Additional Hetero Ring Containing Patents (Class 546/187)
-
Patent number: 5994356Abstract: The present invention relates to carboxylic acid derivatives of the general formula ##STR1## in which R.sub.a to R.sub.c, A, B, D, E and X.sub.1 to X.sub.3 are as defined in claim 1, their tautomers, their stereoisomers including their mixtures, and their salts, in particular their physiologically tolerated salts with inorganic or organic acids or bases, which have useful pharmacological properties, preferably aggregation-inhibiting inhibiting actions, medicaments containing these compounds, their use and processes for their preparation.Type: GrantFiled: April 3, 1997Date of Patent: November 30, 1999Assignee: Karl ThomaeInventors: Helmut Pieper, Gunter Linz, Volkhard Austel, Frank Himmelsbach, Brian Guth, Johannes Weisenberger
-
Patent number: 5990130Abstract: Compounds of formula I ##STR1## wherein G, J, L, M, m and D have any of the meanings given in the specification, their N-oxides, and their pharmaceutically acceptable salts are nonpeptide antagonists of neurokinin A and useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: June 29, 1998Date of Patent: November 23, 1999Assignee: Zeneca LimitedInventor: Scott Carson Miller
-
Patent number: 5990132Abstract: Compounds of Formula (I) have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful in the treatment of diseases of man where subnormal levels of this neurochemical are found, such as in Alzheimer's disease, and other conditions involving learning and cognition.Type: GrantFiled: June 17, 1996Date of Patent: November 23, 1999Assignee: The DuPont Merck Pharmaceutical CompanyInventors: Christopher Allan Teleha, Wendell Wilkie Wilkerson, Richard Alan Earl
-
Patent number: 5986101Abstract: A description is given of compounds obtainable by reacting compounds of the general formula ##STR1## where A is O or N--R.sup.2 andB is a direct bond or O--CH.sub.2 --CH.sub.2, the carbon of the ethylene group being attached to the nitrogen of the piperidine ring, and R.sup.1 is H, C.sub.1 -C.sub.20 alkyl, C.sub.2 -C.sub.20 alkenyl, C.sub.2 -C.sub.20 alkynyl, C.sub.6 -C.sub.20 aryl, C.sub.7 -C.sub.20 aralkyl, O--C.sub.1 -C.sub.20 alkyl, O--C.sub.5 -C.sub.8 cycloalkyl, CO--C.sub.1 -C.sub.20 alkyl, CO--C.sub.6 -C.sub.20 aryl, CO--C.sub.7 -C.sub.20 aralkyl, O--CO--C.sub.1 -C.sub.20 alkyl or C.sub.1 -C.sub.6 alkyl-Z--C.sub.1 -C.sub.6 alkyl, where Z is O, S or C.dbd.O, andR.sup.2 is C.sub.1 -C.sub.12 alkyl or ##STR2## and Y is O or N--R.sup.4, or Y--R.sup.3, following removal of the hydrogen in position 4 of the piperidine ring, is the divatent radical ##STR3## [.fwdarw.spiro compound], and R.sup.3 is C.sub.1 -C.sub.20 alkyl, CO--C.sub.1 -C.sub.20 alkyl, CO--C.sub.6 -C.sub.20 aryl or CO--C.sub.7 -C.sub.Type: GrantFiled: October 9, 1997Date of Patent: November 16, 1999Assignee: Ciba Specialty Chemicals CorporationInventor: Alfred Steinmann
-
Patent number: 5977139Abstract: The present invention relates to novel carboxy substituted cyclic carboxamide derivatives of formula (1), ##STR1## and stereoisomers and pharmaceutically acceptable salts thereof and their use as tachykinin receptor antagonists. Such antagonists are useful in the treatment of tachykinin-mediated diseases and conditions disclosed herein including: asthma, coughs and bronchitis.Type: GrantFiled: November 17, 1997Date of Patent: November 2, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: Timothy P. Burkholder, George D. Maynard, Elizabeth M. Kudlacz
-
Patent number: 5977138Abstract: 1,4 Di-substituted piperidine muscarinic antagonists of formula I ##STR1## or an isomer, pharmaceutically acceptable salt, ester or solvate thereof, whereinX is a bond, --O--, --S--, --SO--, --SO.sub.2 --, --CO--, --C(OR.sup.7).sub.2 --, --CH.sub.2 --O--, --O-- CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 --, --CH(C.sub.1 -C.sub.6 alkyl)-, --C(C.sub.1 -C.sub.6 alkyl).sub.2 --, --CONR.sup.17 --, --NR.sup.17 CO--, --O--C(O)NR.sup.17 --, --NR.sup.17 C(O)--O--, --SO.sub.2 NR.sup.17 -- or --NR.sup.17 SO.sub.2 --;R is cycloalkyl, optionally substituted phenyl or optionally substituted pyridyl;R.sup.2 is H, alkyl, optionally substituted cycloalkyl, cycloalkenyl, t-butoxycarbonyl or optionally substituted piperidinyl; and the remaining variables are as defined in the specification, are disclosed. Compounds of formula I are useful for treating cognitive disorders such as Alzheimer's disease.Type: GrantFiled: August 13, 1997Date of Patent: November 2, 1999Assignee: Schering CorporationInventors: Yuguang Wang, Wei K. Chang, Sundeep Dugar, Samuel Chackalamannil
