Bicyclo Ring System Having The Oxazine Ring As One Of The Cyclos Patents (Class 544/90)
  • Patent number: 11155540
    Abstract: A sulfurized benzoxazine compound, which is usable for the synthesis of a polybenzoxazin, corresponds to formula (A): in which: each benzene nucleus of the two oxazine rings bears at least one radical denoted as “G”; the two oxazine rings are connected together via a central aromatic group, the benzene ring of which bears one, two, three or four groups of formula —Sx—R in which “x” is an integer from 1 to 8 and R represents hydrogen or a hydrocarbon-based group including 1 to 10 carbon atoms and optionally a heteroatom chosen from O, S, N and P; and the at least two radicals G, which may be identical or different, are chosen from various groups.
    Type: Grant
    Filed: June 12, 2018
    Date of Patent: October 26, 2021
    Assignee: COMPAGNIE GENERALE DES ETABLISSEMENTS MICHELIN
    Inventors: Milan Fedurco, Marco Ribezzo
  • Patent number: 11104641
    Abstract: The present disclosure describes a method of synthesizing carbodiimides comprising providing an alkylisothiourea, providing a thiophilic reagent to the reaction mixture and reacting under conditions sufficient to provide the carbodiimide, and wherein the carbodiimide is a polycarbodiimide or a biscarbodiimide. The present disclosure further describes methods for isolating the carbodiimides. The present disclosure additionally describes isolated carbodiimide compositions.
    Type: Grant
    Filed: March 8, 2017
    Date of Patent: August 31, 2021
    Assignee: Dow Global Technologies LLC
    Inventors: Andrew M. Camelio, Arkady L. Krasovskiy
  • Patent number: 10829460
    Abstract: The present invention is directed to compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R2?, L, X, W, Y1, Y2, Y3, and Y4 are described herein, useful as inhibitors of zinc-dependent histone deacetylases (HDACs) and in the treatment of diseases or disorders associated with HDACs.
    Type: Grant
    Filed: June 24, 2019
    Date of Patent: November 10, 2020
    Assignee: Valo Early Discovery, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Jennifer R. Thomason, Mary-Margaret Zablocki, Bingsong Han, Nicholas Barczak, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., Kenneth W. Bair
  • Patent number: 10766887
    Abstract: The present invention relates to a benzoxazine-based mixture and a use thereof and, more specifically, to a benzoxazine-based mixture and a use of a cured product in which the benzoxazine-based mixture is cured, wherein the benzoxazine-based mixture has high dielectric characteristics, heat resistant characteristics, and flame-retardant characteristics by comprising a benzoxazine ring in a molecular structure, and thus can be applied to a sealing material, a molding material, a template material, an adhesive, a material for an electric insulation paint, and the like, which are used for a copper clad laminate or an electronic part, used in a printed circuit board.
    Type: Grant
    Filed: June 30, 2017
    Date of Patent: September 8, 2020
    Assignee: KOLON INDUSTRIES, INC.
    Inventors: Sae Rom Nam, Do Kyung Sung, Hee Jin Cho
  • Patent number: 10736901
    Abstract: This invention relates to deuterated analogs of etifoxine of Formula 1, solvates, prodrugs, and pharmaceutically acceptable salts thereof, as well as to methods for their preparation and use, and to pharmaceutical compositions. Briefly, this invention is generally directed to deuterated analogs of etifoxine as well as to methods for their preparation and use, and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: September 21, 2018
    Date of Patent: August 11, 2020
    Assignee: GABA THERAPEUTICS INC.
    Inventor: Olivier Dasse
  • Patent number: 10544261
    Abstract: The present invention relates to a phosphinated poly(2,6-dimethy phenylene oxide)oligomer, specifically an unsaturated group-containing phosphinated poly(2,6-dimethy phenylene oxide)oligomer, and processes for producing the same. A thermoset produced from the unsaturated group-containing phosphinated poly(2,6-dimethy phenylene oxide)oligomers according to the present invention exhibits flame retardancy and has a low dielectric constant and dissipation factor and a high glass transition temperature.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: January 28, 2020
    Assignee: Chang Chun Plastics Co., Ltd.
    Inventors: Ching Hsuan Lin, Ping-Chieh Wang, An-Pang Tu, Kuen-Yuan Hwang, Chun Yu Tseng
  • Patent number: 10370343
    Abstract: The present invention is directed to compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, solvates, hydrates, tautomers, or isomers or thereof, wherein R1, R2, R2?, L, X, W, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: June 8, 2018
    Date of Patent: August 6, 2019
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Jennifer R. Thomason, Mary-Margaret Zablocki, Bingsong Han, Nicholas Barczak, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Jr., Kenneth W. Bair
  • Patent number: 10227313
    Abstract: A synthesis process for making a benzoxazine compound containing at least one benzoxazine unit from aromatic amine containing at least one primary amino group, at least one phenolic compound with at least one ortho-hydrogen, and alkyl formcel. In one embodiment, the aromatic amine is reacted with alkyl formcel to generate an alkoxymethyl intermediate compound. Subsequently, the intermediate compound is reacted with a phenol to generate the benzoxazine compound. In another embodiment, the benzoxazine compound is formed by reacting aromatic amine with alkyl formcel and phenol in one reaction step. Also disclosed is a method for isolating the alkoxymethyl compound formed by reacting aromatic amine with alkyl formcel. The isolated alkoxymethyl compound is useful as a reactant in a subsequent reaction.
    Type: Grant
    Filed: January 11, 2018
    Date of Patent: March 12, 2019
    Assignee: CYTEC INDUSTRIES INC.
    Inventors: Ram B. Gupta, Manav Gupta
  • Patent number: 10144716
    Abstract: This invention relates to a polybenzoxazine precursor and a method of preparing the same, and more particularly, to a polybenzoxazine precursor which includes benzoxazine obtained by reacting a phenol novolak resin with an aldehyde compound and allylamine and diaminodiphenylmethane as an amine compound, and to a method of preparing the same. The polybenzoxazine precursor may serve to prepare a hardened material having excellent thermal and electrical characteristics and dimensional stability. Accordingly, the polybenzoxazine precursor may be available for use in a copper clad laminate, a semiconductor encapsulant, a printed circuit board, an adhesive, a paint, and a mold.
    Type: Grant
    Filed: December 7, 2015
    Date of Patent: December 4, 2018
    Assignee: KOLON INDUSTRIES, INC.
    Inventors: Hee Jin Cho, Do Kyung Sung, Ki Hyun Park, Sang Hun Park
  • Patent number: 10080755
    Abstract: This invention relates to deuterated analogs of etifoxine of Formula 1, solvates, prodrugs, and pharmaceutically acceptable salts thereof, as well as to methods for their preparation and use, and to pharmaceutical compositions. Briefly, this invention is generally directed to deuterated analogs of etifoxine as well as to methods for their preparation and use, and to pharmaceutical compositions containing the same.
    Type: Grant
    Filed: March 18, 2016
    Date of Patent: September 25, 2018
    Assignee: ANVYL, LLC
    Inventor: Olivier Dasse
  • Patent number: 10029995
    Abstract: The present invention is directed to compounds of Formula I: and pharmaceutically acceptable salts, prodrugs, solvates, hydrates, tautomers, or isomers or thereof, wherein R1, R2, R2?, L, X, W, Y1, Y2, Y3, and Y4 are described herein.
    Type: Grant
    Filed: September 2, 2016
    Date of Patent: July 24, 2018
    Assignee: Forma Therapeutics, Inc.
    Inventors: Xiaozhang Zheng, Pui Yee Ng, Jennifer R. Thomason, Mary-Margaret Zablocki, Bingsong Han, Nicholas Barczak, Cuixian Liu, Aleksandra Rudnitskaya, David R. Lancia, Kenneth W. Bair
  • Patent number: 9902706
    Abstract: A synthesis process for making a benzoxazine compound containing at least one benzoxazine unit from aromatic amine containing at least one primary amino group, at least one phenolic compound with at least one ortho-hydrogen, and alkyl formcel. In one embodiment, the aromatic amine is reacted with alkyl formcel to generate an alkoxymethyl intermediate compound. Subsequently, the intermediate compound is reacted with a phenol to generate the benzoxazine compound. In another embodiment, the benzoxazine compound is formed by reacting aromatic amine with alkyl formcel and phenol in one reaction step. Also disclosed is a method for isolating the alkoxymethyl compound formed by reacting aromatic amine with alkyl formcel. The isolated alkoxymethyl compound is useful as a reactant in a subsequent reaction.
    Type: Grant
    Filed: October 21, 2015
    Date of Patent: February 27, 2018
    Assignee: CYTEC INDUSTRIES INC.
    Inventors: Ram B Gupta, Martin Cohen, Manav Gupta
  • Patent number: 9809584
    Abstract: A synthesis method of a sulfur-containing oxazine compound is provided. First, an oxazine compound as a precursor and an elemental sulfur as a feedstock are provided. Then, the elemental sulfur reacts with the oxazine compound directly to form a sulfur-containing oxazine compound.
    Type: Grant
    Filed: November 22, 2016
    Date of Patent: November 7, 2017
    Assignee: National Tsing Hua University
    Inventors: Ying-Ling Liu, Ho-Keng Lin
  • Patent number: 9611261
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
    Type: Grant
    Filed: November 4, 2015
    Date of Patent: April 4, 2017
    Assignee: Amgen Inc.
    Inventors: Ana Elena Minatti, Jonathan D. Low, Jennifer R. Allen, Albert Amegadzie, James Brown, Michael J. Frohn, Angel Guzman-Perez, Paul E. Harrington, Patricia Lopez, Vu Van Ma, Nobuko Nishimura, Wenyuan Qian, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Adrian L. Smith, Ryan White, Qiufen Xue
  • Patent number: 9217115
    Abstract: The use of tetrahydrobenzoxazines I where R1 is a hydrocarbyl radical and R2, R3, R4 and R5 are each independently hydrogen atoms, hydroxyl groups or hydrocarbyl radicals, and where R2 to R5 may also form a second and a third tetrahydrooxazine ring, with the proviso that at least one of the substituents has from 4 to 3000 carbon atoms and the remaining substituents, when they are hydrocarbyl radicals, each have from 1 to 20 carbon atoms, as stabilizers for stabilizing inanimate organic material, especially turbine fuels, against the action of light, oxygen and heat.
    Type: Grant
    Filed: July 18, 2006
    Date of Patent: December 22, 2015
    Assignee: BASF SE
    Inventors: Arno Lange, Helmut Mach, Hans Peter Rath, Dietmar Posselt
  • Patent number: 9206199
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.
    Type: Grant
    Filed: December 11, 2012
    Date of Patent: December 8, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Barbara Pio, Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Shawn Walsh
  • Patent number: 9120763
    Abstract: The present disclosure provides a method for producing a benzoxazine compound by reacting a bi-functional phenol with formaldehyde and a mono-functional amine in the presence of a solvent system containing an apolar solvent and a polar aprotic solvent. Once formed, the benzoxazine compound may be precipitated from the reaction solution and dried to form a benzoxazine compound in powder form.
    Type: Grant
    Filed: July 24, 2012
    Date of Patent: September 1, 2015
    Assignee: Huntsman Advanced Materials Americas LLC
    Inventors: Dong Wang, Derek Scott Kincaid
  • Patent number: 9085576
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
    Type: Grant
    Filed: March 6, 2014
    Date of Patent: July 21, 2015
    Assignee: AMGEN INC.
    Inventors: Ana Elena Minatti, Jonathan D. Low, Jennifer R. Allen, Albert Amegadzie, James Brown, Michael J. Frohn, Angel Guzman-Perez, Paul E. Harrington, Patricia Lopez, Vu Van Ma, Nobuko Nishimura, Wenyuan Qian, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Adrian L. Smith, Ryan White, Qiufen Xue
  • Publication number: 20150133440
    Abstract: The present invention provides difluoro-cyclopentaoxazinyls and difluoroenzooxazinyls of formula (I) having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
    Type: Application
    Filed: June 24, 2013
    Publication date: May 14, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventor: Hans Hilpert
  • Publication number: 20150126679
    Abstract: The invention relates to polymerizable benzoxazine compounds with interfacial active or surface active properties, having at least one polyalkylene oxide structural element, and to a method for producing said compounds. The invention also relates to benzoxazine (co)polymers comprising at least one of said benzoxazine compounds in the polymerized form.
    Type: Application
    Filed: January 6, 2015
    Publication date: May 7, 2015
    Inventors: Andreas Taden, Stefan Kreiling, Rainer Schoenfeld
  • Patent number: 8969550
    Abstract: The invention is directed to a process for the preparation of a cyclic carbamate starting with o-aminobenzyl alcohol and/or a suitable salt thereof, which is reacted with a cyclization agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C2-5-alkyl C2-5-carboxylates and mixtures of at least one C2-5-alkyl C2-5-carboxylate with at least one C5-8-alkane.
    Type: Grant
    Filed: October 14, 2011
    Date of Patent: March 3, 2015
    Assignee: Lonza Ltd.
    Inventors: Meinrad Brenner, Erick M. Carreira, Nicka Chinkov, Miriam Lorenzi, Aleksander Warm, Lothar Zimmermann
  • Patent number: 8957204
    Abstract: The invention is directed to a process for the preparation of a cyclic carbamate starting with a chiral propargylic alcohol and/or a suitable salt thereof, which is reacted with a cyclization agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction is carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C2-5-alkyl C2-5-carboxylates and mixtures of at least one C2-5-alkyl C2-5-carboxylate with at least one C5-8-alkane. Another aspect of the invention is directed to a process for the synthesis of said cyclic carbamate starting described above, wherein also a process for the preparation of the chiral propargylic alcohol is provided.
    Type: Grant
    Filed: October 14, 2011
    Date of Patent: February 17, 2015
    Assignee: Lonza Ltd.
    Inventors: Meinrad Brenner, Erick M. Carreira, Nicka Chinkov, Miriam Lorenzi, Aleksander Warm, Lothar Zimmermann
  • Patent number: 8865052
    Abstract: The TPU of this invention contains unsaturation in its polymeric backbone. The unsaturation can be present in the soft segment or in the hard segment or in both the soft and hard segments of the TPU. The TPU can be molded like a thermoplastic, and can be subsequently crosslinked by exposure to electron beam irradiation into thermoset articles having excellent chemical resistance, dimensional stability, set properties, heat resistance, oxidative resistance, and creep resistance. In one embodiment, the TPUs of this invention are the reaction product (1) a hydroxyl terminated intermediate, (2) a polyisocyanate, (3) a saturated glycol chain extender, and (4) a glycol chain extender containing carbon-carbon double bonds, such as the allyl moieties present in trimethylolpropane monoallyl ether.
    Type: Grant
    Filed: January 21, 2011
    Date of Patent: October 21, 2014
    Assignee: Lubrizol Advanced Materials, Inc.
    Inventors: Umit G. Makal, Louis J. Brandewiede, George H. Loeber
  • Publication number: 20140275058
    Abstract: The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, each of Ra, Rb, R1, R2, R3 and R7 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formulas II and III, and sub-formula embodiments thereof, intermediates and methods for preparing compounds of the invention.
    Type: Application
    Filed: March 6, 2014
    Publication date: September 18, 2014
    Inventors: Ana Elena MINATTI, Jonathan D. LOW, Jennifer R. ALLEN, Albert AMEGADZIE, James BROWN, Michael J. FROHN, Angel GUZMAN-PEREZ, Paul E. HARRINGTON, Patricia LOPEZ, Vu Van MA, Nobuko NISHIMURA, Wenyuan QIAN, Shannon RUMFELT, Robert M. RZASA, Kelvin SHAM, Adrian L. SMITH, Ryan WHITE, Qiufen XUE
  • Patent number: 8822460
    Abstract: The present invention comprises compounds of Formula (I). wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Grant
    Filed: April 4, 2013
    Date of Patent: September 2, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael P. Winters, Nagy E. Fawzy, Fu-An Kang, Zhihua Sui
  • Patent number: 8784684
    Abstract: A compound which has a benzoxazinone ring and an aromatic ring that directly bonds to the benzoxazinone ring, and has a mesogenic core substituted by a substituent having a polymerizable functional group is excellent in terms of durability, colorless, and exhibits a high ?n while having an azomethine bond.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: July 22, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Satoshi Shimamura, Mitsuyoshi Ichihashi
  • Publication number: 20140163224
    Abstract: The use of tetrahydrobenzoxazines I where R1 is a hydrocarbyl radical and R2, R3, R4 and R5 are each independently hydrogen atoms, hydroxyl groups or hydrocarbyl radicals, and where R2 to R5 may also form a second and a third tetrahydrooxazine ring, with the proviso that at least one of the substituents has from 4 to 3000 carbon atoms and the remaining substituents, when they are hydrocarbyl radicals, each have from 1 to 20 carbon atoms, as stabilizers for stabilizing inanimate organic material, especially turbine fuels, against the action of light, oxygen and heat.
    Type: Application
    Filed: February 12, 2014
    Publication date: June 12, 2014
    Applicant: BASF SE
    Inventors: Arno LANGE, Helmut MACH, Hans Peter RATH, Dietmar POSSELT
  • Publication number: 20140148597
    Abstract: The present disclosure provides a method for producing a benzoxazine compound by reacting a phenolic compound with an aldehyde compound and an amine compound in the presence of a solvent system containing a apolar solvent and a polar aprotic solvent. The benzoxazine compound may be easily recovered from the solvent system to provide a benzoxazine compound in powder form that is substantially solvent-free.
    Type: Application
    Filed: July 24, 2012
    Publication date: May 29, 2014
    Inventors: Dong Wang, Derek Scott Kincaid
  • Publication number: 20140135318
    Abstract: Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: W and Q and G are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bcl-2 family antiapoptotic proteins for the treatment of cancer; and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: May 23, 2012
    Publication date: May 15, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Zhen-Wei Cai, Andrew J. Tebben, Heidi L. Perez, Liping Zhang, Gretchen M. Schroeder, Donna D. Wei
  • Publication number: 20140135320
    Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 15, 2014
    Applicant: Jacobus Pharmaceutical Company, Inc.
    Inventors: Gavin David Heffernan, David Penman Jacobus, Kurt William Saionz, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
  • Patent number: 8653259
    Abstract: The invention provides the process illustrated in scheme 1 for synthesizing heterocyclic compounds of formula I. In the process, an isothiocyanate of formula II is initially reacted with a primary amine or formula III to give a thiourea of formula IV. Subsequently, the thiourea of formula IV is converted to the corresponding heterocycle of formula I using a base and a sulfonyl chloride.
    Type: Grant
    Filed: February 6, 2008
    Date of Patent: February 18, 2014
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Uwe Heinelt, Hans-Jochen Lang
  • Publication number: 20140018356
    Abstract: The present invention comprises compounds of Formula (I). wherein: R0, R1, R2, R3, R4, R5, and A are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Application
    Filed: April 4, 2013
    Publication date: January 16, 2014
    Applicant: Janssen Pharmaceutica, NV
    Inventor: Janssen Pharmaceutica, NV
  • Publication number: 20130281444
    Abstract: The present invention provides a biphenyl benzamide-derived derivatives, which structure is selected from formula I or formula II: and the synthesis and the application thereof.
    Type: Application
    Filed: August 9, 2012
    Publication date: October 24, 2013
    Inventors: Deh-Ming CHANG, Hsu-Shan HUNAG, Chia-Chung LEE, Chun-Liang CHEN
  • Publication number: 20130267659
    Abstract: Disclosed herein are monofunctional benzoxazine compounds having at least one electron-withdrawing group. The monofunctional benzoxazine compounds may be combined with one or more multifunctional benzoxazine compounds to form a unique benzoxazine blend. This benzoxazine blend may be combined with additional components such as catalysts and toughening agents to form a curable resin composition suitable for forming resinous films or composite materials. The presence of monofunctional benzoxazine improves the processability of the benzoxazine-based resin composition by reducing the viscosity of the resin composition, and results in improved tack and drape in the films and composite materials formed from the composition without the loss of modulus in the cured resin.
    Type: Application
    Filed: March 21, 2013
    Publication date: October 10, 2013
    Applicant: Cytec Technology Corp.
    Inventors: Steven Ward, Mark Harriman
  • Publication number: 20130267510
    Abstract: The invention provides compounds of formula (I): Said compounds being inhibitors of Kv3 channels and of use in the prophylaxis or treatment of related disorders.
    Type: Application
    Filed: December 6, 2011
    Publication date: October 10, 2013
    Applicant: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Giuseppe Alvaro, Paolo Dambruoso, Simona Tommasi, Anne Decor, Charles Large
  • Patent number: 8507148
    Abstract: A benzoxazine-based monomer includes a halogen atom-containing functional group and a nitrogen-containing heterocyclic group. A polymer formed from the benzoxazine-based monomer may be used in an electrode for a fuel cell and electrolyte membrane for a fuel cell.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: August 13, 2013
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Seongwoo Choi, Jungock Park
  • Patent number: 8476264
    Abstract: The present invention provides N-(3-(2-amino-6,6-difluoro-4,4a,5,6,7,7a-hexahydro-cyclopenta[e][1,3]oxazin-4-yl)-phenyl)-amides of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: July 2, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Emmanuel Pinard, Thomas Woltering
  • Publication number: 20130150354
    Abstract: The present invention relates to novel and selective antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD as well as pain.
    Type: Application
    Filed: June 14, 2012
    Publication date: June 13, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner EBEL, Sara FRATTINI, Riccardo GIOVANNINI, Stefan SCHEUERER
  • Publication number: 20130123241
    Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) of formula (I) wherein HET is a group selected from among formulas (IIa) (IIb) (IIc) (IId) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD and pain diseases.
    Type: Application
    Filed: May 10, 2011
    Publication date: May 16, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Heiner Ebel, Sara Frattini, Riccardo Giovannini, Christoph Hoenke, Rocco Mazzaferro, Stefan Scheuerer
  • Patent number: 8420808
    Abstract: The present invention is directed to a process for the preparation of Efavirenz, (4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one, of formula (I) comprising reacting the intermediate of formula (II) [0045] as a free base or a salt thereof, with diphosgene (TCMCF, trichlormethylchloroformate) Cl3CO—COCl in an organic solvent or in a biphasic medium comprised of an organic solvent and water, preferably but not mandatorily in the presence of a weak base in an amount sufficient to neutralise the reaction mixture or in an up to 30% molar excess of such amount.
    Type: Grant
    Filed: January 30, 2009
    Date of Patent: April 16, 2013
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Alessandro Leganza, Marco Galvagni
  • Publication number: 20130072478
    Abstract: The present invention provides N-(3-(2-amino-6,6-difluoro-4,4a,5,6,7,7a-hexahydro-cyclopenta[e][1,3]oxazin-4-yl)-phenyl)-amides of formula I having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.
    Type: Application
    Filed: September 11, 2012
    Publication date: March 21, 2013
    Inventors: Hans Hilpert, Emmanuel Pinard, Thomas Woltering
  • Patent number: 8394791
    Abstract: This invention concerns a crystalline, enantiopure hydrochloride salt of N-(5-{2-[3-(4,4-diethyl-2-oxo-4H-benzo[d][1,3]oxazin-1-yl)-1,1-dimethyl-propylamino-1-hydroxy-ethyl}-2-hydroxy-phenyl)-methanesulfonamide, preferably of N-(5-{(R)-2-[3-(4,4-diethyl-2-oxo-4H-benzo[d][1,3]oxazin-1-yl)-1,1-dimethyl-propylamino-1-hydroxy-ethyl}-2-hydroxy-phenyl)-methanesulfonamide and its action as a long acting beta-agonist, alone or in combination with one or multiple other active ingredients for the treatment of respiratory diseases.
    Type: Grant
    Filed: February 17, 2009
    Date of Patent: March 12, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ulrike Werthmann, Marco Santagostino, Adil Duran
  • Publication number: 20130029979
    Abstract: Fused bicyclic compound having an affinity to mineral corticoid receptor (MR), of formula [I]: wherein ring A is benzene having a substituent R1, fused to an adjacent 6-membered heterocyclic ring and further optionally having a substituent(s) other than R1, R1 is alkylsulfonylamino, etc., R2 and R3 are (a) the same of different and are hydrogen, alkyl, or optionally substituted aryl, or (b) combined with each other to form an oxo group or (c) combined with each other at its terminal together with the adjacent carbon atom to form cycloalkyl, X is ?N—, ?C(R4)— or —CH(R4)—, R4 is (a) hydrogen, (b) cyano, (c) halogen, (d) alkyl, (e) alkenyl, (f) cycloalkyl, (g) alkanoyl, (h) carbamoyl, or (i) cycloalkenyl, Ar is an optionally substituted aromatic cyclic group and a dotted line means presence or absence of a double bond, or a pharmaceutically acceptable salt thereof, useful e.g. as an antihypertensive agent.
    Type: Application
    Filed: July 30, 2012
    Publication date: January 31, 2013
    Inventors: Yoichi TAKAHASHI, Nobumasa Awai, Hidenori Akatsuka, Takayuki Kawaguchi, Toru Iljima
  • Patent number: 8318930
    Abstract: Disclosed herein is a novel process for preparing polymorphic Forms of (S)-6-chloro-(cyclopropylethynyl)-1,4-di-hydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one referred as M1, I, II, ?, and ?.
    Type: Grant
    Filed: December 24, 2008
    Date of Patent: November 27, 2012
    Assignee: Matrix Laboratories Limited
    Inventors: Om Dutt Tyagi, Ramakoteswara Rao Jetti, B. A. Ramireddy
  • Patent number: 8288533
    Abstract: This invention relates to syntheses for the preparation of benzoxazine, including benzoxazine monomers and benzoxazime oligomers, from phenolic compounds, aldehyde compounds, and either primary diamine compounds, such as diamino alkylene compounds, e.g., methylene diamine, or diamino arylene compounds, e.g., phenylene diamine, using water, and optionally an organic solvent, as the reaction solvent.
    Type: Grant
    Filed: September 23, 2010
    Date of Patent: October 16, 2012
    Assignee: Henkel Corporation
    Inventors: Wei Helen Li, Wenbo Jiang
  • Publication number: 20120258961
    Abstract: The present invention provide a medicament for treating the diseases induced by production, secretion or deposition of amyloid-? proteins, for example, a compound of the following formula (I) wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, ring A, Y and the dotted line are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: December 22, 2010
    Publication date: October 11, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Shinji Suzuki, Yuuji Kooriyama
  • Publication number: 20120251920
    Abstract: A benzoxazine-based monomer includes a halogen atom-containing functional group and a nitrogen-containing heterocyclic group. A polymer formed from the benzoxazine-based monomer may be used in an electrode for a fuel cell and electrolyte membrane for a fuel cell.
    Type: Application
    Filed: May 4, 2012
    Publication date: October 4, 2012
    Applicant: Samsung Electronics Co., Ltd.
    Inventors: Seongwoo Choi, Jungock Park
  • Publication number: 20120245157
    Abstract: The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-? proteins. A compound of the formula (I): wherein R1, R2a, R2b, R3, R4a, R4b, ring A and the dashed lines are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: December 10, 2010
    Publication date: September 27, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Moriyasu Masui, Akihiro Hori
  • Publication number: 20120245155
    Abstract: The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-?proteins. A compound of the formula (I): wherein R1, R2a, R2b, R3, R4, R5a, R5b, R6a, R6b, X, Y, Z, ring A and the dashed lines are defined in the specification, its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: December 9, 2010
    Publication date: September 27, 2012
    Applicant: Shionogi & Co., Ltd.
    Inventors: Syuhei Yoshida, Issei Kato, Kouki Fuchino, Yuuji Kooriyama, Yoshiyasu Baba, Norihiko Tanimoto
  • Patent number: 8258131
    Abstract: The present invention provides a novel fused bicyclic compound having an affinity to a receptor of mineral corticoid (MR), shown by the formula [I]: wherein the ring A is a benzene ring having a substituent R1, fused to an adjacent 6-membered heterocyclic ring and further optionally having a substituent(s) other than R1, R1 is an alkylsulfonylamino group etc.
    Type: Grant
    Filed: July 21, 2008
    Date of Patent: September 4, 2012
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Yoichi Takahashi, Nobumasa Awai, Hidenori Akatsuka, Takayuki Kawaguchi, Toru Iijima