Oxygen Containing Hetero Ring Having 12-19 Members (e.g., Methymycin, Carbomycin, Spiramycin, Etc.) Patents (Class 536/7.1)
  • Publication number: 20130045936
    Abstract: The invention relates to an amorphous non-crystalline glass form (Form-ll) of 3R,4S,5S,6R,7R,9R,11S,12R,13S,14R-6-[(2S,3R,4S,6R)-4-dimethylamino-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-10-(2-methoxyethoxymethoxyimino)-3,5,7,9,11,13-hexamethyl-1-oxa-cyclotetradecan-2-one or roxithromycin having at least one characteristic infra-red spectrum peak at approximately 3580 to 3464 cm?1. The invention further relates to a preparation method of increasing the solubility of roxithromycin including the steps of selecting anhydrous roxithromycin or monohydrated roxithromycin; elevating the temperature of the roxithromycin to above the melting point thereof; and reducing the temperature of the melt sufficiently to allow it to set into an amorphous non-crystalline glass form (Form-ll) of roxithromycin having relatively increased solubility without decreasing the stability of thereof.
    Type: Application
    Filed: December 15, 2010
    Publication date: February 21, 2013
    Applicant: North-West University
    Inventors: Wilna Leibenberg, Marique Aucamp, Melgardt M. De Villiers
  • Publication number: 20120329741
    Abstract: Compounds of Formula I or II, and methods of making and using thereof, are described herein. M represents a macrolide subunit, E is a C1-6 group, optionally containing one or more heteroatoms, D is an alkyl or aryl group, A is a linking group connected to D, B is an alkyl, alkylaryl or alkylheteroaryl spacer group, ZBG is a Zinc Binding Group, R1, R2 and R4 are independently are selected from hydrogen, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a C1-6 alkanoate group, a C2-6 carbamate group, a C2-6 carbonate group, a C2-6 carbamate group, or a C2-6 thiocarbamate group, R3 is hydrogen or —OR5, R5 is selected from a group consisting of Hydrogen, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, C1-6 alkanoate group, C2-6 carbamate group, C2-6 carbonate group, C2-6 carbamate group, or C2-6 thiocarbamate group.
    Type: Application
    Filed: May 25, 2012
    Publication date: December 27, 2012
    Inventors: Adegboyega Oyelere, Subhasish Tapadar
  • Patent number: 8318684
    Abstract: Seven novel antibiotic substances can be produced by cultivation of a microbial strain which has been isolated from a soil sample and which is designated as Microbispora sp. A 34030 (deposited under an access number FERM BP-10505 in terms of Budapest Treaty). These seven antibiotic substances are named as bispolide A1, bispolide A2, bispolide A3, bispolide B1, bispolide B2a, bispolide B2b and bispolide B3, respectively. These bispolides are each novel compounds which have a chemical structure as collectively represented by the general formula (III) shown below: These bispolides have each a high antibacterial activity against a variety of bacteria, particularly Gram-positive bacteria and their antibiotic-resistant strains, and hence these bispolides each are effective and useful for therapeutically treating bacterial infections of Gram-positive bacteria in humans and animals.
    Type: Grant
    Filed: May 15, 2007
    Date of Patent: November 27, 2012
    Assignees: Nimura Genetic Solutions Co., Ltd., Forest Research Institute Malaysia
    Inventors: Keiichi Numata, Noriyuki Okujo, Siew Eim Khor, Lee Li Tan, Annie George, Szu Ting Ng, Chin Jye Tan, Hironobu Iinuma, Yasuo Fukagawa, Kunimoto Hotta, Seiji Shibahara, Shinichi Kondo, Satoshi Nimura
  • Publication number: 20120283316
    Abstract: Disclosed are drug delivery compositions comprising an oligonucleotide-modified nanoparticle and a therapeutic agent. Specifically, disclosed are compositions comprising a number of oligonucleotide molecules in a ratio to therapeutic agent molecules to allow a sufficient transportation of the therapeutic agent molecules into a cell. The therapeutic agents include both hydrophobic and hydrophilic. Different attachments of therapeutic agents in a composition are also described.
    Type: Application
    Filed: September 1, 2010
    Publication date: November 8, 2012
    Applicant: Northwestern University
    Inventors: Chad A. Mirkin, David A. Giljohann, Weston L. Daniel
  • Publication number: 20120277174
    Abstract: The invention relates to macrolide compounds of formula (I), the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with antiinflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.
    Type: Application
    Filed: August 13, 2010
    Publication date: November 1, 2012
    Applicant: BASILEA PHARMACEUTICA AG
    Inventors: Johannes Laurenz Kellenberger, Jürg Dreier
  • Publication number: 20120252747
    Abstract: The present invention provides macrocyclic compounds useful as therapeutic agents of the formula: or a pharmaceutically acceptable salt, ester, N-oxide, or prodrug thereof, wherein T, R1, R2, R3, D, E, F, and G are as defined herein. More particularly, these compounds are useful as anti-infective, antiproliferative, anti-inflammatory and prokinetic agents.
