Chalcogen Attached Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 549/58)
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Patent number: 10703747Abstract: This invention is benzothiophene-based selective mixed estrogen receptor downregulators and their compositions and uses to treat estrogen-related disorders.Type: GrantFiled: April 24, 2019Date of Patent: July 7, 2020Assignee: The Board of Directors of the University of IllinoisInventors: Gregory R. Thatcher, Rui Xiong, Yunlong Lu, Jiong Zhao, Debra A. Tonetti
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Patent number: 10062922Abstract: A rechargeable lithium battery includes a lithium anode, a cathode, and a separator interposed between the lithium anode and the cathode. The separator includes a porous polymer soaked with a liquid electrolyte. The lithium battery further includes an artificial solid electrolyte interphase membrane interposed between the lithium anode and the separator. The artificial solid electrolyte interphase membrane may be a composite of a carbonaceous material, a high shear modulus conducting polymer, and a conductive additive.Type: GrantFiled: January 26, 2016Date of Patent: August 28, 2018Inventors: Jitendra Kumar, Guru Subramanyam, Fahima Ouchen, James G. Grote
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Patent number: 9670176Abstract: The invention discloses a process for the preparation of Zileuton of formula I by employing acetic acid-1-benzo[b]thiophen-2-yl-ethyl-ester of formula-III as an intermediate.Type: GrantFiled: June 27, 2016Date of Patent: June 6, 2017Assignee: Strides Shasun LimitedInventors: Sankar Arjunan, Ramu Dhanapal, Santha Kumar, Aramanai Lakshmanan Srinivasan, Krishnan Devendra Prasad
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Publication number: 20150126593Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of asthma and allergy may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of respiratory diseases, respiratory disorders, COPD, bronchitis, brain injury, inflammation, inflammatory skin diseases, asthma, allergic reactions, infections due to acute allergy, bronchospasm, respiratory distress, acute asthma, leukotrienes over activity, 5-LO enzyme activity and cancer.Type: ApplicationFiled: February 27, 2013Publication date: May 7, 2015Inventor: Mahesh Kandula
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Patent number: 9023874Abstract: The invention relates to alkylsulfide derivatives compounds of formula I as hereunder depicted or the enantiomers or veterinarily acceptable salts thereof which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to methods for controlling invertebrate pests by using these compounds and to plant propagation material and to agricultural and veterinary compositions comprising said compounds. wherein U, R1, R2, R3U, X, n and p are defined as in the description.Type: GrantFiled: November 11, 2010Date of Patent: May 5, 2015Assignee: Merial, Inc.Inventors: Sebastian Soergel, Ralph Paulini, Steffen Gross, Carsten Beyer, Matthias Pohlman, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Douglas D. Anspaugh, Sarah Thompson, Vincent Salgado
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Publication number: 20150072961Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) for treatment of pulmonary conditions (e.g. asthma). The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.Type: ApplicationFiled: November 14, 2014Publication date: March 12, 2015Inventors: Chongxi YU, Lina XU
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Publication number: 20150018399Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.Type: ApplicationFiled: August 5, 2014Publication date: January 15, 2015Inventors: SONGNIAN LIN, Fengqi Zhang, Emma R. Parmee, Sunita V. Dewnani
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Patent number: 8933250Abstract: A method of preparation of N-(1-benzo[b]thien-2-ylethyl)-N-hydroxyurea of formula (I) with the use of a reaction of 1-(benzo[b]thien-2-yl)-ethanol of formula (II) with hydroxyurea of formula (III) in organic solvents, organic acids, their mixtures or in mixtures thereof with water, being catalyzed by strongly acidic cation exchangers or various hydrogen sulphates.Type: GrantFiled: April 6, 2009Date of Patent: January 13, 2015Assignee: Farmak, A.S.Inventors: Kamil Koristek, Pavel Hradil, Martin Grepl, Petr Slezar
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Publication number: 20140371454Abstract: The present application provides, among other things, compounds and methods for metathesis reactions. In some embodiments, provided compounds promote highly efficient and highly Z-selective metathesis. In some embodiments, provided compounds and methods are particularly useful for producing allyl alcohols. In some embodiments, provided compounds have the structure of formula I. In some embodiments, provided compounds comprise ruthenium, and a ligand bonded to ruthenium through a sulfur atom.Type: ApplicationFiled: June 12, 2014Publication date: December 18, 2014Inventors: Amir H. Hoveyda, R. Kashif M. Khan, Sebastian Torker, Ming Joo Koh
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Publication number: 20140371274Abstract: The present invention relates to novel compounds, their use in the prevention or treatment of symptoms and disorders associated with the bradykinin B1 pathway and pharmaceutical compositions containing them.Type: ApplicationFiled: June 13, 2014Publication date: December 18, 2014Inventors: Andrea Rosario BECCARI, Gianluca BIANCHINI, Chiara LIBERATI, Michela FANI', Mara ZIPPOLI
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Publication number: 20140275552Abstract: Photoactive compositions of matter, methods for their design and synthesis, and various applications of such compositions of matter are disclosed. Such photoactive compositions may, for example, include any one or more of the following: a core moiety; a primary electron donor moiety; an electron-withdrawing moiety; and an alkyl tail. Some photoactive compositions may further include multiple additional electron donor moieties, electron-withdrawing moieties, and alkyl tails. Applications of such photoactive compositions of matter may include use in photovoltaic cells (e.g., as a p- or n-type material of the active layer of some photovoltaic cells, or as a dye to be employed in other photovoltaic cells); batteries, field-effect transistors; and light-emitting diodes.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventors: Michael D. Irwin, Jerred A. Chute, Robert D. Maher, III
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Publication number: 20140275172Abstract: The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.Type: ApplicationFiled: March 7, 2014Publication date: September 18, 2014Applicant: Janssen Pharmaceutica NVInventors: Zhihua Sui, Nalin Subasinghe
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Patent number: 8835654Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.Type: GrantFiled: September 20, 2011Date of Patent: September 16, 2014Assignee: BHI Limited PartnershipInventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
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Publication number: 20140243334Abstract: This invention provides compounds of formula (I): wherein R1a, R1b, R1c, R2a, R2b, R2c, and R2d have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: May 5, 2014Publication date: August 28, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
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Publication number: 20140221657Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.Type: ApplicationFiled: April 7, 2014Publication date: August 7, 2014Applicant: PRISM BioLab CorporationInventors: Hiroyuki Kouji, Yuji Kogami, Takenao Odagami
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Publication number: 20140200354Abstract: The current invention describes novel chiral synthetic routes and intermediates for the manufacture of chiral anti-inflammatory agents of general formula VIII in which at least one of the groups X1, X2, X3 is selected from fluoro, chloro, bromo, hydroxy, methoxy, ethoxy, trifluoromethyl, amino whereas the other groups X1, X2, X3 have the meaning of a hydrogen atom, in which at least one of the groups Z1, Z2, Z3 is selected from —O—, —S—, —N(—CH3)—, whereas the other groups Z1, Z2, Z3 have the meaning of a —CH2— group, and in which Ar is an aromatic group.Type: ApplicationFiled: March 14, 2014Publication date: July 17, 2014Applicant: Intendis GmbHInventor: Steffen SCHWEIZER
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Patent number: 8766242Abstract: This invention relates to dibenzothiopyran compounds. This invention also relates to layers and devices including at least one of these compounds.Type: GrantFiled: November 29, 2011Date of Patent: July 1, 2014Assignee: E I du Pont de Nemours and CompanyInventors: Nora Sabina Radu, Steven W. Shuey, Ying Wang
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Patent number: 8758960Abstract: A novel polymerizable high-refractive index compound which is useful as an optical material, and a holographic recording medium using the same, which has high diffraction efficiency, high light transmittance and small rate of shrinkage, are provided. A composition for forming a holographic recording layer containing a reactive compound represented by the following formula 1, a holograph recording material, and a holographic recording medium provided with a recording layer containing the same, are disclosed.Type: GrantFiled: June 9, 2009Date of Patent: June 24, 2014Assignee: Mitsubishi Chemical CorporationInventors: Yasuaki Miki, Akiko Yabe, Jun Enda
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Publication number: 20140155415Abstract: The present invention relates to compounds of formula I or II, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.Type: ApplicationFiled: April 4, 2012Publication date: June 5, 2014Inventors: Michael David Bartberger, Michael D. Croghan, Christopher H. Fotsch, Mark H. Norman, Lewis Dale Pennington, Andreas Reichelt, David J. St. Jean, JR., Christopher M. Tegley
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Publication number: 20140135322Abstract: The present invention relates to novel chemical compounds formula (I) (C)n—B-(A)m-B—(C)n (I) wherein m is 0 or 1, and n is independently 0, 1, 2 or 3, A, each B and each C are independently selected from phenylene and five- and six-membered heteroaromatic rings, and for a terminal ring B or C also from bicyclic heteroaromatic fused rings having seven to ten ring members, wherein the bond between at least two of the rings A to C may be replaced by a carbonyl group (—CO—), wherein at least two of the rings A to C are substituted with one or two groups R, and wherein each ring A to C further optionally is substituted with one or two groups R1. The compounds are useful in therapy, especially therapy of a mammal suffering from a disease involving misfolded or aggregated forms of proteins.Type: ApplicationFiled: July 13, 2012Publication date: May 15, 2014Inventors: Peter Asberg, Kristin Hammer, Johan Olsson, Martin Henriksson
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Publication number: 20140121246Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.Type: ApplicationFiled: October 15, 2013Publication date: May 1, 2014Applicant: Metabolex, Inc.Inventors: Dong Fang Shi, Jiangao Song, Christopher J. Rabbat, Jingyuan Ma, Aaron Novack, Imad Nashashibi, Xin Chen
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Publication number: 20140107247Abstract: The invention provides a polymerizable compound represented by formula (I), a polymerizable composition, and a polymer that have a practical low melting point, can be produced at low cost, and can produce an optical film that achieves uniform conversion of polarized light over a wide wavelength band, and an optically anisotropic article.Type: ApplicationFiled: April 12, 2012Publication date: April 17, 2014Applicant: ZEON CORPORATIONInventors: Kei Sakamoto, Kumi Okuyama
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Publication number: 20140088079Abstract: The present invention relates to a compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes. The present invention also provides a method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound.Type: ApplicationFiled: June 1, 2012Publication date: March 27, 2014Applicant: GREEN CROSS CORPORATIONInventors: Soongyu Choi, Kwang Seop Song, Suk Ho Lee, Min Ju Kim, Hee Jeong Seo, Eun-Jung Park, Younggyu Kong, So Ok Park, Hyunku Kang, Myung Eun Jung, Kinam Lee, Hyun Jung Kim, Jun Sung Lee, Min Woo Lee, Mi-Soon KIM, Dong Ho Hong, Misuk Kang
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Patent number: 8673178Abstract: The invention relates to compounds of the formula I in which R0, A0, A1, A2, Z0, Z1, Z2, L1, L2, X, l, m and n have the meanings indicated in claim 1, and to the use thereof in liquid-crystalline media, and to liquid-crystalline media comprising one or more compounds of the formula I in electro-optical liquid-crystal displays.Type: GrantFiled: November 29, 2010Date of Patent: March 18, 2014Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Michael Wittek, Brigette Schuler, Volker Reiffenrath, Axel Jansen, Christian Hock, Harald Hirschmann
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Publication number: 20140034915Abstract: A heterocyclic compound is represented by Formula 1. An organic light emitting device includes a first electrode, a second electrode and an organic layer between the first and second electrodes. The organic layer includes the heterocyclic compound. An organic light-emitting display apparatus includes the organic light-emitting device and a transistor including a source, a drain, a gate and an active layer. The source or the drain is electrically connected to the first electrode of the organic light-emitting device.Type: ApplicationFiled: January 25, 2013Publication date: February 6, 2014Applicant: SAMSUNG DISPLAY CO. LTD.Inventors: Sun-Young Lee, Yoon-Hyun Kwak, Bum-Woo Park, Jong-Won Choi, Wha-Il Choi, So-Yeon Kim, Ji-Youn Lee
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Publication number: 20140031405Abstract: Compounds of formula (I) wherein R1 is C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy; R2 is C1-C4alkyl; R3 is hydrogen or halogen; R4 is hydrogen, C1-C4alkyl or C1-C4halogenalkyl; X is methine or nitrogen; A is R5 is hydrogen, halogen, —?—C1-C6alkyl, —?—C3-C7cycloalkyl or -?-aryl; R6 is hydrogen, halogen, —?—C1-C6alkyl, —?—C3-C7cycloalkyl or -?-aryl; and agrochemically acceptable salts/isomers/structural isomers/stereoisomers/diastereoisomers/enantiorners/tautorriers and N-oxides of those compounds are suitable for use as microbiocides.Type: ApplicationFiled: February 16, 2012Publication date: January 30, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Harald Walter, Daniel Stierli
