AR029903A1 - 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 - Google Patents

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

Info

Publication number
AR029903A1
AR029903A1 ARP010101579A ARP010101579A AR029903A1 AR 029903 A1 AR029903 A1 AR 029903A1 AR P010101579 A ARP010101579 A AR P010101579A AR P010101579 A ARP010101579 A AR P010101579A AR 029903 A1 AR029903 A1 AR 029903A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
conhch
present
heteroaryl
Prior art date
Application number
ARP010101579A
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 AR029903A1 publication Critical patent/AR029903A1/es

Links

Classifications

    • 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
    • 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
    • C07K5/12—Cyclic peptides with only normal peptide bonds in the ring
    • 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
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/02—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length in solution
    • 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
    • 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
    • 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
    • C07K5/0806—Tripeptides with the first amino acid being neutral and aliphatic the side chain containing 0 or 1 carbon atoms, i.e. Gly, Ala
    • 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

Abstract

Un compuesto macrocíclico, que incluye los enantiomeros, estereoisomeros, rotámeros y tautomeros de dicho compuesto, y las sales y solvatos farmacéuticamente aceptables de dicho compuesto, teniendo dicho compuesto la formula general (1), en la cual: X e Y, independientemente entre si, son seleccionados de entre las siguientes partes: alquilo, alquil-arilo, heteroalquilo, heteroarilo, aril-heteroarilo, alquil-heteroarilo, cicloalquilo, alquil éter, alquil-aril éter, aril éter, alquil amino, aril amino, alquil-aril amino, alquil sulfuro, alquil-aril sulfuro, aril sulfuro, alquil sulfona, alquil-aril sulfona, aril sulfona, alquil-alquil sulfoxido, alquil-aril sulfoxido, alquil amida, alquil-aril amida, aril amida, alquil sulfonamida, alquil-aril sulfonamida, aril sulfonamida, alquil urea, alquil-aril urea, aril urea, alquil carbamato, alquil-aril carbamato, aril carbamato, alquil-hidrazida, alquil-arida hidrazida, alquil hidroxamida, alquil-aril hidroxamida, alquil sulfonilo, aril sulfonilo, heteroalquil sulfonilo, heteroaril sulfonilo, alquil carbonilo, aril carbonilo, heteroalquil carbonilo, heteroaril carbonilo, alcoxicarbonilo, ariloxicarbonilo, heteroariloxicarbonilo, alquilaminocarbonilo, arilaminocarbonilo, heteroarilaminocarbonilo o una combinacion de los mismos, con la condicion que X e Y pueden estar opcionalmente sustituidos por partes seleccionadas de entre el grupo consistente en aromático, alquilo, alquil-arilo, heteroalquilo, aril-heteroarilo, alquil-heteroarilo, cicloalquilo, alquil éter, alquil-aril éter, alquil sulfuro, alquil-aril sulfuro, alquil sulfona, alquil-aril sulfona, alquil amida, alquil-aril amida, alquil sulfonamida, alquil aminas, alquil-aril aminas, alquil-aril sulfonamida, alquil urea, alquil-aril urea, alquil carbamato y alquil-aril carbamato; R1 = COR5 o B(OR)2, en lo cual R5 = H, OH, OR8, NR9R10, CF3, C2F5, C3F7, CF2R6, R6, COR7, siendo R7 = H, OH, OR8, CHR9R10, o NR9R10, siendo R6, R8, R9 y R10, independientemente entre si, seleccionados de entre el grupo consistente 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')R', 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')CONNR12R13, CH(R1')CONHCH(R2')CONHCH(R3')CONHCH(R4')CONHCH(R5')COOR11, CH(R1')CONHCH(R2')CONHCH(R3')CONHCH(R4')CONHCH(R5') CONR12R13, en lo cual R1', R2', R3', R4', R5', R11, R12, R13 y R' son independientemente entre si seleccionados de entre el grupo consistente en H, alquilo, arilo, heteroalquilo, heteroarilo, cicloalquilo, alquil-arilo, alquil-heteroarilo, aril-alquilo y heteroaralquilo; Z es seleccionado de entre O, N o CH; W puede hallarse