7-position Substituent Contains Hetero Ring Patents (Class 514/206)
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Publication number: 20100222289Abstract: Methods for diagnosing and treating chronic fatigue syndrome in a patient comprise, for example, testing tissue of the patient for the presence of nucleic acid molecules of one or more CFS-causing herpesviruses and one or more non-herpesvirus infectious agents, and diagnosing the patient's CFS as (a) caused by one or more herpesvirus and no non-herpesvirus infectious agent; (b) caused by one or more herpesviruses and at least one non-herpesvirus infectious agent; (c) not caused by a herpesvirus and caused by at least one non-herpesvirus infectious agent; and (d) not caused by a herpesvirus and not caused by at least one non-herpesvirus infectious agent. In some embodiments, the methods of treating comprise administering a therapeutically effective amount of at least one pharmaceutical composition for each herpesvirus and/or non-herpesvirus infectious agent present found in the patient.Type: ApplicationFiled: October 22, 2008Publication date: September 2, 2010Applicant: CFS Research LLCInventor: Albert Martin Lerner
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Publication number: 20100215716Abstract: An orthopedic implant suitable for insertion into the body of a subject, the implant comprising: a metal substrate having one or more surfaces operable to contact a bone tissue or soft tissue when implanted into the subject; a coating comprising a resorbable polymer impregnated with an admixture of a rifamycin antibiotic and a second antibiotic selected from the group consisting of tetracyclines, penicillin, ampicillin, cefazolin, clindamycin, erythromycin, levofloxacin, or vancomycin. The adhered coating layer present on the one or more surfaces is capable of releasing the rifamycin and second antibiotics in an antimicrobially effective amount. Method for making an antibiotic coated implant by mixing a resorbable polymer mixture with an antibiotic solution forming a coating solution, applying the coating solution to a surface of the implant and evaporating the solvent from the coated layer.Type: ApplicationFiled: February 23, 2010Publication date: August 26, 2010Applicant: Biomet Manufacturing Corp.Inventors: Karen S. TROXEL, Sona SUNDARAMURTHY, Ellizabeth PEREPEZKO
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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: 20100160247Abstract: The present invention is directed to a process for preparing a 2,26,6-d4-morpholine derivative represented by Structural Formula (I): or a salt thereof.Type: ApplicationFiled: June 17, 2009Publication date: June 24, 2010Applicant: CoNCERT Pharmaceuticals, Inc.Inventors: Julie F. Liu, Xuejun Tang, Scott L. Harbeson, Craig E. Masse
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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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Patent number: 7700581Abstract: Disclosed herein are a cephalosporin compound of formula I, wherein R1 is selected from the following groups: wherein R2 is selected from the following groups: the preparation and uses thereof. A method of preparing the cephalosporin compound as disclosed herein comprises reacting a starting cephalosporin comprising a C7 amino group and a C3 thio-methyl moiety substituted with an N-containing heterocyclic group with bromoacetyl bromide and then with a N,N?-bissubstituted thiourea. Methods of treating an infectious disease are also disclosed, comprising administering to a patient in need thereof the pharmaceutical composition disclosed herein.Type: GrantFiled: January 31, 2007Date of Patent: April 20, 2010Assignee: Guangzhou Baiyunshan Pharmaceutical Co., Ltd.Inventors: Mao Chen, Shaoxuan Zhu, Xuebin Liu, Chun Luo, Shuwen Xu, Lizhen Zheng, Fang Ye, Chenglong Yi, Xiaona Zhang
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Publication number: 20090155387Abstract: A pharmaceutical composition comprising: at least one ?-lactam antibiotic and at least one ion-chelating agent; wherein when said pharmaceutical composition is used as an anti-microbial drug, it optionally comprises further at least one aminoglycoside antibiotic.Type: ApplicationFiled: February 24, 2009Publication date: June 18, 2009Inventor: Hesheng ZHANG
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Publication number: 20090156518Abstract: A pharmaceutical composition, comprising: at least one ?-lactam antibiotic and at least one buffer component; wherein when the pharmaceutical composition is used as an anti-microbial drug, it optionally comprises further at least one aminoglycoside antibiotic mixed with the ?-lactam antibiotic and the buffer component.Type: ApplicationFiled: February 24, 2009Publication date: June 18, 2009Inventor: Hesheng ZHANG
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Publication number: 20090148497Abstract: A method of treating or preventing infection at a surgical site comprising a bony defect and an implanted metal device is disclosed. Biodegradable microspheres are placed at the site and are capable of near-linear controlled release of an antibiotic agent for a predetermined period of time. The microspheres are configured to be large enough to avoid being phagocytosed and removed from the body, and small enough in diameter to not physically inhibit bone growth at said bony defect site. The microspheres are formed of polylactic-co-glycolic acid (PLGA), with or without polyethylene glycol (PEG), and sufficient antibiotic agent to produce bactericidal levels in body tissues. The microspheres exhibit near-linear delivery of the antibiotic agent for at least 4 weeks at levels exceeding the minimum inhibitory concentration (MIC) for organisms commonly found to be the cause of infections, and facilitate bone ingrowth or regrowth at the site.Type: ApplicationFiled: December 10, 2008Publication date: June 11, 2009Inventors: Catherine G. Ambrose, Terry A. Clyburn, Antonio G. Mikos
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Publication number: 20090075967Abstract: The present application describes deuterium-enriched ceftriaxone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 22, 2008Publication date: March 19, 2009Applicant: PROTIA, LLCInventor: Anthony W. Czarnik
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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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Patent number: 7485632Abstract: A compound of formula wherein the substituents have various meanings, useful as a pharmaceutical.Type: GrantFiled: July 14, 2003Date of Patent: February 3, 2009Assignee: Nabriva Therapeutics Forschungs GmbHInventors: Gerd Ascher, Werner Heilmayer, Michael Schranz, Josef Wieser
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Publication number: 20080312203Abstract: The present invention provides a compound of formula I wherein one of A and B is hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X is O, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof.Type: ApplicationFiled: August 21, 2008Publication date: December 18, 2008Applicant: WyethInventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Itsuki Yamamura, Tsuyoshi Takasaki, Atul Agarwal, Osvaldo Dos Santos, Fuk-Wah Sum, Yang-I Lin
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Publication number: 20080279929Abstract: The present invention provides a composition comprising a cefditoren, or a salt, derivative, prodrug, or other form thereof, for example, cefditoren pivoxil, useful in the treatment and prevention of infections and related conditions. The invention provides a composition which comprises nanoparticulate particles comprising the cefditoren, or a salt, derivative, prodrug, or other form thereof and at least one surface stabilizer. The nanoparticulate particles have an effective average particle size of less than about 2000 nm. The invention provides also a composition that delivers a cefditoren, or a salt, derivative, prodrug, or other form thereof, or nanoparticles comprising the same, in a pulsatile or continuous manner.Type: ApplicationFiled: February 5, 2007Publication date: November 13, 2008Applicant: Elan Corproation plcInventors: John G. Devane, Paul Stark, Nial M. N. Fanning, Gurvinder Singh Rekhi, Scott A. Jenkins, Gary Liversidge
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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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Patent number: 7341993Abstract: This invention provides cross-linked glycopeptide-cephalosporin compounds and pharmaceutically acceptable salts thereof which are useful as antibiotics. This invention also provides pharmaceutical compositions containing such compounds; methods for treating bacterial infections in a mammal using such compounds; and processes and intermediates useful for preparing such compounds.Type: GrantFiled: June 30, 2005Date of Patent: March 11, 2008Assignee: Theravance, Inc.Inventors: Paul R. Fatheree, Martin S. Linsell, Daniel D. Long, Daniel Marquess, Edmund J. Moran, Matthew B. Nodwell, S. Derek Turner, James Aggen
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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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Publication number: 20040023943Abstract: 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: ApplicationFiled: January 29, 2003Publication date: February 5, 2004Inventors: Tomoyasu Ishikawa, Shohei Hashiguchi, Yuji Iizawa
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Patent number: 6599892Abstract: Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of &bgr;-lactamase enzymes.Type: GrantFiled: July 30, 2001Date of Patent: July 29, 2003Assignee: Research Corporation Technologies, Inc.Inventors: John D. Buynak, Brian Bachmann
