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
Links
Classifications
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- 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
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- 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
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- 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
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- 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
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.
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) | CN1432022A (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 (130)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP4080541B2 (ja) * | 1996-10-18 | 2008-04-23 | 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 |
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 |
MXPA03005219A (es) * | 2000-12-12 | 2003-09-25 | Schering Corp | Peptidos diarilicos como inhibidores de ns3-serina proteasa en hepatitis de virus c. |
WO2002057287A2 (en) | 2001-01-22 | 2002-07-25 | 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 |
US7091184B2 (en) | 2002-02-01 | 2006-08-15 | Boehringer Ingelheim International Gmbh | Hepatitis C inhibitor tri-peptides |
US6642204B2 (en) | 2002-02-01 | 2003-11-04 | Boehringer Ingelheim International Gmbh | Hepatitis C inhibitor tri-peptides |
NZ561851A (en) | 2002-04-11 | 2009-05-31 | Vertex Pharma | Inhibitors of serine proteases, particularly hepatitis C virus NS3 - NS4 protease |
US20050075279A1 (en) | 2002-10-25 | 2005-04-07 | Boehringer Ingelheim International Gmbh | Macrocyclic peptides active against the hepatitis C virus |
PT1654261E (pt) | 2003-05-21 | 2008-01-18 | Boehringer Ingelheim Int | Compostos inibidores da hepatite c |
US20090198050A1 (en) * | 2003-06-18 | 2009-08-06 | 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 |
US7476653B2 (en) * | 2003-06-18 | 2009-01-13 | Tranzyme Pharma, Inc. | Macrocyclic modulators of the ghrelin receptor |
WO2004111077A1 (en) | 2003-06-18 | 2004-12-23 | Tranzyme Pharma Inc. | Macrocyclic antagonists of the motilin receptor |
CA2536570A1 (en) | 2003-08-26 | 2005-03-10 | 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 |
DE602004031645D1 (de) | 2003-09-22 | 2011-04-14 | Boehringer Ingelheim Pharma | Makrozyklische peptide mit wirkung gegen das hepatitis-c-virus |
KR20060085248A (ko) * | 2003-09-26 | 2006-07-26 | 쉐링 코포레이션 | C형 간염 바이러스 ns3 세린 프로테아제의마크로사이클릭 억제제 |
CA2541634A1 (en) | 2003-10-10 | 2005-04-28 | Vertex Pharmaceuticals Incorporated | 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 |
US8187874B2 (en) * | 2003-10-27 | 2012-05-29 | Vertex Pharmaceuticals Incorporated | Drug discovery method |
EP1944042A1 (en) | 2003-10-27 | 2008-07-16 | Vertex Pharmceuticals Incorporated | Combinations for HCV treatment |
EP1689770A1 (en) | 2003-11-20 | 2006-08-16 | Schering Corporation | Depeptidized inhibitors of hepatitis c virus ns3 protease |
CA2549851C (en) | 2004-01-21 | 2012-09-11 | Boehringer Ingelheim International Gmbh | Macrocyclic peptides active against the hepatitis c virus |
AU2005212257A1 (en) | 2004-02-04 | 2005-08-25 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases, particularly HCV NS3-NS4A protease |
WO2005087721A2 (en) | 2004-02-27 | 2005-09-22 | Schering Corporation | Compounds as inhibitors of hepatitis c virus ns3 serine protease |
TWI314927B (en) | 2004-02-27 | 2009-09-21 | Schering Corporatio | Sulfur compounds as inhibitors of hepatitis c virus ns3 serine protease |
US7816326B2 (en) | 2004-02-27 | 2010-10-19 | Schering Corporation | Sulfur compounds as inhibitors of hepatitis C virus NS3 serine protease |
