Patents Examined by Bernard I. Dentz
  • Patent number: 4822804
    Abstract: Pharmaceutically useful compounds are 5,6,7-trinor-4,8-inter-m-phenylene PGI.sub.2 derivatives such as5,6,7-trinor-4,8-inter-m-phenylene-2-nor-16,16-dimethyl PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2-nor-17(S)-methyl PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2-nor-17(R)-methyl PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2-nor-16,16-dimethyl-.omega.-homo PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2-nor-17(S)-methyl-.omega.-homo PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2-nor-17(R)-methyl-.omega.-homo PGI.sub.2,5,6, 7-trinor-4,8-inter-m-phenylene-2,17,18,19,20-pentanor-16,16-dimethyl-16-p ropoxy PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2,18,19,20-tetranor-16,16-dimethyl-17-et ho xy PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2,18,19,20-tetranor-16,16-dimethyl-17-pr op oxy PGI.sub.2,5,6,7-trinor-4,8-inter-m-phenylene-2,17,18,19,20-pentanor-16-phenoxy PGI.sub.2 and methyl esters thereof.5,6,7-trinor-4,8-inter-m-phenylene-2,17,18,19,20-pentanor-16,16-dimethyl-16 -phenoxy PGI.sub.
    Type: Grant
    Filed: September 29, 1987
    Date of Patent: April 18, 1989
    Assignee: Toray Industries, Inc.
    Inventors: Kiyotaka Ohno, Hiroshi Nagase, Mamoru Ishikawa, Kazuhisa Matsumoto, Shintaro Nishio
  • Patent number: 4822795
    Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein L is NH or O;X is N or CR.sub.3 wherein R.sub.3 is hydrogen or C.sub.1-6 alkoxy;Y is N or CR.sub.4 wherein R.sub.4 is hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-6 alkylsulphonyl, C.sub.1-6 alkylsulphinyl, C.sub.1-7 acyl, cyano, C.sub.1-6 alkoxycarbonyl, C.sub.1-7 acylamino, hydroxy, nitro or amino, aminocarbonyl, or aminosulphonyl, optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, and C.sub.3-8 cycloalkyl C.sub.1-4 alkyl or disubstituted by C.sub.4 or C.sub.5 polymethylene; phenyl or phenyl C.sub.1-4 alkyl group optionally substituted in the phenyl ring by one or two of halogen, C.sub.1-6 alkoxy or C.sub.1-6 alkyl groups;R.sub.1 and R.sub.2 are independently selected from hydrogen, or halogen;Z is a group of formula (a), (b) or (c): ##STR2## wherein n is 2 or 3; p is 1 or 2; q is 1 to 3; r is 1 to 3; andR.sub.5 or R.sub.
    Type: Grant
    Filed: July 27, 1987
    Date of Patent: April 18, 1989
    Assignee: Beecham Gropup p.l.c.
    Inventor: Francis D. King
  • Patent number: 4822803
    Abstract: Compounds of the Formula I: ##STR1## and pharmaceutically acceptable salts thereof are inhibitors of leukotriene biosynthesis. These compounds inhibit the mammalian 5-lipoxygenase enzyme, thus preventing the metabolism of arachidonic acid to the leukotrienes. These compounds are thus useful in the treatment of asthma, allergic disorders, inflammation, skin diseases and certain cardiovascular disorders.
    Type: Grant
    Filed: February 4, 1988
    Date of Patent: April 18, 1989
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Joseph G. Atkinson, Yvan Guindon, Cheuk K. Lau
  • Patent number: 4818754
    Abstract: A compound of the formula (1) or a salt or solvate thereof: ##STR1## in which: R.sub.0 is hydrogen or C.sub.1-6 alkyl;R.sub.1 and R.sub.2 are both hydrogen; orR.sub.1 is hydrogen, C.sub.1-6 alkyl; and R.sub.2 is CN; CR.sub.5 R.sub.6 Y where R.sub.5 and R.sub.6 are independently selected from hydrogen and C.sub.1-4 alkyl and Y is selected from hydrogen, OR.sub.7 or SR.sub.7 where R.sub.7 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, and NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkanoyl or together are C.sub.4-6 polymethylene; or COR.sub.10 is OH or C.sub.1-4 alkyl, or COR.sub.10 is a pharmaceutically acceptable ester or amide; orR.sub.2 is hydrogen, C.sub.1-6 alkyl, or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; and R.sub.1 is CN, CR.sub.5 R.sub.6 Y or COR.sub.10 as defined for R.sub.2 above; orR.sub.1 and R.sub.2 together form C.sub.3 -C.sub.
    Type: Grant
    Filed: April 16, 1987
    Date of Patent: April 4, 1989
    Assignee: Beecham Group p.l.c. of Beecham House
    Inventors: Robert W. Ward, Roger E. Markwell, Ian Hughes
  • Patent number: 4816592
    Abstract: A process for the production of benzofuran derivatives having the general formula, ##STR1## wherein R is alkyl, in particular of 2,3-dihydro-2,2-dimethyl benzofuran-7-ol, starting from pyrocatechol ethers in one step operation.The process essentially consists of heating a solution of pyrocatechol ether in an inert organic solvent in the presence of a catalyst comprising metals of 3.degree. and 4.degree. group of the Periodic System in form of carboxylates or of modified zeolites.The products are known intermediates for the production of insecticides.
    Type: Grant
    Filed: January 31, 1984
    Date of Patent: March 28, 1989
    Assignee: Enichem Sintesi Spa
    Inventors: Paolo Maggioni, Francesco Minisci, Mariano Correale
  • Patent number: 4816579
    Abstract: A process is provided for preparing a 7-oxabicycloheptane amino alcohol intermediate of the general structure ##STR1## (wherein the above structure represents (D) of (L) isomers) which is useful in preparing thromboxane A.sub.2 receptor antagonists. This intermediate is prepared by reacting mesoanhydride with an aryl amine ##STR2## wherein R is alkyl, CH.sub.2 OH, CO.sub.2 H or CO.sub.2 alkyl, to form the acid ##STR3## which is reduced by treatment with lithium aluminum hydride or diisobutylaluminum hydride or Red-Al to form the alcohol ##STR4## wherein R.sup.1 is CH.sub.2 OH when R is CO.sub.2 H, CO.sub.2 alkyl or CH.sub.2 OH, and R.sup.1 is alkyl; where in the above alcohol R.sup.1 is CH.sub.2 OH, such alcohol compound is treated with an alkyl chloroformate in the presence of base such as an alkali metal alkoxide to form the alcohol ##STR5## which undergoes cleavage by treatment with alkali metal, ammonia and acid to form the amino alcohol intermediate.Where in the above alcohol R.sup.
    Type: Grant
    Filed: January 27, 1988
    Date of Patent: March 28, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John K. Thottathil
  • Patent number: 4816481
    Abstract: Disclosed herein is a cerebral-circulation-metabolism-function-improving agent which contains a 2,6-diphenyl-3,7-dioxabicyclo[3.3.0]octane derivative represented by the following formula as the effective ingredient: ##STR1## wherein, each of R.sub.1, R.sub.3, R.sub.4 and R.sub.6 represents a hydrogen atom or a lower alkoxyl group; each of R.sub.2 and R.sub.5 represents a hydrogen atom, a .beta.-D-glucosyl group or a hydroxyl group; and each of R.sub.7 and R.sub.8 represents an oxygen atom or two hydrogen atoms.
    Type: Grant
    Filed: July 21, 1987
    Date of Patent: March 28, 1989
    Assignee: Wakunaga Seiyaku Kabushiki Kaisha
    Inventors: Naoyuki Takasugi, Mitsuyasu Ushijima, Satoshi Inoue, Terukage Hirata
  • Patent number: 4810488
    Abstract: A method for preparing a stable aerosol formulation of beclomethasone dipropionate in which the steroid is contacted with an alcohol containing 1 to 5 carbon atoms to form a crystalline solvate therewith, the crystalline material so formed being reduced to a particle size below 10 microns and thereafter dispersed in a composition comprising chlorofluorocarbon propellents.
    Type: Grant
    Filed: August 18, 1986
    Date of Patent: March 7, 1989
    Assignee: Riker Laboratories, Inc.
    Inventor: Philip A. Jinks
  • Patent number: 4810803
    Abstract: A process is disclosed for the improvement of a vanadium-phosphorus-oxygen catalyst or a vanadium-phosphorus-oxygen-co-metal catalyst suitable for use in the manufacture of maleic anhydride from butane, which process comprises applying in situ water and a phosphorus compound in an amount to partially deactivate a portion of the catalyst in a catalyst bed containing an exotherm of reaction which was present in the catalyst bed prior to the addition of the phosphorus compound, thereby moving the exotherm downstream into the catalyst bed and thus improving the catalyst.These catalysts are useful for the manufacture of maleic anhydride from butane feedstock.
    Type: Grant
    Filed: December 9, 1987
    Date of Patent: March 7, 1989
    Assignee: Amoco Corporation
    Inventor: Robert C. Edwards
  • Patent number: 4808594
    Abstract: An imidazopyridine of formula (I) ##STR1## in which: either X is CH.sub.3 and Y is CH.sub.2 OR,or, X is CH.sub.2 OR and Y is CH.sub.3,R is a C.sub.1-6 alkyl group,R.sub.1 is a C.sub.1-3 alkyl group, andR.sub.2 is a C.sub.1-3 alkyl group, has useful anxidytic and hypnotic properties.
    Type: Grant
    Filed: November 3, 1987
    Date of Patent: February 28, 1989
    Assignee: Synthelabo
    Inventors: Pascal George, John Allen
  • Patent number: 4808627
    Abstract: A method is provided for preventing or treating toxemia during pregnancy by administering a thromboxane A.sub.2 receptor antagonist before or during toxemia.
    Type: Grant
    Filed: December 16, 1987
    Date of Patent: February 28, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Martin L. Ogletree
  • Patent number: 4808734
    Abstract: 16-Cycloalkyl-7-fluoro prostacyclins having a 16 lower alkyl or fluoro substituent useful as blood platelet anti-aggregating agent, vasodilators, cyto protective lowering agents, anti-ulcerogenic agent and for treating peripheral vascular diseases such as schleroderma.
    Type: Grant
    Filed: December 1, 1986
    Date of Patent: February 28, 1989
    Assignee: Hoffmann-La Roche Inc.
    Inventors: George W. Holland, Perry Rosen, Hans Maag, Ferdinand Lee
  • Patent number: 4808588
    Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein: Het is monocyclic heteroaryl having two adjacent carbon atoms, a and b, depicted in formula (I); p1 R.sub.1 and R.sub.2 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl and C.sub.1-6 Alkoxy;R.sub.3 is hydroxy, C.sub.1-6 alkoxy, C.sub.3-7 alkenyl-methoxy, phenoxy or phenyl C.sub.1-4 alkoxy in which either phenyl moiety may be substituted by one or two C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halo; CO.sub.2 R.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl, CONR.sub.7 R.sub.8 or SO.sub.2 NR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are independently hydrogen or C.sub.1-6 alkyl or together are C.sub.4-6 polymethylene, NO.sub.2, (CH.sub.2).sub.m OR.sub.9 wherein m is 1 or 2 and R.sub.9 is C.sub.1-6 alkyl or S(O).sub.n R.sub.10 wherein n is 0, 1 or 2 and R.sub.10 is C.sub.
    Type: Grant
    Filed: July 30, 1987
    Date of Patent: February 28, 1989
    Assignee: Beecham Group, p.l.c.
    Inventor: Francis D. King
  • Patent number: 4808595
    Abstract: Furopyridine sulfonamides are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure and disorders associated therewith such as glaucoma.
    Type: Grant
    Filed: May 5, 1988
    Date of Patent: February 28, 1989
    Assignee: Merck & Co., Inc.
    Inventor: Jacob M. Hoffman, Jr.
  • Patent number: 4808596
    Abstract: Imidazo[4,5-b]pyridine compounds of the general formula [I] are provided: ##STR1## where R.sup.1 is straight-chain or branched C.sub.1-8 alkoxy which may be substituted with cycloalkyl, or C.sub.2-4 fluoroalkyloxy, R.sup.2 is H, methyl or methoxy, and R.sup.3 and R.sup.4 are each H or methyl and may be the same or different. All these compounds have good activity of inhibiting potassium ion-dependent adenosine triphosphatase and excellent storage stability, so that they are usable for the treatment of gastric and/or duodenal ulcers.
    Type: Grant
    Filed: July 24, 1987
    Date of Patent: February 28, 1989
    Assignee: Tokyo Tanabe Company, Ltd.
    Inventors: Naoto Matsuishi, Haruki Takeda, Kenichi Iizumi, Kiyokazu Murakami, Akira Hisamitsu
  • Patent number: 4806560
    Abstract: Imidazo[4,5-b]pyridin-2-one derivatives of the formula (I) ##STR1## in which n is 2, 3 or 4, x is .dbd.CH-- or .dbd.N--, R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen, halogen or (C.sub.1-4) alkoxy and either R.sub.3 is H or OH and R.sub.4 is H, or R.sub.3 and R.sub.4 together form a direct bond, their enantiomers and their addition salts with pharmaceutically acceptable acids are pharmacologically active, for example as antagonists to histamine and serotonin.
    Type: Grant
    Filed: October 7, 1987
    Date of Patent: February 21, 1989
    Assignee: Synthelabo
    Inventors: Philippe Manoury, Jean Binet, Elisabeth Dewitte
  • Patent number: 4806663
    Abstract: The disclosure relates to compounds of the formula ##STR1## and pharmaceutically acceptable addition salts thereof wherein R.sub.1 represents hydrogen, R.sub.1 represents a group having the formula --OR.sub.2 in which R.sub.2 is a lower alkyl group or an aryl group, or R.sub.1 represents a group having the formula ##STR2## in which R.sub.3 is hydrogen, a lower alkyl group, or an aryl group, wherein R.sub.4 is a lower alkyl group containing 1 to 6 carbon atoms, wherein R.sub.5 is either hydrogen or methyl, wherein NR.sub.6 is a group selected from the class consisting of amino, lower mono and dialkylamino, piperidino, pyrrolidino, and morpholino groups and wherein Y.sub.1 and Y.sub.2 are identical and are hydrogen or a halogen. Compounds in accordance with the invention are useful as vasodilators and as antiarrythmic agents.
    Type: Grant
    Filed: April 6, 1987
    Date of Patent: February 21, 1989
    Assignee: The University of Tennessee Research Corporation
    Inventors: Thomas P. Kennedy, George W. Kabalka
  • Patent number: 4803219
    Abstract: N,N-dimethyl-N'-benzoyl-N'-(2,3-dihydrobenzofuran-2-ylmethyl)1,3-propanedia mine of formula: ##STR1## and its pharmaceutically acceptable salts, in racemic form or in the form of enantiomers, which compounds have anti-arrhythmic properties.
    Type: Grant
    Filed: July 21, 1987
    Date of Patent: February 7, 1989
    Assignee: RIOM Laboratories C.E.R.M.
    Inventors: Michel Combourieu, Nadine Simbille, Marie-Paule Landes, Yvon Bernet
  • Patent number: 4803199
    Abstract: The dicarboxylic, heterocyclic and substituted benzoic acid alkylene bridged piperidyl amides and esters are serotonin M antagonists.
    Type: Grant
    Filed: November 25, 1987
    Date of Patent: February 7, 1989
    Inventors: Peter Donatsch, Gunter Engel, Bruno Hugi, Brian P. Richardson, Paul A. Stadler, deceased, by Hildegard R. Stadler, heir, by Brigitte M. Stadler, heir, by Sigrid A. Stadler, heir, by Gerald Breuleux, legal representative
  • Patent number: 4803276
    Abstract: Novel 1-(imidazo[1,2-a]pyridin-6-yl)-2-alkanone derivatives and (imidazo [1,2-a]pyridin-6-yl) acetaldehyde derivatives are provided. The novel derivatives are intermediates for the production of 5-(6-imidazo[1,2-a]pyridyl)pyridine derivatives which are useful as cardiotonics.
    Type: Grant
    Filed: October 9, 1987
    Date of Patent: February 7, 1989
    Assignee: Eisai Co., Ltd.
    Inventors: Motosuke Yamanaka, Kazutoshi Miyake, Shinji Suda, Hideto Ohhara, Toshiaki Ogawa