Benzene Ring Containing Patents (Class 514/585)
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Patent number: 5449689Abstract: 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 useful in treating or in preventing a disorder of the melatoninergic system.Type: GrantFiled: December 20, 1994Date of Patent: September 12, 1995Assignee: Adir et CompagnieInventors: Daniel Lesieur, Said Yous, Patrick Depreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
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Patent number: 5441984Abstract: The present invention provides novel urea, thiourea and guanidine derivatives, pharmaceutical formulations thereof and a method of using same to prevent diabetic complications.Type: GrantFiled: November 14, 1994Date of Patent: August 15, 1995Assignee: Eli Lilly and CompanyInventors: William F. Heath, Jr., Jill A. Panetta, John K. Shadle
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Patent number: 5395853Abstract: 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: GrantFiled: November 24, 1993Date of Patent: March 7, 1995Assignee: Burroughs Wellcome Co.Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
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Patent number: 5389683Abstract: 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: GrantFiled: August 14, 1992Date of Patent: February 14, 1995Assignee: Adir et CompagnieInventors: Daniel Lesieur, Said Yous, Patrick Depreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
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Patent number: 5385944Abstract: 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: GrantFiled: April 27, 1993Date of Patent: January 31, 1995Assignee: Adir et CompagnieInventors: Daniel Lesieur, Said Yous, Patrick Depreux, Gerard Adam, Pierre Renard, Bruno Pfeiffer, Beatrice Guardiola-Lemaitre
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Patent number: 5290814Abstract: 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: GrantFiled: November 5, 1992Date of Patent: March 1, 1994Assignee: Burroughs Wellcome Co.Inventors: William P. Jackson, Clifford J. Harris, Richard J. Arrowsmith, John G. Dann, Kevin J. O'Connor, Robert F. G. Booth
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Patent number: 5264441Abstract: 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: GrantFiled: February 18, 1992Date of Patent: November 23, 1993Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Paolo Cozzi, Danielle Fancelli, Dino Severino, Augusto Chiari, Giancarlo Ghiselli
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Patent number: 5187197Abstract: 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: GrantFiled: August 20, 1990Date of Patent: February 16, 1993Assignee: Ciba-Geigy CorporationInventor: Josef Ehrenfreund
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Patent number: 5153227Abstract: 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: GrantFiled: February 6, 1989Date of Patent: October 6, 1992Assignee: Imperial Chemical Industries PLCInventors: Steven P. Brown, Anthony L. Cooper, Jethro L. Longridge, Jeffrey J. Morris, John Preston
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Patent number: 5116848Abstract: 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: GrantFiled: March 30, 1988Date of Patent: May 26, 1992Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 5106873Abstract: 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: GrantFiled: June 26, 1990Date of Patent: April 21, 1992Assignee: Warner-Lambert CompanyInventors: Patrick M. O'Brien, Drago R. Sliskovic, Michael W. Wilson
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Patent number: 5091419Abstract: 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: GrantFiled: October 2, 1990Date of Patent: February 25, 1992Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Noriki Ito, Tomoyuki Yasunaga, Yuichi Iizumi, Tomio Araki
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Patent number: 5063247Abstract: 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: GrantFiled: June 13, 1990Date of Patent: November 5, 1991Assignee: Mitsubishi Kasei CorporationInventors: Tetsuo Sekiya, Shinya Inoue, Masao Taniguchi, Kohei Umezu, Kazuo Suzuki
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Patent number: 5015644Abstract: 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: GrantFiled: June 1, 1989Date of Patent: May 14, 1991Assignee: Warner-Lambert CompanyInventors: Bruce D. Roth, Bharat K. Trivedi
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Patent number: 5006539Abstract: 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: GrantFiled: March 6, 1989Date of Patent: April 9, 1991Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 4977170Abstract: Novel isoprenoidamine compounds (I) which show antiulcer activity are provided.Type: GrantFiled: May 3, 1989Date of Patent: December 11, 1990Assignee: Shionogi & Co., Ltd.Inventors: Saichi Matsumoto, Masami Doteuchi, Takuji Mizui, Kentaro Hirai
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Patent number: 4920135Abstract: 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: GrantFiled: February 7, 1989Date of Patent: April 24, 1990Assignee: Duphar International Research B.V.Inventors: Kobus Wellinga, Rudolf Wulder
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Patent number: 4868210Abstract: 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: GrantFiled: March 30, 1988Date of Patent: September 19, 1989Assignee: Warner-Lambert CompanyInventor: Bharat K. Trivedi
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Patent number: 4857556Abstract: 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: GrantFiled: December 8, 1987Date of Patent: August 15, 1989Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Yasuo Yamada, Junichi Saito, Tatsuo Tamura, Shinji Sakawa
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Patent number: 4752615Abstract: 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: GrantFiled: November 13, 1986Date of Patent: June 21, 1988Assignee: Sumitomo Chemical Company, LimitedInventors: Junya Takahashi, Toshiro Kato, Hiroshi Noguchi, Yukio Oguri, Shigeo Yamamoto, Katsuzo Kamoshita
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Patent number: 4731385Abstract: 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: GrantFiled: October 21, 1986Date of Patent: March 15, 1988Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Shinichi Tsuboi, Shoko Sasaki, Yumi Hattori, Yoshio Kurahashi, Shinji Sakawa, Toshihito Kondo
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Patent number: 4628061Abstract: 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: GrantFiled: August 23, 1983Date of Patent: December 9, 1986Assignee: National Research Development CorporationInventors: Robert L. Jones, Norman H. Wilson
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Patent number: 4623662Abstract: 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: GrantFiled: May 23, 1985Date of Patent: November 18, 1986Assignee: American Cyanamid CompanyInventor: Vern G. De Vries
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Patent number: 4607044Abstract: 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: GrantFiled: October 30, 1984Date of Patent: August 19, 1986Assignee: Duphar International Research B.V.Inventors: Kobus Wellinga, Rudolf Mulder
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Patent number: 4564638Abstract: 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: GrantFiled: June 10, 1983Date of Patent: January 14, 1986Assignee: Nihon Tokushu Boyaku Seizo K.K.Inventors: Yasuo Yamada, Junichi Saito, Tatsuo Tamura, Shinji Sakawa