Asymmetrical (e.g., 1,2,4-triazine, Etc.) Patents (Class 514/242)
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Patent number: 8901170Abstract: Compounds of formula (I) wherein the symbols have the meaning given in the specification, as well as processes for preparing the compounds (I), pesticidal compositions and synergistic mixtures comprising compounds (I), methods for the control of insects, acarids or nematodes by contacting the pests or their food supply, habitat or breeding grounds with a pesticidally effective amount of compounds formula (I), and a method for treating, controlling, preventing or protecting animals against infestation or infection by parasites which comprises orally, topically or parenterally administering or applying to the animals a parasiticidally effective amount of compounds of formula (I).Type: GrantFiled: June 22, 2007Date of Patent: December 2, 2014Assignee: BASF SEInventors: Matthias Pohlman, Michael Hofmann, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, Takeo Hokama, Christopher Palmer
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Patent number: 8901122Abstract: Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ cosmetic composition comprising novel active agents that enhance collagen production in the skin.Type: GrantFiled: December 20, 2012Date of Patent: December 2, 2014Assignee: Avon Products, Inc.Inventors: Uma Santhanam, Permanan Raaj Khusial
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Patent number: 8895553Abstract: The invention relates to (among other things) methods for treatment comprising administering oligomer-containing substituted aromatic triazine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.Type: GrantFiled: May 20, 2014Date of Patent: November 25, 2014Assignee: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
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Publication number: 20140343038Abstract: The present invention provides a compound represented by the following general formula (I) or a salt thereof which has a Syk inhibitory effect (in the formula R1 represents a hydrogen atom or an optionally substituted C1-C6 alkyl group; A represents a hydrogen atom, an optionally substituted C1-C8 alkyl group, an optionally substituted C2-C6 alkenyl group, an optionally substituted C2-C6 alkynyl group, an optionally substituted C3-C10 cycloalkyl group, an optionally substituted C6-C14 aromatic hydrocarbon group, an optionally substituted 4- to 10-membered unsaturated heterocyclic group, or an optionally substituted 4- to 10-membered saturated heterocyclic group, or optionally forms a 4- to 10-membered unsaturated heterocyclic ring or a 4- to 10-membered saturated heterocyclic ring together with R1 and the nitrogen atom bonded thereto; R2 represents a hydrogen atom or an optionally substituted C1-C6 alkyl group; and B represents an optionally substituted unsaturated heterocyclic group).Type: ApplicationFiled: September 28, 2012Publication date: November 20, 2014Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Toshihiro Sakamoto, Takashi Mita, Kazuaki Shibata, Yoshio Ogino, Hideya Komatani
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Publication number: 20140336048Abstract: A pesticidal mixture comprising as active ingredient a mixture of component A and component B, wherein component A is a compound of formula (I), in which Q is i or ii wherein X, Y and Z, m and n, A, G, and R, are as defined as in claim 1, and component B is a compound selected from the following insecticides: a), pymetrozine; b). a pyrethroid selected from the group consisting of cyhalothrin, lambda-cyhalothrin, gamma-cyhalothrin; c). a macrolide selected from the group consisting of abamectin, emamectin benzoate, and spinetoram; d). a diamide selected from the group consisting of chlorantraniliprole and cyantraniliprole; e). thiamethoxam; f). sulfoxaflor; g). cyenopyrafen. The present invention also relates to methods of using said mixtures for the control of plant pests.Type: ApplicationFiled: November 29, 2012Publication date: November 13, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Anke Buchholz, Fabienne Hatt, Alfred Rindlisbacher, Michel Muehlebach
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Publication number: 20140336186Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests, including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: ApplicationFiled: July 9, 2014Publication date: November 13, 2014Inventors: Thomas BRETSCHNEIDER, Eva-Maria FRANKEN, Ulrich GÖRGENS, Martin FÜSSLEIN, Achim HENSE, Joachim KLUTH, Hans-Georg SCHWARZ, Adeline KÖHLER, Olga MALSAM, Arnd VOERSTE, Angela BECKER
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Publication number: 20140336154Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II 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: July 29, 2014Publication date: November 13, 2014Inventors: Steven Do, Richard Goldsmith, Tim Heffron, Aleksandr Kolesnikov, Steven Staben, Alan G. Olivero, Michael Siu, Daniel P. Sutherlin, Bing-Yan Zhu, Paul Goldsmith, Tracy Bayliss, Adrian Folkes, Neil Pegg
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Publication number: 20140329819Abstract: Compounds of the formula (I) or (I?), wherein the substituents are as defined in claim 1, are useful as pesticides.Type: ApplicationFiled: November 20, 2012Publication date: November 6, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Sebastian Rendler, Jurgen Harry Schaetzer, Shuji Hachisu, Peter Maienfisch, Thomas Pitterna, Olivier Jacob, Jerome Yves Cassayre
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Patent number: 8864853Abstract: An additive mixture for fuels including a) at least one N-formal, b) at least one antioxidant and c) at least one corrosion inhibitor. The additive mixture ensures that the additized fuels and lubricants have biocidal and corrosion-inhibiting additization, especially when they include proportions of renewable raw materials, such as biodiesel, and when they are in contact with copper-containing surfaces.Type: GrantFiled: June 21, 2010Date of Patent: October 21, 2014Assignee: l'Air Liquide Societe Anonyme pour l'etude et L'exploitation des Procedes Georges ClaudeInventors: Wolfgang Beilfuss, Ralf Gradtke, Jennifer Knopf, Ingo Krull
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Publication number: 20140303142Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.Type: ApplicationFiled: September 28, 2012Publication date: October 9, 2014Inventors: John W. Butcher, David Witter, Christopher Dinsmore, June Kim, John Hendrix, Raksha Acharya, Sean P. Ahearn, Joon Jung, Alexey Rivkin, Philip Jones
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Publication number: 20140303112Abstract: The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity.Type: ApplicationFiled: April 9, 2013Publication date: October 9, 2014Inventors: Han-Min CHEN, Cheng-Yi KUO, Chun-Fang HUANG, Jiun-Tsai LIN
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Patent number: 8846669Abstract: Disclosed is a novel oxazolidinone derivative represented by Formula 1 above, in particular, a novel oxazolidinone compound having a cyclic amidoxime or cyclic amidrazone group. In Formula 1, R and Q are the same as defined in the detailed description. In addition, disclosed is a pharmaceutical composition for an antibiotic which includes the novel oxazolidinone derivative of Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient. The novel oxazolidinone derivative, the prodrug thereof, the hydrate thereof, the solvate thereof, the isomer thereof, and the pharmaceutically acceptable salt thereof have broad antibacterial spectrum against resistant bacteria, low toxicity and strong antibacterial effects against Gram-positive and Gram-negative bacteria and thus may be effectively used as antibiotics.Type: GrantFiled: March 29, 2012Date of Patent: September 30, 2014Assignee: Legochem Biosciences, Inc.Inventors: Young Lag Cho, Sung Yoon Baek, Sang Eun Chae, Sun Young Kim, Hong Bum Lee, Hyang Sook Lee, Kyuman Oh, Hye Jin Heo, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
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Publication number: 20140271850Abstract: Described herein is a pharmaceutical composition comprising lamotrigine as an active ingredient providing a prolonged release characteristic to allow once a day dosage regime. The composition comprises lamotrigine and a swelling agent forming a core or an extended-release composition. The core or an extended-release composition may be coated with a hydrophobic, pH-independent polymer to provide a modified extended-release composition. The formulation may comprise other pharmaceutically acceptable excipients that may act as additional release rate modifier(s), e.g., a pore forming agent in the hydrophobic polymer coat/film. Also described are the processes of preparing such dosage forms and their use.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: PHARMTAK, INC.Inventors: I-Lan Tung Sue, Jung-Chung Lee
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Publication number: 20140275077Abstract: The present application provides compounds of Formula I or salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c, Y, R3, X, E and G are as defined herein, compositions, methods of treatment and uses thereof.Type: ApplicationFiled: May 13, 2014Publication date: September 18, 2014Applicant: Cephalon, Inc.Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
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Publication number: 20140256732Abstract: The invention relates to (among other things) methods for treatment comprising administering oligomer-containing substituted aromatic triazine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.Type: ApplicationFiled: May 20, 2014Publication date: September 11, 2014Applicant: NEKTAR THERAPEUTICSInventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
