Double Bonded Divalent Chalcogen Containing Patents (Class 544/54)
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Patent number: 5095111Abstract: A bifunctional ligand to compositions produced by reaction of those ligand with compounds containing an amino, thiolate or alcholate group, especially proteins, to chelates produced by complexing ligand with metals such as technetium and rhenium and to diagnostic and therapeutic uses of said complexes.Type: GrantFiled: March 17, 1989Date of Patent: March 10, 1992Assignee: The John Hopkins UniversityInventors: Susan Z. Lever, Kwamena E. Baidoo, Alfred V. Kramer, Hugh D. Burns
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Patent number: 5084459Abstract: There is provided a pest control composition containing a compound represented by the formula, ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and independently mean a hydrogen atom, a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted and X means an electron attracting group or a salt thereof.The compounds are of minimal toxicity to man, domestic animals and fish and selectively display remarkable control effect on pests.Type: GrantFiled: October 25, 1989Date of Patent: January 28, 1992Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideki Uneme, Isao Minamida, Tetsuo Okauchi, Noriko Higuchi
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Patent number: 5075293Abstract: O,S-Dialkyl ((nitrogen heterocyclyl)carbonyl)-phosphoramidothioates are prepared by the reaction of O,S-dialkyl phosphoroisocyanatidothioates with selected 5 and 6 membered nitrogen heterocycles, such as thiomorpholine and tetrahydroquinoline, and found to be effective plant systemic and contact insecticides. O,S-dimethyl ((4-thiomorpholinyl)carbonyl)phosphoramidothioate, for example, is prepared from O,S-dimethyl phosphoroisocyanatidothioate and thiomorpholine and found to control aster leafhopper when applied to rice plants.Type: GrantFiled: October 10, 1989Date of Patent: December 24, 1991Assignee: The Dow Chemical CompanyInventors: Walter Reifschneider, Barat Bisabri-Ershadi, James E. Dripps, J. Brian Barron
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Patent number: 5075315Abstract: Novel hexahydro-2H-indeno[1,2-c]pyridines and their pharmaceutically acceptable acid addition salts having useful antipsychotic properties.Type: GrantFiled: May 17, 1990Date of Patent: December 24, 1991Assignee: McNeilab, Inc.Inventor: Chris R. Rasmussen
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Patent number: 5071871Abstract: New benz[b]pyranes and pyranopyridines of formula I, ##STR1## wherein the significances of substituents V, T, W, R.sub.3 to R.sub.5, R.sub.9, R.sub.10, m, X, Y and Z are given in claim 1 and their N-oxides and their salts and their use in the treatment of raised blood pressure in the treatment of vascular disorders and other disorders in which a reduction in tension of the smooth muscles is therapeutically useful, as well as in the treatment of hair loss and baldness. Further the compounds are useful in the treatment of asthma and obstructive disorders of the respiratory system as well as in the prophylactic treatment of obstructive or inflammatory airways disease, for example asthma, as well as novel pharmaceutical compositions comprising said K.sup.+ channel activators suitable for such use.Type: GrantFiled: July 10, 1990Date of Patent: December 10, 1991Assignee: Sandoz Ltd.Inventors: Stefan Blarer, John Morley, Ian D. Chapman
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Patent number: 5072042Abstract: Phenylhydrazones of formula I ##STR1## in which R.sup.1 to R.sup.6 and m and n have the meanings stated above, and the manufacture thereof. The substances are suitable for combating disease and for cosmetic use.Type: GrantFiled: February 8, 1990Date of Patent: December 10, 1991Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest, William V. Murray, Michael P. Wachter, Stanley Bell
