Boron, Phosphorus Or Sulfur Containing Patents (Class 536/7.3)
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Publication number: 20140046043Abstract: A macrolide compound represented by the formula (I) effective against erythromycin resistant bacteria (for example, resistant pneumococci, streptococci and mycoplasmas).Type: ApplicationFiled: February 20, 2012Publication date: February 13, 2014Applicants: MEIJI SEIKA PHARMA CO., LTD., TAISHO PHARMACEUTICAL CO., LTD.Inventors: Tomohiro Sugimoto, Naoki Sasamoto, Jun Kurosaka, Masato Hayashi, Kanako Yamamoto, Masato Kashimura, Yasunobu Ushiki, Haruhisa Ogita, Tomoaki Miura, Kenichi Kanemoto, Kou Kumura, Satoshi Yoshida, Keiji Tamura, Eiki Shitara
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Patent number: 8461120Abstract: 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: July 30, 2010Date of Patent: June 11, 2013Assignee: Synovo GmbHInventors: Hans-Jurgen Gutke, Michael Burnet, Jan-Hinrich Guse
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Patent number: 8445451Abstract: 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: GrantFiled: February 9, 2009Date of Patent: May 21, 2013Assignee: Basilea Pharmaceutica AGInventors: Johannes Laurenz Kellenberger, Jürg Dreier, Stefan Bernhard Reinelt
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Patent number: 8410065Abstract: The invention relates to antibiotic macrolides of formula (I), which have improved anti-inflammatory activity mediated through inhibition of phosphodiesterase 4 (PDE4) useful for the treatment and/or prevention of inflammatory, allergic and proliferative diseases.Type: GrantFiled: February 9, 2009Date of Patent: April 2, 2013Assignee: Basilea Pharmaceutica AGInventors: Johannes Laurenz Kellenberger, Jürg Dreier, Stefan Bernhard Reinelt
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Patent number: 8273720Abstract: 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: February 18, 2009Date of Patent: September 25, 2012Assignee: Enanta Pharmaceuticals, Inc.Inventors: In Jong Kim, Tongzhu Liu, Heejin Kim, Yanchun Wang, Yao-Ling Qiu, Ly Tam Phan, Yat Sun Or
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Patent number: 8173609Abstract: New macrolide general compounds of formula I with improved activity making them useful for inhibiting human phosphodiesterase 4 and treating chronic obstructive pulmonary disease (COPD).Type: GrantFiled: August 8, 2007Date of Patent: May 8, 2012Assignee: Basilea Pharmaceutica AGInventors: Johannes Laurenz Kellenberger, Jürg Dreier, Stefan Bernhard Reinelt
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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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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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Publication number: 20090111760Abstract: A compound of formula (I) compositions comprising same, processes for their preparation and use of said compounds, particularly in the treatment of microbial infections.Type: ApplicationFiled: November 9, 2005Publication date: April 30, 2009Inventor: Catherine Simone Victoire Frydrych
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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: 20090062218Abstract: A compound of formula (I) compositions comprising same, processes for their preparation and use of said compounds, particularly in the treatment of microbial infections.Type: ApplicationFiled: November 9, 2005Publication date: March 5, 2009Applicant: GLAXO GROUP LIMITEDInventors: Andrew Keith Forrest, Robert John Sheppard
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Publication number: 20080241959Abstract: 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: ApplicationFiled: January 13, 2006Publication date: October 2, 2008Applicant: GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.Inventors: Ognjen Culic, Martina Bosnar, Nikola Marianovic, Boris Mildner, Linda Tomaskovic, Sulejman Alihodzic
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Patent number: 7419962Abstract: 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: December 6, 2005Date of Patent: September 2, 2008Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Datong Tang, Ying Sun, Yonghua Gai, Guoyou Xu, Zhe Wang
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Patent number: 7414030Abstract: The present invention discloses compounds of formulaes I, II, III, or IV, or a racemate, enantiomer, regioisomer, salt, ester or prodrug 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: January 5, 2005Date of Patent: August 19, 2008Assignee: Enanta Pharmaceuticals, Inc.Inventors: Nha Huu Vo, Guoqiang Wang, Guoyou Xu, Ying Hou, Ying Sun, Ly Tam Phan, Zhe Wang, Yat Sun Or
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Patent number: 7407942Abstract: 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 16, 2006Date of Patent: August 5, 2008Assignee: Emata Pharmaceuticals, IncInventors: Yat Sun Or, Deqiang Niu, Zhe Wang
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Patent number: 7365056Abstract: The invention relates to substituted 9a-N-{N?-[4-(sulfonyl)phenyl]carbamoyl} derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-0-desosaminyl-9-deoxo-9-di-hydro-9a-aza-9a-homoerithronolide A, novel semisynthetic macrolide antibiotics of the azalide series general formula (1), wherein R represents H or cladinosyl moiety and R1 represents chloro, amino, phenylamino, 2-pyridylamino, 3,4-dimethyl-4-isoxalylamino and 5-methyl-3-isoxazolylamino group, and pharmaceutically acceptable addition salts thereof with inorganic or organic acids.Type: GrantFiled: November 10, 2003Date of Patent: April 29, 2008Assignee: GlaxoSmithKline istrazivacki centar Zagreb d.oInventors: Nedjeljko Kujundzic, Mirjana Bukvic Krajacic, Karmen Brajsa
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Patent number: 7291602Abstract: 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: December 13, 2005Date of Patent: November 6, 2007Assignee: Enanta Pharmaceuticals, Inc.Inventors: Datong Tang, Yonghua Gai, Ying Sun, Zhigang Chen, Yat Sun Or, Zhe Wang
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Patent number: 7229972Abstract: 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: December 7, 2004Date of Patent: June 12, 2007Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Datong Tang, Yonghua Gai, Ying Sun, Guoyou Xu, Zhe Wang
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Patent number: 7071170Abstract: This invention relates to compounds of the formula wherein a, R1, R2, R3, R4, R5, R6 and X are each as defined above, and to pharmaceutically acceptable salts thereof, useful as potent antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating bacterial and protozoal infections by administering the compounds of formula I.Type: GrantFiled: July 21, 2004Date of Patent: July 4, 2006Assignee: Pfizer Inc.Inventor: Takushi Kaneko
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Patent number: 7049417Abstract: Novel 6,11-4-carbon bridged ketolides, pharmaceutically-acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically-acceptable carrier are described. Also described are a method for treating bacterial infections by administering to an animal a pharmaceutical composition containing a therapeutically effective amount of a compound of the invention and processes for the preparation of such compounds.Type: GrantFiled: May 7, 2004Date of Patent: May 23, 2006Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Guoqiang Wang, Deqiang Niu, Ly Tam Phan
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Patent number: 6998390Abstract: Antibacterial compounds having formula (I) and formula (II) and salts, prodrugs, and salts of prodrugs thereof, processes for making the compounds and intermediates employed in the processes, compositions containing the compounds, and methods for prophylaxis or treatment of bacterial infections in a fish or a mammal using the compounds are disclosed.Type: GrantFiled: April 22, 2003Date of Patent: February 14, 2006Inventors: Zhenkun Ma, Stevan Djuric, Alan S. Florjancic, Hong Yong
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Patent number: 6995143Abstract: The invention provides new macrolides antibiotics of formula I with improved biological properties and having the formula wherein R1, R2 and R3 are as herein described.Type: GrantFiled: February 20, 2003Date of Patent: February 7, 2006Assignee: Basilea Pharmaceutica AGInventors: Philippe Guerry, Johannes Laurenz Kellenberger, Stéphanie Blanchard
