C=o Bonded Directly To Benzene Ring Patents (Class 514/685)
  • Patent number: 5776439
    Abstract: Cosmetic compositions containing sunscreens against sun radiation ranging from 280 to 380 nm, and their use for the protection of the skin from UV radiation. The sunscreens comprise, with respect to the weight of the composition:a) from 1 to 10% of one or more compounds of formula (I) ##STR1## wherein Q is hydrogen or C.sub.1 -C.sub.4 alkoxy and G is C.sub.1 -C.sub.8 alkyl; andb) from 0.5 to 10% of one or more compounds of formula (II): ##STR2## wherein R.sub.1 is C.sub.1 -C.sub.8 alkyl and R.sub.2 is hydrogen or an SO.sub.3 M group wherein M is hydrogen, an alkali metal, or a mono- or polyalkyl-substituted ammonium group;with the condition that the weight ratio between the compounds of formula (II) and the compounds of formula (I) is at least 0.5.
    Type: Grant
    Filed: November 29, 1996
    Date of Patent: July 7, 1998
    Assignee: 3V Inc.
    Inventors: Giuseppe Raspanti, Alverio Malpede
  • Patent number: 5760092
    Abstract: Disclosed are allocolchinones, which are anti-mitotic agents. Allocolchinones bind to tubulin reversibly and are more effective at inhibiting microtubule formation than colchicine. 7-Acetamido-allocolchinone inhibits the growth of a number of tumor cell lines at concentrations about 100 times lower than colchicine. Also disclosed is a method of treating an individual with cancer by administering a composition which comprises a therapeutically effective amount of an allocolchinone which inhibits microtubule assembly. Administering a therapeutically effective amount of a composition which comprises an allocolchinone which inhibits microtubule assembly can also be used for treating inflammatory diseases, multiple sclerosis, primary biliary cirrhosis, Alzheimer's Disease and Behcet's Disease.
    Type: Grant
    Filed: March 11, 1996
    Date of Patent: June 2, 1998
    Assignee: Brandeis University
    Inventors: Serge M. Timasheff, Marina J. Gorbunoff, Bernardo Perez-Ramirez
  • Patent number: 5739170
    Abstract: Compositions and methods are disclosed for treating a patient infected with a metazoan parasite by inhibiting the enzymatic action of the metazoan parasite protease, wherein there is employed at least one compound of formula IA--X--Bwherein A is a substituted or unsubstituted homoaromatic ring system comprising one to three rings which bind to at least one of the S2, S1 and S1' subsites; B is a substituted or unsubstituted homoaromatic ring system comprising one to three rings which bind to at least one of the S1', S1 and S2 subsites; and X is --C.dbd.C--C(.dbd.O)--. These compositions and methods have particular utility in the treatment of schistosomiasis, malaria, and other infectious diseases.
    Type: Grant
    Filed: March 30, 1995
    Date of Patent: April 14, 1998
    Assignee: The Regents of the University of California
    Inventors: Fred E. Cohen, James H. McKerrow, George L. Kenyon, Zhe Li, Xiaowu Chen, Baoqing Gong, Rongshi Li
  • Patent number: 5733532
    Abstract: Cosmetic compositions containing sunscreens against sun radiation ranging from 280 to 380 nm, and their use for the protection of the skin from UV radiation. The sunscreens comprise, with respect to the weight of the composition:a) from 1 to 10% of one or more derivatives of formula (I) ##STR1## wherein Q is hydrogen or C.sub.1 --C.sub.4 alkoxy and G is C.sub.1 --C.sub.8 alkyl;b) from 0.5 to 10% of one or more derivatives of formula (II): ##STR2## wherein R.sub.1 is hydrogen or C.sub.1 --C.sub.8 alkyl and R.sub.2 is hydrogen or an SO.sub.3 M group in which M is hydrogen, an alkali metal, or an alkyl ammonium group; andc) from 1 to 10% of one or more derivatives of formula (III) ##STR3## wherein R.sub.3 is C.sub.1 --C.sub.8 alkyl and R.sub.4 has independently the same meanings as R.sub.3 or is hydrogen or is an alkali metal;with the condition that the weight ratio between the compounds of formula (II) and the compounds of formula (I) is at least 0.5.
