6-position Substituent Contains Carbocyclic Ring Patents (Class 514/197)
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Patent number: 6380181Abstract: Catechol derivatives of general formula (I) in which R1 denotes O-acyl and R2 represents amino acid residues in the 3- and/or 4-position function as siderophores and/or as biological chelating agents for iron in gram-negative bacteria. Conjugates with antibiotics improve penetration into bacterial cells, thereby increasing antibacterial efficacy of the cells.Type: GrantFiled: September 10, 1999Date of Patent: April 30, 2002Assignee: Gruenenthal GmbHInventors: Lothar Heinisch, Ute Moellmann, Matthias Schnabelrauch, Rolf Reissbrodt
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Patent number: 6316015Abstract: A surface is provided with antibiotic or antiseptic properties. A solid substrate is modified by covalently fixing one or more spacers having reactive extremities via a proximate reactive extremity, and one or more antibiotic, bactericidal, viricidal or fungicidal molecules covalently bonded to a distal reactive extremity of the spacer or spacers. The spacer has formula A1—(CH2)n—A2, where: A1 is where Z=H, OH or Cl; or SiY3 where Y3 is Cl or an alkoxy group containing 1 to 3 carbon atoms; n is in the range 2 to 18; A2 is selected from the following residues: CH═CH2, OH, halogen or where Z=H, OH or Cl.Type: GrantFiled: February 1, 1999Date of Patent: November 13, 2001Assignees: Institut Curie, Centre National de la Recherche ScientifiqueInventors: Francis Rondelez, Pascal Bezou, Othman Bouloussa
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Publication number: 20010027192Abstract: The present invention includes a formulation which comprises an antibacterial substance and an antiulcer substance, wherein at least either of them is formulated into a gastrointestinal mucosa-adherent solid preparation. The formulation of the present invention shows long retention time in the gastrointestinal tract because of adhesion to the gastrointestinal tract mucosa, synergetically enhances the pharmaceutical effects of an antibacterial substance, specially antibiotic against Helicobacter pylori (HP) and an antiulcer substance, with very low doses of active ingredients, particularly the anti-HP antibiotic with low prevalence of side effects. The present agent is useful as an antiulcer agent, showing potent anti-HP activity.Type: ApplicationFiled: May 17, 2001Publication date: October 4, 2001Inventors: Yohko Akiyama, Masafumi Nakao, Naoki Nagahara, Susumu Iwasa
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Patent number: 6294526Abstract: A novel screening system for detecting a non-antibiotic compound having &bgr;-lactam-sensitivity-inducing activity comprising a non-antibiotic compound and a &bgr;-lactam antibiotic two times serially diluted series and a pharmaceutical composition having anti-MRSA activity comprising a flavone derivative and a &bgr;-lactam antibiotic.Type: GrantFiled: July 23, 1998Date of Patent: September 25, 2001Assignee: Alps Pharmaceutical Ind. Co., Ltd.Inventors: Tomihiko Higuchi, Yoichi Sato, Shoji Murasugi
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Substituted amino bicyclic-&bgr;-lactam penam and cepham derivatives as cysteine protease inhibitors
Patent number: 6232305Abstract: 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: GrantFiled: January 22, 1998Date of Patent: May 15, 2001Assignee: Naeja Pharmaceutical Inc.Inventors: Rajeshwar Singh, Nian Zhou, Deqi Guo, Ronald G. Micetich -
Patent number: 6177421Abstract: A storage-stable combination of at least one &bgr;-lactam antibiotic and at least one &bgr;-lactam inhibitor compressed into tablet form having a hardness of greater than 30 KP is disclosed.Type: GrantFiled: May 4, 1999Date of Patent: January 23, 2001Assignee: Fuisz International Ltd.Inventors: Peter Moir, Siobhan Greene
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Patent number: 6156745Abstract: 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: GrantFiled: December 29, 1998Date of Patent: December 5, 2000Assignee: Research Corporation Technologies, Inc.Inventors: John D. Buynak, Akireddy Srinivasa Rao, Venkata Ramana Doppalapudi
