Nitrogen In Substituent Q Patents (Class 564/163)
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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: 20110269689Abstract: High penetration compositions (HPC) of a parent compound, which are capable of crossing biological barriers with high penetration efficiency. The HPCs are capable of being converted to parent drugs or parent drug-related compounds such as metabolites after crossing one or more biological barriers and thus can render treatments for the conditions that the parent drugs or parent drug-related compounds can. Additionally, the HPCs are capable of reaching areas that their parent drugs or parent drug-related compounds may not be able to access or to render a sufficient concentration at the target areas HPCs of NSAIA, for example, have demonstrated indications such as treating hair loss. A HPC can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.Type: ApplicationFiled: December 4, 2009Publication date: November 3, 2011Inventor: Chongxi Yu
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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: 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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Publication number: 20110263457Abstract: We describe herein a cell-based multiplexing technique called detectable cell barcoding (DCB). In DCB, each individual sample is labeled with a different DCB signature that distinguishes each sample by one or both of detected intensity or type of detection characteristic. The samples are then combined and analyzed for a detectable characteristic of interest (e.g., presence of an analyte). By employing multiple distinct DCB labels at varying concentrations, one can perform multiplex analyses on up to hundreds or thousands (or more) of cell samples in a single reaction tube. DCB reduces reagent consumption by factors of 100-fold or more, significantly reduces data acquisition times and allows for stringent control sample analysis.Type: ApplicationFiled: July 1, 2011Publication date: October 27, 2011Inventors: Peter O. Krutzik, Garry Nolan
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Publication number: 20110251393Abstract: The invention provides a helicene derivative, axially chiral amino acid, amine or amino alcohol derivative, and azaperylene, such as compounds represented by Formulae (I), (I?), (II), (II?), and (III): and a method for producing the same.Type: ApplicationFiled: October 20, 2009Publication date: October 13, 2011Applicant: KYOTO UNIVERSITYInventors: Takumi Furuta, Takeo Kawabata
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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: 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: 20110158909Abstract: The present invention provides compounds useful as contrast agents, such as for the CT imaging of cartilage tissue. The contrast agents are generally iodinated organic molecules that are positively charged under physiological environments. Also provided are compositions containing contrast agents and methods of using the agents, including, for example, the monitoring of glycosaminoglycan content in cartilage tissue. The invention provides non-invasive analytical techniques for the diagnosis of osteoarthritis in its earliest stages. The invention also provides improvements over existing contrast agents for cartilage monitoring, which tend to exhibit low residence times and require high dosages.Type: ApplicationFiled: January 27, 2009Publication date: June 30, 2011Applicant: Trustees of Boston UniversityInventors: Mark W. Grinstaff, Neel Joshi, Prashant Bansal
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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: 7943775Abstract: A tissue is imaged to detect the presence of amyloid deposits or other target proteins prior to their aggregation into plaques, with the assistance of the administration of a labeled bifunctional compound of which one functionality binds to the target protein and the second functionality binds to a chaperone protein that is present in the tissue of interest. The two functionalities have different binding affinities, the target-binding functionality having the greater binding affinity, with the result that the bifunctional compound preferentially remains in the tissue when bound to the chaperone and then the target protein while bifunctional compound that is not bound to the target protein will leave the tissue.Type: GrantFiled: June 13, 2007Date of Patent: May 17, 2011Assignee: The United States of America as represented by the Secretary of the Department of Health and Human ServicesInventors: King C. Li, S. Narasimhan Danthi
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Patent number: 7943785Abstract: The present invention provides a process for producing (Z)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2-phthalimidomethylcyclopropane, which includes reacting (Z)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2-hydroxymethylcyclopropane with an orthoester and a brønsted acid, and reacting the reaction product with a phthalimidating agent; and a process for producing (Z)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2-aminomethylcyclopropane hydrochloride through the above process.Type: GrantFiled: January 26, 2007Date of Patent: May 17, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Yoshihide Niimoto, Hiroharu Kumazawa, Koh Kawami
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Patent number: 7928141Abstract: Taught is a composition for enhancing potency and/or for prolonging the duration of action of an anesthetic comprising dexamethasone, compound vitamin B, metronidazole, berberine, etamsylate, gentamicin, chymotrypsin, methylene blue trihydrate, and 5% sodium bicarbonate aq. When administered with an anesthetic, the composition shortens the onset time of the anesthetic, and prolongs the duration of anesthesia.Type: GrantFiled: January 14, 2008Date of Patent: April 19, 2011Inventor: Fuchao Li
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Publication number: 20110039819Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: April 9, 2009Publication date: February 17, 2011Inventors: Marion Hitchcock, Ingo Hartung
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Publication number: 20110033930Abstract: The present invention relates to a method for obtaining Ngn3-expressing cells and insulin producing-beta cells by contacting a Pdx1-expressing pancreas explant with an amount of at least one histone deacetylase inhibitor (HDACi). The inventive methods have the advantage of being simple and quick, and of providing large amounts of Ngn3-expressing cells and insulin producing-beta cells, that are useful therapeutic tools. The invention also relates to a pharmaceutical composition for the treatment of diabetes which comprises an amount of at least one HDACi.Type: ApplicationFiled: August 21, 2009Publication date: February 10, 2011Inventors: Raphael Scharfmann, Cecile Haumaitre-Sarron, Olivia Lenoir
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Patent number: 7875746Abstract: A photosensitive composition comprising: (A) a compound capable of generating a compound having a specific structure upon irradiation with actinic rays or radiation, a pattern forming method using the photosensitive composition, and a compound capable of generating a compound having a specific structure upon irradiation with actinic rays or radiation.Type: GrantFiled: May 23, 2006Date of Patent: January 25, 2011Assignee: FUJIFILM CorporationInventor: Kenji Wada
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Publication number: 20100324159Abstract: Embodiments of the present invention are directed to porous resins for solid phase extractions. The resins feature at least one hydrophobic component, at least one hydrophilic component and at least one ion exchange functional group. The resins exhibit superior wetting and ion exchange performance.Type: ApplicationFiled: August 12, 2010Publication date: December 23, 2010Applicant: Waters Technologies CorporationInventors: Peter Jeng Jong LEE, John E. O'Gara
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Publication number: 20100280251Abstract: Disclosed is a method for preparing a compound of Formula 1 comprising contacting a compound of Formula 2 with a metal cyanide reagent, a copper(I) salt reagent, an iodide salt reagent and at least one compound of Formula 3 wherein R1 is NHR3 or OR4; R2 is CH3 or Cl; R3 is H, C1-C4 alkyl, cyclopropyl, cyclopropylcyclopropyl, cyclopropylmethyl or methylcyclopropyl; R4 is H or C1-C4 alkyl; Y is Br or Cl; X is NR13 or O; n is 0 or 1; and R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 2 wherein Y is Br and R1 is NHR3 comprising introducing a gas containing bromine into a liquid containing a compound of Formula 4, and further disclosed is a method for preparing a compound of Formula 5 wherein R14, R15, R16 and Z are as defined in the disclosure using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above.Type: ApplicationFiled: December 18, 2007Publication date: November 4, 2010Applicant: E.I. Du Pont De Nemours and CompanyInventors: Joerg Bruening, Gary David Annis, Martin James Currie, Donald J. Dumas, Rafael Shapiro
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Patent number: 7825278Abstract: The invention relates to substituted enaminones of Formula I and their derivatives and the discovery that these compounds modulate the effect of ?-aminobutyric acid (GABA) on the GABAA receptor complex in a therapeutically relevant fashion and may be used to ameliorate CNS disorders amenable to modulation of the GABAA receptor complex.Type: GrantFiled: May 5, 2005Date of Patent: November 2, 2010Assignee: The Regents of the University of CaliforniaInventors: Derk J. Hogenkamp, Timothy B. C. Johnstone, Kelvin W. Gee
