Hydroxy, Bonded Directly To Carbon, Or Ether In Substituent Q (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/165)
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Patent number: 5880156Abstract: Substituted benzoylguanidines, process for their preparation, their use as a pharmaceutical or diagnostic, and pharmaceutical containing them Benzoylguanidines of the formula I ##STR1## are described in which: R(1), R(2), R(3), R(4) are as defined in the specification, and pharmaceutically tolerated salts thereof.Type: GrantFiled: January 30, 1996Date of Patent: March 9, 1999Assignee: Hoechst AktiengesellschaftInventors: Hans-Jochen Lang, Heinz-Werner Kleemann, Wolfgang Scholz, Udo Albus
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Patent number: 5866611Abstract: Compounds of formula I, and their pharmaceutically acceptable salts, ##STR1## in which R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkenyl; or NR.sup.1 R.sup.2 is a heterocyclic group; A is trimethylene optionally substituted by alkyl and the phenyl ring is optionally substituted by substituents such as halogeno, alkenyl, amino, cyano, ureido, alkyl, carbamoylalkyl, alkanoylamino, alkoxycarbonyl, N-alkyl-alkanoylamino, alkanoyl and amines thereof; are inhibitors of squalene synthese and hence useful in treating diseases in which a lowering of cholesterol is desirable. As well as the use of these compounds in medicine, novel compounds, processes for their preparation and pharmaceutical compositions are also referred to.Type: GrantFiled: May 19, 1994Date of Patent: February 2, 1999Assignee: Zeneca LimitedInventors: George Robert Brown, Murdoch Allan Eakin, Peter John Harrison, deceased, Keith Blakeney Mallion
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Patent number: 5866610Abstract: Substituted benzoylguanidines, process for their preparation, their use as a pharmaceutical or diagnostic, and pharmaceutical containing them.Described are benzoylguanidines of the formula I ##STR1## where R(1) to R(3) are H, Hal, (cyclo)alkyl, N.sub.3, CN or OH, alkyloxy, phenyl, phenoxy or benzoyl, and their pharmacologically acceptable salts, but with the exception of the compounds benzoylguanidine, 4-chlorobenzoylguanidine, 3,4-dichlorobenzoylguanidine and 3- or 4-methylbenzoylguanidine.They are obtained by reacting a compound II ##STR2## with guanidine, L being a leaving group.Type: GrantFiled: July 18, 1996Date of Patent: February 2, 1999Assignee: Hoechst AktiengesellschaftInventors: Hans-Jochen Lang, Andreas Weichert, Heinz-Werner Kleemann, Jan-Robert Schwark, Wolfgang Scholz, Udo Albus
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Patent number: 5856573Abstract: A process for producing a compound of the formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen or alkyl, and R is hydrogen or alkyl, which comprises removing the protective group (P) of hydroxyl of a compound of the formula (II): ##STR2## wherein P is a protective group of hydroxyl, .about. indicates an E-isomer, Z-isomer or a mixture thereof, and the other symbols are as defined above; and an intermediate for the production of the compound of the formula (I).Type: GrantFiled: June 10, 1997Date of Patent: January 5, 1999Assignee: Shionogi & Co., LtdInventors: Akira Takase, Hiroyuki Kai, Takami Murashi
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Patent number: 5831094Abstract: The present invention relates to difluorostatone derivatives useful as antiviral agents.Type: GrantFiled: February 20, 1996Date of Patent: November 3, 1998Assignee: Merrell Pharamceuticals Inc.Inventors: Viviane Van Dorsselaer, Daniel Schirlin, Celine Tarnus
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Patent number: 5808080Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective .beta.3 adrenergic receptor agonists useful in the treatment of Type II diabetes and obesity.Type: GrantFiled: May 2, 1997Date of Patent: September 15, 1998Assignee: Eli Lilly and CompanyInventors: Michael Gregory Bell, Thomas Alan Crowell, David Andrew Neel, Mark Alan Winter
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Patent number: 5773476Abstract: The present invention concerns compounds and their use to inhibit the activity of a receptor tyrosine kinase. The invention is preferably used to treat cell proliferative disorders such as cancers charcterized by over-activity or inappropriate activity HER2 or EGFR.Type: GrantFiled: June 7, 1995Date of Patent: June 30, 1998Assignees: Sugen, Inc., Yissum Research and Development Company of the Hebrew University of JerusalemInventors: Hui Chen, Aviv Gazit, Alexander Levitzki, Klaus Peter Hirth, Elaina Mann, Laura K. Shawver, Jianming Tsai, Peng Cho Tang
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Patent number: 5770615Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof. These compounds are beta three adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity and gastrointestinal diseases.Type: GrantFiled: March 28, 1997Date of Patent: June 23, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Peter T. W. Cheng, Gregory S. Bisacchi, Ashvinikumar V. Gavai, Kathleen M. Poss, Denis E. Ryono, Philip M. Sher, Chong-qing Sun, William N. Washburn
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Patent number: 5770614Abstract: A novel 2-(substituted phenyl)-2-alkoxyiino-N-alkylacetamide compounds having a wide fungicidal spectrum and especially an excellent activity of controlling Pseudocercosporella herpotrichoides; and a composition containing the compound for controlling Pseudocercosporella herpotrichoides.Type: GrantFiled: November 12, 1996Date of Patent: June 23, 1998Assignee: Shionogi & Co., Ltd.Inventors: Akira Murabayashi, Akira Takase, Hideyuki Takenaka, Michio Masuko
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Patent number: 5767254Abstract: A compound of the formula ##STR1## is disclosed. X is selected from the group consisting of aryl, alkyl, imte ester, imino ester, amidine, azide, isocyanate, and dithiocarbonate. R' is a group selected from the group consisting of groups containing a hydroxyl moiety, groups containing a protected hydroxyl moiety, and groups containing an O-linked sugar. G is a carbon chain of 0-10 carbons and R is not a methyl group and is a group capable of removal under conditions compatible with glycopeptide synthesis. In a preferred form the compound, R is selected from the group consisting of benzylic or allyl groups and X is CPh.sub.2. A method of forming a glycocide from the compound is also disclosed.Type: GrantFiled: June 6, 1995Date of Patent: June 16, 1998Assignee: The Arizona Board of Regents on Behalf of the University of ArizonaInventor: Robin L. Polt
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Patent number: 5739374Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: February 14, 1997Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5736568Abstract: Compounds of the formula I ##STR1## including pharmaceutically acceptable salts thereof are disclosed in which R.sub.1, R.sub.2, R.sub.3, and R.sub.4 independently represent hydrogen, hydroxy, halo, halogenated alkyl, halogenated alkoxy, alkyl, alkoxy, cyano, a carbamoyl group, carbonyl group, or R.sub.1 and R.sub.2 together with the phenyl ring represent a naphthalene ring (optionally substituted); L.sub.1 represents C.sub.2-6 alkylene; R.sub.5 represents hydrogen or alkyl, R.sub.6 represents hydrogen or alkyl, phenylalkyl (optionally substituted) or R.sub.5 and R.sub.6 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring; L.sub.2 represents a C.sub.1-6 alkylene chain; and R.sub.7 and R.sub.8 independently represent hydrogen or alkyl or R.sub.7 and R.sub.8 together with the nitrogen atom to which they are attached represent a saturated 3-7 membered heterocyclic ring.Type: GrantFiled: November 25, 1996Date of Patent: April 7, 1998Assignee: Knoll AktiengesellschaftInventors: Paul Rafferty, Gerald Bernard Tometzki
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Patent number: 5723489Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R.sup.1 to R.sup.9 are as defined herein and m is the integer 0 or 1.These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity, gastrointestinal diseases and achalasia.Type: GrantFiled: May 7, 1996Date of Patent: March 3, 1998Assignee: Bristol-Myers Squibb CompanyInventors: Philip M. Sher, William N. Washburn, Kathleen M. Poss
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Patent number: 5705528Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein thyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: ##STR1## wherein R.sup.1 represents farnesyl, geranyl or geranyl-geranyl;Z represents C--R.sup.6 or N;R.sup.2 represents H, CN, the groups COOR.sup.7, SO.sub.3 R.sup.7, CONR.sup.7 R.sup.8 and SO.sub.2 NR.sup.7 R.sup.7, wherein R.sup.7 and R.sup.8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO.sub.3 M, wherein M is a cation;R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato;X represents O, S, SO, SO.sub.2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.Type: GrantFiled: November 10, 1994Date of Patent: January 6, 1998Assignee: Ramot University Authority for Applied Research & Industrial DevelopmentInventor: Yoel Kloog
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Patent number: 5696161Abstract: Substituted phenoxymethylphenyl derivatives I ##STR1## X is .dbd.CH--OCH.sub.3, .dbd.CH--CH.sub.3 or .dbd.N--OCH.sub.3 ; R.sup.1 is, inter alia,R.sup.2 and R.sup.3 are, inter alia,H, halogen, CN, NO.sub.2, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.2 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.2 -haloalkoxy;R.sup.4 is, inter alia,CN, Cl, Br, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio or C.sub.1 -C.sub.4 -haloalkoxy;R.sup.5 is, inter alia,NO.sub.2, CN, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -haloalkoxy;n is 0-4; Y is --O--, --NH--, --N(CH.sub.3)--; R.sup.6 is H, C.sub.1 -C.sub.4 -alkyl.The compounds are useful for controlling pests and fungi.Type: GrantFiled: May 13, 1996Date of Patent: December 9, 1997Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Klaus Oberdorf, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Harald Rang, Volker Harries, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5686633Abstract: Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.3 ' and R.sub.4 ' are as defined in claim 1. The compounds are in part novel and are suitable for use as light stabilizers for organic materials.Type: GrantFiled: December 31, 1991Date of Patent: November 11, 1997Assignee: Ciba Specialty Chemicals CorporationInventors: Eric Vieira, Hugh Stephen Laver
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Patent number: 5679857Abstract: L-amino acid amides are converted to the corresponding D-amino acid amides. An amide formed from an L-amino acid and an optically active (S)-.alpha.-alkylbenzylamine is subjected to dehydration condensation with an aryl aldehyde to form a Schiff's base, which is racemized at the amino acid moiety in the presence of a base to yield an N-allylidene-D-amino acid-(S)-amide. The less-soluble diastereomer N-allylidene-D-amino acid-(S)-amide is crystallized from the reaction mixture and recovered by means of solid/liquid separation. The N-allylidene form is readily hydrolyzed into the amino acid-(S)-amide and the starting aldehyde.Type: GrantFiled: November 16, 1995Date of Patent: October 21, 1997Assignee: Ajinomoto Co., Inc.Inventors: Toyoto Hijiya, Chiaki Mochizuki, Tadashi Takemoto
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Patent number: 5677347Abstract: Ortho-substituted phenylacetamides I ##STR1## (R.sup.1 =H, alkyl, cycloalkyl, alkenyl, alkynyl, phenylalkynyl, alkoxyalkyl, alkoxycarbonyl, phenyl, phenylalkyl, phenylalkenyl or phenoxyalkyl, 5- or 6-membered heterocycle with 1-3 hetero atoms to which a benzene ring or a 5- or 6-membered heterocycle can be fused; R.sup.2 and R.sup.3 =H, CN, halogen, alkyl, alkoxy; R.sub.4 and R.sup.5 =H, alkyl and R.sup.4 or R.sup.5 =alkoxy; Y=O, S, SO, SO.sub.2, N.dbd.N, O--CO, CO--O, CO--O--CH.sub.2, alkylene or haloalkylene, alkenylene, alkynylene, oxy- alkylene, thio-alkylene, alkyleneoxy, carbonylalkylene or alkylenecarbonyl, W=alkoxyimino, alkoxymethylene or alkylthiomethylene), excepting compounds where R.sup.1 is hydrogen, phenyl or 2,2-dimethyl-3-(2,2-dichlorovinyl)cyclopropyl, R.sup.2 to R.sup.5 are each hydrogen, Y is carbonyloxymethylene and W is methoxymethylene or methylthiomethylene,are suitable as fungicides and for controlling pests.Type: GrantFiled: January 22, 1996Date of Patent: October 14, 1997Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Eberhard Ammermann, Gisela Lorenz, Hubert Sauter, Klaus Oberdorf, Uwe Kardorff, Christoph Kuenast
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Patent number: 5674905Abstract: Compounds of formula (I), wherein A is selected from (a), (b), (c), (d), (e), (f) and B is selected from (g), (h), and (i), wherein W is a carbonyl, sulphonyl or sulphinyl group, and X is a carbonyl, sulphonyl or sulphinyl group or --C(O)--CH.sub.2 -- (in which the carbonyl group is bonded to Y), provided that at least one of W and X contains carbonyl, Y is R.sub.9 --O-- or R.sub.9 --N(R.sub.10)--, Z is selected from (i), (ii), (iii), (iv) or Z is absent and W is H, with a number of provisions and phamaceutically acceptable salts thereof are ligands at CCK and/or gastrin receptors.Type: GrantFiled: December 19, 1994Date of Patent: October 7, 1997Assignee: James Black Foundation LimitedInventors: Sarkis Barret Kalindjian, Caroline Minli Rachel Low, Michael John Pether, Jonathan Michael Richard Davies, David John Dunstone, Iain Mair McDonald
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Patent number: 5670546Abstract: N-arylalkylphenylacetamide compounds of formula (I), and pharmaceutically acceptable salts thereof, possess potent analgesic and anti-inflammatory activities.Type: GrantFiled: January 11, 1996Date of Patent: September 23, 1997Assignee: Korean Research Institute of Chemical TechnologyInventors: No-Sang Park, Young-Sik Jung, Churl-Min Seong, Jong-Cheol Lee, Jin-Il Choi, Seung-Won Choi, Yeon-Joo Choi, Kwang-Sook Lee
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Patent number: 5656619Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: June 6, 1995Date of Patent: August 12, 1997Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5650539Abstract: A compound of the formula [I] ##STR1## wherein X is hydrogen, lower alkyl, lower alkoxy or halogen; R is lower alkyl; and .about. is any configuration of E-isomer, Z-isomer or a mixture thereof is produced by reacting a compound of the formula ##STR2## wherein X and .about. are defined above, W is --CN or --COOR; and R is a lower alkyl, with methylamine in the presence of methanol. The compound [I] is useful for an agricultural fungicide. An intermediate used for producing the compound [I] is also disclosed.Type: GrantFiled: November 28, 1995Date of Patent: July 22, 1997Assignee: Shionogi & Co., Ltd.Inventors: Akira Takase, Hiroyuki Kai, Kuniyoshi Nishida, Shoji Shinomoto, Masahiko Nagai
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Patent number: 5639768Abstract: The invention relates to the compounds of formula (I) wherein the C(.dbd.NH)--NHR.sub.3 group may be in tautomeric or isomeric form, and pharmaceutically acceptable salts thereof, in which: R.sub.1 is amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen; R.sub.2 is hydroxy which is etherified by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy; R.sub.3 is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid; X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--); and X.sub.2 is a divalent aliphatic hydrocarbon radical which may be interrupted by an aromatic radical.Type: GrantFiled: July 25, 1995Date of Patent: June 17, 1997Assignee: Ciba-Geigy CorporationInventors: Michael M. Morrissey, Hongsuk Suh
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Patent number: 5639904Abstract: The 1-aryloxy-3-alkylamino-2-propanol nitrate esters, having formula I: ##STR1## the enantiomers and diastereoisomers and the therapeutically acceptable salts thereof, wherein R.sub.1 is a chain of general formula II --(CH.sub.2).sub.m --Z--R.sub.2, where: m is 1 or 2; Z is an --O-- ether, --CONH amide or --COO-- ester function; and R.sub.2 is a C.sub.2-3 straight or branched chain alkyl having at least one nitroxy group as substituent; and Ar is a benzene ring when Z is the ether or ester function, and a naphthalene ring when Z is the amide function, are of use for the treatment of cardiovascular affections.Type: GrantFiled: August 11, 1995Date of Patent: June 17, 1997Assignee: Prodesfarma, S.A.Inventors: Maria Prat Quinones, Joan Pi Sallent, Dagmar Vedrilla Veit
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Patent number: 5633288Abstract: This invention relates to a tri(lower alkoxy)benzene derivative of the general formula (I), or its salt, optical isomer or solvate, ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 : same or different and each represents a lower alkyl group;A: a group of the formula ##STR2## and R.sup.4 and R.sup.5 : same or different and each represents a lower alkyl group, an aralkyl group or an aryl group, provided that R.sup.4 and R.sup.5 may, taken together with the adjacent nitrogen atom, form a pyrrolidinyl group, a piperidino group, a morpholino group, a thiomorpholino group, or a piperazinyl group optionally substituted by a lower alkyl group in 4-position;to pharmaceutical compositions containing the same, and to processes for their production. The compound of the invention is useful as value as a pulmonary-surfactant secretion promoting agent.Type: GrantFiled: November 22, 1995Date of Patent: May 27, 1997Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Hiromu Hara, Tatsuya Maruyama, Munetoshi Saito, Toshiyasu Mase
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Patent number: 5610183Abstract: Compounds of Formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein Q is optionally substituted phenyl or naphthyl;X and Y are each H, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or X and Y are together .dbd.O;Z is O or S;R.sup.1 is H, optionally substituted C.sub.1-6 alkyl, optionally substituted phenyl (C.sub.1-4 alkyl), C.sub.2-6 alkenyl, COC.sub.1-6 alkylhalo, COR.sup.a, COOR.sup.a, CONHR.sup.a, COC.sub.1-6 alkylNR.sup.a R.sup.b or CONR.sup.a C.sub.1-6 alkylCONR.sup.a R.sup.b ;R.sup.2 is substituted C.sub.1-6 alkyl, optionally substituted phenyl(C.sub.1-4 alkyl), C.sub.2-6 alkenyl, C.sub.1-6 alkylhalo, COR.sup.a, COOR.sup.a, CONHR.sup.a, COC.sub.1-6 alkylNR.sup.a R.sup.b or CONR.sup.a C.sub.1-6 alkylCONR.sup.a R.sup.b ;or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.p optionally substituted by oxo;R.sup.3 is H [or C.sub.1-6 alkyl];R.sup.4 is H, C.sub.1-6 alkyl or phenyl; andR.sup.5 is optionally substituted (CH.sub.2).sub.Type: GrantFiled: December 17, 1993Date of Patent: March 11, 1997Assignee: Merck, Sharp & Dohme Ltd.Inventors: Andrew P. Owens, Brian J. Williams
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Patent number: 5602181Abstract: Naphthyl ethers of the general formula I ##STR1## where the index and the substituents have the meanings defined in the specification.Type: GrantFiled: October 12, 1994Date of Patent: February 11, 1997Assignee: BASF AktiengesellschaftInventors: Wassilios Grammenos, Reinhard Kirstgen, Hartmann K onig, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5587514Abstract: A process for the synthesis of hydroxyethylene dipeptide isosteres from .alpha.-N,N-di(protected)-amino(alkyl or substituted alkyl)methyl ketones that can be efficiently carried out on an industrial scale. The process proceeds with excellent diastereoselectivity and chemical efficiency, and can be used to prepare a wide variety of hydroxyethylene dipeptide isosteres for a variety of uses, including as HIV-1 protease inhibitors and renin inhibitors.Type: GrantFiled: November 8, 1993Date of Patent: December 24, 1996Assignee: Emory UniversityInventors: Dennis C. Liotta, Bharat R. Lagu
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Patent number: 5567734Abstract: Phenyl-substituted alkylcarboguanidides carrying perfluoroalkyl groups, of the formula I ##STR1## are described where R(A) and R(B) are H, Hal, CN, OR(6), alkyl, O.sub.r -perfluoroalkyl or NR(7)R(8); R(6) is hydrogen, (cyclo)alk(en)yl, perfluoroalkyl, phenyl or benzyl; R(7) and R(8) are defined as R(6); X is 1-3; R(1) is H, alkyl or --O.sub.0-1 (CH.sub.2)O.sub.0-1 perfluoroalkyl; R(2), R(3), R(4) and R(5) are defined as R(1), with the condition, however, that R(1), R(2), R(3), R(4) and R(5) are not simultaneously hydrogen and that R(1), R(2), R(3), R(4) and R(5) can only be alkyl when at least one of the substituents R(A) or R(B) contains a O.sub.r (CH.sub.2).sub.a C.sub.b F.sub.2b+1 group; as are the pharmaceutically acceptable salts thereof. Methods of preparation of compounds of formula I are also described.Type: GrantFiled: January 23, 1995Date of Patent: October 22, 1996Assignee: Hoechst AktiengesellschaftInventors: Jan-Robert Schwark, Heinz-Werner Kleemann, Hans-Jochen Lang, Andreas Weichert, Wolfgang Scholz, Udo Albus
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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: 5548078Abstract: A fungicidal composition for agricultural use, which comprises a compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each hydrogen, lower alkyl or cyclo(lower)alkyl; R.sup.3 is lower alkyl or cyclo(lower)alkyl; R.sup.4 and R.sup.5 are each hydrogen, lower alkyl, lower alkoxy, halogen-substituted lower alkyl, lower alkyl-substituted silyl, halogen or nitro; A represents an unsaturated hydrocarbon group, a halogen-substituted unsaturated hydrocarbon group, a phenyl group or a heterocyclic group, among which the phenyl group and the heterocyclic group may be optionally substituted with not more than three substituents; and Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, --NR-- (R being hydrogen or lower alkyl), --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --OCH.sub.2 --, --SCH.sub.2 -- or --SOCH.sub.2 --.Type: GrantFiled: December 20, 1994Date of Patent: August 20, 1996Assignee: Shionogi Seiyaku Kabushiki KaishaInventors: Yoshio Hayase, Takahiro Kataoka, Hideyuki Takenaka, Mitsuhiro Ichinari, Michio Masuko, Toshio Takahashi, Norihiko Tanimoto
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Patent number: 5545664Abstract: Substituted phenoxymethylphenyl derivatives I ##STR1## X is .dbd.CH--OCH.sub.3, .dbd.C--CH.sub.3 or .dbd.N--OCH.sub.3 ; R.sup.1 is, inter alia,R.sup.2 and R.sup.3 are, inter alia,H, halogen, CN, NO.sub.2, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.2 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 --C.sub.2 -haloalkoxy;R.sup.4 is, inter alia,CN, Cl, Dr, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkylthio or C.sub.1 -C.sub.4 -haloalkoxy;R.sup.5 is, inter alia,NO.sub.2, CN, halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.1 -C.sub.4 -haloalkoxy;n is 0-4; Y is --O--, --NH--, --N(CH.sub.3)--; R.sup.6 is H, C.sub.1 -C.sub.4 -alkyl.The compounds are useful for controlling pests and fungi.Type: GrantFiled: March 23, 1995Date of Patent: August 13, 1996Assignee: BASF AktiengesellschaftInventors: Reinhard Kirstgen, Klaus Oberdorf, Hubert Sauter, Herbert Bayer, Wassilios Grammenos, Harald Rang, Volker Harries, Gisela Lorenz, Eberhard Ammermann
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Patent number: 5527945Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: August 31, 1994Date of Patent: June 18, 1996Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5516805Abstract: 3,5-Substituted aminobenzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing themThere are described benzoylguanidines of the formula I ##STR1## where one of the substituents R(1), R(2), R(3) or R(4) is: an amino group ##STR2## where R(5), R(6)=inter alia, H or alkyl, or alternatively R(5) and R(6), together with the nitrogen atom, are a 5-7-membered ring, and the other substituents R(1), R(2), R(3) and R(4) in each case are: H, Hal, CN, CF.sub.3, NO.sub.2, CF.sub.3 --O--, C.sub.m F.sub.2m+1 --CH.sub.2 --O--, R(11)--C.sub.q H.sub.2q --X.sub.p --, X=O or NR(12), R(11)=H, (cyclo)alkyl, phenyl, and where R(1) and R(4) are not simultaneously hydrogen.The compounds I have very good antiarrhythmic and cardio-protective properties, but no undesired salidiuretic properties.Type: GrantFiled: May 25, 1995Date of Patent: May 14, 1996Assignee: Hoechst AktiengesellschaftInventors: Hans-Jochen Lang, Heinrich Englert, Andreas Weichert, Heinz-Werner Kleemann, Wolfgang Scholz, Udo Albus
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Patent number: 5514683Abstract: The compounds of the formula I ##STR1## and their pharmaceutical acceptable salts, which are defined herein, are ligands for cholecystokinin and/or gastrin receptors.Type: GrantFiled: August 9, 1994Date of Patent: May 7, 1996Assignee: James Black Foundation LimitedInventors: Sarkis B. Kalindjian, Caroline M. R. Low, Iain M. McDonald, Robert A. D. Hull, Nigel P. Shankley, Ildiko M. Buck, Katherine I. M. Steel, Jonathan M. R. Davies, David J. Dunstone, Elaine A. Harper, Michael J. Pether, Michael J. Bodkin, Matthew J. Tozer, Martin L. Hudson
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Patent number: 5514716Abstract: This disclosure relates to a novel class of hydroxamic and carboxylic acid based matrix metalloproteinase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in the treatment of matrix metalloproteinase induced diseases.Type: GrantFiled: February 25, 1994Date of Patent: May 7, 1996Assignee: Sterling Winthrop, Inc.Inventors: Madhusudhan R. Gowravaram, Jeffrey Johnson, Ewell R. Cook, Robert C. Wahl, Alan M. Mathiowetz, Bruce E. Tomczuk, Ashis K. Saha
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Patent number: 5502237Abstract: The 1-aryloxy-3-alkylamino-2-propanol nitrate esters of general formula I ##STR1## the enantiomers and diastereoisomers and the therapeutically acceptable salts thereof wherein R.sub.1 is a chain of general formula II-- (CH).sub.m,--Z--R.sub.2, where: m is 1 or 2; Z is an --O-- ether, --CONH-amide or --COO-- ester function; and R.sub.2 is a C.sub.2-3 straight or branched chain alkyl having at least one --ONO.sub.2 group as a substituent; and Ar is a benzene ring when Z is the ether or ester function, and a naphthalene ring when Z is the amide function, are of use for the treatment of cardiovascular affections.Type: GrantFiled: June 27, 1994Date of Patent: March 26, 1996Assignee: Prodesfarma, S. A.Inventors: Mari/ a Prat Quin, Joan Pi Sallent, Dagmar V. Veit
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Patent number: 5498792Abstract: There is disclosed a process of producing an N-alkylacetamide of the general formula (III): ##STR1## wherein X.sup.1, X.sup.2 and X.sup.3 are the same or different and are independently hydrogen, lower alkyl, lower alkoxy, lower alkenyl, halogen or trifluoromethyl; R.sup.1 and R.sup.2 are the same or different and are independently lower alkyl; and represents a chemical bond of E- or Z-configuration, or a mixture of these configurations, which includes the steps of:(a) reacting an acetonitrile of the general formula (I): ##STR2## wherein X.sup.1, X.sup.2, X.sup.3, R.sup.1 and are each as defined above, with an alkylamine of the general formula (IV):R.sup.2 --NH.sub.2 (IV)wherein R.sup.2 is as defined above, to give an N-alkylacetamidine of the general formula (II): ##STR3## wherein X.sup.1, X.sup.2, X.sup.3, R.sup.1, R.sup.2 and are each as defined above; and(b) reacting the N-alkylacetamidine (II) with a nitrite derivative in the presence of an acid.Type: GrantFiled: September 16, 1994Date of Patent: March 12, 1996Assignees: Shionogi & Co., Ltd., Sumitomo Chemical Co., Ltd.Inventors: Katuhisa Masumoto, Akihiko Nakamura, Yujiro Kiyoshima, Mikio Sasaki, Asako Tanahashi
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Patent number: 5495047Abstract: Fused tricyclic compounds of formula (I) as disclosed herein, and salts and prodrugs thereof, are tachykinin antagonists, useful for treating pain.Type: GrantFiled: April 21, 1994Date of Patent: February 27, 1996Assignee: Merck, Sharp & Dohme (Ltd.)Inventors: Monique B. Van Niel, Brian J. Williams, Walfred S. Saari
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Patent number: 5492917Abstract: Novel compounds of the general structural formula I: ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.Type: GrantFiled: September 29, 1993Date of Patent: February 20, 1996Assignee: Merck & Co., Inc.Inventors: Ralph A. Rivero, Peter D. Williams, Daniel F. Veber
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Patent number: 5491166Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.Type: GrantFiled: December 22, 1992Date of Patent: February 13, 1996Assignee: Eli Lilly and CompanyInventors: Stephen W. Kaldor, Thomas E. Mabry
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Patent number: 5488159Abstract: A compound of the formula [I]: ##STR1## wherein X is hydrogen, lower alkyl, lower alkoxy or halogen; .about. is any configuration of E-isomer, Z-isomer or a mixture thereof is produced by reacting a compound of the formula [II] ##STR2## wherein X and .about. are as defined above; W is --CN or --COOR; and R is a lower alkyl, with methylamine in the presence of methanol. The compound [I] is useful for an agricultural fungicide. An intermediate used for producing the compound [I] is also disclosed.Type: GrantFiled: August 25, 1994Date of Patent: January 30, 1996Assignee: Shionogi & Co., Ltd.Inventors: Akira Takase, Hiroyuki Kai, Kuniyoshi Nishida, Shoji Shinomoto, Masahiko Nagai
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Patent number: 5488160Abstract: The invention relates to the compounds of the formula ##STR1##Type: GrantFiled: December 9, 1993Date of Patent: January 30, 1996Assignee: Ciba-Geigy CorporationInventor: Michael M. Morrissey
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Patent number: 5476860Abstract: Diaromatic compounds, characterized in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.Type: GrantFiled: December 8, 1993Date of Patent: December 19, 1995Assignee: Centre International de Recherches Dermatologiques (CIRD Galderma)Inventor: Jean-Michel Bernardon
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Patent number: 5476964Abstract: Benzyl alcohols having a chiral center at the benzylic carbon can be conveniently racemized by treatment with solid acids which are strongly acidic cation exchange materials. Racemization may be effected generally in the range from 20.degree.-150.degree. C. in aqueous or partly aqueous systems in combination with a water-miscible organic solvent to improve solubility of the alcohol. Similar racemizations may be effected for benzyl ethers and esters. This process is valuable for recycling of unwanted enantiomers obtained in the resolution of racemic mixtures.Type: GrantFiled: November 21, 1994Date of Patent: December 19, 1995Assignee: UOPInventor: David W. House
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Patent number: 5470949Abstract: A compound of the formula ##STR1## is disclosed. X is selected from the group consisting of aryl, alkyl, imidate ester, imino ester, amidine, azide, isocyanate, and dithiocarbonate. R' is a group selected from the group consisting of groups containing a hydroxyl moiety, groups containing a protected hydroxyl moiety, and groups containing an O-linked sugar. G is a carbon chain of 0-10 carbons and R is not a methyl group and is a group capable of removal under conditions compatible with glycopeptide synthesis. In a preferred form the compound, R is selected from the group consisting of benzylic or allyl groups and X is CPh.sub.2. A method of forming a glycocide from the compound is also disclosed.Type: GrantFiled: December 15, 1992Date of Patent: November 28, 1995Assignee: The Arizona Board of Regents on Behalf of the University of ArizonaInventor: Robin L. Polt
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Patent number: 5455274Abstract: The invention relates to the compounds of the formula ##STR1## wherein the C(=NOH)-NH.sub.2 group may be in tautomeric form, and pharmaceutically acceptable salts thereof, in which:R.sub.1 is amino or amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical or is amino which is disubstituted by a divalent aliphatic hydrocarbon radical or a said radical interrupted by oxygen;R.sub.2 is hydrogen, halogen, trifluoromethyl, an aliphatic hydrocarbon radical or hydroxy; or R.sub.2 is hydroxy which is etherified by an aliphatic alcohol, araliphatic alcohol, or aromatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid; or R.sub.2 is hydroxy which is etherified by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy;X.sub.1 and X.sub.Type: GrantFiled: December 9, 1992Date of Patent: October 3, 1995Assignee: Ciba-Geigy CorporationInventor: Hongsuk Suh
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Patent number: 5451700Abstract: The invention relates to the compounds of the formula ##STR1## wherein the C(.dbd.NH)--NHR.sub.3 group may be in tautomeric or isomeric form, and phamaceutically acceptable salts thereof. The compounds are useful as selective LTB.sub.4 receptor antagonists.Type: GrantFiled: November 18, 1992Date of Patent: September 19, 1995Assignee: Ciba-Geigy CorporationInventors: Michael M. Morrissey, Hongsuk Suh
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Patent number: 5449692Abstract: The invention provides new compounds of formula (I) ##STR1## wherein n is an integer of 1 to 4; each of R and R.sub.1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy; R2 is hydrogen or C.sub.1 -C.sub.4 alkyl; and a pharmaceutically acceptable salts thereof; and wherein when, at the same time, R is hydrogen, R.sub.1 is hydrogen or halogen and n is one, then R.sub.2 is other than hydrogen or methyl; and of formula (IA) ##STR2## wherein R.sub.3 is halogen, and a pharmaceutical acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.Type: GrantFiled: March 22, 1994Date of Patent: September 12, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Mario Varasi, Philippe Dostert, Paolo Pevarello, Alberto Bonsignori
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Patent number: 5446066Abstract: The invention provides new compounds of formula (I) ##STR1## wherein, subject to a proviso, n is zero or an integer of 1 to 3; each of R and R.sub.1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy; R.sub.2 is hydrogen or C.sub.1 -C.sub.4 alkyl optionally substituted by hydroxy; each of R.sub.3 and R.sub.4 independently is hydrogen or C.sub.1 -C.sub.4 alkyl; or a pharmaceutically acceptable salt thereof; and of formula (IA) ##STR2## wherein R.sub.5 is hydrogen, halogen, trifluoromethyl or C.sub.1 -C.sub.4 alkoxy, or a pharmaceutically acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.Type: GrantFiled: March 22, 1994Date of Patent: August 29, 1995Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Mario Varasi, Philippe Dostert, Paolo Pevarello, Alberto Bonsignori