The Polycyclo Ring System Is Quinazoline (including Hydrogenated) Patents (Class 514/252.17)
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Publication number: 20110118258Abstract: Compounds of general formula (I); or a stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R8 and R9 are as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as cancers, viral infection and inflammatory diseases or conditions.Type: ApplicationFiled: May 15, 2008Publication date: May 19, 2011Inventors: Stephen Martin Courtney, Mark Whittaker, Owen Clifford Mather, Christopher John Yarnold, Oliver Robin Barker, Christian Aldo Georges Napoleon Montalbetti, Thomas Hesterkamp, Mihaly Daniel Gardiner
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Publication number: 20110118277Abstract: Treating diseased or damaged tissue, particularly the liver, using stem cells. The hepatic stem cell population of a subject suffering from disease or damaged tissue can be expanded by administering at least one regulator of the sympathetic nervous system. The regulator can be an adrenoceptor agonist or antagonist, adrenoceptor antagonists, prazosin, being particularly preferred. The invention also includes the use of agents which mobilize stem cells in the manufacture of medicaments for the treatment of diseased or damaged tissue.Type: ApplicationFiled: June 18, 2010Publication date: May 19, 2011Inventors: Jude A. Oben, Anna M. Diehl
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Publication number: 20110112069Abstract: The specification describes the use of selected purine derivatives for the treatment of hyperproliferative diseases.Type: ApplicationFiled: August 15, 2008Publication date: May 12, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Frank Himmelsbach, Michael Mark, Mohammad Tadayyon, Leo Thomas
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Publication number: 20110112077Abstract: The present invention is directed to 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 Alzheimer's 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: ApplicationFiled: January 15, 2009Publication date: May 12, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Scott D. KUDUK, Ronald K, CHANG
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Publication number: 20110098305Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.Type: ApplicationFiled: May 20, 2009Publication date: April 28, 2011Inventors: Jonathan Bayldon Baell, Guillaume Laurent Lessene, Brad Edmund Sleebs, Wayne Fairbrother, John Flygare, Michael F.T. Koehler
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Publication number: 20110098286Abstract: 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 a process 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 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: July 10, 2007Publication date: April 28, 2011Applicant: H. LUNDBECK A/SInventor: Jan Kehler
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Publication number: 20110092489Abstract: Compounds represented by Structural Formula (I): are useful, for example, in the effective killing or reducing the rate of proliferation of cancer cells, such as in patients suffering from cancer. In addition to the compounds themselves, the invention provides pharmaceutical compositions of the compounds and method of treatment using the compounds.Type: ApplicationFiled: December 22, 2006Publication date: April 21, 2011Applicant: Prolexys Pharmaceuticals ,Inc.Inventors: Longwu QI, Raj Gopal Venkat, Michael Pierce, Paul B. Robbins, Sudhir R. Sahasrabudhe, Robert Selliah
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Publication number: 20110092502Abstract: Diaminothiazoles and pharmaceutical compositions containing them are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the diaminothiazoles in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: December 23, 2010Publication date: April 21, 2011Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland
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Patent number: 7928107Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium 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: March 3, 2006Date of Patent: April 19, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Dean Wilson, Andreas Termin, Jesus Gonzalez, Lev Fanning, Timothy Neubert, Paul Krenitsky, Pramod Joshi, Dennis Hurley, Urvi Sheth
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Publication number: 20110071144Abstract: The invention relates to quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group seleType: ApplicationFiled: April 23, 2010Publication date: March 24, 2011Inventors: Andrew Peter THOMAS, Craig Johnstone, Edward Clayton, Elaine Sophie Elizabeth Stokes, Jean-Jacques Marcel Lohmann, Laurent Francois Andre Hennequin
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Publication number: 20110065671Abstract: The present invention relates to Bicyclic Heterocycle Derivatives of formula (I), compositions comprising a Bi-cyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR1 19 in a patient.Type: ApplicationFiled: May 18, 2009Publication date: March 17, 2011Inventors: Joel M. Harris, Santhosh Francis, Bernard R. Neustadt, Craig D. Boyle, Hong Liu, Jinsong Hao, Andrew Starnford, Samuel Chackalamannil, William J. Greenlee
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Publication number: 20110065703Abstract: The present invention includes a group of chemical compounds useful as modulators of calcium ion (Ca2+) channels, especially for T-type, N-Type and L-type channels. The present invention also includes pharmaceutical compositions comprising these calcium ion channel modulating agents and methods of using these calcium ion channel modulating agents for the treatment diseases and conditions associated with the calcium ion channels.Type: ApplicationFiled: March 12, 2008Publication date: March 17, 2011Inventor: Jay Jie-Qiang Wu
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Publication number: 20110053932Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of Alk, Abl, Aurora-A, B-Raf, C-Raf, Bcr-Abl, BRK, Blk, Bmx, BTK, C-Kit, C-Raf, C-Src, EphB1, EphB2, EphB4, FGFR1, FGFR2, FGFR3, FLT1, Fms, Flt3, Fyn, FRK3, JAK2, KDR, Lck, Lyn, PDGFR?, PDGFR?, PKC?, p38, Src, SIK, Syk, Tie2 and TrkB kinases.Type: ApplicationFiled: June 18, 2008Publication date: March 3, 2011Inventors: Taebo Sim, Truc Ngoc Nguyen, Baogen Wu, Yun He, Yongping Xie, Xing Wang, Guobao Zhang, Nathanael Schiander Gray
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Publication number: 20110039845Abstract: A 2-aminoquinazoline derivative represented by formula (I) {wherein R1 represents a hydrogen atom, or the like, R2 represents a hydrogen atom, R3 represents formula (II) [wherein A1 represents formula (III), or the like, R8 represents lower alkyl, or the like, and R9 represents optionally substituted aryl, or the like], R4 represents hydroxy, or the like, and R5 represents optionally substituted aryl, or the like}, or a pharmaceutically acceptable salt thereof is provided.Type: ApplicationFiled: April 23, 2009Publication date: February 17, 2011Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Hajime Kashima, Tomoyuki Nishikawa, Yusuke Yamada, Toshihiro Seike, Yoshisuke Nakasato, Hiroshi Umehara
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Publication number: 20110034459Abstract: Compounds of formula (I) in which: R1 is: R2 is —CH3 or —CH2CH3; or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions including the compound of formula (I) and a pharmaceutically acceptable carrier. Processes for preparing the compound of formula (I). Methods of inhibiting a receptor tyrosine kinase in a subject in need thereof. Methods of inhibiting the growth of a tumor cell in a subject in need thereof. Methods of treating pancreatic cancer in a subject in need of treatment for pancreatic cancer. Methods of treating HER2 positive breast cancer in a subject in need of treatment for HER2 positive breast cancer. Methods of treating drug resistant non-small cell lung cancer in a subject in need of treatment for drug resistant non-small cell lung cancer. Each of these methods can include administering to the subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 9, 2010Publication date: February 10, 2011Applicant: Natco Pharma Ltd.Inventors: Bhujanga rao ADIBHATLA KALI SATYA, Ramanadham Jyothi Prasad, Bollepalli Nageshwara Rao, Nannapaneni Venkaiah Chowdary
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Publication number: 20110034477Abstract: Crystalline Form IV of doxazosin mesylate, a process for its preparation and uses thereof.Type: ApplicationFiled: July 10, 2008Publication date: February 10, 2011Applicant: CIPLA LIMITEDInventors: Rajendra Narayanrao Kankan, Dharmaraj Ramachandra Rao, Manish Gopaldas Gangrade, Shrikant Suresh Mudgal
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Publication number: 20110028488Abstract: The invention relates to a combination for use in the synergistic treatment of breast cancer comprising an antioestrogen and the Src kinase inhibitor AZD0530, a combination for the synergistic treatment of cancer comprising an EGFR TKI and the Src kinase inhibitor AZD0530 and a triple combination for the synergistic treatment of breast cancer comprising an antioestrogen, an EGFR TKI and the Src kinase inhibitor AZD0530.Type: ApplicationFiled: March 1, 2010Publication date: February 3, 2011Applicant: AstraZeneca ABInventor: Tim Paul GREEN
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Publication number: 20110028473Abstract: Methods employing and uses of a compound of formula (I) in inhibiting the growth of a tumor cell in a subject in need thereof. Methods employing and uses of a compound of formula (I) in treating pancreatic cancer in a subject in need of treatment for pancreatic cancer. Methods employing and uses of a compound of formula (I) in treating HER-2 positive breast cancer in a subject in need of treatment for HER-2 positive breast cancer. Methods employing and uses of a compound of formula (I) in treating drug resistant non-small cell lung cancer in a subject in need of treatment for drug resistant non-small cell lung cancer. Each of these methods can include administering to the subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 9, 2010Publication date: February 3, 2011Applicant: Natco Pharma Ltd.Inventors: Bhujanga rao ADIBHATLA KALI SATYA, Ramanadham JYOTHI PRASAD, Bollepalli NAGESHWARA RAO, Nannapaneni VENKAIAH CHOWDARY
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Publication number: 20110014186Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.Type: ApplicationFiled: March 23, 2009Publication date: January 20, 2011Inventors: Claus Ehrhardt, Leslie Wighton McQuire, Pascal Rigollier, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi
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Publication number: 20100331313Abstract: The present invention relates to novel Thiazole Derivatives, compositions comprising the Thiazole Derivatives, and methods for using the Thiazole Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.Type: ApplicationFiled: October 27, 2008Publication date: December 30, 2010Inventors: Panduranga Adulla P. Reddy, Tzu T. Wong, Lianyun Zhao, Shuyi Tang, Marc A. Labroli, Timothy J. Guzi, M. Arshad Siddiqui
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Publication number: 20100331287Abstract: 6-(Aminoalkyl)indazoles of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, and renal, cardiac and vascular protecting medicinally active ingredients.Type: ApplicationFiled: March 30, 2007Publication date: December 30, 2010Inventors: John J. Baldwin, David A. Claremon, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wenguang Zeng
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Publication number: 20100316713Abstract: The application relates to solid pharmaceutical compositions suitable for oral administration comprising an indolylmaleimide derivative, process for their production and use of the pharmaceutical compositions.Type: ApplicationFiled: December 19, 2008Publication date: December 16, 2010Inventors: Charu Kochhar, Unmesh Deodhar, Aravind Kerudi, G.V. M. Babu
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Publication number: 20100317630Abstract: The invention is directed to methods of using antagonists selective for the metabotropic mGlu5 receptor to treat conditions of neuromuscular dysfunction of the lower urinary tract in a mammal. Provided are methods of treating a mammal suffering from a condition of neuromuscular dysfunction of the lower urinary tract by administering a selective mGlu5 antagonist. The selective mGlu5 antagonist may be administered alone or in combination with one or more additional therapeutic agents for treating such a condition. Also provided are methods of identifying selective mGlu5 antagonists that are useful for treating neuromuscular dysfunction of the lower urinary tract in a mammal. Methods for treating migraine and gastroesophageal reflux disease (GERD) using selective mGlu5 antagonists are also disclosed.Type: ApplicationFiled: February 4, 2010Publication date: December 16, 2010Applicant: RECORDATI IRELAND LIMITEDInventors: Amedeo Leonardi, Gianni Motta, Carlo Riva, Elena Poggesi, Davide Graziani
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Publication number: 20100298294Abstract: The subject disclosure provides compositions for reducing serum cholesterol and/or triglyceride levels in subjects. These compositions can comprise racemic ?-hydroxybutyrate or D-?-hydroxybutyrate, optionally in the acid form, physiologically compatible salts of racemic ?-hydroxybutyrate or D-?-hydroxybutyrate, esters of D-?-hydroxybutyrate, oligomers of D-?-hydroxybutyrate containing from 2 to 20 or more monomeric units in either linear or cyclic form, racemic 1,3 butandiol or R-1,3 butandiol alone and can be, optionally, administered in conjunction with a low fat diet to a subject.Type: ApplicationFiled: January 5, 2009Publication date: November 25, 2010Applicant: ISIS INNOVATION LIMITEDInventors: Kiernan Clarke, Richard Lewis Veech
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Publication number: 20100292159Abstract: This invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of inflammatory pain, including hyperalgesia, thermal or mechanical allodynia, in vertebrate animals and particularly in human subjects. The AT2 receptor antagonists may be provided alone or in combination with other compounds such as those that are useful in the control of inflammatory conditions.Type: ApplicationFiled: March 20, 2007Publication date: November 18, 2010Applicant: UNIVERSITY OF QUEENSLANDInventor: Maree Therese Smith
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Publication number: 20100280042Abstract: The invention concerns quinazoline derivatives of Formula (I) wherein each of Q1, Z, m, R1, R2, R3 and Q2 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.Type: ApplicationFiled: January 29, 2010Publication date: November 4, 2010Inventors: Laurent Francois André HENNEQUIN, Patrick Ple
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Publication number: 20100273809Abstract: Methods and compositions for the treatment of alpha-adrenoceptor mediated conditions.Type: ApplicationFiled: December 13, 2008Publication date: October 28, 2010Inventors: Mihael H. Polymeropoulos, Paolo Baroldi, Curt D. Wolfgang
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Publication number: 20100273808Abstract: This invention provides a compound of formula (I): or a crystalline form thereof, or a pharmaceutical composition thereof, or an oral pharmaceutical dosage form thereof; processes for the synthesis or manufacture of the compound of formula (I), or a crystalline form thereof, or a pharmaceutical composition thereof, or an oral pharmaceutical dosage form thereof; and the use of said compound, or a crystalline form thereof, or a pharmaceutical composition thereof, or an oral pharmaceutical dosage form thereof, for the treatment of patients suffering from or subject to diseases, disorders or conditions involving cell survival, proliferation, and migration, including cardiovascular disease (e.g., arteriosclerosis and vascular reobstruction), cancer, (e.g., AML and malignant glioma)glomerulosclerosis, fibrotic disease and inflammation.Type: ApplicationFiled: November 20, 2009Publication date: October 28, 2010Applicant: Millennium Pharmaceticals, Inc.Inventors: Ian Armitage, Michael E. Bourland, Craig J.S. Boyle, Martin Ian Cooper, Abu J. Ferdous, Marianne Langston
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Publication number: 20100260669Abstract: Multi-dose active agent packages and methods for using the same for treating a subject for a condition are provided. Aspects of the invention include a multi-dose active agent package containing a plurality of unit dosage forms of an active agent configured to modulate at least a portion of a subject's autonomic nervous system during at least one season of the year. The active agent is present in an amount sufficient to alter the parasympathetic activity/sympathetic activity ratio of the subject in a manner effective to treat the subject for the condition. The subject active agent packages and methods find use in the treatment of a variety of different conditions, including disease conditions that increase in severity and/or occurrence during one or more seasons of the year. Also provided are kits for use in practicing the subject methods.Type: ApplicationFiled: April 15, 2010Publication date: October 14, 2010Inventors: Anthony Joonkyoo Yun, Patrick Yuarn-Bor Lee
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Publication number: 20100256120Abstract: The invention concerns a compound of the Formula I wherein m is 1-2 and each R1 is a group such as cyano, halogeno, trifluoromethyl heterocyclyl and heterocyclyloxy; R2 is trifluoromethyl or (1-6C)alkyl; R3 is hydrogen and R4 is, (1-6C)alkyl or (1-6C)alkoxy; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.Type: ApplicationFiled: August 7, 2006Publication date: October 7, 2010Inventors: Dearg Sutherland Brown, Ian Alun Nash, Steve Swallow
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Patent number: 7807683Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: March 31, 2006Date of Patent: October 5, 2010Assignee: Schering CorporationInventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Alan Mallams, Carmen S. Alvarez, Kartik M. Keertikar, Jocelyn Rivera, Tin Yau Chan, Vincent Madison, Thierry O. Fischmann, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park, Vidyadhar M. Paradkar, Douglas Walsh Hobbs
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Publication number: 20100240671Abstract: The present invention relates to substituted heterocyclic compounds of Formula I or XI: or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine II4 receptor inhibitors useful in the treatment of histamine II4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.Type: ApplicationFiled: March 19, 2010Publication date: September 23, 2010Applicant: INCYTE CORPORATIONInventors: Jincong ZHUO, Thomas P. MADUSKUIE, Ding-quan QIAN, Wenqing YAO
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Publication number: 20100233083Abstract: The present invention relates to a microparticle comprising a crosslinked polymer, which polymer is composed of a crosslinkable compound represented by the formula (I) wherein—X is a residue of a multifunctional radically polymerisable compound (having at least a functionality equal to n);—each Y independently is optionally present, and—if present—each Y independently represents a moiety selected from the group of O, S and NR0;—each R0 is independently chosen from the group of hydrogen and substituted and unsubstituted, aliphatic, cycloaliphatic and aromatic hydrocarbon groups which groups optionally contain one or more moieties selected from the group of ester moieties, ether moieties, thioester moieties, thioether moieties, carbamate moieties, thiocarbamate moieties, amide moieties and other moieties comprising one or more heteroatoms, in particular one or more heteroatoms selected from S, O, P and N, each R0 in particular independently being chosen from the group of hydrogen and substituted and unsubstitutType: ApplicationFiled: March 21, 2007Publication date: September 16, 2010Applicant: DSM IP ASSETS B.V.Inventors: Aylvin Jorge Angelo Anthasius Dias, Audrey Petit
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Publication number: 20100222331Abstract: The present invention encompasses compounds of general Formula (1) wherein R2, R3, Q, W, X, Y and Z are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: June 9, 2008Publication date: September 2, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald Engelhardt, Bodo Betzemeier, Guido Boehmelt, Ulrich Guertler, Thomas Karner, Oliver Kraemer, Daniel Kuhn, Jens Juergen Quant, Ulrich Reiser, Otmar Schaaf, Flavio Solca, Heinz Stadtmueller, Ulrike Tontsch-Grunt, Matthias Treu, Stephan Karl Zahn
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Publication number: 20100222359Abstract: The present invention provides quinazolinedione derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, depression and dementia.Type: ApplicationFiled: February 26, 2010Publication date: September 2, 2010Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra, Sureshbabu Dadiboyena, Kouacou Adiey
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Patent number: 7786123Abstract: Indolylmaleimide derivatives comprising either a substituted phenyl, naphthyl, tetrahydronaphthyl, quinazolinyl, quinolyl, isoquinolyl or pyrimidinyl residue have interesting pharmaceutical properties, e.g. in the treatment and/or prevention of T-cell mediated acute or chronic inflammatory diseases or disorders, autoimmune diseases, graft rejection or cancer.Type: GrantFiled: July 7, 2009Date of Patent: August 31, 2010Inventors: Rainer Albert, Nigel Graham Cooke, Sylvain Cottens, Claus Ehrhardt, Jean-Pierre Evenou, Richard Sedrani, Peter Von Matt, Jürgen Wagner, Gerhard Zenke
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Publication number: 20100216767Abstract: The invention provides novel compounds that are inhibitors of PDK1. Also provided are pharmaceutical compositions including the compounds, and methods of treating proliferative diseases, such as cancers, with the compounds or compositions.Type: ApplicationFiled: December 20, 2007Publication date: August 26, 2010Inventors: Mina Aikawa, Payman Amiri, Steven Bashman, Jeffrey Dove, Rama Jain, Xiaodong Lin, Jeremy Murray, Savithri Ramurthy, Alice Rico, Wei Shu, Sharadha Subramanian, Xiaojing Michael Wang, Robert L. Warne, Yasheen Zhou
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Publication number: 20100216808Abstract: Pyrazolo-quinazoline derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: December 17, 2007Publication date: August 26, 2010Applicant: Nerviano Medical Sciences S.r.lInventors: Michele Caruso, Italo Beria, Maria Gabriella Brasca, Ronald Ferguson, Helena Posteri, Barbara Valsasina
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Publication number: 20100210663Abstract: Hybrid compounds containing an aminotetralin moiety or a heterocyclic and/or open chain analog thereof linked through an alkylene group to an aryl ring system-substituted piperidiene moiety exhibit high levels of CNS activity, in some cases exhibiting especially high relative binding efficiencies between D3 and D2 dopaminergic receptor subtypes.Type: ApplicationFiled: April 29, 2010Publication date: August 19, 2010Applicant: WAYNE STATE UNIVERSITYInventor: Aloke K. Dutta
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Publication number: 20100204226Abstract: Quinazolinone compounds of formula (I) are described, which are useful as prolyl hydroxylase inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity. Thus, the compounds may be administered to treat, e.g., anemia, vascular disorders, metabolic disorders, and wound healing.Type: ApplicationFiled: February 10, 2010Publication date: August 12, 2010Inventors: Scott D. Bembenek, Frances M. Hocutt, Barry Eastman Leonard, JR., Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan
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Publication number: 20100179162Abstract: Crystalline forms of the sulfate salt of 4-[6-methoxy-7-(3-piperidin-1-yl-propoxy)quinazolin-4-yl]piperazine-1-carboxylic acid (4-isopropoxyphenyl)-amide, which may be used in pharmaceutical applications, are disclosed. Particular single crystalline forms of the sulfate salt are characterized by a variety of properties and physical measurements. As well, methods of producing the sulfate salts, and using such salts to inhibit excessive tyrosine kinase activity in subjects to treat a number of diseases including cardiovascular disease (e.g., arteriosclerosis and vascular reobstruction), cancer (e.g., leukemia such as acute lymphocytic leukemia), glomerulosclerosis fibrotic diseases and inflammation, and general treatment of cell-proliferative diseases, are also discussed.Type: ApplicationFiled: July 20, 2006Publication date: July 15, 2010Applicant: Millennium Pharmaceuticals , Inc.Inventors: Craig Grant, Hoa Q Luong, Mark D. Angelino
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Publication number: 20100179109Abstract: Disclosed are compounds of Formula (I) wherein the R, R1, R2, R3, X, Y, A, Q, E, and G are defined herein. These compounds bind to aspartic proteases to inhibit their activity and are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also disclosed are methods of use of the compounds of Formula I for ameliorating or treating aspartic protease related disorders in a subject in need thereof.Type: ApplicationFiled: April 4, 2008Publication date: July 15, 2010Inventors: Jonh J. Baldwin, Salvacion Cacatian, David Claremon, Lawrence W. Dillard, Patrick T. Flaherty, Bahman Ghavimi-Alagha, Damiano Ghirlanda, Alexey V. Ishchenko, Lara S. Kallander, Brian Lawhorn, Colin A. Leach, Qing Lu, Gerard McGeehan, Jaclyn R. Patterson, Robert D. Simpson, Suresh B. Singh, Patrick Stoy, Lamont R. Terrell, Colin Tice, Zhenrong Xu, Jing Yuan, Catherine C. K. Yuan, Jing Zhang, Wei Zhao
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Publication number: 20100179144Abstract: Invented is a method of inhibiting the activity/function of PI3 kinases using quinazoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinazoline derivatives.Type: ApplicationFiled: June 12, 2008Publication date: July 15, 2010Inventors: Nicholas D. Adams, Joelle Lorraine Burgess, Michael Gerard Darcy, Steven David Knight, Kenneth Allen Newlander, Lance H. Ridgers, Stanley J. Schmidt
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Publication number: 20100179120Abstract: The present invention provides a novel amide derivative and a pharmaceutically acceptable salt thereof which selectively and effectively inhibits the growth of cancer cells induced by the overexpression of an epidermal growth factor receptor and also prevents the development of drug resistance caused by the mutation of EGFR tyrosine kinase, and a pharmaceutical composition comprising same as an active ingredient.Type: ApplicationFiled: June 5, 2008Publication date: July 15, 2010Applicant: HANMI PHARM. CO., LTD.Inventors: Kwang-Ok Lee, Mi Young Cha, Mi Ra Kim, Young Hee Jung, Chang Gon Lee, Se Young Kim, Keukchan Bang, Bum Woo Park, Bo Im Choi, Yun Jung Chae, Mi Young Ko, Han Kyong Kim, Young-Gil Ahn, Maeng Sup Kim, Gwan Sun Lee
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Publication number: 20100168123Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.Type: ApplicationFiled: September 25, 2009Publication date: July 1, 2010Inventors: Ian S. Mitchell, Keith L. Spencer, Peter Stengel, Yongxin Han, Nicholas C. Kallan, Mark Munson, Guy P.A. Vigers, James Blake, Anthony Piscopio, John Josey, Scott Miller, Dengming Xiao, Rui Xu, Chang Rao, Bing Wang, April L. Bernacki
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Publication number: 20100158863Abstract: A quinazoline derivative of formula (I), or a pharmaceutically acceptable salt thereof: formula (I) for use in treatment of prevention of a flaviviridae infection.Type: ApplicationFiled: January 11, 2007Publication date: June 24, 2010Applicant: ARROW THERAPEUTICS LIMITEDInventors: Neil Mathews, Alexander James Floyd Thomas, Keith Charles Spencer, Nathalie Tiberghien, Christopher John Pilkington, Lyn Jennens, Surinder Chana, Ian John Fraser
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Publication number: 20100160315Abstract: This invention relates to novel 2,3-diamino-quinazolinone derivatives having medical utility, to use of the 2,3-diamino-quinazolinone derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2,3-diamino-quinazolinone derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of Kv7 channels.Type: ApplicationFiled: May 22, 2008Publication date: June 24, 2010Applicant: Neuro Search A/SInventors: Carsten Jessen, William Dalby Brown, Joachim Demnitz, Dorte Strobaek, Mads P.G. Korsgaard, Palle Christophersen
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Publication number: 20100160338Abstract: The present invention relates to new benzenesulfonamide modulators of alpha-1A adrenergic receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 18, 2009Publication date: June 24, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100160316Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels and calcium 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: March 1, 2010Publication date: June 24, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jesus E. Gonzalez, III, Dean M. Wilson, Andreas P. Termin, Peter D. J. Grootenhuis, Yulian Zhang, Benjamin J. Petzoldt, Lev Tyler Dewey Fanning, Timothy D. Neubert, Roger D. Tung, Esther Martinborough, Nicole Zimmerman
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Publication number: 20100160297Abstract: The present invention relates to the compounds of formula I as well as to their use as PIM kinase inhibitors and, thereby, their use for treating oncological diseases, particularly of the hematopoietic system, the liver and the prostate gland.Type: ApplicationFiled: November 11, 2009Publication date: June 24, 2010Inventors: Karoly Nikolich, Laszlo Nadasdi, Tanjew Dittgen, Armin Schneider