Carboxyl, Or Salt Thereof, Bonded Directly To A Ring Patents (Class 562/473)
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Publication number: 20090068738Abstract: The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).Type: ApplicationFiled: March 14, 2008Publication date: March 12, 2009Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: CAROLYN RUTH BERTOZZI, NICHOLAS J. AGARD, JENNIFER A. PRESCHER, JEREMY MICHAEL BASKIN, ELLEN MAY SLETTEN
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Patent number: 7423030Abstract: A 1-amino-phthalazine derivative of general formula (I) wherein the substituents are as defined herein. Also disclosed are a method for preparing such compounds, intermediates for use in such method and medical treatments using the compounds of formula (I).Type: GrantFiled: October 11, 2006Date of Patent: September 9, 2008Assignee: Sanofi-AventisInventors: Jean Michel Augereau, Michel Geslin, Gilles Courtemanche
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Patent number: 7348453Abstract: Described are ortho carboxy phenol derived acetals and compositions containing ortho carboxy phenol derived acetals which are useful for delivering biologically active compounds to cells. The acetals can be used to reversibly link up to three different molecules and have rapid hydrolysis kinetics in conditions which are present in a cell as well as in vivo. Cleavage of the acetal enhances delivery of the biologically active compound.Type: GrantFiled: August 30, 2004Date of Patent: March 25, 2008Assignee: Mirus Bio CorporationInventors: David B. Rozema, Darren Wakefield
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Patent number: 7238835Abstract: The invention relates to a process for the preparation of a compound of the general formula (I) in which a) a compound (II) is reacted in the presence of a base B1 with a compound (III) and b) the compound (IV) formed as intermediate in step a) is reacted in the presence of a base B2 with a compound (V) to give the compound of the general formula (I)Type: GrantFiled: December 21, 2004Date of Patent: July 3, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Wolfgang Fiedler, Bernd Neises, Jochen Hachtel
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Patent number: 7067640Abstract: The invention relates to a method which comprises synthesizing bifunctional compounds then chiral compounds from the bifunctional compounds, also to synthesizing supports comprising these chiral compounds, and the use of these supports for preparing or separating enantiomers, or for asymmetric synthesis. The invention also relates to bifunctional compounds, their use as a source of functionalized polymers, and to the chiral compounds, also to the use of these chiral compounds in a chiral support in the form of a three-dimensional network or for separating or preparing enantiomers, principally for analytical or preparative chromatography, and in a support for the production of chiral molecules by asymmetric synthesis.Type: GrantFiled: April 3, 2000Date of Patent: June 27, 2006Assignee: EKA Chemicals ABInventors: Raphaël Duval, Hubert Leveque
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Patent number: 6909015Abstract: The invention relates to polyetherketones and to a process for the preparation of aromatic polyetherketones which process comprises: a) self-condensing a compound of formula (I) wherein n represents 0 or 1 in the presence of an alkyl or optionally substituted aryl sulphonic acid solvent and in the absence of phosphorous pentoxide; or b) condensing a compound of general formula (II) and a compound of general formula (III) wherein p and q independently represent 0 or 1, in the presence of an alkyl or optionally substituted aryl sulphonic acid solvent and in the absence of phosphorous pentoxide; or c) a combination of a) and b)Type: GrantFiled: February 9, 2001Date of Patent: June 21, 2005Assignee: Victrex Manufacturing LimitedInventors: David John Kemmish, Brian Wilson
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Patent number: 6838574Abstract: A medicament comprising as an active ingredient a compound or a physiologically acceptable salt thereof represented by general formula (I): wherein R1 represents a dicarba-closo-dodecaboran-yl which may be substituted with a lower alkyl group, a lower alkenyl group, carboxyl group or the like; R2 represents carboxyl group, a lower alkoxycarbonyl group, or hydroxyl group; and X represents a single bond or a linking group such as —CO—Y1— wherein Y1 represents oxygen or —N(R3)— wherein R3 represents hydrogen or a lower alkyl.Type: GrantFiled: January 21, 2000Date of Patent: January 4, 2005Assignee: Institute of Medicinal Molecular Design, Inc.Inventor: Yasuyuki Endo
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Publication number: 20040260119Abstract: The invention relates to an improved process for preparing 3-alkoxy-2-methylbenzoic acids by heating substituted naphthalenes in the presence of alkali metal hydroxides and subsequently alkylating.Type: ApplicationFiled: June 10, 2003Publication date: December 23, 2004Inventors: Johannes Scherer, Friedrich Mueller-Hauck
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Patent number: 6822112Abstract: A prostaglandin derivative represented by the formula: wherein X is a halogen atom, R1 is a hydrogen atom, a C1-10 alkyl group or a C3-10 cycloalkyl group, m is an integer of 0 to 5, and Y is a group represented by the formula: wherein R2 is a C3-10 cycloalkyl group, a C3-10 cycloalkyl group substituted with C1-4 alkyl group(s), a C1-4 alkyl group substituted with C3-10 cycloalkyl group(s), a C1-10 alkyl group, a C2-10 alkenyl group, a C2-10 alkynyl group or a bridged cyclic hydrocarbon group, or a group represented by the formula: wherein n is an integer of 1 to 8; a pharmaceutically acceptable salt thereof or a hydrate thereof.Type: GrantFiled: February 5, 2002Date of Patent: November 23, 2004Assignees: Taisho Pharmaceutical Co., Ltd.Inventors: Fumie Sato, Tohru Tanami, Hideo Tanaka, Naoya Ono, Makoto Yagi
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Patent number: 6794538Abstract: Process for the preparation of ethers of hydroxybenzoic acid having general formula (I), which comprises reacting a hydroxybenzoic acid, optionally substituted, with a halide XR1, wherein X is a halogen such as chlorine, in a basic environment and in an aqueous or aqueous/organic biphasic solvent.Type: GrantFiled: May 31, 2002Date of Patent: September 21, 2004Assignee: Borregaard Italia S.p.A.Inventors: Pietro Panseri, Vittorio Messori, Patrizia Mangini
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Patent number: 6762329Abstract: One aspect of the present invention relates to novel reaction conditions that allow the efficient synthesis of diaryl ethers from arenes bearing a leaving group and arenols under relatively mild conditions. Another aspect of the present invention relates to the dramatic effects of acidic activators on Ullmann-type couplings involving electron-poor and/or relatively insoluble substrates.Type: GrantFiled: April 25, 2002Date of Patent: July 13, 2004Assignee: Massachusetts Institute of TechnologyInventors: Jean-Francois Marcoux, Sven Doye, Stephen Buchwald
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Patent number: 6747170Abstract: A thermosensitive recording material has a support and a thermosensitive coloring layer formed thereon containing a leuco dye and a color developer capable of inducing color formation in the leuco dye upon application of heat thereto, with the color developer including at least one compound (A) having in a molecule thereof at least two aromatic ring moieties with specific structures, selected from the group consisting of an aromatic ring moiety having at least one carboxyl group and electron-attracting functional group, an aromatic ring moiety having at least one carboxyl group and electron-donating functional group, and an aromatic ring moiety having at least one carboxyl group, free of the electron-attracting and electron-donating functional groups. An aromatic carboxylic acid compound serving as the above-mentioned compound (A) and the producing method thereof are also disclosed.Type: GrantFiled: May 23, 2002Date of Patent: June 8, 2004Assignee: Ricoh Company, Ltd.Inventors: Kunio Hayakawa, Mitsunobu Morita
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Patent number: 6737544Abstract: A process for drying phenoxymethylbenzoic acids of the general formula I where X, Y, m and n have the following meanings: X, Y halogen or a C-organic radical, m a value from 0 to 4 and n a value from 0 to 5 which comprises drying the water- and/or solvent-wet phenoxymethylbenzoic acids at a temperature in the range from 1° to 25° C. above their melting point under the reaction conditions used.Type: GrantFiled: March 20, 2001Date of Patent: May 18, 2004Assignee: BASF AktiengesellschaftInventors: Heinz Isak, Martin Lambert
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Publication number: 20030162111Abstract: A method for producing a charge controlling agent comprisinig a reaction product of an aromatic hydroxycarboxylic acid and a calcium compound bonded by at least one bondinig system selected from the group consisting of coordinate bonding, covalent bonding and ionic bonding, characterized in that the aromatic hydroxycarboxylic acid and the calcium compound are reacted by dropwise adding a solution of the aromatic hydroxycarboxylic acid to a solution of the calcium compound as a metal-imparting agent, a charge controlling agent produced by said method, which has a shape coefficient (SF-1) average value of at most 250 and a shape coefficient (SF-2) average value of at most 200, and an electrostatic image developing toner containing said charge controlling agent having a presence ratio on a toner surface of at least 2.0 mg/1 g of toner.Type: ApplicationFiled: November 29, 2002Publication date: August 28, 2003Inventors: Shinji Otani, Noriyuki Suzuki, Hideyuki Otsuka, Mitsutoshi Anzai
