Plural Chalcogens Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 546/155)
-
Patent number: 6037350Abstract: This invention comprises the novel compounds of formula (I) ##STR1## wherein the dotted line represents an optional bond; X is oxygen or sulfur; R.sup.1 is hydrogen, C.sub.1-12 alkyl, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, quinolinylC.sub.1-6 alkyl, pyridylC.sub.1-6 alkyl, hydroxyC.sub.1-6 alkyl, C.sub.1-6 alkyloxyC.sub.1-6 alkyl, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyl, aminoC.sub.1-6 alkyl, or a radical of formula -Alk.sup.1 -C(.dbd.O)--R.sup.9, -Alk.sup.1 -S(O)--R.sup.9 or -Alk.sup.1 -S(O).sub.2 --R.sup.9 ; R.sup.2, R.sup.3 and R.sup.16 each independently are hydrogen, hydroxy, halo, cyano, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, hydroxyC.sub.1-6 alkyloxy, C.sub.1-6 alkyloxyC.sub.1-6 alkyloxy, aminoC.sub.1-6 alkyloxy, mono- or di(C.sub.1-6 alkyl)aminoC.sub.1-6 alkyloxy, Ar.sup.1, Ar.sup.2 C.sub.1-6 alkyl, Ar.sup.2 oxy, Ar.sup.2 C.sub.1-6 alkyloxy, hydroxycarbonyl, C.sub.1-6 alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C.sub.2-6 alkenyl; R.sup.4 and R.sup.5 each independently are hydrogen, halo, Ar.Type: GrantFiled: May 26, 1998Date of Patent: March 14, 2000Assignee: Janssen Pharmaceutica, N.V.Inventors: Marc Gaston Venet, Patrick Rene Angibaud, Philippe Muller, Gerard Charles Sanz
-
Patent number: 6028080Abstract: The invention relates to quinoline-2-(1H)-one derivatives of the general formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are in each case independently of one another H, Hal, A or OA; R.sup.4 is H, --(CH.sub.2).sub.m --NR.sup.6 R.sup.7 ; R.sup.5 is H, --(CH.sub.2).sub.n --NR.sup.6 R.sup.7 ; R.sup.6 is H, A or, together with R.sup.7, --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --; R.sup.7 is H, A or --(CH.sub.2).sub.m -- with a bond to the same ring or adjacent ring B or D or, together with R.sup.6, --(CH.sub.2).sub.4 -- or --(CH.sub.2).sub.5 --; X is --CHR.sup.5 --, --NR.sup.5 --, --O--, --S--; A is alkyl having 1-6 C atoms; Hal is F, Cl, Br or I; m is 1-3 and n is 0-3, where at least one of the two radicals R.sup.4 or R.sup.5 has the meaning --(CH.sub.2).sub.m --NR.sup.6 R.sup.7 or --(CH.sub.2).sub.n --NR.sup.6 R.sup.7, their enantiomers, stereoisomers, salts and solvates. Such compounds are useful for the treatment of neurodegenerative diseases.Type: GrantFiled: July 17, 1998Date of Patent: February 22, 2000Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Karl-August Ackermann, Rudlof Gottschlich, Gunter Holzemann, Joachim Leibrock, Wilfried Rautenberg, Christoph Seyfried
-
Patent number: 6025378Abstract: The bicyclic heterocyclic compounds are prepared by reaction of correspondingly substituted carboxylic acids with amines, in particular with phenylglycinolamine. The bicyclic heterocyclic compounds according to the invention are suitable as active compounds in medicaments, in particular in medicaments having an antiatherosclerotic action.Type: GrantFiled: June 18, 1998Date of Patent: February 15, 2000Assignee: Bayer AktiengesellschaftInventors: Richard Connell, Siegfried Goldmann, Ulrich Muller, Stefan Lohmer, Hilmar Bischoff, Dirk Denzer, Rudi Grutzmann, Stefan Wohlfeil
-
Patent number: 5990126Abstract: A class of quinolinic sulfide derivatives of formula I are potent and specific antagonists at the strychnine insensitive glycine bitding site on the NMDA receptor complex with an pharmacological advantageous profile. They may be useful in treatment or prevention of neuro-degenerative disorders. Particularly, the compounds included in the present invention are especially useful for minimizing damage of the central nervous system arising as a consequence of ischemic or hypoxic condition such as stroke, hypoglycemia, cerebral ischemia, cardiac arrest, and physical trauma. They are also useful in prevention of chronic neurodegenerative disorders including epilepsy, Alzheimer's disease, Huntington's disease and Parkinsonism. By virtue of their NMDA receptor antagonist properties, the present compounds may also use as anticonvulsant, analgesic, antidepressant, anxiolytic, and antischizophrenic agent. Formula I ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R are defined in specification.Type: GrantFiled: March 31, 1998Date of Patent: November 23, 1999Assignee: Korea Research Institute of Chemical TechnologyInventors: No Sang Park, Churl Min Seong, Young Sik Jung, Jin Il Choi, Chang Woo Lee, Yong Jun Chung, Seung Won Choi, Jae Yang Kong, Woo Kyu Park
