6,6-di-substituted Patents (Class 514/194)
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Patent number: 8299051Abstract: Inhibitors of the enzyme beta-lactamase of formula (I): are provided. The compounds are adapted to inhibit beta-lactamase as produced by beta-lactam resistant bacterial strains. Methods of treatment of beta-lactam resistant bacterial infections in patients are provided.Type: GrantFiled: May 11, 2009Date of Patent: October 30, 2012Assignee: Southern Methodist UniversityInventors: John D. Buynak, Anjaneyulu Sheri, Sundar Ram Reddy Pagadala
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Patent number: 7723389Abstract: The invention provides pharmaceutical compositions for the treatment or prevention of the toxic effects of therapeutic agents and methods of treating or preventing such toxicity using a toxicity reducing amount of N-acetylcysteine either alone or in combination with a therapeutically effective amount or, to achieve its therapeutic advantages, an amount larger than what is customarily given as a therapeutically effective amount, of a therapeutic agent.Type: GrantFiled: November 4, 2002Date of Patent: May 25, 2010Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Leonard A. Herzenberg, Leonore A. Herzenberg, Stephen C. De Rosa, James Andrus
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Publication number: 20080318918Abstract: Methods for treating and preventing middle ear infections by transmembrane administration of medicament-containing transmembrane carrier compositions comprising a nonionic polymer surfactant, such as an alkyl aryl polyether alcohol (e.g., tyloxapol) to the tympanic membrane. The medicaments delivered according to the methods of the invention include antibiotic, antiviral, anti-fungal and anti-inflammatory agents that are useful in treatment and/or prophylaxis of middle ear infections and their sequelae.Type: ApplicationFiled: August 25, 2006Publication date: December 25, 2008Inventors: William R. Campbell, Neil E. Paulsen, Roland H. Johnson
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Patent number: 7169771Abstract: The present invention provides thiazolyl-based compounds of formula (I), useful for treating p38 kinase-associated conditions, wherein ring A is phenyl or pyridyl, and X, Y, B, R2, R3, Z1 m and n are as defined herein. The invention further pertains to pharmaceutical compositions containing at least one compound according to the invention useful for treating p38 kinase-associated conditions, and methods of inhibiting the activity of p38 kinase in a mammal.Type: GrantFiled: February 6, 2004Date of Patent: January 30, 2007Assignee: Bristol-Myers Squibb CompanyInventors: John Hynes, Hong Wu, Katerina Leftheris, Chunjian Liu, Jagabandhu Das, Robert V. Moquin
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Patent number: 7094431Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.Type: GrantFiled: September 30, 2003Date of Patent: August 22, 2006Inventor: Mickey L. Peshoff
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Patent number: 6852742Abstract: The present invention is directed in part towards methods of modulating the function of calcium channels with pyridine- or 1,4-dihydropyridine-based compounds. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to pyridine- or 1,4-dihydropyridine-based compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: January 14, 2003Date of Patent: February 8, 2005Assignee: Vittal Mallya Scientific Research FoundationInventors: Phani Kumar Pullela, Paramashivappa Rangappa, Srinivasa Rao Alapati, Pillarisetti V. Subbarao, Jeffrey A. Bibbs
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Patent number: 6569679Abstract: The present invention provides recombinant viral vectors carrying a vector construct which directs the expression of a gene product (e.g., HSVTK) that activates a compound with little or no cytotoxicity into a toxic product. Also provided are methods of destroying or inhibiting pathogenic agents in a warm blooded animal, comprising the step of administering to the animal a viral vector such as that described above, in order to inhibit or destroy the pathogenic agent.Type: GrantFiled: June 6, 1995Date of Patent: May 27, 2003Assignee: Chiron CorporationInventors: Jack R. Barber, Harry E. Gruber, Douglas J. Jolly
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Patent number: 6495539Abstract: Compounds of the formula and the salts, esters and amides thereof wherein Z is S, SO, SO2 or O; each of R1, R2 and R3 is independently H or substituted or unsubstituted alkyl (1-10C), substituted or unsubstituted alkenyl, substituted or unsubstituted acyl (2-11C), substituted or unsubstituted aryl (6-14C), substituted or unsubstituted arylcarbonyl (7-15C), substituted or unsubstituted arylalkyl (7-15C), substituted or unsubstituted pyridyl wherein substituents on any alkyl, alkenyl, or acyl moiety are selected from the group consisting of halo, and RO, wherein R is H or alkyl (1-6C), and substituents on any aryl or pyridyl moiety are selected from the group consisting of halo, and RO, where R is H or alkyl (1-6C), —CN and —CF3; with the proviso that R1 is not H and R1 and R3 are not identical and with the proviso that in formula (1), the B ring may contain one double bond that is located between positions 2 and 3, and in formula (2), the B ring may contain one double bond thaType: GrantFiled: February 19, 1999Date of Patent: December 17, 2002Assignee: Washington UniversityInventors: Scott J. Hultgren, Fredrik Almqvist, Gabriel Soto
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Patent number: 6436398Abstract: Compound of formula I: wherein R1, R2, R3, R4 and n 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 novel intermediates useful for the synthesis of compounds of formula I.Type: GrantFiled: November 29, 2000Date of Patent: August 20, 2002Assignee: Research Corporation Technologies, Inc.Inventors: John D. Buynak, Akireddy Srinivasa Rao, Venkata Ramana Doppalapudi
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Patent number: 6403572Abstract: There is disclosed a process for producing an acid salt of a (Z)-2-aminothiazole compound of the formula (I): wherein R1 and R2 independently represent an alkyl group having 1 to 5 carbon atoms, Y represents a halogen atom, —OSO3H or —OPO(OH)2, m indicates the valence number of an inorganic acid of the formula: HY wherein Y represents the same as defined above, and n indicates an integer of 1 or 2, which process is characterized by: reacting an acid salt of a 2-aminothiazole compound of the formula (II): wherein R1 and R2 independently represent an alkyl group having 1 to 5 carbon atoms, X represents a bromine atom or an iodine atom, and the wavy line means that this compound is a mixture of the E- and Z-isomers, with the inorganic acid of the formula HY.Type: GrantFiled: November 26, 2001Date of Patent: June 11, 2002Assignees: Sumitomo Chemical Co., Ltd., Shionogi & co., Ltd.Inventors: Isao Kurimoto, Norihiko Hirata, Akihiko Nakamura, Yuichiro Aratake
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Patent number: 6166014Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: May 19, 1999Date of Patent: December 26, 2000Assignee: Berlex Laboratories, Inc.Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
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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: 5538962Abstract: The present invention provides a compound of the formula (I) ##STR1## wherein: R.sup.1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl;R.sup.2 is hydrogen or C.sub.1-4 alkyl;Z is carboxy, sufonic acid, tetrazol-5-yl or C .sub.1-4 alkylsulfonylcarbamoyl (--CONHSO.sub.2 C.sub.1-4 alkyl);A is a phenyl or thienyl ring;and A is optionally further substituted by one or two substituents or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.Type: GrantFiled: October 6, 1993Date of Patent: July 23, 1996Assignee: Zeneca LimitedInventor: Patrice J. Siret
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Patent number: 5384346Abstract: Polyvinyl butyrals (PVBs) with improved thermal stability and improved light resistance contain as stabilizers polynuclear phenols which phenolic radicals have a quaternary carbon atom in the para-position to the phenolic hydroxyl group and if desired in combination with synergistically acting, nitrogen-containing, sulfur-containing or phosphorus-containing co-stabilizers of the types a) to d). The use of the resulting films of low yellowness as interlayer films having substantially reduced yellowing for the production of laminated glasses and glass composites of silicate glass sheets is described.Type: GrantFiled: May 6, 1993Date of Patent: January 24, 1995Assignee: Hoechst AGInventors: Matthas Gutweiler, Ulrich Hutten, Gerhard Pfahler, Hermann Schindler
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Patent number: 5180719Abstract: Antimicrobial quinolonyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula: ##STR1## wherein (1) R.sup.3, R.sup.4, and R.sup.5, together with bonds "a" and "b", form certain lactam-containing moieties similar to those known in the art to have antimicrobial activity; and(2) A.sup.2, A.sup.2, A.sup.3, R.sup.7, R.sup.8, and R.sup.9 form any of a variety of quinolone or naphthyridine structures similar to those known in the art to have antimicrobial activity.Type: GrantFiled: April 29, 1991Date of Patent: January 19, 1993Assignee: Norwich Eaton Pharmaceuticals, Inc.Inventors: Ronald E. White, Thomas P. Demuth, Jr.
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Patent number: 4877783Abstract: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.Type: GrantFiled: January 24, 1985Date of Patent: October 31, 1989Assignee: Beecham Group p.l.c.Inventor: Peter H. Milner
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Patent number: 4847247Abstract: Derivatives of Penicillin, their sulfoxides and sulfones are found to be potent elastase inhibitors and thereby useful anti-inflammatory/antidegenerative agents.Type: GrantFiled: October 16, 1986Date of Patent: July 11, 1989Assignee: Merck & Co., Inc.Inventors: Kevan R. Thompson, Paul E. Finke, James B. Doherty
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Patent number: 4829053Abstract: New aminoacid derivatives of the formula IX--Z--NR.sup.2 --CHR.sup.3 --CR.sup.4 --(CHR.sup.5).sub.n --CO--E--NR.sup.6 --(CHR.sup.7).sub.s --D Iwherein X, Z, R.sup.2, R.sup.3, R.sup.4, R.sup.5, E, R.sup.6, R.sup.7, D, n and s have the meanings defined herein and their salts, inhibit the activity of human plasma renin.Type: GrantFiled: July 31, 1987Date of Patent: May 9, 1989Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Peter Raddatz, Joachim Gante, Claus J. Schmitges, Klaus Otto Minck, Johannes Sombroek, Gunter Holzemann
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Patent number: 4820701Abstract: Antibacterial agents have the formula (I) or are pharmaceutically acceptable salts or in vivo hydrolysable esters thereof: ##STR1## wherein R.sup.3 is phenyl, substituted phenyl, cyclohexenyl, cyclohexadienyl or an optionally substituted 5- or 6-membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphur or nitrogen, R.sup.4 is hydrogen or formamido, R.sup.5 is hydrogen, C.sub.1-6 alkyl, substituted alkyl, aryl or aralkyl, R.sup.6 and R.sup.7 are the same or different and represent hydrogen, C.sub.1-6 alkyl, substituted alkyl, halogen, amino, phenyl, substituted phenyl, hydroxyl or C.sub.1-6 alkoxy or R.sup.6 and R.sup.7 form the residue of an optionally substituted 5- or 6-membered carbocyclic ring or a 5- or 6- membered heterocyclic ring containing up to three hetero atoms selected from oxygen, sulphr or nitrogen, and X represents ##STR2## or tautomers thereof wherein R.sup.8 and R.sup.9 are the same or different and each represents hydroxy, or protected hydroxy.Type: GrantFiled: October 21, 1987Date of Patent: April 11, 1989Assignee: Beecham Group p.l.c.Inventors: Robert Southgate, Colin H. Frydrych
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Patent number: 4748163Abstract: Antibacterially active and animal growth-promoting novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents the radical ##STR2## Y representing N or CR.sup.9, or Y--R.sup.7 representing >C.dbd.O or >C.dbd.N--R.sup.7,Z representing O, S, or NR.sup.10, andR.sup.2 represents hydrogen or a protective group.Type: GrantFiled: February 21, 1986Date of Patent: May 31, 1988Assignee: Bayer AktiengesellschaftInventors: Gunter Schmidt, Hans-Joachim Zeiler, Karl G. Metzger
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Patent number: 4734407Abstract: Antibacterially active and animal growth-regulating novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents an optionally substituted radical of the formula ##STR2## Z represents oxygen, sulphur or --N--R.sup.Type: GrantFiled: March 10, 1986Date of Patent: March 29, 1988Assignee: Bayer AktiengesellschaftInventors: Gunter Schmidt, Hans-Joachim Zeiler, Karl G. Metzger