-
Patent number: 5972947Abstract: The present invention concerns new oxazolidinone derivatives, processes for their production as well as pharmaceutical agents containing these substances. The present invention concerns compounds of the general formula I ##STR1## in which the symbols have the meanings as listed in the claims.Type: GrantFiled: December 31, 1998Date of Patent: October 26, 1999Assignee: Roche Diagnostics GmbHInventors: Christos Tsaklakidis, Wolfgang Schafer, Liesel Dorge, Walter-Gunar Friebe, Angelika Esswein
-
Patent number: 5973146Abstract: A process for the preparation of compounds of formula I ##STR1## by reacting a pyrrolopyrrole of formula ##STR2## wherein X.sub.1 is a group selected from ##STR3## X.sub.2 is a group selected from ##STR4## or has the same meaning as X.sub.1, with a secondary amine of formula ##STR5## in the molar ratio 1:2, in the presence of an anhydrous dipolar aprotic solvent and of an amount 0.1 to 15 times in excess of stoichiometric proportion, based on the amine of formula III, of an anhydrous organic base, in the temperature range from 50.degree. to 230.degree. C. and under a pressure from 0 to 10 bar.The substituents R.sub.1 to R.sub.8, Y and Hal are as defined in claim 1.The compounds of formula I are especially suitable for use as photoconductive substances.Type: GrantFiled: September 29, 1993Date of Patent: October 26, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Alain Claude Rochat, Olof Wallquist, Abul Iqbal, Jin Mizuguchi
-
Patent number: 5968923Abstract: The present invention provides compounds of formula (I) and the pharmaceutically acceptable salts thereof, wherein R is C.sub.3 -C.sub.7 cycloalkyl, aryl or C.sub.1 -C.sub.6 alkyl, said C.sub.1 -C.sub.6 alkyl, said C.sub.1 -C.sub.6 alkyl being optionally substituted by fluoro, COOH, --COO(C.sub.1 -C.sub.4 alkyl), C.sub.3 -C.sub.7 cycloalkyl, adamantyl, aryl or het.sup.1, and said C.sub.3 -C.sub.7 cycloalkyl being optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.4 alkoxy, hydroxy, fluoro, fluoro (C.sub.1 -C.sub.4) alkyl and fluoro (C.sub.1 -C.sub.4) Alkoxy; R.sub.1 is phenyl, naphthyl, thienyl, benzothienyl or indolyl, each optionally substituted by 1 or 2 substituents each independently selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, halo and trifluormethyl; R.sup.2 is --CO.sub.2 H, --CONR.sup.3 R.sup.4, --CONR.sup.5 (C.sub.3 -C.sub.7 cycloalkyl), --NR.sup.5 (C.sub.2 -C.sub.5 alkanoyl), --NR.sup.Type: GrantFiled: February 10, 1997Date of Patent: October 19, 1999Assignee: Pfizer Inc.Inventors: Alexander Roderick MacKenzie, Allan Patrick Marchington, Sandra Dora Meadows, Donald Stuart Middleton
-
Patent number: 5965565Abstract: The present invention is directed to certain piperidines, pyrrolidines, and hexahydro-1H-azepines of the general structural formula: ##STR1## wherein B is selected from: ##STR2## and R.sup.1, R.sup.1a, R.sup.2a, R.sup.3a, R.sup.3b, R.sup.4, R.sup.4a, R.sup.4b, R.sup.4c, R.sup.5, D, X, Y, n, x and y are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.Type: GrantFiled: December 11, 1997Date of Patent: October 12, 1999Assignee: Merck & Co., Inc.Inventors: Meng H. Chen, Zhijian Lu, Ravi Nargund, Arthur A. Patchett, James R. Tata, Lihu Yang, Mu Tsu Wu
-
