Additional Nitrogen Containing Patents (Class 536/7.4)
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Publication number: 20040266998Abstract: 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: ApplicationFiled: May 7, 2004Publication date: December 30, 2004Inventors: Yat Sun Or, Guoqiang Wang, Deqiang Niu, Ly Tam Phan
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Publication number: 20040266997Abstract: The invention is directed to degradation products of azithromycin, methods for the preparation and identification of the degradation products which may be produced during storage and/or synthesis of azithromycin.Type: ApplicationFiled: March 25, 2004Publication date: December 30, 2004Inventors: Michael Pesachovich, Sarah Isaacs, Claude Singer, Eduard Schwartz, Edit Berger
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Publication number: 20040266703Abstract: Provided is a method for obtaining a macrolide, especially tacrolimus, ascomycin, pimecrolimus, sirolimus, or everolimus, from biomatter.Type: ApplicationFiled: May 12, 2004Publication date: December 30, 2004Inventors: Vilmos Keri, Janos Rako, Ferenc Rantal, Andrea Csorvasi
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Patent number: 6835716Abstract: 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 24, 2002Date of Patent: December 28, 2004Assignee: Pfizer, Inc.Inventor: Takushi Kaneko
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Patent number: 6833444Abstract: This invention relates to compounds of the formula 1: and to pharmaceutically acceptable salts and solvates thereof wherein X1, X2, R2, R8, R9, R10 and R11 are as defined herein. The compounds of formula 1 are 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 1 and to methods of treating bacterial and protozoal infections by administering the compounds of formula 1.Type: GrantFiled: April 5, 2002Date of Patent: December 21, 2004Assignee: Pfizer, Inc.Inventors: William T. McMillen, Takushi Kaneko
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Publication number: 20040254126Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: 1Type: ApplicationFiled: March 23, 2004Publication date: December 16, 2004Inventors: Yao-Ling Qiu, Ly Tam Phan, Zhigang Chen, Tongzhu Liu, Yat Sun Or
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Publication number: 20040254124Abstract: The present invention relates to a compound of formula (I) wherein R1 is hydrogen or together with R2 is oxo; R2 represents hydroxy, OC(O)XR7, OC(O)NHXR7 or R2 together with R1 is an oxo group; R3 is hydrogen or a hydroxyl protecting group; R4 is hydrogen or XR7; R5 is hydrogen, XR7,, C(O)XR7 or C(O)NHXR7; R6 is hydrogen or R5 and R6 taken together with the intervening atoms form a cyclic carbonate having the following structure and pharmaceutically acceptable salts and solvates thereof and solvates thereof; to processes for their preparation and their use in the therapy or prophylaxis of systemic or topical bacterial infections in a human or animal body.Type: ApplicationFiled: February 25, 2004Publication date: December 16, 2004Inventors: Suleman Alihodzic, Andrea Berdik, Francesca Cardullo, Antun Hutinec, Gorjana Lazarevski, Sergio Lociuro, Zprica Marusic-Istuk, Stjepan Mutak, Alfonso Pozzan, Marko Derek
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Patent number: 6831068Abstract: Antibacterial compounds having formula (I) 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: February 10, 2003Date of Patent: December 14, 2004Assignee: Abbott LaboratoriesInventors: Richard Clark, Stevan Djuric, Zhenkun Ma, Sanyi Wang
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Patent number: 6825170Abstract: 6-O-Acyl ketolide antibacterials of the formula: wherein R1, R2, R3, R4, W, X, X′, Y, and Y′ 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: November 21, 2002Date of Patent: November 30, 2004Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Todd C. Henninger, Mark J. Macielag, Manomi A. Tennakoon, Xiaodong Xu
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Patent number: 6825327Abstract: The invention relates to processes for preparing compounds of formula 1 wherein R3 is as defined herein, and to pharmaceutically acceptable salts thereof, as well as intermediates useful in such processes. The compounds of formula 1 are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing compounds prepared by the processes of the invention and to methods of treating bacterial protozoa infections by administering such compounds.Type: GrantFiled: April 25, 2002Date of Patent: November 30, 2004Assignee: Pfizer Inc.Inventors: Constantine Sklavounos, John L. Tucker, Lulin Wei, Kerry P. Mahon, Philip Hammen, Joanna T. Negri, Richard S. Lehner
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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: 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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Publication number: 20040220120Abstract: 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: ApplicationFiled: March 30, 2004Publication date: November 4, 2004Inventors: Nha Huu Vo, Ying Hou, Ly Tam Phan, Yat Sun Or
