Plural Ring Hetero Atoms In The Additional Hetero Ring Patents (Class 514/217.09)
  • Patent number: 11046654
    Abstract: A compound having the following structure: or a pharmaceutically acceptable salt or derivative thereof. The compound may be used in the treatment or prevention of a disorder selected from appetite regulation, obesity, metabolic disorders, cachexia, anorexia, pain, inflammation, neurotoxicity, neurotrauma, stroke, multiple sclerosis, spinal cord injury, Parkinson's disease, levodopa-induced dyskinesia, Huntington's disease, Gilles de la Tourette's syndrome, tardive dyskinesia, dystonia, amyotrophic lateral sclerosis, Alzheimer's disease, epilepsy, schizophrenia, anxiety, depression, insomnia, nausea, emesis, alcohol disorders, drug addictions such as opiates, nicotine, cocaine, alcohol and psychostimulants, hypertension, circulatory shock, myocardial reperfusion injury, atherosclerosis, asthma, glaucoma, retinopathy, cancer, inflammatory bowel disease, acute and chronic liver disease such as hepatitis and liver cirrhosis, arthritis and osteoporosis.
    Type: Grant
    Filed: July 9, 2018
    Date of Patent: June 29, 2021
    Assignee: BIAL-PORTELA & CA, S.A.
    Inventors: Carla Patricia da Costa Pereira Rosa, Rita Gusmao De Noronha, Laszlo Erno Kiss, Patricio Manuel Vieira Araujo Soares Da Silva, Domenico Russo, Jorge Bruno Reis Wahnon, William Maton
  • Patent number: 10377718
    Abstract: This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: August 13, 2019
    Assignee: Research Triangle Institute
    Inventors: Scott P. Runyon, Rangan Maitra, Sanju Narayanan, James Barnwell Thomas
  • Patent number: 10351530
    Abstract: The present invention relates to arylcyclohexyl pyrazole compounds of Formula (I) methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
    Type: Grant
    Filed: October 6, 2016
    Date of Patent: July 16, 2019
    Assignees: GlaxoSmithKline Intellectual Property Development Limited, Astex Therapeutics Limited
    Inventors: James Callahan, Jeffrey K. Kerns, Tindy Li, Brent W. McCleland, Hong Nie, Joseph E. Pero, Thomas Glanmor Davies, Charlotte Mary Griffiths-Jones, Thomas Daniel Heightman, Steven Howard, David Norton, Marinus Leendert Verdonk, Alison Jo-Anne Woolford
  • Patent number: 9993551
    Abstract: Combination therapies are disclosed. The combination therapies can be used to treat or prevent cancerous conditions and/or disorders.
    Type: Grant
    Filed: September 11, 2015
    Date of Patent: June 12, 2018
    Assignee: Novartis AG
    Inventors: David Lebwohl, Malte Peters
  • Patent number: 9884847
    Abstract: Provided herein are compounds of the formulas (I) and (II): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of Retinoic Acid Receptor-Related Orphan Receptor regulated diseases and disorders.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: February 6, 2018
    Assignee: INNOV17 LLC
    Inventors: Anderson Gaweco, Jefferson Tilley, James Blinn
  • Patent number: 9586906
    Abstract: Method of lightening the color of mixtures comprising imidazolium salts or imidazoles, wherein the mixtures are treated with an oxidant.
    Type: Grant
    Filed: December 8, 2008
    Date of Patent: March 7, 2017
    Assignee: BASF SE
    Inventors: Michael Siemer, Matthias Maase, Ingo Richter
  • Patent number: 9440957
    Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating EGFR activity, as well as methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated EGFR activity.
    Type: Grant
    Filed: June 5, 2013
    Date of Patent: September 13, 2016
    Assignee: Novartis AG
    Inventors: Gerald Lelais, Robert Epple, Thomas H. Marsilje, III, Pierre-Yves Michellys, Matthew McNeill, Yun Long, Wenshuo Lu, Bei Chen, Badry Bursulaya, Songchun Jiang
  • Patent number: 8975247
    Abstract: Clemizole and clemizole analog compounds, and pharmaceutical compositions of the same, are useful in methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, and methods of treating liver fibrosis in a host.
    Type: Grant
    Filed: March 16, 2010
    Date of Patent: March 10, 2015
    Assignee: The Board of Trustees of the Leland Stanford Junion University
    Inventors: Ingrid C. Choong, David Cory, Jeffrey S. Glenn, Wenjin Yang
  • Publication number: 20150031681
    Abstract: A medicament for treating diseases associated with cholinergic properties in the central nervous system (CNS) and/or peripheral nervous system (PNS), diseases associated with smooth muscle contraction, endocrine disorders, neurodegenerative disorders and the like, which comprises a compound of Formula (I): wherein A is CR1E or a nitrogen atom, X—Y—Z is N—CO—NR3AR3B and the like, R1A to R1E are each independently a hydrogen atom and the like, R2A to R2D are each independently a hydrogen atom and the like, R3A and R3B are each independently an optionally-substituted C3-10 cycloalkyl and the like, and n is 1 or 2 or a pharmaceutically acceptable salt thereof, which exhibits potent modulatory-effects on the activity of ?7 nicotinic acetylcholine receptor (?7 nAChR).
    Type: Application
    Filed: April 9, 2013
    Publication date: January 29, 2015
    Inventors: Shinya Usui, Hiroki Yamaguchi, Yoko Nakai
  • Patent number: 8940730
    Abstract: Briefly described, embodiments of this disclosure include compounds, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.
    Type: Grant
    Filed: March 16, 2010
    Date of Patent: January 27, 2015
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Jeffrey S. Glenn, Wenjin Yang, Ingrid C. Choong
  • Patent number: 8937184
    Abstract: The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid CB2 receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which cannabinoid CB2 receptors are involved. The compounds have the general formula (I) wherein R1-R4 have the meanings given in the specification.
    Type: Grant
    Filed: February 14, 2006
    Date of Patent: January 20, 2015
    Assignee: Abbvie B.V.
    Inventors: Josephus H. M. Lange, Herman H. Van Stuivenberg, Bernard J. Van Vliet
  • Publication number: 20140364408
    Abstract: The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula (I): or a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.
    Type: Application
    Filed: July 29, 2012
    Publication date: December 11, 2014
    Applicant: KARYOPHARM THERAPEUTICS INC.
    Inventors: Vincent P. Sandanayaka, Sharon Shacham, Dilara McCauley, Sharon Shechter
  • Publication number: 20140309185
    Abstract: This document relates to inhibitors of G protein coupled receptor 6 kinase (GRK6) polypeptides as well as methods and materials for using such inhibitors to treat hematological malignancies, inflammation diseases, and autoimmune disorders.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 16, 2014
    Inventors: Alexander Keith Stewart, Artem Plekhov, Robert Greenhouse
  • Publication number: 20140171403
    Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in diseases and disorders mediated by autotaxin.
    Type: Application
    Filed: March 15, 2013
    Publication date: June 19, 2014
    Applicant: Novartis AG
    Inventors: Darren Mark Legrand, Vikki Furminger, Christopher Thomson, Owen Rhys Hughes, Emily Stanley
  • Publication number: 20140171420
    Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
    Type: Application
    Filed: December 6, 2013
    Publication date: June 19, 2014
    Applicant: ChemoCentryx, Inc.
    Inventors: Xi Chen, Pingchen Fan, Yandong Li, Jay P. Powers, Viengkham Malathong, Sreenivas Punna, Hiroko Tanaka, Penglie Zhang, Dean Dragoli
  • Publication number: 20140171404
    Abstract: The present invention relates to novel compounds that are autotaxin inhibitors, processes for their preparation, pharmaceutical compositions and medicaments containing them and to their use in the treatment of an ATX-dependent or ATX-mediated disease or condition.
