Plural Nitrogens In The Additional Five-membered Hetero Ring Patents (Class 514/254.05)
  • Patent number: 10596169
    Abstract: This invention provides a novel cancer treatment method in which plinabulin (t-butyl-dehydrophenylahistin or NPI-2358) and a taxane compound (such as docetaxel) are used in combination. Our study has shown that the optimum combination of injecting plinabulin after taxane compound has unexpected enhanced efficacy in large tumor populations in animal model and in NSCLC cancer patients compared to taxane compound treatment alone. In addition, this optimum combination can achieve unexpected safety effect in lowering unbearable side effects of taxane compound, including decreasing its neutropenia rates at all grades and decreasing G-CSF use in cancer patients.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: March 24, 2020
    Assignee: BeyondSpring Inc.
    Inventor: Lan Huang
  • Patent number: 10265303
    Abstract: The present invention relates to compounds of formula (I) as defined in the specification for use as pharmacological chaperones having a stabilizing effect on phenylalanine hydroxylase (PAH) for the treatment of hyperphenylalaninemia (HPA), in particular phenylketonuria (PKU). The compounds include trimethoprim and analogues and derivatives thereof.
    Type: Grant
    Filed: August 11, 2016
    Date of Patent: April 23, 2019
    Assignee: BERGEN TEKNOLOGIOVERFØRING AS
    Inventors: Aurora Martinez, Oscar Aubi Catevilla, Lars Skjærven, Jarl Underhaug, Ming Ying, Knut Teigen
  • Patent number: 10206401
    Abstract: The present invention relates to novel pyridine compounds of the formulae I and II, to their salts, to their tautomers, to their N-oxides, and to the salts of these N-oxides or tautomers. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests. The invention also relates to a method for controlling invertebrate pests by using these compounds. The invention further relates to plant propagation material and to agricultural compositions comprising said compounds wherein A is a radical of the formulae A1, A2, A3, A4, A5 or A6 wherein # denotes the binding site to the remainder of formulae I or II; Z is O, S or N—RN; X1 is S, O or NRa; X2 is OR2a, NR2bR2c, S(O)mR2d; X3 is a lone pair or oxygen; R1, R2 and R3 are, inter alia, hydrogen, and RA1, RA2 RA3 RA4, RA5, RA6 and RN, are as defined in claim 1.
    Type: Grant
    Filed: November 7, 2017
    Date of Patent: February 19, 2019
    Assignee: BASF SE
    Inventors: Sebastian Soergel, Christian Defieber, Ronan Le Vezouet, Steffen Gross, Karsten Koerber, Deborah L. Culbertson, Douglas D. Anspaugh
  • Patent number: 10189818
    Abstract: The disclosure herein includes 5-(5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-ylamino)pyrazine-2-carbonitrile (S)-lactate monohydrate that inhibits Chk1/2 and is useful in the treatment of cancer.
    Type: Grant
    Filed: December 1, 2016
    Date of Patent: January 29, 2019
    Assignee: Eli Lilly and Company
    Inventor: Alessandra B. Ennett-Shepard
  • Patent number: 10111861
    Abstract: This disclosure describes the use of one or more compounds that fall within the scope of one or more structural formula I, II, III, IV, V, or VI for treating triple negative breast cancer. Compounds useful for treating breast cancer include those compounds of formulae I, II, III, IV, V, or VI that inhibit proliferation of breast cancer cells and/or lead to the death of breast cancer cells, especially triple negative breast cancer.
    Type: Grant
    Filed: December 9, 2016
    Date of Patent: October 30, 2018
    Assignees: Medivation Prostate Therapeutics, Inc., The Regents of the University of Colorado, a Body Corporate
    Inventors: Andrew A. Protter, Jennifer Richer, Dawn Cochrane
  • Patent number: 9963433
    Abstract: A novel class of drugs for treating androgen receptor (AR) positive cancer including prostate cancer and breast cancer are described. The drugs include the chemical scaffolds of a high affinity androgen receptor ligand and a histone deacetylase inhibitor. Also described are compositions including the novel drugs and methods of treating AR positive cancer using the compositions.
    Type: Grant
    Filed: January 27, 2017
    Date of Patent: May 8, 2018
    Assignee: Wayne State University
    Inventor: Zhihui Qin
  • Patent number: 9862706
    Abstract: Imidazolone and pyrazolone derivatives of formula (I) described herein exhibit human neutrophil elastase inhibitory properties and are useful for the therapy of diseases and conditions in which HNE is implicated.
    Type: Grant
    Filed: May 26, 2017
    Date of Patent: January 9, 2018
    Assignee: CHIESI FARMACEUTICI S.p.A.
    Inventors: Carmelida Capaldi, Elisabetta Armani, Andrew Stephen Robert Jennings
  • Patent number: 9730924
    Abstract: The invention provides a method of treating T-cell mediated diseases and a method of inhibiting the activation of T-cells using certain diketopiperazines. The invention also provides methods of synthesizing diketopiperazines and pharmaceutical compositions comprising certain diketopiperazines. The invention further provides methods of making improved pharmaceutical compositions of proteins and peptides by either increasing or decreasing the content of diketopiperazines in the compositions and the resultant improved pharmaceutical compositions.
    Type: Grant
    Filed: March 3, 2015
    Date of Patent: August 15, 2017
    Assignee: Ampio Pharmaceuticals, Inc.
    Inventors: David Bar-Or, Raphael Bar-Or, Richard Shimonkevitz
  • Patent number: 9688640
    Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.
    Type: Grant
    Filed: June 26, 2015
    Date of Patent: June 27, 2017
    Assignee: ASTRAZENECA AB
    Inventors: David Buttar, Kevin Michael Foote, Maria-Elena Theoclitou, Andrew Peter Thomas
  • Patent number: 9650415
    Abstract: A uric acid-lowering agent containing, as an active ingredient, a tyrosine-containing cyclic dipeptide selected from the group consisting of cyclotryptophanyltyrosine, cycloseryltyrosine, cycloprolyltyrosine, cyclotyrosylglycine, cyclotyrosyltyrosine, cyclophenylalanyltyrosine, cycloleucyltyrosine, cyclolysyltyrosine, cyclohistidyltyrosine, cycloalanyltyrosine, cycloglutamyltyrosine, cyclovalyltyrosine, cycloisoleucyltyrosine, cyclothreonyltyrosine, cycloaspartyltyrosine, cycloasparaginyltyrosine, cycloglutaminyltyrosine, cycloarginyltyrosine, cyclomethionyltyrosine, and cyclotyrosylcysteine, or a salt thereof. The uric acid-lowering agent of the present invention has an excellent action of lowering a uric acid level, and the uric acid-lowering agent is useful in, for example, prevention or treatment of hyperuricemia, gout or the like.
    Type: Grant
    Filed: June 20, 2014
    Date of Patent: May 16, 2017
    Assignee: Suntory Holdings Limited
    Inventors: Toshihide Suzuki, Shinya Fukizawa, Yoshinori Beppu, Hiroshi Watanabe
  • Patent number: 9486445
    Abstract: Treatment of proliferative diseases with a combination of a b-Raf inhibitor and MDM2 inhibitor.
    Type: Grant
    Filed: July 22, 2015
    Date of Patent: November 8, 2016
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Brian Higgins, Kenneth Kolinsky, Gwen Nichols, Kathryn Packman, Fei Su
  • Patent number: 9365542
    Abstract: The present invention provides compounds useful as modulators, agonists or antagonists of androgen receptor (AR), compositions thereof, and methods of making and using the same. Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful in medicine, and particularly for treating any of a variety of diseases, disorders or conditions.
    Type: Grant
    Filed: October 25, 2013
    Date of Patent: June 14, 2016
    Assignee: Memorial Sloan-Kettering Cancer Center
    Inventors: Minna D. Balbas, Michael J. Evans, Charles L. Sawyers, Yang Shen, David Hosfield, Geoffrey L. Greene
  • Patent number: 9216170
    Abstract: Treatment of proliferative diseases with a combination of a b-Raf inhibitor and MDM2 inhibitor.
    Type: Grant
    Filed: February 5, 2013
    Date of Patent: December 22, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Brian Higgins, Kenneth Kolinsky, Gwen Nichols, Kathryn Packman, Fei Su
  • Patent number: 9062007
    Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
    Type: Grant
    Filed: January 6, 2014
    Date of Patent: June 23, 2015
    Assignees: Merck Sharp & Dohme Corp., Pharmacopeia Drug Discovery, Inc.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey H. Lowrie, Kurt W. Saionz, Suresh D. Babu
  • Publication number: 20150148330
    Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 28, 2015
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
  • Patent number: 9040539
    Abstract: A process for the preparation of a chiral compound, in particular posaconazole, wherein the process comprises mixing and reacting the compounds of formula (I) Y3—NH2; of formula (IIa) 0=C?N—Y0 and/or of formula (IIb) and of formula (III) in a solvent in any order to obtain a reaction mixture containing a chiral compound of formula (IV) and/or formula (V).
    Type: Grant
    Filed: May 18, 2011
    Date of Patent: May 26, 2015
    Assignee: SANDOZ AG
    Inventors: Michael Oberhuber, Joerg Salchenegger, Dominic De Souza, Martin Albert, Thorsten Wilhelm, Martin Langner, Hubert Sturm, Hans-Peter Spitzenstaetter
  • Publication number: 20150133468
    Abstract: A compound of formula (I) is useful as an antiviral agent, in particular for the treatment of influenza. A method for preparing the compound of formula (I) and a composition including the compound of formula (I) are described.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Applicant: VIRONOVA AB
    Inventors: Mohammed Homman, Ngarita Kingi, Jan Bergman, Robert Berg
  • Publication number: 20150133422
    Abstract: The present invention embodiments relate to compound of Formula I or pharmaceutically acceptable enantiomers, salts or solvates thereof. The invention further relates in certain embodiments to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates in certain embodiments to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also relates in certain embodiments to a process for manufacturing compounds of Formula I.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 14, 2015
    Inventors: Stefano Crosignani, Sandra Cauwenberghs, Frederik Deroose
  • 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
  • Patent number: 9029356
    Abstract: Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: May 12, 2015
    Assignee: Nerviano Medical Sciences S.R.L.
    Inventors: Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
  • Publication number: 20150126364
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Q is and Z1, Z2, J1, J2, M, R1a, R1b, R2a, R2b, R2c, R2d, R14 and R14a 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: May 13, 2013
    Publication date: May 7, 2015
    Applicant: E I Du Pont de Nemours and Company
    Inventors: Thomas Francis Pahutski, JR., Matthew James Campbell, Dominic Ming-Tak Chan, Jeffrey Keith Long, Thomas Martin Stevenson
  • 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: 20150126499
    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: January 7, 2015
    Publication date: May 7, 2015
    Inventors: Joseph Burlison, Shijie Zhang, Weiwen Ying, Dinesh U. Chimmanamada, Minghu Song, Junghyun Chae, Stefan M. Schweizer
  • Patent number: 9023790
    Abstract: The present invention relates to aqueous solutions useful as pharmaceutical compositions of posaconazole for intravenous administration. These compositions include a solubilizing agent, such as a modified ?-cyclodextrin in an acidified solution, which can also include a chelating agent such as disodium edetate (EDTA). In clinical trials, a 200 mg posaconazole dose of the selected composition was found to achieve acceptable pharmacokinetic properties.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: May 5, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Susan K. Heimbecher, David Monteith, James D. Pipkin
  • Publication number: 20150119380
    Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. In a specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN2 into mRNA that is transcribed from the SMN2 gene. In another specific embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 into mRNA that is transcribed from the SMN1 gene. In yet another embodiment, provided herein are compounds of a form that may be used to modulate the inclusion of exon 7 of SMN1 and SMN2 into mRNA that is transcribed from the SMN1 and SMN2 genes, respectively.
    Type: Application
    Filed: December 28, 2012
    Publication date: April 30, 2015
    Inventors: Matthew G. Woll, Guangming Chen, Soongyu Choi, Amal Dakka, Song Huang, Gary Mitchell Karp, Chang-Sun Lee, Chunshi Li, Jana Narasimhan, Nikolai Naryshkin, Sergey Paushkin, Hongyan Qi, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Emmanuel Pinard, Hasane Ratni
  • 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: 20150105389
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventors: Erik Dean RAAUM, Garrett Thomas POTTER, Tai Wei LY
  • Publication number: 20150099015
    Abstract: Methods and compositions are provided for treating neuropsychiatric disorders such as schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia, and bipolar disorder. The methods entail administering to a patient diagnosed as having a neuropsychiatric disorder (e.g., schizophrenia, depression, attention deficit disorder, mild cognitive impairment, dementia bipolar disorder, etc.) or as at risk for a neuropsychiatric disorder a benzoic acid, benzoic acid salt, and/or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, in combination with a neuropharmacological agent (e.g., an antipsychotic, an antidepressant, medications for attention deficit and hyperactivity disorder, cognitive impairment, or dementia, etc.) where the benzoic acid, benzoic acid salt, or benzoic acid derivative, and/or a sorbic acid, sorbic acid salt, and/or sorbic acid derivative, is in an amount sufficient to increase the efficacy of the neuropharmacological agent.
    Type: Application
    Filed: November 24, 2014
    Publication date: April 9, 2015
    Inventor: Guochuan Emil TSAI
  • 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: 20150087629
    Abstract: The invention relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(?O)—; —C(?O)—C(?O)—; —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —C(?O)—Z—; —NRx—C(?O)—Z—; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —C(?S)—Z—; —NRx—C(?S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(?O)—NRx— or —NRx—C(?O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said
    Type: Application
    Filed: December 5, 2014
    Publication date: March 26, 2015
    Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J.M. De Waepenaert, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
  • Patent number: 8987276
    Abstract: The present invention is concerned with novel substituted triazolyl piperazine and triazolyl piperidine derivatives of Formula (I) wherein R1, R2, R3, R4a, R4b, R5, X, Y1, Y2, L1, and L2 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: March 22, 2012
    Date of Patent: March 24, 2015
    Assignees: Janssen Pharmaceuticals, Inc., Cellzome Limited
    Inventors: Francois Paul Bischoff, Adriana Ingrid Velter, Sven Franciscus Anna Van Brandt, Didier Jean-Claude Berthelot
  • Publication number: 20150080398
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: November 24, 2014
    Publication date: March 19, 2015
    Inventors: Erik Dean RAAUM, Garrett Thomas POTTER, Tai Wei LY
  • Publication number: 20150080397
    Abstract: Provided herein are pharmaceutically acceptable salts of 3,5-diaminopyrazoles, for example, pharmaceutically acceptable salts of compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: September 17, 2014
    Publication date: March 19, 2015
    Inventors: Tai Wei LY, Erik Dean RAAUM
  • Publication number: 20150064283
    Abstract: The invention comprises various aqueous PEG-carbohydrate-lipid based formulations of pharmaceutical active ingredients including compositions for intravenous injections. This invention relates to methods and compositions for improving solubility and the safety profile of pharmaceutical compounds. More particularly, the present invention relates to employing PEG-carbohydrate-lipid conjugates for formulating drug compositions having increased solubility or dispersivity and enhanced stability.
    Type: Application
    Filed: November 7, 2014
    Publication date: March 5, 2015
    Inventor: Nian Wu
  • Patent number: 8962608
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Grant
    Filed: September 21, 2012
    Date of Patent: February 24, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jason Brubaker, Christopher Dinsmore, Dawn Marie Hoffman, Joon Jung, Duan Liu, Scott Peterson, Tony Siu, Luis E. Torres, Hongjun Zhang, Zhongyong Wei, Feng Shi
  • Publication number: 20150051194
    Abstract: 8-Substituted-2,6-methano-3-benzazocines of general structure are useful as analgesics, anti-diarrheal agents, anticonvulsants, antitussives and anti-addiction medications.
    Type: Application
    Filed: October 31, 2014
    Publication date: February 19, 2015
    Applicant: RENSSELAER POLYTECHNIC INSTITUTE
    Inventor: Mark P. WENTLAND
  • Publication number: 20150045372
    Abstract: The present invention relates to processes for preparing pyrazole derivatives of Formula (I) and salts and pharmaceutical compositions of the salts thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to salts of compounds of Formula (I) and pharmaceutical compositions thereof.
    Type: Application
    Filed: October 24, 2014
    Publication date: February 12, 2015
    Inventors: Ashwin M. Krishnan, Tawfik Gharbaoui
  • Patent number: 8937184
    Abstract: The invention relates to a group of 1H-imidazole derivatives which are modulators of cannabinoid CB2 receptors, to methods for the preparation of these compounds, to novel intermediates useful for the synthesis of said imidazole derivatives, to methods for the preparation of these intermediates, to pharmaceutical compositions containing one or more of these 1H-imidazole derivatives as active ingredient, as well as to the use of these pharmaceutical compositions for the treatment of disorders in which cannabinoid CB2 receptors are involved. The compounds have the general formula (I) wherein R1-R4 have the meanings given in the specification.
    Type: Grant
    Filed: February 14, 2006
    Date of Patent: January 20, 2015
    Assignee: Abbvie B.V.
    Inventors: Josephus H. M. Lange, Herman H. Van Stuivenberg, Bernard J. Van Vliet
  • Patent number: 8927546
    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: Grant
    Filed: September 22, 2010
    Date of Patent: January 6, 2015
    Assignee: Dart Neuroscience (Cayman) Ltd.
    Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
  • Publication number: 20140378457
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: September 9, 2014
    Publication date: December 25, 2014
    Inventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson, Bruce E. Tomczuk
  • Patent number: 8916555
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: December 23, 2014
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
  • Publication number: 20140371237
    Abstract: Provided are novel methods and compositions for the diagnosis, prognosis and treatment of leiomyomas, in particular uterine leiomyoma (UL). In addition, methods of identifying anti-tumor agents are described. Furthermore, novel methods and compositions are provided for the treatment of diseases characterized by an aberrant growth of mesenchymal stem cells and their descendants and for the treatment of obesity are disclosed.
    Type: Application
    Filed: August 6, 2014
    Publication date: December 18, 2014
    Inventors: Jörn Bullerdiek, Dominique N. Markowski
  • Publication number: 20140371213
    Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.
    Type: Application
    Filed: May 19, 2014
    Publication date: December 18, 2014
    Applicant: ASTEX THERAPEUTICS, LTD.
    Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Adrian Liam GILL, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
  • Patent number: 8912195
    Abstract: Compounds of Formula (I), including pharmaceutically acceptable salts thereof, wherein A is selected from the group (II), are useful as HIV attachment inhibitors.
    Type: Grant
    Filed: December 1, 2011
    Date of Patent: December 16, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Tao Wang, Zhongxing Zhang, Zhiwei Yin, John F. Kadow, Nicholas A. Meanwell
  • Publication number: 20140350012
    Abstract: The invention further relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5- or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-
    Type: Application
    Filed: August 11, 2014
    Publication date: November 27, 2014
    Inventors: Jean-Pierre Andre Marc Bongartz, Lieven Meerpoel, Maria Gustaaf Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Nestor Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
  • Publication number: 20140348787
    Abstract: Compositions and methods for treating ear infections are disclosed. More specifically, these methods may refer to treatment of internal otitis using an otic composition, such as otic gel for animals and humans. Poloxamer otic gel may be in liquid state at room temperature and may change to gel at about temperature (64° F.) as poloxamer otic gel reaches body temperature, because of the thermo-reversible properties. Consequently, poloxamer otic gel may be an effective treatment in animals and humans, where poloxamer otic gel may reach otitis affected site and remain there for a longer period of time. Additionally, poloxamer otic gel may include APIs such as antifungals, antibiotics and corticosteroids, among others. Furthermore, poloxamer otic gel may be instilled inside the ear, employing calibrated delivery device into the vertical ear canal in order to reach the horizontal ear canal, without puncturing the tympanic membrane.
    Type: Application
    Filed: May 22, 2013
    Publication date: November 27, 2014
    Applicant: PROFESSIONAL COMPOUNDING CENTERS OF AMERICA
    Inventor: Chris V. Simmons
  • Patent number: 8889677
    Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.
    Type: Grant
    Filed: January 11, 2013
    Date of Patent: November 18, 2014
    Assignee: Boehringer Ingellheim International GmbH
    Inventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
  • Patent number: 8889665
    Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R3 and L are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: July 1, 2008
    Date of Patent: November 18, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Ioannis Sapountzis, Peter Ettmayer, Christian Klein, Andreas Mantoulidis, Steffen Steurer, Irene Waizenegger
  • Publication number: 20140336202
    Abstract: Methods of treating subjects with cancer and screening for MDM2 inhibitors that may be effective cancer therapeutics are provided herein. The cancers that may be treated using MDM2 inhibitors using the methods described herein include those that are or may become resistant to treatment with tyrosine kinase inhibitors. Methods of treating subjects with cancers that have, or develop in response to treatment with tyrosine kinase inhibitors, elevated levels of MDM2, Mcl-1 or PP5 or decreased levels of Huwe1 or CAS using MDM2 inhibitors are provided herein. The MDM2 inhibitors may be effective at treating these cancers alone or in combination with a tyrosine kinase inhibitor regardless of p53 status (mutant or wild-type) of the cancer.
    Type: Application
    Filed: December 7, 2012
    Publication date: November 13, 2014
    Applicant: DUKE UNIVERSITY
    Inventors: Sally Kornbluth, Manabu Kurokawa, Neil Spector, Mark Dewhirst
  • Patent number: 8883135
    Abstract: The invention provides crystalline solid forms of (((S)-1-{(S)-2-[4-(4?-{[6-((2R,5S)-2,5-dimethyl-4-methylcarbamoyl-piperazin-1-yl)-pyridine-3-carbonyl]-amino}-2?-trifluoromethoxy-biphenyl-4-yl)-1H-imidazol-2-yl]-pyrrolidine-1-carbonyl}-2-methyl-propyl)-carbamic acid methyl ester. The invention also provides pharmaceutical compositions comprising such crystalline solid forms, methods of using such crystalline solid forms to treat hepatitis C virus infection, and processes useful for preparing such crystalline solid forms.
    Type: Grant
    Filed: April 25, 2013
    Date of Patent: November 11, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Venkat R. Thalladi, Jerry Nzerem, Xiaojun Huang, Weijiang Zhang