Abstract: Use of the 2-amino-2,4,4-trimethylpentane salt of clavulanic acid as an intermediate in the production of pharmaceutically acceptable salts of clavulanic acid.
Abstract: Disclose herein is a novel recombinant mutant protein of human Group IIA phospholipase A2 (PLA2) which has enhanced antibacterial activity when compared to the wild-type human Group IIA PLA2, pharmaceutical formulations comprising the protein and methods of use thereof. Additionally, the formulations may comprise other bioactive compounds, such as, e.g., conventional antibiotics, that act additively or synergistically with Group IIA PLA2 in order to promote bacterial killing.
Type:
Application
Filed:
December 18, 2000
Publication date:
November 21, 2002
Applicant:
New York University
Inventors:
Jerrold Weiss, Peter Elsbach, Ning Sheng Liang
Abstract: A method for treating a skin condition by intimately combining a water soluble antibiotic with the keratin layer of the outermost layer of the cleansed epidermis. The antibiotic is dissolved in the alkaline fraction of an electrolyzed water. The solution is characterized by the absence of hydrolysis products, turbidity, and loss of potency of the antibiotic. The aqueous solution is applied to the treatment area where the water is absorbed by the keratin and the antibiotic is carried into intimate contact with the keratin after which the water is evaporated leaving the antibiotic dispersed across the treatment area.
Inventors:
Eric Hunt, Steven Coulton, Jeremy David Hinks, Stephen Frederick Moss, Stephen Christopher Martin Fell, Alfred John Eglington, George Burton
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: Infections potentially caused by DRSP may be treated by a method which comprises administering a pharmaceutical formulation comprising either: for an adult or older child patient from 800 to 1100 mg amoxycillin and from 100 to 150 mg clavulanate in a weight ratio between 6:1 and 10:1 inclusive; or for a paediatric patient from 30 to 40 mg/kg body weight of amoxycillin and from 3 to 8 mg/kg body weight of clavulanate in a weight ratio between 6:1 and 10:1 inclusive; in combination with a pharmaceutically acceptable carrier or excipient, three times a day(tid).
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: Paediatric aqueous liquid suspension formulations comprising amoxycillin trihydrate and potassium clavulanate in a ratio of from 6:1 to 8:1 are provided for use in a BID dosage regimen for treating bacterial infection.
Type:
Application
Filed:
January 11, 2002
Publication date:
July 25, 2002
Applicant:
SmithKline Beecham p.1.c.
Inventors:
Richard Peregrine Bax, Mike Gale Ramsey
Abstract: A tablet formulation which comprises a core containing a pharmaceutically active material, coated with a release retarding coating, surrounded by a casing layer which includes a second pharmaceutically active material.
Type:
Application
Filed:
December 18, 2001
Publication date:
July 4, 2002
Applicant:
SmithKline Beecham p.l.c.
Inventors:
Francis Walter Grimmett, Nigel Philip McCreath Davidson
Abstract: Use of the 2-amino-2,4,4-trimethylpentane salt of clavulanic acid as an intermediate in the production of pharmaceutically acceptable salts of clavulanic acid.
Abstract: Compounds of formula I are disclosed.
as well as pharmaceutically acceptable salts thereof. The naphthosultam is substituted with various substituent groups including at least one cationic group —A—Q—L—B.
The carbapenems of the invention are effective against susceptible bacterial organisms, including methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant Staphylococcus epidermidis (MRSE), and methicillin resistant coagulase negative Staphylococci (MRCNS).
Type:
Grant
Filed:
March 20, 2000
Date of Patent:
June 4, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Lovji D. Cama, Ronald W. Ratcliffe, Robert R. Wilkening, Kenneth J. Wildonger, Wanying Sun
Abstract: Syrup formulations comprising water and compacted granulates which are mixture of amoxycillin and clavulanic acid, together with an intra-granular disintegrant.
Type:
Application
Filed:
November 19, 2001
Publication date:
May 30, 2002
Applicant:
Laboratorios Beecham SA
Inventors:
Luis Carvajal Martin, Juan Dedios Romero
Abstract: This invention relates to a method for coating a medical device comprising the steps of applying to at least a portion of the surface of said medical device, an antimicrobial coating layer and a non-pathogenic bacterial coating layer, wherein the antimicrobial and non-pathogenic bacterial coating layers inhibit the growth of pathogenic bacterial and flngal organisms. The non-pathogenic bacterium used in the bacterial coating layer is resistant to the antimicrobial agent. Furthermore, the non-pathogenic bacterium layer includes at least one of the following: viable whole cells, non-viable whole cells, or cellular structures or extracts. The antimicrobial agent and non-pathogenic bacterium are used to develop a kit comprising these compositions in one container or in separate containers. The kit is used to coat a catheter prior to implantation in a mammal.
