The Additional Hetero Ring Is A 1,3 Diazine Ring Patents (Class 514/252.14)
  • Patent number: 10358421
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.
    Type: Grant
    Filed: September 11, 2017
    Date of Patent: July 23, 2019
    Assignee: REGENACY PHARMACEUTICALS, LLC
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 10301302
    Abstract: The present invention relates to crystalline 1,2-Propanediol solvate of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide compound of formula-1b, its process for the preparation and its use in the preparation of anhydrous crystalline form (N-6) and monohydrate of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxy ethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide. [formula] 1,2-Propanediol solvate Formula-1b.
    Type: Grant
    Filed: June 27, 2016
    Date of Patent: May 28, 2019
    Assignee: MSN LABORATORIES PRIVATE LIMITED
    Inventors: Srinivasan Thirumalai Rajan, Sajja Eswaraiah, Gutta Madhusudhan, Peri Seetha Rama Sarma, Mogal Khalil Ahamed
  • Patent number: 10246470
    Abstract: The present invention relates to a compound (3S)-3-(4-((3-(6-Oxa-3-azabicyclo[3.1.1]heptan-3-ylmethyl)benzyl)oxy)phenyl)hex-4-ynoic acid methods for use of this and other compounds.
    Type: Grant
    Filed: June 7, 2018
    Date of Patent: April 2, 2019
    Assignee: CADILA HEALTHCARE LIMITED
    Inventors: Ranjit C. Desai, Brijeshkumar Srivastava
  • Patent number: 10239837
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: March 26, 2019
    Assignee: REGENACY PHARMACEUTICALS, LLC
    Inventors: John H. van Duzer, Ralph Mazitschek
  • Patent number: 10011609
    Abstract: The present invention relates to novel GPR 40 agonists of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.
    Type: Grant
    Filed: November 3, 2014
    Date of Patent: July 3, 2018
    Assignee: CADILA HEALTHCARE LIMITED
    Inventors: Ranjit C. Desai, Brijeshkumar Srivastava
  • Patent number: 9969723
    Abstract: The present invention relates to a novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient for the prevention and treatment of metabolic disease. The novel 3-(4-(benzyloxy)phenyl)hex-4-inoic acid derivative, the optical isomer thereof, or the pharmaceutically acceptable salt thereof of the present invention has excellent activities of activating GPR40 protein and promoting insulin secretion accordingly but has no toxicity when co-administered with other drugs.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: May 15, 2018
    Assignee: HYUNDAI PHARM CO., LTD
    Inventors: Jin Yang, Jin Woong Kim, Han Kyu Lee, Jae Hyun Kim, Chang Mo Son, kyu hwan Lee, Hyung-Ho Choi, daehoon Kim, Tae-Young Ha, Jaekeol Rhee
  • Patent number: 9795588
    Abstract: A method for inhibiting mammalian TOR in a cell, comprising: providing a compound of formula (1): and incubating the cell with the compound. Also provided is a method for extending life span of a subject, comprising: providing the compound; and administering the compound to the subject. Yet also provided is a method for treating a mammalian TOR activation-caused disease in a subject, comprising: providing the compound; and administering the compound to the subject.
    Type: Grant
    Filed: August 2, 2016
    Date of Patent: October 24, 2017
    Assignee: Chang Gung University
    Inventors: Chin-Chuan Chen, Yann-Lii Leu, Shu-Huei Wang
  • Patent number: 9701680
    Abstract: The present invention relates to novel pyrimidine and pyridine compounds of formula (I) or a pharmaceutical acceptable salt thereof, wherein R1, R2, R3, R4, R5, X, Y and G are as defined in the description, to pharmaceutical compositions containing them, a process for preparing them, and their use in therapy of a disease responsive to inhibition of FGFR, for example, cancer.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: July 11, 2017
    Assignee: HUTCHISON MEDIPHARMA LIMITED
    Inventors: Wei-Guo Su, Weihan Zhang, Jinshui Li
  • Patent number: 9532970
    Abstract: Compositions comprising LSF compositions and treatment regiments comprising administration of LSF containing compositions are disclosed. Compositions and/or regiments may optionally include the administration of vitamins, minerals, and anti-oxidants. Methods for using these compositions and treatment regimens for treating subjects for diseases, including diseases associated with inflammation and/or oxidative stress, are provided. Various methods for use of the LSF compositions for inhibition of histone deacetylases (HDACs) in various cells, tissues, and/or conditions are also provided.
    Type: Grant
    Filed: July 8, 2015
    Date of Patent: January 3, 2017
    Inventors: Darlene E. McCord, Thomas Karagiannis
  • Patent number: 9376396
    Abstract: The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: June 28, 2016
    Assignees: ABBVIE DEUTSCHLAND GMBH & CO. KG, ABBVIE INC.
    Inventors: Andreas Haupt, Jürgen Dinges, Liliane Unger, Karsten Wicke, Robert van Waterschoot, Scott Mittelstadt, Karla Drescher, Ana Relo
  • Patent number: 9278963
    Abstract: Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with HDAC activity, particularly diseases or disorders that involve activity of HDAC1, HDAC2, and/or HDAC6. Also provided herein are methods for inhibiting migration of a neuroblastoma cell, inducing maturation of a neuroblastoma cell, and altering cell cycle progression of a neuroblastoma cell comprising administering to the cell a therapeutically effective amount of a HDAC1, HDAC2, and/or HDAC6 selective inhibitor or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 9, 2014
    Date of Patent: March 8, 2016
    Assignee: Acetylon Pharmaceuticals, Inc.
    Inventors: John H. van Duzer, Ralph Mazitschek, Simon Stewart Jones, Min Yang, David Lee Tamang
  • Patent number: 9238632
    Abstract: Disclosed in the present invention is a 3-cyanoanilinoalkylarylpiperazine derivatives and use thereof in preparing drugs; the 3-cyanoanilinoalkylarylpiperazine derivatives disclosed by the present invention has very useful pharmaceutical properties and good tolerance, especially the use as novel analgesic drugs, novel antidepressants, and novel analgesic and antidepressive drugs. This class of compounds are central analgesics regulating 5-hydroxytrptamine, and also are novel antidepressants regulating 5-hydroxytrptamine. This class of compounds also has less toxic and side effects and a higher safety range.
    Type: Grant
    Filed: April 9, 2013
    Date of Patent: January 19, 2016
    Assignees: NHWA Pharma, Corporation, Shanghai Institute of Pharmaceutical Industry
    Inventors: Jianqi Li, Guan Wang, Guisen Zhang, Yali Li, Xiangqing Xu, Xiaowen Chen, Shicheng Liu, Song Zhao, Minquan Yu
  • Patent number: 9180386
    Abstract: The present invention relates to the use and to a process involving at least one calix[n]arene derivative substituted by at least one acid functional group on the upper face and at least one aliphatic chain of variable length on the other face, as an additive for crystallization of a polar and/or positively charged molecule. The use and the process of the present invention have the advantage of enabling, facilitating and/or accelerating the crystallization of polar and/or positively charged molecules, especially of membrane proteins that are in solution or soluble, which had previously proved to be very difficult.
    Type: Grant
    Filed: April 2, 2010
    Date of Patent: November 10, 2015
    Assignees: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE—CNRS—, UNIVERSITE CLAUDE BERNARD LYON 1
    Inventors: Pierre G. Falson, Anthony W. Coleman, Rachel Rima Matar Merheb, Antoine Leydier, Frederic Huche
  • Publication number: 20150141434
    Abstract: The invention provides compounds that are useful as sodium channel blockers. In one aspect, the invention provides compounds of Formula I: or pharmaceutically acceptable salts, solvates, hydrates, or diastereomers thereof, wherein R1, R4, X, G, n, p, W1, W2, W3, W4, and the E ring are defined in the disclosure. In certain embodiments, the invention provides compounds of Formulae II-XIII as set forth supra. The invention also provides the use of compounds of any of the above discussed formulae to treat a disorder responsive to blockade of sodium channels. In one embodiment, Compounds of the Invention are useful for treating pain.
    Type: Application
    Filed: September 5, 2014
    Publication date: May 21, 2015
    Inventor: Jae Hyun Park
  • Patent number: 9034850
    Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: May 19, 2015
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
  • Patent number: 9035096
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: May 19, 2015
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C. B. Harriman, Zhan Shi, B. Shaowu Chen
  • Publication number: 20150133441
    Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.
    Type: Application
    Filed: June 6, 2014
    Publication date: May 14, 2015
    Inventor: Gerard M. Housey
  • Patent number: 9029381
    Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.
    Type: Grant
    Filed: November 21, 2011
    Date of Patent: May 12, 2015
    Assignee: Astrazeneca AB
    Inventors: James Arnold, Todd Andrew Brugel, Scott Throner, Steven Wesolowski, Phil Edwards, Andrew Griffin, Thierry Groblewski, Denis Labrecque
  • Publication number: 20150126500
    Abstract: Provided are piperazinyl pyrimidine derivatives of formula I having CCR4 antagonism, and the preparation method, pharmaceutical composition and use thereof in the preparation of a medicament. The medicament is useful for the treatment and prevention of CCR4-related diseases.
    Type: Application
    Filed: January 15, 2013
    Publication date: May 7, 2015
    Inventors: Song Li, Ying Wang, Junhai Xiao, Dalong Ma, Hongwei Gong, Hui Qi, Lili Wang, Xiaomei Ling, Zhibing Zheng, Yang Zhang, Wu Zhong, Meina Li, Yunde Xie, Enquan Xu, Xingzhou Li, Jing Ma, Guoming Zhao, Xinbo Zhou, Xiaokui Wang, Hongying Liu
  • Publication number: 20150126494
    Abstract: A method for treating a disease characterized by excessive lipofuscin accumulation in the retina in mammals afflicted therewith, comprising administering to the mammal an effective amount of a non-retinoid antagonist compound or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 30, 2013
    Publication date: May 7, 2015
    Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Konstantin Petrukhin, Janet R. Sparrow, Rando Allikmets
  • Publication number: 20150126504
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Application
    Filed: January 12, 2015
    Publication date: May 7, 2015
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
  • Publication number: 20150126484
    Abstract: The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: September 12, 2012
    Publication date: May 7, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Lizbeth Celeste Deselm, Yufang Xiao, Hui Qiu, Constantin Neagu, Igor Mochalkin, Theresa L. Johnson
  • Patent number: 9023834
    Abstract: This invention relates to a pharmaceutical kit containing a lyophilized preparation of a pyrimidine compound described in the specification. Also disclosed is a lyophilization process for making this preparation.
    Type: Grant
    Filed: November 12, 2009
    Date of Patent: May 5, 2015
    Assignee: TaiGen Biotechnology Co., Ltd.
    Inventors: Chi-Feng Yen, Judy Yuan, Chi-Hsin Richard King
  • Publication number: 20150111892
    Abstract: The present invention concerns, in a first aspect, compounds of Formula I as defined herein, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing such compounds. The present invention also relates to compounds of Formula I for use as acid ceramidase inhibitors, and in the treatment of cancer and other disorders in which modulation of the levels of ceramide is clinically relevant.
    Type: Application
    Filed: May 27, 2013
    Publication date: April 23, 2015
    Inventors: Daniele Piomelli, Natalia Realini, Marco Mor, Chiara Pagliuca, Daniela Pizzirani, Rita Scarpelli, Tiziano Bandiera
  • Patent number: 9012461
    Abstract: A compound of the formula (I): where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
    Type: Grant
    Filed: July 6, 2012
    Date of Patent: April 21, 2015
    Assignee: Cancer Therapeutics CRC Pty Ltd
    Inventors: Ian Peter Holmes, Ylva Bergman, Gillian Elizabeth Lunniss, Marica Nikac, Neil Choi, Catherine Fae Hemley, Scott Raymond Walker, Richard Charles Foitzik, Danny Ganame, Romina Lessene
  • Patent number: 9011911
    Abstract: The present invention pertains to a high drug load tablet comprising an active ingredient Compound I of formula or a pharmaceutically acceptable salt thereof in an amount from about 30% to 80% in weight of the active moiety based on the total weight of the tablet.
    Type: Grant
    Filed: January 23, 2014
    Date of Patent: April 21, 2015
    Assignee: Novartis AG
    Inventors: Christian-Peter Luftensteiner, Jean-Claude Bianchi, Joerg Ogorka, Oskar Kalb
  • Publication number: 20150105399
    Abstract: Disclosed in the present invention is a 3-cyanoanilinoalkylarylpiperazine derivatives and use thereof in preparing drugs; the 3-cyanoanilinoalkylarylpiperazine derivatives disclosed by the present invention has very useful pharmaceutical properties and good tolerance, especially the use as novel analgesic drugs, novel antidepressants, and novel analgesic and antidepressive drugs. This class of compounds are central analgesics regulating 5-hydroxytrptamine, and also are novel antidepressants regulating 5-hydroxytrptamine. This class of compounds also has less toxic and side effects and a higher safety range.
    Type: Application
    Filed: April 9, 2013
    Publication date: April 16, 2015
    Inventors: Jianqi Li, Guan Wang, Guisen Zhang, Yali Li, Xiangqing Xu, Xiaowen Chen, Shicheng Liu, Song Zhao, Minquan Yu
  • Publication number: 20150105400
    Abstract: The present invention provides a novel therapeutic drug for cerebral infarction, which contains a piperazine compound as an active ingredient. The compound of the present invention can be provided as a novel therapeutic drug for cerebral infarction having an effect of suppressing brain injury volume or improving neurological deficit, since it suppresses production of plural inflammatory cytokines and chemokines present in the brain such as TNF-?, IL-1?, IL-6 and MCP-1 and the like.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: Mitsubishi Tanabe Pharma Corporation
    Inventors: Haruto NAKAGAWA, Naoko ANDO
  • Publication number: 20150105397
    Abstract: The present inventions relate to substituted piperazine derivatives of general formula (I) and to the manufacture of said compounds, pharmaceutical compositions comprising a compound according to general formula (I), and the use of said compounds for the treatment of various medical conditions related to glycine transporter-1 (GlyT1).
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Christoph HOENKE, Riccardo GIOVANNINI, Uta LESSEL, Holger ROSENBROCK, Bernhard SCHMID
  • Patent number: 9006243
    Abstract: HIV replication inhibitors of formula R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2, R3, R6 and R7 are hydrogen; hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(?O)R9; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 and R5 are hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; formyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(?O)R9; cyano; —S(?O)rR9; —NH—S(?O)2R9; —NHC(?O)H; —C(?O)NHNH2; —NHC(?O)R9; Het; —Y-Het; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R5 is pyridyl, —C(?O)NR5aR5b; —CH(OR5c)R5d; —CH2—NR5eR5f; —CH?NOR5a; —CH2—O—C2-6alkenyl; —CH2—O—P(?O)(OR5g)2; —CH2—O—C(?O)—NH2; —C(?O)—R5d; X is —NR1—, —O—, —CH2—, —S—; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compou
    Type: Grant
    Filed: December 28, 2007
    Date of Patent: April 14, 2015
    Assignee: Janssen R&D Ireland
    Inventors: Jerôme Emile Georges Guillemont, Céline Isabelle Mordant
  • Publication number: 20150099749
    Abstract: This invention concerns pyrimidine derivatives of formula having HIV (Human Immunodeficiency Virus) replication inhibiting properties, the preparation thereof and pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 9, 2015
    Inventors: Jerôme Emile Georges Guillemont, Mikaël Paugam, Bruno François Marie Delest
  • Patent number: 8999974
    Abstract: The present invention relates to acyl piperazine derivatives which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved.
    Type: Grant
    Filed: August 9, 2011
    Date of Patent: April 7, 2015
    Assignee: Raqualia Pharma Inc.
    Inventors: Mikiko Morita, Shuzo Watanabe
  • Publication number: 20150087645
    Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.
    Type: Application
    Filed: October 7, 2014
    Publication date: March 26, 2015
    Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
  • Publication number: 20150087639
    Abstract: The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.
    Type: Application
    Filed: July 18, 2013
    Publication date: March 26, 2015
    Applicant: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Yingjun Zhang, Jiancun Zhang, Xiaojun Wang, Runfeng Lin, Shengtian Cao, Zhaohe Wang, Jing Li
  • Publication number: 20150080396
    Abstract: The invention concerns compounds of Formula (I): wherein L1, R1, R2, R3, R4 and X are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of disease, for example cancer.
    Type: Application
    Filed: August 26, 2014
    Publication date: March 19, 2015
    Applicants: DAINIPPON SUMITOMO PHARMA CO., LTD., ASTRAZENECA AB
    Inventors: Nicholas James Bennett, Stephen Thom, Thomas McInally
  • Publication number: 20150080365
    Abstract: This invention relates to certain heteroaryl compounds for use as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of helminth infections and the treatment of parasitosis caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.
    Type: Application
    Filed: March 27, 2013
    Publication date: March 19, 2015
    Inventors: Michael Berger, Marko Eck, Christopher Kern
  • Patent number: 8980890
    Abstract: The invention relates to compounds and methods for treating cell proliferation disorders.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: March 17, 2015
    Assignee: Kinex Pharmaceuticals, LLC
    Inventor: David G. Hangauer, Jr.
  • Publication number: 20150072019
    Abstract: The present invention relates generally to 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimid-4-yl}-1-methyl-urea or a pharmaceutically acceptable salt or solvate thereof or a pharmaceutical composition comprising 3-(2,6-Dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimid-4-yl)-1-methyl-urea or a pharmaceutically acceptable salt or solvate thereof for use in the treatment of X-linked hypophosphatemic rickets (XLH), autosomal dominant hypophosphatemia rickets (ADHR), autosomal recessive hypophosphatemic rickets (ARHR), tumor-induced osteomalacia, post-renal transplant hypophosphatemia, epidermal nevus syndrome, osteoglophonic dysplasia or McCune-Albright syndrome.
    Type: Application
    Filed: March 29, 2013
    Publication date: March 12, 2015
    Inventors: Michaela Kneissel, Vito Gaugnano, Diana Graus Porta, Simon Wöhrle
  • Patent number: 8975249
    Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.
    Type: Grant
    Filed: October 31, 2011
    Date of Patent: March 10, 2015
    Assignee: Celgene Avilomics Research, Inc.
    Inventors: Kwangho Lee, Deqiang Niu, Russell C. Petter, Matthew F. Baevsky, Juswinder Singh
  • Publication number: 20150051195
    Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
    Type: Application
    Filed: October 30, 2014
    Publication date: February 19, 2015
    Inventors: Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
  • Patent number: 8957215
    Abstract: The present invention relates to novel heteroaryl substituted benzothiazole derivatives, precursors thereof, and therapeutic uses for such compounds, having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. Furthermore, the invention relates to novel heteroaryl substituted benzothiazole derivatives that are suitable for imaging amyloid deposits in living patients, their compositions, methods of use and processes to make such compounds. More specifically, the present invention relates to a method of imaging amyloid deposits in brain in vivo to allow antemortem diagnosis of Alzheimer's disease as well as measuring clinical efficacy of Alzheimer's disease therapeutic agents.
