The Additional Five-membered Hetero Ring Consists Of Three Ring Carbons, And Of Nitrogen And Chalcogen In Adjacent Ring Positions (e.g., Isoxazolyl, Isothiazolyl, Etc.) Patents (Class 514/254.04)
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Publication number: 20130267503Abstract: The present invention relates to an injectable, pharmaceutical composition comprising a C1-6 alkyl ester of a C10-20 fatty acid. In an embodiment, the fatty acid is ethyl oleate, isopropyl oleate, ethyl myristate, or isopropyl myristate. These compositions are useful for the delivery of anti-psychotic drugs.Type: ApplicationFiled: March 13, 2013Publication date: October 10, 2013Applicant: ALKERMES PHARMA IRELAND LIMITEDInventors: Jason M. PERRY, Magali B. HICKEY, Julius F. REMENAR, Jennifer VANDIVER
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Publication number: 20130252953Abstract: The present invention relates to novel TMPK inhibitor compositions and their methods of use. In particular, it relates to novel TMPK inhibitor compositions and therapeutics that lead to dUTP-mediated DNA repair in tumor cells and acts as a novel chemosensitizer, which are useful in methods for treating or preventing cancers.Type: ApplicationFiled: November 29, 2011Publication date: September 26, 2013Inventors: Zee-Fen Chang, Jim-Min Fang, Chun-Mei Hu, Ming-Tyng Yeh
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Publication number: 20130245004Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.Type: ApplicationFiled: May 9, 2013Publication date: September 19, 2013Applicant: Synchroneuron Inc.Inventors: Barry S. Fogel, William D. Kerns, Kei-Lai Fong
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Publication number: 20130225586Abstract: The present invention provides a compound having Formula I or II: wherein B, R, X, Ar, and Y are defined herein, pharmaceutically acceptable salts thereof and pharmaceutically acceptable prodrugs thereof. The present invention also provides methods of making and using the compound.Type: ApplicationFiled: September 25, 2012Publication date: August 29, 2013Applicant: CPSI STOCKHOLDER TRUSTInventor: CPSI Stockholder Trust
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Publication number: 20130225600Abstract: The present invention relates to compounds of Formula (I) along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I).Type: ApplicationFiled: October 31, 2011Publication date: August 29, 2013Applicant: LUPIN LIMITEDInventors: Nageswara Rao Irlapati, Gokul Keruji Deshmukh, Vijay Pandurang Karche, Santosh Madhukar Jachak, Neelima Sinha, Venkata P. Palle, Rajender Kumar Kamboj
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Publication number: 20130217687Abstract: Provided herein are arylsulfonamides that are useful for modulating CCR3 activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a CCR3-mediated disorder, disease, or condition.Type: ApplicationFiled: March 15, 2013Publication date: August 22, 2013Applicant: Axikin Pharmaceuticals, Inc.Inventors: Tai Wei LY, Jared Andrew FORRESTER
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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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Patent number: 8513257Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: December 30, 2011Date of Patent: August 20, 2013Assignee: Cytokinetics, IncorporatedInventors: Bradley Paul Morgan, Alex Muci, Pu-Ping Lu, Erica Anne Kraynack, Todd Tochimoto, David J. Morgans, Jr.
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Patent number: 8507480Abstract: Isoxazoles of formula (A) or (B) are inhibitors of HSP90 activity, and useful for treatment of, for example cancers: wherein R1, is a group of formula (IA): —Ar1-(Alk1)p-(Z)r-(Alk2)s-Q, wherein in any compatible combination Ar1 is an optionally substituted aryl or heteroaryl radical, Alk1 and Alk2 are optionally substituted divalent C1-C6 alkylene or C2-C6 alkenylene radicals, p, r and s are independently 0 or 1, Z is -0-, —S—, —(C?O)—, —(C?S)—, —SO.sub.Type: GrantFiled: February 19, 2010Date of Patent: August 13, 2013Assignees: Vernalis (R&D) Limited, Cancer Research Technology Limited, The Institute of Cancer ResearchInventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Publication number: 20130203766Abstract: The invention relates to new pharmaceutical compositions for the treatment of sexual disorders and methods for the preparation thereof. In a preferred embodiment, the instant invention is directed to pharmaceutical combinations comprising flibanserin as one active ingredient in combination with at least one additional active ingredient for the treatment of sexual disorders and methods for the preparation thereof.Type: ApplicationFiled: October 18, 2012Publication date: August 8, 2013Applicant: SPROUT PHARMACEUTICALS, INC.Inventor: Sprout Pharmaceuticals, Inc.
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Patent number: 8501781Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I), in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling phytopathogenic harmful fungi and also processes for preparing compounds of the formula (I).Type: GrantFiled: October 27, 2010Date of Patent: August 6, 2013Assignee: Bayer Cropscience AGInventors: Pierre Cristau, Nicola Rahn, Tomoki Tsuchiya, Joachim Kluth, Pierre Wasnaire, Sebastian Hoffmann, Jürgen Benting, Ulrike Wachendorff-Neumann, Thomas Seitz
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Publication number: 20130196996Abstract: One embodiment provides a method, comprising treating or preventing at least one disease selected from the group consisting of bladder cancer, weight loss accompanying bladder cancer, bone pain accompanying bladder cancer, bladder cancer carcinoma in-situ (CIS), TA stage bladder cancer, T1 stage bladder cancer, T2 stage bladder cancer, T3 stage bladder cancer, T4 stage bladder cancer, lymph node metastasis therefrom, solid organ metastasis therefrom, bony metastasis therefrom, cachexia/anorexia associated with bladder cancer, generalized wasting syndrome associated with bladder cancer, or a combination thereof, by administering to a subject in need thereof one or more compounds described herein, prodrug thereof, salt thereof, or a combination thereof.Type: ApplicationFiled: January 19, 2011Publication date: August 1, 2013Applicant: CPSI STOCKHOLDER TRUSTInventors: John Arthur Taylor, III, Thais Sielecki-Dzurdz
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Publication number: 20130178481Abstract: The present invention is directed to therapeutic agents which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction.Type: ApplicationFiled: March 4, 2013Publication date: July 11, 2013Inventors: Mark T Bilodeau, Kausik K. Nanda, B. Wesley Trotter
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Publication number: 20130172363Abstract: Benzenesulfonamide compounds having a structure of formula (I) are described. Also described, are methods for synthesizing the compounds and to the use thereof in pharmaceutical compositions for human or veterinary medicine and in cosmetic compositions.Type: ApplicationFiled: February 22, 2013Publication date: July 4, 2013Applicant: GALDERMA RESEARCH & DEVELOPMENTInventor: Galderma Research & Development
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Publication number: 20130172365Abstract: Arylsulphonamide derivatives of formula (I) and pharmaceutically acceptable salts thereof. The compounds may be useful for the treatment and/or prevention of disorders of the central nervous system.Type: ApplicationFiled: September 16, 2011Publication date: July 4, 2013Applicant: ADAMED SP. Z.O.O.Inventors: Marcin Kolaczkowski, Piotr Kowalski, Jolanta Jaskowska, Monika Marcinkowska, Katarzyna Mitka, Adam Bucki, Anna Wesolowska, Maciej Pawlowski
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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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Patent number: 8461159Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: GrantFiled: November 24, 2009Date of Patent: June 11, 2013Assignee: Jannsen Pharmaceutica BVInventors: J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Seierstad
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Publication number: 20130143870Abstract: 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: November 30, 2012Publication date: June 6, 2013Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF, Bernd WELLENZOHN
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Publication number: 20130143885Abstract: The present invention relates to compounds and methods for inducing neuronal differentiation in normal neural stem cells and brain cancer stem cells. The methods may take place in vitro, such as in isolates from the adult mammalian brain, or in vivo. Compounds and methods described herein may find use in the treatment of neurodegenerative and psychiatric diseases, the repair and regeneration of the nervous system, and in treatment of neurologic malignancy.Type: ApplicationFiled: June 4, 2012Publication date: June 6, 2013Applicant: The Board of Regents of the University of Texas SystemInventors: Jay Schneider, Jenny Hsieh, Douglas Frantz, Steven L. McKnight, Joseph M. Ready
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Publication number: 20130143867Abstract: Embodiments disclosed herein generally relate to acamprosate formulations, methods of use of the formulations, to methods of using the formulations in combination with at least one other medication, and to combination products and compositions comprising the formulations and at least one other medication, such as neuroleptic (antipsychotic) and/or antidepressant drugs.Type: ApplicationFiled: January 18, 2013Publication date: June 6, 2013Applicant: SYCHRONEURON INC.Inventor: SYCHRONEURON INC.
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Patent number: 8450317Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R5, A, B, D and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: April 27, 2010Date of Patent: May 28, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Jennifer A. Kowalski, Daniel Richard Marshall, Anthony S. Prokopowicz, III, Sabine Schlyer, Robert Sibley, Ronald John Sorcek, Di Wu, Frank Wu, Erick Richard Roush Young
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Patent number: 8450310Abstract: Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.Type: GrantFiled: June 18, 2012Date of Patent: May 28, 2013Assignees: Vernalis (R&D) Limited, Cancer Research Technology Ltd., The Institute of Cancer ResearchInventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Publication number: 20130131063Abstract: The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer.Type: ApplicationFiled: May 15, 2012Publication date: May 23, 2013Applicant: Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. Castro, Kristopher M. Depew, Michael J. Grogan, Charles W. Johannes, Edward B. Holson, Brian T. Hopkins, Gregg F. Keaney, Nii O. Koney, Tao Liu, David A. Mann, Marta Nevalainen, Stephane Peluso, Lawrence Blas Perez, Daniel A. Snyder, Thomas T. Tibbitts
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Publication number: 20130123261Abstract: Methods for treating diabetes in a subject, reducing the blood glucose level of a subject suffering from diabetes, and reducing or preventing an increase in the level of resistin in a subject, comprising administering to said subject a compound having the following formula: wherein R1, R2, R3, R4, R5, X, Y, and R16 are described herein; or salt thereof, prodrug thereof, or combination thereof, optionally in contact with one or more pharmaceutical carrier.Type: ApplicationFiled: November 26, 2010Publication date: May 16, 2013Applicant: CPSI STOCKHOLDER TRUSTInventors: Abhay Satoskar, Thais Sieleck-Dzurdz
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Publication number: 20130108701Abstract: The present invention relates to a solid dosage form comprising an antipsychotic, particularly ziprasidone. The present invention also relates to a process for preparation of solid dosage form comprising ziprasidone.Type: ApplicationFiled: May 23, 2011Publication date: May 2, 2013Inventors: Krishna Murthy Bhavanasi, Nagaprasad Vishnubhotla, Sivakumaran Meenakshisunderam
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Publication number: 20130096089Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.Type: ApplicationFiled: September 7, 2012Publication date: April 18, 2013Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
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Publication number: 20130090329Abstract: Methods and compositions relate to genetic markers of psychotic disorders, e.g., schizophrenia (SZ), are provided. For example, in certain aspects methods for determinations of a OPRP genetic signature are described. Furthermore, the invention provides methods and compositions involving treatment of psychotic disorders using the genetic signature.Type: ApplicationFiled: October 7, 2011Publication date: April 11, 2013Applicant: SUREGENE, LLCInventors: Timothy L. Ramsey, Bharat Mehrotra, Mark D. Brennan
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Patent number: 8410111Abstract: The present invention is directed to therapeutic agents which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction.Type: GrantFiled: August 21, 2012Date of Patent: April 2, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Kausik K. Nanda, B. Wesley Trotter
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Patent number: 8410268Abstract: The present invention relates to a process for preparing Ziprasidone of formula I, or a pharmaceutically acceptable salt or a solvate or a hydrate thereof; comprising the steps of reacting 1-(1,2-benzisothiazol-3-yl) piperazine of formula II or its salt: with 5-(2-haloethyl)-6-chloro-oxindole of formula III: wherein X is leaving groups like fluoro, chloro, bromo, iodo or sulphonyl; in the presence of a dispersing agent and a base in a solvent to form ziprasidone of formula I; and optionally converting the ziprasidone formed into a pharmaceutically acceptable acid addition salts of ziprasidone; or a solvate or a hydrate thereof.Type: GrantFiled: March 9, 2009Date of Patent: April 2, 2013Assignee: Alkem Laboratories LimitedInventors: Shashiprabha, Kanakamajalu Shridhara, Debkiron Mukherjee, Padmashree Badraje, K Sundarraja Rao, Kuppuswamy Nagarajan
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Publication number: 20130079340Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings, having histamine H3 antagonistic activity can be used in pharmaceutical compositions.Type: ApplicationFiled: October 25, 2012Publication date: March 28, 2013Inventors: Florencio Zaragoza Dorwald, Rolf Hohlweg, Inge Thoger Christensen, Jane Marie Lundbeck, Knud Erik Andersen
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Publication number: 20130072497Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.Type: ApplicationFiled: November 14, 2012Publication date: March 21, 2013Applicant: Dow AgroSciences LLCInventor: Dow AgroSciences LLC
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Publication number: 20130072490Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: September 29, 2010Publication date: March 21, 2013Applicant: Amira Pharmaceuticals INC.Inventors: Ryan Clark, Brian Andrew Stearns, Jill Melissa Scott, Heather Renee Coate, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie Arruda, Nicholas Simon Stock, Yen Pham Truong, David Nathan Zalatan
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Publication number: 20130053361Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.Type: ApplicationFiled: July 5, 2012Publication date: February 28, 2013Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
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Publication number: 20130052281Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: August 22, 2012Publication date: February 28, 2013Applicant: Takeda Pharmaceutical Company LimitedInventors: William FARNABY, Charlotte FIELDHOUSE, Catrina KERR, Natasha KINSELLA, David LIVERMORE, Kevin MERCHANT, David MILLER, Katherine HAZEL
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Publication number: 20130053372Abstract: The invention relates to compounds of formula (I), useful for treating disorders mediated by the 5-hydroxytryptamine (serotonin) receptor IB (5-HT1B), e.g. vascular disorders, cancer and CNS disorders. The invention also provides methods of treating such disorders, and compounds and compositions etc. for their treatment.Type: ApplicationFiled: February 15, 2011Publication date: February 28, 2013Inventors: Prashant Bhimrao Kapadnis, Robert Glen, Robin Hiley, James Bell, David Spring
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Publication number: 20130053341Abstract: Methods of treating disorders using compounds that modulate striatal-enriched tyrosine phosphatase (STEP) are de-scribed herein. Exemplary disorders include schizophrenia and cognitive deficit.Type: ApplicationFiled: December 30, 2010Publication date: February 28, 2013Inventors: Masaki Suzuki, Kazumi Kondo, Muneaki Kurimura, Krishna Reddy Valluru, Akira Takahashi, Takeshi Kuroda, Haruka Takahashi, Tae Fukushima, Shin Miyamura, Indranath Ghosh, Abhishek Dogra, Geraldine Harriman, Amy Elder, Satoshi Shimizu, Kevin J. Hodgetts, Jason S. Newcom
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Patent number: 8383616Abstract: The present invention relates to formula I compounds having antitumoural activities through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical compositions containing such compounds.Type: GrantFiled: June 30, 2009Date of Patent: February 26, 2013Assignee: Sigma-Tau Industrie Farmaceutiche Riunite SpAInventors: Giuseppe Giannini, Walter Cabri, Daniele Simoni, Riccardo Baruchello, Claudio Pisano, Gabriella Singrossi, Silvia Carminati, Giuseppe Paolo Carminati
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Publication number: 20130040948Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceutical agents.Type: ApplicationFiled: February 10, 2012Publication date: February 14, 2013Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20130040930Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: April 27, 2011Publication date: February 14, 2013Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
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Publication number: 20130029978Abstract: There is a need for FAAH inhibitors capable of oral administration and having excellent efficacy, particularly agents for the prevention and treatment of pain. Disclosed are novel arylurea compounds represented by formula (I), salts or solvates thereof, and pharmaceutical compositions comprising the same as an active ingredient. The pharmaceutical composition is used primarily for FAAH inhibitors, or agents for prevention and treatment of pain.Type: ApplicationFiled: December 24, 2010Publication date: January 31, 2013Inventors: Tomoyuki Kamino, Yoshitaka Maeda
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Patent number: 8362004Abstract: A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with —N, —O, or —S adjacent to the —Ar substituent or adjacent to the point of attachment for the —Ar substituent; Ar is aryl or heteroaryl; R is —CH3, —CH2F, or —CH?CH2; W is —NO2, —Cl, —Br, —CHO, —CH?CH2, or —CN; X is —Cl, —CH3, or —CN; Y is —CH or —N; and Z is C1-C6 alkyl, C3-C6 cycloalkyl, substituted aryl, substituted heteroaryl, OR1, or NHR1, wherein R1 is selected from the group of H, aryl, heteroaryl, C1-C6 alkyl and C3-C6 cycloalkyl. This compound is useful in compositions for the prevention and treatment of influenza virus.Type: GrantFiled: September 6, 2011Date of Patent: January 29, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Christopher W. Cianci, Samuel Gerritz, Guo Li, Bradley C. Pearce, Annapurna Pendri, Shuhao Shi, Weixu Zhai, Shirong Zhu
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Publication number: 20130018056Abstract: The invention relates to a medicament or a method for treating mental disorders, in detail, ADHD comprising lurasidone, or a combination of lurasidone and a D4 receptor agonist.Type: ApplicationFiled: July 20, 2012Publication date: January 17, 2013Inventors: Kazuhito IKEDA, Takeo ISHIYAMA
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Publication number: 20120328691Abstract: The present invention relates to novel Anilinopiperazine Derivatives of Formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, cancer, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.Type: ApplicationFiled: October 29, 2007Publication date: December 27, 2012Inventors: Gerald W. Shipps, JR., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards, Hongbo Zeng, Binyuan Sun, Panduranga Adulla Reddy, Tzu T. Wong, Praveen K. Tadikonda, M. Arshad Siddiqui, Marc A. Labroli, Cory Poker, Timothy J. Guzi
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Publication number: 20120328679Abstract: Spray dried solid dispersions comprising a sparingly soluble drug and hydroxypropylmethylcellulose acetate succinate (HPMCAS) provide increased aqueous solubility and/or bioavailability in a use environment.Type: ApplicationFiled: September 7, 2012Publication date: December 27, 2012Inventors: William J. Curatolo, Scott M. Herbig, James A. S. Nightingale
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Publication number: 20120322805Abstract: A solid composition of a low-solubility drug and a concentration-enhancing polymer has a portion of the drug in a semi-ordered state.Type: ApplicationFiled: August 23, 2012Publication date: December 20, 2012Applicant: BEND RESEARCH, INC.Inventors: Walter C. Babcock, William B. Caldwell, Marshall D. Crew, Dwayne T. Friesen, Ravi M. Shanker, Daniel T. Smithey
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Publication number: 20120316181Abstract: The present invention is directed to therapeutic agents which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction.Type: ApplicationFiled: August 21, 2012Publication date: December 13, 2012Inventors: Mark T. Bilodeau, Kausik K. Nanda, B. Wesley Trotter
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Publication number: 20120316124Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: February 17, 2011Publication date: December 13, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
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Patent number: 8329702Abstract: The present invention relates to compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: November 8, 2010Date of Patent: December 11, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Wilson, Andreas Termin, Lev T. D. Fanning, Paul Krenitsky, Pramod Joshi
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Publication number: 20120309714Abstract: This invention is directed to compounds, which are PDE10A enzyme inhibitors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention also provides a method of treating a subject suffering from a drug addiction comprising administering to the subject a therapeutically effective amount of a compound of formula I. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I.Type: ApplicationFiled: December 15, 2010Publication date: December 6, 2012Applicant: H. Lundbeck A/SInventors: Ask Püschl, Jacob Nielsen, Jan Kehler, John Paul Kilburn, Mauro Marigo, Morten Langgård
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Patent number: 8314091Abstract: The present invention relates to N-benzyl,N?-arylcarbonylpiperazine derivatives having the general formula I to pharmaceutical compositions comprising the same, and to the use of a these N-benzyl,N?-arylcarbonylpiperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholesterol and bile acids transport and metabolism.Type: GrantFiled: August 19, 2008Date of Patent: November 20, 2012Assignees: MSD OSS B.V., Pharmacopeia, Inc.Inventors: Koc-Kan Ho, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer, Andrew John Cooke, Andrew Stanley Edwards, David Jonathan Bennett