Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1994-08-18
1996-12-10
Datlow, Philip I.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514184, 540465, 540474, C07D40114, C07D40310, A61K 31395, A61K 31555
Patent
active
055831311
DESCRIPTION:
BRIEF SUMMARY
This application is the 356USC371 Nation Stage of PCT/GB92/02334, filed Dec. 16, 1992.
This invention concerns improvements in chemical compounds, more especially it concerns compounds and pharmaceutical compositions. In particular it concerns compositions and compounds having activity in in vitro tests on Human Immunodeficiency Virus-infected cells.
The disease known as Acquired Immune Deficiency Syndrome (AIDS) caused by infection by HIV has attracted immense research effort because of the effects of the disease on infected individuals and the dangers of the disease spreading to a wider section of the population. In general, although various chemo-therapeutic treatments have been advocated, and some compounds have emerged as a potential basis for treatment, there is still a need for alternatives. In particular, most treatments such as the compound known as AZT have a high toxicity to cells, and it would be desirable to find compounds which are less toxic. In man, the development of resistance to AZT has been identified as an additional clinical problem.
We have found a group of compounds which show protective properties in vitro screens of cells challenged with HIV-1 and/or HIV-2, and are therefore useful for the treatment of AIDS and AIDS Related Complex and other vital and especially retrovital infections. Accordingly, the present invention provides the use of compounds defined below, in phamaceutical compositions for treating HIV-infected patients. The invention further provides pharmaceutical compositions comprising a said compound in combination or association with a pharmaceutically acceptable diluent or excipient, for the treatment of HIV-infected patents. The invention may also be defined as the use of a said compound for the manufacture of a medicament for the treatment of HIV-infected patients. The invention further provides a process for the production of a pharmaceutical composition for the treatment of a HIV-infected patient, comprising the combination of a compound as defined below with a pharmaceutically acceptable diluent or excipient, and formulating said composition into a form suitable far administration to said patient. The invention also provides a method of treatment of an HIV-infected patient, comprising administering to said patient an effective dose of a said compound. It is to be understood that treatment includes prophylactic treatment of patients at risk, in view of the protective properties observed. The use of the compounds may also be stated as a method of treating HIV-infected or HIV-challenged human cells to prevent or modulate the multiplication of the HIV, comprising administering to said cells an effective dose of a said compound. Whilst this description is especially directed to combating HIV, this invention includes other aspects in which other diseases may be treated, including for example microbial infections.
A 2,2'-dimer of cyclam has been reported as being isolated as a 2% by-product in the synthesis of cyclam (1,4,8,11-tetraaza-cyclotetradecane) (Barefield et al, J C S Chem Con (1981), 302). This compound was stated to be insoluble in water. We believe that the insoluble 2,2'-bicyclam is a mixture of the 2R,2'R and 2S,2'S enantiomers; we have characterised a soluble dimer which we believe to be the me, so 2R,2'S isomer. The 6,6'-bicyclam isomer has been reported by Fabbrizzi et al, Inorg Chem 25, 2671 (1986). Certain N,N'-linked bicyclic compounds have been reported by Ciampolini et al, Inorg Chem 26, 3527 (1987). No biological activity has been suggested for such compounds.
U.S. Pat. No. 4,156,683 discloses monocyclic and bicyclic macrocyclic compounds, which axe said to have biological activity in regulating sodium, potassium and calcium levels in mammals. Additionally, a specific group of N-alkylated monocyclic compounds are said to possess activity against A.sub.2 influenza viruses in a modified Hermann test on chick fibroblast tissue. It is also said that the preferred compounds, which form complexes of greater stability, are those having three bridging ch
REFERENCES:
patent: 5021409 (1991-06-01), Murrer et al.
patent: 5374416 (1994-12-01), Rousseaux
Ciampolini et al, Inorganic Chem. 26(21), (1987), pp. 3527-3533.
Schneider et al, Helvitica Chimica Acta 69(1), (1986), pp. 53-61.
Yaouanc et al, J. Chem. Soc. Chem. Commun. (1991), pp. 206-207.
Bridger Gary J.
Padmanbhan Sreenivasan
Skerlj Renato T.
Thornton David M.
Datlow Philip I.
Johnson Matthey Public Limited Company
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