Oxy Containing Patents (Class 568/441)
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Patent number: 8802659Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: GrantFiled: August 5, 2010Date of Patent: August 12, 2014Assignee: Biogen Idec MA Inc.Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
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Publication number: 20140128637Abstract: This invention related to atropisomeric 1,8-bisphenolnaphthalenes and derivatives thereof of the general formula (I): which are useful in resolution of enantiomers, enantioselective recognition and asymmetric synthesis.Type: ApplicationFiled: April 3, 2012Publication date: May 8, 2014Inventors: Christian Wolf, Marwan W. Ghosn
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Patent number: 8455540Abstract: Gossypol and apogossypol derivatives of general formula (1), preparation thereof and use thereof.Type: GrantFiled: December 5, 2008Date of Patent: June 4, 2013Assignee: Universite du Maine (Le Mans)Inventors: Jacques Mortier, Anne-Sophie Castanet, Nguyet Trang Thanh Chau
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Patent number: 8436207Abstract: Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, or NHSO2X, wherein X is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, heterocycle, or substituted heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.Type: GrantFiled: September 21, 2011Date of Patent: May 7, 2013Assignee: Burnham Institute for Medical ResearchInventor: Maurizio Pellecchia
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Publication number: 20130101509Abstract: The present invention relates to in vivo imaging and radiotherapeutic methods and agents which target the enzyme aldehyde dehydrogenase (ALDH) and that are suitable for the in vivo imaging of tumours and treatment of cancer.Type: ApplicationFiled: September 19, 2012Publication date: April 25, 2013Applicants: GENERAL ELECTRIC COMPANY, GE HEALTHCARE LIMITEDInventors: GE HEALTHCARE LIMITED, GENERAL ELECTRIC COMPANY
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Publication number: 20130018194Abstract: This invention relates to octahydro-binaphthol derivatives, which can recognize amino acids and amino alcohols enantioselectively and transform L-amino acids into D-amino acids and optically resolve amino acids or amino alcohol with high efficiency.Type: ApplicationFiled: April 1, 2011Publication date: January 17, 2013Applicants: AMINOLUX, INC, EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATIONInventor: Kwan-Mook Kim
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Publication number: 20120248337Abstract: Compositions providing metal-independent phosphorescence due to a directed heavy atom effect are provided. Methods of providing a phosphorescent composition are also provided where a directed heavy atom effect is maintained to cause the composition to be phosphorescent. Manufacture of phosphorescent compositions using intermolecular and intramolecular directed heavy atom effects are disclosed.Type: ApplicationFiled: November 24, 2010Publication date: October 4, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Jinsang Kim, Onas Bolton, Kangwon Lee, Eun Jeong Jeong, Bong-Gi Kim
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Patent number: 8278440Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.Type: GrantFiled: February 15, 2011Date of Patent: October 2, 2012Assignee: Les Laboratoires ServierInventors: Jean-Louis Peglion, Pascal Caignard
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Publication number: 20120190649Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: ApplicationFiled: August 5, 2010Publication date: July 26, 2012Applicant: BIOGEN IDEC MA INC.Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
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Patent number: 8097720Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.Type: GrantFiled: December 23, 2009Date of Patent: January 17, 2012Assignee: Les Laboratories ServerInventors: Jean-Louis Peglion, Aimee Dessinges, Bernard Serkiz, Jean-Michel Lerestif, Jean-Pierre Lecouve