presente o ausente, y si W se halla presente, E es seleccionado de entre C = O, C = S o SO2; Q puede hallarse presente o ausente, y si Q se halla presente, Q es CH, N, P, (CH2)p, (CHR)p, (CRR')p, O, NR, S, o SO2; y cuando Q se halla ausente, M también falta, y A está directamente unido a X; A es O, CH2, (CHR)p, (CHR-CHR')p, (CRR')p , NR, S, SO2 o un enlace; E es CH, N o CR, o un doble enlace hacia, A, L o G; G puede estar presente o ausente, y cuando G se halla presente, G es (CH2)p, (CHR)p, o (CRR')p; y cuando G se halla ausente, J se halla presente y E está directamente conectado al átomo de carbono al cual estaba unido G; J puede hallarse presente o ausente, y si J se halla presente, J es (CH2)p, (CHR)p, o (CRR')p, SO2, NH, NR u O; y cuando J se halla ausente, G se halla presente y E está directamente unido a N; L puede hallarse presente o ausente, y si L se halla presente, L es CH, CR, O, S o NR; y cuando L se halla ausente, entonces M puede hallarse presente o ausente, y si M está presente estando L ausente, entonces M se halla directa e independientemente vinculado a E, y J está directa e independientemente unido a E; M puede estar presente o ausente, y cuando M se halla presente, M es O, NR, S, SO2, (CH2)p, (CHR)p (CHR-CHR')p, o (CRR')p; p es un numero de 0 a 6; y R, R', R2, R3 y R4, independientemente entre si, son seleccionados de entre el grupo consistente en H; alquilo de 1 a 10 átomos de carbono; alquenilo de 2 a 10 átomos de carbono; cicloalquilo de 3 a 8 átomos de carbono; C3-8 cicloalquilo; C3-8 heterocicloalquilo, alcoxi, ariloxi, alquiltio, ariltio, amino, amido, éster, ácido carboxílico, carbamato, urea, cetona, aldehido, ciano, nitro; átomos de oxígeno, nitrogeno, azufre, o fosforo, en una cantidad de uno a seis; (cicloalquil)alquilo y (heterocicloalquil)alquilo, estando dicho cicloalquilo hecho de 3 a 8 átomos de carbono, y de 0 a 6 átomos de oxígeno, nitrogeno, azufre o fosforo; y dicho alquilo es de 1 a 6 átomos de carbono; arilo, heteroarilo; alquil-arilo; y alquil-heteroarilo, pudiendo dichas partes alquilo, heteroalquilo, alquenilo, heteroalquenilo, arilo, heteroarilo, cicloalquilo y heterocicloalquilo, estar opcionalmente sustituidos, refiriéndose dicho término "sustituido" a una sustitucion, opcional y adecuada, con una o mas partes seleccionadas de entre el grupo consistente en alquilo, alquenilo, alquinilo, arilo, aralquilo, cicloalquilo, heterocíclico, halogeno, hidroxi, tio, alcoxi, ariloxi, alquiltio, ariltio, amino, amido, éster, ácido carboxílico, carbamato, urea, cetona, aldehido, ciano, nitro, sulfonamida, sulfoxido, sulfona, sulfonil urea, hidrazida e hidroxamato. En otra forma de realizacion, se revelan composiciones farmacéuticas que comprenden dichos macrociclos y también utilizacion de dichos compuestos para la manufactura de medicamentos a efectos de tratar los trastornos asociados con la HCV proteasa.
ARP010101579A 2000-04-05 2001-04-03 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 AR029903A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US19460700P 2000-04-05 2000-04-05

Publications (1)

Publication Number Publication Date
AR029903A1 true AR029903A1 (es) 2003-07-23

Family

ID=22718227

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP010101579A AR029903A1 (es) 2000-04-05 2001-04-03 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

Country Status (26)

Country Link
US (1) US6846802B2 (es)
EP (1) EP1268525B1 (es)
JP (1) JP4748911B2 (es)
KR (1) KR20030036152A (es)
CN (1) CN1441806A (es)
AR (1) AR029903A1 (es)
AT (1) ATE419270T1 (es)
AU (1) AU2001253124A1 (es)
BR (1) BR0109861A (es)
CA (1) CA2405521C (es)
CZ (1) CZ20023321A3 (es)
DE (1) DE60137207D1 (es)
EC (1) ECSP014009A (es)
ES (1) ES2317900T3 (es)
HK (1) HK1047947A1 (es)
HU (1) HUP0400456A3 (es)
IL (1) IL151934A0 (es)
MX (1) MXPA02009920A (es)
NO (1) NO20024797L (es)
NZ (1) NZ521455A (es)
PE (1) PE20020188A1 (es)
PL (1) PL359359A1 (es)
RU (1) RU2002129564A (es)
SK (1) SK14192002A3 (es)
WO (1) WO2001077113A2 (es)
ZA (1) ZA200207845B (es)

