7-position Substituent Contains Hetero Ring Patents (Class 514/206)
  • Publication number: 20100222289
    Abstract: 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: Application
    Filed: October 22, 2008
    Publication date: September 2, 2010
    Applicant: CFS Research LLC
    Inventor: Albert Martin Lerner
  • Publication number: 20100215716
    Abstract: 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: Application
    Filed: February 23, 2010
    Publication date: August 26, 2010
    Applicant: Biomet Manufacturing Corp.
    Inventors: Karen S. TROXEL, Sona SUNDARAMURTHY, Ellizabeth PEREPEZKO
  • Patent number: 7754707
    Abstract: 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: Grant
    Filed: June 30, 2004
    Date of Patent: July 13, 2010
    Assignee: R.E.D. Laboratories, N.V./S.A.
    Inventors: Karim El Bakkouri, Patrick Englebienne, Kenny De Meirleir, Charles Vincent Herst
  • Publication number: 20100160247
    Abstract: 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: Application
    Filed: June 17, 2009
    Publication date: June 24, 2010
    Applicant: CoNCERT Pharmaceuticals, Inc.
    Inventors: Julie F. Liu, Xuejun Tang, Scott L. Harbeson, Craig E. Masse
  • Patent number: 7723389
    Abstract: 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: Grant
    Filed: November 4, 2002
    Date of Patent: May 25, 2010
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Leonard A. Herzenberg, Leonore A. Herzenberg, Stephen C. De Rosa, James Andrus
  • Patent number: 7700581
    Abstract: 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: Grant
    Filed: January 31, 2007
    Date of Patent: April 20, 2010
    Assignee: Guangzhou Baiyunshan Pharmaceutical Co., Ltd.
    Inventors: Mao Chen, Shaoxuan Zhu, Xuebin Liu, Chun Luo, Shuwen Xu, Lizhen Zheng, Fang Ye, Chenglong Yi, Xiaona Zhang
  • Publication number: 20090155387
    Abstract: 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: Application
    Filed: February 24, 2009
    Publication date: June 18, 2009
    Inventor: Hesheng ZHANG
  • Publication number: 20090156518
    Abstract: 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: Application
    Filed: February 24, 2009
    Publication date: June 18, 2009
    Inventor: Hesheng ZHANG
  • Publication number: 20090148497
    Abstract: 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: Application
    Filed: December 10, 2008
    Publication date: June 11, 2009
    Inventors: Catherine G. Ambrose, Terry A. Clyburn, Antonio G. Mikos
  • Publication number: 20090075967
    Abstract: The present application describes deuterium-enriched ceftriaxone, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.
    Type: Application
    Filed: August 22, 2008
    Publication date: March 19, 2009
    Applicant: PROTIA, LLC
    Inventor: Anthony W. Czarnik
  • Patent number: 7488724
    Abstract: 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: Grant
    Filed: May 10, 2005
    Date of Patent: February 10, 2009
    Assignee: Southern Methodist University Foundation for Research
    Inventors: John D. Buynak, Lakshminarayana Vogeti
  • Patent number: 7485632
    Abstract: A compound of formula wherein the substituents have various meanings, useful as a pharmaceutical.
    Type: Grant
    Filed: July 14, 2003
    Date of Patent: February 3, 2009
    Assignee: Nabriva Therapeutics Forschungs GmbH
    Inventors: Gerd Ascher, Werner Heilmayer, Michael Schranz, Josef Wieser
  • Publication number: 20080312203
    Abstract: 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: Application
    Filed: August 21, 2008
    Publication date: December 18, 2008
    Applicant: Wyeth
    Inventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Itsuki Yamamura, Tsuyoshi Takasaki, Atul Agarwal, Osvaldo Dos Santos, Fuk-Wah Sum, Yang-I Lin
  • Publication number: 20080279929
    Abstract: 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: Application
    Filed: February 5, 2007
    Publication date: November 13, 2008
    Applicant: Elan Corproation plc
    Inventors: John G. Devane, Paul Stark, Nial M. N. Fanning, Gurvinder Singh Rekhi, Scott A. Jenkins, Gary Liversidge
  • Patent number: 7384928
    Abstract: 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: Grant
    Filed: March 18, 2003
    Date of Patent: June 10, 2008
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yasuhiro Nishitani, Yoshinori Yamano
  • Patent number: 7341993
    Abstract: 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: Grant
    Filed: June 30, 2005
    Date of Patent: March 11, 2008
    Assignee: 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
  • Patent number: 6916801
    Abstract: 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: Grant
    Filed: July 24, 2002
    Date of Patent: July 12, 2005
    Assignee: Alamx, LLC
    Inventors: John D. Buynak, Lakshminarayana Vogeti
  • Publication number: 20040023943
    Abstract: 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: Application
    Filed: January 29, 2003
    Publication date: February 5, 2004
    Inventors: Tomoyasu Ishikawa, Shohei Hashiguchi, Yuji Iizawa
  • Patent number: 6599892
    Abstract: Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of &bgr;-lactamase enzymes.
    Type: Grant
    Filed: July 30, 2001
    Date of Patent: July 29, 2003
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Brian Bachmann
  • Patent number: 6599893
    Abstract: 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: Grant
    Filed: August 8, 2001
    Date of Patent: July 29, 2003
    Assignee: Essential Therapeutics, Inc.
    Inventor: Tomasz W. Glinka
  • Patent number: 6531465
    Abstract: 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: Grant
    Filed: May 21, 2001
    Date of Patent: March 11, 2003
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Gerd Ascher, Johannes Ludescher
  • Patent number: 6486149
    Abstract: 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: Grant
    Filed: November 26, 2001
    Date of Patent: November 26, 2002
    Assignee: Meiji Seika Kaisha Ltd.
    Inventors: Masahiro Onodera, Masamichi Sukegawa, Kiyoshi Yasui, Tatsuo Watanabe, Toyomi Sato, Yasushi Murai, Katsuharu Iinuma
  • Patent number: 6440957
    Abstract: 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 defined
    Type: Grant
    Filed: September 21, 2000
    Date of Patent: August 27, 2002
    Assignee: Biochemie Gesellschaft m.b.H.
    Inventors: Gerd Ascher, Werner Heilmayer, Johannes Ludescher, Johannes Hildebrandt, Michael Schranz, Josef Wieser
  • Publication number: 20020115852
    Abstract: A compound of formula 1
    Type: Application
    Filed: November 13, 2001
    Publication date: August 22, 2002
    Inventors: Gerd Ascher, Josef Wieser, Michael Schranz, Johannes Ludescher, Johannes Hildebrandt
  • Publication number: 20020082248
    Abstract: Process for preparing ceftiofur having formula 1: 1
    Type: Application
    Filed: November 20, 2001
    Publication date: June 27, 2002
    Inventors: Andreas Berger, Martin Decristoforo, Johannes Ludescher, Herbert Schleich
  • Patent number: 6407091
    Abstract: 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: Grant
    Filed: April 13, 2000
    Date of Patent: June 18, 2002
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, A. Srinivasa Rao, Greg C. Adam, Sirishkumar D. Nidamarthy, Venkata Ramana Doppalapudi
  • Publication number: 20020068065
    Abstract: A composition comprising:
    Type: Application
    Filed: September 7, 2001
    Publication date: June 6, 2002
    Inventors: Ondrej Hendl, Nancy J. Britten
  • Publication number: 20020037322
    Abstract: 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: Application
    Filed: November 26, 2001
    Publication date: March 28, 2002
    Inventors: Masahiro Onodera, Masamichi Sukegawa, Kiyoshi Yasui, Tatsuo Watanabe, Toyomi Sato, Yasushi Murai, Katsuharu Iinuma
  • Publication number: 20010056089
    Abstract: 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: Application
    Filed: July 18, 2001
    Publication date: December 27, 2001
    Applicant: FUJISAWA PHARMACEUTICAL CO., LTD.
    Inventors: Kohji Kawabata, Takeshi Terasawa, Ayako Ohki, Fumiyuki Shirai, Hirofumi Yamamoto, Ryoichi Kawakami, Chiaki Hamaguchi
  • Patent number: 6303592
    Abstract: Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of &bgr;-lactamase enzymes.
    Type: Grant
    Filed: March 14, 1997
    Date of Patent: October 16, 2001
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Brian Bachmann
  • Publication number: 20010016581
    Abstract: 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 acid
    Type: Application
    Filed: January 23, 2001
    Publication date: August 23, 2001
    Inventors: Johannes Ludescher, Harald Summer, Siegfried Wolf
  • Publication number: 20010011085
    Abstract: 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: Application
    Filed: August 14, 1997
    Publication date: August 2, 2001
    Inventors: MARCO ALPEGIANI, PIERLUIGI BISSOLINO, MASSIMILIANO PALLADINO, ETTORE PERRONE
  • Patent number: 6159961
    Abstract: 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: Grant
    Filed: July 19, 1999
    Date of Patent: December 12, 2000
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kohji Kawabata, Hirofumi Yamamoto, Yoshiteru Eikyu, Shinya Okuda, Hisashi Takasugi
  • Patent number: 6159706
    Abstract: 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: Grant
    Filed: December 18, 1998
    Date of Patent: December 12, 2000
    Assignee: NewBiotics, Inc.
    Inventor: H. Michael Shepard
  • Patent number: 6150350
    Abstract: 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: Grant
    Filed: August 24, 1998
    Date of Patent: November 21, 2000
    Assignee: Hoffman-la Roche Inc.
    Inventors: Peter Angehrn, Ingrid Heinze-Krauss, Malcolm Page, Hans G. F. Richter
  • Patent number: 6133254
    Abstract: Use of a compound of formula (I) wherein R represents hydrogen or chlorine, for preparing an immunosuppressive medicament.
    Type: Grant
    Filed: October 26, 1998
    Date of Patent: October 17, 2000
    Assignee: Gruppo Lepetit, S.p.A.
    Inventor: Khalid Islam
  • Patent number: 6090801
    Abstract: 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: Grant
    Filed: February 14, 1997
    Date of Patent: July 18, 2000
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Kenneth Coleman, Jane Elizabeth Neale
  • Patent number: 6087355
    Abstract: 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: Grant
    Filed: October 11, 1996
    Date of Patent: July 11, 2000
    Assignee: Microcide Pharmaceuticals, Inc.
    Inventors: In-Seop Cho, Scott J. Hecker, Tomasz W. Glinka, Ving J. Lee, Zhijia J. Zhang
  • Patent number: 6066630
    Abstract: 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: Grant
    Filed: October 11, 1996
    Date of Patent: May 23, 2000
    Assignee: Microcide Pharmaceuticals, Inc.
    Inventors: In-Seop Cho, Scott J. Hecker, Tomaz W. Glinka, Ving J. Lee, Zhijia J. Zhang
  • Patent number: 6063778
    Abstract: 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: Grant
    Filed: June 26, 1998
    Date of Patent: May 16, 2000
    Assignee: Il-Dong Pharm. Co., Ltd.
    Inventors: Kee-Won Kim, Jae-Hoon Kang, Dong-Sik Yu, Moo-Soo Jang, Seung-Woo Yu
  • Patent number: 6030965
    Abstract: 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: Grant
    Filed: September 30, 1997
    Date of Patent: February 29, 2000
    Assignee: Microcide Pharmaceuticals, Inc.
    Inventors: In-Seop Cho, Scott J. Hecker, Tomasz W. Glinka, Ving J. Lee, Zhijia J. Zhang
  • Patent number: 6025352
    Abstract: 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: Grant
    Filed: September 29, 1997
    Date of Patent: February 15, 2000
    Assignee: Microcide Pharmaceuticals, Inc.
    Inventors: In-Seop Cho, Scott J. Hecker, Tomasz W. Glinka, Ving J. Lee, Zhijia J. Zhang
  • Patent number: 5994340
    Abstract: 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: Grant
    Filed: August 29, 1997
    Date of Patent: November 30, 1999
    Assignee: 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
  • Patent number: 5958915
    Abstract: 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: Grant
    Filed: April 8, 1998
    Date of Patent: September 28, 1999
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Kenichi Abe, Masato Ota, Hiroyuki Yamaguchi, Chikako Murakami, Toshihiro Kikkoji
  • Patent number: 5958914
    Abstract: 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: Grant
    Filed: March 26, 1998
    Date of Patent: September 28, 1999
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Kohji Kawabata, Hirofumi Yamamoto, Yoshiteru Eikyu, Shinya Okuda, Hisashi Takasugi
  • Patent number: 5827845
    Abstract: 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: Grant
    Filed: July 31, 1996
    Date of Patent: October 27, 1998
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Sohjiro Shiokawa, Kunio Atsumi, Katsuyoshi Iwamatsu, Atsushi Tamura, Seiji Shibahara
  • Patent number: 5804577
    Abstract: 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: Grant
    Filed: August 27, 1996
    Date of Patent: September 8, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Paul Hebeisen, Ingrid Heinze-Krauss, Hans Richter, Valeri Runtz, Henri Stalder, Urs Weiss, George Petros Yiannikouros
  • Patent number: 5789584
    Abstract: 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: Grant
    Filed: March 29, 1995
    Date of Patent: August 4, 1998
    Assignee: Microcide Pharmaceuticals, Inc.
    Inventors: Burton G. Christensen, In-Seop Cho, Tomasz W. Glinka, Scott J. Hecker
  • Patent number: 5736151
    Abstract: 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: Grant
    Filed: December 9, 1996
    Date of Patent: April 7, 1998
    Assignee: Pharmacia & Upjohn Company
    Inventors: Todd P. Foster, David L. Kiefer
  • Patent number: RE35754
    Abstract: 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: Grant
    Filed: July 11, 1990
    Date of Patent: March 24, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Walter Durckheimer, Dieter Bormann, Eberhard Ehlers, Elmar Schrinner, Rene Heymes