Benzene Ring Containing Patents (Class 514/585)
  • Patent number: 5449690
    Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are as defined in the specification, and medicinal products containing the same which are useful in treating or in preventing a disorder of the melatoninergic system.
    Type: Grant
    Filed: December 20, 1994
    Date of Patent: September 12, 1995
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Said Yous, Patrick DePreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
  • Patent number: 5441984
    Abstract: The present invention provides novel urea, thiourea and guanidine derivatives, pharmaceutical formulations thereof and a method of using same to prevent diabetic complications.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: August 15, 1995
    Assignee: Eli Lilly and Company
    Inventors: William F. Heath, Jr., Jill A. Panetta, John K. Shadle
  • Patent number: 5395853
    Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, orPh(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, orR.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, orR.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; ##STR2## Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.
    Type: Grant
    Filed: November 24, 1993
    Date of Patent: March 7, 1995
    Assignee: Burroughs Wellcome Co.
    Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
  • Patent number: 5389683
    Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are as defined in the specification, andmedicinal products containing the same which are in treating or in preventing a disorder of the melatoninergic system.
    Type: Grant
    Filed: August 14, 1992
    Date of Patent: February 14, 1995
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Said Yous, Patrick Depreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
  • Patent number: 5385944
    Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are defined in the specification, andmedicinal products containing the same which are useful in treating or in preventing a disorder of the melatoninergic system.
    Type: Grant
    Filed: April 27, 1993
    Date of Patent: January 31, 1995
    Assignee: Adir et Compagnie
    Inventors: Daniel Lesieur, Said Yous, Patrick Depreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
  • Patent number: 5290814
    Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, or Ph(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, or R.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, or R.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; X is ##STR2## where A is halogen; Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.
    Type: Grant
    Filed: November 5, 1992
    Date of Patent: March 1, 1994
    Assignee: Burroughs Wellcome Co.
    Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
  • Patent number: 5264441
    Abstract: The invention provides new ureas and thioureas derivatives of general formula (I) ##STR1## and pharmaceutically acceptable salts thereof, which are useful as therapeutic agents such as for the prevention of coronary heart disease and as antidyslipidaemic agents.
    Type: Grant
    Filed: February 18, 1992
    Date of Patent: November 23, 1993
    Assignee: Farmitalia Carlo Erba S.r.l.
    Inventors: Paolo Cozzi, Danielle Fancelli, Dino Severino, Augusto Chiari, Giancarlo Ghiselli
  • Patent number: 5187197
    Abstract: Novel substituted phenyl-thioureas, -isothioureas and -carbodiimides of formula I ##STR1## in which R.sub.1 is C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkyl mono- or poly-substituted by halogen and/or by C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl mono- or poly-substituted by C.sub.1 -C.sub.3 alkyl, or is C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 C.sub.4 alkyl; each of R.sub.2 and R.sub.3 is C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl or C.sub.5 -C.sub.6 cycloalkenyl; each of R.sub.4 and R.sub.5 is hydrogen or C.sub.1 -C.sub.4 alkyl; each R.sub.6 is halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 C.sub.4 haloalkoxy or a --CH.dbd.CH, --CH.sub.2 or --CH.sub.2 bridge in the 2,3-or 3,4-position; n is 0, 1 or 2; Z is --NH--CS--NH--, --N.dbd.C(SR.sub.7) --NH--or --N.dbd.C.dbd.N--, and R.sub.7 is C.sub.1 -C.sub.10 alkyl or C.sub.3 -C.sub.
    Type: Grant
    Filed: August 20, 1990
    Date of Patent: February 16, 1993
    Assignee: Ciba-Geigy Corporation
    Inventor: Josef Ehrenfreund
  • Patent number: 5153227
    Abstract: The invention concerns novel pharmaceutical compositions for use in the treatment of certain complications of diabetes and galactosemia and which contain a nitromethane derivative (or its non-toxic salt) as active ingredient. The nitromethane derivatives are inhibitors of the enzyme aldose reductase. Many of the inhibitors are novel and are provided, together with processes for their manufacture and use, as further features of the invention.
    Type: Grant
    Filed: February 6, 1989
    Date of Patent: October 6, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston
  • Patent number: 5116848
    Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxphenyl-N'-diarylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis with urea and thiourea compounds.
    Type: Grant
    Filed: March 30, 1988
    Date of Patent: May 26, 1992
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • 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: 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: 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: 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: 5006539
    Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1]heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.
    Type: Grant
    Filed: March 6, 1989
    Date of Patent: April 9, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • 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: 4920135
    Abstract: Certain organic compounds derived from urea or thiourea having insecticidal activity and methods of their preparation are disclosed. The compounds according to the invention have been found to interfere with the mechanism of metamorphoses which occurs in insects. Hence, the substances according to the invention are specifically active against insects. Owing to this specificity and because of the absence of phytotoxicity effects, the compounds of this invention are of prime importance.
    Type: Grant
    Filed: February 7, 1989
    Date of Patent: April 24, 1990
    Assignee: Duphar International Research B.V.
    Inventors: Kobus Wellinga, Rudolf Wulder
  • 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: 4857556
    Abstract: Substituted benzylcycloalkenylurea derivatives of the formula (I) ##STR1## wherein X represents a halogen atom or a lower alkyl group, Y represents an oxygen atom or a sulfur atom,R.sup.1 represents a cycloalkenyl group andR.sup.2 represents a lower alkyl group, a cycloalkyl group, a benzyl group or a phenyl group optionally substituted by 1 to 5 substituents selected from the group consisting of a hydroxyl group or a lower alkoxy groupand their use as fungicides. They can be synthesized, for example, by reacting of a substituted benzyl-cycloalkenylamine with an isocyanate or by reacting of a carbamoyl halide with an amine. The starting material, the substituted benzyl-cycloalkenyl amines, are also new.
    Type: Grant
    Filed: December 8, 1987
    Date of Patent: August 15, 1989
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Yasuo Yamada, Junichi Saito, Tatsuo Tamura, Shinji Sakawa
  • Patent number: 4752615
    Abstract: A compound of the formula: ##STR1## useful as a fungicidal agent against phytopathogenic fungi, particularly their strains resistant to benzimidazole, thiophanate and/or cyclic imide fungicides.
    Type: Grant
    Filed: November 13, 1986
    Date of Patent: June 21, 1988
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Oguri, Shigeo Yamamoto, Katsuzo Kamoshita
  • Patent number: 4731385
    Abstract: An insecticidal and fungicidal composition comprising (1) An insecticidally effective amount of a nitromethylene derivative of the formula ##STR1## in which X is a lower alkyl group, a lower alkoxy group, or a halogen atom,n is 0, 1 or 2 andm is 2 or 3,and a fungicidally effective amount of at least one fungicide selected from the group consisting of(2) O-ethyl S,S-diphenyl phosphorodithioate,(3) 4,5,6,7-tetrachlorophthalide,(4) 1-(4-chlorobenzyl)-1-cyclopentyl-3-phenylurea,(5) Validamycin A, 3'-iso-propoxy-2-methylbenzenilide, o-trifluoromethyl-m'-isopropoxybenzoylanilide or 6-(3,5-dichloro-4-methylphenyl-3(2H)pyridazinone, and(6) di-isopropyl-1,3-dithiolan-2-ylidenemalonate, 5-methyl-1,2,4-triazo[3,4-b]-benzothiazole, 3-allyloxy-1,2-benzisothiazole 1,1-dioxide, and 1,2,5,6-tetrahydro-4H-pyrrolo-[3,2,1-i,j]quinolin-4-one, [5-amino-2-methyl-6-(2,3,4,5,6-pentahydroxycyclohexyloxy)tetrahydropyran-3 -yl]amino-.alpha.-iminoacetic acid or S-benzyl diisopropylphosphorothiolate.
    Type: Grant
    Filed: October 21, 1986
    Date of Patent: March 15, 1988
    Assignee: Nihon Tokushu Noyaku Seizo K.K.
    Inventors: Shinichi Tsuboi, Shoko Sasaki, Yumi Hattori, Yoshio Kurahashi, Shinji Sakawa, Toshihito Kondo
  • Patent number: 4628061
    Abstract: Novel compounds have a formula (I) ##STR1## wherein ##STR2## represents a bicyclo [2,2,1] hept-2Z-ene, bicyclo [2,2,1] heptane, 7-oxa-bicyclo [2,2,1] hept-2Z-ene, 7-oxa-bicyclo [2,2,1] heptane, bicyclo [2,2,2] oct-2Z-ene or bicyclo [2,2,2] octane substituted at the 5-position by the group R.sup.1 and at the 6-position by the group ANR.sup.2 R, a 6,6-dimethyl-bicyclo [3,1,1] heptane substituted at the 2-position by the group R.sup.1 and at the 3-position by the group ANR.sup.2 R or at the 2-position by the group ANR.sup.2 R and at the 3-position by the group R.sup.1, a cyclohex-1-ene or cyclohexane substituted at the 4-position by the group R.sup.1 and at the 5-position by the group ANR.sup.2 R or a 1-hydroxycyclopentane substituted at the 2-position by the group R.sup.1 and at the 2-position by the group ANR.sup.2 R, R.sup.
    Type: Grant
    Filed: August 23, 1983
    Date of Patent: December 9, 1986
    Assignee: National Research Development Corporation
    Inventors: Robert L. Jones, Norman H. Wilson
  • Patent number: 4623662
    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)cycloalkylalkyl, (C.sub.7 -C.sub.14)aralkyl, and (C.sub.7 -C.sub.
    Type: Grant
    Filed: May 23, 1985
    Date of Patent: November 18, 1986
    Assignee: American Cyanamid Company
    Inventor: Vern G. De Vries
  • Patent number: 4607044
    Abstract: Certain organic compounds derived from urea or thiourea having insectical activity and methods of their preparation are disclosed. The compounds according to the invention have been found to interfere with the mechanism of metamorphoses which occurs in insects. Hence the substances according to the invention are specifically active against insects. Owing to this specificity and because of the absence of phytotoxicity effects, the compounds of this invention are of prime importance.
    Type: Grant
    Filed: October 30, 1984
    Date of Patent: August 19, 1986
    Assignee: Duphar International Research B.V.
    Inventors: Kobus Wellinga, Rudolf Mulder
  • 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