    Type: Grant
    Filed: April 23, 2012
    Date of Patent: February 17, 2015
    Assignee: Navidea Biopharmaceuticals, Inc.
    Inventors: Ylva Gravenfors, Catrin Jonasson, Jonas Malmstrom, Gunnar Nordvall, David Pyring, Can Slivo, Daniel Sohn, Peter Strom, David Wensbo
  • Publication number: 20150045344
    Abstract: The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.
    Type: Application
    Filed: October 23, 2014
    Publication date: February 12, 2015
    Inventors: Franz VON NUSSBAUM, Dagmar KARTHAUS, Sonja ANLAUF, Martina DELBECK, Volkhart Min-Jian LI, Daniel MEIBOM, Klemens LUSTIG, Jens SCHAMBERGER
  • Publication number: 20150045370
    Abstract: The present invention relates to the discovery that salt inducible kinases (SIKs) suppress the formation of anti-inflammatory molecules such as IL-10, which are important for the resolution of inflammation and identifies SIK inhibitors that may be used to treat disorders associated with undesirable inflammation, such as inflammatory bowel disease and/or autoimmune disorders.
    Type: Application
    Filed: March 13, 2013
    Publication date: February 12, 2015
    Inventors: Philip Cohen, Kristopher Clark, Hwan Geun Choi, Nathanael Gray
  • Publication number: 20150038481
    Abstract: Described are compounds of Formula I or Formula II: wherein: ring A is a 5- or 6-membered heteroaryl group; dashed lines are optional double bonds; X is N or O; Y is a carbon atom or an S or N heteroatom in ring A in any suitable location; and substituents are as given herein. Compositions containing the same and methods of using the same in treating cancers such as acute lymphoblastic leukemia are also described.
    Type: Application
    Filed: May 21, 2013
    Publication date: February 5, 2015
    Inventors: Xiaodong Wang, Weihe Zhang, Dmitri Kireev, Dehui Zhang, Andrew Mclver
  • Patent number: 8946413
    Abstract: There is provided a compound of Formula I(a) or I(b): or a pharmaceutically acceptable salt thereof, wherein the various substitutents are defined herein.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: February 3, 2015
    Assignee: Pfizer Inc.
    Inventors: Robert O. Hughes, Rajesh V. Devraj, Donald J. Rogier, John I. Trujillo, Steve R. Turner, Wei Huang
  • Patent number: 8937070
    Abstract: The present invention is directed to methods of inhibiting syk and/or JAK kinase activity, methods of inhibiting platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma with compounds of the formula: and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof.
    Type: Grant
    Filed: June 13, 2013
    Date of Patent: January 20, 2015
    Assignee: Portola Pharmaceuticals, Inc.
    Inventors: Shawn M. Bauer, Anjali Pandey
  • Publication number: 20150018349
    Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: March 27, 2014
    Publication date: January 15, 2015
    Applicant: University of Utah Research Foundation
    Inventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
  • Publication number: 20150011561
    Abstract: The present invention provides a compound of formula (I) or a salt form thereof. The compound of formula (I) has ALK and FAK inhibitory activity, and may be used to treat proliferative disorders.
    Type: Application
    Filed: September 2, 2014
    Publication date: January 8, 2015
    Inventors: Shawn P. Allwein, Laurent Courvoisier, Martin J. Jacobs, Gregory R. Ott
  • Publication number: 20150011560
    Abstract: The present invention relates to the treatment or prevention of skeletal disorders, in particular skeletal diseases, developed by patients that display abnormal increased activation of the fibroblast growth factor receptor 3 (FGFR3), in particular by expression of a constitutively activated mutant or FGFR3.
    Type: Application
    Filed: December 12, 2012
    Publication date: January 8, 2015
    Inventor: Laurence Legeai-Mallet
  • Publication number: 20150005297
    Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.
    Type: Application
    Filed: September 12, 2014
    Publication date: January 1, 2015
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi