Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Nitrogen Patents (Class 549/69)
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Patent number: 5280026Abstract: Thienopyrimidine compounds are disclosed as inhibitors of the H.sup.+ K.sup.+ ATPase enzyme useful in the treatment of gastric acid secretion. A compound of the invention is 2-(2-methylphenylamino)-4-(N-methylphenylamino)thieno[3,2-d]pyrimidine.Type: GrantFiled: November 24, 1992Date of Patent: January 18, 1994Assignee: SmithKline Beecham Intercredit B.V.Inventors: Thomas H. Brown, Robert J. Ife, Colin A. Leach
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Patent number: 5246962Abstract: Retinoid-like activity is exhibited by compounds of the formula ##STR1## where R is hydrogen or lower alkyl; A is pyridyl, thienyl, furyl, pyridazinyl, pyrimidinyl or pyrazinyl; n is 0-5; and B is H, --COOH or an ester or amide thereof, --CH.sub.2 OH or an ether or ester derivative thereof, or --CHO or an acetal derivative thereof, or --COR.sub.1 or a ketal derivative thereof where R.sub.1 is --(CH.sub.2).sub.m CH.sub.3 where m is 0-4; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 21, 1992Date of Patent: September 21, 1993Assignee: Allergan, Inc.Inventor: Roshantha A. S. Chandraratna
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Patent number: 5190961Abstract: Thiourea derivatives represented by the formula (I) ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each represents a lower alkyl group, or R.sub.1 or R.sub.2 taken together represent a group having the formula --(CH.sub.2).sub.m --in which m is 4 or 5, R.sub.3 represents a lower alkyl group or a cycloalkyl group or a group having the formula--(CH.sub.2).sub.l --R.sub.4 in which R.sub.4 is a phenyl, naphthyl, pyridyl, furyl or thienyl group optionally having 1-3 substituents selected from the group consisting of lower alkyl, lower alkoxy, phenoxy, lower alkylthio, hydroxy, halogen, nitro, cyano and trifluoromethyl, and l represents an integer of 0 to 2 and n represents an integer of 1 to 5 or a physiologically acceptable salt thereof.The compounds of the invention are useful as a therapeutic agent for peptic ulcers which is also effective on prevention of the recurrence after discontinuation of the administration due to the antimicrobial activity against Helicobacter pyroli.Type: GrantFiled: August 2, 1991Date of Patent: March 2, 1993Assignee: Terumo Kabushiki KaishaInventors: Hirokazu Hasegawa, Isamu Endo, Shingo Koyama, Masashi Isozaki, Yukari Yoshiyama, Shigenori Nozawa, Norio Arakawa
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Patent number: 5183818Abstract: The present invention provides compounds having the structureY-Het-[Q.sub.1 ]-X-[Q.sub.2 ]-Zwhich inhibit the catalytic action of lipoxygenase enzymes, particularly 5-lipoxygenase, and thereby reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4.In the generic formula given above, X is oxygen or sulfur and Het is a heteroaryl group selected from the group consisting of furyl, thienyl, 2-, 3-, and 4-pyridyl, 2- and 3-benzo[b]furyl, 2- and 3-benzo[b]thienyl and thienothienyl.Y is one or two substituents independently selected from hydrogen, hydroxy, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkoxyaryl), alkylthioaryl, arylalkoxy, arylalkylthio, aryloxy, arylthio, alkylamido, cycloalkyl, alkanoyl, alkoxycarbonyl, amino, alkylamino, dialkylamino, and the following groups wherein R, at each occurrence, is independently selected from hydrogen and alkyl of from one to six carbon atoms: --CRROR, --NRC(O)R, --NRC(O)OR, and --C(O)NRR.The group Q.sub.Type: GrantFiled: August 27, 1991Date of Patent: February 2, 1993Assignee: Abbott LaboratoriesInventors: Dee W. Brooks, Andrew O. Stewart, Jonathan G. Martin
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Patent number: 5166346Abstract: Process for the preparation of thiophene derivatives and also new dihydrothiophene 1-oxides.Thiophene derivatives having an--optionally substituted--amino group on the thiophene ring are prepared by dehydrogenating dihydrothiophenes, substituted in a manner identical to that of the desired thiophene derivatives, by means of H.sub.2 O.sub.2, the dihydrothiophenes being reacted with H.sub.2 O.sub.2 in a first reaction stage in a neutral medium to give the corresponding sulfoxides, which are then rearranged into the thiophene derivatives by means of acid in the second reaction stage.The dihydrothiophene 1-oxides formed as intermediates in this reaction are new compounds. Like the thiophene derivatives formed from them by rearrangement with acid, they are intermediates, mainly in the sector of plant protection agents and pharmaceuticals.Type: GrantFiled: December 20, 1990Date of Patent: November 24, 1992Assignee: Hoechst AktiengesellschaftInventors: Robert Rippel, Hans-Wolfram Flemming, Manfred Rukwied
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Patent number: 5130331Abstract: The novel substituted 3-thienylthioureas, -isothioureas and -carbodiimides of formula I ##STR1## in which R.sub.1 is C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.4 alkyl substituted by a C.sub.3 -C.sub.6 cycloalkyl radical, C.sub.3 -C.sub.8 cycloalkyl, or C.sub.3 -C.sub.6 cycloalkyl substituted by a C.sub.1 -C.sub.4 alkyl radical; R.sub.2, R.sub.3 and R.sub.4 are each, independently of the others, hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl, or phenyl substituted by from 1 to 3 radicals from the group halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.4 alkoxy and C.sub.1 -C.sub.6 haloalkyl having from 1 to 9 halogen atoms; Z is a group --NH--CS--NH--, --N .dbd.C(SR.sub.5)--NH-- or --N.dbd.C.dbd.N--; and R.sub.5 is C.sub.1 -C.sub.6 alkyl or C.sub.3 -C.sub.5 alkenyl; with the proviso that at least one of the radicals R.sub.2, R.sub.3 and R.sub.4 is other than hydrogen; and the salts of compounds of formula I in which Z is the group --N.dbd.C(SR.sub.5 )--NH--, have valuable pesticidal properties.Type: GrantFiled: October 9, 1990Date of Patent: July 14, 1992Assignee: Ciba-Geigy CorporationInventor: Alfons Pascual
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Patent number: 5073184Abstract: Compounds of formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, wherein R.sup.1 and R.sup.2, which are the same or different, are alkyl or fluoroalkyl groups, and Z is either an oxygen or sulphur atom; A is an oxygen or sulphur atom, --NR.sup.3 --, or --CR.sup.4 R.sup.5 --; X, Y and Z.sup.Type: GrantFiled: April 9, 1990Date of Patent: December 17, 1991Assignee: Imperial Chemical Industries PLCInventors: Vivienne M. Anthony, John M. Clough, Paul deFraine, Christopher R. A. Godfrey, Kevin Beautement
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Patent number: 5055471Abstract: This invention relates to derivatives of propanoic acid of the formula ##STR1## Useful as fungicides, insecticides and miticides, to processes for preparing them, to compositions containing them, and to methods of using them to combat fungi, especially fungal infections of plants, and to kill or control insects and mites.Type: GrantFiled: November 15, 1989Date of Patent: October 8, 1991Assignee: Imperial Chemical Industries PLCInventors: Paul J. de Fraine, Anne Martin
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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: 5010104Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formul (I): ##STR1## which strongly antagonize an action of thromboxane A.sub.2 and are expected to have preventive and therapeutic effects on ischemica diseases, cerebro-vascular diseases, etc.Type: GrantFiled: June 29, 1989Date of Patent: April 23, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii
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Patent number: 4983619Abstract: Compounds of the following formula have pharmaceutical properties: ##STR1## in which X is R'(HO)C.dbd.C(CN)--, R.sup.1 (CO)--CH(CN)-- or ##STR2## R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-6 alkyl, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each hydrogen, hydroxy, halogen, nitro, cyano, carboxy, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halo-substituted C.sub.1-4 alkyl, halo-substituted C.sub.1-4 alkoxy, halo-substituted C.sub.1-4 alkylthio, C.sub.2-5 alkoxycarbonyl, optionally substituted phenyl, optionally substituted phenoxy, R'R"N-- where R' and R" are each hydrogen or C.sub.1-4 alkyl or R'"CONH-- where R'" is C.sub.1-4 alkyl, or a group of the formula --CR.sup.7 R.sup.8 R.sup.9 in which R.sup.7, R.sup.8 and R.sup.9 are each C.sub.1-6 alkyl, halo-substituted C.sub.1-6 alkyl or optionally substituted phenyl, or R.sup.7 and R.sup.8, together with the carbon atom to which they are attached, form a cycloalkyl group containing 3 to 7 carbon atoms, or R.sup.7, R.sup.8 and R.sup.Type: GrantFiled: January 11, 1990Date of Patent: January 8, 1991Assignee: Lilly Industries LimitedInventors: Peter T. Gallagher, Terence A. Hicks
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Patent number: 4963548Abstract: Novel fungicidally active compounds of the formula ##STR1## in which R represents alkyl, cyanoalkyl or in each case optionally substituted alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl or phenylalkyl,R.sup.1 represents the --OR.sup.2 or --NR.sup.3 R.sup.4 groups, andR.sup.3 and R.sup.4 have special special definitions.Type: GrantFiled: May 27, 1988Date of Patent: October 16, 1990Assignee: Bayer AktiengesellschaftInventors: Winfried Lunkenheimer, Wilhelm Brandes, Gerd Hanssler
