Three Or More Hetero Atoms In The Polycyclo Ring System Patents (Class 540/578)
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Publication number: 20130217675Abstract: This disclosure is directed to pyrido[4,3-b]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: February 18, 2011Publication date: August 22, 2013Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
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Publication number: 20130210807Abstract: The present invention describes and claims compounds of the Structural Formula I, Structural Formula II, or Structural Formula III: wherein R1, R2, R3 and R3? are —H or methyl, or R3 and R3 taken together form a double bond, or R3? is —H and R2 and R3 taken together form a spiro-cyclopropyl substituent, R4 is —H or —F, and R5 is —H, methyl, —CI or —Br, Formula II wherein R1 is —H, ethyl-, isopropyl-, cyclopropyl-, methyl- or methoxy-, R4 is —H or —F, and “Y” is: (a) —CH2—; (b) —CR6H-0-CR7R8—, wherein R6, R7, and R8 are independently —H or methyl; (c) —CR6H—N(R9)—CR7R8—, wherein R6, R7, and R8 are independently —H or methyl; (d) —CH2—C(R9)(R10)—C(R7)(R8)—, wherein R7, R8, R9 and R10 are independently —H or -methyl, or both R7 and R8 are —F, R9 and R10 are independently —H or -methyl, or both R9 and R10 are —F, or R9 and R10 taken together are (0=), which together with the carbon to which they are attached forms a carbonyl group.Type: ApplicationFiled: July 9, 2011Publication date: August 15, 2013Inventors: Nigel J Liverton, Christelle Boléa, Sylvain Celanire, Yunfu Luo
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Publication number: 20130184256Abstract: The present invention relates to new substituted glycinamides of general formula (I) wherein D, M, R3, R4 and R5 are defined as in the specification, the tautomers, enantiomers, diastereomers, mixtures and salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.Type: ApplicationFiled: March 5, 2013Publication date: July 18, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Henning PRIEPKE, Georg DAHMANN, Kai GERLACH, Roland PFAU, Wolfgang WIENEN, Annette SCHULER-METZ, Sandra HANDSCHUH, Herbert NAR
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Publication number: 20130158011Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 10, 2012Publication date: June 20, 2013Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER, Bernd WELLENZOHN
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Publication number: 20130150341Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 3, 2012Publication date: June 13, 2013Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF, Bernd WELLENZOHN
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Publication number: 20130150347Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 7, 2012Publication date: June 13, 2013Inventors: Klaus RUDOLF, Daniel BISCHOFF, Georg DAHMANN, Matthias GRAUERT, Raimund KUELZER, Bernd WELLENZOHN
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Publication number: 20130143870Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: November 30, 2012Publication date: June 6, 2013Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF, Bernd WELLENZOHN
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Publication number: 20130129677Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: December 7, 2012Publication date: May 23, 2013Applicant: Siga Technologies, Inc.Inventor: Siga Technologies, Inc.
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Publication number: 20130131048Abstract: The invention provides novel compounds and pharmaceutical compositions for the treatment of psychological and/or psychiatric diseases or disorders.Type: ApplicationFiled: January 24, 2013Publication date: May 23, 2013Applicant: RAMOT AT TEL-AVIV UNIVERSITY LTD.Inventor: RAMOT AT TEL-AVIV UNIVERSITY LTD.
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Publication number: 20130079321Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: September 26, 2012Publication date: March 28, 2013Applicant: GENENTECH, INC.Inventor: GENENTECH, INC.
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Patent number: 8404674Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.Type: GrantFiled: March 4, 2008Date of Patent: March 26, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Heinz Stadtmueller, Guido Boehmelt, Harald Engelhardt, Ulrich Hirt, Otmar Schaaf, Irene Waizenegger
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Publication number: 20130053365Abstract: Provided are inhibitors of poly(ADP-ribose)polymerase according to Formula (M): where A, B, Y, Z, D, E, R1, R2, R3, and R4 are as defined herein. Also described are pharmaceutical compositions, methods of preparing, and methods of using a compound of Formula M to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.Type: ApplicationFiled: August 29, 2012Publication date: February 28, 2013Applicant: BioMarin Pharmaceutical, Inc.Inventors: Bing Wang, Daniel Chu
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Publication number: 20130029968Abstract: The present invention relates to compounds of formula (I): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma and COPD.Type: ApplicationFiled: July 5, 2012Publication date: January 31, 2013Applicant: PFIZER LIMITEDInventors: Jotham Wadsworth Coe, Christoph Martin Dehnhardt, Peter Jones, Steven Wade Kortum, Yogesh Anil Sabnis, Florian Michel Wakenhut, Gavin Alistair Whitlock
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Publication number: 20130012496Abstract: Provided is a compound which is useful as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like. The present inventors have investigated compounds having a 5-HT2C receptor agonist activity and have found that the benzazepine compounds of the present invention have an excellent 5-HT2C receptor agonist activity, thereby completing the present invention. That is, the benzazepine compounds of the present invention have a 5-HT2C receptor agonist activity and can be used as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like.Type: ApplicationFiled: March 11, 2011Publication date: January 10, 2013Applicant: ASTELLAS PHARMA INC.Inventors: Hiroyuki Koshio, Norio Asai, Taisuke Takahashi, Takafumi Shimizu, Yasuhito Nagai, Keiko Kawabata, Karl Bruce Thor
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Patent number: 8349827Abstract: The present invention relates to substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted dipyrido-pyrimido-diazepine compounds, substituted benzo-pyrido-pyrimido-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: March 31, 2010Date of Patent: January 8, 2013Assignee: ArQule, Inc.Inventors: Manish Tandon, Yanbin Liu, Nivedita Namdev, Mark A. Ashwell, Rocio Palma
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Publication number: 20120328530Abstract: A compound of formula (III), or a pharmaceutically acceptable derivative thereof for use in a method of combating and/or detecting a pathogen and/or tumour cells; wherein X is selected from O, S and Se; each of R2, R3 and R4 is independently selected from hydrogen or an optionally substituted alkyl, alkenyl, alkynyl or aryl group; and R1 is selected from halogen, sulfo, acyl, sulfoxy, mercapto, nitro, amino, hydroxy or an optionally substituted alkyl, alkenyl, alkynyl, aryl, amine or alkoxy group; wherein R1 is not methyl or hydrogen when each of R3 and R4 is methyl or hydrogen.Type: ApplicationFiled: March 11, 2011Publication date: December 27, 2012Applicant: PHARMALUCIA LIMITEDInventor: Mark Wainwright
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Publication number: 20120329782Abstract: The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: ApplicationFiled: May 23, 2012Publication date: December 27, 2012Applicant: INCYTE CORPORATIONInventors: Argyrios G. Arvanitis, James D. Rodgers, Andrew P. Combs, Richard B. Sparks, Darius J. Robinson, Jordan S. Fridman, Krishna Vaddi
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Publication number: 20120322790Abstract: Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are methods of making and methods of using same.Type: ApplicationFiled: December 16, 2011Publication date: December 20, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Rajashekhar BETAGERI, Brian Nicholas COOK, Darren DiSALVO, Christian HARCKEN, Daniel KUZMICH, Pingrong LIU, John LORD, Can MAO, Hossein RAZAVI
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Publication number: 20120316148Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase signaling cascade.Type: ApplicationFiled: June 7, 2012Publication date: December 13, 2012Applicant: Dynamix Pharmaceuticals LTD.Inventors: Oren M. Becker, Itai Bloch, Efrat Ben-Zeev, Alina Shitrit, Avihai Yacovan, Sharon Gazal, Vered Behar, Alexander Konson, Nili Schutz, Sima Mirilashvili, Gali Golan
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Publication number: 20120277214Abstract: Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.Type: ApplicationFiled: November 24, 2010Publication date: November 1, 2012Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Teresa Disingrini, Sergio Mantegani, Mario Varasi
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Publication number: 20120264737Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.Type: ApplicationFiled: March 8, 2012Publication date: October 18, 2012Applicant: 3-V BIOSCIENCES, INC.Inventors: Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu
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Publication number: 20120253036Abstract: An agent for treating fibromyalgia containing a 5-HT2C receptor agonist as an active ingredientType: ApplicationFiled: December 10, 2010Publication date: October 4, 2012Inventors: Yukinori Nagakura, Mina Tsukamoto, Tomonari Watabiki
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Publication number: 20120245126Abstract: Nitromethylene analogues of imidacloprid and divalent and oxabridged heterocyclic neonicotinoid compounds constructed by dialdehydes, preparation methods and uses thereof are disclosed. Compounds represented by formula (A) or (B), their optical isomers or agrochemically acceptable salts are provided. Agrochemical compositions comprising the said compounds, their optical isomers or agrochemically acceptable salts, the uses of the said agrochemical compositions and the preparation methods of the said compounds, their optical isomers or agrochemically acceptable salts are also disclosed. The compounds and their derivatives have high insecticidal activities to several farming and forestry pests including homoptera and lepidoptera pests, such as aphis, fulgorid, whitefly, leafhopper, common thrips, cotton bollworm, cabbage caterpillar, cabbage moth, cotton leafworm and armyworm.Type: ApplicationFiled: December 9, 2010Publication date: September 27, 2012Applicant: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGYInventors: Xuhong Qian, Zhong Li, Xusheng Shao, Xiaoyong Xu, Zhiping Xu, Gonghua Song
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Publication number: 20120202791Abstract: The present invention relates to chemistry and pharmacy and, in particular, to the production of novel molecular entities, tricyclic and tetracyclic derivatives of benzodiazepine, pyridodiazepine and pyrimidodiazepine type fused with 1,4-dihydropyridine derivatives, having an effect on the central-nervous and vascular systems. Derivatives containing a dihydropyridine ring are used, by means of reactions with compounds of the ortho-phenylenediamine, ortho-diaminopyridine and ortho-diaminopyrimidine type, and also subsequent conversions to some thereof, to obtain tricyclic and tetracyclic derivatives of general formula I-XII that contain a diazepine or diazepinone nucleus fused to a 1,4-dihydropyridine nucleus, in which the A ring is a substituted or unsubstituted benzene, pyridine or pyrimidine ring.Type: ApplicationFiled: October 8, 2010Publication date: August 9, 2012Inventors: Yamila Verdecia Reyes, Estael Ochoa Rodriguez, Alberto Ruiz Reyes, Yanier Nunez Figueredo, Carmen Carillo Dominguez, Juan Enrique Tacoronte Morales, Livan Lázaro Alba Gutiérrez, Gilberto Lázaro Pardo Andreu
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Publication number: 20120202785Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: February 8, 2012Publication date: August 9, 2012Inventors: Robert Heald, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Bohdan Waszkowycz
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Publication number: 20120165313Abstract: Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).Type: ApplicationFiled: March 1, 2012Publication date: June 28, 2012Applicant: Genentech, Inc.Inventors: Philippe Bergeron, Frederick Cohen, Anthony Estrada, Michael F.T. Koehler, Kevin Hon Luen Lau, Coung Ly, Joseph P. Lyssikatos, Daniel Ortwine, Zhonghua Pei, Xianrui Zhao
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Publication number: 20120165304Abstract: The present invention relates to compounds defined by formula (I), wherein the groups X, Y, W and R1 to R4 are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are agonists of the 5-HT2C receptor, and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this receptor, such as metabolic and CNS-related disorders.Type: ApplicationFiled: November 26, 2009Publication date: June 28, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan-Georg Mueller, Christopher John Brown, Alexander Heifetz, Bernd Nosse, Juergen Prestle, Natacha Prevost, Klaus Rudolf, Stefan Scheuerer, Marcus Schindler, Dirk Stenkamp, Leo Thomas, Heather Tye
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Publication number: 20120157428Abstract: The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.Type: ApplicationFiled: December 2, 2011Publication date: June 21, 2012Applicant: CONSTELLATION PHARMACEUTICALS, INC.Inventors: Brian K. Albrecht, James E. Audia, Alexandre Côté, Victor S. Gehling, Jean-Christophe Harmange, Michael C. Hewitt, Yves LeBlanc, Christopher G. Naveschuk, Alexander M. Taylor, Rishi G. Vaswani
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Publication number: 20120142672Abstract: The present invention provides a heterocycle derivative having a superior amyloid ? production inhibitory activity and use thereof. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.Type: ApplicationFiled: July 12, 2010Publication date: June 7, 2012Inventors: Tatsuki Koike, Yasutaka Hoashi, Yoshihide Tomata
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Publication number: 20120135980Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).Type: ApplicationFiled: December 18, 2009Publication date: May 31, 2012Inventors: Theodros Asberom, Zhaoning Zhu, John W. Clader, Zhong-Yue Sun, Mihirbaran Mandal, Gioconda Gallo, Xiaoxiang Liu
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Publication number: 20120135981Abstract: The present invention is concerned with novel substituted triazole and imidazole derivatives of Formula (I) wherein R1, R2, A1, A2, A3, A4, X, and Het1 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.Type: ApplicationFiled: July 13, 2010Publication date: May 31, 2012Inventors: Tongfei Wu, Henricus Jacobus Maria Gijsen, Frederik Jan Rita Rombouts, François Paul Bischoff, Didier Jean-Claude Berthelot, Daniel Oehlrich, Michel Anna Jozef De Cleyn, Serge Maria Aloysius Pieters, Garrett Berlond Minne, Adriana Ingrid Velter', Sven Franciscus Anna Van Brandt, Michel Surkyn
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Publication number: 20120115848Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, U1, U2, U3, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: October 6, 2011Publication date: May 10, 2012Applicant: ELAN PHARMACEUTICALS, INC.Inventors: Robert A. Galemmo, JR., Dean Richard Artis, I, Xiaocong Michael Ye, Danielle L. Aubele, Anh P. Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Patent number: 8173804Abstract: The invention provides a process for production of mirtazapine as a convenient process for obtaining mirtazapine from a reaction mixture obtained by cyclization of 2-(4-methyl-2-phenylpiperazin-1-yl)pyridine-3-methanol with concentrated sulfuric acid, at high purity and in a form suitable for safe use as a drug. The production process for mirtazapine is characterized in that a reaction mixture obtained by cyclization of 2-(4-methyl-2-phenylpiperazin-1-yl)pyridine-3-methanol with concentrated sulfuric acid is diluted with water, the dilution is alkalinized in the presence of propanol, the mirtazapine is extracted with propanol and the mirtazapine is crystallized from the extract.Type: GrantFiled: March 13, 2008Date of Patent: May 8, 2012Assignee: Sumitomo Chemical Company, LimitedInventors: Chiharu Maeda, Takuma Maeda
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Publication number: 20120101086Abstract: The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: ApplicationFiled: June 17, 2010Publication date: April 26, 2012Applicant: GLAXO GROUP LIMITEDInventors: James Matthew Bailey, John Alexander Brown, Emmanuel Hubert Demont, Lee Andrew Harrison, Gail Astra Lorraine Seal, Christian Alan Paul Smethurst, Jason Witherington
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Publication number: 20120095217Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.Type: ApplicationFiled: January 8, 2010Publication date: April 19, 2012Inventors: Tobias Ritter, Laura Brass, Curtis Keith, Alan Watson, David J. Greenblatt
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Patent number: 8147818Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: January 23, 2009Date of Patent: April 3, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Publication number: 20120053168Abstract: The present invention relates to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).Type: ApplicationFiled: February 16, 2010Publication date: March 1, 2012Applicant: Targacept, Inc.Inventors: Balwinder Singh Bhatti, Timothy J. Cuthbertson, Anatoly Mazurov, Joseph Pike Mitchener, Julio A. Munoz, Srinivasa V. Murthy, Yunde Xiao, Daniel Yohannes
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Publication number: 20120028907Abstract: The disclosure relates to methods for identifying a tumor as an E2F-responsive gene over-expressing (ERGO) tumor, methods of determining the likelihood that an ERGO tumor patient will survive to a future date, methods of treating an ERGO tumor in a patient, and methods of selecting patients diagnosed as ERGO tumor prostate cancer patients for aggressive clinical treatment. The methods of the disclosure are applicable to ERGO tumors present in different human organs and tissues such as breast, lung, thyroid, ovary, and prostate.Type: ApplicationFiled: November 13, 2009Publication date: February 2, 2012Applicant: Intelligent Oncotherapeutics, Inc.Inventor: Stanley E. Shackney
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Publication number: 20120022046Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: February 24, 2010Publication date: January 26, 2012Inventors: Chelsea M. Byrd, Dongcheng Dai, Robert Jordan, Dennis E. Hruby
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Publication number: 20120022045Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: the asterisk * in Q denotes the point of attachment to the rest of the compound; and n, L1, L2, X1, X2, ?3, Y, Z, R1, R2 and R3 are defined herein. The N compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: January 25, 2010Publication date: January 26, 2012Inventors: Shankar Venkatraman, John S. Wai, Wayne Thompson, Boyoung Kim, Richard C.A. Isaacs, H. Marie Loughran, Dai-Shi Su, John Lim, Mark W. Embrey, Peter D. Williams
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Publication number: 20120015907Abstract: 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: April 19, 2011Publication date: January 19, 2012Applicant: NOVARTIS AGInventors: David BARNES, Rajiv CHOPRA, Scott Louis COHEN, Jiping FU, Mitsunori Kato, Peichao LU, Mohindra SEEPERSAUD, Wei ZHANG
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Publication number: 20110312942Abstract: The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.Type: ApplicationFiled: August 25, 2011Publication date: December 22, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher F. Claiborne, Todd B. Sells, Stephen G. Stroud
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Publication number: 20110312940Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R4, A, X, m and k are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: October 15, 2009Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Lars Van Der Veen, Darryl McConnell, Tobias Wunberg
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Publication number: 20110312941Abstract: The present invention provides compounds of formula (1) compositions comprising such compounds; the use of such compounds in therapy (such as in the treatment of dysmenorrhoea); and methods of treating patients with such compounds; wherein A and G are as defined herein.Type: ApplicationFiled: February 25, 2010Publication date: December 22, 2011Applicant: VANTIA LIMITEDInventors: Andrzej Roman Batt, Celine Marguerite Simone Heeney
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Publication number: 20110305636Abstract: Briefly described, embodiments of this disclosure include compounds as described herein, labeled compounds as described herein, pharmaceutical composition including compounds described herein, methods of imaging, method of forming a compound as described herein, and the like. In particular, embodiments of the disclosure include a series of triamino-pyridine derivatives and labeled triamino-pyridine derivatives, methods of synthesizing these compounds, intermediate compounds, methods of treatment using these compounds, methods of imaging, diagnosing, localizing, monitoring, and/or assessing a condition (e.g., corticotropin releasing factor type-1 (CRF1)) and/or related biological events, using triamino-pyridine derivatives, and the like. In addition, the present disclosure includes compositions (e.g., labeled triamino-pyridine derivatives that are ligands for the CRF1 receptor) used in and methods relating to non-invasive imaging (e.g., positron emission tomography (PET) imaging or SPECT imaging).Type: ApplicationFiled: March 12, 2010Publication date: December 15, 2011Applicant: EMORY UNIVERSITYInventors: Jeff Stehouwer, Mark Goodman, Clint Kilts, Charles Nemeroff
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Patent number: 8076324Abstract: The present invention relates to di(hetero)arylcyclohexane derivatives of the formula I, in which Ar1, Ar2, R1 and R2 have the meanings indicated in the claims. The compounds of the formula I are valuable pharmaceutical active compounds which inhibit ATP-sensitive potassium channels in the heart muscle and are suitable, for example, for the treatment of disorders of the cardiovascular system such as arrhythmias or a decreased contractility of the heart, such as can occur, for example, in coronary heart disease, cardiac insufficiency or cardiomyopathies. In particular, they are suitable for the prevention of sudden cardiac death. The invention furthermore relates to processes and intermediates for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: December 3, 2009Date of Patent: December 13, 2011Assignee: Sanofi-AventisInventors: Thomas Bohme, Uwe Gerlach, Dirk Gretzke, Heinz-Werner Kleemann, Stefania Pfeiffer-Marek, Henning Vollert, Jean-Michel Altenburger, Sergio Mallart
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Patent number: 8063040Abstract: Novel triazabenzo[e]azulene derivatives of the formula, (I) in which R1, R2 and R3 have the meanings indicated in Claim 1, are inhibitors of TGF-beta receptor kinase and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: September 29, 2007Date of Patent: November 22, 2011Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Guenter Hoelzemann, Hartmut Greiner, Christiane Amendt
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Publication number: 20110275609Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I The structures of rings A and B and substituents Ra, Rb and Rc are described in the specification. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis, treatment and inhibition of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: ApplicationFiled: January 14, 2010Publication date: November 10, 2011Applicant: CARA THERAPEUTICS, INC.Inventor: Robert Zhiyong Luo
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Publication number: 20110275801Abstract: The present invention provides heteroaryl-cyclohexyl-tetraazabenzo[e]azulenes of formula I wherein R1, R2 and R3 are as described herein. The compounds according to the invention act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.Type: ApplicationFiled: May 5, 2011Publication date: November 10, 2011Inventors: Cosimo Dolente, Patrick Schnider
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Publication number: 20110269744Abstract: [Problem] Provided is a compound which is useful as an agent for treating or preventing 5-HT2C receptor-related diseases, particularly incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like. [Means for Solution] The present inventors have investigated compounds having a 5-HT2C receptor agonist activity, which is promising as an active ingredient of a pharmaceutical composition for treating or preventing incontinence such as stress urinary incontinence, urge urinary incontinence, mixed urinary incontinence, and the like, sexual dysfunction such as erectile dysfunction syndrome and the like, obesity, and the like, and have found that the benzazepine compounds of the present invention have an excellent 5-HT2C receptor agonist activity, thereby completing the present invention.Type: ApplicationFiled: March 9, 2011Publication date: November 3, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Hiroyuki KOSHIO, Norio ASAI, Taisuke TAKAHASHI, Takafumi SHIMIZU, Yasuhito NAGAI, Keiko KAWABATA, Karl Bruce THOR