JP5394063B2 - セリンプロテアーゼの阻害剤 - Google Patents

セリンプロテアーゼの阻害剤 Download PDF

Info

Publication number
JP5394063B2
JP5394063B2 JP2008528258A JP2008528258A JP5394063B2 JP 5394063 B2 JP5394063 B2 JP 5394063B2 JP 2008528258 A JP2008528258 A JP 2008528258A JP 2008528258 A JP2008528258 A JP 2008528258A JP 5394063 B2 JP5394063 B2 JP 5394063B2
Authority
JP
Japan
Prior art keywords
optionally substituted
aliphatic
heterocycloaliphatic
cycloaliphatic
heteroaryl
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
JP2008528258A
Other languages
English (en)
Japanese (ja)
Other versions
JP2009506078A5 (enExample
JP2009506078A (ja
Inventor
ケビン・エム・コトレル
ジョン・マックスウェル
タン・キン
アンヌ−ロール・グリヨ
アルノー・ル・ティラン
エマヌエレ・ペローラ
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 JP2009506078A publication Critical patent/JP2009506078A/ja
Publication of JP2009506078A5 publication Critical patent/JP2009506078A5/ja
Application granted granted Critical
Publication of JP5394063B2 publication Critical patent/JP5394063B2/ja
Expired - Fee Related legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07D498/02—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 two hetero rings
    • C07D498/10—Spiro-condensed systems
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D498/20—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • 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
    • C07K5/06—Dipeptides
    • C07K5/06008—Dipeptides with the first amino acid being neutral
    • C07K5/06017—Dipeptides with the first amino acid being neutral and aliphatic
    • C07K5/06026—Dipeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atom, i.e. Gly or Ala
    • 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
    • C07K5/06191—Dipeptides containing heteroatoms different from O, S, or N
    • 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
    • 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
    • C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
    • C07K5/081—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing O or S as heteroatoms, e.g. Cys, Ser
    • 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
    • C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2008528258A 2005-08-26 2006-08-28 セリンプロテアーゼの阻害剤 Expired - Fee Related JP5394063B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US71153005P 2005-08-26 2005-08-26
US60/711,530 2005-08-26
PCT/US2006/033770 WO2007025307A2 (en) 2005-08-26 2006-08-28 Inhibitors of serine proteases

Publications (3)

Publication Number Publication Date
JP2009506078A JP2009506078A (ja) 2009-02-12
JP2009506078A5 JP2009506078A5 (enExample) 2009-10-15
JP5394063B2 true JP5394063B2 (ja) 2014-01-22

Family

ID=37684363

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2008528258A Expired - Fee Related JP5394063B2 (ja) 2005-08-26 2006-08-28 セリンプロテアーゼの阻害剤

Country Status (21)

Country Link
US (2) US7985762B2 (enExample)
EP (3) EP1917269B1 (enExample)
JP (1) JP5394063B2 (enExample)
KR (1) KR20080041715A (enExample)
CN (1) CN101316852A (enExample)
AR (1) AR055395A1 (enExample)
AT (1) ATE530554T1 (enExample)
AU (1) AU2006282771B2 (enExample)
BR (1) BRPI0615223A2 (enExample)
CA (1) CA2620621A1 (enExample)
EA (1) EA200800670A1 (enExample)
EC (1) ECSP088258A (enExample)
ES (1) ES2374943T3 (enExample)
GE (1) GEP20115280B (enExample)
IL (1) IL189668A0 (enExample)
MX (1) MX2008002606A (enExample)
NO (1) NO20081467L (enExample)
NZ (1) NZ566197A (enExample)
TW (1) TW200730533A (enExample)
WO (1) WO2007025307A2 (enExample)
ZA (1) ZA200801793B (enExample)