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Publication number: 20110286922Abstract: The present invention relates to in vivo imaging and radiotherapeutic methods and agents which target the enzyme aldehyde dehydrogenase (ALDH) and that are suitable for the in vivo imaging of tumours and treatment of cancer.Type: ApplicationFiled: October 20, 2009Publication date: November 24, 2011Inventors: Alan Cuthbertson, Peter Brian Iveson, Rajiv Bhalla, Vijaya Raj Kuniyil Kulangara
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Publication number: 20110281293Abstract: A preparation method and its use of derivatisation reagent for detecting L-carnitine or D-carnitine are provided. The present reagent is stable. It can be used for detecting L-carnitine or D-carnitine accurately and sensitively. That is to say, the reagent is applied to detecting the amount of synthesized or natural L-carnitine and the amount of mixing D-carnitine. The compound reagent is used for determining the chiral isomers of chemicals, biological reagents, health care reagents, cosmetic, body fluids and various foods, which contain L-carnitine or/and D-carnitine, and optical isomers of other chiral amino acids.Type: ApplicationFiled: October 9, 2009Publication date: November 17, 2011Inventors: Shuhua Gu, Qingyi Li, Xuecheng Wang
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Patent number: 8039668Abstract: Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, or NHSO2X, wherein X is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, heterocycle, or substituted heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.Type: GrantFiled: April 14, 2010Date of Patent: October 18, 2011Assignee: Burnham Institute for Medical ResearchInventor: Maurizio Pellecchia
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Publication number: 20110021613Abstract: Compounds obtainable from plants, e.g. of the genus Eucalyptus, or from microorganisms are shown to be useful as CNS activity modulators useful e.g. in the treatment of depression, for lifting mood and/or for increasing behavioural initiative and the like. This use and related aspects form embodiments of the invention. Also compounds as such are presented. The compounds useful are acylphloroglucine derivatives of the formula I, wherein the substituents are as defined in the description.Type: ApplicationFiled: December 11, 2007Publication date: January 27, 2011Applicant: INTERMED DISCOVERY GMBHInventors: Ernst Roemer, Torsten Grothe
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Publication number: 20100331398Abstract: Gossypol and apogossypol derivatives of general formula (1), preparation thereof and use thereof.Type: ApplicationFiled: December 5, 2008Publication date: December 30, 2010Applicant: UNIVERSITE DU MAINE (LE MANS)Inventors: Jacques Mortier, Anne-Sophie Castanet, Nguyet Trang Thanh Chau
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Publication number: 20100286284Abstract: The present invention relates to new compounds of formula (I) and to their use as medicaments. Preferably, the said compounds are used in the preparation of a medicament or food supplement intended for the treatment and/or prevention of ailments or pathologies ensuing from a disorder of the reuptake of the following neurotransmitters: dopamine, serotonin and/or noradrenaline.Type: ApplicationFiled: January 13, 2009Publication date: November 11, 2010Applicant: Pierre Fabre MedicamentInventors: Christel Fiorini-Puybaret, Philippe Joulia
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Publication number: 20100267781Abstract: Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, or NHSO2X, wherein X is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, heterocycle, or substituted heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.Type: ApplicationFiled: April 14, 2010Publication date: October 21, 2010Applicant: Burnham Institute for Medical ResearchInventor: Maurizio Pellechia
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Publication number: 20100160628Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.Type: ApplicationFiled: December 23, 2009Publication date: June 24, 2010Applicant: LES LABORATOIRES SERVIERInventors: Jean-Louis Peglion, Aimée Dessinges, Bernard Serkiz, Jean-Michel Lerestif, Jean-Pierre Lecouve
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Patent number: 7470821Abstract: The invention relates to novel aldolase-inhibiting compounds that can be advantageously used as medicaments (in therapeutic doses), especially for treating certain cancers, due to the inhibition efficacy thereof. An inventive compound corresponds to general formula (I) wherein the aldehyde group (—CHO) and the phenol group (—OH) are linked to two carbon atoms adjacent to the same aromatic chain, i.e., the first aromatic chain, and R is a phosphate group or a phosphate group mimetic linked to a carbon atom of the second aromatic chain.Type: GrantFiled: June 29, 2004Date of Patent: December 30, 2008Assignees: Valorisation-Recherche, Limited Partnership, Universite Paul Sabatier Toulouse IIIInventors: Chantal Dax, Casimir Blonski, Laurent Azema, Jurgen Sygusch
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Patent number: 6949682Abstract: The present invention relates to cinnamaldehyde derivatives inhibiting growth of tumor cell and regulating cell cycle, the method for preparation and the pharmaceutical composition thereof. The cinnamaldehyde derivatives of the present invention can be effectively used as a cell cycle regulator or a cancer cell growth inhibitor, since it has an ability to regulate cell cycle by holding the cells in G2/M stage of the cell division and has activity to inhibit cancer cell growth.Type: GrantFiled: May 28, 2004Date of Patent: September 27, 2005Assignee: Korea Research Institute of Bioscience and BiotechnologyInventors: Byoung-Mog Kwon, Kwang-Hee Son, Dong Cho Han, Sangku Lee, Jong Han Kim, Sung-Gyu Choi, Mi-Young Lee, Sun Bok Jeon
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Patent number: 6914074Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10, are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 11, 2002Date of Patent: July 5, 2005Assignee: WyethInventors: Richard E. Mewshaw, Richard J. Edsall, Cuijian Yang, Heather A. Harris, James C. Keith, Jr., Leo M. Albert, Eric S. Manas
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Publication number: 20040225123Abstract: This invention provides estrogen receptor modulators of formula I, having the structure 1Type: ApplicationFiled: March 18, 2004Publication date: November 11, 2004Inventors: Richard E. Mewshaw, Richard J. Edsall, Cuijian Yang, Heather A. Harris, James C. Keith, Leo M. Albert, Eric S. Manas
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Patent number: 6794415Abstract: A method of treating osteoporosis in warm-blooded animals comprising administering to warm-blooded animals in need thereof an effective amount to treat osteoporosis of a compound selected from the group consisting of a compound of the formula: wherein the substituents are defined as in the Specification.Type: GrantFiled: July 8, 2002Date of Patent: September 21, 2004Assignee: Aventis Pharma S.A.Inventors: Dominique Lesuisse, Jean-Georges Teutsch
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Patent number: 6624330Abstract: The present invention relates to a method for stabilizing phenylacetaldehyde by adding at least one additive, in which case the additive contains one or more polybasic carboxylic acids.Type: GrantFiled: December 4, 2001Date of Patent: September 23, 2003Assignee: Haarmann & Reimer GmbHInventor: Walter Kuhn
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Patent number: 6528676Abstract: The application discloses methods of treating mammalian diseases characterized by abnormal cell mitosis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.Type: GrantFiled: February 2, 1999Date of Patent: March 4, 2003Assignee: The Children's Medical Center CorporationInventors: Robert John D'Amato, Moses Judah Folkman
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Patent number: 6509507Abstract: A process for preparing polymerizable biaryl derivatives comprises reacting an aromatic comprising a 6-membered ring which bears ester or benzylic OH groups in the 1,4 position with a second aromatic in a palladium-catalyzed cross-coupling reaction to give a biaryl and converting the ester or benzylic OH groups into polymerizable groups in one or more steps. The biaryls obtained are suitable for preparing polymers which are used as electroluminescence materials.Type: GrantFiled: October 16, 2001Date of Patent: January 21, 2003Assignee: Aventis Research & Technologies GmbH & Co. KGInventors: Hubert Spreitzer, Willi Kreuder, Heinrich Becker, Jochen Krause
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Patent number: 6420610Abstract: Aromatic aldehyde compounds of formula (4) and (6) are disclosed, wherein Y is a methylene group with various substitutions and R represents various substituents.Type: GrantFiled: September 13, 2000Date of Patent: July 16, 2002Assignee: Fuji Photo Film Co., Ltd.Inventors: Takashi Nakamura, Toshiyuki Makuta, Koki Nakamura
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Patent number: 6326369Abstract: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.Type: GrantFiled: July 6, 1999Date of Patent: December 4, 2001Assignee: Takeda Chemicals Industries, Ltd.Inventors: Kaneyoshi Kato, Taiichi Ohra, Masaomi Miyamoto
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Patent number: 6323373Abstract: A process for preparing polymerizable biaryl derivatives comprises reacting an aromatic comprising a 6-membered ring which bears ester or benzylic OH groups in the 1,4 position with a second aromatic in a palladium-catalyzed cross-coupling reaction to give a biaryl and converting the ester or benzylic OH groups into polymerizable groups in one or more steps. The biaryls obtained are suitable for preparing polymers which are used as electroluminescence materials.Type: GrantFiled: June 9, 1999Date of Patent: November 27, 2001Assignee: Aventis Research & Technologies GmbH & Co. KGInventors: Hubert Spreitzer, Willi Kreuder, Heinrich Becker, Jochen Krause
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Patent number: 6162445Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (I): in which X is one of the radicals: ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: October 6, 1997Date of Patent: December 19, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6156750Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds have the structural formula (I): ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: January 13, 1999Date of Patent: December 5, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6147224Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.Type: GrantFiled: October 1, 1998Date of Patent: November 14, 2000Assignee: Allergan Sales, Inc.Inventors: Vidyasagar Vuligonda, Kwok Yin Tsang, Jayasree Vasudevan, Roshantha A. Chandraratna
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Patent number: 5936120Abstract: The invention provides deoxygossylic compounds having useful biological activities, and methods for the synthesis of these and related compounds. The invention further provides valuable intermediates for the synthesis of the compounds, and pharmaceutical compositions containing biologically active compounds according to the invention.Type: GrantFiled: December 10, 1997Date of Patent: August 10, 1999Assignee: University of New MexicoInventors: Robert D. Royer, Lorraine M. Deck, David L. VanderJagt
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Patent number: 5766610Abstract: Novel pharmaceutically/cosmetically-active polycyclic aromatic compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formulae (a)-(e): ##STR2## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: April 26, 1995Date of Patent: June 16, 1998Assignee: Centre International De Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 5656619Abstract: Abstract of the Disclosure: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: June 6, 1995Date of Patent: August 12, 1997Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5476860Abstract: Diaromatic compounds, characterized in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.Type: GrantFiled: December 8, 1993Date of Patent: December 19, 1995Assignee: Centre International de Recherches Dermatologiques (CIRD Galderma)Inventor: Jean-Michel Bernardon
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Patent number: 5470999Abstract: Compounds of Formula 1 ##STR1## where R.sub.1 -R.sub.5 are hydrogen, lower alkyl of 1-6 carbons, or halogen; A is (CH.sub.2).sub.n where n is 0-5, lower branched chain alkyl having 3-6 carbons, cycloalkyl having 3-6 carbons, alkenyl having 2-6 carbons and 1 or 2 double bonds, alkynyl having 2-6 carbons and 1 or 2 triple bonds; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, or CR.sub.7 OR.sub.13 O, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.Type: GrantFiled: December 30, 1993Date of Patent: November 28, 1995Assignee: Allergan, Inc.Inventor: Roshantha A. Chandraratna
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Patent number: 5403823Abstract: The present invention relates, inter alia, to novel alkyl indane aldehyde compounds having fragrant musk-like aroma.Type: GrantFiled: January 21, 1994Date of Patent: April 4, 1995Assignee: Union Camp CorporationInventor: Walter C. Frank
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Patent number: 5401720Abstract: The present invention relates, inter alia, to novel alkyl tetralin aldehyde compounds having fragrant musk-like aroma.Type: GrantFiled: January 21, 1994Date of Patent: March 28, 1995Assignee: Union Camp CorporationInventor: Walter C. Frank
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Patent number: 5232836Abstract: Vitamin D derivatives corresponding to the following formula I ##STR1## in which R.sub.1 denotes a substituted alkyl group having 1 to 15 carbon atoms, in particular the side chains of vitamin D.sub.2 (C.sup.20 to C.sup.28) or D.sub.3 (C.sup.20 to C.sup.Type: GrantFiled: February 18, 1992Date of Patent: August 3, 1993Assignee: Ire-Medgenix S.A.Inventors: Roger Bouillon, Pierre J. De Clerco, Pierre Eliard, Maurits Vanderwalle
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Patent number: 5194663Abstract: An aromatic derivative of butyric acid has the formula ##STR1## These aromatic derivatives of butyric acid are useful in human and veterinary medicines as well as in cosmetic compositions.Type: GrantFiled: August 9, 1991Date of Patent: March 16, 1993Assignee: Societe Anonyme Dite: L'OrealInventors: Jean Maignan, Gerard Malle, Gerard Lang
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Patent number: 5169974Abstract: The invention concerns a novel process for the manufacture of various aryloxyaliphatic aldehydes and related arylthio analogues, which are useful as chemical intermediates. The process involves reacting a dihalogenohydroxyalkane of the formula: HO.C(R.sup.2).sub.2.CHX.sub.2 wherein R.sup.2 is alkyl and X is chloro or bromo with a phenol or thiophenol in the presence of base and is applicable to large scale use.Type: GrantFiled: October 20, 1989Date of Patent: December 8, 1992Assignee: Imperial Chemical Industries PLCInventors: Gregory D. Harris, Stanley A. Lee
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Patent number: 5128479Abstract: Oxidized diphenylheteroalkanes of the formula I ##STR1## where R.sup.1 to R.sup.6 and A have the meanings specified in the description, and the preparation thereof are described. The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: January 29, 1990Date of Patent: July 7, 1992Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5112869Abstract: This invention concerns compounds having the structure: ##STR1## wherein each of R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.2', R.sup.3', R.sup.4', and R.sup.5', is independently hydrogen (--H), or a hydroxyl (--OH), methoxy (--OMe), methyl (--Me), carboxaldehyde (--CHO) or phenylformazen (Ph--N.dbd.CH--) group.This invention also provides a novel process of synthesizing the compounds of the subject invention, including intermediate compounds useful in the process.The present invention also provides pharmaceutical compositions comprising a pharmaceutically effective amount of a compound according to the subject invention and a pharmaceutically acceptable carrier. Finally, the invention provides spermicidal methods and methods of killing or of retarding the proliferation of, cancer cells.Type: GrantFiled: April 4, 1989Date of Patent: May 12, 1992Assignee: Sloan-Kettering Institute For Cancer ResearchInventors: Kyoichi A. Watanabe, Tsann-Long Su, Jai-Tung Huang
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Patent number: 5093519Abstract: Vitamin D derivatives corresponding to the following formula I ##STR1## in which R.sub.1 denotes a substituted alkyl group having 1 to 15 carbon atoms, in particular the side chains of vitamin D.sub.2 (C.sup.20 to C.sup.28) or D.sub.3 (C.sup.20 to C.sup.Type: GrantFiled: May 1, 1989Date of Patent: March 3, 1992Assignee: Ire-Medgenix S.A.Inventors: Roger Bouillon, Pierre J. De Clercq, Pierre Eliard, Maurits Vandewalle
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Patent number: 5087743Abstract: Diphenylheteroalkyl derivatives of the formula I ##STR1## where A and R.sup.1 -R.sup.6 have the meanings specified in the description, and the preparation thereof are described.The substances are suitable for controlling diseases and as cosmetic agents.Type: GrantFiled: January 23, 1990Date of Patent: February 11, 1992Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Quinoline substituted naphthalenepropionic acid derivatives as anti-inflammatory/antiallergic agents
Patent number: 5084575Abstract: There are disclosed compounds of the formula ##STR1## wherein a is alkyl 3-19 carbon atoms, diloweralkyl allyl, diahaloallyl, diphenylallyl, lower alkynyl, ##STR2## W is --CR.sub.2 O--, --CH.dbd.CH-- or --CH.dbd.CHCH.sub.2 O-- X is N or CR;Z is ##STR3## R is hydrogen or lower alkyl; Y is ##STR4## R.sup.1 is hydrogen, lower alkyl or phenyl; R.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 taken together form a benzene ring, optionally substituted by halo;R.sup.3 is --OR, ##STR5## -- NHSO.sub.2 R.sup.4 ; R.sup.4 is phenyl or loweralkyl substituted phenyl;R.sup.5 is halo;and the pharmaceutically acceptable salts thereof, and their use in the treatment of leukotriene-mediated naso-bronchial obstructive airpassageway conditions, such as alelrgic rhinitis, allergic bronchial asthma and the like, in psoriasis, ulcerative colitis, rheumatoid arthritis as well as in other immediate hypersensitivity reactions.Type: GrantFiled: September 6, 1990Date of Patent: January 28, 1992Assignee: American Home Products CorporationInventors: Anthony F. Kreft, III., John H. Musser, James J. Bicksler, John W. Giberson, Dennis M. Kubrak, Annette L. Banker -
Patent number: 4983627Abstract: Compounds useful in treating or preventing gastrointestinal ulcers and in treating cardiovascular disorders such as thrombosis, hypertension and atherosclerosis are depicted in formulas (1), (2) and (3): ##STR1## wherein: A is --C.tbd.C--, trans --HC.dbd.CH--, trans --CH.dbd.CHCH.sub.2 -- or --CH.sub.2 CH.sub.2 --;X is lower alkyl of 1-6 carbon atoms;Y is hydrogen, exo-(lower alkyl) or endo-(lower alkyl);n is an integer from 2-4;R.sub.1 is --CH.sub.2 OH, --CHO, --CO.sub.2 R or --CO.sub.2 H, and the olefin formed by the R.sub.1 (CH.sub.2).sub.n CH.dbd. moiety is either (E) or (Z);R.sub.2 is hydrogen or methyl, or optionally --CH.dbd.CH.sub.2 when A is trans --CH.dbd.CHCH.sub.2 --; andR.sub.3 is linear or branched alkyl, alkenyl or alkynyl having 5-10 carbon atoms, ##STR2## --(CH.sub.2).sub.m -phenyl or CH.sub.2 O-phenyl; in which each phenyl may be optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen.Type: GrantFiled: November 10, 1988Date of Patent: January 8, 1991Assignee: Syntex (U.S.A.) Inc.Inventors: Counde O'Yang, Walter Kurz, Keith A. M. Walker, Helen Y. Wu
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Patent number: 4760089Abstract: Potent, irreversible dopamine-.beta.-hydroxylase inhibitors having the Formula: ##STR1## which are useful to inhibit dopamine-.beta.-hydroxylase activity, pharmaceutical compositions including these inhibitors or 2-cyano-2-phenethylamine, and methods of using these inhibitors or 2-cyano-2-phenethylamine to inhibit dopamine-.beta.-hydroxylase activity in mammals. Also disclosed are novel intermediates useful in preparing the presently invented inhibitors.Type: GrantFiled: September 9, 1985Date of Patent: July 26, 1988Assignee: SmithKline Beckman CorporationInventors: Pamela A. Chambers, James S. Frazee, Carl Kaiser, Lawrence I. Kruse
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Patent number: 4739099Abstract: The invention provides a compound of formula (II): ##STR1## and the corresponding isomers and salts; in this formula, a equals 0 or 1; R.sub.1 and R.sub.2 represent, independently, H or a C.sub.1 -C.sub.4 alkyl group; R.sub.3 denotes --C.tbd.N; oxazolinyl; --CH.sub.2 OR.sub.4 (R.sub.4 =H, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.6 mono- or poly-hydroxyalkyl, cyclopentyl or cyclohexyl, or --OR.sub.4 =tetrahydropyranyl); --COR.sub.5 (R.sub.5 =H, C.sub.1 -C.sub.4 alkyl, --NR'R" where R' and R" have various meanings); --OR.sub.6 (R.sub.6 =H, C.sub.1 -C.sub.18 alkyl, C.sub.2 -C.sub.3 monohydroxyalkyl or C.sub.3 -C.sub.6 polyhydroxyalkyl with 2-5 OH groups), which has useful medicinal and cosmetic applications.Type: GrantFiled: September 30, 1985Date of Patent: April 19, 1988Assignee: L'OrealInventors: Gerard Lang, Serge Forestier, Alain Lagrange, Braham Shroot