1-thia-4-aza-bicyclo (3.2.0) Heptane Ring Containing (including Dehydrogenated) (e.g., Penicillins, Etc.) Patents (Class 514/192)
  • Patent number: 6232305
    Abstract: The present invention provides substituted amino bicyclic-&bgr;-lactam penam derivatives and substituted amino bicyclic-&bgr;-lactam cepham derivatives and their diastereoisomers of formula I, as well as compositions, methods of making, and methods of using, which exhibit excellent cysteine protease inhibitory activity and which may be used for treatment of different diseases such as cancer (including cancer metastasis), osteoporosis, rheumatoid arthritis.
    Type: Grant
    Filed: January 22, 1998
    Date of Patent: May 15, 2001
    Assignee: Naeja Pharmaceutical Inc.
    Inventors: Rajeshwar Singh, Nian Zhou, Deqi Guo, Ronald G. Micetich
  • Patent number: 6225282
    Abstract: Compositions and methods are provided for prophylactic or therapeutic treatment of a mammal for hearing impairments involving neuronal damage, loss, or degeneration, preferably of spinal ganglion neurons, by administration of a therapeutically effective amount of a trkB or trkC agonist, particularly a neurotrophin, more preferably NT-4/5. Also provided are improved compositions and methods for treatments requiring administration of a pharmaceutical having an ototoxic side-effect, wherein the improvement includes administering a therapeutically effective amount of a trkB or trkC agonist to treat the ototoxicity.
    Type: Grant
    Filed: January 2, 1997
    Date of Patent: May 1, 2001
    Assignee: Genentech, Inc.
    Inventor: Wei-Qiang Gao
  • Patent number: 6207661
    Abstract: The present invention provides a premixed form of a buffered piperacillin product having a near neutral pH and capable of a shelf life of at least nine months, with freezer storage (−20° C. or lower), or a refrigerated shelf life of up to 14 days at about 5° C. The piperacillin may additionally contain a tazobactam component to inactivate beta-lactamases that commonly cause resistance to penicillins, allowing the piperacillin component to destroy susceptible bacteria. With the addition of dextrose, the premixed composition is physiologically isosmotic.
    Type: Grant
    Filed: February 22, 1999
    Date of Patent: March 27, 2001
    Assignee: Baxter International Inc.
    Inventors: Stacey S. Thompson, Rao Chilamkurti, Mary Samuel, Norma Stephens
  • Patent number: 6165975
    Abstract: A method of treatment, in an organism, of a vascular condition, comprising administration of at least one agent at a level which enhances NO and which does not appreciably alter normal systemic vascular tone in said organism. At least one agent is an NO donor selected from the group consisting of glyceryl trinitrate, isosorbide 5-mononitrate, isosorbide dinitrate, pentaerythritol tetranitrate, erythrityl tetranitrate, sodium nitroprusside, 3-morpholinosydnonimine molsidomine, S-nitroso-N-acetylpenicillamine, S-nitrosoglutathione, and N-hydroxy-L-arginine.
    Type: Grant
    Filed: December 22, 1999
    Date of Patent: December 26, 2000
    Assignee: Queen's University at Kingston
    Inventors: Michael A. Adams, Jeremy P. W. Heaton, James D. Banting
  • Patent number: 6156745
    Abstract: Compounds of formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting .beta.-lactamase enzymes, for enhancing the activity of .beta.-lactam antibiotics, and for treating .beta.-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.
    Type: Grant
    Filed: December 29, 1998
    Date of Patent: December 5, 2000
    Assignee: Research Corporation Technologies, Inc.
    Inventors: John D. Buynak, Akireddy Srinivasa Rao, Venkata Ramana Doppalapudi
  • Patent number: 6140306
    Abstract: The present invention relates to methods and compositions for treating gram-negative bacterial infections, using BPI protein products. Co-treatment, or concurrent administration, of BPI protein product with an antibiotic in treatment of gram-negative bacterial infections improves the therapeutic effectiveness of the antibiotic, including increasing antibiotic susceptibility of gram-negative bacteria and reversing resistance of the bacteria to antibiotics.
