Additional Nitrogen Containing Patents (Class 536/7.4)
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Patent number: 7488811Abstract: Macrolide compounds lacking cladinose in position 3 having antiinflammatory activity and substantially free of antibiotic properties, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them as active ingredient.Type: GrantFiled: July 29, 2003Date of Patent: February 10, 2009Assignee: 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: 20090036388Abstract: The present invention relates to novel 2?-O-substituted 9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A derivatives having antimalarial activity. More particularly, the invention relates to 2?-O-substituted-9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A and 2?-O-substituted-3-O-decladinosyl-9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A derivatives having antimalarial activity, to the intermediates for their preparation, to the methods for their preparation, to their use as therapeutic agents, and to salts thereof having antimalarial activity.Type: ApplicationFiled: July 28, 2008Publication date: February 5, 2009Inventors: Sulejman Alihodzic, Mihaela Peric, Dijana Pesic
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Publication number: 20090005325Abstract: Provided herein are ketolide 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, Bacillus, Enterobactericeae, Propionibacterium acnes or any combination thereof. Also provided are processes for preparation of compounds described herein, pharmaceutical compositions thereof, and methods of treating bacterial infections.Type: ApplicationFiled: November 21, 2006Publication date: January 1, 2009Inventors: Biswajit Bas, Anjan Chakrabarti, Ramadass Venkataramanan, Atul Kashinath Hajare, Anish Bandyopadhyay, Rita Katoch, Gobind Singh Kapkoti, Yogash Baban Surase, Mohammad Salman, Dilip J. Upadhyay
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Publication number: 20080318878Abstract: The present invention provides acylide derivatives, which can be used as antibacterial agents. Compounds disclosed 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, Bacillus, Enterobactericeae or any combination thereof. Also provided are processes for preparing compounds disclosed herein, pharmaceutical compositions thereof, and method of treating bacterial infections.Type: ApplicationFiled: September 27, 2005Publication date: December 25, 2008Inventors: Biswajit Das, Rita Katoch, Atul Kashinath Hajare, Anish Bandyopadhyay, Santosh Haribhau Kurhade, Sujata Rathy, Ashok Rattan
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Patent number: 7468428Abstract: The invention provides among other things a stable, sterile pharmaceutical formulation comprising lyophilized azithromycin and ethanol. The invention also provides a method of producing a stable, sterile pharmaceutical product comprising lyophilized azithromycin. The invention also provides a pharmaceutical dosage form comprising the pharmaceutical formulation, as well as a method of treating a disease in a patient comprising administering a solution of the pharmaceutical formulation to a patient.Type: GrantFiled: March 17, 2004Date of Patent: December 23, 2008Assignee: APP Pharmaceuticals, LLCInventors: Byung Ho Woo, K. Keith Kwok, Kang Yong Yang
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Publication number: 20080312167Abstract: The present invention relates to 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: ApplicationFiled: May 9, 2006Publication date: December 18, 2008Inventors: Sulejman Alihodzic, Gorjana Lazarevski
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Patent number: 7462600Abstract: Macrolide compounds per se, as shown below and defined herein, and their use, e.g., as antibacterial and antiprotozoal agents in animals, including humans: Also disclosed are methods of preparing the compounds, intermediates, and pharmaceutical compositions thereof, and methods of treating or preventing disease by administering the compounds to subjects in need. This abstract is only an excerpt and is not limiting of the invention.Type: GrantFiled: December 21, 2005Date of Patent: December 9, 2008Assignee: Pfizer IncInventors: Louis S. Chupak, Mark E. Flanagan, Takushi Kaneko, Thomas V. Magee, Mark C. Noe, Usa Reilly
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Publication number: 20080293646Abstract: The invention relates to compounds of Formula (I): wherein R1, R2 and X are as defined herein. The invention also relates to pharmaceutical compositions and methods of treating bacterial infections using compounds of Formula (I).Type: ApplicationFiled: March 12, 2008Publication date: November 27, 2008Inventors: Thomas V. Magee, Usa Reilly, Mark Carl Noe, Mark E. Flanagan, Zhengong Bryan Li, Richard Allen Buzon, Daniel William Widlicka
