Polycyclo Ring System Having The Additional 1,3-diazine Ring As One Of The Cyclos Patents (Class 514/252.16)
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Patent number: 8198282Abstract: This invention relates to substituted azaquinazolines, to a process for their preparation, to pharmaceutical compositions containing them, and to their use for the treatment and/or prophylaxis of diseases, especially for use as antiviral agents, in particular against cytomegaloviruses.Type: GrantFiled: December 24, 2009Date of Patent: June 12, 2012Assignee: Aicuris GmbH & Co. KGInventors: Tobias Wunberg, Judith Baumeister, Mario Jeske, Frank Suessmeier, Holger Zimmermann, Kerstin Henninger, Dieter Lang
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Patent number: 8198281Abstract: The present invention relates to the crystalline forms of 2-allyl-1-[6-(I-hydroxy-1 methylethyl)pyridin-2-yl]-6-{[4-(4-methylpiperazin-1-yl)phenyl]amino}-1,2-dihydro-3H-pyrazolo[3,4-d]pyrimidin-3-one or a salt thereof, which are useful in the field of treatment of various cancers as a kinase inhibitor, especially as a Weel kinase inhibitor.Type: GrantFiled: April 22, 2008Date of Patent: June 12, 2012Assignee: Merck Sharp & Dohme Corp.Inventors: Masashi Kawasaki, Hiroo Mizuno, Toshihiro Sakamoto, Kimimasa Suzuki, Arlene E. McKeown
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Publication number: 20120141454Abstract: The present methods and compositions are of use for treatment of conditions involving fibrosis, such as Peyronie's disease plaque, penile corporal fibrosis, penile veno-occlusive dysfunction, Dupuytren's disease nodules, vaginal fibrosis, clitoral fibrosis, female sexual arousal disorder, abnormal wound healing, keloid formation, general fibrosis of the kidney, bladder, prostate, skin, liver, lung, heart, intestines or any other localized or generalized fibrotic condition, vascular fibrosis, arterial intima hyperplasia, atherosclerosis, arteriosclerosis, restenosis, cardiac hypertrophy, hypertension or any condition characterized by excessive fibroblast or smooth muscle cell proliferation or deposition of collagen and extracellular matrix in the blood vessels and/or heart.Type: ApplicationFiled: February 13, 2012Publication date: June 7, 2012Applicant: Los Angeles Biomedical Research Institute at Harbor-UCLA Medical CenterInventors: Nestor F. Gonzalez-Cadavid, Jacob Rajfer
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Publication number: 20120142680Abstract: The present invention relates to pyrimidine compounds that are useful as anti-proliferative agents. More particularly, the present invention relates to heteroalkyl linked and substituted pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative disorders including tumours and cancers as well as other conditions or disorders associated with kinases.Type: ApplicationFiled: February 13, 2012Publication date: June 7, 2012Applicant: S*BIO Pte Ltd.Inventors: Stephanie Blanchard, Kantharaj Ethirajulu, Cheng Hsia Angeline Lee, Harish Kumar Mysore Nagaraj, Anders Poulsen, Eric T. Sun, Yee Ling Evelyn Tan, Ee Ling Teo, Anthony Deodaunia William
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Patent number: 8193178Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: GrantFiled: September 12, 2008Date of Patent: June 5, 2012Assignee: Janssen Pharmaceutica NVInventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Patent number: 8193200Abstract: The present invention relates to method for treating inflammatory bowel disease that includes administration of an effective amount of an antagonist of A2B adenosine receptors (ARs).Type: GrantFiled: November 5, 2007Date of Patent: June 5, 2012Assignees: University of Virginia Patent Foundation, Emory UniversityInventors: Shanthi V. Sitaraman, Joel M. Linden, Guoquan Wang, Robert Douglas Thompson, Jayson M. Rieger
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Publication number: 20120135986Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: January 25, 2012Publication date: May 31, 2012Applicant: ARIAD Pharmaceuticals, Inc.Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antionette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
