Chalcogen Attached Indirectly To The Bicyclo Ring System By Nonionic Bonding Patents (Class 549/58)
  • Patent number: 10703747
    Abstract: This invention is benzothiophene-based selective mixed estrogen receptor downregulators and their compositions and uses to treat estrogen-related disorders.
    Type: Grant
    Filed: April 24, 2019
    Date of Patent: July 7, 2020
    Assignee: The Board of Directors of the University of Illinois
    Inventors: Gregory R. Thatcher, Rui Xiong, Yunlong Lu, Jiong Zhao, Debra A. Tonetti
  • Patent number: 10062922
    Abstract: 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: Grant
    Filed: January 26, 2016
    Date of Patent: August 28, 2018
    Inventors: Jitendra Kumar, Guru Subramanyam, Fahima Ouchen, James G. Grote
  • Patent number: 9670176
    Abstract: 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: Grant
    Filed: June 27, 2016
    Date of Patent: June 6, 2017
    Assignee: Strides Shasun Limited
    Inventors: Sankar Arjunan, Ramu Dhanapal, Santha Kumar, Aramanai Lakshmanan Srinivasan, Krishnan Devendra Prasad
  • Publication number: 20150126593
    Abstract: 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: Application
    Filed: February 27, 2013
    Publication date: May 7, 2015
    Inventor: Mahesh Kandula
  • Patent number: 9023874
    Abstract: 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: Grant
    Filed: November 11, 2010
    Date of Patent: May 5, 2015
    Assignee: 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
  • Publication number: 20150072961
    Abstract: 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: Application
    Filed: November 14, 2014
    Publication date: March 12, 2015
    Inventors: Chongxi YU, Lina XU
  • Publication number: 20150018399
    Abstract: 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: Application
    Filed: August 5, 2014
    Publication date: January 15, 2015
    Inventors: SONGNIAN LIN, Fengqi Zhang, Emma R. Parmee, Sunita V. Dewnani
  • Patent number: 8933250
    Abstract: 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: Grant
    Filed: April 6, 2009
    Date of Patent: January 13, 2015
    Assignee: Farmak, A.S.
    Inventors: Kamil Koristek, Pavel Hradil, Martin Grepl, Petr Slezar
  • Publication number: 20140371454
    Abstract: 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: Application
    Filed: June 12, 2014
    Publication date: December 18, 2014
    Inventors: Amir H. Hoveyda, R. Kashif M. Khan, Sebastian Torker, Ming Joo Koh
  • Publication number: 20140371274
    Abstract: 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: Application
    Filed: June 13, 2014
    Publication date: December 18, 2014
    Inventors: Andrea Rosario BECCARI, Gianluca BIANCHINI, Chiara LIBERATI, Michela FANI', Mara ZIPPOLI
  • Publication number: 20140275552
    Abstract: 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: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Inventors: Michael D. Irwin, Jerred A. Chute, Robert D. Maher, III
  • Publication number: 20140275172
    Abstract: 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: Application
    Filed: March 7, 2014
    Publication date: September 18, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Nalin Subasinghe
  • Patent number: 8835654
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: September 16, 2014
    Assignee: BHI Limited Partnership
    Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
  • Publication number: 20140243334
    Abstract: 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: Application
    Filed: May 5, 2014
    Publication date: August 28, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Emily F. Calderwood, Dylan B. England, Alexandra E. Gould, Sean J. Harrison, Liting Ma
  • Publication number: 20140221657
    Abstract: 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: Application
    Filed: April 7, 2014
    Publication date: August 7, 2014
    Applicant: PRISM BioLab Corporation
    Inventors: Hiroyuki Kouji, Yuji Kogami, Takenao Odagami
  • Publication number: 20140200354
    Abstract: 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: Application
    Filed: March 14, 2014
    Publication date: July 17, 2014
    Applicant: Intendis GmbH
    Inventor: Steffen SCHWEIZER
  • Patent number: 8766242
    Abstract: This invention relates to dibenzothiopyran compounds. This invention also relates to layers and devices including at least one of these compounds.
    Type: Grant
    Filed: November 29, 2011
    Date of Patent: July 1, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Nora Sabina Radu, Steven W. Shuey, Ying Wang
  • Patent number: 8758960
    Abstract: 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: Grant
    Filed: June 9, 2009
    Date of Patent: June 24, 2014
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Yasuaki Miki, Akiko Yabe, Jun Enda
  • Publication number: 20140155415
    Abstract: 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: Application
    Filed: April 4, 2012
    Publication date: June 5, 2014
    Inventors: 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
  • Publication number: 20140135322
    Abstract: 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: Application
    Filed: July 13, 2012
    Publication date: May 15, 2014
    Inventors: Peter Asberg, Kristin Hammer, Johan Olsson, Martin Henriksson
  • Publication number: 20140121246
    Abstract: 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: Application
    Filed: October 15, 2013
    Publication date: May 1, 2014
    Applicant: Metabolex, Inc.
    Inventors: Dong Fang Shi, Jiangao Song, Christopher J. Rabbat, Jingyuan Ma, Aaron Novack, Imad Nashashibi, Xin Chen
  • Publication number: 20140107247
    Abstract: 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: Application
    Filed: April 12, 2012
    Publication date: April 17, 2014
    Applicant: ZEON CORPORATION
    Inventors: Kei Sakamoto, Kumi Okuyama
  • Publication number: 20140088079
    Abstract: 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: Application
    Filed: June 1, 2012
    Publication date: March 27, 2014
    Applicant: GREEN CROSS CORPORATION
    Inventors: 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
  • Patent number: 8673178
    Abstract: 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: Grant
    Filed: November 29, 2010
    Date of Patent: March 18, 2014
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Michael Wittek, Brigette Schuler, Volker Reiffenrath, Axel Jansen, Christian Hock, Harald Hirschmann
  • Publication number: 20140034915
    Abstract: 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: Application
    Filed: January 25, 2013
    Publication date: February 6, 2014
    Applicant: 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
  • Publication number: 20140031405
    Abstract: 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: Application
    Filed: February 16, 2012
    Publication date: January 30, 2014
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Harald Walter, Daniel Stierli
  • Publication number: 20140012005
    Abstract: The present invention relates to a process for preparing chiral amino acids with excellent enantiomeric excesses.
    Type: Application
    Filed: December 22, 2011
    Publication date: January 9, 2014
    Applicant: Diverchim
    Inventors: Sylvain Darses, Nicolas Lefevre, Benoit Folleas, Jean-Louis Brayer
  • Publication number: 20140005301
    Abstract: 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: Application
    Filed: February 22, 2012
    Publication date: January 2, 2014
    Applicant: BASF SE
    Inventors: Kazuhiko Kunimoto, Hisatoshi Kura
  • Publication number: 20130324684
    Abstract: 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: Application
    Filed: January 31, 2012
    Publication date: December 5, 2013
    Applicants: JX NIPPON OIL & ENERGY CORPORATION, TOKYO INSTITUTE OF TECHNOLOGY
    Inventors: Yuki Arajawa, Gen-Ichi Konishi, Shunpei Nakajima, Sungmin Kang, Junji Watanabe, Takuya Matsumoto, Suzushi Nishimura, Takehiro Toyooka
  • Patent number: 8586603
    Abstract: 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: Grant
    Filed: December 20, 2010
    Date of Patent: November 19, 2013
    Inventors: Peter Gmeiner, Miriam Ruberg, Harald Hüebner
  • Patent number: 8552032
    Abstract: 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: Grant
    Filed: December 16, 2010
    Date of Patent: October 8, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Edward C. Lawson, Dennis J. Hlasta, Shyamali Ghosh, Renee L. DesJarlais, Carsten Schubert
  • Publication number: 20130253022
    Abstract: 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: Application
    Filed: November 18, 2011
    Publication date: September 26, 2013
    Applicants: FOX CHASE CHEMICAL DIVERSITY CENTER, INC., ADVANCED NEURAL DYNAMICS, INC.
    Inventors: Garry Robert Smith, Douglas E. Brenneman, Allen B. Reitz, Yan Zhang, Yanming Du
  • Publication number: 20130253183
    Abstract: 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: Application
    Filed: May 24, 2013
    Publication date: September 26, 2013
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Yumiko MIZUKI, Masakazu Funahashi, Mitsunori Ito, Masahiro Kawamura
  • Publication number: 20130245283
    Abstract: 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: Application
    Filed: April 23, 2013
    Publication date: September 19, 2013
    Applicant: Allergan, Inc.
    Inventors: Wha-Bin Im, Robert M. Burk, Mark Holoboski
  • Patent number: 8530512
    Abstract: 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: Grant
    Filed: December 20, 2010
    Date of Patent: September 10, 2013
    Inventors: Aaron P. Monte, M. Shahjahan Kabir, Marc A. Rott, William R. Schwan, James M. Cook, III, Jennifer A. Miskowski, Ranjit Verma, Leah Defoe
  • Patent number: 8518560
    Abstract: 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: Grant
    Filed: December 22, 2008
    Date of Patent: August 27, 2013
    Assignee: Idemitsu Kosan Co., Ltd.
    Inventors: Yumiko Mizuki, Masakazu Funahashi, Mitsunori Ito, Masahiro Kawamura
  • Publication number: 20130157195
    Abstract: 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: Application
    Filed: September 21, 2012
    Publication date: June 20, 2013
    Applicant: ROHM AND HAAS ELECTRONIC MATERIALS LLC
    Inventor: Rohm and Haas Electronic Materials LLC
  • Patent number: 8455497
    Abstract: 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: Grant
    Filed: February 12, 2009
    Date of Patent: June 4, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: 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
  • Patent number: 8445530
    Abstract: 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: Grant
    Filed: October 1, 2012
    Date of Patent: May 21, 2013
    Assignee: Sanofi
    Inventors: Matthias Schaefer, Josef Pernerstorfer, Dieter Kadereit, Hartmut Strobel, Werngard Czechtizky, L. Charlie Chen, Alena Safarova, Aleksandra Weichsel, Marcel Patek
  • Patent number: 8394971
    Abstract: 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: Grant
    Filed: January 20, 2010
    Date of Patent: March 12, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: James C. Lanter, Zhihua Sui, James J. Fiordeliso, Weiqin Jiang, Xuqing Zhang
  • Publication number: 20130035377
    Abstract: 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: Application
    Filed: April 15, 2011
    Publication date: February 7, 2013
    Applicants: UNIVERSITÀ DEGLI STUDI DI ROMA "LA SAPIENZA", UNIVERSITÀ DEGLI STUDI DI MILANO, UNIVERSITÀ DEGLI STUDI DI PAVIA, FONDAZIONE IEO
    Inventors: Saverio Minucci, Antonello Mai, Andrea Mattevi
  • Publication number: 20120302546
    Abstract: 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: Application
    Filed: February 3, 2011
    Publication date: November 29, 2012
    Applicants: FOX CHASE CHEMICAL DIVERSITY CENTER, INC., ADVANCED NEURAL DYNAMICS, INC.
    Inventors: Garry Robert Smith, Douglas Eric Brenneman, Allen B. Reitz, Yanming Du
  • Publication number: 20120273723
    Abstract: 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: Application
    Filed: November 29, 2010
    Publication date: November 1, 2012
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Michael Wittek, Brigitte Schuler, Volker Reiffenrath, Axel Jansen, Christian Hock, Harald Hirschmann
  • Publication number: 20120277262
    Abstract: 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: Application
    Filed: December 20, 2010
    Publication date: November 1, 2012
    Inventors: Peter Gmeiner, Miriam Ruberg, Harald Huebner
  • Patent number: 8283478
    Abstract: The present invention is directed to novel process for the preparation of sulfonylimine and sulfamide derivatives.
    Type: Grant
    Filed: April 19, 2006
    Date of Patent: October 9, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: Ahmed F. Abdel-Magid, Steven J. Mehrman
  • Publication number: 20120252836
    Abstract: 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: Application
    Filed: June 18, 2012
    Publication date: October 4, 2012
    Applicant: EVOLVA SA
    Inventors: Alexandra Santana Sorensen, Jean-Phillippe Meyer, Peteris Alberts, Mainkar Prathama
  • Patent number: 8273902
    Abstract: 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: Grant
    Filed: January 6, 2011
    Date of Patent: September 25, 2012
    Assignee: Toyama Chemical Co., Ltd.
    Inventors: Akihito Saitoh, Yoshiaki Suzuki, Kenji Yonezawa, Mitsuhide Kawamura, Takahiko Kusanagi, Takashi Nakai
  • Publication number: 20120165293
    Abstract: 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: Application
    Filed: July 13, 2010
    Publication date: June 28, 2012
    Inventors: George Petros Yiannikouros, Panos Kalaritis, Chaminda Priyapushpa Gamage, Stephenie Bosse Abernathy
  • Publication number: 20120157462
    Abstract: 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: Application
    Filed: January 30, 2008
    Publication date: June 21, 2012
    Inventors: Alan T. Johnson, Guan-Sheng Jiao
  • Patent number: 8202894
    Abstract: Compounds of the formula (I) in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Grant
    Filed: June 30, 2008
    Date of Patent: June 19, 2012
    Assignee: Syngenta Crop Protection LLC
    Inventors: Harald Walter, Daniel Stierli, Hans Tobler