[go: up one dir, main page]

AR030558A1 - COMPUESTOS MACROCICLICOS, QUE INCLUYEN ENANTIOMEROS, ESTEROISOMEROS, ROTAMEROS Y TAUTOMEROS, SALES Y SOLVATOS FARMACEUTICAMENTE ACEPTABLES, COMPOSICIoN FARMACEUTICA, UN METODO PARA SU PREPARACION Y EL USO DE DICHOS COMPUESTOS PARA LA ELABORACION DE UN MEDICAMENTO, INHIBIDORES DE LA SERINA PROTEASA, - Google Patents

COMPUESTOS MACROCICLICOS, QUE INCLUYEN ENANTIOMEROS, ESTEROISOMEROS, ROTAMEROS Y TAUTOMEROS, SALES Y SOLVATOS FARMACEUTICAMENTE ACEPTABLES, COMPOSICIoN FARMACEUTICA, UN METODO PARA SU PREPARACION Y EL USO DE DICHOS COMPUESTOS PARA LA ELABORACION DE UN MEDICAMENTO, INHIBIDORES DE LA SERINA PROTEASA,

Info

Publication number
AR030558A1
AR030558A1 ARP010101794A ARP010101794A AR030558A1 AR 030558 A1 AR030558 A1 AR 030558A1 AR P010101794 A ARP010101794 A AR P010101794A AR P010101794 A ARP010101794 A AR P010101794A AR 030558 A1 AR030558 A1 AR 030558A1
Authority
AR
Argentina
Prior art keywords
conhch
alkyl
cycloalkyl
aryl
carbamate
Prior art date
Application number
ARP010101794A
Other languages
English (en)
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
Publication of AR030558A1 publication Critical patent/AR030558A1/es

