The Shared Ring Nitrogen Is Bonded Directly To A Ring Nitrogen Of The Second Ring Of The Bicyclo Ring System (e.g., Pyrazolo[1,5-a]pyrimidine, Etc.) Patents (Class 514/259.3)
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Patent number: 8404694Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-5 and 7-8, D?, L1, L2, R1, R3, R6-8, n and o are defined herein, and synthetic intermediates, which are capable of modulating the activity of Aurora kinase proteins and, thereby, influencing various disease states and conditions related to the activities of Aurora kinases. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.Type: GrantFiled: March 19, 2009Date of Patent: March 26, 2013Assignee: Amgen Inc.Inventors: Ryan White, Jason Brooks Human
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Publication number: 20130072494Abstract: The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: or a salt or solvate thereof, wherein ring A, Ca, Cb, Z, R5, W and Cy are defined herein. The disclosure further provides pharmaceutical compositions including the compounds of the present disclosure and methods of making and using the compounds and compositions of the present disclosure, e.g., in the treatment and prevention of various disorders, such as Alzheimer's disease.Type: ApplicationFiled: September 14, 2012Publication date: March 21, 2013Inventors: Hing L. SHAM, Roy K. Hom, Andrei W. Konradi, Gary D. Probst, Simeon Bowers, Anh Truong, R. Jeffrey Neitz, Jennifer Sealy, Gergely Toth
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Publication number: 20130065901Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: November 5, 2012Publication date: March 14, 2013Applicant: ARRAY BIOPHARMA INC.Inventor: Array BioPharma Inc.
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Publication number: 20130040932Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: September 24, 2012Publication date: February 14, 2013Applicants: Neuromed Pharmaceuticals Ltd., Merck Sharp & Dohme Corp.Inventors: Merck Sharp & Dohme Corp., Neuromed Pharmaceuticals Ltd.
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Patent number: 8372851Abstract: A compound according to Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R6, R7 and Z are as defined in the specification; pharmaceutical compositions thereof; and methods of use thereof.Type: GrantFiled: October 23, 2006Date of Patent: February 12, 2013Assignee: Exelixis, Inc.Inventors: Kenneth D. Rice, Joerg Bussenius, Simona Costanzo, Abigail R. Kennedy, Angie Inyoung Kim, Jean-Claire Limun Manalo, Csaba J. Peto
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Publication number: 20130035324Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: ApplicationFiled: August 17, 2010Publication date: February 7, 2013Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Simon Fraser Campbell
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Patent number: 8367681Abstract: The invention provides compounds of general formula (I) that inhibit selected kinases (Pim and/or CK2 kinases) and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain infections and immunological disorders.Type: GrantFiled: May 20, 2010Date of Patent: February 5, 2013Assignee: Cylene Pharmaceuticals, Inc.Inventors: Mustapha Haddach, Joe Tran
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Publication number: 20130029982Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: July 18, 2012Publication date: January 31, 2013Applicants: INTELLIKINE, LLC, INFINITY PHARMACEUTICALS, INC.Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Publication number: 20130022676Abstract: In one aspect, the present invention is concerned with a treatment where it is desired that an active agent is designed to be released in a pulse at a time point some time after administration of the active agent. The present invention is particularly suited to administering an agent which may be released whilst a subject is sleeping. As well as treating certain conditions by a particular regime, the invention also provides novel formulations for a delayed, followed by a pulsed release of drug.Type: ApplicationFiled: March 4, 2011Publication date: January 24, 2013Applicant: UNIVERSITY OF STRATHCLYDEInventors: Alexander Mullen, Howard Stevens, Sarah Eccleston
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Publication number: 20130023412Abstract: Fungicidal mixtures based on azolopyrimidinylamines.Type: ApplicationFiled: March 23, 2011Publication date: January 24, 2013Applicant: BASF SEInventors: Markus Gewehr, Jordi Tormo I Blasco, Egon Haden
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Publication number: 20130005655Abstract: A composition comprising doxepin, or a pharmaceutically acceptable salt, or prodrug thereof, and a compound that enhances sleep onset, sleep maintenance or reduces early morning awakenings. These compositions are useful for treating multiple manifestations of insomnia.Type: ApplicationFiled: September 12, 2012Publication date: January 3, 2013Applicant: Somaxon Pharmaceuticals, Inc.Inventors: Philip Jochelson, Robert Mansbach, Michael Skinner, Neil B. Kavey