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Publication number: 20080280841Abstract: The present invention relates to stable amorphous 3-De[(2,6-dideoxy-3-C-methyl-3-O-methyl-?-L-ribohexopyranosyl)oxy]-11,12-dideoxy-6-O-methyl-3-oxo-12,11-[oxycarbonyl[[4-[4-(3-pyridinyl)-1H-imidazol-1-yl]butyl]imino]]erythromycin (telithromycin), methods for the preparation thereof, the use of stable amorphous telithromycin in the treatment of bacterial infections and to pharmaceutical compositions comprising stable amorphous telithromycin.Type: ApplicationFiled: January 4, 2007Publication date: November 13, 2008Applicant: SANDOZ AGInventors: Johannes Ludescher, Ulrich Griesser, Christoph Langes
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Patent number: 7446097Abstract: 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: January 3, 2002Date of Patent: November 4, 2008Assignee: Glaxosmithkline Istrazivacki Centar Zagreb D.O.OInventors: Mladen Mercep, Milan Mesic, Linda Tomaskovic, Marijana Komac, Boska Hrvacic, Stribor Markovic
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Publication number: 20080262208Abstract: 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: May 20, 2008Publication date: October 23, 2008Inventors: 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: 7438924Abstract: This invention relates to a pharmaceutical formulation, in the form of a tablet, sachet or powder for suspension dosage form, which comprises dry granulated particles of a non-dihydrate form of azithromycin and, optionally, one or more pharmaceutically acceptable excipients. Preferably, the pharmaceutical formulation is a tablet containing between about 40%, by weight, to about 90%, by weight, non-dihydrate azithromycin. More preferably, the pharmaceutical formulation contains non-dihydrate azithromycin selected from the forms B, D, E, F, G, H, J, M, N, O, P, Q, R, or mixtures thereof. Even more preferably, the invention relates to a pharmaceutical formulation wherein the dosage of azithromycin is 250 mgA, 500 mgA, 600 mgA or 1000 mgA. The present invention further relates to a dry granulated azithromycin particle, comprising a form of azithromycin, selected from forms D, E, F, G, H, J, M, N, O, P, Q, R and mixtures of non-dihydrate forms, and at least one pharmaceutically acceptable excipient.Type: GrantFiled: January 31, 2003Date of Patent: October 21, 2008Assignee: Pfizer IncInventors: Barbara A. Johnson, Ernest S. Quan
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Publication number: 20080255060Abstract: 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: ApplicationFiled: May 2, 2005Publication date: October 16, 2008Inventors: Sulejman Alihodzic, Stjepan Mutak, Drazen Pavlovic, Ivana Palej, Vlado Stimac, Samra Kapic, Adrijana Vinter, Maja Matanovic Skugor
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Patent number: 7435805Abstract: The present disclosure relates to new 11-O-alkyl macrolides and azalides and pharmaceutically acceptable salts and solvates thereof, and to pharmaceutical compositions thereof. The disclosure also relates to a process for the preparation of 11-O-alkyl macrolides and azalides by regioselective 11-O-alkylation of macrolides and azalides having a vicinal diol system, using diazoalkanes in the presence of transition-metal halides or boric acid as catalysts. In another aspect, the disclosure relates to uses of the 11-O-alkyl macrolides and azalides as antibacterial agents or intermediates for the synthesis of other antibacterial agents.Type: GrantFiled: May 21, 2004Date of Patent: October 14, 2008Assignee: GlaxpSmithkline IstrazivackiInventors: Davor Kidemet, Gorjana Lazarevski, Marko Derek, Marija Leljak
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Publication number: 20080249033Abstract: 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: ApplicationFiled: May 3, 2005Publication date: October 9, 2008Inventors: Sulejman Alihodzic, Stjepan Mutak, Ivana Palej
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Publication number: 20080248105Abstract: The present invention includes EP-13420 polymorphic crystalline forms: Form I, Form II, Form Ia, and monohydrate and amorphous EP-13420 which posses distinct physical properties. In another embodiment of the present invention, there are provided methods of producing the various polymorphic forms in pure form or in combination with one another. The present invention also provides pharmaceutical compositions and formulations comprising the polymorphic and amorphous forms and methods of treating bacterial infections by administering the pharmaceutical compositions to a subject in need of such treatment.Type: ApplicationFiled: April 18, 2008Publication date: October 9, 2008Inventors: Datong Tang, Guoyou Xu, Yonghua Gai, Zhe Wang, Yat Sun Or, Hui-Yin Li
