Patents Examined by Catherine S. Scalzo
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Patent number: 5457112Abstract: 3-(6-Quinolylmethyl)-4H-imidazol-4-one derivatives corresponding to the formula (I): ##STR1## in which R.sub.1 represents an unbranched or branched (C.sub.2 -C.sub.5) alkyl group,R.sub.2 and R.sub.3 represent, each independently of one another, either a hydrogen atom, or an unbranched or branched (C.sub.1 -C.sub.5)alkyl group, or a (CH.sub.2).sub.n -aryl group where n=0 to 3, or R.sub.2 and R.sub.3 with the imidazole ring can form a spirocyclo(C.sub.3 -C.sub.8)alkyl group,as well as their addition salts with pharmaceutically acceptable acids and bases.Type: GrantFiled: December 13, 1993Date of Patent: October 10, 1995Assignee: SynthelaboInventors: Gerard Cremer, Jean Claude Muller
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Patent number: 5451586Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is hydrogen or (C.sub.1 -C.sub.6)alkyl; R.sup.2 is phenyl, pyridyl, thienyl or furyl, and R.sup.2 may optionally be substituted with from one to three substituents independently selected from (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, chloro, fluoro, bromo, iodo, and trifluoromethyl; R.sup.3 is phenyl, naphthyl, pyridyl, thienyl or furyl, and R.sup.3 may optionally be substituted with from one to three substituents independently selected from (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, chloro, fluoro, bromo, iodo and trifluoromethyl; and the pharmaceutically acceptable salts of such compounds.These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.Type: GrantFiled: December 13, 1993Date of Patent: September 19, 1995Assignee: Pfizer Inc.Inventor: John A. Lowe, III
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Patent number: 5434161Abstract: The imidazopyridines compounds of the present invention are serotonergic 5-HT.sub.3 antagonists. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, gastric stasis, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.Type: GrantFiled: November 6, 1992Date of Patent: July 18, 1995Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moormann, Roger Nosal, Clara I. Villamil
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Patent number: 5356901Abstract: Benzofurancarboxamides having basic substituents, of the formula I ##STR1## in which R.sup.1 and X have the meanings stated in the description, a process for the preparation thereof, and therapeutic agents containing them.Type: GrantFiled: February 16, 1993Date of Patent: October 18, 1994Assignee: BASF AktiengesellschaftInventors: Rainer Schlecker, Hans-Juergen Teschendorf, Liliane Unger
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Patent number: 5300506Abstract: A series of novel indol-3-ylalkyl derivatives of alkoxypyrimidinylpiperazines are disclosed as Formula I. ##STR1## These compounds are intended to be useful agents for alleviation of vascular headache on the basis of their potent affinity and agonist activity at 5-HT1D binding sites.Type: GrantFiled: October 13, 1992Date of Patent: April 5, 1994Assignee: Bristol-Myers Squibb CompanyInventors: David W. Smith, Frank D. Yocca, Joseph P. Yevich, Ronald J. Mattson, Andrew Williams, Edward H. Ruediger
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Patent number: 5281608Abstract: There are disclosed compounds of the formula ##STR1## wherein R is hydrogen, lower alkyl or phenyl;R.sup.1 is hydrogen, lower alkyl, phenyl, halo, hydroxy, lower alkoxy or trifluoromethyl;R.sup.2 is phenyl, phenylloweralkyl, thienyl, furyl, pyrrolyl, pyridyl, benzothienyl, benzofuryl, indolyl, quinolinyl, or any of the foregoing substituted with halo, lower alkyl, lower alkylcarbonyl, benzoyl, carboxy, lower alkoxycarbonyl, OR.sup.3, N(R.sup.3).sub.2, CON(R.sup.3).sub.2, phenylsulfonyl, lower alkylsulfonyl, cyano, nitro or trifluoromethyl;R.sup.3 is hydrogen, lower alkyl or phenyl; ##STR2## R.sup.Type: GrantFiled: August 28, 1992Date of Patent: January 25, 1994Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Robert M. Kearney
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Patent number: 5231181Abstract: The invention provides a process for preparing single enantiomers of compounds represented by the formula: ##STR1## and chiral acid addition salts thereof; wherein: X and Y are independently hydrogen; lower alkyl; lower alkoxy; or halo; or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy;which includes reduction of a compound represented by the formula: ##STR2## to give a mixture of stereoisomers represented by the formula: ##STR3## wherein each wavy line independently represents a bond in either the .alpha. or .beta. position;followed by dissolving the mixture of stereoisomers and a chiral resolving acid in a suitable solvent and allowing the solution to crystallize, giving a salt of the desired enantiomer.Type: GrantFiled: March 21, 1991Date of Patent: July 27, 1993Assignee: Syntex (U.S.A.) Inc.Inventors: Norman H. Dyson, John O. Gardner, John C. Rohloff
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Patent number: 5015655Abstract: Compounds useful in the treatment of Alzheimers's disease, senile dementia or memory disorders of the aged of the formula ##STR1## in which n represents the number 1, 2 or 3,R.sub.1 and R.sub.2, identical or different, represent hydrogen, a linear, branched or cyclic alkyl, alkenyl, or alkynyl which contain up to 6 carbon atoms, R.sub.1 and R.sub.2 optionally substituted by hydroxy, alkoxy containing up to 6 carbon atoms, aralkyl containing up to 14 carbon atoms, a COOalk.sub.1 radical in which alk.sub.1 represents alkyl containing up to 6 carbon atoms, a --CON(alk.sub.2).sub.2 radical in which alk.sub.2 represents alkyl containing up to 6 carbon the radical --C(R.sub.1).dbd.NOR.sub.2 being in position 2, 3 or 4, in all their isomer forms and their mixture, as well as their addition salts with pharmaceutically acceptable organic or mineral acids. Also therapeutic compositions containing the compounds, method of treatment and method of preparation.Type: GrantFiled: October 26, 1989Date of Patent: May 14, 1991Assignee: Roussel UCLAFInventors: Giulio Galliani, Fernando Barzaghi, Carla Bonetti, Emilio Toja
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Patent number: 4939160Abstract: Hydropyridine derivatives of the formula ##STR1## in which R.sub.1 represents carboxy, lower alkoxycarbonyl, carbamoyl, N-lower alkylcarbamoyl or N,N-di-lower alkylcarbamoyl, R.sub.2 represents hydrogen, an optionally etherified or acylated hydroxy group or an optionally acylated amino group, and R.sub.3 represents a radical of the formula R- (Ia), R-alk.sub.1 - (Ib) or R'=alk.sub.2 - (Ic) in which R represents a benzocycloalkenyl radical having a total of from 8 to 12 ring carbon atoms which is bonded via a saturated carbon atom and which is unsubstituted or is mono- or poly-substituted in the benzo moiety by hydroxy, lower alkoxy, lower alkanoyloxy, halogen, lower alkyl and/or by trifluoromethyl, and/or substituted in the .alpha.Type: GrantFiled: December 9, 1988Date of Patent: July 3, 1990Assignee: Ciba-Geigy CorporationInventors: Georg von Sprecher, Wolfgang Frostl, Armin Zust
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Patent number: 4929624Abstract: Novel 1-substituted 1H-imidazo-[4,5-c]quinolin-4-amines are disclosed. These compounds function as antiviral agents, and they are potential synthetic intermediates in the preparation of known antiviral agents and labeled known antiviral agents. This invention also provides intermediates for preparing such compounds, pharmaceutical compositions containing such compounds, and pharmacological methods of using such compounds.Type: GrantFiled: March 23, 1989Date of Patent: May 29, 1990Assignee: Minnesota Mining and Manufacturing CompanyInventors: John F. Gerster, Roy T. Knafla
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Patent number: 4919843Abstract: The invention relates to antifoam compositions containing an essentially linear organopolysiloxane, a silicone resin containing essentially triorganosiloxy and SiO.sub.4/2 units, and a filler.Type: GrantFiled: July 22, 1988Date of Patent: April 24, 1990Assignee: Wacker-Chemie GmbHInventors: Ernst Innertsberger, Jakob Schmidlkofer, Peter Huber, Willibald Burger, Joachim Schulze
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Patent number: 4913544Abstract: A plastic organic photochromic article, typically a lens such as an ophthalmic lens or a window such as a vehicle roof light, comprisig a plastics host material having a photochromic compound incorporated therein or applied thereto, the article exhibiting the following properties, measured at Air Mass 2 at 25.degree. C.:(a) an integrated visible transmission in the faded state (B.IVT) ranging from 90 to 25%,(b) an integrated visible transmission in the darkened state (D.IVT) ranging from 1 to 50%, preferably 4 to 30%,(c) the rate of darkening of the article when it is exposed to actinic radiation is such that 88% of the darkening range is achieved in 30 seconds or less, i.e. T.sub.88 .ltoreq.30 secs,(d) the rate of fading of the article from its fully darkened condition is such that more than 60% of the optical density range is recovered in 60 seconds, i.e. % ODG-1.gtoreq.60%, and(e) the induced optical density of the article, i.e.Type: GrantFiled: May 1, 1987Date of Patent: April 3, 1990Assignee: Pilkington plcInventors: Martin Rickwood, John D. Hepworth