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Publication number: 20140012005Abstract: The present invention relates to a process for preparing chiral amino acids with excellent enantiomeric excesses.Type: ApplicationFiled: December 22, 2011Publication date: January 9, 2014Applicant: DiverchimInventors: Sylvain Darses, Nicolas Lefevre, Benoit Folleas, Jean-Louis Brayer
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Publication number: 20140005301Abstract: The present invention relates to a heat-curable composition comprising (a) at least one compound which is capable of undergoing cationic polymerization; and (b) at least one sulfonium sulfate selected from compounds of the formulae Ia and Ib where Yn? is a monovalent or divalent anion selected from (1) where n, M, R1 to R10 are as defined in claim 1 and in the description. The present invention also relates to novel sulfonium sulfates of the formulae Ia and Ib, to a process for curing cationically polymerizable material and to the cured material obtained by said process.Type: ApplicationFiled: February 22, 2012Publication date: January 2, 2014Applicant: BASF SEInventors: Kazuhiko Kunimoto, Hisatoshi Kura
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Publication number: 20130324684Abstract: The present invention provides a diacetylene derivative represented by the following formula (A) which exhibits liquid crystallinity by itself and has a large refractive index anisotropy or does not exhibit liquid crystallinity by itself but exhibits a large refractive index anisotropy when added to a liquid crystalline compound: R1-Sp1-(Ar1)p-(Ar3)q-(Phe)r-C?C—C?C-(Phe)r-(Ar4)q-(Ar2)p-Sp2-R2??(A) (wherein R1 and R2 are a hydrogen, halogen, cyano, isothiocyanate, alkyl, alkenyl, alkynyl or reactive group, SP1 and SP2 are each a spacer group, Ar1 and Ar2 are each a non-substituted or substituted aromatic carbocyclic or heterocyclic group, Ar3 and Ar4 are each a non-substituted or substituted heterocyclic group, Phe is a non-substituted or substituted 1,4-phenylene group, and p, q and r are each 0 or 1.Type: ApplicationFiled: January 31, 2012Publication date: December 5, 2013Applicants: JX NIPPON OIL & ENERGY CORPORATION, TOKYO INSTITUTE OF TECHNOLOGYInventors: Yuki Arajawa, Gen-Ichi Konishi, Shunpei Nakajima, Sungmin Kang, Junji Watanabe, Takuya Matsumoto, Suzushi Nishimura, Takehiro Toyooka
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Patent number: 8586603Abstract: The present application relates to compounds of formula (I): and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds in producing medicaments for the treatment of various diseases and conditions, such as of the central nervous system.Type: GrantFiled: December 20, 2010Date of Patent: November 19, 2013Inventors: Peter Gmeiner, Miriam Ruberg, Harald Hüebner
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Patent number: 8552032Abstract: The present invention is directed to novel bicyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.Type: GrantFiled: December 16, 2010Date of Patent: October 8, 2013Assignee: Janssen Pharmaceutica NVInventors: Edward C. Lawson, Dennis J. Hlasta, Shyamali Ghosh, Renee L. DesJarlais, Carsten Schubert
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Publication number: 20130253022Abstract: Pharmaceutical compositions of the invention include fluorinated sulfamide derivatives having a disease-modifying action in the treatment of diseases associated with excitotoxicity and accompanying oxidative stress that include epilepsy, Alzheimer's disease, Parkinson's disease, Huntington's disease, heavy metal toxicity and any neurodegenerative disease involving glutamate toxicity.Type: ApplicationFiled: November 18, 2011Publication date: September 26, 2013Applicants: FOX CHASE CHEMICAL DIVERSITY CENTER, INC., ADVANCED NEURAL DYNAMICS, INC.Inventors: Garry Robert Smith, Douglas E. Brenneman, Allen B. Reitz, Yan Zhang, Yanming Du
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Publication number: 20130253183Abstract: Provided are: an aromatic amine derivative in which a terminal substituent such as a dibenzofuran ring or a dibenzothiophene ring is bonded to a nitrogen atom directly or through an arylene group or the like; an organic electroluminescence device including an organic thin film layer formed of one or more layers including a light emitting layer and interposed between a cathode and an anode in which a layer of the organic thin film layer contains the aromatic amine derivative by itself or as a component of a mixture, and the device has a long lifetime and high luminous efficiency; and an aromatic amine derivative for realizing the device.Type: ApplicationFiled: May 24, 2013Publication date: September 26, 2013Applicant: IDEMITSU KOSAN CO., LTD.Inventors: Yumiko MIZUKI, Masakazu Funahashi, Mitsunori Ito, Masahiro Kawamura
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Publication number: 20130245283Abstract: A compound comprising a prodrug of a prostaglandin EP4 agonist, wherein said prodrug is an ester, ether, or amide of an amino acid is disclosed herein. Maintenance of the colonic mucosal barrier by method comprising administering a therapeutically effective amount of a prostaglandin EP4 agonist to a colon of a mammal is also disclosed herein. Dosage forms, medicaments, and compositions, related thereto are also disclosed.Type: ApplicationFiled: April 23, 2013Publication date: September 19, 2013Applicant: Allergan, Inc.Inventors: Wha-Bin Im, Robert M. Burk, Mark Holoboski
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Patent number: 8530512Abstract: The present invention provides compounds and methods of using of the compounds as anti-infective and anthelminitc agents. In a preferred embodiment, the present invention provides the following compound of Formula III: wherein: R1 is not H when R2 is H and R2 is not H when R1 is H, further wherein R1 is OH or CH(2n+1)O, wherein n is 1-10; R2 is OH or CH(2n+1)O, where n is 1-10; W is alkyl, phenyl, halophenyl, pyridyl, piperidyl, or a substituted or unsubstituted aryl group, including unsubstituted and substituted aromatic heterocycles; and L is an optional linker or linking group selected from O, S, NH, CF2, or CH2, and x=0 or 1, i.e., if x=0, no linking group is present and when x=0, W is not phenyl.Type: GrantFiled: December 20, 2010Date of Patent: September 10, 2013Inventors: Aaron P. Monte, M. Shahjahan Kabir, Marc A. Rott, William R. Schwan, James M. Cook, III, Jennifer A. Miskowski, Ranjit Verma, Leah Defoe
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Patent number: 8518560Abstract: Provided are: an aromatic amine derivative in which a terminal substituent such as a dibenzofuran ring or a dibenzothiophene ring is bonded to a nitrogen atom directly or through an arylene group or the like; an organic electroluminescence device including an organic thin film layer formed of one or more layers including a light emitting layer and interposed between a cathode and an anode in which a layer of the organic thin film layer contains the aromatic amine derivative by itself or as a component of a mixture, and the device has a long lifetime and high luminous efficiency; and an aromatic amine derivative for realizing the device.Type: GrantFiled: December 22, 2008Date of Patent: August 27, 2013Assignee: Idemitsu Kosan Co., Ltd.Inventors: Yumiko Mizuki, Masakazu Funahashi, Mitsunori Ito, Masahiro Kawamura
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Publication number: 20130157195Abstract: A molecular glass compound includes (A) a tetrameric reaction product of a specific aromatic compound having at least one hydroxy group, and a specific polycyclic or fused polycyclic aromatic aldehyde; and (B) an acid-removable protecting group as an adduct with the hydroxy group of the aromatic compound and/or a hydroxy group of the polycyclic or fused polycyclic aromatic aldehyde. A photoresist composition including the molecular glass compound, and a coated substrate including a layer of the photoresist composition are also disclosed.Type: ApplicationFiled: September 21, 2012Publication date: June 20, 2013Applicant: ROHM AND HAAS ELECTRONIC MATERIALS LLCInventor: Rohm and Haas Electronic Materials LLC
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Patent number: 8455497Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: GrantFiled: February 12, 2009Date of Patent: June 4, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
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Acylamino-substituted fused cyclopentanecarboxylic acid derivatives and their use as pharmaceuticals
Patent number: 8445530Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: GrantFiled: October 1, 2012Date of Patent: May 21, 2013Assignee: SanofiInventors: Matthias Schaefer, Josef Pernerstorfer, Dieter Kadereit, Hartmut Strobel, Werngard Czechtizky, L. Charlie Chen, Alena Safarova, Aleksandra Weichsel, Marcel Patek -
Patent number: 8394971Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: January 20, 2010Date of Patent: March 12, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
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Publication number: 20130035377Abstract: Tranylcypromine derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of histone demethylases LSD1 and LSD2, such as the diseases characterized by deregulation of gene transcription, cell differentiation and proliferation, e.g. tumors, viral infections, are herein described. These compounds belong to the structural formula (I) wherein A and R3 are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to compositions containing them and to therapeutic use thereof.Type: ApplicationFiled: April 15, 2011Publication date: February 7, 2013Applicants: UNIVERSITÀ DEGLI STUDI DI ROMA "LA SAPIENZA", UNIVERSITÀ DEGLI STUDI DI MILANO, UNIVERSITÀ DEGLI STUDI DI PAVIA, FONDAZIONE IEOInventors: Saverio Minucci, Antonello Mai, Andrea Mattevi