Families Citing this family (152)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SK286105B6 (sk) 1996-10-18 2008-03-05 Vertex Pharmaceuticals Incorporated Inhibítory serínových proteáz, najmä NS3 proteázyvírusu hepatitídy C, farmaceutická kompozícia a použitie
US6608027B1 (en) 1999-04-06 2003-08-19 Boehringer Ingelheim (Canada) Ltd Macrocyclic peptides active against the hepatitis C virus
US7244721B2 (en) * 2000-07-21 2007-07-17 Schering Corporation Peptides as NS3-serine protease inhibitors of hepatitis C virus
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
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
DE60336986D1 (de) 2002-03-05 2011-06-16 Sumitomo Chemical Co Verfahren zur herstellung von biarylverbindungen
RU2004133044A (ru) 2002-04-11 2006-01-27 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибиторы сериновых протеаз, в частности, протеазы ns3-ns4a hcv
US20050075279A1 (en) 2002-10-25 2005-04-07 Boehringer Ingelheim International Gmbh Macrocyclic peptides active against the hepatitis C virus
RS51294B (sr) 2003-05-21 2010-12-31 Boehringer Ingelheim International Gmbh. Inhibitorna jedinjenja za hepatitis c
DK1633774T3 (da) 2003-06-18 2010-05-25 Tranzyme Pharma Inc Makrocykliske motilinreceptorantagonister
JP4527722B2 (ja) 2003-08-26 2010-08-18 シェーリング コーポレイション Ｃ型肝炎ウイルスの新規のペプチド模倣性ｎｓ３−セリンプロテアーゼインヒビター
MY148123A (en) 2003-09-05 2013-02-28 Vertex Pharma Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
PE20050431A1 (es) 2003-09-22 2005-07-19 Boehringer Ingelheim Int Peptidos macrociclicos activos contra el virus de la hepatitis c
TWI280964B (en) * 2003-09-26 2007-05-11 Schering Corp Macrocyclic inhibitors of hepatitis C virus NS3 serine protease
NZ546663A (en) 2003-10-10 2010-01-29 Vertex Pharma Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US7491794B2 (en) * 2003-10-14 2009-02-17 Intermune, Inc. Macrocyclic compounds as inhibitors of viral replication
WO2005043118A2 (en) 2003-10-27 2005-05-12 Vertex Pharmaceuticals Incorporated Drug discovery method
EP1944042A1 (en) 2003-10-27 2008-07-16 Vertex Pharmceuticals Incorporated Combinations for HCV treatment
WO2005051980A1 (en) 2003-11-20 2005-06-09 Schering Corporation Depeptidized inhibitors of hepatitis c virus ns3 protease
JP4682155B2 (ja) 2004-01-21 2011-05-11 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型肝炎ウイルスに対して活性な大環状ペプチド
JP4902361B2 (ja) * 2004-01-30 2012-03-21 メディヴィル・アクチエボラーグ Ｈｃｖｎｓ−３セリンプロテアーゼインヒビター
US7683033B2 (en) 2004-02-04 2010-03-23 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly HCV NS3-NS4A protease
US20070049593A1 (en) 2004-02-24 2007-03-01 Japan Tobacco Inc. Tetracyclic fused heterocyclic compound and use thereof as HCV polymerase inhibitor
RS50815B (sr) 2004-02-24 2010-08-31 Japan Tobacco Inc. Kondenzovana heterotetraciklična jedinjenja i njihova upotreba kao inhibitora hcv polimeraza
DE602005015093D1 (de) 2004-02-27 2009-08-06 Schering Corp Neue verbindungen als inhibitoren der ns3-serinprotease des hepatitis-c-virus
CN1946692A (zh) 2004-02-27 2007-04-11 先灵公司 作为丙型肝炎病毒ns3丝氨酸蛋白酶抑制剂的3,4－(环戊基)－稠合的脯氨酸化合物
US7816326B2 (en) 2004-02-27 2010-10-19 Schering Corporation Sulfur 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
RU2428428C9 (ru) 2004-02-27 2012-03-10 Шеринг Корпорейшн Серусодержащие соединения, действующие как ингибиторы сериновой протеазы ns3 вируса гепатита с