Abstract: The present invention provides antimicrobial sulfonamide derivatives of lipopeptide antibiotics, pharmaceutical compositions of antimicrobial sulfonamide derivatives, methods for making antimicrobial sulfonamide derivatives, methods for inhibiting microbial growth with antimicrobial sulfonamide derivatives and methods for treating or preventing microbial infections in a subject with antimicrobial sulfonamide derivatives. Antimicrobial sulfonamide derivatives are generally an amino core antibiotic that has been further modified with a lipophilic sulfonyl group.
Type:
Application
Filed:
July 13, 2001
Publication date:
March 7, 2002
Inventors:
William V. Curran, Richard A. Leese, Howard Jarolmen, Donald B. Borders
Abstract: A stable fixed dose oral pharmaceutical formulation is provided. The formulation contains at least one anti-infective agent and at least one susceptible microorganism as active ingredients. At least one of the active ingredients is coated to provide a protective barrier around the active ingredient, the active ingredients being contained in a single pharmaceutical formulation. The formulation may be a tablet, a capsule, or a powder which may be made into a stable liquid. The protective barrier protectis the susceptible micro-organism from the effect of the anti-infective agent to maintain the susceptible micro-organism in a viable form for a period of at least three months. The anti-infective agent can be an antibiotic such as an amoxycillin and the microorganism can be Lactobacillus acidophilus.
Abstract: An alternate drug delivery system for dissolution of pharmaceuticals in the mouth wherein a therapeutically effective amount of a drug is encapsulated using an encapsulation method. Encapsulation reduces the perceived off flavors of drugs, allowing the active components to dissolve pleasantly in the mouth. This allows more rapid absorption of the active compounds through the oral cavity compared to traditional tablets, which require breakdown and absorption in the gastrointestinal tract. The delivery system can be incorporated into a variety of applications, such as breath mint tablets or chewing gum. Benefits of this invention include portability and the ability to take pharmaceuticals without water and without the off taste of chewable tablets, thereby leading to increased patient compliance.
Abstract: Compounds of formula I:
as well as pharmaceutically acceptable salts thereof useful as carbapenem antibacterial agents are disclosed wherein X is CH2 or C═O.
Type:
Grant
Filed:
June 23, 1999
Date of Patent:
February 12, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Timothy A. Blizzard, Kevin D. Dykstra, Ronald W. Ratcliffe
Abstract: Compounds of formula I:
as well as pharmaceutically acceptable salts thereof and compositions useful as carbapenem antibacterial agents are disclosed.
Type:
Grant
Filed:
June 23, 1999
Date of Patent:
February 12, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Timothy A. Blizzard, Ronald W. Ratcliffe, Sherman T. Waddell, Jerry D. Morgan, II
Abstract: A method of treating an individual exhibiting at least one symptom of a mental disorder is provided which comprises administering to the individual an antimicrobial composition in an amount effective to inhibit or eliminate the at least one symptom of the disorder. This invention also pertains to a method of treating an individual exhibiting at least one symptom of a mental disorder by administering a probiotic mixture to replenish gastrointestinal microbes.
Abstract: An antibiotic product for delivering at least two different antibiotics that is comprised of three dosage forms with different release profiles with each antibiotic being present in at least one of the dosage forms.
Type:
Application
Filed:
February 23, 2001
Publication date:
January 10, 2002
Inventors:
Edward M. Rudnic, James D. Isbister, Donald J. Treacy, Sandra E. Wassink
Abstract: A novel rapid-melt, semi-solid molded composition, including methods of making the same, and methods of using the same for the delivery of prophylactic and therapeutic active materials to a mammal wherein the prophylactic or therapeutic active is a psychotropic, a gastrointestinal therapeutic or a migraine therapeutic.
Abstract: Novel neuroprotectant compositions and methods are described. &bgr;-Lactamase inhibitors are used to prevent or reduce loss of neuronal cells and neuronal cell function in patients afflicted with or susceptible to disease states or conditions known to result in or cause neuronal tissue insult.
Abstract: Antibiotic composition having four dosage forms with different release profiles providing for initial release of a beta lactam antibiotic followed by release of a beta-lactamase inhibitor, followed by release of the antibiotic followed by release of the inhibitor. In a preferred embodiment, release from the second, third and fourth dosage forms is initiated after the component released from the immediately previous form reaches Cmax.