    Type: Grant
    Filed: June 3, 1996
    Date of Patent: October 31, 2000
    Assignee: Xoma Corporation
    Inventors: Lewis H. Lambert, Jr., Roger G. Little, II
  • Patent number: 6124328
    Abstract: The present invention relates to methods and pharmaceutical compositions for stimulating the growth of neutering in nerve cells. The compositions comprise a neurotrophic amount of a compound which binds to the FK-506 binding protein (FKBP) and a neurotrophic factor, such as nerve growth factor NGF. The methods comprise treating nerve cells with the above-described compositions or compositions comprising the FKBP binding compound without a neurotrophic factor. The methods of this invention can be used to promote repair of neuronal damage caused by disease or physical trauma.
    Type: Grant
    Filed: February 28, 1997
    Date of Patent: September 26, 2000
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventor: David M. Armistead
  • Patent number: 6093414
    Abstract: The present invention relates generally to silver-based antimicrobial compositions and processes for making such compositions. More particularly, the present invention describes stable, purified silver-based antimicrobial compositions, and processes for making such compositions, comprising carrier-free silver thiosulfate ion complexes either suspended in a base or incorporated into a matrix. These silver thiosulfate ion complex antimicrobial compositions are useful in the treatment and prevention of infections and diseases.
    Type: Grant
    Filed: August 11, 1997
    Date of Patent: July 25, 2000
    Assignee: Christopher C. Capelli
    Inventor: Christopher C. Capelli
  • Patent number: 6054431
    Abstract: The present invention relates to methods of treating gram-positive bacterial infections by administration of a BPI protein product alone, or in combination with an antibiotic. BPI protein product alone has a bactericidal or growth inhibitory effect on selected gram-positive organisms. BPI protein product also increases the susceptibility of gram-positive organisms to antibiotics and can even reverse resistance of gram-positive organisms to antibiotic.
    Type: Grant
    Filed: July 20, 1998
    Date of Patent: April 25, 2000
    Assignee: XOMA Corporation
    Inventors: Arnold Horwitz, Lewis H. Lambert, Jr., Roger G. Little, II
  • Patent number: 6051553
    Abstract: The present invention provides methods of potentiating the gram-negative bactericidal activity of BPI protein products by means of administering LBP protein products.
    Type: Grant
    Filed: June 22, 1998
    Date of Patent: April 18, 2000
    Assignee: Xoma Corporation
    Inventor: Arnold Horwitz
  • Patent number: 6015808
    Abstract: Pharmaceutical compositions with heretofore unknown and enhanced physical, chemical, and biological properties are prepared by combining known biologically active parent compounds with oxo thia azabicyclo compounds, such as lactam and .beta.-lactam compounds, capable of rapidly transporting the parent compounds in undegraded form to their target sites of action. A process for combining the parent compound with .beta.-lactam compounds consists of dissolving the parent compound in a polar solvent, adding a .beta.-lactam compound, incubating the resulting mixture, followed by drying, and subjecting the remaining solid material to solvent washing or extraction to further purify the new pharmaceutical composition. The new pharmaceutical composition possesses the biological and therapeutic activity of the parent compound and the barrier penetrating characteristics of the .beta.
    Type: Grant
    Filed: August 22, 1995
    Date of Patent: January 18, 2000
    Inventors: Mandayam Jeersannidhi Thirumalachar, Mandayam Jeersannidhi Narasimhan, Jr.
  • 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: 5985259
    Abstract: An improved method of sterilizing the field of surgery prior to an ophthalmic surgical procedure is described. The invention eliminates the need for painfull and potentially traumatic injections of antibiotics by utilizing sustained release compositions which allow the antibiotics contained therein to penetrate deeply into the eye, thereby ensuring a sterile field of surgery during intraocular surgical procedures. The compositions may also be utilized to prevent post-surgical infections.
    Type: Grant
    Filed: April 30, 1997
    Date of Patent: November 16, 1999
    Assignee: Alcon Laboratories, Inc.
    Inventors: Gerald D. Cagle, Tai-Lee Ke, Barry A. Schlech, Ole J. Lorenzetti
  • Patent number: 5981499
    Abstract: The invention provides a medicament for topically treating aphthous ulcers in the oral mucosa, and methods of use. The medicament comprises a troche or powder comprising a dry dosage of one or more antibiotics and, preferably, one or more polyvalent metal compounds. The troche or powder is directly applied to the aphthous ulcer and dissolves in saliva, within about 5 to about 15 minutes, thereby directly delivering a supratherapeutic dosage of the antibiotic to the ulcerated oral tissue. Further, in a preferred embodiment the troche/powder directly delivers a therapeutically high concentration of a polyvalent metal compound in suspension to the aphthous ulcer, thereby forming a protective barrier over the ulcerated oral tissue.
