Hoffmann-la Roche Inc.

Other

John A McLane

Milan R Uskokovic

Thomas I Doran

Michelangelo Scalone

Peter Michael Wovkulich

Masami Okabe

Ann Goldstein

Giacomo Pizzolato

Bernard Michael Hennessy

Farhad Sedarati

Satyanarayama G Reddy

Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or acyl; provided that only one of R.sup.1 or R.sup.2 is hydrogen are taught as useful in the treatment of hyperproliferative skin diseases and sebaceous gland diseases.

Vitamin D3 analogs for the treatment of psoriasis and sebaceous gland

Compounds of the formula ##STR1## wherein R is hydrogen, hydroxy, or fluorine, X is H.sub.2 or .dbd.CH.sub.2, and the 23,24-double bond is E or Z, are useful as agents for the treatment of hyperproliferative disorders of the skin such as psoriasis, as agents for the treatment of tumors such as breast cancer, as agents for the treatment of neoplastic diseases such as leukemia, and as agents for the treatment of sebaceous gland diseases such as acne and seborrheic dermatitis.

Vitamin D3 fluorinated analogs

The invention relates to the compounds 1,25-dihydroxy-16-ene-24-oxo-cholecalciferol and 1,24,25-trihydroxy-16-ene-cholecalciferol which stimulate differentiation of HL-60 cells, rendering them useful as an agent for the treatment of neoplastic diseases such as leukemia, and also decrease proliferation of human keratinocytes, rendering them useful as an agent for the treatment of hyperproliferative disorders of the skin such as psoriasis.

Stable and active metabolites of 1,25-dihydroxy-16-ene-cholecalciferol

The invention comprises compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or acyl; provided that only one of R.sup.1 or R.sup.2 is hydrogen, useful in the treatment of hyperproliferative skin diseases and sebaceous gland diseases. The invention also includes a process for making these compounds and steroid intermediates of the process.

Steroid intermediates for the formation of vitamin D.sub.3 analogues

The invention is drawn to compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or acyl; provided that only one of R.sup.1 or R.sup.2 is hydrogen, useful in the treatment of hyperproliferative skin diseases and sebaceous gland diseases.

Vitamin D3 analogs

The invention relates to compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl; ##STR2## wherein R.sub.2 is lower alkyl; R.sub.3 is phenyl, or phenyl substituted by 1 to 3 substituents selected from the group consisting of halo, lower alkyl, and lower alkoxy; and R.sub.4 is hydrogen or methyl or the corresponding hydroxy acid of formula ##STR3## and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as described above; or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid, an acetylamino-substituted-C.sub.1-4 alkyl ester of said acid, a phenyl-dimethylamino ester of said acid or a .alpha.-monoglyceride of said acid. The compounds of formulas I and II are useful as agents for the treatment of hyperproliferative skin diseases such as psoriasis.

Antipsoriatic agents

The invention relates to compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl; A is ##STR2## or A is ##STR3## wherein R.sub.2 is lower alkyl; R.sub.3 is phenyl, or phenyl substituted by 1 to 3 substituents selected from the group consisting of halo, lower alkyl, and lower alkoxy; and R.sub.4 is hydrogen or methyl or the corresponding hydroxy acid of formula ##STR4## wherein A is ##STR5## or A is ##STR6## and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as described above; or a pharmaceutically acceptable salt of said acid, a C.sub.1-4 alkyl ester of said acid, an acetylamino-substituted-C.sub.1-4 alkyl ester of said acid, a phenyl-dimethylamino ester of said acid or a .alpha.-monoglyceride of said acid. The compounds of formulas I and II are useful as agents for the treatment of hyperproliferative skin diseases such as psoriasis.

A method of treating hyperproliferative skin diseases, such as psoriasis, using a compound of formula ##STR1## wherein R.sub.1 is hydrogen when R.sub.2 is hydroxy, and R.sub.1 is methyl when R.sub.2 is hydrogen; and A is alkyl; cycloalkyl; alkenyl; alkyl substituted with trifluoromethyl; phenyl; halophenyl; phenyl-C.sub.1-3 alkyl; phenyl-C.sub.1-3 alkyl substituted on the phenyl with 1 to 3 substituents selected from the group consisting of halo, C.sub.1-3 alkyl, and C.sub.1-3 alkoxy; or

Growing community of inventors

West Haven, CT, United States of America

John A McLane