Abstract: Stable pharmaceutical formulations and methods of making same are provided. In a general embodiment, the present disclosure provides a method of making a stable pharmaceutical formulation comprising adding one or more vitrifying additives to an aqueous pharmaceutical solution to raise the glass transition temperature of the aqueous pharmaceutical solution. The aqueous pharmaceutical solution can be cooled to a temperature of about ?50° C. to about ?10° C. The vitrifying additive enhances the formation of a glass or amorphous solid of the aqueous pharmaceutical solution at cryogenic temperatures (?50 to ?10° C.), and the pharmaceutical formulation can be thawed to liquid form and administered to a mammalian subject.
Type:
Application
Filed:
May 8, 2009
Publication date:
November 19, 2009
Applicants:
Baxter International Inc., Baxter Healthcare S.A.
Inventors:
JAMES E. KIPP, JOSEPH CHUNG TAK WONG, LAKSHMY NAIR, REAGAN MILLER, BARRETT E. RABINOW
Abstract: An orally administrable antibacterial agent which contains as an active ingredient a carbapenem compound represented by the formula [1] below, wherein R0 represents hydrogen atom or the like; R1 represents C1-C3 alkyl substituted by hydroxyl group or the like; R represents hydrogen atom or a group which regenerates a carboxyl group by hydrolysis in a living body; L represents a single bond, methylene, —OCH2(CO)— or the like; and Het represents a group represented by the following formula [2], wherein m and n independently represent 0 or 1; A and B independently represent methylene, carbonyl or the like; Y represents methylene, ethylene, oxygen atom, —OCH2—, —NRaCH2— (wherein Ra represents hydrogen atom, optionally substituted C1-C4 alkyl group or the like) or the like.
Abstract: Compounds of formula (I): (wherein variable groups are as defined within) pharmaceutically acceptable salts, solvates, solvates of such salts and prodrugs thereof and their use as cholesterol absorption inhibitors for the treatment of hyperlipidaemia are described.
Type:
Grant
Filed:
July 1, 2003
Date of Patent:
December 30, 2008
Assignee:
AstraZeneca AB
Inventors:
Ingemar Starke, Mikael Ulf Johan Dahlstrom, Ann-Margret Lindqvist, Mats Peter Nordberg, Tore Skjaret, Malin Anita Lemurell
Abstract: Carbapenem compounds represented by the general formula [1] or pharmaceutically acceptable salts thereof: wherein R1 is C1-C3 alkyl or hydroxylated C1-C3 alkyl, R is hydrogen atom or a group which is hydrolyzed in vivo into a carboxy group, and G is a group represented by one of the formulae [G1], [G2], and [G3].
Type:
Grant
Filed:
April 6, 2004
Date of Patent:
December 23, 2008
Assignee:
Dainippon Sumitomo Pharma Co., Ltd.
Inventors:
Makoto Sunagawa, Akira Sasaki, Seiji Hori
Abstract: A compound or its pharmaceutically acceptable salt represented by the following formula: The invention is a carbapenem compound which has a potent antibacterial activity over a broad range of Gram negative and Gram positive bacteria, especially penicillin-resistant Streptococcus pneumoniae (PRSP) which has been isolated at an elevated frequency in recent years and thus causes a serious clinical problem, and Haemophilus influenzae which has acquired resistance against the existing ?-lactam antibiotics over a wide scope due to penicillin-binding protein (PBP) mutations such as ?-lactamase non-producing ampicillin-resistant (BLNAR) Haemophilus influenzae, and has excellent oral absorbability.
Abstract: Carbapenem compounds having a substituted phenyl or a substituted thienyl directly attached to the 3-position of carbapenem nucleus as represented by the formula: wherein Ring E is benzene ring or thiophene ring; R1 is optionally OH-substituted C1-3 alkyl; R2 and R3 represent each H, optionally substituted lower alkyl, etc.; R is H, or a group which is hydrolyzed in the living body to regenerate a carboxyl group, etc.; X is O or S; and Y represents H, lower alkyl, etc., or pharmaceutically acceptable salts thereof and medicaments containing said compound as the active ingredient.
Abstract: An objective of the present invention is to provide carbapenem derivatives which have strong antibiotic activity also against MRSA, PRSP, Influenzavirus, and ?-lactamase producing bacteria and are stable to DHP-1. The carbapenem derivatives according to the present invention are compounds represented by formulae (I) and (II) or pharmaceutically acceptable salts thereof: wherein R1 represents H or methyl, R2 and R3 each independently represent H; halogen; substituted or unsubstituted alkyl; cycloalkyl; substituted or unsubstituted alkylcarbonyl; carbamoyl; substituted or unsubstituted aryl; substituted or unsubstituted alkylthio; morpholinyl; alkylsulfonyl; or formyl, n is 0 (zero) to 4, and Hy represents a substituted or unsubstituted monocyclic or bicyclic heterocyclic group.
Abstract: Methods for Cystic Fibrosis disease assessment in an individual comprise detecting the presence or absence of outer membrane protein in a sample from an individual or the methods comprise detecting the presence or absence of outer membrane protein antibodies in a sample from an individual. Methods for treating anaerobic Pseudomonas aeruginosa biofilms in Cystic Fibrosis disease comprise detecting the presence of outer membrane protein in a sample from an individual; and selecting a therapy regimen for the individual based on the presence of OprF, wherein the anaerobic Pseudomonas aeruginosa biofilms in Cystic Fibrosis disease are treated by the therapy regimen or the methods comprise detecting the presence of outer membrane protein antibodies in a sample from an individual; and selecting a therapy regimen for the individual based on the presence of OprF antibodies; wherein the anaerobic Pseudomonas aeruginosa biofilms in Cystic Fibrosis disease are treated by the therapy regimen.
Type:
Application
Filed:
October 20, 2003
Publication date:
December 30, 2004
Inventors:
Daniel J. Hassett, George M. Hilliard, San-Sun Yoon
Abstract: Bacterial infections may be treated using a high dosage regimen of amoxicillin and potassium clavulanate. Preferably, the dosage is provided by a bilayer tablet.
Type:
Application
Filed:
June 17, 2004
Publication date:
December 2, 2004
Applicant:
Beecham Pharmaceutials (Pte) Limited
Inventors:
Kevin H. Storm, Creighton P. Conley, John A. Roush
Abstract: An objective of the present invention is to provide carbapenem derivatives which have potent antibiotic activity against MRSA, PRSP, Influenzavirus, and &bgr;-lactamase-producing bacteria and are stable against DHP-1. The compounds according to the present invention are compounds represented by formula (I) or pharmaceutically acceptable salts thereof:
wherein R1 represents H or methyl; R2 and R3 each independently represent H, halogen, lower alkyl or the like; R4 represents optionally substituted lower alkylthio or the like; and R5 represents optionally substituted lower alkyl or the like.
Abstract: Administration of &bgr;-Lactam compounds, including &bgr;-lactam antibiotics and &bgr;-lactamase inhibitors provides significant neurotropic effects in warm-blooded vertebrates evidenced inter alia by anxiolytic and anti-aggressive behavior modification and enhanced cognition. Therapeutic methods for using such compounds and their pharmaceutical formulations are described.
Abstract: The present invention provides methods and compositions useful for preventing bacteremia by decolonizing the intestinal tract of a patient. Although the present invention is useful for preventing bacteremia by any Gram-positive bacteria, it is particularly useful against antibiotic-resistant bacteria, such as vancomycin-resistant Enterococcus (VRE), methicillin-resistant Staphylococcus aureus (MRSA), glycopeptide intermediary susceptible Staphylococcus aureus (GISA), and penicillin-resistant Streptococcus pneumoniae (PRSP). Decolonization therapy using the methods and compositions of this invention are also useful for preventing a Gram-negative bacteremia.
Abstract: Provided, among other things, is a method of treating or ameliorating pulmonary infection in a cystic fibrosis patient comprising pulmonary administration of an effective amount of a liposomal/complexed antiinfective to the patient, wherein the (i) administrated amount is 50% or less of the comparative free drug amount, or (ii) the dosing is once a day or less, or (iii) both.
Abstract: The present invention relates to novel Death Domain Containing Receptor-5 (DR5) proteins which are members of the tumor necrosis factor (TNF) receptor family, and have now been shown to bind TRAIL. In particular, isolated nucleic acid molecules are provided encoding the human DR5 proteins. DR5 polypeptides are also provided as are vectors, host cells and recombinant methods for producing the same. The invention further relates to screening methods for identifying antagonists and antagonists of DR5 activity.
Type:
Application
Filed:
February 10, 2004
Publication date:
July 22, 2004
Applicant:
Human Genome Sciences, Inc.
Inventors:
Jian Ni, Reiner L. Gentz, Guo-Liang Yu, Craig A. Rosen
Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.
Type:
Application
Filed:
June 20, 2003
Publication date:
July 15, 2004
Inventors:
William Fenical, Paul Jensen, Tracy Mincer, Robert H.R. Feling
Abstract: A pharmaceutical composition comprising an active ingredient and clavulanate wherein the clavulanate is in the form of granulated and hydrophobised particles; and intermediates in its preparation, e.g. clavulanate is granulated and/or hydrophobised form.
Type:
Application
Filed:
February 12, 2004
Publication date:
July 8, 2004
Inventors:
Otto Damon, Herwig Jennewein, Thomas Lentner, Franz Xaver Schwarz, Robert Veigl
Abstract: The invention features novel RNase P molecules and nucleic acids encoding the same. Methods for discovery of antimicrobial compounds are also featured.
Type:
Application
Filed:
March 1, 2001
Publication date:
July 1, 2004
Inventors:
Venkat Gopalan, Milan Jovanovic, Paul S. Eder, Tony Giordano, Gordon D. Powers, K. Asish Xavier
Abstract: Carbapenem compounds having a substituted phenyl or a substituted thienyl directly attached to the 3-position of carbapenem nucleus as represented by the formula: 1
Abstract: The present invention provides a cored tablet comprising a core layer containing clavulanate, and an outer layer containing amoxicillin and surrounding the core layer, and a method for preparing the same.
Type:
Application
Filed:
July 29, 2003
Publication date:
February 5, 2004
Applicant:
Daewoong Pharm Co., Ltd., Republic of Korea
Abstract: Administration of clavulanic acid and related compounds at low dosages provides significant neurotropic effects in warm-blooded vertebrates evidenced inter alia by anxiolytic and anti-aggressive behavior and enhanced cognition believed to be mediated by inhibition of neurogenic enzyme activity. Therapeutic methods for using such compounds and their pharmaceutical formulations are described.
Abstract: Disclosed is a novel carbapenem derivative having a substituted imidazo[5,1-b]thiazole group at the 2-position on the carbapenem ring have high anti microbial activities against &bgr;-lactamase producing bacteria, MRSA, resistant-Pseudomonas aeruginosa, PRSP, enterococci, and influenza, and high stabilities to DHP-1.
Abstract: This invention relates to novel substituted succinic acid metallo-&bgr;-lactamase inhibitors which are useful potentiators of &bgr;-lactam antibiotics.
Type:
Application
Filed:
January 9, 2003
Publication date:
November 6, 2003
Inventors:
James M. Balkovec, Mark L. Greenlee, Steven H. Olson, Gregory P. Rouen
Abstract: Co-administration of a lysostaphin or other anti-staphylococcal agent which cleaves cross-links of peptidoglycans of staphylococci cell walls such as lysostaphin and an antibiotic effective against staphylococci due to antibiotic activity mediated by cell-wall activity is effective against staphylococcal infection, even staphylococci that may be resistant to one or other of lysostaphin or the cell-wall active antibiotic. Co-administration simultaneously suppresses the generation of antibiotic-resistant mutant strains. Effective cell-wall active antibiotics include &bgr;-lactams and glycopeptides.
Type:
Application
Filed:
April 16, 2003
Publication date:
October 23, 2003
Inventors:
Michael Climo, Ellen Murphy, Gordon Archer
Abstract: The present invention relates to novel drugs which may be used in combating infectious micro-organisms, particularly bacteria.
Type:
Application
Filed:
March 27, 2002
Publication date:
October 23, 2003
Inventors:
Peter E. Nielsen, Liam Good, Henrik Frydenlund Hansen, Frederik Beck, Leila Malik, Carsten Schou, Margit Wissenbach, Birgit Kjaeldgaard Giwercman
Abstract: The present invention provides a unique approach for the diagnosis and management of infections by Chlamydia species, particularly C. pneumoniae. The invention is based, in part, upon the discovery that a combination of agents directed toward the various stages of the chlamydial life cycle is effective in substantially reducing infection. Products comprising combination of antichlamydial agents, novel compositions and pharmaceutical packs are also described.
Type:
Application
Filed:
March 19, 2002
Publication date:
October 16, 2003
Inventors:
William M. Mitchell, Charles W. Stratton
Abstract: The invention relates to the individualization of therapy on the basis of a phenotypic profile of an individual. More specifically, the present invention relates to the use of metabolic phenotyping for the individualization of treatment with antibiotic agents.
Abstract: The present invention relates to methods for treating a subject suffering from infection with Mycobacteria, such as M. leprae or M. tuberculosis comprising administering to the subject a composition comprising a bactericidal/permeability-inducing (BPI) protein product alone or in combination with administration of an anti-Mycobacterial antibiotic.
Abstract: The present invention provides a unique approach for the diagnosis and management of infections by Chlamydia species, particularly C. pneumoniae. The invention is based, in part, upon the discovery that a combination of agents directed toward the various stages of the chlamydial life cycle is effective in substantially reducing infection. Products comprising combination of antichlamydial agents, novel compositions and pharmaceutical packs are also described.
Type:
Application
Filed:
March 19, 2002
Publication date:
September 11, 2003
Inventors:
William M. Mitchell, Charles W. Stratton
Abstract: The present invention relates to novel Death Domain Containing Receptor (DR3 and DR3-V1) proteins that are members of the tumor necrosis factor (TNF) receptor family. In particular, isolated nucleic acid molecules are provided encoding the human DR3 and DR3-V1 proteins. DR3 and DR3-V1 polypeptides are also provided, as are vectors, host cells and recombinant methods for producing the same. The invention further relates to screening methods for identifying agonists and antagonists of DR3 and DR3-V1 activity.
Type:
Application
Filed:
July 5, 2002
Publication date:
September 11, 2003
Applicant:
Human Genome Sciences, Inc.
Inventors:
Guo-Liang Yu, Jian Ni, Reiner L. Gentz, Patrick J. Dillon
Inventors:
Eric Hunt, Steven Coulton, Jeremy David Hinks, Stephen Frederick Moss, Stephen Christopher Martin Fell, Alfred John Eglington, George Burton
Abstract: Neurotherapeutically pharmaceutical effective compositions are prepared using carboxypeptidase E inhibitors. One class of carboxypeptidase E inhibitors found to exhibit significant neurotropic activity are &bgr;-lactam compounds, particularly penam and cephem &bgr;-lactam antibiotics and non-antibiotic derivatives thereof.
Abstract: Disclosed is a novel carbapenem derivative having a substituted imidazo[5,1-b]thiazole group at the 2-position on the, carbapenem ring have high anti-microbial activities against &bgr;-lactamase producing bacteria, MRSA, resistant-Pseudomonas aeruginosa, PRSP, enterococci, and influenza, and high stabilities to DHP-1.
Abstract: The present invention relates to a topical antimicrobial composition containing an antimicrobial complex that provides sustained antimicrobial disinfecting action upon contact with microorganisms for prolonged periods, without the necessity for reapplication. The topical antimicrobial composition provides both initial and residual contact-killing disinfecting activity, and does not release its antimicrobial components into contacting liquids at levels that result in solution disinfection.
Type:
Application
Filed:
September 9, 1999
Publication date:
August 7, 2003
Inventors:
SAMUEL P. SAWAN, SUNDAR SUBRAMANYAM, ALEXANDER V. YURKOVETSKIY, GURUSAMY MANIVANNAN, MICHAEL GOLDBLATT
Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
Type:
Grant
Filed:
June 3, 1998
Date of Patent:
August 5, 2003
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Yong Mi Choi-Sledeski, Henry W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong
Abstract: The present invention relates to a new composition, use and method to improve the cure of infections caused by antibiotic resistant microbial pathogens, in particular beta-lactam resistant microorganisms. Lactoferrin (LF) or Lactoferricin (LFC) can be administrated alone or in combination with antibiotic to affect growth, physiology and morphology of targeted microorganism. Lactoferrin increase susceptibility and can reverse resistance of microorganism to antibiotics.
Type:
Application
Filed:
September 23, 2002
Publication date:
July 17, 2003
Inventors:
Moussa S. Diarra, Pierre Lacasse, Denis Petitclerc
Abstract: Novel coamoxiclav formulations are described, having reduced weight compared to existing formulations, as well as formulations comprising amoxycillin and potassium clavulanate in a ratio of 8:1 and formulations prepared from granulates of amoxycillin and granulates of amoxycillin and clavulanate.
Abstract: A tablet formulation comprising amoxycillin and potassium clavulanate, in a weight ratio amoxycillin:clavulanate between 1:1 to 20:1 (expressed as the weight of the corresponding parent acids) inclusive, wherein the amoxycillin is sodium amoxycillin or a mixture of sodium amoxycillin and amoxycillin trihydrate and the tablet has an enteric film coating is of use in treating bacterial infection.
Abstract: A method of use of clavulanate to enhance the antibacterial activity of an antibacterial compound against microorganisms having an antibiotic resistance mechanism other than &bgr;-lactans enzyme mediated resistance. Pharmaceutical formulations and methods of use which exploit this method.
Type:
Application
Filed:
December 17, 2002
Publication date:
June 12, 2003
Applicant:
SmithKline Beecham p.l.c.
Inventors:
Gillian Marjory Smith, Christine Elaine Thorburn, Karen Hazel Abbott, Tim Neil Brown
Abstract: Nitrate salts of antimicrobial agents for the preparation of antimicrobial medicaments, specifically antiviral, antifungal and antibacterial medicaments.
Abstract: The present invention relates to the use of endotoxin neutralizing protein (ENP) and derivatives thereof as stand alone microbial inhibitors or as synergistic enhancers of antibiotics and preservatives. Compositions comprising ENP or alone or in combination with an antibiotic may be used to prevent or treat gram-negative bacterial infections, endotoxemia, septic shock, gram-positive bacterial infections, yeast infections and fungal infections.
Abstract: The present invention relates to carbapenems and provides a compound of the formula (I):
or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein:
R1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;
R2 is hydrogen or C1-4alkyl;
R3 is hydrogen or C1-4alkyl;
R4 and R5 are the same or different and are selected from hydrogen, halo, cyano, C1-4alkyl, nitro, hydroxy, carboxy, C1-4alkoxy, C1-4alkoxycarbonyl, aminosulphonyl, C1-4alkylaminosulphonyl, di-C1-4-alkylaminosulphonyl, carbamoyl, C1-4alkylcarbamoyl, di-C1-4 alkylcarbamoyl, trifluoromethyl, sulphonic acid, amino, C1-4alkylamino, di-C1-4alkylamino, C1-4alkanoylamino, C1-4alkanoyl(N—C1-4alkyl)amino, C1-4alkanesulphonamido and C1-4alkylS(O)n— wherein n is zero; one or two:
with the proviso that there is no hydroxy or carboxy substituent in a position ortho to the link to —NR3—.
Type:
Grant
Filed:
February 13, 2001
Date of Patent:
February 18, 2003
Assignee:
Zeneca Ltd.
Inventors:
Michael John Betts, Gareth Morse Davies, Michael Lingard Swain
Abstract: An objective of the present invention is to provide carbapenem derivatives which have potent antibiotic activity against MRSA, PRSP, Influenzavirus, and &bgr;-lactamase-producing bacteria and are stable against DHP-1.
Abstract: Stabilized preparations which contain a &bgr;-lactam antibiotic having an esterified carboxyl group attached directly to the mother nucleus, an oil and a phosphate.
Type:
Grant
Filed:
February 5, 2001
Date of Patent:
February 4, 2003
Assignee:
Takeda Schering-Plough Animal Health K.K.
Abstract: An objective of the present invention is to provide carbapenem derivatives which have potent antibiotic activity against MRSA, PRSP, Influenzavirus, and &bgr;-lactamase-producing bacteria and are stable against DHP-1.