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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: 4684639Abstract: A compound having the partial structure (I) ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and each is hydrogen or a group --COR.sup.5 or --CO--OR.sup.5 wherein R.sup.5 represents an optionally substituted hydrocarbon group; R.sup.3 is halogen and R.sup.4 is hydrogen, methoxy, hydroxymethyl or formamido.These compounds are suitably bicyclic .beta.-lactam antibiotics.Type: GrantFiled: July 5, 1984Date of Patent: August 4, 1987Assignee: Beecham GroupInventors: George Burton, Desmond J. Best
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Patent number: 4675317Abstract: Disclosed are 6- and 6,6-disubstituted-2-substituted thio-pen-2-em-3-carboxylic acids of the following structure: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from: hydrogen; substituted and unsubstituted: alkyl, cycloalkyl, halo, alkoxyl, alkenyl, aralkyl, aryl, heterocyclyl, heteroaryl, and heterocyclylalkyl; W is an electron withdrawing group, and, for example, is selected from: --COR.sup.5, --CN, SO.sub.2 C.sub.6 H.sub.5 ; R.sup.5 is hydrogen; substituted and unsubstituted: alkyl, aryl, aralkyl, heteroaryl, heterocyclyl, or heterocyclylalkyl; or R.sup.5 may be --OR.sup.6, --NR.sup.7 R.sup.8, and --SR.sup.9 ; wherein R.sup.6 is H; substituted and unsubstituted: alkyl, alkenyl, or a group which defines --CO.sub.2 R.sup.6 as a pharmaceutically acceptable ester wherein R.sup.6 is, for example, phthalidyl, or 5-methyl-2-oxo-1,3-dioxolen-4-ylmethyl; R.sup.7 and R.sup.Type: GrantFiled: January 25, 1983Date of Patent: June 23, 1987Assignee: Merck & Co., Inc.Inventors: Frank P. DiNinno, William J. Leanza, Ronald W. Ratcliffe, David A. Muthard
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Patent number: 4670431Abstract: A compound having the partial structure (A): ##STR1## wherein n is 1 or 2.Type: GrantFiled: January 19, 1984Date of Patent: June 2, 1987Assignee: Beecham Group p.l.c.Inventor: Peter H. Milner
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Patent number: 4647457Abstract: .beta.-lactams of the formula ##STR1## wherein R.sup.1 signifies hydrogen or a group readily cleavable by hydrolysis, A signifies the group R.sup.2 --N.dbd.C(CH.sub.3)--CH.dbd.C< or O.dbd.C(CH.sub.3)--CH.sub.2 --C(R.sup.3)<, R.sup.2 signifies hydroxy, lower alkoxy or arylamino and R.sup.3 signifies arylthio, lower alkanoylthio, lower alkoxycarbonylhydrazino or a N-containing saturated heterocycle attached via a N-atom, and pharmaceutically acceptable salts thereof, are disclosed. The compounds and their salts exhibit .beta.-lactamase inhibiting activities against .beta.-lactamases from bacteria.Type: GrantFiled: March 2, 1984Date of Patent: March 3, 1987Assignee: Hoffmann-La Roche Inc.Inventor: Solange Adam-Molina
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Patent number: 4614738Abstract: This invention relates to 2-(N-heterocycloaliphaticthio)penems wherein the nitrogen of the heterocyclic ring is connected to the alkyl group, and to their use as antibacterial agents.Type: GrantFiled: March 25, 1983Date of Patent: September 30, 1986Assignee: Schering CorporationInventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace
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Patent number: 4609652Abstract: .beta.-Lactam antibiotics having an .alpha.-formamido substituent on the carbon atom adjacent to the carbonyl group of the .beta.-lactam ring and in particular bicyclic compounds having the partial structure: ##STR1## Intermediates and processes for the preparation of the compounds are further disclosed.Type: GrantFiled: January 24, 1985Date of Patent: September 2, 1986Assignee: Beecham Group p.l.c.Inventor: Peter H. Milner
