Oxygen Containing Hetero Ring Having 12-19 Members (e.g., Methymycin, Carbomycin, Spiramycin, Etc.) Patents (Class 536/7.1)
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Publication number: 20130045936Abstract: 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: ApplicationFiled: December 15, 2010Publication date: February 21, 2013Applicant: North-West UniversityInventors: Wilna Leibenberg, Marique Aucamp, Melgardt M. De Villiers
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Publication number: 20120329741Abstract: 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: ApplicationFiled: May 25, 2012Publication date: December 27, 2012Inventors: Adegboyega Oyelere, Subhasish Tapadar
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Patent number: 8318684Abstract: 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: GrantFiled: May 15, 2007Date of Patent: November 27, 2012Assignees: Nimura Genetic Solutions Co., Ltd., Forest Research Institute MalaysiaInventors: 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
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Publication number: 20120283316Abstract: 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: ApplicationFiled: September 1, 2010Publication date: November 8, 2012Applicant: Northwestern UniversityInventors: Chad A. Mirkin, David A. Giljohann, Weston L. Daniel
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Publication number: 20120277174Abstract: 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: ApplicationFiled: August 13, 2010Publication date: November 1, 2012Applicant: BASILEA PHARMACEUTICA AGInventors: Johannes Laurenz Kellenberger, Jürg Dreier
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Publication number: 20120252747Abstract: 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: ApplicationFiled: June 18, 2012Publication date: October 4, 2012Inventors: 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
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Patent number: 8268975Abstract: 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: GrantFiled: April 3, 2009Date of Patent: September 18, 2012Assignees: DOW Agrosciences LLC, Kroff Chemical CompanyInventors: Paul Rey, Steve P. Ceplecha, David M. Sunderlik
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Patent number: 8263566Abstract: 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, mixtuType: GrantFiled: May 27, 2011Date of Patent: September 11, 2012Assignee: Merial LimitedInventors: Peter Maienfisch, Fiona Murphy Kessabi, Jerome Cassayre, Laura Quaranta, Thomas Pitterna, Ottmar Franz Hueter, Pierre Jung
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Patent number: 8263753Abstract: 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: GrantFiled: July 30, 2010Date of Patent: September 11, 2012Assignee: Intervet International B.V.Inventors: Monika Brink, Hans P. Niedermann, Tanja Schweisel, Stephan Veit, Kerstin Fleischhauer, Ralf Warrass, Heinz-Jorg Wennesheimer
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Publication number: 20120196819Abstract: 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: ApplicationFiled: January 4, 2012Publication date: August 2, 2012Applicant: NEWMARKET PHARMACEUTICALS LLCInventors: David ROCK, Mark RIDALL
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Publication number: 20120190635Abstract: 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: ApplicationFiled: September 27, 2010Publication date: July 26, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shengying Li, David H. Sherman, John Montgomery, Mani R. Chaulagain, Allison R. Knauff
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Patent number: 8227429Abstract: 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: GrantFiled: July 26, 2007Date of Patent: July 24, 2012Assignee: Intervet International B.V.Inventors: Ralf Warrass, Fritz Blatter, Meinrad Brenner, Guixan Hu, Tamo Rager
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Publication number: 20120172323Abstract: 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: ApplicationFiled: September 10, 2010Publication date: July 5, 2012Applicant: CEMPRA PHARMACEUTICALS, INC.Inventor: Prabhavathi Fernandes
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Publication number: 20120121702Abstract: 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: ApplicationFiled: January 25, 2012Publication date: May 17, 2012Applicant: Dow Pharmaceutical Sciences, Inc.Inventors: Radhakrishnan Pillai, Pramod Sarpotdar, David W. Osborne, Gordon J. Dow
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Publication number: 20120122808Abstract: 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: ApplicationFiled: January 26, 2012Publication date: May 17, 2012Applicant: INTERVET INTERNATIONAL B.V.Inventors: Ralf Warrass, Fritz Blatter, Meinrad Brenner, Guixan Hu, Timo Rager
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Publication number: 20120071429Abstract: 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: ApplicationFiled: July 26, 2011Publication date: March 22, 2012Inventors: Jonathan Duffield, Chan-Kou Hwang, Yoshitaka Ichikawa, Youe-Kong Shue
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Patent number: 8133871Abstract: 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: GrantFiled: October 13, 2006Date of Patent: March 13, 2012Assignees: The Kitasato Institute, Aphoenix, Inc.Inventors: Satoshi Omura, Toshiaki Sunazuka, Kenichiro Nagai, Hideaki Shima, Haruko Yamabe
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Publication number: 20120058963Abstract: 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: ApplicationFiled: November 15, 2011Publication date: March 8, 2012Applicant: Glaxo Group LimitedInventors: Sulejman Alihodzic, Martina Bosnar, Ognjen Culic, Vesna Erakovic Haber, Antun Hutinec, Dubravko Jelic, Goran Kragol, Nikola Marjanovic, Zorica Marusic-Istuk, Marija Ribic, Vanja Vela
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Publication number: 20120040922Abstract: 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: ApplicationFiled: October 24, 2011Publication date: February 16, 2012Inventors: Yoshi Ichikawa, Yu-Hung Chiu, Youe-Kong Shue, Farah Kondori Babakhani
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Publication number: 20120035352Abstract: 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: ApplicationFiled: July 18, 2011Publication date: February 9, 2012Inventors: 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
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Patent number: 8053418Abstract: 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: GrantFiled: January 24, 2006Date of Patent: November 8, 2011Assignee: Microbial Chemistry Research FoundationInventors: Toshiaki Miyake, Yoshiaki Takahashi
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Patent number: 8044030Abstract: 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: GrantFiled: November 28, 2008Date of Patent: October 25, 2011Assignee: Optimer Pharmaceuticals, Inc.Inventors: Yoshi Ichikawa, Yu-Hung Chiu, Youe-Kong Shue, Farah Kondori Babakhani
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Publication number: 20110237784Abstract: 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: ApplicationFiled: August 6, 2008Publication date: September 29, 2011Applicants: 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
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Publication number: 20110230429Abstract: 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, mixtuType: ApplicationFiled: May 27, 2011Publication date: September 22, 2011Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Peter Maienfisch, Fiona Murphy Kessabi, Jérôme Cassayre, Laura Quaranta, Thomas Pitterna, Ottmar Franz Hueter, Pierre Jung
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Patent number: 8017589Abstract: 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, mixtuType: GrantFiled: April 27, 2010Date of Patent: September 13, 2011Assignee: Syngenta Crop Protection LLCInventors: Peter Maienfisch, Fiona Murphy Kessabi, Jerome Cassayre, Laura Quaranta, Thomas Pitterna, Ottmar Franz Hueter, Pierre Jung
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Publication number: 20110178036Abstract: 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: ApplicationFiled: March 28, 2011Publication date: July 21, 2011Inventors: Lesley S. Burns, Paul R. Graupner, Paul Lewer, Christine J. Martin, William A. Vousden, Clive Waldron, Barrie Wilkinson
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Publication number: 20110124850Abstract: 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: ApplicationFiled: February 1, 2011Publication date: May 26, 2011Inventor: Jon Thorson
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Publication number: 20110071096Abstract: 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: ApplicationFiled: August 19, 2010Publication date: March 24, 2011Applicant: IDEXX Laboratories, Inc.Inventors: Murthy V.S.N. Yerramilli, Michael Randolph Atkinson, Hengguang Ll, Christopher Alan Cox
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Patent number: 7910558Abstract: 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: GrantFiled: January 23, 2004Date of Patent: March 22, 2011Assignee: Enanta Pharmaceuticals, Inc.Inventor: Yat Sun Or
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Publication number: 20110053875Abstract: 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: ApplicationFiled: July 30, 2010Publication date: March 3, 2011Inventors: Fritz Blatter, Meinrad Brenner, Monika Brink, Kerstin Fleischhauer, Guixian Hu, Hans Peter Niedermann, Timo Rager, Tanja Schweisel, Stephan Veit, Ralf Warrass, Heinz-Jörg Wennesheimer
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Publication number: 20110053876Abstract: 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: ApplicationFiled: February 9, 2009Publication date: March 3, 2011Inventors: Johannes Laurenz Kellenberger, Jürg Dreier, Stefan Bernhard Reinelt
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Publication number: 20110040078Abstract: 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: ApplicationFiled: October 10, 2008Publication date: February 17, 2011Applicants: SANDOZ AGInventors: Ingolf Macher, Dominic de Souza
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Publication number: 20110028417Abstract: The invention features novel macrocyclic compounds, methods of making the compounds, pharmaceutical compositions including the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: July 30, 2010Publication date: February 3, 2011Applicant: Synovo GmbHInventors: Hans-Jurgen Gutke, Michael Burnet, Jan-Hinrich Guse
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Patent number: 7879809Abstract: 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: GrantFiled: May 15, 2006Date of Patent: February 1, 2011Assignee: Eli Lilly and CompanyInventors: Clayton Paul Dick, Daniel Earl Snyder, Joseph Raymond Winkle
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Publication number: 20110021449Abstract: 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: ApplicationFiled: February 9, 2009Publication date: January 27, 2011Inventors: Johannes Laurenz Kellenberger, Jürg Dreier, Stefan Bernhard Reinelt
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Patent number: 7863249Abstract: 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: GrantFiled: April 11, 2008Date of Patent: January 4, 2011Assignee: Optimer Pharmaceuticals, Inc.Inventors: Yu-Hung Chiu, Tessie Mary Che, Alex Romero, Yoshi Ichikawa, Youe-Kong Shue
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Publication number: 20100280230Abstract: 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: ApplicationFiled: April 30, 2010Publication date: November 4, 2010Inventors: XINTANG RAO, Zhijian Ding, Hangbin Lou, Jing Wu, Yanglin Fang, Baineng Deng
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Patent number: 7816370Abstract: 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: GrantFiled: January 28, 2005Date of Patent: October 19, 2010Assignees: Institut National de la Sante et de la Recherche Medicale, Commissariat a l'Energie Atomique, Helmhaltz Zentrum Fur Infektions Forschung GmbHInventors: Annie Andrieux, Didier Job, Annie Schweitzer, Gerhard Höfle
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Publication number: 20100249050Abstract: 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: ApplicationFiled: June 9, 2010Publication date: September 30, 2010Applicant: SHANDONG UNIVERSITYInventors: Yuezhong LI, Yuemao SHEN, Lin ZHAO, Chunhua LU
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Publication number: 20100234312Abstract: 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 preparationType: ApplicationFiled: August 8, 2007Publication date: September 16, 2010Applicant: BAYER CROPSCIENCE AGInventors: Peter Jeschke, Gunter Karig, Robert Velten, Reiner Fischer, Olga Malsam, Ulrich Görgens, Christian Arnold, Erich Sanwald, Achim Harder, Andreas Turberg
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Patent number: 7781411Abstract: 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: GrantFiled: August 19, 2005Date of Patent: August 24, 2010Assignee: Syngenta Crop Protection, Inc.Inventors: Ottmar Franz Hueter, Thomas Pitterna, Pierre Jung, Fiona Murphy Kessabi, Laura Quaranta
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Publication number: 20100210574Abstract: 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, mixType: ApplicationFiled: April 27, 2010Publication date: August 19, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Peter Maienfisch, Fiona Murphy Kessabi, Jerome Cassayre, Laura Quaranta, Thomas Pitterna, Ottmar Franz Hueter, Pierre Jung
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Publication number: 20100197622Abstract: 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: ApplicationFiled: December 21, 2009Publication date: August 5, 2010Inventor: Adegboyega Oyelere
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Patent number: 7737261Abstract: 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: GrantFiled: December 19, 2003Date of Patent: June 15, 2010Assignee: Syngenta Corp Protection, Inc.Inventors: Peter Maienfisch, Fiona Murphy Kessabi, Jérôme Cassayre, Laura Quaranta, Thomas Pitterna, Ottmar Franz Hueter, Pierre Jung
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Patent number: 7732416Abstract: 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: GrantFiled: December 28, 2005Date of Patent: June 8, 2010Assignee: Merial LimitedInventors: Thomas Pitterna, Anthony Cornelius O'Sullivan, William Lutz
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Publication number: 20100137234Abstract: 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: ApplicationFiled: September 30, 2009Publication date: June 3, 2010Applicant: C10 Pharma ASInventors: Kjell Undheim, Solvi Gunnes
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Publication number: 20100120706Abstract: 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 indeType: ApplicationFiled: August 8, 2007Publication date: May 13, 2010Inventors: Johannes Laurenz Kellenberger, Jürg Dreier, Stefan Bernhard Reinelt
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Publication number: 20100113757Abstract: 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: ApplicationFiled: November 9, 2007Publication date: May 6, 2010Applicant: HELMHOLTZ-ZENTRUM FUR INFEKTIONSFORSCHUNGInventors: Rolf Jansen, Brigitte Kunze, Herbert Irschik
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Patent number: 7709447Abstract: A spinosyn or a physiologically acceptable derivative or salt thereof for promoting or accelerating wound healing in humans.Type: GrantFiled: April 29, 2004Date of Patent: May 4, 2010Assignee: Eli Lilly and CompanyInventors: Kristina Clare Hacket, Lionel Barry Lowe
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Patent number: 7704961Abstract: 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 orType: GrantFiled: August 27, 2004Date of Patent: April 27, 2010Assignee: Merial LimitedInventors: Fiona Murphy Kessabi, Thomas Pitterna, Peter Maienfisch, Jérôme Cassayre, Laura Quaranta, Pierre Jung, Ottmar Franz Hueter