The Chalcogen, X, Is Part Of A -c(=x)x- Group, Wherein The X's Are The Same Or Diverse Chalcogens Patents (Class 546/335)
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Patent number: 5633231Abstract: The present invention relates to valine-containing, substituted pseudopeptides of the general formula (I) ##STR1## in which the substituents have the meaning given in the description, to processes for their preparation, and to their use as anti-viral agents, in particular against cytomegaloviruses.Type: GrantFiled: September 7, 1994Date of Patent: May 27, 1997Assignee: Bayer AktiengesellschaftInventors: Dieter Habich, Thomas J. Schulze, Jurgen Reefschlager, Jutta Hansen, Rainer Neumann, Gert Streissle, Arnold Paessens
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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: 5631262Type: GrantFiled: May 11, 1995Date of Patent: May 20, 1997Assignee: SmithKline Beecham CorporationInventors: Pamela A. Chambers, Robert A. Daines, Dalia R. Jakas, William D. Kingsbury, Israil Pendrak
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Patent number: 5605915Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning defined in the specification.Type: GrantFiled: May 31, 1996Date of Patent: February 25, 1997Assignee: AllerganInventors: Vidyasagar Vuligonda, Richard L. Beard, Alan T. Johnson, Min Teng, Tae K. Song, Roshantha A. Chandraratna
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Patent number: 5602119Abstract: Succinoylamino hydroxyethylamino sulfamic acid derivative compounds which are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: January 31, 1995Date of Patent: February 11, 1997Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
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Patent number: 5599975Abstract: A compound selected from those of formula (I): ##STR1## wherein A, X, Y, Z, R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in the description.This compound or its physiologically tolerable salts may be used therapeutically as platelet anti-aggregation agent.Type: GrantFiled: October 27, 1994Date of Patent: February 4, 1997Assignee: Adir Et CompagnieInventors: Ren e Gree, Ali M. Hachem, Danielle Gree, Yves Le Floc'h, Yves Rolland, Serge Simonet, Tony Verbeuren
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Patent number: 5599966Abstract: Compounds of the formula (I): Ar.sub.1 --CH(OH)--CH.sub.2 --NH--CH.sub.2 --X--CH.sub.2 --E--(CH.sub.2).sub.n --Y--Ar.sub.2, in which the substituents and symbols have the meanings given in the description, are novel active compounds having, in particular, a broncholytic action.Type: GrantFiled: April 17, 1995Date of Patent: February 4, 1997Assignee: BYK Nederland BVInventors: Jan Bron, Geert J. Sterk, Hendrik Timmerman, Meta E. J. Veerman, Jan F. Van Der Werf
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Patent number: 5597837Abstract: Methods of inhibiting cell proliferation in a patient suffering from such disorder comprising the use of a styryl-substituted heteroaryl compound wherein the heteroaryl group is a monocyclic ring with 1 or 2 heteroatoms, or a bicyclic ring with 1 to about 4 heteroatoms, said compound optionally substituted or polysubstituted, with the proviso that when said ring is polysubstituted, the substituents do not have a common point of attachment to said ring, and those compounds wherein no substituent on the heteroaryl group is a carboxy group or an ester group, and pharmaceutical compositions comprising such compounds.Type: GrantFiled: April 11, 1994Date of Patent: January 28, 1997Assignee: Rh one-Poulenc Rorer Pharmaceuticals Inc.Inventors: Alfred P. Spada, Paul E. Persons
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Patent number: 5596009Abstract: A fused benzeneoxyacetic acid derivative of the formula (I): ##STR1## A is --COW, --NR.sup.4 --Y or --Z--NR.sup.4 --CONR.sup.2 R.sup.3 ; and salts thereof possess an agonistic on PGI.sub.2 receptor, so it is useful for prevention and/or treatment of thrombosis, arteriosclerosis, ischemic heart diseases, gastric ulcer and hypertention.Type: GrantFiled: May 19, 1994Date of Patent: January 21, 1997Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Nobuyuki Hamanaka, Kanji Takahashi, Hidekado Tokumoto
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Patent number: 5585391Abstract: The invention concerns the discovery of the surprising and unexpected therapeutic effects of hydroxyl ions. The observed medicinal properties of these ions are both novel and broad in scope. The acute corrosive effects and toxicity of hydroxyl ions on living tissue has previously overwhelmed their therapeutic attributes. Unique hydroxyl ion modulating compounds have been discovered and are within the scope of the invention. When used appropriately as companions with hydroxyl ions, these modulating compounds obviate and attenuate the harmful effects of hydroxyl ions, unmasking and revealing their previously unknown and undemonstratable therapeutic properties. These hydroxyl ion modulating compounds do not significantly interfere with the surprising and unexpected therapeutic benefits of the hydroxyl ions. The novel hydroxyl ion modulating compounds are generally characterized as N,N-disubstituted-aminoacetate salts and substituted N,N-substituted-aminoacetate salts.Type: GrantFiled: October 8, 1993Date of Patent: December 17, 1996Assignee: FHJ Scientific, Inc.Inventors: Delton R. Carrell, Edward J. Cragoe, Jr.
