Nitrogen In R Patents (Class 514/619)
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Patent number: 8168827Abstract: Amide derivatives represented by the formula (I): wherein: A is a cycloalkyl group, an aryl group or a heteroaryl group; X is a nitrogen atom or CR17; Y is —NRa-, —(CRbRb?)m-, and the like; m is 0 to 4; and R1 to R17 may be the same or different and each is a hydrogen atom, a halogen atom, a cyano group, a nitro group, a carboxyl group, a formyl group, a hydroxyl group, an ammonium group, an alkyl group optionally having one or more substituents, -ZR18 and the like, Z is —O—, —S(O)p-, —S(O)pO—, —NH—, —NR19-, and the like; or a pharmaceutically acceptable salt thereof, a hydrate thereof, or a solvate thereof may be applied to pharmaceutical use such as anti-inflammatory and analgesic action and the like.Type: GrantFiled: June 19, 2009Date of Patent: May 1, 2012Assignee: Ajinomoto Co., Inc.Inventors: Tadakiyo Nakagawa, Tamotsu Suzuki, Kaoru Takenaka, Shinichi Fujita, Youji Yamada, Yoichiro Shima, Tatsuya Okuzumi, Toshihiko Yoshimura, Masanao Yoshida, Masahiro Murata
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Publication number: 20120101147Abstract: The invention relates to methods and products for enhancing and improving recovery of lost memories. In particular the methods are accomplished by inhibiting HDAC2 and or selectively inhibiting HDAC1/2 or HDAC1/2/3.Type: ApplicationFiled: December 2, 2009Publication date: April 26, 2012Applicant: The General Hospital Corporation d/b/a Massachusetts General HospitalInventors: Li-Huei Tsai, Andre Fischer, Stephen J. Haggarty, Weiping Tang, Stuart L. Schreiber, Edward Holson, Florence Wagner, Mikel P. Moyer
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Publication number: 20120095051Abstract: This invention provides a compound having the structure wherein ?, ?, X, Y, and R1-R11 are defined herein. This invention also provides a pharmaceutical composition comprising the above compounds, a method of inhibiting the activity and/or levels of a matrix metalloproteinase (MMP), a method of inhibiting the production of a cytokine in a population of cells, a method of inhibiting the production of a growth factor in a population of cells, and a method of inhibiting NF?-B activation in a population of cells.Type: ApplicationFiled: May 14, 2010Publication date: April 19, 2012Inventors: Francis Johnson, Lorne Golub
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Publication number: 20120088794Abstract: The invention provides aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, n, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: December 19, 2011Publication date: April 12, 2012Applicant: THERAVANCE, INC.Inventors: Michael R. Leadbetter, Sean G. Trapp, Daniel D. Long, John R. Jacobsen, Sabine Axt
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Patent number: 8153693Abstract: The present invention relates to amino-salicylic-aminophenyl compounds for use in the treatment of the inflammatory component of celiac disease. These compounds act by blocking the cytokines released in celiac disease and are specifically useful in the treatment of refractory cases.Type: GrantFiled: December 23, 2008Date of Patent: April 10, 2012Assignee: Giuliani International LimitedInventors: Sergio Baroni, Salvatore Bellinvia
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Publication number: 20120078165Abstract: A therapeutic agent eluting element includes an elongate body member and one or more therapeutic agents elutable from the body member. The elongate body member is configured to be implanted subcutaneously along side of a therapy delivery element. The elongate body member may be formed from a polymeric material, and the agent eluting element may consist essentially of the body member and the one or more therapeutic agents. The therapeutic agent eluting element may be a part of a system or kit that includes a therapy delivery element and a tunneling tool, such as a dilator, sheath, catheter passer, or the like.Type: ApplicationFiled: December 5, 2011Publication date: March 29, 2012Applicant: MEDTRONIC, INC.Inventor: Thomas C. Bischoff
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Publication number: 20120070390Abstract: An over-the-counter (OTC) regulated therapeutic composition for self-medication use for application to wounds having a potential pathogen load, in which the composition comprises a tissue penetration enhancer comprising a Class I pharmaceutical incipient; a pharmaceutical antibiotic agent in a dosing suitable for use in an OTC listing; a hygroscopic carrier agent comprising a Class I pharmaceutical incipient suitable for mixing in solution with the tissue penetration enhancer and the antibiotic agent; and wherein the activity/water (Aw) measurement of the composition is less than the Aw measurement for a target pathogen in a tissue wound.Type: ApplicationFiled: April 21, 2011Publication date: March 22, 2012Inventors: D. Howard Phillips, Steven Keough