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Patent number: 6599893Abstract: The present invention relates to chemical compounds having the formula: or a pharmaceutically acceptable salt thereof. R1 is selected from the group consisting of: R2 is selected from the group consisting of hydrogen, CH3—, FCH2—, F2CH— R3 is selected from the group consisting of: X is selected from the group consisting of hydrogen, halogen, cyano, —NH2, —N(CH3)2, —HSO2NH2, —SO2NH2 and —SCH3. The subscript n is 0 or 1.Type: GrantFiled: August 8, 2001Date of Patent: July 29, 2003Assignee: Essential Therapeutics, Inc.Inventor: Tomasz W. Glinka
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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: 6486149Abstract: Processes are provided for the preparation of orally administrable, yellow and powdery compositions essentially consisting of particles composed of a homogeneous mixture of an amorphous Cefditoren pivoxil substance with a water soluble high-molecular additive. These compositions can be produced by dissolving crystalline Cefditoren pivoxil substance and the water-soluble high-molecular additive in an aqueous solution of an acid, then neutralizing the resultant solution, to co-precipitate the product, and drying the thus precipitated product, followed by recovering the product in the form of the above-mentioned particles.Type: GrantFiled: November 26, 2001Date of Patent: November 26, 2002Assignee: Meiji Seika Kaisha Ltd.Inventors: Masahiro Onodera, Masamichi Sukegawa, Kiyoshi Yasui, Tatsuo Watanabe, Toyomi Sato, Yasushi Murai, Katsuharu Iinuma
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Patent number: 6440957Abstract: A compound useful as an anti-bacterial agent, having the formula wherein R2 together with the nitrogen atom to which it is attached forms a cyclic aminoguanidine group or derivative thereof as definedType: GrantFiled: September 21, 2000Date of Patent: August 27, 2002Assignee: Biochemie Gesellschaft m.b.H.Inventors: Gerd Ascher, Werner Heilmayer, Johannes Ludescher, Johannes Hildebrandt, Michael Schranz, Josef Wieser
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Publication number: 20020115852Abstract: A compound of formula 1Type: ApplicationFiled: November 13, 2001Publication date: August 22, 2002Inventors: Gerd Ascher, Josef Wieser, Michael Schranz, Johannes Ludescher, Johannes Hildebrandt
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Publication number: 20020082248Abstract: Process for preparing ceftiofur having formula 1: 1Type: ApplicationFiled: November 20, 2001Publication date: June 27, 2002Inventors: Andreas Berger, Martin Decristoforo, Johannes Ludescher, Herbert Schleich
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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: 20020068065Abstract: A composition comprising:Type: ApplicationFiled: September 7, 2001Publication date: June 6, 2002Inventors: Ondrej Hendl, Nancy J. Britten
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Publication number: 20020037322Abstract: Processes are provided for the preparation of orally administrable, yellow and powdery compositions essentially consisting of particles composed of a homogeneous mixture of an amorphous Cefditoren pivoxil substance with a water soluble high-molecular additive. These compositions can be produced by dissolving crystalline Cefditoren pivoxil substance and the water-soluble high-molecular additive in an aqueous solution of an acid, then neutralizing the resultant solution, to co-precipitate the product, and drying the thus precipitated product, followed by recovering the product in the form of the above-mentioned particles.Type: ApplicationFiled: November 26, 2001Publication date: March 28, 2002Inventors: Masahiro Onodera, Masamichi Sukegawa, Kiyoshi Yasui, Tatsuo Watanabe, Toyomi Sato, Yasushi Murai, Katsuharu Iinuma
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Publication number: 20010056089Abstract: A novel crystal of 7&bgr;-[2-(2-aminothiazol-4-yl)-2-(Z)-(hydroxyimino)acetamido]-3-[pyrazol-4-yl)methylthio]3-cephem-4-carboxylic acid or a salt thereof.Type: ApplicationFiled: July 18, 2001Publication date: December 27, 2001Applicant: FUJISAWA PHARMACEUTICAL CO., LTD.Inventors: Kohji Kawabata, Takeshi Terasawa, Ayako Ohki, Fumiyuki Shirai, Hirofumi Yamamoto, Ryoichi Kawakami, Chiaki Hamaguchi
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Patent number: 6303592Abstract: Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of &bgr;-lactamase enzymes.Type: GrantFiled: March 14, 1997Date of Patent: October 16, 2001Assignee: Research Corporation Technologies, Inc.Inventors: John D. Buynak, Brian Bachmann
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Publication number: 20010016581Abstract: Process of depleting 7-amino-3-[(E)-2-(4-methyl-5-thiazolyl)vinyl]-3-cephem-4-carboxylic acid in Z/E mixtures of 7-amino-3-[2-(4-methyl-5-thiazolyl)vinyl]-3-cephem-4-carboxylic acidType: ApplicationFiled: January 23, 2001Publication date: August 23, 2001Inventors: Johannes Ludescher, Harald Summer, Siegfried Wolf
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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: 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: 6150350Abstract: The invention relates to antimicrobial compositions comprising a combination of (1) a therapeutically effective amount of a compound of formula I ##STR1## with (2) a second ingredient selected from carbapenem antibiotics or with .beta.-lactamase inhibitors, to the use of the compositions for producing a medicament for the treatment and prophylaxis of infectious diseases, including MRSA infections, and to pharmaceutical compositions containing the combination.Type: GrantFiled: August 24, 1998Date of Patent: November 21, 2000Assignee: Hoffman-la Roche Inc.Inventors: Peter Angehrn, Ingrid Heinze-Krauss, Malcolm Page, Hans G. F. Richter
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Patent number: 6133254Abstract: Use of a compound of formula (I) wherein R represents hydrogen or chlorine, for preparing an immunosuppressive medicament.Type: GrantFiled: October 26, 1998Date of Patent: October 17, 2000Assignee: Gruppo Lepetit, S.p.A.Inventor: Khalid Islam
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Patent number: 6090801Abstract: Pharmaceutical formulations comprising ceftriaxone in combination with a penem of formula (I) in which R.sup.1 is hydrogen or an organic group; R.sup.2 is a ring system of formula (II), wherein R.sup.4 and R.sup.5 are hydrogen or one or more substituents; m is 2 or 3; p is 0, 1 or 2; R.sup.3 is hydrogen, a pharmaceutically acceptable salt-forming cation or a pharmaceutically acceptable in-vivo hydrolysable ester-forming group; and with a pharmaceutically acceptable carrier. The formulations have antibacterial activity, the compound of formula (I) acting as a .beta.-lactamase inhibitor.Type: GrantFiled: February 14, 1997Date of Patent: July 18, 2000Assignee: SmithKline Beecham p.l.c.Inventors: Kenneth Coleman, Jane Elizabeth Neale
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Patent number: 6087355Abstract: The present invention includes novel compounds of formula ##STR1## where A, B, D, and E are selected from the group consisting of carbon, nitrogen and sulfur, 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 NR.sup.13 R.sup.14, ##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: July 11, 2000Assignee: Microcide Pharmaceuticals, Inc.Inventors: In-Seop Cho, Scott J. Hecker, Tomasz W. Glinka, Ving J. Lee, Zhijia J. Zhang
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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
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Patent number: 6063778Abstract: The invention provides novel cephalosporin derivatives of the formula (I) ##STR1## and salts thereof for use in pharmaceutical compositions. Also novel precursors for synthesis of the cephalosporins are disclosed.Type: GrantFiled: June 26, 1998Date of Patent: May 16, 2000Assignee: Il-Dong Pharm. Co., Ltd.Inventors: Kee-Won Kim, Jae-Hoon Kang, Dong-Sik Yu, Moo-Soo Jang, Seung-Woo Yu
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Patent number: 6030965Abstract: The present invention includes novel compounds of formula where A, B, D, and E are selected from the group consisting of carbon, nitrogen and sulfur, R.sup.99 is selected from the group consisting of sulfur, SO, S0.sub.2, NH, N-alkyl, oxygen, C.dbd.C (cis or trans), and C.tbd.C, and R.sup.12 is NR.sup.13 R.sup.14, ##STR1## 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: September 30, 1997Date of Patent: February 29, 2000Assignee: Microcide Pharmaceuticals, Inc.Inventors: In-Seop Cho, Scott J. Hecker, Tomasz W. Glinka, Ving J. Lee, Zhijia J. Zhang
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Patent number: 6025352Abstract: The present invention includes novel compounds of formula ##STR1## where G, H, J, L and M are carbon or nitrogen, R.sup.99 is selected from the group consisting of sulfur, SO, SO.sub.2, NH, N-alkyl, oxygen, C.tbd.C (cis or trans), and C.tbd.C, and R.sup.12 is NR.sup.13 R.sup.14, ##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: September 29, 1997Date of Patent: February 15, 2000Assignee: Microcide Pharmaceuticals, Inc.Inventors: In-Seop Cho, Scott J. Hecker, Tomasz W. Glinka, Ving J. Lee, Zhijia J. Zhang
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Patent number: 5994340Abstract: New 2-oxo-1-azetidine sulfonic acid derivatives with an aminoalkyl substituted "anti" (E-isomer) oxyimino group in the acylamino substituent at the 3 position of the monobactam ring. These compounds are potent inhibitors of bacterial .beta.-lactamases. These compounds can be used in combination with .beta.-lactam antibiotics to increase the effectiveness of the .beta.-lactam antibiotics in fighting infection caused by .beta.-lactamase producing bacteria.Type: GrantFiled: August 29, 1997Date of Patent: November 30, 1999Assignee: SynPhar Laboratories, Inc.Inventors: Samarendra N. Maiti, Oludotun A. Phillips, Eduardo L. Setti, Andhe V. Narender Reddy, Ronald G. Micetich, Fusahiro Higashitani, Chieko Kunugita, Koichi Nishida, Tatsuya Uji
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Patent number: 5958915Abstract: A new, antibacterial composition for use in oral administration is now provided, which composition comprises a mixture of Cefditoren pivoxyl with a water soluble casein salt. This composition has a reduced bitter taste of Cefditoren pivoxyl and also has improved properties regarding the rate and concentration of dissolution of Cefditoren pivoxyl in water and a ratio of dissolution out of Cefditoren pivoxyl into water. This composition further can attain a high absorbability of the Cefditoren component at the digestive tubes upon oral administration thereof. In this composition, the ratio (by weight) of Cefditoren pivoxyl to the casein salt added may preferably be in a range of 1:0.1 to 1:4. By further addition of a water-soluble polyphosphoric acid salt to the composition, the composition can prevent a ratio of dissolution out into water of the Cefditoren pivoxyl component being decreased when the composition was stored under severe conditions.Type: GrantFiled: April 8, 1998Date of Patent: September 28, 1999Assignee: Meiji Seika Kaisha, Ltd.Inventors: Kenichi Abe, Masato Ota, Hiroyuki Yamaguchi, Chikako Murakami, Toshihiro Kikkoji
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Patent number: 5958914Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is amino, R.sup.2 is hydrogen,R.sup.3 is carboxy,R.sup.4 is heterocyclic(lower)alkylthio wherein said heterocyclic group is pyrazolyl and said lower alkyl group is methyl, andR.sup.5 is halogen; and pharmaceutically acceptable salts thereof.Type: GrantFiled: March 26, 1998Date of Patent: September 28, 1999Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kohji Kawabata, Hirofumi Yamamoto, Yoshiteru Eikyu, Shinya Okuda, Hisashi Takasugi
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Patent number: 5827845Abstract: A cephalosporin derivative which has a substituted or unsubstituted 2-(5-thiazolyl)vinyl group at the 3-position and is represented by the following formula (I) ##STR1## wherein X is CH or N, R.sup.1 is an amino group or a protected amino group, R.sup.2 is a hydrogen atom or a hydroxyimino-protecting group, R.sup.3 is a hydrogen atom, a salt-forming cation or a carboxyl-protecting group, R.sup.4 is a hydrogen atom, and R.sup.5 is a hydrogen atom, a lower alkyl group, a halo-(lower)alkyl group or a halogen atom, is now synthetised as a cephem compound which exhibits excellent antibacterial activities and is useful as a therapeutic agent for various bacterial infections.Type: GrantFiled: July 31, 1996Date of Patent: October 27, 1998Assignee: Meiji Seika Kaisha, Ltd.Inventors: Sohjiro Shiokawa, Kunio Atsumi, Katsuyoshi Iwamatsu, Atsushi Tamura, Seiji Shibahara
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Patent number: 5804577Abstract: The present invention relates to compounds of formula I ##STR1## wherein R.sup.1 is a group selected from 2-, 3-, and 4-hydroxyphenyl, 3-nitrophenyl, and 3-fluoro-4-hydroxyphenyl; as well as readily hydroyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts.Type: GrantFiled: August 27, 1996Date of Patent: September 8, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Paul Hebeisen, Ingrid Heinze-Krauss, Hans Richter, Valeri Runtz, Henri Stalder, Urs Weiss, George Petros Yiannikouros
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Patent number: 5789584Abstract: The present invention includes (7R)-7-(acylamino)-3-(substituted-pyridinyl)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against methicillin-resistant bacteria and are therefore useful as antibacterial agents.Type: GrantFiled: March 29, 1995Date of Patent: August 4, 1998Assignee: Microcide Pharmaceuticals, Inc.Inventors: Burton G. Christensen, In-Seop Cho, Tomasz W. Glinka, Scott J. Hecker
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Patent number: 5736151Abstract: The present invention provides for the inclusion of small amounts of water in oil suspensions of active drugs, such as ceftiofur hydrochloride of formula I. The resulting suspensions have improved resuspendability. Improved resuspendability results in an improved product because less shaking of the suspension is required before dosing.Type: GrantFiled: December 9, 1996Date of Patent: April 7, 1998Assignee: Pharmacia & Upjohn CompanyInventors: Todd P. Foster, David L. Kiefer
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Patent number: RE35754Abstract: Cephem derivatives of the general formula ##STR1## is which the R.sub.2 O group is in the syn-position, a process for their manufacture and pharmaceutical formulations which are active against bacterial infections and contain these compounds.Type: GrantFiled: July 11, 1990Date of Patent: March 24, 1998Assignee: Hoechst AktiengesellschaftInventors: Walter Durckheimer, Dieter Bormann, Eberhard Ehlers, Elmar Schrinner, Rene Heymes