    Type: Grant
    Filed: February 20, 1998
    Date of Patent: November 9, 1999
    Assignee: Atlantic Biomed Corporation
    Inventor: Kee Hung Hau
  • Patent number: 5972309
    Abstract: Intra-erythrocytic exogenous bacterial structures or parasites seen by giemsa and phase contrast microscopy in several patients with systemic lupus erythematosus (SLE) and not in controls were identified as bacteria. Treatment of an SLE patient is contemplated with an antibacterial amount of a rifamycin in conjunction with an antibacterial amount of either a macrolide such as clarithromycin or a third generation cephalosporin such as cefpodoxime that is itself more preferably used in conjunction with an adjuvant amount of probenecid.
    Type: Grant
    Filed: August 11, 1998
    Date of Patent: October 26, 1999
    Inventor: Charles A. Kallick
  • Patent number: 5945420
    Abstract: An immunopotentiating and infection protective agent comprising riboflavin and/or a riboflavin derivative, which is safe for the human, animals or the like, an immunopotentiating and infection protective agent comprising riboflavin and/or a riboflavin derivative and (1) proline and/or glutamine, (2) an antibiotic, or (3) a water-soluble polymer or lecithin, which is safe for the human, animals or the like, and a process for the production thereof.
    Type: Grant
    Filed: April 15, 1998
    Date of Patent: August 31, 1999
    Assignee: Eisai Co., Ltd.
    Inventors: Seiichi Araki, Mamoru Suzuki, Masatoshi Fujimoto
  • Patent number: 5858962
    Abstract: Lysostaphin is used to eliminate and cure staphylococcal infections including the cure of mastitis by intramammary infusion. Administration of from 2 mg to 400 mg of lysostaphin to an infected bovine mammary gland eliminates staphylococci, and the reoccurrence common with antibiotic therapy is not observed. Teat-dips containing lysostaphin, mutanolysin and lysozyme can be used as a prophylactic. Synergistic enhancement of the killing effect of lysostaphin is observed when a mild surfactant or penicillin or both is included in the formulation.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: January 12, 1999
    Assignee: Ambi Inc.
    Inventors: Peter Blackburn, June Polak
  • Patent number: 5834424
    Abstract: Compositions of lactoferrin, ovotransferrin or serotransferrin in apo or iron-saturated form are provided which have bacterial anti-invasive properties against Streptococcus pyogenes and Staphylococcus aureus. Methods of treatment of epithelial calls and mucosal membranes are described.
    Type: Grant
    Filed: September 5, 1997
    Date of Patent: November 10, 1998
    Assignee: Gambit International Limited
    Inventors: Piera Valenti, Giovanni Antonini
  • Patent number: 5827543
    Abstract: The subject invention encompasses methods for prevention and treatment of a human or lower animal subject having a urogenital disorder caused or mediated by one or more parasitic protozoa comprising administering to the subject bismuth and one or more antimicrobials. The subject invention also encompasses compositions comprising bismuth and one or more antimicrobials for the prevention and treatment of a human or lower animal subject having a urogenital disorder caused or mediated by one or more parasitic protozoa.
    Type: Grant
    Filed: December 7, 1995
    Date of Patent: October 27, 1998
    Assignee: The Procter & Gamble Company
    Inventor: Jamesina Anne Fitzgerald
  • Patent number: 5795563
    Abstract: Intra-erythrocytic exogenous bacterial structures or parasites seen by giemsa and phase contrast microscopy in several patients with systemic lupus erythematosus (SLE) and not in controls were identified as bacteria. Treatment of an SLE patient is contemplated with an antibacterial amount of a rifamycin in conjunction with an antibacterial amount of either a macrolide such as clarithromycin or a third generation cephalosporin such as cefpodoxime that is itself more preferably used in conjunction with an adjuvant amount of probenecid.
    Type: Grant
    Filed: December 13, 1996
    Date of Patent: August 18, 1998
    Assignee: Sphingomonas Research Partners, L.P.
    Inventor: Charles A. Kallick
  • Patent number: 5783561
    Abstract: The present invention relates to methods of treating gram-positive bacterial infections by administration of a BPI protein product alone, or in combination with an antibiotic. BPI protein product alone has a bactericidal or growth inhibitory effect on selected gram-positive organisms. BPI protein product also increases the susceptibility of gram-positive organisms to antibiotics and can even reverse resistance of gram-positive organisms to antibiotic.
    Type: Grant
    Filed: November 25, 1996
    Date of Patent: July 21, 1998
    Assignee: XOMA Corporation
    Inventors: Arnold Horwitz, Lewis H. Lambert, Jr., Roger G. Little, II
  • Patent number: 5780049
    Abstract: The invention involves pharmaceutical compositions for topical application comprising:(a) a safe and effective amount of a pharmaceutical active; and(b) from about 0.05% to about 5% of a non-ionic polyacrylamide having a molecular wight of from about 1,000,000 to about 30,000,000.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: July 14, 1998
    Assignee: Richardson-Vicks Inc.
    Inventors: George Endel Deckner, Brian Scott Lombardo
  • Patent number: 5776919
    Abstract: The present invention provides antimicrobial compositions, especially compositions comprising an antimicrobial (microbiocidal or microbiostatic) compound and a potentiator of antimicrobial activity. Compositions of the invention combining an antimicrobial compound and a potentiator are able to kill or inhibit the growth of microorganisms using much lower concentrations of the antimicrobial compound. The potentiator also enhances the efficacy of antimicrobial compounds against resistant strains of the microorganism.
    Type: Grant
    Filed: April 5, 1996
    Date of Patent: July 7, 1998
    Assignee: Asahi Kasai Kogyo Kabushiki Kaisha
    Inventors: Masayuki Sukigara, Isao Kubo
  • Patent number: 5760026
    Abstract: Lysostaphin is used to eliminate and cure staphylococcal infections including the cure of mastitis by intramammary infusion. Administration of from 2 mg to 400 mg of lysostaphin to an infected bovine mammary gland eliminates staphylococci, and the reoccurrence common with antibiotic therapy is not observed. Teat-dips containing lysostaphin, mutanolysin and lysozyme can be used as a prophylactic. Synergistic enhancement of the killing effect of lysostaphin is observed when a mild surfactant or penicillin or both is included in the formulation.
    Type: Grant
    Filed: September 9, 1994
    Date of Patent: June 2, 1998
    Assignee: Ambi Inc.
    Inventors: Peter Blackburn, June Polak
  • Patent number: 5750496
    Abstract: A method for controlling infections caused by Cryptosporidium parvum. The method comprises using protease inhibiting compounds, preferably serine protease inhibitors, to inhibit excystation, invasion, and parasite maturation and development. The method is directed to therapeutic treatment of mammals, such as humans, exposed to C. parvum, and additionally as a prophylactic treatment in immunocompromised subjects at high risk for contracting cryptosporidiosis.
    Type: Grant
    Filed: August 12, 1996
    Date of Patent: May 12, 1998
    Assignee: Utah State University
    Inventors: John R. Forney, Shiguang Yang, Mark C. Healey
  • Patent number: 5747483
    Abstract: Penem derivatives of general formula (I), below, and pharmaceutically acceptable salts thereof are disclosed. ##STR1## wherein: R.sub.1 is H, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.7 cycloalkyl, or an optionally protected C.sub.1 -C.sub.6 hydroxyalkyl; R.sub.2 is a free or esterified carboxyl group or a carboxylate anion; R.sub.3 is H or C.sub.1 -C.sub.6 alkyl; R.sub.4 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 mercaptoalkyl, C.sub.1 -C.sub.6 aminoalkyl, C.sub.1 -C.sub.6 alkyl substituted by a quaternary ammonium group, C.sub.1 -C.sub.6 carboxyalkyl, cycloalkyl, aryl, arylalkyl, heterocyclyl-alkyl optionally substituted, saturated or unsaturated heterocycle, or R.sub.3 and R.sub.4 are linked together to form a heterocyclic ring having 3-7 atoms; R.sub.5 and R.sub.6 independently are H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 mercaptoalkyl, C.sub. -C.sub.6 aminoalkyl, alkenyl, cycloalkyl, aryl, arylalkyl, alkylaryl, heterocyclyl-alkyl, C.sub.
    Type: Grant
    Filed: March 17, 1995
    Date of Patent: May 5, 1998
    Assignees: A. Menarini Industrie Farmaceutiche Riunite, Istituto Lusofarmaco D'Italia
    Inventors: Maria Altamura, Federico Maria Arcamone, Enzo Perrotta, Vittorio Pestellini, Piero Sbraci, Giuseppe Cascio
  • Patent number: 5741782
    Abstract: An antibiotic cocktail for sterilizing tissue comprising amphotericin B and fluconazole as antifungal agents and a plurality of antibacterial agents. The agents are present in amounts effective to substantially inhibit fungal and bacterial growth while substantially maintaining the viability of the tissue. Also, a method of sterilizing a tissue comprising contacting the tissue with the antibiotic cocktails of the invention at a temperature and for a period of time effective to substantially inhibit fungal and bacterial growth while substantially maintaining the viability of the tissue.
