Nitrogen Or -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Piperazine Ring Patents (Class 514/255.01)
  • ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
    Publication number: 20110152290
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: November 4, 2010
    Publication date: June 23, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Matthias SCHAEFER, Josef PERNERSTORFER, Dieter KADEREIT, Hartmut STROBEL, Werngard CZECHTIZKY, L. Charlie CHEN, Alena SAFAROVA, Aleksandra WEICHSEL, Marcel PATEK
  • NOVEL AROMATIC COMPOUNDS AND THEIR USE IN MEDICAL APPLICATIONS
    Publication number: 20110152291
    Abstract: Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) and a pharmaceutically acceptable carrier wherein the symbols have the following meaning —X- is e.g. and Y being e.g. or the pharmaceutically acceptable salts can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.
    Type: Application
    Filed: March 1, 2011
    Publication date: June 23, 2011
    Applicant: REVOTAR BIOPHARMACEUTICALS AG
    Inventors: Ewald M. AYDT, Remo Kranich, Anke S. Busemann
  • Compounds and Compositions for Use as Modulators of Tau Aggregation and Alleviation of Tauopathies
    Publication number: 20110144124
    Abstract: This invention relates to the use of bis- and tris-dihydroxyaryl compounds as well as sulfonamides, heteroaryls, tricycloalkyl and their analogs and pharmaceutically acceptable salts, for modulating tau aggregation and alleviating tauopathies, such as Alzheimer's disease (AD), Pick's disease (PiD), progressive supranuclear palsy (PSP), corticobasal degeneration (CBD) and familial frontotemporal dementia/Parkinsonism linked to chromosome 17 (FTDP-17), amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia.
    Type: Application
    Filed: January 20, 2011
    Publication date: June 16, 2011
    Inventors: Alan D. Snow, Qubai Hu, Thomas Lake
  • Guanidine-containing compounds useful as muscarinic receptor antagonists
    Patent number: 7960385
    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 5, 2008
    Date of Patent: June 14, 2011
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
  • Bis-Acylated Hydroxylamine Derivatives
    Publication number: 20110136827
    Abstract: The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: December 7, 2010
    Publication date: June 9, 2011
    Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • THERAPEUTIC AGENT FOR CANCER RESISTANT TO PROTEASE INHIBITOR
    Publication number: 20110112099
    Abstract: The present invention provides therapeutic agents for a cancer resistant to a protease inhibitor which comprises, as an active ingredient, a benzoyl compound represented by formula (I): [wherein n represents an integer of 1 to 5; R1 represents substituted or unsubstituted lower alkyl, CONR7R8 (wherein R7 and R8, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like), or the like; R2 represents substituted or unsubstituted aryl or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, or the like; R4 represents a hydrogen atom or the like; and R6 represents a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, or the like] or a pharmaceutically acceptable salt thereof as a heat shock protein 90 (Hsp90) family protein inhibitor, and the like.
    Type: Application
    Filed: August 21, 2008
    Publication date: May 12, 2011
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Takayuki Nakashima, Yukimasa Shiotsu
  • MOLECULES INHIBITING A METABOLIC PATHWAY INVOLVING THE SYK PROTEIN TYROSINE KINASE AND METHOD FOR IDENTIFYING SAID MOLECULES
    Publication number: 20110112098
    Abstract: The present invention relates to the C-13 molecule (methyl 2-{5-[(3-benzyl-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]-2-furyl}-benzoate) and to organic molecules functionally equivalent to the C-13 molecule, capable of inhibiting the binding of an antibody or antibody fragment with the human Syk protein tyrosine kinase, to the use of these molecules for the production of medicaments for the prevention or treatment of diseases dependent on metabolic pathways involving Syk, and also to a method for identifying such molecules.
