Nitrogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/352)
Plural acyclic nitrogens bonded directly to the same carbon or bonded directly to each other (Class 514/353)
  • Pyridine compounds, process for their preparation and compositions containing them
    Patent number: 7622486
    Abstract: The present invention provides new heterocyclic compounds, particularly substituted pyridines, methods and compositions for making and using these heterocyclic compounds, and methods for treating a variety of diseases and disease states, including atherosclerosis, arthritis, restenosis, diabetic nephropathy, or dyslipidemia, or disease states mediated by the low expression of Perlecan.
    Type: Grant
    Filed: September 23, 2005
    Date of Patent: November 24, 2009
    Assignee: Reddy US Therapeutics, Inc.
    Inventors: Manojit Pal, Christopher W. Alexander, Ish Khanna, Javed Iqbal, Ram Pillarisetti, Santanu Maitra, Gayla W. Roberts, Lavanya Sagi, Chintakunta Vamsee Krishna, Jennepalli Sreenu
  • Pyridine Analogues VI
    Publication number: 20090286834
    Abstract: The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.
    Type: Application
    Filed: July 2, 2007
    Publication date: November 19, 2009
    Applicant: AstraZeneca AB
    Inventors: Fabrizio Giordanetto, Johan Johansson
  • Opsin Stabilizing Compounds and Methods of Use
    Publication number: 20090286808
    Abstract: The present invention provides compositions and methods useful in the treatment and/or prevention of ophthalmic conditions and diseases, such as retinitis pigmentosa, that are dependent upon or related to misfolded opsin proteins in vivo. In addition, screening assays for agents useful in such treatment methods are described.
    Type: Application
    Filed: January 21, 2009
    Publication date: November 19, 2009
    Applicant: University of Florida Research Foundation, Inc.
    Inventors: Shalesh Kaushal, Syed M. Noorwez, David A. Ostrov
  • Pharmaceutical preparation for treating fibromyalgia
    Publication number: 20090280177
    Abstract: It is difficult to develop pharmaceutical agents for treating fibromyalgia since both the pathogenetic cause and the onset mechanism remain to be clarified. An antirheumatic agent salazosulfapyridine was administered to fibromyalgia patients. Unexpectedly, salazosulfapyridine was seen to be effective in fibromyalgia patients in whom neither the rheumatoid factor nor an immune disorder was detectable, in particular to relieve pain of enthesitis. Furthermore, salazosulfapyridine was also effective to alleviate enthesitis and to relieve pain in fibromyalgia. In addition, the combined use of salazosulfapyridine with a corticosteroid or a nonsteroidal anti-inflammatory agent potentiated the therapeutic effect of salazosulfapyridine in clinical patients to whom salazosulfapyridine alone was not effective enough.
    Type: Application
    Filed: October 4, 2007
    Publication date: November 12, 2009
    Inventor: Kusuki Nishioka
  • TRICYCLIC COMPOUNDS, COMPOSITIONS AND METHODS
    Publication number: 20090281148
    Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.
    Type: Application
    Filed: July 21, 2009
    Publication date: November 12, 2009
    Applicant: Pfizer,Inc.
    Inventors: Hengmiao (Henry) Cheng, Rajesh Devraj, Gary A. Decresenzo, Xiao Hu, Kevin D. Jerome, Mark Obukowicz, Lisa Olson, Ronald Keith Webber
  • ENHANCING PHOTOSTABILIZATION OF OXYMETAZOLINE
    Publication number: 20090281156
    Abstract: The photostability of oxymetazoline in a topical decongestant composition is enhanced by lowering the pH of the composition using a buffer solution.
    Type: Application
    Filed: December 19, 2008
    Publication date: November 12, 2009
    Inventors: Nanhye Kim, Hanwei William Chang
  • ANTI-INFLAMMATORY COMPOUNDS
    Publication number: 20090281093
    Abstract: The present invention relates to novel non steroidal anti-inflammatory compounds (NSAIDs) that release hydrogen sulfide (H2S). The present invention also provides methods for treating, preventing and/or reducing inflammation-associated diseases by releasing H2S in the cardiovascular, connective tissue, pulmonary, gastrointestinal, respiratory, urogenital, nervous, or cutaneous systems as well as infective diseases employing said compounds.
