Plural Carboxamide Groups Or Plural C=o Groups Bonded Directly To The Same Nitrogen Patents (Class 514/616)
-
Publication number: 20120094971Abstract: This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.Type: ApplicationFiled: September 3, 2009Publication date: April 19, 2012Applicant: REPLIGEN CORPORATIONInventors: James R. Rusche, Norton P. Peet, Allen T. Hopper
-
Publication number: 20120088794Abstract: The invention provides aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, n, and m are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: December 19, 2011Publication date: April 12, 2012Applicant: THERAVANCE, INC.Inventors: Michael R. Leadbetter, Sean G. Trapp, Daniel D. Long, John R. Jacobsen, Sabine Axt
-
Publication number: 20120083533Abstract: A therapy for renal diseases, in particular renal diseases which develop in diabetic patients or patients who have been subjected to a treatment with an antitumor chemotherapy such as a platinum derivative and more generally cytotoxic drugs at renal level for treating of neoplastic diseases. More particularly, the present invention relates to palmitoylethanolamide and diethanolamide of fumaric acid for use in the treatment of renal diseases, in particular those caused by dysmetabolic diseases or by toxic or chemotherapy agents, such as platinum derivatives. Palmitoylethanolamide is used preferably in micronized or ultra-micronized form. Diethanolamide of fumaric acid is used preferably in aqueous solution.Type: ApplicationFiled: October 3, 2011Publication date: April 5, 2012Inventors: Francesco Della Valle, Raffacle Migliaccio, Maria Federica Della Valle
-
Publication number: 20120083493Abstract: Provided are small-molecule Trp-p8 modulators, including Trp-p8 agonists and Trp-p8 antagonists, and compositions comprising small-molecule Trp-p8 agonists as well as methods for identifying and characterizing novel small-molecule Trp-p8 modulators and methods for decreasing viability and/or inhibiting growth of Trp-p8 expressing cells, methods for activating Trp-p8-mediated cation influx, methods for stimulating apoptosis and/or necrosis, and related methods for the treatment of diseases, including cancers such as lung, breast, colon, and/or prostate cancers as well as other diseases, such as benign prostatic hyperplasia, that are associated with Trp-p8 expression.Type: ApplicationFiled: August 9, 2010Publication date: April 5, 2012Applicant: Dendreon CorporationInventors: Ofir Moreno, Sateesh Natarajan, David F. Duncan
-
Publication number: 20120083440Abstract: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; and a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion.Type: ApplicationFiled: October 5, 2011Publication date: April 5, 2012Inventors: William M. Pierce, JR., K. Grant Taylor, Leonard C. Waite, Kevyn Merten
-
Patent number: 8148576Abstract: The invention relates to solid states of pharmaceutically acceptable compounds of aliskiren, and processes for preparation thereof. The invention further provides pharmaceutical formulations comprising the amorphous or crystalline forms of pharmaceutically acceptable compounds of aliskiren and processes thereof; and a method of inhibiting renin for treating hypertension.Type: GrantFiled: February 5, 2010Date of Patent: April 3, 2012Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Nina Finkelstein, Ariel Mittelman
-
Patent number: 8143445Abstract: This invention provides the compound having the structure wherein n is 1-10; X is C—R11 or N, wherein R11 is H, OH, SH, F, Cl, SO2R7, NO2, trifluoromethyl, methoxy, or CO—R7, wherein R7 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl; Z is R2 is H or NR3R4, wherein R3 and R4 are each independently H, C1-C6 alkyl, or C3-C8 cycloalkyl; R5 is OH or SH; and R6, R12, R13, and R14 are each independently H, OH, SH, F, Cl, SO2R15, NO2, trifluoromethyl, methoxy, or CO—R15 wherein R15 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl, or a salt of the compound, which is useful in the treatment of tumors.Type: GrantFiled: October 1, 2008Date of Patent: March 27, 2012Assignee: Lixte Biotechnology, Inc.Inventors: John S. Kovach, Francis Johnson
-
Patent number: 8143242Abstract: The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: January 7, 2010Date of Patent: March 27, 2012Assignee: Sanofi-AventisInventors: Henning Steinhagen, Hauke Szillat, Markus Follmann, Reinhard Kirsch, Volkmar Wehner, Hans Matter, Martin Lorenz, Kent W. Neuenschwander, Anthony C. Scotese
-
Patent number: 8143446Abstract: A pharmaceutical composition comprising a compound having Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; R2 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; and X is, for example, a hydroxyl group or a C1-C6 alkoxy group].Type: GrantFiled: May 11, 2006Date of Patent: March 27, 2012Assignee: Daiichi Sankyo Company, LimitedInventors: Kazumasa Aoki, Koji Suda, Toshio Kaneko, Tomio Kimura
-
Patent number: 8143418Abstract: Caspase activity and apoptosis are promoted using active, dimeric Smac peptide mimetics of the general formula M1-L-M2, wherein moieties M1 and M2 are monomeric Smac mimetics and L is a covalent linker. Target cancerous or inflammatory cells are contacted with an effective amount of an active, dimeric Smac mimetic, and a resultant increase in apoptosis of the target cells is detected. The contacting step may be effected by administering to a pharmaceutical composition comprising a therapeutically effective amount of The compoundic mimetic, wherein the individual may be subject to concurrent or antecedent radiation or chemotherapy for treatment of a neoproliferative pathology.Type: GrantFiled: February 7, 2011Date of Patent: March 27, 2012Assignee: Board of Regents, The University of Texas SystemInventors: Patrick G. Harran, Xiaodong Wang, Jef K. De Brabander, Lin Li, Ranny Mathew Thomas, Hidetaka Suzuki
-
Publication number: 20120071528Abstract: The invention is directed to novel compounds of Formula I: as well as its stereoisomers and/or pharmaceutically acceptable salts, for the treatment of diabetes and diabetes associated dyslipidemia.Type: ApplicationFiled: September 20, 2011Publication date: March 22, 2012Applicant: KAREUS THERAPEUTICS, SAInventors: Ish Khanna, Sivaram Pillarisetti
-
Publication number: 20120070369Abstract: The present invention is directed to HIF inhibitors and methods of preventing cell proliferation, reducing inflammation, and treating an angiogenic disease or disorders.Type: ApplicationFiled: December 10, 2009Publication date: March 22, 2012Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Othon Iliopoulos, Michael Zimmer
-
Publication number: 20120071539Abstract: Methods and compositions comprising chemical compounds that modulate the silencing of a polynucleotide of interest in a cell are provided. Such chemical compounds when used in combination with an appropriate silencing element can be used to modulate (increase or decrease) the level of the polynucleotide targeted by the silencing element. Methods of using such compositions both in therapies involving RNAi-mediated suppression of gene expression, as well as, in vitro methods that allow for the targeted modulation of expression of a polynucleotide of interest are provided. Pharmaceutical or cosmetic compositions comprising such compounds and silencing elements also are disclosed. Methods for screening a compound of interest for the ability to modulate the activity of a heterologous silencing element also are provided.Type: ApplicationFiled: December 12, 2007Publication date: March 22, 2012Applicant: Emory UniversityInventor: Peng Jin
-
Publication number: 20120070394Abstract: The invention concerns a methionine-derived peptidomimetic represented by the following general formula (II): R=X—C(O)—NH— with X=alkyl or alkyloxy (C1-C4); R?=H The invention also concerns a composition for preventing or fighting cutaneous disorders associated to a mitochondrial dysfunction, and the use of a methionine-derived peptidomimetic as a cosmetic agent for protecting and/or stimulating the mitochondria of cutaneous cells.Type: ApplicationFiled: September 16, 2011Publication date: March 22, 2012Applicant: EXSYMOL S.A.M.Inventor: Marie-Christine Seguin
-
Publication number: 20120053212Abstract: A human undergoing an injection of a contrast agent is treated by the administration of an iron chelator. Administration of the iron chelator can essentially prevent the onset of acute renal failure in a human. Administration of the iron chelator can reduce the severity of the acute renal failure and/or reduce the severity of kidney disease consequent to the acute renal failure.Type: ApplicationFiled: March 29, 2011Publication date: March 1, 2012Applicant: Shiva Biomedical, LLCInventor: Sudhir V. Shah
-