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Publication number: 20080234211Abstract: 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: ApplicationFiled: January 13, 2006Publication date: September 25, 2008Applicant: 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: 20080221046Abstract: The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides substituted at the 4? position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-?, IL-1, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.Type: ApplicationFiled: January 13, 2006Publication date: September 11, 2008Inventors: Ognjen Culic, Martina Bosnar, Nikola Marjanovic, Dubravko Jelic, Sulejman Alihodzic, Vanja Vela, Zorica Marusic-Istuk, Vesna Erakovic, Berislav Bosnjak, Boska Hrvacic, Marija Tomaskovic, Vanesa Munic, Vanesa Ivetic, Antun Hutinec, Goran Kragol, Marija Leljak
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Patent number: 7419961Abstract: Macrolides with anti-inflammatory activity are described. Particularly described are 9a-azalides and their anti-inflammatory activity without cladinose in position 3, the pharmaceutically acceptable salts thereof and the pharmaceutical composition that contain them as active principle.Type: GrantFiled: October 28, 2003Date of Patent: September 2, 2008Assignee: Zambon S.p.A.Inventors: Mauro Napoletano, Andrea Mereu, Ermanno Moriggi, Fernando Ornaghi, Gabriele Morazzoni, Franco Pellacini
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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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Publication number: 20080200404Abstract: Novel 9a-N?-substituted-carbamoyl- and thiocarbamoyl-aminoalkyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A and 3-O-decladinosyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A compounds having antimalarial activity are claimed. More particularly, the invention relates to 9a-N?-substituted-carbamoyl- and thiocarbamoyl-?-aminoethyl- or -?-aminopropyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A and 3-O-decladinosyl-9a-aza-9-deoxo-9-dihydro-9a-homoerythromycin A compounds and to pharmaceutically acceptable derivatives thereof having antimalarial activity.Type: ApplicationFiled: January 13, 2006Publication date: August 21, 2008Inventors: Mirjana Bukvic Krajacic, Nedjeljko Kujundzic, Zrinka Ivezic, Sulejman Alihodzic, Antun Hutinec, Andrea Fajdetic
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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: 7414114Abstract: The present invention provides a stable form of azithromycin derivatives that act as antibiotics. These compounds are in anhydrous form and have increased stability over the hydrated forms.Type: GrantFiled: February 24, 2003Date of Patent: August 19, 2008Assignee: Wockhardt LimitedInventors: Shiva P. Singh, Siddiqui M. Jaweed Mukarram, Manish Purohit, Anjum R. Khan
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Patent number: 7410952Abstract: The invention relates to derivatives of azithromycin, processes for the manufacture thereof and pharmaceutical compositions thereof preferably together with azithromycin.Type: GrantFiled: April 16, 2004Date of Patent: August 12, 2008Assignee: Sandoz AGInventors: Albert Codony, José Diago, Rafael Garcia, Jordi Rifa
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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: 7402568Abstract: The present invention discloses compounds of formulae I and 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: September 27, 2005Date of Patent: July 22, 2008Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Yao-Ling Qiu, Guoqiang Wang, Deqiang Niu, Ly Tam Phan
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Patent number: 7384922Abstract: 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: GrantFiled: May 3, 2006Date of Patent: June 10, 2008Assignee: Enanta Pharmaceuticals, Inc.Inventors: Guoqiang Wang, Ly Tam Phan, Yat Sun Or
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Patent number: 7384921Abstract: The present invention includes EP-13420 polymorphic crystalline forms: Form I, Form II, Form Ia, and monohydrate and amorphous EP-13420 which posses distinct physical properties. In another embodiment of the present invention, there are provided methods of producing the various polymorphic forms in pure form or in combination with one another. The present invention also provides pharmaceutical compositions and formulations comprising the polymorphic and amorphous forms and methods of treating bacterial infections by administering the pharmaceutical compositions to a subject in need of such treatment.Type: GrantFiled: February 14, 2005Date of Patent: June 10, 2008Assignee: Enanta Pharmaceuticals, Inc.Inventors: Datong Tang, Guoyou Xu, Yonghua Gai, Zhe Wang, Yat Sun Or, Hui-Yin Li
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Publication number: 20080119418Abstract: 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: ApplicationFiled: November 15, 2007Publication date: May 22, 2008Inventors: Ly Tam Phan, Yao-Ling Qiu, Yat Sun Or
