The Additional Hetero Ring Consists Of Carbon And Chalcogen As The Only Ring Members Patents (Class 514/266.24)
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Patent number: 8586091Abstract: The present invention relates to a pharmaceutical composition comprising N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furyl]-4-quinazolinamine as active pharmaceutical ingredient and a process of preparing such composition.Type: GrantFiled: August 24, 2009Date of Patent: November 19, 2013Assignee: ratiopharm GmbHInventors: Katrin Rimkus, Frank Muskulus, Sandra Brueck, Jana Paetz
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Publication number: 20130303551Abstract: This invention relates to the use of pyrimidinone derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of pyrimidinones in the treatment of cancer.Type: ApplicationFiled: January 10, 2012Publication date: November 14, 2013Inventors: Nicholas D. Adams, Alexander Joseph Reif, Kenneth Wiggall
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Publication number: 20130302328Abstract: This disclosure provides ten (10) specific peptides, and particular peptide characteristics, from the cell membrane-bound Her2 protein and a diagnostic assay useful for determining the presence and amount of full length and truncated versions of the full-length Her2 protein in cells derived from formalin fixed paraffin embedded tissue.Type: ApplicationFiled: December 8, 2011Publication date: November 14, 2013Applicant: Expression Pathology, Inc.Inventor: David Krizman
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Publication number: 20130296271Abstract: Agri-horticultural pest control compositions having outstanding control effect on pests, in particular, agri-horticultural pests, which comprise as active ingredients one or more 4-(3-butynyl)aminopyrimidine derivatives represented by the general formula [I], namely, where R1 is typically selected from among: a) phenyl c) —SiR5R6R7 (R5, R6, and R7 which may be the same or different represent a linear or branched alkyl having 1-6 carbon atoms, a linear or branched haloalkyl having 1-3 carbon atoms which is substituted by one halogen atom, a linear or branched cyanoalkyl having 1-3 carbon atoms which is substituted by one cyano group, and phenyl); d) hydropgen atom; R2 typically represents a hydrogen atom; R3 typically represents a hydrogen atom; R4 represents a hydrogen atom and one or more agri-horticultural pest control compounds selected from among agri-horticultural antimicrobial compounds, say, multi-site contact active compouns, nucleic acids synthesis inhibitory active compounds, mitosis and cellType: ApplicationFiled: December 27, 2011Publication date: November 7, 2013Applicant: SDS Biotech K.K.Inventors: Masaaki Sakai, Tomoaki Matsumura, Satohiro Midorikawa, Takashi Nomoto, Tomoko Muraki, Ryutaro Katsuki
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Publication number: 20130296350Abstract: The present invention is directed to methods and agents that are useful in the prevention and amelioration of signs and symptoms associated with neuropathic conditions. More particularly, the present invention discloses the use of angiotensin II receptor 2 (AT2 receptor) antagonists for the treatment, prophylaxis, reversal and/or symptomatic relief of neuropathic pain, including mechanical hyperalgesia, thermal or mechanical allodynia, diabetic pain and entrapment pain, 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 neuropathic conditions.Type: ApplicationFiled: June 20, 2013Publication date: November 7, 2013Inventors: Maree Therese Smith, Bruce Douglas Wyse
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Publication number: 20130296332Abstract: The present invention relates to 1H-Quinazoline-2,4-diones of formula (I) wherein R1 and R2 are as defined in the specification, their preparation, their use as pharmaceuticals, and pharmaceutical compositions containing them. Further, intermediates for the manufacture of compounds of formula (I) are and combinations comprising compounds of formula (I) are disclosed.Type: ApplicationFiled: July 1, 2013Publication date: November 7, 2013Inventors: Hans ALLGEIER, Yves AUBERSON, David CARCACHE, Philipp FLOERSHEIM, Christel GUIBOURDENCHE, Wolfgang FROESTL, Jörg KALLEN, Manuel KOLLER, Henri MATTES, Joachim NOZULAK, David ORAIN, Johanne RENAUD
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Publication number: 20130289057Abstract: The invention relates to N-arylaminomethylenebenzothiophenones of General Formula (I) for use as a drug for the treatment of cardiovascular diseases: wherein E is S, O, or CH2, D is CH or NH, and Ar is a phenyl or naphtyl moiety substituted by an electron-withdrawing group, an unsubstituted heteroaryl residue, or a heteroaryl residue substituted by alkyl or an electron-withdrawing group.Type: ApplicationFiled: January 12, 2012Publication date: October 31, 2013Applicants: FORSCHUNGSVERBUND BERLIN E.V., MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZINInventors: Enno Klussmann, Walter Rosenthal, Jelena Milic, Martin W. Bergmann
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Publication number: 20130289056Abstract: Disclosed are methods of treating a patient having cancer with an EGFR inhibitor requiring an active step of avoiding or modifying the co-administration of such drugs with P-gp modulators. This invention also relates to a medicament for treating a patient having cancer, comprising an EGFR inhibitor as the active product ingredient, customized for avoiding co-administration with P-gp inducers and/or inhibitors by an instruction added to the medicament or the package containing said medicament.Type: ApplicationFiled: August 24, 2011Publication date: October 31, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Robert Michael Lorence, Mehdi Shahidi, Peter Stopfer
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Publication number: 20130281397Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer, including NUT midline carcinoma, Burkitt's Lymphoma, Acute Myelogenous Leukemia, and Multiple Myeloma; autoimmune or inflammatory diseases or conditions, and sepsis.Type: ApplicationFiled: March 15, 2013Publication date: October 24, 2013Applicant: RVX Therapeutics Inc.Inventors: Kevin G. McLure, Peter Ronald Young
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Publication number: 20130281398Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of diseases or disorders that are susceptible to administration of a BET inhibitor.Type: ApplicationFiled: March 15, 2013Publication date: October 24, 2013Applicant: RVX Therapeutics Inc.Inventors: Kevin G. McLure, Peter R. Young
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Publication number: 20130266563Abstract: Selenophene compounds of formula (I) are described herein. In the compounds of Formula (I), ring A is a 6-membered aromatic fused ring, optionally containing one, two or three nitrogen atoms; a 5-membered heteroaromatic fused ring; or a mono- or bicyclic saturated heterocyclic fused ring having at least one ring member selected from the group consisting of N, O, S, SO and SO2; Y in ring B is nitrogen or substituted carbon; X is NR6, O, S, S(O), or S(O)2. R1, R2, R3, R4, and R6 are defined in the specification. Selenophene compounds of formula (I) may be used in methods of treating cell proliferative disorders, particularly cancer. Pharmaceutical compositions containing selenophene compounds of formula (I) may be used for treatment, inhibition, or control of cancer.Type: ApplicationFiled: May 17, 2013Publication date: October 10, 2013Inventors: Ganga Raju Gokaraju, Sudhakar Kasina, Venkateswarlu Somepalli, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Kiran Bhupathiraju, Trimurtulu Golakoti, Krishanu Sengupta, Venkata Krishna Raju Alluri
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Patent number: 8552018Abstract: Protein kinase inhibitors are disclosed having utility in the treatment of protein kinase-mediated diseases and conditions, such as cancer. The compounds of this invention have the following structure: including steroisomers, prodrugs and pharmaceutically acceptable salts thereof, wherein A is a ring moiety selected from: and wherein R1, R2, R3, X, Z, L1, Cycl1, L2 and Cycl2 are as defined herein. Also disclosed are compositions containing a compound of this invention, as well as methods relating to the use thereof.Type: GrantFiled: March 18, 2011Date of Patent: October 8, 2013Assignees: Arizona Board of Regents on behalf of the University of Arizona, Astex Pharmaceutials, Inc.Inventors: Laurence H. Hurley, Daruka Mahadevan, David J. Bearss, Hariprasad Vankayalapati, Sridevi Bashyam, Steven L. Warner, James Welsh
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Publication number: 20130259858Abstract: A method of predicting outcome in a subject with for example Her2+ (ER??) breast cancer comprising: a. determining a HTICs expression signature comprising determining an expression level of 2 or more HTICS biomarkers selected from Aurkb, Ccna2, Scrn1, Npy, Atp7b, Chaf1b, Ccnb1 Cldn8, Nrp1, Ccr2, C1qb, Cd74, Vcam1, Cd180, Itgb2, Cd72, St8sia4 Kif11, Plk1, Chek1, Mphosph6, Coro1a, Ccl5, Cd3e Hcls1, Vav1, Plek, Arhgdib, Il2rg, Sash3, Lck, Il2rb, Cybb, Cd79b, Sell, Ccnd2, Tnfrsf1b, Rftn1, Rac2 and Ly86; and b. calculating a signature score, the signature score comprising a sum of HTICs biomarker expression parameters; wherein a signature score greater than a selected cut-off or control signature score is indicative of a poor outcome (HTICS+) and a signature score less than a selected cut-off is indicative of a good outcome (HTICS?). The methods can be used to prognose outcome and/or select suitable treatment. Arrays and kits for use with the methods are also provided.Type: ApplicationFiled: March 14, 2013Publication date: October 3, 2013Applicant: UNIVERSITY HEALTH NETWORKInventors: Eldad Zacksenhaus, Jeff Liu
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Patent number: 8545884Abstract: The present invention relates to a pharmaceutical dosage form containing the active substance BIBW 2992 as the dimaleate salt, providing an immediate release profile of the active substance, further, the invention relates to compacted intermediates comprising BIBW 2992 dimaleate salt (BIBW 2992 MA2) in form of a powder prepared using a combined roller compaction and sieving step from BIBW 2992 MA2, intermediate blends prepared from said compacted intermediate as well as solid oral formulations providing an immediate release profile of the active substance, made from said compacted intermediate or from said intermediate blends ready for use/ingestion, e.g. capsule and tablet formulations such as uncoated or film-coated tablets prepared by direct-compression, and methods for their production.Type: GrantFiled: June 5, 2009Date of Patent: October 1, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Roman Messerschmid, Thomas Friedl
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Publication number: 20130251702Abstract: Methods for screening compounds for treating sepsis are disclosed. The present methods and compositions are targeting NOD2 mediated signaling pathway and the agents identified by the present methods are qualified as drug candidates for clinical development. Further Methods and composition for treating sepsis are disclosed.Type: ApplicationFiled: March 21, 2013Publication date: September 26, 2013Applicant: SNU R&DB FOUNDATIONInventors: Doo Hyun CHUNG, Sae Jin OH, Ji Hyung KIM
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Publication number: 20130251631Abstract: Disclosed are oxo-hydroquinazolines that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.Type: ApplicationFiled: May 17, 2013Publication date: September 26, 2013Applicants: Forschungsverbund Berlin E.V., The Government of the United States of America as represented by the Secretary of the Department ofInventors: Marvin C. Gershengorn, Susanne Neumann, Bruce M. Raaka, Craig J. Thomas, James Inglese, Noel T. Southall, Steven Titus, Wei Zheng, Wenwei Huang, Gerd Krause, Gunnar Kleinau
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Publication number: 20130252979Abstract: The present invention relates to a novel crystalline anhydrous form of [(5-chlorothiophene-2-ylsulfonylcarbamoyl)-(4-(6-fluoro-7-(methylamino)-2,4-dioxo-1,2-dihydroquinazolin-3(4H)-yl)phenyl)amide, potassium salt, and its use in the treatment or prevention of a condition or a disorder with platelet ADP receptor inhibition, in particular, P2Y12 inhibition, in animals, particularly humans. It also relates processes for making such a novel crystalline form. The present invention also relates to a solid, oral for mulation of this novel crystalline form, its preparation and use thereof.Type: ApplicationFiled: December 5, 2011Publication date: September 26, 2013Inventors: Ulrich Meier, Nicole Bieri, Dieter Becker, Julien Taillemite, Marie-Pierre Filliot, Tanja Meister
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Patent number: 8524721Abstract: Novel compounds of formulae (I) and (VIII), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I) to (VIII), or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 10, 2011Date of Patent: September 3, 2013Assignee: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles K. Marlowe, Kim A. Kane-Maguire
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Publication number: 20130225596Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R16)— or the like; R16 is hydrogen, substituted or unsubstituted alkyl or the like; R7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q1 and Q2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: August 9, 2011Publication date: August 29, 2013Inventors: Hiroyuki Kai, Takeshi Endoh, Sae Jikihara, Kentaro Asahi, Tohru Horiguchi
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Publication number: 20130216523Abstract: Methods are provided for facilitating the diagnosis of subjects with HER1-activated cancers. In addition, method of treating subjects with a cancer characterized as having high levels of activated HER1 are provided. Also provided are methods for determining or otherwise assessing the prognosis of an subject with a HER1-activated cancer. The methods include the analysis of samples for the presence or the absence of activated HER1 markers as indicated by HER1-HER1 homodimers, HER1 phosphorylation at position 1173, pan-phosphorylation of HER1 or associated molecules, or HER1-HER2 heterodimers. Activated HER1 measurements can be used to track a subject's response to a treatment regimen, predict the success of using a particular treatment regimen, determine the effects of a treatment regimen, or for categorizing a subject in order to create a homogenous group for a clinical trial.Type: ApplicationFiled: April 2, 2012Publication date: August 22, 2013Applicant: LABORATORY CORPORATION OF AMERICA HOLDINGSInventors: Gerald J. Wallweber, John William Winslow
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Publication number: 20130210805Abstract: This application provides for compounds of the formula Formula I or a pharmaceutically acceptable salt thereof, wherein the individual variables are defined herein, as well as processes to prepare these compounds, pharmaceutical compositions comprising the same and their use in treating disease state associated with the CRTH2 receptor.Type: ApplicationFiled: October 6, 2011Publication date: August 15, 2013Inventors: Robert G. Aslanian, Christopher W. Boyce, Robert D. Mazzola, JR., Brian A. McKittrick, Kevin D. McCormick, Anandan Palani, Jun Qin, Haiqun Tang, Dong Xiao, Younong Yu, John P. Caldwell, Elizabeth Helen Kelley, Hongjun Zhang, Phieng Siliphaivanh, Rachel N. MacCoss, Joey L. Methot, Jolicia Polivina Gauuan, Qin Jiang, Andrew J. Leyhane, Johny Biju, Li Dong, Xian Huang, Ning Shao, Wei Zhou, Pawan K. Dhondi
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Publication number: 20130209461Abstract: A method for treating an Epidermal Growth Factor Receptor (EGFR) dependent diseases or diseases that have acquired resistance to agents that target EGFR family members comprising administering a therapeutically effective amount of a compound of formula (I) alone or in combination with an EGFR modulator, to a warm-blooded animal in need thereof; combinations comprising the compound of formula (I) and an EGFR modulator for the treatment of said diseases; and pharmaceutical preparations for the treatment of said diseases comprising the compound of formula (I), alone or in combination with an EGFR modulator.Type: ApplicationFiled: November 7, 2011Publication date: August 15, 2013Applicant: NOVARTIS AGInventors: Saskia Maria Brachmann, Christine Fritsch, Sauveur-Michel Maira, Christian Rene Schnell, Carlos Garcia-Echeverria
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Publication number: 20130202587Abstract: The present disclosure provides a method for identifying whether a subject is more or less likely to be responsive to VEGF-based therapy, comprising screening a nucleic acid sample obtained from the subject to provide output information which identifies the presence or absence of an allelic variant, wherein the presence or absence of an allelic variant indicates whether the subject is more or less likely to be responsive to VEGF-based therapy.Type: ApplicationFiled: August 24, 2012Publication date: August 8, 2013Applicant: Randox Laboratories Ltd.Inventor: John Lamont
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Publication number: 20130195870Abstract: The present invention concerns somatic ErbB3 mutations in cancer including methods of identifying, diagnosing, and prognosing ErbB3 cancers, as well as methods of treating cancer, including certain subpopulations of patients.Type: ApplicationFiled: November 29, 2012Publication date: August 1, 2013Applicant: Genentech, Inc.Inventor: Genentech, Inc.
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Publication number: 20130190321Abstract: Methods and kits for aiding in detection, assessment and treatment of a proliferative disorder of the prostate gland in a subject are provided according to aspects of the present invention which include assaying a first biological sample comprising prostate gland cells obtained from the subject for expression of one or more biomarkers selected from the group consisting of: alcohol dehydrogenase 1B, alcohol dehydrogenase 1C, alcohol dehydrogenase 4 and hepatocyte nuclear factor 1B; and determining, based on the expression of the one or more biomarkers in the sample that the subject has, or is at risk of having, a proliferative disorder of the prostate gland.Type: ApplicationFiled: January 23, 2013Publication date: July 25, 2013Applicant: WEST CHESTER UNIVERSITY OF PENNSYLVANIAInventor: West Chester University of Pennsylvania
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Patent number: 8492396Abstract: The disclosure relates to methods of using an adrenergic ?-1 receptor antagonist or its pharmaceutically acceptable salts for treating and/or preventing interstitial cystitis, overactive bladder or detrusor overactivity.Type: GrantFiled: March 24, 2010Date of Patent: July 23, 2013Assignee: SANOFIInventor: Pierangelo Geppetti
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Publication number: 20130183297Abstract: The method of treating a person having a cancer selected from carcinoma, sarcoma or hematopoietic cancer by administering (a) an effective amount of at least one anti-cancer drug selected from the group consisting of an epidermal growth factor receptor (EGFR) inhibitor, a vascular endothelial growth factor receptor (VEGFR) inhibitor and a Raf kinase inhibitor and (b) an effective amount of 5-(4-(6-(4-amino-3,5-dimethyl-phenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy)-benzyl)-thiazolidine-2,4-dione.dihydrochloride provided that said carcinoma is not lung cancer when an EGFR inhibitor is erlotinib. The invention also provides a pharmaceutical composition that may be used in practicing said method.Type: ApplicationFiled: February 26, 2013Publication date: July 18, 2013Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventor: DAIICHI SANKYO COMPANY, LIMITED
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Publication number: 20130178443Abstract: Novel quinazolinamide derivatives of the formula (I), in which R1-R43 and X have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: August 31, 2011Publication date: July 11, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Hans-Michael Eggenweiler, Christian Sirrenberg, Hans-Peter Buchstaller
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Publication number: 20130178487Abstract: The present invention relates to the use of quinazolines of formula (I), wherein the groups Ra to Rd have the meanings given in the claims and specification, in cancer therapy.Type: ApplicationFiled: February 14, 2013Publication date: July 11, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Flavio SOLCA, Andree AMELSBERG, Jacobus C.A. van MEEL, Anke BAUM, Gerd STEHLE
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Publication number: 20130172334Abstract: Disclosed herein are compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein X1, L, Rx, Ry, G, Z, A, m, n, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: December 17, 2012Publication date: July 4, 2013Applicant: ABBVIE INC.Inventor: AbbVie Inc.
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Publication number: 20130172374Abstract: A novel solid composition and methods for making and using the solid composition are provided. The solid composition comprises: (a) at least one active agent with a solubility of less than about 0.3 mg/ml in an aqueous solution with a pH of at most about 6.8 at a temperature of about 37° C.; and (b) a hydrophilic polymer matrix composition comprising: i) a hydrophilic polymer selected from the group consisting of METHOCEL™, POLYOX™ WSR 1105 and combinations thereof; and optionally ii) a hydrophobic polymer selected from the group consisting of Ethocel 20 premium; and (c) an alkalizer selected from the group consisting of calcium carbonate, magnesium oxide heavy and sodium bicarbonate; wherein the composition provides at least about 70% release of the active between about 7 to about 12 hours following oral administration.Type: ApplicationFiled: October 1, 2012Publication date: July 4, 2013Applicant: Portola Pharmaceuticals, Inc.Inventor: Portola Pharmaceuticals, Inc.
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Publication number: 20130165458Abstract: A compound for treating protein kinase-related disease or disorder having a structure of formula (A): wherein X is N or CH; Y is NH, O, or CH2; Z is an aryl or a heteroaryl; and R1, R2, R3, and R4 are independently H, halo, nitro, cyano, aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, cycloalkenyl, heterocycloalkenyl, —ORa, —C(O)Ra, —C(O)NRaRb, —NRaC(O)Rb, —NRaRb, —S(O)2Ra, —S(O)2NRa Rb, —NRaS(O)2Rb, —N?CRaRb, or —NRaC(O)NHRb, wherein each of Ra and Rb, independently, is H, alkyl, alkenyl, alkynyl, aryl, aryloxy, alkoxy, hydroxy, heteroaryl, cycloalkyl, heterocycloalkyl, cycloalkenyl, or heterocycloalkenyl, or Ra and Rb, together with the nitrogen atom to which they are bonded, form heteroaryl, heterocycloalkyl, or heterocycloalkenyl; or R3 and R4 are as defined above, and R1 and R2 together with the carbons, to which they are attached, form a heterocycloalkenyl or heteroaryl.Type: ApplicationFiled: December 27, 2011Publication date: June 27, 2013Applicant: DEVELOPMENT CENTER FOR BIOTECHNOLOGYInventors: Jiann-Jyh Huang, Chu-Bin Liao, Pao-Nien Chen
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Publication number: 20130164218Abstract: This disclosure relates to Hypoxia Inducible Factor-1 pathway inhibitors and uses as anticancer and imaging agents. In certain embodiments, the disclosure contemplates compounds and pharmaceutical compositions disclosed herein.Type: ApplicationFiled: December 27, 2012Publication date: June 27, 2013Applicant: EMORY UNIVERSITYInventor: EMORY UNIVERSITY
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Publication number: 20130165459Abstract: The present invention is concerned with a solid delivery form of elinogrel for the treatment of thrombosis which is notable for its multi-pH dissolution, immediate release and improved pharmacokinetic properties and stability in storage. The delivery and dosage form is a solid, oral formulation comprising: a) at least about 15% by weight elinogrel or a pharmaceutically acceptable salt thereof relative to the total weight of the overall pharmaceutical composition, and b) at least one pharmaceutically acceptable carrier. A further aspect of the present invention concerns the preparation and use of such a formulation.Type: ApplicationFiled: January 12, 2011Publication date: June 27, 2013Applicants: NORVARTIS PHARMA AG, PORTOLA PHARMACEUTICALS, INC.Inventors: Juan Wang, Chandir Ramani, Joe Lambing, Christine Ye, Elizabeth Vadas, Julian Taillemite, Marie-Pierre Filliot, Dieter Becker
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Publication number: 20130143841Abstract: Embodiments herein provide compounds and methods of making and using such compounds for prevention and treatment of multidrug resistant bacteria. In particular, embodiments are directed to anti-bacterial agents from benzo[d]heterocyclic scaffolds for prevention and treatment of multidrug resistant bacteria.Type: ApplicationFiled: January 29, 2013Publication date: June 6, 2013Applicant: UNIVERSITY OF NOTRE DAME DU LACInventor: UNIVERSITY OF NOTRE DAME DU LAC
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Publication number: 20130129809Abstract: The invention relates to compositions and methods for treating cancer comprising administering to a subject in need a pharmaceutically effective dose of a cancer stem cell inhibitor, methods of inhibiting the growth of cancer stem cells or tumor initiating cell comprising administering to a subject in need a pharmaceutically effective dose of a cancer stem cell inhibitor, and methods of enhancing the biological effects of chemotherapeutic drugs or irradiation on cancer cells comprising administering to a subject in need a pharmaceutically effective dose of a chemotherapeutic drug and a pharmaceutically effective dose of a cancer stem cell inhibitor.Type: ApplicationFiled: May 21, 2012Publication date: May 23, 2013Applicant: Glax L.L.C.Inventors: Rakesh K. Srivastava, Sharmila Shankar
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Publication number: 20130131089Abstract: The present invention is concerned with a liquid delivery form of Elinogrel for the treatment of thrombosis which is notable for its improved dosage properties and stability. The dosage form is a liquid or a lyophilized form which is reconstituted for an injectable formulation comprising: a) at least about 3 mg/ml or up to about 15 mg/ml Elinogrel or a pharmaceutically acceptable salt thereof (post reconstitution or in liquid form), and b) at least one pharmaceutically acceptable excipient. Further aspects of the present invention concern the preparation and use of such a formulation.Type: ApplicationFiled: May 2, 2011Publication date: May 23, 2013Applicant: Portola Phamaceuticals Inc.Inventors: Hui Li, Juan Wang, Joe Lambing, Harry Tiemessen
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Publication number: 20130131090Abstract: The present invention provides novel dioxalate salt of lapatinib, process for its preparation and pharmaceutical compositions comprising it. The present invention also provides novel monobesylate salt of lapatinib, process for its preparation and pharmaceutical compositions comprising it. The present invention further provides a process for the preparation of monohydrate form of lapatinib ditosylate. The present invention further provides a process for the preparation of anhydrous form of lapatinib ditosylate.Type: ApplicationFiled: August 1, 2011Publication date: May 23, 2013Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivasa Rao, Bandi Vamsi Krishna
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Publication number: 20130109706Abstract: Quinazoline derivatives are provided that specifically inhibit proliferation of T cells without affecting the level of IL-2 secreted from said T cells. These compounds as well as pharmaceutical composition comprising them are useful for the treatment of indications mediated by T cell proliferation.Type: ApplicationFiled: January 27, 2011Publication date: May 2, 2013Applicant: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERSALEM LTD.Inventors: Alexander Levitzki, Idit Sagiv
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Publication number: 20130108697Abstract: There is provided a modified release dosage form comprising a core coated with a polymeric coat, said polymeric coat comprising one or more rate controlling polymers, said dosage form having a hole extending through the dosage form resulting in an inner radial surface and an outer radial surface, said core comprising at least one therapeutically active ingredient, characterized in that the inner radial surface is partially coated with said polymeric coat.Type: ApplicationFiled: March 2, 2011Publication date: May 2, 2013Inventors: Ramakant Kashinath Gundo, Rahul Sudhakar Dabre, Girish Kumar Jain
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Publication number: 20130102602Abstract: Provided is a compound of the formula I or a pharmaceutically acceptable salt, solvate or stereoisomer thereof: wherein Ar represents R5, R6, R7, R8, R1?, R2?, R3?, R4?, R5?, R6?, R7?, R8? independently represent H, OH, F, Cl, Br, C1 to C6 alkyl group, C1 to C6 alkoxy group, C2 to C6 alkenyl group, C2 to C6 alkenoxy group, C2 to C6 alkynyl group, C2 to C6 alkynoxy group, amine group, mono- or di-substituted amino group, cyclic C1 to C5 alkylamino group, imidazolyl group, morpholino group, piperazinyl group, optionally substituted with one or more hydroxy or halo; and X represents NH, O or S. The present invention also provides a composition comprising the compound of formula I. The compound and the composition in accordance with the present invention are effective on treating or alleviating a disease or disorder, such as malignant glioma.Type: ApplicationFiled: October 20, 2011Publication date: April 25, 2013Applicant: China Medical UniversityInventors: Mann-Jen Hour, Po-Wu Gean, Sheng-Chu Kuo, Hong-Zin Lee, Jai-Sing Yang, Li-Chen Chou, Tai-Lin Chen
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Publication number: 20130096145Abstract: The invention concerns the use of competitive AMPA receptor antagonists for the treatment, prevention or delay of progression of spasticity.Type: ApplicationFiled: June 24, 2011Publication date: April 18, 2013Applicant: Novartis AGInventor: Hans O. Kalkman
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Publication number: 20130090346Abstract: The invention concerns the use of competitive AMPA receptor antagonists for the treatment or prevention of photosensitive epilepsy.Type: ApplicationFiled: September 5, 2012Publication date: April 11, 2013Inventors: Donald Johns, Georges Imbert, Klaus Kucher
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Patent number: 8404697Abstract: The present invention relates to the use of quinazolines of formula (I), wherein the groups Ra to Rd have the meanings given in the claims and specification, in cancer therapy.Type: GrantFiled: November 9, 2006Date of Patent: March 26, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Flavio Solca, Andree Amelsberg, Gerd Stehle, Jacobus C. A. Van Meel, Anke Baum
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Publication number: 20130072507Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering N-{3-Chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methanesulphonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine, or a pharmaceutically acceptable hydrate and/or salt thereof, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, to a human in need thereof.Type: ApplicationFiled: May 19, 2011Publication date: March 21, 2013Inventors: Tona M. Gilmer, Rakesh Kumar
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Publication number: 20130072484Abstract: The present invention provides methods of killing, inhibiting the growth, and/or inhibiting the reproduction of kinetoplastid or apicomplexan protozoan with tyrosine kinase inhibitors.Type: ApplicationFiled: November 14, 2012Publication date: March 21, 2013Applicant: UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.Inventor: UNIVERSITY OF GEORGIA RESEARCH FOUND
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Publication number: 20130053381Abstract: The invention relates to a 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivative being (A) a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; or (B) a compound selected from a certain group of 2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl-sulfonamide derivatives disclosed in the specification; in free form or in salt form; to their preparation, to their use as medicament and to medicaments comprising them. In a first aspect, the invention provides prodrugs of AMPA receptor antagonists which potentially useful in the treatment of a wide range of disorders, particularly epilepsy.Type: ApplicationFiled: May 18, 2011Publication date: February 28, 2013Inventors: Yves Auberson, David Carcache, Andreas Lerchner, Joachim Nozulak
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Publication number: 20130052283Abstract: The invention generally relates to methods of treating a male subject with a prostate condition, for example, benign prostate hyperplasia (BPH). In certain embodiments, the invention provides methods of treating a male subject with a prostate condition, which include administering a MetAP2 inhibitor at a dose that does not substantially modulate angiogenesis.Type: ApplicationFiled: January 7, 2011Publication date: February 28, 2013Inventor: James E. Vath
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Publication number: 20130035350Abstract: This disclosure concerns novel quinazoline compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful anticancer agents, especially in inhibiting the function of the EGF receptor tyrosine kinases, HER1 tyrosine kinase, and HER2 tyrosine kinase. Thus, the disclosure also concerns a method of treating hyperproliferative diseases or conditions, such as various cancers and benign prostate hyperplasia (BPH), by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: December 21, 2010Publication date: February 7, 2013Inventors: Qiang Zhang, Hongwen Zhu
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Publication number: 20130029942Abstract: Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: ApplicationFiled: October 4, 2012Publication date: January 31, 2013Applicant: Myrexis, Inc.Inventor: Myrexis, Inc.