Chalcogen Bonded Directly At 2-position Of The Oxazole Ring Patents (Class 548/229)
  • Patent number: 11034683
    Abstract: The present invention relates to the novel key intermediate, 4-{4-[(5S)-(Aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]-phenyl}-morpholin-3-one perchlorate, in the synthesis of rivaroxaban. The invention further relates to the crystalline form of novel intermediate, the process to prepare the novel intermediate and method of preparing rivaroxaban using this novel intermediate. The invention provides an improved and efficient process for preparation of Rivaroxaban.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: June 15, 2021
    Assignee: UNICHEM LABORATORIES LTD
    Inventors: Dhananjay G. Sathe, Arijit Das, Sanjay Raikar, Yashwant S. Surve, Bhushan S. Pandit
  • Patent number: 9695104
    Abstract: The invention relates to a process for transvinylation of a carboxylic acid feedstock with a vinyl ester feedstock to obtain a vinyl ester product and the corresponding acid of the vinyl ester feedstock in the presence of one or more ruthenium catalysts, wherein a) the vinyl ester feedstock, the carboxylic acid feedstock and a ruthenium catalyst are fed to the reactor, and b) the transvinylation reaction is carried out, characterized in that a carbonyl-free Ru(III) carboxylate is used as the ruthenium catalyst and in that no carbon monoxide is supplied, c) the reaction is carried out at a temperature of 110 to 170° C., d) upon completion of the transvinylation reaction, the vinyl ester feedstock and the corresponding acid are separated from the reaction mixture by distillation, e) the vinyl ester product is separated by distillation from the bottom product of the distillation, and f) the remaining reaction mixture is recycled into the reactor.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: July 4, 2017
    Assignee: Wacker Chemie AG
    Inventors: Peter Gigler, Maria Leute, Jürgen Stohrer
  • Patent number: 9422274
    Abstract: The present invention relates to oxazolidinone compounds represented by Chemical Formula 1, pharmaceutically acceptable salts thereof or hydrates, a method of preparing the same, and a pharmaceutical composition for preventing or treating Hepatitis C infection: Wherein R1, R7 and X are defined in the detailed description.
    Type: Grant
    Filed: November 12, 2014
    Date of Patent: August 23, 2016
    Assignee: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Sung Key Jang, Gyo Chang Keum, Eunice Eun-Kyeong Kim, Soon Bang Kang, Suyeon Yeom, Juhyeon Lee, SeungGi Lee, Hee Sun Kim
  • Publication number: 20150133676
    Abstract: The present disclosure relates to a method for preparing a disubstituted urea and carbamate compounds simultaneously through a one-pot reaction of an amine, carbon dioxide and an alkylene oxide compound in the presence of an ionic liquid-based complex catalyst system containing indium. In accordance with the present disclosure, a disubstituted urea and carbamate compounds can be prepared simultaneously at high yield. In addition, the ionic liquid-based catalyst containing indium according to the present disclosure is economical because it can be reused several times.
    Type: Application
    Filed: December 20, 2013
    Publication date: May 14, 2015
    Applicant: Korea Institute of Industrial Technology
    Inventors: Yong Jin Kim, Vivek Mishra, Guang Meang Son, Jin Ku Cho, Baek Jin Kim
  • Patent number: 9012631
    Abstract: This invention provides 1,3-oxazolidin-2-one compounds of formula I and their salts, their preparation methods, and use in the preparation of linezolid racemate and its optical isomer, which are used as oxazolidinone antibacterial agents. In the formula, R is H, hydroxyl, halogen, C1-C12 alkyl, C1-C12 alkoxy, nitro and carboxyl; and R can be placed at any position on the benzene rings; and the compound is a racemate or an optical isomer.
    Type: Grant
    Filed: August 10, 2011
    Date of Patent: April 21, 2015
    Assignees: Yabang Pharmaceutical Co., Ltd, Jiangsu Yabang Shengyuan Pharmaceutical Co., Ltd, Changzhou Yabang Pharmaceutical Co., Ltd
    Inventors: Si-Qing Wang, Yong Deng, Zai-Xin Chen, Hui Zhang, Zhi-Pei San, Bai-Yang Mao, Zheng-Jun Xia, Long Jiang, Ming-Guang Zhang, Song Lin, Ming-Lin Wang
  • Patent number: 9006453
    Abstract: The present invention provides a convenient and industrially viable process for preparation of Zolmitriptan (I) having desired purity. The invention specifically relates to a method for isolating (S)-4-(4-hydrazinobenzyl)-1,3-oxazolidin-2-one hydrochloride (IIIa) of desired purity by separating the undesired inorganic side products such as stannous hydroxide by manipulation of pH at different stages and finally treating with N,N-dimethylamino butyraldehyde diethyl acetal in an acidic medium to provide Zolmitriptan (I) conforming to regulatory specifications.
    Type: Grant
    Filed: August 27, 2012
    Date of Patent: April 14, 2015
    Assignee: Emcure Pharmaceuticals Limited
    Inventors: Mukund Keshav Gurjar, Neelakandan Kaliaperumal, Pravin Prabhakar Ahirrao, Raghuramireddy Baireddy, Prabhakaran Balasubramanian, Srinivas Nandala, Prasad Pandurang Panchabhai, Samit Satish Mehta
  • Publication number: 20150099696
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed to compounds suitable for the treatment of Disease conditions such as hyperlipidemia.
    Type: Application
    Filed: June 26, 2012
    Publication date: April 9, 2015
    Applicant: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pandya, Sairam V.V.M. Kalapatapu
  • Patent number: 8987256
    Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: March 24, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Friederike Stoll, Stefan Heitmeier, Klaus Münter, Nils Griebenow, Thomas Lampe, Sherif El Sheikh, Volkhart Min-Jian Li
  • Publication number: 20150056164
    Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.
    Type: Application
    Filed: April 24, 2014
    Publication date: February 26, 2015
    Applicant: AbbVie Inc.
    Inventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
  • Publication number: 20150011595
    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: Application
    Filed: May 6, 2014
    Publication date: January 8, 2015
    Applicant: Concert Pharmaceuticals, Inc.
    Inventor: Roger D. Tung
  • Publication number: 20140378474
    Abstract: The invention relates to a compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
    Type: Application
    Filed: January 25, 2013
    Publication date: December 25, 2014
    Applicant: NOVARTIS AG
    Inventors: Stefanie Flohr, Christian Markert, Kenji Namoto, Bernard Pirard
  • Patent number: 8912291
    Abstract: Embodiments include oxazolidone ring containing adducts obtainable by combining an aliphatic epoxy compound, an aromatic epoxy compound, and a diisocyanate. Embodiments further include a curable powder coating composition including a resin component and a hardener component, where the resin component includes the oxazolidone ring containing adduct.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: December 16, 2014
    Assignee: DOW Global Technologies LLC
    Inventors: Joseph Gan, Emile C. Trottier
  • Publication number: 20140350059
    Abstract: The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.
    Type: Application
    Filed: August 13, 2014
    Publication date: November 27, 2014
    Inventors: Jae Keol RHEE, Weon Bin IM, Chong Hwan CHO, Sung Hak CHOI, Tae Ho LEE
  • Publication number: 20140303380
    Abstract: An efficient process is disclosed for producing the compound of formula I, which is the CETP inhibitor anacetrapib, which raises HDL-cholesterol and reduces LDL-cholesterol in human patients and may be effective for treating or reducing the risk of developing atherosclerosis:
    Type: Application
    Filed: October 26, 2012
    Publication date: October 9, 2014
    Inventors: Cheol K. Chung, Guy R. Humphey, Peter E. Maligres, Timothy J. Wright
  • Patent number: 8835426
    Abstract: This invention relates to novel compounds of the Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds of the Formula (I) and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
    Type: Grant
    Filed: February 26, 2008
    Date of Patent: September 16, 2014
    Assignee: Vitae Pharmaceuticals, Inc.
    Inventors: David A. Claremon, Gerard McGeehan, Suresh B. Singh, Colin M. Tice, Yuanjie Ye, Wei Zhao
  • Publication number: 20140256700
    Abstract: The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using said compositions in the treatment of various disorders.
    Type: Application
    Filed: February 26, 2014
    Publication date: September 11, 2014
    Inventors: Michael A. Poss, David R. Tortolani, Dharmpal S. Dodd, Christopher P. Mussari, John S. Tokarski, Ashvinikumar V. Gavai, Yufen Zhao, George V. Delucca, Daniel O'Malley, Derek J. Norris, Patrice Gill, Claude A. Quesnelle, Wen-Ching Han
  • Publication number: 20140228582
    Abstract: The present invention provides a convenient and industrially viable process for preparation of Zolmitriptan (I) having desired purity. The invention specifically relates to a method for isolating (S)-4-(4-hydrazinobenzyl)-1,3-oxazolidin-2-one hydrochloride (IIIa) of desired purity by separating the undesired inorganic side products such as stannous hydroxide by manipulation of pH at different stages and finally treating with N,N-dimethylamino butyraldehyde diethyl acetal in an acidic medium to provide Zolmitriptan (I) conforming to regulatory specifications.
    Type: Application
    Filed: August 27, 2012
    Publication date: August 14, 2014
    Applicant: EMCURE PHARMACEUTICALS LIMITED
    Inventors: Mukund Keshav Gurjar, Neelakandan Kaliaperumal, Pravin Prabhakar Ahirrao, Raghuramireddy Baireddy, Prabhakaran Balasubramanian, Srinivas Nandala, Prasad Pandurang Panchabhai, Samit Satish Mehta
  • Publication number: 20140221383
    Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
    Type: Application
    Filed: April 14, 2014
    Publication date: August 7, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Hallet, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
  • Publication number: 20140213620
    Abstract: In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.
    Type: Application
    Filed: July 17, 2013
    Publication date: July 31, 2014
    Inventors: James Elliot Bradner, Ralph Mazitschek
  • 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
  • Publication number: 20140171640
    Abstract: This invention provides 1,3-oxazolidin-2-one compounds of formula I and their salts, their preparation methods, and use in the preparation of linezolid racemate and its optical isomer, which are used as oxazolidinone antibacterial agents. In the formula, R is H, hydroxyl, halogen, C1-C12 alkyl, C1-C12 alkoxy, nitro and carboxyl; and R can be placed at any position on the benzene rings; and the compound is a racemate or an optical isomer.
    Type: Application
    Filed: August 10, 2011
    Publication date: June 19, 2014
    Applicants: Yabang Pharmaceutical Co., Ltd, Changzhou Yabang Pharmaceutical Co., Ltd., Jiangsu Yabang Shengyuan Pharmaceutical Co., Ltd.
    Inventors: Si-Qing Wang, Yong Deng, Zai-Xin Chen, Hui Zhang, Zhi-Pei San, Bai-Yang Mao, Zheng-Jun Xia, Long Jiang, Ming-Guang Zhang, Song Lin, Ming-Lin Wang
  • Patent number: 8735435
    Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
    Type: Grant
    Filed: November 25, 2009
    Date of Patent: May 27, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Hallett, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith
  • Patent number: 8729112
    Abstract: This application describes compounds useful as anti-microbial agents, including as antibacterial, disinfectant, antifungal, germicidal or antiviral agents.
    Type: Grant
    Filed: November 14, 2012
    Date of Patent: May 20, 2014
    Assignee: Novabay Pharmaceuticals, Inc.
    Inventors: Timothy Shiau, Charles Francavilla, Eddy Low, Eric Douglas Turtle, Donogh John Roger O'Mahony, Rakesh K. Jain
  • Publication number: 20140135368
    Abstract: The present invention relates to the field of organic chemistry, more specifically to the synthesis of intermediate compounds which can be used in the synthesis of pharmaceutically active agents such as anacetrapib or derivatives thereof.
    Type: Application
    Filed: December 21, 2011
    Publication date: May 15, 2014
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Jan Humljan, Nenad Maras
  • Patent number: 8722715
    Abstract: The present application relates to N-chlorinated oxazolidinone, hydantoin and imidazolidinone compounds of Formula I or pharmaceutically acceptable salts thereof, and associated compositions and methods of use as antimicrobial agents.
    Type: Grant
    Filed: November 4, 2009
    Date of Patent: May 13, 2014
    Assignee: NovaBay Pharmaceuticals
    Inventors: Rakesh K. Jain, Eddy Low, Charles Francavilla, Timothy P. Shiau, Bum Kim, Satheesh K. Nair
  • Patent number: 8703963
    Abstract: This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against Staphylococcus spp., including methicillin resistant Staphylcoccus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.
    Type: Grant
    Filed: February 8, 2008
    Date of Patent: April 22, 2014
    Assignee: University of South Florida
    Inventors: Edward Turos, Rajesh Kumar Mishra, Kevin Revell
  • Publication number: 20140094480
    Abstract: This invention relates generally to stimulating neurogenesis (e.g., post-natal neurogenesis, e.g., post-natal hippocampal neurogenesis) and protection from neuron cell death.
    Type: Application
    Filed: December 9, 2013
    Publication date: April 3, 2014
    Applicant: Board of Regents of The University of Texas System
    Inventors: Steven L. McKnight, Joseph M. Ready, Andrew A. Pieper, Jef K. De Brabander
  • Publication number: 20140065095
    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: Application
    Filed: June 5, 2013
    Publication date: March 6, 2014
    Inventors: Ulrich Heiser, Daniel Ramsbeck, Robert Sommer, Antje Meyer, Torsten Hoffmann, Livia Boehme, Hans-Ulrich Demuth
  • Publication number: 20130324739
    Abstract: An object of the present invention is to provide crystal polymorphs which have a high bulk density and are excellent in storage stability, among crystal polymorphs of a glutamic acid benzyl ester N-carboxylic anhydride. According to the present invention, the crystal polymorphs of glutamic acid benzyl ester N-carboxylic anhydride that have a bulk density of 0.45 g/cm3 or higher can be obtained by dissolving glutamic acid benzyl ester N-carboxylic anhydride in a solvent which has been heated at a temperature equal to or higher than 40° C. and lower than a boiling point thereof and is in an amount of 0.5 L or more per mol of the glutamic acid benzyl ester N-carboxylic anhydride, adding a poor solvent which is in an amount of 1.4 L or more per mol of the glutamic acid benzyl ester N-carboxylic anhydride at a temperature equal to or higher than 40° C. and lower than a boiling point thereof, precipitating crystals at a temperature equal to or higher than 40° C.
    Type: Application
    Filed: March 19, 2012
    Publication date: December 5, 2013
    Applicant: NIPPON SODA CO., LTD.
    Inventors: Hiroshi Sumiya, Junji Ipposhi
  • Publication number: 20130281366
    Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as Hyperlipidemia and also have a beneficial effect on cholesterol.
    Type: Application
    Filed: December 26, 2011
    Publication date: October 24, 2013
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Harikishore Pingali, Pankaj Makadia, Vrajesh Pankaj, Sairam Kalapatapu, V.V.M., Mukul R. JAIN
  • Publication number: 20130261130
    Abstract: The invention relates to acylamino-phthalic acid amides and related compounds of formula (I) wherein A is —CON—R3R4, —NR5COR6, —NHR7, —OR8, —SR9, —CH2NR10R11, —(CH2)2-R12, —CH?CH—R12, —C?C—R12, optionally substituted phenyl, optionally substituted thiophenyl, or optionally substituted 1,2,3-triazol-4-yl, W is hydrogen, hydroxy or carboxymethoxy, Y is carboxy, methoxycarbonyl or 2H-tetrazol-5-yl, and the various substituents R have the meanings indicated in the description. These compounds are useful for the treatment and/or prophylaxis of skeletal muscle atrophy, schizophrenia and Alzheimer's disease, and as cognitive enhancers.
    Type: Application
    Filed: October 31, 2011
    Publication date: October 3, 2013
    Inventors: Shaheen Ahmed, Stefan Hettwer, Jan Willem Vrijbloed, Carlo Farina, Hans Allgeier
  • Publication number: 20130210769
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).
    Type: Application
    Filed: March 15, 2013
    Publication date: August 15, 2013
    Applicant: IRM LLC
    Inventors: Hong Liu, Xiaohui He, Dean Paul Phillips, Xuefeng Zhu, Kunyong Yang, Thomas Lau, Baogen Wu, Yongping Xie, Truc Ngoc Nguyen, Xing Wang
  • Patent number: 8507521
    Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: August 13, 2013
    Assignee: Merck Sharp + Dohme B.V.
    Inventors: Julia Adam, Jonathan Gillespie, Steven Laats, John Kinnaird Ferguson MacLean, Duncan Robert McArthur
  • Publication number: 20130197226
    Abstract: The present invention features pharmaceutical compositions and methods of using the pharmaceutical compositions for treating left ventricular diastolic dysfunction. In particular, the pharmaceutical compositions include an apolipoprotein complex comprising a lipid fraction and a protein fraction.
    Type: Application
    Filed: July 19, 2011
    Publication date: August 1, 2013
    Inventors: Jean-Claude Tardif, David Busseuil, Éric Rhéaume
  • Patent number: 8497381
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the antagonists of PGD2 receptors described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Grant
    Filed: February 25, 2009
    Date of Patent: July 30, 2013
    Assignee: Panmira Pharmaceuticals, LLC
    Inventors: John Howard Hutchinson, Brian Andrew Stearns, Thomas Jonathan Seiders, Jill Melissa Scott, Jeannie M. Arruda, Bowei Wang
  • Publication number: 20130078170
    Abstract: An ionic liquid composition having the following chemical structural formula: wherein R1, R2, R3, and R4 are independently selected from hydrocarbon groups containing at least 1 and up to 20 carbon atoms, and X? is a cyclic anion that possesses a negatively-charged group reactive with a gaseous electrophilic species, particularly carbon dioxide or sulfur dioxide. Methods for capturing a gaseous electrophilic species, such as CO2 or SO2, by contacting the gaseous electrophilic species with an ionic liquid according to Formula (1) are also described.
    Type: Application
    Filed: September 22, 2011
    Publication date: March 28, 2013
    Applicant: UT BATTELLE
    Inventors: Sheng Dai, Congmin Wang, Huimin Luo, De-en Jiang
  • Publication number: 20130072490
    Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
    Type: Application
    Filed: September 29, 2010
    Publication date: March 21, 2013
    Applicant: Amira Pharmaceuticals INC.
    Inventors: Ryan Clark, Brian Andrew Stearns, Jill Melissa Scott, Heather Renee Coate, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie Arruda, Nicholas Simon Stock, Yen Pham Truong, David Nathan Zalatan
  • Patent number: 8383622
    Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein Ring A is a group represented by the formula: Ring B is optionally substituted heteroaryl, provided that optionally substituted isoxazole is excluded, or optionally substituted heterocycle, R1 is hydrogen or optionally substituted alkyl, R2 is —OR5, —SR5, halogen, halogenated alkyl or the like, R3 is optionally substituted alkyl or the like, R4 is optionally substituted alkyl or the like, R5 is optionally substituted alkyl or the like, R6 is hydrogen or the like, R7 and R8 are each independently hydrogen or the like, R10 and R11 are each independently hydrogen or the like, R12 is optionally substituted alkyl or the like, m and p are each independently integer of 1 to 3.
    Type: Grant
    Filed: May 7, 2008
    Date of Patent: February 26, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventors: Koji Masuda, Tomoyuki Ogawa, Takuji Nakatani
  • Publication number: 20130040977
    Abstract: This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like.
    Type: Application
    Filed: August 24, 2012
    Publication date: February 14, 2013
    Inventors: Steven L. McKnight, Andrew A. Pieper, Joseph M. Ready, Jef K. De Brabander
  • Patent number: 8324398
    Abstract: The present invention relates to processes for the preparation of biaryl oxazolidinones. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.
    Type: Grant
    Filed: July 28, 2004
    Date of Patent: December 4, 2012
    Assignee: Rib-X Pharmaceuticals, Inc.
    Inventors: Yusheng Wu, Shili Chen, Yi Chen, Roger Hanselmann, Rongliang Lou, Jiacheng Zhou
  • Publication number: 20120220622
    Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.
    Type: Application
    Filed: November 2, 2010
    Publication date: August 30, 2012
    Inventors: Julia Adam, Jonathan Gillespie, Steven Laats, John Kinnaird Ferguson MacLean, Duncan Robert McArthur
  • Patent number: 8216973
    Abstract: The invention relates to 2-[(1H-pyrazol-4-ylmethyl)-sulfonyl]-oxazole derivatives, chiral 2-[(1H-pyrazol-4-ylmethyl)-sulfinyl]-oxazole derivatives, and 2-[(1H-pyrazol-4-ylmethyl)-sulfanyl]-oxazole derivatives of general formula (I) and the salts thereof, methods for the production thereof, and the use thereof as herbicides and plant growth regulators, in particular as herbicides for selectively controlling weeds in plant crops.
    Type: Grant
    Filed: April 15, 2009
    Date of Patent: July 10, 2012
    Assignee: Bayer Cropscience AG
    Inventors: Heinz Kehne, Hansjorg Dietrich, Dieter Feucht, Dirk Schmutzler, Isolde Hauser-Hahn, Christian Paulitz, Jan Dittgen, Arianna Marteletti, Christopher Hugh Rosinger
  • Patent number: 8202895
    Abstract: The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders.
    Type: Grant
    Filed: March 18, 2010
    Date of Patent: June 19, 2012
    Assignee: Bayer Pharma Aktiengesellschaft
    Inventors: Ulf Brüggemeier, Chantal Fürstner, Volker Geiβ, Joerg Keldenich, Armin Kern, Martina Delbeck, Peter Kolkhof, Axel Kretschmer, Elisabeth Pook, Carsten Schmeck, Hubert Trübel
  • Publication number: 20120149911
    Abstract: This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against Staphylococcus spp., including methicillin resistant Staphylcoccus aureus (MRSA), and Bacillus spp., including Bacillus anthracis.
    Type: Application
    Filed: February 8, 2008
    Publication date: June 14, 2012
    Applicant: UNIVERSITY OF SOUTH FLORIDA
    Inventors: Edward Turos, Rajesh Kumar Mishra
  • Patent number: 8198483
    Abstract: (1R)-2-[(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)amino]-1-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)ethanol and (5R)-3-(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)-5-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)-1,3-oxazolidin-2-one are claimed.
    Type: Grant
    Filed: June 21, 2011
    Date of Patent: June 12, 2012
    Assignee: Glaxo Group Limited
    Inventors: Philip Charles Box, Diane Mary Coe, Brian Edgar Looker, Inderjit Singh Mann, Panayiotis Alexandrou Procopiou
  • Publication number: 20120129046
    Abstract: A nonaqueous secondary battery, comprising: a positive electrode; a negative electrode; and a nonaqueous electrolyte solution, the nonaqueous electrolyte solution containing at least a cyclic compound having, in the molecule, a functional group having an ester bond to which a nitrogen atom is attached, in which is the general formula (I).
    Type: Application
    Filed: November 16, 2011
    Publication date: May 24, 2012
    Inventor: Hisayuki UTSUMI
  • Patent number: 8178665
    Abstract: A process for the production of 1-(4-3(R)-[3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) according to the following reaction scheme: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), (X), (XI) where the substances of the general Formulas II, IV, VI, VIII, IX, X and XI are new, Formula III is a non-isolated intermediate, R1, R2 and R3 are represented by the compounds of Formulas Va-Vd, (Va), (Vb), (Vc), (Vd) and R4 is a silyl, e.g., tert-butyl-dimethyl-silyl, tert-butyl-diphenyl-silyl group.
    Type: Grant
    Filed: December 18, 2006
    Date of Patent: May 15, 2012
    Assignee: Richter Gedeon Nyrt.
    Inventors: József Bódi, János Éles, Katalin Szöke, Krisztina Vukics, Tamás Gáti, Krisztina Temesvári, Dorottya Kiss-Bartos
  • Patent number: 8163793
    Abstract: The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: April 24, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Rubén Alvarez Sánchez, David Banner, Simona M. Ceccarelli, Uwe Grether, Wolfgang Haap, Peter Hartman, Guido Hartmann, Hans Hilpert, Holger Kuehne, Harald Mauser, Jean-Marc Plancher
  • Patent number: 8148363
    Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.
    Type: Grant
    Filed: May 18, 2009
    Date of Patent: April 3, 2012
    Assignee: Schering Corporation
    Inventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick, Liyuan Wang, Xiaobang Gao
  • Patent number: 8143417
    Abstract: In the preparation of zolmitriptan of formula III the reduction of the diazonium salt to (5)-4-(4-hydrazinobenzyl)-1,3-oxazolidin-2-one of formula IV is performed in a more concentrated mixture and by the effect on an alkali metal disulphite, preferably sodium disulphite. A zolmitriptan toluene solvate, characterized by a toluene content of 9 to 14% by weight according to the gas chromatography determination and by a maximum of the corresponding mass loss at temperatures of about 111° C. in the gravimetric analysis record. A zolmitriptan toluene solvate, showing strong Raman bands at the wave numbers of 1443 and 1354 cm?1, characteristic for the crystal lattice of zolmitriptan with built-in toluene, and further marked bands at 1004 and 786 cm?1, characteristic for toluene.
    Type: Grant
    Filed: February 25, 2008
    Date of Patent: March 27, 2012
    Assignee: Zentiva k.s.
    Inventors: Michal Voslar, Monika Zatopkova, Ludek Ridvan, Tomas Pekarek