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Publication number: 20120134955Abstract: The invention is to provide a novel anticancer agent or sensitizer for cancer chemotherapy or radiotherapy. A compound of a general formula (I): wherein A means an aryl group or a heteroaryl group, or a group of a formula (a):; R1 means a —(C?O)aOb(C1-C6)alkyl group, a —(C?O)aOb(C2-C6)alkenyl group, a —(C?O)aOb(C3-C6)cycloalkyl group, an aryl group or a heteroaryl group; R2 and R3 each mean a hydrogen atom, a halogen atom, a hydroxyl group, a carboxyl group, a —(C?O)aOb(C1-C6)alkyl group or a group of —(C?O)aN(R1e)R2e; R4 means a hydrogen atom or a (C1-C6)alkyl group, and the like have an excellent Wee 1-kinase-inhibitory effect, and are therefore useful in the field of medicine, especially in the field of various cancer treatments.Type: ApplicationFiled: February 18, 2010Publication date: May 31, 2012Inventors: Yasuhiro Goto, Kenji Niyama, Satoshi Sunami, Keiji Takahashi
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Publication number: 20120128732Abstract: The present invention provides combination therapy methods of treating a proliferative disease (such as cancer) comprising a first therapy comprising administering to an individual an effective amount of a taxane in a nanoparticle composition, and a second therapy which may include the administration of an effective amount of at least one other agent that inhibits a pro survival and/or inflammatory signal.Type: ApplicationFiled: December 11, 2009Publication date: May 24, 2012Inventors: Vuong Trieu, Osmond D'Cruz, Neil P. Desai
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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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Publication number: 20120129868Abstract: Compounds of the following formula are provided for use with PARP: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.Type: ApplicationFiled: July 29, 2010Publication date: May 24, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Jason W. Brown, Anthony R. Gangloff, Andre A. Kiryanov
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Publication number: 20120128740Abstract: The present invention is directed to nanostructured (nanoparticulated) Sildenafil base, its pharmaceutically acceptable salts and co-crystals, compositions containing them, process for the preparation thereof and pharmaceutical compositions containing them. The nanoparticles of Sildenafil base, its pharmaceutically acceptable salts and co-crystals, compositions containing them according to the invention have an average particle size of less than about 500 nm. Sildenafil citrate is inhibiting cGMP specific phosphodiesterase type 5 (PDEV), an enzyme that regulates blood flow in the penis. The compositions of the invention are useful in the treatment of male or female sexual dysfunction and pulmonary arterial hypertension (PAH).Type: ApplicationFiled: June 18, 2010Publication date: May 24, 2012Inventors: Genovéva Filipcsei, Zsolt Ötvös, Katalin Pongrácz, Ferenc Darvas
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Publication number: 20120129807Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing scleroderma, keloids, UV injury, or sunburn, and methods for improving or preventing scar formation.Type: ApplicationFiled: October 20, 2011Publication date: May 24, 2012Inventors: Brydon L. Bennett, Brian Edwin Cathers, Kristen Lee Jensen-Pergakes, Heather Raymon, Weilin Xie, Jaman May Maroni
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Patent number: 8183248Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of Abl, Bcr-Abl, Bmx, BTK, b-RAF, c RAF, CSK, cSRC, Fes, FGFR3, Flt3, IKK?, IKK?, JNK1?1, JNK2?2, Lck, Met, MKK4, MKK6, p70S6K, PAK2, PDGFR?, PKA, PKC?, PKD2, ROCK-II, Ros, Rsk1, SAPK2?, SAPK2?, SAPK3, SAPK4, SGK, Syk, Tie2 and TrkB kinases.Type: GrantFiled: May 10, 2006Date of Patent: May 22, 2012Assignee: IRM LLCInventors: Advait Nagle, Nathanael Schiander Gray, Yi Liu, Pingda Ren, Taebo Sim, Shuli You
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Publication number: 20120122838Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: November 10, 2011Publication date: May 17, 2012Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