AU2005222055A1 (en) 2004-02-27 2005-09-22 Schering Corporation Compounds as inhibitors of hepatitis C virus NS3 serine protease
US7399749B2 (en) 2004-05-20 2008-07-15 Schering Corporation Substituted prolines as inhibitors of hepatitis C virus NS3 serine protease
JP2005350417A (ja) * 2004-06-11 2005-12-22 Dai Ichi Seiyaku Co Ltd 還元的エーテル化法を用いたピロリジン誘導体の製造法
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
WO2006026352A1 (en) 2004-08-27 2006-03-09 Schering Corporation Acylsulfonamide compounds as inhibitors of hepatitis c virus ns3 serine protease
WO2007001406A2 (en) * 2004-10-05 2007-01-04 Chiron Corporation Aryl-containing macrocyclic compounds
US7659263B2 (en) 2004-11-12 2010-02-09 Japan Tobacco Inc. Thienopyrrole compound and use thereof as HCV polymerase inhibitor
JP4705164B2 (ja) * 2005-05-02 2011-06-22 メルク・シャープ・エンド・ドーム・コーポレイション Ｈｃｖｎｓ３プロテアーゼ阻害剤
AU2006252553B2 (en) * 2005-06-02 2012-03-29 Merck Sharp & Dohme Corp. Combination of HCV protease inhibitors with a surfactant
US20110104109A1 (en) * 2005-07-13 2011-05-05 Frank Bennett Tetracyclic indole derivatives and their use for treating or preventing viral infections
TWI387603B (zh) 2005-07-20 2013-03-01 Merck Sharp & Dohme Ｈｃｖ ｎｓ３蛋白酶抑制劑
CN101263156A (zh) 2005-07-25 2008-09-10 因特蒙公司 C型肝炎病毒复制的新颖大环抑制剂
NZ565269A (en) * 2005-08-01 2010-03-26 Merck & Co Inc Macrocyclic peptides as HCV NS3 protease inhibitors
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
PT1934179E (pt) 2005-08-19 2010-07-12 Vertex Pharma PROCESSOS E INTERMEDIáRIOS
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
DK1999129T3 (da) 2005-10-11 2011-02-07 Intermune Inc Forbindelser og fremgangsmåder til inhibering af replikationen af hepatitis C-virus
NZ568324A (en) 2005-11-11 2012-01-12 Vertex Pharma Hepatitis C virus variants
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
CN101489557B (zh) 2006-02-27 2013-12-18 弗特克斯药品有限公司 包含vx-950的共晶体和包含所述共晶体的药物组合物
WO2007109080A2 (en) 2006-03-16 2007-09-27 Vertex Pharmaceuticals Incorporated Deuterated hepatitis c protease inhibitors
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
GB0612423D0 (en) 2006-06-23 2006-08-02 Angeletti P Ist Richerche Bio Therapeutic agents
KR20090024834A (ko) * 2006-07-05 2009-03-09 인터뮨, 인크. Ｃ형 간염 바이러스 복제의 신규 억제제
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
KR20090042973A (ko) 2006-08-17 2009-05-04 베링거 인겔하임 인터내셔날 게엠베하 바이러스 폴리머라제 억제제
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
AU2007309488B2 (en) * 2006-10-24 2012-10-11 Merck Sharp & Dohme Corp. HCV NS3 protease inhibitors
JP5345541B2 (ja) * 2006-10-24 2013-11-20 メルク・シャープ・アンド・ドーム・コーポレーション Ｈｃｖｎｓ３プロテアーゼ阻害剤
JP5268927B2 (ja) * 2006-10-27 2013-08-21 メルク・シャープ・アンド・ドーム・コーポレーション Ｈｃｖｎｓ３プロテアーゼ阻害剤
CN101568346B (zh) * 2006-10-27 2015-11-25 默沙东公司 Hcv ns3蛋白酶抑制剂
CA2672250C (en) 2006-12-20 2013-04-30 Ian Stansfield Antiviral indoles
GB0625345D0 (en) 2006-12-20 2007-01-31 Angeletti P Ist Richerche Bio Therapeutic compounds
GB0625349D0 (en) 2006-12-20 2007-01-31 Angeletti P Ist Richerche Bio Therapeutic compounds
MX2009006878A (es) * 2006-12-22 2009-07-07 Schering Corp Derivados indolicos con anillo unido en las posiciones 4,5 para tratar o prevenir infecciones virales por virus de la hepatitis c e infecciones virales relacionadas.
