The Additional Hetero Ring Consists Of One Oxygen And Four Carbons Patents (Class 546/214)
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Patent number: 5350852Abstract: The invention relates to a process for making compounds of formula: ##STR1##Type: GrantFiled: August 13, 1993Date of Patent: September 27, 1994Assignee: SanofiInventors: Xavier Emonds-Alt, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5350758Abstract: The present invention relates to piperidyl sulfonamides and sulfoxamides which are useful as inhibitors of cholesterol biosynthesis and as agents which lower total serum cholesterol in patients in need thereof.Type: GrantFiled: December 18, 1992Date of Patent: September 27, 1994Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Marion W. Wannamaker, William A. VanSickle, William R. Moore
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Patent number: 5336686Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein the substituents are defined as in the application having antiglucocorticoid and antiprogestomimetic properties and a process and intermediates for their preparation.Type: GrantFiled: February 19, 1993Date of Patent: August 9, 1994Assignee: Roussel-UclafInventors: Lucien Nedelec, Francois Nique, Daniel Philibert
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Patent number: 5332817Abstract: The present invention relates to novel 3-amino-piperidine derivatives and related nitrogen containing heterocyclic compounds, and specifically, to compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, Y and m are as defined below. These novel compounds are useful in the treatment of inflammatory and central nervous system disorders, as well as other disorders. The invention also relates to novel intermediates used in the synthesis of compounds of the formula I.Type: GrantFiled: February 8, 1993Date of Patent: July 26, 1994Assignee: Pfizer Inc.Inventors: Manoj C. Desai, Terry J. Rosen
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Patent number: 5328916Abstract: New heterocyclic compounds of the formulaX--W--CR.sup.1 R.sup.2 --CO--Y--NR.sup.3 --CHR.sup.4 --CR.sup.5 --CH.sub.2 --(CR.sup.6 R.sup.7).sub.r --Z--Het Iin which R.sup.1 to R.sup.7, W, X, Y, Z, r and Het have the meanings defined herein, and the salts thereof, inhibit the activity of human plasma renin.Type: GrantFiled: May 2, 1991Date of Patent: July 12, 1994Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Peter Raddatz, Claus J. Schmitges, Klaus-Otto Minck
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Patent number: 5300500Abstract: Novel podophyllotoxin compounds and their use in treating tumors are disclosed.Type: GrantFiled: December 8, 1992Date of Patent: April 5, 1994Assignees: The University of North Carolina at Chapel Hill, Yale UniversityInventors: Kuo-Hsiung Lee, Yung-Chi Cheng, Yi-Lin Zhang
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Patent number: 5294719Abstract: Compounds useful as a stabilizer for a variety of organic materials of an intermediate thereof, or as an intermediate of medicines or agricultural chemicals are disclosed, which are cyclohexylamine derivatives represented by the general formula [I]: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an acyl group having 2 to 7 carbon atoms or an arylalkyl group having 7 to 10 carbon atoms; R.sup.2 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; R.sup.3 and R.sup.4 both represent a hydrogen atom, or one of R.sup.3 and R.sup.4 represents a hydrogen atom and the other represents a group --CH.sub.2 --R.sup.5, or R.sup.3 and R.sup.4 together form a group .dbd.CH--R.sup.5, in which R.sup.5 represents an unsubstituted or C.sub.1 -C.sub.4 alkyl substituted phenyl group, a 2-furyl group, a cyclohexyl group or a 2-tetrahydrofuryl group; X represents an alkylene group having 1 to 3 carbon atoms; and n denotes 1 or 2.Type: GrantFiled: December 23, 1992Date of Patent: March 15, 1994Assignee: Mitsubishi Petrochemical Company LimitedInventors: Hideki Kurokawa, Mitsumasa Kaitoh, Akiyoshi Ohnishi
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Patent number: 5290796Abstract: The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein R.sup.1 is lower-alkyl, or phenyl-lower-alkyl;R.sup.2, R.sup.3 and R.sup.4 are the same or different lower-alkyl;n is zero or one;R.sup.5 is hydrogen, lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl, lower-alkoxy, phenyl, phenyl-lower-alkyl, phenyl-lower-alkyl in which the phenyl ring is substituted in the 2, 3, or 4-position by one to two, the same or different, halogen substituents, or R.sup.5 is a 5-membered aromatic monocyclic heterocycle selected from the group consisting of thienyl, furanyl and isoxazolyl;R.sup.6 is hydrogen or lower-alkyl; or when n is zero, R.sup.5 and R.sup.6 together are --(CH.sub.2).sub.m -- wherein m is an integer from four to six; with the proviso that when R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are methyl, n is zero and R.sup.6 is hydrogen or methyl, R.sup.5 cannot be hydrogen; further provided that when n is zero, R.sup.Type: GrantFiled: November 20, 1992Date of Patent: March 1, 1994Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne, Martha R. Heimann
