The Hetero Ring Is Substituted Patents (Class 514/465)
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Publication number: 20110152220Abstract: The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are TPH1 inhibitors or serotonin receptor antagonists.Type: ApplicationFiled: March 30, 2009Publication date: June 23, 2011Inventors: Gerard Karsenty, Patricia F. Ducy, Yuli Xie, Donald Landry, Vijay Kumar Yadav
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Patent number: 7943663Abstract: To provide a process and an apparatus by means of which a composition that contains episesamin in a concentration greater than 50 wt % on the basis of the sum weight of sesamin and episesamin can be produced conveniently and at high yield. There are provided a process and an apparatus which comprise the step of applying epimerization to sesamin or a sesamin-containing composition so that at least part of the sesamin is converted to episesamin and the step of selectively crystallizing episesamin by recrystallization and by means of which a composition that contains episesamin in a concentration greater than 50 wt % can be produced conveniently and at high yield.Type: GrantFiled: September 29, 2006Date of Patent: May 17, 2011Assignee: Suntory Holdings LimitedInventors: Yukihiro Aoshima, Masaaki Nakai, Kenji Katano, Asako Okada
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Publication number: 20110076244Abstract: The present invention relates to skin coating compositions and methods and, in particular, to coatings containing an active agent. In some embodiments, the coating may be applied to a skin surface and may be essentially colorless and transparent. In some aspects, the coating comprises a polymer and an active agent, and the polymer may be configured for sustained release of the active agent. In some aspects, the coating forms a barrier essentially impermeable to microorganisms yet permeable to water vapor. The coating may also be flexible and conformable to the surface. The coating may be applied to the skin using any suitable method. In some embodiments, the polymer and/or active agent are dissolved and/or suspended in an alcohol solvent. In some embodiments, the alcohol may function as an antiseptic on skin.Type: ApplicationFiled: September 24, 2010Publication date: March 31, 2011Applicant: Pharmasol CorporationInventor: James Donald Hammer
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Publication number: 20110059907Abstract: This invention relates to certain complexes of ascorbic acid and its derivatives with certain natural antioxidant and anti-inflammatory ketones for topical or oral application; said complexes having general chemical formula (I), its isomers, and salts thereof, including their optically active or racemic forms.Type: ApplicationFiled: November 16, 2010Publication date: March 10, 2011Applicant: Island Kinetics Inc.Inventors: SHYAM K. GUPTA, Linda Walker
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Patent number: 7902255Abstract: A ?-butyrolactone compound as shown in Formula (I) and pharmaceutical composition thereof: wherein X?N, O, S, Se; and A and B are selected from substituents having the following formula: wherein R1, R2, R3, R4, and R5 are selected from a hydrogen atom, a halogen atom, a hydroxyl group, a mercapto group, an amino group, an alkoxy group, and a nitro group. The ?-butyrolactone compound and pharmaceutical composition thereof butyrolactone have inhibitory effects on hepatoma, ovarian cancer, breast cancer, lung cancer, malignant glioblastoma or colorectal carcinoma, and are cytotoxic with high specificity to inhibit Paclitaxel-resistant tumor cells at later stage of chemotherapy without any damage on normal cells.Type: GrantFiled: February 17, 2009Date of Patent: March 8, 2011Assignee: Tzu Chi Buddhist General HospitalInventors: Shinn-Zong Lin, Horng-Jyh Harn
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Patent number: 7884128Abstract: Process for producing compound of Formula: wherein P2, P3 and R2 are the same as defined below, characterized by comprising reacting a compound represented by Formula (7): wherein P3 means a protecting group for hydroxy group; and Het means a 1-phenyl-1H-tetrazol-5-yl group, with a compound represented by Formula (8): wherein P2 means a protecting group for hydroxy group; and R2 means a phenyl group which may be substituted, in the presence of a base.Type: GrantFiled: April 21, 2010Date of Patent: February 8, 2011Assignee: Eisai R&D Management Co., Ltd.Inventors: Regina Mikie Kanada, Daisuke Ito, Takashi Sakai, Naoki Asai, Yoshihiko Kotake, Jun Niijima
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Patent number: 7846925Abstract: The present invention is related to azolidinedione-vinyl fused-benzene derivatives of formula (I) for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, graft rejection or lung injuries. Formula (I), wherein A, X, Y, Z, R1, R2 and n are as described in the description.Type: GrantFiled: July 10, 2003Date of Patent: December 7, 2010Assignee: Merck Serono SAInventors: Thomas Rueckle, Xuliang Jiang, Pascale Gaillard, Dennis Church, Tania Grippi Vallotton
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Publication number: 20100261735Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.Type: ApplicationFiled: June 24, 2010Publication date: October 14, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
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Publication number: 20100261675Abstract: Conventional many fungicidal compositions have had practical problems such that either a preventive effect or a curing effect is inadequate, the residual effect tends to be inadequate, or the controlling effect against plant diseases tends to be inadequate depending upon the application site, and a fungicidal composition to overcome such problems has been desired.Type: ApplicationFiled: June 24, 2010Publication date: October 14, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Yuji Nakamura, Shigeru Mitani, Tetsuo Yoneda
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Patent number: 7807142Abstract: Stabilized liquid polypeptide-containing pharmaceutical compositions are provided. The compositions comprise an amino acid base, which serves as the primary stabilizing agent of the polypeptide, and an acid and/or its salt form to buffer the solution within an acceptable pH range for stability of the polypeptide. Methods for increasing stability of a polypeptide in a liquid pharmaceutical composition and for increasing storage stability of such a pharmaceutical composition are also provided.Type: GrantFiled: December 5, 2005Date of Patent: October 5, 2010Assignee: Novartis Vaccines and Diagnostics, Inc.Inventors: Bao-Lu Chen, Maninder S. Hora
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Patent number: 7799954Abstract: Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.Type: GrantFiled: November 14, 2007Date of Patent: September 21, 2010Assignee: Abraxis BioScience, LLCInventors: Chunlin Tao, Qinwei Wang, Vuong Trieu, Neil Desai, Patrick Soon-Shiong
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Patent number: 7790758Abstract: This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositions containing the derivatives and processes for their preparation.Type: GrantFiled: February 13, 2006Date of Patent: September 7, 2010Assignee: Glaxo Group LimitedInventors: Daniele Andreotti, Luca Arista, Francesca Cardullo, Simone Spada, Kevin Michael Thewlis, Simon Edward Ward
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Patent number: 7763650Abstract: A new pharmaceutical compound for treating central nervous disorders, the compound comprising a therapeutically effective amount of valproic acid or pharmaceutically acceptable derivative thereof covalently bonded to myo-inositol. The invention also provides a composition, method for treating a patient and a method for obtaining the compound.Type: GrantFiled: March 15, 2006Date of Patent: July 27, 2010Assignees: Medipharma S.A., University Nacional De La PlataInventors: Luis Bruno-Blanch, Sung Chin Moon
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Patent number: 7754761Abstract: Therapeutic compounds and methods for inhibiting amyloid deposition in a subject, whatever its clinical setting, are described. Amyloid deposition is inhibited by the administration to a subject of an effective amount of a therapeutic compound comprising an anionic group and a carrier molecule, or a pharmaceutically acceptable salt thereof, such that an interaction between an amyloidogenic protein and a basement membrane constituent is inhibited. Preferred anionic groups are sulfonates and sulfates. Preferred carrier molecules include carbohydrates, polymers, peptides, peptide derivatives, aliphatic groups, alicyclic groups, heterocyclic groups, aromatic groups and combinations thereof.Type: GrantFiled: February 16, 2007Date of Patent: July 13, 2010Assignee: Bellus Health (International) LimitedInventors: Robert Kisilevsky, Walter A. Szarek, Donald F. Weaver