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Publication number: 20120065204Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.Type: ApplicationFiled: September 7, 2011Publication date: March 15, 2012Inventors: Lei Guo, Guozhi Tang, Zhanguo Wang, Jason Christopher Wong, Weixing Zhang
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Publication number: 20120058100Abstract: Disclosed are co-electrospun polymeric fibers comprising polymers comprising pharmaceutically active agents and/or biologically active agents and capable of release at a combined release rate. Also disclosed are processes for preparing polymeric fibers capable of release at a combined release rate. Also disclosed are processes of modulating delivery rate of pharmaceutically active agents and/or biologically active agents. Also disclosed are processes of delivering pharmaceutically active agents and/or biologically active agents. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: November 11, 2011Publication date: March 8, 2012Inventors: V. Prasad Shastri, Jay C. Sy
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Patent number: 8129431Abstract: An aqueous liquid preparation of the present invention containing 2-amino-3-(4-bromobenzoyl)phenylacetic acid or its pharmacologically acceptable salt or a hydrate thereof, an alkyl aryl polyether alcohol type polymer such as tyloxapol, or a polyethylene glycol fatty acid ester such as polyethylene glycol monostearate is stable. Since even in the case where a preservative is incorporated into said aqueous liquid preparation, the preservative exhibits a sufficient preservative effect for a long time, said aqueous liquid preparation in the form of an eye drop is useful for the treatment of blepharitis, conjunctivitis, scleritis, and postoperative inflammation. Also, the aqueous liquid preparation of the present invention in the form of a nasal drop is useful for the treatment of allergic rhinitis and inflammatory rhinitis (e.g. chronic rhinitis, hypertrophic rhinitis, nasal polyp, etc.).Type: GrantFiled: January 16, 2004Date of Patent: March 6, 2012Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Shirou Sawa, Shuhei Fujita
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Publication number: 20120046242Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.Type: ApplicationFiled: December 21, 2009Publication date: February 23, 2012Applicants: MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTONInventors: Randall T. Moon, Travis L. BIechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
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Publication number: 20120035265Abstract: A method for a prevention and/or treatment of dysmenorrhea or amelioration of a symptom thereof in a subject, comprising administering to said subject an effective amount of a compound of formula I:Type: ApplicationFiled: March 7, 2011Publication date: February 9, 2012Inventors: Kazuko MATSUDA, Yuichi Iwaki, Maria Feldman, Kale Ruby
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Publication number: 20120029084Abstract: Topical suspension compositions of nepafenac are disclosed. The compositions are especially suitable for topical ophthalmic administration.Type: ApplicationFiled: October 5, 2011Publication date: February 2, 2012Applicant: NOVARTIS AGInventor: Warren Wong
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Publication number: 20120021989Abstract: The invention relates to procedures and methods of determining a susceptibility to cardiac arrhythmia, including Atrial Fibrillation, Atrial Flutter and Stroke, by assessing the presence or absence of alleles at polymorphic markers found to be associated with risk of these conditions. The invention further relates to kits encompassing reagents for assessing such markers, and diagnostic 5 methods, uses and procedures for utilizing such susceptibility markers.Type: ApplicationFiled: March 30, 2010Publication date: January 26, 2012Applicant: deCODE Genetics ehf.Inventors: Hilma Holm, Daniel Gudbjartsson
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Publication number: 20120015001Abstract: The present invention relates to a methods and compositions for the treatment of and management of symptoms for thyroid eye disease. The methods include administering to a patient having thyroid eye disease an agent that interferes with hyaluronan synthesis in an amount that is effective to inhibit hyaluronan synthesis in a retro-ocular space. The pharmaceutical compositions hat includes a carrier suitable for ophthalmic delivery and an agent that interferes with hyaluronan synthesis. Combination therapies are also disclosed.Type: ApplicationFiled: May 3, 2011Publication date: January 19, 2012Applicant: UNIVERSITY OF ROCHESTERInventors: Richard P. Phipps, Naxin Guo, Steven Feldon
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Publication number: 20120015050Abstract: This document provides methods and materials involved in assessing samples (e.g., cancer cells) for the presence of a loss of heterozygosity (LOH) signature. For example, methods and materials for determining whether or not a cell (e.g., a cancer cell) contains an LOH signature are provided. Materials and methods for identifying cells (e.g., cancer cells) having a deficiency in homology directed repair (HDR) as well as materials and methods for identifying cancer patients likely to respond to a particular cancer treatment regimen also are provided.Type: ApplicationFiled: June 20, 2011Publication date: January 19, 2012Applicant: Myriad Genetics, IncorporatedInventors: Victor Abkevich, Alexander Gutin, Kirsten Timms, Jerry Lanchbury
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Patent number: 8093295Abstract: The present invention provides a pharmaceutical composition or crystalline composition with a specific dissolution profile, which comprises suberoylanilide hydroxamic acid or a pharmaceutically acceptable salt or hydrate thereof as an active ingredient. The present invention provides a process of producing said crystalline composition or pharmaceutical composition. The present invention also provides compositions with a specific particle size distribution.Type: GrantFiled: May 16, 2006Date of Patent: January 10, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Jeannie Chow Wong, Benjamin Max Cohen, Aaron S. Cote, Erik A. Dienemann, Kimberly Gallagher, Craig Ikeda, Justin Moser, Pavol Rajniak, Robert A. Reed, Brian Sell, Cindy Starbuck, Hsien-Hsin Tung, Qingxi Wang, Vincent R. Capodanno
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INHIBITION OF FATTY ACID SYNTHESIS BY IODO-NITROBENZAMIDE COMPOUNDS AND METHODS OF TREATMENT THEREOF
Publication number: 20120004260Abstract: The present invention relates to a method of treating a fatty acid synthesis related disease comprising administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis, wherein the fatty acid synthesis related disease is obesity, diabetes, or cardiovascular disease. The present invention also relates to a method of treating a cancer in a subject comprising: (i) identifying a level of fatty acid in a sample from the subject, and (ii) administering an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis in the subject, wherein the administration is based on the level of fatty acid, thereby treating the cancer in the subject. The present invention further relates to a method of treating Her-2 related cancers by administering to a patient in need thereof an effective amount of a PARP inhibitor or metabolite thereof to inhibit fatty acid synthesis.Type: ApplicationFiled: June 27, 2011Publication date: January 5, 2012Applicant: BiPar Sciences, Inc.Inventors: Valeria Ossovskaya, Barry Sherman -
Patent number: 8088828Abstract: This invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of benign prostate hyperplasia in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of treating a subject suffering from hair loss, comprising the step of administering to the subject a therapeutically effective amount of a 5-? reductase enzyme type 1 and/or type 2 inhibitor, wherein said inhibitor is a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein.Type: GrantFiled: June 30, 2010Date of Patent: January 3, 2012Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka, Wenqing Gao
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Patent number: 8084645Abstract: A compound of the present invention, or a pharmaceutically acceptable salt thereof is indicated by formula (1) below: wherein, R1, R2, R3, R4, R5, R6, Q, R8, and R9 have the same meanings as R1, R2, R3, R4, R5, R6, Q, R8, and R9 in the specification.Type: GrantFiled: September 16, 2004Date of Patent: December 27, 2011Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Yoshiaki Isshiki, Yasunori Kohchi, Kazuo Hattori, Nobuo Shimma, Masanori Miwa, Naohito Inagaki, Hitoshi Iikura, Yasuaki Matsubara
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Publication number: 20110301242Abstract: The present invention relates to methods (and pharmaceutical compositions) for treating and/or preventing for obesity associated disorders, particularly related to a deregulation of glucose homeostasis, by administrating Cathepsin S inhibitors. The invention also relates to methods for diagnosing insulin resistance and glucose tolerance by measuring Cathepsin S levels in a biological sample obtained from a subject.Type: ApplicationFiled: March 22, 2010Publication date: December 8, 2011Inventors: Karine Clement, Michele Guerre Millo, Nadia Naour
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Publication number: 20110301110Abstract: A method for diagnosing a chronic myelomonocytic leukemia (CMML) in a subject includes the steps of (i) determining the level of expression of the Trim33 (tripartite motif-containing 33) gene in a biological sample from the subject, and (ii) comparing the level of expression of the Trim33 gene in the biological sample with its normal level of expression; wherein an under-expression of the Trim33 gene is associated with CMML, and to a kit for diagnosing CMML in a subject including at least one nucleic acid probe or oligonucleotide or at least one antibody, which can be used in a such a method.Type: ApplicationFiled: June 2, 2011Publication date: December 8, 2011Inventors: Aucagne Romain, Bastie Jean Noël, Delva Laurent, Droin Nathalie, Solary Eric
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Patent number: 8071575Abstract: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; and a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion.Type: GrantFiled: February 22, 2008Date of Patent: December 6, 2011Assignee: University of Louisville Research FoundationInventors: William M. Pierce, Jr., K. Grant Taylor, Leonard C. Waite
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Publication number: 20110287026Abstract: Provided herein are SIRT4 compositions and methods of use thereof. The invention provides functional information for use in the identification and design of compounds that modulate SIRT4 enzyme activity (e.g., inhibition of fatty acid oxidation, ADP ribosylation, and/or downregulation of glutamate dehydrogenase), and to the compounds identified by such methods and the research, diagnostic and therapeutic uses of such compounds.Type: ApplicationFiled: September 23, 2009Publication date: November 24, 2011Applicant: President and Fellows of Harvard CollegeInventors: Marcia Haigis, Vincent De Boer
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Patent number: 8063247Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, are opioid receptor modulators, e.g. mu-opioid receptor antagonists, neutral antagonists or inverse agonists, and are useful inter alia for the treatment of obesity.Type: GrantFiled: September 8, 2008Date of Patent: November 22, 2011Assignee: Prosidion LimitedInventors: Jason Bloxham, Stuart Edward Bradley, Thomas Martin Krulle, Martin James Procter, Colin Peter Sambrook-Smith, Karen Lesley Schofield, Donald Smyth
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Publication number: 20110269834Abstract: Described herein are compounds and compositions, and methods for using the compounds and compositions, for treating respiratory diseases and illness, such as severe acute respiratory syndrome (SARS).Type: ApplicationFiled: August 21, 2009Publication date: November 3, 2011Applicants: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS, PURDUE RESEARCH FOUNDATIONInventors: Arun K. Ghosh, Jun Takayama, Andrew David Mesecar, Michael E. Johnson, Kiira M. Ratia, Rima Chaudhuri, Debbie C. Mulhearn
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Publication number: 20110269706Abstract: The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.Type: ApplicationFiled: January 7, 2010Publication date: November 3, 2011Applicant: Northlake Biosciences LLCInventors: Yu Chen, Yi Chen
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Publication number: 20110269785Abstract: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, anxiety, or manic depression, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: ApplicationFiled: January 7, 2011Publication date: November 3, 2011Applicant: Purdue Neuroscience CompanyInventors: Nancy C. Lan, Yan Wang, Sui Xiong Cai
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Publication number: 20110263604Abstract: The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases.Type: ApplicationFiled: April 18, 2011Publication date: October 27, 2011Applicant: Oryzon Genomics, S.A.Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
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Patent number: 8044078Abstract: The invention relates to a compound of the general formula (I), as defined herein which is useful for the treatment of a pathology in a patient wherein a CCR3 receptor plays a role in the development of the pathology, and pharmaceutical preparations containing such compound. The invention is also directed to a process for preparing the compound of the general formula (I), and intermediate useful in the preparation.Type: GrantFiled: March 19, 2008Date of Patent: October 25, 2011Assignee: Sanofi-AventisInventors: Agnes Pappne Behr, Zoltan Kapui, Peter Aranyi, Sandor Batori, Veronika Bartane Bodor, Lajos T. Nagy, Mihalyne Santa, legal representative, Marton Varga, Endre Mikus, Katalin Urban-Szabo, Judit Vargane Szeredi, Tibor Szabo, Edit Susan, Marianna Kovacs
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Publication number: 20110245335Abstract: The present invention relates in general to a compound which is characterized by a formula selected from the following formulas A, B, C, D, E or F; or a pharmaceutically acceptable salt thereof. The present invention further relates to pharmaceutical composition comprising the inhibitor(s) of the invention and to their use in the treatment of (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer. The present invention furthermore relates to the use of at least one inhibitor of the invention for the preparation of a pharmaceutical composition for the treatment of (for treating) a disease which is associated with an excess transport of hyaluronan across a lipid bilayer. The present invention also relates to a method for manufacturing a pharmaceutical composition comprising the steps of formulating the inhibitor defined herein in a pharmaceutically acceptable form.Type: ApplicationFiled: December 14, 2009Publication date: October 6, 2011Inventor: Peter Prehm
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Publication number: 20110245250Abstract: Compounds of formula (I) and pharmacologically acceptable salts and pro-drugs thereof wherein: Ar1 and Ar2 are aryl or heteroaryl; a is 0 to 5; R1 is alkyl, halogen, haloalkyl, alkoxy, haloalkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and, where a is greater than 1, each substituent R1 may be the same or different; b is 0 to 5; R2 is alkyl, halogen, haloalkyl, haloalkoxy, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monoalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino or cyano and where b is greater than 1, each substituent R2 may be the same or different; V is selected from the group consisting of (CR3aR3b)pCON(R3b)X and (CR3aR3b)pN(R3b)CO(X), wherein said groups are in the 3- (meta) or 4- (para) position with respect to the substituent Z; W is selected from the group consisting of NR4a, O, S, S?O, SO2 and C(R4aR4b)2; X is hydrogeType: ApplicationFiled: July 20, 2009Publication date: October 6, 2011Applicant: Ramot at tel-Aviv University Ltd.Inventors: Simon David Edwards, Meriel Ruth Kimberley, Richard Edward Armer, Nawaz Mohammed Khan
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Patent number: 8030518Abstract: This invention is directed to compounds of formula I, where G is —O—, —S—, —C(g1)(g2)-, or —NH—, and n=1, 2, or 3. Such compounds modulate potassium channels. The compounds are useful for the treatment and prevention of diseases and disorders which are affected by modulation of potassium ion channels. One such condition is seizure disorders.Type: GrantFiled: November 28, 2007Date of Patent: October 4, 2011Assignee: Valeant Pharmaceuticals InternationalInventors: Huanming Chen, Jianlan Song, Jean-Michel Vernier, Jim Zhen Wu
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Patent number: 8021687Abstract: A milnacipran formulation that provides delayed and extended release of milnacipran has been developed. The formulation comprises milnacipran or a salt thereof; an extended release excipient, and a delayed release excipient. The formulation provides, upon administration to a human subject, a Tmax of 4-10 hours.Type: GrantFiled: April 7, 2010Date of Patent: September 20, 2011Assignee: Collegium Pharmaceutical, Inc.Inventors: Jane C. Hirsh, Roman V. Rariy, Shubha Chungi, Srinivas G. Rao, Michael T. Heffernan
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Publication number: 20110224303Abstract: The invention relates to methods and compositions for promoting cognitive function and/or treating cognitive function disorders and impairments. In particular the methods are accomplished by administering to a subject CI-994 or dinaline or a pharmaceutically acceptable salt, ester, prodrug or metabolite thereof.Type: ApplicationFiled: November 1, 2010Publication date: September 15, 2011Inventors: Li-Huei Tsai, Ji-Song Guan, Stephen J. Haggarty, Edward Holson, Florence Wagner, Johannes Graeff
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Patent number: 8017630Abstract: Novel cyclohexylacetic acid compounds corresponding to formula I: processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including these compounds and related methods of treating or inhibiting certain diseases or conditions.Type: GrantFiled: November 9, 2006Date of Patent: September 13, 2011Assignee: Gruenenthal GmbHInventors: Claudia Hinze, Bernd Sundermann, Hans Schick, Birgitta Henkel
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Patent number: 8008348Abstract: This invention provides: 1) a method of treating a subject suffering from a muscle wasting disorder; 2) a method of preventing a muscle wasting disorder in a subject; 3) a method of treating, preventing, suppressing, inhibiting or reducing muscle loss in a subject suffering from a muscle wasting disorder; 4) a method of treating, preventing, inhibiting, reducing or suppressing muscle wasting in a subject suffering from a muscle wasting disorder; and/or 5) a method of treating, preventing, inhibiting, reducing or suppressing muscle protein catabolism in a subject suffering from a muscle wasting disorder, by administering to the subject a selective androgen receptor modulator (SARM) and/or an analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, prodrug, polymorph, impurity or crystal of said SARM compound, or any combination thereof.Type: GrantFiled: June 7, 2004Date of Patent: August 30, 2011Assignee: University of Tennessee Research FoundationInventors: Mitchell S. Steiner, Karen A. Veverka, James T. Dalton, Duane D. Miller
