Piperidinyl Or Tetrahydropyridyl Patents (Class 514/266.22)
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Publication number: 20120329795Abstract: The invention concerns quinazoline derivatives of Formula I: wherein each of R1, X1, R2, R3, R5, n and m 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 antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of EGF and erbB receptor tyrosine kinases.Type: ApplicationFiled: September 10, 2012Publication date: December 27, 2012Inventors: Laurent Francois Andre Hennequin, Bernard Christophe Barlaam, Robert Hugh Bradbury
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Publication number: 20120329778Abstract: The present invention relates to bicyclic heterocycles of general formula wherein Ra to Rc, A to E and X are defined as in claim 1, the tautomers, stereoisomers and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.Type: ApplicationFiled: September 5, 2012Publication date: December 27, 2012Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank HIMMELSBACH, Elke LANGKOPF, Thomas METZ, Flavio SOLCA, Birgit JUNG, Anke BAUM
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Publication number: 20120315298Abstract: A method for treating a neurofibroma, e.g. dermal neurofibroma, a subdermal neurofibroma, or a superficial plexiform neurofibroma, in a subject in need of such treatment is disclosed. The method comprises locally applying a composition to a neurofibroma either topically or intralesionally. This method does not encompass systemic administration of the composition to the subject to have an effect on the neurofibromas. Compositions useful for such treatments and methods of preparing the compositions are disclosed.Type: ApplicationFiled: June 15, 2012Publication date: December 13, 2012Applicant: NEXGENIX PHARMACEUTICALS, INCInventors: Ruihong CHEN, Allan E. Rubenstein, Xiaodong Shen, Scott Stewart, Jin-Chen Yu
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Patent number: 8329712Abstract: Compounds having the formula I wherein R1, R2, R3 and X are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: GrantFiled: July 6, 2011Date of Patent: December 11, 2012Assignee: Roche Palo Alto LLCInventors: Ryan Craig Schoenfeld, Francisco Xavier Talamas, Leanna Renee Staben
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Publication number: 20120294930Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth.Type: ApplicationFiled: February 23, 2012Publication date: November 22, 2012Applicant: Intellikine LLCInventors: Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
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Patent number: 8314113Abstract: The invention relates to substituted dihydroquinazolines and to a method for the production thereof, the use thereof for treating and/or preventing diseases and for producing drugs for treating and/or preventing diseases, in particular for the use of the inventive dihydroquinazolines in the form of antiviral agents, in particular against cytomegaloviruses.Type: GrantFiled: October 28, 2004Date of Patent: November 20, 2012Assignee: Aicuris GmbH & Co. KGInventors: Tobias Wunberg, Judith Baumeister, Mario Jeske, Peter Nell, Susanne Nikolic, Frank Suessmeier, Holger Zimmermann, Rolf Grosser, Guy Hewlett, Jorg Keldenich, Dieter Lang, Kerstin Henninger
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Patent number: 8309544Abstract: The present invention relates to spiroindalone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.Type: GrantFiled: May 12, 2008Date of Patent: November 13, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Joan M. Fletcher, Jeffrey J. Hale, Shouwu Miao, Petr Vachal
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Patent number: 8309561Abstract: Specific phenylalanine derivatives and analogues thereof have an antagonistic activity to ?4 integrin. They are used as therapeutic agents for various diseases concerning ?4 integrin.Type: GrantFiled: December 21, 2007Date of Patent: November 13, 2012Assignee: Ajinomoto Co., Inc.Inventors: Kazuyuki Sagi, Tatsuya Okuzumi, Tatsuhiro Yamada, Shunsuke Kageyama, Yoichiro Shima, Tadakiyo Nakagawa, Munetaka Tokumasu, Masayuki Sugiki, Hajime Ito, Itsuya Tanabe, Tamotsu Suzuki, Akira Nakayama, Kazuyuki Ubukata, Kenji Shinkai, Yasuhiro Tanaka, Misato Noguchi, Ayatoshi Andou, Yoriko Yamamoto, Noriyasu Kataoka, Koichi Fujita