ATE438622T1 (de) | 2004-02-27 | 2009-08-15 | Schering Corp | 3,4-(cyclopentyl)kondensierte prolinverbindungen als inhibitoren der ns3-serinprotease des hepatitis-c-virus |
RU2006134002A (ru) | 2004-02-27 | 2008-04-10 | Шеринг Корпорейшн (US) | Новые соединения, действующие как ингибиторы сериновой протеазы ns3 вируса гепатита с |
TW200536528A (en) | 2004-02-27 | 2005-11-16 | Schering Corp | Novel inhibitors of hepatitis C virus NS3 protease |
WO2005113581A1 (en) | 2004-05-20 | 2005-12-01 | Schering Corporation | Substituted prolines as inhibitors of hepatitis c virus ns3 serine protease |
UY29016A1 (es) | 2004-07-20 | 2006-02-24 | Boehringer Ingelheim Int | Analogos de dipeptidos inhibidores de la hepatitis c |
EP1771454B1 (en) | 2004-07-20 | 2011-06-15 | Boehringer Ingelheim International GmbH | Hepatitis c inhibitor peptide analogs |
US7550559B2 (en) | 2004-08-27 | 2009-06-23 | 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 |
US20070237818A1 (en) * | 2005-06-02 | 2007-10-11 | Malcolm Bruce A | Controlled-release formulation of HCV protease inhibitor and methods using the same |
NZ563365A (en) * | 2005-06-02 | 2011-02-25 | Schering Corp | Combination of HCV protease inhibitors with a surfactant |
US8119602B2 (en) | 2005-06-02 | 2012-02-21 | Schering Corporation | Administration of HCV protease inhibitors in combination with food to improve bioavailability |
US20110104109A1 (en) * | 2005-07-13 | 2011-05-05 | Frank Bennett | Tetracyclic indole derivatives and their use for treating or preventing viral infections |
JP5249028B2 (ja) | 2005-07-25 | 2013-07-31 | 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 |
MX2008001402A (es) * | 2005-07-29 | 2008-04-04 | Tibotec Pharm Ltd | Inhibidores macrociclicos del virus de la hepatitis c. |
AU2006275413B2 (en) | 2005-08-02 | 2012-07-19 | Vertex Pharmaceuticals Incorporated | Inhibitors of serine proteases |
US8399615B2 (en) | 2005-08-19 | 2013-03-19 | Vertex Pharmaceuticals Incorporated | Processes and intermediates |
EP2357170A1 (en) * | 2005-08-19 | 2011-08-17 | 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 |
DE602006019323D1 (de) | 2005-10-11 | 2011-02-10 | Intermune Inc | Verbindungen und verfahren zur inhibierung der replikation des hepatitis-c-virus |
US7705138B2 (en) * | 2005-11-11 | 2010-04-27 | Vertex Pharmaceuticals Incorporated | Hepatitis C virus variants |
EP1951748B1 (en) | 2005-11-11 | 2013-07-24 | Vertex Pharmaceuticals, Inc. | Hepatitis c virus variants |
US7816348B2 (en) | 2006-02-03 | 2010-10-19 | Boehringer Ingelheim International Gmbh | Viral polymerase inhibitors |
JP5436864B2 (ja) | 2006-02-27 | 2014-03-05 | 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 | Vx−950を含む共結晶体およびそれを含む医薬組成物 |
EP1993994A2 (en) | 2006-03-16 | 2008-11-26 | Vertex Pharmceuticals Incorporated | Deuterated hepatitis c protease inhibitors |
CA2647158C (en) * | 2006-03-23 | 2012-07-31 | Schering Corporation | Combinations of hcv protease inhibitor(s) and cyp3a4 inhibitor(s), and methods of treatment related thereto |
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 |
RU2009109355A (ru) | 2006-08-17 | 2010-09-27 | БЕРИНГЕР ИНГЕЛЬХАЙМ ИНТЕРНАЦИОНАЛЬ ГмбХ (DE) | Ингибиторы вырусной полимеразы |
US8710178B2 (en) | 2006-10-18 | 2014-04-29 | Lincoln University | Macrocyclic cysteine protease inhibitors and compositions thereof |
ATE543808T1 (de) | 2006-12-22 | 2012-02-15 | Schering Corp | 5,6-ring-annelierte indolderivate und ihre verwendung |
KR20090106539A (ko) * | 2006-12-22 | 2009-10-09 | 쉐링 코포레이션 | Hcv 및 관련 바이러스 감염을 치료 또는 예방하기 위한 4,5-환 환상 인돌 유도체 |
US8557848B2 (en) | 2006-12-22 | 2013-10-15 | Merck Sharp & Dohme Corp. | 4,5-ring annulated indole derivatives for treating or preventing of HCV and related viral infections |
ES2379905T3 (es) | 2007-02-27 | 2012-05-04 | Vertex Pharmceuticals Incorporated | Co-cristales y composiciones farmacéuticas que los comprenden |
NZ579295A (en) | 2007-02-27 | 2012-03-30 | Vertex Pharma | Inhibitors of serine proteases |
EP2177523A1 (en) * | 2007-05-03 | 2010-04-21 | Intermune, Inc. | Novel macrocyclic inhibitors of hepatitis c virus replication |
CN102872461A (zh) | 2007-05-04 | 2013-01-16 | 弗特克斯药品有限公司 | 用于治疗hcv感染的组合治疗 |
JP2010526834A (ja) * | 2007-05-10 | 2010-08-05 | 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ペプチド阻害剤 |
US8242140B2 (en) | 2007-08-03 | 2012-08-14 | Boehringer Ingelheim International Gmbh | Viral polymerase inhibitors |
BRPI0815811A2 (pt) * | 2007-08-29 | 2015-02-18 | Schering Corp | Derivados de indol substituído e métodos de uso dos mesmos |
WO2009032125A1 (en) * | 2007-08-29 | 2009-03-12 | Schering Corporation | 2,3-substituted azaindole derivatives for treating viral infections |
KR20100049667A (ko) * | 2007-08-29 | 2010-05-12 | 쉐링 코포레이션 | 바이러스 감염 치료용 2,3-치환된 인돌 유도체 |
CL2008002549A1 (es) | 2007-08-30 | 2010-09-03 | Vertex Pharma | Cocristal que comprende vx-950 y un formador de cocristal seleccionado de acido 3-metoxi-4hidroxibenzoico,acido 2,4-dihidroxibenzoico y acido 2,5-dihidroxibenzoico; metodo de preparacion; composicion farmaceutica que comprende el cocristal, util como agente antiviral en el tratamiento del hcv. |
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 |
CA2705586A1 (en) * | 2007-11-16 | 2009-05-22 | Schering Corporation | 3-heterocyclic substituted indole derivatives and methods of use thereof |
CN102317285A (zh) * | 2007-11-16 | 2012-01-11 | 先灵公司 | 3-氨基磺酰基取代的吲哚衍生物及其使用方法 |
US8476257B2 (en) | 2007-12-19 | 2013-07-02 | Boehringer Ingelheim International Gmbh | Viral polymerase inhibitors |
US8293705B2 (en) | 2007-12-21 | 2012-10-23 | Avila Therapeutics, Inc. | HCV protease inhibitors and uses thereof |
WO2009082701A1 (en) | 2007-12-21 | 2009-07-02 | Avila Therapeutics, Inc. | Hcv protease inhibitors and uses thereof |
CA2709535A1 (en) * | 2007-12-21 | 2009-07-02 | Avila Therapeutics, Inc. | Hcv protease inhibitors and uses thereof |
US8309685B2 (en) | 2007-12-21 | 2012-11-13 | Celgene Avilomics Research, Inc. | HCV protease inhibitors and uses thereof |
EP2250174B1 (en) | 2008-02-04 | 2013-08-28 | IDENIX Pharmaceuticals, Inc. | Macrocyclic serine protease inhibitors |
CA2705300A1 (fr) * | 2008-02-15 | 2009-06-04 | Xeda International | Macrocyclic inhibitors of hepatitis c protease |
CN102015652A (zh) | 2008-03-20 | 2011-04-13 | 益安药业 | 作为丙型肝炎病毒抑制剂的氟化大环化合物 |
SG175692A1 (en) * | 2008-04-15 | 2011-11-28 | Intermune Inc | Novel macrocyclic inhibitors of hepatitis c virus replication |
US8901139B2 (en) * | 2008-06-13 | 2014-12-02 | Merck Sharp & Dohme Corp. | Tricyclic indole derivatives and methods of use thereof |
TW201020245A (en) | 2008-08-20 | 2010-06-01 | Schering Corp | Ethynyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections |
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 |
AR072938A1 (es) | 2008-08-20 | 2010-09-29 | Southern Res Inst | Derivados de piridina y pirimidina azosustituidos y su uso en el tratamiento de infecciones virales |
TW201020238A (en) | 2008-08-20 | 2010-06-01 | Schering Corp | Ethenyl-substituted pyridine and pyrimidine derivatives and their use in treating viral infections |
SG172848A1 (en) | 2009-01-07 | 2011-08-29 | Scynexis Inc | Cyclosporine derivative for use in the treatment of hcv and hiv infection |
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 |
US8377962B2 (en) | 2009-04-08 | 2013-02-19 | Idenix Pharmaceuticals, Inc. | Macrocyclic serine protease inhibitors |
WO2010138791A1 (en) | 2009-05-29 | 2010-12-02 | Schering Corporation | Antiviral compounds composed of three linked aryl moieties to treat diseases such as hepatitis c |
AR077712A1 (es) | 2009-08-05 | 2011-09-14 | Idenix Pharmaceuticals Inc | Inhibidores de serina proteasa macrociclica |
CA2770338A1 (en) | 2009-08-27 | 2011-03-03 | Merck Sharp & Dohme Corp. | Processes for preparing protease inhibitors of hepatitis c virus |
CA2775697A1 (en) * | 2009-09-28 | 2011-03-31 | 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 |
JP2013512246A (ja) | 2009-11-25 | 2013-04-11 | メルク・シャープ・アンド・ドーム・コーポレーション | ウイルス疾患治療に有用な縮合型三環式化合物およびその誘導体 |
MY159958A (en) | 2009-12-18 | 2017-02-15 | Idenix Pharmaceuticals Inc | 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 |
EP2536410B1 (en) | 2010-02-18 | 2015-09-23 | Merck Sharp & Dohme Corp. | Substituted pyrimidine derivatives and their use in treating viral infections |
MA34147B1 (fr) | 2010-03-09 | 2013-04-03 | Merck Sharp & Dohme | Composes tricycliques fusionnes de silyle et leurs methodes d'utilisation dans le cadre du traitement de maladies virales |
JP2013528217A (ja) | 2010-06-07 | 2013-07-08 | アッヴィ・インコーポレイテッド | 大環状c型肝炎セリンプロテアーゼ阻害薬 |
CA2805440A1 (en) | 2010-07-26 | 2012-02-09 | Merck Sharp & Dohme Corp. | Substituted biphenylene compounds and methods of use thereof for the treatment of viral diseases |
US9254292B2 (en) | 2010-09-29 | 2016-02-09 | Merck Sharp & Dohme Corp. | Fused tetracycle derivatives and methods of use thereof for the treatment of viral diseases |
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 |
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 |
EP2696681B1 (en) | 2011-04-13 | 2018-10-03 | Merck Sharp & Dohme Corp. | 2'-substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases |
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 |
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 |
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 |
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 |
EP2755981A4 (en) | 2011-09-14 | 2015-03-25 | Merck Sharp & Dohme | HETEROCYCLIC COMPOUNDS CONTAINING SILYL AND METHODS OF USING THE SAME FOR TREATING VIRAL DISEASES |
WO2013100132A1 (ja) | 2011-12-28 | 2013-07-04 | 中外製薬株式会社 | ペプチド化合物の環化方法 |
NZ727792A (en) * | 2013-01-09 | 2018-04-27 | Gilead Sciences Inc | Therapeutic compounds |
US20160229866A1 (en) | 2013-09-20 | 2016-08-11 | Idenix Pharmaceuticals Inc. | Hepatitis c virus inhibitors |
EP3063140A4 (en) | 2013-10-30 | 2017-11-08 | Merck Sharp & Dohme Corp. | Pseudopolymorphs of an hcv ns5a inhibitor and uses thereof |
EP3114122A1 (en) | 2014-03-05 | 2017-01-11 | 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 |
DK3269809T3 (da) | 2015-03-13 | 2022-09-12 | Chugai Pharmaceutical Co Ltd | MODIFICERET AMINOACYL-tRNA-SYNTETASE OG ANVENDELSE DERAF |
KR102610527B1 (ko) | 2017-06-09 | 2023-12-05 | 추가이 세이야쿠 가부시키가이샤 | N-치환 아미노산을 포함하는 펩타이드의 합성 방법 |
US11834515B2 (en) * | 2017-10-11 | 2023-12-05 | Cornell University | Macrocyclic compounds as proteasome inhibitors |
US11492369B2 (en) | 2017-12-15 | 2022-11-08 | Chugai Seiyaku Kabushiki Kaisha | Method for producing peptide, and method for processing bases |
US11732002B2 (en) | 2018-11-30 | 2023-08-22 | Chugai Seiyaku Kabushiki Kaisha | Deprotection method and resin removal method in solid-phase reaction for peptide compound or amide compound, and method for producing peptide compound |
Family Cites Families (18)
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 |
FI77875C (fi) * | 1982-11-26 | 1989-05-10 | Nyegaard & Co As | Foerfarande foer framstaellning av nya terapeutiskt anvaendbara peptider. |
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 |
ES2012739T5 (es) | 1987-11-18 | 2001-12-01 | Chiron Corp | Diagnosticos para nanbv. |