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Publication number: 20110207823Abstract: The present invention consists of an extended-release metoclopramide hydrochloride pharmaceutical composition, in 15 mg drug substance tablets, for use in gastrointestinal disorders. The formulation is mainly composed of a hydrophilic polymer, a hydrophobic polymer, a hydrophilic component and metoclopramide hydrochloride. The hydrophilic polymer is swollen by hydration when contacting water, forming a gel coat which controls drug substance release. The water inside the matrix dissolves the drug substance and this is diffused outside through the gel coat. The hydrophobic polymer shows plastic deformation properties under compression, tending to surround the drug substance particles reducing the pore quantity and dimensions in the matrix structure, delaying as a consequence the drug substance release. The hydrophilic component is part of the gel coating structure providing support thereto. Drug substance is the metoclopramide hydrochloride or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 27, 2009Publication date: August 25, 2011Applicant: POSIVISIONARY SOLUTIONS LLPInventors: John Claude Savoir Vilboeuf, Maria Teresa de Jesus Francisco Doce, Teresita del Niño Jesús Costales González, Miriam Villa Vargas
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Publication number: 20110201603Abstract: The present invention relates to novel Acylaminobenzamide derivatives represented by the following formula (I) and use thereof as pesticides: wherein V represents an aromatic ring group of V1 to V5 described in the detailed description, Q represents an aromatic ring group of Q1 to Q7 described in the detailed description, G1 and G2 represent O or S, R1 represents hydrogen, alkyl, haloalkyl, alkoxy, haloalkoxy, phenyl or a heterocyclic group and R2 and R3 represent hydrogen, alkyl, haloalkyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl or haloalkoxycarbonyl.Type: ApplicationFiled: July 30, 2009Publication date: August 18, 2011Applicant: Bayer CropScience AGInventors: Jun Mihara, Tetsuya Murata, Kei Domon, Yukiyoshi Watanabe, Yasushi Yoneta, Takuma Mori, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara, Masashi Ataka, Ulrich Görgens
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Publication number: 20110201601Abstract: The present invention relates to the use of compounds of general formula (I) and (II) for the preparation of a drug for preventing and/or treating disorders caused by Shiga toxins and related toxins.Type: ApplicationFiled: June 17, 2009Publication date: August 18, 2011Applicants: COMMISSAR. A L'ENERG. ATOM. ET AUX ENERG. ALTERN., INSTITUT CURIE, CENTRE NAT DE LA RECHERCHE SCIENTIFIQUEInventors: Daniel Gillet, Julien Barbier, Ludger Johannes, Bahne Stechmann, Siau-Kun Bai
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Publication number: 20110178077Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.Type: ApplicationFiled: June 17, 2009Publication date: July 21, 2011Inventors: Priscille Brodin, Thierry Christophe, Zaesung No, Jaeseung Kim, Auguste Genovesio, Denis Philippe Cedric Fenistein, Heekyoung Jeon, Fanny Anne Ewann, Sunhee Kang, Saeyeon Lee, Min Jung Seo, Eunjung Park, Monica Contreras Dominguez, Ji Youn Nam, Eun Hye Kim
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Publication number: 20110178163Abstract: The present disclosure provides methods of determining the levels of BRCA1 in a cell, altering the levels of BRCA1 in a cell, determining the likelihood of developing cancer, and determining the prognosis of a patient with cancer using miR-182 and analogs thereof. Importantly, the invention also provides methods of determining whether a patient should be treated with PARP inhibitors, improving PARP therapy in cancer, as well as methods for selecting and improving genotoxic therapies. Also featured are methods of treating patients with cancers based on the expression levels of miR-182. The invention also features compositions comprising miR-182 and analogs thereof, antagomirs of mIR-182 and analogs thereof, in combination with PARP inhibitors and genotoxic agents.Type: ApplicationFiled: January 13, 2011Publication date: July 21, 2011Inventor: Dipanjan Chowdhury
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Publication number: 20110177085Abstract: The present invention relates to bitter-taste receptors and their role in bitter taste transduction. The invention also relates to assays for screening molecules that modulate, e.g. suppress or block, bitter taste transduction, or enhance bitter taste response.Type: ApplicationFiled: March 25, 2011Publication date: July 21, 2011Inventors: Bernd Bufe, Thomas Hofmann, Dietmar Krautwurst, Christina Kuhn, Wolfgang Meyerhof
