Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each selected from the group consisting of C.sub.1 -C.sub.2 lower alkyl; X is NH or S; and n is a whole number within the range of 1-4 inclusive; and when n=0, X is (CH.sub.2).sub.3 and the pharmaceutically acceptable salts thereof have been shown to be effective in treating tamoxifen resistant tumors.
Abstract: Novel pyridiniminyl-1,2-benzisoxazoles and -benzisothiazoles, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction and treating depression utilizing the 1,2-benzisoxazoles and -benzisothiazoles and intermediates, or compositions thereof are disclosed.
Type:
Grant
Filed:
May 2, 1996
Date of Patent:
September 16, 1997
Assignee:
Hoechst Marion Roussel Inc.
Inventors:
David M. Fink, Barbara E. Kurys, Gregory M. Shutske, John D. Tomer, IV
Abstract: Diarylalkyl piperidines of formula (1) ##STR1## reverse drug resistance in multi-drug resistant tumors. These compounds apparently function by inhibiting a p-glycoprotein pump which becomes activated in late stage tumor development and which is inherently present in tumors from certain origins.
Abstract: The present invention is directed toward a novel process of preparing 2'-exocyclic vinylfluoride derivatives of cytidine analogues for use as ribonucleotide reductase inhibitors. The novel process of the present invention utilizes a cytidine derivative as the required starting material and provides the ribonucleotide reductase inhibitor in a more efficient than the reaction sequence. The process is more efficient than the process disclosed by McCarthy et al. in European Patent Application Publication No. 0 372 268 published Jun. 13, 1990, in that it requires fewer chromatographies and results in an overall yield of greater than 25% for the five steps. The present invention further provides the ribonucleotide reductase inhibitor in a four step reaction sequence and results in an overall yield of greater than 35%.
Type:
Grant
Filed:
April 10, 1995
Date of Patent:
December 31, 1996
Assignee:
Merrell Pharmaceuticals Inc.
Inventors:
James R. McCarthy, Donald P. Matthews, Jeffrey S. Sabol, James R. McConnell, Richard E. Donaldson, Robert Duquid
Abstract: The present invention provides an oral pharmaceutical composition in solution form, comprising,a) a therapeutically effective amount of a piperidinoalkanol compound or a pharmaceutically acceptable salt thereof; andb) a suitable solvent systems, comprising propylene glycol and glacial acetic acid.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
November 12, 1996
Assignee:
Hoechst Marion Roussel, Inc.
Inventors:
Thomas T. Ortyl, Paul F. Skultety, Gail H. Hurst
Abstract: The present invention relates to a novel process for preparing 1-(3-trialkylsilylphenyl)-2,2,2-trifluoromethyl ethanones which are useful for the treatment of Alzheimer's disease and senile dementia as disclosed by Schirlin, et al. in European Patent Application Publication No. 0 409 676, published Jan. 23, 1991.
Abstract: The present invention is directed toward a novel process of preparing 2'-exocyclic vinylfluoride derivatives of cytidine analogues for use as ribonucleotide reductase inhibitors. The novel process of the present invention utilizes a cytidine derivative as the required starting material and provides the ribonucleotide reductase inhibitor in a more efficient five step reaction sequence. The present invention further provides the ribonucleotide reductase inhibitor in a four step reaction sequence and results in an overall yield of greater than 35%.
Type:
Grant
Filed:
May 11, 1995
Date of Patent:
April 16, 1996
Assignee:
Hoeschst Marion Roussel, Inc.
Inventors:
James R. McCarthy, Donald P. Matthews, Jeffrey S. Sabol, James R. McConnell, Richard E. Donaldson, Robert Duquid
Abstract: The present invention relates to a novel process for preparing 1-halo-3-trialkylsilanyl-benzenes from 1,3-dihalo-benzenes which are useful intermediates in the preparation of 1-(3-trialkylsilylphenyl)-2,2,2-trifluoromethyl ethanones which are useful for the treatment of Alzheimer's disease and senile dementia.
Abstract: The compound (R)-2-[(phenylisopropyl)amino]adenosine whose structure is given below: ##STR1## (R)-2-[(phenylisopropyl)amino]adenosine is about two orders of magnitude greater in its selectivity between the A-1 and A-2 adenosine receptors than its diastereoisomer. This compound is useful for lowering blood pressure.
Type:
Grant
Filed:
September 15, 1994
Date of Patent:
June 20, 1995
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Norton P. Peet, David R. Borcherding, Nelsen L. Lentz, Philip M. Weintraub, Philip R. Kastner
Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each selected from the group consisting of C.sub.1 -C.sub.2 lower alkyl; X is NH or S; and n is a whole number within the range of 1-4 inclusive; and when n=0, X is (CH.sub.2).sub.3 and the pharmaceutically acceptable salts thereof have been shown to be effective in treating tamoxifen resistant tumors.