Families Citing this family (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA001915B1 (ru) * 1996-10-18 2001-10-22 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы серин-протеаз, в частности ns3 протеазы вируса гепатита c (hvc)
IL152022A0 (en) * 2000-04-03 2003-04-10 Vertex Pharma Compounds useful as protease inhibitors and pharmaceutical compositions containing the same
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
MY140680A (en) 2002-05-20 2010-01-15 Bristol Myers Squibb Co Hepatitis c virus inhibitors
TW200510391A (en) * 2003-04-11 2005-03-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
AU2004257288A1 (en) * 2003-07-18 2005-01-27 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
TW201127828A (en) * 2003-09-05 2011-08-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US20050119189A1 (en) * 2003-09-18 2005-06-02 Cottrell Kevin M. Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
CA2541634A1 (en) * 2003-10-10 2005-04-28 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
KR20060120162A (ko) * 2003-10-27 2006-11-24 버텍스 파마슈티칼스 인코포레이티드 Ｈｃｖ 치료용 배합물
EP1711515A2 (en) * 2004-02-04 2006-10-18 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
EP2305697A3 (en) 2005-07-25 2011-07-27 Intermune, Inc. Macrocyclic inhibitors of Hepatitis C virus replication
US8399615B2 (en) 2005-08-19 2013-03-19 Vertex Pharmaceuticals Incorporated Processes and intermediates
US7964624B1 (en) * 2005-08-26 2011-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
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
US8039475B2 (en) 2006-02-27 2011-10-18 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
KR20080112303A (ko) 2006-03-16 2008-12-24 버텍스 파마슈티칼스 인코포레이티드 중수소화 ｃ형 간염 프로테아제 억제제
KR101059593B1 (ko) 2006-04-11 2011-08-25 노파르티스 아게 Ｈｃｖ/ｈｉｖ 억제제 및 이들의 용도
EP2049474B1 (en) 2006-07-11 2015-11-04 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
JP2010502184A (ja) * 2006-08-28 2010-01-28 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 プロテアーゼ阻害剤の同定方法
AU2007298549A1 (en) * 2006-09-22 2008-03-27 Ranbaxy Laboratories Limited Inhibitors of phosphodiesterase type-IV
US8343477B2 (en) 2006-11-01 2013-01-01 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus
US7772180B2 (en) 2006-11-09 2010-08-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8003604B2 (en) 2006-11-16 2011-08-23 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7888464B2 (en) 2006-11-16 2011-02-15 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7763584B2 (en) 2006-11-16 2010-07-27 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2008106130A2 (en) * 2007-02-26 2008-09-04 Achillion Pharmaceuticals, Inc. Tertiary amine substituted peptides useful as inhibitors of hcv replication
EA200970806A1 (ru) 2007-02-27 2010-08-30 Вертекс Фармасьютикалз Инкорпорейтед Сокристаллы и содержащие их фармацевтические композиции
NZ579295A (en) 2007-02-27 2012-03-30 Vertex Pharma Inhibitors of serine proteases
FR2914920B1 (fr) * 2007-04-11 2011-09-09 Clariant Specialty Fine Chem F Procede de deacetalisation d'alpha-aminoacetals.
EP2494991A1 (en) 2007-05-04 2012-09-05 Vertex Pharmaceuticals Incorporated Combination therapy for the treatment of HCV infection
US7932277B2 (en) * 2007-05-10 2011-04-26 Intermune, Inc. Peptide inhibitors of hepatitis C virus replication
EP2100881A1 (en) * 2008-03-13 2009-09-16 Laboratorios Almirall, S.A. Pyrimidyl- or pyridinylaminobenzoic acid derivatives
UY31272A1 (es) * 2007-08-10 2009-01-30 Almirall Lab Nuevos derivados de ácido azabifenilaminobenzoico
WO2009032198A1 (en) 2007-08-30 2009-03-12 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
MX2010003916A (es) 2007-10-10 2010-05-05 Novartis Ag Espiro-pirrolidinas y su uso contra infeccion por el virus de hepatitis c (hcv) y por el virus de inmunodeficiencia humana (vih).
WO2009053828A2 (en) * 2007-10-22 2009-04-30 Enanta Pharmaceuticals, Inc. P3 hydroxyamino macrocyclic hepatitis c serine protease inhibitors
US8383583B2 (en) 2007-10-26 2013-02-26 Enanta Pharmaceuticals, Inc. Macrocyclic, pyridazinone-containing hepatitis C serine protease inhibitors
US8202996B2 (en) 2007-12-21 2012-06-19 Bristol-Myers Squibb Company Crystalline forms of N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-((7-chloro-4-methoxy-1-isoquinolinyl)oxy)-N- ((1R,2S)-1-((cyclopropylsulfonyl)carbamoyl)-2-vinylcyclopropyl)-L-prolinamide
NZ587133A (en) 2008-02-04 2012-10-26 Idenix Pharmaceuticals Inc Macrocyclic serine protease inhibitor compounds for treating an HCV infection
US8372802B2 (en) 2008-03-20 2013-02-12 Enanta Pharmaceuticals, Inc. Fluorinated macrocyclic compounds as hepatitis C virus inhibitors
