CN101245097A - 丝氨酸蛋白酶、特别是丙型肝炎病毒ns3-ns4蛋白酶的抑制剂 - Google Patents

丝氨酸蛋白酶、特别是丙型肝炎病毒ns3-ns4蛋白酶的抑制剂 Download PDF

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Publication number
CN101245097A
CN101245097A CNA2008100823499A CN200810082349A CN101245097A CN 101245097 A CN101245097 A CN 101245097A CN A2008100823499 A CNA2008100823499 A CN A2008100823499A CN 200810082349 A CN200810082349 A CN 200810082349A CN 101245097 A CN101245097 A CN 101245097A
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ring
compound
independently
group
cycloalkyl
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Chinese (zh)
Inventor
J·皮特里克
K·M·克特雷尔
L·J·法默
R·B·波尼
L·F·考特尼
J·H·范迪里
M·A·默科
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Vertex Pharmaceuticals Inc
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Vertex Pharmaceuticals Inc
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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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
    • 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
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    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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  • Immunology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
CNA2008100823499A 2002-04-11 2003-04-11 丝氨酸蛋白酶、特别是丙型肝炎病毒ns3-ns4蛋白酶的抑制剂 Pending CN101245097A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US37184602P 2002-04-11 2002-04-11
US60/371,846 2002-04-11

Related Parent Applications (1)

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CNB03809665XA Division CN100381440C (zh) 2002-04-11 2003-04-11 丝氨酸蛋白酶、特别是丙型肝炎病毒ns3-ns4蛋白酶的抑制剂

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CN101245097A true CN101245097A (zh) 2008-08-20

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CNA2008100823499A Pending CN101245097A (zh) 2002-04-11 2003-04-11 丝氨酸蛋白酶、特别是丙型肝炎病毒ns3-ns4蛋白酶的抑制剂
CNB03809665XA Expired - Fee Related CN100381440C (zh) 2002-04-11 2003-04-11 丝氨酸蛋白酶、特别是丙型肝炎病毒ns3-ns4蛋白酶的抑制剂

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Country Status (17)

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US (3) US7273885B2 (https=)
EP (2) EP2468744A2 (https=)
JP (3) JP2005535574A (https=)
KR (2) KR20110028665A (https=)
CN (2) CN101245097A (https=)
AU (2) AU2003223602B8 (https=)
CA (1) CA2481369C (https=)
IL (1) IL164455A0 (https=)
MX (1) MXPA04009938A (https=)
NO (2) NO20044889L (https=)
NZ (2) NZ561851A (https=)
PL (1) PL373399A1 (https=)
RU (1) RU2004133044A (https=)
SG (1) SG159385A1 (https=)
TW (1) TW200403236A (https=)
WO (1) WO2003087092A2 (https=)
ZA (1) ZA200408243B (https=)