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Patent number: 5055579Abstract: Compounds of general formula I are disclosed ##STR1## wherein L denotes a hydrogen atom, an aryl radial or a substituent of the formula ##STR2## M denotes an alkylene radical or alkenylene radical or a 1,2-arylene radical,Q denotes a sulfur, selenium or oxygen atom, a dialkylmethylene group, an alken 1,2-ylene radical, a 1,2-phenylene radical or an N-R.sup.1 group,denotes an alkyl, aralkyl, aryloxyalkyl or alkoxyalkyl radical,R.sup.2 and R.sup.3 denote a hydrogen atom or a 4,6-bis-trichloromethyl-s-triazin-2-yl group, andn is 0 or 1.The compounds are suitable for use as photoinitiators in photosensitive systems that are induced to reaction by free radicals or acid cations. The compounds are characterized by high sensitivity in the visible spectral region.Type: GrantFiled: March 1, 1989Date of Patent: October 8, 1991Assignee: Hoechst AktiengesellschaftInventors: Georg Pawlowski, Heidrun Lutz
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Patent number: 5051418Abstract: Antibacterial 8-cyano-1-cyclopropyl-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid derivatives of the formula ##STR1## in which Y represents a carboxyl group, a nitrile group, an ester group --COOR.sup.1 or an acid amide group --CONR.sup.2 R.sup.3,X.sup.1 represents hydrogen nitro, alkyl or halogenX.sup.4 can be hydrogen or halogen, or alkyl,R.sup.4 and R.sup.5, together with the nitrogen atom to which they are bonded, form a 5- or 6-membered heterocyclic ring which can additionally contain the atoms or groups --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## as ring members or the group ##STR3## can also represent a ring system of the structure ##STR4## which can optionally be substituted on the ring carbons by methyl and pharmaceutically usable hydrates, salts or esters thereof.These compounds have a high antibacterial activity and are therefore suitable as active compounds for human and veterinary medicine.Type: GrantFiled: November 13, 1989Date of Patent: September 24, 1991Assignee: Bayer AktiengesellschaftInventors: Michael Schriewer, Klaus Grohe, Uwe Petersen, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
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Patent number: 5028693Abstract: Urethane-protected NCAs and MTAs are prepared by reacting an NCA or NTA with a haloformate in an inert diluent, under anhydrous conditions and in the presence of a tertiary nitrogen-containing base having an atom or functional group sufficiently electron rich and positioned relative to the nitrogen of said base so as to render said atom or group capable of complexing with the H--N< group of said N-carboxyanhydride or N-thiocarboxyanhydride but able to generate N-carboxyanhydride or N-thiocarboxyanhydride anionic complexes capable of reacting with the haloformate.Type: GrantFiled: July 13, 1989Date of Patent: July 2, 1991Assignee: Bioresearch, Inc.Inventors: William D. Fuller, Michael P. Cohen, Fred R. Naider, Murray Goodman
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Patent number: 5028711Abstract: Benzopyran derivatives of the general formula I ##STR1## are disclosed. The compounds are therapeutic active compounds.Type: GrantFiled: July 6, 1989Date of Patent: July 2, 1991Assignee: Beiersdorf AktiengesellschaftInventors: Wolfgang Stenzel, Theo Schotten, Ben Armah
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Patent number: 5017721Abstract: A new process for preparing oxalyl- and oxamyl-hydrazides which comprises contacting oxamide or diacetyloxamide with the corresponding hydrazine derivative of formulaR.sub.1 R.sub.2 N--NHR.sub.3wherein R.sub.1 represents a hydrogen atom or an optionally substituted alkyl, cycloalkyl, aryl, or aryl-alkyl group, R.sub.2 is a hydrogen atom or an optionally substituted alkyl group, or R.sub.1 and R.sub.2 taken together with the adjacent nitrogen atom represent a saturated heterocyclic ring, and R.sub.3 is a hydrogen atom or an optionally substituted alkyl group.Type: GrantFiled: April 21, 1989Date of Patent: May 21, 1991Assignee: Enichim ANIC S.p.A.Inventors: Giuseppe Messina, Loreno Lorenzoni, Paolo Calaresu, Giovanni M. Sechi
