Five-membered Hetero Ring Having Two Or More Ring Hetero Atoms Of Which At Least One Is Nitrogen Patents (Class 544/132)
  • Patent number: 9913853
    Abstract: The present invention relates to stable pharmaceutical compositions of fosaprepitant or a salt thereof in the form of ready-to-use or ready-to-dilute compositions suitable for parenteral administration.
    Type: Grant
    Filed: November 3, 2016
    Date of Patent: March 13, 2018
    Assignee: Cipla Limited
    Inventors: Geena Malhotra, Sarabjit Singh, Abhijit Jadhav
  • Patent number: 9340697
    Abstract: In accordance with some embodiments, compositions and methods for forming solvent-based and water-based carbon nanotubes inks with removable additives are provided. In some embodiments, an ink composition is provided that includes a plurality of carbon nanotubes, a solvent, and a triazole-based removable additive, where the plurality of carbon nanotubes are dispersed within the solvent and wherein the triazole-based removable additive stabilizes the plurality of carbon nanotubes that are dispersed in the solvent.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: May 17, 2016
    Assignee: NANO-C, INC.
    Inventors: Ramesh Sivarajan, Henning Richter, Viktor Vejins
  • Patent number: 9227958
    Abstract: An amorphous form of aprepitant and a process for its preparation is provided. Also provided are mixtures of polymorph Forms I and II of aprepitant and a process for the preparation thereof.
    Type: Grant
    Filed: February 2, 2007
    Date of Patent: January 5, 2016
    Assignee: Glenmark Pharmaceuticals Limited
    Inventors: Mangesh Shivram Sawant, Girish Dixit, Nitin Sharad Chandra Pradhan, Mubeen Ahmad Khan, Sukumar Sinha
  • Patent number: 9029369
    Abstract: A 1:1:1 aprepitant L-proline H2O composition and a 1:1:1 aprepitant L-proline H2O cocrystal are disclosed as well as pharmaceutical compositions containing a 1:1:1 aprepitant L-proline H2O composition or cocrystal and a pharmaceutically acceptable carrier. The 1:1:1 aprepitant L-proline H2O composition or cocrystal may be used in the same way as aprepitant to treat or prevent disorders relating to emesis, a neuropsychiatric disease, an inflammatory disease, pairs, cancer, a skin disease, itch, a respiratory disease, or an addiction.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: May 12, 2015
    Assignee: Nuformix Limited
    Inventors: Joanne Holland, Christopher Frampton, Alan Chorlton, Daniel Gooding
  • Publication number: 20150119395
    Abstract: The present invention relates to novel triazole Hsp90 inhibitors that possess significant inhibitory activity against Hsp90, which are suitable for the treatment of hyperproliferative diseases such as cancer, infections, immune disorders, inflammation, and CNS related disorders. Furthermore, pharmaceutical compositions, including combination products, are also provided in the present application. Further provided are methods of using the pharmaceutical compositions and/or combination products.
    Type: Application
    Filed: April 4, 2013
    Publication date: April 30, 2015
    Inventors: Dinesh U. Chimmanamada, Weiwen Ying
  • Publication number: 20150111893
    Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.
    Type: Application
    Filed: May 9, 2013
    Publication date: April 23, 2015
    Inventors: Vincent P. Sandanayaka, Sharon Shechter, Sharon Shacham, Dilara McCauley, Erkan Baloglu
  • Publication number: 20150094284
    Abstract: A series of S-triazolyl ?-mercaptoacetanilides having general structure (1) are provided, where Q is CO2H, CONR2, SO3H, or SO2NR2. The compounds inhibit several variants of the reverse transcriptase of HIV, and are useful in the treatment of HIV infections.
    Type: Application
    Filed: December 3, 2014
    Publication date: April 2, 2015
    Inventors: Jean-Luc GIRARDET, Yung-Hyo KOH, Martha DE LA ROSA, Esmir GUNIC, Zhi HONG, Stanley LANG, Woo-Hong KIM
  • Publication number: 20150087828
    Abstract: A molecule with neural activities, especially 4-substituent-2-hydroxymorpholin-3-one, as a new intermediate of neurokinin-1 receptor antagonist aprepitant, and preparation method thereof.
    Type: Application
    Filed: April 15, 2013
    Publication date: March 26, 2015
    Applicants: Zhejiang Hisun Pharmaceutical Co., Ltd., Shanghai Institute of Pharmaceutical Industry
    Inventors: Fuli Zhang, Chonghao Liu, Pengcheng Qiu, Jian Chai, Qingfeng Cai
  • Publication number: 20150065506
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted tetrazolyl, R2 is optionally substituted phenyl, optionally substituted pyridinyl or optionally substituted thienyl, and R3, R4, R5, R6 R7 and R8 are as defined herein. Also provided are methods of using the compounds for treating diseases associated with the P2X3 and/or a P2X2/3 receptor antagonist and methods of making the compounds.
    Type: Application
    Filed: August 13, 2014
    Publication date: March 5, 2015
    Applicant: ROCHE PALO ALTO LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • 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
  • Patent number: 8940890
    Abstract: Disclosed is a synthesis method of a compound of formula 1,5-[[2(R)-[1(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxyl]-3(S)-4-fluorophenyl-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazole-3-one (i.e. aprepitant), which comprises cyclizing a compound of formula 4 in a solvent, wherein R is C1-C5 alkyl. The intermediate for preparing aprepitant is also disclosed. The present method is especially suitable for industrial production of aprepitant.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: January 27, 2015
    Assignee: Chengdu DI'AO Pharmaceutical Group Co., Ltd.
    Inventors: Jianxin Ji, Qiang Zhang, Fengtian Du, Yi Jin, Tao Zhang, Na Guo, Xiaowei Yan, Yongrongn Yang, Bogang Li
  • Patent number: 8927548
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Grant
    Filed: January 13, 2012
    Date of Patent: January 6, 2015
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, David James, Shijie Zhang, Junghyun Chae, Teresa Kowalczyk-Przewloka, Howard P. Ng, Hao Li, Zachary Demko, Dinesh U. Chimmanamada, Chi-wan Lee, Zhenjian Du, Kevin Foley, Minghu Song, Lijun Sun, Keizo Koya, Dan Zhou, Shuzhen Qin
  • Publication number: 20140371222
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: August 29, 2014
    Publication date: December 18, 2014
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Lijun Sun, Weiwen Ying, Junghyun Chae, Teresa Kowalczyk-Prezewloka, Shijie Zhang, Dinesh U. Chimmanamada, Kevin Paul Foley, Zhenjian Du, Hao Li, David James, Howard P. Ng, Zachary Demko, Dan Zhou, Shuzhen Qin
  • Publication number: 20140364603
    Abstract: In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
    Type: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes
  • Publication number: 20140343060
    Abstract: Aprepitant L-proline solvate compositions and aprepitant L-proline solvate cocrystals are disclosed as well as pharmaceutical compositions containing them. The compositions and cocrystals of the invention are: 1:1:1 aprepitant L-proline methanol composition; a 1:1:1 aprepitant L-proline methanol cocrystal; a 1:1:1:1 aprepitant L-proline ethanol composition; a 1:1:1 aprepitant L-proline ethanol cocrystal; l 1:1:1 aprepitant L-proline n-propanol composition; and a 1:1:1 aprepitant L-proline n-propanol cocrystal: The aprepitant L-proline solvate compositions or cocrystals may be used in the same way as aprepitant to treat or prevent disorders relating to emesis, a neuropsychiatric disease, an inflammatory disease, pain, cancer, a skin disease, itch a respiratory disease, or an addiction.
    Type: Application
    Filed: November 21, 2012
    Publication date: November 20, 2014
    Inventors: Joanne Holland, Christopher Frampton, Alan Chorlton, Daniel Gooding
  • Patent number: 8889673
    Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of JAK kinase activity in a patient are disclosed.
    Type: Grant
    Filed: June 21, 2012
    Date of Patent: November 18, 2014
    Assignee: Genentech, Inc.
    Inventors: Bing-Yan Zhu, Michael Siu, Steven R. Magnuson, Richard Pastor, He Haiying, Xiao Yisong, Zheng Jifu, Xu Xing, Zhao Junping, Wendy Liu
  • Publication number: 20140329812
    Abstract: The present invention relates to aryl triazole derivatives of Formula I having antitumoural activity through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical composition containing such compounds.
    Type: Application
    Filed: December 13, 2011
    Publication date: November 6, 2014
    Applicant: SIGMA-TAU RESEARCH SWITZERLAND S.A.
    Inventors: Giuseppe Giannini, Walter Cabri, Loredana Vesci, Maria Luisa Cervoni, Claudio Pisano, Maurizio Taddei, Serena Ferrini
  • Publication number: 20140322247
    Abstract: Disclosed herein are immunoconjugates comprising an inhibitor of Eg5 linked to an antigen binding moiety such as an antibody, that are useful for treating cell proliferative disorders. Also disclosed are novel inhibitors of Eg5 that can be used either alone or as part of an immunoconjugate to treat cell proliferation disorders. The Eg5 inhibitors include compounds of this formula as described herein: The invention further provides pharmaceutical compositions comprising these compounds and immunoconjugates, and compositions comprising the immunoconjugates or compounds with a therapeutic co-agent, and methods to use these compounds, conjugates and compositions for treating cell proliferation disorders.
    Type: Application
    Filed: March 13, 2014
    Publication date: October 30, 2014
    Applicant: NOVARTIS AG
    Inventors: Paul A. Barsanti, Sylvie Chamoin, Lionel Doumampouom-Metoul, Stephanie Guerro-Lagasse, Robert Martin Grotzfeld, Alexei Karpov, Marc Lafrance, Cristina Montserrat Nieto-Oberhuber, Grazia Piizzi
  • Publication number: 20140288301
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 25, 2014
    Inventors: Dinesh U. Chimmanamada, Joseph A. Burlison, Weiwen Ying, Lijun Sun, Stefan M. Schweizer, Shijie Zhang, Zachary Demko, David James, Teresa Kowalczyk-Przewloka
  • Patent number: 8816072
    Abstract: The present invention provides a process for preparation of crystalline aprepitant having not more than 15% by weight of Form I content which comprises, a) dissolving aprepitant in a suitable solvent to obtain a solution, b) cooling the solution to 10-15° C., c) optionally seeding the solution with aprepitant Form I crystals, d) adding an anti-solvent to the solution, and e) isolating crystalline aprepitant having not more than 15% by weight of Form I content.
    Type: Grant
    Filed: June 2, 2010
    Date of Patent: August 26, 2014
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Deepak Mohanlal Jain, Maneck Khurana, Hiten Sharadchandra Mehta, Abhay Tatiya, Asok Nath, Sanjay Mahadeo Gade, Mohan Prasad, Subhash Dhar
  • Publication number: 20140179699
    Abstract: The present invention relates to compounds useful as inhibitors of indoleamine 2,3-dioxygenase (IDO). The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications. The compounds of this invention have formula I-A: wherein the variables are as defined herein.
    Type: Application
    Filed: November 19, 2013
    Publication date: June 26, 2014
    Inventors: Dean Boyall, Christopher Davis, James Dodd, Simon Everitt, Andrew Miller, Peter Weber, James Westcott, Stephen Young
  • Publication number: 20140107337
    Abstract: The present invention provides a novel process for reducing palladium content in fosaprepitant dimeglumine.
    Type: Application
    Filed: May 21, 2012
    Publication date: April 17, 2014
    Applicant: HETERO RESEARCH FOUNDATION
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivasa Rao, Bandi Vamsi Krishna
  • Publication number: 20140100213
    Abstract: This invention relates to the use of triazolone derivatives for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.
    Type: Application
    Filed: November 4, 2013
    Publication date: April 10, 2014
    Applicant: GlaxoSmithKline LLC
    Inventors: Nicholas David Adams, Christopher Joseph Aquino, Amita M. Chaudhari, Jonathan Michael Chergurovich, Terence John Kiesow, Cynthia Ann Parrish, Alexander Joseph Reif, Kenneth Wiggall
  • Patent number: 8680269
    Abstract: The present invention concerns novel heteroaryl-N-aryl thiosemicarbazones and their use in pest control, as insecticides and aca?cides This invention also includes preparation of the pesticide compositions containing the compounds, and methods of controlling insects using the compounds.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: March 25, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Annette V. Brown, Gary D. Crouse, Thomas C. Sparks, CaSandra L. McLeod, Emily M. Rigsbee, William T. Lambert, Noormohamed M. Niyaz
  • Publication number: 20140080826
    Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.
    Type: Application
    Filed: September 25, 2013
    Publication date: March 20, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: SARA SABINA HADIDA RUAH, Peter Diederik Jan Grootenhuis, Frederick F. Van Goor, Jinglan Zhou, Brian Richard Bear, Mark Thomas Miller, Jason Mc Cartney, Mehdi Numa, Xiaoqing Yang
  • Publication number: 20140072532
    Abstract: Compounds, compositions and methods are provided for the prophylaxis and treatment of infections caused by viruses of the Pneumovirinae subfamily of Paramyxoviridae and diseases associated with such infection.
    Type: Application
    Filed: October 11, 2013
    Publication date: March 13, 2014
    Applicant: MICRODOSE THERAPEUTX, INC.
    Inventors: Theodore J. Nitz, Janet A. Gaboury, Christopher J. Burns, Sylvie Laguerre, Daniel C. Pevear, Thomas A. Lessen, David J. Rys
  • Publication number: 20140066443
    Abstract: The present invention is directed to aminomethyl biaryl benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Application
    Filed: April 30, 2012
    Publication date: March 6, 2014
    Inventors: Douglas C. Beshore, Robert M. Garbaccio, Scott D. Kuduk, Adam W. Johnson, Jason W. Skudlarek
  • Publication number: 20140056880
    Abstract: The present invention provides triazole compounds of Formula I: as further described herein. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, and a method of treating a disorder mediated, at least in part, by KSP in a mammalian patient comprising administering to a mammalian patient in need of such treatment a therapeutically effective amount of a compound of Formula I.
    Type: Application
    Filed: August 28, 2013
    Publication date: February 27, 2014
    Applicant: NOVARTIS AG
    Inventors: Tinya Abrams, Paul Barsanti, Yu Ding, David Duhl, Wooseok Han, Cheng Hu, Yue Pan
  • Publication number: 20140018318
    Abstract: The present invention provides inhibitors of a wide variety of serine hydrolase enzymes. The inhibitors of the present invention are N1- and N2-carbamoyl-1,2,3-triazole compounds such as those of Formula (I): in which N1, N2, and N3 are the nitrogen atoms at positions 1, 2, and 3, respectively, of the triazole ring, and R4, R5, R6 and R7 in Formula (I) are as described herein. Methods of inhibiting serine hydrolase enzymes and methods of preparing carbamoyl-1,2,3-triazole compounds also are described.
    Type: Application
    Filed: April 5, 2012
    Publication date: January 16, 2014
    Applicant: The Scipps Research Institute
    Inventors: Benjamin Cravatt, Alexander Adibekian, Katsunori Tsuboi, Ku-Lung Hsu
  • Publication number: 20140010783
    Abstract: The present invention discloses compounds of Formula I: wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection.
    Type: Application
    Filed: July 2, 2013
    Publication date: January 9, 2014
    Inventors: Joseph A. Bilotta, Zhi Chen, Elbert Chin, Qingjie Ding, Shawn D. Erickson, Stephen D. Gabriel, Klaus G. Klumpp, Han Ma, Eric Mertz, Jean-Marc Plancher, Robert J. Weikert
  • Patent number: 8623844
    Abstract: The present invention generally relates to a process for the preparation of fosaprepitant dimeglumine intermediate and its use in the preparation of fosaprepitant dimeglumine; to a neutral form of fosaprepitant in a solid state and processes for the preparation thereof; and to a stable amorphous fosaprepitant dimeglumine, having a stability at temperatures of about 2° C. to about 8° C. and at a relative humidity below at least 60%; and a process for the preparation thereof.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: January 7, 2014
    Inventors: Navin Ganesh Bhatt, Nikhil Rasiklal Trivedi, Mahesh Khedekar, Sukumar Sinha, Mubeen Ahmed Khan, Ramjilal Yadav
  • Patent number: 8618285
    Abstract: Novel triazole derivatives of the formula (I), in which R1-R6, and Y have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: January 25, 2006
    Date of Patent: December 31, 2013
    Assignee: Merck Patent GmbH
    Inventors: Hans-Michael Eggenweiler, Michael Wolf
  • Publication number: 20130345418
    Abstract: The present invention relates to a process for obtaining pure aprepitant substantially free of undesired diastereomeric isomer, namely 5-[2(S)-[1(RS)-[3,5-bis(trifluoromethyl)-phenypethoxy]-3-(S)-(4-fluorophenyl)-morpholin-4-yl-methyl]-3,4-dihydro-2H-1,2,4-triazol-3-one. The present invention further provides an improved process for preparation of aprepitant crystalline form II. The present invention also relates to novel amorphous form of aprepitant, a process for its preparation and to a pharmaceutical composition comprising it. The present invention further relates to aprepitant having a mean particle size of less than about 11.5 microns, a process for its preparation and to a pharmaceutical composition comprising it. Thus, for example, aprepitant having a content of diastereomeric impurity of 1.1% is dissolved in ethyl acetate at 70° C., the solution is concentrated to half the initial volume by distilling off ethyl acetate, and the resulting solid is collected at 0-5° C.
    Type: Application
    Filed: April 29, 2013
    Publication date: December 26, 2013
    Applicant: HETERO DRUGS LIMITED
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Thungathurthy Srinivasa Rao
  • Publication number: 20130317031
    Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.
    Type: Application
    Filed: May 9, 2013
    Publication date: November 28, 2013
    Applicant: Karyopharm Therapeutics Inc.
    Inventor: Karyopharm Therapeutics Inc.
  • Publication number: 20130303493
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a pharmaceutical composition comprising such a compound.
    Type: Application
    Filed: July 12, 2013
    Publication date: November 14, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Joseph Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Patent number: 8557810
    Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: October 15, 2013
    Assignee: Ambit Biosciences Corporation
    Inventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
  • Patent number: 8546374
    Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.
    Type: Grant
    Filed: July 9, 2012
    Date of Patent: October 1, 2013
    Assignee: Abbvie Inc.
    Inventors: William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biquin C. Li
  • Publication number: 20130252949
    Abstract: A 1:1:1 aprepitant L-proline H20 composition and a 1:1:1 aprepitant L-proline H20 cocrystal are disclosed as well as pharmaceutical compositions containing a 1:1:1 aprepitant L-proline H20 composition or cocrystal and a pharmaceutically acceptable carrier. The 1:1:1 aprepitant L-proline H20 composition or cocrystal may be used in the same way as aprepitant to treat or prevent disorders relating to emesis, a neuropsychiatric disease, an inflammatory disease, pairs, cancer, a skin disease, itch, a respiratory disease, or an addiction.
    Type: Application
    Filed: September 23, 2011
    Publication date: September 26, 2013
    Applicant: NUFORMIX LIMITED
    Inventors: Joanne Holland, Christopher Frampton, Alan Chorlton, Daniel Gooding
  • Publication number: 20130217689
    Abstract: This invention provides compounds of formula I: wherein R1, R2, CY, Y1, Y2, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: April 1, 2013
    Publication date: August 22, 2013
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventor: Millennium Pharmaceuticals, Inc.
  • Publication number: 20130210796
    Abstract: The present invention relates to novel tetrazole compounds; to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.
    Type: Application
    Filed: July 8, 2011
    Publication date: August 15, 2013
    Inventors: Paul Beswick, Robert James Gleave, Shuji Hachisu, Sadie Vile, Nicholas Bertheleme, Simon E. Ward
  • Publication number: 20130209521
    Abstract: The present invention is directed to nanostructured Aprepitant compositions, process for the preparation thereof and pharmaceutical compositions containing them. The nanoparticles of Aprepitant according to the invention have an average particle size of less than about 200 nm. The stable nanostructured particles of the invention are presented by increased solubility, dissolution rate, permeability and bioequivalent or enhanced biological performance characterized by significantly decreased fed/fasted effect compared to the reference and marketed drug. Aprepitant is a chemical compound that belongs to a class of drugs called substance P antagonists (SPA). It mediates its effect by acting on neurokinin 1 receptor. Aprepitant is manufactured by Merck & Co. under the brand name Emend for prevention of acute and delayed chemotherapy-induced nausea and vomiting (CINV) and for prevention of postoperative nausea and vomiting.
    Type: Application
    Filed: June 17, 2011
    Publication date: August 15, 2013
    Inventors: Genovéva Filipcsei, Zsolt Ötvös, Gábor Heltovics, Ferenc Darvas
  • Publication number: 20130197217
    Abstract: The present invention provides a 1,2,4-triazolone derivative represented by Formula (1A) having an antagonistic activity on the arginine-vasopressin 1b receptor or a pharmaceutically acceptable salt thereof and provides a pharmaceutical composition comprising the compound or the salt as an active ingredient, in particular, a therapeutic or preventive agent exhibiting favorable pharmacokinetics in a disease such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, or alopecia.
    Type: Application
    Filed: September 30, 2011
    Publication date: August 1, 2013
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Takeshi Kuwada, Mitsukane Yoshinaga, Tomoko Ishizaka, Daisuke Wakasugi, Shin-ichi Shirokawa, Nobutaka Hattori, Youichi Shimazaki, Naoki Miyakoshi
  • Publication number: 20130158018
    Abstract: Disclosed are Cathepsin-S reversible inhibitor compounds of the formula (I) which are useful in the treatment of autoimmune and other diseases. Also disclosed are pharmaceutical compositions containing the same, and methods of making and using the same.
    Type: Application
    Filed: March 2, 2011
    Publication date: June 20, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Michael J. Burke, Derek Cogan, Donghong Amy Gao, Alexander Heim-Riether, Eugene Richard Hickey, Matthew Russell Netherton, Philip Dean Ramsden, David Charles Thompson, Zhaoming Xiong
  • Patent number: 8450353
    Abstract: Topical compositions and methods of use to treat symptoms of reduced skin elasticity are provided comprising desthiobiotin and certain desthiobiotin analogues. These compounds are effective in stimulating LOXL-1 activity and can thus increase elastin remodeling and improve appearance of fine lines, wrinkles, skin sagging and other symptoms of reduced elastin function.
    Type: Grant
    Filed: November 19, 2008
    Date of Patent: May 28, 2013
    Assignee: Avon Products, Inc.
    Inventors: Dmitri S. Ptchelintsev, Xiaochun Luo, Siming W. Chen
  • Publication number: 20130116252
    Abstract: Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.
    Type: Application
    Filed: November 7, 2012
    Publication date: May 9, 2013
    Applicant: NIPPON KAYAKU KABUSHIKI KAISHA
    Inventor: NIPPON KAYAKU KABUSHIKI KAISHA
  • Publication number: 20130116431
    Abstract: Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.
    Type: Application
    Filed: November 5, 2012
    Publication date: May 9, 2013
    Applicant: Nippon Kayaku Kabushiki Kaisha
    Inventor: Nippon Kayaku Kabushiki Kaisha
  • Publication number: 20130109853
    Abstract: Disclosed is a synthesis method of a compound of formula 1,5-[[2(R)-[1(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxyl]-3(S)-4-fluorophenyl-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazole-3-one (i.e. aprepitant), which comprises cyclizing a compound of formula 4 in a solvent, wherein R is C1-C5 alkyl. The intermediate for preparing aprepitant is also disclosed. The present method is especially suitable for industrial production of aprepitant.
    Type: Application
    Filed: May 20, 2011
    Publication date: May 2, 2013
    Inventors: Jianxin Ji, Qiang Zhang, Fengtian Du, Yi Jin, Tao Zhang, Na Guo, Xiaowei Yan, Yongrong Yang, Bogang Li
  • Publication number: 20130102568
    Abstract: [PROBLEMS] The present invention provides a novel alkoxyimino derivative or a salt thereof, as well as to a pest control agent containing the derivative or salt thereof as an active ingredient, which shows an excellent pest control effect on a wide range of pests in the agricultural and horticultural field and is also capable of controlling resistant pests. [MEANS FOR SOLVING PROBLEMS] The novel alkoxyimino derivative is characterized by being represented by general formula [I] (in the formula, X, R1, R2 and Q are as defined in the specification) and the post control agent is characterized by containing as an active ingredient the alkoxyimino derivative or a salt thereof.
    Type: Application
    Filed: June 21, 2011
    Publication date: April 25, 2013
    Applicant: Kumiai Chemical Industry Co., Ltd. and Ihara Chemical Industry Co., Ltd.
    Inventors: Shunichirou Fukumoto, Daisuke Shikama, Keiji Toriyabe, Toshihiro Nagata, Masaaki Komatsu, Takeshi Matsuda, Yuki Nakano
  • Publication number: 20130072461
    Abstract: The present invention relates to substituted triazole compounds and compositions comprising substituted triazole compounds. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted triazole compound of the invention, or a composition comprising such a compound.
    Type: Application
    Filed: November 13, 2012
    Publication date: March 21, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventor: Synta Pharmaceuticals Corp.
  • Patent number: 8399464
    Abstract: Disclosed is a triazole derivative(s) represented by the general formula (1) below or a pharmacologically acceptable salt(s) thereof. Also disclosed are a prodrug(s) of such a triazole derivative(s) and an HSP90 inhibitor(s) containing any one of them as an active constituent. (1) (In the formula, X represents a halogen atom, an optionally substituted alkyl group, an optionally substituted alkynyl group or the like; Y represents a mercapto group, a hydroxyl group, an optionally substituted sulfonyl group, an optionally substituted amino group or the like; and R represents an optionally substituted aryl or alkyl group or the like.
    Type: Grant
    Filed: March 8, 2006
    Date of Patent: March 19, 2013
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Hiroshi Kuramochi, Setsuko Niitsuma, Masaharu Nakamura, Yoshitaka Sato, Seiichi Saito, Arihiro Tomura, Yuh-ichiro Ichikawa, Yousuke Kasuga