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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: 7365174Abstract: Compounds represented by the general formula (1) or pharmaceutically acceptable salts thereof, effective in the prevention and/or treatment of infections with microbes: (1) (a) wherein R1 is hydrogen or straight-chain C1-6 alkylcarbonyl; R2 is hydrogen or C1-6 alkylcarbonyl; R3 is hydrogen, C1-6 alkyl, C1-6 alkylcarbonyl, C1-6 alkenyl, C2-6 alkenylcarbonyl, C2-6 alkynyl, or an Ar—B— group (wherein Ar is aryl or a heterocyclic group; and B is C1-6 alkyl, C1-6 alkylcarbonyl, C2-6 alkenyl, C2-6 alkenylcarbonyl, or C2-6 alkynyl); R5, R6, R7 and R8 are each hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, or an Ar—B?— group (wherein B? is C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl); X is oxygen or —NR4— (wherein R4 is hydrogen, C1-6 alkyl or C1-6 alkyl which may be substituted with Ar); and R4? is hydrogen or a group represented by the general formula (a) (wherein R3? and R4? are each hydrogen or straight-chain or branched C1-6 alkylcarbonyl)Type: GrantFiled: August 20, 2004Date of Patent: April 29, 2008Assignee: Meiji Seika Kaisha, Ltd.Inventors: Tomoaki Miura, Kenichi Kanemoto, Satomi Natsume, Naoto Ohkura, Yumiko Fujihira, Takashi Watanabe, Hideki Fushimi, Kunio Atsumi, Keiichi Ajito
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Patent number: 7351696Abstract: The present invention relates to compounds 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: October 29, 2003Date of Patent: April 1, 2008Assignee: Glaxo Group LimitedInventors: John Michael Berge, Catherine Simone Victoire Frydrych, Richard Lewis Jarvest
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Patent number: 7342000Abstract: The invention relates to N?-substituted 9a-N-(N?-carbamoyl-?-aminopropyl), 9a-N-(N?-thiocarbamoyl-?-aminopropyl), 9a-N-[N?-?-cyanoethyl)-N?-carbamoyl-?-aminopropyl] and 9a-N-[N?-?-cyanoethyl)-N?-thiocarbamoyl-?-am inopropyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-O-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerithronolide A, novel semi-synthetic macrolide antibiotics of the azalide series, of the general formula 1, wherein R represents H or cladinosyl moiety, R1 represents H or ?-cyanoethyl moiety, R2 represents isopropyl, 1-naphtyl, 2-naphtyl, benzyl, 2-(trifluoromethyl)phenyl, 3-phenylpropyl, ?-phenylethyl, ethoxycarbonyl-methyl, 1-(1-naphtyl)ethyl, 3,4,5-trimethoxyphenyl and 2,4-dichlorophenyl group, and X represents O and S, and their acceptable addition salts thereof with inorganic or organic acids, to the process for preparation of their pharmaceutical compositions as well as the use their compositions in the treatment of bacterial infections.Type: GrantFiled: December 10, 2003Date of Patent: March 11, 2008Assignee: GlaxoSmithKline istrazivacki center ZagrebInventors: Nedjeljko Kujundzic, Mirjana Bukvic Krajacic, Karmen Brajsa
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Publication number: 20080051352Abstract: The present invention relates to the process for the preparation of compounds of formula (I) or its pharmaceutically acceptable salts wherein, R isType: ApplicationFiled: December 18, 2006Publication date: February 28, 2008Applicant: ALEMBIC LIMITEDInventors: Pandurang Balwant Deshpande, Manish Kanchanbhai Patel, Kalpesh Haribhai Dhameliya, Parven Kumar Luthra
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Patent number: 7335753Abstract: The invention provides a family of bifunctional heterocyclic compounds useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. The invention also provides methods of making the bifunctional heterocyclic compounds, and methods of using such compounds as anti-infective, anti-proliferative agents, anti-inflammatory, and/or prokinetic agents.Type: GrantFiled: February 21, 2006Date of Patent: February 26, 2008Assignee: Rib-X Pharmaceuticals, Inc.Inventors: Deping Wang, Joyce A. Sutcliffe, Adegboyega K. Oyelere, Timothy S. McConnell, Joseph A. Ippolito, John N. Abelson, Dane M. Springer, Joseph M. Salvino, Rongliang Lou, Joel A. Goldberg, Jay J. Farmer, Erin M. Duffy, Ashoke Bhattacharjee
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Patent number: 7332476Abstract: Antimicrobial macrolide and ketolide compounds are provided having formulas XII: 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: April 23, 2004Date of Patent: February 19, 2008Assignee: Novartis AGInventors: Matthew T. Burger, Georgia Law Carroll, Daniel Chu, Xiaodong Lin, Jacob Plattner, Alice Rico
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Patent number: 7312201Abstract: 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: December 25, 2007Assignee: Enanta Pharmaceuticals, Inc.Inventors: Datong Tang, Yonghua Gai, Ying Sun, Yat Sun Or, Zhe Wang
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Patent number: 7309782Abstract: The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections.Type: GrantFiled: August 28, 2003Date of Patent: December 18, 2007Assignee: Pfizer Inc.Inventors: Zheng J. Li, Andrew V. Trask
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Patent number: 7307156Abstract: The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections.Type: GrantFiled: August 27, 2003Date of Patent: December 11, 2007Assignee: Pfizer Inc.Inventors: Zheng J. Li, Andrew V. Trask, Joseph E. Mertz
