Additional Hetero Ring Containing Patents (Class 549/337)
  • Patent number: 9080007
    Abstract: Carboxylic acid salts of tertiary amines for use as an accelerator for an anhydride based epoxy curing agents are disclosed. The disclosed carboxylic acid salts of certain tertiary amines are latent anhydride accelerators and enable epoxy resin curing when heated to an elevated temperature (e.g., an onset temperature of greater than about 50° C.).
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: July 14, 2015
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Gauri Sankar Lal, Gamini Ananda Vedage, Stephen Michael Boyce, Pritesh G. Patel, Dilipkumar Nandlal Shah, Atteye Houssein Abdourazak
  • Patent number: 8975422
    Abstract: Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided.
    Type: Grant
    Filed: April 10, 2014
    Date of Patent: March 10, 2015
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Francis G. Fang, Bryan M. Lewis, Matthew Schnaderbeck
  • Publication number: 20140221635
    Abstract: Intermediates and methods of their use in the synthesis of anslogs of halichondrin B are provided.
    Type: Application
    Filed: April 10, 2014
    Publication date: August 7, 2014
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Francis G. FANG, Bryan M. LEWIS, Matthew SCHNADERBECK
  • Publication number: 20120029213
    Abstract: Intermediates and methods of their use in the synthesis of analogs of halichondrin B are provided.
    Type: Application
    Filed: June 29, 2011
    Publication date: February 2, 2012
    Applicant: Eisai R&D Management Co., Ltd.
    Inventors: Brian Austad, Farid Benayoud, Trevor Calkins, Silvio Campagna, Charles E. Chase, William Christ, Francis G. Fang, Yongbo Hu, Bryan M. Lewis, Marc Pesant, Matthew Schnaderbeck, Gordon Wilkie, Xiaojie Zhu
  • Patent number: 8067620
    Abstract: A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the invention unexpectedly provide a single-dose cure for malaria, as well as prophylactic activity against the same. The compounds are also active against schistosomiasis and cancer.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: November 29, 2011
    Assignee: Medicines for Malaria Venture MMV
    Inventors: Jonathan L. Vennerstrom, Yuxiang Dong, Susan A. Charman, Sergio Wittlin, Jacques Chollet, Darren J. Creek, Xiaofang Wang, Kamaraj Spiraghavan, Lin Zhou, Hugues Matile, William N. Charman
  • Patent number: 7385067
    Abstract: The invention relates to a process for the preparation of compounds containing at least one —CF2—O— bridge in the molecule, in which a) an acid is added onto at least one ketene dithioketal, b) the resultant bis(alkylthio)carbenium salt is reacted with at least one compound having at least one hydroxyl group in the presence of a base, c) and subsequently, preferably in situ, the resultant dithioorthoester is subjected to oxidative fluorodesulfurisation using a fluorinating agent and an oxidant to give the compound containing at least one —CF2—O— bridge in the molecule.
    Type: Grant
    Filed: June 2, 2006
    Date of Patent: June 10, 2008
    Assignee: Merck Patent GmbH
    Inventors: Peer Kirsch, Andreas Taugerbeck, Alexander Hahn
  • Patent number: 7157589
    Abstract: The present invention is directed to a one-step process for the preparation of fructopyranose sulfamate derivatives of the general formula (I) wherein X, R1, R3, R4, R5 and R6 are as described in the specification.
    Type: Grant
    Filed: March 1, 2004
    Date of Patent: January 2, 2007
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Joachim Ernst Berkner, Scott Duncan, John Mills
  • Patent number: 6962938
    Abstract: The present application describes novel spiro-cyclic ?-amino acid derivatives of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring B is a 3-13 membered carbocycle or heterocycle, ring C forms a 3-11 membered spiro-carbocycle or spiro-heterocycleon ring B, and the other variables are defined in the present specification, which are useful as as matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), and/or aggrecanase inhibitors.