    Type: Application
    Filed: June 18, 2012
    Publication date: October 4, 2012
    Inventors: Jay J. Farmer, Ashoke Bhattacharjee, Yi Chen, Joel A. Goldberg, Joseph A. Ippolito, Zoltan F. Kanyo, Rongliang Lou, Adegboyega K. Oyelere, Edward C. Sherer, Joyce A. Sutcliffe, Deping Wang, Yusheng Wu, Yanming Du
  • Patent number: 8268975
    Abstract: The present invention provides compositions, systems and methods for demulsifying an emulsion including an aqueous phase and an organic phase by adding an effective amount of a composition comprising at least one quaternary organopolysiloxane or salt thereof to the emulsion, the composition optionally including at least one of quaternary epihalohydrin/polyamine copolymers or salts, and/or (poly)diallyldimethylammonium halides.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: September 18, 2012
    Assignees: DOW Agrosciences LLC, Kroff Chemical Company
    Inventors: Paul Rey, Steve P. Ceplecha, David M. Sunderlik
  • Patent number: 8263566
    Abstract: What is described are a compound of the formula wherein n is 0 or 1; A-B is —CH?CH— or —CH2—CH2—; R1 is C1-C12-alkyl, C3-C8-cycloalkyl or C2-C12-alkenyl; R2 is for example C1-C12-alkyl, C2-C12-alkenyl or C2-C12-alkinyl; which are optionally substituted with one to five substituents selected from the group consisting of OH, halogen, CN, —N3, —NO2, C3-C8-Cycloalkyl, norbornylenyl-, C3-C8-Cycloalkenyl; C3-C8-halocycloalkyl, C1-C12-alkoxy, C1-C6-alkoxy-C1-C6-alkoxy, C3-C8-cycloalkoxy, C1-C12-haloalkoxy, C1-C12-alkylthio, C3-C8-cycloalkylthio, C1-C12-haloalkylthio, C1-C12-alkylsulfinyl, C3-C8-cycloalkylsulfinyl, C1-C12-haloalkylsulfinyl, C3-C8-halocycloalkylsulfinyl, C1-C12-alkylsulfonyl, C3-C8-cycloalkylsulfonyl, C1-C12-haloalkylsulfonyl, C3-C8-halocycloalkylsulfonyl, —NR4R6, —X—C(?Y)—R4, —X—C(?Y)—Z—R4, —P(?O)(OC1-C6-alkyl)2, aryl, heterocyclyl, aryloxy, arylthio and heterocyclyloxy; R3 is for example H, C1-C12-alkyl or C1-C12-alkyl which is optionally substituted and, where applicable, to E/Z isomers, mixtu
    Type: Grant
    Filed: May 27, 2011
    Date of Patent: September 11, 2012
    Assignee: Merial Limited
    Inventors: Peter Maienfisch, Fiona Murphy Kessabi, Jerome Cassayre, Laura Quaranta, Thomas Pitterna, Ottmar Franz Hueter, Pierre Jung
  • Patent number: 8263753
    Abstract: This invention relates to a method for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides. This invention also relates to solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: September 11, 2012
    Assignee: Intervet International B.V.
    Inventors: Monika Brink, Hans P. Niedermann, Tanja Schweisel, Stephan Veit, Kerstin Fleischhauer, Ralf Warrass, Heinz-Jorg Wennesheimer
  • Publication number: 20120196819
    Abstract: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said compositon dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.
    Type: Application
    Filed: January 4, 2012
    Publication date: August 2, 2012
    Applicant: NEWMARKET PHARMACEUTICALS LLC
    Inventors: David ROCK, Mark RIDALL
  • Publication number: 20120190635
    Abstract: The present invention provides regio- and stereoselective oxidation of unactivated C—H bonds using an engineered mutant cytochrome P450 monooxygenase and an engineered substrate.
    Type: Application
    Filed: September 27, 2010
    Publication date: July 26, 2012
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shengying Li, David H. Sherman, John Montgomery, Mani R. Chaulagain, Allison R. Knauff
  • Patent number: 8227429
    Abstract: This invention relates to a method for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides. This invention also relates to solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.
    Type: Grant
    Filed: July 26, 2007
    Date of Patent: July 24, 2012
    Assignee: Intervet International B.V.
    Inventors: Ralf Warrass, Fritz Blatter, Meinrad Brenner, Guixan Hu, Tamo Rager
  • Publication number: 20120172323
    Abstract: Described herein are formulations and methods for treating diseases caused by infectious pathogens, including mycobacterium avium complex, mycobacterium tuberculosis, Nocardia, Plasmodium falcium, and Plasmodium berghei.
    Type: Application
    Filed: September 10, 2010
    Publication date: July 5, 2012
    Applicant: CEMPRA PHARMACEUTICALS, INC.
    Inventor: Prabhavathi Fernandes
  • Publication number: 20120121702
    Abstract: A solid dosage form for oral administration comprising azithromycin in an amount below that which causes gastrointestinal side effects, which dosage form is a controlled release dosage form.
    Type: Application
    Filed: January 25, 2012
    Publication date: May 17, 2012
    Applicant: Dow Pharmaceutical Sciences, Inc.
    Inventors: Radhakrishnan Pillai, Pramod Sarpotdar, David W. Osborne, Gordon J. Dow
  • Publication number: 20120122808
    Abstract: Described are methods for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, among other uses, may be used to make macrolides. Also described are solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.
    Type: Application
    Filed: January 26, 2012
    Publication date: May 17, 2012
    Applicant: INTERVET INTERNATIONAL B.V.
    Inventors: Ralf Warrass, Fritz Blatter, Meinrad Brenner, Guixan Hu, Timo Rager
  • Publication number: 20120071429
    Abstract: Described herein are novel macrolides, the preparation of novel macrolides, the use of novel macrolides for preventing, treating, or ameliorating various conditions, and the use of novel macrolides as antibacterial agents.
    Type: Application
    Filed: July 26, 2011
    Publication date: March 22, 2012
    Inventors: Jonathan Duffield, Chan-Kou Hwang, Yoshitaka Ichikawa, Youe-Kong Shue
  • Patent number: 8133871
    Abstract: A compound represented by the formula [I] wherein each symbol is as defined in the specification or a pharmacologically acceptable salt thereof, and a pharmaceutical composition containing the compound as an active ingredient.
    Type: Grant
    Filed: October 13, 2006
    Date of Patent: March 13, 2012
    Assignees: The Kitasato Institute, Aphoenix, Inc.
    Inventors: Satoshi Omura, Toshiaki Sunazuka, Kenichiro Nagai, Hideaki Shima, Haruko Yamabe
  • Publication number: 20120058963
    Abstract: The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides substituted at the 4? position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-?, IL-1, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.
    Type: Application
    Filed: November 15, 2011
    Publication date: March 8, 2012
    Applicant: Glaxo Group Limited
    Inventors: Sulejman Alihodzic, Martina Bosnar, Ognjen Culic, Vesna Erakovic Haber, Antun Hutinec, Dubravko Jelic, Goran Kragol, Nikola Marjanovic, Zorica Marusic-Istuk, Marija Ribic, Vanja Vela
  • Publication number: 20120040922
    Abstract: The invention encompasses an active metabolite of the 18-membered macrocyclic antimicrobial agents, specifically, a metabolite of tiacumicin B and in certain embodiments, R-Tiacumicin B or and its related compounds. In particular, the invention encompasses a compound that acts as a potent antibiotic agent for the treatment of bacterial infections, specifically GI infections caused by toxin producing strains of Clostridium difficile (C. difficile) and Clostridium perfringens (C. perfringens).
    Type: Application
    Filed: October 24, 2011
    Publication date: February 16, 2012
    Inventors: Yoshi Ichikawa, Yu-Hung Chiu, Youe-Kong Shue, Farah Kondori Babakhani
  • Publication number: 20120035352
    Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.
    Type: Application
    Filed: July 18, 2011
    Publication date: February 9, 2012
    Inventors: Yat Sun Or, Guoqiang Wang, Ly Tam Phan, Deqiang Niu, Nha Huu Vo, Yao-Ling Qiu, Yanchun Wang, Marina Busuek, Ying Hou, Yulin Peng, Heejin Kim, Tongzhu Liu, Jay Judson Farmer, Gouyou Xu
  • Patent number: 8053418
    Abstract: A novel compound that has antimicrobial activity against penicillin-resistant Streptococcus pneumoniae, and an anti-penicillin resistant pneumococci agent that includes the compound as an active ingredient are provided. Thus, an anti-penicillin resistant pneumococci agent is provided that includes as an active ingredient a compound represented by the following formula (I) or a pharmacologically acceptable salt thereof, or hydrates thereof: wherein, in the formula (I), R represents any one of a halogen atom, an azido group, Ra-Wa-, Rb-Wb-, Rc-Wc-, and RdRd?N—.
    Type: Grant
    Filed: January 24, 2006
    Date of Patent: November 8, 2011
    Assignee: Microbial Chemistry Research Foundation
    Inventors: Toshiaki Miyake, Yoshiaki Takahashi
  • Patent number: 8044030
    Abstract: The invention encompasses an active metabolite of the 18-membered macrocyclic antimicrobial agents, specifically, a metabolite of tiacumicin B and in certain embodiments, R-Tiacumicin B or and its related compounds. In particular, the invention encompasses a compound that acts as a potent antibiotic agent for the treatment of bacterial infections, specifically GI infections caused by toxin producing strains of Clostridium difficile (C. difficile) and Clostridium perfringens (C. perfringens).
