The Additional Hetero Ring Is Part Of A Polycyclo Ring System Patents (Class 514/205)
  • Patent number: 8829028
    Abstract: This invention provides the use of a 5-HT4 receptor antagonist in the manufacture of a medicament for treating or preventing heart failure. Particular heart disorders to be treated are selected from the group comprising chronic heart failure, congestive heart failure, chronic congestive heart failure and heart failure resulting from ischaemic heart disease. Methods of treating heart failure using 5-HT4 receptor antagonists and pharmaceutical compositions containing 5-HT4 receptor antagonists are also provided.
    Type: Grant
    Filed: February 17, 2009
    Date of Patent: September 9, 2014
    Assignee: Serodus AS
    Inventor: Finn Olav Levy
  • Patent number: 8790691
    Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.
    Type: Grant
    Filed: May 26, 2009
    Date of Patent: July 29, 2014
    Assignee: The University of British Columbia
    Inventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
  • Publication number: 20110195066
    Abstract: The present invention relates to new quinoline inhibitors of tyrosine kinases, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: February 3, 2011
    Publication date: August 11, 2011
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventor: Chengzhi Zhang
  • Patent number: 7807684
    Abstract: Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: July 17, 2006
    Date of Patent: October 5, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Sandeep A. Saggar, John T. Sisko, Thomas J. Tucker, Robert M. Tynebor, Dai-Shi Su, Neville J. Anthony
  • 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
  • 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
  • Publication number: 20100029604
    Abstract: The invention relates to a pharmaceutical composition comprising an ethylene derivatives of tricyclic carbapenems of the general Formula (I) in the form of pure diastereoisomers and in the form of pure geometric isomers or a salt, ester or amide derivate thereof and an antibiotic and the use of this composition as a broad band spectrum ?-lactamase inhibitor.
    Type: Application
    Filed: February 13, 2008
    Publication date: February 4, 2010
    Inventors: Andrej Prezelj, Uros Urleb, Tomaz Solmajer
  • 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: 7115624
    Abstract: The present invention provides a method of inhibiting a member of a family of Protein Tyrosine Phosphatases (PTPases, PTPs) such as PTP1B, TC-PTP, CD45, SHP-1, SHP-2, PTP?, PTP?, PTP?, PTP?, PTP?, PTP?, PTP?, PTPD1, PTPD2, PTPH1, PTP-MEG1, PTP-LAR, and HePTP by exposing said Ptpase member by administration to a host or otherwise to at least one compound with certain structural, physical and spatial characteristics that allow for the interaction of said compound with specific residues of the active site of PTP1B and/or TC-PTP. These compounds are indicated in the management or treatment of a broad range of diseases such as autoimmune diseases, acute and chronic inflammation, osteoporosis, various forms of cancer and malignant diseases, and type I diabetes and type II diabetes, as well as in the isolation of PTPases and in elucidation or further elucidation of their biological function.
    Type: Grant
    Filed: September 11, 2000
    Date of Patent: October 3, 2006
    Assignee: Novo Nordisk A/S
    Inventors: Henrik Sune Andersen, Thomas Kruse Hansen, Lars Fogh Iversen, Jesper Lau, Niels Peter Hundahl Møller, Ole Hvilsted Olsen, Frank Urban Axe, Yu Ge, Daniel Dale Holsworth, Todd Kevin Jones, Luke Milburn Judge, Wiliam Charles Ripka, Barry Zvi Shapira, Roy Teruyuki Uyeda
  • 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: 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
  • 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
  • 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: 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
  • Patent number: 6294527
    Abstract: An antibacterial compound wherein represents benzene ring, pyridine ring, pyrazine ring or 5-membered aromatic neterocycle (having one oxygen or sulfur atom as ring-constituting atom), there being no R4 where  represents 5-membered aromatic heterocycle; X and Y respectively represent hydrogen atom or CXY represents C═N—OR5 wherein R5 represents hydrogen atom, halo C1-C6 alkyl or C3-C7 cycloalkyl; R1 represents phenyl, furyl, thienyl, thiazolyl (which may be substituted by amino group), tetrazolyl or thiadiazolyl, R2, R3 and R4 respectively represent hydrogen atom, halogen, hydroxyl group, nitro, C1-C6 alkoxy, trifluoromethyl, isothiuronium C1-C6 alkyl, amino C1-C6 alkyl, halo C1-C6 alkyl, morpholino, piperidino or piperazinyl.