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Publication number: 20100137428Abstract: The present invention relates to compounds of formula (I), or salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof.Type: ApplicationFiled: December 21, 2005Publication date: June 3, 2010Inventors: Andrea Bozzoli, Clive Leslie Branch, Jacqueline Anne MacRitchie, Howard Robert Marshall, Roderick Alan Porter, Simone Spada
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Patent number: 7728020Abstract: The present invention relates to new amino acid derivatives, process for the production, their use, in particular in transplantation, and pharmaceutical compositions containing them.Type: GrantFiled: March 8, 2005Date of Patent: June 1, 2010Assignee: Novartis AGInventors: Klaus Hinterding, Klemens Högenauer
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Publication number: 20100076018Abstract: The invention features compositions and methods that are useful for treating or preventing AAT deficiency and associated conditions. In addition, the invention provides methods for identifying compounds useful for treatment of AAT deficiency and associated conditions.Type: ApplicationFiled: July 9, 2009Publication date: March 25, 2010Applicant: University of Florida Research Foundation, Inc.Inventors: Chen Liu, David A. Ostrov
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Patent number: 7683084Abstract: The invention relates to a series of thiazoline and oxazoline derivatives, compositions thereof, and methods of treating conditions and disorders using such compounds.Type: GrantFiled: June 27, 2007Date of Patent: March 23, 2010Assignee: Abbott LaboratoriesInventors: Ramin Faghih, Gregory A. Gfesser, Christopher L. Lynch, Murali Gopalakrishnan, Sujatha Gopalakrishnan, John Malysz, Earl J. Gubbins, Rachid El Kouhen, Jinhe Li, Kathy A. Sarris, Melissa J. Michmerhuizen, Ying Wang
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Publication number: 20100048686Abstract: It is an object of the present invention to discover that a perfume can change a person's temperature sense and humidity sense, to identify a perfume component that can change temperature sense, and to provide a perfume composition for controlling temperature sense that contains this perfume component, and to a sense control method or sense control article such as an aromatic or a cosmetic that is beneficial for controlling temperature sense, and to a perfume map for selecting a perfume suited to controlling temperature sense. The perfume composition is characterized in that a perfume component that changes the temperature subjectively sensed by a person (temperature sense) is contained, and that the perfume component that changes the temperature sense is a perfume component identified on the basis of a temperature image obtained from test subject assessment.Type: ApplicationFiled: August 24, 2009Publication date: February 25, 2010Applicant: SHISEIDO CO., LTD.Inventors: Ken Shoji, Sumie Taguchi, Yushi Terajima
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Publication number: 20090286872Abstract: Composition for oral consumption in the form of a substantially 5 homogeneous aqueous emulsion, suspension or dispersion comprising genistein and docosahexaenoic acid (DHA) and less than 1% by weight of soy protein, wherein the weight ratio of genistein to DHA is in the range of from 1:100 to 1:1, the composition comprises genistein in an amount of from 0.0001% to 0.1% by 10 weight and the genistein and DHA exhibit an anti-ageing effect on skin.Type: ApplicationFiled: April 10, 2007Publication date: November 19, 2009Inventors: John Casey, Gail Jenkins, Linda Jane Wainwright
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Publication number: 20090274650Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: ApplicationFiled: February 12, 2009Publication date: November 5, 2009Inventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
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Publication number: 20090247616Abstract: The present invention is a method for the treatment of anxiety and related disorders comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and formula (II) as herein defined. The present invention is directed to a method for the treatment of anxiety and related disorders, which includes mono-therapy and alternatively, co-therapy with at least one anxiolytic.Type: ApplicationFiled: March 26, 2008Publication date: October 1, 2009Inventor: Virginia L. Smith-Swintosky
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Publication number: 20090220454Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: February 26, 2009Publication date: September 3, 2009Applicant: Pharmacyclics, Inc.Inventors: Erik J. Verner, Joseph J. Buggy
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Publication number: 20090208426Abstract: The invention relates to the use of 2,5-diacetyl-3a,5,6,6a-tetrahydro-6a-hydroxy-2,3a,5-trimethylfuro[2,3-d]-1,3-dioxole (diacetyl trimer) of the formula in the form of one of its stereoisomers or in the form of a mixture consisting of or containing two or more of the stereoisomers (i) as an odoriferous or aromatic substance, (ii) for imparting, intensifying and/or modifying a creamy and/or fatty sensation in the mouth, (iii) for imparting, intensifying and/or modifying a sweet, buttery, cream-like and/or creamy flavour, and/or (iv) for masking a bitter flavour. The invention furthermore relates to corresponding aromatic compositions as well as compositions which serve for nutrition, oral hygiene, consumption for pleasure or for oral pharmaceutical use.Type: ApplicationFiled: November 30, 2005Publication date: August 20, 2009Applicant: SYMRISE GMBH & CO. KGInventors: Ian Gatfield, Jakob Ley, Ingo Reiss, Günter Kindel, Gerhard Krammer
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Publication number: 20090163583Abstract: To provide a process and an apparatus by means of which a composition that contains episesamin in a concentration greater than 50 wt % on the basis of the sum weight of sesamin and episesamin can be produced conveniently and at high yield. There are provided a process and an apparatus which comprise the step of applying epimerization to sesamin or a sesamin-containing composition so that at least part of the sesamin is converted to episesamin and the step of selectively crystallizing episesamin by recrystallization and by means of which a composition that contains episesamin in a concentration greater than 50 wt % can be produced conveniently and at high yield.Type: ApplicationFiled: September 29, 2006Publication date: June 25, 2009Inventors: Yukihiro Aoshima, Masaaki Nakai, Kenji Katano, Asako Okada
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Publication number: 20090012090Abstract: This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.Type: ApplicationFiled: September 10, 2008Publication date: January 8, 2009Inventors: Matthias Friebe, Peter Muschick, Andreas Huth
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Publication number: 20080311099Abstract: Methods for treating angina are described. A method for treating angina includes concurrently administering a compound with a therapeutic cardiovascular compound. A combination therapy employs suitable therapeutic cardiovascular compounds, such as a calcium channel blocker, a ?-adrenergic blocker, nitrates, partial fatty acid oxidation inhibitors, potassium channel activators, or a mixture thereof, in combination with a compound such as pyridoxal-5?phosphate, pyridoxic acid, pyridoxal, pyridoxamine, 3-acylated analogues of pyridoxal, 3-acylated analogues of pyridoxal-4,5-aminal, pyridoxine phosphonate analogues, a pharmaceutically acceptable acid addition salt thereof, or a mixture thereof. The invention also includes a novel composition comprising at least one compound and nitrates, partial fatty acid oxidation inhibitors, potassium channel activators, calcium channel blockers, ?-adrenergic blockers, or a mixture thereof.Type: ApplicationFiled: September 26, 2005Publication date: December 18, 2008Inventor: Albert Friesen
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Publication number: 20080312317Abstract: There provided a 12-membered-ring macrolactam derivative having antitumor activity: A compound represented by Formula (1) or a salt thereof. In this Formula, R1 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkylcarbonyl group or a C6-14 arylcarbonyl group; R2 is a hydrogen atom or a C1-6 alkyl group; R3 is a hydrogen atom or a hydroxyl group; R4 is a hydrogen atom or a hydroxyl group; R5 is a hydrogen atom or a C1-6 alkyl group; R6 is a hydrogen atom or a hydroxyl group; and R7 is an acetyl group or the like.Type: ApplicationFiled: April 10, 2008Publication date: December 18, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Masayuki Miyano, Daisuke Ito, Norio Murai
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Publication number: 20080255228Abstract: This invention relates to certain complexes of ascorbic acid and its derivatives with certain aryl alkyl ketones; said complexes having being formed via a kinetically-controlled process, and having general chemical formula (I) in FIG. 1. Said complexes can be in their various optically active or racemic forms. This invention also relates to a method of treatment of skin condition, including dark skin, age spots, acne, inflammation, loss of cellular antioxidants, collagen loss with aging, loss of skin pliability, loss of skin suppleness, skin wrinkles, oxidation, damage from radiation, malfunction of matrix metalloproteases, malfunction of tyrosinases, damage from free radicals, photo-damage, and combinations thereof; [FIG. 1].Type: ApplicationFiled: June 16, 2008Publication date: October 16, 2008Applicant: BIODERM RESEARCHInventor: SHYAM K. GUPTA
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Publication number: 20080194650Abstract: The invention provides well-defined aryl fluoroethyl ureas that are useful as selective alpha2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of alpha2 adrenergic receptors.Type: ApplicationFiled: December 5, 2007Publication date: August 14, 2008Inventors: Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Daniel W. Gil, Michael E. Garst
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Publication number: 20080176280Abstract: This invention relates to the field of biotechnology or genetic engineering. Specifically, this invention relates to the field of gene expression. More specifically, this invention relates to a novel ecdysone receptor/chimeric retinoid X receptor-based inducible gene expression system and methods of modulating gene expression in a host cell for applications such as gene therapy, large-scale production of proteins and antibodies, cell-based high throughput screening assays, functional genomics and regulation of traits in transgenic organisms.Type: ApplicationFiled: August 20, 2007Publication date: July 24, 2008Inventors: Marianna Zinovjevna Kapitskaya, Subba Reddy Palli
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Publication number: 20080153904Abstract: Synergistic and residual pesticidal compositions containing synergistic and residual mixtures of plant essential oils in admixture with enzyme inhibitors, with or without other compounds not previously used as active ingredients in pesticidal formulations. In addition, the present invention is directed to a method for controlling pests by applying a pesticidally-effective amount of the above synergistic and residual pesticidal compositions to a locus where pest control is desired.Type: ApplicationFiled: March 12, 2008Publication date: June 26, 2008Applicant: ECOSMART TECHNOLOGIES, INC.Inventor: Steven M. BESSETTE
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Patent number: 7288567Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: March 26, 2001Date of Patent: October 30, 2007Assignee: Methylgene Inc.Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg
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Patent number: 7241806Abstract: Synergistic and residual pesticidal compositions containing synergistic and residual mixtures of plant essential oils in admixture with enzyme inhibitors, with or without other compounds not previously used as active ingredients in pesticidal formulations. In addition, the present invention is directed to a method for controlling pests by applying a pesticidally-effective amount of the above synergistic and residual pesticidal compositions to a locus where pest control is desired.Type: GrantFiled: October 31, 2005Date of Patent: July 10, 2007Assignee: Ecosmart Technologies, Inc.Inventor: Steven M. Bessette
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Patent number: 7238726Abstract: Synergistic and residual pesticidal compositions containing synergistic and residual mixtures of plant essential oils in admixture with enzyme inhibitors, with or without other compounds not previously used as active ingredients in pesticidal formulations. In addition, the present invention is directed to a method for controlling pests by applying a pesticidally-effective amount of the above synergistic and residual pesticidal compositions to a locus where pest control is desired.Type: GrantFiled: October 31, 2005Date of Patent: July 3, 2007Assignee: Ecosmart Technologies, Inc.Inventor: Steven M. Bessette
