Tricyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/344)
  • Patent number: 5885988
    Abstract: The invention provides compounds of formula I ##STR1## wherein X, Y, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the description, and a process for preparing them. The compounds of formula I are useful as pharmaceuticals.
    Type: Grant
    Filed: January 7, 1998
    Date of Patent: March 23, 1999
    Assignee: Novartis AG
    Inventors: Peter Neumann, Paul Pfaeffli, Max Peter Seiler, Robert Swoboda
  • Patent number: 5854245
    Abstract: Fibrinogen receptor antagonists having the structureX--Y--Z--A--Band pharmaceutically acceptable salts, wherein X is a 5, 6 or 7 membered aromatic or nonaromatic ring, and Y is a 5 or 6 membered aromatic ring, e.g.
    Type: Grant
    Filed: June 26, 1997
    Date of Patent: December 29, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Melissa S. Egbertson, George D. Hartman, Steven D. Young, Nathan C. Ihle
  • Patent number: 5854237
    Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.
    Type: Grant
    Filed: June 17, 1997
    Date of Patent: December 29, 1998
    Assignee: American Cyanamid Company
    Inventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Efren Guillermo Delos Santos
  • Patent number: 5852018
    Abstract: Piperazine derivatives of formula (A): ##STR1## wherein .sub.-------- denotes an optional bond, provided that either .sub.----.sup.a.sub.---- and .sub.----.sup.c.sub.---- are both bonds and .sub.----.sup.b.sub.---- and .sub.----.sup.d.sub.---- are not bonds, or .sub.----.sup.b.sub.---- and .sub.----.sup.d.sub.---- are both bonds and .sub.----.sup.a.sub.---- and .sub.----.sup.c.sub.---- are not bonds; each of R.sub.14 and R.sub.15 is independently selected from hydrogen and C.sub.1 -C.sub.6 alkyl which is unsubstituted or substituted by an organic functional group; and each of R.sub.1 to R.sub.10, which may be the same or different, is independently hydrogen or an organic functional group; and the pharmaceutically acceptable salts and esters thereof have utility as modulators of multiple drug resistance (MDR).
    Type: Grant
    Filed: November 4, 1996
    Date of Patent: December 22, 1998
    Assignee: Xenova Limited
    Inventors: Justin Stephen Bryans, Christopher John Latham, Stephen James Brocchini
  • Patent number: 5849742
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLX-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described.
    Type: Grant
    Filed: May 9, 1997
    Date of Patent: December 15, 1998
    Assignees: Sugen Inc., Yissum Research Development Co. of The Hebrew Universuty of Jerusalem
    Inventors: Harald App, Gerald M. McMahon, Peng Cho Tang, Aviv Gazit, Alexander Levitzki
  • Patent number: 5849743
    Abstract: Quinoxaline-2,3-(1H,4H)-diones of the formula I ##STR1## and their tautomeric and enantiomeric forms and their physiologically tolerated salts, the variables R, R.sup.1 and R.sup.2 have the meanings specified in claim 1, and are useful for therapeutic treatment of neurodegenerative disorders, neurotoxic disturbances or as antiepileptics, antidepressants and anxiolytics; and drugs composed thereof.
    Type: Grant
    Filed: June 20, 1997
    Date of Patent: December 15, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Wilfried Lubisch, Berthold Behl, Hans Peter Hofmann
  • Patent number: 5843944
    Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.
    Type: Grant
    Filed: July 11, 1997
    Date of Patent: December 1, 1998
    Assignee: American Cyanamid Company
    Inventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Efren Guillermo Delos Santos
  • Patent number: 5785720
    Abstract: The present invention relates to a process for bulk coloration of high molecular weight organic material, which comprises the use of a compound of the formula (I) ##STR1## in which Q is O or S, and X is C(R.sub.3) or N,R.sub.1, R.sub.2 and R.sub.3 independently of one another are hydrogen, halogen chosen from the group consisting of chlorine, bromine and fluorine, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxyl, cyano, nitro, amino, morpholino, ##STR2## in which A.sub.1 and A.sub.2 independently of one another are unsubstituted or substituted C.sub.6 -C.sub.12 aryl or C.sub.3 -C.sub.12 heteroaryl, which contains, in the ring system, 1 to 3 hetero atoms chosen from the group consisting of N, O and S, and E.sub.1 is ##STR3## or R.sub.1 and R.sub.2 together, or R.sub.1 and R.sub.3 together, are a radical A.sub.3,which A.sub.3 is unsubstituted or substituted C.sub.4 -C.sub.8 alkenylene or C.sub.8 -C.sub.12 arylene.Individual novel compounds of the formula (I) are claimed themselves.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: July 28, 1998
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Thomas Eichenberger, Thomas Ruch
  • Patent number: 5780471
    Abstract: Tricyclic diazepines of the Formula I: ##STR1## wherein A, B, D, E, F, Y, and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.
    Type: Grant
    Filed: May 23, 1996
    Date of Patent: July 14, 1998
    Assignee: American Cyanamid Company
    Inventors: Aranapakam M. Venkatesan, Jay D. Albright, George T. Grosu
  • Patent number: 5773439
    Abstract: Novel amido-quinoxalinediones of the formula ##STR1## where R.sup.1 -R.sup.5, n and m have the meanings stated in the description, and the preparation thereof are described. The compounds are suitable for controlling diseases.
    Type: Grant
    Filed: December 20, 1996
    Date of Patent: June 30, 1998
    Assignee: BASF Aktiengesellschaft
    Inventors: Wilfried Lubisch, Berthold Behl, Hans Peter Hofmann
  • Patent number: 5750526
    Abstract: Pyrido?1,2,3-de!quinoxaline derivatives of formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 each mean hydrogen, --POXY, halogen or --COR,R.sup.4 means hydrogen or OH,R.sup.5, R.sup.6 and R.sup.7 are the same or different and mean hydrogen, halogen, nitro, NR.sup.12 R.sup.13, cyano, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-4 alkoxy, orR.sup.5 and R.sup.6 or R.sup.6 and R.sup.7 represent a fused benzene ring, and means a single or double bond,are described as well as their production and use in pharmaceutical agents.
    Type: Grant
    Filed: December 27, 1995
    Date of Patent: May 12, 1998
    Assignee: Schering Aktiengesellschaft
    Inventors: Martin Kruger, Werner Seelen, Lechoslaw Turski
  • Patent number: 5733648
    Abstract: Organic compounds having at least one ethylenically-unsaturated group are described, the organic compounds being suitable for use in coatable compositions as reactive diluents; compounds of the invention preferably have a divalent organic linking moiety devoid of reactive groups other than optional ethylenically-unsaturated groups, and a polar organic moiety and are particularly adept in solubilizing aminoplast resins having radiation-curable pendant groups.
    Type: Grant
    Filed: February 23, 1996
    Date of Patent: March 31, 1998
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
  • Patent number: 5721234
    Abstract: Novel glutamate receptor antagonists represented by the formula ##STR1## or a pharmaceutically acceptable salt thereof, whereinZ is an alicyclic fused ring having 5 to 7 carbon atoms;R.sup.1 is hydrogen, an alkyl or an arylalkyl; andA is O, CH.sub.2, NR.sup.4, CH.sub.2 NR.sup.4, CN, tetrazole or CO wherein R.sup.4 is hydrogen, alkyl, hydroxyalkyl, aminoalkyl or aralkyl, wherein(i) when A is O, CH.sub.2, NR.sup.4 or CH.sub.2 NR.sup.4 then B is hydrogen, alkyl, alkenyl, alkynyl, aryl, aralkyl, hydroxyalkyl, alkoxy, aminoalkyl, heterocyclic, alkylheterocyclic, heterocyclic-methyl, heterocyclic-ethyl, alkylcarbonyl, cycloalkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclic-carbonyl, alkylheterocyclic-carbonyl, or when A is NR.sup.4 or CH.sub.2 NR.sup.4 then B is a naturally occurring .alpha.-amino acid moiety joined by an amide bond or B joins with R.sup.4 and the nitrogen to form a four to seven membered heterocyclic ring, provided that when Z is a fused cyclohexyl ring and R.sup.
    Type: Grant
    Filed: October 23, 1995
    Date of Patent: February 24, 1998
    Assignee: Warner-Lambert Company
    Inventors: Christopher Franklin Bigge, Daniel Martin Retz
  • Patent number: 5712395
    Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction and particularly KDR/FLK-1 receptor signal transduction in order to regulate and/or modulate vasculogenesis and angiogenesis. The invention is based, in part, on the demonstration that KDR/FLK-1 tyrosine kinase receptor expression is associated with endothelial cells and the identification of vascular endothelial growth factor (VEGF) as the high affinity ligand of FLK-1. These results indicate a major role for KDR/FLK-1 in the signaling system during vasculogenesis and angiogenesis. Engineering of host cells that express FLK-1 and the uses of expressed FLK-1 to evaluate and screen for drugs and analogs of VEGF involved in FLK-1 modulation by either agonist or antagonist activities is also described.
    Type: Grant
    Filed: February 9, 1995
    Date of Patent: January 27, 1998
    Assignees: Yissum Research Development Corp., Sugen
    Inventors: Harald App, Gerald M. McMahon, Peng Cho Tang, Aviv Gazit, Alexander Levitzki
  • Patent number: 5710138
    Abstract: Compounds of formula I ##STR1## are described, in which substituents R.sup.1 -R.sup.4 have the meanings mentioned in the application as well as their production and use in pharmaceutical agents.
    Type: Grant
    Filed: January 22, 1996
    Date of Patent: January 20, 1998
    Assignee: Schering Aktiengesellschaft
    Inventors: Peter Holscher, Lechoslaw Turski
  • Patent number: 5708123
    Abstract: Stable, electroactive material which when a potential is applied from the outside is subjected to one or more reversible redox reactions, for use in devices with an electrochromic display or another electrochromic color change or in batteries.The material comprises a condensed ring structure, the oxidized form of which is of the formula ##STR1## in which R.sub.1, R.sub.2, X, and A may have any meaning with the proviso that the condensed ring structure maintains the reversible properties.The material can be prepared by various processes and it is suited for use as electrochromic material for use in devices with an electrochromic display or as coating on windows because it presents a distinct and easily visible color change when it is subjected to a potential. In addition, the material is suited for use in rechargeable batteries because is possesses an excellent capacity and reversibility.
    Type: Grant
    Filed: June 26, 1995
    Date of Patent: January 13, 1998
    Assignee: NKT Research Center A/S
    Inventors: Ib Johannsen, Mikkel J.o slashed.rgensen
  • Patent number: 5696130
    Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: December 9, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, David T. Winn, Mark E. Goldman, Lawrence G. Hamann, Lin Zhi, Luc J. Farmer, Robert L. Davis
  • Patent number: 5696127
    Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: December 9, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, Lin Zhi, James P. Edwards, Christopher M. Tegley, Sarah J. West
  • Patent number: 5693647
    Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: December 2, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, Lin Zhi, Christopher M. Tegley, David T. Winn, Lawrence G. Hamann, James P. Edwards, Sarah J. West
  • Patent number: 5693646
    Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: December 2, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, Christopher M. Tegley, Lin Zhi, James P. Edwards, Sarah J. West
  • Patent number: 5688808
    Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: November 18, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, David T. Winn, Lin Zhi, Lawrence G. Hamann, Christopher M. Tegley, Charlotte L. F. Pooley
  • Patent number: 5688791
    Abstract: Disclosed are an aryl group- or heterocyclic group-substituted aminoquinolone compound represented by the formula (Ia), (Ib) or (Ic): ##STR1## wherein each of the substitutents are defined in the specification, or a salt of the compound, and an AIDS curing agent containing the same as an effective ingredient.
    Type: Grant
    Filed: September 11, 1995
    Date of Patent: November 18, 1997
    Assignee: UBE Industries, LTD.
    Inventors: Tomio Kimura, Tetsushi Katsube
  • Patent number: 5688810
    Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: November 18, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, Mark E. Goldman, Charlotte L.F. Pooley, David T. Winn, James P. Edwards, Sarah J. West, Christopher M. Tegley, Lin Zhi
  • Patent number: 5656759
    Abstract: When the counter ion of hydrophilic cationic dyes is substituted with an organic anion including a sulfosuffinate anion such as diethylhexylsulfonate anion, an alkylbenzenesulfonate anion such as a dodecylbenzenesulfonate, an alkylsulfate anion such as a laurylsulfate anion, or a soap anion such as a laurylsulfate anion, the cationic dyes are imparted with hydrophobicity. An ink layer 3 containing the hydrophobic cationic dye is formed on a support 2 to provide a thermal transfer ink ribbon 10.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: August 12, 1997
    Assignee: Sony Corporation
    Inventors: Kengo Ito, Masanobu Hida, Kaori Isaji
  • Patent number: 5646146
    Abstract: The present invention relates to 9H-indeno[1,2-b]pyrazin-3(4H)-ones and 9H-indeno[1,2-b]pyrazine-2,3(1H,4H)-diones or tautomeric forms thereof which are useful in treating neurological and psychiatric diseases based on the antagonism of the glycine binding site on the NMDA receptor complex.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: July 8, 1997
    Assignee: Novo Nordisk A/S
    Inventors: Peter Faarup, Palle Jakobsen, Anker Steen J.o slashed.rgensen, Henrik Klitgaard
  • Patent number: 5633371
    Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.
    Type: Grant
    Filed: September 15, 1995
    Date of Patent: May 27, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mos e Da Prada, Gerhard Z urcher
  • Patent number: 5622950
    Abstract: A class of pyrrolo[2,3-b]pyridine derivatives, substituted at the 3-position by a substituted piperazinylmethyl moiety, are antagonists of dopamine receptor subtypes within the brain, having a selective affinity for the dopamine D.sub.4 receptor subtype over other dopamine receptor subtypes, and are accordingly of benefit in the treatment and/or prevention of psychotic disorders such as schizophrenia whilst manifesting fewer side-effects than those associated with classical neuroleptic drugs.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: April 22, 1997
    Assignee: Merck, Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Neil R. Curtis, Janusz J. Kulagowski, Paul D. Leeson, Mark P. Ridgill, Adrian L. Smith
  • Patent number: 5618935
    Abstract: A pyrazine compound of formula (I) and a pyrazine compound of formula (II): ##STR1## wherein R is an unsubstituted or substituted phenyl group, an unsubstituted or substituted naphthyl group; and an electrophotographic photoconductor which includes an electroconductive support and a photoconductive layer formed thereon containing a charge generating material and a charge transporting material which is any of the above-mentioned pyrazine compounds of formula (I) and formula (II).
    Type: Grant
    Filed: March 24, 1995
    Date of Patent: April 8, 1997
    Assignee: Ricoh Company, Ltd.
    Inventors: Masayuki Shoshi, Yumi Ichikawa, Kaoru Teramura, Masayuki Koyano, Megumi Kawahara
  • Patent number: 5616586
    Abstract: Tricyclic quinoxalinediones of the formula: ##STR1## wherein X is alkyl, halogen, cyano, trifluoromethyl, nitro, hydroxy, amino, etc.; R.sup.1 is H, etc.; R.sup.2 is H, alkyl, cycloalkyl, alkenyl, alkynyl, cycloalkylalkyl, arylalkyl, substituted arylalkyl, aryl, or substituted aryl; W is H, CO.sub.2 R.sup.3, CO.sub.2 Y, CONR.sup.3 R.sup.4, CONR.sup.3 Y, CON(OR.sup.3)R.sup.4, COR.sup.3, CN, tetrazolyl, or substituted alkyl; R.sup.3 and R.sup.4 independently are H, alkyl, cycloalkyl, alkenyl, alkynyl, etc.
    Type: Grant
    Filed: April 1, 1994
    Date of Patent: April 1, 1997
    Assignee: Sumitomo Pharmaceuticals Company, Limited
    Inventors: Ryu Nagata, Norihiko Tanno, Toru Kodo
  • Patent number: 5602168
    Abstract: Disclosed are compounds of the formula ##STR1## or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy;Ar represents optionally substituted aryl or heteroarylZ represents carbon or nitrogen provided thatwhere Z is carbon, R.sub.11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; andwhere Z is nitrogen, R.sub.11 represents an electron pair;R.sub.5 is hydrogen or lower alkyl;L and m represent integers;n is 0, or an integer;R.sub.12 and R.sub.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: February 11, 1997
    Assignee: Neurogen Corporation
    Inventors: Xiao-shu He, Brian de Costa, Jan W. F. Wasley
  • Patent number: 5599812
    Abstract: The present invention relates to a compound selected from these of formula (I): ##STR1## in which A and R.sub.1 are as defined in the description, and medicinal product containing the same which is useful for treating a disorder linked to the 5-HT.sub.3 receptors.
    Type: Grant
    Filed: April 29, 1994
    Date of Patent: February 4, 1997
    Assignee: Adir Et Compagnie
    Inventors: Sylvain Rault, Jean-Charles Lancelot, Herv e Prunier, Max Robba, Philippe Delagrange, Pierre Renard, G erard Adam
  • Patent number: 5597922
    Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome, treating or preventing the adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions and inducing anesthesia are disclosed by administering to an animal in need of such treatment a compound which has high binding to the glycine receptor.
    Type: Grant
    Filed: July 29, 1994
    Date of Patent: January 28, 1997
    Assignees: State of Oregon, Acting by and through the Oregon State Board of Higher Education, Acting for and on Behalf of the Oregon Health Sciences University and the University of Oregon, Acea Pharmaceuticals, Inc., The Regents of the University of California
    Inventors: Sui X. Cai, John F. W. Keana, Eckard Weber
  • Patent number: 5545835
    Abstract: There are provided 5,6-disubstituted-3-pyridylmethyl ammonium halide compounds, a method for the preparation thereof and the use thereof for the preparation of 5-(substituted methyl)-2,3-pylidinedicarboxylic acids.
    Type: Grant
    Filed: November 4, 1994
    Date of Patent: August 13, 1996
    Assignee: American Cyanamid Company
    Inventor: Henry L. Strong
  • Patent number: 5541330
    Abstract: Ion-sensitive compounds are provided comprising a quaternary polypyridinium receptor designed to bind anionic species by the formation of a receptor-substrate complex. The receptor comprises one or more quaternary 2,2'-bipyridyl moieties. The compounds are of use in applications requiring anion detection or removal.
    Type: Grant
    Filed: May 12, 1995
    Date of Patent: July 30, 1996
    Assignee: Eastman Kodak Company
    Inventors: Trevor J. Wear, Christopher P. Moore, Paul D. Beer, John W. Wheeler
  • Patent number: 5538971
    Abstract: 6-hydroxy or 6-alkoxy-1,2,3,4,4a,5,10,10a-octahydro-benzo[g]quinoxalines bearing in position 4 an optionally substituted phenyl group may be used in the treatment of schizophrenia, drug abuse or self-injurious behavior.
    Type: Grant
    Filed: May 27, 1994
    Date of Patent: July 23, 1996
    Assignee: Sandoz Ltd.
    Inventors: Peter Gull, Rudolf Markstein, Robert Swoboda
  • Patent number: 5521173
    Abstract: Tricyclic diazepines of the Formula I: ##STR1## wherein A, B, D, E, F, Y, and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: May 28, 1996
    Assignee: American Home Products Corporation
    Inventors: Aranapakam M. Venkatesan, Jay D. Albright, George T. Grosu
  • Patent number: 5516774
    Abstract: Tricyclic diazepines of the formula: ##STR1## wherein A, B, D, E, F, Y and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: May 14, 1996
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, Marvin F. Reich, Fuk-Wah Sum, Efren G. Delos Santos
  • Patent number: 5468748
    Abstract: The present invention relates to 9H-indeno[1,2-b]pyrazin-3(4H)-ones and 9H-indeno[1,2-b]pyrazine-2,3(1H,4H)-diones or tautomeric forms thereof which are useful in treating neurological and psychiatric diseases based on the antagonism of the glycine binding site on the NMDA receptor complex.
    Type: Grant
    Filed: January 31, 1994
    Date of Patent: November 21, 1995
    Inventors: Peter Faarup, Palle Jakobsen, Anker S. Jorgensen, Henrik Klitgaard
  • Patent number: 5436240
    Abstract: Tricyclic nitrogen containing compounds, having central nervous system activity of the following structural formula: ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1, R.sub.2, and R.sub.3 are independently hydrogen, C.sub.1-6 alkyl, alkenyl, or alkynyl, C.sub.3-10 cycloalkyl, or R.sub.1 and R.sub.2 are joined to form a C.sub.3-7 cyclic amine which can contain additional heteroatoms; X is hydrogen, C.sub.1-6 alkyl, halogen, hydroxy, alkoxy, cyano, carboxamide, carboxyl, or carboalkoxyl; A is SO.sub.2, N, CH, CH.sub.2, CHCH.sub.3, C=O, C=S, C-SCH.sub.3, C=NH, C-NH.sub.2, C-NHCH.sub.3, CNHCOOCH.sub.3, or C-NHCN. B is CH.sub.2, CH, C=O, N, NH or N-CH.sub.3 ; n is 0 or 1; and D is CH, CH.sub.2, C=O, 0, N, NH or N-CH.sub.3. These new compounds are suitable for treating schizophrenia, Parkinson's disease, anxiety, depression or as compounds for lowering blood pressure in animal or human hosts.
    Type: Grant
    Filed: October 6, 1993
    Date of Patent: July 25, 1995
    Assignee: The Upjohn Company
    Inventors: Malcolm W. Moon, Richard F. Heier, Jeanette K. Morris
  • Patent number: 5405847
    Abstract: Novel compounds of the formula ##STR1## where the phenyl ring can also contain a nitrogen atom instead of a CH group, R.sub.1 is C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.3 -C.sub.6 -alkenyloxy, C.sub.3 -C.sub.6 -alkynyloxy, C.sub.2 -C.sub.6 -alkanoyloxy, benzoyloxy, morpholinocarbonyloxy, C.sub.1 -C.sub.6 -alkyloxycarbonyloxy, C.sub.1 -C.sub.6 -alkylaminocarbonyloxy, C.sub.1 -C.sub.6 -dialkylaminocarbonyloxy or the group -Alk-A, where Alk represents C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -hydroxyalkyl or C.sub.3 -C.sub.6 -cycloalkyl and the symbol A represents hydrogen or other substituents.R.sub.2, R.sub.3 and R.sub.4 represent various substituents, where R.sub.1 may also be hydrogen, when R.sub.2 is the group ##STR2## and R.sub.5 represents phenyl, C.sub.1 -C.sub.4 -alkoxyphenyl or diphenylmethyl and R.sub.3 and R.sub.4 are hydrogen and their salts. The compounds provide anti-allergic, anti-asthmatic, anxiolytic and hypotensive effects.
    Type: Grant
    Filed: August 24, 1993
    Date of Patent: April 11, 1995
    Assignee: Asta Medica Aktiengesellschaft
    Inventors: Hans-Reinhold Dieter, Jurgen Engel, Karl-Heinz Klingler, Bernhard Kutscher, Stefan Szelenyi, Ute Achterath-Tuckermann, Jurgen Schmidt, Peter Metzenauer
  • Patent number: 5389653
    Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.
    Type: Grant
    Filed: April 16, 1993
    Date of Patent: February 14, 1995
    Assignee: Hoffman-La Roche Inc.
    Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
  • Patent number: 5378843
    Abstract: There are provided 5,6-disubstituted-3-pyridylmethyl ammonium halide compounds, a method for the preparation thereof and the use thereof for the preparation of 5-(substituted methyl)-2,3-pyridinedicarboxylic acids.
    Type: Grant
    Filed: November 22, 1993
    Date of Patent: January 3, 1995
    Assignee: American Cyanamid Company
    Inventor: Henry L. Strong
  • Patent number: 5288866
    Abstract: There are provided 5,6-disubstituted-3-pyridylmethyl ammonium halide compounds, a method for the preparation thereof and the use thereof for the preparation of 5-(substituted methyl)-2,3-pyridinedicarboxylic acids.
    Type: Grant
    Filed: October 14, 1992
    Date of Patent: February 22, 1994
    Assignee: American Cyanamid Company
    Inventor: Henry L. Strong
  • Patent number: 5246933
    Abstract: Compounds of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are independently hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, halogen, haloalkyl, alkoxy, alkenoxy, alkoxyalkyl, haloalkoxy, alkylthio, cyano, nitro, amino, NR.sup.7 R.sup.8, hydroxy, acylamino, --CO.sub.2 R.sup.6, phenyl, phenoxy, benzyl or benzyloxy, the phenyl group or phenyl moiety of the benzyl group being optionally substituted; or R.sup.2 and R.sup.3 when taken together form a 5- or 6-membered ring; R.sup.6 and R.sup.8 are hydrogen or C.sub.1-4 alkyl; R.sup.7 is C.sub.1-4 alkyl; and n is 0, 1 or 2: and compositions thereof, are useful for killing or controlling nematodes.
    Type: Grant
    Filed: August 6, 1992
    Date of Patent: September 21, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Michael D. Turnbull, John Finney
  • Patent number: 5237060
    Abstract: The invention relates to a process for the preparation of highly antibacterially active enantiomerically pure 1,8-bridged 4-quinolone-3-carboxylic acids and derivatives of the formula (I) ##STR1## in which 1) a compound of the formula ##STR2## is reacted with a compound of the formula ##STR3## to form a compound of the formula ##STR4## followed by cyclization to form a compound of the formula ##STR5## and further cyclization to form a compound of the formula ##STR6## an finally reaction of the cyclized product with amines of the formula ##STR7##
    Type: Grant
    Filed: February 23, 1989
    Date of Patent: August 17, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Michael Schriewer, Klaus Grohe, Hans-Joachim Zeiler, Karl Metzger
  • Patent number: 5153195
    Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is hydroxy; andR.sup.5 and R.sup.6 together form a fused phenyl, cyclohexyl or pyridyl ring, which is optionally substituted with halogen or CN; and R.sup.7 and R.sup.8 independently are hydrogen, hydroxy, NO.sub.2, halogen, CN, CF.sub.3, C.sub.1-4 -alkoxy, acetyl, SO.sub.2 NHCOCO.sub.2 Et, SO.sub.2 NR'R' or SO.sub.2 R', wherein R' is hydrogen or C.sub.1-4 -alkyl; orR.sup.5 and R.sup.6 independently are hydroxy, hydrogen, NO.sub.2, halogen, CN, CF.sub.3, C.sub.1-4 -alkoxy, acetyl, SO.sub.2 NHCOCO.sub.2 Et, SO.sub.2 NR'R' or SO.sub.2 R', wherein R' is hydrogen or C.sub.1-4 -alkyl; and R.sup.7 and R.sup.8 together form a fused phenyl, cyclohexyl or pyridyl ring which is optionally substituted with halogen or CN.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.
    Type: Grant
    Filed: November 15, 1991
    Date of Patent: October 6, 1992
    Assignee: Novo Nordisk A/S
    Inventors: Tage Honore, Poul Jacobsen, Flemming E. Nielsen, Lars Naerum
  • Patent number: 5136099
    Abstract: 5-Hydroxy-benzo-(1',2')-cyclodeca-2,7-diyne-1-one and derivatives thereof and related fused ring diyneone macrocyclic compounds are disclosed. The compounds possess DNA-cleaving, antibiotic and tumor growth-inhibiting properties. Methods of making and using the same are also disclosed.
    Type: Grant
    Filed: August 1, 1990
    Date of Patent: August 4, 1992
    Assignee: Scripps Clinic and Research Foundation
    Inventors: Golfo Skokotas, Kyriacos C. Nicolaou
  • Patent number: 5126344
    Abstract: The invention concerns pharmaceutically useful novel compounds of the formula I, in which ring B, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, X and Z have the various meanings defined herein, and their non-toxic salts, and pharmaceutical compositions containing them. The novel compounds are of value in treating conditions such as hypertension and congestive heart failure. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.
    Type: Grant
    Filed: November 19, 1990
    Date of Patent: June 30, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: David A. Roberts, Robert J. Pearce, Robert H. Bradbury, Richard W. A. Luke
  • Patent number: 5109006
    Abstract: This invention relates to novel derivatives of 1,7'-[imidazo-[1,2-a]pyridine]5'-(6'H)ones, to the method for their preparation and to their use as anti-hypertensive, anxiety, anti-depressant and anti-migraine agents, and to their use as appetite regulators useful for the treatment of anorexia and obesity.
    Type: Grant
    Filed: August 22, 1991
    Date of Patent: April 28, 1992
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventor: Marcel Hibert
  • Patent number: 5101032
    Abstract: Cycloalkylidene dyes have the formula ##STR1## where m is 0 or 1,L is a chemical bond or C.sub.1 -C.sub.2 -alkylene, which may be substituted,R.sup.1 is hydrogen, C.sub.1 -C.sub.20 -alkyl, which may be phenyl-substituted, substituted or unsubstituted phenyl, naphthyl or C.sub.3 -C.sub.7 -cycloalkyl,Y is oxygen or two hydrogens,X.sup.1 is oxygen andX.sup.2 is C.sub.1 -C.sub.8 -alkanoyloxy, substituted or unsubstituted benzoyloxy, C.sub.1 -C.sub.6 -trialkylsilyloxy or a radical of the formula OR.sup.1 or NR.sup.2 R.sup.3, where R.sup.1 is as defined above and R.sup.2 and R.sup.3 are identical or different and each is independently of the other C.sub.1 -C.sub.20 -alkyl, which may be phenyl-substituted, substituted or unsubstituted phenyl, naphthyl, or C.sub.3 -C.sub.7 -cycloalkyl or R.sup.2 and R.sup.3 together with the nitrogen atom joining them are saturated heterocyclyl, or else one of R.sup.2 and R.sup.3 is hydrogen, or X.sup.1 and X.sup.
    Type: Grant
    Filed: October 22, 1990
    Date of Patent: March 31, 1992
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans-Dieter Martin, Bernhard Albert, Knut Kessel