Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, Y and W are as described herein, compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
December 12, 2014
Date of Patent:
November 15, 2016
Assignee:
Hoffmann-La Roches Inc.
Inventors:
Daniel Hunziker, Patrizio Mattei, Harald Mauser, Marco Prunotto, Christoph Ullmer
Abstract: The present invention is directed to novel diaminothiazoles of formula
These compounds inhibit cyclin-dependent kinase 4 (Cdk4) and are selective against Cdk2 and Cdk1. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung and colon and prostate tumors.
Type:
Grant
Filed:
May 5, 2003
Date of Patent:
November 16, 2004
Assignee:
Hoffmann-La Roches
Inventors:
Xin-Jie Chu, Qingjie Ding, Nan Jiang, Kyungjin Kim, Allen John Lovey, Warren William McComas, John Guifoyle Mullin, Jr., Jefferson Wright Tilley
Abstract: The present invention relates to a parenteral composition comprising a bisphosphonic acid or a pharmaceutically acceptable salt thereof (bisphosphonate) as active component and a pharmaceutically acceptable chelating agent, processes of the preparation of this composition, and methods of their use in the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, hypercalcemia of malignancy, and metabolic bone disease. The compositions are especially useful for improving the local tolerance of the active component when administered parenterally.
Type:
Grant
Filed:
January 11, 2001
Date of Patent:
January 13, 2004
Assignee:
Hoffmann-La Roches Inc.
Inventors:
Anke Diederich, Pierre Goldbach, Thomas Pfister
Abstract: A process for synthesizing 3-acryloxymethyl antibacterialcephalosporin compounds of formula ##STR1## wherein R is hydrogen or a carboxylic acid protecting group; R.sup.1 is hydrogen or an acyl group; R.sup.2 is hydrogen or lower alkoxy; and R.sup.3 is carbocyclic aryl substituted on the ring with one or more members selected from the group consisting of hydroxy, lower alkyl, amino, cyano, lower alkoxy, halogen and alkylcarboxy,as well as the corresponding readily hydrolyzable esters, pharmaceutically acceptable salts and hydrates of these compounds where R is hydrogen, in which a 2-carboxylic acid 3-hydroxymethyl cephalosporin compound is first treated with an organic base to form an organic salt therewith, followed by acylation of the 3-hydroxymethyl substituent.
Type:
Grant
Filed:
April 27, 1990
Date of Patent:
May 12, 1992
Assignee:
Hoffmann-La Roches Inc.
Inventors:
Dennis D. Keith, Chung-Chen Wei, Kevin F. West
Abstract: A process for producing .alpha.-tocopherol (Vitamin E) by condensing trimethylhydroquinone with either a phytol or an isophytol derivative thereof in the presence of trifluoroacetic acid.