    Type: Grant
    Filed: November 28, 2008
    Date of Patent: October 25, 2011
    Assignee: Optimer Pharmaceuticals, Inc.
    Inventors: Yoshi Ichikawa, Yu-Hung Chiu, Youe-Kong Shue, Farah Kondori Babakhani
  • Publication number: 20110237784
    Abstract: A novel 10a-azalide compound crosslinked at the 10a- and 12-positions, which is represented by the following formula, and is effective on even Hemophilus influenzae, or erythromycin resistant bacteria (e.g., resistant pneumococci and streptococci).
    Type: Application
    Filed: August 6, 2008
    Publication date: September 29, 2011
    Applicants: TAISHO PHARMACEUTICAL CO., LTD., MEIJI SEIKA KAISHA, LTD.
    Inventors: Tomohiro Sugimoto, Kanako Yamamoto, Jun Kurosaka, Naoki Sasamoto, Masato Kashimura, Tomoaki Miura, Kenichi Kanemoto, Tomohiro Ozawa, Ken Chikauchi, Eiki Shitara
  • Publication number: 20110230429
    Abstract: What is described are a compound of the formula wherein n is 0 or 1; A-B is —CH?CH— or —CH2—CH2—; R1 is C1-C12-alkyl, C3-C8-cycloalkyl or C2-C12-alkenyl; R2 is for example C1-C12-alkyl, C2-C12-alkenyl or C2-C12-alkinyl; which are optionally substituted with one to five substituents selected from the group consisting of OH, halogen, CN, —N3, —NO2, C3-C8-Cycloalkyl, norbornylenyl-, C3-C8-Cycloalkenyl; C3-C8-halocycloalkyl, C1-C12-alkoxy, C1-C6-alkoxy-C1-C6-alkoxy, C3-C8-cycloalkoxy, C1-C12-haloalkoxy, C1-C12-alkylthio, C3-C8-cycloalkylthio, C1-C12-haloalkylthio, C1-C12-alkylsulfinyl, C3-C8-cycloalkylsulfinyl, C1-C12-haloalkylsulfinyl, C3-C8-halocycloalkylsulfinyl, C1-C12-alkylsulfonyl, C3-C8-cycloalkylsulfonyl, C1-C12-haloalkylsulfonyl, C3-C8-halocycloalkylsulfonyl, —NR4R6, —X—C(?Y)—R4, —X—C(?Y)—Z—R4, —P(?O)(OC1-C6-alkyl)2, aryl, heterocyclyl, aryloxy, arylthio and heterocyclyloxy; R3 is for example H, C1-C12-alkyl or C1-C12-alkyl which is optionally substituted and, where applicable, to E/Z isomers, mixtu
    Type: Application
    Filed: May 27, 2011
    Publication date: September 22, 2011
    Applicant: SYNGENTA CROP PROTECTION, LLC
    Inventors: Peter Maienfisch, Fiona Murphy Kessabi, Jérôme Cassayre, Laura Quaranta, Thomas Pitterna, Ottmar Franz Hueter, Pierre Jung
  • Patent number: 8017589
    Abstract: What is described are a compound of the formula wherein n is 0 or 1; A-B is —CH?CH— or —CH2—CH2—; R1 is C1-C12-alkyl, C3-C8-cycloalkyl or C2-C12-alkenyl; R2 is for example C1-C12-alkyl, C2-C12-alkenyl or C2-C12-alkinyl; which are optionally substituted with one to five substituents selected from the group consisting of OH, halogen, CN, —N3, —NO2, C3-C8-Cycloalkyl, norbornylenyl-, C3-C8-Cycloalkenyl; C3-C8-halocycloalkyl, C1-C12-alkoxy, C1-C6-alkoxy-C1-C6-alkoxy, C3-C8-cycloalkoxy, C1-C12-haloalkoxy, C1-C12-alkylthio, C3-C8-cycloalkylthio, C1-C12-haloalkylthio, C1-C12-alkylsulfinyl, C3-C8-cycloalkylsulfinyl, C1-C12-haloalkylsulfinyl, C3-C8-halocycloalkylsulfinyl, C1-C12-alkylsulfonyl, C3-C8-cycloalkylsulfonyl, C1-C12-haloalkylsulfonyl, C3-C8-halocycloalkylsulfonyl, —NR4R6, —X—C(?Y)—R4, —X—C(?Y)—Z—R4, —P(?O)(OC1-C6-alkyl)2, aryl, heterocyclyl, aryloxy, arylthio and heterocyclyloxy; R3 is for example H, C1-C12-alkyl or C1-C12-alkyl which is optionally substituted and, where applicable, to E/Z isomers, mixtu
    Type: Grant
    Filed: April 27, 2010
    Date of Patent: September 13, 2011
    Assignee: Syngenta Crop Protection LLC
    Inventors: Peter Maienfisch, Fiona Murphy Kessabi, Jerome Cassayre, Laura Quaranta, Thomas Pitterna, Ottmar Franz Hueter, Pierre Jung
  • Publication number: 20110178036
    Abstract: The invention provides, biologically active spinosyns, hybrid spinosyn polyketide synthases capable of functioning in Saccharopolyspora spinosa to produce the spinosyns, and methods of controlling insects using the spinosyns.
    Type: Application
    Filed: March 28, 2011
    Publication date: July 21, 2011
    Inventors: Lesley S. Burns, Paul R. Graupner, Paul Lewer, Christine J. Martin, William A. Vousden, Clive Waldron, Barrie Wilkinson
  • Publication number: 20110124850
    Abstract: The present invention provides glycorandomized structures and combinatorial methods for rapidly generating a diverse library of glycorandomized structures, comprising incubating one or more aglycons and a pool of NDP-sugars in the presence of a glycosyltransferase. The glycosyltransferase may be one that is associated with or involved in production of natural secondary metabolites, or one which is putatively associated with or involved in production of natural secondary metabolites. The glycosyltransferase may show significant flexibility with respect to its NDP-sugar donors and/or its aglycons. NDP-sugar donors may be commercially available, or may be produced by utilizing mutant or wild type nucleotidyltransferases significant flexibility with respect to their substrates.
    Type: Application
    Filed: February 1, 2011
    Publication date: May 26, 2011
    Inventor: Jon Thorson
  • Publication number: 20110071096
    Abstract: The present invention relates to a semi-synthetic macrolide having antimicrobial activity, in particular antibacterial activity; pharmaceutical compositions comprising the macrolide; and methods of using the macrolide to treat or prevent an infection.
    Type: Application
    Filed: August 19, 2010
    Publication date: March 24, 2011
    Applicant: IDEXX Laboratories, Inc.
    Inventors: Murthy V.S.N. Yerramilli, Michael Randolph Atkinson, Hengguang Ll, Christopher Alan Cox
  • Patent number: 7910558
    Abstract: The present invention provides a method for preparing bridged macrocyclic compounds comprising the step of reacting a macrocyclic compound characterized by having at least two nucleophilic moieties with a bifunctional bridging reagent optionally in the presence of a catalyst, thereby producing a bridged macrocyclic product.
    Type: Grant
    Filed: January 23, 2004
    Date of Patent: March 22, 2011
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventor: Yat Sun Or
  • Publication number: 20110053875
    Abstract: This invention relates to a method for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides. This invention also relates to solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.
    Type: Application
    Filed: July 30, 2010
    Publication date: March 3, 2011
    Inventors: Fritz Blatter, Meinrad Brenner, Monika Brink, Kerstin Fleischhauer, Guixian Hu, Hans Peter Niedermann, Timo Rager, Tanja Schweisel, Stephan Veit, Ralf Warrass, Heinz-Jörg Wennesheimer
  • Publication number: 20110053876
    Abstract: The invention relates to macrolide compounds of formula (I), the use of said compounds as medicaments, in particular for the treatment or prevention of inflammatory and allergic diseases, pharmaceutical compositions containing said compounds and to processes for their preparation. The invention relates in particular to macrolide compounds with anti-inflammatory activity mediated primarily through inhibition of phosphodiesterase 4 (PDE4) which makes them useful for the treatment and/or prevention of inflammatory and allergic diseases such as chronic obstructive pulmonary disease (COPD), asthma, rheumatoid arthritis, atopic dermatitis or inflammatory bowel disease or proliferative diseases such as cancer.
    Type: Application
    Filed: February 9, 2009
    Publication date: March 3, 2011
    Inventors: Johannes Laurenz Kellenberger, Jürg Dreier, Stefan Bernhard Reinelt
  • Publication number: 20110040078
    Abstract: The present invention relates to a process for the preparation of erythromysin derivatives, in particular telithromycin of formula (I) and its pharmaceutically acceptable salts, providing the isolated intermediates in crystalline form of superior stability and purity.
    Type: Application
    Filed: October 10, 2008
    Publication date: February 17, 2011
    Applicants: SANDOZ AG
    Inventors: Ingolf Macher, Dominic de Souza
  • Publication number: 20110028417
    Abstract: The invention features novel macrocyclic compounds, methods of making the compounds, pharmaceutical compositions including the compounds, and methods of treatment using the compounds.
    Type: Application
    Filed: July 30, 2010
    Publication date: February 3, 2011
    Applicant: Synovo GmbH
    Inventors: Hans-Jurgen Gutke, Michael Burnet, Jan-Hinrich Guse
  • Patent number: 7879809
    Abstract: This invention is directed to the use of spinosyn or a physiologically acceptable derivative or salt thereof for improved production of fish; controlling ectoparasite infestations in aquaculture raised fish; and fish feed formulations.
