AP604A - Substituted indoloquinoxalines and their use as HIV integrase inhibiting compositions. - Google Patents

Substituted indoloquinoxalines and their use as HIV integrase inhibiting compositions. Download PDF

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Publication number
AP604A
AP604A APAP/P/1995/000751A AP9500751A AP604A AP 604 A AP604 A AP 604A AP 9500751 A AP9500751 A AP 9500751A AP 604 A AP604 A AP 604A
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AP
ARIPO
Prior art keywords
group
iodine
lower alkyl
formula
hiv integrase
Prior art date
Application number
APAP/P/1995/000751A
Other versions
AP9500751A0 (en
Inventor
Jan Olof Einar Bergman
Original Assignee
Leif J I Lundblad
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 Leif J I Lundblad filed Critical Leif J I Lundblad
Publication of AP9500751A0 publication Critical patent/AP9500751A0/en
Application granted granted Critical
Publication of AP604A publication Critical patent/AP604A/en

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)
  • Medicines Containing Plant Substances (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Use of a compound having the formula 1 and the pysiologically acceptable addition products of the compounds with acids and halogen adducts, preferably adducts with iodine, iodine monochloride or iodine monobromide, for preparing a medicament for inhibiting the enzyme human immunodeficiency virus integrase (hiv integrase).

Description

INHIBITOR
The present invention relates to use of indolo-2,3b-quinoxalines of the general formula I
c wherein R^ represents hydrogen or one or several, preferably 1 to 4, similar or different substituents in the positions 1-4 and/or 7-10, selected from halogen, preferably Br, lower alkyl/alkoxy group having not more than 4 carbon atoms, trifluoromethyl group, trichloromethyl group;
X is a group -(CH2)n-R2 wherein R2 represents a nitrogen containing basic residue such as NH2, NHR^ or NR^Rg wherein R4 , Rg and Rg independently are lower alkyl or cycloalkyl and n is an integer of from 1 to 4 and
R2 represents hydrogen, lower alkyl/cycloalkyl group having not more than 4 carbon atoms, and the physiologically acceptable addition products of the compounds with acids and halogen adducts, preferably adducts with iodine, iodine monochloride or iodine monobromide, as inhibitors of human immunodeficiency virus (HIV) integrase.
AP/P/ 9 5 / 0 0 7 5
AP.00304
Substituted indoloquinoxalines of formula I have previously been demonstrated to possess valuable activity against several types of vira and several of the compounds also have been demonstrated to show a high anti-cancer effect, cf. our previous patents EP 0,238,459 and U.S. 4,990,510. However, they have also been shown to be Inactive as enzyme inhibitors, cf. Harmenberg et al. Antimicrobial Agents and Chemotherapy, November 1988, pp. 1720-1724. These studies included several virus polymerases.
Of the RNA viruses the retroviruses are of particular importance. Retroviruses are a sub-group of RNA viruses which In order to replicate must first reverse transcribe the RNA of their genome into DNA (transcription is a conventional description of the synthesis of RNA from DNA). Once in the form of DNA the viral genome may be incorporated into the host cell genome which allows it to take advantage of the transcription/translation of the host cell for the purposes of replication. Once incorporated in the host cell the viral DNA is virtually indistinguishable from the host's DNA and, in this state, the virus may persist for the life of the cell.
AP/P/ 9 5 / 0 0 7 5 1
Human Immunodeficiency Virus (HIV) is a species of retrovirus which has been reproducibly isolated from humans with Acquired Immune Deficiency Syndrome (AIDS) or with the symptoms that frequently precede AIDS. AIDS is an immunosuppressive or immunodestructive disease that predisposes subjects to fatal opportunistic infections. AIDS is characteristically associated with a progressive depletion of T-cells, especially the helper-inducer subset bearing the OKT4 surface marker. HIV is cytopathic and seems to preferentially infect and destroy T-cells bearing the OKT4 marker and it is generally recognised that HIV is the etiological agent of AIDS.
AP .0 0 6 0 4
The treatment of human immunodeficiency virus (HIV) is thus an increasing and important problem which needs to be solved.
It has according to the present invention unexpectedly been found that compounds of the general formula I are active against the enzyme human immunodeficiency virus integrase which was a surprising discovery in view of the fact that compounds of the same type previously had been shown to be inactive as enzyme inhibitors, cf. the article of Harmenberg et al cited above.
According to the present invention it has surprisingly been found that these indoloquinoxalines are active against the enzyme human immunodeficiency virus integrase (HIV integrase). This is evidenced from an in vitro assay in accordance with the method described by M.R. Fesen et al in Proc. Natl. Acad. Sci., USA, March 1993, Vol. 90, pp. 23992403.
In this test the sequental cleavage and integration reactions in the retroviral integrase assay can be illustrated by means of the following figure:
AP/P/ 95/00751
The cleavage reaction removes a dinucleotide from the 3' end of one of the strands at the integration site, thereby conOO verting the P-labeled 21-mer to a 19-mer (step 1). Step 2, the integration can occur at several sites in either recipient strand. Reaction products were separated by electrophoresis and analyzed by autoradiography.
AP. Ο Ο 6 0 A
The substances of formula I used according to the present invention generally show low toxicity; thus, e-g- the compound 2,3-dimethyl-6-(N,N-dimethylaminoethyl)-6H-indologuinoxaline having the formula II ,N-
CIL
CH/ CII3 showed the following data when tested as to toxicity:
Acute toxicity
LD p.o. rats > 800 mg/kg
LD i.v. rats > 100 mg/kg
General toxicity after repeated administration NOEL (no observable effect level)
i.v. rats 12.5 mg/kg for 28 days dermal rabbits 200 mg/kg for 28 days (except for local toxicity)
APIPI 9 5 / 0 0 7 5 1
The substances of formula I used according to the present invention are prepared in accordance with the methods described in our above cited previous patents EP 0,238,459 and U.S. 4,990,510.
One compound of the general formula I, viz. the abovementioned compound II, was tested as an inhibitor· human immunodeficiency virus integrase by the method described by M. R. Fesen et al in the above ci ted article in Pro'·. Natl .
Acad. Sci.
AP.00604
The test results have been plotted in Figure 1 wherein % inhibition is shown as a function of concentration.
Compounds of the general structure I form salts with reverse transcriptase inhibiting phosphonoalkanoic acids (e.g. phosphonoformic acid) hence these are interesting possibilities Cor synergistic effects.