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Patent number: 7202247Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.Type: GrantFiled: December 19, 2002Date of Patent: April 10, 2007Assignee: AtheroGenics, Inc.Inventors: James A. Sikorski, Charles Q. Meng, M. David Weingarten
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Patent number: 7199148Abstract: The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(?O)—, —O—C(?O)—, —NR8—C(?O)—, —O—C1-6alkanediyl-C(?O)—, —NR8—C1-6alkanediyl-C(?O)—, —S(?O)2—, —O—S(?O)2—, —NR8—S(?O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(?O), carboxyl, aminoC(?O), mono- or di(C1-4alkyl)aminoC(?O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5a and R5b is C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl or C1-6alkyl, optionally substituted on one or more atoms; R5a and R5b may also be hydrogen, aryl, Het1, Het2; R6 is hydrogen or C1-6alkyl optionally substituted on one ore more carbon atoms.Type: GrantFiled: August 14, 2003Date of Patent: April 3, 2007Assignee: Tibotec Pharmaceuticals LtdInventors: Abdellah Tahri, Piet Tom Bert Paul Wigerinck
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Patent number: 7192965Abstract: Compounds of formula wherein A1, A2 and A3 are each independently of the others a bond or a C1–C6alkylene bridge; A4 is a C1–C6alkylene bridge; D is CH or N; W is, for example, O, NR7 or S; T is, for example, a bond, O, NH or NR7; Q is O, NR7, S, SO or SO2; Y is O, NR7, S, SO or SO2; X1 and X2 are each independently of the other fluorine, chlorine or bromine; R1, R2 and R3 are, for example, H, halogen, CN, nitro, C1–C6alkyl, C1–C6haloalkyl, C1–C6alkylcarbonyl or C2–C6alkenyl; R4 is, for example, H, halogen, CN, nitro or C1–C6alkyl; R5 and R6 are, for example, H, CN, OH, C1–C6alkyl, C3–C8cycloalkyl, C3–C8cycloalkyl-C1–C6alkyl, C1–C6haloalkyl, C1–C6alkoxy or C1–C6haloalkoxy; R7 is H, C1–C6alkyl, C1–C6alkoxyalkyl or C1–C6alkylcarbonyl; k, when D is nitrogen, is 1, 2 or 3; or, when D is CH, is 1, 2, 3 or 4; and m is 1 or 2; and, where applicable, their possible E/Z isomers, E/Z isomeric mixtures and/or tautomers, in each case in free form or in salt form, a process for the preparation of those compounds andType: GrantFiled: June 27, 2003Date of Patent: March 20, 2007Assignee: Syngenta Crop Protection, Inc.Inventors: Werner Zambach, Peter Renold, Arthur Steiger, Stephan Trah, Roger Graham Hall
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Patent number: 7179839Abstract: The present invention relates to acylated indanyl amines according to the general formula (I) wherein R1–R4 have the meanings given in the description, A is CH2, CHOH or CH—(C1–C3-alkyl), B is CH2 or CH—(C1–C3-alkyl), and R5 is an aryl or heteroaryl group, possibly substituted by the substituents listed in the description.Type: GrantFiled: February 13, 2002Date of Patent: February 20, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Hartmut Strobel, Paulus Wohlfart, Alena Safarova, Armin Walser, Teri Suzuki, Karl Schönafinger
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Patent number: 7157495Abstract: Compositions comprising bis-tetrahydrofuran benzodioxyolyl sulfonamide compounds that are surprisingly effective protease inhibitors and a second antiretroviral compound are disclosed. Methods of inhibiting retrovirus proteases, in particular multi-drug resistant retrovirus proteases, methods of treating or preventing infection or disease associated with retrovirus infection in a mammal, and methods of inhibiting viral replication are also disclosed.Type: GrantFiled: June 25, 2003Date of Patent: January 2, 2007Assignees: Tibotec Pharmaceuticals, Ltd., The United States of America as represented by the Department of Health and Human ServicesInventors: Guangyang Wang, Michael Eissenstat, John W. Erickson, Piet T. B. P. Wigerinck
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Patent number: 7144909Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subcllinical hyperthyrodism and liver diseases.Type: GrantFiled: January 30, 2002Date of Patent: December 5, 2006Assignee: Karo Bio ABInventors: Johan Malm, Erik Flöistrup, Spiros Grivas, Yi-Lin Li
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Patent number: 7115596Abstract: The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the ?v?3 and/or the ?v?5 integrin without significantly inhibiting the ?v?6 integrin.Type: GrantFiled: December 19, 2003Date of Patent: October 3, 2006Assignee: Pharmacia CorporationInventors: John A. Wendt, Heather Stenmark, Hongwei Wu, Yaping Wang, Barbara B. Chen, Thomas D. Penning, Victoria L. Downs, Mark L. Boys, Mark Russell, Dale P. Spangler