Families Citing this family (122)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AP1019A (en) 1996-10-18 2001-10-16 Vertex Pharma Inhibitors of serinre proteases, particularly hepatitis C virus NS3 protease.
AU2001251165A1 (en) * 2000-04-03 2001-10-15 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
AU2002348414B2 (en) * 2001-10-24 2009-10-01 Vertex Pharmaceuticals Incorporated Inhibitors of serine protease, particularly hepatitis C virus NS3-NS4A protease, incorporating a fused ring system
AU2003223602B8 (en) * 2002-04-11 2010-05-27 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis C virus NS3-NS4 protease
WO2004092161A1 (en) * 2003-04-11 2004-10-28 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
EP1636208B1 (en) * 2003-04-11 2012-02-29 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
AU2011203054B2 (en) * 2003-04-11 2012-04-26 Vertex Pharmaceuticals, Incorporated Inhibitors of Serine Proteases, Particularly HCV NS3-NS4A Protease
EP1646642A2 (en) * 2003-07-18 2006-04-19 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
UY28500A1 (es) * 2003-09-05 2005-04-29 Vertex Pharma Inhibidores de proteasas de serina, en particular proteasa ns3-ns4a del vhc.
WO2005028502A1 (en) 2003-09-18 2005-03-31 Vertex Pharmaceuticals, Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
WO2005037860A2 (en) * 2003-10-10 2005-04-28 Vertex Pharmaceuticals Incoporated 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
WO2005042484A1 (en) * 2003-10-28 2005-05-12 Vertex Pharmaceuticals, Incorporated Preparation of 4,5-dialkyl-3-acyl-pyrrole-2-carboxylic acid derivatives by fischer-fink type synthesis and subsequent acylation
PL1713822T3 (pl) 2004-01-30 2010-08-31 Medivir Ab Inhibitory proteazy serynowej HCV NS-3
WO2005077969A2 (en) 2004-02-04 2005-08-25 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
US7781478B2 (en) 2004-07-14 2010-08-24 Ptc Therapeutics, Inc. Methods for treating hepatitis C
RU2007116265A (ru) * 2004-10-01 2008-11-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Ингибирование протеазы ns3-ns4a вируса hcv
AU2005319333A1 (en) 2004-12-20 2006-06-29 Codman & Shurtleff, Inc. A method and system for treating Hepatitis C
CN101163444B (zh) * 2005-04-20 2012-12-05 皇家飞利浦电子股份有限公司 患者监护系统
BRPI0610283A2 (pt) 2005-05-13 2010-10-19 Virochem Pharma Inc composto, uso do mesmo na preparação de um medicamento para o tratamento ou prevenção de uma infecção por vìrus de hepatite c, composição farmacêutica e combinação farmacêutica
AU2006276246B2 (en) * 2005-07-25 2012-09-27 Intermune, Inc. Novel macrocyclic inhibitors of hepatitis C virus replication
JO2768B1 (en) 2005-07-29 2014-03-15 تيبوتيك فارماسيوتيكالز ليمتد Large cyclic inhibitors of hepatitis C virus
RU2436787C2 (ru) 2005-07-29 2011-12-20 Тиботек Фармасьютикалз Лтд. Макроциклические ингибиторы вируса гепатита с
PE20070211A1 (es) 2005-07-29 2007-05-12 Medivir Ab Compuestos macrociclicos como inhibidores del virus de hepatitis c
CN101273042B (zh) 2005-07-29 2013-11-06 泰博特克药品有限公司 丙型肝炎病毒的大环抑制剂
PE20070343A1 (es) 2005-07-29 2007-05-12 Medivir Ab Inhibidores macrociclicos del virus de la hepatitis c
BRPI0614620A2 (pt) 2005-07-29 2011-04-12 Tibotec Pharm Ltd compostos inibidores macrocìclicos do vìrus da hepatite c, uso dos mesmos, processo para preparar os referidos compostos, combinação e composição farmacêutica
TW200745061A (en) 2005-07-29 2007-12-16 Tibotec Pharm Ltd Macrocylic inhibitors of hepatitis C virus
TWI375670B (en) 2005-07-29 2012-11-01 Tibotec Pharm Ltd Macrocylic inhibitors of hepatitis c virus
US8012939B2 (en) 2005-07-29 2011-09-06 Tibotec Pharmaceuticals Ltd. Co Macrocyclic inhibitors of hepatitis C virus
PE20070210A1 (es) 2005-07-29 2007-04-16 Tibotec Pharm Ltd Compuestos macrociclicos como inhibidores del virus de 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
AR055395A1 (es) 2005-08-26 2007-08-22 Vertex Pharma Compuestos inhibidores de la actividad de la serina proteasa ns3-ns4a del virus de la hepatitis c
US7964624B1 (en) * 2005-08-26 2011-06-21 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
ES2356776T3 (es) * 2005-10-11 2011-04-13 Intermune, Inc. Compuestos y métodos para inhibir la replicación del virus de la hepatitis.
EP2392589A3 (en) 2005-11-11 2012-06-20 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
US7705138B2 (en) 2005-11-11 2010-04-27 Vertex Pharmaceuticals Incorporated Hepatitis C virus variants
AU2007217355B2 (en) 2006-02-27 2012-06-21 Vertex Pharmaceuticals Incorporated Co-crystals comprising VX-950 and pharmaceutical compositions comprising the same
WO2007109080A2 (en) 2006-03-16 2007-09-27 Vertex Pharmaceuticals Incorporated Deuterated hepatitis c protease inhibitors
AU2007249668B2 (en) * 2006-04-11 2011-04-07 Novartis Ag HCV/HIV inhibitors and their uses
WO2007120595A2 (en) * 2006-04-11 2007-10-25 Novartis Ag Amines for the treatment of hcv
DK2032535T3 (da) * 2006-06-01 2012-11-05 Sanofi Sa Spiro-cycliske nitriler som protease-inhibitorer
RU2008152171A (ru) 2006-07-05 2010-08-10 Интермьюн, Инк. (Us) Новые ингибиторы вирусной репликации гепатита с
CA2670260A1 (en) 2006-11-15 2008-05-22 Virochem Pharma Inc. Thiophene analogues for the treatment or prevention of flavivirus infections
BRPI0718798A2 (pt) 2006-11-17 2013-12-03 Tibotec Pharm Ltd Inibidores macrocíclicos de vírus da hepatite c
WO2008106058A2 (en) * 2007-02-27 2008-09-04 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases
HRP20120330T1 (hr) * 2007-02-27 2012-05-31 Vertex Pharmaceuticals Incorporated Sukristali i farmaceutski pripravci koji ih sadrže
SG174809A1 (en) * 2007-05-03 2011-10-28 Intermune Inc Macrocyclic compounds useful as inhibitors of hepatitis c virus
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
NZ583699A (en) * 2007-08-30 2012-04-27 Vertex Pharma Co-crystals of vx-950 (telaprevir) other components and pharmaceutical compositions comprising the same
US8293705B2 (en) 2007-12-21 2012-10-23 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
RU2515318C2 (ru) 2007-12-21 2014-05-10 Авила Терапьютикс, Инк. Ингибиторы протеазы вируса гепатита с и их применение
TWI487522B (zh) 2007-12-21 2015-06-11 賽基艾維洛米斯研究股份有限公司 Ｈｃｖ蛋白酶抑制劑及其用途（一）
US8309685B2 (en) 2007-12-21 2012-11-13 Celgene Avilomics Research, Inc. HCV protease inhibitors and uses thereof
WO2009142842A2 (en) * 2008-04-15 2009-11-26 Intermune, Inc. Novel macrocyclic inhibitors of hepatitis c virus replication
US8188137B2 (en) 2008-08-15 2012-05-29 Avila Therapeutics, Inc. HCV protease inhibitors and uses thereof
KR20110075019A (ko) * 2008-10-15 2011-07-05 인터뮨, 인크. 치료용 항바이러스성 펩티드
