KR20140053330A - 마크로락탐의 제조를 위한 방법 및 중간체 - Google Patents

마크로락탐의 제조를 위한 방법 및 중간체 Download PDF

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KR20140053330A
KR20140053330A KR1020147006858A KR20147006858A KR20140053330A KR 20140053330 A KR20140053330 A KR 20140053330A KR 1020147006858 A KR1020147006858 A KR 1020147006858A KR 20147006858 A KR20147006858 A KR 20147006858A KR 20140053330 A KR20140053330 A KR 20140053330A
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South Korea
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compound
compounds
salt
rti
added
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Korean (ko)
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펑 수
가이 험프리
타오 페이
지궈 제이크 숭
타오 왕
로라 아르티노
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머크 샤프 앤드 돔 코포레이션
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Publication of KR20140053330A publication Critical patent/KR20140053330A/ko
Withdrawn legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C35/00Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C07C35/02Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring monocyclic
    • C07C35/04Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring monocyclic containing a three or four-membered rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/04Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups from amines with formation of carbamate groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/32Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C271/34Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of rings other than six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00Preparation of carboxylic acid esters
    • C07C67/14Preparation of carboxylic acid esters from carboxylic acid halides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/013Esters of alcohols having the esterified hydroxy group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/02Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
    • C07C69/12Acetic acid esters
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/16Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08Tripeptides
    • C07K5/0802Tripeptides with the first amino acid being neutral
    • C07K5/0804Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/12Cyclic peptides with only normal peptide bonds in the ring
    • C07K5/126Tetrapeptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Communicable Diseases (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Oncology (AREA)
  • Veterinary Medicine (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Cephalosporin Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
KR1020147006858A 2011-08-19 2012-08-16 마크로락탐의 제조를 위한 방법 및 중간체 Withdrawn KR20140053330A (ko)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201161525462P 2011-08-19 2011-08-19
US61/525,462 2011-08-19
US201161533439P 2011-09-12 2011-09-12
US61/533,439 2011-09-12
US201161533915P 2011-09-13 2011-09-13
US61/533,915 2011-09-13
US201161539540P 2011-09-27 2011-09-27
US61/539,540 2011-09-27
PCT/US2012/051177 WO2013028470A1 (en) 2011-08-19 2012-08-16 Process and intermediates for preparing macrolactams

Publications (1)

Publication Number Publication Date
KR20140053330A true KR20140053330A (ko) 2014-05-07

Family

ID=47746773

Family Applications (2)

Application Number Title Priority Date Filing Date
KR1020147006858A Withdrawn KR20140053330A (ko) 2011-08-19 2012-08-16 마크로락탐의 제조를 위한 방법 및 중간체
KR1020147006888A Withdrawn KR20140059236A (ko) 2011-08-19 2012-08-16 Hcv 프로테아제 억제제의 결정 형태

Family Applications After (1)

Application Number Title Priority Date Filing Date
KR1020147006888A Withdrawn KR20140059236A (ko) 2011-08-19 2012-08-16 Hcv 프로테아제 억제제의 결정 형태

Country Status (11)