Patent number: 5962683Abstract: A description is given of compounds of the formula I ##STR1## where r is 0 or 1 and y is a number from the range 1-3; X is a direct bond or --NR.sub.8 --, --CO--, --CONH-- or --COO-- or a divalent aliphatic or mixed aromatic-aliphatic C.sub.1 -C.sub.18 hydrocarbon radical;Z is an aromatic, aliphatic or mixed aromatic-aliphatic C.sub.3 -C.sub.18 hydrocarbon radical which is interrupted in the aliphatic moiety by one or more divalent functional groups, in each case in a carbon-carbon single bond, and/or in the aromatic or aliphatic moiety by one or more divalent functional groups, in each case in a carbon-hydrogen bond, possible functional groups being --O--, --NR.sub.8 --, --S--, --SO--, --SO.sub.Type: GrantFiled: June 17, 1997Date of Patent: October 5, 1999Assignee: Ciba Specialty Chemicals Corp.Inventors: Alfred Steinmann, Rolf Mulhaupt
-
Patent number: 5962474Abstract: This invention provides novel 5-HT.sub.1F agonists of Formula I ##STR1## where A--B, R,R.sup.1 and X are as defined in the specification, which are useful for the treatment of migraine and associated disorders.Type: GrantFiled: November 24, 1997Date of Patent: October 5, 1999Assignee: Eli Lilly and CompanyInventors: James Edmund Audia, Bruce Anthony Dressman, James Joseph Droste, James Erwin Fritz, Stephen Warren Kaldor, Daniel James Koch, Joseph Herman Krushinski, Jr., Jeffrey Scott Nissen, Vincent Patrick Rocco, John Mehnert Schaus, Dennis Charles Thompson
-
Patent number: 5962473Abstract: This invention provides methods for the treatment or amelioration of the symptoms of the common cold or allergic rhinitis which comprises administering to a mammal in need thereof a serotonin 5-HT.sub.1F agonist.Type: GrantFiled: August 5, 1997Date of Patent: October 5, 1999Assignee: Eli Lilly and CompanyInventors: Kirk Willis Johnson, Lee Alan Phebus
-
Patent number: 5952354Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in the inhibition of the esterification of cholesterol and are therefore implicated in the inhibition of absorption of cholesterol and thus can lower serum cholesterol levels. Compounds of the formula: ##STR1## where Z is ##STR2## or --Ar.sup.1 --(CR.dbd.CR).sub.1-3 --Ar.sup.2, --AR.sup.1 --NR.sup.7 --AR.sup.2 and A is a linking group inhibit the enzymes CEH and/or ACAT (in vitro) and inhibit absorption of cholesterol.Type: GrantFiled: July 21, 1993Date of Patent: September 14, 1999Assignee: American Home Products CorporationInventors: Thomas Joseph Commons, Donald Peter Strike, Christa Marie LaClair
-
Patent number: 5948781Abstract: This invention relates to a method of treating cancer by administering a compound of the formula wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, E.sup.1, E.sup.2, p, Het' and Het" are defined as indicated in the specification.Type: GrantFiled: May 27, 1997Date of Patent: September 7, 1999Assignee: Pfizer IncInventors: Joseph P. Lyssikatos, Robert A. Volkmann
-
Patent number: 5945429Abstract: Novel compounds of the formula: ##STR1## are disclosed. Compounds of Formula 1.0 are represented by the compounds of formulas: ##STR2## wherein R.sup.1, R.sup.3 and R.sup.4 are each independently selected from halo.Also disclosed are methods of inhibiting farnesyl protein transferase and the growth of abnormal cells, such as tumor cells.Type: GrantFiled: September 11, 1997Date of Patent: August 31, 1999Assignee: Schering CorporationInventors: Arthur G. Taveras, Alan K. Mallams, Adriano Afonso, Ronald J. Doll
-
Patent number: 5942523Abstract: A compound of formula: in which:Ar represents a pyrid-2-yl or a phenyl which is unsubstituted or substituted by a halogen, a methyl or a (C.sub.1 -C.sub.4)alkoxy;R.sub.1 represents a methyl group;R.sub.11 represents hydrogen;or R.sub.1 and R.sub.11 together represent a --(CH.sub.2).sub.3 -- group;R.sub.2 represents a hydroxyl; a (C.sub.1 -C.sub.7)alkoxy; a (C.sub.1 -C.sub.7)acyloxy; a cyano; an --NR.sub.6 R.sub.7 group; an --NR.sub.3 COR.sub.4 group; an --NR.sub.3 COOR.sub.8 group; an --NR.sub.3 SO.sub.2 R.sub.9 group; an --NR.sub.3 CONR.sub.10 R.sub.12 group; a (C.sub.1 -C.sub.7)acyl group; a (C.sub.1 -C.sub.7)alkoxycarbonyl; a --CONR.sub.10 R.sub.12 group; a --CH.sub.2 OH group; a (C.sub.1 -C.sub.7)alkoxymethyl; a (C.sub.1 -C.sub.7)acyloxymethyl; a (C.sub.1 -C.sub.7)alkylaminocarbonyloxymethyl; a --CH.sub.2 NR.sub.13 R.sub.14 group; a --CH.sub.2 NR.sub.3 COR.sub.4 group; a --CH.sub.2 NR.sub.3 COOR.sub.8 group; a --CH.sub.2 NR.sub.3 SO.sub.2 R.sub.9 group; a --CH.sub.2 NR.sub.3 CONR.sub.10 R.sub.Type: GrantFiled: February 29, 1996Date of Patent: August 24, 1999Assignee: SanofiInventors: Daniel Bichon, Patrick Gueule, Didier Van Broeck, Xavier Emonds-Alt, Vincenzo Proietto
-
Patent number: 5939411Abstract: Piperidine derivatives, process for obtaining them and pharmaceutical compositions containing them, of formula ##STR1## used as neurokinin receptor antagonists, which are, in particular, useful for the treatment of all substance P- and neurokinin-dependent pathologies.Type: GrantFiled: August 25, 1997Date of Patent: August 17, 1999Assignee: SanofiInventors: Nathalie Chabert, Jean-Philippe Ducoux, Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
-
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: 5935974Abstract: The invention relates to a diphenylmethylene piperidine derivative of the formula ##STR1## wherein n is 1 or 2; or a pharmaceutically acceptable salt thereof, for use in therapy, in particular for use as a dopamine antagonist for the treatment or prophylaxis of psychotic disorders.Type: GrantFiled: January 7, 1998Date of Patent: August 10, 1999Assignee: Akzo Nobel, N.V.Inventors: Duncan Robertson Rae, David Robert Jaap
-
Patent number: 5932735Abstract: Selected derivatives of 1-oxyl-2,2,6,6-tetramethyl-4-hydroxypiperidine are surprisingly effective as inhibitors to prevent the premature polymerization of acrylic and methacrylic acids, their esters, their amides, vinyl acetate and acrylonitrile in the presence of water. Some of these derivatives are new compounds.Type: GrantFiled: June 10, 1998Date of Patent: August 3, 1999Assignee: Ciba Specialty Chemicals CorporationInventors: Glen T. Cunkle, Matthew E. Gande, Raymond Seltzer, Thomas F. Thompson
-
Patent number: 5929089Abstract: Compounds corresponding to the general formula (I) ##STR1## in which R.sub.1 represents a (C.sub.1 -C.sub.4)alkyl or (C.sub.3 -C.sub.7)cycloalkylmethyl group, X.sub.1 represents a hydrogen or halogen atom or a (C.sub.1 -C.sub.4)alkoxy group or else OR.sub.1 and X.sub.1 together represent a group of formula -OCH.sub.2 O-, -O(CH.sub.2).sub.2 -, -O(CH.sub.2).sub.3 -, -O(CH.sub.2).sub.2 O- or -O(CH.sub.2).sub.3 O-, X.sub.2 represents a hydrogen atom or an amino group, X.sub.3 represents a hydrogen or halogen atom, and R.sub.2 represents either a hydrogen atom or an optionally substituted (C.sub.1 -C.sub.6) alkyl group or a phenyl (C.sub.1 -C.sub.4) alkyl group which is optionally substituted on the phenyl ring or a phenyl (C.sub.2 -C.sub.3) alkenyl group or a phenoxy (C.sub.2 -C.sub.4) alkyl group or a cyclo (C.sub.3 -C.sub.7) alkylmethyl group or a 2,3-dihydro-1H-inden-1-yl or 2,3-dihydro-1H-inden-2-yl group or a group of general formula -(CH.sub.2).sub.Type: GrantFiled: May 8, 1998Date of Patent: July 27, 1999Assignee: SynthelaboInventors: Samir Jegham, Alistair Lochead, Frederic Galli, Alain Nedelec, Axelle Solignac, Laurence De Cruz
-
Patent number: 5925758Abstract: The invention relates to novel compounds of the formula I in which the general symbols are as defined in claim 1, as stabilizers for organic materials against oxidative, thermal or light-induced degradation.Type: GrantFiled: April 5, 1995Date of Patent: July 20, 1999Assignee: Ciba Specialty Chemicals CorporationInventor: Rita Pitteloud
-
Patent number: 5919784Abstract: A compound of general formula (I): ##STR1## where A, X, R.sub.1, Y, n and Ar are defined in the description. Medicinal products containing the same are useful as D.sub.4 receptor Ligands.Type: GrantFiled: November 7, 1997Date of Patent: July 6, 1999Assignee: Adir Et CompagnieInventors: Daniel Lesieur, Pascal Carato, Jean-Paul Bonte, Patrick Depreux, Daniel-Henri Caignard, Mark Millan, Adrian Newman-Tancredi, Pierre Renard, Marie-Claire Rettori
-
Patent number: 5919798Abstract: 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 6, 1999Assignee: 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: 5919914Abstract: Clathrates of bis?6-hydroxy-4-methyl-5-(3-methyl-imidazolium-1-yl)-3-(phen-4-ylazo)pyrid in-2-one!ethylene with aromatics of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -hydroxyalkyl, C.sub.1 -C.sub.5 -alkoxy, C.sub.1 -C.sub.5 -hydroxyalkoxy, C.sub.1 -C.sub.10 -alkyl which is interrupted by 1, 2 or 3 non-neighboring oxygen atoms and is unsubstituted or substituted by hydroxyl, C.sub.1 -C.sub.10 -alkoxy which is interrupted by 1, 2 or 3 non-neighboring oxygen atoms and is unsubstituted or substituted by hydroxyl, or is C.sub.1 -C.sub.6 -alkanoyl, hydroxy, carboxyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, phenylcarbonyl or C.sub.1 -C.sub.6 -alkenyl andR.sup.2 is R.sup.1, hydrogen or phenoxy,a process for their preparation and their use for the preparation of formulations of the dye.Type: GrantFiled: March 17, 1998Date of Patent: July 6, 1999Assignee: BASF AktiengesellschaftInventors: Manfred Ruske, Peter Erk, Heidi Hengelsberg
-
Patent number: 5919768Abstract: The present invention provides compounds having structure (II), and the pharmaceutically acceptable salts, esters, amides and prodrugs thereof.Type: GrantFiled: February 11, 1998Date of Patent: July 6, 1999Assignee: Texas Biotechnology CorporationInventors: Timothy P. Kogan, Brian Dupre, Ian L. Scott, Huong Bui, Kathy L. Wheeler, Karin M. Keller, Jamal M. Kassir
-
Patent number: 5917034Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and pharmaceutically acceptable solvates of either entity, wherein A is optionally monosaturated C.sub.1 -C.sub.4 alkylene optionaly monounsaturatred with C.sub.1 -C.sub.4 alkyl; B is C.sub.1 -C.sub.3 alkylene optionally substituted with C.sub.1 -C.sub.4 alkyl; R.sup.1 is N-amidino-4-piperidyl or 4-amidinophenyl; R.sup.2 is C.sub.4 -C.sub.12 alkyl; (C.sub.3 -C.sub.8 cycalkyl)C.sub.1 -C.sub.4 alkylene; optionally methylene-bridged C.sub.5 -C.sub.8 cycloalkyl optionally substituted with one to three C.sub.1 -C.sub.4 alkyl groups or with hydroxy; C.sub.5 -C.sub.8 alkenyl; C.sub.5 -C.sub.8 cycloalkenyl optionally subsituted with C.sub.1 -C.sub.4 alkyl; piperidyl N-substituted with C.sub.1 -C.sub.4 alkyl; tetrahydrothiopyranyl or tetrahydropyranyl; and R.sup.3 is H or C.sub.1 -C.sub.4 alkyl optionally substituted with C.sub.1 -C.sub.4 alkoxy or with hydroxy; or R.sup.2 and R.sup.Type: GrantFiled: March 9, 1998Date of Patent: June 29, 1999Assignee: Pfizer Inc.Inventors: Alan Daniel Brown, John Christopher Danilewicz, Paul Vincent Fish
-
Patent number: 5912256Abstract: A series of 1-(4-indolyloxy)-3-(4-hydroxy-4-naphthylpiperidin-1-yl)propanes are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor, yet lack mutagenic potential as measured by assays of chromosomal aberration. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.Type: GrantFiled: May 22, 1997Date of Patent: June 15, 1999Assignee: Eli Lilly and CompanyInventors: Daniel James Koch, Vincent Patrick Rocco
-
Patent number: 5892037Abstract: The invention relates to compounds obtainable by polymerization of esters or phenol ethers of the formula V ##STR1## and/or of the formula VI ##STR2## in which m and n are each 0 or 1, and A, E, R.sup.1 to R.sup.6 and X are as defined in claim 1, and up to 50 mol % of other, ethylenically unsaturated compounds. The homopolymers and copolymers according to the invention can advantageously be employed for the stabilization of organic polymers against the harmful effect of light, oxygen and/or heat.Type: GrantFiled: March 12, 1996Date of Patent: April 6, 1999Assignee: Ciba Specialty Chemicals CorporationInventor: Alfred Steinmann
-
Patent number: 5889006Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.Type: GrantFiled: August 8, 1996Date of Patent: March 30, 1999Assignee: Schering CorporationInventors: Derek B. Lowe, Wei K. Chang, Joseph A. Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W. Clader, Samuel Chackalamannil, Yuguang Wang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom, Craig D. Boyle
-
Patent number: 5889023Abstract: A fibrinogen receptor antagonist which is 3(R)-?2-(Piperidin-4-yl)ethyl!-2-piperidon-1-ylacetyl-3(S)-(3-pyridyl)-.be ta.-alanine.Type: GrantFiled: May 5, 1997Date of Patent: March 30, 1999Assignee: Merck & Co., Inc.Inventors: John H. Hutchinson, George D. Hartman, Wasyl Halczenko
-
Patent number: 5889024Abstract: Compounds of formula I ##STR1## wherein Q.sup.1, Q.sup.2, Q.sup.3, Q.sup.4 and Q.sup.5 have any of the meanings given in the specification, their N-oxides, and their pharmacuetically acceptable salts are nonpeptide antagonists NKA, useful for the treatment of asthma, etc. Also disclosed are pharmaceutical compositions, processes for preparing the compounds of formula I and intermediates.Type: GrantFiled: April 23, 1996Date of Patent: March 30, 1999Assignee: Zeneca LimitedInventors: Scott C. Miller, Robert T. Jacobs, Ashokkumar B. Shenvi
-
Patent number: 5886191Abstract: The present application describes amidinoindoles, amidinoazoles, and analogs thereof of formula I: ##STR1## wherein W, W.sup.1, W.sup.2, and W.sup.3 are selected from CH and N, provided that one of W.sup.1 and W.sup.2 is C(C(.dbd.NH)NH.sub.2) and at most two of W, W.sup.1, W.sup.2, and W.sup.3 are N and one of J.sup.a and J.sup.b is substituted by --(CH.sub.2).sub.n --Z--A--B, which are useful as inhibitors of factor Xa or thrombin.Type: GrantFiled: August 18, 1997Date of Patent: March 23, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Celia Dominguez, Qi Han, Daniel Emmett Duffy, Jeongsook Maria Park, Mimi Lifen Quan, Karen Anita Rossi, Ruth Richmond Wexler
-
Patent number: 5883096Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds of formula I ##STR1## wherein one of Y and Z is N and the other is N, CH, or C-alkyl;X is --O--, --SO.sub.0-2 --, amino, substituted amino, --CO--, --CH.sub.2 --, mono or di-substituted methylene, --CS--, --CONR.sup.20 --, --NR.sup.20 --SO.sub.2 --, --NR.sup.20 CO--, --SO.sub.2 NR.sup.20 --, --CH.dbd.CH--, --C.tbd.C-- or --NHC(O)NH--;R is optionally substituted phenyl, aryl or cycloalkyl, or other substituents as defined in the specification;R.sup.1 and R.sup.21 are H, CN or optionally substituted alkyl, or other substituents as defined in the specification;R.sup.2 is optionally substituted cycloalkyl or piperidyl, or other substituents as defined in the specification; andR.sup.3, R.sup.4, R.sup.5, R.sup.20, R.sup.27 and R.sup.Type: GrantFiled: February 16, 1996Date of Patent: March 16, 1999Assignee: Schering CorporationInventors: Derek Lowe, Wei Chang, Joseph Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W. Clader, Samuel Chackalamannil, Wang Yuguang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom
-
Patent number: 5861414Abstract: The invention provides the compounds of formula (I) ##STR1## and pharmaceutically acceptable derivatives thereof, in which: X represents either CH.sub.2 --CH.sub.2 or CH.dbd.CH, andY represents a hydrogen atom or a phenylmethyl group, wherein the phenyl group is optionally substituted by one or more halogen atoms.Compounds of formula (I) inhibit blood platelet aggregation.Type: GrantFiled: May 29, 1997Date of Patent: January 19, 1999Assignee: Glaxo Group LimitedInventors: David George Allen, Colin David Eldred, William Leonard Mitchell
-
Patent number: 5856520Abstract: A novel substituted benzenedithiol metal complex represented by the general formula (1) is provided. The substituted benzenedithiol metal complex is useful as a singlet oxygen quencher and as an optical data recording medium per se. ##STR1## wherein M is a transition metal; A.sup.+ is a quaternary ammonium group; and R is an organic group selected from the group consisting of organic groups represented by the formulae (i), (ii), (iii) and (iv): ##STR2## (wherein R.sup.1 is an alkyl group having 1 to 4 carbon atoms), ##STR3## (wherein n is 3, 4 or 5), ##STR4## (wherein R.sup.2 is one of a hydrogen atom and a substitutent having 1 to 4 carbon atoms).Type: GrantFiled: October 20, 1997Date of Patent: January 5, 1999Assignee: Sumitomo Seika Chemicals Co., Ltd.Inventors: Kazuyoshi Hirako, Satoshi Kimura, Michio Suzuki
-
Patent number: 5849780Abstract: The invention relates to 1-Benzenesulfonyl-1,3-dihydroindol-2-one derivatives of the formula ##STR1## and their salts, where appropriate, to their preparation and to pharmaceutical compositions in which they are present. These compounds have an affinity for the vasopressin and/or ocytocin receptors.Type: GrantFiled: October 17, 1994Date of Patent: December 15, 1998Assignee: SanofiInventors: Alain Di Malta, Loic Foulon, Georges Garcia, Dino Nisato, Richard Roux, Claudine Serradeil-Legal, Gerard Valette, Jean Wagnon
-
Patent number: 5837707Abstract: This subject invention relates to dimeric 4-phenylpiperidine, 4-phenyl-1,2,3,6-tetrahydropyridine, or 4-phenylpiperazine compounds or dimeric spirocyclic piperidine compounds having general formula (I), ##STR1## wherein n is 1-5; R.sup.1 to R.sup.4 are substituents; R.sup.5 and R.sup.6 each hydrogen or alkyl or form together an ethylene or propylene bridge; X is O, S, SO, SO.sub.2, CO or (CH.sub.2).sub.m, m being 0 or 1, X is NR.sup.7, R.sup.7 being H, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, or phenylalkyl, or X is CR.sup.8 R.sup.9, wherein R.sup.8 and R.sup.9 are selected from hydroxy and the substituents defined under R.sup.7 ; and (i) Z.sup.1 is a substituent and Z.sup.2 is (CH.sub.2).sub.p wherein p is 0; and Y is N, C or CH; (ii) Z.sup.1 and Y are linked together via a single bond, thereby forming a spirocyclic junction; in which case Y is C; Z.sup.1 is O, S, (CH.sub.2).sub.q, q being 1, 2 or 3, or Z.sup.1 is CH.sub.2 O, CH.sub.2 S, CH.sub.2 CH.sub.2 O, CH.sub.2 CH.sub.2 S, CH.dbd.CH, CH.dbd.CHCH.Type: GrantFiled: June 6, 1995Date of Patent: November 17, 1998Assignee: H. Lundbeck A/SInventors: Jens Perregaard, John W. Stenberg, Ejner K. Moltzen
-
Patent number: 5830905Abstract: Derivatives of piperidine are useful in prophylaxis and treatment of hepatitis C virus infections.Type: GrantFiled: March 29, 1996Date of Patent: November 3, 1998Assignee: Viropharma IncorporatedInventors: Guy D. Diana, Thomas R. Bailey, Theodore J. Nitz
-
Patent number: 5821239Abstract: There are disclosed various substituted 4-amino-3-pyridinol compounds of the formula below, ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are as defined in the specification, which are useful for alleviating various memory dysfunctions characterized by a cholinergic deficit such as Alzheimer's disease.Type: GrantFiled: February 16, 1996Date of Patent: October 13, 1998Assignee: Frommer Lawrence & Huag LLPInventors: Gregory Micahel Shutske, Kevin James Kapples, John Dick Tomer, Nicholas Joseph Hrib, John Gerard Jurcak
-
Patent number: 5817677Abstract: 5-Membered heterocyclic compounds, of which the following compounds are exemplary:(a) 4-??trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-1-(4-piperidyl)imida zole,(b) 5-??trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-4-methyl-2-(4-piperi dyl)-1,3-thiazole,(c) 5-??4-(carboxymethoxy)phenyl!aminocarbonyl!-4-methyl-2-(4-piperidyl)-1,3-t hiazole,(d) 5-??trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-2-(4-piperidyl)-1,3, 4-thiadiazole,(e) 5-??4-(carboxymethoxy)phenyl!aminocarbonyl!-2-(4-piperidyl)-1,3,4-thiadiaz ole,(f) 5-??trans-4-(carboxymethoxy)cyclohexyl!aminocarbonyl!-2-(4-piperidyl)-1,3- thiazole,(g) 5-??4-(carboxymethoxy)phenyl!aminocarbonyl!-2-(4-piperidyl)-1,3-thiazole,(h) 5-??trans-4-(2-carboxyethyl)cyclohexyl!aminocarbonyl!-2-(4-piperidyl)-1,3- thiazole, and(i) 4-??trans-4-carboxycyclohexyl!aminocarbonyl!-1-?2-(4-piperidyl)ethyl!imida zole.Type: GrantFiled: October 18, 1996Date of Patent: October 6, 1998Assignee: Dr. Karl Thomae GmbHInventors: Gunter Linz, Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Brian Guth, Johannes Weisenberger
-
Patent number: 5814636Abstract: A compound represented by the general formula (I) and a pharmaceutically acceptable salt and solvate thereof having an effect for inhibiting the aggregation of platelets is disclosed: ##STR1## wherein A, B and C represent independently CH.sub.2 or C.dbd.O;X and Y are different from each other, and each of them is CH or N;D is --(CH.sub.2).sub.k -- or --(CH.sub.2).sub.m --CO-- where k is an integer of 1 to 4; and m is an integer of 0 to 3;E is the following group (II) or (III): ##STR2## wherein n is an integer of 1 to 3; and Z is --W--(CH.sub.2).sub.p --COOR.sup.3 (wherein W is --O-- or a bond; p is an integer of 1 to 4; and R.sup.3 is hydrogen, lower alkyl or an ester residue which can be removed under physiological conditions); R.sup.1 is hydrogen or lower alkyl; and R.sup.2 is hydrogen atom or lower alkyl.Type: GrantFiled: July 10, 1996Date of Patent: September 29, 1998Assignee: Meiji Seika Kabushiki KaishaInventors: Kiyoaki Katano, Shokichi Ohuchi, Tomoaki Miura, Eiki Shitara, Masaro Shimizu, Kazue Yaegashi, Naoto Ohkura, Yasuko Isomura, Hiroyuki Iida, Midori Ishikawa, Kenji Asai, Emiko Hatsushiba
-
Patent number: 5808064Abstract: We have found that 2-unsubstituted indoles of structural formula (IV) can be cost-effectively synthesized in high yield by the palladium-catalyzed coupling/ring closure of a 2-halo or 2-trifluoromethylsulfonyloxy aniline (I) and an acyl silane derivative (II), followed by deprotection of the silyl protecting groups. ##STR1## The process of the present invention is particularly useful to form indoles containing acid-labile substituents such as triazole, acetyl, ketal, cyano, and carbamate, or indoles having a good leaving group in the benzyl position. The advantages of the present process are that it does not require the use of triphenyl phosphine or tetrabutyl ammonium chloride or lithium chloride. When applied to 5-triazolyl substituted indoles, the present process also eliminates the tendency of triazolyl polymerization in the Fischer indole synthesis.Type: GrantFiled: August 7, 1997Date of Patent: September 15, 1998Assignee: Merck & Co., Inc.Inventors: Cheng-Yi Chen, Robert D. Larsen
-
Patent number: 5807852Abstract: Novel compounds of Formula (7.0a), (7.0b) or (7.0c): ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the formula (7.0a), (7.0b) or (7.0c) to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.Type: GrantFiled: May 19, 1995Date of Patent: September 15, 1998Assignee: Schering CorporationInventors: Ronald J. Doll, F. George Njoroge
-
Patent number: 5795893Abstract: This invention relates to novel compounds which inhibit platelet aggregation, pharmaceutical compositions containing the compounds, and methods of using the compounds.Type: GrantFiled: June 20, 1997Date of Patent: August 18, 1998Assignee: SmithKline Beecham CorporationInventors: William E. Bondinell, Thomas Wen-Fu Ku
-
Patent number: 5786371Abstract: Compounds of Formula I ##STR1## in which the variables are defined herein, processes for the production thereof as well as pharmaceutical agents containing these compounds for the treatment of diseases which are the result of thromboembolytic events.Type: GrantFiled: August 11, 1997Date of Patent: July 28, 1998Assignee: Boehringer Mannheim GmbHInventors: Christos Tsaklakidis, Alfred Mertens, Gerd Zimmermann, Wolfgang Schafer, Liesel Dorge
-
Patent number: 5783576Abstract: New compounds of general formula (I) are provided: ##STR1## which are explained in the specification can be prepared by a variety of methods. The compounds may be used in pharmaceutical compositions.Type: GrantFiled: August 9, 1996Date of Patent: July 21, 1998Assignee: Boehringer Ingelheim KGInventors: Otto Roos, Georg Speck, Walter Losel, Dietrich Arndts, Wolf-Dietrich Bechtel
-
Patent number: 5777113Abstract: The invention relates to novel compounds of formula I ##STR1## wherein the general symbols are as defined in claim 1, as stabilizers for organic materials against oxidative, thermal or light-induced degradation.Type: GrantFiled: October 10, 1995Date of Patent: July 7, 1998Assignee: Ciba Specialty Chemicals CorporationInventor: Rita Pitteloud
-
Patent number: 5776937Abstract: Compounds of the formula I ##STR1## wherein R.sup.1 and Y have the meanings indicated, and also their physiologically acceptable salts, inhibit the binding of fibrinogen to the corresponding receptor and can be employed for the treatment of thromboses, osteoporoses, oncoses, apoplexy, cardiac infarct, inflammations, arteriosclerosis and osteolytic disorders.Type: GrantFiled: November 7, 1995Date of Patent: July 7, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Joachim Gante, Horst Juraszyk, Peter Raddatz, Hanns Wurziger, Sabine Bernotat-Danielowski, Guido Melzer