Chalcogen Bonded Directly To The Bicyclo-carbocyclic Ring System Patents (Class 546/206)
  • Patent number: 9637454
    Abstract: The present invention relates to the field of pharmaceutical chemistry and pharmacotherapeutics, and in particular to compounds of general formula I, racemates, R-isomers, S-isomers, and pharmaceutically acceptable salts thereof and their mixtures, and the preparation methods thereof and a pharmaceutical composition containing the compounds and uses thereof as an acetylcholine esterase inhibitor.
    Type: Grant
    Filed: October 17, 2013
    Date of Patent: May 2, 2017
    Assignee: SHANGHAI INSTITUTE OF MATERIA MADICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Hong Liu, Haiyan Zhang, Yu Zhou, Yan Fu, Hualiang Jiang, Xican Tang, Kaixian Chen
  • Patent number: 9000010
    Abstract: The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.
    Type: Grant
    Filed: January 19, 2011
    Date of Patent: April 7, 2015
    Assignee: Sanofi
    Inventors: Ahmed Abouabdellah, Antoine Ravet
  • Patent number: 8992976
    Abstract: A pharmaceutical composition is provided according to the invention which is suited for the production of tablets by direct compression and which contains donepezil hydrochloride of polymorphic form I. The polymorphic form I of donepezil hydrochloride in the directly compressed tablet is also stable during long storage.
    Type: Grant
    Filed: December 15, 2006
    Date of Patent: March 31, 2015
    Assignee: ratiopharm, GmbH
    Inventors: Julia Schulze Nahrup, Frank Muskulus, Peter Kraass
  • Patent number: 8993768
    Abstract: Disclosed are compounds that inhibit RNase H activity of retroviruses, for example, a compound of formula (I) wherein R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment or prevention of infection by human immunodeficiency virus (HIV).
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: March 31, 2015
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: John A. Beutler, Stuart F. J. LeGrice, Craig Thomas, Jian-Kang Jiang, Suhman Chung, Jennifer Wilson
  • Patent number: 8987458
    Abstract: The present invention provides a process for preparing donepezil or a salt thereof, the process comprising reducing a 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2-yl)methylene]pyridonium halide of formula II, wherein X is bromide or chloride, in the presence of an ionic compound, a solvent, a catalyst and a source of hydrogen, to form donepezil and optionally converting the donepezil to the salt thereof.
    Type: Grant
    Filed: March 24, 2009
    Date of Patent: March 24, 2015
    Assignee: Cipla Limited
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Srinivas Laxminarayan Pathi
  • Publication number: 20150072980
    Abstract: The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor ?t (ROR?t)/ROR?. The compounds of the present invention are useful for modulating ROR?t)/ROR? activity and for treating diseases or conditions mediated by ROR?t)/ROR? such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer.
    Type: Application
    Filed: August 27, 2014
    Publication date: March 12, 2015
    Inventors: Hariprasad Vankayalapati, Venkatakrishnareddy Yerramreddy
  • Publication number: 20150005283
    Abstract: The present invention provides compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: February 21, 2013
    Publication date: January 1, 2015
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Adrian Wai-Hing Cheung, Ryan Craig Schoenfeld, Weiya Yun, Shu-Hai Zhao
  • Publication number: 20140371209
    Abstract: Compounds of formula (I) or (II) can modulate the activity of SIP receptors.
    Type: Application
    Filed: February 3, 2012
    Publication date: December 18, 2014
    Inventors: Jermaine Thomas, Sha Mi, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Kevin Guckian, Gnanasambandam Kumaravel
  • Patent number: 8906938
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Grant
    Filed: May 14, 2013
    Date of Patent: December 9, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay P. Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Publication number: 20140315952
    Abstract: The composition containing a pamoate salt of donepezil, the method of preparation and the use thereof are disclosed.
    Type: Application
    Filed: November 29, 2012
    Publication date: October 23, 2014
    Inventor: Ziqiang Gu
  • Publication number: 20140249181
    Abstract: Disclosed are compounds that inhibit RNase H activity of retroviruses, for example, a compound of formula (I) wherein R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment or prevention of infection by human immunodeficiency virus (HIV).