Patent number: 8124121Abstract: The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers, —savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.Type: GrantFiled: October 23, 2008Date of Patent: February 28, 2012Assignee: Senomyx, Inc.Inventors: Catherine Tachdjian, Andrew P. Patron, Sara L. Adamski-Werner, Farid Bakir, Qing Chen, Vincent Darmohusodo, Stephen Terrence Hobson, Xiaodong Li, Ming Qi, Daniel H. Rogers, Marketa Rinnova, Guy Servant, Xiao-Qing Tang, Mark Zoller, David Wallace, Amy Xing, Klaus Gubernator
-
Publication number: 20120046272Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.Type: ApplicationFiled: August 19, 2011Publication date: February 23, 2012Applicant: GRUNENTHAL GMBHInventor: Ramesh SESHA
-
Publication number: 20120046226Abstract: The invention concerns a novel treatment multiple sclerosis, based on induced anaemia, followed by administration of an erythropoiesis-stimulating agent (ESA). In a preferred embodiment, the ESA is darbopoietin alpha, CERA or Hematide. The anaemia is induced by successive bloodlettings or by administration of an iron chelator, such as deferiprone, deferoxamine, polyanionic amines, substituted polyaza compounds, desferrithiocon, hydroxybenzyl-ethylenediamine-diacetic acid and pyridoxal isonicotinoyl hydra z one.Type: ApplicationFiled: February 12, 2010Publication date: February 23, 2012Applicant: Assis-tance Publique - Hopitaux de ParisInventors: Alain Creange, Frédéric Galacteros, Jean-Pascal Lefaucheur
-
Patent number: 8119685Abstract: The present invention relates to a novel class of disubstituted aniline compounds. These compounds can 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: GrantFiled: April 20, 2007Date of Patent: February 21, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Heidebrecht, Joey Methot, Dawn Mampreian, Thomas Miller, Phieng Siliphaivanh
-
Patent number: 8119841Abstract: This invention relates to crystal forms of aliskiren hemifumarate and various embodiments related thereto, e.g. pharmaceutical preparations, processes for the manufacture of the crystal forms, pharmaceuticals uses and the like. The crystal forms have particularly advantageous properties e.g. they are useful in the manufacture of blood-pressure lowering pharmaceutical preparations and the like.Type: GrantFiled: November 5, 2007Date of Patent: February 21, 2012Assignee: Novartis AGInventors: Frank Stowasser, Stephanie Monnier
-
Publication number: 20120039909Abstract: The invention relates to methods and products for enhancing and improving recovery of lost memories. In particular the methods are accomplished through the increase of histone acetylation.Type: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Applicants: The General Hospital Corporation d/b/a Massachusetts General Hospital, Massachusetts Institute of Technology, President and Fellows of Harvard CollegeInventors: Li-Huei Tsai, Andre Fischer, Stephen Haggarty, Weiping Tang, Stuart L. Schreiber
-
Publication number: 20120039893Abstract: The emergence of mutations in tyrosine kinases following treatment of cancer patients with molecular-targeted therapy represents a major mechanism of acquired drug resistance. Here, we describe a mutation in the serpentine receptor, Smoothened (SMO), which results in resistance to a Hedgehog (Hh) pathway inhibitor in medulloblastoma. A single amino acid substitution in a conserved glutamic acid residue of SMO maintains Hh signaling, but results in the inability of the Hh pathway inhibitor, GDC-0449, to bind SMO and suppress the pathway. The invention provides screening methods to detect SMO mutations and methods to screen for drugs that specifically modulate mutant SMO exhibiting drug resistance.Type: ApplicationFiled: October 5, 2011Publication date: February 16, 2012Applicant: Genentech, Inc.Inventor: Frederic J. de Sauvage
-
Publication number: 20120041067Abstract: The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo.Type: ApplicationFiled: October 19, 2011Publication date: February 16, 2012Inventors: Victoria M. Richon, Judy H. Chiao, William Kevin Kelly, Thomas A. Miller
-
Publication number: 20120027844Abstract: Compounds and their syntheses are disclosed herein. Compositions and pharmaceutical compositions comprising a compound are also described, and include compositions also comprising liposomes. Methods for the treatment of cancer in animals comprising administering a compound or a composition comprising a compound are also described.Type: ApplicationFiled: February 9, 2010Publication date: February 2, 2012Applicants: XAVIER UNIVERSITY OF LOUISIANA, TULANE UNIVERSITYInventors: Barbara S. Beckman, Maryam Foroozesh, Jiawang Liu
-
Publication number: 20120029083Abstract: Provided are amorphous and polymorphic forms of aliskiren hemifumarate, pharmaceutical compositions thereof, and processes for their preparation.Type: ApplicationFiled: November 13, 2008Publication date: February 2, 2012Inventors: Nina Finkelstein, Boris Finkelstein, Ariel Mittelman, Tamás Koltai
-
Publication number: 20120028995Abstract: The invention relates to compounds of general formula (I) as set forth in the claims as well as to the use of the compounds of the general formula (1) in the medical field, specifically for use in the suppression of DNA synthesis and inflammatory cytokine production as well as in the stimulation of anti-inflammatory cytokine production in vitro and in vivo. This abstract is neither intended to define the invention disclosed in this specification nor intended to limit the scope of the invention in any way.Type: ApplicationFiled: July 19, 2011Publication date: February 2, 2012Applicant: IMTM GMBHInventors: Siegfried ANSORGE, Ute BANK, Anke HEIMBURG, Heiko JULIUS, Karsten NORDHOFF, Michael TAEGER
-
Publication number: 20120029067Abstract: The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.Type: ApplicationFiled: October 11, 2011Publication date: February 2, 2012Applicants: UNIVERSITY OF SOUTH FLORIDA, THE HONG KONG POLYTECHNIC UNIVERSITY, MCGILL UNIVERSITYInventors: Q. Ping DOU, Tak-Hang CHAN, David M. SMITH
-
Publication number: 20120021989Abstract: The invention relates to procedures and methods of determining a susceptibility to cardiac arrhythmia, including Atrial Fibrillation, Atrial Flutter and Stroke, by assessing the presence or absence of alleles at polymorphic markers found to be associated with risk of these conditions. The invention further relates to kits encompassing reagents for assessing such markers, and diagnostic 5 methods, uses and procedures for utilizing such susceptibility markers.Type: ApplicationFiled: March 30, 2010Publication date: January 26, 2012Applicant: deCODE Genetics ehf.Inventors: Hilma Holm, Daniel Gudbjartsson
-
Publication number: 20120015992Abstract: Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, or NHSO2X, wherein X is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, heterocycle, or substituted heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.Type: ApplicationFiled: September 21, 2011Publication date: January 19, 2012Applicant: Burnham Institute for Medical ResearchInventor: Maurizio Pellecchia
-
Publication number: 20120016035Abstract: The invention relates to a combination comprising the renin inhibitor of formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 19, 2011Publication date: January 19, 2012Inventors: William Hewitt, Daniel Lucius Vasella, Randy Lee Webb
-
Patent number: 8097758Abstract: The invention relates to the compounds of formula (I) having antithrombotic activity which especially inhibit blood clotting factor IXa, to methods for producing the same and to the use thereof as drugs.Type: GrantFiled: March 9, 2009Date of Patent: January 17, 2012Assignee: Sanofi-AventisInventors: Henning Steinhagen, Markus Follmann, Jochen Goerlitzer, Herman Schreuder
-
Publication number: 20120010295Abstract: The invention relates to a combination comprising the renin inhibitor of formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 19, 2011Publication date: January 12, 2012Inventors: William Hewitt, Daniel Lucius Vasella, Randy Lee Webb
-
Publication number: 20120004209Abstract: A novel class of compounds of the general formula (I), their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds modulate the activity of 11?-hydroxy-steroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, e.g. the metabolic syndrome.Type: ApplicationFiled: September 19, 2011Publication date: January 5, 2012Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Soren Ebdrup, Henrik Sune Andersen
-
Publication number: 20120004311Abstract: A compound of Formula I: or a pharmaceutically acceptable salt thereof is disclosed. In addition, pharmaceutical compositions thereof, methods for preparing and methods for using this compound or composition for treating a variety of diseases, including cancer and inflammation are also provided.Type: ApplicationFiled: December 3, 2010Publication date: January 5, 2012Applicant: Sanford-Burnham Medical Research InstituteInventor: Maurizio Pellecchia