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Patent number: 4959390Abstract: Compounds of the present invention, are represented by the general formula ##STR1## wherein R.sub.1 group which may be alkyl of from 1 to about 6 carbon atoms, alkenyl of from 2 to about 6 carbon atoms, alkynyl of from 2 to about 10 carbon atoms, alkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms, halogen, acetamido, amino, nitro, alkylamino of from 1 to about 6 carbon atoms, hydroxy, hydroxyalkyl of from 1 to about 6 carbon atoms, cyano or arylalkoxy wherein the alkyl group contains from 1 to about 6 carbon atoms R.sub.2, R.sub.3 and R.sub.4 are hydrogen or hydroxyl groups or the combination of either hydrogen or hydroxyl groups; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NHCOR.sub.5, --NHCONR.sub.5 R.sub.6, or --NHCOOR.sub.5 wherein R.sub.5 and R.sub.Type: GrantFiled: December 15, 1988Date of Patent: September 25, 1990Assignee: E. I. du Pont de Nemours and CompanyInventors: Ghanshyam Patil, William L. Matier, Khuong H. X. Mai
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Patent number: 4894464Abstract: Amides of L-aspartyl-D-amino acid dipeptides of the formula ##STR1## and physiologically acceptable cationic and acid addition salts thereof wherein R.sup.a is methyl, ethyl, n-propyl or isopropyl; R is a branched member selected from the group consisting of fenchyl, diisopropylcarbinyl, d-methyl-t-butylcarbinyl, d-ethyl-t-butylcarbinyl, di-t-butylcarbinyl, 2-methylthio-2,4-dimethylpentan-3-yl, ##STR2## where at least one of R.sup.3, R.sup.4, R.sup.5, R.sup.6 is alkyl having from one to four carbon atoms and the remainder are hydrogen or alkyl having from one to four carbon atoms, X is O, S, SO, SO.sub.2 C.dbd.O or CHOH; m is zero or 1-4, n and p are each zero, 1, 2 or 3 where the sum of n+p is not greater than 3 and the sum of the carbon atoms in R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is not greater than six, and when both of R.sup.3 and R.sup.4 or R.sup.5 and R.sup.6 are alkyl they are methyl or ethyl, ##STR3## where one of R.sup.7, R.sup.8, R.sup.Type: GrantFiled: October 26, 1988Date of Patent: January 16, 1990Assignee: Pfizer Inc.Inventors: Thomas M. Brennan, Michael E. Hendrick
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Patent number: 4889865Abstract: Mono, di and tri-esters of 1,8-dihydroxy-10-phenyl-9-anthrone or -9-anthranol have the formula ##STR1## wherein p is 0 or 1,(a) when p=0, t=1 and R.sub.2 represents hydrogen or --COR.sub.3,(b) when p=1, t=0 and R.sub.1 and R.sub.2 each independently represent hydrogen or --COR.sub.3,R.sub.3 represents linear or branched alkyl having 1-17 carbon atoms, cycloalkyl, phenyl or phenyl substituted by lower alkyl, lower alkoxy, halogen, a nitro function, --CF.sub.3 or a hydroxyl function, and mixtures of said esters. These esters are prepared by reacting 1,8-dihydroxy-10-phenyl-9-anthrone with an activated form of an acid. The esters are useful in human or veterinary medicine and in cosmetic compositions.Type: GrantFiled: February 21, 1989Date of Patent: December 26, 1989Assignee: Centre International de Recherches Dermatologiques C.I.R.D.Inventors: Braham Shroot, Gerard Lang, Jean Maignan, Serge Restle, Christopher Hensby, Michel Colin
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Patent number: 4859699Abstract: Substituted N-benzoyl-N'-thienylureas, processes for making these compounds, intermediates therefor and the use of the compounds for the control of pests, and in particular for the control of insects and acarids.Type: GrantFiled: February 23, 1989Date of Patent: August 22, 1989Assignee: Sandoz Ltd.Inventors: Robert L. Carney, Alfred S. T. Lui, Fred Kuhnen, John M. Gruber
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Patent number: 4855086Abstract: The specification describes and claims methods of controlling acarine pests by application of a compound of Formula (I), methods of controlling arthropod pests by application of a compound of Formula (IA), compounds of Formula (IA) per se, pesticidal compositions comprising a compound of Formula (IA), and processes for preparing a compound of Formula (IA).Type: GrantFiled: October 11, 1983Date of Patent: August 8, 1989Assignee: Burroughs Wellcome Co.Inventors: Malcolm H. Black, Robert J. Blade
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Patent number: 4818273Abstract: Novel substituted triazolo[1,5-a]pyrimidine-2-sulfonamides, e.g., 5,7-dimethyl-N-(2,6-dichlorophenyl)-1,2,4-triazolo[1,5-a]pyrimidine-2-sulf onamide and their agriculturally acceptable salts are prepared. These compounds and compositions containing them are useful for the control of unwanted vegetation. Novel substituted triazolo[1,5-a]pyrimidine-2-sulfonyl chlorides and substituted anilines and their use as intermediates are also described.Type: GrantFiled: December 10, 1986Date of Patent: April 4, 1989Assignee: The Dow Chemical CompanyInventors: William A. Kleschick, Robert J. Ehr, Mark J. Costales, Ben C. Gerwick, III, Richard W. Meikle, deceased, William T. Monte, Pearson, Norman R.
