Patents Examined by James H. Turnipseed
  • Patent number: 5322953
    Abstract: Anti-inflammatory 4-substituted 2-furanones are made from intermediates having the formula ##STR1## where R.sub.1, R.sub.2 and R.sub.3 independently are n-or branched chain alkyl of 1 to 6 carbons. These compounds can be used as intermediates to produce 4-substituted 2-furanones which are anti-inflammatory agents.
    Type: Grant
    Filed: October 28, 1992
    Date of Patent: June 21, 1994
    Assignee: Allergan, Inc.
    Inventors: Gary C. M. Lee, Michael E. Garst
  • Patent number: 5314887
    Abstract: There are provided novel 1,4-dihydropyridine compounds possessing both calcium agonist and alpha.sub.1 -antagonist activity useful for treating congestive heart failure, pharmaceutical compositions containing them and methods of using these compounds to treat congestive heart failure in a mammal.
    Type: Grant
    Filed: October 30, 1992
    Date of Patent: May 24, 1994
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: Paul E. Aldrich, Richard A. Earl, Philip Ma
  • Patent number: 5314884
    Abstract: The invention relates to substituted 2-pyrimidinyl-1-piperazine derivatives defined herein by formula (I), processes for their manufacture, compositions containing said substituted 2-pyrimidinyl-1-piperazine derivatives as active materials and the use of said compounds and compositions as agents effecting the central nervous system. Also included in the invention are intermediates of formula (VIII) for making the active formula (I) compounds.
    Type: Grant
    Filed: August 31, 1992
    Date of Patent: May 24, 1994
    Assignee: Troponwerke GmbH & Co.
    Inventors: Peter-Rudolf Seidel, Harald Horstmann, Jorg Traber, Wolfgang Dompert, Thomas Glaser, Teunis Schuurman
  • Patent number: 5312922
    Abstract: Fluorogenic chelators for Eu.sup.3+ and Tb.sup.3+ are provided, they form highly fluorescent complexes with Eu.sup.3+ and Tb.sup.3+. In all cases, the fluorescence observed was lanthanide-specific, long-lived and it was monitored by microsecond time-resolved fluorometry. The fluorogenic chelators could be quantified, in the presence of excess lanthanide, at levels <10.sup.-8 mol/L. Two new fluorogenic chelators can form ternary complexes with Eu.sup.3+ and Tb.sup.3+, in the presence of EDTA. The structures of the identified chelators is such that enzyme substrates can be used for enzyme-labelled time-resolved fluorometric immunoassays. The chelator 4-methylumbelliferyl phosphate which forms fluorescent, long-lived complexes with Eu.sup.3+, can be split by alkaline phosphatase to phosphate and 4-methylumbelli-ferone which does not form fluorescent complexes with Eu.sup.3+. Highly sensitive immunoassays for thyrotropin and thyroxine in human serum are demonstrated.
    Type: Grant
    Filed: April 6, 1992
    Date of Patent: May 17, 1994
    Assignee: Nordion International Inc.
    Inventor: Eleftherios P. Diamandis
  • Patent number: 5310919
    Abstract: Fungicidal pyridyl-substituted acrylic esters of the formula ##STR1## in which R.sup.1 represents alkyl or represents optionally substituted aralkyl,R.sup.2 represents dialkylanino or represents a radical --Z--R.sup.3,X represents oxygen or sulphur or represents a radical ##STR2## and Py represents optionally substituted pyridyl, whereR.sup.3 represents alkyl or represents optionally substituted aralkyl,R.sup.4 represents hydrogen, alkyl or alkanoyl or represents in each case optionally substituted aralkyl or aryl andZ represents oxygen or sulphur, their geometric isomers and isomer mixtures.
    Type: Grant
    Filed: January 31, 1992
    Date of Patent: May 10, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Alexander Klausener, Gerd Kleefeld, Dieter Berg, Stefan Dutzmann, Gerd Hanssler
  • Patent number: 5306719
    Abstract: Novel carbostyril derivatives and salts thereof having useful pharmacological activities such as myocardial contraction increasing activity (positive inotropic activity), coronary blood flow increasing activity, hypotensive activity, activity for inhibiting vasoconstriction induced by norepinephrine, and anti-inflammatory effect in one hand, while they do not possess activity for increasing heart beat at all substantially as well as show quite low toxicity and low side-effects in central nervous system activities.
    Type: Grant
    Filed: September 16, 1991
    Date of Patent: April 26, 1994
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Shigeharu Tamada, Takafumi Fujioka, Hidenori Ogawa, Shuji Teramoto, Kazumi Kondo
  • Patent number: 5306720
    Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from substituted or unsubstituted quinazolinedione,X denotes a group of the formula ##STR2## n is an integer of 1 through 7, the ring A denotes a group of the formula ##STR3## a group of the formula ##STR4## or a group of the formula ##STR5## and R.sup.2 denotes a hydrogen atom, a lower alkyl group, a substituted benzoyl group, a pyridyl group, a 2-hydroxyethyl group, a pyridylmethyl group, or a group of the formula ##STR6## wherein Z represents a halogen atom). The novel compounds of this invention are used for treating dementias and sequelae of cerebrovascular diseases.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: April 26, 1994
    Assignee: Eisai Co., Ltd.
    Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
  • Patent number: 5302601
    Abstract: The present invention relates to a class of compounds represented by the formula ##STR1## or a pharmaceutically acceptable salt thereof useful in the treatment of diseases or disorders mediated by platelet activating factor (PAF).
    Type: Grant
    Filed: November 6, 1992
    Date of Patent: April 12, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Ish K. Khannal, Roger Nosal, Richard M. Weier, Kirk T. Lentz
  • Patent number: 5302602
    Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.
    Type: Grant
    Filed: May 18, 1992
    Date of Patent: April 12, 1994
    Assignee: Kyowa Hakko Kogyo Co., Ltd.
    Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
  • Patent number: 5300644
    Abstract: The invention relates to a new process for the preparation of compounds of the general Formula I ##STR1## wherein R stands for piperazinyl, 4-methyl-piperazinyl or 4-ethyl-piperazinyl group and pharmaceutically acceptable salts thereof which comprises reacting a compound of the general Formula II ##STR2## wherein R.sup.1 and R.sup.2 stand for halogen, for an aliphatic acyloxy group containing 2 to 6 carbon atoms and optionally substituted by halogen, or for an aromatic acyloxy group containing 7 to 11 carbon atoms with a piperazine derivative of the general Formula III ##STR3## wherein R.sup.3 stands for hydrogen, methyl or ethyl or a salt thereof and subjecting the compound of the general Formula IV ##STR4## thus obtained wherein R, R.sup.1 and R.sup.2 are as stated above to hydrolysis after or without isolation and if desired converting the compound of the general Formula I thus obtained into a salt thereof or setting free the same from its salt.
    Type: Grant
    Filed: September 6, 1991
    Date of Patent: April 5, 1994
    Assignee: Chinoin Gyogyser- es Vegyeszeti Termekek Gyara Rt.
    Inventors: Istvan Hermecz, Geza Kereszturi, Lelle Vasvari, Agnes Horvath, Maria Balogh, Peter Ritli, Judit Sipos, Aniko Pajor, Katalin Marmarosi
  • Patent number: 5300513
    Abstract: Novel carbostyril derivatives of the formula: ##STR1## wherein X is 0 or S; Y is H or alkyl; R.sup.A is a group of the ##STR2## {wherein n is 1 or 2, A is alkylene, R.sup.1 is benzoyl having optionally 1-3 substituents, R.sup.2A is ##STR3## is (i) alkoxy, (ii) substituted or unsubstituted 5- or 6-membered heterocylic group, (iii) alkenylthio, (iv) pyrrolidinyl-alkyl--S--, (v) pyrrolidinyl-alkyl--SO--, (vi) pyrrolidinyl-alkyl--SO.sub.2 --, (vii) --O--B--NR.sup.4 R.sup.5 [B is alkylene having optionally OH, R.sup.4 is H, R.sup.5 is tricyclo[3.3.1.1]decanyl, tricyclo[3.3.1.1]decanylalkyl, etc., or R.sup.4 and R.sup.5 may together form a group of ##STR4## (R.sup.6 is substituted or unsubstituted amino)] or (viii) substituted alkoxy; m is 1 to 3]}, which have excellent vasopressin antagonistic activities and are useful as vasodilator, hypotensive agent, water diuretics, platelet agglutination inhibitor, and a vasopressin antagonistic composition containing the compound as the active ingredient.
    Type: Grant
    Filed: August 6, 1991
    Date of Patent: April 5, 1994
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hidenori Ogawa, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Hajime Komatsu, Michinori Tanaka, Kazuyoshi Kitano, Takafumi Fujiioka, Shuji Teramoto, Michiaki Tominaga, Yoichi Yabuuchi
  • Patent number: 5300643
    Abstract: New quinolone-carboxylic acids of the general formula (I) ##STR1## wherein the definitions for R.sub.1 -R.sub.9 are given in the description, a process for their preparation and their use as medicaments, in particular as antiviral agents.
    Type: Grant
    Filed: August 25, 1992
    Date of Patent: April 5, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Grohe, Wolfgang Dummer, Kai Rossen, Arnold Paessens
  • Patent number: 5298513
    Abstract: For treatment of disorders of the central nervous system, the cardiovascular system or the intestinal tract, the new substituted basic 2-aminotetralins of the formula ##STR1## in which R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen, alkyl or acyl, andR.sup.3 represents quinuclidine ora group of the formula --(CH.sub.2).sub.a --R.sup.4, --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.b --R.sup.4, --CH.sub.2 --C.tbd.C--(CH.sub.2).sub.b --R.sup.4, ##STR2## wherein a denotes a number from 1 to 10,b denotes a number 0, 1, 2, 3 or 4,c denotes a number 0, 1 or 2,d denotes a number 2 or 3, andX denotes oxygen, sulphur or NR.sup.5,and their salts.
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: March 29, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudolf Schohe, Thomas Glaser, Jorg Traber, George S. Allen
  • Patent number: 5298633
    Abstract: Anti-inflammatory 4-substituted 2-furanones are made from intermediates having the formulas: ##STR1##
    Type: Grant
    Filed: October 28, 1992
    Date of Patent: March 29, 1994
    Assignee: Allergan, Inc.
    Inventors: Gary C. M. Lee, Michael E. Garst
  • Patent number: 5296599
    Abstract: A class of novel heterocyclic aromatic carbamate compounds is described. A method of derivatizing amine-functional compounds with the novel carbamates is also disclosed. The derivatives can be detected using a fluorescence detector. The present composition and method allow femtomole quantities of amine compounds to be detected and measured.
    Type: Grant
    Filed: September 19, 1991
    Date of Patent: March 22, 1994
    Assignee: Millipore Corporation
    Inventors: Steven A. Cohen, Dennis P. Michaud
  • Patent number: 5296483
    Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are compounds of the formula ##STR1## and the non-toxic pharmaceutically acceptable salts thereof, wherein D is the residue of a centrally acting primary, secondary or tertiary amine and ##STR2## is an unsubstituted or substituted dihydropyridyl, dihydroquinolyl or dihydroisoquinolyl radical. The corresponding ionic pyridinium, quinolinium and isoquinolinium salts ##STR3## wherein X.sup.- is the anion of a non-toxic pharmaceutically acceptable acid, are also disclosed.
    Type: Grant
    Filed: September 27, 1991
    Date of Patent: March 22, 1994
    Assignee: University of Florida
    Inventor: Nicholas S. Bodor
  • Patent number: 5294712
    Abstract: The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen: or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) to hydrolysis after or without isolation and if desired converting the compound of the Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the Formula I are known antibacterial agents.
    Type: Grant
    Filed: September 14, 1990
    Date of Patent: March 15, 1994
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
    Inventors: Istvan Hermecz, Geza Keresturi, Lelle V. Debreczy, Agnes Horvath, Maria Balogh, Gabor Kovacs, Tamas Szuts, Peter Ritli, Judit Sipos, Aniko Pajor
  • Patent number: 5292746
    Abstract: The present invention is directed to a new class of cyclic nitrones and their use as spin trapping agents.
    Type: Grant
    Filed: August 5, 1992
    Date of Patent: March 8, 1994
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Albert A. Carr, Craig E. Thomas, Ronald C. Bernotas, George Ku
  • Patent number: 5290934
    Abstract: Novel 4-oxoquinoline-3-carboxylic acid compounds of the formula: ##STR1## wherein R.sup.1 is cyclopropyl which may have 1 to 3 substituents of alkyl and halogen; phenyl which may be substituted by 1 to 3 substituents of alkoxy, halogen and OH; alkyl which may be substituted by halogen, alkanoyloxy or OH; alkenyl; or thienyl, R.sup.2 is 5- to 9-membered saturated or unsaturated heterocyclic ring which may be substituted, R.sup.3 is alkyl, R is H or alkyl, and X is halogen, and pharmaceutically acceptable salts thereof, said compounds having excellent antimicrobial activity and hence being useful as an antimicrobial agent, and a pharmaceutical composition containing said compound as an active ingredient.
    Type: Grant
    Filed: June 4, 1991
    Date of Patent: March 1, 1994
    Assignee: Otsuka Pharmaceutical Company, Limited
    Inventors: Hiraki Ueda, Hisashi Miyamoto, Hiroshi Yamashita, Hitoshi Tone
  • Patent number: RE34630
    Abstract: Novel substituted isoquinoline compounds are disclosed together with novel 2-phenylethylamides useful as precursors or intermediates for the production of the isoquinolines. The substituted isoquinolines exhibit activity in antagonizing the effects of platelet activating factor (PAF).
    Type: Grant
    Filed: January 27, 1992
    Date of Patent: June 7, 1994
    Assignee: Euroceltique, S.A.
    Inventors: T. Scott Shoupe, Stephen M. Coutts, Lloyd J. Dolby