Links

Classifications

    • 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
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0202—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-X-X-C(=0)-, X being an optionally substituted carbon atom or a heteroatom, e.g. beta-amino acids
    • 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
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • 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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biophysics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Un compuesto macrocíclico, incluyendo los enantiomeros, estereoisomeros rotámeros y tautomeros de dicho compuesto , así como las sales o solvatos farmacéuticamente aceptables de dicho compuesto, que tiene la estructura general expuesta en la formula (1) en la cual E, X e Y pueden estar independientemente presentes o ausentes y, en caso de estar presentes, son independientemente seleccionados entre las porciones: alquilo, arilo, alquilarilo, heteroarilo, arilheteroarilo, alquilheteroarilo, cicloalquilo, éter alquílico, éter alquilarílico, éter arílico, alquilamino, arilamino, alquilarilamino, alquilsulfuro, alquilarilsulfuro, arilsulfuro, alquilsulfona, alquilarilsulfona, arilsulfona, alquilalquilsulfoxido, alquilarilsulfoxido, alquilamida, arilamida, alquilsufonamida, alquilarilsulfonamida, arilsulfonamida, alquilurea, alquilarilurea, arilurea, carbamato de alquilo, carbamato de alquilarilo, carbamato de arilo, alquilhidrazida, alquilarilhidrazida, alquilhidroxamida, alquilarilhidroxamida, alquilsufonilo, arilsulfonilo, heteroalquilsulfonilo, hetroarilsulfonilo, alquilcarbonilo, arilcarbonilo, heteroarilalquilcarbonilo, heteroarilcarbonilo, alcoxicarbonilo, ariloxicarbonilo, hetoroariloxicarbonilo, alquilaminocarbonilo, arilaminocarbonilo, heteroarilaminocarbonilo, o una combinacion de las mismas; con la condicion de que optativamente E, X, e Y pueden estar sustituidas además con porciones seleccionadas entre el grupo que consiste en aromáticos, alquilo, alquilarilo, heteroalquilo, arilheteroarilo, alquilheteroarilo, cicloalquilo, éter alquílico, éter alquilarílico, alquilsulfuro, alquilarilsulfuro, alquilsulfona, alquilarilsulfona, alquilamida, alquilarilamida, alquilsulfonamida, alquilaminas, alquilarilsulfonamida, alquilurea, alquilarilurea, carbamato de alquilo, carbamato de alquilarilo, halogeno, hidroxilamino, carbazato de alquilo, carbazato de arilo; R1=COR5 o B(OR)2, donde R5=H, OH, OR8NR9R10, CF3, C2F5, C3F7, CF2R6, R6, COR7 donde R7 = H, OH, OR8, CHR9R10, donde R6, R8, R9 y R10 son independientemente seleccionados entre el grupo que consiste en H, alquilo, arilo, heteroalquilo, heteroarilo, cicloalquilo, cicloalquilo, arilalquilo, heteroarilalquilo, CH(R1')COOR11, CH(R1')CONR12R13, CH(R1')CONHCH(R2')COOR11, CH(R1')CONHCH(R2')CONR12R13, CH(R1')CONHCH(R2')CONHCH(R3')COOR11, CH(R1')CONHCH(R2')CONHCH(R3')CONR12R13, CH(R1')CONHCH(R2')CONHCH(R3')CONHCH(R4')COOR11, CH(R1')CONHCH(R2')CONHCH(R3')CONHCH(R4')CONR12R13, CH(R1')CONHCH(R2')CONHCH(R3')CONHCH(R4')CONHCH(R5')COOR11, CH(R1')CONHCH(R2')CONHCH(R3')CONHCHR4')CONHCH(R5')CONR12R13 donde R1', R2', R3', R4,', R5', R11, R12, R13 son independientemente seleccionados entre el grupo que consiste en H, alquilo, arilo, heteroalquilo, heteroarilo, cicloalquilo, alquilarilo, alquilheteroarilo, arilalquilo, y heteroaralquilo; Z es seleccionado entre O, N o CH; W puede estar presente o ausente y, en caso de estar presente W es seleccionado entre C=O, C=S, SO2 o C=NR; Q es (NR)p, O, S, CH2, CHR, CRR' o un enlace doble hacia V; A es O, CH2, (CHR)p, (CHR-CHR')p, (CRR')p, NR, S, SO2, C=O o un enlace; G es (CH2)p, (CHR)p, (CRR')p, NR, O, S, SO2, S(O)2NH, C=O o un enlace doble hacia E o V; V es CH, CR o N; p es un numero de 0 a 6 y R, R', R2, R3, y R4 son independientemente seleccionados entre el grupo que consiste en H, alquilo, C1-10, alquenilo C2-10, cicloalquilo C3-8, heterocicloalquilo C3-8, arilo, alcoxi, ariloxi, alquiltio, ariltio, amino, amido, éster, ácido carboxílico, carbamato, urea, cetona, aldehído, ciano, nitro, heteroarilo, alquilarilo, alquilheteroarilo, (cicloalquil)alquilo y (heterocicloalquil)alquilo, donde dicho cicloalquilo se compone de tres a ocho átomos de carbono y de cero a seis átomos de oxígeno, nitrogeno, azufre o fosforo y dicho alquilo es de uno a seis átomos de carbono; donde dichas porciones alquilo, heteroarilo, alquenilo, heteroalquenilo, arilo, heteroarilo cicloalquilo y heterocicloalquilo pueden estar optativamente sustituidas, y donde dicho término "sustituido" se refiere a una sustitucion optativa y adecuada con una o más opciones seleccionadas entre el grupo que consiste en alquilo, alquenilo, alquinilo, arilo, aralquilo, cicloalquilo, heterocíclico, halogeno, hidroxi, tio, alcoxi, ariloxi, alquiltio, ariltio, amino, amido, éster, ácido carboxílico, carbamato, urea, cetona, aldehído, ciano, nitro, sulfonamida, sulfoxido, sulfona, sulfonilurea, hidrazida e hidraxamato y tiourea; así como métodos para la preparacion de dichos compuestos. En otra realizacion, también se describen composiciones farmacéuticas que comprenden dichos macrocíclicos así como su uso para la cloracion de un medicamento en el tratamiento de trastornos asociados con la proteasa de VHC, inhibidores de la reina proteasa NS-3 del virus de la hepatitis C.
ARP010101794A 2000-04-19 2001-04-17 COMPUESTOS MACROCICLICOS, QUE INCLUYEN ENANTIOMEROS, ESTEROISOMEROS, ROTAMEROS Y TAUTOMEROS, SALES Y SOLVATOS FARMACEUTICAMENTE ACEPTABLES, COMPOSICIoN FARMACEUTICA, UN METODO PARA SU PREPARACION Y EL USO DE DICHOS COMPUESTOS PARA LA ELABORACION DE UN MEDICAMENTO, INHIBIDORES DE LA SERINA PROTEASA, AR030558A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US19820400P 2000-04-19 2000-04-19

Publications (1)

Publication Number Publication Date
AR030558A1 true AR030558A1 (es) 2003-08-27

Family

ID=22732422

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP010101794A AR030558A1 (es) 2000-04-19 2001-04-17 COMPUESTOS MACROCICLICOS, QUE INCLUYEN ENANTIOMEROS, ESTEROISOMEROS, ROTAMEROS Y TAUTOMEROS, SALES Y SOLVATOS FARMACEUTICAMENTE ACEPTABLES, COMPOSICIoN FARMACEUTICA, UN METODO PARA SU PREPARACION Y EL USO DE DICHOS COMPUESTOS PARA LA ELABORACION DE UN MEDICAMENTO, INHIBIDORES DE LA SERINA PROTEASA,

Country Status (22)

