The Five-membered Hetero Ring Has At Least Oxygen And Nitrogen As Ring Hetero Atoms Patents (Class 544/137)
  • Patent number: 11524002
    Abstract: The present invention is a method of treating or preventing Mycobacterium tuberculosis infection in a subject by administering to the subject an effective amount of oxazolidinone, specifically (N—(((S)-3-(dibenzo[b,e][1,4]dioxin-7-yl)-2-oxooxazolidin-5-yl)methyl)acetamide) or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof.
    Type: Grant
    Filed: May 20, 2021
    Date of Patent: December 13, 2022
    Assignees: The Johns Hopkins University, University of St. Thomas
    Inventors: Gyanu Lamichhane, J. Thomas Ippoliti
  • Patent number: 11472781
    Abstract: The present disclosure is concerned with 2-aminoaryl-5-aryloxazole compounds that are capable of activating NF-?B signaling. The present disclosure is also concerned with methods of using these compounds for the treatment of neurological disorders such as, for example, amyotrophic lateral sclerosis (ALS), Alzheimer's disease, Parkinson's disease, spinal muscular atrophy, traumatic brain injury, vascular dementia, Huntington's disease, mental retardation, and attention deficit and hyperactivity disorder (ADHD), and neuromuscular disorders such as, for example, Duchenne muscular dystrophy (DMD). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: February 20, 2019
    Date of Patent: October 18, 2022
    Assignee: SOUTHERN RESEARCH INSTITUTE
    Inventors: Mark J. Suto, Bini Mathew, Rita Cowell, Corinne E. Augelli-Szafran
  • Patent number: 11471417
    Abstract: Compounds, compositions, methods, and uses are described for therapeutic deuterated N,N-dimethyltryptamine compounds (e.g., a single compound or a plurality of deuterated N,N-dimethyltryptamine compounds) such as N,N-dimethyltryptamine compounds, ?-protio, ?-deutero-N,N-dimethyltryptamine compounds, ?,?-dideutero-N,N-dimethyltryptamine compounds, and pharmaceutically acceptable salts of these compounds. The deuterated N,N-dimethyltryptamine compound may have an increased half-life compared with the half-life of undeuterated N,N-dimethyltryptamine. For example, a deuterated N,N-dimethyltryptamine compound may be used in therapy and have a Formula (I): wherein: the ratio of deuterium:protium in the compound is greater than that found naturally in hydrogen; each R1 is independently selected from H and D; R2 is selected from CH3 and CD3; R3 is selected from CH3 and CD3; each yH is independently selected from H and D, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: August 26, 2021
    Date of Patent: October 18, 2022
    Assignee: Small Pharma Ltd
    Inventors: Peter Rands, Tiffanie Benway, Zelah Joel, Marie Layzell, Ellen James
  • Patent number: 10112921
    Abstract: The invention discloses a method for the preparation of thiophene-2-carbonyl chlorides starting from thiophenes with oxalyl chloride at elevated temperature with short reaction time.
    Type: Grant
    Filed: November 2, 2016
    Date of Patent: October 30, 2018
    Assignee: LONZA LTD
    Inventors: Daniel Zollinger, Florencio Zaragoza Doerwald
  • Patent number: 9567307
    Abstract: Embodiments of the invention provide methods and materials for chemical cross-coupling reactions that utilize aryl alcohol derivatives as cross-coupling partners. Embodiments of the invention include methods for the amination of aryl sulfamates and carbamates, which are attractive cross-coupling partners, particularly for use in multistep synthesis. Illustrative embodiments include versatile means to use simple derivatives of phenol as precursors to polysubstituted aryl amines, as exemplified by a concise synthesis of the antibacterial drug linezolid.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: February 14, 2017
    Assignee: The Regents of the University of California
    Inventors: Neil K. Garg, Stephen D. Ramgren, Amanda L. Silberstein, Kyle W. Quasdorf
  • Patent number: 9533962
    Abstract: In one aspect, the invention relates to a compound of the structure: or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.
    Type: Grant
    Filed: February 12, 2016
    Date of Patent: January 3, 2017
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Melissa Fleury, Adam D. Hughes, Anne-Marie Beausoleil, Erik Fenster, Venkat R. Thalladi, Miroslav Rapta
  • Patent number: 9161924
    Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Grant
    Filed: July 3, 2012
    Date of Patent: October 20, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig Boyle, William Greenlee, Samuel Chackalamannil, Claire Lankin
  • Publication number: 20150133657
    Abstract: The present invention provides processes for the preparation of rivaroxaban. The present invention also provides an intermediate for the preparation of rivaroxaban.
    Type: Application
    Filed: May 23, 2013
    Publication date: May 14, 2015
    Inventors: Pankaj Kumar Singh, Mukesh Kumar Sharma, Chandra Has Khanduri
  • Publication number: 20150133451
    Abstract: The present invention provides a heterocyclic compound having an IRAK-4 inhibitory action, which is useful for the prophylaxis or treatment of inflammatory disease, autoimmune disease, osteoarticular degenerative disease, neoplastic disease and the like, and a medicament containing thereof. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 14, 2015
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Masato Yoshida, Kazuaki TAKAMI, Yusuke TOMINARI, Zenyu SHIOKAWA, Akito SHIBUYA, Yusuke SASAKI, Tony GIBSON, Terufumi TAKAGI
  • Publication number: 20150126733
    Abstract: The present inventors have surprisingly found that rivaroxaban of formula I can be prepared in a one-pot process, in high purity and with high yield, by reacting 5-chlorothiophene-2-carboxylic acid or a salt thereof with a sulfonylating agent to produce a sulfonyl ester intermediate, which is then condensed with 4-[4-[(SS)-5-(aminomethyl)-2-oxo-1,3-oxazolidin-3-yl]phenyl]morjJholine-3-one or an acid addition salt thereof to produce rivaroxaban.
    Type: Application
    Filed: May 2, 2012
    Publication date: May 7, 2015
    Applicant: SYMED LABS LIMITED
    Inventors: Mohan Rao Dodda, Venkat Reddy Buthukuri
  • Publication number: 20150119376
    Abstract: The present invention relates to cycloalkenyl aryl derivatives, isomers thereof, pharmaceutically acceptable salts thereof, hydrates thereof, or solvates thereof; a method for preparing the derivatives; and pharmaceutical compositions containing the same. The compounds of the present invention show the effect of CETP activity inhibition. It means that the compounds can increase HDL-cholesterol and decrease LDL-cholesterol.
    Type: Application
    Filed: April 12, 2012
    Publication date: April 30, 2015
    Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: SeoHee LEE, JungTaek OH, JaeKwang LEE, JaeWon LEE, Suyeal BAE, Nina HA, Sera LEE
  • Publication number: 20150119571
    Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
    Type: Application
    Filed: September 4, 2014
    Publication date: April 30, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Adam D. Hughes, Melissa Fleury
  • 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: 9006276
    Abstract: The invention relates to novel oxindole derivatives of general formula (I), wherein the substituents R1, R2, A, B, and Y are defined as in claim 1. The invention further relates to medicaments containing said derivatives, and use thereof for the prevention and/or treatment of vasopressin-dependent diseases.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: April 14, 2015
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Thorsten Oost, Wilfried Lubisch, Wolfgang Wernet, Wilfried Hornberger, Liliane Unger, Herve Geneste, Astrid Netz
  • Publication number: 20150099719
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Application
    Filed: October 6, 2014
    Publication date: April 9, 2015
    Inventors: Shawn Stachel, Daniel V. Paone, Jing Li, Kausik Nanda
  • Publication number: 20150099714
    Abstract: The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 9, 2015
    Inventors: Julie F. Liu, Xuejun Tang, Scott L. Harbeson, Craig E. Masse
  • Patent number: 8993556
    Abstract: The present invention relates to substituted resorcinol derivatives which inhibit the activity of Heat Shock Protein HSP90. The compounds of the invention are therefore useful in treating proliferative diseases such as cancer and neurodegenerative diseases. The present invention also provides processes for preparing these compounds, pharmaceutical compositions comprising them, methods of treating diseases and the pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: March 31, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Maria Gabriella Brasca, Elena Casale, Ron Ferguson, Paolo Polucci, Fabio Zuccotto
  • Publication number: 20150079519
    Abstract: A photosensitive compound represented by formula (1) or formula (2). (Chemical formula 1) (In formula (1) and formula (2), n is an integer of 1-3; R1 is a linear or branched alkyl group having 1-6 carbon atoms or an alkylene group having 2-6 carbon atoms formed from two R1 together; R2 is —NR3R4; R3 and R4 are each independently a linear or branched alkyl group or alkenyl group having 1-6 carbon atoms, a linear or branched alkylene group having 2-6 carbon atoms formed by R3 and R4 together, or a linear or branched alkylene group or alkenylene group having 3-8 carbon atoms optionally containing an oxygen atom or nitrogen atom.
    Type: Application
    Filed: February 28, 2013
    Publication date: March 19, 2015
    Inventor: Toru Shibuya
  • Publication number: 20150080382
    Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.
    Type: Application
    Filed: June 24, 2014
    Publication date: March 19, 2015
    Inventors: Damian O. Arnaiz, Greg Brown, Emmanuel Claret, Arwed Cleve, David Davey, William Guilford, Seock-Kyu Khim, Thomas Kirkland, Monica J. Kochanny, Amy Liang, David Light, John Parkinson, Guo Ping Wei, Bin Ye
  • Publication number: 20150080570
    Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.
    Type: Application
    Filed: April 11, 2014
    Publication date: March 19, 2015
    Applicants: Coferon, Inc., Cornell University
    Inventors: Lee Daniel Arnold, Maneesh Pingle
  • Patent number: 8980892
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.
    Type: Grant
    Filed: February 18, 2010
    Date of Patent: March 17, 2015
    Assignees: Syngenta Crop Protection LLC, Syngenta Limited
    Inventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
  • Patent number: 8975254
    Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: October 27, 2010
    Date of Patent: March 10, 2015
    Assignee: Orion Corporation
    Inventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, Iisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
  • Publication number: 20150057282
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 26, 2015
    Applicant: SAREUM LIMITED
    Inventors: John Charles READER, John Mark ELLARD, Helen BOFFEY, Susanne TAYLOR, Andrew David CARR, Michael CHERRY, Michelle WILSON, Richard Boakye OWOARE
  • Patent number: 8962827
    Abstract: Provided are a linezolid intermediate and the preparation method thereof and a method for synthesizing linezolid. The structure of the intermediate is shown as formula F2, wherein the compound is prepared by a condensation reaction of (S)—N-(3-chloro-2-hydroxy-1-propyl) acetamide and the compound shown in formula F4. In the preparation methods of the compound shown in formula F2 and linezolid, the reaction system is mild, side reactions are few and the product yield is high.
    Type: Grant
    Filed: April 12, 2012
    Date of Patent: February 24, 2015
    Assignee: Zhejiang Medicine Co. Ltd. Xinchang Pharmaceutical Factory
    Inventors: Xiaoyue Jiang, Guofeng Wu, Weidong Ye, Runpu Shen, Xiaohua Song
  • Patent number: 8957063
    Abstract: Compounds which modulate the CB2 receptor are disclosed. The compounds are useful for treating CB2 receptor-mediated diseases such as pain.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: February 17, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Monika Ermann, Innocent Mushi
  • Publication number: 20150045359
    Abstract: The present invention relates to compounds of formula wherein R1 and R2 are as described herein. Compounds of the invention are useful in the treatment and/or prophylaxis of diseases associated with TAAR modulation.
    Type: Application
    Filed: January 8, 2013
    Publication date: February 12, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Guido Galley, Annick Goergler, Roger Norcross, Philippe Pflieger
  • Publication number: 20150038704
    Abstract: A method for preparing a Rivaroxaban intermediate I is presented, including the following step: in a non-protonic solvent, under the effect of lewis acid, performing cyclization reaction on 4-(4-phenyl isocyanate)morpholine-3-ketone (II) and (S)-epoxy compound (III), the reaction temperature ranging from 20° C. to 60° C., where R is amino replaced by amino protecting group. The preparation method of the present invention has a mild condition, a simple process, a low cost, and high efficiency; the product is easy to purify and the method is applicable to industrial production.
    Type: Application
    Filed: February 22, 2013
    Publication date: February 5, 2015
    Applicants: China National Medicines Guorui Pharmaceutical Co., Shanghai Institute of Pharmaceutical Industry
    Inventors: Fuli Zhang, Bin Liang, Chunbo Yang, Chonghao Liu, Yang Gao, Jian Wang, Min Jiang
  • Publication number: 20150025236
    Abstract: The invention relates to a substantially pure linezolid hydroxide having R-isomer content more than about 99.9% relative to its S-isomer. Further aspect of invention provides the ambient moisture condition, which is critical for enantiomeric pure linezolid hydroxide. The obtained substantially enantiomerically pure linezolid hydroxide compound of formula-II can be subsequently converted into the linezolid compound of formula-I, having S-isomer content more than 99.9% relative to R-isomer. Further the invention provides an improved process for preparation of enantiomeric pure linezolid Form-I, wherein linezolid Form-I having the purity more than 99.9% relative to any other known polymorphic form of linezolid. The obtained enantiomeric pure linezolid Form-I can be subsequently converted into the other known polymorphic forms linezolid. The invention also provides stable and substantially solvent-free crystal of Form-I of linezolid.
    Type: Application
    Filed: January 22, 2013
    Publication date: January 22, 2015
    Inventors: Sujay Biswas, Atulya Kumar Panda, Ashish Kumar Gupta, Shishupal Singh, Praveen Tiwari, Dharam Vir, Saji Thomas
  • Publication number: 20150011756
    Abstract: An improved process for the preparation of Rivaroxaban wherein the process substantially eliminates the potential impurities. process for preparation of Rivaroxaban which uses a novel intermediate. A process for preparing the novel intermediate which is used for the preparation of Rivaroxaban.
    Type: Application
    Filed: February 5, 2013
    Publication date: January 8, 2015
    Inventors: Vijayavitthal Thippannachar Mathad, Nilesh Sudhir Patil, Navnath Chintaman Niphade, Anil Chaturlal Mali, Mahendra Bhagirath Bodake, Sharad Subhash Ippar, Rajesh Talla
  • Publication number: 20150011757
    Abstract: Disclosed is a new method for preparing a methyl substitute of a linezolid intermediate, (S)-2-(3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazoline) (I), wherein the intermediate (I) is obtained by the cyclization of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III). This process has a short process route, low cost, easy operation, and high yield, so is suitable for a large-scale industrial production.
    Type: Application
    Filed: February 8, 2013
    Publication date: January 8, 2015
    Applicants: Zhejiang Hisun Pharmaceutical Co., Ltd., Shanghai Institute of Pharmaceutical Industry
    Inventors: Fuli Zhang, Chunbo Yang, Bin Liang, Pengcheng Qiu, Hairong Luo, Jiang Li, Jian Chai, Qingfeng Cai
  • Patent number: 8921544
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Grant
    Filed: June 3, 2014
    Date of Patent: December 30, 2014
    Assignee: Sareum Limited
    Inventors: John Charles Reader, John Mark Ellard, Helen Boffey, Susanne Taylor, Andrew David Carr, Michael Cherry, Michelle Wilson, Richard Boakye Owoare
  • Publication number: 20140378682
    Abstract: The invention discloses processes for the preparation of rivaroxaban and its pharmaceutically acceptable salts, solvates, and hydrates thereof. The invention also relates to novel intermediates for the preparation of rivaroxaban.
    Type: Application
    Filed: September 10, 2012
    Publication date: December 25, 2014
    Applicant: CADILA HEALTHCARE LIMITED
    Inventors: Shriprakash Dhar Dwivedi, Ashok Prasad, Daya Ram Pal, Mukul Hari Prasad Sharma, Kuldeep Natwarlal Jain, Naitik Bharatbhai Patel
  • Publication number: 20140356322
    Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.
    Type: Application
    Filed: January 11, 2013
    Publication date: December 4, 2014
    Inventors: Craig M. Crews, Dennis Buckley, Alessio Ciulli, William Jorgensen, Peter C. Gareiss, Inge Van Molle, Jeffrey Gustafson, Hyun-Seop Tae, Julien Michel, Dentin Wade Hoyer, Anke G. Roth, John David Harling, Ian Edward David Smith, Afjal Hussain Miah, Sebastien Andre Campos, Joelle Le
  • Publication number: 20140336190
    Abstract: This application relates to chemical compounds which may act as inhibitors of; or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2, R2b, R3, R4a, R4b, and R5 are described herein.
    Type: Application
    Filed: May 8, 2014
    Publication date: November 13, 2014
    Applicant: Gilead Sciences, Inc.
    Inventors: Evangelos Aktoudianakis, Gregory Chin, Britton Kenneth Corkey, Jinfa Du, Kristyna Elbel, Robert H. Jiang, Tetsuya Kobayashi, Rick Lee, Ruben Martinez, Samuel E. Metobo, Michael Mish, Manuel Munoz, Sophie Shevick, David Sperandio, Hai Yang, Jeff Zablocki
  • Publication number: 20140315881
    Abstract: The present invention relates to novel retinoid-related orphan receptor gamma (ROR?) modulators and their use in the treatment of diseases mediated by ROR?.
    Type: Application
    Filed: July 27, 2012
    Publication date: October 23, 2014
    Inventors: Erkan Baloglu, Gary J. Bohnert, Shomir GHOSH, Mercedes Lobera, Darby R. Schmidt, Leonard Sung
  • Publication number: 20140296229
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4, A1 and A2 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Application
    Filed: March 26, 2014
    Publication date: October 2, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Harald ENGELHARDT, Davide GIANNI, Andreas MANTOULIDIS, Christian SMETHURST
  • Patent number: 8846947
    Abstract: Provided herein are sirtuin-modulating compounds of formula (II). The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders relating to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: September 30, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
  • Publication number: 20140275041
    Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicant: Sareum Limited
    Inventors: John Charles READER, John Mark ELLARD, Helen BOFFEY, Susanne TAYLOR, Andrew David CARR, Michael CHERRY, Michelle WILSON, Richard Boakye OWOARE
  • Publication number: 20140256723
    Abstract: The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof that are aldosterone receptor antagonists which might be useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula (I), to their possible use for the treatment of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I).
    Type: Application
    Filed: October 8, 2012
    Publication date: September 11, 2014
    Inventors: Hong Shen, Christine Yang, Jason M. Cox, Kun Liu
  • Publication number: 20140256721
    Abstract: The present invention is directed to novel polymorphs and salts of a compound which is an inhibitor of kinase activity.
    Type: Application
    Filed: April 14, 2014
    Publication date: September 11, 2014
    Applicant: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Charlotte Jane Mitchell, Nigel James Parr, Robert David Willacy
  • Publication number: 20140256658
    Abstract: The present invention describes antibiotic conjugates. These single drug entities are formed connecting one antibiotic with another antibiotic. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs.
    Type: Application
    Filed: March 6, 2014
    Publication date: September 11, 2014
    Applicant: Allergan, Inc.
    Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, LIMING WANG, MICHAEL E. GARST, MAYSSA ATTAR, BRANDON D. SWIFT
  • 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
  • Patent number: 8828992
    Abstract: Provided are a substituted azole derivative and pharmaceutically acceptable salts thereof, a pharmaceutical composition including an effective amount of the derivative, and a method for treating Parkinson's disease in a mammal including administering an effective amount of the compound to the mammal. The azole derivative of the following Formula (I) and pharmaceutically useful salts thereof have an efficacy against Parkinson's disease from inhibitory effects of the activity of MAO-B.
    Type: Grant
    Filed: February 25, 2010
    Date of Patent: September 9, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Cheol-Hyoung Park, Hye-Kyung Min, Mi-Jung Lim, Ji-Won Lee, Jin-Yong Chung, Choon-Ho Ryu, Yeo-Jin Yoon, Mi-Kyung Ji, Joo-Young Park
  • Patent number: 8822466
    Abstract: The invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.
    Type: Grant
    Filed: March 9, 2012
    Date of Patent: September 2, 2014
    Assignee: Novartis AG
    Inventors: Noëlle Gauvry, Steve Nanchen
  • Publication number: 20140219989
    Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Application
    Filed: July 3, 2012
    Publication date: August 7, 2014
    Inventors: Craig Boyle, William Greenlee, Samuel Chackalamannil, Claire Lankin
  • Patent number: 8796267
    Abstract: This invention relates to novel N-[[3-[3-Fluoro-4-(4-morpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]-acetamide derivatives, their acceptable acid addition salts, solvates and hydrates. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by antimicrobial agents.
    Type: Grant
    Filed: June 17, 2008
    Date of Patent: August 5, 2014
    Assignee: Concert Pharmaceuticals, Inc.
    Inventors: Roger Tung, Scott Harbeson
  • Publication number: 20140213784
    Abstract: The present invention relates to methods for the preparation of a compound having the formula (X). Individual reaction steps as well as intermediates are additionally claimed.
    Type: Application
    Filed: April 11, 2012
    Publication date: July 31, 2014
    Applicant: SANDOZ AG
    Inventors: Hubert Sturm, Kerstin Knepper
  • Publication number: 20140206651
    Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II): and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L1-L4, A, B, R1-R4, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.
    Type: Application
    Filed: March 24, 2014
    Publication date: July 24, 2014
    Applicant: Pfizer Inc.
    Inventors: Matthew Frank Brown, Charles Francis Donovan, Edmund Lee Ellsworth, Denton Wade Hoyer, Timothy Allan Johnson, Manjinder Singh Lall, Chris Limberakis, Sean Timothy Murphy, Debra Ann Sherry, Clarke Bentley Taylor, Joseph Scott Warmus
  • Publication number: 20140194426
    Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: October 24, 2013
    Publication date: July 10, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Paul R. Fatheree, Ryan Hudson, Robert Murray McKinnell
  • Patent number: RE47606
    Abstract: The present invention relates to an improved process for the preparation of Linezolid. More specifically, the present invention relates to an improved process for preparing (S)—N-[[3-[3-fluoro-4-[4-morpholinyl]phenyl]-2-oxo-5-oxazolidinyl]methyl] phthalimide and (S)-glycidyl phthalimide intermediates, which are used in the preparation of Linezolid.
    Type: Grant
    Filed: August 30, 2018
    Date of Patent: September 17, 2019
    Assignee: OPTIMUS DRUGS PRIVATE LIMITED
    Inventors: Srinivas Reddy Desi Reddy, Subba Reddy Peketi, Dnyandev Ragho Rane, Venkata Srinivasa Rao Velivela