Patents Examined by David B. Springer
  • Patent number: 5776970
    Abstract: Tryptophan derivatives substituted by a hydrophobic group, e.g. carbobenzoxy, at the N-terminus, and a hydrophilic group, e.g. --COOH, --SO.sub.3 H or --PO.sub.3 H, at the C-terminus, were found to be cell-permeable blockers of protein tyrosine kinases (PTKs). These PTK blockers are useful in basic research and in the treatment of neoplastic diseases.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: July 7, 1998
    Assignees: Yeda Research and Development Co. Ltd., Yissum Research Development Co.
    Inventors: Yoram Shechter, David Naor
  • Patent number: 5767286
    Abstract: 1,4-Disubstituted-5(4H)-tetrazolinones of the formula (I) ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 have the meanings given in the specification), which are known to be useful as herbicides, can be obtained in very good yields by reacting the corresponding 1-substituted-5(4H)-tetrazolinones with the corresponding carbamoyl chlorides in the presence of 4-dimethylaminopyridine.
    Type: Grant
    Filed: September 23, 1994
    Date of Patent: June 16, 1998
    Assignee: Nihon Bayer Agrochem K. K.
    Inventors: Akihiko Yanagi, Yukiyoshi Watanabe, Shin-ichi Narabu
  • Patent number: 5719287
    Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of their use.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: February 17, 1998
    Assignee: Eli Lilly and Company
    Inventors: Stephen W. Kaldor, Marlys Hammond
  • Patent number: 5684163
    Abstract: A process for the preparation of a N-)ortho-alkylphenyl)-imide of the formula ##STR1## in which R.sup.1 to R.sup.9 is defined in the specification which comprises reacting a cyclic anhydride of the formula ##STR2## wherein R.sup.6 to R.sup.9 are difined in the specification with an amine of the formula ##STR3## optionally in the presence of an acid catalyst and optionally in the presence of a solvent which is immiscible or only slightly miscible with water but can form an azeotrope with water, at a temperature between to C. under conditions so that the water formed during the reaction is removed from the reaction mixture without the addition of a polymerization inhibitor or a dipolar solvent. The final products are used as intermediates to prepare heat-stable plastics as well as intermediates to prepare pharmaceutical and agricultural chemicals.
    Type: Grant
    Filed: February 5, 1996
    Date of Patent: November 4, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Torsten Groth, Bernd-Michael Konig, Josef Kasbauer, Michael Schwamborn
  • Patent number: 5674641
    Abstract: A battery module includes a number of electrically connected electrochemical cells. In a preferred embodiment, the battery includes multi-cell batteries in which electrodes are separated from different potential electrodes by a layer of polymer electrolyte. The battery module is formed from a number of multi-cell batteries stacked on top of one another, the electrodes of each multi-cell being electrically connected to one another, and the different potential electrodes of each multi-cell being electrically connected to one another so that a battery module having desired power characteristics is formed. The battery module includes electrically conductive spacers for electrically connecting tabs on the electrodes to tabs on other electrodes and tabs on the different potential electrodes to tabs on other different potential electrodes and for preventing damage to the tabs or the electrodes or different potential electrodes from bending the tabs excessively.
    Type: Grant
    Filed: October 29, 1992
    Date of Patent: October 7, 1997
    Assignee: Valence Technology, Inc.
    Inventor: Scot Stacey Cheu
  • Patent number: 5663123
    Abstract: This invention relates to an earth stabilization fluid and to a method for using such an earth stabilization fluid. This invention uses a continuous phase that has been added to a borehole and a polymer material that forms gel masses having desired functional properties when added to the continuous phase.
    Type: Grant
    Filed: February 1, 1995
    Date of Patent: September 2, 1997
    Assignee: KB Technologies Ltd.
    Inventors: K. Gifford Goodhue, Jr., Max M. Holmes
  • Patent number: 5663171
    Abstract: The present invention is directed to certain compounds of the general structural formula: ##STR1## wherein R.sub.1, R.sub.1a, R.sub.2a, R.sub.3, R.sub.3a, R.sub.4, R.sub.5, R.sub.6, A, W, and n are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.
    Type: Grant
    Filed: March 3, 1995
    Date of Patent: September 2, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Meng Hsin Chen, Gregori J. Morriello, Ravi Nargund, Arthur A. Patchett, Lihu Yang
  • Patent number: 5661014
    Abstract: Enantiomeric glutarimides such as aminoglutethimide and rogletimide are prepared by cyclisation of a corresponding ester-nitrile which is a good substrate for biotransformation with an enantiospecific esterase.
    Type: Grant
    Filed: May 30, 1995
    Date of Patent: August 26, 1997
    Assignee: Chiroscience Limited
    Inventors: Christopher Thomas Evans, Raymond McCague, Stephen John Clifford Taylor
  • Patent number: 5659063
    Abstract: The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 19, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Norman Anthony Abood, Daniel Lee Flynn, Scott Anthony Laneman, Roger Nosal, Lori Ann Schretzman
  • Patent number: 5654260
    Abstract: This invention concerns a corrosion-inhibitor nominally comprised of a phenolic compound and a hydroxide-bearing compound capable of imparting a pH of 9 to water, the inclusion thereof in aerated water-based fluids and foams, and the use of these fluids in wellbore applications; particularly applications conducted at elevated temperatures.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: August 5, 1997
    Assignee: Phillips Petroleum Company
    Inventor: Yulin Wu
  • Patent number: 5650428
    Abstract: An arylsulfonamide derivative of the formula (I): ##STR1## wherein R.sup.1 is unsubstituted phenyl or naphthyl, or phenyl substituted by 1 to 3 same or different substituents selected from the group consisting of halogen, alkyl, nitro and alkoxy, R.sup.2 is straight, branched, or branched cyclic alkyl with 1 to 15 carbon atoms, phenyl, phenyloxyl, phenyloxy substituted by one or more halogen atoms, cycloalkyl with 5 to 7 carbon atoms, indolyl, alkylthiol with 1 to 4 carbon atoms, hydroxyl, protected hydroxyl, imidazolyl, pyridyloxyl, or --OSO.sub.2 R.sup.4, R.sup.4 is straight or branched alkyl with 1 to 15 carbon atoms, or unsubstituted phenyl or thienyl, or phenyl or thienyl substituted by 1 to 3 same or different substituents of halogen, alkyl, nitro and alkoxy, R.sup.3 is hydrogen or straight or branched alkyl with 1 to 20 carbon atoms, n is an integer of 0 to 10, p is an integer of 0 to 10, X is a group of the formula--(CH.sub.2)m-A-(CH.sub.
    Type: Grant
    Filed: February 28, 1995
    Date of Patent: July 22, 1997
    Assignee: NKK Corporation
    Inventors: Masayuki Ohmori, Shin-Ichi Sawamura, Takehiro Yamamoto, Yoshiko Kawada, Shihoko Maeda, Takeshi Yago, Akihiro Nakajima, Masatsugu Mizuguchi, Yasuo Miyoshi
  • Patent number: 5650374
    Abstract: Herbicidal 1-cyclopropyl tetrazolinones of the formula ##STR1## wherein X represents C.sub.1-3 alkyl, C.sub.2-4 alkenyl or halogen,n represents 0 to 5,R.sup.1 and R.sup.2 each independently represents C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-7 cycloalkyl which may optionally be substituted by C.sub.1-3 alkyl, epoxy-C.sub.3-5 alkan-1-yl, phenyl which may optionally be substituted, or aralkyl which may optionally be substituted, orR.sup.1 and R.sup.2 together with the N-atom to which they are attached, represent a cyclic ring which may be substituted, and some novel intermediates therefor.
    Type: Grant
    Filed: November 7, 1995
    Date of Patent: July 22, 1997
    Assignee: Nihon Bayer Agrochem K.K.
    Inventors: Toshio Goto, Yoshinori Kitagawa, Seishi Ito, Katsuhiko Shibuya, Kazuhiro Ukawa, Yoshiko Kyo
  • Patent number: 5646300
    Abstract: There are disclosed neuroprotective compounds having the formula ##STR1## wherein the moieties are defined in the specification, and processes for making them.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: July 8, 1997
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Raymond W. Kosley, Jr., Denise M. Flanagan, Lawrence L. Martin, Peter A. Nemoto
  • Patent number: 5646164
    Abstract: The present inventors have discovered three classes of novel .alpha.-methylene-.gamma.-butyrolactones with excellent antiplatelet activity. As a result of intensive studies, it has been found that compounds represented by the formula I-III are potent inhibitors of platelet aggregation. ##STR1## For the formula I, R.sub.1 is a methyl, a phenyl group optionally substituted with one or two group selected from halide, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, phenyl, nitro, amino.For the formula II, R.sub.1 is a methyl, a phenyl group optionally substituted with one or two group selected from halide, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.sub.4) alkoxy, phenyl, nitro, amino; R.sub.2 represents hydrogen, halide, (C.sub.1 -C.sub.4) alkyl, phenyl, nitro, amino; R.sub.3 represents hydrogen, halide, (C.sub.1 -C.sub.4) alkyl, phenyl, nitro, amino.For the formula III, R.sub.1 is a methyl, a phenyl group optionally substituted with one or two group selected from halide, (C.sub.1 -C.sub.4) alkyl, (C.sub.1 -C.
    Type: Grant
    Filed: November 14, 1995
    Date of Patent: July 8, 1997
    Assignee: National Science Council
    Inventors: Cherng-Chyi Tzeng, Yeh-Long Chen, Tai-Chi Wang, Che-Ming Teng
  • Patent number: 5646162
    Abstract: Oxy-phenyl-(phenyl)gycinolamides with heterocyclic substituents are prepared by reaction of the corresponding oxyphenylcarboxylic acids with heterocyclic substituents with phenylglycinol. The new substances are suitable as active compounds in medicaments, in particular in agents having an antiatherosclerotic action.
    Type: Grant
    Filed: December 1, 1995
    Date of Patent: July 8, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Muller, Richard Connell, Siegfried Goldmann, Klaus-Helmut Mohrs, Siegfried Raddatz, Michael Matzke, Rudi Grutzmann, Martin Beuck, Stefan Wohlfeil, Hilmar Bischoff, Dirk Denzer
  • Patent number: 5646171
    Abstract: An angiotensin II antagonist of the formula: ##STR1## in which: R.sub.p.sup.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl or C.sub.1 -C.sub.6 alkanoyl; R.sub.p.sup.2 represents a single bond, C.sub.1 -C.sub.4 alkylene or C.sub.1 -C.sub.4 alkylidene; R.sub.p.sup.3 and R.sub.p.sup.4 are independently selected from the group consisting of hydrogen and C.sub.1 -C.sub.6 alkyl; R.sub.p.sup.5 represents hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl, naphthyl, benzyl, diphenylmethyl, naphthylmethyl, alkanoyloxyalkyl, cycloalkanecarbonyloxyalkyl, alkoxycarbonyloxyalkyl, cycloalkyloxycarbonyloxyalkyl, (5-phenyl-2-oxo-1,3-dioxolen-4-yl)methyl, (5-alkyl-2-oxo-1,3-dioxolen-4-yl)methyl or phthalaidyl; R.sub.p.sup.6 represents a carboxy or a tetrazol-5-yl; and X.sub.p represents an oxygen or sulfur, and pharmaceutically acceptable salts thereof. The compounds have hypotensive activity and can thus be used for the treatment and prophylaxis of hypertension.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: July 8, 1997
    Assignee: Sankyo Company, Limited
    Inventors: Hiroaki Yanagisawa, Yoshiya Amemiya, Yasuo Shimoji, Takuro Kanazaki, Hiroyuki Koike, Toshio Sada
  • Patent number: 5643878
    Abstract: Compounds of formula I ##STR1## or their hydroxy-protected derivatives, and compounds of formula I' ##STR2## wherein T is an acyl radical of formula Z ##STR3## wherein R.sup.z is unsubstituted or substituted hydrocarbyl wherein at least one carbon atom has been replaced by a hetero atom with the proviso that a hetero atom is not bonded directly to the carbonyl to which the radical R.sup.z is bonded, alkyl having two or more carbon atoms, lower alkenyl, lower alkynyl, aryl or unsubstituted or substituted amino, and wherein the radicals R.sub.1, B.sub.1, R.sub.2, R.sub.3, A.sub.1, A.sub.2 and NR.sub.4 R.sub.5 are as defined in the description, and precursors thereof, are described. The compounds have pharmaceutical activity, for example in the treatment of retroviral diseases, such as AIDS.
    Type: Grant
    Filed: March 8, 1994
    Date of Patent: July 1, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Guido Bold, Marc Lang, Alexander Fassler, Hans-Georg Capraro, Shripad Bhagwat, Peter Schneider, Peter van Hoogevest
  • Patent number: 5641798
    Abstract: This invention provides novel bicyclic compounds which are useful as excitatory amino acid receptor antagonists and in the treatment of neurological disorders. This invention also provides intermediates useful in the synthesis of excitatory amino acid antagonists.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: June 24, 1997
    Assignee: Eli Lilly and Company
    Inventor: James A. Monn
  • Patent number: 5641800
    Abstract: A class of novel 1H-indole-1-functional compounds is disclosed together with the use of such indole compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock. The compounds are 1H-indole-1-acetamides, 1H-indole-1-acetic acid hydrazides, and 1H-indole-1-glyoxylamides.
    Type: Grant
    Filed: April 13, 1995
    Date of Patent: June 24, 1997
    Assignee: Eli Lilly and Company
    Inventors: Nicholas J. Bach, Robert D. Dillard, Susan E. Draheim
  • Patent number: 5641787
    Abstract: The present invention accordingly provides the use of a compound of formula I, or a pharmaceutically acceptable salt thereof or a prodrug thereof: ##STR1## wherein R.sup.1 represents hydrogen or C.sub.1-6 alkyl;Z represents --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --;R.sup.2 represents hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, aryl(C.sub.1-6)alkyl or halogen;R.sup.3, R.sup.4 and R.sup.5 independently represent hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro, --OR.sup.a, --SR.sup.a, --SOR.sup.a, --SO.sub.2 R.sup.a, --SO.sub.2 NR.sup.a R.sup.b, --NR.sub.a R.sup.b, --NR.sup.a COR.sup.b, --NR.sup.a CO.sub.2 R.sup.b, --COR.sup.a, --CO.sub.2 R.sup.a or --CONR.sup.a R.sup.b ; andR.sup.a and R.sup.b independently represent hydrogen, hydrocarbon or a heterocyclic group;for the manufacture of a medicament for the treatment and/or prevention of psychotic disorders such as schizophrenia.
    Type: Grant
    Filed: September 12, 1995
    Date of Patent: June 24, 1997
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Ian Michael Mawer, Howard Barff Broughton, Janusz Jozef Kulagowski, Paul David Leeson