1,3-oxazoles (including Hydrogenated) Patents (Class 548/215)
  • Patent number: 10253007
    Abstract: The present invention provides taxanes compounds with a formula (I) or formula (II) structure, a method for preparing the compounds, as well as the use of the compositions containing the compounds, pharmaceutically acceptable salts and solvates thereof as active ingredients in manufacturing oral antitumor medicaments, In formula (I), R1 is —COR6, —COOR6 or —CONR7aR7b; R2 is a C1-C6 alkyl, a C1-C6 alkenyl, a substituted hydrocarbon group, a heterocyclic group, an aromatic group or a substituted aromatic group; R3 is —OR6, —OCOOR6, —OCOSR6 or —OCONR7aR7b; R4 is —OR6, —OCOOR6, —OCOSR6, —OCONR7aR7b or H; wherein, R6 is a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group; R7a and R7b are respectively hydrogen, a hydrocarbon group, a substituted hydrocarbon group or a heterocyclic group.
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: April 9, 2019
    Assignee: Jiangsu Tasly Diyi Pharmaceutical Co., Ltd.
    Inventors: Wei Zhou, Yunrong Jing, Yongfeng Wang, Guocheng Wang
  • Patent number: 9951000
    Abstract: A method for synthesizing florfenicol comprises the steps of cyclization, selective reduction, fluorination, ring opening, deprotection, acylation, esterification with sulfonic acids, epimerization and hydrolysis. Florfenicol is prepared by successively purifying, selectively reducing, and epimerizing chiral (R)-amino ketones. This improves atom economy, reduces waste water pollution and accordingly reduces costs for treating waste water and pollution to the environment, thus lowering costs and simplifying the process. Furthermore, triethylamine hydrofluoride is used as a fluorinating reagent, resulting in improved safety, because of the use of liquid reaction conditions as compared to gaseous reaction conditions, and reduced corrosion to the reaction equipment.
    Type: Grant
    Filed: July 11, 2016
    Date of Patent: April 24, 2018
    Inventors: Yaowu Peng, Wenjing Tian, Qing Ye, Zhicheng Fang
  • Patent number: 9951252
    Abstract: Sealant systems that are pre-applied to a part to be sealed include a layer of an uncured moisture-curable sealant and a frangible barrier coating applied over the uncured moisture-curable sealant. During assembly, the barrier coating breaks to expose the moisture-curable sealant to moisture to initiate the curing reaction. The moisture-curable sealant systems are suitable for aerospace applications and include sulfur-containing prepolymers. Various curing chemistries can be used.
    Type: Grant
    Filed: August 10, 2015
    Date of Patent: April 24, 2018
    Assignee: PRC-DeSoto International, Inc.
    Inventors: Bruce Virnelson, Renhe Lin
  • Patent number: 9952758
    Abstract: The present invention provides a method an a device for mapping a virtual user input interface to a physical user input interface. The method is provided for mapping a virtual user input interface to a physical user input interface on a mobile terminal device. The mobile terminal device comprises a first physical user input interface, a display and a processing unit being connected to said display and said physical user interface, wherein an application is configured for use with a second user interface. The method of the invention comprises detecting an event indicative of an application to be executed that is configured for use with said second user interface and displaying a virtual user input interface representing said second user input interface on said display. If a a physical user input is received on said first physical user input interface, it is mapping to said displayed virtual user input interface, and displayed as an indication of a virtual input on said displayed virtual user input interface.
    Type: Grant
    Filed: May 31, 2014
    Date of Patent: April 24, 2018
    Assignee: Conversant Wireless Licensing S.a.r.l.
    Inventors: Sawako-Eeva Hayashi, Olaf Joeressen
  • Patent number: 9453008
    Abstract: The invention relates to the field of chemical and pharmaceutical industry and medicine and concerns compounds which can be used to produce agents for the treatment of cardiovascular diseases. The use of 2-[2-cyano-2-[5-(hydroxymethyl)-3-methyl-1,3-oxazolidin-2-ylidene]ethylidene]indolin-3-one of formula I is proposed as a biologically active compound exhibiting the properties of exogenous nitric oxide donor, a platelet aggregation inhibitor, also exhibiting antihypertensive activity and activating activity towards the soluble guanylate cyclase enzyme. Variants of methods for synthesizing the above compound are also proposed.
    Type: Grant
    Filed: October 29, 2012
    Date of Patent: September 27, 2016
    Assignee: PROTON OOO
    Inventors: Svetlana Yurevna Ryabova, Valery Aleksandrovich Parshin, Vladimir Grigorevich Granik, Nikita Borisovich Grigoriev, Ludmila Mikhaylovna Alekseeva
  • Patent number: 9233938
    Abstract: The invention relates to novel oxazolidinones their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering cholesterol ester transfer protein inhibitors.
    Type: Grant
    Filed: May 6, 2014
    Date of Patent: January 12, 2016
    Assignee: CoNCERT Pharmaceuticals, Inc.
    Inventor: Roger D. Tung
  • Patent number: 9199916
    Abstract: The invention is a novel process for the preparation of lacosamide by employing novel intermediates of formula III and IV:
    Type: Grant
    Filed: November 8, 2012
    Date of Patent: December 1, 2015
    Assignee: RAMAMOHAN RAO DAVULURI
    Inventors: Ramamohan Rao Davuluri, Guruswamy Batthini, Swetha Mustyala, Sudheer Kallepalli, Praveen Kumar Neela, Ravi Ponnaiah
  • Patent number: 8980886
    Abstract: The present invention relates to novel anthranilic acid derivatives of the general formula (I) in which R1, R2, R3, R4, R5, Qx, A, Qy and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and to a plurality of processes for their preparation.
    Type: Grant
    Filed: June 14, 2011
    Date of Patent: March 17, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Rüdiger Fischer, Christoph Grondal, Markus Heil, Heinz-Juergen Wroblowsky, Ernst Rudolf Gesing, Arnd Voerste, Ulrich Görgens
  • Publication number: 20150065494
    Abstract: The present invention provides an aminostyrylbenzofuran compound of Formula (I), and a pharmaceutical composition comprising same. The pharmaceutical composition of the present invention comprising the compound of Formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate, and a solvate thereof as an active ingredient can be useful for the prevention and treatment of degenerative brain diseases caused by accumulation of beta-amyloid.
    Type: Application
    Filed: April 1, 2013
    Publication date: March 5, 2015
    Inventors: Dong Jin Kim, Kyung Ho Yoo, Young Soo Kim, Woong Seo Park, Yong Koo Kang, Hye Yun Kim, Yun Kyung Kim, Ki Duk Park, Maeng Sup Kim, Kwee Hyun Suh, Young Gil Ahn
  • Patent number: 8969578
    Abstract: Disclosed herein are compounds derived from a chemical structure according to the formula (I) wherein X comprises oxygen or sulfur, R1 comprises a phenyl or naphthyl group, R2 comprises an amide group and R3 comprises a phosphate group. The disclosed compounds demonstrate inhibitory activity against STAT3, a protein found in certain tumor tissues and which promotes cellular overproliferation and resistance to apoptosis. The invention includes compositions containing the disclosed compounds, as well as methods of treatment therewith.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: March 3, 2015
    Assignee: University of Central Florida Research Foundation, Inc.
    Inventors: James Turkson, Andrew D. Hamilton
  • Patent number: 8962665
    Abstract: The present invention is concerned with substituted azole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant proteine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. In particular, several of these compounds are potent and selective Flt-3 inhibitors or/and syk inhibitors.
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: February 24, 2015
    Assignee: AB Science
    Inventors: Alain Moussy, Abdellah Benjahad, Jason Martin, Emmanuel Chevenier, Didier Pez, Franck Sandrinelli, Willy Picoul
  • Patent number: 8962857
    Abstract: The present invention provides methods for preparing TLR-4 receptor agonist E6020: and stereoisomers thereof, which compounds are useful as an immunological adjuvants when co-administered with antigens such as vaccines for bacterial and viral diseases. Also provided are synthetic intermediates.
    Type: Grant
    Filed: May 5, 2014
    Date of Patent: February 24, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Francis G. Fang, James E. Foy, Lynn Hawkins, Charles Lemelin, Andre LesCarbeau, Xiang Niu, Kuo-Ming Wu
  • Patent number: 8946442
    Abstract: Foams of ionic compounds are described. Methods of making the foams are also provided. The foams are ionic and can be used for catalysis, separations, gas storage, biosensors, electronics, and electrochemical applications.
    Type: Grant
    Filed: December 21, 2010
    Date of Patent: February 3, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: Mark Brandon Shiflett, Akimichi Yokozeki
  • Publication number: 20140323738
    Abstract: The invention is a novel process for the preparation of lacosamide by employing novel intermediates of formula III and IV:
    Type: Application
    Filed: November 8, 2012
    Publication date: October 30, 2014
    Inventor: RAMAMOHAN RAO DAVULURI
  • Publication number: 20140323458
    Abstract: The present disclosure provides substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes, of Formula I D-M-D??(Formula I) useful as antiviral agents. In certain embodiments disclosed herein M is a group —P-A-P— where A is Certain substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions/and combinations containing one or more substituted aliphanes, cyclophanes, heteraphanes, heterophanes, hetero-heteraphanes and metallocenes and a pharmaceutically acceptable carrier are also provided by this disclosure. Methods for treating viral infections, including Hepatitis C viral infections are provided by the disclosure.
    Type: Application
    Filed: July 10, 2014
    Publication date: October 30, 2014
    Inventors: Jason Allan Wiles, Qiuping Wang, Akihiro Hashimoto, Godwin Pais, Xiangzhu Wang, Venkat Gadhachanda, Avinash Phadke, Milind Deshpande, Dawei Chen
  • Patent number: 8864849
    Abstract: The present specification provides for an agent for coloring keratinic fibers. The agent includes, a cosmetic carrier, a compound of formula (I), R1 and R2 independently of one another denote hydrogen, a C1-C6 alkyl group, a C2-C6 alkenyl group, a hydroxyl group, a halogen, a C1-C6 alkoxy group, an amino group, a nitro group, an acetyl amino group, or a sulfonamide group; or when in ortho-position to one another, form a 5- or 6-membered, saturated or unsaturated ring, which optionally include further heteroatoms.
    Type: Grant
    Filed: May 6, 2014
    Date of Patent: October 21, 2014
    Assignee: Henkel AG & Co. KGaA
    Inventors: Wibke Gross, Ralph Nemitz, Melanie Moch, Astrid Kroos, Antje Gebert
  • Patent number: 8864848
    Abstract: The invention relates to agents for coloring keratinic fibers, in particular human hair, including in a cosmetic carrier at least one compound of the formula (I). The structures the of the general formula (I) have a heterocycle A which bears a quaternary nitrogen atom and thus a positive charge. The invention furthermore relates to the use of these novel azo dyes in agents for coloring hair and to the dyes themselves.
    Type: Grant
    Filed: May 5, 2014
    Date of Patent: October 21, 2014
    Assignee: Henkel AG & Co. KGAA
    Inventors: Wibke Gross, Ralph Nemitz, Melanie Moch
  • Patent number: 8846943
    Abstract: An object of the present invention is to provide a pyrrole derivative useful as an immunosuppressive agent and a method for producing the same. For achieving the object, the present invention provides a method for producing a compound represented by the general formula (I) by heating a compound represented by the general formula (III) and a compound represented by the general formula (IV) in a nonpolar solvent under reduced pressure.
    Type: Grant
    Filed: May 31, 2013
    Date of Patent: September 30, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Makoto Yamaoka, Yoshitaka Nakamura
  • Publication number: 20140288312
    Abstract: The invention relates to oseltamivir derivatives as influenza neuraminidase inhibitors for treating influenza infections and to a method for producing said compounds.
    Type: Application
    Filed: October 29, 2012
    Publication date: September 25, 2014
    Inventors: Bernd Clement, Joscha Kotthaus, Jurke Kotthaus, Dennis Schade
  • Patent number: 8841281
    Abstract: The present invention relates to the fields of chemistry and pharmaceuticals. Embodiments of the present invention provide transition metal complexes of amino acids. Transition metal complexes of embodiments of the invention according to Categories I, II, III, and/or IV may be used as antimicrobial, anti-malarial, and anti-cancer agents, as well as catalysts in chemical reactions. Such compounds of the invention are particularly useful for combating multi-drug resistance against a broad range of microbials (such as MRSA and mycobacteria), including gram positive and gram negative bacteria, as well as can be used as anti-cancer agents against bladder cancer, breast cancer, colon cancer, rectal cancer, endometrial cancer, kidney cancer, leukemia, lung cancer, melanoma, non-Hodgkin's lymphoma, pancreatic cancer, prostate cancer, and thyroid cancer, to name a few.
    Type: Grant
    Filed: October 17, 2012
    Date of Patent: September 23, 2014
    Assignee: Virginia Tech Intellectual Properties, Inc.
    Inventor: Joseph S. Merola
  • Patent number: 8834841
    Abstract: The present invention provides novel amino acid compounds useful in detecting and evaluating brain and body tumors. These compounds have the advantageous properties of rapid uptake and prolonged retention in tumors and can be labeled with halogen isotopes such as fluorine-18, iodine-123, iodine-124, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77, bromine-82, astatine-210, astatine-211, and other astatine isotopes. These compounds can also be labeled with technetium and rhenium isotopes using known chelation complexes. The compounds disclosed herein bind tumor tissues in vivo with high specificity and selectivity when administered to a subject. Preferred compounds show a target to non-target ratio of at least 2:1, are stable in vivo and substantially localized to target within 1 hour after administration. Preferred compounds include 1-amino-2-[18F]fluorocyclobutyl-1-carboxylic acid (2-[18F]FACBC) and 1-amino-2-[18]fluoromethylcyclobutyl-1-carboxylic acid (2-[18F]FMACBC).
    Type: Grant
    Filed: April 5, 2013
    Date of Patent: September 16, 2014
    Assignee: Emory University
    Inventor: Mark M. Goodman
  • Patent number: 8828908
    Abstract: Bicyclic dione compounds of formula (I), and derivatives thereof, which are suitable for use as herbicides.
    Type: Grant
    Filed: May 27, 2008
    Date of Patent: September 9, 2014
    Assignee: Syngenta Limited
    Inventors: Christopher John Mathews, Matthew Brian Hotson, Alan John Dowling, James Nicholas Scutt, Mangala Govenkar, Lee Challinor
  • Publication number: 20140235868
    Abstract: The invention relates to the field of chemical and pharmaceutical industry and medicine and concerns compounds which can be used to produce agents for the treatment of cardiovascular diseases. The use of 2-[2-cyano-2-[5-(hydroxymethyl)-3-methyl-1,3-oxazolidin-2-ylidene]ethylidene]indolin-3-one of formula I is proposed as a biologically active compound exhibiting the properties of exogenous nitric oxide donor, a platelet aggregation inhibitor, also exhibiting antihypertensive activity and activating activity towards the soluble guanylate cyclase enzyme. Variants of methods for synthesizing the above compound are also proposed.
    Type: Application
    Filed: October 29, 2012
    Publication date: August 21, 2014
    Applicant: PROTON OOO
    Inventors: Svetlana Yurevna Ryabova, Valery Aleksandrovich Parshin, Vladimir Grigorevich Granik, Vladimir Vladimirovich Grank, Nikta Borisovich Grigoriev, Ludmila Mikhaylovna Aleksseva
  • Publication number: 20140200245
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: March 14, 2014
    Publication date: July 17, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Carl R. ILLIG, Jinsheng CHEN, Renee Louise DESJARLAIS, Kenneth WILSON
  • Patent number: 8759383
    Abstract: The invention relates to novel oxazolidinones their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering cholesterol ester transfer protein inhibitors.
    Type: Grant
    Filed: March 14, 2008
    Date of Patent: June 24, 2014
    Assignee: Concert Pharmaceuticals, Inc.
    Inventor: Roger Tung
  • Patent number: 8748463
    Abstract: The invention provides novel classes of HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided as well as methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.
    Type: Grant
    Filed: July 17, 2012
    Date of Patent: June 10, 2014
    Assignee: Georgetown University
    Inventors: Alan P. Kozikowski, Anatoly Dritschilo, Mira Jung, Pavel A. Petukhov, Bin Chen
  • Patent number: 8729113
    Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.
    Type: Grant
    Filed: February 24, 2011
    Date of Patent: May 20, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
  • Patent number: 8722714
    Abstract: The present invention provides therapeutically active oxazolidine derivatives and compositions as NMDA antagonists, which are useful in preventing and treating central nervous system disorders by inhibiting over-activation of NMDA receptors. In one aspect, the present invention provides methods of treating and/or preventing neurodegenerative diseases and neuropathological disorders, methods of providing neuroprotection under stress conditions such as a stroke, and methods of enhancing the brain's cognitive functions in mammals and humans. For example, the compounds can prevent glutamate-induced neuro-toxicity by inhibiting the activities of the NMDA receptor in the presence of toxic doses of NMDA. In addition, the compounds can potentiate the calcium current in the presence of low dose of NMDA.
    Type: Grant
    Filed: January 16, 2009
    Date of Patent: May 13, 2014
    Assignee: The Honk Kong University of Science and Technology
    Inventors: Nancy Yuk-Yu Ip, Hua-Jie Zhu, Fanny Chui-Fun Ip
  • Patent number: 8722900
    Abstract: The present invention relates to processes for making cabazitaxel, cabazitaxel analogues and intermediates thereof. The invention provides novel compounds useful in the synthesis of cabazitaxel.
    Type: Grant
    Filed: October 30, 2012
    Date of Patent: May 13, 2014
    Assignee: ScinoPharm Taiwan, Ltd.
    Inventors: TsungYu Hsiao, Julian Paul Henschke, HsinChang Tseng
  • Publication number: 20140128614
    Abstract: To provide pesticidal allylAryl heterocycle derivatives that are useful as a pesticidal compound. Pesticidal allylAryl heterocycle derivatives that are expressed by the Formula (I), and pesticides and an agent for controlling animal parasites which include the allylAryl heterocycle derivatives as an effective component.
    Type: Application
    Filed: April 24, 2012
    Publication date: May 8, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Mamoru Hatazawa, Tetsuya Murata, Peter Bruechner, Daiei Yamazaki, Eiichi Shimojo, Teruyuki Ichihara, Katsuhiko Shibuya, Tadashi Ishikawa
  • Patent number: 8685369
    Abstract: One aspect of the invention relates to complexes of a radionuclide with various heteroaryl ligands, e.g., imidazolyl and pyridyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to imidazolyl and pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the radionuclide complexes are also described. Another aspect of the invention relates to imidazolyl and pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.
    Type: Grant
    Filed: February 14, 2005
    Date of Patent: April 1, 2014
    Assignee: Molecular Insight Pharmaceuticals, Inc.
    Inventors: John Babich, Kevin Maresca, James Kronauge
  • Publication number: 20140039198
    Abstract: An object of the present invention is to provide a pyrrole derivative useful as an immunosuppressive agent and a method for producing the same. For achieving the object, the present invention provides a method for producing a compound represented by the general formula (I) by heating a compound represented by the general formula (III) and a compound represented by the general formula (IV) in a nonpolar solvent under reduced pressure.
    Type: Application
    Filed: May 31, 2013
    Publication date: February 6, 2014
    Inventors: Makoto YAMAOKA, Yoshitaka NAKAMURA
  • Publication number: 20140031317
    Abstract: The present invention is directed to a novel 2-substituted benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.
    Type: Application
    Filed: October 1, 2013
    Publication date: January 30, 2014
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Vernon C Alford, JR., James C. Lanter, Raymond A. Ng
  • Patent number: 8609839
    Abstract: Camphor-derived compounds are disclosed, which are represented as the following formula (I): wherein R1, R2, R3, and R4 each are defined as described in the specification. In addition, a method for manufacturing the camphor-derived compounds and application thereof are disclosed.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: December 17, 2013
    Assignee: National Tsing Hua University
    Inventors: Biing-Jiun Uang, Bo-Yao Yang
  • Patent number: 8598340
    Abstract: The present invention can provide new spirooxazine radical derivatives of the following general formula (1) which have chromic property enabling the distinction between the radical species and the cation species on the basis of absorption wavelength:
    Type: Grant
    Filed: November 2, 2012
    Date of Patent: December 3, 2013
    Assignee: NEC Corporation
    Inventor: Atsumasa Sawada
  • Publication number: 20130303525
    Abstract: The present invention relates to a series of substituted compounds having the general formula (I), including their stereoisomers and/or their pharmaceutically acceptable salts. (I) Wherein A, m, R1s, R2, R3, R4 are as defined herein. This invention also relates to methods of making these compounds including intermediates. The compounds of this invention are effective at the kappa (?) opioid receptor (KOR) site. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic pain, and associated disorders, particularly functioning peripherally at the CNS.
    Type: Application
    Filed: July 19, 2011
    Publication date: November 14, 2013
    Applicants: DR. REDDY'S LABORATORIES, INC., DR. REDDY;S LABORATORIES LTD.
    Inventors: Pradip Kumar Sasmal, Vamsee Krishna Chintakunta, Vijay Potluri, Ish Kumar Khanna, Ashok Tehim, Mahaboobi Jaleel, Thomas Hogberg, Oystein Rist, Lisbeth Elster, Thomas Michael Frimurer, Lars-Ole Gerlach
  • Patent number: 8575358
    Abstract: Oxazolidinium compounds are formed by the reaction of a halohydrin or an epoxide with a secondary amine and an aldehyde or a ketone. The oxazolidinium compounds are formed directly and do not require the reaction of a pre-formed oxazolidine with an alkylating agent. The compounds are useful as gas hydrate inhibitors in oil and gas production and transportation. The oxazolidinium compounds have the structure: where R is a saturated or unsaturated alkyl group containing from 3 to 20 carbon atoms, where R has an absence of aryl groups; R1 and R2 each independently have 1 to 20 carbon atoms, may be linear, branched or cyclic; linear, branched or cyclic groups having 1 to 20 carbon atoms substituted with alkyl groups, aryl groups, alkylaryl groups, and aryl groups substituted with alkoxy groups, and X is selected from the group consisting of chlorine, fluorine, bromine or iodine.
    Type: Grant
    Filed: March 2, 2012
    Date of Patent: November 5, 2013
    Assignee: Baker Hughes Incorporated
    Inventors: Gordon T. Rivers, Jun Tian, James A. Hackerott
  • Patent number: 8541595
    Abstract: The present invention is directed to imidazoisoindole compounds which are antagonists of neuropeptide S receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which the neuropeptide S receptor is involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the neuropeptide S receptor is involved.
    Type: Grant
    Filed: November 3, 2009
    Date of Patent: September 24, 2013
    Assignee: Merch Sharp & Dohme Corp.
    Inventors: Peter J. Manley, Kausik K Nanda, B. Wesley Trotter
  • Patent number: 8536210
    Abstract: The present invention relates to compounds of general formula (i) having an oxime moiety or a pharmaceutically acceptable salt, hydrate or solvate thereof and its use for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1), a pharmaceutical composition comprising the compound or a salt, hydrate or solvate thereof as an active ingredient, a method for the prevention or the treatment of a SSAO/VAP-1 related disease, said diseases including acute or chronic inflammatory diseases, diseases related to carbohydrate metabolism, diabetes-associated complications, diabetic retinopathy and macular oedema, diseases related to adipocyte or smooth muscle dysfunctions, neurodegenerative diseases and vascular diseases.
    Type: Grant
    Filed: September 11, 2009
    Date of Patent: September 17, 2013
    Assignee: Semmelweis Egyetem
    Inventors: Péter Mátyus, Kálmán Magyar, Marjo Pihlavisto, Klára Gyires, Norbert Haider, Yinghua Wang, Patrick Woda, Petra Dunkel, Éva Tóth-Sarudy, György Túrós
  • Patent number: 8530461
    Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 10, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Bernd Nosse, Martin Fleck, Niklas Heine, Gerald Juergen Roth
  • Patent number: 8513290
    Abstract: Analogs of largazole are described herein. Methods of treating cancer and blood disorders using largazole and largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.
    Type: Grant
    Filed: June 7, 2012
    Date of Patent: August 20, 2013
    Assignees: Colorado State University Research Foundation, Dana-Farber Cancer Institute, Inc., University of Notre Dame du Lac
    Inventors: Robert M. Williams, James E. Bradner, Albert Bowers, Tenaya Newkirk, Olaf G. Wiest
  • Patent number: 8492371
    Abstract: Disclosed herein are compounds of formula (I) wherein Ring A and R1 are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and pharmaceutical compositions are also disclosed.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: July 23, 2013
    Assignee: AbbVie Inc.
    Inventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Steven P. Latshaw, Tongmei Li, Bo Liu, Sridhar Peddi, Xueqing Wang, Teodozyj Kolasa, Derek W. Nelson, Arturo Perez-Medrano
  • Patent number: 8486940
    Abstract: The invention relates to novel pyrrolidine derivatives of formula (I): wherein R1, R2 and R3 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
    Type: Grant
    Filed: September 13, 2010
    Date of Patent: July 16, 2013
    Assignee: Probiodrug AG
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
  • Patent number: 8466145
    Abstract: Described are novel compounds of the Formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol, triglyceride levels; treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis, rheumatoid arthritis; treatment and/or prophylaxis of type II diabetes. These compounds are more particularly dipeptidyl peptidase (DPP IV) inhibitors.
    Type: Grant
    Filed: January 7, 2010
    Date of Patent: June 18, 2013
    Assignee: Orchid Chemicals & Pharmaceuticals Limited
    Inventors: Gopalan Balasubramanian, Sukumar Sakamuri, Gajendra Singh, Sivanesan Dharmalingam, Franklin Pooppady Xavier, Shridhar Narayanan, Jeyamurugan Mookkan, Jeganatha Sivakumar Balasubramanian, Agneeswari Rajalingam, Jayanarayan Kulathingal
  • Patent number: 8460851
    Abstract: A salt represented by the formula (I): wherein Q1 and Q2 each independently represent a fluorine atom or a C1-C6 perfluoroalkyl group, L1 represents *—CO—O-La- or *—CH2—O-Lb-, * represents a binding position to —C(Q1)(Q2)-, La and Lb independently represent a C1-C15 divalent saturated hydrocarbon group in which one or more —CH2— can be replaced by —O— or —CO—, ring W1 represents a C2-C36 nitrogen-containing heterocyclic group in which one or more —CH2— can be replaced by —O—, and Z1? represents an organic counter ion.
    Type: Grant
    Filed: January 6, 2011
    Date of Patent: June 11, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Satoshi Yamaguchi, Koji Ichikawa
  • Publication number: 20130116444
    Abstract: The present invention relates to processes for making cabazitaxel, cabazitaxel analogues and intermediates thereof. The invention provides novel compounds useful in the synthesis of cabazitaxel.
    Type: Application
    Filed: October 30, 2012
    Publication date: May 9, 2013
    Applicant: Scinopharm Taiwan, LTD.
    Inventor: Scinopharm Taiwan, LTD.
  • Patent number: 8426645
    Abstract: Disclosed is a process for producing a protected optically active fluoroamine, which comprises the step of reacting an imine-protected optically active hydroxyamine, an oxazolidine-protected optically active hydroxyamine, or a mixture of the imine-protected optically active hydroxyamine and the oxazolidine-protected optically active hydroxyamine, with sulfuryl fluoride (SO2F2) in the presence of a tertiary amine having a carbon number of 7 to 18 (produced by substituting all of three hydrogen atoms in ammonia by alkyl groups). The desired optically active fluoroamine can be produced by hydrolyzing the protected optically active fluoroamine under acidic conditions.
    Type: Grant
    Filed: January 27, 2009
    Date of Patent: April 23, 2013
    Assignee: Central Glass Company, Limited
    Inventors: Akihiro Ishii, Takako Yamazaki, Manabu Yasumoto
  • Patent number: 8426587
    Abstract: The present invention is related to the preparation and pharmaceutical use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification: (I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases.
    Type: Grant
    Filed: November 19, 2008
    Date of Patent: April 23, 2013
    Assignee: Pharmaxis Ltd.
    Inventors: Ian A. McDonald, Craig Ivan Turner, Mandar Deodhar, Jonathan Stuart Foot
  • Publication number: 20130072678
    Abstract: The present invention can provide new spirooxazine radical derivatives of the following general formula (1) which have chromic property enabling the distinction between the radical species and the cation species on the basis of absorption wavelength:
    Type: Application
    Filed: November 2, 2012
    Publication date: March 21, 2013
    Applicant: NEC CORPORATION
    Inventor: NEC CORPORATION
  • Publication number: 20130058990
    Abstract: The present invention relates to a cosmetic composition containing a combination i) of at least one screening agent of the dibenzoylmethane derivative type and ii) of at least one particular hydrophilic or water-soluble merocyanin UV-screening agent, especially corresponding to one of the formulae (I) or (II) below: in which at least one or two of the radicals contain: either an alkylsulfonate radical in its acid or salified form, or one or two hydroxyl radicals. The invention also relates to a process for the radiation-photostabilization of at least one screening agent of the dibenzoylmethane derivative type with an effective amount of at least one particular hydrophilic or water-soluble merocyanin UV-screening agent, especially corresponding to one of the formulae (I) or (II).
    Type: Application
    Filed: March 7, 2011
    Publication date: March 7, 2013
    Applicant: L'OREAL
    Inventors: Herve Richard, Benoit Muller