EA201270651A1 - Карбоксамиды пиридинон гидроксициклопентила: ингибиторы вич интегразы и области терапевтического применения - Google Patents

Карбоксамиды пиридинон гидроксициклопентила: ингибиторы вич интегразы и области терапевтического применения

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Publication number
EA201270651A1
EA201270651A1 EA201270651A EA201270651A EA201270651A1 EA 201270651 A1 EA201270651 A1 EA 201270651A1 EA 201270651 A EA201270651 A EA 201270651A EA 201270651 A EA201270651 A EA 201270651A EA 201270651 A1 EA201270651 A1 EA 201270651A1
Authority
EA
Eurasian Patent Office
Prior art keywords
hiv
aids
compounds
methods
carboxamides
Prior art date
Application number
EA201270651A
Other languages
English (en)
Inventor
Васу Наир
Морис Окелло
Абдумалик А. Нишонов
Санджайкумар Мишра
Original Assignee
Юниверсити Оф Джорджия Рисерч Фаундейшн, Инк.
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Application filed by Юниверсити Оф Джорджия Рисерч Фаундейшн, Инк. filed Critical Юниверсити Оф Джорджия Рисерч Фаундейшн, Инк.
Publication of EA201270651A1 publication Critical patent/EA201270651A1/ru

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Classifications

    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Описаны новые хиральные и ахиральные оксизамещенные циклопентильные пиридинон дикетокарбоксамиды и их производные и способы их получения. Соединения включают таутомеры, региоизомеры и геометрические изомеры. Указанные сложные карбоксамиды созданы в качестве ингибиторов ВИЧ-репликации путем ингибирования ВИЧ интегразы. Соединения являются эффективными при профилактике и лечении инфекции, вызванной ВИЧ, и при лечении СПИДа и СПИД-ассоциированного комплекса либо в виде соединений, либо в виде фармацевтически приемлемых солей с фармацевтически приемлемыми носителями, используемыми либо в отдельности, либо в сочетании с антивирусными препаратами, иммуномодуляторами, антибиотиками, вакцинами и иными терапевтическими препаратами, в частности с другими анти-ВИЧ соединениями (включающими другие анти-ВИЧ агенты, обладающие ингибирующей интегразу активностью), которые могут быть использованы для получения смесей из различных анти-ВИЧ лекарственных препаратов. Также приведено описание способов лечения СПИДа и СПИД-ассоциированных комплексов и способов лечения и профилактики инфекции, вызванной ВИЧ.
EA201270651A 2009-12-07 2010-12-07 Карбоксамиды пиридинон гидроксициклопентила: ингибиторы вич интегразы и области терапевтического применения EA201270651A1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US28367509P 2009-12-07 2009-12-07
US32042910P 2010-04-02 2010-04-02
PCT/US2010/059183 WO2011071849A2 (en) 2009-12-07 2010-12-07 Pyridinone hydroxycyclopentyl carboxamides: hiv integrase inhibitors with therapeutic applications

Publications (1)

Publication Number Publication Date
EA201270651A1 true EA201270651A1 (ru) 2013-01-30

Family

ID=44146132

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201270651A EA201270651A1 (ru) 2009-12-07 2010-12-07 Карбоксамиды пиридинон гидроксициклопентила: ингибиторы вич интегразы и области терапевтического применения

Country Status (15)

Country Link
US (1) US8703801B2 (ru)
EP (1) EP2509949B1 (ru)
JP (1) JP2013512957A (ru)
KR (1) KR20120094098A (ru)
CN (1) CN102753526B (ru)
AU (1) AU2010328325B2 (ru)
CA (1) CA2783540C (ru)
EA (1) EA201270651A1 (ru)
IL (1) IL220113A0 (ru)
MX (1) MX2012006485A (ru)
MY (1) MY172005A (ru)
NZ (1) NZ600873A (ru)
SG (1) SG181524A1 (ru)
WO (1) WO2011071849A2 (ru)
ZA (1) ZA201204147B (ru)

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EP2509949B1 (en) 2009-12-07 2014-04-23 University Of Georgia Research Foundation, Inc. Pyridinone hydroxycyclopentyl carboxamides: hiv integrase inhibitors with therapeutic applications
KR101406201B1 (ko) * 2011-10-19 2014-06-12 한국생명공학연구원 인제난 타입의 디테르펜 화합물 및 이를 포함하는 바이러스 감염 질환의 치료 또는 예방용 약학적 조성물
ES2734495T3 (es) 2011-12-22 2019-12-10 Geron Corp Análogos de guanina como sustratos de telomerasa y afectores de la longitud de los telómeros
US9650360B2 (en) 2012-03-31 2017-05-16 University Of Georgia Research Foundation, Inc. Anti-mycobacterial drugs against tuberculosis
CN103524396B (zh) * 2012-09-29 2018-05-25 中国医学科学院医药生物技术研究所 含吲哚环的二脒类衍生物及其制备方法和应用
JP6767011B2 (ja) * 2015-09-18 2020-10-14 ヤマサ醤油株式会社 抗ｄｎａウィルス活性などの生理活性を有するヌクレオシド誘導体
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BR112018014615A2 (pt) 2016-01-20 2018-12-11 The Scripps Research Institute composições de anticorpo para ror1 e métodos relacionados
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Also Published As

Publication number Publication date
EP2509949A4 (en) 2013-04-17
NZ600873A (en) 2014-08-29
MX2012006485A (es) 2012-08-23
ZA201204147B (en) 2013-02-27
US20120282218A1 (en) 2012-11-08
US8703801B2 (en) 2014-04-22
AU2010328325A1 (en) 2012-06-21
MY172005A (en) 2019-11-11
IL220113A0 (en) 2012-07-31
CA2783540C (en) 2018-04-24
SG181524A1 (en) 2012-07-30
KR20120094098A (ko) 2012-08-23
CN102753526A (zh) 2012-10-24
AU2010328325B2 (en) 2015-02-05
EP2509949A2 (en) 2012-10-17
CN102753526B (zh) 2014-11-26
CA2783540A1 (en) 2011-06-16
JP2013512957A (ja) 2013-04-18
WO2011071849A2 (en) 2011-06-16
EP2509949B1 (en) 2014-04-23
WO2011071849A3 (en) 2011-10-06

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