Carbocyclic Ring Bonded Directly To The Nitrogen Patents (Class 544/165)
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Patent number: 4873241Abstract: 2-Amino-N-(2-phenylindan-2-yl)acetamides of the following formula are provided ##STR1## wherein, a=0 to 3,R.sub.1, R.sub.2 and R.sub.3 are independently selected from hydrogen and methyl,R.sub.4 is hydrogen or C.sub.1 -C.sub.4 alkyl,R.sub.5 is selected from hydrogen, C.sub.1 -C.sub.4 alkyl, cyclopropyl and (aminomethyl)carbonyl, orR.sub.4 and R.sub.5 taken together with the nitrogen atom to which they are attached from a heterocyclic ring selected from pyrrolidinyl, piperidinyl and morpholinyl, orR.sub.3 and R.sub.4 taken together with the carbon atom and nitrogen atom to which they are respectively attached form a heterocyclic ring selected from pyrrolidinyl and piperidinyl, andR.sub.6 is selected from hydrogen, halogen, C.sub.1 -C.sub.4 alkoxy, trifluoromethyl, C.sub.1 -C.sub.4 alkyl and combinations thereof.The compounds have antiepileptic or antihypoxia activity.Type: GrantFiled: October 31, 1988Date of Patent: October 10, 1989Assignee: Fisons CorporationInventors: James J. Napier, Ronald C. Griffith
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Patent number: 4810725Abstract: 1-Aryloxy-3-(substituted aminoalkylamino)-2-propanols and pharmaceutically acceptable salts thereof have .beta.-adrenergic blocking activity with some cardioselectivity and hence are useful as anti-hypertensive, antianginal, antiarrhythmic and cardioprotective agents and in the treatment of elevated intraocular pressure such as glaucoma.Type: GrantFiled: October 14, 1986Date of Patent: March 7, 1989Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello, Sandor L. Varga
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Patent number: 4783535Abstract: A process for the preparation of 1,4-oxazepinones and thiones having the formula: ##STR1## wherein A is an aromatic ring selected from benzene, naphthalene, quinoline or pyridine; n is 1 to 3; Z is an amino radical; R is hydrogen, loweralkyl, cycloalkyl or phenylloweralkyl; and R.sup.4 and R.sup.5 are hydrogen and loweralkyl starting from chloroaromatic carboxylates and alkanolamines is disclosed. The oxazepinones and oxazepinethiones prepared by the process have utility as antihistaminics with low sedative potential. Novel intermediate compounds are also disclosed.Type: GrantFiled: March 18, 1986Date of Patent: November 8, 1988Assignee: A. H. Robins Company, IncorporatedInventors: Young S. Lo, Albert D. Cale, Jr.
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Patent number: 4760146Abstract: Novel compounds and processes for making and using them. The compounds include ethyl 1-[3-(1-piperidinyl)propyl]-6-phenyl-3-cyclohexene-1-carboxylate, 1-[3-(1-piperidinyl)propyl]-6-phenyl-3-cyclohexene-1-carboxyamide, and N,N-dimethyl-1-[3-(1-piperidinyl)propyl]-6-phenyl-3-cyclohexene-1-carboxam ide.Type: GrantFiled: February 18, 1986Date of Patent: July 26, 1988Assignee: Pennwalt CorporationInventor: Bruce H. Toder
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Patent number: 4758563Abstract: 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: November 9, 1987Date of Patent: July 19, 1988Assignee: McNeilab, Inc.Inventors: Philip P. Grous, Richard J. Mohrbacher
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Patent number: 4753934Abstract: Compounds of the formula ##STR1## wherein A, B, R.sub.1, X and Q are substituents of various types, and acid addition salts thereof. The compounds are useful as fungicides.Type: GrantFiled: September 29, 1986Date of Patent: June 28, 1988Assignee: Celamerck GmbH & Co. KGInventors: Josef Nickl, Helmut Pieper, Jurgen Curtze, Christo Drandarevski, Sigmund Lust
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Patent number: 4739106Abstract: A process for preparing a 2-carbamoyloxyalkyl-1,4-dihydropyridine derivative represented by the general formula: ##STR1## which comprises: (a) reacting a 3-amino-3-carbamoyloxyalkylacrylic acid derivative represented by the general formula: ##STR2## with a benzylidene compound represented by the general formula: ##STR3## (b) reacting the 3-amino-3-carbamoyloxyalkylacrylic acid derivative of the general formula II with an aldehyde compound represented by the general formula: ##STR4## and a .beta.-keto-ester compound represented by the general formula:R.sup.4 --CO--CH.sub.2 --COOR.sup.2 (V)(c) reacting a 3-carbamoyloxyalkylpropiolic acid derivative represented by the general formula: ##STR5## with the benzylidene compound of the general formula III and ammonia or its salt; or(d) reacting the 3-carbamoyloyalkylpropiolic acid derivative of the general formula VI with the aldehyde compound of the general formula IV, the .beta.-keto-ester compound of the general formula V and ammonia or its salt.Type: GrantFiled: May 16, 1986Date of Patent: April 19, 1988Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Tetsuji Miyano, Kunio Suzuki, Nobuo Harada
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Patent number: 4737498Abstract: Novel N-alkyl-2,6-dimethylmorpholinocarboxamide salts of the general formula I, ##STR1## processes for their preparation, and their use as fungicides for controlling pathogenic fungi. The agents according to the invention additionally possess plant growth-regulating properties. The meanings of R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X.sup.- are given in the description.Type: GrantFiled: July 2, 1986Date of Patent: April 12, 1988Assignee: BASF AktiengesellschaftInventors: Lothar Banasiak, Wilfried Edlich, Horst Lyr, Eva Nega, Marianne Sunkel
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Patent number: 4731383Abstract: The invention relates to new aminoguanidine derivatives of the general formula (I), ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each represent hydrogen or halogen atom, C.sub.1-4 alkyl, nitro, trifluoromethyl or C.sub.1-4 alkoxy group,R.sup.4 and R.sup.5 represent a C.sub.1-4 alkyl group, furthermore NR.sup.4 R.sup.5 may form a 5 to 7 membered saturated heterocyclic group containing either one or two nitrogen atoms or a nitrogen and an oxygen atom and being optionally substituted by one or two methyl, hydroxymethyl or hydroxyethyl groups,R.sup.6 and R.sup.7 each represent a hydrogen atom, normal or branched C.sub.1-4 alkyl or C.sub.2-4 alkenyl group,and to their pharmaceutically acceptable acid addition salts as well as to a process for the preparation thereof.The new compounds of the invention possess valuable antiarrhythmic activity and are devoid of the undesired circulatory side effects of the known antiarrhythmic compounds.Type: GrantFiled: October 29, 1986Date of Patent: March 15, 1988Assignee: Biogal GyogyszergyarInventors: Istvan Erczi, Jeno Marosfalvi, Gyorgy Rabloczky, Andras Varro, Maria Kuhar nee Kurthy, Istvan Elekes, Laszlo Szatmary, Laszlo Jaszlits
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Patent number: 4730008Abstract: The invention provides compounds of the general formula (I) ##STR1## wherein Ar, R.sup.1, R.sup.2, X, Y and Q are defined in the specification and physiologically acceptable salts and solvates thereof.The compounds have a selective stimulant action at .beta..sub.2 -adrenoreceptors and may be used, inter alia, in the treatment of diseases associated with reversible airways obstruction such as asthma and chronic bronchitis.Type: GrantFiled: January 10, 1986Date of Patent: March 8, 1988Assignee: Glaxo Group LimitedInventors: Ian F. Skidmore, Harry Finch, Alan Naylor, Lawrence H. C. Lunts, Ian B. Campbell
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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: 4693850Abstract: Novel synthetic steps and intermediates leading to guanidines such as the anti-diabetic compound linogliride.Type: GrantFiled: November 26, 1986Date of Patent: September 15, 1987Assignee: McNeilab, Inc.Inventors: Cynthia A. Maryanoff, James N. Plampin, Robin C. Stanzione
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Patent number: 4692446Abstract: Novel compounds of the general formula ##STR1## wherein R.sub.1 is lower alkyl, lower cycloalkyl, lower alkenyl, lower alkynyl, lower alkyl carboxymethyl, aryl carboxymethyl, aryl, or aralkyl; A is a direct bond, lower alkylene, or lower alkenylene; x is 1 or 2, provided that when x is greater than 1, different occurrences of the ##STR2## group may be the same or different; Ar is heterocyclic, unsubstituted aromatic or aromatic substituted with lower alkyl, lower alkenyl, lower alkynyl, lower alkoxy, halogen, acetamido, amino, nitro, lower alkylamino, hydroxy, lower hydroxyalkyl or cyano; W is alkylene containing from 1 to about 10 carbon atoms; and B is --NR.sub.2 COR.sub.3, --NR.sub.2 CONR.sub.3 R.sub.4, --NR.sub.2 SO.sub.2 R.sub.3, --NR.sub.2 SO.sub.2 NR.sub.3 R.sub.4, or --NR.sub.2 COOR.sub.5, wherein R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, alkoxyaryl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.3 and R.Type: GrantFiled: October 28, 1986Date of Patent: September 8, 1987Assignee: E. I. Du Pont de Nemours & Co., Inc.Inventors: Paul W. Erhardt, William L. Matier
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Patent number: 4686220Abstract: This disclosure describes certain substituted piperazine-1,4-naphthalenediones useful as anti-asthmatic agents.Type: GrantFiled: December 19, 1985Date of Patent: August 11, 1987Assignee: American Cyanamid CompanyInventors: Jeffrey B. Medwid, Lawrence W. Torley, Andrew S. Tomcufcik
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Patent number: 4670434Abstract: This invention relates to compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein the various substituents are defined herein. These compounds are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic and inotropic agents in mammals.Type: GrantFiled: November 14, 1985Date of Patent: June 2, 1987Assignee: Syntex (U.S.A.) Inc.Inventor: Michael C. Venuti
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Patent number: 4659721Abstract: Alkanol derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--CH.sub.2 X--CH.sub.2 --Y--(CH.sub.2).sub.n --NHR.sup.3 (I)which have a highly selective action on histamine-H.sub.2 receptors are described. Due to this action, these compounds may advantageously be used for treatment of diseases caused by raised gastric secretion.Type: GrantFiled: January 22, 1985Date of Patent: April 21, 1987Assignee: Ludwig Heumann & Co. GmbHInventors: Helmut Schickaneder, Stefan Postius, Istvan Szelenyi, Peter Morsdorf, Rolf Herter, Kurt H. Ahrens
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Patent number: 4656270Abstract: Novel synthetic steps and intermediates leading to guanidines such as the anti-diabetic compound linogliride.Type: GrantFiled: March 15, 1985Date of Patent: April 7, 1987Assignee: McNeilab, Inc.Inventors: Cynthia A. Maryanoff, James N. Plampin, Robin C. Stanzione
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Patent number: 4656180Abstract: Diamine derivatives corresponding to the general formula IR.sup.1 R.sup.2 N--(CH.sub.2).sub.m --Q--A--NH--R--NH--B--Q'--(CH.sub.2).sub.n NR.sup.3 R.sup.4 (I)which have a highly selective action on histamine-H.sub.2 receptors and are therefore suitable for use as anti-ulcerative agents are described. Processes for the preparation of these compounds and pharmaceutical preparations containing these compounds are also described.Type: GrantFiled: March 5, 1985Date of Patent: April 7, 1987Assignee: Ludwig Heumann & Co., GmbHInventors: Stefan Postius, Rolf Herter, Peter Morsdorf, Helmut Schickaneder, Istvan Szelenyi, Kurt H. Ahrens
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Patent number: 4642379Abstract: This invention provides certain 4-acylamino benzamide derivatives, their pharmaceutical formulations, and their use as anticonvulsant agents.Type: GrantFiled: August 30, 1985Date of Patent: February 10, 1987Assignee: Eli Lilly and CompanyInventors: Edward E. Beedle, David W. Robertson
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Patent number: 4639449Abstract: Propionylanilides, and relative salts of addition, having the following general formula: ##STR1## The new compounds are useful in the treatment of morbid cold-induced forms.Type: GrantFiled: April 23, 1986Date of Patent: January 27, 1987Assignee: Erregierre Industria Chimica SpaInventor: Egidio Molinari
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Patent number: 4634713Abstract: Certain 3-(ureidocyclohexyleneamino)propane-1,2-diol derivatives, such as the compounds of formula III below, represent novel and useful pharmaceutical agents, e.g. potent antihypertensive and cardioactive agents demonstrating both .alpha.- and .beta.-adrenergic blocking activity. ##STR1## R.sub.3 is hydrogen or lower alkyl; R.sub.7 is cyano, lower alkoxycarbonyl, pyrrolyl, morpholino, alkenyloxy of 3 to 6 carbon atoms, alkynyloxy of 3 to 6 carbon atoms, alkoxy of 1 to 3 carbon atoms substituted by cyclopropyl.Type: GrantFiled: August 19, 1985Date of Patent: January 6, 1987Assignee: Ciba-Geigy CorporationInventors: Lincoln H. Werner, Neville Ford
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Patent number: 4632987Abstract: A process for the preparation of triarylmethane compounds which comprises reacting a benzene or naphthalene compound with a formylating agent for such compounds in the presence of an acid catalyst to form an aromatic aldehyde compound; adding water to the reaction mixture and thereby hydrolyzing the acid catalyst without isolating the aromatic aldehyde compound from the reaction mixture; and uninterruptedly condensing the aromatic aldehyde compound with an aromatic compound in the resulting mixture.Type: GrantFiled: December 2, 1983Date of Patent: December 30, 1986Assignee: Mitsui Toatsu Chemicals IncorporatedInventors: Michihiro Tsujimoto, Hiroyuki Akahori, Kiyoharu Hasegawa, Makoto Asano
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Patent number: 4610985Abstract: Allophanate derivatives of the formula ##STR1## in which R.sup.1 and R.sup.2 can be identical or different and represent an aliphatic, cycloaliphatic, araliphatic or aromatic radical each of which is optionally monosubstituted or polysubstituted by identical or different substituents andR.sup.3 represents the radical --XR.sup.4 or --NR.sup.5 R.sup.6,whereinR.sup.4 represents alkyl, alkoxyalkyl, or aryl which is optionally monosubstituted or polysubstituted by identical or different substituents, X represents oxygen or sulphur andR.sup.5 and R.sup.6 are identical or different and represent hydrogen, alkyl, or aryl which is optionally monosubstituted or polysubstituted by identical or different substituents, orR.sup.5 and R.sup.6, together with the nitrogen atom on which they stand, form a saturated heterocyclic radical which is optionally monosubstituted or polysubstituted by identical or different substituents and can be interrupted by further hetero-atoms,which possess fungicidal activity.Type: GrantFiled: April 10, 1985Date of Patent: September 9, 1986Assignee: Bayer AktiengesellschaftInventors: Wolfgang Fuhrer, Engelbert Kuhle, Gerd Hanssler
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Patent number: 4605654Abstract: The present invention relates to new 2-(arylalkyloxymethyl)morpholine derivatives, the preparation thereof and their application as drugs which are useful in the treatment of disorders of the central nervous system.The 2-(arylalkyloxymethyl)morpholine derivatives according to the invention correspond to the general formula (I): ##STR1## in which: Ar denotes an aromatic group and more especially the following radicals: ##STR2## in the case where Ar denotes a phenyl radical and R denotes a hydrogen atom, an alkyl, alkoxy or halogen group, a trifluoromethyl radical, a nitro or amino group, a hydroxy group or an arylalkyloxy group.Type: GrantFiled: December 17, 1985Date of Patent: August 12, 1986Assignee: P. F. MedicamentInventors: Henri Cousse, Gilbert Mouzin, Jean-Pierre Rieu, Mike Briley, Antoine Stenger
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Patent number: 4588719Abstract: A class of bicyclic benzenoid aminoalkylene ether and thioether compounds exhibiting pharmacological activity, including anti-secretory and anti-ulcerogenic activity, pharmaceutical compositions comprising these compounds, and methods for the treatment of gastrointestinal hyperacidity and ulcerogenic disorders in mammals using said compositions.Type: GrantFiled: October 24, 1984Date of Patent: May 13, 1986Assignee: William H. Rorer, Inc.Inventors: William L. Studt, Donald E. Kuhla, Henry F. Campbell
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Patent number: 4566900Abstract: Aniline derivatives of the formula ##STR1## where R.sup.1, Y, A, Z and n have the meanings given in the description, are used for controlling undesirable plant growth.Type: GrantFiled: December 1, 1982Date of Patent: January 28, 1986Assignee: BASF AktiengesellschaftInventors: Peter Plath, Ulrich Schirmer, Gernot Reissenweber, Bruno Wuerzer, Guenter Retzlaff
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Patent number: 4556649Abstract: Insecticidally active novel substituted malonic acid diamide insecticides of the formula ##STR1## wherein R.sup.1 represents aryl or heteroaryl, each of which can optionally be substituted,R.sup.2 represents hydrogen or trialkylsilyl, and represents alkyl, cycloalkyl, alkenyl, alkinyl, aralkyl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, alkylsulphenyl, arylsulphenyl, alkylsulphonyl, arylsulphonyl, alkylaminosulphonyl, dialkylaminosulphonyl, arylaminosulphonyl or arylalkylaminosulphonyl, each of which can optionally be substituted, and represents radicals of the formula--CO--NR.sup.5 R.sup.6whereinR.sup.5 and R.sup.6 independently of one another represent hydrogen, alkyl, cycloalkyl, aryl, alkylaminocarbonyl, arylaminocarbonyl, alkylcarbonyl, arylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, alkylsulphonyl or arylsulphonyl, it being possible for these radicals to be optionally substituted,R.sup.3 represents hydrogen or the radical R.sup.4,R.sup.7 and R.sup.Type: GrantFiled: December 21, 1984Date of Patent: December 3, 1985Assignee: Bayer AktiengesellschaftInventors: Herbert Salzburg, Rudolf Fauss, Kurt Findeisen, Bernhard Homeyer
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Patent number: 4549016Abstract: Novel 2-(hydroxyphenylamino)benzamides and oxidation products thereof, useful as inhibitors of lipoxygenase, are of the formulas ##STR1## wherein R is hydrogen, lower-alkyl, halo or lower-alkoxy; R' is hydrogen or lower-alkyl; R" is hydrogen, lower-alkyl or halo; and N.dbd.Z is amino or substituted amino. The compounds of Formula I are prepared by de-etherification of the corresponding alkyl or benzyl ethers; and the compounds of Formula II are prepared by oxidation of the compounds of Formula I where R' is hydrogen and OH is in the 4-position.Type: GrantFiled: January 9, 1985Date of Patent: October 22, 1985Assignee: Sterling Drug Inc.Inventor: Denis M. Bailey
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Patent number: 4544755Abstract: Phthalimides of the formula I ##STR1## where R is a substituent and the ring A can be further substituted, are cleaved by a process in which a compound of the formula I is treated with an alkanolamine.The compounds prepared according to the invention are useful intermediates for the preparation of dyes, drugs and plastics.Type: GrantFiled: May 23, 1984Date of Patent: October 1, 1985Assignee: Basf AktiengesellschaftInventors: Helmut Hagen, Rolf-Dieter Kohler
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Patent number: 4537989Abstract: A compound of the formula ##STR1## wherein X.sup.1 is a free or an esterified carboxyl group, or a group of the formula: ##STR2## (R.sup.a and R.sup.b are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7 membered saturated heterocyclic group), Y is a group of the formula: ##STR3## (R.sup.6 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) or ##STR4## (R.sup.6 is as defined above), R.sup.1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sup.2 is a hydrogen atom or R.sup.1 and R.sup.2, when taken together, mean a single linkage to form a double bond between the carbon atoms which they are linked, R.sup.3 is a hydroxyl group or a protected hydroxyl group, R.sup.4 is a hydrogen atom or a C.sub.1 -C.sub.Type: GrantFiled: April 15, 1983Date of Patent: August 27, 1985Assignee: Sumitomo Chemical Company, LimitedInventors: Keiichi Ono, Akihiko Sugie, Masami Muraoka, Michihiro Yamamoto
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Patent number: 4536598Abstract: A new color-forming 4-(4'-secondary or tertiary-amino)anilino-1-carboxamidonaphthalene dye precursor in a photographic material and process enables formation of a dye image by means of cross-oxidation without the need for a coupling reaction. The color-forming 4-(4'-secondary or tertiary-amino)anilino-1-carboxamidonaphthalene dye precursor is useful in a photographic silver halide material for producing (i) a dye image, or (ii) a dye image and silver image. The exposed photographic material is processed to produce (a) a positive dye image, (b) a negative dye and negative silver image, (c) a negative dye image or (d) a positive dye image and a positive silver image. New naphthoquinoneimide dyes are also described.Type: GrantFiled: March 10, 1983Date of Patent: August 20, 1985Assignee: Eastman Kodak CompanyInventors: James E. Klijanowicz, Csaba A. Kovacs
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Patent number: 4532249Abstract: New acyl derivatives of p-aminophenol and esters of same useful as pharmacologically active ingredients and process for their preparation.Type: GrantFiled: October 28, 1982Date of Patent: July 30, 1985Inventors: Francois Molnar, Suzanne Szabo, Peter R. Statkov, Manuel Armijo, Carlos Sunkel, Fernando Cillero
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Patent number: 4530925Abstract: Compounds are described of the formulae (1a) and (1b) ##STR1## in which: --COR.sup.1 is an ester group,n is 1 or 2,W is C.sub.1-7 alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,Y is a saturated heterocyclic amino group,R.sup.2 is substituted or unsubstituted phenylalkyl, thienylalkyl or naphthylalkyl or cinnamyl, andR.sup.3 is --H or C.sub.1-5 alkanoyl, including their salts.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic or antiasthmatic agents.Type: GrantFiled: March 14, 1984Date of Patent: July 23, 1985Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw
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Patent number: 4510139Abstract: Novel 2-(hydroxyphenylamino)benzamides and oxidation products thereof, useful as inhibitors of lipoxygenase, are of the formulas ##STR1## wherein R is hydrogen, lower-alkyl, halo or lower-alkoxy; R' is hydrogen or lower-alkyl; R" is hydrogen, lower-alkyl or halo; and N.dbd.Z is amino or substituted amino. The compounds of Formula I are prepared by de-etherification of the corresponding alkyl or benzyl ethers; and the compounds of Formula II are prepared by oxidation of the compounds of Formula I where R' is hydrogen and OH is in the 4-position.Type: GrantFiled: January 6, 1984Date of Patent: April 9, 1985Assignee: Sterling Drug Inc.Inventor: Denis M. Bailey
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Patent number: 4488993Abstract: Novel phenylamidinourea compounds and processes for their preparation are described. These compounds have an effective degree of anti-hypertensive properties and exert activities on the cardiovascular system. A method for the treatment of hypertensive disorders is also described.Type: GrantFiled: October 25, 1982Date of Patent: December 18, 1984Assignee: William H. Rorer, Inc.Inventors: George H. Douglas, Julius Diamond
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Patent number: 4482549Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienzlalkyl, naphthylalkyl or cinnamyl, and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstriction and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: February 8, 1984Date of Patent: November 13, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter, Alan Wadsworth
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Patent number: 4478836Abstract: The present invention concerns new derivatives of 1-aryl 2-aminomethyl cyclopropane carboxamides (Z) of general formula I: ##STR1## in which: R represents a hydrogen or halogen atom, a lower alkyl group, a lower alkoxy group, or a hydroxy. nitro or amino group;n represents the value 1 or 2;R.sub.1 and R.sub.2 represent a hydrogen atom, a lower alkyl group, an aryl or lower alkaryl group, possibly substituted, preferably in para position, by a halogen atom, preferably a chlorine atom;R.sub.1 and R.sub.2 may also form a heterocycle having 5 or 6 members with the adjacent nitrogen atom;R.sub.3 and R.sub.4 represent a hydrogen atom or a lower alkyl group;R.sub.3 and R.sub.Type: GrantFiled: June 22, 1982Date of Patent: October 23, 1984Assignee: Pierre Fabre S.A.Inventors: Gilbert Mouzin, Henri Cousse, Bernard Bonnaud, Michel Morre, Antoine Stenger
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Patent number: 4447428Abstract: Prostanoid compounds are described having the formula: ##STR1## where A is a cyclopentane ring, which is substituted by oxo and/or hydroxy or etherified hydroxy and may be saturated or unsaturated; X is --CH.dbd.CH--or --(CH.sub.2).sub.2 --; R is alkyl having a terminal --COOH or ester group; and Y is amino or substituted amino, particularly heterocyclic amino.The compounds have bronchodilator activity and/or inhibit blood platelet aggregation.The preparation and pharmaceutical formulation of the compounds is also described.Type: GrantFiled: July 15, 1983Date of Patent: May 8, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Harry Finch, Roger F. Newton
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Patent number: 4438112Abstract: Prostanoids are described of the formulae ##STR1## (and the salts thereof) in which: X is cis or trans --CH.dbd.CH-- or CH.sub.2 CH.sub.2 --;R.sup.1 is C.sub.1-7 alkyl terminated by --COOR.sup.10 where R.sup.10 is H, C.sub.1-6 alkyl or aralkyl;Y is a saturated heterocyclic amino group; andR.sup.4 is aralkyl (in which the aryl portion is substituted by alkylthio, alkylsulphinyl, alkylsulphonyl, alkanoylamino, aroylamino, phenalkyl, aminosulphonyl, alkanoylaminosulphonyl, phenylsulphonyl, nitro, tetrazolyl, substituted phenyl or thienyl).These compounds inhibit blood platelet aggregation and have bronchodilatory action, and may be formulated for use as anti-asthmatics and antithrombotic agents.Type: GrantFiled: September 17, 1982Date of Patent: March 20, 1984Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, John Bradshaw
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Patent number: 4436935Abstract: The invention relates to thiocarbamoylalkoxyphenylureas of the general formula ##STR1## wherein X is hydrogen, halogen, C.sub.1 -C.sub.2 haloalkoxy or C.sub.1 -C.sub.2 haloalkyl,Y is a thiocarbamoylalkyl group of the formula ##STR2## n is 0, 1 or 2, R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl or C.sub.1 -C.sub.4 alkoxy,R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 alkenyl,R.sub.3, R.sub.4 and R.sub.6, each independently or the other, are hydrogen or C.sub.1 -C.sub.4 alkyl,R.sub.5 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or C.sub.2 -C.sub.5 alkoxyalkyl,R.sub.7 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 alkoxy or C.sub.1 -C.sub.2 alkylphenyl, andR.sub.8 is hydrogen or C.sub.1 -C.sub.4 alkyl, while R.sub.1 and R.sub.2 or R.sub.7 and R.sub.Type: GrantFiled: August 7, 1981Date of Patent: March 13, 1984Assignee: Ciba-Geigy CorporationInventors: Dagmar Berrer, Georg Pissiotas, Otto Rohr
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Patent number: 4435567Abstract: A process for the preparation of substituted urea derivatives, and compositions and concentrates for the same purpose are disclosed. According to the process the substituted urea derivatives of formula (I) ##STR1## wherein R is hydrogen, alkyl, aryl, cycloalkyl or aralkyl, R.sup.1 and R.sup.2 are hydrogen, alkyl, alkenyl, alkinyl, alkoxy, oxyalkyl, cycloalkyl, aralkyl, alkoxycarbonylalkyl, aryl or heteroaryl, or R.sup.1 and R.sup.Type: GrantFiled: December 28, 1981Date of Patent: March 6, 1984Assignee: Chinoin Gyogyszer es Vesgyeszeti Termekek Gyara R. T.Inventors: Gyorgy Lugosi, Antal Simay, Janos Bodnar, Laszlo Simandi, Eva Somfai
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Patent number: 4435187Abstract: The reduction of octane requirement in a spark-ignited, internal combustion engine is achieved by introducing, with the combustion intake charge, a fuel and/or lubricant composition containing an octane requirement reduction amount of a substituted urea compound represented by the formula: ##STR1## in which X is an oxygen or sulfur atom, R.sub.1 and R.sub.3 are hydrocarbyl radicals having from 1 to 3 carbon atoms, and R.sub.2 is selected from the group consisting of ##STR2## Particularly useful as ORR agents are: (a) 4-[N-(2,4-xylyl) carbamoyl] morpholine;(b) 1-[N-(2,4-xylyl) carbamoyl] piperidine; and(c) 1-(2-pyridyl)-3-(3,4-xylyl)-2-thiourea.Type: GrantFiled: December 31, 1981Date of Patent: March 6, 1984Assignee: Shell Oil CompanyInventors: L. B. Graiff, T. E. Kiovsky
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Patent number: 4414211Abstract: 5-Membered, 6-membered and 7-membered heterocyclic derivatives of guanidine having hypoglycemic activity.Type: GrantFiled: March 14, 1980Date of Patent: November 8, 1983Assignee: McNeilab, Inc.Inventor: Chris R. Rasmussen
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Patent number: 4410521Abstract: Compounds are described of the formula ##STR1## in which --COR.sup.1 is a complex ester or thioester group,W is alkylene,X is cis or trans --CH.dbd.CH or --CH.sub.2 CH.sub.2 --,n is 1 or 2,Y is a saturated heterocyclic amino group having 5-8 ring members, andR.sup.2 is unsubstituted or substituted phenylalkyl, thienylalkyl, naphthylalkyl or cinnamyl,and their salts and solvates.These compounds inhibit blood platelet aggregation and bronchoconstruction and may be formulated for use as antithrombotic and antiasthmatic agents.Type: GrantFiled: September 16, 1982Date of Patent: October 18, 1983Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Peter Hallett, Christopher J. Wallis, Norman F. Hayes, John Bradshaw, Malcolm Carter
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Patent number: 4410697Abstract: The invention relates to a new method for the preparation of N-aryl-N'-(mono- or disubstituted)-urea derivatives having the general formula (I), ##STR1## wherein Aryl is an optionally substituted phenyl group, andR.sup.1 and R.sup.2 each stand for an optionally substituted alkyl, cycloalkyl, alkoxy or phenyl group, orR.sup.1 and R.sup.2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic group which may contain a further hetero atom, orone of R.sup.1 and R.sup.2 may also stand for hydrogen,with the proviso that if one of R.sup.1 and R.sup.2 is an optionally substituted phenyl group, the other may represent only hydrogen atom or an optionally substituted alkyl or alkoxy group,by reacting a carbamate of the general formula (II) with an amine of the general formula (III),R.sup.1 R.sup.2 N--CO--X (II)Aryl--NH.sub.2 (III)or a carbamate of the general formula (IV) with an amine of the general formula (V),Aryl--NH--CO--X (IV)R.sup.1 R.sup.2 NH (V)wherein R.sup.1, R.sup.Type: GrantFiled: August 28, 1981Date of Patent: October 18, 1983Assignee: Reanal FinomvegyszergyarInventors: Sandor Torok, Lajos Voroshazy, Peter Galambos, Ivan Daroczi, Zoltan Ormenyi
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Patent number: 4409213Abstract: Prostanoid compounds are described having the formula: ##STR1## where A is a cyclopentane ring, which is substituted by oxo and/or hydroxy or etherified hydroxy and may be saturated or unsaturated; X is --CH.dbd.CH-- or --(CH.sub.2).sub.2 --; R is alkyl having a terminal --COOH or ester group; and Y is amino or substituted amino, particularly heterocyclic amino.The compounds have bronchodilator activity and/or inhibit blood platelet aggregation.The preparation and pharmaceutical formulation of the compounds is also described.Type: GrantFiled: November 10, 1982Date of Patent: October 11, 1983Assignee: Glaxo Group LimitedInventors: Eric W. Collington, Harry Finch, Roger F. Newton, Christopher J. Wallis
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Patent number: 4402953Abstract: Amino aceto anilides of the formula I shown hereinafter are effective microbicides. They may be used to control fungi on plants or parts of plants or to prevent them from fungi attack.Type: GrantFiled: November 10, 1980Date of Patent: September 6, 1983Assignee: Ciba-Geigy CorporationInventors: Adolf Hubele, Walter Kunz, Wolfgang Eckhardt
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Patent number: 4395413Abstract: The invention relates to novel oxime ethers of the general formula /I/ and acid addition salts and quaternary ammonium derivatives thereof, ##STR1## wherein A represents a C.sub.2-6 straight or branched alkylene chain,R and R.sup.1 each represent a C.sub.1-6 alkyl group or they form together with the adjacent nitrogen atom a heterocyclic ring containing 4 to 7 carbon atoms and optionally a further hetero atom, i.e. an oxygen, sulfur or nitrogen atom, and said ring may be optionally substituted by a C.sub.1-3 alkyl, phenyl or benzyl group,R.sup.2 and R.sup.3 each denote a hydrogen atom or together form a valency bond,R.sup.4 denotes a C.sub.1-10 alkyl or C.sub.2-10 alkenyl group, andn denotes an integer from 3 to 7.The compounds of the general formula /I/ are prepared according to the invention by reacting a cycloalkane derivative of the general formula /II/ ##STR2## wherein R.sup.2, R.sup.3, R.sup.4 and n have the same meaning as above, whereasY denotes an oxygen or sulphur atom or a .dbd.Type: GrantFiled: June 24, 1980Date of Patent: July 26, 1983Assignee: Egyt Gyogyszervegyeszeti GyarInventors: Zoltan Budai, Aranka Lay nee Konya, Tibor Mezei, Lujza Petocz, Katalin Grasser, Ibolya Kosoczky, Eniko Szirt nee Kiszelly, Peter Gorog
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Patent number: 4393077Abstract: Compounds having the formula: ##STR1## wherein X.sub.1, X.sub.2, R, R.sub.1, R.sub.2 and R.sub.3 are as set forth hereinafter, their preparation and uses as ganglionic blocking agents are disclosed.Type: GrantFiled: July 2, 1981Date of Patent: July 12, 1983Assignee: William H. Rorer, Inc.Inventors: George H. Douglas, Henry F. Campbell
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Patent number: 4382930Abstract: The present invention relates to 2'-(ortho-chlorobenzoyl)-4'-chloroglycylanilides, compositions thereof, and their use as medicaments, e.g., as anxiolytic agents.The compounds of the invention have the general formula I ##STR1## in which R represents hydrogen or alkyl,R.sub.1 and R.sub.2 may be identical or different and are selected from hydrogen, alkyl, hydroxyalkyl, alkenyl, and alkynyl, possibly substituted by alkyl, and cycloalkyl having three to six members, possibly substituted by alkyl, with the proviso that, when one of R.sub.1 and R.sub.2 represents hydrogen, the other is not lower alkyl or hydroxyalkyl; and with the further proviso that R.sub.1 and R.sub.2 may not simultaneously represent either hydrogen or lower-alkyl. R.sub.1 and R.sub.2 may furthermore form, with the nitrogen atom to which they are connected, a nitrogen heterocycle possibly containing a second heteroatom selected from oxygen and nitrogen.Type: GrantFiled: December 29, 1980Date of Patent: May 10, 1983Assignee: Pierre Fabre S.A.Inventors: Gilbert Mouzin, Henri Cousse, Antoine Stenger