The Additional Hetero Ring Is One Of The Cyclos In A Bicyclo Ring System Patents (Class 544/61)
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Patent number: 5990305Abstract: Disclosed is a photochromic compound having a diaryl-3H-napthopyran structure, which has at the 8-position a nitrogen atom-linked hetercyclus, in which the heterocylcus can also have a HALS compound as a substituent or the heterocyclus itself can be formed as a HALS compound.Furthermore a photochromic compound is described having a diaryl-3H-naphtopyran structure which has at the 8-position an N-atom linked and an alkyl-bridge linked HALS compound.Type: GrantFiled: February 5, 1998Date of Patent: November 23, 1999Assignee: Optische Werke G. RodenstockInventors: Herbert Zinner, Manfred Melzig
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Patent number: 5990109Abstract: Novel heterocyclo-substituted imidazopyrazines and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic disorders.Type: GrantFiled: March 4, 1999Date of Patent: November 23, 1999Assignee: Bristol-Myers Squibb Co.Inventors: Ping Chen, Derek J. Norris, Joel C. Barrish, Edwin J. Iwanowicz
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Patent number: 5981524Abstract: Optically active or racemic compounds represented by the formula ##STR1## where R.sub.1 is C.sub.1 to C.sub.4 straight chain or branched alkyl; R.sub.2 is selected from the group consisting of H, --OR.sub.1, --SR.sub.1, --NH(R.sub.1), --N(R.sub.4)(R.sub.5), aminocarbonyl, halogen, and --CN, where R.sub.4 and R.sub.5 are independently C.sub.1 to C.sub.6 straight chain or branched alkyl, or taken together form a 3- to 7-membered heterocycloalkyl substituent, such heteroatom selected from the group consisting of oxygen, nitrogen and sulfur, optionally including an additional heteroatom which is selected from the group consisting of nitrogen, oxygen, and sulfur; R.sub.3 is cyclopentyl or: ##STR2## where R' and R" are independently H, .dbd.O, --OH, or --NH.sub.2, with the proviso that R' and R" can be taken together form the following structure as R.sub.3 : ##STR3## where R'" is --OH or --NH.sub.2 ; and with the further proviso that when R.sub.3 is cyclopentyl or norbornyl, then R.sub.Type: GrantFiled: August 4, 1997Date of Patent: November 9, 1999Assignee: Discovery Therapeutics, Inc.Inventors: James V. Peck, Ronald J. Wysocki, Ibrahim M. Uwaydah, Noel J. Cusack
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Patent number: 5972975Abstract: Substituted 2-aminopyridine compounds of Formula (I) and pharmaceutically acceptable salts which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders.Type: GrantFiled: May 22, 1997Date of Patent: October 26, 1999Assignee: Merck & Co., Inc.Inventors: Craig Esser, William Hagmann, William Hoffman, Shrenik Shah, Kenny Wong, Renee Chabin, Ravindra Guthikonda, Malcolm Maccoss, Charles Caldwell, Philippe Durette
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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
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Patent number: 5965555Abstract: Compounds of the formula I, ##STR1## in which one of the radicals R.sup.1 and R.sup.3 is an alkynol residue of the formula Ia or Ib ##STR2## are suitable for producing pharmaceuticals having a neuroprotective effect.Type: GrantFiled: May 30, 1997Date of Patent: October 12, 1999Assignee: Hoechst AktiengesellschaftInventors: Ulrich Gebert, Elisabeth Defossa, Uwe Heinelt, Karl Rudolphi, John J. Grome
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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
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Patent number: 5919789Abstract: Compounds of the formula (i) ##STR1## have therapeutic utility via inhibition of TNF or phophodiesterase.Type: GrantFiled: November 17, 1997Date of Patent: July 6, 1999Assignee: Darwin Discovery LimitedInventors: Hazel Joan Dyke, John Gary Montana
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Patent number: 5912246Abstract: The present invention relates to imidazo?1,2-a!pyridine compounds of formula (1) ##STR1## which are dopamine D-4 antagonists and useful as anti-psychotic agents.Type: GrantFiled: August 14, 1997Date of Patent: June 15, 1999Assignee: Pharmacia & Upjohn CompanyInventor: Ruth E. Tenbrink
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Patent number: 5869499Abstract: A compound of chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein X and Y are each hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, halosubstituted C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl, C.sub.1 -C.sub.6 alkylsulfonyl, or tri(C.sub.1 -C.sub.6 alkyl)silyl; Ar.sup.1 and Ar.sup.2 are each independently aryl or heteroaryl, optionally substituted by halogen; A is --CO-- or -(CH.sub.2)-; Z-A- is at the 2 or 3 position on the quinuclidine ring; and Z is --OH, C.sub.1 -C.sub.6 alkoxy, NR.sup.1 R.sup.2 or the like. Representative compounds are (3S,4R,5S,6S)-5-?3,5-bis(trifluoromethyl)-benzyloxy!-N,N-dimethyl-6-diphen ylmethyl-1-azabicyclo?2.2.2!octan-3-carboxamide, and -3-carboxylic acid.Type: GrantFiled: March 3, 1996Date of Patent: February 9, 1999Assignee: Pfizer IncInventors: Kunio Satake, Hiroaki Wakabayashi
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Patent number: 5821240Abstract: Pyrimido?5,4-d!pyrimidines of the general formula ##STR1## which have an inhibitory effect on signal transduction mediated by tyrosine kinases, their use for the treatment of disorders, in particular of oncoses, and their preparation. Exemplary compounds are:4-?(3-Chloro-4-fluorophenyl)amino!-6-?1-methyl-4-piperidinylamino!pyrimido? 5,4-d!pyrimidine, and4-?(3-Chloro-4-fluorophenyl)amino!-6-?trans-4-dimethyl-aminocycohexylamino! pyrimido?5,4-d!pyrimidine.Type: GrantFiled: March 5, 1997Date of Patent: October 13, 1998Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Georg Dahmann, Thomas von Ruden, Thomas Metz
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Patent number: 5814642Abstract: A novel compound of the formula ##STR1## wherein Ar represents a tetracyclic fused heterocyclic group which may be substituted; R.sup.1 represents H or a hydrocarbon group which may be substituted; Y represents an amino acid or nitrogen-containing saturated heterocyclic group which may be substituted, its salt, inhibiting excellent cholinesterase inhibitory activity and monoamine uptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.Type: GrantFiled: July 30, 1996Date of Patent: September 29, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Giichi Goto, Yuji Ishihara, Masaomi Miyamoto
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Patent number: 5804685Abstract: Disclosed are compounds of the formula ##STR1## wherein Ar represents an aryl or heteroaryl group; andR.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 represent organic or inorganic substituents,which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and, thus, are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.Type: GrantFiled: June 7, 1995Date of Patent: September 8, 1998Assignee: Neurogen CorporationInventors: Jun Yuan, Alan Hutchison
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Patent number: 5770599Abstract: The invention concerns quinazoline derivatives of the formula I ##STR1## wherein n is 1, 2 or 3 and each R.sup.2 is independently halogeno, trifluoromethyl or (1-4C)alkyl;R.sup.3 is (1-4C)alkoxy; andR.sup.1 is di-?(1-4C)alkyl!amino-(2-4C)alkoxy, pyrrolidin-1-yl-(2-4C)alkoxy, piperidino-(2-4C)alkoxy, morpholino-(2-4C)alkoxy, piperazin-1-yl-(2-4C)alkoxy, 4-(1-4C)alkylpiperazin-1-yl-(2-4C)alkoxy, imidazol-1-yl-(2-4C)alkoxy, di-?(1-4C)alkoxy-(2-4C)alkyl!amino-(2-4C)alkoxy, thiamorpholino-(2-4C)alkoxy, 1-oxothiamorpholino-(2-4C)alkoxy or 1,1-dioxothiamorpholino-(2-4C)alkoxy, and wherein any of the above-mentioned R.sup.1 substituents comprising a CH.sub.2 (methylene) group which is not attached to a N or O atom optionally bears on said CH.sub.Type: GrantFiled: April 26, 1996Date of Patent: June 23, 1998Assignee: Zeneca LimitedInventor: Kieth Hopkinson Gibson
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Patent number: 5767128Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## wherein R.sub.1, W and Y are as defined in the description, its geometric and/or optical isomers, and its pharmaceutically-acceptable addition salts with an acid or a base useful as analgesies.Type: GrantFiled: November 5, 1996Date of Patent: June 16, 1998Assignee: Adir et CompagnieInventors: Gerald Guillaumet, Marie-Claude Viaud, Laurence Savelon, Panayota Pavli, Pierre Renard, Bruno Pfeiffer, Daniel-Henri Caignard, Jean-Guy Bizot-Espiard, Gerard Adam