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Patent number: 6603012Abstract: New compounds containing bicyclic fused rings, one of which being a phenyl moiety connected by an aliphatic chain to a cycloalkyl or aryl moiety, and pharmaceutically active salts thereof are useful as RAR selective retinoid agonists. Furthermore, such retinoic acid receptor agonists, particularly retinoic acid receptor &ggr; (RAR&ggr;) selective agonists, are useful for the treatment of emphysema and associated pulmonary diseases, as well as for the therapy and prophylaxis of dermatological disorders, for the therapy and prophylaxis of malignant and premalignant epithelial lesions, tumors and precancerous changes of the mucous membrane in the mouth, tongue, larynx, esophagus, bladder, cervix and colon.Type: GrantFiled: April 23, 2001Date of Patent: August 5, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Paula Nanette Belloni, Synese Jolidon, Michael Klaus, Jean-Marc Lapierre
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Patent number: 6566548Abstract: Novel molecular compounds containing carboxylic acid derivatives represented by general formula (I) or (II) as the constituent compound and exhibiting excellent performances in various technical fields including selective separation of useful substances, chemical stabilization, nonvolatilization, prolongation of release and powderization, wherein X is (CH2)n or p-phenylene; n is 0, 1, 2 or 3; R1 to R8 and R13 to R20 are each hydrogen, C1-C6 alkyl, C2-C4 alkenyl, phenyl optionally substituted with C1-C6 alkyl, halogeno or C1-C6 alkoxy; and R9 to R12 and R21 to R24 are each hydrogen, C1-C6 alkyl, C2-C4 alkenyl, C11-C12 aralkyl or an alkali metal.Type: GrantFiled: March 29, 2001Date of Patent: May 20, 2003Assignee: Nippon Soda Co., Ltd.Inventors: Satoru Abe, Hiroshi Suzuki
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Patent number: 6417178Abstract: Amyloid binding compounds which are derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing Chrysamine G and derivatives thereof and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.Type: GrantFiled: November 6, 1997Date of Patent: July 9, 2002Assignee: University of PittsburghInventors: William E. Klunk, Jay W. Pettegrew, Chester A. Mathis, Jr.
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Patent number: 6395930Abstract: A method for enhancing the purity of a desired compound comprising: Step (a) treating a crude reaction product which contains at least one desired compound, unreacted starting materials and/or byproducts with at least one bifunctional quenching agent that is capable of selective covalent reaction with unwanted byproducts, or excess reagents; Step (b) allowing the quenching agent to covalently react with unreacted starting materials and/or byproducts to afford a derivatized compound of the quenching agent: and Step (c) isolating the desired compound is described as well as novel quenching agents and methods for their use in the rapid purification of synthetic intermediates and products in synthesis, combinatorial chemistry, and automated organic synthesis.Type: GrantFiled: May 25, 2000Date of Patent: May 28, 2002Assignee: Warner LambertInventor: Sham Nikam
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Patent number: 6395939Abstract: One aspect of the present invention relates to novel reaction conditions that allow the efficient synthesis of diaryl ethers from arenes bearing a leaving group and arenols under relatively mild conditions. Another aspect of the present invention relates to the dramatic effects of acidic activators on Ullmann-type couplings involving electron-poor and/or relatively insoluble substrates.Type: GrantFiled: October 5, 1998Date of Patent: May 28, 2002Assignee: Massachusetts Institute of TechnologyInventors: Jean-Francois Marcoux, Sven Doye, Stephen Buchwald
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Patent number: 6384273Abstract: The invention concerns a method for orthometalation of a carbocyclic aromatic derivative bearing at least an electron donor group, characterised in that it consists in reacting said carbocyclic aromatic derivative with an efficient amount of at least one alkaline metal in the presence of a compound of formula (I): RX, wherein: R represents a hydrocarbon radical having 1 to 20 carbon atoms which can be a saturated or unsaturated, linear or branched, acyclic aliphatic radical; a saturated or unsaturated, monocyclic or polycyclic cycloaliphatic radical; a saturated or unsaturated, linear or branched aliphatic radical bearing a cyclic substituent; and X represents a bromine or chlorine atom.Type: GrantFiled: January 24, 2001Date of Patent: May 7, 2002Assignee: Rhodia ChimieInventors: Virginie Pevere, Jean Roger Desmurs, Charles Mioskowski, Alain Wagner, Arnaud Gissot
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Patent number: 6376546Abstract: Compounds represented by general formula I or salts thereof, wherein n is an integer of 2 or 3; R represents a straight-chain or branched saturated alkyl group having 4 or 4 carbon atoms, a cyclopentyl group, a cyclohexyl group or the like, Y represents a hydroxyl or amino group, A represents a hydrogen atom, a hydroxyl, methoxy, nitro group or the like, Q represents a hydrogen atom or a hydroxyl or methoxy group. They can be formulated to give pharmaceutical compositions that are effective as prophylactic or therapeutic agents for allergic diseases associated with IgE production inhibitors or IgE antibodies.Type: GrantFiled: June 8, 2000Date of Patent: April 23, 2002Assignee: Asahi Kasei Kabushiki KaishaInventors: Motoshi Shoda, Hiromichi Itoh
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Patent number: 6369225Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: GrantFiled: August 29, 2000Date of Patent: April 9, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
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Patent number: 6365773Abstract: This invention describes processes for producing halomagnesium fluoroaryl carboxylates. In one such process, a fluoroaryl Grignard reagent is added to an anhydrous liquid ethereal medium pretreated with carbon dioxide.Type: GrantFiled: June 13, 2000Date of Patent: April 2, 2002Assignee: Albemarle CorporationInventors: Chi H. Cheng, Ronny W. Lin
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Patent number: 6342592Abstract: The invention relates to a method which comprises synthesising bifunctional compounds then chiral compounds from the bifunctional compounds, also to synthesising supports comprising these chiral compounds, and the use of these supports for preparing or separating enantiomers, or for asymmetric synthesis. The invention also relates to bifunctional compounds, their use as a source of functionalised polymers, and to the chiral compounds, also to the use of these chiral compounds in a chiral support in the form of a three-dimensional network or for separating or preparing enantiomers, principally for analytical or preparative chromatography, and in a support for the production of chiral molecules by asymmetric synthesis.Type: GrantFiled: March 16, 1998Date of Patent: January 29, 2002Assignee: Institut Francais du Petrole and ChiralsepInventors: Raphaël Duval, Hubert Leveque
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Publication number: 20020002290Abstract: 1Type: ApplicationFiled: June 14, 2001Publication date: January 3, 2002Applicant: Secretary of State for Defence in her Britannic Majesty's Government of the United KingdomInventors: Graeme P. Nicholson, Mark J. Kan, Gareth Williams, Michael G. Drew, Paul D. Beer
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Patent number: 6262293Abstract: &ohgr;-Cycloalkyl-prostaglandin E2 derivatives of formula (I) (wherein all symbols are as defined in the description); and non-toxic salts thereof, prodrugs thereof and cyclodextrin clathrates thereof. Compounds of formula (I) strongly bind on the EP2 subtype receptor. Therefore, they are useful for prevention and/or treatment of immunological diseases (autoimmune diseases, organ transplantation etc.), asthma, abnornmal bone formation, neuronal cell death, liver damage, abortion, premature birth or retina neuropathy of glaucoma etc.Type: GrantFiled: June 23, 2000Date of Patent: July 17, 2001Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kousuke Tani, Shuichi Ohuchida
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Patent number: 6187950Abstract: Compounds of the formula Y3(R4)—X—Y1(R1R2)—Z—Y2(R2)—A—B where the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid inverse agonist type biological activity.Type: GrantFiled: March 12, 1999Date of Patent: February 13, 2001Inventors: Tae K. Song, Min Teng, Roshantha A. Chandraratna
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Patent number: 6168776Abstract: Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing non-azo derivatives of Chrysamine G and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using non-azo Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using non-azo Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.Type: GrantFiled: April 18, 1997Date of Patent: January 2, 2001Assignee: University of PittsburghInventors: William E. Klunk, Jay W. Pettegrew, Chester A. Mathis, Jr.
