Additional Hetero Ring Patents (Class 514/202)
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Publication number: 20020115642Abstract: The present invention provides compositions comprising improved beta-lactam antibiotics and methods for applying these compositions to inhibit the growth of microbial infections. The improved antibiotics are capable of inhibiting the growth of both antibiotic sensitive and antibiotic resistant microorganisms In addition, the invention provides methods for treating a subject infected with a microorganism by administering the compositions of the invention.Type: ApplicationFiled: May 1, 2001Publication date: August 22, 2002Inventors: Ming Fai Chan, Rosario S. Castillo, Qing Li, Venkata Ramana Doppalapudi, Mark Stephen Hixon, Thomas J. Lobl
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Publication number: 20020106408Abstract: In one embodiment, the invention relates to sustained-release compositions comprising one or more prolamins, one or more gelling agents, and one or more active agents. Such compositions are particularly useful for controlled delivery of high solubility and/or high dosage active agents. In another embodiment, the present invention relates to delayed-onset compositions comprising a dry coating comprising one or more prolamins and one or more gelling agents.Type: ApplicationFiled: December 1, 2000Publication date: August 8, 2002Inventors: Johnatan Bacon, Alain Desjardins
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Publication number: 20020091252Abstract: A compound of formula 1Type: ApplicationFiled: November 13, 2001Publication date: July 11, 2002Inventors: Gerd Ascher, Josef Wieser, Michael Schranz, Johannes Ludescher, Johannes Hildebrandt
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Patent number: 6407091Abstract: The invention provides compounds of formula I and IV: wherein R1-R11 and A have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting &bgr;-lactamase enzymes, for enhancing the activity of &bgr;-lactam antibiotics, and for treating &bgr;-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I and IV, and novel intermediates useful for the synthesis of compounds of formula I and IV. The A can be, for example, thio, sulfinyl, or sulfonyl.Type: GrantFiled: April 13, 2000Date of Patent: June 18, 2002Assignee: Research Corporation Technologies, Inc.Inventors: John D. Buynak, A. Srinivasa Rao, Greg C. Adam, Sirishkumar D. Nidamarthy, Venkata Ramana Doppalapudi
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Publication number: 20020065262Abstract: Crystalline 7-[2-(2-formylaminothiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-3-methoxymethyl-3-cephem-4-carboxylic acid-1-(isopropoxycarbonyloxy)ethyl ester and its use.Type: ApplicationFiled: October 31, 2001Publication date: May 30, 2002Inventors: Julia Greil, Johannes Ludescher, Klaus Totschnig, Siegfried Wolf
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Publication number: 20020019381Abstract: A process is provided for the preparation of vinyl-pyrrolidinone cephalosporine derivatives. Intermediates of the process are also provided.Type: ApplicationFiled: May 17, 2001Publication date: February 14, 2002Inventors: Paul Hebeisen, Hans Hilpert, Roland Humm
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Patent number: 6342493Abstract: Processes are provided for the preparation of orally administrable, yellow and powdery compositions essentially consisting of particles composed of a homogeneous mixture of an amorphous Cefditoren pivoxil substance with a water soluble high-molecular additive. These compositions can be produced by dissolving crystalline Cefditoren pivoxil substance and the water-soluble high-molecular additive in an aqueous solution of an acid, then neutralizing the resultant solution, to co-precipitate the product, and drying the thus precipitated product, followed by recovering the product in the form of the above-mentioned particles.Type: GrantFiled: July 7, 2000Date of Patent: January 29, 2002Assignee: Meiji Seika Kaisha Ltd.Inventors: Masahiro Onodera, Masamichi Sukegawa, Kiyoshi Yasui, Tatsuo Watanabe, Toyomi Sato, Yasushi Murai, Katsuharu Iinuma
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Patent number: 6323193Abstract: This invention relates to a bioavailable oral dosage form comprising of amorphous cefuroxime axetil containing from 7 to 25% crystalline cefuroxime axetil.Type: GrantFiled: August 21, 2000Date of Patent: November 27, 2001Assignee: Ranbaxy Laboratories LimitedInventors: Jitendra Krishan Somani, Indu Bhushan, Himadri Sen