Country Link
US (3) US9073825B2 (enExample)
EP (3) EP2744336B1 (enExample)
JP (2) JP2014521750A (enExample)
KR (2) KR20140053330A (enExample)
CN (2) CN103874414A (enExample)
AU (2) AU2012299218A1 (enExample)
BR (2) BR112014003798A2 (enExample)
CA (2) CA2844386A1 (enExample)
MX (2) MX2014001944A (enExample)
RU (2) RU2014110400A (enExample)
WO (3) WO2013028470A1 (enExample)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011014487A1 (en) 2009-07-30 2011-02-03 Merck Sharp & Dohme Corp. Hepatitis c virus ns3 protease inhibitors
US8957203B2 (en) 2011-05-05 2015-02-17 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
BR112014003798A2 (pt) 2011-08-19 2017-03-01 Merck Sharp & Dohme método para fabricar um composto, e, composto
UA119315C2 (uk) 2012-07-03 2019-06-10 Гіліад Фармассет Елелсі Інгібітори вірусу гепатиту с
SI2909205T1 (sl) 2012-10-19 2017-02-28 Bristol-Myers Squibb Company 9-metil substituiran heksadekahidrociklopropa(e)pirolo(1,2-A)(1,4)diazaciklopentadecinil karbamat derivati kot nestrukturalni 3 (NS3) proteazni inhibitorji za zdravljenje hepatitis C virusnih infekcij
EP2914613B1 (en) 2012-11-02 2017-11-22 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
US9643999B2 (en) 2012-11-02 2017-05-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2914598B1 (en) 2012-11-02 2017-10-18 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
US9409943B2 (en) 2012-11-05 2016-08-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2764866A1 (en) 2013-02-07 2014-08-13 IP Gesellschaft für Management mbH Inhibitors of nedd8-activating enzyme
US9580463B2 (en) 2013-03-07 2017-02-28 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
SG11201507223TA (en) 2013-03-15 2015-10-29 Gilead Sciences Inc Macrocyclic and bicyclic inhibitors of hepatitis c virus
KR20160075508A (ko) * 2013-10-18 2016-06-29 머크 샤프 앤드 돔 코포레이션 마크로락탐을 제조하기 위한 방법 및 중간체
WO2015095437A1 (en) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Methods and intermediates for the preparation of macrolactams
AU2015209239C1 (en) 2014-01-24 2026-05-07 Turning Point Therapeutics, Inc. Diaryl macrocycles as modulators of protein kinases
WO2015188045A1 (en) 2014-06-06 2015-12-10 Abbvie Inc. Crystal forms
MX2017017097A (es) 2015-07-02 2018-05-23 Tp Therapeutics Inc Macrociclos diarílicos quirales como moduladores de proteínas quinasas.
PL3319969T3 (pl) * 2015-07-06 2024-06-24 Turning Point Therapeutics, Inc. Diarylowe polimorfy makrocykliczne
LT3733187T (lt) * 2015-07-21 2024-12-10 Turning Point Therapeutics, Inc. Chiralinis diarilo makrociklas ir jo panaudojimas vėžio gydymui
EP4483875A3 (en) 2016-05-10 2025-04-02 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
EP3455219A4 (en) 2016-05-10 2019-12-18 C4 Therapeutics, Inc. AMINE-RELATED C3-GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION
CN109641874A (zh) 2016-05-10 2019-04-16 C4医药公司 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体
CN109562107A (zh) 2016-05-10 2019-04-02 C4医药公司 用于靶蛋白降解的杂环降解决定子体
RU2019105587A (ru) 2016-07-28 2020-08-28 Тёрнинг Поинт Терапьютикс, Инк. Макроциклические ингибиторы киназ
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
EP3641762B1 (en) 2017-06-20 2026-02-18 C4 Therapeutics, Inc. N/o-linked degrons and degronimers for protein degradation
CA3069232A1 (en) 2017-07-28 2019-01-31 Turning Point Therapeutics, Inc. Macrocyclic compounds and uses thereof
HUE060711T2 (hu) 2017-12-19 2023-04-28 Turning Point Therapeutics Inc Makrociklusos vegyületek betegségek kezelésére
CN111057045A (zh) * 2019-12-18 2020-04-24 安徽红杉生物医药科技有限公司 Hcv ns3/4a蛋白酶抑制剂中间体及其合成方法、应用
CN112174982A (zh) * 2020-09-10 2021-01-05 上海希迈医药科技有限公司 一种洛普替尼晶型及其制备方法

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4871868A (en) 1987-03-11 1989-10-03 Takeda Chemical Industries, Ltd. Production of substituted acetylenic compounds
GB9207987D0 (en) * 1992-04-10 1992-05-27 Smithkline Beecham Plc Novel container and closure
US5716960A (en) * 1995-01-13 1998-02-10 U.S. Bioscience Inc. And Individuals Crystalline trimetrexate salts and the process for making the same
NO317155B1 (no) 1997-02-04 2004-08-30 Ono Pharmaceutical Co <omega>-cykloalkyl-prostagladin-E<N>2</N>-derivater
ZA98879B (en) * 1997-02-04 1998-08-03 Ono Pharmaceutical Co Omega-cycloalkyl-prostaglandin e2 derivatives
WO2006088129A1 (ja) * 2005-02-18 2006-08-24 Mitsubishi Pharma Corporation プロリン誘導体の塩、またはその溶媒和物、及びその製造方法
WO2006102087A2 (en) 2005-03-22 2006-09-28 Merck & Co., Inc. Hcv protease substrates
WO2006119061A2 (en) 2005-05-02 2006-11-09 Merck & Co., Inc. Hcv ns3 protease inhibitors
TWI387603B (zh) 2005-07-20 2013-03-01 Merck Sharp & Dohme Hcv ns3蛋白酶抑制劑
UA90909C2 (en) * 2005-07-20 2010-06-10 Мерк Шарп Энд Домэ Корп. Hcv ns3 protease inhibitors
KR20080036598A (ko) 2005-08-01 2008-04-28 머크 앤드 캄파니 인코포레이티드 Hcv ns3 프로테아제 억제제로서의 마크로사이클릭펩티드
AU2007224367A1 (en) 2006-03-07 2007-09-13 The Procter & Gamble Company Compositions for oxidatively dyeing keratin fibers and methods for using such compositions
GB0609492D0 (en) 2006-05-15 2006-06-21 Angeletti P Ist Richerche Bio Therapeutic agents
GB0612423D0 (en) 2006-06-23 2006-08-02 Angeletti P Ist Richerche Bio Therapeutic agents
AU2007309546A1 (en) 2006-10-24 2008-05-02 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. HCV NS3 protease inhibitors
AU2007309488B2 (en) 2006-10-24 2012-10-11 Merck Sharp & Dohme Corp. HCV NS3 protease inhibitors
CA2667031C (en) 2006-10-27 2013-01-22 Merck & Co., Inc. Hcv ns3 protease inhibitors
CN101568346B (zh) 2006-10-27 2015-11-25 默沙东公司 Hcv ns3蛋白酶抑制剂
KR20100024920A (ko) 2007-05-03 2010-03-08 인터뮨, 인크. C형 간염 바이러스 복제의 신규 마크로사이클릭 저해제
AU2008277377B2 (en) 2007-07-19 2013-08-01 Msd Italia S.R.L. Macrocyclic compounds as antiviral agents
CA2714604A1 (en) 2008-02-25 2009-09-03 Merck Sharp & Dohme Corp. Macrocyclic hcv ns3 protease inhibitors
WO2009131196A1 (ja) * 2008-04-24 2009-10-29 武田薬品工業株式会社 置換ピロリジン誘導体およびその用途
CA2722326A1 (en) 2008-04-24 2009-10-29 Incyte Corporation Macrocyclic compounds and their use as kinase inhibitors
EP2271345B1 (en) 2008-04-28 2015-05-20 Merck Sharp & Dohme Corp. Hcv ns3 protease inhibitors
ME02024B (me) 2008-07-22 2015-05-20 Merck Sharp & Dohme Makrociklična jedinjenja hinoksalina kao inhibitori hcv ns3 proteaze
WO2011014487A1 (en) 2009-07-30 2011-02-03 Merck Sharp & Dohme Corp. Hepatitis c virus ns3 protease inhibitors
CA2770338A1 (en) * 2009-08-27 2011-03-03 Merck Sharp & Dohme Corp. Processes for preparing protease inhibitors of hepatitis c virus
BR112014003798A2 (pt) 2011-08-19 2017-03-01 Merck Sharp & Dohme método para fabricar um composto, e, composto

Also Published As

Publication number Publication date
US20140243519A1 (en) 2014-08-28
RU2014110399A (ru) 2015-09-27
MX2014001944A (es) 2014-03-27
EP2744507A1 (en) 2014-06-25
CA2844386A1 (en) 2013-02-28
WO2013028465A1 (en) 2013-02-28
KR20140059236A (ko) 2014-05-15
WO2013028470A1 (en) 2013-02-28
CN103889439A (zh) 2014-06-25
BR112014003802A2 (pt) 2017-06-13
US20140206605A1 (en) 2014-07-24
JP2014524442A (ja) 2014-09-22
US20140200343A1 (en) 2014-07-17
EP2744507A4 (en) 2015-01-28
US9073825B2 (en) 2015-07-07
EP2744336A4 (en) 2014-12-31
CN103874414A (zh) 2014-06-18
AU2012299218A1 (en) 2014-02-20
BR112014003798A2 (pt) 2017-03-01
AU2012299223A1 (en) 2014-02-27
CA2844388A1 (en) 2013-02-28
US9238604B2 (en) 2016-01-19
EP2744331A4 (en) 2015-01-21
EP2744336B1 (en) 2017-07-05
MX2014001945A (es) 2014-03-27
WO2013028471A1 (en) 2013-02-28
EP2744331A1 (en) 2014-06-25
EP2744336A1 (en) 2014-06-25
RU2014110400A (ru) 2015-09-27
JP2014521750A (ja) 2014-08-28
US9242917B2 (en) 2016-01-26

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Patent event date: 20140314

Patent event code: PA01051R01D

Comment text: International Patent Application

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WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid