CA2156420A1 - Inhibitors of hiv reverse transcriptase - Google Patents

Inhibitors of hiv reverse transcriptase

Info

Publication number
CA2156420A1
CA2156420A1 CA002156420A CA2156420A CA2156420A1 CA 2156420 A1 CA2156420 A1 CA 2156420A1 CA 002156420 A CA002156420 A CA 002156420A CA 2156420 A CA2156420 A CA 2156420A CA 2156420 A1 CA2156420 A1 CA 2156420A1
Authority
CA
Canada
Prior art keywords
carboxamide
chloro
chloroindole
phenylsulfonyl
title compound
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA002156420A
Other languages
English (en)
French (fr)
Inventor
Theresa M. Williams
William C. Lumma Jr.
Joel R. Huff
Clarence S. Rooney
Philip E. Sanderson
Terrence M. Ciccarone
Walfred S. Saari
John S. Wai
William J. Greenlee
Suresh K. Balani
Mark E. Goldman
Anthony D. Theoharides
Jacob M. Hoffman Jr.
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
SHARON A THEOHARIDES
Merck and Co Inc
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 SHARON A THEOHARIDES, Merck and Co Inc filed Critical SHARON A THEOHARIDES
Publication of CA2156420A1 publication Critical patent/CA2156420A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • 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
    • 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
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
    • C07D417/12—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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Immunology (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)
CA002156420A 1993-02-24 1994-02-15 Inhibitors of hiv reverse transcriptase Abandoned CA2156420A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US2192593A 1993-02-24 1993-02-24
US08/021,925 1993-02-24

Publications (1)

Publication Number Publication Date
CA2156420A1 true CA2156420A1 (en) 1994-09-01

Family

ID=21806886

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002156420A Abandoned CA2156420A1 (en) 1993-02-24 1994-02-15 Inhibitors of hiv reverse transcriptase

Country Status (13)

Country Link
EP (1) EP0686148A4 (bg)
JP (1) JPH08507067A (bg)
KR (1) KR960701010A (bg)
CN (1) CN1119856A (bg)
AU (1) AU6254294A (bg)
BG (1) BG62089B1 (bg)
BR (1) BR9405737A (bg)
CA (1) CA2156420A1 (bg)
FI (1) FI953954A0 (bg)
HU (1) HUT74614A (bg)
NO (1) NO953308L (bg)
PL (1) PL175788B1 (bg)
WO (1) WO1994019321A1 (bg)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7642277B2 (en) 2002-12-04 2010-01-05 Boehringer Ingelheim International Gmbh Non-nucleoside reverse transcriptase inhibitors

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6989263B1 (en) * 1994-09-23 2006-01-24 The United States Of America As Represented By The Secretary Of The Department Of Health And Human Services Method for identifying and using compounds that inactivate HIV-1 and other retroviruses by attacking highly conserved zinc fingers in the viral nucleocapsid protein
US5811425A (en) * 1997-03-04 1998-09-22 Abbott Laboratories Heterocyclic compounds as COX-2 inhibitors
GB9902455D0 (en) * 1999-02-05 1999-03-24 Zeneca Ltd Chemical compounds
AU7962200A (en) * 1999-10-29 2001-05-14 Wakunaga Pharmaceutical Co., Ltd Novel indole derivatives and drugs containing the same as the active ingredient
EP1390029B1 (en) * 2001-04-11 2009-12-16 Idenix (Cayman) Limited Phenylindoles for the treatment of hiv
SE0201635D0 (sv) * 2002-05-30 2002-05-30 Astrazeneca Ab Novel compounds
TW200307542A (en) 2002-05-30 2003-12-16 Astrazeneca Ab Novel compounds
SE0202241D0 (sv) 2002-07-17 2002-07-17 Astrazeneca Ab Novel Compounds
US7365090B2 (en) 2002-08-07 2008-04-29 Idenix Pharmaceuticals, Inc. Substituted phenylindoles for the treatment of HIV
AU2003261415C1 (en) * 2002-08-09 2010-01-14 Merck Sharp & Dohme Corp. Tyrosine kinase inhibitors
WO2004014300A2 (en) * 2002-08-09 2004-02-19 Merck & Co., Inc. Tyrosine kinase inhibitors
SE0301569D0 (sv) 2003-05-27 2003-05-27 Astrazeneca Ab Novel compounds
SE0302232D0 (sv) 2003-08-18 2003-08-18 Astrazeneca Ab Novel Compounds
CN100439367C (zh) * 2003-12-11 2008-12-03 安万特药物公司 作为酪蛋白激酶Iε抑制剂的取代的1H-吡咯并[3,2-b、3,2-c和2,3-c]吡啶-2-甲酰胺以及相关类似物
CA2577511A1 (en) * 2004-08-19 2006-03-02 Aventis Pharmaceuticals Inc. 3-arylthioindole-2-carboxamide derivatives and analogs thereof as inhibitors of casein kinase ie
NZ554232A (en) 2004-09-17 2010-09-30 Idenix Pharmaceuticals Inc Phosphoindoles as HIV inhibitors
GB0500604D0 (en) 2005-01-13 2005-02-16 Astrazeneca Ab Novel process
CN102558021A (zh) 2006-05-26 2012-07-11 阿斯利康(瑞典)有限公司 联芳基或芳基-杂芳基取代的吲哚类化合物
EP2078029B1 (en) * 2006-09-29 2014-05-14 IDENIX Pharmaceuticals, Inc. Enantiomerically pure phosphoindole as hiv inhibitor
BRPI0908851A2 (pt) * 2008-02-22 2017-05-30 Irm Llc compostos e composições como moduladores da atividades de gpr119
CA2797281A1 (en) * 2010-05-06 2011-11-10 Merck Sharp & Dohme Corp. Aza-indole derivatives useful as modulators of faah
CN106892854B (zh) * 2015-12-21 2019-04-30 中国海洋大学 一种吲哚生物碱类化合物及其制备方法和用途
CN107151223B (zh) * 2016-03-10 2020-03-31 中国医学科学院药物研究所 一类n-烷基吲哚类化合物在制备抗流感病毒药物中的用途
CN106995400B (zh) * 2017-04-10 2019-08-06 湘潭大学 一种化合物及其盐及其合成方法
CN112375027B (zh) * 2020-12-07 2023-03-31 中国药科大学 吲哚磺酰胺类衍生物及其医药用途

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1935671C3 (de) * 1968-04-26 1975-01-09 Sumitomo Chemical Co 2-Aminomethylindole und ihre Salze
US4255442A (en) * 1977-08-29 1981-03-10 Schering Corporation 2-[(Methylsulfinyl)]-3-phenylindoles
IT1098266B (it) * 1977-08-29 1985-09-07 Scherico Ltd 2-sostituti-3-fenilindoli,procedimento per la loro preparazione e per il loro impiego come immunosoppresori
NZ222878A (en) * 1986-12-17 1991-02-26 Merck Frosst Canada Inc 3-hetero-substituted-n-benzyl-indole derivatives, and pharmaceutical compositions
CA1338012C (en) * 1987-04-27 1996-01-30 John Michael Mccall Pharmaceutically active amines
US5268389A (en) * 1989-10-16 1993-12-07 Uniroyal Chemical Company, Inc. Thiocarboxylate ester compounds compositions containing the same
ES2093090T3 (es) * 1989-12-28 1996-12-16 Upjohn Co Compuestos sustituidos diaromaticos anti-sida.
WO1993005020A1 (en) * 1991-09-06 1993-03-18 Merck & Co., Inc. Indoles as inhibitors of hiv reverse transcriptase

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7642277B2 (en) 2002-12-04 2010-01-05 Boehringer Ingelheim International Gmbh Non-nucleoside reverse transcriptase inhibitors

Also Published As

Publication number Publication date
EP0686148A4 (en) 1996-02-07
JPH08507067A (ja) 1996-07-30
KR960701010A (ko) 1996-02-24
NO953308L (no) 1995-10-24
EP0686148A1 (en) 1995-12-13
HUT74614A (en) 1997-01-28
AU6254294A (en) 1994-09-14
PL175788B1 (pl) 1999-02-26
NO953308D0 (no) 1995-08-23
BG62089B1 (bg) 1999-02-26
HU9502468D0 (en) 1995-10-30
PL310410A1 (en) 1995-12-11
CN1119856A (zh) 1996-04-03
FI953954A (fi) 1995-08-23
WO1994019321A1 (en) 1994-09-01
BG99879A (bg) 1996-02-28
FI953954A0 (fi) 1995-08-23
BR9405737A (pt) 1995-12-05

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