Bicyclo Ring System Having The Thiazole Ring As One Of The Cyclos Patents (Class 514/367)
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Patent number: 8519149Abstract: The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.Type: GrantFiled: October 28, 2011Date of Patent: August 27, 2013Assignee: Glenmark Pharmaceuticals S.A.Inventors: Laxmikant A. Gharat, Nagarajan Muthukaman, Lakshminarayana Narayana, Neelima Khairatkar-Joshi, Vidya G. Kattige
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Publication number: 20130216552Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed herein.Type: ApplicationFiled: June 24, 2011Publication date: August 22, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Takashi Nakai, James Jia, Jason Rohde, Regina Graul, Ara Mermerian
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Publication number: 20130217699Abstract: Provided are dihydroisoxazole compounds I useful for controlling parasites both in animals and agriculture. Further provided are methods for controlling parasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling parasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. Also provided are compounds and processes useful for making the dihydroisoxazole compounds.Type: ApplicationFiled: May 8, 2012Publication date: August 22, 2013Applicant: ELI LILLY AND COMPANYInventors: Zengyun An, Liang Chen, Shuhui Chen, Jean Marie Defauw, Scott Dale Holmstrom, Ping Hu, Chongzhi Tang, William Hunter White, Wentao Wu, Yang Zhang
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Publication number: 20130217727Abstract: The present invention relates to fungicidal 1-(heterocyclic carbonyl)-2-substituted pyrrolidines and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.Type: ApplicationFiled: October 20, 2011Publication date: August 22, 2013Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Hiroyuki Hadano, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
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Patent number: 8513280Abstract: The present invention is about the use of at least one epothilone or derivative thereof as an active ingredient for manufacturing a medicament for use in the treatment of disease(s) involving a neuronal connectivity defect.Type: GrantFiled: September 9, 2010Date of Patent: August 20, 2013Assignees: Institut National de la Sante et de la Recherche Medicale, Commissariat a l'Energie Atomique, Gesellschaft fur Biotechnologische Forschung mbH (GBF)Inventors: Annie Andrieux, Didier Job, Annie Schweitzer, Gerhard Höfle
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Patent number: 8513291Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.Type: GrantFiled: June 1, 2011Date of Patent: August 20, 2013Assignee: Angion Biomedica Corp.Inventors: Bijoy Panicker, Lambertus J. W. M. Oehlen, James G. Tarrant, Dong Sung Lim, Xiaokang Zhu, Dawoon Jung, Rama K. Mishra
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Publication number: 20130209553Abstract: The present invention discloses an extended release pharmaceutical composition of pramipexole or salts thereof comprising at least 40% w/w of hydrogenated castor oil, and one or more pharmaceutically acceptable excipients.Type: ApplicationFiled: April 15, 2011Publication date: August 15, 2013Applicant: CADILA HEALTHCARE LIMITEDInventors: Sunilendu Bhushan Roy, Sushrut Krishnaji Kulkarni, Ajay Kumar Handa, Pranav Dhirajbhai Jogani
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Publication number: 20130210872Abstract: Disclosed is a method of treating a tumor in a patient, comprising (a) administering riluzole in an amount effective to sensitize the tumor cells to ionizing radiation, and (b) irradiating the tumor cells with ionizing radiation in a dose effective to reduce tumor cell growth. The method can further comprise administering an effective amount of one or more additional therapeutic agents.Type: ApplicationFiled: February 15, 2013Publication date: August 15, 2013Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventor: University of Medicine and Dentistry of New Jersey
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Patent number: 8507509Abstract: Compounds of the general formula (I), wherein the substituents are as defined in claim 1, are useful as fungicides.Type: GrantFiled: September 3, 2008Date of Patent: August 13, 2013Assignee: Syngenta Crop Protection LLCInventors: Fiona Murphy Kessabi, Hans-Georg Brunner, Renaud Beaudegnies, Laura Quaranta, Fredrik Cederbaum, Jayant Umarye
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Publication number: 20130203764Abstract: Substances and methods are disclosed for reducing or preventing metastatic behaviour in VGSC expressing cancer by the effect of at least reducing the persistent part of the voltage gated sodium channel current without eliminating the transient part. Inhibition of metastatic cell behaviours such as detachability, lateral motility, transverse migration and invasiveness is demonstrated using the known drugs ranolazine and riluzole.Type: ApplicationFiled: October 13, 2010Publication date: August 8, 2013Inventor: Mustafa Bilgin Ali Djamgoz
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Publication number: 20130203730Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: March 13, 2013Publication date: August 8, 2013Applicant: AstraZeneca ABInventor: AstraZeneca AB
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Patent number: 8501933Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for treating diseases mediated by a P2X3 and/or a P2X2/3 receptor antagonist and methods of making the subject compounds.Type: GrantFiled: July 26, 2010Date of Patent: August 6, 2013Assignee: Roche Palo Alto LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Publication number: 20130196981Abstract: Novel active compound combinations comprising a carboxamide of the general formula (I) (group 1) in which A, R1, R2 and R3 are as defined in the description, and the active compound groups (2) to (23) listed in the description have very good fungicidal properties.Type: ApplicationFiled: March 13, 2013Publication date: August 1, 2013Applicant: Bayer Intellectual Property GmbHInventor: Bayer Intellectual Property GmbH
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Publication number: 20130196960Abstract: The present disclosure relates to compounds useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders either alone or in combination therapy.Type: ApplicationFiled: February 9, 2011Publication date: August 1, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Jason Rohde, Charles Kim, Takashi Nakai, Galen John Carey
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Patent number: 8497283Abstract: The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: GrantFiled: September 14, 2012Date of Patent: July 30, 2013Assignee: Merck Patent GmbHInventors: Melanie Schultz, Kai Schiemann, Jr., Wolfgang Staehle
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Publication number: 20130190343Abstract: Methods and compositions are provided for preventing or reversing loss of the therapeutic effect of a drug, where the loss is associated with the repeated administration of the drug to a patient. The method includes administering to the patient a dopamine receptor agonist or partial agonist or a drug that increases the extracellular level of dopamine by enhancing release of dopamine, decreasing the removal of dopamine from the extracellular space, enhancing the synthesis of dopamine within the brain, or decreasing metabolic degradation of dopamine; and also administering to the patient an opioid receptor antagonist in an ultra-low dose amount, wherein the ultra-low dose amount is effective to prevent or reverse loss of therapeutic effects associated with the repeated administration of the drug to the patient. The methods are useful for various treatments, including treating Parkinson's Disease, Restless Leg Syndrome, depression, schizophrenia, psychostimulant drug abuse, or attention deficit disorder.Type: ApplicationFiled: February 4, 2013Publication date: July 25, 2013Inventors: David M. Bear, Robert M. Kessler
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Patent number: 8492568Abstract: The present invention provides chromane derivatives as transient receptor potential vanilloid (TRPV) modulators. In particular, the compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: GrantFiled: May 19, 2009Date of Patent: July 23, 2013Assignee: Glenmark Pharamceuticals S.A.Inventors: V. S. Prasada Rao Lingam, Abraham Thomas, Javed Yusuf Khatik, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Publication number: 20130183278Abstract: The present invention relates to method of identifying whether or not an individual has Parkinson's disease (PD). In particular, the invention relates to a method for identifying whether or not an individual has PD as opposed to another neurodegenerative disease. The method of the invention comprises measuring the concentration of ?-synuclein (?-syn) and the concentration of unphosphorylated tau (tau) and/or phosphorylated tau (p-tau) in a cerebrospinal fluid sample taken from an individual. The method also comprises calculating the ratio of the concentration of tau and/or p-tau to the concentration of ?-syn, and thereby determining whether or not the individual has PD.Type: ApplicationFiled: July 6, 2011Publication date: July 18, 2013Applicant: United Arab Emirates UniversityInventors: Omar El-Agnaf, Lucilla Parnetti, Paolo Calabresi
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Publication number: 20130183269Abstract: 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: ApplicationFiled: January 7, 2013Publication date: July 18, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Patent number: 8486981Abstract: Potent and selective ligands for the dopamine 3 (D3) receptor are disclosed. The D3 receptor ligands have a structural formula: wherein R1 is C1-6 alkyl or C3-6cycloalkyl; or wherein R2 is substituted with one or two halogen(s) or OC1-3alkyl.Type: GrantFiled: February 28, 2012Date of Patent: July 16, 2013Assignees: The Regents of the University of Michigan, University of KansasInventors: Shaomeng Wang, Jianyong Chen, Gregory Collins, Beth Levant, James H. Woods
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Publication number: 20130178453Abstract: The present disclosure relates to compounds useful as agonists of the cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders, either alone or in combination therapy. The compounds of the invention have Formula (I).Type: ApplicationFiled: February 9, 2011Publication date: July 11, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Jason Rohde, Bo Peng, Takashi Nakai, Kevin Sprott, Ara MermerÃan, Wayne C. Schairer, Galen John Carey
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Patent number: 8481532Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.Type: GrantFiled: July 9, 2009Date of Patent: July 9, 2013Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Patent number: 8481574Abstract: The present invention relates to compounds of formula (I) wherein A, E, L2, R1, R3, R4 and R5 are as defined in the herein, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: October 12, 2007Date of Patent: July 9, 2013Assignee: Abbott LaboratoriesInventors: Michael D. Meyer, Michael J. Dart, William A. Carroll, Meena V. Patel, Tedozyi Kolasa, Xueqing Wang
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Patent number: 8481547Abstract: The present invention is directed to substituted benzothiazole and benzoxazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.Type: GrantFiled: December 16, 2010Date of Patent: July 9, 2013Assignee: Janssen Pharmaceutica NVInventors: Alfonzo D. Jordan, Renee L. DesJarlais, Dennis J. Hlasta, Michael H. Parker, Carsten Schubert, Kimberly White
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Publication number: 20130172341Abstract: Disclosed are the ERK inhibitors of Formula (I): (Formula (I)) and the pharmaceutically acceptable salts thereof. All substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of Formula (I).Type: ApplicationFiled: September 12, 2011Publication date: July 4, 2013Inventors: Gerald W. Shipps, JR., Yongqi Deng, Alan B. Cooper, Xiaolei Gao, Binyuan Sun, James Wang, Liang Zhu
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Publication number: 20130172333Abstract: Provided is a pharmaceutical composition comprising a pharmaceutically acceptable organic solvent, a pharmaceutically acceptable surfactant, and a compound according to the following formula: wherein the variables are defined herein. Optionally, the pharmaceutical composition further comprises a co-solvent. Also provided is a method of using the pharmaceutical composition disclosed herein for the treatment of a patient in need thereof.Type: ApplicationFiled: May 20, 2011Publication date: July 4, 2013Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Neera Jain, Suresh R. Babu, Shweta Kotecha, Hong Yang
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Publication number: 20130172364Abstract: Disclosed are novel derivatives of propargyl-trifluoromethoxy-amino-benzothiazole which are effective in treating neurologic disorders, including Parkinson's disease and multiple sclerosis.Type: ApplicationFiled: September 29, 2011Publication date: July 4, 2013Applicant: TEVA PHARMACEUTICAL INDUSTRIES LTD.Inventors: Eliezer Falb, Jeffrey Sterling, Yaacov Herzig, Raphael Nudelman, Konstantin Ulanenko
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Publication number: 20130172394Abstract: The present invention is directed to compositions comprising pramipexole and the use of such compositions to treat neurodegenerative diseases such as amyotrophic lateral sclerosis (ALS). As shown in FIG. 6B the mean+/?SEM serum 2,3-DHBA levels for the 12 ALS participants decreased significantly after pramipexole treatment.Type: ApplicationFiled: February 26, 2013Publication date: July 4, 2013Applicant: University of Virginia Patent FoundationInventor: University of Virginia Patent Foundation
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Patent number: 8476450Abstract: A method to detect the presence or amount of at least one molecule in a sample which employs a derivative of luciferin or a derivative of a fluorophore is provided. Compounds and compositions for carrying out the methods of the invention are also provided.Type: GrantFiled: July 3, 2008Date of Patent: July 2, 2013Assignee: Promega CorporationInventors: James J. Cali, William Daily, Erika Hawkins, Dieter Klaubert, Jianquan Liu, Poncho Meisenheimer, Michael Scurria, John Shultz, James Unch, Michael P. Valley, Keith V. Wood, Wenhui Zhou
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Publication number: 20130165454Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: ApplicationFiled: October 18, 2012Publication date: June 27, 2013Applicant: HYDRA BIOSCIENCES, INC.Inventor: HYDRA BIOSCIENCES, INC.
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Patent number: 8470829Abstract: An imidazole derivative represented by formula (I): wherein Q is: A is hydrogen, halogen, or a substituted or unsubstituted C1-4 alkyl group; E is independently selected from a C1-6 alkyl group; R2 and R3 are independently selected from C1-6 alkyls; X1 and X2 are independently selected from O and S; Y is selected from a substituted or unsubstituted arylene group and a substituted or unsubstituted divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group; Z is —CON(—Ra)—, —CO—, —OOO—, —NRa—C(?NH)NRb—, —NRa—C(?N—CN)NRb—, —N(—Ra)COO—, —C(?NH)—, —SO2—, —SO2N(—Ra)—, —SO2NR1—, —N(—Ra)CO—, —N(—Ra)CON(—Rb)—, —N(COR1)CO—, —N(—Ra)SO2—, —N(SO2R1)SO2—, —N(—Ra)— or —N(—Ra)SO2N(—Rb)—; R1 is independently a hydrogen atom, a hydroxyl group, or substituted or unsubstituted group selected from C1-6 alkyl group, heterocyclic group, aryl group, C3-8 cycloalkyl group and C3-8 cycloalkenyl group; or salt or prodrug thereof.Type: GrantFiled: September 9, 2005Date of Patent: June 25, 2013Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Kazutaka Tachibana, Haruhiko Sato, Masateru Ohta, Mitsuaki Nakamura, Takuya Shiraishi, Hitoshi Yoshino, Takashi Emura, Akie Honma, Etsuro Onuma, Hiromitsu Kawata, Kenji Taniguchi
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Patent number: 8471036Abstract: A rhodacyanine derivative represented by the following General Formula (1), wherein, in General Formula (1), R1, R2, and R3 each independently represent an alkyl group which may be substituted; Y1 and Y2 each independently represent a hydrogen atom, a chlorine atom, or a fluorine atom provided that Y1 and Y2 do not represent hydrogen atoms at the same time; and X represents a counter anion. A pharmaceutical composition for treating leishmaniasis including the rhodacyanine derivative and a pharmaceutically acceptable carrier.Type: GrantFiled: October 6, 2010Date of Patent: June 25, 2013Assignees: FUJIFILM Corporation, Hoshi UniversityInventors: Masataka Ihara, Isamu Itoh
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Publication number: 20130158011Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 10, 2012Publication date: June 20, 2013Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER, Bernd WELLENZOHN
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Publication number: 20130157924Abstract: Described herein are compositions and methods for treating or preventing a sexually transmitted infection in a subject.Type: ApplicationFiled: April 22, 2011Publication date: June 20, 2013Applicants: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, University of RochesterInventors: Stephen Dewhurst, Bradley Nilsson, Joanna Olsen, Jerry Yang
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Publication number: 20130150345Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein: one of R3 and R4 is H, and the other is selected from C1-6-alkyl, C1-6-haloalkyl, C1-6-alkoxy, and C6-12-aralkyl; or R3 and R4 are each independently selected from C1-6-alkyl and halo; R9 is a substituted 5 or 6-membered aryl or heteroaryl group or a 6,5- or 6,6-fused biaryl or heterobiaryl group. Compounds of formula (I) exhibit surprisingly high efficacies for human cathepsin S, excellent selectivity verses other mammalian cathepsins and are useful for treatment of diseases such as rheumatoid arthritis, multiple sclerosis, myasthenia gravis, transplant rejection, diabetes, Sjogrens syndrome, Grave's disease, systemic lupus erythematosis, osteoarthritis, psoriasis, idiopathic thrombocytopenic purpura, allergic rhinitis, asthma, atherosclerosis, obesity, chronic obstructive pulmonary disease and chronic pain.Type: ApplicationFiled: January 18, 2013Publication date: June 13, 2013Applicant: AMURA THERAPEUTICS LIMITEDInventor: AMURA THERAPEUTICS LIMITED
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Publication number: 20130150341Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 3, 2012Publication date: June 13, 2013Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF, Bernd WELLENZOHN
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Publication number: 20130150346Abstract: The present disclosure relates to methods of using fatty acid amide hydrolase (FAAH) inhibitors to treat aspects of Parkinson's disease (PD), restless legs syndrome (RLS) and periodic limb movement disorder (PLMD), the use of FAAH inhibitors for the manufacture of medicaments for use in the treatment of PD, RLS and PLMD, as well as pharmaceutically acceptable compositions comprising FAAH inhibitors for use in the treatment of PD, RLS and PLMD.Type: ApplicationFiled: January 7, 2011Publication date: June 13, 2013Applicants: Ironwood Pharmaceutical, Inc.Inventors: James Philip Pearson, Todd G. Milne, Thomas Henry Johnston, Jonathan Michael Brotchie
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Publication number: 20130150367Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: September 12, 2012Publication date: June 13, 2013Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20130150392Abstract: The compound (I) or a salt thereof has an excellent controlling activity against pests. Then the compound (I) or a salt thereof is useful for an active ingredient of a pesticidal composition.Type: ApplicationFiled: February 8, 2013Publication date: June 13, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: SUMITOMO CHEMICAL COMPANY, LIMITED
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Publication number: 20130150347Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 7, 2012Publication date: June 13, 2013Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER, Bernd WELLENZOHN
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Patent number: 8461348Abstract: The present invention aims to provide a compound having superior pharmacological action, physicochemical properties and the like and useful as an sGC activation drug, or an agent for the prophylaxis and/or treatment of diseases such as hypertension, ischemic cardiac disease, cardiac failure, kidney disease, arteriosclerotic disease, atrial fibrillation, pulmonary hypertension, diabetes, diabetic complications, metabolic syndrome, peripheral arterial obstruction, erectile dysfunction and the like. An sGC activation drug containing a compound represented by the formula (II): wherein each symbol is as defined in the specification, or a salt thereof, as an active ingredient.Type: GrantFiled: April 3, 2009Date of Patent: June 11, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Nobuyuki Matsunaga, Yoshihisa Nakada, Yusuke Ohba, Hideyuki Nakagawa
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Publication number: 20130143841Abstract: Embodiments herein provide compounds and methods of making and using such compounds for prevention and treatment of multidrug resistant bacteria. In particular, embodiments are directed to anti-bacterial agents from benzo[d]heterocyclic scaffolds for prevention and treatment of multidrug resistant bacteria.Type: ApplicationFiled: January 29, 2013Publication date: June 6, 2013Applicant: UNIVERSITY OF NOTRE DAME DU LACInventor: UNIVERSITY OF NOTRE DAME DU LAC
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Patent number: 8450304Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, and R4 are as defined in the specification. The invention also comprises pharmaceutical compositions comprising the compounds of formula (I) and methods of preventing, treating or ameliorating a CCR2 mediated syndrome, disorder or disease, for example, type II diabetes, obesity or asthma, by administering the compounds of formula (I).Type: GrantFiled: December 9, 2009Date of Patent: May 28, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Xuqing Zhang, Heather Rae Hufnagel, Cuifen Hou, Dana L. Johnson, Zhihua Sui, Barry Fegely, David Breslin
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Publication number: 20130129839Abstract: Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined in the disclosure; and (b) at least one additional fungicidal compound. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an N-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed is a composition comprising: (a) at least one compound selected from the compounds of Formula 1 described above, N-oxides, and salts thereof; and at least one invertebrate pest control compound or agent.Type: ApplicationFiled: September 1, 2011Publication date: May 23, 2013Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: Jeffrey Keith Long, Vann Gregory, Steven Gutteridge, Andrew Edmund Taggi, James Francis Bereznak
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Publication number: 20130131129Abstract: An agent that increases local concentration of retinoic acid (RA) in the intestine through modifying enzymatic pathways involved in RA metabolism is administered in a dose effective to inhibit or reverse production of inflammatory mediators by intestinal dendritic cells and thereby reduce intestinal inflammation and tumor growth associated with intestinal inflammation.Type: ApplicationFiled: August 22, 2012Publication date: May 23, 2013Inventors: Hwei Xian Leong, Edgar G. Engleman
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Publication number: 20130131044Abstract: The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: May 10, 2011Publication date: May 23, 2013Inventors: Tong-Shuang Li, Ernest J. Mceachern, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu
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Patent number: 8445474Abstract: Compositions of predetermined amounts of R(+) pramipexole and S(?) pramipexole and methods of using the same, including for the treatment and prevention of Parkinson's disease, are provided.Type: GrantFiled: August 5, 2011Date of Patent: May 21, 2013Assignee: Knopp Neurosciences, Inc.Inventors: Michael E. Bozik, Thomas Petzinger, Jr., Valentin Gribkoff
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Publication number: 20130123312Abstract: Pharmaceutical compositions of R(+) pramipexole and methods of using such compositions for the treatment or prevention of diseases associated with or related to mitochondrial dysfunction or increased oxidative stress are disclosed.Type: ApplicationFiled: December 20, 2012Publication date: May 16, 2013Applicant: Knopp Neurosciences Inc.Inventor: Knopp Neurosciences Inc.
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Patent number: 8440705Abstract: Compounds and compositions are provided for treatment or amelioration of one or more symptoms of ?-synuclein toxicity, ?-synuclein mediated diseases or diseases in which ?-synuclein fibrils are a symptom or cause of the disease. In one embodiment, the compounds for use in the compositions and methods are heteroaryl acylguanidines, heteroarylhydrazones, dihydropyridones, heteroaryl and aryl styryl ketones, and heteroarylpyrazoles.Type: GrantFiled: September 16, 2005Date of Patent: May 14, 2013Assignees: Whitehead Institute for Biomedical Research, FoldRx Pharmaceuticals, Inc.Inventors: Susan L. Lindquist, Tiago Outeiro, Richard Labaudinière
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Patent number: 8440706Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease.Type: GrantFiled: February 28, 2011Date of Patent: May 14, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Kevin M. Cottrell, John Maxwell, Qing Tang, Anne-Laure Grillot, Arnaud Le Tiran, Emanuele Perola