Patents Examined by James H. Turnipseed
  • Patent number: 5095116
    Abstract: A block amido-amine condensation product having the formula: ##STR1## wherein R' represents hydrogen or methyl, andR" represents an organic group selected from the group consisting of polyoxyethylene groups, polyoxypropylene groups, polyoxyethylene/oxypropylene groups, and polyethylene amino groups.
    Type: Grant
    Filed: September 4, 1990
    Date of Patent: March 10, 1992
    Assignee: Texaco Chemical Company
    Inventors: George P. Speranza, Jiang-Jen Lin
  • Patent number: 5095119
    Abstract: A compound of the formula: ##STR1## wherein A is ##STR2## in which X is .dbd.CH-- or .dbd.N--; R.sup.2 is hydrogen, alkyl, phenyl, benzyl or phenethyl; Y is --CH.sub.2--, --NH-- or --O--; and Z is --H.sub.2 or .dbd.O; B is His, Leu, Ile, Nva, Nle, Ala or Val; and R.sup.1 is hydrogen, alkyl, phenyl or phenylalkyl; or a pharmaceutically acceptable salt thereof are renin inhibitors.
    Type: Grant
    Filed: November 16, 1990
    Date of Patent: March 10, 1992
    Assignee: American Home Products Corporation
    Inventors: Timothy D. Ocain, David D. Deininger
  • Patent number: 5091530
    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 ##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: November 23, 1988
    Date of Patent: February 25, 1992
    Assignee: Chinoin Gyogyszer- es Vegyeszeti Termekek Gyara Rt.
    Inventors: Istvan Hermecz, Geza Kereszturi, Lelle Vasvari, Agnes Horvath, Marie Balogh, Peter Ritli, Judit Sipos, Aniko Pajor, Katalin Marmarosi
  • Patent number: 5084461
    Abstract: The present invention provides certain novel azadecalin amides and thioamides which are useful as inhibitors of cholesterol biosynthesis and as agents which lower total serum cholesterol in patients in need thereof.
    Type: Grant
    Filed: March 27, 1991
    Date of Patent: January 28, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Marion W. Wannamaker, William A. Van Sickle, William R. Moore
  • Patent number: 5084457
    Abstract: This invention is compounds of the formula: ##STR1## and a method of treating cognitive and related neuronal behavioral problems in mammals using the compounds.
    Type: Grant
    Filed: July 23, 1990
    Date of Patent: January 28, 1992
    Assignee: American Cyanamid Company
    Inventors: William J. Fanshawe, Joseph W. Epstein, Jeremy I. Levin
  • Patent number: 5082954
    Abstract: Anti-inflammatory 4-substituted 2-furanones are made from intermediates having the formulas: ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 independently are n-alkyl of 1 to 6 carbons, or branched chain alkyl of 1 to 6 carbons; X is H, OH, NH.sub.2, I or Br; R.sub.4 is H, alkyl of 1-20 carbons, phenyl[C.sub.1 -C.sub.20 alkyl], naphthyl[C.sub.1 -C.sub.20 alkyl], CH.sub.2 OH, CH.sub.2 NH.sub.2, CH.sub.2 CH.sub.2 OH, CH.sub.2 --CHO, CH.sub.2 --COOH or CH.sub.2 --COOR.sub.5, and R.sub.5 is alkyl of 1 to 6 carbons, with the proviso that when X is hydrogen then R.sub.4 is selected from the group consisting of CH.sub.2 OH, CH.sub.2 NH.sub.2, CH.sub.2 CH.sub.2 OH, CH.sub.2 --CHO, or CH.sub.2 --COOR.sub.5 ; ##STR2## in which R.sub.1, R.sub.2 and R.sub.3 independently are n-alkyl of 1 to 6 carbons, or branched chain alkyl or 1 to 6 carbons, and R.sub.5 is alkyl or 1 to 6 carbons; ##STR3## in which R.sub.1, R.sub.2 and R.sub.3 independently are n-alkyl of 1 to 6 carbons, or branched chain alkyl of 1 to 6 carbons, and R.
    Type: Grant
    Filed: April 24, 1991
    Date of Patent: January 21, 1992
    Assignee: Allergan, Inc.
    Inventors: Gary C. M. Lee, Michael E. Garst
  • Patent number: 5081124
    Abstract: A quinazoline of the formula: ##STR1## wherein R.sup.1 is alkyl, cycloalkyl, alkenyl, alkynyl, alkoxy, alkylthio, aryl, aryloxy, arylalkyl, halogeno, hydroxy, mercapto, pyridylthio, pyrimidinylthio, or substituted alkyl or alkoxy;wherein R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, substituted alkyl or alkanoyl;wherein Ar is phenylene, naphthylene or heterocyclene which is unsubstituted or bears one or more substituents and wherein R.sup.3 is such that R.sup.3 --NH.sub.2 is an amino acid;or a pharmaceutically-acceptable salt or ester thereof. The compounds possess anti-tumor activity.
    Type: Grant
    Filed: September 5, 1990
    Date of Patent: January 14, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventor: Leslie R. Hughes
  • Patent number: 5081121
    Abstract: Quinolone derivatives having a quinolone structure: ##STR1## where Yo is O or S are disclosed, which are useful as cardiotonic agents. Typical examples of the quinolone derivatives include: 6,7-dimethoxy-4 (1H) quinolone (compound 6) and 5-hydroxy-6-methoxy-4(1H) quinolone (compound 1) as typical compounds of the formulae[I] and [I'], respectively, shown in the specification.
    Type: Grant
    Filed: May 23, 1989
    Date of Patent: January 14, 1992
    Inventors: Tatsushi Osawa, Hideo Ohta, Kohji Akimoto, Katsuhiko Harada, Hiroshi Soga, Yasuhiro Jinno
  • Patent number: 5081147
    Abstract: Compounds of the formula ##STR1## where R.sub.1 is H or alkyl of 1 to 20 carbons, CO--R.sub.1 *, CO--O--R.sub.1 *, CO--NH--R.sub.1 *, or PO(OR.sub.1 *).sub.2, PO(OR.sub.1 *)R.sub.1 * where R.sub.1 * independently is H, alkyl of 1 to 20 carbons, phenyl, or substituted phenyl;R.sub.2 is H or alkyl of 1 to 20 carbons;X is H, R.sub.3, CO--R.sub.3, CO--O--R.sub.3, CO--NH--R.sub.3, CO--N--(R.sub.3).sub.2, PO(OR.sub.3).sub.2, PO(OR.sub.3)R.sub.3, and R.sub.3 independently is H, phenyl, substituted phenyl, alkyl of 1 to 20 carbons or is alkyl of 1 to 20 carbons substituted with a hydroxyl, alkoxy, substituted amino, thioalkoxy or with a COR.sub.3 * group where R.sub.3 * is H, lower alkyl, OH, OR.sub.3 **, NH.sub.2, NHR.sub.3 ** or N(R.sub.3 **).sub.2 group wherein R.sub.3 ** independently is H or lower alkyl, with the proviso that when X is CO--O--R.sub.3 or is CO--NH--R.sub.3 then R.sub.3 is not hydrogen;Y is H, R.sub.4, CO--R.sub.4, CO--O--R.sub.
    Type: Grant
    Filed: March 15, 1990
    Date of Patent: January 14, 1992
    Assignee: Allergan, Inc.
    Inventor: Gary C. M. Lee
  • Patent number: 5081246
    Abstract: Novel quinoline sulfonamino derivatives having a vessel smooth muscle relaxation activity as well as a platelet agglutination inhibitory activity and inhibitory activity to protein kinase A, myosin light chain kinase, proteinkinase C, and calmodulindependent proteinkinase II, but having little action or cardio function; a process for the production of the derivatives, and a pharmaceutical composition containing the derivative.
    Type: Grant
    Filed: December 20, 1989
    Date of Patent: January 14, 1992
    Assignees: Hiroyoshi Hidaka, Tobishi Yakuhin Kogyo Kabushiki Kaisha
    Inventors: Horoyoshi Hidaka, Tomohiko Ishikawa, Masatoshi Hagiwara, Tsutomu Inoue, Kenji Naitoh, Osamu Sakuma, Masayuki Yuasa, Tadashi Morita, Tadashi Toshioka, Isao Umezawa, Takashi Inaba
  • Patent number: 5081261
    Abstract: Compounds of Formula 1, and of Formula 2, ##STR1## in which R.sub.1 is H or alkyl of 1 to 20 carbons, CO--R.sub.1.sup.* CO--O--R.sub.1.sup.* CO--NH--R.sub.1.sup.* or PO(OR.sub.1.sup.*).sub.2 or PO(OR.sub.1.sup.*)R.sub.1.sup.* where R.sub.1.sup.* independently is H, alkyl of 1 to 20 carbons, phenyl, or substituted phenyl; R.sub.2 is H, alkyl of 1 to 20 carbons, or R.sub.2 and Y jointly represent a heterocycle which incorporates the sulfonamide nitrogen in the ring as a heteroatom; R.sub.3 is H or alkyl of 1 to 20 carbons; X is H, R.sub.4, CO--R.sub.4, CO--O--R.sub.4, CO--NH--R.sub.4, CO--N--(R.sub.4).sub.2, PO(OR.sub.4).sub.2 or PO(OR.sub.4)R.sub.4, and R.sub.4 independently is H, phenyl, substituted phenyl, alkyl of 1 to 20 carbons or is alkyl of 1 to 20 carbons substituted with a hydroxyl, alkoxy, substituted amino, thioalkoxy, with a O--COR.sub.4.sup.* group or with a COR.sub.4.sup.* group where R.sub.4.sup.* is H, lower alkyl, OH, OR.sub.4.sup.**, NH.sub.2, NHR.sub.4.sup.** or N(R.sub.4.sup.**).sub.
    Type: Grant
    Filed: March 23, 1990
    Date of Patent: January 14, 1992
    Assignee: Allergan, Inc.
    Inventor: Gary C. M. Lee
  • Patent number: 5077429
    Abstract: The invention relates to 7-amino-1-cyclo-propyl-4-oxo-1,4-dihydro-naphthyridine (or quinoline)-3-carboxylic acids of Formula I as defined in the specification. Also included in the invention is a process for the preparation of said compounds of Formula I and Ia. Further, the invention includes compositions containing the compounds of Formula I or Ia and the use of said compounds and compositions as antibacterial agents.
    Type: Grant
    Filed: April 1, 1986
    Date of Patent: December 31, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Grohe, Hans-Joachim Zeiler, Karl G. Metzger
  • Patent number: 5073556
    Abstract: Compounds of formula (I): ##STR1## (in which: R.sup.1 represents fluorinated methoxy; R.sup.2 represents a nitrogen-containing heterocyclic group and R.sup.3 represents hydrogen or amino) and pharmaceutically acceptable salts, esters and amides thereof are valuable antibacterial agents, which may be prepared by reacting a compound similar to that of formula (I) but in which R.sup.2 is replaced by a halogen atom with a compound providing the required group R.sup.2.
    Type: Grant
    Filed: February 22, 1991
    Date of Patent: December 17, 1991
    Assignees: Sankyo Company Limited, Ube Industries Limited
    Inventors: Masayuki Iwata, Tomio Kimura, Teruhiko Inoue, Yoshimi Fujihara, Tetsushi Katsube
  • Patent number: 5071860
    Abstract: Insecticidally active substituted heteroaryl phenyl ethers of the formula ##STR1## in which Het represents an optionally substituted heteroaromatic radical,X represents O, S, --CH.sub.2 --, --O--CH.sub.2 --, --S--CH.sub.2 --, --CH.sub.2 --O--, ##STR2## Y represents O, --O--CH.sub.2 -- or S, Z represents an optionally substituted aromatic or heteroaromatic radical;m represents integers from 1-4n represents 0, 1, 2, 3, 4O represents 0, 1, 2, 3, 4, provided than n and o do not simultaneously represent 0p represents integers from 1-4,R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently of one another represent hydrogen, C.sub.1 -C.sub.6 -alkyl which is optionally substituted; two radicals adjacent to one another can also, together with the C atoms to which they are bonded, form a saturated carbocyclic 5- or 6-ring,R.sup.1 represents identical or different radicals hydrogen, halogen, CN, C.sub.1-4 -alkyl, 1-5-halogeno-C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy, C.sub.1-4 -alkylthio, 1-5-halogeno-C.sub.
    Type: Grant
    Filed: March 7, 1990
    Date of Patent: December 10, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd Alig, Wilhelm Stendel, Michael Londershausen
  • Patent number: 5071856
    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 11, 1989
    Date of Patent: December 10, 1991
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Shigeharu Tamada, Takafumi Fujioka, Hidenori Ogawa, Shuji Teramoto, Kazumi Kondo
  • Patent number: 5068264
    Abstract: The invention relates to new formylpiperazine group-containing (meth)acrylic acid esters and (meth)acrylamides (I) of the general formula (L) ##STR1## in which R.sup.1 is hydrogen or methyl,R.sup.2 is a divalent aliphatic or cycloaliphatic radical, andX is --O-- or --NH--,and to preparations which contain these compounds, for use as adhesive component for the treatment of collagen-containing materials, and to processes for the preparation and to the use of the preparations.
    Type: Grant
    Filed: April 12, 1990
    Date of Patent: November 26, 1991
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Muller, Wolfgang Podszun
  • Patent number: 5064833
    Abstract: 2,4-diaminoquinazoline compounds are inhibitors of the H.sup.+ K.sup.+ ATPase enzyme and useful for the treatment of diseases of the stomach based on excessive gastric acid secretion. A compound of the invention is 2-[2-methyl-4-fluorophenyl)amino]-4-(N-methylphenylamino)quinazoline.
    Type: Grant
    Filed: May 8, 1990
    Date of Patent: November 12, 1991
    Assignee: Smithkline Beecham Intercredit B.V.
    Inventors: Robert J. Ife, Thomas H. Brown, Colin A. Leach, David J. Keeling
  • Patent number: 5061714
    Abstract: The use of isoquinoline derivatives for the treatment of glaucoma or ocular hypertension. The isoquinoline derivatives are of formula I ##STR1## wherein R.sub.1 is a hydrogen or a C.sub.1 -C.sub.6 alkyl group and R.sub.2 is a C.sub.1 -C.sub.6 alkyl group. The stability of the isoquinoline derivatives when used in the form of a solution is improved by incorporating therein compounds having a phenolic hydroxyl group and/or glycols serving as a stabilizer.
    Type: Grant
    Filed: March 4, 1991
    Date of Patent: October 29, 1991
    Assignee: Nisshin Flour Milling Co., Ltd.
    Inventors: Toyohiro Tadokoro, Kiyoshi Sato, Shigeki Hatakeyama, Shigeo Kawase, Masao Ueno
  • Patent number: 5059608
    Abstract: The invention relates to a compound useful as an anticonvulsant, and for treatment of delayed neuronal death, the compound being a bicyclic amine of the formula: ##STR1## wherein R.sup.1 is lower alkyl,R.sup.2 is aryl which may have one or more suitable substituent(s), cyclo(lower)alkyl or heterocyclic group,R.sup.3 is hydrogen, lower alkyl which may have one or more suitable substituent(s), lower alkenyl, or acyl which may have one or more suitable substituent(s),R.sup.4 is hydrogen, lower alkyl, or hydroxy(lower)alkyl,R.sup.5 is hydrogen, lower alkyl, halogen, or protected amino, andn is an integer of 1 or 2, with the proviso that when R.sup.3 is lower alkyl which may have one or more suitable substituent(s), R.sup.2 is cyclo(lower)alkyl or heterocyclic group,or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 23, 1989
    Date of Patent: October 22, 1991
    Assignee: Fujisawa Pharmaceutical Company, Ltd.
    Inventors: Hisashi Takasugi, Atsushi Kuno, Mitsuru Ohkubo
  • Patent number: 5051505
    Abstract: A novel process for preparing piperazinyl quinolone derivatives of the formula (I) is disclosed. The process comprises reacting dihaloquinolones with piperazine derivatives and tetraalkyl ammonium halides in the presence of a polar solvent such as acetonitrile, dimethylformamide, pyridine, sulfolane and dimethyl sulfoxide.
    Type: Grant
    Filed: August 2, 1990
    Date of Patent: September 24, 1991
    Assignee: Korea Institute of Science and Technology
    Inventors: Sang W. Park, You S. Kim, Jin H. Lee