Chalcogen Or Nitrogen Attached Directly To Ring Carbon Of The Thiadiazole Ring By Nonionic Bonding Patents (Class 548/135)
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Patent number: 4803211Abstract: This invention relates to novel heterocyclic compounds structurally characterized by containing a specific heterocyclic group and by the presence of --CH.sub.2 --S-- directly bound to the specific heterocyclic group. These heterocyclic compounds are useful as medicines, particularly as antagonists of SRS-A (slow reacting substance of anaphylaxis).Type: GrantFiled: July 14, 1986Date of Patent: February 7, 1989Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Toshiyasu Mase, Ryuji Tsuzuki, Hiromu Hara, Kiyoshi Murase, Kenichi Tomioka
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Patent number: 4782083Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein: one of R.sub.1 and R.sub.2 is hydrogen or C.sub.1-4 alkyl and the other is C.sub.1-4 alkyl or R.sub.1 and R.sub.2 together are C.sub.2-5 -polymethylene;either R.sub.3 is hydrogen, hydroxy, C.sub.1-6 alkoxy or C.sub.1-7 acyloxy and R.sub.4 is hydrogen or R.sub.3 and R.sub.4 together are a bond;R.sub.5 is hydrogen C.sub.1-6 alkyl optionally substituted by halogen hydroxy, C.sub.1-6 alkoxy, C.sub.1-6 alkoxycarbonyl, carboxy or amino optionally substituted by one or two independent C.sub.1-6 alkyl groups, or C.sub.2-6 alkenyl, amino optionally substituted by a C.sub.1-6 alkyl or C.sub.1-6 alkenyl group or by a C.sub.1-6 alkanoyl group optionally substituted by up to three halo atoms, by a phenyl group optionally substituted by C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen, or aryl or hetroaryl, either being optionally substituted by one or more groups or atoms selected from the class of C.sub.1-6 alkyl, C.sub.Type: GrantFiled: August 29, 1986Date of Patent: November 1, 1988Assignee: Beecham Group P.L.C.Inventors: Frederick Cassidy, Geoffrey Stemp, John M. Evans
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Patent number: 4778897Abstract: Novel 6H-dibenz[b,e][1,4]oxathiepin derivatives of the formulae I and Ia are employed in the treatment and control of allergic conditions such as allergic asthma.Type: GrantFiled: May 28, 1987Date of Patent: October 18, 1988Assignee: Merck & Co., Inc.Inventors: Edward J. Cragoe, Jr., Clarence S. Rooney, Joshua Rokach
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Patent number: 4772309Abstract: A 5-Acylamino-pyrazole derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen or nitro,R.sup.2 represents hydrogen, alkyl, alkenyl, alkinyl or optionally substituted cycloalkyl,R.sup.3 represents hydrogen or alkyl,R.sup.4 represents hydrogen or alkyl,X represents oxygen or sulphur,n represents the integer 0, 1 or 2,Ar represents in each case optionally substituted phenyl or pyridyl andHet represents an optionally substituted 5- or 6- membered heterocyclic radical linked via a carbon atom,which exhibit herbicidal and plant growth regulating activity.Type: GrantFiled: March 19, 1987Date of Patent: September 20, 1988Assignee: Bayer AktiengesellschaftInventors: Jorg Stetter, Reinhold Gehring, Otto Schallner, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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Patent number: 4762848Abstract: Heterocyclic sulfides of the general formula heterocycle-S-R, a process for their preparation and, in particular, their use for immunostimulation, immunorestoration and cytostatic treatment, and pharmaceutical agents, which contain a sulfide of this type, for these indications.Type: GrantFiled: March 10, 1986Date of Patent: August 9, 1988Assignee: Hoechst AktiengesellschaftInventors: Karl-Heinz Scheunemann, Walter Durckheimer, Jurgen Blumbach, Michael Limbert, Hans-Ulrich Schorlemmer, Gerhard Dickneite, Hans-Harald Sedlacek
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Patent number: 4746669Abstract: Thiazole derivatives have been made, for example, by reacting a 2-aryl-2,2-dialkoxyethylamine with an appropriately substituted aryl acetyl halide followed by treating the resulting amide with diphosphoryl pentasulfide. The thiazole derivatives are found to be effective immunoregulants.Type: GrantFiled: March 26, 1987Date of Patent: May 24, 1988Assignee: Merck & Co., Inc.Inventors: Charles G. Caldwell, Ihor Kopka, Milton L. Hammond, Robert A. Zambias
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Patent number: 4746672Abstract: Sulphur derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion of the formula I: ##STR1## in which R.sup.1 and R.sup.2 independently are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene or a 1-8C alkylene chain into which is optionally inserted one or two groups; p is 1 or 2; R.sup.3 is a variety of radicals described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes for the derivatives, intermediates and pharmaceutical compositions are also part of the invention.Type: GrantFiled: May 10, 1982Date of Patent: May 24, 1988Assignee: ICI Americas Inc.Inventors: Tobias O. Yellin, Philip N. Edwards, Michael S. Large
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Patent number: 4743600Abstract: A class of benzocyclobutene 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: July 28, 1986Date of Patent: May 10, 1988Assignee: Rorer Pharmaceutical CorporationInventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
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Patent number: 4742060Abstract: Novel insecticides of the formula ##STR1## in which n is 0 or 1,X is S, O, ##STR2## Y is N or ##STR3## Z is a 5- or 6-membered nitrogen-containing heterocyclic ring, and R to R.sup.9 variously represent hydrogen or specified organic radicals.Type: GrantFiled: January 21, 1986Date of Patent: May 3, 1988Assignee: Nihon Tokushu Noyaku Seizo K. K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
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Patent number: 4740231Abstract: 1-Aryl-5-alkoximinoalkylamino-pyrazoles of the formula ##STR1## in which R represents cyano or nitro, or represents an optionally substituted heterocyclic radical,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl, or represents optionally substituted aryl,R.sup.3 represents hydrogen, alkyl or alkenyl, or represents in each case optionally substituted aralkyl or aryl andAr represents optionally substituted phenyl or pyridyl,are active as herbicides and plant growth regulants. Compounds of the formula ##STR2## in which R" has the same definition as R other than cyano, are also active and useful as intermediates as well.Type: GrantFiled: May 22, 1986Date of Patent: April 26, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhold Gehring, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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Patent number: 4732980Abstract: This invention relates to intermediates of Mannich-alkynyl aminothiadiazole oxides having histamine H.sub.2 -antagonist activity. A particular final product of this invention is 3-amino-4-[7-piperidinohept-5-ynylamino]-1,2,5-thiadiazole-1-oxide.Type: GrantFiled: December 8, 1986Date of Patent: March 22, 1988Assignee: Smith Kline & French Laboratories LimitedInventors: Thomas H. Brown, Peter Blurton
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Patent number: 4695311Abstract: This invention relates to ortho-(isoxazolyl, isothiazolyl, pyrazolyl, thiadiazolyl, oxadiazolyl, and triazolyl)benzenesulfonamides and their use as herbicides.Type: GrantFiled: May 9, 1986Date of Patent: September 22, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Morris P. Rorer
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Patent number: 4695567Abstract: The present invention provided pyrrolobenzimidazoles or tautomer thereof, of the general formula: ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.3 -C.sub.7 cycloalkyl;R.sub.2 is hydrogen, cyano, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or a carbonyl group substituted by hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyoxy, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino or hydrazino, orR.sub.2 and R.sub.1 together with the carbon to which they are attached form a C.sub.3 -C.sub.8 spirocycloalkyl ring, or R.sub.1 and R.sub.2 together form C.sub.3 -C.sub.7 alkylidene or C.sub.3 -C.sub.7 cycloalkylkidene,X is a valency bond, C.sub.1 -C.sub.Type: GrantFiled: January 17, 1986Date of Patent: September 22, 1987Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Jens-Peter Holck, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein, Egon Roesch
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Patent number: 4692531Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.Type: GrantFiled: September 25, 1986Date of Patent: September 8, 1987Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4673747Abstract: Substituted aminoalkylphenoxy derivatives represented by the general formula of: ##STR1## wherein the substituting group Z is either one of the following groups of: ##STR2## were prepared. These derivatives exert antagonism against Histamine H.sub.2 -receptors and hence are efficacious for the treatments of digestive ulcers.Type: GrantFiled: December 3, 1985Date of Patent: June 16, 1987Assignee: Ikeda Mohando Co., Ltd.Inventors: Fujio Nohara, Tomoaki Fujinawa
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Patent number: 4668673Abstract: A class of bicyclic benzo-oxy heterocyclic 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: July 2, 1986Date of Patent: May 26, 1987Assignee: William H. Rorer, Inc.Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt, Kent W. Neuenschwander
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Patent number: 4663331Abstract: This invention relates to Mannich-alkynyl aminothiadiazole oxides having histamine H.sub.2 -antagonist activity. A particular compound of this invention is 3-amino-4-[7-piperidinohept-5-ynylamino]-1,2,5-thiadiazole-1-oxide.Type: GrantFiled: January 16, 1986Date of Patent: May 5, 1987Assignee: SmithKline & French Laboratories LimitedInventors: Thomas H. Brown, Peter Blurton
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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: 4656176Abstract: 2,3-Unsaturated nitrogen-containing heterocyclic compounds with a 3-nitro group and a 2-heterocyclyl alkylamino group. The alkyl group of 2-position substituents is preferably interrupted by sulfur or oxygen. The compounds of the invention are preferably dihydropyrroles or tetrahydropyrridines or pyrimidines. The compounds of the invention are histamine H.sub.2 -receptor antagonists.Type: GrantFiled: March 21, 1985Date of Patent: April 7, 1987Assignee: SmithKline & French Laboratories LimitedInventors: Michael L. Roantree, Rodney C. Young
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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: 4647559Abstract: 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: May 23, 1986Date of Patent: March 3, 1987Assignee: William H. Rorer, Inc.Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
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Patent number: 4644006Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.Type: GrantFiled: June 22, 1984Date of Patent: February 17, 1987Assignee: Bristol-Myers CompanyInventors: Aldo A. Algieri, Ronnie R. Crenshaw
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Patent number: 4639523Abstract: Substituted aminoalkylphenoxy derivatives represented by the general formula of: ##STR1## wherein the substituting group Z is either one of the following groups of: ##STR2## These derivatives exert antagonism against Histamine H.sub.2 -receptors and hence are efficacious for the treatments of digestive ulcers.Type: GrantFiled: May 24, 1985Date of Patent: January 27, 1987Assignee: Ikeda Mohando Co., Ltd.Inventors: Fujio Nohara, Tomoaki Fujinawa
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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: 4623652Abstract: 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: January 16, 1985Date of Patent: November 18, 1986Assignee: American Hospital Supply CorporationInventors: Paul W. Erhardt, William L. Matier
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Patent number: 4622403Abstract: Novel dibenz[b,f]thiepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma.Type: GrantFiled: October 11, 1983Date of Patent: November 11, 1986Assignee: Merck Frosst Canada, Inc.Inventors: Haydn Williams, Joshua Rokach
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Patent number: 4607106Abstract: Pyridine derivatives are disclosed which are useful as histamine H.sub.1 -antagonists.Type: GrantFiled: May 17, 1985Date of Patent: August 19, 1986Assignee: Smith Kline & French Laboratories LimitedInventor: Robert J. Ife
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Patent number: 4606755Abstract: This invention relates to ortho-(isoxazolyl, isothiazolyl, pyrazolyl, thiadiazolyl, oxadiazolyl, and triazolyl)benzenesulfonamides and their use as herbicides.Type: GrantFiled: December 21, 1984Date of Patent: August 19, 1986Assignee: E. I. Du Pont de Nemours and CompanyInventor: Morris P. Rorer
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Patent number: 4600779Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.Type: GrantFiled: April 16, 1984Date of Patent: July 15, 1986Assignee: Bristol-Myers CompanyInventors: Ronnie R. Crenshaw, Aldo A. Algieri
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Patent number: 4593039Abstract: 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 antihypertensive, antianginal, antiarrhythmic and cardioprotective agents and in the treatment of elevated intraocular pressure such as glaucoma.Type: GrantFiled: April 2, 1984Date of Patent: June 3, 1986Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Sandor L. Varga, Gerald S. Ponticello
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Patent number: 4578470Abstract: Phthalimides and the like in which the substituent on the imide nitrogen is a highly electron-deficient group may be prepared by the reaction of the appropriate amine with phthalic anhydride. These imides are useful for the preparation of polyimides by reaction with diamines.Type: GrantFiled: June 20, 1983Date of Patent: March 25, 1986Assignee: General Electric CompanyInventor: Jimmy L. Webb
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Patent number: 4578388Abstract: The compounds are C.sub.2 -C.sub.8 straight chain alkanes terminally substituted, symmetrically or unsymmetrically, by N-(N'-substituted guanidino), N-(N',N"-disubstituted guanidino). N-(N'-substituted thioureido), N-(nitromethylene amidino) or S-(N-substituted isothioureido) groups. Two compounds of the invention are 1,3-bis-[N'-(2-(5-methyl-4-imidazolylmethylthio)ethyl)guanidino]propane and 1,3-bis-[S-(N-2-(5-methyl-4-imidazolylmethylthio)ethyl)isothioureido]p ropane. The compounds of this invention are inhibitors of H-2 histamine receptors.Type: GrantFiled: June 30, 1983Date of Patent: March 25, 1986Assignee: SmithKline & French Laboratories LimitedInventors: Graham J. Durant, Charon R. Ganellin
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Patent number: 4578390Abstract: Hydroxybenzylamino derivatives have been prepared from an appropriate hydroxybenzaldehyde and an amine followed by reduction. These compounds are found to be active topical anti-inflammatory agents.Type: GrantFiled: April 13, 1983Date of Patent: March 25, 1986Assignee: Merck & Co., Inc.Inventors: Norman P. Jensen, Michael N. Chang
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Patent number: 4567191Abstract: Novel amino-phenyl-thiadiazoledioxides and related compounds and processes for preparing such compounds are disclosed. The compounds are useful for suppressing gastric acid secretions in mammals.Type: GrantFiled: June 7, 1983Date of Patent: January 28, 1986Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Adolph Pietruszkiewicz, William A. Bolhofer, William C. Lumma, Jr.
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Patent number: 4562184Abstract: Novel substituted-aminohydroxypropoxy-thiadiazoles and pharmaceutically acceptable salts thereof exhibit .beta.-adrenergic blocking activity.Type: GrantFiled: April 2, 1984Date of Patent: December 31, 1985Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello
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Patent number: 4555521Abstract: A method for controlling nematodes in agricultural crops utilizing selected 3-substituted-4-phenyl-1,2,5-thiadiazoles, nematicidal compositions thereof, and novel compounds useful therefor are disclosed and exemplified.Type: GrantFiled: November 16, 1983Date of Patent: November 26, 1985Assignee: FMC CorporationInventors: John F. Engel, Joseph M. Puglis
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Patent number: 4543352Abstract: A class of naphthalene 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 are disclosed.Type: GrantFiled: April 29, 1983Date of Patent: September 24, 1985Assignee: William H. Rorer, Inc.Inventors: Donald E. Kuhla, Henry F. Campbell, William L. Studt
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Patent number: 4539317Abstract: Novel 4-substituted amino-3-[3-alkylindoloamino-2-hydroxypropoxy] thiadiazole compounds and methods for their preparation are disclosed. These compounds and their salts exhibit pharmacological activity including antihypertensive and .beta.-adrenergic blocking activity.Type: GrantFiled: April 9, 1984Date of Patent: September 3, 1985Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, Gerald S. Ponticello
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Patent number: 4528378Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.Type: GrantFiled: April 16, 1984Date of Patent: July 9, 1985Assignee: Bristol-Myers CompanyInventors: Ronnie R. Crenshaw, Aldo A. Algieri
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Patent number: 4528377Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.1 are as defined herein, and their nontoxic pharmaceutically acceptable salts, hydrates and solvates are novel anti-ulcer agents which are prepared by ring closure of a substituted ethanediimidamide of the formula ##STR2## .Type: GrantFiled: March 16, 1983Date of Patent: July 9, 1985Assignee: Bristol-Myers CompanyInventors: Ronnie R. Crenshaw, Aldo A. Algieri
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Patent number: 4528375Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.Type: GrantFiled: April 16, 1984Date of Patent: July 9, 1985Assignee: Bristol-Myers CompanyInventors: Ronnie R. Crenshaw, Aldo A. Algieri
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Patent number: 4517366Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.Type: GrantFiled: April 16, 1984Date of Patent: May 14, 1985Assignee: Bristol-Myers CompanyInventors: Ronnie R. Crenshaw, Aldo A. Algieri
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Patent number: 4508725Abstract: Novel compounds are disclosed having the formula ##STR1## wherein R is lower alkyl, lower cycloalkyl, lower haloalkyl, lower alkylcarboxymethyl, arylcarboxymethyl, lower alkenyl, lower alkynyl, aryl having from 6 to about 10 carbon atoms, or aralkyl; R.sub.1 is lower alkyl, lower hydroxyalkyl, lower alkenyl, lower alkynyl, aralkyl, or --WB; where 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, where 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.sub.5 are not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.3 or --NR.sub.2 COOR.sub.5, or R.sub.3 and R.sub.Type: GrantFiled: December 22, 1982Date of Patent: April 2, 1985Assignee: American Hospital Supply CorporationInventors: William L. Matier, Paul W. Erhardt, Ghanshyam Patil
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Patent number: 4504304Abstract: Novel compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are H or alkyl and R is an optionally-substituted unsaturated, cycloalkyl, secondary-alkyl, aromatic or heterocyclic group, are useful as plant growth regulators and herbicides. Certain intermediates are also novel.Type: GrantFiled: August 29, 1983Date of Patent: March 12, 1985Assignee: Shell Oil CompanyInventors: Herbert Estreicher, George B. Payne
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Patent number: 4497813Abstract: Derivatives of 3-aminopropane-1,2-diol of the formula ##STR1## in which Ar represents optionally substituted aryl,n represents the number 0 or 1, andalk represents alkylene having 2 to 5 carbon atoms, the nitrogen atom and the oxygen atom, or, if n is zero, the phenyl radical, being separated from one another by at least two carbon atoms, andR.sub.1 and R.sub.2, independently of one another, each represents hydrogen or lower alkyl, or together they represent lower alkylene, oxa-lower alkylene, thia-lower alkylene, aza-lower alkylene or N-lower alkyl-aza-lower alkylene,and salts of such compounds, processes for their manufacture, medicaments containing the new compounds and their use for the treatment of Angina pectoris and cardiac arrhythmia, and as blood pressure-reducing agents, as well as for the treatment of reactive or endogenic states of depression.Type: GrantFiled: May 14, 1982Date of Patent: February 5, 1985Assignee: Ciba-Geigy CorporationInventors: Franz Ostermayer, Markus Zimmermann
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Patent number: 4463176Abstract: A process for resolving a racemic modification of .beta.-adrenergic aryl- or hetaryl-oxypropanolamines such as (.+-.)-2-[2-hydroxy-3-[[2-(1H-indol-3-yl)-1,1-dimethylethyl]amino]propoxy] benzonitrile into its individual enantiomers is described. The process comprises converting the racemic modification into a pair of diastereomeric urea derivatives by reaction with a chiral aralkylisocyanate; separation into the individual diastereomers; and facile regeneration of the starting amine by cleavage of the intermediate urea compound using hydrazine. This final step is improved by the addition of an .alpha.-keto carboxylic acid, such as pyruvic acid, which functions as a scavenger of nucleophilic by-products.Type: GrantFiled: September 13, 1982Date of Patent: July 31, 1984Assignee: Mead Johnson & CompanyInventors: Ronald D. Dennis, Terence M. Dolak, William E. Kreighbaum
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Patent number: 4440775Abstract: The compounds are novel N-substituted-N'-heterocyclic alkylthioureas, guanidines and 1-nitro-2,2-diaminoethylene compounds which are histamine H.sub.2 -antagonists.Type: GrantFiled: June 18, 1982Date of Patent: April 3, 1984Assignee: Smith Kline & French Laboratories LimitedInventors: Graham J. Durant, Charon R. Ganellin, Geoffrey R. Owen, Rodney C. Young
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Patent number: 4440933Abstract: Histamine H.sub.2 -receptor antagonists of the formula ##STR1## wherein A, m, Z, n and R.sup.1 are as defined herein, and their nontoxic pharmaceutically acceptable salts, hydrates and solvates are novel anti-ulcer agents which are prepared by ring closure of a substituted ethanediimidamide of the formula ##STR2## with a compound of the formulaR--S--Rin which R is as defined herein.Type: GrantFiled: March 16, 1983Date of Patent: April 3, 1984Assignee: Bristol-Myers CompanyInventor: Thomas A. Montzka
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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: 4411899Abstract: There are disclosed substituted derivatives of amino alkane diols and related compounds as well as processes for the preparation of such compounds. These compounds are useful for the suppression of gastric acid secretions in mammals and compositions for such uses are also disclosed.Type: GrantFiled: December 21, 1981Date of Patent: October 25, 1983Assignee: Merck & Co., Inc.Inventors: John J. Baldwin, William C. Lumma, Jr.