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Patent number: 6953782Abstract: The present invention discloses compounds of formulae I, II, III or IV 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: December 24, 2003Date of Patent: October 11, 2005Assignee: Enanta Pharmaceuticals, Inc.Inventors: Ly Tam Phan, Yat Sun Or, Jay Judson Farmer
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Patent number: 6946446Abstract: The invention relates to novel methods for using macrolide anti-infective agents. The macrolide anti-infective agents demonstrate antibacterial activity against multi-drug resistant strains of bacteria and, in particular, methicillin-resistant Staphylococcus aureus (MRSA). Methods for inhibiting the activity of multi-drug resistant bacterial organisms and methods for treating a bacterial infection caused by such organisms are described herein.Type: GrantFiled: February 23, 2001Date of Patent: September 20, 2005Assignee: Abbott LaboratoriesInventors: Zhenkun Ma, Peter Nemoto, Suoming Zhang, Hong Yong, Yat Sun Or
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Patent number: 6933283Abstract: Antibacterial compounds having formula (I) and formula (II) and salts, prodrugs, and salts of prodrugs thereof, processes for making the compounds and intermediates used in the processes, compositions containing the compounds, and methods for prophylaxis or treatment of bacterial infections using the compounds are disclosed.Type: GrantFiled: April 23, 2003Date of Patent: August 23, 2005Assignee: Abbott LaboratoriesInventors: Richard Clark, Stevan Djuric, Zhenkun Ma
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Patent number: 6900183Abstract: 11,12 ? lactone ketolides of the following formula: and pharmaceutically acceptable salts and solvates thereof, wherein R, R1, R2, and R3 are as described herein. The disclosure also relates to processes for the preparation of such compounds, to compositions containing them, and to their use in the therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.Type: GrantFiled: December 20, 2001Date of Patent: May 31, 2005Assignee: Glaxo Group LimitedInventors: Daniele Andreotti, Stefano Biondi, Sergio Lociuro
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Patent number: 6872707Abstract: The invention relates to halo derivatives of 9a-N-(N?-arylcarbamoyl)- and 9a-N-(N?-arylthiocarbamoyl)-9-deoxo-9a-aza-9a-homoerythromycin A of the general formula (I) wherein R has the meaning of a substituted aryl group of the formula (II) wherein substituents a, b, c, d and e are the same or different and at least one of them has the meaning of halo, a (C1-C6)haloalkyl or a (C1-C6)haloalkoxy group, whereas the remaining ones have the meaning of hydrogen, halo, a (C1-C6)alkyl or a (C1-C6)alkoxy group, and X has the meaning of oxygen or sulfur, and pharmaceutically acceptable addition salts thereof with inorganic or organic acids, to a process for their preparation, to a process for the preparation of pharmaceutical compositions comprising them and to the use of these pharmaceutical compositions for the treatment or prevention of bacterial infections.Type: GrantFiled: May 2, 2000Date of Patent: March 29, 2005Assignee: PLIVA farmaceutska industrija dionicko drustvoInventors: Zorica Maru{hacek over (s)}ic-I{hacek over (s)}tuk, Nedjelko Kujund{hacek over (z)}ić , Gabrijela Kobrehel, Stjepan Mutak, Nata{hacek over (s)}a Mar{hacek over (s)}ić
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Patent number: 6852702Abstract: 9a-N-[N?-(phenylsulfonyl)carbamoyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin A and of 5-O-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerythronolide A and their pharmaceutically acceptable addition salts with inorganic or organic acids are provided, along with a process for their preparation, pharmaceutical compositons, and use in treating bacterial infections.Type: GrantFiled: February 27, 2002Date of Patent: February 8, 2005Assignee: Pliva D.D.Inventors: Nedjeljko Kujundzic, Mirjana Bukvic Krajacic, Miljenko Dumic, Andrea Hasenohrl
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Patent number: 6849608Abstract: A macrolide antibiotic of the formula wherein the variables are defined as described herein.Type: GrantFiled: June 3, 2003Date of Patent: February 1, 2005Assignee: Pfizer, Inc.Inventors: Wei-Guo Su, Yan Chen
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Patent number: 6841664Abstract: Novel 6,11-4-carbon bridged ketolides, pharmaceutically-acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically-acceptable carrier are described. Also described are a method for treating bacterial infections by administering to an animal a pharmaceutical composition containing a therapeutically effective amount of a compound of the invention and processes for the preparation of such compounds.Type: GrantFiled: July 25, 2002Date of Patent: January 11, 2005Assignee: Enanra Pharmaceuticals, Inc.Inventors: Yat Sun Or, Guoqiang Wang, Deqiang Niu, Ly Tam Phan
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Patent number: 6825171Abstract: The invention relates to novel erythromycin derivatives, particularly ones with novel C-13 R13 substitutents, and to pharmaceutically acceptable salts thereof. The compounds of this invention are useful as antibacterial agents and antiprotozoa agents and for other applications (e.g., anticancer, atherosclerosis, gastric motility reduction, etc.) in mammals, including man, as well as in fish and. The invention also relates to pharmaceutical compositions containing such compounds and to methods of treating bacterial protozoa infections by administering such compounds. The invention also relates to methods of preparing such compounds and to intermediates useful in such preparation.Type: GrantFiled: April 8, 2003Date of Patent: November 30, 2004Assignee: Pfizer, Inc.Inventor: Yong-Jin Wu
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Patent number: 6825172Abstract: 3-Descladinosyl-6-O-carbamoyl and 6-O-carbonoyl macrolide antibacterial agents of the formula: wherein R1, W, R3, R4, R5, R6, X, X′, and Z are as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.Type: GrantFiled: May 28, 2003Date of Patent: November 30, 2004Assignee: Janssen Pharmaceutica, NVInventors: Todd C. Henninger, Mark J. Macielag, Brett A. Marinelli, Bin Zhu
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Patent number: 6812216Abstract: There are described 11-C-substituted derivatives of clarithromycin and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier. Also described is a method for treating bacterial infections by administering to an animal a pharmaceutical composition containing a therapeutically-effective amount of a compound of the invention, and processes for the preparation of such compounds.Type: GrantFiled: June 25, 2002Date of Patent: November 2, 2004Assignee: Enanta Pharmaceuticals, Inc.Inventors: Ly Tam Phan, Jay Judson Farmer, Yat Sun Or
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Patent number: 6809188Abstract: Clarithromycin can be easily prepared by reacting erythromycin A N-oxide with a methylating agent to obtain 6-O-methylerythromycin A N-oxide; and treating 6-O-methylerythromycin A N-oxide obtained above with a reducing agent in a high yield.Type: GrantFiled: May 1, 2002Date of Patent: October 26, 2004Assignee: Hanmi Pahrm. Co., Ltd.Inventors: Kwee-Hyun Suh, Mi-Ra Seong, Nam-Du Kim, Gwan-Sun Lee
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Patent number: 6790835Abstract: 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: June 5, 2003Date of Patent: September 14, 2004Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ly Tam Phan, Tongzhu Liu, Zhigang Chen, Yat Sun Or
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Patent number: 6777543Abstract: The invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3, R4, R5, R17, Rf, A, X, and Y are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formulas 1, methods of using the compounds of formula 1 in the treatment of infections and methods of preparing the compounds of formula 1.Type: GrantFiled: May 19, 2003Date of Patent: August 17, 2004Assignee: Pfizer, Inc.Inventors: Yong-Jin Wu, Wei-Guo Su, Takushi Kaneko, Hamish McArthur
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Patent number: 6774115Abstract: 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: June 5, 2003Date of Patent: August 10, 2004Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ly Tam Phan, Yat Sun Or
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Patent number: 6767998Abstract: The object of the present invention is to prepare purified erythromycin by removing erythromycin F from erythromycin. The present invention provides a method for preparing purified erythromycin from which erythromycin F is removed, which comprises the step of extracting erythromycin F from erythromycin using (i) an organic solvent and (ii) water or an aqueous solution of an inorganic and/or organic material.Type: GrantFiled: September 23, 2002Date of Patent: July 27, 2004Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Kaname Tsuzaki, Megumi Ishii
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Patent number: 6764998Abstract: 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: June 18, 2003Date of Patent: July 20, 2004Assignee: Enanta Pharmaceuticals, Inc.Inventors: Guoqiang Wang, Yat Sun Or, Ly Tam Phan
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Patent number: 6756359Abstract: Antimicrobial macrolide compounds are provided having formulas II: as well as pharmaceutically acceptable salts, esters or prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: GrantFiled: July 3, 2002Date of Patent: June 29, 2004Assignee: Chiron CorporationInventors: Daniel Chu, Matthew Burger, Xiaodong Lin, Georgia Law Carroll, Jacob Plattner, Alice Rico
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Patent number: 6753318Abstract: Novel 6,11-4-carbon bridged erythromycin derivatives and pharmaceutically-acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically-acceptable carrier are described. Also described are methods for treating bacterial infections by administering to an animal a pharmaceutical composition containing a therapeutically effective amount of a compound of the invention and processes for the preparation of such compounds.Type: GrantFiled: July 25, 2002Date of Patent: June 22, 2004Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Guoqiang Wang, Deqiang Niu, Ly Tam Phan
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Patent number: 6740642Abstract: The invention provides new macrolides antibiotics of formula I with improved biological properties and improved stability of the formula wherein R1 is hydrogen, cyano, —S(L)mR2, —S(O)(L)mR2, or —S(O)2(L)mR2; L represents —(CH2)n— or —(CH2)nZ(CH2)n′—; m is 0 or 1; n is 1, 2, 3, or 4; n′ is 0, 1, 2, 3, or 4; Z is O, S or NH; R2 is hydrogen, alkyl, heterocyclyl or aryl; which heterocyclyl and the aryl groups may be further substituted; * indicates a chiral center which is in the (R) or (S) form, as well as a pharmaceutically acceptable acid addition salts or in vivo cleavable esters thereof.Type: GrantFiled: February 21, 2003Date of Patent: May 25, 2004Assignee: BAsilea Parmaceutica AGInventors: Peter Angehrn, Daniel Hunziker, Pierre-Charles Wyss
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Patent number: 6734292Abstract: The present invention is to obtain novel anti-inflammatory agents having decreased antibacterial activity and increased anti-inflammatory action, and is psedoerythromycin derivatives represented by the following general formula [I], wherein R1 and R2 are same or different and each represents H, alkyl, alkynyl, acyl or sulfonyl, in which these groups may optionally have substituents, and Me indicates methyl.Type: GrantFiled: July 25, 2002Date of Patent: May 11, 2004Assignee: The Kitasato InstituteInventors: Satoshi Omura, Yuzuru Iwai, Toshiaki Sunazuka, Tohru Nagamitsu
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Patent number: 6727229Abstract: Novel 11-12 substituted lactone ketolide derivatives and pharmaceutically-acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically-acceptable carrier are described. Also described are a method for treating bacterial infections by administering to an animal a pharmaceutical composition containing a therapeutically effective amount of a compound of the invention and processes for the preparation of such compounds.Type: GrantFiled: August 19, 2002Date of Patent: April 27, 2004Assignee: Enanta Pharmaceuticals, Inc.Inventors: Nha Huu Vo, Ly Tam Phan, Ying Hou, Tongzhu Liu, Yat Sun Or
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Patent number: 6720308Abstract: Novel 11-12 substituted lactone anhydrolide derivatives and pharmaceutically-acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically-acceptable carrier are described. Also described are a method for treating bacterial infections by administering to an animal a pharmaceutical composition containing a therapeutically effective amount of a compound of the invention and processes for the preparation of such compounds.Type: GrantFiled: November 7, 2002Date of Patent: April 13, 2004Assignee: Enanta Pharmaceuticals, Inc.Inventors: Nha Huu Vo, Ying Hou, Ly Tam Phan, Yat Sun Or
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Patent number: 6713615Abstract: There is provided a preparation process useful for an efficient synthesis of 6-O-substituted ketolide derivatives by combining a characterized step of introduction of a substituent at the 6-position by selective cleavage of a C—O bond of the cyclic acetal at the 9-position side via 6,9-cyclic acetal 5-O-desosaminyl erythronolide derivative, a step of conversion into carbonyl groups at the 9- and 3-positions, and a step of 11,12-cyclic carbamation to lead to 6-O-substituted ketolide derivatives.Type: GrantFiled: February 12, 2003Date of Patent: March 30, 2004Assignee: Taisho Pharmaceutical Co., Ltd.Inventors: Masato Kashimura, Hiroaki Kamiyama, Takeshi Kuwada, Nobuyuki Suzuki, Takashi Adachi
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Patent number: 6642364Abstract: This process is intended to obtain clarithromycin. According to the process, it starts from the erythromycin A 9-oxime hydrochloride, which is transformed into clarithromycin by means of a synthetic sequence in which an acetal of the 9-oxime is initially formed. The use of the oxime hydrochloride permits that only the use of catalytic amounts of pyridine salts are necessary to favor the reaction. Next, the hydroxyls in positions 2′ and 4″ are protected with a silylating agent and the hydroxyl in position 6 is methylated; all this without the isolation of any reaction intermediate being necessary. Finally, the acetal and 2′ and 4″ silanes unprotection, followed by the deoximation yields clarithromycin with a high yield and a form which is easily applicable industrially.Type: GrantFiled: June 27, 2002Date of Patent: November 4, 2003Assignee: Ercros Industrial, S.A.Inventors: Ramón Asensio Dominguez, Maria del Carmen Cruzado Rodriguez, Luis Ángel Diaz Tejo, Rosa Nomen Ribé, Julià Sempere Cebrián, José Ignacio Borrell Bilbao
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Patent number: 6600025Abstract: An erythromycin A 9-O-benzodithiol oxime intermediate represented by the following formula (III) useful for synthesis of clarthromycin and crystalline solvate thereof: Wherein, Y1 and Y2 are independently a hydrogen atoms or trimethylsilyl groups. And, a process for the preparation of clarithromycin using the erythromycin A 9-O-benzodithiol oxime intermediate as described in the specification.Type: GrantFiled: September 6, 2001Date of Patent: July 29, 2003Assignees: Chemtech Research Incorporation, Hansol Chemience Co., Ltd.Inventors: Tae Suk Lee, Chang Hyun Yoo, Kyoung Soo Kim, Hyun Suk An, Jung Young Kim, Wan Joo Kim
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Patent number: RE39383Abstract: A procedure for preparing 6-O-alkyl erythromycin compounds having the formula: wherein R1 is a loweralkyl group, R2 and R3 an independently hydrogen or a hydroxy-protecting group, except that R2 and R3 may not both be hydrogen simultaneously; Y is oxygen or a specifically substituted oxime; and Z is hydrogen, hydroxy or protected-hydroxy; by reaction of the compound wherein R1 is hydrogen with an alkylating reagent, is the presence of a strong alkali metal base and also in the presence of a weak organic amino base, in a suitable stirred or agitated polar aprotic solvent, or a mixture of such polar aprotic solvents maintained at a reaction temperature and for a period of time sufficient to effect alkyation.Type: GrantFiled: March 22, 2004Date of Patent: November 7, 2006Assignee: Abbott LaboratoriesInventors: Jih-Hua Liu, George A. Foster, Jr., Stephen H. Montgomery