Quinuclidines (including Unsaturation) Patents (Class 514/305)
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Patent number: 5837711Abstract: Certain novel substituted quinuclidine compounds having the ability to antagonize substance P and having the following formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 are each, independently, thienyl, phenyl, fluorophenyl, chlorophenyl or bromophenyl;X is --CONR.sup.3 R.sup.4, --CO.sub.2 R.sup.3, --CH.sub.2 OR.sup.3, --CH.sub.2 NR.sup.3 R.sup.4 or --CONR.sup.3 OR.sup.4 ;R.sup.1, R.sup.3 and R.sup.4 are each, independently, hydrogen or alkyl having 1 to 4 carbon atoms;R.sup.Type: GrantFiled: April 28, 1995Date of Patent: November 17, 1998Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Toshihide Kokura, Masami Nakane, Kunio Satake, Hiroaki Wakabayashi
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Patent number: 5834499Abstract: A 5-HT.sub.3 receptor against containing a thiazole derivative as the effective ingredient is provided and is represented by the Formula (I): ##STR1## wherein the A ring is substituted or unsubstituted and represents a benzene or a heterocyclic ring with one or two heteroatoms;one of L.sub.1 or L.sub.Type: GrantFiled: August 26, 1996Date of Patent: November 10, 1998Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kiyoshi Iwaoka, Hideki Anan, Naoki Imanishi, Kenichi Kazuta, Hiroyuki Koshio, Takeshi Suzuki, Hirotsune Itahana, Hiroyuki Ito, Keiji Miyata, Mitsuaki Ohta
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Patent number: 5830902Abstract: A quinuclidine derivative represented by the following general formula (I), a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, which has strong squalene synthase inhibiting activity and is useful as a cholesterol lowering agent without causing side effects. ##STR1## (Symbols in the formula represent the following meanings; R.sub.1 : a hydrogen atom, a halogen atom or a lower alkyl group,R.sub.2 : a hydrogen atom, a hydroxyl group or a lower alkoxy group,. . : a single bond or a double bond, with the proviso thatR.sub.2 does not exist when . . . is a double bond,X and Y: the same or different from each other and each represents a bond, an oxygen atom (--O--), a carbonyl group (--CO--), a group represented by the formula --S(O).sub.p -- or a group represented by the formula --NR.sub.3 --,p: 0, 1 or 2,R.sub.3 : a hydrogen atom or a lower alkyl group which may have a substituent,A: a saturated or unsaturated lower alkylene group, a group of the formula --(CH.sub.2).sub.m Z(CH.sub.Type: GrantFiled: August 21, 1997Date of Patent: November 3, 1998Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Masahiko Isaka, Tsukasa Ishihara, Koyo Matsuda, Hirotoshi Kakuta, Hiroshi Moritani
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Patent number: 5824650Abstract: The invention relates to a therapeutic composition for topical application containing at least one product with an irritant side effect and a substance P antagonist for reducing or even eliminating the irritant effect of this product.It also relates to the use of a substance P antagonist for the preparation of a pharmaceutical composition for topical application containing at least one product with an irritant side effect for reducing or even eliminating the irritant effect of this product.The substance P antagonist may be a peptide compound or a nitrogen-containing compound or a nitrogen-, sulphur- or oxygen-containing heterocyclic compound.Type: GrantFiled: December 19, 1995Date of Patent: October 20, 1998Assignee: L'OrealInventors: Olivier De Lacharriere, Lionel Breton
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Patent number: 5807867Abstract: Compounds of the formula ##STR1## wherein R.sup.1 is methoxy and R.sup.2 is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl; and the pharmaceutically acceptable salts of such compounds.These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.Type: GrantFiled: May 23, 1994Date of Patent: September 15, 1998Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Hiroshi Kondo, Masami Nakane, Kaoru Shimada, John Adams Lowe, III, Terry Jay Rosen
