Additional Hetero Atom In The Polycyclo Ring System Patents (Class 514/215)
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Patent number: 8273734Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.Type: GrantFiled: June 14, 2012Date of Patent: September 25, 2012Assignee: Arena Pharmaceuticals, Inc.Inventors: Brian Smith, Jeffrey Smith
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Patent number: 8258128Abstract: The present invention relates to novel aza-thia-benzoazulene derivatives of formula I as defined in the claims, their preparation, the use of these novel compounds for the preparation of pharmaceutical compositions, the use of these novel compounds and compositions for managing arthritis and arthritis-related conditions as well as in the treatment of pain in animals and humans. More particularly, the present invention relates to pharmaceutical, preferably veterinary compositions and methods for reducing inflammation and pain associated with acute inflammation of body parts, particularly joints, due to injury or due to arthritic conditions or other disease conditions.Type: GrantFiled: February 21, 2007Date of Patent: September 4, 2012Assignee: Novartis AGInventors: Pietro Bollinger, Mahavir Prashad, Bernhard Riss, Janet Dawson King, Peter C. Hiestand, Yugang Liu, Jonathan King, Vincent Schmid, Friedrich Schuerch
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Publication number: 20120222142Abstract: The present application relates to a composition including gut flora-derived extracellular vesicles, and to an animal disease model using same. In addition, the present application relates to a method for using the gut flora-derived extracellular vesicles to efficiently search for a candidate drug which may prevent or treat diseases that occur due to gut flora-derived extracellular vesicles, and to a vaccine which can efficiently prevent or treat infections caused by gut flora or diseases that occur due to gut flora-derived extracellular vesicles. Further, the development of diagnostic technology to discover, using the gut flora-derived extracellular vesicles of the present application, the etiology of diseases that occur due to gut flora-derived extracellular vesicles, can be achieved.Type: ApplicationFiled: July 20, 2010Publication date: August 30, 2012Applicant: AEON MEDIX INC.Inventors: Yoon Keun Kim, Yong Song Gho, Kyoung Su Park, Bok Sil Hong, Ji Hyun Kim, You Sun Kim, Won Hee Lee, Jung Wook Kim, Dae-Kyum Kim
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Publication number: 20120220572Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein X, Y, Z, R3 and R4 are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.Type: ApplicationFiled: February 28, 2012Publication date: August 30, 2012Applicant: ABBOTT LABORATORIESInventors: Yunsong Tong, Thomas D. Penning, Alan S. Florjancic, Julie Miyashiro, Keith W. Woods
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Patent number: 8247405Abstract: Skin lightening additives and skin lightening compositions having an acetylcholinesterase inhibitor are described. The compositions are suitable for topical application and may comprise inhibitors like galanthamine, taspine or both.Type: GrantFiled: December 10, 2008Date of Patent: August 21, 2012Assignee: Conopco, Inc.Inventor: Stephen Alan Madison
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Publication number: 20120207769Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: ApplicationFiled: April 26, 2012Publication date: August 16, 2012Applicant: NOVARTIS AGInventors: Mark G. PALERMO, Sushil Kumar SHARMA, Christopher STRAUB, Run-Ming WANG, Leigh ZAWEL, Yanlin ZHANG, Zhuoliang CHEN, Yaping WANG, Fan YANG, Wojciech WRONA, Gang LIU, Mark G. CHAREST, Feng HE
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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: 20120196846Abstract: The present invention relates to anti-RSV compounds of Formula (I) and methods for use of the compounds in the treatment and prevention of RSV infection.Type: ApplicationFiled: July 7, 2010Publication date: August 2, 2012Applicant: Gilead Sciences, Inc.Inventors: Richard L. Mackman, David Sperandio, Hai Yang
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Publication number: 20120190648Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, a stereoisomer or a mixture in all proportions of stereoisomers thereof, in particular a mixture of enantiomers, such as a racemic mixture, wherein R represents a (C1-C6)alkyl or (C1-C6)alkenyl group, optionally substituted by one or more groups chosen among an halogen atom, ORa, SRb, NRcRd, PO(ORe)(ORf), CO2Rg, SO2Rh SO3R1, P0(0H)(CH(0H)Rk), CN, N3 and NH—C(?NH)NH2, with Ra, Rb, Rc and Rd, representing, independently of each other, an hydrogen atom, a (C1-C6)alkyl group or a —CO—(C1-C6)alkyl group, Re, Rf, Rg, Rh and R1 representing, independently of each other, an hydrogen atom or a (C1-C6)alkyl group, and Rk representing an aryl or heteroaryl group, said group being optionally substituted by one or more groups selected from an halogen atom and NO2, as well as to the use thereof and to a process for preparing such a compound, to a pharmaceutical composition containing it and to synthesis intermediates.Type: ApplicationFiled: July 23, 2010Publication date: July 26, 2012Inventors: Philippe Jubault, Jean-Charles Quirion, Gerald Lemonnier, Cedric Lion
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Publication number: 20120189642Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (a) and include tautomers, solvates, prodrugs, esters, and deuterates thereof, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, ring C, m, n, p, q, -L1-, -L2-, L3-, and L4- is selected independently and as defined herein. The compounds of the invention have, surprisingly and advantageously, improved solution stability. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers Disease, are also disclosed.Type: ApplicationFiled: October 6, 2010Publication date: July 26, 2012Applicant: Schering CorporationInventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh, Lingyan Wang, Wei Li
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Publication number: 20120184531Abstract: The present invention relates to benzofuro[3,2-c]pyridine and azepine analogs as serotonin sub-type 6 (5-HT6) modulators, pharmaceutical compositions including these compounds, methods of preparation, and use thereof. These compounds are useful in the treatment of central nervous system disorders including obesity, metabolic syndrome, cognition, schizophrenia, attention deficit hyperactivity disorder, bipolar disorder, rare and orphan diseases, and sleep disorders. The subject compounds have the structure of formula (I) with the substituents being described herein.Type: ApplicationFiled: January 18, 2012Publication date: July 19, 2012Applicant: ALBANY MOLECULAR RESEARCH, INC.Inventors: Peter R. GUZZO, Alan J. HENDERSON, Matthew ISHERWOOD, Chong Yew LEE, Animesh GHOSH, He ZHAO
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Publication number: 20120184532Abstract: Prodrugs of galantamine or its 3-hydroxy metabolite with amino acids or short peptides, pharmaceutical compositions containing such prodrugs and methods for treating a memory or cognition disorder with the galantamine prodrugs are provided herein. Prodrugs having side chains of valine, phenylalanine, tyrosine or para amino benzoic acid and mono-, di- and tripeptides thereof are preferred. Additionally, methods for avoiding or minimizing the adverse gastrointestinal side effects associated with galantamine administration, as well as improving the pharmacokinetics of galantamine are provided herein.Type: ApplicationFiled: July 23, 2010Publication date: July 19, 2012Applicant: SHIRE LLCInventors: Richard Franklin, Bernard T. Golding, Robert G. Tyson
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Publication number: 20120183563Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): (I) and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-,L2-, and L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (A?) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers disease, are also disclosed.Type: ApplicationFiled: October 6, 2010Publication date: July 19, 2012Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming, Ulrich Iserloh, Jeffrey A. Misiaszek, Guoqing Li
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Publication number: 20120178740Abstract: The invention relates to compounds of general formula (I) wherein A, R1, R2, R3, R4, R5, R9, m and n are defined as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, as JAK kinase and protein tyrosine kinase inhibitors for preventing, treating or ameliorating diseases and complications thereof, including, for example, psoriasis, atopic dermatitis, rosacea, lupus, multiple sclerosis, rheumatoid arthritis, Type I diabetes, asthma, cancer, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, leukaemia, eye diseases such as diabetic retinopathy and macular degeneration as well as other autoimmune diseases and indications where immunosuppression would be desirable for example in organ transplantation.Type: ApplicationFiled: July 8, 2010Publication date: July 12, 2012Applicant: LEO PHARMA A/SInventors: Simon Feldbæk Nielsen, Daniel Rodriguez Greve, Carsten Ryttersgaard, Gunnar Grue-Sørensen, Erik Rytter Ottosen, Tina Dahlerup Poulsen, Søren Christian Schou, Anthony Murray
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Patent number: 8217031Abstract: The present invention relates to a compound represented by formula [1] or a pharmaceutically acceptable salt thereof: In formula [1], one of X and Y is CH and the other is oxygen or sulfur; R is hydrogen, etc.; Z is hydrogen, etc.; Ar is phenyl, etc.; and n is 1 or 2 and or m is 1 or 2, excluding compounds where n is 2 and m is 2 simultaneously. Also provided is a pharmaceutical composition comprising a compound of formula [1] or a pharmaceutically acceptable salt thereof as an active ingredient. The composition is usable as an agent for the prevention or treatment of depression, panic disorder, anxiety, obsessive-compulsive disorder, chronic pain, fibromyalgia, obesity, stress urinary incontinence, and overactive bladder.Type: GrantFiled: March 28, 2008Date of Patent: July 10, 2012Assignee: Nippon Shinyaku Co., Ltd.Inventors: Masato Matsuoka, Tatsuya Oyama
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Publication number: 20120172349Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.Type: ApplicationFiled: December 29, 2011Publication date: July 5, 2012Inventors: Francesco G. Salituro, Jeffrey Saunders, Shunqi Yan
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Publication number: 20120171303Abstract: Compositions comprising melatonin and one or more carotenoids and methods for using such compositions for enhancing cognitive and related functions such as reducing or preventing a decline of social interaction, reducing or preventing age-related behavioral changes, increasing trainability, improving attention, maintaining optimal brain function, facilitating learning and memory, reducing memory loss, and preventing or treating cognitive decline caused by dementia in an animal. Preferably, the compositions are food compositions useful for enhancing cognitive function in humans and companion animals.Type: ApplicationFiled: September 2, 2010Publication date: July 5, 2012Inventors: Brian Michael Zanghi, Ziad Saad Ramadan
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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: 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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Patent number: 8207159Abstract: The invention relates to the use of galanthamine, as free base or as acid addition salt, for the treatment of cerebral, central nervous or psychiatric symptoms, defunctionalization manifestations or disorders occurring through intake of psychotropic substances as a consequence of occasional or chronic abuse of addictive substances, intoxicants or medicines, or as side effects of the use, especially repeated or prolonged, as intended of medicaments, or as an effect of use, in particular repeated or prolonged, not as intended of medicaments, or as a result of acute poisoning by psychotropic toxic substances, or as a result of chronic exposure to toxic substances with a psychotropic effect in humans or other vertebrates.Type: GrantFiled: April 18, 2002Date of Patent: June 26, 2012Assignee: HF Arzneimittelforschung GmbHInventors: Klaus Opitz, Joachim Moormann, Thomas Hille, Frank Becher
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Patent number: 8207158Abstract: The present invention relates to novel compounds of Formula (I): which act as 5HT2C receptor modulators. These compounds are useful in pharmaceutical compositions whose use includes the treatment of obesity.Type: GrantFiled: May 27, 2011Date of Patent: June 26, 2012Assignee: Arena Pharmaceuticals, Inc.Inventors: Brian Smith, Jeffrey Smith
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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: 20120157410Abstract: The invention relates to compositions, conjugates and methods comprising pyridazine compounds and cholinesterase inhibitors for modulation of cellular pathways (e.g., signal transduction pathways), for treatment or prevention of inflammatory diseases (e.g., Alzheimer's disease), for research, drug screening, and therapeutic applications.Type: ApplicationFiled: February 17, 2012Publication date: June 21, 2012Applicants: U.S. Government, National Institute of Health (NIH), U.S. Department of Health and Human Services (DHSS),Inventors: D. Martin WATTERSON, Linda VAN ELDIK, Wenhui HU
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Publication number: 20120148603Abstract: In its many embodiments, the present invention provides provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (I): and tautomers thereof, and solvates, prodrugs, esters, and deuterates of said compounds and said tautomers, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, R11, ring A, ring B, m, n, p, q, r, -L1-, L2-, and L3- is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimers Disease, are also disclosed.Type: ApplicationFiled: October 6, 2010Publication date: June 14, 2012Applicant: Schering CorporationInventors: Andrew W. Stamford, Jared N Cumming
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Publication number: 20120148495Abstract: The present invention provides methods and compositions for treating subjects suffering from a disorder associated with a nicotinic acetylcholine receptor (nAChR), methods for treating a subject having a disorder that would benefit from an increase in neural plasticity, and methods for modulating the plasticity of the primary visual cortex in subjects by modulating the expression, stability, and/or activity of Lynx1.Type: ApplicationFiled: November 11, 2011Publication date: June 14, 2012Applicants: Technology and Innovation Development Office, President and Fellows of Harvard CollegeInventor: Takao K. Hensch
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Publication number: 20120135953Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: ApplicationFiled: August 6, 2010Publication date: May 31, 2012Applicant: Tibotec PharmaceuticalsInventors: David Mc Gowan, Samuel Dominique Demin, Stefaan Julien Last, Koen Vandyck, Pierre Jean-Marie Bernard Raboisson
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Publication number: 20120129838Abstract: Provided are a pharmaceutical composition, a cosmetic composition and health foods for preventing and treating alopecia disorder, which include a norgalanthamine compound as an active ingredient. Since the norgalanthamine compound has an effect on growth and proliferation of dermal papilla cells that play an important role in hair growth, the norgalanthamine compound may be used for the pharmaceutical composition, the cosmetic composition and health foods, which are useful in preventing and treating alopecia disorder.Type: ApplicationFiled: November 27, 2009Publication date: May 24, 2012Applicant: The Industry & Academic Cooperation in Chungnam National UniversityInventors: Young-Ho Kim, Hee Kyoung Kang, Sang Cheol Kim, Jung Il Kang, Eun Sook Yoo, Ki Ho Kim, Young Heui Kim
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Publication number: 20120107300Abstract: Cannabinoid compositions and methods of administering said cannabinoid compositions are disclosed. The cannabinoid compositions disclosed herein include compounds which have been strategically selected to eliminate, or least mitigate, one of the negative side effects associated with consuming cannabinoids. A daytime formula includes compounds aimed at nullifying the negative side effects that cannabinoid consumption has on a patient's daily operations and activities. A nighttime formula includes compounds aimed at nullifying the negative side effects that cannabinoid consumption has a patient's sleep.Type: ApplicationFiled: November 1, 2010Publication date: May 3, 2012Inventor: Jeffrey Nathan Schirripa
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Publication number: 20120101082Abstract: The present invention concerns compounds inter alia according to general formula 1a. Compounds according to the invention are vasopressin V1a receptor antagonists. Pharmaceutical compositions of the compounds are useful as treatment of dysmenorrhoea.Type: ApplicationFiled: December 19, 2011Publication date: April 26, 2012Inventors: ANDRZEJ ROMAN BATT, MARTIN LEE STOCKLEY, MICHAEL BRYAN ROE, CELINE Marguerite Simone HEENEY, ANDREW JOHN BAXTER, PETER HUDSON, RACHEL HANDY
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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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Patent number: 8153621Abstract: The present invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist. In addition, the invention relates to a composition comprising phentermine and a selective 5HT-2C receptor agonist having Formula (I): or a pharmaceutically acceptable salt, solvate or hydrate thereof. These compositions are useful in pharmaceutical compositions whose use includes the treatment of obesity.Type: GrantFiled: December 21, 2005Date of Patent: April 10, 2012Assignee: Arena Pharmaceuticals, Inc.Inventors: Dominic P. Behan, Brian M. Smith, Christina Bjenning
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Publication number: 20120083486Abstract: A kit, composition, product or medicament for treating cognitive impairment is provided, which includes a therapeutic agent for neurodegenerative disease and a heterocyclic compound represented by the following General Formula (I): or a hydrate thereof, a solvate thereof or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 15, 2011Publication date: April 5, 2012Applicant: ZENYAKU KOGYO KABUSHIKIKAISHAInventors: Yoshimasa YAMAGUCHI, Toshiyuki Matsuno, Kenichi Saitoh
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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: 20120046272Abstract: The present invention describes a series of therapeutically active compounds of formula I, X—Y—Z??(I) that are useful for treating a disorder in a mammal. In the formula I, X and Z, which may be same or different, are independently selected from substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkylalkyl, substituted or unsubstituted aryl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted heterocyclic group or substituted or unsubstituted heterocyclylalkyl; and Y is a linker selected from —O—, —S—, —NH—, —(CH2)n—, —CO—, —CONRa—, —NRaCO—, —NRaCOO—, —COO—, —CONRaCO—, —CONRaCOO— and —COOCOO—.Type: ApplicationFiled: August 19, 2011Publication date: February 23, 2012Applicant: GRUNENTHAL GMBHInventor: Ramesh SESHA
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Publication number: 20120040965Abstract: The invention relates to novel chemical compounds, searching for novel physiologically active substances, leader compounds, “molecular tools”, and drug candidates obtained on the basis of screening of combinatorial and focused libraries of the said compounds, and also to pharmaceutical composition, methods for preparation and use thereof.Type: ApplicationFiled: August 8, 2007Publication date: February 16, 2012Inventors: Frolov Yevgeniy Borisovich, Khvat Alexander Viktorovich, Malyarchuk Sergey Viktorovich, Mitkin Oleg Dmitrievich, Okun Ilya Matusovich, Kyselev Alexandr Sergeevich, Savchuk Nikolay Filippovich, Ivashchenk Andrey Alexandrovich, Ivashchenko Alexander Vasilievich
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Publication number: 20120040966Abstract: The compounds provided herein are suitable for inhibiting a virus in a patient and for treating a patient suffering from a viral infection such as an influenza virus. Also provided is a method for screening of compounds for use in treating and preventing viral infections. The assay screens compounds for activity against an influenza virus by measuring the cytopathogenic effect (CPE) of the compound on influenza infected-cells using percent cell viability as the end point.Type: ApplicationFiled: December 28, 2009Publication date: February 16, 2012Applicant: Southern Research Institute Office of Commercialization and Intellectual PropInventors: Joseph A. Maddry, Bill Severson, Colleen B. Jonsson, James W. Noah, Diana L. Noah, Xi Chen
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Publication number: 20120034236Abstract: Disclosed herein are therapies for treating or preventing reoccurrence of cancer. The therapies involved inhibition of LIMK1 in conjunction with AurKA inhibition. Specifically exemplified herein is the administration of an AurKA inhibitor in conjunction with a LIMK1 RNA interfering molecule.Type: ApplicationFiled: June 23, 2011Publication date: February 9, 2012Inventor: Ratna Chakrabarti
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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: 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: 20120015935Abstract: The present invention relates to substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tetrahydropyrazolo-pyrido-azepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: ArQule, Inc.Inventors: Jean-Marc Lapierre, Rui-Yang Yang, Nivedita Namdev, Jeffrey S. Link
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Publication number: 20120009278Abstract: Compositions and methods are described for delaying the onset of the symptoms of Alzheimer's disease in humans. The compositions can include curcumin, piperine, oleic acid, oleanolic acid, ursolic acid, galantamine, and huperzine A, among other compounds. Curcumin is an antioxidant, while galantamine and huperzine A inhibit the activity of acetylcholinesterase in the brain. Piperine and oleic acid increase the bioavailability and gastrointestinal absorption of curcumin, galantamine, huperzine A, and other nutrients. The composition can also include at least one of phytic acid, piracetam, aniracetam, or indium.Type: ApplicationFiled: September 19, 2011Publication date: January 12, 2012Inventor: Stephen C. Perry
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Publication number: 20120004206Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome, and other diseases and conditions that are mediated by excessive glucocorticoid action.Type: ApplicationFiled: August 25, 2011Publication date: January 5, 2012Inventors: Marina A. Pliushchev, Dariusz Wodka, Bryan K. Sorensen, James T. Link
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Patent number: 8088790Abstract: 1H-Imidazo[4,5-c]quinolin-4-amines with a hydroxy, alkoxy, hydroxyalkoxy, or alkoxyalkoxy substituent at the 2-position, pharmaceutical compositions containing these compounds, methods of making the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: November 3, 2006Date of Patent: January 3, 2012Assignee: 3M Innovative Properties CompanyInventors: Tushar A. Kshirsagar, Philip D. Heppner, Scott E. Langer
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Publication number: 20110319387Abstract: The invention relates to a compound of the following formula (I), or to a pharmaceutically acceptable salt thereof or to a stereoisomer or mixture of stereoisomers at any proportions, where: X1 is a CH2 or C?O group; X2 is a linear saturated or unsaturated carbohydrate chain with 8 to 24 carbon atoms; R1 is a hydrogen atom or an OH or (C1-C6)alkoxy group such as methoxy; and R2 is a CH3 or CH2OR3 group, with R3 being a hydrogen atom or a (C1-C6)alkyl, CO—(C1-C6)alkyl or NH—(C1-C6)alkyl group. The invention also relates to the use of said compound as a drug, in particular for treating neurodegenerative diseases, and to a method for preparing same.Type: ApplicationFiled: March 2, 2010Publication date: December 29, 2011Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS)Inventors: Fanny Schmidt, Bruno Figadere, Rita Raisman-Vozari, Pierre Champy
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Publication number: 20110319386Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on muscarinic receptor modulation, such as via inhibition of acetylcholine esterase (AChE) activity, alone or in combination with another neurogenic agent to stimulate or activate the formation of new nerve cells.Type: ApplicationFiled: June 10, 2011Publication date: December 29, 2011Applicant: BrainCells Inc.Inventors: Carrolee Barlow, Todd A. Carter, Kai Treuner, Michael Lee
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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: 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: 20110312943Abstract: 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