    Type: Grant
    Filed: May 15, 2006
    Date of Patent: February 1, 2011
    Assignee: Eli Lilly and Company
    Inventors: Clayton Paul Dick, Daniel Earl Snyder, Joseph Raymond Winkle
  • Publication number: 20110021449
    Abstract: Macrolides of Formula (I) or (I-A): and wherein the residues R1, R2, R3, R4, R12, R13 and R14 have certain meanings defined in this application are useful for treating or preventing inflammatory or allergic diseases or. cancer in animals and humans.
    Type: Application
    Filed: February 9, 2009
    Publication date: January 27, 2011
    Inventors: Johannes Laurenz Kellenberger, Jürg Dreier, Stefan Bernhard Reinelt
  • Patent number: 7863249
    Abstract: The invention relates to novel forms of compounds displaying broad spectrum antibiotic activity, especially crystalline polymorphic forms and amorphous forms of such compounds, compositions comprising such crystalline polymorphic forms and amorphous forms of such compounds, processes for manufacture and use thereof. The compounds and compositions of the invention are useful in the pharmaceutical industry, for example, in the treatment or prevention of diseases or disorders associated with the use of antibiotics, chemotherapies, or antiviral therapies, including, but not limited to, colitis, for example, pseudo-membranous colitis; antibiotic associated diarrhea; and infections due to Clostridium difficile (“C. difficile”), Clostridium perfringens (“C. perfringens”), Staphylococcus species, for example, methicillin-resistant Staphylococcus, or Enterococcus including Vancomycin-resistant enterococci.
    Type: Grant
    Filed: April 11, 2008
    Date of Patent: January 4, 2011
    Assignee: Optimer Pharmaceuticals, Inc.
    Inventors: Yu-Hung Chiu, Tessie Mary Che, Alex Romero, Yoshi Ichikawa, Youe-Kong Shue
  • Publication number: 20100280230
    Abstract: This invention discloses a method of manufacturing clarithromycin, where an erythromycin A 9-oxime thiocyanate salt is used directly to perform an etherification reaction, and then successively silanizattion, methylattion and hydrolysis reactions are sequentially conducted. It is a new process with simple process with a high yield, low cost, less pollution, high quality and is suitable for commercial manufacturing.
    Type: Application
    Filed: April 30, 2010
    Publication date: November 4, 2010
    Inventors: XINTANG RAO, Zhijian Ding, Hangbin Lou, Jing Wu, Yanglin Fang, Baineng Deng
  • Patent number: 7816370
    Abstract: The present invention is about the use of at least one epothilone or derivative thereof as an active ingredient for manufacturing a medicament for use in the treatment of disease(s) involving a neuronal connectivity defect, such as schizophrenia or autism.
    Type: Grant
    Filed: January 28, 2005
    Date of Patent: October 19, 2010
    Assignees: Institut National de la Sante et de la Recherche Medicale, Commissariat a l'Energie Atomique, Helmhaltz Zentrum Fur Infektions Forschung GmbH
    Inventors: Annie Andrieux, Didier Job, Annie Schweitzer, Gerhard Höfle
  • Publication number: 20100249050
    Abstract: An epothilone glycoside having a formula of and a pharmaceutical composition having the epothilone glycoside and a pharmaceutically acceptable excipient. The epothilone glycoside or the pharmaceutical composition having the epothilone glycoside can prevent or treat cancers such as liver cancer, lung cancer, and breast cancer.
    Type: Application
    Filed: June 9, 2010
    Publication date: September 30, 2010
    Applicant: SHANDONG UNIVERSITY
    Inventors: Yuezhong LI, Yuemao SHEN, Lin ZHAO, Chunhua LU
  • Publication number: 20100234312
    Abstract: Novel avermectin derivatives of the formula (I) in which —C22R1-A-C23R2, R3, R4 and R5 have the meanings given in the description, processes for preparing these compounds and their use for controlling animal pests, and also novel intermediates and their preparation
    Type: Application
    Filed: August 8, 2007
    Publication date: September 16, 2010
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Peter Jeschke, Gunter Karig, Robert Velten, Reiner Fischer, Olga Malsam, Ulrich Görgens, Christian Arnold, Erich Sanwald, Achim Harder, Andreas Turberg
  • Patent number: 7781411
    Abstract: Certain derivatives of avermectin, avermectin monosaccharide and avermectin aglycone, having on the 4?, 4? or 13 position, respectively, a 6-membered cyclic acetal with a substituent on position 2, that are useful in controlling pests, in particular pests that are harmful to crop plants and to its propagation material, such as representatives of the class insecta, the order acarina and the class nematode, are provided.
    Type: Grant
    Filed: August 19, 2005
    Date of Patent: August 24, 2010
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Ottmar Franz Hueter, Thomas Pitterna, Pierre Jung, Fiona Murphy Kessabi, Laura Quaranta
  • Publication number: 20100210574
    Abstract: What is described are a compound of the formula wherein n is 0 or 1; A-B is —CH?CH— or —CH2—CH2—; R1 is C1-C12-alkyl, C3-C8-cycloalkyl or C2-C12-alkenyl; R2 is for example C1-C12-alkyl, C2-C12-alkenyl or C2-C12-alkinyl; which are optionally substituted with one to five substituents selected from the group consisting of OH, halogen, CN, —N3, —NO2, C3-C8-Cycloalkyl, norbornylenyl-, C3-C8-Cycloalkenyl; C3-C8-halocycloalkyl, C1-C12-alkoxy, C1-C6-alkoxy-C1-C6-alkoxy, C3-C8-cycloalkoxy, C1-C12-haloalkoxy, C1-C12-alkylthio, C3-C8-cycloalkylthio, C1-C12-haloalkylthio, C1-C12-alkylsulfinyl, C3-C8-cycloalkylsulfinyl, C1-C12-haloalkylsulfinyl, C3-C8-halocycloalkylsulfinyl, C1-C12-alkylsulfonyl, C3-C8-cycloalkylsulfonyl, C1-C12-haloalkylsulfonyl, C3-C8-halocycloalkylsulfonyl, —NR4R6, —X—C(?Y)—R4, —X—C(?Y)—Z—R4, —P(?O)(OC1-C6-alkyl)2, aryl, heterocyclyl, aryloxy, arylthio and heterocyclyloxy; R3 is for example H, C1-C12-alkyl or C1-C12-alkyl which is optionally substituted and, where applicable, to E/Z isomers, mix
    Type: Application
    Filed: April 27, 2010
    Publication date: August 19, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Peter Maienfisch, Fiona Murphy Kessabi, Jerome Cassayre, Laura Quaranta, Thomas Pitterna, Ottmar Franz Hueter, Pierre Jung
  • Publication number: 20100197622
    Abstract: Compounds of Formula I or II, and methods of making and using thereof, are described herein. M represents a macrolide subunit, n is a C1-6 group, optionally containing one or more heteroatoms, D is an alkyl or aryl group, A is a linking group connected to D, B is an alkyl, alkylaryl or alkylheteroaryl spacer group, ZBG is a Zinc Binding Group, R1, R2 and R4 are independently are selected from hydrogen, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a C1-6 alkanoate group, a C2-6 carbamate group, a C2-6 carbonate group, a C2-6 carbamate group, or a C2-6 thiocarbamate group, R3 is hydrogen or —OR5, R5 is selected from a group consisting of Hydrogen, a C1-6 alkyl hgroup, a C2-6 alkenyl group, a C2-6 alkynyl group, C1-6 alkanoate group, C2-6 carbamate group, C2-6 carbonate group, C2-6 carbamate group, or C2-6 thiocarbamate group.
    Type: Application
    Filed: December 21, 2009
    Publication date: August 5, 2010
    Inventor: Adegboyega Oyelere
  • Patent number: 7737261
    Abstract: Avermectin B1 and avermectin B1 monosaccharide derivative compounds having an alkoxymethyl substituent in the 4?- or 4?-position; a process for preparing and using these compounds and their tautomers; pesticides whose active compound is selected from these compounds and their tautomers; and a process for preparing these compounds and compositions are provided.
    Type: Grant
    Filed: December 19, 2003
    Date of Patent: June 15, 2010
    Assignee: Syngenta Corp Protection, Inc.
    Inventors: Peter Maienfisch, Fiona Murphy Kessabi, Jérôme Cassayre, Laura Quaranta, Thomas Pitterna, Ottmar Franz Hueter, Pierre Jung
  • Patent number: 7732416
    Abstract: What is described are a compound of the formula in which R1 is C1-C12alkyl, C3-C8cycloalkyl or C2-C12alkenyl; R2 is H, unsubstituted or mono- to pentasubstituted C1-C12alkyl or unsubstituted or mono- to pentasubstituted C1-C12alkenyl; R3 is C2-C12alkyl, mono- to pentasubstituted C1-C12alkyl, unsubstituted or mono- to pentasubstituted C1-C6alkoxy-C1-C6alkyl, unsubstituted or mono- to pentasubstituted C3-C12cycloalkyl, C2-C12alkenyl, C2-C12alkynyl; or R2 and R3 together are an alkylene or alkenylene bridge; with the proviso that R1 is not sec-butyl or isopropyl if R2 is H and R3 is 2-hydroxyethyl, isopropyl, n-octyl or benzyl; or, if appropriate, in E/Z isomer, an E/Z isomer mixture and/or a tautomer thereof; a process for preparing and using these compounds and their tautomers; pesticides whose active compound is selected from these compounds and their tautomers; and a process for preparing these compounds and compositions, and the use of these compounds and compositions.
    Type: Grant
    Filed: December 28, 2005
    Date of Patent: June 8, 2010
    Assignee: Merial Limited
    Inventors: Thomas Pitterna, Anthony Cornelius O'Sullivan, William Lutz
  • Publication number: 20100137234
    Abstract: Disclosed herein are 10-desmethyl, 10 substituted-macrolides, their preparation, pharmaceutical compositions containing them, their use and methods of treatment using them. The 10-desmethyl macrolides are particularly useful as antibiotics.
    Type: Application
    Filed: September 30, 2009
    Publication date: June 3, 2010
    Applicant: C10 Pharma AS
    Inventors: Kjell Undheim, Solvi Gunnes
  • Publication number: 20100120706
    Abstract: Macrolide compounds of formula I: with PDF4 inhibiting activity are described, wherein R1 is a residue —Y—X-Q; Y is S, SO or SO2; X is a bond or a linear group consisting of hydrogen atoms and with up to 9 atoms selected from C, N, O and/or S, of which up to 2 atoms can be N and one atom can be O or S, one carbon atom can appear as a CO group and the sulphur atom can appear as an SO2 group and two adjacent C atoms can be present as —CH?CH— or —C?C— and which group X is unsubstituted or is substituted with —COO—W or —CONH—W; Q is a residue —V-A1-L-A2-W or, if X does not represent a bond, may also be —NR6R7; V is a divalent aromatic or heterocyclic group; W is aryl or heterocyclyl; or in a group —V-A1-L-A2-W, wherein at least one of the groups A1; L or A2 is present, can also be a monovalent substituted or unsubstituted, saturated or unsaturated linear group with up to 5 atoms consisting of C, N, O and/or S of which one carbon can appear as a CO group one sulphur atom can appear as an SO2 group, A1, A2 are inde
    Type: Application
    Filed: August 8, 2007
    Publication date: May 13, 2010
    Inventors: Johannes Laurenz Kellenberger, Jürg Dreier, Stefan Bernhard Reinelt
  • Publication number: 20100113757
    Abstract: The invention provides novel Thuggacin-Type macrolide compounds which form rearrangement products forming a lacton bond to different carbon atoms. The novel compounds can be produced by fermentation of Sorangium cellulosum and Chondromyces crocatus and can be isolated by adsorption and chromoatograhic processing steps. The compounds are found to have antibiotic activity. The invention also relates to Thuggacin A, Thuggacin B, Thuggacin C, 13-Methyl-Thuggacin A, Thuggacin CMC-A, Thuggacin CMC-B and Thuggacin CMC-C AS Antimycobacterial Agents.
    Type: Application
    Filed: November 9, 2007
    Publication date: May 6, 2010
    Applicant: HELMHOLTZ-ZENTRUM FUR INFEKTIONSFORSCHUNG
    Inventors: Rolf Jansen, Brigitte Kunze, Herbert Irschik
  • Patent number: 7709447
    Abstract: A spinosyn or a physiologically acceptable derivative or salt thereof for promoting or accelerating wound healing in humans.
    Type: Grant
    Filed: April 29, 2004
    Date of Patent: May 4, 2010
    Assignee: Eli Lilly and Company
    Inventors: Kristina Clare Hacket, Lionel Barry Lowe
  • Patent number: 7704961
    Abstract: Described is a compound of the formula (I) wherein the bond between carbon atoms 22 and 23 is a single or double bond; m is 0 or 1; R1, is C1-C12alkyl, C3-C8cycloalkyl or C2-C12alkenyl; and either (A) R2 is —N(R3)R4, and (1) X is 0, wherein R3 is, for instance, hydrogen, unsubstituted or mono- to pentasubstituted C1-C12alkyl, and R4 is, for instance, mono- to pentasubstituted C1-C12alkyl, unsubstituted or mono- to pentasubstituted C3-C12cycloalkyl; or (2) X is S, wherein R3 is, for instance, hydrogen, unsubstituted or mono- to pentasubstituted C1-C12alkyl, and R4 is, for instance, hydrogen, unsubstituted or mono- to pentasubstituted C1-C12alkyl; or (3) X is 0 or S, wherein R3 and R4 together are, for instance, a three- to seven membered alkylene or a four- to seven-membered alkenylene bridge; or (B) R2 is OR5, X is 0 or S, wherein R5 is, for instance, C1-C12alkyl, mono- to pentasubstituted C1-C12alkyl; or, if appropriate, an E/Z isomer, E/Z isomer mixture and/or tautomer thereof, in each case in free form or
    Type: Grant
    Filed: August 27, 2004
    Date of Patent: April 27, 2010
    Assignee: Merial Limited
    Inventors: Fiona Murphy Kessabi, Thomas Pitterna, Peter Maienfisch, Jérôme Cassayre, Laura Quaranta, Pierre Jung, Ottmar Franz Hueter