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Publication number: 20120270858Abstract: The invention provides isoquinoline, quinoline, and quinazoline derivatives to treat a variety of disorders, diseases and pathologic conditions, and more specifically to the use of isoquinoline, quinoline, and quinazoline derivatives to inhibit the hedgehog signaling pathway and to the use of those compounds to the treatment of hyperproliferative diseases and pathologic angiogenesis.Type: ApplicationFiled: June 9, 2010Publication date: October 25, 2012Applicant: CALIFORNIA CAPITAL EQUITY, LLCInventors: Chunlin Tao, Xiaowen Sun, Hongna Han, Lukasz Koroniak, Neil Desai
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Publication number: 20120270856Abstract: Disclosed are compounds of the following formula and their pharmaceutically-acceptable salts, which have an effect of glucokinase activation and are useful in the field of medicines for treatment for diabetes, obesity, etc. (wherein ring A represents a pyrazolyl group optionally having a lower alkyl group, etc.; ring B represents a heteroaryl group; R represents a lower alkyl group, etc.; R1 represents a group of a formula: (wherein R11 and R12 each independently represent a hydrogen atom, etc.; m indicates an integer of from 2 to 6), etc.; R2 represents a lower alkyl group, etc.; r indicates an integer of from 0 to 3; k indicates an integer of from 0 to 4).Type: ApplicationFiled: July 2, 2012Publication date: October 25, 2012Inventors: Tomoharu IINO, Akio OHNO, Norikazu OTAKE, Takuya SUGA, Masanori ASAI
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Publication number: 20120263802Abstract: The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal which is optionally being treated with ionising radiation, which comprises the administration of ZD6474 in combination with a platinum anti-tumour agent; to a pharmaceutical composition comprising ZD6474 and a platinum anti-tumour agent; to a combination product comprising ZD6474 and a platinum anti-tumour agent for use in a method of treatment of a human or animal body by therapy; and to a kit comprising ZD6474 and a platinum anti-tumour agent.Type: ApplicationFiled: November 10, 2011Publication date: October 18, 2012Inventors: Stephen Robert Wedge, Anderson Joseph Ryan
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Publication number: 20120263677Abstract: A method for the treatment of cancer comprising administration of a therapeutically effective amount of an intralesional chemoablative pharmaceutical composition, or variant of said composition, in combination with a therapeutically effective amount of a systemic immunomodulatory anticancer agent. A further method for the treatment of cancer comprising administration of a therapeutically effective amount of an intralesional chemoablative pharmaceutical composition, or variant of said composition, in combination with a therapeutically effective amount of a systemic targeted anticancer agent. The present invention is further directed to pharmaceutical compositions for treatment of cancer. The intralesional chemoablative pharmaceutical composition can comprise an IL chemoablative agent comprising primarily a halogenated xanthene.Type: ApplicationFiled: March 9, 2012Publication date: October 18, 2012Inventors: Craig J. Eagle, H. Craig Dees, Eric A. Wachter, Jamie Singer
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Patent number: 8283354Abstract: 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: August 31, 2005Date of Patent: October 9, 2012Assignee: 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: 20120252826Abstract: The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human, which is optionally being treated with ionising radiation, particularly a method for the treatment of a cancer, particularly a cancer involving a solid tumour, which comprises: the administration of ZD6474 in combination with 5-FU; ZD6474 in combination with CPT-11; or ZD6474 in combination with 5-FU and CPT-11.Type: ApplicationFiled: October 27, 2011Publication date: October 4, 2012Applicant: AstraZeneca ABInventors: Stephen Robert Wedge, Anderson Joseph Ryan
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Publication number: 20120252827Abstract: The present invention relates to a method for the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human, particularly a method for the treatment of a cancer involving a solid tumour, which comprises the administration of ZD6474 in combination with a taxane; to a pharmaceutical composition comprising ZD6474 and a taxane; to a combination product comprising ZD6474 and a taxane for use in a method of treatment of a human or animal body by therapy; to a kit comprising ZD6474 and a taxane; to the use of ZD6474 and a taxane in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human which is optionally being treated with ionising radiation.Type: ApplicationFiled: November 7, 2011Publication date: October 4, 2012Inventor: Stephen Robert WEDGE
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Publication number: 20120245139Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.Type: ApplicationFiled: June 4, 2012Publication date: September 27, 2012Applicant: EXELIXIS PATENT COMPANY LLCInventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
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Patent number: 8273757Abstract: The present invention is a novel analgesic combination and its use. It is classified to be an invention in the field of medicine and technology. The purpose of this invention is to solve the problem that existing analgesics does not effectively attenuate pain or produces serious side-effects in clinic. The ingredients of the analgesic combination include ketanserin and propranolol. This combination is used to make a drug to treat pain. Because the ingredients of the analgesic combination target peripheral receptors, the unwanted effects could be only minimal. The big advantage of this combination is that each of the ingredients acts on the different receptors producing the synergizing analgesic. Therefore, the analgesia that the combination produces is remarkable and the effective doses are low.Type: GrantFiled: August 30, 2010Date of Patent: September 25, 2012Inventor: Yanguo Hong
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Publication number: 20120238570Abstract: The present invention is directed to a compound of Formula I or a single isomer thereof; where the compound is optionally as a pharmaceutically acceptable salt, hydrate, solvate or combination thereof, in addition to methods of preparing a Compound of Formula I, and methods of using a Compound of Formula I to treat cancer.Type: ApplicationFiled: June 4, 2012Publication date: September 20, 2012Applicant: EXELIXIS PATENT COMPANY LLCInventors: Suleyman Bahceci, William Bajjalieh, Jeff Chen, Sergey Epshteyn, Timothy Patrick Forsyth, Tai Phat Huynh, Byung Gyu Kim, James W. Leahy, Matthew Sangyup Lee, Gary L. Lewis, Morrison B. Mac, Grace Mann, Charles K. Marlowe, Brian Hugh Ridgway, Joan C. Sangalang, Xian Shi, Craig Stacy Takeuchi, Yong Wang
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Patent number: 8268841Abstract: Quinazoline derivatives of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.Type: GrantFiled: April 28, 2009Date of Patent: September 18, 2012Assignee: Astrazeneca ABInventors: Nicola Murdoch Heron, Andrew Austen Mortlock, Frederic Henri Jung, Georges Rene Pasquet
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Publication number: 20120230983Abstract: Provided herein are methods of treating, preventing and/or managing cancers, which comprise administering to a patient 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, or an enantiomer or a mixture of enantiomers thereof, or a pharmaceutically acceptable salt, solvate, hydrate, co-crystal, clathrate, or polymorph thereof.Type: ApplicationFiled: March 9, 2012Publication date: September 13, 2012Inventors: George W. Muller, Peter H. Schafer, Hon-Wah Man, Ling-Hua Zhang, Anita Gandhi, Rajesh Chopra
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Publication number: 20120232100Abstract: Solid forms comprising 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosedType: ApplicationFiled: March 9, 2012Publication date: September 13, 2012Inventors: George Muller, Hon-Wah Man, Benjamin M. Cohen, Ying Li, Jean Xu, William W. Leong
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Publication number: 20120225872Abstract: A method of preparing a compound of formula (I), A method for treating cancer or inhibiting growth of cancer cells including administering to a patient mammal in need thereof a pharmaceutical preparation including the compound. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal including administering to a mammal a pharmaceutical preparation including the compound.Type: ApplicationFiled: May 11, 2012Publication date: September 6, 2012Inventor: Hesheng ZHANG
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Patent number: 8242126Abstract: The invention relates to quinazolinedione derivatives of the general formula (I): wherein A, R1, R2, R3, R4, m, n, p, p?, and r are as defined herein, processes for the preparation thereof and their therapeutic applications.Type: GrantFiled: April 5, 2010Date of Patent: August 14, 2012Assignee: SanofiInventors: Annie Clauss, Christophe Glaess, Gilbert Marciniak, Nicolas Muzet, Jean-Francois Nave, André Seyer, Bertrand Vivet
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Patent number: 8227476Abstract: The invention relates to a method for the treatment of obesity and related diseases comprising the administration of a therapeutically effective amount of Flibanserin.Type: GrantFiled: July 31, 2006Date of Patent: July 24, 2012Assignee: Sprout Pharmaceuticals, Inc.Inventors: Angelo Ceci, Marcus Schindler
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Publication number: 20120184522Abstract: A subject-matter of the present invention is the use of compounds of formula (I) in the base, hydrate or solvate form or in the form of their mixtures, as medicaments or for the preparation of medicaments intended for the treatment of at least one cardiovascular disease and/or to prevent the appearance of at least one cardiovascular disease.Type: ApplicationFiled: October 7, 2011Publication date: July 19, 2012Applicant: SANOFIInventors: Philip JANIAK, Gilbert MARCINIAK, Jean-Francois NAVE, Fabrice VIVIANI
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Patent number: 8217029Abstract: The invention relates to compounds of formula (I) wherein U, V, W, X, R1, R2, R3, R4, R5, R6, A, B, D, E, G, m, and n are as defined in the description, to pharmaceutically acceptable salts of such compounds for use in the manufacture of a medicament for the prevention or treatment of a bacterial infection. Certain compounds of formula (I) are new and are also part of this invention.Type: GrantFiled: April 11, 2008Date of Patent: July 10, 2012Assignee: Actelion Pharmaceuticals LtdInventors: Daniel Bur, Christian Hubschwerlen, Georg Rueedi, Jean-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20120172365Abstract: The present invention pertains to the use of inhibitors of phosphodiesterase I, IV and V for the prophylaxis and treatment of prostatic diseases, in particular the use of a) 2-(2-propoxy- phenyl)-8-azapurin-6-one (zaprinast); b) dipyridamole; c) 1-(3-chlorophenylamino)-4-phenylphthalazine (M5445); d) 2-(N-(4-carboxypiperidine-6-chloro-4-(3,4-(methylendioxy)benzyl)amino)quinazoline (E 4021, ER 21355); e) 2,3-dihydro-8-hydroxy-7-nitro-1,4-benzodioxine-2-methanol, alpha-nitrate (E 4701); f) 4-((3,4-(methylendioxy)benzyl)amino)-6,7,8-trimethoxy-quinazoline; g) 1-methly-3-propyl-6-(5-(N-(4-methylmorpholino)sulfonyl)-2-ethoxyphenyl)pyrazole[4,5]pyrimidin-4(5H)one (sildenafil); i) 1-cyclopentyl-3-methyl-6-(4-pyridinyl)pyrazolo(3,4-d)pyrimidin-4(5H)-one (WIN 58237); j) 7-(3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxypropoxy)-2-carboxy-2,3-didehydro-chronan-4-one (PPL-557212); k).Type: ApplicationFiled: December 29, 2011Publication date: July 5, 2012Inventors: Wolf-Georg Forssmann, Christian Georg Steif, Michael Carsten Truß, Stefan Uckert, Udo Jonas
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Publication number: 20120149698Abstract: The present invention relates to new CGRP-antagonists of general formulae Ia and Ib wherein R1, R2, R3, R4 and R5 are defined as mentioned below, the tautomers, the isomers, the diastereomers, the enantiomers, the hydrates, the mixtures and the salts thereof as well as the hydrates of the salts, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof.Type: ApplicationFiled: November 21, 2008Publication date: June 14, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Dirk Gottschling, Georg Dahmann, Henri Doods, Annekatrin Heimann, Stephan Georg Mueller, Klaus Rudolf, Gerhard Georg Schaenzle, Dirk Stenkamp
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Publication number: 20120130144Abstract: In one aspect, the present invention provides a method of treating lung cancer, comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor. In another aspect, the present invention provides a method of treating non-small cell lung cancer comprising administering to a subject at least one PARP inhibitor in combination with at least one growth factor inhibitor.Type: ApplicationFiled: February 4, 2010Publication date: May 24, 2012Applicant: BiPar Sciences, Inc.Inventors: Barry M. Sherman, Charles Bradley, Valeria S. Ossovskaya
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Patent number: 8178531Abstract: The present invention relates to antiviral compounds of formula (I), compositions containing these compounds, processes for their preparation, intermediates in their synthesis, and their use as therapeutics for prevention of organ transplantation rejection, the treatment of immune disorders and inflammation, and treatment of viral (particularly hepatitis C viral) infection.Type: GrantFiled: February 23, 2011Date of Patent: May 15, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Guoqiang Wang, Xuri Gao
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Publication number: 20120108570Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.Type: ApplicationFiled: January 6, 2012Publication date: May 3, 2012Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventors: Miodrag Radulovacki, David W. Carley
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Publication number: 20120107304Abstract: The invention relates to new methods for the treatment of oncological and fibrotic disease comprising the combined administration of a cell signalling and/or angiogenesis inhibitor in conjunction with an Aurora kinase inhibitor.Type: ApplicationFiled: April 19, 2011Publication date: May 3, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Flavio Solca, Ulrich Guertler, Ulrike Tontsch-Grunt
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Publication number: 20120095006Abstract: This invention relates to the use of certain cyclic guanosine 3?,5?-monophosphate phosphodiesterase type five (cGMP PDE5) inhibitors, including in particular the compound sildenafil, for the treatment of pulmonary hypertension.Type: ApplicationFiled: December 16, 2011Publication date: April 19, 2012Inventors: Ghazwan Saleem Butrous, Timothy Michael Lukas, Ian Machin
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Publication number: 20120095010Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.Type: ApplicationFiled: December 22, 2011Publication date: April 19, 2012Inventors: John R. Carson, Ellen Codd, Christine M. Razler, Andrea Works, Mark McDonnell, James J. McNally
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Publication number: 20120095030Abstract: Methods of using specific microRNA to identify subjects with non-small cell lung cancer likely or unlikely to respond to treatment with tyrosine kinase inhibitors such as erlotinib, sunitinib, or vandetanib; methods of treating subjects based on identification of said subjects as likely to respond to treatment with tyrosine kinase inhibitors; and kits that facilitate the performance of the methods are disclosed.Type: ApplicationFiled: April 19, 2010Publication date: April 19, 2012Applicant: THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTEInventor: Glen Weiss
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Publication number: 20120094997Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, Ra, R2a, R2b, R1, and X have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: October 14, 2011Publication date: April 19, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Dylan B. England, Kenneth M. Gigstad, Alexandra E. Gould, Liting Ma, He Xu
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Patent number: 8153642Abstract: 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: GrantFiled: March 1, 2010Date of Patent: April 10, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jesus Gonzalez, III, Dean Wilson, Andreas Termin, Peter Grootenhuis, Yulian Zhang, Benjamin Petzoldt, Lev Fanning, Timothy Neubert, Roger Tung, Esther Martinborough, Nicole Hilgraf
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Publication number: 20120077811Abstract: The invention provides novel prodrug compounds comprising a kinase inhibitor and a reductively-activated fragmenting aromatic nitroheterocycle or aromatic nitrocarbocycle trigger, where the compound carries a positive charge. In preferred embodiments, the compounds are of Formula I: where: X is any negatively charged counterion; R1 is a group of the formula —(CH2)nTr, where Tr is an aromatic nitroheterocycle or aromatic nitrocarbocycle and —(CH2)nTr acts as a reductively-activated fragmenting trigger; and n is an integer from 0 to 6; R2, R3 and R4 may each independently be selected from aliphatic or aromatic groups of a tertiary amine kinase inhibitor (R2)(R3)(R4)N, or two of R2, R3, and R4 may form an aliphatic or aromatic heterocyclic amine ring of a kinase inhibitor, or one of R2, R3 and R4 may be absent and two of R2, R3 and R4 form an aromatic heterocyclic amine ring of a kinase inhibitor. The compounds of the invention are useful in treating proliferative diseases such as cancer.Type: ApplicationFiled: March 11, 2010Publication date: March 29, 2012Inventors: Jeffrey Bruce Smaill, Adam Vorn Patterson, Michael Patrick Hay, William Alexander Denny, William Robert Wilson, Guo-Liang Lu, Robert Forbes Anderson, Ho Huat Lee, Amir Ashoorzadeh
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Publication number: 20120065216Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, L1, L2, X, Y and Z have defined meanings.Type: ApplicationFiled: November 17, 2011Publication date: March 15, 2012Inventors: Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
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Publication number: 20120065188Abstract: Compounds of the general Formula I, wherein X1, X2, X3, X4, X5, X6, X7, R1, R2, R4, R5, R6, R7, R8, R9, R10, Y1, n, m, p and q are defined as above, their preparation and their use as antimicrobial agents.Type: ApplicationFiled: November 22, 2011Publication date: March 15, 2012Inventors: Steven Joseph Brickner, Jinshan Michael Chen, Zhengong Bryan Li, Anthony Marfat, Mark Joseph Mitton-Fry, Michael A. Plotkin, Usa Datta Reilly, Chakrapani Subramanyam, Zhijun Zhang, Shaughnessy Robinson
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Publication number: 20120064025Abstract: Compounds, pharmaceutical compositions and methods for modulating the activity of nuclear receptors are provided. In particular, quinazolinones are provided for modulating the activity of farnesoid X receptor (FXR) and/or orphan nuclear receptors.Type: ApplicationFiled: September 28, 2011Publication date: March 15, 2012Applicant: EXELIXIS, INC.Inventors: Richard Martin, Jeffrey D. Kahl, Brenton T. Flatt, Ronald Griffith
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Publication number: 20120058987Abstract: The subject matter of the present invention is the use of compounds of formula (I) in the form of a base, a hydrate or a solvate, or of mixtures thereof, as a medicament or for preparing a medicament intended for the treatment and/or prevention of disorders associated with the central nervous system (abbreviated to CNS) and/or associated with the peripheral nervous system (abbreviated to PNS).Type: ApplicationFiled: March 25, 2010Publication date: March 8, 2012Applicant: SANOFIInventors: Gilbert Marciniak, Jean-Francois Nave, Fabrice Viviani
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Publication number: 20120046300Abstract: The present invention relates to compounds of the formula I: wherein: ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which moiety may be saturated or unsaturated, which may be aromatic or non-aromatic, and which optionally may contain 1-3 heteroatoms selected independently from O, N and S; is —O— —NH— or —S—; is 0, 1, 2, 3, 4 or 5; is 0, 1, 2 or 3; and R2 and R1 are as defined herein; and salts thereof; their use in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals; processes for the preparation of such compounds; pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof and methods of treating disease states involving angiogenesis by administering a compound of formula I or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 20, 2011Publication date: February 23, 2012Inventor: Laurent Francois Andre Hennequin
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Publication number: 20120046269Abstract: The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: February 4, 2010Publication date: February 23, 2012Applicant: Merck Patent GmbHInventors: Amanda E. Sutton, Ruoxi Lan, Thomas E. Richardson, David Perrey, Harold George Vandeveer, Bayard R. Huck, Srinivasa R. Karra, Xiaoling Chen, Lesley Liu-Bujalski, Andreas Goutopoulos, Frank Steiber, Brian L. Hodous, Hui Qiu, Reinaldo C. Jones, Brian H. Heasley
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Publication number: 20120040980Abstract: The present invention relates to quinazolinone compounds, processes for their preparation and their use as pharmaceutical agents for the treatment of Parkinson's disease (PD). The quinazolinone compounds are of general formula (I).Type: ApplicationFiled: December 23, 2009Publication date: February 16, 2012Applicant: PRANA BIOTECHNOLOGY LIMITEDInventors: Penelope Jane Huggins, Jack Gordon Parsons
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Publication number: 20120040935Abstract: 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: ApplicationFiled: May 18, 2011Publication date: February 16, 2012Applicant: Vertex Pharmaceuticals, Inc.Inventors: Dean M. Wilson, Andreas P. Termin, Timothy D. Neubert, Jian Wang, Yulian Zhang, Jesus E. Gonzalez, III, Esther Martinborough, Nicole Zimmerman
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Patent number: 8106061Abstract: The present invention pertains to the use of inhibitors of phosphodiesterase I, IV and V for the prophylaxis and treatment of prostatic diseases, in particular the use of a) 2-(2-propoxy-phenyl)-8-azapurin-6-one (zaprinast); b) dipyridamole; c) 1-(3-chlorophenylamino)-4-phenylphthalazine (M5445); d) 2-(N-(4-carboxypiperidine-6-chloro-4-(3,4-(methylen-dioxy)benzyl)amino)quinazoline (E 4021, ER 21355); e) 2,3-dihydro-8-hydroxy-7-nitro-1,4-benzodioxine-2-methanol, alpha-nitrate (E 4701); f) 4-((3,4-(methylendioxy)benzyl)amino)-6,7,8-trimethoxy-quinazoline; g) 1-methyl-3-propyl-6-(5-(N-(4-methylmorpholino)sulfonyl)-2-ethoxyphenyl)pyrazole[4,5]pyrimidin-4(5H)one (sildenafil); i) 1-cyclopentyl-3-methyl-6-(4-pyridinyl)pyrazolo (3,4-d)pyrimidin-4(5H)-one (WIN 58237); j) 7-(3-(4-acetyl-3-hydroxy-2-propyl-phenoxy)-2-hydroxy-propoxy)-2-carboxy-2,3-didehydro-chronan-4-one (FPL-557212); k) quinazolines and their trimethoxy derivatives; l) Pyrazolopyrimidones; as well as pharmacologically compatible salts thereof, quiType: GrantFiled: May 23, 2003Date of Patent: January 31, 2012Assignee: Uropep Biotech GBRInventors: Wolf-Georg Forssmann, Christian Georg Stief, Michael Carsten Truss, Stefan Uckert, Udo Jonas
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Publication number: 20120020881Abstract: This invention relates to novel compounds suitable for labeling by positron emitting isotopes, such as 18F, 11C, 13N and 15O, through appropriate labeling reagents, such as 18F reagents and methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).Type: ApplicationFiled: December 4, 2009Publication date: January 26, 2012Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Lutz Lehmann, Timo Stellfeld, Keith Graham, Jessica Becaud, Linjing Mu
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Publication number: 20110319434Abstract: The present invention relates to novel Bicyclic Heterocyclic Derivatives, pharmaceutical compositions comprising the Bicyclic Heterocyclic Derivatives and the use of these compounds for treating or preventing treating allergy, an allergy-induced airway response, congestion, a cardiovascular disease, an inflammatory disease, a gastrointestinal disorder, a neurological disorder, a cognitive disorder, a metabolic disorder, obesity or an obesity-related disorder, diabetes, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: ApplicationFiled: December 18, 2009Publication date: December 29, 2011Applicant: Schering Plough CorporationInventors: Anandan Palani, Ashwin U. Rao, Xiao Chen, Ning Shao, Ying R. Huang, Robert G. Aslanian
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Patent number: RE43431Abstract: A compound of general formula I wherein: Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino, N-methyl-N-ethylamino, diethylamino, N-methyl-N-isopropylamino, N-methyl-N-cyclopropylamino, N-methyl-N-(2-methoxyethyl)amino, N-ethyl-N-(2-methoxyethyl)amino, bis(2-methoxyethyl)amino, morpholino, N-methyl-N-(tetrahydrofuran-3-yl)amino, N-methyl-N-(tetrahydrofuran-2-ylmethyl)amino, N-methyl-N-(tetrahydrofuran-3-ylmethyl)amino, N-methyl-N-(tetrahydropyran-4-yl)amino, or N-methyl-N-(tetrahydropyran-4-ylmethyl)amino group; and Rc is a cyclopropylmethoxy, cyclobutyloxy, cyclopentyloxy, tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a tautomer, stereoisomer, or salt thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction medType: GrantFiled: August 18, 2009Date of Patent: May 29, 2012Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Frank Himmelsbach, Elke Langkopf, Stefan Blech, Birgit Jung, Anke Baum, Flavio Solca