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Patent number: 6300347Abstract: Novel 2-substituted 4,5-diaryl imidazoles are provided, in particular compounds of Formula I wherein R1, R2, R3 and R4 are as defined, in free or pharmaceutically-acceptable acid addition salt or physiologically-cleavable ester form, which have p38 MAP kinase (Mitogen Activated Protein Kinase) inhibiting activity. The compounds are used as pharmaceuticals for treating TNF&agr; and IL-1 mediated diseases such as rheumatoid arthritis and diseases of bone metabolism, e.g. osteoporosis.Type: GrantFiled: December 29, 1999Date of Patent: October 9, 2001Assignee: Novartis AGInventor: Lászlo Révész
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Publication number: 20010011085Abstract: The present invention relates to cephem-derivatives and to a process for their preparation, having proper substituents at C-2 position, i.e. heterocyclylthio or acyloxy group. They are potent protease inhibitors, in particular human leucocyte elastase (HLE) inhibitors.Type: ApplicationFiled: August 14, 1997Publication date: August 2, 2001Inventors: MARCO ALPEGIANI, PIERLUIGI BISSOLINO, MASSIMILIANO PALLADINO, ETTORE PERRONE
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Patent number: 6262044Abstract: The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.Type: GrantFiled: March 11, 1999Date of Patent: July 17, 2001Assignees: Novo Nordisk A/S, Ontogen CorporationInventors: Niels Peter Hundahl Møller, Henrik Sune Andersen, Lars Fogh Iversen, Ole Hvilsted Olsen, Sven Branner, Daniel Dale Holsworth, Farid Bakir, Luke Milburn Judge, Frank Urban Axe, Todd Kevin Jones, William Charles Ripka, Yu Ge, Roy Teruyuki Uyeda
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Patent number: 6232306Abstract: The present invention provides compounds of formula I wherein R1 is hydrogen, C1-6-alkyl, C1-6-alkyl substituted by fluoro, or C3-6-cycloalkyl; R2 is hydrogen or a substituent selected from the group consisting of —CH2C(═CHR)—COOR, —CH2OCOR, —CH(R)OCOR, —CH(R)OCOOR, —CH(OCOR)OCOR, —CH2COCH2OCOR and R3 is hydrogen or a substituent selected from the group consisting of —CH2C(═CH2)—COOR, —COOCH2C(═CHR)—COOR, —COOCH2OCOR, —COOCH(R)OCOR, —COOCH(R)OCOOR, —COOCH(OCOR)OCOR, —COOCH2COCH2OCOR, and with the proviso that one of R2 and R3 is hydrogen and the other is not hydrogen, R is hydrogen or C1-6-alkyl; R4 is hydrogen or hydroxy, R5 is hydrogen or &ohgr;-hydroxyalkyl; and X is CH or N, pharmaceutically acceptable salts of the compounds and hydrates of the compounds and of their salts.Type: GrantFiled: June 14, 1999Date of Patent: May 15, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Paul Hebeisen, Christian Hubschwerlen, Jean-Luc Specklin
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Patent number: 6180621Abstract: A method for the prophylaxis or treatment of infectious diseases caused by helicobacter pyloir, by administering a pharmacologically effective amount of a 1-methoylcarbapenem coumpund of formula (I) or a pharmacologically acceptable salt or ester thereof: R1 represents a group of the following formula: R2 is a hydrogen atom or a C1-C6 alkyl group, and R3 is a hydrogen atom or a C1-C6 alkyl group.Type: GrantFiled: November 6, 1998Date of Patent: January 30, 2001Assignee: Sankyo Company, LimitedInventors: Isao Kawamoto, Satoshi Ohya, Yukio Utsui
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Patent number: 6159961Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is amino or protected amino,R.sup.2 is hydrogen or hydroxy protective group,R.sup.3 is carboxy or protected carboxy,R.sup.4 is hydrogen, lower alkenyl, acyloxy(lower)alkenyl, optionally substituted heterocyclic(lower)alkenyl, optionally substituted heterocyclic(lower)alkenylthio, optionally substituted heterocyclic(lower)alkylthio, or optionally substituted heterocyclic-thio(lower)alkylthio andR5 is halogen or lower alkyland pharmaceutically acceptable salts thereof, which is useful as a medicament for prophylactic and therapeutic treatment of infectious diseases.Type: GrantFiled: July 19, 1999Date of Patent: December 12, 2000Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kohji Kawabata, Hirofumi Yamamoto, Yoshiteru Eikyu, Shinya Okuda, Hisashi Takasugi
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Patent number: 6150350Abstract: The invention relates to antimicrobial compositions comprising a combination of (1) a therapeutically effective amount of a compound of formula I ##STR1## with (2) a second ingredient selected from carbapenem antibiotics or with .beta.-lactamase inhibitors, to the use of the compositions for producing a medicament for the treatment and prophylaxis of infectious diseases, including MRSA infections, and to pharmaceutical compositions containing the combination.Type: GrantFiled: August 24, 1998Date of Patent: November 21, 2000Assignee: Hoffman-la Roche Inc.Inventors: Peter Angehrn, Ingrid Heinze-Krauss, Malcolm Page, Hans G. F. Richter
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Patent number: 6063778Abstract: The invention provides novel cephalosporin derivatives of the formula (I) ##STR1## and salts thereof for use in pharmaceutical compositions. Also novel precursors for synthesis of the cephalosporins are disclosed.Type: GrantFiled: June 26, 1998Date of Patent: May 16, 2000Assignee: Il-Dong Pharm. Co., Ltd.Inventors: Kee-Won Kim, Jae-Hoon Kang, Dong-Sik Yu, Moo-Soo Jang, Seung-Woo Yu
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Patent number: 6020329Abstract: .beta.-Lactam antibiotics of formula (I) or a salt thereof, wherein R.sup.1 is hydrogen, methoxy or formamido; R.sup.2 is an acy group; CO.sub.2 R.sup.3 is a carboxy group or a carboxylate anion, or R.sup.3 is a readily removable carboxy protecting group; R.sup.4 represents up to four substituents; X is S, SO, SO.sub.2, O or CH.sub.Type: GrantFiled: October 20, 1997Date of Patent: February 1, 2000Assignee: Pzifer Inc.Inventors: John Hargreaves Bateson, George Burton, Stephen Christopher Martin Fell
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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: 5981519Abstract: The present invention relates to compounds having the formula ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are as defined herein as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts. These compounds have valuable pharmacological activity for the treatment and prophylaxis of infectious diseases, especially those caused by methicillin resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa.Type: GrantFiled: December 8, 1997Date of Patent: November 9, 1999Assignee: Hoffman-La Roche Inc.Inventors: Peter Angehrn, Paul Hebeisen, Ingrid Heinze-Krauss, Malcolm Page, Valerie Runtz
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Patent number: 5925632Abstract: Compounds of formula (I) ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aralkyl, cycloalkyl, R.sup.3 CO-- or --C(R.sup.4 R.sup.5)CO.sub.2 R.sup.6 ; where R.sup.4 and R.sup.5 are each independently hydrogen or lower alkyl, or R.sup.4 and R.sup.5 taken together with the carbon atom to which they are attached form a cycloalkyl group; R.sup.3 is hydrogen or lower alkyl and R.sup.6 is hydrogen, lower alkyl, lower alkenyl or a carboxylic acid protecting group;R.sup.2 is isobutyl, 2,2-dimethyl-propyl or cyclohexyl-methyl;n is 0, 1 or 2;X is CH or N;as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts are disclosed. These compounds have valuable antibacterial activity.Type: GrantFiled: July 25, 1997Date of Patent: July 20, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Ingrid Heinze-Krauss, Hans Richter
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Patent number: 5883248Abstract: Novel intermediates of the formula ##STR1## wherein the substituents are defined in the specification.Type: GrantFiled: July 30, 1997Date of Patent: March 16, 1999Assignee: Roussel UclafInventors: Jozsef Aszodi, Jean-Francois Chantot, Patrick Fauveau, Solange Gouin D'Ambrieres, Daniel Humbert, Christophe Dini
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Patent number: 5856320Abstract: Novel cephalosporin derivatives of formula (II): ##STR1## wherein R.sup.2 is hydrogen, methyl, or fluoromethyl; R.sup.3 is hydrogen, methyl or carboxyl; R.sup.4 is hydrogen or methyl; A is methylene or propenylene; Q is nitrogen or CH, and pharmaceutically acceptable salts, solvates, hydrates and esters thereof, a process for their preparation and an antimicrobial composition containing them.Type: GrantFiled: October 15, 1996Date of Patent: January 5, 1999Assignee: Katayama Seiyakusyo Co., Ltd.Inventors: Sadao Hayashi, Yasuyuki Kurita
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Patent number: 5843937Abstract: The present invention relates to novel DNA alkylating agents and the prodrugs of these agents which are useful as antitumor agents and DNA labelling agents. The compounds are hydroxy dihydrobenzindole oligopeptides and prodrugs thereof wherein the monomeric constituents are derived from monocyclic or bicyclic heterocyclic aromatic residues.Type: GrantFiled: May 23, 1996Date of Patent: December 1, 1998Assignee: Panorama Research, Inc.Inventors: Yuqiang Wang, Susan C. Wright, James W. Larrick
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Patent number: 5804577Abstract: The present invention relates to compounds of formula I ##STR1## wherein R.sup.1 is a group selected from 2-, 3-, and 4-hydroxyphenyl, 3-nitrophenyl, and 3-fluoro-4-hydroxyphenyl; as well as readily hydroyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts.Type: GrantFiled: August 27, 1996Date of Patent: September 8, 1998Assignee: Hoffmann-La Roche Inc.Inventors: Paul Hebeisen, Ingrid Heinze-Krauss, Hans Richter, Valeri Runtz, Henri Stalder, Urs Weiss, George Petros Yiannikouros
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Patent number: 5760027Abstract: The present invention relates to the use of 7-alkylidene derivatives of cephalosporin esters, such as sulfides, sulfoxides, and sulfones, as inhibitors of human leukocyte elastase. These materials are therefore useful as anti-inflammatory and anti-degenerative agents.Type: GrantFiled: December 6, 1996Date of Patent: June 2, 1998Assignee: Research Corporation Technologies, Inc.Inventors: John D. Buynak, Akireddy Srinivasa Rao, Greg C. Adam
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Patent number: 5747484Abstract: Novel crystalline cephem acid addition salts and processes for their preparationCompounds of the formula I ##STR1## in which n is equal to 1 or 2 andm is 0.4-2.6, and where X is the anion of a carboxylic acid, have antibacterial activity.Type: GrantFiled: November 1, 1995Date of Patent: May 5, 1998Assignee: Hoechst AktiengesellschaftInventors: Rudolf Lattrell, Walter Durckheimer, Peter Schmid
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Patent number: 5728691Abstract: Derivatives of 7-aminoceph-3-em-4-carboxylic acid with 6-fluoroquinolone derivatives in which the cephem and 6-fluoroquinolone moieties are bound to each other through a carboxamido bond as well as the pharmaceutical compositions containing them are described. These compounds possess antibacterial, growth promoting and probiotic activity.Type: GrantFiled: August 22, 1996Date of Patent: March 17, 1998Assignees: Laboratorios Aranda S.A. De C.V., Judith Marcia Arrieta MunguiaInventor: Miguel Angel Corpi Constantino
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Patent number: 5726170Abstract: The salts are prepared by reacting a benzhydrylamine of the formula I (or a salt thereof) with clavulanic acid (or a salt thereof) in solvent, and isolating the resulting salt. In formula I, each of R.sup.1 and R.sup.2 is hydrogen (preferred) or an acceptable substituent. ##STR1## The clavulanic acid salts can be used in pharmaceutical formulations together with a pharmaceutically acceptable carrier, and, preferably, a beta-lactam antibiotic.Type: GrantFiled: February 22, 1996Date of Patent: March 10, 1998Assignee: Spurcourt LimitedInventor: George Leo Callewaert
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Patent number: 5721229Abstract: A dry solid mixture of a hydroxypolycarboxylic acid and a cephalosporin where the hydroxypolycarboxylic acid of the formula ##STR1## where x and y are 0 or 1 and z is 0 to 3, in the weight ration of hydroxypolycarboxylic acid to cephalosporin of at least 1.8. The invention comprises a solution made from the dry solid mixture and a process of treating animals with cephalosporin by including the solution in the water fed to the animals so that the animals can ingest the cephalosporin. A particularly preferred mixture is one of citric acid and cephalexin.Type: GrantFiled: December 26, 1995Date of Patent: February 24, 1998Assignee: Veterinary Pharmacy CorporationInventors: Michael A. Strobel, Pat Soderlund
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Patent number: 5712266Abstract: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids wherein the substituents are defined as in the application having anti-bacterial properties.Type: GrantFiled: May 30, 1995Date of Patent: January 27, 1998Assignee: Roussel UclafInventors: Jozsef Aszodi, Jean-Francois Chantot, Patrick Fauveau, Solange Gouin D'Ambrieres, Daniel Humbert, Christophe Dini
