Abstract: Processes for preparing dihydro-prostacyclin analogs, which are 9-deoxy-5,9-cyclic ethers of prostaglandin F.sub.1 .alpha.-type compounds, illustrated, for example, by a compound of the formula ##STR1## wherein .about. indicates alpha or beta configuration; including the products and intermediates produced therein, said products having pharmacological utility.
Abstract: Processes for preparing dihydro-prostacyclin analogs, which are 9-deoxy-5,9-cyclic ethers of prostaglandin F.sub.1 .alpha.-type compounds, illustrated, for example, by a compound of the formula ##STR1## wherein .about. indicates alpha or beta configuration; including the products and intermediates produced therein, said products having pharmacological utility.
Abstract: The present invention provides novel pyridinyl-benzofurans and derivatives thereof which are useful as thromboxane A.sub.2 (TXA.sub.2) synthetase inhibitors and as such represent potent pharmacological agents.
Abstract: Processes for preparing dihydro-prostacyclin analogs, which are 9-deoxy-5,9-cyclic ethers of prostaglandin F.sub.1 .alpha.-type compounds, illustrated, for example, by a compound of the formula ##STR1## wherein .about. indicates alpha or beta configuration; including the products and intermediates produced therein, said products having pharmacological utility.
Abstract: Processes for preparing dihydro-prostacyclin analogs, which are 9-deoxy-5,9-cyclic ethers of prostaglandin F.sub.1 .alpha.-type compounds, illustrated, for example, by a compound of the formula ##STR1## wherein .about. indicates alpha or beta configuration; including the products and intermediates produced therein, said products having pharmacological utility.
Abstract: The present invention provides novel 2-, 3-, or 4-pyridinylmethylamino arylic acids which are useful as thromboxane A.sub.2 (TXA.sub.2) synthetase inhibitors and 5-lipoxygenase inhibitors and as such represent useful pharmacological agents.
Abstract: Potent cell growth inhibitory substances have been obtained from the Indian Ocean sea hare Dolabella. These substances have been given the names dolastatin A and dolastatin B. These compounds are characterized by physical and chemical parameters.
Abstract: The present invention provides novel methods of inducing diuresis and/or an antihypertensive effect employing certain 2,6-diaryl-4-pyridinecarboxylic acid derivatives. Also provided are novel compositions to be used in these methods.
Abstract: The present invention provides novel 1-(6-hydroxy-4- or 7-methoxy or 4,7-dimethoxy-5-benzofuranyl)-4-substituted-1,3-butanediones which are useful as intermediates in the synthesis of khellin and related anti-atherosclerotic furochromones.
Abstract: The present invention provides a total synthesis of known intermediates useful in the synthesis of khellin and antiatherosclerotic analogs thereof from pyrogallol. Pyrogallol is converted to 3,6,7-benzofurantriol triacetate using zinc chloride and chloracetanitrile, then catalytically reduced and deactoxylated at the 3 position to yield the corresponding 2,3-dihydrofuran. This substance is subjected to a Fries rearrangement to the corresponding diol, the phenolic hydroxyl group of which is then selectively alkylated. This yields 6-hydroxy-7-alkoxy-5-benzofuranyl methyl ketone, a known intermediate for the production of 4-desmethoxy khellin and analogs thereof. This compound is then selectively alkoxylated at the 4 position using lead tetraacetate or thallium (III) nitrate in an alkanol solvent to yield known chemical intermediates in the preparation of khellin and analogs thereof.
Abstract: This specification concerns the use to treat hypertension in mammals of novel and known 4H-s-triazolo[4,3-a][1,4]benzodiazepines, known 4H-s-triazolo[4,3-a][1,3,4]benzotriazepines and 2,4-dihydro-2-alkyl-1H-s-triazolo[4,3-a][1,4]benzodiazepin-1-ones, and novel 2,4-dihydro-2-alkyl-1H-s-triazolo[4,3-a][1,4]benzodiazepin-1-thiones.
Abstract: The present invention provides novel pyridinyl-benzofurans and derivatives thereof which are useful as thromboxane A.sub.2 (TXA.sub.2) inhibitors and as such represent potent pharmacological agents.
Abstract: The present invention provides novel imidazolyl-benzofurans and derivatives thereof which are useful as thromboxane A.sub.2 (TXA.sub.2) synthetase inhibitors and as such represent potent pharmacological agents.
Type:
Grant
Filed:
September 30, 1982
Date of Patent:
June 5, 1984
Assignee:
The Upjohn Company
Inventors:
Roy A. Johnson, Chiu-Hong Lin, Gordon L. Bundy
Abstract: The present invention provides novel dibenzo diazocines which are useful as thromboxane A.sub.2 (TXA.sub.2) synthetase inhibitors and as such represent potent pharmacological agents.
Abstract: The present invention provides novel imidazolyl-benzothiophenes and derivatives thereof which are useful as thromboxane A.sub.2 (TXA.sub.2) synthetase inhibitors and as such represent potent pharmacological agents.
Abstract: The present specification provides novel analogs of khellin, a natural product, which are useful in the treatment and prevention of atherosclerosis. Particularly, the present disclosure provides novel 5H-furo[3,2-g]-benzopyran-5-one substituted at the four and nine positions by methoxy or optionally substituted at the four position by hydroxy or alkoxy groups other than methoxy, certain 7-(N,N-dialkylaminoethen-2-yl substituted compounds. Also provided are certain novel antiatherosclerotic 7H-furo[3,2-g][1]benzopyrans.
Abstract: The present specification provides a total synthesis of known intermediates useful in the synthesis of khellin and antiatherosclerotic analogs thereof. 3-Furoic acid is treated with succinic anhydride and diesterified to 3-carboxy-.delta.-oxo-2-furanbutanoic acid bis (alkyl ester). Following amination, cyclization and bis methylation, 6-formyl-4,7-dimethoxy-5-benzofurancarboxcyclic acid alkyl ester is prepared. This compound is then converted to known intermediates in the synthesis of khellin and analogs. Further, the present invention provides numerous novel anti-atherosclerotic 4,9-di-(C.sub.2 -C.sub.4)-alkoxyfurochromones.