JP4690545B2 - セリンプロテアーゼ、特にｃ型肝炎ウイルスｎｓ３プロテアーゼの阻害因子 - Google Patents

セリンプロテアーゼ、特にｃ型肝炎ウイルスｎｓ３プロテアーゼの阻害因子 Download PDF

Info

Publication number
JP4690545B2
JP4690545B2 JP2000541139A JP2000541139A JP4690545B2 JP 4690545 B2 JP4690545 B2 JP 4690545B2 JP 2000541139 A JP2000541139 A JP 2000541139A JP 2000541139 A JP2000541139 A JP 2000541139A JP 4690545 B2 JP4690545 B2 JP 4690545B2
Authority
JP
Japan
Prior art keywords
compound
resin
synthesis
compounds
formula
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
JP2000541139A
Other languages
English (en)
Japanese (ja)
Other versions
JP2002509910A5 (https=
JP2002509910A (ja
Inventor
ロジャー・ディ・トゥン
リュック・ジ・ファルメ
ゴビンダ・アール・ビセッテイ
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.)
Vertex Pharmaceuticals Inc
Original Assignee
Vertex Pharmaceuticals 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 Vertex Pharmaceuticals Inc filed Critical Vertex Pharmaceuticals Inc
Publication of JP2002509910A publication Critical patent/JP2002509910A/ja
Publication of JP2002509910A5 publication Critical patent/JP2002509910A5/ja
Application granted granted Critical
Publication of JP4690545B2 publication Critical patent/JP4690545B2/ja
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides
    • C07D213/82—Amides; Imides in position 3
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/42—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Peptides Or Proteins (AREA)
JP2000541139A 1998-03-31 1999-03-31 セリンプロテアーゼ、特にｃ型肝炎ウイルスｎｓ３プロテアーゼの阻害因子 Expired - Fee Related JP4690545B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US8006098P 1998-03-31 1998-03-31
US60/080,060 1998-03-31
PCT/US1999/007149 WO1999050230A1 (en) 1998-03-31 1999-03-31 Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease

Publications (3)

Publication Number Publication Date
JP2002509910A JP2002509910A (ja) 2002-04-02
JP2002509910A5 JP2002509910A5 (https=) 2006-06-08
JP4690545B2 true JP4690545B2 (ja) 2011-06-01

Family

ID=22155006

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2000541139A Expired - Fee Related JP4690545B2 (ja) 1998-03-31 1999-03-31 セリンプロテアーゼ、特にｃ型肝炎ウイルスｎｓ３プロテアーゼの阻害因子

Country Status (9)

Country Link
US (3) US6608067B1 (https=)
EP (1) EP1066247B1 (https=)
JP (1) JP4690545B2 (https=)
AT (1) ATE346035T1 (https=)
AU (1) AU3376699A (https=)
DE (1) DE69934104T2 (https=)
DK (1) DK1066247T3 (https=)
ES (1) ES2281170T3 (https=)
WO (1) WO1999050230A1 (https=)

Families Citing this family (127)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100509388B1 (ko) * 1996-10-18 2005-08-23 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 간염 ｃ 바이러스 ｎｓ３ 프로테아제의 저해제
WO2000024725A1 (en) * 1998-10-26 2000-05-04 Vertex Pharmaceuticals Incorporated Pentacyclic compounds useful as inhibitors of hepatitis c virus ns3 helicase
US6608027B1 (en) 1999-04-06 2003-08-19 Boehringer Ingelheim (Canada) Ltd Macrocyclic peptides active against the hepatitis C virus
UA74546C2 (en) * 1999-04-06 2006-01-16 Boehringer Ingelheim Ca Ltd Macrocyclic peptides having activity relative to hepatitis c virus, a pharmaceutical composition and use of the pharmaceutical composition
ES2240446T3 (es) * 2000-04-03 2005-10-16 Vertex Pharma Inhibidores de serina proteasas, particularmente la proteasa ns3 del virus de la hepatitis c.
US6613801B2 (en) 2000-05-30 2003-09-02 Transtech Pharma, Inc. Method for the synthesis of compounds of formula I and their uses thereof
US7423177B2 (en) 2001-03-05 2008-09-09 Transtech Pharma, Inc. Carboxamide derivatives as therapeutic agents
AR034127A1 (es) * 2000-07-21 2004-02-04 Schering Corp Imidazolidinonas como inhibidores de ns3-serina proteasa del virus de hepatitis c, composicion farmaceutica, un metodo para su preparacion, y el uso de las mismas para la manufactura de un medicamento
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
US6846806B2 (en) 2000-10-23 2005-01-25 Bristol-Myers Squibb Company Peptide inhibitors of Hepatitis C virus NS3 protein
AU2002230764A1 (en) 2000-12-13 2002-06-24 Bristol-Myers Squibb Pharma Company Imidazolidinones and their related derivatives as hepatitis c virus ns3 protease inhibitors
SK286630B6 (sk) 2001-01-22 2009-02-05 Merck & Co., Inc. Nukleozidové deriváty, farmaceutický prostriedok s ich obsahom a ich použitie
CN1235583C (zh) 2001-03-05 2006-01-11 特兰斯泰克制药公司 用作治疗剂的苯并咪唑衍生物
CA2449504A1 (en) 2001-07-11 2003-01-23 Vertex Pharmaceuticals Incorporated Bridged bicyclic serine protease inhibitors
US7241796B2 (en) 2001-10-24 2007-07-10 Vertex Pharmaceuticals Inc. Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US7119072B2 (en) 2002-01-30 2006-10-10 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis C virus
US7091184B2 (en) 2002-02-01 2006-08-15 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
US6642204B2 (en) 2002-02-01 2003-11-04 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
DK1482931T3 (da) 2002-03-05 2011-12-19 Transtech Pharma Inc Mono- og bicycliske azolderivater der inhiberer interaktionen af ligander med RAGE
KR20040099425A (ko) * 2002-04-11 2004-11-26 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 ｃ형 간염 바이러스 ｎｓ3-ｎｓ4프로테아제의 억제제
WO2004032827A2 (en) 2002-05-20 2004-04-22 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
JP4312711B2 (ja) 2002-05-20 2009-08-12 ブリストル−マイヤーズ スクイブ カンパニー ヘテロ環式スルホンアミドｃ型肝炎ウイルス阻害剤
JP4271148B2 (ja) 2002-05-20 2009-06-03 ブリストル−マイヤーズ スクイブ カンパニー 置換シクロアルキルｐ１’ｃ型肝炎ウイルスインヒビター
MY140680A (en) 2002-05-20 2010-01-15 Bristol Myers Squibb Co Hepatitis c virus inhibitors
US20050075279A1 (en) 2002-10-25 2005-04-07 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis C virus
JP2006526011A (ja) * 2003-04-11 2006-11-16 バーテックス　ファーマシューティカルズ　インコーポレイテッド セリンプロテアーゼ（特に、ｈｃｖｎｓ３−ｎｓ４ａプロテアーゼ）のインヒビター
WO2004092161A1 (en) * 2003-04-11 2004-10-28 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
KR101031825B1 (ko) 2003-04-18 2011-04-29 이난타 파마슈티칼스, 인코포레이티드 거대고리형 퀴녹살리닐 ｃ형 간염 세린 단백질분해효소억제제
CL2004001161A1 (es) 2003-05-21 2005-04-08 Boehringer Ingelheim Int Compuestos describe compuestos derivados de quinolina; composicion farmaceutica; y su uso para tratar una enfermedad causada por el virus de la hepatitis c.
CN1852920B (zh) 2003-07-18 2010-12-15 沃泰克斯药物股份有限公司 丝氨酸蛋白酶抑制剂、特别是hcv ns3-ns4a蛋白酶抑制剂
TWI359147B (en) 2003-09-05 2012-03-01 Vertex Pharma Inhibitors of serine proteases, particularly hcv n
EP1664091A1 (en) * 2003-09-18 2006-06-07 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
ES2361997T3 (es) 2003-09-22 2011-06-27 Boehringer Ingelheim International Gmbh Péptidos macrocíclicos activos contra el virus de la hepatitis c.
WO2005037860A2 (en) 2003-10-10 2005-04-28 Vertex Pharmaceuticals Incoporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
WO2005037214A2 (en) 2003-10-14 2005-04-28 Intermune, Inc. Macrocyclic carboxylic acids and acylsulfonamides as inhibitors of hcv replication
US8187874B2 (en) 2003-10-27 2012-05-29 Vertex Pharmaceuticals Incorporated Drug discovery method
EP1944042A1 (en) 2003-10-27 2008-07-16 Vertex Pharmceuticals Incorporated Combinations for HCV treatment
KR20060120166A (ko) 2003-10-27 2006-11-24 버텍스 파마슈티칼스 인코포레이티드 Ｈｃｖ ｎｓ３－ｎｓ４ａ 단백질분해효소 저항성 돌연변이
US7132504B2 (en) 2003-11-12 2006-11-07 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7135462B2 (en) 2003-11-20 2006-11-14 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7309708B2 (en) 2003-11-20 2007-12-18 Birstol-Myers Squibb Company Hepatitis C virus inhibitors
ATE495185T1 (de) 2004-01-21 2011-01-15 Boehringer Ingelheim Int Makrocyclische peptide mit wirkung gegen das hepatitis-c-virus
CN1938332B (zh) * 2004-02-04 2011-10-19 沃泰克斯药物股份有限公司 丝氨酸蛋白酶、特别是hcv ns3-ns4a蛋白酶的抑制剂
US20050182252A1 (en) 2004-02-13 2005-08-18 Reddy K. R. Novel 2'-C-methyl nucleoside derivatives
US20070049593A1 (en) 2004-02-24 2007-03-01 Japan Tobacco Inc. Tetracyclic fused heterocyclic compound and use thereof as HCV polymerase inhibitor
PT1719773E (pt) 2004-02-24 2009-06-03 Japan Tobacco Inc Compostos heterotetracíclicos fundidos e a sua utilização como inibidores da polimerase do hcv
CA2568379A1 (en) 2004-06-15 2005-12-29 Merck & Co., Inc. C-purine nucleoside analogs as inhibitors of rna-dependent rna viral polymerase
CA2571079A1 (en) 2004-06-24 2006-02-02 Merck & Co., Inc. Nucleoside aryl phosphoramidates for the treatment of rna-dependent rna viral infection
JP4914355B2 (ja) 2004-07-20 2012-04-11 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｃ型肝炎インヒビターペプチド類似体
UY29016A1 (es) 2004-07-20 2006-02-24 Boehringer Ingelheim Int Analogos de dipeptidos inhibidores de la hepatitis c
US7597884B2 (en) 2004-08-09 2009-10-06 Alios Biopharma, Inc. Hyperglycosylated polypeptide variants and methods of use
RU2007116265A (ru) 2004-10-01 2008-11-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибирование протеазы ns3-ns4a вируса hcv
US7659263B2 (en) 2004-11-12 2010-02-09 Japan Tobacco Inc. Thienopyrrole compound and use thereof as HCV polymerase inhibitor
AU2006242475B2 (en) 2005-05-02 2011-07-07 Merck Sharp & Dohme Corp. HCV NS3 protease inhibitors
TWI387603B (zh) 2005-07-20 2013-03-01 Merck Sharp & Dohme Ｈｃｖ ｎｓ３蛋白酶抑制劑
MX2008001166A (es) 2005-07-25 2008-03-18 Intermune Inc Nuevos inhibidores macrociclicos de la replicacion del virus de hepatitis c.
BRPI0614205A2 (pt) 2005-08-01 2016-11-22 Merck & Co Inc composto, composição farmacêutica, e, uso de composto
KR20080033481A (ko) * 2005-08-02 2008-04-16 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제의 억제제
CA2618560A1 (en) 2005-08-09 2007-02-22 Merck & Co., Inc. Ribonucleoside cyclic acetal derivatives for the treatment of rna-dependent rna viral infection
PL385229A1 (pl) 2005-08-19 2008-09-29 Vertex Pharmaceuticals Incorporated Sposoby i związki pośrednie
US8399615B2 (en) 2005-08-19 2013-03-19 Vertex Pharmaceuticals Incorporated Processes and intermediates
AR055395A1 (es) 2005-08-26 2007-08-22 Vertex Pharma Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c
US7964624B1 (en) 2005-08-26 2011-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
AU2006301966A1 (en) 2005-10-11 2007-04-19 Array Biopharma, Inc. Compounds and methods for inhibiting hepatitis C viral replication
EP2392589A3 (en) 2005-11-11 2012-06-20 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
US7705138B2 (en) 2005-11-11 2010-04-27 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
EP1991229A2 (en) 2006-02-27 2008-11-19 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
EP1993994A2 (en) 2006-03-16 2008-11-26 Vertex Pharmceuticals Incorporated Deuterated hepatitis c protease inhibitors
BRPI0710153A2 (pt) * 2006-04-11 2011-08-02 Novartis Ag compostos orgánicos e seus usos
US8017612B2 (en) 2006-04-18 2011-09-13 Japan Tobacco Inc. Piperazine compound and use thereof as a HCV polymerase inhibitor
GB0609492D0 (en) 2006-05-15 2006-06-21 Angeletti P Ist Richerche Bio Therapeutic agents
US8268776B2 (en) 2006-06-06 2012-09-18 Enanta Pharmaceuticals, Inc. Macrocylic oximyl hepatitis C protease inhibitors
US9526769B2 (en) 2006-06-06 2016-12-27 Enanta Pharmaceuticals, Inc. Macrocylic oximyl hepatitis C protease inhibitors
GB0612423D0 (en) 2006-06-23 2006-08-02 Angeletti P Ist Richerche Bio Therapeutic agents
EP1886685A1 (en) 2006-08-11 2008-02-13 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods, uses and compositions for modulating replication of hcv through the farnesoid x receptor (fxr) activation or inhibition
KR20090057035A (ko) * 2006-08-21 2009-06-03 유나이티드 세러퓨틱스 코오포레이션 바이러스 감염의 치료를 위한 병용 요법
WO2008027397A2 (en) * 2006-08-28 2008-03-06 Vertex Pharmaceuticals Incorporated Method for identifying protease inhibitors
JP2010507656A (ja) 2006-10-24 2010-03-11 メルク エンド カムパニー インコーポレーテッド Ｈｃｖｎｓ３プロテアーゼ阻害剤
US8138164B2 (en) 2006-10-24 2012-03-20 Merck Sharp & Dohme Corp. HCV NS3 protease inhibitors
CN101583372A (zh) 2006-10-24 2009-11-18 默克公司 Hcv ns3蛋白酶抑制剂
AU2007318164B2 (en) 2006-10-27 2013-02-07 Merck Sharp & Dohme Corp. HCV NS3 protease inhibitors
WO2008057209A1 (en) 2006-10-27 2008-05-15 Merck & Co., Inc. Hcv ns3 protease inhibitors
GB0625349D0 (en) 2006-12-20 2007-01-31 Angeletti P Ist Richerche Bio Therapeutic compounds
GB0625345D0 (en) 2006-12-20 2007-01-31 Angeletti P Ist Richerche Bio Therapeutic compounds
CN103224506A (zh) 2006-12-20 2013-07-31 P.安杰莱蒂分子生物学研究所 抗病毒的吲哚
JP5349332B2 (ja) * 2007-02-06 2013-11-20 チェルシー・セラピューティクス，インコーポレイテッド 新規化合物、その調製方法、およびその使用
DK2114924T3 (da) 2007-02-27 2012-04-10 Vertex Pharma Co-krystaller og farmaceutiske sammensætninger omfattende disse
JP2010519329A (ja) 2007-02-27 2010-06-03 バーテックス ファーマシューティカルズ インコーポレイテッド セリンプロテアーゼ阻害剤
JP2010520200A (ja) 2007-02-28 2010-06-10 クオナトウス ファーマシューティカルズ，インコーポレイテッド 特定のマトリックスメタロプロテイナーゼ（ｍｍｐ）阻害剤を使用する肝疾患を治療する方法
WO2008106167A1 (en) * 2007-02-28 2008-09-04 Conatus Pharmaceuticals, Inc. Combination therapy comprising matrix metalloproteinase inhibitors and caspase inhibitors for the treatment of liver diseases
US7964580B2 (en) * 2007-03-30 2011-06-21 Pharmasset, Inc. Nucleoside phosphoramidate prodrugs
EP2142215B1 (en) 2007-05-04 2012-03-07 Vertex Pharmceuticals Incorporated Combination therapy for the treatment of hcv infection
EA019749B1 (ru) 2007-06-29 2014-06-30 Джилид Сайэнс, Инк. Противовирусные соединения
WO2009005677A2 (en) 2007-06-29 2009-01-08 Gilead Sciences, Inc. Antiviral compounds
AU2008277440A1 (en) 2007-07-17 2009-01-22 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa Macrocyclic indole derivatives for the treatment of hepatitis C infections
AU2008277377B2 (en) 2007-07-19 2013-08-01 Msd Italia S.R.L. Macrocyclic compounds as antiviral agents
CN101835774B (zh) * 2007-08-30 2014-09-17 弗特克斯药品有限公司 共晶体和包含该共晶体的药物组合物
GB0718575D0 (en) 2007-09-24 2007-10-31 Angeletti P Ist Richerche Bio Nucleoside derivatives as inhibitors of viral polymerases
US8383583B2 (en) 2007-10-26 2013-02-26 Enanta Pharmaceuticals, Inc. Macrocyclic, pyridazinone-containing hepatitis C serine protease inhibitors
US8193346B2 (en) 2007-12-06 2012-06-05 Enanta Pharmaceuticals, Inc. Process for making macrocyclic oximyl hepatitis C protease inhibitors
WO2009117594A1 (en) 2008-03-20 2009-09-24 Enanta Pharmaceuticals, Inc. Fluorinated macrocyclic compounds as hepatitis c virus inhibitors
AU2009241445A1 (en) 2008-04-28 2009-11-05 Merck Sharp & Dohme Corp. HCV NS3 protease inhibitors
PT2540350E (pt) 2008-07-22 2014-08-27 Merck Sharp & Dohme Combinações de um composto de quinoxalina macrocílico o qual é um inibidor da protease ns3 do hcv com outros agentes do hcv
UY32099A (es) 2008-09-11 2010-04-30 Enanta Pharm Inc Inhibidores macrocíclicos de serina proteasas de hepatitis c
EP3025727A1 (en) 2008-10-02 2016-06-01 The J. David Gladstone Institutes Methods of treating liver disease
WO2010082050A1 (en) 2009-01-16 2010-07-22 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Macrocyclic and 7-aminoalkyl-substituted benzoxazocines for treatment of hepatitis c infections
GB0900914D0 (en) 2009-01-20 2009-03-04 Angeletti P Ist Richerche Bio Antiviral agents
EP2408449A4 (en) 2009-03-18 2012-08-08 Univ Leland Stanford Junior METHOD AND COMPOSITIONS FOR TREATING FLAVIVIRIDAE VIRUS INFECTIONS
US8828930B2 (en) 2009-07-30 2014-09-09 Merck Sharp & Dohme Corp. Hepatitis C virus NS3 protease inhibitors
HUE030402T2 (en) 2009-09-15 2017-05-29 Taigen Biotechnology Co Ltd HCV protease inhibitors
JP5805646B2 (ja) 2009-09-30 2015-11-04 ブイティーブイ・セラピューティクス・エルエルシー アルツハイマー病の治療のための置換イミダゾール誘導体
AU2011209051B2 (en) 2010-01-27 2015-01-15 AB Pharma Ltd. Polyheterocyclic compounds highly potent as HCV inhibitors
WO2012107589A1 (en) 2011-02-11 2012-08-16 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for the treatment and prevention of hcv infections
WO2012171332A1 (zh) 2011-06-16 2012-12-20 爱博新药研发(上海)有限公司 抑制丙型肝炎病毒的大环状杂环化合物及其制备和应用
WO2013072328A1 (en) 2011-11-14 2013-05-23 Sanofi Use of telaprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases
US9328138B2 (en) 2011-11-15 2016-05-03 Msd Italia S.R.L. HCV NS3 protease inhibitors
BR112014013649A2 (pt) 2011-12-06 2020-10-27 The Board Of Trustees Of The Leland Stanford Junior University métodos e agentes para o tratamento de doenças virais e usos dos referidos agentes
WO2013106344A1 (en) 2012-01-12 2013-07-18 Ligand Pharmaceuticals, Inc. 2 '-c-methyl nucleosides containing a cyclic phosphate diester of 1, 3-propanediol (2-oxo-[1, 3, 2]-dioxaphosphorinane) at position 5'
WO2014053533A1 (en) 2012-10-05 2014-04-10 Sanofi Use of substituted 3-heteroaroylamino-propionic acid derivatives as pharmaceuticals for prevention/treatment of atrial fibrillation
WO2014121418A1 (en) 2013-02-07 2014-08-14 Merck Sharp & Dohme Corp. Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis c
WO2014121417A1 (en) 2013-02-07 2014-08-14 Merck Sharp & Dohme Corp. Tetracyclic heterocycle compounds and methods of use thereof for the treatment of hepatitis c
EP2899207A1 (en) 2014-01-28 2015-07-29 Amikana.Biologics New method for testing HCV protease inhibition
AU2015217221A1 (en) 2014-02-13 2016-08-11 Ligand Pharmaceuticals, Inc. Prodrug compounds and their uses
CN106687118A (zh) 2014-07-02 2017-05-17 配体药物公司 前药化合物及其用途
CA3087932A1 (en) 2018-01-09 2019-07-18 Ligand Pharmaceuticals, Inc. Acetal compounds and therapeutic uses thereof
KR102835299B1 (ko) 2018-12-04 2025-07-18 브리스톨-마이어스 스큅 컴퍼니 다중 동위원소체 반응 모니터링에 의한 샘플내 보정 곡선을 사용한 분석 방법
CN114516810B (zh) * 2022-01-18 2023-12-26 浙江奥翔药业股份有限公司 制备药物中间体2-氨基-4-羟基苯甲酸的方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5798442A (en) * 1995-04-21 1998-08-25 Merck Frosst Canada, Inc. Peptidyl derivatives as inhibitors of pro-apoptotic cysteine proteinases
IT1283467B1 (it) * 1996-07-19 1998-04-21 Menarini Farma Ind Derivati di cicloalcani 1,2 sostituiti come inibitori della trombina, procedimento per la loro preparazione e loro impiego in formulazioni
KR100509388B1 (ko) * 1996-10-18 2005-08-23 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 간염 ｃ 바이러스 ｎｓ３ 프로테아제의 저해제
DE19648793A1 (de) * 1996-11-26 1998-05-28 Basf Ag Neue Benzamide und deren Anwendung
ES2234144T3 (es) * 1997-08-11 2005-06-16 Boehringer Ingelheim (Canada) Ltd. Analogos de peptidos inhibidores de la hepatitis c.

Also Published As

Publication number Publication date
ATE346035T1 (de) 2006-12-15
EP1066247A1 (en) 2001-01-10
US20040077600A1 (en) 2004-04-22
US20110112114A1 (en) 2011-05-12
DK1066247T3 (da) 2007-04-02
EP1066247B1 (en) 2006-11-22
DE69934104D1 (de) 2007-01-04
US6608067B1 (en) 2003-08-19
ES2281170T3 (es) 2007-09-16
WO1999050230A1 (en) 1999-10-07
JP2002509910A (ja) 2002-04-02
AU3376699A (en) 1999-10-18
DE69934104T2 (de) 2007-06-28

Similar Documents

Publication Publication Date Title
JP4690545B2 (ja) セリンプロテアーゼ、特にｃ型肝炎ウイルスｎｓ３プロテアーゼの阻害因子
JP4080541B2 (ja) セリンプロテアーゼ、特にｃ型肝炎ウイルスｎｓ３プロテアーゼの阻害因子
JP4806154B2 (ja) セリンプロテアーゼ、特にｃ型肝炎ウイルスｎｓ３プロテアーゼのインヒビター
EP1136498A1 (en) Inhibitors of serine proteases, particularly hepatitis c virus NS3 protease
AU719984C (en) Inhibitors of serine proteases, particularly hepatitis c virus NS3 protease
HK1167410A (en) Inhibitors of serine proteases, especially of the ns3 protease of the hepatitis c virus
HK1023779B (en) Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
HK1157355A (en) Inhibitors of hepatitis c virus ns3 serine protease
HK1039781A (en) Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
AU2012202576A1 (en) Inhibitors of Serine Proteases, Particularly HCV NS3-NS4A Protease

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20060323

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20060323

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20090729

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20090811

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20091110

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20091117

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20091211

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20091218

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20100212

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20100622

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20100922

A602 Written permission of extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A602

Effective date: 20100930

TRDD Decision of grant or rejection written
A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20110125

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20110218

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

FPAY Renewal fee payment (event date is renewal date of database)

Free format text: PAYMENT UNTIL: 20140225

Year of fee payment: 3

LAPS Cancellation because of no payment of annual fees