Vitamin D compounds and method of preparing these compounds
First Claim
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1. A method for the treatment and prophylaxis of disease states selected from the group consisting of autoimmune diseases, ache, alopecia, skin aging, imbalance in the immune system, inflammatory diseases and diseases related to abnormal cell differentiation or proliferation, in a warm-blooded living being, comprising administering to said being or treating said being with a composition comprising at least one member selected from the group consisting of a pharmaceutically acceptable carrier and pharmaceutically acceptable auxiliary substances and mixtures thereof, and, as an active ingredient a compound of formula (1) ##STR25## wherein R1 is a hydrogen atom or a hydroxy group;
- R2 is a (C1 -C3)alkyl group, a hydroxy(C1 -C3)alkyl group, a (C1 -C2)alkoxymethyl group or a (C2 -C3)alkenyl or alkynyl group;
R3 is a branched or non-branched, saturated or unsaturated aliphatic 3- to 5-membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxylR4 is a sec. or tert. (C3 -C6)alkyl group or a (C3 -C6)cycloalkyl group; and
A and B are each individually hydrogen atoms or ethyl groups, orA and B form together a methylene group in a quantity effective for the intended purpose.
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Abstract
The invention relates to a new vitamin D compound of the general formula ##STR1## wherein: R1 is a hydrogen atom or a hydroxy group;
R2 is a (C1 -C3)alkyl group, a hydroxy(C1 -C3)alkyl group, a (C1 -C2)alkoxymethyl group or a (C2 -C3)alkenyl or alkynyl group;
R3 is a branched or non-branched, saturated or unsaturated aliphatic 3- to 5 -membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy;
R4 is a sec. or tert. (C3 -C6)alkyl group or a (C3 -C6)cycloalkyl group; and
A and B are each individually hydrogen atoms or methyl groups, or
A and B form together a methylene group.
The invention further relates to a method of preparing these compounds and to their use in pharmacotherapy and cosmetics.
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Citations
12 Claims
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1. A method for the treatment and prophylaxis of disease states selected from the group consisting of autoimmune diseases, ache, alopecia, skin aging, imbalance in the immune system, inflammatory diseases and diseases related to abnormal cell differentiation or proliferation, in a warm-blooded living being, comprising administering to said being or treating said being with a composition comprising at least one member selected from the group consisting of a pharmaceutically acceptable carrier and pharmaceutically acceptable auxiliary substances and mixtures thereof, and, as an active ingredient a compound of formula (1) ##STR25## wherein R1 is a hydrogen atom or a hydroxy group;
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R2 is a (C1 -C3)alkyl group, a hydroxy(C1 -C3)alkyl group, a (C1 -C2)alkoxymethyl group or a (C2 -C3)alkenyl or alkynyl group; R3 is a branched or non-branched, saturated or unsaturated aliphatic 3- to 5-membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxyl R4 is a sec. or tert. (C3 -C6)alkyl group or a (C3 -C6)cycloalkyl group; and A and B are each individually hydrogen atoms or ethyl groups, or A and B form together a methylene group in a quantity effective for the intended purpose. - View Dependent Claims (2, 3)
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4. A method for the treatment and prevention of skin disorders in a warm-blooded living being, comprising treating said being with a cosmetical composition comprising at least one member selected from the group consisting of conventionally acceptable, non-toxic carriers and auxiliary substances and mixtures thereof, and, as the active ingredient a compound of formula (I) ##STR27## wherein:
- R1 is a hydrogen atom or a hydroxy group;
R2 is a (C4 -C3)alkyl group, a hydroxy(C1 -C3)alkyl group, a (C1 -C2)alkoxymethyl group or a (C2 -C3)alkenyl or alkynyl group; R3 is a branched or non-branched, saturated or unsaturated aliphatic 3- to 5-membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy; R4 is a sec. or tert. (C3 -C6)alkyl group or a (C3 -C6)cycloalkyl group; and A and B are each individually hydrogen atoms or ethyl groups, or A and B form together a methylene group in an effective quantity.
