Patents Examined by Lenora Miltenberger
  • Patent number: 5236928
    Abstract: There are disclosed substituted imidazole derivatives of Formula I bearing acidic functional groups which are useful as angiotensin II antagonists.
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: August 17, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Prasun K. Chakravarty, William J. Greenlee, Arthur A. Patchett
  • Patent number: 5225424
    Abstract: N-[5-(aminosulfonyl)-3-methyl-1,3,4-thiadiazol-2(3H)ylidene] -2-acetyloxyacetamide, commonly referred to as acetylhydroxymethazolamide and is a water soluble pharmacologically active carbonic anhydrase inhibitor.
    Type: Grant
    Filed: October 21, 1992
    Date of Patent: July 6, 1993
    Assignee: University of Iowa Research Foundation
    Inventors: Ronald D. Schoenwald, Charles F. Barfknecht
  • Patent number: 5225567
    Abstract: Heterocyclic acetylenic amine compounds having the following structural formula ##STR1## where X is ##STR2## having cholinergic agonist or antagonist activity useful in the treatment of mental disorders, extrapyramidal motor disorders, disorders of the parasympathetic nervous system and glaucoma or as analgesics for the treatment of pain. Typical central nervous system disorders for which the subject compounds can be used include cognitive disorders of all ages, including senile dementia, Alzheimer's disease and other related disorders. The compounds are particularly developed to improve mental performance when a mental deficiency is diagnosed.
    Type: Grant
    Filed: July 30, 1992
    Date of Patent: July 6, 1993
    Assignee: The Upjohn Company
    Inventors: Malcolm W. Moon, Richard F. Heier
  • Patent number: 5225431
    Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein R, R.sup.1 and R.sup.2 are independently selected from hydrogen and C.sub.1-4 alkyl;R.sup.3 and R.sup.4 are independently selected from hydrogen, C.sub.1-6 alkyl (including cycloalkyl) and aryl (wherein the alkyl or aryl group, which latter includes benzyl, is optionally substituted by one or more atoms or groups independently selected from halogen, C.sub.1-4 alkyl and aryl), provided R.sup.3 benzyl or substituted benzyl when R.sup.4 =H;m is an integer of from 0 to 2;n is an integer of from 0 to 3;(W) is a group of formula (i), (ii), (iii), or (iv) ##STR2## wherein Y is selected from oxygen, methylene and >N--R.sup.5, where R.sup.5 is hydrogen, C.sub.1-4 alkyl, or benzyl, Z and Z' are independently selected from >C.dbd.O, >C.dbd.
    Type: Grant
    Filed: February 26, 1991
    Date of Patent: July 6, 1993
    Assignee: Burroughs Wellcome Co.
    Inventors: Alan D. Robertson, Graeme R. Martin, Janet S. Buckingham
  • Patent number: 5225563
    Abstract: A photochromatic compound represented by the following general formula (I): ##STR1## where: R.sub.1 and R.sub.2 independently represent a linear, branched or cyclic C1-C10 alkyl radical, H, OH, F, Cl, Br, NH.sub.2, N(R.sub.4).sub.2, COOH, OR.sub.4 or COOR.sub.4 where R.sub.4 is a C1-C10 linear, branched or cyclic alkyl radical, or an aryl radical;R.sub.3 is a variously substituted mono or polycondensed heterocyclic or aryl radical.A compound (I) demonstrates marked photochromatic characteristics both when in an organic solvent solution and when incorporated into polymer matrices.
    Type: Grant
    Filed: December 18, 1990
    Date of Patent: July 6, 1993
    Assignee: Enichem Synthesis S.p.A.
    Inventors: Carlo Neri, William Giroldini, Antonio Rinaldi, Luciana Crisci
  • Patent number: 5223525
    Abstract: The invention describes novel 1-arylimidazoles of formula (I) ##STR1## wherein typically preferred substituents are: X is S(O).sub.n R.sub.1, in which R.sub.1 is an alkyl group, preferably a methyl group, which is fully substituted by halogen atoms, and n is 0, 1 and 2;Y is hydrogen, halogen, alkyl, alkoxy, alkoxyalkylideneimino, alkylsulfenyl, alkylsulfinyl or alkylsulfonyl;Z is hydrogen, halogen, alkyl, preferably methyl; andR.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are individually hydrogen, halogen or an unsubstituted or halo-substituted alkyl, alkoxy, alkylsulfenyl, alkylsulfinyl or alkylsulfonyl.The invention further describes intermediates and processes to make the compounds, compositions of the compounds, and methods of use of the compounds for the control of arthropods (especially mites, aphids or insects), nematodes, helminths, or protozoa.
    Type: Grant
    Filed: October 31, 1990
    Date of Patent: June 29, 1993
    Assignee: Rhone-Poulenc AG Company
    Inventors: Tai-Teh Wu, David N. Sinodis, Philip R. Timmons, Gail S. Powell, David T. Chou, Peter W. Newsome, Lee S. Hall
  • Patent number: 5219856
    Abstract: Novel heterocycle substituted imidazoles of Formula (I), which are useful as angiotensin-II antagonists, are disclosed: ##STR1##
    Type: Grant
    Filed: April 6, 1992
    Date of Patent: June 15, 1993
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Richard E. Olson
  • Patent number: 5217985
    Abstract: Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney.
    Type: Grant
    Filed: August 28, 1990
    Date of Patent: June 8, 1993
    Assignee: G. D. Searle & Co.
    Inventors: David B. Reitz, Robert E. Manning
  • Patent number: 5217986
    Abstract: The compound of the formula ##STR1## is described. This compound is active in an H.sub.3 receptor assay and is an H.sub.3 antagonist. Accordingly, the compound of formula I is useful in the treatment of diseases and conditions such as asthma, rhinitis, airway congestion, inflammation, cardiac arrhythmias, hypertension, hyper and hypo motility and acid secretion of the gastrointestinal tract, hypo and hyper activity of the central nervous system (CNS), migraine, and glaucoma.
    Type: Grant
    Filed: March 26, 1992
    Date of Patent: June 8, 1993
    Assignee: Harbor Branch Oceanographic Institution, Inc.
    Inventors: Shirley A. Pomponi, Vincent P. Gullo, Ann C. Horan, Mahesh G. Patel, Stephen Coval
  • Patent number: 5216008
    Abstract: The present invention is directed to a new class of arylalkoxyphenoxy-imidazoline compounds and their use for the treatment of depression, anxiety, hypertension, and migraine headaches.
    Type: Grant
    Filed: February 6, 1992
    Date of Patent: June 1, 1993
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Jules Freedman, Bruce M. Baron, Mark W. Dudley
  • Patent number: 5214155
    Abstract: This invention is a method for making 1,2-substituted imidazoline compositions utilizing a polyamine mixture containing a high concentration of linear polyamine. The polyamine is either triethylenetetramine or tetraethylenepentamine. The polyamine mixture is reacted with a fatty acid, fatty dimer acid or the fatty esters thereof to yield the 1,2-substituted imidazoline composition. The highly linear polyamine provides higher yields of the imidazoline compound in the composition.
    Type: Grant
    Filed: April 29, 1992
    Date of Patent: May 25, 1993
    Assignee: Texaco Chemical Company
    Inventors: Donald R. Hollingsworth, Jeffrey H. Edwards
  • Patent number: 5214063
    Abstract: A compound of formula (I): ##STR1## in which R, R.sub.1 and R.sub.2 are as defined in the description. Medicinal product, which is useful in treating disorders related to a dysfunction of GABA.sub.B receptors.
    Type: Grant
    Filed: July 28, 1992
    Date of Patent: May 25, 1993
    Assignee: Adir et Compagnie
    Inventors: Michel Debaert, Pascal Berthelot, Claude Vaccher
  • Patent number: 5214061
    Abstract: This invention relates to p-acylaminophenoxycarbamates having the formula ##STR1## where R.sub.1 and R.sub.2 are each independently hydrogen, loweralkyl, aryl and arylloweralkyl; R.sub.3 is hydrogen, loweralkyl, arylloweralkyl; R.sub.4 is hydrogen, loweralkyl, formyl, alkylcarbonyl, arylloweralkyl, phenylcarbonyl, arylloweralkylcarbonyl, substituted phenylcarbonyl, pyridylcarbonyl, and substituted pyridylcarbonyl with the proviso that if R.sub.4 contains a carbonyl group directly attached to the oxygen of the N-O moiety, R.sub.3 cannot be hydrogen; or R.sub.3 and R.sub.4 taken together from a heterocyclic ring selected from the group consisting of imidazole or loweralkylimidazole; X is hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; and p is an integer selected from 0 and 1; the pharmaceutically acceptable acid addition salts thereof, and where applicable, the geometric and stereoisomers and racemic mixtures thereof.
    Type: Grant
    Filed: February 18, 1992
    Date of Patent: May 25, 1993
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Allen, Raymond W. Kosley, Jr., Bettina Spahl
  • Patent number: 5212198
    Abstract: This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof ##STR1## wherein R is alkyl, alkenyl, alkynyl, or (CH.sub.2).sub.m R.sup.3 whereR.sup.3 is cycloalkyl and m is 1 or 2;R.sup.1 is alkyl;R.sup.2 is hydrogen or alkyl;R.sup.4 is alkyl;n is an integer from 1 to 5;p is an integer from 0 to 6;Y is NH, oxygen or sulfur; andZ is hydrogen, alkyl, alkoxy, NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently hydrogen or alkyl, or SR.sup.6 wherein R.sup.6 is hydrogen, benzyl or alkyl.The compounds of Formula I are leukotriene B.sub.4 antagonists and are useful as anti-inflammatory agents and in the treatment of leukotriene B.sub.4 mediated conditions.
    Type: Grant
    Filed: October 9, 1992
    Date of Patent: May 18, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Stevan W. Djuric, Thomas D. Penning, James P. Snyder
  • Patent number: 5210209
    Abstract: The invention provides a method for the production of a pyrazolo(1,5-a)benzimidazole of the general formula (A): ##STR1## wherein R is a substituted or unsubstituted alkyl or aryl group, andR.sup.1 -R.sup.4 =R, H, halogen, OR, COOR, CONHR, SO.sub.2, NO.sub.2 NHR, NR.sub.2, or CN, andX is hydogen or a reactive group releasable on coupling with an oxidized color developer, wherein the invention provides reacting a 2-amino or 2-mercapto substituted benzimidazole to form a triazepinone or a thiadiazino derivative respectively, ring contracting said triazepinone or thiadiazino derivative to give the corresponding 2-methylpyrazolobenzimidazole product, and subsequently removing the substituents at the -3 or -4 positions to provide a compound of the general formula (1).
    Type: Grant
    Filed: June 3, 1991
    Date of Patent: May 11, 1993
    Assignee: Eastman Kodak Company
    Inventor: Michael W. Crawley
  • Patent number: 5200453
    Abstract: An ophthalmic formulation comprising a salt of sepazonium or a similar imidazolium compound as a preservative is provided.
    Type: Grant
    Filed: September 17, 1990
    Date of Patent: April 6, 1993
    Assignee: Iolab Corporation
    Inventor: Herwig J. Janssen
  • Patent number: 5196545
    Abstract: Process for the preparation of allantoin in a two-stage reaction by reaction of methyl glyoxylate methyl hemiacetal with urea in the presence of an inorganic acid at a pH-value of 1.0-2.0 and carrying out the ring-closure reaction at a pH-value of 7.0 to 9.0 in a second reaction stage.
    Type: Grant
    Filed: May 30, 1991
    Date of Patent: March 23, 1993
    Assignee: Chemie Linz Gesellschaft m.b.H.
    Inventors: Karl Schermanz, Klaus Fitzinger
  • Patent number: 5194624
    Abstract: The invention relates to compounds of the formula: ##STR1## in which R.sup.4 is an unsaturated, 5 or 6-membered heteromonocyclic group,R.sup.5 is hydrogen, lower alkanimidoyl or imino-protective group,R.sup.7 is ar(lower)alkyl or acyl derived from a carboxylic, carbonic, sulfonic or carbamic acid, andA is lower alkylene,or a salt thereof, useful as intermediates in the preparation of antimicrobial agents.
    Type: Grant
    Filed: May 9, 1990
    Date of Patent: March 16, 1993
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Masayoshi Murata, Hideo Tsutumi, Keiji Matsuda, Kohji Hattori, Takashi Nakajima
  • Patent number: 5182405
    Abstract: A process for the preparation of 1,3-disubstituted imidazolium salts that comprises reaction of an .alpha.-dicarbonyl compound, an aldehyde, an amine and an acid is disclosed.
    Type: Grant
    Filed: September 18, 1991
    Date of Patent: January 26, 1993
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Anthony J. Arduengo, III
  • Patent number: 5164512
    Abstract: A triarylimidazole derivative of the formula: ##STR1## wherein X is O or S; Y is an arylsulfonyl group, an alkyl group, etc.; R.sup.2, R.sup.3 and R.sup.4 are independently an aryl group, etc., is stable in water or a buffer solution, high in measuring sensitivity and is suitable as an oxidizable color producing reagent for determining hydrogen peroxide, etc. generated by enzymatic reaction in a living body sample.
    Type: Grant
    Filed: June 19, 1990
    Date of Patent: November 17, 1992
    Assignee: Wako Pure Chemical Industries, Ltd.
    Inventors: Kazunari Hashizume, Haruhiko Sugiyama