    Type: Application
    Filed: April 8, 2009
    Publication date: May 12, 2011
    Inventors: Piona Dariavach, Pierre Emile Ulysse Martineau, Bruno Villoutreix
  • HETEROCYCLIC DERIVATIVES AS HDAC INHIBITORS
    Publication number: 20110105474
    Abstract: This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; R1 is hydrogen, halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl or C1 C6 haloalkoxy; R2, R3 are, independently, hydrogen; C1-C6 alkyl; aryl; or taken together with the carbon atoms to which they are bound form a bridged bicyclic ring or a fused heterocycle; X is CH or nitrogen; Y is a bond, oxygen, (CH2)mCR4R5(CH2)n, or (CH2)oNR6(CH2)p; m, n, o, p, R4, R5 and R6 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
    Type: Application
    Filed: June 8, 2009
    Publication date: May 5, 2011
    Inventors: Florian Thaler, Mario Varasi, Stefania Gagliardi, Andrea Colombo, Saverio Minucci, Ciro Mercurio
  • Piperazines and piperidines as Mglur5 potentiators
    Patent number: 7935703
    Abstract: Compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: wherein Ar1, Ar2, A, X, Y, m, n and R1, R2, R3, R4 and R5 are as described in the specification, processes for their preparation, pharmaceutical formulations comprising them and their use in therapy, particularly in the therapy of neurological and psychiatric disorders associated with glutamate dysfunction.
    Type: Grant
    Filed: January 5, 2007
    Date of Patent: May 3, 2011
    Assignee: AstraZeneca AB
    Inventors: Abdelmalik Slassi, Methvin Isaac, Jalaj Arora, Dean Brown
  • METHODS OF INHIBITING THE FORMATION OF AMYLOID-BETA DIFFUSABLE LIGANDS USING ACYLHYDRAZIDE COMPOUNDS
    Publication number: 20110098309
    Abstract: Disclosed are methods of inhibiting, regulating, and/or modulating the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers from amyloid ?1-42 monomers using acylhydrazide compounds. Also disclosed are methods of treating a patient suffering from diseases associated with the formation of soluble, globular, non-fibrillar, neurotoxic amyloid ?1-42 oligomers using acylhydrazide compounds.
    Type: Application
    Filed: July 11, 2008
    Publication date: April 28, 2011
    Applicant: ACUMEN PHARMACEUTICALS, INC.
    Inventors: Gary Charles Look, Lauri Schultz, Alexandre Mikhaylovich Polozov, Nikhil Bhagat, Jian Wang, David E. Zembower, William F. Goure, Todd Pray, Grant A. Krafft
  • 2-aminocarbonyl substituted piperazine or diaza-cyclic compounds as apoptosis protein inhibitors (lap) modulators
    Patent number: 7932255
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates or pharmaceutically acceptable formulations thereof. These compounds may be used to modulate cellular proliferation and to prevent and/or treat proliferative diseases.
    Type: Grant
    Filed: April 13, 2006
    Date of Patent: April 26, 2011
    Assignee: Novartis AG
    Inventors: Robert Eckl, Roswitha Taube, Michael Almstetter, Michael Thormann, Andreas Treml, Christopher Straub, Zhouliang Chen
  • Spirocyclopropyl amides and acids and their therapeutic applications
    Patent number: 7932245
    Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of epilepsy, bipolar disorder, psychiatric disorders, migraine, pain, or movement disorders, and to provide neuroprotection.
    Type: Grant
    Filed: October 22, 2003
    Date of Patent: April 26, 2011
    Assignee: Abbott Laboratories
    Inventors: Youssef L. Bennani, William H. Bunnelle, Sou-Jen Chang, Sanjay R. Chemburkar, Jinhua Chen, Michael J. Dart, Dilinie P. Fernando, Yi-Yin Ku, Mark Lockwood, Lei Wang
  • Antifouling Compounds And Use Thereof
    Publication number: 20110092518
    Abstract: The present invention relates to the use of compounds which have the following general formula (I), wherein R1 and R2 are independently selected from optionally substituted aryl, optionally substituted C1 to C12 alkyl and H; and R3 and R4 are independently selected from hydroxy, optionally substituted C1 to C6 alkyl, optionally substituted phenyl and H, in a method of preventing or reducing fouling, particularly in the marine environment. The compounds of the present invention have the considerable advantage of providing the antifouling coating market with an organic alternative to the existing technology which relies heavily on the addition of copper to obtain significant antifouling effects. The compounds we have developed may be used as cheap, easy to prepare additives that do not contain metals and therefore have reduced toxicity in marine environment.
    Type: Application
    Filed: May 18, 2009
    Publication date: April 21, 2011
    Applicants: NATIONAL UNIVERSITY OF SINGAPORE, AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH, MARITIME AND PORT AUTHORITY OF SINGAPORE
    Inventors: Lay Ming Serena Teo, Daniel Rittschof, Felicity Jameson, Christina Chai, Chia Lung Chen, Siew Chen Serina Lee
  • N-HYDROXYAMIDE DERIVATIVES AND USE THEREOF
    Publication number: 20110086864
    Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
    Type: Application
    Filed: December 16, 2010
    Publication date: April 14, 2011
    Inventors: Dominique Swinnen, Jerome Gonzalez
  • Methods of Treating Aneurysmal Dilatation, Blood Vessel Wall Weakness and Specifically Abdominal Aortic and Thoracic Aneurysm Using Matrix Metalloprotease-2 Inhibitors
    Publication number: 20110082114
    Abstract: The present invention provides methods of treating aneurysmal dilatation, blood vessel wall weakness, and specifically abdominal aortic aneurysm and thoracic aneurysm by inhibiting MMPs and ADAM-10. Such compounds are useful in the in vitro study of the role of MMPs and ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more MMPs or ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of aneurysmal dilatation or blood vessel wall weakness, for example abdominal aortic aneurysm and thoracic aneurysm.
    Type: Application
    Filed: September 30, 2010
    Publication date: April 7, 2011
    Applicant: SYMPHONY EVOLUTION, INC.
    Inventor: Alastair J.J. Wood
  • CLASS OF HISTONE DEACETYLASE INHIBITORS
    Publication number: 20110077247
    Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.
    Type: Application
    Filed: December 7, 2010
    Publication date: March 31, 2011
    Applicant: DAC S.r.I.
    Inventors: Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Pier Giuseppe Pelicci, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
  • NOVEL 17 BETA LUPANE DERIVATIVES
    Publication number: 20110077251
    Abstract: The invention relates to 17? lupane derivatives of formula (I): wherein R1 and X are as defined herein, and pharmaceutically acceptable salts and solvates thereof. These compounds exhibit significant anti-HIV activity. Thus, the invention also relates to methods for prevention or treatment of HIV infection by administering therapeutically effective amounts of a compound of formula (I), or a pharmaceutically acceptable salt or solvate thereof to a subject in need of such treatment.
    Type: Application
    Filed: August 16, 2010
    Publication date: March 31, 2011
    Inventors: Christophe Moinet, Bingcan Liu, Liliane Halab, Nathalie Turcotte, Real Denis, Carl Poisson, Paul Nguyen-Ba, Monica Bubenik, Laval Chan Chun Kong
  • SUBSTITUTED PHENYLAMINO-BENZENE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH MITOGEN EXTRACELLULAR KINASE ACTIVITY
    Publication number: 20110071125
    Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 9, 2008
    Publication date: March 24, 2011
    Inventors: Joachim Rudolph, Jaques Dumas, Li Yingfu, Daniel Auclair, Mario Lobell, Marion Hitchcock, Ingo Hartung, Marcus Koppitz, Dominic Brittain, Florian Puehler, Kirstin Petersen, Judith Guenther, Benjamin Bader
  • Prostaglandin derivatives
    Patent number: 7910767
    Abstract: Prostaglandin nitroderivatives having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.
    Type: Grant
    Filed: November 6, 2009
    Date of Patent: March 22, 2011
    Assignee: Nicox S.A.
    Inventors: Ennio Ongini, Valerio Chiroli, Francesca Benedini, Piero Del Soldato
  • 1,4-NAPHTHOQUINONES DERIVATIVES AND THERAPEUTIC USE THEREOF
    Publication number: 20110059972
    Abstract: 1,4 naphthoquinones derivatives, of formula (I) wherein A is selected from the following rings: their preparation and their application as antimalarial agents
    Type: Application
    Filed: March 25, 2009
    Publication date: March 10, 2011
    Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Elisabeth Davioud-Charvet, Tobias Muller, Holger Bauer, R. Heiner Schirmer
  • METHOD OF TREATING INHERITED SEVERE NEUTROPENIA
    Publication number: 20110059960
    Abstract: The invention is directed to a method of treating severe neutropenia, and in particular, cyclic neutropenia (CN) or severe congenital neutropenia (SCN), in a patient in need of such treatment comprising: administering a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 5, 2008
    Publication date: March 10, 2011
    Inventors: David C. Dale, Paul E. Finke, Richard A. Munford, Andranik Andrew Aprikyan
  • Hydroxamate-Based Inhibitors of Deacetylases
    Publication number: 20110053925
    Abstract: The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, ring A, and are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of using compounds of Formula I in treating, inhibiting, or preventing pathologic conditions or disorders mediated wholly or in part by deacetylases.