    Type: Grant
    Filed: December 18, 2003
    Date of Patent: November 8, 2005
    Assignee: Bristol-Myers Squibb Pharma Company
    Inventors: Gregory R. Ott, Xiao Tao Chen, Jingwu Duan, Matthew E. Voss
  • Patent number: 6756497
    Abstract: Benzoic acid derivatives useful as intermediates for the preparation of drugs and agricultural chemicals, particularly compounds having herbicidal activity; and easy and economical processes for the preparation of the same. The processes are specifically those represented by reaction formula for the preparation of compounds represented by general formulae (1) and (6).
    Type: Grant
    Filed: January 12, 2001
    Date of Patent: June 29, 2004
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Yuuki Nakagawa, Masao Yamaguchi, Hiroyuki Adachi, Hiroyuki Yamanaka, Tomio Yagihara, Masami Hatano
  • Patent number: 6673937
    Abstract: Oxidative cyclization of bis-naphthyl ethers allows concise total syntheses of palmarumycin CP1 and deoxypreussomerin A in 8-9 steps and 15-35% overall yield from 5-hydroxy-8-methoxy-1-tetralone. A small library of palmarumycin analogs was created. Biological evaluation of these naphthoquinone spiroketals against MCF-7 and MDA-MB-231 human breast cancer cells revealed several low-micromolar growth inhibitors. A number of the analogs inhibit the thioredoxin—thioredoxin reductase system.
    Type: Grant
    Filed: July 19, 2001
    Date of Patent: January 6, 2004
    Assignee: The University of Pittsburgh
    Inventors: John S. Lazo, Peter Wipf, Billy W. Day
  • Patent number: 6315928
    Abstract: The present invention relates to specific photochromic 3H-naphtho[2,1-b]pyran derivatives and to their use in plastics of all types, especially for ophthalmic purposes. In particular, the present invention relates to spiro compounds derived from naphthopyrans and having a fluorene structure, referred to as spirofluorenopyrans, in which an annelated ring system is joined by a spiro bond to the central carbon atom of the fluorene structure.
    Type: Grant
    Filed: March 2, 2001
    Date of Patent: November 13, 2001
    Assignee: Optische Werke G. Rodenstock
    Inventors: Claudia Mann, Manfred Melzig, Udo Weigand
  • Patent number: 6149841
    Abstract: Described are novel photochromic benzopyrano-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted benzopyran group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds.
    Type: Grant
    Filed: December 17, 1999
    Date of Patent: November 21, 2000
    Assignee: PPG Industries Ohio, Inc.
    Inventor: Anil Kumar
  • Patent number: 6022495
    Abstract: Described are novel photochromic benzopyrano-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted benzopyran group fused to one side of the naphtho portion of the naphthopyran and having certain substituents at the position ortho to the oxygen atom of the naphthopyran ring. These compounds may be represented by the following graphic formulae: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, nenzopyrans, and spiro(indoline)type compounds.
    Type: Grant
    Filed: July 10, 1998
    Date of Patent: February 8, 2000
    Assignee: Transitions Optical, Inc.
    Inventor: Anil Kumar
  • Patent number: 5786496
    Abstract: The present invention provides a new tetradentate bis-amido bis-alkoxo, 1,2-(bis-2,20diphenyl-2-hydroxyethanamido)benzene (H.sub.4 PHAB) and various derivatives thereof. This ligand is able to stabilize high valen metal oxo complexes by providing strong sigma donor ligands and through the use of steric bulk to prevent decomposition via formation of the .mu.-oxo dimers. Disclosed are novel metal oxo structural chemistry and oxidation reactions carried out with the novel metal oxo complexes.
    Type: Grant
    Filed: November 15, 1996
    Date of Patent: July 28, 1998
    Assignee: Northwestern University
    Inventors: Thomas V. O'Halloran, Frederick M. MacDonnell, Nathanael L. P. Fackler
  • Patent number: 5703249
    Abstract: The present invention relates to novel bicycloaliphatic 2-methylene-1,3-dioxepanes, which are suitable as starting materials for the preparation of polymers and copolymers, preferably of composite and dental materials. The 2-methylene-1,3-dioxepanes according to the invention, which can undergo radical polymerisation with ring opening with only very little volume shrinkage, can be prepared in a simple manner, are easy to purify and to modify chemically, and are characterised by lack of odour and advantageous physical properties.
    Type: Grant
    Filed: October 25, 1995
    Date of Patent: December 30, 1997
    Assignee: Ivoclar AG
    Inventors: Volker Rheinberger, Norbert Moszner, Ulrich Salz, Thomas Voelkel
  • Patent number: 5663393
    Abstract: Chiral catalysts for enantioselectively epoxidizing a prochiral olefin and for enantioselectively oxidizing a prochiral sulfide are disclosed, together with methods of using such catalysts. In accordance with one aspect of the invention, the catalyst is a salen derivative which has the following general structure: ##STR1## In accordance with another aspect of the present invention is a method of, producing an epoxychroman using a chiral catalyst. In accordance with this method, a chromene derivative, an oxygen atom source, and a chiral catalyst are reacted under such conditions and for such time as is needed to epoxidize said chromene derivative. In accordance with yet another aspect of this invention is a method of enantioselectively epoxidizing a cis-cinnamate derivative to make taxol or an analog thereof. In accordance with another aspect a method of disproportionation of hydrogen peroxide using the catalysts of the present invention is disclosed.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: September 2, 1997
    Assignee: Research Corporation Technologies, Inc.
    Inventors: Eric N. Jacobsen, Wei Zhang, Li Deng
  • Patent number: 5645767
    Abstract: Described are novel photochromic indeno-fused naphthopyran compounds, examples of which are naphthopyran compounds having a substituted or unsubstituted indeno group, the 2,1 positions of which are fused to the f side of the naphtho portion of the naphthopyran, and certain substituents at the 3-position of the pyran ring. Certain substituents may also be present at the number 5, 6, 7, 8, 9, 10, 11, 12, or 13 carbon atoms of the compounds. These compounds may be represented by the following graphic formula: ##STR1## Also described are polymeric organic host materials that contain or that are coated with such compounds. Optically clear articles such as ophthalmic lenses or other plastic transparencies that incorporate the novel naphthopyran compounds or combinations thereof with complementary photochromic compounds, e.g., certain other naphthopyrans, benzopyrans, and spiro(indoline)type compounds, are also described.
    Type: Grant
    Filed: October 13, 1995
    Date of Patent: July 8, 1997
    Assignee: Transitions Optical, Inc.
    Inventor: Barry Van Gemert
  • Patent number: 5463087
    Abstract: A process for the preparation of a compound. That compound is converted to a novel compound of the formula ##STR1## in which R.sup.1, R.sup.2 and R.sup.5 each independently is alkyl of 3 to 14 carbon atoms, which is used to make novel anti-inflammatories.
    Type: Grant
    Filed: January 13, 1995
    Date of Patent: October 31, 1995
    Assignee: Bayer Pharma
    Inventors: Erwin Bischoff, Zhan Gao, Stefan Wohlfeil, Gabriele Hecker, Jeannine Cleophax, Didier Dubreuil, Stephane Gero, Alice Olesker, Catherine Verre-Sebrie, Mauro Vieira de Almeida, Georges Vass
  • Patent number: 5387700
    Abstract: A process for producing chlorosulfate and sulfamate esters of 2,3:4,5-bis-O-(1-methylethylidene)-.beta.-D-fructopyranose and (1-methylcyclohexyl)methanol is disclosed. The process involves a two step procedure involving in the first step reacting of an alcohol with sulfuryl chloride in the presence of a tertiary or heterocyclic amine base in a solvent selected from the group consisting of toluene, t-butyl methyl ether or tetrahydrofuran to produce a chlorosulfate intermediate, which is preferably stabilized by an aqueous wash and/or treatment with a base, and in the second step reacting of the resulting intermediate with an amine in a solvent selected from the group consisting of t-butyl methyl ether, tetrahydrofuran and lower alkanol.
    Type: Grant
    Filed: August 12, 1993
    Date of Patent: February 7, 1995
    Assignee: McNeilab, Inc.
