C-o- Group In R Patents (Class 514/622)
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Publication number: 20120289595Abstract: The present invention relates to a novel biarylamide derivative and a pharmaceutical composition or a cosmetic composition comprising the same as an active ingredient. More particularly, the present invention relates to a novel biarylamide derivative, a pharmaceutical composition or a cosmetic composition for preventing or treating a pigmentation disorder caused by an abnormal excess of melanin or a disease caused by melanocyte hyperplasia comprising the same as an active ingredient. The biarylamide derivative of the present invention inhibits melanin production and thus inhibits melanocyte hyperplasia. Therefore, a cosmetic composition comprising the biarylamide is excellent in a whitening effect, and a pharmaceutical composition comprising the biarylamide is effective in the prevention or treatment of pigmentation disorders of skin such as lentigo, melasma, freckle, etc. and malignant melanoma.Type: ApplicationFiled: July 25, 2012Publication date: November 15, 2012Applicant: Catholic University Industry Academy Cooperation FoundationInventor: Dong Heon Shin
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Patent number: 8309608Abstract: The present invention relates to the use of compounds which enhance the transcription of endothelial nitric oxide synthase (eNOS) for treating stem and progenitor cells in the cell therapy of patients with ischemic heart diseases such as coronary heart disease or ischemic cardiomyopathy. Treatment of such cells which are isolated from bone marrow, for example, with an eNOS transcription enhancer prior to their administration improves their functional activity and ameliorates neovascularization of the heart and cardiac regeneration.Type: GrantFiled: November 2, 2004Date of Patent: November 13, 2012Assignee: Sanofi-Aventis Deutschland GmbHInventors: Andreas Zeiher, Stefanie Dimmeler, Christopher Heeschen, Hartmut Ruetten
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Patent number: 8309606Abstract: The present invention provides compounds, pharmaceutical compositions and methods for treating, immuno-allergical diseases, autoimmune diseases, and organ or tissue rejection following transplantation.Type: GrantFiled: August 21, 2009Date of Patent: November 13, 2012Assignee: Novaremed LimitedInventor: Eliahu Kaplan
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Publication number: 20120283200Abstract: The present invention provides a pharmaceutical composition for preventing or treating a chronic heart disease, comprising a compound of a formula (I): wherein: R1 is one independently selected from a group consisting of a hydrogen, a methyl and an ethyl; R2 is one of a hydrogen and a methyl; and R3 is one selected from a group consisting of a hydrogen, (CH2)nAr and (CH2)nArR?R?, wherein n is one of 1 and 2, R? and R? is located at C-3 and C-4 positions, respectively, R? is a hydrogen and R? is one of a hydroxy, a fluorine, a bromine and a OMe, or R?+R?=—OCH2O—; or R2+R3 is one of wherein n is one of 4 and 5.Type: ApplicationFiled: March 27, 2012Publication date: November 8, 2012Applicants: CHINA MEDICAL UNIVERSITY, National Taiwan UniversityInventors: MING-JAI SU, YUEH-HSIUNG KUO
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Publication number: 20120283216Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Q is O or S; Z1 and Z2 are each independently CR9 or N; and R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: December 22, 2010Publication date: November 8, 2012Inventors: Alvin Donald Crews, JR., Amy X. Ding, Chi-Ping Tseng
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Publication number: 20120270946Abstract: The crystalline form A of Bimatoprost of formula I, its preparation method and use are provided. There are characteristic peaks where diffraction angles 2? are 3.2+0.2°, 5.5+0.2°, 11.4+0.2°, 16.7+0.2°, 17.6+0.2°, 19.9+0.2°, 20.8±02° and 22.8+0.2° in the X-ray powder diffraction pattern of the crystalline form A.Type: ApplicationFiled: July 30, 2010Publication date: October 25, 2012Applicant: SHANGHAI TECHWELL BIOPHARMACEUTICAL CO., LTD.Inventors: Bingming He, Zhijun Tang, Zhonghao Zhuo, Yunman Zheng, Xiaoliang Gao, Xiaoming Ji
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Patent number: 8293798Abstract: A compound of formula (I) or salts thereof, wherein R1, R2, R3, R4, n and X are as defined in the specification; a process for preparing such compounds, a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.Type: GrantFiled: October 30, 2008Date of Patent: October 23, 2012Assignee: Glaxo Group LimitedInventors: Alessandra Gaiba, Susan Roomans, Martin Edward Swarbrick
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Publication number: 20120264760Abstract: One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5?-monophosphate-dehydrogenase over human inosine-5?-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.Type: ApplicationFiled: June 6, 2012Publication date: October 18, 2012Applicants: University of Georgia Research Foundation, Inc., Brandeis UniversityInventors: Lizbeth K. Hedstrom, Boris Striepen