    Type: Grant
    Filed: March 29, 1996
    Date of Patent: April 21, 1998
    Assignee: Cryolife, Inc.
    Inventors: Kelvin G.M. Brockbank, Steven Goldstein, Chigoke Adoma, Judith K. Sheldon, Patti E. Dawson
  • Patent number: 5712268
    Abstract: There are described pharmaceutical compositions comprising(a) compounds of the formula ##STR1## in which R signifies lower alkoxycarbonyl, lower alkoxy-carbonylamino, the acyl residue of an .alpha.- or .beta.-amino acid or a residue of the general formulaQ--X--Y-- (a)wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulphur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear "spacer" with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulphur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulphur, and Y represents one of the groups --CO--, --CS--, --CONH-- and (where X contains neither sulphur nor carbonyl as a terminal component) --SO.sub.2 --; and in which R.sup.1 and R.sup.2 together signify a group of the formula ##STR2## wherein A represents hydrogen or a residue which is usable in the 3-position of cephalosporin antibiotics, and in which R.sub.
    Type: Grant
    Filed: April 12, 1995
    Date of Patent: January 27, 1998
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christian Hubschwerlen, Robert Charnas, Ingrid Heinze, Klaus Gubernator
  • Patent number: 5698577
    Abstract: There are described pharmaceutical compositions comprising(a) compounds of the formula ##STR1## in which R signifies lower alkoxycarbonyl, lower alkoxy-carbonylamino, the acyl residue of an .alpha.- or .beta.-amino acid or a residue of the general formulaQ--X--Y-- (a)wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulphur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear "spacer" with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulphur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulphur, and Y represents one of the groups --CO--, --CS--, --CONH-- and (where X contains neither sulphur nor carbonyl as a terminal component) --SO.sub.2 --; and in which R.sup.1 signifies hydrogen, halogen, carbamoyloxy, lower alkanoyloxy or a group of the formula --S--Het, wherein Het represents a 5- or 6-membered heteroaromatic group containing nitrogen, sulphur and/or oxygen, and R.sup.
    Type: Grant
    Filed: April 12, 1995
    Date of Patent: December 16, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christian Hubschwerlen, Robert Charnas, Ingrid Heinze, Klaus Gubernator
  • Patent number: 5691385
    Abstract: .beta.-Phenethanolamines are effective in promoting growth and improving feed efficiency and leanness in animals.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: November 25, 1997
    Assignee: Eli Lilly and Company
    Inventors: David B. Anderson, Klaus K. Schmiegel, Edward L. Veenhuizen
  • Patent number: 5681593
    Abstract: Psoriasis, seborrheic dermatitis and eczema are treated by oral administration of inorganic nickel compound(s), with or without inorganic bromide(s). In an especially preferred embodiment, the nickel compound used to treat these diseases is NiBr.sub.2.
    Type: Grant
    Filed: July 18, 1995
    Date of Patent: October 28, 1997
    Inventors: Steven A. Smith, Lorraine J. Smith
  • Patent number: 5674858
    Abstract: The use is described of both (i) ranitidine bismuth citrate and (ii) one or more Helicobacter pylori-inhibiting antibiotics in treating or preventing gastrointestinal disorders.Pharmaceutical compositions containing both (i) and (ii) and methods for the preparation of pharmaceutical compositions containing (i) and (ii) are also described.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: October 7, 1997
    Assignee: Glaxo Group Limited
    Inventor: Andrew Alexander McColm
  • Patent number: 5650394
    Abstract: The present invention provides a method of diagnosing and treating a pregnant female at risk for impending preterm delivery. The method comprises the step of diagnosing imminent preterm delivery by testing with a method that has a sensitivity of at least 80% and a specificity of at least 80%, or by testing for fetal fibronectin in the female's vaginal or cervical secretions. If imminent preterm delivery is indicated by the test, the next step comprises administering to the female a combination of a tocolytic agent, at least one urinastatin-like compound, and at least one antibiotic. Also provided is a pharmaceutical composition of MGMTSRYFYNGTSMA (SEQ ID NO:1), RAFIQLWAFDAVKGK (SEQ ID NO:2) and an antibiotic.
    Type: Grant
    Filed: November 4, 1993
    Date of Patent: July 22, 1997
    Assignee: Adeza Biomedical
    Inventors: Toshihiko Terao, Naohiro Kanayama, David Casal
  • Patent number: 5643902
    Abstract: A formulation comprising amoxycillin or a veterinarily acceptable derivative thereof, clavulanic acid or a veterinarily acceptable derivative thereof, and a veterinarily acceptable carrier is used in the treatment of farrowing fever and/or bacterial pneumonia in pigs.
    Type: Grant
    Filed: March 16, 1994
    Date of Patent: July 1, 1997
    Assignee: Pfizer Inc.
    Inventor: Victor Charles Cracknell
  • Patent number: 5637579
    Abstract: The present invention discloses compounds having the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is --COR.sup.4, --CN, --CH.sub.2 R.sup.5, halogen, --CH.dbd.CHR.sup.6 or Q and the other is hydrogen or lower alkyl or both R.sup.1 and R.sup.2 together form a .gamma.-lactam ring,R.sup.3 is hydrogen, lower alkyl, aryl-alkyl, allyl or a residue which is cleavable in vivo,R.sup.4 is hydrogen, lower alkyl, lower alkoxy, benzyloxy, amino, lower alkylamino or lower alkyl-lower alkoxyamino,R.sup.5 is hydroxy, --OCONHR.sup.7, --OCONH.sub.2 or a five- or six-membered hetero-aromatic ring which contains N,S and/or O and which is linked via a nitrogen atom,R.sup.6 is --CN or CHO,R.sup.7 is --COCH.sub.2 Cl,Q is a five- or six-membered hetero-aromatic ring which contains N, S and/or O andn is 0, 1 or 2,and the pharmaceutically compatible salts thereof.These compounds are good .beta.-lactamase inhibitors. They can be used for the prevention or treatment of bacterial infections, optionally together with a .beta.
    Type: Grant
    Filed: August 22, 1994
    Date of Patent: June 10, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christian Hubschwerlen, Hans Richter, Jean-Luc Specklin
  • Patent number: 5599795
    Abstract: A new method for the prevention and treatment of Idiopathic inflammatory Bowel Disease (IIBD), including Crohn's Disease and Ulcerative Colitis, in human patients is provided. The key steps include sterilizing the intestinal tract with multiple antibiotics to kill the pre-existing bacterial flora, and replacing the latter with different, select, well-characterized bacteria taken from normal humans. The new microflora serve to generate more normal metabolic and immune responses, remitting thereby the IIBD.
    Type: Grant
    Filed: August 19, 1994
    Date of Patent: February 4, 1997
    Inventors: Michael McCann, Richard S. Abrams
  • Patent number: 5523288
    Abstract: The present invention relates to methods and compositions for treating gram-negative bacterial infections, using BPI protein products. Co-treatment, or concurrent administration, of BPI protein product with an antibiotic in treatment of gram-negative bacterial infections improves the therapeutic effectiveness of the antibiotic, including increasing antibiotic susceptibility of gram-negative bacteria and reversing resistance of the bacteria to antibiotics.
    Type: Grant
    Filed: September 22, 1994
    Date of Patent: June 4, 1996
    Assignee: Xoma Corporation
    Inventors: Jonathan Cohen, Ada H. C. Kung, Lewis H. Lambert, Jr., Roger G. Little, II
  • Patent number: 5506225
    Abstract: Antibiotic penem compounds are represented by the following formula: ##STR1## wherein R represents a physiological-hydrolyzable, ester-forming group. The physiologically hydrolyzable, ester-forming group useful in the penem compound of the present invention means a group which can be removed easily by in vivo hydrolysis, such as an acetyloxymethyl, 1-(acetyloxy)ethyl, pivaloyloxymethyl, 1-(ethoxycarbonyloxy)ethyl, 1-(isopropyloxycarbonyloxy)ethyl, 1-(cyclohexyloxycarbonyloxy)ethyl or 3-phthalidyl group. Antibiotic compositions for oral administration are also described.
    Type: Grant
    Filed: February 19, 1993
    Date of Patent: April 9, 1996
    Assignee: Suntory Limited
    Inventors: Hiromitsu Iwata, Takashi Nakatsuka, Rie Tanaka, Masaji Ishiguro
  • Patent number: 5492903
    Abstract: Crystalline acetoxymethyl and pivaloyloxymethyl esters of (+)-(5R, 6S)-6-[(R)-1-hydroxyethyl]-3-(3-pyridyl)-7-oxo-4-thia-1-azabicyclo-[3.2.0] hept-2-ene-carboxylic acid can be obtained by adding a poor solvent to a solution of acetoxymethyl or pivaloyloxymethyl ester of (+)-(5R, 6S)-6-[(R)-1-hydroxyethyl]-3-(3-pyridyl)-7-oxo-4-thia-1-azabicyclo-[3.2.0] hept-2-ene-carboxylic acid in a good solvent. The crystalline penem compounds obtained show improved stability and are useful antibacterial agents.
    Type: Grant
    Filed: August 26, 1993
    Date of Patent: February 20, 1996
    Assignee: Takeda Chemical Industries Ltd.
    Inventors: Yoshiharu Maeda, Yukio Ishibashi, Tetsuya Tsukamoto, Masahiro Mizuno
  • Patent number: 5491139
    Abstract: Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked, by a non-ester linking moiety, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula: ##STR1## wherein (1) R.sup.3, R.sup.4, and R.sup.5, together with bonds "a" and "b", form any of a variety of lactam-containing moieties similar to those known in the art to have antimicrobial activity;(2) A, R.sup.6, R.sup.7, and R.sup.8 form any of a variety of quinolone or naphthyridine structures similar to those known in the art to have antimicrobial activity; and(3) Y, together with R.sup.5, form a variety of non-ester linking moieties between the lactam-containing moiety and the quinolone moiety.
    Type: Grant
    Filed: April 6, 1994
    Date of Patent: February 13, 1996
    Assignee: The Procter & Gamble Company
    Inventors: Thomas P. Demuth, Jr., Ronald E. White
  • Patent number: 5484809
    Abstract: The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn-glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of zaxol and taxol-related compounds. Potency of the lipid prodrugs is comparable to that of the corresponding nonderivatized drugs. In a preferred embodiment, taxol or substituted taxol is covalently bound to a phospholipid.
    Type: Grant
    Filed: December 14, 1994
    Date of Patent: January 16, 1996
    Assignee: Vestar, Inc.
    Inventors: Karl Y. Hostetler, Nagarajan C. Sridhar
  • Patent number: 5478819
    Abstract: A method of and composition for treating a Helicobacter pylori infection in a mammal. The method comprises administering to said mammal orally a therapeutically effective amount of a Helicobacter pylori eradicating antibiotic and a phospholipid. The composition comprises a Helicobacter pylori eradicating antibiotic and a phospholipid.
    Type: Grant
    Filed: June 23, 1993
    Date of Patent: December 26, 1995
    Assignee: Simo Tarpila
    Inventors: Simo Tarpila, Anneli Kivinen
  • Patent number: 5474993
    Abstract: The present invention is related to compounds which inhibit pancreatic cholesterol esterase. The compounds have the formula: ##STR1## wherein R.sup.1 is H or C.sub.1-6 alkyl;R.sup.2 is H or C.sub.1-6 alkyl;R.sup.3 is H or C.sub.1-6 alkyl;X is CHR.sup.6, S or O;R.sup.6 is H or C.sub.1-6 alkyl;R.sup.4 is a hydrophobic moiety; and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: June 14, 1994
    Date of Patent: December 12, 1995
    Assignee: Sterling Winthrop, Inc.
    Inventors: Byron Rubin, Kenneth C. Mattes, Terrence C. Mungal
  • Patent number: 5464616
    Abstract: A 6.beta.-substituted penicillanic acid of the formula XII: ##STR1## or a pharmaceutically acceptable salt or ester thereof, whereinA and B are each hydrogen wherein the carbon atoms to which A and B are attached are linked by a single bond, or A and B together form a bond, wherein the carbon atoms to which A and B are attached are linked by a double bond,R1 is selected from the group consisting of a) hydrogen, b) a pharmaceutically acceptable salt and c) a pharmaceutically acceptable group selected from the group consisting of C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, C.sub.3-10 cycloalkyl, C.sub.
    Type: Grant
    Filed: August 4, 1994
    Date of Patent: November 7, 1995
    Assignee: Synphar Laboratories, Ind.
    Inventors: Kazuharu Noguchi, Ronald G. Micetich, Mohsen Daneshtalab
  • Patent number: 5460813
    Abstract: The invention relates to various methodologies for diagnosing Kawasaki syndrome. Various bacteria, including TSST-1 producing Staphylococcus aureus, and SPEB and SPEC producing streptococcus have been found to be indicative of the pathological condition. Also described is a Kawasaki syndrome implicated isolate of S. aureus, and therapeutic methodologies for preventing treating the condition. These involve the administration of anti-TSST-1 agents which are not gamma globulin.
    Type: Grant
    Filed: April 5, 1993
    Date of Patent: October 24, 1995
    Assignee: National Jewish Center for Immunology and Respiratory Medicine
    Inventors: Donald Leung, Patrick Schlievert, Cody Meissner, David Fulton, Brian Kotzin
  • Patent number: 5433954
    Abstract: Psoriasis, seborrheic dermatitis and eczema are treated by oral administration of inorganic nickel compound(s), with or without inorganic bromide(s). In an especially preferred embodiment, the nickel compound used to treat these diseases is NiBr.sub.2.
    Type: Grant
    Filed: December 3, 1992
    Date of Patent: July 18, 1995
    Inventors: Steven A. Smith, Lorraine J. Smith
  • Patent number: 5416208
    Abstract: Antibacterial penems of formula (I), where R represents a hydrogen atom or a hydroxy protecting group, are prepared by reacting a .beta.-lactam of formula (II) with an oxalyl halide in an inert solvent in the presence of an organic or inorganic base or an acid scavenger to produce a compound of formula (III), wherein X is a halogen atom, treating the resultant compound of formula (III) with a 1,3-dioxolen-2-one of formula (IV), wherein Y is a hydroxy group, in the presence of molecular sieves or an organic or inorganic base to produce a compound of formula (V), and cyclizing the compound of formula (V) in the presence of a trialkylphosphite to provide the penems of formula (I).
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: May 16, 1995
    Assignee: Farmitalia Carlo Erba S r l
    Inventors: Ettore Perrone, Marco Alpegiani, Franco Zarini, Giuseppe Mazzini, Giovanni Franceschi
  • Patent number: 5411947
    Abstract: The oral delivery of many classes of drugs is facilitated by converting drugs having suitable functional groups to 1-O-alkyl-, 1-O-acyl-, 1-S-acyl, and 1-S-alkyl-sn-glycero-3-phosphate derivatives. The method confers the ability to be absorbed through the digestive tract to drugs that are not orally bioavailable in the non-derivatized state, and enhances the effectiveness of drugs that are poorly absorbed or rapidly eliminated. The method provides orally bioavailable lipid prodrugs of pharmaceutical compounds having diverse physiological activities, including anticancer and antiviral agents, anti-inflammatory agents, antihypertensives and antibiotics. Potency of the lipid prodrugs is comparable to that of the corresponding non-derivatized drugs.
    Type: Grant
    Filed: December 16, 1992
    Date of Patent: May 2, 1995
    Assignee: Vestar, Inc.
    Inventors: Karl Y. Hostetler, Raj Kumar
  • Patent number: 5350680
    Abstract: A cephalosporinase testing agent comprising a cephalosporin antibiotic, a penicillinase inhibitor in an amount of 20% by weight or less based on the weight of the cephalosporin-antibiotic, and a pH indicator which may be bromcresol purple is provided. A cephalosporinase producing bacteria can be judged by smearing a sample containing bacteria to be tested on the testing agent and observing the color tone change. According to this agent, cephalosporinase-active penicillinase producing bacteria are judged cephalosporinase-negative owing to the action of the penicillinase inhibitor, which may be clavulanic acid. Therefore, since only cephalosporinase producing bacteria are judged cephalosporinase-positive, this agent enables error free judgment.
    Type: Grant
    Filed: February 2, 1993
    Date of Patent: September 27, 1994
    Assignee: Showa Yakuhin Kako Co., Ltd.
    Inventors: Matsuhisa Inoue, Akira Sakai
  • Patent number: 5302588
    Abstract: A crystalline form of (5R,6S)-2-carbamoyloxymethyl-6-[(1R)-hydroxyethyl]-2-penem-3-carboxylic acid incorporates two molecules of water per molecule of the acid and is useful as an antibacterial agent.
    Type: Grant
    Filed: June 16, 1992
    Date of Patent: April 12, 1994
    Assignee: Farmitalia Carlo Erba
    Inventors: Carlo Battistini, Roberto Bianchini, Stefano del Nero, Pierluigi Griggi, Sergio Vioglio