    Type: Application
    Filed: August 27, 2010
    Publication date: March 3, 2011
    Inventors: Young Shin CHO, Lei JIANG, Michael SHULTZ, Christine Hiu-Tung CHEN, Gang LIU, Jianke LI
  • NOVEL COMPOUNDS ADVANTAGEOUS IN THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISEASES AND DISORDERS
    Publication number: 20110046128
    Abstract: A series of novel compounds showing anticonvulsant, chemical countermeasure(s), and analgesic activities is described. Such pharmaceutically active compounds may also show utility in the treatment of other central nervous system (“CNS”) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, Parkinson's disease, spasticity, Alzheimer's disease, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), chronic neurodegenerative diseases (such as Alzheimer's disease and Huntington's disease), and/or traumatic brain and/or spinal cord injuries. Moreover, these/such compounds may also be useful in the treatment of status epilepticus and/or as chemical countermeasures.
    Type: Application
    Filed: September 13, 2010
    Publication date: February 24, 2011
    Applicant: AURIMMED PHARMA, INC.
    Inventors: Amir Pesyan, Manuel F. Balandrin
  • BENZOCYCLOHEPTANE AND BENZOXEPINE DERIVATIVES
    Publication number: 20110046139
    Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor.
    Type: Application
    Filed: April 27, 2009
    Publication date: February 24, 2011
    Inventors: Bruno Schoentjes, Alain Philippe Poncelet, Julien Georges Pierre-Olivier Doyon, Joannes Theodorus Maria Linders, Lieven Meerpoel, Luc August Laurentius Ver Donck
  • TREATMENT OF HEARING AND BALANCE IMPAIRMENTS WITH REDOX-ACTIVE THERAPEUTICS
    Publication number: 20110046156
    Abstract: Compositions and methods are provided for prophylactic or therapeutic treatment of a mammal for hearing or balance impairments involving neuronal damage, loss, or degeneration, by administration of a therapeutically effective amount of a redox-active therapeutic. Also provided are improved compositions and methods for treatments requiring administration of a pharmaceutical having an ototoxic side-effect in combination with a therapeutically effective amount of a redox-active therapeutic to treat the ototoxicity.
    Type: Application
    Filed: March 4, 2009
    Publication date: February 24, 2011
    Inventor: Guy M. Miller
  • NOVEL PIPERAZINE DERIVATIVES AS INHIBITORS OF STEAROYL-CoA DESATURASE
    Publication number: 20110046134
    Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
    Type: Application
    Filed: October 29, 2010
    Publication date: February 24, 2011
    Inventors: Alexander Bischoff, Hosahalli Subramanya, Kumar Sundaresan, Srinivasa Raju Sammeta, Anil Kumar Vaka
  • Treating psychological conditions using muscarinic receptor Mantagonists
    Patent number: 7893053
    Abstract: Provided are methods of treating psychological diseases and conditions by administration of a preferential muscarinic acetylcholine receptor M1 antagonist, optionally with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist. The invention also provides for pharmaceutical compositions and kits for administration of at least one selective muscarinic acetylcholine receptor M1 antagonist in combination with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist.
    Type: Grant
    Filed: June 14, 2007
    Date of Patent: February 22, 2011
    Assignee: Theracos, Inc.
    Inventors: Brian Seed, Jordan Mechanic
  • Compositions and methods for inhibiting growth and metastasis of melanoma
    Patent number: 7888355
    Abstract: There are provided methods of inhibiting growth and metastasis of melanoma, methods of sensitizing melanoma cells to apoptosis, and methods of treating a subject having melanoma using acetyl isogambogic acid, celastrol, or a derivative thereof. There are further provided derivatives of celastrol and compositions comprising acetyl isogambogic acid, celastrol, or a derivative thereof.
    Type: Grant
    Filed: August 11, 2010
    Date of Patent: February 15, 2011
    Assignee: Burnham Institute for Medical Research
    Inventors: Ze′ev A. Ronai, Anindita Bhoumik, Nicholas D. P. Cosford, Russell Dahl
  • HOMOCYSTEINE SYNTHASE INHIBITOR
    Publication number: 20110034440
    Abstract: The invention provides a homocysteine synthase inhibitor useful for the prophylaxis or treatment of diseases involving homocysteine synthase. The homocysteine synthase inhibitor is a compound of the formula (I) wherein each symbol is as defined herein, or a pharmacologically acceptable salt thereof, or a solvate thereof.
