилпептидазы-iv

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US (4) US9187488B2 (enExample)
EP (2) EP2726075A4 (enExample)
JP (4) JP2014518266A (enExample)
KR (2) KR20140034861A (enExample)
CN (3) CN103702562A (enExample)
AR (1) AR089554A1 (enExample)
AU (2) AU2012275638A1 (enExample)
CA (2) CA2838738A1 (enExample)
MX (2) MX341299B (enExample)
RU (2) RU2014102764A (enExample)
TW (1) TWI574965B (enExample)
WO (2) WO2013003249A1 (enExample)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2012275638A1 (en) 2011-06-29 2013-11-14 Merck Sharp & Dohme Corp. Process for preparing chiral dipeptidyl peptidase-IV inhibitors
US9073930B2 (en) 2012-02-17 2015-07-07 Merck Sharp & Dohme Dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
EP2874626A4 (en) 2012-07-23 2016-03-23 Merck Sharp & Dohme TREATMENT OF DIABETES WITH DIPEPTIDYLPEPTIDASE IV INHIBITORS
WO2014018350A1 (en) 2012-07-23 2014-01-30 Merck Sharp & Dohme Corp. Treating diabetes with dipeptidyl peptidase-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
EP2997008B1 (en) * 2014-03-20 2016-06-29 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Process for the preparation of key intermediates of omarigliptin
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
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
WO2017093209A1 (en) 2015-12-03 2017-06-08 F.I.S. - Fabbrica Italiana Sintetici S.P.A. Process for preparing aminotetrahydropyrans
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
CN107849051B (zh) * 2015-12-25 2020-11-13 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
US10822319B2 (en) * 2016-08-12 2020-11-03 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Crystal of DPP-IV long-acting inhibitor and salt
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
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
EP3335704A1 (en) 2016-12-16 2018-06-20 Hexal AG Pharmaceutical composition comprising omarigliptin
PT3448859T (pt) 2017-03-20 2019-10-25 Forma Therapeutics Inc Composições de pirrolopirrole como ativadores de piruvato quinase (pkr).
ES2989438T3 (es) 2018-09-19 2024-11-26 Novo Nordisk Healthcare Ag Activación de la piruvato cinasa R
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
CN114615977B (zh) 2019-09-19 2025-01-14 诺沃挪第克健康护理股份公司 丙酮酸激酶r(pkr)活化组合物
CN111793071B (zh) * 2020-07-06 2021-06-04 四川凯科医药科技有限公司 奥格列汀的合成工艺
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R

Family Cites Families (55)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5041442A (en) 1990-07-31 1991-08-20 Syntex (U.S.A.) Inc. Pyrrolo(1,2-a)pyrazines as inhibitors of gastric acid secretion
NZ337164A (en) * 1997-03-21 2001-05-25 Du Pont Pharm Co Method of preparing 4-arylamino-1-alkyl-[1,2,3]-triazolo][4,5-c]pyridine derivatives
PA8474101A1 (es) * 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
CN1243707C (zh) 2000-09-14 2006-03-01 国家海洋局第一海洋研究所 共轭亚油酸的制造方法
ATE395912T1 (de) 2001-03-27 2008-06-15 Merck & Co Inc Dipeptidylpeptidase-hemmer für die behandlung oder prävention von diabetes
CA2450475A1 (en) 2001-06-20 2003-01-03 Linda Brockunier Dipeptidyl peptidase inhibitors for the treatment of diabetes
JP2004535433A (ja) 2001-06-20 2004-11-25 メルク エンド カムパニー インコーポレーテッド 糖尿病治療用のジペプチジルペプチダーゼ阻害薬
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
CN1212303C (zh) 2001-12-31 2005-07-27 中国科学院新疆理化技术研究所 使用混合溶剂合成共轭亚油酸的方法
US7307164B2 (en) 2002-03-25 2007-12-11 Merck & Co., Inc. β-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
DE60330485D1 (de) 2002-07-15 2010-01-21 Merck & Co Inc Zur behandlung von diabetes
EP1554280B1 (en) 2002-10-07 2007-08-15 Merck & Co., Inc. Antidiabetic beta-amino heterocyclic dipeptidyl peptidase inhibitors
PL216527B1 (pl) 2002-10-18 2014-04-30 Merck & Co Inc Związki ß-aminoheterocykliczne i kompozycja farmaceutyczna
EP1562925B1 (en) 2002-11-07 2007-01-03 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
CA2508487A1 (en) 2002-12-04 2004-06-17 Merck & Co., Inc. Phenylalanine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
EP1583534A4 (en) 2002-12-20 2007-08-29 Merck & Co Inc 3-AMINO-4-PHENYLBUTANIC ACID DERIVATIVES AS DIPEPTIDYL-PEPTIDASE INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
CA2512546A1 (en) 2003-01-17 2004-08-05 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
CA2513684A1 (en) 2003-01-31 2004-08-19 Merck & Co., Inc. 3-amino-4-phenylbutanoic acid derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
ATE441994T1 (de) * 2003-04-03 2009-09-15 Nokia Corp Verwaltung von kontext-bezogener information mit einer mobilstation
CN1787823A (zh) 2003-05-14 2006-06-14 麦克公司 作为二肽基肽酶抑制剂用于治疗或预防糖尿病的3-氨基-4-苯基丁酸衍生物
CN1798556A (zh) 2003-06-06 2006-07-05 麦克公司 作为治疗或者预防糖尿病的二肽基肽酶抑制剂的稠合吲哚
WO2004112701A2 (en) 2003-06-17 2004-12-29 Merck & Co., Inc. Cyclohexylglycine derivatives as dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes
JO2625B1 (en) * 2003-06-24 2011-11-01 ميرك شارب اند دوم كوربوريشن Phosphoric acid salts of dipeptidyl betidase inhibitor 4
CA2533893A1 (en) 2003-07-31 2005-02-10 Merck & Co., Inc. Hexahydrodiazepinones as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
JP2007510651A (ja) 2003-11-04 2007-04-26 メルク エンド カムパニー インコーポレーテッド 糖尿病の治療又は予防のためのジペプチジルペプチダーゼ−iv阻害剤としての縮合フェニルアラニン誘導体
CN1950349A (zh) 2004-05-04 2007-04-18 默克公司 作为用于治疗或预防糖尿病的二肽基肽酶-ⅳ抑制剂的1,2,4-噁二唑衍生物
JP2007538079A (ja) 2004-05-18 2007-12-27 メルク エンド カムパニー インコーポレーテッド 糖尿病の治療又は予防のためのジペプチジルペプチダーゼ−iv阻害剤としてのシクロヘキシルアラニン誘導体
US7482336B2 (en) 2004-06-21 2009-01-27 Merck & Co., Inc. Aminocyclohexanes as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
WO2006023750A2 (en) 2004-08-23 2006-03-02 Merck & Co., Inc. Fused triazole derivatives as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
US7884104B2 (en) 2004-10-01 2011-02-08 Merck Sharp & Dohme Corp. Aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
WO2006065826A2 (en) 2004-12-15 2006-06-22 Merck & Co., Inc. Process to chiral beta amino acid derivatives by asymmetric hydrogenation
EP1841770B1 (en) 2005-01-19 2009-11-11 Merck & Co., Inc. Bicyclic pyrimidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2006104997A2 (en) 2005-03-29 2006-10-05 Merck & Co., Inc. Tartaric acid salts of a dipeptidyl peptidase-iv inhibitor
AU2006242219A1 (en) 2005-05-02 2006-11-09 Merck & Co., Inc. Combination of dipeptidyl peptidase-IV inhibitor and a cannabinoid CB1 receptor antagonist for the treatment of diabetes and obesity
WO2006127530A2 (en) 2005-05-25 2006-11-30 Merck & Co., Inc. Aminocyclohexanes as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
US20090221592A1 (en) 2005-07-25 2009-09-03 Ellison Martha E Dodecylsulfate Salt Of A Dipeptidyl Peptidase-Iv Inhibitor
CA2619111C (en) 2005-08-26 2013-04-09 Merck & Co., Inc. Fused aminopiperidines as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
EP1962601B1 (en) 2005-12-14 2014-10-15 Merck Sharp & Dohme Corp. Fused aminopiperidines as dipeptidyl peptidase-4 inhibitors for the treatment or prevention of diabetes
US8414921B2 (en) 2005-12-16 2013-04-09 Merck Sharp & Dohme Corp. Pharmaceutical compositions of combinations of dipeptidyl peptidase-4 inhibitors with metformin
US7750034B2 (en) 2006-01-25 2010-07-06 Merck Sharp & Dohme Corp. Aminocyclohexanes as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
US7910596B2 (en) 2006-02-15 2011-03-22 Merck Sharp & Dohme Corp. Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
TW200806669A (en) * 2006-03-28 2008-02-01 Merck & Co Inc Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
CA2652367A1 (en) 2006-05-16 2007-11-29 Merck & Co., Inc. Aminotetrahydropyrans as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
CA2668662A1 (en) 2006-11-14 2008-05-22 Merck & Co., Inc. Tricyclic heteroaromatic compounds as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
WO2009025784A1 (en) 2007-08-21 2009-02-26 Merck & Co., Inc. Heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment or prevention of diabetes
JO2870B1 (en) * 2008-11-13 2015-03-15 ميرك شارب اند دوهم كورب Amino Tetra Hydro Pirans as Inhibitors of Peptide Dipeptide IV for the Treatment or Prevention of Diabetes
EP2228366B1 (de) 2009-03-12 2011-12-28 Archimica GmbH Verfahren zur Herstellung von 2-Amino-4-(halogenalkyl)pyridin-Derivaten durch Cyclisierung geeigneter Nitril-Vorstufen mit Stickstoff-Verbindungen
KR20120092096A (ko) * 2009-09-02 2012-08-20 머크 샤프 앤드 돔 코포레이션 당뇨병의 치료 또는 예방을 위한 디펩티딜 펩티다제-iv 억제제로서의 아미노테트라히드로피란
US8716482B2 (en) 2009-09-25 2014-05-06 Merck Sharp & Dohme Corp. Substituted aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment of diabetes
US8980929B2 (en) 2010-05-21 2015-03-17 Merck Sharp & Dohme Corp. Substituted seven-membered heterocyclic compounds as dipeptidyl peptidase-iv inhibitors for the treatment of diabetes
WO2012078448A1 (en) 2010-12-06 2012-06-14 Schering Corporation Tricyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors
WO2012118945A2 (en) 2011-03-03 2012-09-07 Merck Sharp & Dohme Corp. Fused bicyclic heterocycles useful as dipeptidyl peptidase-iv inhibitors
AU2012275638A1 (en) 2011-06-29 2013-11-14 Merck Sharp & Dohme Corp. Process for preparing chiral dipeptidyl peptidase-IV inhibitors
US9051329B2 (en) 2011-07-05 2015-06-09 Merck Sharp & Dohme Corp. Tricyclic heterocycles useful as dipeptidyl peptidase-IV inhibitors
JP6480788B2 (ja) * 2015-04-07 2019-03-13 株式会社マキタ 打撃工具

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