-
Publication number: 20120004243Abstract: The invention concerns a compound of the Formula (I), wherein Qa is heteroaryl and is substituted with halogeno; R1 and R2 are hydrogen; and Qb is phenyl or heteroaryl, and Qb may optionally bear 1 or 2 substituents selected from hydroxy, halogeno and (1-6C)alkyl, or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: April 5, 2011Publication date: January 5, 2012Applicant: AstraZeneca ABInventors: Dearg Sutherland Brown, John Graham Cumming, Ian Alun Nash
-
Publication number: 20120003242Abstract: This invention relates to PCIF1 and its use as a target for the improvement of pancreatic islet ? cell mass and function in diabetes. Specifically, the invention relates to the use of compounds capable of modulating the expression or function of PCIF1 and their effect on the function of Pdx-1.Type: ApplicationFiled: March 3, 2008Publication date: January 5, 2012Inventor: Doris Stoffers
-
Publication number: 20120004312Abstract: The invention relates to a combination comprising the renin inhibitor of formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: September 19, 2011Publication date: January 5, 2012Inventors: William Hewitt, Daniel Lucius Vasella, Randy Lee Webb
-
Publication number: 20120004310Abstract: Methods and compounds for treating neurological and other disorders are provided. Included is the administering to a subject in need thereof an effective amount of a compound having binding and/or modulation specificity for a TrkB receptor molecule.Type: ApplicationFiled: May 27, 2011Publication date: January 5, 2012Inventors: Frank M. LONGO, Stephen M. Massa, Sandeep Gupta
-
Publication number: 20120004227Abstract: The present invention discloses novel cyclohexane derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), or a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted aryl or heterocyclyl; a combination of X and Y is a combination selected from (X, Y)?(C(?O)N(R1), C(?O)N(R2)), (C(?O)N(R1), imidazole-1,3-diyl), (N(R1), C(?O)N(R2)), (O, C(?O)N(R2)), (C(R3)(R4), N(R2)) or (a single bond, C(?O)N(R2)); R1, R2 and R3 are independently hydrogen or substituted or unsubstituted alkyl; R5 is substituted or unsubstituted aryl or heterocyclyl; R6 is halogen, oxo, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy; m is 0 or 1; and n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or fused bicyclic heterocycle.Type: ApplicationFiled: March 5, 2010Publication date: January 5, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Hiroshi Yoshida, Keisuke Tonogaki, Masahiro Sakagami, Kenji Takaya
-
Patent number: 8088828Abstract: This invention provides a method of treating, preventing, suppressing, inhibiting or reducing the incidence of benign prostate hyperplasia in a male subject, by administering to the subject a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein. This invention also provides a method of treating a subject suffering from hair loss, comprising the step of administering to the subject a therapeutically effective amount of a 5-? reductase enzyme type 1 and/or type 2 inhibitor, wherein said inhibitor is a selective androgen receptor modulator (SARM) and/or its analog, derivative, isomer, metabolite, pharmaceutically acceptable salt, pharmaceutical product, hydrate, N-oxide, or any combination thereof as described herein.Type: GrantFiled: June 30, 2010Date of Patent: January 3, 2012Assignee: University of Tennessee Research FoundationInventors: James T. Dalton, Duane D. Miller, Mitchell S. Steiner, Karen A. Veverka, Wenqing Gao
-
Patent number: 8088763Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I, processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including these compounds and related methods of treating or inhibiting certain diseases or conditions.Type: GrantFiled: November 9, 2006Date of Patent: January 3, 2012Assignee: Gruenenthal GmbHInventors: Corinna Sundermann, Bernd Sundermann
-
Publication number: 20110319454Abstract: The invention provides well defined compounds having FPRL-1 agonist or antagonist activity. As such, the compounds of the invention are useful for treating a variety of ocular disorders.Type: ApplicationFiled: June 24, 2011Publication date: December 29, 2011Applicant: ALLERGAN, INC.Inventors: Richard L. Beard, John E. Donello, Vidyasagar Voligonda, Michael E. Garst