    Type: Application
    Filed: December 17, 2013
    Publication date: June 19, 2014
    Applicant: NOVARTIS AG
    Inventors: Vikki FURMINGER, Owen Rhys HUGHES, Darren Mark LEGRAND, Emily STANLEY, Christopher THOMSON
  • Patent number: 8735388
    Abstract: The present invention relates to heterocyclic compounds of formula (I) having affinity to muscarinic receptors, a pharmaceutical composition containing the compounds, as well as the use of the compounds for the preparation of a medicament for treating, alleviating or preventing muscarinic receptor medicated diseases and conditions.
    Type: Grant
    Filed: October 16, 2013
    Date of Patent: May 27, 2014
    Assignee: AbbVie B.V.
    Inventors: Axel Stoit, Hein K. A. C. Coolen, Cornelis G. Kruse, Jan H. Reinders
  • Publication number: 20140094450
    Abstract: The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R?, R?, R??, R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 19, 2013
    Publication date: April 3, 2014
    Applicant: SANOFI
    Inventors: Stephanie HACHTEL, Paulus WOHLFART, John WESTON, Marco MUELLER, Elisabeth DEFOSSA, Katharina MERTSCH, Jian-Hui WENG, Robert Alan BINNIE, Farid ABDUL-LATIF, William Jerome BOCK, Armin WALSER
  • Publication number: 20140051688
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, R3, Q, and G are defined herein.
    Type: Application
    Filed: August 16, 2013
    Publication date: February 20, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Michael WINTERS, Zhihua Sui
  • Patent number: 8623863
    Abstract: The present invention is directed to disubstituted azepan and oxazepan amide 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: Grant
    Filed: October 15, 2009
    Date of Patent: January 7, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Mark E. Fraley, John D. Schreier
  • Patent number: 8569504
    Abstract: For the prevention and/or treatment of chymase-mediated diseases such as skin diseases, circulatory diseases, digestive system diseases, respiratory diseases, liver diseases, ocular diseases or the like, a drug is provided having as an active ingredient a compound having extremely strong chymase inhibitory activity, high safety, and high metabolic stability. The compound represented by the formula (I): wherein all symbols have the same meanings as in the description, a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof, is useful as a pharmaceutical ingredient having chymase inhibitory activity for preventing and/or treating of chymase-mediated disease, such as skin diseases, circulatory diseases, digestive system diseases, respiratory diseases, liver diseases, ocular diseases or the like.
    Type: Grant
    Filed: June 16, 2010
    Date of Patent: October 29, 2013
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Jun Takeuchi, Takayuki Inukai, Masaru Sakai
  • Publication number: 20130183269
    Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
    Type: Application
    Filed: January 7, 2013
    Publication date: July 18, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130172324
    Abstract: This invention is directed to methods of preventing or treating diseases or conditions associated with excessive cell proliferation, remodeling, inflammation, and vasoconstriction. Particularly, this invention is directed to methods of treating cardiovascular diseases or conditions such as stent restenosis and thrombosis, vascular thrombosis, cerebral vasospasm, atherosclerosis, systemic hypertension, cardiac hypertrophy, and sexual dysfunction. The method comprises identifying a subject in need of the treatment, and administering to the subject an effective amount of a novel Rho kinase inhibitor compound to treat the disease.
    Type: Application
    Filed: February 22, 2013
    Publication date: July 4, 2013
    Applicant: INSPIRE PHARMACEUTICALS, INC.
    Inventor: Inspire Pharmaceuticals, Inc.
  • Publication number: 20130158014
    Abstract: This invention is directed to methods of preventing or treating diseases or conditions associated with alterations in cellular integrity including alterations in endothelial permeability, excessive cell proliferation or tissue remodeling. Particularly, this invention is directed to methods of treating diabetic nephropathy, malaria, or cancer. The method comprises identifying a subject in need of the treatment, and administering to the subject an effective amount of a novel rho kinase inhibitor compound to treat the disease.
    Type: Application
    Filed: February 8, 2013
    Publication date: June 20, 2013
    Applicant: Inspire Pharmaceuticals, Inc.
    Inventor: Inspire Pharmaceuticals, Inc.
  • Patent number: 8410159
    Abstract: The present invention relates to compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: April 2, 2013
    Assignee: Laboratories del Dr. Esteve, S.A.
    Inventors: Rosa Cuberes-Altisent, Joerg Holenz
  • Publication number: 20130012493
    Abstract: The present invention relates to compounds of the general formula (I): wherein ring A, ring B, G, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
    Type: Application
    Filed: March 22, 2011
    Publication date: January 10, 2013
    Inventors: He Zhao, Ping Chen, Peishan Lin, Peng Dai, Jason Louis Davis, Duane E. DeMong, Michael W. Miller, Xing Dai, Michael K. Wong, Brian J. Lavey, Wensheng Yu, Guowei Zhou, Andrew W. Stamford, Joseph A. Kozlowski, William J. Greenlee
  • Publication number: 20120277217
    Abstract: Presently provided are IDO inhibitors of general formulae (VII), (VIII) as shown below and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase; treating indoleamine 2,3-dioxygenase (IDO) mediated immunosuppression; treating a medical conditions that benefit from the inhibition of enzymatic activity of indoleamine-2,3-dioxygenase; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosupression associated with an infectious disease.
    Type: Application
    Filed: October 27, 2010
    Publication date: November 1, 2012
    Applicant: NewLink Genetics Corporation
    Inventors: Mario R. Mautino, Sanjeev Kumar, Firoz Jaipuri, Jesse Waldo, Tanay Kesharwani, Xiaoxia Zhang
  • Publication number: 20120276050
    Abstract: Clemizole and clemizole analog compounds, and pharmaceutical compositions of the same, are useful in methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, and methods of treating liver fibrosis in a host.
    Type: Application
    Filed: March 16, 2010
    Publication date: November 1, 2012
    Inventors: Ingrid C. Choong, David Cory, Jeffrey S. Glenn, Wenjin Yang
  • Patent number: 8299063
    Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.
    Type: Grant
    Filed: March 13, 2009
    Date of Patent: October 30, 2012
    Assignee: The University of Edinburgh
    Inventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
  • Publication number: 20120238550
    Abstract: There is provided a compound of formula I wherein Z is selected from N and CR22, wherein R22 is H or a bond with D; wherein D is selected from a bond, C?O, and linear or branched hydrocarbon groups having a carbon chain of from 1 to 6 carbon atoms, wherein the carbon chain optionally contains an oxy group (?O), an ether (—O—) or thioether (—S—) link, wherein R1 is selected from: triazolyl, imidazolyl, pyrimidinyl radical wherein each of R2 to R6 is independently selected from —H, NO2, halo, —CN, —N[(C?O)0-1R12][(C?O)0-1R13] and —(CH2)0-1R14, or two adjacent groups of R2 to R6, together with the carbon atoms to which they are attached, form a ring, wherein at least one of R2 to R6 is —CN, wherein (i) at least one of R2 to R6 is —(CH2)0-1R14, or (ii) at least one of R2 to R6 is —N[(C?O)0-1R12][(C?O)0-1R13], or (iii) at least two adjacent groups of R2 to R6 together with the carbon atoms to which they are attached, form a ring, or (iv) at least one of R2 to R6 is —(CH2)0-1—O—R?14, wherein R12 and R13
    Type: Application
    Filed: August 23, 2010
    Publication date: September 20, 2012
    Inventors: Lok Wai Lawrence Woo, Christian Bubert, Paul Michael Wood, Aurélien Putey, Atul Purohit, Barry Victor Lloyd Potter
  • Publication number: 20120207765
    Abstract: A compound represented by general formula (I): a salt thereof, a solvate thereof, or a prodrug thereof wherein all symbols are as defined in the specification has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, systemic erythematosus, retinopathy, macular degeneration, pulmonary fibrosis, transplanted organ rejection, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiac/vascular disease (for example, arteriosclerosis, myocardial infarction, stenocardia, cerebral infarction, chronic arterial occlusive disease, etc.), metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.
    Type: Application
    Filed: March 8, 2012
    Publication date: August 16, 2012
    Applicant: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Masaya Kokubo, Hiroshi Ochiai, Yoshikazu Takaoka, Shiro Shibayama
  • Publication number: 20120165311
    Abstract: Thieno[2,3-c]pyrazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.
    Type: Application
    Filed: February 24, 2012
    Publication date: June 28, 2012
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Daniele Fancelli, Paola Vianello, Mario Varasi, Simona Bindi, Sergio Vioglio, Dania Tesei
  • Patent number: 8207156
    Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
    Type: Grant
    Filed: February 28, 2011
    Date of Patent: June 26, 2012
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Antoni Torrens, Jordi Quintana, Helmut Buschmann, Albert Dordal, Josep Mas
  • Patent number: 8202884
    Abstract: The invention relates to the use of a monoamine neurotransmitter re-uptake inhibitor comprising a 2,3-disubstituted tropane moiety, or a tautomer, a pharmaceutically acceptable salt, solvate, or physiologically functional derivative thereof for the manufacture of a medicament for the treatment of diabetic patients.
    Type: Grant
    Filed: October 31, 2006
    Date of Patent: June 19, 2012
    Assignee: Neurosearch A/S
    Inventors: Klaus Dugi, Andreas Raschig, Juergen Reess, Frank Berger, Laurence Salin
  • Publication number: 20120148534
    Abstract: Briefly described, embodiments of this disclosure include compounds, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of inhibiting HCV replication in a host, methods of inhibiting the binding of NS4B polypeptide to the 3?UTR of HCV negative strand RNA in a host, methods of treating liver fibrosis in a host, and the like.
    Type: Application
    Filed: March 16, 2010
    Publication date: June 14, 2012
    Inventors: Jeffrey S. Glenn, Wenjin Yang, Ingrid C. Choong
  • Publication number: 20120088751
    Abstract: Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: A represents a group selected from one of the following: (CH2)t—, —(CH2)—S(O)z—, or —S(O)z—(CH2)—, B is a heteroaryl, optionally substituted; R is a group selected from the following: alkyl, aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; R? is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R?, a ketonic group of formula —C(O)—Z?, wherein Z? is as defined below; a substituent having an hydroxyl function of formula —CH(OH)—Z?; an amide substituent of formula —C(O)—NH-T?.
    Type: Application
    Filed: December 16, 2011
    Publication date: April 12, 2012
    Applicant: NEUROSCIENCZE PHARMANESS S.C. A R.L.
    Inventors: Paolo LAZZARI, Stefania RUIU, Gerard Aime PINNA, Gabrielle MURINEDDU
  • Publication number: 20120088752
    Abstract: Heterocyclic compounds that modulate the hedgehog signaling pathway, pharmaceutical composition thereof and their therapeutic applications.
    Type: Application
    Filed: June 9, 2010
    Publication date: April 12, 2012
    Applicant: SIENA BIOTECH S.p.A.
    Inventors: J. Russell Thomas, Gal.la Pericot Mohr, Chiara Caramelli, Giacomo Minetto, Marta Bellini
  • Patent number: 8138174
    Abstract: Compounds with a combination of cannabinoid CB1 antagonism and serotonin reuptake inhibition, pharmaceutical compositions containing these compounds, methods for preparing these compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing these compositions are disclosed. Uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders are disclosed. In at least one embodiment, the invention relates to compounds of the general formula (1): wherein the substitutents have the definitions given in the specification.
    Type: Grant
    Filed: January 7, 2008
    Date of Patent: March 20, 2012
    Assignee: Solvay Pharmaceuticals B.V.
    Inventors: Josephus H. M. Lange, Cornelis G. Kruse
  • Publication number: 20120065191
    Abstract: The invention relates to compounds and compositions for inhibiting the enzyme fatty acid amide hydrolase (FAAH), the use of the compounds in therapy and, in particular, for treating or preventing conditions whose development or symptoms are linked to substrates of the FAAH enzyme, and methods of treatment or prevention using the compounds and compositions.
    Type: Application
    Filed: December 23, 2009
    Publication date: March 15, 2012
    Applicant: BIAL - PORTELA & Cª, S.A.
    Inventors: Laszlo Erno Kiss, David Alexander Learmonth, Carla Patrícia da Costa Pereira Rosa, Rita Gusmão de Noronha, Pedro Nuno Leal Palma, Patrício Manuel Vieira Araújo Soares da Silva, Alexander Beliaev
  • Publication number: 20120046275
    Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.
    Type: Application
    Filed: October 13, 2011
    Publication date: February 23, 2012
    Inventors: John W. Lampe, Paul S. Watson, David J. Slade, Ward M. Peterson, Christopher S. Crean, Jason L. Vittitow, Jonathan Bryan DeCamp, Nicholas F. Pelz
  • Publication number: 20120010195
    Abstract: The present invention relates to novel imidazole derivatives of formula (I) having microbiocidal, in particular fungicidal, activity, to processes for their preparation and intermediates used in their preparation, to agrochemical compositions comprising them and to the use in agriculture or horticulture for controlling or preventing infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, preferably fungi.
    Type: Application
    Filed: February 8, 2010
    Publication date: January 12, 2012
    Applicant: SYNGENTA CROP PROTECTION, LLC
    Inventors: Raphael Dumeunier, Clemens Lamberth, Stephan Trah
  • Publication number: 20120004211
    Abstract: The invention relates to the use of compounds having pharmacological activity towards the sigma receptor, and more particularly to 1,2,4-triazole derivatives of formula I to processes of preparation of such compounds and to pharmaceutical compositions comprising them.
    Type: Application
    Filed: September 12, 2011
    Publication date: January 5, 2012
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Nadine Jagerovic, Jose Maria Cumella-Montanchez, Maria Pilar Goya-Laza, Alberto Dordal Zueras, Maria Rosa Cuberes-Altisent
  • Publication number: 20110281848
    Abstract: The present invention relates to compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals.
    Type: Application
    Filed: July 29, 2011
    Publication date: November 17, 2011
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Rosa CUBERES-ALTISENT, Joerg HOLENZ
  • Publication number: 20110251176
    Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: April 6, 2011
    Publication date: October 13, 2011
    Inventor: Xiaojing Wang
  • Publication number: 20110212941
    Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is 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 the neuropeptide S receptor is involved.
    Type: Application
    Filed: November 3, 2009
    Publication date: September 1, 2011
    Inventors: Peter J. Manley, Kausik K. Nanda, B. Wesley Trotter
  • Publication number: 20110207719
    Abstract: A series of novel anthra[1,2-d]imidazole-6,11-dione derivatives, and the preparation method and application of said derivatives, wherein said application includes a pharmaceutical composition containing said derivatives for treating cancer, and said application involves effects of said derivatives for inhibiting telomerase activity, inhibiting the growth of cancer cell, treating cancer and the like.
    Type: Application
    Filed: February 25, 2010
    Publication date: August 25, 2011
    Inventor: Hsu-Shan HUANG
  • Publication number: 20110207715
    Abstract: The present invention is directed to disubstituted azepan and oxazepan amide 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: October 15, 2009
    Publication date: August 25, 2011
    Inventors: Christopher D. Cox, Mark E. Fraley, John D. Schreier
  • Patent number: 7989485
    Abstract: The present invention relates to compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals.
    Type: Grant
    Filed: March 5, 2007
    Date of Patent: August 2, 2011
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Rosa Cuberes-Altisent, Joerg Holenz
  • Publication number: 20110160188
    Abstract: Embodiments of the present disclosure include methods for identifying a compound or compounds useful as therapeutic agents in the treatment of paramyxovirus infections, compounds for the treatment of measles, and high throughput screening methods for identifying compounds capable of inhibiting the proliferation of a paramyxovirus.
    Type: Application
    Filed: February 11, 2008
    Publication date: June 30, 2011
    Inventors: Richard K. Plemper, James P. Snyder, Aiming Sun
  • Publication number: 20110160181
    Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.
    Type: Application
    Filed: February 28, 2011
    Publication date: June 30, 2011
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: ANTONI TORRENS, JORDI QUINTANA, HELMUT BUSCHMANN, ALBERT DORDAL, JOSEP MAS