Country Link
US (1) US6914122B2 (es)
EP (1) EP1274724A2 (es)
JP (1) JP4748912B2 (es)
KR (1) KR20020097220A (es)
CN (3) CN1935833A (es)
AR (1) AR030558A1 (es)
AU (1) AU2001253621A1 (es)
BR (1) BR0110104A (es)
CA (1) CA2406532A1 (es)
CZ (1) CZ20023473A3 (es)
HK (1) HK1048479A1 (es)
HU (1) HUP0302957A2 (es)
IL (1) IL151935A0 (es)
MX (1) MXPA02010375A (es)
NO (1) NO20025030L (es)
NZ (1) NZ521456A (es)
PE (1) PE20011288A1 (es)
PL (1) PL358591A1 (es)
RU (1) RU2002131163A (es)
SK (1) SK14952002A3 (es)
WO (1) WO2001081325A2 (es)
ZA (1) ZA200208014B (es)

Families Citing this family (131)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA79749C2 (en) * 1996-10-18 2007-07-25 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
US6608027B1 (en) 1999-04-06 2003-08-19 Boehringer Ingelheim (Canada) Ltd Macrocyclic peptides active against the hepatitis C virus
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
HUP0303436A2 (hu) * 2000-12-12 2004-01-28 Schering Corp. Diaril-peptidek mint a hepatitis C vírus NS3-szerin proteáz inhibitorai, ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
GEP20053601B (en) 2001-01-22 2005-08-10 Merck & Co Inc Nucleoside Derivatives as Inhibitors of RNA-Dependent RNA Viral Polymerase
US7119072B2 (en) 2002-01-30 2006-10-10 Boehringer Ingelheim (Canada) Ltd. Macrocyclic peptides active against the hepatitis C virus
US6642204B2 (en) 2002-02-01 2003-11-04 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
US7091184B2 (en) 2002-02-01 2006-08-15 Boehringer Ingelheim International Gmbh Hepatitis C inhibitor tri-peptides
KR20040099425A (ko) * 2002-04-11 2004-11-26 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 ｃ형 간염 바이러스 ｎｓ3-ｎｓ4프로테아제의 억제제
US20050075279A1 (en) 2002-10-25 2005-04-07 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis C virus
MY143076A (en) 2003-05-21 2011-02-28 Boehringer Ingelheim Int Hepatitis c inhibitors compounds
US20090198050A1 (en) * 2003-06-18 2009-08-06 Tranzyme Pharma Inc. Macrocyclic Modulators of the Ghrelin Receptor
JP4928261B2 (ja) 2003-06-18 2012-05-09 トランザイム・ファーマ・インコーポレイテッド モチリン受容体の大環状拮抗薬
US7476653B2 (en) * 2003-06-18 2009-01-13 Tranzyme Pharma, Inc. Macrocyclic modulators of the ghrelin receptor
US8921521B2 (en) 2003-06-18 2014-12-30 Ocera Therapeutics, Inc. Macrocyclic modulators of the Ghrelin receptor
MXPA06002250A (es) 2003-08-26 2006-05-17 Schering Corp Inhibidores peptidomimeticos novedosos de la serina proteasa ns3 del virus de la hepatitis c.
AR045596A1 (es) * 2003-09-05 2005-11-02 Vertex Pharma Inhibidores de proteasas de serina en particular proteasa ns3-ns4a del vhc
MXPA06003141A (es) 2003-09-22 2006-06-05 Boehringer Ingelheim Int Peptidos macrociclicos activos contra el virus de la hepatitis c.
RU2006113880A (ru) * 2003-09-26 2007-11-20 Шеринг Корпорейшн (US) Макроциклические ингибиторы сериновой протеиназы ns3 вируса гепатита с
KR20120010278A (ko) 2003-10-10 2012-02-02 버텍스 파마슈티칼스 인코포레이티드 세린 프로테아제, 특히 ｈｃｖ ｎｓ3-ｎｓ4ａ 프로테아제의 억제제
US7491794B2 (en) * 2003-10-14 2009-02-17 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
EP1944042A1 (en) 2003-10-27 2008-07-16 Vertex Pharmceuticals Incorporated Combinations for HCV treatment
US8187874B2 (en) 2003-10-27 2012-05-29 Vertex Pharmaceuticals Incorporated Drug discovery method
EP1689770A1 (en) 2003-11-20 2006-08-16 Schering Corporation Depeptidized inhibitors of hepatitis c virus ns3 protease
ES2358333T3 (es) 2004-01-21 2011-05-09 Boehringer Ingelheim International Gmbh Péptidos macrocíclicos con acción contra el virus de la hepatitis c.
EP1711515A2 (en) 2004-02-04 2006-10-18 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
DK1730110T3 (da) 2004-02-27 2010-09-27 Schering Corp Svovlforbindelser som inhibitorer af hepatitis C-virus NS3-serinprotease
AR048413A1 (es) 2004-02-27 2006-04-26 Schering Corp Compuestos prolina 3,4- (ciclopentil) - fusionados , como inhibidores de serina proteasa ns3 del virus de la hepatitis c
US7816326B2 (en) 2004-02-27 2010-10-19 Schering Corporation Sulfur compounds as inhibitors of hepatitis C virus NS3 serine protease