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Publication number: 20070281894Abstract: The present disclosure is directed to novel macrolide antibiotics of Formula 1 and pharmaceutically acceptable salts and prodrugs thereof; and the chemical syntheses and medical uses of these novel macrolide antibiotics for the treatment and/or management of infections caused by various aerobic and anaerobic gram-positive and gram-negative microorganisms as well as various mycobacteria.Type: ApplicationFiled: May 31, 2007Publication date: December 6, 2007Applicant: Auspex Pharmaceuticals, Inc.Inventors: Thomas G. GANT, Sepehr Sarshar
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Patent number: 7297682Abstract: 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]-?-L-ribo-hexopryanosyl]oxy]-2-ethyl-3,4,10-trihydroxy-3,5,8,10,12,14-hexamethyl-11-[[3,4,6-trideoxy-3-(dimethylamino)-?-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: GrantFiled: May 6, 2004Date of Patent: November 20, 2007Assignees: Pfizer Inc., Pfizer Products Inc.Inventors: Robert J. Rafka, Colman B. Ragan, Douglas J. M. Allen
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Publication number: 20070259822Abstract: The present invention discloses compounds of formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which exhibit antibacterial properties. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject in need of antibiotic treatment. The invention also relates to methods of treating a bacterial infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention. The invention further includes process by which to make the compounds of the present invention.Type: ApplicationFiled: May 1, 2007Publication date: November 8, 2007Inventors: Yat Sun Or, Ly Tam Phan, Guoqiang Wang
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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: 7282486Abstract: The invention relates to novel crystal forms of azithromycin, an antibiotic useful in the treatment of infections.Type: GrantFiled: August 27, 2003Date of Patent: October 16, 2007Assignee: Pfizer IncInventors: Zheng J. Li, Andrew V. Trask
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Patent number: 7276487Abstract: 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: September 21, 2004Date of Patent: October 2, 2007Assignee: Enanta Pharmaceuticals, Inc.Inventors: Guoqiang Wang, Yulin Peng, Yanchun Wang, Ly Tam Phan, Yat Sun Or
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Patent number: 7273853Abstract: 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: January 25, 2005Date of Patent: September 25, 2007Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Guoqiang Wang, 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, Guoyou Xu
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Patent number: 7271155Abstract: The present invention discloses compounds of formulae I and 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: January 3, 2006Date of Patent: September 18, 2007Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yat Sun Or, Ly Tam Phan, Guoqiang Wang, Yanchun Wang, Yulin Peng
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Publication number: 20070207972Abstract: The present invention relates to processes and intermediates for the preparation of 6-11 bicyclic erythromycin derivative known as EDP-182 (IX-a).Type: ApplicationFiled: January 23, 2007Publication date: September 6, 2007Inventors: Guoyou Xu, Yonghua Gai, Guoqlang Wang, Yat Sun Or, Zhe Wang
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Patent number: RE39836Abstract: Compounds of the formula wherein Ra is H; substituted or unsubstituted alkyl (1-10C); substituted or unsubstituted alkenyl (2-10C); substituted or unsubstituted alkynyl (2-10C); substituted or unsubstituted aryl (4-14C); substituted or unsubstituted arylalkyl (5-20C); or ORa is replaced by H; 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 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; L is methylene or carbonyl; T is —O—, —N(R)—, —N(OR)—, —N(NHCOR)—, —N(N?CHR)—, or —N(NHR)— wherein R is H or Ra as defined above, with the proviso that when L is methylType: GrantFiled: July 13, 2005Date of Patent: September 11, 2007Assignee: Kosan Biosciences, Inc.Inventors: Daniel Chu, Gary Ashley
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Patent number: RE40040Abstract: The subject-matter of the invention is a process for the stereoselective preparation of a compound of general formula I by stereoselective displacement by a nitrogenous nucleophilic compound of the activated alcohol functional group present at this 4? position in a corresponding derivative of formula II.Type: GrantFiled: September 9, 2005Date of Patent: January 29, 2008Assignee: Merial LimitedInventors: Patrick Leon, Frederic Lhermitte, Ronan Guevel, Denis Pauze, Laurent Garel, Gilles Oddon