CN104169293A - 抑制丙肝病毒复制的大环类化合物 - Google Patents

抑制丙肝病毒复制的大环类化合物 Download PDF

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Publication number
CN104169293A
CN104169293A CN201280069837.0A CN201280069837A CN104169293A CN 104169293 A CN104169293 A CN 104169293A CN 201280069837 A CN201280069837 A CN 201280069837A CN 104169293 A CN104169293 A CN 104169293A
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China
Prior art keywords
cyclopropyl
carbamyl
compound
ring
azepine
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Pending
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CN201280069837.0A
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English (en)
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李本
陈力
翟培彬
江涛
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Ginkgo Tree Pharmaceutical Suzhou Co ltd
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Ginkgo Tree Pharmaceutical Suzhou Co ltd
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Priority to CN201280069837.0A priority Critical patent/CN104169293A/zh
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    • C07—ORGANIC CHEMISTRY
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    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1002—Tetrapeptides with the first amino acid being neutral
    • C07K5/1005—Tetrapeptides with the first amino acid being neutral and aliphatic
    • C07K5/1013—Tetrapeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/005—Enzyme inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/16—Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/55—Protease inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07K5/08—Tripeptides
    • C07K5/0802—Tripeptides with the first amino acid being neutral
    • C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04—Linear peptides containing only normal peptide links
    • C07K7/06—Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06034—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 2 to 4 carbon atoms
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06078—Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Peptides Or Proteins (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

本发明提供一种式I化合物，其中基团定义如说明书所述。该化合物作为HCV蛋白酶抑制剂，用于治疗丙肝病毒感染。

Description

PCT国内申请，说明书已公开。

Claims (1)

  1. PCT国内申请，权利要求书已公开。
CN201280069837.0A 2012-02-16 2012-12-05 抑制丙肝病毒复制的大环类化合物 Pending CN104169293A (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201280069837.0A CN104169293A (zh) 2012-02-16 2012-12-05 抑制丙肝病毒复制的大环类化合物

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
CN201210034872.0 2012-02-16
CN201210034872.0A CN102617705B (zh) 2012-02-16 2012-02-16 抑制丙肝病毒复制的大环类化合物
PCT/CN2012/085912 WO2013120371A1 (zh) 2012-02-16 2012-12-05 抑制丙肝病毒复制的大环类化合物
CN201280069837.0A CN104169293A (zh) 2012-02-16 2012-12-05 抑制丙肝病毒复制的大环类化合物

Publications (1)

Publication Number Publication Date
CN104169293A true CN104169293A (zh) 2014-11-26

Family

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Family Applications (2)

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CN201210034872.0A Expired - Fee Related CN102617705B (zh) 2012-02-16 2012-02-16 抑制丙肝病毒复制的大环类化合物
CN201280069837.0A Pending CN104169293A (zh) 2012-02-16 2012-12-05 抑制丙肝病毒复制的大环类化合物

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Country Status (10)

Country Link
US (1) US9321809B2 (zh)
EP (1) EP2816054A4 (zh)
JP (1) JP6105632B2 (zh)
KR (1) KR102004381B1 (zh)
CN (2) CN102617705B (zh)
AU (1) AU2012370125A1 (zh)
CA (1) CA2864488A1 (zh)
IL (1) IL233899A0 (zh)
IN (1) IN2014MN01637A (zh)
WO (1) WO2013120371A1 (zh)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8957203B2 (en) 2011-05-05 2015-02-17 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
CN102617705B (zh) * 2012-02-16 2014-12-31 上海纬诺医药科技有限公司 抑制丙肝病毒复制的大环类化合物
JP6154474B2 (ja) 2012-10-19 2017-06-28 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｃ型肝炎ウイルス阻害剤
US9643999B2 (en) 2012-11-02 2017-05-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2014070964A1 (en) 2012-11-02 2014-05-08 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
EP2914598B1 (en) 2012-11-02 2017-10-18 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
EP2914614B1 (en) 2012-11-05 2017-08-16 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
EP2964664B1 (en) 2013-03-07 2017-01-11 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
CN104447952A (zh) * 2014-12-11 2015-03-25 上海唐润医药科技有限公司 丙肝病毒蛋白酶抑制剂及其合成方法
CN110963986B (zh) * 2018-09-28 2022-03-29 北京瑞莱博基医药科技有限公司 一种糖尿病治疗药物中间体的合成工艺

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1894274A (zh) * 2003-09-26 2007-01-10 先灵公司 丙肝病毒ns3丝氨酸蛋白酶的大环抑制剂
WO2010033466A1 (en) * 2008-09-16 2010-03-25 Phenomix Corporation Macrocyclic inhibitors of hepatitis c protease
CN102617705B (zh) * 2012-02-16 2014-12-31 上海纬诺医药科技有限公司 抑制丙肝病毒复制的大环类化合物

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2369711A1 (en) * 2002-01-30 2003-07-30 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis c virus
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
GB0612423D0 (en) 2006-06-23 2006-08-02 Angeletti P Ist Richerche Bio Therapeutic agents
US8138164B2 (en) 2006-10-24 2012-03-20 Merck Sharp & Dohme Corp. HCV NS3 protease inhibitors
US7964560B2 (en) * 2008-05-29 2011-06-21 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US20100160403A1 (en) * 2008-12-19 2010-06-24 Gilead Sciences, Inc. Hcv ns3 protease inhibitors
JP5639155B2 (ja) * 2009-05-13 2014-12-10 エナンタ ファーマシューティカルズ インコーポレイテッド Ｃ型肝炎ウイルスインヒビターとしての大環状化合物
WO2011009961A1 (en) * 2009-07-24 2011-01-27 Virologik Gmbh Combination of proteasome inhibitors and anti-hepatitis medication for treating hepatitis

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1894274A (zh) * 2003-09-26 2007-01-10 先灵公司 丙肝病毒ns3丝氨酸蛋白酶的大环抑制剂
WO2010033466A1 (en) * 2008-09-16 2010-03-25 Phenomix Corporation Macrocyclic inhibitors of hepatitis c protease
CN102617705B (zh) * 2012-02-16 2014-12-31 上海纬诺医药科技有限公司 抑制丙肝病毒复制的大环类化合物

Also Published As

Publication number Publication date
CA2864488A1 (en) 2013-08-22
EP2816054A1 (en) 2014-12-24
IL233899A0 (en) 2014-09-30
AU2012370125A1 (en) 2014-07-31
US9321809B2 (en) 2016-04-26
WO2013120371A1 (zh) 2013-08-22
KR20140134273A (ko) 2014-11-21
KR102004381B1 (ko) 2019-10-01
IN2014MN01637A (zh) 2015-07-03
JP6105632B2 (ja) 2017-03-29
US20150031603A1 (en) 2015-01-29
CN102617705B (zh) 2014-12-31
EP2816054A4 (en) 2015-07-29
JP2015508761A (ja) 2015-03-23
CN102617705A (zh) 2012-08-01

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Application publication date: 20141126