-
Patent number: 5969140Abstract: Naphthalene derivatives of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are each H, protected or unprotected OH, one of R.sup.3 and R.sup.4 is protected or unprotected hydroxymethyl, and the other is H, lower alkyl, or protected or unprotected hydroxymethyl, R.sup.5 and R.sup.6 are the same or different and are each H, substituted or unsubstituted lower alkyl, substituted or unsubstituted phenyl or protected or unprotected NH.sub.2, or both combine together with the adjacent N to form substituted or unsubstituted heterocyclic group, and pharmaceutically acceptable salts thereof, these compounds showing excellent bronchoconstriction inhibitory activity, and hence, being useful in the prophylaxis or treatment of asthma.Type: GrantFiled: July 2, 1998Date of Patent: October 19, 1999Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Tatsuzo Ukita, Katsuo Ikezawa, Shinsuke Yamagata
-
Patent number: 5968252Abstract: Compounds of formula ##STR1## wherein R and R' are each independently of the other hydrogen, C.sub.1 -C.sub.18 alkyl, COR.sub.1, COR.sub.2 or COOR.sub.1,X and X' are each independently of the other hydrogen, halogen, OH, NH.sub.2, COOH, C.sub.1 -C.sub.18 -alkyl, isocyclic or heterocyclic aromatic radicals, OR.sub.3, OCOR.sub.3, OCOR.sub.4, OCOR.sub.3, NHR.sub.3, N(R.sub.3).sub.2, NHCOR.sub.3, NHCOR.sub.4 or NHCOOR.sub.3,Y and Y' are each independently of the other hydrogen, halogen, OH, NH.sub.2, nitro, cyano, C.sub.1 -C.sub.18 alkyl, isocyclic or heterocyclic aromatic radicals, COR.sub.5, COR.sub.6, COOR.sub.5, COOR.sub.6, CONH.sub.2, SO.sub.2 R.sub.5, SO.sub.2 R.sub.6, SO.sub.2 NH.sub.2, SO.sub.3 H, PO(OR.sub.5).sub.2 or PO(OH).sub.2, andZ and Z' are each independently of the other hydrogen, halogen, OH, NH.sub.2, COOH, cyano, C.sub.1 -C.sub.18 alkyl, isocyclic or heterocyclic aromatic radicals, OR.sub.7, OR.sub.8, OCOR.sub.7, OCOR.sub.8, OCOOR.sub.7, NHR.sub.7, N(R.sub.7).sub.2, NHR.sub.8, CONH.sub.Type: GrantFiled: March 24, 1998Date of Patent: October 19, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Robert Moretti, Gary Wooden
-
Patent number: 5962479Abstract: Corticotropin-releasing factor (CRF) antagonists having formulae (I), (II) or (III) wherein the dashed lines, A, B, Y, Z, G, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.16 and R.sub.17 are as defined in the description, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment of CNS and stress-related disorders.Type: GrantFiled: December 6, 1996Date of Patent: October 5, 1999Assignee: Pfizer Inc.Inventor: Yuhpyng Liang Chen
-
Patent number: 5942522Abstract: Compounds useful as antihypertensive agents and useful as antiviral agents against DNA-containing viruses, such as herpes group viruses, are disclosed. The compounds are represented by Formula 1.0: ##STR1## and their pharmaceutically acceptable salts and solvates. Pharmaceutical compositions containing compounds represented by Formula 1.0 are disclosed. Methods of treating a viral infection using compounds represented by Formula 1.0 are disclosed. Also disclosed are methods of treating hypertension using compounds of Formula 1.0 wherein R is selected from the group consisting of H, halogen and --C(O)OR.sup.6 ; and R.sup.1 is selected from the group consisting of --OR.sup.14, --O(CH.sub.2).sub.a C(H).sub.3-i Z.sub.i and --O(CH.sub.2).sub.h N(R.sup.15).sub.2.Type: GrantFiled: February 26, 1997Date of Patent: August 24, 1999Assignee: Schering CorporationInventors: Adriano Afonso, Jay Weinstein, Margaret Jevnik Gentles
-
