Boron Or Silicon Containing Patents (Class 544/229)
  • Patent number: 5053072
    Abstract: Compounds of the formula I or salts thereof ##STR1## where R.sup.1 is H or an aliphatic radical; R.sup.2 and R.sup.3 are H, alkyl or phenyl; W is O, S, NR.sup.4 or NOR.sup.4 ; X is CHR.sup.2, O or NR.sup.4 ; L is a (substituted) phenyl, naphthyl or monocyclic heteroaryl radical, A is a (substituted) pyrimidyl, triazinyl, triazolyl or bicyclic heteroaryl radical, and m and n are 0 or 1, have advantageously herbicidal or plant growth-regulating properties.
    Type: Grant
    Filed: July 31, 1989
    Date of Patent: October 1, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Oswald Ort, Lothar Willms, Klaus Bauer, Hermann Bieringer, Arno Schulz
  • Patent number: 5053537
    Abstract: Ammonium compounds of the formula (I) ##STR1## in which at least one of the radicals R.sub.1 to R.sub.4 denotes a fluorine-containing alkyl radical having 4 to 30 carbon atoms and not more than three of the radicals R.sub.1 to R.sub.4 independently of one another denote hydrogen atoms or alkyl or hydroxyalkyl radicals having 1 to 30 carbon atoms, and R.sub.5 to R.sub.8 denote aryl, alkylaryl or halogenoaryl radicals or fluorine atoms, and iminium compounds of the formula (II) ##STR2## in which Q, together with the constituent ##STR3## forms a ring system having 4 to 17 carbon atoms, which can be interrupted by 1 to 4 hetero atoms and contain 2 to 9 double bonds, and which can be substituted by fluorine, chlorine, bromine or iodine atoms or alkyl (C.sub.1 -C.sub.6), alkoxy (C.sub.1 -C.sub.6), nitro or amino groups, R.sub.9 denotes a fluorine-containing alkyl (C.sub.1 -C.sub.30) radical, R.sub.10 denotes a hydrogen, fluorine, chlorine, bromine or iodine atom or an alkyl(C.sub.1 -C.sub.6), alkoxy (C.sub.1 -C.
    Type: Grant
    Filed: November 2, 1989
    Date of Patent: October 1, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Jorg Gitzel, Hans-Tobias Macholdt, Frank Wehowsky, Gunther Prossel
  • Patent number: 5043327
    Abstract: The present invention relates to novel positive inotropic and lusitropic 3,5-dihydroimidazo[2,1-b]quinazolin-2(1H)-one derivatives having positive inotropic and lusitropic properties which are useful in the treatment of warm-blooded animals suffering from Congestive Heart Failure. Pharmaceutical compositions containing said compounds as an active ingredient. Methods of preparing said compounds and pharmaceutical compositions.
    Type: Grant
    Filed: November 16, 1990
    Date of Patent: August 27, 1991
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers
  • Patent number: 5026708
    Abstract: A compound of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, C.sub.1-3 alkoxy, n-butoxy, i-butoxy, sec-butoxy, R.sup.5 R.sup.6 N-- (wherein R.sup.5 and R.sup.6 are independently hydrogen or C.sub.1-3 alkyl), trifluoromethyl, trifluoromethoxy, difluoromethoxy, fluoro, chloro, bromo, phenyl, phenoxy, benzyloxy, hydroxy, trimethylsilyloxy, diphenyl-t-butylsilyloxy, hydroxymethyl or --O(CH.sub.2).sub.l OR.sup.15 (wherein R.sup.15 is hydrogen or C.sub.1-3 alkyl, and l is 1, 2 or 3); or when located at the ortho position to each other, R.sup.1 and R.sup.2 together form --CH.dbd.CH--CH.dbd.CH-- or methylene dioxy; Y is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 --CH.dbd.CH-- or --CH.dbd.CH--CH.sub.2 --; Z is --Q--CH.sub.2 WCH.sub.2 --CO.sub.2 R.sup.12, ##STR2## (wherein Q is --C(O)--, --C(OR.sup.13).sub.2 -- or --CH(OH)--; W is --C(O)--, --C(OR.sup.13).sub.2 -- or --C(R.sup.11) (OH)--; R.sup.11 is hydrogen or C.sub.
    Type: Grant
    Filed: September 12, 1988
    Date of Patent: June 25, 1991
    Assignee: Nissan Chemical Industries Ltd.
    Inventors: Yoshihiro Fujikawa, Mikio Suzuki, Hiroshi Iwasaki, Mitsuaki Sakashita, Masaki Kitahara
  • Patent number: 5021572
    Abstract: The present invention pertains to boron containing thiouracil derivatives, their method of preparations, and their use in the therapy of malignant melanoma using boron neutron capture therapy.
    Type: Grant
    Filed: January 27, 1989
    Date of Patent: June 4, 1991
    Assignee: The United States Department of Energy
    Inventor: Detlef Gabel
  • Patent number: 5013854
    Abstract: An improved process for preparing trialkylsilyl ester and acid halide derivatives of carboxylic acids is provided along with novel trialkylsilyl ester intermediates of 2-(2-furyl)-2-methoximinoacetic acid.
    Type: Grant
    Filed: February 2, 1989
    Date of Patent: May 7, 1991
    Assignee: Eli Lilly and Company
    Inventor: Charles A. Bunnell
  • Patent number: 5011765
    Abstract: A novel cyan dye-forming coupler suitable for color photographic materials is disclosed. The coupler forms a cyan dye images excellent in resistivities to heat and moisture and fastness to light. The coupler has the following a chemical structure of Formula I; ##STR1## wherein X represents a group a group or atom, except hydrogen atom, capable of being split off upon reaction with the oxidized product of a color developing agent; R.sub.1, R.sub.2 and Y individually represent a hydrogen atom or a substituent; n is an integer of zero to 4, provided that the R.sub.2 s may be the same with or different from each other when n is 2, 3 or 4.
    Type: Grant
    Filed: June 22, 1990
    Date of Patent: April 30, 1991
    Assignee: Konica Corporation
    Inventors: Kimie Tachibana, Yutaka Kaneko
  • Patent number: 5010203
    Abstract: Novel cyclic N,N,N' and N,N,N',N'-substituted organyloxysilyl-functional silanes are prepared by reacting an aminopropyl silane with carbon disulfide and heating the dithiocarbamate.
    Type: Grant
    Filed: May 26, 1989
    Date of Patent: April 23, 1991
    Assignee: Degussa Aktiengesellschaft
    Inventors: Ulrich Deschler, Peter Kleinschmit
  • Patent number: 5008425
    Abstract: A process which comprises reacting under substantially anhydrous conditions a perfluoroalkyltrihydrocarbylsilane and a carbonyl compound in the presence of a catalyst such that the carbonyl compound is perfluoroalkylated.
    Type: Grant
    Filed: April 12, 1989
    Date of Patent: April 16, 1991
    Assignee: Ethyl Corporation
    Inventor: G. Patrick Stahly
  • Patent number: 5001241
    Abstract: Processes and intermediates are disclosed for the formation of compounds of formula (I) and (II): ##STR1##
    Type: Grant
    Filed: February 2, 1990
    Date of Patent: March 19, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Gerald E. Stokker, Ta J. Lee
  • Patent number: 4997943
    Abstract: Compounds of formula (I): ##STR1## (in which R.sup.1 is alkoxy, R is alkyl, haloalkyl, alkylamino, cycloalkyl or optionally substituted phenyl, X is chlorine or fluorine and Y is selected from certain specific heterocycles) have excellent antibacterial activity. They may be prepared by introducing the group represented by Y into the corresponding compound in which Y is replaced by a halogen atom.
    Type: Grant
    Filed: March 31, 1987
    Date of Patent: March 5, 1991
    Assignees: Sankyo Company Limited, Ube Industries Limited
    Inventors: Masayuki Iwata, Tomio Kimura, Yoshimi Fujihara, Tetsushi Katsube
  • Patent number: 4985426
    Abstract: There is disclosed a compound represented by the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or a lower alkyl group; R.sub.2 and R.sub.3 each independently represent a halogen atom or a lower alkyl group; R.sub.
    Type: Grant
    Filed: November 13, 1989
    Date of Patent: January 15, 1991
    Assignees: UBE Industries, Ltd., The Institute of Physical and Chemical Research
    Inventors: Hirosuke Yoshioka, Tokio Obata, Katsutoshi Fujii, Kiyoshi Tsutsumiuchi, Haruo Yoshiya
  • Patent number: 4981966
    Abstract: The invention relates to a new process for the preparation of compounds of the Formula I ##STR1## (wherein R stands for hydrogen or methyl) and pharmaceutically acceptable salts thereof which comprises reacting a compound of the Formula V ##STR2## (wherein R.sup.1 and R.sup.2 stand for an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or for an aromatic acyloxy group comprising 7-11 carbon atoms) with an amine of the Formula VI ##STR3## (wherein R has the same meaning as stated above) or a salt thereof and subjecting the compound of the Formula VII ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) to hydrolysis after or without isolation and if desired converting the compound of the Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the Formula I are known antibacterial agents.
    Type: Grant
    Filed: January 10, 1989
    Date of Patent: January 1, 1991
    Assignee: Chinoin Gyogyszer Es Vegyeszeti Termekek Gyara Rt.
    Inventors: Istvan Hermecz, Geza Kereszturi, Lelle Vasvari nee Debreczy, Agnes Horvath, Maria Balogh, Gabor Kovacs, Tamas Szuts, Peter Ritli, Judit Sipos, Aniko Pajor
  • Patent number: 4978656
    Abstract: There are disclosed synthetic derivatives of the natural product paraherquamide. The synthetic derivatives are prepared by reactions at the parahequamide A, B, E, F and G rings, that is at carbon atoms 14 to 16, the lactam ring and carbon atoms 24 to 26 as well as carbon atoms 5 and 12. The compounds are active antiparasitic agents and compositions for that use are also disclosed.
    Type: Grant
    Filed: August 12, 1988
    Date of Patent: December 18, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Timothy A. Blizzard, Helmut Mrozik, Gaye Marino, Peter J. Sinclair
  • Patent number: 4977291
    Abstract: A process of producing a silanic or siloxanic compound containing at least one cycloalkyl ring by the hydrogenation of a corresponding compound containing at least one aromatic ring, in the presence of a Raney nickel catalyst having a granulometry comprised essentially between 10 and 150 micrometers and a surface area of at least 80 m.sup.2 /g.
    Type: Grant
    Filed: September 15, 1989
    Date of Patent: December 11, 1990
    Assignee: Istituto Guido Donegani S.p.A.
    Inventors: Francesco Gementi, Loris Sogli, Raffaele Ungarelli
  • Patent number: 4977161
    Abstract: The present invention provides a compound of the formula: ##STR1## process for their production, pharmaceutical compositions containing them and their pharmaceutical uses, and intermediates useful for their production and processes for the production of such intermediates. The compounds are used as anti-hyperlipoproteinemic agents for example.
    Type: Grant
    Filed: November 13, 1989
    Date of Patent: December 11, 1990
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Yoshihiro Fujikawa, Mikio Suzuki, Hiroshi Iwasaki, Mitsuaki Sakashita, Masaki Kitahara
  • Patent number: 4965358
    Abstract: A new compound called N,N'-carbonyl-bis-(4-ethyl-2,3-dioxo)-piperazine of Formula I ##STR1## A process for the preparation thereof based on the reaction of 4-ethyl-2,3-dioxo-piperazine or a trimethylsilyl derivative thereof with carbonyl chloride or a derivative thereof.The use of the compound of Formula I as an intermediate in the preparation of compounds of Formula II ##STR2## where R is a radical, substituted in alpha position, of a molecule of an acid selected from the group formed by phenylacetic acid, p-hydroxy phenylacetic acid, a 6-(phenylacetamido)-penicillanic acid and a 7-(phenylacetamido)-cephalosporanic acid.
    Type: Grant
    Filed: November 10, 1988
    Date of Patent: October 23, 1990
    Assignee: Gema, S. A.
    Inventors: Juan Cabre Castellvi, Jose Diago Meseguer, Asuncion Esteve Bianchini, Carlos E. Lenhardt Padro, Esteve Sans Pitarch
  • Patent number: 4962109
    Abstract: This invention provides novel insecticidally and acaricidally active pyrimidine derivatives of formula (I): ##STR1## and stereoisomers thereof, wherein R.sup.1 is selected from alkyl; alkenyl; alkynyl; haloalkyl; haloalkenyl; and cycloalkyl optionally substituted by alkyl or halogen;R.sup.2 is selected from alkyl; haloalkyl; alkoxy; alkylamino; dialkylamino; halogen; cycloalkyl optionally substituted by halogen or alkyl; and phenyl optionally substituted by alkyl, haloalkyl, halogen or alkoxy;R.sup.3 is selected from hydrogen and halogen;R.sup.4 is the residue of an alcohol of formula R.sup.4 --OH which forms an insecticidal ester when combined with chrysanthemic acid, permethrin acid or cyhalothrin acid; andX is selected from oxygen and sulphur.
    Type: Grant
    Filed: June 13, 1988
    Date of Patent: October 9, 1990
    Assignee: Imperial Chemical Industries PLC
    Inventors: Edward McDonald, Roger Salmon, Alan J. Whittle
  • Patent number: 4960775
    Abstract: Therapeutically useful pyrrolo[2,1-a]phthalazine derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 represent cycloalkyl, optionally substituted alkyl, alkenyl, alkynyl, aryl or heteroaryl, X represents ethylene or vinylene, R.sup.3 represents a group of the formula:--Y--CH.sub.2 --CH(OH)--CH.sub.2 --COOR.sup.5wherein Y represents carbonyl or hydroxymethylene and R.sup.5 represents hydrogen or optionally substituted alkyl, or R.sup.3 represents a lactone ring and the symbols R.sup.4 represent hydrogen, halogen, optionally substituted alkyl, alkenyl, alkynyl, aryl or heteroaryl, or R.sup.6 O-- wherein R.sup.6 represents alkyl, aryl or arylalkyl and salts thereof, processes for their preparation and compositions containing them are described.
    Type: Grant
    Filed: December 2, 1988
    Date of Patent: October 2, 1990
    Assignee: May & Baker Limited
    Inventors: Michael J. Ashton, Andrew W. Bridge, Donald I. Dron, Garry Fenton, David J. Lythgoe, Christopher G. Newton, David Riddell, Christopher Smith, Keith A. J. Stuttle
  • Patent number: 4960454
    Abstract: Herbicides of the formula (I):L--SO.sub.2 --NH--CO--NR.sub.6 --Ain which:L denotes one of the groups of the formulae L-1 to L-6 given below,A denotes the group of the formula (II) given below, ##STR1## R.sub.1, R.sub.2 and R.sub.3 can be identical or different and represent a C.sub.1 -C.sub.4 alkyl radical or a C.sub.7 -C.sub.11 aralkyl radical, especially benzyl;R.sub.7, R.sub.8 and R.sub.9 can be identical or different and represent a hydrogen or halogen atom, a C.sub.1 -C.sub.4 radical which is optionally substituted by one or more halogen atoms or C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio radicals, C.sub.3 -C.sub.6 cycloalkyl which is optionally substituted by one or more halogen atoms or C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio radicals, C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio which are optionally substituted by one or more halogen atoms or C.sub.1 -C.sub.4 alkoxy or C.sub.1 -C.sub.4 alkylthio radicals, R.sub.13 S(O).sub.
    Type: Grant
    Filed: June 15, 1988
    Date of Patent: October 2, 1990
    Assignee: Rhone-Poulenc Agrochimie
    Inventors: Guy Borrod, Alain Gadras
  • Patent number: 4954414
    Abstract: A composition including a cationic transition metal coordination complex and a borate anion, wherein said composition is capable of absorbing actinic radiation and producing free radicals which can initiate free radical addition polymerization of a free radical addition polymerizable or crosslinkable monomer is disclosed. The compositions are particularly useful as visible light photoinitiators.
    Type: Grant
    Filed: November 8, 1988
    Date of Patent: September 4, 1990
    Assignee: The Mead Corporation
    Inventors: Paul C. Adair, Peter Gottschalk
  • Patent number: 4948416
    Abstract: This invention relates to novel condensed ring sulfonylureas and their use as herbicides and growth regulants.
    Type: Grant
    Filed: March 27, 1989
    Date of Patent: August 14, 1990
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Robert J. Pasteris
  • Patent number: 4948418
    Abstract: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable compositions containing them, and their use as broad spectrum herbicides.
    Type: Grant
    Filed: August 30, 1989
    Date of Patent: August 14, 1990
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Joseph E. Semple
  • Patent number: 4946495
    Abstract: A 2-phenoxypyrimidine derivative having the formula: ##STR1## wherein X is a halogen atom or ##STR2## wherein X.sup.1 is a halogen atom, a lower alkyl group or a lower alkoxy group and k is 0, 1 or 2; R.sup.1 is a hydrogen atom, a benzyl group, --(CH.sub.2).sub.m R.sup.3 wherein R.sup.3 is a cyano group, a formyl group, a dialkylamino group, a phenyl group, a pyridyl group, a trimethylsilyl group, a naphthyl group, an alkoxycarbonyl group, a benzoyl group, an alkylthio group, a phenylthio group, an alkylsulfonyl group or a benzyloxy group and m is 1, 2 or 3, or ##STR3## wherein R.sup.4 is a hydrogen atom or a lower alkyl group, R.sup.5 is a lower alkyl group or ##STR4## wherein X.sup.2 is a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group or a nitro group, n is 0 or 1, provided that when R.sup.5 is an alkyl group, n is 1; and R.sup.2 is a chlorine atom or a methoxy group, provided that when R.sup.1 is a hydrogen atom or a benzyl group, X is ##STR5## and R.sup.
    Type: Grant
    Filed: April 13, 1988
    Date of Patent: August 7, 1990
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Nobuhide Wada, Yoshihiro Saito, Shoji Kusano, Yasufumi Toyokawa, Takeshige Miyazawa, Satoru Takahashi, Takayoshi Takehi
  • Patent number: 4939126
    Abstract: 1-Pyrrolidineacetamide derivatives of the formula ##STR1## wherein R.sub.1 is hydrogen atom or a trialkylsilyl group, R.sub.2 and R.sub.3 are hydrogen atom, respectively, when R.sub.1 is hydrogen atom, R.sub.4 is an alkyl group, R.sub.5 is a radical of ##STR2## in which R.sub.6 and R.sub.7 are an alkyl group, respectively, m and n are an integer of 1 to 3, respectively,or R.sub.4 represents together with R.sub.5 a hetero cyclic ring having nitrogen and silicon atoms or piperazine ring having a substituent of ##STR3## in which R.sub.6 and n have the meanings as referred to, and R.sub.2 and R.sub.4 as well as R.sub.3 and R.sub.5 form a hetero cyclic ring, respectively, connected with an alkylene chain, where R.sub.1 is the trialkylsilyl group, salts thereof, a process for the preparation thereof, as well as use thereof as for a medicine.
    Type: Grant
    Filed: July 11, 1988
    Date of Patent: July 3, 1990
    Assignee: Sanwa Kagaku Kenkyusho Co. Ltd.
    Inventors: Masayasu Kurono, Tsunemasa Suzuki, Tomoo Suzuki, Kiyotaka Hirooka, Yukiharu Matsumoto, Hiroshi Ozawa, Kiichi Sawai
  • Patent number: 4935426
    Abstract: N,N'-disubstituted piperazines of the general formula I ##STR1## where the group is unsaturated (.dbd.) or saturated (--) and the substituents R.sup.1, R.sup.2 and A have the following meanings:A is --, --CH.dbd., --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --,R.sup.1 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, alkylcycloalkyl, cycloalkenylalkyl, alkylcycloalkenyl, bicycloalkyl, bicycloalkylalkyl or alkylbicycloalkyl, these radicals being unsubstituted or substituted by hydroxy, halogen, alkoxy or trialkylsilyl,R.sup.1 is further heterocycloalkyl with oxygen and/or sulfur, heterocycloalkylmethyl with oxygen and/or sulfur, alkyl-substituted heterocycloalkylmethyl with oxygen and/or sulfur, andR.sup.2 is alkyl, alkoxy, trimethylsilyl, cycloalkyl, alkylthio,and plant-physiologically tolerated salts thereof, and fungicides containing these compounds.
    Type: Grant
    Filed: February 8, 1989
    Date of Patent: June 19, 1990
    Assignee: BASF Aktiengesellschaft
    Inventors: Matthias Zipplies, Hubert Sauter, Franz Roehl, Thomas Kuekenhoehner, Lothar Janitschke, Eberhard Ammermann, Gisela Lorenz
  • Patent number: 4927453
    Abstract: This invention relates to a novel class of sulfonylureas and their use as herbicides and plant growth regulants.
    Type: Grant
    Filed: August 30, 1988
    Date of Patent: May 22, 1990
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Stephen K. Gee
  • Patent number: 4927898
    Abstract: A polysiloxane having pendant, sterically-hindered heterocyclic moieties attached to a siloxane chain, and their use in stabilizing synthetic polymer compositions.
    Type: Grant
    Filed: September 6, 1988
    Date of Patent: May 22, 1990
    Assignee: Union Carbide Chemicals and Plastics Company Inc.
    Inventors: Roswell King, III, George N. Foster, Herbert E. Petty
  • Patent number: 4921974
    Abstract: This invention relates to novel intermediates and novel processes for their preparation where said intermediates are useful in the preparation of 5'-oxygenated derivatives (I) of lovastation and analogs thereof at the 8'-acyl side chain and 6'-position of the polyhydronaphthyl ring. Derivatives (I) and analogs thereof are useful in treating hypercholesterolemia.
    Type: Grant
    Filed: September 29, 1988
    Date of Patent: May 1, 1990
    Assignee: Merck & Co., Inc.
    Inventor: Mark E. Duggan
  • Patent number: 4921632
    Abstract: Liquid Crystal compounds represented by the following formula are disclosed. ##STR1## wherein R and R' are independently selected from alkyl groups containing 1.about.20 carbon atoms; X is --O--, --O--CO--O-- or direct bond; A.sub.1 and A.sub.2 are independently cyclic groups (such as phenylene and biphenylene), said cyclic groups may be substituted with 1.about.4 fluorine, chlorine or bromine atoms, or 1 or 2 substituent groups selected from the group consisting of cyano, nitro and trifluoromethyl groups; Y is --CO--O--, --O--CO--, --C.tbd.C--, --CH.sub.2 O--, --OCH.sub.2 --, --CH.dbd.N--, --N.dbd.CH--, --N.dbd.N--, --CH.sub.2 S--, --SCH.sub.2 -- or direct bond; and * represents asymmetric atom providing optical activity.
    Type: Grant
    Filed: August 19, 1988
    Date of Patent: May 1, 1990
    Assignees: NEC Corporation, Sanyo Chemical Industries, Ltd.
    Inventors: Toyokazu Nakamura, Yuzi Kato, Shohei Naemura, Chizuka Tani, Masahiro Satoh, Kunikiyo Yoshio, Hiroshi Kishiki, Hiroshi Hoshino
  • Patent number: 4920124
    Abstract: N-substituted 3,4-dihydropyrimidine compounds of the formula: ##STR1## wherein R is straight, branched, cyclic or cyclo-straight alkyl having from one to four carbon atoms; and X.sup.1, X.sup.2 and X.sup.3 are the same or different and are hydrogen, halogen, lower alkyl having from one to four carbon atoms, lower alkoxy having from one to four carbon atoms, nitro, trifluoromethyl, hydroxy, or t-butyldimethylsilyloxy with the proviso that the case wherein X.sup.1, X.sup.2 and X.sup.3 are all hydrogen is not applicable have substantially strong and lasting vasodilative effects. Therefore, the compounds are useful as agents for treating disorders of the cardiovascular system, for example, antihypertensive agents, circulation improver and antianginal agents.
    Type: Grant
    Filed: February 19, 1988
    Date of Patent: April 24, 1990
    Assignee: Suntory Limited
    Inventors: Hidetsura Cho, Masaru Ueda
  • Patent number: 4913723
    Abstract: Disclosed are herbicidal compounds, compositions containing them, and a method of use for the compositions in controlling undesired plant growth. The herbicidal compounds are compounds of the formula ##STR1## in which W is S or O and Z-Ph is a substituted phenyl group in which Z is -C(R).dbd.Q; R is H, lower alkyl, or aryl; Q is NR' or oxygen; R' is alkoxy, hydroxy, alkenyloxy, alkynyloxy, alkylcarbonyloxy, arylcarbonloxy, trialkylsilyloxy, arylalkoxy, aryl, alkyl, cycloalkyl, or a group of the formula --SO.sub.2 R", --OCO.sub.2 R", OC(O)NHR", or --CH.sub.2 CO.sub.2 R"; and R" is lower alkyl or aryl. The phenyl moiety Ph is advantageously multisubstituted.
    Type: Grant
    Filed: August 8, 1988
    Date of Patent: April 3, 1990
    Assignee: FMC Corporation
    Inventor: Jun H. Chang
  • Patent number: 4914206
    Abstract: The present invention provides lankacidin derivatives of the formula ##STR1## and procedures for the production thereof. The lankacidin derivatives [1] show excellent antimicrobial activities and thus can be used for prophylaxis and treatment of infectious disease in animals.
    Type: Grant
    Filed: December 15, 1988
    Date of Patent: April 3, 1990
    Assignee: Takeda Chemical Industries, LTD.
    Inventors: Isao Minamida, Naoto Hashimoto
  • Patent number: 4906749
    Abstract: Novel chromophor derivatives of cyclic anhydrides are provided which have the ability to react with a variety of organic substrates forming adducts which are useful in analytical techniques for the detection and measurement of biological compounds.
    Type: Grant
    Filed: January 24, 1989
    Date of Patent: March 6, 1990
    Assignee: Viomedics Inc.
    Inventor: Spyros Theodoropulos
  • Patent number: 4906278
    Abstract: This invention relates to certain heterocyclic sulfonylurea herbicidal compounds, agriculturally suitable compositions thereof and a method of their use.
    Type: Grant
    Filed: March 30, 1987
    Date of Patent: March 6, 1990
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Barry A. Wexler
  • Patent number: 4902686
    Abstract: New heterocyclic compounds having the general formula ##STR1## wherein R.sup.3 is ##STR2## CO.sub.2 R' or CONR'R", wherein R' and R" independently are C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl or C.sub.1-6 -alkoxymethyl;--A-- is --C(.dbd.O)--NR'"--, --NR'"--C(.dbd.O)--, or ##STR3## wherein R'" is C.sub.1-6 -alkyl; X is C or N; andR.sup.4 is hydrogen, halogen, CN, C.sub.1-6 -alkyl, C.sub.1-6 -alkynyl, trimethylsilyl-C.sub.1-6 -alkynyl, aryloxy which may be substituted with halogen, aralkoxy, C.sub.3-7 -cycloalkoxy which may be substituted with one or more C.sub.1-6 -alkyl groups, or NR""R'"", wherein R"" and R""' independently are C.sub.1-6 -alkyl or together with the nitrogen atom form a 3-7 membered heterocyclic ring.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics.
    Type: Grant
    Filed: April 20, 1989
    Date of Patent: February 20, 1990
    Assignee: A/S Ferrosan
    Inventors: Frank Watjen, Holger C. Hansen
  • Patent number: 4897108
    Abstract: The invention relates to certain sulfonylurea compounds having an ester group ortho to the sulfonylurea linkage which have been found to be excellent preemergent and postemergent herbicides or plant growth regulators.
    Type: Grant
    Filed: June 24, 1988
    Date of Patent: January 30, 1990
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Donald J. Dumas
  • Patent number: 4895885
    Abstract: The present invention relates to olefin polymers stabilized with polysiloxanes containing sterically hindered heterocyclic moieties, said polysiloxanes represented by the general formula M*.sub.v D.sub.x D*.sub.y T.sub.z Q.sub.w M*.sub.v.
    Type: Grant
    Filed: September 6, 1988
    Date of Patent: January 23, 1990
    Assignee: Union Carbide Chemicals and Plastics Company Inc.
    Inventors: George N. Foster, Herbert E. Petty, Roswell E. King, III
  • Patent number: 4895849
    Abstract: There are disclosed a compound represented by the formula: ##STR1## wherein R.sub.1 represents a hydrogen atom or a lower alkyl group; R.sub.2 and R.sub.3 each independently represent a halogen atom or a lower alkyl group; R.sub.
    Type: Grant
    Filed: October 5, 1987
    Date of Patent: January 23, 1990
    Assignee: Ube Industries, Ltd.
    Inventors: Hirosuke Yoshioka, Tokio Obata, Katsutoshi Fujii, Kiyoshi Tsutsumiuchi, Haruo Yoshiya
  • Patent number: 4881967
    Abstract: This invention pertains to novel heterocyclic 2,3-dihydrobenzofuran and chromane compounds, including stereoisomers, agriculturally suitable composition containing them, and their use as broad spectrum herbicides.
    Type: Grant
    Filed: June 2, 1988
    Date of Patent: November 21, 1989
    Assignee: E. I. Du Pont De Nemours and Company
    Inventor: Joseph E. Semple
  • Patent number: 4877779
    Abstract: Novel compounds and their salts are disclosed having the Formulas: ##STR1## wherein: R.sub.1 is hydrogen, phenyl, 9H-fluoren-9-yl, 10,11-dihydro-5H-dibenzo [a,d]cyclohepten-5-yl, 5H-dibenzo[a,d]cyclohepten-5-yl, 1,2,3,4-tetrahydro-1-naphthyl, 9H-xanthen-9-yl, 9H-thioxanthen-9-yl, 2-chloro-9H-thioxanthen-9-yl, 4H-chromanyl, diphenylmethyl, phenylcycloalkylmethyl wherein the bridgehead methylene may optionally be substituted with a hydroxy group and any of the phenyl or benzo-fused rings may be substituted with one or more R.sub.5 groups wherein R.sub.5 is selected from halogen, trifluoromethyl, lower alkyl, hydroxy or lower alkoxy groups; andR.sub.2 and R.sub.3, which may be the same or different, are hydrogen, lower alkyl, phenylalkyl (C.sub.1 -C.sub.5), wherein the phenyl ring may be substituted with one or more R.sub.5 groups or NR.sub.2 R.sub.
    Type: Grant
    Filed: May 17, 1988
    Date of Patent: October 31, 1989
    Assignee: Marion Laboratories, Inc.
    Inventors: Waclaw J. Rzeszotarski, Maria E. Guzewska, John P. Carter, Theodore C. Adams, Andrea C. Dupont, Carl Kaiser
  • Patent number: 4875928
    Abstract: Substituted azolylcyclopropyl-azolylmethyl-carbinol derivatives of the formula ##STR1## in which Ar is optionally substituted aryl or optionally substituted heteroaryl,R is hydrogen, alkyl, alkenyl, alkinyl, trialkylsilyl, optionally substituted phenylalkyl or an acyl radical, andX and Y each independently is a nitrogen atom or a CH group,and addition products thereof with acids and metal salts are effective in regulating plant growth and combating fungi. New intermediates are described, some of which are themselves active.
    Type: Grant
    Filed: October 28, 1985
    Date of Patent: October 24, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Erik Regel, Klaus Bockmann, Karl H. Buchel, Klaus Lurssen, Wilhelm Brandes, Jorg Konze, Paul Reinecke
  • Patent number: 4874861
    Abstract: Novel 3(2H)-pyridazinone derivatives having the general formula (I): ##STR1## wherein, R denotes a straight or branched C.sub.1 to C.sub.6 alkyl; A denotes a straight or branched C.sub.1 to C.sub.6 alkyl or a halogen; X denotes oxygen or sulfur atom; Q denotes a group; ##STR2## when A is a straight or branched C.sub.1 to C.sub.6 alkyl, and Q denotes a group: ##STR3## when A is a halogen atom; R.sup.1 and R.sup.2 denote each independently hydrogen, a lower alkyl, a lower haloalkyl, or 4-tert-butylphenyl; B denotes --CR.sup.6 .dbd.CR.sup.7 --, --CR.sup.6 R.sup.7 O--, or ##STR4## (wherein, R.sup.6 and R.sup.7 denote various specific organic radicals. A process for preparation of said derivatives is also provided. These derivatives are useful as an active ingredient of insecticidal, acaricidal, nematicidal and/or fungicidal compositions for agricultural and horticultural uses as well as of expellent compositions for ticks parasitic on animals.
    Type: Grant
    Filed: November 30, 1987
    Date of Patent: October 17, 1989
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Tomoyuki Ogura, Yasuo Kawamura, Shigeru Ishii, Masatoshi Baba, Masakazu Taniguchi, Masayoshi Hirose, Kiminori Hirata, Yoshinori Ochiai
  • Patent number: 4872901
    Abstract: Novel compounds of the formula: ##STR1## wherein R.sub.1 is a pyrazolyl group which may be substituted; R.sub.2 and R.sub.3 respectively are a lower alkyl group or a lower alkoxy group; and Z is CH or N, which are useful as herbicides.
    Type: Grant
    Filed: October 22, 1986
    Date of Patent: October 10, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Isao Aoki, Takashi Kuragano, Nobuyuki Okajima, Yoshiyuki Okada
  • Patent number: 4873244
    Abstract: New heterocyclic compounds having the general formula ##STR1## wherein ##STR2## CO.sub.2 R' or CONR'R", whereinR' and R" independently are C.sub.1-6 -alkyl, C.sub.3-7 -cycloalkyl or C.sub.1-6 -alkoxymethyl;--A-- is --C(.dbd.O)--NR'"--, --NR'"--C(.dbd.O)--, or ##STR3## wherein R'" is C.sub.1-6 -alkyl;X is C or N; andR.sup.4 is hydrogen, halogen, CN, C.sub.1-6 -alkyl, C.sub.1-6 -alkynyl, trimethylsilyl-C.sub.1-6 -alkynyl, aryloxy which may be substituted with halogen, aralkoxy, C.sub.3-7 -cycloalkoxy which may be substituted with one or more C.sub.1-6 -alkyl groups, or NR""R'"", wherein R"" and R'"" independently are C.sub.1-6 -alkoxy or together with the nitrogen atom form a 3-7 membered heterocyclic ring.The compounds are useful in psychopharmaceutical preparations as anticonvulsants, anxiolytics, hypnotics, and nootropics.
    Type: Grant
    Filed: February 16, 1988
    Date of Patent: October 10, 1989
    Assignee: A/S Ferrosan
    Inventors: WaFrank, Holger C. Hansen
  • Patent number: 4871849
    Abstract: The present invention relates to a process for the preparation of compounds of the general Formula I ##STR1## and pharmaceutically acceptable salts thereof (wherein R stands for piperazinyl or 4-methyl-piperazinyl) which comprises reacting a compound of the general Formula II ##STR2## (wherein R.sup.1 and R.sup.2 stand for halogen; an aliphatic acyloxy group comprising 2-6 carbon atoms and optionally substituted by halogen; or an aromatic acyloxy group comprising 7-11 carbon atoms) with a piperazine of the general Formula III ##STR3## (wherein R.sup.3 represent hydrogen or methyl) or a salt thereof, hydrolysing the compound of the general Formula IV ##STR4## thus obtained (wherein R, R.sup.1 and R.sup.2 are as stated above) without or after hydrolysis and if desired converting the compound of the general Formula I thus obtained into a salt thereof or setting free the same from its salt.The compounds of the general Formula I are known antibacterial agents.
    Type: Grant
    Filed: June 24, 1987
    Date of Patent: October 3, 1989
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
    Inventors: Istvan Hermecz, Geza Kereszturi, Lelle Vasvavi, Agnes Horvath, Maria Balogh, Gabor Kovacs, Tamas Szuts, Peter Ritli, Judit Sipos, Aniko Pajor
  • Patent number: 4871719
    Abstract: Novel 13-spiro-2'-[tetrahydrofuran]-milbemycins of the formula I ##STR1## in which X represents one of the groups --CH(OR.sub.1)--, --C(.dbd.O)-- or --C(.dbd.N--OH)--;R.sub.1 represents hydrogen or a OH-protecting group;R.sub.2 represents methyl, ethyl, isopropyl or sec.-butyl or the group --C(CH.sub.3).dbd.CH--A in which A represents methyl, ethyl or isopropyl; andR.sub.3 represents hydrogen; C.sub.1 -C.sub.10 -alkyl; C.sub.1 -C.sub.10 -alkyl substituted by at least one substituent selected from the group consisting of halogen, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkoxyalkoxy C.sub.3 -C.sub.9 -alkoxyalkoxyalkoxy, C.sub.1 -C.sub.6 -alkylthio, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.1 -C.sub.3 -alkyl-substituted C.sub.3 -C.sub.7 -cycloalkyl, hydroxy, benzyloxy, C.sub.1 -C.sub.6 -acyl and C.sub.1 -C.sub.6 -acyloxy, it being possible for each of the above-mentioned radicals representing or containing an alkoxy group to be terminally substituted at a terminal alkoxy group by hydroxy, halogen, C.sub.1 -C.sub.
    Type: Grant
    Filed: March 16, 1988
    Date of Patent: October 3, 1989
    Assignee: Ciba-Geigy Corporation
    Inventor: Peter Maienfisch
  • Patent number: 4871736
    Abstract: Stereoisomeric tricyclic bis(dioxopiperazines) of the formula ##STR1## wherein R is H or ##STR2## and the processes for the synthesis thereof are provided. The compounds are effective as antitumor or antimetastatic drugs.
    Type: Grant
    Filed: November 25, 1986
    Date of Patent: October 3, 1989
    Assignee: The Ohio State University
    Inventors: Raghunathan V. Nair, Donald T. Witiak
  • Patent number: 4868189
    Abstract: An organo-silicone compound of the formula ##STR1## wherein X is a methylene or carbonyl radical, Y is an NH or O, n is an integer, R.sub.1 is a hydrogen atom, halogen atom or alkyl group, R.sub.2, R.sub.3 and R.sub.4 are an alkyl group, alkoxy group, phenyl radical or substituted phenyl radical, respectively, and R.sub.5 is a hydrogen atom or a group of ##STR2## in which X, Y, n, R.sub.2, R.sub.3 and R.sub.4 have the meanings as referred to, and used as an anti-tumor agent or for use in anti-tumor compositions.
    Type: Grant
    Filed: January 4, 1988
    Date of Patent: September 19, 1989
    Assignee: Sanwa Kagaku Kenkyusho Co.
    Inventors: Masayasu Kurono, Ryoichi Unno, Hiromoto Kimura, Hiroshi Ozawa, Takahiko Mitani, Takahito Jomori, Masahiko Koketsu, Hisashi Michishita, Kiichi Sawai
  • Patent number: 4868187
    Abstract: Nucleoside analogues having a ring-open structure, of general formula: ##STR1## where R and R' may be hydrogen, silyl groups, substituted alkyl groups, benzyl groups and the like, and X is an optionally substituted base such as guanine or adenine, have been shown to exhibit anti-viral and other biological acivities at non-toxic levels.
    Type: Grant
    Filed: March 9, 1987
    Date of Patent: September 19, 1989
    Assignee: Syntex (U.S.A.) Inc.
    Inventor: Kelvin K. Ogilvie