Sulfur In R Patents (Class 514/618)
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Patent number: 5753715Abstract: The invention relates to cyclohexenyl antibacterial compounds of the formula I: ##STR1## and pharmaceutical compositions containing the compounds, methods for their production and use.Type: GrantFiled: June 2, 1995Date of Patent: May 19, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Robert H. Chen, Maud Urbanski, Min Xiang, John Francis Barrett
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Patent number: 5747541Abstract: The present invention relates to substituted benzoylguanidines, a process for their preparation, their use as medicament or diagnostic agent, and medicament comprising them.Type: GrantFiled: June 12, 1997Date of Patent: May 5, 1998Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Joachim Brendel, Heinz-Werner Kleemann, Hans Jochen Lang, Jan-Robert Schwark, Udo Albus, Wolfgang Scholz
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Patent number: 5747539Abstract: Fluorine-containing benzoylguanidines of the formula I ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 have the meanings indicated, and their physiologically acceptable salts, have antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter, for example.Type: GrantFiled: May 15, 1996Date of Patent: May 5, 1998Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Dieter Dorsch, Manfred Baumgarth, Rolf Gericke, Klaus-Otto Minck, Norbert Beier
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Patent number: 5744339Abstract: The present invention is directed to thiomethylene group-containing aldehyde inhibitors of cysteine or serine proteases. Methods for the use of the protease inhibitors are also described.Type: GrantFiled: August 30, 1996Date of Patent: April 28, 1998Assignee: Cephalon, Inc.Inventor: Sankar Chatterjee
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Patent number: 5739140Abstract: Novel compounds of Formula I and methods of making and using the compounds which are useful as fungicides, particularly in the agricultural field: ##STR1## wherein C.sub.1 and C.sub.2 are carbon atoms which are part of an aromatic ring; W is alkoxyimino, alkoxymethylene or alkylthiomethylene; R.sub.1 is independently selected from the group consisting of halogen, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, wherein the alkyl or alkoxy are optionally substituted by halogen, and p is 0, 1, or 2; Z is --CH.sub.2 --, --CH(OH)--, --CO--, --O--, --S--, NR.sub.2 wherein R.sub.2 is hydrogen or a lower aliphatic group, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, ##STR2## --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 S(O)--, --OCH.sub.2 --, --SCH.sub.2 --, --S(O)CH.sub.2 --, --CH.sub.2 ON.dbd.C(R.sub.3)-- or --CH.dbd.NB wherein B is --O--CO--, --N.dbd.CR.sub.3, or --CR.sub.3 R.sub.4 -- wherein R.sub.3 and R.sub.4 are independently hydrogen or C.sub.1 -C.sub.Type: GrantFiled: October 23, 1996Date of Patent: April 14, 1998Assignee: Monsanto CompanyInventors: William P. Clinton, Jim I. McLoughlin, Anita E. Otal, John J. Parlow, Dennis P. Phillion, Ajit S. Shah
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Patent number: 5734081Abstract: Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N,R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.Type: GrantFiled: June 1, 1995Date of Patent: March 31, 1998Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Edward Faith Elslager, Rocco Dean Gogliotti
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Patent number: 5733935Abstract: A hydroxylamine derivatives of formula (I): ##STR1## wherein R represents ##STR2## in which R.sup.1 and R.sup.2 represents alkyl group, alkenyl group, alkynyl group, cycloalkyl group, haloalkyl group, haloalkynyl group, alkoxy - alkyl group, phenoxy - alkyl group, alkylthio - alkyl group, alkylsulfonyl - alkyl group, alkylamino - alkyl group, phenyl group, benzyl group, phenethyl group, cinnamyl group, pyridyl group, furyl group, thienyl group, X represents CO.sub.2, CO or SO.sub.2, and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 represent a hydrogen atom or a lower alkyl group, and n represents 0 or 1, and fungicides contain said compound as an active ingredient.The compounds of the present invention have excellent effects for controlling wood-rot fungi, plant diseases and fungi of humans and animals, and are useful as industrial, agricultural and medical fungicides.Type: GrantFiled: June 17, 1996Date of Patent: March 31, 1998Assignee: Nihon Nohyaku Co., Ltd.Inventors: Nobuharu Andoh, Tsutomu Nishiguchi, Katsutoshi Endo
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Patent number: 5731351Abstract: Alkyl-benzoylguanidines of the formula I ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 have the meanings given, and physiologically acceptable salts thereof show antiarrhythmic properties and act as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.Type: GrantFiled: August 23, 1996Date of Patent: March 24, 1998Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Rolf Gericke, Manfred Baumgarth, Klaus-Otto Minck, Norbert Beier
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Patent number: 5728737Abstract: The present invention relates to novel N-alkoxy-arnidine derivatives of the formula (I), to a process for their preparation and to their use as pesticides. In addition, the invention also relates to novel intermediates and to a process for their preparation.Type: GrantFiled: January 23, 1997Date of Patent: March 17, 1998Assignee: Bayer AktiengesellschaftInventors: Ulrich Heinemann, Bernd-Wieland Kruger, Ralf Tiemann, Stefan Dutzmann, Klaus Stenzel
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Patent number: 5719168Abstract: The present invention relates to compounds of formula (I) wherein R.sub.1 is selected from H and 3-chloro; R.sub.2 is selected from a phenyl group and a pyridyl group; R.sub.3 and R.sub.4 are selected independently of each other from H and methyl; R.sub.5 and R.sub.6 are selected independently of each other from H and a pyridyl-methyl group or both represent an ethyl group; n=0 or 1; R.sub.1, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are not simultaneously H when R.sub.2 is phenyl. The salts of the compounds have a pyridyl group with pharmaceutical acceptable acids are also disclosed.Type: GrantFiled: April 22, 1996Date of Patent: February 17, 1998Assignee: Laboratoire L. LafonInventor: Philippe Laurent
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Patent number: 5709867Abstract: Novel pharmaceutically/cosmetically-active polyaromatic amides have the structural formula (I): ##STR1## wherein Z is a radical --CO--NH-- or --NH--CO--, and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: December 15, 1994Date of Patent: January 20, 1998Assignee: Centre International De Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 5708034Abstract: Substituted sulfonimidamides, processes for their preparation, their use as a medicament or diagnostic, and medicament comprising themSulfonimidamides of the formula I ##STR1## in which at least one of the three substituents R(1), R(2) and R(3) is a benzoylguanidine, and in which the other substituents have the meanings indicated in the claims, are outstandingly suitable as medicaments having action on the cardiovascular system; that is as antiarrhythmic pharmaceuticals having a cardioprotective component as well as for treating ischemically induced damage; also in operative interventions, such as organ transplantation.Type: GrantFiled: October 31, 1996Date of Patent: January 13, 1998Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Joachim Brendel, Jan-Robert Schwark, Andreas Weichert, Hans Jochen Lang, Udo Albus, Wolfgang Scholz
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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: 5700839Abstract: Benzoylguanidines of the formula I ##STR1## wherein R.sup.1 and R.sup.2 have the meanings indicated herein, and their physiologically acceptable salts, show anti-arrhythmic properties and act as inhibitors of the cellular NA.sup.+ /H.sup.+ antiporter.Type: GrantFiled: October 20, 1995Date of Patent: December 23, 1997Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Rolf Gericke, Dieter Dorsch, Manfred Baumgarth, Klaus-Otto Minck, Norbert Beier
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Patent number: 5696167Abstract: 4-Mercaptobenzoylguanidines of the formula I ##STR1## in which A, R.sub.1, R.sub.2 and R.sub.3 have the meanings given, and the physiologically unobjectionable salts thereof exhibit antiarrhythmic properties and are active as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.Type: GrantFiled: January 30, 1996Date of Patent: December 9, 1997Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rolf Gericke, Manfred Baumgarth, Klaus-Otto Minck, Norbert Beier
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Patent number: 5693672Abstract: 3,4,5-Substituted benzoylguanidines, process for their preparation, their use as a medicament or diagnostic and medicament containing themBenzoylguanidines of the formula I ##STR1## where R(1) is R(4)--SO.sub.m or R(5)R(6)N--SO.sub.2 --, where R(4) and R(5) are alk(en)yl, --C.sub.n H.sub.2n --R(7), and where R(7) is cycloalkyl or phenyl, where R(5) is also H, R(6) is H or C.sub.1 --C.sub.4 --alkyl,R(2) is hydrogen, (cyclo)-alk(en)(yn)yl, aryl and hetaryl,R(3) is defined as R(2)and their pharmaceutically tolerable salts are described.Type: GrantFiled: May 26, 1995Date of Patent: December 2, 1997Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Hans-Jochen Lang, Wolfgang Scholz, Udo Albus, Florian Lang
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Patent number: 5683713Abstract: A pharmaceutical and cosmetical preparation which rapidly penetrates through human skin, and which thus is able to bring about the rapid transdermal penetration of a wide variety of active ingredients. The compounds which enhance the rate of dermal penetration are also anti-oxidative agents and thus protect active substances susceptible to oxidative degradation. Preferred agents enhancing penetration and which protect against oxidation are higher esters and higher amides of thioglycolic acid and of mercaptopropionic acid. The preparations can be in the form of mixtures or there may be prepared chemical compounds which are a combination of the active substance and the said thioacids.Type: GrantFiled: October 24, 1996Date of Patent: November 4, 1997Inventors: Izhak Blank, Alon Blank
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Patent number: 5677303Abstract: Enolethers and thioenolethers of formula I ##STR1## are disclosed. The compounds are useful for combatting phytopathogenic fungi.Type: GrantFiled: June 20, 1996Date of Patent: October 14, 1997Assignee: American Cyanamid CompanyInventors: Juergen Curtze, Guido Albert
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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: 5670544Abstract: There are described benzoylguanidines of the formula I ##STR1## where R(1) is hydrogen, Hal, --NO.sub.2, --CN, --CF.sub.3, R(4)--SO.sub.m or R(5)R(6)N--SO.sub.2 --, where m is zero to 2, R(4) and R(5) are alk(en)yl or --C.sub.n H.sub.2n --R(7), n is zero to 4, where R(5) also has the meaning of H,R(6) is H or (C.sub.1 -C.sub.4)-alkyl, where R(5) and R(6) together can be 4 or 5 methylene groups,R(2) is --SR(10), --OR(10), --NRH(10), --NR(10)R(11), --CHR(10)R(12), ##STR2## where R(10) and R(11) are identical or different and are--?CHR(16)!.sub.s --(CH.sub.2).sub.p --(CHOH).sub.q --(CH.sub.2).sub.r --(CH.sub.2 OH).sub.t --R(21) or --(CH.sub.2).sub.p --O--(CH.sub.2 --CH.sub.2 O).sub.q --R(21)R(12) and R(13) are hydrogen or alkyl or, together with the carbon atom carrying them, form a cycloalkyl,R(14) is H, (cyclo)alkyl or --C.sub.n H.sub.2n --R(15),R(3) is defined as R(1), or is alkyl, hydrogen or --X--R(22) where X is oxygen, S or NR(16),and their pharmaceutically tolerable salts.Type: GrantFiled: May 26, 1995Date of Patent: September 23, 1997Assignee: Hoechst AktiengesellschaftInventors: Andreas Weichert, Hans-Jochen Lang, Heinz-Werner Kleemann, Wolfgang Scholz, Udo Albus
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Patent number: 5670545Abstract: Bucillamine and N-2,2-dimethyl-3-mercaptopropionyl)-L-cysteine or related compounds can be used to prevent damage to living tissue from the formation or presence of reactive oxygen species. These reactive oxygen species are formed when tissue is first rendered hypoxic due to interruption of blood flow and then reoxygenated by restoration of blood flow. In particular, the invention is directed to the administration of bucillamine and N-2,2-dimethyl-3-mercaptopropionyl)-L-cysteine prior to or coincidental with reperfusion to prevent damage to myocardium from formation of reactive oxygen species. Also presented are application of these compounds to similar ischemia-related cell injury in other organs.Type: GrantFiled: February 9, 1996Date of Patent: September 23, 1997Assignee: Board of Regents of the University of ColoradoInventor: Lawrence D. Horwitz
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Patent number: 5668291Abstract: Arylthiol and dithiobisarylamide antibacterial and antiviral agents have the general formula ##STR1## where A is monocyclic or bicyclic aryl which can contain up to 3 heteroatoms selected from O, S, and N, R.sup.1 and R.sup.2 are substituent groups, X is ##STR2## or SO.sub.2 NR.sup.4 Z, Y is H or SZ when n is 1, a single bond when n is 2; R.sup.4 and Z can be hydrogen or alkyl.Type: GrantFiled: June 7, 1995Date of Patent: September 16, 1997Assignee: Warner-Lambert CompanyInventors: John Michael Domagala, Edward Faith Elslager, Rocco Dean Gogliotti
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Patent number: 5668178Abstract: Phenylthiols and dithiobisbenzamides are potent antibacterial and antiviral agents.Type: GrantFiled: May 19, 1995Date of Patent: September 16, 1997Assignee: Warner-Lambert CompanyInventors: Edward Faith Elslager, Rocco Dean Gogliotti
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Patent number: 5641792Abstract: Benzoylguanidines substituted by heterocyclic N-oxide, process for their preparation, their use as a medicament or diagnostic agent, medicament containing them and intermediate products for their preparationBenzoylguanidines of the formula I ##STR1## with the meanings given in the text for the substituents, are described. These are compounds which have an outstanding activity on the cardiovascular system.Type: GrantFiled: September 8, 1995Date of Patent: June 24, 1997Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 5629347Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is R.sup.9 CR.sup.10 R.sup.11 or CH.sub.2 R.sup.9 CR.sup.10 R.sup.11 where R.sup.9 is H or OH and R.sup.10 and R.sup.11 are optionally substituted phenyl, optionally substituted benzyl, C.sub.5-7 cycoalkyl or (C.sub.5-7 cycloalkyl)methyl; R.sup.1 and R.sup.2 are H, optionally substituted C.sub.1-6 alkyl, optionally substituted phenyl(C.sub.1-4 alkyl), C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, COR.sup.a, COOR.sup.a, COC.sub.1-6 alkylhalo, COC.sub.1-6 alkylNR.sup.a R.sup.b, CONR.sup.12 C.sub.1-6 alkylCONR.sup.a R.sup.b, CONR.sup.a R.sup.b, or SO.sub.2 R.sup.a, or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.q optionally substituted by oxo where one methylene group may optionally be replaced by O or NR.sup.x ; R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; R.sup.4 is optionally substituted phenyl(C.sub.1-3 alkyl); X and Y are H, or X and Y together are .dbd.O; and Z is O, S, or NR.sup.7 ; are tachykinin antagonists.Type: GrantFiled: December 22, 1993Date of Patent: May 13, 1997Assignee: Merck Sharp & Dohme Ltd.Inventors: Christopher J. Swain, Martin R. Teall, Brian J. Williams
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Patent number: 5624961Abstract: Novel benzylaminoethoxybenzene derivatives of the formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl, a lower hydroxyalkyl, a lower alkoxyalkyl, an allyl or a benzyl; R.sup.2 is a hydrogen atom, a lower alkyl, a lower acyl, an allyl or a benzyl; R.sup.3 is a hydrogen atom, a lower alkyl, a lower alkoxyalkyl, a lower dialkylaminoalkyl or a lower acyl; and R.sup.4 is a hydrogen atom, a halogen atom, a lower alkoxy, an amino, a lower acylamino, a hydroxy, a lower acyloxy, a lower acyl, a carboxy or a lower alkoxycarbonyl, salts thereof and solvates thereof. An .alpha..sub.1 -adrenoceptor blocker obtained from this compound has a strong .alpha..sub.1 -adrenoceptor blocking effect and causes less side effects such as orthostatic hypotension.Type: GrantFiled: December 11, 1995Date of Patent: April 29, 1997Assignee: Japan Tobacco Inc.Inventors: Masakazu Ban, Kiyotaka Shinoda, Mitsuru Takahashi, Shuhei Deguchi, Hiroaki Taguchi, Takeo Katsushima
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Patent number: 5621011Abstract: The invention relates to [.alpha.-(tert.butyl aminomethyl)-3,4-dichlorobenzyl] thioacetamide of the formula: ##STR1## and its addition salts with pharmaceutically acceptable acids. These compounds can be used as antidepressants as well as to promote the feed intake.Type: GrantFiled: June 29, 1995Date of Patent: April 15, 1997Assignee: Laboratoire L. LafonInventor: Louis L. Lafon
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Patent number: 5618845Abstract: Pharmaceutical compositions comprising modafinil in the form of particles of defined size. The particle size of modafinil can have a significant effect on the potency and safety profile of the drug.Type: GrantFiled: October 6, 1994Date of Patent: April 8, 1997Assignee: Cephalon, Inc.Inventors: Peter E. Grebow, Vincent Corvari, David Stong
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Patent number: 5612379Abstract: The present invention relates to the utilization of modafinil for the treatment of ventilation disorders of central origin such as sleep apnea.Type: GrantFiled: April 30, 1996Date of Patent: March 18, 1997Assignee: Laboratoire L. LafonInventor: Philippe Laurent
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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: 5601811Abstract: Substantive UV-absorbing cinnamido amine cationic quaternary salts are disclosed. Detergent and household cleaning product compositions and hair and skin personal care product compositions, as well as sunscreen and tanning lotion compositions, containing the compounds of the present invention are also described.Type: GrantFiled: August 1, 1994Date of Patent: February 11, 1997Assignee: Croda, Inc.Inventors: Kevin F. Gallagher, Abel G. Pereira
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Patent number: 5591754Abstract: Benzoylguanidines, process for their preparation, their use as a medicament and medicament containing them.The invention relates to benzoylguanidines of the formula I ##STR1## where R(1) or R(2) is R(3)-S(O).sub.n -- or R(4)R(5)N--O.sub.2 S-- and the other substituent R(1) or R(2) in each case is H, OH, F, Cl, Br, I, alkyl, alkoxy, benzyloxy or phenoxy, R(3)-S(O).sub.n or R(4)R(5)N-- or 3,4-dehydropiperidine and R(3) is alkyl, cycloalkyl, cyclopentylmethyl, cyclohexylmethyl or phenyl, R(4) and R(5) are alkyl or phenylalkyl or phenyl,and in which R (4) and R (5) can also together be a C.sub.4 -C.sub.7 -chain, and in which R(4) and R(5), together with the nitrogen atom to which they are bonded, can be a dihydroindole, tetrahydroquinoline or tetrahydroisoquinoline system,and where n is zero, 1 or 2 and their pharmaceutically tolerable salts are excellent antiarrhythmics.Type: GrantFiled: May 5, 1995Date of Patent: January 7, 1997Assignee: Hoechst AktiengesellschaftInventors: Hans-Jochen Lang, Andreas Weichert, Heinz-Werner Kleemann, Heinrich Englert, Wolfgang Scholz, Udo Albus
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Patent number: 5571842Abstract: Perfluoroalkyl-substituted benzoylguanidines, a process for their preparation, their use as a medicament or diagnostic agent, and a medicament containing themA description is given of perfluoroalkyl-substituted benzoylguanidines of the formula I ##STR1## where R(1) is (C.sub.1 -C.sub.6)-perfluoroalkyl-SO.sub.m ; R(2) and R(3) are H, halogen, alk(yl)(oxy), phenoxy; R(4) and R(5) are H, alkyl, Hal, CN, OR(7), NR(8)R(9), --(CH.sub.2).sub.n --(CF.sub.2).sub.o --CF.sub.3 and of the pharmacologically acceptable salts thereof; the compounds I are obtained by reacting a compound II ##STR2## with guanidine, L being a leaving group which is able readily to undergo nucleophilic substitution.Type: GrantFiled: May 11, 1995Date of Patent: November 5, 1996Assignee: Hoechst AktiengesellschaftInventors: Heinz-Werner Kleemann, Hans-Jochen Lang, Jan-Robert Schwark, Andreas Weichert, Wolfgang Scholz, Udo Albus
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Patent number: 5516804Abstract: 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.dbd.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: December 6, 1994Date of Patent: May 14, 1996Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Eberhard Ammermann, Gisela Lorenz, Hubert Sauter, Klaus Oberdorf, Uwe Kardorff, Christoph Kuenast
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Patent number: 5508275Abstract: Lipid-selective antioxidants of the formula I(A).sub.a (L)(X).sub.a, (I),in whichA=an antioxidative component,L=a bridging member,X=a lipophilic componenta and a'=independently of one another the numbers 1 or 2.The compounds are used for the protection of lipid-containing substances against oxidation and in pharmaceuticals for the prophylaxis and treatment of diseases in which bioradicals are involved, in particular of coronary, circulatory and vascular diseases.Type: GrantFiled: March 15, 1994Date of Patent: April 16, 1996Assignee: Hoechst AktiengesellschaftInventors: Klaus-Ulrich Weithmann, Gunther Wess, Dirk Seiffge
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Patent number: 5506267Abstract: A compound of the invention is represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different, an acyl group; R.sup.3, R.sup.4, R.sup.6 and R.sup.7 are the same or different, hydrogen or an alkyl group; R.sup.5 is hydrogen, an alkyl group or a hydroxyl group which may optionally be protected, or R.sup.4 and R.sup.5 are combined to form a chemical bond; X is a carbonyl group or a sulfonyl group; Y is an amino acid sequence consisting of 1 to 7 amino acid residues which may optionally be protected and having optionally an intervening --SO.sub.2 NH--; n is an integer of 0 to 2, or a salt thereof.Type: GrantFiled: September 8, 1994Date of Patent: April 9, 1996Assignee: Takeda Chemical Industries, Ltd.Inventors: Tetsuya Aono, Koichi Yukishige, Seiichi Tanida
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Patent number: 5504115Abstract: 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: June 28, 1994Date of Patent: April 2, 1996Assignee: Merck & Co., Inc.Inventors: Albert A. Deana, deceased, S. Jane deSolms, Samuel L. Graham, Robert L. Smith
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Patent number: 5502061Abstract: The present invention provides HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.Type: GrantFiled: September 26, 1994Date of Patent: March 26, 1996Assignee: Eli Lilly and CompanyInventors: Kwan Y. Hui, Charles D. Jones, Louis N. Jungheim, Pamela A. Pennington
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Patent number: 5502079Abstract: 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: November 17, 1994Date of Patent: March 26, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Philippe Dostert, Paolo Pevarello, Franco Heidempergher, Mario Varasi, Alberto Bonsignori, Romeo Roncucci
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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: 5489612Abstract: Calixarene derivatives, their synthesis and use as chloride channel blockers are described. Preferred calixarene derivatives are of the formula: ##STR1## wherein R is an acidic group or salt thereof, such as SO.sub.3 X or R.sup.1 SO.sub.3 X where X is H or Na, and R.sup.1 is ##STR2## where m=1-2, and R.sup.3 and R.sup.4 the same or different is each H or a C.sub.1-4 alkyl, or a nitrogen-containing group of the formula ##STR3## or A, wherein R.sup.5 is a C.sub.1-4 alkyl, R.sup.6 is a C.sub.1-4 alkyl and A is ##STR4## where R.sup.7 and R.sup.8, the same or different each is H or a C.sub.1-4 alkyl, and R.sup.9 and R.sup.10, the same or different, each is H or a C.sub.1-4 alkyl; R' is H or a C.sub.1-4 alkyl; and n is an integer of 4-8, preferably 4, 6 or 8.Type: GrantFiled: January 7, 1994Date of Patent: February 6, 1996Assignee: The University of Alabama at Birmingham Research FoundationInventors: Jerry L. Atwood, Robert J. Bridges, Ravindra K. Juneja, Ashvani K. Singh
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Patent number: 5488066Abstract: Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing cycloalkylalkyl alanine amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: ##STR1## wherein m is two or three; wherein x is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is selected from cycloalkylalkyl groups containing from three to about twelve carbon atoms; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.9 and R.sup.10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: January 23, 1995Date of Patent: January 30, 1996Assignee: G. D. Searle & Co.Inventors: Barbara B. Chen, Gunnar J. Hanson, John S. Baran
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Patent number: 5488067Abstract: Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing propargyl amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: ##STR1## wherein q is two or three; wherein r is zero or two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is propargyl or a propargyl containing moiety; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.12 and R.sup.13 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: January 23, 1995Date of Patent: January 30, 1996Assignee: G. D. Searle & Co.Inventor: Gunnar J. Hanson
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Patent number: 5482942Abstract: This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.Type: GrantFiled: June 28, 1994Date of Patent: January 9, 1996Assignee: American Home Products CorporationInventors: Richard M. Soll, Paul J. Dollings
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Patent number: 5478835Abstract: Disclosed is a tricyclic compound represented by the formula (I): ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represents hydrogen, C1-6 alkyl, C1-6 alkoxy, C1-6 alkylthio, amino, C1-6 alkylamino, halogenated C1-6 alkyl, halogenated C1-6 alkoxy, halogen, nitro, cyano, carboxy, C1-6 alkoxycarbonyl, hydroxymethyl, CR.sup.9 R.sup.10 CO.sub.2 R.sup.11 (wherein each of R.sup.9, R.sup.10 and R.sup.11 independently represents hydrogen or C1-6 alkyl) or CONR.sup.12 R.sup.13 (wherein each of R.sup.12 and R.sup.13 independently represents hydrogen or C1-6-alkyl); R.sup.5 represents hydrogen or C1-6 alkyl; each of R.sup.6, R.sup.7 and R.sup.8 independently represents hydrogen, C1-6 alkyl, hydroxy, C1-6 alkoxy, C1-6 alkanoyloxy, C1-6 alkylthio, thiocyanato or halogen; X represents CH or N; Y.sup.1 -Y.sup.2 represents CH.sub.2 -O, CH.sub.2 -S(O).sub.n, (wherein n represents 0, 1, or 2), CH.sub.2 CH.sub.2, CH.dbd.CH or CON(R.sup.14) (wherein R.sup.Type: GrantFiled: May 2, 1994Date of Patent: December 26, 1995Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Toshiaki Kumazawa, Masashi Yanase, Hiroyuki Harakawa, Hiroyuki Obase, Shoji Oda, Shiro Shirakura, Koji Yamada, Kazuhiro Kubo
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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: 5476944Abstract: The present invention relates to derivatives of cyclic phenolic thioethers of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, which are inhibitors or stimulators of superoxide generation, and which may also inhibit cyclooxygenase and/or 5-lipoxygenase, to pharmaceutical compositions containing one or more of these compounds in combination with a pharmaceutically-acceptable carrier, and to medical methods of treatment employing these compounds.Type: GrantFiled: May 19, 1994Date of Patent: December 19, 1995Assignee: G. D. Searle & Co.Inventors: Richard A. Partis, Richard A. Mueller, Francis J. Koszyk, Richard M. Weier
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Patent number: 5475034Abstract: Novel ester and amide derivatives of 3-benzoylphenylacetic acid are disclosed. The use of these novel derivatives and certain known derivatives in topically administrable compositions for the treatment of ophthalmic inflammatory disorders is also disclosed.Type: GrantFiled: June 6, 1994Date of Patent: December 12, 1995Assignee: Alcon Laboratories, Inc.Inventors: John M. Yanni, Gustav Graff, Mark R. Hellberg
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Patent number: 5466715Abstract: Certain 3,4-disubstituted phenols and pharmaceutically acceptable salts thereof are provided which mimic IL-1 activity by inducing IL-2 synthesis and subsequent IL-2 receptor expression. Specifically, the invention provides compounds of Formula I and acid addition salts thereof: ##STR1## wherein Y is ##STR2## NHSO.sub.2 or SO.sub.2 NH where R.sup.4 is H; Z is --O--, --NH--, --NR--, --S--, or other heteroatoms capable of hydrogen bonding with R.sup.4 to give a preferred conformation;R is alkyl;R.sup.1 is --OH;R.sup.2 is H, alkyl, cycloalkyl, aralkyl, substituted or unsubstituted aryl, or a substituted or unsubstituted nitrogen heterocyclic group having 4 to 5 nuclear carbon atoms; andR.sup.3 is a lipophilic moiety selected from the group consisting of substituted C.sub.1 -C.sub.10 alkyl, C.sub.3 -C.sub.16 cycloalkyl and 2,4-di-t-pentylphenyl.Type: GrantFiled: March 8, 1994Date of Patent: November 14, 1995Assignee: Sterling Winthrop Inc.Inventors: William N. Washburn, Barbara B. Lussier, Carl R. Illig, Lee H. Latimer
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Patent number: 5461075Abstract: The present invention provides methods of preventing lesions due to herpes simplex infections in humans and lower animals by treatment with natural and synthetic vanilloid compounds.Type: GrantFiled: March 14, 1991Date of Patent: October 24, 1995Assignee: The Procter & Gamble CompanyInventors: Timothy P. O'Neill, Gerald B. Kasting, Thomas L. Cupps