Chalcogen Bonded Directly To Ring Carbon Of The Tricyclo Ring System Patents (Class 546/86)
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Publication number: 20110091382Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.Type: ApplicationFiled: February 17, 2009Publication date: April 21, 2011Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Qianwa Liang, Brian A. Duclos, Wei Zhang, Peter J.H. Scott, Kai Chen, Zhiyong Gao, Tieming Zhao, Vani P. Mocharla, Dhanalakshmi Kasi, Gang Chen, Eric Wang, Anjana Sinha, Chunfang Xia, Henry Clifton Padgett, Farhad Karimi
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Publication number: 20110077404Abstract: The invention relates to a novel process for the preparation of pharmacologically interesting indolopyridine derivatives containing tetracyclic tetrahydro-?-carboline-hydantoines linked to a basic side chain and the corresponding salts, which can be used as Eg5 inhibitor, with very high overall chemical yield and enantiomeric purity.Type: ApplicationFiled: March 5, 2009Publication date: March 31, 2011Applicant: 4SC AGInventors: Bernd Muller, Helmut Schlemper
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Publication number: 20110046378Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled flavones, coumarins, carbazoles, quinolinones, chromenones, imidazoles and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's DiseaseType: ApplicationFiled: February 17, 2009Publication date: February 24, 2011Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Qianwa Liang, Brian A. Duclos, Wei Zhang, Peter J.H. Scott, Kai Chen, Zhiyong Gao, Tieming Zhao, Vani P. Mocharla, Dhanalakshmi Kasi, Gang Chen, Eric Wang, Anjana Sinha, Chunfang Xia, Henry Clifton Padgett, Farhad Karimi
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Publication number: 20110046368Abstract: The invention relates to novel ligands of 5-HT6 receptor, to a pharmaceutical composition containing said novel ligands of 5-HT6 receptor as active component and to novel medicaments used for humans and warm-blooded animals for treating diseases and conditions of central nervous system, in pathogenesis of which neuromediator systems induced by 5-HT6 receptors are playing an essential role. Azaheterocyclic compounds of the general formula 1 or racemates, or optical or geometrical isomers, or pharmaceutically acceptable salts and/or hydrates thereof are used as 5-HT6 ligands.Type: ApplicationFiled: November 15, 2007Publication date: February 24, 2011Inventors: Andrey Alexandrovich Ivashchenko, Alexander Vasilievich Ivashchenko, Sergey Yevgenievich Tkachenko, Ilya Matusovich Okun, Nikolay Filippovich Savchuk
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Patent number: 7893266Abstract: Methods for detection of cancer cells and for determining the proliferative status of cells in a tissue sample in vitro are disclosed. These methods comprise contacting a tissue sample with a radiolabeled compound or salt thereof of Formula wherein at least one of X, Y, and Z comprises a radioisotope, n is an integer from 2 to about 10; and each of A and A1 is a C1-C4 alkoxyl, a C1-C4 fluoroalkyl or a C1-C4 fluoroalkoxyl. The methods further comprise detecting the distribution of the radioisotope in the tissue sample, whereby a cell having a high density of the radioisotope compared to quiescent cells is diagnostic for a cancer cell.Type: GrantFiled: August 28, 2009Date of Patent: February 22, 2011Assignee: Washington UniversityInventors: Robert H. Mach, Michael J. Welch, Douglas J. Rowland, Zhude Tu
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Publication number: 20100317667Abstract: Provided herein are 1-aryl or 1-heteroarylsubstituted phenanthrene diketo acid compounds. These compounds comprise a ?-carboline ring structure substituted at C1 with an aryl or heteroaryl moiety and individually substituted at C3-C8 and N9 with a C1-C4 alkyl, a C1-C4 alkoxy, a C1-C4 alkoxyphenyl, halogen, thiol, alkylthiol, sulfonyl, sulfomainde, amide, substituted amide, ester, nitrile, OH, amino, substituted amine, haloalkyl, haloalkoxy, acyl, or a hydrogen. Also provided are methods for inhibiting proliferation of a cancer cell or for treating a cell proliferative disease by contacting the cancer cell or tumor comprising the same with the compounds provided herein or by administering the compounds to a subject with a cell proliferative disease.Type: ApplicationFiled: April 26, 2010Publication date: December 16, 2010Inventors: John K. Buolamwini, Shivaputra Patil, James K. Addo, D. Parker Suttle, Ruiwen Zhang, Zhengxiang Zhu, Sharma Horrick
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Publication number: 20100254916Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.Type: ApplicationFiled: February 19, 2010Publication date: October 7, 2010Applicant: Senomyx, Inc.Inventors: Donald S. Karanewsky, Joseph Fotsing, Catherine Tachdjian, Melissa Arellano
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Publication number: 20100216833Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, R3, R4, R5, X1, X2, X3, X4, n, and k are defined in the description and claims, and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for in the treatment and prophylaxis of diseases which are modulated by LXR? and/or LXR? agonists, including increased lipid and cholesterol levels, particularly low HDL-cholesterol, high LDL-cholesterol, atherosclerotic diseases, diabetes, particularly non-insulin dependent diabetes mellitus, metabolic syndrome, dyslipidemia, Alzheimer's disease, sepsis, inflammatory diseases such as colitis, pancreatitis, cholestasis/fibrosis of the liver, and diseases that have an inflammatory component such as Alzheimer's disease or impaired/improvable cognitive function.Type: ApplicationFiled: May 6, 2010Publication date: August 26, 2010Inventors: Henrietta Dehmlow, Bernd Kuhn, Raffaello Masciadri, Narendra Panday, Hasane Ratni, Matthew Blake Wright
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Publication number: 20100210762Abstract: A compound represented by formula (I-1): wherein R21, R22, R23 and R24 each independently represent a hydrogen atom or a monovalent substituent, with the proviso that compounds, in which R21, R22, R23 and R24 each are an alkylthio group, are excluded; R21 and R22 and/or R23 and R24 each may bond to each other to form a ring, with the proviso that compounds, in which the formed ring is a dithiol ring or a dithiolane ring, are excluded; R25 and R26 each independently represent a hydrogen atom or a monovalent substituent; X21, X22, X23 and X24 each independently represent a hetero atom; compounds, wherein R21, R22, R23 and R24 each represent a cyan group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group or a hydrogen atom, are excluded; and compounds, wherein R21 and R23 each represent a hydrogen atom; R22 and R24 each represent an arylcarbonyl group; X21, X22, X23 and X24 each represent a sulfur atom; and R25 and R26 each represent a hydroxyl group, are eType: ApplicationFiled: August 15, 2008Publication date: August 19, 2010Applicant: FUJIFILM CORPORATIONInventors: Naoyuki Hanaki, Masuji Motoki, Toshihiko Yawata
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Publication number: 20100190773Abstract: Heterocyclic compounds and analogues thereof and their use as inhibitors of Mitogen-Activated Protein Kinase-Activated Protein kinase-2 (MAPKAP-k2), and also to a method for preventing or treating a disease or disorder that can be treated or prevented by modulating the activity of MAPKAP-K2 in a subject and to pharmaceutical compositions and kits that include these MAPKAP-K2 inhibitors.Type: ApplicationFiled: March 19, 2010Publication date: July 29, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha ABEYWARDANE, Craig Andrew MILLER, Tina Marie MORWICK, Neil MOSS, Matthew Russell NETHERTON, Roger John SNOW, Ji WANG, Jiang-Ping WU, Zhaoming XIONG
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Publication number: 20100144778Abstract: The present invention encompasses compounds of Formula (I): as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: June 26, 2006Publication date: June 10, 2010Inventors: Subharekha Raghavan, Steven L. Colletti, Fa-Xiang Ding, Hong Shen, James R. Tata, Ashley Rouse Lins, Abigail Lee Smenton, Weichun Chen, Darby Rye Schmidt, George Scott Tria
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Publication number: 20100145052Abstract: A fused tricyclic compound having aldose reductase inhibitory activity and shown by the following formula, wherein R1 represents 1 to 3 atoms or substituents selected from a hydrogen atom, a halogen atom, a substituted or unsubstituted alkyl, cycloalkyl, alkylene, or alkoxy group, and a protected or unprotected hydroxyl or carboxyl group, R2 represents a protected or unprotected carboxyl group, R3 represents 1 or 2 atoms or substituents selected from a hydrogen atom, a halogen atom, an oxo group, a substituted or unsubstituted alkyl or alkoxy group, and a protected or unprotected carboxyl group, A represents an alkylene group, and B represents an oxygen atom, a sulfur atom, or a group shown by the following formula, wherein R4 represents an alkyl or aryl group substituted by an aryl, cycloalkyl, or heterocyclic group, and X represents an oxygen atom or a sulfur atom, provided that, when B represents a group shown by the following formula: wherein R4 represents an alkyl or aryl group substituted wiType: ApplicationFiled: February 11, 2010Publication date: June 10, 2010Applicant: National University Corporation University of ToyamaInventors: Naoki TOYOOKA, Atsushi KATO, Isao ADACHI
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Patent number: 7732461Abstract: Tricyclic nitrogen containing compounds of formula (I) and their use as antibacterials.Type: GrantFiled: April 25, 2007Date of Patent: June 8, 2010Assignee: Glaxo Group LimitedInventors: Gerald Brooks, Ilaria Giordano, Alan Joseph Hennessy, Neil David Pearson
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Patent number: 7732460Abstract: Tricyclic nitrogen containing compounds of formula (I) and their use as antibacterials.Type: GrantFiled: December 15, 2006Date of Patent: June 8, 2010Assignee: Glaxo Group LimitedInventors: Nathalie Cailleau, David Thomas Davies, Alan Joseph Hennessy, Graham Elgin Jones, Timothy James Miles, Neil David Pearson
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Publication number: 20100137353Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.Type: ApplicationFiled: April 17, 2008Publication date: June 3, 2010Applicant: GLAXO GROUP LIMITEDInventor: Neil David Pearson
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Publication number: 20100113478Abstract: The present invention relates to new indolone modulators of 5-HT3 receptor, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: September 11, 2009Publication date: May 6, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100105912Abstract: Some exemplary embodiments comprise fluoro-containing derivatives of pyrido[4,3-b]indoles (and exemplary methods of making the same) that may be administered to a mammal (including a human) in an effective amount for potential use in the treatment or prophylaxis of neurological disorders including AD, mild cognitive impairment, senile and vascular dementia, HD, ALS, Parkinson's disease, AIDS-related dementia, ischaemic cerebral pathologies, neuropathic pain, ADHD (attention deficit disorder/hyperactivity syndrome), eating disorders such as anorexia and bulimia, panic attacks, withdrawal from drug abuse such as cocaine, ethanol, nicotine and benzodiazepines, schizophrenia (in particular the cognitive deficit of schizophrenia), stroke and also disorders associated with spinal trauma and/or head injury. These derivatives may also be useful for the treatment of borderline personality disorder, obesity, and for use as geroprotectors.Type: ApplicationFiled: January 14, 2010Publication date: April 29, 2010Applicant: D2E, LLCInventors: Alexey Aksinenko, Sergey Bachurin, Sergey Sablin, Bogdan Beznosko, Vladimir Sokolov, Bogdan Beznosko
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Publication number: 20100098634Abstract: Provided herein are compounds and compositions which comprise the formulae as disclosed herein, wherein the compound is an amyloid binding compound. An amyloid binding compound according to the invention may be administered to a patient in amounts suitable for in vivo imaging of amyloid deposits, and distinguish between neurological tissue with amyloid deposits and normal neurological tissue. Amyloid probes of the invention may be used to detect and quantitate amyloid deposits in diseases including, for example, Down's syndrome, familial Alzheimer's Disease. In another embodiment, the compounds may be used in the treatment or prophylaxis of neurodegenerative disorders. Also provided herein are methods of allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing a neurodegenerative disease.Type: ApplicationFiled: July 24, 2009Publication date: April 22, 2010Inventors: Hartmuth C. Kolb, Joseph C. Walsh, Wei Zhang, Umesh B. Gangadharmath, Dhanalakshmi Kasi, Kai Chen, Anjana Sinha, Eric Wang, Gang Chen, Peter J.H. Scott, Henry Clifton Padgett, Qianwa Liang, Zhiyong Gao, Tieming Zhao, Chunfang Xia
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Publication number: 20100035912Abstract: Chemical compounds that disrupt retroviral assembly and maturation are presented herein. More particularly, this disclosure provides small molecule compounds that disrupt the formation and maturation of virus particles and methods of using such small molecules to treat HIV-1 infection.Type: ApplicationFiled: August 6, 2009Publication date: February 11, 2010Inventors: Asim Kumar Debnath, Hongtao Zhang, Francesca Curreli
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Patent number: 7659400Abstract: Fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labelled with 18F, can be used as radiotracers for imaging of tumors by positron emission tomography (PET). In addition, these compounds, when labelled with 123I, can be used as radiotracers for imaging of tumors by single photon emission computed tomography (SPECT). Methods for synthesis of these compounds are also disclosed.Type: GrantFiled: June 1, 2007Date of Patent: February 9, 2010Assignee: Washington UniversityInventors: Robert H. Mach, Zhude Tu
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Patent number: 7649093Abstract: The present invention relates to cycloalkylidene compounds with a variety of therapeutic uses, more particularly novel naphthalene compounds that are particularly useful for selective estrogen receptor modulation.Type: GrantFiled: June 21, 2005Date of Patent: January 19, 2010Assignee: Glaxo Smith Kline LLCInventors: Dennis Heyer, Jing Fang, Frank Navas, III, Subba Reddy Katamreddy, Jennifer Poole Peckham, Philip Stewart Turnbull, Aaron Bayne Miller, Adwoa Akwabi-Ameyaw
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Publication number: 20100004230Abstract: Tricyclic nitrogen containing compounds and their use as antibacterials.Type: ApplicationFiled: July 3, 2007Publication date: January 7, 2010Applicant: GLAXO GROUP LIMITEDInventors: Gerald Brooks, Timothy James Miles, Neil David Pearson
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Publication number: 20090275554Abstract: The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. wherein all symbols are described in the specification.Type: ApplicationFiled: December 12, 2005Publication date: November 5, 2009Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Hiromu Habashita, Haruto Kurata, Shinji Nakade
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Patent number: 7612206Abstract: Novel benzamide compounds of Formula (I), Formula (II), and Formula (III), salts, water soluble salts, analogs and radiolabeled counterparts thereof as sigma-2 receptor radiotracers for imaging the proliferative status of solid tumors. A method for diagnosing a mammal for the presence of a mammalian tumor therein comprises administering to the mammal a diagnostic imaging detectable effective amount of a benzamide compound having a structure illustrated in Formula (I), Formula (II) and Formula (III) and detecting binding of the compound to a tumor in the mammal. A method for diagnostic imaging of a mammalian tissue having cell surface sigma-2 receptors comprising administering to a mammal a diagnostic imaging amount of a compound having a structure illustrated in Formula (I) Formula (II) and Formula (III) and detecting an image of a tissue having an ample cells with sigma-2 receptors.Type: GrantFiled: March 8, 2008Date of Patent: November 3, 2009Assignee: Washington UniversityInventors: Robert Mach, Michael J. Welch, Douglas J. Rowland, Zhude Tu
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Publication number: 20090238761Abstract: This invention provides novel aryl piperazine derivatives having medical utility, in particular as modulators of dopamine and serotonin receptors, preferably the D3, D2-like and 5-HT2 receptor subtypes, and in particular useful for the treatment of neuropsychiatric disorders incl. schizophrenia.Type: ApplicationFiled: January 2, 2006Publication date: September 24, 2009Applicant: Universita Degli Studi Di SienaInventors: Giuseppe Campiani, Stefania Butini, Caterina Fattorusso, Francesco Trotta, Silvia Franceschini, Meri De Angelis, Karin Sandager Nielsen
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Publication number: 20090156557Abstract: Compounds are provided for use with kinases that comprise a compound selected from the group consisting of: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: April 15, 2008Publication date: June 18, 2009Applicant: TAKEDA SAN DIEGO, INC.Inventors: Jason W. Brown, Qing Dong, Bheema R. Paraselli, Jeffrey A. Stafford, Xianchang Gong, Yan Liu, Nicholas Scorah, Michael B. Wallace
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Publication number: 20090093512Abstract: The present invention relates to novel fused bicyclicpyrrolidine pyridone compounds of the formula (I) wherein R, RP and n are as defined herein, their pharmaceutically acceptable salts, pharmaceutical compositions and their use in treating addictive disorders such as the use of tobacco or other nicotine containing products and in the treatment of neurological and mental disorders related to a decrease in cholinergic function.Type: ApplicationFiled: November 30, 2005Publication date: April 9, 2009Inventors: Brian T. O'Neill, Kristen J. Procko, Daniel Yohannes
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Publication number: 20090062545Abstract: The present invention relates to a trisazo compound represented by the following formula (1) or a salt thereof, The formula (1) (wherein, the group A is a substituted phenyl group, the group B and the group C are substituted para-phenylene groups, R1 represents a C1 to C4 alkyl group (which may be substituted by a carboxy group), a phenyl group (which may be substituted by a sulfo group), or a carboxy group, R2 represents a cyano group, a carbamoyl group or a carboxy group, each of R3 and R4 independently represents a hydrogen atom, a methyl group, a chlorine atom or a sulfo group, respectively) and a water-based black ink composition containing said compound; said compound has high solubility in a medium where the main component is water, its aqueous solution having a high concentration and ink are stable when stored for a long period of time, black-recorded images with it can be provided where both light fastness and ozone gas fastness of the printed images are excellent.Type: ApplicationFiled: December 28, 2006Publication date: March 5, 2009Inventors: Takahiko Matsui, Yoshiyuki Dejima, Takashi Yoshimoto, Ryoutarou Morita, Koji Hirota
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Publication number: 20090048276Abstract: The instant invention provides for compounds which comprise substituted 3-aryl-4-hydroxyquinolin-2(1H)-ones that inhibit FAS activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting FAS activity by administering the compound to a patient in need of treatment of cancer.Type: ApplicationFiled: January 26, 2007Publication date: February 19, 2009Inventors: Mark T. Goulet, Benito Munoz, Alexey A. Rivkin
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Publication number: 20090042926Abstract: The present invention encompasses compounds of Formula (I): as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: December 20, 2006Publication date: February 12, 2009Inventors: Jason Imbriglio, Steven L. Colletti, James R. Tata, Richard T. Beresis, Daria Marley, Subharekha Raghavan, Darby Rye Schmidt, Ashley Rouse Lins, Abigail L. Smenton, Weichun Chen, Hong Shen, Fa-Xiang Ding, Rena Bodner
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Publication number: 20090036433Abstract: Tricyclic nitrogen containing compounds of formula (I) and their use as antibacterials.Type: ApplicationFiled: December 15, 2006Publication date: February 5, 2009Inventors: Nathalie Caileau, David Thomas Davies, Alan Joseph Hennessy, Graham Elgin Jones, Timothy James Miles, Neil David Pearson
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Publication number: 20090012046Abstract: Nucleotide-competing reverse transcriptase inhibitors (NcRTI) bind to the active site of HIV reverse transcriptase (RT) in competition with the next incoming nucleotide. To further investigate the impact of RT inhibitor resistance mutations on the activity of NcRTIs, the susceptibility of >6000 recent clinical isolates for a prototype compound, NcRTI-1, was determined. Over 80% of the profiled clinical isolates remained susceptible for NcRTI-1 (FC<4). No cross-resistance was observed between NcRTI-1 and currently used RT inhibitors, apart from limited cross-resistance with 3TC/FTC. Analysis of the genotype of >1700 of these viruses showed that the combination of active site mutations M184V+Y115F correlated most with resistance to NcRTI-1 (FC=75). Analysis also indicated that the K65R mutation is associated with hypersusceptibility to NcRTI-1 and that it reverses the reduced susceptibility caused by M184V. These findings were confirmed in SDM strains.Type: ApplicationFiled: February 5, 2007Publication date: January 8, 2009Inventors: Dirk Edward Desire Jochmans, Piet Tom Bert Paul Wigerinck
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Publication number: 20090012077Abstract: The present invention relates to compounds and compositions for treating diseases associated with cysteine protease activity. The compounds are reversible inhibitors of cysteine proteases, including cathepsins B, K, C, F, H, L, O, S, W and X. Of particular interest are diseases associated with Cathepsin K.Type: ApplicationFiled: June 25, 2008Publication date: January 8, 2009Inventors: Alexander Graham Dossetter, Nicola Murdoch Heron
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Publication number: 20080280941Abstract: Compounds of Formula I and corresponding pharmaceutical compositions are disclosed.Type: ApplicationFiled: February 24, 2005Publication date: November 13, 2008Inventor: Pierre Lourtie
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Publication number: 20080262020Abstract: The disclosure relates to compounds of formula (I): wherein R1, R2, R3, R4, are R5 are as defined in the disclosure; their preparation method, compositions containing the same and therapeutic use thereof.Type: ApplicationFiled: April 9, 2008Publication date: October 23, 2008Applicant: SANOFI-AVENTISInventors: Yvette MUNEAUX, Samir JEGHAM, Bernard BOURRIE, Pierre CASELLAS, Paola CIAPETTI, Jean-Marie DEROCQ, Camille-Georges WERMUTH
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Publication number: 20080249125Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, and R4 are as defined herein and hetaryl is a one or two ring-membered heteroaromatic ring system, connected to the carbon atoms of the piperidine group selected from the group consisting of or to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. These compounds are orexin receptor antagonists and may be useful in the treatment of disorders in which orexin pathways are involved, like sleep disorders.Type: ApplicationFiled: March 27, 2008Publication date: October 9, 2008Inventors: Luca Gobbi, Henner Knust, Parichehr Malherbe, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
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Publication number: 20080214538Abstract: The present disclosure relates to pyridoindolone derivatives of general formula (I): to processes for preparing the same and to their use in therapeutics.Type: ApplicationFiled: May 12, 2008Publication date: September 4, 2008Applicant: SANOFI-AVENTISInventors: Bernard Bourrie, Pierre Casellas, Paola Ciapetti, Jean-Marie Derocq, Samir Jegham, Yvette Muneaux, Camille-Georges Wermuth
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Patent number: 7390902Abstract: Novel benzamide compounds of Formula (I), Formula (II) and Formula (III, salts, water soluble salts, analogs and radiolabeled counterparts thereof as sigma-2 receptor radiotracers for imaging the proliferative status of solid tumors. A method for diagnosing a mammal for the presence of a mammalian tumor therein comprises administering to the mammal a diagnostic imaging detectable effective amount of a benzamide compound having a structure illustrated in Formula (I), Formula (II) and Formula (III) and detecting binding of the compound to a tumor in the mammal. A method for diagnostic imaging of a mammalian tissue having cell surface sigma-2 receptors comprising administering to a mammal a diagnostic imaging amount of a compound having a structure illustrated in Formula (I) Formula (II) and Formula (III) and detecting an image of a tissue having an ample cells with sigma-2 receptors.Type: GrantFiled: July 30, 2004Date of Patent: June 24, 2008Assignee: Washington UniversityInventors: Robert H. Mach, Michael J. Welch, Douglas J. Rowland, Jr., Zhude Tu
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Patent number: 7358364Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): which are useful in the treatment of metabolic disorders related to insulin resistance or hyperglycemia. These compounds include inhibitors of protein tyrosine phosphatase (PTP-1B) that are useful in the treatment of diabetes and other PTP-1B mediated diseases, such as cancer, neurodegenerative diseases and the like. The compounds of the invention are also useful in pharmaceutical compositions and methods of treating the aforementioned conditions.Type: GrantFiled: April 14, 2004Date of Patent: April 15, 2008Assignee: The Institute for Pharmaceutical Discovery LLCInventors: Michael C. Van Zandt, Darren Whitehouse, Kerry Combs, Shaojing Hu
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Patent number: 7297796Abstract: Novel sulfamoyl benzamide compounds, pharmaceutical compositions containing the sulfamoyl benzamide compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the sulfamoyl benzamide compounds are agonists and/or modulating ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ischemic conditions, immune-related disorders, hypertension, neurological disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, for inhibiting mechanical hyperalgesia associated with nerve injury, and as an appetite stimulant.Type: GrantFiled: October 13, 2005Date of Patent: November 20, 2007Assignee: Adolor CorporationInventors: Roland E. Dolle, Karin Worm, Q. Jean Zhou
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Patent number: 7211572Abstract: The present invention relates to a nitrogen-containing fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, and an anti-HIV agent containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an agent for the prophylaxis or treatment of AIDS, or as an anti-HIV agent. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Because it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects.Type: GrantFiled: October 13, 2005Date of Patent: May 1, 2007Assignee: Japan Tobacco Inc.Inventors: Susumu Miyazaki, Susumu Katoh, Kaoru Adachi, Hirotaka Isoshima, Satoru Kobayashi, Yuji Matsuzaki, Wataru Watanabe, Kazunobu Yamataka, Shinichi Kiyonari, Shuichi Wamaki
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Patent number: 7189851Abstract: The present invention relates to novel fused heterocyclic ring system compounds and methods for their use in the treatment and prevention of diseases or conditions.Type: GrantFiled: February 24, 2003Date of Patent: March 13, 2007Assignee: SmithKline Beecham CorporationInventors: Ashok Bhandari, Eric Eugene Boros, David John Cowan, Anthony Louis Handlon, Clifton Earl Hyman, Jeffrey Alan Oplinger, Michael Howard Rabinowitz, Philip Stewart Turnbull
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Patent number: 7125886Abstract: The subject invention provides useful and novel 5-HT3 antagonists. The subject invention also provides methods for synthesizing the compounds of invention. The invention also provides methods for the treatment of irritable bowel syndrome and other such conditions.Type: GrantFiled: May 28, 2004Date of Patent: October 24, 2006Assignee: Aryx TherapeuticsInventors: Xiaoming Zhang, Jurg R. Pfister, Cyrus Becker, Pascal Druzgala
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Patent number: 7122554Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.Type: GrantFiled: January 3, 2002Date of Patent: October 17, 2006Assignee: Lilly Icos LLC.Inventors: Jason S. Sawyer, Mark W. Orme, Raymond F. Brown, Alain C. Daugan, Agnes Bombrun
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Patent number: 7109339Abstract: The present invention is directed to novel compounds represented by structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R4a, R5, R6, R7, R8, R9,and m, are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain central nervous system disorders. The compounds of this invention are serotonin receptor modulators, in particular 5HT2C receptor agonists and antagonists, and are useful in the control or prevention of central nervous system disorders including obesity, anorexia, bulemia, depression, anxiety, psychosis, schizophrenia, migraine, addictive behavior, obsessive-compulsive disorder, and sexual disorders.Type: GrantFiled: December 19, 2003Date of Patent: September 19, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Taekyu Lee, Wenting Chen, Wei Deng, Albert J. Robichaud, Ruth R. Wexler
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Patent number: 7084154Abstract: A chemical genus of 2-(aminomethyl)arylamides, which are useful as analgesics, is disclosed.Type: GrantFiled: February 11, 2003Date of Patent: August 1, 2006Assignee: Pharmacopeia Drug Disclovery, Inc.Inventors: Koc-Kan Ho, John J. Baldwin, Adolph C. Bohnstedt, Steven G. Kultgen, Edward McDonald, Tao Guo, John Richard Morphy, Zoran Rankovic, Robert Horlick, Kenneth C. Appell
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Patent number: 7022856Abstract: Compounds of the general structural formula and use of the compounds and salts and solvates thereof, as therapeutic agents.Type: GrantFiled: December 18, 2001Date of Patent: April 4, 2006Assignee: LIlly Icos LLC.Inventors: Mark W. Orme, Jason S. Sawyer, Agnes Bombrun, Romain L. Gosmini, Anne Bouillot, Nerina Dodic, Michael Sierra
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Patent number: 7001911Abstract: The invention pertains to fused cyclic compounds having the formula, wherein G is an optionally substituted aryl or heterocyclo, L is an optional linker, M is a bond, O, CR7R7? or NR10, and M? is a bond or NR10, with the proviso that at least one of M or M? must be a bond; E is C?Z2, CR7CR7?, SO2, P?OR2, or P?OOR2; Z1 is O, S, NH, or NR6; Z2 is O, S, NH, or NR6; A1 is CR7 or N; A2 is CR7 or N; Y is J—J?—J? where J is (CR7R7?)n and n=0-3, J? is a bond or O, S, S?O, SO2, NH, NR6, C?O, OC?O, NR1C?O, CR7R7?, C?CR8R8?, R2P?O, OPOOR2, OPO2, OSO2, C?N, NHNH, NHNR6, NR6NH, N?N, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo or aryl or substituted aryl, and J? is (CR7R7?)n and n=0-3; W is CR7R7?—CR7R7?, CR8?CR8?, CR7R7?—C?O, NR9—CR7R7?, N?CR8, N?N, NR9—NR9?, cycloalkyl or substituted cycloalkyl, cycloalkenyl or substituted cycloalkenyl, heterocyclo or substituted heterocyclo, or aryl or substituted aryl; and O, R2, R6, R7, R7?, R8, R8?, R9, R9Type: GrantFiled: December 18, 2002Date of Patent: February 21, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Mark E. Salvati, James Aaron Balog, Weifang Shan, Sören Giese, Lalgudi S. Harikrishnan
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Patent number: 6987115Abstract: Compounds of the formula (I) are disclosed and are useful in the treatment bacterial infections: wherein: R1 is Ar or Het; R2 is C1-6alkyl, (R?)2N—(CH2)m— or Ar—C0-6alkyl; X is H, C1-4alkyl, OR?, SR?, C1-4alkylsulfonyl, C1-4alkylsulfoxyl, CN, N(R?)2, CH2N(R?)2, NO2, CF3, CO2R?, CON(R?)2, COR?, NR?C(O)R?, F, Cl, Br, I, or CF3S(O)r—; R? is H, C1-6alkyl or Ar—C0-6alkyl; each R? independently is H, C1-6alkyl or Ar—C0-6alkyl; m is 1 or 2; n is 0, 1 or 2; and r is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 7, 2001Date of Patent: January 17, 2006Assignee: SmithKline Beecham CorporationInventor: Mark A. Seefeld
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Patent number: 6984646Abstract: The invention relates to imidazopyridinones of the formula wherein the groups R1, R2, R3, and R4 are as defined in claim 1, to the process for their preparation, to pharmaceutical compositions containing them, and to a method of using them for treatment of chronic inflammatory processes in humans or animals.Type: GrantFiled: July 15, 2002Date of Patent: January 10, 2006Assignee: Bayer Healhcare AGInventors: Cristina Alonso-Alija, Martin Michels, Hartmut Schirok, Karl-Heinz Schlemmer, Sara Dodd, Mary Fitzgerald, John Bell, Andrew Gill