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Publication number: 20140255517Abstract: In certain embodiments, the disclosure relates to methods of treating or preventing posttraumatic stress disorder comprising administering a pharmaceutical composition comprising effective amount of an angiotensin-converting enzyme inhibitor to a subject in need thereof. In certain embodiments, the angiotensin-converting enzyme inhibitor is administered in combination with an angiotensin receptor blocker.Type: ApplicationFiled: March 5, 2014Publication date: September 11, 2014Applicant: EMORY UNIVERSITYInventors: Kerry J. Ressler, Paul J. Marvar
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Publication number: 20140248378Abstract: The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, Y and Z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: July 5, 2012Publication date: September 4, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Xiao-Ling Fan Cockcroft, William Farnaby, Natasha Kinsella, Kevin Merchant, David Miller
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Patent number: 8822489Abstract: This invention relates to an abuse deterrent dosage form of opioid analgesics, wherein an analgesically effective amount of opioid analgesic is combined with a polymer to form a matrix.Type: GrantFiled: February 27, 2013Date of Patent: September 2, 2014Assignee: Acura PharmaceuticalsInventors: Vijai Kumar, David Dixon, Divya Tewari, Dilip B. Wadgaonkar
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Patent number: 8822465Abstract: The present invention relates to a quinoline derivative represented by general formula (I) or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof, wherein Ar, R1, R2, R3, X, Y and n have the meanings given in the description. The present invention also relates to the comparatively strong effect of the compound represented by general formula (I) on inhibiting c-Met kinase. The present invention further relates to the use of this compound or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof in the manufacturing of a medicament for treating the disease caused by abnormally over-expressing c-Met kinase, in particular, for treating or preventing cancer.Type: GrantFiled: March 14, 2013Date of Patent: September 2, 2014Assignee: Wuhan Shengyun Biopharma Co., Ltd.Inventor: Hua Xu
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Publication number: 20140243342Abstract: Provided are articles of manufacture, compositions and methods for prophylaxis and/or therapy for disorders involving dizziness and/or vertigo. The articles of manufacture and compositions contain lamotrigine and/or bupropion and pharmaceutically acceptable salts thereof. The compositions include pharmaceutical compositions which are intended to alleviate dizziness and/or vertigo. In certain aspects the disclosure includes articles of manufacture and kits which include printed material which provides an indication that the articles or compositions are intended to be used for prophylaxis and/or therapy of Meniere's disease or a symptom thereof.Type: ApplicationFiled: February 18, 2014Publication date: August 28, 2014Inventor: Lixin Zhang
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Publication number: 20140243343Abstract: The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The compounds are of formula I: in which R1 is a halo-alkyl group and A is an optionally substituted aromatic heterocyclic or carbocyclic ring system, or a pharmaceutically acceptable salt or solvate thereof.Type: ApplicationFiled: April 30, 2014Publication date: August 28, 2014Applicant: University of GreenwichInventors: Michael Leach, Karl Franzmann, Dieter Riddall, Laurence Harbige
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Publication number: 20140235442Abstract: A composition comprising at least a pyridylethylbenzamide derivative of general formula (I) (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.Type: ApplicationFiled: April 25, 2014Publication date: August 21, 2014Inventors: Heike HUNGENBERG, Gilbert LABOURDETTE, Albert SCHIRRING, Burkhard SCHUETZ, Anne SUTY-HEINZE, Wolfgang THIELERT, Martin VAUPEL
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Patent number: 8809525Abstract: According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1-A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, whicType: GrantFiled: February 7, 2011Date of Patent: August 19, 2014Assignee: Heptares Therapeutics LimitedInventors: Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