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Patent number: 6162943Abstract: Process for the preparation of .alpha.-alkoxy-.alpha.-trifluoromethyl-arylacetic esters of the formula (I) ##STR1## wherein R is a component selected from the group consisting of C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.6 -C.sub.10 -aryl and C.sub.1 -C.sub.6 -halogenoalkyl, R' is selected from the group consisting of C.sub.1 -C.sub.4 -alkyl, X is selected from the group consisting of halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.4 -alkenyl, C.sub.6 -C.sub.10 -aryl or C.sub.1 -C.sub.4 -alkoxy and nitro, and n is zero or an integer from 1 to 3.Type: GrantFiled: April 16, 1999Date of Patent: December 19, 2000Assignee: Bayer AktiengesellschaftInventors: Norbert Lui, Albrecht Marhold
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Patent number: 6150412Abstract: The invention relates to compounds of formula (I) ##STR1## wherein R.sub.1 is an electronegative substituent, preferably nitro, cyano, formyl or carboxy, R.sub.2 is --A--R.sub.4, wherein A is a branched or straight chain C.sub.1-9 alkylene and R.sub.4 is carboxy or 5-tetrazolyl; R.sub.3 is an electronegative substituent, preferably nitro, cyano, halogen, formyl, carboxy, C.sub.1-5 alkyl carbonyl, aryl carbonyl or SO.sub.2 R.sub.6, wherein R.sub.6 is a branched or straight chain C.sub.1-5 alkyl, aryl alkyl, aryl or NR.sub.7 R.sub.8, wherein R.sub.7 and R.sub.8 are independently hydrogen, a branched or straight chain C.sub.1-5 alkyl or together form a C.sub.3-6 ring; or a pharmaceutically acceptable ester or salt thereof. The compounds are peripheral, long acting COMT (catechol-O-methyl transferase) inhibitors and are useful, e.g., in the treatment of Parkinson's disease and hypertension.Type: GrantFiled: November 21, 1997Date of Patent: November 21, 2000Assignee: Orion-yhtyma OyInventors: Jarmo Pystynen, Anne Luiro, Timo Lotta, Martti Ovaska, Jukka Vidgren
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Patent number: 6121460Abstract: Process for the preparation of an optically active N-acyl-indoline-2-carboxylic acid in which a mixture of enantiomers of N-acyl-indoline-carboxylic acid is contacted with an optically active resolving agent and the optically active N-acyl-indoline-2-carboxylic acid is liberated from the resulting diastereomeric salt, as resolving agent use being made of a compound of formula 1, where R.sub.1 represents an alkyl group and R.sub.2 a hetero-aryl group or where R.sub.1 and R.sub.2 together with the C atoms to which they are bound form a cycloalkyl group with 5-8 C atoms, fused with a hetero-aryl group.Type: GrantFiled: February 12, 1999Date of Patent: September 19, 2000Assignee: DSM N.V.Inventors: Andreas J. J. Hendrickx, Thijs Kuilman
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Patent number: 6103762Abstract: The invention concerns bi-aromatic compounds of formula (I) in which Ar represents (a), Z being O or S, R.sub.1 is --CH.sub.3, --CH.sub.2 --O--R.sub.6, --OR.sub.6 or --COR.sub.7 ; R.sub.2 is --OR.sub.8, --SR.sub.8 or a polyether radical if in the latter case R.sub.4 is C.sub.1 -C.sub.20 alkyl and is in ortho or meta position relative to X--Ar; R.sub.3 is alkyl or R.sub.2 and R.sub.3 together form a cycle optionally interrupted by O or S; R.sub.4 is aryl radical; R.sub.5 is H, halogen, C.sub.1 -C.sub.20 alkyl or --OR.sub.8 ; R.sub.6 is H, alkyl or --COR.sub.9 ; R.sub.7 is H, alkyl, --N(r')(r") or --OR.sub.10 ; R.sub.8 is H, alkyl or --COR.sub.9 ; R.sub.9 is alkyl; R.sub.10 is H, C.sub.1 -C.sub.20 alkyl, alkenyl, monohydroxyalkyl or polyhydroxyalkyl, aryl or aralkyl or a sugar residue, r' and r" are H, alkyl mono- or polyhydroxyalkyl, aryl, an amino acid or sugar residue or together form a heterocycle, X represents a radical of formula (d) or (e) in which R.sub.11 is H or --OR.sub.6 ; R.sub.Type: GrantFiled: March 23, 1999Date of Patent: August 15, 2000Assignee: Galderma Research & DevelopmentInventors: Jean-Michel Bernardon, Simon Trouille
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Patent number: 6046220Abstract: The invention relates to novel propynyl or dienyl biaromatic compounds which have the general formula (I) ##STR1## as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.Type: GrantFiled: January 26, 1998Date of Patent: April 4, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 5977117Abstract: Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (I): ##STR1## where X and Y are selected from groups that include O, S, and NH; and Ar.sup.1, Ar.sup.2 and Ar.sup.3 are independently selected from substituted or unsubstituted groups that include 5 to 6 membered aryl groups and heteraryl groups that contain one or two heteroatom(s). The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.Type: GrantFiled: January 23, 1996Date of Patent: November 2, 1999Assignee: Texas Biotechnology CorporationInventors: Ming Fai Chan, Vitukudi Narayanaiyengar Balaji, Rosario Silvestre Castillo, Adam Kois, Bore Gowda Raju, Chengde Wu