    Type: Application
    Filed: May 10, 2012
    Publication date: September 4, 2014
    Applicant: The united States of America, as represented by the Secretary, Department of Health and Human Serv
    Inventors: John A. Beutler, Stuart F.J. LeGrice, Craig Thomas, Jian-Kang Jiang, Suhman Chung, Jennifer Wilson
  • Publication number: 20140249183
    Abstract: Treatments are described for stress disorders and substance use disorders, for example, substance use disorders associated with use of alcohol, cocaine, amphetamines, and the like.
    Type: Application
    Filed: February 22, 2014
    Publication date: September 4, 2014
    Applicant: Baylor College of Medicine
    Inventors: Thomas F. Newton, Colin N. Haile
  • Publication number: 20140235641
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: September 21, 2012
    Publication date: August 21, 2014
    Inventors: Jason Brubaker, Joshua Close, Tony Siu, Graham Frank Smith, Luis E. Torres, Hyun Chong Woo, Jonathan R. Young, Zhongyong Wei, Feng Shi
  • Patent number: 8748613
    Abstract: Compounds of formula (I): wherein A, R1, R2, X, m, and n are as defined in the specification, are selective M3 receptor antagonists and may be used in the treatment of, inter alia, a respiratory disease such as asthma and COPD.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: June 10, 2014
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Gabriele Amari, Cristina Pesenti, Stefano Bossolo
  • Patent number: 8669275
    Abstract: The present application describes deuterium-enriched donepezil, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Grant
    Filed: October 3, 2012
    Date of Patent: March 11, 2014
    Assignee: DeuteRx, LLC
    Inventor: Anthony W. Czarnik
  • Patent number: 8653304
    Abstract: A 2,3-dihydro-1H-indene-2-yl urea represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:
    Type: Grant
    Filed: September 30, 2010
    Date of Patent: February 18, 2014
    Assignee: Toray Industries, Inc.
    Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida
  • Publication number: 20140031341
    Abstract: An in vitro method of screening candidate compounds for the preventive or curative treatment of rosacea is described. The method can include determining the capacity of a compound to modulate the expression or activity of the Transient Receptor Potential (TRPs), as well as the use of modulators of the expression or activity of this transcription factor for the treatment of rosacea. The method can also include in vitro diagnosis or prognosis of this pathology.
    Type: Application
    Filed: December 19, 2011
    Publication date: January 30, 2014
    Applicants: UNIVERSITAT MUNSTER, GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Jerome Aubert, Martin Steinhoff
  • Patent number: 8618133
    Abstract: The present invention relates to an aralkyl alcohol piperidine derivative and use as antidepressant thereof. The said aralkyl alcohol piperidine derivative has a triple inhibition effect on the reuptaking of 5-HT, NA and DA. The derivative may be administered to the patient in need of such treatment in the form of composition by oral administration, injection and the like.
    Type: Grant
    Filed: June 8, 2009
    Date of Patent: December 31, 2013
    Assignee: Jiangsu Hengyi Pharmaceutical Co., Ltd.
    Inventors: Jianqi Li, Kai Gao, Wangping Cai, Yongyong Zheng
  • 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
  • Publication number: 20130324576
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof in which m, n, W, X, Y, Z, R, R1, R2, R3 and R4 are as defined in the specification, for use in therapy.
    Type: Application
    Filed: May 29, 2013
    Publication date: December 5, 2013
    Inventors: Colm Carroll, Anne Goldby, Martin Teall
  • Patent number: 8580822
    Abstract: The present invention provides novel indanone derivatives which can be advantageously used for treating and/or preventing of a medical condition for which inhibition of a cholinesterase is desired.
    Type: Grant
    Filed: June 8, 2012
    Date of Patent: November 12, 2013
    Assignee: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan Bhat, Prabhu Prasad Mohapatra
  • Publication number: 20130296283
    Abstract: Preparation methods of mesylate, para-toluenesulfonate, succinate, tartrate, sulphate, nitrate, phosphate, salicylate, fumarate, maleate, gallate, acetylsalicylate, benzenesulphonate, citrate, aspartate, glutaminate, lactate, gluconate, ascorbate, malonate, malate, sorbate, acetate or formate of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine (i.e., Donepezil). Novel polymorphs formed from these salts and their preparation methods. Co-crystals formed from Donepezil hydrochloride and maleic acid, fumaric acid, citric acid, salicylic acid, tartaric acid or succinic acid.
    Type: Application
    Filed: July 5, 2013
    Publication date: November 7, 2013
    Inventor: Hesheng Zhang
  • Publication number: 20130289280
    Abstract: Crystalline salts, polymorphs, solvates, and hydrates of bicalutamide, 5-fluorouracil, donepezil, anastrozole, nelfinavir, mirtazapine, lansoprazole, and tamsulosin, or derivatives thereof are provided by the subject invention. Methods of making and using the same are also provided.
    Type: Application
    Filed: May 7, 2013
    Publication date: October 31, 2013
    Applicants: TRANSFORM PHARMACEUTICALS, INC., UNIVERSITY OF SOUTH FLORIDA
    Inventors: University of South Florida, Transform Pharmaceuticals, Inc.
  • Patent number: 8552195
    Abstract: The method in accordance with the present invention has: mixing E2M, an organic solvent, a weak base, sodium dithionite, and a phase transfer catalyst to obtain an E2M mixture solution; heating the E2M mixture solution and adding water to obtain a heated E2M aqueous solution having an organic layer; and extracting the organic layer from the heated E2M aqueous solution, and condensing and drying the organic layer to obtain donepezil. Employing sodium dithionite as a reducing agent improves safety over hydrogen gas used in conventional methods and lowers the cost in contrast to the conventional noble metal catalysts that are extremely expensive. Furthermore, the method of the present invention requires only 60 minutes of reaction time to synthesize donepezil with a promising yield more than 85%, which greatly raises the efficiency and economic value of the manufacture of donepezil.
    Type: Grant
    Filed: August 5, 2011
    Date of Patent: October 8, 2013
    Assignee: Taiwan Biotech Co., Ltd.
    Inventors: Kuen-Wang Sheu, Shu-Fen Huang
  • Patent number: 8524947
    Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.
    Type: Grant
    Filed: February 23, 2009
    Date of Patent: September 3, 2013
    Assignees: University of South Florida, H. Lee Moffitt Cancer Center and Research Institute, Inc.
    Inventors: Hong-Gang Wang, Roman Manetsch, Xiangdong Hu, Sameer Kulkarni, Jiazhi Sun
  • Patent number: 8513237
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: August 20, 2013
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Kristof Van Emelen, Leo Jacobus Jozel Backx, Sven Franciscus Anna Van Brandt, Patrick René Angibaud, Isabelle Noëlle Constance Pilatte, Marc Gustaaf Celine Verdonck, Hans Louis Jos De Winter, Jimmy Arnold Viviane Van heusden
  • Patent number: 8507538
    Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
    Type: Grant
    Filed: November 15, 2010
    Date of Patent: August 13, 2013
    Assignee: Receptos, Inc.
    Inventors: Marcus F. Boehm, Esther Martinborough, Enugurthi Brahmachary, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam Richard Yeager
  • Publication number: 20130203709
    Abstract: The present disclosure relates to acylsulfonamides and processes for their preparation. The processes involve a target-guided synthesis approach, whereby a thioacid and a sulfonyl azide are reacted in the presence of a biological target protein, a Bcl-2 family protein, to form the acylsulfonamide.
    Type: Application
    Filed: August 9, 2011
    Publication date: August 8, 2013
    Applicants: THE PENN STATE RESEARCH FOUNDATION, UNIVERSITY OF SOUTH FLORIDA
    Inventors: Roman Manetsch, Sameer Kulkarni, Iredia D. Iyamu, Hong-Gang Wang, Kenichiro Doi, Wayne Guida, Daniel Santiago, Courtney du Boulay
  • Patent number: 8501779
    Abstract: Preparation methods of mesylate, para-toluenesulfonate, succinate, tartrate, sulphate, nitrate, phosphate, salicylate, fumarate, maleate, gallate, acetylsalicylate, benzenesulphonate, citrate, aspartate, glutaminate, lactate, gluconate, ascorbate, malonate, malate, sorbate, acetate or formate of 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine (i.e., Donepezil). Novel polymorphs formed from these salts and their preparation methods. Co-crystals formed from Donepezil hydrochloride and maleic acid, fumaric acid, citric acid, salicylic acid, tartaric acid or succinic acid.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: August 6, 2013
    Assignee: Tianjin Hemay Bio-Tech Co., Ltd.
    Inventor: Hesheng Zhang
  • Patent number: 8476300
    Abstract: The present invention is directed to a compound of the formula (A): or a pharmaceutically acceptable salt thereof; and also to compounds of formula (I): or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 3, 2009
    Date of Patent: July 2, 2013
    Assignee: Eli Lilly and Company
    Inventors: Jeffrey Alan Dodge, Timothy Ivo Richardson, Christian Alexander Clarke, Scott Alan Jones, Ronald Jay Hinklin, Conrad Wilson Hummel, George Sal Lewis
  • Publication number: 20130131034
    Abstract: The instant invention relates to derivatives of formula (I) and their application in therapeutics.
    Type: Application
    Filed: March 1, 2011
    Publication date: May 23, 2013
    Applicant: SANOFI
    Inventors: Markus Follmann, Pascale Goberville, Stéphanie Hachtel, Gerhard Hessler, Heinz-Werner Kleemann, Thomas Maier, Gary MC Cort, Carsten Struebing, Bérangère Thiers, Li-Hsing Wang
  • Publication number: 20130131079
    Abstract: The present invention is directed to a compound of formula (I) for use in a method to treat or ameliorate amyloid or tau pathologies, such as Alzheimer's disease, or symptoms thereof. The invention is also directed to new compounds of formula (I), of subformula (II), (III), (IV), or (V).
    Type: Application
    Filed: May 23, 2011
    Publication date: May 23, 2013
    Applicant: FAES FARMA, S.A.
    Inventors: Francisco Ledo Gómez, Ana Muñoz Muñoz, Carmen Pumar Durán
  • Patent number: 8445515
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Grant
    Filed: December 21, 2009
    Date of Patent: May 21, 2013
    Assignee: Chemocentryx, Inc.
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Publication number: 20130090357
    Abstract: The present application describes deuterium-enriched donepezil, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: October 3, 2012
    Publication date: April 11, 2013
    Applicant: DEUTERIA PHARMACEUTICALS INC
    Inventor: DEUTERIA PHARMACEUTICALS INC.
  • Publication number: 20130090476
    Abstract: Thiazolylpiperidine derivatives of the formula (I), in which the symbols A, G, Y, n, R1, R2, R3, R4 and R5 have the meanings given in the description, and also agrochemically active salts thereof, and their use for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).
    Type: Application
    Filed: September 5, 2012
    Publication date: April 11, 2013
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Pierre CRISTAU, Nicola Rahn, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann, Jurgen Benting
  • Publication number: 20130090477
    Abstract: Thiazolylpiperidine derivatives of the formula (I), in which the symbols A, G, Y, n, R1, R2, R3, R4 and R5 have the meanings given in the description, and also agrochemically active salts thereof, and their use for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).
    Type: Application
    Filed: September 5, 2012
    Publication date: April 11, 2013
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Pierre CRISTAU, Nicola RAHN, Tomoki TSUCHIYA, Ulrike WACHENDORFF-NEUMANN, Jürgen BENTING
  • Publication number: 20130035490
    Abstract: The method in accordance with the present invention has: mixing E2M, an organic solvent, a weak base, sodium dithionite, and a phase transfer catalyst to obtain an E2M mixture solution; heating the E2M mixture solution and adding water to obtain a heated E2M aqueous solution having an organic layer; and extracting the organic layer from the heated E2M aqueous solution, and condensing and drying the organic layer to obtain donepezil. Employing sodium dithionite as a reducing agent improves safety over hydrogen gas used in conventional methods and lowers the cost in contrast to the conventional noble metal catalysts that are extremely expensive. Furthermore, the method of the present invention requires only 60 minutes of reaction time to synthesize donepezil with a promising yield more than 85%, which greatly raises the efficiency and economic value of the manufacture of donepezil.
    Type: Application
    Filed: August 5, 2011
    Publication date: February 7, 2013
    Applicant: Taiwan Biotech Co, Ltd.
    Inventors: Kuen-Wang Sheu, Shu-Fen Huang
  • Patent number: 8343967
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: April 27, 2012
    Date of Patent: January 1, 2013
    Assignee: Abbott Laboratories
    Inventors: Hong Ding, Steven W. Elmore, Laura A. Hexamer, Aaron R. Kunzer, Cheol-Min Park, Andrew J. Souers, Gerard M. Sullivan, Michael D. Wendt
  • Publication number: 20120323012
    Abstract: 4-(azacycloalkyl)-benzene-1,3-diol compounds with the following general formula (I): Also described, are compositions that include these compounds and processes for their preparation and use in pharmaceutical or cosmetic compositions for treating pigmentary disorders.
    Type: Application
    Filed: December 8, 2010
    Publication date: December 20, 2012
    Applicant: GALDERMA RESEARCH & DEVELOPMENT
    Inventors: Jean-Guy Boiteau, Anne-Pascale Luzy
  • Patent number: 8318942
    Abstract: A process for producing a Donepezil derivative represented by the formula (I), wherein R1, R2, R3, and R4 each independently represents H, F, an alkyl having from 1 to 4 carbon atoms, or an alkoxy having from 1 to 4 carbon atoms; R5 represents a phenyl or a substituted phenyl; and n is an integer from 0 to 2, characterized in that the process comprises: (a) a reaction of 4-pyridinecarboxaldehyde with a compound of formula (II) in the presence of a strong acid HX to form a compound of formula (III); (b) a catalytic hydrogenation of a compound of formula (III) or a compound of formula (V) to yield a compound of formula (IV); and (c) an alkylation reaction of a compound of formula (IV) to yield a compound of formula (I).
    Type: Grant
    Filed: October 28, 2004
    Date of Patent: November 27, 2012
    Assignee: Tianjin Hemay Bio-Tech Co., Ltd.
    Inventor: Heshang Zhang
  • Publication number: 20120295909
    Abstract: The invention relates to compounds corresponding to the general formula (I): in which R2 represents a hydrogen, fluorine, hydroxyl, cyano, trifluoromethyl, C1-6-alkyl, C1-6-alkoxy or —NR8R9; n and m represent, independently of one another, an integer equal to 1, 2 or 3, it being understood that the sum m+n is at most equal to 5; A represents a covalent bond, an oxygen, a C1-6-alkylene or —O—C1-6-alkylene; R1 represents a phenyl or a heterocycle which is optionally substituted; R3 represents a hydrogen, fluorine, C1-6-alkyl or trifluoromethyl; R4 represents an optionally substituted 5-membered heterocycle; in the form of the base or of an addition salt with an acid; with the exclusion of 5-methylisoxazol-3-ylmethyl 4-hydroxy-4-(4-chlorophenyl)piperidine-1-carboxylate. The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.
    Type: Application
    Filed: January 19, 2011
    Publication date: November 22, 2012
    Applicant: SANOFI
    Inventors: Ahmed Abouabdellah, Antoine Ravet
  • Patent number: 8309715
    Abstract: A novel camphor-derived ?-amino alcohol compound is disclosed. The novel camphor-derived ?-amino alcohol compound can be used in asymmetric addition of organozinc to aromatic and aliphatic aldehydes, including linear aliphatic ones, thus generating corresponding secondary alcohols in high yields and enantiomeric excess.
    Type: Grant
    Filed: June 18, 2010
    Date of Patent: November 13, 2012
    Assignee: National Tsing Hua University
    Inventors: Biing-Jiun Uang, Chi-Rui Wu, Hsyueh-Liang Wu, Ping-Yu Wu
  • Patent number: 8304435
    Abstract: The present application describes deuterium-enriched donepezil, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Grant
    Filed: August 22, 2008
    Date of Patent: November 6, 2012
    Assignee: Deuteria Pharmaceuticals Inc.
    Inventor: Anthony W Czarnik
  • Publication number: 20120270877
    Abstract: The invention provides compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
    Type: Application
    Filed: November 1, 2010
    Publication date: October 25, 2012
    Applicant: MannKind Corporation
    Inventors: Qingping Zeng, Warren S. Wade, John Bruce Patterson
  • Publication number: 20120252842
    Abstract: The present invention provides novel indanone derivatives which can be advantageously used for treating and/or preventing of a medical condition for which inhibition of a cholinesterase is desired.
    Type: Application
    Filed: June 8, 2012
    Publication date: October 4, 2012
    Applicant: REVIVA PHARMACEUTICALS, INC.
    Inventors: Laxminarayan BHAT, Prabhu Prasad MOHAPATRA
  • Publication number: 20120220629
    Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor.
    Type: Application
    Filed: February 24, 2012
    Publication date: August 30, 2012
    Inventors: Silvina GARCIA RUBIO, Claudio Pietra, Claudio Giuliano, Zhigang Li
  • Patent number: 8252814
    Abstract: Agents for improving potency of the urinary bladder which comprise an amine compound of non-carbamate-type having an acetylcholinesterase-inhibiting action. Particularly, crystals of a tricyclic, condensed, heterocyclic derivative are provided, which possess an excellent action to inhibit acetylcholinesterase and an action to improve the excretory potency of the urinary bladder. As an example, crystals of 8-[3-[1-[(3-fluorophenyl)-methyl]-4-piperidinyl]-1-oxopropyl]-1,2,5,6-tetrahydro-4H-pyrrolo[3,2,1-ij]quinolin-4-one or a salt thereof and pharmaceutical compositions containing them are disclosed.
    Type: Grant
    Filed: July 17, 2008
    Date of Patent: August 28, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yuji Ishihara, Takayuki Doi, Hiroshi Nagabukuro, Yuji Ishichi
  • Publication number: 20120202756
    Abstract: The present invention relates to prodrugs of a wide variety of drugs and pharmaceutical compositions containing such prodrugs. Methods for minimizing locally mediated (from within the gut lumen) adverse gastrointestinal events associated with the underivatised drug and increasing the sustainment of plasma drug levels with the aforementioned prodrugs are also provided. Thus, the present invention relates to the use of prodrugs of a wide diversity of drugs (other than opioids) to transiently inactivate them and so reduce directly, locally mediated adverse gastrointestinal (GI) side-effects normally evident after administration of the parent compound. Additionally, such prodrugs may confer improved pharmacokinetics.
    Type: Application
    Filed: October 5, 2011
    Publication date: August 9, 2012
    Inventors: Richard Franklin, Martin Quibell, Robert G. Tyson, Bernard T. Golding
  • Publication number: 20120196852
    Abstract: The invention is directed towards novel naphthoquinone and naphthothiazole compounds, and methods of treating disorders related to MetAP, including tuberculosis and bacterial infection, using various naphthoquinone, hydroxyquinonline, and naphthothiazole compounds.
    Type: Application
    Filed: August 5, 2010
    Publication date: August 2, 2012
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Jun O. Liu, Omonike Arike Olaleye, Shridhar Bhat
  • Publication number: 20120184735
    Abstract: A 2,3-dihydro-1H-indene-2-yl urea derivative represented by Formula (Ia) or a pharmaceutically acceptable salt thereof:
    Type: Application
    Filed: September 30, 2010
    Publication date: July 19, 2012
    Applicant: TORAY INDUSTRIES, INC.
    Inventors: Hiroaki Kaneko, Hideki Kawai, Yosuke Iura, Hideki Inoue, Mie Kaino, Hiroyuki Meguro, Tazuru Uchida