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Publication number: 20120263779Abstract: A drug delivery system (DDS) comprised of segmented biodegradable implants sized and suitable for implantation in an ocular region or site and methods for treating ocular conditions. The segmented implants provide an extended release of an active agent at a therapeutically effective amount for a period of time between 50 days and one year, or longer, and permit the DDS to have segments that possess individual and different drug release characteristics.Type: ApplicationFiled: June 13, 2012Publication date: October 18, 2012Inventors: Robert T. Lyons, James A. Burke, Michael R. Robinson
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Publication number: 20120263659Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.Type: ApplicationFiled: November 22, 2010Publication date: October 18, 2012Applicants: BASF SE, SYMRISE AGInventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel
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Patent number: 8288426Abstract: A composition comprising fenamidone (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.Type: GrantFiled: December 21, 2007Date of Patent: October 16, 2012Assignee: Bayer CropScience AGInventors: Heike Hungenberg, Wolfgang Thielert, Koen Van Den Eynde
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Publication number: 20120252891Abstract: Three unique subtypes of N-hydroxyamides and N-hydroxycarbamates containing both the vanilloid moiety (4-hydroxy-3-methoxybenzyl) and a lipophilic aliphatic moiety. Also disclosed are direct syntheses of these vanilloid fatty hydroxamates. The compounds possess inhibitory activity against the enzymes fatty acid amide hydrolase (FAAH) and matrix metallo-proteinase 9 (MMP-9). In addition, these substances bind to the calcium channel protein TRPV1 and inhibit vesicant-induced inflammation in skin and cornea. The compounds have utility in treating topical or systemic inflammatory processes in the skin and/or eye.Type: ApplicationFiled: March 16, 2012Publication date: October 4, 2012Applicants: University of Medicine and Dentistry of New Jersey, Lehigh University, Rutgers, The State University of New JerseyInventors: Jeffrey D. Laskin, Ned D. Heindel, Carl Jeffrey Lacey, Abhilash N. Pillai, Marion Gordon, Diane E. Heck
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Publication number: 20120251613Abstract: A method of stimulating melanogenesis in a skin surface of a patient, by treating the skin surface with a topical formulation comprising an effective amount of 17-phenyl-18,19,20-trinor-PGF2? ethyl amide in a dermatologically acceptable carrier. The topical formulation may be a cream, a gel, a lotion, a spray, an ointment, an aqueous solution, a nonaqueous solution, or a transdermal patch. The dermatologically acceptable carrier may contain an oily carrier or an aqueous carrier.Type: ApplicationFiled: July 29, 2011Publication date: October 4, 2012Applicant: AGILA SPECIALITIES PVT. LTD.Inventors: Rajeev JAIN, Tarun Narang, Satya Srinivas Chetlapalli
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Publication number: 20120238633Abstract: Biocompatible intraocular implants include a prostamide component and a biodegradable polymer that is effective in facilitating release of the prostamide component into an eye for an extended period of time. The prostamide component may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants may be placed in an eye to treat or reduce a at least one symptom of an ocular condition, such as glaucoma.Type: ApplicationFiled: May 8, 2012Publication date: September 20, 2012Applicant: ALLERGAN, INC.Inventor: Patrick M. Hughes
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Publication number: 20120232105Abstract: A pharmaceutical composition for inhibiting osteoclast growth is disclosed in the present invention. The pharmaceutical composition includes a compound represented by a formula (I), and a pharmaceutically acceptable salt and carrier: wherein R1, R2, R3, R4 can be one selected from a group consisting of hydrogen, halogen, C1?C10 alkyl group, C2?C10 alkynyl group, amino group, haloalkyl group and sulfonamide group.Type: ApplicationFiled: July 11, 2011Publication date: September 13, 2012Applicant: NATIONAL DEFENSE MEDICAL CENTERInventors: Deh-Ming CHANG, Hsu-Shan Huang
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Publication number: 20120232155Abstract: The invention relates to a novel hydroxyphenyl compound, to the preparation of the compound and intermediates used therein, to the use of the compound as an antibacterial medicament and pharmaceutical compositions containing the compound.Type: ApplicationFiled: November 11, 2009Publication date: September 13, 2012Inventors: Vincent Gerusz, Fabien Faivre, Mayalen Oxoby, Alexis Denis, Yannick Bonvin
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Publication number: 20120219611Abstract: Biocompatible intraocular implants include a prostamide component and a biodegradable polymer that is effective in facilitating release of the prostamide component into an eye for an extended period of time. The prostamide component may be associated with a biodegradable polymer matrix, such as a matrix of a two biodegradable polymers. The implants may be placed in an eye to treat or reduce a at least one symptom of an ocular condition, such as glaucoma.Type: ApplicationFiled: May 8, 2012Publication date: August 30, 2012Applicant: ALLERGAN, INC.Inventor: PATRICK M. HUGHES
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Publication number: 20120214858Abstract: Imidamide (amidine) analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumors.Type: ApplicationFiled: August 16, 2010Publication date: August 23, 2012Applicant: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. Macdonald, Thomas P. Mathews, Andrew Kennedy, Yugesh Kharel
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Publication number: 20120214782Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: August 17, 2011Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Gerald Juergen ROTH, Martin FLECK, Heike NEUBAUER, Bernd NOSSE
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Publication number: 20120202886Abstract: Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A, B, Z, X, R1 and R2 are as defined in the specification. Such compositions are used in treating the skin or scalp of a human or non-human animal. Bimatoprost is preferred for this treatment.Type: ApplicationFiled: April 6, 2012Publication date: August 9, 2012Applicant: ALLERGAN, INC.Inventors: David F. WOODWARD, Amanda M. VANDENBURGH
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Patent number: 8227643Abstract: This invention relates to bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable salts and their use in the modulation of Sirtuin 1 (Sirt1) and there use in neuroprotection for subject suffering from neurodegenerative diseases such as Alzheimer's disease, Huntington's disease, Amyotrophic lateral sclerosis, frontotemporal dementia, Parkinson's disease, including Parkinson's plus diseases such as multiple system atrophy, progressive supranuclear palsy, corticobasal degeneration and dementia with Lewy bodies, and in the manufacture of medicaments for such Sirt1 modulation and neuroprotection.Type: GrantFiled: January 12, 2010Date of Patent: July 24, 2012Assignee: ProteoTech, Inc.Inventors: Alan D. Snow, Qubai Hu, Judy A. Cam
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Publication number: 20120184553Abstract: The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.Type: ApplicationFiled: September 27, 2010Publication date: July 19, 2012Inventors: Paula Louise Nichols, Andrew John Eatherton, Paul Bamborough, Karamjit Singh Jandu, Oliver James Philps, Daniele Andreotti
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Publication number: 20120178747Abstract: The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm.Type: ApplicationFiled: November 14, 2006Publication date: July 12, 2012Inventors: Dianqing (Dan) Wu, Dakai Liu, James J. Donegan
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Publication number: 20120178749Abstract: The present invention generally relates to compounds to treat viral infections and methods of their use. In particular, compounds of the present invention inhibit the activity of NS1 protein, thereby mitigating viral infection and, in particular, influenza virus infection. Accordingly, NS1 protein inhibitors and methods of treatment that employ such inhibitors are contemplated by the present invention.Type: ApplicationFiled: February 21, 2012Publication date: July 12, 2012Inventors: Michael Roth, Beatriz Fontoura, Shuguang Wei, Neal Satterly
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Patent number: 8216971Abstract: The present invention relates to a pesticide composition intended for protecting plants, crops or seeds against phyto-pathogenic fungi or damaging insects, and the corresponding methods of treatment using the said composition. More precisely, the subject of the present invention is a pesticide composition based on propamocarb-HCl, an insecticide active substance and optionally a further fungicide active substance.Type: GrantFiled: December 21, 2007Date of Patent: July 10, 2012Assignee: Bayer Intellectual Property GmbHInventors: Koen van Den Eynde, Wolfgang Thielert, Heike Hungenberg
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Patent number: 8211882Abstract: The present invention discloses methods of modulating the activity of Group I mGluRs using a defined class of benzamide compounds. In one embodiment, methods of modulating the activity of mGluR1 are provided. In another embodiment, methods of modulating the activity of mGluR5 are provided. In still another embodiment, methods of simultaneously modulating the activities of both mGluR1 and mGluR5 are provided. The present invention also provides methods of treating diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of benzamide compounds. The present invention further provides methods of preventing diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of compounds.Type: GrantFiled: March 6, 2009Date of Patent: July 3, 2012Inventors: Richard Delarey Wood, William J Welsh, Sean Ekins, Ni Ai
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Publication number: 20120165293Abstract: The presently disclosed subject matter provides a method of synthesizing prostaglandins and prostaglandin analogs comprising the ring closing metathesis of compounds of Formula (I). Also provided are novel compounds of Formula (I) and Formula (II). In addition to their use as synthetic intermediates in the presently disclosed methods, compounds of Formula (II) can be used as prostaglandin and/or prostaglandin analog prodrugs.Type: ApplicationFiled: July 13, 2010Publication date: June 28, 2012Inventors: George Petros Yiannikouros, Panos Kalaritis, Chaminda Priyapushpa Gamage, Stephenie Bosse Abernathy
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Publication number: 20120165339Abstract: A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: wherein A1, A2 and A3 each independently represent an aryl group, a heterocyclyl group or the like, R1, R2 and R3 each independently represent a hydrogen atom, a C1-6 alkyl group or the like, X represents an oxygen atom or the like, and L represents a bond or the like.Type: ApplicationFiled: December 20, 2011Publication date: June 28, 2012Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Taro Terauchi, Ayumi Takemura, Yuji Kazuta, Fumihiro Ozaki, Takashi Doko, Yu Yoshida, Toshiaki Tanaka, Keiichi Sorimachi, Yoshimitsu Naoe, Carsten Beuckmann
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Patent number: 8206695Abstract: Effective enhancement of eyelash length and density can be obtained by topical applications of an active agent selected from a class of compounds consisting of synthetic prostaglandin agonists, polymers thereof and mixtures thereof preferably having the chemical formula of C24H35NO5, such as 7-[3.5-dihydroxy-2-(3-hydroxy-4phenoxy-but-1-enyl)-cyclopentyl]-hept-5-enoic acid ethylamide. Such active agents having a molecular weight of 417.54 can be employed in concentrations from 0.00075% to 0.03% by weight in mixtures with inactive ingredients, such as gels, oils, etc. Results are obtained by daily topical applications of active agent in such liquid mixtures (tinctures) at the roots of the lashes and/or lash follicles.Type: GrantFiled: October 10, 2007Date of Patent: June 26, 2012Assignee: La Canada Ventures, Inc.Inventor: Suan Lin
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Patent number: 8198332Abstract: The application discloses compounds of Formula I: wherein Q1, Q2, R1, R2, R3, and n are defined as described herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the subject compounds.Type: GrantFiled: August 12, 2009Date of Patent: June 12, 2012Assignee: Roche Palo Alto LLCInventor: Todd Richard Elworthy
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Publication number: 20120142771Abstract: The present invention provides a compound of formula (I) or a salt thereof, wherein R1, R2 and R3 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, bromine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R4 and R5 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R6 and R7 are independently selected from the group consisting of hydrogen atom, fluorine atom, methyl, ethyl, hydroxy group, and others; and R8 and R9 are independently selected from the group consisting of hydrogen atom, C1-6 alkyl, and others, which is useful as an agent for treating or preventing various types of epilepsy including partial seizures and/or generalized seizures.Type: ApplicationFiled: February 7, 2012Publication date: June 7, 2012Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Seiji IWAMA, Tomoyuki Tanaka, Nana Yajima
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Publication number: 20120142782Abstract: A composition comprising from 0.005% to 0.02% bimatoprost by weight and from 100 ppm to 250 ppm benzalkonium chloride, wherein said composition is an aqueous liquid which is formulated for ophthalmic administration is disclosed herein. A method which is useful in treating glaucoma or ocular hypertension related thereto is also disclosed herein.Type: ApplicationFiled: February 10, 2012Publication date: June 7, 2012Applicant: ALLERGAN, INC.Inventors: Chin-Ming Chang, James N. Chang, Rhett M. Schiffman, R. Scott Jordan, Joan-En Chang-Lin
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Publication number: 20120142783Abstract: A composition comprising from 0.005% to 0.02% bimatoprost by weight and from 100 ppm to 250 ppm benzalkonium chloride, wherein said composition is an aqueous liquid which is formulated for ophthalmic administration is disclosed herein. A method which is useful in treating glaucoma or ocular hypertension related thereto is also disclosed herein.Type: ApplicationFiled: February 10, 2012Publication date: June 7, 2012Applicant: ALLERGAN, INC.Inventors: Chin-Ming Chang, James N. Chang, Rhett M. Schiffman, R. Scott Jordan, Joan-En Chang-Lin
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Publication number: 20120122934Abstract: Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.Type: ApplicationFiled: May 18, 2011Publication date: May 17, 2012Inventors: Orion D. Jankowski, Kieron E. Wesson, Paul Mollard, William D. Shrader
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Publication number: 20120122989Abstract: Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A, B, Z, X, R1 and R2 are as defined in the specification. Such compositions are used in treating the skin or scalp of a human or non-human animal. Bimatoprost is preferred for this treatment.Type: ApplicationFiled: January 23, 2012Publication date: May 17, 2012Applicant: ALLERGAN, INC.Inventors: David F. Woodward, Amanda M. Vandenburgh
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Publication number: 20120122918Abstract: Compounds of formula (1) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)-Q.Type: ApplicationFiled: November 28, 2011Publication date: May 17, 2012Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTDInventors: David Ryall BROWN, Ian COLLINS, Lloyd George CZAPLEWSKI, David John HAYDON
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Publication number: 20120122976Abstract: The invention relates to a phosphate-free pharmaceutical composition which comprises at least one FP prostanoid receptor agonist and/or at least one prostamide receptor agonist and also citrate salts and/or citric acid.Type: ApplicationFiled: May 14, 2010Publication date: May 17, 2012Applicant: URSAPHARM ARZNEIMITTEL GMBHInventor: Frank Holzer
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PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF SALICYLANILIDES FOR TREATMENT OF HEPATITIS VIRUSES
Publication number: 20120108592Abstract: A new class of salicylanilides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: October 28, 2011Publication date: May 3, 2012Inventors: J. Edward Semple, Jean-Francois Rossignol -
Publication number: 20120108666Abstract: The invention relates to compounds and their use in treating cell proliferative disorders, more specifically Syk tyrosine kinase-mediated disorders.Type: ApplicationFiled: January 6, 2012Publication date: May 3, 2012Inventor: Eliahu Kaplan
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Publication number: 20120101087Abstract: The present invention relates to, in part, novel bisphenol compounds useful for the recognition, attachment and growth of unwanted biologics on natural and manmade surfaces. Another aspect of the invention relates to combinatorial libraries for producing the same. Another aspect of the invention relates to pharmaceutical formulations comprising the same.Type: ApplicationFiled: December 12, 2008Publication date: April 26, 2012Inventors: Randall S. Alberte, Robert D. Smith
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Publication number: 20120093742Abstract: A method of modulating the flavour of an orally-receivable product, such as a foodstuff, beverage, dentifrice or medicine, comprising the addition thereto of a flavour-modulating proportion of at least one compound of the formula I in which X is selected from CHOH, C?O, CH2—CO and CH?C(OH), Y is selected from C1-C7 linear and branched alkyl and CH2CH2OH, Z is selected from CH3 and a moiety of the formula II in which the wavy bond represents bond linking Z to X and R1 and R2 are selected from the possibilities (i) both hydrogen; (ii) independently OH and OCH3; and (iii) R1 and R2 together with their bonds to the phenyl ring form a ring of the formula —O—CH2—O—; such that, when Z is CH3, X is C?O and Y is CH2CH2OH.Type: ApplicationFiled: June 24, 2010Publication date: April 19, 2012Applicant: Givaudan S.A.Inventors: Abdelmajid Kaouas, Harry Renes, Alexander P. Tondeur, Cornelis Winkel
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Patent number: 8158682Abstract: This present invention relates to methods for treating or attenuating pain in a patient. Specifically, the invention provides a method for attenuating pain in proximity to the site of an open wound or surgical incision comprising instilling a pharmaceutical composition comprising a capsaicinoid into the wound or incision, allowing the pharmaceutical composition to dwell for a predetermined period of time, and aspirating the wound or incision to remove the pharmaceutical composition. The invention also provides a method for attenuating pain in proximity to a joint comprising intra-articularly injecting a pharmaceutical composition comprising a capsaicinoid into the joint, allowing the pharmaceutical composition to dwell for predetermined period of time, and aspirating the joint to remove the pharmaceutical composition. In certain embodiments of the invention, the capsaicinoid is capsaicin.Type: GrantFiled: September 14, 2009Date of Patent: April 17, 2012Assignee: Vallinex, Inc.Inventors: Lakshmi Sangameswaran, Susan Kramer
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Publication number: 20120077845Abstract: The present invention relates to methods for reducing testosterone levels by reduction of luteinizing hormone (LH) or independent of LH levels in a male subject and methods of treating, suppressing, reducing the incidence, reducing the severity, or inhibiting prostate cancer, advanced prostate cancer, and castration-resistant prostate cancer (CRPC) and palliative treatment of prostate cancer, advanced prostate cancer and castration-resistant prostate cancer (CRPC). The compounds of this invention suppress free or total testosterone levels to castrate levels which may be used to treat prostate cancer, advanced prostate cancer, and CRPC without causing bone loss, decreased bone mineral density, increased risk of bone fractures, increased body fat, hot flashes and/or gynecomastia.Type: ApplicationFiled: August 23, 2011Publication date: March 29, 2012Inventors: James T. DALTON, Mitchell S. STEINER, Ronald A. MORTON
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Publication number: 20120065247Abstract: Provided herein are compounds and methods for use in preventing or treating a viral infection mediated by a virus comprising an IRES-containing RNA molecule or cancer related to an increase or decrease in IRES-mediated translation of an RNA molecule. Also provided are methods of inhibiting or promoting IRES-mediated translation. Also provided are methods of screening for an agent that inhibits IRES-mediated translation.Type: ApplicationFiled: March 26, 2010Publication date: March 15, 2012Applicants: DiscoveryBiomed, Inc., The UAB Research FoundationInventors: Sunnie R. Thompson, Erik Mills Schwiebert, John H. Streiff
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Publication number: 20120059064Abstract: The present invention is directed to methods of modulating the activity of an isoform of manganese superoxide dismutase which is useful for the treatment of diseases such as neurodegenerative diseases and heart failure.Type: ApplicationFiled: June 28, 2011Publication date: March 8, 2012Applicant: MitoTek, LLCInventor: Paul Q. Anziano
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Publication number: 20120046293Abstract: The present invention relates to renin inhibitor compounds having the structure and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: October 10, 2011Publication date: February 23, 2012Applicant: Merck Frosst Canada Ltd.Inventors: CHRISTOPHER I. BAYLY, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
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Patent number: 8114898Abstract: Embodiments of the present invention are directed to compositions and methods for the treatment of purpura. Preferred compositions comprise an ? adrenergic receptor agonist selected from selective ?1 adrenergic receptor agonist, selective ?2 adrenergic receptor agonist, non-selective ?1/?2 adrenergic receptor agonist, agents with ?2 adrenergic receptor agonist activity and combinations thereof, in a pharmaceutically acceptable carrier in order to treat and improve the cosmetic appearance of hemorrhagic (purpuric) lesions in the skin.Type: GrantFiled: November 17, 2008Date of Patent: February 14, 2012Assignee: Allergan, Inc.Inventors: Stuart D. Shanler, Andrew Ondo
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Publication number: 20120022039Abstract: The invention relates to substituted indanes and derivatives thereof, to physiologically acceptable salts and physiologically functional derivatives thereof, to the production thereof, to drugs containing at least one substituted indane according to the invention or derivative thereof, and to the use of the substituted indanes according to the invention and to derivatives thereof as MCH antagonists.Type: ApplicationFiled: February 12, 2010Publication date: January 26, 2012Applicant: SANOFIInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Klaus Wirth
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Publication number: 20120015978Abstract: This invention provides well defined 6-alkyl or hydroxyalkyl-1-naphthamide or quinoline compounds for treating glaucoma or ocular hypertension.Type: ApplicationFiled: June 27, 2011Publication date: January 19, 2012Applicant: ALLERGAN, INC.Inventor: David W. Old
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Patent number: 8097759Abstract: A medicament having inhibitory activity against NF-?B activation, which comprises a compound represented by the following general formula (I) or a pharmacologically acceptable salt as an active ingredient: wherein X represents a connecting group, A represents hydrogen atom or acetyl group, E represents an aryl group or a heteroaryl group, and ring X represents an arene or a heteroarene.Type: GrantFiled: July 2, 2010Date of Patent: January 17, 2012Assignee: Institute of Medicinal Molecular Design, Inc.Inventors: Susumu Muto, Tatsuo Nagano, Tomomi Sotome, Akiko Itai