-
Publication number: 20110312964Abstract: Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic painType: ApplicationFiled: December 18, 2009Publication date: December 22, 2011Applicant: Medivir UK LTDInventors: Susana Ayesa, Anna Karin Belfrage, Björn Classon, Urszula Grabowska, Ellen Hewitt, Vladimir Ivanov, Daniel Jönsson, Pia Kahnberg, Peter Lind, Magnus Nilsson, Lourdes Odén, Mikael Pelcman, Horst Wähling
-
Publication number: 20110312875Abstract: The present invention provides a compound of formula I, II, III and IV as defined herein and pharmaceutically acceptable derivatives thereof. The present invention further provides use of the compounds of the present invention in the treatment of bacterial infection and in the treatment of HIV infection. Also provided are pharmaceutical compositions comprising the compounds of the present invention.Type: ApplicationFiled: August 2, 2011Publication date: December 22, 2011Applicant: UNIVERSITY OF WOLLONGONGInventors: Timothy Patrick Boyle, John Barnard Bremner, Zinka Brkic, Jonathan Alan Victor Coates, Neal Kevin Dalton, John Deadman, Paul Anthony Keller, Jody Morgan, Stephen Geoffrey Pyne, David Ian Rhodes, Mark James Robertson
-
Publication number: 20110312997Abstract: Peptidomimetics that inhibit the interaction between MLL1 and WDR5 are disclosed. Methods of inhibiting MLL1 activity and methods of treating cancers also are disclosed.Type: ApplicationFiled: June 14, 2011Publication date: December 22, 2011Inventors: Shaomeng Wang, Hacer Karatas, Yali Dou, Elizabeth Townsend, Denzil Bernard
-
Publication number: 20110306600Abstract: The invention discloses a number of therapeutic compounds and a method of treating a disorder in mammal.Type: ApplicationFiled: June 10, 2011Publication date: December 15, 2011Applicant: Grunenthal GmbHInventor: Ramesh SESHA
-
Publication number: 20110306668Abstract: A process for synthesizing and screening solution phase derived libraries of fenbufen and ethacrynic acid is provided in the present invention. Compounds in the present invention having cytotoxicities are useful for a variety of therapeutic applications.Type: ApplicationFiled: June 9, 2010Publication date: December 15, 2011Applicant: NATIONAL TSING HUA UNIVERSITYInventors: Chung-Shan Yu, Yuan-Hsiao Su, Li-Wu Chiang, Chia-Rong Chen, Shao-Wei Chen, Chia-Wen Huang, Ho-Lien Huang, Yin-Cheng Huang
-
Publication number: 20110301235Abstract: Provided herein are organoselenium compounds and pharmaceutical compositions thereof. Also provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders using the compounds and pharmaceutical compositions provided herein.Type: ApplicationFiled: December 2, 2010Publication date: December 8, 2011Applicant: Alquest Therapeutics, Inc.Inventors: Daniel A. Erlanson, Stig K. Hansen
-
Patent number: 8071575Abstract: Bone targeted compounds and methods are provided. Compounds can include a Bone Targeting Portion (RT), having an affinity for bone; a Bone Active Portion (RA) for interacting with and affecting bone; and a Linking Portion (RL) connecting the Bone Targeting Portion and the Bone Active Portion.Type: GrantFiled: February 22, 2008Date of Patent: December 6, 2011Assignee: University of Louisville Research FoundationInventors: William M. Pierce, Jr., K. Grant Taylor, Leonard C. Waite
-
Patent number: 8071640Abstract: A method for treating a cytotoxic disease by administrating compounds having a general formula X-(A)n-Y, wherein: n varies between 6 and 20; X denotes a hydrogen atom, an RaCO, RaOCO, RaNHCO or RaSO2 group, Ra being an alkyl, alkenyl, alkynyl, aryl, aralkyl, heteroaryl group, the groups being substituted or not, on condition that X is different from H when n is equal to 6; A denotes either a group having formula (I) or (II), wherein Ri is a hydrogen atom, an amino acid side chain, an alkyl, alkenyl, alkynyl, aryl, aralkyl or heteroaryl group, said groups being substituted or not, i being an integer of between 1 and n; Y is an NRbRc, Rb and Rc group having the same meaning as given earlier for Ra.Type: GrantFiled: March 3, 2010Date of Patent: December 6, 2011Assignee: Centre National de la Recherche ScientifiqueInventors: Gilles Francois Roger Guichard, Jean-Paul Briand, Vincent Semetey, Patrick Neuberg