Pyrazoles Patents (Class 514/406)
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Patent number: 8895517Abstract: A composition comprising a carboxamide compound represented by following formula (I), wherein R1 represents a hydrogen atom or a methyl group, and R2 represents a methyl group, a difluoromethyl group or a trifluoromethyl group, and abamectin is provided by the present invention, and this composition has an excellent pesticidal effect.Type: GrantFiled: April 25, 2011Date of Patent: November 25, 2014Assignee: Sumitomo Chemical Company, LimitedInventor: Yuichi Matsuzaki
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Patent number: 8895601Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: GrantFiled: April 28, 2011Date of Patent: November 25, 2014Assignee: Astex Therapeutics LtdInventors: Gordon Saxty, Christopher William Murray, Valerio Berdini, Gilbert Ebai Besong, Christopher Charles Frederick Hamlett, Christopher Norbert Johnson, Steven John Woodhead, David Charles Rees, Laurence Anne Mevellec, Patrick René Angibaud, Eddy Jean Edgard Freyne, Timothy Pietro Suren Perera, Ronaldus Arnodus Hendrika Joseph Gilissen, Berthold Wroblowski, Jean Fernand Armand Lacrampe, Alexandra Papanikos, Oliver Alexis Georges Querolle, Elisabeth Thérèse Jeanne Pasquier, Isabelle Noëlle Constance Pilatte, Pascal Ghislain André Bonnet, Werner Constant Johan Embrechts, Rhalid Akkari, Lieven Meerpoel
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Publication number: 20140343018Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.Type: ApplicationFiled: July 24, 2014Publication date: November 20, 2014Inventors: Steven L. McKnight, Andew A. Pieper, Joseph M. Ready, Jef K. De Brabander, Jeffrey M. Zigman
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Publication number: 20140343037Abstract: Disclosed are compounds and pharmaceutically acceptable salts of Formula I wherein R1, R2, R3, R4, R5, R6, R7, n, Q1, Q2, Q3, Y, and X1-X4 are as defined herein. Compounds of Formula I are useful in the treatment of diseases and/or conditions related to cell proliferation, such as cancer, inflammation, arthritis, angiogenesis, or the like. Also disclosed are pharmaceutical compositions comprising compounds of the invention and methods of treating the aforementioned conditions using such compounds.Type: ApplicationFiled: August 4, 2014Publication date: November 20, 2014Inventors: Kenneth He Huang, Jeron Eaves, Gunnar Hanson, James Veal, Thomas Barta, Lifeng Geng, Lindsay Hinkley
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Publication number: 20140343077Abstract: A compound of formula (I) useful for the treatment or prevention of hepatitis C viral infection, (Formula (I)) wherein: X1 and X2 are each independently CRB or N; RB is H, (C1-6)alkyl, (C1-6)haloalkyl, halo.Type: ApplicationFiled: August 22, 2012Publication date: November 20, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Christian Brochu, Chantal Grand-Maitre, Lee Fader, Cyrille Kuhn, Megan Bertrand-Laperle, Marc Pesant
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Publication number: 20140343113Abstract: The present invention relates to fungicidal N-bicycloalkyl and N-tricycloalkyl pyrazole-4-(thio)carboxamide derivatives of formula (I), wherein T represents 0 or S; n represents 0 or 1; and B represents where the bond marked by * is attached to the (CZ2Z3)n-N amide moiety, 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: November 29, 2012Publication date: November 20, 2014Inventors: Jürgen Benting, Stéphane Brunet, Pierre-Yves Coqueron, Pierre Cristau, Peter Dahmen, Philippe Desbordes, Stéphanie Gary, Jörg Greul, Hélène Lachaise, Jan-Peter Schmidt, Philippe Rinolfi, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
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Publication number: 20140342912Abstract: This invention relates to the use of aromatic phosphate esters of formula (I) wherein R1, R2 and R2 are as defined within the description, as adjuvants in compositions, particularly for agrochemical use, as well to compositions comprising such an aromatic phosphate ester, in combination with at least one agrochemical and optionally at least one surfactant. The invention further extends to methods of making and using such compositions.Type: ApplicationFiled: November 23, 2012Publication date: November 20, 2014Applicant: SYNGENTA LIMITEDInventors: Gordon Alastair Bell, Philip Taylor
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Patent number: 8889727Abstract: An anti-fungal agent for tinea comprising as active ingredient a compound having the skeleton of 2-(1H-pyrazol-1-yl)phenol represented by the following formula (I) or (II) or a salt thereof is providedType: GrantFiled: January 30, 2012Date of Patent: November 18, 2014Assignee: Meiji Seika Pharma Co., Ltd.Inventors: Makoto Ohyama, Yuji Tabata, Maiko Iida, Kaori Kaneda, Sho Takahata
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Publication number: 20140336440Abstract: Compounds and compositions having activity as inhibitors of Rho-associated proteinkinases (ROCKs), and methods of making and using the subject compounds are disclosed.Type: ApplicationFiled: January 24, 2013Publication date: November 13, 2014Inventors: Ernst Schonbrunn, Rongshi Li, Said M. Sebti
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Publication number: 20140336154Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II 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: ApplicationFiled: July 29, 2014Publication date: November 13, 2014Inventors: Steven Do, Richard Goldsmith, Tim Heffron, Aleksandr Kolesnikov, Steven Staben, Alan G. Olivero, Michael Siu, Daniel P. Sutherlin, Bing-Yan Zhu, Paul Goldsmith, Tracy Bayliss, Adrian Folkes, Neil Pegg
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Publication number: 20140336224Abstract: Compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases are disclosed. Processes for preparing compounds of the Formula (I), use of the compounds for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and pharmaceutical compositions which comprise compounds of the Formula (I) are disclosed.Type: ApplicationFiled: October 18, 2012Publication date: November 13, 2014Inventors: Ping Lan, Kun Liu, Anthony Ogawa, Hong Shen, Christine Yang, Yuguang Wang, Richard Beresis, Changhe Qi
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Publication number: 20140336194Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.Type: ApplicationFiled: July 28, 2014Publication date: November 13, 2014Applicant: NOVARTIS AGInventor: Shi Yin FOO
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Patent number: 8883850Abstract: The present invention is directed to naphthalene carboxamide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimers disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: May 23, 2011Date of Patent: November 11, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Douglas C. Beshore, Christina Ng DiMarco, Scott D. Kukuk
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Patent number: 8883826Abstract: The present invention relates to novel compounds of formula I wherein W, n, X and W? are defined in the description; invention compounds are modulators of metabotropic glutamate receptors—subtype 5 (“mGluR5”) which are useful for the treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.Type: GrantFiled: December 20, 2011Date of Patent: November 11, 2014Assignee: Addex Pharma SAInventors: Anne-Sophie Bessis, Christelle Bolea, Beatrice Bonnet, Mark Epping-Jordan, Nicolas Poirier, Sonia-Maria Poli, Jean-Philippe Rocher, Yves Thollon
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Publication number: 20140329777Abstract: Methods to treat infectious diseases are disclosed herein. Some embodiments of the invention include administration of one or more COX inhibitors (e.g., COX-1 or COX-2 inhibitors) to treat infectious diseases. Other embodiments of the invention include administration of one or more COX inhibitors (e.g., COX-1 or COX-2 inhibitors) and administration of one or more antibiotics to treat infectious diseases.Type: ApplicationFiled: April 22, 2014Publication date: November 6, 2014Inventors: Lisa Ann Morici, Saja Asakrah
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Publication number: 20140329817Abstract: This disclosure relates to antiviral compounds disclosed herein and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions. Typically, the pharmaceutical composition comprises a compound of formula I: Formula I, or salt, prodrug, or ester thereof wherein X, Y, and R1 and R10 to R13 are described herein.Type: ApplicationFiled: October 24, 2012Publication date: November 6, 2014Applicants: CHILDREN'S HEATLHCARE OF ATLANTA, INC., EMORY UNIVERSITYInventors: Richard K. Plemper, James P. Snyder, Aiming Sun
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Publication number: 20140329796Abstract: The present invention aims to provide a novel compound having a TRPA1 antagonist activity, and a medicament containing the compound. Moreover, the present invention aims to provide a TRPA1 antagonist and a medicament useful for the prophylaxis or treatment of diseases involving TRPA1. A medicament containing a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: July 16, 2014Publication date: November 6, 2014Applicant: Ajinomoto Co., Inc.Inventors: Tamotsu SUZUKI, Kaori Kobayashi, Sayaka Asari, Seiji Shiraishi, Tatsuya Okuzumi
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Patent number: 8877795Abstract: Disclosed herein are compounds and compositions thereof which find use in increasing stability of TTR tetramers reducing its tendency to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of TTR and thereby decreasing aggregate formation by TTR. Also disclosed herein are methods to screen for candidate compounds that increase stability of TTR. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PPIs of a target protein.Type: GrantFiled: May 5, 2011Date of Patent: November 4, 2014Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Isabella A. Graef, Mamoun Alhamadsheh
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Patent number: 8877754Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: August 17, 2011Date of Patent: November 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Gerald Juergen Roth, Martin Fleck, Heike Neubauer, Bernd Nosse
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Publication number: 20140323436Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein W is O or S; V is a direct bond or NR3; Q is or CR6aR6b, O, NR7, C?N—O—R7 or C(?O); Y is —C(R5)?N—O—(CR8aR8b)p—X—(CR9aR9b)q—SiR10aR10bR10c; or a phenyl ring substituted as defined in the disclosure; or Z; and R1, R2, R3, R4, R5, R6a, R6b, R7, R8a, R8b, R9a, R9b, R10a, R10b, R10c, Z, p and q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: July 8, 2014Publication date: October 30, 2014Inventors: Bruce Lawrence FINKELSTEIN, Andrew Edmund TAGGI, Jeffrey Keith LONG, Paula Louise SHARPE, Chi-Ping TSENG, Stephen Frederick MCCANN, Amy X DING, Steven Lewis SWANN, JR.
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Publication number: 20140323518Abstract: Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R1 to R9 have meanings as defined in the Specification, are useful as estrogen receptor ligands.Type: ApplicationFiled: August 2, 2012Publication date: October 30, 2014Inventors: Aiping Cheng, Neeraj Garg, Lars Krüger, Joakim Löfstedt, Eva Koch, Konrad Koehler, Lars Hagberg, Daniel Nöteberg
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Publication number: 20140323539Abstract: Subject matter of the present invention is an emulsifiable concentrate comprising a water-insoluble pesticide, dimethyl sulfoxide, benzyl alcohol, alkyl lactate and a diester of the formula (I) R1—O(O)C—R2—C(O))—R1??(I), where R1 is C1-C8-alkyl and R2 is C2-C10-alkanediyl or C2-C10-alkenediyl. A further subject matter is an emulsion obtainable by mixing water with the emulsifiable concentrate; a process for the preparation of the emulsifiable concentrate; and a method for controlling phytopathogenic fungi and/or undesired vegetation and/or undesired attack by insects or mites and/or for regulating the growth of plants, where the concentrate or the emulsion is allowed to act on the respective pests, their environment or on the crop plants to be protected from the respective pests, on the soil and/or on undesired plants and/or on the crop plants and/or their environment.Type: ApplicationFiled: November 21, 2012Publication date: October 30, 2014Applicant: BASF SEInventors: Cedric Dieleman, Winfried Mayer, Manuel Schmitt, Juergen Jakob, Siegfried Strathmann
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Publication number: 20140323537Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.Type: ApplicationFiled: March 14, 2014Publication date: October 30, 2014Applicant: EPIZYME, INC.Inventors: RICHARD CHESWORTH, LORNA HELEN MITCHELL, GIDEON SHAPIRO, PAULA ANN BORIACK-SJODIN, OSCAR MIGUEL MORADEI, LEI JIN, KENNETH W. DUNCAN
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Publication number: 20140323538Abstract: Compounds according to formula I: wherein Ar is a fused aryl group, R1 is selected from alkyl and aryl amides, CF3, and CH2OH, and R2 is selected from hydrogen, —C(?O)CH2NH2, and —C(?O)CH2CH2NH2 are described. The compounds are effective for inhibiting p21-activated kinases, and can be used for prevention and treatment of cancer.Type: ApplicationFiled: March 31, 2014Publication date: October 30, 2014Applicant: Ohio State Innovation FoundationInventors: Ching-Shih Chen, Matthew David Ringel, Motoyashi Saji, Yihui Ma
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Patent number: 8871679Abstract: Fungicidal mixtures, comprising as active components 1) at least one 1-methylpyrazol-4-ylcarboxanilide of the formula I where R1?C1-C4-alkyl or C1-C4-haloalkyl, R2=hydrogen or halogen, X=hydrogen or halogen, Q=direct bond, a cyclopropylene or an anellated bicyclo[2.2.Type: GrantFiled: July 2, 2009Date of Patent: October 28, 2014Assignee: BASF SEInventors: Markus Gewehr, Ulf Groeger, Egon Haden, Michael Vonend
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Patent number: 8871796Abstract: The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: October 5, 2010Date of Patent: October 28, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: William Colby Brown, Jason Brubaker, Christian Fischer, Richard W. Heidebrecht, John T. Hendrix, Elizabeth H. Kelley, Rachel N. MacCoss, Joey L. Methot, Thomas Miller, Karin M. Otte, Phieng Siliphaivanh, Thomas Reger, Peter D. Williams, Catherine M. Wiscount
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Patent number: 8871797Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the prophylaxis or treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders and the like.Type: GrantFiled: September 14, 2012Date of Patent: October 28, 2014Assignee: Arena Pharmaceuticals, Inc.Inventors: Bradley Teegarden, Honnappa Jayakumar, Hongmei Li, Sonja Strah-Pleynet, Peter I. Dosa
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Patent number: 8871792Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.Type: GrantFiled: June 6, 2013Date of Patent: October 28, 2014Assignee: Theravance Biopharma R&D IP, LLCInventors: Adam D. Hughes, Melissa Fleury
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Publication number: 20140315945Abstract: The present invention relates to azole compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: March 14, 2014Publication date: October 23, 2014Applicant: EPIZYME, INC.Inventors: John Emmerson Campbell, Kevin Wayne Kuntz
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Publication number: 20140315894Abstract: The invention provides methods of inhibiting the growth or metastasis of a cancer in a mammal by inhibiting a Ral GTPase in the mammal. The invention also provides small molecule inhibitors of Ral GTPases useful in the methods of the invention and pharmaceutical compositions containing the therapeutically effective compounds of the invention, and methods of using the same.Type: ApplicationFiled: December 21, 2012Publication date: October 23, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATEInventors: Dan Theodorescu, Michael Fitzpatrick Wempe, David Ross, Samy Meroueh, Martin A. Schwartz, Phillip Reigan
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Publication number: 20140315956Abstract: In one aspect, the invention relates to substituted 2-(1H-indol-3-yl)ethanol analogs and substituted 3,3a,8,8a-tetrahydro-2H-furo[2,3-b]indole analogs, derivatives thereof, and related compounds, which are useful as inhibitors of IL-6 mediated activation of the Jak2/STAT3 pathway; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a IL6 dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: July 29, 2012Publication date: October 23, 2014Applicants: NATIONWIDE CHILDREN'S HOSPITAL, OHIO STATE INNOVATION FOUNDATIONInventors: James Fuchs, Chenglong Li, Pui Kai Li, Jiayuh Lin
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Publication number: 20140315961Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.Type: ApplicationFiled: March 14, 2014Publication date: October 23, 2014Applicant: Epizyme, Inc.Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
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Publication number: 20140315889Abstract: The present invention relates to a novel hydroxamate derivatives, more specifically, to novel hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC), isomers thereof, pharmaceutically acceptable salts thereof, hydrates or solvates thereof, use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, treatment method using said composition, and a preparing method of novel hydroxamate derivatives. The novel selective hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC) compositions can be used for treatment of inflammatory disease, rheumatoid arthritis, or degenerative disease.Type: ApplicationFiled: October 26, 2012Publication date: October 23, 2014Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: Yuntae Kim, Changsik Lee, Hyun-mo Yang, Hojin Choi, Jaeki Min, Soyoung Kim, Dal-Hyun Kim, Nina Ha, Jung-Min Kim, Hyojin Lim, Eunhee Ko
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Publication number: 20140315904Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.Type: ApplicationFiled: March 14, 2014Publication date: October 23, 2014Applicant: Epizyme, Inc.Inventors: Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro
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Patent number: 8865751Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and the compositions in the treatment of various disease, conditions, or disorders. The invention also relates to processes for preparing compounds of the inventions.Type: GrantFiled: July 3, 2012Date of Patent: October 21, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Ronald Knegtel, Daniel Robinson, Philip Collier
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Publication number: 20140309200Abstract: The present invention comprises compounds and compositions thereof for enhanced drug delivery. Pro-drug and double pro-drug derivatives of corticosteroids non-steroid anti-inflammatory drugs (NSAIDs), and ruboxistaurin for delivery to the eye are provided. The compounds and compositions are useful for treating various ocular diseases, including ocular diseases effecting the posterior segments of the eye. In addition, the present invention is directed to particle in particle carrier formulations for sustained release of therapeutic agents.Type: ApplicationFiled: November 16, 2012Publication date: October 16, 2014Inventors: Uday B. Kompella, Sarath Yandrapu, Ashish Thakur
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Patent number: 8859537Abstract: This invention relates to the use of a ligand of the 5-HT4 receptor or of a pharmaceutically acceptable salt of this ligand and to a nucleic acid coding for a 5-HT4 receptor or of a functionally equivalent receptor for a drug for treating and/or preventing a pathology associated with an obsessional behavior such as anorexia, bulimia and the addiction to drugs of abuse or obesity. The invention also relates to a method for identifying a compound that is biologically active in the treatment and/or the prevention of a pathology associated with an obsessional conduct or obesity including: a) placing the 5-HT4 receptor or a functionally equivalent receptor in contact with this biologically active compound, and b) the determination of whether this biologically active compound is capable of modulating the basal activity of the 5-HT4 receptor or of a functionally equivalent receptor.Type: GrantFiled: April 29, 2005Date of Patent: October 14, 2014Assignee: Centre National de la Recherche Scientifique-CNRSInventor: Valerie Compan
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Patent number: 8859606Abstract: The present invention provides a compound, that is a 1-[(2-{[(alkyl or aryl)methyl]oxy}halo or haloalkyl substituted-phenyl)alkyl]-5-hydrocarbyl or substituted hydrocarbyl-1H-pyrazole carboxylic acid or alkylenylcarboxylic acid or a hydrocarbyl or substituted hydrocarbyl sulfonamide of said carboxylic acid or said alkylenylcarboxylic acid, provided however said compound is not a 3-carboxylic acid, a sulfonamide thereof, or a 3-methylenylcarboxylic acid. The compound may be represented by the following formula Wherein R1, R2, R3, R4, R5, R6, X, W, X and Y are as defined in the specification. The compounds may be administered to treat DP1, FP, EP1, TP and/or EP4 receptor mediated diseases or conditions.Type: GrantFiled: January 21, 2013Date of Patent: October 14, 2014Assignee: Allergan, Inc.Inventors: David F. Woodward, William R. Carling, Jose L. Martos, Jenny W. Wang, Jussi J. Kangasmetsa
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Publication number: 20140303186Abstract: The present application relates to nitrogen-containing fused ring compounds shown by general formula (I), a pharmaceutically acceptable salt thereof and a stereoisomer thereof as CRTH2 antagonist, wherein X1, X2, X3, X4, X5, W, X, Y, L1, L2, L3, A, B are as defined in the description; the present application further relates to a method for preparing the compounds, a pharmaceutical formulation and a pharmaceutical composition comprising the compounds, a use of the compounds for the manufacture of a medicament for the treatment and/or prevention of diseases related to activity of CRTH2.Type: ApplicationFiled: November 16, 2012Publication date: October 9, 2014Inventors: Yan Zhang, Min Zhang, Hoyin Lo
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Publication number: 20140303223Abstract: The invention provides methods for muscle repair or regeneration comprising administering therapeutically effective amounts of RAR agonists or stem cells that are pretreated with contact with a RAR agonist to a subject at a site of muscle damage. Additionally, the invention provides compositions comprising RAR agonist treated stem cells and methods of use of said cells for muscle repair or regeneration. In one embodiment, the stem cells are mesenchymal stem cells. In one embodiment, the RAR agonist is an RAR? agonist. In one embodiment, administration of the RAR agonist is begun during a period of increased endogenous retinoid signaling in the subject resulting from incurrence of the damaged muscle tissue.Type: ApplicationFiled: June 18, 2014Publication date: October 9, 2014Inventors: Masahiro IWAMOTO, Maurizio PACIFICI
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Publication number: 20140303109Abstract: Water-soluble fluorinated analogs of natural curcumin, and particularly difluoro Knoevenagel condensates and Schiff bases, along with their corresponding copper (H) complexes have improved bioavailablity over curcumin. The fluorine-substituted analogs of curcumin are useful as chemopreventive and/or therapeutic agents against cancers and/or against the development of drug-resistant cancer. A preferred compound is (IE,6E)-1,7-bis(4-hydroxy-3-methoxyphenyl)hepta-1,6-diene{4(3,4 difluorobenzaldehyde)}-3,5-dione.Type: ApplicationFiled: March 25, 2011Publication date: October 9, 2014Inventors: Fazlul H. Sarkar, Subhash Padhye
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Publication number: 20140303175Abstract: The present invention relates to 2-(substituted sulphur, sulphone or sulphoxide)-3-(substituted phenyl)propionic acid derivatives, 2-(substituted oxygen)-3-(substituted phenyl)propionic acid derivatives, benzoic acid derivatives, and derivatives of 2-methyl-2-(phenoxy or phenylthio)propanoic acid and 2-(methyl or ethyl)-2-(phenoxy or phenylthio)butanoic acid, to processes for preparing such compounds, to their use in the treatment of inflammatory conditions, and to pharmaceutical compositions containing them.Type: ApplicationFiled: June 11, 2014Publication date: October 9, 2014Inventors: Anders Broo, Johan Gottfries, Michael Kossenjans, Li Lanna, Eva-Lotte Lindstedt-Alstermark, Kristina A. Nilsson, Bengt Ohlsson, Maria Thorstensson, Maria Boije
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Patent number: 8853205Abstract: Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or CB2 cannabinoid receptors. Aspects disclose hetero pyrrole analogs acting as CB1 and/or CB 1 receptor antagonists, having selectivity for the CB 1 or CB2 receptor, acting as neutral antagonists, acting preferentially on CB 1 receptors located in the peripheral nervous system, and/or acting as nitric oxide donors. Pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect are also disclosed.Type: GrantFiled: February 19, 2009Date of Patent: October 7, 2014Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Venkata Kiran Vemuri
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Patent number: 8853196Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.Type: GrantFiled: August 3, 2012Date of Patent: October 7, 2014Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Wilhelm Amberg, Udo Lange, Frauke Pohlki
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Patent number: 8853207Abstract: The present invention relates to a compound of formula (I): or hydrates, solvates, prodrugs, or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, ring A, R3 and R4 are as defined in the detailed description and claims. The compound of formula (I) are receptor tyrosine kinase (RTK) inhibitors and have efficacy for the treatment, prevention, or amelioration of RTK-related diseases.Type: GrantFiled: April 12, 2012Date of Patent: October 7, 2014Assignee: Development Center for BiotechnologyInventors: Chu-Bin Liao, Chao-Cheng Chiang, Huei-Ru Yang, Yuan-Chun Liao, Paonien Chen
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Patent number: 8853212Abstract: The present invention is directed to novel substituted aminotetrahydrothiopyrans and derivatives thereof of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 dipeptidyl peptidase-IV enzyme is involved.Type: GrantFiled: February 17, 2011Date of Patent: October 7, 2014Assignee: Merck Sharp & Dohme CorpInventors: Robert R. Wilkening, James M. Apgar, Tesfaye Biftu, Danqing Feng, Xiaoxia Qian, Lan Wei
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Publication number: 20140296292Abstract: Some embodiments include compositions and methods of using or identifying compounds that modulate the activity of the granulocyte colony-stimulating factor receptor (GCFR). Some embodiments include use of compounds to treat certain disorders, such as hematopoietic or neurological disorders.Type: ApplicationFiled: November 12, 2012Publication date: October 2, 2014Inventors: Lin Zhi, Keith Marschke, Virginia H. Grant, Steven L. Roach, Yixing Shen, Jason C. Pickens, Bijan Pedram, C. Arjan van Oeveren, Lino J. Valdez, Andrew R. Hudson
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Publication number: 20140296315Abstract: A compound represented by the following formula: wherein n is 1 or 2, or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof.Type: ApplicationFiled: March 14, 2014Publication date: October 2, 2014Applicant: JAPAN TOBACCO INC.Inventors: Takahisa Motomura, Gakujun Shomi
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Publication number: 20140296316Abstract: A compound represented by the formula (J): or a crystal thereof, or a compound represented by the formula (Q): or a crystal thereof.Type: ApplicationFiled: March 14, 2014Publication date: October 2, 2014Applicant: JAPAN TOBACCO INC.Inventor: Takahisa Motomura
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Publication number: 20140296283Abstract: The present invention relates to azole bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.Type: ApplicationFiled: March 14, 2014Publication date: October 2, 2014Applicant: EPIZYME, INC.Inventors: John Emmerson Campbell, Kevin Wayne Kuntz