Ching-San Lai - Encinitas CA Tingmin Wang - San Marcos CA
Assignee:
Medinox, Inc. - San Diego CA
International Classification:
C07D20704
US Classification:
514423, 514 2, 514514, 530402, 548565, 548573
Abstract:
In accordance with the present invention, there are provided conjugates of nitric oxide scavengers (e. g. , dithiocarbamates, or âDCâ) and pharmacologically active agents (e. g. , NSAIDs). Invention conjugates provide a new class of pharmacologically active agents (e. g. , anti-inflammatory agents) which cause a much lower incidence of side-effects due to the protective effects imparted by modifying the pharmacologically active agents as described herein. In addition, invention conjugates are more effective than unmodified pharmacologically active agents because cells and tissues contacted by the pharmacologically active agent(s) are protected from the potentially damaging effects of nitric oxide overproduction induced thereby as a result of the co-production of nitric oxide scavenger (e. g. , dithiocarbamate), in addition to free pharmacologically active agent, when invention conjugate is cleaved.
C3²-Methylene Hydrogen Phosphonate Monomers And Related Compounds
Phillip Dan Cook - Fallbrook CA Haoyun An - Carlsbad CA Tingmin Wang - San Marcos CA Muthiah Manoharan - Carlsbad CA
Assignee:
ISIS Pharmaceuticals, Inc. - Carlsbad CA
International Classification:
C07H 2100
US Classification:
536 253
Abstract:
The present invention is directed to nucleoside monomers wherein the 3â-O atom is replaced with a methylene group. The present invention also provides oligomers comprising a plurality of such monomers which are linked by methylenephosphonate linkages. Further, methods of preparing monomers and oligomers according to the present invention are provided.
Modified Forms Of Pharmacologically Active Agents And Uses Therefor
In accordance with the present invention, there are provided modified forms of nonsteroidal anti-inflammatory drugs (NSAIDs). Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.
Hydroxamate Derivatives Of Non-Steroidal Anti-Inflammatory Drugs
In accordance with the present invention, there are provided novel chemical entities which have multiple utilities, e. g. , as prodrugs of NSAIDs; as dual inhibitors of cyclooxygenase (COX) and 5-lipoxygenase (5-LO); as anticancer agents (through promoting apoptosis and/or inhibiting the matrix metalloproteinases (MMPs)), and the like. Invention compounds comprise a non-steroidal anti-inflammatory agent (NSAID), covalently linked to a hydroxamate. Invention compounds are useful for a variety of applications, such as, for example, treating inflammation and inflammation-related conditions; reducing the side effects associated with administration of anti-inflammatory agents; promoting apoptosis; inhibiting matrix metalloproteinases; and the like.
Protected Forms Of Pharmacologically Active Agents And Uses Therefor
Ching-San Lai - Encinitas CA Tingmin Wang - San Marcos CA Vassil P. Vassilev - San Diego CA
Assignee:
Medinox, Inc. - San Diego CA
International Classification:
A61K 3116
US Classification:
514599, 514423, 514514, 514706, 558235
Abstract:
In accordance with the present invention, there are provided conjugates of dithiocarbamates âDCâ) and pharmacologically active agents (e. g. , NSAIDs). Invention conjugates provide a new class of pharmacologically active agents (e. g. , anti-inflammatory agents) which cause a much lower incidence of side-effects due to the protective effects imparted by modifying the pharmacologically active agents as described herein.
Protected Forms Of Pharmacologically Active Agents And Uses Thereof
In accordance with the present invention, there are provided normal modified forms of nonsteroidal anti-inflammatory drugs. Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.
P-Toluene Sulfonic Acid Salt Of 5-Amino-3-(2′-O-Acetyl-3′-Deoxy-Β-D-Ribofuranosyl)-3H-Thiazole[4,5-D]Pyrimidine-2-One And Methods For Preparation
David Kucera - Del Mar CA, US Gregory J. Haley - San Diego CA, US Erik J. Rueden - San Diego CA, US Tingmin Wang - San Diego CA, US Fritz Blatter - Reinach BL, DE Martin Viertelhaus - Basel, DE
Assignee:
Anadys Pharmaceuticals, Inc. - San Diego CA
International Classification:
C07H 19/00 A61K 31/70 A01N 43/04
US Classification:
514 45, 536 272
Abstract:
The present disclosure relates to p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-beta-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and to its use in treating conditions such as viral infections, tumors, and cancer. Also disclosed is a method of preparing the p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-β-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and methods for producing furanose compounds which are useful intermediates in the preparation of pharmaceutical compounds such as p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-β-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and the like.
David Kucera - Del Mar CA, US Gregory J. Haley - San Diego CA, US Erik J. Rueden - Belmont CA, US Tingmin Wang - San Diego CA, US
Assignee:
Anadys Pharmaceuticals, Inc. - San Diego CA
International Classification:
C07H 1/08
US Classification:
536124
Abstract:
The present disclosure relates to methods for preparing furanose compounds of Formula (3), which are useful as intermediates in the preparation of a p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-beta-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and the like.
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