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Patent number: 5573999Abstract: .beta.-Substituted cinnamic acid derivatives of the formula 1, ##STR1## where R.sup.1 is alkyl, chlorine or bromine, --X-- is --O--, --S--, ##STR2## m is 0 or 1, --Y is --OR.sup.4, --O--N.dbd.CR.sup.5 R.sup.6, --NR.sup.7 R.sup.8, --N(OR.sup.9)R.sup.10 or --SR.sup.11, where the above-mentioned substituents R.sup.2 to R.sup.11 are alkyl, and R.sup.2, and R.sup.3 and R.sup.5 to R.sup.11 can also be hydrogen,Z is halogen, nitro, cyano, alkyl, cycloalkyl, aralkyl, aryloxyalkyl, arylthioalkyl, hetarylalkyl, hetaryloxyalkyl, hetarylthioalkyl, alkenyl, aralkenyl, aryloxyalkenyl, arylthioalkenyl, hetarylalkenyl, hetaryloxyalkenyl, hetarylthioalkenyl, alkynyl, arylalkynyl, hetarylalkynyl, aryl, hetaryl, arylazo, acylamino, --OR.sup.12, --SR.sup.13, --SOR.sup.14, --SO.sub.2 R.sup.15, --COOR.sup.16, --CONR.sup.17 R.sup.18, --COR.sup.19, --CR.sup.20 .dbd.NR.sup.21, --N.dbd.CR.sup.22, R.sup.23, --CR.sup.24 .dbd.N--OR.sup.25, --CR.sup.25 R.sup.26 --O--, N.dbd.CR.sup.27 R.sup.28, --CH.sub.2 --OCOR.sup.39 or --NR.sup.37 R.Type: GrantFiled: May 15, 1995Date of Patent: November 12, 1996Assignee: BASF AktiengesellschaftInventors: Hubert Sauter, Herbert Bayer, Klaus Oberdorf, Horst Wingert, Wolfgang von Deyn, Wassilios Grammenos, Hartmann Koenig, Harald Rang, Franz Roehl, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5567723Abstract: Compounds having the structural formula ##STR1## wherein R is C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkyl; R.sup.1 is fluorenyl, thienyl, pyridyl or thiazolyl, unsubstituted or substituted by one or more substituents selected from C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkylthio, halogen, C.sub.1 -C.sub.4 haloalkyl and nitro; and R.sup.2 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.6 haloalkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.2 -C.sub.6 alkoxyalkyl. The compounds of this invention are effective for controlling mites and nematodes.Type: GrantFiled: July 5, 1995Date of Patent: October 22, 1996Assignees: Uniroyal Chemical Company, Inc., Uniroyal Chemical Ltd./LteeInventors: Mark A. Dekeyser, Derek J. McPhee, Paul T. McDonald
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Patent number: 5565606Abstract: The invention relates to compounds of the formula I ##STR1## in which A denotes hydrogen or an amino protective group, B denotes one or more amino acids, X denotes alkylene or aralkylene, Y.sup.1, Y.sup.2, Y.sup.3 and Y.sup.4 are identical or different and denote hydrogen, methyl, methoxy or nitro, V denotes hydrogen or a carboxyl protective group, W denotes --[CH.sub.2 ].sub.n -- or --O--[CH.sub.2 ].sub.n --, m denotes 0 or 1, n denotes 0 to 6, and p denotes 0 to 5, to a process for their preparation. The compounds of formula I are useful as linkage agents or anchor groups in the solid-phase synthesis of peptide aminoalkylamides and peptide hydrazides.Type: GrantFiled: June 8, 1994Date of Patent: October 15, 1996Assignee: Hoechst AktiengesellschaftInventors: Gerhard Breiphol, Jochen Knolle
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Patent number: 5563168Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.Type: GrantFiled: June 16, 1995Date of Patent: October 8, 1996Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 5559140Abstract: This invention relates to novel difluoro statone analogs, to the processes and intermediates useful for their preparation and to their use as anti-viral agents.Type: GrantFiled: June 30, 1993Date of Patent: September 24, 1996Assignee: Merrell Pharmaceuticals Inc.Inventors: Daniel Schirlin, Viviane Van Dorsselaer, Celine Tarnus
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Patent number: 5557006Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth fire disclosed.Type: GrantFiled: April 20, 1995Date of Patent: September 17, 1996Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
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Patent number: 5550247Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.Type: GrantFiled: April 20, 1995Date of Patent: August 27, 1996Assignee: Hoechst Roussel Pharmaceuticals Inc.Inventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Harner, Brian S. Freed, Gregory H. Merriman
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Patent number: 5545741Abstract: The invention relates to a process for the preparation of racemic or optically active epibatidine of the Formula XIV ##STR1## which comprises subjecting racemic or optically active epi-epibatidine-of the Formula XIII ##STR2## to epimerization in the presence base. The advantage of the process is that readily available starting materials are used and the procedure is suitable for industrial scale productions too.Epibatidine is a known highly affective analgesic active ingredient.Type: GrantFiled: December 5, 1994Date of Patent: August 13, 1996Assignee: Egis Gyogyszergyar Rt.Inventors: Csaba Sz antay, Zsuzsanna B. Kardos, Istv an Moldvai, Eszter T. Major, Csaba Sz antay, Jr., Attila M andi, G abor Blask o, Gyula Simig, Gy orgyi Lax, S andor Drabant, Tamas Sz all asi, M arton Fekete, G abor Gigler