CA2557247A1 (en) 2004-02-27 2005-09-22 Schering Corporation Compounds as inhibitors of hepatitis c virus ns3 serine protease
EP1737881B1 (en) 2004-02-27 2009-06-24 Schering Corporation Novel compounds as inhibitors of hepatitis c virus ns3 serine protease
TW200536528A (en) 2004-02-27 2005-11-16 Schering Corp Novel inhibitors of hepatitis C virus NS3 protease
JP2008502718A (ja) 2004-05-20 2008-01-31 シェーリング　コーポレイション Ｃ型肝炎ウイルスｎｓ３セリンプロテアーゼのインヒビターとしての置換型プロリン
UY29016A1 (es) 2004-07-20 2006-02-24 Boehringer Ingelheim Int Analogos de dipeptidos inhibidores de la hepatitis c
WO2006007708A1 (en) 2004-07-20 2006-01-26 Boehringer Engelheim International Gmbh Hepatitis c inhibitor peptide analogs
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.
WO2007001406A2 (en) * 2004-10-05 2007-01-04 Chiron Corporation Aryl-containing macrocyclic compounds
PE20070011A1 (es) * 2005-06-02 2007-03-08 Schering Corp Formulaciones farmaceuticas de compuestos inhibidores de proteasa del vhc o catepsina
US8119602B2 (en) 2005-06-02 2012-02-21 Schering Corporation Administration of HCV protease inhibitors in combination with food to improve bioavailability
US20070237818A1 (en) * 2005-06-02 2007-10-11 Malcolm Bruce A Controlled-release formulation of HCV protease inhibitor and methods using the same
US20110104109A1 (en) * 2005-07-13 2011-05-05 Frank Bennett Tetracyclic indole derivatives and their use for treating or preventing viral infections
US20090148407A1 (en) * 2005-07-25 2009-06-11 Intermune, Inc. Novel Macrocyclic Inhibitors of Hepatitis C Virus Replication
DK1913015T3 (en) * 2005-07-29 2014-03-10 Janssen R & D Ireland Macrocyclic inhibitors of hepatitis C virus
MX2008001528A (es) 2005-08-02 2008-04-04 Vertex Pharma Inhibidores de serina proteasas.
US8399615B2 (en) 2005-08-19 2013-03-19 Vertex Pharmaceuticals Incorporated Processes and intermediates
KR20130110236A (ko) 2005-08-19 2013-10-08 버텍스 파마슈티칼스 인코포레이티드 방법 및 중간체
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
CN101415705B (zh) 2005-10-11 2011-10-26 因特蒙公司 抑制丙型肝炎病毒复制的化合物和方法
KR20140098867A (ko) 2005-11-11 2014-08-08 버텍스 파마슈티칼스 인코포레이티드 Ｃ형 간염 바이러스 변이체
US7705138B2 (en) 2005-11-11 2010-04-27 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
US7816348B2 (en) 2006-02-03 2010-10-19 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
WO2007098270A2 (en) 2006-02-27 2007-08-30 Vertex Pharmaceuticals Incorporated Co-crystals comprising vx-950 and pharmaceutical compositions comprising the same
EP2194039A1 (en) 2006-03-16 2010-06-09 Vertex Pharmceuticals Incorporated Process for preparing optically enriched compounds
JP2009530382A (ja) * 2006-03-23 2009-08-27 シェーリング コーポレイション Ｈｃｖプロテアーゼインヒビターとｃｙｐ３ａ４インヒビターとの組み合わせ、および関連する処置方法
RU2008152171A (ru) * 2006-07-05 2010-08-10 Интермьюн, Инк. (Us) Новые ингибиторы вирусной репликации гепатита с
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
JP2010500978A (ja) 2006-08-17 2010-01-14 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 ウイルスポリメラーゼインヒビター
WO2008048121A2 (en) 2006-10-18 2008-04-24 Lincoln University Macrocyclic cysteine protease inhibitors and compositions thereof
CN101631773A (zh) 2006-12-22 2010-01-20 先灵公司 治疗或预防hcv和相关病毒感染的4,5-环化吲哚衍生物
ATE543808T1 (de) 2006-12-22 2012-02-15 Schering Corp 5,6-ring-annelierte indolderivate und ihre verwendung
US8546420B2 (en) * 2006-12-22 2013-10-01 Merck Sharp & Dohme Corp. 4, 5-ring annulated indole derivatives for treating or preventing of HCV and related viral infections
KR20090115970A (ko) 2007-02-27 2009-11-10 버텍스 파마슈티칼스 인코포레이티드 공-결정 및 그를 포함하는 제약 조성물
WO2008106058A2 (en) 2007-02-27 2008-09-04 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
CA2686138A1 (en) * 2007-05-03 2008-11-13 Intermune, Inc. Novel macrocyclic inhibitors of hepatitis c virus replication
CA2686051A1 (en) 2007-05-04 2008-11-13 Vertex Pharmaceuticals Incorporated Combination therapy for the treatment of hcv infection
CL2008001381A1 (es) * 2007-05-10 2008-11-03 Intermune Inc Y Array Biopharma Inc Compuestos derivados de tripeptidos que contienen heterociclos nitrogenados; composicion farmaceutica que comprende a dichos compuestos; y uso para tratar una infeccion de hepatitis c o vih.
CA2693997C (en) 2007-08-03 2013-01-15 Pierre L. Beaulieu Viral polymerase inhibitors
BRPI0816116A2 (pt) * 2007-08-29 2015-03-03 Schering Corp Derivados de indol 2,3-substituídos para o tratamento de infecções virais.
ATE541845T1 (de) 2007-08-29 2012-02-15 Schering Corp 2,3-substituierte azaindolderivate zur behandlung von virusinfektionen
AR068106A1 (es) 2007-08-29 2009-11-04 Schering Corp Derivados de indol 2-carboxi sustituidos y una composicion farmaceutica
TW200922933A (en) 2007-08-30 2009-06-01 Vertex Pharma Co-crystals and pharmaceutical compositions comprising the same
GB0718575D0 (en) 2007-09-24 2007-10-31 Angeletti P Ist Richerche Bio Nucleoside derivatives as inhibitors of viral polymerases
US8419332B2 (en) * 2007-10-19 2013-04-16 Atlas Bolt & Screw Company Llc Non-dimpling fastener
US8383583B2 (en) 2007-10-26 2013-02-26 Enanta Pharmaceuticals, Inc. Macrocyclic, pyridazinone-containing hepatitis C serine protease inhibitors
CN102099351A (zh) * 2007-11-16 2011-06-15 先灵公司 3-杂环取代的吲哚衍生物及其使用方法
JP5416708B2 (ja) * 2007-11-16 2014-02-12 メルク・シャープ・アンド・ドーム・コーポレーション ３−アミノスルホニル置換インドール誘導体およびそれらの使用方法
MX2010006313A (es) 2007-12-19 2010-06-25 Boehringer Ingelheim Int Inhibidores de la polimerasa virica.
US8309685B2 (en) 2007-12-21 2012-11-13 Celgene Avilomics Research, Inc. HCV protease inhibitors and uses thereof
US8778877B2 (en) * 2007-12-21 2014-07-15 Celgene Avilomics Research, Inc. HCV protease inhibitors and uses thereof
US9163061B2 (en) * 2007-12-21 2015-10-20 Celgene Avilomics Research, Inc. HCV protease inhibitors and uses thereof
US8293705B2 (en) 2007-12-21 2012-10-23 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
KR20100118991A (ko) 2008-02-04 2010-11-08 아이데닉스 파마슈티칼스, 인코포레이티드 매크로시클릭 세린 프로테아제 억제제
CA2705300A1 (fr) * 2008-02-15 2009-06-04 Xeda International Macrocyclic inhibitors of hepatitis c protease
WO2009117594A1 (en) 2008-03-20 2009-09-24 Enanta Pharmaceuticals, Inc. Fluorinated macrocyclic compounds as hepatitis c virus inhibitors
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
CN102159579B (zh) * 2008-06-13 2015-03-25 默沙东公司 三环吲哚衍生物及其使用方法
CA2734489C (en) 2008-08-20 2016-11-08 Southern Research Institute Ethenyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections
US8470834B2 (en) 2008-08-20 2013-06-25 Merck Sharp & Dohme Corp. AZO-substituted pyridine and pyrimidine derivatives and their use in treating viral infections
US8697694B2 (en) 2008-08-20 2014-04-15 Merck Sharp & Dohme Corp. Substituted pyridine and pyrimidine derivatives and their use in treating viral infections
TW201020245A (en) 2008-08-20 2010-06-01 Schering Corp Ethynyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections
MX2011007195A (es) 2009-01-07 2013-07-12 Scynexis Inc Derivado de ciclosporina para el uso en el tratamiento de infección de virus de hepatitis c (vhc) y virus de inmunodeficiencia humana (vih).
US8102720B2 (en) * 2009-02-02 2012-01-24 Qualcomm Incorporated System and method of pulse generation
AR075584A1 (es) * 2009-02-27 2011-04-20 Intermune Inc COMPOSICIONES TERAPEUTICAS QUE COMPRENDEN beta-D-2'-DESOXI-2'-FLUORO-2'-C-METILCITIDINA Y UN DERIVADO DE ACIDO ISOINDOL CARBOXILICO Y SUS USOS. COMPUESTO.
JP5690286B2 (ja) 2009-03-04 2015-03-25 イデニク プハルマセウティカルス，インコーポレイテッド ホスホチオフェン及びホスホチアゾールｈｃｖポリメラーゼ阻害剤
JP2012523419A (ja) 2009-04-08 2012-10-04 イデニク プハルマセウティカルス，インコーポレイテッド 大環状セリンプロテアーゼ阻害剤
EP2435424B1 (en) 2009-05-29 2015-01-21 Merck Sharp & Dohme Corp. Antiviral compounds composed of three linked aryl moieties to treat diseases such as hepatitis c
EP2461811B1 (en) 2009-08-05 2016-04-20 Idenix Pharmaceuticals LLC. Macrocyclic serine protease inhibitors useful against viral infections, particularly hcv
JP5789260B2 (ja) 2009-08-27 2015-10-07 メルク・シャープ・エンド・ドーム・コーポレイション Ｃ型肝炎ウイルスのプロテアーゼ阻害薬の調製方法
PH12012500602A1 (en) * 2009-09-28 2017-08-23 Intermune Inc Cyclic peptide inhibitors of hepatitis c virus replication
WO2011063076A1 (en) 2009-11-19 2011-05-26 Itherx Pharmaceuticals, Inc. Methods of treating hepatitis c virus with oxoacetamide compounds
CA2782024A1 (en) 2009-11-25 2011-06-03 Schering Corporation Fused tricyclic compounds and derivatives thereof useful for the treatment of viral diseases
AU2010330862B2 (en) 2009-12-18 2015-06-25 Idenix Pharmaceuticals, Inc. 5,5-fused arylene or heteroarylene hepatitis C virus inhibitors
AU2010341537A1 (en) 2009-12-22 2012-08-09 Merck Sharp & Dohme Corp. Fused Tricyclic Compounds and methods of use thereof for the treatment of viral diseases
EP2536410B1 (en) 2010-02-18 2015-09-23 Merck Sharp & Dohme Corp. Substituted pyrimidine derivatives and their use in treating viral infections
JP2013522202A (ja) 2010-03-09 2013-06-13 メルク・シャープ・エンド・ドーム・コーポレイション 縮合三環式シリル化合物およびウイルス疾患の治療のためのその使用方法
CN103025736B (zh) * 2010-06-07 2016-07-06 Abbvie公司 大环的丙型肝炎丝氨酸蛋白酶抑制剂
US20140377223A1 (en) 2010-07-26 2014-12-25 Joseph A. Kozlowski Substituted biphenylene compounds and methods of use thereof for the treatment of viral diseases
WO2012050848A1 (en) 2010-09-29 2012-04-19 Schering Corporation Fused tetracycle derivatives and methods of use thereof for the treatment of viral diseases
AR085352A1 (es) 2011-02-10 2013-09-25 Idenix Pharmaceuticals Inc Inhibidores macrociclicos de serina proteasa, sus composiciones farmaceuticas y su uso para tratar infecciones por hcv
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
EP2489669A1 (en) * 2011-02-18 2012-08-22 Helmholtz-Zentrum für Infektionsforschung GmbH Haprolid and derivatives thereof as inhibitors of HCV
US20120252721A1 (en) 2011-03-31 2012-10-04 Idenix Pharmaceuticals, Inc. Methods for treating drug-resistant hepatitis c virus infection with a 5,5-fused arylene or heteroarylene hepatitis c virus inhibitor
EP2697242B1 (en) 2011-04-13 2018-10-03 Merck Sharp & Dohme Corp. 2'-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
KR20130138840A (ko) 2011-04-13 2013-12-19 머크 샤프 앤드 돔 코포레이션 2''-치환된 뉴클레오시드 유도체 및 바이러스성 질환의 치료를 위한 그의 사용 방법
WO2013033900A1 (en) 2011-09-08 2013-03-14 Merck Sharp & Dohme Corp. Tetracyclic heterocycle compounds and methods of use thereof for the treatment of viral diseases
WO2013033901A1 (en) 2011-09-08 2013-03-14 Merck Sharp & Dohme Corp. Heterocyclic-substituted benzofuran derivatives and methods of use thereof for the treatment of viral diseases
WO2013033899A1 (en) 2011-09-08 2013-03-14 Merck Sharp & Dohme Corp. Substituted benzofuran compounds and methods of use thereof for the treatment of viral diseases
EP2755981A4 (en) 2011-09-14 2015-03-25 Merck Sharp & Dohme SILICULAR HETEROCYCLIC DERIVATIVES AND METHOD FOR THEIR USE FOR THE TREATMENT OF VIRUS DISEASES
TWI787670B (zh) 2011-12-28 2022-12-21 日商中外製藥股份有限公司 具有環狀部之胜肽化合物及其醫藥組成物
SI2943493T1 (sl) * 2013-01-09 2017-11-30 Gilead Sciences, Inc. Terapevtske spojine za zdravljenje virusnih infekcij
EP3046924A1 (en) 2013-09-20 2016-07-27 IDENIX Pharmaceuticals, Inc. Hepatitis c virus inhibitors
US10167298B2 (en) 2013-10-30 2019-01-01 Merck Sharp & Dohme Corp. Pseudopolymorphs of an HCV NS5A inhibitor and uses thereof
US20170066779A1 (en) 2014-03-05 2017-03-09 Idenix Pharmaceuticals Llc Solid forms of a flaviviridae virus inhibitor compound and salts thereof
WO2015134561A1 (en) 2014-03-05 2015-09-11 Idenix Pharmaceuticals, Inc. Pharmaceutical compositions comprising a 5,5-fused heteroarylene flaviviridae inhibitor and their use for treating or preventing flaviviridae infection
JP7020910B2 (ja) 2015-03-13 2022-02-16 中外製薬株式会社 改変アミノアシルｔＲＮＡ合成酵素およびその用途
JP7229158B2 (ja) 2017-06-09 2023-02-27 中外製薬株式会社 Ｎ－置換アミノ酸を含むペプチドの合成方法
EP3694508A4 (en) * 2017-10-11 2021-11-24 Cornell University MACROCYCLIC COMPOUNDS USED AS PROTEASOME INHIBITORS
JP7411414B2 (ja) 2017-12-15 2024-01-11 中外製薬株式会社 ペプチドの製造方法、及び塩基の処理方法
KR20210098476A (ko) 2018-11-30 2021-08-10 추가이 세이야쿠 가부시키가이샤 펩티드 화합물 또는 아마이드 화합물의 탈보호법 및 고상 반응에 있어서의 탈수지 방법, 및 펩티드 화합물의 제조 방법
CN113692401A (zh) 2019-03-15 2021-11-23 中外制药株式会社 芳香族氨基酸衍生物的制备方法

