Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/357)
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Patent number: 8916553Abstract: Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.Type: GrantFiled: July 25, 2011Date of Patent: December 23, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Joel Francis Austin, Lisa S. Sharma, James Aaron Balog, Audris Huang, Upender Velaparthi, Chetan Padmakar Darne, Mark George Saulnier
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Patent number: 8916614Abstract: The present invention is directed to methods of treatment for scabies using different concentrations of lindane lotions for varying contact times. Compositions of low concentration lindane lotions are also included.Type: GrantFiled: February 15, 2008Date of Patent: December 23, 2014Assignee: Wockhardt EU Operations (Swiss) AGInventor: Brian Tambi
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Publication number: 20140370080Abstract: The present invention relates generally to methods, compounds and compositions for treatment of adhesions, such as surgical adhesions.Type: ApplicationFiled: October 26, 2012Publication date: December 18, 2014Inventors: Arthur F. Stucchi, Michael Cassidy
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Publication number: 20140371214Abstract: Compounds of the form In which Q is selected from —CH?NR12, —W, —CH2NHR13, —CH?O and —CH(OR17)2 capable of modulating the activity of histone demethylases (HDMEs), which are useful for prevention and/or treatment of diseases in which genomic dysregulation is involved in the pathogenesis, such as e.g. cancer and formulations and methods of use of such compounds.Type: ApplicationFiled: August 28, 2014Publication date: December 18, 2014Inventors: Marc Labelle, Thomas Boesen, Qasim Khan, Ramkrishna Reddy Vakiti, Utpal Sharma, Ying Yang, Mukund Mehrotra, Neerja Saraswat, Farman Ullah
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Publication number: 20140371316Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropiomc acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).Type: ApplicationFiled: November 23, 2012Publication date: December 18, 2014Inventors: Jill S. FABRICANT, Iraj LALEZARI
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Patent number: 8912229Abstract: The present application discloses new taxane analogs, intermediates and methods for producing them. The present application is also directed to pharmaceutical formulations comprising abeo-taxanes and methods of treating cancer with the abeo-taxanes.Type: GrantFiled: April 6, 2012Date of Patent: December 16, 2014Assignee: Arbor Therapeutics, LLCInventors: James D. McChesney, John T. Henry, Sylesh Venkataraman, Mahesh Kumar Gundluru
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Patent number: 8912184Abstract: The invention relates to methods of treating diseases, particularly cancers, that respond favorably to the inhibition of Nicotinamide phosphoribosyltransferase (Nampt); it also relates to therapeutic methods that utilize Nampt inhibitors in combination with NAD biosynthesis precursors to intentionally kill cancer cells while limiting or minimizing toxicity to normal host cells; and it relates to methods of identifying cancers that will be most responsive to treatment with Nampt inhibitors, particularly when administered in combination with nicotinic acid.Type: GrantFiled: September 16, 2011Date of Patent: December 16, 2014Assignee: Alzheimer's Institute of America, Inc.Inventors: Tracey C. Fleischer, Daniel M. Cimbora, Jeffrey S. Flick, Andrew D. Gassman, Vijay R. Baichwal, Damon I. Papac
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Patent number: 8912222Abstract: N-Substituted sulfoximines are effective at controlling insects resistant to common insecticides.Type: GrantFiled: December 18, 2012Date of Patent: December 16, 2014Assignee: Dow AgroSciences, LLC.Inventors: Jim X. Huang, Richard B. Rogers, Nailah Orr, Thomas C. Sparks, James M. Gifford, Michael R. Loso, Yuanming Zhu, Thomas Meade
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Publication number: 20140364383Abstract: Methods and materials useful for applying pharmacologic agents to the ear are described. The methods involve delivering a composition that contains at least one viscogenic agent and at least one pharmacologic agent to the epidermal surface of the tympanic membrane via the ear canal. The composition is delivered to the tympanic membrane in a flowable form and, after delivery to the tympanic membrane, becomes sufficiently viscous such that the pharmacologic agent is localized against the tympanic membrane. Such compositions can be used to prophylactically and/or therapeutically treat middle and inner ear conditions, including otitis media.Type: ApplicationFiled: May 21, 2014Publication date: December 11, 2014Applicant: Regents of the University of MinnesotaInventors: Ronald J. Sawchuk, Belinda W.Y. Cheung
