The Substituent Nitrogen Is An Amino Nitrogen Attached Indirectly To A Ring By Acyclic Nonionic Bonding Patents (Class 564/164)
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Publication number: 20110218200Abstract: The present invention is directed to compounds that inhibit amyloid aggregation and methods of treatment there-with.Type: ApplicationFiled: August 28, 2009Publication date: September 8, 2011Inventors: Christopher J. Barden, Michael D. Carter, Mark A. Reed, Donald F. Weaver, Arun Yadav, Shengguo Sun
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Publication number: 20110212943Abstract: Provided herein are novel bridged cyclic derivatives of the general formula (I), their analogs, tautomeric forms, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds can inhibit HDACs and are useful as therapeutic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, autoimmune diseases, skin diseases, infections, inflammation, neurode-generative disorders etc.Type: ApplicationFiled: October 14, 2009Publication date: September 1, 2011Applicant: ORCHID RESEARCH LABORATORIES LIMITEDInventors: Gopalan Balasubramanian, Ponpandian Thanasekaran, Sridharan Rajagopal, Bharathimohan Kuppusamy, Virendra Kachhadia, Vignesh Radhakrishnan, Sivasudar Velaiah, Shridhar Narayanan, Mandar Bhonde, Praveen Rajendran, Sriram Rajagopal
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Publication number: 20110207783Abstract: The present invention relates to acyclic amino amide renin inhibitor compounds and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: August 4, 2008Publication date: August 25, 2011Inventors: Daniel Dube, Austin Chen, Daniel J. McKay
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Patent number: 8003689Abstract: This invention provides metabolites of SARM compounds including inter alia glucuronidated metabolites and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, muscle wasting disease and/or disorder, a bone related disease and/or disorder, metabolic syndrome, diabetes and associated diseases, and others.Type: GrantFiled: June 19, 2009Date of Patent: August 23, 2011Assignee: GTx, Inc.Inventor: Karen A. Veverka
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Publication number: 20110172310Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S, and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: ApplicationFiled: January 11, 2011Publication date: July 14, 2011Applicant: ViroBay, Inc.Inventors: John O. Link, Craig J. Mossman, Jie Liu, Soon Hyung Woo
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Patent number: 7968721Abstract: This invention relates to a process for preparing a selective androgen receptor modulator (SARM) compound represented by the structure of formula I: wherein X is O; and T, Z, Y, Q, R and R1 are defined herein. The process includes coupling between an amide of formula II and a phenol of formula III followed by a purification step consisting of precipitating the compound of formula (I) in a mixture of alcohol and water alone.Type: GrantFiled: January 12, 2004Date of Patent: June 28, 2011Assignee: University of Tennessee Research FoundationInventors: Duane D. Miller, Karen A. Veverka, Kiwon Chung
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Publication number: 20110144210Abstract: The present invention relates to stable dosage forms of levomilnacipran and pharmaceutically acceptable salts thereof. Processes for the preparation of these dosage forms and methods of using these dosage forms are also described.Type: ApplicationFiled: January 14, 2011Publication date: June 16, 2011Applicant: FOREST LABORATORIES HOLDINGS LTD.Inventors: Anil Chhettry, Murali Divi, Rahul Surana
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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
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Publication number: 20110112197Abstract: The present invention relates to novel crystalline forms of (1S,2R)-2-(amino methyl)-N,N-diethyl-1-phenyl cyclopropane carboxamide. Processes for the preparation of this form, compositions containing the form, and methods of use thereof are also described.Type: ApplicationFiled: November 8, 2010Publication date: May 12, 2011Applicant: FOREST LABORATORIES HOLDINGS LTD.Inventors: Mahendra G. Dedhiya, Rahul Surana
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Patent number: 7939541Abstract: This invention relates to a process for the preparation of (3-trifluoromethylsulfonyl)-N-[4-methyl-3-(4-pyridin-3yl-pyrimidin-2ylamino)-phenyl]-benzamide (formula (I)) starting from 4-methyl-2-nitro-aniline (formula (II)) through intermediates (3-trifluoromethylsulfonyl)-N-[4-methyl-3-nitrophenyl]-benzamide (formula (III)), (3-trifluoromethylsulfonyl)-N-[3-amino-4-methylphenyl]-benzamide (formula (IV)) and (3-trifluoromethylsulfonyl)-N-[3-guanidino-4-methylphenyl]-benzamide (formula (V)). This invention also relates to processes for the preparation of these intermediates.Type: GrantFiled: March 4, 2008Date of Patent: May 10, 2011Assignee: Natco Pharma LimitedInventors: Amala kishan Kompella, Bhujanga rao Adibhatla Kali Satya, Sreenivas Rachakonda, Nannapaneni Venkaiah Chowdary
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Patent number: 7893112Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S, and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: GrantFiled: April 1, 2008Date of Patent: February 22, 2011Assignee: Virobay, Inc.Inventors: John O. Link, Craig J. Mossman, Jie Liu, Soon Hyung Woo
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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: 20100324046Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 24, 2008Publication date: December 23, 2010Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
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Patent number: 7851642Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.Type: GrantFiled: June 12, 2009Date of Patent: December 14, 2010Assignee: Novartis AGInventors: Daniel Kaspar Baeschlin, Juergen Klaus Maibaum, Holger Sellner
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Publication number: 20100298593Abstract: The present invention provides a methoxyimino compound, and a fungicide composition comprising same as an active ingredient. The methoxyimino compound of the present invention, which has an excellent antifungal activity against a wide spectrum of fungi even at a low application rate, can be used to protect various crops.Type: ApplicationFiled: December 5, 2008Publication date: November 25, 2010Applicant: KYUNG NONG CORPORATIONInventors: Joo-Kyung Kim, Hyung-Ho Kim, In-Cheon Hwang, Ho-tae Nam
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Publication number: 20100292509Abstract: A bloating ameliorant, a lymphatic vessel activator and a VEGFC production promoter comprising a tranexamic acid amide derivative and/or salt thereof.Type: ApplicationFiled: January 16, 2009Publication date: November 18, 2010Inventors: Kentaro Kajiya, Eriko Taguchi
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Publication number: 20100274050Abstract: The present invention provides novel solid milnacipran in crystalline form-G and a process for its preparation. The present invention also provides a process for the preparation of milnacipran hydrochloride from the novel solid crystalline milnacipran.Type: ApplicationFiled: July 6, 2009Publication date: October 28, 2010Applicant: Glenmark Generics LimitedInventors: Joseph Prabahar KOILPILLAI, Pravin Chhaburao THOMBRE, Sudam Nanabhau SINARE, Mubeen Ahmed KHAN
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Publication number: 20100168243Abstract: The present invention is directed to aspartic protease inhibitors. The present invention is also directed to pharmaceutical compositions comprising the disclosed aspartic protease inhibitors. The present invention is further directed to methods of antagonizing one or more aspartic proteases in a subject in need thereof, and methods for treating an aspartic protease mediated disorder in a subject using the disclosed aspartic protease inhibitors.Type: ApplicationFiled: June 20, 2008Publication date: July 1, 2010Inventors: John J. Baldwin, Salvacion Cacatian, David A. Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Alexey V. Ishehenko, Lanqi Jia, Gerard McGeehan, Robert D. Simpson, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Jing Yuan, Wei Zhao, Linghang Zhuang, Jing Zhang
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Patent number: 7745492Abstract: This invention is directed to carboxamido opioid compounds pharmaceutically useful as agents for treating or modulating a central nervous system disorder and methods for treating or modulating a central nervous system disorder.Type: GrantFiled: July 30, 2008Date of Patent: June 29, 2010Assignee: Janssen PharmaceuticalInventors: John R. Carson, Philip M. Pitis
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Publication number: 20100143391Abstract: The invention generally relates to hapten compounds comprising either (+)methamphetamine or (+)amphetamine conjugated to a linker. Generally speaking, hapten compounds of the invention may be used to elicit an immune response to one or more of (+)methamphetamine, (+)amphetamine, or (+)MDMA.Type: ApplicationFiled: April 18, 2008Publication date: June 10, 2010Applicant: The Board of Trustees of the University of ArkansasInventors: S. Michael Owens, Melinda Gunnell, F. Ivy Carroll
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Publication number: 20100145099Abstract: The present invention relates to polymorphic forms of milnacipran hydrochloride. The polymorphic forms are designated as Form (I), Form (II), Form (III), Form (IV) and Form V of milnacipran hydrochloride. The present invention also relates to processes for the preparation of the polymorphic forms.Type: ApplicationFiled: February 28, 2008Publication date: June 10, 2010Applicant: RANBAXY LABORATORIES LIMITEDInventors: Roshan Ramesh Medhane, Nitin Maheswari, Keshav Deo, Mohan Prasad, Joydeep Kant
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Publication number: 20100144808Abstract: Disclosed is a novel pest control agent, in particular a pesticide or a miticide. Specifically disclosed are a substituted isoxazoline compound or a substituted enone oxime compound represented by the general formula (1) below or the general formula (2) below, and a pest control agent containing any of them. (In the formulae, the symbols are as defined in the description.Type: ApplicationFiled: June 27, 2008Publication date: June 10, 2010Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Takeshi Mita, Kenichi Toyama, Yuki Furukawa, Mitsuaki Komoda
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Patent number: 7671033Abstract: An amphiphilic dendritic dipeptide, comprises a dipeptide(s) comprising one or more of a naturally occurring or synthetic amino acids and a dendron. These are suitable for use in various formulations, films, coatings, membranes and sensors, among other applications.Type: GrantFiled: July 1, 2005Date of Patent: March 2, 2010Assignee: The Trustees of The University of PennsylvaniaInventor: Virgil Percec
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Publication number: 20100016636Abstract: The present invention discloses a process for preparing optically pure milnacipran and their pharmaceutically acceptable salts, which adopts racemic milnacipran as starting material, tartaric acid derivatives and their compositions as resolving agents to resolve.Type: ApplicationFiled: November 28, 2007Publication date: January 21, 2010Inventors: Lin Ai, Xiao Liu
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Publication number: 20100004326Abstract: This invention provides metabolites of SARM compounds including inter alia glucuronidated metabolites and uses thereof in treating a variety of diseases or conditions in a subject, including, inter alia, muscle wasting disease and/or disorder, a bone related disease and/or disorder, metabolic syndrome, diabetes and associated diseases, and others.Type: ApplicationFiled: June 19, 2009Publication date: January 7, 2010Inventor: Karen A. VEVERKA
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Patent number: 7632850Abstract: The present invention provides a compound of the formula (I): in which R1, R2, R3, A and n are described and set forth more fully herein. Also provided are their preparation and their application in therapy.Type: GrantFiled: July 21, 2005Date of Patent: December 15, 2009Assignee: Sanofi-aventisInventors: Ahmed Abouabdellah, Antonio Almario Garcia, Christian Hoornaert, Antoine Ravet
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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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Publication number: 20090291988Abstract: The instant invention relates to compounds of formula I, diagrammed below, wherein R3, E, D and Y are defined in the application, which are useful as reversible inhibitors of monoamine oxidase-B and/or monoamine oxidase-A, and therefore useful to treat or prevent neurological diseases or conditions in mammals, preferably humans.Type: ApplicationFiled: June 14, 2006Publication date: November 26, 2009Inventor: Renata Oballa
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Publication number: 20090291945Abstract: To provide a compound having an excellent cysteine protease inhibitory effect, and to provide a drug for treatment or prevention of the disease selected from the group consisting of osteoporosis, osteoarthritis, chronic rheumatoid arthritis, Paget's disease of bone, hypercalcemia, bone metastasis of cancer, and ostealgia. A compound represented by formula (1) or a pharmaceutically acceptable salt thereof, or a drug or pharmaceutical composition containing the same as an effective component.Type: ApplicationFiled: April 7, 2009Publication date: November 26, 2009Applicant: Teijin Pharma LimitedInventors: Gen Unoki, Takashi Hayamizu, Hiroshi Eguchi, Yumiko Muroga, Toshiyuki Kaneko, Naoki Yajima
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Publication number: 20090253166Abstract: Methods for the selective conjugation of peptides which comprises an enzymatic incorporation of a functional group at the C-terminal end of a peptide followed by reaction with a second compound comprising the moiety to be conjugated to the peptide, wherein said second compound comprises a functional group which selectively reacts with the incorporated functional group.Type: ApplicationFiled: March 18, 2009Publication date: October 8, 2009Applicant: Novo Nordisk A/SInventors: Magali A. Zundel, Bernd Peschke, Florencio Zaragoza Dorwald, Niels Peter Fiil, Nils Langeland Johansen, Henning Ralf Stennicke
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Patent number: 7598419Abstract: Novel styrylacrylonitrile compounds which are useful in treating a variety of cell proliferative disorders such as cancer are disclosed.Type: GrantFiled: March 22, 2005Date of Patent: October 6, 2009Assignee: HSC Research and Development Limited PartnershipInventors: Chaim M. Roifman, Peter Demin, Andrew Freywald, Thomas Grunberger, Olga Rounova, Nigel Sharfe
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Patent number: 7592485Abstract: The present invention provides a process for producing (Z)-1-phenyl-1-diethylaminocarbonyl-2-aminomethylcyclopropane or hydrochloride thereof, which comprises a step of reacting (Z)-1-phenyl-1-diethylaminocarbonyl-2-phthalimidomethylcyclopropane by contacting said compound with an aqueous methylamine solution having a concentration of from 1 to 25% by weight to obtain (Z)-1-phenyl-1-diethylaminocarbonyl-2-aminomethylcyclopropane.Type: GrantFiled: June 23, 2005Date of Patent: September 22, 2009Assignee: Sumitomo Chemical Company, LimitedInventors: Yoshihide Niimoto, Hiroharu Kumazawa, Osamu Tokuda, Fumiaki Ibukuro
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Publication number: 20090209787Abstract: The present invention encompasses a process for preparing compounds of formula (1), wherein a compound of general formula (2) is reacted in the presence of a catalyst and a solvent under hydrogen pressure to form a compound of general formula (1) and wherein A and R1-R4 are defined as in claim 1.Type: ApplicationFiled: May 15, 2007Publication date: August 20, 2009Inventors: Guenter Linz, Gerd Kraemer, Zeno Andreas Leuter, Markus Ostermeier, Werner Rall, Claudia Ochs, Rolf Schmid
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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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Patent number: 7553969Abstract: Substituted phenethylamine compounds of Formula (1) that function as motilin receptor antagonists: Formula (1).Type: GrantFiled: January 28, 2000Date of Patent: June 30, 2009Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Hiroharu Matsuoka, Tsutomu Sato, Tadakatsu Takahashi, Dong Ick Kim, Kyung Yun Jung, Chan Hee Park
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Publication number: 20090163549Abstract: The present invention provides a novel modulator of the TRPV1-receptor function, comprising a compound of the formula; wherein ring A is an optionally substituted carbocycle or heterocycle, ring B is an optionally substituted benzene ring or an optionally substituted 6-membered heteroaromatic ring containing N atom, a dashed line means existence or absence of a bond, n is 1 or 2, R1 and R2 are hydrogen etc., R3 is lower alkyl, R4 is lower alkyl or aryloxy, or R3 and R4 taken together may form optionally substituted 5- or 6-membered non-aromatic heterocycle.Type: ApplicationFiled: December 13, 2006Publication date: June 25, 2009Inventor: Hiroyuki Kai
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Publication number: 20090137681Abstract: Provided herein are compositions and methods for treating or preventing cancer and autoimmune diseases. Compositions comprise a sirtuin inhibitory compound that decreases the activity of a sirtuin, such as SIRT1 or Sir2. Exemplary methods comprise contacting a cell or a molecule with a sirtuin inhibitory compound that decreases the activity of a sirtuin and thereby reduces the life span of a cell, kills the cell or renders it susceptible to certain cell stresses including radiation and chemotherapy. Other methods include treating pathogens expressing a sirtuin.Type: ApplicationFiled: April 6, 2006Publication date: May 28, 2009Inventors: David A Sinclair, Antonello Mai
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Publication number: 20090118339Abstract: The present invention concerns lysine related derivatives, their use as protease inhibitors, in particular as HIV aspartyl protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. The present invention also concerns combinations of the present lysine related derivatives with another anti retroviral agent. It further relates to their use in assays as reference compounds or as reagents.Type: ApplicationFiled: May 30, 2007Publication date: May 7, 2009Inventors: Tim Hugo Maria Jonckers, Inge Dierynck, Stefaan Julien Last, Herman De Kock
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Publication number: 20080293819Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S, and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.Type: ApplicationFiled: April 1, 2008Publication date: November 27, 2008Applicant: ViroBay, Inc.Inventors: John O. Link, Craig J. Mossman, Jie Liu
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Patent number: 7449315Abstract: Energy-reversible acyl conjugates, intermediates, and related compositions are disclosed.Type: GrantFiled: March 30, 2007Date of Patent: November 11, 2008Assignee: Cryolife, Inc.Inventors: Carl W. Gilbert, Eleanor B. McGowan, Kirby S. Black, T. Gregory P. Harper
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Publication number: 20080255205Abstract: The present invention relates to compounds of Formulas I and II, wherein B1, B2, B3, B4, C1, C2, ring D, L1, L2 and R1-4 are defined herein, synthetic intermediates, and pharmaceutical compositions, comprising such compounds. The compounds and compositions are capable of modulating various protein kinase receptors such as Tie-2 and Aurora and, therefore, influencing kinase related disease states and conditions. The compounds, for example, are capable of treating cancer caused by unregulated angiogenesis, and inflammation as well as other proliferative disorders.Type: ApplicationFiled: October 25, 2007Publication date: October 16, 2008Applicant: Amgen Inc.Inventors: Brian L. Hodous, Stephanie D. Geuns-Meyer, Philip R. Olivieri, Vinod F. Patel, Paul A. Tempest
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Publication number: 20080234254Abstract: The present invention relates to a benzamide derivative comprising a head, spacer and cap group wherein the spacer includes a benzene ring substituted with an additional spacer and wherein the additional spacer is an unsaturated group.Type: ApplicationFiled: June 7, 2005Publication date: September 25, 2008Applicant: UNIVERSITY OF LEEDSInventors: Ronald Grigg, Andrew Cook
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Patent number: 7423154Abstract: An asymmetric synthesis of diarylmethylpiperazines is described. The synthetic route enables preparation of a variety of enatiomerically pure amines with different N-alkyl groups. The invention includes an asymmetric addition of organometallic compounds to chiral sulfinimine to give adducts in predominantly one diastereomer can subsequently be transferred into pure enantiomers of by cleavage of the chiral auxilliary which is followed by synthesis of the piperazine ring by alkylation procedures.Type: GrantFiled: November 22, 2005Date of Patent: September 9, 2008Assignee: AstraZeneca ABInventors: William Brown, Niklas Plobeck
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Publication number: 20080188529Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.Type: ApplicationFiled: April 8, 2008Publication date: August 7, 2008Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra Baskaran
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Patent number: 7390925Abstract: There is provided a series of substituted oxime-containing acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, their pharmaceutical compositions and methods of use. These compounds inhibit the processing of amyloid precursor protein (APP) by ?-secretase and, more specifically, inhibit the production of A?-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to ?-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.Type: GrantFiled: March 29, 2007Date of Patent: June 24, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Samuel Gerritz, Shuhao Shi, Shirong Zhu
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Patent number: 7390923Abstract: Compounds of formula (I) wherein R1 to R4, X and A are as defined in the claims and pharmaceutically acceptable salts and esters thereof, are disclosed. The compounds of formula (I) possess utility as tissue-selective androgen receptor modulators (SARM) and are useful in hormonal therapy, e.g., in the treatment or prevention of male hypogonadism and age-related conditions such as andropause.Type: GrantFiled: June 24, 2004Date of Patent: June 24, 2008Assignee: Orion CorporationInventors: Jari Ratilainen, Anu Moilanen, Olli Törmäkangas, Arja Karjalainen, Paavo Huhtala, Gerd Wohlfahrt, Pekka Kallio
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Publication number: 20080139636Abstract: The invention provides adamantane derivatives of formula (I), a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy. In formula (I) D represents CH2 or CH2CH2, E represents C(O)NH or NHC(O) and R3 represents a group of formula (I).Type: ApplicationFiled: June 20, 2007Publication date: June 12, 2008Inventors: Lilian Alcaraz, Moya Caffrey, Mark Furber, Timothy Luker, Michael Mortimore, Austen Pimm, Philip Thorne, Paul Willis
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Publication number: 20080125491Abstract: The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In certain embodiments, the GPCR is human. In certain embodiments, the GPCR is expressed endogenously by neuronal cells or muscle cells. In certain embodiments, the GPCR is neuroprotective or myoprotective. In certain embodiments, the GPCR is a Humanin receptor. The present invention also relates to methods of using a modulator of said GPCR. A preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of neurodegenerative diseases in general, including Alzheimer's disease, Parkinson's disease, prion-associated disease, stroke and motor-neuron disease in particular, peripheral neuropathy, cerebral amyloid beta-protein angiopathy, and ischemic heart disease, including myocardial infarction and congestive heart failure.Type: ApplicationFiled: March 15, 2004Publication date: May 29, 2008Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Sonia Villegas, Gregory S. Kelner, David J. Unett, Joel Gatlin
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Patent number: 7282608Abstract: The invention provides compoods and methods for treating cell proliferative-diseases. The invention provides new inhibitors of histone deacetylase enzymatic activity, compositions of the compounds comprising the inhibitors and a pharmaceutically acceptable carrier, excipient, or diluent, and methods of using the compounds to inhibit cellular proliferation in vitro and therapeutically.Type: GrantFiled: October 16, 2003Date of Patent: October 16, 2007Assignee: Methylgene, Inc.Inventors: Stephane Raeppel, Frederic Gaudette, Daniel Delorme
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Patent number: RE40259Abstract: The present invention relates to novel and known alpha-aminoamide compounds, to a process for their preparation, to pharmaceutical composition containing them and to their use as therapeutic agents. In particular, the compounds of the present invention are endowed with analgesic properties and are particularly useful for the treatment and alleviation of chronic and neuropathic pain.Type: GrantFiled: December 12, 1998Date of Patent: April 22, 2008Assignee: Newron Pharmaceuticals, S.p.A.Inventors: Paolo Pevarello, Mario Varasi, Patricia Salvati, Claes Post