Additional Hetero Ring Patents (Class 514/444)
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Patent number: 8198271Abstract: A compound having the following formula (1) or a salt thereof: wherein R1 and R2 represent hydrogen, a lower alkyl, a lower alkenyl, a lower alkynyl or a group having the following formula (2): (R6)n—{circle around (A)}—Z—??(2), R3 represents hydroxy, a lower alkoxy, a lower cycloalkyloxy, an aryloxy, carboxy, a lower alkoxycarbonyl, or —NRaRb having the following formula (3): (R7)o—{circle around (B)}—??(3), R4 and R5 represent halogen, a lower alkyl, hydroxy, or a lower alkoxy; R6 represents halogen, a lower alkyl, an aryl group, a heterocyclic, a hydroxy, a lower alkoxy, mercapto, a lower alkylthio, a lower alkylcarbonyl, amino, nitro or cyano; R7 represents a lower alkyl, hydroxy or a lower alkoxy; Ra and Rb represent hydrogen or a lower alkyl; the ring A represents a cyclic hydrocarbon or a heterocyclic ring; the ring B represents a heterocyclic ring having one or more heteroatoms selected from the group consisting of nitrogen and oxygen; X represents a lower alkylene; Y represents a lower alkyleType: GrantFiled: May 25, 2009Date of Patent: June 12, 2012Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Hiroyuki Mogi, Hisashi Tajima, Noriko Mishina, Yusuke Yamazaki, Shinji Yoneda, Katsuhiko Watanabe, Junko Fujikawa, Minoru Yamamoto
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Patent number: 8183391Abstract: A process for resolving dorzolamide trans racemate, which comprises reacting said racemate with (1S)-(+)-10-camphorsulfonic acid so obtaining the (4S,6S) enantiomer by selectively precipitating and recovering the camphorsulfonic acid salt thereof (dorzolamide camphorsulfonate), and neutralizing dorzolamide camphorsulfonate to obtain dorzolamide.Type: GrantFiled: April 16, 2007Date of Patent: May 22, 2012Assignee: Zach Systems S.p.A.Inventors: Paolo Maragni, Ivan Michieletto, Livius Cotarca
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Publication number: 20120115915Abstract: Compositions and methods for inhibiting translation initiation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using N,N?-diarylureas and/or N,N?-diarylthiourea compounds are described.Type: ApplicationFiled: May 28, 2010Publication date: May 10, 2012Applicant: President and Fellows of Harvard CollegeInventors: Bertal Huseyin Aktas, José A. Halperin, Michael Chorev
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Publication number: 20120114765Abstract: Disclosed are novel compounds which are useful as therapeutics, especially in anti-neoplastic therapy and in other therapeutic regimes where cysteine protease inhibition is implicated.Type: ApplicationFiled: March 31, 2010Publication date: May 10, 2012Inventors: Ping Cao, Joseph Weinstock, William D. Kingsbury, Craig A. Leach, Suresh Kumar Kizhakkethil-George, Benjamin Nicholson
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Publication number: 20120108636Abstract: The present invention provides compounds of formula (I) wherein W, R1, R5 and R6 have a meaning as defined herein in the specification. The compounds of formula (I) are allosteric enhancers of the A1 adenosine receptor and, thus, may be employed for the treatment of conditions mediated by the A1 adenosine receptor. Accordingly, the compounds of formula (I) may be employed for treatment of pain, in particular, chronic pain such as neuropathic pain, and inflammatory pain, cardiac disease or disorder such as cardiac disarrhythmias, e.g., peroxysmal supraventricular tachycardia, angina, myocardial infarction and stroke, neurological disease or injury, sleep disorders, epilepsy and depression.Type: ApplicationFiled: January 11, 2012Publication date: May 3, 2012Inventors: Pier Giovanni Baraldi, Allan R. Moorman, Romeo Romagnoli
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Publication number: 20120095012Abstract: The present invention provides compounds of formula (I), wherein R1 is a monocyclic 5- or 6-membered heteroaryl; R4 is phenyl or monocyclic 5- or 6-membered heteroaryl; and the other substituents as defined in the claims, that inhibit cell and cell division and that inhibit the activation of Hypoxia Inducible Factor (HIF)—mediated transcription and signaling under hypoxic conditions. In one aspect, the compounds of the present invention are useful for the preparation of a medicament for the treatment or prevention of a disease or disorder selected from the group consisting of an inflammatory disease, a hyperproliferative disease or disorder, a hypoxia-related pathology and a disease characterized by excessive vascularisation. Also provided is a pharmaceutical composition, comprising a compound of the invention and a second therapeutic agent or radiation, useful for the treatment or prevention of the mentioned diseases or disorders.Type: ApplicationFiled: December 30, 2009Publication date: April 19, 2012Applicant: Elara Pharmaceuticals GmbHInventors: Jorge Alonson, Arantxa Encinas Lopez, Marcel Muelbaier, Jochen Ammenn, Bernd Wendt, Joe Lewis, Christoph Schultes, Bernd Janssen
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Publication number: 20120088783Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.Type: ApplicationFiled: September 26, 2011Publication date: April 12, 2012Applicant: Ampere Life Sciences, Inc.Inventors: Bing WANG, Gail Walkinshaw, Donald R. James
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Patent number: 8153670Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: GrantFiled: January 5, 2009Date of Patent: April 10, 2012Assignee: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
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Patent number: 8148410Abstract: The invention relates to novel thiophene derivatives (I), their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I).Type: GrantFiled: December 9, 2008Date of Patent: April 3, 2012Assignee: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, Cyrille Lescop, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner
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Patent number: 8143242Abstract: The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: January 7, 2010Date of Patent: March 27, 2012Assignee: Sanofi-AventisInventors: Henning Steinhagen, Hauke Szillat, Markus Follmann, Reinhard Kirsch, Volkmar Wehner, Hans Matter, Martin Lorenz, Kent W. Neuenschwander, Anthony C. Scotese
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Publication number: 20120071523Abstract: The instant invention provides novel benzofuran-4,5-diones and pharmaceutical compositions thereof useful for inhibiting PDF and for treating proliferative and infectious diseases. Compounds may be selective for eukaryotic (e.g., human) PDF or prokaryotic PDF.Type: ApplicationFiled: May 5, 2010Publication date: March 22, 2012Applicant: Sloan-Kettering Institute for Cancer ResearchInventors: Hakim Djaballah, Christophe Antczak
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Publication number: 20120065231Abstract: The present invention provides a compound represented by the formula (I) or its salt, solvate, or physiologically functional derivative; and a pharmaceutical composition which is useful for treatment or prevention of conditions or disorders having sensitivity to selective androgen receptor modulation, the composition comprising the above-described compound; among others:Type: ApplicationFiled: April 28, 2010Publication date: March 15, 2012Applicant: SUMITOMO CHEMICAL COMPANY LTD.Inventors: Koichiro Harada, Kozo Motonaga, Koichi Saito, Akio Tanaka
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Publication number: 20120059012Abstract: Disclosed is a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is 1: a C3-8 cycloalkyl C1-4 alkyl group, 2: a C7-14 aralkyl group, in which the aryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, (b) C1-4 alkyl, which is optionally substituted with 1 to 3 fluorine atoms, (c) C1-4 alkoxy, which is optionally substituted with 1 to 3 fluorine atoms, and (d) C1-4 alkylcarbonyl, which is optionally substituted with C1-4 alkoxy, 3: a five- to ten-membered heteroaryl-C1-4 alkyl group, in which the heteroaryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, and (b) C1-4 alkyl, or 4: a C6-10 aryl C2-6 alkenyl group; and R2 is a cyano group or a nitro group.Type: ApplicationFiled: May 12, 2010Publication date: March 8, 2012Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Akihito Fujii, Kazumi Niidome, Chiaki Migihashi, Toshiyuki Kamei, Takafumi Matsumoto, Tomoyuki Hirata
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Patent number: 8124649Abstract: The invention provides compounds that inhibit PIM kinases and Flt3 kinase, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation.Type: GrantFiled: June 30, 2009Date of Patent: February 28, 2012Assignee: Cylene Pharmaceuticals, Inc.Inventors: Mustapha Haddach, Johnny Yasuo Nagasawa
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Publication number: 20120046350Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? suptype.Type: ApplicationFiled: January 18, 2010Publication date: February 23, 2012Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Lone Jeppesen, Ingrid Pettersson, Per Sauerberg, Pavel Pihera, Miroslav Havranek
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Publication number: 20120046238Abstract: A method for treating an infection with a virus. The method includes administering to a subject in need thereof an effective amount of one or more coumarin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, and X are defined herein. Also disclosed is a pharmaceutical composition including a coumarin compound.Type: ApplicationFiled: November 10, 2011Publication date: February 23, 2012Applicant: National Health Research InstitutesInventors: Hsing-Pang Hsieh, Tsu-An Hsu, Jiann-Yih Yeh, Jim-Tong Horng, Shin-Ru Shih, Sui-yuan Chang, Yu-Sheng Chao
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Publication number: 20120046320Abstract: The present invention discloses ?-diketones, ?-diketones or ?-hydroxyketones or analogs thereof, that activate Wnt/?-catenin signaling and thus treat or prevent diseases related to signal transduction, such as osteoporosis and osteoarthropathy; osteogenesis imperfecta, bone defects, bone fractures, periodontal disease, otosclerosis, wound healing, craniofacial defects, oncolytic bone disease, traumatic brain injuries related to the differentiation and development of the central nervous system, comprising Parkinson's disease, strokes, ischemic cerebral disease, epilepsy, Alzheimer's disease, depression, bipolar disorder, schizophrenia; eye diseases such as age related macular degeneration, diabetic macular edema or retinitis pigmentosa and diseases related to differentiation and growth of stem cell, comprising hair loss, hematopoiesis related diseases and tissue regeneration related diseases.Type: ApplicationFiled: August 17, 2011Publication date: February 23, 2012Applicant: WINTHERIX, LLCInventors: Sunil Kumar KC, David Mark Wallace, John Hood, Charlene F. Barroga
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Patent number: 8106211Abstract: The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.Type: GrantFiled: March 19, 2007Date of Patent: January 31, 2012Assignee: Bayer CropScience AGInventors: Peter Jeschke, Robert Velten, Thomas Schenke, Otto Schallner, Michael Edmund Beck, Rolf Pontzen, Olga Malsam, Udo Reckmann, Ralf Nauen, Ulrich Görgens, Leonardo Pitta, Thomas Müller, Christian Arnold, Erich Sanwald
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Patent number: 8106212Abstract: The present invention relates to novel substituted enaminocarbonyl compounds, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.Type: GrantFiled: March 19, 2007Date of Patent: January 31, 2012Assignee: Bayer Cropscience AGInventors: Peter Jeschke, Robert Velten, Thomas Schenke, Otto Schallner, Michael Beck, Olga Malsam, Ralf Nauen, Ulrich Görgens, Thomas Müller, Christian Arnold, Erich Sanwald
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Publication number: 20120022116Abstract: Disclosed are compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically related to GPR35, and/or GPR35-hERG signaling complex. For example, disclosed are compounds for preventing and/or treating diseases which are pathophysiologically related to GPR35 in a subject.Type: ApplicationFiled: July 13, 2011Publication date: January 26, 2012Inventors: Huayun Deng, Ye Fang, Mingqian He, Haibei Hu, Weijun Niu, Haiyan Sun
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Publication number: 20120022080Abstract: The present invention provides a novel compound having plasminogen activator inhibitor-1 inhibitory activity, and an inhibitor of PAI-1 comprising the compound as an active ingredient. The present invention also provides a pharmaceutical composition having an inhibitory action on PAI-1 activity and being efficacious in the prevention and treatment of various diseases whose onset is associated with PAI-1 activity.Type: ApplicationFiled: March 31, 2010Publication date: January 26, 2012Applicant: RENASCIENCE CO., LTD.Inventors: Toshio Miyata, Kenji Murano, Nagahisa Yamaoka, Akihisa Maeda
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Publication number: 20120015911Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: ApplicationFiled: September 20, 2011Publication date: January 19, 2012Applicant: Bellus Health Inc.Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
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Publication number: 20120010187Abstract: The invention provides FIG. 1 novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: ApplicationFiled: March 16, 2010Publication date: January 12, 2012Applicant: University of Virginia Patent FoundationInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. Macdonald, Thomas Eric Ballard, JR.
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Publication number: 20120009259Abstract: The present invention is directed a pharmaceutical compositions for co-therapy treatment and prevention of glucose-related disorders such as Type 2 diabetes mellitus and Syndrome X.Type: ApplicationFiled: July 6, 2011Publication date: January 12, 2012Inventors: Urbain Alfons Clementina Delaet, Anne Faure, Philip Erna Hortentia Gilbert Heyns, Eugeen Maria Jozef Jans, Aniruddha Railkar
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Publication number: 20120010219Abstract: The invention features salvinorin compositions that are selective for kappa opioid receptors; methods of treating mania by using a selective kappa receptor agonist; and methods of treating mood disorders, such as depressive disorders and manic disorders, using salvinorin compositions.Type: ApplicationFiled: December 14, 2009Publication date: January 12, 2012Applicant: The McLean Hospital CorporationInventors: Cecile Beguin, Justin Stephen Potuzak, Thomas Anthony Munro, Katherine K. Duncan, William A. Carlezon, Bruce M. Cohen, Lee-yuan Liu Chen
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Patent number: 8093270Abstract: The invention relates to a solid pharmaceutical preparation containing (R)-(?)-2-[5-(4-fluorophenyl-3-pyridylmethylaminomethyl]chroman as an active substance and at least one sugar alcohol (e.g. mannitol, sorbitol) as a filler. Also disclosed is the production of said solid pharmaceutical preparation, which is provided with an increased shelf life also at elevated temperatures and can be used for the treatment of dyskinesia associated with Parkinson's disease.Type: GrantFiled: June 9, 2006Date of Patent: January 10, 2012Assignee: Merck Patent GmbHInventors: Klaus Kunath, Kirstin Heil, Roland Rupp
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Patent number: 8088925Abstract: The present invention relates to compounds of the formula I, which exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses.Type: GrantFiled: November 15, 2007Date of Patent: January 3, 2012Assignee: Sanofi-AventisInventors: Michael Wagner, Matthias Urmann, Volkmar Wehner, Martin Lorenz, Armin Bauer, Marc Nazare, Hans Matter
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Publication number: 20110319446Abstract: Compounds of formula (I) have muscarinic M3 receptor modulating activity; wherein A is an oxygen atom or group —N(R12)—; (i) R1 is C1-C6-alkyl or a hydrogen atom; and R2 is a hydrogen atom or a group —R5, —Z—Y—R5, —Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H; and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (ii) R1 and R3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R2 is a hydrogen atom; or a group —R5, —Z—Y—R5, —Z—NR9R10, —Z—CO—NR9R10, —Z—NR9—CO—R5, or —Z—CO2H, in which cases the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (iii) R1 and R2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group —Y—R5, —Z—Y—R5, —Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to whiType: ApplicationFiled: June 20, 2011Publication date: December 29, 2011Applicant: Argenta Discovery Ltd.Inventors: Harry Finch, Nicholas Charles Ray, Richard James Bull, Monique Bodil van Niel, Andrew Stephen Robert Jennings
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Patent number: 8084467Abstract: One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.Type: GrantFiled: June 24, 2005Date of Patent: December 27, 2011Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Qian Liu, Rajesh Thotapally, Venkata Kiran Vemuri
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Patent number: 8084489Abstract: The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have glucagon receptor antagonist or inverse agonist activity, as well as methods of using these compounds and intermediates and methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising N compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.Type: GrantFiled: February 9, 2006Date of Patent: December 27, 2011Assignee: Eli Lilly and CompanyInventors: Mark Donald Chappell, Scott Eugene Conner, Allie Edward Tripp, Guoxin Zhu
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Publication number: 20110312919Abstract: The teachings relate to methods of identifying inhibitors of dimerization of tyrosine receptor kinases such as EGFR. The methods comprise providing, on a digital computer, a molecular model comprising a complex of extracellular dimerization domains of an RTK, docking a chemical databases to the molecular model, scoring the compounds comprised by the database, and identifying one or more high-scoring compounds. The methods further comprise testing a compound for RTK inhibitory activity in vitro, and testing a compound for specificity as an RTK inhibitor. Also disclosed are compounds selected by the described methods, and methods of treatment using the compounds. Two compounds (NSC11241 and NSC56452) are disclosed that inhibit EGF receptor kinase activation in a dose-dependent manner.Type: ApplicationFiled: June 10, 2011Publication date: December 22, 2011Applicant: Washington UniversityInventors: Garland R. Marshall, Linda J. Pike, Robert Yang
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Publication number: 20110313032Abstract: The present invention is directed to a compound of formula (I), its diastereoisomers, its enantiomers or its pharmaceutically acceptable salts or solvates, formula (I), to procedures of obtaining the same, to intermediates thereof, and use as competitive inhibitors of the third enzyme of the shikimic acid pathway, the type II dehydroquinase.Type: ApplicationFiled: December 23, 2009Publication date: December 22, 2011Applicant: UNIVERSIDADE DE SANTIAGO DE COMPOSTELAInventors: Cóncepcion González Bello, Verónica Filipa Vieira Prazeres, Sonia Paz Gómez, Cristina Sánchez Sixto, Lorena Tizón Valverde
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Publication number: 20110286927Abstract: In one aspect, the invention relates to a method for identifying a drug candidate with activity as a neuroprotective agent. The method includes determining whether a compound reduces ATF4 activity; and identifying the compound that reduces ATF4 activity as a drug candidate.Type: ApplicationFiled: August 4, 2008Publication date: November 24, 2011Applicant: CORNELL UNIVERSITYInventor: Rajiv R. Ratan
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Publication number: 20110288052Abstract: The class compounds of the present invention may be represented by Formula (I), wherein X may be O, S, or N. R1 and R2 are independently either H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl. R3 and R4 are independently either H, an aryl group, a heteroaryl group, and a heterocyclic ring group having 4 to 6 carbon atoms, wherein the aryl, heteroaryl, and heterocyclic moieties are optionally substituted with one or more of a first substitution group defined herein. In a further embodiment, R3 and R4 along with the atoms and bonds to which they are attached, form an optionally substituted 5-7 membered ring having at least one nitrogen atom within the ring structure.Type: ApplicationFiled: June 2, 2009Publication date: November 24, 2011Inventors: Craig A. Townsend, Kandasamy Subburaj, Jill Marie McFadden
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Publication number: 20110280867Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Ar, R1, R2, R3, R4 and R5 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: ApplicationFiled: July 27, 2011Publication date: November 17, 2011Applicant: Schering CorporationInventors: Zhaoning Zhu, Andrew W. Stamford, Brian McKittrick
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Publication number: 20110281883Abstract: The present invention relates to the use of compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, R7, r, Y and G have the meanings given above as insecticides and/or acaricides and/or fungicides.Type: ApplicationFiled: January 14, 2010Publication date: November 17, 2011Applicant: Bayer Cropscience AGInventors: Reiner Fischer, Stefan Lehr, Arnd Voerste
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Publication number: 20110275703Abstract: The present invention provides a compound represented by Formula (II): wherein R1 is a chlorine atom, a fluorine atom, a methyl group or an ethynyl group; Ar is a group represented by the following Formula (a), Formula (b), Formula (c) or Formula (d): wherein R2 is a C1-6 alkyl group which may be substituted with one or more halogen atoms, a C1-6 alkoxy group which may be substituted with one or more halogen atoms, a C1-3 alkylthio group, a halogen atom, a C1-3 alkylcarbonyl group or a C2-5 alkynyl group which may be substituted with —OR4; R3 is a hydrogen atom or a C1-3 alkyl group; R4 is a hydrogen atom or a C1-3 alkyl group; provided that Ar is a group represented by Formula (a) when R1 is a fluorine atom, methyl group or an ethynyl group, and that R2 is methoxy group, an ethoxy group, an isopropyl group, a propyl group, a trifluoromethyl group, a trifluoromethoxy group, 2-fluoroethyl group or 1-propynyl group when R1 is a methyl group or a pharmaceutically acceptable salt or a solvate thereof aType: ApplicationFiled: July 27, 2007Publication date: November 10, 2011Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Tsutomu Sato, Kiyofumi Honda, Takahiro Kawai, Koo Hyeon Ahn
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Publication number: 20110275616Abstract: Methods of utilizing an opioid agonist in a mammalian subject in a manner that inhibits peripheral effects of the opioid agonist are described. The methods comprise administering the opioid agonist in an amount sufficient to confer analgesia the subject and co-administering a neutral opioid antagonist or pharmaceutically acceptable isomorph or pharmaceutically acceptable salt thereof in an amount sufficient to substantially inhibit peripheral effects and insufficient to block substantial central effects of the opioid agonist in the subject.Type: ApplicationFiled: July 18, 2011Publication date: November 10, 2011Applicant: AIKO BIOTECHNOLOGYInventors: Wolfgang Sadée, Edward Bilsky, Janet Yancey-Wrona
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Patent number: 8039492Abstract: The present invention provides a substituted cyclic compound of the following general formula I or II: its preparation process and its use as a glucagon-like peptide-1 receptor regulator for preventing or treating metabolic disorders including, but not limited to, diabetes, insulin resistance and obesity, etc.Type: GrantFiled: June 21, 2006Date of Patent: October 18, 2011Assignee: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Mingwei Wang, Na Li, Xin Xie, Qing Liu, Caihong Zhou, Fajun Nan, Guangxing Wang
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Publication number: 20110250254Abstract: An agent comprising the compound according to general formula (I) wherein R1, R2, R3 and R4 are each independently H or a substituent, and wherein at least one of R1, R3 and R4 is halogen, cyano, cyanate, thiocyanate or C1-C6 haloalkyl.Type: ApplicationFiled: October 9, 2009Publication date: October 13, 2011Inventors: Anne Aamdal Scheie, Tore Benneche, Jessica Lonn-Stensrud, Jan Skramstad
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Publication number: 20110245262Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.Type: ApplicationFiled: August 20, 2007Publication date: October 6, 2011Inventors: Lijun Sun, Keizo Koya, Shoujun Chen, Zachary Demko, Zhi-Qiang Xia
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Publication number: 20110245265Abstract: Methods to treat or prevent acute kidney injury and chronic kidney injury in subjects using CXCR4 antagonists are disclosed.Type: ApplicationFiled: August 28, 2009Publication date: October 6, 2011Applicant: GENZYME CORPORATIONInventors: Anna Zuk, Steven Ledbetter, Nibedita Chattopadhyay
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Publication number: 20110236400Abstract: Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.Type: ApplicationFiled: July 1, 2008Publication date: September 29, 2011Inventors: Wen-Lian Wu, Thomas A. Bara, Duane A. Burnett, John W. Clader, Martin S. Domalski, Yan Jin, Hubert B. Josien, Hongmei Li, Xian Liang, Dmitri A. Pissarnitski, Thavalakulamgara K. Sasikumar, Jesse K. Wong, Ruo Xu, Zhiqiang Zhao, Paul E. McNamara
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Publication number: 20110200553Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating flaviviridae viral infection.Type: ApplicationFiled: April 7, 2011Publication date: August 18, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Laval Chan Chun Kong, Jean Bedard, Sanjoy Kumar Das, Nghe Nguyen Ba, Oswy Z. Pereira, Thumkunta Jagadeeswar Reddy, Mohammed Arshad Siddiqui, Wuyi Wang, Constanin G. Yannopoulos
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Patent number: 7994211Abstract: Compounds of formula (I) have muscarinic M3 receptor modulating activity; Formula (I) wherein A is an oxygen atom or group —N(R12)—; (i) R1 is C1-C6-alkyl or a hydrogen atom; and R2 is a hydrogen atom or a group —R5, —Z—Y—R5—Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H; and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (ii) R1 and R3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R2 is a hydrogen atom; or a group —R5, —Z—Y—R5, —Z—NR9R10, —Z—CO—NR9R10, —Z—NR9—CO—R5, or —Z—CO2H, in which cases the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (iii) R1 and R2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group —Y—R5, —Z—Y—R5, —Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom toType: GrantFiled: August 8, 2006Date of Patent: August 9, 2011Assignee: Argenta Discovery LimitedInventors: Nicholas Charles Ray, Andrew Stephen Robert Jennings
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Patent number: 7989488Abstract: In one aspect, the present invention provides a novel thiophene-containing polynitrone compound having structure (II) wherein R1 is independently at each occurrence a C1-C20 aliphatic radical, a C3-C20 cycloaliphatic radical, or a C2-C30 aromatic radical; R2 is independently at each occurrence hydrogen, deuterium, a C1-C20 aliphatic radical, a C3-C20 cycloaliphatic radical, or a C2-C30 aromatic radical; and “a” is an integer from 2 to 4.Type: GrantFiled: September 28, 2007Date of Patent: August 2, 2011Assignee: General Electric CompanyInventors: Christoph Georg Erben, Michael Jeffrey Mclaughlin, Kathryn Lynn Longley, Shantaram Narayan Naik, Mahesh Kisan Chaudhari, Jyoti Balkrishna Shet, Varadarajan Sundararaman, Yogendrasinh Bharatsinh Chauhan, Gary Charles Davis, Sumeet Jain, Moitreyee Sinha
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Publication number: 20110178058Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: ApplicationFiled: January 14, 2011Publication date: July 21, 2011Applicant: Gilead Sciences, Inc.Inventors: Eda CANALES, Lee S. Chong, Michael O' Neil Hanrahan Clarke, Edward Doerffler, Scott E. Lazerwith, Willard Lew, Michael Mertzman, Philip A. Morganelli, William J. Watkins
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Publication number: 20110178165Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula (I): as defined in the specification. The invention is also directed to compositions containing the compounds of formula (I). They are useful in the treatment of CNS disorders.Type: ApplicationFiled: September 25, 2009Publication date: July 21, 2011Inventors: Kimberly Gail Estep, Christopher John O'Donnell, Longfei Xie
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Publication number: 20110178129Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: ApplicationFiled: January 14, 2011Publication date: July 21, 2011Applicant: Gilead Sciences, Inc.Inventors: Eda Canales, Michael O' Neil Hanrahan Clarke, Scott E. Lazerwith, Willard Lew, Philip Anthony Morganelli, William J. Watkins
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Publication number: 20110178127Abstract: The present invention relates to a new amine compound or a pharmaceutically acceptable salt thereof, wherein the definitions of X, R1, R2 and n are given in the description, to a pharmaceutical composition containing the compound as active ingredient, and to use of the amine compound or its pharmaceutically acceptable salt for the manufacture of an anti-depressent drug.Type: ApplicationFiled: June 23, 2009Publication date: July 21, 2011Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. ChinaInventors: Bohua Zhong, Youzhi Zhang, Yangping Zhang, Rui Xue, Xinhua He, Yunfeng Li, Hongxia Chen, Nan Zhao, Melying Li