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Patent number: 5723608Abstract: This invention encompasses compounds of the formula ##STR1## wherein Ar represents a mono-, di- or trisubstituted aryl group where at least one position on Ar ortho to the point of attachment to the pyrazole ring is substituted; andR.sub.1 represents lower alkyl;R.sub.2 is hydrogen or lower alkyl; andR.sub.3 and R.sub.4 independently represent organic and inorganic substituents,which compounds are highly selective partial agonists or antagonists at human CRF.sub.1 receptors and are useful in the diagnosis and treatment of treating stress related disorders such as post traumatic stress disorder (PTSD) as well as depression, headache and anxiety.Type: GrantFiled: December 31, 1996Date of Patent: March 3, 1998Assignee: Neurogen CorporationInventor: Jun Yuan
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Patent number: 5719147Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: September 8, 1995Date of Patent: February 17, 1998Assignee: Merck & Co., Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm MacCoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
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Patent number: 5719279Abstract: Xanthine derivatives of formula ##STR1## wherein R.sub.1 is hydrogen, alkyl or alkynyl,R.sub.2 is different and is alkyl, alkynyl, phenyl-alkylene, phenyl alkenylene, cycloalkyl, inter alia,R.sub.3 is cycloalkyl, phenyl, norbornane, inter alia andR.sub.4 is hydrogen, methyl, benzyl, inter alia.Type: GrantFiled: June 11, 1996Date of Patent: February 17, 1998Assignee: Boehringer Ingelheim KGInventors: Ulrike Kufner-Muhl, Helmut Ensinger, Joachim Mierau, Franz Josef Kuhn, Erich Lehr, Enzio Muller
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Patent number: 5708172Abstract: A novel industrial process excellent in yield and purity for preparing a compound of the formula: ##STR1## or a salt thereof, which comprises reacting a compound of the formula: ##STR2## or a salt thereof with a compound of the formula:R.sup.3 --A--OHor its reactive derivative or a salt thereof,wherein R.sup.2 is cyclo(lower)alkyl, aryl or ar(lower)alkyl, each of which may be substituted with halogen,R.sup.Type: GrantFiled: January 18, 1996Date of Patent: January 13, 1998Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Teruo Oku, Hiroshi Kayakiri, Hirokazu Tanaka
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Patent number: 5707989Abstract: The present invention relates to pyrimido?5,4-d!pyrimidines of the general formula ##STR1## in which R.sub.a to R.sub.c are as defined herein, their tautomers, their stereoisomers and their salts, in particular their physiologically tolerated salts with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibiting action on signal transduction mediated by tyrosine kinases, their use for the treatment of diseases, in particular tumor diseases.Type: GrantFiled: September 7, 1995Date of Patent: January 13, 1998Assignee: Dr. Karl Thomae GmbHInventors: Frank Himmelsbach, Thomas von Ruden, Georg Dahmann, Thomas Metz
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Patent number: 5703075Abstract: This invention relates to compounds of Formula I ##STR1## which are useful in association with a pharmaceutical carrier as antiatherosclerotic agents. In addition, various compounds of Formula I are useful inhibitors of cell proliferation.Type: GrantFiled: June 7, 1995Date of Patent: December 30, 1997Assignee: Pharmacia & Upjohn CompanyInventors: Ronald B. Gammill, Thomas M. Judge, Joel Morris
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Patent number: 5679670Abstract: Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.Type: GrantFiled: December 15, 1994Date of Patent: October 21, 1997Assignee: Alcon Laboratories, Inc.Inventors: Thomas Robert Dean, Hwang-Hsing Chen, Jesse Albert May
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Patent number: 5674878Abstract: Compound of general formula I ##STR1## wherein A is a benzo or thieno group;R.sub.1 is (C.sub.4-6)cycloalkyl, (C.sub.4-6)cycloalkyl-(C.sub.1-5)alkyl or ##STR2## R.sup.2, m, R.sup.3, R.sup.4, R and u are defined as in the specification, and pharmaceutical preparations containing this compound and the new pharmaceutical uses thereof.Type: GrantFiled: June 7, 1995Date of Patent: October 7, 1997Assignee: Boehringer Ingelheim KGInventors: Dietrich Arndts, Walter Losel, Otto Roos
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Patent number: 5670501Abstract: Optically active or racemic compounds represented by the formula ##STR1## where R.sub.1 is C.sub.1 to C.sub.4 straight chain or branched alkyl; R.sub.2 is selected from the group consisting of H, --OR.sub.1, --SR.sub.1, --NH(R.sub.1), --N(R.sub.4)(R.sub.5), aminocarbonyl, halogen, and --CN, where R.sub.4 and R.sub.5 are independently C.sub.1 to C.sub.6 straight chain or branched alkyl, or taken together form a 3- to 7-membered heterocycloalkyl substituent, such heteroatom selected from the group consisting of oxygen, nitrogen and sulfur, optionally including an additional heteroatom which is selected from the group consisting of nitrogen, oxygen, and sulfur; R.sub.3 is cyclopentyl or: ##STR2## where R' and R" are independently H, .dbd.O, --OH, or --NH.sub.2, with the proviso that R' and R" can be taken together form the following structure as R.sub.3 : ##STR3## where R'" is --OH or --NH.sub.2 ; and with the further proviso that when R.sub.3 is cyclopentyl or norbornyl, then R.sub.Type: GrantFiled: September 1, 1994Date of Patent: September 23, 1997Assignee: Discovery Therapeutics, Inc.Inventors: James V. Peck, Ronald J. Wysocki, Ibrahim M. Uwaydah, Noel J. Cusack
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Patent number: 5661148Abstract: A pyrrolo[2,3-d]pyrimidine derivative having the general formula [I] ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, Y and Z have the same definitions as those given in the description, a pharmaceutically acceptable acid addition salt thereof, and a pharmaceutical preparation comprising the same, are provided.Type: GrantFiled: June 7, 1995Date of Patent: August 26, 1997Assignee: Teijin LimitedInventors: Yasuji Sakuma, Masaichi Hasegawa, Kenichiro Kataoka, Kenji Hoshina, Noboru Yamazaki, Takashi Kadota, Hisao Yamaguchi
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Patent number: 5656758Abstract: A process for preparing a compound of the formula (I): ##STR1## in which, R.sup.1 and R.sup.2 each represents hydrogen or C.sub.1 -C.sub.6 alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocycle; E represents methylene, sulfur, oxygen or imino group optionally substituted with C.sub.1 -C.sub.6 alkyl or aralkyl; ring A is aryl or heteroaryl ring, optionally substituted; R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl and R.sup.4 is hydrogen or R.sup.3 and R.sup.4 together represent a group of formula (IV):--(CR.sup.a R.sup.a).sub.m --C(.dbd.Y)-- (IV)(wherein R.sup.a and R.sup.a is C.sub.1 -C.sub.6 alkyl or hydrogen, up to a maximum of 3 alkyl groups, m is 1, 2, or 3, and Y is two hydrogens or oxygen); provided that when E represents a methylene group, then R.sup.3 is a C.sub.1 -C.sub.6 alkyl group or R.sup.3 and R.sup.Type: GrantFiled: March 24, 1995Date of Patent: August 12, 1997Assignee: Sankyo Company, LimitedInventors: Atsusuke Terada, Yoshio Iizuka, Kazuyuki Wachi, Kenji Fujibayashi
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Patent number: 5627136Abstract: Pyridine-N-oxide-substituted salicylaldehyde and salicylic acid derivatives of the general formula I ##STR1## where R is a formyl group, a CO.sub.2 H group or a radical which can be hydrolyzed to CO.sub.2 H and the other substituents have the following meanings:R.sup.2 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio;X is nitrogen or CR.sup.13, R.sup.13 being hydrogen or halogen or together with R.sup.3 forming a 3- to 4-membered alkylene or alkenylene chain in which at least one methylene group is replaced by oxygen;R.sup.3 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio, or R.sup.3 is linked with R.sup.13 as indicated above to give a 5- or 6-membered ring;Y is oxygen or sulfur;R.sup.14 -R.sup.Type: GrantFiled: November 1, 1994Date of Patent: May 6, 1997Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Uwe J. Vogelbacher, Ernst Baumann, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
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Patent number: 5618819Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## wherein R.sub.1, W and Y are as defined in the description, its geometric and/or optical useful as anti-algies.Type: GrantFiled: July 3, 1995Date of Patent: April 8, 1997Assignee: Adir et CompagnieInventors: G erald Guillaumet, Marie-Claude Viaud, Laurence Savelon, Panayota Pavli, Pierre Renard, Bruno Pfeiffer, Daniel-Henri Caignard, Jean-Guy Bizot-Espiard, G erard Adam
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Patent number: 5593943Abstract: Heteroaromatically condensed hydroxypyridonecarboxamides of the structure I ##STR1## where the substituents and the ring Q have the following meanings: R.sup.1 hydrogen, hydroxyl, substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, alkoxy;R.sup.2 hydrogen, substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, alkenyloxy, dialkylamino;orR.sup.1, R.sup.2 together denote an alkylene chain with 2-6 members and which may be interrupted by oxygen, sulfur or N-methyl;X oxygen or sulfur;Q a 5- or 6-membered heteroaromatic ring containing from 1 to 3 nitrogen atoms and/or one oxygen or sulfur atom as heteroatoms, and which may be substituted one to three times,and environmentally compatible salts thereof.Type: GrantFiled: June 17, 1994Date of Patent: January 14, 1997Assignee: BASF AktiengesellschaftInventors: Christoph Nuebling, Wolfgang von Deyn, Hans Theobald, Karl-Otto Westphalen, Uwe Kardorff, Helmut Walter, Thomas Kappe, Matthias Gerber
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Patent number: 5574037Abstract: This invention concerns novel compounds of the formula I: ##STR1## in which P is a group of formula II or a group of formula III; R.sup.1 is alkyl, cycloalkyl, cycloalkylalkyl, phenyl or phenylalkyl; R.sup.2 is hydrogen, alkyl, amino or alkylamino; R.sup.3 and R.sup.4 are independently hydrogen, alkyl, phenyl or benzyl; R.sup.6 is alkyl, amino or alkylamino; C and D are independently ethylene or trimethylene; Z is a direct bond between C and D, or an oxy, thio, carbonyl, methylene, ethylenedioxymethylene, ethylidene, or isopropylidene link, or Z is a group of the formula .dbd.N.R.sup.5 in which R.sup.5 is alkyl, phenyl or benzyl; R8 is hydrogen, cycloalkylalkyl, alkyl, alkenyl, alkynyl or phenylalkyl; or R8 is a alkylene or alkenylene linked to the nitrogen atom of the group Q.A.Type: GrantFiled: June 7, 1995Date of Patent: November 12, 1996Assignee: Imperial Chemical Industries PLCInventors: Stuart D. Mills, Rodney B. Hargreaves, Bernard J. McLoughlin
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Patent number: 5506262Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthetase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.Type: GrantFiled: November 10, 1993Date of Patent: April 9, 1996Assignee: Merck & Co., Inc.Inventors: Robert M. Burk, William H. Parsons, John J. Acton, III, Gregory D. Berger, Tesfaye Biftu, Robert L. Bugianesi, Yuan-Ching P. Chiang, Claude Dufresne, Narindar N. Girotra, Robert W. Marquis, Jr., Chan-Hwa Kuo, Sandra P. Plevyak, Mitree M. Ponpipom, Lori L. Whiting, James D. Bergstrom, Conrad Santini
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Patent number: 5502187Abstract: The pharmaceutically active bicyclic heterocyclic amines (XXX) ##STR1## where W.sub.1 is --N.dbd. or --CH.dbd.; W.sub.3 is --N.dbd. or --CH.dbd.; W.sub.5 is --N.dbd. or --CR.sub.5 -- with the proviso that W.sub.5 is --CR.sub.5 -- when both W.sub.1 and W.sub.3 are --N.dbd. which are useful as pharmaceuticals in treating mild and/or moderate to severe head injury, subarachnoid hemorrhage and subsequent ischemic stroke, asthma and reduction of mucous formation/secretion in the lung and other diseases and injuries.Type: GrantFiled: October 3, 1994Date of Patent: March 26, 1996Assignee: The Upjohn CompanyInventors: Donald E. Ayer, Gordon L. Bundy, Eric J. Jacobsen
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Patent number: 5470975Abstract: Novel A-II receptor antagonists have the formula ##STR1## and its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.Type: GrantFiled: January 11, 1994Date of Patent: November 28, 1995Assignee: E.R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 5428160Abstract: Disclosed are compounds of formula I ##STR1## wherein R.sub.1 represents hydrogen, lower alkyl, substituted lower alkyl, nitro, halogen, free, etherified or esterified hydroxy, free, etherified, oxidised etherified or esterified mercapto, unsubstituted, mono- or disubstituted amino, ammonio, free or functionally modified sulfo, free or functionally modified formyl, C.sub.2 -C.sub.20 -acyl, cyano, free or functionally modified carboxy; and R.sub.2 represents hydrogen, lower alkyl, substituted lower alkyl, halogen; free, etherified or esterified hydroxy; free, etherified, oxidised etherified or esterified mercapto; free or functionally modified carboxy, or acyl; the 7,8-dihydro derivatives thereof; and compounds of the formula I* ##STR2## wherein n denotes 0, 1, 2, 3, or 4, and R.sub.1 and R.sub.2 are as defined above under formula I and salts thereof; e.g. as aromatase inhibitors; pharmaceutical compositions containing these compounds; the use of these compounds for the treatment of conditions responsive to e.Type: GrantFiled: December 21, 1990Date of Patent: June 27, 1995Assignee: Ciba-Geigy CorporationInventor: Leslie J. Browne
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Patent number: 5413997Abstract: A triphenylmethane derivative represented by the following general formula: ##STR1## exhibits bone absorption inhibiting effects and is useful as a medicament for treating osteoporosis.Type: GrantFiled: January 21, 1993Date of Patent: May 9, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Iwao Kinoshita, Daisuke Machii, Yasuo Onoda, Haruki Takai, Nobuo Kosaka, Katsuichi Shuto, Katsushige Gomi, Makoto Morimoto, Akio Ishii
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Patent number: 5391733Abstract: The present invention is directed to a method for production of a 2-amino-6-halogenopurine, a novel synthesis intermediate therefor and a method for production of said synthesis intermediate. The desired 2-amino-6-halogenopurine is an intermediate for the production of compounds useful as an antiviral agent, and by using the compound of the present invention as a starting material, the 2-amino-6-halogenopurine can be produced in high yield.Type: GrantFiled: August 31, 1992Date of Patent: February 21, 1995Assignee: Sumika Fine Chemicals Co., Ltd.Inventors: Masami Igi, Taketo Hayashi
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Patent number: 5378700Abstract: Disclosed is a fused pyrimidine of the formula [I] ##STR1## wherein R.sup.1, R.sup.2, and R.sup.Type: GrantFiled: June 9, 1992Date of Patent: January 3, 1995Assignee: Teijin LimitedInventors: Yasuji Sakuma, Masaichi Hasegawa, Kenichiro Kataoka, Kenji Hoshina, Noboru Yamazaki, Takashi Kadota, Hisao Yamaguchi
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Patent number: 5354753Abstract: Disclosed is a compound represented by the formula: ##STR1## wherein R.sup.1 : CH.sub.2, CH.sub.2 CH.sub.2, CH.sub.2 O, CH.sub.2 S, CH.sub.2 SO; R.sup.2 : hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms or a benzyl group; n: an integer of 1 to 4; R.sup.3 : COOR.sup.4, NHCOR.sup.5, CONR.sup.6 R.sup.7, PO.sub.3 H.sub.2, SO.sub.3 H.The compound shows potent antirheumatic function, psoriasis curing function and carcinostatic function and has low toxicity whereby it is available as a medicine.Type: GrantFiled: February 12, 1993Date of Patent: October 11, 1994Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Nobuhiro Ohi, Hiroharu Matsuoka, Katushito Miyamoto, Hiroshi Suzuki, Nobuaki Kato, Keiichiro Tsuji, Yasuhisa Takeda, Masahiko Mihara, Hiromichi Nishina, Shin Shimaoka, Kenichi Akamatsu
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Patent number: 5336676Abstract: Compounds of formula (I) ##STR1## wherein R is an alkyl group; R.sub.1 is a cyano, carboxy, alkoxycarbonyl or hydroxylaminocarbonyl group; R.sub.2 is substituted or unsubstituted phenyl (C.sub.3 -C.sub.7)-cycloalkyl, .alpha.-, .beta.- or .gamma.-pyridyl or a benzoheteroxcyclic ring; R.sub.3 is carboxy or carboalkoxy; Y is a group of the formula --COOX; --NHCOA; --NCO; --COA; --CONHOR.sub.e ; --OCOA; A; --COCH.sub.2 COR.sub.f ; --NHCSA; --OCSA; (a); X is hydrogen, alkyl or succinimidyl group; A is a cyclic or acyclic amino group; and n is 1 or 2; having pharmacological characteristics which render them useful in the treatment of inflammatory conditions of the respiratory tract and asthmatic conditions.Type: GrantFiled: December 4, 1992Date of Patent: August 9, 1994Assignee: Boehringer Mannheim Italia S.p.A.Inventors: Carmelo A. Gandolfi, Giampiero De Cillis, Giorgio Long, Licia Gallico
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Patent number: 5330987Abstract: Novel substituted pyridopyrimidinones of formula (I), which are useful as angiotensin II antagonists, are disclosed.Type: GrantFiled: June 4, 1992Date of Patent: July 19, 1994Assignee: Merck & Co., Inc.Inventors: Eric E. Allen, Prasun K. Chakravarty, Stephen E. de Laszlo, William J. Greenlee, Arthur A. Patchett, Thomas F. Walsh
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Patent number: 5326783Abstract: This invention is directed to compounds of formula (I) which are novel C3- or C5-acyl sulfonamide, carboxamic acid or tetrazolyl analogs of the Zaragozic acids. These compounds inhibit the enzyme squalene synthase and are useful as cholesterol lowering agents.Type: GrantFiled: January 19, 1993Date of Patent: July 5, 1994Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, Chan-Hwa Kuo, Conrad Santini
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Patent number: 5260285Abstract: Novel substituted imidazopyridazines of formula (I) which are useful as angiotensin II antagonists, are disclosed.Type: GrantFiled: November 25, 1991Date of Patent: November 9, 1993Assignee: Merck & Co., Inc.Inventors: Eric E. Allen, William J. Greenlee, Prasun K. Chakravarty, Malcolm MacCoss, Arthur A. Patchett, Thomas F. Walsh
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Patent number: 5250533Abstract: Fungicidal pyridinylpyrimidines of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, alkoxy, alkylthio, halogenoalkyl, amino or dialkylamino, where, in the case of dialkylamino, the two radicals may, together with the nitrogen to which they are bonded, form a 5- to 7-membered, saturated or unsaturated ring which optionally contains a further hetero atom and which is optionally substituted by 1 or 2 alkyl groups; orR.sup.1 represents in each case optionally substituted aryloxy, arylthio, aralkyloxy or aralkylthio,R.sup.2 and R.sup.3 are independent of one another and are identical or different and in each case represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, alkylthio or alkoxycarbonyl,orR.sup.2 and R.sup.3 together represent anaylene chain having 3 to 6 carbon atoms which are linked via the ring positions 3 and 4 or 4 and 5,R.sup.Type: GrantFiled: March 2, 1992Date of Patent: October 5, 1993Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Alexander Klausener, Dieter Berg, Stefan Dutzmann, Wilhelm Brandes
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Patent number: 5250521Abstract: Novel substituted pyrazolopyrimidines of formula (I) which are useful as angiotensin II antagonists, are disclosed.Type: GrantFiled: November 25, 1991Date of Patent: October 5, 1993Assignee: Merck & Co., Inc.Inventors: Eric E. Allen, William J. Greenlee, Prasun K. Chakravarty, Malcolm MacCoss, Arthur A. Patchett, Thomas F. Walsh
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Patent number: 5229522Abstract: Novel bis-(indolyl)ethylenes, process for their production and record systems utilizing such bis-(indolyl)ethylene chromogens are described.Bis-(indolyl)ethylenes of the following general formula are prepared: ##STR1## wherein each L.sup.1 and L.sup.2 is the same or different and is each independently selected from indole moieties (J1) through (J4) (L.sup.1 need not be the same as L.sup.2), ##STR2## wherein Z is hydrogen, alkyl (C.sub.1 -C.sub.8), substituted or unsubstituted aryl, aralkyl, aroxyalkyl, alkoxyalkyl or halogen.Type: GrantFiled: September 4, 1990Date of Patent: July 20, 1993Assignee: Appleton Papers Inc.Inventor: Ponnampalam Mathiaparanam
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Patent number: 5227379Abstract: Piperidine compounds having the formula ##STR1## wherein R.sup.3 is 3,4-methylenedioxyphenyl, phenyl, or naphthyl which are optionally substituted with one or more halogen, C.sub.1-6 -alkoxy, or phenoxy, cyano, mono or poly halogenated C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl, C.sub.1-6 -alkyl, or C.sub.3-5 -alkylene, R.sup.1 is straight or branched C.sub.1-8 -alkyl substituted with piperidinyl morpholinyl thiomorpholinyl dioxolanyl or tetrahydrofuranyl, which heterocyclic radical is unsubstituted or C.sub.1-6 -alkyl substituted,X is hydrogen, halogen, trifluoromethyl, hydroxy, cyano, or C.sub.1-8 -alkoxy,Y is O or S; and pharmaceutically-acceptable acid addition salts thereof.The compounds are useful in the treatment of anoxia, migraine, ischemia, and epilepsy.Type: GrantFiled: December 5, 1991Date of Patent: July 13, 1993Assignee: Novo Nordisk A/SInventors: Palle Jakobsen, Jorgen Drejer
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Patent number: 5217973Abstract: The present invention relates to the derivatives of formula: ##STR1## as well as to their addition salts and to their use in therapy, in particular for the treatment of cardiovascular diseases, especially for the treatment of hypertension, cardiac insufficiency and diseases of the arterial wall.Type: GrantFiled: August 7, 1991Date of Patent: June 8, 1993Assignee: Laboratoires UPSAInventors: Nicole Bru-Magniez, Eric Nicolai, Jean-Marie Teulon
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Patent number: 5216001Abstract: Specific 6-substituted or 2-alkyl substituted indole or 2,3-dihydroindole compounds are provided, having long lasting serotonin activity with specific binding to 5-HT.sub.2 receptors of the central nervous system. These compounds are suitable for therapeutic treatment of CNS disorders, such as anxiety, depression, sleep disturbances, migraine, negative symptoms of schizophrenia, and Parkinson's disease.Type: GrantFiled: June 27, 1991Date of Patent: June 1, 1993Assignee: H. Lunbeck A/SInventors: Jens K. Perregaard, Kim Andersen, Klaus P. Boegesoe, Henrik Pedersen
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Patent number: 5202324Abstract: The imidazo[1,2-b]pyridazine compounds of the formula: ##STR1## wherein R.sub.1 is a hydrogen or halogen atom, or a lower alkyl group optionally having substituent(s), R.sub.2 and R.sub.3 are, independently, a hydrogen atom, a lower alkyl group optionally having substituent(s), a cycloalkyl group or a phenyl group optionally having substituent(s) or R.sub.2 and R.sub.3 together with the adjacent nitrogen atom to which they bond may form a heterocyclic ring optionally having substituent(s), X is an oxygen atom or S(O).sub.n (n=0 to 2), Alk is a straight or branched chain alkylene group containing 1-10 carbon atoms and optionally having substituent(s), or their pharmaceutically acceptable salts which possess antiallergic, anti-inflammatory and anti-PAF activities, and their production and use.Type: GrantFiled: January 31, 1990Date of Patent: April 13, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Akio Miyake, Masaaki Kuwahara, Hisashi Kuriki
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Patent number: 5182275Abstract: There are disclosed novel compounds of the formula ##STR1## where X is hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, nitro or trifluoromethyl; R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen, loweralkyl, arylloweralkyl or --(CH.sub.2).sub.m R.sub.7 wherein m is 1, 2 or 3 and R.sub.7 is cyano or amino; R.sub.3 and R.sub.4 are independently hydrogen or loweralkyl; R.sub.5 and R.sub.6 are independently hydrogen or loweralkyl, or R.sub.5 +R.sub.6 taken together with the carbon atom to which they are attached constitute a cyclobutane, cyclopentane, cyclohexane, cycloheptane, pyrrolidine, piperidine, morpholine or thiomorpholine ring, or R.sub.5 is hydrogen and R.sub.6 is aryl or --CH.sub.2 OR.sub.8 wherein R.sub.8 is hydrogen, loweralkyl or loweralkylcarbonyl, which are useful for enhancing memory.Type: GrantFiled: May 10, 1990Date of Patent: January 26, 1993Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: Karl Schonafinger, Helen H. Ong