Polycyclo Ring System Having The Oxazole Ring As One Of The Cyclos Patents (Class 548/217)
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Patent number: 5665737Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition as compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE III inhibition.Type: GrantFiled: October 12, 1994Date of Patent: September 9, 1997Assignee: Euro-Celtique, S.A.Inventors: John David Cavalla, Lloyd J. Dolby, Peter Hofer, Mark Chasin
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Patent number: 5648534Abstract: 1,2-di-substituted indan expressed by general formula (I) wherein X is a substituent which can be drawn out under an acidic condition to form a carbocation at 1-position of an indan skeleton, Y is a halogen atom, and X and Y can be in either cis- or trans-configuration forming either a racemic body or an optically active substance; or 1,2-di-substituted indan expressed by general formula (I') wherein X is a substituent which can be drawn out under an acidic condition to form a carbocation at 1-position of an indan skeleton, and X and OH group can be in either cis- or trans-configuration forming either a racemic body or an optically-active substance; or cis-1,2-epoxyindan expressed by general formula (VI) wherein R is phenyl or a lower alkyl group, oxazoline ring is in cis-configuration forming either a racemic body or an optically active substance is reacted, under an acidic condition, with a nitrile expressed by general formula (II) wherein R is phenyl or a lower alkyl group to produce cis-1-aminoindan-2-olType: GrantFiled: November 30, 1994Date of Patent: July 15, 1997Assignee: Ichikawa Gosei Chemical Co., Ltd.Inventors: Yoshio Igarashi, Fumihiro Asano, Makoto Shimoyamada, Masayuki Harada, Shigeru Nakano, Ryoji Iwai, Keisuke Yagami, Yuzi Konno
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Patent number: 5643958Abstract: The present invention relates to a compound of the formula (I): ##STR1## wherein Ar.sup.1, Ar.sup.2 and Ar.sup.3 represent an aryl group or a heteroaromatic ring group; A represents a hydrocarbon group which may be substituted; Q represents a group of the formula --(CH.sub.2).sub.m -- (m is an integer of from 1 to 6) or --(CH.sub.2).sub.n --W--(CH.sub.2).sub.p -- (W is an oxygen atom, a sulfur atom, a vinylene group or an ethynylene group; n and p are a integer of from 0 to 3); R.sup.1 represents a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group, a lower alkoxy group, an aryl or heteroaromatic ring group which may be substituted; R.sup.2, R.sup.7 and R.sup.8 represent a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group; R.sup.3 and R.sup.Type: GrantFiled: March 15, 1996Date of Patent: July 1, 1997Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Aoyama, Kumiko Kawakami, Sachie Arai, Toshihiko Satoh, Yoshiaki Monden
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Patent number: 5637724Abstract: Disclosed are compounds of the formula: ##STR1## wherein: T is NH, O, or S;X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide;the W ring is an optionally substituted aryl or heteroaryl group; and ##STR2## represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: June 5, 1995Date of Patent: June 10, 1997Assignee: Neurogen CorporationInventors: Robert W. DeSimone, Charles A. Blum
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Patent number: 5637725Abstract: Disclosed are compounds of the formula: ##STR1## wherein: T is NH, O, or S;X is hydrogen, hydroxyl, lower alkyl, or an optionally substituted amide;the W ring is an optionally substituted aryl or heteroaryl group; and ##STR2## represents an optionally substituted benzo group or an optionally substituted 5, 6, 7, or 8 membered ring.These compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory.Type: GrantFiled: June 5, 1995Date of Patent: June 10, 1997Assignee: Neurogen CorporationInventors: Robert W. DeSimone, Charles A. Blum
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Patent number: 5635107Abstract: Fluorine-containing five-membered ring compounds of the formula IR.sup.1 -(A.sup.1 -Z.sup.1).sub.m -A.sup.2 -Z.sup.2 -W Iin whichW is ##STR1## is a cyclohexane, cyclohexene or phenyl,Y.sup.1 is O or S,Y.sup.2 is (a) O, S, C.dbd.O or fluoroalkyl,Y.sup.3 is (a) N, CH or CF,Q is C.dbd.O, CHF, CF.sub.2, CHR.sup.2 or CFR.sup.2Q' is CF or CR.sup.2,R.sup.2 is C.sub.1-15 -alkyl, optionally at least mono-substituted by F,X is H, F or Cl,R.sup.1 H or hydrocarbyl,A.sup.1 and A.sup.2 are a carbocyclic, aromatic or heterocyclic radicalZ.sup.1 and Z.sup.2 are --CO--O, --O--CO--, --CH.sub.2 O--, --O--CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.ident.C-- or a single bond, andm is 0, 1 or 2, and liquid-crystalline media containing same.Type: GrantFiled: January 8, 1993Date of Patent: June 3, 1997Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Ekkehard Bartmann, Georg Weber
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Patent number: 5631253Abstract: Compounds having the formula (I): ##STR1## and stereoisomers thereof, wherein A is hydrogen, halo, hydroxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 haloalkyl, C.sub.1-4 haloalkoxy, C.sub.1-4 alkylcarbonyl, C.sub.1-4 alkoxycarbonyl, phenoxy, nitro or cyano; R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocyclylalkyl, optionally substituted cycloalkylalkyl, optionally substituted aralkyl, optionally substituted heteroarylalkyl, optionally substituted aryloxyalkyl, optionally substituted heteroaryloxyalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aryloxy, optionally substituted heteroaryloxy, nitro, halo, cyano, --NR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --S(O).sub.n R.sup.3 wherein n is 0, 1 or 2, (CH.sub.2).sub.m PO(OR.Type: GrantFiled: December 2, 1994Date of Patent: May 20, 1997Assignee: Zeneca LimitedInventors: Paul J. de Fraine, Anne Martin
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Patent number: 5629265Abstract: Disclosed herein are cyanoketone derivatives of the following formula (1) ##STR1## such as 1-cyano-1-piperidinocarbonyl-3-[4-(2-chloro-4-trifluoromethylphenoxy)pheno xy]-2-butanone, 1-cyano-1-piperidinocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-pyridyloxy )phenoxy]-2-butanone, 1-cyano-1-(N-methyl-N-dichlorophenyl)aminocarbonyl-3-[4-(2-quinoxalyloxy)p henoxy]-2-butanone, 1-cyano-1-(N,N-dibutyl)aminocarbonyl-3-[4-(3-chloro-5-trifluoromethyl-2-py ridyloxy)phenoxy-2-butanone, and the like, which are characterized by excellent herbicidal activity and effectiveness against a variety of gramineous weeds.Type: GrantFiled: June 22, 1994Date of Patent: May 13, 1997Assignee: Tokuyama CorporationInventors: Masahiko Ishizaki, Seiji Nagata, Junji Takenaka
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Patent number: 5618939Abstract: A process is disclosed for making a chiral compound of the formula ##STR1## comprising reacting an epoxide compound of the formula ##STR2## and an amide of the formula ##STR3## in the presence of a strong base at a low temperature.Type: GrantFiled: June 7, 1995Date of Patent: April 8, 1997Assignee: Merck & Co., Inc.Inventors: David Askin, Paul Reider, Kai Rossen, Richard J. Varsolona, Ralph P. Volante, Kenneth M. Wells
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Patent number: 5616725Abstract: Pyrrolo[3,4-c]pyrroles of formula ##STR1## wherein D and E are each independently of the other a group of formula ##STR2## The symbols Q, R.sub.8, R.sub.9, R.sub.10, R.sub.11, X, Y, Z, m and n are as defined in claim 1.These pyrrolo[3,4-c]pyrroles are distinguished by outstanding solid state fluorescence in the UV range as well as by the ease with which they can be converted to pyrrolopyrrole pigments even in the substrate in which they are incorporated.Type: GrantFiled: October 11, 1995Date of Patent: April 1, 1997Assignee: Ciba-Geigy CorporationInventors: John S. Zambounis, Zhimin Hao, Abul Iqbal
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Patent number: 5614544Abstract: [Object]To provide a new 2,4-oxazolidinedione derivative possessing excellent hypoglycemic and hypolipidemic activities.[Constituent]A 2,4-oxazolidinedione derivative represented by the general formula: ##STR1## wherein X represents --CH.sub.2 --, --C(.dbd.O)--, --CH(OH)--, --C(.dbd.NOH)-- or --CH.dbd.CH--; R represents a hydrocarbon residue or heterocyclic group which may be substituted; n represents an integer from 0 to 5, and m represents an integer from 1 to 3; ....... represents a single or double bond; provided that n is an integer from 1 to 5 when X is --C(.dbd.O)--, or a pharmacologically acceptable salt thereof.Type: GrantFiled: September 8, 1994Date of Patent: March 25, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Takashi Sohda, Hitoshi Ikeda, Yu Momose
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Patent number: 5612480Abstract: Novel 2-chloro and 2-bromo derivatives of 1,5-iminosugars are disclosed, especially such derivatives of 1,5-dideoxy-1,5-imino-D-glucitol. These compounds are useful inhibitors of glucosidase enzymes and also are useful as antiviral agents and as intermediates for the synthesis of other enzyme inhibitors and antiviral compounds.Type: GrantFiled: March 6, 1995Date of Patent: March 18, 1997Assignee: G. D. Searle & Co.Inventors: Thomas E. Barta, Richard A. Mueller
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Patent number: 5591762Abstract: Disclosed herein are angiotensin-II antagonists of the formula ##STR1## wherein R.sub.1 is, other than hydrogen and, inter alia, halogen, lower alkyl or cycloalkyl; R.sub.2 is, inter alia, optionally substituted benzimidazol-2-yl, 5,6,7,8-tetrahydro-imidazo[1,2-a]pyridin-2-yl, butanesultam-1-yl, imidazol-4-yl, and tetrahydobenzimidazol-2-yl; R.sub.3 is, inter alia, lower alkyl; and, R.sub.4 is an acidic group, such as carboxyl or tetrazolyl.An exemplary compound is:(a) 4'-[[2-n-propyl-4-methyl-6-(1-methylbenzimidazole-2-yl)-benzimidazol-1-yl] methyl]-biphenyl-2-carboxylic acid.Type: GrantFiled: June 1, 1995Date of Patent: January 7, 1997Assignee: Dr. Karl Thomae GmbHInventors: Norbert Hauel, Berthold Narr, deceased, Uwe Ries, Jacobus C. A. van Meel, Wolfgang Wienen, Michael Entzeroth
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Patent number: 5587112Abstract: A new class of proton transfer, benzazole, fluorescent compounds is composed of a 2-benzazolyl moiety covalently bonded to an aromatic fused ring heterocyclic moiety. The 2-benzazolyl moiety may be a 2-benzoxazolyl, 2-benzothiazolyl, or 2-benzimidazolyl. The aromatic fused ring heterocyclic moiety may be a 3-dibenzofuranyl or 3-dibenzothiophenyl each substituted at the 2 position with a proton donating group, or a 2-carbazolyl substituted at the 3 position with a proton donating group. The proton donating group may be hydroxy, sulfonamido, carbonamido, and the like, and preferably is hydroxy. The fluors are soluble in organic matrix materials such as solvents, monomers, resins, polymers, and the like. The UV-excited fluors emit short-lived fluorescence at .gtoreq.520 nm and may be used in the manufacture of fluorescent coatings, objects, scintillators, light sources and the like.Type: GrantFiled: September 2, 1994Date of Patent: December 24, 1996Assignee: Philadelphia College of Pharmacy and ScienceInventors: Joel M. Kauffman, Peter T. Litak
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Patent number: 5587482Abstract: The present invention is directed to a dye suitable for spectral sensitization of a photographic element. Specifically, the dye is a compound having the structure: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, and R.sup.4 each independently represents H; halogen; alkyl of 1-6 carbons; aryl of 6-24 carbons; alkoxy of 1-6 carbons; carbonyl; or sulfonate; or R.sup.1 and R.sup.2, R.sup.2 and R.sup.3, or R.sup.3 and R.sup.4 taken together represent the atoms necessary to complete a six-membered carbocylic ring;R.sup.5 represents hydrogen, alkyl of 1-6 carbons or aryl of 6-24 carbons;R.sup.6, R.sup.7, and R.sup.8 independently represent alkyl 1-6 carbons; aryl of 6-24 carbons; or any pair of R.sup.6, R.sup.7 and R.sup.8 taken together represent a five- or six-member heterocyclic ring;X represents O, S, CH.dbd.CH, Se, Te or N--R.sup.10 ;Y represents O, S, or N--R.sup.9 ;Z represents O, S or Se;R.sup.9 represents alkyl of 1-6 carbons; or an aryl of 6-24 carbons;R.sup.Type: GrantFiled: March 7, 1996Date of Patent: December 24, 1996Assignee: Sterling Diagnostic Imaging, Inc.Inventors: Dietrich M. Fabricius, Ralf H. Harms, James J. Welter
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Patent number: 5587393Abstract: The invention relates to benzimidazoles of general formula ##STR1## wherein R.sub.1 to R.sub.4 are as defined herein, the 1-, 3-isomer mixtures thereof and the addition salts thereof. The new compounds are useful, in particular, as angiotensin antagonists.Type: GrantFiled: September 1, 1994Date of Patent: December 24, 1996Assignee: Dr. Karl Thomae GmbHInventors: Berthold Narr, Norbert Hauel, Jacques Van Meel, Wolfgang Wienen, Michael Entzeroth, Uwe Ries
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Patent number: 5585247Abstract: The invention relates to fluorogenic compounds for the detection of hydrolyzing enzymes and the use of the fluorogenic compounds.Type: GrantFiled: May 21, 1990Date of Patent: December 17, 1996Assignee: Behringwerke AktiengesellschaftInventor: Klaus Habenstein
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Patent number: 5580888Abstract: Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR.sup.1, wherein R.sup.1 is an optionally substituted alkyl group; X is --O--, --S-- or --N(R.sup.6)--, where R.sup.6 is a hydrogen atom or an alkyl group; R.sup.2 is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R.sup.3 and R.sup.4, which may be the same or different, is each a group --(CH.sup.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms and n is zero or an integer 1, 2 or 3; R.sup.5 is a hydrogen atom or an optionally substituted alkyl group; and the salts, solvates, hydrates and N-oxides. Compounds according to the invention are potent, selective and orally active PDE IV inhibitors and are useful in the prophylaxis and treatment of asthma.Type: GrantFiled: June 5, 1995Date of Patent: December 3, 1996Assignee: Celltech Therapeutics LimitedInventors: Graham J. Warrellow, Ewan C. Boyd, Rikki P. Alexander