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Publication number: 20110178153Abstract: Methods of treating or preventing chemoresistance or relapse growth of cancer cells are provided. Methods of treating or preventing resistance to tyrosine kinase based chemotherapeutic treatment in hematologic and solid tumors are provided. BCR-ABL drug resistance in chronic myelogenous leukemia (CML) and models for conducting further study on the same are presented. The methods comprise administering a therapeutically effective amount of one or more SIRT1 modulators to the cells or subject in need thereof. The methods may be administered in combination with, prior to or subsequent to chemotherapy or may be administered to counteract the effect of a spontaneous genetic mutation. Methods of using SIRT1 inhibitors to treat or prevent insulin and transferrin-induced resistance are also presented. A novel cell model to study mechanisms of acquired chemoresistance is also provided.Type: ApplicationFiled: February 5, 2008Publication date: July 21, 2011Inventor: Wenyong CHEN
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Patent number: 7981937Abstract: A dispersion of 2,2-dibromo-3-nitrilopropionamide (“DBNPA”) particles in a restrictedly viscosified concentrated brine solution effectively negates gelling of the brine solution because the naturally occurring gum used does not exhibits Ellis-Plastic behavior in the concentrated brine at a pH of from about 1 to 4. Because the DBNPA particles are much less soluble in the brine than in water, the particles are held in the stable dispersion. Moreover, a dispersion of DBNPA particles in viscosified brine provides at least the same biocidal effect as a solution of DBNPA, relative to the same concentration of DBNPA in solution in glycol, but also concurrently nullifies the degradation of the DBNPA during storage so that the loss due to hydrolysis of the DBNPA is less than 3% over a period of three months at a temperature in the range from ?5° C. to 25° C. A process is disclosed for making the dispersion which can be stored at a temperature in the range from about ?5° C. to 25° C.Type: GrantFiled: January 10, 2007Date of Patent: July 19, 2011Assignee: Aurora Specialty Chemistries Corp. AuroraInventors: Vijay Vinayak Pendse, Harry James Moyle
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Patent number: 7973079Abstract: Compounds that reduce serum retinol levels are used to treat ophthalmic conditions associated with the overproduction of waste products that accumulate during the course of the visual cycle. We describe methods, compounds, and compositions to treat, for example, the macular degenerations and dystrophies or to alleviate symptoms associated with such ophthalmic conditions.Type: GrantFiled: September 15, 2008Date of Patent: July 5, 2011Assignee: Revision Therapeutics, Inc.Inventors: Nathan L. Mata, Kim B. Phan, Tam V. Bui, Mustapha Haddach
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Publication number: 20110150775Abstract: The present invention provides systems for developing and/or testing therapies for prenatal diseases and conditions including Down Syndrome. The present invention also provides diagnostic methods for Down Syndrome involving, in some embodiments, gene expression analyses of fetal RNA and/or detection of expression of particular genes involved in Down Syndrome. Also provided are microarrays and kits useful in prenatal diagnostic applications.Type: ApplicationFiled: June 1, 2009Publication date: June 23, 2011Inventors: Donna Slonim, Kirby Johnson, Diana Bianchi
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Patent number: 7960436Abstract: This invention provides compounds of formula I where Ar1 is a 5- to 10-member mono- or bicyclic aromatic group, optionally substituted; where the —NR3R4 group is situated ortho to the NHC(?X) group; n=1 or 2; X?O or S; Y is O or S; and q=1 or 0. The invention also provides pharmaceutical compositions comprising compounds of formula I and/or salts, esters, and prodrugs thereof. These compounds modulate the activation and inactivation of potassium channels. The compounds are useful for the treatment and prevention of diseases and disorders—such as seizure disorders—which are affected by modulation of potassium ion channels.Type: GrantFiled: June 4, 2007Date of Patent: June 14, 2011Assignee: Valeant Pharmaceuticals InternationalInventors: Huanming Chen, Jean-Michel Vernier
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Patent number: 7956093Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts.Type: GrantFiled: August 29, 2007Date of Patent: June 7, 2011Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
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Publication number: 20110124653Abstract: The invention relates to dimeric aryl-sulphonamido compounds endowed with inhibitory activity against metalloproteases MMP, having formula (I) below (M)-L-(M?) (I), wherein M and M?, the same or different from each other, represent the residues of the metalloproteases inhibitors of formula (II), wherein R, R1, R2, R3, G and n have the meanings reported in the specification; the invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders.Type: ApplicationFiled: July 21, 2009Publication date: May 26, 2011Applicant: BRACCO IMAGING S.P.A.Inventors: Armando Rossello, Elisa Nuti, Tiziano Tuccinardi, Elisabetta Orlandini