CN103328466B - Hcv ns3蛋白酶抑制剂 - Google Patents

Hcv ns3蛋白酶抑制剂 Download PDF

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Publication number
CN103328466B
CN103328466B CN201180063866.1A CN201180063866A CN103328466B CN 103328466 B CN103328466 B CN 103328466B CN 201180063866 A CN201180063866 A CN 201180063866A CN 103328466 B CN103328466 B CN 103328466B
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CN
China
Prior art keywords
compound
compounds
hcv
alkyl
aryl
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.)
Expired - Fee Related
Application number
CN201180063866.1A
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English (en)
Chinese (zh)
Other versions
CN103328466A (zh
Inventor
热罗姆·库尔卡姆贝克
菲利普·阿尔丰
穆拉德·布齐迪
史蒂文·J·科茨
理查德·安东尼·惠特克
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.)
Jinnoss Pharmaceuticals
RFS Pharma LLC
Original Assignee
Jinnoss Pharmaceuticals
RFS Pharma 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 Jinnoss Pharmaceuticals, RFS Pharma LLC filed Critical Jinnoss Pharmaceuticals
Publication of CN103328466A publication Critical patent/CN103328466A/zh
Application granted granted Critical
Publication of CN103328466B publication Critical patent/CN103328466B/zh
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • 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
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/4035Isoindoles, e.g. phthalimide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Enzymes And Modification Thereof (AREA)
CN201180063866.1A 2010-11-01 2011-10-28 Hcv ns3蛋白酶抑制剂 Expired - Fee Related CN103328466B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US40898910P 2010-11-01 2010-11-01
US61/408,989 2010-11-01
PCT/US2011/058404 WO2012061248A2 (en) 2010-11-01 2011-10-28 Novel specific hcv ns3 protease inhibitors

Publications (2)

Publication Number Publication Date
CN103328466A CN103328466A (zh) 2013-09-25
CN103328466B true CN103328466B (zh) 2016-08-03

Family

ID=46025037

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180063866.1A Expired - Fee Related CN103328466B (zh) 2010-11-01 2011-10-28 Hcv ns3蛋白酶抑制剂

Country Status (10)

Country Link
US (1) US8729014B2 (enExample)
EP (1) EP2635570B1 (enExample)
JP (1) JP5828903B2 (enExample)
CN (1) CN103328466B (enExample)
AU (1) AU2011323658A1 (enExample)
BR (1) BR112013010836A2 (enExample)
CA (1) CA2815855C (enExample)
IL (1) IL225908A0 (enExample)
MX (1) MX2013004906A (enExample)
WO (1) WO2012061248A2 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN2012MN02896A (enExample) 2010-06-24 2015-06-12 Panmed Ltd
WO2012061248A2 (en) 2010-11-01 2012-05-10 Rfs Pharma, Llc Novel specific hcv ns3 protease inhibitors
US8912141B2 (en) 2011-06-23 2014-12-16 Panmed Ltd. Treatment of hepatitis C virus
CN104039774A (zh) 2012-01-12 2014-09-10 Rfs制药公司 Hcv ns3蛋白酶抑制剂
UA119315C2 (uk) 2012-07-03 2019-06-10 Гіліад Фармассет Елелсі Інгібітори вірусу гепатиту с
EA029088B1 (ru) 2013-03-15 2018-02-28 Джилид Сайэнс, Инк. Макроциклические и бициклические ингибиторы вируса гепатита c
AU2015247706A1 (en) * 2014-04-15 2016-10-27 Cocrystal Pharma, Inc. Potent and selective inhibitors of hepatitis C virus
CN105315261A (zh) * 2014-08-04 2016-02-10 正大天晴药业集团股份有限公司 Hcv ns3蛋白酶抑制剂的钠盐

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101189223A (zh) * 2005-02-08 2008-05-28 布里斯托尔-迈尔斯斯奎布公司 丙型肝炎病毒抑制剂
CN101495457A (zh) * 2006-07-05 2009-07-29 因特蒙公司 C型肝炎病毒复制的新颖抑制剂

Family Cites Families (24)

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WO1995000536A1 (en) 1993-06-22 1995-01-05 Fujisawa Pharmaceutical Co., Ltd. Peptide compounds
CN1133649C (zh) 1996-10-18 2004-01-07 沃泰克斯药物股份有限公司 丝氨酸蛋白酶、特别是丙型肝炎病毒ns3蛋白酶的抑制剂
US6767991B1 (en) 1997-08-11 2004-07-27 Boehringer Ingelheim (Canada) Ltd. Hepatitis C inhibitor peptides
ATE297946T1 (de) 2000-04-03 2005-07-15 Vertex Pharma Inhibitoren von serin proteasen, speziell der hepatitis-c-virus ns3-protease
WO2003013571A1 (en) 2001-08-10 2003-02-20 Palatin Technologies, Inc. Peptidomimetics of biologically active metallopeptides
MY140680A (en) 2002-05-20 2010-01-15 Bristol Myers Squibb Co Hepatitis c virus inhibitors
AU2003299519A1 (en) 2002-05-20 2004-05-04 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
US7718671B2 (en) 2003-07-10 2010-05-18 Achillion Pharmaceuticals, Inc. Substituted arylthiourea derivatives useful as inhibitors of viral replication
DK1713823T3 (da) 2004-01-30 2010-03-08 Medivir Ab HCV NS-3 serinproteaseinhibitorer
US7399749B2 (en) 2004-05-20 2008-07-15 Schering Corporation Substituted prolines as inhibitors of hepatitis C virus NS3 serine protease
EP1875780A2 (en) 2005-04-19 2008-01-09 Philips Intellectual Property & Standards GmbH Illumination system comprising a red-emitting ceramic luminescence converter
AR057456A1 (es) 2005-07-20 2007-12-05 Merck & Co Inc Inhibidores de la proteasa ns3 del vhc
AU2006275605B2 (en) 2005-08-01 2011-01-06 Merck Sharp & Dohme Corp. Macrocyclic peptides as HCV NS3 protease inhibitors
US20090304631A1 (en) 2006-01-27 2009-12-10 David Alan Campbell Hepatitis c serine protease inhibitors and uses therefor
RU2008152171A (ru) * 2006-07-05 2010-08-10 Интермьюн, Инк. (Us) Новые ингибиторы вирусной репликации гепатита с
US7635683B2 (en) 2006-08-04 2009-12-22 Enanta Pharmaceuticals, Inc. Quinoxalinyl tripeptide hepatitis C virus inhibitors
CN101553170B (zh) 2006-11-24 2011-11-09 株式会社岛津制作所 X射线透视摄影装置
US20080287449A1 (en) 2007-04-26 2008-11-20 Deqiang Niu Aza-tripeptide hepatitis c serine protease inhibitors
CA2708150A1 (en) 2007-12-05 2009-06-18 Enanta Pharmaceuticals, Inc. Fluorinated tripeptide hcv serine protease inhibitors
US8293705B2 (en) * 2007-12-21 2012-10-23 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
CN101951769B (zh) 2007-12-21 2014-12-31 阿维拉制药公司 Hcv蛋白酶抑制剂和其用途
CN102046622A (zh) 2008-04-15 2011-05-04 因特蒙公司 丙型肝炎病毒复制的新颖大环抑制剂
CA2788155C (en) * 2010-01-27 2018-04-24 AB Pharma Ltd. Polyheterocyclic compounds highly potent as hcv inhibitors
WO2012061248A2 (en) 2010-11-01 2012-05-10 Rfs Pharma, Llc Novel specific hcv ns3 protease inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101189223A (zh) * 2005-02-08 2008-05-28 布里斯托尔-迈尔斯斯奎布公司 丙型肝炎病毒抑制剂
CN101495457A (zh) * 2006-07-05 2009-07-29 因特蒙公司 C型肝炎病毒复制的新颖抑制剂

Also Published As

Publication number Publication date
BR112013010836A2 (pt) 2019-09-24
CN103328466A (zh) 2013-09-25
WO2012061248A8 (en) 2013-08-01
WO2012061248A2 (en) 2012-05-10
US8729014B2 (en) 2014-05-20
CA2815855C (en) 2016-02-02
JP2013542955A (ja) 2013-11-28
JP5828903B2 (ja) 2015-12-09
EP2635570A4 (en) 2014-04-16
CA2815855A1 (en) 2012-05-10
AU2011323658A1 (en) 2013-05-23
MX2013004906A (es) 2013-12-06
EP2635570B1 (en) 2017-12-13
EP2635570A2 (en) 2013-09-11
US20120129765A1 (en) 2012-05-24
IL225908A0 (en) 2013-06-27
WO2012061248A3 (en) 2012-08-02

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Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
EE01 Entry into force of recordation of patent licensing contract

Application publication date: 20130925

Assignee: BIOLINERX Ltd.

Assignor: RFS PHARMA, LLC|Jinnoss Pharmaceuticals

Contract record no.: 2014990000851

Denomination of invention: Macrocyclic compounds as hcv ns3 protease inhibitors

License type: Exclusive License

Record date: 20141104

LICC Enforcement, change and cancellation of record of contracts on the licence for exploitation of a patent or utility model
C14 Grant of patent or utility model
GR01 Patent grant
CF01 Termination of patent right due to non-payment of annual fee
CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20160803