Claims (2)

1. Use of a compound having the formula I
AP. 0Q6n 4
CLAIMS wherein R^ represents hydrogen or one or several, preferably 1 to 4, similar or different substituents in the positions 1-4 and/or 7-10, selected from halogen, preferably Br, lower alkyl/alkoxy group having not more than 4 carbon atoms, trifluoromethyl group, trichloromethyl group;
X is a group -(CH2)n-R2 wherein R2 represents a nitrogen containing basic residue such as NH2, NHR4 or NR^Rg wherein r4, Rg and Rg Independently are lower alkyl or cyeloalkyl and n is an Integer of from 1 to 4 and
Rg represents hydrogen, lower alkyl/cyeloalkyl group having not more than 4 carbon atoms,· and the physiologically acceptable addition products of the compounds with acids and halogen adducts, preferably adducts with iodine, iodine monochloride or iodine monobromide, for preparing a medicament for inhibiting the enzyme . human immunodeficiency virus integrese (HIV integrase).
2. Use according to claim 1, characterized in that the compound corresponds to the formula
Ns
CH,Z CHj wherein Rj is hydrogen or Br.
APAP/P/1995/000751A 1994-06-23 1995-06-21 Substituted indoloquinoxalines and their use as HIV integrase inhibiting compositions. AP604A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
SE9402241A SE504289C2 (en) 1994-06-23 1994-06-23 Use of certain indolo-2,3b-quinoxalins for the preparation of a drug for inhibiting the enzyme HIV integrase

Publications (2)

Publication Number Publication Date
AP9500751A0 AP9500751A0 (en) 1995-07-31
AP604A true AP604A (en) 1997-07-21

Family

ID=20394513

Family Applications (1)

Application Number Title Priority Date Filing Date
APAP/P/1995/000751A AP604A (en) 1994-06-23 1995-06-21 Substituted indoloquinoxalines and their use as HIV integrase inhibiting compositions.

Country Status (9)

Country Link
US (1) US5866575A (en)
EP (1) EP0760662B1 (en)
AP (1) AP604A (en)
AU (1) AU2812195A (en)
DE (1) DE69523450T2 (en)
ES (1) ES2166400T3 (en)
IL (1) IL114201A (en)
SE (1) SE504289C2 (en)
WO (1) WO1996000067A1 (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE504289C2 (en) * 1994-06-23 1996-12-23 Leif J I Lundblad Use of certain indolo-2,3b-quinoxalins for the preparation of a drug for inhibiting the enzyme HIV integrase
SE504862C2 (en) * 1994-12-27 1997-05-20 Leif J I Lundblad Use of certain indolo- §2,3b-quinoxalines for the preparation of a drug for the protection of DNA in the initiation and / or promotional phase of carcinogenesis and for the prevention of oxidative stress in patients with diseases related to free radicals
US6465466B1 (en) 1995-12-22 2002-10-15 Leif J. I. Lundblad Uses of indolo-2 [2,3b] -quinoxalines
SE9704723D0 (en) * 1997-12-17 1997-12-17 Leif J I Lundblad ligands
SE516133C2 (en) * 1999-02-25 2001-11-19 Lundblad Leif J I Use of certain substituted indoloquinoxalins for the preparation of an agent for the protection of tissues, organs and cells during transplantation
WO2021250204A1 (en) * 2020-06-10 2021-12-16 Cyxone Ab Oral formulation comprising a crystalline form of rabeximod

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0238459A1 (en) * 1986-01-21 1987-09-23 Lundblad, Leif Substituted indoloquinoxalines

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE504289C2 (en) * 1994-06-23 1996-12-23 Leif J I Lundblad Use of certain indolo-2,3b-quinoxalins for the preparation of a drug for inhibiting the enzyme HIV integrase
SE504862C2 (en) * 1994-12-27 1997-05-20 Leif J I Lundblad Use of certain indolo- §2,3b-quinoxalines for the preparation of a drug for the protection of DNA in the initiation and / or promotional phase of carcinogenesis and for the prevention of oxidative stress in patients with diseases related to free radicals

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0238459A1 (en) * 1986-01-21 1987-09-23 Lundblad, Leif Substituted indoloquinoxalines

Also Published As

Publication number Publication date
DE69523450D1 (en) 2001-11-29
IL114201A (en) 2000-11-21
US5866575A (en) 1999-02-02
SE504289C2 (en) 1996-12-23
SE9402241D0 (en) 1994-06-23
EP0760662B1 (en) 2001-10-24
SE9402241L (en) 1995-12-24
AU2812195A (en) 1996-01-19
AP9500751A0 (en) 1995-07-31
EP0760662A1 (en) 1997-03-12
DE69523450T2 (en) 2002-05-16
WO1996000067A1 (en) 1996-01-04
IL114201A0 (en) 1995-10-31
ES2166400T3 (en) 2002-04-16

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