EA200900969A1 - Макроциклические ингибиторы протеазы гепатита с - Google Patents
Макроциклические ингибиторы протеазы гепатита сInfo
- Publication number
- EA200900969A1 EA200900969A1 EA200900969A EA200900969A EA200900969A1 EA 200900969 A1 EA200900969 A1 EA 200900969A1 EA 200900969 A EA200900969 A EA 200900969A EA 200900969 A EA200900969 A EA 200900969A EA 200900969 A1 EA200900969 A1 EA 200900969A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- hepatitis
- protease
- compounds
- inhibitors
- present
- Prior art date
Links
- 108091005804 Peptidases Proteins 0.000 title abstract 3
- 239000004365 Protease Substances 0.000 title abstract 3
- 102100037486 Reverse transcriptase/ribonuclease H Human genes 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 2
- 208000006454 hepatitis Diseases 0.000 title 1
- 231100000283 hepatitis Toxicity 0.000 title 1
- 208000005176 Hepatitis C Diseases 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 230000003612 virological effect Effects 0.000 abstract 2
- 241000711549 Hepacivirus C Species 0.000 abstract 1
- 239000003443 antiviral agent Substances 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 239000003814 drug Substances 0.000 abstract 1
- 208000010710 hepatitis C virus infection Diseases 0.000 abstract 1
- 150000002678 macrocyclic compounds Chemical class 0.000 abstract 1
- 230000003278 mimic effect Effects 0.000 abstract 1
- 108090000765 processed proteins & peptides Proteins 0.000 abstract 1
- 239000003001 serine protease inhibitor Substances 0.000 abstract 1
- 239000000758 substrate Substances 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 229940124597 therapeutic agent Drugs 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—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
- C07D403/08—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 carbon chain containing alicyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0827—Tripeptides containing heteroatoms different from O, S, or N
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0804—Tripeptides with the first amino acid being neutral and aliphatic
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
- C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
- C07K5/08—Tripeptides
- C07K5/0802—Tripeptides with the first amino acid being neutral
- C07K5/0812—Tripeptides with the first amino acid being neutral and aromatic or cycloaliphatic
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07K—PEPTIDES
- C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
- C07K7/50—Cyclic peptides containing at least one abnormal peptide link
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Molecular Biology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biophysics (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Virology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Gastroenterology & Hepatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
Abstract
Данное изобретение предусматривает новые макроциклические соединения, которые имитируют пептидные субстраты вирусной протеазы гепатита С и ингибируют вирусную протеазу, более конкретно, являются ингибиторами серинпротеазы NS3 из вируса гепатита С. Предусмотрены также способы синтеза этих соединений. Соединения находят применение в качестве противовирусных агентов в случае гепатита С. Кроме того, данное изобретение предусматривает способы применения таких ингибиторов в отдельности или в комбинации с другими терапевтическими агентами для лечения инфекции, вызванной вирусом гепатита С, у субъекта, нуждающегося в таком лечении.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US88394607P | 2007-01-08 | 2007-01-08 | |
PCT/US2008/050208 WO2008086161A1 (en) | 2007-01-08 | 2008-01-04 | Macrocyclic hepatitis c protease inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
EA200900969A1 true EA200900969A1 (ru) | 2010-02-26 |
Family
ID=39345472
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200900969A EA200900969A1 (ru) | 2007-01-08 | 2008-01-04 | Макроциклические ингибиторы протеазы гепатита с |
Country Status (8)
Country | Link |
---|---|
US (1) | US20100323953A1 (ru) |
EP (1) | EP2111227A1 (ru) |
KR (1) | KR20090101372A (ru) |
CN (1) | CN101668538A (ru) |
AU (1) | AU2008205116A1 (ru) |
CA (1) | CA2679563A1 (ru) |
EA (1) | EA200900969A1 (ru) |
WO (1) | WO2008086161A1 (ru) |
Families Citing this family (47)
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ES2448494T3 (es) | 2006-07-13 | 2014-03-14 | Achillion Pharmaceuticals, Inc. | Péptidos de 4-amino-4-oxobutanoilo en calidad de inhibidores de la replicación viral |
JP5439384B2 (ja) | 2007-12-21 | 2014-03-12 | エフ.ホフマン−ラ ロシュ アーゲー | 大員環の製造方法 |
KR101647520B1 (ko) * | 2008-08-07 | 2016-08-10 | 에프. 호프만-라 로슈 아게 | 거대환식 화합물의 제조 방법 |
UY32099A (es) | 2008-09-11 | 2010-04-30 | Enanta Pharm Inc | Inhibidores macrocíclicos de serina proteasas de hepatitis c |
MX2011006244A (es) | 2008-12-10 | 2011-06-27 | Achillion Pharmaceuticals Inc | Nuevos peptidos de 4-amino-4-oxobutanoilo como inhibidores de replica viral. |
CA2758072A1 (en) | 2009-04-08 | 2010-10-14 | Idenix Pharmaceuticals, Inc. | Macrocyclic serine protease inhibitors |
US8232246B2 (en) | 2009-06-30 | 2012-07-31 | Abbott Laboratories | Anti-viral compounds |
CA2769652A1 (en) | 2009-08-05 | 2011-02-10 | Idenix Pharmaceuticals, Inc. | Macrocyclic serine protease inhibitors useful against viral infections, particularly hcv |
KR20120118008A (ko) | 2009-12-18 | 2012-10-25 | 아이데닉스 파마슈티칼스, 인코포레이티드 | 5,5-융합 아릴렌 또는 헤테로아릴렌 간염 c 바이러스 억제제 |
PE20140039A1 (es) | 2010-12-30 | 2014-03-01 | Enanta Pharm Inc | Inhibidores de serina proteasa de hepatitis c a base de macrociclicos de fenantridina |
CN103534256B (zh) | 2010-12-30 | 2016-08-10 | 益安药业 | 大环丙型肝炎丝氨酸蛋白酶抑制剂 |
TW201309690A (zh) | 2011-02-10 | 2013-03-01 | Idenix Pharmaceuticals Inc | 巨環絲胺酸蛋白酶抑制劑,其醫藥組合物及其於治療hcv感染之用途 |
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 |
US8957203B2 (en) | 2011-05-05 | 2015-02-17 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
US10201584B1 (en) | 2011-05-17 | 2019-02-12 | Abbvie Inc. | Compositions and methods for treating HCV |
ES2572328B1 (es) | 2011-10-21 | 2017-08-24 | Abbvie Inc. | Combinación de al menos dos agentes antivirales de acción directa y ribavirina pero no interferón, para su uso en el tratamiento del vhc |
SE1450131A1 (sv) | 2011-10-21 | 2014-05-07 | Abbvie Inc | DAA-kombinationsbehandling (t.ex. med ABT-072 eller ABT-333)för användning vid behandling av HCV |
US8466159B2 (en) | 2011-10-21 | 2013-06-18 | Abbvie Inc. | Methods for treating HCV |
US8492386B2 (en) | 2011-10-21 | 2013-07-23 | Abbvie Inc. | Methods for treating HCV |
PT2909205T (pt) | 2012-10-19 | 2017-02-06 | Bristol Myers Squibb Co | Derivados de carbamato de hexadecahidrociclopropa(e)pirrolo(1,2- a)(1,4)diazaciclopentadecinilo substituídos com 9-metilo como inibidores da protease não estrutural 3 (ns3) para o tratamento de infeções por vírus da hepatite c |
EP2914598B1 (en) | 2012-11-02 | 2017-10-18 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
EP2914613B1 (en) | 2012-11-02 | 2017-11-22 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
US9643999B2 (en) | 2012-11-02 | 2017-05-09 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
US9409943B2 (en) | 2012-11-05 | 2016-08-09 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
EP2920182A4 (en) * | 2012-11-16 | 2016-05-11 | Adelaide Res & Innovation Pty | MACROCYCLIC COMPOUNDS AND USES THEREOF |
WO2014137869A1 (en) | 2013-03-07 | 2014-09-12 | Bristol-Myers Squibb Company | Hepatitis c virus inhibitors |
MX2015013020A (es) | 2013-03-15 | 2016-06-10 | Achillion Pharmaceuticals Inc | Polimorfos de sovaprevir y metodos de fabricacion de los mismos. |
US9006423B2 (en) | 2013-03-15 | 2015-04-14 | Achillion Pharmaceuticals Inc. | Process for making a 4-amino-4-oxobutanoyl peptide cyclic analogue, an inhibitor of viral replication, and intermediates thereof |
US9085607B2 (en) | 2013-03-15 | 2015-07-21 | Achillion Pharmaceuticals, Inc. | ACH-0142684 sodium salt polymorph, composition including the same, and method of manufacture thereof |
US20160229866A1 (en) | 2013-09-20 | 2016-08-11 | Idenix Pharmaceuticals Inc. | Hepatitis c virus inhibitors |
EP3089757A1 (en) | 2014-01-03 | 2016-11-09 | AbbVie Inc. | Solid antiviral dosage forms |
JP6466461B2 (ja) | 2014-02-03 | 2019-02-06 | ヴァイティー ファーマシューティカルズ,インコーポレイテッド | Rorガンマのジヒドロピロロピリジン阻害剤 |
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 |
JP6564029B2 (ja) | 2014-10-14 | 2019-08-21 | ヴァイティー ファーマシューティカルズ,エルエルシー | Ror−ガンマのジヒドロピロロピリジン阻害剤 |
US9845308B2 (en) | 2014-11-05 | 2017-12-19 | Vitae Pharmaceuticals, Inc. | Isoindoline inhibitors of ROR-gamma |
US9663515B2 (en) | 2014-11-05 | 2017-05-30 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
EP3331876B1 (en) | 2015-08-05 | 2020-10-07 | Vitae Pharmaceuticals, LLC | Modulators of ror-gamma |
MA53943A (fr) | 2015-11-20 | 2021-08-25 | Vitae Pharmaceuticals Llc | Modulateurs de ror-gamma |
CN105712901B (zh) * | 2016-01-22 | 2017-07-14 | 成都柏睿泰生物科技有限公司 | 一种光学活性中间体n‑叔丁氧羰基‑2‑氨基‑8‑壬烯酸二环己胺盐的合成方法 |
TW202220968A (zh) | 2016-01-29 | 2022-06-01 | 美商維它藥物有限責任公司 | ROR-γ調節劑 |
JP7129703B2 (ja) | 2016-04-28 | 2022-09-02 | エモリー ユニバーシティー | アルキン含有ヌクレオチド及びヌクレオシド治療組成物並びにそれらに関連した使用 |
EP3452492A1 (en) | 2016-05-05 | 2019-03-13 | Novartis AG | Amatoxin derivatives and conjugates thereof as inhibitors of rna polymerase |
US9481674B1 (en) | 2016-06-10 | 2016-11-01 | Vitae Pharmaceuticals, Inc. | Dihydropyrrolopyridine inhibitors of ROR-gamma |
CN107915672A (zh) * | 2016-10-09 | 2018-04-17 | 浙江九洲药物科技有限公司 | 一种取代异吲哚啉化合物的制备方法 |
WO2019018975A1 (en) | 2017-07-24 | 2019-01-31 | Vitae Pharmaceuticals, Inc. | INHIBITORS OF ROR GAMMA |
SG11202000621VA (en) | 2017-07-24 | 2020-02-27 | Vitae Pharmaceuticals Llc | Inhibitors of ror? |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
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US6608027B1 (en) * | 1999-04-06 | 2003-08-19 | Boehringer Ingelheim (Canada) Ltd | Macrocyclic peptides active against the hepatitis C virus |
CN1771050A (zh) * | 2003-02-07 | 2006-05-10 | 益安药业 | 丙型肝炎丝氨酸蛋白酶的大环抑制剂 |
DK1615613T3 (da) * | 2003-04-18 | 2010-03-22 | Enanta Pharm Inc | Quinoxalinyl-makrocykliske hepatitis C serin protease-inhibitorer |
HRP20130098T1 (hr) * | 2003-10-14 | 2013-02-28 | F. Hoffmann - La Roche Ag | MAKROCIKLIÄŚKE KARBOKSILNE KISELINE I ACILSULFONAMIDNI SPOJEVI KAO INHIBITORI REPLIKACIJE HCV-a |
JP4950026B2 (ja) * | 2004-03-30 | 2012-06-13 | インターミューン・インコーポレーテッド | ウイルス複製阻害剤としての大環状化合物 |
WO2007001406A2 (en) * | 2004-10-05 | 2007-01-04 | Chiron Corporation | Aryl-containing macrocyclic compounds |
SG166791A1 (en) * | 2005-07-25 | 2010-12-29 | 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 |
KR20080056295A (ko) * | 2005-10-11 | 2008-06-20 | 인터뮨, 인크. | C형 간염 바이러스 복제를 억제하기 위한 화합물 및 방법 |
US7772183B2 (en) * | 2005-10-12 | 2010-08-10 | Bristol-Myers Squibb Company | Hepatitis C virus inhibitors |
US7605126B2 (en) * | 2006-08-11 | 2009-10-20 | Enanta Pharmaceuticals, Inc. | Acylaminoheteroaryl hepatitis C virus protease inhibitors |
-
2008
- 2008-01-04 EA EA200900969A patent/EA200900969A1/ru unknown
- 2008-01-04 US US12/526,018 patent/US20100323953A1/en not_active Abandoned
- 2008-01-04 WO PCT/US2008/050208 patent/WO2008086161A1/en active Application Filing
- 2008-01-04 EP EP08713524A patent/EP2111227A1/en not_active Withdrawn
- 2008-01-04 CA CA002679563A patent/CA2679563A1/en not_active Abandoned
- 2008-01-04 AU AU2008205116A patent/AU2008205116A1/en not_active Abandoned
- 2008-01-04 CN CN200880007634A patent/CN101668538A/zh active Pending
- 2008-01-04 KR KR1020097016594A patent/KR20090101372A/ko not_active Withdrawn
Also Published As
Publication number | Publication date |
---|---|
AU2008205116A1 (en) | 2008-07-17 |
EP2111227A1 (en) | 2009-10-28 |
KR20090101372A (ko) | 2009-09-25 |
CN101668538A (zh) | 2010-03-10 |
WO2008086161A1 (en) | 2008-07-17 |
US20100323953A1 (en) | 2010-12-23 |
CA2679563A1 (en) | 2008-07-17 |
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