The Additional Hetero Ring Consists Of One Nitrogen And Four Carbons (e.g., Nicotine, Etc.) Patents (Class 514/343)
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Publication number: 20150126485Abstract: The present invention relates to compounds of formula (I): in which Y, Y, R, R 2, R 3 and R 4 are defined in the Summary of the Invention; capable of inhibiting the tyrosine kinase enzymatic activity of the Abelson protein (ABL1), the Abelson-related protein (ABL2) and related chimeric proteins, in particular BCR-ABL1. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancers.Type: ApplicationFiled: May 9, 2013Publication date: May 7, 2015Applicant: Novartis AGInventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
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Publication number: 20150126522Abstract: This invention relates to novel substituted benzamides according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.Type: ApplicationFiled: May 15, 2013Publication date: May 7, 2015Applicant: GlaxoSmithKline LLCInventors: Joelle Lorraine Burgess, Celine Duquenne, Steven David Knight, William Henry Miller, Kenneth Allen Newlander, Sharad Kumar Verma
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Publication number: 20150126490Abstract: The present invention provides a compound of Formula (I) or a salt thereof; and therapeutic uses of these compounds. The present invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds with a therapeutic co-agent.Type: ApplicationFiled: October 29, 2014Publication date: May 7, 2015Applicant: Novartis AGInventors: Jeffrey T. BAGDANOFF, Yu DING, Wooseok HAN, Zilin HUANG, Qun JIANG, Jeff Xianming JIN, Xiang KOU, Patrick LEE, Mika LINDVALL, Zhongcheng MIN, Yue PAN, Sabina PECCHI, Keith Bruce PFISTER, Daniel POON, Vivek RAUNIYAR, Xiaojing Michael WANG, Qiong ZHANG, Jianguang ZHOU, Shejin ZHU
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Publication number: 20150119378Abstract: 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: October 24, 2014Publication date: April 30, 2015Inventors: Srinivasa Rao Akireddy, Scott R. Breining
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Publication number: 20150119384Abstract: The present invention relates to ethynyl derivatives of formula I X, O, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined hereinor to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.Type: ApplicationFiled: January 6, 2015Publication date: April 30, 2015Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Patent number: 9018206Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: GrantFiled: September 12, 2012Date of Patent: April 28, 2015Assignees: AbbVie Deutschland GmbH & Co. KG, AbbVie Inc.Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20150111928Abstract: A water soluble film that is disintegrable in the oral cavity to deliver an active agent is provided. The disintegrable film includes at least one water soluble polymer and an active agent. Also provided are methods for preparing the disintegrable oral film and for using the disintegrable film to administer an effective dosage of an active agent into the oral cavity for absorption through the oral mucosa. According to certain embodiments, the disintegrable film includes at least one water soluble polymer and a nicotine active.Type: ApplicationFiled: October 24, 2014Publication date: April 23, 2015Inventors: Christopher Edward FANKHAUSER, Greg SLOMINSKI, Stephan MEYER
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Devices for thermally induced transformations controlled by irradiation of functionalized fullerenes
Patent number: 9011309Abstract: An electromagnetic radiation activated device comprises a property changing material and at least one functionalized fullerene that upon irradiation of the functionalized fullerenes with electromagnetic radiation of one or more frequencies a thermally activated chemical or physical transformation occurs in the property changing material. The thermal activated transformation of the property changing material is triggered by the heating or combustion of the functionalized fullerenes upon their irradiation. The device can include a chemical agent that is embedded in the property changing material and is released when the material is heated by the functionalized fullerenes upon irradiation.Type: GrantFiled: May 12, 2011Date of Patent: April 21, 2015Assignee: University of Florida Research Foundation, Inc.Inventors: Vijay Krishna, Karl Zawoy, Brij M. Moudgil, Benjamin L. Koopman, Nathanael Ian Stevens, Kevin William Powers -
Publication number: 20150105386Abstract: The present invention relates to novel 4-(4-pyridyl)-benzamides of the formula (I). The compounds I possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of Rho kinases (ROCKs).Type: ApplicationFiled: October 24, 2014Publication date: April 16, 2015Inventors: Helmut Mack, Nicole Teusch, Bernhard K. Muller, Wilfried Hornberger, Michael F. Jarvis, Daryl Sauer, Steven L. Swann, Jr., Dominique Bonafoux, Ryan Keddy, Adrian Donald Hobson, Anil Vasudevan
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Publication number: 20150105392Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Paul R. Fatheree, Robert Murray McKinnell
