Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-04-01
1996-05-07
Bond, Robert T.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
540456, A61K 31395, C07D49816
Patent
active
055146864
DESCRIPTION:
BRIEF SUMMARY
DESCRIPTION
NEW USE
This invention relates to a new use of macrolide compounds for eye diseases. More specifically, this invention relates to a new use of macrolide compounds for eye diseases, particularly, allergic conjunctivitis.
Accordingly, this invention provides a new use of the macrolide compounds for preventing or treating eye diseases as mentioned above.
Further, this invention provides a prophylactic or therapeutic agent for eye diseases as mentioned above, which comprises the macrolide compounds.
Still further, this invention provides a method for preventing or treating eye diseases as mentioned above, which comprises administering said macrolide compounds to mammals.
Some of the macrolide compounds used in this invention are known and disclosed, for example, in European Patent Publication No. 0184162 and International Patent Application WO 89/05304.
Those known macrolide compounds include the fermentation products, such as FR-900506, FR-900520, FR-900523 and FR-900525, isolated from microorganisms belonging to genus Streptomyces, such as Streptomyces tsukubaensis No. 9993 (FERM BP-927) or Streptomyces hygroscopicus. subsp. yakushimaensis No. 7238 (FERM BP-928), and their related compounds prepared from these fermentation products. And new macrolide compounds can be prepared from the above known macrolide compounds in a conventional manner.
These macrolide compounds were indicated inter alia for use in the treatment of rejection to transplantation, autoimmune diseases and infectious diseases caused by pathogenic microorganisms, such as various fungi (Aspergills fumigatus, Fusarium oxysperum, Trichophyton asteroides, etc)(e.g.J. Antibiotics, XL(9), 1249-1255, 1987).
The inventors of this invention have surprisingly found that the macrolide compounds mentioned hereinbelow are useful for preventing or treating eye diseases, particularly, allergic conjunctivitis, and also other allergic diseases such as food allergy, allergic rhinitis, etc.
The macrolide compounds used in this invention can be represented by the following general formula (I). ##STR1##
wherein each vicinal pair of substituents R.sup.1 and R.sup.2 !, R.sup.3 and R.sup.4 !, R.sup.5 and R.sup.6 ! independently a) represent two vicinal hydrogen atoms, or b) form a second bond between the vicinal carbon atoms to which they are attached;
in addition to its significance above, R.sup.2 may represent an alkyl group;
R.sup.7 represents H, OH, protected hydroxy or O-alkyl, or in conjunction with R.sup.1 it may represent =O;
R.sup.8 and R.sup.9 independently represent H or OH;
R.sup.10 represents H, alkyl, alkyl substituted by one or more hydroxyl groups, alkenyl, alkenyl substituted by one or more hydroxyl groups, or alkyl substituted by =O;
X represents O,s (H, OH), (H,H) or --CH.sub.2 O--;
Y represents O, (H, OH) (H,H) N--NR.sup.11 R.sup.12 or N--OR.sup.13 ;
R.sup.11 and R.sup.12 independently represent H, alkyl, aryl or tosyl;
R.sup.13, R.sup.14, R.sup.15, R.sup.16, R.sup.17, R.sup.18, R.sup.19, R.sup.22 and R.sup.23 independently represent H or alkyl;
R.sup.20 and R.sup.21 independently represent O, or they may independently represent (R.sup.20 a,H) and (R.sup.21 a,H) respectively; R.sup.20 a and R.sup.21 a independently represent OH, O--alkyl or OCH.sub.2 OCH.sub.2 CH.sub.2 OCH.sub.3 or R.sup.21 a is protected hydroxy;
in addition, R.sup.20 a and R.sup.21 a may together represent an oxygen atom in an epoxide ring;
n is 1, 2 or 3;
in addition to their significances above Y, R.sup.10 and R.sup.23, together with the carbon atoms to which they are attached, may represent a 5- or 6- membered N-, S- or O-containing heterocyclic ring, which may be saturated or unsaturated, and which may be substituted by one or more groups selected from alkyl, hydroxy, alkyl substituted by one or more hydroxyl groups, O--alkyl, benzyl and --CH.sub.2 Se(C.sub.6 H.sub.5); and pharmaceutically acceptable derivatives thereof.
The specific examples of the definitions of compound (I) and the preferred working modes of the invention are described in detail below.
Th
REFERENCES:
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Kobayasshi et al. "Transplantation Proceedings" vol. XXI, No. 1, (1989) pp. 3156-3158.
Transplantation Proceedings, vol. 21, No. 1, Feb. 1989, C. Kobayashi, et al., "Supression of Corneal Graft Rejection in Rabbits By a New Immunosuppressive Agent, FK-506", pp. 3156-3158.
The Journal of Immunology, vol. 146, No. 7, Apr. 1, 1991, pp. 2374-2381, Amato de Paulis, et al., "FK-506, A Potent Novel Inhibitor of the Release of Proinflammatory Mediators from Human FceRI.sup.+ Cells.sup.1 ".
The Journal of Allergy and Clinical Immunology, vol. 87, No. 1, Part 2, Jan. 1991, p. 207.
Iwaki Yoichi
Mochizuki Manabu
Bond Robert T.
Fujisawa Pharmaceutical Co. Ltd.
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