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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: 6809080Abstract: This invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs, and solvates thereof wherein X, Y, R1, R2, R3, R4, and R6 are as defined herein. The compounds of formula I are 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, methods of making the compounds, and to methods of treating bacterial and protozoal infections by administering the compounds.Type: GrantFiled: June 26, 2001Date of Patent: October 26, 2004Assignee: Pfizer, Inc.Inventors: Takushi Kaneko, William Thomas McMillen
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Publication number: 20040209827Abstract: 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: ApplicationFiled: May 7, 2004Publication date: October 21, 2004Inventors: Ly Tam Phan, Jay Judson Farmer, Yat Sun Or
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Publication number: 20040209826Abstract: This invention relates to a novel crystalline diphosphate salt of (2R,3S,4R,5R,8R,10R,11R,12S,13S,14R)-13-[[2,6-dideoxy-3-C-methyl-3-O-methyl-4-C-[(propylamino)methyl]-&agr;-L-ribo-hexopryanosyl]oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-&bgr;-D-xylo-hexopyranosyl]oxy]-1-oxa-6-azacyclopentadecan-15-one that is useful as an antibacterial and antiprotozoal agent in mammals. This invention also relates to pharmaceutical compositions containing the free base of the diphosphate salt and the methods of treating bacterial and protozoal infections in mammals by administering the free base of the diphosphate to mammals requiring such treatment. The free base of the diphosphate salt of the present invention possesses potent activity against various bacterial and protozoal infections when given by parenteral application to mammals.Type: ApplicationFiled: May 6, 2004Publication date: October 21, 2004Inventors: Robert J. Rafka, Colman B. Ragan, Douglas J.M. Allen
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Publication number: 20040198677Abstract: 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: ApplicationFiled: December 29, 2003Publication date: October 7, 2004Inventors: Mlanden Mercep, Milan Mesic, Linda Tomaskovic, Marijana Komac, Boska Hrvacic, Stribor Markovic
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Publication number: 20040186063Abstract: This invention features a compound of the following formula:Type: ApplicationFiled: August 20, 2003Publication date: September 23, 2004Inventors: Hans-Jurgen Gutke, Christian Flohr, Albert Beck, Simona Margutti, Mary Eggers, Jan-Hinrich Guse, Moussa Khobzaoui, Michael Burnet
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Patent number: 6794366Abstract: Compounds of the formula or the 10,11-anhydro forms therefor, wherein Ra is H or OH; Rb is H or halogen; Rc is H or a protecting group; Rd is methyl; unsubstituted alkyl (3-10C); substituted alkyl (1-10C); substituted or unsubstituted alkenyl (2-10C) or substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); substituted or unsubstituted arylalkenyl (5-20C); substituted or unsubstituted arylalkynyl (5-20C); substituted or unsubstituted amidoarylalkyl (5-20C); substituted or unsubstituted amidoarylalkenyl (5-20C); or substituted or unsubstituted amidoarylalkynyl (5-20C); Re is H or a protecting group or is mono- or disubstituted amino carbonyl; Rf is H; substituted or unsubstituted alkyl (1-10C); substituted or unsubstituted alkenyl (1-10C); substituted or unsubstituted alkynyl (1-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); or —ORf may be replaced bType: GrantFiled: April 17, 2002Date of Patent: September 21, 2004Assignee: Kosan Biosciences, Inc.Inventors: Daniel Chu, Gary Ashley
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Publication number: 20040180841Abstract: The invention provides novel apoptosis-inducing compounds that include isolated, purified isoapoptolidin, and selectively functionalized isoapoptolidin derivatives and stereoisomers thereof; selectively functionalized apoptolidin derivatives and stereoisomers thereof; and deglycosylated isoapoptolidin and selectively functionalized derivatives and stereoisomers thereof. The isoapoptolidin, apoptolidin, and deglycosylated isoapoptolidin derivatives may be functionalized by substituting any or all of the methoxyl or hydroxyl groups of the parent molecule. Pharmaceutical compositions and methods for using the compounds are also provided.Type: ApplicationFiled: January 13, 2004Publication date: September 16, 2004Inventors: Paul A. Wender, Orion D. Jankowski, Elie A. Tabet
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Publication number: 20040180842Abstract: The invention relates to a method of preparing compounds of the formula 1Type: ApplicationFiled: March 26, 2004Publication date: September 16, 2004Applicant: Pfizer IncInventors: Brian Scott Bronk, Michael Anthony Letavic, Takushi Kaneko, Bingwei Vera Yang, Edward Alan Glazer, Hengmiao Cheng
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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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Publication number: 20040171818Abstract: The present invention relates to processes and intermediates for the preparation of 6-11 bicyclic erythromycin derivatives.Type: ApplicationFiled: January 14, 2004Publication date: September 2, 2004Inventors: Guoyou Xu, Datong Tang, Yonghua Gai, Heejin Kim, Guoqiang Wang, Ly Tam Phan, Yat Sun Or, Zhe Wang
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Publication number: 20040167083Abstract: Conjugates of epothilones and epothilone derivatives (as effectors) with suitable saccharides or saccharide derivatives (as recognition units) are described. Their production is carried out by the recognition units being reacted with suitable linkers, and the compounds that are produced are conjugated to the effectors. The pharmaceutical use of the conjugates for treating proliferative or angiogenesis-associated processes is described.Type: ApplicationFiled: December 5, 2003Publication date: August 26, 2004Inventors: Klaus Bosslet, Holger Hess-Stumpp, Jens Hoffmann, Ulrich Klar, Andrea Rotgeri
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Patent number: 6777393Abstract: The invention relates to a method of preparing compounds of the formula and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial protozoa infections by administering the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1 and to intermediates useful in such preparation.Type: GrantFiled: October 18, 2002Date of Patent: August 17, 2004Assignee: Pfizer Inc.Inventors: Brian Scott Bronk, Michael Anthony Letavic, Takushi Kaneko, Bingwei Vera Yang, Edward Alan Glazer, Hengmiao Cheng
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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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Publication number: 20040157787Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: 1Type: ApplicationFiled: November 19, 2003Publication date: August 12, 2004Inventors: Yat Sun Or, Wang Guoqiang, Ly Tam Phan, Deqiang Niu, Nha Huu Vo, Yao-Ling Qiu, Yanchun Wang, Marina Busuyek, Ying Hou, Yulin Peng, Heejin Kim, Tongzhu Liu, Jay Judson Farmer, Guoyav Xu
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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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Publication number: 20040147461Abstract: The present invention provides novel macrolide compounds of the formulas 1Type: ApplicationFiled: November 12, 2003Publication date: July 29, 2004Inventors: Gary Ashley, Brian Metcalf, Zong-Qiang Tian, Daniel Santi
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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: 6764997Abstract: Compositions and methods of stabilizing azithromycin compositions are described. Stabilized azithromycin compositions comprise an intimate admixture of azithromycin and a stabilizing-effective amount of an antioxidant to improve the resistance of the azithromycin to degradation. Coprecipitation or co-milling of azithromycin and an antioxidant are particularly preferred means of achieving an intimate admixture. Pharmaceutical formulations comprising a stabilized azithromycin composition and methods of making such formulations are also described.Type: GrantFiled: October 18, 2002Date of Patent: July 20, 2004Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Ruth Tenengauzer, Joseph Schwarz, Julia Hrakovsky, Tania Lessen, Lev Khondo, Mathi Mathivanan, Claude Singer, Michael Pesachovich
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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: 6764996Abstract: Compounds of formula (I) formula (II) formula (III) and formula (IV) or pharmaceutically acceptable salts or prodrugs thereof, are antibacterial agents. Compositions containing the compounds, processes for making the compounds, synthetic intermediates employed in the processes, and methods for treatment and prevention of bacterial infections are disclosed.Type: GrantFiled: July 25, 2000Date of Patent: July 20, 2004Assignee: Abbott LaboratoriesInventors: Yat Sun Or, Robert F. Keyes, Zhenkun Ma
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Publication number: 20040138150Abstract: Motilide compounds having the formula (I), 1Type: ApplicationFiled: August 26, 2003Publication date: July 15, 2004Inventors: Daniel V. Santi, Brian Metcalf, Christopher Carreras, Yaoquan Liu, Robert McDaniel, Eduardo J. Rodriguez
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Patent number: 6762168Abstract: The invention is directed towards antibacterial compounds. The invention concerns macrolide antibiotics useful as antiinfective agents.Type: GrantFiled: February 3, 2003Date of Patent: July 13, 2004Assignee: Kosan Biosciences, Inc.Inventor: Daniel T. W. Chu
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Publication number: 20040127433Abstract: Erythromycin derivatives or salt thereof having excellent antibacterial activity against a typical acid-fast mycobacteria and useful as antibacterial agent, which is represented by the following general formula: 1Type: ApplicationFiled: March 24, 2003Publication date: July 1, 2004Inventors: Hideo Kato, Toshihiko Yoshida, Akemi Nishimoto, Shinobu Ohmoto