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Publication number: 20140220144Abstract: The compositions of the present invention composition comprise a therapeutically effective amount of particles comprising lamotrigine, in combination with granules comprising a disintegrant, and a sugar alcohol and/or a saccharide. These compositions are useful in treating epilepsy and bipolar disorder, particularly for patients with dysphagia, and to improve compliance with bipolar patients.Type: ApplicationFiled: February 5, 2014Publication date: August 7, 2014Applicant: Aptalis Pharmatech, Inc.Inventors: Gopi M. Venkatesh, Nehal H. Vyas, Michael Gosselin, Jin-Wang Lai
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Publication number: 20140221298Abstract: The present invention provides an agricultural and horticultural fungicidal composition including a compound A which is at least one selected from a nitrogen-containing heterocyclic compound having a specific structure including a compound represented by the formula (1), and a salt thereof, and a compound B which is at least one selected from the group of specific pesticidally active compounds: in the formula (1), X each independently represents a halogeno group or a C1 to 6 alkyl group; n represents the number of X(s) and is an integer of 0 to 6; and X? represents a halogeno group; and R1, R2 and R3 each independently represent a C1 to 6 alkyl group or a hydroxyl group.Type: ApplicationFiled: September 24, 2012Publication date: August 7, 2014Inventor: Raito Kuwahara
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Publication number: 20140221362Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: ApplicationFiled: February 4, 2014Publication date: August 7, 2014Applicant: Bayer CropScience AGInventors: Thomas BRETSCHNEIDER, Martin Füßlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria FRANKEN, Arnd VOERSTE
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Publication number: 20140213590Abstract: Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.Type: ApplicationFiled: January 3, 2014Publication date: July 31, 2014Applicant: FOCHON PHARMA, INC.Inventors: WEIBO WANG, TONGSHUANG LI
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Patent number: 8778837Abstract: The invention relates to the novel use of known active substance combinations which consist firstly of 3,4-dichloro-2?-cyano-1,2-thiazole-5-carboxanilide, of the formula which is known, and secondly further known insecticidal active substances, for controlling animal pests, especially arthropods, in particular insects.Type: GrantFiled: November 27, 2008Date of Patent: July 15, 2014Assignee: Bayer CropScience AGInventors: Lutz Assmann, Ulrike Wachendorff-Neumann, Heike Hungenberg, Wolfgang Thielert
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Patent number: 8778835Abstract: A composition comprising at least a pyridylethylbenzamide derivative of general formula (I) (a) and an insecticide compound (b) in a (a)/(b) weight ratio of from 1/1000 to 1000/1. A composition further comprising an additional fungicidal compound. A method for preventively or curatively combating the pests and diseases of crops by using this composition.Type: GrantFiled: July 5, 2007Date of Patent: July 15, 2014Assignee: Bayer Cropscience AGInventors: Heike Hungenberg, Gilbert Labourdette, Albert Schirring, Burkhard Schuetz, Anne Suty-Heinze, Wolfgang Thielert, Martin Vaupel
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Patent number: 8779129Abstract: The present invention provides novel compounds of formula I wherein W1, W2, W3, W4, W5, B, X1, X2, X3, X4, X5, E and L are as defined herein; invention compounds are gamma amino butyrique acid receptor-subtype B (“GABAB”) positive allosteric modulators (enhancers), which are useful to provide methods of treating or preventing diseases or disorders, including treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, panic disorder, posttraumatic stress disorders, urge urinary incontinence, gastroesophageal reflux disease, transient lower oesophageal sphincter relaxations, functional gastrointestinal disorders and irritable bowel syndrome.Type: GrantFiled: December 14, 2012Date of Patent: July 15, 2014Assignee: Addex Pharma S.A.Inventors: Eric Riguet, Brice Campo, Antoine Gibelin, Karim Mhalla
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Publication number: 20140194408Abstract: Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X1, X2, and X3 are N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: March 13, 2014Publication date: July 10, 2014Applicant: Genentech, Inc.Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
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Publication number: 20140194428Abstract: The invention relates generally to novel compositions and methods comprising a scyllo-inositol compound and one or both of valproic acid compound and lamotrigine. The compositions and methods provide beneficial effects in the treatment of bipolar disorders.Type: ApplicationFiled: September 28, 2012Publication date: July 10, 2014Applicant: Elan Pharmaceuticals. Inc.Inventor: Elan Pharmaceuticals. Inc.
