3-position Substituent Contains Pyridine Ring Patents (Class 514/203)
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Patent number: 8119622Abstract: 7-phenyl-substituted tetracycline compounds which are substantially free of positional isomers, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-phenyl-substituted tetracycline compounds are described. 7-substituted tetracycline compounds which are substantially free of positional isomers, methods of treating tetracycline responsive states, and pharmaceutical compositions containing the 7-substituted tetracycline compounds are described.Type: GrantFiled: December 10, 2009Date of Patent: February 21, 2012Assignee: Trustees of Tufts CollegeInventors: Mark L. Nelson, Mohamed Y. Ismail
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Publication number: 20120027833Abstract: Polymeric porous films, capable of eluding a bioactive agent when coming in contact with a physiological medium according to a pre-determined and controlled release profile suitable for particular type of drug and indication, and medical devices including the same are disclosed. Also disclosed are processes for producing the polymeric porous films by freeze-drying an inverted emulsion formulation in which the polymer's composition, the polymer's concentration, the polymer's initial molecular weight, the concentration and/or the type of a surfactant, the homogenization rate and/or the oil phase to aqueous phase ratio (O:A) are selected so as to impart a desired release profile of the bioactive agent from the polymeric film.Type: ApplicationFiled: August 2, 2011Publication date: February 2, 2012Applicant: Ramot at Tel-Aviv University Ltd.Inventor: Meital ZILBERMAN
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Publication number: 20120010180Abstract: The present invention relates to new dosage forms of cephem compounds, useful for the treatment of bacterial infections. The dosage forms are stable, exhibit enhanced solubility, and are particularly well suited for, e.g., parenteral administration.Type: ApplicationFiled: September 19, 2011Publication date: January 12, 2012Applicant: FOREST LABORATORIES HOLDINGS LTD.Inventors: Mahendra G. Dedhiya, Yigong Ge, Chun (Vernon) Jiang
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Publication number: 20110294774Abstract: The present invention provides a pharmaceutical composition useful for treating bacterial infections in humans and animals which comprises administering to a human or animal in need thereof, an antibacterially effective combination of a ?-lactam antibiotic and an inhibitor of any bacterial peptidoglycan biosynthesis enzyme, especially GlmU, GlmU, MurA, MurB, MurC, MurD, MurE, MurF, MurG, MraY, and UppS.Type: ApplicationFiled: May 6, 2011Publication date: December 1, 2011Applicant: TRIUS THERAPEUTICSInventors: Vickie Brown-Driver, Kedar GC, John M. Finn, Robert Haselbeck, Mark Hilgers, Karen Shaw, Mark Stidham
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Publication number: 20110257147Abstract: A method for improving sexual function is described. A mammal suffering from sexual dysfunction or otherwise in need of enhanced sexual function is administered a compound selected from those that are capable of inhibiting the activity of ?-lactams, penicillin-binding protein, carboxypeptidase. Such compounds, including particularly ?-lactam ring-containing compounds, can be used to formulate pharmaceutical formulations useful for improving sexual function.Type: ApplicationFiled: June 27, 2011Publication date: October 20, 2011Applicant: Revaax Pharmaceuticals, LLCInventor: Gary A. Koppel
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Publication number: 20110245148Abstract: The present invention relates to a composition comprising: a) 0.01-20% wt/wt acetic acid and b) a physiologically tolerable buffer capable of maintaining acetic acid at a pH in the range of 2-7; and use of such a composition as an antimicrobial agent.Type: ApplicationFiled: June 23, 2009Publication date: October 6, 2011Applicants: DANMARKS TEKNISKE UNIVERSITET, BISPEBJERG HOSPITAL, RIGSHOSPITALET COPENHAGEN UNIVERTISY HOSPITALInventors: Michael Christian Givskov, Thomas Bjarnsholt, Preben Homoe, Niels Hoiby, Peter Østrup Jensen, Helle Krogh Johansen, Klaus Kirketerp-Moller