AR074758A1 (es) 2008-12-22 2011-02-09 Gilead Sciences Inc Compuestos macrociclicos antivirales
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.
CA2763140A1 (en) 2009-05-29 2010-12-02 Schering Corporation Antiviral compounds composed of three linked aryl moieties to treat diseases such as hepatitis c
PL2477980T3 (pl) 2009-09-15 2017-02-28 Taigen Biotechnology Co., Ltd. Inhibitory proteazy hcv
CN102741270B (zh) * 2009-09-28 2015-07-22 英特穆恩公司 C型肝炎病毒复制的环肽抑制剂
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
JP2013512247A (ja) 2009-11-25 2013-04-11 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 フラビウイルス感染症の治療または予防のための５−アルキニル−チオフェン−２−カルボン酸誘導体およびそれらの使用
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
WO2011079327A1 (en) 2009-12-24 2011-06-30 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus 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
TW201141857A (en) 2010-03-24 2011-12-01 Vertex Pharma Analogues for the treatment or prevention of flavivirus infections
WO2011119858A1 (en) 2010-03-24 2011-09-29 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
CN103038237A (zh) 2010-03-24 2013-04-10 沃泰克斯药物股份有限公司 用于黄病毒感染治疗或预防的类似物
CA2794145A1 (en) 2010-03-24 2011-09-29 Vertex Pharmaceuticals Incorporated Analogues for the treatment or prevention of flavivirus infections
WO2011156545A1 (en) 2010-06-09 2011-12-15 Vertex Pharmaceuticals Incorporated Viral dynamic model for hcv combination therapy
WO2011159826A2 (en) 2010-06-15 2011-12-22 Vertex Pharmaceuticals Incorporated Hcv ns5b protease mutants
AU2011276526A1 (en) 2010-06-28 2013-01-10 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of Flavivirus infections
WO2012006070A1 (en) 2010-06-28 2012-01-12 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flavivirus infections
EP2585448A1 (en) 2010-06-28 2013-05-01 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of flavivirus infections
WO2012018534A2 (en) 2010-07-26 2012-02-09 Schering Corporation Substituted biphenylene compounds and methods of use thereof for the treatment of viral diseases
AU2011292040A1 (en) 2010-08-17 2013-03-07 Vertex Pharmaceuticals Incorporated Compounds and methods for the treatment or prevention of Flaviviridae viral infections
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
BR112013026345A2 (pt) 2011-04-13 2019-04-24 Merck Sharp & Dohe Corp. composto, composição farmacêutica, uso de um composto, e, método para tratar um paciente infectado com hcv
WO2012142075A1 (en) 2011-04-13 2012-10-18 Merck Sharp & Dohme Corp. 2'-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases
WO2013016499A1 (en) 2011-07-26 2013-01-31 Vertex Pharmaceuticals Incorporated Methods for preparation of thiophene compounds
WO2013016492A1 (en) 2011-07-26 2013-01-31 Vertex Pharmaceuticals Incorporated Thiophene compounds
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
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
US20140378416A1 (en) 2011-09-14 2014-12-25 Michael P. Dwyer Silyl-containing heterocyclic compounds and methods of use thereof for the treatment of viral diseases
WO2013072328A1 (en) 2011-11-14 2013-05-23 Sanofi Use of telaprevir and related compounds in atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases
US9012427B2 (en) 2012-03-22 2015-04-21 Alios Biopharma, Inc. Pharmaceutical combinations comprising a thionucleotide analog
WO2014053533A1 (en) 2012-10-05 2014-04-10 Sanofi Use of substituted 3-heteroaroylamino-propionic acid derivatives as pharmaceuticals for prevention/treatment of atrial fibrillation
US20150065439A1 (en) 2013-02-28 2015-03-05 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions
WO2015065817A1 (en) 2013-10-30 2015-05-07 Merck Sharp & Dohme Corp. Pseudopolymorphs of an hcv ns5a inhibitor and uses thereof
EP2899207A1 (en) 2014-01-28 2015-07-29 Amikana.Biologics New method for testing HCV protease inhibition
EP3365340B1 (en) 2015-10-19 2022-08-10 Incyte Corporation Heterocyclic compounds as immunomodulators
US20170145025A1 (en) 2015-11-19 2017-05-25 Incyte Corporation Heterocyclic compounds as immunomodulators
ES2916874T3 (es) 2015-12-17 2022-07-06 Incyte Corp Derivados de N-fenil-piridina-2-carboxamida y su uso como moduladores de la interacción proteína/proteína PD-1/PD-L1
AU2016379372A1 (en) 2015-12-22 2018-08-02 Incyte Corporation Heterocyclic compounds as immunomodulators
ES2906460T3 (es) 2016-05-06 2022-04-18 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
ES2905980T3 (es) 2016-05-26 2022-04-12 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
BR112018076534A2 (pt) 2016-06-20 2019-04-02 Incyte Corporation compostos heterocíclicos como imunomoduladores
JP7164521B2 (ja) 2016-06-21 2022-11-01 オリオン・オフサルモロジー・エルエルシー 炭素環式プロリンアミド誘導体
HUE064412T2 (hu) 2016-06-21 2024-03-28 Orion Ophthalmology LLC Heterociklusos prolinamid-származékok
MA45669A (fr) 2016-07-14 2019-05-22 Incyte Corp Composés hétérocycliques utilisés comme immunomodulateurs
ES2941716T3 (es) 2016-08-29 2023-05-25 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
ES2874756T3 (es) 2016-12-22 2021-11-05 Incyte Corp Derivados de triazolo[1,5-A]piridina como inmunomoduladores
WO2018119286A1 (en) 2016-12-22 2018-06-28 Incyte Corporation Bicyclic heteroaromatic compounds as immunomodulators
AU2017382870B2 (en) 2016-12-22 2022-03-24 Incyte Corporation Benzooxazole derivatives as immunomodulators
ES2899402T3 (es) 2016-12-22 2022-03-11 Incyte Corp Derivados de piridina como inmunomoduladores
RU2650610C1 (ru) 2017-02-28 2018-04-16 Васильевич Иващенко Александр Противовирусная композиция и способ ее применения
CR20200520A (es) 2018-03-30 2021-03-09 Incyte Corp Compuestos heterocíclicos como inmunomoduladores
WO2019217821A1 (en) 2018-05-11 2019-11-14 Incyte Corporation Tetrahydro-imidazo[4,5-c]pyridine derivatives as pd-l1 immunomodulators
WO2020247736A1 (en) * 2019-06-07 2020-12-10 University Of Massachusetts Hepatitis c virus ns3/4a protease inhibitors
EP4010342A1 (en) 2019-08-09 2022-06-15 Incyte Corporation Salts of a pd-1/pd-l1 inhibitor
WO2021067217A1 (en) 2019-09-30 2021-04-08 Incyte Corporation Pyrido[3,2-d]pyrimidine compounds as immunomodulators
BR112022009031A2 (pt) 2019-11-11 2022-10-11 Incyte Corp Sais e formas cristalinas de um inibidor de pd-1/pd-l1
US11780836B2 (en) 2020-11-06 2023-10-10 Incyte Corporation Process of preparing a PD-1/PD-L1 inhibitor
US11866434B2 (en) 2020-11-06 2024-01-09 Incyte Corporation Process for making a PD-1/PD-L1 inhibitor and salts and crystalline forms thereof
WO2022099075A1 (en) 2020-11-06 2022-05-12 Incyte Corporation Crystalline form of a pd-1/pd-l1 inhibitor

Family Cites Families (45)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5807876A (en) 1996-04-23 1998-09-15 Vertex Pharmaceuticals Incorporated Inhibitors of IMPDH enzyme
US5990276A (en) 1996-05-10 1999-11-23 Schering Corporation Synthetic inhibitors of hepatitis C virus NS3 protease
EP0907659A1 (en) 1996-05-10 1999-04-14 Schering Corporation Synthetic inhibitors of hepatitis c virus ns3 protease
AP1019A (en) 1996-10-18 2001-10-16 Vertex Pharma Inhibitors of serinre proteases, particularly hepatitis C virus NS3 protease.
GB9623908D0 (en) 1996-11-18 1997-01-08 Hoffmann La Roche Amino acid derivatives
GB9707659D0 (en) 1997-04-16 1997-06-04 Peptide Therapeutics Ltd Hepatitis C NS3 Protease inhibitors
EP1012180B1 (en) 1997-08-11 2004-12-01 Boehringer Ingelheim (Canada) Ltd. Hepatitis c inhibitor peptide analogues
ES2241157T3 (es) 1997-08-11 2005-10-16 Boehringer Ingelheim (Canada) Ltd. Peptidos inhibidores de la hepatitis c.
US6211338B1 (en) * 1997-11-28 2001-04-03 Schering Corporation Single-chain recombinant complexes of hepatitis C virus NS3 protease and NS4A cofactor peptide
US6075150A (en) * 1998-01-26 2000-06-13 Cv Therapeutics, Inc. α-ketoamide inhibitors of 20S proteasome
IT1299134B1 (it) 1998-02-02 2000-02-29 Angeletti P Ist Richerche Bio Procedimento per la produzione di peptidi con proprieta' inibitrici della proteasi ns3 del virus hcv, peptidi cosi' ottenibili e peptidi
DK1066247T3 (da) 1998-03-31 2007-04-02 Vertex Pharma Inhibitorer af serinproteaser, især hepatitis C virus NS3 protease
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
DE19836514A1 (de) 1998-08-12 2000-02-17 Univ Stuttgart Modifikation von Engineeringpolymeren mit N-basischen Gruppe und mit Ionenaustauschergruppen in der Seitenkette
GB9825946D0 (en) 1998-11-26 1999-01-20 Angeletti P Ist Richerche Bio Pharmaceutical compounds for the inhibition of hepatitis C virus NS3 protease
UA74546C2 (en) 1999-04-06 2006-01-16 Boehringer Ingelheim Ca Ltd Macrocyclic peptides having activity relative to hepatitis c virus, a pharmaceutical composition and use of the pharmaceutical composition
US7122627B2 (en) * 1999-07-26 2006-10-17 Bristol-Myers Squibb Company Lactam inhibitors of Hepatitis C virus NS3 protease
WO2001007407A1 (en) 1999-07-26 2001-02-01 Bristol-Myers Squibb Pharma Company Lactam inhibitors of hepatitis c virus ns3 protease
AU7077400A (en) * 1999-08-31 2001-03-26 Basf Aktiengesellschaft Method of identifying inhibitors of cdc25
US6774212B2 (en) * 1999-12-03 2004-08-10 Bristol-Myers Squibb Pharma Company Alpha-ketoamide inhibitors of hepatitis C virus NS3 protease
EP1261611A2 (en) 2000-02-29 2002-12-04 Bristol-Myers Squibb Pharma Company Inhibitors of hepatitis c virus ns3 protease
AU2001251165A1 (en) * 2000-04-03 2001-10-15 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis c virus ns3 protease
ES2317900T3 (es) 2000-04-05 2009-05-01 Schering Corporation Inhibidores de serina proteasa ns3 macrociclicos del virus de la hepatitis c que comprenden fragmentos n-ciclicas p2.
AU2001253621A1 (en) 2000-04-19 2001-11-07 Schering Corporation Macrocyclic NS3-serine protease inhibitors of hepatitis C virus comprising alkyl and aryl alanine P2 moieties
AR034127A1 (es) * 2000-07-21 2004-02-04 Schering Corp Imidazolidinonas como inhibidores de ns3-serina proteasa del virus de hepatitis c, composicion farmaceutica, un metodo para su preparacion, y el uso de las mismas para la manufactura de un medicamento
WO2002008251A2 (en) 2000-07-21 2002-01-31 Corvas International, Inc. Peptides as ns3-serine protease inhibitors of hepatitis c virus
CN1498224A (zh) * 2000-07-21 2004-05-19 ���鹫˾ 用作丙型肝炎病毒ns3-丝氨酸蛋白酶抑制剂的新型肽
SK742003A3 (en) 2000-07-21 2003-06-03 Schering Corp Novel peptides as NS3-serine protease inhibitors of hepatitis C virus
AR029851A1 (es) 2000-07-21 2003-07-16 Dendreon Corp Nuevos peptidos como inhibidores de ns3-serina proteasa del virus de hepatitis c
SV2003000617A (es) * 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
WO2002022828A1 (en) * 2000-09-12 2002-03-21 Degussa Ag Isolation and sequencing of the pknb gene of c. glutamicum
US6846806B2 (en) * 2000-10-23 2005-01-25 Bristol-Myers Squibb Company Peptide inhibitors of Hepatitis C virus NS3 protein
ES2263687T3 (es) 2000-11-20 2006-12-16 Bristol-Myers Squibb Company Inhibidores tripeptidicos de la hepatitis c.
WO2002048116A2 (en) 2000-12-13 2002-06-20 Bristol-Myers Squibb Pharma Company Inhibitors of hepatitis c virus ns3 protease
WO2002048157A2 (en) 2000-12-13 2002-06-20 Bristol-Myers Squibb Pharma Company Imidazolidinones and their related derivatives as hepatitis c virus ns3 protease inhibitors
GB0107924D0 (en) 2001-03-29 2001-05-23 Angeletti P Ist Richerche Bio Inhibitor of hepatitis C virus NS3 protease
IL159087A0 (en) * 2001-07-11 2004-05-12 Vertex Pharma Bridged bicyclic compounds and pharmaceutical compositions containing the same
AU2002348414B2 (en) * 2001-10-24 2009-10-01 Vertex Pharmaceuticals Incorporated Inhibitors of serine protease, particularly hepatitis C virus NS3-NS4A protease, incorporating a fused ring system
AU2003223602B8 (en) * 2002-04-11 2010-05-27 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hepatitis C virus NS3-NS4 protease
WO2004092161A1 (en) * 2003-04-11 2004-10-28 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
EP1636208B1 (en) * 2003-04-11 2012-02-29 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
EP1646642A2 (en) * 2003-07-18 2006-04-19 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease
WO2005077969A2 (en) * 2004-02-04 2005-08-25 Vertex Pharmaceuticals Incorporated Inhibitors of serine proteases, particularly hcv ns3-ns4a protease

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