Spiro Or Additional Polycyclo Ring System Patents (Class 514/193)
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Patent number: 11700501Abstract: Systems and methods for adjusting bass levels of a multi-channel audio signal include, among other features, (i) receiving the multi-channel signal via a playback device; (ii) separating, from the multi-channel signal, low-frequency signals comprising frequencies less than a threshold frequency; (iii) determining electrical energies of the low-frequency signals; (iv) determining a first energy by summing the electrical energies of the low-frequency signals; (v) consolidating the low-frequency signals into a consolidated low-frequency signal; (vi) determining a second energy by determining an electrical energy of the consolidated low-frequency signal; (vii) generating a gain-adjusted low-frequency signal by adjusting a gain of the consolidated low-frequency signal based on both (a) the first energy and (b) the second energy; (viii) generating a gain-adjusted multi-channel signal by mixing the gain-adjusted low-frequency signal back into the multi-channel signal; and (ix) using the gain-adjusted multi-channel sType: GrantFiled: December 28, 2020Date of Patent: July 11, 2023Assignee: Sonos, Inc.Inventors: Hilmar Lehnert, Aurelio Ramos, Bob Dizon
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Patent number: 11440880Abstract: 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: GrantFiled: October 29, 2020Date of Patent: September 13, 2022Assignees: The USA, as represented by the Secretary, Department of Health and Human Services, University Court of the University of AberdeenInventors: Nigel H. Greig, Weiming Luo, David Tweedie, Neil Vargesson, Shaunna Beedie, William Douglas Figg
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Patent number: 11230545Abstract: Provided is a compound that can have an effect of inhibiting MALT1 and is expected as useful as a prophylactic or therapeutic drug for cancer, etc. A compound represented by formula (I) [wherein each symbol is as defined in the description], a salt thereof, or a cocrystal, a hydrate or a solvate of the same.Type: GrantFiled: July 2, 2021Date of Patent: January 25, 2022Assignee: Takeda Pharmaceutical Company LimitedInventors: Takaharu Hirayama, Yoshiteru Ito, Hiroshi Banno, Hidekazu Tokuhara, Toshio Tanaka, Yasuyoshi Arikawa, Noriyuki Nii, Youichi Kawakita, Shinichi Imamura
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Patent number: 11186556Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to salts of (Z)-5-((Z)-3-chloro-4-((R)-2,3-dihydroxypropoxy)benzylidene)-2-(propylimino)-3-(o-tolyl)thiazolidin-4-one.Type: GrantFiled: October 15, 2019Date of Patent: November 30, 2021Assignee: Celgene CorporationInventors: Lianfeng Huang, Daozhong Zou
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Patent number: 10889577Abstract: 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: GrantFiled: July 6, 2017Date of Patent: January 12, 2021Assignee: Cyclerion Therapeutics, Inc.Inventors: Vasu Sethuraman, Ahmad Hashash, Song Xue, Robert C. Livingston, Kwame Wiredu Nti-Addae
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Patent number: 10836721Abstract: 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: GrantFiled: June 24, 2020Date of Patent: November 17, 2020Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, University Court of the University of AberdeenInventors: Nigel H. Greig, Weiming Luo, David Tweedie, Neil Vargesson, Shaunna Beedie, William Douglas Figg
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Patent number: 10730835Abstract: 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: GrantFiled: September 29, 2016Date of Patent: August 4, 2020Assignees: The United States of America, as represented by the Secretary, Health and Human Services, University Court of the University of AberdeenInventors: Nigel H. Greig, Weiming Luo, David Tweedie, Neil Vargesson, Shaunna Beedie, William Douglas Figg
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Patent number: 10376585Abstract: This invention relates to a composition, including penethamate (PNT) or a pharmaceutical equivalent thereof; and at least one oily vehicle.Type: GrantFiled: July 16, 2013Date of Patent: August 13, 2019Assignee: BAYER NEW ZEALAND LTDInventors: Fadil Al Alawi, Olaf Bork, Rohit Jain, Karthigeyan Nanjan, Ian George Tucker
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Patent number: 10144708Abstract: 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: GrantFiled: March 30, 2017Date of Patent: December 4, 2018Assignee: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Hiroshi Miyazaki, Takao Komasaka, Joji Tsurumoto, Takeshi Uemura, Yuuji Morita
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Patent number: 9518004Abstract: 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: GrantFiled: December 2, 2013Date of Patent: December 13, 2016Assignee: KANEKA CORPORATIONInventors: Teruyoshi Koga, Yoshihisa Okamoto, Takao Yamaguchi
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Publication number: 20140271921Abstract: 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: ApplicationFiled: May 28, 2014Publication date: September 18, 2014Applicant: SLA PHARMA AGInventor: DAVID NIGEL ARMSTRONG
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Patent number: 8324175Abstract: 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: GrantFiled: August 3, 2010Date of Patent: December 4, 2012Inventor: Young Hee Ko
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Publication number: 20120065182Abstract: 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: ApplicationFiled: November 18, 2011Publication date: March 15, 2012Applicant: Taro Pharmaceuticals North America, Inc.Inventors: Shen GAO, Daniel A. Moros, Satish Asotra
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Publication number: 20110288063Abstract: 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: ApplicationFiled: May 19, 2011Publication date: November 24, 2011Applicant: 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
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Publication number: 20110182869Abstract: 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: ApplicationFiled: July 14, 2009Publication date: July 28, 2011Inventors: Jan Knol, Kaouther Ben Amor, Richèle Deodata Wind
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Publication number: 20100227843Abstract: ?-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: ApplicationFiled: May 21, 2010Publication date: September 9, 2010Applicant: ZHEJIANG YONGNING PHARMACEUTICAL FACTORYInventors: Fengqi YE, Shanzong FANG, Xiuwel LU
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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: 20100040548Abstract: 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: ApplicationFiled: June 10, 2009Publication date: February 18, 2010Inventor: Chongxi Yu
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Patent number: 7241756Abstract: 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: GrantFiled: June 1, 2006Date of Patent: July 10, 2007Assignee: SmithKline Beecham CorporationInventors: Jonathan Robert Sanders Arch, James Martin Lenhard
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Patent number: 7112582Abstract: 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: GrantFiled: May 1, 2003Date of Patent: September 26, 2006Assignee: WyethInventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Itsuki Yamamura, Tsuyoshi Takasaki, Atul Agarwal, Osvaldo dos Santos, Fuk-Wah Sum, Yang-I Lin
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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: 7078397Abstract: 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: GrantFiled: June 19, 2001Date of Patent: July 18, 2006Assignee: SmithKline Beecham CorporationInventors: Jonathan Robert Sanders Arch, James Martin Lenhard
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Patent number: 7018997Abstract: 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: GrantFiled: May 1, 2003Date of Patent: March 28, 2006Assignee: WyethInventors: Aranapakam Mudumbai Venkatesan, Tarek Suhayl Mansour, Takao Abe, Ado Mihira, Atul Agarwal, Hideki Ushirogochi, Yansong Gu, Satoshi Tamai, Fuk-Wah Sum
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Publication number: 20030124141Abstract: 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: ApplicationFiled: November 16, 2001Publication date: July 3, 2003Inventors: Rainer Haas, Harold Kleanthous, Jean-Francois Tomb, Charles Miller, Amal Al-Garawi, Stefan Odenbreit, Thomas Meyer
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Publication number: 20030124597Abstract: 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: ApplicationFiled: November 6, 2002Publication date: July 3, 2003Inventor: Ambrose Cheung
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Publication number: 20030100002Abstract: 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: ApplicationFiled: November 6, 2002Publication date: May 29, 2003Inventor: Ambrose Cheung
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Patent number: 6489316Abstract: 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: GrantFiled: January 26, 2001Date of Patent: December 3, 2002Assignee: American Cyanamid CompanyInventors: Vincent P. Sandanayaka, Amarnauth S. Prashad
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Patent number: 6472383Abstract: 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: GrantFiled: September 14, 2000Date of Patent: October 29, 2002Assignee: SmithKline Beecham p.l.c.Inventors: Kenneth Coleman, Jane Elizabeth Neale
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Patent number: 6426342Abstract: 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: GrantFiled: February 13, 2001Date of Patent: July 30, 2002Assignee: Revaax Pharmaceuticals, LLCInventor: Gary A. Koppel
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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: 5945413Abstract: 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: GrantFiled: September 30, 1996Date of Patent: August 31, 1999Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roger Dennis Tung, Francesco Gerald Salituro, David D. Deininger, Govinda Rao Bhisetti, Christopher Todd Baker, Andrew Spaltenstein
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Patent number: 5939066Abstract: 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: GrantFiled: January 26, 1998Date of Patent: August 17, 1999Assignee: SmithKline Beecham p.l.c.Inventors: Kenneth Coleman, Jane Elizabeth Neale
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Patent number: 5911985Abstract: 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: GrantFiled: March 14, 1997Date of Patent: June 15, 1999Assignee: SmithKline Beecham p.l.c.Inventors: Kenneth Coleman, Jane Elizabeth Neale
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Patent number: 5883252Abstract: 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: GrantFiled: January 26, 1996Date of Patent: March 16, 1999Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roger Dennis Tung, Francesco Gerald Salituro, David D. Deininger, Govinda Rao Bhisetti, Christopher Todd Baker
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Patent number: 5776455Abstract: 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: GrantFiled: June 1, 1995Date of Patent: July 7, 1998Assignee: SmithKline Beecham p.l.c.Inventors: Kenneth Coleman, Jane Elizabeth Neale
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Patent number: 5637580Abstract: 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: GrantFiled: June 7, 1995Date of Patent: June 10, 1997Assignee: The Procter & Gamble CompanyInventors: Ronald E. White, Thomas P. Demuth, Jr.
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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: 5124441Abstract: 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: GrantFiled: April 29, 1985Date of Patent: June 23, 1992Assignee: Pharmacia AktiebolagInventors: Jan P. E. Carlsson, Rolf E. A. V. Axen
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Patent number: 5008257Abstract: 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: GrantFiled: January 11, 1989Date of Patent: April 16, 1991Assignee: University of FloridaInventor: Nicholas S. Bodor
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Patent number: 4923856Abstract: 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: GrantFiled: December 16, 1988Date of Patent: May 8, 1990Assignee: Beecham Group p.l.c.Inventors: Nigel J. P. Broom, Gerald Brooks, Steven Coulton
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Patent number: 4876251Abstract: 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: GrantFiled: June 9, 1987Date of Patent: October 24, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Akira Morimoto, Nobuo Choh, Noriyoshi Noguchi
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Patent number: 4826833Abstract: 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: GrantFiled: July 30, 1986Date of Patent: May 2, 1989Assignee: Pfizer Inc.Inventor: Yuhpyng L. Chen
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Patent number: 4782050Abstract: 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: GrantFiled: December 4, 1987Date of Patent: November 1, 1988Assignee: Pfizer Inc.Inventor: Yuhpyng L. Chen
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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: 4631150Abstract: 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: GrantFiled: August 6, 1984Date of Patent: December 23, 1986Assignee: Farmitalia Carlo Erba S.p.A.Inventors: Carlo Battistini, Maurizio Foglio, Giovanni Franceschi, Cosimo Scarafile
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Patent number: 4614737Abstract: 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: GrantFiled: September 13, 1984Date of Patent: September 30, 1986Assignee: Pfizer Inc.Inventor: Ernest S. Hamanaka
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Patent number: 4582829Abstract: 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: GrantFiled: May 15, 1985Date of Patent: April 15, 1986Assignee: Pfizer Inc.Inventor: Michael S. Kellogg
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Patent number: 4540687Abstract: 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: GrantFiled: August 12, 1982Date of Patent: September 10, 1985Assignee: Pfizer Inc.Inventor: Michael S. Kellogg