Nitrogen Attached Indirectly To The Piperidine Ring By Nonionic Bonding Patents (Class 514/331)
  • PIPERIDINE DERIVATIVES AS HUMAN PAPILLOMA VIRUS INHIBITORS
    Publication number: 20120220633
    Abstract: HPV inhibitors with formula (I) where G1 represents a hydrocarbonated bond or chain possibly substituted by one or two alkyl groups, G2 represents a group (see formula Ia+Ib) or R represents a hydrogen, an alkyl, halogenoalkyl, or a prodrug radical such as carbamate, acetyl or dialkylaminomethy, G represents a bond or a hydrocarbonated chain possibly substituted by one or two alkyls, W represents an oxygen or sulphur, R1 and R2 each represent a group chosen from among hydrogen, halogen, hydroxyl, thio, alkoxy, halogenoalkoxy, alkylthis, halogenoalkylthio, amino, monoalkylamino, dialkylamino, cycloalkyl, alkyl or halogenoalkyl, R3 represents an acid or a prodrug radical of the acid function or a bioisotere of the acid function, A represents an aryl, cycloalkyl, cycloalkenyl or a heterocycle with 6 chains, each possibly substituted, and pharmaceutically acceptable salts.
    Type: Application
    Filed: May 8, 2012
    Publication date: August 30, 2012
    Inventors: Marta Blumenfeld, Delphine Compere, Jean-Michael Gauthier
  • 2-PHENYLETHYLAMINO DERIVATIVES AS CALCIUM AND/OR SODIUM CHANNEL MODULATORS
    Publication number: 20120220592
    Abstract: 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.
    Type: Application
    Filed: January 26, 2012
    Publication date: August 30, 2012
    Applicant: Newron Pharmaceuticals S.p.A.
    Inventors: Florian THALER, Mauro NAPOLETANO, Cibele SABIDO-DAVID, Ermanno MORIGGI, Carla CACCIA, Laura FARAVELLI, Alessandra RESTIVO, Patricia SALVATI
  • Vanilloid receptor ligand compounds, pharmaceutical compositions containing them, a method of producing them and the use thereof to treat pain and various other conditions
    Patent number: 8252816
    Abstract: Compounds corresponding to formula I: which act as vanilloid receptor ligands, pharmaceutical composition s containing such compounds, a method for producing the compounds, and the use of such compounds to treat pain and various other conditions.
    Type: Grant
    Filed: April 11, 2008
    Date of Patent: August 28, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Jeewoo Lee
  • Novel Ethanediamone Hepcidine Antagonists
    Publication number: 20120214798
    Abstract: The present invention relates to novel hepcidin antagonists of formula (I), pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for treatment of disorders in iron metabolism, such as, in particular, iron deficiency diseases and anaemias, in particular anaemias in connection with chronic inflammatory diseases (ACD: anaemia of chronic disease and AI: anaemia of inflammation).
    Type: Application
    Filed: September 6, 2010
    Publication date: August 23, 2012
    Applicant: VIFOR (INTERNATIONAL) AG
    Inventors: Franz Dürrenberger, Susanna Burckhardt, Wilm Buhr, Peter O. Geisser, Felix Funk, Vincent A. Corden, Stephen M. Courtney, Tara Davenport, Stefan Jaeger, Mark P. Ridgill, Mark Slack, Christopher J. Yarnold, Wei Tsung Yau
  • Diagnostic and Therapeutic Alkyl Piperidine/Piperazine Compounds and Process
    Publication number: 20120208847
    Abstract: Described herein are piperidine and piperazine compounds useful for treating neurodegenerated diseases characterized by a lack of dopamine neuron activity. The compounds are also useful for imaging dopamine neurons.
    Type: Application
    Filed: February 14, 2012
    Publication date: August 16, 2012
    Applicant: The General Hospital Corporation
    Inventors: David R. Elmaleh, Choi Sungwoon, Alan J. Fischman
  • METHOD AND PHARMACEUTICAL COMPOSITIONS FOR TRANS-BUCCAL MUCOSA TREATMENT OF POSTPRANDIAL HYPERGLYCAEMIA IN TYPE II DIABETES
    Publication number: 20120190618
    Abstract: The invention provides a method and a pharmaceutical composition in the form of a hydroalcoholic solution in which at least one hypoglycemia-inducing/insulinotropic active principle is dissolved in a stable and complete manner at a dosage that is reduced by 30% to 50% compared with the usual oral unit dosage, for its trans-buccal mucosal application in the spot treatment of postprandial hyperglycemia in type II diabetes in man or animals. The invention also pertains to a method of preparing said formulation and to its specific use in the spot treatment of postprandial hyperglycemia (PPHG) in the context of type II diabetes.
    Type: Application
    Filed: July 7, 2010
    Publication date: July 26, 2012
    Inventors: Philippe Perovitch, Marc Maury, Jean-Pierre Dumonteix
  • N- and O-substituted 4-[2-(diphenylmethoxy)-ethyl]-1-[(phenyl)methyl]piperidine analogs and methods of treating CNS disorders therewith
    Patent number: 8211916
    Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl] piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.
    Type: Grant
    Filed: January 22, 2008
    Date of Patent: July 3, 2012
    Assignee: Wayne State University
    Inventor: Aloke K. Dutta
  • Method of Treating Skin with microRNA Modulators
    Publication number: 20120165373
    Abstract: Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ active agents that suppress or down-regulate microRNA expression in dermal fibroblast, resulting in enhanced production of collagen, elastin and/or fibrillin in the skin. Also provided are methods for screening for activity against specific microRNAs and the methods of using active agents identified by the screening protocol in the treatment of skin.
    Type: Application
    Filed: December 28, 2010
    Publication date: June 28, 2012
    Applicant: Avon Products, Inc.
    Inventors: Permanan Raaj Khusial, Uma Santhanam, John W. Lyga
  • COMPOSITIONS AND METHODS FOR THE TREATMENT OF KRABBE AND OTHER NEURODEGENERATIVE DISEASES
    Publication number: 20120156180
    Abstract: Provided are compositions and methods for the treatment of Krabbe and other neurodegenerative diseases, including storage diseases such as GM1 gangliosidosis, Niemann-Pick disease, Tay-Sachs disease, Sandhoff disease, metachromatic leukodystrophy, Canavan disease, Pelizaeus-Merzbacher disease, and storage conditions facilitated by aging of lysosomal functions, which are associated with psychosine (and/or other storage material)-mediated axonal degeneration.
    Type: Application
    Filed: August 10, 2010
    Publication date: June 21, 2012
    Applicant: The Board of Trustees of the University of Illinois
    Inventor: Ernesto Bongarzone
  • NEW COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF
    Publication number: 20120157425
    Abstract: The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: June 21, 2011
    Publication date: June 21, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Gerald Juergen ROTH, Martin FLECK, Thorsten LEHMANN-LINTZ, Heike NEUBAUER, Bernd NOSSE
  • ALPHA-ARYLMETHOXYACRYLATE DERIVATIVE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME
    Publication number: 20120149707
    Abstract: The present invention relates to an alpha-arylmethoxyacrylate derivative, a preparation method thereof and a pharmaceutical composition comprising the same, and the alpha-arylmethoxyacrylate derivative is inhibitory of HIF, which plays an important role in the regulation of genes associated with energy metabolism, vasomotion, angiogenesis and apoptosis and in the response of cells under hypoxic conditions, so that it can be used for preventing or treating of diseases such as cancer, arthritis, psoriasis, diabetic retinopathy and macular degeneration.
    Type: Application
    Filed: April 21, 2011
    Publication date: June 14, 2012
    Applicant: OSCOTEC INC.
    Inventors: Se-Won Kim, Jung Ho Kim, Se-Nyum Kim, Dae-Pil Kang, Youn Ho Han, Guo Fan Jin, Dong-Sik Jung, Sung-Ho Park, Ji Min Kim, Jhi Zheng
  • Guanidine-containing compounds useful as muscarinic receptor antagonists
    Patent number: 8198304
    Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: September 9, 2011
    Date of Patent: June 12, 2012
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
  • Substituted sulphonamides, process for their preparation, pharmaceutical composition comprising thereof and their use
    Patent number: 8193184
    Abstract: Substituted sulphonamides having the general formula (I) and salts, hydrates and solvates thereof were prepared and described, wherein R1 is CO or SO2 and R2 is NH or O and where R represents linear or cyclic aliphatic chain and n represents number of linking aliphatic chain carbons (n can be 0, 1, 2 or 3), which are useful in the manufacture of the medicaments due to the carboanhydrase inhibition. These compounds are prepared by nucleophilic reaction of an amine with 4-sulfamoylbenzenesulphonyl chloride in the presence of triethylamine excess in tetrahydrofurane or in ether at temperature 0 to 20° C. The compounds show an antiglaucomatic activity.
    Type: Grant
    Filed: April 20, 2008
    Date of Patent: June 5, 2012
    Assignee: Unimed Pharma, SPOL, S.R.O.
    Inventors: Fridrich Gregan, Milan Remko, Elena Sluciakova, Jarmila Knapikova
  • BENZENESULFONYL OR SULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO THE MODULATION OFTHE SEROTONIN 5-HT6 RECEPTOR
    Publication number: 20120129883
    Abstract: The present invention relates to benzenesulfonyl or sulfonamide compounds of formulae IA and IB wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.
    Type: Application
    Filed: November 1, 2011
    Publication date: May 24, 2012
    Applicants: Abbott Laboratories, Abbott GmbH & Co. KG
    Inventors: Andreas Haupt, Frauke Pohlki, Liliane Unger, Ana Lucia Relo, Karsten Wicke, Min Zhang
  • LIBRARIES OF N-SUBSTITUTED-N-PHENYLETHYLSULFONAMIDES FOR DRUG DISCOVERY
    Publication number: 20120122920
    Abstract: New compounds are continually being sought for the treatment and prevention of disorders. The invention relates to N-substituted-N-phenylethylsulfonamides libraries which can be used in the search for, and identification of, new lead compounds that could modulate the functional activity of a biological target.
    Type: Application
    Filed: December 22, 2011
    Publication date: May 17, 2012
    Inventors: JOSEP CASTELLS BOLIART, David Enrique MIGUEL CENTENO, Marta PASCUAL GILABERT
  • Pharmaceutical composition comprising phenylamidine derivative and method of using the pharmaceutical composition in combination with antifungal agent
    Patent number: 8173157
    Abstract: A pharmaceutical composition comprising a phenylamidine derivative or a salt thereof, represented by a general formula, wherein R1 and R2 may be same or different, and represent an optionally substituted C3-4alkyl group; and one or more agents selected from azole antifungal agents, polyene antifungal agents, candin antifungal agents and fluoropyrimidine antifungal agents, and a method for combination use of the phenylamidine derivative or a salt thereof and the agents are useful for treating fungal infections caused by a fungal pathogen.
    Type: Grant
    Filed: October 3, 2007
    Date of Patent: May 8, 2012
    Assignee: Toyama Chemical Co., Ltd.
    Inventor: Hiroshi Nishikawa
  • NEW THERAPEUTIC APPROACHES FOR TREATING NEUROINFLAMMATORY CONDITIONS
    Publication number: 20120108528
    Abstract: The present invention relates to novel compositions which can be used for the treatment of neuroinflammation, in particular in subjects having a neurodegenerative, autoimmune, infectious, toxic or traumatic disorder. More particularly, the invention relates to combined therapies for treating neuroinflammation. The invention also discloses new methods for treating neuroinflammation pathological conditions in a subject.
    Type: Application
    Filed: March 29, 2010
    Publication date: May 3, 2012
    Applicant: Pharnext
    Inventors: Daniel Cohen, Serguei Nabirochkin, Ilya Chumakov
  • METHODS FOR DELIVERING A DRUG TO A HOSPITAL PATIENT FOR SHORT-TERM USE WHILE MINIMIZING LONG-TERM USE OF THE DRUG
    Publication number: 20120101130
    Abstract: Novel methods for delivering a drug to hospital patients for short-term in-hospital use while minimizing long-term use of the drug. Embodiments are provided in which hospitals are identified which may be eligible to treat patients, for example, perform certain types of surgery, and which have measures in place to limit use of the drug to short-term use. The identified hospitals are preferably registered in a storage medium, including computer readable storage media, and may be authorized to receive the shipments of the drug. The received drug may then be dispensed to the patient.
    Type: Application
    Filed: December 29, 2011
    Publication date: April 26, 2012
    Applicant: Adolor Corporation
    Inventors: George Raymond Maurer, Robert Barnett Jones
  • Sulfonamide compounds as cysteine protease inhibitors
    Patent number: 8163735
    Abstract: The present invention is directed to compounds of formula (I) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is -alkylene-SO2NR5R6.
    Type: Grant
    Filed: December 1, 2005
    Date of Patent: April 24, 2012
    Assignee: Virobay, Inc.
    Inventors: Soon H. Woo, Randall W. Vivian, John O. Link
  • COMPOUNDS FOR ACTIVATING TGF-BETA SIGNALING
    Publication number: 20120095000
    Abstract: Compositions and methods for treatment and prevention of disorders and conditions characterized by reduced TGF-? signaling are described.
    Type: Application
    Filed: December 12, 2011
    Publication date: April 19, 2012
    Applicants: SRI International, The Board of Trustees of the Leland Stanford Junior University
    Inventors: Anton Wyss-Coray, Mary J. Tanga
  • 5-HT RECEPTOR MODULATING COMPOUNDS
    Publication number: 20120094989
    Abstract: The present invention relates to compounds having 5-hydroxytryptamine receptor modulating activity, in particular compounds having an acidic moiety held distant from the 5-HT pharmacophore by a rigid linker group, to compositions containing such compounds and methods of treatment using them. Such compounds have an increased affinity for the 5-HT receptor and a reduced hERG effect. Certain compounds of the invention further exhibit an angiotensin II receptor modulating activity. Claimed are compounds of formula (I): HT-L-A. HT is a 5-HT receptor modulating moiety containing a basic nitrogen atom; A is an acid moiety; L is a linker moiety.
    Type: Application
    Filed: April 1, 2010
    Publication date: April 19, 2012
    Applicant: SERODUS AS
    Inventors: Jo Klaveness, Bjame Brudeli, Finn Olav Levy, Lise Roman Moltzau, Trygve Gulbrandsen
  • Modified malonate derivatives
    Patent number: 8158825
    Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: June 21, 2006
    Date of Patent: April 17, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jonathan Grimm, Paul Harrington, Richard Heidebrecht, Jr., Thomas Miller, Karin Otte, Phieng Siliphaivanh, David Sloman, Matthew Stanton, Kevin Wilson, David Witter, Solomon Kattar, Paul Tempest
  • THERAPEUTICS FOR AGE-RELATED MACULAR DEGENERATION
    Publication number: 20120087928
    Abstract: The invention provides compositions and methods of predicting a subject's risk of developing age-related macular degeneration (AMD) and methods of treating, delaying, or preventing the development and progression of AMD.
    Type: Application
    Filed: October 28, 2011
    Publication date: April 12, 2012
    Inventor: Kameran Lashkari
  • Piperidine derivative or salt thereof
    Patent number: 8153658
    Abstract: To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).
    Type: Grant
    Filed: November 14, 2007
    Date of Patent: April 10, 2012
    Assignee: Astellas Pharma, Inc.
    Inventors: Shunichiro Hachiya, Kazuhiro Ikegai, Ryotaro Ibuka, Taisuke Takahashi, Makoto Oku, Ryushi Seo, Yoh Terada, Masanao Sanagi
  • Dopamine-, norepinephrine- and serotonin-transporter-selective heterocyclic compounds and their therapeutic applications
    Patent number: 8153657
    Abstract: One aspect of the invention relates to piperidine compounds that are useful as inhibitors of monoamine transporters. The invention also relates to pharmaceutical compositions, comprising a piperidine compound of the invention. Another aspect of the present invention relates to the use of the aforementioned compounds in a method of treating a disorder of the central nervous system in a mammal.
    Type: Grant
    Filed: October 22, 2004
    Date of Patent: April 10, 2012
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Jia Zhou
  • Polymorph of N,N-diethyl-4-(3-fluorophenyl-piperidin-4-ylidene-methyl)-benzamide hydrochloride salt
    Patent number: 8148406
    Abstract: Polymorphs of N,N-diethyl-4-(3-fluorophenyl-piperidin-4-ylidene-methyl)-benzamide hydrochloride salt, methods of making these polymorphs and uses thereof are described.
    Type: Grant
    Filed: October 5, 2005
    Date of Patent: April 3, 2012
    Assignee: AstraZeneca AB
    Inventors: Simon Nicholas Black, Steve Cook, Louis Joseph Diorazio, James Hulsizer, Gary Moore, Kathryn Quigley
  • ESTROGEN RECEPTOR LIGANDS AND METHODS OF USE THEREOF
    Publication number: 20120077845
    Abstract: The present invention relates to methods for reducing testosterone levels by reduction of luteinizing hormone (LH) or independent of LH levels in a male subject and methods of treating, suppressing, reducing the incidence, reducing the severity, or inhibiting prostate cancer, advanced prostate cancer, and castration-resistant prostate cancer (CRPC) and palliative treatment of prostate cancer, advanced prostate cancer and castration-resistant prostate cancer (CRPC). The compounds of this invention suppress free or total testosterone levels to castrate levels which may be used to treat prostate cancer, advanced prostate cancer, and CRPC without causing bone loss, decreased bone mineral density, increased risk of bone fractures, increased body fat, hot flashes and/or gynecomastia.
    Type: Application
    Filed: August 23, 2011
    Publication date: March 29, 2012
    Inventors: James T. DALTON, Mitchell S. STEINER, Ronald A. MORTON
  • Method of using compounds having ?adrenergic receptor agonist and muscarinic receptor antagonist activity
    Patent number: 8143277
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8a, R8b, W, a, b, c and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Accordingly, such compounds are expected to be useful as therapeutic agents for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: June 5, 2009
    Date of Patent: March 27, 2012
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, Trevor Mischki, Adam Hughes, YuHua Ji
  • METHOD FOR REDUCING THROMBOCYTOPENIA AND THROMBOCYTOPENIA-ASSOCIATED MORTALITY
    Publication number: 20120059036
    Abstract: Disclosed are methods for reducing the risk of thrombocytopenia-associated mortality and morbidity, and for reducing the risk of becoming thrombocytopenic, in patients whose treatment requires inhibition of platelet aggregation. The methods involve administration of a pharmaceutically acceptable salt of tirofiban.
    Type: Application
    Filed: November 20, 2009
    Publication date: March 8, 2012
    Inventor: Marco Valgimigli
  • METHODS AND COMPOSITIONS FOR TREATING INTERNAL AND EXTERNAL HEMORRHOIDS
    Publication number: 20120046318
    Abstract: The present invention relates to compositions and methods for treatment of internal and/or external hemorrhoids, wherein the treatment includes topically administering to a subject a composition comprising from 0.3% to 0.7% of S-2?-[2-(1-methyl-2-piperidyl)ethyl]cinnamanilide, wherein the S-2?-[2-(1-methyl-2-piperidyl)ethyl]cinnamanilide not only treats the hemorrhoidal symptoms but delays or inhibits the recurrence of hemorrhoids and/or symptoms thereof.
    Type: Application
    Filed: August 23, 2010
    Publication date: February 23, 2012
    Inventor: Moh Samir Amer
  • Novel Therapeutic Compounds
    Publication number: 20120046272
    Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.
    Type: Application
    Filed: August 19, 2011
    Publication date: February 23, 2012
    Applicant: GRUNENTHAL GMBH
    Inventor: Ramesh SESHA
  • Diagnostic and therapeutic alkyl piperidine/piperazine compounds and process
    Patent number: 8114379
    Abstract: Piperidine or piperazine compounds useful for treating neurodegenerated diseases characterized by the lack of dopamine neurons activity or for imaging the dopamine neurons are provided.
    Type: Grant
    Filed: April 9, 2008
    Date of Patent: February 14, 2012
    Assignee: The General Hospital Corporation
    Inventors: David R. Elmaleh, Choi Sungwoon, Alan J. Fischman
  • RENIN INHIBITORS
    Publication number: 20120035214
    Abstract: The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: April 1, 2010
    Publication date: February 9, 2012
    Applicants: Merck Canada Inc., Merck Sharp & Dohme Corp.
    Inventors: Daniel J. McKay, Melissa Arbour, Renee Aspiotis, Austin Chen, Pierre-Andre Fournier, Michel Gallant, Yongxin Han, Helene Juteau, Patrick Lacombe, Sebastien Laliberte, Sophie Lauzon, Carmela Molinaro, Paul O'Shea, Yeeman Ramtohul, Daniel Simard, Dwight MacDonald, Bruce Mackay, Christophe Mellon, Krista Morley, Chit Tsui, Sarah Jennifer Dolman, Greg Hughes, Jacob Janey
  • TRANSDERMAL PHARMACEUTICAL PREPARATION AND ADMINISTRATION OF TIROFIBAN
    Publication number: 20120029447
    Abstract: The present invention provides a titratable transdermal drug delivery system comprising an effective dose of an antithrombotic agent, such as tirofiban, or a pharmaceutically acceptable salt thereof. The dosage of the drug delivered is proportional to the size of the patch applied and achieves 60-85% platelet inhibition. The system enables and individualized treatment for patients. Also provided are methods for the treatment of various disorders where platelet inhibition is desired.
    Type: Application
    Filed: March 18, 2010
    Publication date: February 2, 2012
    Applicant: Medicure International Inc.
    Inventors: George Roby Thomas, Dawson James Reimer, Albert D. Friesen
  • INHIBITORS OF FRUCTOSE 1,6-BISPHOSPHATASE AND METHODS OF USE THEREOF
    Publication number: 20120028892
    Abstract: The invention is directed to a compound according to formula (I). The compounds of formula (I) include prodrugs, pharmaceutically acceptable salts, stereoisomer mixtures, and enantiomers thereof. The invention is also directed to a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier and to methods for treating diabetes by administering such a pharmaceutical composition alone or in combination with other therapeutic agents. The invention is also directed to inhibitors of fructose-1,6-bisphosphatase.
    Type: Application
    Filed: February 4, 2010
    Publication date: February 2, 2012
    Applicant: Trustees of Boston College
    Inventors: Evan R. Kantrowitz, Sabrina Heng
  • ACRYLAMIDE COMPOUNDS AND THE USE THEREOF
    Publication number: 20120022069
    Abstract: The invention relates to acrylamide compounds of Formula I mentioned below. The invention is also directed to the use compounds of Formula I to treat or prevent a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Application
    Filed: April 2, 2010
    Publication date: January 26, 2012
    Applicant: Shionogi & Co., Ltd.
    Inventors: Hidenori Mikamiyama, Akira Matsumura, Moriyasu Masui, Kosuke Anan, Kayoko Hata
  • TABLET FORMULATION
    Publication number: 20120012499
    Abstract: The present invention relates to a pharmaceutical fixed dose combination tablet comprising repaglinide and metformin. The present invention also provides a method of producing said tablet.
    Type: Application
    Filed: September 23, 2011
    Publication date: January 19, 2012
    Applicant: Novo Nordisk A/S
    Inventors: Koichi Wada, Hikaru Fujita, Manabu Nakatani, Thomas Friedl
  • (2-ARYLOXYACETYLAMINO) PHENYLPROPIONIC ACID DERIVATIVES, PROCESSES FOR PREPARATION THEREOF AND USE THEREOF AS MEDICAMENTS
    Publication number: 20120004167
    Abstract: The invention relates to substituted (2-aryloxyacetylamino)phenylpropionic acid derivatives, and to the physiologically acceptable salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9 and A are each defined as specified, and the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
    Type: Application
    Filed: July 5, 2011
    Publication date: January 5, 2012
    Applicant: SANOFI
    Inventors: Elisabeth DEFOSSA, Stefanie KEIL, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
  • HETEROCYCLICALLY SUBSTITUTED METHOXYPHENYL DERIVATIVES WITH AN OXO GROUP, PROCESSES FOR PREPARATION THEREOF AND USE THEREOF AS MEDICAMENTS
    Publication number: 20120004165
    Abstract: Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments The invention relates to heterocyclically substituted methoxyphenyl derivatives with an oxo group, and to physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R10, X, n, B1, B2, B3 and B4 are each defined as specified, and to the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
    Type: Application
    Filed: June 7, 2011
    Publication date: January 5, 2012
    Applicant: SANOFI
    Inventors: Stefanie KEIL, Elisabeth DEFOSSA, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
  • BENZOYL-PIPERIDINE DERIVATIVES AS DUAL MODULATORS OF THE 5-HT2A AND D3 RECEPTORS
    Publication number: 20120004208
    Abstract: The present invention relates to compounds of the general formula as dual modulators of the 5-HT2a and D3 receptors useful against CNS disorders, wherein A, R1, R2, n, p, q and r are as defined in the specification.
    Type: Application
    Filed: September 15, 2011
    Publication date: January 5, 2012
    Inventors: Luca Gobbi, Georg Jaeschke, Thomas Luebbers, Olivier Roche, Rosa Maria Rodriguez-Sarmiento, Lucinda Steward
  • ARYLOXYALKYLENE-SUBSTITUTED HYDROXYPHENYLHEXYNOIC ACIDS, PROCESS FOR PREPARATION THEREOF AND USE THEREOF AS A MEDICAMENT
    Publication number: 20120004166
    Abstract: The invention relates to aryloxyalkylene-substituted hydroxyphenylhexynoic acid derivatives, and to physiologically compatible salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14 and A are each defined as specified, and physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.
    Type: Application
    Filed: July 5, 2011
    Publication date: January 5, 2012
    Applicant: SANOFI
    Inventors: Stefanie KEIL, Elisabeth DEFOSSA, Viktoria DIETRICH, Siegfried STENGELIN, Andreas HERLING, Guido HASCHKE, Thomas KLABUNDE
  • UNIT DOSES, AEROSOLS, KITS, AND METHODS FOR TREATING HEART CONDITIONS BY PULMONARY ADMINISTRATION
    Publication number: 20120003318
    Abstract: Methods of treating atrial arrhythmia include administering an effective amount of at least one antiarrhythmic pharmaceutical agent to a patient in need thereof, such that the at least one antiarrhythmic pharmaceutical agent first enters the heart through the pulmonary vein to the left atrium. Other methods of treating atrial arrhythmia include administering by inhalation an effective amount of at least one antiarrhythmic pharmaceutical agent to a patient in need thereof. An amount of the at least one antiarrhythmic pharmaceutical agent may peak in the coronary sinus of the heart at a time ranging from 10 seconds to 30 minutes from initiation of the administering. Unit doses, aerosols, and kits are also contemplated.
    Type: Application
    Filed: March 18, 2010
    Publication date: January 5, 2012
    Inventors: Carlos A. Schuler, Rangachari Narasimhan
  • Pharmaceutical composition comprising a sodium hydrogen exchange inhibitor and an angiotensin converting enzyme inhibitor
    Patent number: 8088799
    Abstract: This invention is directed to a pharmaceutical composition comprising the sodium-hydrogen exchanger (NHE) inhibitor cariporide and an angiotensin converting enzyme (ACE) inhibitor which exhibits unexpectedly efficacious properties for preventing heart failure and other age-related organ dysfunctions, age-related disorders and for prolonging life, and to methods of preventing heart failure and other age-related organ dysfunctions, age-related disorders and for prolonging life comprising administering pharmaceutically effective amounts of the sodium-hydrogen exchange inhibitor cariporide and an ACE inhibitor.
    Type: Grant
    Filed: August 4, 2004
    Date of Patent: January 3, 2012
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Wolfgang Linz, Ursula Schindler
  • Carbocyclic GlyT-1 receptor antagonists
    Patent number: 8080541
    Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: December 20, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • N-Hydroxylsulfonamide Derivatives as New Physiologically Useful Nitroxyl Donors
    Publication number: 20110306614
    Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.
    Type: Application
    Filed: August 19, 2011
    Publication date: December 15, 2011
    Applicants: THE JOHNS HOPKINS UNIVERSITY, CARDIOXYL PHARMACEUTICALS, INC.
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish
  • LARGE SUBSTITUENT, NON-PHENOLIC OPIOIDS AND METHODS OF USE THEREOF
    Publication number: 20110306603
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: August 23, 2011
    Publication date: December 15, 2011
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. Wentland
  • THYROID RECEPTOR LIGANDS
    Publication number: 20110301200
    Abstract: The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta (TR-Beta). Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them.
    Type: Application
    Filed: October 22, 2009
    Publication date: December 8, 2011
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Saurin Raval, Preeti Raval
  • TRYPSIN-LIKE SERINE PROTEASE INHIBITORS, AND THEIR PREPARATION AND USE
    Publication number: 20110301196
    Abstract: The invention provides compounds that are effective as inhibitors of human plasmin and plasma kallikrein, and that are useful for the prevention of blood loss and as components of fibrin adhesives. The invention further provides methods of making and using the compounds.
    Type: Application
    Filed: January 28, 2011
    Publication date: December 8, 2011
    Applicant: The Medicines Company (Leipzig) GmbH
    Inventors: Peter HEROLD, Mohammed DAGHISH, Stjepan JELAKOVIC, Friedrich-Alexander LUDWIG, Claudia REICHELT, Alexander SCHULZE, Andrea SCHWEINITZ
  • Pharmaceutical Formulation Comprising Metformin and Repaglinide
    Publication number: 20110294852
    Abstract: The invention is related to a pharmaceutical composition comprising repaglinide in combination with metformin or a salt thereof in unit dosage form wherein a pre-formulation of the repaglinide has a pH independent dissolution profile and a relative humidity of less than about 25% prior to mixing with the metformin or a salt thereof; and optionally one or more pharmaceutically acceptable excipients and to a method for its preparation.
    Type: Application
    Filed: August 9, 2011
    Publication date: December 1, 2011
    Applicant: Novo Nordisk A/S
    Inventors: Bent Højgaard, Breian Knudsen, Stella Rudkjær Rasmussen, Lene Orup Jacobsen
  • NOVEL COMPOUNDS
    Publication number: 20110294775
    Abstract: Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumour pain and headache diseases.
    Type: Application
    Filed: August 12, 2008
    Publication date: December 1, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter