Hoffmann-la Roche Inc.

Syntex (u.s.a.) Inc.

Other

University of Texas System

Roche Palo Alto LLC

The United States of America As Represented by the Department of

Milan R Uskokovic

Enrico G Baggiolini

Giacomo Pizzolato

Pasquale N Confalone

Peter Michael Wovkulich

Shian-Jan Shiuey

John Joseph Partridge

Andrew D Batcho

Bernard Michael Hennessy

Guenter Grethe

Gary A Truitt

Hsi L Lee

John A McLane

John Joseph Partridge, Jr

Elizabeth D Lollar

Enrico G Baggiolini, Deceased

Jerome Anthony Iacobelli

Naresh K Chadha

Percy Sarwood Manchand

Alfred Boris

Thomas I Doran

John Sereno

Graeme Findlay Bryce

Richard Lewis Momparler

Barbara J Baggiolini

Thomas A Narwid

Benoit Thomas Dore

Michelangelo Scalone

Brian H Vickery

Michael F Holick

Masami Okabe

Marianne Rouge

Norberto J Palleroni

Ann Goldstein

Carl Despreaux

John J Nestor

John J Nestor, Jr

Charles Y Pak

Thomas Henry Williams

Juerg Albert Gutzwiller

Farhad Sedarati

Donald E Berger, Jr

Ronald L Horst

Satyanarayama G Reddy

Joseph E Zerwekh

Joseph L Napoli

Peng C Tang

The present invention provides a method for treating osteoporosis, hyperparathyroidism or an autoimmune disease in a patient by administering to the patient a 3-desoxy vitamin Danalog of the formula: 

Methods of treatment using 3-desoxy vitamin D3 analogs

3-Desoxy-vitamin D3 analog esters

1,3-dihydroxy-20,20-cycloalkyl-vitamin D3analogs

Vitamin D3 analogs

The invention relates to a process for the preparation of vitamin D.sub.3 compounds of formula I. ##STR1## Wherein A is a single or a double bond; B is a single, cis-double, trans double or a triple bond; R.sub.1 and R.sub.2 are independently hydrogen, a lower alkyl, e.g., a C.sub.1 -C.sub.4 alkyl; R.sub.3 and R.sub.4 are independently a lower alkyl, e.g., C.sub.1 -C.sub.4 alkyl, a hydroxyalkyl, and a haloalkyl, e.g., a fluoroalkyl; and X and Y are independently hydrogen or hydroxy in the case when B is a single or a double bond.

Synthesis of 3-epi vitamin D.sub.3 metabolites and analogs

The invention relates to a compound of the formula ##STR1## wherein A is ##STR2## Et is ethyl, and R is hydroxy and R.sup.1 is hydrogen or .dbd.CH.sub.2 or R is hydrogen or fluoro and R.sup.1 is .dbd.CH.sub.2. Compounds of formula I stimulate HL-60 cell differentiation. Accordingly, the compounds of formula I are useful as agents for the treatment of neoplastic diseases, such as leukemia.

16-ene-26,27-bishomo cholecalciferols

This invention provides Vitamin D.sub.3 analogs of the Formula I ##STR1## wherein: X is H.sub.2 or CH.sub.2 ;

Vitamin D.sub.3 analogs with bis C-20 side chains

This invention provides a method of treating or preventing neoplastic diseases. The method comprises adminstering to a host in need of such treatment or prevention an effective amount of a Vitamin D.sub.3 analog of the Formula I wherein:

Method of using vitamin D.sub.3 analogs with bis C-20 side chains

Compounds of the formula ##STR1## wherein R is hydrogen, fluorine, or hydroxyl, each R.sub.2 is lower alkyl or C(R.sub.3).sub.3 and R.sub.3 is halogen, X is .dbd.CH.sub.2 or when R is hydroxy, X is hydrogen or .dbd.CH.sub.2, and A is --C.tbd.C-- ##STR2## or --CH.sub.2 --CH.sub.2 --, which are useful in the treatment of hyperproliferative skin disorders, neoplastic diseases, and sebaceous gland diseases.

Vitamin D.sub.3 analogs

A method of inducing inhibition or loss of cell proliferation in solid tumors utilizing a Vitamin D.sub.3 analog, as well as a method of inducing loss of cell proliferation in solid tumors utilizing trans retinoic acid and a Vitamin D.sub.3 analog. In another aspect, a method of inducing inhibition or loss of cell proliferation in solid tumors utilizing a Vitamin D.sub.3 metabolite, as well as a method of inducing loss of cell proliferation in solid tumors utilizing trans retinoic acid and a Vitamin D.sub.3 metabolite.

Methods of treatment

A compound of formula I ##STR1## wherein R is hydrogen, fluorine or hydroxy, and X is .dbd.CH.sub.2 or when R is hydroxy, X is hydrogen or .dbd.CH.sub.2 which are useful in the treatment of hyperproliferative disorders, neoplastic diseases and sebaceous gland diseases.

Fluorinated Vitamin D.sub.3 analogs

Fluorinated Vitamin D.sub.3 analogs, intermediates for their preparation, compositions comprising the analogs and methods of treatment of osteoporosis and related conditions with these and related analogs are provided.

Fluorinated vitamin D3 analogs

Growing community of inventors

Upper Montclair, NJ, United States of America

Milan R Uskokovic