Two Of The Cyclos Share At Least Three Ring Members Or A Ring Member Is Shared By Three Of The Cyclos (e.g., Bridged, Peri-fused, Etc.) Patents (Class 540/456)
  • Patent number: 9988398
    Abstract: A novel crystalline form of rifaximin and process for its preparation are described. A pharmaceutical composition comprising crystalline rifaximin is also described.
    Type: Grant
    Filed: June 6, 2017
    Date of Patent: June 5, 2018
    Assignee: CADILA HEALTHCARE LIMITED
    Inventors: Kumar Kamlesh Singh, Nikhil Amar Singh, Prashant Rameshchandra Bhatt, Amol Kashinath Patil
  • Patent number: 9867911
    Abstract: A new class of rapamycin 40-O-cyclic hydrocarbon esters is disclosed. The 40-O position of the rapamycin ester has the form 40-O—R, where R is C(O)—(CH2)n-X, n is 0, 1 or 2, and X is a cyclic hydrocarbon having 3-8 carbons, optionally containing one or more unsaturated bonds, and one or more linear (CH2)) and/or cyclic (X) carbon atoms may have an OH or halide group. Also disclosed are therapeutic compositions and methods that employ the novel analogs.
    Type: Grant
    Filed: July 18, 2016
    Date of Patent: January 16, 2018
    Assignee: Biotronik AG
    Inventors: Ronald E. Betts, John Dang Nguyen
  • Patent number: 9840563
    Abstract: Disclosed herein is a method for treating and/or preventing atrial fibrillation in a subject, comprising administering to the subject a pharmaceutical composition comprising an anti-CD44 neutralizing antibody or an antigen binding portion thereof which specifically binds to the amino-terminal domain of CD44. The anti-CD44 neutralizing antibody is a monoclonal antibody. The pharmaceutical composition further includes a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: October 6, 2015
    Date of Patent: December 12, 2017
    Assignee: Chang Gung Memorial Hospital, Linkou
    Inventors: Wei-Jan Chen, Yung-Hsinn Yeh, Shang-Hung Chang
  • Patent number: 9765090
    Abstract: The present invention relates to an epidithiodioxopiperazine derivative represented by the following Chemical Formula 1 or its reduced derivative; a method for preparing a compound represented by Chemical Formula 1 having improved intracellular permeability and mimicking the activity of 2-Cys-Prx in its reduced form in the cells; a pharmaceutical composition for preventing or treating vascular diseases comprising an epidithiodioxopiperazine compound or its derivatives or pharmaceutically acceptable salts thereof as an active ingredient; a drug delivery device for local administration including the pharmaceutical composition; and a pharmaceutical composition for inhibiting melanoma metastasis comprising the epidithiodioxopiperazine compound or its derivatives or pharmaceutically acceptable salts thereof as an active ingredient.
    Type: Grant
    Filed: May 23, 2014
    Date of Patent: September 19, 2017
    Assignee: EWHA UNIVERSITY-INDUSTRY COLLABORATION FOUNDATION
    Inventors: Sang Won Kang, Dong Hoon Kang, Doo Jae Lee
  • Patent number: 9605001
    Abstract: The present invention relates to production of polyketides and other natural products and to libraries of compounds and individual novel compounds. One important area is the isolation and potential use of novel FKBP-ligand analogues and host cells that produce these compounds. The invention is particularly concerned with methods for the efficient transformation of strains that produce FKBP analogues and recombinant cells in which cloned genes or gene cassettes are expressed to generate novel compounds such as polyketide (especially rapamycin) FKBP-ligand analogues, and to processes for their preparation, and to means employed therein (e.g. nucleic acids, vectors, gene cassettes and genetically modified strains).
    Type: Grant
    Filed: March 2, 2015
    Date of Patent: March 28, 2017
    Assignee: Buck Institute for Research On Aging
    Inventors: Matthew Alan Gregory, Steven James Moss
  • Patent number: 9434744
    Abstract: The present invention provides improved processes for obtaining rapamycin derivatives including Biolimus A9.
    Type: Grant
    Filed: July 21, 2015
    Date of Patent: September 6, 2016
    Assignee: Biosensors International Group, Ltd.
    Inventors: Margaret W. Kayo, Richard S. Fornicola, Ivan Kovacik
  • Patent number: 9408884
    Abstract: A new class of rapamycin 40-O-cyclic hydrocarbon esters is disclosed. The 40-O position of the rapamycin ester has the form 40-O—R, where R is C(O)—(CH2)n-X, n is 0, 1 or 2, and X is a cyclic hydrocarbon having 3-8 carbons, optionally containing one or more unsaturated bonds, and one or more linear (CH2)n) and/or cyclic (X) carbon atoms may have an OH or halide group. Also disclosed are therapeutic compositions and methods that employ the novel analogs.
    Type: Grant
    Filed: June 3, 2013
    Date of Patent: August 9, 2016
    Assignee: Biotronik AG
    Inventors: Ronald E. Betts, John Dang Nguyen
  • Patent number: 9403844
    Abstract: Amorphous rifaximin, methods of making it, and pharmaceutical compositions containing it. Also described are methods of converting amorphous rifaximin to crystalline rifaximin and vice versa.
    Type: Grant
    Filed: June 8, 2015
    Date of Patent: August 2, 2016
    Assignee: Cipla Ltd.
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Manjinder Singh Phull, Maruti Ghagare
  • Patent number: 9382266
    Abstract: There is provided inter alia a compound of formula (I) or a pharmaceutically acceptable salt thereof and its use in therapy.
    Type: Grant
    Filed: December 21, 2012
    Date of Patent: July 5, 2016
    Assignee: BUCK INSTITUTE FOR RESEARCH ON AGING
    Inventors: Matthew Alan Gregory, Steven James Moss, Barrie Wilkinson
  • Patent number: 9284334
    Abstract: There is provided compounds of formula I, wherein R1, R2a, R2b, R2c, X, Y, Z, R3 and ring A/B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K, PIM family kinase and/or mTOR) is desired and/or required, and particularly in the treatment of cancer. The invention also relates to combinations containing such compounds.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: March 15, 2016
    Assignee: Fundación Centro Nacional de Investigaciones Oncologicas Carlos III
    Inventors: Joaquin Pastor Fernández, Rosa Maria Álvarez Escobar, Rosario Concepción Riesco Fagundo, Ana Belén García García, Antonio Rodriguez Hergueta, Jose Ignacio Martín Hernando, Carmen Blanco Aparicío, David Álvaro Cebrián Muñoz
  • Patent number: 9273066
    Abstract: The present invention relates to Rifaximin polymorphic forms, to their use in medicinal preparations and to therapeutic methods using them.
    Type: Grant
    Filed: October 24, 2013
    Date of Patent: March 1, 2016
    Assignee: Salix Pharmaceuticals, Inc.
    Inventors: Karen S. Gushurst, Donglai Yang, Petinka Vlahova, Jeffrey S. Stults
  • Patent number: 9273063
    Abstract: A process is described which enables Rifaximin in a completely amorphous form to be obtained. Said process comprises the steps of dissolving crude Rifaximin in absolute ethanol while hot and then collecting after precipitation by—cooling the title compound under amorphous form.
    Type: Grant
    Filed: April 24, 2014
    Date of Patent: March 1, 2016
    Assignee: Salix Pharmaceuticals, Inc.
    Inventors: Emilio Vecchio, Roberta Pizzocaro
  • Patent number: 9260419
    Abstract: The disclosure is in part directed to crystalline forms of an oxalate salt of 6-O-(4-dimethylaminoethoxy)cinnamoyl fumagillol.
    Type: Grant
    Filed: May 7, 2013
    Date of Patent: February 16, 2016
    Assignee: Zafgen, Inc.
    Inventor: Thomas Crawford
  • Patent number: 9238604
    Abstract: The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams from the intermediates. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: January 19, 2016
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Feng Xu, Guy Humphrey, Tao Pei, Zhiguo Jake Song, Tao Wang, Laura Artino
  • Patent number: 9134329
    Abstract: The disclosure provides rifamycin and rifamycin derivative compositions, including rifabutin and rifabutin derivative compositions able to cause drug-sensitization in a cancer cell or inhibition of a cancer cell. The disclosure also provides methods of administering such compositions to cancer cells to sensitize them to drugs, such as chemotherapeutics, or directly inhibit them. The disclosure also provides methods of administering such compositions to increase reactive oxygen species (ROS), particularly superoxides, in cancer cells. The disclosure further provides methods of determining whether a cancer will respond to chemotherapeutics and whether to administer rifamycin or a rifamycin derivative based on ROS levels in cancer cells of a patient.
    Type: Grant
    Filed: July 2, 2014
    Date of Patent: September 15, 2015
    Assignee: The Texas A&M University System
    Inventors: James Sacchettini, Niam Zhou, Dwight Baker, Steven A. Maxwell, Deeann Wallis
  • Patent number: 9079918
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Grant
    Filed: July 31, 2014
    Date of Patent: July 14, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Mimi L. Quan, Carl P. Decicco, James R. Corte, Cailan Wang
  • Patent number: 9051336
    Abstract: The invention refers to the selective acylation of Rapamycin at the 42-position (I) with an acylating agent of the formula (II) wherein R4 and R5 are the same or different, individually the rest of an acetal, especially tetrahydropyran, or of a carbonate or the rest of a silyl ether or taken together are the rest of a boronate, an acetal or ketal.
    Type: Grant
    Filed: March 30, 2012
    Date of Patent: June 9, 2015
    Assignee: SANDOZ
    Inventors: Wolfgang Felzmann, Niklas Schone
  • Publication number: 20150148294
    Abstract: A method for treating endocrine tumors by administration of an mTOR inhibitor, optionally in combination with another drug.
    Type: Application
    Filed: January 29, 2015
    Publication date: May 28, 2015
    Applicant: Novartis AG
    Inventors: Peter Wayne Marks, David Lebwohl
  • Patent number: 9034892
    Abstract: The present invention relates to Rifaximin polymorphic, salt, hydrate, and amorphous forms, to their use in medicinal preparations and to therapeutic methods using them.
    Type: Grant
    Filed: June 27, 2013
    Date of Patent: May 19, 2015
    Assignee: Salix Pharmaceuticals, Inc.
    Inventors: Karen S. Gushurst, Donglai Yang, Petinka Vlahova, Jeffrey S. Stults
  • Patent number: 9024014
    Abstract: This disclosure concerns a new family of phosphorus-containing compounds of Formula (I): and pharmaceutically acceptable derivatives thereof. Compositions containing such compounds and uses thereof are also provided.
    Type: Grant
    Filed: November 14, 2011
    Date of Patent: May 5, 2015
    Assignee: Ariad Pharmaceuticals, Inc.
    Inventors: David L. Berstein, Leonard W. Rozamus, Yihan Wang, Chester A. Metcalf, III
  • Patent number: 9018373
    Abstract: A method for preparing temsirolimus, the method including: using a substituted aromatic aldehyde to protect 2,2-dimethylol propionic acid to produce intermediate II; carrying out reaction between the intermediate II and 2,4,6-trichlorobenzoyl chloride; carrying out condensation reaction between a resulting product and rapamycin to produce intermediate III; and finally using sulfuric acid to remove a protecting group from the intermediate III to yield temsirolimus.
    Type: Grant
    Filed: July 3, 2013
    Date of Patent: April 28, 2015
    Assignee: Tianjin Weijie Technology Co., Ltd.
    Inventors: Honghai Song, Long Tang, Wei Chen, Zheng Li, Jinzhou Li, Zhicun Sun, Jiajin Feng
  • Publication number: 20150112058
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: December 22, 2014
    Publication date: April 23, 2015
    Inventors: James R. Corte, Tianan Fang, Carl P. Decicco, Donald J.P. Pinto, Karen A. Rossi, Zilun Hu, Yoon Jeon, Mimi L. Quan, Joanne M. Smallheer, Yufeng Wang, Wu Yang
  • Patent number: 9012629
    Abstract: Disclosed is a method of preparing an amino acid ester of maytansinol by reacting maytansinol with an N-carboxyanhydride of an amino acid (NCA) in the presence of a drying agent. Also disclosed is an improved method of preparing an amino acid ester of maytansinol in which a nucleophile is added to the reaction mixture after completion of the reaction between maytansinol and an N-carboxyanhydride of an amino acid.
    Type: Grant
    Filed: September 26, 2013
    Date of Patent: April 21, 2015
    Assignee: ImmunoGen, Inc.
    Inventors: Wayne C. Widdison, Robert Yongxin Zhao
  • Patent number: 9012441
    Abstract: Compounds of formula I: or salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for treating a Retroviridae viral infection including an infection caused by the HIV virus.
    Type: Grant
    Filed: January 9, 2014
    Date of Patent: April 21, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Steven S. Bondy, Carina E. Cannizzaro, Chien-Hung Chou, Yunfeng Eric Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
  • Patent number: 8980872
    Abstract: A method for preventing and/or treating a functional gastrointestinal disorder, comprising administering, to a subject with the functional gastrointestinal disorder, rifaximin as an effective ingredient. The functional gastroinstestinal disorder includes a functional esophageal disorder, a functional gastroduodenal disorder (e.g., a functional dyspepsia), a functional bowel disorder (e.g., a functional bloating, a functional diarrhea), a functional abdominal pain syndrome, a functional gallbladder and Sphincter of Oddi disorder, a functional anorectal disorder (e.g., a functional fecal incontinence, a functional anorectal pain, a functional defecation disorder), a functional disorder in neonates and toddlers (e.g., an infant functional diarrhea), a functional disorder in children and adolescents (e.g., a childhood functional abdominal pain, a childhood nonretentive fecal incontinence), and other diseases.
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: March 17, 2015
    Assignee: Aska Pharmaceutical Co., Ltd.
    Inventors: Satoru Tamaoki, Jun Sato, Katsuichi Sudo
  • Publication number: 20150057262
    Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: October 30, 2014
    Publication date: February 26, 2015
    Inventors: Patrick Y.S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
  • Publication number: 20150051183
    Abstract: The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain.
    Type: Application
    Filed: March 15, 2013
    Publication date: February 19, 2015
    Inventors: Daniel Obrecht, Philipp Ermert, Said Oumouch, Arnaud Piettre, Jean-François Gosalbes, Marc Thommen
  • Publication number: 20150051242
    Abstract: A semi-synthetic rapamycin analog with a triazole moiety or a pharmaceutically acceptable salt or prodrug thereof, is a broad-spectrum cytostatic agent and a mTOR inhibitor, and is useful in the treatment of various cancers, or tumors in organs such as kidney, liver, breast, head and neck, lung, prostate, and restenosis in coronary arteries, peripheral arteries, and arteries in the brain, immune and autoimmune diseases. Also disclosed are fungal growth-, restenosis-, post-transplant tissue rejection- and immune- and autoimmune disease-inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosois, post-transplant tissue rejection, and immune and autoimmune disease in a mammal.
    Type: Application
    Filed: November 30, 2012
    Publication date: February 19, 2015
    Applicant: ZHEJIANG ZYLOX MEDICAL DEVICE CO., LTD.
    Inventor: Jonathon Z. Zhao
  • Publication number: 20150045533
    Abstract: The present invention relates to a sorbent comprising a solid support material, the surface of which comprises a residue of a general formula (I), wherein the residue is attached via a covalent single bond to a functional group on the surface of either the bulk solid support material itself or of a polymer film on the surface of the solid support material.
    Type: Application
    Filed: September 17, 2012
    Publication date: February 12, 2015
    Inventors: Markus Arendt, Björn Degel, Thomas Schwarz, Gerhard Stumm, Martin Welter
  • Publication number: 20150017219
    Abstract: The invention provides therapeutic particulates including a macrolide, such as rapamycin, in solid state crystalline form, having a size of 20 ?m or less, or 10 ?m or less. The particulates are formed in one method by preparing a composition with a macrolide and first (e.g., xylene) and second (e.g., an alcohol, acetone, or acetonitrile) solvents. In the composition a maximum solubility for the macrolide that is greater than a maximum solubility of the macrolide dissolved in either the first or second solvent individually. The first and second solvents are then evaporated from the composition to provide the macrolide particulates. In another method, the particulates can be formed by a method including sonication and stirring/evaporation steps, and the particulates can be obtained from a supersaturated solution, formed during the process.
    Type: Application
    Filed: June 12, 2014
    Publication date: January 15, 2015
    Inventors: Joram Slager, Aleksey V. Kurdyumov, Toni M. Heyer
  • Patent number: 8933110
    Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B—W??(I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: October 4, 2011
    Date of Patent: January 13, 2015
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Hui Cao, Yat Sun Or
  • Patent number: 8921319
    Abstract: The invention provides methods of making and using compounds of the formula shown, which are inhibitors of human plasmin and plasma kallikrein. (Formula I) The compounds are useful for the prevention of blood loss, and as components of fibrin adhesives.
    Type: Grant
    Filed: July 5, 2011
    Date of Patent: December 30, 2014
    Assignee: The Medicines Company (Leipzig) GmbH
    Inventors: Torsten Steinmetzer, Sebastian Martin Saupe
  • Publication number: 20140356417
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Application
    Filed: June 12, 2014
    Publication date: December 4, 2014
    Inventors: Peter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Publication number: 20140356361
    Abstract: This invention relates to repeated administration of antigen-specific immunotherapeutics using protocols, or elements thereof, that do not induce immunosuppression. In some embodiments, the protocol has been previously shown not to induce immunosuppression in a subject.
    Type: Application
    Filed: June 4, 2014
    Publication date: December 4, 2014
    Applicant: Selecta Biosciences, Inc.
    Inventors: Roberto A. Maldonado, Takashi Kei Kishimoto
  • Publication number: 20140343491
    Abstract: The disclosure provides macrolide particulates including a macrolide therapeutic agent such as rapamycin at high concentration in the particulate. In one method the particulates are made by adding a composition containing an polyoxyethylene sorbitan n-acyl ester, poly(ethyleneimine), or alkylated quaternary ammonium salt to a composition including macrolide dissolved in an alcohol such as ethanol. In another method the particulates are made by adding a non-solvent composition to a composition including macrolide and an alkyl-substituted chromanol dissolved in an alcohol such as ethanol. The formed macrolide particulates have one or more desirable properties including sizes in the range of 0.1 ?m to 10 ?m, spherical or near spherical shapes, low polydispersity, and/or stability. The macrolide particulates can be used for therapeutic compositions, or in association with an implantable or insertable medical device, such as associated with a polymeric coating on a device.
    Type: Application
    Filed: May 16, 2014
    Publication date: November 20, 2014
    Inventor: Joram Slager
  • Publication number: 20140343276
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: July 31, 2014
    Publication date: November 20, 2014
    Inventors: Mimi L. Quan, Carl P. Decicco, James R. Corte, Cailan Wang
  • Patent number: 8889855
    Abstract: Provided are efficient methods for direct coupling of a maytansinoid with a carboxylic acid to prepare a maytansinoid C-3 ester in high yield using a rare earth metal-based or trifluoromethanesulfonate-based Lewis acid catalyst and a base together with a coupling reagent. Also provided are compositions used in such methods.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: November 18, 2014
    Assignee: Bio-Thera Solutions Ltd., Co.
    Inventor: Xiaobin Deng
  • Patent number: 8871753
    Abstract: The present invention relates to macrocyclic compounds of Formula I: or pharmaceutically acceptable salts thereof or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are JAK/ALK inhibitors useful in the treatment of JAK/ALK-associated diseases including, for example, inflammatory and autoimmune disorders, as well as cancer.
    Type: Grant
    Filed: April 23, 2009
    Date of Patent: October 28, 2014
    Assignee: Incyte Corporation
    Inventors: Andrew Paul Combs, Richard B. Sparks, Eddy W. Yue, Hao Feng, Michael Jason Bower, Wenyu Zhu
  • Publication number: 20140303159
    Abstract: The present invention relates to macrocylic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of FLT3 (FMS-Related Tyrosine kinase 3). Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine, in particular for the treatment of cell proliferative disorders, such as cancer.
    Type: Application
    Filed: September 28, 2012
    Publication date: October 9, 2014
    Inventors: Petra Marcella Francoise Blom, Jan Marie Cyriel Jozef Hoflack
  • Publication number: 20140274878
    Abstract: The present application describes organic compounds of Formula (I) and pharmaceutical compositions thereof, and their use for the treatment, prevention and/or amelioration of diseases, particularly bacterial infections.
    Type: Application
    Filed: May 30, 2014
    Publication date: September 18, 2014
    Applicant: NOVARTIS AG
    Inventors: Simon Bushell, Matthew J. Lamarche, Jennifer Leeds, Lewis Whitehead
  • Patent number: 8835452
    Abstract: Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin ? and rifaximin ?, and a poorly crystalline form named rifaximin ?, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.
    Type: Grant
    Filed: November 19, 2012
    Date of Patent: September 16, 2014
    Assignee: Alfa Wassermann S.p.A.
    Inventors: Giuseppe Claudio Viscomi, Manuela Campana, Dario Braga, Donatella Confortini, Vincenzo Cannata, Paolo Righi, Goffredo Rosini
  • Publication number: 20140256714
    Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR13—C1-5alkyl-, —C1-5alkyl-NR14—CO—C1-5alkyl-, —C1-2alkyl-NR21—H2—CO—NH—C1-3alkyl- or —C1-2alkyl-NR23—CO—CR16R17—NH—; X1 represents O or —O—C1-2alkyl-; X2 represents a direct bond, C1-2alkyl, —CO—C1-2alkyl or NR12—C1-2alkyl; R1 represents hydrogen or halo; R2 represents halo, acetylene or Het1 R3 represents hydrogen or cyano; R4 represents Ar4—C1-4alkyloxy-, C1-4alkyloxy- or C1-4alkyloxy substituted with one or where possible two or more substituents selected from Het2, NR7R8, hydroxy and C1-4alkyloxy-C1-4alkyloxy-; R7 represents hydrogen or C1-4alkyl; R8 represents C1-4alkyl substituted with NR25R26 or C1-4alkylsulfonyl; R12 represents hydrogen or C1-4alkyl-; R13 represents Ar6-sulfonyl or C1-6alkyloxycarbonyl optionally substituted with phenyl; R16 and R17 represents hydr
    Type: Application
    Filed: May 22, 2014
    Publication date: September 11, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Eddy Jean Edgard FREYNE, Marc Willems, Peter Ten Holte, Alexandra Papanikos, Werner Constant Johan Embrechts, Pierre Henri Storck, Virginie Sophie Poncelet
  • Publication number: 20140248372
    Abstract: The disclosure relates to compounds and compositions for bone formation, fracture treatment, bone grafting, bone fusion, cartilage maintenance and repair and methods related thereto. In certain embodiments, the disclosure relates to compositions comprising one or more compound(s) disclosed herein, such as clotrimazole, honokiol, magnolol, tacrolimus, pimecrolimus, sirolimus, everolimus, temsirolimus, spironolactone, fluticasone, fluticasone propionate, fluticasone furoate, linezolid, telmisartan, chlorambucil, retinol, isotretinoin, acitretin, etretinate, retinoic acid (tretinoin), teniposide, mitomycin C, cytarabine, decitabine, vinblastine, vincristine, vindesine, vinorelbine, valrubicin, doxorubicin, daunorubicin, epirubicin, idarubicin, mitoxantrone, pixantrone, plicamycin, pazopanib, topotecan, camptothecin, irinotecan, sunitinib, derivatives, or salt thereof, for use in bone growth processes.
    Type: Application
    Filed: September 17, 2012
    Publication date: September 4, 2014
    Applicant: EMORY UNIVERSITY
    Inventors: Scott D. Boden, Sreedhara Sangadala
  • Patent number: 8822678
    Abstract: A method for synthesizing temsirolimus, the method including: using a substituted boric acid to protect 2,2-dimethylol propionic acid to produce intermediate II; carrying out a reaction between the intermediate II and 2,4,6-trichlorobenzoyl chloride; carrying out condensation reaction between a resulting product and rapamycin to produce intermediate III; and finally using a diol to remove a protecting group from the intermediate III to yield temsirolimus.
    Type: Grant
    Filed: July 1, 2013
    Date of Patent: September 2, 2014
    Assignee: Tianjin Wiejie Technology Co., Ltd.
    Inventors: Honghai Song, Long Tang, Wei Chen, Zheng Li, Jinzhou Li, Zhicun Sun, Jiajin Feng
  • Publication number: 20140243284
    Abstract: The present invention provides a compound of the formula (I) or (II), wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(?O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(?O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent.
    Type: Application
    Filed: May 12, 2014
    Publication date: August 28, 2014
    Applicant: The United States of America, as represented by the Secretary, Department of Health and Human Serv
    Inventors: Michael R. Boyd, Kirk R. Gustafson, Charles L. Cantrell
  • Publication number: 20140243519
    Abstract: The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity.
    Type: Application
    Filed: August 16, 2012
    Publication date: August 28, 2014
    Inventors: Nobuyoshi Yasuda, Jeffrey T. Kuethe, Guy Humphrey, Gregory L. Beutner, Yong-Li Zhong, Edward Cleator, Carl Baxter
  • Patent number: 8815888
    Abstract: The present invention relates to new rifaximin forms kappa, theta, rifaximin:piperazine cocrystal 1 and rifaximin:piperazine cocrystal 2, methods of making same and to their use in medicinal preparations and therapeutic methods.
    Type: Grant
    Filed: July 31, 2013
    Date of Patent: August 26, 2014
    Assignee: Salix Pharmaceuticals, Ltd.
    Inventors: Yiduo Wu, Stephan D. Parent, Nathan Carl Schultheiss, Melanie Janelle Bevill, Petinka Vlahova, Travis L. Houston
  • Patent number: 8815872
    Abstract: Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.
    Type: Grant
    Filed: September 3, 2009
    Date of Patent: August 26, 2014
    Assignee: Merck Patent GmbH
    Inventors: Henry Yu, Lizbeth Celeste De Selm, Xuliang Jiang, Benny C. Askew, Jr., Srinivasa R. Karra, Andreas Goutopoulos
  • Publication number: 20140235821
    Abstract: A substance contains a phosphatidylinositol-3-kinase (PI3K) inhibitor including a depsipeptide-class compound represented by formula (1), or a physiologically acceptable salt thereof that combines a PI3K inhibitory effect and an HDAC inhibitory effect to provide an anti-cancer pharmaceutical composition for the treatment of an intractable cancer.
    Type: Application
    Filed: September 25, 2012
    Publication date: August 21, 2014
    Applicant: TOHOKU UNIVERSITY
    Inventors: Ken Saijo, Chikashi Ishioka, Tadashi Katoh
  • Publication number: 20140221338
    Abstract: The present invention provides compounds of Formula (Ia): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
    Type: Application
    Filed: August 6, 2012
    Publication date: August 7, 2014
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventors: Donald J. P. Pinto, James R. Corte, Paul J. Gilligan, Tianan Fang, Leon M. Smith, II, Yufeng Wang, Wu Yang, William R. Ewing