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Publication number: 20150105431Abstract: The present invention relates to nicotine lozenge compositions comprising reduced levels of buffering agents from traditional nicotine lozenges and which provide optimal oral pH and prompt nicotine absorption in a smaller, more convenient dosage form.Type: ApplicationFiled: December 17, 2014Publication date: April 16, 2015Inventor: Li-Lan CHEN
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Patent number: 9006271Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C1-4 alkyl useful in the treatment of diseases and conditions for which antagonism of NK1 receptor is beneficial.Type: GrantFiled: May 16, 2014Date of Patent: April 14, 2015Assignee: Nerre Therapeutics LimitedInventors: Giuseppe Alvaro, Agostino Marasco
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Publication number: 20150098996Abstract: A nicotine lozenge provided herein includes a body that is partially or wholly receivable in an oral cavity. The body includes a soluble-fiber matrix and nicotine or a derivative thereof dispersed in the soluble-fiber matrix. In some cases, a nicotine lozenge provided herein includes at least 40 weight percent of soluble fiber. In some cases, soluble fiber in a nicotine lozenge provided herein can include maltodextrin. The nicotine lozenge is adapted to release the nicotine or a derivative thereof from the body when the body is received within the oral cavity of an adult consumer and exposed to saliva. A method of making nicotine lozenges provided herein includes forming a molten mixture of at least 40 weight percent soluble fiber, nicotine, and less than 15 weight percent water while maintaining a mixture temperature of less than 150° C. and portioning the molten mixture into a plurality of nicotine lozenges. In some cases, the ingredients can be mixed to form the molten mixture in an extruder.Type: ApplicationFiled: October 3, 2014Publication date: April 9, 2015Inventors: Feng Gao, Diane L. Gee, Phillip M. Hulan, Shuzhong Zhuang, William J. Burke
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Publication number: 20150099786Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, R4, Q, Y, A and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula Ia and Ib in which R1, r, R2b, R3a, R3b, R4, Y and X have the meanings mentioned in the claims, including the tautomers thereof and the pharmaceutically suitable salts thereof.Type: ApplicationFiled: December 15, 2014Publication date: April 9, 2015Inventors: Helmut Mack, Andreas Kling, Katja Jantos, Achim Moeller, Wilfried Hornberger, Charles W. Hutchins
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Publication number: 20150099787Abstract: One aspect of the present invention relates to substituted pyridines and pharmaceutially acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels.Type: ApplicationFiled: October 15, 2014Publication date: April 9, 2015Applicant: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-sen Lai
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Publication number: 20150099740Abstract: A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-?-hydroxysteroid dehydrogenase Type 1 enzyme activity.Type: ApplicationFiled: December 12, 2014Publication date: April 9, 2015Inventors: R. Scott Bitner, Kaitlin E. Browman, Michael E. Brune, Yixian Chen, Jurgen Dinges, Karla Drescher, Peer Jacobson, Hwan-soo Jae, Ravi Kurukulasuriya, James T. Link, David J. Madar, Jyoti R. Patel, Marina A. Pliushchev, Jeffrey J. Rohde, Lynne E. Rueter, Qi Shuai, Bryan K. Sorensen, Jiahong Wang, Karsten M. Wicke, Martin Winn, Dariusz Wodka, Vince Yeh, Hong Yong
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Patent number: 8999971Abstract: Disclosed herein are methods for controlling the activity of hypoxia-inducible transcription factor 1-alpha (HIF-1?) and diseases, conditions, or syndromes related thereto, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. Further disclosed are pharmaceutical compositions comprising HIF-1? prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related thereto the activity of HIF-1?.Type: GrantFiled: August 21, 2014Date of Patent: April 7, 2015Assignee: Aerpio Therapeutics Inc.Inventors: Robert Shalwitz, Joseph H. Gardner
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Publication number: 20150080364Abstract: Provided herein are carbamate compounds which may be useful in the treatment of for example, pain, solid tumors and/or obesity.Type: ApplicationFiled: March 15, 2013Publication date: March 19, 2015Applicants: Abide Therapeutics, Inc., The Scripps Research InsitituteInventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Dong-Hui Wang, Olivia Weber, Benjamin F. Cravatt, Micah J. Niphakis, Armand Cognetta, Jae Won Chang
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Publication number: 20150080381Abstract: Method of treating alopecia and acne with are disclosed.Type: ApplicationFiled: April 12, 2013Publication date: March 19, 2015Inventors: Mark G. Currie, Yueh-tyng Chien
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Publication number: 20150080365Abstract: This invention relates to certain heteroaryl compounds for use as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of helminth infections and the treatment of parasitosis caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.Type: ApplicationFiled: March 27, 2013Publication date: March 19, 2015Inventors: Michael Berger, Marko Eck, Christopher Kern
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Publication number: 20150080362Abstract: The present description relates to compounds and forms and pharmaceutical compositions thereof and methods for use thereof to treat or ameliorate bacterial infections caused by wild-type and multi-drug resistant Gram-negative and Gram-positive pathogens.Type: ApplicationFiled: August 29, 2012Publication date: March 19, 2015Applicant: PTC THERAPEUTICS, INC.Inventors: Arthur Branstrom, Vara Prasad Venkata Nagendra Josyula, Michael Andrew Arnold, Aleksey I. Gerasyuto, Gary Karp, Jiashi Wang, Tamil Arasu, John David Baird, Wu Du, Olya Ginzburg, Yi Jin Kim Gorske, Jana Narasimhan, Srinivasa Peddi, Hongyan Qi, Sean Wesley Smith, Anthony Allan Turpoff, Richard Gerald Wilde, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang
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Patent number: 8980886Abstract: The present invention relates to novel anthranilic acid derivatives of the general formula (I) in which R1, R2, R3, R4, R5, Qx, A, Qy and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and to a plurality of processes for their preparation.Type: GrantFiled: June 14, 2011Date of Patent: March 17, 2015Assignee: Bayer Cropscience AGInventors: Rüdiger Fischer, Christoph Grondal, Markus Heil, Heinz-Juergen Wroblowsky, Ernst Rudolf Gesing, Arnd Voerste, Ulrich Görgens
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Publication number: 20150072959Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: November 13, 2014Publication date: March 12, 2015Inventors: Dane Goff, Jing Zhang, Catherine Sylvain, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding
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Publication number: 20150071972Abstract: A composition intended to be employed for therapeutic purposes incorporates a nicotinic compound, a sugar substitute, and a sugar alcohol syrup. Representative forms of nicotine include free base (e.g., as a mixture of nicotine and microcrystalline cellulose), a nicotine salt (e.g., as nicotine bitartrate) or nicotine polacrilex. The composition is useful for treatment of central nervous system conditions, diseases, and disorders, and as a nicotine replacement therapy.Type: ApplicationFiled: November 13, 2014Publication date: March 12, 2015Inventors: Darrell Holton, JR., Nelly Fransén, Matt Reddick
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Publication number: 20150065464Abstract: The present disclosure relates to substituted amide compounds that are inhibitors of Fatty Acid Amide Hydrolase (FAAH), their stereoisomers, tautomers, prodrugs, polymorphs, solvates, pharmaceutically acceptable salts, and pharmaceutical compositions containing them.Type: ApplicationFiled: September 21, 2012Publication date: March 5, 2015Inventors: Rajendra Kharul, Debnath Bhuniya, Kasim A. Mookhtiar, Umesh Singh, Atul Hazare, Satish Patil, Laxmikant Datrange, Mahesh Thakkar
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Patent number: 8968770Abstract: A multi-part kit for administering at least one active pharmaceutical ingredient including at least one piece of chewing gum including the active pharmaceutical ingredient, the piece of chewing gum comprising gum base; and at least one further flavor-containing formulation; wherein the gum base content of the at least one further flavor-containing formulation is less than 70% by weight of the gum base content of said piece of chewing gum.Type: GrantFiled: June 20, 2011Date of Patent: March 3, 2015Assignee: Fertin Pharma A/SInventors: Kurt Møller Pedersen, Jette Bæk Andersen
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Patent number: 8969383Abstract: The present invention relates to picolinamide derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.Type: GrantFiled: June 12, 2014Date of Patent: March 3, 2015Assignee: RaQualia Pharma Inc.Inventors: Hirohide Noguchi, Tadashi Inoue, Mikio Morita, Yoshimasa Arano
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Patent number: 8969338Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, Y, R1, R2, R2?, R3, R3? and R8 are described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).Type: GrantFiled: September 27, 2012Date of Patent: March 3, 2015Assignee: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Patent number: 8969389Abstract: In one aspect, the invention relates to substituted 6-methylnicotinamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: May 24, 2011Date of Patent: March 3, 2015Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Shaun R. Stauffer, Ya Zhou, Jason Manka, Gregor McDonald, José Manuel Bartolome-Nebreda
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Publication number: 20150057248Abstract: Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors.Type: ApplicationFiled: September 1, 2014Publication date: February 26, 2015Applicant: The Board of Regents of The University of Texas SystemInventors: Jia Zhou, Haijun Chen, Kenneth M. Johnson, Cheng Z. Wang
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Publication number: 20150057260Abstract: The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: ApplicationFiled: August 22, 2014Publication date: February 26, 2015Applicant: Genentech, Inc.Inventors: Nicole Blaquiere, Georgette Castanedo, Jianwen A. Feng, Baihua Hu, Steven Staben, Po-wai Yuen, Guosheng Wu, Xingyu Lin, Jason Burch
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Publication number: 20150051200Abstract: Described are pharmacological compositions comprising a gum resin; a pharmacologically active agent and a topically acceptable volatile solvent for the gum resin and active agent. Also described are methods for the transdermal or transmucosal delivery of a pharmacologically active agent using such compositions.Type: ApplicationFiled: September 5, 2014Publication date: February 19, 2015Applicant: Jaleva Pharmaceuticals, LLCInventors: Alex Battaglia, Eva Beim
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Publication number: 20150051253Abstract: The present invention is directed to (?)-(2R,3S)-2-amino-3-hydroxy-3-pyridin-4-yl-1-pyrrolidin-1-yl-propan-1-one (L)-(+)tartrate salt, a pharmaceutical composition comprising said salt, a process for making said salt, and the use of said salt in the treatment of pain.Type: ApplicationFiled: August 14, 2014Publication date: February 19, 2015Inventors: Gyorgy F. Ambrus, Katherine C. Kurjan, Jacopo Zanon, Giovanna Libralon, Carla De Faveri
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Patent number: 8957213Abstract: The present invention relates to ethynyl derivatives of formula I X, G, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.Type: GrantFiled: April 23, 2012Date of Patent: February 17, 2015Assignee: Hoffman-La Roche Inc.Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Publication number: 20150045364Abstract: The present invention provides pyridine and pyrazine derivatives which restore or enhance the function of mutant and/or wild type CFTR to treat cystic fibrosis, primary ciliary dyskinesia, chronic bronchitis, chronic obstructive pulmonary disease, asthma, respiratory tract infections, lung carcinoma, xerostomia and keratoconjunctivitis sire, or constipation (IBS, IBD, opioid induced). Pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: October 23, 2014Publication date: February 12, 2015Applicant: NOVARTIS AGInventors: Urs BAETTIG, Kamlesh BALA, Emma BUDD, Lee EDWARDS, Catherine HOWSHAM, Glyn Alan HUGHES, Darren Mark LEGRAND, Katrin SPIEGEL
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Patent number: 8952038Abstract: A smokeless tobacco product or medicinal nicotine product includes nicotine and camphor dissolved in a non-flavored oily carrier. Preferably, the camphor is present in a concentration ranging from about 600 ppm to about 1300 ppm. Also disclosed are methods of making such products.Type: GrantFiled: March 25, 2011Date of Patent: February 10, 2015Assignee: Philip Morris USA Inc.Inventors: Gerd Kobal, Prasad Polur, Maria Gogova, Diana McKinney
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Patent number: 8952001Abstract: The invention relates to amino-heteroaryl derivatives having the general Formula I or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.Type: GrantFiled: December 20, 2010Date of Patent: February 10, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Simon James Anthony Grove, Angus John Morrison, Craig Jamieson, Ronald Palin, John Kinnaird Ferguson Maclean
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Patent number: 8940772Abstract: The present invention relates to nicotine lozenge compositions comprising reduced levels of buffering agents from traditional nicotine lozenges and which provide optimal oral pH and prompt nicotine absorption in a smaller, more convenient dosage form.Type: GrantFiled: June 26, 2013Date of Patent: January 27, 2015Assignee: GlaxoSmithKline, LLCInventor: Li-Lan Chen
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Publication number: 20150024012Abstract: The invention discloses an article for swaddling in the mouth to deliver pharmacologically active substances, particularly nicotine, in combination with dyes or flavorings, across the buccal membranes when said article is swaddled in the mouth. The article comprises a non-edible substantially cylindrical core element, such as a toothpick, and the indicator element may be a bulb, trinket, insignia or other marking. In a preferred embodiment, the invention makes a social statement about the beneficial uses of nicotine. Methods for using the invention to mitigate sensations of nervousness and boredom are also disclosed.Type: ApplicationFiled: October 6, 2014Publication date: January 22, 2015Inventor: Evan Grossman
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Publication number: 20150025111Abstract: The present invention provides salt adducts comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted, methods of their preparation, and pharmaceutical compositions and medicaments comprising them.Type: ApplicationFiled: October 3, 2014Publication date: January 22, 2015Inventors: Rina Yamin, Dalia Megiddo
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Patent number: 8937055Abstract: The present invention provides a compound having a muscle cell or adipocyte differentiation regulating action, useful for the prophylaxis or treatment of diseases such as diabetes, obesity, dyslipidemia and the like, and the like, and having superior efficacy. The present invention provides a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof.Type: GrantFiled: July 14, 2011Date of Patent: January 20, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Osamu Ujikawa, Kazuaki Takami, Nobuyuki Takakura, Nozomu Sakai
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Publication number: 20150018341Abstract: The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.Type: ApplicationFiled: December 28, 2012Publication date: January 15, 2015Applicant: CENTAURUS BIOPHARMA CO., LTD.Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Rong Yu, Wei Hu, Na Zhao, Yong Peng, Hong Luo, Yongxin Han
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Publication number: 20150018334Abstract: The present invention relates to aryl pyrazoles, and pharmaceutically acceptable salts thereof. The aryl pyrazoles of the present invention are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorders. The present invention also relates to pharmaceutical compositions comprising the aryl pyrazoles of the present invention, methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: July 14, 2014Publication date: January 15, 2015Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, John BROADWATER, Steven Richard BRUNETTE, Thomas Martin KIRRANE, JR., Hossein RAZAVI, Robert SIBLEY, Lana Louise SMITH KEENAN, Qiang ZHANG
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Publication number: 20150011553Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the field of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.Type: ApplicationFiled: July 3, 2014Publication date: January 8, 2015Inventors: Ulrich GÖRGENS, Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Koichi Araki, Norio Sasaki, Kei Domon, Mamoru Hatazawa, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
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Patent number: 8927730Abstract: Compounds and related compositions and methods as can be used to selectively inhibit neuronal nitric oxide synthase and as can be employed in the treatment of various neurodegenerative diseases.Type: GrantFiled: September 30, 2011Date of Patent: January 6, 2015Assignee: Northwestern UniversityInventors: Richard B. Silverman, Fengtlan Xue
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Patent number: 8927534Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.Type: GrantFiled: January 31, 2007Date of Patent: January 6, 2015Assignee: Shire Orphan Therapies GmbHInventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
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Patent number: 8921356Abstract: The disclosure is directed at least in part to compositions and methods comprising nicotinic agonists for treating e.g., nervous system disorders, in particular, to combination therapies that include a nicotinic agonist (for example, nicotine) and a nicotinic acetylcholine receptor desensitization inhibitor (for example, opipramol).Type: GrantFiled: August 24, 2012Date of Patent: December 30, 2014Assignee: NeuroDerm, Ltd.Inventor: Eliahu Heldman
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Patent number: 8921364Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.Type: GrantFiled: December 20, 2012Date of Patent: December 30, 2014Assignee: Rhizen Pharmaceuticals SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Gayatri Swaroop Merikapudi, Swaroop Kumar V. S. Vakkalanka
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Publication number: 20140378428Abstract: Disclosed are heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. The compounds are useful for treating a mammal suffering from any one of a range of therapeutic indications, including Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism, trichotillomania, and hypothermia.Type: ApplicationFiled: November 9, 2012Publication date: December 25, 2014Applicants: Georgetown University, Duke UniversityInventors: Yingxian Xiao, Kenneth J. Kellar, Milton L. Brown, Mikell A. Paige, Yong Liu, Edward D. Levin, Amir H. Rezvani
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Publication number: 20140378512Abstract: The invention relates to a pharmacologically active combination, having utility in treating insomnia patients, which comprises: (a) at least one first active ingredient selected from melatonin, other melatonergic agents, melatonin agonists and melatonin antagonists; and (b) at least one second active ingredient selected from nicotine and nicotine receptor agonists; to use of a medicament containing component (a) with or without component (b) for alleviation of at least one adverse effect which occurs in a patient in the course of nicotine replacement therapy, or otherwise, selected from impairment of the quality of sleep, impairment of cognition and impairment of memory, as well as to a kit having utility in treating insomnia patients, which comprises components (a) and (b) in unit dosage form.Type: ApplicationFiled: September 10, 2014Publication date: December 25, 2014Applicant: NEURIM PHARMACEUTICALS (1991) LTD.Inventors: Nava ZISAPEL, Moshe LAUDON