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Patent number: 5545838Abstract: Compounds of the formula ##STR1## wherein Z is SO or SO.sub.2 possess renin inhibition activity and are useful in treating hypertension and other diseases where the reduction of the levels of circulating angiotensin II are beneficial.Type: GrantFiled: January 27, 1992Date of Patent: August 13, 1996Assignee: E. R. Squibb & Sons, Inc.Inventor: Michael A. Poss
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Patent number: 5543423Abstract: The present invention relates to compounds that can maintain, increase, or restore sensitivity of cells to therapeutic or prophylactic agents. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well-suited for treatment of multi-drug resistant cells, for prevention of the development of multi-drug resistance, and for use in multi-drug resistant cancer therapy.Type: GrantFiled: January 23, 1995Date of Patent: August 6, 1996Assignee: Vertex Pharmaceuticals, IncorporatedInventors: Robert E. Zelle, Matthew W. Harding
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Patent number: 5532375Abstract: Compounds useful in the treatment of Alzheimer's disease, senile dementia, or memory disorders which have the formula ##STR1## in which R represents a hydrogen atom, a linear, branched or cyclic alkyl radical, saturated or unsaturated, containing up to 8 carbon atoms, possibly substituted by a free or esterified carboxy radical or R represents an aralkyl radical containing up to 10 carbon atoms and R' represents a linear or branched, saturated or unsaturated, alkyl radical, containing up to 8 carbon atoms, a radical --COalk.sub.1 or a radical --(CH.sub.2).sub.2 N(alk.sub.2).sub.2, alk.sub.1 and alk.sub.2 representing an alkyl radical containing up to 8 carbon atoms, as well as their addition salts with acids. Also compositions containing the same, method of preparation and method of treatment using the same.Type: GrantFiled: September 30, 1994Date of Patent: July 2, 1996Assignee: Roussel-UCLAFInventors: Giulio Galliani, Fernando Barzashi, Alina Butti, Carla Bonetti, Emilio Toja
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Patent number: 5516786Abstract: Combating fungi with substituted amine acid derivatives of the formula ##STR1## in which R.sup.1 represents alkyl, alkenyl, alkinyl, halogenoalkyl, halogenoalkenyl, halogenoalkinyl, cycloalkyl or cycloalkenyl,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and represent hydrogen, cycloalkyl or alkyl, orR.sup.3 and R.sup.4, together with the carbon atom to which they are bonded, form a cycloalkyl ring, andR.sup.6 represents hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, unsubstituted or substituted phenylalkyl, unsubstituted or substituted phenyl or unsubstituted or substituted cycloalkyl, or represents unsubstituted or substituted heterocyclyl or heterocyclylalkyl,orR.sup.5 and R.sup.6, together with the nitrogen atom to which they are bonded, represent a heterocyclyl radical, which can contain further hetero atoms.Type: GrantFiled: November 21, 1994Date of Patent: May 14, 1996Assignee: Bayer AktiengesellschaftInventors: Detlef Wollweber, Thomas Seitz, Wilhelm Brandes
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Patent number: 5514808Abstract: The invention concerns the discovery of the surprising and unexpected therapeutic effects of hydroxyl ions. The observed medicinal properties of these ions are both novel and broad in scope. The acute corrosive effects and toxicity of hydroxyl ions on living tissue has previously overwhelmed their therapeutic attributes. Unique hydroxyl ion modulating compounds have been discovered and are within the scope of the invention. When used appropriately as companions with hydroxyl ions, these modulating compounds obviate and attenuate the harmful effects of hydroxyl ions, unmasking and revealing their previously unknown and undemonstratable therapeutic properties. These hydroxyl ion modulating compounds do not significantly interfere with the surprising and unexpected therapeutic benefits of the hydroxyl ions. The novel hydroxyl ion modulating compounds are generally characterized as N,N-disubstituted-aminoacetate salts and substituted N,N-substituted-aminoacetate salts.Type: GrantFiled: August 25, 1994Date of Patent: May 7, 1996Assignee: FHJ Scientific, IncInventors: Delton R. Carrell, Edward J. Cragoe, Jr.
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Patent number: 5514694Abstract: A novel class of peptide .alpha.-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula Y--CO--AA.sup.2 --AA.sup.1 --CO--NH--X. Processes for the synthesis of peptidyl .alpha.-ketoamide derivatives.Type: GrantFiled: June 24, 1993Date of Patent: May 7, 1996Assignee: Georgia Tech Research CorpInventors: James C. Powers, Zhaozhao Li, Girish S. Patil, Der-Lun Chu
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Patent number: 5510344Abstract: Compounds of formula I ##STR1## wherein X is oxygen or sulphur, W is CH or N, m is 0 or 1, and either a) n is 1 and Q is a non-aromatic heterocyclic ring of 3 to 10 ring atoms, containing one to three hetero atoms selected from oxygen, sulphur and nitrogen, which may be substituted and may be fused to another ring, with the proviso a) that if Q is thiazol-2-in-2-yl, it is substituted but not by methylene, and b) Q is not a six membered ring containing only two nitrogen atoms, or b) n is 0 or 1 and Q is ##STR2## where R.sup.1 is alkyl, alkoxy or alkylthio, and R.sup.2 is heteroaryl, non aromatic heterocyclyl, optionally substituted cycloalkyl or optionally substituted alkyl containing at least 5 carbon atoms, phenyl substituted by one or more groups selected from halogen, optionally substituted alkyl, alkoxy, haloalkoxy, aryloxy, alkylthio and alkoxycarbonyl, and when R.sup.1 is alkyl or alkoxy, or, when W is nitrogen, R.sup.2 can also be unsubstituted phenyl, have pesticidal especially fungicidal activity.Type: GrantFiled: May 4, 1994Date of Patent: April 23, 1996Assignee: Schering Agrochemicals LimitedInventors: Geoffrey R. Cliff, Ian C. Richards
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Patent number: 5502198Abstract: Pharmaceutically useful compounds having acyl-coenzyme A: cholesterol acyltransferase inhibitory activity having the general formula ##STR1## wherein Ar is di- or trisubstituted aryl or heteroaryl; R.sub.14 and R.sub.15 are each independently aryl, heteroaryl, hydrogen, fluorine, or alkyl, with the proviso that R.sub.14 and R.sub.15 are not both hydrogen, fluorine, or a straight or branched chain alkyl or a combination thereof; and R.sub.16 is a straight or branched hydrocarbon chain having 1 to 20 carbon atoms and is saturated or unsaturated and has 1 to 3 double bonds, the double bonds being adjacent or nonadjacent.Type: GrantFiled: March 6, 1995Date of Patent: March 26, 1996Assignee: Warner-Lambert CompanyInventors: Joseph A. Picard, Drago R. Sliskovic
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Patent number: 5502050Abstract: Inhibitor of the use of tetrahydrobiopterin as a cofactor for nitric oxide synthase, e.g., substituted 4-phenyl(hydropyridines) such as 1-methyl-4-(3',4'-dihydroxyphenyl)-1,2,3,6-tetrahydropyridine or, 4-(3',4'-dihydroxyphenyl)-1,2,3,6-tetrahydropyridine) or tetrahydropterin analog which does not replace tetrahydrobiopterin as a substrate for nitric oxide synthase such as (6R,S)-6,7-dimethyl-tetrahydropterin or (6R,S)-tetrahydrofolic acid or 2,4-diamino-, 2,6-diamino, or 4,6-diamino mono- or disubstituted pyrimidines or the corresponding pyrimidine-3-oxides such as 2,4-diamino-6-(diethylamino)pyrimidine, 2,4-diamino-6-piperidino-pyrimidine-3-oxide, 2,4-diamino-6-hydroxypyrimidine, 4,6-diamino-2-hydroxypyrimidine or 2,5-diamino-4,6-dihydroxypyrimidine is administered to inhibit nitric oxide synthesis from arginine in vascular cells in a subject in need of such inhibition (e.g., for prophylaxis or treatment of cytokine- or endotoxin-induced hypotension (e.g., septic shock).Type: GrantFiled: November 29, 1993Date of Patent: March 26, 1996Assignee: Cornell Research Foundation, Inc.Inventor: Steven S. Gross
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Patent number: 5495023Abstract: A new nitro compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each lower alkyl or lower alkoxy(lower)alkyl, or ##STR2## is cyclized to form ##STR3## X is --O--, --S-- or --NH--, m is an integer 0 or 1, andR.sup.3 is carbamoyl, lower alkylcarbamoyl, lower alkanoyl, di-lower alkylaminosulfonyl, lower alkylsulfonyl, oxamoyl or a group of the formula: --(Y).sub.n --R.sup.4whereinY is --CO--, --SO.sub.2 --, --COCH.sub.2 -- or ##STR4## n is an integer of 0 or 1, and R.sup.4 is heterocyclic group which is optionally substituted with one or more substituents selected from lower alkyl, lower alkoxy, phenyl, carbamoyl, halogen, amino, lower alkylthio, hydroxy, lower alkylsulfonylamino and carbamoylmethyl, and pharmaceutically acceptable salt thereof, which are useful as vasodilators.Type: GrantFiled: May 3, 1994Date of Patent: February 27, 1996Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Masayuki Kato, Shigetaka Nishino, Mitsuko Hamano, Hisashi Takasugi
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Patent number: 5488149Abstract: A compound of the formula (I) or its pharmaceutically acceptable salt or ester: ##STR1## wherein each of the substituents are herein defined.Type: GrantFiled: June 6, 1995Date of Patent: January 30, 1996Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takashi Nomoto, Masahiro Hayashi, Jun Shibata, Yoshikazu Iwasawa, Morihiro Mitsuya, Yoshiaki Iida, Katsumasa Nonoshita, Yasufumi Nagata
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Patent number: 5476864Abstract: A glycerin derivative having the following formula (I) or (I') and a pharmacologically acceptable salt thereof are useful to treat diseases caused by the platelet activating factor.Type: GrantFiled: November 10, 1993Date of Patent: December 19, 1995Assignee: Eisai Co., Ltd.Inventors: Kazuo Okano, Osamu Asano, Naoyuki Shimomura, Tetsuya Kawahara, Shinya Abe, Shuhei Miyazawa, Mitsuaki Miyamoto, Hiroyuki Yoshimura, Koukichi Harada, Junsaku Nagaoka, Tsutomu Kawata, Tsutomu Yoshimura, Hiromasa Suzuki, Shigeru Souda, Yoshimasa Machida, Kouichi Katayama, Isao Yamatsu
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Patent number: 5475119Abstract: Ionic monomeric diallylammonium compounds having a targeted combination of diallylammonium cations with selected anions have particularly high and constant charge control properties and very good heat stabilities and dispersibilities.The compounds according to the invention are outstandingly suitable for use as colorless charge control agents in toners and developers for electrophotographic recording processes and for use as charge-improving agents in powders and paints for surface coating, in particular in triboelectrically or electrokinetically sprayed powder paints.Type: GrantFiled: December 17, 1992Date of Patent: December 12, 1995Assignee: Hoechst AktiengesellschaftInventors: Rudiger Baur, Hans-Tobias Macholdt
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Patent number: 5436343Abstract: Compounds of formula (I): ##STR1## in which: R.sub.1 and R.sub.2, which may be identical or different, represent a linear or branched (C.sub.1 C.sub.6) alkyl radical, a substituted or unsubstituted phenyl radical, a pyridyl radical or a thienyl radical, or, with the carbon atom to which they are attached, a substituted or unsubstituted (C.sub.4 -C.sub.7) cycloalkyl ring,R.sub.3 representsa substituted or unsubstituted phenylsulfonyl radical,a linear or branched (C.sub.1 -C.sub.6) alkyl radical,an alkylaminocarbonyl radical,or a linear or branched (C.sub.1 -C.sub.6) acyl radical,R.sub.4 represents any one of the radicals:--CH.dbd.CH--(CH.sub.2).sub.p --CO.sub.2 H or --CH.sub.2 --CH.sub.2 --(CH.sub.2)p--CO.sub.2 Hin which p is equal to 0, 1, 2 or 3, n and m, which may be identical or different, represent 0, 1 or 2,their isomers, enantiomers, diastereoisomers and epimers as well as their addition salts with a pharmaceutically acceptable acid or base.Type: GrantFiled: May 14, 1993Date of Patent: July 25, 1995Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Patrick Hautefaye, Michel Laubie, Tony Verbeuren
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Patent number: 5434267Abstract: Process for the preparation of compounds of the formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, X and n have the meaning given in the description, by reacting acetates with carbon monoxide in the presence of a basic auxiliary, followed by alkylation. The products are intermediates for fungicidal acrylates.Type: GrantFiled: March 14, 1994Date of Patent: July 18, 1995Assignee: Bayer AktiengesellschaftInventors: Helmut Kraus, Alexander Klausener, Hans-Joachim Diehr
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Patent number: 5432186Abstract: Disclosed are the compounds of formula I ##STR1## wherein R represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl-lower alkyl or cycloalkyl-lower alkyl;R.sub.1 represents hydrogen, lower alkyl, cycloalkyl, carbocyclic aryl or heterocyclic aryl, or biaryl;R.sub.3 represents hydrogen or acyl;R.sub.4 represents hydrogen, lower alkyl, carbocyclic or heterocyclic aryl, carbocyclic or heterocyclic aryl-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, biaryl or biaryl-lower alkyl;R.sub.Type: GrantFiled: November 19, 1993Date of Patent: July 11, 1995Assignee: Ciba-Geigy CorporationInventor: Cynthia A. Fink
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Patent number: 5420287Abstract: A class of 1,2-diarylcyclopentenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein A is selected from ##STR2## wherein each of R.sup.1 and R.sup.2 is independently selected from hydrido, methyl, ethyl, fluoro, hydroxymethyl, carbomethoxy, trifluoromethyl, carboxyl and fluoromethyl; wherein each of R.sup.3, R.sup.4, R.sup.6 through R.sup.9, R.sup.11 and R.sup.12 is independently selected from hydrido, methyl, fluoro and chloro; and wherein each of R.sup.5 and R.sup.10 is independently selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, methoxy, methylthio, cyano, trifluoromethyl, hydroxymethyl, methoxymethyl, methylsulfonyl and sulfamyl; provided that when A is ##STR3## R.sup.5 cannot be hydrido when R.sup.10 is selected from hydrido, cyano, halo, methyl, trifluoromethyl and methoxy.; further provided that R.sup.10 cannot be hydrido when R.sup.Type: GrantFiled: June 3, 1994Date of Patent: May 30, 1995Assignee: G. D. Searle & Co.Inventors: David B. Reitz, Jinglin Li
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Patent number: 5418244Abstract: Compounds of the formula ##STR1## wherein the variables are defined in the specification. The compounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.Type: GrantFiled: August 11, 1993Date of Patent: May 23, 1995Assignee: University of FloridaInventors: Richard H. Hammer, Nicholas S. Bodor
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Patent number: 5411936Abstract: Cyclohexenone oxime ethers of the general formula I ##STR1## where R.sup.1 is C.sub.1 -C.sub.6 -alkyl, A is substituted or unsubstituted C.sub.4 -alkylene or C.sub.4 -alkenylene,x is nitro, cyano, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl and/or phenyl,n is from 0 to 3 or from 1 to 5 when X is halogen,R.sup.2 is C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.4 -alkylthio-C.sub.1 -C.sub.6 -alkyl, substituted or unsubstituted C.sub.3 -C.sub.7 -cycloalkyl or C.sub.5 -C.sub.Type: GrantFiled: January 19, 1993Date of Patent: May 2, 1995Assignee: BASF AktiengesellschaftInventors: Juergen Kast, Dieter Kolassa, Norbert Meyer, Ulrich Schirmer, Albrecht Harreus, Jochen Wild, Karl-Otto Westphalen, Bruno Wuerzer
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Patent number: 5399589Abstract: Oxalyl hydrazide-hydroxamic acid derivatives of the formula I ##STR1## where the substituents have the following meanings: R, R.sup.1, R.sup.2 and R.sup.3 independently of one another arehydrogen, substituted or unsubstituted alkyl, alkenyl or alkynyl orsubstituted or unsubstituted cycloalkyl or cycloalkylmethyl,substituted or unsubstituted cycloalkenyl or cycloalkenylmethyl,substituted or unsubstituted phenyl, phenylalkyl, phenylalkenyl, hetaryl- or hetarylalkyl radicals, where R.sup.2 and R.sup.3 may also. together with the nitrogen atom whose substituents they are, form a 5- or 6-membered ring, orR.sup.2 together with R.sup.3 is the group ##STR2## where R.sup.4 and R.sup.5 are one of the radicals R, R.sup.1, R.sup.2 or R.sup.3, or R.sup.4 together with R.sup.5 and the carbon atom whose substituents they are, are monocyclic or polycyclic cycloalkyl, orR.sup.4 together with R.sup.5 and the carbon atom whose substituents they are, form a 5- or 6-membered, saturated heterocycle containing O, S or --N(R.sup.Type: GrantFiled: November 29, 1993Date of Patent: March 21, 1995Assignee: BASF AktiengesellschaftInventors: Costin Rentzea, Albrecht Harreus, Eberhard Ammermann, Gisela Lorenz
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Patent number: 5399575Abstract: Compounds of the formula I ##STR1## in which A signifies an alkylene radical with 1 to 3 carbon atoms or a group --CH.dbd.CH--, B an oxygen atom or a valency bond, m a whole number from 0 to 5, n the number 0 or 1, X a valency bond, an oxygen atom or a sulphur atom, Y a valency bond or a phenylene radical substituted, if desired, one or more times by C.sub.1 - to C.sub.6 -alkyl, C.sub.1 - to C.sub.6 -alkoxy, halogen, hydroxyl or aminocarbonyl, Z hydrogen, halogen, C.sub.1 - to C.sub.6 -alkyl or cyano and R a group CN, COOH, COOC.sub.1 - to C.sub.6 -alkyl, CONH-tetrazolyl, CON(OH)(C.sub.1 -C.sub.6 -alkyl) or 5-(1H)-tetrazolyl, as well as, for the case that Y represents a phenylene radical, also hydrogen, with the exception of the compound 4-[2-(4)-pyridinovinyl]-carboxymethoxybenzene, their physiologically compatible salts and processes for their preparation, as well as medicaments containing these compounds for the treatment of allergic diseases.Type: GrantFiled: June 14, 1993Date of Patent: March 21, 1995Assignee: Boehringer Mannheim GmbHInventors: Walter-Gunar Friebe, Wolfgang Kampe, Marcel Linssen, Otto-Henning Wilhelms
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Patent number: 5391577Abstract: N-phenylalkyl substituted .alpha.-amino carboxamide derivatives of formula (I) ##STR1## wherein R is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, furyl, thienyl, pyridyl or unsubstituted or substituted phenyl; A is a --(CH.sub.2).sub.m -- or --(CH.sub.2).sub.p --X--(CH.sub.2).sub.q -- group wherein X is --O--, --S-- or --NR.sub.4 --; R.sub.1, R.sub.2, R.sub.3, R'.sub.3, R.sub.4, n, m, p and q are as herein defined; and each of R.sub.5 and R.sub.6 is independently hydrogen or C.sub.1 -C.sub.6 alkyl, and the pharmaceutically acceptable salts thereof, are active on the central nervous system and can be used as anti-epileptic, anti-Parkinson, neuroprotective, antidepressant, antispastic and/or hypnotic agents in mammals.Type: GrantFiled: May 25, 1993Date of Patent: February 21, 1995Assignee: Farmitalia Carlo Erba S r lInventors: Philippe Dostert, Paolo Pevarello, Franco Heidempergher, Mario Varasi, Alberto Bonsignori, Romeo Roncucci
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Patent number: 5374724Abstract: A process for the preparation of a substituted acetic acid of the Formula (2): ##STR1## wherein --X--Z is an optionally substituted aromatic or heteroaromatic optionally substituted amino radical; by reacting a compound of the Formula (7):Z--Y--H Formula 7with glyoxylic acid. The compounds of Formula (2) are useful as intermediates in the preparation of polycyclic dyes.Type: GrantFiled: November 2, 1992Date of Patent: December 20, 1994Assignee: Zeneca, LimitedInventors: Nigel Hall, Nigel Hughes, Prakash Patel
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Patent number: 5373023Abstract: The invention provides compounds which are tetrahydronaphthalene derivatives of the formula (I) ##STR1## wherein R.sub.1 represents a halogen atom, a cyano group, a nitro group, an unbranched (C.sub.1 -C.sub.6) alkoxy group, a (C.sub.1 -C.sub.6 cycloalkyl) (C.sub.1 -C.sub.2 alkoxy) group or an aryl (C.sub.1 -C.sub.2 alkoxy) group,R.sub.2 represents a (C.sub.1 -C.sub.4) alkyl group, an aryl group optionally substituted with at least one methoxy group, a pyridyl group or a benzodioxanyl group,R.sub.3 represents a hydrogen atom or a (C.sub.1 -C.sub.2) alkyl group, and n=0 to 3, or are addition salts with pharmaceutically acceptable acids. The compounds of the invention have anti-ischaemic activity.Type: GrantFiled: August 4, 1993Date of Patent: December 13, 1994Assignee: SYNTHELABOInventors: Paul Howard Williams, Christian Hoornaert, Jean Claude Muller
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Patent number: 5371084Abstract: 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: October 28, 1993Date of Patent: December 6, 1994Assignee: Zeneca LimitedInventors: Paul J. de Fraine, Anne Martin
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Patent number: 5371267Abstract: Amino acid derivatives of the general formula (I) ##STR1## are disclosed. The active compounds are suitable for use as plant protection agents, in particular as fungicides.Type: GrantFiled: October 16, 1992Date of Patent: December 6, 1994Assignee: Bayer AktiengesellschaftInventors: Thomas Seitz, Wolfgang Bender, Heinz-Wilhelm Dehne
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Patent number: 5360811Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols of the formulaRCH(OR.sup.1)CH(NR.sup.2 R.sup.3)R.sup.4 or RCH.sub.2 CR.sup.35 (NR.sup.2 R.sup.3)R.sup.4wherein R is ##STR1## wherein R.sup.5 is CH.sub.3 (CH.sub.2).sub.m C.tbd.C, CH.sub.3 (CH.sub.2).sub.m CH.dbd.CH,CH.sub.3 (CH.sub.2).sub.m CH.sub.2 CH.sub.2, ##STR2## wherein m is 3 to 15, n is 0 to 12, and W and X are independently hydrogen, hydroxy, alkyl, alkoxy, halogen, or trifluoromethyl, ##STR3## wherein R.sup.23 loweralkyl; Z is S, O, or C.dbd.O; and A is S or O; R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.35 and R.sup.40 are as defined in the specification, the optical isomers thereof, or the pharmaceutically acceptable salts thereof, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.Type: GrantFiled: September 10, 1992Date of Patent: November 1, 1994Assignee: Hoechst-Roussel Pharmaceuticals IncorporatedInventors: John J. Tegeler, Barbara S. Rauckman, Russell R. L. Hamer, Brian S. Freed, Gregory H. Merriman
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Patent number: 5356914Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1 represents a 1,2,5,6-tetrahydropyridin-3-yl group N-substituted by R.sub.10 wherein R.sub.10 represents OH; a group hydrolysable in vivo to OH or hydrogen; C.sub.1-8 alkoxy; C.sub.2-8 alkenyloxy; C.sub.2-8 alkynyloxy; C.sub.3-8 cycloalkyloxy; or COR.sub.13 wherein R.sub.13 represents hydrogen, C.sub.1-8 alkyl, phenyl or phenyl C.sub.1-4 alkyl; in which any phenyl moiety is optionally substituted by up to 3 substituents independently selected from C.sub.1-6 alkoxy, C.sub.1-6 alkyl, halo, C.sub.1-6 alkoxycarbonyl, cyano, C.sub.1-6 alkylthio or C.sub.1-6 alkylsulphonyl; enhance acetylcholine function via an action at muscarinic receptors within the central nervous system and are therefore of potential use in the treatment and/or prophylaxis of dementia in mammals.Type: GrantFiled: April 5, 1993Date of Patent: October 18, 1994Assignee: Beecham Group p.l.c.Inventors: Steven M. Bromidge, Barry S. Orlek, Steven Dabbs
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Patent number: 5340828Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.Type: GrantFiled: September 30, 1991Date of Patent: August 23, 1994Assignee: Merck & Co., Inc.Inventors: Samuel L. Graham, S. Jane deSolms
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Patent number: 5330965Abstract: Cyclohexenone oxime ethers of the formula I ##STR1## (R.sup.1 =C.sub.1 -C.sub.6 -alkyl; A=substituted or unsubstituted alkylene or alkenylene;Z=a 5-membered or 6-membered heteroaromatic structure;X=substituted or unsubstituted amino, nitro, cyano, halogen, alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -haloalkoxy, carboxyl, C.sub.1 -C.sub.4 -alkoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl and phenyl;n=0 to 3, or 1 to 4 where Z is halogen-substituted pyridyl; andR.sup.Type: GrantFiled: January 15, 1993Date of Patent: July 19, 1994Assignee: BASF AktiengesellschaftInventors: Ulf Misslitz, Norbert Meyer, Juergen Kast, Norbert Goetz, Albrecht Harreus, Thomas Kuekenhoehner, Bruno Wuerzer, Helmut Walter, Karl-Otto Westphalen, Matthias Gerber
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Patent number: 5324747Abstract: Compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, n, m, o, p and q are as hereinafter set forth, and, when R.sub.2 is hydrogen, pharmaceutically acceptable salts thereof with bases, are described. The compounds of formula 1 are potent inhibitors of phospholipases A.sub.2 (PLA.sub.2 's) and are therefore useful in the treatment of inflammatory diseases, such as psosiasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia/reperfusion, and trauma induced inflammation, such as spinal cord injury.Type: GrantFiled: July 15, 1992Date of Patent: June 28, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Mathew Carson, Ru-Jen L. Han, Ronald A. LeMahieu, Vincent S. Madison
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Patent number: 5324840Abstract: Compounds that provide non-teratogenic effects and lack irritation to the skin are shown in the formula below where the partially drawn ring signifies an aromatic ring which may be carbocyclic or heteroaromatic, 6-membered or 5-membered, and may be condensed with another ring. R.sub.1 is lower alkyl, Cl, Br, or I, R.sub.2 is H, lower alkyl, Cl, Br, or I, and R.sub.3 is lower alkyl, Cl, Br, I, or is an ether, thioether, ester, thioester, amine or substituted amine group.Type: GrantFiled: June 11, 1992Date of Patent: June 28, 1994Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna