3-position Substituent Contains Sulfur Patents (Class 514/204)
  • Patent number: 10092247
    Abstract: Embodiments include a system for determining cardiovascular information for a patient with coronary artery disease. The system may include at least one computer system configured to receive patient-specific data regarding a geometry of the patient's heart and create a model representing at least a portion of the patient's heart based on the patient-specific data. The at least one computer system may be further configured to create, for a given level of physical activity, a physics-based model of blood flow through the patient's heart simulated during a selected level of physical activity; determine and normalize one or more values of at least one blood flow characteristic within the patient's heart during the simulated level of physical activity; and compare the one or more normalized values of the at least one blood flow characteristic to a threshold to determine whether the level of physical activity exceeds an acceptable level of risk.
    Type: Grant
    Filed: September 25, 2014
    Date of Patent: October 9, 2018
    Assignee: HeartFlow, Inc.
    Inventor: Charles A. Taylor
  • Patent number: 9834567
    Abstract: A novel crystalline form is defined by diffraction angle 2?° of X-ray powder diffraction pattern and characteristic peak of differential scanning calorimetry (DSC). The novel crystalline form of Cefamandole Nafate is prepared as follows: adding Cefamandole Nafate in solid state to an organic solvent to form a suspension with a concentration of 0.04˜0.3 g/ml, stirring the suspension at 40˜50° C. for a period of time, and then cooling to 5˜15° C. at certain cooling rate, continuing to stir for a period of time, then suction filtrating the obtained suspension, the resulting filer cake is Cefamandole Nafate as wet product, which is dried to constant weight to provide the novel crystalline form of Cefamandole Nafate as final product.
    Type: Grant
    Filed: August 25, 2017
    Date of Patent: December 5, 2017
    Assignees: TIANJIN UNIVERSITY, HAINAN LINGKANG PHARMACEUTICAL CO., LTD
    Inventors: Hongxun Hao, Linggang Tao, Fang He, Baohong Hou, Jingkang Wang, Jun Lv, Qiuxiang Yin, Yongli Wang, Junbo Gong, Chuang Xie, Ying Bao
  • Patent number: 9668700
    Abstract: Embodiments include a system for determining cardiovascular information for a patient with coronary artery disease. The system may include at least one computer system configured to receive patient-specific data regarding a geometry of the patient's heart and create a model representing at least a portion of the patient's heart based on the patient-specific data. The at least one computer system may be further configured to create, for a given level of physical activity, a physics-based model of blood flow through the patient's heart simulated during a selected level of physical activity; determine and normalize one or more values of at least one blood flow characteristic within the patient's heart during the simulated level of physical activity; and compare the one or more normalized values of the at least one blood flow characteristic to a threshold to determine whether the level of physical activity exceeds an acceptable level of risk.
    Type: Grant
    Filed: September 9, 2014
    Date of Patent: June 6, 2017
    Assignee: HeartFlow, Inc.
    Inventor: Charles A. Taylor
  • Publication number: 20150017099
    Abstract: The invention provides methods and compositions for the diagnosis, prognosis and treatment of respiratory tract diseases. Specifically, the invention provides diagnosis, prognosis and treatment of respiratory infections using bitter and sweet taste signal transduction pathways. In one aspect, the invention relates to a method for treating a respiratory infection by administering a composition to the respiratory tract of a subject in an amount capable of activating bitter taste signaling and/or inhibiting sweet taste signaling. The composition comprises at least a bitter receptor agonist and, optionally, a pharmaceutically acceptable carrier for delivering the composition to the respiratory tract. In another aspect, the invention relates to a composition for treatment of a respiratory infection. Such composition comprises at least a bitter receptor agonist and, optionally, a pharmaceutically acceptable carrier for delivering the composition to the respiratory tract.
    Type: Application
    Filed: January 25, 2013
    Publication date: January 15, 2015
    Inventors: Noam A. Cohen, Robert J. Lee, Danielle R. Reed
  • Patent number: 8809314
    Abstract: The cephalosporin compound of formula (I) is disclosed, which exhibits antibiotic activity against Gram-negative (e.g., Pseudomonas aeruginosa) and Gram-positive (e.g., methicillin-resistant Staphylococcus aureus) bacteria. Methods of manufacturing the compound of formula (I), and uses of the compound in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.
    Type: Grant
    Filed: September 6, 2013
    Date of Patent: August 19, 2014
    Assignee: Cubist Pharmacueticals, Inc.
    Inventors: Yong He, Yu Gui Gu, Ning Yin, Dong Zou, Andre Lee Pearson
  • Publication number: 20140128359
    Abstract: The invention relates to N-heterocyclic substituent-containing antibiotics, their preparation, and their use. Disclosed are sodium and potassium salts of 7-(?-((N,N?-diisopropylamidino)thio)acetylamino)-3-(((1,2,5,6-tetrahydro-2-methyl-5,6-diox o-1,2,4-triazin-3-yl)thio)methyl) cephalosporanic acid as presented by the general structure (I), their preparation, and their use. The antibiotics of the invention can be used to treat diseases caused by Gram-positive or Gram-negative bacteria such as septicaemia, gastrointestinal tract infection, and urinary tract infection. They have increased half-life in blood and lowered toxicity. They can reduce the frequency of drug use and lower medical treatment costs. They have improved stability and can be stored at ambient temperatures. The method of the invention is simple, and it produces high purity products which can meet the requirements of clinical use.
    Type: Application
    Filed: November 2, 2012
    Publication date: May 8, 2014
    Applicants: GUANGZHOU PHARMACEUTICAL INDUSTRIAL RESEARCH INSTI, GUANGZHOU BAIYUNSHAN PHARMACEUTICAL CO., LTD. GUANGZHOU BAIYUNSHAN PHARMACEUTICAL FACTORY
    Inventors: Mao Chen, Shaoxuan Zhu, Xuebin Liu, Lizhen Zheng, Liwei Lin, Shuwen Xu, Yuping Wang, Wei Yang, Yunfeng Li, Fang Ye, Xiaona Zhang
  • Publication number: 20140088069
    Abstract: An antibacterial composition is provided including a combination of a ?-lactam antibiotic that has a binding affinity for bacterial penicillin-binding protein 2; and a non-antibiotic compound which may be a thienopyridine or a non-thienopyridine compound. A method of treatment using the composition is also provided.
    Type: Application
    Filed: November 29, 2013
    Publication date: March 27, 2014
    Inventors: Eric D. Brown, Maya Farha, Alexander Leung, Gerry Wright, Kalinka Koteva, Ted Sewell, Linda Ejim
  • Publication number: 20110294774
    Abstract: 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: Application
    Filed: May 6, 2011
    Publication date: December 1, 2011
    Applicant: TRIUS THERAPEUTICS
    Inventors: Vickie Brown-Driver, Kedar GC, John M. Finn, Robert Haselbeck, Mark Hilgers, Karen Shaw, Mark Stidham
  • Publication number: 20100285012
    Abstract: 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: Application
    Filed: January 5, 2009
    Publication date: November 11, 2010
    Applicant: University of FLorida Research Foundation Inc.
    Inventors: William A. Dunn, JR., Debra E. Akin, Ann Progulske-Fox, David A. Ostrov
  • 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
  • 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: 20100048528
    Abstract: 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: Application
    Filed: November 2, 2009
    Publication date: February 25, 2010
    Applicant: Novexel
    Inventors: Jozsef Aszodi, Claude Fromentin, Maxime Lampilas, David Alan Rowlands
  • 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
  • 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: 20080182836
    Abstract: Disclosed herein are a cephalosporin compound comprising a C3 thio-methyl moiety substituted with an N-containing heterocyclic group, and a C7 thiourea acetamido group, 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: Application
    Filed: January 31, 2007
    Publication date: July 31, 2008
    Inventors: Mao Chen, Shaoxuan Zhu, Xuebin Liu, Chun Luo, Shuwen Xu, Lizhen Zheng, Fang Ye, Chenglong Yi, Xiaona Zhang
  • Publication number: 20080069870
    Abstract: The invention relates to a controlled release composition comprising a cephalosporin that in operation delivers the drug in a pulsed or bimodal manner for the treatment of bacterial infection. The controlled release composition comprises an immediate release component and a modified release component; the immediate release component comprising a first population of cephalosporin-containing particles and the modified release component comprising a second population of cephalosporin-containing particles coated with a controlled release coating; wherein the combination of the immediate release and modified release components in operation deliver the active ingredient in a pulsed or bi-modal manner. Preferably, the cephalosporin is cefcapene pivoxil or a salt thereof which can be released from the dosage form in an erodable, diffusion and/or osmotic-controlled release profile.
    Type: Application
    Filed: April 12, 2006
    Publication date: March 20, 2008
    Applicant: Elan Corporation Pic
    Inventors: Scott A. Jenkins, Gary Liversidge
  • 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
  • Patent number: 6846492
    Abstract: The use of compounds of formula (1) is described, in which compounds R1, R2 and R3 are each independently of the others hydrogen; C1-C20alkyl; C3-C7cycloalkyl; C2-C20alkenyl; C4-C7cycloalkenyl; C2-C20alkynyl, C4-C7cycloalkynyl; or unsubstituted or C1-C5alkyl-, C3-C7cylcoalkyl-, C1-C5alkoxyl-, C3-C7cycloakoxy-, halo-, oxo-, carboxy-, carboxy-C1-C7alkyl ester-, carboxy-C3-C7cylcloalkyl ester-, cyano-, trifluoromethyl-, pentafluoroethyl-, amino-, N,N-mono- or di-C1-C20alkylamino- or nitro-substituted phenyl-C1-C5alkyl, naphthyl-C1-C5alkyl, phenylcarbonyl-C1-C5alkyl, naphthylcarbonyl-C1-C5alkyl, pyrrolylalkyl, furanylalkyl, thiophenylalkyl, pyrazolylalkyl, imidazolylalkyl, oxazolylalkyl, thiazolylalkyl, isoxazolylalkyl, isothiazolylalkyl, 1,2,3-triazolylalkyl, 1,2,4-triazolylalkyl, 1,2,3-oxadiazolylalkyl, 1,3,4-oxadiazolylalkyl, 1,2,3-thiadiazolylalkyl, 1,3,4-thiadiazolylalkyl, indolylalkyl, pyridylalkyl, pyridazinylalkyl, pyrimidinylalkyl, pyridazinylalkyl, quinolinylalkyl, isoquinolinylalkyl, pyrrolyl, furanyl,
    Type: Grant
    Filed: February 13, 2001
    Date of Patent: January 25, 2005
    Assignee: Ciba Specialty Chemicals Corporation
    Inventors: Wolfgang Haap, Werner Hölzl, Dietmar Ochs, Karin Petzold, Marcel Schnyder
  • Patent number: 6723716
    Abstract: 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: Grant
    Filed: September 21, 2000
    Date of Patent: April 20, 2004
    Assignee: Essential Therapeutics, Inc.
    Inventors: Scott J. Hecker, Aesop Cho, Tomasz W. Glinka, Trevor Calkins, Ving J. Lee
  • Publication number: 20030162763
    Abstract: The present invention relates to a novel cephalosporin compound and pharmaceutically acceptable non-toxic salt, physiologically hydrolysable ester, hydrate, solvate or isomer thereof, to a pharmaceutical composition containing the compound and to a process for preparing the compound.
    Type: Application
    Filed: November 21, 2002
    Publication date: August 28, 2003
    Inventors: Chang-Seok Lee, Seong-Ho Oh, Eun-Jung Ryu, Seong-Baek Lee, Ha-Sik Youn, Yong-Jin Jang, Geun-Tae Kim, Hyang-Sook Lee
  • 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: 6583133
    Abstract: 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: Grant
    Filed: June 22, 1999
    Date of Patent: June 24, 2003
    Assignee: Basilea Pharmaceutica AG
    Inventors: Peter Angehrn, Erwin Götschi, Ingrid Heinze-Krauss, Hans G. F. Richter
  • 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
  • Publication number: 20030008858
    Abstract: 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 &bgr;-lactams, penicillin-binding protein, carboxypeptidase,. Such compounds, including particularly &bgr;-lactam ring-containing compounds, can be used to formulate pharmaceutical formulations useful for improving sexual function.
    Type: Application
    Filed: June 18, 2002
    Publication date: January 9, 2003
    Inventor: Gay A. Koppel
  • Patent number: 6414002
    Abstract: Compounds are provided which have the structure wherein Q is C or N, A is 0 or S, Z is O or a bond, X is CH or N and R1, R2, R2a, R2b, R2c, R3, Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.
    Type: Grant
    Filed: March 20, 2001
    Date of Patent: July 2, 2002
    Assignee: Bristol-Myers Squibb Company
    Inventors: Peter T. Cheng, Pratik Devasthale, Yoon Jeon, Sean Chen, Hao Zhang
  • 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: 20020065263
    Abstract: A new parenteral dosage form for 7-D-mandelamido-3-(1-sulfomethyltetrazol-5-yl)thiomethyl) -3-cephem-4-carboxylic acid mono sodium salt (“Cefonicid”) is provided.
    Type: Application
    Filed: November 30, 2001
    Publication date: May 30, 2002
    Applicant: SmithKline Beecham S.A.
    Inventors: Africa Aranda Garcia, Fernando Hijar Ordovas
  • Patent number: 6329363
    Abstract: The invention provides new fluorinated cephalosporin antibiotics and methods of preventing or treating infection, particularly mastitis in ruminants, using these antibiotics, and veterinary and pharmaceutical formulations comprising these antibiotics.
    Type: Grant
    Filed: November 6, 1998
    Date of Patent: December 11, 2001
    Assignee: Eli Lilly and Company
    Inventor: Karl Robert Dahnke
  • Patent number: 6319904
    Abstract: The present invention includes a formulation which comprises an antibacterial substance and an antiulcer substance, wherein at least either of them is formulated into a gastrointestinal mucosa-adherent solid preparation. The formulation of the present invention shows long retention time in the gastrointestinal tract because of adhesion to the gastrointestinal tract mucosa, synergetically enhances the pharmaceutical effects of an antibacterial substance, specially antibiotic against Helicobacter pylori (HP) and an antiulcer substance, with very low doses of active ingredients, particularly the anti-HP antibiotic with low prevalence of side effects. The present agent is useful as an antiulcer agent, showing potent anti-HP activity.
    Type: Grant
    Filed: July 7, 1999
    Date of Patent: November 20, 2001
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yohko Akiyama, Masafumi Nakao, Naoki Nagahara, Susumu Iwasa
  • 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: 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: 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: 6150351
    Abstract: This invention relates to new cephem compound represented by the following general formula (I): ##STR1## wherein each symbol is as defined in the specification or a salt thereof, which has antimicrobial activity against Helicobacter pylori, and are useful as anti-Helicobacter pylori agents, anti-gastritis agents, anti-ulcer agents and anti-cancer agents.
    Type: Grant
    Filed: August 12, 1998
    Date of Patent: November 21, 2000
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Yoshiki Yoshida, Shinya Okuda, Hiroshi Sasaki, Keiji Matsuda, Hisashi Takasugi
  • 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: 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: 5945414
    Abstract: Cefazolin, cefazedone, cefoperazone, cefamandole, cefatrizine or ceftriaxone is prepared by reacting glutaryl 7-ACA of the formula: ##STR1## with a compound of formula (II):R--SH (II)wherein R is 5-methyl-1,3,4-thiadiazol-2-yl, 1H-1,2,3-triazol-4-yl, 1-methyl-tetrazol-5-yl or1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-1,2,4-triazin-3-yl group, and R.sup.1 and R.sup.2 are both hydrogen and the other is an acyl group, in an aqueous solution in an amount of 3-5 mols per mol of glutaryl 7-ACA to about 90.degree. C. and for a time from about 2 to about 10 hours;optionally recovering the excess of the compound of formula (II), thereby preparing a compound of formula (III) in an aqueous solution: ##STR2## wherein R is as above defined and optionally deacylating said compound of formula (III); andconverting the resulting compound of formula (I) ##STR3## wherein R, R.sup.1 and R.sup.2 are as defined above in the presence of a non-chlorinated solvent into one of said cephalosporins.
    Type: Grant
    Filed: December 2, 1997
    Date of Patent: August 31, 1999
    Assignee: Antibioticos S.p.A.
    Inventors: Loris Sogli, Daniele Terrassan, Ermanno Bernasconi, Francisco Salto
  • Patent number: 5728691
    Abstract: Derivatives of 7-aminoceph-3-em-4-carboxylic acid with 6-fluoroquinolone derivatives in which the cephem and 6-fluoroquinolone moieties are bound to each other through a carboxamido bond as well as the pharmaceutical compositions containing them are described. These compounds possess antibacterial, growth promoting and probiotic activity.
    Type: Grant
    Filed: August 22, 1996
    Date of Patent: March 17, 1998
    Assignees: Laboratorios Aranda S.A. De C.V., Judith Marcia Arrieta Munguia
    Inventor: Miguel Angel Corpi Constantino
  • Patent number: 5710146
    Abstract: Cephem derivatives of the general formula ##STR1## in 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 22, 1994
    Date of Patent: January 20, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Walter Durckheimer, Dieter Bormann, Eberhard Ehlers, Elmar Schrinner, Rene Heymes
  • Patent number: 5705496
    Abstract: The present invention relates to benzathine salts of cefonicid, a member of the cephalosporin family of antibiotics, which are crystalline.
    Type: Grant
    Filed: September 25, 1995
    Date of Patent: January 6, 1998
    Assignee: SmithKline Beecham Corporation
    Inventor: Theodore John Polansky
  • Patent number: 5698544
    Abstract: The present invention provides a cephem compound having a high antimicrobial activity against various pathogenic bacteria.The cephem compound of the invention is represented by the formula ##STR1## wherein Q represents CH or N, R.sup.1 represents a carboxylate or the like, R.sup.2 represents a hydrogen atom, and R represents ##STR2## wherein R.sup.3 represents a group --(CH.sub.2).sub.m --Y (wherein m is an integer of 1 to 5, and Y represents a quaternary ammonium group) or the like, n is an integer of 0 to 4, B.sup.- represents an anion, f is 0 or 1 when R.sup.1 represents a carboxylate, and 2 when R.sup.1 represents a carboxyl group, and the ring C represents a 5-membered heterocyclic group of not more than 4 nitrogen atoms, which may be substituted by a lower alkyl group.
    Type: Grant
    Filed: November 16, 1995
    Date of Patent: December 16, 1997
    Assignees: Otsuka Kagaku Kabushiki Kaisha, Taiho Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Akagi, Masaru Yasui, Takae Yamada, Masahiro Ito, Akio Hyodo, Hideaki Hanaki
  • Patent number: 5698547
    Abstract: The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their 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: May 31, 1995
    Date of Patent: December 16, 1997
    Assignee: Microcide Pharmaceuticals, Inc.
    Inventors: Burton Christensen, In-Seop Cho, Tomasz Glinka, Scott Hecker, Ving J. Lee, Zhijia J. Zhang
  • Patent number: 5635501
    Abstract: Compound of formula (I) or salts thereof wherein R.sup.1 is hydrogen, methoxy or formamido; R.sup.2 is an acyl group; CO.sub.2 R.sup.3 is a carboxy group or a carboxylate anion, or R.sup.3 is a readily removable carboxy protecting group or a pharmaceutically acceptable salt-forming group or in vivo hydrolysable ester group; R.sup.4 represents hydrogen or up to four substituents; X is S, SO, SO.sub.2 or CH.sub.2 ; Y is O, S, SO or SO.sub.2 ; n is 0 or 1; m is 1 or 2; and wherein in the (a) ring system the dotted line indicates that one pair of adjacent ring carbon atoms is joined by a C.dbd.C double bond. These compounds have antibacterial activity.
    Type: Grant
    Filed: January 25, 1995
    Date of Patent: June 3, 1997
    Assignee: Pfizer Inc.
    Inventors: George Burton, John H. Bateson, Richard L. Elliott, Stephen C. M. Fell
  • Patent number: 5629306
    Abstract: Derivatives of 7-alkylidene cephalosporanic acid sulfone and the pharmaceutically active salts thereof are found to be potent inhibitors of .beta.-lactamase enzymes.
    Type: Grant
    Filed: December 9, 1994
    Date of Patent: May 13, 1997
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Brian Bachmann
  • Patent number: 5593986
    Abstract: The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their 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: March 29, 1995
    Date of Patent: January 14, 1997
    Assignee: Microcide Pharmaceuticals, Inc.
    Inventors: Burton G. Christensen, In-Seop Cho, Tomasz W. Glinka, Scott J. Hecker