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Patent number: 6127355Abstract: The present invention is directed compositions of the formula: ##STR1## wherein: D is a residue of a biologically active moiety;X is an electron withdrawing group;Y and Y' are independently O or S;(n) is zero (0) or a positive integer, preferably from 1 to about 12;R.sub.1 and R.sub.2 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls and substituted C.sub.1-6 alkyls;R.sub.3 is a substantially non-antigenic polymer, C.sub.1-12 straight or branched alkyl or substituted alkyl, C.sub.5-8 cycloalkyl or substituted cycloalkyl, carboxyalkyl, carboalkoxy alkyl, dialkylaminoalkyl, phenylalkyl, phenylaryl or ##STR2## R.sub.4 and R.sub.5 are independently selected from the group consisting of H, C.sub.1-6 alkyls, aryls, substituted aryls, aralkyls, heteroalkyls, substituted heteroalkyls, and substituted C.sub.1-6 alkyls or jointly form a cyclic C.sub.5 -C.sub.7 ring.Type: GrantFiled: March 26, 1999Date of Patent: October 3, 2000Assignee: Enzon, Inc.Inventors: Richard B. Greenwald, Annapurna Pendri, Hong Zhao
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Patent number: 6066629Abstract: A dry powder formulation of antibiotic and .beta.-lactam inhibitor is provided which is suitable for use in a liquid suspension.Type: GrantFiled: May 4, 1999Date of Patent: May 23, 2000Assignee: Fuisz Technologies Ltd.Inventors: Peter Moir, Siobhan Greene
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Patent number: 6048852Abstract: A method of treatment of bacterial infections in humans or animals which comprises administering, in combination with a .beta.-lactam antibiotic, a therapeutically effective amount of an amino acid derivative of Formula (I) or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, ##STR1## wherein: R is hydrogen, a salt forming cation or an in vivo hydrolysable ester-forming group; R.sub.1 is hydrogen, (C.sub.1-6)alkyl optionally substituted by up to three halogen atoms or by a mercapto, (C.sub.1-6)alkoxy, hydroxy, amino, nitro, carboxy, (C.sub.1-6)alkylcarbonyloxy, (C.sub.1-6)alkoxycarbonyl, formyl or (C.sub.1-6)alkylcarbonyl group, (C.sub.3-7)cycloalkyl, (C.sub.3-7)cycloalkyl(C.sub.2-6)alkyl, (C.sub.2-6)alkenyl, (C.sub.2-6)alkynyl, aryl, aryl(C.sub.1-6)alkyl, heterocyclyl or heterocyclyl(C.sub.1-6)alkyl; R.sub.2 is hydrogen, (C.sub.1-6)alkyl or aryl(C.sub.1-6)alkyl; R.sub.3 is hydrogen, (C.sub.1-6)alkyl optionally substituted by up to three halogen atoms, (C.sub.Type: GrantFiled: January 13, 1999Date of Patent: April 11, 2000Assignee: SmithKline Beecham p.l.c.Inventors: John Hargreaves Bateson, David R Witty, Brian Charles Gasson, Desmond John Best, David John Payne
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Patent number: 6013647Abstract: This invention relates to new benzoxazinedione derivatives corresponding to the formula I: ##STR1## wherein R.sup.1 =H or carboxyalkyl, R.sup.2 =H, alkyl or phenyl, and R.sup.3 represents different acid groups derived from amino acids, dipeptides and hydrazones or conjugates thereof with active ingredients, e.g. antibiotics. The compounds may be present as free acids, in the form of their salts or as readily cleavable esters. The compounds according to the invention constitute heterocyclically protected catechol derivatives and are effective as siderophores against gram-negative bacterial strains, particularly against Pseudomonads and strains of E. coli and Salmonella. In the form of their conjugates with active ingredients, e.g. antibiotics (as "siderophore-antibiotic conjugates"), they can transport the latter into bacterial cells and can improve or extend the antibacterial effect thereof, sometimes even in relation to bacterial strains which are resistant to other .beta.-lactams.Type: GrantFiled: March 5, 1998Date of Patent: January 11, 2000Assignee: Gruenenthal GmbHInventors: Lothar Heinisch, Steffen Wittmann, Ute Moellmann, Rolf Reissbrodt
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Patent number: 5994340Abstract: 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: GrantFiled: August 29, 1997Date of Patent: November 30, 1999Assignee: 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