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Publication number: 20120122840Abstract: The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.Type: ApplicationFiled: September 23, 2011Publication date: May 17, 2012Applicant: Myrexis, Inc.Inventors: Dange Vijay Kumar, Ian A. McAlexander, Matthew Gregory Bursavich, Christophe Hoarau, Paul M. Slattum, David A. Gerrish, Jeffrey W. Lockman, Weston R. Judd, Michael Saunders, Daniel P. Parker, Daniel Feodore Zigar, In Chul Kim, J. Adam Willardsen, Kraig M. Yager, Mark D. Shenderovich, Brandi L. Williams, Keith D. Tardif
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Publication number: 20120114739Abstract: The present invention provides methods for inhibiting mTOR using pyrazolo[1,5-a]pyrimidine compounds and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with mTOR using such compounds.Type: ApplicationFiled: April 8, 2010Publication date: May 10, 2012Inventors: Yongqi Deng, Binyuan Sun, Hongbo Zeng, Matthew Richards, Gerald W. Shipps, JR., Cliff C. Cheng, Yinyan Zhao, Andrew McRiner, Zhaoyang Meng, Yang Nan, Mehul F. Patel, Iwona E. Wrona, Panduranga Adulla Reddy, Brian M. Eklov, Shuyi Tang, Duan Liu, Amit K. Mandal, Lianyun Zhao, M. Asshad Siddiqui
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Publication number: 20120115863Abstract: The invention relates to novel cycloalkyl- or cycloalkenyl-substituted pyrazolopyrimidinones of formula (I), wherein ? is selected from the group A1 consisting of a C3-C8-cycloalkyl group or a C4-C8-cycloalkenyl group, whereby the members of C3-C8-cycloalkyl group being selected from the group of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptanyl and cyclooctanyl; and the members of the C4-C8-cycloalkenyl group, being selected from cyclobutenyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, cyclooctenyl, cyclopentadienyl, cyclohexadienyl, cycloheptadienyl, cyclooctadienyl, cycloheptatrienyl, cyclooctathenyl, cyclooctatetraenyl. The new compounds shall be used for the manufacture of medicaments, in particular medicaments for improving perception, concentration, learning and/or memory in patients in need thereof.Type: ApplicationFiled: September 4, 2009Publication date: May 10, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Klaus Fuchs, Cornelia Dorner-Ciossek, Christian Eickmeier, Dennis Fiegen, Thomas Fox, Riccardo Giovannini, Niklas Heine, Martin Hendrix, Holger Rosenbrock, Gerhard Schaenzle
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Publication number: 20120115878Abstract: This invention relates to (1) process of making 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide and salts thereof; (2) novel salt(s) of 7-Cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-carboxylic acid dimethylamide; (3) pharmaceutical compositions comprising the same; and (4) methods of treatment using the same.Type: ApplicationFiled: November 8, 2011Publication date: May 10, 2012Inventors: John Vincent Calienni, Guang-Pei Chen, Baoqing Gong, Prasad Koteswara Kapa, Vishal Saxena
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Publication number: 20120115849Abstract: This disclosure is directed to treatment of addictions and primary impulse-control disorders using phosphodiesterase 7 (PDE7) inhibitors, alone or in combination with other therapeutic agents.Type: ApplicationFiled: November 7, 2011Publication date: May 10, 2012Inventors: Gregory A. Demopulos, George A. Gaitanaris
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Publication number: 20120114641Abstract: The present invention provides a combination comprising (a) a compound of formula (I) and (b) one or more antineoplastic agents selected from the group consisting of an antimetabolite agent, analkylating or alkylating-like agent, an intercalating agent, a topoisomerase I or II inhibitor, an antimitotic agent, a kinase inhibitor, a proteasome inhibitor and an antibody inhibiting a growth factor or its receptor, wherein active ingredients of the combination are present in each case in free form or in the form of a pharmaceutically acceptable salt or any hydrate or solvate thereof, useful in the treatment of tumors.Type: ApplicationFiled: May 21, 2010Publication date: May 10, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Barbara Valsasina, Italo Beria, Antonella Ciavolella, Dario Ballinari, Enrico Pesenti, Valter Domenico Croci, Mara Emanuela Casnaghi, Alessandro Luciano Croci, Juergen Moll
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Publication number: 20120115864Abstract: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.Type: ApplicationFiled: March 12, 2010Publication date: May 10, 2012Inventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
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Publication number: 20120108568Abstract: Compounds of Formula (I) and salts thereof in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.Type: ApplicationFiled: July 9, 2010Publication date: May 3, 2012Applicant: ARRAY BIOPHARMA INC.Inventors: Shelley Allen, Steven Wade Andrews, Kevin Ronald Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Kercher, Jeongbeob Seo
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Publication number: 20120108534Abstract: The invention relates to new dihydrothienopyrimidine of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2 and R3 have the meanings given in the description, and which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: ApplicationFiled: January 4, 2012Publication date: May 3, 2012Inventors: Pascale POUZET, Christoph HOENKE, Rolf GOEGGEL, Birgit JUNG, Peter NICKOLAUS, Dennis FIEGEN, Thomas FOX
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Publication number: 20120108604Abstract: A series of amine salts including a structure of formula (I) and formula (III) have provided. In formula I or formula (III), R1, Ra and RX are as defined in the specification. The amine complex salts disclosed in the present invention are characterized in a pro-drug active form and various pharmaceutical function.Type: ApplicationFiled: March 10, 2011Publication date: May 3, 2012Applicant: KAOHSIUNG MEDICAL UNIVERSITYInventor: Ing-Jun Chen
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Patent number: 8163755Abstract: The present invention provides mTOR inhibitors of the formula wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods of making the compounds and intermediates thereof; and methods of using the compounds.Type: GrantFiled: August 26, 2010Date of Patent: April 24, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Bohan Jin, Nicholas Scorah, Qing Dong
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Patent number: 8163753Abstract: The present invention provides a 2,3-dihydro-6-nitroimidazo[2,1-b]oxazole compound represented by the following general formula: (1) in the above formula (1), R1 represents a hydrogen atom or C1-C6 alkyl group, n represents an integer of 0 to 6, R1 and —(CH2)nR2 may form a spiro ring represented by the formula (30) below, together with the adjacent carbon atom (in the formula below, RRR represents a piperidyl group which may have substituents on the piperidine ring), (30) and R2 represents a benzothiazolyloxy group, quinolyloxy group, pyridyloxy group or the like. The present compound has an excellent bactericidal action against Mycobacterium tuberculosis, multi-drug-resistant Mycobacterium tuberculosis, and atypical acid-fast bacteria.Type: GrantFiled: October 29, 2004Date of Patent: April 24, 2012Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hidetsugu Tsubouchi, Hirofumi Sasaki, Motohiro Itotani, Yoshikazu Haraguchi, Shin Miyamura, Makoto Matsumoto, Hiroyuki Hashizume, Tatsuo Tomishige, Masanori Kawasaki, Kinue Ohguro, Takumi Sumida, Takeshi Hasegawa, Kazuho Tanaka, Isao Takemura
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Patent number: 8163754Abstract: Compounds of formula I in free or salt form, wherein R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: GrantFiled: October 21, 2005Date of Patent: April 24, 2012Assignee: Novartis AGInventors: Robin Alec Fairhurst, Roger John Taylor, Harinder Pal Singh
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Publication number: 20120094975Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, X1, X1, X3, L1 and L2 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or anomalous cell pro-liferation, and the use thereof in such a treatment.Type: ApplicationFiled: September 8, 2009Publication date: April 19, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Andreas Mantoulidis, Georg Dahmann, Peter Ettmayer, Christian Klein, Steffen Steurer, Irene Waizenegger, Stephan Karl Zahn
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Publication number: 20120094985Abstract: The invention relates to a pharmaceutical composition for treating serotonergic neurotransmission related disease or condition, including an effective amount of a chlorophenylpiperazine derived compound of Formula (I), or the pharmaceutically acceptable salt thereof. The pharmaceutical composition is safe and does not have side effect on lethargy.Type: ApplicationFiled: December 29, 2011Publication date: April 19, 2012Applicant: KAOHSIUNG MEDICAL UNIVERSITYInventor: Ing-Jun Chen
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Publication number: 20120094987Abstract: The invention relates to compounds of general formula (I); 1a, 1b, 1c and 1d. The invention also relates to a method for the production thereof, pharmaceutical preparations containing said compounds and/or physiologically compatible salts thereof which can be produced therefrom and/or solvates thereof, and to the pharmaceutical use of said compounds, salts or solvates thereof as inhibitors of phosphodiesterase 4. The compounds comprise active ingredients for the treatment of diseases which can have a positive influence by inhibiting the activity of phosphodiesterase 4 and/or TNF?-release, for example, in lymphocytes, eosinophile and basophile granulocytes, macrophages and mastocytes.Type: ApplicationFiled: October 3, 2011Publication date: April 19, 2012Inventors: Claudia Reichelt, Alexander Ludwig, Alexander Schulze, Mohammed Daghish, Siegfried Leistner, Andreas Krödel, Jochen Heinicke
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Publication number: 20120095005Abstract: A series of substituted pyrazolo[1,5-?][1,3,5]triazine and pyrazolo[1,5-?j-pyrimidine derivatives, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions. Formula (I).Type: ApplicationFiled: May 19, 2010Publication date: April 19, 2012Applicant: UCB PHARMA S.A.Inventors: Daniel Rees Allen, Julien Alistair Brown, Roland Burli, Alan Findlay Haughan, Barry John Langham, Mizio Matteucci, Andrew Pate Owens, Gilles Raphy, Andrew Sharpe
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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: 20120094999Abstract: The present invention relates to novel pyrimidine, pyrrolo-pyrimidine, pyrrolo-pyridine, pyridine, purine and triazine compounds which are able to modulate epidermal growth factor receptor (EGFR), including Her-kinases, and the use of such compounds in the treatment of various diseases, disorders or conditions.Type: ApplicationFiled: May 5, 2010Publication date: April 19, 2012Applicant: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Pasi Janne, Michael J. Eck, Wenjun Zhou
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Publication number: 20120095013Abstract: A pharmaceutical composition for improving a cardiac function is provided. The pharmaceutical composition comprises an effective amount of an active component being one of a KMUP-3 compound and a salt thereof.Type: ApplicationFiled: April 12, 2011Publication date: April 19, 2012Applicant: KAOHSIUNG MEDICAL UNIVERSITYInventor: Ing-Jun Chen
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Publication number: 20120088775Abstract: The present invention provides new pyrazolo-[1,5-a]-pyrimidone derivates and pharmaceutical compositions comprising said compounds and one or more pharmaceutically acceptable carriers or diluents. The uses of the compounds for the manufacture of potassium channel openers, anti-epilepsy medicaments, anti-anxiety medicaments and analgesic medicaments are also provided in the present invention.Type: ApplicationFiled: June 3, 2010Publication date: April 12, 2012Applicants: PEKING UNIVERSITY, HEBEI MEDICAL UNIVERSITYInventors: Hailin Zhang, Jinlong Qi, Diqun Zhang, Kewei Wang, Fan Zhang, Yan Fu, Yi Mi, Wen Xu, Xiaona Du, Yibing Wu, Qingzhong Jia, Shuangge Yang
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Publication number: 20120088753Abstract: The invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R1 is —NR7(CO)R11; R2 is aryl, heteroaryl, fused aryl-C3-6-heterocycloalkyl or fused heteroaryl-C3-6-heterocycloalkyl, each of which is optionally substituted; each R7 is selected from hydrogen, C1-6-alkyl and C3-7-cycloalkyl, wherein said C1-6-alkyl is optionally substituted by one or more halogens; each R11 is independently selected from C1-6-alkyl, C3-7-cycloalkyl, C1-6alkyl-C3-7-cycloalkyl, C?-heterocycloalkyl, aryl and heteroaryl, each of which may be optionally substituted. Further aspects of the invention relate to pharmaceutical compositions comprising the same, and methods for treating or preventing a disorder selected from cancer, septic shock, Primary open Angle Glaucoma (POAG), hyperplasia, rheumatoid arthritis, psoriasis, artherosclerosis, retinopathy, osteoarthritis, endometriosis, chronic inflammation and Alzheimer's disease.Type: ApplicationFiled: March 4, 2010Publication date: April 12, 2012Applicant: MEDICAL RESEARCH COUNCIL TECHNOLOGYInventors: Edward Giles Mciver, Joanne HOUGH, Joanne Hough
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Patent number: 8153628Abstract: The present invention provides compounds and pharmaceutical compositions that are substituted xanthines of formula I: or pharmaceutically acceptable salts thereof, wherein: Z is selected from the group consisting of oxazoyl, isoxazoyl, thiazolyl, and isothiazoyl; and Z1 is a 5-14 member substituted or unsubstituted heteroaryl ring; which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: July 22, 2009Date of Patent: April 10, 2012Assignee: Forest Laboratories Holdings LimitedInventors: Guoquan Wang, Jayson M Rieger, Robert D Thompson
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Publication number: 20120077819Abstract: The invention provides a low molecular weight ATP-competitive CDK inhibitor and TRKA inhibitor of formula (I) for use in the treatment of thymoma and thymic carcinoma. The compound can be administered together with one or more cytotoxic or cytostatic agents.Type: ApplicationFiled: March 15, 2010Publication date: March 29, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Angela Scaburri, Maria Adele Pacciarini, Marina Ciomei, Bernard Laffranchi, Silvia Comis
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Publication number: 20120076732Abstract: The invention provides for compounds that are phosphodiesterase inhibitors. The invention further provides for a method for screening compounds that bind to and modulate a phosphosdiesterase protein. The invention also provides methods for treating conditions associated with accumulated amyloid-beta peptide deposit accumulations by administering a phosphodiesterase-binding compound to a subject.Type: ApplicationFiled: June 23, 2011Publication date: March 29, 2012Inventors: Yan Feng, Ottavio Arancio, Shixian Deng, Donald W. Landry
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Patent number: 8143249Abstract: Disclosed are prodrugs of A2B adenosine receptor antagonists of the formula: wherein R1 and R2 are independently lower alkyl; R4 is optionally substituted phenyl; X is hydrogen or methyl; and Y is —C(O)R, in which R is optionally substituted aryl or optionally substituted heteroaryl or a pharmaceutically acceptable salt thereof, and their use in treating mammals for various disease states.Type: GrantFiled: January 21, 2011Date of Patent: March 27, 2012Assignee: Gilead Sciences, Inc.Inventors: Rao Kalla, Dmitry Koltun, Jeff Zablocki, Elfatih Elzein
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Publication number: 20120071489Abstract: The present invention relates to a compound represented by the formula wherein each symbol is as defined in the present specification, which has a superior RBP4-lowering action and is useful as a pharmaceutical composition for the prophylaxis or treatment of a disease or condition mediated by an increase in RBP4.Type: ApplicationFiled: April 16, 2010Publication date: March 22, 2012Inventors: Shizuo Kasai, Kevin Francis McGee, JR.
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Publication number: 20120071490Abstract: The present invention provides p70 S6 kinase inhibitors of the formula: pharmaceutical formulations comprising them, and methods for their use.Type: ApplicationFiled: November 30, 2011Publication date: March 22, 2012Applicant: ELI LILLY AND COMPANYInventors: Robert Dean Dally, Jianping Huang, Sajan Joseph, Timothy Alan Shepherd, Christian L. Holst
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Publication number: 20120071488Abstract: The invention relates to an orodispersible tablet comprising the components pharmaceutically acceptable sildenafil salt (a), polymeric adsorbent (b), in particular cation exchanger resin, sweetener (c), and flavoring (d) and, preferably, mucilage (e) and glidant (f).Type: ApplicationFiled: March 31, 2010Publication date: March 22, 2012Applicant: ratiopharm GmbHInventors: Sven Winter, Max-Werner Scheiwe
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Patent number: 8138172Abstract: The present invention provides 8-oxoadenine derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The 8-oxoadenine derivatives act as modulators of Toll-like Receptor (TLR) 7 and thus may be used in the treatment of asthma, hepatitis, allergic diseases, viral and bacterial infection as well as cancer.Type: GrantFiled: July 3, 2007Date of Patent: March 20, 2012Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co Ltd.Inventors: Anthony Cook, Tom McInally, Stephen Thom, Hiroki Wada
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Publication number: 20120065189Abstract: The present invention provides a novel heterocyclic compound. A heterocyclic compound represented by general formula (1) wherein, R1 and R2, each independently represent hydrogen; a phenyl lower alkyl group that may have a substituent(s) selected from the group consisting of a lower alkyl group and the like on a benzene ring and/or a lower alkyl group; or a cyclo C3-C8 alkyl lower alkyl group; or the like; R3 represents a lower alkynyl group or the like; R4 represents a phenyl group that may have a substituent(s) selected from the group consisting of a 1,3,4-oxadiazolyl group that may have e.g., halogen or a heterocyclic group selected from pyridyl group and the like; the heterocyclic group may have at least one substituent(s) selected from a lower alkoxy group and the like or a salt thereof.Type: ApplicationFiled: May 27, 2010Publication date: March 15, 2012Inventors: Akira Takahashi, Masaki Suzuki, Yuichi Nakamura, Yohji Sakurai
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Publication number: 20120065165Abstract: Compositions and methods of treating endothelial disorders, including: asthma, erectile dysfunction, pulmonary hypertension, cardiovascular disorders, and other disorders, using a synergistic combination of at least one arginase inhibitor and at least one phosphodiesterase (PDE1), (PDE2) and/or (PDE5) inhibitor are described.Type: ApplicationFiled: November 2, 2009Publication date: March 15, 2012Applicant: ARGINETIX, INCInventors: Simon E. Aspland, Dan E. Berkowitz, Trinity Bivalacqua, Hunter Champion
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Publication number: 20120065183Abstract: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.Type: ApplicationFiled: July 1, 2011Publication date: March 15, 2012Applicant: NOVARTIS AGInventors: Nigel Graham COOKE, Paulo FERNANDES GOMES DOS SANTOS, Nadege GRAVELEAU, Christina HEBACH, Klemens HOEGENAUER, Gregory John HOLLINGWORTH, Alexander Baxter SMITH, Nicolas SOLDERMANN, Frank STOWASSER, Ross STRANG, Nicola TUFILLI, Anette VON MATT, Romain WOLF, Frédéric ZECRI
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Publication number: 20120059000Abstract: Chemical compounds that modulate kinase activity, including PI3 kinase activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: May 20, 2011Publication date: March 8, 2012Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Alfredo C. Castro, Catherine A. Evans
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Publication number: 20120053182Abstract: The present invention provides a method for alleviating motor complications and motor indications in a patient suffering from moderate to severe Parkinson's disease by administering a composition which provides an effective amount of the compound of Formula I.Type: ApplicationFiled: January 13, 2010Publication date: March 1, 2012Applicant: SCHERING CORPORATIONInventors: Marc Cantillon, Susan B. Huyck, Kenneth P. Wolski