Abstract: Use of the 2-amino-2,4,4-trimethylpentane salt of clavulanic acid as an intermediate in the production of pharmaceutically acceptable salts of clavulanic acid.
Abstract: The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2 -position with a iodophenoxy linked through a group —Z—CH2—; The compound is further substituted with various substituent groups including at least one cationic group.
The compounds are represented by formula I:
wherein Z represents trans-ethenediyl or ethynediyl.
Pharmaceutical compositions and methods of use are also included.
Abstract: Compounds of formula I:
as well as pharmaceutically acceptable salts therefor and compositions useful as carbapenem antibacterial agents are disclosed.
Type:
Grant
Filed:
June 23, 1999
Date of Patent:
September 25, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Timothy A. Blizzard, Robert R. Wilkening, Ronald W. Ratcliffe
Abstract: Compounds of formula I:
as well as pharmaceutically acceptable salts thereof useful as carbapenam antibacterial agents are disclosed wherein X is CR2R2, NR2, or O.
Type:
Grant
Filed:
June 23, 1999
Date of Patent:
September 18, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Timothy A. Blizzard, Robert R. Wilkening, Ronald W. Ratcliffe
Abstract: The present invention relates to tricyclic carbapenem antibacterial agents in which the carbapenem nucleus is fused to a 6 membered carbocyclic ring. The compound is further substituted with various substituent groups including at least one cationic group.
The compounds are represented by formula I:
Pharmaceutical compositions and methods of use are also included.
Type:
Grant
Filed:
May 24, 1999
Date of Patent:
September 11, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Frank P. Dininno, Milton L. Hammond, Kevin D. Dykstra
Abstract: The present invention relates to tricyclic carbapenem antibacterial agents in which the carbapenem nucleus is fused to a 6 membered carbocyclic ring. The compound is further substituted with various substituent groups including at least one cationic group.
Abstract: The present invention relates to tricyclic carbapenem antibacterial agents wherein X is CH2, CHRa, CHRb, C═CHRa, C═CHRb, O, S, SO, SO2, CO, COO<OCO, NRa, NRb; and Z is trans-ethenediyl or ethynediyl. The compound is further substituted with various substituent groups including at least one cationic group.
The compounds are represented by formula I:
Pharmaceutical compositions and methods of use are also included.
Abstract: The present invention relates to carbapenem antibacterial agents of the formula I:
as well as salts and hydrates thereof. Pharmaceutical compositions and methods of treatment are also included wherein X is present or absent, when present, represents a members selected from the group consisting of:
CH2, C(R)2, C═CR2, O, S(O)x, with x equal to 0, 1 or 2; C(O), C(O)O, OC(O) and NR—.
Abstract: Provided is a process for preparation and/or purification of clavulanic acid or a pharmaceutically acceptable salt or ester thereof including removing solids from a clavulanic acid containing fermentation broth by microfiltration to form a first filtrate, further removing solids from the first filtrate by ultrafiltration to form a second filtrate, concentrating the second filtrate by removal of water, and treating the concentrated second filtrate to isolate clavulanic acid or a pharmaceutically acceptable salt or ester thereof.
Type:
Grant
Filed:
August 14, 2000
Date of Patent:
August 14, 2001
Assignee:
LEK Pharmaceutical and Chemical Co. D. D.
Abstract: The present invention relates to tricyclic carbapenem antibacterial agents in which the carbapenem nucleus is fused to a 6 membered carbocyclic ring. The compound is further substituted with various substituent groups including at least one cationic group.
Abstract: The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with an iodo-substituted phenyl linked through a CH2—O— group. The compounds of the invention are represented by formula I:
wherein A represent O, S or —CH2— attached at position 3, 4 or 6; Q is selected from the group consisting of:
&agr; represents O, S or NRs; &bgr;, &dgr;, &ggr;, &mgr; and &sgr; represent CRt, N or N+Rs, provided that no more than one of &bgr;, &dgr;, &ggr;, &mgr; and &sgr; is N+Rs, balanced by L− or a carboxylate anion. Salts and hydrates thereof are included. The iodo-substituted phenyl ring is further substituted with various substituent groups including at least one cationic group. Pharmaceutical compositions and methods of treatment are also included.
Abstract: The present invention relates to carbapenem antibacterial agents of formula I:
or a pharmaceutically acceptable salt thereof, wherein:
R2 represents:
in formula I, in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH2 group. The naphthosultam is further substituted with various substituent groups including at least one cationic group.
Type:
Grant
Filed:
March 13, 2000
Date of Patent:
June 26, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Timothy A. Blizzard, Ronald W. Ratcliffe, Jerry D. Morgan, II, Robert R. Wilkening