AU2007339382B2 (en) 2006-12-22 2013-05-02 Merck Sharp & Dohme Llc 4,5-ring annulated indole derivatives for treating or preventing of HCV and related viral infections
CA2674831A1 (en) 2006-12-22 2008-11-13 Schering Corporation 5,6-ring annulated indole derivatives and methods of use thereof
AR065498A1 (es) 2007-02-27 2009-06-10 Vertex Pharma Co- critales de vx-950 (un inhibidor del virus de la hepatitis c) y composiciones farmaceuticas que los comprenden
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
SG174809A1 (en) * 2007-05-03 2011-10-28 Intermune Inc Macrocyclic compounds useful as inhibitors of hepatitis c virus
EP2142215B1 (en) 2007-05-04 2012-03-07 Vertex Pharmceuticals 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.
CN101754970B (zh) 2007-07-17 2013-07-10 P.安杰莱蒂分子生物学研究所 用于治疗丙型肝炎的大环吲哚衍生物
CA2699891C (en) 2007-07-19 2013-10-22 Nigel Liverton Macrocyclic compounds as antiviral agents
EP2188274A4 (en) 2007-08-03 2011-05-25 Boehringer Ingelheim Int VIRAL POLYMERASE HEMMER
AR068107A1 (es) * 2007-08-29 2009-11-04 Schering Corp Derivados indolicos 2,3 sustituidos y una composicion farmaceutica
EP2408761B1 (en) 2007-08-29 2014-01-01 Merck Sharp & Dohme Corp. Substituted indole derivatives and methods of use thereof
AR068108A1 (es) 2007-08-29 2009-11-04 Schering Corp Derivados azaindol 2,3-sustituidos y una composicion farmaceutica
CA2704284A1 (en) * 2007-08-30 2009-03-12 Vertex Pharmaceuticals Incorporated Co-crystals and pharmaceutical compositions comprising the same
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
CL2008003384A1 (es) 2007-11-14 2009-12-11 Enanta Pharm Inc Compuestos derivados de quinoxalina macrocíclica, inhibidores de serina proteasa; composicion farmaceutica que los comprende; y su uso en el tratamiento de la hepatitis c.
EP2219454A4 (en) 2007-11-14 2012-05-30 Enanta Pharm Inc HEMMER OF MACROCYCLIC TETRAZOLYL HEPATITIS C SERIN PROTEASE
EP2222660B1 (en) * 2007-11-16 2014-03-26 Merck Sharp & Dohme Corp. 3-heterocyclic substituted indole derivatives and methods of use thereof
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
WO2009079352A1 (en) 2007-12-14 2009-06-25 Enanta Pharmaceuticals, Inc. Macrocyclic oximyl hepatitis c serine protease inhibitors
WO2009079353A1 (en) 2007-12-14 2009-06-25 Enanta Pharmaceuticals, Inc. Triazole-containing macrocyclic hcv serine protease inhibitors
AU2008338273B2 (en) 2007-12-19 2014-10-02 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
KR100967989B1 (ko) * 2008-01-16 2010-07-07 연세대학교 산학협력단 구조변경이 가능한 전환형 휠체어
BRPI0908021A2 (pt) 2008-02-04 2015-07-21 Idenix Pharmaceuticals Inc Composto, composição farmacêutica, e, usos do composto ou da composição farmacêutica
EP2268285B1 (en) 2008-02-25 2018-06-27 Merck Sharp & Dohme Corp. Therapeutic compounds
EP2268619A4 (en) * 2008-03-20 2012-04-04 Enanta Pharm Inc FLUORINATED MACROCYCLIC COMPOUNDS AS INHIBITORS OF HEPATITIS C VIRUS
JP2011519364A (ja) 2008-04-15 2011-07-07 インターミューン・インコーポレーテッド Ｃ型肝炎ウイルス複製の新規大環状阻害剤
AU2009241445A1 (en) 2008-04-28 2009-11-05 Merck Sharp & Dohme Corp. HCV NS3 protease inhibitors
WO2009152200A1 (en) * 2008-06-13 2009-12-17 Schering Corporation Tricyclic indole derivatives and methods of use thereof
NZ590638A (en) 2008-07-22 2012-06-29 Merck Sharp & Dohme MACROCYCLIC QUINOXALINE COMPOUNDS AS Hepatitis C Virus NS3 PROTEASE INHIBITORS
TWI409265B (zh) 2008-08-20 2013-09-21 Merck Sharp & Dohme 經取代之吡啶及嘧啶衍生物及彼等於治療病毒感染之用途
AR072939A1 (es) 2008-08-20 2010-09-29 Schering Corp Derivados de piridina y pirimidina sustituidas con etenilo y su uso en el tratamiento de infecciones virales
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
TW201020245A (en) 2008-08-20 2010-06-01 Schering Corp Ethynyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections
RU2011127080A (ru) 2009-01-07 2013-02-20 Сайнексис, Инк. Производное циклоспорина для применения в лечении заражения вирусом гепатита с и вич
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.
EP2403860B1 (en) 2009-03-04 2015-11-04 IDENIX Pharmaceuticals, Inc. Phosphothiophene and phosphothiazole as hcv polymerase inhibitors
EP2417134B1 (en) 2009-04-08 2017-05-17 Idenix Pharmaceuticals LLC. Macrocyclic serine protease inhibitors
US8936781B2 (en) * 2009-05-13 2015-01-20 Enanta Pharmaceuticals, Inc. Macrocyclic compounds as hepatitis C virus inhibitors
AU2010253791A1 (en) 2009-05-29 2011-11-24 Merck Sharp & Dohme Corp. Antiviral compounds composed of three linked Aryl moieties to treat diseases such as Hepatitis C
US8937150B2 (en) 2009-06-11 2015-01-20 Abbvie Inc. Anti-viral compounds
ES2565536T3 (es) * 2009-06-11 2016-04-05 Abbvie Bahamas Ltd. Heterociclos trisustituidos como inhibidores de la replicación del virus de la Hepatitis C VHC
WO2011014487A1 (en) 2009-07-30 2011-02-03 Merck Sharp & Dohme Corp. Hepatitis c virus ns3 protease inhibitors
AU2009350857A1 (en) * 2009-08-05 2012-02-02 Polyphor Ag Conformationally constrained, fully synthetic macrocyclic compounds
WO2011017389A1 (en) 2009-08-05 2011-02-10 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors useful against viral infections, particularly hcv
AU2010298028A1 (en) * 2009-09-28 2012-04-19 Intermune, Inc. Cyclic peptide inhibitors of hepatitis C virus replication
US20110117055A1 (en) 2009-11-19 2011-05-19 Macdonald James E Methods of Treating Hepatitis C Virus with Oxoacetamide Compounds
WO2011066241A1 (en) 2009-11-25 2011-06-03 Schering Corporation Fused tricyclic compounds and derivatives thereof useful for the treatment of viral diseases
EP2513113B1 (en) 2009-12-18 2018-08-01 Idenix Pharmaceuticals LLC 5,5-fused arylene or heteroarylene hepatitis c virus inhibitors
US20130156731A1 (en) 2009-12-22 2013-06-20 Kevin X. Chen Fused tricyclic compounds and methods of use thereof for the treatment of viral diseas
US9433621B2 (en) 2010-02-18 2016-09-06 Merck Sharp & Dohme Corp. Substituted pyridine and pyrimidine derivatives and their use in treating viral infections
EA201290882A1 (ru) 2010-03-09 2013-04-30 Мерк Шарп Энд Домэ Корп. Конденсированные трициклические силильные соединения и способы их применения для лечения вирусных заболеваний
NZ605440A (en) 2010-06-10 2014-05-30 Abbvie Bahamas Ltd Solid compositions comprising an hcv inhibitor
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
AU2011305695B2 (en) 2010-09-21 2016-05-19 Enanta Pharmaceuticals, Inc. Macrocyclic proline derived HCV serine protease inhibitors
JP2013540122A (ja) 2010-09-29 2013-10-31 メルク・シャープ・エンド・ドーム・コーポレイション 縮合四環式化合物誘導体およびウィルス疾患治療のためのそれの使用方法
WO2012109398A1 (en) 2011-02-10 2012-08-16 Idenix Pharmaceuticals, Inc. Macrocyclic serine protease inhibitors, pharmaceutical compositions thereof, and their use for treating hcv infections
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
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
US9156872B2 (en) 2011-04-13 2015-10-13 Merck Sharp & Dohme Corp. 2′-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
US9061041B2 (en) 2011-04-13 2015-06-23 Merck Sharp & Dohme Corp. 2′-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
US10201584B1 (en) 2011-05-17 2019-02-12 Abbvie Inc. Compositions and methods for treating HCV
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
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
WO2013039876A1 (en) 2011-09-14 2013-03-21 Merck Sharp & Dohme Corp. Silyl-containing heterocyclic compounds and methods of use thereof for the treatment of viral diseases
US9034832B2 (en) 2011-12-29 2015-05-19 Abbvie Inc. Solid compositions
US11484534B2 (en) 2013-03-14 2022-11-01 Abbvie Inc. Methods for treating HCV
US10051347B2 (en) 2013-08-02 2018-08-14 Stephen Hollis Displacement sensor
US20160229866A1 (en) 2013-09-20 2016-08-11 Idenix Pharmaceuticals Inc. Hepatitis c virus inhibitors
WO2015065817A1 (en) 2013-10-30 2015-05-07 Merck Sharp & Dohme Corp. Pseudopolymorphs of an hcv ns5a inhibitor and uses thereof
EP3089757A1 (en) 2014-01-03 2016-11-09 AbbVie Inc. Solid antiviral dosage forms
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
WO2015134560A1 (en) 2014-03-05 2015-09-11 Idenix Pharmaceuticals, Inc. Solid forms of a flaviviridae virus inhibitor compound and salts thereof
JP2015155430A (ja) * 2015-04-02 2015-08-27 ポリフォー・アクチェンゲゼルシャフトＰｏｌｙｐｈｏｒ Ａｇ コンホメーションを固定された、合成マクロ環化合物
JP2017160247A (ja) * 2017-05-10 2017-09-14 ポリフォー・アクチェンゲゼルシャフトＰｏｌｙｐｈｏｒ Ａｇ コンホメーションを固定された、合成マクロ環化合物
WO2019055657A1 (en) * 2017-09-14 2019-03-21 The Board Of Trustees Of The Leland Stanford Junior University BAF COMPLEX MODULATION COMPOUNDS AND METHODS OF USE
US20210315876A1 (en) * 2018-07-12 2021-10-14 The Board Of Trustees Of The Le-Land Stanford Junior University Methods for reversing hiv latency using baf complex modulating compounds
CN113387842A (zh) * 2021-07-08 2021-09-14 成都泰和伟业生物科技有限公司 一种通过OTf胺化合成芳香伯胺的方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HU216017B (hu) 1987-11-18 1999-04-28 Chiron Corp. Eljárás HCV-1 polipeptidek, HCV-1 polinukleotidok, rekombináns vektorok és gazdasejtek, valamint immunesszé kit, hepatitis C vírusfertőzés elleni vakcinák, a fertőzés kimutatására szolgáló diagnosztikumok előállítására, és immunvizsgálati és vírustenyészt
DE69024378T2 (de) 1989-02-01 1996-09-12 Asahi Glass Co Ltd Azeotrope oder azeotropähnliche Zusammensetzung auf der Basis von Chlorfluorkohlenwasserstoffen
ES2219637T3 (es) 1990-04-04 2004-12-01 Chiron Corporation Proteasa del virus de la hepatitis c.
SK286105B6 (sk) 1996-10-18 2008-03-05 Vertex Pharmaceuticals Incorporated Inhibítory serínových proteáz, najmä NS3 proteázyvírusu hepatitídy C, farmaceutická kompozícia a použitie
GB9623908D0 (en) 1996-11-18 1997-01-08 Hoffmann La Roche Amino acid derivatives
EP1012180B1 (en) * 1997-08-11 2004-12-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor peptide analogues
GB9812523D0 (en) * 1998-06-10 1998-08-05 Angeletti P Ist Richerche Bio Peptide inhibitors of hepatitis c virus ns3 protease
US6576613B1 (en) * 1998-07-24 2003-06-10 Corvas International, Inc. Title inhibitors of urokinase
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

