Polycyclo Ring System Having The 1,3-oxazole Ring As One Of The Cyclos Patents (Class 546/271.7)
-
Patent number: 8541404Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.Type: GrantFiled: November 3, 2010Date of Patent: September 24, 2013Assignee: ElexoPharm GmbHInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
-
Patent number: 8540521Abstract: Disclosed are benzoxazole-based compounds, kits, and methods of producing and using the described compounds in fluorescence-based detection of analytes (e.g., metal ions). Also disclosed are uses of benzoxazole-based compounds as ratiometric metal ion indicators.Type: GrantFiled: December 29, 2009Date of Patent: September 24, 2013Assignee: Life Technologies CorporationInventors: Kyle Gee, Vladimir Martin
-
Publication number: 20130190271Abstract: Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a nitrogen atom or the like; R1 and R4 independently represent a halogen atom or the like; R2 and R3 independently represent a halogen atom or the like; R5 and R6 independently represent a linear C1-C6 hydrocarbon group which may be substituted, or the like (provided that both R5 and R6 cannot represent a hydrogen atom simultaneously); and n represents 0 or 1]. The harmful arthropod control composition has an excellent efficacy to control harmful arthropods.Type: ApplicationFiled: March 8, 2013Publication date: July 25, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Sumitomo Chemical Company, Limited
-
Publication number: 20130190350Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist, such as a small molecule, in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.Type: ApplicationFiled: December 12, 2012Publication date: July 25, 2013Applicant: CURIS, INC.Inventor: Curis, Inc.
-
Publication number: 20130178456Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).Type: ApplicationFiled: February 28, 2013Publication date: July 11, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
-
Patent number: 8476269Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: GrantFiled: July 9, 2012Date of Patent: July 2, 2013Assignee: Novartis AGInventors: Urs Baettig, Kamlesh Jagdis Bala, Emma Budd, Lee Edwards, Catherine Howsham, Glyn Alan Hughes, Darren Mark Legrand, Katrin Spiegel
-
Publication number: 20130157996Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: June 21, 2012Publication date: June 20, 2013Applicant: Amgen Inc.Inventors: Kaustav Biswas, James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Vu Van Ma, Holger Monenschein, Thomas T. Nguyen, David J. St. Jean, JR., Chester Chenguang Yuan, Wenge Zhong
-
Patent number: 8455497Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: February 12, 2009Date of Patent: June 4, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
-
Patent number: 8455522Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: May 12, 2010Date of Patent: June 4, 2013Assignee: Novartis AGInventors: Qi-Ying Hu, Julien Papillon
-
Publication number: 20130137875Abstract: The invention describes the preparation and use of fluorescent stains for nucleic acids derived from unsymmetrical cyanine dyes, dimmers, trimers, or tetramers. In particular, the invention describes unsymmetric cyanine dyes, dimmers, trimer and tetramers having a water soluble substituent. The dyes of the invention possess superior fluorescent properties when complexed with nucleic acids, and have utility in any application which requires detection of nucleic acids, such as detection of nucleic acids in solution, in gels, in blots, in microarrays, and in bacteria and cells, and for use in analysis of cell structure, membrane integrity, and function. The presence of the water soluble substituent results in improved water soluability and stability, resulting in improved detection of nucleic acids.Type: ApplicationFiled: November 24, 2012Publication date: May 30, 2013Inventor: Laiqiang Ying
-
Publication number: 20130131084Abstract: The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: for the manufacture of a pharmaceutical composition intended for the treatment of cancer.Type: ApplicationFiled: August 17, 2012Publication date: May 23, 2013Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Catherine GUILLOU, Frank Kozielski, Christophe Labriere, Francoise Gueritte, Sergey Tcherniuk, Dimitrios Skoufias, Claude Thal, Henri-Philippe Husson
-
Publication number: 20130109649Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: ApplicationFiled: October 25, 2012Publication date: May 2, 2013Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
-
Publication number: 20130079339Abstract: The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1.Type: ApplicationFiled: December 22, 2010Publication date: March 28, 2013Applicant: PHARMESTE S.R.L.Inventors: Mauro Napoletano, Marcello Trevisani, Maria Giovanna Pavani, Francesca Fruttarolo
-
Publication number: 20130079325Abstract: Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: November 14, 2012Publication date: March 28, 2013Inventors: Jennifer R. Allen, Biswas Kaustav, Frank Chavez, Ning Chen, Frenel Fils De Morin, James R. Falsey, Michael J. Frohn, Paul E. Harrington, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Roxanne Kunz, Holger Monenschein, Thomas T. Nguyen, Alexander J. Pickrell, Andreas Reichelt, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Guomin Yao
-
Publication number: 20130079374Abstract: The present invention provides a compound represented by the formula which is useful as an agent for the prophylaxis or treatment of diseases related to the action of melatonin, or a salt thereof and the like.Type: ApplicationFiled: October 23, 2012Publication date: March 28, 2013Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventor: TAKEDA PHARMACEUTICAL COMPANY LIMITE
-
Patent number: 8383932Abstract: A compound for an organic photoelectric device, represented by the following Chemical Formula 1:Type: GrantFiled: April 19, 2010Date of Patent: February 26, 2013Assignee: Cheil Industries, Inc.Inventors: Ho-Kuk Jung, Myeong-Soon Kang, Jin-Seong Park, Nam-Soo Kim, Kyu-Yeol In, Eiu-Su Kang, Mi-Young Chae
-
Patent number: 8372980Abstract: Fused-ring, heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein ?represents an optional double bond, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: GrantFiled: July 22, 2011Date of Patent: February 12, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Mariappan V. Chelliah, Samuel Chackalamannil
-
Publication number: 20130018054Abstract: The present invention provides organic compounds of the following structure; A-L1-B—C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: NOVARTIS AGInventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming Liu
-
Publication number: 20130018074Abstract: The present invention provides organic compounds of the following structure; A-L1-B—C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Applicant: NOVARTIS AGInventors: Michael H. SERRANO-WU, Young-shin KWAK, Wenming Liu
-
Publication number: 20130018052Abstract: The present invention provides a novel 2-pyridyl substituted imidazole derivative, or a pharmaceutically acceptable salt or solvate thereof, which selectively inhibits the transforming growth factor-? (TGF-?) type I receptor (ALK5) and/or the activin type I receptor (ALK4); a pharmaceutical composition comprising same as an active ingredient; and a use of the 2-pyridyl substituted imidazole derivative for the manufacture of a medicament for preventing or treating a disease mediated by ALK5 and/or ALK4 receptors in a mammal.Type: ApplicationFiled: July 13, 2012Publication date: January 17, 2013Applicant: SK CHEMICALS CO., LTD.Inventors: Ju Young LEE, Keun-Ho RYU, Jae-Sun KIM, Yong-Hyuk KIM, Dong Chul SHIN, Bong-yong LEE, Sang-hwan KANG, Hyun-Jung LEE, Hoechul JUNG, Young Ah SHIN, Euisun PARK, Jaeseung AHN
-
Patent number: 8293721Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are potent CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In formula I, A-B is an arylamide moiety.Type: GrantFiled: June 16, 2008Date of Patent: October 23, 2012Assignee: Merck Sharpe & Dohme Corp.Inventors: Julianne A. Hunt, Ramzi F. Sweis, Peter J. Sinclair
-
Publication number: 20120245167Abstract: Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a nitrogen atom or the like; R1 and R4 independently represent a halogen atom or the like; R2 and R3 independently represent a halogen atom or the like; R5 and R6 independently represent a linear C1-C6 hydrocarbon group which may be substituted, or the like (provided that both R5 and R6 cannot represent a hydrogen atom simultaneously); and n represents 0 or 1]. The harmful arthropod control composition has an excellent efficacy to control harmful arthropods.Type: ApplicationFiled: April 17, 2012Publication date: September 27, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Mitsuhiko IWAKOSHI, Ippei UEMURA
-
Publication number: 20120232071Abstract: The present invention relates to compounds of formula I wherein R1a to R1e, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
-
Publication number: 20120225861Abstract: Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.Type: ApplicationFiled: April 23, 2012Publication date: September 6, 2012Inventors: James C. Sutton, Marion Wiesmann, Weibo Wang, Mika Lindvall, Jiong Lan, Savithri Ramurthy, Anu Sharma, Elizabeth J. Mieuli, Liana M Klivansky, William Lenahan, Susan Kaufman, Hong Yang, Simon C. Ng, Keith Pfister, Allan S. Wagman, Victoria Sung, Martin Sendzik
-
Publication number: 20120226046Abstract: Compounds useful in porous films for light extraction and/or light scattering in electronic devices, such as light-emitting devices, are described herein. These compounds may be represented by Formula 1, as described herein.Type: ApplicationFiled: March 2, 2012Publication date: September 6, 2012Applicant: NITTO DENKO CORPORATIONInventors: Shijun Zheng, Jensen Cayas, David T. Sisk
-
Patent number: 8242128Abstract: The invention relates to compounds of formula 1, the production and use thereof as a medicament for the treatment of diseases, particularly tumours and/or diseases caused, mediated or propagated by angiogenesis. The compounds of formula 1 are effective inhibitors of tyrosin kinases, particularly TIE-2 and VEGFR, and Raf-kinases.Type: GrantFiled: September 1, 2004Date of Patent: August 14, 2012Assignee: Merck Patent GmbHInventors: Wolfgang Stähle, Alfred Jonczyk, Wilfried Rautenberg
-
Publication number: 20120157403Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
-
Publication number: 20120157434Abstract: The present invention provides heterocyclic compounds of the following formula I: or pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof useful as antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: ApplicationFiled: February 29, 2008Publication date: June 21, 2012Inventors: Mikhail Fedorovich Gordeev, Zhengyu Yuan, Jinqian Liu
-
Publication number: 20120149718Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.Type: ApplicationFiled: December 13, 2011Publication date: June 14, 2012Inventors: Christine E. Brotherton-Pleiss, Keith A. M. Walker
-
Publication number: 20120142714Abstract: The present invention provides a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes and the like, and having superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: November 29, 2011Publication date: June 7, 2012Inventors: TSUNEO YASUMA, MAKOTO KAMATA, TOHRU YAMASHITA, HIDEKI HIROSE, MASATAKA MURAKAMI, ASATO KINA, KAZUKO YONEMORI, RYO MIZOJIRI, IKUO FUJIMORI, TAKUYA FUJIMOTO, ZENICHI IKEDA
-
Patent number: 8178668Abstract: 2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.Type: GrantFiled: February 4, 2009Date of Patent: May 15, 2012Assignee: OSI Pharmaceuticals, LLCInventors: Arno G. Steinig, Mark J. Mulvihill, Jing Wang, Douglas S. Werner, Qinghua Weng, Heather Coate, Xin Chen
-
Publication number: 20120115856Abstract: A compound depicted by the formula below, or a pharmaceutically acceptable salt or solvate thereof. wherein, R1 represents (1) a C3-6 alkyl group, (2) a C1-6 alkyl group substituted with one or more substituent group(s) selected from those consisting a halogen atom, etc., (3) a C3-10 non-aromatic cyclic hydrocarbon group or a 5- to 6-membered non-aromatic heterocyclic group which respectively is optionally substituted with one or more substituent group(s) selected from those consisting an oxo group, etc., (4) an aromatic cyclic hydrocarbon group substituted with one or more substituent selected from the group consisting halogen atom and C1-4 alkoxy group; X represents NH, O, or S; Y represents CH or N; Z represents N or a C—R2; R2 represents (1) hydrogen atom, (2) a C1-6 alkyl group, a C2-6 alkenyl group or a C2-6 alkynyl group that respectively is optionally substituted with one or more substituent group(s) selected from among those consisting (a) a halogen atom, etc.Type: ApplicationFiled: May 28, 2010Publication date: May 10, 2012Inventors: Junichi Ishikawa, Koichi Saito, Norihisa Ohe, Kentaro Kobayashi
-
Publication number: 20120108586Abstract: Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a nitrogen atom or the like; R1 and R4 independently represent a halogen atom or the like; R2 and R3 independently represent a halogen atom or the like; R5 and R6 independently represent a linear C1-C6 hydrocarbon group which may be substituted, or the like (provided that both R5 and R6 cannot represent a hydrogen atom simultaneously); and n represents 0 or 1]. The harmful arthropod control composition has an excellent efficacy to control harmful arthropods.Type: ApplicationFiled: December 30, 2011Publication date: May 3, 2012Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Mitsuhiko IWAKOSHI, Ippei UEMURA
-
Publication number: 20120108585Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: August 11, 2009Publication date: May 3, 2012Applicant: Sirtris Pharmaceuticals, Inc.Inventor: Chi B. Vu
-
Patent number: 8168653Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist of formula (I) in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.Type: GrantFiled: August 2, 2010Date of Patent: May 1, 2012Assignees: Curis, Inc., Genentech, Inc.Inventors: Oivin M. Guicherit, Edward Andrew Boyd, Shirley Ann Brunton, Stephen Price, John Harry Alexander Stibbard, Colin H. Mackinnon
-
Publication number: 20120071512Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: May 12, 2010Publication date: March 22, 2012Applicant: NOVARTIS AGInventors: Qi-Ying Hu, Sylvie Chamoin, Christopher M. Adams, Chun Zhang
-
Publication number: 20120071514Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: May 12, 2010Publication date: March 22, 2012Applicant: NOVARTIS AGInventors: Qi-Ying Hu, Julien Papillon
-
Publication number: 20120064181Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: ApplicationFiled: March 15, 2010Publication date: March 15, 2012Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem Nguyen, Daniel V. Paone, Craig M. Potteiger, Shaun R. Stauffer, Carolyn Segerdell, Ashley Nomland, John J. Lim
-
Patent number: 8119624Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: GrantFiled: October 27, 2010Date of Patent: February 21, 2012Assignee: Pfizer Inc.Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukui, Ru Zhou
-
Publication number: 20120029190Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, psychiatric disorders, neuro-muscular disorders, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds provided herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.Type: ApplicationFiled: April 1, 2010Publication date: February 2, 2012Inventors: Douglas Burdi, Kerry L. Spear, Larry Wendell Hardy
-
Publication number: 20120016131Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: ApplicationFiled: September 22, 2011Publication date: January 19, 2012Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
-
Publication number: 20120004227Abstract: The present invention discloses novel cyclohexane derivatives having NPY Y5 receptor antagonistic activity. Specifically, the present invention discloses a compound represented by the formula (I), or a pharmaceutically acceptable salt or a solvate thereof: wherein A is substituted or unsubstituted aryl or heterocyclyl; a combination of X and Y is a combination selected from (X, Y)?(C(?O)N(R1), C(?O)N(R2)), (C(?O)N(R1), imidazole-1,3-diyl), (N(R1), C(?O)N(R2)), (O, C(?O)N(R2)), (C(R3)(R4), N(R2)) or (a single bond, C(?O)N(R2)); R1, R2 and R3 are independently hydrogen or substituted or unsubstituted alkyl; R5 is substituted or unsubstituted aryl or heterocyclyl; R6 is halogen, oxo, substituted or unsubstituted alkyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aryloxy; m is 0 or 1; and n is an integer of 0 to 5; and B is aromatic carbocycle, monocyclic heterocycle or fused bicyclic heterocycle.Type: ApplicationFiled: March 5, 2010Publication date: January 5, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Hiroshi Yoshida, Keisuke Tonogaki, Masahiro Sakagami, Kenji Takaya
-
Publication number: 20110313001Abstract: According to the invention there is provided a compound of formula (I): (I) or a pharmaceutically acceptable salt or hydrate thereof; wherein the variables are as defined herein. The compounds selectively attenuate the production of A?42 and hence are useful in treatment of Alzheimer's disease and related conditions.Type: ApplicationFiled: December 7, 2009Publication date: December 22, 2011Inventors: Christian Fischer, Adam J. Schell, Benito Munoz
-
Publication number: 20110306082Abstract: Disclosed are benzoxazole-based compounds, kits, and methods of producing and using the described compounds in fluorescence-based detection of analytes (e.g., metal ions). Also disclosed are uses of benzoxazole-based compounds as ratiometric metal ion indicators.Type: ApplicationFiled: December 29, 2009Publication date: December 15, 2011Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Kyle Gee, Vladimir Martin
-
Publication number: 20110306591Abstract: Heteroaryloxycarbocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: May 11, 2011Publication date: December 15, 2011Inventors: Jennifer R. Allen, Michael J. Frohn, Paul E. Harrington, Essa Hu, Alexander J. Pickrell, Robert M. Rzasa, Kelvin K. C. Sham
-
Publication number: 20110301112Abstract: Fused-ring, heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: ApplicationFiled: July 22, 2011Publication date: December 8, 2011Inventors: Yan Xia, Mariappan V. Chelliah, Samuel Chackalamannil
-
Patent number: 8071593Abstract: Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds.Type: GrantFiled: May 8, 2008Date of Patent: December 6, 2011Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
-
Patent number: 8071595Abstract: 1,2-disubstituted heterocyclic compounds which are inhibitors of phosphodiesterase 10 are described. Also described are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function. Among the disorders which may be treated are neurological, neurodegenerative and psychiatric disorders including, but not limited to, those associated with cognitive deficits or schizophrenic symptoms.Type: GrantFiled: June 24, 2009Date of Patent: December 6, 2011Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
-
Publication number: 20110293744Abstract: Inhibitors of poly(ADP-ribose)polymerase having a structure of Formula (I), ways to make them and methods of treating patients using them are disclosed.Type: ApplicationFiled: January 19, 2010Publication date: December 1, 2011Applicant: ABBOTT LABORATORIESInventors: Magdalena K. Przytulinska, Thomas D. Penning, Yunsong Tong
-
Patent number: 8067602Abstract: Asymmetric cyanine fluorescent dyes are represented by general formula I. These kinds of dyes may be used as a staining agent for nucleic acids, with the spectra at 600-900 nm in the near-infrared region and without interference from background fluorescence. These kinds of dyes may be useful with small-type red semiconductor lasers as the light source (such as 633 nm). Compositions comprising these dyes and methods for staining biological samples using these dyes or compositions are also provided.Type: GrantFiled: December 12, 2008Date of Patent: November 29, 2011Assignee: Shenzhen Mindray Bio-Medical Electronics Co., Ltd.Inventor: Jianhui Shao