Abstract: Disclosed are cis-2,6-disubstituted tetrahydropyran derivatives represented by Chemical Formula 1 and a preparation method thereof. The tetrahydropyran derivatives can be prepared by Prins-reacting tetrahydropyran derivatives with homopargylicalcohol derivatives in the presence of trimethylsilyltriflate. The tetrahydropyran derivatives with cis-substituents at both C2 and C6 positions of the tetrahydropyran ring are useful as intermediates for use in the synthesis and development of therapeutically effective, naturally occurring compounds. (wherein, R1, R2 and R3 are as defined in the specification.).
Type:
Grant
Filed:
October 1, 2008
Date of Patent:
February 14, 2012
Assignee:
Korea Institute of Science and Technology
Inventors:
Yong Seo Cho, You Seung Kim, Jae Kyun Lee, Hyunah Choo, Ae Nim Pae
Abstract: The present application relates to a novel AMPelopsin unsaturated sodium salt compound (AMP-Na), a method for preparing the same and the applications thereof. The physicochemical properties of AMP-Na according to the present application are significantly altered compared to those of AMPelopsin (AMP). AMP-Na shows significantly reduced toxicity than AMP as evidenced by the in vivo acute toxicity studies. As demonstrated by pharmacological evaluation, AMP-Na exhibits synergistic action when administered in combination with clinically used anti-cancer drugs, therefore reducing their dosages without compromising their therapeutic effects.
Abstract: The present invention relates to a process for preparation of a delta-9-tetrahydrocannabinol compound or derivative thereof involving treating a first intermediate compound with an organoaluminum-based Lewis acid catalyst, under conditions effective to produce the delta-9-tetrahydrocannabinol compound or derivative thereof. Another aspect of the present invention relates to a process for preparation of a cannabidiol or cannabidiolate compound involving reacting a first starting compound with a second starting compound in the presence of a metal triflate catalyst, under conditions effective to form the cannabidiol or cannabidiolate compound. The present invention also relates to a compound of the formula: where R8, R9, and R10 are the same or different and independently selected from the group consisting of H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or halo, with R1, R2, and R3 defined herein.
Type:
Grant
Filed:
May 16, 2011
Date of Patent:
January 31, 2012
Assignee:
Albany Molecular Research, Inc.
Inventors:
David C. Burdick, Steven J. Collier, Betina Biolatto, Harold Meckler
Abstract: The invention discloses novel processes for production, enrichment and/or isolation of alpha-tocotrienol from source material comprising at least one non-alpha-tocotrienol, such as natural extracts comprising mixed tocotrienols.
Type:
Grant
Filed:
October 27, 2009
Date of Patent:
January 31, 2012
Assignee:
Edison Pharmaceuticals, Inc.
Inventors:
Kieron E. Wesson, Andrew W. Hinman, Orion D. Jankowski
Abstract: This invention relates to a new method for the stereospecific thiocarboxylation and nitration of organic compounds for the preparation of compounds according to formula (I): comprising the following steps: (a) reacting a compound of formula (II): with a sulfonic derivative of formula (III) wherein the R is chosen from the groups C1-3-alkyl, C1-3-alkyl substituted with 1 to 3 halogen atoms, phenyl, C1-3-alkyl-phenyl and C1-3-alkyl-phenyl wherein the alkyl is substituted with 1 to 3 halogen atoms and G is a halogen atomo or a group —O—SO2—R wherein R is as hereinabove defined to yield a compound of formula (IV) (b) treating compound (IV) with a thiocarboxylic acid of formula (V) or a salt thereof: wherein Z is as defined above, to yield compound (VI) and (c) treating compound (VI) with tetrabutylammonium nitrate to yield a compound of formula (I).
Type:
Grant
Filed:
February 20, 2009
Date of Patent:
January 31, 2012
Assignee:
Lacer, S.A.
Inventors:
José Repollés Moliner, Francisco Pubill Coy, Lydia Cabeza Llorente, Joan Martínez Bonnin
Abstract: A novel compound showing anti-tumor properties was synthesized by reacting Cp2TiCl2 with maltol (3-hydroxy-2-methyl-4-pyrone) and a pH of 5.4, leading to a complete replacement of Cp and chloride ligands affording, Ti(maltolato)2(OH)2. The further crystallization of Ti(maltolato)2(OH)2 at pH of 8.4 leads to the formation of the novel anti-tumor compound [Ti4(maltolato)8(?-O4)].
Abstract: Disclosed is a novel composition comprising a novel bi-cyclic compound, which is expected to be pharmaceutically active, and a glyceride. The stability of the bi-cyclic compound can be improved significantly by dissolving the same in a glyceride.
Abstract: Genipin derivatives and pharmaceutical compositions thereof that inhibit the activity of uncoupling protein-2 (UCP2) and are useful in treating deficient first-phase insulin secretion, non-insulin dependent diabetes mellitus, and ischemia in a mammal are disclosed.
Type:
Grant
Filed:
November 19, 2009
Date of Patent:
January 10, 2012
Assignees:
Beth Israel Deaconess Medical Center, Trustees of Boston University
Inventors:
Chen-Yu Zhang, Bradford B. Lowell, John A Porco, Jr., Ruichao Shen, Cheng T. Lin, Stefan Krauss
Abstract: Disclosed is a novel composition comprising a novel bi-cyclic compound, which is expected to be pharmaceutically active, and a glyceride. The stability of the bi-cyclic compound can be improved significantly by dissolving the same in a glyceride.
Abstract: This invention relates to dibenzothiopyran compounds. This invention also relates to layers and devices including at least one of these compounds.
Type:
Grant
Filed:
January 16, 2009
Date of Patent:
January 3, 2012
Assignee:
E.I. du Pont de Nemours and Company
Inventors:
Nora Sabina Radu, Steven W. Shuey, Ying Wang
Abstract: The present invention is directed to novel sulfamide and sulfamate derivatives, pharmaceutical compositions containing them and their use in the treatment of epilepsy and related disorders.
Type:
Grant
Filed:
June 16, 2005
Date of Patent:
December 27, 2011
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
David F. McComsey, Michael H. Parker, Allen B. Reitz, Bruce E. Maryanoff
Abstract: The present invention relates to a process for reducing a compound of formula (I) wherein X is halogen, a hydroxy group, an alkylsulfoniloxy group or an arylsulfonyloxy group; to give a compound of formula (II) as a diastereoisomerically pure compound of RS/SR configuration characterized in that said reduction is carried out by the use of (+)-B-chlorodiisopinocampheylborane or (?)-B-chlorodiisopinocampheylborane. The compounds of formula (II) are useful as intermediates for the preparation of Nebivolol.
Type:
Grant
Filed:
March 16, 2009
Date of Patent:
December 27, 2011
Assignee:
Zach System S.p.A.
Inventors:
Raffaella Volpicelli, Paolo Maragni, Franco Massaccesi, Ilaria Munari, Livius Cotarca, Johnny Foletto
Abstract: The present invention provides a cosmetic having equal to or a higher antioxidant activity and moisture retaining property than the above-described conventional vitamin E derivatives. The cosmetic also has an excellent emulsifying ability and solubilizing ability and remarkably reduces a sticky feeling on the skin (in particular, the sticky feeling during drying after the application on the skin). That is, the cosmetic of the present invention containing a vitamin E derivative represented by the following formula (I) or a salt thereof. [In the formula, R1, R2, and R3 represent a hydrogen atom or a methyl group; R4 represents a C1-6 alkanoyl group, a C1-6 alkyl group, a SO3H group, a P(O)(OH)2 group, a CH2COOH group or a COCH2CH(SO3H)COOH group; EO represents an ethylene oxide group; BO represents a butylene oxide group; k and n independently represent any one of numbers 0 to 30; and m represents any one of numbers 1 to 30.
Abstract: The present invention provides an industrially available method for efficiently producing high-purity S-(?)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid excellent in solid-liquid separability from an S-(?)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid ester, and also provides products obtained by the method. Under a temperature condition of 50-80° C. in an aqueous solvent, (A) an S-(?)-6-hydroxy-2,5,7,8-tetramethylchromane-2-carboxylic acid ester represented by the general formula (1) is hydrolyzed under a basic condition for 1-3 hours; then (B) the insoluble matters contained in the reaction solution resulting from the hydrolysis are removed; and (C) an acid is added to the resulting solution to effect crystallization; provided that R in the general formula (1) represents an alkyl or aryl group.
Abstract: Compounds of Formula (I) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by sodium-glucose transporter inhibitors (in particular, SGLT2 inhibitors).
Abstract: Flow reactor having a plurality of walled conduits each having an outer surface disposed for contact with a heat-transfer medium, an inlet distribution manifold in flow communication with a downstream manifold through channels formed by heterogeneous catalytic material disposed within each conduit during operation, and a sequence of zones comprising at least two zones, the zones including the walled conduits. The walled conduits within each zone have the same or different length measured along a longitudinal coordinate of the zone, the walled conduits within each zone have essentially uniform cross-section measured in a plane perpendicular to the longitudinal coordinate thereby defining volume of the zone, and in the sequence of zones, the total cross-sectional area of the conduits in each downstream zone varies from the prior upstream zone.
Type:
Grant
Filed:
December 4, 2007
Date of Patent:
December 20, 2011
Assignee:
BP Corporation North America Inc.
Inventors:
Hassan Taheri, Curtis D. Dickinson, Paul A. Jacobson
Abstract: The present invention relates to the technical purification of vinylene carbonate (VC) by means of a simple thermal treatment with organic compounds which possess amidic nitrogen-hydrogen bonds, followed by a distillation and a melt crystallization. In this way VC of ultra-high purity is obtained. The high-purity vinylene carbonate can be stored and transported without stabilizer.
Type:
Grant
Filed:
May 4, 2006
Date of Patent:
December 6, 2011
Assignee:
Saltigo GmbH
Inventors:
Reinhard Langer, Paul Wagner, Heinrich Grzinia
Abstract: 7-ethynyl-2,4,9-trithiaadamantane and related methods are presented. Manufacturing 7-ethynyl-2,4,9-trithiaadamantane includes the steps of: (1) reducing alkyl 2,4,9-trithiaadamantane-7-carboxylate to produce 7-hydroxymethyl-2,4,9-trithiaadamantane; (2) oxidizing 7-hydroxymethyl-2,4,9-trithiaadamantane to produces 7-carbonyl-2,4,9-trithiaadamantane; and (3) reacting 7-carbonyl-2,4,9-trithiaadamantane with Ohira-Bestmann reagent to produces 7-ethynyl-2,4,9-trithiaadamantane. Molecular wires having 2,4,9-trithiaadamantane surface anchors are also disclosed.