CN103930404B - 用于抗疟疾治疗方法的取代的2-烷基-1-氧代-n-苯基-3-杂芳基-1,2,3,4-四氢异喹啉-4-酰胺 - Google Patents

用于抗疟疾治疗方法的取代的2-烷基-1-氧代-n-苯基-3-杂芳基-1,2,3,4-四氢异喹啉-4-酰胺 Download PDF

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Publication number
CN103930404B
CN103930404B CN201280041436.4A CN201280041436A CN103930404B CN 103930404 B CN103930404 B CN 103930404B CN 201280041436 A CN201280041436 A CN 201280041436A CN 103930404 B CN103930404 B CN 103930404B
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oxo
amide
tetrahydroisoquinoline
base
phenyl
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CN201280041436.4A
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Chinese (zh)
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CN103930404A (zh
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R·K·盖
F·朱
W·A·吉古伊姆德
D·佛洛德
S·耐普
P·斯坦因
S·卡斯特罗
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MMV Medicines for Malaria Venture
St Jude Childrens Research Hospital
Rutgers State University of New Jersey
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MMV Medicines for Malaria Venture
St Jude Childrens Research Hospital
Rutgers State University of New Jersey
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
    • C07D417/04—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
    • 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)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201280041436.4A 2011-08-25 2012-08-24 用于抗疟疾治疗方法的取代的2-烷基-1-氧代-n-苯基-3-杂芳基-1,2,3,4-四氢异喹啉-4-酰胺 Active CN103930404B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161527594P 2011-08-25 2011-08-25
US61/527,594 2011-08-25
PCT/IB2012/054305 WO2013027196A1 (en) 2011-08-25 2012-08-24 Substituted 2-alkyl-1-oxo-n-phenyl-3-heteroaryl-1,2,3,4- tetrahydroisoquinoline-4-carboxamides for antimalarial therapies

Publications (2)

Publication Number Publication Date
CN103930404A CN103930404A (zh) 2014-07-16
CN103930404B true CN103930404B (zh) 2016-08-24

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US (1) US9416124B2 (enExample)
EP (1) EP2748147B1 (enExample)
JP (1) JP6035334B2 (enExample)
CN (1) CN103930404B (enExample)
BR (1) BR112014004437B1 (enExample)
CA (1) CA2846507C (enExample)
CY (1) CY1119748T1 (enExample)
DK (1) DK2748147T3 (enExample)
ES (1) ES2644082T3 (enExample)
HR (1) HRP20171567T1 (enExample)
HU (1) HUE034721T2 (enExample)
LT (1) LT2748147T (enExample)
ME (1) ME02908B (enExample)
PL (1) PL2748147T3 (enExample)
PT (1) PT2748147T (enExample)
RS (1) RS56544B1 (enExample)
SI (1) SI2748147T1 (enExample)
SM (1) SMT201700528T1 (enExample)
WO (1) WO2013027196A1 (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111886225A (zh) * 2017-08-21 2020-11-03 纳维根公司 Arf6抑制剂及相关方法
EP3892332A1 (en) 2020-04-09 2021-10-13 University Of Kentucky Research Foundation New anti-malarial agents
CA3214899A1 (en) 2021-04-15 2022-10-20 Lutz Weber Isoquinoline derivatives for use as antiviral and antitumour agents
EP4074314A1 (en) 2021-04-15 2022-10-19 Valdospan GmbH Isoquinoline derivatives for use as antiviral and antitumour agents
AU2023363824A1 (en) 2022-10-17 2025-04-17 Rdp Pharma Ag Isoquinoline derivatives as protein degraders, e7 degraders, antivirals, tumor therapeutics and immune suppressives

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995021616A1 (en) * 1994-02-14 1995-08-17 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Naphthylisoquinoline alkaloids, pharmaceutical compositions containing them and their use for the treatment of malaria
WO2003044021A2 (en) * 2001-11-16 2003-05-30 Amgen Inc. Substituted indolizine-like compounds and methods of use
WO2004004727A1 (en) * 2002-07-03 2004-01-15 Axys Pharmaceuticals, Inc. 3,4-dihydroisoquinolin-1-one derivatives as inducers of apoptosis
CN1314683C (zh) * 2002-08-17 2007-05-09 塞诺菲-安万特德国有限公司 用于调节IkB激酶的吲哚或苯并咪唑衍生物
WO2007105989A2 (en) * 2006-03-14 2007-09-20 Ivashchenko, Andrey Alexandrovich 1-oxo-3-(1h-indole)-3-il-1,2,3,4-tetrahydroisoxynolines, methods for the production thereof, combinatoric library and focused library
CN100364978C (zh) * 2003-03-24 2008-01-30 塞诺菲-安万特德国有限公司 取代的4-苯基四氢异喹啉、其制备方法、其制备药物的用途和含有这类化合物的药物
CN101258148A (zh) * 2005-03-25 2008-09-03 葛兰素集团有限公司 8-苯基-7,8-二氢吡啶并[2,3-d]嘧啶-7-酮及其作为药物的用途
WO2010055164A2 (en) * 2008-11-14 2010-05-20 Katholieke Universiteit Leuven, K.U.Leuven R&D Novel inhibitors of flavivirus replication

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5409938A (en) * 1994-02-14 1995-04-25 The United States Of America As Represented By The Secretary, Department Of Health And Human Services Antimalarial korupensamines and pharmaceutical compositions and medical uses thereof
BRPI0912871A2 (pt) * 2008-05-19 2015-10-20 Actelion Pharmaceuticals Ltd novas tetraidroisoquinolinas como agentes antimaláricos.

Patent Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995021616A1 (en) * 1994-02-14 1995-08-17 The United States Of America, Represented By The Secretary, Department Of Health And Human Services Naphthylisoquinoline alkaloids, pharmaceutical compositions containing them and their use for the treatment of malaria
WO2003044021A2 (en) * 2001-11-16 2003-05-30 Amgen Inc. Substituted indolizine-like compounds and methods of use
WO2004004727A1 (en) * 2002-07-03 2004-01-15 Axys Pharmaceuticals, Inc. 3,4-dihydroisoquinolin-1-one derivatives as inducers of apoptosis
CN1314683C (zh) * 2002-08-17 2007-05-09 塞诺菲-安万特德国有限公司 用于调节IkB激酶的吲哚或苯并咪唑衍生物
CN100364978C (zh) * 2003-03-24 2008-01-30 塞诺菲-安万特德国有限公司 取代的4-苯基四氢异喹啉、其制备方法、其制备药物的用途和含有这类化合物的药物
CN101258148A (zh) * 2005-03-25 2008-09-03 葛兰素集团有限公司 8-苯基-7,8-二氢吡啶并[2,3-d]嘧啶-7-酮及其作为药物的用途
WO2007105989A2 (en) * 2006-03-14 2007-09-20 Ivashchenko, Andrey Alexandrovich 1-oxo-3-(1h-indole)-3-il-1,2,3,4-tetrahydroisoxynolines, methods for the production thereof, combinatoric library and focused library
WO2010055164A2 (en) * 2008-11-14 2010-05-20 Katholieke Universiteit Leuven, K.U.Leuven R&D Novel inhibitors of flavivirus replication

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
Chemical genetics of Plasmodium falciparum;W. Armand Guiguemde,等;《Nature》;20100520;第465卷(第7296期);第312页图1 *
W. Armand Guiguemde,等.Chemical genetics of Plasmodium falciparum.《Nature》.2010,第465卷(第7296期), *

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BR112014004437A8 (pt) 2018-01-23
CN103930404A (zh) 2014-07-16
BR112014004437B1 (pt) 2021-12-14
ME02908B (me) 2018-10-20
RS56544B1 (sr) 2018-02-28
US20140235593A1 (en) 2014-08-21
BR112014004437A2 (pt) 2017-03-28
HUE034721T2 (hu) 2018-02-28
SMT201700528T1 (it) 2018-01-11
DK2748147T3 (da) 2017-11-13
EP2748147B1 (en) 2017-08-02
EP2748147A1 (en) 2014-07-02
ES2644082T3 (es) 2017-11-27
PT2748147T (pt) 2017-11-14
US9416124B2 (en) 2016-08-16
WO2013027196A9 (en) 2013-04-18
JP6035334B2 (ja) 2016-11-30
WO2013027196A1 (en) 2013-02-28
LT2748147T (lt) 2017-10-25
JP2014524464A (ja) 2014-09-22
PL2748147T3 (pl) 2018-01-31
HK1199443A1 (en) 2015-07-03
CA2846507A1 (en) 2013-02-28
CA2846507C (en) 2020-03-10
CY1119748T1 (el) 2018-06-27
HRP20171567T1 (hr) 2017-11-17
SI2748147T1 (sl) 2017-11-30

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