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Publication number: 20140364398Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.Type: ApplicationFiled: August 27, 2014Publication date: December 11, 2014Applicant: PFIZER INC.Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly
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Patent number: 8906945Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.Type: GrantFiled: April 6, 2010Date of Patent: December 9, 2014Assignee: Microbiotix, Inc.Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams
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Patent number: 8906946Abstract: Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: Wherein R is selected from: H, Br, CN, NO2, SO2NH2, SO2NHR? and SO2NR?2, where R? is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 alkyl Het is a heteroaryl group selected from a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted orType: GrantFiled: January 27, 2012Date of Patent: December 9, 2014Assignee: Dompe' S.p.A.Inventors: Alessio Moriconi, Gianluca Bianchini, Andrea Aramini, Laura Brandolini, Chiara Liberati, Silvia Bovolenta, Andrea Beccari, Simone Lorenzi
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Publication number: 20140357682Abstract: Non ligand binding pocket antagonists for the human androgen receptor. The androgen receptor (AR) is a member of the Nuclear Receptor (NR) family and its role is to modulate the biological effects of the endogenous androgens, testosterone (tes) and dihydrotestosterone (DHT). Synthetic androgens and anti-androgens have therapeutic value in the treatment of various androgen dependent conditions, from regulation of male fertility to prostate cancer. Current treatment of prostate cancer (PCa) typically involves administration of ‘classical’ antiandrogens, competitive inhibitors of natural AR ligands, DHT and tes, for the ligand binding pocket (LBP) in the C-terminal ligand binding domain (LBD) of the AR. However, prolonged LBP-targeting can often lead to androgen resistance and alternative therapies and therapeutic strategies are urgently required. Disclosed herein are a class of non-steroidal, small molecule AR antagonists which inhibit the transcriptional activity of the AR by non LBP-mediated modulation.Type: ApplicationFiled: November 23, 2012Publication date: December 4, 2014Applicant: THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, & THE OTHER MEMBERS OF BOARD, OF THE COLLEGE OF THE HOLYInventors: David George Lloyd, Darren Fayne, Mary Jane Meegan, Miriam Carr, Gemma Karena Kinsella, Laura Caboni, Wiliam Nicholas Jagoe, Billy Egan, Fernando Blanco
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Publication number: 20140357673Abstract: Disclosed herein are methods of inhibiting a deubiquitinase (DUB), methods of treating pathogenic infections (e.g., viral, bacterial, and/or parasitic), methods of inhibiting cell proliferation, methods of treating a neurodegenerative disease, methods of treating one or more symptoms of a neurodegenerative disease or a genetic disorder, and compounds.Type: ApplicationFiled: July 31, 2014Publication date: December 4, 2014Inventors: Nicholas J. Donato, Christiane Wobus, Hollis D. Showalter, Moshe Talpaz, Jeffrey William Perry, Roderick Joseph Sorenson, Mary Xuan Dziem O'Riordan, Yafei Jin
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Publication number: 20140357628Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof, with the proviso that the compound is no Tranilast.Type: ApplicationFiled: June 27, 2014Publication date: December 4, 2014Applicant: Fibrotech Therapeutics Pty LtdInventors: Spencer John Williams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
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Publication number: 20140357599Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.Type: ApplicationFiled: August 18, 2014Publication date: December 4, 2014Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING
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Publication number: 20140357597Abstract: The present invention relates to compositions, in particular within a fungicide composition, which comprises (A) a dithiino-tetracarboximide of formula (I) and a further fungicidally active compound (B). Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and to the treated seed.Type: ApplicationFiled: August 19, 2014Publication date: December 4, 2014Inventors: Thomas SEITZ, Ulrike Wachendorff-Neumann, Peter Dahmen
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Patent number: 8901155Abstract: A method for treating a TRPV1-mediated disease by administering to a patient a therapeutically effective amount of a compound or a salt thereof having the following formula [I]: wherein A represents a lower alkylene group or a lower alkenylene group; R1 represents a hydrogen atom, an unsubstituted or substituted alkyl group or an unsubstituted or substituted alkenyl group; and R2 and R3 are the same or different and represent a hydrogen atom, an unsubstituted lower alkyl group or a lower alkyl group substituted by a monocyclic cycloalkyl group, a polycyclic cycloalkyl group or an aryl group.Type: GrantFiled: November 19, 2012Date of Patent: December 2, 2014Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Kenji Oki, Fumio Tsuji, Chikako Setoguchi, Iwao Seki, Masaaki Murai, Minoru Sasano
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Publication number: 20140350032Abstract: The present invention relates to a compound characterized by the following Formula I: or a pharmaceutically acceptable salt thereof, wherein X, Y, and Z are as described herein. Compounds of the present invention are useful for the treatment of HIV.Type: ApplicationFiled: December 14, 2012Publication date: November 27, 2014Inventors: Nianhe Han, Brian Alvin Johns, Jun Tang
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Publication number: 20140350017Abstract: Compounds, compositions, and methods comprising a polyamine compound are described, which may be used to kill, disperse, treat, reduce biofilms, and/or inhibit or substantially prevent biofilm formation. In certain aspects, the present invention relates to compounds, compositions, and methods comprising polyamine compounds that have antimicrobial or dispersing activity against a variety of bacterial strains capable of forming biofilms.Type: ApplicationFiled: November 8, 2013Publication date: November 27, 2014Applicants: The University of Utah, Curza Global, LLCInventors: Dustin Williams, Ryan Looper, Sujeevini Jeyapalina, Travis Haussener, Paul R. Sebahar, Hari Kanna Reddy
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Publication number: 20140348880Abstract: A method for treating or preventing a microbial infection in a subject in need thereof, the method comprising administering to the subject, a therapeutically effective amount of a compound of Formula Ia, a compound of Formula IIa, one or more compounds of Formula Ia or Formula IIa complexed with a metal core, or a pharmaceutically acceptable salt, prodrug or hydrate thereof.Type: ApplicationFiled: May 23, 2014Publication date: November 27, 2014Inventors: Matthias Bierenstiel, Harshiny Muthukumar
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Patent number: 8895589Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: GrantFiled: August 23, 2012Date of Patent: November 25, 2014Assignee: Roche Palo Alto LLCInventors: Chris Allen Broka, Ronald Charles Hawley
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Publication number: 20140341999Abstract: The invention relates to the field of pharmaceutics and medicine and concerns a medicinal composition of antitubercular preparations with a phospholipid transport system, the composition consisting of a fatty acid salt, phosphatidylcholine of vegetative origin (73-97%), maltose and an antitubercular agent selected from rifamycin, protionamide, rifabutin and rifapentine, and a method for producing the composition.Type: ApplicationFiled: November 15, 2012Publication date: November 20, 2014Applicant: OBSCHESTVO S OGRANICHENNOY ONVETSTVENNOSTYU ''IBMKH-EKOBIOFARM'Inventors: Olga Mikhaylovna Ipatova, Natalya Velorikovna Medvedeva, Vladimir Nikolayevich Prozorovskiy, Maksim Aleksandrovich Sanzhakov, Yelena Georgiyevna Tikhonova, Oksana Sergeevna Druzhilovskaya
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Publication number: 20140343064Abstract: The present invention belongs to the field of natural medicine and pharmaceutical chemistry, and specifically relates to novel 2-substituted oleanolic acid derivatives of formula (I) or a pharmaceutically acceptable salt thereof, to a process for the preparation of these compounds, compositions containing such compounds and their use in preparing antineoplastic medicaments.Type: ApplicationFiled: November 30, 2012Publication date: November 20, 2014Applicant: Hanghzhou Bensheng Pharmaceutical Co., LtdInventors: Rongzhen Xu, Frank Rong, Hongxi Lai, Fuwen Xie