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Publication number: 20100267780Abstract: 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: ApplicationFiled: September 8, 2008Publication date: October 21, 2010Inventors: Jason Bloxham, Stuart Edward Bradley, Thomas Martin Krulle, Colin Peter Sambrook-Smith, Karen Lesley Schofield, Donald Smyth
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Patent number: 7816386Abstract: Cinnamic and phenylpropiolic acid derivatives of formula (I) having antitumour and chemo sensitizing activity are described. Also described are pharmaceutical compositions containing the above-mentioned compounds, for the treatment of tumours.Type: GrantFiled: May 31, 2006Date of Patent: October 19, 2010Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Claudio Pisano, Gianfranco Battistuzzi, Maria Di Marzo, Giuseppe Giannini, Mauro Marzi, Loredana Vesci, Franco Zunino, Riccardo Pezzi
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Publication number: 20100234469Abstract: The invention relates to 2-amino-3-benzoylbenzeneacetamide, i.e. nepafenac, crystals having reduced chargeability, to processes for the preparation thereof, and to the use thereof for preparing pharmaceutical formulations.Type: ApplicationFiled: March 12, 2010Publication date: September 16, 2010Applicant: Medichem, S.A.Inventors: Ana Gavaldá Escudé, Ernesto Duran Lopez
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Publication number: 20100222338Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A, B, W, R3, R4, R5, i and j are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, methods of use for these compounds, including treatment of AD and related diseases, by administering the compound(s) of Formula I, or compositions including them, to a subject. The invention also comprises further embodiments of Formulas II and III, intermediates and processes useful for the preparation of compounds of the invention.Type: ApplicationFiled: May 13, 2010Publication date: September 2, 2010Inventors: Wenge Zhong, Stephen Hitchcock, Brian K. Albrecht, Michael D. Bartberger, James Brown, Ryan Brown, Stuart C. Chaffee, Yuan Cheng, Michael Croghan, Russell Graceffa, Scott Harried, Dean Hickman, Daniel Horne, Randall Hungate, Ted Judd, Matthew Kaller, Charles Kreiman, Daniel La, Patricia Lopez, Craig E. Masse, Thomas Nixey, Vinod F. Patel, Lewis Pennington, Matthew Weiss, Qiufen Xue, Bryant Yang, Holger Monenschein, Thomas Nguyen
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Publication number: 20100174090Abstract: The present application relates to novel methods for the preparation of primary, secondary and tertiary carbinamine compounds, particularly the preparation of compounds of formulae I, IV and VI, from a carbonyl compound of formula II in the presence of ammonia or an ammonium equivalent of the formula NH4+X?, by way of allylation, crotylation, arylation, reductive amination and catalytic hydrogenation.Type: ApplicationFiled: March 28, 2008Publication date: July 8, 2010Inventors: Avinash N. Thadani, Bhartesh Dhudshia
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Publication number: 20100137365Abstract: Long chain N-alkyl amino and imino compounds, oxa-substituted derivatives thereof, and pharmaceutical compositions including such compounds are described. The long chain N-alkyl group is a C8-C16 alkyl group. The long chain N-alkyl compounds and oxa-substituted derivatives thereof can be used in the treatment of viral infections, in particular hepatitis B virus or hepatitis C virus, in a cell or an individual. For example, the long chain N-alkyl compounds or oxa-substituted derivatives thereof can be derived from piperidines, pyrrolidines, phenylamines, pyridines, pyrroles, or amino acids.Type: ApplicationFiled: January 28, 2010Publication date: June 3, 2010Inventors: Nicole Zitzmann, Terry D. Butters, Frances M. Platt, Gary S. Jacob, Donald H. Picker, Sandra Carrouee, George W.J. Fleet, Raymond A. Dwek, David Durantel, Anand Mehta, Timothy M. Block
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Publication number: 20100137296Abstract: Compounds that can be used as openers or blockers of voltage-dependent potassium channels, and which are useful in the treatment of conditions such as central or peripheral nervous system disorders through the modulation of potassium ion flux through voltage-dependent potassium channels and/or depressing or enhancing cortical and/or peripheral neuron activity, compositions containing same and methods utilizing same are disclosed. Also disclosed are modulators of voltage-dependent potassium channels, which exhibit blocking of a TRPV1 channel, and hence are useful in the treatment of TRPV1-related conditions.Type: ApplicationFiled: September 18, 2008Publication date: June 3, 2010Applicant: Ramot At Tel Aviv University Ltd.Inventors: Bernard Attali, Asher Peretz
