R Contains Benzene Ring Patents (Class 514/617)
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Patent number: 8563594Abstract: Disclosed herein are compositions and methods for treating pain using S1P3 receptor inhibitors.Type: GrantFiled: May 7, 2008Date of Patent: October 22, 2013Assignee: Allergan, Inc.Inventors: John E. Donello, Richard L. Beard, Fabien J. Schweighoffer
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Patent number: 8557872Abstract: This present disclosure relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present disclosure provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.Type: GrantFiled: January 28, 2009Date of Patent: October 15, 2013Assignee: Amorepacific CorporationInventors: Song Seok Shin, Jin Kwan Kim, Sun-Young Kim, Ki-Wha Lee, Byoung Young Woo, Joo-Hyun Moh, Yeon Su Jeong, Kyung Min Lim, Jin Kyu Choi, Hyun-Ju Koh, Young-Ho Park
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Patent number: 8557800Abstract: The invention relates to substituted adamantane compounds, pharmaceutical compositions thereof, processes for their preparation, and methods for inhibiting sphingosine kinase and for treating or preventing hyperproliferative disease, inflammatory disease, or angiogenic disease.Type: GrantFiled: October 19, 2011Date of Patent: October 15, 2013Assignee: Apogee Biotechnology CorporationInventors: Charles D. Smith, Kevin J. French, Yan Zhuang
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Publication number: 20130267571Abstract: The present application provides a terpene analogue of Formula (I) or a pharmaceutically acceptable isomer, salt or ester thereof, and methods and uses thereof for treating neurological conditions such as pain in general and neuropathic pain. These terpene analogues can also be used to treat other electrical disorders in the central and peripheral nervous system. Also provided are methods of synthesizing the terpene analogues of Formula I.Type: ApplicationFiled: September 14, 2011Publication date: October 10, 2013Applicant: NeuroQuest Inc.Inventors: Mark A. Reed, Donald Weaver, Shengguo Sun, Alexander McLellan, Erhu Lu
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Patent number: 8552065Abstract: 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: GrantFiled: July 25, 2012Date of Patent: October 8, 2013Assignee: Catholic University Industry Academy Cooperation FoundationInventor: Dong Heon Shin
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Publication number: 20130261133Abstract: The compounds of the invention exhibit antiprotozoal, antimicrobial, and anticancer properties that are useful for the treatment or prevention of infections or cancer in a patient (e.g., a human). For example, the compounds and methods described herein can be used for the treatment or prevention of protozoal infections such as leishmaniasis, malaria, and trypanosoma infections, bacterial infections such as S. aureus and C. albicans, and cancers such as breast, colon, lung, or prostate cancer. The invention further provides methods of synthesizing such compounds as well as kits useful for administering the compounds.Type: ApplicationFiled: March 14, 2013Publication date: October 3, 2013Applicant: The University of MontanaInventors: John Howard Hoody, David Brian Bolstad
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Patent number: 8546451Abstract: The present invention relates to methods of treating androgen deprivation therapy (ADT) induced hot flashes and severe hot flashes in a subject.Type: GrantFiled: February 23, 2010Date of Patent: October 1, 2013Assignee: GTx, Inc.Inventors: James T. Dalton, Mitchell S. Steiner, Jeetendra Eswaraka
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Patent number: 8541466Abstract: A method for treating hair loss in mammals uses compositions containing prostaglandin F analogs. The compositions can be applied topically to the skin. The compositions can arrest hair loss, reverse hair loss, and promote hair growth.Type: GrantFiled: August 4, 2009Date of Patent: September 24, 2013Assignee: Duke UniversityInventors: Mitchell Anthony DeLong, John McMillan McIver, Robert Scott Youngquist
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Patent number: 8530465Abstract: The invention provides a series of novel 1,2-disubstituted amido-anthraquinone derivatives. Further, the invention also provides the preparation method and application of said derivatives, said application comprises: said derivatives with therapeutically effective amount are prepared into pharmaceutical compositions for inhibition of cancer cell growth, further treating cancer.Type: GrantFiled: August 1, 2012Date of Patent: September 10, 2013Assignee: National Defense Medical CenterInventors: Hsu-Shan Huang, Chia-Chung Lee
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Patent number: 8530457Abstract: Treatment of lymphangioleiomyomatosis with the MEK1/2 inhibitor CI-1040 delayed the development of primary tumors and blocked the estrogen-induced lung metastases in treated animals. Such treatment also reduced the number of circulating ELT3 cells and decreased their lung colonization after intravenous injection.Type: GrantFiled: May 20, 2009Date of Patent: September 10, 2013Assignee: Fox Chase Cancer CenterInventors: Elizabeth Petri Henske, Jane Yu
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Publication number: 20130231351Abstract: Compounds are disclosed which inhibit SIR2 base exchange more than deacetylation, thus enhancing SIR2 deacetylation activity. Methods of using the compounds for enhancing SIR2 deacetylation activity and increasing longevity of an organism are also disclosed. Methods for screening for compounds that enhance SIR2 deacetylation activity and increase longevity of an organism are additionally disclosed.Type: ApplicationFiled: January 23, 2013Publication date: September 5, 2013Applicant: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Vern L. Schramm, Anthony A. Sauve
