ECSP014109A - Derivados de pirrol - Google Patents

Derivados de pirrol

Info

Publication number
ECSP014109A
ECSP014109A EC2001004109A ECSP014109A ECSP014109A EC SP014109 A ECSP014109 A EC SP014109A EC 2001004109 A EC2001004109 A EC 2001004109A EC SP014109 A ECSP014109 A EC SP014109A EC SP014109 A ECSP014109 A EC SP014109A
Authority
EC
Ecuador
Prior art keywords
alkyl
aryl
hydrogen
heterocyclic
cycloalkyl
Prior art date
Application number
EC2001004109A
Other languages
English (en)
Inventor
Philip Stephen Jones
Brian William Dymock
John Herbert Merrett
Martin John Parratt
Original Assignee
Hoffmann La Roche
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.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of ECSP014109A publication Critical patent/ECSP014109A/es

Links

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
    • C07D401/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
    • C07D207/36—Oxygen or sulfur atoms
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D409/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms

Landscapes

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

Abstract

La invención se refiere a nuevos derivados de pirrol, un proceso para su fabricación, composiciones farmacéuticas y el uso de tales compuestos en medicina. En particular, los compuestos de fórmula 1 son inhibidores del enzima transcriptasa inversa del virus de la inmunodeficiencia humana, que está implicado en la replicación vírica. En concecuencia , los compuestos de esta invención pueden utilizarse ventajosamente como agentes terapéuticos para el proceso mediado por el VIH. (Gráfico) en donde R1 es alquilo, cicloalquilo, arilo o heterociclico; R2 es alquilo, cicloalquilo, arilo o heterociclico; R3 es hidrógeno, alquilo cicloalquilo, arilo o heterociclico; R4, es hidrógeno, alquilo, carboxilo, C(==)R, CONR´R, ciano o laquenilo, en donde R es hidrógeno, alquilo, alcoxilo, trifluorometilo, metil-oxi-carbonilo o etil-oxi-carbonilo, y en donde R5 es alquilo, arilo o un grupo -Z-C(=O)R... donde 7 es un enlace sencillo o -CH=CH-, y en donde R´´ es hidrógeno o alquilo; X representa S. S(O), S(O)2, 0, N(alquilo) ó X-R2 en conjunto representan CH2-arilo ó CH2-heterociclico; y con la condición de que solamente uno de R3 y R4 es hidrógeno y el alquilo en R3 no es CF3; y ésteres o éteres hidrolizables de los mismos o una sal farmacéuticamente aceptable de los mismos
EC2001004109A 2000-07-04 2001-07-04 Derivados de pirrol ECSP014109A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0016453.3A GB0016453D0 (en) 2000-07-04 2000-07-04 Pyrrole derivatives

Publications (1)

Publication Number Publication Date
ECSP014109A true ECSP014109A (es) 2002-02-25

Family

ID=9895031

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2001004109A ECSP014109A (es) 2000-07-04 2001-07-04 Derivados de pirrol

Country Status (17)

Country Link
US (1) US6737429B2 (es)
EP (1) EP1301481A1 (es)
JP (1) JP2004502674A (es)
KR (1) KR100549884B1 (es)
CN (1) CN1440385A (es)
AR (1) AR028602A1 (es)
AU (2) AU2001263874B2 (es)
BR (1) BR0112241A (es)
CA (1) CA2412270A1 (es)
EC (1) ECSP014109A (es)
GB (1) GB0016453D0 (es)
GT (1) GT200100111A (es)
MX (1) MXPA02012409A (es)
PA (1) PA8516201A1 (es)
PE (1) PE20020269A1 (es)
UY (1) UY26720A1 (es)
WO (1) WO2002002524A1 (es)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1405849A1 (en) * 2002-10-04 2004-04-07 Corning Incorporated Halogenated styrene compounds and low-absorption-loss polymers obtainable therefrom
WO2005063293A1 (ja) * 2003-12-26 2005-07-14 Masatoshi Hagiwara Sr蛋白質のリン酸化制御方法、および、sr蛋白質の活性制御剤を有効成分とする抗ウイルス剤
US8048909B2 (en) 2004-09-30 2011-11-01 Takeda Pharmaceutical Company Limited Proton pump inhibitors
TW200628446A (en) * 2004-12-14 2006-08-16 Takeda Pharmaceuticals Co Substituted pyrrole derivative
US20080176919A1 (en) * 2005-01-06 2008-07-24 Pfizer Inc Imidazole Derivatives As Enzyme Reverse Transcriptase Modulators
ES2391757T3 (es) 2005-08-30 2012-11-29 Akeda Pharmaceutical Company Limited Derivados de 1-H-pirrol sustituidos con 1-heterociclilsulfonilo, 2-aminometilo, 5-heteroarilo como inhibidores de la secreción de ácido
EP2076492A4 (en) * 2006-10-06 2010-12-22 Merck Sharp & Dohme NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
CA2669675A1 (en) * 2006-11-10 2008-05-15 Syndax Pharmaceuticals, Inc. Combination of er.alpha.+ ligands and histone deacetylase inhibitors for the treatment of cancer
US8933105B2 (en) 2007-02-28 2015-01-13 Takeda Pharmaceutical Company Limited Pyrrole compounds
WO2009015180A2 (en) * 2007-07-23 2009-01-29 Syndax Pharmaceuticals, Inc. Novel compounds and methods of using them
EP2179329A1 (en) * 2007-10-16 2010-04-28 Nikon Corporation Illumination optical system, exposure apparatus, and device manufacturing method
US20090131367A1 (en) * 2007-11-19 2009-05-21 The Regents Of The University Of Colorado Combinations of HDAC Inhibitors and Proteasome Inhibitors
JO2871B1 (en) 2008-08-27 2015-03-15 تاكيدا فارماسوتيكال كمبني ليمتد Perol compounds
GB0823001D0 (en) * 2008-12-17 2009-01-28 Syngenta Participations Ag Thiophene,furan and pyrrole derivatives with plant growth regulating properties
CN101775011B (zh) * 2009-01-13 2013-07-31 中国人民解放军军事医学科学院毒物药物研究所 N-取代苯基-3-甲烯杂环芳烃-2,5-二甲基吡咯类化合物及其抗hiv/aids的应用
AU2020388636A1 (en) * 2019-11-19 2022-05-26 New York Blood Center, Inc. Substituted heterocyclics with therapeutic activity in HIV

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3644631A (en) * 1969-05-13 1972-02-22 Endo Lab Therapeutic methods utilizing aryl pyrrol-3-yl ketones
US4282242A (en) * 1980-03-07 1981-08-04 Pfizer Inc. Antidiabetic pyrrolecarboxylic acids
US4347186A (en) * 1980-10-20 1982-08-31 Syntex (U.S.A.) Inc. Process for preparing 5-aroyl 1,2-dihydro-3-H pyrrolo[1,2-a]pyrrole-1-carboxylic acids and novel intermediates therein
ES2139676T3 (es) * 1992-12-17 2000-02-16 Pfizer Pirazoles sustituidos como antagonistas del crf.
EP0764153A1 (en) * 1994-06-06 1997-03-26 Pfizer Inc. Substituted pyrazoles having corticotropin-releasing factor (crf) antagonist activity
TW406075B (en) * 1994-12-13 2000-09-21 Upjohn Co Alkyl substituted piperidinyl and piperazinyl anti-AIDS compounds
CA2260213C (en) * 1996-07-11 2005-03-29 Pfizer Inc. Pyridylpyrrole compounds useful as interleukin- and tnf antagonists
DE19963174A1 (de) * 1999-12-27 2001-07-12 Gruenenthal Gmbh Substituierte Pyrrol-Mannichbasen

Also Published As

Publication number Publication date
US6737429B2 (en) 2004-05-18
BR0112241A (pt) 2003-06-24
MXPA02012409A (es) 2003-04-25
AU6387401A (en) 2002-01-14
CA2412270A1 (en) 2002-01-10
GB0016453D0 (en) 2000-08-23
EP1301481A1 (en) 2003-04-16
PE20020269A1 (es) 2002-04-08
JP2004502674A (ja) 2004-01-29
CN1440385A (zh) 2003-09-03
KR20030014321A (ko) 2003-02-15
WO2002002524A1 (en) 2002-01-10
US20020032221A1 (en) 2002-03-14
AU2001263874B2 (en) 2006-10-19
GT200100111A (es) 2002-03-18
AR028602A1 (es) 2003-05-14
UY26720A1 (es) 2001-11-30
PA8516201A1 (es) 2002-07-30
KR100549884B1 (ko) 2006-02-06

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