Hoffmann-La Roche Inc.

Giacomo Pizzolato

Milan R Uskokovic

Pasquale N Confalone

Elizabeth D Lollar

Peter Michael Wovkulich

Enrico G Baggiolini

Jin-Jun Liu

Qingjie Ding

Gary A Truitt

Chung-Chen Wei

Marianne Rouge

Sung-Sau So

Vincent Stewart Madison

Yi Ren

Kin-Chun Thomas Luk

Zhuming Zhang

Binh Vu

Allen John Lovey

Norman Kong

Kshitij Chhabilbhai Thakkar

Bernard Michael Hennessy

Bradford Graves

John A McLane

John Lawson Roberts

Thomas I Doran

Milan R Uskovic

Farhad Sedarati

There is provided a compound of formula I and the pharmaceutically acceptable salts and esters thereofwherein X, X, R, R, R, R, Rand Rare herein described. The compounds exhibit activity as anticancer agents.

4,4,5,5, tetrasubstituted imidazolines

The present invention provides compounds of formula I wherein R, R, R, R, and Rare described herein. The invention also provides syntheses for preparation of such compounds and pharmaceutical compositions containing them. The invention further provides methods for inhibiting kinases, in particular CDK2, for inhibiting angiogenesis, and for treating cancers, in particular breast, colon, prostate, and lung cancer.

7,8-disubstituted pyrazolobenzodiazepines

Disclosed is a novel method for synthesizing pyrazolobenzodiazepines of formula Iusing intermediates of formula Pyrazolobenzodiazepines of formula I are useful in the treatment and control of solid tumors.

Method for synthesizing pyrazolobenzodiazepines

Disclosed are novel pyrazolobenzodiazepines having the formula These compounds are useful in the preparation of the pyrazolobenzodiazepines of formula I, which are useful in the treatment and control of solid tumors.

Pyrazolobenzodiazepines

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

26, 26, 26-Trifluoro-1.alpha., 25-dihydroxy-cholecalciferol, and the 25R or 25S epimer thereof, are described, as well as processes and intermediates utilized to prepare the same, as well as pharmaceutical compositions containing the same. 26,26,26-trifluoro 1.alpha., 25-dihydroxycholecalciferol and the 25R or 25S epimer thereof are useful agents in the treatment of disease states such as osteoporosis, oseodystrophy and leukemia.

Trifluorinated-1.alpha.,25S-dihydroxy vitamin D3 compounds

26,26,26-Trifluoro-1.alpha.,25-dihydroxy-cholecalciferol, and the 25R or 25S epimer thereof, are described, as well as processes and intermediates utilized to prepare the same, as well as pharmaceutical compositions containing the same. 26,26,26-trifluoro 1.alpha.,25-dihydroxycholecalciferol and the 25R or 25S epimer thereof are useful agents in the treatment of disease states such as osteoporosis, osteodystrophy and leukemia.

Novel trifluorinated vitamin D3 intermediates

Novel hexafluoro-cholecalciferol compounds and processes for preparing such compounds are disclosed. Intermediates utilized in the preparation of such compounds and pharmaceutical preparations containing these compounds are also disclosed.

Fluorinated vitamin D.sub.3 compounds

Thiophene derivatives having utility as blood lipid lowering agents and as antiobesity agents are disclosed.

Novel thiophene derivatives

Novel thiophene compounds having utility as biotin intermediates and blood lipid lowering agents, as well as related processes and intermediates, are disclosed.

Novel thiophene compounds

A novel process for the preparation of biotin is disclosed wherein said process employs inexpensive starting materials and reagents resulting in the obtention of biotin devoid of the biologically inactive stereoisomers.

Novel cycloheptathiophene intermediates for the synthesis of biotin

The invention relates to synthetic processes to produce the known pharmacologically active 8-methoxypsoralen and derivatives thereof. Also disclosed are various novel intermediates utilized in these processes.

Growing community of inventors

Belleville, NJ, United States of America

Giacomo Pizzolato