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Patent number: 5576432Abstract: A process of preparing a dihydropyrimidine compound of the structure (I): ##STR1## wherein R.sup.1 and R.sup.2 are bonded together to form an aromatic or heterocyclic ring, which may be substituted or unsubstituted, or are individually selected from the group consisting of hydrogen, or a substituted or unsubstituted aliphatic, carbocyclic, or heterocyclic group;R.sup.3, R.sup.4 and R.sup.5 are individually selected from the group consisting of hydrogen or a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; andX represents the atoms necessary to form a 5 or 6 membered heterocyclic ring, and is selected from the group consisting of oxygen, sulfur, selenium, ##STR2## wherein R.sup.6, R.sup.7, and R.sup.8 are individually selected from the group consisting of a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; comprising combining a compound (A) of the structure: ##STR3## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.Type: GrantFiled: December 23, 1994Date of Patent: November 19, 1996Assignee: Eastman Kodak CompanyInventors: Roger Lok, Antony J. Williams
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Patent number: 5576343Abstract: An anticoagulant agent which comprises, as an active ingredient, an aromatic amidine derivative represented by the following general formula (1) or a salt thereof: ##STR1## wherein the group represented by ##STR2## is a group selected from indolyl, benzofuranyl, benzothienyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, naphthyl, tetrahydronaphthyl and indanyl; X is a single bond, an oxygen atom, a sulfur atom or a carbonyl group; and Y is a saturated or unsaturated 5- or 6-membered heterocyclic moiety or cyclic hydrocarbon moiety optionally having a substituent group, an amino group optionally having a substituent group or an aminoalkyl group optionally having a substituent group.The inventive compound has a high anticoagulant capacity based on its excellent FXa inhibition activity.Type: GrantFiled: June 6, 1995Date of Patent: November 19, 1996Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Takayasu Nagahara, Naoaki Kanaya, Kazue Inamura, Yukio Yokoyama
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Patent number: 5569655Abstract: Substitutued heterocyclylisoquinolinium salts, pharmaceutical compositions containing them and methods for the treatment or prevention of neurodegenerative disorders or neurotoxic injuries utilizing them.Type: GrantFiled: July 29, 1994Date of Patent: October 29, 1996Assignee: Sterling Winthrop Inc.Inventors: John A. Dority, Jr., William G. Earley, Virendra Kumar, John P. Mallamo, Matthew S. Miller, Chakrapani Subramanyam
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Patent number: 5554633Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.Type: GrantFiled: January 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme, Ltd.Inventor: Martin R. Teall
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Patent number: 5554627Abstract: Compounds of formula (I), wherein Q.sup.1 represents an aryl group; the dotted line represents an optional covalent bond; one of X and Y represents H and the other represents hydroxy or C.sub.1-6 alkoxy, or X and Y together form a group .dbd.O or .dbd.NOR.sup.5 where R.sup.5 is H or C.sub.1-6 alkyl; Z represents O, S or NR.sup.2, where R.sup.2 is H or C.sub.1-6 alkyl; W represents a bond or a saturated or unsaturated hydrocarbon chain of 1, 2, 3, 4, 5 or 6 carbon atoms; R.sup.1 represents H or C.sub.1-6 alkyl. R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; R.sup.4 represents an optionally substituted phenyl group; and R.sup.6 represents a specified amino group or an optionally substituted aromatic or non-aromatic azacyclic or azabicyclic group; and salts and prodrugs are tachykinin receptor antagonists.Type: GrantFiled: April 27, 1995Date of Patent: September 10, 1996Assignee: Merck, Sharp & Dohme Ltd.Inventors: Richard T. Lewis, Angus M. MacLeod, Kevin J. Merchant
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Patent number: 5552422Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.Type: GrantFiled: January 11, 1995Date of Patent: September 3, 1996Assignee: Merck Frosst Canada, Inc.Inventors: Jacques Y. Gauthier, Cheuk K. Lau, Yves LeBlanc, Chun-Sing Li, Patrick Roy, Michel Therien, Zhaoyin Wang
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Patent number: 5541199Abstract: Compounds of the formula: ##STR1## in which n is one of the integers 1, 2, 3,or 4; m is one of the integers 0 or 1; R is ##STR2## or a pharmaceutically acceptable salt thereof, are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.Type: GrantFiled: June 2, 1995Date of Patent: July 30, 1996Assignee: American Home Products CorporationInventor: Richard E. Mewshaw
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Patent number: 5529998Abstract: The invention relates to benzoxazolyl- and benzothiazolyloxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.Type: GrantFiled: July 27, 1995Date of Patent: June 25, 1996Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Bernd Riedl, Martin Ruppelt, Andreas Stolle, Hanno Wild, Rainer Endermann, Klaus D. Bremm, Hein-Peter Kroll, Harald Labischinski, Klaus Schaller, Hans-Otto Werling
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Patent number: 5530117Abstract: The disclosure is drawn to novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds. These compounds are useful to treat infections caused by a wide spectrum of bacterial organisms, including those which are resistant to tetracycline.Type: GrantFiled: May 31, 1995Date of Patent: June 25, 1996Assignee: American Cyanamid CompanyInventors: Joseph J. Hlavka, Phaik-Eng Sum, Yakov Gluzman, Ving J. Lee, Adma A. Ross
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Patent number: 5527914Abstract: Methine compounds are described, which can be represented by general formula [Ic]: ##STR1##Type: GrantFiled: May 3, 1994Date of Patent: June 18, 1996Assignee: Fuji Photo Film Co., Ltd.Inventors: Takanori Hioki, Tadashi Ikeda
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Patent number: 5525436Abstract: The subject invention relates to solid polymer electrolyte membranes comprising proton conducting polymers stable at temperatures in excess of 100.degree. C., the polymer being basic polymer complexed with a strong acid or an acid polymer. The invention further relates to the use of such membranes in electrolytic cells and acid fuel cells. Particularly, the invention relates to the use of polybenzimidazole as a suitable polymer electrolyte membrane.Type: GrantFiled: November 1, 1994Date of Patent: June 11, 1996Assignee: Case Western Reserve UniversityInventors: Robert F. Savinell, Morton H. Litt
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Patent number: 5523312Abstract: Disclosed herein are compounds and pharmaceutical compositions useful for combating picornaviruses and preventing or treating picornaviral infections. The compounds have the formula: ##STR1## wherein Het.sub.1 is chosen from the group consisting of oxazolyl, isoxazolyl, oxadiazolyl;Y is an alkylene bridge of 3 to 9 carbon atoms;Het.sub.2 is benzofuranyl or indolyl;R.sub.1 and R.sub.2 are each independently chosen from hydrogen, halo, acetyl, alkyl, alkenyl, amino, alkylthio, hydroxy, hydroxyalkyl, alkoxyalkyl, alkylthioalkyl, alkylsulfinyl alkyl, alkylsulfonylalkyl, alkoxy, nitro, carboxy, alkoxycarbonyl, dialkylaminoalkyl, alkylaminoalkyl, aminoalkyl, difluoromethyl, trifluromethyl, or cyano; andR.sub.3 is oxazolyl, oxadiazolyl, isoxazolyl or any of these substituted with alkyl, halo, alkoxyalkyl, cycloalkyl, haloalkyl, hydroxyalkyl, alkoxy, hydroxy, furyl, thienyl, or fluoroalkyl;the N-oxide thereof or a pharmaceutically acceptable acid addition salt thereof.Type: GrantFiled: September 27, 1994Date of Patent: June 4, 1996Assignee: Sterling Winthrop Inc.Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Gee-Hong Kuo, Theodore J. Nitz, Michael Reuman
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Patent number: 5518713Abstract: Benzoxazole derivatives having the following formula (I): ##STR1## wherein the groups are hereinafter defined are disclosed together with the use thereof as sunscreen agents and cosmetic compositions containing them.Type: GrantFiled: February 13, 1995Date of Patent: May 21, 1996Assignee: 3V Inc.Inventor: Giuseppe Raspanti
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Patent number: 5516782Abstract: The meso-azacyclic aromatic acid amides and esters of the present invention are useful in the treatment of the central nervous system and gastrointestinal motility disorders such as gastroesophageal reflux, non-ulcer dyspepsia, delayed gastric emptying, ileus, irritable bowel syndrome, and the like. Additionally, the compounds of the present invention find utility as antagonists of serotonin 5-HT.sub.3 receptors. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, irritable bowel syndrome, emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.Type: GrantFiled: May 18, 1995Date of Patent: May 14, 1996Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moorman, Roger Nosal, Clara I. Villamil
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Patent number: 5514679Abstract: Compounds of the formula ##STR1## wherein: R.sub.1 and R.sub.2 are independently hydrogen, halo, alkyl, alkenyl, alkoxy, hydroxy, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, alkylthioalkynyl, hydroxyalkoxy, alkylthioalkyl, alkylsulfinylalkyl, alkylsulfonylalkyl, amino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy or cyanomethyl, nitro, difluoromethyl, trifluoromethyl or cyano;Y is alkylene of 3 to 9 carbon atoms;R.sub.3 and R.sub.4 are independently hydrogen, alkyl, alkoxy, hydroxy, cycloalkyl, hydroxyalkyl, hydroxyhaloalkyl, alkoxyalkyl, hydroxyalkoxy, alkylthioalkyl, alkanoyl, alkanoyloxy, alkylsulfinylalkyl, alkylsulfonylalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxycarbonyl, carboxy, cyanomethyl, fluoroalkyl, cyano, phenyl, alkynyl, alkene, or halo;R.sub.5 is alkoxycarbonyl, alkyltetrazolyl, phenyl or a heterocycle;or a pharmaceutically acceptable acid addition salts thereof; N-oxides thereof, are useful as antipirconaviral agents.Type: GrantFiled: May 13, 1994Date of Patent: May 7, 1996Assignee: Sterling Winthrop Inc.Inventors: David J. Aldous, Thomas R. Bailey, Guy D. Diana, Theodore J. Nitz
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Patent number: 5502201Abstract: The title compounds of the formula ##STR1## in which R.sup.1 and R.sup.2, independently of one another, represent hydrogen, straight-chain or branched C.sub.1 -C.sub.4 -alkyl, straight-chain or branched C.sub.1 -C.sub.4 -alkoxy, nitro, fluorine, chlorine, bromine, SO.sub.2 Cl, cyano or SO.sub.2 -C.sub.1 -C.sub.4 -alkyl, andX represents sulphur or oxygen,can be prepared from the corresponding 2-mercapto-benzothiazoles or 2-mercapto-benzoxazoles by chlorination with thionyl chloride in the presence of phosphorous acid compounds of the formulaYP(OR.sup.5).sub.2 (III),in whichR.sup.5 represents hydrogen, straight-chain or branched, substituted or unsubstituted C.sub.1 -C.sub.12 -alkyl, phenyl or C.sub.7 -C.sub.10 -aralkyl andY represents hydrogen or OR.sup.5.Type: GrantFiled: April 20, 1994Date of Patent: March 26, 1996Assignee: Bayer AktiengesellschaftInventor: Volker Ka/ ss
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Patent number: 5502204Abstract: A process for the preparation of a 1-substituted-5(4H)-tetrazolinone of the formula ##STR1## wherein R.sub.1 is defined in the specificationn is 0, 1, 2, 3 or 4,which comprises reacting a 1-substituted-5(4H)-tetrazolinethione of the formula ##STR2## with an ethylene oxide of the formula ##STR3## wherein R.sup.2 represents hydrogen, methyl or ethyl,in the presence of a base and in the presence of water, an alcohol or a mixture thereof.Type: GrantFiled: September 7, 1994Date of Patent: March 26, 1996Assignee: Nihon Bayer Agrochem K.K.Inventors: Akihiko Yanagi, Yukiyoshi Watanabe, Shin-ichi Narabu
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Patent number: 5498621Abstract: Compounds of the formulae ##STR1## where R is cycloalkyl or aryl; R.sub.1 is alkyl, X is O or C.dbd.O; A is O or S; and B is N or CH are useful as hypoglycemic agents.Type: GrantFiled: August 12, 1994Date of Patent: March 12, 1996Assignee: Pfizer Inc.Inventors: Robert L. Dow, Bernard Hulin, David A. Clark
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Patent number: 5496948Abstract: Intermediates of structural formula ##STR1## can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.Type: GrantFiled: June 21, 1995Date of Patent: March 5, 1996Assignee: Merck & Co., Inc.Inventors: David Askin, Kan K. Eng, Ralph P. Volante
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Patent number: 5496853Abstract: Pharmaceutical compositions containing a benzoxazole compound and a 2,3-dihydrobenzofuran compound represented by the following formula (I) and its pharmaceutically acceptable salt: ##STR1## In the formula, any one of P, Q, R and S is a group represented by the formula: ##STR2## and R.sub.1, R.sub.2 and the reining three substituents out of the substituents P to S each independently stand for various substituents. These compositions are used as an ATCAT inhibitor or for treating hyperlipidemia and atherosclerosis.Type: GrantFiled: April 26, 1995Date of Patent: March 5, 1996Assignee: Teijin LimitedInventors: Tatsuki Shiota, Takumi Takeyasu, Kenichiro Kataoka, Tsutomu Mochizuki, Hirofumi Tanabe, Mikio Ota, Masatoshi Kano, Hisao Yamaguchi
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Patent number: 5492925Abstract: There are provided thienyl- and furylpyrrole compounds of formula I ##STR1## and their use for the control of insects and acarina. Further provided are compositions and methods comprising those compounds for the protection of plants from attack by insects and acarina.Type: GrantFiled: August 31, 1993Date of Patent: February 20, 1996Assignee: American Cyanamid CompanyInventors: Roger W. Addor, Joseph A. Furch, III, Laurelee A. Duncan, Jack K. Siddens, deceased
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Patent number: 5493011Abstract: Water-insoluble azo colorants, their preparation and use The invention relates to monoazo and disazo compounds of the formula (I) ##STR1## in which D is the radical of a carbocyclic or heterocyclic diazo or bisdiazo component, R.sup.1 and R.sup.2, independently of one another, are each a substituted or unsubstituted aryl or heteroaryl radical, X.sup.1 and X.sup.2, independently of one another, are each ring-forming ether oxygen or a substituted or unsubstituted imide grouping and n has the value 0 or 1, in which rings A and B, independently of one another, can each be additionally substituted and/or carry substituted or unsubstituted fused rings.These new compounds of the formula (I) are obtained by coupling diazotized amines or diamines of the type D--NH.sub.2 or H.sub.2 N--D--NH.sub.2 with (benzoxazol-2-yl)- or (benzimidazol-2-yl)-arylacetamides.Depending on the presence and length of alkyl chains, the compounds of the formula (I) are suitable for use as pigments, disperse dyes or oil-soluble dyes.Type: GrantFiled: November 6, 1992Date of Patent: February 20, 1996Assignee: Hoechst AGInventors: Rudiger Jung, Reinhold Deubel
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Patent number: 5489603Abstract: An insecticidal composition containing a guanidine derivative of the formula: ##STR1## wherein R.sup.1 is an optionally substituted homocyclic or heterocyclic group, n is 0 or 1, R.sup.2 is a hydrogen atom or an optionally substituted hydrocarbon group, R.sup.3 is a primary, secondary or tertiary amino group, X is an electron attractive group such as nitro or trifluoroacetyl group, provided that when n is 0, R.sup.1 is an optionally substituted heterocyclic group or a salt thereof.Type: GrantFiled: July 15, 1993Date of Patent: February 6, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideki Uneme, Koichi Iwanaga, Noriko Higuchi, Isao Minamida, Tetsuo Okauchi
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Patent number: 5489570Abstract: The invention relates to isoxazole derivatives of formula (I): ##STR1## wherein: Ar represents phenyl optionally substituted by from one to three groups and wherein two substituents on adjacent positions of the phenyl ring, together with the two atoms to which they are attached, form a 5- to 7-membered ring which is optionally substituted;R represents the hydrogen atom or a group --CO.sub.2 R.sup.3 ;R.sup.1 represents alkyl, haloalkyl or optionally substituted cycloalkyl;R.sup.3 represents alkyl, alkenyl or alkynyl containing up to six carbon atoms which is optionally substituted by one or more halogen atoms;and their use as herbicides.Type: GrantFiled: July 29, 1994Date of Patent: February 6, 1996Assignee: Rhone-Poulenc Agriculture LimitedInventors: Neil Geach, David W. Hawkins, Christopher J. Pearson, Philip H. G. Smith, Nicolas White
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Patent number: 5486616Abstract: A method for detecting a component of an aqueous liquid comprising adding to the liquid a luminescent dye selected from the group consisting of cyanine, merocyanine and styryl dyes containing at least one sulfonic acid or sulfonate group attached to an aromatic nucleus and reacting the dye with the component. The labeled component is then detected by an optical detection method.Type: GrantFiled: November 29, 1993Date of Patent: January 23, 1996Assignee: Carnegie Mellon UniversityInventors: Alan S. Waggoner, Lauren A. Ernst, Ratnakar B. Mujumdar
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Patent number: 5482942Abstract: This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.Type: GrantFiled: June 28, 1994Date of Patent: January 9, 1996Assignee: American Home Products CorporationInventors: Richard M. Soll, Paul J. Dollings
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Patent number: 5482962Abstract: This invention relates to N,N'-disubstituted-N,N'-diacylhydrazines which are useful as insecticides, compositions containing those compounds and methods of their use. This invention also relates to the production of intermediates useful in the production of such compounds.The compounds of this invention may be represented by the formula ##STR1## wherein R.sup.1 is cyano or H,R.sup.2 is branched alkyl,B is aryl or substituted aryl,R.sup.a is H or a variety of substituents, andZ forms a fused 5-member heterocyclic ring.Type: GrantFiled: July 22, 1994Date of Patent: January 9, 1996Assignee: Rohm and Haas CompanyInventor: Robert E. Hormann
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Patent number: 5476935Abstract: Dye-donor element for use according to thermal dye transfer comprising least one dye corresponding to the general formula (I): ##STR1## wherein Z is --CN, --COOR.sup.1 or --CONR.sup.2 R.sup.3 ; R.sup.1 is --H, (cyclo)alkyl, or aryl; R.sup.2 and R.sup.3 is --H, (cyclo)alkyl, aryl, or R.sup.2 and R.sup.3 together represent the atoms necessary to complete a heterocyclic nucleus; R.sup.4 and R.sup.5 is --H, (cyclo)alkyl, aryl, a heterocyclic ring, SO.sub.2 R.sup.8, COR.sup.8, CSR.sup.8, POR.sup.8 R.sup.9, OR.sup.6, NR.sup.6 R.sup.7, SR.sup.6, or R.sup.4 and R.sup.5 together represent the atoms necessary to complete a aliphatic ring, a heterocyclic ring including a heterocyclic ring carrying a fused-on aliphatic or aromatic ring; R.sup.6 and R.sup.7 is (cyclo)alkyl, aryl, alkenyl, aralkyl, aryl, a heterocyclic group, or R.sup.6 and R.sup.7 together represent the atoms necessary to complete a 5- or 6-membered ring; R.sup.8 and R.sup.Type: GrantFiled: May 18, 1994Date of Patent: December 19, 1995Assignee: Agfa-Gevert, N.V.Inventors: Luc Vanmaele, Hans Junek, Renate Dworczak
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1,2-ethanediol derivative and salt thereof and cerebral function-improving agent comprising the same
Patent number: 5472984Abstract: This invention relates to a 1,2-ethanediol derivative and a salt thereof, a process for producing the same, and a cerebral function-improving agent comprising the same. The cerebral function-improving agent of this invention is useful for treating cerebrovascular dementia, senile dementia, Alzheimer's dementia, sequelae of ischemic encephalopathy and cerebral apoplexy.Type: GrantFiled: December 29, 1993Date of Patent: December 5, 1995Assignee: Toyama Chemical Co., Ltd.Inventors: Satoshi Ono, Tetsuo Yamafuji, Hisaaki Chaki, Mutsuko Maekawa, Yozo Todo, Hirokazu Narita -
Patent number: 5466813Abstract: Imine dyes useful in photographic materials have the formula ##STR1## wherein R.sup.1, E.sup.1, E.sup.2, L.sup.1, L.sup.2, L.sup.3,D and m are defined as in the specification.Solid particle dispersions of dyes of formula (I) that contain at least one base-ionizable functional group such as carboxy, sulfonamido, or sulfamoyl are useful as filter dyes in photographic elements.Type: GrantFiled: July 20, 1993Date of Patent: November 14, 1995Assignee: Eastman Kodak CompanyInventors: Donald R. Diehl, Margaret J. Helber, Hugh Williamson
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Patent number: 5462953Abstract: The invention concerns a bicyclic heterocyclic derivative of the formula I ##STR1## wherein Q is an optionally substituted 9-membered bicyclic heterocyclic moiety containing 1 or 2 N's and optionally a further N, O or S heteroatom;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is optionally substituted phenylene or pyridylene;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: July 15, 1994Date of Patent: October 31, 1995Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Pierre A. R. Bruneau, Graham C. Crawley, Keith Oldham
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Patent number: 5462694Abstract: A mesomorphic compound of the formula (I) according to claim 1 characterized by having at least one cyclic group selected from .beta. class including, e.g., thiazole-2,5-diyl, benzoxazole-2,5-diyl, indan-2,5-diyl, and quinoxaline-2,6-diyl and also having a linkage of Y.sup.1 (CH.sub.2).sub.m Y.sup.2, where Y.sup.1 and Y.sup.2 are --CH.sub.2 --, --O--, --COO-- or --OCO-- and m is 1-16, is suitable as a component for a liquid crystal composition providing improved response characteristics. A liquid crystal device is constituted by disposing the liquid crystal composition between a pair of substrates. The liquid crystal device is used as a display panel constituting a liquid crystal apparatus providing good display characteristics.Type: GrantFiled: August 30, 1994Date of Patent: October 31, 1995Assignee: Canon Kabushiki KaishaInventors: Yoko Kosaka, Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Shinichi Nakamura, Ikuo Nakazawa