Spiro Or Additional Polycyclo Ring System Patents (Class 514/193)
  • Patent number: 10889577
    Abstract: The present disclosure relates to crystalline solid forms of a stimulator of soluble guanylate cyclase (sGC), Compound I: Also provided herein are methods for the preparation of these solid forms. The invention also relates to pharmaceutical formulations and dosage forms comprising these solid forms and their uses thereof, alone or in combination with one or more additional agents, for treating and/or preventing various diseases or disorders; these diseases or disorders are ones that may benefit from sGC stimulation or from an increase in the concentration of nitric oxide (NO) and/or cyclic guanosine monophosphate (cGMP).
    Type: Grant
    Filed: July 6, 2017
    Date of Patent: January 12, 2021
    Assignee: Cyclerion Therapeutics, Inc.
    Inventors: Vasu Sethuraman, Ahmad Hashash, Song Xue, Robert C. Livingston, Kwame Wiredu Nti-Addae
  • Patent number: 10836721
    Abstract: Thalidomide analogs and methods of using the thalidomide analogs are disclosed. Some embodiments of the disclosed compounds exhibit anti-angiogenic and/or anti-inflammatory activity. Certain embodiments of the disclosed compounds are non-teratogenic.
    Type: Grant
    Filed: June 24, 2020
    Date of Patent: November 17, 2020
    Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, University Court of the University of Aberdeen
    Inventors: Nigel H. Greig, Weiming Luo, David Tweedie, Neil Vargesson, Shaunna Beedie, William Douglas Figg
  • Patent number: 10730835
    Abstract: Thalidomide analogs and methods of using the thalidomide analogs are disclosed. Some embodiments of the disclosed compounds exhibit anti-angiogenic and/or anti-inflammatory activity. Certain embodiments of the disclosed compounds are non-teratogenic.
    Type: Grant
    Filed: September 29, 2016
    Date of Patent: August 4, 2020
    Assignees: The United States of America, as represented by the Secretary, Health and Human Services, University Court of the University of Aberdeen
    Inventors: Nigel H. Greig, Weiming Luo, David Tweedie, Neil Vargesson, Shaunna Beedie, William Douglas Figg
  • Patent number: 10376585
    Abstract: This invention relates to a composition, including penethamate (PNT) or a pharmaceutical equivalent thereof; and at least one oily vehicle.
    Type: Grant
    Filed: July 16, 2013
    Date of Patent: August 13, 2019
    Assignee: BAYER NEW ZEALAND LTD
    Inventors: Fadil Al Alawi, Olaf Bork, Rohit Jain, Karthigeyan Nanjan, Ian George Tucker
  • Patent number: 10144708
    Abstract: The present invention provides novel crystal forms of arylalkylamine compounds. Specifically, the novel crystal forms of 4-(3S-(1R-(1-naphthyl)ethylamino)pyrrolidin-1-yl)phenylacetic acid have excellent stability and therefore are useful as pharmaceutical ingredients. The present invention also provides industrially advantageous processes for producing the arylalkylamine compounds.
    Type: Grant
    Filed: March 30, 2017
    Date of Patent: December 4, 2018
    Assignee: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Hiroshi Miyazaki, Takao Komasaka, Joji Tsurumoto, Takeshi Uemura, Yuuji Morita
  • Patent number: 9518004
    Abstract: A reduced coenzyme Q10 derivative represented by formula (1), wherein R1 and R2 are each independently H or an alkoxycarbonyl group represented by formula (2), and at least one of them is an alkoxycarbonyl group represented by the formula (2); in the formula (2), R3 is an optionally substituted linear, branched, or cyclic alkyl group having 1 to 20 carbon atoms, an optionally substituted aryl group having 6 to 20 carbon atoms, or an optionally substituted heteroaryl group having 4 to 20 carbon atoms, and when R3 is a group substituted with polyethylene glycol, the molecular weight of the polyethylene glycol is not more than 300.
    Type: Grant
    Filed: December 2, 2013
    Date of Patent: December 13, 2016
    Assignee: KANEKA CORPORATION
    Inventors: Teruyoshi Koga, Yoshihisa Okamoto, Takao Yamaguchi
  • Publication number: 20140271921
    Abstract: A topical composition comprises at least 5 wt % metronidazole or a pharmacologically acceptable derivative thereof in a non-aqueous vehicle. The composition may be used in the treatment of conditions of the colon, rectum, anorectum and perianal region, in particular inflammatory bowel disease and perianal Crohn's disease. The composition also relieves pain and inflammation and promotes healing of the colon, rectum, anorectum and perianal region following surgical operations. One advantage of the composition is that topical administration of metronidazole results in a primarily local effect and thus side effects observed from systemic administration are avoided.
    Type: Application
    Filed: May 28, 2014
    Publication date: September 18, 2014
    Applicant: SLA PHARMA AG
    Inventor: DAVID NIGEL ARMSTRONG
  • Patent number: 8324175
    Abstract: The present invention discloses anti-cancer compositions, and associated methods, including an anti-cancer composition comprising: a cellular energy inhibitor having the structure according to formula I wherein X is selected from the group consisting of: a nitro, an imidazole, a halide, sulfonate, a carboxylate, an alkoxide, and amine oxide; and R is selected from the group consisting of: OR?, N(R?)2, C(O)R??, C1-C6 alkyl, C6-C12 aryl, C1-C6 heteroalkyl, a C6-C12 heteroaryl, H, and an alkali metal; where R? represents H, alkali metal, C1-C6 alkyl, C6-C12 aryl or C(O)R??, R? represents H, C1-C6 alkyl, or C6-C12 aryl, and R?? represents H, C1-C20 alkyl or C6-C12 aryl. The anti-cancer composition can additionally comprise at least one sugar, which stabilizes the cellular energy inhibitor by substantially preventing the inhibitor from hydrolyzing. Also, the anti-cancer composition can comprise a hexokinase inhibitor.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: December 4, 2012
    Inventor: Young Hee Ko
  • Publication number: 20120065182
    Abstract: The present invention is directed to improved liquid antibiotic formulations. In some embodiments, the present invention is directed to a composition comprising an antibiotic in a liquid comprising triglycerides, wherein the composition has less than about 5% water (w/v).
    Type: Application
    Filed: November 18, 2011
    Publication date: March 15, 2012
    Applicant: Taro Pharmaceuticals North America, Inc.
    Inventors: Shen GAO, Daniel A. Moros, Satish Asotra
  • Publication number: 20110288063
    Abstract: A compound of formula (I) or formula (Ia) Wherein R1, Ra, R2, X, R3, Y1, Y2, A, B and C are as defined herein. Also, pharmaceutical compositions comprising such compounds and excipients, methods of treating bacterial infections comprising administering such compounds, methods for making such compounds and hydrates of such compounds.
    Type: Application
    Filed: May 19, 2011
    Publication date: November 24, 2011
    Applicant: Naeja Pharmaceutical Inc.
    Inventors: Samarendra N. MAITI, Rong Ling, Judy Yip, Chuanjun Gao, Dai Nguyen, Biswajeet Ganguli, Hong Liang, Jehangir Khan, Andhe V. Narender Reddy
  • Publication number: 20110182869
    Abstract: This invention relates to products comprising antibiotics or probiotics and the use thereof for the treatment of gut motility disorders such as irritable bowel syndrome (IBS).
    Type: Application
    Filed: July 14, 2009
    Publication date: July 28, 2011
    Inventors: Jan Knol, Kaouther Ben Amor, Richèle Deodata Wind
  • Publication number: 20100227843
    Abstract: ?-lactamase resistant cephalosporin ester compound chosen from those represented by formula (I): wherein, and pharmaceutical salts thereof, composition thereof, and use thereof are disclosed.
    Type: Application
    Filed: May 21, 2010
    Publication date: September 9, 2010
    Applicant: ZHEJIANG YONGNING PHARMACEUTICAL FACTORY
    Inventors: Fengqi YE, Shanzong FANG, Xiuwel LU
  • Patent number: 7723389
    Abstract: 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: Grant
    Filed: November 4, 2002
    Date of Patent: May 25, 2010
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Leonard A. Herzenberg, Leonore A. Herzenberg, Stephen C. De Rosa, James Andrus
  • Publication number: 20100040548
    Abstract: The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.
    Type: Application
    Filed: June 10, 2009
    Publication date: February 18, 2010
    Inventor: Chongxi Yu
  • Patent number: 7241756
    Abstract: A method for the treatment of diabetes mellitus, especially Type 2 diabetes and conditions associated with diabetes mellitus in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of a dipeptidyl peptidase IV inhibitor and another antidiabetic agent, to a mammal in need thereof.
    Type: Grant
    Filed: June 1, 2006
    Date of Patent: July 10, 2007
    Assignee: SmithKline Beecham Corporation
    Inventors: Jonathan Robert Sanders Arch, James Martin Lenhard
  • Patent number: 7112582
    Abstract: The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof. wherein one of A and B denotes hydrogen and the other an optionally substituted fused bicyclic heteroaryl group; and X is S.
    Type: Grant
    Filed: May 1, 2003
    Date of Patent: September 26, 2006
    Assignee: Wyeth
    Inventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Itsuki Yamamura, Tsuyoshi Takasaki, Atul Agarwal, Osvaldo dos Santos, Fuk-Wah Sum, Yang-I Lin
  • Patent number: 7094431
    Abstract: 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: Grant
    Filed: September 30, 2003
    Date of Patent: August 22, 2006
    Inventor: Mickey L. Peshoff
  • Patent number: 7078397
    Abstract: Disclosed is a method for the treatment of diabetes mellitus, especially Type 2 diabetes and conditions associated with diabetes mellitus in a mammal such as a human, which method comprises administering an effective, non-toxic and pharmaceutically acceptable amount of a dipeptidyl peptidase IV inhibitor and another antidiabetic agent, to a mammal in need thereof.
    Type: Grant
    Filed: June 19, 2001
    Date of Patent: July 18, 2006
    Assignee: SmithKline Beecham Corporation
    Inventors: Jonathan Robert Sanders Arch, James Martin Lenhard
  • Patent number: 7018997
    Abstract: The present invention provides a compound of formula I, pharmaceutical compositions and the use thereof for the treatment of bacterial infection or disease in a patient in need thereof. wherein one of A and B denotes hydrogen and the other an optionally substituted fused tricyclic heteroaryl group; and X is S.
    Type: Grant
    Filed: May 1, 2003
    Date of Patent: March 28, 2006
    Assignee: Wyeth
    Inventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Ado Mihira, Atul Agarwal, Hideki Ushirogochi, Yansong Gu, Satoshi Tamai, Fuk-Wah Sum
  • Publication number: 20030124597
    Abstract: A nucleic acid sequence which regulates the autolytic activity of bacteria is provided. Methods for identifying and using agents which interact with the gene to inhibit bacterial growth and infectivity also are provided.
    Type: Application
    Filed: November 6, 2002
    Publication date: July 3, 2003
    Inventor: Ambrose Cheung
  • Publication number: 20030124141
    Abstract: The invention provides Helicobacter polypeptides that can be used in vaccination methods for preventing or treating Helicobacter infection, and polynucleotides that encode these polypeptides.
    Type: Application
    Filed: November 16, 2001
    Publication date: July 3, 2003
    Inventors: Rainer Haas, Harold Kleanthous, Jean-Francois Tomb, Charles Miller, Amal Al-Garawi, Stefan Odenbreit, Thomas Meyer
  • Publication number: 20030100002
    Abstract: A nucleic acid sequence which regulates the autolytic activity of bacteria is provided. Also provided are polypeptides encoded by these nucleic acid sequences or mutants thereof as well as vector and host cells for expressing these polypeptides. Methods for identifying and using agents which prevent or reduce multiple antibiotic resistance also are provided.
    Type: Application
    Filed: November 6, 2002
    Publication date: May 29, 2003
    Inventor: Ambrose Cheung
  • Patent number: 6489316
    Abstract: The 6-(spirocyclopropyl)-penicillanic acid 4,4-dioxides of the general Formula (I): as defined herein above which exhibit beta-lactamase inhibiting activity, use of such compounds in combination with beta-lactam antibiotics for inhibiting beta-lactamases, pharmaceutical compositions and processes for preparing such compounds.
    Type: Grant
    Filed: January 26, 2001
    Date of Patent: December 3, 2002
    Assignee: American Cyanamid Company
    Inventors: Vincent P. Sandanayaka, Amarnauth S. Prashad
  • Patent number: 6472383
    Abstract: A pharmaceutical formulation comprises, in combination with a penem of formula (I): in which: R1 is hydrogen or an organic substituent group; R2 is a fused bicyclic heterocyclic ring system of general formula:  wherein R4 and R5 are independently hydrogen or one or more substituents replacing hydrogen atoms in the ring system shown; m is 2 or 3; p is zero, 1 or 2; and R3 is hydrogen, a salt-forming cation or an ester-forming group; and the symbol ═/═ indicates that the double bond may be in either the E or Z configuration; and a pharmaceutically acceptable carrier; a &bgr;-lactam antibiotic selected from the group consisting of ceftazidime, cefotaxime, amoxycillin, and piperacillin, and pharmaceutically acceptable derivatives thereof.
    Type: Grant
    Filed: September 14, 2000
    Date of Patent: October 29, 2002
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Kenneth Coleman, Jane Elizabeth Neale
  • Patent number: 6426342
    Abstract: Novel neuroprotectant methods are described. &bgr;-Lactamase inhibitors are used to prevent or reduce loss of neuronal cells and neuronal cell function in patients afflicted with or susceptible to disease states or conditions known to result in or cause neuronal tissue insult.
    Type: Grant
    Filed: February 13, 2001
    Date of Patent: July 30, 2002
    Assignee: Revaax Pharmaceuticals, LLC
    Inventor: Gary A. Koppel
  • Patent number: 6180621
    Abstract: 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: Grant
    Filed: November 6, 1998
    Date of Patent: January 30, 2001
    Assignee: Sankyo Company, Limited
    Inventors: Isao Kawamoto, Satoshi Ohya, Yukio Utsui
  • Patent number: 5945413
    Abstract: This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.
    Type: Grant
    Filed: September 30, 1996
    Date of Patent: August 31, 1999
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Roger Dennis Tung, Francesco Gerald Salituro, David D. Deininger, Govinda Rao Bhisetti, Christopher Todd Baker, Andrew Spaltenstein
  • Patent number: 5939066
    Abstract: A pharmaceutical formulation comprises, in combination with a penem of formula (I): ##STR1## in which: R.sup.1 is hydrogen or an organic substituent group;R.sup.2 is a fused bicyclic heterocyclic ring system of general formula: ##STR2## wherein R.sup.4 and R.sup.5 are independently hydrogen or one or more substituents replacing hydrogen atoms in the ring system shown; m is 2 or 3; p is zero, 1 or 2; and R.sup.3 is hydrogen, a salt-forming cation or an ester-forming group; and the symbol =/= indicates that the double bond may be in either the E or Z configuration; and a pharmaceutically acceptable carrier; a .beta.-lactam antibiotic selected from the group consisting of ceftazidime, cefotaxime, amoxycillin, and piperacillin, and pharmaceutically acceptable derivatives thereof.
    Type: Grant
    Filed: January 26, 1998
    Date of Patent: August 17, 1999
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Kenneth Coleman, Jane Elizabeth Neale
  • Patent number: 5911985
    Abstract: A pharmaceutical formulation comprises, in combination with a penem of formula (I), in which: R.sup.1 is hydrogen or an organic substituent group; R.sup.2 is a fused bicyclic heterocyclic ring system of general formula (a), wherein R.sup.4 and R.sup.5 are independently hydrogen or one or more substituents replacing hydrogen atoms in the ring system shown; m is 2 or 3; p is zero, 1 or 2; and R.sup.3 is hydrogen, a salt-forming cation or an ester-forming group; and the symbol .dbd./.dbd. indicates that the double bond may be in either the E or Z configuration; and a pharmaceutically acceptable carrier, a .beta.-lactam antibiotic selected from the group consisting of ceftazidime, cefotaxime, amoxycillin, and piperacillin, and pharmaceutically acceptable derivatives thereof.
    Type: Grant
    Filed: March 14, 1997
    Date of Patent: June 15, 1999
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Kenneth Coleman, Jane Elizabeth Neale
  • Patent number: 5883252
    Abstract: This invention relates to a novel class of compounds that are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting aspartyl protease activity and methods for treating viral infections using the compounds and compositions of this invention.
    Type: Grant
    Filed: January 26, 1996
    Date of Patent: March 16, 1999
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Roger Dennis Tung, Francesco Gerald Salituro, David D. Deininger, Govinda Rao Bhisetti, Christopher Todd Baker
  • Patent number: 5776455
    Abstract: A pharmaceutical formulation comprises, in combination with a penem of formula (I): ##STR1## in which: R.sup.1 is hydrogen or an organic substituent group;R.sup.2 is a fused bicyclic heterocyclic ring system of general formula: ##STR2## wherein R.sup.4 and R.sup.5 are independently hydrogen or one or more substituents replacing hydrogen atoms in the ring system shown; m is 2 or 3; p is zero, 1 or 2; and R.sup.3 is hydrogen, a salt-forming cation or an ester-forming group; and the symbol .dbd./.dbd. indicates that the double bond may be in either the E or Z configuration; and a pharmaceutically acceptable carrier; a .beta.-lactam antibiotic selected from the group consisting of ceftazidime, cefotaxime, amoxycillin, and piperacillin, and pharmaceutically acceptable derivatives thereof.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: July 7, 1998
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Kenneth Coleman, Jane Elizabeth Neale
  • Patent number: 5637580
    Abstract: Compounds of structure: ##STR1## as well as their pharmaceutically-acceptable salts and biohydrolyzables esters, and hydrates thereof, are effective antiinfective agents, useful in treating and preventing infection.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: June 10, 1997
    Assignee: The Procter & Gamble Company
    Inventors: Ronald E. White, Thomas P. Demuth, Jr.
  • Patent number: 5384346
    Abstract: 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: Grant
    Filed: May 6, 1993
    Date of Patent: January 24, 1995
    Assignee: Hoechst AG
    Inventors: Matthas Gutweiler, Ulrich Hutten, Gerhard Pfahler, Hermann Schindler
  • Patent number: 5124441
    Abstract: Therapeutically active organic compound exhibiting at least one group comprising a structure --S'--S"--R, wherein the group --S"--R is defined by R being an organic group comprised in a physiologically acceptable compound H--S"--R obtainable by the splitting of the disulfide bridge --S'--S"-- in said structure, in which compound H--S"--R the sulfur atom S" is bound to a carbon atom in a heterocyclic aromatic ring in R having a configuration being such that the compound H--S"--R, while maintaining physiological acceptability, is stabilized, by tautomerism or resonance involving the sulfur atom S" bound to R, so as to be mainly excluded from reaction involving thiol disulfide exchange; S' being bound to an aliphatic carbon atom; and said compound, in addition to the group or groups comprising the structure --S'--S"--R, consisting of a residue of a therapeutically active organic base compound of non-polypeptide structure bound to S'.