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Patent number: 7090853Abstract: An adjuvant composition comprising noscapine and its derivatives, for use in the treatment of tumors, cancer, as an adjuvant for vaccines.Type: GrantFiled: November 6, 2002Date of Patent: August 15, 2006Assignee: Emory UniversityInventors: Judith Kapp, Yong Ke
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Patent number: 7084136Abstract: A compound of the formula (I): wherein A is alkylene optionally having an unsaturated bond; R is —C(?O)—R1; R1 is hydroxy or the like; m is 0 or 1; p is 0 or 1; X1 and X3 are each independently optionally substituted aryl or optionally substituted heteroaryl or the like; X2 is a bond, —CH2—, —S—, —SO2—, —CH2—O—, —O—CH2—, —CH2—S—, —S—CH2—, or the like; X4 is —CH2—, —CH2—CH2—, —C(?O)—, or the like, having a dual antagonistic activity against both a thromboxane A2 receptor and a prostaglandin D2 receptor is found.Type: GrantFiled: May 28, 2001Date of Patent: August 1, 2006Assignee: Shionogi & Co., Ltd.Inventors: Norihiko Tanimoto, Akinori Arimura
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Patent number: 7078541Abstract: Certain benzofuran derivatives are useful in the treatment of certain ischemic or inflammatory conditions, as well as neuroinflammation, neurodegeneration or degenerative diseases in which mitochondrial dysfunction leads to tissue degeneration. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: GrantFiled: September 17, 2003Date of Patent: July 18, 2006Assignee: Galileo Pharmaceuticals, Inc.Inventors: Sekhar Boddupalli, Gail Walkinshaw, Bing Wang
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Patent number: 7078565Abstract: Disclosed are phenyl-alkylene benzamides useful as orexin antagonistsType: GrantFiled: October 30, 2002Date of Patent: July 18, 2006Assignee: SmithKline Beecham plcInventors: Wai Ngor Chan, Amanda Johns, Roderick Alan Porter, Rachel Elizabeth Anne Stead, Mythily Vimal
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Patent number: 7045545Abstract: The present invention provides serotonergic aminoalkylbenzofurans of Formula (I): where R, R1, R2, R3, R4, R4?, R5, R5?, and R12 are as described in the specification.Type: GrantFiled: January 19, 2000Date of Patent: May 16, 2006Assignee: Eli Lilly and CompanyInventors: Karin Briner, Joseph Paul Burkhart, Timothy Paul Burkholder, Matthew Joseph Fisher, William Harlan Gritton, Daniel Timothy Kohlman, Sidney Xi Liang, Shawn Christopher Miller, Jeffrey Thomas Mullaney, Yao-Chang Xu, Yanping Xu
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Patent number: 7037914Abstract: A peroxisome proliferator activated receptor regulator containing a carboxylic acid derivative of formula (I) (wherein all symbols are as defined in the specification), a non-toxic acid thereof or a hydrate thereof as active ingredient. Because of having an effect of regulating PPAR, a compound of formula (I) is useful as a hypoglycemic agent, a hypolipidemic agent, a preventive and/or a remedy for diseases associating metabolic disorders (diabetes, obesity, syndrome X, hypercholesterolemia, hyperlipoproteinemia, etc.), hyperlipemia, atherosclerosis, hypertension, circulatory diseases, overeating, coronary heart diseases, etc., an HDL cholesterol-elevating agent, an LDL cholesterol and/or VLDL cholesterol-lowering agent and a drug for relief from risk factors of diseases or syndrome X.Type: GrantFiled: September 23, 2002Date of Patent: May 2, 2006Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Hisao Tajima, Yoshisuke Nakayama, Daikichi Fukushima
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Patent number: 7034015Abstract: The invention relates to a novel class of aminobenzophenones derivatives, to pharmaceutical preparations comprising said compounds, to dosage units of such preparations, to methods of treating patients comprising administering said compounds, and to the use of said compounds in the manufacture of pharmaceutical preparations.Type: GrantFiled: August 28, 2002Date of Patent: April 25, 2006Assignee: Leo Pharma A/SInventors: Erik Rytter Ottosen, Anne Marie Horneman, Xifu Liang
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Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang