Carbocyclic Ring Containing Patents (Class 546/213)
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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: 5071859Abstract: Novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which an ether group forms part of the N-substituent, the compounds thus having the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each represents phenyl, 2-thienyl or 3-thienyl, 2-pyrrolyl or 3-pyrrolyl, substituted with one or more substituents selected among the following atoms or groups: hydrogen, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy or cyano; R.sup.3 and R.sup.4 each represents hydrogen or together represent a bond; m is 1 or 2 and n is 1 when m is 1 and n is 0 when m is 2; R.sup.5 and R.sup.6 each represents hydrogen or may--when m is 2--together represent a bond, and R.sup.7 is OH or C.sub.1 -C.sub.8 -alkoxy, p is 0 or 1 or 2, q is 0 or 1 or 2, R.sup.8 is H and C.sub.1 -C.sub.4 -alkyl, are potent inhibitors of GABA uptake from the synaptic cleft.Type: GrantFiled: December 14, 1989Date of Patent: December 10, 1991Inventors: Lars Jacob S. Knudsen, Anker S. Jorgensen, Knud E. Andersen, Ursula Sonnewald
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Patent number: 5061704Abstract: 1. New thiophene compounds of the formula: ##STR1## in which: X represents hydrogen, halogen, C.sub.1 -C.sub.5 alkyl or alkoxy or dialkylamino;n represents 1 or 2;a represents an integer of from 2 to 6;b represents 2 or 3;c represents 1 or 2, and is such that b+c=4;R.sub.1 and R.sub.2 represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the carbon atom to which they are bonded form a hydrocarbon ring containing from 3 to 6 carbon atoms; andR and R' represent hydrogen or (C.sub.1 -C.sub.5)alkyl, or together with the nitrogen atom to which they are bonded form a pentagonal or hexagonal heterocycle optionally containing an oxygen atom or a second nitrogen atom which may itself be substituted; and their physiologically tolerable salts.The products of the invention can be used therapeutically especially in the treatment of pathologies that are characterized by a loss of bone tissue.2.Type: GrantFiled: November 23, 1990Date of Patent: October 29, 1991Assignee: Adir et CompagnieInventors: Michel Wierzbicki, Frederic Sauveur, Jacqueline Bonnet, Martine Brisset, Charles Tordjman
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Patent number: 5053411Abstract: This invention pertains to novel substituted N-aryl-N-[4-(1-heterocyclicalkyl)piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein R, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are defined in the disclosure.Type: GrantFiled: April 20, 1989Date of Patent: October 1, 1991Assignee: Anaquest, Inc.Inventors: Jerome R. Bagley, Nhora L. Lalinde, Bao-Shan Huang, H. Kenneth Spencer
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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: 5019650Abstract: Known and novel 4-aryl-4-piperidinecarbinols and heterocyclic analogs are useful as analgesics. Also provided are novel pyrrolidinecarbinols and hexhydroazepine carbinols which are useful as analgesics, antidepressants and, in some cases, as anorectic agents.Type: GrantFiled: August 28, 1989Date of Patent: May 28, 1991Assignee: E. I. Du Pont de Nemours and CompanyInventors: Engelbert Ciganek, Leonard Cook
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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: 4994471Abstract: This invention pertains to novel N-aryl-N-[N-substituted 3-alkoxy-4-piperidinyl]amides useful as analgesics, and methods of administering analgesia, which comprises the systemic administration to mammals of such compounds, and pharmaceutical compositions containing such compounds, wherein the novel compounds have the general formula: ##STR1## including optically active isomeric forms, cis/trans isomeric forms and the pharmaceutically acceptable acid addition salts therof, wherein:R is an aryl group selected from the group consisting of phenyl and substituted phenyl, wherein the substituents on the phenyl group are independently selected from the group consisting of halogen, lower-alkyl, lower-alkoxy, and combinations thereof;R.sub.1 is an alkyl group selected from the group consisting of lower-alkyl, lower-alkenyl, and lower-alkoxy lower-alkyl, each alkyl group having from 1 to 6 carbon atoms;R.sub.Type: GrantFiled: May 12, 1989Date of Patent: February 19, 1991Assignee: BOC, Inc.Inventors: Nhora L. Lalinde, John Moliterni, H. Kenneth Spencer
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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
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Patent number: 4987132Abstract: A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity.Type: GrantFiled: August 16, 1988Date of Patent: January 22, 1991Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Toshiyasu Mase, Hiromu Hara, Hitoshi Nagaoka, Takumi Takahashi, Takeshi Suzuki, Kenichi Tomioka, Toshimitsu Yamada
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Patent number: 4980349Abstract: The invention relates to new compounds corresponding to formula I: ##STR1## in which: W represents C=O, CH.sub.2 or CHOH,Z represents ##STR2## R.sub.1 and R.sub.2 represent especially Cl or F, R, R' and R" represent especially H,X represents especially CH.sub.2,Y represents especially COOH,u and v are two integers ranging from 0 to 10,p and q take the value 0 or 1,n and m are two integers ranging 0 to 10 andt is 0 or 1the total number of carbon atoms in the chain ##STR3## ranging from 2 to 20, and to their physiologically acceptable salts obtained with organic or inorganic acids.These compounds are useful for preparing medicinal products which have, especially, anti-inflammatory properties.Type: GrantFiled: November 12, 1987Date of Patent: December 25, 1990Assignee: SANOFIInventors: Pierre Roger, Jean-Paul Fournier, Alain Martin, Jean Choay
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Patent number: 4962115Abstract: Novel N-(3-hydroxy-4-piperidinyl)benzamides and derivatives thereof, said compounds being useful as stimulators of the motility of the gastro-intestinal system.Type: GrantFiled: November 28, 1989Date of Patent: October 9, 1990Assignee: Janssen Pharmaceutica N.V.Inventor: Georges Van Daele
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Patent number: 4960768Abstract: Novel fungicidally active acyloxythiophene-carboxamides of the formula ##STR1## in which R.sup.1 represents alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl, alkinyl or cycloalkyl,R.sup.2 represents alkyl or optionally substituted phenyl,R.sup.Type: GrantFiled: May 8, 1989Date of Patent: October 2, 1990Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Gerd Hanssler
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N-substituted derivatives of 1-desoxynojirimycin and 1-desoxymannonojirimycin and pharmaceutical use
Patent number: 4940705Abstract: N-substituted derivatives of 1-desoxynojirimycin and 1-desoxymannojirimycin of the formula ##STR1## in which one of R and R' are hydroxyl and the other is hydrogenn is a number from 1 to 6R.sup.1 is hydrogen, alkyl or benzyl andR.sup.2 is alkyl which is optionally substituted by an optionally substituted aryl or by pyridyl, thienyl, furyl, pyrimidyl, pyrazinyl or quinolyl or R.sub.1 is cycloalkyl or R.sup.2 is optionally substituted by aryl or R.sup.2 is a saturated bridged heterocycle or R.sup.1 and R.sup.2 together can form a heterocyclic ring which is optionally substituted. These compounds are useful in the treatment of and prophylaxis of viral infections.Type: GrantFiled: October 26, 1988Date of Patent: July 10, 1990Assignee: Bayer AktiengesellschaftInventors: Horst Boshagen, Bodo Junge, Arnold Paessens, Matthias Schuller -
Patent number: 4931450Abstract: Compounds of the Formula I ##STR1## wherein R.sup.1 represents phenyl, or phenyl substituted by one, or more substituents selected from the group consisting of halogen, C.sub.1-7 -alkyl, and C.sub.1-7 -alkoxy, R.sup.2 represents furanyl, thienyl, pyridyl or pyrrolyl ortho substituted with C.sub.1-7 -alkyl or halogen and wherein R.sup.3 represents 3-carboxypiperidin-1-yl, 3-carboxy-1,2,5,6-tetrahydropyridin-1-yl or 3-carboxymethyl-pyrrolidin-1-yl, pharmaceutical compositions containing effective amounts of a compound of formula I and treatment of central nervous system ailments by administering a compound of formula I.Type: GrantFiled: October 17, 1988Date of Patent: June 5, 1990Assignee: Novo Industri A/SInventor: Ursula Sonnewald
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Patent number: 4921864Abstract: Compounds are disclosed of the formula ##STR1## where R.sup.2 is unsubstituted or substituted phenyl, R.sup.3 is lower alkyl, lower cycloalkyl or lower alkoxy lower alkyl, and L is selected from a wide variety of groups. This new class of compounds exhibit improved analgesic and anesthetic properties.Type: GrantFiled: October 7, 1988Date of Patent: May 1, 1990Assignee: BOC, Inc.Inventors: Linas V. Kudzma, H. Kenneth Spencer, Sherry A. Severnak
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Patent number: 4921863Abstract: Cyclic amine derivatives of the formula: ##STR1## or the pharmacologically acceptable salts thereof, wherein the symbols are as defined in the specification, as effective in relieving, curing or preventing mental symptoms due to cerebral vascular disorders.Type: GrantFiled: February 17, 1988Date of Patent: May 1, 1990Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Norio Karibe, Isao Saito, Kunizou Higurashi, Masahiro Yonaga, Takeru Kaneko, Takahiro Nakazawa, Masataka Ueno, Kiyomi Yamatsu
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Patent number: 4914111Abstract: Thiophene (or furan)-2-sulfonamides with a 4-benzyl substituent are effective in the treatment of elevated intraocular pressure and glaucoma following topical ocular administration.Type: GrantFiled: March 23, 1987Date of Patent: April 3, 1990Assignee: Merck & Co., Inc.Inventors: George D. Hartman, Wasyl Halczenko
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Patent number: 4910312Abstract: Selected analogs of nipecotic acid are the novel compounds of the present invention. The analogs are GABA uptake inhibitors for use to treat epilepsy and, thus, the invention is also pharmaceutical compositions and methods of use therefor.Type: GrantFiled: June 16, 1988Date of Patent: March 20, 1990Assignee: Warner-Lambert CompanyInventor: Michael R. Pavia
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Patent number: 4904686Abstract: Compounds of the following formula have pharmacutical properties: ##STR1## in which R.sup.1 and R.sup.2 independently are hydrogen, halo, nitro, amino, C.sub.2-5 acylamino, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, C.sub.1-4 alkylsulphonyl, N-substituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or R.sup.1 and R.sup.2 together form a C.sub.3-5 alkylene bridge, R.sup.3 is C.sub.1-4 alkyl or C.sub.2-4 alkenyl, and X is (i) --(CH.sub.2).sub.n N(R.sup.4).sub.2 where each R.sup.4 independently is C.sub.1-4 alkyl, C.sub.2-4 alkenyl or optionally substituted C.sub.6 H.sub.5 CH.sub.2 --, and n is 1, 2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a C.sub.1-3 alkylene chain; and salts thereof.Type: GrantFiled: April 11, 1988Date of Patent: February 27, 1990Assignee: Lilly Industries LimitedInventors: Maria I. F. Fernandez, Terrence M. Hotten, David E. Tupper
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Patent number: 4888433Abstract: A new enantioselective process is described for preparing optically active alpha-arylalkanoic acids by:(a) halogenation on the aliphatic carbon atom alpha to the ketal group, of ketals of formula ##STR1## in which Ar represents an aryl, optionally substituted;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, represent a hydroxy, a O.sup.- M.sup.+, OR.sub.3 or NR.sub.4 R.sub.5 group;the carbon atoms indicated by an asterisk both simultaneously are in (R) or (S) configuration.This reaction is diastereoselective, so that a mixture of alpha-haloketals is obtained in which one of the two epimers prevails, and generally strongly prevails, over the other.(b) rearrangement of the haloketals of formula ##STR2## in which X is Cl, Br or I to alpha-arylalkanoic acids in a single stage or in two successive stages, by way of esters of formula ##STR3## The compounds (A) and (C) are all new compounds. The rearrangement step (b) may be performed under new, inventive conditions.Type: GrantFiled: August 5, 1987Date of Patent: December 19, 1989Assignee: Zambon, S.p.A.Inventors: Claudio Giordano, Graziano Castaldi, Fulvio Uggeri, Silvia Cavicchioli
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Patent number: 4880800Abstract: Compounds are described of the formula ##STR1## where: R.sup.1 is --H or --CH.sub.3,n is 1, m is 2-4 and X is --CH.dbd.CH-- or --CH.sub.2 CH.sub.2 --;Y is a saturated heterocyclic amino group,R.sup.2 is (i) substituted or unsubstituted phenylalkyl, thineylalkyl or naphthylalkyl or (ii) cinnamyl, and their salts and solvates.These compounds inhibit blood platelet aggregation, bronchoconstriction and vasoconstriction and may be formualted for use as antithrombotic or antiasthmatic agents.Type: GrantFiled: September 15, 1987Date of Patent: November 14, 1989Assignee: Glaxo Group LimitedInventors: Christopher J. Wallis, Harry Finch, Peter Hallett
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Patent number: 4853384Abstract: 1-Carbonyl derivatives of 4-aryl-4-aryloxypiperidines and methods for alleviating pain and treating convulsions utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: March 14, 1988Date of Patent: August 1, 1989Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Grover C. Helsley, Larry Davis, Gordon E. Olsen
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Patent number: 4849521Abstract: The present invention is directed to an improved stereoselective tandem substitution and reduction of an imine precursor to the cis form of 3-substituted-4-(phenylanilo)piperidine compounds or their substituted derivatives.Type: GrantFiled: November 2, 1987Date of Patent: July 18, 1989Assignee: BOC, Inc.Inventors: Linas V. Kudzma, H. Kenneth Spencer, Sherry A. Severnak
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Patent number: 4837316Abstract: Alkylamide derivatives having the formula, These compounds have a strong antiulcer action depend on histamine H.sub.2 -receptor antagonistic action and a cytoprotective action upon gastric mucous membrance.Type: GrantFiled: August 27, 1986Date of Patent: June 6, 1989Assignee: Fujirebio Kabushiki KaishaInventors: Yasuo Sekine, Nobuhiro Hirakawa, Noriaki Kashiwaba, Tetsuaki Yamaura, Hisako Harada, Teruo Kutsuma, Hajime Matsumoto, Akihiro Sekine, Yoshikazu Isowa
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Patent number: 4831192Abstract: Compounds are disclosed of the formula ##STR1## Where R.sup.1 is an unsubstituted or substituted heterocyclic ring system; R.sup.2 is an unsubstituted or substituted phenyl; R.sup.3 is a lower alkyl or lower alkoxy, and L is selected from a wide variety of groups.Type: GrantFiled: December 31, 1987Date of Patent: May 16, 1989Assignee: BOC, Inc.Inventors: Bor-Sheng Lin, Joseph W. Scheblein
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Patent number: 4806552Abstract: The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --NM.dbd.N--; R.sup.4, R.sup.5 and R.sup.6 ; and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.Type: GrantFiled: November 12, 1986Date of Patent: February 21, 1989Assignee: John Wyeth & Brother, LimitedInventors: John L. Archibald, Terence J. Ward
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Patent number: 4791120Abstract: Compounds are disclosed of the formula ##STR1## where R.sup.1 is an unsubstituted or substituted heterocyclic ring system; R.sup.2 is an unsubstituted or substituted phenyl; R.sup.3 is a lower alkyl or lower alkoxy, and L is selected from a wide variety of groups.Type: GrantFiled: December 31, 1987Date of Patent: December 13, 1988Assignee: The BOC Group, Inc.Inventors: Bor-Sheng Lin, Linas V. Kudzma, H. Kenneth Spencer
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Patent number: 4791121Abstract: Compounds are disclosed of the formula ##STR1## where R.sup.2 is unsubstituted or substituted phenyl, R.sup.3 is lower alkyl, lower cycloalkyl or lower alkoxy lower alkyl, and L is selected from a wide variety of groups. This new class of compounds exhibit improved analgesic and anesthetic properties.Type: GrantFiled: November 2, 1987Date of Patent: December 13, 1988Assignee: The BOC Group, Inc.Inventors: Linas V. Kudzma, H. Kenneth Spencer, Sherry A. Severnak
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Patent number: 4788184Abstract: Compounds of the formula ##STR1## wherein R.sup.12 is a leaving group, Z is S, O or CH.sub.2 and A is a phenyl, furyl, thienyl or pyridyl ring substituted by a ##STR2## moiety, in which R.sup.8 and R.sup.9 are various substituents or, when taken together with the nitrogen, may be a specified heterocyclic ring, are intermediates in the preparation of histamine H.sub.2 -antagonist anti-ulcer agents of the formula ##STR3## in which R.sup.1 and R.sup.2 are any of several specified substituents.Type: GrantFiled: November 13, 1987Date of Patent: November 29, 1988Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4772618Abstract: Substituted benzamides of the general formula I ##STR1## in which: R represents an alkoxy, alkenyloxy or alkynyloxy group containing up to 7 carbon atoms in the group,R.sub.1 is hydrogen or a NR.sub.4 R.sub.5, or NR.sub.6 COR.sub.7 group, where R.sub.4, R.sub.5 and R.sub.6, which may be the same or different, is each hydrogen or an alkyl group and R.sub.7 is an alkyl or trifluoromethyl group,R.sub.2 is hydrogen, halogen, or a nitro, or sulphamoyl group,R.sub.3 represents hydrogen or a methyl or methoxy group,X represents a hydrocarbon chain containing 1 to 4 carbon atoms, one of which may optionally be replaced by an oxygen atom,Y represents a non-aromatic cyclic ether or a non-aromatic cyclic thioether group and pharmaceutically acceptable salts thereof are useful in the treatment of gastro-intestinal disorders. Various methods of synthesis are described including synthesis via novel amines of the formula ##STR2## which are themselves obtained by reduction of the corresponding oximes.Type: GrantFiled: July 31, 1986Date of Patent: September 20, 1988Assignee: Fordonal, S.A.Inventors: Armando Vega-Noverola, Jose M. Prieto-Soto, Fernando Pujol-Noguera, Jacinto Moragues-Mauri, Robert G. W. Spickett
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Patent number: 4772615Abstract: Analogs of nipecotic acid are the novel compounds of the present invention. The analogs are GABA uptake inhibitors for use to treat epilepsy and, thus, the invention is also pharmaceutical compositions and methods of use therefor.Type: GrantFiled: October 14, 1987Date of Patent: September 20, 1988Assignee: Warner-Lambert CompanyInventor: Michael R. Pavia
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Patent number: 4767757Abstract: Novel fungicidally active acyloxythiophene-carboxamides of the formula ##STR1##Type: GrantFiled: March 19, 1987Date of Patent: August 30, 1988Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Gerd Hanssler
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Patent number: 4755527Abstract: The present invention relates to new compounds of the formula ##STR1## where X is ##STR2## alkylene, or --S--where R.sub.1 is hydrogen, alkyl, or aryl; W is hydrogen, hydroxy, amino, alkyloxy, aryloxy, O-alkyl, or O-aralkyl; (Y).sub.A) is --CH.sub.2 NR.sub.2 R.sub.3 where R.sub.2 and R.sub.3 may be hydrogen, substituted alkyls, aryls, or together with N form a 5 to 7 membered heterocyclic group; and Ar is a substituted or unsubstituted aryl. These compounds are useful in the treatment of various cardiac arrhythmias.Type: GrantFiled: December 27, 1985Date of Patent: July 5, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: David M. Stout, William L. Matier
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Patent number: 4752607Abstract: Alkoxycarbonyl-substituted hydroxythiophenecarboxamides of the formula ##STR1## in which R.sup.1 represents alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl or alkinyl or represents cycloalkyl,R.sup.2 represents alkyl or optionally substituted phenyl,R.sup.3 represents alkyl, alkoxyalkyl, alkylthioalkyl, cyanoalkyl, fluoroalkyl, alkenyl, alkinyl, cycloalkyl or alkoxy andR.sup.4 represents hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl, fluoroalkyl, cyanoalkyl, alkenyl, alkinyl or cycloalkyl, orR.sup.3 and R.sup.4, together with the nitrogen atom, represent a heterocyclic radical which is optionally substituted by alkyl and can be further substituted in the alkylene chain by oxygen, sulphur or nitrogen,are useful as fungicides and intermediates.Type: GrantFiled: June 17, 1986Date of Patent: June 21, 1988Assignee: Bayer AktiengesellschaftInventors: Werner Daum, Gerd Hanssler
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Patent number: 4743602Abstract: According to the invention there are provided compounds useful for combatting fungi having the general formula (I): ##STR1## and stereoisomers thereof, wherein one of X and Y, but not both, is a group of the formula (II): ##STR2## and the other of X and Y is a hydrogen atom, a halogen atom, or an alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, aralkyl, alkoxy, aryloxy or haloalkyl group or a ##STR3## group wherein R.sup.9, R.sup.10 and R.sup.11 can be alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or aryl, Z is an oxygen atom, a sulphur atom or an --NH-group, A and B have the same significance as X or Y excluding a group of formula (II), R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each represent a hydrogen atom, a halogen atom or an alkyl group containing from 1 to 4 carbon atoms, R.sup.5 and R.sup.6 each represent a hydrogen atom or an alkyl group containing from 1 to 4 carbon atoms, and R.sup.7 and R.sup.8 each represent an alkyl group containing from 1 to 4 carbon atoms or R.sup.7 and R.sup.Type: GrantFiled: June 30, 1987Date of Patent: May 10, 1988Assignee: Imperial Chemical Industries PLCInventors: Paul A. Worthington, Vivienne M. Anthony
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Patent number: 4736055Abstract: Oxime sulfonates of formula I ##STR1## wherein Y is a polymerizable unsaturated group or epoxide group or an --OH, --NHR.sup.5, --COOH, COOR.sup.6, --COCl, --CH.sub.2 Hal, --SO.sub.2 Cl or --NCO group, Z is an (x+y)-valent connecting member, R.sup.1 and R.sup.2 are monovalent organic radicals, m is 0 or 1, x is 1 or 2 and y is 1 or 2, can be converted into polymers which can be thermally or photochemically dissociated to form free sulfonic acid groups. Said polymers can therefore be used as photoresists which can be developed with aqueous alkalis.Type: GrantFiled: April 11, 1986Date of Patent: April 5, 1988Assignee: Ciba-Geigy CorporationInventors: Kurt Dietliker, Werner Rutsch, Godwin Berner, Max Hunziker, Christopher G. Demmer
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Patent number: 4734507Abstract: Compounds of formula ##STR1## wherein Ar represents an optionally substituted aryl group;R represents a C.sub.1 -C.sub.4 alkyl;R.sub.1 and R.sub.2, equal to or different from each other, represent hydroxy, O.sup.- M.sup.+, OR.sub.3 or ##STR2## R.sub.3 represents a C.sub.1 -C.sub.24 alkyl, a C.sub.3 -C.sub.6 cycloalkyl, a phenyl or a benzyl;M.sup.+ represents the cation of an alkaline metal;R.sub.4 and R.sub.5, equal to or different from each other, represent a hydrogen atom, a C.sub.1 -C.sub.4 alkyl, a C.sub.5 -C.sub.6 cycloalkyl, a (CH.sub.2).sub.n --CH.sub.2 OH group with n=1, 2 or 3, or R.sub.4 and R.sub.5 together are a group (CH.sub.2).sub.m with m=4 or 5, a group --CH.sub.2 --CH.sub.2 --R.sub.6 --CH.sub.2 --CH.sub.2 -- in which R.sub.6 is an oxygen atom, an N--H or N--(C.sub.1 -C.sub.Type: GrantFiled: April 5, 1985Date of Patent: March 29, 1988Assignee: Zambon S.p.A.Inventors: Claudio Giordano, Graziano Castaldi, Fulvio Uggeri, Silvia Cavicchioli
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Patent number: 4734508Abstract: A process is provided for preparing 4-hydroxy-4-phenyl-proline derivatives of the structure ##STR1## wherein R.sub.1 is a nitrogen protecting group such as benzoyl, benzyloxycarbonyl, t-butoxycarbonyl, benzyl, benzhydryl, trityl, acetyl, trifluoromethylacetyl, sulfonamides, and the like and wherein X is OR.sub.2 and R.sub.2 is hydrogen or an acid protecting group such as lower alkyl, aryl-lower alkyl or a metal ion, such as Na or K, or X is NR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 may be the same or different and are hydrogen, lower alkyl, aryl or arylalkyl, or R.sub.3 and R.sub.4 together with the nitrogen to which they are attached form a 5-, 6- or 7-membered ring. The process includes the steps of forming triphenylcerium [(C.sub.6 H.sub.5).sub.3 Ce], for example, by reacting cerium trichloride (CeCl.sub.3) with phenyllithium, and reacting the triphenylcerium with the keto acid ##STR2## in the presence of an inert organic solvent such as tetrahydrofuran.Type: GrantFiled: May 1, 1987Date of Patent: March 29, 1988Assignee: E. R. Squibb & Sons, Inc.Inventor: John K. Thottathil
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Patent number: 4727072Abstract: Propylamines of the formula (I): ##STR1## and isomers thereof, particularly those enantiomers and racemates relative to the chiral carbon indicated by an asterisk (*). The propylamines can be used for the treatment of hypertension or angina in humans. A is pyrrolidine, piperidine or morpholine and B is an aromatic heterocycle, aromatic carbocycle or saturated carbocycle.Type: GrantFiled: February 12, 1986Date of Patent: February 23, 1988Assignee: McNeilab, Inc.Inventors: Philip P. Grous, Richard J. Mohrbacher
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Patent number: 4722930Abstract: The invention concerns the preparation of compounds of formula ##STR1## and acid addition and quaternary ammonium salts thereof, wherein the dotted line represents an optional bond, Ar represents a ring system of formula ##STR2## in which Q is O, S, --CR.sup.7 .dbd.CR.sup.8 --, --N.dbd.CR.sup.8 -- and --N.dbd.N--; R.sup.4, R.sup.5 and R.sup.6, and R.sup.7 and R.sup.8 when present, each represent hydrogen or a substituent selected from lower alkyl, lower alkenyl, lower alkoxy, NO.sub.2, NH.sub.2, haloloweralkyl, hydroxyloweralkyl, aminoloweralkyl, substituted amino, halogen, loweralkoxycarbonyl, cyano, CONH.sub.2 and hydroxy; and additionally either R.sup.4 and R.sup.5 when adjacent or R.sup.6 and R.sup.Type: GrantFiled: September 30, 1985Date of Patent: February 2, 1988Assignee: John Wyeth and Brother LimitedInventors: John L. Archibald, Terence J. Ward
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Patent number: 4678496Abstract: As new compound is provided a cyclohexane derivative of the formula ##STR1## wherein R represents a hydrogen atom or an alkyl group, an alkylthioalkyl group or an unsubstituted or substituted phenyl group; and R.sup.1 represents an alkyl group, an unsubstituted or substituted benzyl group, a phenethyl group, a phenoxymethyl group, a 2-thienylmethyl group, an alkoxymethyl group or an alkylthiomethyl group, or a salt of said cyclohexane compound.This cyclohexane compound exhibits useful plant-growth regulating effects on crop-plants and also non-crop plants such as lawn and may be prepared by cyclization of an acetonylsuccinic acid dialkyl ester, followed by reaction with an organic acid chloride and by intermolecular rearrangement.Type: GrantFiled: August 1, 1985Date of Patent: July 7, 1987Assignee: Kumiai Chemical Industry Co., Ltd.Inventors: Kenji Motojima, Takeshige Miyazawa, Yasufumi Toyokawa, Masafumi Matsuzawa, Hiroshi Hokari, Shoji Kusano
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Patent number: 4652679Abstract: Aziridine and phenethanolamine derivatives of formulae I and II-1 ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or lower-alkyl; Z.sup.1 is phenyl or a phenyl group substituted in a defined manner; Z.sup.2 and Z.sup.21 are phenyl or thienyl substituted in a defined manner; and, n is an integer from 1-4. The disclosed compounds have catabolic activity and can be used for the treatment of obesity and/or of sugar illnesses. The compounds of formula I are obtained by dehydrating .beta.-aminoalcohols (e.g. those of formula II-1) which, in turn, can be prepared by adding amines to epoxides or by reducing corresponding iminoketones, iminoalcohols a-keto-.beta.-hydroxyamines or .beta.-ketoamines.Type: GrantFiled: May 9, 1983Date of Patent: March 24, 1987Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Marcel Muller
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Patent number: 4642315Abstract: Peptides of the formula ##STR1## wherein X is various amino or imino acids or esters are useful as hypotensive agents.Type: GrantFiled: October 22, 1984Date of Patent: February 10, 1987Assignee: E. R. Squibb & Sons, Inc.Inventors: Eric M. Gordon, Harold N. Weller, III
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Patent number: 4639436Abstract: The invention includes certain 3,4,5-trihydroxypiperidine compounds, methods for their preparation, compositions containing said 3,4,5-trihydroxypiperidine compounds and methods for the use of said compounds and compositions.The subject matter of the invention is useful against diabetes, hyperlipaemia and adiposity as well as in animal nutrition.Type: GrantFiled: August 23, 1978Date of Patent: January 27, 1987Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Hans P. Krause, Lutz Muller, Walter Puls
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Patent number: 4613597Abstract: Compounds are described of the formulae (1a) and 1b) ##STR1## in which: R.sup.1 is -H, C.sub.1-6 alkyl or C.sub.7-10 aralkyl,W is C.sub.1-7 alkyleneX is cis or trans --CH.dbd.CH--,Y is a saturated heterocyclic amino group having 5-8 ring members,R.sup.2 is (i) substituted or unsubstituted phenylalkyl, thienylalkyl or naphthylalkyl or (ii) cinnamyl, and Z is --CH.sub.2 OH, --CHO or --CONHR.sup.4 where R.sup.4 is --H or methyl,and their salts and solvates.These compounds inhibit blood platelet aggregation, bronchoconstriction and vasoconstriction, and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: September 5, 1984Date of Patent: September 23, 1986Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes
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Patent number: 4607105Abstract: Certain 1-(substituted amino)-2-(amino or substituted amino)cyclobutene-3,4-diones are potent histamine H.sub.2 -antagonists useful in the treatment of peptic ulcers.Type: GrantFiled: October 1, 1984Date of Patent: August 19, 1986Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4594351Abstract: Compounds of the following formula (I): ##STR1## wherein Alk is a straight or branched chain alkylene of about 1 to 12 carbons and R.sup.1 is a heterocyclic ring system, have been found to possess potent antisecretory activity and are thus useful in the treatment of hyperacidity.Type: GrantFiled: April 25, 1985Date of Patent: June 10, 1986Assignee: McNeilab, Inc.Inventor: Malcolm K. Scott
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Patent number: RE33125Type: GrantFiled: July 11, 1986Date of Patent: December 5, 1989Assignee: Rorer Pharmaceutical CorporationInventors: Henry F. Campbell, Thomas H. Scholtz, George H. Douglas
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Patent number: RE33495Abstract: The present invention is directed to an improved stereoselective tandem substitution and reduction of an imine precursor to the cis form of .[.3-substituted-4-(phenylamino)piperidine.]. .Iadd.3-substituted-4-anilino piperidine .Iaddend.compounds or their substituted derivatives.Type: GrantFiled: September 27, 1989Date of Patent: December 18, 1990Assignee: BOC, Inc.Inventors: Linas V. Kudzma, H. Kenneth Spencer, Sherry A. Savernak