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Patent number: 5948773Abstract: The present invention includes a formulation which comprises an antibacterial substance and an antiulcer substance, wherein at least either of them is formulated into a gastrointestinal mucosa-adherent solid preparation. The formulation of the present invention shows long retention time in the gastrointestinal tract because of adhesion to the gastrointestinal tract mucosa, synergetically enhances the pharmaceutical effects of an antibacterial substance, specially antibiotic against Helicobacter pylori (HP) and an antiulcer substance, with very low doses of active ingredients, particularly the anti-HP antibiotic with low prevalence of side effects. The present agent is useful as an anti ulcer agent, showing potent anti-HP activity.Type: GrantFiled: May 27, 1997Date of Patent: September 7, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Yohko Akiyama, Masafumi Nakao, Naoki Nagahara, Susumu Iwasa
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Patent number: 5900413Abstract: An infection with Helicobacter may successfully be treated with a compound of the formula ##STR1## wherein R.sub.1 is hydrogen or methyl and R.sub.2 is hydrogen or L-alanine-L-alanyl, and the pharmaceutically acceptable acid additive salts thereof. These compounds are useful in the treatment of gastric and duodenal ulcers.Type: GrantFiled: January 13, 1998Date of Patent: May 4, 1999Assignee: Pfizer Inc.Inventors: Arthur E. Girard, Thomas D. Gootz
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Patent number: 5883074Abstract: Methods for screening for compounds which potentiate the activity of antibacterial agents against bacteria resistant to the antibacterial agent alone, pharmaceutical compositions including such potentiators, and methods of treating bacterial infections using a combination of a potentiator and a potentiated antibacterial agent, which are useful for overcoming the resistance of a bacterial strain for an antibacterial agent.Type: GrantFiled: February 8, 1995Date of Patent: March 16, 1999Assignee: Microcide Pharmaceuticals, Inc.Inventors: Amy Boggs, Joaquim Trias, Scott Hecker
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Patent number: 5849797Abstract: Now are provided (R)-3,6-diamino-N-(.omega.-aminoalkyl)-hexanamides which are novel compounds having the general formula (I): ##STR1## wherein n stands for 2-5, and which may be for example, (R)-3,6-diamino-N-(2-aminoethyl)hexanamide (n=2) and (R)-3,6-diamino-N-(3-aminopropyl)hexanamide (n=3). Their preparation process is also provided. These novel compounds and acid addition salts thereof have activities inhibitory against Gram-positive bacteria, Gram-negative bacteria and AIDS virus, as well as tumor cells and are chemically stable.These novel compounds and their salts are useful as chemotherapeutic agents for diseases caused by these bacteria or virus and also as antitumor agent.Type: GrantFiled: February 24, 1997Date of Patent: December 15, 1998Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu KaiInventors: Shinichi Kondo, Yoko Ikeda, Tomio Takeuchi, Rie Shinei, Shuichi Gomi, Seiji Shibahara, Hiroo Hoshino
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Patent number: 5801153Abstract: A method for controlling plant diseases utilizes a mixture of antibiotics and food additives or food preservatives. The mixture is sprayed on the plants twice per week for three weeks, then once every three weeks. Such a regimen has been found to cure plant diseases of bacterial, fungal and viral origin. The preferred form of the mixture has four ingredients, with the antibiotics and food additives in a ratio of from 1:1 to 1:3. The antibiotics are selected from amoxicillin trihydrate and neomycin sulfate, and the food additives are selected from sodium propionate, sorbic acid, potassium sorbate, caffeine, vanillin, ascorbic acid, L-Arginine, thymol, cupric sulfate and ammonium benzoate.Type: GrantFiled: February 20, 1996Date of Patent: September 1, 1998Inventor: Mohammed A. Badaway
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Patent number: 5747483Abstract: 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: GrantFiled: March 17, 1995Date of Patent: May 5, 1998Assignees: A. Menarini Industrie Farmaceutiche Riunite, Istituto Lusofarmaco D'ItaliaInventors: Maria Altamura, Federico Maria Arcamone, Enzo Perrotta, Vittorio Pestellini, Piero Sbraci, Giuseppe Cascio
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Patent number: 5681563Abstract: Cephalosporins with an exocyclic allene in the 7-position and their pharmaceutically active salts are potent inhibitors of .beta.-lactamases and are therefore useful in the treatment of penicillin resistant infections.Type: GrantFiled: June 17, 1996Date of Patent: October 28, 1997Assignee: Research Corporation Technologies, Inc.Inventors: John D. Buynak, Brian Bachmann
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Patent number: 5668130Abstract: 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: GrantFiled: June 5, 1995Date of Patent: September 16, 1997Assignee: Glaxo Group LimitedInventor: Andrew Alexander McColm
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Patent number: 5559241Abstract: A process for the preparation of sterile sodium amoxycillin characterized by the fact that a solution of amoxycillin trihydrate in a mixture of methyl alcohol and a lower C.sub.2 -C.sub.5 alcohol is reacted in a sterile ambient, optionally in the presence of a suitable amine, with a solution of a suitable salifying agent selected from the group consisting of an alcoholate or carboxylate of sodium in methyl acetate followed by separation of the precipitate is described.Type: GrantFiled: September 15, 1995Date of Patent: September 24, 1996Assignee: Instituto Biochimico Italiano Giovanni Lorenzini S.p.A.Inventors: Giordano B. Corsi, Alberto Brandt, Loredana Cecchetelli
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Patent number: 5474993Abstract: 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: GrantFiled: June 14, 1994Date of Patent: December 12, 1995Assignee: Sterling Winthrop, Inc.Inventors: Byron Rubin, Kenneth C. Mattes, Terrence C. Mungal
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Patent number: 5122377Abstract: A veterinary drug delivery system suitable for oral administration to animals comprising a suitable medication, a nonvolatile oil, silicone dioxide, capric/caprylic triglyceride and/or capric/caprylic/stearic triglyceride. Flavorings can be added to enhance the taste, however, even without extra flavorings the drug delivery system in administrable form is palatable. At room temperature ay and physical analysis demonstrated no significant changes in active ingredient quality. Additionally, no separation of ingredients and no changes in overall physical appearance were noted.Type: GrantFiled: November 19, 1990Date of Patent: June 16, 1992Assignee: A.H. Robins, Company, IncorporatedInventors: Larry C. Miller, Thomas S. Ingallinera, Kyong K. Saw
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Patent number: 5069899Abstract: Anti-thrombobenic, anti-microbial compositions containing heparin reacted with quaternary ammonium components and bound with water-insoluble polymers are disclosed. Such compositions may also contain additional quaternary ammonium compounds not reacted with heparin and may also contain quaternary ammonium compound(s) reacted with antibiotics.Type: GrantFiled: November 2, 1989Date of Patent: December 3, 1991Assignee: Sterilization Technical Services, Inc.Inventors: Richard J. Whitbourne, Margaret A. Mangan
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Patent number: 4997830Abstract: A pharmaceutical combination of Metronidazole and Amoxicillin for the treatment of periodontitis. Conventional therapeutic doses of both the Metronidazole and Amoxicillin given as a combination therapy has been unexpectedly found to effectively treat periodontitis.Type: GrantFiled: February 7, 1990Date of Patent: March 5, 1991Assignee: The Research Foundation of State University of New YorkInventors: Arie J. van Winkelhoff, Edwin G. Winkel, Ronald J. Goene, Lars A. Christersson, Joseph J. Zambon, Robert J. Genco
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Patent number: 4988679Abstract: There is provided an orally ingestible liquid composition for suspending therein an orally administrable pharmaceutically active composition releasable over an extended period of time comprises triglyceride of a medium chain length alkanoic acid or distilled acetylated monoglycerides, a liquid, high HLB polyglyceryl ester, and colloidal silicon dioxide together with a material soluble or dispersible therein and capable of being insolubilized by a pharmaceutically acceptable polyvalent cation and a solid pharmaceutically acceptable salt containing the cation required therefore. Sustained release compositions based thereon containing pharmaceutically active agents are also disclosed.Type: GrantFiled: June 19, 1989Date of Patent: January 29, 1991Inventors: Leonard Chavkin, Leonard Mackles
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Patent number: 4966899Abstract: An antibacterial lyophilized preparation which comprises as an active ingredient aspoxicillin and a basic salt of aspoxicillin in a molar ratio of 1 : about 0.7 to 7 and optionally an alkali metal halide as a stabilizer, and a method for preparing the same, said antibacterial lyophilized preparation being able to be rapidly dissolved in distilled water to give a stable solution which can be injected to patients for the treatment of various bacterial infectious diseases.Type: GrantFiled: January 14, 1988Date of Patent: October 30, 1990Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Keiichi Kohno, Hiroshi Miura, Yoshiyuki Hirakawa, Toshiyuki Ueki, Seiichi Morikuni
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Patent number: 4898731Abstract: An antibacterial synergistic composition consisting essentially of a mixture of a penicillin or cephalosporin derivative of the formula ##STR1## and a penicillin of the formula ##STR2## preferably in association with a pharmaceutical carrier.Type: GrantFiled: June 24, 1985Date of Patent: February 6, 1990Assignees: Astra Lakemedel Aktiebolag, Astra Pharmaceutical Products, Inc.Inventors: Peter Bamberg, Bertil A. Ekstrom, Ulf E. Forsgren, Berndt O. H. Sjoberg
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Patent number: 4876086Abstract: Injectable pharmaceutical compositions are provided which comprise fine particles of amoxycillin trihydrate coated with a dispersing agent, the ratio of amoxycillin trihydrate to dispersing agent being from 1000:1 to 20:1. A preferred dispersing agent is a mixture of polyvinylpyrrolidone and lecithin. Such compositions give surprising prolonged blood levels of amoxycillin after administration. The compositions can be used in the treatment of both humans and domestic animals.Type: GrantFiled: September 17, 1987Date of Patent: October 24, 1989Assignee: Beecham Group p.l.c.Inventor: John S. Dowrick
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Patent number: 4868177Abstract: There are disclosed compounds having the formula ##STR1## where n is 1, 2 or 3;X is hydrogen, loweralkyl, loweralkoxy, halogen, hydroxy, nitro or trifluoromethylR.sub.1 and R.sub.2 are each independently hydrogen, lower alkyl or arylloweralkyl, but both may not be arylloweralkyl simultaneously;R.sub.3 and R.sub.4 are each independently hydrogen, lower alkyl, arylloweralkyl, formyl or lower alkylcarbonyl, or alternatively the group --NR.sub.3 R.sub.4 taken as a whole constitutes ##STR2## stereo isomers thereof and pharmaceutically acceptable acid addition salts thereof, which are useful for the treatment of various memory dysfunctions characterized by decreased cholinergic function, such as Alzheimer's disease.Type: GrantFiled: November 29, 1988Date of Patent: September 19, 1989Assignee: Hoechst-Roussel Pharmaceuticals, Inc.Inventors: Gregory M. Shutske, Kevin J. Kapples
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Patent number: 4863915Abstract: Crystalline anhydrous amoxycillin is prepared by removing bound solvent molecules from a crystalline solvate (other than the trihydrate) of amoxycillin. A preferred crystalline solvate is the monomethanolate.Type: GrantFiled: December 10, 1987Date of Patent: September 5, 1989Assignee: Beecham Group p.l.c.Inventor: Neil Ward
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Patent number: 4861768Abstract: Disclosed is a penicillin derivative of the formula: ##STR1## wherein n is an integer of 0, 1 or 2; Y is a cyano group, a lower acyl group, a mono- or di-lower alkylthiocarbamoyl group, ##STR2## wherein R.sub.1 is a hydrogen atom, a lower alkyl group, a phenyl group, a group --(CH.sub.2).sub.m --OR.sub.2 or --(CH.sub.2).sub.m COOR.sub.2 (m is an integer of 1 to 6 and R.sub.2 is a hydrogen atom or a penicillin carboxyl ester-forming group which is commonly used for penicillin derivatives) or a phenyl group substituted by at least one member selected from the class consisting of lower alkyl group, halogen atom and lower alkoxy group; and R is a hydrogen atom or a penicillin carboxyl ester-forming group, or a salt thereof. They are useful as .beta.-lactamase inhibitors.Type: GrantFiled: February 18, 1987Date of Patent: August 29, 1989Assignee: Taiho Pharmaceutical Company, LimitedInventors: Sigeru Torii, Hideo Tanaka, Motoaki Tanaka, Shozo Yamada, Akira Nakai, Hisashi Ohbayashi
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Patent number: 4803196Abstract: A solid pharmaceutical composition comprising one or more .beta.-lactam antibiotics in acid or amphoteric form in association with at least one physiologically acceptable base in the presence of a gaseous atmosphere containing a stabilizing amount of carbon dioxide at a concentration greater than that of atmospheric air. The compositions exhibit enhanced stability. A preferred antibiotic for the compositions is ceftazidime or a hydrate thereof, and a preferred base is sodium cabonate or a mixture thereof with one or more other bases.Type: GrantFiled: June 4, 1987Date of Patent: February 7, 1989Assignee: Glaxo Group LimitedInventor: Betty L. Richardson
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Patent number: 4742052Abstract: Novel .beta.-lactam compounds classified into penem compounds, a process for preparing the same and use of such .beta.-lactam compounds are disclosed. These .beta.-lactam compounds exhibit excellent antimicrobial activities useful as pharmaceuticals or they are important intermediates for the synthesis of compounds having antimicrobial activities.Type: GrantFiled: July 15, 1982Date of Patent: May 3, 1988Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Makoto Sunagawa, Haruki Matsumura, Takaaki Inoue, Masao Enomoto
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Patent number: 4731360Abstract: Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs.Type: GrantFiled: August 16, 1985Date of Patent: March 15, 1988Assignee: Merck & Co., Inc.Inventors: Jose Alexander, A. J. Repta, Joseph A. Fix
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Patent number: 4729989Abstract: Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs.Type: GrantFiled: June 28, 1985Date of Patent: March 8, 1988Assignee: Merck & Co., Inc.Inventors: Jose Alexander, Joseph A. Fix
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Patent number: 4692441Abstract: Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.Type: GrantFiled: August 16, 1985Date of Patent: September 8, 1987Assignee: Merck & Co., Inc.Inventors: Jose Alexander, A. J. Repta, Joseph A. Fix
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Patent number: 4609542Abstract: The present invention relates to a new pharmaceutical form for oral use in the nature of delayed action and controlled absorption medicaments.This form comprises an association of miniaturized granules obtained by high to very high compression: (a) with pH control agents, (b) coated with excipients determining the slow penetration of digestive and/or (c) coated with a very thin layer of lipids. These miniaturized granules may contain glucose, nay have pH control agents with different solubilities, and may be in the form of miniaturized granules with a pH gradient.Type: GrantFiled: July 1, 1985Date of Patent: September 2, 1986Assignee: Elan Corporation, P.L.C.Inventors: Donald E. Panoz, Gilbert Corneille
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Patent number: 4607029Abstract: Novel sodium amoxicillin preparations which are easily converted into stable, suitably injectable solutions which are free of allergic reactions-causing chemicals and which contain besides sodium amoxicillin, a small amount of sodium hydroxide and optionally also a small amount of sodium chloride, and a process for their preparation and a process for the preparation of aqueous sodium amoxicillin containing injection solutions. The sodium amoxicillin preparations are prepared by the as fast but gradual addition as possible of an excess of sodium hydroxide to a suspension of amoxicillin trihydrate in water until the amoxicillin has completely dissolved, whereafter optionally a part of the excess of base is immediately neutralized with hydrochloric acid while the temperature is kept between 0.degree.-30.degree. C., followed by sterile filtration of the obtained solution, freezing the solution and freeze drying the obtained solid in flasks or in bulk.Type: GrantFiled: April 23, 1985Date of Patent: August 19, 1986Assignee: Gist-Brocades N.V.Inventors: Hayo de Jonge, Jan W. Groenendaal, Gerrit J. Sijbrands, Annita Bagerman-Deetman
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Patent number: 4591459Abstract: beta-Lactamase inhibitors which are aminoacid esters of 6-alpha- and 6-beta-(hydroxymethyl)pencillanic acid 1,1-dioxides; pharmaceutically-acceptable salts thereof; conventional esters thereof which are hydrolyzable in vivo; bis-methanediol esters thereof; or mixed methanediol esters with said beta-lactamase inhibitors and sulbactam. Pharmaceutical compositions comprising said beta-lactamase inhibitors and a conventional beta-lactam antibiotic, said compositions useful in the treatment of bacterial infections. Compounds useful as intermediates in the synthesis of said beta-lactamase inhibitors. Antibacterial mixed bis-methanediol esters of said aminoacyloxymethyl penicillanic acid 1,1-dioxides and ampicillin or amoxicillin, also useful in the treatment of bacterial infections; and intermediates therefor.Type: GrantFiled: December 3, 1984Date of Patent: May 27, 1986Assignee: Pfizer Inc.Inventor: Wayne E. Barth
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Patent number: 4540688Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof have antibacterial activity: ##STR1## wherein R is hydrogen, C.sub.1-6 alkylcarbonyl or C.sub.1-6 alkyl; R.sup.1 is hydrogen or hydrocarbon; R.sup.2 is hydrogen, or optionally substituted hydrocarbon or optionally substituted heterocyclyl or CXR.sup.d, where X is O or S and R.sup.d is hydrogen or optionally substituted hydrocarbon or optionally substituted heterocyclyl; or R.sup.1 and R.sup.2 together with the nitrogen to which they are attached, form an optionally substituted heterocyclyl group. A process for the preparation of such compounds and compositions comprising them, are also described.Type: GrantFiled: April 27, 1983Date of Patent: September 10, 1985Assignee: Beecham Group p.l.c.Inventor: Michael J. Driver
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Patent number: 4537887Abstract: A unit dose pharmaceutical composition suitable for oral administration which composition comprises a pharmaceutically acceptable carrier, a desiccant, amoxycillin trihydrate equivalent to 20 mg to 1500 mg of amoxycillin and potassium clavulanate equivalent to 20 mg to 500 mg of clavulanic acid, with the proviso that the weight ratio of amoxycillin to clavulanic acid is in the range 12:1 to 1:1; characterized in that the composition is in tablet form, wherein the desiccant is edible and incorporated within the tablets.Type: GrantFiled: October 5, 1983Date of Patent: August 27, 1985Assignee: Beecham Group LimitedInventors: David J. Rooke, Barry W. Burnstead
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Patent number: 4521533Abstract: Salts of readily hydrolyzable esters of 6-alpha-(aminomethyl)penicillanic acid 1,1-dioxide and (a) prodrug forms of ampicillin and amoxicillin or (b) ampicillin and amoxicillin and a dibasic acid are readily absorbed following oral adminstration, and are useful in treating bacterial infections.Type: GrantFiled: July 12, 1984Date of Patent: June 4, 1985Assignee: Pfizer Inc.Inventors: Ernest S. Hamanaka, John G. Stam
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Patent number: 4518606Abstract: A pharmaceutical composition for injection which comprises an aqueous sterile solution of a penicillin or salt thereof and from 1 to 10% of benzyl alcohol, a two-pack container or two-part syringe wherein one pack or part contains a penicillin or salt thereof in the form of a dry powder and the second pack or part contains an aqueous solution of benzyl alcohol, such that mixing the contents of the two packs or parts produces an aqueous solution of the penicillin and from 1 to 10% of benzyl alcohol, and a two-pack container or two-part syringe wherein one pack or part contains a penicillin in a solid free acid form, and the second part contains an aqueous solution of benzyl alcohol and substantially one equivalent of a basic pharmaceutically acceptable salt, such that mixing the contents of the two packs or parts produces an aqueous solution of a salt of the penicillin and from 1 to 10% of benzyl alcohol.Type: GrantFiled: July 9, 1982Date of Patent: May 21, 1985Assignee: Beecham Group LimitedInventor: Edmond Saias
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Patent number: 4496574Abstract: A penicillin derivative having an antibacterial activity similar to a penicillin antibiotic in a living body without affecting the intestinal bacterial colonies, a process for preparing the derivative and a pharmaceutical composition in a dosage unit form containing the derivative as an active ingredient are disclosed.Type: GrantFiled: September 16, 1982Date of Patent: January 29, 1985Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Shigeaki Muto, Kouichi Niimura, Takao Ando, Akihiko Kanno, Takao Furusho, Chikao Yoshikumi