Plural 1,3-diazine Rings Patents (Class 544/296)
-
Patent number: 8349833Abstract: The invention relates to classes of pharmaceutically-active heterocyclic compounds and pharmaceutically acceptable salts, and hydrates thereof, and compositions comprising the same. The invention also relates to methods for treating or preventing a disease or disorder, which comprises administering a therapeutically or prophylactically effective amount a compound described herein.Type: GrantFiled: October 18, 2011Date of Patent: January 8, 2013Assignee: Cerenis Therapeutics Holding SAInventors: Daniela Carmen Oniciu, Jean-Louis Henri Dasseux, Ronald Barbaras, Valery Kochubey, Dmitry Kovalsky, Oleg Gennadievich Rodin, Otto Geoffroy, Anna Rzepiela
-
Publication number: 20130004457Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: ApplicationFiled: September 11, 2012Publication date: January 3, 2013Inventors: Carol Bachand, Makonen Bekema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
-
Publication number: 20120329784Abstract: Disclosed are compounds having the formula: wherein R1, R2, R3, R4, R5, and R6 are as defined herein, and methods of making and using the same.Type: ApplicationFiled: January 11, 2011Publication date: December 27, 2012Inventors: Lara S. Kallander, Brian Griffin Lawhorn, Joanne Philp, Yongdong Zhao
-
Publication number: 20120329807Abstract: Disclosed are conjugates which bind VLA-4. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such conjugates are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The conjugates can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: ApplicationFiled: September 7, 2012Publication date: December 27, 2012Applicant: ELAN PHARMACEUTICALS, INC.Inventors: Andrei Konradi, Michael A. Pleiss, Christopher M. Semko, Theodore Yednock, Jenifer L. Smith
-
Publication number: 20120322795Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, C, R1a, R1b, R2, R3, R4a and R4b are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: December 14, 2011Publication date: December 20, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela BERRY, Zhidong CHEN, Stephane DE LOMBAERT, Michel Jose EMMANUEL, Pui Leng LOKE, Chuk Chui MAN, Tina Marie MORWICK, Hidenori TAKAHASHI
-
Patent number: 8334291Abstract: The present application relates to novel aliphatically substituted pyrazolopyridines, to processes for their preparation, to their use, alone or in combination, for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.Type: GrantFiled: December 8, 2009Date of Patent: December 18, 2012Assignee: Bayer Intellectual Property GmbHInventors: Hartmut Schirok, Nils Griebenow, Chantal Fürstner, Joachim Mittendorf, Johannes-Peter Stasch, Frank Wunder, Stefan Heitmeier
-
Publication number: 20120316171Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.Type: ApplicationFiled: November 4, 2010Publication date: December 13, 2012Inventor: Tamas Oravecz
-
Publication number: 20120316155Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), the TGF? pathway and/or the Wnt pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), the TGF? pathway and/or the Wnt pathway.Type: ApplicationFiled: February 17, 2011Publication date: December 13, 2012Applicant: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger
-
Patent number: 8329390Abstract: The present invention relates generally to the detection and measurement of transmembrane potentials using an N,N,N?-trialkyl thiobarbituric acid-derived polymethine oxonol (shown below). In particular, the present invention is directed to compositions and optical methods for determining transmembrane potentials across the plasma membrane of biological cells using a slightly hydrophobic N,N,N?-trialkyl thiobarbituric acid-derived polymethine oxonols. The method comprises a slightly hydrophobic N,N,N?-trialkyl thiobarbituric acid-derived polymethine oxonol anion capable of redistributing from a first face of the membrane to a second face of the membrane in response to changes in the potential of the membrane. In one aspect the method is used to identify compounds which modulate membrane potentials in biological membranes.Type: GrantFiled: August 25, 2005Date of Patent: December 11, 2012Assignee: AnaSpec IncorporatedInventors: Zhenjun Diwu, Jianjun He, Yi Tang
-
Patent number: 8329725Abstract: The invention relates to annelated pyrrolidin sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: GrantFiled: May 22, 2009Date of Patent: December 11, 2012Assignee: SanofiInventors: Stefanie Keil, Matthias Urmann, Wolfgang Wendler, Ulrike Wendler, Maike Glien, Hans Matter, Eugen Falk
-
Publication number: 20120309735Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.Type: ApplicationFiled: December 16, 2010Publication date: December 6, 2012Inventors: Michael D. Altman, Kenneth L. Arrington, Jason Burch, Bernard Cote, Jean-Francois Fournier, Jacques Yves Gauthier, Solomon Kattar, Sandra Lee Knowles, Jongwon Lim, Michelle R. Machacek, Alan B. Northrup, Michael H. Reutershan, Joel S. Robichaud, Adam J. Schell, Kerrie B. Spencer
-
Publication number: 20120305851Abstract: The present invention relates to compounds of the formula (1) which are suitable for use in electronic devices, in particular organic electroluminescent devices, and to electronic devices which contain these compounds.Type: ApplicationFiled: December 17, 2010Publication date: December 6, 2012Applicant: Merck Patent GmbHInventors: Junyou Pan, Herwig Buchholz, Teresa Mujica-Fernaud, Irina Martynova
-
Patent number: 8324234Abstract: The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a compound represented by formula (1) or a pharmacologically acceptable salt thereof: wherein, R1, R3, R4, and R6 are each independently C1-3 alkyl; and R2 and R5 are each independently a hydrogen atom or C1-3 alkyl.Type: GrantFiled: February 6, 2009Date of Patent: December 4, 2012Assignee: Shiseido Company Ltd.Inventors: Naoto Hanyu, Tomoko Saito, Takako Shibata, Kiyoshi Sato, Kimihiro Ogino
-
Patent number: 8324232Abstract: The invention relates to the compound of structural formula (I) and the salts thereof. Said compound is useful as endothelin receptor antagonist. The invention further relates to a process for preparing said compound.Type: GrantFiled: August 15, 2008Date of Patent: December 4, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, Christoph Boss, Alexander Treiber
-
Publication number: 20120298975Abstract: A material for organic electroluminescence devices comprising a compound in which a heterocyclic group having nitrogen is bonded to an arylcarbazolyl group or a carbazolylalkylene group and an organic electroluminescence device comprising an anode, a cathode and an organic thin film layer comprising at least one layer and disposed between the anode and the cathode, wherein at least one layer in the organic thin film layer comprises the material for organic electroluminescence devices described above. The material can provide an organic electroluminescence device emitting bluish light with a high purity of color. The organic electroluminescence device uses the material.Type: ApplicationFiled: May 31, 2012Publication date: November 29, 2012Applicant: Idemitsu Kosan Co., Ltd.Inventors: Toshihiro IWAKUMA, Hiroshi Yamamoto, Yoshio Hironaka, Hidetsugu Ikeda, Chishio Hosokawa, Seiji Tomita, Takashi Arakane
-
Publication number: 20120295896Abstract: The present invention relates to compounds of formula (I) and (IA): and pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: September 20, 2011Publication date: November 22, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, Jonathon Alan DINES, John D. HUBER, Weimin W. LIU, Pui Leng LOKE, Tina Marie MORWICK, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
-
Publication number: 20120289525Abstract: The present invention relates to Pyrimidine Ether Derivatives, compositions comprising a Pyrimidine Ether Derivative, and methods of using the Pyrimidine Ether Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of a G-protein coupled receptor (GPCR) in a patient.Type: ApplicationFiled: November 16, 2010Publication date: November 15, 2012Inventors: Santhosh Francis Neelamkavil, Andrew Stamford, Samuel Chackalamannil, William J. Greenlee
-
Patent number: 8309126Abstract: The invention relates to dispersible tablets comprising the compound 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(pyrimidin-2-yl)-pyrimidin-4-yl]-benzenesulfonamide.Type: GrantFiled: June 7, 2011Date of Patent: November 13, 2012Assignee: Actelion Pharmaceuticals, Ltd.Inventors: Lovelace Holman, Timm Trenktrog
-
Publication number: 20120283440Abstract: The present invention relates to crystalline forms of bosentan salts and processes for their preparation.Type: ApplicationFiled: November 12, 2010Publication date: November 8, 2012Applicant: RANBAXY LABORATORIES LIMITEDInventors: Rakesh Singh, Anu Mittal, Gopal Singh Bisht, Mahavir Singh Khanna, Rajesh Kumar Thaper, Mohan Prasad
-
Publication number: 20120283219Abstract: The present invention relates novel diaminopteridine derivatives, their compositions and method of treatment comprising the same for use as anti-infectives.Type: ApplicationFiled: March 25, 2010Publication date: November 8, 2012Inventors: Philip D.G. Coish, Phil Wickens, Brian R. Dixon, David Osterman, Uday R. Khire, Manuel Navia, Judd Berman, Harpreet Kaur, Jeffrey Wilson, Dennis Underwood
-
Patent number: 8303944Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: February 13, 2008Date of Patent: November 6, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
-
Patent number: 8288402Abstract: The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: GrantFiled: December 9, 2008Date of Patent: October 16, 2012Assignee: Bayer Intellectual Property GmbHInventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig, Jens Schamberger
-
Patent number: 8288401Abstract: Novel polymorphic forms of bosentan and processes for their preparation are disclosed. Further, pharmaceutical compositions comprising said polymorphic forms and the use of said compositions in the treatment of patients suffering from endothelin receptor mediated disorders, for example, cardiovascular disorders such as hypertension, pulmonary hypertension, ischemia, vasospasm and angina pectoris are disclosed.Type: GrantFiled: May 8, 2008Date of Patent: October 16, 2012Assignee: Generics [UK] LimitedInventors: Abhay Gaitonde, Bindu Manojkumar, Sandeep Mekde, Dattaatraya Shinde, Prakash Bansode
-
Publication number: 20120256174Abstract: A compound for an organic photoelectric device, the compound being represented by Chemical Formula 1 or 2:Type: ApplicationFiled: June 18, 2012Publication date: October 11, 2012Inventors: Sung-Hyun JUNG, Myeong-Soon KANG, Ho-Kuk JUNG, Nam-Soo KIM, Nam-Heon LEE, Eui-Su KANG, Dong-Min KANG, Mi-Young CHAE
-
Publication number: 20120252818Abstract: The present subject matter relates to a compound represented by the general formula (I) or (I?) or a pharmacologically acceptable salt thereof; pharmaceutical compositions containing at least one of these compounds; methods of making at least one of these compounds; methods of using at least one of these compounds for treating and/or preventing various cancers and/or proliferation disorders; methods of using at least one of these compounds for monitoring the effectiveness of an anticancer therapy against various cancers. In one embodiment, the subject matter relates to compounds that bind with a level of specificity to heat shock protein 70 (Hsp70). In another embodiment, the subject matter relates to compounds that bind with a level of specificity to inhibit both heat shock protein 70 (Hsp70) and heat shock cognate protein 70 (Hsc70).Type: ApplicationFiled: August 17, 2010Publication date: October 4, 2012Applicant: MEMORIAL SLOAN-KETTERING CANCER CENTERInventors: Gabriela Chiosis, Tony Taldone, Anna Rodina, Pallav Patel, Yanlong Kang
-
Patent number: 8277957Abstract: A quinoxaline derivative represented by Formula (I) or (II) is provided. In Formula (I) or (II), R1 and R2 are, independently, hydrogen, halogen, methyl, ethyl, propyl, butyl, aryl or heteroaryl, for example phenyl, furyl, thienyl, pyridyl, pyrimidyl, benzothiazolyl or benzoimidazolyl. An organic light-emitting diode including the quinoxaline derivative is also provided.Type: GrantFiled: August 27, 2010Date of Patent: October 2, 2012Assignee: Industrial Technology Research InstituteInventors: Heh-Lung Huang, Teng-Chih Chao, Hao-Chun Lee
-
Publication number: 20120245148Abstract: The present invention relates to tetrahydroquinoxaline urea derivatives, to their preparation and to their therapeutic application.Type: ApplicationFiled: May 30, 2012Publication date: September 27, 2012Applicant: SANOFIInventors: Alain Jean Braun, Olivier Crespin, Claudie Namane, Eric Nicolai, Francois Pacquet, Cecile Pascal, Christophe Philippo, Olivier Venier
-
Publication number: 20120232103Abstract: The present invention provides a novel antimetabolic anticancer agent that has an excellent balance between antitumor effect and toxicity. Specifically, the present invention provides a medicament containing, as an active ingredient, a 5-fluorouracil derivative represented by Formula (I) or a salt thereof: wherein R1 represents a hydrogen atom or a protecting group of a hydroxy group, R2 represents a lower alkoxy-lower alkyl group or a tetrahydrofuranyl group, X represents a carbon atom or a nitrogen atom, and Y represents a halogen atom or a cyano group.Type: ApplicationFiled: March 14, 2012Publication date: September 13, 2012Inventors: Masakazu FUKUSHIMA, Shozo Yamada, Ryo Oyama
-
Publication number: 20120232270Abstract: Disclosed are an oligomer and a phthalonitrile monomer having the formulas: M is a metal or H. The value n is an integer greater than or equal to 1 for the oligomer and greater than or equal to 0 for the phthalonitrile monomer. Ar1 and Ar2 are independently selected aromatic- or heterocyclic-containing groups. Ar1, Ar2, or both are heteroaromatic or heterocyclic groups containing a nitrogen, sulfur, or oxygen heteroatom. Also disclosed are thermosets and pyrolyzed materials made from the phthalonitrile monomer.Type: ApplicationFiled: May 24, 2012Publication date: September 13, 2012Applicant: The Government of the United States of America, as represented by the Secretary of the NavyInventors: Matthew Laskoski, Teddy M. Keller
-
Patent number: 8263799Abstract: The present invention relates to chiral binaphthyl compounds having good solubility and high helical twisting power. The chiral binaphthyl compounds as dopants in the liquid crystal compositions can help enhance the display quality of the liquid crystal panels.Type: GrantFiled: April 27, 2011Date of Patent: September 11, 2012Assignee: Industrial Technology Research InstituteInventors: Jian-Wen Lin, Chun-Ming Wu, Shih-Hsien Liu, Kung-Lung Cheng
-
Patent number: 8258130Abstract: This invention is directed to a compound of formula (I): wherein R1, R2, R3, R4 and L1 are as defined herein, a pharmaceutical composition comprising the compound, and the use of the compound to treat allergic and/or inflammatory disorders, particularly disorders such as allergic rhinitis, asthma and/or chronic obstructive pulmonary disease (COPD).Type: GrantFiled: September 30, 2009Date of Patent: September 4, 2012Assignee: SanofiInventors: Suzanne C Aldous, Michael W Fennie, John Z Jiang, Stanly John, Lan Mu, Brian Pedgrift, James R Pribish, Barbara S Rauckman, Jeffrey S Sabol, Grzegorz T Stoklosa, Sukanthini Thurairatnam, Christopher Loren Vandeusen
-
Publication number: 20120220614Abstract: The present invention relates to Substituted Biaryl Derivatives, compositions comprising a Substituted Biaryl Derivative, and methods of using the Substituted Biaryl Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.Type: ApplicationFiled: November 16, 2010Publication date: August 30, 2012Inventors: Craig D. Boyle, Claire M. Lankin, William J. Greenlee, Joel M. Harris
-
Publication number: 20120220561Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: August 12, 2011Publication date: August 30, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, John D. HUBER, Ho Yin LO, Pui Leng LOKE, Weimin LIU, Tina Marie MORWICK, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
-
Patent number: 8252800Abstract: The present invention relates to compounds of the Formula I, the pharmaceutically acceptable salts and stereoisomers thereof, which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions in mammals: wherein n is an integer, preferably n is 1; wherein R1 and R2 are independently selected from the group consisting of:Type: GrantFiled: July 28, 2009Date of Patent: August 28, 2012Inventors: Wayne R. Danter, Martyn Brown, George Ma, Ghenadie Rusu, Jianhua Zhong, Natalie Lazarowych, Stephen Houldsworth
-
Publication number: 20120214762Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: ApplicationFiled: March 15, 2012Publication date: August 23, 2012Applicant: Genentech, Inc.Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A.G.N. Montalbetti
-
Patent number: 8247411Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: March 11, 2011Date of Patent: August 21, 2012Assignee: Pfizer IncInventors: Michael Joseph Luzzio, Kevin Daniel Freeman-Cook, Samit Kumar Bhattacharya, Matthew Merrill Hayward, Catherine Angela Hulford, Christopher Lowell Autry, Xumiao Zhao, Jun Xiao, Kendra Louise Nelson
-
Publication number: 20120208797Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C—X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1-C3 alkyl group; L represents single bond or a C1-C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: ApplicationFiled: August 11, 2010Publication date: August 16, 2012Applicants: SANOFI, MITSUBISHI TANABE PHARMA CORPORATIONInventors: Kazuki Nakayama, Daiki Sakai, Kazutoshi Watanabe, Toshiyuki Kohara, Keiichi Aritomo
-
Publication number: 20120208812Abstract: Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: October 21, 2010Publication date: August 16, 2012Applicant: Janssen Pharmaceutica N.V.Inventors: Wenying Chai, Michael A. Letavic, Kiev S. Ly, Daniel J. Pippel, Dale A. Rudolph, Kathleen C. Sappey, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman, Akinola Soyode-Johnson, Emily M. Stocking, Devin M. Swanson
-
Publication number: 20120202783Abstract: Disubstituted 3,8-diaza-bicyclo[4.2.0]octane and 3,6-diazabicyclo[3.2.0]heptane compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.Type: ApplicationFiled: October 21, 2010Publication date: August 9, 2012Inventors: Bryan James Branstetter, Michael A. Letavic, Kiev S. Ly, Dale A. Rudolph, Brad M. Savall, Chandravadan R. Shah, Brock T. Shireman
-
Publication number: 20120196859Abstract: The compositions and methods described herein disclose the design, synthesis and testing of compounds that act as inhibitors of DHFR. The basic scaffold of these inhibitors includes a 2,4-diaminopyrimidine ring with a propargyl linker to another substituted aryl, bicyclo or heteroaryl ring. These DHFR inhibitors are potent and selective for many different pathogenic organisms, including the DHFR enzyme from bacteria such as Bacillus anthracis and methicillin-resistant Staphylococcus aureus, fungi such as Candida glabrata, Candida albicans and Cryptococcus neoformans and protozoa such as Cryptosporidium hominis and Toxoplasma gondii. These compounds and other similar compounds are also potent against the mammalian enzyme and may be useful as anti-cancer therapeutics.Type: ApplicationFiled: November 7, 2011Publication date: August 2, 2012Inventors: Amy C. Anderson, Dennis L. Wright, Kathleen Mary Frey, Janet Leigh Paulsen, Eric William Scocchera, Kishore Viswanathan
-
Publication number: 20120190666Abstract: The present invention provides compounds that are PIKK inhibitors, more specifically, mTOR and/or PI3K? kinase inhibitors and are therefore useful for the treatment of diseases treatable by inhibition of kinases, specifically PI3 kinases, more specifically, mTOR and/or PI3K?, such as cancer. Also provided are pharmaceutical compositions containing such compounds and processes for preparing such compounds.Type: ApplicationFiled: May 12, 2010Publication date: July 26, 2012Applicant: Amgen Inc.Inventors: Christiane Bode, Alessandro Boezio, Alan C. Cheng, Deborah Choquette, James Robert Coats, Katrina Woodin Copeland, Hongbing Huang, Daniel La, Richard Thomas Lewis, Hongyu Liao, Michele Potashman, John Stellwagen, Shuyan Yi, Mark H. Norman, Markian M. Stec, Emily Anne Peterson, Russell Graceffa
-
Publication number: 20120190693Abstract: The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.Type: ApplicationFiled: April 2, 2012Publication date: July 26, 2012Inventors: John H. van Duzer, Ralph Mazitschek, Walter Ogier, James E. Bradner, Guoxiang Huang, Dejian Xie, Nan Yu
-
Publication number: 20120184516Abstract: Compounds of Formula I are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.Type: ApplicationFiled: June 30, 2011Publication date: July 19, 2012Inventors: Charles Kim, Takashi Nakai, Thomas Wai-Ho Lee, Joel Moore, Nicholas Robert Perl, Jason Rohde, Rajesh R. Iyengar, Ara Mermerian
-
Publication number: 20120184520Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that a compound of the present invention or a salt thereof exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. The present invention further relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound of the present invention or a salt thereof, and an excipient.Type: ApplicationFiled: September 15, 2010Publication date: July 19, 2012Applicant: Astellas Pharma Inc.Inventors: Kousei Yoshihara, Daisuke Suzuki, Susumu Yamaki, Yuji Koga, Norio Seki, Jiro Fujiyasu, Masahiro Neya
-
Publication number: 20120184572Abstract: Aryl GPR119 agonists are provided. These compounds are useful for the treatment of diabetic diseases, including Type II diabetes and other diseases associated with poor glycemic control.Type: ApplicationFiled: January 13, 2011Publication date: July 19, 2012Inventors: Jiangao Song, Jingyuan Ma, Christopher J. Rabbat, Imad Nashashibi, Xin Chen, Zuchun Zhao
-
Publication number: 20120178681Abstract: Bipiperidinyl compounds of the formula I, are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: ApplicationFiled: March 21, 2012Publication date: July 12, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: HAROLD B. WOOD, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang
-
Publication number: 20120168734Abstract: Disclosed are a compound including 5-membered heterocycles, an organic electronic device using the same, and a terminal including the latter.Type: ApplicationFiled: August 9, 2010Publication date: July 5, 2012Applicant: DUKSAN HIGH METAL CO., LTD.Inventors: Junghwan Park, Daesung Kim, Jungcheol Park, Yongwook Park, Hwasoon Jung, Soungyun Mun, Daehyuk Choi, Dongha Kim, Bumsung Lee
-
Publication number: 20120172378Abstract: Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atherosclerosis.Type: ApplicationFiled: December 2, 2011Publication date: July 5, 2012Inventors: Deirdre Mary Bernadette HICKEY, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith, Steven James Stanway
-
Publication number: 20120165353Abstract: Disclosed are: a novel compound which has both an antagonistic activity on an angiotensin II receptor and a PPAR?-activating activity and is therefore useful as a prophylactic and/or therapeutic agent for hypertension, heart diseases, arteriosclerosis, type-2 diabetes, diabetic complications, metabolic syndrome or the like; and a pharmaceutical composition containing the compound.Type: ApplicationFiled: September 29, 2010Publication date: June 28, 2012Applicant: KOWA COMPANY, LTD.Inventors: Toru Miura, Seiichi Sato, Hajime Yamada, Junya Tagashira, Ryohei Sekimoto, Rie Ishida, Hitomi Aoki, Tadaaki Ohgiya
-
Publication number: 20120165528Abstract: The present invention relates to chiral binaphthyl compounds having good solubility and high helical twisting power. The chiral binaphthyl compounds as dopants in the liquid crystal compositions can help enhance the display quality of the liquid crystal panels.Type: ApplicationFiled: April 27, 2011Publication date: June 28, 2012Applicant: INDUSTRIAL TECHNOLOGY RESEARCH INSTITUTEInventors: Jian-Wen Lin, Chun-Ming Wu, Shih-Hsien Liu, Kung-Lung Cheng