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Patent number: 5286733Abstract: The invention is related to compounds, being useful in treating psychosis, of the formula: ##STR1## wherein: R.sup.1 is hydrogen, lower-alkyl, phenyl-lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl-lower-alkyl, or hydroxy-C.sub.3 -C.sub.7 -monocycliccycloalkyl-lower-alkyl;R.sup.2 is lower-alkyl;R.sup.3 is hydrogen or lower-alkyl;R.sup.4 is lower-alkyl;n is an integer from zero to three; andR.sup.5 is hydroxy, lower-alkoxy, lower-alkyl, C.sub.3 -C.sub.7 -monocyclic cycloalkyl, phenyl, or a 5-membered heterocycle selected from furanyl, thienyl and isoxazolyl;with the proviso that when n is zero, R.sup.5 is other than hydroxy or a pharmaceutically acceptable acid-addition salt thereof.Type: GrantFiled: November 20, 1992Date of Patent: February 15, 1994Assignee: Sterling Winthrop Inc.Inventors: Diane L. DeHaven-Hudkins, John P. Mallamo, William F. Michne, Martha R. Heimann
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Patent number: 5260443Abstract: Disclosed is a piperidine derivatives of a formula: ##STR1## wherein R.sup.0 indicates a hydrogen atom or a group R--CO).sub.n where R is an alkyl, alkylene or arylene group capable of having 1 to 4 carboxylic group;R.sup.1 indicates a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an acyl group having 2 to 7 carbon atoms, or an arylalkyl group having 7 to 10 carbon atoms;R.sup.2 and R.sup.2' respectively indicate a hydrogen atom, or an alkyl group having 1 to 4 carbon atoms;R.sup.3 and R.sup.4 in combination indicate a group .dbd.CH--R.sup.5, or R.sup.3 indicates a hydrogen atom and R.sup.4 indicates either --CH.sub.2 --R.sup.5 wherein R.sup.5 is a substituted or non-substituted phenyl group or a substituted or non-substituted cyclohexyl group the substituent being an alkyl having 1 to 4 carbon atoms, or a 2-furyl group or a tetrahydrofuryl group; andn indicates an integer of 1 to 4.The piperidine derivatives are improved photostabilizer to various organic materials including poly-.alpha.Type: GrantFiled: August 17, 1992Date of Patent: November 9, 1993Assignee: Mitsubishi Petrochemical Company LimitedInventors: Mitsumasa Kaitoh, Hideki Kurokawa, Akiyoshi Ohnishi
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Patent number: 5254569Abstract: This invention relates to (amidomethyl)nitrogen heterocyclic and pyrrolidine compounds, pharmaceutical compositions containing them, methods of using such compounds and processes for making such compounds.Type: GrantFiled: January 14, 1991Date of Patent: October 19, 1993Assignee: The Du Pont Merck Pharmaceutical CompanyInventors: Robert S. Cheeseman, Hollis S. Kezar, III, Richard M. Scribner
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Patent number: 5250683Abstract: A taxane derivative of the formula ##STR1## wherein R.sub.1 and R.sub.3 are independently selected from the group comprising phenyl, naphthalene, C.sub.6 H.sub.5 CHCH--, and ##STR2## provided, however, R.sub.1 and R.sub.3 are not both phenyl;Q is CH.sub.3 --, (CH.sub.3).sub.3 C--, CH.sub.3 O--, Cl, Br, F, NO.sub.2, ##STR3## Z is --OT.sub.1, T.sub.1 is hydrogen, hydroxyl protecting group, or --COT.sub.2,T.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, C.sub.1 -C.sub.6 alkynyl or monocylic aryl,Ac is acetyl, andE.sub.1 and E.sub.2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.Type: GrantFiled: April 3, 1992Date of Patent: October 5, 1993Assignee: Florida State UniversityInventors: Robert A. Holton, Hossain Nadizadeh, Seokchan Kim, Ronald J. Beidiger
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Patent number: 5243045Abstract: A taxane derivative of the formula ##STR1## wherein R.sub.1 is phenyl or substituted phenyl,R.sub.3 is CH.sub.3 O--, or CH.sub.3 CH.sub.2 O--,Z is --OT.sub.1,T.sub.1 is hydrogen, hydroxyl protecting group, or --COT.sub.2.T.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, C.sub.1 -C.sub.6 alkynyl or monocylic aryl,Ac is acetyl, andE.sub.1 and E.sub.2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.Type: GrantFiled: April 3, 1992Date of Patent: September 7, 1993Assignee: Florida State UniversityInventors: Robert A. Holton, Ronald J. Beidiger
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Patent number: 5236921Abstract: The invention relates to compounds of formula: ##STR1## in which Y represents--either a group Cy--N in whichCy represents a phenyl, optionally substituted; a C.sub.3 -C.sub.7 cycloalkyl group; a pyrimidinyl group or a pyridyl group;or a group ##STR2## in which Ar represents a phenyl, optionally substituted, a pyridyl group; a thienyl group;x is zero or one;X represents a hydroxyl, a C.sub.1 -C.sub.4 alkoxy; a hydroxyalkyl; a C.sub.1 -C.sub.4 acyloxy; a phenacyloxy; a carboxyl; a C.sub.1 -C.sub.4 carbalkoxy; a cyano; an aminoalkylene; a group --N--(X.sub.1).sub.2 in which the groups X.sub.1 independently represent hydrogen, a C.sub.1 -C.sub.4 alkyl; a group ##STR3## in which Alk represents a C.sub.1 -C.sub.6 alkyl; a group ##STR4## in which the Alk.sub.1 is a C.sub.1 -C.sub.3 alkylene and Alk'.sub.1 is a C.sub.1 -C.sub.3 alkyl; a C.sub.1 -C.sub.4 acyl; a group --S--X.sub.2 in which X.sub.2 represents hydrogen or a C.sub.1 -C.sub.Type: GrantFiled: September 5, 1991Date of Patent: August 17, 1993Assignee: SanofiInventors: Xavier Emonds-Ai, Pierre Goulaouic, Vincenzo Proietto, Didier Van Broeck
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Patent number: 5234895Abstract: Compounds having the formula ##STR1## in which: R.sub.1 is hydrogen or fluoro;R.sub.2 is halo, trihalomethyl, pentahaloethyl, mono- or difluoromethyl, di-, tri- or tetrafluoroethyl, C.sub.1 -C.sub.2 fluoroalkylthio, C.sub.1 -C.sub.2 fluoroalkoxy, methylthio, methylsulfonyl, halomethylsulfonyl, C.sub.1 -C.sub.2 alkyl or methoxy;R.sub.3 is hydrogen or halo;R.sub.4 is hydrogen, C.sub.1 -C.sub.4 alkyl; C.sub.2 -C.sub.4 alkenyl; C.sub.2 -C.sub.4 alkynyl; C.sub.1 -C.sub.4 haloalkyl; C.sub.2 -C.sub.4 haloalkenyl; C.sub.1 -C.sub.4 alkoxy; C.sub.2 -C.sub.4 alkoxyalkyl, 3-trifluoromethylphenyl, or --(CH.sub.2).sub.n Y;R.sub.5 and R.sub.6 are hydrogen, or R.sub.5 and R.sub.6 together form a bond;R.sub.7 is C.sub.1 -C.sub.4 alkyl;R.sub.8 and R.sub.9 are hydrogen, or R.sub.8 and R.sub.9 together form a bond;Y is cyano; 4-chlorophenyl; C.sub.3 -C.sub.6 cycloalkyl, furyl or tetrahydrofuryl optionally substituted by halo or C.sub.1 -C.sub.4 alkyl; or COR.sub.10 in which R.sub.10 is hydroxy, C.sub.1 -C.sub.5 alkoxy, C.sub.Type: GrantFiled: June 19, 1992Date of Patent: August 10, 1993Assignee: Imperial Chemical Industries PLCInventor: Raymond A. Felix
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Patent number: 5231105Abstract: An ethylamine derivative of formula (I): ##STR1## wherein A represents a carbon atom or a nitrogen atom;B represents a substituted or unsubstituted aralkyl or aryl group;C represents hydrogen, alkyl, aralkyl, or aryl, each of which may optionally be substituted orC may optionally be bonded to A to form an alkylene bridge which is optionally substituted,Q represents a substituted or unsubstituted aryl group, said group optionally being substituted by hetero atom(s) or substituent(s) optionally containing hetero atom(s); andX represents an alkylene bridge having from 2 to 20 carbon atoms and is optionally substituted with groups which include hetero atoms with the non-hetero atom substituents optionally containing hetero atoms.Type: GrantFiled: May 22, 1989Date of Patent: July 27, 1993Assignee: Ajinomoto Co., Inc.Inventors: Masataka Shoji, Kozo Toyota, Chikahiko Eguchi, Ryota Yoshimoto, Yosikatsu Koyama, Hideki Domoto, Akira Kamimura
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Patent number: 5227400Abstract: A taxane derivative of the formula ##STR1## wherein ##STR2## Z is --OT.sub.1, T.sub.1 is hydrogen, hydroxyl protecting group, or --COT.sub.2,T.sub.2 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkenyl, C.sub.1 -C.sub.6 alkynyl or monocylic aryl,R.sub.3 is benzoyl, substituted benzoyl or C.sub.1 -C.sub.6 alkoxycarbonyl,Ac is acetyl, andE.sub.1 and E.sub.2 are independently selected from hydrogen and functional groups which increase the water solubility of the taxane derivative are useful as antitumor agents.Type: GrantFiled: April 3, 1992Date of Patent: July 13, 1993Assignee: Florida State UniversityInventors: Robert A. Holton, Hossain Nadizadeh, Ronald J. Beidiger
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Patent number: 5227379Abstract: Piperidine compounds having the formula ##STR1## wherein R.sup.3 is 3,4-methylenedioxyphenyl, phenyl, or naphthyl which are optionally substituted with one or more halogen, C.sub.1-6 -alkoxy, or phenoxy, cyano, mono or poly halogenated C.sub.1-6 -alkyl, C.sub.2-6 -alkenyl, C.sub.1-6 -alkyl, or C.sub.3-5 -alkylene, R.sup.1 is straight or branched C.sub.1-8 -alkyl substituted with piperidinyl morpholinyl thiomorpholinyl dioxolanyl or tetrahydrofuranyl, which heterocyclic radical is unsubstituted or C.sub.1-6 -alkyl substituted,X is hydrogen, halogen, trifluoromethyl, hydroxy, cyano, or C.sub.1-8 -alkoxy,Y is O or S; and pharmaceutically-acceptable acid addition salts thereof.The compounds are useful in the treatment of anoxia, migraine, ischemia, and epilepsy.Type: GrantFiled: December 5, 1991Date of Patent: July 13, 1993Assignee: Novo Nordisk A/SInventors: Palle Jakobsen, Jorgen Drejer
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Patent number: 5216167Abstract: Phenylacetic acid benzylamides having the following general structure ##STR1## wherein the substituents are defined herein, are disclosed, which compounds are hypoglcemic agents.Type: GrantFiled: June 21, 1990Date of Patent: June 1, 1993Assignee: Dr. Karl Thomae GmbHInventors: Wolfgang Grell, Rudolf Hurnaus, Gerhart Griss, deceased, Robert Sauter, Manfred Reiffen, Eckhard Rupprecht
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Patent number: 5208232Abstract: Novel piperidine compounds having the formula ##STR1## wherein the symbols have the same meanings as set forth in the specification, and salts thereof with a pharmaceutically acceptable acid, are disclosed.The novel compounds are useful in the treatment of anoxia, migraine, ischemia and epilepsy.Type: GrantFiled: March 22, 1991Date of Patent: May 4, 1993Assignee: Novo Nordisk A/SInventors: Palle Jakobsen, Jorgen Dreger
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Patent number: 5207817Abstract: Herbicidal 5H-furan-2-one derivatives of the formula ##STR1## in which X represents the radical OR.sup.1 or the radical ##STR2## q represents the number 0 or 1, R.sup.2 is optionally substituted aryl, andR.sup.3 and R.sup.6 are hydrogen or various organic radicals,with certain provisos and exceptions.Type: GrantFiled: October 17, 1991Date of Patent: May 4, 1993Assignee: Bayer AktiengesellschaftInventors: Wolfgang Kramer, Gerd Kleefeld, Jurgen Bachmann, Peter Babczinski, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
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Patent number: 5196532Abstract: Compounds of formula I ##STR1## where R.sup.1 and R.sup.2 are each hydrogen or methyl, A is an ethylene or methylene radical which is unsubstituted or substituted by methyl, hydroxyl or oxo,L is a saturated or unsaturated five-membered or six-membered heterocyclic structure which is unsubstituted or substituted by hydroxyl, mercapto, C.sub.1 -C.sub.6 -alkyl, or C.sub.1 -C.sub.4 -alkanoyl and has from 1 to 3 heteroatoms from the group consisting of N, O and S, the second and third heteroatoms being a nitrogen atom,R.sup.3 is hydrogen, a hydroxy or C.sub.1 -C.sub.6 -alkoxy group,R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl, halogen or methoxy,R.sup.5 is hydrogen or methoxy or tert-butyl,R.sup.6 is hydrogen methyl, nitrile or a C.sub.2 -C.sub.10 -ketal group or the radical --CHR.sup.7 OR.sup.8 --CHR.sup.7 --NR.sup.9 R.sup.10, --COR.sup.11, --SR.sup.12, ##STR2## in which R.sup.7 is hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.8 is hydrogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.Type: GrantFiled: June 18, 1991Date of Patent: March 23, 1993Assignee: BASF AktiengesellschaftInventors: Hans-Heiner Wuest, Bernd Janssen, William V. Murray, Michael P. Wachter, Stanley Bell
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Patent number: 5190958Abstract: The invention provides piperidine derivatives of the general formula ##STR1## or an acid-addition salt or metal salt complex thereof, in which R represents a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl, alkoxy, cycloalkyl, aryl, arylcarbonyl, heterocyclyl or heterocyclyloxy group; R.sup.1 represents an optionally substituted alkyl, phenyl, benzyl or cycloalkyl group; R.sup.2 represents a hydrogen atom or an optionally substituted alkyl group; one of W and X represents --CH.sub.2 --, --CH.sub.2 CH.sub.2 -- or --O--, the other of W and X being --CH.sub.2 -- or --CH.sub.2 CH.sub.2 or X represents a single chemical bond; m is 0 or 1 and n represents an integer from 0 to 3; processes for their preparation; compositions containing such compounds and their use as fungicides.Type: GrantFiled: December 24, 1990Date of Patent: March 2, 1993Assignee: Shell Research LimitedInventors: Paul A. Carter, Surinder Singh
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Patent number: 5190961Abstract: Thiourea derivatives represented by the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a lower alkyl group, or R.sub.1 or R.sub.2 taken together represent a group having the formula --(CH.sub.2).sub.m --in which m is 4 or 5, R.sub.3 represents a lower alkyl group or a cycloalkyl group or a group having the formula--(CH.sub.2).sub.l --R.sub.4 in which R.sub.4 is a phenyl, naphthyl, pyridyl, furyl or thienyl group optionally having 1-3 substituents selected from the group consisting of lower alkyl, lower alkoxy, phenoxy, lower alkylthio, hydroxy, halogen, nitro, cyano and trifluoromethyl, and l represents an integer of 0 to 2 and n represents an integer of 1 to 5 or a physiologically acceptable salt thereof.The compounds of the invention are useful as a therapeutic agent for peptic ulcers which is also effective on prevention of the recurrence after discontinuation of the administration due to the antimicrobial activity against Helicobacter pyroli.Type: GrantFiled: August 2, 1991Date of Patent: March 2, 1993Assignee: Terumo Kabushiki KaishaInventors: Hirokazu Hasegawa, Isamu Endo, Shingo Koyama, Masashi Isozaki, Yukari Yoshiyama, Shigenori Nozawa, Norio Arakawa
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Patent number: 5189172Abstract: Disclosed is a piperidine derivatives of a formula: ##STR1## wherein: R.sup.o indicates a hydrogen atom or a group R--CO).sub.n where R is an alkyl, alkylene or arylene group capable of having 1 to 4 carboxylic group;R.sup.1 indicates a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an acyl group having 2 to 7 carbon atoms, or an arylalkyl group having 7 to 10 carbon atoms;R.sup.2 and R.sup.2' respectively indicate a hydrogen atom, or an alkyl group having 1 to 4 carbon atoms;R.sup.3 and R.sup.4 in combination indicate a group .dbd.CH--R.sup.5, or R.sup.3 indicates a hydrogen atom and R.sup.4 indicates either --CH.sub.2 --R.sup.5 wherein R.sup.5 is a substituted or non-substituted phenyl group or a substituted or non-substituted cyclohexyl group the substituent being an alkyl having 1 to 4 carbon atoms, or a 2-furyl group or a tetrahydrofuryl group; andn indicates an integer of 1 to 4.The piperidine derivatives are improved photostabilizer to various organic materials including poly-.alpha.Type: GrantFiled: June 3, 1992Date of Patent: February 23, 1993Assignee: Mitsubishi Petrochemical Company LimitedInventors: Mitsumasa Kaitoh, Hideki Kurokawa, Akiyoshi Ohnishi
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Patent number: 5185335Abstract: Piperidine derivatives of formula ##STR1## wherein A is a radical of formula ##STR2## wherein one or two hydrogen atoms in said radicals (a-1) to (a-3) may be replaced by a C.sub.1-6 alkyl radical;R.sup.1 is hydrogen or halo; R.sup.2 is hydrogen, amino, mono or di(C.sub.1-6 alkyl)amino or C.sub.1-6 alkylcarbonylamino; R.sup.3 is hydrogen or C.sub.1-6 alkyl; L is C.sub.3-6 cycloalkyl, C.sub.5-6 cycloalkanone, C.sub.3-6 alkenyl optionally substituted with aryl, or L is a radical of formula ##STR3## the N-oxide forms, addition salts and stereochemically isomeric forms thereof, said compounds having gastrointestinal motility stimulating properties. Pharmaceutical compositions containing these compounds as active ingredient, and a method of preparing said compounds and pharmaceutical compositions.Type: GrantFiled: February 4, 1991Date of Patent: February 9, 1993Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Jean-Paul R. M. A. Bosmans, Michel A. J. De Cleyn
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Patent number: 5166416Abstract: The invention relates to new propenone oxime ethers, a method of preparing them and pharmaceutical compositions containing them.Said new propenone oxime ethers have the formula ##STR1## in which--Ar and Ar' each independentlyl denotes a phenyl group non-substituted, mono or polysubstituted, a 9-anthryl group or a naphthyl group, a pyridyl, thienyl or furyl group;R.sub.1 R.sub.2 each independently denotes hydrogen, a C.sub.1 -C.sub.4 alkyl group or together with the N-atom to which they are bonded a 1-pyrrolidinyl, piperidino, morpholino or 1-piperazinyl group;M=H, Cl, Br or a C.sub.1 -C.sub.6 alkyl groupn=2 or 3.The invention also deals with the salts of compounds of formula (I). Said compounds have good activity in the anti platelet-clotting tests and are also antagonists of the 5HT.sub.2 receptors.Type: GrantFiled: December 1, 1989Date of Patent: November 24, 1992Assignee: Societe Anonyme: SanofiInventors: Christian Congy, Patrick Gueule, Bernard Labeeuw, Murielle Rinaldi
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Patent number: 5145975Abstract: The present invention relates to the treatment of diseases caused by invading organisms in a host by first identifying an enzymatic difference between the host and the invading organism and then administering to the host a pharmaceutically effective amount of a subversive substrate for the differing enzyme of the invading organism, whereby the action of the differing enzyme causes a result counter to the intended result and function of the enzyme that results in its debilitation or death. In particular, treatment of parasitic diseases caused by kinetoplastids including trypanosomes and leishmanias, e.g., African sleeping sickness, Chagas' disease, oriental sore and kala-azar is accomplished by administration of a pharmaceutically effective antiparasitic amount of a competitive toxigenic substrate for trypanothione reductase. Methods of treatment and compositions therefor contain a competitive toxigenic substrate for trypanothione reductase. Numerous compounds and corresponding compositions are disclosed.Type: GrantFiled: July 6, 1990Date of Patent: September 8, 1992Assignee: The Rockefeller UniversityInventors: Graeme B. Henderson, Peter C. Ulrich, Anthony Cerami
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Patent number: 5144037Abstract: Antiviral O-acylated derivatives of 1,5-dideoxy-1,5-imino-D-glucitol are disclosed that contain an N-alkyl or N-aroyl radical in which from one to four of the free hydroxyl groups are O-acylated with carboxylic alkanoyl radicals selected from the group consisting of .omega.,.omega.,.omega.-trifluoro alkanoyl having from three to eight carbon atoms, carboxylic cycloalkanoyl groups having from four to eight carbon atoms and carboxylic acyclic alkanoyl groups having from two to ten carbon atoms, wherein the N-aroyl radical is selected from the group consisting of p-decylbenzoyl, 3-(p-chlorophenoxy)propanoyl, 2-(acetyloxy)benzoyl, [1,1'-biphenyl]-4-ylcarbonyl, 2-thiopheneacetyl, trans-3-furanacryloyl, 3-methoxyphenylacetyl and 3-(trifluoromethyl)benzoyl, and wherein the N-alkyl contains from one to fourteen carbon atoms, provided that when N-alkyl contains from one to five carbon atoms the O-acylated groups are .omega.,.omega.,.omega.-trifluoro alkanoyl or carboxylic cycloalkanoyl.Type: GrantFiled: January 10, 1991Date of Patent: September 1, 1992Assignee: G. D. Searle & Co.Inventors: Richard A. Partis, Francis J. Koszyk, Richard A. Mueller
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Patent number: 5134128Abstract: New 5-hydroxy-2-furanone compounds having anti-inflammatory, immunosuppressive and anti-proliferative activity and are useful in treating psoriasis and modifying calcium homeostasis.Type: GrantFiled: May 13, 1991Date of Patent: July 28, 1992Assignee: Allergan, Inc.Inventors: Gary C. M. Lee, Michael E. Garst, John N. Bonfiglio, Elizabeth T. Syage
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Patent number: 5128348Abstract: Certain hexane and heptane amines including geometric and stereoisomers, agricultural compositions containing them and their use as fungicides.Type: GrantFiled: September 12, 1990Date of Patent: July 7, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventor: Gregory S. Basarab
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Patent number: 5120746Abstract: This invention relates to amine derivatives and salts thereof. These compounds have an anti-ulcer activity which is effective to human beings and animals. This disclosure relates to such compound, a process for the preparation thereof and an anti-ulcer agent containing the same.Type: GrantFiled: March 30, 1990Date of Patent: June 9, 1992Assignee: Toyama Chemical Co., Ltd.Inventors: Shiro Hirai, Hiroshi Hirano, Hirotoshi Arai, Yasuo Kiba, Hisanari Shibata, Yoshikazu Kusayanag, Minako Yotsuji, Kazuhiko Hashiba, Kikuko Tanada
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Patent number: 5110986Abstract: This application relates to a process for preparing a N-t-alkyl-1,2-diacylhydrazine by reacting a 1,3,4-oxadiazole with a tertiary alkyl cation precursor in the presence of a strong acid catalyst. Preferably, the 1,3,4-oxadiazole is a 2,5-disubstituted-1,3,4-oxadiazole and more preferably a 2,5-diaryl-1,3,4-oxadiazole. The strong acid catalyst is preferably a sulfur containing acid and more preferably sulfuric acid.Type: GrantFiled: April 26, 1988Date of Patent: May 5, 1992Assignee: Rohm and Haas CompanyInventor: Martha J. Kelly
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Patent number: 5106843Abstract: Aryl ureas and carbamic acid derivatives of formulaA--NHCW--Y--Band pharmaceutically acceptable salts thereof whereinA is a specified aromatic radical including 3,5-dichlorophenylW is O or SY is NH or O andB is a specified saturated azacyclic ring, e.g. tropan-3-yl or quinuclidin-3-yl,possess 5-HT.sub.3 -antagonistic activity and are, for example, useful in treatment of migraine, emesis, anxiety, gastro-intestinal disorders and as anti-psychotics.Type: GrantFiled: December 19, 1989Date of Patent: April 21, 1992Assignee: American Home Products CorporationInventors: Terence J. Ward, Janet C. White
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Patent number: 5098915Abstract: Substituted N-benzylpiperidine amides, which have activity as Class III antiarrhythmic agents, acting by prolonging cardiac action potential repolarization. The invention further provides for compositions incorporating the compunds and methods of their use, as well as providing for pharmaceutically acceptable salts of the compounds.Type: GrantFiled: September 5, 1989Date of Patent: March 24, 1992Assignee: G. D. Searle & Co.Inventors: Bipinchandra N. Desai, Kerry W. Fowler, Alan E. Moormann
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Patent number: 5091426Abstract: A method of preventing epileptic seizures in a human or lower animal subject susceptible to said seizures, comprising systemically administering to said subject a safe and effective amount of a compound of the formula: ##STR1## wherein (a) X is halo or nil, and Y is a substituent selected from the group consisting of unsubstituted or halogen-substituted methyl, halo, nitro, amino, and methoxy; and(b) R is R.sup.1 C(O)OH, R.sup.1 C(O)N(R.sup.2).sub.2, or R.sup.1 N(R.sup.2).sub.2 ; whereR.sup.1 is C.sub.1 -C.sub.3 alkylene which is unsubstituted or substituted with C.sub.1 -C.sub.2 alkyl; andeach R.sup.2 is, independently, hydrogen or lower alkyl; orboth R.sup.2 groups are connected to form a saturated 5- or 6-membered heterocycle containing 1 or 2 heteroatoms, wherein one of which is nitrogen and the other is selected from oxygen and nitrogen and said heterocycle is unsubstituted or substituted with lower alkyl or hydroxy-substituted lower alkyl;or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: June 23, 1989Date of Patent: February 25, 1992Assignee: Norwich Eaton Pharmaceuticals, Inc.Inventor: Stanford S. Pelosi, Jr.
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Patent number: 5075301Abstract: A furan derivative and a pharmaceutically acceptable salt thereof having gastrointestinal enterokinetic activity which is expected to be used in a broad spectrum of diseases associated with gastrointestinal dyskinesia.Type: GrantFiled: August 14, 1990Date of Patent: December 24, 1991Assignee: Kyowa Hakko Kogyo, Co., Ltd.Inventors: Setsuya Sasho, Shunji Ichikawa, Hiromasa Kato, Hiroyuki Obase, Katsuichi Shuto, Yoshimasa Oiji
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Patent number: 5053504Abstract: A process is disclosed for providing benzazepine intermediates of the formulae ##STR1## wherein R.sub.3, R.sub.4 and Y are as defined herein, which intermediates are useful in a process for the preparation of pharmaceutically useful benzazepine derivatives.Type: GrantFiled: November 29, 1989Date of Patent: October 1, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Wen-Sen Li, John K. Thottathil, Michael Murphy
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Patent number: 5043459Abstract: This invention relates to novel saccharoascorbic acid derivatives and their production. The derivatives are represented by the general formula set forth below, for example, an amido, a thioester or carboxylic ester of saccharoascorbic acid, and their salts.The compounds of the present invention are useful for food additives as antioxidants, an intermediate for the production of dichiral compounds and medicines having antithrombotic activity. ##STR1## wherein Z represents ##STR2## --SR.sub.6 or --OR.sub.7, R.sub.4 and R.sub.5 independently represent hydrogen or a hydrocarbon group of 1 to 24 carbon atoms, or R.sub.4 and R.sub.5 may together form --CH.sub.2 --.sub.n in which n is an integer of 4 to 7, R.sub.6 represents a hydrocarbon group of 1 to 24 carbon atoms, R.sub.7 represents hydrogen or a hydrocarbon group of 1 to 24 carbon atoms, R.sub.1, R.sub.2 and R.sub.3 independently represent hydrogen, an acyl group of 1 to 18 carbon atoms or a hydrocarbon group of 1 to 24 carbon atoms, and .about.Type: GrantFiled: January 31, 1990Date of Patent: August 27, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Koichi Matsumura, Yoshihiro Sugihara, Yoshiaki Shimizu, Kouichi Iida, Toshiro Yamashita
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Patent number: 5043349Abstract: Substituted pyrroles, pyrazoles and triazoles such as ##STR1## and their pharmaceutically suitable salts are useful as antihypertensive agents and for treatment of congestive heart failure.Type: GrantFiled: March 26, 1990Date of Patent: August 27, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventors: Carini, David J., John J. V. Duncia, Gregory J. Wells
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Patent number: 5039685Abstract: Novel O-alkylated oximes of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are optionally substituted aromatic or heteroaromatic rings, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is a nitrogen containing, substituted ring or an amino group carrying a substituted ring, and n and m independently are 0, 1 or 2, are potent inhibitors of GABA reuptake from the synaptic cleft.Type: GrantFiled: May 10, 1989Date of Patent: August 13, 1991Assignee: Novo Nordisk A/SInventors: Lars J. S. Knutsen, Knud E. Andersen, Anker S. Jorgensen, Ursula Sonnewald
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Patent number: 5026750Abstract: 1-Hydrocarbyloxy hindered amine mercaptoacid esters, thioacetals, sulfides and disulfides are effective light stabilizers for protecting a variety of polymer substrates from the deleterious effects of actinic light.Type: GrantFiled: February 14, 1990Date of Patent: June 25, 1991Assignee: Ciba-Geigy CorporationInventor: Ramanathan Ravichandran
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Patent number: 5023272Abstract: A method of preventing epileptic seizures in a human or mammal subject susceptible to said seizures, comprising systemically administering to said subject a safe and effective amount of a compound of the formula: ##STR1## wherein (a) X is halo or hydrogen, and Y is a substituent selected from the group consisting of unsubstituted or halogen-substituted methyl, halo, nitro, amino, and methoxy; and(b) R is N(R.sup.3).sub.2, OR.sup.1 N(R.sup.3).sub.2, N(R.sup.2)R.sup.1 N(R.sup.3).sub.2, or N(R.sup.2)N(R.sup.3).sub.2 ; whereR.sup.1 is C.sub.1 -C.sub.3 alkylene which is unsubstituted or substituted with C.sub.1 -C.sub.2 alkyl;R.sup.2 is hydrogen or lower alkyl; andeach R.sup.3 is, independently, hydrogen or lower alkyl; or both R.sup.Type: GrantFiled: June 23, 1989Date of Patent: June 11, 1991Assignee: Norwich Eaton Pharmaceuticals, Inc.Inventors: Homer A. Burch, Alan W. Castellion, Stanford S. Pelosi, Jr.
