CN103957908A - 作为包括肝细胞癌在内的癌症的抑制剂和作为肝炎病毒复制抑制剂的取代的氨基噻唑 - Google Patents

作为包括肝细胞癌在内的癌症的抑制剂和作为肝炎病毒复制抑制剂的取代的氨基噻唑 Download PDF

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Publication number
CN103957908A
CN103957908A CN201280059490.1A CN201280059490A CN103957908A CN 103957908 A CN103957908 A CN 103957908A CN 201280059490 A CN201280059490 A CN 201280059490A CN 103957908 A CN103957908 A CN 103957908A
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Prior art keywords
pyridin
pyrimidin
thiazol
amine
ylamino
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CN201280059490.1A
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Chinese (zh)
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A·库克纳提
X·徐
T·M·布洛克
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INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH
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INSTITUTE FOR HEPATITIS AND VIRUS RESEARCH
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • C07D417/14—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 three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/42—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • C07D417/02—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
    • C07D417/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • C07D417/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201280059490.1A 2011-10-04 2012-10-04 作为包括肝细胞癌在内的癌症的抑制剂和作为肝炎病毒复制抑制剂的取代的氨基噻唑 Pending CN103957908A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161542907P 2011-10-04 2011-10-04
US61/542,907 2011-10-04
PCT/US2012/058674 WO2013052613A1 (en) 2011-10-04 2012-10-04 Substituted aminothiazoles as inhibitors of cancers, including hepatocellular carcinoma, and as inhibitors of hepatitis virus replication

Publications (1)

Publication Number Publication Date
CN103957908A true CN103957908A (zh) 2014-07-30

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CN201280059490.1A Pending CN103957908A (zh) 2011-10-04 2012-10-04 作为包括肝细胞癌在内的癌症的抑制剂和作为肝炎病毒复制抑制剂的取代的氨基噻唑

Country Status (13)

Country Link
US (2) US20140249154A1 (https=)
EP (1) EP2763674A4 (https=)
JP (2) JP6240078B2 (https=)
KR (1) KR20140071472A (https=)
CN (1) CN103957908A (https=)
AU (1) AU2012318670B2 (https=)
BR (1) BR112014007963A2 (https=)
CA (1) CA2850779A1 (https=)
HK (1) HK1200361A1 (https=)
IL (1) IL231923A0 (https=)
PH (1) PH12014500724A1 (https=)
SG (1) SG11201401207XA (https=)
WO (1) WO2013052613A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105524056A (zh) * 2016-01-05 2016-04-27 中山大学肿瘤防治中心 一种氨基噻唑化合物及其制备方法和应用
CN109689632A (zh) * 2016-07-11 2019-04-26 巴鲁克斯布伦博格研究所 取代氨基噻唑

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Publication number Priority date Publication date Assignee Title
US9582896B2 (en) * 2011-09-02 2017-02-28 Qualcomm Incorporated Line tracking with automatic model initialization by graph matching and cycle detection
JP6329958B2 (ja) * 2012-11-07 2018-05-23 カルス セラピューティクス リミテッド 新規ヒストンデアセチラーゼインヒビターおよび治療におけるその使用
WO2014159938A1 (en) * 2013-03-13 2014-10-02 The Broad Institute, Inc. Substituted aminothiazoles for the treatment of tuberculosis
NZ714283A (en) 2013-05-10 2020-04-24 Karus Therapeutics Ltd Novel histone deacetylase inhibitors
US10442779B2 (en) 2014-09-22 2019-10-15 Fratagene Therapeutics S.R.L. Compositions and methods for treating Friedreich's ataxia
WO2016046759A2 (en) 2014-09-22 2016-03-31 Fratagene Therapeutics Ltd. Compositions and methods for treating friedreich's ataxia
GB201419264D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
GB201419228D0 (en) 2014-10-29 2014-12-10 Karus Therapeutics Ltd Compounds
MX2017013795A (es) * 2015-04-29 2018-03-21 Foresight Biotherapeutics Inc Combinaciones terapeuticas de tratamientos antivirales y antiinflamatorios.
EP3641772B1 (en) * 2017-06-22 2023-08-02 Celgene Corporation Treatment of hepatocellular carcinoma characterized by hepatitis b virus infection
US10426775B2 (en) 2017-09-11 2019-10-01 Fratagene Therapeutics Srl Methods for treating Friedreich's ataxia with etravirine
US20240025891A1 (en) * 2020-10-23 2024-01-25 Celgene Corporation Heterocyclic compounds and their use for treatment of helminthic infections and diseases
WO2025017207A1 (en) 2023-07-20 2025-01-23 Cemm - Forschungszentrum Für Molekulare Medizin Gmbh Inhibitors of smndc1 and their therapeutic use
WO2025151517A1 (en) * 2024-01-08 2025-07-17 Wavebreak Therapeutics Limited Thiazole compounds, compositions and methods of treating disorders associated with missfolding of alpha-synuclein protein

Citations (4)

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WO2003015773A2 (en) * 2001-08-13 2003-02-27 Janssen Pharmaceutica N.V. 2-amino-4,5-trisubstituted thiazolyl derivatives and their use against autoimmune diseases
WO2005099673A1 (en) * 2004-04-13 2005-10-27 Icagen, Inc. Polycylic thiazoles as potassium ion channel modulators
WO2009114552A1 (en) * 2008-03-10 2009-09-17 The Board Of Trustees Of The Leland Stanford Junior University Heteroaryl compounds, compositions, and methods of use in cancer treatment
WO2010111711A2 (en) * 2009-03-27 2010-09-30 Zacharon Pharmaceuticals, Inc. Ganglioside biosynthesis modulators

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AU2001237401B2 (en) * 2000-03-01 2006-11-09 Janssen Pharmaceutica N.V. 2,4-disubstituted thiazolyl derivatives
JP2007530696A (ja) * 2004-03-30 2007-11-01 メルク　エンド　カムパニー　インコーポレーテッド アスパラギン酸プロテアーゼ阻害剤として有用な２−アミノチアゾール化合物
NZ563866A (en) 2005-05-09 2011-03-31 Achillion Pharmaceuticals Inc Thiazole compounds and methods of use
WO2007103550A2 (en) * 2006-03-08 2007-09-13 Achillion Pharmaceuticals, Inc. Substituted aminothiazole derivatives with anti-hcv activity
WO2008083098A1 (en) * 2006-12-27 2008-07-10 The Johns Hopkins University Agents for reversing epigenetic silencing of genes

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003015773A2 (en) * 2001-08-13 2003-02-27 Janssen Pharmaceutica N.V. 2-amino-4,5-trisubstituted thiazolyl derivatives and their use against autoimmune diseases
WO2005099673A1 (en) * 2004-04-13 2005-10-27 Icagen, Inc. Polycylic thiazoles as potassium ion channel modulators
WO2009114552A1 (en) * 2008-03-10 2009-09-17 The Board Of Trustees Of The Leland Stanford Junior University Heteroaryl compounds, compositions, and methods of use in cancer treatment
WO2010111711A2 (en) * 2009-03-27 2010-09-30 Zacharon Pharmaceuticals, Inc. Ganglioside biosynthesis modulators

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105524056A (zh) * 2016-01-05 2016-04-27 中山大学肿瘤防治中心 一种氨基噻唑化合物及其制备方法和应用
CN109689632A (zh) * 2016-07-11 2019-04-26 巴鲁克斯布伦博格研究所 取代氨基噻唑

Also Published As

Publication number Publication date
US20140249154A1 (en) 2014-09-04
HK1200361A1 (en) 2015-08-07
PH12014500724A1 (en) 2014-05-19
US20170066758A1 (en) 2017-03-09
AU2012318670A1 (en) 2014-05-22
EP2763674A1 (en) 2014-08-13
EP2763674A4 (en) 2015-04-29
JP6240078B2 (ja) 2017-11-29
JP2014528450A (ja) 2014-10-27
KR20140071472A (ko) 2014-06-11
IL231923A0 (en) 2014-05-28
SG11201401207XA (en) 2014-05-29
AU2012318670B2 (en) 2017-09-07
WO2013052613A1 (en) 2013-04-11
JP2017149753A (ja) 2017-08-31
US10087173B2 (en) 2018-10-02
BR112014007963A2 (pt) 2013-04-11
CA2850779A1 (en) 2013-04-11

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