Also Published As

Publication number Publication date
US6846802B2 (en) 2005-01-25
WO2001077113A2 (en) 2001-10-18
NO20024797D0 (no) 2002-10-04
PL359359A1 (en) 2004-08-23
PE20020188A1 (es) 2002-03-13
KR20030036152A (ko) 2003-05-09
HK1047947A1 (zh) 2003-03-14
JP4748911B2 (ja) 2011-08-17
HUP0400456A3 (en) 2005-09-28
JP2003530401A (ja) 2003-10-14
ES2317900T3 (es) 2009-05-01
NO20024797L (no) 2002-12-04
ECSP014009A (es) 2003-03-31
CZ20023321A3 (cs) 2003-01-15
US20020107181A1 (en) 2002-08-08
CN1441806A (zh) 2003-09-10
EP1268525A2 (en) 2003-01-02
CA2405521C (en) 2010-06-29
NZ521455A (en) 2004-06-25
ZA200207845B (en) 2004-02-11
BR0109861A (pt) 2003-06-10
IL151934A0 (en) 2003-04-10
EP1268525B1 (en) 2008-12-31
HUP0400456A2 (hu) 2004-06-28
DE60137207D1 (de) 2009-02-12
RU2002129564A (ru) 2004-05-10
AU2001253124A1 (en) 2001-10-23
ATE419270T1 (de) 2009-01-15
MXPA02009920A (es) 2003-03-27
CA2405521A1 (en) 2001-10-18
WO2001077113A3 (en) 2002-06-20
SK14192002A3 (sk) 2003-03-04

Similar Documents

Publication Publication Date Title
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
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,
AR038214A1 (es) Compuestos de prolina como inhibidores de la serina proteasa ns3 del virus de la hepatitis c
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
AR033985A1 (es) Peptidos inhibidores de proteasa serina-ns3 del virus de la hepatitis c, composicion farmaceutica que los comprende, un metodo para su preparacion, uso de los mismos para la fabricacion de un medicamento y un metodo de modulacion de la actividad de la proteasa del virus de la hepatitis c
AR034127A1 (es) 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
AR038183A1 (es) Peptidos como inhibidores de la proteasa serina ns3 del virus de la hepatitis c
AR055198A1 (es) Formulaciones farmaceuticas y metodos de tratamiento que las utilizan
ATE556058T1 (de) 1-(2h)-isochinolonderivat
TW200745029A (en) Sulfonamide derivatives exhibiting PGD2 receptor antagonism
CY1105899T1 (el) Πυριδινοϋλοπιπepιδινες ως 5-ht1f αγωνιστες
CA2445190A1 (en) Indole, azaindole and related heterocyclic amidopiperazine derivatives
AR031905A1 (es) Peptidos diarilicos como inhibidores de ns3-serina proteasa en hepatitis de virus c
MX9202142A (es) Nuevos derivados de urea, proceso para su preparacion, y composicion farmaceutica que los comprende.
ATE368655T1 (de) Stickstoffhaltige heterocyclische verbindung und arzneimittel davon
AR015512A1 (es) Derivados ciclicos n-acilo amina, un procedimiento para su preparacion, un intermediario y una composicion farmaceutica
HRP20070430T3 (en) (3-oxo-3,4-dihydro-quinoxalin-2-yl-amino)-benzamide derivatives and related compounds as glycogen phosphorylase inhibitors for the treatment of diabetes and obesity
AR033379A1 (es) Compuestos de difenilurea, procedimiento para su preparacion y composiciones farmaceuticas que los contienen
IT1228293B (it) Benzoderivati di composti eterociclici contenenti azoto.
EA200300718A1 (ru) Производные 3-индолина, которые могут применяться при лечении психиатрических и неврологических расстройств
DE602004031722D1 (de) Kondensierte bizyklisch substituierte amine als histamin 3 rezeptor liganden
ATE276257T1 (de) Pyrazinonderivate
DE69934514D1 (de) Chinolinderivate als nk-2 und nk-3 rezeptor-liganden
AR037459A1 (es) Antagonistas vi del receptor ccr-3
EA200602193A1 (ru) Меркаптоимидазолы в качестве антагонистов рецептора ccr2

Legal Events

Date Code Title Description
FB Suspension of granting procedure