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Patent number: 4814465Abstract: Abstract of the Disclosure: Aminothiophene derivatives of the formula I ##STR1## where R is unsubstituted or substituted C.sub.1 -C.sub.8 -alkyoxycarbonyl, unsubstituted or substituted carbamyl or cyano, are prepared by a process in which a compound of the formula IINC--CH.sub.2 --R (II),where R has the above meanings, is reacted in water with a base and simultaneously or subsequently with a haloacetyl halide, and the product is then reacted with hydrogen sulfide or a water-soluble sulfide.Type: GrantFiled: August 13, 1987Date of Patent: March 21, 1989Assignee: Basf AktiengesellschaftInventor: Karl-Heinz Etzbach
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Patent number: 4806656Abstract: The invention provides compounds of formula I ##STR1## wherein R is C.sub.1-4 alkoxy-C.sub.2-4 alkyl of which the C.sub.1-4 alkoxy group is separated by at least 2 C-atoms from the N-atom to which R is bound,each of R.sub.2 and R.sub.4 independently is CH.sub.3 or C.sub.2 H.sub.5 andR.sub.5 is H or CH.sub.3,the preparation of such compounds and the use of such compounds for the preparation of N-(thien-3-yl)-chloroacetamides.Type: GrantFiled: August 5, 1985Date of Patent: February 21, 1989Assignee: Sandoz Ltd.Inventor: Hermann Schneider
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Patent number: 4798892Abstract: The present invention relates to compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1, wherein R.sub.1, R.sub.2 and R.sub.3 may be alike or different and may be hydrogen, alkyl, alkoxyalkyl cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 membered heterocyclic group and the pharmaceutically acceptable salts thereof. The compounds exhibit beta-adrenergic blocking activity and are also useful in the treatment of glaucoma.Type: GrantFiled: April 14, 1986Date of Patent: January 17, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventors: Sheung T. Kam, William L. Matier, Ghanshyam Patil, Khuong H. X. Mai
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Patent number: 4757153Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, lower alkoxy, --O(CH.sub.2).sub.n phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, and R.sup.9 may be the same or different and represent hydrogen, lower alkyl, cycloalkyl having 3 to 8 carbons, unsaturated lower alkyl, or --(CH.sub.2).sub.m cycloalkyl with the cycloalkyl having 3 to 8 carbons and m is 1 to 4; R.sup.10 is hydrogen or --(CH.sub.2).sub.p phenyl or with the phenyl optionally substituted with --NH.sub.2, --OH, halogen, --NO.sub.2, or lower alkyl or --(CH.sub.2).sub.p thienyl wherein p is 1 to 4; one of R.sup.7 or R.Type: GrantFiled: July 14, 1986Date of Patent: July 12, 1988Assignee: G. D. Searle & Co.Inventors: Donald W. Hansen, Jr., Daniel R. Pilipauskas, Michael Clare
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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: 4711954Abstract: Azo dyestuffs which contain at least one water-solubilizing group and have the formula ##STR1## wherein K stands for the radical of a coupling component,R.sub.1 stands for CN, COOX, CONXY or COZ,R.sub.2 stands for hydrogen, halogen, CN, alkyl or aryl,R.sub.3 stands for alkyl or aryl,X stands for H, alkyl, alkenyl, cycloalkyl, aryl or aralkyl andY stands for H or alkyl andZ stands for alkyl or aryl,are highly suitable for dyeing polyamide fibres. The resulting dyeings are distinguished by good all-round fastness properties.Type: GrantFiled: March 4, 1986Date of Patent: December 8, 1987Assignee: Bayer AktiengesellschaftInventors: Holger Heidenreich, Gerhard Wolfrum
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Patent number: 4692461Abstract: Fungicidally active novel thienylurea derivatives of the formula ##STR1## in which X represents oxygen or sulphur,R represents cyano, hydroxycarbonyl or alkoxycarbonyl,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl,R.sup.3 represents hydrogen, alkyl or optionally substituted aryl,R.sup.4 represents hydrogen, alkyl or optionally substituted aryl,R.sup.5 represents hydrogen, alkyl or optionally substituted aryl, orR.sup.4 and R.sup.5 together represent the radical --(CH.sub.2).sub.n --, andn represents the numbers 3, 4, 5 or 6,or acid addition salts thereof.Type: GrantFiled: November 21, 1986Date of Patent: September 8, 1987Assignee: Bayer AktiengesellschaftInventors: Werner Hallenbach, Hans Lindel, Wilhelm Brandes
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Patent number: 4687857Abstract: Novel alkyl .beta.-oxo-benzenepropanoates of the formula ##STR1## wherein X is in the 5-,6-,7- or 8-position and is selected from the group consisting of hydrogen, halogen, alkyl of 1 to 5 carbon atoms, alkoxy of 1 to 4 carbon atoms, CF.sub.3 --, CF.sub.3 S-- and CF.sub.3 O--, R.sub.1 ' is selected from the group consisting of hydrogen and alkyl of 1 to 4 carbon atoms, R.sub.2 ' is selected from the group consisting of hydrogen, thiazolyl, 4,5-dihydrothiazolyl, pyridinyl, oxazolyl, isoxazolyl, imidazolyl, pyrimidyl, tetrazolyl, thienyl, benzothiazolyl and phenyl optionally substituted with at least one member of the group consisting of halogen, alkoxy of 1 to 4 carbon atoms, hydroxy, phenyl, CF.sub.3 --, NO.sub.2 -- alkyl of 1 to 4 carbon atoms and alkyl of 1 to 4 carbon atoms substituted with amino, alkylamino or dialkylamino with alkyls of 1 to 3 carbon atoms or R.sub.1 ' and R.sub.Type: GrantFiled: October 12, 1984Date of Patent: August 18, 1987Assignee: Roussel UclafInventors: Francois Clemence, Odile Le Martret
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Patent number: 4666502Abstract: The invention provides 5-membered heteroaromatic compounds of formula IArN(Y)COCH.sub.2 Cl Iwherein Ar is a 5-membered heteroaromatic group comprising 1 or 2 heteroatoms selected from O, S and N and linked by a ring C-atom to the N-atom of the N(Y)COCH.sub.2 Cl group to which it is bound, whereby where Ar is pyrazolyl, said N(Y)COCH.sub.2 Cl group is in the 4-position,and Y is as specified in the description,the use of these compounds as herbicides, compositions for facilitating such use and the preparation of the chloroacetamides.Type: GrantFiled: February 3, 1983Date of Patent: May 19, 1987Assignee: Sandoz Ltd.Inventors: Karl Seckinger, Fred Kuhnen, Karlheinz Milzner
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Patent number: 4643758Abstract: N-(Substituted heterocyclic)-2-pyrrolidinone derivatives useful as herbicides both alone and in combination with other herbicides.Type: GrantFiled: November 8, 1984Date of Patent: February 17, 1987Assignee: Eli Lilly and CompanyInventors: Kenneth W. Burow, Jr., James C. Williams, Jr.
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Patent number: 4608385Abstract: Use of an N-phenylcarbamate of the formula: ##STR1## as a fungicidal agent against phytopathogenic fungi, particularly their strains resistant to benzimidazole thiophanate fungicides and/or cyclic imide fungicides.Type: GrantFiled: October 22, 1982Date of Patent: August 26, 1986Assignee: Sumitomo Chemical Company, LimitedInventors: Hiroshi Noguchi, Toshiro Kato, Junya Takahashi, Yukio Ishiguri, Shigeo Yamamoto, Katsuzo Kamoshita
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Patent number: 4582923Abstract: Urethanes are made by reacting a primary amine with carbon monoxide and a compound containing at least one hydroxyl group in the presence of an oxidizing agent and a catalyst system. The catalyst system is made up of (i) a noble metal and/or a noble metal compound of a metal of the Eighth Secondary Group of the Periodic System of Elements and (ii) an oxidizing quinoid and/or a compound capable of being converted to an oxidizing quinoid compound under the reaction conditions. The catalyst system may optionally include (iii) metal compounds of elements of the Third to Fifth Main Groups and/or First to Eighth Secondary Groups of the Periodic System of Elements and/or (iv) a tertiary amine. This reaction is generally carried out at a temperature of from 100.degree. to 300.degree. C. and at a pressure of from 5 to 500 bars. The product urethanes are useful in the production of isocyanates and pesticides.Type: GrantFiled: May 17, 1985Date of Patent: April 15, 1986Assignee: Bayer AktiengesellschaftInventors: Gunter Stammann, Robert Becker, Johann Grolig, Helmut Waldmann
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Patent number: 4582855Abstract: Novel compounds of the general formula ##STR1## wherein Ar represents a substituted or unsubstituted aromatic or heterocyclic group; W represents alkylene of from 1 to about 10 carbon atoms; and B represents --NR.sub.2 COR.sub.1, --NR.sub.2 CONR.sub.1 R.sub.3, --NR.sub.2 SO.sub.2 R.sub.1, --NR.sub.2 SO.sub.2 NR.sub.1 R.sub.3, or --NR.sub.2 COOR.sub.1 wherein R.sub.1, R.sub.2 and R.sub.3 may be the same or different and may be hydrogen, alkyl, alkoxyalkyl, cycloalkyl, alkenyl, alkynyl, aryl, heteroaryl, or aralkyl, except that R.sub.1 is not hydrogen when B is --NR.sub.2 SO.sub.2 R.sub.1 or --NR.sub.2 COOR.sub.1, or R.sub.1 and R.sub.3 may together with N form a 5 to 7 momoered heterocyclic group; and the pharmaceutically acceptable salts thereof. These compounds exhibit .beta.-adrenergic blocking activity and are also useful in the treatment of glaucoma.Type: GrantFiled: November 12, 1981Date of Patent: April 15, 1986Assignee: American Hospital Supply CorporationInventors: Sheung T. Kam, William L. Matier
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Patent number: 4565826Abstract: This invention relates to a novel class of heterocyclic amidinourea and heterocyclic amidinothiourea compounds wherein the heterocyclic substitution is at the 1-N urea nitrogen atom. These compounds exhibit pharmaceutical activity and may be incorporated into pharmaceutical preparations for producing anti-ulcerogenic, antisecretory, antispasmodic, antimotility, cardiovascular, antidiarrheal or antiparasitic action.Type: GrantFiled: February 24, 1984Date of Patent: January 21, 1986Assignee: William H. Rorer, Inc.Inventors: William L. Studt, Harry K. Zimmerman, George H. Douglas
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Patent number: 4563527Abstract: Amidine compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof are novel compounds and are useful as powerful anti-trypsin, anti-plasmin, anti-kallikrein and anti-thrombin agents. They are also useful as a powerful anti-complement agent.Type: GrantFiled: July 19, 1984Date of Patent: January 7, 1986Assignee: Torii & Co., Ltd.Inventors: Setsuro Fujii, Toyoo Nakayama, Shigeki Nunomura, Kimio Sudo, Shin-ichi Watanabe, Toshiyuki Okutome, Yojiro Sakurai, Masateru Kurumi, Takuo Aoyama
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Patent number: 4497964Abstract: A process for the production of an N-acyl-.alpha.-amino acid represented by the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4, independently from each other, represent a hydrogen atom, an alkyl or cycloalkyl group which may be substituted, or an aryl or heteroaromatic group selected from the group consisting of furyl, pyrrolyl, pyridinyl, thienyl and indolyl which may be substituted, which comprises reacting an oxirane represented by the general formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, an amide compound represented by the general formulaR.sup.3 CONHR.sup.4 (III)wherein R.sup.3 and R.sup.4 are as defined above, and carbon monoxide in the presence of hydrogen, a cobalt-containing catalyst, and a promoter composed of a compound containing a metal selected from Groups I, II, III and IV of the periodic table.Type: GrantFiled: November 15, 1982Date of Patent: February 5, 1985Assignee: Sagami Chemical Research CenterInventors: Iwao Ojima, Kenji Hirai
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Patent number: 4496542Abstract: Compounds of the formula ##STR1## wherein R and R.sub.9 are independently hydroxy and lower alkoxy,R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, aryl-lower alkyl having from 7 to 12 carbon atoms, or heterocyclic-lower alkyl having from 6 to 12 carbon atoms,R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are hydrogen or lower alkyl,R.sub.6 is heterocyclic and their pharmaceutically acceptable, nontoxic acid addition salts and where R or R.sub.9 or both are hydroxy, their pharmaceutically acceptable, nontoxic basic salts, possess antihypertensive activity.Type: GrantFiled: April 13, 1983Date of Patent: January 29, 1985Assignee: USV Pharmaceutical CorporationInventors: Jerry W. Skiles, Raymond D. Youssefyeh, John T. Suh, Howard Jones
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Patent number: 4472425Abstract: The invention provides novel N-acylamino thiophene derivatives, e.g. N-(methoxyacetyl)-N-(5-bromo-4-methyl-2-methylthiothien-3-yl)alanine methyl ester, which are useful as fungicides. Other objects of the invention are fungicidal compositions comprising such novel compounds and methods of combatting phytopathogenic fungi with the acid of said novel compounds.Type: GrantFiled: September 6, 1983Date of Patent: September 18, 1984Assignee: Sandoz Ltd.Inventors: Rudolf Sandmeier, Karl Seckinger
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Patent number: 4467101Abstract: Acylamido-3-cephem-4-carboxylic acid compounds of the formula ##STR1## in which the index n represents an integer of from 1 to 4,the index m represents 0 or 1,X represents oxygen, sulphur or an --NH-- group,W represents a --CO--, --CO--NHSO.sub.2 -- or --SO.sub.2 NH--CO-- group, orX-W together represent a --CO-- or --CO--NHSO.sub.2 -- group,A represents optionally substituted phenylene, thienylene or furylene,Y represents hydrogen, hydroxyl, formyloxy, amino or sulpho optionally present in salt form, andZ represents hydrogen, orY and Z together represent an oxo group or an .dbd.N--O--R.degree. group in which R.degree. represents hydrogen or optionally substituted lower alkyl,R.sub.1 represents hydrogen, lower alkyl, lower alkoxy, halogen or a group of the formula --CH.sub.2 --R.sub.2 in which R.sub.2 is a free, esterified or etherified hydroxy or mercapto group or a quaternary ammonium group, andR.sub.Type: GrantFiled: September 20, 1982Date of Patent: August 21, 1984Assignee: Ciba-Geigy CorporationInventors: Karoly Kocsis, Peter Schneider, Bruno Fechtig, Riccardo Scartazzini
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Patent number: 4454328Abstract: Amides of L-aspartyl-D-amino acid dipeptides of the formula ##STR1## and physiologically acceptable cationic and acid addition salts thereof wherein R.sup.a is CH.sub.2 OH or CH.sub.2 OCH.sub.3 ; R is a branched member selected from the group consisting of fenchyl, diisopropylcarbinyl, d-methyl-t-butylcarbinyl, d-ethyl-t-butylcarbinyl, di-t-butylcarbinyl, 2-methylthio-2,4-dimethylpentan-3-yl, ##STR2## where at least one of R.sup.3, R.sup.4, R.sup.5, R.sup.6 is alkyl having from one to four carbon atoms and the remainder are hydrogen or alkyl having from one to four carbon atoms, X is O, S, SO, SO.sub.2, C.dbd.O or CHOH; m is zero or 1-4, n and p are each zero, 1, 2 or 3 where the sum of n+p is not greater than 3 and the sum of the carbon atoms in R.sup.3, R.sup.4, R.sup.5 and R.sup.6 is not greater than six, and when both of R.sup.3 and R.sup.4 or R.sup.5 and R.sup.6 are alkyl they are methyl or ethyl, ##STR3## where one of R.sup.7, R.sup.8, R.sup.Type: GrantFiled: April 1, 1983Date of Patent: June 12, 1984Assignee: Pfizer Inc.Inventors: Thomas M. Brennan, Michael E. Hendrick
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Patent number: 4447624Abstract: Process for the preparation of thiophenes having the structure ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 can be various substituents. The compounds can be converted to the corresponding 2-amino compounds from which azo dyes can be prepared.Type: GrantFiled: June 21, 1982Date of Patent: May 8, 1984Assignee: Eastman Kodak CompanyInventors: James J. Krutak, Robert J. Maleski
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Patent number: 4437878Abstract: Dihydrothiophenecarboxylates of the formula ##STR1## where R.sup.1 and R.sup.2 have the meanings given in the description, are used for controlling undesirable plant growth.Type: GrantFiled: March 31, 1983Date of Patent: March 20, 1984Assignee: BASF AktiengesellschaftInventors: Rolf-Dieter Acker, Phillip A. Rossy, Gerhard Hamprecht, Bruno Wuerzer
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Patent number: 4419363Abstract: Novel 1-aryloxy-3-amidoamidoalkylamino-2-propanol derivatives, processes for their manufacture, pharmaceutical compositions containing them and methods of using them in the treatment of heart diseases. Representative of the compounds disclosed is 1-(o-cyanophenoxy)-3-.beta.-(2-thenamidoacetamido)ethylaminopropan-2-ol.Type: GrantFiled: June 4, 1982Date of Patent: December 6, 1983Assignee: Imperial Chemical Industries PLCInventor: Leslie H. Smith
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Patent number: 4412856Abstract: The novel compounds of the formula I are useful selective herbicides for postemergence application in crops of cereals, maize and rice.In formula I, ##STR1## A is an unsubstituted or substituted amino group, Q is a C.sub.2 -C.sub.6 alkylene bridge, Y is an oxygen or sulfur atom or an unsubstituted or substituted nitrogen atom, and Z is an unsubstituted or substituted phenyl, naphthyl or heterocyclic radical, which phenyl radical, containing the bridge member Y, can additionally carry one to four further substituents.Type: GrantFiled: May 22, 1981Date of Patent: November 1, 1983Assignee: Ciba-Geigy CorporationInventors: Hans-Georg Brunner, Rolf Schurter, Henry Szczepanski
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Patent number: 4388469Abstract: Diphenylalkanoether and diphenylalkanone oxime-ether derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an aryl group optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, cyano, di(C.sub.1 -C.sub.4)alkylamino, amino, benzyloxy, hydroxyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkanoylamino, C.sub.1 -C.sub.4 alkylamino and N-(C.sub.1 -C.sub.4)alkyl-N-(C.sub.1 -C.sub.4)alkanoylamino, Z.sup.1 is a group of the formula: ##STR2## (wherein R.sup.3 and R.sup.4 are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or an ar(C.sub.1 -C.sub.Type: GrantFiled: April 2, 1980Date of Patent: June 14, 1983Assignee: Sumitomo Chemical Company, LimitedInventors: Keiichi Ono, Hajime Kawakami, Junki Katsube
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Patent number: 4382143Abstract: This disclosure described novel (monosubstituted-amino)heteroaryl carboxylic acids and analogs which are useful as hypolipidemic and antiatherosclerotic agents.Type: GrantFiled: July 23, 1979Date of Patent: May 3, 1983Assignee: American Cyanamid CompanyInventor: Robert G. Shepherd
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Patent number: 4382031Abstract: A process is disclosed for producing d-biotin from L or DL-cystine ester via novel intermediates.Type: GrantFiled: November 23, 1981Date of Patent: May 3, 1983Assignee: Hoffmann-La Roche Inc.Inventors: Enrico G. Baggiolini, Hsi L. Lee, Milan R. Uskokovic
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Patent number: 4359467Abstract: Prostanoic acid derivatives of the formula ##STR1## wherein R.sub.1 is an acid, ester, amide or hydroxyalkylene group; R.sub.2 and R.sub.3 are H or alkyl; R.sub.4 and R.sub.5 are both CH.sub.3 or one is Cl and the other is CH.sub.3 ; A is CH.sub.2 CH.sub.2 or --CH.dbd.CH; B is CH.sub.2 CH.sub.2, trans- ##STR2## W is free or functionally modified hydroxyalkylene or carbonyl; Z is free or functionally modified hydroxymethylene or carbonyl; X Y is either ##STR3## or, when Z is free or functionally modified hydroxymethylene, ##STR4## or, when Z is free or functionally modified carbonyl, --CH.dbd.CH--, R.sub.12 being H, CH.sub.3, CN or free or functionally modified hydroxy; and physiologically acceptable salts thereof when R.sub.1 is an acid group, possess pharmacological activity, including abortion triggering activity.Type: GrantFiled: April 22, 1981Date of Patent: November 16, 1982Assignee: Schering AktiengesellschaftInventors: Helmut Vorbruggen, Norbert Schwarz, Olaf Loge, Walter Elger
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Patent number: 4349686Abstract: The present invention refers to new 5-(N-Alkyl-N-acyl-amino)-thiophen-2-carboxylic acid derivatives having the general formula I ##STR1##Type: GrantFiled: November 12, 1981Date of Patent: September 14, 1982Assignee: A. Nattermann & Cie GmbHInventors: Hans-Heiner Lautenschlager, Hans Betzing, Johannes Winkelmann, Manfred Probst, Brigitte Stoll
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Patent number: 4335138Abstract: Novel carbamates derived from substituted cyclic .beta.-keto-alcohols, their preparation, and pharmaceutical formulations which contain these compounds and which may be used as hypnotics in the treatment of sleep disturbance and as sedatives.Type: GrantFiled: September 15, 1980Date of Patent: June 15, 1982Assignee: BASF AktiengesellschaftInventors: Walter-Wielant Wiersdorff, Karl-Heinz Geiss, Harald Weifenbach, Wolfgang Worstmann, Dieter Lenke, Rolf Kretzschmar
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Patent number: 4327110Abstract: Symmetrical N-substituted bis-carbamoyloximino disulfide compounds exhibit outstanding nematocidal, miticidal and insecticidal activity, coupled with substantially reduced mammalian toxicity and phytotoxicity as compared to known pesticidal compounds having a comparable spectrum of activity against insect, arachnid and nematode pests.Type: GrantFiled: March 28, 1977Date of Patent: April 27, 1982Assignee: Union Carbide CorporationInventor: Themistocles D. J. D'Silva
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Patent number: 4320056Abstract: A process is disclosed for producing d-biotin from L or DL-cystine ester via novel intermediates.Type: GrantFiled: March 12, 1981Date of Patent: March 16, 1982Assignee: Hoffmann-La Roche Inc.Inventors: Enrico G. Baggiolini, Hsi L. Lee, Milan R. Uskokovic