Nitrogen Or Sulfur In Phenolic Moiety Patents (Class 560/142)
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Patent number: 11213496Abstract: The disclosure provides a method for systemic delivery of a therapeutically effective amount of epinephrine to a subject comprising orally administering dipivefrin or a dipivefrin salt to the subject. The disclosure also includes a method of treatment of a disease amenable to treatment by in vivo delivery of systemic epinephrine comprising administering dipivefrin or a dipivefrin salt to a subject in need of in vivo delivery of systemic epinephrine. The disease can be a respiratory disorder, anaphylaxis, cancer, or a microbial infection. The disclosure also includes dipivefrin or dipivefrin HCl orally dissolving tablets.Type: GrantFiled: September 10, 2018Date of Patent: January 4, 2022Assignee: INSIGNIS THERAPEUTICS, INC.Inventor: Mingbao Zhang
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Patent number: 9650332Abstract: Provided is a compound of formula (II) as a prodrug of probucol, and a method for preparing the same, as well as a method for preventing or treating dyslipidemia with an effective amount of a compound of formula (II) to a subject in need thereof,Type: GrantFiled: June 16, 2016Date of Patent: May 16, 2017Inventor: Yong Xu
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Patent number: 8987262Abstract: The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.Type: GrantFiled: November 16, 2012Date of Patent: March 24, 2015Assignees: Universite de Bordeaux, Centre Hospitalier Universitaire de BordeauxInventors: Christine Leaute-Labreze, Eric Dumas De La Roque, Alain Taieb, Jean-Benoit Thambo
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Patent number: 8946456Abstract: The present invention regards an improved and industrially advantageous process for the preparation of the 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol intermediates, also called “feso chromenyl” and (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol, also called “(R)-feso deacyl”, which are in turn used in the synthesis of fesoterodine and in particular of fesoterodine fumarate. This process utilises reagents which are non-toxic and manageable at industrial level and enables obtaining a new stable and non-hygroscopic crystalline form of the key intermediate “(R)-feso deacyl”, called form B.Type: GrantFiled: April 29, 2011Date of Patent: February 3, 2015Assignee: Chemi S.p.A.Inventors: Umberto Ciambecchini, Stefano Turchetta, Lorenzo De Ferra, Maurizio Zenoni
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Publication number: 20140357678Abstract: A pharmaceutically acceptable salt, prodrug or derivative compound of the formula I, wherein R1 is selected from H, a (C1-C5) alkyl group and a COR4 group; R2 is selected from H, a (C1-C5) alkyl group and a COR5 group; R3 is selected from H, a (C1-C5) alkyl group, a (C1-C5)-O-alkyl group, a cycloalkyl of (C5-C6) carbon atoms, an aryl group, and an aryl (C1-C5) alkyl group wherein the aryl group can be an unsubstituted aryl or substituted with one or more R6 groups and an NHCOR5 group, or the R2 and R3 groups together with N may form a piperidine, morpholine or piperazine group; R4 is selected from H and a (C1-C5)alkyl group; R5 is selected from an aryl group unsubstituted or substituted with one or more R6, linear or branched(C1-C5) alkyl or pyridyne groups and a pyridine group; R6 is selected from (C1-C5)alkyl groups, halogen and nitro.Type: ApplicationFiled: January 10, 2013Publication date: December 4, 2014Inventors: Gerardo Burton, Javier Duran, David Martinez, Elvira Zini, Veronica Mora Munoz, Lucila Bertoncello
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Patent number: 8816001Abstract: This invention pertains to methods for producing homogeneous recombinant proteins that contain polymer initiators at defined sites. The unnatural amino acid, 4-(2?-bromoisobutyramido)phenylalanine of formula 1, was designed and synthesized as a molecule comprising a functional group further comprising an initiator for an atom-transfer radical polymerization (‘ATRP”) that additionally would provide a stable linkage between the protein and growing polymer. We evolved a Methanococcus jannaschii (Mj) tyrosyl-tRNA synthetase/tRNACUA pair to genetically encode this unnatural amino acid in response to an amber codon. To demonstrate the utility of this functional amino acid, we produced Green Fluorescent Protein with the unnatural amino acid initiator of formula 1 site-specifically incorporated on its surface (GFP-1).Type: GrantFiled: March 7, 2013Date of Patent: August 26, 2014Assignee: Franklin and Marshall CollegeInventors: Ryan A. Mehl, Krzysztof Matyjaszewski, Saadyah Averick
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Patent number: 8722937Abstract: The present invention provides N-alkylthio ?-lactams and disulfide compounds (e.g., alkyl-coenzyme A asymmetric disulfides or aryl-alkyl disulfides), compositions containing such compounds, and method of their use as anti-bacterial agents.Type: GrantFiled: February 27, 2007Date of Patent: May 13, 2014Assignee: University of South FloridaInventors: Edward Turos, Kevin D. Revell
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Patent number: 8618323Abstract: A composition comprising a polymer backbone and at least one side group, wherein the side group comprises a benzene ring-based chromophore comprising a ketone at the 1-position, a substituted or unsubstituted amino group at the 2-position, and an oxygen atom at the 3-position of the benzene ring. The chromophore is a kynurenine-based compound. Methods of making and using the composition are also provided. The composition can be used in an ophthalmic lens or device for protecting the retina by blocking UV rays and filtering violet rays.Type: GrantFiled: January 28, 2011Date of Patent: December 31, 2013Assignee: Benz Research and Development CorporationInventors: Patrick H. Benz, Jose A. Ors
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Publication number: 20130261259Abstract: This invention pertains to methods for producing homogeneous recombinant proteins that contain polymer initiators at defined sites. The unnatural amino acid, 4-(2?-bromoisobutyramido)phenylalanine of formula 1, was designed and synthesized as a molecule comprising a functional group further comprising an initiator for an atom-transfer radical polymerization (‘ATRP”) that additionally would provide a stable linkage between the protein and growing polymer. We evolved a Methanococcus jannaschii (Mj) tyrosyl-tRNA synthetase/tRNACUA pair to genetically encode this unnatural amino acid in response to an amber codon. To demonstrate the utility of this functional amino acid, we produced Green Fluorescent Protein with the unnatural amino acid initiator of formula 1 site-specifically incorporated on its surface (GFP-1).Type: ApplicationFiled: March 7, 2013Publication date: October 3, 2013Applicant: FRANKLIN AND MARSHALL COLLEGEInventors: Ryan A. Mehl, Krzysztof Matyjaszewski, Saadyah Averick
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Publication number: 20130079399Abstract: The present invention refers to the compounds corresponding to the following general formula (I): wherein: R?C4-C8 alkanoyl; and X?NH—R1 where R1?H, or an amine protecting group; and/or the pharmaceutically acceptable salts thereof. Preferred compounds according to the present invention are represented by the following formula (Ia): wherein: R?C4-C8 alkanoyl; and/or the pharmaceutically acceptable salts thereof. In a preferred embodiment, an object of the present invention is to provide 5-amino-2-(butyryloxy)benzoic acid and/or the pharmaceutically acceptable salts thereof, preferably hydrochloride salt. A further object of the present invention is represented by the use of the compounds of formula (Ia), in particular 5-amino-2-(butyryloxy)benzoic acid and/or pharmaceutically acceptable salts thereof, as a medicament and by the use thereof for the treatment of intestinal inflammatory diseases.Type: ApplicationFiled: November 21, 2012Publication date: March 28, 2013Applicant: SOFAR SPAInventor: Carla LABRUZZO
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Publication number: 20130079532Abstract: The present invention regards an improved and industrially advantageous process for the preparation of the 2-hydroxy-4-phenyl-3,4-dihydro-2H-chromen-6-yl-methanol intermediates, also called “feso chromenyl” and (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)phenol, also called “(R)-feso deacyl”, which are in turn used in the synthesis of fesoterodine and in particular of fesoterodine fumarate. This process utilises reagents which are non-toxic and manageable at industrial level and enables obtaining a new stable and non-hygroscopic crystalline form of the key intermediate “(R)-feso deacyl”, called form B.Type: ApplicationFiled: April 29, 2011Publication date: March 28, 2013Applicant: CHEMI S.P.A.Inventors: Umberto Ciambecchini, Stefano Turchetta, Lorenzo De Ferra, Maurizio Zenoni
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Patent number: 8389671Abstract: The present invention can provide a composition for optical members, which contains (a) a compound having one or more of any group selected from the group consisting of an acryloyl group, a methacryloyl group, an allyl group and a vinyl group and one or more ?-epithiopropyl groups in a molecule. In a preferable embodiment of the present invention, the composition for optical members further contains at least one compound selected from (b) a compound having one or more ?-epithiopropyl groups in a molecule while having no polymerizable unsaturated bond group, (c) an inorganic compound having a sulfur atom and/or a selenium atom, (d) a compound having one or more thiol groups in a molecule, (e) a compound having one or more amino groups in a molecule while having no heterocyclic ring, and (f) a compound having one or more of at least one group selected from the group consisting of a vinyl group, an acryloyl group, a methacryloyl group and an allyl group in a molecule.Type: GrantFiled: March 11, 2008Date of Patent: March 5, 2013Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Motoharu Takeuchi, Hiroshi Horikoshi, Hiroaki Tanaka, Hirohito Ishizuka
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Publication number: 20120322715Abstract: The storage stability of a serine hydrolase acting on ester bonds in a formulation without a protease can be improved by incorporating a serine protease inhibitor.Type: ApplicationFiled: January 4, 2011Publication date: December 20, 2012Applicant: NOVOZYMES A/SInventors: Lise Munch Mikkelsen, Tomas Tage Hansen, Esben Peter Friis
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Patent number: 8222296Abstract: Conjugates of a gamma-aminobutyric acid (GABA) compound or a glycine compound and an analgesic drug are disclosed. Further disclosed are pharmaceutical compositions containing these conjugates and uses thereof in the treatment of CNS-associated diseases or disorders, optionally in combination with a psychotropic drug.Type: GrantFiled: July 17, 2007Date of Patent: July 17, 2012Assignees: Ramot at Tel-Aviv University Ltd., Bar-Ilan University, BioLineRX Ltd.Inventors: Abraham Nudelman, Ada Rephaeli, Irit Gil-Ad, Abraham Weizman, Ran Lifshitz, Ilan Winkler
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Publication number: 20120108549Abstract: Apocynin derivative compounds, active pharmaceutical ingredients, dosage forms, and methods of use thereof as neuroprotectants in the brain of mammals.Type: ApplicationFiled: April 15, 2010Publication date: May 3, 2012Inventors: Balaraman Kalyanaraman, Joy Joseph, Anumantha Kanthasamy
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Patent number: 8168734Abstract: The invention relates to compounds represented by Formula (1): wherein Ra is independently halogen, cyano, —CF3, —CF2H, —CFH2, —OCF3, —OCF2H, —N?C?O, —N?C?S or alkyl having a carbon number of approximately 1 to approximately 20; in the alkyl, optional —CH2— may be substituted with —O—, —S—, —SO2—, —CO—, —COO—, —OCO—, —CH?CH—, —CF?CF— or —C?C—, and optional hydrogen may be substituted with halogen; Rb is fluorine or —CF3; A is independently 1,4-cyclohexylene, 1,4-cyclohexenylene, 1,4-phenylene, naphthalene-2,6-diyl, tetrahydronaphthalene-2,6-diyl, fluorene-2,7-diyl or bicyclo[2.2.Type: GrantFiled: February 23, 2011Date of Patent: May 1, 2012Assignees: JNC Corporation, Chisso Petrochemical CorporationInventor: Takashi Kato
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Patent number: 8143325Abstract: Absorbable polyurethanes, polyamides and polyester urethanes prepared from at least one compound selected from: or the diamines and diisocyanates thereof, wherein each X represents a member independently selected from —CH2COO— (glycolic acid moiety), —CH(CH3)COO— (lactic acid moiety), —CH2CH2OCH2COO— (dioxanone), —CH2CH2CH2CH2CH2COO— (caprolactone moiety), —(CH2)yCOO— where y is one of the numbers 2, 3, 4 or 6-24 inclusive, and —(CH2CH2O)z?CH2COO— where z? is an integer between 2 and 24, inclusive; each Y represents a member independently selected from —COCH2O— (glycolic ester moiety), —COCH(CH3)O— (lactic ester moiety), —COCH2OCH2CH2O— (dioxanone ester), —COCH2CH2CH2CH2CH2O— (caprolactone ester), —CO(CH2)mO— where m is an integer between 2, 3, 4 or 6-24 inclusive, —COCH2O(CH2CH2O)n— where n is an integer between 2 and 24, inclusive; R? is hydrogen, benzyl or an alkyl group, the alkyl group being either straight-chained or branched; p is an integer between 1 and 4, inclusive; and Rn represents one or moreType: GrantFiled: June 25, 2010Date of Patent: March 27, 2012Assignee: Bezwada Biomedical, LLCInventor: Rao S. Bezwada
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Publication number: 20110312890Abstract: This invention relates to pharmaceutical compounds and nutritional supplements that are acetylated derivatives of naturally occurring amino acids and acetylated derivatives of peptides derived from naturally occurring amino acids containing hydroxyl groups. They are as useful as anti-platelet drugs, and as nutritional supplements.Type: ApplicationFiled: August 1, 2011Publication date: December 22, 2011Applicant: SIGNATURE R&D HOLDINGS, LLCInventor: V. Ravi Chandran
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Publication number: 20110263545Abstract: The present invention provides hepatoprotectant acetaminophen mutual prodrugs, which have an acetaminophen moiety covalently linked to a second moiety that may act as a hepatoprotectant against acetaminophen hepatotoxicity. Additionally, acetaminophen mutual prodrugs may have improved water solubility which may provide better suitability for parenteral and other dosage forms relative to administration of acetaminophen. Also provided are methods of treating a disease or condition that is responsive to acetaminophen (such as fever, pain and ischemic injury) using hepatoprotectant acetaminophen mutual prodrugs, as well as kits and unit dosages.Type: ApplicationFiled: May 20, 2009Publication date: October 27, 2011Inventors: Naweed Muhammad, Keith R. Bley, Jeffrey Tobias
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Patent number: 8044235Abstract: A monomer is provided which is excellent in reactivity, can give high heat resistance and high refractive index, and has two or more polymerizable functional groups with different polymerization properties and an aromatic ring in the molecule. An industrial advantageous process for producing the monomer is also provided. The monomer is an aromatic isocyanate compound containing a (meth)acryloyl group, and is represented by Formula (I): wherein R1 is a single bond or a linear or branched alkylene group of 1 to 5 carbon atoms, R2 is a hydrogen atom or a methyl group, R3 is a single bond or a linear or branched alkylene group of 1 to 3 carbon atoms, X is independently a halogen atom or an electron-withdrawing group, m is an integer ranging from 0 to 4, n is an integer ranging from 1 to 3, and 1?m+n?5.Type: GrantFiled: March 15, 2006Date of Patent: October 25, 2011Assignee: Showa Denko K.K.Inventors: Kaneo Nozawa, Katsutoshi Ohno, Yotaro Hattori
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Patent number: 7919648Abstract: The invention relates to compounds represented by Formula (1): wherein Ra is alkyl or the like; Rb is fluorine or —CF3; A is 1,4-cyclohexylene, 1,4-phenylene or the like; Z is a single bond, alkylene or the like; Y is a single bond, alkylene or the like; and m and n are an integer of approximately 0 to approximately 5.Type: GrantFiled: December 7, 2006Date of Patent: April 5, 2011Assignees: Chisso Corporation, Chisso Petrochemical CorporationInventor: Takashi Kato
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Publication number: 20100273725Abstract: The present invention relates to photosensitizer compounds for use in cosmetic and therapeutic applications of photodynamic therapy. The compounds of the present invention are designed for topical application and are characterized by a low permeability to the stratum corneum (the outer skin layer of an individual) and/or a low allergenic potential. Surprisingly, such compounds have beneficial properties in the treatment of certain diseases and lack the undesired damages to healthy skin entailed by prior art compounds. ALA (5-aminolevulinic acid)-esters of body-owned, natural compound such as aminoacids, steroids, carbohydrades, alcohols are preferred, examples of photosensitizers of the present invention. The compounds of the present invention are used in the treatment of skin diseases such as psoriasis, sebaceous glands related conditions including acne, seborrhoic dermatitis, rosacea, skin cancer and precancer, as well as in cosmetic hair removal.Type: ApplicationFiled: December 12, 2008Publication date: October 28, 2010Inventors: Thomas Glanzmann, Jérôme Barge, Georges Wagnieres
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Publication number: 20100256231Abstract: The invention concerns novel derivatives of 3,3-diphenylpropylamines, methods for their preparation, pharmaceutical compositions containing the novel compounds, and the use of the compounds for preparing drugs. More particularly, the invention relates to novel prodrugs of antimuscarinic agents with superior pharmacokinetic properties compared to existing drugs such as oxybutynin and tolterodine, methods for their preparation, pharmaceutical compositions containing them, a method of using said compounds and compositions for the treatment of urinary incontinence, gastrointestinal hyperactivity (irritable bowel syndrome) and other smooth muscle contractile conditions.Type: ApplicationFiled: June 14, 2010Publication date: October 7, 2010Applicant: UCB Pharma GmbHInventors: Claus MEESE, Bengt SPARF
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Patent number: 7772352Abstract: Absorbable polyurethanes, polyamides and polyester urethanes prepared from at least one compound selected from: or the diamines and diisocyanates thereof, wherein each X represents a member independently selected from —CH2COO— (glycolic acid moiety), —CH(CH3)COO— (lactic acid moiety), —CH2CH2OCH2COO— (dioxanone), —CH2CH2CH2CH2CH2COO— (caprolactone moiety), —(CH2)yCOO— where y is one of the numbers 2, 3, 4 or 6-24 inclusive, and —(CH2CH2O)z?CH2COO— where z? is an integer between 2 and 24, inclusive; each Y represents a member independently selected from —COCH2O— (glycolic ester moiety), —COCH(CH3)O— (lactic ester moiety), —COCH2OCH2CH2O— (dioxanone ester), —COCH2CH2CH2CH2CH2O— (caprolactone ester), —CO(CH2)mO— where m is an integer between 2, 3, 4 or 6-24 inclusive, —COCH2O(CH2CH2O)n— where n is an integer between 2 and 24, inclusive; R? is hydrogen, benzyl or an alkyl group, the alkyl group being either straight-chained or branched; p is an integer between 1 and 4, inclusive; and Rn represents one or moreType: GrantFiled: October 20, 2005Date of Patent: August 10, 2010Assignee: Bezwada Biomedical LLCInventor: Rao S. Bezwada
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Publication number: 20100120912Abstract: Provided are nutraceutical or dietary supplemental compositions comprising esterified capsaicinoids. The esterified capsaicinoids may converted to the active parent capsaicinoid compound following enzymatic or chemical hydrolysis. In various embodiments, these esterified capsaicinoids have a higher lipophilicity, lipid solubility and result in less irritation to the stomach than the parent capsaicinoid, and hence may be included in certain dietary supplement formulations, including capsules, pills and tablets dietary supplement formulations. The dietary supplement compositions may be used for pain management in mammals in vivo and/or in the treatment of various pathological conditions in humans.Type: ApplicationFiled: October 30, 2009Publication date: May 13, 2010Applicant: Trinity Laboratories Inc.Inventors: Chandra Ulagaraj Singh, Rao Nulu Jagaveerabhadra
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Patent number: 7649114Abstract: The invention concerns a method for the isolation of a stereoisomer from a mixture comprising the two stereoisomers of the general formulae (I-A) and (I-A?) and/or the two stereoisomers of the general formulae (I-B) and (I-B?) in which R1, R2 and R3, identical or different, are selected from the group consisting of —H, —F, —Cl, —C1-C6-alkyl, —S—C1-C6-alkyl, —OH, —O—C1-C6-alkyl, —O—C1-C6-alkylenephenyl, —OCO—C1-C6-alkyl, —OCON(C1-C6-alkyl)2 and —O—SiR8R9R10 (in which R8, R9 and R10, identical or different, are —C1-C6-alkyl or -phenyl); R4 is —H or —C1-C6-alkyl; R5 is —C1-C6-alkyl; and R6 and R7, identical or different, are —H or —C1-C6-alkyl; or their salts with organic or inorganic acids; comprising the step (a) manipulating the mixture ratio of the stereoisomers in the mixture so that at least one of the stereoisomers is present in an enantiomeric excess.Type: GrantFiled: May 29, 2006Date of Patent: January 19, 2010Assignee: Gruenenthal GmbHInventors: Helmut Heinrich Buschmann, Wolfgang Hell
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Patent number: 7622604Abstract: A probucol or a probucol derivative can be efficiently converted to a monoester or monoether of probucol by reacting the free hydroxyl-containing probucol or a derivative thereof (by which is meant a probucol compound with at least one substituent that is different from that on the parent probucol molecule but which maintains the two free hydroxyl groups) with a Grignard reagent or a lithium reagent that produces a magnesium bromide or lithium salt of probucol or the probucol derivative. The probucol compound anion is then reacted with an ester or ether forming compound.Type: GrantFiled: September 13, 2007Date of Patent: November 24, 2009Assignee: Salutria Pharmaceuticals LLCInventor: M. David Weingarten
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Patent number: 7598419Abstract: Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.Type: GrantFiled: March 22, 2005Date of Patent: October 6, 2009Assignee: HSC Research and Development Limited PartnershipInventors: Chaim M. Roifman, Peter Demin, Andrew Freywald, Thomas Grunberger, Olga Rounova, Nigel Sharfe
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Publication number: 20090082590Abstract: The present invention provides a 4-mercaptophenyl ester of acetic acid, which is useful as a raw material for synthesizing a developer, etc., and a process for producing the same. The present invention provides a 4-mercaptophenyl ester of acetic acid represented by Formula (1); wherein Ac is an acetyl group, and R is a C1-4 alkyl group, and a process for producing the 4-mercaptophenyl ester of acetic acid having a step of reducing a 4-halosulfonylphenyl ester of acetic acid represented by Formula (2); wherein Ac is an acetyl group, R is a C1-4 alkyl group, and X is a halogen atom.Type: ApplicationFiled: April 26, 2006Publication date: March 26, 2009Applicant: SUMITOMO SEIKA CHEMICALS CO., LTD.Inventors: Koji Fujita, Sachio Iida, Mikio Yamamoto, Kohei Washizaki
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Patent number: 7345191Abstract: A method is described for the preparation of polymorphic forms of water-soluble derivatives of probucol compounds having the following formula where R1, R2, R3, R4, R5, R6, Z and Z? are defined herein.Type: GrantFiled: February 26, 2005Date of Patent: March 18, 2008Assignee: Cambrex Charles City, Inc.Inventors: Paul Alan Jass, Jason Scott Douglas
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Patent number: 7294737Abstract: Provided are methods for manufacturing compounds of Formula I wherein all substituents are described herein.Type: GrantFiled: April 20, 2005Date of Patent: November 13, 2007Assignee: AtheroGenics, Inc.Inventor: M. David Weingarten
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Patent number: 7294736Abstract: A method is described for the preparation of polymorphic forms of water-soluble derivatives of probucol compounds having the following formula where R1, R2, R3, R4, R5, R6, Z and Z? are defined herein.Type: GrantFiled: April 9, 2004Date of Patent: November 13, 2007Assignee: Cambrex Charles City, Inc.Inventors: Paul Alan Jass, Jason Scott Douglas
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Patent number: 7189870Abstract: This invention is in the area of methods and compositions for the inhibition of the expression of VCAM-1 and, in particular, for the treatment of diseases mediated by VCAM-1, including cardiovascular and inflammatory diseases.Type: GrantFiled: August 25, 2003Date of Patent: March 13, 2007Assignee: AtheroGenic, Inc.Inventor: Patricia K. Somers
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Patent number: 6864381Abstract: A process for preparing acyloxybenzenesulfonates by reacting a carboxylic acid derivative with a salt of a phenolsulfonic acid in the presence of an antioxidant, preferably 2,6-di-tert-butyl-4-methylphenol. The addition of such antioxidants gives a product having a high color quality.Type: GrantFiled: January 13, 2004Date of Patent: March 8, 2005Assignee: Clariant GmbHInventors: Alexander Lerch, Michael Seebach, Wolf-Dieter Mueller
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Patent number: 6858650Abstract: The present invention concerns highly pure, crystalline, stable compounds of novel derivatives of 3,3-diphenylpropylamines in the form of their salts, a method for the manufacture and highly pure, stable intermediate products. The method is in particular characterized by regio- and chemoselectivity and high yield. Salts of phenolic monoesters of 3,3-diphenylpropylamines are provided, that are particularly well-suited for use in pharmaceutical formulations. Preferred compounds are R-(+)-2-(3-diisopropylamino-1-phenyl-propyl)-4-hydroxymethylphenylisobutyrate ester hydrogen fumarate and R-(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenylisobutyrate ester hydrochloride hydrate. Furthermore, stable, crystalline intermediate products that are essential for obtaining the abovementioned salts are provided. A preferred intermediate product is R-(?)-3-(3-diisopropylamino-phenyl-propyl)-4-hydroxy-benzoic acid methyl ester.Type: GrantFiled: November 15, 2000Date of Patent: February 22, 2005Assignee: Schwarz Pharma AGInventor: Claus Meese
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Patent number: 6822113Abstract: A process for preparing acyloxybenzenesulfonates by reacting anhydrous phenolsulfonates with carboxylic acid derivatives comprises conducting the reaction with a salt of a phenolsulfonic acid which has a water content of less than 0.5% by weight and has been contacted with a substance having basic properties.Type: GrantFiled: May 8, 2003Date of Patent: November 23, 2004Assignee: Clariant GmbHInventors: Gerd Reinhardt, Peter Naumann, Alexander Lerch, Wolf-Dieter Mueller, Narayan D. Sadanani
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Patent number: 6790981Abstract: The invention relates to a process for the preparation of acyloxybenzenesulfonates starting from carbonyl halides and salts of phenolsulfonic acid which have a low water content. Surprisingly, it was discovered that acyloxybenzenesulfonates can be prepared in high yields and good grades, irrespective of the grade or reactivity of the phenolsulfonic acid derivative, if the reaction of the phenolsulfonic acid with an alkanecarboxylic acid derivative is carried out in an aliphatic or aromatic solvent in the presence of 0.5 to 25% by weight of a polyglycol ether.Type: GrantFiled: December 13, 2002Date of Patent: September 14, 2004Assignee: Clariant Finance (BVI) LimitedInventors: Wolf-Dieter Mueller, Peter Naumann
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Patent number: 6639096Abstract: Process for the preparation of acyloxybenzenesulfonates by reaction of phenolsulfonate with a water content of less than 0.5% by weight and alkanecarbonyl halide in a hydrocarbon as solvent and in the presence of a catalyst in the form of a basic nitrogen-containing compound.Type: GrantFiled: August 1, 2002Date of Patent: October 28, 2003Assignee: Clariant GmbHInventors: Gerd Reinhardt, Peter Naumann, Miriam Ladwig, Ina Golla, Torsten Pilz, Reto Wieduwilt, Henri Jourdan
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Patent number: 6624193Abstract: The present invention provides a prophylactic and therapeutic medicament for ophthalmic diseases, especially ophthalmic inflammatory diseases and corneal ulcer, comprising as an active ingredient a compound represented by the formula (I): or a pharmacologically acceptable salt or hydrate thereof.Type: GrantFiled: April 2, 2002Date of Patent: September 23, 2003Assignees: Ono Pharmaceutical Co., Ltd., Senju Pharmaceutical Co., Ltd.Inventors: Hiroaki Naka, Kazuhito Kawabata, Hideki Tokushige
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Publication number: 20030125577Abstract: A compound of the formula (I) 1Type: ApplicationFiled: November 4, 2002Publication date: July 3, 2003Inventors: Paul F. Corey, Steven W. Felman, Gary E. Rehm, Michael J. Pugia
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Publication number: 20030105148Abstract: The present invention provides, inter alia, triphenylethylene derivatives, such as, 3-{4-[6-(3-Methoxy-phenyl)-8,9-dihydro-7H-benzocyclohepten-5-yl]-phenyl}-acrylic acid, as selective estrogen receptor modulators. Also provided are methods for the treatment and/or prevention of estrogen stimulated diseases in mammals including breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as pharmaceutical compositions of the compounds of the present invention.Type: ApplicationFiled: August 9, 2002Publication date: June 5, 2003Inventors: Robert F. Kaltenbach, Simon P. Robinson, George L. Trainor
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Patent number: 6573297Abstract: A (2-substituted oxyphenyl)alkanamide derivative or a salt thereof expressed by the following Formula (I): wherein one of A and B is a hydrocarbon group of C3-30 expressed by R1 and the other is —(CH2)n-NR2R3; Z is —CO— or —CONR6—; R2 and R3 individually represent H, lower alkyl or benzyl, or —NR2R3 may be a heterocycle having 3-7 members; wherein —CONR5—(CH2)n-NR2R3 or —CONR6—(CH2)n-NR2R3 may be the following Group (II): wherein ring Y is a heterocycle of 6 or 7 members; R4 is selected from the group consisting of H, halogen, lower alkyl, lower acyl and etc; R5 and R6 are individually H, lower alkyl, lower acyl or lower alkylcarbamoyl, or may form a part of said Group(II); 1 is 0 or 1; m is 1 or 2; and n is an integer of 0-5.Type: GrantFiled: October 29, 2001Date of Patent: June 3, 2003Assignee: Shiseido Co., Ltd.Inventors: Koji Kobayashi, Hirotada Fukunishi, Tokuro Iwabuchi
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Publication number: 20030100698Abstract: Materials for dielectrics and/or buffer layers in microelectronics utilize polymers can be based on bis-o-nitrophenols. The bis-o-nitrophenols carry a tert-butoxycarbonyl group on at least one of the hydroxyl groups. The polybenzoxazoles prepared from these compounds have a lower dielectric constant than corresponding polymers which are prepared from bis-o-nitrophenols that do not have a tert-butoxycarbonyl group.Type: ApplicationFiled: September 16, 2002Publication date: May 29, 2003Inventor: Recai Sezi
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Publication number: 20030096992Abstract: The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide via a dicarboxylated salicylamide intermediate. The present invention also relates to dicarboxylic salicylamide delivery agent compounds for the delivery of active agents. Methods of administration are provided as well.Type: ApplicationFiled: September 20, 2002Publication date: May 22, 2003Inventors: Joseph N. Bernadino, Doris C. O'Toole, William E. Bay
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Patent number: 6566394Abstract: Salicylamide derivatives represented by formulae (1a) and (1b); intermediates in the production thereof; a process for producing the same; and drugs containing the same as the active ingredient. The salicylamide derivatives represented by formulae (1a) and (1b) are useful as anti-inflammatory agents and immunosuppressive agents which exert an effect of inhibiting the activation of NF-&kgr;B with little side effects.Type: GrantFiled: May 30, 2002Date of Patent: May 20, 2003Assignees: Mercian Corporation, Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Tomio Takeuchi, Kazuo Umezawa, Sakino To-E, Naoki Matsumoto, Tsutomu Sawa, Takeo Yoshioka, Naoki Agata, Shin-ichi Hirano, Kunio Isshiki
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Patent number: 6527690Abstract: The invention relates to a process for purifying and decolorizing a phenyl ester salt. The process combines a phenyl ester salt with a solvent to form a mixture and then stirs the mixture to form a slurry. The phenyl ester salt is substantially insoluble in this solvent. The process then collects the phenyl ester salt from the slurry. The collected phenyl ester salt may then be optionally dried or recrystallized. The collected phenyl ester salt is dissolved in a solvent to form a solution. The solution is decolorized and then spray dried to form a powder of the phenyl ester salt. As a result of the process the phenyl ester salt powder has a higher purity and an improved color as compared to the starting phenyl ester salt.Type: GrantFiled: June 4, 2001Date of Patent: March 4, 2003Inventors: Bhaskar Krishna Arumugam, Michael Eugene Burns, Dimmick Lee Bymaster, Jeffrey Scott DuPont, Robert Richard Dykstra, Robert Lee Eagan, Eddie Joseph Eckart, Jarvey Eugene Felty, Jr., Kevin John Fontenot, Jeffrey William Green, Shane Kipley Kirk, Gary Paul Lutz, Tony Lee Sander, Thomas Hugh Williams, George Chester Zima
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Patent number: 6476076Abstract: The present invention is related to new vanilloid analogues containing resiniferatoxin pharmacophores, pharmaceutical compositions comprising such analogues, and their uses as vanilloid receptor agonists and potent analgesics. The present invention provides a pharmaceutical composition for treating acute, chronic, inflammatory or neuropathic pains or for treating bladder hypersensitivity.Type: GrantFiled: August 20, 2001Date of Patent: November 5, 2002Assignees: Pacific Corporation, Digital Biotech Co., Ltd.Inventors: Jeewoo Lee, Uhtaek Oh, Young-Ho Park, Young-Ger Suh, Hyeung-Geun Park, Hee-Doo Kim
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Patent number: 6448442Abstract: The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents of formula I wherein n is 0 or 1, and where n is 1 each C6R5 moiety may be the same or different; X denotes a bond or a group providing a 1 to 7 atom chain linking two C6R5 moieties or, where n is 0, X denotes a group R; each group R is a hydrogen atom, an iodine atom or a hydrophilic moiety M or M1, two or three non-adjacent R groups in each C6R5 moiety being iodine and at least one R group in each C6R5 moiety being an M or M1 moiety; each M which may be the same or different, is a non-ionic hydrophilic moiety; and each M1 independently represents a —CHOHCON(R1)2 group wherein each R1, which may be the same or different, is a hydrogen atom, an OH group or a C1-6 alkoxy or optionally hydroxylated C1-5 alkyl group; at least one R group in the molecule being an M1 moiety; and isomers thereof.Type: GrantFiled: April 28, 2000Date of Patent: September 10, 2002Assignee: Amersham Health ASInventors: Torsten Almen, Fredrik Ek
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Publication number: 20020099096Abstract: This invention provides a novel class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds which are tissue-selective androgen receptor modulators (SARM), which are useful for oral testosterone replacement therapy, male contraception, maintaining sexual desire in women, treating prostate cancer and imaging prostate cancer. These agents have an unexpected in-vivo activity for an androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. These agents may be active alone or in combination with progestins or estrogens. The invention further provides a novel class of non-steroidal agonist compounds. The invention further provides compositions containing the selective androgen modulator compounds or the non-steroidal agonist compounds and methods of binding an androgen receptor, modulating spermatogenesis, treating and imaging prostate cancer, and providing hormonal therapy for androgen-dependent conditions.Type: ApplicationFiled: August 23, 2001Publication date: July 25, 2002Inventors: James T. Dalton, Duane D. Miller, Donghua Yin, Yali He
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Patent number: 6410775Abstract: aPL analogs that (a) bind specifically to B cells to which an aPL epitope binds and are disclosed. Optimized analogs lack T cell epitope(s) are useful as conjugates for treating aPL antibody-mediated diseases. Conjugates comprising aPL analogs and nonimmunogenic valency platform molecules are provides as are novel nonimmunogenic valency platform molecules and linkers. Methods of preparing and identifying said analogs, methods of treatment using said analogs, methods and compositions for preparing conjugates of said analogs and diagnostic immunoassays for aPL antibodies are disclosed.Type: GrantFiled: September 24, 1998Date of Patent: June 25, 2002Assignee: La Jolla Pharmaceutical CompanyInventors: Edward Jess Victoria, David Matthew Marquis, David S. Jones, Lin Yu