C=x Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding (x Is Chalcogen) Patents (Class 514/423)
  • THERAPEUTIC USES OF AMPA RECEPTOR MODULATORS FOR TREATMENT OF MOTOR DYSFUNCTION
    Publication number: 20110218190
    Abstract: The application describes treatment of motoneuronal dysfunctions or disorders using AMPA receptor modulators. Examples of a motoneuronal dysfunction or disorder include obstructive sleep apnea, snoring, multiple sclerosis, spinal cord injury, e.g., crush, partial or complete transection, motor neuron diseases, motor weakness due to aging, stroke, tumor, hemorrhage, degenerative or wasting diseases, and spasticity. One example of an AMPA receptor modulator is a benzothiadiazide compound. Another example of an AMPA receptor modulator is an ampakine. Yet another example of an AMPA receptor modulator is aniracetam.
    Type: Application
    Filed: November 9, 2009
    Publication date: September 8, 2011
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Walter E. Babiec, Shane A. Saywell, Jack L. Feldman, Wiktor A. Janczewski
  • CRYSTALLINE SODIUM ATORVASTATIN
    Publication number: 20110218228
    Abstract: Crystalline sodium atorvastatin, compositions containing the same and methods for the production thereof.
    Type: Application
    Filed: May 20, 2011
    Publication date: September 8, 2011
    Applicant: ARROW INTERNATIONAL LIMITED
    Inventors: Kailan Zhou, Hong Liu, Zhirong Chen, Huabin Hong, Yang Sun, Yunde Wang, Jiangchun Pan
  • Uses of morelloflavone
    Publication number: 20110217293
    Abstract: Provided herein are methods of treating postangiplasty, in-stent restenosis or atherosclerosis in an individual in need of such treatment, comprising the step of administering to said individual an effective dose of morelloflavone with or with a effective dose of one or more of an HMG-CoA reductase inhibitor or a hypolipidemic agent or lipid-lowering agent or other lipid agent or lipid modulating agent or anti-atherosclerotic agent. Also provided are pharmaceutical compositions comprising a morelloflavone or pharmaceutical combinations comprising a morelloflavone and one of an HMG-CoA reductase inhibitor or a hypolipidemic agent or lipid-lowering agent or other lipid agent or lipid modulating agent or anti-atherosclerotic agent.
    Type: Application
    Filed: January 28, 2011
    Publication date: September 8, 2011
    Inventors: Kenichi Fujise, Nongporn Towatana, Wilawan Mahabusarakam
  • PHARMACEUTICALLY ACCEPTABLE SALTS OF NOVEL BETULINIC ACID DERIVATIVES
    Publication number: 20110218204
    Abstract: The present invention relates to certain novel salts of Betulinic acid derivatives, to process for preparing such compounds, to use the compounds in treating diseases or disorders mediated by HIV infection, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: January 10, 2011
    Publication date: September 8, 2011
    Applicant: HETERO RESEARCH FOUNDATION, HETERO DRUGS LIMITED
    Inventors: Bandi PARTHASARADHI REDDY, Vedula MANOHAR SHARMA, Kura RATHNAKAR REDDY, Musku MADHANMOHAN REDDY
  • SUBSTITUTED HYDROXAMIC ACIDS AND USES THEREOF
    Publication number: 20110213003
    Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, 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, He Xu
  • AGENT FOR TREATMENT OF DIABETES
    Publication number: 20110212892
    Abstract: The present invention provides a hypoglycemic agent useful for treating diabetes or other similar diseases which has no adverse effects. Furthermore, the present invention provides a hypoglycemic agent comprising a combination of an antidiabetic drug and 2-methyl-2-[(4-{(1E)-3-[2-(4-methylbenzoyl)-1H-pyrrol-1-yl]prop-1-en-1-yl}benzyl)oxy]propanoic acid or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: October 26, 2009
    Publication date: September 1, 2011
    Applicant: Dainippon Sumitomo Pharma Co., Ltd.
