Additional Nitrogen Containing Patents (Class 536/7.4)
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Patent number: 8097708Abstract: [Object]: To provide a compound having a novel structure effective against Hemophilus influenzae and erythromycin resistant bacteria (for example, resistant pneumococci and streptococci) as well as against conventional erythromycin sensitive bacteria. [Solution]: A novel 10a-azalide compound represented by the formula (I), a pharmaceutically acceptable salt thereof or a solvate thereof, or an intermediate for the preparation of the same. The compound of the present invention has superior antibacterial activity against Hemophilus influenzae, erythromycin resistant pneumococci and the like, and therefore, the compound can be used as a therapeutic agent of infectious diseases.Type: GrantFiled: February 7, 2007Date of Patent: January 17, 2012Assignees: Taisho Pharmaceutical Co., Ltd., Meiji Seika Kaisha, Ltd.Inventors: Tomohiro Sugimoto, Kanako Yamamoto, Akira Manaka, Haruhisa Ogita, Jun Kurosaka, Madoka Kawamura, Masato Kashimura, Naoki Sasamoto, Tomoaki Miura, Kenichi Kanemoto, Tomohiro Ozawa, Ken Chikauchi, Eiki Shitara, Dai Kubota
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Patent number: 8097594Abstract: The present invention provides compounds having antimicrobial activity for preventing and treating diseases caused by microbial infections. Thus, the present invention relates to novel semi-synthetic 11,12-? lactone macrolides and ketolides having antimicrobial activity, processes for making compounds as well as pharmaceutical compositions containing said compounds as active ingredients and methods of treating microbial infections with the compounds.Type: GrantFiled: February 24, 2009Date of Patent: January 17, 2012Assignee: Wockhardt Ltd.Inventors: Milind Dattatraya Sindkhedkar, Vijaya Narayan Desai, Rajesh Maganlal Loriya, Mahesh Vithalbhai Patel, Bharat Kalidas Trivedi, Rajesh Onkardas Bora, Santosh Devidas Diwakar, Ganesh Rajaram Jadhav, Shivaji Sampatrao Pawar
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Patent number: 8080529Abstract: 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: GrantFiled: January 13, 2006Date of Patent: December 20, 2011Assignee: 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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Patent number: 8076301Abstract: 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: GrantFiled: September 30, 2009Date of Patent: December 13, 2011Assignee: C10 Pharma ASInventors: Kjell Undheim, Solvi Gunnes
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Patent number: 8063021Abstract: Compounds according to formula I wherein m is 0 or 1; X is and R1, R2, R3 R4, and R5 are as defined herein, are useful as anti-infective agents.Type: GrantFiled: June 30, 2004Date of Patent: November 22, 2011Assignee: Kosan Biosciences IncorporatedInventors: Yong Li, Yandong Li, Yan Zhu, Chaitan Khosla, David C. Myles
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Publication number: 20110281812Abstract: 2?-O-substituted 14- or 15-membered azalide macrolides of Formula (I) wherein R6 represents (i) —C1-8alkyl, unsubstituted or substituted at the terminal carbon atom by a group selected from hydroxy, —C1-3alkoxy and —C(O)OC1-3alkyl, or when —C1-8alkyl is branched, substitution can alternatively be by a hydroxyl group at each of two terminal carbon atoms, (ii) —CH(NH2)C1-4alkyl, wherein the —C1-4alkyl group may be optionally interrupted by a heteroatom selected from O, S and N, (iii) —CH2N(R7)(R8), wherein R7 and R8 each independently represent H or —C1-3alkyl provided that R7 and R8 cannot both simultaneously represent H, (iv) a 4-6-membered heterocyclic ring containing up to 2 heteroatoms independently selected from O, S and N, wherein the heterocyclic ring is unsubstituted or substituted by —C1-3alkyl, (v) 5-6 membered heteroaromatic ring, unsubstituted or substituted by one to three groups independently selected from halo, hydroxyl, —C1-3alkyl, —C1-3alkoxy, —CF3, —OCF3 and —NH2, (vi) —CH(NH2)CHType: ApplicationFiled: January 28, 2010Publication date: November 17, 2011Inventors: Sulejman Alihodzic, Antun Hutinec, Sanja Kostrun, Maja Matanovic Skugor, Ivana Palej Jakopovic
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Patent number: 8030282Abstract: The invention provides polymorphs of a motilide having a structure represented by formula IaType: GrantFiled: April 16, 2010Date of Patent: October 4, 2011Inventors: Peter J. Licari, Jorge L. Galazzo, Greg O. Buchanan, Alexander Redvers Eberlin, Mark D. Eddleston
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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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Patent number: 8012943Abstract: 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: GrantFiled: April 27, 2009Date of Patent: September 6, 2011Assignee: Optimer Pharmaceuticals, Inc.Inventors: Jonathan Duffield, Chan-Kou Hwang, Yoshitaka Ichikawa, Youe-Kong Shue
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Patent number: 7989600Abstract: The present invention relates to new macrolide compounds represented by the general structure I, wherein M is a macrolide, P is a photo-affinity group bearing subunit containing biotin, and L is a linking molecule, and to their pharmaceutically acceptable salts and solvates, to processes and intermediates for their preparation and to the use of these compounds for the macrolide target identification.Type: GrantFiled: January 13, 2006Date of Patent: August 2, 2011Assignee: GlaxoSmithKline Istrazivacki Centar Zagreb D.O.O.Inventors: Ognjen Culic, Martina Bosnar, Nikola Marjanovic, Boris Mildner, Linda Tomaskovic, Sulejman Alihodzic
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Publication number: 20110184158Abstract: The present invention relates to a macrolide derivative as well as preparation and use thereof. The macrolide derivative of the present invention, i.e., a hydrate of erythromycin salts, has a molecular formula of C37H67NO13.A.nH2O, n=1.0-11.0, in which A is an organic acid or an organic acids, selected from lactobionic acid, thiocyanic acid, maleic acid, fumaric acid, thiocyanic acid, acetic acid, methanesulfonic acid, benzenesulfonic acid, nicotinic acid, lactic acid, citric acid, tartaric acid, aspartic acid, glutamic acid and phosphoric acid, the hydrate has good water solubility and better storage stability, which is suitable for the manufacture of a medicament for the treatment and prophylaxis of infectious diseases in human or animal caused by Gram-positive or negative bacteria.Type: ApplicationFiled: July 10, 2009Publication date: July 28, 2011Inventor: Li Liu
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Patent number: 7928078Abstract: The present invention relates to novel compounds represented by the structure I and pharmaceutical preparations thereof for the treatment of inflammatory diseases in humans and animals.Type: GrantFiled: September 16, 2008Date of Patent: April 19, 2011Assignee: GlaxoSmithKline Istrazivacki Centar Zagreb D.O.O.Inventors: Mladen Mercep, Milan Mesic, Linda Tomaskovic, Marijana Komac, Boska Hrvacic, Stribor Markovic
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Patent number: 7910559Abstract: The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides lacking cladinose sugar substituted at the C-3 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-6, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.Type: GrantFiled: January 13, 2006Date of Patent: March 22, 2011Assignee: GlaxoSmithKline istrazivacki centar Zagreb d.o.o.Inventors: Ognjen Culic, Martina Bosnar, Sulejman Alihodzic, Gorjana Lazarevski, Zorica Marusic Istuk, Antun Hutinec, Vanja Vela, Goran Kragol
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Publication number: 20110039795Abstract: Novel 2?-O,3?-N-bridged macrolides useful in treatment of inflammatory diseases. More particularly, the invention relates to 2?-O,3?-N-bridged 14-membered macrolides and to 2?-O,3?-N-bridged 15-membered azalide macrolides useful in treatment of neutrophil dominated inflammatory diseases resulting from neutrophilic infiltration and/or diseases associated with altered cellular functionality of neutrophils, to intermediates for their preparation, to the methods for their preparation, to their use as therapeutic agents, and to salts thereof.Type: ApplicationFiled: April 20, 2009Publication date: February 17, 2011Inventors: Mirjana Bukvic-Krajacic, Antun Hutinec, Goran Kragol, Nedjeljko Kujundzic, Zorica Marusic-Istuk
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Patent number: 7872109Abstract: The invention provides polymorphs of a motilide having a structure represented by formula IaType: GrantFiled: December 4, 2007Date of Patent: January 18, 2011Inventors: Peter J. Licari, Jorge L. Galazzo, Greg O. Buchanan, Alexander Redvers Eberlin, Mark D. Eddleston
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Publication number: 20100227829Abstract: The invention provides polymorphs of a motilide having a structure represented by formula IaType: ApplicationFiled: April 16, 2010Publication date: September 9, 2010Applicant: PFIZER INC.Inventors: Peter J. Licari, Jorge L. Galazzo, Greg O. Buchanan, Alexander Redvers Eberlin, Mark D. Eddleston
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Publication number: 20100216731Abstract: Described herein are processes for the preparation of compounds of formula (I): and pharmaceutically acceptable salts, solvates, and hydrates thereof.Type: ApplicationFiled: October 23, 2008Publication date: August 26, 2010Applicant: CEMPRA PHARMACEUTICALS, INC.Inventors: David E. Pereira, Manish Kanchanbhai Patel, Keshav Deo
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Publication number: 20100197623Abstract: The compound 3?-N-demethyl-4?-O-(2-diethylaminoethanoyl)-6-O-methyl-9a-aza-9a-homoerythromycin A, having the Formula (I): or a salt thereof, compositions comprising the compound, its use in the treatment of neutrophil dominated inflammatory diseases, and methods for its preparation.Type: ApplicationFiled: January 28, 2010Publication date: August 5, 2010Inventors: Caroline Jane Day, Julien Bruno Douillet, Darko Filic, Leanda Jane Kindon, Goran Kragol, Zorica Marusic-Istuk
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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: 7767797Abstract: The invention features novel macrocyclic compounds, methods of making the compounds, pharmaceutical compositions including the compounds, and methods of treatment using the compounds.Type: GrantFiled: September 30, 2005Date of Patent: August 3, 2010Assignee: Synovo GmbHInventors: Hans-Jurgen Gutke, Michael Burnet, Jan-Hinrich Guse
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Publication number: 20100145035Abstract: The present invention relates to methods for synthesizing macrolide compounds which are known to have antibacterial activity, and are useful in the therapy of bacterial infections in mammals. More specifically, the invention relates to methods for synthesizing the macrolide antibiotic, gamithromycin utilizing a novel configuration of catalysts, chemical structures, and/or methods. An embodiment of the present invention may include allowing multiple chemical reactions to proceed without the isolation of chemical intermediates. Thus, multiple reactions may occur in one reaction vessel allowing for a considerable decrease in the cycle-time. The present invention also provides a novel method for inhibiting degradation while isolating a structure of a pharmaceutical composition.Type: ApplicationFiled: October 23, 2009Publication date: June 10, 2010Inventors: Zita Mendes, António Carlos Silva Henriques, William Heggie
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Publication number: 20100130437Abstract: A topical pharmaceutical composition comprising an antibiotic is useful for the prevention of Lyme disease.Type: ApplicationFiled: July 24, 2008Publication date: May 27, 2010Inventors: Gustave Huber, Uta Hüttenes, Caroline Roosens-von Bidder
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Patent number: 7718621Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, having antimicrobial activity, processes for their preparation, compositions containing them and to their use in medicine.Type: GrantFiled: November 9, 2005Date of Patent: May 18, 2010Assignees: Glaxo Group Ltd., Pliva-Istrazivacki InstitutInventors: Desmond John Best, John Stephen Elder, Andrew Keith Forrest, Robert John Sheppard, Andrea Fajdetic
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Patent number: 7704960Abstract: Macrolide compounds endowed with antiinflammatory activity are described, and more particularly macrolide derivatives lacking cladinose in position 3, with antiinflammatory activity, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing them as active ingredient.Type: GrantFiled: October 28, 2008Date of Patent: April 27, 2010Assignee: Zambon Group S.p.A.Inventors: Mauro Napoletano, Ermanno Moriggi, Andrea Mereu, Fernando Ornaghi, Gabriele Morazzoni, Roberto Longoni, Carlo Riva, Luciano Pacchetti, Franco Pellacini
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Publication number: 20100099634Abstract: The present invention relates to macrolide derivatives of formula (I) in which R1 and R2 have the meanings given in the description; which are endowed with antiinflammatory activity and are substantially free of antibiotic properties, to pharmaceutically acceptable salts thereof and to pharmaceutical compositions containing them as active ingredient.Type: ApplicationFiled: December 12, 2006Publication date: April 22, 2010Applicant: Zambon S.p.AInventors: Andrea Mereu, Ermanno Moriggi, Mauro Napoletano, Franco Pellacini
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Patent number: 7683162Abstract: The present invention provides a process of preparing a crystalline azithromycin monohydrate. The process involves dissolving azithromycin in a solution containing ethanol, adding the dissolved azithromycin into water to precipitate the crystals, isolating and drying the precipitate to a water content of about 5% (w/w) to about 7% (w/w). The resulting azithromycin monohydrate is stable, exhibiting less than 2% degradation, and non-hydroscopic.Type: GrantFiled: August 24, 2005Date of Patent: March 23, 2010Assignee: Taro Pharmaceutical Industries LimitedInventors: Daniella Gutman, Lea Shachal
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Publication number: 20100041618Abstract: 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 processes by which to make the compounds of the present invention.Type: ApplicationFiled: August 18, 2009Publication date: February 18, 2010Inventors: Guoqiang Wang, Ly Tam Phan, Yat Sun Or, Yao-Ling Qiu, Deqiang Niu, Yulin Peng, Marina Busuyek, Yanchun Wang, Suanne Nakajima
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Patent number: 7622452Abstract: The present invention discloses compounds of formulae (I), (II) 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: GrantFiled: November 15, 2007Date of Patent: November 24, 2009Assignee: Enanta Pharmaceuticals, Inc.Inventors: Ly Tam Phan, Yao-Ling Qiu, Yat Sun Or
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Publication number: 20090281292Abstract: [Object]: To provide a compound having a novel structure effective against Hemophilus influenzae and erythromycin resistant bacteria (for example, resistant pneumococci and streptococci) as well as against conventional erythromycin sensitive bacteria. [Solution]: A novel 10a-azalide compound represented by the formula (I), a pharmaceutically acceptable salt thereof or a solvate thereof, or an intermediate for the preparation of the same. The compound of the present invention has superior antibacterial activity against Hemophilus influenzae, erythromycin resistant pneumococci and the like, and therefore, the compound can be used as a therapeutic agent of infectious diseases.Type: ApplicationFiled: February 7, 2007Publication date: November 12, 2009Inventors: Tomohiro Sugimoto, Kanako Yamamoto, Akira Manaka, Haruhisa Ogita, Jun Kurosaka, Madoka Kawamura, Masato Kashimura, Naoki Sasamoto, Tomoaki Miura, Kenichi Kanemoto, Tomohiro Ozawa, Ken Chikauchi, Eiki Shitara, Dai Kubota
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Publication number: 20090281293Abstract: The present invention relates to processes and intermediates for the preparation of 2-fluoro 6-11 bicyclic erythromycin derivatives.Type: ApplicationFiled: May 8, 2009Publication date: November 12, 2009Inventors: Guoyou Xu, Datong Tang, In Jong Kim, Ly Tam Phan, Yat Sun Or, Zhe Wang
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Patent number: 7608596Abstract: 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: GrantFiled: December 22, 2003Date of Patent: October 27, 2009Assignee: C10 Pharma ASInventors: Kjell Undheim, Solvi Gunnes
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Patent number: 7601695Abstract: Described herein are novel macrolides, the preparation of novel macrolides, to the use of novel macrolides for preventing, treating, or ameliorating various conditions, and the use of novel macrolides as antibacterial agents.Type: GrantFiled: March 5, 2004Date of Patent: October 13, 2009Assignee: Optimer Pharmaceuticals, Inc.Inventors: Chang-Hsing Liang, Jonathan Duffield, Alex Romero, Yu-Hung Chiu, David Rabuka, Sulan Yao, Steve Sucheck, Kenneth Marby, Youe-kong Shue, Yoshi Ichikawa, Chan-Kou Hwang
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Publication number: 20090247478Abstract: The present invention provides compounds having antimicrobial activity for preventing and treating diseases caused by microbial infections. Thus, the present invention relates to novel semi-synthetic 11,12-? lactone macrolides and ketolides having antimicrobial activity, processes for making compounds as well as pharmaceutical compositions containing said compounds as active ingredients and methods of treating microbial infections with the compounds.Type: ApplicationFiled: February 24, 2009Publication date: October 1, 2009Inventors: Milind Dattatraya Sindkhedkar, Vijaya Narayan Desai, Rajesh Maganlal Loriya, Mahesh Vithalbhai Patel, Bharat Kalidas Trivedi, Rajesh Onkardas Bora, Santosh Devidas Diwakar, Ganesh Rajaram Jadhav, Shivaji Sampatrao Pawar
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Patent number: 7595300Abstract: 15-fluoroketolides of the formula having improved activity and safety, compositions comprising them, and methods for their preparation and use in the treatment of bacterial infections.Type: GrantFiled: December 7, 2006Date of Patent: September 29, 2009Assignee: Kosan Biosciences IncorporatedInventors: Simon James Shaw, Gary W Ashley, Mark A. Burlingame
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Patent number: 7589067Abstract: 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: GrantFiled: October 10, 2006Date of Patent: September 15, 2009Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Guoqiang Wang, Tongzhu Liu, Ly Tam Phan
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Patent number: 7582611Abstract: Compounds having a structure according to formula (I) where RA, RB, RC, RD, RE, and RF are as defined herein, are useful as prokinetic agents.Type: GrantFiled: May 2, 2006Date of Patent: September 1, 2009Assignee: Pfizer Inc.Inventors: Yaoquan Liu, Christopher Carreras, David C. Myles, Yong Li, Simon James Shaw, Hong Fu, Yue Chen, Hao Zheng, Yandong Li, Mark A. Burlingame
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Patent number: 7579324Abstract: This invention features a compound of the following formula: T-(-L-C)m, T is a transportophore, L is a bond or a linker having a molecular weight up to 240 dalton, C is a non-antibiotic therapeutic agent, and m is 1, 2, 3, 4, 5, 6, 7, or 8, in which the transportophore has an immune selectivity ratio of at least 2, the transportophore is covalently bonded to the non-antibiotic therapeutic agent via the bond or the linker, and the compound has an immune selectivity ratio of at least 2.Type: GrantFiled: February 14, 2003Date of Patent: August 25, 2009Assignee: c-a-i-r biosciences GmbHInventors: Michael Burnet, Jan-Hinrich Guse, Hans-Jurgen Gutke, Albert Beck, Georgia Tsotsou, Irina Droste-Borel, Jeannette Reichert, Kattie Luyten, Maximilian Busch, Michael Wolff, Moussa Khobzaoui, Simona Margutti, Thomas Meindl, Gene Kim, Laurence Barker
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Patent number: 7572773Abstract: The present disclosure related to a method of treating an infection by oral administration of a single dose of a fast dissolving form of azithromycin. The disclosure also relates to a method of reducing the adverse effects arising from treatment of a subject having an infection by administering a single dose of a fast dissolving form of azithromycin.Type: GrantFiled: July 22, 2004Date of Patent: August 11, 2009Assignee: Pliva Hrvatska D.O.O.Inventors: Aleksandar Danilovski, Knezevic Zdravka
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Patent number: 7569549Abstract: Substantially pure isostructural pseudopolymorphs of 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A having the Formula I: wherein S is an organic solvent which is at least partially miscible with water, x is 1, 1.25, 1.5 or 2, y is 0, 0.5, or 1, the pseudopolymorph being characterized by the monoclinic space group P21 and average unit cell parameters comprising: crystal axis lengths of a=15.5-17.0 ?, b=15.5-17.0 ?, and c=17.5-19.5 ?, and angles between the crystal axes of ?=?=90° and ?=106°-112°. In addition, this disclosure is directed to processes for the preparation of the substantially pure isostructural pseudopolymorphs of Formula I; to pharmaceutical compositions containing substantially pure isostructural pseudopolymorphs of Formula I; and to a method for the treatment of bacterial and protozoan infections, and inflammation-related diseases by administration of a pharmaceutical composition containing the substantially pure isostructural pseudopolymorphs of Formula I.Type: GrantFiled: March 17, 2003Date of Patent: August 4, 2009Assignee: Pliva Hrvatska D.O.O.Inventors: Miljenko Dumic, Mladen Vinkovic, Marina Oresic, Ernest Mestrovic, Aleksandar Danilovski, Alojz Dumbovic, Zdravka Knezevic, Gorjana Lazarevski, Dominik Cincic, Darko Filic, Katica Lazaric, Dejan Kresimir Bucar
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Patent number: 7569550Abstract: The present invention relates to 14- or 15-membered macrolides substituted at the 4? position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical microbial infections in a human or animal body.Type: GrantFiled: May 11, 2004Date of Patent: August 4, 2009Assignees: Glaxo Group Limited, Pliva-Istrazivacki InstitutInventors: Sulejman Alihodzic, Andrew Keith Forrest, Richard Lewis Jarvest, Gorjana Lazarevski, Drazen Pavlovic
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Patent number: 7563877Abstract: The present invention relates to processes and intermediates for the preparation of 6-11 bicyclic erythromycin derivative known as EDP-182 (IX-a).Type: GrantFiled: January 23, 2007Date of Patent: July 21, 2009Assignee: Enanta Pharmaceuticals, Inc.Inventors: Guoyou Xu, Yonghua Gai, Guoqlang Wang, Yat Sun Or, Zhe Wang
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Patent number: 7547679Abstract: The present invention relates to 14- or 15-membered macrolides substituted at the 4? position of formula (I) and pharmaceutically acceptable derivatives thereof, to processes for their preparation and their use in therapy or prophylaxis of systemic or topical microbial infections in a human or animal body.Type: GrantFiled: May 9, 2006Date of Patent: June 16, 2009Assignees: GlaxoSmithKline istrazivacki center Zagreb d.o.o, Glaxo Group LimitedInventors: Sulejman Alihodzic, Drazen Pavlovic, Eric Hunt, Andrew Keith Forrest, Ivana Palej, Samra Kapic, Vlado Stimac
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Publication number: 20090130225Abstract: The present invention provides macrolide derivatives, which can be used as antibacterial agents. Compounds described herein can be used for treating or preventing conditions caused by or contributed to by gram-positive, gram-negative or anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Moraxalla spp., Chlamydia spp., Mycoplasm, Legionella spp., Mycobacterium, Helicobacter, Clostridium, Bacteroides, Corynebacterium, Propionibeacterium, Bacillus, Enterobactericeae or any combination thereof. Also provided are processes for preparing compounds described herein, pharmaceutical compositions thereof, and methods of treating bacterial infections.Type: ApplicationFiled: November 21, 2006Publication date: May 21, 2009Inventors: Anjan Chakrabarti, Biswajit Das, Jitendra Sambhaji Jadhav, Dilip J. Upadhyay
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Patent number: 7524823Abstract: The present invention relates to new antibiotic macrolide compounds of the general formula I: with improved activity, to medicaments comprising such antibiotics, and to the use of such antibiotics for the treatment of infectious diseases, inflammatory diseases and human diseases or disorders which can be ameliorated by inhibition human phospdiesterases.Type: GrantFiled: May 8, 2006Date of Patent: April 28, 2009Assignee: Basilea Pharmaceutica AGInventors: Johannes Laurenz Kellenberger, Stuart Robert Shapiro, Salima Mathews, Philippe Guerry, Pierre Jacques Noël Barbier
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Patent number: 7521428Abstract: Macrolide derivatives having enhancing effect for activities of azole antifungal agents, acting at low concentration and within a short time against fungal infection and reducing the frequency of appearance of resistant microorganisms. One such substance is a compound represented by the formula [I]: wherein R1 is Ac, R2 and R3 are Ac, and R4 is Me; when R1 is H, R2 and R3 are Ac, and R4 is Me; when R1 is H, R2 and R3 are Ac, and R4 is H, when R1 Bzl, R2 and R3 are Bzl, and R4 is Me; when R1 is Ac, R2 and R3 are Pr, and R4 is Me; when R1 is Ac, R2 and R3 are Hex, and R4 is Me; when R1 is Ac, R2 and R3 are Bzl, and R4 is Me; when R1 is H, R2 and R3 are Pr, and R4 is Me; when R1 is H, R2 and R3 are Hex, and R4 is Me; when R1 is H, R2 and R3 are Bzl, and R4 is Me; when R1 is H, R2 is H, R3 is Bzl, and R4 is Me; when R1 is H, R2 and R3 are Hex, and R4 is H, or when R1 is H, R2 and R3 are Hex, and R4 is Et.Type: GrantFiled: October 29, 2002Date of Patent: April 21, 2009Assignee: The Kitasato InstituteInventors: Satoshi Omura, Hiroshi Tomoda, Toshiaki Sunazuka, Masayoshi Arai, Tohru Nagamitsu
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Patent number: 7517859Abstract: 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: GrantFiled: May 3, 2006Date of Patent: April 14, 2009Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yonghua Gai, Datong Tang, Ying Sun, Zhigang Chen, Yat Sun Or, Zhe Wang
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Patent number: 7507721Abstract: Macrolide compounds of formula (I) wherein X, R, R1, R2, R3 and R4, have the meanings as defined in the specification, pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them as active ingredient and the use thereof in the treatment and prophylaxis of inflammatory diseases, are described.Type: GrantFiled: January 25, 2005Date of Patent: March 24, 2009Assignee: Zambon Group S.p.A.Inventors: Andrea Mereu, Mauro Napoletano, Fernando Ornaghi, Ermanno Moriggi, Franco Pellacini
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Publication number: 20090075917Abstract: The present application describes deuterium-enriched telithromycin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: September 15, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090062220Abstract: The present application describes deuterium-enriched azithromycin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 21, 2008Publication date: March 5, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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Publication number: 20090054357Abstract: Macrolide compounds endowed with antiinflammatory activity are described, and more particularly macrolide derivatives lacking cladinose in position 3, with antiinflammatory activity, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing them as active ingredient.Type: ApplicationFiled: October 28, 2008Publication date: February 26, 2009Applicant: ZAMBON GROUP S.P.A.Inventors: Mauro NAPOLETANO, Ermanno Moriggi, Andrea Mereu, Fernando Ornaghi, Gabriele Morazzoni, Roberto Longoni, Carlo Riva, Luciano Pacchetti, Franco Pellacini