    Type: Application
    Filed: April 10, 2009
    Publication date: February 10, 2011
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Akira Nakao, Hiroko Suzuki, Ryo Tatsumi, Maki Seki, Minoru Tanaka, Tomofumi Setsuta, Hiroshi Iwasaki
  • ANTHELMINTIC AGENTS AND THEIR USE
    Publication number: 20110021506
    Abstract: This invention is directed to compounds and salts that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds and salts, pharmaceutical compositions and kits comprising the compounds and salts, uses of the compounds and salts to make medicaments, and treatments comprising the administration of the compounds and salts to animals in need of the treatments.
    Type: Application
    Filed: December 16, 2008
    Publication date: January 27, 2011
    Applicant: INTERVET INTERNATIONAL B.V.
    Inventors: Christophe Pierre Alain Chassaing, Jörg Schröder, Thomas Simon Ilg, Manfred Uphoff, Thorsten Meyer
  • LUPEOL-TYPE TRITERPENE DERIVATIVES AS ANTIVIRALS
    Publication number: 20110015196
    Abstract: The invention relates to novel lupeol-type triterpene derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.
    Type: Application
    Filed: July 2, 2010
    Publication date: January 20, 2011
    Applicant: HETERO RESEARCH FOUNDATION
    Inventors: Bandi PARTHASARADHI REDDY, Vedula MANOHAR SHARMA, Kura RATHNAKAR REDDY, Musku MADHANMOHAN REDDY, Nelli YELLA REDDY, Lanka VL SUBRAHMANYAM
  • Histamine H3 Receptor Ligands
    Publication number: 20110009420
    Abstract: The present invention provides compounds of the formula wherein R1, R2 and B are as herein described, pharmaceutical compositions comprising these compounds, use of these compounds for the preparation of pharmaceutical compositions and methods of use thereof for the treatment and/or prevention of disorders and diseases wherein modulation of the H3 receptor is beneficial.
    Type: Application
    Filed: September 16, 2010
    Publication date: January 13, 2011
    Applicant: HIGH POINT PHARMACEUTICALS, LLC
    Inventor: Knud Erik Andersen
  • N-hydroxyamide derivatives and use thereof
    Patent number: 7868009
    Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I): and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
    Type: Grant
    Filed: January 27, 2006
    Date of Patent: January 11, 2011
    Assignee: Merck Serono, S.A.
    Inventors: Dominique Swinnen, Jerome Gonzalez
  • Human Adam-10 Inhibitors
    Publication number: 20110003812
    Abstract: Magnesium salts/complexes of compounds useful for inhibiting the ADAM-IO protein and methods of making and purifying them are provided. Further provided are compositions comprising magnesium salts/complexes of the compounds in combination with a pharmaceutically acceptable carrier. The compounds well as such compositions comprising them are useful for the treatment of cancer, arthritis, diseases related to angiogenesis, such as renal diseases, heart diseases, such as heart failure, atherosclerosis, and stroke, inflammation, ulcer, infertility, scleroderma, endometriosis, mesothelioma, and diabetes. In addition, methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role are provided.
    Type: Application
    Filed: October 15, 2008
    Publication date: January 6, 2011
    Applicant: SYMPHONY EVOLUTION, INC.
    Inventors: Sriram Naganathan, JoAnn Wilson, Daniel Dickman
  • Opsin-binding ligands, compositions and methods of use
    Publication number: 20110003784
    Abstract: Compounds and compositions of said compounds along with methods of use of compounds are disclosed for treating ophthalmic conditions related to mislocalization of opsin proteins, the misfolding of mutant opsin proteins and the production of toxic visual cycle products that accumulate in the eye. Compounds and compositions useful in the these methods, either alone or in combination with other therapeutic agents, are also described.
    Type: Application
    Filed: June 16, 2010
    Publication date: January 6, 2011
    Inventors: David S. Garvey, Gregory J. LaRosa, Jeremy R. Greenwood, Mark L. Brewer, Tan Quach, Jamie B. Côté, Judd Berman
  • N-SULPHONYLATED AMINO ACID DERIVATIVES, METHOD FOR THE PRODUCTION AND USE THEREOF
    Publication number: 20110002992
    Abstract: The present invention relates to N-sulfonylated amino acid derivatives, where an aryl radical is linked via the sulfonyl group N-terminally to the amino acid and a radical which comprises at least one imino group and at least one further basic group which represents an optionally modified amino, amidino or guanidino group is linked C-terminally via the carbonyl group. The invention likewise relates to processes for preparing these compounds and to their use, in particular as inhibitors of matriptase.
    Type: Application
    Filed: July 1, 2010
    Publication date: January 6, 2011
    Applicant: The Medicines Company (Leipzig) GmbH
    Inventors: Jörg Stürzebecher, Torsten Steinmetzer, Andrea Schweinitz, Anne Stürzebecher, Kerstin Uhland
  • DERIVATIVES OF SUBSTITUTED TARTARIC ACID AND USAGE FOR PREPARING BETA-SECRETASE INHIBITORS
    Publication number: 20100331345
    Abstract: The present invention relates to compounds represented by formula (I), or isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof: in which each substituent of formula (I) is as defined in the specification. The present invention also relates to preparation methods of compounds represented by formula (I), a pharmaceutical composition comprising compounds represented by formula (I) and usage of compounds represented by formula (I) for treating chronic neurodegenerative diseases such as Alzheimer's disease and other diseases induced by aggregation or deposition of ?-amyloid peptide.
    Type: Application
    Filed: February 5, 2007
    Publication date: December 30, 2010
    Inventors: Song Li, Guochao Liao, Junhai Xiao, Aihua Nie, Lili Wang, Wu Zhong, Zhibing Zheng
  • METHODS FOR TREATING DRUG ADDICTION AND IMPROVING ADDICTION-RELATED BEHAVIOR
    Publication number: 20100331332
    Abstract: The invention is directed to a method of treating addiction to drugs of abuse in a subject, comprising administering a therapeutically effective amount of a cabamoyl compound, or pharmaceutically acceptable salt or ester thereof.
    Type: Application
    Filed: June 26, 2009
    Publication date: December 30, 2010
    Applicant: SK HOLDINGS CO., LTD.
    Inventors: Sung James Lee, Susan Marie Melnick
  • Antibacterial Agents
    Publication number: 20100324025
    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: September 21, 2009
    Publication date: December 23, 2010
    Applicant: University of Washington
    Inventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • NOVEL CYCLOPENTANE DERIVATIVES
    Publication number: 20100317647
    Abstract: The invention relates to a compound of formula (I) wherein A1 and R1 to R5 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: June 2, 2010
    Publication date: December 16, 2010
    Inventors: David Banner, Simona M. Ceccarelli, Uwe Grether, Wolfgang Haap, Hans Hilpert, Holger Kuehne, Harald Mauser, Jean-Marc Plancher, Rubén Alvarez Sánchez
  • Composition Comprising An NK-1 Receptor Antagonist And An SSRI For The Treatment Of Tinnitus And Hearing Loss
    Publication number: 20100317666
    Abstract: The present invention relates to methods for treating a subject suffering from tinnitus, hearing loss, or tinnitus and hearing loss comprising administering to the subject an effective amount of an NK1 receptor antagonist alone, or in combination with an effective amount of a selective serotonin reuptake inhibitor. Compositions and pharmaceutical formulations are also provided.
    Type: Application
    Filed: October 18, 2007
    Publication date: December 16, 2010
    Inventors: Soren Rahn Christensen, Emilio Merlo Pich, Emiliangelo Ratti, Tadataka Yamada
  • META-SUBSTITUTED PHENYL SULFONYL AMIDES OF SECONDARY AMINO ACID AMIDES, THE PRODUCTION THEREOF, AND USE THEREOF AS MATRIPTASE INHIBITORS
    Publication number: 20100305090
    Abstract: The invention relates to meta-substituted phenyl sulfonyl amides of secondary amino acid amides according to the general formula (I), (II), or (III), the production thereof, and the use thereof as matriptase inhibitors, in particular the use thereof as drugs for inhibiting tumor growth and/or metastasization.
    Type: Application
    Filed: March 5, 2008
    Publication date: December 2, 2010
    Inventors: Torsten Steinmetzer, Andrea Schweinitz, Daniel Donnecke
  • Piperazine derivatives as inhibitors of stearoyl-CoA desaturase
    Patent number: 7842696
    Abstract: The present invention relates to piperazine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
    Type: Grant
    Filed: June 23, 2008
    Date of Patent: November 30, 2010
    Assignee: Forest Laboratories Holdings Limited
    Inventors: Alexander Bischoff, Hosahalli Subramanya, Kumar Sundaresan, Srinivasa Raju Sammeta, Anil Kumar Vaka
  • METHOD FOR TESTING AND SCREENING P38 MAP KINASE MODIFIERS
    Publication number: 20100297665
    Abstract: This invention provides methods for treating diseases associated with elevated p38 mitogen-activated protein kinase activity. Moreover, the invention provides methods for testing a candidate compound for a p38 mitogen-activated protein kinase modifying activity by calculating the level of relocalization of an SMN complex component from the cytoplasm to the nucleus of a cell. Additionally, the invention provides a kit and a system for calculating the same.
    Type: Application
    Filed: June 4, 2008
    Publication date: November 25, 2010
    Inventors: Gideon Dreyfuss, Mumtaz Kasim
  • NON-PEPTIDE DERIVATIVES AS BRADYKININ B1 ANTAGONISTS
    Publication number: 20100298299
    Abstract: The present invention relates to new non-peptide derivatives of formula (I), wherein R1-R5, Q and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, to pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.
    Type: Application
    Filed: October 27, 2007
    Publication date: November 25, 2010
    Inventors: Istvan Vago, Sandor Farkas, Katalin Hornok, Gyula Beke, Eva Bozo, Monika Vastag, Eva Szentirmay, Gyorgy Keseru, Eva Schmidt
  • Glycine Transporter-1 Inhibitors
    Publication number: 20100298341
    Abstract: The present invention provides compounds that are glycine transporter 1 (hereinafter referred to as GlyT-1) inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of GlyT1 such as cognitive disorders associated with Schizophrenia, ADHD (attention deficit hyperactivity disorder), MCI (mild cognitive impairment), and the like. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
    Type: Application
    Filed: December 11, 2008
    Publication date: November 25, 2010
    Inventors: Stephen A. Hitchcock, Wenyuan Qian, Albert Amegadzie
  • Diamine-containing, tetra-substituted piperazine compounds having identical 1- and 4-substituents
    Patent number: 7834017
    Abstract: There is provided compounds having the formula of structure I: wherein the groups —C(R8)(CH2)vCH(R9)(CH2)y-Q and —C(R8)(CH2)vCH(R9)(CH2)y-J are the same, and R1a, R1b, R2a, R2b, R8, R9, J, Q, W, X, L2, v and y have meanings given in the description. The use of such compounds in the treatment of a condition responsive to changes in melanocortin receptor function in a human or non-human mammal (e.g. male sexual dysfunction, female sexual dysfunction, an eating disorder, above optimal body weight, obesity, below-optimal body weight or cachexia) is also described.
    Type: Grant
    Filed: August 10, 2007
    Date of Patent: November 16, 2010
    Assignee: Palatin Technologies, Inc.
    Inventors: Kevin Burris, Yi-Qun Shi, Shubh D. Sharma, Yadi Reddy Bonuga, Papireddy Purma
  • CXCR3 RECEPTOR ANTAGONISTS
    Publication number: 20100280028
    Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R5, A, B, D and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: April 27, 2010
    Publication date: November 4, 2010
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Jennifer A. KOWALSKI, Daniel Richard MARSHALL, Anthony S. PROKOPOWICZ, III, Sabine SCHLYER, Robert SIBLEY, Ronald John SORCEK, Di WU, Frank WU, Erick Richard Roush YOUNG
  • DICARBONYL DERIVATIVES AND METHODS OF USE
    Publication number: 20100279963
    Abstract: Derivatives of dicarbonyl compounds having antitumor and antibiotic activity which can be used as anticancer agents.
    Type: Application
    Filed: July 1, 2010
    Publication date: November 4, 2010
    Applicant: Abraxis BioScience, LLC
    Inventors: Chunlin Tao, Qinwei Wang, Vuong Trieu, Neil Desai, Patrick Soon-Shiong
  • Derivatives Of Hydroxamic Acid As Metalloproteinase Inhibitors
    Publication number: 20100280018
    Abstract: A compound of formula (I), or an enantiomer or diastereoisomer thereof, or a salt, hydrate or solvate thereof: for the treatment or prophylaxis of arthritis in mammals.
    Type: Application
    Filed: July 20, 2010
    Publication date: November 4, 2010
    Applicants: Laboratoires Serono S.A., Vernalis (Oxford) Limited
    Inventors: Gilles Pain, Stephen John Davies, Agnes Bombrun