    Inventor: Jun Nagamine
  • NOVEL MICROBIOCIDES
    Publication number: 20110207781
    Abstract: Compounds of Formula (I), in which the substituents are as defined in claim 1, are suitable for use as microbiocides.
    Type: Application
    Filed: June 9, 2009
    Publication date: August 25, 2011
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Daniel Stierli, Harald Walter, Sebastian Wendeborn, Antoine Daina
  • DPP-IV INHIBITOR COMBINED WITH A FURTHER ANTIDIABETIC AGENT, TABLETS COMPRISING SUCH FORMULATIONS, THEIR USE AND PROCESS FOR THEIR PREPARATION
    Publication number: 20110206766
    Abstract: The present invention relates to pharmaceutical compositions comprising fixed dose combinations of a DPP-4 inhibitor drug and a partner drug, processes for the preparation thereof, and their use to treat certain diseases.
    Type: Application
    Filed: April 2, 2009
    Publication date: August 25, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Thomas Friedl, Michael Braun, Kenji Egusa, Hikaru Fujita, Megumi Maruyama, Takaaki Nishioka
  • Inhibitors of Human Cathepsin L, Cathepsin B, and Cathepsin S
    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
  • METHODS FOR THE DIAGNOSIS AND TREATMENT OF BONE DISORDERS
    Publication number: 20110209227
    Abstract: This invention pertains to chemometric methods for the analysis of chemical, biochemical, and biological data, for example, spectral data, for example, nuclear magnetic resonance (NMR) spectra, and their applications, including, e.g., classification, diagnosis, prognosis, etc., especially in the context of bone disorders, e.g., conditions associated with low bone mineral density, e.g., osteoporosis.
    Type: Application
    Filed: February 4, 2011
    Publication date: August 25, 2011
    Inventors: Jeremy Kirk Nicholson, Elaine Holmes, John Christopher Lindon, Joanne Tracey Brindle, David John Grainger
  • N-(L-ALKYL-2-PHENYLETHYL)-CARBOXAMIDE DERIVATIVES AND USE THEREOF AS FUNGICIDES
    Publication number: 20110207771
    Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Application
    Filed: June 6, 2007
    Publication date: August 25, 2011
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Daniel Stierli, John J. Taylor, Harald Walter, Paul Anthony Worthington, Ramya Rajan
  • TARGETING PAX2 FOR THE TREATMENT OF BREAST CANCER
    Publication number: 20110206666
    Abstract: The present application provides methods of prevention and/or treatment of breast cancer in a subject by inhibiting expression of PAX2. In the cancer treatment methods disclosed, the method of inhibiting expression of PAX2 can be by administration of a nucleic acid encoding an siRNA for PAX2. A method of treating cancer in a subject by administering DEFB1 is also provided. Similarly, provided is a method of treating cancer in a subject by increasing expression of DEFB1 in the subject.
    Type: Application
    Filed: March 25, 2011
    Publication date: August 25, 2011
    Applicant: PHIGENIX, INC.
    Inventor: Carlton D. DONALD
  • Acetylated amino acids as anti-platelet agents, nutritional and vitamin supplements
    Patent number: 8003683
    Abstract: This invention relates to pharmaceutical compounds and nutritional supplements that are acetylated derivatives of naturally occurring amino acids and acetylated derivatives of peptides derived from naturally occurring amino acids containing hydroxyl groups. They are as useful as anti-platelet drugs, and as nutritional supplements.
    Type: Grant
    Filed: November 13, 2006
    Date of Patent: August 23, 2011
    Assignee: Signature R&D Holdings, LLC
    Inventor: V. Ravi Chandran
  • Methods and Compositions for Treatment of Prostate Intraepithelial Neoplasia
    Publication number: 20110201664
    Abstract: Provided herein are methods of treatment of prostate intraepithelial neoplasia (PIN) by administering bexarotene. Also provided are pharmaceutical compositions and dosing regimens.
    Type: Application
    Filed: October 14, 2006
    Publication date: August 18, 2011
    Inventors: Jack I. Zweig, Elizabeth Zweig
  • NITRIC OXIDE RELEASING AMINO ACID ESTER COMPOUND, COMPOSITION AND METHOD OF USE
    Publication number: 20110195935
    Abstract: There is provided amino acid ester compounds comprising at least one nitric oxide releasing group, pharmaceutically acceptable salts thereof and compositions thereof. These compounds involve an amino acid side-chain or an amino acid derivative thereof and a nitric oxide releasing group as depicted in the following structures: wherein R1 is either an ethyl or an amino acid side-chain group or an amino acid derivative thereof and R2 is an amino acid side-chain group or an amino acid derivative thereof and n is an integer from 1 to 10.
    Type: Application
    Filed: September 24, 2009
    Publication date: August 11, 2011
    Inventor: Michael Farber
  • 2-ARYL-ACETIC ACIDS, THEIR DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
    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
  • COMPOUNDS FOR THE TREATMENT OF FLAVIVIRAL INFECTIONS
    Publication number: 20110195929
    Abstract: Described are various compounds and methods for the treatment of flaviviral infections. In particular, alkaloids and imino sugars in arabinose and/or lyxose stereochemical configuration with antiflaviviral activity are described.
    Type: Application
    Filed: August 4, 2009
    Publication date: August 11, 2011
    Applicant: SUMMIT CORPORATION PLC
    Inventors: Olivier De Moor, Graeme Horne, Penny Jane Middleton, Frank Schroer, Stephen Paul Wren, Maria Ines Passos Eleuterio, Renate Van Well, Colin Richard Dorgan, Francis Xavier Wilson, Robert Nash, Richard Storer, Graham Michael Wynne, Alan Geoffrey Roach, Akane Kawamura, Jonathon Mark Tinsley
  • Methods and compositions for treating pain comprising a statin
    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
  • ARYL BENZYLAMINE COMPOUNDS
    Publication number: 20110190258
    Abstract: The present invention relates to substituted aryl-benzylamine compounds, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Application
    Filed: January 28, 2011
    Publication date: August 4, 2011
    Applicant: NOVARTIS AG
    Inventors: Daniela ANGST, Birgit BOLLBUCK, Philipp JANSER, Jean QUANCARD, Nikolaus Johannes STIEFL
  • Substituted Pyrrole Derivatives and Their Use as HMG-CO Inhibitors
    Publication number: 20110190369
    Abstract: The present invention relates to substituted pyrrole derivatives, which can be used as 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors. Compounds disclosed herein can function as cholesterol lowering agents and can be used for the treatment of cholesterol-related diseases and related symptoms. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and methods of treating cholesterol-related diseases and related symptoms.
    Type: Application
    Filed: April 11, 2011
    Publication date: August 4, 2011
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Mohammad SALMAN, Jitendra SATTIGERI, Yatendra KUMAR, Ram Chander ARYAN, Vikram Krishna RAMANATHAN, Anita CHUGH
  • Substituted Pyrrole Derivatives and Their Use as HMG-CO Inhibitors
    Publication number: 20110190296
    Abstract: The present invention relates to substituted pyrrole derivatives, which can be used as 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitors. Compounds disclosed herein can function as cholesterol lowering agents and can be used for the treatment of cholesterol-related diseases and related symptoms. Processes for the preparation of disclosed compounds are provided, as well as pharmaceutical compositions containing the disclosed compounds, and methods of treating cholesterol-related diseases and related symptoms.
    Type: Application
    Filed: April 11, 2011
    Publication date: August 4, 2011
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Mohammad SALMAN, Jitendra SATTIGERI, Yatendra KUMAR, Ram Chander ARYAN, Vikram Krishna RAMANATHAN, Anita CHUGH
  • GASTRORETENTIVE PHARMACEUTICAL DOSAGE FORM
    Publication number: 20110182988
    Abstract: This invention relates to an orally administrable, gastroretentive pharmaceutical dosage form which contains at least one pharmaceutically active ingredient and at least one polymeric adjuvant. The adjuvant serves to retain the dosage form in a selected region of the gastrointestinal tract for sufficient time for the pharmaceutically active ingredient to be released and absorbed. Ideally the dosage form will contain two or more pharmaceutically active ingredients which are delivered to different regions of the gastrointestinal tract.
    Type: Application
    Filed: June 3, 2009
    Publication date: July 28, 2011
    Inventors: Viness Pillay, Yahya Choonara, Caragh Murphy, Sarashnee Moonisami
  • Agents and methods for denervation
    Publication number: 20110182912
    Abstract: Various agents are described to denerve, modulate, or otherwise affect the renal nerves and other neural tissue. Also, various delivery devices are described to deliver an agent locally to the renal nerves. The delivery devices are positioned in the renal artery and penetrate into the wall of the renal artery to deliver the agent to the renal nerves. The delivery devices may be used to deliver the agent according to longitudinal position, radial position, and depth of the renal nerves relative to the renal artery. In addition, various methods are described to denervate, modulate, or otherwise affect the renal nerves and other neural tissue.
    Type: Application
    Filed: January 26, 2011
    Publication date: July 28, 2011
    Inventors: Michael A. EVANS, Kondapavulur T. VENKATESWARA-RAO, Emily A. STEIN
  • Dipeptidyl peptidase IV inhibitors and processes for their preparation and pharmaceutical compositions containing them
    Patent number: 7985759
    Abstract: The present invention relates to novel compounds representated by formula (I), where R, R1, R2, R3, X, Y, m, n are as defined. The present invention relates to compounds of the general formula I their derivatives, their analogs, their tautomeric forms, their stereoisomers, their diastereomers, their bioisosteres, their polymorphs, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them which are predominantly dipeptidyl peptidase IV inhibitors. The present invention also relates to the processes for the preparation of novel compounds of formula (I) and their use in treating type II diabetes and diabetic complications thereof and also for treating dislipidemia, hypercholesterolemia, obesity and hyperglycemia.
    Type: Grant
    Filed: March 30, 2007
    Date of Patent: July 26, 2011
    Assignee: Matrix Laboratories Ltd.
    Inventors: Gopalan Balasubramanian, Ravi Dhamjewar, Rasheed Mohammed, Sreedhara Swamy Keshavapura Hosamane, Ishtiyaque Ahmad
  • INHIBITORS OF PROTEIN PRENYLTRANSFERASES
    Publication number: 20110178138
    Abstract: The present invention is directed to novel compounds. These compounds can be useful in inhibiting the activity of protein prenyltransferases including GGTase I and/or RabGGTase. The compounds can also be used as anti-cancer therapeutics including as part of methods for treating cancer, in assays, and in kits.
    Type: Application
    Filed: July 28, 2008
    Publication date: July 21, 2011
    Applicant: The Regents of the University of California
    Inventors: Ohyun Kwon, Fuyuhiko Tamanoi, Hanna Fiji, Masaru Watanabe
  • DUAL-ACTING THIOPHENE, PYRROLE, THIAZOLE AND FURAN ANTIHYPERTENSIVE AGENTS
    Publication number: 20110178101
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: January 18, 2011
    Publication date: July 21, 2011
    Inventors: Paul R. Fatheree, Robert Murray McKinnell
  • LONG-TERM TREATMENT OF SYMPTOMATIC HEART FAILURE
    Publication number: 20110178111
    Abstract: The main object here is the use of omega-3 polyunsaturated fatty acids (as ethyl esters, hereinafter called “n-3 PUFA”) as a medicament, either alone or in combination with other therapeutic agents, for reducing mortality for a cardiovascular cause, in particular arrhythmia or for reducing hospitalization for any cause, in particular a cardiovascular cause and for the daily administration to patients with symptomatic heart failure (HF) for more than 3.5 years.
    Type: Application
    Filed: July 23, 2009
    Publication date: July 21, 2011
    Applicants: SPA SOCIETA' PRODOTTI ANTIBIOTICI S.P.A, SIXTERPHARMA S.R.L.
    Inventors: Claudio Cavazza, Maria Giovanna Caccia
  • Anti-infective compounds
    Publication number: 20110178077
    Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.
    Type: Application
    Filed: June 17, 2009
    Publication date: July 21, 2011
    Inventors: Priscille Brodin, Thierry Christophe, Zaesung No, Jaeseung Kim, Auguste Genovesio, Denis Philippe Cedric Fenistein, Heekyoung Jeon, Fanny Anne Ewann, Sunhee Kang, Saeyeon Lee, Min Jung Seo, Eunjung Park, Monica Contreras Dominguez, Ji Youn Nam, Eun Hye Kim
  • COMPOUNDS AND METHODS OF TREATING OBESITY
    Publication number: 20110178151
    Abstract: The present invention relates to novel fatty acid derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds and compositions, especially as agents for the treatment of obesity and related disorders, and for improving cognition.
    Type: Application
    Filed: March 4, 2009
    Publication date: July 21, 2011
    Applicant: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW
    Inventors: Jehoshua Katzhendler, Elliot Berry, Yosefa Avraham, Yousef Najajreh, Meir Saidian, Raphael Mevorach
  • NITROGEN-CONTAINING HETEROCYCLIC COMPOUND AND USE OF SAME
    Publication number: 20110178060
    Abstract: The present invention relates to a compound represented by the formula wherein ring A is a nitrogen-containing heterocycle; ring B is an aromatic ring optionally having substituent(s); ring D is an aromatic ring optionally having substituent(s); L is a group represented by the formula R2, R3, R4a and R4b are each independently a hydrogen atom, an optionally halogenated C1-6 alkyl group or an optionally halogenated C3-6 cycloalkyl group, or R2 and R3 are optionally bonded via an alkylene chain or an alkenylene chain, or R4a and R4b are optionally bonded via an alkylene chain or an alkenylene chain; R1 is a hydrogen atom or a substituent; m and n are each independently an integer of 0 to 5; m+n is an integer of 2 to 5; and is a single bond or double bond, or a salt thereof; and the like.
    Type: Application
    Filed: September 18, 2009
    Publication date: July 21, 2011
    Inventors: Junya Shirai, Hideyuki Sugiyama, Taku Kamei, Hironobu Maezaki
  • USE OF TARGETED NITROXIDE AGENTS IN PREVENTING, MITIGATING AND TREATING RADIATION INJURY
    Publication number: 20110172214
    Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
    Type: Application
    Filed: January 14, 2011
    Publication date: July 14, 2011
    Inventors: Peter Wipf, Natalia A. Belikova, Jianfei Jiang, Joshua Pierce, Joel Greenberger, Michael Epperly, Valerian Kagan
  • NOVEL CATECHOL DERIVATIVE, PHARMACEUTICAL COMPOSITION CONTAINING THE SAME, USE OF THE CATECHOL DERIVATIVE, AND USE OF THE PHARMACEUTICAL COMPOSITION
    Publication number: 20110172208
    Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.
    Type: Application
    Filed: June 26, 2009
    Publication date: July 14, 2011
    Applicant: Kissei Pharmaceutical Co., Ltd.
    Inventors: Takehiro Ishikawa, Satoko Kobayashi, Hitoshi Inoue, Yasunori Ueno, Masako Yoshida, Nobuyuki Tanaka
  • Antibacterial agents
    Publication number: 20110172174
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Application
    Filed: October 31, 2007
    Publication date: July 14, 2011
    Inventors: Niels H. Andersen, Jason Bowman, Alice Erwin, Eric Harwood, Toni Kline, Khisimuzi Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • Inhibitors of plasma kallikrein
    Patent number: 7977380
    Abstract: The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment.
    Type: Grant
    Filed: November 20, 2009
    Date of Patent: July 12, 2011
    Assignee: Activesite Pharmaceticals, Inc.
    Inventors: Sukanto Sinha, Tamie Jo Chilcote
  • Pyrrole derivative having ureido group and aminocarbonyl group as substituents
    Patent number: 7977371
    Abstract: Objects of the present invention are to study on the synthesis of a novel pyrrole derivative having a ureido group and an aminocarbonyl group as substituents or a salt thereof, to find a pharmacological effect of the derivative or a salt thereof, and to find a medicinal agent which has a prophylactic and/or therapeutic effect on a retinal disease or the like through oral administration. A compound represented by the general formula (1) or a salt thereof has an inhibitory activity against the production of interleukin-6 and/or an inhibitory effect on choroidal neovascularization, and is therefore useful as a prophylactic and/or therapeutic agent for a disease associated with interleukin-6, an ocular inflammatory disease and/or a retinal disease.
    Type: Grant
    Filed: February 26, 2008
    Date of Patent: July 12, 2011
    Assignee: Santen Pharmaceutical Co., Ltd.
    Inventors: Kenji Kawashima, Hiroshi Enomoto, Noriko Ishizaka, Minoru Yamamoto, Kazuhiro Kudou, Masaaki Murai, Takaaki Inaba, Kazuyoshi Okamoto
  • Ortho aminoamides for the treatment of cancer
    Patent number: 7977372
    Abstract: Compounds of formula are HDAC inhibitors. These compounds are useful for the treatment of diseases such as cancer in humans or animals.
    Type: Grant
    Filed: February 19, 2010
    Date of Patent: July 12, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Chungen Liang, Guozhi Tang, Jason Christopher Wong, Xihan Wu, Zhenshan Zhang
  • PHARMACEUTICAL COMPOSITIONS OF ATORVASTATIN
    Publication number: 20110165239
    Abstract: The present invention provides stable pharmaceutical compositions comprised of atorvastatin and sodium bicarbonate or L-arginine. The compositions are prepared as bulk drug compositions and also as oral dosage units, such as tablets or capsules. The compositions are useful for preparation of monolithic and bi-layer tablets containing atorvastatin as the only active agent or combined with one or more additional active agents. The compositions are useful for treating hypercholesterolemia and related conditions.
    Type: Application
    Filed: September 21, 2009
    Publication date: July 7, 2011
    Inventors: Laman Alani, Soumojeet Ghosh
  • Pyrrolin-2-ylamino Compounds For Combating Animal Pests
    Publication number: 20110160269
    Abstract: The present invention relates to pyrrolin-2-ylamino compounds for combating animal pests. The invention also relates to a method for controlling animal pests by using these compounds, to plant propagation material and to an agricultural composition comprising said compounds. The invention also relates to a method for treating or protecting an animal from infestation or infection by parasites by using said compounds. wherein n is 0, 1, 2, 3, 4 or 5; m is 0, 1, 2, 3, 4 or 5; R1, R2 are each independently selected from the group consisting of: halogen, CN, N3, NO2, C1-C6-alkyl, C2-C6-alkenyl and C2-C6-alkynyl, where the last 3 radicals mentioned may be partly or completely halogenated and/or may carry any combination of 1, 2 or 3 radicals R#, etc.
    Type: Application
    Filed: September 8, 2009
    Publication date: June 30, 2011
    Inventors: Ralph Paulini, Ronan Le Vezouet, Markus Kordes, Deborah L. Culbertson
  • AMPHIPHILIC PROTEINS AS MORPHOLOGY MODIFIERS
    Publication number: 20110159050
    Abstract: Disclosed is a process for modifying the morphology and/or polymorphism of an organic substance, which process comprises treating the solid substance, or a solution or dispersion thereof, with one or more amphiphilic proteins.
    Type: Application
    Filed: June 23, 2009
    Publication date: June 30, 2011
    Applicant: BASF SE
    Inventors: Andreas Hafner, Andreas Buthe, Paul Adriaan Van Der Schaaf, Franz Kaufmann, Gordon Bradley
  • Treating Vascular Events with Statins by Inhibiting PAR-1 and PAR-4
    Publication number: 20110160236
    Abstract: The present invention relates to new methods for treating and/or preventing vascular events by inhibiting G-coupled Protease Activating Receptor (PAR)-1 and/or PAR-4 with the administration of statins. In one embodiment, individuals who are at risk for vascular events, but have cholesterol levels (e.g., total cholesterol or Low Density Lipoprotein) in normal ranges, are treated with statins.
    Type: Application
    Filed: November 29, 2010
    Publication date: June 30, 2011
    Inventor: Victor L. Serebruany
  • CO-CRYSTALS OF DULOXETINE AND COX-INHIBITORS FOR THE TREATMENT OF PAIN
    Publication number: 20110160273
    Abstract: The present invention relates to co-crystals of duloxetine and co-crystal formers selected from COX-INHIBITORs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.
    Type: Application
    Filed: May 20, 2009
    Publication date: June 30, 2011
    Inventors: Helmut Heinrich Buschmann, Lluis Solá Carandell, Jordi Benet Buchholz, Jordi Carles Ceròn Bertran, Jesüs Ramirez Artero
  • TRYTOPHAN CATABOLISM IN CANCER TREATMENT AND DIAGNOSIS
    Publication number: 20110159017
    Abstract: The unexpected expression of tryptophan 2,3-dioxygenase (TDO2) in cancer cells and tumors has been established. Methods for diagnosing cancer based on the expression of TDO2 are provided, as are methods for treating cancer and inhibiting the growth of cancer cells by inhibiting TDO2, as well as pharmaceutical compositions.
    Type: Application
    Filed: April 10, 2009
    Publication date: June 30, 2011
    Applicant: Ludwig Institute for Cancer Research Ltd.
    Inventors: Benoit Van Den Eynde, Luc Pilotte, Etienne De Plaen
  • COMPOSITIONS AND METHODS FOR MUCOSITIS AND ONCOLOGY THERAPIES
    Publication number: 20110158983
    Abstract: In alternative embodiments, this invention provides compositions and methods for treating cancer or any condition caused by dysfunctional cells, side effects from treatments for cancer or any condition caused by dysfunctional cells, e.g., mucositis therapies (e.g., for oral mucositis; digestive mucositis; esophageal mucositis; intestinal mucositis). In alternative embodiments, the invention provides cytoprotection products that may be used either alone or in combination with other medical therapies such as cancer chemotherapies and radiation therapies.
    Type: Application
    Filed: March 5, 2009
    Publication date: June 30, 2011
    Inventors: Newell Bascomb, John Maki, Fredric S. Young
  • FENOFIBRATE FORMULATION WITH ENHANCED ORAL BIOAVAILABILITY
    Publication number: 20110160274
    Abstract: The present invention provides a formulation of fenofibrate with enhanced oral bioavailability, simplicity of design and manufacture and absence of food effect. The formulation comprises fenofibrate dissolved in a lipophilic surfactant, with a hydrophilic surfactant optionally added. The formulation can be effectively used in the management and treatment of conditions such as hypertriglyceridemia, hypercholesterolemia and mixed dyslipidemia, and can also be effective at lower doses as compared to commercially available products. The invention additionally relates to the process of manufacture of the formulation and to dosage forms comprising the same.
    Type: Application
    Filed: June 26, 2009
    Publication date: June 30, 2011
    Applicant: PANACEA BIOTEC LIMITED
    Inventors: Rajesh Jain, Sarabjit Singh, Naveen Jain, Shivanand Puthli
  • METHODS AND COMPOSITIONS FOR USE OF ANGIOGENESIS INHIBITORS IN THE PREVENTION AND/OR CONTROL OF EPILEPSY
    Publication number: 20110160272
    Abstract: In accordance with some preferred embodiments, without limitation, the invention comprises methods and compositions for the prophylactic and/or antiepileptic administration of angiogenesis inhibitors in conjunction with seizures or traumatic insults to the brain, which administration may limit the extent of trauma-associated angiogenesis and/or decrease the likelihood that angiogenesis will give rise to regional epileptogenecity by preventing/reducing the associated increases in blood-brain barrier permeability among new or existing blood vessels along with their epileptogenic effects.
    Type: Application
    Filed: December 29, 2010
    Publication date: June 30, 2011
    Inventor: KENNETH A. JENROW
  • 1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides and their use in medicaments
    Patent number: 7968591
    Abstract: 1,3-disubstituted 4-methyl-1H-pyrrole-2-carboxamides corresponding to formula I methods for their production, pharmaceutical compositions containing them, and the use thereof for noradrenalin receptor regulation, particularly for inhibiting noradrenalin reuptake, and/or for 5-HT receptor regulation, particularly for inhibiting 5-hydroxy tryptophan reuptake, and/or for opioid receptor regulation and/or for batrachotoxin (BTX) receptor regulation and/or for treating or inhibiting pain and other conditions.
    Type: Grant
    Filed: December 9, 2008
    Date of Patent: June 28, 2011
    Assignee: Gruenenthal GmbH
    Inventors: Stefan Oberboersch, Bernd Sundermann, Corinna Sundermann, Edward Bijsterveld, Hagen-Heinrich Hennies
  • Compositions and Methods for Preventing Migraines
    Publication number: 20110151024
    Abstract: The present invention relates to compositions and methods for preventing migraines. The migraine prophylaxis composition is a single dosage form comprising at least one form of elemental magnesium and at least one NSAID. The prophylaxis composition, comprising at least one form of elemental magnesium and a therapeutically effective concentration of acetylsalicylic acid may also provide cardiac protection and prevent cardiovascular diseases.
    Type: Application
    Filed: March 1, 2011
    Publication date: June 23, 2011
    Inventor: Alexander Mauskop
  • STABILIZED PHARMACEUTICAL COMPOSITION
    Publication number: 20110152342
    Abstract: A pharmaceutical composition is provided which can easily be prepared and which can prevent decomposition of an aminoacetylpyrrolidine carbonitrile derivative, as an effective component, which derivative is in general instable in a pharmaceutical composition. More specifically, the pharmaceutical composition comprises an aminoacetyl pyrrolidine carbonitrile derivative represented by the following general formula (1): (in the formula (1), A represents CH2, CHF or CF2; and R1 represents a secondary amino group which may have a substituent), and the following components blended with the derivative: (1) a sugar alcohol; (2) calcium carbonate, sodium citrate or sodium sulfate; and (3) a neutral low melting point oily and/or fatty substance.
    Type: Application
    Filed: August 14, 2009
    Publication date: June 23, 2011
    Inventors: Hiroshi Uchida, Mamoru Fukuda, Seigo Aritomi
  • CLEAVAGE OF B-AMYLOID PRECURSOR PROTEIN
    Publication number: 20110152341
    Abstract: Methods and means for the identification of meprin-? and meprin-? as novel ?-secretases and antagonists thereof for use in the treatment of amyloidosis.
    Type: Application
    Filed: December 22, 2010
    Publication date: June 23, 2011
    Applicant: PROBIODRUG AG
    Inventors: Stephan Schilling, Dagmar Schlenzig, Hans-Ulrich Demuth
  • Topical application agents against mimic and age-related wrinkles
    Patent number: 7964630
    Abstract: The compounds of formula (I) wherein X represents a bond or NH—CH(C?O)—(CH2)3+n—NH—R5, n represents 0, 1 or 2, R1, R4 and R5—independently from each other—represent hydrogen, possibly substituted C1-C6-alkyl, amidino or tetra-C1-C6-alkylamidinium, R2 represents hydrogen or possibly substituted C1-C6-alkyl or R1 and R2 together with the residue to which they are bound represent a 5- to 7-membered, saturated ring, R3 represents C1-C12-alkoxy, C1-C12-alkylamino, possibly substituted aryl-C1-C6-alkylamino, possibly substituted heteroaryl-C1-C6-alkylamino, possibly substituted aryl-C1-C6-alkoxy or possibly substituted heteroaryl-C1-C6-alkoxy, and R6 represents hydrogen or, when n is 1, also amino or together with R1 and the residue to which R6 and R1 are bound a 5- to 7-membered, saturated ring, as well as their physiologically acceptable salts are new.
    Type: Grant
    Filed: November 1, 2005
    Date of Patent: June 21, 2011
    Assignee: DSM IP Assets B.V.
    Inventors: Dominic Imfeld, Hugo Ziegler, Peter Wikstroem