C=x Bonded Directly Or Indirectly By An Acyclic Carbon Or Carbon Chain To Ring Carbon Of The Five-membered Hetero Ring (e.g., Tryptophan, Etc.) (x Is Chalcogen) Patents (Class 514/419)
  • Publication number: 20110269678
    Abstract: A method of improving nutrition and/or treating low grade inflammation in an elderly human subject comprises administering to said subject a cysteine source so as to provide metabolically available cysteine in the diet of said subject in a proportion relative to all available amino acids which is greater that the proportion of cysteine relative to all amino acids which corresponds to the requirements of a healthy young human subject.
    Type: Application
    Filed: July 12, 2011
    Publication date: November 3, 2011
    Applicants: INSTITUT NATIONAL RECHERCHE AGRONOMIQUE, NESTEC S.A.
    Inventors: Denis Breuille, Sabine Mercier, Isabelle Papet, Philippe Patureau Mirand, Christiane Obled
  • Publication number: 20110269786
    Abstract: Administration of sPLA2 inhibitors in combination with statins has been found to reduce the occurrence of major adverse cardiac events (MACEs), specifically unstable angina (UA) requiring urgent hospitalization, in diabetic subjects who have recently experienced an index ACS event to a significantly greater degree than statins alone. These results were unexpected given previous results showing that statins alone are insufficient to satisfactorily reduce MACEs and inflammation in this high-risk population, combined with the high levels of baseline inflammation associated with diabetes. Therefore, provided herein are methods of treating MACEs, including UA requiring urgent hospitalization, in a diabetic subject who has previously experienced an ACS event by administering one or more sPLA2 inhibitors alone or in combination with one or more statins.
    Type: Application
    Filed: April 29, 2011
    Publication date: November 3, 2011
    Inventors: Colin Hislop, Joaquim Trias, Debra Odink, Paul Truex
  • Publication number: 20110263567
    Abstract: The present invention relates to compounds of general formula (i) having an oxime moiety or a pharmaceutically acceptable salt, hydrate or solvate thereof and its use for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1), a pharmaceutical composition comprising the compound or a salt, hydrate or solvate thereof as an active ingredient, a method for the prevention or the treatment of a SSAO/VAP-1 related disease, said diseases including acute or chronic inflammatory diseases, diseases related to carbohydrate metabolism, diabetes-associated complications, diabetic retinopathy and macular oedema, diseases related to adipocyte or smooth muscle dysfunctions, neurodegenerative diseases and vascular diseases.
    Type: Application
    Filed: September 11, 2009
    Publication date: October 27, 2011
    Applicant: Semmelweis Egyetem
    Inventors: Péter Mátyus, Kálmán Magyar, Marjo Pihlavisto, Klára Gyires, Norbert Haider, Yinghua Wang, Patrick Woda, Petra Dunkel, Éva Tóth-Sarudy, Gÿorgy Túrós
  • Publication number: 20110263599
    Abstract: Compounds which inhibit the activity of anti-apoptotic Mcl-1 protein, compositions containing the compounds, and methods of treating diseases involving overexpressed or unregulated Mcl-1 protein are disclosed.
    Type: Application
    Filed: April 15, 2011
    Publication date: October 27, 2011
    Inventors: Xiaohong Song, Hong Ding, Steven W. Elmore, Milan Bruncko, David J. Madar, Andrew J. Souers, Cheol-Min Park, Zhi-Fu Tao, Xilu Wang, Aaron R. Kunzer
  • Publication number: 20110263554
    Abstract: The invention provides methods to identify agents useful to prevent, inhibit or treat viral infections, e.g. filovirus infections, as well as compositions having one or more agents to prevent, inhibit or treat viral infection.
    Type: Application
    Filed: November 6, 2009
    Publication date: October 27, 2011
    Applicant: WARF - Wisconsin Alumni Research Foundation
    Inventors: Yoshihiro Kawaoka, Shinji Watanabe, Yasuko Hatta
  • Publication number: 20110263601
    Abstract: Methods are disclosed for treating ulcerative colitis and related diseases and disorders, which comprise inhibiting tryptophan hydroxylase (TPH) in patients in need thereof.
    Type: Application
    Filed: October 25, 2010
    Publication date: October 27, 2011
    Inventors: Philip Manton Brown, Qingyun Liu, Brian Zambrowicz
  • Publication number: 20110263626
    Abstract: The present invention relates to compounds of general formula I wherein n, R1, R2, R3, R4, R5, R6, R7 and R8 are defined as stated hereinafter, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.
    Type: Application
    Filed: August 28, 2008
    Publication date: October 27, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Norbert Hauel, Angelo Ceci, Enzo Cereda, Henri Doods, Ingo Konetzki, Juergen Mack, Henning Priepke, Annette Schuler-metz, Rainer Walter
  • Publication number: 20110263556
    Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.
    Type: Application
    Filed: October 20, 2010
    Publication date: October 27, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Robert ROENN, Benjamin PELCMAN
  • Patent number: 8044091
    Abstract: 3-phosphoindole compounds for the treatment of retroviral infections, and particularly for HIV, are described. Also included are compositions comprising the 3-phosphoindole derivatives alone or in combination with one or more other anti-retroviral agents, processes for their preparation, and methods of manufacturing a medicament incorporating these compounds.
    Type: Grant
    Filed: November 21, 2008
    Date of Patent: October 25, 2011
    Assignee: Idenix Pharmaceuticals, Inc.
    Inventors: Richard Storer, Cyril Dousson, Francois-Rene Alexandre, Arlene Roland
  • Publication number: 20110257239
    Abstract: The present invention is directed to solid, sustained-release, oral dosage form pharmaceutical compositions which contain therapeutic amounts of a pharmaceutically active agent, hydroxypropyl methyl cellulose and a non-ionic, hydrophilic polymer selected froth the group consisting of hydroxyethyl cellulose having a number average molecular weight ranging from 90,000 to 1,300,000, hydroxypropyl cellulose having a number average molecular weight of 370,000 to 1,500,000, and poly(ethylene oxide) having a number average molecular weight ranging from 100,000 to 500,000.
    Type: Application
    Filed: May 24, 2011
    Publication date: October 20, 2011
    Inventors: Rajen Shah, Arun Parmanand Patel, Roy Thomas Sandry
  • Publication number: 20110257085
    Abstract: Physical crystal structures of a compound of the formula I: are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
    Type: Application
    Filed: April 6, 2011
    Publication date: October 20, 2011
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Jack Z. Gougoutas, Mary F. Malley, John D. DiMarco, Xiaotian S. Yin, Chenkou Wei, Jurong Yu, Truc Chi Vu, Gregory Scott Jones, Scott A. Savage
  • Publication number: 20110251196
    Abstract: The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.
    Type: Application
    Filed: October 5, 2010
    Publication date: October 13, 2011
    Inventors: Carolyn Diane Dzierba, Richard A. Hartz, Yingzhi Bi, Vijay T. Ahuja, Joanne J. Bronson, Kenneth Carson, Giovanni Cianchetta, Michael Green, David Kimball, S. Roy Kimura, Soojin Kwon, John E. Macor, Yulian Zhang, Greg Zipp
  • Publication number: 20110251171
    Abstract: Compounds of the formula provide pharmacological agents which are potent agonists of Peroxisome Proliferator-Activated Receptors (PPARs). Accordingly, the compounds of the instant invention are useful for the treatment of conditions mediated by the PPAR receptor activity in mammals. Such conditions include dyslipidemia, hyperlipidemia, hypercholesteremia, atherosclerosis, hypertriglyceridemia, heart failure, myocardial infarction, vascular diseases, cardiovascular diseases, hypertension, obesity, inflammation, arthritis, cancer, Alzheimer's disease, skin disorders, respiratory diseases, ophthalmic disorders, inflammatory bowel diseases, ulcerative colitis and Crohn's disease. The compounds of the present invention are particularly useful in mammals as hypoglycemic agents for the treatment and prevention of conditions in which impaired glucose tolerance, hyperglycemia and insulin resistance are implicated, such as type-1 and type-2 diabetes, and Syndrome X.
    Type: Application
    Filed: June 22, 2011
    Publication date: October 13, 2011
    Inventors: Andrew Thomas Bach, Prasad Koteswara Kapa, George Tien-San Lee, Eric M. Loeser, Michael Lloyd Sabio, James Lawrence Stanton, Thalaththani Ralalage Vedananda
  • Publication number: 20110245188
    Abstract: The present invention relates to methods and compositions of treating or preventing inflammatory diseases or conditions in a patient comprising administering to the patient a therapeutically effective amount of a composition comprising a glutathione donor, 5-amino 4-imidazolecarboxamide ribotide (AICAR), a 3-hydroxy-3-methylgluatryl-coenzymeA (HMG-CoA) reductase inhibitor, D-threo-1-Phenyl-2-decanoylamino-3-morpholino-1-propanol HCl (D-PDMP), and/or 1,5-(butylimino)-1,5-dideoxy-D-glucitol (Miglustat), or derivatives thereof.
    Type: Application
    Filed: March 25, 2011
    Publication date: October 6, 2011
    Applicant: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventor: Inderjit Singh
  • Publication number: 20110245158
    Abstract: The present disclosure relates to high protein dietary supplements for treating various symptoms and diseases associated with protein deficiency including weight gain, obesity, catabolic diseases, fibromyalgia, anxiety reactions, posttraumatic stress and chronic fatigue syndrome. Embodiments of dietary supplements comprise combinations of proteins, essential and semi-essential amino acids including L-Lysine, L-Arginine, and/or L-Histidine.
    Type: Application
    Filed: June 20, 2011
    Publication date: October 6, 2011
    Inventor: George Scheele
  • Publication number: 20110245283
    Abstract: The invention provides methods for optimizing therapeutic efficacy for treating hypercholesterolemia in a subject having a cardiovascular disease (CVD), comprising (a) determining subject characteristics that affect the likelihood of reaching a goal level of low density lipoprotein (LDL); and (b) obtaining success probabilities of a variety of statin treatments for reaching said goal level of LDL using said subject characteristics and a multivariate model; and (c) administrating the optimal statin treatment with the highest success probability of step (b) to said subject thereby optimizing therapeutic efficacy for treating hypercholesterolemia in said subject.
    Type: Application
    Filed: December 21, 2010
    Publication date: October 6, 2011
    Inventor: Glen H. Murata
  • Publication number: 20110245316
    Abstract: The present invention provides a method for preventing or delaying the onset of oral mucositis, including the onset of ulcerative or severe OM, in a patient receiving cancer therapy. The method comprises administering to the patient an effective regimen of ?-D-glutamyl-L-tryptophan (SCV-07) over the course of therapy. The regimen, which includes scheduled doses of SCV-07 with respect to radiation exposure and/or chemotherapy, is effective for preventing or delaying the onset of OM. In accordance with the invention, the patient is more able to complete the planned course of cancer therapy (including chemotherapy and/or radiation therapy), by maintaining a sufficient nutritional state, and by avoiding the significant pain and discomfort associated with OM.
    Type: Application
    Filed: March 29, 2011
    Publication date: October 6, 2011
    Applicant: SCICLONE PHARMACEUTICALS, INC.
    Inventor: Israel RIOS
  • Publication number: 20110244045
    Abstract: The present invention provides a controlled-release composition which provides a therapeutically effective plasma concentration of N-acetylcysteine over prolonged period of time. The present invention also includes the use of the controlled-release composition, either alone or in combination with at least one additional active agent, for reduction of vascular inflammation marker and treatment of diseases, conditions, and/or symptoms associated with systemic and/or vascular inflammation in a patient. Furthermore, the present invention provides a process of making granules comprising N-acetylcysteine, or a salt, solvate, prodrug, and/or analog thereof.
    Type: Application
    Filed: May 11, 2009
    Publication date: October 6, 2011
    Applicant: TIARA PHARMACEUTICALS ,INC.
    Inventors: Yadon Arad, Liang C. Dong
  • Publication number: 20110245313
    Abstract: The present invention relates to compositions suitable for the treatment of pathological conditions distinguished by insufficient or reduced mitochondrial function. The compositions comprise, as principal active ingredients, the amino acids leucine, isoleucine and valine. The compositions may also comprise, as further active ingredients, amino acids threonine and lysine, and optionally, histidine, phenylalanine, methionine, tryptophan, as well as tyrosine and cysteine.
    Type: Application
    Filed: June 15, 2011
    Publication date: October 6, 2011
    Applicant: PROFESSIONAL DIETETICS S.r.I.
    Inventor: Francesco Saverio DIOGUARDI
  • Publication number: 20110245312
    Abstract: The present invention relates to compositions suitable for the treatment of pathological conditions distinguished by insufficient or reduced mitochondrial function. The compositions comprise, as principal active ingredients, the amino acids leucine, isoleucine and valine. The compositions may also comprise, as further active ingredients, amino acids threonine and lysine, and optionally, histidine, phenylalanine, methionine, tryptophan, as well as tyrosine and cysteine.
    Type: Application
    Filed: June 15, 2011
    Publication date: October 6, 2011
    Applicant: PROFESSIONAL DIETETICS S.r.I.
    Inventor: Francesco Saverio DIOGUARDI
  • Publication number: 20110236395
    Abstract: Inhibitors of matrix metalloproteinase 2 are used to treat or prevent a fibrotic disorder of the posterior capsule of the eye, for example posterior capsule opacification (PCO), or of a tissue or structure of the eye other than the lens or capsular bag.
    Type: Application
    Filed: September 9, 2009
    Publication date: September 29, 2011
    Applicant: UNIVERSITY OF EAST ANGLIA
    Inventors: Ian Michael Wormstone, Lucy Dawes, Julie Ann Eldred, Dylan Edwards, Lisa Hodgkinson
  • Publication number: 20110237595
    Abstract: The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ischaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula (I): wherein A, n, R1, R7 and R8 are as defined herein.
    Type: Application
    Filed: June 9, 2011
    Publication date: September 29, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Ahmed ABOUABDELLAH, Regine BARTSCH-LI, Christian HOORNAERT, Antoine RAVET
  • Publication number: 20110237525
    Abstract: A method of supplementing a diet and ameliorating oxidative stress in a mammal includes administering a pharmaceutically effective amount of lipid soluble, hydrophobic active compounds having a chemical structure: wherein R1 is an aromatic backbone and R2 is a sulfur containing ligand. Through formation of disulfide linkages other moieties can be attached to R2 converting the hydrophobic base into a water soluble entity, for ease of delivery, which can be reconverted back to the original compound by biochemical reduction in the blood stream.
    Type: Application
    Filed: June 18, 2010
    Publication date: September 29, 2011
    Inventors: Boyd E. Haley, Niladri Narayan Gupta
  • Publication number: 20110236453
    Abstract: The present invention relates to a peptide or peptidomimetic for use in the treatment of a biofilm-associated infection in a subject, wherein said peptide or peptidomimetic a) carries a net positive charge, b) is 1 to 6 amino acids in length or is an equivalently sized peptidomimetic; and c) is amphipathic in nature, having one or more lipophilic groups, one of said lipophilic groups comprising at least 7 non-hydrogen atoms.
    Type: Application
    Filed: October 2, 2009
    Publication date: September 29, 2011
    Applicant: LYTIX BIOPHARMA AS
    Inventors: Wenche Stensen, Frederick Alan Leeson, Stig Olov Magnus Engqvist, Trond Flægstad, Øystein Rekdal, John Sigurd Svendsen
  • Patent number: 8026271
    Abstract: This invention relates to an oral formulation containing an effective amount of the compound of the following formula I: d-alpha-tocopheryl polyethylene glycol 1000 succinate (“TPGS”); and 2-(2-ethoxyethoxy)ethanol (“Transcutol”). R1 through R4 and n are defined herein. Also disclosed is a method of treating cancer by administering this formula to a subject orally.
    Type: Grant
    Filed: July 11, 2008
    Date of Patent: September 27, 2011
    Assignee: National Health Research Institutes
    Inventors: Teng-Kuang Yeh, Chiung-Tong Chen, Yu-Sheng Chao
  • Publication number: 20110230452
    Abstract: The present invention relates generally to pharmaceutical agents, and in particular, to metalloprotease inhibitor compounds. More particularly, the present invention provides a new class of dual acting MMP-2 and MMP-9 inhibiting compounds that exhibit increased potency, metabolic stability and/or reduced toxicity in relation to currently known MMP-2 and MMP-9 inhibitors for the treatment of pain and other diseases. Additionally, the present invention relates to methods for treating pain, addiction and/or withdrawal symptoms in a patient comprising administering to the patient a pain-reducing effective amount of a present compound.
    Type: Application
    Filed: September 23, 2010
    Publication date: September 22, 2011
    Inventor: Irving Sucholeiki
  • Publication number: 20110230524
    Abstract: The present invention relates to novel substituted 2-(5-hydroxy-2-methyl-1H-indol-3-yl)acetic acids, to novel antiviral active ingredients, pharmaceutical compositions, antiviral medicaments, methods for prophylaxis and treatment of viral diseases particularly caused by influenza viruses and infectious hepatisis C (HCV) viruses.
    Type: Application
    Filed: November 27, 2009
    Publication date: September 22, 2011
    Inventors: Andrey Alexandrovich Ivashchenko, Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko, Pavel Mikhailovich Yamanushkin, Oleg Dmitrievich Mitkin, Vladimir Yurievich Vvedensky, Vadim Vasilievich Bichko
  • Publication number: 20110229464
    Abstract: Pharmaceutical compositions and methods for treating and/or preventing age-related macular degeneration with melatonin analogues are provided.
    Type: Application
    Filed: June 17, 2009
    Publication date: September 22, 2011
    Inventors: David Baron, Keisuke Hirai, Yasushi Shintani, Osamu Uchikawa
  • Patent number: 8021681
    Abstract: The present invention is directed to a method of treating a patient suffering from the metabolic syndrome and/or related disorders including obesity, Type 2 diabetes, pre-diabetes, hypertension, dyslipidemia, insulin resistance, endothelial dysfunction, pro-inflammatory state, and pro-coagulative state, and having the steps of (a) providing to the patient a dietary regimen that decreases overactive CNS noradrenergic tone; followed by (b) providing to the patient a dietary regimen that increases dopaminergic tone while maintaining the above decreased overactive CNS noradrenergic tone. The present invention is also directed to prepackaged meals and recipes useful in implementing the dietary regimens.
    Type: Grant
    Filed: September 17, 2004
    Date of Patent: September 20, 2011
    Inventor: Anthony Cincotta
  • Publication number: 20110224184
    Abstract: The present invention provides pharmaceutical compositions comprising substituted 1,4 naphthoquinones that are effective in preventing oligomerization of beta amyloid and subsequent pathologies associated with amyloid fibrils. These compositions are useful for the treatment of disease involving amyloidogenesis including neurodegenerative diseases such as Alzheimer's Disease or senile dementia. Particularly effective compositions comprise 1,4 naphthoquinones substituted with an amino acid residue selected from a heterocyclic or aromatic amino acid.
    Type: Application
    Filed: September 6, 2009
    Publication date: September 15, 2011
    Applicant: RAMOT AT TEL AVIV UNIVERSITY LTD.
    Inventors: Roni Scherzer, Ehud Gazit, Daniel Segal
  • Publication number: 20110224213
    Abstract: The invention relates to the use of glutaric acid derivatives of general formula (I), which are disclosed in the invention description, as anti-arrhythmic agents.
    Type: Application
    Filed: March 18, 2009
    Publication date: September 15, 2011
    Inventors: Vladimir Evgenievich Nebolsin, Dmitry Sergeevich Blinov, Vladimir Pavlovich Balashov, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina
  • Patent number: 8017645
    Abstract: The present invention relates to a disposable container for a medicament or cosmetic agent for topical application, containing a single dose of melatonin or of a melatonin derivative which corresponds to a locally effective dose but which does not cause any systemic effect.
    Type: Grant
    Filed: May 7, 2008
    Date of Patent: September 13, 2011
    Assignee: ASAT AG Applied Science & Technology
    Inventor: Hans W. Schmid
  • Patent number: 8017159
    Abstract: The present invention relates to pharmaceutical compositions in the form of a gel for controlled- or sustained-release of an aptamer and to methods for treating or preventing a condition in an animal by administering to an animal in need thereof the pharmaceutical compositions.
    Type: Grant
    Filed: April 10, 2006
    Date of Patent: September 13, 2011
    Assignee: IDEXX Laboratories, Inc.
    Inventor: Yerramilli V. S. N. Murthy
  • Publication number: 20110218227
    Abstract: New (2R,4R) monatin monosodium salt hydrate crystals characterized by having specific characteristic X-ray diffraction peaks provide general-purpose, stable, and safe monatin sodium salt crystals incorporating no organic solvent. These crystal may be prepared by a method that requires no organic solvent in the crystallization, separation, and drying steps. These crystal are useful as sweeteners and for the preparation of orally consumed products, such as foods, beverages, pharmaceutical products, topical pharmaceutical products, and feeds containing general-purpose, stable, and safe monatin sodium salt crystals.
    Type: Application
    Filed: May 10, 2011
    Publication date: September 8, 2011
    Applicant: AJINOMOTO CO., INC
    Inventors: Kenichi MORI, Eriko ONO
  • Publication number: 20110213012
    Abstract: The present invention is directed, inter alia, to methods of treating NUT midline carcinoma (NMC) by administering compounds that promote increased histone acetylation. The invention also includes assay methods for determining the responsiveness of NMC to specific histone deacetylases and other compounds.
    Type: Application
    Filed: July 21, 2009
    Publication date: September 1, 2011
    Applicants: THE BRIGHAM AND WOMEN'S HOSPITAL, INC., DANA-FARBER CANCER INSTITUTE
    Inventors: Christopher French, Jon Aster, Matthias Hofer, James Bradner
  • Publication number: 20110212992
    Abstract: The present application is directed to novel P2X7R antagonists that are N-indol-3-yl-acetamide and N-azaindol-3-yl-acetamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.
    Type: Application
    Filed: February 25, 2011
    Publication date: September 1, 2011
    Applicant: AFFECTIS PHARMACEUTICALS AG
    Inventor: Michael BOES
  • Publication number: 20110212969
    Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.
    Type: Application
    Filed: February 25, 2011
    Publication date: September 1, 2011
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Christopher Blackburn, Kenneth M. Gigstad, Sean J. Harrison, He Xu
  • Patent number: 8008295
    Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating signal transduction of both receptor-type and non-receptor type tyrosine kinases. The compounds of the instant invention possess a core structure that comprises an indole-sulfonamide moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Grant
    Filed: October 26, 2009
    Date of Patent: August 30, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher J. Dinsmore, Douglas C. Beshore, Jeffrey M. Bergman, Craig W. Lindsley
  • Publication number: 20110207783
    Abstract: The present invention relates to acyclic amino amide renin inhibitor compounds and their use in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: August 4, 2008
    Publication date: August 25, 2011
    Inventors: Daniel Dube, Austin Chen, Daniel J. McKay
  • Publication number: 20110207710
    Abstract: Administration of sPLA2 inhibitors has been found to decrease cholesterol levels, atherosclerotic plaque formation and aortic aneurysm in mice, and to decrease cholesterol and triglyceride levels in humans. Interestingly, administration of sPLA2 inhibitors was found to decrease cholesterol levels even when the inhibitors were administered only once per day. Therefore, provided herein are methods of treating dyslipidemia, CVD, and conditions associated with CVD such as atherosclerosis and metabolic syndrome, by administering one or more sPLA2 inhibitors. Significantly, administration of sPLA2 inhibitors and various compounds used in the treatment of CVD, such as for example statins, resulted in greater decreases in LDL and LDL particle levels in a synergistic manner. In addition, administration of sPLA2 inhibitors and statins resulted in a synergistic decrease in plaque content.
    Type: Application
    Filed: March 17, 2011
    Publication date: August 25, 2011
    Inventors: Joaquim TRIAS, Colin Hislop, Paul Truex, Bernadine Fraser, Debra Odink, Scott Chadwick
  • Publication number: 20110207726
    Abstract: The present invention is directed to novel protease inhibitors that are specific for cathepsin L, cathepsin B, and cathepsin S. Accordingly, the present invention encompasses compositions and methods for treating and preventing diseases and disorders associated with cathepsin L, cathepsin B, or cathepsin S function or activity.
    Type: Application
    Filed: April 17, 2009
    Publication date: August 25, 2011
    Inventors: Scott L. Diamond, Mary Pat Beavers, Donna Huryn, Michael C. Myers, Amos B. Smith, Parag P. Shah, Zhuqing Liu
  • Patent number: 8003682
    Abstract: Compounds of formula (I): wherein: R1 represents an alkyl, cycloalkyl or cycloalkylalkyl group, R2 represents a linear or branched (C1-C6)alkyl group, and n represents from 1 to 6. Medicaments.
    Type: Grant
    Filed: October 17, 2007
    Date of Patent: August 23, 2011
    Assignee: Les Laboratories Servier
    Inventors: Pascal Marchand, Vincent Babonneau, Sylvie Piessard, Muriel Duflos, Jean Albert Boutin, Valérie Audinot, Philippe Delagrange, Daniel-Henri Caignard
  • Patent number: 7998698
    Abstract: Provided is a method for determining whether an individual is likely to be susceptible to radiation pneumonitis from radiation therapy and for developing a treatment based on the determination of susceptibility. The method involves measuring SOD and GPX activity levels. A high SOD or low GPX activity, or a combination thereof, is indicative that the individual is likely to be susceptible to radiation pneumonitis.
    Type: Grant
    Filed: May 31, 2007
    Date of Patent: August 16, 2011
    Assignee: Health Research Inc.
    Inventors: Young-Mee Park, Gary Y. Yang, Nithya Ramnath
  • Publication number: 20110196013
    Abstract: The present invention relates to an animal feed composition that comprises free indole acetic acid (free IAA) or a derivative thereof. The invention also relates to a method for enhancing animal growth by feeding the animal with a composition according to the invention. The invention also relates to the use of free IAA or a derivative thereof in a method of therapy of animals in need of a growth-promoting treatment, such as immunocompromised animals, animals with a growth deficit or slow growing animals. The invention also relates to the use of free IAA or a derivative thereof for the preparation of a therapeutical composition for increasing the growth rate and/or the feed conversion rate and/or the immunity of animals in need of such a treatment, in particular immunocompromised or slow growing animals. A composition according to the invention may preferably be in the form of a food or feed supplement.
    Type: Application
    Filed: April 19, 2011
    Publication date: August 11, 2011
    Inventors: Hubert Jean Marie Francois Gillessen, Christian Rebiere
  • Publication number: 20110195962
    Abstract: Compositions and methods for treating nasal disorders associated with nasal inflammation using a multipharmacophoric agent (MPA) that can prevent the production and/or release of at least one or more pro-inflammatory cytokines (for instance IL-1 and TNF?) and inhibit p38 MAP kinase or at least one matrix metalloproteinases (MMP-1 and MMP-9) are disclosed.
    Type: Application
    Filed: April 18, 2011
    Publication date: August 11, 2011
    Applicant: ALCON RESEARCH, LTD.
    Inventors: Najam A. Sharif, Martin B. Wax
  • Publication number: 20110195967
    Abstract: Selected 2-arylacetic acids, their derivatives and pharmaceutical compositions that contain these compounds are useful in inhibiting 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 their activation. In particular, 2(ortho)-substituted arylacetic acids or their derivatives, such as amides and sulfonamides, lack 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: Application
    Filed: April 22, 2011
    Publication date: August 11, 2011
    Applicant: DOMPE PHA.R.MA S.P.A.
    Inventors: Alessio MORICONI, Marcello ALLEGRETTI, Maria Candida CESTA, Riccardo BERTINI, Cinzia BIZZARRI, Francesco COLOTTA
  • Patent number: 7993666
    Abstract: Methods and compositions are provided for reducing, treating or preventing pain and/or inflammation in a patient in need of such treatment, the methods and compositions comprising administering a therapeutically effective amount of a statin or pharmaceutically acceptable salt thereof to a target tissue site beneath the skin.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: August 9, 2011
    Assignee: Warsaw Orthopedic, Inc.
    Inventors: William McKay, John Zanella
  • Publication number: 20110190294
    Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification.
    Type: Application
    Filed: April 16, 2009
    Publication date: August 4, 2011
    Inventors: Patrik Rhönnstad, Elisabet Kallin, Theresa Apelqvist, Mattias Wennerstål, Aiping Cheng
  • Publication number: 20110189305
    Abstract: An immunomodulatory compound is administered to treat, prevent, inhibit, or reduce lung cancer in a subject.
    Type: Application
    Filed: August 21, 2008
    Publication date: August 4, 2011
    Inventor: Cynthia W. Tuthill
  • Patent number: 7989487
    Abstract: A method for preventing, diagnosing, or treating a condition mediated by an estrogen receptor by administering to a patient in need thereof an effective amount of a compound of formula I, II, or a combination thereof: wherein R1, R3, R4, and R5 are independently selected from H, OH, and ORa; R2 is selected from H, OH, and (C?O)(C1-7)alkyl; Ra is (C1-7)alkyl or (C?O)(C1-7)alkyl; or a derivative of the compound selected from N-oxide derivatives, prodrug derivatives, protected derivatives, isomers, and mixtures of isomers of the compound; or a pharmaceutically acceptable salt or solvate of the compound or the derivative. Compounds of formula I and II and pharmaceuticals compositions thereof are also presented.
    Type: Grant
    Filed: July 6, 2007
    Date of Patent: August 2, 2011
    Assignee: University of Medicine and Dentistry of New Jersey
    Inventors: William J. Welsh, Nina Ching Y. Wang, Ni Ai