Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.
Type:
Grant
Filed:
September 13, 2007
Date of Patent:
July 29, 2008
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Lieven Meerpoel, Leo Jacobs Jozef Backx
Abstract: A process for the preparation of 4-hydroxyalkylamino-2-nitro-anisoles of the general formula (I) wherein m is 2 or 3; by reaction of a 4-halogeno-3-nitro-aniline of formula (II) with a chloroalkyl-chloroformate of formula (III), alkaline ring closure of the resulting carbamate and nucleophilic replacement of the halogeno atom by a methoxy group to form a derivative of formula (IV), and finally ring opening of the resulting cyclic carbamate by treatment with methanolic alkali metal hydroxide, followed by neutralization with inorganic or organic acids, wherein the complete reaction is executed in a non-aqueous medium; as well as process for the preparation of 2-amino-4-hydroxyalkylamino-anisoles of formula (V)
Type:
Grant
Filed:
April 19, 2007
Date of Patent:
July 29, 2008
Assignee:
The Procter & Gamble Company
Inventors:
Otto Göttel, Emmanuel Morand, Hans-Jürgen Braun
Abstract: Disclosed are compounds that include two or more haptens conjugated by a spacer or a carrier. The haptens may include diethylenetriaminepentaacetate (DTPA), histimine-succinyl-glutamine (HSG), or combinations of DTPA and HSG. The compound also includes an effector molecule which may be conjugated to one or more of the haptens, the spacer/carrier, or both. The effector molecule may be conjugated by a number of linkages including an ester linkage, an imino linkage, an amino linkage, a sulfide linkage, a thiosemicarbazone linkage, a semicarbazone linkage, an oxime linkage, an ether linkage, or combinations of these linkages. Also disclosed are methods of synthesizing the compounds and/or precursors of the compounds.
Type:
Grant
Filed:
February 11, 2004
Date of Patent:
July 29, 2008
Assignee:
Immunomedics, Inc.
Inventors:
William J. McBride, David M. Goldenberg, Carl Noren, Hans J. Hansen
Abstract: The present invention provides an improved process for the preparation of carbamates with high selectivity of pharmaceutical interest by an eco-friendly, non-toxic, phosgene-/isocyanate-/CO-free clean route through a reaction of amine, organic halide compound and carbon dioxide in the presence of a solid, reusable catalyst at moderate conditions and does not require additional cocatalyst/promoter as well as solvent.
Type:
Grant
Filed:
May 22, 2006
Date of Patent:
July 29, 2008
Assignee:
Council of Scientific and Industrial Research
Inventors:
Darbha Srinivas, Rajendra Srivastava, Paul Ratnasamy
Abstract: A process for forming a diarylamine compound, including reacting an aniline and an arylbromide in the presence of a palladium ligated catalyst and a base.
Abstract: Adamantane derivates which can be material compounds of a polymer excellent in etching resistance and having improved transmittance to light having a short wavelength, represented by the formula (2A?) wherein Y1F is a fluorine atom or a hydroxyl group.
Abstract: A process is disclosed that relates to the removal of impurities, specifically benzoic acid, from a mother liquor produced in the synthesis of carboxylic acid, typically terephthalic acid.
Type:
Grant
Filed:
August 11, 2005
Date of Patent:
July 22, 2008
Assignee:
Eastman Chemical Company
Inventors:
Robert Lin, Philip Edward Gibson, Kenny Randolph Parker
Abstract: The present invention is directed to secondary amino- and cycloamino-cycloalkanol derivatives, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.
Type:
Grant
Filed:
October 12, 2004
Date of Patent:
July 22, 2008
Assignee:
Wyeth
Inventors:
Paige Erin Mahaney, Michael Byron Webb, Lori Krim Gavrin, Eugene John Trybulski
Abstract: The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has ?3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus.
Abstract: There is herein provided a process for Zr-mediated hydroboration of alkynes which offers (E)-vinylboronic esters in high yield with stereoselectivity and regioselectivity.
Abstract: A compound comprising Formula I, or a mixture thereof, wherein Y is a bond or CmH2m?p(OA)p wherein m is 0 to 4, and p is 0 or 1, X? is X or H, X is CH2CH2OA, CH(CH2OA)2, C(CH2OA)3, or X and X? combine to form (CH2CH2)2NCH2CH2OA or (CH2CH2)2O, provided that when X and X? combine to form (CH2CH2)2O then Y is CH2CH(OA)CH2, A is CF2CFHO—Rf or H, Rf is CnF2n+1 wherein n is an integer of 1 to about 6, M is a cation having a charge equal to a, and a is a positive integer equal to 1 or 2, provided that at least one of X, X?, or Y contains A equal to CF2CFHO—Rf, and its use in lowering surface tension and imparting improved surface effects.
