Plural Rings In A Substituent E Patents (Class 564/221)
  • Publication number: 20140336252
    Abstract: The present invention provides compounds having the structure represented by general formula I, pharmaceutically acceptable salts thereofagonist, preparation methods therefor and a use thereof in the preparation of a medicine for the treatment of nervous system diseases. The compounds or pharmaceutical compositions thereof can be used as the KCNQ potassium channel agonist for treating nervous system diseases. Compared to retigabine, a compound in the prior art, the compound of the present invention have the same or better therapeutic effect, are easier for synthesis and storage, and less prone to oxidate deterioration.
    Type: Application
    Filed: October 23, 2012
    Publication date: November 13, 2014
    Inventors: Fajun Nan, Min Li, Zhaobing Gao, Fei Chen, Yangming Zhang, Pingzheng Zhou, Haining Hu, Haiyan Xu, Sheng Liu
  • Patent number: 8871976
    Abstract: The invention includes a compound represented by the following structural formula: wherein is described herein. The compounds of the invention are useful in staining embryonic stem cells.
    Type: Grant
    Filed: August 26, 2011
    Date of Patent: October 28, 2014
    Assignees: National University of Singapore, Agency for Science, Technology and Research
    Inventors: Young-Tae Chang, Sung Chan Lee, Nam Young Kang
  • Publication number: 20140274699
    Abstract: Described herein are methods and compositions for enhancing pathogen immunity in plants and improving plant growth.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Thomas Eulgem, Melinda Rodriguez-Salus, Colleen M. Knoth
  • Patent number: 8741259
    Abstract: Disclosed are oxo-hydroquinazolines that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.
    Type: Grant
    Filed: October 20, 2008
    Date of Patent: June 3, 2014
    Inventors: Marvin C. Gershengorn, Susanne Neumann, Bruce M. Raaka, Craig J. Thomas, James Inglese, Noel T. Southall, Steven Titus, Wei Zheng, Wenwei Huang, Gerd Krause, Gunnar Kleinau
  • Publication number: 20140135300
    Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like. Processes for making the compound of formula (I), as well as related intermediates, are disclosed.
    Type: Application
    Filed: January 17, 2014
    Publication date: May 15, 2014
    Applicant: SUNOVION PHARMACEUTICALS INC.
    Inventors: Craig R. Abolin, H. Scott Wilkinson, Paul McGlynn, William K. McVicar
  • Patent number: 8722929
    Abstract: This invention provides compounds of formula A and formula B which are modulators of potassium ion channels and are useful for the treatment of seizure disorders.
    Type: Grant
    Filed: October 10, 2007
    Date of Patent: May 13, 2014
    Assignee: Valeant Pharmaceuticals International
    Inventors: Jean-Michel Vernier, Jianlan Song, Huanming Chen, Zhi Hong
  • Publication number: 20140080800
    Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, or prodrug thereof, wherein U, J, V, X, R2a, R2b, R2c, R5 and t are as described herein. The present invention relates generally to inhibitors of histone deacetylase and to methods of making and using them. These compounds are useful for promoting cognitive function and enhancing learning and memory formation. In addition, these compounds are useful for treating, alleviating, and/or preventing various conditions, including for example, neurological disorders, memory and cognitive function disorders/impairments, extinction learning disorders, fungal diseases and infections, inflammatory diseases, hematological diseases, and neoplastic diseases in humans and animals.
    Type: Application
    Filed: October 28, 2013
    Publication date: March 20, 2014
    Inventors: Edward Holson, Florence Fevrier Wagner, Michel Weiwer, Li-Huei Tsai, Stephen Haggarty, Yan-Ling Zhang
  • Patent number: 8664441
    Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like. Processes for making the compound of formula (I), as well as related intermediates, are disclosed.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: March 4, 2014
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Craig R. Abolin, H. Scott Wilkinson, Paul McGlynn, William K. McVicar
  • Publication number: 20130331568
    Abstract: The invention provides compounds of formula I wherein n, A, R, R?, R?, R0, X and Y are as defined in the description, and their preparation. The compounds of formula I are useful as pharmaceuticals.
    Type: Application
    Filed: August 15, 2013
    Publication date: December 12, 2013
    Applicant: Novartis AG
    Inventors: Fabrizio Gasparini, Yves Auberson, Silvio Ofner, Terance W. Hart, Kaspar Zimmermann
  • Publication number: 20130296607
    Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like. Processes for making the compound of formula (I), as well as related intermediates, are disclosed.
    Type: Application
    Filed: July 3, 2013
    Publication date: November 7, 2013
    Inventors: Craig R. Abolin, H. Scott Wilkinson, Paul McGlynn, William K. McVicar
  • Publication number: 20130230542
    Abstract: Provided are compounds according to the following Formula I: The Formula I compounds are activated in the presence of reactive oxygen species (ROS) and are therefore selective anti-cancer therapeutics for cancers associated with elevated ROS. Also provided are methods and pharmaceutical compositions for treating cancers associated with increased ROS.
    Type: Application
    Filed: March 1, 2013
    Publication date: September 5, 2013
    Applicants: CINCINNATI CHILDREN'S HOSPITAL MEDICAL CENTER, UNIVERSITY OF CINCINNATI
    Inventors: Edward J. Merino, James C. Mulloy, Guorui Li, Tiffany Bell-Horwath
  • Publication number: 20130224790
    Abstract: The invention includes a compound represented by the following structural formula: wherein is described herein. The compounds of the invention are useful in staining embryonic stem cells.
    Type: Application
    Filed: August 26, 2011
    Publication date: August 29, 2013
    Applicants: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH, NATIONAL UNIVERSITY OF SINGAPORE
    Inventors: Young-Tae Chang, Sung Chan Lee, Nam Young Kang
  • Publication number: 20130225596
    Abstract: The present invention provides novel compounds having a P2X3 and/or P2X2/3 receptor antagonistic effect. A pharmaceutical composition having a P2X3 and/or P2X2/3 receptor antagonistic effect comprising a compound of the formula (I): wherein ring A is substituted or unsubstituted 5 to 7-membered cycloalkane, substituted or unsubstituted 5 to 7-membered cycloalkene or the like; C is a carbon atom; —X— is —N(R16)— or the like; R16 is hydrogen, substituted or unsubstituted alkyl or the like; R7 is substituted or unsubstituted 5- or 6-membered heteroaryl, substituted or unsubstituted 6 to 10 membered aryl; Q1 and Q2 are each independently a carbon atom or a nitrogen atom; -L- is —O—, —S— or the like; R6 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted cycloalkenyl or the like; R2 is hydrogen, hydroxy or the like, or its pharmaceutically acceptable salt or a solvate thereof.
    Type: Application
    Filed: August 9, 2011
    Publication date: August 29, 2013
    Inventors: Hiroyuki Kai, Takeshi Endoh, Sae Jikihara, Kentaro Asahi, Tohru Horiguchi
  • Patent number: 8501994
    Abstract: The compound of formula (I) is a water-stable, long acting ?2-selective adrenoceptor agonist useful as a bronchodilator in the treatment of bronchoconstriction associated with reversible obstructive airways diseases and the like.
    Type: Grant
    Filed: August 22, 2008
    Date of Patent: August 6, 2013
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Craig R. Abolin, H. Scott Wilkinson, Paul McGlynn, William K. McVicar
  • Patent number: 8487109
    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R1; R2; R3; R4; R5; J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process for aryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional aryl-1-alkynes of the formula I.
    Type: Grant
    Filed: December 23, 2009
    Date of Patent: July 16, 2013
    Assignee: Sanofi
    Inventors: Omar Rkyek, Marc Nazare, Andreas Lindenschmidt, Matthias Urmann, Nis Halland, Jorge Alonso
  • Patent number: 8455689
    Abstract: The present invention relates to a process for preparing substituted biphenylanilides of the formula I wherein R1 is a protected amino group which comprises reacting a compound of formula II in the presence of a base and of a palladium catalyst in a solvent, with an organoboron compound of formula (III)
    Type: Grant
    Filed: April 24, 2009
    Date of Patent: June 4, 2013
    Assignee: Bayer CropScience AG
    Inventors: Michael Dockner, Heiko Rieck, Wahed Ahmed Moradi, Norbert Lui
  • Patent number: 8436211
    Abstract: The present invention relates to a process for the preparation of substituted biphenyls by reacting aryl halides with tetraarylborates in the presence of palladium catalysts.
    Type: Grant
    Filed: August 30, 2010
    Date of Patent: May 7, 2013
    Assignee: Bayer CropScience AG
    Inventors: Wahed Ahmed Moradi, Norbert Lui, Michael Dockner, Thomas Jagusch
  • Publication number: 20130018077
    Abstract: Provided are alkynyl phenyl derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: September 14, 2012
    Publication date: January 17, 2013
    Applicant: Acucela Inc.
    Inventors: Ian Leslie Scott, Vladmir Aleksandrovich Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Jennifer Gage, Feng Hong
  • Publication number: 20130018026
    Abstract: The present invention provides compositions and methods for the targeted delivery, release and/or formation of a drug compound at a target site(s) within the body of an individual, such as a diseased and/or inflamed tissue in the body of the individual. These compositions may comprise a halogenated phenol ring cleavably linked to a core structure of a drug compound. Due to the variety of substituents that may be utilized in forming the different types of linkages, numerous examples of drug compounds linked to a halogenated phenol ring are proposed. The present invention further provides compositions comprising halogenated phenol starting compounds that do not undergo cleavage during a dehalogenation reaction to form a drug compound in a targeted tissue when administered to an individual. Methods of administering these non-cleaving compounds are further provided.
    Type: Application
    Filed: July 13, 2012
    Publication date: January 17, 2013
    Inventor: Keith R. Latham
  • Patent number: 8110706
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: April 26, 2010
    Date of Patent: February 7, 2012
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
  • Publication number: 20120029237
    Abstract: An autocatalytic process for the synthesis of chiral propargylic alcohols.
    Type: Application
    Filed: April 9, 2010
    Publication date: February 2, 2012
    Inventors: Nicka Chinkov, Aleksander Warm, Erick Carreira
  • Publication number: 20110313199
    Abstract: Provided herein are improved, convenient and industrially advantageous processes for the preparation of N-[2-hydroxy-5-[(1R)-1-hydroxy-2-[[(1R)-2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]phenyl]formamide (Arformoterol) or a pharmaceutically acceptable salt thereof, in high yield and purity. Provided further herein is an improved and industrially advantageous process for the preparation of a substantially enantiomerically pure arformoterol intermediate, (R)-4-methoxy-?-methyl-N-(phenylmethyl)benzeneethanamine.
    Type: Application
    Filed: December 28, 2009
    Publication date: December 22, 2011
    Applicant: ACTAVIS GROUP PTC EHF
    Inventors: Girish Dixit, Nandkumar Gaikwad, Nitin Sharadchandra Pradhan
  • Publication number: 20110195018
    Abstract: Disclosed are oxo-hydroquinazolines that are useful as selective TSHR agonists. The compounds may be used for detecting or treating thyroid cancer, or treating a bone degenerative disorder.
    Type: Application
    Filed: October 20, 2008
    Publication date: August 11, 2011
    Inventors: Marvin C. Gershengorn, Susanne Neumann, Bruce M. Raaka, Craig J. Thomas, James Inglese, Noel T. Southall, Steven Titus, Wei Zheng, Wenwei Huang, Gerd Krause, Gunnar Kleinau
  • Patent number: 7964753
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: June 7, 2010
    Date of Patent: June 21, 2011
    Assignee: Sunovion Pharmaceuticals Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
  • Publication number: 20110105796
    Abstract: The present invention relates to a process for the preparation of substituted biphenyls by reacting aryl halides with tetraarylborates in the presence of palladium catalysts.
    Type: Application
    Filed: August 30, 2010
    Publication date: May 5, 2011
    Applicant: Bayer CropScience AG
    Inventors: Wahed Ahmed MORADI, Norbert Lui, Michael Dockner, Thomas Jagusch
  • Publication number: 20110105760
    Abstract: The present invention relates to a process for preparing substituted 2-aminobiphenyls and to a process for preparing (Het)arylamides of such 2-aminobiphenyls.
    Type: Application
    Filed: July 3, 2009
    Publication date: May 5, 2011
    Applicant: BASF SE
    Inventors: Michael Keil, Michael Rack, Thomas Zierke, Markus Heinrich, Alexander Wetzel
  • Publication number: 20110092736
    Abstract: The present invention relates to a process for preparing substituted biphenylanilides of the formula I wherein R1 is a protected amino group which comprises reacting a compound of formula II in the presence of a base and of a palladium catalyst in a solvent, with an organoboron compound of formula (III)
    Type: Application
    Filed: April 24, 2009
    Publication date: April 21, 2011
    Applicant: Bayer CropScience AG
    Inventor: Michael DOCKNER
  • Publication number: 20110082176
    Abstract: The present disclosure provides non-naturally occurring polyphenol compounds that upregulate the expression of Apolipoprotein A-I (ApoA-I). The disclosed compositions and methods can be used for treatment and prevention of cardiovascular disease and related disease states, including cholesterol or lipid related disorders, such as, e.g., atherosclerosis.
    Type: Application
    Filed: October 15, 2010
    Publication date: April 7, 2011
    Inventors: Norman C.W. Wong, Joseph E.L. Tucker, Henrik C. Hansen, Fabrizio S. Chiacchia, David McCaffrey
  • Publication number: 20100286204
    Abstract: There is provided a compound having Formula I wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, —OC(R13)3, —OCH(R13)2, —OCH2R13, C(R13)3, —CH(R13)2, or —CH2R13 wherein R13 is a halogen; (c) —CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (l) aryloxy; (m) —SO2-alkyl; and (n) —N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (f) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=0
    Type: Application
    Filed: November 19, 2008
    Publication date: November 11, 2010
    Applicant: Sterix Limited
    Inventors: Nigel Vicker, Helen Victoria Bailey, Wesley Heaton, Joanna Mary Day, Atul Purohit, Barry Victor Lloyd Potter
  • Publication number: 20100261910
    Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R1; R2; R3; R4; R5; J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process for aryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional aryl-1-alkynes of the formula I.
    Type: Application
    Filed: December 23, 2009
    Publication date: October 14, 2010
    Applicant: sanofi-aventis
    Inventors: Omar RKYEK, Marc NAZARE, Andreas LINDENSCHMIDT, Matthias URMANN, Nis HALLAND, Jorge ALONSO
  • Publication number: 20100249459
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Application
    Filed: June 7, 2010
    Publication date: September 30, 2010
    Applicant: SEPRACOR INC.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
  • Patent number: 7732641
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: December 5, 2008
    Date of Patent: June 8, 2010
    Assignee: Sepracor Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
  • Publication number: 20100125150
    Abstract: The invention provides a novel ?2 adrenergic receptor agonist in crystalline salt form. The invention also provides pharmaceutical compositions comprising the novel ?2 adrenergic receptor agonist in crystalline salt form, formulations containing the pharmaceutical compositions, methods of using the crystalline salt to treat diseases associated with ?2 adrenergic receptor activity, and processes useful for preparing such crystalline compounds.
    Type: Application
    Filed: May 13, 2009
    Publication date: May 20, 2010
    Applicant: THERAVANCE, INC.
    Inventors: Ioanna Stergiades, Edward Yost, Cristin Hubbard, Weijiang Zhang
  • Publication number: 20100063157
    Abstract: The present invention relates to the preparation of a ?2 adrenergic agonist in crystalline salt form. In particular the invention relates to preparation of a crystalline salt of compound (I) in particular a crystalline monohydrochloride salt. The invention also relates to a new crystalline form (polymorph) of the monohydrochloride salt of compound (Ia) and a process for preparing it.
    Type: Application
    Filed: March 30, 2005
    Publication date: March 11, 2010
    Inventor: Darren Michael CAINE
  • Patent number: 7601870
    Abstract: The present invention relates to aniline derivatives of the general formula I or salts thereof, described therein, and their use.
    Type: Grant
    Filed: December 20, 2005
    Date of Patent: October 13, 2009
    Assignee: H. Lundbeck A/S
    Inventors: Christian Wenzel Tornøe, Mario Rottländer, Daniel Rodriguez Greve, Nikolay Khanzhin, Andreas Ritzén, William Patrick Watson
  • Publication number: 20090234162
    Abstract: A radioactive halogen-labeled phenyoxyaniline derivative represented by the following formula: wherein R1 represents a group such as an alkyl group; X1, X2, X3 and X4 represent each a hydrogen atom, an alkyl group, an alkoxy group, an alkoxy group carrying 11C introduced thereinto or a radioactive halogen atom, provided that at least one of X1, X2, X3 and X4 represents an alkoxy group carrying 11C introduced thereinto or a radioactive halogen atom; which is a compound useful as a PBR ligand having a high affinity and a high selectivity. In in vitro measurement of PBR, a PBR ligand having a high affinity and a high selectivity is labeled with a radioactive halogen nuclear species so as to enable the measurement of PBR in vivo with the use of means including not only PET but also SPECT. Thus, a compound which is useful in early diagnosing, preventing and treating diseases such as Alzheimer type dementia can be obtained.
    Type: Application
    Filed: December 28, 2005
    Publication date: September 17, 2009
    Applicants: Taisho Pharmaceutical Co., Ltd., National Institute of Radiological Sciences
    Inventors: Kazutoshi Suzuki, Tetsuya Suhara, Christer Halldin, Ming-Rong Zhang, Atsuro Nakazato
  • Publication number: 20090156862
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Application
    Filed: December 5, 2008
    Publication date: June 18, 2009
    Applicant: Sepracor Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
  • Publication number: 20090042961
    Abstract: The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
    Type: Application
    Filed: May 8, 2008
    Publication date: February 12, 2009
    Inventors: Varghese John, Michel Maillard, Barbara Jagodzinska, Jose Aquino, Gary Probst, Jay Tung
  • Patent number: 7479572
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: January 14, 2008
    Date of Patent: January 20, 2009
    Assignee: Sepracor Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayaka, Donald W. Kessler
  • Publication number: 20080262011
    Abstract: The present invention relates to a compound of formula I, or a pharmaceutically acceptable salt thereof. Formula (I), wherein R1 and R2 are each independently H or alkyl; Y is an alkyl group. CONR3R4, COOR5SO2NR16R17, NHSO2R18 or CN; X is an aryl or heteroaryl group, each of which may be optionally substituted with one or more substituents selected from (CH2)mZ where Z is halogen, OH, CN, alkyl, alkoxy, NO2, CF3, CONR6R7, CN, NR8R9, COOR10 or NHCOR11 and m is 0 to 3; R3 to R11 are each independently H, alkyl or aryl, wherein said alkyl and aryl groups are optionally substituted by one or more substituents selected from halogen, OH, CN, alkyl, alkoxy, NO2, CF3, CONR12R13, CN, NH2, COOR14, NHCOR15, and CN; R12 to R18 are each independently H or alkyl, more preferably H or Me; n is 1 to 6; wherein the compound is other than 3?,5?-dimethyl-4-(1,1-dimethylheptyl)-1,1?-biphenyl-2-ol.
    Type: Application
    Filed: December 21, 2005
    Publication date: October 23, 2008
    Inventors: David Selwood, Cristina Visintin, David Baker, Gareth Pryce, Masahiro Okuyama
  • Publication number: 20080207701
    Abstract: A compound of the formula (I) wherein the variables X1, X2, B, D, R1 to R7 including R3?, p, y, q, and z, are as defined or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixtures thereof, useful for the treatment, prevention or amelioration of obesity and Related Diseases is disclosed.
    Type: Application
    Filed: April 2, 2008
    Publication date: August 28, 2008
    Inventors: Mark Donald Chappell, Charles Howard Mitch, Steven James Quimby, Miles Goodman Siegel
  • Publication number: 20080188561
    Abstract: This invention provides compounds of formula A and formula B which are modulators of potassium ion channels and are useful for the treatment of seizure disorders.
    Type: Application
    Filed: October 10, 2007
    Publication date: August 7, 2008
    Inventors: Jean-Michel Vernier, Jianlan Song, Huanming Chen, Zhi Hong
  • Patent number: 7342132
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: August 4, 2006
    Date of Patent: March 11, 2008
    Assignee: Sepracor Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
  • Patent number: 7262326
    Abstract: A process for preparing indanylamine and aminotetralin derivatives from indanone or tetralone oximes by acylating the oximes with an organic anhydride, followed by catalytic hydrogenation in the presence of an organic anhydride with subsequent hydrolysis is described. The process is commercially feasible providing indanylamine and aminotetralin derivatives in high yield that are useful as intermediates in the production of therapeutically active compounds. Also described are novel intermediates, 1-indanone O-acetyl oximes and 1-tetralone O-acetyl oximes.
    Type: Grant
    Filed: September 7, 2005
    Date of Patent: August 28, 2007
    Assignee: Teva Pharmaceuticals Industries Ltd.
    Inventors: Sylvie Blanchet, Bertrand Blandine, Alain Burgos, Yvon Derrien, Marie-Laure Moreau
  • Patent number: 7145036
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: February 7, 2005
    Date of Patent: December 5, 2006
    Assignee: Sepracor Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W. Kessler
  • Patent number: 6964963
    Abstract: The present invention describes a process for preparing 4-amino-1-naphthol ethers which is characterized in that naphthol ethers are first prepared from 1-naphthols, the former are then converted to the corresponding 4-acetamino-1-naphthol ethers and then the acyl group is cleaved off, and further describes 4-acetamino-1-naphthol ethers obtained thereby.
    Type: Grant
    Filed: August 27, 2002
    Date of Patent: November 15, 2005
    Assignee: Bayer Aktiengesellschaft
    Inventors: Joachim Komoschinski, Herbert Diehl
  • Patent number: 6870069
    Abstract: A phenyloxyaniline derivative useful as a ligand for peripheral benzodiazepine receptor having a strong affinity and a high selectivity, which is represented by formula (1): wherein X1 and X2 are same or different and each is hydrogen atom or halogen atom; R1 and R2 are same or different and each is hydrogen atom, an alkyl group having 1 to 10 carbon(s) or a halogen-substituted alkyl group having 1 to 10 carbon(s); and R3 is a halogen-substituted alkyl group having 1 to 5 carbon(s), or a radioisotope thereof.
    Type: Grant
    Filed: November 4, 2003
    Date of Patent: March 22, 2005
    Assignees: National Institute of Radiological Sciences, Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co., Ltd.
    Inventors: Kazutoshi Suzuki, Ming-Rong Zhang, Tetsuya Suhara, Atsuro Nakazato, Makoto Goto
  • Patent number: 6720453
    Abstract: A method of preparation of a highly pure salt of R,R-formoterol L-tartrate is disclosed. The process provides the most thermodynamically stable polymorph by recrystallization of a novel polymorph.
    Type: Grant
    Filed: September 10, 2002
    Date of Patent: April 13, 2004
    Assignee: Sepracor Inc.
    Inventors: Gerald J. Tanoury, Chris H. Senanayake, Donald W Kessler
  • Patent number: 6706765
    Abstract: Aminoguanidine and alkoxyguanidine compounds, including compounds of the formula: wherein X is O or NR9 and R1-R4, R6-R9, R11, R12, Ra, Rb, Rc, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit proteolytic enzymes such as thrombin are described. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin, or are intermediates useful for forming compounds having antithrombotic activity.
    Type: Grant
    Filed: February 6, 2003
    Date of Patent: March 16, 2004
    Assignee: 3-Dimensional Pharmaceuticals, Inc.
    Inventors: Bruce E. Tomczuk, Richard M. Soll, Tianbao Lu, Cynthia L. Fedde, Carl R. Illig, Thomas P. Markotan, Thomas P. Stagnaro
  • Patent number: RE39072
    Abstract: The present invention relates to a compound of the general formula wherein R1, R2, R3 and R4 are each a hydrogen or an acyl, a pharmaceutically acceptable acid addition salt thereof or a hydrate thereof; a pharmaceutical comprising this compound; a pharmaceutical composition comprising this compound and a pharmaceutically acceptable carrier; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)propane-1,3-diol, the derivatives of the two compounds whose amino group and/or hydroxy group are(is) protected or a salt thereof. The compound of the present invention shows superior immunosuppressive action with less toxicity and higher safety, and is useful as a drug for prevention or suppression of rejection of organs or bone marrow transplantation, or as a drug for prevention or treatment of various autoimmune diseases or allergic diseases.
    Type: Grant
    Filed: April 3, 1998
    Date of Patent: April 18, 2006
    Assignee: Mitsubishi Pharma Corporation
    Inventors: Kunitomo Adachi, Yoshiyuki Aoki, Tokushi Hanano, Koji Teshima, Yukio Hoshino, Tetsuro Fujita