    Type: Application
    Filed: July 29, 2005
    Publication date: November 12, 2009
    Applicant: C.T.G. PHARMA S.R.L.
    Inventors: Anna Sparatore, Piero Del Soldato
  • Antithrombotic ethers
    Patent number: 7615568
    Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor (I).
    Type: Grant
    Filed: April 13, 2004
    Date of Patent: November 10, 2009
    Assignee: Eli Lilly and Company
    Inventors: Jeffry Bernard Franciskovich, David Kent Herron, Jared Harris Linebarger, Angela Lynn Marquart, John Joseph Masters, David Mendel, Leander Merritt, Andrew Michael Ratz, Gerald Floyd Smith, Leland Otto Weigel, Michael Robert Wiley, Ying Kwong Yee
  • Pyridyl Amide T-Type Calcium Channel Antagonists
    Publication number: 20090275550
    Abstract: The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
    Type: Application
    Filed: April 11, 2007
    Publication date: November 5, 2009
    Inventors: James C. Barrow, Kelly-Ann S. Bieber, Rowena V. Cube, Mamio Christa Mattern, Thomas S. Reger, Youheng Shu, Zhi-Qiang Yang
  • Certain chemical entities, compositions, and methods
    Publication number: 20090275537
    Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.
    Type: Application
    Filed: August 11, 2008
    Publication date: November 5, 2009
    Inventors: Xiangping Qian, Chihyuan (Grace) Chuang, Pu-Ping Lu, Bing Yao, Qing (Kevin) Lu, Hong Jiang, Wenyue Wang, Bradley P. Morgan, David J. Morgans, JR.
  • Compounds Which Modulate The CB2 Receptor
    Publication number: 20090275611
    Abstract: Compounds are provided which bind to and are agonist, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula (I) wherein R1, R2, R3, X and Ar have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: April 2, 2007
    Publication date: November 5, 2009
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Doris Riether, David Smith Thomson, Lifen Wu, Renee M. Zindell
  • Iminopyridine Derivatives and Use Thereof
    Publication number: 20090270393
    Abstract: The present invention aims to provide an iminopyridine derivative compound having an ?1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: April 22, 2009
    Publication date: October 29, 2009
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: MASATO YOSHIDA, NOBUKI SAKAUCHI, AYUMU SATO
  • SULFASALAZINE FORMULATIONS IN A BIODEGRADABLE POLYMER CARRIER
    Publication number: 20090264478
    Abstract: Effective treatments of acute pain and/or inflammation for extended periods of time are provided. Through the administration of an effective amount of sulfasalazine at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least three days. In some embodiments, the relief can be for at least twenty-five days, at least fifty days, at least one hundred days, at least one hundred and thirty-five days or at least one hundred and eighty days.
    Type: Application
    Filed: April 18, 2008
    Publication date: October 22, 2009
    Applicant: Warsaw Orthopedic, Inc.
    Inventors: Stephen M. Cox, Christopher M. Hobot, John M. Zanella, Vanja M. King, William F. McKay, Kathy L. Remsen
  • DRUG DEPOTS HAVING DIFFREENT RELEASE PROFILES FOR REDUCING, PREVENTING OR TREATING PAIN AND INFLAMMATION
    Publication number: 20090263441
    Abstract: Effective treatments of pain and/or inflammation are provided. Through the administration of an effective amount of at least analgesic and/or at least one anti-inflammatory agent at or near a target site, one can reduce, prevent or treat inflammation and pain.
    Type: Application
    Filed: April 18, 2008
    Publication date: October 22, 2009
    Applicant: Warsaw Orthopedic, Inc.
    Inventor: William McKay
  • Aminoethane Sulfonamide Orexin Receptor Antagonists
    Publication number: 20090258903
    Abstract: The present invention is directed to aminoethane sulfonamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Application
    Filed: July 31, 2006
    Publication date: October 15, 2009
    Inventors: Paul J. Coleman, Christopher D. Cox, David B. Whitman
  • Pharmaceutical salts and polymorphs of a factor Xa inhibitor
    Patent number: 7598276
    Abstract: The present invention provides for salts comprising a compound of Formula I and an acid that has activity against mammalian factor Xa. The present invention is also directed to methods of making the compound of Formula I.
    Type: Grant
    Filed: November 7, 2006
    Date of Patent: October 6, 2009
    Assignee: Millenium Pharmaceuticals, Inc.
    Inventors: Craig Grant, James P. Kanter, Graeme Langlands
  • Tricyclic compound, compositions, and methods
    Patent number: 7598231
    Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.
    Type: Grant
    Filed: January 31, 2008
    Date of Patent: October 6, 2009
    Assignee: Pfizer, Inc.
    Inventors: Hengmiao (Henry) Cheng, Rajesh Devraj, Gary A DeCresenzo, Xiao Hu, Kevin D. Jerome, Mark Obukowicz, Lisa Olson, Paul V. Rucker, Ronald Keith Webber
  • NEW COMPOUNDS
    Publication number: 20090247534
    Abstract: The present invention provides organic compounds of the following structure; A-L1-B-C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
    Type: Application
    Filed: March 28, 2007
    Publication date: October 1, 2009
    Inventors: Michael H. Serrano-Wu, Young-Shin Kwak, Wenming Liu
  • PYRIDYL DERIVATIVES AS CFTR MODULATORS
    Publication number: 20090246137
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Application
    Filed: March 25, 2009
    Publication date: October 1, 2009
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
  • Compounds having selective inhibiting effect at GSK3
    Patent number: 7595321
    Abstract: The present invention relates to new compounds of formula (I) wherein Z is N; Y is CONR5, NR5CO, SO2NR5, NR5SO2, CH2NR5, NR5, NR5CONR5, CH2CO, CO, O or CH2O; X is CH or N; P is phenyl or a 5 or 6 membered heteroaromatic ring containing one or more heteroatoms selected from N, O or S and said phenyl ring or 5 or 6 membered heteroaromatic ring may optionally be fused with a 5 or 6 membered saturated, partially saturated or unsaturated ring containing one or more atoms selected from C, N, O or S; Q is C1-6alkyl, C2-6alkenyl or C2-6alkynyl, a process for their preparation and new intermediates used therein, pharmaceutical formulations containing said therapeutically active compounds and to the use of said active compounds in therapy, such as provide compounds having a selective inhibiting effect at GSK3.
    Type: Grant
    Filed: December 15, 2003
    Date of Patent: September 29, 2009
    Assignee: AstraZeneca AB
    Inventors: Stefan Berg, Sven Hellberg
  • Amides that inhibit vanilloid receptor subtype 1 (VR1)
    Patent number: 7595332
    Abstract: The present invention relates to compounds of formula (I) that are novel VR1 antagonists useful in treating pain, inflammatory thermal hyperalgesia, urinary incontinence, or bladder overactivity.
    Type: Grant
    Filed: January 19, 2006
    Date of Patent: September 29, 2009
    Assignee: Abbott Laboratories
    Inventors: Chih-Hung Lee, John R. Koenig, Brian S. Brown
  • Kinase protein binding inhibitors
    Publication number: 20090239850
    Abstract: The invention relates to protein binding inhibitor compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating a variety of diseases and disorders, including cell proliferative disorders, especially cancer.
    Type: Application
    Filed: September 15, 2008
    Publication date: September 24, 2009
    Applicant: University of Florida Research Foundation
    Inventors: William G. Cance, Elena Kurenova, Vita Golubovskaya, David A. Ostrov
  • Kinase Inhibitors
    Publication number: 20090233960
    Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula I, II, or III or a stereoisomer, tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, I II III wherein X, R1, R2, R3, R31, n, and m have the meaning defined in the claims. In particular, the present invention relates more specifically to ROCK inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.
    Type: Application
    Filed: October 13, 2006
    Publication date: September 17, 2009
    Applicant: Devgen NV
    Inventors: Philippe Van Rompaey, Philippe Arzel, Olivier Raynald Defert, Dirk Casimir Maria Leysen
  • Methods and compositions for treating mammalian spinal cord injuries
    Patent number: 7582680
    Abstract: Methods of treating an injured vertebrate spinal cord are described. In one aspect of the invention, a method of treating an injured vertebrate spinal cord includes contacting the spinal cord with a biomembrane fusion agent such as a polyalkylene glycol, especially polyethylene glycol. In alternative embodiments of the invention, methods of treating an injured vertebrate spinal cord include contacting the cord with a biomembrane fusion agent and a potassium channel blocker. Other aspects of the invention include compositions for treating a vertebrate nervous system. A preferred composition includes a biomembrane fusion agent, such as a polyalkylene glycol, and a potassium channel blocker, such as an amino-substituted pyridine.
    Type: Grant
    Filed: November 12, 1999
    Date of Patent: September 1, 2009
    Assignees: Purdue Research Foundation, The United States of America as represented by the Secretary of the Army, National Science Foundation
    Inventors: Riyi Shi, Richard B. Borgens
  • Roflumilast for the Treatment of Pulmonary Hypertension
    Publication number: 20090215836
    Abstract: The invention relates to the use of Roflumilast, Roflumilast N-Oxide or a pharmaceutically acceptable salt of either for the treatment of pulmonary hypertension. The invention additionally relates to the use of Roflumilast, Roflumilast N-oxide or a pharmaceutically acceptable salt of either in combination with a PDE5 inhibitor or a pharmaceutically acceptable salt thereof for the treatment of pulmonary hypertension.
    Type: Application
    Filed: April 12, 2006
    Publication date: August 27, 2009
    Applicant: NYCOMED GMBH
    Inventors: Rolf Beume, Armin Hatzelmann, Degenhard Marx, Christian Schudt, Hermann Tenor, Saadia Eddahibi, Serge Adnot
  • COMPOSITIONS AND METHODS FOR EFFECTING NAD+ LEVELS USING A NICOTINAMIDE PHOSPHORIBOSYL TRANSFERASE INHIBITOR
    Publication number: 20090215823
    Abstract: The present invention relates to methods for decreasing cellular DNA repair in a patient diagnosed with or suspected to have chronic lymphocytic leukemia (CLL); decreasing cellular NAD+ biosynthesis in a patient diagnosed with or suspected to have CLL; or sensitizing a patient diagnosed with or suspected to have CLL to a DNA damaging therapy. The invention relates to methods for treating a patient diagnosed with or suspected to have CLL.
    Type: Application
    Filed: March 25, 2009
    Publication date: August 27, 2009
    Inventors: Anne Roulston, Pierre Beauparlant
  • Substituted indole derivatives
    Publication number: 20090215828
    Abstract: Substituted indole derivatives, processes for the preparation thereof, medicinal products and pharmaceutical compositions containing these compounds and the use of substituted indole derivatives to treat pain and other conditions and for other medical purposes.
    Type: Application
    Filed: February 19, 2009
    Publication date: August 27, 2009
    Applicant: GRUNENTHAL GMBH
    Inventors: Stefan Schunk, Stefan Oberborsch, Werner Englberger, Bernd Sunderman
  • Eye drop containing roflumilast
    Publication number: 20090209599
    Abstract: An object of the present invention is to enhance the efficacy of roflumilast in an eye drop containing roflumilast as an active ingredient. By formulating at least one type of viscosity-increasing agent in the eye drop containing roflumilast as an active ingredient, an eye drop in which the efficacy of roflumilast is enhanced can be prepared.
    Type: Application
    Filed: June 9, 2006
    Publication date: August 20, 2009
    Inventors: Yoko Endo, Akio Kimura
  • Heterocyclic compounds as inhibitors of factor VIIa
    Patent number: 7576098
    Abstract: The present invention relates generally to compounds that inhibit serine proteases. In particular it is directed to novel heterocyclic compounds, or a stereoisomer or pharmaceutically acceptable salt, solvate, or prodrug form thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
    Type: Grant
    Filed: December 7, 2005
    Date of Patent: August 18, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter W. Glunz, Nicolas Wurtz, Xuhong Cheng
  • 2,5-disubstituted 3-mercaptopentanoic acid
    Patent number: 7572817
    Abstract: The present invention concerns compounds of formula (I), and pharmaceutically acceptable salts or solvates thereof, or solvates of such salts, which compounds inhibit carboxypeptidase U and thus can be used in the prevention and treatment of diseases where inhibition of carboxypeptidase U is beneficial. In further aspects, the invention relates to compounds of the invention for use in therapy; to processes for preparation of such new compounds; to pharmaceutical compositions containing at least one compound of the invention, or a pharmaceutically acceptable salt or solvate thereof, as active ingredient; and to the use of the active compounds in the manufacture of medicaments for the medical use indicated above.
    Type: Grant
    Filed: June 10, 2003
    Date of Patent: August 11, 2009
    Assignee: AstraZeneca AB
    Inventor: Magnus Polla
  • Pyridinylamines
    Publication number: 20090196912
    Abstract: Described are pyridinylamines and pharmaceutically acceptable salts thereof, the use of these pyridinylamines for the prophylaxis and/or treatment of various diseases such as infectious diseases, including opportunistic infections, prion diseases immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as pharmaceutical compositions containing at least one pyridinylamine and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the pyridinylamines are disclosed.
    Type: Application
    Filed: August 1, 2005
    Publication date: August 6, 2009
    Applicant: GPC Botech AG
    Inventors: Jan Elke Eickhoff, Doris Hafenbradl, Wilfried Schwab, Matthew Cotton, Bert Matthias Kiebl, Birgit Zech, Stefan Muller, John Harris, Vladimir Savic, Jackie MacRitchie
  • Gene expression markers for inflammatory bowel disease
    Publication number: 20090186034
    Abstract: The present invention relates to methods of gene expression profiling for inflammatory bowel disease pathogenesis, in which the differential expression in a test sample from a mammalian subject of one or more IBD markers relative to a control is determined, wherein the differential expression in the test sample is indicative of an IBD in the mammalian subject from which the test sample was obtained.
    Type: Application
    Filed: December 19, 2007
    Publication date: July 23, 2009
    Applicant: Genetech, Inc.
    Inventors: Alexander Abbas, Hilary Clark, Lauri Diehl
  • 1,2-dihydropyridine compounds, manufacturing method thereof and use thereof
    Patent number: 7563811
    Abstract: The present invention provides a novel compound having an excellent AMPA receptor inhibitory action and/or kainate inhibitory action. A compound represented by the following formula, a salt thereof or hydrates thereof. In the formula, Q indicates NH, O or S; and R1, R2, R3, R4 and R5 are the same as or different from each other and each indicates hydrogen atom, a halogen atom, a C1-6 alkyl group or a group represented by the formula —X-A (wherein X indicates a single bond, an optionally substituted C1-6 alkylene group etc.; and A indicates an optionally substituted C6-14 aromatic hydrocarbocyclic group or 5- to 14-membered aromatic heterocyclic group etc.).
    Type: Grant
    Filed: July 6, 2005
    Date of Patent: July 21, 2009
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Satoshi Nagato, Kohshi Ueno, Koki Kawano, Yoshihiko Norimine, Koichi Ito, Takahisa Hanada, Masataka Ueno, Hiroyuki Amino, Makoto Ogo, Shinji Hatakeyama, Yoshio Urawa, Hiroyuki Naka, Anthony John Groom, Leanne Rivers, Terence Smith
  • COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS
    Publication number: 20090181991
    Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Lck, IR, IGF-1R, JNK1?, Flt3, Fes, EFGR (Her-1, erbB-1), cSRC, CDK1/cyclinB, c-RAF, BTK, Bmx, Axl, Aurora-A, Abl, BCR-Abl, TrkB, Tie2, Syk, SGK, SAPK2a, Rsk1 and Met kinases.
    Type: Application
    Filed: November 3, 2006
    Publication date: July 16, 2009
    Inventors: Qiong Zhang, Nathanael S. Gray, Yi Liu, Qiang Ding, Tetsuo Uno
  • OPTICAL ENANTIOMERS OF PHENYRAMIDOL AND PROCESS FOR CHIRAL SYNTHESIS
    Publication number: 20090182016
    Abstract: The present invention discloses optically pure (R) and (S) Phenyramidol enantiomers and their pharmaceutically acceptable salts, a process for synthesising such enantiomers by means of a styrene oxide based asymmetric synthesis, and also a clinical evaluation of (R) and (S) enantiomers of Phenyramidol, their salts and compositions thereof for enhanced/newer therapeutic benefits.
    Type: Application
    Filed: May 21, 2007
    Publication date: July 16, 2009
    Inventors: Anupama Datla, Pramod Abaji Walavalker, Ashok Konda, Sreenath Babunath Trivikram
  • Inhibitors of Histone Deacetylase
    Publication number: 20090181971
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Application
    Filed: August 13, 2007
    Publication date: July 16, 2009
    Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg
  • COMPOUNDS WITH ACTIVITY AT RETINOIC ACID RECEPTORS
    Publication number: 20090176837
    Abstract: Disclosed herein are novel compounds with activity at RAR? 2 receptors. Further disclosed are the use of such compounds for treatment of or to alleviate symptoms of cancer, neurological disorders such as memory deficits and schizophrenia, neurodegenerative disorders such as Parkinson's and Alzheimer's diseases, inflammatory disorders such as psoriasis and rheumatoid arthritis, eye disorders and depression.
    Type: Application
    Filed: July 12, 2006
    Publication date: July 9, 2009
    Applicant: SONY CORPORATION
    Inventors: Roger Olsson, Fabrice Piu, Birgitte Lund
  • COMBINATIONS OF POTASSIUM CHANNEL OPENERS AND SODIUM CHANNEL INHIBITORS OR SODIUM CHANNEL-INFLUENCING ACTIVE COMPOUNDS FOR TREATING PAINS
    Publication number: 20090176814
    Abstract: The invention relates to pharmaceutical combinations of potassium channel openers and sodium channel inhibitors. for treating pains which are accompanied by an increase in muscle tone.
    Type: Application
    Filed: March 12, 2009
    Publication date: July 9, 2009
    Applicant: Valeant Pharmaceuticals North America
    Inventors: Istvan SZELENYI, Kay BRUNE, Robert HERMANN, Mathias LOCHER
  • BRCA1-BASED BREAST OR OVARIAN CANCER PREVENTION AGENTS AND METHODS OF USE
    Publication number: 20090170842
    Abstract: A pharmaceutical composition for use in treating, inhibiting, and/or preventing breast and/or ovarian cancer can include: a molecule having a structure of one of Compounds 1-38, pharmaceutically acceptable salt thereof, or analog thereof, and a pharmaceutically acceptable carrier containing the compound. The pharmaceutically acceptable carrier can be configured for oral, systemic, transdermal, intranasal, suppository, parenteral, intramuscular, intravenous, or subcutaneous administration. The compound can be present in the composition in a therapeutically effective amount for treating, inhibiting, and/or preventing breast and/or ovarian cancer. Also, the compound can be present in a therapeutically effective amount for enhancing production of BRCA1.
    Type: Application
    Filed: November 13, 2008
    Publication date: July 2, 2009
    Applicant: University of Kansas
    Inventors: Roy A. Jensen, Lisa M. Harlan-Williams, Frank J. Schoenen, Jeffrey Aube, Gerald H. Lushington
  • Combination of flupirtine and tramadol
    Patent number: 7553858
    Abstract: The subject of the present invention is to provide a combination of two centrally acting analgesics, flupirtine and tramadol, or their respective pharmaceutically acceptable salts for the treament of pain.
    Type: Grant
    Filed: December 3, 2004
    Date of Patent: June 30, 2009
    Assignee: MEDA Pharma GmbH & Co. KG
    Inventors: Istvan Szelenyi, Joachim Maus, Peter J. Cnota
  • Cannabinergic Lipid Ligands
    Publication number: 20090163557
    Abstract: One aspect of this disclosure relates generally to lipid compounds that exert diverse effects in the endocannabinoid system, such as regulating CB1 and CB2 receptor or moderating other bio-macromolecules within the endocannabinoid system. Some of the compounds showed improved receptor binding affinity, and/or improved receptor subtype selectivity, and improved bio-stability. Some of the compounds exhibit activities to regulate the enzymes that moderate the bio-disposal of endogenous cannabinoids, such as the fatty acid amide hydrolase (FAAH). Some of the compounds exhibit activities to inhibit the anandamide transporter. Other aspects of the invention are pharmaceutical preparations employing these ligands and methods of administering therapeutically effective amounts of the preparations to provide a physiological effect.
    Type: Application
    Filed: October 12, 2005
    Publication date: June 25, 2009
    Inventors: Alexandros Makriyannis, Chen Li, Dai Lu
  • Compounds Which Bind to the Active Site of Protein Kinase Enzymes
    Publication number: 20090163515
    Abstract: The present invention relates to a compound and a group of compounds which are inhibitors of Rho kinase (ROK, ROCK). In addition, the invention relates to methods of treatment and use of the compounds in the manufacture of a medicament for application to a number of therapeutic indications including cardiovascular disease (coronary vasospasm, hypertensive disease, arteriosclerosis), stroke, cancer, erectile dysfunction, asthma, osteoporosis, glaucoma and AIDS. The compounds can be used in screening programmes against protein kinases. The invention also provides methods for making compounds and libraries that include these compounds.
    Type: Application
    Filed: July 1, 2004
    Publication date: June 25, 2009
    Inventors: Veronique Birault, C. John Harris
  • Compositions and Methods for Effecting NAD+ Levels Using A Nicotinamide Phosphoribosyl Tranferase Inhibitor
    Publication number: 20090162454
    Abstract: The present invention relates to methods for decreasing cellular DNA repair in a target patient; decreasing cellular NAD+ biosynthesis in a target patient; increasing efficiency of radiation therapy in a target patient; modulating nicotinamide phosphoribosyl transferase activity in a patient; or sensitizing a patient to a DNA damaging therapy. The invention relates to methods for treating a patient who received a toxic dose of an nicotinamide phosphoribosyl transferase inhibitor. The invention also relates to pharmaceutical compositions comprising a physiologically acceptable carrier; an effective amount of a NMPRT inhibitor; and nicotinic acid. The invention also relates to methods for treating a patient diagnosed with or suspected to have a cancer deficient in nicotinic acid pathway.
    Type: Application
    Filed: September 25, 2008
    Publication date: June 25, 2009
    Inventors: Anne Roulston, Pierre Beauparlant
  • Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of Alzheimer's disease
    Patent number: 7550481
    Abstract: The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: December 15, 2004
    Date of Patent: June 23, 2009
    Assignee: Merck & Co., Inc.
    Inventors: James C. Barrow, Craig A. Coburn, Philippe G. Nantermet, Harold G. Selnick, Shawn J. Stachel, Matthew G. Stanton, Shaun R. Stauffer, Linghang Zhuang, Jennifer R. Davis
  • Tricyclic compounds, compositions, and methods
    Patent number: 7547714
    Abstract: The present invention is directed to compounds of Formula I: or salt thereof, which are modulators of the glucocorticoid receptor. The compounds and salts of the invention are useful in the treatment of conditions mediated by glucocorticoid receptor activity.
    Type: Grant
    Filed: January 31, 2008
    Date of Patent: June 16, 2009
    Assignee: Pfizer, Inc.
    Inventor: Hengmiao (Henry) Cheng
  • Combination of Anticholinergics and Inhibitors of Phosphodiesterase Type 4 For The Treatment of Respiratory Disease
    Publication number: 20090136429
    Abstract: The present invention relates to a combination of an inhaled/oral PDE 4 inhibitor in combination with inhaled anticholinergic bronchodilators (muscarinic receptor antagonists), preferentially Roflumilast or AWD-12-281 and R, R-glycopyrrolate, for symptomatic or prophylactic treatment of respiratory diseases, especially those accompanied by obstruction or inflammation such as chronic obstructive pulmonary disease (COPD) or asthma. It further comprises the presentation of this combination in a locally applied (inhaled) formulation and application in an inhalation device for instance in the Novolizer®.
    Type: Application
    Filed: February 3, 2009
    Publication date: May 28, 2009
    Inventors: Joachim Maus, Peter Juergen Cnota, Istvan Szelenyi, Beatrix Fyrnys
  • GROWTH FACTOR-BINDING COMPOUNDS AND METHODS OF USE
    Publication number: 20090131487
    Abstract: Growth factor binding compounds having a plurality of acyclic isophthalic acid groups attached to a non-peptide organic scaffold and pharmaceutical compositions of the same are disclosed. Methods of administering and using the growth factor binding compounds or the growth factor binding compositions are also taught. These novel growth factor binding compounds are useful for treating angiogenesis, excessive cellular proliferation, tumor growth, and a combination thereof as well as inhibiting growth factor binding to cells and phosphorylation.
    Type: Application
    Filed: December 18, 2008
    Publication date: May 21, 2009
    Inventors: Said M. Sebti, Andrew D. Hamilton, Rishi Jain
  • Structural Analogues of Avenanthramides, Their Use in Compositions Useful in the Treatment of Dermatological Disorders
    Publication number: 20090124669
    Abstract: Novel compounds for the prevention and treatment of dermatological disorders with an immunoallergic, hyperproliferative and inflammatory component, and a method of producing such compounds. The compounds are bioisosteres of substances with avenanthramide structures.
    Type: Application
    Filed: February 21, 2006
    Publication date: May 14, 2009
    Inventor: Carlo Ghisalberti
  • PHARMACEUTICAL COMPOUNDS
    Publication number: 20090124610
    Abstract: Compounds of the formula (I), and salts, solvates, tautomers and N-oxide thereof, wherein TG is selected from groups (1) and (2): wherein the asterisk (*) represents the point of attachment of the group E to the group X; R1a is an optionally substituted aryl or heteroaryl group; R1b is hydrogen or a group R1a; X is an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 are heteroatoms selected from O, N and S; and A, E, R2, R3, R4, Q1 and Q2 are as defined in the claims; provided that when E is aryl or heteroaryl, then Q2 is other than a bond; and further provided that the moiety (a) is other than a group (BG1) or (BG2); wherein (BG1) and (BG2) are each optionally substituted; T is N or CRZ; J1-J2 is selected from N?C(RZ), (RZ)C?N, (RZ)N—C(O), (RZ)2C—C(O), N?N and (RZ)C?C(R6); J4-J3 is a group N?C(RZ) or a group (RZ)N—CO; and RZ is hydrogen or a substituent.
    Type: Application
    Filed: April 25, 2007
    Publication date: May 14, 2009
    Inventors: Gordon Saxty, Marinus Leendert Verdonk, John Caldwell, Ian Collins, Kwai-Ming Cheung, Tatiana Faria Da Fonseca McHardy
  • Amide Derivatives as Kinase Inhibitors
    Publication number: 20090118283
    Abstract: The present invention relates to new AGC kinase inhibitors, in particular to compounds of Formula (I) or (II) or a stereoisomer tautomer, racemic, metabolite, pro- or predrug, salt, hydrate, or solvate thereof, wherein Ar1, Ar2, R1, R3, p and n have the meaning defined in the claims In particular, the present invention relates to more specifically AGC kinases inhibitors, compositions, in particular pharmaceuticals, comprising such inhibitors, and to uses of such inhibitors in the treatment and prophylaxis of disease.
    Type: Application
    Filed: July 11, 2006
    Publication date: May 7, 2009
    Applicant: Devgen NV
    Inventors: Olivier Raynald Defert, Gert De Wilde, Petra Blom, Dirk Casimir Maria Leysen, Thomas Brown, Nadzeya Kaval