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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: 6753415Abstract: There are described novel 5-O-mycaminosyltylonide (OMT) analogs possessing increased antibacterial activity toward Gram positive and Gram negative bacteria as well as macrolide resistant Gram positives and pharmaceutically acceptable compositions comprising a therapeutically effective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier.Type: GrantFiled: April 19, 2002Date of Patent: June 22, 2004Assignee: Enanta Pharmaceuticals, Inc.Inventors: Ly Tam Phan, Yao-Ling Qiu, Yat Sun Or, Nha Vo, Tianying Jian, Ying Hou, Marina Busuyek
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Patent number: 6750205Abstract: The present invention provides novel macrolide compounds of the formulas wherein: R is hydroxyl or methoxy; R1 is selected from the group consisting of hydrogen, hydroxyl, halide, NH2, OR9, where R9 is C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl or heteroaryl and R10 and R11 are each independently hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, or aryl; R2 and R3 are each independently selected from the group consisting of hydrogen, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, alkylaryl, alkenylaryl alkynylaryl or R2 and R3 together form a cycloalkyl or a cycloaryl moiety; R4 is hydrogen or methyl; R5 is hydrogen, hydroxyl, oxo, or together with R6 and the carbons to which they are attached form a cyclic carbonate; R6 is hydrogen, hydroxyl, OR12 where R12 is C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, or together with R5 and the carbons to which they are attached form a cyclic carbonate; R7 is methyl, C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynType: GrantFiled: April 7, 2003Date of Patent: June 15, 2004Assignee: Kosan Biosciences, Inc.Inventors: Gary Ashley, Mark Burlingame, Christopher Carreras, Daniel Santi
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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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Publication number: 20040097434Abstract: The present invention relates (a) to new compounds represented by Formula I: 1Type: ApplicationFiled: July 7, 2003Publication date: May 20, 2004Applicant: PLIVA Pharmaceutical Industry, IncorporatedInventors: Mladen Mercep, Milan Mesic, Linda Tomaskovic, Stribor Markovic
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Publication number: 20040092459Abstract: The invention relates to novel erythromycin analogs and azalides, particularly ones with novel C-13 substituents, and to pharmaceutically acceptable salts thereof. The compounds of this invention are antibacterial agents that may be used to treat various bacterial and protozoa infections. 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: ApplicationFiled: July 30, 2002Publication date: May 13, 2004Applicant: Pfizer Inc.Inventors: John Philip Dirlam, Hamish Alastair Irvine McArthur, Alan Elwood Blize
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Publication number: 20040092460Abstract: Substantially pure amorphous 9-deoxo-9a-aza-9a-methyl-9a-homoerythromycin A.Type: ApplicationFiled: July 21, 2003Publication date: May 13, 2004Applicant: Pliva Pharmaceutical Industry, IncorporatedInventors: Miljenko Dumic, Mladen Vinkovic, Marina Oresic, Ernest Mestrovic, Aleksandar Danilovski, Alojz Dumbovic, Knezevic Zdravka, Gorjana Lazarevski, Darko Filic, Dominik Cincic, Katica Lazaric, Dejan-Kresimir Bucar
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Publication number: 20040082526Abstract: 1Type: ApplicationFiled: December 3, 2003Publication date: April 29, 2004Inventors: Daniele Andreotti, Stefano Biondi, Sergio Lociuro
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Publication number: 20040082527Abstract: The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections.Type: ApplicationFiled: August 28, 2003Publication date: April 29, 2004Applicant: Pfizer IncInventors: Zheng J. Li, Andrew V. Trask
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Patent number: 6727352Abstract: This invention relates to methods of preparing a compound of Formulae 2, 5 and 7, wherein R2-R5, R7, R9, R10 and R15 are defined herein.Type: GrantFiled: August 23, 2002Date of Patent: April 27, 2004Assignee: Pfizer, Inc.Inventors: Hengmiao Cheng, Chao Li
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Patent number: RE38520Abstract: A subject of the invention is the compounds of formula (I): in which: X represents a CH2 or SO2 radical or an oxygen atom, Y represents a (CH2)m—(CH═CH)n(CH2)o radical, with m+n+o≦8, n=0 or 1, Ar represents an aryl radical, W represents a hydrogen atom, or the remainder of a carbamate function. The compounds of formula (I) have useful antibiotic properties.Type: GrantFiled: April 19, 2001Date of Patent: May 18, 2004Assignee: Aventis Pharma S.A.Inventors: Constantin Agouridas, Jean-Francois Chantot