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Patent number: 5710146Abstract: Cephem derivatives of the general formula ##STR1## in which the R.sub.2 O group is in the syn-position, a process for their manufacture and pharmaceutical formulations which are active against bacterial infections and contain these compounds.Type: GrantFiled: July 22, 1994Date of Patent: January 20, 1998Assignee: Hoechst AktiengesellschaftInventors: Walter Durckheimer, Dieter Bormann, Eberhard Ehlers, Elmar Schrinner, Rene Heymes
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Patent number: 5710147Abstract: The syn isomer of (R) or (S) or (R,S) mixture, in the form of internal salts or salts with acids or bases of a compound of the formula ##STR1## wherein the substituents are defined as in the specification having a very good antibiotic activity.Type: GrantFiled: July 7, 1995Date of Patent: January 20, 1998Assignee: Roussel UclafInventors: Jozsef Aszodi, Patrick Fauveau
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Patent number: 5693791Abstract: A group of reagents, as diisocyanates, dianhydrides, diacidchlorides, diepoxides, carbodiimides and the like are utilized to link a wide variety of antibiotic moities, reacted two at a time with said reagents, the said antibiotic moieties containing groups reactive with the linking reagents as carboxylic acid, alcolhol, primary amine, and secondary amine functional groups, said functional groups being present as singularities or as multiplicities, products being readily purified using chromatographic techniques, and said products of above reactions being valuable for the treatment of microbial infections of man and animals.Type: GrantFiled: April 11, 1995Date of Patent: December 2, 1997Inventor: William L. Truett
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Patent number: 5663162Abstract: Compounds represented by the following formula (I), that is, cephem derivatives having substituted or unsubstituted imidazo[5,1-b]thiazolium-6-yl as a substituent at the 3-position of the cephem ring: ##STR1## wherein X represents CH or N, R.sup.1 represents H, alkyl, alkenyl or the like, and R.sup.2, R.sup.3, R.sup.4 and R.sup.5 represent H, alkyl, carbamoyl, amino or the like. The above compounds have excellent antibacterial activity, and useful as medicines for the treatment of various infectious diseases caused by bacteria.Type: GrantFiled: July 25, 1995Date of Patent: September 2, 1997Assignee: Meiji Seika Kabushiki KaishaInventors: Kunio Atsumi, Eijiro Umemura, Yuko Kano, Sohjiro Shiokawa, Toshiaki Kudo, Masaki Tsushima, Katsuyoshi Iwamatsu, Atsushi Tamura, Seiji Shibahara
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Patent number: 5663163Abstract: The present invention relates to new cephem compounds, pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same and anti-bacterial methods of using the same. The subject cephem compounds comprise a thiadiazine ring bonded to the cephem through an iminoacetamido chain and a pyarzolium ring bonded to the cephem through a methylene chain.Type: GrantFiled: January 22, 1996Date of Patent: September 2, 1997Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Takao Takaya, Kazuo Sakane, Kenzi Miyai, Kohji Kawabata
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Patent number: 5661144Abstract: Compounds represented by the following formula (I), that is, cephem derivatives having substituted or unsubstituted 3-(imidazo[5,1-b]thiazolium-6-yl)-1-propenyl as a substituent at the 3-position of the cephem ring: ##STR1##Type: GrantFiled: June 28, 1996Date of Patent: August 26, 1997Assignee: Meiji Seika Kabushiki KaishaInventors: Masaki Tsushima, Kunio Atsumi, Katsuyoshi Iwamatsu, Atsushi Tamura
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Patent number: 5656623Abstract: Antimicrobial lactam-quinolone compounds comprising a lactam-containing moiety linked to a quinolone moiety, of the formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, R.sup.4 and R.sup.6 generally form any of a variety of quinolone, naphthyridine or related cyclic moieties known in the art to have antimicrobial activity; and(2) R.sup.1 or R.sup.3 contain a linking moiety, linking the quinolone moiety to a lactam-containing moiety having the formula: ##STR2## wherein (3) R.sup.10, R.sup.11, R.sup.12, R.sup.13, and R.sup.Type: GrantFiled: April 26, 1991Date of Patent: August 12, 1997Assignee: The Procter & Gamble CompanyInventors: Ronald Eugene White, Thomas Prosser Demuth, Jr.
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Patent number: 5620968Abstract: The invention provides compounds of the formula: ##STR1## wherein the variables are hereinbelow described; and salts thereof. Also, pharmaceutical formulations and methods for treating bacterial infections in man or other animals using the above compounds are disclosed.Type: GrantFiled: May 24, 1995Date of Patent: April 15, 1997Assignee: Eli Lilly and CompanyInventor: Ho-Shen Lin
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Patent number: 5604217Abstract: A 7-acyl-3-substituted carbamoyloxy cephem compound represented by the following formula (1): ##STR1## wherein A means a --CH.dbd. or --N.dbd. group; R.sup.1 denotes a hydroxyl, lower alkoxyl, fluorine-substituted lower alkoxyl or protected hydroxyl group; R.sup.2 and R.sup.3 are the same or different and individually represent a lower alkyl, hydroxyl-substituted lower alkyl, a carbamoyl-substituted lower alkyl group or cyano-substituted lower alkyl group, R.sup.2 is a hydrogen atom and R.sup.3 is a lower alkoxyl or alkyl group optionally substituted by one or more halogen atoms or the group ##STR2## means a 4-6 membered heterocyclic group, which contains one nitrogen atom, or a morpholino group, said heterocyclic group or morpholino group being optionally substituted by one or more lower alkyl, hydroxyl and/or hydroxyl-substituted lower alkyl groups; and R.sup.Type: GrantFiled: June 5, 1995Date of Patent: February 18, 1997Assignee: Eisai Co., Ltd.Inventors: Shigeto Negi, Motosuke Yamanaka, Kanemasa Katsu, Isao Sugiyama, Yuuki Komatu, Atsushi Kamata, Akihiko Tsuruoka, Yoshimasa Machida
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Patent number: 5602117Abstract: .beta.-lactam antibiotics of formula (I) or a salt thereof, wherein R.sup.1 is hydrogen, methoxy of formamido; R.sup.2 is an acyl group, in particular that of an antibacterially active cephalosporin; CO.sub.2 R.sup.3 is a carboxy group or a carboxylate anion, or R.sup.3 is a readily removable carboxy protecting group (such as a pharmaceutically acceptable in vivo hydrolysable ester group); R.sup.4 represents up to four substituents selected from alkyl, alkenyl, alkynyl, alkoxy, hydroxy, halogen, amino, alkylamino, acylamino, dialkylamino, CO.sub.2 R, CONR.sub.2, SO.sub.2 NR.sub.2 (where R is hydrogen or C.sub.1-6 alkyl), aryl and heterocyclyl, which may be the same or different and wherein any R.sup.4 alkyl substituent is optionally substituted by any other R.sup.4 substituent; X is S, SO, SO.sub.2, O or CH.sub.2 ; Y is S, SO or SO.sub.2 ; and m is 1 or 2, useful in the treatment of bacterial infections in humans and animals.Type: GrantFiled: June 1, 1994Date of Patent: February 11, 1997Assignee: Pfizer Inc.Inventors: George Burton, Stephen C. M. Fell
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Patent number: 5599557Abstract: A dry hydrated cephalosporin, e.g. ceftibuten having about 7 to 14% by weight of water, powder formulation, pharmaceutical compositions in the form of an oral suspension dosage form and a method of making the dry powder formulations are disclosed.Type: GrantFiled: October 27, 1994Date of Patent: February 4, 1997Assignee: Schering CorporationInventors: Donald A. Johnson, Lorraine Wearley, Rebecca Galeos, Joel A. Sequeira
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Patent number: 5595986Abstract: A stably storable and readily water soluble composition for use in preparing injections and containing Cefditoren, namely a cephalosporin of the formula ##STR1## is now provided, which composition comprises a physical mixture of Cefditoren or a non-toxic salt thereof with a proportion of arginine and/or lysine and/or a non-toxic salt thereof. This new composition of Cefditoren can be stored for long periods of time without discoloration and without undesirable reduction in the antibacterial activity, and the composition can be dissolved completely and quickly in water.Type: GrantFiled: August 2, 1995Date of Patent: January 21, 1997Assignee: Meiji Seika Kaisha, Ltd.Inventors: Makoto Okada, Masaki Takahashi, Kaoru Hosoi, Shokichi Nakajima
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Patent number: 5593984Abstract: The present invention relates to novel cephalosporin derivatives or pharmaceutically acceptable non-toxic salts thereof useful as antibiotics and to processes for the preparation thereof. ##STR1## wherein: R.sup.1 is a hydrogen or an optionally halogen-substituted C.sub.1-3 alkyl group, a propargyl group or --C(R.sup.a)(R.sup.b)COOH, wherein R.sup.1 and R.sup.b are independently a hydrogen or a C.sub.1-3 alkyl group;R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are independently a hydrogen or halogen or a C.sub.1-3 alkyl, amino or hydroxy C.sub.1-3 alkylthio, cyano, carbamoyl, carboxyl, hydroxy C.sub.1-3 alkyl, nitro, acetyl or formyl group; andQ is CH, N or CCl.Type: GrantFiled: March 31, 1995Date of Patent: January 14, 1997Assignee: Yuhan CorporationInventors: Jong W. Lee, Jeong S. Chae, Young R. Choi, Yeong N. Lee, Eun R. Rho, Heui I. Kang, Jae W. Hyun
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Patent number: 5587373Abstract: The present invention provides cephalosporin sulphones of formula (I) and the pharmaceutically and veterinarily acceptable salts thereof: ##STR1## wherein n is one or two: A and B are both or each independently hydrogen or an organic radical;R.sup.1 represents halogen, A, OA, --S(O).sub.m A wherein m is 0-2, --OC(O)A, --OS(O).sub.2 A, --NHC(O)A or --NH--Z wherein Z is a mono, di- or tripeptide and A is as defined above;R.sup.2 represents a halogen, A, --S(O).sub.m A, --O--A, --C(O)A, --C(O)OA, --CH.sub.2 --OA, --CH.sub.2 S(O).sub.m A, --CH.sub.2 OC(O)A, --CH.sub.2 O--Z, --CH.sub.2 SC(O) A, --CH.sub.2 --N(A)A, --CH.sub.2 N.sup.+ (A)(A')A", --CH.sub.2 NH--C(O)A or --CH.sub.2 NH--Z wherein A and Z are as defined above.The compounds of formula (I) and their salts are elastase inhibitors.Type: GrantFiled: November 4, 1994Date of Patent: December 24, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Marco Alpegiani, Pierluigi Bissolino, Ettore Perrone
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Patent number: 5587372Abstract: A syn isomer in (R) or (S) form or a mixture thereof of a compound of the formula ##STR1## syn isomer, in the (R) or (S) form or in the form of an (R,S) mixture, in the form of an internal salt or their salts with organic or mineral acids,wherein the variables are herein below defined, having antibacterial properties.Type: GrantFiled: December 13, 1993Date of Patent: December 24, 1996Assignee: Roussel UclafInventors: Jozsef Aszodi, Jean-Francois Chantot, Patrick Fauveau, Solange G. D'Ambrieres, Daniel Hunbert, Christophe Dini
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Patent number: 5585372Abstract: The present invention provides compounds of formula (I) and pharmaceutically or veterinarily salts thereof; ##STR1## wherein R.sub.1 is hydrogen or halogen or an organic group; R.sub.2 is hydrogen or an optionally substituted C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.6 -C.sub.10 aryl or C.sub.7 -C.sub.14 aralkyl group;R.sub.3 is hydrogen or halogen, or an organic groupR.sub.4 is hydrogen or a group defined as R.sub.2 above or R.sub.4 taken together with R.sub.3 constitutes a C.sub.2 -C.sub.6 alkanediyl or an alkanediyl radical optionally substituted by methyl or phenyland X is either oxygen or sulphur or NR.sub.6, wherein R.sub.6 is either hydrogen or a group as defined for R.sub.2. A process for their preparation by cyclization of appropriate intermediates is also described.The compounds of formula I and the pharmaceutically and veterinarily acceptable salts thereof are elastase inhibitors.Type: GrantFiled: January 20, 1995Date of Patent: December 17, 1996Assignee: Pharmacia S.p.A.Inventors: Marco Alpegiani, Pierluigi Bissolino, Ettore Perrone, Vincenzo Rizzo
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Patent number: 5580865Abstract: The present invention provides cephalosporin sulphones or formula (I), and pharmaceutically or veterinarily acceptable salts thereof; ##STR1## wherein n is zero, one or two; R.sub.1 is hydrogen, halogen or an optionally substituted C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio or C.sub.1 -C.sub.4 carboxamido group;R.sub.2 is hydrogen or an optionally substituted C.sub.1 -C.sub.8 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.2 -C.sub.5 alkenyl or C.sub.3 -C.sub.6 cycloalkyl group;R.sub.3 is hydrogen or acetoxymethyl, methoxymethyl, methyl or an optionally substituted heterocyclylthiomethyl group;R.sub.4 is an optionally substituted C.sub.1 -C.sub.8 alkyl, C.sub.2 -C.sub.6 alkenyl, aryl(C.sub.1 -C.sub.8)alkyl or heterocyclyl(C.sub.1 -C.sub.8)alkyl group; andR.sub.5 is an optionally substituted C.sub.6 -C.sub.10 aryl or a heterocyclyl group.The compounds of formula I and the pharmaceutically and veterinarily acceptable salts thereof are elastase inhibitors.Type: GrantFiled: April 5, 1993Date of Patent: December 3, 1996Assignee: Farmitalia Carlo Erba S.r.l.Inventors: Marco Alpegiani, Pierluigi Bissolino, Ettore Perrone, Vincenzo Rizzo
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Patent number: 5556850Abstract: The invention relates to crystalline acid addition salt of the two diastereomers of the 1-(2,2-dimethylpropionyloxy)ethyl 3-cephem-4-carboxylate of the general formula II ##STR1## in which X is the anion of a physiologically acceptable, mono- or polybasic, inorganic or organic acid and the group .dbd.N--OH is in the syn-position, pharmaceutical formulations which are active against bacterial infections and contain such cephem derivatives, processes for the preparation of the cephem derivatives and the use of the cephem derivatives for combating bacterial infections.Type: GrantFiled: May 23, 1995Date of Patent: September 17, 1996Assignee: Hoechst AktiengesellschaftInventors: Elisabeth Defossa, Gerd Fischer, Joachim-Heiner Jendralla, Rudolf Lattrell, Theodor Wollmann, Dieter Isert
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Patent number: 5541175Abstract: The present invention relates to a cephalosporin compound represented by the following general formula (I): ##STR1## its pharmaceutically acceptable non-toxic salt, physiologically hydrolyzable ester, hydrate or solvate, or isomers thereof, in whichR.sup.1 represents hydrogen or an amino-protecting group,R.sup.2 and R.sup.3 can be identical or different and independently of one another represent hydrogen or a hydroxy-protecting group, orR.sup.2 and R.sup.3 together can form a cyclic diol-protecting group,R.sup.4 represents hydrogen or a carboxyl-protecting group,R.sup.5, R.sup.6 and R.sup.7 independently of one another represent hydrogen, amino or substituted amino, hydroxy, alkoxy, C.sub.1-4 alkyl, carboxyl or alkoxycarbonyl, orR.sup.5 and R.sup.6 together with the carbon atoms to which they are attached can form a C.sub.3-7 cycle, andQ represents CH or N,and to a process for preparation thereof and a pharmaceutical composition containing the compound (I) as an active ingredient.Type: GrantFiled: September 7, 1994Date of Patent: July 30, 1996Assignee: Lucky, Ltd.Inventors: Jae H. Yeo, Chan S. Bang, Jong C. Lim, Young M. Woo, Deog H. Yang, Se H. Kim, Jae H. Jeon, Mu Y. Kim, Sam S. Kim, Tae H. Lee, Yong Z. Kim, Hun S. Oh