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Patent number: 8772479Abstract: The invention relates to (among other things) oligomer-containing substituted aromatic triazine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.Type: GrantFiled: May 13, 2010Date of Patent: July 8, 2014Assignee: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
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Patent number: 8772291Abstract: This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders.Type: GrantFiled: December 8, 2009Date of Patent: July 8, 2014Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Joseph Barbosa, Li Dong, Cynthia Anne Fink, Jiancheng Wang, G. Gregory Zipp
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Publication number: 20140179701Abstract: Disclosed is a composition effective in reducing skin wrinkles. The composition comprises or uses a phosphodiesterase 5 (PDE5) inhibitor as an active ingredient. Further disclosed is a method for reducing skin wrinkles using the composition.Type: ApplicationFiled: March 3, 2014Publication date: June 26, 2014Applicant: SK CHEMICALS CO., LTD.Inventors: Soo-Min LEE, Sooheun LEE, Keun-Ho RYU, Bong-Yong LEE, Jae-Sun KIM, Jung-Hoon OH, Ye-Ji JEON
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Publication number: 20140179641Abstract: Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ cosmetic composition comprising novel active agents that enhance collagen production in the skin.Type: ApplicationFiled: December 20, 2012Publication date: June 26, 2014Applicant: AVON PRODUCTS, INC.Inventors: Uma Santhanam, Permanan Raaj Khusial
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Publication number: 20140178503Abstract: The present invention relates to new cyclohexyl urea modulators of D2 receptors and/or modulators of D3 receptors, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: February 26, 2014Publication date: June 26, 2014Applicant: Auspex Pharmaceuticals, Inc.Inventors: Ronald C. Newbold, Chengzhi Zhang
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Publication number: 20140179691Abstract: Disclosed is a novel oxazolidinone derivative represented by Formula 1 above, in particular, a novel oxazolidinone compound having a cyclic amidoxime or cyclic amidrazone group. In Formula 1, R and Q are the same as defined in the detailed description. In addition, disclosed is a pharmaceutical composition for an antibiotic which includes the novel oxazolidinone derivative of Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient. The novel oxazolidinone derivative, the prodrug thereof, the hydrate thereof, the solvate thereof, the isomer thereof, and the pharmaceutically acceptable salt thereof have broad antibacterial spectrum against resistant bacteria, low toxicity and strong antibacterial effects against Gram-positive and Gram-negative bacteria and thus may be effectively used as antibiotics.Type: ApplicationFiled: March 29, 2012Publication date: June 26, 2014Applicant: LEGOCHEM BIOSCIENCES, INC.Inventors: Young Lag Cho, Sung Yoon Baek, Sang Eun Chae, Sun Young Kim, Hong Bum Lee, Hyang Sook Lee, Kyuman Oh, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim, Hye Jin Heo
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Publication number: 20140179688Abstract: Methods for preventing, ameliorating, or reducing dermatological signs of aging are provided which employ active agents that modulate the PLOD-2 enzyme in the skin. Also provided are methods for screening for substances which modulate PLOD-2 enzyme levels and the methods of using active agents identified by the screening protocol in the treatment of skin.Type: ApplicationFiled: December 20, 2012Publication date: June 26, 2014Applicant: AVON PRODUCTS, INC.Inventors: Uma Santhanam, Permanan Raaj Khusial
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Publication number: 20140171383Abstract: The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS.Type: ApplicationFiled: June 28, 2013Publication date: June 19, 2014Inventors: Daniel J. ABRAMS, Raymond Bunch, Tom Anchordoquy
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Patent number: 8754082Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and 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 the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.Type: GrantFiled: May 9, 2013Date of Patent: June 17, 2014Assignee: Siga Technologies, Inc.Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Ryan A. Larson
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Patent number: 8748599Abstract: The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The compounds are of formula (I): in which z is a single bond or an optionally substituted linking group, R1 is a halo-alkyl group; and A is an optionally substituted aromatic heterocyclic or carbocyclic ring system; or a salt thereof.Type: GrantFiled: July 8, 2010Date of Patent: June 10, 2014Assignee: University Of GreenwichInventors: Michael Leach, Karl Franzmann, Dieter Riddall, Laurence Harbige
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Patent number: 8748600Abstract: The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The triazine compounds are of formula (I) wherein: R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when R1 is hydrogen or ?NH when R1 is a substituent group; R3 and R4 are both carbocyclic, heterocyclic or alkyl groups and may be same or different; and R5 is hydrogen, alkyl or a cyclic aryl group, with the proviso that: when R3 and R4 are both alkyl they are linked to form a cycloalkyl group, and R5 is a cyclic aromatic group; and when R3 and R4 are both carbocyclic or heterocyclic groups, R5 is hydrogen or an alkyl group; or a salt thereof.Type: GrantFiled: July 8, 2010Date of Patent: June 10, 2014Assignee: University of GreenwichInventors: Michael Leach, Karl Franzmann, Dieter Riddall, Laurence Harbige
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Publication number: 20140155403Abstract: A method of treating a disorder. The method includes administering to a subject in need thereof a compound of formula (I): Each of A, N*, X, Y, Z, R1, and R2 is defined herein. Also disclosed are compounds of the formula and a pharmaceutical composition containing such a compound.Type: ApplicationFiled: February 6, 2014Publication date: June 5, 2014Applicant: University of GreenwichInventors: Michael Leach, Laurence Harbige, Dieter Riddall, Karl Franzmann
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Publication number: 20140120185Abstract: The present invention provides a medicament having a wider treatment spectrum, causing a fewer side effects and superior in tolerability and safety, as compared to known typical antipsychotic agents and atypical antipsychotic agents. The present invention related to a medicament containing (I) a compound which is 7-[4-(4-benzo[b]thiophen-4-yl-piperazin-1-yl)butoxy]-1H-quinolin-2-one or a salt thereof, and (II) at least one drug selected from the group consisting of a mood stabilizer, a serotonin reuptake inhibitor, a norepinephrine reuptake inhibitor, a serotonin and norepinephrine reuptake inhibitor, a noradrenergic and specific serotonergic antidepressant, an antianxiety drug, a tricyclic antidepressant, a tetracyclic antidepressant, an antipsychotic drug and an anti-ADHD drug, in combination.Type: ApplicationFiled: April 4, 2012Publication date: May 1, 2014Inventors: Tsuyoshi Hirose, Kenji Maeda, Tetsuro Kikuchi, Masafumi Toda
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Patent number: 8703803Abstract: Provided are tris-quaternary ammonium compounds which are modulators of nicotinic acetylocholine receptors. Also provided are methods of using the compounds for modulating the function of a nicotinic acetylcholine receptor, and for the prevention and/or treatment of central nervous system disorders, substance use and/or abuse and or gastrointestinal tract disorders.Type: GrantFiled: September 21, 2012Date of Patent: April 22, 2014Inventors: Peter A. Crooks, Linda P. Dwoskin, Roger Papke, Guangrong Zheng, Sangeetha Sumithran
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Publication number: 20140107125Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.Type: ApplicationFiled: April 29, 2013Publication date: April 17, 2014Applicant: Dermira (Canada), Inc.Inventor: Dermira (Canada), Inc.
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Patent number: 8697698Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2?are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: September 28, 2012Date of Patent: April 15, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
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Publication number: 20140100183Abstract: The present invention concerns compositions, methods and/or apparatus of central administration of various CNS-active agents. In particular embodiments, intrathecal administration is advantageous for decreasing the systemic concentrations of CNS agent, thereby decreasing side effect toxicity, while allowing more effective delivery of the agent to the site of action, simultaneously decreasing the dosage delivered to the subject. In particular embodiments, ICV delivery may be of use for patients who have previously proven to be refractory to systemic administration of CNS agents, in some cases due to systemic side effects, or for those patients whose symptoms are of sufficient severity to warrant more aggressive therapeutic intervention. ICV administration allows not only lower systemic concentration but also higher therapeutically effective concentration within the CNS.Type: ApplicationFiled: April 12, 2013Publication date: April 10, 2014Applicant: The Regents of the University of Colorado, a body corporateInventors: Daniel J. ABRAMS, Raymond BUNCH, Tom ANCHORDOQUY, Karen E. STEVENS
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Patent number: 8691818Abstract: Compounds of general structure in which X and Y are each N or C with at least one of X and Y being N; Z is a single bond or an optionally substituted linking group R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when RI is hydrogen or ?NH when R1 is a substituent group; or N* is a group NRaRb where Ra and Rb are independently H or an alkyl group; or N* is an optionally substituted piperazinyl ring; and A is an optionally substituted heterocyclic or carbocyclic ring system which may be linked to the triazo/diazo ring through R2 to form a fused multicyclic ring; are indicated as suitable for treatment of disorders in mammals that are susceptible to sodium channel blockers and antifolates, and particularly disorders such epilepsy, multiple sclerosis, glaucoma and uevitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motorneurone disease, Alzheimer's disease, Parkinson's disease, chronic inflType: GrantFiled: January 16, 2009Date of Patent: April 8, 2014Assignee: University Of GreenwichInventors: Michael Leach, Laurence Harbige, Dieter Riddall, Karl Franzmann