Abstract: Triazolone derivatives represented by the formula
wherein R1 represents optionally substituted C1-10 alkyl, A1—L1—, A1—ON═CA2, etc.; R2 represents hydrogen, C1-6 alkyl, etc.; R3 represents C1-6 alkoxy, etc.; one of T, U, and V represents CR4, another represents CH or nitrogen, and the remaining one represents CR5 or nitrogen; and W represents CR6 or nitrogen.
Abstract: A polymorph of 1-{6-ethoxy-5-[3-ethyl-6,7-dihydro-2-(2-methoxyethyl)-7-oxo-2H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-pyridylsulfonyl}-4-ethylpiperazine.
Type:
Grant
Filed:
July 26, 2001
Date of Patent:
July 16, 2002
Assignee:
Pfizer Inc.
Inventors:
Laurence James Harris, Richard Anthony Storey, Albert Shaw Wood
Abstract: It has now been found that N-L-alpha-aspartyl-L-phenylalanine 1-methyl ester (APM) exhibits antisickling properties. In vitro testing verified that APM significantly lowered the frequency of sickling of red blood cells from each of twelve pediatric aged patients being treated for sickle-cell anemia by exchange transfusion. Sickling was also inhibited in an “index” patient after oral administering of APM. These in vitro and in vivo results identify APM as a therapeutic agent for the family of sickle cell molecular diseases.
Abstract: The invention relates to novel N-(substituted phenyl)-N′-[&ohgr;-(3-substituted phenyl-4-isoxazolecarbonylamino)alkyl]piperazines, their N-oxides, and pharmaceutically acceptable salts thereof. The compounds are endowed with enhanced selectivity for alpha1-adrenergic receptors and a low activity in lowering blood pressure. The compounds are useful in the treatment of obstructive syndromes of the lower urinary tract, including benign prostatic hyperplasia (BPH), and in the treatment of lower urinary tract symptoms (LUTS) and neurogenic lower urinary tract dysfunction (NLUTD), and other conditions.
Type:
Grant
Filed:
October 18, 2000
Date of Patent:
April 2, 2002
Assignee:
Recordati, S.A., Chemical and Pharmacueticals Company
Inventors:
Amedeo Leonardi, Gianni Motta, Carlo Riva, Elena Poggesi
Abstract: Novel compounds that are potent and selective inhibitors of PIDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.
Type:
Grant
Filed:
November 17, 2000
Date of Patent:
February 19, 2002
Assignee:
ICOS Corporation
Inventors:
Kerry W. Fowler, Amy Oliver, Joshua Odingo
Abstract: A method for preparing protected, preferably chiral, 5-trityloxymethyl-oxazolidinone in one step directly from optically active 3-hydroxy-4-trityloxy butyramide is described. Oxazolidinones are an important class of molecules in the pharmaceutical industry especially in the areas of antimicrobials and behavioral disorders.
Type:
Grant
Filed:
September 19, 2000
Date of Patent:
September 11, 2001
Assignee:
Board of Trustees operating Michigan State University