Patent number: 5942535Abstract: The present invention relates to heterocyclic compounds of the formula ##STR1## in which R.sup.1 -R.sup.7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid group and for the prevention of allergically induced diseases.Type: GrantFiled: March 28, 1997Date of Patent: August 24, 1999Assignee: Merckle GmbHInventors: Stefan Laufer, Hans Gunther Striegel, Gerd Dannhardt
-
Patent number: 5942521Abstract: The present invention offers 7-aminoquinolinone derivatives, physiologically acceptable salts thereof, anti-allergic agents having as an active ingredient a 7-aminoquinolinone derivative or physiologically acceptable salt thereof, and 7-nitroquinolinone derivatives, wherein the 7-aminoquinolinone derivative is expressed by the following general formula (I): ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl group;R.sub.2 and R.sub.3 are mutually different groups, each of which is selected from among hydrogen atoms, acyl groups, alkyl groups or alkenyl groups; andR.sub.4 and R.sub.5 are mutually different or identical groups, each of which is selected from among hydrogen atoms, acyl groups, alkyl groups, alkenyl groups or aralkyl groups; and physiologically acceptable salts thereof.Type: GrantFiled: January 16, 1997Date of Patent: August 24, 1999Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Hidetsugu Takagaki, Masayoshi Abe, Mitsuru Sakai, Yasuo Aoki, Shigenori Nakanishi, Nobuyuki Kimura, Akihide Koda
-
Patent number: 5939452Abstract: The invention relates to novel benzopyran and other benzo-fused leukotriene B.sub.4 (LTB.sub.4) antagonists of formula I and the pharmaceutically acceptable salts thereof, to pharmaceutical compositions containing such compounds, and to a method of using such compounds as LBT.sub.4 antagonists. The compounds of the invention inhibit the action of LTB.sub.4 and are therefore useful in the treatment of LTB.sub.4 induced illnesses such as inflammatory disorders including rheumatoid arthritis, osteoarthritis, inflammatory bowel disease, psoriasis and other skin disorders such as eczema, erythema, pruitus and acne, stroke and other forms of reperfusion injury, graft rejection, autoimmune diseases, asthma and other conditions where marked neutrophil infiltration occurs.Type: GrantFiled: April 9, 1997Date of Patent: August 17, 1999Assignee: Pfizer IncInventors: Mark Anthony Dombroski, Kevin Koch, Anthony Daniel Piscopio
-
Patent number: 5935973Abstract: Compounds of formula I ##STR1## and pharmaceutically acceptable salts thereof in which A is methylene or O; B is methylene or O; g is 0,1,2,3 or 4; R.sub.1 is an optional substituent; U is an alkylene chain optionally substituted by one or more alkyl; Q represents a divalent group containing nitrogen atoms; and T represents CO.HET, have utility in the treatment of central nervous system disorders, for example depression, anxiety, psychoses (for example schizophrenia), tardive dyskinesia, Parkinson's disease, obesity, hypertension, Tourette's syndrome, sexual dysfunction, drug addiction, drug abuse, cognitive disorders, Alzheimer's disease, senile dementia, obsessive-compulsive behavior, panic attacks, social phobias, eating disorders and anorexia, cardiovascular and cerebrovascular disorders, non-insulin dependent diabetes mellitus, hyperglycaemia, constipation, arrhythmia, disorders of the neuroendocrine system, stress, prostatic hypertrophy, and spasticity.Type: GrantFiled: January 5, 1998Date of Patent: August 10, 1999Assignee: Knoll AktiengesellschaftInventors: Alan Martin Birch, David John Heal, Frank Kerrigan, Keith Frank Martin, Patricia Lesley Needham, Bruce Jeremy Sargent
-
Patent number: 5912349Abstract: The present invention is an improved process to prepare roquinimex (IV) which comprises:(1) contacting N-methyl-N-phenyl-.alpha.-carbomethoxyamide (V) with from about one to about two equivalents of base and(2) contacting the mixture of step (1) with N-methylisatoic anhydride (I).Type: GrantFiled: January 13, 1998Date of Patent: June 15, 1999Assignee: Pharmacia & Upjohn CompanyInventor: John C. Sih