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Patent number: 5965741Abstract: The invention provides compounds of formula I: ##STR1## wherein A, B, D, X, R.sup.1, and R.sup.3 have any of the values defined in the specification, as well as N-oxides thereof, S-oxides thereof, pharmaceutically acceptable salts thereof, and in vivo hydrolizable esters and amides thereof, that are useful to relieve pain. The invention also provides pharmaceutical compositions as well as synthetic and therapeutic methods relating to such compounds.Type: GrantFiled: February 21, 1997Date of Patent: October 12, 1999Assignee: Zeneca LimitedInventors: Gloria Anne Breault, Howard Tucker, John Oldfield, Peter Warner
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Patent number: 5952382Abstract: Pharmaceutically/cosmetically-active adamantyl-substituted retinoid compounds have the structural formula (I): ##STR1## wherein Ar is a radical having one of the formula (a) - (d): ##STR2## and are useful for the treatment of disorders and/or ailments manifesting an overregulation of RAR receptors and/or a hypervitaminosis A.Type: GrantFiled: May 3, 1996Date of Patent: September 14, 1999Assignee: Centre International De Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 5929116Abstract: Novel cyclopentane derivatives are described which are endothelin receptor antagonists.Type: GrantFiled: October 13, 1995Date of Patent: July 27, 1999Assignee: SmithKline Beecham CorporationInventors: John Duncan Elliott, Deborah Lynne Bryan
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Patent number: 5925487Abstract: A toner resin composition comprising a toner resin and the metal salt or complex of a carbocyclic hydroxy caboxylic acid containing at least one methylene group optionally substituted by hydroxy or amino such as 4-(N-methyl-N-2-hydroxyethyl)aminomethyl-3-hydroxy-2-naphthoic acid. Iron and zinc salts are preferred.Type: GrantFiled: June 27, 1997Date of Patent: July 20, 1999Assignee: Zeneca LimitedInventors: David Melville Fawkes, Peter Gregory, James Stanley Campbell
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Patent number: 5925795Abstract: This invention relates to processes for the preparation of aryl-.beta.-diketones and aryl-pyrimidine ketones. In addition, this invention relates to the preparation of aryl-.beta.-triketones and dimethyl aminomethylene .beta.-diketones, which are useful as crop protection intermediates.Type: GrantFiled: September 16, 1996Date of Patent: July 20, 1999Assignee: Zeneca LimitedInventors: Raymond A. Felix, Hsiao-Ling M. Chin, Frank X. Woolard, David L. Lee
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Patent number: 5910605Abstract: The invention relates to a process for the preparation of 3-hydroxy-2-methylbenzoic acid and 3-acetoxy-2-methylbenzoic acid, which comprises reacting 3-chloro-2-methylphenol (3) with benzyl chloride to give 2-benzyloxy-6-chlorotoluene (4) subjecting this to a Grignard reaction with magnesium to give (3-benzyloxy-2-methylphenyl)magnesium chloride (5) reacting this with CO.sub.2 to give 3-benzyloxy-2-methylbenzoic acid (6) hydrogenating this or its alkali metal salts in the presence of a hydrogenation catalyst to give 3-hydroxy-2-methylbenzoic acid (2) and optionally acetylating this to give 3-acetoxy-2-methylbenzoic acid.Type: GrantFiled: February 6, 1998Date of Patent: June 8, 1999Assignee: Clariant GmbHInventors: Robert Cosmo, Andreas Dierdorf
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Patent number: 5834468Abstract: This invention relates to substituted and unsubstituted ???(aryl- and heteroaryl-) alkyl-, alkyloxy-, alkylthio-, oxo-, thio-, and alkylamino!- heteroaryl and aryl!- alkylamino-, aminoalkyl-, alkyloxy-, and alkylthio!- aryl and heteroaryl compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, which are useful as antagonists of the pain enhancing effects of E-type prostaglandins, to processes for the preparation of such compounds, to pharmaceutical compositions comprising such compounds, and to methods for treating pain comprising the administration of such compounds.Type: GrantFiled: July 2, 1996Date of Patent: November 10, 1998Assignee: Zeneca LimitedInventors: Gloria Anne Breault, John Oldfield, Howard Tucker, Peter Warner
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Patent number: 5792876Abstract: A process is described for producing acetals comprising reacting an aldehyde or a ketone with an alcohol in the presence of a titanium compound having an acetylacetone as a ligand, or in the presence of a compound selected from the group consisting of stannous chloride dihydrate, cerium chloride hexahydrate and bismuth chloride. The process can be used in the synthesis of unstable acetals or when water exists in the reaction mixture, and therefore the process can be used for a wide variety of applications.Type: GrantFiled: November 6, 1996Date of Patent: August 11, 1998Assignee: Kuraray Co., Ltd.Inventors: Hideharu Iwasaki, Masahiko Kitayama, Takashi Onishi
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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: 5753715Abstract: The invention relates to cyclohexenyl antibacterial compounds of the formula I: ##STR1## and pharmaceutical compositions containing the compounds, methods for their production and use.Type: GrantFiled: June 2, 1995Date of Patent: May 19, 1998Assignee: Ortho Pharmaceutical CorporationInventors: Robert H. Chen, Maud Urbanski, Min Xiang, John Francis Barrett
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Patent number: 5739374Abstract: 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: February 14, 1997Date of Patent: April 14, 1998Assignee: BASF AktiengesellschaftInventors: Bernd Janssen, Hans-Heiner Wuest
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Patent number: 5710194Abstract: The invention provides polymerizable dental, compounds, compositions, including the compounds and products for mixing the compositions and methods of using the compositions. Aryl acid compounds are provided in accordance with the invention. The compositions include at least one polymerizable aryl acid compound, an effective amount of a polymerization initiator, and at least 10 percent by weight of ceramic, metal and/or metal oxide filler particles having a particle size less than 500 microns. The dental products of the invention include a polymerizable composition in an enclosure having at least two chambers separated by a wall adapted to be ruptured prior to or during mixing of the composition. Compositions of the invention are preferred for use in these enclosures. Core build up material including a polymerizable acid containing compound is used to support dental crowns and adhere them to teeth in accordance with the invention.Type: GrantFiled: February 15, 1996Date of Patent: January 20, 1998Assignee: Dentsply Research & Development Corp.Inventors: Paul D. Hammesfahr, Kewang Lu, Paul A. Silver
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Patent number: 5705528Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein thyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: ##STR1## wherein R.sup.1 represents farnesyl, geranyl or geranyl-geranyl;Z represents C--R.sup.6 or N;R.sup.2 represents H, CN, the groups COOR.sup.7, SO.sub.3 R.sup.7, CONR.sup.7 R.sup.8 and SO.sub.2 NR.sup.7 R.sup.7, wherein R.sup.7 and R.sup.8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO.sub.3 M, wherein M is a cation;R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato;X represents O, S, SO, SO.sub.2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.Type: GrantFiled: November 10, 1994Date of Patent: January 6, 1998Assignee: Ramot University Authority for Applied Research & Industrial DevelopmentInventor: Yoel Kloog
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Patent number: 5705703Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein. the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds: the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: January 21, 1997Date of Patent: January 6, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
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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: RE39682Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein methyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: wherein R1represents farnesyl, geranyl or geranyl-geranyl; Z represents C—R6 or N; R2 represents H, CN, the groups COOR7, SO3R7, CONR7R8 and SO2NR7R7, wherein R7 and R8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO3M, wherein M is a cation; R3, R4, R5 and R6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato; X represents O, S, SO, SO2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.Type: GrantFiled: March 30, 2005Date of Patent: June 5, 2007Assignee: Ramot at Tel Aviv University Ltd.Inventor: Yoel Kloog