    Type: Grant
    Filed: November 29, 1996
    Date of Patent: March 31, 1998
    Assignee: 3V Inc.
    Inventors: Giuseppe Raspanti, Alverio Malpede
  • Patent number: 5679696
    Abstract: This invention is directed to the pharmaceutical use of phenyl compounds, which are linked to an aryl moiety by various linkages, for inhibiting tumor necrosis factor. The invention is also directed to the compounds, their preparation and pharmaceutical compositions containing these compounds. Furthermore, this invention is directed to the pharmaceutical use of the compounds for inhibiting cyclic AMP phosphodiesterase.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: October 21, 1997
    Assignee: Rhone-Poulenc Rorer Limited
    Inventors: Garry Fenton, Andrew David Morley, Malcolm Norman Palfreyman, Andrew James Ratcliffe, Brian William Sharp, Keith Alfred James Stuttle, Sukanthini Thurairatnam, Bernard Yvon Jack Vacher
  • Patent number: 5679716
    Abstract: A therapeutic agent for osteoporosis comprising as an active ingredient xanthohumol. Xanthohumol obtained from hop extracts has a bone resorption inhibiting activity and is useful as a therapeutic agent for osteoporosis.
    Type: Grant
    Filed: September 27, 1996
    Date of Patent: October 21, 1997
    Assignee: Hoechst Japan Limited
    Inventors: Hiroyasu Tobe, Kazuyuki Kitamura, Osamu Komiyama
  • Patent number: 5668156
    Abstract: Di(aromatic) compounds corresponding to the following formula: ##STR1## in which: Ar represents either ##STR2## n=1 or 2 or: ##STR3## X represents a divalent radical, Z represents O, S or a divalent radical, and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent a hydrogen atom or various organic radicals, and the salts of the compounds of formula (I) when R.sub.1 is a carboxylic acid function.Use in human and veterinary medicine and in cosmetics.
    Type: Grant
    Filed: April 28, 1995
    Date of Patent: September 16, 1997
    Assignee: Centre International de Recherches Dermatologiques Galderma (Cird Galderma)
    Inventors: Jean-Michel Bernardon, William Robert Pilgrim
  • Patent number: 5624663
    Abstract: A photostable cosmetic filter composition for protecting human skin against UV radiation at wavelengths between 280 and 380 nm comprises, in a cosmetically acceptable support medium containing at least one oily phase, 1 to 3% by weight of a dibenzoylmethane derivative and at least 1% by weight of a substituted dialkylbenzalmalonate having formula I: ##STR1## R.sub.1 and R.sub.3 may be identical or different and represent H or a straight- or branched-chain C.sub.1 -C.sub.8 alkoxy radical.R.sub.2 and R.sub.4 represent a straight- or branched-chain C.sub.1 -C.sub.8 alkyl radical.The molar ratio of compound (I) to the dibenzoylmethane derivative is greater than or equal to 0.6.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: April 29, 1997
    Assignee: L'Oreal
    Inventors: Andre Deflandre, Serge Forestier, Gerard Lang, Herve Richard, Madeleine Leduc
  • Patent number: 5605680
    Abstract: The invention relates to a photostable screening cosmetic composition for protecting human skin against UV rays, comprising, in a cosmetically acceptable substrate containing at least one fatty phase, 1 to 3% by weight of 4-(1,1-dimethylethyl)-4'-methoxydibenzoylmethane and at least 4.5% by weight of p-methylbenzylidenecamphor, the weight ratio of p-methylbenzylidenecamphor to 4-(1,1-dimethyl-ethyl)-4'-methoxydibenzoylmethane being higher than or equal to 3.It also relates to a process for protecting the skin against UV radiation and to a process for stabilizing 4-(1,1-dimethylethyl)-4'-methoxydibenzoylmethane against UV radiation.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: February 25, 1997
    Assignee: L'Oreal
    Inventors: Andre Deflandre, Serge Forestier, Gerard Lang, Jean F. Grollier, Jean Cotteret
  • Patent number: 5604212
    Abstract: The present invention relates to a method for regulating wrinkles and/or atrophy in mammalian skin comprising treating the skin with a safe and effective amount of salicylic acid and/or additional active component.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: February 18, 1997
    Assignee: Richardson-Vicks, Inc.
    Inventor: Roy L. Blank
  • Patent number: 5587150
    Abstract: A photostable cosmetic screening composition and process for protection of the human epidermis against UV rays of wavelengths between 280 and 380 nm, the composition having, in a cosmetically acceptable vehicle containing at least one fatty phase, 1 to 5% by weight of a dibenzoylmethane derivative and at least 1% by weight of an alkyl .beta.-.beta.-diphenylacrylate or .alpha.-cyano-.beta.-.beta.-diphenylacrylate of formula (I), the mole ratio of the compound of formula (I) to the dibenzoylmethane derivative being not less than 0.8.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: December 24, 1996
    Assignee: L'Oreal
    Inventors: Andre Deflandre, Michel Dubois, Serge Forestier, Herve Richard
  • Patent number: 5576354
    Abstract: A photostable cosmetic screening composition and process for protection of the human epidermis against UV rays of wavelengths between 280 and 380 nm, the composition having, in a cosmetically acceptable vehicle containing at least one fatty phase, 1 to 5% by weight of a dibenzoylmethane derivative and at least 1% by weight of an alkyl .beta.-.beta.-diphenylacrylate or .alpha.-cyano-.beta.-.beta.-diphenylacrylate of formula (I), the mole ratio of the compound of formula (I) to the dibenzoylmethane derivative being not less than 0.8.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: November 19, 1996
    Assignee: L'Oreal
    Inventors: Andre Deflandre, Michel DuBois, Serge Forestier, Herve Richard
  • Patent number: 5545399
    Abstract: A composition for topical application to the skin in order to promote the repair of photo-damaged or aged skin and/or to reduce or prevent damaging effects of ultra-violet light on skin and/or to lighten the skin comprising a hydrocalchone of general structure: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3, which may be the same or different, represent H, --OH, --OR or --COR (where R is a C.sub.1-20 alkyl group);R.sub.4, R.sub.5, R.sub.6 and R.sub.7, which may be the same or different, represent H or --COR (where R is as herein before defined).Optional additional ingredients include sunscreens and other skin lightening skin lightening agents, particularly retinol or derivatives thereof.
    Type: Grant
    Filed: October 24, 1994
    Date of Patent: August 13, 1996
    Assignee: Chesebrough-Pond's USA Co.
    Inventors: Caroline M. Lee, Martin R. Green, Giuseppe Prota
  • Patent number: 5446068
    Abstract: This invention relates to 1-phenyl-3-phenyl-2-propyne-1-ones, the use of these compounds as calcium uptake inhibitors in leukocytes and thrombocytes, and pharmaceutical compositions containing these compounds as active ingredients, and the process of their preparation.
    Type: Grant
    Filed: September 16, 1994
    Date of Patent: August 29, 1995
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Robert J. Dinerstein, Jeffrey S. Sabol, Keith A. Diekema
  • Patent number: 5430062
    Abstract: The present invention relates to stilbene derivatives which possess utility as anti-cancer agents. The compounds can be used to treat cancers which are susceptible to treatment therewith, and can be utilized in a method of treating such cancers. Pharmaceutical compositions containing the compounds are disclosed. Three preferred compounds among those disclosed are (Z)-1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene, (Z)-1-(4-methylphenyl)-2-(3,4,5-trimethoxyphenyl)ethene, and 4-methyl-3',4',5'-trimethoxybenzylaniline hydrochloride.
    Type: Grant
    Filed: June 23, 1993
    Date of Patent: July 4, 1995
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Mark S. Cushman, Ernest Hamel
  • Patent number: 5276058
    Abstract: Novel 3,4-dihydroxychalcone derivatives useful as a pharmaceutical material, and novel anti-inflammatory preparations. The 3,4-dihydroxychalcone derivatives are compounds of the formula [I], ##STR1## wherein X is a substituted phenyl group represented, e.g., by the formula (i), ##STR2## in which R.sup.1 is a hydrogen atom or an alkyl group and R.sup.2 is an alkyl group, an alkoxy group or an --OH group (excluding an OH-group in the 4-position)or salts thereof. The anti-inflammatory preparations contain one of the above 3,4-dihydroxychalcone derivatives as an active ingredient.
    Type: Grant
    Filed: June 9, 1993
    Date of Patent: January 4, 1994
    Assignee: Nippon Hypox Laboratories Incorporated
    Inventors: Toshio Satoh, Hitoshi Matsumoto, Yasunori Niiro
  • Patent number: 5234951
    Abstract: The present invention relates to an anti-ulcer agent comprising a compound represented by the following general formula I as the effective ingredient, and a novel chalcone derivative included in the compound represented by this general formula I: ##STR1## wherein X and Y independently stand for a hydrogen atom or together form a single bond, R.sub.1 stands for a hydroxyl group, an acetoxy group, a carboxymethoxy group or a methoxycarbonylmethoxy group, R.sub.2 stands for a hydrogen atom, an isoprenyl group, isopentyl group or a propyl group, R.sub.3 stands for a hydroxyl group or a methoxy group, R.sub.4 stands for a hydrogen atom, a hydroxyl group or a methoxy group, R.sub.5 stands for a hydrogen atom, a hydroxyl group, a methoxy group or an isopentyl group, R.sub.6 stands for a hydroxyl group, a methoxy group or a carboxymethoxy group, and R.sub.7 stands for a hydrogen atom or a methoxy group.
    Type: Grant
    Filed: November 25, 1991
    Date of Patent: August 10, 1993
    Assignee: Tsumura Juntendo, Inc.
    Inventors: Yukio Komazawa, Shigefumi Takeda, Kunio Hosaka, Hiroshi Mitsuhashi, Toshihiko Watanabe
  • Patent number: 5140037
    Abstract: Substituted imidazoles such as 2-butyl-4-chloro-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]-5-(hydroxy methyl)imidazole and 2-butyl-4-chloro-1-[(2'-carboxybiphenyl-4-yl)-methyl]-5-(hydroxymethyl)imi dazole and pharmaceutically acceptable salts thereof are useful for treating central nervous system disorders, such as cognitive and learning disorders, mediated by angiotensin II.
    Type: Grant
    Filed: March 20, 1990
    Date of Patent: August 18, 1992
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Andrew T. Chiu, Victor J. DeNoble, John J. V. Duncia, Pancras C. B. Wong
  • Patent number: 5106871
    Abstract: The present invention relates to an anti-ulcer agent comprising a compound represented by the following general formula I as the effective ingredient, and a novel chalcone derivative included in the compound represented by this general formula I: ##STR1## wherein X and Y independently stand for a hydrogen atom or together form a single bond, R.sub.1 stands for a hydroxyl group, an acetoxy group, a carboxymethoxy group or a methoxycarbonylmethoxy group, R.sub.2 stands for a hydrogen atom, an isoprenyl group, isopentyl group or a propyl group, R.sub.3 stands for hydroxyl group or a methoxy group, R.sub.4 stands for a hydrogen atom, a hydroxyl group or a methoxy group, R.sub.5 stands for a hydrogen atom, a hydroxyl group, a methoxy group or an isopentyl group, R.sub.6 stands for a hydroxyl group, a methoxy group or a carboxymethoxy group, and R.sub.7 stands for a hydrogen atom or a methoxy group.
    Type: Grant
    Filed: July 19, 1991
    Date of Patent: April 21, 1992
    Assignee: Tsumura & Co.
    Inventors: Yukio Komazawa, Shigefumi Takeda, Kunio Hosaka, Hiroshi Mitsuhashi, Toshihiko Watanabe
  • Patent number: 5093372
    Abstract: A pharmaceutical composition which is a physical mixture of exifone and certain water soluble cellulose derivatives. The mixture exhibits surprisingly improved solubility and bio availability.
    Type: Grant
    Filed: March 2, 1990
    Date of Patent: March 3, 1992
    Assignee: Fujisawa Pharmaceutical Co. Inc.
    Inventors: Yoshio Uedo, Fumio Shimojo, Mitsuru Yasumara, Kenzo Toyoshima, Nobumitsu Nakahasi
  • Patent number: 5084478
    Abstract: A compound of the formula ##STR1## wherein X has the formula --CR.sup.5 .dbd.CR.sup.6 --, --C.tbd.C-- or ##STR2## wherein ring A is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl;wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent or each is hydrogen or alkyl, alkoxy or dialkylamino, provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substituent;wherein R.sup.5 and R.sup.6, each is hydrogen, halogeno or alkylwherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 has the formula --Y--Q--R.sup.9 wherein Y is straight- or branched-chain alkylene or alkenylene; wherein Q is --O--, --S--, --SO-- or --SO.sub.2 --;and wherein R.sup.9 is alkyl of up to 6 carbon atoms which contains one or more defined substituents, processes for their manufacture and pharmaceutical compositions containing them.
    Type: Grant
    Filed: April 14, 1989
    Date of Patent: January 28, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: Leslie R. Hughes, Howard Tucker
  • Patent number: 5059627
    Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is a lower alkyl group; R.sup.2 is a hydrogen atom or an alkyl or alkenyl group which may be substituted; R.sup.3 and R.sup.4 each independently means a lower alkyl or lower alkoxy group or, taken together, mean a butadienylene group; and X.sup.1 and X.sup.2 each means a free hydroxy group or an esterified or etherified hydroxy group, has nerve growth factor secretion inducing activity, and a mammal suffering from degenerative nervous system disorders such as senile dementia, Alzheimer's disease, etc. is treated by administering said compound to said mammal.
    Type: Grant
    Filed: March 2, 1990
    Date of Patent: October 22, 1991
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Kyozo Hayashi
  • Patent number: 5032580
    Abstract: Compositions for anti-AIDS virus and other antivirus medicines are disclosed. Included are one having the ingredients other than glycyrrhizin contained in licorice, specifically flavonoids contained in licorice and more specifically not less than one kind of substance selected from a group consisting of liquiritigenin, i-liquiritigenin, liquiritin and i-liquiritin and glycyrrhizin produces allowed to contain not less than 3% of flavonoids contained in licorice based on glycyrrhizin as major constituting elements. Method of preparing said compositions having the filtrate obtained through the ultrafiltration of aqueous extract from licorice using ultrafiltration membrane with a fractionatable molecular weight of 10,000 to 100,000 as an effective ingredient and drugs for the pevention from infection and onset and for the therapy against AIDS used said compositions are also claimed.
    Type: Grant
    Filed: November 29, 1988
    Date of Patent: July 16, 1991
    Assignee: Sanyo-Kokusaku Pulp Co., Ltd.
    Inventors: Kazuhiro Watanabe, Makoto Yashiro, Makoto Machida
  • Patent number: 5025036
    Abstract: The invention relates to catechol carboxylic acid derivatives of the formula ##STR1## wherein, R.sub.1 is ##STR2## acetyl, hydrogen, hydroxy or alkanoyloxy, R.sub.2 is ##STR3## hydroxy, hydrogen or alkanoyloxy, wherein R is hydrogen, lower alkyl or --(CH.sub.2).sub.n --N--(lower alkyl).sub.2,R.sub.3 is hydrogen, lower alkyl or amino,R.sub.4 is hydrogen, lower alkyl, halogen or aminoA is ##STR4## wherein, R.sub.5 is hydrogen or acyl, R.sub.6 is hydrogen, halogen, lower alkyl, aryl or cycloalkyl, and R.sub.7 and R.sub.8, independently, are hydrogen, lower alkyl or halogen, orA is ##STR5## wherein, R.sub.5 is hydrogen or acyl, R.sub.9 is hydrogen, lower alkyl, R.sub.10 is hydrogen, lower alkyl or halogen, R.sub.11 is hydrogen, lower alkyl, cycloalkyl or halogen, m is 0 or 1, n is an integer of 2-10, provided, that no more than one of R.sub.1 or R.sub.2 can be hydroxy, alkanoyloxy or ##STR6## and when R is hydrogen, salts thereof with pharmaceutically acceptable bases or when R is --(CH.sub.2).sub.
    Type: Grant
    Filed: May 3, 1989
    Date of Patent: June 18, 1991
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Matthew Carson, Ru-Jen L. Han, Ronald A. LeMahieu
  • Patent number: 4952401
    Abstract: A composition and a method of using the same wherein said composition comprises a rodenticide and an additive selected from the group consisting of1. polyoxyalkylated alkyl phenols;2. sorbitan fatty acids and polyoxyalkylated derivatives thereof;3. polyoxyalkylated fatty amines;4. polyoxyalkylated branched or linear alcohols, diols or polyols;5. polyoxyalkylated branched or linear mercaptans;6. polyoxyalkylated esters; and7. polyoxyalkylated amines.The composition may optionally include an organic solvent and/or a dye. The rodenticide may be selected from a wide host of compounds, including brodifacoum, bromadiolone, diphacinone, chlorodiphacinone, monofluoroacetatic acid, bromethalin, calciferol, flocoumafen, and salts of such compounds.
    Type: Grant
    Filed: June 12, 1990
    Date of Patent: August 28, 1990
    Assignee: ICI Americas Inc.
    Inventor: David G. Hobbs
  • Patent number: 4898890
    Abstract: A novel medicine containing isoliquiritigenin as the active ingredient is disclosed, which exhibits excellent effects when used as a medicine for the therapy and prevention of kidney diseases, a medicine for the therapy and prevention of liver diseases, and a medicine for the therapy and prevention of complication resulting from diseases of these organs.
    Type: Grant
    Filed: December 23, 1987
    Date of Patent: February 6, 1990
    Assignees: Dainippon Ink and Chemicals, Inc., Nippon Hypox Laboratories Incorporated
    Inventors: Toshio Sato, Hitoshi Matsumoto, Hisao Kakegawa
  • Patent number: 4888342
    Abstract: Various effects of photoaging or sundamage of skin including impairment of differentiation of epidermal epithelial cells and loss of collagen fibers, abnormal changes in elastic fibers and deterioration of small blood vessels in the dermis of the skin are retarded by applying topically to the epidermis in a maintenance therapy program effective amounts of retinoids including retinoid derivatives and stereoisomers thereof such that epithelial growths are substantially reduced and prevented and the skin substantially regains and maintains its firmness, turgor and elasticity. Moreover, with persistent treatment dermal blood cells and vessels increase and the epidermis and dermis thicken, resulting in improved ability of the skin to sense, resist and recover from irritation or injury. Further, hyperpigmentation, lines and wrinkles due to aging are reduced and prevented. The treatment is particularly useful for human facial skin and preferably applied in amounts insufficient to cause excessive irritation.
    Type: Grant
    Filed: March 8, 1988
    Date of Patent: December 19, 1989
    Inventor: Albert M. Kligman
  • Patent number: 4791123
    Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I ##STR1## in which R.sub.1, R.sub.2, R.sub.3, R.sub.4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.
    Type: Grant
    Filed: January 22, 1987
    Date of Patent: December 13, 1988
    Assignee: Schering Akt.
    Inventors: Helga Franke, Heinrich Franke, Hans-Rudolf Kruger, Hartmut Joppien, Dietrich Baumert, David Giles
  • Patent number: 4686235
    Abstract: Substituted cinnamyl-2,3-dihydrobenzofurans and analogs were prepared from the nucleophlic substitution of a cinnamylhalide with a 2,3-dihydrobenzofuran anion or an analog thereof. These compounds were found to be potent topical anti-inflammatory agents.
    Type: Grant
    Filed: August 12, 1985
    Date of Patent: August 11, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Michael N. Chang, Norman P. Jensen, Milton L. Hammond, Robert A. Zambias, John McDonald, Kathleen M. Rupprecht
  • Patent number: 4643994
    Abstract: This invention relates to novel organic trithio oxides of the formula:R.sup.1 --X --R--X.sup.1 --R.sup.1wherein R is selected from --CH.sub.2 CH.dbd.CH--, ##STR1## and (CH.sub.2).sub.3 ; X is selected from ##STR2## X.sup.1 is selected from --S--S, ##STR3## and, each R.sup.1 is independently selected from carboxyalkyl, alkoxy, alkylthio, amino, alkylamino and acyl substituted and unsubstituted lower alkyl, lower alkenyl, lower alkynyl, phenyl and lower alkylphenyl; provided when R is --CH.sub.2 CH.dbd.CH--, X is ##STR4## and X.sup.1 is --S--S--, then R.sup.1 is not in both instances --CH.sub.2 CH.dbd.CH.sub.2.This invention also relates to a method of preparing the above-identified compounds by heating and further oxidizing various oxides of organic disulfides and to antithrombotic uses of the compounds.
    Type: Grant
    Filed: December 17, 1984
    Date of Patent: February 17, 1987
    Assignee: The Research Foundation of State University of New York
    Inventors: Eric Block, Saleem Ahmad
  • Patent number: 4621098
    Abstract: The present invention provides thioethers of the general formula: ##STR1## wherein Ar is a phenyl radical which is optionally substituted one, two or three times by alkyl, alkenyl, alkoxy, alkylthio, alkanoyl, hydroxyl, hydroxyalkyl, carboxyl, alkoxycarbonyl, carbamoyl, nitro, amino or halogen, Q is an oxygen or sulphur atom or an NH group, A is a straight-chained or branched C.sub.2 -C.sub.8 alkylene radical which is optionally substituted by a hydroxyl group or can be interrupted by an ethenylene or ethynylene group, n is 0, 1 or 2, and R is a hydrogen atom or a straight-chained or branched alkyl radical which is optionally substituted one or more times by the same or different radicals selected from alkoxycarbonyl, alkoxy, hydroxyl, carboxyl or optionally substituted carbamoyl or amino; as well as the pharmacologically acceptable salts thereof, with the proviso that A cannot be ethylene when Ar is a phenyl radical, Q is an oxygen atom and R is the group --CH.sub.2 COOH.
    Type: Grant
    Filed: July 2, 1984
    Date of Patent: November 4, 1986
    Assignee: Boehringer Mannheim GmbH
    Inventors: Robert Umminger, Walter-Gunar Friebe, Wolfgang Kampe, Androniki Roesch, Otto-Henning Wilhelms
  • Patent number: 4613611
    Abstract: A method of treating diabetes mellitus using arylglyoxals which are known compounds.
    Type: Grant
    Filed: October 14, 1983
    Date of Patent: September 23, 1986
    Assignee: American Cyanamid Company
    Inventors: Middleton B. Floyd, Jr., Jo A. Goidl
  • Patent number: 4605674
    Abstract: Antivirally active compounds of the formula ##STR1## wherein R.sup.1 represents hydroxy, acyloxy derived from an aliphatic acid having 2-18 carbon atoms or a heterocyclic carboxylic acid containing nitrogen atom(s), lower alkoxycarbonyloxy, aminoacyloxy or carboxyalkanoyloxy;R.sup.2 represents lower alkoxy;R.sup.3 represents hydrogen or lower alkoxy; andR.sup.4 represents phenyl which may be substituted by one or more substituents selected from the group consisting of lower alkyl, lower alkoxy, benzyloxy, allyloxy, alkylthio, dialkylamino, amino, cyano, hydroxy, halo and alkylenedioxy; or pyridyl, furyl, thienyl or pyrrolyl which may be substituted by lower alkyl,pharmaceutical compositions containing them and a process for the preparation of those compounds of formula I which are novel.
    Type: Grant
    Filed: April 24, 1984
    Date of Patent: August 12, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Morio Fujiu, Yasuji Suhara, Hideo Ishitsuka