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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KR1020147006858A
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English (en)
Korean (ko)
Inventor
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Withdrawn legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C35/00—Compounds having at least one hydroxy or O-metal group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C07C35/02—Compounds 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
    • C07C35/04—Compounds 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/04—Preparation 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/32—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of rings other than six-membered aromatic rings
    • C07C271/34—Esters 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C67/00—Preparation of carboxylic acid esters
    • C07C67/14—Preparation of carboxylic acid esters from carboxylic acid halides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/013—Esters of alcohols having the esterified hydroxy group bound to a carbon atom of a ring other than a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C69/00—Esters of carboxylic acids; Esters of carbonic or haloformic acids
    • C07C69/02—Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen
    • C07C69/12—Acetic acid esters
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic 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
    • C07D498/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/0808—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms, e.g. Val, Ile, Leu
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/12—Cyclic peptides with only normal peptide bonds in the ring
    • C07K5/126—Tetrapeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal 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)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Cephalosporin Compounds (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) EP2744507A4 (enExample)
JP (2) JP2014521750A (enExample)
KR (2) KR20140053330A (enExample)
CN (2) CN103889439A (enExample)
AU (2) AU2012299218A1 (enExample)
BR (2) BR112014003802A2 (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
EP2744507A4 (en) 2011-08-19 2015-01-28 Merck Sharp & Dohme CRYSTAL FORMS OF AN HCV PROTEASE HEMMER
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
US9598433B2 (en) 2012-11-02 2017-03-21 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2014071007A1 (en) 2012-11-02 2014-05-08 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
US9643999B2 (en) 2012-11-02 2017-05-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2014070974A1 (en) 2012-11-05 2014-05-08 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
US9617310B2 (en) 2013-03-15 2017-04-11 Gilead Sciences, Inc. Inhibitors of hepatitis C virus
WO2015057611A1 (en) * 2013-10-18 2015-04-23 Merck Sharp & Dohme Corp. Methods and intermediates for preparing macrolactams
WO2015095437A1 (en) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Methods and intermediates for the preparation of macrolactams
WO2015112806A2 (en) * 2014-01-24 2015-07-30 Tp Therapeutics, Inc. Diaryl macrocycles as modulators of protein kinases
EP4403223A3 (en) * 2014-06-06 2024-10-09 AbbVie Inc. Crystal forms
ES2864839T3 (es) 2015-07-02 2021-10-14 Turning Point Therapeutics Inc Macrociclos de diarilo quirales como moduladores de proteína quinasas
ES2979111T3 (es) * 2015-07-06 2024-09-24 Turning Point Therapeutics Inc Polimorfo de macrociclo de diarilo
MX383823B (es) * 2015-07-21 2025-03-14 Turning Point Therapeutics Inc Macrociclos de diarilo quirales y usos de los mismo.
EP3454862B1 (en) 2016-05-10 2024-09-11 C4 Therapeutics, Inc. Spirocyclic degronimers for target protein degradation
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
WO2017197055A1 (en) 2016-05-10 2017-11-16 C4 Therapeutics, Inc. Heterocyclic degronimers for target protein degradation
CN109790143A (zh) 2016-05-10 2019-05-21 C4医药公司 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体
CN109715165A (zh) 2016-07-28 2019-05-03 Tp生物医药公司 巨环激酶抑制剂
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
CN110769822A (zh) 2017-06-20 2020-02-07 C4医药公司 用于蛋白降解的n/o-连接的降解决定子和降解决定子体
MY201925A (en) 2017-07-28 2024-03-23 Turning Point Therapeutics Inc Macrocyclic compounds and uses thereof
JP7194188B2 (ja) 2017-12-19 2022-12-21 ターニング・ポイント・セラピューティクス・インコーポレイテッド 疾患を治療するための大環状化合物
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
ZA98879B (en) * 1997-02-04 1998-08-03 Ono Pharmaceutical Co Omega-cycloalkyl-prostaglandin e2 derivatives
NO317155B1 (no) * 1997-02-04 2004-08-30 Ono Pharmaceutical Co <omega>-cykloalkyl-prostagladin-E<N>2</N>-derivater
EA013119B1 (ru) 2005-02-18 2010-02-26 Мицубиси Танабе Фарма Корпорейшн Соль производного пролина, ее сольват и способ ее получения
US7834145B2 (en) 2005-03-22 2010-11-16 Merck Sharp & Dohme Corp. HCV protease substrates
AU2006242475B2 (en) 2005-05-02 2011-07-07 Merck Sharp & Dohme Corp. HCV NS3 protease inhibitors
AR057456A1 (es) 2005-07-20 2007-12-05 Merck & Co Inc Inhibidores de la proteasa ns3 del vhc
UA90909C2 (en) * 2005-07-20 2010-06-10 Мерк Шарп Энд Домэ Корп. Hcv ns3 protease inhibitors
RU2008107972A (ru) 2005-08-01 2009-09-10 Мерк энд Ко., Инк. (US) Макроциклические пептиды в качестве ингибиторов ns3-протеазы hcv
EP2018146A2 (en) * 2006-03-07 2009-01-28 The Procter and 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
US8309540B2 (en) 2006-10-24 2012-11-13 Merck Sharp & Dohme Corp. HCV NS3 protease inhibitors
AU2007309546A1 (en) 2006-10-24 2008-05-02 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. HCV NS3 protease inhibitors
EP2086982B1 (en) 2006-10-27 2018-08-29 Merck Sharp & Dohme Corp. Hcv ns3 protease inhibitors
EP2083844B1 (en) 2006-10-27 2013-11-27 Merck Sharp & Dohme Corp. Hcv ns3 protease inhibitors
EP2160392A2 (en) 2007-05-03 2010-03-10 Intermune, Inc. Novel macrocyclic inhibitors of hepatitis c virus replication
WO2009010804A1 (en) 2007-07-19 2009-01-22 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Macrocyclic compounds as antiviral agents
EP2268285B1 (en) 2008-02-25 2018-06-27 Merck Sharp & Dohme Corp. Therapeutic compounds
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
JP2011518836A (ja) 2008-04-24 2011-06-30 インサイト・コーポレイション 大環状化合物およびそれらのキナーゼ阻害剤としての使用
CA2720850A1 (en) 2008-04-28 2009-11-05 Merck Sharp & Dohme Corp. Hcv ns3 protease inhibitors
PL2310095T3 (pl) 2008-07-22 2013-03-29 Msd Italia Srl Makrocykliczne związki chinoksaliny jako inhibitory proteazy NS3 HCV
WO2011014487A1 (en) 2009-07-30 2011-02-03 Merck Sharp & Dohme Corp. Hepatitis c virus ns3 protease inhibitors
AU2010286681A1 (en) * 2009-08-27 2012-02-09 Merck Sharp & Dohme Corp. Processes for preparing protease inhibitors of hepatitis C virus
EP2744507A4 (en) 2011-08-19 2015-01-28 Merck Sharp & Dohme CRYSTAL FORMS OF AN HCV PROTEASE HEMMER

Also Published As

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

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Patent event date: 20140314

Patent event code: PA01051R01D

Comment text: International Patent Application

PG1501 Laying open of application
PC1203 Withdrawal of no request for examination
WITN Application deemed withdrawn, e.g. because no request for examination was filed or no examination fee was paid