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Patent number: 5017702Abstract: Useful stabilizers for organic material, in particular plastics and paints, and metal ion deactivators are amides of the formula ##STR1## where R.sup.1 and R.sup.2 are singly methyl or together tetramethylene or pentamethylene, R.sup.3 is hydrogen, alkyl, alkoxycarbonyl, alkanoyl, benzyl, hydroxyethyl, cyanomethyl or aminomethyl, n is 1, 2 or 3 and--when n is 1--R.sup.4 is hydrogen and R.sup.5 is --CO--R.sup.6 is H, alkyl, cycloalkyl, aralkyl, phenoxyalkyl, aryl, a 5- or 6-membered heterocycle, alkoxy, aryloxy, cycloalkyloxy, phenylalkoxy, carbamoyl or --SO.sub.2 --R.sup.8 where R.sup.8 is alkyl or phenyl or ##STR2## is a phthalimide group or--when n is 2--R.sup.4 is H and R.sup.5 is --CO--Z--CO-- where Z is a chemical bond, C.sub.1 -C.sub.8 -alkylene, oxaalkylene, phenylene, cyclohexylene, biphenylene, biphenylene oxide, dioxyphenylene, diaminophenylene, diaminocyclohexylene, 1-.OMEGA.-diiminoalkylene or a 2-valent heterocycle or ##STR3## is a pyromellimide group or--when n is 3--R.sup.4 is H and R.sup.Type: GrantFiled: July 6, 1989Date of Patent: May 21, 1991Assignee: BASF AktiengesellschaftInventors: Alexander Aumueller, Peter Neumann, Hubert Trauth
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Patent number: 5015678Abstract: The Michael addition products of N-hydroxy hindered amines with alpha,beta-unsaturated carbonyl compounds including derivatives of esters, amids, imides and anhydrides are effective stabilizers for protecting organic polymers from the deleterious effects of actinic light.Type: GrantFiled: February 14, 1990Date of Patent: May 14, 1991Assignee: Ciba-Geigy CorporationInventors: Raymond Seltzer, James P. Galbo, Ramanathan Ravichandran
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Patent number: 5010090Abstract: 1-Aminobut-3-en derivatives having optionally substituted furanyl, thienyl, pyridyl and/or pyrrolyl in the 4-position and 3-carboxypiperidin-1-yl, 3-carboxytetrahydropyrid-1-yl or 3 carboxymethylpyrrolidin-1-yl in the 1-position potentiate GABA-ergic neurotransmission.Type: GrantFiled: October 7, 1988Date of Patent: April 23, 1991Assignee: Novo Nordisk A/S.Inventors: Frederik C. Gronvald, Claus Braestrup
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Patent number: 4996215Abstract: A new piperidine compound is pharmacologically effective for treatment of the arrythmia and is defined by the formula: ##STR1## in which R.sup.1 is a lower alkyl or a tolyl, R.sup.2 is hydrogen, hydroxyl, a lower alkoxy or a lower alkyl, R.sup.3 is hydrogen, a lower alkyl, a lower alkenyl, a cycloalkyl or a cycloalkylalkyl, X is --CO--, --CH.sub.2 -- or --CHOH--, g is an integer of 1 to 3, h is an integer of 1 to 3, Y is hydrogen, a lower alkyl, a lower alkenyl, cyano, --CH.sub.2 COOR, R being hydrogen or a lower alkyl, a cycloalkyl, a cycloalkylalkyl, ##STR2## l being 1 or 2, --A--B, A being --(CH.sub.2).sub.Type: GrantFiled: September 15, 1989Date of Patent: February 26, 1991Assignee: Eisai Co., Ltd.Inventors: Hitoshi Oinuma, Motosuke Yamanaka, Kazutoshi Miyake, Tomonori Hoshiko, Norio Minami, Tadao Shoji, Yoshiharu Daiku, Kohei Sawada, Kenichi Nomoto
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Patent number: 4996203Abstract: The present invention is directed to a specifically substituted tetrahydrofuran of the formula (I) ##STR1## wherein R.sup.4 is an alkylthio, alkylsulfinyl or alkylsulfonyl containing group and at least one of the substituents at positions 3,4 or 5 contains a heterocyclic, heteroaryl or substituted phenylthio moiety.Type: GrantFiled: June 8, 1989Date of Patent: February 26, 1991Assignee: Merck & Co., Inc.Inventors: Tesfaye Biftu, Robert L. Bugianesi, Nirindar N. Girotra, Mitree M. Ponpipom, Soumya P. Sahoo, Chan H. Kuo
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Patent number: 4992441Abstract: Mannich bases of the formula (I): ##STR1## where X is oxygen or NR.sup.2, Alk is divalent alkyl, R.sup.1 is an aromatic ring, R.sup.2 is a substituent and the salts thereof. Useful as antipsychotic agents in man to be used in a manner similar to chlorpromazine.Type: GrantFiled: September 30, 1988Date of Patent: February 12, 1991Assignee: McNeilab, Inc.Inventor: Malcolm K. Scott
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Patent number: 4988727Abstract: A compound selected from the group consisting of all enantiomeric and diastereoisomeric forms possible of compounds of the formula ##STR1## wherein X is selected from the group consisting of hydrogen, halogen, and alkyl and alkoxy of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms, one of A and B being ##STR2## and the other being ##STR3## R is hydrogen or alkyl of 1 to 5 carbon atoms, Z is --(CH.sub.2).sub.n -- or branched alkylene of 2 to 8 carbon atoms, n is an integer from 0 to 5, Y is selected from the group consisting of naphthyl, indenyl, heterobicyclics and heteromonocyclic containing 5 to 6 ring members, all optionally substituted with at least one member of the group consisting of alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --OH, --CF.sub.3, --NO.sub.2, --NH.sub.Type: GrantFiled: September 19, 1989Date of Patent: January 29, 1991Assignee: Roussel UclafInventors: Francois Clemence, Michel Fortin