Tricyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/344)
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Patent number: 5885988Abstract: 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: GrantFiled: January 7, 1998Date of Patent: March 23, 1999Assignee: Novartis AGInventors: Peter Neumann, Paul Pfaeffli, Max Peter Seiler, Robert Swoboda
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Patent number: 5854245Abstract: 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: GrantFiled: June 26, 1997Date of Patent: December 29, 1998Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Melissa S. Egbertson, George D. Hartman, Steven D. Young, Nathan C. Ihle
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Patent number: 5854237Abstract: 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: GrantFiled: June 17, 1997Date of Patent: December 29, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Efren Guillermo Delos Santos
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Patent number: 5852018Abstract: 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: GrantFiled: November 4, 1996Date of Patent: December 22, 1998Assignee: Xenova LimitedInventors: Justin Stephen Bryans, Christopher John Latham, Stephen James Brocchini
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Patent number: 5849742Abstract: 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: GrantFiled: May 9, 1997Date of Patent: December 15, 1998Assignees: Sugen Inc., Yissum Research Development Co. of The Hebrew Universuty of JerusalemInventors: Harald App, Gerald M. McMahon, Peng Cho Tang, Aviv Gazit, Alexander Levitzki
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Patent number: 5849743Abstract: 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: GrantFiled: June 20, 1997Date of Patent: December 15, 1998Assignee: BASF AktiengesellschaftInventors: Wilfried Lubisch, Berthold Behl, Hans Peter Hofmann
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Patent number: 5843944Abstract: 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: GrantFiled: July 11, 1997Date of Patent: December 1, 1998Assignee: American Cyanamid CompanyInventors: Jay Donald Albright, Marvin Fred Reich, Fuk-Wah Sum, Efren Guillermo Delos Santos
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Patent number: 5785720Abstract: 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: GrantFiled: September 6, 1996Date of Patent: July 28, 1998Assignee: Ciba Specialty Chemicals CorporationInventors: Thomas Eichenberger, Thomas Ruch
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Patent number: 5780471Abstract: 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: GrantFiled: May 23, 1996Date of Patent: July 14, 1998Assignee: American Cyanamid CompanyInventors: Aranapakam M. Venkatesan, Jay D. Albright, George T. Grosu
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Patent number: 5773439Abstract: 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: GrantFiled: December 20, 1996Date of Patent: June 30, 1998Assignee: BASF AktiengesellschaftInventors: Wilfried Lubisch, Berthold Behl, Hans Peter Hofmann
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Patent number: 5750526Abstract: 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: GrantFiled: December 27, 1995Date of Patent: May 12, 1998Assignee: Schering AktiengesellschaftInventors: Martin Kruger, Werner Seelen, Lechoslaw Turski
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Patent number: 5733648Abstract: 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: GrantFiled: February 23, 1996Date of Patent: March 31, 1998Assignee: Minnesota Mining and Manufacturing CompanyInventors: Ernest L. Thurber, Eric G. Larson, Alan R. Kirk, Gregg D. Dahlke
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Patent number: 5721234Abstract: 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: GrantFiled: October 23, 1995Date of Patent: February 24, 1998Assignee: Warner-Lambert CompanyInventors: Christopher Franklin Bigge, Daniel Martin Retz
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Patent number: 5712395Abstract: 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: GrantFiled: February 9, 1995Date of Patent: January 27, 1998Assignees: Yissum Research Development Corp., SugenInventors: Harald App, Gerald M. McMahon, Peng Cho Tang, Aviv Gazit, Alexander Levitzki
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Patent number: 5710138Abstract: 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: GrantFiled: January 22, 1996Date of Patent: January 20, 1998Assignee: Schering AktiengesellschaftInventors: Peter Holscher, Lechoslaw Turski
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Patent number: 5708123Abstract: 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: GrantFiled: June 26, 1995Date of Patent: January 13, 1998Assignee: NKT Research Center A/SInventors: Ib Johannsen, Mikkel J.o slashed.rgensen
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Patent number: 5696130Abstract: 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: GrantFiled: June 5, 1995Date of Patent: December 9, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, David T. Winn, Mark E. Goldman, Lawrence G. Hamann, Lin Zhi, Luc J. Farmer, Robert L. Davis
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Patent number: 5696127Abstract: 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: GrantFiled: June 5, 1995Date of Patent: December 9, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Lin Zhi, James P. Edwards, Christopher M. Tegley, Sarah J. West
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Patent number: 5693647Abstract: 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: GrantFiled: June 5, 1995Date of Patent: December 2, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Lin Zhi, Christopher M. Tegley, David T. Winn, Lawrence G. Hamann, James P. Edwards, Sarah J. West
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Patent number: 5693646Abstract: 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: GrantFiled: June 5, 1995Date of Patent: December 2, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Christopher M. Tegley, Lin Zhi, James P. Edwards, Sarah J. West
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Patent number: 5688808Abstract: 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: GrantFiled: June 5, 1995Date of Patent: November 18, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, David T. Winn, Lin Zhi, Lawrence G. Hamann, Christopher M. Tegley, Charlotte L. F. Pooley
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Patent number: 5688791Abstract: 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: GrantFiled: September 11, 1995Date of Patent: November 18, 1997Assignee: UBE Industries, LTD.Inventors: Tomio Kimura, Tetsushi Katsube
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Patent number: 5688810Abstract: 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: GrantFiled: June 5, 1995Date of Patent: November 18, 1997Assignee: Ligand Pharmaceuticals IncorporatedInventors: Todd K. Jones, Mark E. Goldman, Charlotte L.F. Pooley, David T. Winn, James P. Edwards, Sarah J. West, Christopher M. Tegley, Lin Zhi
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Patent number: 5656759Abstract: 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: GrantFiled: June 7, 1995Date of Patent: August 12, 1997Assignee: Sony CorporationInventors: Kengo Ito, Masanobu Hida, Kaori Isaji
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Patent number: 5646146Abstract: 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: GrantFiled: May 25, 1995Date of Patent: July 8, 1997Assignee: Novo Nordisk A/SInventors: Peter Faarup, Palle Jakobsen, Anker Steen J.o slashed.rgensen, Henrik Klitgaard
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Patent number: 5633371Abstract: 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: GrantFiled: September 15, 1995Date of Patent: May 27, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mos e Da Prada, Gerhard Z urcher
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Patent number: 5622950Abstract: 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: GrantFiled: June 2, 1995Date of Patent: April 22, 1997Assignee: Merck, Sharp & Dohme Ltd.Inventors: Raymond Baker, Neil R. Curtis, Janusz J. Kulagowski, Paul D. Leeson, Mark P. Ridgill, Adrian L. Smith
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Patent number: 5618935Abstract: 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: GrantFiled: March 24, 1995Date of Patent: April 8, 1997Assignee: Ricoh Company, Ltd.Inventors: Masayuki Shoshi, Yumi Ichikawa, Kaoru Teramura, Masayuki Koyano, Megumi Kawahara
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Patent number: 5616586Abstract: 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: GrantFiled: April 1, 1994Date of Patent: April 1, 1997Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Ryu Nagata, Norihiko Tanno, Toru Kodo
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Patent number: 5602168Abstract: 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: GrantFiled: June 5, 1995Date of Patent: February 11, 1997Assignee: Neurogen CorporationInventors: Xiao-shu He, Brian de Costa, Jan W. F. Wasley
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Patent number: 5599812Abstract: 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: GrantFiled: April 29, 1994Date of Patent: February 4, 1997Assignee: Adir Et CompagnieInventors: Sylvain Rault, Jean-Charles Lancelot, Herv e Prunier, Max Robba, Philippe Delagrange, Pierre Renard, G erard Adam
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Patent number: 5597922Abstract: 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: GrantFiled: July 29, 1994Date of Patent: January 28, 1997Assignees: 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 CaliforniaInventors: Sui X. Cai, John F. W. Keana, Eckard Weber
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Patent number: 5545835Abstract: 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: GrantFiled: November 4, 1994Date of Patent: August 13, 1996Assignee: American Cyanamid CompanyInventor: Henry L. Strong
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Patent number: 5541330Abstract: 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: GrantFiled: May 12, 1995Date of Patent: July 30, 1996Assignee: Eastman Kodak CompanyInventors: Trevor J. Wear, Christopher P. Moore, Paul D. Beer, John W. Wheeler
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Patent number: 5538971Abstract: 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: GrantFiled: May 27, 1994Date of Patent: July 23, 1996Assignee: Sandoz Ltd.Inventors: Peter Gull, Rudolf Markstein, Robert Swoboda
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Patent number: 5521173Abstract: 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: GrantFiled: January 17, 1995Date of Patent: May 28, 1996Assignee: American Home Products CorporationInventors: Aranapakam M. Venkatesan, Jay D. Albright, George T. Grosu
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Patent number: 5516774Abstract: 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: GrantFiled: June 13, 1994Date of Patent: May 14, 1996Assignee: American Cyanamid CompanyInventors: Jay D. Albright, Marvin F. Reich, Fuk-Wah Sum, Efren G. Delos Santos
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Patent number: 5468748Abstract: 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: GrantFiled: January 31, 1994Date of Patent: November 21, 1995Inventors: Peter Faarup, Palle Jakobsen, Anker S. Jorgensen, Henrik Klitgaard
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Patent number: 5436240Abstract: 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: GrantFiled: October 6, 1993Date of Patent: July 25, 1995Assignee: The Upjohn CompanyInventors: Malcolm W. Moon, Richard F. Heier, Jeanette K. Morris
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Patent number: 5405847Abstract: 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: GrantFiled: August 24, 1993Date of Patent: April 11, 1995Assignee: Asta Medica AktiengesellschaftInventors: Hans-Reinhold Dieter, Jurgen Engel, Karl-Heinz Klingler, Bernhard Kutscher, Stefan Szelenyi, Ute Achterath-Tuckermann, Jurgen Schmidt, Peter Metzenauer
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Patent number: 5389653Abstract: 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: GrantFiled: April 16, 1993Date of Patent: February 14, 1995Assignee: Hoffman-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
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Patent number: 5378843Abstract: 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: GrantFiled: November 22, 1993Date of Patent: January 3, 1995Assignee: American Cyanamid CompanyInventor: Henry L. Strong
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Patent number: 5288866Abstract: 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: GrantFiled: October 14, 1992Date of Patent: February 22, 1994Assignee: American Cyanamid CompanyInventor: Henry L. Strong
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Patent number: 5246933Abstract: 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: GrantFiled: August 6, 1992Date of Patent: September 21, 1993Assignee: Imperial Chemical Industries PLCInventors: Michael D. Turnbull, John Finney
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Patent number: 5237060Abstract: 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: GrantFiled: February 23, 1989Date of Patent: August 17, 1993Assignee: Bayer AktiengesellschaftInventors: Michael Schriewer, Klaus Grohe, Hans-Joachim Zeiler, Karl Metzger
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Patent number: 5153195Abstract: 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: GrantFiled: November 15, 1991Date of Patent: October 6, 1992Assignee: Novo Nordisk A/SInventors: Tage Honore, Poul Jacobsen, Flemming E. Nielsen, Lars Naerum
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Patent number: 5136099Abstract: 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: GrantFiled: August 1, 1990Date of Patent: August 4, 1992Assignee: Scripps Clinic and Research FoundationInventors: Golfo Skokotas, Kyriacos C. Nicolaou
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Patent number: 5126344Abstract: 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: GrantFiled: November 19, 1990Date of Patent: June 30, 1992Assignee: Imperial Chemical Industries PLCInventors: David A. Roberts, Robert J. Pearce, Robert H. Bradbury, Richard W. A. Luke
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Patent number: 5109006Abstract: 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: GrantFiled: August 22, 1991Date of Patent: April 28, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Marcel Hibert
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Patent number: 5101032Abstract: 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: GrantFiled: October 22, 1990Date of Patent: March 31, 1992Assignee: BASF AktiengesellschaftInventors: Hans-Dieter Martin, Bernhard Albert, Knut Kessel