- R1 is a hydrogen atom or a hydroxy group;
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5. A method for the treatment and prophylaxis of disease states selected from the group consisting of autoimmune diseases, ache, alopecia, skin aging, imbalance in the immune system, inflammatory diseases and diseases related to abnormal cell differentiation or proliferation, in a warm-blooded living being, comprising administering to said being or treating said being with a composition comprising at least one member selected from the group consisting of a pharmaceutically acceptable carrier and pharmaceutically acceptable auxiliary substances and mixtures thereof, and, as an active ingredient a compound of formula (1) ##STR28## wherein:
- R1 is a hydroxy group;
R2 is a (C1 -C3)alkyl group, a hydroxy(C1 -C3)alkyl group, a (C1 -C2)alkoxymethyl group or a (C2 -C3)alkenyl or alkynyl group; R3 is a biradical of the formula
space="preserve" listing-type="equation">--O--CH.sub.2 --(CH.sub.2).sub.n --, --CH.sub.2 --CH.sub.2 --(CH.sub.2).sub.n --, --CH═
CH--(CH.sub.2).sub.n -- or --CH.sub.2 --CH.sub.2 --CH(CH.sub.3)--,wherein n is 1 or 2; R4 is an isopropyl group, a cyclopropyl group or a tert.-butyl group; and A and B are hydrogen atoms or form together a methylene group in a quantity effective for the intended purpose. - View Dependent Claims (7, 11)
- R1 is a hydroxy group;
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6. A method for the treatment and prophylaxis of disease states selected from the group consisting of autoimmune diseases, acne, alopecia, skin aging, imbalance in the immune system, inflammatory diseases and diseases related to abnormal cell differentiation or proliferation, in a warm-blooded living being, comprising administering to said being or treating said being with a composition comprising at least one member selected from the group consisting of a pharmaceutically acceptable carrier and pharmaceutically acceptable auxiliary substances and mixtures thereof, and, as an active ingredient at least one compound of formula (1) ##STR29## wherein:
- R1 is a hydrogen atom or a hydroxy group;
R3 is a branched or non-branched, saturated or unsaturated aliphatic 3- to 5-branched hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy; R4 is an isopropyl group A and B are each individually hydrogen atoms or ethyl groups, or A and B form together a methylene group in a quantity effective for the intended purpose. - View Dependent Claims (8, 12)
- R1 is a hydrogen atom or a hydroxy group;
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9. A method for the treatment and prevention of skin disorders in a warm-blooded living being, comprising treating said being with a cosmetical composition comprising at least one member selected from the group consisting of conventionally acceptable, non-toxic carriers and auxiliary substances and mixtures thereof, and, as the active ingredient a compound of formula (I) ##STR30## wherein:
- R1 is a hydroxy group;
R2 is a (C1 -C3)alkyl group, a hydroxy(C1 -C3)alkyl group, a (C1 -C2)alkoxymethyl group or a (C2 -C3)alkenyl or alkynyl group; R3 is a biradical of the formula
space="preserve" listing-type="equation">--O--CH.sub.2 --(CH.sub.2).sub.n --, --CH.sub.2 --C.sub.2 --(CH.sub.2).sub.n --, --CH═
CH--(CH.sub.2).sub.n -- or --CH.sub.2 --CH.sub.2 --CH(CH.sub.3)--,wherein n is 1 or 2; R4 is an isopropyl group, a cyclopropyl group or a tert.-butyl group; and A and B are hydrogen atoms or form together a methylene group in a quantity effective for the intended purpose.
- R1 is a hydroxy group;
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10. A method for the treatment and prevention of skin disorders in a warm-blooded living being, comprising treating said being with a cosmetical composition comprising at least one member selected from the group consisting of conventionally acceptable, non-toxic carriers and auxiliary substances and mixtures thereof, and, as the active ingredient a compound of formula (I) ##STR31## wherein:
- R1 is a hydrogen atom or a hydroxy group;
R3 is a branched or non-branched, saturated or unsaturated aliphatic 3- to 5-membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy; R4 is an isopropyl group A and B are each individually hydrogen atoms or ethyl groups, or A and B form together a methylene group in a quantity effective for the intended purpose.
- R1 is a hydrogen atom or a hydroxy group;
Specification
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Current AssigneeDuphar International Research B.V. (Abbott Laboratories)
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Original AssigneeDuphar International Research B.V. (Abbott Laboratories)
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InventorsZorgdrager, Jan, Halkes, Sebastianus J., van de Velde, Jan-Paul, Mourino, Antonio, Dijkstra, Gerhardus D. H., Sestelo, Jose P., Mascarenas, Jose L.
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Primary Examiner(s)DEES, JOSE G
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Application NumberUS08/070,998Time in Patent Office830 DaysField of Search514/167, 514/555, 260/397.2, 552/505, 552/555, 552/652, 552/653, 568/715, 568/808, 568/816, 568/817, 568/822, 568/838US Class Current514/167CPC Class CodesC07C 35/32 the condensed ring system b...C07C 401/00 Irradiation products of cho...C07C 45/292 with chromium derivativesC07C 49/477 having two ringsC07C 49/513 a keto group being part of ...