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Patent number: 5015284Abstract: Compounds of the formula I, their stereoisomers or their salts ##STR1## wherein A denotes >C(R.sup.4).sub.2 or >C.dbd.C(R.sup.5).sub.2 ; R.sup.1 denotes H, an optionally substituted aliphatic or cycloaliphatic radical, forfuryl, tetrahydrofurfuryl or (substituted) phenyl; R.sup.2 denotes H, alkyl, alkenyl, alkynyl or alkoxy; R.sup.3 denotes a radical of the formulae ##STR2## X denotes O, S or NR.sup.12 and Y denotes O or S, possess excellent herbicidal and plant-growth regulating properties.Type: GrantFiled: April 6, 1989Date of Patent: May 14, 1991Assignee: Hoechst AktiengesellschaftInventors: Lothar Willms, Klaus Bauer, Hermann Bieringer, Helmut Burstell
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Patent number: 5001138Abstract: 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: May 4, 1989Date of Patent: March 19, 1991Assignee: Nihon Tokushu Noyaku Seizo, K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Koichi Moriya
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Patent number: 4997822Abstract: There are disclosed compounds of the formula ##STR1## The compounds have antitumour and AIDS treatment activity.Type: GrantFiled: February 20, 1987Date of Patent: March 5, 1991Assignee: Asta Pharma AktiengesellschaftInventors: Hans-Jurgen Hohorst, Ludmilla Bielicki, Georg Voelcker, Ulf Niemeyer
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Patent number: 4988701Abstract: Cyclic amino-thioacetal amides of formula I ##STR1## wherein X is O, S, p is 1 or 2, R and R.sub.1 are optionally esterified hydrogen or carboxy, A is a single bond, methylene or ethylene, m is zero or 1, n is an integer 1 to 7 and y is a imidazole or .beta.-pyridylmethyl residue.Compounds I have valuable therapeutic properties.Type: GrantFiled: December 15, 1989Date of Patent: January 29, 1991Assignee: Boehringer Biochemia Robin S.p.A.Inventors: Roberto Di Domenico, Carmelo A. Gandolfi, Silvano Spinelli, Bruno Lumachi, Odoardo Tofanetti, Sergio Tognella
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Patent number: 4987132Abstract: A saturated heterocyclic carboxamide derivative of the following general formula (I) and salts thereof which have platelet activating factor (PAF) antagonizing activity.Type: GrantFiled: August 16, 1988Date of Patent: January 22, 1991Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Toshiyasu Mase, Hiromu Hara, Hitoshi Nagaoka, Takumi Takahashi, Takeshi Suzuki, Kenichi Tomioka, Toshimitsu Yamada
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Patent number: 4985444Abstract: The invention relates to pyrazolopyridine compounds for the treatment of melancholia, heart failure, hypertension, renal insufficiency, edema, obesity, bronchial asthma, gout, hyperuricemia, sudden infant death syndrome, immunosuppression, diabetes, myocardiac infection, thrombosis, obstruction, arteriosclerosis obliterans, thrombophlebitis, cerebral infarction, transient ischemic attack or angina pectoris, said compounds being of the formula ##STR1## wherein R.sup.1 is aryl, andR.sup.2 is unsaturated heterocyclic group which contains at least one heteroatom selected from the group consisting of N, O and S, which may have one or more suitable substituent(s),or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 18, 1990Date of Patent: January 15, 1991Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Youichi Shiokawa, Atsushi Akahane, Hirohito Katayama, Takafumi Mitsunaga
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Patent number: 4977141Abstract: Non-peptidyl compounds characterized generally as aminoacyl aminodiol carbamates are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: October 1, 1987Date of Patent: December 11, 1990Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 4960908Abstract: Novel isoflavone derivatives are provided which have the formula ##STR1## and which exhibit cancerocidal and immunosuppressive activity. The invention also provides pharmaceutical compositions containing the derivatives, methods of use and processes for their preparation.Type: GrantFiled: October 21, 1988Date of Patent: October 2, 1990Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Hiroshi Ogawara, Shunichi Watanabe
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Patent number: 4957941Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## where Y is H or OH;j is an integer from 0 to 4;k is an integer from 0 to 4, and whereinm is an integer from 1 to 4;n is an integer from 1 to 4;p is an integer from 1 to 4; andX may be nonexistent or may be O, S, NH or CH.sub.2 or salts thereof, but when X is nonexistent the terminal group in which both the n-chain and the p-chain is a methyl group. ##STR2## The reaction was performed under reflux condensation. Following the reaction, which was usually complete within a few hours, the acid chlorides were vacuum distilled and reacted with a thiol compound as described above.The compounds of this invention are anti-muscarinic agents (cholinergic-muscarinic receptor antagonists) which inhibit the actions of acetylcholine on autonomic effectors innervated by postganglionic cholinergic nerves as well as on smooth muscle that lacks cholinergic innervation.Type: GrantFiled: January 9, 1990Date of Patent: September 18, 1990Assignee: United Pharmaceuticals, Inc.Inventor: William M. Davis
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Patent number: 4946942Abstract: The invention relates to urethane-protected amino acid-N-carboxyanhydride and N-thiocarboxyanhydride compounds which are useful in peptide, polypeptide and protein synthesis. Disclosed herein is the preparation and use of these novel compounds.Type: GrantFiled: March 11, 1988Date of Patent: August 7, 1990Assignee: Bioresearch, Inc.Inventors: William D. Fuller, Michael P. Cohen, Fred R. Naider, Murray Goodman
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Patent number: 4939140Abstract: A heterocyclic oxophthalazinyl acetic acid having aldose reductast inhibitory activity of the formula ##STR1## wherein X is oxygen or sulfur; Z is a covalent bond, O, S, NH or CH.sub.2 or CHR.sub.5 Z is vinyl; R.sub.1 is hydroxy, or a prodrug group; R.sub.2 is a heterocyclic group, R.sub.3 and R.sub.4 are hydrogen or the same or a different substituent, and R.sub.5 is hydrogen, methyl or trifluoromethyl. The pharmaceutically acceptable acid addition salts of the above compounds wherein R.sub.1 is di(C.sub.1 -C.sub.4)alkylamino or (C.sub.1 -C.sub.4)alkoxy substituted by N-morpholino or di(C.sub.1 -C.sub.4)alkylamino and the pharmaceutically active base addition salts of the above compounds wherein R.sub.1 is hydroxy are also aldose reductase inhibitors.Type: GrantFiled: October 27, 1988Date of Patent: July 3, 1990Assignee: Pfizer Inc.Inventors: Eric R. Larson, Banavara L. Mylari
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Patent number: 4923987Abstract: The invention provides a process for the preparation of nitromethylene heterocyclic compounds of general formula ##STR1## wherein R.sup.1 represents a hydrogen atom or a formyl or acetyl group, each moiety R.sup.2 is independently selected from hydrogen atoms and C.sub.1-4 alkyl and benzyl groups, and n is 2 or 3, which process comprises reacting an alkali metal methylnitrodithioacetate with a compound of formulaH.sub.2 N--(CR.sub.2.sup.2).sub.n --OSO.sub.3 H (II)wherein R.sup.2 and n are as defined above, optionally followed by conversion of the resulting compound of Formula I wherein R.sup.1 is hydrogen to the corresponding compound of Formula I wherein R.sup.1 is formyl or acetyl. Certain compounds of Formula I are known insecticidally active compounds.Type: GrantFiled: July 25, 1988Date of Patent: May 8, 1990Assignee: E. I. du Pont de Nemours and CompanyInventors: Martin Harris, Graham Heyes, Arthur Jackson
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Patent number: 4923858Abstract: Compounds of the general formula: ##STR1## wherein the radicals R.sub.1 and R.sub.2 are the same or different and represent hydrogen or C.sub.1 -C.sub.6 -alkyl, the radicals R.sub.3 and R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkanoyloxy, halogen or C.sub.2 -C.sub.6 -alkanoyl, X is oxygen, sulphur or the group --NR.sub.5 and R.sub.5 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkanoyl or benzoyl, m and n in each case may represent the integers 1, 2 or 3 and the phenyl radical A is unsubsituted or is substituted by halogen, nitro, C.sub.1 -C.sub.6 -alkyl, trifluoromethyl, C.sub.3 -C.sub.7 -cycloalkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkanoyloxy, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, C.sub.2 -C.sub.6 -alkanoylamino, CN, carboxy, C.sub.1 -C.sub.6 -alkoxycarbonyl, phenyl, C.sub.1 -C.sub.Type: GrantFiled: May 16, 1989Date of Patent: May 8, 1990Assignee: Asta Pharma AktiengesellschaftInventors: Jurgen Engel, Peter Emig, Bernd Nickel, Istvan Szelenyi
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Patent number: 4908453Abstract: Reagents useful in the preparation of 5'-biotinylated oligonucleotides are disclosed.Type: GrantFiled: January 23, 1989Date of Patent: March 13, 1990Assignee: E. I. Du Pont De Nemours and CompanyInventor: Anthony J. Cocuzza
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Patent number: 4904661Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus;wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate.Type: GrantFiled: December 16, 1987Date of Patent: February 27, 1990Assignee: Imperial Chemical Industries PLCInventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
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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: 4889848Abstract: Compounds of the formula ##STR1## wherein Q.sup.1 and the nitrogen atom taken together are a group of the formula >N--CH.sub.2 CH.sub.2 -- (a), >N--CH.sub.2 CH.sub.2 CH.sub.2 -- (b), >N--CH.dbd.CH-- (c), >N--CH.sub.2 --CH.dbd.CH-- (d), >N--CH.sub.2 --S(O).sub.p -- (e), >N--CH.sub.2 CH.sub.2 --S(O).sub.p -- (f) or >N--CH.dbd.CH--S(O).sub.p -- (g), p is the integer 0, 1 or 2, Ra is a phenyl, pyridyl or thienyl group which is optionally substituted by halogen, trifluoromethyl, nitro, lower alkyl or lower alkoxy, Rb and Rc each, independently, are hydrogen, halogen, trifluoromethyl, lower alkyl, lower alkoxy or nitro and the dotted line signifies an optional bond, or Rb and Rc together with the carbon atom denoted by .alpha. are a group of the formula >C.alpha.--S--CH.dbd.CH-- (h), >C.alpha.--CH.dbd.CH--S-- (i) or >C.alpha.--CH.dbd.CH--CH.dbd.Type: GrantFiled: January 5, 1988Date of Patent: December 26, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Ulf Fischer, Fernand Schneider, Ulrich Widmer
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Patent number: 4877785Abstract: Non-peptidyl compounds characterized generally as .beta.-succinamidoacyl aminodios are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: October 1, 1987Date of Patent: October 31, 1989Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 4876247Abstract: The invention relates to methylenediphosphonic acid derivatives of the formula: ##STR1## in which: R.sub.1 represents:a C.sub.1 -C.sub.6 alkyl group,a C.sub.5 -C.sub.7 cycloalkyl group,a phenyl group optionally monosubstituted or polysubstituted by a halogen, a C.sub.1 -C.sub.6 alkyl group or a trifluoromethyl group, ora 5-membered or 6-membered heterocycle containing 1 or 2 heteroatoms chosen from nitrogen and sulfur,Alk denotes a linear or branched C.sub.1 -C.sub.6 alkylene group,R.sub.2 represents hydrogen, a C.sub.1 -C.sub.6 alkyl group or a --CONH.sub.2 group,R.sub.3 represents hydrogen, a C.sub.1 -C.sub.6 alkyl group, a benzyl group or a phenyl group optionally substituted by chlorine or methyl groups; or alternativelyR.sub.2 and R.sub.3, taken together, represent a (CH.sub.2).sub.m group, in which m=4 or 5, and finallyn represents 0 or the integer 1 or 2.These derivatives possess antirheumatic properties.Type: GrantFiled: October 30, 1987Date of Patent: October 24, 1989Assignee: SanofiInventors: Alain Barbier, Jean-Claude Breliere, Georges Garcia
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Patent number: 4861879Abstract: Substituted [[4-[4-(4-phenyl-1-piperazinyl)phenoxymethyl]-1,3-dioxolan-2-yl]methyl]-1H -imidazoles and 1H-1,2,4-triazoles having antimicrobial properties and being particularly useful in the treatment of vaginal candidosis.Type: GrantFiled: February 9, 1988Date of Patent: August 29, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Jan Heeres, Raymond A. Stokbroekx, Leo J. J. Backx
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Patent number: 4851406Abstract: The present invention provides indole derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl, cycloalkyl, cycloalkenyl, carboxyl, cyano, alkylcarbonyl, alkoxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl or aryl radical, R.sub.2 is a hydrogen atom or an alkyl, trihalogenomethyl, hydroxyl, cycloalkyl, cyano, carboxyl, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl, alkylaminocarbonyl or dialkylaminocarbonyl radical; R.sub.2 is a heterocyclic five-membered ring containing 1 to 4 heteroatoms or a heterocyclic six-membered ring containing 1 to 5 heteroatoms, the heteroatoms of the five- and six-membered rings being the same or different and being nitrogen, oxygen or sulphur and one or more of the nitrogen atoms optionally carrying an oxygen atom, the said five- and six-membered rings optionally being substituted by one or more alkyl, alkoxy, alkylthio, oxo, hydroxyl, nitro, amino, halogen or cyano groups; or R.sub.Type: GrantFiled: September 4, 1986Date of Patent: July 25, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Wolfgang von der Saal, Walter-Gunar Friebe, Bernd Muller-Beckmann, Gisbert Sponer
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Patent number: 4839356Abstract: The invention provides thiazinone derivatives of general formula I: ##STR1## wherein X is O, S or NH, and R represents an optionally substituted alkyl, alkenyl, heterocyclic or aryl group; a process for the preparation of such compounds; compositions containing them and their use as fungicides.Type: GrantFiled: May 13, 1987Date of Patent: June 13, 1989Assignee: Shell Internationale Research Maatschappij B.V.Inventor: Mandy E. Coombs
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Patent number: 4835280Abstract: The present invention provides Indolines of the formula: ##STR1## ps useful to provide pharmaceutically active pyrrolobenzimidazoles or tautomers thereof, of the formula: These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.Type: GrantFiled: July 14, 1987Date of Patent: May 30, 1989Assignee: Boehringer Mannheim GmbHInventors: Alfred Martens, Jens-Peter Holck, Herbert Berger, Bernd Muller-Beckman, Klaus Strein, Egon Roesch
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Patent number: 4832732Abstract: Novel herbicidal 1-methyl-1H-imidazole -5-carboxylic acid derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants. Further the invention also relates to a process for making these novel compounds.Type: GrantFiled: December 17, 1987Date of Patent: May 23, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: William R. Lutz, Guy R. E. Van Lommen, Victor Sipido, Wim G. Verschueren
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Patent number: 4831032Abstract: The present invention provides benzimidazoles of the general formula: ##STR1## wherein R.sub.1, X, A, and R.sub.2 are as defined in the specification. The present invention also provides processes for the preparation of these new benzimidazoles and pharmaceutical compositions containing them, as well as intermediates for the preparation thereof.The new benzimidazoles are useful to treat heart or circulatory diseases which respond to a lowering of blood pressure, a positive inotropic action and/or an improvement in microcirculation.Type: GrantFiled: July 3, 1986Date of Patent: May 16, 1989Assignee: Boehringer Mannheim GmbHInventors: Wolfgang von der Saal, Alfred Mertens, Herbert Berger, Bernd Muller-Beckmann, Klaus Strein
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Patent number: 4816454Abstract: Substituted 4,5-dihydro-3(2H)-pyridazinones of the formula I ##STR1## wherein R, for example, denotes a radical of the formula ##STR2## R.sup.1 and R.sup.2, for example, denote hydrogen or methyl, R.sup.3, for example, denotes 2-methoxy-ethoxy, 3-pyridyl-methoxy, amino-carbonyl-methoxy, hydroxy-carbonyl-methoxy, methyl-thio, (2-methoxy-ethyl)-amino-carbonyl-methoxy, 3-pyridyl-methyl or 5-methyl-1,3,4-oxadiazol-2-yl and R.sup.4, for example, denotes hydrogen, have useful pharmacological properties and can therefore be used for the preparation of pharmacological products.Type: GrantFiled: September 12, 1985Date of Patent: March 28, 1989Assignee: Cassella AktiengesellschaftInventors: Gerhard Zoller, Rudi Beyerle, Melitta Just, Helmut Bohn, Piero Martorana, Rolf-Eberhard Nitz
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Patent number: 4804663Abstract: 3-Piperdinyl-1,2-benzisothiazoles and 3-piperidinyl-1,2-benzisoxazoles and their pharmaceutically acceptable acid addition salts having useful antipsychotic properties and being useful in the treatment of a variety of complaints in which serotonin release is of predominant importance.Type: GrantFiled: February 5, 1986Date of Patent: February 14, 1989Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo E. J. Kennis, Jan Vandenberk
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Patent number: 4783451Abstract: An organophosphorus compound having the formula: ##STR1## wherein X is ##STR2## Z is an oxygen atom or a sulfur atom, and each of R.sub.1 and R.sub.2 is an alkyl group which may be substituted by halogen, alkoxy or alkylthio. The compound is useful as an insecticide, miticide, nematicide or soil pesticide.Type: GrantFiled: June 25, 1986Date of Patent: November 8, 1988Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Takahiro Haga, Tadaaki Toki, Toru Koyanagi, Hiroshi Okada, Kiyomitsu Yoshida, Osamu Imai
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Patent number: 4778914Abstract: Herbicidal mixtures comprising (1) a diphenyl ether of the formula: ##STR1## or a salt thereof, wherein R.sup.1 is, for example, alkyl; R.sup.2 is hydrogen, halogen or nitro; R.sup.3 is hydrogen, halogen, alkyl, trifluoromethyl or cyano; R.sup.4 is hydrogen, halogen or trifluoromethyl; R.sup.5 is hydrogen, halogen or trifluoromethyl and R.sup.6 is hydrogen or alkyl of 1 to 6 carbons and (2) another herbicide not of formula (I). Intermediates for preparing the formula (I) compounds and processes for using these compounds are also disclosed.Type: GrantFiled: February 19, 1986Date of Patent: October 18, 1988Assignee: Imperial Chemical Industries PLCInventors: David Cartwright, David J. Collins
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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: 4772706Abstract: An improved process for the preparation of 7-substituted amino-1-alkyl- or cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids is described where tetrafluorobenzoyl chloride is converted in three operations via 1-alkyl or 1-cycloalkyl-1,4-dihydro-6,7,8-trifluoro-4-oxoquinoline-3-carbonitrile which in a separate step or in situ is displaced and hydrolyzed to the desired product.Type: GrantFiled: January 13, 1986Date of Patent: September 20, 1988Assignee: Warner-Lambert CompanyInventors: James N. Wemple, James R. Zeller, John M. Domagala
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Patent number: 4762550Abstract: This invention relates to novel pyrazolesulfonamides, agricultural compositions thereof and the methods of their use as general and/or selective herbicides and/or plant growth regulants.Type: GrantFiled: August 13, 1987Date of Patent: August 9, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Stephen L. Hartzell
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Patent number: 4759790Abstract: This invention relates to herbicidally active sulfonamide compounds having a heterocyclic carbonyl group ortho to the sulfonyl bridge.Type: GrantFiled: May 21, 1987Date of Patent: July 26, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Joel R. Christensen
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Patent number: 4755211Abstract: This invention relates to herbicidally active sulfonamide compounds, agriculturally suitable compositions thereof and a method of their use as general and/or selective herbicides or plant growth regulants. More specifically the herbicidally active sulfonamides of this invention have an ortho cyclic saturated or partially saturated group which includes a carbonyl or sulfonyl radical.In the most common situation, the control of undesired vegetation is desired to permit the growth of useful crops such as cotton, rice, corn, wheat and soybeans, to name a few. Unchecked weed growth in such useful crops can cause significant losses, reducing profit to the farmer and increasing costs to the consumer. In other situations, herbicides are desired which will control all plant growth. Examples of areas in which complete control of all vegetation is desired and areas around fuel storage tanks, ammunition depots and industrial storage areas.Type: GrantFiled: January 29, 1987Date of Patent: July 5, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Mark E. Thompson
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Patent number: 4746738Abstract: Skin treating composition on the basis of compatible carrier and additional compositions with a content of a defined tetrahydro-1,3-thiazine-2,4-dion derivatives as active ingredients for thickening the epidermis. The skin treating compositions are applied 1-2 times daily onto the skin for about 3 to 4 weeks. Due to the thickening of the epidermis they cause a reinforcmenet of the skin, in particular against sun rays, cold and the contact with noxious environmental substances of all kinds. Moreover, the skin treating compositions are suitable for a proplylactic fighting of the so-called old age skin. An object of the invention are novel tetrahydro-1,3-thiazine-2,4-dion derivative which are active in the aforementioned manner having the formula ##STR1## wherein R denotes H, alkyl, aryl, arylalkyl has substituted arylalkyl or substituted aryl in the aryl portion, R.sup.a =H is aryl or substituted aryl, R.sup.b =H, denotes aryl or substituted aryl and R.sup.c -H, represents alkyl or aryl, provided that R.sup.Type: GrantFiled: March 24, 1987Date of Patent: May 24, 1988Assignee: Wella AktiengesellschaftInventors: Wolfgang Hanefeld, Rudi Rothlisberger, Friedrich Noser
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Patent number: 4742169Abstract: The invention is a process for the preparation of halohydroxyalkyl carbamates which comprises contacting an epihalohydrin carbonate with a secondary amine-containing compound, wherein the secondary amine has a pKa at which the secondary amine will react with the epihalohydrin carbonate and which does not catalyze the formation of unwanted by-products in the further presence of an acid scavenger capable of forming a salt with the hydrogen halide by-product formed, in an amount sufficient to prevent the formation of unwanted by-products, in a polar organic solvent under conditions such that a halohydroxyalkyl carbamate, wherein the carbamate nitrogen is tertiary, is prepared.Type: GrantFiled: April 5, 1985Date of Patent: May 3, 1988Assignee: The Dow Chemical CompanyInventors: Marsha A. Paul, George A. Doorakian
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Patent number: 4737184Abstract: Novel N-(heterocyclicaminocarbonyl) substituted thiophene-, furan- and pyrrolesulfonamides, such as N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno- [3,2-b]thiopyran-3-sulfonamide, 4,4-dioxide and N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno[3,2-b ]thiopyran-3-sulfonamide, 4,4-dioxide and their method-of-use as herbicides are described.Type: GrantFiled: May 10, 1985Date of Patent: April 12, 1988Assignee: E. I. Du Pont De Nemours and CompanyInventor: Robert J. Pasteris
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Patent number: 4732898Abstract: The present invention are 2-(2-aryl-2-oxo-alkylidene) analogs of 1,2,3,4-tetrahydropyridine-3,5-pyridinecarboxylic acids and particularly esters thereof having valuable calcium antagonist and positive inotropic activity useful in the treatment of cardiovascular disorders, pharmaceutical compositions and methods of use therefor.Type: GrantFiled: March 3, 1987Date of Patent: March 22, 1988Assignee: Warner-Lambert CompanyInventors: Edward W. Badger, Michael D. Taylor
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Patent number: 4730000Abstract: Quinoline compounds having the formula: ##STR1## wherein R is a phenyl group or an aromatic heterocyclic group, Z is an aliphatic heterocyclic group or an amine, and R.sub.1 is hydrogen or a carboxy-protecting group. The compounds here disclosed have antibacterial properties.Type: GrantFiled: October 7, 1985Date of Patent: March 8, 1988Assignee: Abbott LaboratoriesInventor: Daniel T. Chu