Abstract: Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.
Abstract: The present invention is directed to gelatin treated polyhydric alcohol compositions, their preparation, and to pharmaceutical lozenges prepared therefrom. The pre-granulation of a polyhydric alcohol with an aqueous gelatin solution prior to compression, produces lozenges having a delayed rate of dissolution.
Abstract: Controlled release pharmaceutical beads are provided having a multi-layered core and a multi-layered periphery. The core contains at least (A) an inner portion having a suitable organic acid and (B) a sustainably-acid-releasing coating thereover. The periphery contains at least (A) an inner portion having a mixture of at least (i) a pharmaceutical compound and (ii) a surface-active agent, and (B) a sustainably-drug-releasing exterior coating.
Type:
Grant
Filed:
December 22, 1992
Date of Patent:
June 14, 1994
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Kazuo Noda, Yoshiyuki Hirakawa, Hiroyuki Yoshino, David D. MacLaren, Paul F. Skultety, John R. Lefler, Greg M. Beck
Abstract: The present invention relates to the enzymatic resolution of a racemic mixture of stereospecific, pharmaceutically useful in vivo inhibitors of .gamma.-aminobutyric acid transaminase (GABA-T), specifically .gamma.-ethynyl GABA, .gamma.-vinyl GABA and .gamma.-allenyl GABA using penicillin acylase (PA).
Abstract: The present invention is directed towards a process for producing a superior tasting pharmaceutical composition having porous granules produced through in situ gas generation using effervescence-producing ingredients. The method disclosed herein is especially suitable for producing superior tasting antacid tablets as well as superior tasting calcium supplements.
Type:
Grant
Filed:
May 12, 1992
Date of Patent:
April 12, 1994
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Deepak S. Phadke, Melissa P. Neddermeyer
Abstract: Water-dispersible sugar-free powdered, bulk laxative compositions containing cellulose ethers as the active agent are disclosed. These bulk laxative compositions form smooth, palatable dispersions in water which dispersions contain a therapeutically effective amount of the cellulose ether.
Abstract: Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.
Abstract: This invention relates to certain inhibitors of lysyl oxidase and their use in the treatment of diseases and conditions associated with the abnormal deposition of collagen.
Type:
Grant
Filed:
June 10, 1992
Date of Patent:
October 12, 1993
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Michael G. Palfreyman, Philippe Bey, Ian A. McDonald
Abstract: The present invention relates to a group of compounds which are novel substituted alkyl piperidines and which act to inhibit the synthesis of cholesterol in mammals and in fungi.
Type:
Grant
Filed:
March 17, 1992
Date of Patent:
June 8, 1993
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
James R. McCarthy, Charlotte L. Barney, Marion W. Wannamaker
Abstract: The present invention is directed to a process for producing (-) 2-substituted-ornithines comprising contacting a 2-substituted-piperidone with L-.alpha.-E-aminocaprolactam-hydrolas in the presence of a divalent cation.
Abstract: This invention relates to alkoxyimino ether derivatives of 5-acyl-2(1H)-pyridinones and to their use as cardiotonic agents useful in treating cardiac failure, and to the process useful in the preparation thereof.
Type:
Grant
Filed:
June 16, 1992
Date of Patent:
May 18, 1993
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Winton D. Jones, Richard A. Schnettler, Richard C. Dage
Abstract: This invention relates to alkoxyimino ether derivatives of 5-acyl-2(1H)-pyridinones and to their use as cardiotonic agents useful in treating cardiac failure, and to the process useful in the preparation thereof.
Type:
Grant
Filed:
July 29, 1991
Date of Patent:
May 18, 1993
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Winton D. Jones, Richard C. Dage, Richard A. Schnettler
Abstract: Applicants have discovered that certain previously known lactamimide derivatives possess, as a class, valuable calcium channel blocking activity. By virtue of this calcium antagonism activity the compounds are antihypertensives and will have other activities associated with calcium antagonists.
Type:
Grant
Filed:
July 21, 1992
Date of Patent:
March 30, 1993
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Michael G. Palfreyman, Norbert L. Wiech, Hsien C. Cheng, John M. Kane
Abstract: This invention relates to certain inhibitors of lysyl oxidase and their use in the treatment of diseases and conditions associated with the abnormal deposition of collagen.
Type:
Grant
Filed:
March 6, 1991
Date of Patent:
January 26, 1993
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Michael G. Palfreyman, Philippe Bey, Ian A. McDonald
Abstract: The present invention is directed to new de-(acetylglucosaminyl)-di(dehydro)deoxy teicoplanin derivatives which possess antibiotic activity mainly against gram positive bacteria.The new compounds are obtained by chemical modification of a teicoplanin antibiotic substance.
Type:
Grant
Filed:
October 21, 1991
Date of Patent:
November 17, 1992
Assignee:
Gruppo Lepetit S.p.A.
Inventors:
Adriano Malabarba, Pietro Ferrari, Aldo Trani, Giorgio Tarzia
Abstract: Applicants have discovered that certain previously known lactamimide derivatives possess, as a class, valuable calcium channel blocking activity. By virtue of this calcium antagonism activity the compounds are antihypertensives and will have other activities associated with calcium antagonists.
Type:
Grant
Filed:
March 11, 1992
Date of Patent:
October 27, 1992
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Michael G. Palfreyman, Hsien C. Cheng, Norbert L. Wiech, John M. Kane
Abstract: The present invention relates to an apparatus which is able to form a desired number of wells in gelatinous media, as for example agar-based media contained in dishes or plates such as the normal microbiological culture dishes or plates.
Abstract: This invention relates to alkylamino alkylene derivatives of certain 2H-1-benzopyrans useful as plasma cholesterol lowering agents and to their end-use application as therapeutic agents.
Abstract: Applicants have discovered that certain previously known lactamimide derivatives possess, as a class, valuable calcium channel blocking activity. By virtue of this calcium antagonism activity the compounds are antihypertensives and will have other activities associated with calcium antagonists.
Type:
Grant
Filed:
September 23, 1991
Date of Patent:
July 7, 1992
Assignee:
Merrell Dow Pharmaceuticals Inc.
Inventors:
Michael G. Palfreyman, Norbert L. Wiech, Hsien C. Cheng, John M. Kane