The Benzene Ring Is Part Of A Substituent Which Contains Halogen Bonded Directly To Carbon Patents (Class 564/53)
  • Patent number: 5223529
    Abstract: Compounds of formula: ##STR1## in which R.sub.1 is (a) a phenyl radical or a substituted phenyl radical, (b) a chain --CH(R.sub.8)--COOR.sub.4, (c) a chain --CH.sub.2 --CO--NR.sub.5 R.sub.6 or (d) a phenylalkyl radical, R.sub.2 is a methylene or ethylene radical or a radical --CH(R.sub.7)--, R.sub.3 is a 1- or 2-naphthyl radical, 2- or 3-indolyl or phenylamino radical in which the phenyl ring is optionally substituted on the understanding that, when R.sub.3 is 1- or 2-naphthyl or 2- or 3-indolyl radical, R.sub.7 cannot represent a benzyl, alkylthioalkyl or phenyl radical, as well as, when R.sub.2 is a radical --CH(R.sub.7)--, their racemates and their stereoisomers, and medicinal products containing them.
    Type: Grant
    Filed: May 11, 1990
    Date of Patent: June 29, 1993
    Assignee: Rhone-Poulenc Sante
    Inventors: Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Gerard Roussel, Franco Manfre
  • Patent number: 5198582
    Abstract: A process for preparing N,N'-disubstituted urea derivatives of the following formula (I) ##STR1## wherein Ar represents an unsubstituted aromatic radical or an aromatic radical substituted with a halogen atom, an alkyl group, or an alkoxy group, which comprises reacting an aromatic mono-nitro compound, an aromatic primary amine, and synthesis gas in the presence of a catalyst consisting essentially of a divalent palladium compound as a main catalyst component and an ammonium or a phosphonium salt containing halogen atom as a co-catalyst component, and a non-polar solvent.
    Type: Grant
    Filed: October 22, 1991
    Date of Patent: March 30, 1993
    Assignee: Lucky Ltd.
    Inventors: Jae S. Oh, Sang M. Lee
  • Patent number: 5166429
    Abstract: Diurea Derivatives represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A chloresterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester to the smooth muscle of arterial wall in the blood vessel.
    Type: Grant
    Filed: September 24, 1991
    Date of Patent: November 24, 1992
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
  • Patent number: 5126483
    Abstract: Novel 1-phenylakyl-3-phenylurea derivatives represented by the following formula (I): ##STR1## wherein R.sup.1 is an alkyl group of 1 to 8 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, R.sup.2 is an alkyl group of 1 to 15 carbon atoms, each of R.sup.3 and R.sup.4 is independently an alkyl group of 1 to 5 carbon atoms, m is an integer of 1 to 3, and n is 0 or 1, are provided.The compounds are potent in reducing the cholesterol level in serum, and useful for treating hyperlipemia and atherosclerosis.
    Type: Grant
    Filed: August 3, 1990
    Date of Patent: June 30, 1992
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Tetsuo Sekiya, Shinya Inoue, Chiaki Hyodo, Hiromi Okushima, Kohei Umezu, Kazuo Suzuki
  • Patent number: 5106873
    Abstract: This invention relates to novel compounds which are ACAT inhibitors rendering them useful in lowering blood cholesterol levels. The compounds contain two urea or thiourea, amide, or amine moieties or combinations of said moieties and have the following general formula: ##STR1## wherein m and n are zero or one, W and YNH and ##STR2## form the urea, thiourea, amide or amine moieties; and R.sub.1 and R .sub.2 are hydrogen or a hydrocarbon radical.
    Type: Grant
    Filed: June 26, 1990
    Date of Patent: April 21, 1992
    Assignee: Warner-Lambert Company
    Inventors: Patrick M. O'Brien, Drago R. Sliskovic, Michael W. Wilson
  • Patent number: 5099021
    Abstract: Process for the preparation of pure, unsymmetrically disubstituted ureas of the general formula ##STR1## in which R denotes a phenyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy, aryloxy or trifluoromethyl groups, an oxazolyl, isoxazolyl, thiazolyl, isothiazolyl, benzoxazolyl or benzothiazolyl radical which is unsubstituted, or monosubstituted or polysubstituted by halogen atoms or alkyl, alkoxy or trifluoromethyl groups and R.sub.1 and R.sub.2 independently of one another denote a hydrogen atom or an alkyl group, where R.sub.1 and R.sub.2 are not simultaneously hydrogen or R.sub.1 and R.sub.2 together denote a butylene or pentylene group, by reaction of an N-alkyl- or N,N-dialkylurea with an unsubstituted or substituted arylamine or a heterocyclic amine in the presence of that amine which is already present in the starting material, the respective N-alkyl- or N,N-dialkylurea.
    Type: Grant
    Filed: October 30, 1990
    Date of Patent: March 24, 1992
    Assignee: Agrolinz Agrarchemikalien Gesellschaft m.b.H.
    Inventors: Rudolf H. Worther, Horst Korntner, Egmont Auer, Kurt Thonhofer
  • Patent number: 5091419
    Abstract: Diurea derivatives are provided which are represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A cholesterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester on the smooth muscle of arterial wall in the blood vessels.
    Type: Grant
    Filed: October 2, 1990
    Date of Patent: February 25, 1992
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
  • Patent number: 5091571
    Abstract: A process for preparing N, N-disubstituted urea and more particularly, to an improved process for preparing N,N'-disubstituted urea derivatives of the following formula (I) comprising ##STR1## wherein each of Ar.sup.1 and Ar.sup.2 represents unsubstituted aromatic radical or aromatic radical substituted with halogen, atom, alkyl group, or alkoxy group, and Ar.sup.1 and Ar.sup.2 are the same or different, reacting aromatic mono-nitro compound, aromatic primary amines, and carbon monoxide in the presence of the catalyst composition consisting of a palladium compound as a main catalyst and an ammonium or a phosphonium salt containing halogen atom aS a co-catalyst, and a non-polar solvent.
    Type: Grant
    Filed: October 31, 1990
    Date of Patent: February 25, 1992
    Assignee: Lucky, Ltd.
    Inventors: Chul Woo Lee, Jae Sung Lee, Sang Moo Lee
  • Patent number: 5063247
    Abstract: Novel diphenylurea derivatives represented by the following formula (I): ##STR1## wherein R.sub.1 is an alkyl group of 5 to 18 carbon atoms, each of R.sub.2 and R.sub.3 is independently an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, R.sub.4 is hydrogen atom, an alkyl group of 1 to 5 carbon atoms, an alkoxy group of 1 to 5 carbon atoms or a halogen atom, and X is oxygen atom or sulfur atom, are provided.The compounds are potent in reducing the cholesterol level in serum, and useful for treating hyperlipemia and atherosclerosis.
    Type: Grant
    Filed: June 13, 1990
    Date of Patent: November 5, 1991
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Tetsuo Sekiya, Shinya Inoue, Masao Taniguchi, Kohei Umezu, Kazuo Suzuki
  • Patent number: 5055582
    Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.
    Type: Grant
    Filed: December 13, 1988
    Date of Patent: October 8, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert B. Garland, Masateru Miyano
  • Patent number: 5015762
    Abstract: Aralkylphenylureas of the formula ##STR1## where R.sup.1 and R.sup.2 are hydrogen, alkoxy or unsubstituted or substituted alkyl, cycloalkyl, alkenyl or alkynyl, or R.sup.1 and R.sup.2 together are unsubstituted or substituted alkylene which may or may not be interrupted by oxygen or sulfur, Y is hydrogen, alkyl, halogen, alkoxy or haloalkyl, A is unsubstituted or substituted alkylene, Z is hydrogen, alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, aralkyl, aryl, aryloxy, halogen, a C.sub.4 H.sub.4 chain which is fused to the benzene ring to give a substituted or unsubstituted naphthyl ring, alkoxy, haloalkoxy, alkylthio, thiocyanato, cyano, ##STR2## R' and R" being hydrogen, alkyl, alkoxy, alkylthio, cycloalkyl or unsubstituted or substituted phenyl and n is 1, 2, 3 or 4, and herbicides containing these ureas.
    Type: Grant
    Filed: May 28, 1981
    Date of Patent: May 14, 1991
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulrich Schirmer, Wolfgang Rohr, Bruno Wuerzer
  • Patent number: 5015644
    Abstract: Certain substituted urea, thiourea, carbamate, and thiocarbamate compounds are potent inhibitors of the enzyme acyl-CoA: cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol, and for lowering blood plasma cholesterol.
    Type: Grant
    Filed: June 1, 1989
    Date of Patent: May 14, 1991
    Assignee: Warner-Lambert Company
    Inventors: Bruce D. Roth, Bharat K. Trivedi
  • Patent number: 5003106
    Abstract: This invention is concerned with ureas and thioureas which may be represented by the formula: ##STR1## wherein X represents at least one substituent selected from the group consisting of (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkenyl, (C.sub.1 -C.sub.4)alkynyl, phenoxy, mercapto, amino, (C.sub.1 -C.sub.4)alkylamino, di-(C.sub.1 -C.sub.4)alkylamino, halo, trihalomethyl, (C.sub.1 -C.sub.4)alkanoyl, benzoyl, (C.sub.1 -C.sub.4)alkanamido, haloacetamido, nitro, cyano, carboxy, (C.sub.1 -C.sub.4)carboalkoxy, carbamoyl, sulfamyl, methylenedioxy, phenyl, orthophenylene, tolyl, benzyl, halobenzyl, methylbenzyl; Y is selected from the group consisting of oxygen and sulfur; R.sub.1 and R.sub.2 are different and are independently selected from the group consisting of (C.sub.4 -C.sub.12)alkyl, (C.sub.4 -C.sub.12)alkenyl, (C.sub.4 -C.sub.12)alkynyl, (C.sub.4 -C.sub.12)cycloalkyalkyl, (C.sub.7 -C.sub.14)aralkyl, and (C.sub.7 -C.sub.
    Type: Grant
    Filed: September 12, 1986
    Date of Patent: March 26, 1991
    Assignee: American Cyanamid Company
    Inventor: Vern G. De Vries
  • Patent number: 4983630
    Abstract: There are provided new 2,2-difluorocyclopropylethane derivatives of general formula I ##STR1## in which A, B and R.sup.1-5 have the meanings given in the description and processes for their preparation. The compounds of the invention can be used as pesticides, especially against insects and mites.
    Type: Grant
    Filed: November 28, 1988
    Date of Patent: January 8, 1991
    Assignee: Schering Aktiengesellschaft
    Inventors: Peter Wegner, Hartmut Joppien, Gunter Homberger, Arnim Kohn
  • Patent number: 4977170
    Abstract: Novel isoprenoidamine compounds (I) which show antiulcer activity are provided.
    Type: Grant
    Filed: May 3, 1989
    Date of Patent: December 11, 1990
    Assignee: Shionogi & Co., Ltd.
    Inventors: Saichi Matsumoto, Masami Doteuchi, Takuji Mizui, Kentaro Hirai
  • Patent number: 4872902
    Abstract: The invention relates to the novel cyclohexanediones of formula I ##STR1## in which R is hydrogen or C.sub.1 -C.sub.6 -alkyl,A is R.sub.2, OR.sub.3 or NR.sub.3 R.sub.4,R.sub.2 is C.sub.1 -C.sub.6 -alkyl that is unsubstituted or is mono-substituted by C.sub.1 -C.sub.4 -alkoxy or mono- or poly-substituted by halogen, or is C.sub.3 -C.sub.6 -cycloalkyl,R.sub.3 is C.sub.1 -C.sub.6 -alkyl or C.sub.3 -C.sub.6 -cycloalkyl, or is phenyl or benzyl each of which is unsubstituted or is mono-, di- or tri-substituted by R.sub.5,R.sub.4 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkoxy or C.sub.3 -C.sub.6 -cycloalkyl,R.sub.3 and R.sub.4 are, in addition, together with the nitrogen atom to which they are bonded, a pyrrolidine, morpholine or piperidine radical,B is one of the radicals ##STR2## m is 0, 1, 2 or 3, R.sub.5 is halogen, nitro, cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkylsulphinyl or C.sub.1 -C.sub.
    Type: Grant
    Filed: February 8, 1988
    Date of Patent: October 10, 1989
    Assignee: Ciba-Geigy Corporation
    Inventor: Hans-Georg Brunner
  • Patent number: 4868210
    Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.
    Type: Grant
    Filed: March 30, 1988
    Date of Patent: September 19, 1989
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 4855478
    Abstract: An N,N-diaryl-N-alkylurea having the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are selected from the group consisting of hydrogen, halogen, cyano, trifluoromethyl, trifluoromethylthio, trifluoromethyl thionyl, trifluoromethane sulfonyl, sulfonamido, substituted phenoxy and substituted pyridyloxy groups wherein the substituent is any one of halogen, cyano, trifluoromethyl, trifluoromethylthio, trifluoromethyl thionyl, trifluoromethane sulfonyl, sulfonamido; andR.sub.5 is selected from the group consisting of alkyl, alkenyl, haloalkyl, haloalkenyl, hydroxyalkyl, hydroxylalkenyl, acetoxyalkyl, acetoxyalkenyl, mercaptoalkyl, and mercaptoalkenyl, wherein the alkyl or alkenyl group in each alkyl- or alkenyl-containing moiety has from 3 to 6 carbon atoms;X is oxygen or sulfur;and agriculturally acceptable salts thereof.Also disclosed is an herbicidal composition and method of treating weeds.
    Type: Grant
    Filed: November 30, 1987
    Date of Patent: August 8, 1989
    Assignee: ICI Americas Inc.
    Inventor: Frank X. Woolard
  • Patent number: 4840967
    Abstract: A compound which is a carbamate or urea derivative of general formula (I) ##STR1## wherein X is hydrogen, halogen or methylthio,Y is oxygen or ##STR2## R is C.sub.1 -C.sub.4 alkyl, R.sub.1 is hydrogen, one or two halogen atoms or trifluoromethyl groups, a methyl group, a methyl group, a cyano group, a nitro group, a methoxycarbonyl group, a methylenedioxy group linked to two adjacent carbon atoms of the benzene ring to which it is attached, or a fused benzo group forming an .alpha.-naphthyl or .beta.-naphthyl group with the benzene ring to which it is attached,R.sub.2 is a linear or branched C.sub.1 -C.sub.8 alkyl or alkenyl group optionally substituted with halogen atoms or a methoxy group, a cyclopropylmethyl group, or a phenyl group optionally substituted with one or two halogen atoms or methyl groups,n is 1 or 2, andm is 2 or 3, or an addition salt thereof with a pharmacologically acceptable acid is pharmacologically active as a calcium antagonist.
    Type: Grant
    Filed: July 7, 1987
    Date of Patent: June 20, 1989
    Assignee: Synthelabo
    Inventors: Nigel Beeley, Gerard Cremer
  • Patent number: 4820871
    Abstract: N,N-Diaryl-ureas of the formulaR.sup.1 --NR.sup.2 --CO--NH--R.sup.3whereinR.sup.1 and R.sup.2 denote aryl andR.sup.3 denotes alkyl, aralkyl or aryl, can be prepared by a process in which a diarylamine of the formulaR.sup.1 --NH--R.sup.2is reacted with an isocyanate of the formulaR.sup.3 --NCOwherein R.sup.1, R.sup.2 and R.sup.34 have the above meaning, in the presence of acid compounds and in the presence or absence of an inert solvent and/or diluent at elevated temperature.
    Type: Grant
    Filed: October 7, 1987
    Date of Patent: April 11, 1989
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfram Kissener, Joachim Franke, Helmut Fiege, Karlfried Wedemeyer
  • Patent number: 4814499
    Abstract: Process for preparing a substituted phenylurea.A suitably substituted aniline, excess urea in a mole ratio of at least 1.1 with respect to the aniline, and a secondary amine are reacted simultaneously in a non-hydroxyl-containing organic solvent at a temperature of 130.degree. to 250.degree. C., with removal of ammonia as it forms.The phenylureas obtained are used as herbicides.
    Type: Grant
    Filed: February 7, 1986
    Date of Patent: March 21, 1989
    Assignee: Rhone-Poulenc Agrochimie
    Inventor: Jean C. Parron
  • Patent number: 4806653
    Abstract: A process of the preparation of iminooxazolidines which comprises (a) reacting a urea alcohol of the formula ##STR1## X, Y, n and R are as defined, with a dehydrating agent to form an intermediate salt compound of the formula ##STR2## wherein X, Y, n and R are as previously defined and X.degree.
    Type: Grant
    Filed: October 17, 1986
    Date of Patent: February 21, 1989
    Assignee: Stauffer Chemical Company
    Inventor: Raymond A. Felix
  • Patent number: 4704401
    Abstract: This invention relates to a method of lowering blood pressure in humans and mammals using 2,6-disubstituted phenyl amidinoureas in which the phenyl ring is additionally substituted by a hydroxy, alkoxy, aralkoxy, alkenyloxy, alkynyloxy, haloacyloxy, or acyloxy group and to novel 2,6-disubstituted phenyl amidinoureas which possess pharmaceutical properties, including blood pressure lowering activity.
    Type: Grant
    Filed: December 6, 1984
    Date of Patent: November 3, 1987
    Assignee: Rorer Pharmaceutical Corporation
    Inventors: William L. Studt, Richard L. Riley, George H. Douglas
  • Patent number: 4656182
    Abstract: Substituted trans-1,2-diaminocyclohexyl amide compounds demonstrating selective opioid receptor binding possess utility as analgesic, diuretic, and psychotherapeutic agents. A method of preparing the compounds, pharmaceutical compositions employing the compounds, and a method of alleviating pain employing the compounds are also disclosed.
    Type: Grant
    Filed: November 13, 1984
    Date of Patent: April 7, 1987
    Assignee: Warner-Lambert Company
    Inventor: David Horwell
  • Patent number: 4597902
    Abstract: N-(arylthioalkyl)-N'-(aminoalkyl)ureas and thioureas and oxidation derivatives having the formula ##STR1## wherein B is thio, sulfinyl or sulfonyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, cycloalkyl, 2-furanyl, phenyl, substituted phenyl or phenyl-loweralkyl and R.sup.3 and R.sup.4 are hydrogen, loweralkyl, phenyl or phenyl-loweralkyl wherein phenyl is optionally substituted, or R.sup.3 and R.sup.4 taken with the adjacent nitrogen form a heterocyclic residue.
    Type: Grant
    Filed: June 20, 1985
    Date of Patent: July 1, 1986
    Assignee: A. H. Robins Company, Incorporated
    Inventors: James R. Shanklin, Jr., Christopher P. Johnson, III
  • Patent number: 4579585
    Abstract: The invention provides novel phenylurea of formula I ##STR1## wherein R.sub.1 is H or CHO,R.sub.2 is H, CH.sub.3 or OCH.sub.3R.sub.3 is a group G.sub.1 of the formula ##STR2## or a group G.sub.2 of the formula CH(CH.sub.3)CH.sub.2 Y in which Y is halogen selected from Cl or F or is CH.sub.3 O andX is H or halogen selected from Cl or Br,the use of these novel compounds as herbicides, compositions for facilitating such use and the preparation of the novel phenylurea.
    Type: Grant
    Filed: March 4, 1985
    Date of Patent: April 1, 1986
    Assignee: Sandoz Ltd.
    Inventor: Karl Seckinger
  • Patent number: 4569689
    Abstract: Aniline derivatives of the formula ##STR1## where R.sup.1 is alkoxy, alkylthio, unsubstituted or substituted cycloalkoxy or the radical --NR.sup.2 R.sup.3, X is --CH.sub.2 --, --CH(OH)-- or --CO--, A is an unsubstituted or substituted alkylene chain, B is unsubstituted or substituted methylene or dimethylene, Z is hydrogen, halogen, alkyl, alkoxy, haloalkyl or haloalkoxy, and n is 1, 2 or 3, are used for controlling undesirable plant growth.
    Type: Grant
    Filed: June 14, 1984
    Date of Patent: February 11, 1986
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulrich Schirmer, Norbert Goetz, Bruno Wuerzer
  • Patent number: 4564640
    Abstract: A method of inducing blood pressure reduction in humans and mammals by administering 2,6-disubstituted phenyl N-alkyl amidinoureas in which the phenyl ring is additionally substituted by a hydroxy, alkoxy, aralkoxy, alkenyloxy, alkynyloxy, acyloxy or halo acyloxy group and a novel class of amidinourea compounds having pharmaceutical uses, including blood pressure lowering activity.
    Type: Grant
    Filed: February 2, 1984
    Date of Patent: January 14, 1986
    Assignee: William H. Rorer, Inc.
    Inventors: William L. Studt, Richard L. Riley, George H. Douglas
  • Patent number: 4564638
    Abstract: Fungicidally active novel benzylurea derivatives of the formula ##STR1## in which R.sup.1 is a halogen atom or a lower alkyl group,X is an oxygen or sulfur atom, andR.sup.2 is an alkyl group, a cycloalkyl group having 5 to 8 carbon atoms, or a phenyl group which may be substituted by at least one member of the class consisting of halogen atoms, lower alkyl groups, lower alkoxy groups and hydroxyl groups.
    Type: Grant
    Filed: June 10, 1983
    Date of Patent: January 14, 1986
    Assignee: Nihon Tokushu Boyaku Seizo K.K.
    Inventors: Yasuo Yamada, Junichi Saito, Tatsuo Tamura, Shinji Sakawa
  • Patent number: 4536341
    Abstract: Dihalo and haloalkyl, haloalkoxy or haloalkylthio-substituted anilines and aniline derivatives, e.g. isocyanates that are useful in the preparation of acyl ureas having insecticidal activity.
    Type: Grant
    Filed: August 3, 1983
    Date of Patent: August 20, 1985
    Assignee: The Dow Chemical Company
    Inventors: Raymond H. Rigterink, Ronald J. Sbragia
  • Patent number: 4519834
    Abstract: The ethynyl-phenylureas of the formula I ##STR1## wherein X is hydrogen, halogen, lower alkyl, lower alkoxy, haloalkyl or nitro, Y is oxygen or sulfur, R.sub.1 is hydrogen, alkyl, alkoxy, alkenyl, phenyl or benzyl, R.sub.2 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl or benzyl, R.sub.1 and R.sub.2 together with the nitrogen atom to which they are bound are also a pyrrolidine, piperidine, morpholino or piperazine ring, R.sub.3 is hydrogen or lower alkyl, and R.sub.4 is hydrogen, alkyl, phenyl, pyridyl, alkenyl, cycloalkyl or cycloalkenyl, are novel substances. They are characterized by strong herbicidal activity.
    Type: Grant
    Filed: July 11, 1983
    Date of Patent: May 28, 1985
    Assignee: Ciba-Geigy Corporation
    Inventor: Henry Szczepanski
  • Patent number: 4518804
    Abstract: Novel N-aroyl N'-phenyl urea compounds having halogen substituents in the 2- and 5-position of the phenyl radical possess exceptional insecticidal activity.
    Type: Grant
    Filed: August 3, 1983
    Date of Patent: May 21, 1985
    Assignee: The Dow Chemical Company
    Inventors: Raymond H. Rigterink, Barat Bisabri-Ershadi
  • Patent number: 4488993
    Abstract: Novel phenylamidinourea compounds and processes for their preparation are described. These compounds have an effective degree of anti-hypertensive properties and exert activities on the cardiovascular system. A method for the treatment of hypertensive disorders is also described.
    Type: Grant
    Filed: October 25, 1982
    Date of Patent: December 18, 1984
    Assignee: William H. Rorer, Inc.
    Inventors: George H. Douglas, Julius Diamond
  • Patent number: 4487779
    Abstract: This invention relates to a method of lowering blood pressure in humans and mammals using 2,6-disubstituted phenyl amidinoureas in which the phenyl ring is additionally substituted by a hydroxy, alkoxy, aralkoxy, alkenyloxy, alkynyloxy, haloacyloxy, or acyloxy group and to novel 2,6-disubstituted phenyl amidinoureas which possess pharmaceutical properties, including blood pressure lowering activity.
    Type: Grant
    Filed: July 6, 1981
    Date of Patent: December 11, 1984
    Assignee: William H. Rorer, Inc.
    Inventors: William L. Studt, Richard L. Riley, George H. Douglas
  • Patent number: 4482739
    Abstract: Imidazolidine derivatives of the formula ##STR1## wherein X is oxygen or imino and R is one of the groups ##STR2## their preparation, use as antiandrogenically or schistosomicidally active agents, and corresponding pharmaceutical preparations, are described.
    Type: Grant
    Filed: May 12, 1983
    Date of Patent: November 13, 1984
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karl Bernauer, Helmut Link, Harro Stohler
  • Patent number: 4474806
    Abstract: Sulfonyl or carbonyl derivatives of inositols are found to be effective phospholipase C inhibitors and thereby potent anti-inflammatory and analgesic agents. These inositol derivatives are prepared by condensation of a protected inositol with a substituted sulfonic or carboxylic acid derivative followed by removal of protecting groups.
    Type: Grant
    Filed: May 10, 1982
    Date of Patent: October 2, 1984
    Assignee: Merck & Co., Inc.
    Inventors: Thomas R. Beattie, Shu S. Yang
  • Patent number: 4474707
    Abstract: Compounds of the formula: ##STR1## wherein: Y is 2,6-dimethylphenyl, 2,5-dimethylphenyl, 5-bromo-2-methylphenyl, or 5-chloro-2-methylphenyl; andX is propenyl, propynyl, or cyclopropyl; or a non-toxic, pharmaceutically acceptable acid addition salt thereof; possess anti-arrhythmic activity.
    Type: Grant
    Filed: August 26, 1981
    Date of Patent: October 2, 1984
    Assignee: American Home Products Corporation
    Inventors: Theodore S. Sulkowski, James L. Bergey, Albert A. Mascitti
  • Patent number: 4473579
    Abstract: Tetrasubstituted urea and thiourea compounds useful as antiatherosclerotic agents, compositions thereof and processes for their preparation.
    Type: Grant
    Filed: January 26, 1982
    Date of Patent: September 25, 1984
    Assignee: American Cyanamid Company
    Inventors: Vern G. Devries, Ransom B. Conrow
  • Patent number: 4454107
    Abstract: This invention relates to novel derivatives of imino diacetic acid of the formula: ##STR1## wherein R.sup.1 is selected from the group consisting of: ##STR2## wherein X is halo (chloro, bromo or iodo) and R.sup.2 is lower alkyl of from 1-5 carbon atoms. It also relates to a novel diagnostic kit for hepatobiliary imaging comprising ingredients employed in the intravenous injection of a complex of technetium 99m, and an imino diacetic acid of the above formula. It also relates to a process for preparing said compounds by reaction of nitrilotriacetic acid anhydride and an amine of the formula R.sup.1 NH.sub.2 wherein R.sup.1 is as defined hereinabove.
    Type: Grant
    Filed: August 30, 1982
    Date of Patent: June 12, 1984
    Assignee: Merck & Co., Inc.
    Inventor: Richard E. Rolleston
  • Patent number: 4440949
    Abstract: A new class of chemical compounds and their process of preparation is described. These compounds have valuable properties as anti-secretory, anti-spasmodic, anti-ulcerogenic and anti-diarrheal agents.
    Type: Grant
    Filed: December 30, 1980
    Date of Patent: April 3, 1984
    Assignee: William H. Rorer, Inc.
    Inventors: George H. Douglas, William L. Studt, Stuart A. Dodson
  • Patent number: 4435567
    Abstract: A process for the preparation of substituted urea derivatives, and compositions and concentrates for the same purpose are disclosed. According to the process the substituted urea derivatives of formula (I) ##STR1## wherein R is hydrogen, alkyl, aryl, cycloalkyl or aralkyl, R.sup.1 and R.sup.2 are hydrogen, alkyl, alkenyl, alkinyl, alkoxy, oxyalkyl, cycloalkyl, aralkyl, alkoxycarbonylalkyl, aryl or heteroaryl, or R.sup.1 and R.sup.
    Type: Grant
    Filed: December 28, 1981
    Date of Patent: March 6, 1984
    Assignee: Chinoin Gyogyszer es Vesgyeszeti Termekek Gyara R. T.
    Inventors: Gyorgy Lugosi, Antal Simay, Janos Bodnar, Laszlo Simandi, Eva Somfai
  • Patent number: 4430262
    Abstract: Isocyanates and derivatives thereof are prepared by oxidative conversion of compounds having at least one group ##STR1## wherein X represents OY or ##STR2## wherein Y is H, a metal ion or group NR.sup.3 R.sup.4 R.sup.5 R.sup.6 wherein each of R.sup.3, R.sup.4, R.sup.5 and R.sup.6 which may be the same or different, is H, alkyl or (substituted) (alk)aryl and Z is a (substituted) alkyl or aryl group. Phenyl isocyanate and derivatives thereof are preferably prepared electrochemically from the corresponding oxamides and oxanilides.
    Type: Grant
    Filed: March 11, 1982
    Date of Patent: February 7, 1984
    Assignee: Shell Oil Company
    Inventors: Rainer Engels, Jan H. H. Meurs
  • Patent number: 4422871
    Abstract: Aralkylphenylureas of the formula ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen, alkoxy or unsubstituted or substituted alkyl, cycloalkyl, alkenyl or alkynyl, or R.sup.1 and R.sup.2 together are unsubstituted or substituted alkylene which may or may not be interrupted by oxygen or sulfur, Y is hydrogen, alkyl, halogen, alkoxy or haloalkyl, A is unsubstituted or substituted alkylene, Z is hydrogen, alkyl, haloalkyl, alkoxyalkyl, cycloalkyl, aralkyl, aryl, aryloxy, halogen, a C.sub.4 H.sub.4 chain which is fused to the benzene ring to give a substituted or unsubstituted naphthyl ring, alkoxy, haloalkoxy, alkylthio, thiocyanato, cyano, ##STR2## R' and R" being hydrogen, alkyl, alkoxy, alkylthio, cycloalkyl or unsubstituted or substituted phenyl and n is 1, 2, 3 or 4, and herbicides containing these ureas.
    Type: Grant
    Filed: May 7, 1982
    Date of Patent: December 27, 1983
    Assignee: BASF Aktiengesellschaft
    Inventors: Ulrich Schirmer, Wolfgang Rohr, Bruno Wuerzer
  • Patent number: 4418209
    Abstract: This invention describes a new class of 1-amidino-3-phenylthiourea and N'-phenylamidinothiourea compounds wherein the phenyl group is ortho substituted, and processes for their preparation. The phenylamidinothiourea compounds may be incorporated into pharmaceutical preparations which are useful for producing anti-ulcerogenic, antisecretory, antispasmodic, antihypertensive, anti-arrhythmic, anesthetic, antidiarrheal and antiparasitic action.
    Type: Grant
    Filed: December 21, 1981
    Date of Patent: November 29, 1983
    Assignee: William H. Rorer, Inc.
    Inventors: George H. Douglas, Julius Diamond, William L. Studt, Stuart A. Dodson
  • Patent number: 4410697
    Abstract: The invention relates to a new method for the preparation of N-aryl-N'-(mono- or disubstituted)-urea derivatives having the general formula (I), ##STR1## wherein Aryl is an optionally substituted phenyl group, andR.sup.1 and R.sup.2 each stand for an optionally substituted alkyl, cycloalkyl, alkoxy or phenyl group, orR.sup.1 and R.sup.2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocyclic group which may contain a further hetero atom, orone of R.sup.1 and R.sup.2 may also stand for hydrogen,with the proviso that if one of R.sup.1 and R.sup.2 is an optionally substituted phenyl group, the other may represent only hydrogen atom or an optionally substituted alkyl or alkoxy group,by reacting a carbamate of the general formula (II) with an amine of the general formula (III),R.sup.1 R.sup.2 N--CO--X (II)Aryl--NH.sub.2 (III)or a carbamate of the general formula (IV) with an amine of the general formula (V),Aryl--NH--CO--X (IV)R.sup.1 R.sup.2 NH (V)wherein R.sup.1, R.sup.
    Type: Grant
    Filed: August 28, 1981
    Date of Patent: October 18, 1983
    Assignee: Reanal Finomvegyszergyar
    Inventors: Sandor Torok, Lajos Voroshazy, Peter Galambos, Ivan Daroczi, Zoltan Ormenyi
  • Patent number: 4406691
    Abstract: The ethynyl-phenylureas of the formula I ##STR1## wherein X is hydrogen, halogen, lower alkyl, lower alkoxy, haloalkyl or nitro, Y is oxygen or sulfur, R.sub.1 is hydrogen, alkyl, alkoxy, alkenyl, phenyl or benzyl, R.sub.2 is hydrogen, alkyl, cycloalkyl, alkenyl, alkynyl or benzyl, R.sub.1 and R.sub.2 together with the nitrogen atom to which they are bound are also a pyrrolidine, piperidine, morpholino or piperazine ring, R.sub.3 is hydrogen or lower alkyl, and R.sub.4 is hydrogen, alkyl, phenyl, pyridyl, alkenyl, cycloalkyl or cycloalkenyl, are novel substances. They are characterized by strong herbicidal activity.
    Type: Grant
    Filed: December 9, 1980
    Date of Patent: September 27, 1983
    Assignee: Ciba-Geigy Corporation
    Inventor: Henry Szczepanski
  • Patent number: 4405644
    Abstract: The invention relates primarily to pharmaceutical compositions and medicaments containing a compound of Formula (I), infra as the active ingredient. Also included in the invention are methods for combatting lipometabolic illnesses by administration of an active compound of the invention alone, in combination with a diluent or in the form of a medicament.
    Type: Grant
    Filed: December 17, 1981
    Date of Patent: September 20, 1983
    Assignee: Bayer Aktiengesellschaft
    Inventors: Hans-Joachim Kabbe, Erich Klauke, Hans P. Krause, Mithat Mardin, Rudiger Sitt
  • Patent number: 4399076
    Abstract: 2-Vinyl- and 2-ethylcyclopropanes having an aryl group and a nitrogen-containing radical substituted at the 1-position on the ring are provided. The novel 1,1-disubstituted 2-vinylcyclopropane and 2-ethylcyclopropane compounds of this invention have utility in herbicidal applications and are useful reactants. The 2-vinylcyclopropane derivatives are useful monomers for anionic and radical polymerizations.
    Type: Grant
    Filed: February 22, 1982
    Date of Patent: August 16, 1983
    Assignee: National Distillers and Chemical Corporation
    Inventors: Richard G. Fayter, Jr., Allen L. Hall
  • Patent number: 4358606
    Abstract: Novel esters of phenylalkyloxy- or phenylalkylthioacylamino acids and pyridylalkyloxy- or pyridylalkylthioacylamino acids, synthesis thereof, intermediates therefor, and the use of said esters for the control of weeds.
    Type: Grant
    Filed: June 19, 1981
    Date of Patent: November 9, 1982
    Assignee: Zoecon Corporation
    Inventors: Shy-Fuh Lee, Clive A. Henrick
  • Patent number: 4353842
    Abstract: A novel method of treating gastrointestinal, spasmolytic and ulcerogenic disorders by the administration of amidinoureas is disclosed.
    Type: Grant
    Filed: February 5, 1980
    Date of Patent: October 12, 1982
    Assignee: William H. Rorer, Inc.
    Inventors: Julius Diamond, George H. Douglas