    Inventors: Cynthia A. Maryanoff, Lorraine Scott, Kirk L. Sorgi
  • Patent number: 5354495
    Abstract: A physical property-improving reagent which comprises an alkenoylcarbamate compound of the formula: ##STR1## wherein R is a hydrogen atom or a lower alkyl group, X is an oxygen atom (--O--), a sulfur atom (--S--) or a substituted or unsubstituted imino group (--NR'--), R' being a hydrogen atom or a lower alkyl group, and Y is the residue of an active hydrogen atom-containing compound excluding --X--H therefrom dissolved in an organic solvent having a solubility parameter of not less than 8, which can impart excellent physical properties to a polymer produced with the same.
    Type: Grant
    Filed: March 1, 1990
    Date of Patent: October 11, 1994
    Assignee: Nippon Paint Co., Ltd.
    Inventors: Satoshi Urano, Ryuzo Mizuguchi, Noriyuki Tsuboniwa, Kei Aoki, Yuji Suzuki, Takeyasu Itoh
  • Patent number: 4965257
    Abstract: Bicyclo-[2,2,1]-heptanes, bicyclo-[2,2,2]-octanes and bicyclo-[2,2,3]-nonanes, having 2 or 3 ring hetero atoms selected from O, S and N, substituted at the 1-position by a 4-alkynylphenyl group and at the 4-position and optionally at the 3 and/or 5-position are valuable pesticides, particularly insecticides and acaracides. The compounds may be prepared by reacting an alkyne with the corresponding 4-iodophenyl substituted compounds or by debromination of the corresponding 4-dibromomethylphenyl substituted compound.
    Type: Grant
    Filed: July 24, 1989
    Date of Patent: October 23, 1990
    Assignee: The Regents of the University of California
    Inventors: John E. Casida, Christopher J. Palmer, John P. Larkin, Ian H. Smith
  • Patent number: 4927963
    Abstract: A process for preparing compounds represented by the formula ##STR1## wherein: X is hydrogen or lower alkoxy;Y is hydrogen, exo-(lower alkyl) or endo-(lower alkyl);n is an integer from 2-4;R.sub.2 is hydrogen or methyl; andR.sub.3 is linear or branched alkyl, ##STR2## --(CH.sub.2).sub.m -phenyl or --CH.sub.2 O-phenyl; in which any phenyl may be optionally substituted with lower alkyl, lower alkoxy, trifluoromethyl, or halogen, anda is an integer of 0, 1 or 2;b is an integer of 3-7;m is an integer of 0, 1 or 2,as a mixture or separately in a sequence starting from an epoxide represented by the formula ##STR3## and processes for making the novel intermediates.
    Type: Grant
    Filed: April 28, 1989
    Date of Patent: May 22, 1990
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Keith A. M. Walker, Denis J. Kertesz
  • Patent number: 4925956
    Abstract: The invention relates to a process for manufacturing optically active carbacyclin intermediate products from racemic cis-bicyclo[3.3.0]octane-2-carboxylic acids. This process makes it possible in an advantageous way to produce important intermediates for the synthesis of stable and pharmacologically active carbacyclin derivatives.
    Type: Grant
    Filed: July 13, 1988
    Date of Patent: May 15, 1990
    Assignee: Schering Aktiengesellschaft
    Inventors: Werner Skuballa, Helmut Dahl
  • Patent number: 4841075
    Abstract: A method of preparing an acetal or ketal from a corresponding aldehyde or ketone is disclosed. A hydrous oxide of an element of Group IV of the Periodic Table is used as a catalyst, and the aldehyde or ketone is caused to react with an alcohol. The hydrous oxide can be obtained by partially dehydrating a hydroxide of the corresponding element. The method does not require an acid catalyst and is applicable to a carbonyl compound which is not stable in acids.
    Type: Grant
    Filed: December 7, 1987
    Date of Patent: June 20, 1989
    Assignee: Japan Tobacco, Inc.
    Inventors: Hajime Matsushita, Makoto Shibagaki, Kyoko Takahashi, Hideyuki Kuno
  • Patent number: 4792606
    Abstract: A process for the preparation of a dimeric aromatic acyl cyanide of the formula ##STR1## in which Ar is optionally substituted phenyl, naphthyl or hetaryl,comprising reaction an acyl halide of the formulaAr--CO--Halin whichHal is fluorine, chlorine or bromine, with an alkali metal cyanide in a two-phase system comprising water and a water-immiscible or only sparingly water-miscible aliphatic ketone, and in the presence of a phase-transfer catalyst. The products are known intermediates for pesticides.
    Type: Grant
    Filed: July 16, 1987
    Date of Patent: December 20, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Reinhard Lantzsch, Hermann-Dieter Krall
  • Patent number: 4599327
    Abstract: 2,6-di-O-methyl-beta-cyclodextrin complexes of compounds of the formula (1a) ##STR1## wherein R.sup.2' stands for C.sub.1 to C.sub.12 alkyl or a group of the formula ##STR2## in which R.sup.11 is C.sub.1 to C.sub.4 alkyl;R.sup.12 is hydrogen or C.sub.1 to C.sub.4 alkyl;n is 0 or 1;p is 1 to 4;r is 1 to 4; andR.sup.3' and R.sup.4' are each C.sub.1 to C.sub.4 alkyl, or pharmaceutically salts thereof are disclosed, having analgesic activity.
    Type: Grant
    Filed: December 2, 1983
    Date of Patent: July 8, 1986
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara RT
    Inventors: Mihaly Nogradi, Dezso Korbonits, Agnes Gottsegen, Sandor Antus, Zsuzsa Furst, Jozsef Knoll, Jozsef Szejtli, Agnes Stadler, Gabor Kovacs, Katalin Marmarosi
  • Patent number: 4582916
    Abstract: Sulfamates of the following formula (I): ##STR1## wherein X is O or CH.sub.2 and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as herein defined have been found to exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Further, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and intermediates form part of the present invention.
    Type: Grant
    Filed: February 11, 1985
    Date of Patent: April 15, 1986
    Assignee: McNeilab, Inc.
    Inventors: Bruce E. Maryanoff, Joseph F. Gardocki
  • Patent number: 4513006
    Abstract: Sulfamates of the following formula (I): ##STR1## wherein X is O or CH.sub.2 and R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as herein defined have been found to exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Further, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and intermediates form part of the present invention.
    Type: Grant
    Filed: September 26, 1983
    Date of Patent: April 23, 1985
    Assignee: McNeil Lab., Inc.
    Inventors: Bruce E. Maryanoff, Joseph F. Gardocki
  • Patent number: 4510159
    Abstract: Compound of the formula ##STR1## in which R and R' represent hydrogen or an optionally substituted hydrocarbon radical or acyl radical,R.sub.1 represents hydrogen or an optionally substituted hydrocarbon radical of aliphatic or aromatic character,R.sub.2 represents hydrogen or an optionally substituted hydrocarbon radical of higher aliphatic or aromatic character,it being possible forR.sub.1 and R.sub.2 together to represent also an optionally substituted alkylene radical or an optionally substituted biphenyl-2,2'-ylene radical,whereby however, when R, R.sub.1 and R.sub.2 are hydrogen, R' cannot be methyl and salts of such compounds that contain a salt-forming grouping, and pharmaceutical compositions containing these compounds.The pharmaceutical compositions containing these compounds are particularly valuable for treating liver and veneous diseases.
    Type: Grant
    Filed: May 31, 1983
    Date of Patent: April 9, 1985
    Assignee: Zyma SA
    Inventors: Alban I. Albert, Marc E. Ballenegger, Jan C. Overeem, Robert G. Tyson
  • Patent number: 4331602
    Abstract: Compounds having the formula ##STR1## wherein ##STR2## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.
    Type: Grant
    Filed: March 16, 1981
    Date of Patent: May 25, 1982
    Assignee: Pfizer Inc.
    Inventors: Michael R. Johnson, Lawrence S. Melvin, Jr.