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Publication number: 20100130757Abstract: The present invention provides methods and compositions for detecting, identifying and measuring the abundance of chemical nerve agents. Methods and compositions of the present invention are capable of providing selective detection of phosphorous based nerve agents, such as nerve agents that are esters of methyl phosphonic acid derivatives incorporating a moderately good leaving group at the phosphorus. Selectivity in the present invention is provided by a sensor composition having an alpha (?) effect nucleophile group that undergoes specific nucleophilic substitution and rearrangement reactions with phosphorus based nerve agents having a tetrahederal phosphorous bound to oxygen. The present invention includes embodiments employing a sensor composition further comprising a reporter group covalently linked to the alpha effect nucleophile group allowing rapid optical readout of nerve agent detection events, including direct visual readout and optical readout via spectroscopic analysis.Type: ApplicationFiled: January 21, 2010Publication date: May 27, 2010Applicant: UNIVERSITY OF WYOMINGInventors: Robert C. Corcoran, Aaron D. Strickland
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Publication number: 20100056522Abstract: An object of the present invention is to find a novel pharmacological effect of a compound having an HDAC inhibitory effect. The compound having an HDAC inhibitory effect of the invention has an excellent effect of cell morphological change on trabecular meshwork cells and/or effect of intraocular pressure reduction, and is therefore useful as a preventive and/or therapeutic agent for a disease considered to be associated with aqueous humor circulation and/or intraocular pressure, particularly as a preventive and/or therapeutic agent for glaucoma or ocular hypertension.Type: ApplicationFiled: March 28, 2008Publication date: March 4, 2010Applicant: Santen Pharmaceutical Co., Ltd.Inventors: Shinji Yoneda, Koushi Fujisawa, Katsuhiko Watanabe, Junko Fujikawa, Atsushi Shimazaki, Tomoko Kirihara, Hisashi Tajima
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Publication number: 20100016611Abstract: The invention discloses compounds of formula II: and methods of making the compounds, which are VR1 antagonists that are useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence and bladder overactivity.Type: ApplicationFiled: March 20, 2009Publication date: January 21, 2010Applicant: ABBOTT LABORATORIESInventors: Kirill A. Lukin, Brian J. Kotecki, Su Yu, Lei Wang, Anthony R. Haight
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Publication number: 20090312429Abstract: Nepafenac or derivatives thereof are useful for the treatment of dermatological conditions related to a keratinization disorder that may have an inflammatory immunoallergic component, for example rosacea, acne, psoriasis or atopic dermatitis.Type: ApplicationFiled: June 19, 2009Publication date: December 17, 2009Applicant: GALDERMA RESEARCH&DEVELOPMENTInventors: Irina Safonova, Cecile Cousin, Leila Zarif
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Publication number: 20090312575Abstract: Disclosed is a process for preparing anti-inflammatory compound nepafenac comprising preparing a compound of formula (V) wherein a N-halosuccinimide is used as the halogenating agent, followed by desulfurization using Raney Nickel. Also disclosed is a polymorphic form B of 2-amino-3-benzoyl-?-(methylthio)-benzeneacetamide (i.e.Type: ApplicationFiled: June 12, 2009Publication date: December 17, 2009Applicant: Medichem, S.A.Inventors: Gabriel Tojo Suarez, Ana Gavalda Escude
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Publication number: 20090306372Abstract: Disclosed is a method for preparing a compound of Formula 1 by contacting compound of Formula 2 with R1—NH2 in the presence of a carboxylic acid and a method for preparing a compound of Formula 2 by contacting a compound of Formula 4 with phosphorus tribromide. wherein R1 is H, C1-C4 alkyl, cyclopropyl, cyclopropylmethyl or methylcyclopropyl; R2 is CH3 or Cl; R3 is C1-C6 alkyl or C3-C6 alkenyl, each optionally substituted with up to 3 halogen and up to 1 phenyl; and X is Cl or Br. Also disclosed is a method for preparing a compound of Formula 5 wherein R4, R5, R6 and Z are as defined in the disclosure, using a compound of Formula 1 that is characterized by preparing the compound of Formula 1 by the method above.Type: ApplicationFiled: June 27, 2007Publication date: December 10, 2009Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: Richard F. Davis, Rafael Shapiro, Eric G. Taylor
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Patent number: 7629493Abstract: The invention relates to a process for the crystallization of the compounds of the formula (I) or acid-addition salts thereof, in which R1, R2 and R3 have the meaning indicated in Claim 1.Type: GrantFiled: April 10, 2004Date of Patent: December 8, 2009Assignee: Merck Patent GmbHInventors: Michael Kirschbaum, Ekkehard Bartmann, Dieter Bensinger, Alexander Haas, Ricky Lippert
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Patent number: 7622612Abstract: The present invention relates to tricyclic colchicine derivatives represented by the formulas (I) or (II), pharmaceutically acceptable salts thereof, and a method for providing an immuno-suppressive or immuno-modulating effect, an anti-proliferative effect, an anti-inflammatory effect or a method for treating cancer comprising administering to a patient an effective amount of one or more colchicine derivatives:Type: GrantFiled: July 10, 2006Date of Patent: November 24, 2009Assignees: Chemtech Research Incorporation, KT & G CorporationInventors: Dong Jo Chang, Eun Young Yoon, Gun Bong Lee, Soon Ok Kim, Wan Joo Kim
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Patent number: 7605288Abstract: Novel compounds useful for inhibiting the 90 kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.Type: GrantFiled: March 26, 2007Date of Patent: October 20, 2009Assignee: University of KansasInventors: Brian Blagg, Gang Shen, Randell C. Clevenger
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Publication number: 20090247627Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n 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: March 31, 2009Publication date: October 1, 2009Inventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
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Publication number: 20090192202Abstract: The present invention is directed to a new class of 4-cyano-phenoxy-alkyl carboxyl derivatives and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.Type: ApplicationFiled: February 9, 2009Publication date: July 30, 2009Inventors: Lain-Yen Hu, Huangshu Lei, Daniel Y. Du, Bruce A. Lefker, Yvonne Dorothy Smith, Victor Fedij
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Publication number: 20090182019Abstract: The present invention provides novel HDAC inhibitors and methods of treating diseases using the same.Type: ApplicationFiled: April 18, 2006Publication date: July 16, 2009Applicants: The Johns Hopkins University, Wayne State UniversityInventors: Robert A. Casero, Patrick M. Woster, Sheeba Varghese
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Publication number: 20090181971Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: ApplicationFiled: August 13, 2007Publication date: July 16, 2009Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg
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Publication number: 20090163588Abstract: This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.Type: ApplicationFiled: February 25, 2009Publication date: June 25, 2009Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Philip Stewart Turnbull, Rodolfo Cadilla, David John Cowan, Andrew Lamont Larkin, Istvan Kaldor, Eugene Lee Stewart
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Publication number: 20090131441Abstract: Metabolites of 2-(R)-4-isobutylarylpropionamides and pharmaceutical compositions containing such compounds are useful in inhibiting the chemotactic activation of neutrophils (PMN leukocytes) induced by the interaction of Interleukin-8 (IL-8) with CXCR1 and CXCR2 membrane receptors. The compounds are used for the prevention and treatment of pathologies deriving from said activation. Notably, these metabolites are devoid of cyclo-oxygenase inhibition activity and are particularly useful in the treatment of neutrophil-dependent pathologies such as psoriasis, ulcerative colitis, melanoma, chronic obstructive pulmonary disease (COPD), bullous pemphigoid, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and in the prevention and treatment of damages caused by ischemia and reperfusion.Type: ApplicationFiled: January 24, 2006Publication date: May 21, 2009Applicant: DOMPE phar.r.ma S.p.A.Inventors: Riccardo Bertini, Cinzia Bizzarri, Marco Mosca, Marcello Allegretti, Francesco Colotta
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Publication number: 20090076235Abstract: This invention relates to polymerizable ultraviolet light absorbers and yellow colorants and their use in ophthalmic lenses. In particular, this invention relates to polymerizable ultraviolet light absorbing methine compounds and yellow compounds of the methine and anthraquinone classes that block ultraviolet light and/or violet-blue light transmission through ophthalmic lenses.Type: ApplicationFiled: October 23, 2008Publication date: March 19, 2009Inventors: Jason Clay Pearson, Max Allen Weaver, Jean Carroll Fleischer, Gregory Allan King
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Publication number: 20090069431Abstract: The present application describes deuterium-enriched milnacipran, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 3, 2008Publication date: March 12, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Patent number: 7476754Abstract: The present invention relates to compounds derived from biphenyl with activity as calpain inhibitors. One compound of the present invention is a 2,2?-disubstituted biphenyl, where the substituents in the 2 and 2? positions of the biphenyl skeleton are chains containing structures related to amino acids, including fragments of aminocarbonylic compounds where at least one of the substituents in said 2- or 2?-positions is bonded to the biphenyl skeleton via a thiocarbonyl group, forming compounds with thioamide functionality. The present invention also encompasses any of the conformational isomers (atropisomers) of said compound of formula I. The compounds of formula I have application in the preventive or therapeutic treatment of a degenerative disease.Type: GrantFiled: May 6, 2005Date of Patent: January 13, 2009Assignee: Consejo Superior de Investigaciones CientificasInventors: Bernardo Herradon Garcia, Mercedes Alonso Giner, Esperanza Benito Cano, Antonio Chana Lopez, Ana Montero Aguado
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Publication number: 20080306041Abstract: The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one heterocyclic nitric oxide donor group, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension and (n) treating ophthalmic disorders. The cardiovascular compounds are preferably ?-adrenergic antagonists, angiotensin-converting enzyme (ACE) inhibitors, anti-hyperlipidemic compounds, and antithrombotic and vasodilator compounds.Type: ApplicationFiled: January 23, 2006Publication date: December 11, 2008Inventor: David S. Garvey
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Publication number: 20080280988Abstract: The present invention provides, as novel use of a certain (N?-methyl)benzoylurea compound in soil treatment for protecting the aerial part of a plant from damage by a pest, a method for protecting the aerial part of a plant from damage by a pest, which comprises a step of applying a (N?-methyl)benzoylurea compound represented by the formula (I): wherein R1 represents a hydrogen atom, a C1-C6 alkyl group optionally substituted with a halogen atom, or the like, R2 represents a halogen atom, or the like, and R3 represents a halogen atom, a C1-C4 alkyl group optionally substituted with a halogen atom, a C1-C4 alkoxy group optionally substituted with a halogen atom, or the like; to soil where the plant is grown.Type: ApplicationFiled: April 18, 2008Publication date: November 13, 2008Inventors: Norihisa Sakamoto, Masato Konobe
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Patent number: 7439356Abstract: The present invention relates to intermediates of the formula useful in the preparation of piperazinyl-substituted indan derivatives, wherein Y is CONR2 wherein R2 is H or C1-C6 alkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5, wherein R4 and R5 are as defined in the specification; and R9 is H, C1-C6 alkyl, C3-C6 cycloalkyl, OCF3, OCHF2, OCH2F, halogen, CN, CF3, OH, C1-C6 alkoxy, C1-C6 alkoxy-C1-C6 alkyl, NR6R7, SO3CH3, SO3CF3, SO2NR6R7, an unsubstituted or substituted heterocyclic or heteroaromatic ring containing one or two heteroatoms selected from N and O, wherein the substituent(s) is(are) C1-C6 alkyl; or COR8; wherein R6, R7 and R8 are as defined in the specification. The invention further relates to a process for the preparation of the intermediates.Type: GrantFiled: October 3, 2006Date of Patent: October 21, 2008Assignee: AstraZeneca ABInventors: Stefan Berg, Lennart Florvall, Svante Ross, Seth-Olov Thorberg
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Publication number: 20080242698Abstract: The invention relates to novel diamines of the formula in which all variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: ApplicationFiled: August 29, 2006Publication date: October 2, 2008Inventors: Peter Josef Flor, Andreas Marzinzik, Joachim Nozulak, Silvio Ofner, Bernard Lucien Roy, Carsten Spanka
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Publication number: 20080221166Abstract: The present invention relates to compounds of formula I wherein Ar1, Ar2, Ar3, n, and R1 to R8 are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. These compounds are orexin receptor antagonists and may be useful in the treatment of disorders, in which orexin pathways are involved, like sleep disorders.Type: ApplicationFiled: February 27, 2008Publication date: September 11, 2008Inventors: Luca Gobbi, Henner Knust, Parichehr Malherbe, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Patent number: RE41151Abstract: In accordance with the present invention, there are provided normal modified forms of nonsteroidal anti-inflammatory drugs. Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.Type: GrantFiled: August 20, 2008Date of Patent: February 23, 2010Assignee: Medinox, Inc.Inventors: Ching-San Lai, Tingmin Wang