Patents Examined by D. Margaret M. Mach
  • Patent number: 5739338
    Abstract: Compounds of the formula ##STR1## where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid inverse agonist-like biological activity.
    Type: Grant
    Filed: November 5, 1996
    Date of Patent: April 14, 1998
    Assignee: Allergan
    Inventors: Richard L. Beard, Min Teng, Diana F. Colon, Tien T. Duong, Roshantha A. Chandraratna
  • Patent number: 5734057
    Abstract: The present invention provides HIV protease inhibitors, intermediates for preparing HIV protease inhibitors. The enzyme, HIV protease, represents a viable target for the inhibition of HIV viral replication, thus providing a method for treating and/or preventing HIV infection.
    Type: Grant
    Filed: August 5, 1996
    Date of Patent: March 31, 1998
    Assignee: Eli Lilly and Company
    Inventors: William J. Hornback, John E. Munroe
  • Patent number: 5734058
    Abstract: New intercalating cyanine dyes are provided in which the benzothiazole portion of the cyanine dye has been modified to produce dyes with improved properties for labelling nucleic acids. The fluorescent cyanine dyes have a positively charged substituent attached to the positively charged nitrogen on the benzothiazole portion of the cyanine dye.
    Type: Grant
    Filed: November 9, 1995
    Date of Patent: March 31, 1998
    Assignee: Biometric Imaging, Inc.
    Inventor: Linda G. Lee
  • Patent number: 5728869
    Abstract: There is disclosed a process for the preparation of an indanylamine compound of general formula ##STR1## wherein R.sup.1 represents an optionally substituted alkyl group, and R.sup.2, R.sup.3 and R.sup.4 independently represent a hydrogen atom or an optionally substituted alkyl group, the process including the steps of hydrogenating a compound of general formula ##STR2## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as described above and R.sup.5 and R.sup.6 independently represent a halogen atom, a hydroxyl, nitro or cyano group, or an optionally substituted alkyl, alkoxy, alkoxycarbonyl, alkylcarboxy or alkylamino group provided that R.sup.5 and R.sup.6 represent different atoms or groups, and subsequent rearrangement and derivatisation of the product thereof. Compounds of general formula I may be used to prepare preferred stereoisomers of fungicidal N-indanyl carboxamide compounds.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: March 17, 1998
    Assignee: American Cyanamid Company
    Inventor: Paul Howard Briner
  • Patent number: 5726305
    Abstract: The invention relates to substituted quinoline-2-carboxylic acid amides of the formula I ##STR1## their preparation and their use, and intermediates which are formed in the preparation of the compounds of the formula I. The compounds according to the invention are used as inhibitors of prolyl 4-hydroxylase and as pharmaceuticals (medicaments) for treatment of fibrotic diseases.
    Type: Grant
    Filed: July 3, 1996
    Date of Patent: March 10, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Klaus Weidmann, Karl-Heinz Baringhaus, Georg Tschank, Martin Bickel
  • Patent number: 5726191
    Abstract: A compound of the formula ##STR1## wherein R.sup.1 is hydrogen or C.sub.1-6 -alkyl;R.sup.2 is C.sub.1-6 -alkyl or adamantyl;R.sup.3 is C.sub.1-6 -alkyl or hydroxy; orR.sup.2 and R.sup.3 taken together are --(CR.sup.6 R.sup.7).sub.n --;R.sup.4 is C.sub.2-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.2-8 -alkynyl, --OCH.sub.2 R.sup.5 or C.sub.2-8 -alkanoyl; and hydrogen when R.sup.3 is hydroxy;R.sup.5 is C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl or C.sub.2-6 -alkynyl;R.sup.6 and R.sup.7 are hydrogen or C.sub.1-6 -alkyl;Y is oxygen or sulphur; andn is 3, 4 or 5,and pharmaceutically usable salts of carboxylic acids of formula I act as selective ligands of retinoic acid .gamma.-receptors and are useful for the treatment of epithelial lesions.
    Type: Grant
    Filed: October 23, 1996
    Date of Patent: March 10, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Klaus, Peter Mohr
  • Patent number: 5726164
    Abstract: The present invention relates to a pharmaceutical composition for the intravenous administration of the sparingly soluble staurosporin derivative N-benzoyl-staurosporin. The composition comprises the following preferred components:a) the therpeutic agent N-benzoyl-staurosporin;b) a polyoxyethylene/polyoxypropylene block copolymer;c) ethanol and water as carrier liquids; andd) purified lecithin from soybeans ande) as water-soluble excipients glycerol and sorbitol.
    Type: Grant
    Filed: March 20, 1996
    Date of Patent: March 10, 1998
    Assignee: Novartis Corporation
    Inventors: Hans Georg Weder, Peter van Hoogevest
  • Patent number: 5723627
    Abstract: Process for the preparation of antibacterial compounds of the formula ##STR1## comprises condensing an oxo compound of the formula ##STR2## with an amino compound of the formula ##STR3## to produce a compound of the formula ##STR4## reacting the compound of the formula (III) with a compound of the formula ##STR5## to give a compound of the formula ##STR6## and then eliminating the amino-protective group ##STR7##
    Type: Grant
    Filed: February 20, 1997
    Date of Patent: March 3, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Uwe Petersen, Andreas Krebs, Thomas Schenke, Klaus Grohe, Michael Schriewer, Ingo Haller, Karl Georg Metzger, Rainer Endermann, Hans-Joachim Zeiler
  • Patent number: 5723453
    Abstract: A stabilized, essentially sodium free, alkaline and aspirin combination compound which is readily soluble in a preselected fluid, which when dissolved forms potassium acetylsalicylate. Such alkaline and aspirin combination compound consisting essentially of aspirin, having a predetermined particle size. Such aspirin being present in the alkaline and aspirin combination compound generally within a range of between about 325.0 mg and about 1,000.0 mg per unit dose. A preselected alkaline compound is present in such alkaline and aspirin combination compound generally within a range of between about 250.0 mg and about 3,000.0 mg per unit dose. The preselected alkaline compound having a ph generally within a range of between about 8.0 and 10.0 and such preselected alkaline compound being present in this alkaline and aspirin combination compound in a molar amount which is greater than a molar amount required to neutralize the aspirin.
    Type: Grant
    Filed: November 13, 1995
    Date of Patent: March 3, 1998
    Assignee: Health Corporation
    Inventor: Howard P. Phykitt
  • Patent number: 5721249
    Abstract: The present invention is directed to a new 5HT.sub.2 antagonist, (+)-.alpha.-(2,3-dimethoxyphenyl)-1-?2-(4-fluorophenyl)ethyl!-4-piperidine methanol, and its use in the treatment of a number of disease states.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: February 24, 1998
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Albert A. Carr, John M. Kane, David A. Hay, Christopher J. Schmidt
  • Patent number: 5719164
    Abstract: The invention relates to substituted quinoline-2-carboxylic acid amides of the formula I ##STR1## their preparation and their use, and intermediates which are formed in the preparation of the compounds of the formula I. The compounds according to the invention are used as inhibitors of prolyl 4-hydroxylase and as pharmaceuticals (medicaments) for treatment of fibrotic diseases.
    Type: Grant
    Filed: July 3, 1996
    Date of Patent: February 17, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Klaus Weidmann, Karl-Heinz Baringhaus, Georg Tschank, Martin Bickel
  • Patent number: 5719178
    Abstract: A regimen and composition for treating Attention Deficit/Hperactivity Disorder (ADHD) by the use of proanthocyanidin both with and without a heterocyclic anti-depresssant, preferably desipramine and a citrus bioflavinoid.
    Type: Grant
    Filed: November 20, 1995
    Date of Patent: February 17, 1998
    Inventors: Julie Chasen Paul, Steven Joseph Tenenbaum
  • Patent number: 5714488
    Abstract: Compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein W is selected from the group consisting of optionally substituted quinolyl, optionally substituted benzothiazolyl, optionally substituted benzoxazolyl, optionally substituted benzimidazolyl, optionally substituted quinoxalyl, optionally substituted pyridyl, optionally substituted pyrimidyl, and optionally substituted thiazolyl; R.sup.1 and R.sup.2 are one or more groups independently selected from hydrogen, alkyl, halolalkyl, alkoxy, and halogen; Z is selected from the group consisting of N--OH, N--O--A--COM, CH--COM, and CH--CH.dbd.N--0--A--COM wherein A is selected from the group consisting of alkylene, alkenylene, cycloalkylene, and optionally substituted alkylphenyl wherein the alkyl portion is of one to six carbon atoms, and M is selected from the group consisting of a pharmaceutically acceptable, metabolically clearable group, --OR.sup.3, and --NR.sup.4 R.sup.
    Type: Grant
    Filed: September 17, 1996
    Date of Patent: February 3, 1998
    Assignee: Abbott Laboratories
    Inventors: Clint D. W. Brooks, Pramila Bhatia, Teodozyj Kolasa
  • Patent number: 5712310
    Abstract: A stable aqueous suspension including a substantially water-insoluble drug suspended in a completely water-soluble mixture including hydroxypropylmethylcellulose, polyoxyethylene sorbitan monooleate, and xanthan gum.
    Type: Grant
    Filed: June 14, 1996
    Date of Patent: January 27, 1998
    Assignee: Alpharma USPD, Inc.
    Inventor: Edward A. Koch
  • Patent number: 5710163
    Abstract: This invention relates to hexa- and octahydrobenzo?f!quinolin-3-ones, pharmaceutical formulations containing those compounds and methods of their use as steroid 5.alpha.-reductase inhibitors.
    Type: Grant
    Filed: July 17, 1996
    Date of Patent: January 20, 1998
    Assignee: Eli Lilly and Company
    Inventor: James E. Audia
  • Patent number: 5710160
    Abstract: The invention encompasses the novel compound of Formula I useful in the treatment of diseases, including asthma, by raising the level of cyclic adenosine-3',5'-monophosphate (cAMP) through the inhibition of phosphodiesterase IV (PDE IV). ##STR1## The invention also encompasses certain pharmaceutical compositions and methods for treatment of diseases by inhibition of PDE IV, resulting in an elevation of cAMP, comprising the use of compounds of Formula I.
    Type: Grant
    Filed: December 10, 1996
    Date of Patent: January 20, 1998
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Daniel Guay, Yves Girard, Yves Ducharme
  • Patent number: 5708174
    Abstract: Compounds of formula (I), wherein formula I consists of formulae (I-1) to (I-4), which are defined in the specification, and pharmaceutically acceptable salts thereof, and the use of a compound of formula I or a pharmaceutically acceptable salt thereof, and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorder.
    Type: Grant
    Filed: April 11, 1995
    Date of Patent: January 13, 1998
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Francis David King, Laramie Mary Gaster, Graham Francis Joiner, Keith Raymond Mulholland, Shirley Katherine Rahman
  • Patent number: 5707931
    Abstract: The present invention relates to novel 4-amino-2-quinolinone derivatives of the formula (I) useful in agriculture, especially as fungicides, insecticides and herbicides ##STR1## wherein, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently hydrogen, halogen, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.1 -C.sub.3 haloalkoxy, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 haloalkyithio, NO.sub.2, CN, C.sub.1 -C.sub.4 alkoxy carbonyl, phenyl, phenoxy, benzoyl, benzenesulfonyl, benzyl or morpholine; R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, cyclopropyl, phenyl, halophenyl, benzyl or phenylthiomethyl; R.sub.6 is hydrogen, C.sub.1 -C.sub.5 alkyl, C.sub.3 -C.sub.6 alkenyl or C.sub.3 -C.sub.6 alkynyl; and R.sub.7 is ##STR2## wherein, R.sub.8, R.sub.9, R.sub.10, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.15, R.sub.16, R.sub.17, R.sub.18, R.sub.19, R.sub.20, X, Y, m, n, p and q are defined within the description.
    Type: Grant
    Filed: December 19, 1995
    Date of Patent: January 13, 1998
    Assignee: Korea Research Intsituted of Chemical Technology
    Inventors: Chwang Siek Pak, Eun Bok Choi, Gyu Hwan Yon, Heui Cheol Yang, Hyeon Kyu Lee, Ge Hyeong Lee, Jin Pyo Lee, Gyung Ja Choi
  • Patent number: 5708005
    Abstract: A compound of the formula: ##STR1## wherein R.sup.1 represents hydrogen or an optionally substituted hydrocarbon group; R.sup.2 represents an optionally substituted hydrocarbon group, an optionally substituted amino group or a substituted hydroxyl group; X represents an optionally halogenated lower alkylene group; Y represents a substituent; n represents an integer of 0 to 6; and m represents 0 or 1; or a salt thereof, a process for producing it, an intermediate for the production, and a pharmaceutical composition containing it are provided.
    Type: Grant
    Filed: December 10, 1996
    Date of Patent: January 13, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shigenori Ohkawa, Osamu Uchikawa, Masaomi Miyamoto
  • Patent number: 5700810
    Abstract: Novel compound represented by the formula: ##STR1## wherein A", B, C, D, E, G, Ar, X, Y, and Z are defined herein or a salt thereof. The compounds have excellent activity of inhibiting ACAT, lowering Cholesterol in blood and inhibiting tachykinin receptor, or a salt thereof, their production and use.
    Type: Grant
    Filed: October 11, 1995
    Date of Patent: December 23, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Hideaki Natsugari, Hitoshi Ikeda, Takenori Ishimaru, Takayuki Doi