    Type: Grant
    Filed: July 20, 1999
    Date of Patent: September 25, 2001
    Assignee: Zenyaku Kogyo Kabushiki Kaisha
    Inventors: Hideaki Hanaki, Hiroaki Yamazaki, Yoshio Tsuchida, Hideki Sato, Keiichi Hiramatsu, Seiichiro Kawashima
  • 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: 6262044
    Abstract: The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.
    Type: Grant
    Filed: March 11, 1999
    Date of Patent: July 17, 2001
    Assignees: Novo Nordisk A/S, Ontogen Corporation
    Inventors: Niels Peter Hundahl Møller, Henrik Sune Andersen, Lars Fogh Iversen, Ole Hvilsted Olsen, Sven Branner, Daniel Dale Holsworth, Farid Bakir, Luke Milburn Judge, Frank Urban Axe, Todd Kevin Jones, William Charles Ripka, Yu Ge, Roy Teruyuki Uyeda
  • Patent number: 6242437
    Abstract: A compound represented by the following formula (I) is disclosed. This compound has potent antimicrobial activity against a wide spectrum of bacteria from Gram-positive bacteria to Grame-negative bacteria including &bgr;-lactamase producing bacteria. In particular, it has higher antimicrobial activity against methicilline-resistant Staphylococcus aureus (MRSA), penicillin-resistant Streptococcus pneumoniae (PRSP), and imipenem-resistant Pseudomonas aeruginosa than the existing onium salt type cephem derivatives and hence is very useful as a therapeutic agent for infectious diseases derived from various pathogenic bacteria. wherein X represents CH or N, R1 represents a hydrogen atom, substituted or unsubstituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, or cycloalkyl; any one of R2, R3, R4, and R5 represents R6R7NSO2NH—C1-6 alkyl where R6 and R7, which may be the same or different, represent a hydrogen atom or C1-6 alkyl; and n is 0 or 1.
    Type: Grant
    Filed: June 7, 1999
    Date of Patent: June 5, 2001
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Kazuko Kobayashi, Eijirou Umemura, Kunio Atsumi, Takashi Ida
  • Patent number: 6180621
    Abstract: A method for the prophylaxis or treatment of infectious diseases caused by helicobacter pyloir, by administering a pharmacologically effective amount of a 1-methoylcarbapenem coumpund of formula (I) or a pharmacologically acceptable salt or ester thereof: R1 represents a group of the following formula: R2 is a hydrogen atom or a C1-C6 alkyl group, and R3 is a hydrogen atom or a C1-C6 alkyl group.
    Type: Grant
    Filed: November 6, 1998
    Date of Patent: January 30, 2001
    Assignee: Sankyo Company, Limited
    Inventors: Isao Kawamoto, Satoshi Ohya, Yukio Utsui
  • 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: 5883089
    Abstract: Compounds, represented by the following formula (I), having a .beta.-(substituted or unsubstituted imidazo?5,1-b!thiazolyl)vinyl group at the 3-position of the cephem ring and a salt and an ester thereof are disclosed. The compounds have antibacterial activity against a very wide spectrum of bacteria and potent antibacterial activity against Gram-positive bacteria, Gram-negative bacteria, and resistant bacteria. ##STR1## wherein X represents CH or N, R.sup.1 represents a hydrogen atom or an amino protective group, R.sup.2 represents a hydrogen atom, a C.sub.1-6 alkyl group, a C.sub.3-7 cycloalkyl group, or a hydroxy protective group, R.sup.3 is absent or represents a hydrogen atom, a salt forming cation, or a carboxyl protective group, R.sup.4, R.sup.5, and R.sup.6, which may be the same or different, each independently represent a hydrogen atom or a C.sub.1-6 alkyl group, R.sup.7+ is absent or a cation of a C.sub.1-6 alkyl, and n is an integer of 0 to 1.
    Type: Grant
    Filed: March 12, 1997
    Date of Patent: March 16, 1999
    Assignee: Meiji Seika Kabushiki Kaisha
    Inventors: Eijiro Umemura, Kunio Atsumi, Katsuyoshi Iwamatsu, Atsushi Tamura
  • 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: 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: 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: 5607927
    Abstract: An aminothiazolyl- or aminothiadiazolyl-cephalosporin derivative represented by the following general formula (I) which has a condensed-ring thio group as a 3-positioned substituent group that contains a thiazolylthio group, an oxazolylthio group or a heterocyclic ring thereof as one of the ring components. The compound according to the present invention has excellent activities to inhibit growth of various bacteria, especially Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA), and therefore, the antibacterial agent comprising, as an active ingredient, the inventive compound can be used as a therapeutic drug for the treatment of various bacterial infections.
    Type: Grant
    Filed: February 7, 1995
    Date of Patent: March 4, 1997
    Assignee: Meiji Seika Kaisha, Ltd.
    Inventors: Masaki Tsushima, Katsuyoshi Iwamatsu, Atsushi Tamura, Seiji Shibahara
  • Patent number: 5607926
    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: March 4, 1997
    Assignee: Microcide Pharmaceuticals, Inc.
    Inventors: Scott J. Hecker, In-Seop Cho, Burton G. Christensen, Tomasz W. Glinka
  • Patent number: 5604218
    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 30, 1995
    Date of Patent: February 18, 1997
    Assignee: Microcide Pharmaceuticals, Inc.
    Inventors: Scott Hecker, In-Seop Cho, Burton Christensen, Tomasz Glinka, Ving J. Lee
  • 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
  • Patent number: 5593984
    Abstract: The present invention relates to novel cephalosporin derivatives or pharmaceutically acceptable non-toxic salts thereof useful as antibiotics and to processes for the preparation thereof. ##STR1## wherein: R.sup.1 is a hydrogen or an optionally halogen-substituted C.sub.1-3 alkyl group, a propargyl group or --C(R.sup.a)(R.sup.b)COOH, wherein R.sup.1 and R.sup.b are independently a hydrogen or a C.sub.1-3 alkyl group;R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are independently a hydrogen or halogen or a C.sub.1-3 alkyl, amino or hydroxy C.sub.1-3 alkylthio, cyano, carbamoyl, carboxyl, hydroxy C.sub.1-3 alkyl, nitro, acetyl or formyl group; andQ is CH, N or CCl.
    Type: Grant
    Filed: March 31, 1995
    Date of Patent: January 14, 1997
    Assignee: Yuhan Corporation
    Inventors: Jong W. Lee, Jeong S. Chae, Young R. Choi, Yeong N. Lee, Eun R. Rho, Heui I. Kang, Jae W. Hyun
  • Patent number: 5587372
    Abstract: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids,wherein the variables are herein below defined, having antibacterial properties.
    Type: Grant
    Filed: December 13, 1993
    Date of Patent: December 24, 1996
    Assignee: Roussel Uclaf
    Inventors: Jozsef Aszodi, Jean-Francois Chantot, Patrick Fauveau, Solange G. D'Ambrieres, Daniel Hunbert, Christophe Dini
  • Patent number: 5571804
    Abstract: Cephalosporin compounds of formula (I): ##STR1## wherein: R.sup.1 is a hydrogen or an amino protecting group;R.sup.2 and R.sup.3 are, independently, a hydrogen or a hydroxy protecting group, or form together a cyclic diol protecting group;R.sup.4 and R.sup.5 are, independently, a hydrogen or a carboxyl protecting group;X and Y are a nitrogen and a carbon atom, respectively, or a carbon and a nitrogen atom, respectively;R.sup.6 and R.sup.7 are, independently, a hydrogen or an amino, substituted amino, hydroxy, alkoxy, C.sub.1-4 alkyl, carboxyl or alkoxy carbonyl group, or jointly form a C.sub.3-7 cycloalkyl group together with the carbon to which they are attached, when X and Y are a nitrogen and a carbon, respectively, or R.sup.7 is a hydrogen or an amino group when X and Y are a carbon and a nitrogen, respectively; andQ is .dbd.CH-- or .dbd.
    Type: Grant
    Filed: September 9, 1994
    Date of Patent: November 5, 1996
    Assignee: Lucky Limited
    Inventors: Chan S. Bang, Jae H. Yeo, Young M. Woo, Jong C. Lim, Deog H. Yang, Se H. Kim, Jae H. Jeon, Mi K. Seo, Sam S. Kim, Tae H. Lee, Yong Z. Kim, Hun S. Oh
  • Patent number: 5446037
    Abstract: This invention relates to 2-[(substituted)methylene]cephalosporin sulfones and in particular 2-[(heteroaryl substituted)methylene]cephalosporin sulfones which are effective elastase inhibitors as well as effective thrombin inhibitors and therefore are useful as anti-inflammatory, anti-degenerative and anti-thrombin agents.
    Type: Grant
    Filed: December 13, 1993
    Date of Patent: August 29, 1995
    Assignee: Synphar Laboratories, Inc.
    Inventors: Samarendra Maiti, Charles Fiakpui, A. V. N. Reddy, David Czajkowski, Paul Spevak, Harninder Atwal, Ronald G. Micetich
  • Patent number: 5409917
    Abstract: A method and composition for topically treating acne and acneiform dermal disorders includes applying an amount of a cephalosporin antibiotic effective to treat the acne and acneiform dermal disorders. The antibiotic is blended with a carrier suitable for topical application to dermal tissues. The carrier is selected from the group consisting of an aqueous liquid, an alcohol base, a water soluble gel, a lotion, an ointment, a nonaqueous liquid base, a mineral oil base, a blend of mineral oil and petrolatum, liposomes, a time-release patch, and a liquid-absorbed wipe. The cephalosporin can also be combined with benzoyl peroxide in a gel carrier.
    Type: Grant
    Filed: September 24, 1993
    Date of Patent: April 25, 1995
    Assignees: Marvin S. Towsend, Leonard Bloom
    Inventors: Howard N. Robinson, Neil F. Martin
  • Patent number: 5373000
    Abstract: A cephalosporin derivative represented by the formula: ##STR1## wherein R.sub.1 represents a lower alkyl group, and A is selected from: a group of the following formula: ##STR2## where R.sub.2 and R.sub.3 are the same or different lower alkyl group, R.sub.4 represents a substituted lower alkyl or amino group;a group which may be substituted and which is represented by the following formula: ##STR3## where R.sub.5 represents a lower alkyl group; or a group of the following formula: ##STR4## where R.sub.5 is as defined above, R.sub.6 represents a hydroxyl lower alkyl or carboxyl group, or its pharmacologically acceptable salt, and a process for preparing the same, as well as an antibacterial agent containing the same.
    Type: Grant
    Filed: April 1, 1992
    Date of Patent: December 13, 1994
    Assignee: Eisai Co., Ltd.
    Inventors: Yoshimasa Machida, Takashi Kamiya, Shigeto Negi, Toshihiko Naito, Yuuki Komatu, Seiichiro Nomoto, Isao Sugiyama, Hiroshi Yamauchi
  • Patent number: 5312813
    Abstract: A method of killing microorganisms which form a biofilm on a tissue or implant surfaces in a patient, and which are refractory to a biocide at a dose which is effective to kill the microorganism in planktonic form. The effect of the biocide is potentiated, to an effective killing level, by applying an electric field across the surface containing the biofilm.
    Type: Grant
    Filed: July 22, 1992
    Date of Patent: May 17, 1994
    Assignee: University Technologies International
    Inventors: John W. F. Costerton, Antoine E. Khoury, Frank Johnson
  • Patent number: 5192770
    Abstract: .alpha.-Oxoacetamides of the formula R.sup.1 C(O)C(O)NR.sup.2 R.sup.3 in which R.sup.1 is optionally substituted phenyl, 1-indolyl, 2,3-dihydro-1-indolyl, 1-benzimidazolidinonyl, 3-benzofuranyl, 3-benzothiophenyl, 3-indolyl, and 1,2-alkano-3-indolyl; R.sup.2 is selected from: ##STR1## and R.sup.3 is selected from hydrogen or lower alkyl; and the pharmaceutically acceptable salts, individual isomers, mixtures of isomers, processes for preparation, compositions, and methods of use thereof.
    Type: Grant
    Filed: December 7, 1990
    Date of Patent: March 9, 1993
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Robin D. Clark, Richard M. Eglen, Joseph M. Muchowski, William L. Smith, Klaus K. Weinhardt
  • Patent number: 4826834
    Abstract: A compound having the general formula ##STR1## wherein, R.sup.0 is a hydrogen atom, a nitrogen-containing heterocyclic group, an acyl group or an amino-protective group; Z is S, S.fwdarw.O,O or CH.sub.2 ; R.sup.4 is a hydrogen atom, a methoxy group, or a formamide group; R.sup.13 is a hydrogen atom, a methyl group, a hydroxyl group, or a halogen atom; A.sym. is a condensed triazolio group which may be substituted, or a pharmaceutically acceptable salt or ester thereof is novel and has an excellent antibacterial activity.
    Type: Grant
    Filed: September 22, 1986
    Date of Patent: May 2, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Yoshinobu Yoshimura, Naoto Hashimoto, Shoji Kishimoto
  • Patent number: 4814328
    Abstract: The compound having the formula: ##STR1## wherein R is a straight chain, branched chain or cyclic lower alkyl, a lower alkenyl or a lower alkynyl group which may be substituted by a carboxyl group, and R.sup.1 is hydrogen atom or an acetyl group; or a pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.
    Type: Grant
    Filed: September 26, 1986
    Date of Patent: March 21, 1989
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Susumu Nakagawa, Norikazu Otake, Ryosuke Ushizima
  • Patent number: 4788185
    Abstract: A compound of the formula; ##STR1## wherein R.sup.0 stands for hydrogen atom, nitrogen-containing heterocyclic group, acyl group or esterified carboxyl group, Z stands for S, S.fwdarw.O, O or CH.sub.2, R.sup.4 stands for hydrogen atom, methoxy group or formamido group, R.sup.13 stands for hydrogen atom, methyl group, hydroxyl group or halogen atom and A stands for an optionally substituted imidazol-1-yl group forming a condensed ring at the 2,3- or 3,4-position or a physiologically or pharmaceutically acceptable salt or ester thereof.This compound is novel and has excellent antibacterial activity.
    Type: Grant
    Filed: April 23, 1985
    Date of Patent: November 29, 1988
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Akio Miyake, Masahiro Kondo, Masahiko Fujino
  • Patent number: 4748163
    Abstract: Antibacterially active and animal growth-promoting novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents the radical ##STR2## Y representing N or CR.sup.9, or Y--R.sup.7 representing >C.dbd.O or >C.dbd.N--R.sup.7,Z representing O, S, or NR.sup.10, andR.sup.2 represents hydrogen or a protective group.
    Type: Grant
    Filed: February 21, 1986
    Date of Patent: May 31, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunter Schmidt, Hans-Joachim Zeiler, Karl G. Metzger
  • Patent number: 4734407
    Abstract: Antibacterially active and animal growth-regulating novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents an optionally substituted radical of the formula ##STR2## Z represents oxygen, sulphur or --N--R.sup.
    Type: Grant
    Filed: March 10, 1986
    Date of Patent: March 29, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunter Schmidt, Hans-Joachim Zeiler, Karl G. Metzger
  • Patent number: 4731360
    Abstract: Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs.
    Type: Grant
    Filed: August 16, 1985
    Date of Patent: March 15, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, A. J. Repta, Joseph A. Fix
  • Patent number: 4729989
    Abstract: Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs.
    Type: Grant
    Filed: June 28, 1985
    Date of Patent: March 8, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, Joseph A. Fix
  • Patent number: 4692441
    Abstract: Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.
    Type: Grant
    Filed: August 16, 1985
    Date of Patent: September 8, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, A. J. Repta, Joseph A. Fix
  • Patent number: 4692443
    Abstract: Cephalosporin compounds substituted in the 7-position by a 2-(5- or 6-membered heterocyclic)-2-oximinoacetylamino group and in the 3-position with an imidazolo, oxazolo or thiazolopyridinium-methyl group are broad spectrum antibiotics highly effective in combating bacterial infections of gram-negative and gram-positive microorganisms. The cephalosporins are best prepared by reacting a silylated 7-[2-(heterocyclic)-2-oximinoacetylamino]-3-iodomethyl-3-cephem-4-carboxyl ic acid with an imidazolopyridine, and oxazolopyridine or a thiazolopyridine. Pharmaceutical formulations comprising a compound of the invention and a method for treating bacterial infections comprising their use are also provided.
    Type: Grant
    Filed: December 10, 1984
    Date of Patent: September 8, 1987
    Assignee: Eli Lilly and Company
    Inventor: Allen S. Katner
  • Patent number: RE33948
    Abstract: Antibacterially active and animal growth-promoting novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents the radical ##STR2## Y representing N or CR.sup.9, or Y--R.sup.7 representing ##STR3## Z representing O, S, or NR.sup.10, and R.sup.2 represents hydrogen or a protective group.
    Type: Grant
    Filed: August 29, 1989
    Date of Patent: June 2, 1992
    Assignee: Bayer Aktiengesellschaft
    Inventors: Gunter Schmidt, Hans-Joachim Zeiler, Karl G. Metzger