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Publication number: 20140341891Abstract: The present invention is based, at least in part, on the identification of a pharmaceutical container formed, at least in part, of a glass composition which exhibits a reduced propensity to delaminate, i.e., a reduced propensity to shed glass particulates. As a result, the presently claimed containers are particularly suited for storage of pharmaceutical compositions and, specifically, a pharmaceutical solution comprising a pharmaceutically active ingredient, for example, LYXUMIA (lixisenatide), LEMTRADA (alemtuzumab), REGN727/SAR236553 (alirocumab), SAR2405550/BSI-201 (iniparib), OTAMIXABAN (otamixaban), SARILUMAB (sarilumab), LANTUS and LYXUMIA (insulin glargine and lixisenatide) or VISAMERIN/MULSEVO (semuloparin sodium).Type: ApplicationFiled: April 23, 2014Publication date: November 20, 2014Applicant: CORNING INCORPORATEDInventors: Wendell P. Weeks, Robert Anthony Schaut, Steven Edward DeMartino, John Stephen Peanasky
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Publication number: 20140336440Abstract: Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.Type: ApplicationFiled: January 24, 2013Publication date: November 13, 2014Inventors: Ernst Schonbrunn, Rongshi Li, Said M. Sebti
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Publication number: 20140336194Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.Type: ApplicationFiled: July 28, 2014Publication date: November 13, 2014Applicant: NOVARTIS AGInventor: Shi Yin FOO
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Publication number: 20140335019Abstract: Provided herein are compositions and methods for the treatment and analysis of neurological disorders. In particular, provided herein are small molecules targeted to amyloid-? (A?) or metal-A? species for the treatment, diagnosis, or study of neurological conditions such as Alzheimer's disease (AD) and other diseases and conditions.Type: ApplicationFiled: November 30, 2012Publication date: November 13, 2014Inventors: Mi Hee Lim, Katayoun Saatchi, Urs Hafeli, Joo-Yong Lee
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Publication number: 20140336198Abstract: The present invention relates to compounds useful in the modulation of potassium channel activity in cells, in particular the activity of Kv1.3 channels found in T cells. The invention also relates to the use of these compounds in the treatment or prevention of autoimmune and inflammatory diseases, including multiple sclerosis, pharmaceutical compositions containing these compounds and methods for their preparation.Type: ApplicationFiled: May 16, 2012Publication date: November 13, 2014Applicants: MERCK PATENT GMBH, BIONOMICS LIMITEDInventors: Andrew Harvey, Agnes Bombrun, Rachel Cooke, Isabelle Jeanclaude-Etter, Nathan Kuchel, Jerome Molette, Jorgen Mould, Dharam Paul, Rajinder Singh, Cristina Donini, Veronique Colovray, Thomas Avery, Julia Crossman, Justin Ripper
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DISINTEGRANT-FREE DELAYED RELEASE DOXYLAMINE AND PYRIDOXINE FORMULATION AND PROCESS OF MANUFACTURING
Publication number: 20140335176Abstract: The present invention relates to a delayed release pharmaceutical composition containing doxylamine succinate and pyridoxine HCl for treatment of nausea and vomiting during pregnancy. More specifically, the present invention concerns a disintegrant-free delayed release pharmaceutical composition for oral administration comprising a core and an enteric coating, wherein said core comprising: a) at least one pharmaceutically active ingredient, and b) at least one pharmaceutically acceptable excipient, wherein said composition provides an in vitro drug release profile of about 80% of active ingredient dissolved within 20 minutes as measured by USP Type II apparatus and also a manufacturing process of said pharmaceutical composition.Type: ApplicationFiled: December 7, 2012Publication date: November 13, 2014Inventors: Prashant Monohar Mandaogade, David Ma, Naresh Talwar -
Patent number: 8883850Abstract: The present invention is directed to naphthalene carboxamide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimers disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: May 23, 2011Date of Patent: November 11, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Douglas C. Beshore, Christina Ng DiMarco, Scott D. Kukuk
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Patent number: 8884022Abstract: Disclosure is provided for carbamate compounds that prevent, remove and/or inhibit the formation of biofilms, compositions including these compounds, devices including these compounds, and methods of using the same.Type: GrantFiled: January 4, 2013Date of Patent: November 11, 2014Assignee: North Carolina State UniversityInventors: Christian Melander, Steven A. Rogers
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Patent number: 8883180Abstract: The invention relates to active compound combinations, in particular a fungicidal and/or insecticidal composition, comprising Isotianil (3,4-dichloro-N-(2-cyanophenyl)-5-isothiazolecarboxamide) and at least one further insecticide of the anthranilamide group and optionally one further insecticide of the neonicotinoids. Moreover, the invention relates to a method for curatively or preventively controlling the phytopathogenic fungi and/or microorganisms and/or pests of plants or crops, to the use of a combination according to the invention for the treatment of seed, to a method for protecting a seed and not at least to the treated seed.Type: GrantFiled: August 29, 2013Date of Patent: November 11, 2014Assignee: Bayer Intellectual Property GmbHInventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Peter Dahmen, Heike Hungenberg, Wolfgang Thielert
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Publication number: 20140328913Abstract: The present invention relates to an improved gelatinous coated dosage form having two end regions coated with gelatinous materials and an exposed circumferential band. Openings are provided in at least the exposed band to reveal the core material. The invention also relates to methods for manufacturing such gelatinous coated dosage forms.Type: ApplicationFiled: July 18, 2014Publication date: November 6, 2014Inventors: Roger A. Rinker, Nicholas J. Casale, James H. Comly, Brenda Pollack, Johan Geerke, Martin Costello, Dennis Wieand, Kishor Parekh
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Publication number: 20140329833Abstract: The invention relates to methods and compositions for the treatment or prevention of inflammation and inflammatory diseases or conditions. In particular, the invention relates to an LSD1 inhibitor, such as a 2-cyclylcylopropan-1-amine derivative, a phenelzine derivative and a propargylamine derivative, for use in treating or preventing inflammation and inflammatory diseases or conditions.Type: ApplicationFiled: May 21, 2012Publication date: November 6, 2014Applicant: ORYZON GENOMICS, S.AInventors: Tamara Maes, Marc Martinell Pedemonte, Julio Castro-Palomino Laria
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Patent number: 8877784Abstract: Compounds of formula (I) wherein R1, R2, R3, and Y are defined in the description are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: GrantFiled: January 2, 2009Date of Patent: November 4, 2014Assignee: Abbvie Inc.Inventors: Richard J. Perner, Michael E. Kort, Stanley DiDomenico, Jun Chen, Anil Vasudevan
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Patent number: 8877754Abstract: 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: GrantFiled: August 17, 2011Date of Patent: November 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Gerald Juergen Roth, Martin Fleck, Heike Neubauer, Bernd Nosse
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Publication number: 20140323532Abstract: Compounds are provided according to formula 1: where A, B, W, X?, L, R1, R3, R4b, and m? are as defined herein. Provided compounds and pharmaceutical compositions thereof are useful for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, cognitive disorders, anxiety, depression, and others.Type: ApplicationFiled: July 9, 2014Publication date: October 30, 2014Inventors: Zhi-Liang WEI, Sumithra GOWLUGARI, Carl KAUB, Zhan WANG, Yeyu CAO, John KINCAID
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Publication number: 20140323518Abstract: Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R1 to R9 have meanings as defined in the Specification, are useful as estrogen receptor ligands.Type: ApplicationFiled: August 2, 2012Publication date: October 30, 2014Inventors: Aiping Cheng, Neeraj Garg, Lars Krüger, Joakim Löfstedt, Eva Koch, Konrad Koehler, Lars Hagberg, Daniel Nöteberg
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Publication number: 20140323530Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.Type: ApplicationFiled: March 26, 2014Publication date: October 30, 2014Applicant: Acucela Inc.Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, Ryo Kubota
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Publication number: 20140323390Abstract: The invention provides a novel class of compounds, immunogenic compositions and pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with Toll-Like Receptors 2. In one aspect, the compounds are useful as adjuvants for enhancing the effectiveness of a vaccine.Type: ApplicationFiled: July 9, 2014Publication date: October 30, 2014Applicant: IRM LLCInventors: Tom Yao-Hsiang WU, Yefen Zou, Timothy Z. Hoffman, Jianfeng Pan
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Publication number: 20140323487Abstract: Novel compounds which are antagonists or inverse agonists at one or more of the opioid receptors, pharmaceutical compositions containing them, to processes for their preparation.Type: ApplicationFiled: July 8, 2014Publication date: October 30, 2014Inventors: David John Cowan, Andrew Lamont Larkin, Cunyu Zhang, David Lee Musso, Gary Martin Green, Rodolfo Cadilla, Paul Kenneth Spearing, Michael Joseph Bishop, Jason Daniel Speake
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Publication number: 20140323531Abstract: Compounds of formula (I) inhibit HDAC activity: wherein A, B and D independently represent ?C— or ?N—; W is a divalent radical —CH?CH— or CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.Type: ApplicationFiled: July 7, 2014Publication date: October 30, 2014Inventors: Alan Hornsby DAVIDSON, David Festus Charles Moffat, Francesca Ann Day, Alastair David Graham Donald
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Publication number: 20140323513Abstract: Disclosed are compound for targeting chemotherapeutic agents to mammalian mitochondria. Also disclosed are monoamine oxidase-specific compositions, and methods of using them for the selective therapy of mammalian cancers, and in particular, in the treatment of human gliomas. Also disclosed are methods employing the novel targeted chemotherapeutics with one or more conventional anti-cancer therapies, including, for example, radiotherapy, or multi-drug regimens.Type: ApplicationFiled: April 30, 2014Publication date: October 30, 2014Inventors: David S. Baskin, Martyn Alun Sharpe
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Patent number: 8871762Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more carboxamide fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease. Group (A): a group consisting of thifluzamide, oxadixyl, pencycuron, benalaxyl-M, fenhexamid, furametpyr, isopyrazam, isotianil, mepronil, tecloftalam, boscalid, fluopyram, fluopicolide, carpropamid, diclocymet, mandipropamid, dimethomorph, flumorph, penthiopyrad, and bixafen.Type: GrantFiled: March 2, 2011Date of Patent: October 28, 2014Assignee: Sumitomo Chemical Company, LimitedInventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
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Publication number: 20140315954Abstract: Compounds having cytotoxic and/or anti-mitotic activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having structure (I).Type: ApplicationFiled: March 14, 2014Publication date: October 23, 2014Inventors: Geoffrey C. WINTERS, Alexander L. Mandel, BRADLEY J. HEDBERG
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Publication number: 20140315840Abstract: Insect controlling compositions including an N-substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximine compound exhibiting increased stability, along with methods for preparing same, are disclosed.Type: ApplicationFiled: July 1, 2014Publication date: October 23, 2014Inventors: Kuide Qin, Raymond E. Boucher, Jr.
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Publication number: 20140315960Abstract: The present invention relates to novel depot formulations (prodrugs) comprising an immobility promoting unit linked via an ester to an active pharmaceutical ingredient, i.a. common NSAIDs. The novel depot formulations are suitable for intra-articular injections and are soluble at slightly acidic pH to facilitate ease of injection, and sparingly soluble at physiological pH thereby precipitating at the site of administration. The precipitate will slowly dissolve and the active drug is released from dissolved depot formulation following esterase mediated cleavage of the ester link between the immobility promoting unit and the active pharmaceutical agent.Type: ApplicationFiled: October 31, 2012Publication date: October 23, 2014Inventor: Claus Selch LARSEN
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Publication number: 20140315905Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.Type: ApplicationFiled: July 2, 2014Publication date: October 23, 2014Inventor: Soren Ebdrup
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Publication number: 20140315898Abstract: The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparationType: ApplicationFiled: December 12, 2012Publication date: October 23, 2014Applicant: BAYER CROPSCIENCE AGInventors: Adeline Koehler, Bernd Alig, Angela Becker, Arnd Voerste, Ulrich Goergens, Reiner Fischer, Wahed Ahmed Moradi, Silvia Cerezo-Galvez, Julia Johanna Hahn, Kerstin Ilg, Hans-Georg Schwarz, Takuya Gomibuchi, Masahito Ito, Daiei Yamazaki, Katsuhiko Shibuya, Eiichi Shimojo