Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-04-07
2000-06-27
Huang, Evelyn Mei
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514211, 514212, 514218, 5142222, 514241, 514253, 514255, 540467, 540470, 540474, 540481, 540545, 540554, 540597, 544363, 544128, 546172, A61K 3147, C07D40112, C07D40114
Patent
active
06080758&
DESCRIPTION:
BRIEF SUMMARY
FIELD OF THE INVENTION
The present invention relates to novel benzenesulfonamide compounds, to the process for their preparation and to their use in therapeutics.
These novel compounds have especially an antagonistic action towards bradykinin and are useful in therapeutics, particularly for the treatment of pain, inflammation, asthma and allergic rhinitis.
PRIOR ART
It is known that one of the possible ways of treating certain pathological conditions of a painful and/or inflammatory nature (such as asthma, rhinitis, septic shock, toothache, etc.) is to antagonize the action of certain hormones such as bradykinin or kallidin. These peptide hormones are in fact involved in a large number of physiological processes, some of which are closely associated with these pathological conditions.
Although no products possessing this mode of action have yet been marketed, numerous studies have been undertaken to create compounds capable of antagonizing the bradykinin receptors. Bradykinin is a peptide hormone consisting of 9 amino acids (Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg SEQ ID NO: 1) and kallidin is a peptide hormone (Lys-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg SEQ ID NO: 2) which has an additional amino acid (Lys) compared with bradykinin. Earlier studies are known to have provided peptides which react with the bradykinin receptors: some of them, such as bradycor (CP.0127 from Cortech), icatibant (HOE 140 from Hoechst) ["bradycor" and "icatibant" are international non-proprietary names (INN)] or NPC 17761 (from Scios-Nova), have an inhibitory action on the binding of bradykinin to the bradykinin B.sub.2 receptor. More recently, non-peptide compounds have been proposed as bradykinin antagonists in respect of binding to the bradykinin B.sub.2 receptor, especially in EP-A-0596406 and EP-A-0622361. It is also known that certain compounds which are structurally related to those referred to in the two patent applications cited above have already been described as possibly having antithrombotic properties, especially in DE-A-3617183 and EP-A-0261539.
OBJECT OF THE INVENTION
There is a need for reducing or eliminating pain and inflammation in mammals and particularly in man.
To meet this need, a novel technical solution has been sought which is effective on the one hand in the treatment of pain, irrespective of its origin, especially pain associated with inflammatory phenomena, and on the other hand in the treatment of inflammation.
According to the invention, it is proposed to provide a novel technical solution which involves competitive binding, at the bradykinin B.sub.2 receptor, between (i) bradykinin and related or analogous hormones, and (ii) an antagonistic substance, and utilizes benzenesulfonamide compounds which are structurally different from the known products mentioned above and which limit or substantially inhibit the binding of bradykinin and analogous hormones to said bradykinin B.sub.2 receptor.
In accordance with this novel technical solution, it is proposed according to a first feature of the invention to provide benzenesulfonamide compounds as novel industrial products, according to a second feature of the invention to provide a process for the preparation of these compounds, and according to a third feature of the invention to provide the use of these compounds, especially in therapeutics, as analgesic and/or anti-inflammatory active ingredients.
SUBJECT OF THE INVENTION
In accordance with the novel technical solution of the invention, a benzenesulfonamide compound is recommended as a novel industrial product, said compound being characterized in that it is selected from the group consisting of: ##STR2## in which: X is a halogen atom, ##STR3## A is a group --CH.sub.2 --, --CH(OH)-- or --CH(NH--COCH.sub.3)-- or a sulfur atom, CO--N(R.sub.2)--B--R.sub.1, CH.sub.2 --NR.sub.3 R.sub.4 or a phenyl group, -C.sub.10 -alkyl group, group, it being possible for NR.sub.3 R.sub.4 to be a saturated heterocyclic radical having from 5 to 8 ring members and containing at least one nitrogen atom, and the carbon ca
REFERENCES:
patent: 5563162 (1996-10-01), Oku
Stewart JM. Bioplymers. 37, 143-155, 1995.
Stewart JM. Agents and Actions Suppl. 38 (1), 546-550, 1992.
Barth Martine
Bondoux Michel
Dodey Pierre
Houziaux Patrick
Ou Khan
Fournier Industrie et Sante
Huang Evelyn Mei
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