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Publication number: 20120302546Abstract: Pharmaceutical compositions of the invention include sulfamide derivatives having a disease-modifying action in the treatment of diseases associated with excitotoxicity and accompanying oxidative stress that include epilepsy, Alzheimer's disease, and any neurodegenerative disease involving glutamate toxicity.Type: ApplicationFiled: February 3, 2011Publication date: November 29, 2012Applicants: FOX CHASE CHEMICAL DIVERSITY CENTER, INC., ADVANCED NEURAL DYNAMICS, INC.Inventors: Garry Robert Smith, Douglas Eric Brenneman, Allen B. Reitz, Yanming Du
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Publication number: 20120277262Abstract: The present application relates to compounds of formula (I): and pharmaceutically acceptable salts and solvates thereof, wherein the substituents are as defined herein, compositions containing such compounds and the uses of such compounds in producing medicaments for the treatment of various diseases and conditions, such as of the central nervous system.Type: ApplicationFiled: December 20, 2010Publication date: November 1, 2012Inventors: Peter Gmeiner, Miriam Ruberg, Harald Huebner
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Publication number: 20120273723Abstract: The invention relates to compounds of the formula I in which R0, A0, A1, A2, Z0, Z1, Z2, L1, L2, X, l, m and n have the meanings indicated in claim 1, and to the use thereof in liquid-crystalline media, and to liquid-crystalline media comprising one or more compounds of the formula I in electro-optical liquid-crystal displays.Type: ApplicationFiled: November 29, 2010Publication date: November 1, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Michael Wittek, Brigitte Schuler, Volker Reiffenrath, Axel Jansen, Christian Hock, Harald Hirschmann
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Patent number: 8283478Abstract: The present invention is directed to novel process for the preparation of sulfonylimine and sulfamide derivatives.Type: GrantFiled: April 19, 2006Date of Patent: October 9, 2012Assignee: Janssen Pharmaceutica NVInventors: Ahmed F. Abdel-Magid, Steven J. Mehrman
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Publication number: 20120252836Abstract: The present invention relates to compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.Type: ApplicationFiled: June 18, 2012Publication date: October 4, 2012Applicant: EVOLVA SAInventors: Alexandra Santana Sorensen, Jean-Phillippe Meyer, Peteris Alberts, Mainkar Prathama
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Patent number: 8273902Abstract: A Process for production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which comprises using as a starting compound as a (phenylthio)acetic acid derivative or salts thereof represented by the general formula: wherein X1 represents a halogen atom, is useful as a safe process for mass production of 1-(3-(2-(1-benzothiophen-5-yl)ethoxy)propyl)azetidin-3-ol or salts thereof which is useful as a remedy for disease of central and peripheral nerve.Type: GrantFiled: January 6, 2011Date of Patent: September 25, 2012Assignee: Toyama Chemical Co., Ltd.Inventors: Akihito Saitoh, Yoshiaki Suzuki, Kenji Yonezawa, Mitsuhide Kawamura, Takahiko Kusanagi, Takashi Nakai
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Publication number: 20120165293Abstract: The presently disclosed subject matter provides a method of synthesizing prostaglandins and prostaglandin analogs comprising the ring closing metathesis of compounds of Formula (I). Also provided are novel compounds of Formula (I) and Formula (II). In addition to their use as synthetic intermediates in the presently disclosed methods, compounds of Formula (II) can be used as prostaglandin and/or prostaglandin analog prodrugs.Type: ApplicationFiled: July 13, 2010Publication date: June 28, 2012Inventors: George Petros Yiannikouros, Panos Kalaritis, Chaminda Priyapushpa Gamage, Stephenie Bosse Abernathy
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Publication number: 20120157462Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of aniline and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.Type: ApplicationFiled: January 30, 2008Publication date: June 21, 2012Inventors: Alan T. Johnson, Guan-Sheng Jiao
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Patent number: 8202894Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.Type: GrantFiled: June 30, 2008Date of Patent: June 19, 2012Assignee: Syngenta Crop Protection LLCInventors: Harald Walter, Daniel Stierli, Hans Tobler