DE69024378T2 (de) | 1989-02-01 | 1996-09-12 | Asahi Glass Co Ltd | Azeotrope oder azeotropähnliche Zusammensetzung auf der Basis von Chlorfluorkohlenwasserstoffen |
CA2079105C (en) | 1990-04-04 | 2000-06-13 | Michael Houghton | Hepatitis c virus protease |
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 |
JP4080541B2 (ja) | 1996-10-18 | 2008-04-23 | 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 |
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 |
CZ20003798A3 (cs) * | 1998-04-15 | 2001-08-15 | Aventis Pharmaceuticals Products, Inc. | Způsob výroby cyklických peptidů vázaných k polymernímu nosiči |
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 |
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. |
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 |
-
2001
- 2001-04-17 CN CN01810566A patent/CN1432022A/zh active Pending
- 2001-04-17 CA CA002406532A patent/CA2406532A1/en not_active Abandoned
- 2001-04-17 SK SK1495-2002A patent/SK14952002A3/sk not_active Application Discontinuation
- 2001-04-17 RU RU2002131163/04A patent/RU2002131163A/ru not_active Application Discontinuation
- 2001-04-17 NZ NZ521456A patent/NZ521456A/en unknown
- 2001-04-17 KR KR1020027013965A patent/KR20020097220A/ko not_active Application Discontinuation
- 2001-04-17 CN CNA2009100067369A patent/CN101580536A/zh active Pending
- 2001-04-17 JP JP2001578418A patent/JP4748912B2/ja not_active Expired - Fee Related
- 2001-04-17 IL IL15193501A patent/IL151935A0/xx unknown
- 2001-04-17 CZ CZ20023473A patent/CZ20023473A3/cs unknown
- 2001-04-17 AU AU2001253621A patent/AU2001253621A1/en not_active Abandoned
- 2001-04-17 BR BR0110104-8A patent/BR0110104A/pt not_active IP Right Cessation
- 2001-04-17 MX MXPA02010375A patent/MXPA02010375A/es active IP Right Grant
- 2001-04-17 CN CNA2006101537103A patent/CN1935833A/zh active Pending
- 2001-04-17 PE PE2001000348A patent/PE20011288A1/es not_active Application Discontinuation
- 2001-04-17 WO PCT/US2001/012530 patent/WO2001081325A2/en active IP Right Grant
- 2001-04-17 US US09/836,636 patent/US6914122B2/en not_active Expired - Fee Related
- 2001-04-17 EP EP01927142A patent/EP1274724A2/en not_active Withdrawn
- 2001-04-17 HU HU0302957A patent/HUP0302957A2/hu unknown
- 2001-04-17 AR ARP010101794A patent/AR030558A1/es unknown
- 2001-04-17 PL PL01358591A patent/PL358591A1/xx not_active Application Discontinuation
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2002
- 2002-10-04 ZA ZA200208014A patent/ZA200208014B/en unknown
- 2002-10-18 NO NO20025030A patent/NO20025030L/no not_active Application Discontinuation
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2003
- 2003-01-18 HK HK03100478.8A patent/HK1048479A1/zh unknown
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PL358591A1 (en) | 2004-08-09 |
KR20020097220A (ko) | 2002-12-31 |
HUP0302957A2 (hu) | 2003-12-29 |
RU2002131163A (ru) | 2004-06-27 |
EP1274724A2 (en) | 2003-01-15 |
US20020016294A1 (en) | 2002-02-07 |
CN1935833A (zh) | 2007-03-28 |
BR0110104A (pt) | 2003-01-07 |
HK1048479A1 (zh) | 2003-04-04 |
CN101580536A (zh) | 2009-11-18 |
AU2001253621A1 (en) | 2001-11-07 |
CZ20023473A3 (cs) | 2003-01-15 |
US6914122B2 (en) | 2005-07-05 |
IL151935A0 (en) | 2003-04-10 |
MXPA02010375A (es) | 2003-04-25 |
JP2003531199A (ja) | 2003-10-21 |
ZA200208014B (en) | 2004-02-12 |
NO20025030L (no) | 2002-12-18 |
CA2406532A1 (en) | 2001-11-01 |
WO2001081325A2 (en) | 2001-11-01 |
NO20025030D0 (no) | 2002-10-18 |
NZ521456A (en) | 2004-07-30 |
CN1432022A (zh) | 2003-07-23 |
WO2001081325A3 (en) | 2002-08-01 |
JP4748912B2 (ja) | 2011-08-17 |
PE20011288A1 (es) | 2001-12-12 |
SK14952002A3 (sk) | 2003-03-04 |
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