Patents Examined by D. Margaret M. Mach
  • Patent number: 5700813
    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: December 23, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Albert A. Carr, John M. Kane, David A. Hay
  • Patent number: 5700828
    Abstract: A method for treating or preventing anoxic or ischemic brain injury that includes administering melatonin to a person who is suffering from or has a high risk of suffering from an anoxic or ischemic insult or injury. The method may also include administering complementary agents.
    Type: Grant
    Filed: December 7, 1995
    Date of Patent: December 23, 1997
    Assignee: Life Resuscitation Technologies, Inc.
    Inventors: Michael G. Federowicz, Gregory M. Fahy, Lawrence E. Wood
  • Patent number: 5700812
    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: December 23, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Albert A. Carr, John M. Kane, David A. Hay
  • Patent number: 5698699
    Abstract: Processes for production of quinoline or quinazoline derivatives and intermediates therefor ##STR1## A process for producing a compound of formula (2) of value as antiinflammatory agents, which comprises reacting a compound of formula (3) or a salt thereof with 4-amino-1,2,4-triazole to give a compound of formula (1) or a salt thereof and deaminating the same, and an intermediate compound (1).In the above formulas, Y represents N or C-G in which G represents carboxyl which may be esterified or amidated, acyl, hydroxyalkyl which may be protected, or halogen; ring A and ring B each may be substituted; k is equal to 0 or 1; X represents a leaving group.
    Type: Grant
    Filed: September 26, 1995
    Date of Patent: December 16, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yoshiharu Maeda, Atsushi Inagaki
  • Patent number: 5698579
    Abstract: Cyclic amides are inhibitors of tumor necrosis factor and can be used to combat cachexia, endotoxic shock, and retrovirus replication. A typical embodiment is 3-phenyl-3-(1-oxoisoindolin-2-yl)propionamide.
    Type: Grant
    Filed: August 27, 1996
    Date of Patent: December 16, 1997
    Assignee: Celgene Corporation
    Inventor: George W. Muller
  • Patent number: 5698494
    Abstract: Substituted N-phenylglutarimides I ##STR1## X.sup.1, X.sup.2 =O, S; R.sup.1 =halogen, NO.sub.2, CN, CF.sub.3 ; R.sup.2 =H, halogen;R.sup.3, R.sup.4, R.sup.5 =H, halogen, CN, alkyl, cyctoalkyl, alkenyl, alkynyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkyl-thio, cyanoalkyl, alkoxycarbonyl, unsubstituted or substituted phenyl or benzyl,or 2 substituents of a C atom or 2 substituents of adjacent C atoms of the glutarimide ring are bonded to one another via a chain which may be substituted;A=CHR.sup.6 --CHR.sup.7 --CO--B or CR.sup.6 .dbd.CR.sup.8 --CO--B;R.sup.6 =H, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -haloalkyl;R.sup.7 =halogen, haloalkyl, OH, alkoxy or alkylcarbonyloxy;R.sup.
    Type: Grant
    Filed: April 26, 1995
    Date of Patent: December 16, 1997
    Assignee: BASF Aktiengesellschaft
    Inventors: Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schaefer, Uwe Kardorff, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
  • Patent number: 5696103
    Abstract: A method for treating osteoporosis via administration of a compound of the formula, 1.alpha.-fluoro-25-hydroxy-16-ene-23-yne-26,27-hexafluorocholecalciferol, in an amount therapeutically effective to restore bone density to an asymptomatic level, without inducing hypercalciuria, hypercalcemia, or nephrotoxicity is provided.
    Type: Grant
    Filed: November 17, 1995
    Date of Patent: December 9, 1997
    Assignees: Syntex (U.S.A.) Inc., Hoffmann-La Roche Inc.
    Inventors: John Joseph Nestor, Jr., Brian Henry Vickery, Milan Radoje Uskokovic
  • Patent number: 5696132
    Abstract: Quinolone derivatives are known as synthetic antimicrobial agents having a condensed pyridonecarboxylic acid skeleton, and those having substituents on various replaceable positions of said skeleton are known. In particular, if diastereomers exist, there are 4 or more kinds of stereoisomers. A mixture of diastereomers is a mixture of isomers having different physical properties and is difficult to apply as a drug as such. The present invention provides an antimicrobial 1-(1,2-cis-2-fluorocyclopropyl)-substituted quinolone derivative represented by formula I shown below which, although involving diastereomers, consists of a single stereoisomer. ##STR1## wherein R.sup.1 represents a methyl group, a difluoromethyl group, etc.; R.sup.2 represents a saturated nitrogen-containing heterocyclic group; A represents C--X.sup.3 or a nitrogen atom; X.sup.1 and X.sup.2 each represents a halogen atom; and X.sup.3 and Z represent a hydrogen atom, etc.
    Type: Grant
    Filed: January 26, 1994
    Date of Patent: December 9, 1997
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Isao Hayakawa, Youichi Kimura, Hisashi Takahashi
  • Patent number: 5693650
    Abstract: 4-(Quinolin-2-yl-methoxy)-phenyl-acetic acid derivatives are prepared by reacting quinoline-methoxy-phenyl-acetic acids with the corresponding glycinol derivatives, if appropriate with activation of the carboxylic acid function. The new compounds are suitable as active compounds in medicaments, in particular in antiatherosclerotic medicaments.
    Type: Grant
    Filed: December 5, 1995
    Date of Patent: December 2, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Muller, Richard Connell, Siegfried Goldmann, Klaus-Helmut Mohrs, Rolf Angerbauer, Matthias Muller-Gliemann, Ulrich Niewohner, Rudi Grutzmann, Martin Beuck, Stefan Wohlfeil, Hilmar Bischoff, Dirk Denzer
  • Patent number: 5693315
    Abstract: A tooth sensitivity treating composition containing hydroxyethyl methacrylate, sodium fluoride, anti,icrobial compound and an inert solvent, with an antidegenerate preserative.
    Type: Grant
    Filed: June 10, 1996
    Date of Patent: December 2, 1997
    Assignee: Abco Trust
    Inventor: Al Bevilacqua
  • Patent number: 5693815
    Abstract: Compounds of formula ##STR1## wherein Ar, W, Z, Q, R.sub.1, U, and L are as set forth herein, are described. These compounds are active as agents against HIV and inhibit renin and therefore are also active against hypertension. Similar retroviruses against which the compounds of the invention are active include the retrovirus which causes feline AIDS, and the retrovirus which causes Rous' sarcoma which is a disease of chickens.
    Type: Grant
    Filed: July 14, 1995
    Date of Patent: December 2, 1997
    Assignee: Schering Corporation
    Inventors: Frank Bennett, Viyyoor M. Girijavallabhan, Naginbhai M. Patel
  • Patent number: 5693814
    Abstract: A method for selectively obtaining any one of an anhydrate, a 1/2 hydrate, a 1 hydrate, and a 3/2 hydrate of 7-?(7-(S)-amino-5-azaspiro?2.4!heptan-5-yl!-8-chloro-6-fluoro-1-?(1R,2S)-2 -fluorocyclopropyl!-4-oxo-1,4-dihydroquinoline-3-carboxylic acid is disclosed, comprising treating the compound in an aqueous solvent or water or recrystallizing the compound from an aqueous solvent or water.
    Type: Grant
    Filed: September 12, 1994
    Date of Patent: December 2, 1997
    Assignee: Daiichi Pharmaceutical Co., Ltd.
    Inventors: Youichi Kimura, Katsuhiro Kawakami, Norimasa Mikata, Keiji Uchiyama, Tazuo Uemura, Yusuke Yukimoto
  • Patent number: 5688815
    Abstract: Described are 3-hydroxypyridin-4-ones of formula I ##STR1## wherein R.sub.1 -R.sub.4, A and B are as defined in the description. The compounds have valuable pharmaceutical properties and are especially effective as chelators of iron. They can be used to treat excess iron in the bodies of warm-blooded animals.
    Type: Grant
    Filed: September 27, 1996
    Date of Patent: November 18, 1997
    Assignee: Ciba Geigy Corporation
    Inventor: Paul Zbinden
  • Patent number: 5686619
    Abstract: Provided is a process for preparing chloroalkyl pyridinium hydrochloride compounds and various regioisomers and analogs thereof having substantially high purity levels and yields and a free-flowing, non-dusting form.
    Type: Grant
    Filed: March 6, 1995
    Date of Patent: November 11, 1997
    Assignee: Cytec Technology Corp.
    Inventors: William Elliott Bay, Matthew A. Brown, David R. Kilanowski
  • Patent number: 5686486
    Abstract: The present invention relates to compounds of formula I which are 4-hydroxy-benzopyran-2-ones and 4-hydroxy-cycloalkyl?b!pyran-2-ones useful for inhibiting a retrovirus in a mammalian cell infected with said retrovirus. ##STR1## Wherein R.sub.10 and R.sub.
    Type: Grant
    Filed: August 4, 1995
    Date of Patent: November 11, 1997
    Assignee: Pharmacia & Upjohn Company
    Inventors: Paul Kosta Tomich, Michael John Bohanon, Steven Ronald Turner, Joseph Walter Strohbach, Suvit Thaisrivongs, Richard C. Thomas, Karen Rene Romines, Chih-Ping Yang, Paul Adrian Aristoff, Harvey Irving Skulnick, Paul D. Johnson, Ronald B. Gammill, Qingwei Zhang, Gordon L. Bundy, David John Anderson, Lee S. Banitt
  • Patent number: 5681839
    Abstract: This invention concerns a compound of generic formula ##STR1## or a pharmaceutically acceptable salt thereof, where the dotted lines represent optional bonds,R.sup.3 is an optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl group;R.sup.4 represents hydrogen, or a group of formula --CR.sup.a R.sup.b R.sup.c where R.sup.a, R.sup.b and R.sup.c are independently selected from hydrogen, C.sub.1 -C.sub.6 alkyl C.sub.6 -C.sub.10 aryl, heteroaryl, C.sub.1 -C.sub.6 alkyl substituted by optionally substituted C.sub.6 -C.sub.10 aryl or heteroaryl;R' represents one or more optional substituents the same or different, selected from halogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkoxycarbonyl, C.sub.1 -C.sub.6 hydroxyalkyl, CN, aminocarbonyl, C.sub.2 -C.sub.7 alkanoyloxy(C.sub.1 -C.sub.6)alkyl, carboxy, C.sub.2 -C.sub.7 alkanoxylamino, C.sub.6 -C.sub.10 or heteroaryl or an (C.sub.6 -C.sub.
    Type: Grant
    Filed: December 7, 1995
    Date of Patent: October 28, 1997
    Assignee: John Wyeth & Brother
    Inventors: Roger Crossley, Albert Opalko, Barry John Langham
  • Patent number: 5679623
    Abstract: Compounds of the formula ##STR1## in which R.sub.l, R.sub.2, R.sub.3, R.sub.4, Y and Z are as defined in claim 1, and, if appropriate, the tautomers thereof, in each case in free form or in salt form, can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: October 21, 1997
    Assignee: Ciba-Geigy Corporation
    Inventors: Henry Szczepanski, Haukur Kristinsson
  • Patent number: 5674878
    Abstract: Compound of general formula I ##STR1## wherein A is a benzo or thieno group;R.sub.1 is (C.sub.4-6)cycloalkyl, (C.sub.4-6)cycloalkyl-(C.sub.1-5)alkyl or ##STR2## R.sup.2, m, R.sup.3, R.sup.4, R and u are defined as in the specification, and pharmaceutical preparations containing this compound and the new pharmaceutical uses thereof.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 7, 1997
    Assignee: Boehringer Ingelheim KG
    Inventors: Dietrich Arndts, Walter Losel, Otto Roos
  • Patent number: 5675010
    Abstract: The present invention relates to new chloropyridinium chlorides of the general formula (I) ##STR1## in which R.sup.1 represents in each case optionally substituted alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, arylalkyl or heteroarylalkyl,R.sup.2 represents optionally substituted alkyl, andR.sup.3 represents hydrogen, halogen or optionally substituted alkyl,to a process for their preparation and to their use for the preparation of chloropyridines.
    Type: Grant
    Filed: May 8, 1996
    Date of Patent: October 7, 1997
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhard Lantzsch, Klaus Jelich, Carl Casser, Christoph Mannheims, Knud Lawrenz
  • Patent number: 5670518
    Abstract: Unsubstituted or substituted halo nitro and nitroso compounds and their metabolites are potent, selective and non-toxic inhibitors and supressants of cancer growth and viral infections in a mammalian host. The compounds are particularly useful for treatment and supression of tumors and viruses associated with breast cancer, AIDS, herpetic episodes and cytomegaloviral infections. The methods of treatment of tumorigenic and viral diseases by halo nitro and nitroso compounds and their metabolites are described.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 23, 1997
    Inventors: Ernest Kun, Jerome Mendeleyev, Eva Kirsten