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Patent number: 5792777Abstract: Biphenylylquinuclidine compounds of the formula I: ##STR1## and pharmaceutically-acceptable salts thereof; wherein R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen; or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 -CR.sup.2 is a double bond; and one or both ring A and ring B may be optionally unsubstituted or independently substituted by one or more substituents selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, (1-6C)alkyl, (1-6C)alkoxy, (1-6C)alkylamino, di-?(1-6C)alkyl!amino, N-?(1-6C)alkyl!carbamoyl, N,N-di-?(1-6C)alkyl!carbamoyl, (1-6C)alkoxycarbonyl, (1-6C)alkylthio, (1-6C)alkylsulphinyl, (1-6C)alkylsulphonyl and halogeno-(1-6C)alkyl; are inhibitors of squalene synthase and are hence useful in treating diseases or medical conditions such as hypercholesterolemia, atherosclerosis and fungal diseases.Type: GrantFiled: June 30, 1993Date of Patent: August 11, 1998Assignee: Zeneca LimitedInventors: George Robert Brown, Peter John Harrison, deceased, Keith Blakeney Mallion
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Patent number: 5780466Abstract: The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycle.Type: GrantFiled: August 27, 1996Date of Patent: July 14, 1998Assignee: SanofiInventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck, Joelle Taillades
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Patent number: 5776981Abstract: A method of systemically controlling endoparasites and ectoparasites of warm-blooded animals by orally or percutaneously administering to the animal a parasiticidally effective amount of an acyl urea compound.Type: GrantFiled: April 21, 1995Date of Patent: July 7, 1998Assignee: Novartis CorporationInventors: Michael Fred Potter, George Lorton Rotramel, Andrew James Caruso, David Teh-Wei Chou, Paul Alfred Cain
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Patent number: 5773458Abstract: The compound of the formula: ##STR1## where R is H, alkyl, haloalkyl, cycloalkyl, alkenyl or alkynyl; Y is oxygen, sulfur or NR.sub.2 where R.sub.2 is H or alkyl; or a pharmaceutically acceptable salt thereof, are centrally active muscarinic agents.Type: GrantFiled: October 17, 1997Date of Patent: June 30, 1998Assignee: American Home Products CorporationInventors: Annmarie L. Sabb, Reinhardt P. Stein
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Patent number: 5770608Abstract: Quinuclidine compounds of the formula I: ##STR1## R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen;or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 --CR.sup.2 is a double bond;X is selected from --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 NH--, --NHCH.sub.2 --, --CH.sub.2 CO--, --COCH.sub.2 --, --CH.dbd.N--, --N.dbd.CH--, --CH.sub.2 S--, --SCH.sub.Type: GrantFiled: February 24, 1997Date of Patent: June 23, 1998Assignee: Imperial Chemical Industries PLCInventors: George Robert Brown, Keith Blakeney Mallion, Peter John Harrison, deceased
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Patent number: 5763457Abstract: The present invention relates a method for treating anxiety using azacyclic and azabicyclic oxadiazole compounds.Type: GrantFiled: October 22, 1996Date of Patent: June 9, 1998Assignee: Eli Lilly and CompanyInventors: Neil C. Bodick, Franklin P. Bymaster, Walter W. Offen, Harlan E. Shannon
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Patent number: 5756514Abstract: Methods of treating and preventing drug-induced pruritus in patients by administration of a serotonin type 3 antagonist are provided.Type: GrantFiled: December 30, 1996Date of Patent: May 26, 1998Inventor: Ghassem E. Larijani
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Patent number: 5750538Abstract: The present invention relates to a novel method for treating a mammal suffering from hypercholesterolemia and related disorders.Type: GrantFiled: January 3, 1997Date of Patent: May 12, 1998Assignee: Novo Nordisk A/SInventors: Per Sauerberg, Kristian Tage Hansen
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Combinational therapeutic methods employing nitric oxide scavengers and compositions useful therefor
Patent number: 5747532Abstract: In accordance with the present invention, there are provided combinational therapeutic methods for the in vivo inactivation or inhibition of formation (either directly or indirectly) of species which induce the expression of nitric oxide synthase, as well as reducing nitric oxide levels produced as a result of .NO synthase expression. In contrast to the inhibitory approach described in the prior art (i.e., wherein the function of the enzymes responsible for nitric oxide production is inhibited), the present invention employs a combination of inactivation (or inhibition) and scavenging approach whereby the stimulus of nitric oxide synthase expression is inactivated, or the production thereof is inhibited, and overproduced nitric oxide is bound in vivo to a suitable nitric oxide scavenger. The resulting complexes render the stimulus of nitric oxide synthase expression inactive (or inhibit the production thereof), and nitric oxide harmless.Type: GrantFiled: November 21, 1995Date of Patent: May 5, 1998Assignee: Medinox, Inc.Inventor: Ching-San Lai -
Patent number: 5744480Abstract: The present invention relates to novel fluoroalkoxybenzylamino derivatives of nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula ##STR1## wherein Q, X.sup.1, X.sup.2 and X.sup.3 are as defined below. These novel compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders.Type: GrantFiled: May 22, 1995Date of Patent: April 28, 1998Assignee: Pfizer Inc.Inventors: John Adams Lowe, III, Terry Jay Rosen
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Patent number: 5741819Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds of structure: ##STR1## or pharmaceutically acceptable salts thereof; whereinR.sup.1 is alkyl, substituted alkyl, cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; R.sup.2 is one of hydrogen, alkyl, cycloalkyl or aryl; R.sup.3 is one of hydrogen, hydroxy or alkoxy; R.sup.4 is one of --NH.sub.2, phenyl or pyridyl, wherein said phenyl and said pyridyl are optionally substituted with one or two of halogen, hydroxy, hydroxyalkyl, alkoxy, amino, monoalkylamino, dialkylamino, aminoalkyl, monoalkylaminoalkyl and/or dialkylaminoalkyl; X is one of --CH.sub.2 -- or --C(O)--; and n is from zero to eleven; provided that when R.sup.4 is --NH.sub.2, then R.sup.3 is hydrogen and n is other than zero; and also provided that when R.sup.Type: GrantFiled: June 7, 1995Date of Patent: April 21, 1998Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Carl R. Illig, Richard M. Soll, Joseph M. Salvino, Bruce E. Tomczuk, Tianbao Lu, Nalin L. Subasinghe
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Patent number: 5741797Abstract: Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of the formula I and the pharmaceutically-acceptable salts thereof; ##STR1## wherein R is C.sub.1 -C.sub.6 alkyl; X is C.sub.1 -C.sub.6 alkyl having one or more substituents which include at least one heteroatom; Ar.sup.1 and Ar.sup.2 are each, independently, aryl optionally substituted by one C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, halogen, cyano, nitro, phenoxy, mono C.sub.1 -C.sub.6 alkylamino, di C.sub.1 -C.sub.6 alkylamino, halosubstituted C.sub.1 -C.sub.6 alkyl, or halosubstituted C.sub.1 -C.sub.6 alkoxy; Y is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, Z--(CH.sub.2).sub.p --, or W--(CH.sub.2).sub.m --CHR.sup.2 --(CH.sub.2).sub.n --NR.sup.1 CO-- wherein Y is at the 4-, 5- or 6-position on the quinuclidine ring; R.sup.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, benzyl or --(CH.sub.2).sub.r --W; R.sup.Type: GrantFiled: November 20, 1995Date of Patent: April 21, 1998Assignee: PFizer Inc.Inventor: Kunio Satake
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Patent number: 5731323Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts in which R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen; or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 --CR.sup.2 is a double bond; X is selected from --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.ident.C--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 NH--, --NHCH.sub.2 --, --CH.sub.2 CO--, --COCH.sub.2 --, --N.dbd.CH--, --CH.dbd.N--, --CH.sub.2 S-- and --SCH.sub.Type: GrantFiled: June 5, 1995Date of Patent: March 24, 1998Assignee: Zeneca LimitedInventor: Paul Robert Owen Whittamore
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Patent number: 5716961Abstract: A method of treating tinnitus in a mammal in need of such treatment, in which the method comprises administering a therapeutically effective amount of a compound of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 -R.sup.6 are as defined herein.Type: GrantFiled: September 9, 1996Date of Patent: February 10, 1998Assignee: Pfizer Inc.Inventor: Steven B. Sands
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Patent number: 5716965Abstract: Compounds of the formula ##STR1## wherein W, Ar.sup.1, Ar.sup.2 and Ar.sup.3 are defined as below; and the pharmaceutically acceptable salts of such compounds.These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.Type: GrantFiled: December 20, 1993Date of Patent: February 10, 1998Assignee: Pfizer Inc.Inventors: Fumitaka Ito, Toshihide Kokura, Masami Nakane, Kunio Satake, Hiroaki Wakabayashi
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Patent number: 5714496Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts in which R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen; or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 -CR.sup.2 is a double bond; X is selected from --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 O--, --CH.sub.2 NH--, --NHCH.sub.2 --, --CH.sub.2 CO--, --COCH.sub.2 --, --CH.sub.2 S-- and --SCH.sub.2 --; Ar.sup.1 is a phenylene moiety; Ar.sup.2 is a heteroaryl moiety; and wherein one or both of Ar.sup.1 and Ar.sup.2 may optionally bear one or more substituents independently selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, di-alkylamino, N-alkylcarbamoyl, di-N,N-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, halogeno-alkyl, carboxyalkyl and alkanoylamino; provided that when R.sup.1 is hydroxy, X is not selected from --NHCH.sub.2 -- and --SCH.sub.Type: GrantFiled: February 28, 1995Date of Patent: February 3, 1998Assignee: Zeneca LimitedInventors: George Robert Brown, Keith Blakeney Mallion, Paul Robert Owen Whittamore, David Robert Brittain
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Patent number: 5712271Abstract: The present invention relates to a novel method for treating a mammal suffering from urinary bladder dysfunctions.Type: GrantFiled: October 3, 1996Date of Patent: January 27, 1998Inventors: Mark A. Muhlhauser, Harlan E. Shannon, Karl B. Thor
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Patent number: 5712287Abstract: The present invention relates to a novel method for treating a mammal suffering from urinary bladder dysfunctions.Type: GrantFiled: October 3, 1996Date of Patent: January 27, 1998Inventors: Mark A. Muhlhauser, Harlan E. Shannon, Karl B. Thor
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Patent number: 5712288Abstract: The invention relates to quaternary basic amides of the formula ##STR1## in which Ar is an optionally substituted mono-, di- or tri-cyclic aromatic or heteroaromatic group;T is a direct bond, a hydroxymethylene group, an alkoxymethylene group in which the alkoxy group is C.sub.1 -C.sub.4, or a C.sub.1 -C.sub.5 -alkylene group;Ar' is an unsubstituted or mono- or poly-substituted phenyl, a thienyl, a benzothienyl, a naphthyl or an indolyl;R is hydrogen or a C.sub.1 -C.sub.4 -alkyl, or a C.sub.1 -C.sub.4 -.omega.-alkoxy(C.sub.2 -C.sub.4)alkyl, or a C.sub.2 -C.sub.4 -.omega.-alkanoyloxy (C.sub.1 -C.sub.4)alkyl;Q is hydrogen;or else Q and R together form a 1,2-ethylene, 1,3-propylene or 1,4-butylene group;Am.sup..sym. is the radical ##STR2## in which X.sub.1, X.sub.2 and X.sub.3, together with the nitrogen atom to which they are bonded, form a 1-azoniabicyclo?2.2.2!octane optionally substituted by a phenyl or benzyl group; andA.sup..crclbar. is a pharmaceutically acceptable anion.Type: GrantFiled: October 18, 1996Date of Patent: January 27, 1998Assignee: SanofiInventors: Xavier Emonds-Alt, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5710151Abstract: The present invention relates to a novel method for treating a mammal suffering from urinary bladder dysfunctions.Type: GrantFiled: October 3, 1996Date of Patent: January 20, 1998Inventors: Mark A. Muhlhauser, Harlan E. Shannon, Karl B. Thor
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Patent number: 5707985Abstract: There are disclosed novel substituted naphthyl-, quinolyl- and isoquinolyl- sulfonamide derivatives that are useful in a method of treating immuno-inflammatory diseases in a mammalian patient suffering therefrom. Pharmaceutical compositions containing the sulfonamide compounds are also provided.Type: GrantFiled: June 7, 1995Date of Patent: January 13, 1998Assignee: Tanabe Seiyaku Co. Ltd.Inventors: Thomas Charles McKenzie, Gilbert M. Rishton, Nancy K. Harn, Wolfgang Scholz, James Hu
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Patent number: 5700827Abstract: The invention relates to new amino acid derivatives of general formula IR.sup.1 --R.sup.11 --A.sup.1 B (I)and the pharmaceutically acceptable salts thereof, wherein group B is --A.sup.2 --NR.sup.2 R.sup.3 or R.sup.5, and whereinR.sup.1, A.sup.1, A.sup.2, R.sup.2, R.sup.3, R.sup.5 and R.sup.11 have the meanings described in the specification, as well as the preparation and use thereof. The novel compounds are valuable neurokinin (tachykinin) antagonists.Type: GrantFiled: June 7, 1995Date of Patent: December 23, 1997Assignee: Boehringer Ingelheim GmbHInventors: Gerd Schnorrenberg, Franz Esser, Horst Dollinger, Birgit Jung, Georg Speck, Erich Burger
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Patent number: 5691349Abstract: Quinuclidine derivatives of formula, and their pharmaceutically acceptable salts, in which: R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen; pr R.sup.1 and R.sup.2 are joined together so that CR.sup.1 -CR.sup.2 is a double bond; X is selected from --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.dbd.C--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 NH--, NHCH.sub.2 --, --CH.sub.2 CO--, --COCH.sub.2 --, --CH.sub.2 S(O).sub.n -- and --S(O).sub.n CH.sub.2 -- wherein n is 0, 1 or 2; and AR is phenyl which may be optionally unsubstituted or substituted by one or more substituents such as halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, dialkylamino, N-alkylcarbamoyl, N,N-di-alkylcarbamoyl, alkoxycarbonyl, alkythio, alkylsulphinyl, alkylsulphonyl, halogeno alkyl, alkanoylamino, alkylenedioxy, alkanoyl and oxime derivatives thereof and O-alkyl ethers of said oximes; provided that when X is selected from --OCH.sub.2 --, --NHCH.sub.2 --, and SCH.sub.2 --, R.sup.Type: GrantFiled: June 23, 1995Date of Patent: November 25, 1997Assignee: Zeneca LimitedInventors: Keith Blakeney Mallion, George Robert Brown, Paul Robert Owen
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Patent number: 5686463Abstract: A class of novel oxadiazoles, substituted on one of the ring carbon atoms with a non-aromatic azacyclic or azabicyclic ring, and substituted on the other ring carbon atom with a substituent of low lipophilicity; are potent muscarinic agonists, and have good CNS penetrability. The compounds are therefore useful in the treatment of neurological and mental illnesses.Type: GrantFiled: March 19, 1987Date of Patent: November 11, 1997Assignee: Merck, Sharp & Dohme, Ltd.Inventors: Raymond Baker, Kevin John Merchant, Angus Murray MacLeod, John Saunders
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Patent number: 5686461Abstract: The invention relates to compounds of formula (I). ##STR1## or a salt, or metabolically labile ester thereof wherein R.sub.1 represents a group selected from halogen, alkyl, alkoxy, amino, alkylamino, dialkylamino, hydroxy, trifluoromethyl, trifluoromethoxy, nitro, cyano, SO.sub.2 R.sub.3 or COR.sub.3 wherein R.sub.3 represents hydroxy, methoxy, or amino; m is zero or an integer 1 or 2;A represents an ethynyl group or an optionally substituted ethenyl group;X represents a bond or a C.sub.1-4 alkylene chain;R.sub.2 represents a bridged cycloalkyl or bridged heterocyclic group; which are antagonists of excitatory amino acids, to processes for their preparation and to their use in medicine.Type: GrantFiled: September 18, 1995Date of Patent: November 11, 1997Assignee: Glaxo Wellcome S.p.A.Inventors: Alfredo Cugola, Giovanni Gaviraghi, Fabrizio Micheli
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Patent number: 5679686Abstract: The present invention relates to a novel method for treating a mammal suffering from or susceptible to schizophrenia and schizophreniform diseases.Type: GrantFiled: June 5, 1995Date of Patent: October 21, 1997Assignee: Novo Nordisk A/SInventors: Franklin Porter Bymaster, Harlan E. Shannon, Per Sauerberg, Preben H. Olesen, John Stanley Ward, Charles H. Mitch
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Patent number: 5677313Abstract: The present invention relates to a novel method for treating a mammal suffering from or susceptible to schizophrenia and schizophreniform diseases.Type: GrantFiled: June 5, 1995Date of Patent: October 14, 1997Assignee: Novo Nordisk A/SInventors: Franklin Porter Bymaster, Harlan E. Shannon, Per Sauerberg, Preben H. Olesen, John Stanley Ward, Charles H. Mitch
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Patent number: 5677314Abstract: The invention relates to bis(methylidene)phenylene derivatives of the formulaA.sup.1 -Phe-A.sup.2 Iwherein Phe is an unsubstituted or substituted phenylene group, A.sup.1 is a group selected from the formulae 1, 2 and 3 and A.sup.2 is a group other than A.sup.1 selected from the formulae 1, 2 and 3 ##STR1## wherein R.sup.1 and R.sup.2 are independently H or CH.sub.3 and their preparation and use as UV filters, in particular cosmetic and pharmaceutical preparations.Type: GrantFiled: November 28, 1995Date of Patent: October 14, 1997Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Inge Stein, Michael Schwarz, Ulrich Heywang, Michael Kompter
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Patent number: 5675007Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof (I) wherein R.sub.1 represents (a), R.sub.2 is a group OCH.sub.3, and R.sub.3 is cyano, for use in the treatment and/or prophylaxis of dementia in mammals.Type: GrantFiled: November 12, 1996Date of Patent: October 7, 1997Assignee: SmithKline Beecham p.l.c.Inventors: John Keogh, Gary Thomas Borrett, Steven Mark Bromidge, Erol Ali Faruk, Mark Jason Hughes, John Kitteringham, Martyn Voyle
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Patent number: 5672607Abstract: The present invention provides novel antiviral naphthoquinone compounds, which may be isolated from plants of the genus Conospermum or synthesized chemically, in accordance with the present inventive methods. The antiviral naphthoquionone compounds, derivatives thereof, and prodrugs thereof, may be used alone or in combination with other antiviral agents in compositions, such as pharmaceutical compositions, to inhibit the growth or replication of a virus, such as a retrovirus, in particular a human immunodeficiency virus, specifically HIV-1 or HIV-2, in the treatment or prevention of viral infection.Type: GrantFiled: January 29, 1993Date of Patent: September 30, 1997Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Michael R. Boyd, John H. Cardellina, II, Kirk R. Gustafson, Laurent A. Decosterd, Ian Parsons, Lewis Pannell, James B. McMahon, Gordon M. Cragg
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Patent number: 5668144Abstract: The compounds of the formula: ##STR1## where R is H, alkyl, haloalkyl, cycloalkyl, alkenyl or alkynyl; Y is oxygen, sulfur or NR.sub.2 where R.sub.2 is H or alkyl; or a pharmaceutically acceptable salt thereof, are useful centrally active muscarinic agents.Type: GrantFiled: October 30, 1996Date of Patent: September 16, 1997Assignee: American Home Products CorporationInventors: Annmarie L. Sabb, Reinhardt P. Stein
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Patent number: 5663182Abstract: The present invention relates to a novel method for treating a mammal suffering from or susceptible to schizophrenia and schizophreniform diseases.Type: GrantFiled: April 17, 1996Date of Patent: September 2, 1997Inventors: Franklin Porter Bymaster, Harlan E. Shannon, Per Sauerberg, Preben H. Olesen, John Stanley Ward, Charles H. Mitch
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Patent number: 5658925Abstract: To provide a compound which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio. An aminobenzoic acid derivative represented by the general formula (I) or (II) or a pharmacologically acceptable salt thereof: ##STR1## [wherein R.sup.1 represents a group represented by the formula ##STR2## etc., {wherein A represents a group represented by formula --CH.sub.2 --X--CH.sub.2 -- (wherein X represents O, >N--R.sup.6 or >CHR.sup.7 (wherein R.sup.6 represents lower alkyl and R.sup.7 represents hydrogen or lower alkoxy)), etc.; D and E each represents a group represented by formula --(CH.sub.2).sub.3 --, etc., and R.sup.2 represents lower alkyl, etc.}; R.sup.9 represents alkynyl; R.sup.10 represents amino, etc.; R.sup.11 represents halogen; R.sup.12 and R.sup.13 each represent lower alkyl; a is an integer of 1 to 5; and b is an integer of 0 to 5].Type: GrantFiled: June 1, 1995Date of Patent: August 19, 1997Assignee: Eisai Co., Ltd.Inventors: Shuhei Miyazawa, Yorihisa Hoshino, Hisashi Shibata, Kazuo Hirota, Takaaki Kameyama, Shinya Abe, Takashi Yamanaka
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Patent number: 5656639Abstract: The invention relates to compounds of the formula ##STR1## in which: m is 2 or 3;n is 0, 1 or 2;Am is ##STR2## R.sub.1 is a (C.sub.1 -C.sub.4)-alkyl or a benzyl; R.sub.2 is a substituted or unsubstituted phenyl;x is zero or one;Ar is a substituted or unsubstituted phenyl, a naphthyl or an indolyl;Z is a substituted or unsubstituted phenyl; andA.sup..crclbar. is an anion;the salts thereof, where appropriate, with mineral or organic acids and the solvates thereof, where appropriate.These compounds have a strong affinity for the NK.sub.1 receptor and are useful for preparing drugs for the treatment of substance P-dependent pathological conditions.Type: GrantFiled: January 30, 1996Date of Patent: August 12, 1997Assignee: SanofiInventors: Xavier Emonds-Alt, Isabelle Grossriether, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5654315Abstract: Quinuclidine compounds of the formula I: ##STR1## R.sup.1 is hydrogen or hydroxy; R.sup.2 is hydrogen;or R.sup.1 and R.sup.2 are joined together so that CR.sup.1 --CR.sup.2 is a double bond;X is selected from --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.sub.2 NH--, --NHCH.sub.2 --, --CH.sub.2 CO--, --COCH.sub.2 --, --CH.dbd.N--, --N.dbd.CH--, --CH.sub.2 S--, --SCH.sub.Type: GrantFiled: June 23, 1994Date of Patent: August 5, 1997Assignee: Imperial Chemical Industries PLCInventors: George Robert Brown, Keith Blakeney Mallion, Peter John Harrison, deceased
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Patent number: 5654281Abstract: Nontoxic substances that block the N-methyl-D-aspartate (NMDA) receptor, e.g., a morphinan such as dextromethorphan or dextrorphan, or that block a major intracellular consequence of NMDA receptor activation, e.g., a ganglioside such as GM.sub.1 or GT.sub.1b, a phenothiazine such as trifluoperazine or a naphthalenesulfonamide such as N-(6-aminohexyl) -5-chloro-1-naphthalenesulfonamide, inhibit the development of tolerance to and/or dependence on addictive drugs, e.g., narcotic analgesics such as morphine, codeine, etc.Type: GrantFiled: April 26, 1995Date of Patent: August 5, 1997Assignee: Virginia Commonwealth UniversityInventors: David J. Mayer, Donald D. Price, Jianren Mao, John W. Lyle
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Patent number: 5648085Abstract: Pest populations that have developed pesticide resistance can be treated and killed with an inhibitor for ATP-dependent 150-180 kDa membrane P-glycoprotein as a pretreatment or simultaneously with application of a pesticide at doses which, by themselves, are not toxic to the pests.Type: GrantFiled: March 15, 1995Date of Patent: July 15, 1997Assignee: Duke UniversityInventors: Christine L. Lanning, Mohammed B. Abou-Donia, Robert L. Fine, James J. Corcoran
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Patent number: 5643923Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 is hydrogen, halogen or alkyl; R.sup.2 is hydrogen, alkyl, optionally substituted phenyl or a heterocycle; or R.sup.1 and R.sup.2 together form a group of formula --CR.sup.4 .dbd.CR.sup.5 --CR.sup.6 .dbd.CR.sup.7 --, where R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are hydrogen, halogen, alkyl group, alkoxy, halomethyl, alkylamino, dialkylamino, hydroxy, nitro, aliphatic carboxylic acylamino or amino; and R.sup.3 is piperidyl, substituted piperidyl or quinuclidinyl. The compounds are useful in the treatment and prophylaxis of cognitive disorders, notably senile dementia, including Alzheimer's disease. Processes for preparing the compounds are also provided.Type: GrantFiled: August 27, 1992Date of Patent: July 1, 1997Assignee: Sankyo Company, LimitedInventors: Mitsuo Nagano, Takeo Kobayashi, Junichi Sakai, Masao Kozuka, Nobuyoshi Iwata, Yoshiko Kubo
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Patent number: 5641777Abstract: The invention relates to neurokinin receptor antagonist compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycleAPPLICATION: Neurokinin receptor antagonists.Type: GrantFiled: January 30, 1996Date of Patent: June 24, 1997Assignee: SanofiInventors: Xavier Emonds-Alt, Isabelle Grossriether, Patrick Gueule, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5637596Abstract: Novel 5-HT.sub.3 receptor antagonist compounds having the general formula (I) ##STR1## wherein each of R, R.sub.1 and R.sub.2, which may be the same or different, is hydrogen, halogen, hydroxy, cyano, C.sub.1 -C.sub.6 alkyl, CF.sub.3, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, formyl, C.sub.2 -C.sub.6 alkanoyl, carboxy, C.sub.1 -C.sub.6 alkoxy-carbonyl, nitro, --N(R.sub.4 R.sub.5) in which each of R.sub.4 and R.sub.5 independently is hydrogen, C.sub.1 -C.sub.6 alkyl, formyl or C.sub.2 -C.sub.6 alkanoyl; or a (R.sub.6 R.sub.7)N--SO.sub.2 group, in which each of R.sub.6 and R.sub.7 independently is hydrogen or C.sub.1 -C.sub.6 alkyl; ##STR2## wherein n is an integer of 1 or 2 and R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl unsubstituted or substituted by phenyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, formyl or C.sub.2 -C.sub.6 alkanoyl; and the pharmaceutically acceptable salts thereof, are provided.Type: GrantFiled: January 24, 1996Date of Patent: June 10, 1997Assignee: Pharmacia S.p.A.Inventors: Mario Varasi, Franco Heidempergher, Carla Caccia, Patricia Salvati
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Patent number: 5635515Abstract: Cinchonine, dihydrocinchonine or hydroquinidine are used as multidrug resistance inhibiting substance in the treatment of cancerous tumors by the use of cytotoxic agents. Particularly, cinchonine, dihydrocinchonine or hydroquinidine are used in the preparation of pharmaceutical compositions used in the treatment of cancerous tumors developing the phenomenon of multidrug resistance. Application to the treatment of human cancers.Type: GrantFiled: March 3, 1995Date of Patent: June 3, 1997Assignee: Debiopharm S.A.Inventors: Bruno Chauffert, Philippe Genne, Gilles Gutierrez, Rolland-Yves Mauvernay
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Patent number: 5622976Abstract: Heterocyclic compounds of the formula:R.sup.1 --Q--Z--X--A--MwhereinR.sup.1 is lower alkyl, a heterocyclic group which may have suitable substituent(s), etc;Q is oxadiazolediyl,Z is bond or vinyl,X is bond,a group of the formula: ##STR1## (in which R.sup.4 is hydrogen or lower alkyl), a group of the formula: ##STR2## (in which R.sup.8 is hydroxy or protected hydroxy), etc; A is bond, lower alkylene or lower alkynylene andM is a heterocyclic group containing at least one nitrogen atom which may have one substituent selected from the group consisting of lower alkyl, an imino protective group and ar(lower)alkyl which may have suitable substituent(s),and a pharmaceutically acceptable salt thereof which are useful as a medicament.Type: GrantFiled: June 24, 1994Date of Patent: April 22, 1997Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hisashi Takasugi, Atsushi Kuno, Mitsuru Ohkubo
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Patent number: 5612351Abstract: The present invention relates to a novel method for treating a mammal suffering from urinary bladder dysfunctions.Type: GrantFiled: November 8, 1994Date of Patent: March 18, 1997Assignee: Novo Nordisk A/SInventors: Mark A. Muhlhauser, Harlan E. Shannon, Karl B. Thor
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Patent number: 5612352Abstract: Biphenylylquinuclidine derivatives of formula I, Q--Ar.sup.1 --Ar.sup.2, in which Q is of formula Ia or Ib, ##STR1## in which R.sup.1 and R.sup.2 are independently selected from hydrogen, alkyl, halogeno and hydroxy; or R.sup.1 and R.sup.2 when taken together define an oxo group; Xb is selected from --CH.sub.2 --, .dbd.CH-- and --CH(OH); Xa is selected from --CH.sub.2 --, .dbd.CH--, CO, --O--, and --S(O)n (wherein n=0, 1 or 2); Ar.sup.1 is a phenylene moiety; Ar.sup.2 is phenyl; and wherein one or both of Ar.sup.1 and Ar.sup.Type: GrantFiled: July 14, 1994Date of Patent: March 18, 1997Assignee: Zeneca LimitedInventors: George R. Brown, Peter J. Harrison, deceased, Keith B. Mallion
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Patent number: RE35593Abstract: A compound of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 represents ##STR2## in which each of p and q independently represents an integer of 2 to 4, r represents an integer of 2 to 4, s represents 1 or 2 and t represents 0 or 1;R.sub.2 is a group OR.sub.4, where R.sub.4 is C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, a group OCOR.sub.5 where R.sub.5 is hydrogen or R.sub.4, or a group NHR.sub.6 or NR.sub.7 R.sub.8 where R.sub.6, R.sub.7 and R.sub.8 are independently C.sub.1-2 alkyl; andR.sub.3 is chloro, fluoro, bromo, cyclopropyl, C.sub.1-3 alkyl substituted by one, two or three halogen atoms, or R.sub.3 is a group (CH.sub.2).sub.n R.sub.9 where R.sub.9 is --CN, --OH, --OCH.sub.3, --SH, --SCH.sub.3, --C.tbd.CH or --CH.dbd.CH.sub.2 and n is O or 1, with the proviso that when n is 0, R.sub.9 is not --OH or --SH.Type: GrantFiled: January 11, 1996Date of Patent: August 19, 1997Assignee: Beecham Group p.l.c.Inventors: Barry S. Orlek, Steven M. Bromidge, Steven Dabbs