Ring Nitrogen Is Shared By Two Cyclos Patents (Class 544/282)
  • Patent number: 9896454
    Abstract: Compounds of the formula (I), wherein Y—X, R1, R2, R3, R4, R5, R6, R7, R8, A1, A2, A3, Ra and n areas defined in claim 1. Furthermore, the present invention relates to agrochemical compositions which comprise compounds of formula (I), to preparation of these compositions, and to the use of the compounds or compositions in agriculture or horticulture for combating, preventing or controlling infestation of plants, harvested food crops, seeds or non-living materials by phytopathogenic microorganisms, in particular fungi.
    Type: Grant
    Filed: February 26, 2015
    Date of Patent: February 20, 2018
    Assignee: Syngenta Participations AG
    Inventors: Laura Quaranta, Stephan Trah, Farhan Bou Hamdan, Clemens Lamberth
  • Patent number: 9108965
    Abstract: A compound of Formula 2 is disclosed wherein R1, MA and MB are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 1 wherein R1 and X are as defined in the disclosure comprising contacting a compound of Formula 2 with a halogenating agent. Also disclosed is a method for preparing a compound of Formula 4 wherein R1, R3 and R4 are as defined in the disclosure, comprising reacting a compound of Formula 5 wherein R3 and R4 are as defined in the disclosure with a compound of Formula 1, with a compound of Formula 1, the process of preparing the compound of Formula 4 includes the step of preparing the compound of Formula 1 from the compound of Formula 2 by the method disclosed above. Also disclosed is compound that is methyl 3,5-dichlorobenzeneethanimidate methyl 3,5-dichlorobenzeneethanimidate or ethyl 3,5-dichlorobenzeneethanimidate or salts thereof.
    Type: Grant
    Filed: December 13, 2012
    Date of Patent: August 18, 2015
    Assignee: E I DU PONT DE NEMOURS AND COMPANY
    Inventor: Wenming Zhang
  • Patent number: 9045486
    Abstract: The present invention relates to a compound having the general formula (I), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.
    Type: Grant
    Filed: January 7, 2014
    Date of Patent: June 2, 2015
    Assignees: Savira pharmaceuticals GmbH, European Molecular Biology Laboratory, F. Hoffman-La Roche AG
    Inventors: Andrea Wolkerstorfer, Oliver Szolar, Norbert Handler, Helmut Buschmann, Stephen Cusack, Mark Smith, Sung-Sau So, Ronald Charles Hawley, Achyutharao Sidduri, Zhuming Zhang
  • Patent number: 9040695
    Abstract: The present invention relates to a novel acid addition salt of risperidone, wherein acid counterion is selected from the group consisting of pamoic acid, caproic acid, cypionic acid, decanoic acid, camphor sulfonic acid, enanthic acid, palmitic acid, fusidic acid, gluceptic acid, gluconic acid, lactobionic acid, lauric acid, levulinic acid and valeric acid, a process for the preparation and pharmaceutical composition comprising the same. Further, the invention relates to the use of said pharmaceutical composition comprising the acid addition salt of risperidone in the treatment of patient suffering from psychotic disorders.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: May 26, 2015
    Assignee: TORRENT PHARMACEUTICALS LIMITED
    Inventors: Sunil Sadanand Nadkarni, Arunkumar Gupta, Manish Parikh, Jaya Abraham, Vivek Mishra
  • Patent number: 9018219
    Abstract: The present invention provides, for example, the following compound: wherein ring A is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle, X1—X2?X3 is CR5—CR6?CR7, N—CR6?CR7, CR5—N?CR7 or CR5—CR6?N, R1 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2a and R2b are each independently hydrogen, substituted or unsubstituted alkyl or the like, R4a, R4b, R5, R6 and R7 are each independently hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like, its pharmaceutically acceptable salt or a solvate thereof having an effect of inhibiting amyloid ? production, especially a BACE1 inhibitory activity, and useful as a medicament for treating diseases induced by production, secretion or deposition of amyloid ? proteins.
    Type: Grant
    Filed: October 27, 2011
    Date of Patent: April 28, 2015
    Assignee: Shionogi & Co., Ltd.
    Inventors: Moriyasu Masui, Genta Tadano
  • Patent number: 9018220
    Abstract: Disclosed are compounds of Formula 1, wherein X is O or S; Y is O or S; and R1, R2, R3 and R4 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: August 15, 2013
    Date of Patent: April 28, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: Caleb William Holyoke, Jr., Wenming Zhang
  • Publication number: 20150105549
    Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, X is CH or N; Y is C(O) or S(O)2; provided that when Y is S(O)2, then X is CH; A is a radical selected from the group consisting of and B1, B2, B3, T, R1, R2R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: KANU MAGANBHAI PATEL, Thomas Paul Selby, Brenton Todd Smith, Andrew Edmund Taggi, Patrick Ryan Kovacs
  • Patent number: 9006431
    Abstract: There is provided a hemihydrate form of the sodium salt of pemirolast.
    Type: Grant
    Filed: May 12, 2014
    Date of Patent: April 14, 2015
    Assignee: RSPR Pharma AB
    Inventors: Anett Perlberg, Martin Viertelhaus, Ulrika Rosenström, Karol Horvath
  • Patent number: 8999981
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications (including in particular diabetic retinopathy, nephropathy or neuropathy), cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, viral diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Grant
    Filed: January 6, 2012
    Date of Patent: April 7, 2015
    Assignees: Pfizer Inc., Pfizer Products Inc.
    Inventors: Iriny Botrous, Yufeng Hong, Hui Li, Kevin Kun-Chin Liu, Seiji Nukui, Min Teng, Eileen Valenzuela Tompkins, Chunfeng Yin
  • Publication number: 20150087832
    Abstract: The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.
    Type: Application
    Filed: October 22, 2012
    Publication date: March 26, 2015
    Applicant: MERCK SHARP & DOHME, CORP.
    Inventors: John Y.L. Chung, Kevin Campos, Edward Cleator, Robert F. Dunn, Andrew Gibson, R. Scott Hoerrner, Stephen Keen, Dave Liebermann, Zhuqing Liu, Joseph Lynch, Kevine M. Maloney, Feng Xu, Nobuyoshi Yasuda, Naoki Yoshikawa, Yong-Li Zhong
  • Publication number: 20150038329
    Abstract: Disclosed are compounds of Formula 1, wherein R1 is phenyl or pyridinyl, each optionally substituted with Q and up to 3 substituents independently selected from R2; each R2 is independently halogen, cyano, SF5, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C1-C4 alkylthio or C1-C4 haloalkylthio; and Q is phenyl or pyridinyl, each optionally substituted with up to 5 substituents independently selected from the group consisting of halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy and C1-C4 haloalkoxy. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: October 22, 2014
    Publication date: February 5, 2015
    Inventor: THOMAS FRANCIS PAHUTSKI, JR.
  • Patent number: 8940749
    Abstract: An improved process for the synthesis of 3-[2-[4-((6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]-pyrimidin-4-one (Paliperidone) and Paliperidone Palmitate through a novel intermediate (2-Chloroethyl)-6,7,8,9-tetrahydro-2-methyl-9-hydroxy-4H-pyrido [1,2-a]pyrimidine-4-one Palmitate ester.
    Type: Grant
    Filed: May 30, 2012
    Date of Patent: January 27, 2015
    Inventors: Ramamohan Rao Davuluri, Ravi Ponnaiah, Praveen Kumar Neela, Guruswamy Batthini, Telagareddy Venkata Narasimharao, Kosireddy Ravanababu, Kallepally Sudheer
  • Publication number: 20150011544
    Abstract: The compounds according to formula (VIII), their pharmaceutically acceptable acid or base addition salts, and the uses thereof. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for preparing medicaments for modulating estrogen related receptors (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity. The substituents of the formula are defined in the description.
    Type: Application
    Filed: July 2, 2014
    Publication date: January 8, 2015
    Inventors: Ke Ding, Chiwai Wong, Lijie Peng, Zhanfang Kang, Xi Zhou
  • Publication number: 20150005289
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.
    Type: Application
    Filed: February 8, 2013
    Publication date: January 1, 2015
    Inventors: Hongyan Qi, Soongyu Choi, Amal Dakka, Gary Mitchell Karp, Jana Narasimhan, Nikolai Naryshkin, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Matthew G. Woll, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Luke Green, Emmanuel Pinard, Hasane Ratni
  • Publication number: 20140378476
    Abstract: The present invention provides the use of certain compounds to treat peripheral or central pain syndrome and other disorders associated with the T-type calcium ion channels.
    Type: Application
    Filed: September 9, 2014
    Publication date: December 25, 2014
    Inventor: Jay Jie-Qiang Wu
  • Publication number: 20140378475
    Abstract: Disclosed are compounds of Formula (I) wherein: the two dotted lines represent either two single or two double bonds; Q is: R1 is F, Cl, —CN, or —CH3; R2 is Cl or —CH3; R3 is —C(CH3)2OH or —CH2CH2OH; Ra is H or —CH3; each Rb is independently F, Cl, —CH3, and/or —OCH3; and n is zero, 1, or 2. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Application
    Filed: June 25, 2014
    Publication date: December 25, 2014
    Inventors: Douglas G. Batt, Myra Beaudoin Bertrand, George Delucca, Michael A. Galella, Soo Sung Ko, Charles M. Langevine, Qingjie Liu, Qing Shi, Anurag S. Srivastava, Joseph A. Tino, Scott Hunter Watterson
  • Patent number: 8916586
    Abstract: A styrylquinoline derivative of structure I or IV or a benzodioxol isoquinoline of structure II or III for use in the treatment of an angiogenesis-related disease or disorder. The invention also provides a composition comprising a styrylquinoline derivative of structure I or IV or a benzodioxol isoquinoline of structure II or III for use as a medicament.
    Type: Grant
    Filed: January 16, 2012
    Date of Patent: December 23, 2014
    Assignee: University College Dublin—National University of Ireland, Dublin
    Inventors: Breandan Kennedy, Yolanda Alvarez, Jacintha O'Sullivan
  • Publication number: 20140343284
    Abstract: A compound of Formula 2 is disclosed wherein R1, MA and MB are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 1 wherein RI and X are as defined in the disclosure comprising contacting a compound of Formula 2 with a halogenating agent. Also disclosed is a method for preparing a compound of Formula 4 wherein R1, R3 and R4 are as defined in the disclosure, comprising reacting a compound of Formula 5 wherein R3 and R4 are as defined in the disclosure with a compound of Formula 1, with a compound of Formula 1, the process of preparing the compound of Formula 4 includes the step of preparing the compound of Formula 1 from the compound of Formula 2 by the method disclosed above. Also disclosed is compound that is methyl 3,5-dichlorobenzeneethanimidate methyl 3,5-dichlorobenzeneethanimidate or ethyl 3,5-dichlorobenzeneethanimidate or salts thereof.
    Type: Application
    Filed: December 13, 2012
    Publication date: November 20, 2014
    Inventor: Wenming Zhang
  • Patent number: 8883801
    Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: November 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lianyun Zhao, Duan Liu, Shuyi Tang, Amit K. Mandal, Umar Faruk Mansoor, Lalanthi Dilrukshi Vitharana, Panduranga Adulla P. Reddy, M. Arshad Siddiqui
  • Publication number: 20140329839
    Abstract: There is provided a hemihydrate form of the sodium salt of pemirolast.
    Type: Application
    Filed: May 12, 2014
    Publication date: November 6, 2014
    Applicant: CARDOZ AB
    Inventors: Anett Perlberg, Martin Viertelhaus, Ulrika Rosenström, Karol Horvath
  • Publication number: 20140315912
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor. (I).
    Type: Application
    Filed: July 18, 2011
    Publication date: October 23, 2014
    Inventors: Gregori J. Morriello, Harvey R. Wendt, Scott D. Edmondson
  • Patent number: 8859563
    Abstract: The present invention provides a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment or prophylaxis of a viral infection in a subject comprising administering to said subject an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative, salt or prodrug thereof. A pharmaceutical composition or medicament comprising a compound of Formula I is also provided.
    Type: Grant
    Filed: February 27, 2012
    Date of Patent: October 14, 2014
    Assignee: Avexa Limited
    Inventors: Eric Dale Jones, Jonathan Alan Victor Coates, David Ian Rhodes, John Joseph Deadman, Nicholas Andrew Van de Graff, Lisa Jane Winfield, Neeranat Thienthong, William Issa, Neil Choi, Katherine Macfarlane
  • Patent number: 8853197
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.
    Type: Grant
    Filed: June 3, 2014
    Date of Patent: October 7, 2014
    Assignee: Wockhardt Ltd.
    Inventors: Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Satish Bhawasar, Sachin Bhagwat, Mohammad Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Sanjeev Joshi
  • Patent number: 8853221
    Abstract: The compounds according to formula (VIII), their pharmaceutically acceptable acid or base addition salts, and the uses thereof. These compounds and their pharmaceutically acceptable acid or base addition salts can be used for preparing medicaments for modulating estrogen related receptors (ERR), and treating metabolic diseases, such as high blood fat, fatty liver, hyperglycemia, diabetes, obesity. The substituents of the formula are defined in the description.
    Type: Grant
    Filed: March 6, 2009
    Date of Patent: October 7, 2014
    Assignee: Guangzhou Institute of Biomedicine & Health, Chinese Academy of Sciences
    Inventors: Ke Ding, Chiwai Wong, Lijie Peng, Zhanfang Kang, Xi Zhou
  • Publication number: 20140296257
    Abstract: The present invention relates to water-soluble carrier-linked prodrugs of formula (I), wherein B, A and Hyp form the carrier, B is a branching core, each A is independently a poly(ethylene glycol)-based polymeric chain, each Hyp is independently a branched moiety, each SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, each D is independently a biologically active moiety, each x is independently 0 or 1, each m is independently an integer of from 2 to 64, n is an integer from 3 to 32; or the pharmaceutically acceptable salt thereof. It further relates to pharmaceutical compositions comprising said water-soluble carrier-linked prodrugs, their use as medicament or diagnostic, and methods of treatment.
    Type: Application
    Filed: August 10, 2012
    Publication date: October 2, 2014
    Applicant: Ascendis Pharma A/S
    Inventors: Ulrich Hersel, Guillaume Maitro, Harald Rau, Dirk Vetter
  • Patent number: 8846851
    Abstract: A salt catalyst comprises an ionic complex of i) a nitrogen base comprising one or more guanidine and/or amidine functional groups, and ii) an oxoacid comprising one or more active acid groups, the active acid groups independently comprising a carbonyl group (C?O), sulfoxide group (S?O), and/or a phosphonyl group (P?O) bonded to one or more active hydroxy groups; wherein a ratio of moles of the active hydroxy groups to moles of the guanidine and/or amidine functional groups is greater than 0 and less than 2.0. The salt catalysts are capable of catalyzing ring opening polymerization of cyclic carbonyl compounds.
    Type: Grant
    Filed: February 20, 2013
    Date of Patent: September 30, 2014
    Assignee: International Business Machines Corporation
    Inventors: Daniel J. Coady, Kazuki Fukushima, James L. Hedrick, Hans W. Horn, Julia E. Rice
  • Publication number: 20140243254
    Abstract: The present invention relates to water-soluble carrier-linked prodrugs of formula (I), wherein POL is a polymeric moiety, each Hyp is independently a hyperbranched moiety, each moiety SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, m is 0 or 1, each n is independently an integer from 2 to 200 and each x is independently 0 or 1. It further relates to pharmaceutical compositions comprising said water-soluble carrier-linked prodrugs and methods of treatment.
    Type: Application
    Filed: August 10, 2012
    Publication date: August 28, 2014
    Applicant: Ascendis Pharma A/S
    Inventors: Ulrich Hersel, Guillaume Maitro, Herald Rau, Tobias Voigt
  • Publication number: 20140235647
    Abstract: Disclosed are azaindazole compounds of Formula (I): or a pharmaceutically acceptable salt thereof, wherein: X is O and Y is N; or X is S and Y is CH; Z is CR2 or N; Q is a heteroaryl; and R1 is defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.
    Type: Application
    Filed: September 27, 2012
    Publication date: August 21, 2014
    Inventors: James Aaron Balog, Audris Huang, Upender Velaparthi, Peiying Liu
  • Publication number: 20140213767
    Abstract: The invention relates to compounds of Formula I, wherein L1, L2, and L3 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from paliperidone. The invention also relates to conjugates of a paliperidone hapten and a protein.
    Type: Application
    Filed: August 20, 2013
    Publication date: July 31, 2014
    Applicants: Ortho-Clinical Diagnostics, Inc., Janssen Pharmaceutica NV
    Inventors: Pieter Rik HASPESLAGH, Maarten Vliegen, Eric Hryhorenko, Thomas R. DeCory, Banumathi Sankaran
  • Publication number: 20140206681
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.
    Type: Application
    Filed: January 22, 2014
    Publication date: July 24, 2014
    Inventors: RONALD M. KIM, Jian Liu, Xiaolei Gao, Sobhana Babu Boga, Deodialsingh Guiadeen, Joseph A. Kozlowski, Wensheng Yu, Rajan Anand, Younong Yu, Oleg B. Selyutin, Ying-Duo Gao, Hao Wu, Shilan Liu, Chundao Yang, Hongjian Wang
  • Publication number: 20140206536
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; A is O, S, NR3e or C(R3c)?C(R3d); Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 1, 2 or 3; and R1, R2, R3a-R3e, R4, R5, R6, R7, R8, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: March 19, 2014
    Publication date: July 24, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: WENMING ZHANG, CALEB WILLIAM HOLYOKE, JR., KENNETH ANDREW HUGHES, GEORGE PHILIP LAHM, THOMAS FRANCIS PAHUTSKI, JR., MY-HANH THI TONG, MING XU
  • Patent number: 8785452
    Abstract: The present invention relates to 4H-pyrido[1,2-a]pyrimidin-4-one compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.
    Type: Grant
    Filed: June 17, 2009
    Date of Patent: July 22, 2014
    Assignees: Institut National de la Sante et de la Recherche Medicale, Institut Pasteur Korea
    Inventors: Priscille Brodin, Thierry Christophe, Zaesung No, Jaeseung Kim, Auguste Genovesio, Denis Philippe Cedric Fenistein, Heekyoung Jeon, Fanny Anne Ewann, Sunhee Kang, Saeyeon Lee, Min Jung Seo, Eunjung Park, Monica Contreras Dominguez, Ji Youn Nam, Eun Hye Kim
  • Publication number: 20140200228
    Abstract: The present invention provides a process for the preparation of paliperidone or a pharmaceutically acceptable salt thereof, wherein the process comprises condensing a compound of formula (II) with a compound of formula (III) or a salt thereof, in a suitable solvent and a base, in the presence of a catalyst and an inhibiting agent, wherein the inhibiting agent is added to the reaction system before the compound of formula (II) and compound of formula (III) have reacted or as the reaction of the compound of formula (II) and compound of formula (III) is initiated, and optionally converting the paliperidone to a salt thereof, wherein X is a suitable leaving group. The present invention also provides substantially pure paliperidone or a salt thereof, paliperidone or a salt thereof as prepared by the process and uses of the paliperidone or salt thereof.
    Type: Application
    Filed: May 30, 2012
    Publication date: July 17, 2014
    Applicant: CIPLA LIMITED
    Inventors: Ravikumar Puppala, Srinivas Laxminarayan Pathi, Rajendra Narayanrao Kankan
  • Publication number: 20140187776
    Abstract: Disclosed are compositions comprising (a) at least one compound selected from compounds of Formula 1, N-oxides, and salt thereof, wherein R1 is phenyl optionally substituted with up to 5 substituents independently selected from R3, or pyridinyl optionally substituted with up to 4 substituents independently selected from R3; R2 is C1-C4 haloalkyl; or thiazolyl, pyridinyl or pyrimidinyl, each optionally substituted with up to 2 substituents independently selected from the group consisting of halogen and C1-C4 alkyl; each R3 is independently halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, C1-C4 haloalkoxy, C(R4)?NOR4 or Q; each R4 is independently C1-C4 alkyl; Z is CH?CH or S; and each Q is independently phenyl or pyridinyl, each optionally substituted with up to 3 substituents independently selected from the group consisting of halogen, cyano, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy and C1-C4 haloalkoxy; and (b) at least one invertebrate pest control agent.
    Type: Application
    Filed: February 20, 2014
    Publication date: July 3, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: CALEB WILLIAM HOLYOKE, JR., WENMING ZHANG, MY-HANH THI TONG, THOMAS FRANCIS PAHUTSKI, JR.
  • Patent number: 8754089
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: June 17, 2014
    Assignee: Amgen Inc.
    Inventors: Timothy David Cushing, Xiaolin Hao, Julia Winslow Lohman, Youngsook Shin
  • Publication number: 20140163009
    Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.
    Type: Application
    Filed: January 23, 2012
    Publication date: June 12, 2014
    Applicant: CHDI Foundation
    Inventors: Christopher A Luckhurst, Alen F Haughan, Perla Breccia, Andrew J Stott, Roland W Burli, Samantha J Hughes, Ignacio Munoz-Sanjuan, Celia Dominguez
  • Publication number: 20140155585
    Abstract: The invention relates to compounds of Formula I, wherein R1 and R2 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from risperidone and paliperidone. The invention also relates to conjugates of a risperidone or paliperidone hapten and a protein.
    Type: Application
    Filed: August 20, 2013
    Publication date: June 5, 2014
    Applicants: Ortho-Clinical Diagnostics, Inc., Janssen Pharmaceutica NV
    Inventors: Pieter Rik HASPESLAGH, Maarten VLIEGEN, Eric HRYHORENKO, Thomas R. DeCORY, Banumathi SANKARAN
  • Publication number: 20140148431
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.
    Type: Application
    Filed: August 24, 2012
    Publication date: May 29, 2014
    Inventors: Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Satish Bhawsar, Sachin Bhagwat, Mohammed Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Sanjeev Joshi
  • Patent number: 8722690
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein X is O or S; Y is O or S; A is O, S, NR3e or C(R3c)?C(R3d); Z is a direct bond, O, S(O)n, NR6, C(R7)2O, OC(R7)2, C(?X1), C(?X1)E, EC(?X1), C(?NOR8) or C(?NN(R6)2); a is 1, 2 or 3; and R1, R2, R3a-R3e, R4, R5, R6, R7, R8, X1 and E are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: May 13, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Wenming Zhang, Caleb William Holyoke, Jr., Kenneth Andrew Hughes, George Philip Lahm, Thomas Francis Pahutski, Jr., My-Hanh Thi Tong, Ming Xu
  • Publication number: 20140107128
    Abstract: Novel heterocyclic compounds having the Formula I: wherein A, B, D, E, G, K, L, M, Q, T, X, Y and Z are as defined herein, which exhibit a dopamine receptor (preferably a D4 receptor) agonistic activity, and/or a PDE5 inhibitory activity, processes of preparing same, pharmaceutical compositions containing same and uses thereof in the treatment of sexual disorders such as decreased libido, orgasm disorder and erectile dysfunction are disclosed.
    Type: Application
    Filed: December 17, 2013
    Publication date: April 17, 2014
    Inventors: Dmitry TWOROWSKI, Ron Matsievitch, Vladimir Kogan
  • Publication number: 20140088120
    Abstract: The present specification discloses compositions comprising at least one therapeutic compound capable of modulating androgen production and methods and uses for treating a disorder associated with androgen production using such compositions and/or compounds.
    Type: Application
    Filed: September 26, 2013
    Publication date: March 27, 2014
    Applicant: TANGENT REPROFILING LIMITED
    Inventors: Suzanne Dilly, Gregory Stoloff, Paul Taylor
  • Publication number: 20140088122
    Abstract: The present invention relates generally to the field of treatment and prophylaxis of retinal degenerative diseases. More particularly, the present invention contemplates a method for preventing, reducing the risk of development of, or otherwise treating or ameliorating the symptoms of, age-related macular degeneration (AMD) or related retinal conditions in mammals and in particular humans. The present invention further provides therapeutic compositions enabling dose-dependent or dose-specific administration of agents useful in the treatment and prophylaxis of age-related macular degeneration or related retinal degenerative conditions.
    Type: Application
    Filed: November 22, 2013
    Publication date: March 27, 2014
    Applicant: PRANA BIOTECHNOLOGY LIMITED
    Inventors: Penelope Jane HUGGINS, Gaik Being KOK
  • Publication number: 20140073787
    Abstract: An improved process for the synthesis of 3-[2-[4-((6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]-pyrimidin-4-one (Paliperidone) and Paliperidone Palmitate through a novel intermediate (2-Chloroethyl)-6,7,8,9-tetrahydro-2-methyl-9-hydroxy-4H-pyrido [1,2-a]pyrimidine-4-one Palmitate ester.
    Type: Application
    Filed: May 30, 2012
    Publication date: March 13, 2014
    Inventors: Ramamohan Rao Davuluri, Ravi Ponnaiah, Praveen Kumar Neela, Guruswamy Batthini, Telagareddy Venkata Narasimharao, Kosireddy Ravanababu, Kallepally Sudheer
  • Patent number: 8653260
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: June 20, 2012
    Date of Patent: February 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Ding-Ming Shen, Liping Wang, Cheng Zhu
  • Publication number: 20140045864
    Abstract: The present invention relates to a novel acid addition salt of risperidone, wherein acid counterion is selected from the group consisting of pamoic acid, caproic acid, cypionic acid, decanoic acid, camphor sulfonic acid, enanthic acid, palmitic acid, fusidic acid, gluceptic acid, gluconic acid, lactobionic acid, lauric acid, levulinic acid and valeric acid, a process for the preparation and pharmaceutical composition comprising the same. Further, the invention relates to the use of said pharmaceutical composition comprising the acid addition salt of risperidone in the treatment of patient suffering from psychotic disorders.
    Type: Application
    Filed: April 25, 2012
    Publication date: February 13, 2014
    Applicant: TORRENT PHARMACEUTICALS LIMITED
    Inventors: Sunil Sadanand Nadkarni, Arunkumar Gupta, Manish Parikh, Jaya Abraham, Vivek Mishra
  • Publication number: 20140031206
    Abstract: Substituted imine compounds of formula (I), wherein D is C(R2)?N˜Z—R1 or C(?Y1)NRAY2RB and the other symbols have the meanings given in the description, their N-oxides and salts are useful for combating animal pests.
    Type: Application
    Filed: April 4, 2012
    Publication date: January 30, 2014
    Applicant: BASF SE
    Inventors: Joachim Dickhaut, Florian Kaiser, Arun Narine, Wolfgang Von Deyn, Karsten Koerber, Prashant Deshmukh, Gemma Veitch, Nina Gertrud Bandur, Juergen Langewald, Deborah L. Culbertson
  • Patent number: 8614219
    Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein Y, R1, R2, R3, and R4 are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates thereof and their use in therapeutics.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: December 24, 2013
    Assignees: Sanofi-aventis, Mitsubishi Tanabe Pharma Corporation
    Inventors: Aude Fayol, Alistair Lochead, Mourad Saady, Julien Vache, Philippe Yaiche
  • Publication number: 20130338002
    Abstract: Disclosed are compounds of Formula 1, wherein X is O or S; Y is O or S; and R1, R2, R3 and R4 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: August 15, 2013
    Publication date: December 19, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: CALEB WILLIAM HOLYOKE, JR., WENWING ZHANG
  • Publication number: 20130296319
    Abstract: The invention provides a compound of Formula (I) or a pharmaceutically acceptable salt of the compound, wherein R1, R2, R3 and R4 are as described herein; pharmaceutical compositions thereof and the use thereof in treating diseases, conditions or disorders modulated by the inhibition of an acetyl-CoA carboxylase enzyme(s) in an animal.
    Type: Application
    Filed: July 11, 2013
    Publication date: November 7, 2013
    Inventors: Scott William Bagley, David Andrew Griffith, Daniel Wei-Shung Kung
  • Publication number: 20130289052
    Abstract: Disclosed is an arthropod pest control composition having an excellent controlling effect on arthropod pests, which comprises a compound represented by formula (I): wherein each symbol is as defined in the present description; and metalaxyl or metalaxyl M.
    Type: Application
    Filed: February 18, 2011
    Publication date: October 31, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Norihisa Sakamoto, Emiko Sakamoto, Atsushi Iwata