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Publication number: 20110091515Abstract: Composite structures composed of a device as a core structure, being a medical device or article, and a porous polymeric coat and designed capable of encapsulating bioactive agents while retaining the activity of these agents are disclosed. Further disclosed are processes of preparing such composite structures.Type: ApplicationFiled: June 11, 2009Publication date: April 21, 2011Applicant: Ramot at Tel-Aviv University Ltd.Inventors: Meital Zilberman, Yoel Kloog, Amir Kraitzer, Jonathan Elsner
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Publication number: 20110082099Abstract: The present invention relates to methods and compositions to treat subjects having cystic fibrosis. These compositions comprise the class of isothiocyanates. Isothiocyanates, absorbed by a cell are conjugated with glutathione GSH by glutathione-s-tranferase (GST). The conjugates are substrates of the multi-drug resistance associated (MRP)/multi-drug resistance (MDR) proteins. These proteins are functionally redundant to the cystic fibrosis transmembrane conductance regulator (CFTR), allowing for the substrate conjugates to be exported from the cell. The export of GSH conjugates restores intracellular and extracellular levels of GSH to normal levels. Normalizing both extracellular and intracellular GSH via the increased conjugation of isothiocyanates with GSH, and subsequent export, can significantly rectify numerous enzymatic processes and correct the pathologies that are typical of patients suffering from cystic fibrosis.Type: ApplicationFiled: June 14, 2010Publication date: April 7, 2011Inventor: Melanie Childers
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Publication number: 20110046102Abstract: The invention concerns the compounds meeting formula (I: wherein one of R1 and R2 is a hydrogen and the other a fluorine or both represent a fluorine, in free form, in the form of zwitterions and of salts with pharmaceutically acceptable mineral or organic bases, the preparation thereof and their use as medicinal products inhibiting the action of ?-lactamases by pathogenic bacteria.Type: ApplicationFiled: April 24, 2009Publication date: February 24, 2011Applicant: NovexelInventors: Benoit Ledoussal, Marie-Edith Gourdel
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Patent number: 7875604Abstract: The present invention describes novel methods of identifying compounds which inhibit HIV particle formation and Rev-dependent HIV production. The present invention also provides methods and compounds for inhibiting HIV particle formation and or treating patients infected with HIV.Type: GrantFiled: February 1, 2005Date of Patent: January 25, 2011Assignee: University of Virginia Patent FoundationInventors: David Rekosh, Marie-Louise Hammarskjöld
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Patent number: 7871997Abstract: This invention provides cephalosporin compounds and salts thereof. Such compounds are useful for preparing cross-linked glycopeptide-cephalosporin antibiotics.Type: GrantFiled: December 19, 2007Date of Patent: January 18, 2011Assignee: Theravance, Inc.Inventors: Paul R. Fatheree, Martin S. Linsell, Daniel Marquess, Daniel D. Long, Jason P. Chinn, Matthew B. Nodwell, Edmund J. Moran, James B. Aggen
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Publication number: 20100285012Abstract: The subject application provides small compounds that are able to suppress autophagy in various cells. These compounds are useful in augmenting the existing treatments of various cancers and microbial/parasitic infections. Thus, the subject application also provides methods of treating various types of cancers and microbial/parasitic infections. Also provided by the subject application are methods of suppressing the expansion of autophagosomes within cells or individuals and inhibiting the lipidation of autophagy-related protein 8 (Atg8).Type: ApplicationFiled: January 5, 2009Publication date: November 11, 2010Applicant: University of FLorida Research Foundation Inc.Inventors: William A. Dunn, JR., Debra E. Akin, Ann Progulske-Fox, David A. Ostrov
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Publication number: 20100272808Abstract: Drugs are formulated as oral dosage forms for controlled release in which the release rate limiting portion is a shell surrounding the drug-containing core. The shell releases drug from the core by permitting diffusion of the drug from the core. The shell also motes gastric retention of the dosage form by swelling upon imbibition of gastric fluid to size that is retained in the stomach during the postprandial or fed mode.Type: ApplicationFiled: April 29, 2010Publication date: October 28, 2010Inventors: Bret Berner, Jenny Louie-Helm, Gloria Gusler, John N. Shell
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Publication number: 20100216745Abstract: The present invention relates to new cephem compounds useful for the treatment of bacterial infections. The invention also relates to methods of preparing the compounds, pharmaceutical compositions comprising the compounds, and to methods of treatment using the compounds. The new cephem compounds are stable, exhibit good solubility, and are particularly well suited for, e.g., parenteral administration for the treatment of bacterial infections.Type: ApplicationFiled: February 23, 2010Publication date: August 26, 2010Applicant: FOREST LABORATORIES HOLDINGS LTD.Inventors: Mahendra G. Dedhiya, Brahma N. Singh
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Publication number: 20100197650Abstract: The present invention provides compositions comprising ceftaroline or a pharmaceutically acceptable salt, solvate or a prodrug thereof alone or in combination with an antibacterial agent. The present invention provides methods of treating bacterial infection, which include administering an effective amount of ceftaroline or a pharmaceutically acceptable salt, solvate or a prodrug thereof alone or in combination with an antibacterial agent.Type: ApplicationFiled: August 28, 2009Publication date: August 5, 2010Applicant: FOREST LABORATORIES HOLDINGS LTD.Inventor: Donald Biek
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Patent number: 7754707Abstract: Methods for treating a host suffering from a chronic immune disease, e.g., MS or CFS, are provided. In practicing the subject methods, an effective amount of an elastase inhibitory agent, e.g., a ?-lactam containing compound, is administered to the host. Also provided are compositions for use in practicing the subject methods.Type: GrantFiled: June 30, 2004Date of Patent: July 13, 2010Assignee: R.E.D. Laboratories, N.V./S.A.Inventors: Karim El Bakkouri, Patrick Englebienne, Kenny De Meirleir, Charles Vincent Herst
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Publication number: 20100152101Abstract: The present invention relates to the use of a Compound of formula I preferably 4-[3,5-bis(2-hydroxyphenyl)-[1,2,4]triazol-1-yl]benzoic acid or a pharmaceutically acceptable salt thereof for the preparation of a medicament for use in the treatment of biofilm formation, e.g. of P. aeruginosa, e.g. in cystic fibrosis patients.Type: ApplicationFiled: May 21, 2008Publication date: June 17, 2010Applicant: Novartis AGInventor: David Reid
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Patent number: 7723389Abstract: The invention provides pharmaceutical compositions for the treatment or prevention of the toxic effects of therapeutic agents and methods of treating or preventing such toxicity using a toxicity reducing amount of N-acetylcysteine either alone or in combination with a therapeutically effective amount or, to achieve its therapeutic advantages, an amount larger than what is customarily given as a therapeutically effective amount, of a therapeutic agent.Type: GrantFiled: November 4, 2002Date of Patent: May 25, 2010Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Leonard A. Herzenberg, Leonore A. Herzenberg, Stephen C. De Rosa, James Andrus
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Publication number: 20100029604Abstract: The invention relates to a pharmaceutical composition comprising an ethylene derivatives of tricyclic carbapenems of the general Formula (I) in the form of pure diastereoisomers and in the form of pure geometric isomers or a salt, ester or amide derivate thereof and an antibiotic and the use of this composition as a broad band spectrum ?-lactamase inhibitor.Type: ApplicationFiled: February 13, 2008Publication date: February 4, 2010Inventors: Andrej Prezelj, Uros Urleb, Tomaz Solmajer
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Publication number: 20100004189Abstract: Provided are electrokinetically-altered fluids (gas-enriched (e.g., oxygen-enriched) electrokinetic fluids) comprising an ionic aqueous solution of charge-stabilized oxygen-containing nanostructures in an amount sufficient to provide, upon contact with a cell, modulation of at least one of cellular membrane potential and cellular membrane conductivity, and therapeutic compositions and methods for using same in treating cystic fibrosis or a symptom thereof. The electrokinetically-altered fluid compositions and methods include electrokinetically-altered fluids optionally in combination with other therapeutic agents (e.g., antibiotics, albuterol, budesonide, etc.). Particular embodiments comprise use and/or synergy with tobramycin for treating bacterial infection, and use and/or synergy with a bronchiodilator.Type: ApplicationFiled: May 1, 2009Publication date: January 7, 2010Applicant: Revalesio CorporationInventors: Richard L. Watson, Anthony B. Wood, Gregory J. Archambeau
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Publication number: 20090306035Abstract: Methods and compositions comprising chemical compounds that modulate the silencing of a polynucleotide of interest in a cell are provided. Such chemical compounds when used in combination with an appropriate silencing element can be used to modulate (increase or decrease) the level of the polynucleotide targeted by the silencing element. Methods of using such compositions both in therapies involving RNAi-mediated suppression of gene expression, as well as, in vitro methods that allow for the targeted modulation of expression of a polynucleotide of interest are provided. Pharmaceutical or cosmetic formulations comprising such compounds and silencing elements also are disclosed. Methods for screening a compound of interest for the ability to modulate the activity of a heterologous silencing element also are provided.Type: ApplicationFiled: August 25, 2006Publication date: December 10, 2009Applicant: Emory UniversityInventors: Jin Peng, Ge Shan, Stephen Warren
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Patent number: 7612087Abstract: This invention discloses and claims methods for inhibiting bacterial ?-lactamases and treating bacterial infections by inhibiting bacterial ?-lactamases in man or an animal comprising administering a therapeutically effective amount to said man or said animal of a compound, or pharmaceutically acceptable salt thereof, of formula (I) either alone or in combination with a ?-lactamine antibiotic wherein said combination can be administered separately, together or spaced out over time. Pharmaceutical compositions comprising a compound of formula (I), or a combination of a compound of formula (I) and a therapeutically effective amount of a ?-lactamine antibiotic, and a pharmaceutically acceptable carrier are also disclosed and claimed.Type: GrantFiled: July 26, 2004Date of Patent: November 3, 2009Assignee: NovexelInventors: Jozsef Aszodi, Claude Fromentin, Maxime Lampilas, David Alan Rowlands
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Publication number: 20090131394Abstract: Broad spectrum beta-lactamase inhibitors. Certain inhibitors also exhibit potent antibiotic activity in addition to beta-lactamase inhibition. Compounds of the invention are designed such that on cleavage of the beta-lactam ring reactive moieties are generated which can inactivate beta-lactamase. Also provided are methods of making beta-lactamase inhibitors and beta-lactam antibiotics exhibiting such inhibition. Additionally provided are pharmaceutical compositions for treatment or prevention of bacterial infections and methods of treatment of such infections.Type: ApplicationFiled: October 9, 2008Publication date: May 21, 2009Inventors: Larry Sutton, Sophia Yu
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Publication number: 20090053149Abstract: A surfactant can be added, safely and effectively, to a drug solution containing any antimicrobial agent, such as an antibiotic like tobramycin, that is suitable for administration to the lungs via inhalation. Thus, when an aerosolized drug solution includes surfactant, Marangoni flows cause the drug particles, once deposited in the lungs, to spread over a wider surface area, thereby ensuring greater antimicrobial efficacy. A solution that contains, for example, an antibiotic and tyloxapol or another surfactant providing a similar surface tension to the composition is optimally delivered by the functional combination of a breath-actuated nebulizer and a high-flow compressor.Type: ApplicationFiled: August 21, 2008Publication date: February 26, 2009Inventors: Tim Corcoran, Amy Lise Marcinkowski, Joseph Pilewski, Kristina Thomas
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Patent number: 7488724Abstract: The invention provides compounds of formula (I): wherein: R1-R4 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting ?-lactamase enzymes, for enhancing the activity of ?-lactam antibiotics, and for treating ?-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula (I), and intermediates useful for the synthesis of compounds of formula (I).Type: GrantFiled: May 10, 2005Date of Patent: February 10, 2009Assignee: Southern Methodist University Foundation for ResearchInventors: John D. Buynak, Lakshminarayana Vogeti
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Publication number: 20080318919Abstract: This invention is directed generally to cefquinome compositions, processes for making such compositions, uses of such compositions to make medicaments, kits for making such compositions, and methods for using such compositions and kits to treat infections.Type: ApplicationFiled: October 27, 2006Publication date: December 25, 2008Applicant: Intervet International B.V.Inventors: Susan M. Cady, Carole Barbot
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Publication number: 20080226736Abstract: Inhalatory pharmaceutical composition comprising a drug, a soluble excipient and a surfactant, characterized by: said soluble excipient is present in an amount between 10% and less than 100% by weight; —the weight ratio between said surfactant and said drug is between 0.01 and 10; —the particle size of at least 50% of the particles of said powder is below 5 ?m; —the bulk density db of said powder is between 0.1 and 0.3 g/cc; —the tapped density dt of said powder is between 0.15 and 0.7 g/cc; —the ratio db/dt is between 0.2 and 0.65.Type: ApplicationFiled: October 20, 2006Publication date: September 18, 2008Applicant: ERATECH S.R.L.Inventors: Giovanni Caponetti, Loretta Maggi, Laura Zanellotti, Cristina Veneziani
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Patent number: 7419973Abstract: A cephem compound (particularly its crystal) represented by the formula [I], wherein X is CH3COOH, CH3CH2COOH or CH3CN, and n is 0 to 5, is useful as an antibacterial agent (particularly anti-MRSA agent) and shows superior quality such as high solid stability, possible long-term stable preservation and the like.Type: GrantFiled: February 23, 2005Date of Patent: September 2, 2008Assignee: Takeda Pharmaceutical Company LimitedInventors: Tomoyasu Ishikawa, Shohei Hashiguchi, Yuji Iizawa
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Patent number: 7384928Abstract: A compound of the formula: (wherein, T is S, SO or O; X is halogen, CN, carbamoyl optionally substituted with lower alkyl, lower alkyl, lower alkoxy, or lower alkylthio; A is substituted lower alkylene (wherein the substituent is optionally substituted mono lower alkyl, optionally substituted lower alkylidene, or optionally substituted lower alkylene); Z+ is an optionally substituted, a cation and an N atom-containing heterocyclic group), ester, amino-protected compound wherein the amino bonds to a thiazole ring at the 7-position, or pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: March 18, 2003Date of Patent: June 10, 2008Assignee: Shionogi & Co., Ltd.Inventors: Yasuhiro Nishitani, Yoshinori Yamano
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Publication number: 20080132457Abstract: Efflux pump inhibitors are co-administered with antimicrobial agents for the treatment of ophthalmic or otic infections. The agents may be co-administered directly to the site of infection (e.g., the eye or ear).Type: ApplicationFiled: September 17, 2007Publication date: June 5, 2008Inventors: Keith Bostian, Thomasz Glinka, Olga Lomovskaya, Mark Surber, Neil Berkley, David Griffith
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Patent number: 6936709Abstract: A protected 2?-deoxycytidine is purified by precipitating the protected 2?-deoxycytidine represented by general formula (3) in the form of a hydrated crystal from a solution containing the protected 2?-deoxycytidine and water, and by recovering the protected 2?-deoxycytidine: wherein R1 represents a 4-methoxytrityl, 4, 4?-dimethoxytrityl, or triphenylmethyl group; and B1 represents a cytosine group having a protected amino group. The compound represented by general formula (3) is, in particular, a protected 2?-deoxycytidine represented by formula (4): The 2?-deoxycytidine is used as a raw material for antisense DNA.Type: GrantFiled: June 4, 2003Date of Patent: August 30, 2005Assignee: Mitsui Chemicals, Inc.Inventors: Hiroki Ishibashi, Kiyoteru Nagahara, Yasushi Fukuiri, Yasuko Matsuba
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Patent number: 6916801Abstract: The invention provides compounds of formula (I): wherein: R1-R4 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting ?-lactamase enzymes, for enhancing the activity of ?-lactam antibiotics, and for treating ?-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula (I), wherein R1 and R2 are each independently hydrogen, (C1-C10)alkyl, (C2-C10)alkenyl, (C2-C10)alkenyl, (C3-C8)cycloalkyl, (C1-C10)alkoxy, (C1-C10)alkanoyl, (C1-C10)alkanoyloxy, (C1-C10)alkoxycarbonyl, aryl, heterocycle, halo, cyano, nitro, —COORe, —C(?O)NRfRg, —OC(?O)NRfRg, NRfRg, or —S(O)nRh; R3 is hydrogen, halo, aryl, heteroaryl, —S(O)nRh, or —CH?CHC(?O)NRmRp; R4 is hydrogen; A is thio, sulfinyl, or sulfonyl; and intermediates useful for the synthesis of compounds of formula (I).Type: GrantFiled: July 24, 2002Date of Patent: July 12, 2005Assignee: Alamx, LLCInventors: John D. Buynak, Lakshminarayana Vogeti
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Patent number: 6906055Abstract: A cephem compound (particularly its crystal) represented by the formula [I], wherein X is CH3COOH, CH3CH2COOH or CH3CN, and n is 0 to 5, is useful as an antibacterial agent (particularly anti-MRSA agent) and shows superior quality such as high solid stability, possible long-term stable preservation and the like.Type: GrantFiled: August 10, 2001Date of Patent: June 14, 2005Assignee: Takeda Chemical Industries, Ltd.Inventors: Tomoyasu Ishikawa, Shohei Hashiguchi, Yuji Iizawa
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Patent number: 6800621Abstract: A cefem compound of the formula (I) shows wide antibacterial spectrum against various pathogenic bacteria including MRSA. wherein, X is N or CY and Y is H or halogen; R1 is amino or protected amino; R2 is hydrogen or optionally substituted lower alkyl etc.; R3 is hydrogen etc.; R4 is hydrogen, optionally substituted lower alkyl, or optionally substituted N-containing heterocyclic group etc.; R5 is hydrogen etc.; and a wavy line means syn- or anti-isomerism or a mixture thereof.Type: GrantFiled: December 13, 2002Date of Patent: October 5, 2004Assignee: Shionogi & Co., Ltd.Inventors: Yasuhiro Nishitani, Hikaru Itani, Tadashi Irie
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Publication number: 20040157821Abstract: The present invention provides sulfates of cefem compound (I) of the following formula, solvates thereof or crystals of the same, which are of high quality and useful as medicines such as an injection.Type: ApplicationFiled: October 3, 2003Publication date: August 12, 2004Inventors: Hikaru Itani, Tadashi Irie, Fumihiko Matsubara, Hidetoshi Myojyo
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Patent number: 6723716Abstract: The present invention relates to a cephem prodrug having formula III or formula IV: or a pharmaceutically acceptable salt thereof, wherein R′1 is selected from the group consisting of hydrogen and —C(O)CH(NH2)CH3 and R′2 is selected from the group consisting of hydrogen and an acyl group that is cleaved by an enzyme found in mammals, with the proviso that, when either R′1 or R′2 is hydrogen, the other is not. A, B, L, G, E, and J are each independently nitrogen or carbon such that the respective rings are selected from the group consisting of provided that the group —CH2—S—CH2CH2NHR′2 is attached only to a carbon atom of said heterocyclic group, and Q is selected from the group consisting of nitrogen and —CX, wherein X is selected from the group consisting of hydrogen and chlorine.Type: GrantFiled: September 21, 2000Date of Patent: April 20, 2004Assignee: Essential Therapeutics, Inc.Inventors: Scott J. Hecker, Aesop Cho, Tomasz W. Glinka, Trevor Calkins, Ving J. Lee
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Publication number: 20030149014Abstract: A cefem compound of the formula (I) shows wide antibacterial spectrum against various pathogenic bacteria including MRSA.Type: ApplicationFiled: December 13, 2002Publication date: August 7, 2003Applicant: Shionogi & Co., Ltd.Inventors: Yasuhiro Nishitani, Hikaru Itani, Tadashi Irie
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Patent number: 6583133Abstract: Disclosed are cephalosporin derivatives of the general formula wherein R is an organic residue with a molecular weight not exceeding 400 bonded to the adjacent sulphur atom via carbon and consisting of carbon, hydrogen, and optional oxygen, sulfur, nitrogen and/or halogen atoms; R1 is hydrogen, lower alkyl or phenyl; and A is a secondary, tertiary or quaternary nitrogen atom bound directly to the propenyl group and being substituted by an organic residue with a molecular weight not exceeding 400 and consisting of carbon, hydrogen, and optional oxygen, sulfur, nitrogen and/or halogen atoms, as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts.Type: GrantFiled: June 22, 1999Date of Patent: June 24, 2003Assignee: Basilea Pharmaceutica AGInventors: Peter Angehrn, Erwin Götschi, Ingrid Heinze-Krauss, Hans G. F. Richter
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Patent number: 6531465Abstract: A compound of formula wherein Ac, R1 and R2 have various meanings, a process for a preparation thereof and its use as a pharmaceutical, i.e. as antibacterial agent.Type: GrantFiled: May 21, 2001Date of Patent: March 11, 2003Assignee: Biochemie Gesellschaft m.b.H.Inventors: Gerd Ascher, Johannes Ludescher
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Patent number: 6518263Abstract: A cefem compound of the formula (I) shows wide antibacterial spectrum against various pathogenic bacteria including MRSA. wherein, X is N or CY and Y is H or halogen; R1 is amino or protected amino; R2 is hydrogen or optionally substituted lower alkyl etc.; R3 is hydrogen etc.; R4 is hydrogen, optionally substituted lower alkyl, or optionally substituted N-containing heterocyclic group etc.; R5 is hydrogen etc.; and a wavy line means syn- or anti-isomerism or a mixture thereof.Type: GrantFiled: May 25, 2001Date of Patent: February 11, 2003Assignee: Shionogi & Co., Ltd.Inventors: Yasuhiro Nishitani, Hikaru Itani, Tadashi Irie
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Patent number: 6407091Abstract: The invention provides compounds of formula I and IV: wherein R1-R11 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting &bgr;-lactamase enzymes, for enhancing the activity of &bgr;-lactam antibiotics, and for treating &bgr;-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I and IV, and novel intermediates useful for the synthesis of compounds of formula I and IV. The A can be, for example, thio, sulfinyl, or sulfonyl.Type: GrantFiled: April 13, 2000Date of Patent: June 18, 2002Assignee: Research Corporation Technologies, Inc.Inventors: John D. Buynak, A. Srinivasa Rao, Greg C. Adam, Sirishkumar D. Nidamarthy, Venkata Ramana Doppalapudi
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Publication number: 20020049191Abstract: The present invention provides a novel series of cephem derivatives of the general formula I 1Type: ApplicationFiled: May 29, 2001Publication date: April 25, 2002Inventors: Dane M. Springer, Bing Y. Luh, Stanley V. D'Andrea, Thomas W. Hudyma, Oak K. Kim
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Patent number: 6294527Abstract: An antibacterial compound wherein represents benzene ring, pyridine ring, pyrazine ring or 5-membered aromatic neterocycle (having one oxygen or sulfur atom as ring-constituting atom), there being no R4 where represents 5-membered aromatic heterocycle; X and Y respectively represent hydrogen atom or CXY represents C═N—OR5 wherein R5 represents hydrogen atom, halo C1-C6 alkyl or C3-C7 cycloalkyl; R1 represents phenyl, furyl, thienyl, thiazolyl (which may be substituted by amino group), tetrazolyl or thiadiazolyl, R2, R3 and R4 respectively represent hydrogen atom, halogen, hydroxyl group, nitro, C1-C6 alkoxy, trifluoromethyl, isothiuronium C1-C6 alkyl, amino C1-C6 alkyl, halo C1-C6 alkyl, morpholino, piperidino or piperazinyl.Type: GrantFiled: July 20, 1999Date of Patent: September 25, 2001Assignee: Zenyaku Kogyo Kabushiki KaishaInventors: Hideaki Hanaki, Hiroaki Yamazaki, Yoshio Tsuchida, Hideki Sato, Keiichi Hiramatsu, Seiichiro Kawashima
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Publication number: 20010011085Abstract: The present invention relates to cephem-derivatives and to a process for their preparation, having proper substituents at C-2 position, i.e. heterocyclylthio or acyloxy group. They are potent protease inhibitors, in particular human leucocyte elastase (HLE) inhibitors.Type: ApplicationFiled: August 14, 1997Publication date: August 2, 2001Inventors: MARCO ALPEGIANI, PIERLUIGI BISSOLINO, MASSIMILIANO PALLADINO, ETTORE PERRONE
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Patent number: 6265394Abstract: Provided by the present invention are cephem derivatives represented by the general formula wherein Ar is an optionally substituted lipophilic phenyl, naphthyl or pyridyl group; L1 and L2 are (C1-C6)alkylene optionally substituted with hydroxy or oxo and/or optionally interrupted with a vinylene group, S, O, aryl, heteroaryl, in which R1 is H or (C1-C6)alkyl; A is CO2H, PO3H, SO3H, tetrazolyl or x′{circle around (−)} is a pharmaceutically acceptable anion; and Q is an quaternized nitrogen group. The derivatives are gram-positive antibacterial agents especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.Type: GrantFiled: August 4, 1999Date of Patent: July 24, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Roman Z. Sterzycki, Oak K. Kim, Yasutsugu Ueda, Stanley V. D'Andrea, Dane M. Springer
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Patent number: 6214818Abstract: A cephem compound, wherein the cephem ring has a substituent at the 3-position, which substituent is shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a): The cephem compounds of the present invention are useful as antibiotic agents.Type: GrantFiled: October 1, 1998Date of Patent: April 10, 2001Assignee: Shionogi & Co., Ltd.Inventors: Yasuhiro Nishitani, Koji Ishikura
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Patent number: 6159961Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is hydrogen or hydroxy protective group,R.sup.3 is carboxy or protected carboxy,R.sup.4 is hydrogen, lower alkenyl, acyloxy(lower)alkenyl, optionally substituted heterocyclic(lower)alkenyl, optionally substituted heterocyclic(lower)alkenylthio, optionally substituted heterocyclic(lower)alkylthio, or optionally substituted heterocyclic-thio(lower)alkylthio andR5 is halogen or lower alkyland pharmaceutically acceptable salts thereof, which is useful as a medicament for prophylactic and therapeutic treatment of infectious diseases.Type: GrantFiled: July 19, 1999Date of Patent: December 12, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kohji Kawabata, Hirofumi Yamamoto, Yoshiteru Eikyu, Shinya Okuda, Hisashi Takasugi
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Patent number: 6159706Abstract: The present invention provides a method for targeting toxic antimetabolites to gram negative infections. It provides a means of taking advantage of a key disease resistance mechanism to activate these drugs locally, and to overcome the resistance phenotype of the microbes. The invention further provides a method for selecting for antibiotic sensitivity, since a likely mechanism by which organisms are likely to gain resistance to the prodrugs is via loss of enzyme activity, which will make the bacteria sensitive to antibiotics once again.Type: GrantFiled: December 18, 1998Date of Patent: December 12, 2000Assignee: NewBiotics, Inc.Inventor: H. Michael Shepard
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Patent number: 6093712Abstract: Provided are cephem derivatives represented by the general formula ##STR1## wherein Ar, R.sup.1, R.sup.2, R.sup.3, R.sup.9 and R.sup.10 are as defined in the application. The derivatives are gram-positive antibacterial agents especially useful in the treatment of diseases caused by methicillin-resistant Staphylococcus aureus.Type: GrantFiled: December 10, 1998Date of Patent: July 25, 2000Assignee: Bristol-Meyers Squibb CompanyInventors: John D. Matiskella, Stanley V. D'Andrea, Thomas W. Hudyma, Yasutsugu Ueda, Oak K. Kim, Raymond F. Miller, Shelley E. Hoeft, Joanne J. Bronson
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Patent number: 6066630Abstract: The present invention includes novel compounds of formula ##STR1## where R.sup.99 is selected from the group consisting of sulfur, SO, SO.sub.2, NH, N-alkyl, oxygen, C.dbd.C (cis or trans), and C.tbd.C, and R.sup.12 is ##STR2## The invention also includes the pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.Type: GrantFiled: October 11, 1996Date of Patent: May 23, 2000Assignee: Microcide Pharmaceuticals, Inc.Inventors: In-Seop Cho, Scott J. Hecker, Tomaz W. Glinka, Ving J. Lee, Zhijia J. Zhang