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SG11201604482QA - Synthesis of a macrocyclic hcv ns3 inhibiting tripeptide - Google Patents

Synthesis of a macrocyclic hcv ns3 inhibiting tripeptide

Info

Publication number
SG11201604482QA
SG11201604482QA SG11201604482QA SG11201604482QA SG11201604482QA SG 11201604482Q A SG11201604482Q A SG 11201604482QA SG 11201604482Q A SG11201604482Q A SG 11201604482QA SG 11201604482Q A SG11201604482Q A SG 11201604482QA SG 11201604482Q A SG11201604482Q A SG 11201604482QA
Authority
SG
Singapore
Prior art keywords
synthesis
macrocyclic hcv
tripeptide
inhibiting
inhibiting tripeptide
Prior art date
Application number
SG11201604482QA
Inventor
Amy Cagulada
Johann Chan
Lina Chan
Denise A Colby
Kapil Kumar Karki
Darryl Kato
Katie Ann Keaton
Sudha Kondapally
Chris Levins
Adam Littke
Ruben Martinez
Dominika Pcion
Troy Reynolds
Bruce Ross
Michael Sangi
Adam J Schrier
Pamela Seng
Dustin Siegel
Nathan Shapiro
Donald Tang
James G Taylor
Jonathan Tripp
Lawrence Yu
Andrew W Waltman
Original Assignee
Gilead Sciences Inc
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 Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of SG11201604482QA publication Critical patent/SG11201604482QA/en

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Classifications

    • 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
    • C07D498/18Bridged systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • C07C205/00Compounds containing nitro groups bound to a carbon skeleton
    • C07C205/49Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups
    • C07C205/57Compounds containing nitro groups bound to a carbon skeleton the carbon skeleton being further substituted by carboxyl groups having nitro groups and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00Preparation of compounds containing amino groups bound to a carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/02Formation of carboxyl groups in compounds containing amino groups, e.g. by oxidation of amino alcohols
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/02Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C07C233/09Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having nitrogen atoms of carboxamide groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with carbon atoms of carboxamide groups bound to carbon atoms of an acyclic unsaturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C251/00Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C251/02Compounds containing nitrogen atoms doubly-bound to a carbon skeleton containing imino groups
    • C07C251/04Compounds containing nitrogen atoms doubly-bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C251/10Compounds containing nitrogen atoms doubly-bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of an unsaturated carbon skeleton
    • C07C251/12Compounds containing nitrogen atoms doubly-bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of an unsaturated carbon skeleton being acyclic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/61Carboxylic acid nitriles containing cyano groups and nitrogen atoms being part of imino groups bound to the same carbon skeleton
    • 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
    • C07C51/00Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/09Preparation of carboxylic acids or their salts, halides or anhydrides from carboxylic acid esters or lactones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D241/00Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/36Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40Benzopyrazines
    • C07D241/44Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • 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
    • C07D453/00Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • 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
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/02Systems containing only non-condensed rings with a three-membered ring
    • 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

Landscapes

  • 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)
  • Engineering & Computer Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
SG11201604482QA 2013-12-23 2014-12-18 Synthesis of a macrocyclic hcv ns3 inhibiting tripeptide SG11201604482QA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201361920446P 2013-12-23 2013-12-23
PCT/US2014/071319 WO2015100145A1 (en) 2013-12-23 2014-12-18 Synthesis of a macrocyclic hcv ns3 inhibiting tripeptide

Publications (1)

Publication Number Publication Date
SG11201604482QA true SG11201604482QA (en) 2016-07-28

Family

ID=52278856

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201604482QA SG11201604482QA (en) 2013-12-23 2014-12-18 Synthesis of a macrocyclic hcv ns3 inhibiting tripeptide

Country Status (20)

Country Link
US (2) US9440991B2 (en)
EP (1) EP3087085B1 (en)
JP (1) JP6425727B2 (en)
KR (1) KR102366697B1 (en)
CN (3) CN105849118B (en)
AR (1) AR098959A1 (en)
AU (1) AU2014370125B2 (en)
CA (1) CA2934537C (en)
EA (1) EA201691031A1 (en)
ES (1) ES2724460T3 (en)
IL (1) IL246064A0 (en)
MX (1) MX2016008452A (en)
NZ (1) NZ720745A (en)
PL (1) PL3087085T3 (en)
PT (1) PT3087085T (en)
SG (1) SG11201604482QA (en)
SI (1) SI3087085T1 (en)
TR (1) TR201906413T4 (en)
TW (3) TWI671292B (en)
WO (1) WO2015100145A1 (en)

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SI3027618T1 (en) 2013-07-30 2021-01-29 Kronos Bio, Inc. Polymorph of syk inhibitors
HK1222329A1 (en) * 2013-07-30 2017-06-30 吉利德康涅狄格公司 Formulation of syk inhibitors
SG11201604482QA (en) 2013-12-23 2016-07-28 Gilead Sciences Inc Synthesis of a macrocyclic hcv ns3 inhibiting tripeptide
TWI735853B (en) 2013-12-23 2021-08-11 美商克洛諾斯生技有限公司 Syk inhibitors
US9809576B1 (en) 2014-07-18 2017-11-07 Abbvie Inc. Synthetic route to anti-viral agents
US9809534B1 (en) * 2014-07-21 2017-11-07 Abbvie Inc. Difluoroalkylcyclopropyl amino acids and esters, and syntheses thereof
US10059969B1 (en) 2014-10-03 2018-08-28 Abbvie Inc. Process for the preparation of (S)-2-amino-non-8-enoic acid
US10316338B1 (en) 2015-01-30 2019-06-11 Abb Vie Inc. Enzymatic process for the preparation of (1S,2R)-2-(difluoromethyl)-1-(propoxycarbonyl)cyclopropanecarboxylic acid
WO2017002712A1 (en) * 2015-06-29 2017-01-05 セントラル硝子株式会社 Method for producing fluorine-containing cyclopropane carboxylic acid compound
US10689675B2 (en) 2017-02-01 2020-06-23 Abbvie Inc. Enzymatic processes for the preparation of (±)-2-(difluoromethyl)-1-(alkoxycarbonyl)-cyclopropanecarboxylic acid and (±)-2-(vinyl)-1-(alkoxycarbonyl)-cyclopropanecarboxylic acid
CN107739319A (en) * 2017-10-31 2018-02-27 上海同昌生物医药科技有限公司 A kind of preparation method of Glecaprevir synthetic intermediates and its amine salt
WO2019084740A1 (en) * 2017-10-31 2019-05-09 上海同昌生物医药科技有限公司 Method for preparing glecaprevir synthetic intermediate and amine salt thereof
CN107827748A (en) * 2017-11-14 2018-03-23 安徽华胜医药科技有限公司 Synthesis method of 2-allyl cyclopropyl acetate racemate
KR102519417B1 (en) 2018-11-28 2023-04-10 삼성디스플레이 주식회사 Stretchable display device
CN113950479A (en) 2019-02-22 2022-01-18 克洛诺斯生物股份有限公司 Solid forms of condensed pyrazines as SYK inhibitors
CN116041181A (en) * 2023-01-04 2023-05-02 广州巨元生化有限公司 A kind of method for preparing 4-halo-2-methyl-2-butenoic acid alkyl ester

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KR20060109937A (en) * 2003-12-15 2006-10-23 니뽄 다바코 산교 가부시키가이샤 N-substituted-N-sulfonylaminocyclopropane compounds and pharmaceutical uses thereof
CL2008003384A1 (en) * 2007-11-14 2009-12-11 Enanta Pharm Inc Macrocyclic quinoxaline derived compounds, serine protease inhibitors; pharmaceutical composition comprising them; and its use in the treatment of hepatitis c.
US8211891B2 (en) 2008-04-30 2012-07-03 Enanta Pharmaceuticals, Inc. Difluoromethyl-containing macrocyclic compounds as hepatitis C virus inhibitors
EP2540350B1 (en) * 2008-07-22 2014-05-21 Merck Sharp & Dohme Corp. Combinations of a macrocyclic quinoxaline compound which is an hcv ns3 protease inhibitor with other hcv agents
US8283310B2 (en) 2008-12-15 2012-10-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2289880A1 (en) * 2009-07-08 2011-03-02 Bayer CropScience AG 2-Pyridinylcyclopropylbenzamide fungicides
WO2012040040A1 (en) * 2010-09-21 2012-03-29 Merck Sharp & Dohme Corp. Hcv ns3 protease inhibitors
EP2618831B1 (en) * 2010-09-21 2016-01-06 Enanta Pharmaceuticals, Inc. Macrocyclic proline derived hcv serine protease inhibitors
AR084217A1 (en) * 2010-12-10 2013-05-02 Gilead Sciences Inc MACROCICLIC INHIBITORS OF VIRUS FLAVIVIRIDAE
UA119315C2 (en) 2012-07-03 2019-06-10 Гіліад Фармассет Елелсі HEPATITIS VIRUS INHIBITORS C
WO2015095430A1 (en) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Methods and intermediates for the preparation of macrolactams
SG11201604482QA (en) 2013-12-23 2016-07-28 Gilead Sciences Inc Synthesis of a macrocyclic hcv ns3 inhibiting tripeptide
JP6568541B2 (en) 2013-12-23 2019-08-28 ギリアド ファーマセット エルエルシー Crystal form of macrocyclic HCV NS3 inhibitory tripeptide

Also Published As

Publication number Publication date
CN111320610B (en) 2023-06-06
AU2014370125B2 (en) 2017-11-16
SI3087085T1 (en) 2019-05-31
WO2015100145A1 (en) 2015-07-02
NZ720745A (en) 2018-02-23
TR201906413T4 (en) 2019-05-21
PT3087085T (en) 2019-06-04
CN116813596A (en) 2023-09-29
TWI671292B (en) 2019-09-11
KR102366697B1 (en) 2022-02-25
CN111320610A (en) 2020-06-23
US20170210756A1 (en) 2017-07-27
CA2934537C (en) 2022-08-16
US10030033B2 (en) 2018-07-24
US9440991B2 (en) 2016-09-13
MX2016008452A (en) 2016-10-14
PL3087085T3 (en) 2019-07-31
TW201609711A (en) 2016-03-16
US20150175626A1 (en) 2015-06-25
JP2017509585A (en) 2017-04-06
KR20160101934A (en) 2016-08-26
HK1222401A1 (en) 2017-06-30
JP6425727B2 (en) 2018-11-21
CA2934537A1 (en) 2015-07-02
TWI710547B (en) 2020-11-21
TWI762003B (en) 2022-04-21
EA201691031A1 (en) 2017-01-30
CN105849118B (en) 2020-03-31
TW202106661A (en) 2021-02-16
EP3087085A1 (en) 2016-11-02
EP3087085B1 (en) 2019-02-20
TW201938527A (en) 2019-10-01
IL246064A0 (en) 2016-07-31
AU2014370125A1 (en) 2016-06-23
ES2724460T3 (en) 2019-09-11
CN105849118A (en) 2016-08-10
AR098959A1 (en) 2016-06-22

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