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5377083A (en) * 1976-12-16 1978-07-08 Asahi Chem Ind Co Ltd Penicillins and their derivatives
US4260601A (en) * 1979-10-23 1981-04-07 Nyegaard & Co. A/S Chemical compounds
ZA838780B (en) * 1982-11-26 1985-01-30 Nyegaard & Co As Peptide compounds
US4956344A (en) * 1987-09-17 1990-09-11 Hafslund Nycomed A/S Method for treatment of lesions in the large intestinal epithelium with a tripeptide
HU220204B (hu) 1987-11-18 2001-11-28 Chiron Corp. HCV polipeptidek és HCV polinukleotidok, ilyen polinukleotidokat tartalmazó vektorok és ezekkel transzformált gazdasejtek, valamint HCV fertőzés kimutatására szolgáló diagnosztikumok és immunvizsgálati készlet
DE69024378T2 (de) 1989-02-01 1996-09-12 Asahi Glass Co. Ltd., Tokio/Tokyo Azeotrope oder azeotropähnliche Zusammensetzung auf der Basis von Chlorfluorkohlenwasserstoffen
ATE270326T1 (de) 1990-04-04 2004-07-15 Chiron Corp Protease von hepatitis-c-virus
JPH07228594A (ja) * 1994-02-18 1995-08-29 Suntory Ltd エンドセリン受容体拮抗ペプチド
IL109943A (en) * 1994-06-08 2006-08-01 Develogen Israel Ltd Conformationally constrained backbone cyclized peptide analogs
AU4156197A (en) 1996-08-21 1998-03-06 Hybridon, Inc. Oligonucleotide prodrugs
UA79749C2 (en) 1996-10-18 2007-07-25 Vertex Pharma Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
GB9623908D0 (en) 1996-11-18 1997-01-08 Hoffmann La Roche Amino acid derivatives
ES2234144T3 (es) * 1997-08-11 2005-06-16 Boehringer Ingelheim (Canada) Ltd. Analogos de peptidos inhibidores de la hepatitis c.
KR20010085236A (ko) * 1998-04-15 2001-09-07 오흘러 로스 제이. 수지-결합된 사이클릭 펩타이드의 제조방법
GB9812523D0 (en) * 1998-06-10 1998-08-05 Angeletti P Ist Richerche Bio Peptide inhibitors of hepatitis c virus ns3 protease
AR022061A1 (es) * 1998-08-10 2002-09-04 Boehringer Ingelheim Ca Ltd Peptidos inhibidores de la hepatitis c, una composicion farmaceutica que los contiene, el uso de los mismos para preparar una composicion farmaceutica, el uso de un producto intermedio para la preparacion de estos peptidos y un procedimiento para la preparacion de un peptido analogo de los mismos.
US6323180B1 (en) 1998-08-10 2001-11-27 Boehringer Ingelheim (Canada) Ltd Hepatitis C inhibitor tri-peptides
US6407066B1 (en) * 1999-01-26 2002-06-18 Elan Pharmaceuticals, Inc. Pyroglutamic acid derivatives and related compounds which inhibit leukocyte adhesion mediated by VLA-4

Also Published As

Publication number Publication date
JP4748912B2 (ja) 2011-08-17
US20020016294A1 (en) 2002-02-07
BR0110104A (pt) 2003-01-07
EP1274724A2 (en) 2003-01-15
CN101580536A (zh) 2009-11-18
AU2001253621A1 (en) 2001-11-07
ZA200208014B (en) 2004-02-12
IL151935A0 (en) 2003-04-10
US6914122B2 (en) 2005-07-05
SK14952002A3 (sk) 2003-03-04
CA2406532A1 (en) 2001-11-01
PE20011288A1 (es) 2001-12-12
NZ521456A (en) 2004-07-30
JP2003531199A (ja) 2003-10-21
KR20020097220A (ko) 2002-12-31
RU2002131163A (ru) 2004-06-27
PL358591A1 (en) 2004-08-09
HK1048479A1 (zh) 2003-04-04
MXPA02010375A (es) 2003-04-25
NO20025030L (no) 2002-12-18
CN1432022A (zh) 2003-07-23
HUP0302957A2 (hu) 2003-12-29
WO2001081325A2 (en) 2001-11-01
WO2001081325A3 (en) 2002-08-01
CZ20023473A3 (cs) 2003-01-15
CN1935833A (zh) 2007-03-28
NO20025030D0 (no) 2002-10-18

Similar Documents

Publication Publication Date Title
AR030558A1 (es) COMPUESTOS MACROCICLICOS, QUE INCLUYEN ENANTIOMEROS, ESTEROISOMEROS, ROTAMEROS Y TAUTOMEROS, SALES Y SOLVATOS FARMACEUTICAMENTE ACEPTABLES, COMPOSICIoN FARMACEUTICA, UN METODO PARA SU PREPARACION Y EL USO DE DICHOS COMPUESTOS PARA LA ELABORACION DE UN MEDICAMENTO, INHIBIDORES DE LA SERINA PROTEASA,
AR029903A1 (es) Inhibidores macrociclicos de la ns3-serina proteasa, del virus de la hepatitis c, que comprenden partes p2 n-ciclicas, composiciones farmaceuticas y utilizacion de los mismos para la manufactura de un medicamento
AR030249A1 (es) Peptidos como inhibidores de ns3-serina proteasa del virus de la hepatitis c, composicion farmaceutica que lo comprende, un metodo para su preparacion y el uso de los mismos para la manufactura de medicamentos y un metodo para modular el procesamiento de un polipeptido del virus
AR033379A1 (es) Compuestos de difenilurea, procedimiento para su preparacion y composiciones farmaceuticas que los contienen
JP2003531199A5 (es)
ECSP045064A (es) Agonistas receptores de trombina
AR043938A1 (es) Compuesto heterociclico derivado de quinolina o naftiridina, composicion farmaceutica que lo comprende y su uso para preparar esta ultima
AR036598A1 (es) Derivados de 4,5-dihidro-1h-pirazol que tienen potente actividad antagonista de cb1
AR046758A1 (es) Inhibidores de la ns3/ns4a serina proteasa del virus de la hepatitis c
RU2004110719A (ru) Зздабиторы протеаз, расщепляющих за пролином
AR038183A1 (es) Peptidos como inhibidores de la proteasa serina ns3 del virus de la hepatitis c
TW200745029A (en) Sulfonamide derivatives exhibiting PGD2 receptor antagonism
AR043674A1 (es) Derivados de piridazinona como inhibidores no nucleosidos de la transcriptasa reversa
AR036492A1 (es) Inhibidores de la 17beta-hidroxiesteroide deshidrogenasa tipo 3, composiciones farmaceuticas y el uso de dichos inhibidores para la elaboracion de un medicamento para el tratamiento de enfermedades androgeno dependientes
NO20073357L (no) 5-karboksamid substituerte tiazol derivater som reagerer med ionekanaler, i saerdeleshet med ionekanaler fra Kv familien
JP2003530401A5 (es)
EA200600892A1 (ru) Новые хинолиновые производные
DK0622361T3 (da) Heterocykliske forbindelser som bradykininantagonister
RU2006113880A (ru) Макроциклические ингибиторы сериновой протеиназы ns3 вируса гепатита с
AR038214A1 (es) Compuestos de prolina como inhibidores de la serina proteasa ns3 del virus de la hepatitis c
MXPA03011638A (es) Nuevos derivados de 4-piperazinil indol con afinidad por el receptor 5-ht6.
AR058587A1 (es) Compuestos de pirrolo-1,5-naftiridinona,su uso como agentes antibacterianos, composiciones farmaceuticas que los contienen y compuestos intermediarios para preparar dichos compuestos
AR037465A1 (es) Compuesto derivado de 5-sulfanil-4h-1,2,4-triazol, composicion farmaceutica que lo comprende y proceso para su preparacion en fase liquida
AR045155A1 (es) Derivados de 6-indolilsulfonamidas, su preparacion y su aplicacion como medicamentos
DE60024471D1 (de) Benzopyran derivate

Legal Events

Date Code Title Description
FB Suspension of granting procedure