US8163921B2 (en) 2008-04-16 2012-04-24 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7964560B2 (en) 2008-05-29 2011-06-21 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8044023B2 (en) 2008-05-29 2011-10-25 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8207341B2 (en) 2008-09-04 2012-06-26 Bristol-Myers Squibb Company Process or synthesizing substituted isoquinolines
UY32099A (es) 2008-09-11 2010-04-30 Enanta Pharm Inc Inhibidores macrocíclicos de serina proteasas de hepatitis c
US8044087B2 (en) 2008-09-29 2011-10-25 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US8563505B2 (en) 2008-09-29 2013-10-22 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
CA2740728A1 (en) * 2008-10-15 2010-04-22 Intermune, Inc. Therapeutic antiviral peptides
US8283310B2 (en) 2008-12-15 2012-10-09 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP2210615A1 (en) * 2009-01-21 2010-07-28 Almirall, S.A. Combinations comprising methotrexate and DHODH inhibitors
CA2758072A1 (en) 2009-04-08 2010-10-14 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors
US8512690B2 (en) 2009-04-10 2013-08-20 Novartis Ag Derivatised proline containing peptide compounds as protease inhibitors
US8232246B2 (en) * 2009-06-30 2012-07-31 Abbott Laboratories Anti-viral compounds
CA2769652A1 (en) 2009-08-05 2011-02-10 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors useful against viral infections, particularly hcv
WO2011041551A1 (en) * 2009-10-01 2011-04-07 Intermune, Inc. Therapeutic antiviral peptides
JP2013529210A (ja) * 2010-05-18 2013-07-18 メルク・シャープ・エンド・ドーム・コーポレイション Ｓｓｔｒ５アンタゴニストとしてのスピロイソオキサゾリン化合物
WO2011156545A1 (en) 2010-06-09 2011-12-15 Vertex Pharmaceuticals Incorporated Viral dynamic model for hcv combination therapy
US8742110B2 (en) 2010-08-18 2014-06-03 Merck Sharp & Dohme Corp. Spiroxazolidinone compounds
US8951964B2 (en) 2010-12-30 2015-02-10 Abbvie Inc. Phenanthridine macrocyclic hepatitis C serine protease inhibitors
CN103534256B (zh) 2010-12-30 2016-08-10 益安药业 大环丙型肝炎丝氨酸蛋白酶抑制剂
TW201309690A (zh) 2011-02-10 2013-03-01 Idenix Pharmaceuticals Inc 巨環絲胺酸蛋白酶抑制劑，其醫藥組合物及其於治療ｈｃｖ感染之用途
US8957203B2 (en) 2011-05-05 2015-02-17 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US10201584B1 (en) 2011-05-17 2019-02-12 Abbvie Inc. Compositions and methods for treating HCV
US8691757B2 (en) 2011-06-15 2014-04-08 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
CN103304571B (zh) * 2012-03-06 2018-02-16 凯惠科技发展(上海)有限公司 螺环化合物、其制备方法、中间体、药物组合物和应用
TW201408669A (zh) 2012-08-08 2014-03-01 Merck Sharp & Dohme Ｈｃｖ ｎｓ３蛋白酶抑制劑
DK2909205T3 (en) 2012-10-19 2017-03-06 Bristol Myers Squibb Co 9-METHYL-SUBSTITUTED HEXADECAHYDROCYCLOPROPA (E) PYRROL (1,2-A) (1,4) DIAZOCYCLOPENTADECINYLCARBAMATE DERIVATIVES AS NON-STRUCTURAL 3 (NS3) PROTEASE INHIBITORS FOR TREATMENT
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
US9334279B2 (en) 2012-11-02 2016-05-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
WO2014070974A1 (en) 2012-11-05 2014-05-08 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
FR3000064A1 (fr) * 2012-12-21 2014-06-27 Univ Lille Ii Droit & Sante Composes de type spiroisoxazoline ayant une activite potentialisatrice de l'activite d'un antibiotique-composition et produit pharmaceutiques comprenant de tels composes
EP2964664B1 (en) 2013-03-07 2017-01-11 Bristol-Myers Squibb Company Hepatitis c virus inhibitors
EP2883876A1 (en) 2013-12-16 2015-06-17 Actelion Pharmaceuticals Ltd. Stereoselective synthesis of substituted pyrrolidines
WO2015103490A1 (en) 2014-01-03 2015-07-09 Abbvie, Inc. Solid antiviral dosage forms
US11130780B2 (en) 2015-03-09 2021-09-28 Washington University Inhibitors of growth factor activation enzymes
MX375424B (es) 2015-07-31 2025-03-06 Pfizer Derivados de 1,1,1-trifluoro-3-hidroxipropan-2-il carbamato y derivados de 1,1,1-trifluoro-4- hidroxibutan-2-il carbamato como inhibidores de magl
EP3426674A4 (en) 2016-03-09 2019-08-14 Blade Therapeutics, Inc. CYCLIC KETO AMID COMPOUNDS AS CALPAIN MODULATORS AND METHOD FOR THE PRODUCTION AND USE THEREOF
KR102512201B1 (ko) * 2016-06-21 2023-03-20 오리온 옵탈몰로지 엘엘씨 지방족 프롤린아미드 유도체
EP3481835A4 (en) 2016-07-05 2020-02-26 Blade Therapeutics, Inc. CALPAIN MODULATORS AND THEIR THERAPEUTIC USES
US10934261B2 (en) 2016-09-28 2021-03-02 Blade Therapeutics, Inc. Calpain modulators and therapeutic uses thereof
MX2019008626A (es) 2017-01-20 2019-09-19 Pfizer Derivados de 1,1,1-trifluoro-3-hidroxipropan-2-ilcarbamato como inhibidores de monoacilglicerol lipasa (magl).
SG11201906427QA (en) 2017-01-23 2019-08-27 Pfizer Heterocyclic spiro compounds as magl inhibitors
RU2650610C1 (ru) 2017-02-28 2018-04-16 Васильевич Иващенко Александр Противовирусная композиция и способ ее применения
CN107954990A (zh) * 2017-11-14 2018-04-24 安徽诺全药业有限公司 一种雷迪帕维的制备方法
PE20212111A1 (es) * 2018-03-28 2021-11-04 Blade Therapeutics Inc Moduladores calpaina y usos terapeuticos de los mismos

Family Cites Families (194)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US472484A (en) * 1892-04-05 Pneumatic tire
US633770A (en) 1898-10-15 1899-09-26 Diven Brothers & Company Rotary plow.
US3025516A (en) * 1952-11-03 1962-03-13 Stewart Warner Corp Frequency control system for radio identification apparatus
DE3226768A1 (de) 1981-11-05 1983-05-26 Hoechst Ag, 6230 Frankfurt Derivate der cis, endo-2-azabicyclo-(3.3.0)-octan-3-carbonsaeure, verfahren zu ihrer herstellung, diese enthaltende mittel und deren verwendung
DE3211676A1 (de) 1982-03-30 1983-10-06 Hoechst Ag Neue derivate von cycloalka (c) pyrrol-carbonsaeuren, verfahren zu ihrer herstellung, diese enthaltende mittel und deren verwendung sowie neue cycloalka (c) pyrrol-carbonsaeuren als zwischenstufen und verfahren zu deren herstellung
US4499082A (en) * 1983-12-05 1985-02-12 E. I. Du Pont De Nemours And Company α-Aminoboronic acid peptides
FR2575753B1 (fr) 1985-01-07 1987-02-20 Adir Nouveaux derives peptidiques a structure polycyclique azotee, leur procede de preparation et les compositions pharmaceutiques qui les contiennent
US5496927A (en) 1985-02-04 1996-03-05 Merrell Pharmaceuticals Inc. Peptidase inhibitors
EP0204571B1 (en) 1985-06-07 1992-01-22 Ici Americas Inc. Selected difluoro derivatives
US5231084A (en) * 1986-03-27 1993-07-27 Hoechst Aktiengesellschaft Compounds having a cognition adjuvant action, agents containing them, and the use thereof for the treatment and prophylaxis of cognitive dysfuncitons
US5736520A (en) * 1988-10-07 1998-04-07 Merrell Pharmaceuticals Inc. Peptidase inhibitors
NZ235155A (en) 1989-09-11 1993-04-28 Merrell Dow Pharma Peptidase substrates in which the carboxy terminal group has been replaced by a tricarbonyl radical
DE4019586A1 (de) * 1990-06-20 1992-01-02 Bosch Gmbh Robert Kraftstoffeinspritzsystem fuer brennkraftmaschinen
US5371072A (en) 1992-10-16 1994-12-06 Corvas International, Inc. Asp-Pro-Arg α-keto-amide enzyme inhibitors
ES2150933T3 (es) * 1992-12-22 2000-12-16 Lilly Co Eli Inhibidores de la proteasa vih utiles para el tratamiento del sida.
CA2605872A1 (en) 1992-12-29 1994-06-30 Abbott Laboratories Intermediates for retroviral protease inhibiting compounds
US5384410A (en) * 1993-03-24 1995-01-24 The Du Pont Merck Pharmaceutical Company Removal of boronic acid protecting groups by transesterification
US5656600A (en) 1993-03-25 1997-08-12 Corvas International, Inc. α-ketoamide derivatives as inhibitors of thrombosis
US5672582A (en) 1993-04-30 1997-09-30 Merck & Co., Inc. Thrombin inhibitors
IL110752A (en) 1993-09-13 2000-07-26 Abbott Lab Liquid semi-solid or solid pharmaceutical composition for an HIV protease inhibitor
US5559158A (en) 1993-10-01 1996-09-24 Abbott Laboratories Pharmaceutical composition
US5468858A (en) 1993-10-28 1995-11-21 The Board Of Regents Of Oklahoma State University Physical Sciences N-alkyl and n-acyl derivatives of 3,7-diazabicyclo-[3.3.1]nonanes and selected salts thereof as multi-class antiarrhythmic agents
IL111991A (en) * 1994-01-28 2000-07-26 Abbott Lab Liquid pharmaceutical composition of HIV protease inhibitors in organic solvent
RU95104898A (ru) 1994-03-31 1996-12-27 Бристоль-Мейерз Сквибб Компани (US) Имидазолсодержащие ингибиторы фарнезид-протеинтрансферазы, способ лечения связанных с ней заболеваний
US6420522B1 (en) 1995-06-05 2002-07-16 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1β converting enzyme
US5756466A (en) 1994-06-17 1998-05-26 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5847135A (en) 1994-06-17 1998-12-08 Vertex Pharmaceuticals, Incorporated Inhibitors of interleukin-1β converting enzyme
US5716929A (en) 1994-06-17 1998-02-10 Vertex Pharmaceuticals, Inc. Inhibitors of interleukin-1β converting enzyme
US5861267A (en) * 1995-05-01 1999-01-19 Vertex Pharmaceuticals Incorporated Methods, nucleotide sequences and host cells for assaying exogenous and endogenous protease activity
US6037157A (en) 1995-06-29 2000-03-14 Abbott Laboratories Method for improving pharmacokinetics
US6060469A (en) * 1995-11-23 2000-05-09 Merck Sharp & Dohme Ltd. Spiro-piperidine derivatives and their use as tachykinin antagonists
US6054472A (en) * 1996-04-23 2000-04-25 Vertex Pharmaceuticals, Incorporated Inhibitors of IMPDH enzyme
US5807876A (en) 1996-04-23 1998-09-15 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
ZA972195B (en) * 1996-03-15 1998-09-14 Du Pont Merck Pharma Spirocycle integrin inhibitors
HUP0004421A3 (en) * 1996-04-23 2002-10-28 Vertex Pharmaceuticals Inc Cam Urea derivatives and pharmaceutical compositions containing them, use thereof for the treatment of deseases mediated by impdh enzyme
US5990276A (en) 1996-05-10 1999-11-23 Schering Corporation Synthetic inhibitors of hepatitis C virus NS3 protease
EP0907659A1 (en) 1996-05-10 1999-04-14 Schering Corporation Synthetic inhibitors of hepatitis c virus ns3 protease
US6153579A (en) 1996-09-12 2000-11-28 Vertex Pharmaceuticals, Incorporated Crystallizable compositions comprising a hepatitis C virus NS3 protease domain/NS4A complex
AU723414B2 (en) * 1996-09-25 2000-08-24 Merck Sharp & Dohme Limited Spiro-azacyclic derivatives, their preparation and their use as tachykinin antagonists
US6348608B1 (en) * 1996-10-08 2002-02-19 Yian Shi Catalytic asymmetric epoxidation
EA001915B1 (ru) * 1996-10-18 2001-10-22 Вертекс Фармасьютикалз Инкорпорейтед Ингибиторы серин-протеаз, в частности ns3 протеазы вируса гепатита c (hvc)
GB9623908D0 (en) 1996-11-18 1997-01-08 Hoffmann La Roche Amino acid derivatives
DE19648011A1 (de) * 1996-11-20 1998-05-28 Bayer Ag Cyclische Imine
PT966465E (pt) * 1997-03-14 2003-11-28 Vertex Pharma Inibidores do enzima imfdh
GB9707659D0 (en) 1997-04-16 1997-06-04 Peptide Therapeutics Ltd Hepatitis C NS3 Protease inhibitors
GB9708484D0 (en) * 1997-04-25 1997-06-18 Merck Sharp & Dohme Therapeutic agents
GB9711114D0 (en) * 1997-05-29 1997-07-23 Merck Sharp & Dohme Therapeutic agents
US6767991B1 (en) 1997-08-11 2004-07-27 Boehringer Ingelheim (Canada) Ltd. Hepatitis C inhibitor peptides
AU757072B2 (en) 1997-08-11 2003-01-30 Boehringer Ingelheim (Canada) Ltd. Hepatitis C inhibitor peptide analogues
DK1003775T3 (da) 1997-08-11 2005-05-30 Boehringer Ingelheim Ca Ltd Hepatitis C-inhibitorpeptider
US6183121B1 (en) * 1997-08-14 2001-02-06 Vertex Pharmaceuticals Inc. Hepatitis C virus helicase crystals and coordinates that define helicase binding pockets
US20040058982A1 (en) * 1999-02-17 2004-03-25 Bioavailability System, Llc Pharmaceutical compositions
US20020017295A1 (en) * 2000-07-07 2002-02-14 Weers Jeffry G. Phospholipid-based powders for inhalation
US6211338B1 (en) * 1997-11-28 2001-04-03 Schering Corporation Single-chain recombinant complexes of hepatitis C virus NS3 protease and NS4A cofactor peptide
IT1299134B1 (it) 1998-02-02 2000-02-29 Angeletti P Ist Richerche Bio Procedimento per la produzione di peptidi con proprieta' inibitrici della proteasi ns3 del virus hcv, peptidi cosi' ottenibili e peptidi
JP4690545B2 (ja) 1998-03-31 2011-06-01 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ｃ型肝炎ウイルスｎｓ３プロテアーゼの阻害因子
US6251583B1 (en) 1998-04-27 2001-06-26 Schering Corporation Peptide substrates for HCV NS3 protease assays
GB9812523D0 (en) 1998-06-10 1998-08-05 Angeletti P Ist Richerche Bio Peptide inhibitors of hepatitis c virus ns3 protease
US6323180B1 (en) 1998-08-10 2001-11-27 Boehringer Ingelheim (Canada) Ltd Hepatitis C inhibitor tri-peptides
DE19836514A1 (de) * 1998-08-12 2000-02-17 Univ Stuttgart Modifikation von Engineeringpolymeren mit N-basischen Gruppe und mit Ionenaustauschergruppen in der Seitenkette
US6117639A (en) 1998-08-31 2000-09-12 Vertex Pharmaceuticals Incorporated Fusion proteins, DNA molecules, vectors, and host cells useful for measuring protease activity
US6025516A (en) 1998-10-14 2000-02-15 Chiragene, Inc. Resolution of 2-hydroxy-3-amino-3-phenylpropionamide and its conversion to C-13 sidechain of taxanes
GB9825946D0 (en) 1998-11-26 1999-01-20 Angeletti P Ist Richerche Bio Pharmaceutical compounds for the inhibition of hepatitis C virus NS3 protease
EP1970052A2 (en) * 1999-02-09 2008-09-17 Pfizer Products Inc. Basic drug compositions with enhanced bioavailability
US20020042046A1 (en) * 1999-02-25 2002-04-11 Vertex Pharmaceuticals, Incorporated Crystallizable compositions comprising a hepatitis C virus NS3 protease domain/NS4A complex
AR029341A1 (es) 1999-03-19 2003-06-25 Vertex Pharma Inhibidores de la enzima impdh (inosina-5'-monofosfato dehidrogenasa)
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
US7122627B2 (en) * 1999-07-26 2006-10-17 Bristol-Myers Squibb Company Lactam inhibitors of Hepatitis C virus NS3 protease
WO2001007407A1 (en) 1999-07-26 2001-02-01 Bristol-Myers Squibb Pharma Company Lactam inhibitors of hepatitis c virus ns3 protease
US20020183249A1 (en) 1999-08-31 2002-12-05 Taylor Neil R. Method of identifying inhibitors of CDC25
GB9925955D0 (en) 1999-11-02 1999-12-29 Angeletti P Ist Richerche Bio Hcv n33 protease inhibitors
AU2055301A (en) 1999-12-03 2001-06-12 Bristol-Myers Squibb Pharma Company Alpha-ketoamide inhibitors of hepatitis c virus ns3 protease
AU2001234837A1 (en) 2000-02-08 2001-08-20 Schering Corporation Azapeptides useful in the treatment of hepatitis c
CA2396504A1 (en) * 2000-02-29 2001-09-07 Dupont Pharmaceuticals Company Inhibitors of hepatitis c virus ns3 protease
IL152022A0 (en) 2000-04-03 2003-04-10 Vertex Pharma Compounds useful as protease inhibitors and pharmaceutical compositions containing the same
CZ20023321A3 (cs) * 2000-04-05 2003-01-15 Schering Corporation Makrocyklická sloučenina a farmaceutický prostředek
CN101580536A (zh) * 2000-04-19 2009-11-18 先灵公司 含有烷基和芳基丙氨酸p2部分的丙型肝炎病毒的大环ns3-丝氨酸蛋白酶抑制剂
EP1295876A4 (en) 2000-06-30 2005-10-19 EPOXYCARBOXYLIC AMIDE, AZIDE AND AMINO ALCOHOLS AND THEIR USE IN PROCESSES FOR THE PREPARATION OF ALPHA KETOAMIDES
CA2416603A1 (en) 2000-07-20 2003-01-31 Merck & Co., Inc. Inhibiting hepatitis c virus processing and replication
US7012066B2 (en) 2000-07-21 2006-03-14 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
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
CA2418199A1 (en) 2000-07-21 2002-01-31 Corvas International, Inc. Peptides as ns3-serine protease inhibitors of hepatitis c virus
AR029851A1 (es) 2000-07-21 2003-07-16 Dendreon Corp Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c
US7244721B2 (en) 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
HUP0303358A3 (en) 2000-07-21 2005-10-28 Schering Corp Novel peptides as ns3-serine protease inhibitors of hepatitis c virus and pharmaceutical compositions containing them
US6777400B2 (en) 2000-08-05 2004-08-17 Smithkline Beecham Corporation Anti-inflammatory androstane derivative compositions
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
US6939692B2 (en) 2000-09-12 2005-09-06 Degussa Ag Nucleotide sequences coding for the pknB gene
US6846806B2 (en) 2000-10-23 2005-01-25 Bristol-Myers Squibb Company Peptide inhibitors of Hepatitis C virus NS3 protein
JP3889708B2 (ja) 2000-11-20 2007-03-07 ブリストル−マイヤーズ スクイブ カンパニー Ｃ型肝炎トリペプチド阻害剤
EP1343807B1 (en) 2000-12-12 2009-04-29 Schering Corporation Diaryl peptides as ns3-serine protease inhibitors of hepatits c virus
WO2002048157A2 (en) 2000-12-13 2002-06-20 Bristol-Myers Squibb Pharma Company Imidazolidinones and their related derivatives as hepatitis c virus ns3 protease inhibitors
US6653295B2 (en) * 2000-12-13 2003-11-25 Bristol-Myers Squibb Company Inhibitors of hepatitis C virus NS3 protease
WO2002048116A2 (en) 2000-12-13 2002-06-20 Bristol-Myers Squibb Pharma Company Inhibitors of hepatitis c virus ns3 protease
BR0206614A (pt) * 2001-01-22 2004-02-17 Merck & Co Inc Composto, composição farmacêutica, método para inibir a polimerase viral de rna dependente de rna e/ou inibir a replicação viral de rna dependente de rna, método para tratar uma infecção viral de rna dependente de rna, e, uso de um composto
WO2002061149A2 (en) 2001-01-30 2002-08-08 Vertex Pharmaceuticals Incorporated A quantitative assay for nucleic acids
GB0102342D0 (en) * 2001-01-30 2001-03-14 Smithkline Beecham Plc Pharmaceutical formulation
MXPA03008882A (es) 2001-03-27 2003-12-08 Vertex Pharma Composiciones y metodos utiles para la infeccion por hcv.
GB0107924D0 (en) 2001-03-29 2001-05-23 Angeletti P Ist Richerche Bio Inhibitor of hepatitis C virus NS3 protease
CA2450545A1 (en) * 2001-07-03 2003-01-16 Altana Pharma Ag Process for the production of 3-phenylisoserine
US6909000B2 (en) 2001-07-11 2005-06-21 Vertex Pharmaceuticals Incorporated Bridged bicyclic serine protease inhibitors
JP2003055389A (ja) 2001-08-09 2003-02-26 Univ Tokyo 錯体及びそれを用いたエポキシドの製法
US6824769B2 (en) * 2001-08-28 2004-11-30 Vertex Pharmaceuticals Incorporated Optimal compositions and methods thereof for treating HCV infections
AU2002348414B2 (en) * 2001-10-24 2009-10-01 Vertex Pharmaceuticals Incorporated Inhibitors of serine protease, particularly hepatitis C virus NS3-NS4A protease, incorporating a fused ring system
CA2465597A1 (en) * 2001-11-14 2003-06-12 Ben Zion Dolitzky Amorphous and crystalline forms of losartan potassium and process for their preparation
AU2003207625B2 (en) 2002-01-23 2006-09-07 Schering Corporation Proline compounds as NS3-serine protease inhibitors for use in treatment of hepatites C virus infection
CA2369711A1 (en) 2002-01-30 2003-07-30 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis c virus
CA2370396A1 (en) 2002-02-01 2003-08-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor tri-peptides
AR038375A1 (es) 2002-02-01 2005-01-12 Pfizer Prod Inc Composiciones farmaceuticas de inhibidores de la proteina de transferencia de esteres de colesterilo
US6642204B2 (en) 2002-02-01 2003-11-04 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
CA2369970A1 (en) 2002-02-01 2003-08-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor tri-peptides
US7091184B2 (en) 2002-02-01 2006-08-15 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
EP1497282A2 (en) 2002-04-11 2005-01-19 Vertex Pharmaceuticals Incorporated Inhibitors of serine protease, particularly hepatitis c virus ns3-ns4 protease
PL215228B1 (pl) 2002-05-20 2013-11-29 Bristol Myers Squibb Co Zwiazki tripeptydowe, ich zastosowanie i kompozycja farmaceutyczna je zawierajaca oraz jej zastosowanie
KR20050040912A (ko) * 2002-08-01 2005-05-03 파마셋 인코포레이티드 플라비비리다에 감염 치료용의 비사이클로[4.2.1]노난시스템을 가지는 화합물
WO2004026896A2 (en) 2002-09-23 2004-04-01 Medivir Ab Hcv ns-3 serine protease inhibitors
US20040138109A1 (en) 2002-09-30 2004-07-15 Boehringer Ingelheim Pharmaceuticals, Inc. Potent inhibitor of HCV serine protease
US20050075279A1 (en) 2002-10-25 2005-04-07 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis C virus
US20050159345A1 (en) 2002-10-29 2005-07-21 Boehringer Ingelheim International Gmbh Composition for the treatment of infection by Flaviviridae viruses
CA2413705A1 (en) * 2002-12-06 2004-06-06 Raul Altman Use of meloxicam in combination with an antiplatelet agent for treatment of acute coronary syndrome and related conditions
US7601709B2 (en) 2003-02-07 2009-10-13 Enanta Pharmaceuticals, Inc. Macrocyclic hepatitis C serine protease inhibitors
US7223785B2 (en) 2003-01-22 2007-05-29 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
US7098231B2 (en) 2003-01-22 2006-08-29 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
US20040180815A1 (en) 2003-03-07 2004-09-16 Suanne Nakajima Pyridazinonyl macrocyclic hepatitis C serine protease inhibitors
EP1590442A4 (en) 2003-02-07 2007-07-18 Enanta Pharm Inc MACROCYCLIC HEPATITIS C SERIN PROTEASE INHIBITORS
MXPA05008106A (es) 2003-02-18 2005-09-21 Pfizer Inhibidores del virus de la hepatitis c, composiciones y tratamientos que los emplean.
CA2516018C (en) 2003-03-05 2011-08-23 Boehringer Ingelheim International Gmbh Hepatitis c inhibitor peptide analogs
WO2004101605A1 (en) 2003-03-05 2004-11-25 Boehringer Ingelheim International Gmbh Hepatitis c inhibiting compounds
EP1615949A1 (en) 2003-04-10 2006-01-18 Boehringer Ingelheim International GmbH Process for the preparation of macrocyclic compounds by ruthenium complex catalysed metathesis reaction
TW200510391A (en) * 2003-04-11 2005-03-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
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
DE602004019518D1 (de) 2003-04-16 2009-04-02 Bristol Myers Squibb Co Makrocyclische isochinolinpeptidinhibitoren des hepatitis-c-virus
EP2143727B1 (en) 2003-04-18 2015-01-21 Enanta Pharmaceuticals, Inc. Quinoxalinyl macrocyclic hepatitis C serine protease inhibitors
EP1654261B1 (en) 2003-05-21 2007-11-14 Boehringer Ingelheim International GmbH Hepatitis c inhibitor compounds
WO2004113365A2 (en) 2003-06-05 2004-12-29 Enanta Pharmaceuticals, Inc. Hepatitis c serine protease tri-peptide inhibitors
US7125845B2 (en) 2003-07-03 2006-10-24 Enanta Pharmaceuticals, Inc. Aza-peptide macrocyclic hepatitis C serine protease inhibitors
AU2004257288A1 (en) 2003-07-18 2005-01-27 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
WO2005018330A1 (en) * 2003-08-18 2005-03-03 Pharmasset, Inc. Dosing regimen for flaviviridae therapy
EP1664090A2 (en) 2003-08-26 2006-06-07 Schering Corporation Novel peptidomimetic ns3-serine protease inhibitors of hepatitis c virus
TW201127828A (en) 2003-09-05 2011-08-16 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
NZ545871A (en) * 2003-09-12 2010-04-30 Vertex Pharma Animal model for protease activity and liver damage
US20050119189A1 (en) * 2003-09-18 2005-06-02 Cottrell Kevin M. Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US6933760B2 (en) * 2003-09-19 2005-08-23 Intel Corporation Reference voltage generator for hysteresis circuit
DE602004031645D1 (de) * 2003-09-22 2011-04-14 Boehringer Ingelheim Pharma Makrozyklische peptide mit wirkung gegen das hepatitis-c-virus
EP1664092B1 (en) 2003-09-26 2011-02-02 Schering Corporation Macrocyclic inhibitors of hepatitis c virus ns3 serine protease
CA2541634A1 (en) 2003-10-10 2005-04-28 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
AR045870A1 (es) * 2003-10-11 2005-11-16 Vertex Pharma Terapia de combinacion para la infeccion de virus de hepatitis c
RS20060259A (sr) 2003-10-14 2008-08-07 Intermune Inc., Makrociklične karboksilne kiseline i acilsulfonamidi kao inhibitori replikacije hcv
KR20060120162A (ko) * 2003-10-27 2006-11-24 버텍스 파마슈티칼스 인코포레이티드 Ｈｃｖ 치료용 배합물
WO2005043118A2 (en) * 2003-10-27 2005-05-12 Vertex Pharmaceuticals Incorporated Drug discovery method
AU2004285019B9 (en) * 2003-10-27 2011-11-24 Vertex Pharmaceuticals Incorporated HCV NS3-NS4A protease resistance mutants
JP4942485B2 (ja) 2003-10-28 2012-05-30 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 Ｆｉｓｃｈｅｒ−ｆｉｎｋ型合成および続くアシル化による４，５−ジアルキル−３−アシル−ピロール−２−カルボン酸誘導体の製造
US20050119318A1 (en) * 2003-10-31 2005-06-02 Hudyma Thomas W. Inhibitors of HCV replication
US7132504B2 (en) 2003-11-12 2006-11-07 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
US7309708B2 (en) 2003-11-20 2007-12-18 Birstol-Myers Squibb Company Hepatitis C virus inhibitors
WO2005051980A1 (en) 2003-11-20 2005-06-09 Schering Corporation Depeptidized inhibitors of hepatitis c virus ns3 protease
US7135462B2 (en) 2003-11-20 2006-11-14 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
EP1689857A1 (en) 2003-12-01 2006-08-16 Vertex Pharmaceuticals Incorporated Compositions comprising fetal liver cells and methods useful for hcv infection
EP1742913A1 (en) 2003-12-11 2007-01-17 Schering Corporation Inhibitors of hepatitis c virus ns3/ns4a serine protease
WO2005070955A1 (en) 2004-01-21 2005-08-04 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis c virus
HRP20100048T1 (hr) 2004-01-30 2010-04-30 Medivir Ab Inhibitori hcv ns-3 serin proteaze
EP1711515A2 (en) 2004-02-04 2006-10-18 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
US20050187192A1 (en) 2004-02-20 2005-08-25 Kucera Pharmaceutical Company Phospholipids for the treatment of infection by togaviruses, herpes viruses and coronaviruses
UY28758A1 (es) 2004-02-20 2005-09-30 Boehringer Ingelheim Int Inhibidores de polimerasa viral
CN1972956A (zh) 2004-02-27 2007-05-30 先灵公司 用作丙型肝炎病毒ns3丝氨酸蛋白酶抑制剂的新化合物
US7192957B2 (en) 2004-02-27 2007-03-20 Schering Corporation Compounds as inhibitors of hepatitis C virus NS3 serine protease
RU2428428C9 (ru) 2004-02-27 2012-03-10 Шеринг Корпорейшн Серусодержащие соединения, действующие как ингибиторы сериновой протеазы ns3 вируса гепатита с
CA2557304C (en) 2004-02-27 2013-08-06 Schering Corporation Ketoamides with cyclic p4's as inhibitors of ns3 serine protease of hepatitis c virus
KR20060124725A (ko) 2004-02-27 2006-12-05 쉐링 코포레이션 Ｃ형 간염 바이러스 ｎｓ3 프로테아제의 억제제
EP1737821B1 (en) 2004-02-27 2009-08-05 Schering Corporation 3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis c virus ns3 serine protease
SI2399915T1 (sl) * 2004-03-12 2015-05-29 Vertex Pharmaceuticals Incorporated Postopek in intermediati za pripravo inhibitorjev asparagin-acetal-kaspaze
CA2560897C (en) 2004-03-30 2012-06-12 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
US20050249702A1 (en) 2004-05-06 2005-11-10 Schering Corporation (1R,2S,5S)-N-[(1S)-3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide as inhibitor of hepatitis C virus NS3/NS4a serine protease
CN1984922A (zh) 2004-05-20 2007-06-20 先灵公司 用作丙型肝炎病毒ns3丝氨酸蛋白酶抑制剂的取代脯氨酸
AR049297A1 (es) * 2004-06-08 2006-07-12 Vertex Pharma Una composicion farmaceutica y dispersiones solidas de vx-950 (inhibidor de la proteasa de hcv ns3/4a) y proceso de obtencion
US7705146B2 (en) 2004-06-28 2010-04-27 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor peptide analogs
WO2006007708A1 (en) 2004-07-20 2006-01-26 Boehringer Engelheim International Gmbh Hepatitis c inhibitor peptide analogs
UY29016A1 (es) 2004-07-20 2006-02-24 Boehringer Ingelheim Int Analogos de dipeptidos inhibidores de la hepatitis c
US7423113B2 (en) * 2004-08-25 2008-09-09 Vib Vzw Leptin antagonist
MX2007002371A (es) 2004-08-27 2007-04-23 Schering Corp Compuestos de acilsulfonamida como inhibidores de la serina proteasa ns3 del virus de la hepatitis c.
AU2005291918A1 (en) 2004-10-01 2006-04-13 Vertex Pharmaceuticals Incorporated HCV NS3-NS4A protease inhibition
TW201424733A (zh) * 2004-10-29 2014-07-01 Vertex Pharma 劑量型式
US7863274B2 (en) 2005-07-29 2011-01-04 Concert Pharmaceuticals Inc. Deuterium enriched analogues of tadalafil as PDE5 inhibitors
CN101277950B (zh) * 2005-08-02 2013-03-27 弗特克斯药品有限公司 丝氨酸蛋白酶抑制剂
CA2619659A1 (en) * 2005-08-19 2007-02-22 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
US7705138B2 (en) 2005-11-11 2010-04-27 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
US8039475B2 (en) 2006-02-27 2011-10-18 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
KR20080112303A (ko) * 2006-03-16 2008-12-24 버텍스 파마슈티칼스 인코포레이티드 중수소화 ｃ형 간염 프로테아제 억제제
WO2007109023A1 (en) 2006-03-16 2007-09-27 Vertex Pharmaceuticals Incorporated Processes and intermediates for preparing steric compounds
US20070218012A1 (en) 2006-03-20 2007-09-20 Bittorf Kevin J Pharmaceutical Compositions
AU2007226983A1 (en) 2006-03-20 2007-09-27 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions
JP2009538912A (ja) * 2006-05-31 2009-11-12 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 インターロイキン−１β変換酵素阻害剤の経口制御放出剤形

Also Published As

Publication number Publication date
WO2007025307A3 (en) 2007-04-26
IL189668A0 (en) 2008-06-05
US8440706B2 (en) 2013-05-14
ES2374943T3 (es) 2012-02-23
AU2006282771A1 (en) 2007-03-01
EP2364984A1 (en) 2011-09-14
AU2006282771B2 (en) 2012-08-09
NZ566197A (en) 2011-07-29
AR055395A1 (es) 2007-08-22
ZA200801793B (en) 2008-12-31
EP2366704B1 (en) 2013-10-23
KR20080041715A (ko) 2008-05-13
US7985762B2 (en) 2011-07-26
NO20081467L (no) 2008-05-15
CN101316852A (zh) 2008-12-03
CA2620621A1 (en) 2007-03-01
TW200730533A (en) 2007-08-16
EP2366704A1 (en) 2011-09-21
WO2007025307A2 (en) 2007-03-01
JP2009506078A (ja) 2009-02-12
ECSP088258A (es) 2008-06-30
EP1917269B1 (en) 2011-10-26
US20070179167A1 (en) 2007-08-02
MX2008002606A (es) 2008-03-14
ATE530554T1 (de) 2011-11-15
GEP20115280B (en) 2011-09-12
EP1917269A2 (en) 2008-05-07
EA200800670A1 (ru) 2009-12-30
US20110165120A1 (en) 2011-07-07
BRPI0615223A2 (pt) 2009-07-14

Similar Documents

Publication Publication Date Title
JP5394063B2 (ja) セリンプロテアーゼの阻害剤
US7964624B1 (en) Inhibitors of serine proteases
US8575208B2 (en) Inhibitors of serine proteases
JP2007532474A (ja) セリンプロテアーゼ、特にｈｃｖのｎｓ３−ｎｓ４ａプロテアーゼの阻害剤
KR20080033481A (ko) 세린 프로테아제의 억제제
KR20060052836A (ko) 세린 프로테아제, 특히 ｈｃｖ ｎｓ3-ｎｓ4ａ 프로테아제의억제제
HK1156317A (en) Inhibitors of serine proteases for the treatment of hcv infections
HK1123557A (en) Inhibitors of serine proteases
HK1151284A (en) Inhibitors of serine proteases
HK1098164B (en) Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
HK1144824A (zh) 丝氨酸蛋白酶抑制剂、特别是hcv ns3-ns4a蛋白酶抑制剂

Legal Events

Date Code Title Description
A524 Written submission of copy of amendment under article 19 pct

Free format text: JAPANESE INTERMEDIATE CODE: A524

Effective date: 20090826

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20090826

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20120501

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20120529

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20120823

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20130122

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130328

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20130507

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130806

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: 20130917

A61 First payment of annual fees (during grant procedure)

Free format text: JAPANESE INTERMEDIATE CODE: A61

Effective date: 20131016

R150 Certificate of patent or registration of utility model

Free format text: JAPANESE INTERMEDIATE CODE: R150

LAPS Cancellation because of no payment of annual fees