Type:
Grant
Filed:
August 6, 2007
Date of Patent:
July 15, 2008
Assignee:
E. I. du Pont de Nemours and Company
Inventors:
Peter Michael Murphy, Andrew Edward Feiring, Stephan James McLain, Jessica Sinks
Abstract: A phospholipid derivative represented by the following formula (I) wherein R1CO and R2CO independently represent an acyl group; R3 represents hydrogen atom, or a hydrocarbon group; symbol “a” represents an integer of 0 to 4; symbol “b” represents 0 or 1, provided that when a is 0, b is 0; X represents hydrogen atom, an alkali metal atom, an ammonium, or an organic ammonium; A1O and A3O represent an oxyalkylene group containing oxyethylene group, wherein the ratio of the oxyethylene group to the oxyalkylene group in A1O and A3O is 0.5 or larger in terms of a weight ratio; A2O represents an oxyalkylene group; symbols “m” and “q” represent an average molar number of added oxyalkylene groups; and symbol “n” represent an average molar number of added oxyalkylene groups; provided that m, n and q satisfy the following conditions: 5?m?600, 1?n?45, 0?q?200, 10?m+n+q?600, 0.04?n/(m+n+q), and q/(m+n+q)?0.
Abstract: Disclosed is an optimized process and apparatus for more efficiently and economically carrying out the liquid-phase oxidation of an oxidizable compound. Such liquid-phase oxidation is carried out in a bubble column reactor that provides for a highly efficient reaction at relatively low temperatures. When the oxidized compound is para-xylene and the product from the oxidation reaction is crude terephthalic acid (CTA), such CTA product can be purified and separated by more economical techniques than could be employed if the CTA were formed by a conventional high-temperature oxidation process.
Type:
Grant
Filed:
June 16, 2005
Date of Patent:
July 15, 2008
Assignee:
Eastman Chemical Company
Inventors:
Alan George Wonders, Howard Wood Jenkins, Jr., Lee Reynolds Partin, Wayne Scott Strasser, Marcel de Vreede
Abstract: Process for esterification of farnesol in an initial mixture comprising alpha-bisabolol, farnesol and optionally other components, with the following steps: 1. Preparation or production of the initial mixture, 2.
Type:
Grant
Filed:
October 27, 2006
Date of Patent:
July 15, 2008
Assignee:
Symrise GmbH & Co. KG
Inventors:
Marcus Betzer, Walter Kuhn, Burghard Wilkening, Dietmar Schatkowski, Oskar Koch
Abstract: A process and catalyst blend for selectively producing mercaptans and sulfides from alcohols. The alcohol is reacted with hydrogen sulfide, in the presence of a catalyst blend containing a hydrotreating catalyst and a dehydration catalyst to convert the alcohol to mercaptan or sulfide in one-pass. The alcohols can include primary and secondary alcohols. The mercaptan or sulfide having less than about 30% unreacted alcohol contained therein.
Type:
Grant
Filed:
December 13, 2005
Date of Patent:
July 15, 2008
Assignee:
Chevron Phillips Chemical Company LP
Inventors:
Daniel M. Hasenberg, Mitchell D. Refvik
Abstract: Pyrimidinedione derivatives of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them are useful for the treatment of inflammation and immunological diseases.
Abstract: The present invention provides novel intermediates represented by general formula (I) etc. for preparing a phenoxyacetic acid derivative represented by general formula (X) or a pharmaceutically acceptable salt thereof, which has ?3-adrenoceptor stimulating activity and are useful for treating or preventing obesity, hyperglycemia, diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression or biliary calculus.
Abstract: The present invention relates to biarylbisphosphines and intermediates thereof. The scope of the invention further encompasses catalysts preparable from the biarylbisphosphines and their use in asymmetric syntheses.
Abstract: A process for preparing N,N-dihydrocarbylhydroxylamines of the general formula (I) where R1, R2, R3 and R4 are selected independently from among hydrogen, aliphatic, cycloaliphatic, heteroaromatic and aromatic radicals, or R1 and R2 and/or R3 and R4 are joined to form a ring, and not more than one radical among R1, R2, R3 and R4 is hydrogen, which comprises the steps a) reaction of hydroxylamine H2NOH or a salt of hydroxylamine with a compound of the general formula (II) or (III) where R1, R2, R3 and R4 are as defined in formula (I), b) hydrogenation of the compound formed in step a) in the presence of a catalyst, c) further reaction of the compound formed in step b) with a compound of the general formula (II) or (III) and hydrogenation of the reaction mixture in the presence of a catalyst and d), if appropriate, reaction of the salt of the dihydrocarbylhydroxylamine formed in step c) with a base.