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Patent number: 8519000Abstract: Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly used for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital, and gastrointestinal diseases.Type: GrantFiled: May 14, 2008Date of Patent: August 27, 2013Assignee: Newron Pharmaceuticals S.p.A.Inventors: Piero Melloni, Alessandra Restivo, Emanuela Izzo, Simona Francisconi, Elena Colombo, Cibele Sabido-David
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Patent number: 8519001Abstract: 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: GrantFiled: May 18, 2011Date of Patent: August 27, 2013Assignee: Edison Pharmaceuticals, Inc.Inventors: Orion D. Jankowski, Kieron E. Wesson, Paul Mollard, William D. Shrader
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Patent number: 8513455Abstract: The present invention relates to a crystalline oxybutynin base and process for preparing the same. Further, this invention discloses a process for preparing an acid addition salt of oxybutynin employing the crystalline oxybutynin base.Type: GrantFiled: February 4, 2009Date of Patent: August 20, 2013Assignee: Matrix Laboratories LimitedInventors: Purna Chandra Ray, Madhuresh Sethi, Sanjay Mahajan, Om Dutt Tyagi
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Patent number: 8507723Abstract: Aspects of the present invention relate to compounds and methods useful in modulating angiogenesis and methods of treating or preventing diseases associated with angiogenesis by administering a polycationic compound. The present invention relates to methods of use and compositions for inhibiting angiogenesis-mediated disorders in mammals including animals and humans. Additionally, this invention relates to the combined use of polycations with other anti-angiogenesis agents for the treatment of different angiogenesis-mediated disorders. Additionally, those polycationic compounds can be used with various anti-inflammatory and cytotoxic agents as well as with radio-therapeutic agents in cancer patients to prevent and treat tumor growth and metastasis.Type: GrantFiled: June 21, 2012Date of Patent: August 13, 2013Assignee: Polymedix, Inc.Inventors: Shaker Mousa, Dahui Liu
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Compositions and methods for targeted ablation of mutational escape of targeted therapies for cancer
Patent number: 8501167Abstract: Provided herein are compositions and methods for targeted ablation of mutational escape in the face of cancer therapeutic agents. Compositions comprising the yeast-based vehicles are used in combination with other cancer therapeutic agents.Type: GrantFiled: January 17, 2008Date of Patent: August 6, 2013Assignee: GlobeImmune, Inc.Inventors: David Apelian, Alex Franzusoff, Timothy C. Rodell -
Publication number: 20130195937Abstract: A method for preventing or treating a brain nervous disease includes administering to a subject in need thereof a therapeutically effective amount of a carbon nanotube, wherein the nervous disease is a brain disease or a traumatic central nervous system injury. The composition of the present invention enables patients to recover from physical damage to the brain, exhibits superior efficacy for inhibiting the onset of Parkinson's disease and strokes in animal models for Parkinson's disease and strokes, and the cytotoxic effects of beta amyloid in beta amyloid toxicity tests. Therefore, the composition of the present invention can be effectively used in the preparation of medicine for protecting cranial nerves, therapeutic agents for preventing or treating brain disease, or therapeutic agents for treating traumatic injuries to the central nervous system.Type: ApplicationFiled: July 14, 2011Publication date: August 1, 2013Applicant: BRAINGUARD CO., LTD.Inventors: Yoonhwa Jeong, Hyun Jung Lee, Do Yeon Lee, Yoo Hun Noh, Do Hee Kim, Ok Hyeon Kim, Ji Ae Park, Jiwon Lee
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Publication number: 20130178466Abstract: The invention provides compositions, medicaments and methods of treating microbial infections, and especially respiratory disorders caused by microbial infections. In particular, the invention relates to the treatment of respiratory diseases caused by pathogenic infections using certain either alkyl substituted or un-substituted 2-aryl acetic acid, or 2-aryl, N-hydroxyacetamide derivatives, or pentoxifylline, and to the use of these compounds in methods of treatment.Type: ApplicationFiled: November 9, 2010Publication date: July 11, 2013Applicant: BIOCOPEA LIMITEDInventors: Robin Mark Bannister, Wilson Caparros Wanderlay, John Brew
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Publication number: 20130172388Abstract: Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.Type: ApplicationFiled: December 14, 2012Publication date: July 4, 2013Applicant: University of Pittsburgh -- Of the Commonwealth System of Higher EducationInventor: University of Pittsburgh -- Of the Commonwealth System of Higher Education
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Publication number: 20130165505Abstract: Administration of certain 1-phenylalkanecarboxylic acid derivatives is useful for improving Cognitive Function; treating Cognitive Impairment, in particular Mild Cognitive Impairment; and preventing and/or reducing the risk of developing Alzheimer's Disease in a cognitively normal subject.Type: ApplicationFiled: December 21, 2012Publication date: June 27, 2013Applicant: Chiesi Farmaceutici S.p.A.Inventor: Chiesi Farmaceutici S.p.A.
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Publication number: 20130158112Abstract: A pharmaceutical composition for inhibiting amyloid beta peptide in a subject includes a compound having the formula (I): where M is selected from a substituted or unsubstituted alkyl, halo, alkoxy, aryl, cyclic, or heterocyclic group; p is an integer from 0-3; X1 is a 3-9 atoms in length linker connecting A and B; B is selected from a substituted or unsubstituted aryl, alkoxy or amine group; and a pharmaceutically acceptable salt thereof; and a pharmaceutical carrier.Type: ApplicationFiled: June 20, 2012Publication date: June 20, 2013Inventors: Jonathan D. Smith, Enakshi Chakrabarti, Subrata Ghosh, Marti Sayre, Gregory Tochtrop
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Patent number: 8460635Abstract: Synthetic peptidomimetic derivatives and phenyl group derivatives of Fenretinide (4-HPR) are disclosed, as are their uses as therapeutic, diagnostic and imaging agents for cancer and other diseases.Type: GrantFiled: March 11, 2009Date of Patent: June 11, 2013Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Ganjam V. Kalpana, Bhaskar C. Das
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Publication number: 20130144250Abstract: A method of treatment, such as treating an estrogen-related disorder or a psychotic disorder, by implanting a reservoir-based drug delivery composition into a subject to systemically deliver a therapeutically effective amount of an active pharmaceutical ingredient (such as an aromatase inhibitor or risperidone) to the subject for a long period of time (e.g., one month or one year). The drug delivery composition may include a rate-controlling excipient (e.g., an elastomeric polymer) defining a reservoir containing at least one discrete solid dosage form (e.g., one or more pellets), which includes an active pharmaceutical ingredient and optionally, a sorption enhancer.Type: ApplicationFiled: October 24, 2012Publication date: June 6, 2013Applicant: Endo Pharmaceuticals Solutions Inc.Inventor: Endo Pharmaceuticals Solutions Inc.
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Patent number: 8455549Abstract: The present invention relates to the use of a particular group of carbonylamino derivatives for the treatment or alleviation of a disease or condition relating to certain inflammatory disorders.Type: GrantFiled: August 21, 2008Date of Patent: June 4, 2013Assignee: Aniona ApsInventors: Lars Siim Madsen, Palle Christophersen
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Publication number: 20130136704Abstract: An object of the present invention is to provide a novel technology for preventing crystal precipitation of p-menthane-3,8-diol, and stable products utilizing this technology. Provided is a p-menthane-3,8-diol isomer mixture, wherein the mass ratio of cis isomers:trans isomers in terms of the relative configuration at Positions 3 and 4 is 55:45 to 45:55. Also provided are stable products and the like containing the p-menthane-3,8-diol isomer mixture.Type: ApplicationFiled: November 27, 2012Publication date: May 30, 2013Applicant: TAKASAGO INTERNATIONAL CORPORATIONInventor: TAKASAGO INTERNATIONAL CORPORATION
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Patent number: 8450309Abstract: A method and solution for perioperatively inhibiting a variety of pain and inflammation processes during arthroscopic procedures. The solution preferably includes a vasoconstrictor that exhibits alpha-adrenergic activity and one or more additional pain and inflammation inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. The solution is applied by continuous irrigation of a wound during a surgical procedure for peripheral vasoconstriction and inhibition of pain and/or inflammation while avoiding undesirable side effects associated with systemic application of larger doses of the agents.Type: GrantFiled: March 14, 2011Date of Patent: May 28, 2013Assignee: Omeros CorporationInventors: Gregory A. Demopulos, Pamela Pierce Palmer, Jeffrey M. Herz
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Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals
Patent number: 8445530Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: October 1, 2012Date of Patent: May 21, 2013Assignee: SanofiInventors: Matthias Schaefer, Josef Pernerstorfer, Dieter Kadereit, Hartmut Strobel, Werngard Czechtizky, L. Charlie Chen, Alena Safarova, Aleksandra Weichsel, Marcel Patek -
Patent number: 8445011Abstract: Methods and compositions for reducing the frequency of urination are disclosed. One method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising an analgesic agent formulated in a delayed-release formulation. Another method comprises administering to a subject in need thereof an effective amount of a pharmaceutical composition comprising multiple active ingredients. Yet another method comprises administering to a subject in need thereof an effective amount of a diuretic followed with another administration of an pharmaceutical composition comprising an analgesic agent.Type: GrantFiled: July 27, 2012Date of Patent: May 21, 2013Assignee: Wellesley Pharmaceuticals, LLCInventor: David A. Dill
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Publication number: 20130123356Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof,Type: ApplicationFiled: October 18, 2012Publication date: May 16, 2013Applicant: UNIVERSITY COLLEGE LONDONInventors: Masahiro Okuyama, David Selwood, Cristina Visintin, David Baker, Gareth Pryce
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Publication number: 20130123326Abstract: The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds.Type: ApplicationFiled: January 4, 2013Publication date: May 16, 2013Applicants: REGION MIDTJYLLAND, AARHUS UNIVERSITETInventors: AARHUS UNIVERSITET, REGION MIDTJYLLAND
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Publication number: 20130121919Abstract: The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject.Type: ApplicationFiled: June 11, 2012Publication date: May 16, 2013Applicant: The Trustees of Columbia University in the City of New YorkInventors: Yan FENG, Mauro Fa, Ottavio Arancio, Shi Xian Deng, Donald W. Landry, Yitshak Francis
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Patent number: 8440711Abstract: The present invention relates to (R,S) 2-aryl-2-fluoropropanoic acids, their single enantiomers (R) and (S), their derivatives amides and acylsulfonamides and to pharmaceutical compositions containing them, which are used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonucleated neutrophils (PMN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the treatment of damages caused by ischemia and reperfusion.Type: GrantFiled: December 18, 2007Date of Patent: May 14, 2013Assignee: Dompe Pha.r.ma S.p.A.Inventors: Marcello Allegretti, Andrea Aramini, Maria Candida Cesta
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Publication number: 20130116227Abstract: Disclosed is a novel biaryl amide derivative represented by formula (1) and having an affinity for the aldosterone receptor; also disclosed is a pharmaceutically acceptable salt thereof. (In the formula, A is any of the groups represented by formula (a); L is —CONH—, etc.; R1 is a substitutable aminosulfonyl group, etc.; R2 is a hydrogen atom, etc.; R3 is a hydrogen atom, etc.; R4 is a hydrogen atom, a halogen atom, hydroxy group, a substitutable amino group, a substitutable C1-6 alkoxy group, a substitutable 4- to 7-membered cyclic amino group, etc.; R5a, R5b and R5c are each independently hydrogen atoms, etc.; R6 is a halogen atom, a cyano group, etc.; R7 and R8 are each independently a hydrogen atom, etc.; and m is an integer such as 0.Type: ApplicationFiled: July 12, 2011Publication date: May 9, 2013Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Seiji Katayama, Seiji Hori, Futoshi Hasegawa, Kuniko Suzuki
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Patent number: 8436207Abstract: Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, or NHSO2X, wherein X is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, heterocycle, or substituted heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.Type: GrantFiled: September 21, 2011Date of Patent: May 7, 2013Assignee: Burnham Institute for Medical ResearchInventor: Maurizio Pellecchia
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Patent number: 8431600Abstract: Use of carboxamides of the formula (I) in which A, R1, M, Q and R are as defined in the description for controlling certain rust fungi, such as soya bean rust and coffee rust, in crop protection.Type: GrantFiled: May 26, 2006Date of Patent: April 30, 2013Assignee: Bayer CropScience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Herbert Gayer, Jörg Nico Greul, Ulrike Wachendorff-Neumann, Peter Dahmen, Ingo Wetcholowsky, Haruko Sawada, Hiroyuki Hadano
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Patent number: 8426644Abstract: 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: GrantFiled: June 28, 2011Date of Patent: April 23, 2013Assignee: MitoTek, LLCInventor: Paul Q. Anziano
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Patent number: 8404738Abstract: The present invention provides compounds of formula or pharmaceutically acceptable salts, esters or stereoisomers thereof, wherein R1 to R4, A and Y have the meanings given herein, as well as methods for making those compounds and their use as medicament, in particular as medicament for the treatment of cancer.Type: GrantFiled: January 17, 2012Date of Patent: March 26, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Jason Christopher Wong, Zhenshan Zhang
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Patent number: 8404891Abstract: The present invention concerns a liquid formulation that is stable to oxidation and that is based on paracetamol in an aqueous solvent obtainable by the following steps: (i) dissolving in a reaction vessel paracetamol in an aqueous solvent having a temperature between 65° C. and 95° C., and having pH between 5.0 and 6.0; (ii) cooling the solution so formed to a temperature equal to or above 35° C. and below 40° C. under an atmosphere of nitrogen; (iii) adding cysteine hydrochloride and sodium hydroxide simultaneously to the solution without stirring; (iv) closing the reaction vessel, and stirring the solution of step iii) in a nitrogen atmosphere. It further relates to a method for preparing the formulation.Type: GrantFiled: September 3, 2010Date of Patent: March 26, 2013Assignee: Neogen N.V.Inventor: Khaled Al Dandachi Atassi
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Patent number: 8383682Abstract: A composition comprises surface-modified nanoparticles of at least one amphoteric metal oxide or oxyhydroxide. The nanoparticles bear, on at least a portion of their surfaces, a surface modification comprising (i) at least one surface modifier selected from lactate, thiolactate, and mixtures thereof, and (ii) at least one surface modifier selected from halide, nitrate, acetate, carbonate, formate, propionate, sulfate, bromate, perchlorate, tribromoacetate, trichloroacetate, trifluoroacetate, carboxylate comprising from one to about four alkyleneoxy moieties, chlorate, and mixtures thereof.Type: GrantFiled: December 16, 2008Date of Patent: February 26, 2013Assignee: 3M Innovative Properties CompanyInventor: Timothy D. Dunbar
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Publication number: 20130045178Abstract: The invention provides in part dialkoxybenzene and eugenol compounds for controlling infestation by a Lymantria dispar, and methods thereof. The compounds include a compound of Formula I: where R1 may be methyl, ethyl, propyl, n-butyl, isopentyl (3-methylbutyl) or allyl; R2 may be at positions 2, 3 or 4 and may be H, methyl, ethyl, propyl, n-butyl, isopentyl (3-methylbutyl) or allyl; and R3 may be optionally present at positions 2, 3 and 4, and is allyl; with the provisos that when R2 is at position 2, R3 if present is at position 3, or when R2 is at position 3, R3 if present is at positions 2 or 4, or when R2 is at position 4, R3 if present is at position 2; or of Formula II: where R1 may be methyl, ethyl, propyl, n-butyl, isopentyl (3-methylbutyl) or allyl; or mixtures thereof.Type: ApplicationFiled: August 22, 2012Publication date: February 21, 2013Inventors: ERIKA PLETTNER, Yongmei Gong, Regine Gries
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Publication number: 20130040998Abstract: Fluorinated deacetylase inhibitors of the general formulae (I), (II), and (III): and pharmaceutically acceptable salts thereof, as described herein, are useful as inhibitors of histone deacetylases or other deacetylases, and thus are useful for the treatment of various diseases and disorders associated with acetylase activity as described herein (e.g., cancer, neurodegenerative diseases, inflammatory diseases).Type: ApplicationFiled: January 5, 2011Publication date: February 14, 2013Applicants: Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard CollegeInventors: James Elliot Bradner, Ralph Mazitschek
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Publication number: 20130039960Abstract: The present invention provides drug therapy formulations. In some embodiments, the present invention provides combinations of pharmaceutical agents (e.g., stimulant and non-stimulant), pharmaceutical formulations (e.g., nanoparticulate, non-nanoparticulate, etc.), and release profiles (e.g., immediate release, delayed release, sustained release, etc.) to provide therapeutic benefit with reduced side effects.Type: ApplicationFiled: October 19, 2012Publication date: February 14, 2013Inventor: Subhash Desai
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Publication number: 20130035377Abstract: Tranylcypromine derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e.g. tumors, viral infections, are herein described. These compounds belong to the structural formula (I) wherein A and R3 are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to compositions containing them and to therapeutic use thereof.Type: ApplicationFiled: April 15, 2011Publication date: February 7, 2013Applicants: UNIVERSITÀ DEGLI STUDI DI ROMA "LA SAPIENZA", UNIVERSITÀ DEGLI STUDI DI MILANO, UNIVERSITÀ DEGLI STUDI DI PAVIA, FONDAZIONE IEOInventors: Saverio Minucci, Antonello Mai, Andrea Mattevi
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Publication number: 20130035284Abstract: The present invention concerns methods and compositions involving small molecule inhibitors for the treatment or prophylaxis of flavivirus infection, such as dengue virus and West Nile virus.Type: ApplicationFiled: March 5, 2012Publication date: February 7, 2013Applicant: The Board of Regents of the University of Texas SystemInventors: Stanley J. Watowich, Suzanne M. Tomlinson, Scott Gilbertson
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Publication number: 20130035328Abstract: The invention relates to compounds having antiviral activity and methods utilizing the compounds to treat viral infections.Type: ApplicationFiled: July 19, 2012Publication date: February 7, 2013Inventors: Peter William Gage, Gary Dinneen Ewart, Lauren Elizabeth Wilson, Wayne Best, Anita Premkumar
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Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals
Patent number: 8362073Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: November 4, 2010Date of Patent: January 29, 2013Assignee: SanofiInventors: Matthias Schaefer, Josef Pernerstorfer, Dieter Kadereit, Hartmut Strobel, Werngard Czechtizky, L. Charlie Chen, Alena Safarova, Aleksandra Weichsel, Marcel Patek -
Publication number: 20130011417Abstract: The present invention relates to colchicine derivatives expressed in chemical formula 1, or to pharmaceutically acceptable salts thereof, to a method for preparing said derivatives, and to a pharmaceutical composition comprising said derivatives. The colchicine derivatives according to the present invention exhibit superior immunomodulatory effects as compared with conventional immunomodulators or colchicines, and therefore can be valuably used as an immunomodulator for modulating an acute or chronic immune response in organ transplantation.Type: ApplicationFiled: February 18, 2011Publication date: January 10, 2013Inventors: Duck Jong Han, Sung-eun Yoo, Jeehee Suh
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Publication number: 20130005802Abstract: Methods of treating Wnt/Frizzled-related diseases, comprising administering niclosamide compounds are provided. Methods of predicting whether a disease will respond to treatment with a niclosamide compound are also provided.Type: ApplicationFiled: September 21, 2010Publication date: January 3, 2013Inventors: Wei Chen, Minyong Chen, H. Kim Lyerly, Lawrence S. Barak, Robert Mook, Takuya Osada, Michael A. Morse
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Publication number: 20130005759Abstract: MicroRNAs are a class of endogenous regulators of gene function. Aberrant regulation of microRNAs has been linked to various human diseases, most importantly cancer. Small molecule intervention of microRNA misregulation has the potential to provide new therapeutic approaches to such diseases. microRNA miR-122 is the most abundant microRNA in the liver and is involved in hepatocellular carcinoma development and hepatitis C virus (HCV) infection. Small molecule inhibitors and activators of the microRNA miR-122 are described, and methods for their identification are reported. These small molecule inhibitors reduce viral replication in liver cells and thus represent a new approach to the treatment of HCV infections. Moreover, small molecule activation of miR-122 in liver cancer cells selectively induced apoptosis through caspase activation, and thus has implications in cancer chemotherapy.Type: ApplicationFiled: January 21, 2011Publication date: January 3, 2013Inventors: Alexander Deiters, Douglas D. Young
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Patent number: 8344029Abstract: It is an object of the present invention to provide a substituted propanamide derivative or a pharmacologically acceptable salt thereof that is useful as a prophylactic or therapeutic agent for a bone metabolic disease. The present invention relates to a pharmaceutical composition comprising a compound having General Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 represents a C6-C10 aryl group that may be substituted by a group selected from Substituent Group ?, for example; R2 represents a C6-C10 aryl group that may be substituted by a group selected from Substituent Group ?, for example; and X represents a hydroxyl group or a C1-C6 alkoxy group, for example].Type: GrantFiled: July 18, 2006Date of Patent: January 1, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Kazumasa Aoki, Koji Suda, Kentoku Gotanda, Tomio Kimura