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Patent number: 8338436Abstract: The present invention relates to an amorphous form of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide, methods for its preparation, its use as a therapeutically active agent and pharmaceutical compositions comprising the novel form.Type: GrantFiled: November 7, 2007Date of Patent: December 25, 2012Assignee: Ferrer International, S.A.Inventors: Luis Anglada, Albert Palomer, Antonio Guglietta
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Publication number: 20120322791Abstract: The present invention provides Pyrazolopyrimidine Compounds of Formula (I): wherein L, T, Z, U, V, W, R3, R6, R7, R8, and m are as defined herein, and pharmaceutically acceptable salts of such Pyrazolopyrimidine Compounds. The Pyrazolopyrimidine Compounds are useful in the treatment of cancer and other diseases or disorders wherein mTOR is deregulated.Type: ApplicationFiled: January 18, 2011Publication date: December 20, 2012Inventors: M. Arshad Siddiqui, Yang Nan, Mehul F. Patel, Panduranga Adulla P. Reddy, Umar Faruk Mansoor, Zhaoyang Meng, Lalanthi Dilrukshi Vitharana, Lianyun Zhao, Amit K. Mandal, Duan Liu, Shuyi Tang, Andrew McRiner, David B. Belanger, Patrick J. Curran, Chaoyang Dai, Angie R. Angeles, Liping Yang, Matthew Hersh Daniels
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Publication number: 20120316161Abstract: The present invention relates to compounds of formula (A) as defined herein having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.Type: ApplicationFiled: December 20, 2010Publication date: December 13, 2012Applicant: KATHOLIEKE UNIVERSITEIT LEUVENInventors: Gunter Carlens, Patrick Chaltin, Frauke Christ, Zeger Debyser, Arnaud Marchand, Damien Marchand, Arnout Voet, Marc De Maeyer
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Publication number: 20120309772Abstract: The present disclosure describes inhibitors of fatty acid uptake and methods of using such inhibitors. Specifically, the present disclosure describes inhibitors with specificity for FATP2.Type: ApplicationFiled: August 10, 2012Publication date: December 6, 2012Inventors: Concetta DiRusso, Paul Black
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Publication number: 20120309754Abstract: The present invention relates to a compound represented by formula [I]: wherein: R1 is hydrogen, halogen, lower alkyl or cyano; Ring A is an optionally substituted heterocyclic group; Ring B is an optionally substituted 3 to 6-membered monocyclic group; and Y is optionally substituted amino, optionally substituted cyclic amino, optionally substituted aliphatic 3 to 6-membered monocyclyloxy, optionally substituted lower alkyl or optionally substituted lower alkyl-O—, or a pharmaceutically acceptable salt thereof, and to their use as PDE10 inhibitor.Type: ApplicationFiled: February 25, 2011Publication date: December 6, 2012Inventors: Eiji Kawanishi, Mitsuya Hongu, Yoshihito Tanaka
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Publication number: 20120302585Abstract: The present disclosure describes inhibitors of fatty acid uptake and methods of using such inhibitors. Specifically, the present disclosure describes inhibitors with specificity for FATP2.Type: ApplicationFiled: August 10, 2012Publication date: November 29, 2012Inventors: CONCETTA DIRUSSO, PAUL BLACK
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Publication number: 20120295896Abstract: The present invention relates to compounds of formula (I) and (IA): and pharmaceutically acceptable salts thereof, wherein R1-R5 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: ApplicationFiled: September 20, 2011Publication date: November 22, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, Jonathon Alan DINES, John D. HUBER, Weimin W. LIU, Pui Leng LOKE, Tina Marie MORWICK, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
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Patent number: 8314098Abstract: The present invention has searched for a variety of compounds which show IL-12/IL-23 production-inhibitory activities and herein provides a pharmaceutical composition and an agent for preventing or treating IL-12/IL-23 excess production-related diseases, which comprise the compound.Type: GrantFiled: June 27, 2011Date of Patent: November 20, 2012Assignee: Ajinomoto Co., Inc.Inventors: Takashi Yamamoto, Ayatoshi Andou, Nobuhiko Hayakawa, Masatsugu Noguchi, Kanna Kuribayashi, Agung Eviryanti, Ryohei Yokoyama, Shunsuke Fukuda, Toshihiko Sugiura, Shunsuke Kageyama, Yoichiro Shima, Misato Noguchi
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Patent number: 8309559Abstract: The present invention relates to novel substituted 2-amino-3-(arylsulfonyl)pyrazolo[1,5-a]pyrimidines of general formula 1, to serotonin 5-HT6 receptor antagonists, to novel drug substances and pharmaceutical compositions, to medicaments, methods for preparation thereof, and to methods for prophylaxis and treatment of various CNS diseases, pathogenesis of which is associated with disturbance of monoaminergic signaling pathways, more specifically over- or hypo-activation of serotonin 5-HT6 receptors. Ar represents optionally substituted aryl or optionally substituted heterocyclyl; R1 and R3 independently of each other represent C1-C3 alkyl or aryl; R2 represents hydrogen or C1-C3 alkyl; R41, and R42 independently of each other represent hydrogen, optionally substituted C1-C3 alkyl or optionally substituted phenyl, or R41, and R42 together with nitrogen atom they are attached to form optionally substituted heterocyclyl.Type: GrantFiled: January 23, 2009Date of Patent: November 13, 2012Inventors: Nikolay Filippovich Savchuk, Alexander Vasilievich Ivashchenko
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Publication number: 20120283274Abstract: The present invention relates to novel co-crystals of pyrazolopyrimidines and a co-crystal former, wherein the co-crystal former is an organic carboxylic acid, preferably selected from the group of gentisic acid, succinic acid and xinafoic acid.Type: ApplicationFiled: November 24, 2010Publication date: November 8, 2012Inventors: Patrick Plitt, Bernhard Hauptmeier, Peter Boderke
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Publication number: 20120277224Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: ApplicationFiled: April 26, 2012Publication date: November 1, 2012Applicant: BIOENERGENIXInventors: John M. McCall, Robert C. Kelly, Donna L. Romero
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Publication number: 20120264739Abstract: Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.Type: ApplicationFiled: December 30, 2010Publication date: October 18, 2012Inventors: Wei-Guo Su, Hong Jia, Guangxiu Dai
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Publication number: 20120252778Abstract: The present invention relates to pyrazolo pyrimidine derivatives, to methods of preparing these, to combinations and pharmaceutical composition comprising these, and to their use in the treatment of diseases and disorders which may for example involve autoimmune diseases, angiogenesis, pain, and/or inflammatory diseases.Type: ApplicationFiled: March 26, 2012Publication date: October 4, 2012Applicant: NOVARTIS AGInventors: Wolfgang MILTZ, Berndt OBERHAUSER, Andrea VAUPEL, Juraj VELCICKY, Klaus WEIGAND, Rajender Reddy LELETI, Yugang LIU, Zhengming DU
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Publication number: 20120245136Abstract: The invention relates to chroman spirocyclic piperidine amide derivatives 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: ApplicationFiled: February 16, 2012Publication date: September 27, 2012Inventors: Sara Sabina HADIDA-RUAH, Mark Thomas Miller, Edward Adam Kallel, Brian Richard Bear, Vijayalaksmi Arumugam, Michael Paul Deninno, Jinglan Zhou, Johnny Uy, Bryan A. Frieman
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Publication number: 20120245162Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein.Type: ApplicationFiled: September 20, 2011Publication date: September 27, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, John D. HUBER, Weimin LIU, Ho Yin LO, Pui Leng LOKE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
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Patent number: 8273753Abstract: The present invention relates to a method of treating anxiety, epilepsy, sleep disorders, and insomnia, for inducing sedation-hypnosis, anesthesia, and muscle relaxation, and for modulating the necessary time to induce sleep and its duration, which comprises administering a therapeutically effective amount of Polymorph B of N-{2-Fluoro-5-[3-(thiophene-2-carbonyl)-pyrazolo[1,5-a]pyrimidin-7-yl]-phenyl}-N-methyl-acetamide characterized by a powder X-Ray diffraction pattern containing specific peaks at 2?=7.1° (±0.1°) and 21.4° (±0.1°) to a patient in need thereof.Type: GrantFiled: May 25, 2011Date of Patent: September 25, 2012Assignee: Ferrer International, S.A.Inventors: Luis Anglada, Albert Palomer, Antonio Guglietta
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Publication number: 20120238581Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof. Pharmaceutical compositions of formula (I) and related methods for treating or preventing metabolic diseases or conditions.Type: ApplicationFiled: May 31, 2012Publication date: September 20, 2012Inventors: Andrew J. Souers, Ju Gao, Todd M. Hasen, Rajesh R. Iyengar, Philip R. Kym, Bo Liu, Zhonghua Pei, Vince S. Yeh, Gang Zhao, Zhili Xin
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Publication number: 20120225867Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: October 27, 2010Publication date: September 6, 2012Inventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, lisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
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Publication number: 20120225888Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: ApplicationFiled: September 2, 2011Publication date: September 6, 2012Inventors: Annapurna Pendri, Guo Li, Samuel Gerritz, David R. Langley, George L. Trainor, Nicholas A. Meanwell
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Publication number: 20120214787Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1-R5 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: ApplicationFiled: August 23, 2011Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, Jonathon Alan DINES, John D. HUBER, Weimin LIU, Ho Yin LO, Pui Leng LOKE, Tina Marie MORWICK, Peter Allen NEMOTO, Alan OLAGUE, Doris RIETHER, Heather Tye, Lifen WU, Renee M. ZINDELL
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Publication number: 20120214815Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 6, 2012Publication date: August 23, 2012Applicant: UCB Pharma, S.A.Inventors: Benoît KENDA, Yannick QUESNEL, Ali ATES, Philippe MICHEL, Laurent TURET, Joël MERCIER
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Patent number: 8247415Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: April 2, 2009Date of Patent: August 21, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Cheng Zhu
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Publication number: 20120196866Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 6, 2012Publication date: August 2, 2012Applicant: UCB PHARMA, S.A.Inventors: Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joël Mercier
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Publication number: 20120190665Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.Type: ApplicationFiled: July 2, 2010Publication date: July 26, 2012Applicant: Genentech, Inc.Inventors: Paul Gibbons, Emily Hanan, Wendy Liu, Joseph P. Lyssikatos, Steven R. Magnuson, Rohan Mendonca, Richard Pastor, Thomas E. Rawson, Michael Siu, Mark Zak, Aihe Zhou, Bing-Yan Zhu
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Publication number: 20120183496Abstract: The present invention provides, among other things, compounds represented by the general Formula I: and pharmaceutically acceptable salts thereof, wherein X, Y, R1A, R1B, R2, and R3 are as defined in classes and subclasses herein and compositions (e.g., pharmaceutical compositions) comprising such compounds, which compounds are useful as inhibitors of hepatitis C virus polymerase, and thus are useful, for example, as medicaments for the treatment of HCV infection.Type: ApplicationFiled: December 16, 2011Publication date: July 19, 2012Applicant: COCRYSTAL DISCOVERY, INC.Inventors: Sam SK Lee, Wang Shen, Xiaoling Zheng, Irina C. Jacobson
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Publication number: 20120178715Abstract: Compounds of Formula I: and salts thereof in which R1, R2, R2a, R3, n, X and ring B have the meanings given in the specification, are inhibitors of mTOR and are useful in the treatment of diseases which are sensitive to inhibition of mTOR, such as cancers.Type: ApplicationFiled: September 3, 2010Publication date: July 12, 2012Applicant: ARRAY BIOPHARMA INC.Inventors: Steven W. Andrews, Kevin Ronald Condroski, Lisa A. De Meese, Jay Bradford Fell, John P. Fischer, John A. Josey, Kevin Koch, Yvan Le Huerou, Gregory F. Miknis, Martha E. Rodriguez, George T. Topalov, Eli M. Wallace, Rui Xu
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Patent number: 8211854Abstract: The present invention provides methods for inhibiting protein kinases selected from the group consisting of AKT, Checkpoint kinase, Aurora kinase, Pim kinases, and tyrosine kinase using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with protein kinases using such compounds.Type: GrantFiled: January 15, 2010Date of Patent: July 3, 2012Assignee: Schering CorporationInventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, David A. Parry
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Patent number: 8211828Abstract: Fungicidal mixtures comprising as active components: 1) at least one 1-methylpyrazol-4-ylcarboxanilide of the formula I ?in which the substituents are defined according to the description and 2) at least one azolopyrimidinylamine of the formula II ?in which the substituents are defined according to the description in a synergistically effective amount. Methods for controlling harmful fungi using mixtures of the compound I and compound II and also the use of the compound I and the compound II for preparing such mixtures, and compositions comprising such mixtures.Type: GrantFiled: January 17, 2008Date of Patent: July 3, 2012Assignee: BASF SEInventors: Jochen Dietz, Ulrich Schoefl, Egon Haden
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Publication number: 20120164209Abstract: An abuse resistant oral pharmaceutical composition, comprising: a barrier layer, comprising a first polymer; a diffusion layer, comprising a second polymer, substantially covering the barrier layer, wherein the diffusion layer is bonded to the barrier layer and comprises a drug that is substantially homogeneously distributed within the second polymer and diffuses from the diffusion layer within the gastrointestinal (GI) tract; and optionally an expansion layer comprising an expandable polymer, wherein the expansion layer is substantially covered by the barrier layer. Methods of making the same and methods of using the same are also provided.Type: ApplicationFiled: February 29, 2012Publication date: June 28, 2012Applicant: INSPIRION DELIVERY TECHNOLOGIIES, LLCInventors: Manish S. Shah, Ray Difalco
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Publication number: 20120165336Abstract: Disclosed in certain embodiments is a pharmaceutical packaging system comprising: a receptacle comprising an openable seal for accessing the interior of the receptacle; a pharmaceutical dosage form contained in the receptacle; and an activatable color-changing material, wherein upon activation, the material exhibits a visually discernible color change upon the lapsing of a predetermined time period.Type: ApplicationFiled: December 22, 2011Publication date: June 28, 2012Applicant: PURDUE PHARMA L.P.Inventor: LaDonna Steiner
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Publication number: 20120157451Abstract: Compounds of Formula (I) are useful for inhibition of Raf kinases. Methods of using compounds of Formula (I) and stereoisomers, tautomers and pharmaceutically acceptable salts thereof, 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: August 27, 2010Publication date: June 21, 2012Applicant: GENENTECH, INCInventors: Stefan Gradl, Joachim Rudolph, Li Ren
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Patent number: 8202878Abstract: The present invention relates to a compound of formula (I), or a pharmaceutically acceptable salt thereof, a pharmaceutical composition of formula (I), and related methods for treating or preventing metabolic diseases or conditions.Type: GrantFiled: November 29, 2007Date of Patent: June 19, 2012Assignee: Abbott LaboratoriesInventors: Andrew J. Souers, Ju Gao, Todd M. Hansen, Rajesh R. Iyengar, Philip R. Kym, Bo Liu, Zhonghua Pei, Vince S. Yeh, Gang Zhao, Zhili Xin
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Patent number: 8193372Abstract: Provided herein are phosphothiophene and phosphothiazole compounds, for example, of any of Formulae I, IA, IIA, IIIA, IVA, VA, VIA, VIIA, IB, IIB, IIIB, IVB, VB, VIB and VIIB disclosed herein, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host infected with HCV.Type: GrantFiled: March 3, 2010Date of Patent: June 5, 2012Assignee: Idenix Pharmaceuticals, Inc.Inventors: Cyril Dousson, Claire Pierra, Jean-Francois Griffon, Frederic Leroy, Jean-Laurent Paparin, David Dukhan, Dominique Surleraux
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Publication number: 20120135975Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.Type: ApplicationFiled: May 14, 2007Publication date: May 31, 2012Applicant: MERCK & CO., INC.Inventors: Vincent J. Colandrea, William K. Hagmann, Jeffrey J. Hale, Irene E. Whitney
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Patent number: 8188097Abstract: The present invention relates to a novel pyrazolo[1,5-a]pyrimidine compound of the formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc. Q is single bond, a methylene group or a group of the formula: —N(RQ)—, RQ is an alkyl group, Ring A is a substituted pyrazole ring fused to the adjacent pyrimidine ring having the following formula (A), (B) or (C), R3 and R4 are the same or different and a hydrogen atom, a cyano group etc. E is one of the following groups (i) to (v): R00 is an alkyl group, Q1 is a single bond etc., Q2 is a single bond or an alkylene group, one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., one of R50 and R60 is a hydrogen atom or an alkyl group and the other is a hydrogen atom, an alkyl group etc., R51 is an alkyl group or an optionally substituted arylsulfonyl group, R61 is an alkylamino group or an azido group, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 20, 2006Date of Patent: May 29, 2012Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Yasunori Moritani, Kimihiro Shirai, Mariko Oi
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Publication number: 20120122888Abstract: Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein R1, R2, R3, R4, and R5 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.Type: ApplicationFiled: November 2, 2011Publication date: May 17, 2012Applicant: ABBOTT LABORATORIESInventors: Xiangdong Xu, Jennifer Van Camp, Marc J. Scanio, William H. Bunnelle, Lei Shi, Augustine T. Osuma, David DeGoey, Arturo Perez-Medrano, Sridhar Peddi, Jyoti R. Patel
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Publication number: 20120122838Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: November 10, 2011Publication date: May 17, 2012Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
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Publication number: 20120121540Abstract: Provided are certain chemical entities, pharmaceutical compositions, and methods of treatment of a member of the flaviviradae family of viruses such as hepacivirus (Hepatitis C or HCV).Type: ApplicationFiled: August 8, 2008Publication date: May 17, 2012Inventors: Franz Ulrich Schmitz, Vincent W.F Tai, Roopa Ral, Christopher Don Roberts, Ali Dehghani Mohammad Abadi, Subramanian Baskaran, Irina Slobodov, Jack Maung, Martin Leon Neitzel
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Patent number: 8178533Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: May 31, 2006Date of Patent: May 15, 2012Assignee: UCB Pharma, S.A.Inventors: Benoît Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joël Mercier