-
Patent number: 5866579Abstract: This invention is directed to novel imidazole and imidazoline derivatives which are selective agonists for cloned human .alpha..sub.2 adrenergic receptors. This invention is also related to the use of these compounds for the treatment of any disease where modulation of the .alpha..sub.2 receptors may be useful. The invention further provides for a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: April 11, 1997Date of Patent: February 2, 1999Assignee: Synaptic Pharmaceutical CorporationInventors: Wai C. Wong, Yoon T. Jeon, T. G. Murali Dhar, Charles Gluchowski
-
Patent number: 5859025Abstract: Fluoroalkyl- and fluoroalkoxy-substituted heterocyclic bradykinin antagonists, process or their preparation, and their useHeterocyclic fluoroalkyl derivatives and fluoroalkoxy derivatives of the formula (I) having bradykinin-antagonistic action ##STR1## in which X.sub.1 -X.sub.3 are N or CR.sup.5, R.sup.1 and R.sup.2 are H or halogen, R.sup.3 and R.sup.4 are H, halogen, alkyl or alkenyl, R.sup.5 is H, halogen, (substituted) alkyl, O--R.sup.6, S--R.sup.6, NHR.sup.6, (substituted) aryl, (substituted)aryl-alkyl, --C(O)--OR.sup.6 or --C(O)--H, R.sup.6 and R.sup.8 H, alkyl, alkenyl or aryl-alkyl, R.sup.7 is (substituted) alkyl or (substituted) alkoxy, B is an aminocarboxylic acid, D is alkenediyl, alkanediyl or --(CH.sub.2).sub.n --Y.sub.p --(CH.sub.2).sub.m --, E is oxygen or sulfur, Y is oxygen, sulfur or NR.sup.8, n and m are a number 0-3, o is a number 1-3 and p is 0 or 1, and their physiologically tolerable salts and a process for their preparation are described.Type: GrantFiled: March 18, 1997Date of Patent: January 12, 1999Assignee: Hoechst AktiengesellschaftInventors: Adalbert Wagner, Holger Heitsch, Gerhard Nolken, Klaus Wirth, Bernward Scholkens
-
Patent number: 5834485Abstract: The subject invention pertains to quinolinesulfonamides. The subject compounds can be used to treat disease states, such as those that are associated with proteins that mediate cellular activity, for example, by inhibiting phosphodiesterase IV (PDE IV) or tumor necrosis factor (TNF). The invention also pertains to methods of treating disease states, including those states capable of being modulated by inhibition of PDE IV or TNF.Type: GrantFiled: May 20, 1997Date of Patent: November 10, 1998Assignee: Chiroscience LimitedInventors: Hazel Joan Dyke, John Gary Montana
-
Patent number: 5798451Abstract: Quinoline-3-carboxamides I ##STR1## where R.sup.1 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, and the organic radicals may be substituted or unsubstituted;R.sup.2 is hydrogen, hydroxyl, alkoxy, alkenyloxy, dialkylamino, alkyl, alkenyl, alkynyl, cycloalkyl, and the organic radicals may be substituted or unsubstituted;orR.sup.1, R.sup.2 together denote an alkylene chain of 4 to 7 members and which may be interrupted by oxygen, sulfur or N-methyl;R.sup.3 -R.sup.6 are hydrogen, alkyl, alkoxy, haloalkyl, haloalkoxy, alkylthio, haloalkylthio, halogen, cyano or nitro;X is oxygen or sulfur;with the proviso that R.sup.2 is not hydrogen, C.sub.1 -C.sub.3 -alkyl, n-butyl, 3-methylbutyl, cyclohexyl, hexyl, heptyl, octyl, 2-chlorobenzyl, 3-(dimethylamino)propyl, 3-(diethylamino)propyl, 2-morpholinoethyl or 2-(3,4-dimethoxyphenyl)ethyl when R.sup.1 and R.sup.3 to R.sup.6 are hydrogen and X is oxygen, and that R.sup.2 is not benzyl when R.sup.1 is methyl, R.sup.3 to R.sup.6 are hydrogen and X is oxygen, and that R.Type: GrantFiled: February 3, 1997Date of Patent: August 25, 1998Assignee: BASF AktiengesellschaftInventors: Wolfgang von Deyn, Hans Theobald, Christoph Nuebling, Uwe Kardorff, Helmut Walter, Karl-Otto Westphalen, Thomas Kappe, Matthias Gerber
-
Patent number: 5795889Abstract: This invention relates to bis mono- and/or bicyclic aryl and/or heteroaryl compounds exhibiting protein tyrosine kinase inhibition activity. More specifically, it relates to the method of inhibiting abnormal cell proliferation in a patient suffering from a disorder characterized by such proliferation comprising the administration thereto of an EGF and/or PDGF receptor inhibiting effective amount of said bis mono- and/or bicyclic aryl and/or heteroaryl compound and to the preparation of said compounds and their use in pharmaceutical compositions used in this method.Type: GrantFiled: February 9, 1995Date of Patent: August 18, 1998Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: Alfred P. Spada, Michael R. Myers, Martin P. Maguire, Paul E. Persons
-
Patent number: 5776949Abstract: A compound of formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3, which are identical or different, represent hydrogen, halogen, alkyl, nitro, cyano, aminosulfonyl, imidazolyl, or pyrrolyl, or alternatively, when two of them are situated on adjacent carbons, may form with the carbon atoms to which they are attached a benzene ring on C.sub.3 -C.sub.7 cyloalkylR.sub.4 represents hydroxyl, alkoxy, phenoxy, or amino,their isomers as well as their addition salts with a pharmaceutically-acceptable base, and medicinal products containing the same which are useful as inhibitors of the the pathological phenomena linked to hyperactivation of the neurotransmission pathways by the excitatory amino acids.Type: GrantFiled: July 10, 1997Date of Patent: July 7, 1998Assignee: Adir et CompagnieInventors: Alex Cordi, Patrice Desos, Jean Lepagnol, Philippe Morain, Pierre Lestage
-
Patent number: 5760197Abstract: Hydroxyquinolone monoazo dyestuffs of the formula I ##STR1## in which D is an organic radical such as one of the disclosed aromatic radicals, and R is substituted or unsubstituted alkyl, benzyl, phenyl, phenoxy, or alkoxy (most preferably C.sub.1 -C.sub.6 -alkyl) are especially well suited to dyeing and printing of hydrophobic materials and other dyeing or printing applications. The dyestuffs are prepared by diazotizing an amine (D--NH.sub.2) and coupling the diazotization product to a hydroxyquinolone compound.Type: GrantFiled: July 3, 1996Date of Patent: June 2, 1998Assignee: Dystar Japan Ltd.Inventor: Ulrich Buhler
-
Patent number: 5756517Abstract: The present invention relates to the use of bisquinolines of the general formula ##STR1## in which the substituents mentioned have the meanings given in the description.The invention furthermore relates to new bisquinolines of the general formula (I), to a process for the preparation of the known and the new bisquinolines, to the use of the new bisquinolines as medicaments, to their use for the preparation of medicaments, and to medicaments comprising them.Type: GrantFiled: October 25, 1996Date of Patent: May 26, 1998Assignee: Bayer AktiengesellschaftInventors: Rudolf Schohe-Loop, Peter-Rudolf Seidel, William Bullock, Achim Feurer, Georg Terstappen, Joachim Schuhmacher, Franz-Josef van der Staay, Bernard Schmidt, Richard J. Fanelli, Jane C. Chisholm, Richard T. McCarthy
-
Patent number: 5728715Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.Type: GrantFiled: October 30, 1996Date of Patent: March 17, 1998Assignee: Rohm and Haas CompanyInventors: Enrique Luis Michelotti, Anne Ritchie Egan, Ronald Ross, Jr., Willie Joe Wilson
-
Patent number: 5698581Abstract: The invention relates to heteroaroylguanidines of the formula I ##STR1## in which the substituents HA and R(1) to R(5) have the meanings given in the specification. These compounds exhibit very good antiarrhythmic properties and are outstandingly suitable for use as antiarrhythmic pharmaceuticals possessing a cardioprotective component for the prophylaxis and treatment of infarction and for the treatment of angina pectoris, in connection with which they also inhibit or strongly reduce, in a preventative manner, the pathophysiological processes associated with the genesis of ischemically induced damage, in particular associated with the elicitation of ischemically induced cardiac arrhythmias.Type: GrantFiled: April 7, 1995Date of Patent: December 16, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
-
Patent number: 5698550Abstract: Compounds of the formula ##STR1## wherein R is an optionally substituted heteroaryl group such as 2-chromanyl, 2-pyridyl or 5-fluoro-2-benzothiazoyl;X is O, S or (CH.sub.2).sub.m ;R.sup.1 is phenyl or pyridyl, optionally substituted by one or more (C.sub.1 -C.sub.3)alkyl, (C.sub.1 -C.sub.3)alkoxy, carboxy or ?(C.sub.1 -C.sub.3)alkoxy!carbonyl groups;n is 0, 1 or 2;m is 1 or 2;Y and Y.sup.1 are taken together and are oxygen, or Y and Y.sup.1 are taken separately, Y is hydrogen and Y.sup.1 is hydroxy or an in vivo hydrolyzable acyloxy group;Z is CH.sub.2, NR.sup.2, O or S; andR.sup.2 is hydrogen or (C.sub.1 -C.sub.3)alkyl;are useful in the treatment of asthma, arthritis and related diseases mediated by leukotrienes.Type: GrantFiled: June 14, 1993Date of Patent: December 16, 1997Assignee: Pfizer Inc.Inventors: James F. Eggler, Anthony Marfat, Lawrence S. Melvin, Jr.
-
Patent number: 5696241Abstract: Novel sulfonated quinolone compounds used in the preparation of fiber reactive dyes having the formula: ##STR1## being N-alkyl substituted-4-hydroxy-6-sulfo-2-quinolone. The alkyl group bonded to the nitrogen in the quinolone has from 1 to 4 carbon atoms which may be further substituted by an hydroxy, amino, or sulfo group. The compounds of the invention may be prepared by the sulfonation of an N-alkyl substituted-4-hydroxy-2-quinolones, ##STR2## followed by selective desulfonation to yield the compounds of interest. New monoazo fiber reactive dyes having the formulas: ##STR3## and their metal complexes, may be prepared from these sulfonated compounds by the diazotization of an amine component, selected from an unsubstituted, or a substituted benzene or naphthalene compound, containing a fiber reactive group, and coupling the diazo component to the compounds of the invention.Type: GrantFiled: January 15, 1997Date of Patent: December 9, 1997Assignee: Dystar, L.P.Inventors: Philomen Z. deCroos, Ronald P. Pedemonte, Thomas S. Phillips
-
Patent number: 5693815Abstract: 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: GrantFiled: July 14, 1995Date of Patent: December 2, 1997Assignee: Schering CorporationInventors: Frank Bennett, Viyyoor M. Girijavallabhan, Naginbhai M. Patel
-
Patent number: 5691322Abstract: Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have a quinoline or a pyridine anchor attached by means of a linker to a binding domain sidechain, which compounds inhibit the enzyme 3-hydroxy-3-methyl-glutaryl-coenzyme A reductase.Type: GrantFiled: October 31, 1995Date of Patent: November 25, 1997Assignee: E.R. Squibb & Sons, Inc.Inventor: Jeffrey Adam Robl
-
Patent number: 5684046Abstract: Described herein are Benzopyran and other benzo-fused leukotriene B.sub.4 antagonists have the formula ##STR1## wherein R.sup.1 is a phenyl or substituted phenyl group, and A, n, R.sup.2 and R.sup.3 are as defined herein.Type: GrantFiled: May 3, 1996Date of Patent: November 4, 1997Assignee: Pfizer IncInventor: Kevin Koch
-
Patent number: 5663449Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: September 2, 1997Assignee: Hoechst Marion Roussel, Inc.Inventor: Joseph T. Strupczewski
-
Patent number: 5663375Abstract: Pharmaceutical compounds of the formula ##STR1## in which n is 0, 1 or 2 and R.sup.1 is attached at any of the positions 7, 8, 9 or 10, and each R.sup.1 is halo, carboxy, trifluoromethyl, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, hydroxy-C.sub.1-4 alkyl, hydroxy-C.sub.1-4 alkoxy, nitrogen-containing heterocyclyl, nitro, trifluoromethoxy, --COOR.sup.5 where R.sup.5 is an ester group, --COR.sup.6, --CONR.sup.6 R.sup.7 or --NR.sup.6 R.sup.7 where R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl;R.sup.2 is phenyl, naphthyl or heteroaryl selected from thienyl, pyridyl, benzothienyl, quinolinyl, benzofuranyl or benzimidazolyl, said phenyl, naphthyl and heteroaryl groups being optionally substituted, or R.sup.2 is furanyl optionally substituted with C.sub.1-4 alkyl;R.sup.3 is nitrile, carboxy, --COOR.sup.8 where R.sup.8 is an ester group, or --CONR.sup.9 R.sup.10 where R.sup.9 and R.sup.10 are each hydrogen or C.sub.1-4 alkyl; andR.sup.4 is --NR.sup.11 R.sup.12, --NR.sup.11 COR.sup.Type: GrantFiled: August 22, 1994Date of Patent: September 2, 1997Assignees: Eli Lilly and Company, Lilly Industries LimitedInventors: Michael Brunavs, Colin Peter Dell, Peter Thaddeus Gallagher, William Martin Owton, Colin William Smith
-
Patent number: 5658911Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: September 20, 1994Date of Patent: August 19, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley
-
Patent number: 5654319Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: August 5, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
-
Patent number: 5652368Abstract: Disclosed herein are substituted or unsubstituted 1,2,3,4-tetrahydroquinoline-2,3,4-trione-3 or 4-oximes or pharmaceutically acceptable salts thereof that have high binding to the glycine receptor and are usefully administered to animals for the treatment or prevention of the adverse consequences of the hyperactivity of the excitatory amino acids, or neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, for the treatment of anxiety, chronic pain, convulsions, and neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome; and for the inducement of anesthesia.Type: GrantFiled: September 29, 1995Date of Patent: July 29, 1997Assignees: The Regents of the University of California, State of Oregon, acting by and through the Oregon State Board of Higer Education, acting for and on behalf of the Oregon Health Sciences University, University of OregonInventors: Sui Xiong Cai, John F. W. Keana, Eckard Weber
-
Patent number: 5652250Abstract: The present invention relates to new compounds of formula ##STR1## wherein A is a bicyclic ring chosen from naphthalene, tetrahydronaphthalene, quinoline, isoquinoline and indole.B is a R.sup.2 substituted benzene ring or an unsubstituted pyridine or thiophene ring;R is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy or a group NR.sup.3 R.sup.4 wherein each of R.sup.3 and R.sup.4 is independently hydrogen or C.sub.1 -C.sub.6 alkyl;R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkanoyl;R.sup.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, nitro, cyano, carboxy, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyloxy or a group NR.sup.3 R.sup.4 wherein R.sup.3 and R.sup.4 are as defined above;n is zero or an integer of 1 to 2;x is zero or an integer of 1 to 5;and the pharmaceutically acceptable salts thereof.The compounds of the invention are useful as tyrosine kinase inhibitors.Type: GrantFiled: November 21, 1995Date of Patent: July 29, 1997Assignee: Pharmacia S.p.A.Inventors: Franco Buzzetti, Angelo Crugnola, Antonio Longo, Maria Gabriella Brasca, Dario Ballinari
-
Patent number: 5646098Abstract: The invention relates to novel compositions comprising ene and free radical adducts of unsaturated and saturated hydrocarbons, and acyclic and cyclic vicinal polycarbonyl compounds such as diethyl ketomalonate and indantrione. The adducts are reacted with nucleophiles such as amines, electrophiles such as anhydrides and esters, and metal ions. Post-products are obtained via reaction of said products with capping reagents such as boric acid. Compositions containing said adducts, products and post-products include oleaginous substances such as fuels and lube oils.Type: GrantFiled: May 13, 1994Date of Patent: July 8, 1997Assignee: Exxon Chemical Patents IncInventor: Stanley J. Brois
-
Patent number: 5646161Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: July 8, 1997Assignee: Hoechst-Marion-Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
-
Patent number: 5639764Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: June 17, 1997Assignee: Hoechst-Marion-Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
-
Patent number: 5639886Abstract: The present invention relates to a one-pot process for the preparation of 7-heterocyclyl-substituted 3-quinolonecarboxylic acid derivatives. They possess a strong anti-microbial effect. They include active compounds such as, for example, ofloxacin, ciprofloxacin or enrofloxacin.Type: GrantFiled: December 2, 1994Date of Patent: June 17, 1997Assignee: Bayer AktiengesellschaftInventors: Rudolf Zerbes, Paul Naab, Gerhard Franckowiak, Herbert Diehl
-
Patent number: 5637710Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: December 22, 1995Date of Patent: June 10, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
-
Patent number: 5633379Abstract: 3-Heteroaliphatyl- and 3-hetero(aryl)aliphatyl-2(1H)quinolone derivatives of formula I ##STR1## wherein the radicals R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently of the others hydrogen, an aliphatic hydrocarbon radical, free or etherified hydroxy, mercapto or etherified and/or oxidised mercapto, unsubstituted or aliphaticaliy substituted amino, nitro, free or esterified or amidated carboxy, cyano, free or amidated sulfamoyl, halogen or trifluoromethyl, X is oxy or optionally oxidised thio, A is a divalent aliphatic radical and R.sub.Type: GrantFiled: June 1, 1995Date of Patent: May 27, 1997Assignee: Ciba-Geigy CorporationInventor: Hans Allgeier
-
Patent number: 5633265Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: May 27, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
-
Patent number: 5629326Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: May 13, 1997Assignee: Hoechst-Marion-Roussel, Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler
-
Patent number: 5627281Abstract: 6,7-propylene-, butylene-, or pentylene-bridged imidazopyridin-4-amines and their intermediate compounds are described. Also disclosed are pharmaceutical compositions containing such compounds and methods of inducing interferon (.alpha.) biosynthesis and treating vital infections involving the use of such compounds.Type: GrantFiled: July 3, 1996Date of Patent: May 6, 1997Assignee: Minnesota Mining and Manufacturing CompanyInventors: Nick Nikolaides, John F. Gerster
-
Patent number: 5624927Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: April 29, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
-
Patent number: 5622965Abstract: 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 substituted or unsubstituted 4-hydroxy-3-nitro-1,2-dihydroquinolin-2-one or pharmaceutically acceptable salts thereof which have high binding to the glycine receptor.Type: GrantFiled: August 2, 1993Date of Patent: April 22, 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, Eugene Oregon, The Regents of the University of CaliforniaInventors: Sui X. Cai, Eckard Weber, John F. W. Keana
-
Patent number: 5620988Abstract: Substituted tetrahydropyridines and hydroxypiperidines and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as central nervous system agents and are particularly useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.Type: GrantFiled: June 6, 1995Date of Patent: April 15, 1997Assignee: Warner-Lambert CompanyInventors: Shelly Glase, Juan C. Jaen, Sarah J. Smith, Lawrence D. Wise
-
Patent number: 5614543Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: March 25, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau, Edward J. Glamkowski, Yulin Chiang, Grover C. Helsley
-
Patent number: 5612343Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: March 18, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Edward J. Glamkowski, Yulin Chiang
-
Patent number: 5612342Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: June 6, 1995Date of Patent: March 18, 1997Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Joseph T. Strupczewski, Kenneth J. Bordeau
-
Patent number: 5607624Abstract: A process for the preparation of compounds of formula I ##STR1## wherein the general symbols are as defined in claim 1, which comprises reacting a compound of formula III ##STR2## wherein the general symbols are as defined in claim 1, with a compound of formula IV[H].sub.n --R.sub.1 (IV).Type: GrantFiled: September 12, 1994Date of Patent: March 4, 1997Assignee: Ciba-Geigy CorporationInventors: Peter Nesvadba, Samuel Evans, Ralf Schmitt