Nitrogen Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 514/426)
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Patent number: 5286743Abstract: There are provided N-aminoalkylcarbonyloxyalkylpyrrole compounds of formula I ##STR1## and their use for the control of insects, acarina and mollusks. Further provided are compositions and methods comprising those compounds for the protection of plants from attack by insects, acarina and mollusks.Type: GrantFiled: October 27, 1992Date of Patent: February 15, 1994Assignee: American Cyanamid CompanyInventors: David G. Kuhn, Stephen F. Donovan, Joseph A. Furch
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Patent number: 5286741Abstract: There are provided N-oxy- and thioalkylcarbonyloxyalkylpyrrole compounds of formula I and their use for the control of insects, acarina and mollusks. Further provided are compositions and methods comprising those compounds for the protection of plants from attack by insects, acarina and mollusks.Type: GrantFiled: October 27, 1992Date of Patent: February 15, 1994Assignee: American Cyanamid CompanyInventors: David G. Kuhn, Stephen F. Donovan, Joseph A. Furch
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Patent number: 5284863Abstract: Haloalkylthio, -sulfinyl and -sulfonyl arylpyrrole compounds which are effective for the phytopathogenic fungi are described. A method for the fungicidal use of said compounds and methods for the preparation of said compounds are presented.Type: GrantFiled: December 4, 1991Date of Patent: February 8, 1994Assignee: American Cyanamid CompanyInventors: Keith D. Barnes, Victor M. Kamhi, Robert E. Diehl
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Patent number: 5280021Abstract: There is provided a method for the prevention and control of fungus infestation of a plant which comprises contacting the fungus or plant, or the soil or water in which the plant is growing, with a 1-(substituted)thioalkylpyrrole compound of formula I ##STR1##Type: GrantFiled: December 4, 1991Date of Patent: January 18, 1994Assignee: American Cyanamid CompanyInventors: David G. Kuhn, Venkataraman Kameswaran
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Patent number: 5264453Abstract: This invention relates to pyrrolidine derivatives and pharmaceutically acceptable salts thereof of the structure ##STR1## where R.sup.1, R.sup.2, and R.sup.3 are as defined herein. These compounds are for pharmaceutical use in treating thrombotic diseases, asthma or nephritis.Type: GrantFiled: February 28, 1992Date of Patent: November 23, 1993Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Akihiko Sawada, Hirokazu Tanaka, Masashi Hashimoto
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Patent number: 5254559Abstract: There are provided 1-(substituted)thioalkylpyrrole compounds of formula I ##STR1## the use thereof for the control of insect, acarid and mollusk pests and methods and compositions for the protection of crops from the ravages of said pests.Type: GrantFiled: December 4, 1991Date of Patent: October 19, 1993Assignee: American Cyanamid CompanyInventors: David G. Kuhn, Venkataraman Kameswaran
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Patent number: 5223530Abstract: Novel arylcycloalkanepolyalkylamines useful as anti-psychotic, anti-ischemia, anti-stroke, anti-dementia and anti-convulsant agents. These arylcycloalkanepolyalkylamines are selective high-affinity ligands to the sigma binding-sites containing three basic units: arylcycloalkyl group, an amine group and an intermediate chain. Their preparation and use for treatment of psychoses, ischemia, stroke, dementia and convulsions are also disclosed.Type: GrantFiled: September 12, 1991Date of Patent: June 29, 1993Assignee: SRI, InternationalInventor: Daniel W. Parish
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Patent number: 5214063Abstract: A compound of formula (I): ##STR1## in which R, R.sub.1 and R.sub.2 are as defined in the description. Medicinal product, which is useful in treating disorders related to a dysfunction of GABA.sub.B receptors.Type: GrantFiled: July 28, 1992Date of Patent: May 25, 1993Assignee: Adir et CompagnieInventors: Michel Debaert, Pascal Berthelot, Claude Vaccher
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Patent number: 5204332Abstract: There are provided certain insecticidal, acaricidal and molluscicidal pyrrole carbonitrile and nitropyrrole compounds and a method for controlling insects, acarids and mollusks therewith. The invention also provides a method for protecting growing plants from insect, acarid and mollusk attack by applying to said plants or the soil or water in which they are growing, an insecticidally, acaricidally or molluscicidally effective amount of a pyrrole carbonitrile or nitropyrrole compound. The present invention further relates to methods for the preparation of said pyrrole carbonitrile and nitropyrrole compounds.Type: GrantFiled: November 20, 1991Date of Patent: April 20, 1993Assignee: American Cyanamid CompanyInventors: Dale G. Brown, Robert E. Diehl, Gregory T. Lowen, Donald P. Wright, Jr., Christine F. Kukel, Rod A. Herman, Roger W. Addor
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Patent number: 5198433Abstract: Applicants have discovered that certain previously known lactamimide derivatives possess, as a class, valuable calcium channel blocking activity. By virtue of this calcium antagonism activity the compounds are antihypertensives and will have other activities associated with calcium antagonists.Type: GrantFiled: July 21, 1992Date of Patent: March 30, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Michael G. Palfreyman, Norbert L. Wiech, Hsien C. Cheng, John M. Kane
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Patent number: 5187185Abstract: Substituted-1-arylpyrrole compounds of general formula (I) below, are useful as pesticides, in particular for the control of insects, arachnids, and nematodes. Processes to make the compounds and intermediates used for their preparation are described. Additionally, compositions containing the compounds and methods of use therefore are provided. Preferred compounds are the compounds of general formula (I) ##STR1## wherein typically preferred substituents are: X is halogen or a group R.sup.5 S(O).sub.n, in which n is 0, 1, or 2 and R.sup.5 is CH.sub.3, CF.sub.3, CCl.sub.3, CF.sub.2 Cl, CFCl.sub.2, CF.sub.2 Br, CHF.sub.2, CHCl.sub.2 or CHClF;R.sup.1 is H, F, Cl, Br, OCH.sub.3, SCH.sub.3, or CH.sub.3 optionally substituted;R.sup.2 is CN;R.sup.3 is H, F, Cl, Br, OCH.sub.3, or CH.sub.3 optionally substituted;Y is CF.sub.3, CF.sub.3 O, H, F, Cl or Br;X.sup.1 and X.sup.4 are individually H, F, Cl, Br, CH.sub.3, OCH.sub.3 or SCH.sub.3 ; andX.sup.2 and X.sup.3 are each H.Type: GrantFiled: June 5, 1990Date of Patent: February 16, 1993Assignee: Rhone-Poulenc AG CompanyInventors: Russell J. Outcalt, Philip R. Timmons, Susan M. Cramp, Patricia L. Kwiatkowski, Anibal Lopes, Paul A. Cain, David N. Sinodis, Lee S. Hall, Jean-Pierre A. Vors
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Patent number: 5180734Abstract: This invention relates to new diarylpyrrolecarbonitrile and new diarylnitropyrrole compounds. It also relates to the use of said compounds as insecticidal and acaricidal agents and to a method of protecting plants, particularly crop plants, from attack by insects and acarina by application of a new diarylpyrrolecarbonitrile or diarylnitropyrrole to said plants or to the locus in which they are growing.Type: GrantFiled: November 30, 1990Date of Patent: January 19, 1993Assignee: American Cyanamid CompanyInventors: David G. Kuhn, Joseph A. Furch, Victor M. Kamhi
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Patent number: 5162308Abstract: There are provided certain insecticidal, acaricidal and molluscicidal pyrrole carbonitrile and nitropyrrole compounds and a method for controlling insects, acarids and mollusks therewith. The invention also provides a method for protecting growing plants from insect, acarid and mollusk attack by applying to said plants or the soil or water in which they are growing, an insecticidally, acaricidally or molluscicidally effective amount of a pyrrole carbonitrile or nitropyrrole compound. The present invention further relates to methods for the preparation of said pyrrole carbonitrile and nitropyrrole compounds.Type: GrantFiled: October 15, 1991Date of Patent: November 10, 1992Assignee: American Cyanamid CompanyInventors: Dale G. Brown, Robert E. Diehl, Gregory T. Lowen, Donald P. Wright, Jr., Christine F. Kukel, Rod A. Herman, Roger W. Addor
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Patent number: 5158945Abstract: Applicants have discovered that certain previously known lactamimide derivatives possess, as a class, valuable calcium channel blocking activity. By virtue of this calcium antagonism activity the compounds are antihypertensives and will have other activities associated with calcium antagonists.Type: GrantFiled: March 11, 1992Date of Patent: October 27, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Michael G. Palfreyman, Hsien C. Cheng, Norbert L. Wiech, John M. Kane
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Patent number: 5143935Abstract: A benzamide derivative represented by the formula: ##STR1## having a promoting activity of gastrointestinal tract and pharmacentical composition containing the same.Type: GrantFiled: October 16, 1991Date of Patent: September 1, 1992Assignee: Teikoku Chemical Industry Co., Ltd.Inventors: Hiromichi Fujiwara, Akihiko Ogawa, Hideyo Sakiyama, Toshiaki Tamura
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Patent number: 5132307Abstract: New tetralin derivatives of the formula I ##STR1## wherein R.sup.1 to R.sup.8 and Z have the meanings indicated herein and salts thereof, exhibit an effect on the cardiovascular system.Type: GrantFiled: November 7, 1989Date of Patent: July 21, 1992Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Manfred Baumgarth, Rolf Gericke, Rolf Bergmann, Jacques De Peyer, Ingeborg Lues
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Patent number: 5130328Abstract: This invention relates to N-alkanoylaminomethyl and N-aroylaminomethyl pyrrole compounds. It also relates to the use of said compounds as insecticidal and acaricidal agents and to a method of protecting plants from attack by insects and acarina by application of an N-alkanoylaminomethyl or N-aroylaminomethyl pyrrole to said plants or to the locus in which they are growing.Type: GrantFiled: September 6, 1991Date of Patent: July 14, 1992Assignee: American Cyanamid CompanyInventor: Venkataraman Kameswaran
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Patent number: 5128337Abstract: Applicants have discovered that certain previously known lactamimide derivatives possess, as a class, valuable calcium channel blocking activity. By virtue of this calcium antagonism activity the compounds are antihypertensives and will have other activities associated with calcium antagonists.Type: GrantFiled: September 23, 1991Date of Patent: July 7, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Michael G. Palfreyman, Norbert L. Wiech, Hsien C. Cheng, John M. Kane
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Patent number: 5120718Abstract: Compounds which inhibit Candida acid protease are disclosed which have the formula: ##STR1## wherein R.sub.1 is loweralkyl, loweralkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, arylalkyl or (heterocyclic)alkyl;R.sub.2 is loweralkyl, cycloalkylalkyl or arylalkyl;R.sub.3 is --OH or --NH.sub.2 ;R.sub.4 is(a) --CH(OH)--R.sub.5 wherein R.sub.5 is loweralkyl, cycloalkyl or cycloalkylalkyl or(b) --CH.sub.2 CH(R.sub.6)C(O)NHR.sub.7 wherein R.sub.6 is loweralkyl and R.sub.7 is loweralkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxyalkyl, alkoxyalkyl, thioalkoxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, cyanoalkyl or (heterocyclic)alkyl; andA is ##STR2## wherein R.sub.8 is arylalkyl, B is --C(O) or --S(O).sub.2 -- and R.sub.9 is aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl; or ##STR3## wherein R.sub.10 is arylalkyl and R.sub.11 is (a) --C(O)R.sub.12 wherein R.sub.12 is alkoxy, arylalkoxy, aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl or (b) --S(O).sub.2 --R.sub.Type: GrantFiled: June 13, 1991Date of Patent: June 9, 1992Assignee: Abbott LaboratoriesInventors: Robert C. Goldman, William R. Baker, Hwan-Soo Jae, Biswanath De, Thomas M. Zydowsky, Edwin de Lara
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Patent number: 5112868Abstract: The present invention is novel selected hydroxamic acid derivatives of acyl residues of selected NSAIDS, i.e. having 5-lipoxygenase and cyclooxygenase inhibiting properties, pharmaceutical compositions for treating conditions advantageously affected by the inhibition and methods for treating these conditions in mammals, including humans suffering therefor.Type: GrantFiled: May 2, 1990Date of Patent: May 12, 1992Assignee: Warner-Lambert CompanyInventors: Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Jagadish C. Sircar
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Patent number: 5098916Abstract: Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, henalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.16 and R.sup.Type: GrantFiled: March 29, 1990Date of Patent: March 24, 1992Assignee: G. D. Searle & Co.Inventors: Nancy M. Gray, Brian K. Cheng
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Patent number: 5082837Abstract: Applicants have discovered that certain previously known lactamimide derivatives possess, as a class, valuable calcium channel blocking activity. By virtue of this calcium antagonism activity the compounds are antihypertensives and will have other activites associated with calcium antagonists.Type: GrantFiled: November 29, 1990Date of Patent: January 21, 1992Assignee: Merrell Dow PharmaceuticalsInventors: Michael G. Palfreyman, Norbert L. Wiech, Hsien C. Cheng, John M. Kane
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Patent number: 5075337Abstract: Deuterated 2-alkylaminoacetamide compounds are described having the alpha carbon of the alkyl side chain of the compounds substituted by one or two deuterium atoms. These compounds have pharmacokinetic properties which enable treatment of CNS diseases with lower toxic effects. These compounds are also useful in evaluating the metabolic fate of non-deuterated counterpart compounds. Of particular interest are compounds of Formula I: ##STR1## wherein X is deutero or hydrido; wherein R.sup.1 is selected from alkyl and aralkenyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and alkyl; wherein each of R.sup.1, R.sup.2 and R.sup.3 having a substitutable position may be substituted with one or more halo radicals; or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: July 26, 1989Date of Patent: December 24, 1991Assignee: G. D. Searle & Co.Inventors: Alex A. Cordi, Philippe Janssens de Varebeke, Hugo Gorissen
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Patent number: 5070087Abstract: A method of treating cardiac dysfunction, the effects of histamine, and gastric secretion excesses with aryl(alkyl and alkylene)-N-[(phenoxy and phenythio)alkyl]aminoheterocyclics corresponding to the formula: ##STR1## wherein Ar is phenyl or substituted phenyl; R is phenyl, substituted phenyl, pyridinyl or cycloalkyl; A is hydrogen, hydroxy, cyano, amido and amino; Q is --CH.sub.2 --, --CH--, or --CHOH--; d and n are zero or one and the dotted lines form double bonds consistent with the valence of carbon; p is zero, one or two; m is one to six inclusive; B is oxygen, nitrogen, sulfur, sulfinyl or sulfonyl; z is zero or one; l is zero or one; W is hydrogen, loweralkyl, halo, nitro, loweralkoxy or hydroxy; X is hydrogen, loweralkyl, halogen, loweralkoxy or hydroxy; Y is --CH(OH)CH.sub.2 OH, --CH(OH)C(O)OH, --C(O)C(O)OH, --C(O)CH.sub.2 OH,--C(O)C(O)OCH.sub.3, --C(O)C(O)OC.sub.2 H.sub.5, --CH.sub.2 C(O)OC.sub.2 H.sub.5, --CH(OH)C(O)OCH.sub.3, --CH(OH)C(O)OC.sub.2 H.sub.5 or --C(O)CH.sub.2 OC(O)CH.sub.Type: GrantFiled: May 8, 1989Date of Patent: December 3, 1991Assignee: A. H. Robins Company, IncorporatedInventors: Lina C. Teng, David A. Walsh, James R. Shanklin, Jr.
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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: 5021237Abstract: A gel insecticide bait to be contained in a pressurized container, for dispensing a bead of gel bait in cracks, crevices and the like for destroying insects, in particular cockroaches, said composition comprising an oil-in-water emulsion of a pentadienone toxicant-fatty acid mixture in a corn syrup solution, together with a gellant.Type: GrantFiled: November 27, 1989Date of Patent: June 4, 1991Assignee: The Clorox CompanyInventor: Francis J. Bruey
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Patent number: 5010098Abstract: This invention is directed to certain novel insecticidal, acaricidal and nematicidal arylpyrrole agents and a method for controlling insects, acarids and nematodes therewith. The invention also is directed to a method for protecting growing plants from insect, acarid and nematode attack by applying to said plants or the soil in which they are growing, an insecticidally, acaricidally or nematicidally effective amount of a novel arylpyrrole compound. The present invention further is directed to a method for the preparation of the arylpyrrole compounds.Type: GrantFiled: June 23, 1988Date of Patent: April 23, 1991Assignee: American Cyanamid CompanyInventors: Dale G. Brown, Jack K. Siddens, Robert E. Diehl, Donald P. Wright, Jr.
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Patent number: 5010087Abstract: Novel tricyclic compounds having a TXA.sub.2 -antagonizing activity represented by formula (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: July 18, 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: 5010072Abstract: Applicants have discovered that certain previously known lactamimide derivatives possess, as a class, valuable calcium channel blocking activity. By virtue of this calcium antagonism activity the compounds are antihypertensives and will have other activities associated with calcium antagonists.Type: GrantFiled: June 28, 1988Date of Patent: April 23, 1991Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Michael G. Palfreyman, Norbert L. Wiech, Hsien C. Cheng, John M. Kane
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Patent number: 5001148Abstract: Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.Type: GrantFiled: June 7, 1989Date of Patent: March 19, 1991Assignee: E. R. Squibb & Sons, Inc.Inventors: Jeffrey O. Saunders, Eric M. Gordon
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Patent number: 4988711Abstract: Inhibiting HMG-CoA reductase, as in treating hyperlipopproteinaemia, lipoproteinaemia and arteriosclerosis, with the new N-substituted N-amino-pyrroles of the formula ##STR1## in which R.sup.1 is an organic radical,R.sup.2 is an aryl or heteroaryl radical,R.sup.3 is a hydrogen or an organic radical,R.sup.4 and R.sup.5 each independently is hydrogen or an organic radical or, together, they complete a heterocylic ring,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.10 is hydrogen or alkyl, and R.sup.11 is hydrogen, an organic radical or a cation.Type: GrantFiled: April 12, 1989Date of Patent: January 29, 1991Assignee: Bayer AktiengesellschaftInventors: Rolf Angerbauer, Walter Hubsch, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
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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: 4966901Abstract: Pyrrole derivatives of the general formula I ##STR1## wherein R denotes alkyl which is substituted by --NH.sub.2 or acylamino, R.sup.1 and R.sup.2 independently of one another denote hydrogen or alkyl having 1 to 4 carbon atoms, R.sup.3 denotes hydrogen, alkyl having 1 to 4 carbon atoms or a carboxylic acid grouping, R.sup.Type: GrantFiled: May 23, 1989Date of Patent: October 30, 1990Assignee: Cassella AktiengesellschaftInventors: Gerhard Zoller, Rudi Beyerle, Ursula Schindler
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Patent number: 4929634Abstract: This invention relates to methods of controlling mollusks with arylpyrrole compounds and to bait compositions containing a molluscicidally effective amount of an arylpyrrole compound.Type: GrantFiled: July 11, 1988Date of Patent: May 29, 1990Assignee: American Cyanamid CompanyInventors: Rod A. Herman, Christine F. Kukel
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Patent number: 4925652Abstract: Diagnostic media suitable for NMR diagnoses contain compounds of Formula I ##STR1## wherein is a single bond or a double bond,X is the grouping --(CH.sub.2).sub.n -- or , if is a single bond, also the grouping --NHCO(CH.sub.2).sub.n -- wherein n means 0 to 4,m means the numbers 0, 1, or 2,R.sub.1 is an alkyl residue substituted by hydroxy groups, acyloxy groups and/or alkylidenedioxy groups,R.sub.2 has the same meanings as R.sub.1 or is a hydrogen atom or an alkyl residue,R.sub.3 and R.sub.4 are alkyl residues, andR.sub.5 and R.sub.6 are alkyl residues optionally substituted by hydroxy groups.Type: GrantFiled: August 3, 1984Date of Patent: May 15, 1990Assignee: Schering AktiengesellschaftInventors: Heinz Gries, Ulrich Niedballa, Hanns-Joachim Weinmann
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Patent number: 4921939Abstract: Substituted guanidines and ethanamidines are provided as high potency sweetening agents.Type: GrantFiled: March 3, 1987Date of Patent: May 1, 1990Assignee: Universite Claude Bernard -Lyon 1Inventors: Claude Nofre, Jean M. Tinti, Farroudja Ouar Chatzopoulos
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Patent number: 4917826Abstract: Provided are cyclic hydrocarbons of Formula I ##STR1## with an aminoalkyl sidechain that are useful for treating phospholipase A2 mediated conditions, diabetes, and obesity.Type: GrantFiled: June 16, 1987Date of Patent: April 17, 1990Assignee: The Upjohn CompanyInventors: Roy A. Johnson, Gordon L. Bundy, Gilbert A. Youngdale, Douglas R. Morton, Donald P. Wallach, deceased
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Patent number: 4916152Abstract: The invention relates to novel compounds of the formula: ##STR1## wherein R.sup.1 is hydrogen, lower alkoxycarbonyl, phenylsulfonyl, phenylsulfonyl substituted with 1 to 3 substituent(s) selected from the group consisting of halogen, nitro, lower alkoxy, mono (or di or tri)halo(lower)alkyl and lower alkyl, phenylcarbamoyl, lower alkylsulfonyl, benzoyl or thienylsulfonyl;R.sup.2 is phenylsulfonyl or phenylsulfonyl substituted with 1 to 3 substituent(s) selected from the group consisting of halogen, lower alkyl, lower alkoxy and mono(or di or tri)halo(lower)alkyl,R.sup.3 is carboxy(lower)alkyl, lower alkyl substituted with carboxy and 1 to 3 halogen atom(s), esterified carboxy(lower)alkyl, carbamoyl(lower)alkyl, lower alkylsulfonylcarbamoyl(lower)alkyl, phenylsulfonylcarbamoyl(lower)alkyl, carboxyphenyl, esterified carboxyphenyl, carboxy, esterified carboxy, hydroxy(lower)alkyl, sulfino(lower)alkyl, phosphono(lower)alkyl, di(lower)alkoxyphosphoryl(lower)alkyl or halo(lower)alkyl,R.sup.Type: GrantFiled: April 28, 1988Date of Patent: April 10, 1990Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Hiroyuki Setoi, Hideo Hirai, Hiroshi Marusawa, Akio Kuroda, Hirokazu Tanaka, Masashi Hashimoto
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Patent number: 4904679Abstract: Pyrrolophenylalkanolamines of the formula ##STR1## R.sup.1 and R.sup.2 represent hydrogen or various radicals, R.sup.3 represents hydrogen, acyl or trialkylsilyl,R.sup.4 represents hydrogen or alkyl,R.sup.5 represents hydrogen, or, together with R.sup.3, represents ##STR2## wherein R.sup.7 represents hydrogen or alkyl, andR.sup.6 represents branched or cyfclic alkyl, which is optionally substituted,and salts thereof promote the yield of animals. Many new intermediates are also shown.Type: GrantFiled: April 22, 1988Date of Patent: February 27, 1990Assignee: Bayer AktiengesellschaftInventors: Hartmund Wollweber, Jurgen Stoltefuss, Friedrich Berschauer, Ann de Jong, Martin Scheer
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Patent number: 4897397Abstract: Certain aryl-alkynoic, alkenoic and alkanoic acids and derivatives and their use in treating inflammation, allergy and hyperproliferative skin disease are disclosed.Type: GrantFiled: December 16, 1988Date of Patent: January 30, 1990Assignee: Schering CorporationInventors: Neng Y. Shih, David J. Blythin
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Patent number: 4892871Abstract: The invention is directed to azido-substituted octopamine agonists and the radiolabeled derivatives thereof. The invention also relates to past controlling compositions comprising the azido-substituted octopamine agonists of the invention.The invention also relates to methods of controlling invertebrate pests by bringing the pest into contact with an invertebrate pest-controlling composition of the invention and to an apparatus for controlling invertebrate pests utilizing the pest-controlling compositions of the invention. The pest-controlling compositions may be used alone or in conjunction with ultraviolet light.The invention also relates to methods for the isolation of octopamine receptor proteins utilizing the radiolabeled azido-substituted octopamine agonists of the invention.Type: GrantFiled: April 12, 1988Date of Patent: January 9, 1990Assignee: The General Hospital CorporationInventor: James A. Nathanson
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Patent number: 4877895Abstract: Sweetening agents, characterized in that they conform to the following formula: ##STR1## wherein: A is an imino (.dbd.N--), iminium (.dbd.N.sup.+ <), methylene (.dbd.C<) group, the iminium group being able to be salified by a physiologically acceptable anion;m and n are number equal to 1 or 2;B:when n=1, represents H, CN, OCH.sub.3, NO.sub.2, SO.sub.2 R, SOR, SO.sub.2 NHR, SO.sub.2 NR.sub.2, wherein R is an alkyl, cycloalkyl or aryl group having up to 10 carbon atoms;when n=2, represents H, CN, OCH.sub.3 ;X:represents CN, NO.sub.2, when B is H, CN, OCH.sub.3 ;represents CN, NO.sub.2, COCH.sub.3, CHO, Cl, CF.sub.3, F, H, when B is NO.sub.2, SO.sub.2 R, SOR, SO.sub.2 NHR, SO.sub.2 NR.sub.2 ;M is a hydrogen atom or a physiologically acceptable organic or inorganic cation.Type: GrantFiled: March 4, 1986Date of Patent: October 31, 1989Assignee: Universite Claude Bernard - Lyon 1Inventors: Claude Nofre, Jean M. Tinti, Farroudja O. Chatzopoulos
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Patent number: 4783457Abstract: The invention relates to an invertebrate pest controlling composition comprising an invertebrate pest-controlling amount of a non-formamidine octopamine against having substantial activity toward an octopamine receptor present in an invertebrate pest and a pesticidally inert carrier.Type: GrantFiled: March 17, 1987Date of Patent: November 8, 1988Assignee: The General Hospital CorporationInventor: James A. Nathanson
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Patent number: 4737513Abstract: Novel pyrrole derivatives of the formula ##STR1## wherein one of R.sub.2 and R.sub.3 is ##STR2## and the other of R.sub.2 and R.sub.3 as well as R.sub.4 and R.sub.5 are individually selected from the group consisting of hydrogen, halogen, alkyl of 1 to 18 carbon atoms, aryl of 6 to 14 carbon atoms, aralkyl of 7 to 18 carbon atoms, --CN, --CF.sub.3, --NO.sub.2, --COOAlk and Alk is alkyl of 1 to 8 carbon atoms, alkoxy of 1 to 8 carbon atoms, ##STR3## n is 0, 1 or 2, R', R.sub.1 ' and R.sub.2 ' are alkyl of 1 to 8 carbon atoms and R.sub.4 and R.sub.5 taken together with the carbon atoms to which they are attached may form an optionally further unsaturated carbon homocycle of up to 8 carbon atoms, Z is selected from the group consisting of hydrogen, --CN, --C.tbd.CH, --CF.sub.3 and alkyl of 1 to 3 carbon atoms, A is the residue of a pyrethrinoid acid, R.sub.Type: GrantFiled: August 13, 1985Date of Patent: April 12, 1988Assignee: Roussel UclafInventors: Jean Tessier, Jean-Pierre Demoute, Laurent Taliani
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Patent number: 4725602Abstract: Acetylenes of the following formula (I): ##STR1## wherein Y, m, R.sup.1, R.sup.2, R.sup.3, n and R.sup.4 are defined herein and R.sup.5 is hydrogen, alkyl, cycloalkyl or substituted alkyl are useful vasodilators and antihypertensives.Type: GrantFiled: October 24, 1985Date of Patent: February 16, 1988Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4701457Abstract: Amidinoureas are disclosed as useful for the treatment of irritable bowel syndrome.Type: GrantFiled: January 13, 1984Date of Patent: October 20, 1987Assignee: Rorer Pharmaceutical CorporationInventors: John Yelnosky, Ghulam N. Mir
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Patent number: 4699918Abstract: This invention relates to therapeutically useful compounds, particularly in the cardiovascular field, having the formula: ##STR1##Type: GrantFiled: September 17, 1985Date of Patent: October 13, 1987Assignee: Laboratoires Jacques LogeaisInventors: Jacques G. Maillard, Tri V. Van, Jacky M. Legeai, Marguerite M. Benharkate
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Patent number: 4663334Abstract: Heterocyclic acetylenes of the formula (I): ##STR1## wherein Y is alkyl, alkoxy, alkoxyalkyl, chloro, fluoro, bromo or carboxamidoalkyl and R.sup.1 is hydrogen, alkyl, alkoxy, alkylthio, alkoxycarbonyl, chloro, fluoro or dialkylamino, m is 0-2, R.sup.2 is branched alkyl and Het is an aromatic heterocycle. The acetylenes are useful in treating hypertension and/or angina.Type: GrantFiled: December 11, 1985Date of Patent: May 5, 1987Assignee: McNeilab, Inc.Inventor: John R. Carson
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Patent number: 4629739Abstract: Novel substituted sulfonamidobenzamides are described as useful antiarrhythmic agents. Their use in the treatment of cardiac arrhythmias, especially re-entrant arrhythmias, via the prolongation of the action potential of cardiac tissue is provided. Pharmaceutical formulations containing such compounds are also disclosed.Type: GrantFiled: September 23, 1985Date of Patent: December 16, 1986Assignee: Schering A.G.Inventors: David D. Davey, William C. Lumma, Jr., Ronald A. Wohl
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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