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Patent number: 4596677Abstract: A novel stereocontrolled process is disclosed for converting 6-aminopenicillanic acid to an optically active azetidinone of the formula ##STR1## wherein R" is a hydroxy-protecting group by use of a 6,6-dihaloanhydropenicillin or 6,6-bis(phenylselenyl)anhydropenicillin intermediate.Type: GrantFiled: April 6, 1984Date of Patent: June 24, 1986Assignee: Bristol-Myers CompanyInventors: Alain Martel, Jean-Paul Daris
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Patent number: 4540689Abstract: 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: September 10, 1985Assignee: Kureha Kagaku Kogyo Kabushiki KaishaInventors: Shigeaki Muto, Kouichi Niimura, Takao Ando, Akihiko Kanno, Takao Furusho, Chikao Yoshikumi
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Patent number: 4537886Abstract: A compound of formula (1) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R.sup.1 is phenyl, substituted phenyl or a 5- or 6-membered heterocyclic ring containing up to three heteroatoms selected from oxygen, sulphur or nitrogen, optionally substituted with hydroxy, amino, halogen or C.sub.1-6 alkoxy;X represents; ##STR2## wherein R.sup.Y is methyl or acetyl; R.sup.2 and R.sup.3 may be the same or different and each is hydrogen, an aryl group, a heterocyclyl group or a C.sub.1-6 alkyl group optionally substituted by an aryl group or a heterocyclyl group; and R.sup.4 is hydrogen, a C.sub.1-6 alkylcarbonyl group, an aryl group, a heterocyclyl group, a C.sub.1-6 alkyl group optionally substituted by an aryl group or a heterocyclyl group;R.sup.5 represents, hydrogen, methoxy or --NHCHO; and Y is: ##STR3## wherein Y.sup.1 is oxygen, sulphur or --CH.sub.2 -- and Z represents hydrogen, halogen or an organic group such as C.sub.1-4 alkoxy, --CH.sub.2 Q or --CH.dbd.Type: GrantFiled: March 29, 1983Date of Patent: August 27, 1985Assignee: Beecham Group p.l.c.Inventors: Andrew W. Taylor, Richard T. Cook
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Patent number: 4505915Abstract: This invention relates to a new class of penicillins (I) and their pharmaceutically acceptable salts and esters which are useful as antibiotics: ##STR1## wherein the stylized radical (hereafter referred to as R'): ##STR2## attached to the 6-amino nitrogen moiety of the penicillin (or ring analogue thereof) nucleus represents a mono- or polycyclic N-containing heterocyclic group;X is S, SO, CH.sub.2, or O; m is 0, 1 or 2;R is, inter alia, hydrogen, substituted and unsubstituted: alkyl, aryl, alkenyl, heterocyclylalkyl, heterocyclylalkenyl, aralkenyl, aralkyl, --NR.sub.2, COOR, CONR.sub.2, --OR, or CN;R.sup.2 is H, or lower alkoxyl.Type: GrantFiled: March 16, 1981Date of Patent: March 19, 1985Assignee: Merck & Co., Inc.Inventor: John Hannah
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Patent number: RE33948Abstract: Antibacterially active and animal growth-promoting novel .beta.-lactam compounds of the formula ##STR1## in which R.sup.1 represents the radical ##STR2## Y representing N or CR.sup.9, or Y--R.sup.7 representing ##STR3## Z representing O, S, or NR.sup.10, and R.sup.2 represents hydrogen or a protective group.Type: GrantFiled: August 29, 1989Date of Patent: June 2, 1992Assignee: Bayer AktiengesellschaftInventors: Gunter Schmidt, Hans-Joachim Zeiler, Karl G. Metzger