EP0686148A4 - Inhibitors of hiv reverse transcriptase - Google Patents

Inhibitors of hiv reverse transcriptase

Info

Publication number
EP0686148A4
EP0686148A4 EP94909663A EP94909663A EP0686148A4 EP 0686148 A4 EP0686148 A4 EP 0686148A4 EP 94909663 A EP94909663 A EP 94909663A EP 94909663 A EP94909663 A EP 94909663A EP 0686148 A4 EP0686148 A4 EP 0686148A4
Authority
EP
European Patent Office
Prior art keywords
inhibitors
reverse transcriptase
hiv reverse
hiv
transcriptase
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.)
Withdrawn
Application number
EP94909663A
Other languages
German (de)
French (fr)
Other versions
EP0686148A1 (en
Inventor
Theresa M Williams
Terrence M Ciccarone
Walfred S Saari
John S Wai
William J Greenlee
Suresh K Balani
Mark E Goldman
Jacob M Hoffman Jr
William C Lumma Jr
Joel R Huff
Clarence S Rooney
Philip E Sanderson
Anthony D Theoharides
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.)
Merck and Co Inc
Original Assignee
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 Merck and Co Inc filed Critical Merck and Co Inc
Publication of EP0686148A1 publication Critical patent/EP0686148A1/en
Publication of EP0686148A4 publication Critical patent/EP0686148A4/en
Withdrawn legal-status Critical Current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)
  • Pharmacology & Pharmacy (AREA)
  • Immunology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Indole Compounds (AREA)
EP94909663A 1993-02-24 1994-02-15 Inhibitors of hiv reverse transcriptase Withdrawn EP0686148A4 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US2192593A 1993-02-24 1993-02-24
US21925 1993-02-24
PCT/US1994/001694 WO1994019321A1 (en) 1993-02-24 1994-02-15 Inhibitors of hiv reverse transcriptase

Publications (2)

Publication Number Publication Date
EP0686148A1 EP0686148A1 (en) 1995-12-13
EP0686148A4 true EP0686148A4 (en) 1996-02-07

Family

ID=21806886

Family Applications (1)

Application Number Title Priority Date Filing Date
EP94909663A Withdrawn EP0686148A4 (en) 1993-02-24 1994-02-15 Inhibitors of hiv reverse transcriptase

Country Status (13)

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

Families Citing this family (26)

* 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
WO2002083126A1 (en) * 2001-04-11 2002-10-24 Idenix (Cayman) Limited Phenylindoles for the treatment of hiv
SE0201635D0 (en) * 2002-05-30 2002-05-30 Astrazeneca Ab Novel compounds
TW200307542A (en) 2002-05-30 2003-12-16 Astrazeneca Ab Novel compounds
SE0202241D0 (en) 2002-07-17 2002-07-17 Astrazeneca Ab Novel Compounds
WO2004014364A1 (en) * 2002-08-07 2004-02-19 Idenix (Cayman) Limited Substituted phenylindoles for the treatment of hiv
DE60334386D1 (en) * 2002-08-09 2010-11-11 Merck Sharp & Dohme tyrosine kinase inhibitors
CA2493575A1 (en) * 2002-08-09 2004-02-19 Christopher J. Dinsmore Tyrosine kinase inhibitors
US7642277B2 (en) 2002-12-04 2010-01-05 Boehringer Ingelheim International Gmbh Non-nucleoside reverse transcriptase inhibitors
SE0301569D0 (en) 2003-05-27 2003-05-27 Astrazeneca Ab Novel compounds
SE0302232D0 (en) 2003-08-18 2003-08-18 Astrazeneca Ab Novel Compounds
DK1747220T3 (en) * 2003-12-11 2009-08-10 Aventis Pharma Inc Substituted 1H-pyrrolo [3,2-B, 3,2-C and 2,3-C] pyridine-2-carboxamides and related analogues as inhibitors of casein kinase I epsilon
ES2334927T3 (en) * 2004-08-19 2010-03-17 Aventis Pharmaceuticals Inc. DERIVATIVES OF 3-ARILTIOINDOL-2-CARBOXAMIDE AND ITS ANALOGS AS IMHIBITORS OF CASEINA QUINASA I.
AU2005305609B2 (en) 2004-09-17 2011-10-06 Idenix Pharmaceuticals, Inc. Phosphoindoles as HIV inhibitors
GB0500604D0 (en) 2005-01-13 2005-02-16 Astrazeneca Ab Novel process
EP2125722A2 (en) 2006-05-26 2009-12-02 AstraZeneca AB Bi-aryl or aryl-heteroaryl substituted indoles
NZ575831A (en) * 2006-09-29 2011-12-22 Idenix Pharmaceuticals Inc Enantiomerically pure phosphoindoles as hiv inhibitors
US20110172244A1 (en) * 2008-02-22 2011-07-14 Irm Llc Compounds and compositions as modulators of gpr119 activity
EP2566481A4 (en) * 2010-05-06 2014-01-22 Merck Sharp & Dohme Aza-indole derivatives useful as modulators of faah
CN106892854B (en) * 2015-12-21 2019-04-30 中国海洋大学 A kind of indole alkaloids compound and its preparation method and application
CN107151223B (en) * 2016-03-10 2020-03-31 中国医学科学院药物研究所 Application of N-alkyl indole compounds in preparation of anti-influenza virus drugs
CN106995400B (en) * 2017-04-10 2019-08-06 湘潭大学 A kind of compound and its salt and its synthetic method
CN112375027B (en) * 2020-12-07 2023-03-31 中国药科大学 Indolesulfonamide derivative and medical application thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0530907A1 (en) * 1991-09-06 1993-03-10 Merck & Co. Inc. Indoles as inhibitors of HIV reverse transcriptase

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1935671C3 (en) * 1968-04-26 1975-01-09 Sumitomo Chemical Co 2-aminomethylindoles and their salts
US4255442A (en) * 1977-08-29 1981-03-10 Schering Corporation 2-[(Methylsulfinyl)]-3-phenylindoles
IT1098266B (en) * 1977-08-29 1985-09-07 Scherico Ltd 2-SUBSTITUTES-3-PHENYLINDOLS, PROCEDURE FOR THEIR PREPARATION AND FOR THEIR USE AS IMMUNOSOPPRESSION
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
AU654808B2 (en) * 1989-12-28 1994-11-24 Pharmacia & Upjohn Company Diaromatic substituted anti-aids compounds

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0530907A1 (en) * 1991-09-06 1993-03-10 Merck & Co. Inc. Indoles as inhibitors of HIV reverse transcriptase

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
See also references of WO9419321A1 *
THERESA M. WILLIAMS ET AL.: "5-Chloro-3-(phenylsulfonyl)indole-2-carboxamide: a novel, non-nucleoside inhibitor of HIV-1 reverse transcriptase", JOURNAL OF MEDICINAL CHEMISTRY, vol. 36, no. 9, 30 April 1993 (1993-04-30), WASHINGTON US, pages 1291 - 1294 *

Also Published As

Publication number Publication date
BG99879A (en) 1996-02-28
CN1119856A (en) 1996-04-03
PL175788B1 (en) 1999-02-26
KR960701010A (en) 1996-02-24
FI953954A (en) 1995-08-23
WO1994019321A1 (en) 1994-09-01
FI953954A0 (en) 1995-08-23
JPH08507067A (en) 1996-07-30
HUT74614A (en) 1997-01-28
NO953308D0 (en) 1995-08-23
BG62089B1 (en) 1999-02-26
NO953308L (en) 1995-10-24
CA2156420A1 (en) 1994-09-01
BR9405737A (en) 1995-12-05
PL310410A1 (en) 1995-12-11
AU6254294A (en) 1994-09-14
EP0686148A1 (en) 1995-12-13
HU9502468D0 (en) 1995-10-30

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Inventor name: HOFFMAN, JACOB, M., JR.

Inventor name: GOLDMAN, MARK, E.

Inventor name: BALANI, SURESH, K.

Inventor name: GREENLEE, WILLIAM, J.

Inventor name: WAI, JOHN, S.

Inventor name: SAARI, WALFRED, S.

Inventor name: CICCARONE, TERRENCE, M.

Inventor name: WILLIAMS, THERESA, M.

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