    Type: Grant
    Filed: April 29, 1985
    Date of Patent: June 23, 1992
    Assignee: Pharmacia Aktiebolag
    Inventors: Jan P. E. Carlsson, Rolf E. A. V. Axen
  • Patent number: 5008257
    Abstract: The subject compounds, which are adapted for the site-specific/sustained delivery of centrally acting drug species to the brain, are:(a) compounds of the formula[D-DHC] (I)wherein [D] is a centrally acting drug species, and [DHC] is the reduced, biooxidizable, blood-brain barrier penetrating lipoidal form of a dihydropyridine.revreaction.pyridinium salt redox carrier, with the proviso that when [DHC] is ##STR1## wherein R is a lower alkyl or benzyl and [D] is a drug species containing a single NH.sub.2 or OH functional group, the single OH group when present being a primary or secondary OH group, said drug species being linked directly through said NH.sub.
    Type: Grant
    Filed: January 11, 1989
    Date of Patent: April 16, 1991
    Assignee: University of Florida
    Inventor: Nicholas S. Bodor
  • Patent number: 4923856
    Abstract: Compounds of the general formula (II): ##STR1## and pharmaceutically acceptable salts and in-vivo hydrolysable esters thereof, in whichR denotes a hydrogen atom or an in vivo hydrolysable acyl group;and the wavy line denotes either the E- or Z-isometric position,are novel compounds which exhibit .beta.-lactamase inhibitory action and have antibacterial properties.
    Type: Grant
    Filed: December 16, 1988
    Date of Patent: May 8, 1990
    Assignee: Beecham Group p.l.c.
    Inventors: Nigel J. P. Broom, Gerald Brooks, Steven Coulton
  • Patent number: 4876251
    Abstract: The compounds, having a 4,10-dioxo-3-oxa-7-thia-1-azatricyclo[6,2,0,0.sup.2,6 ]decane-2-carboxylic acid skeleton as the base structure, their esters and their salts, are useful antibacterial agents.
    Type: Grant
    Filed: June 9, 1987
    Date of Patent: October 24, 1989
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Akira Morimoto, Nobuo Choh, Noriyoshi Noguchi
  • Patent number: 4826833
    Abstract: Beta-lactamase inhibiting compounds of the formula ##STR1## or a pharmaceutically acceptable acid addition or carboxylate salt thereof; where n is zero, 1 or 2; X.sub.3 is H or Br, R.sup.1 is H, the residue of certain carboxy-protecting groups or the residue of an ester group readily hydrolyzable in vivo; one of R.sup.12 and R.sup.13 is H and the other is vinyl, certain aryl, alkylthio, alkylsulfonyl or certain heterocyclyl, aminomethyl, thiocarboxamido or amidino groups; one or R.sup.2 and R.sup.3 is H and the other is as disclosed for the other of R.sup.12 and R.sup.13, or is Cl or CH.sub.2 OH, and R.sup.18 is H or certain acyl groups; intermediates useful in their production, methods for their preparation and use, and pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 30, 1986
    Date of Patent: May 2, 1989
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng L. Chen
  • Patent number: 4782050
    Abstract: Antibacterial penicillins of the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.1 is a heterocyclic group and R is hydrogen, the residue of certian carboxy protecting groups or the residue of an ester group readily hydrolyzable in vivo having activity against resistant organisms.
    Type: Grant
    Filed: December 4, 1987
    Date of Patent: November 1, 1988
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng L. Chen
  • Patent number: 4731360
    Abstract: Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs.
    Type: Grant
    Filed: August 16, 1985
    Date of Patent: March 15, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, A. J. Repta, Joseph A. Fix
  • Patent number: 4729989
    Abstract: Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs.
    Type: Grant
    Filed: June 28, 1985
    Date of Patent: March 8, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, Joseph A. Fix
  • Patent number: 4692441
    Abstract: Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.
    Type: Grant
    Filed: August 16, 1985
    Date of Patent: September 8, 1987
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, A. J. Repta, Joseph A. Fix
  • Patent number: 4631150
    Abstract: A process for preparing 2-methyl substituted penems useful as antibiotics agent and/or as intermediates thereof, by reacting an appropriate 1-imido-3,4-disubstituted azetidinone derivative with a trivalent organophosphorus compound in an inert solvent at a temperature of from 110.degree. to 150.degree. C. for a period of from 2 hours to a few days.
    Type: Grant
    Filed: August 6, 1984
    Date of Patent: December 23, 1986
    Assignee: Farmitalia Carlo Erba S.p.A.
    Inventors: Carlo Battistini, Maurizio Foglio, Giovanni Franceschi, Cosimo Scarafile
  • Patent number: 4614737
    Abstract: Certain 2-dioxacycloalkylthio-2-penem-3-carboxylic acid compounds are useful as antibacterials for treating mammals and have the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R is ##STR2## A is carbonyl, methylene or thiocarbonyl; B is alkylene having 2-5 carbon atoms;alk is alkylene having 1-6 carbon atoms;R.sub.1 is hydrogen or a group which results in an ester which is hydrolyzable in vivo; andn is zero or one.
    Type: Grant
    Filed: September 13, 1984
    Date of Patent: September 30, 1986
    Assignee: Pfizer Inc.
    Inventor: Ernest S. Hamanaka
  • Patent number: 4582829
    Abstract: 6-(2-Amino-2-[4-acyloxyphenyl]acetamido)penicillanoyloxymethyl esters of penicillanic acid 1,1-dioxide are useful as antibacterial agents. Derivatives of the aforesaid antibacterial agents which have an amino protecting group on the amino function in the 2-amino-2-(4-acyloxyphenyl)acetamido side chain are useful intermediates to the antibacterial agents themselves.
    Type: Grant
    Filed: May 15, 1985
    Date of Patent: April 15, 1986
    Assignee: Pfizer Inc.
    Inventor: Michael S. Kellogg
  • Patent number: 4540687
    Abstract: 6-(2-Amino-2-[4-acyloxyphenyl]acetamido)penicillanoyloxymethyl esters of penicillanic acid 1,1-dioxide are useful as antibacterial agents. Derivatives of the aforesaid antibacterial agents which have an amino protecting group on the amino function in the 2-amino-2-(4-acyloxyphenyl)acetamido side chain are useful intermediates to the antibacterial agents themselves.
    Type: Grant
    Filed: August 12, 1982
    Date of Patent: September 10, 1985
    Assignee: Pfizer Inc.
    Inventor: Michael S. Kellogg
  • Patent number: 4537886
    Abstract: 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: Grant
    Filed: March 29, 1983
    Date of Patent: August 27, 1985
    Assignee: Beecham Group p.l.c.
    Inventors: Andrew W. Taylor, Richard T. Cook
  • Patent number: 4524073
    Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof: ##STR1## wherein R represents an alkyl or aralkyl group, substituted on an alkyl carbon atom other than that adjacent to --NH-- group, with one or more functional groups selected from halogen, non-aromatic heterocyclyl linked through carbon, aromatic heterocyclyl, nitro, oxo, --OR.sup.1, SR.sup.1 --P(O)R.sup.2 R.sup.3, --NR.sup.4 R.sup.5, .dbd.NR.sup.6, or a sulphur linked organic radical, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are various organic radicals.Processes for the preparation of these compounds and pharmaceutical compositions containing them are also disclosed.
    Type: Grant
    Filed: July 20, 1983
    Date of Patent: June 18, 1985
    Assignee: Beecham Group p.1.c.
    Inventors: Irene Stirling, Gordon Bruton, Stephen H. Calvert, Brian P. Clarke
  • Patent number: 4505915
    Abstract: 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: Grant
    Filed: March 16, 1981
    Date of Patent: March 19, 1985
    Assignee: Merck & Co., Inc.
    Inventor: John Hannah