Oxy In Acid Moiety Patents (Class 560/29)
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Patent number: 7368566Abstract: Disclosed is a new process and intermediates for preparing benzazepines of Formula (I): wherein R1 and R2 are as defined herein.Type: GrantFiled: March 29, 2004Date of Patent: May 6, 2008Assignee: SmithKline Beecham CorporationInventors: Jose J. Conde, Lewilynn L. Goldfinger, Michael A. McGuire, Susan C. Shilcrat, Michael D. Wallace, Marvin Sungwhan Yu
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Patent number: 7365085Abstract: Disclosed is a compound having the formula: pharmaceutically acceptable salts or solvates thereof and pharmaceutical compositions containing the same, wherein the structural variables are as defined herein. The compounds, salts and solvates of this invention are useful as LXR agonists.Type: GrantFiled: March 26, 2003Date of Patent: April 29, 2008Assignee: SmithKline Beecham CorporationInventors: Ajita Bhat, John Jeffrey McAtee, Scott K. Thompson, James S. Frazee, Lara S. Kallander, Chun Ma, Joseph Marino, Michael J. Neeb, Robert A. Stavenger
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Publication number: 20080085930Abstract: The present invention relates to a novel crystal of (S)-(+)-2-(2-chlorophenyl)-2-hydroxy-ethyl carbamate, pharmaceutical compositions comprising this crystal and, and methods of making and using this crystal.Type: ApplicationFiled: October 5, 2007Publication date: April 10, 2008Inventor: Matthew Peterson
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Patent number: 7312360Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein the variables G, L, A, W, E, R2, R3, R4, R5, RN, and Rc are defined herein. These compounds interact with and inhibit the activity of the enzyme beta-secretase. These compounds are therefore useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions and methods of treatment of these diseases are also disclosed.Type: GrantFiled: December 6, 2002Date of Patent: December 25, 2007Assignees: Elan Pharmaceuticals, Inc., Pharmacia & Upjohn CompanyInventors: Ruth TenBrink, Michel Maillard, Martha Warpehoski
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Patent number: 7312345Abstract: The present invention provides, according to an aspect thereof, a novel process for the preparation of dronedarone [1] and pharmaceutically acceptable salts thereof. According to a preferred embodiment, the process comprises N-acetylating of p-anisidine or p-phenetidine with acetic anhydride, reacting of the obtained N-(4-alkoxyphenyl)acetamide with 2-bromohexanoyl chloride or bromide in the presence of aluminum chloride or bromide to obtain N-[3-(2-bromohexanoyl)-4-hydroxyphenyl]acetamide [6a], converting the compound [6a] into 2-butyl-5-benzofuranamine hydrochloride [12a] and subsequently converting [12a] into [1] or pharmaceutically acceptable salts thereof. In accordance with another aspect of this invention, there are provided novel intermediates, inter alia the novel compounds [6a] and [12a]. The novel intermediates of the present invention are stable, solid compounds, obtainable in high yields, which can be easily purified by crystallization and stored for long periods of time.Type: GrantFiled: November 6, 2002Date of Patent: December 25, 2007Assignee: ISP Investments Inc.Inventors: Arie Gutman, Gennadi Nisnevich, Lev Yudovitch
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Publication number: 20070270487Abstract: The present invention relates to a novel process suitable for large-scale production of phenyl propane derivatives as well as to novel intermediates in the process.Type: ApplicationFiled: May 17, 2007Publication date: November 22, 2007Inventors: Martin Hedberg, Marita Hogberg, Weimin Tong
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Patent number: 7045660Abstract: This invention is directed to a [di(ether or thioether)heteroaryl or fluoro substituted aryl] compound or an N-oxide thereof or a pharmaceutically acceptable salt thereof, which is useful for inhibiting the production or physiological effects of TNF in the treatment of a patient suffering from a disease state associated with a physiologically detrimental excess of tumor necrosis factor (TNF). Compounds within the scope of the present invention also inhibit cyclic AMP phosphodiesterase, and are useful in treating a disease state associated with pathological conditions that are modulated by inhibiting cyclic AMP phosphodiesterase, such disease states including inflammatory and autoimmune diseases, in particular type IV cyclic AMP phosphodiesterase. The present invention is therefore directed to their pharmacological use for inhibiting TNF and/or cyclic AMP phosphodiesterase, pharmacological compositions comprising the compounds and methods for their preparation.Type: GrantFiled: March 3, 2004Date of Patent: May 16, 2006Assignee: Aventis Pharma LimitedInventors: Garry Fenton, Tahir Nadeem Majid, Malcolm Norman Palfreyman
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Patent number: 7022872Abstract: The invention relates to a method for preparing F-Dopa and 18F-Dopa and intermediates that are useful in the method. The invention is a method that synthesizes F-Dopa and 18F-Dopa in good yield with high enantiopurity without the need for further transformations. The method includes the step of reacting a benzaldehyde derivative with a phosphonic acid derivative to produces an olefin intermediate that can be asymmetrically hydrogenated to produce the desired enantiomer.Type: GrantFiled: December 19, 2003Date of Patent: April 4, 2006Assignee: Molecular Technologies, Inc.Inventors: Joseph C. Walsh, Henry C. Padgett
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Patent number: 6972292Abstract: The present invention relates to certain substituted polyketides of formula I, wherein A, B, C, D, E, F and m are as defined herein, pharmaceutical compositions containing said compounds, and the use of said compounds in treating tumors.Type: GrantFiled: August 5, 2002Date of Patent: December 6, 2005Assignee: Novartis AGInventors: Frederick Ray Kinder, Jr., Kenneth W. Bair, Timothy M. Ramsey, Michael L. Sabio
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Patent number: 6953850Abstract: The invention provides collections of orthogonally-protected monosaccharides as universal building blocks for the synthesis of glycoconjugates of non-carbohydrate molecules, neo-glycoconjugates and oligosaccharides. This orthogonal protection strategy allows for the specific deprotection of any substituent ono the saccharide ring, and greatly facilitates targeted or library-focused carbohydrate-related syntheses. In particular, the invention provides a universal monosaccharide building block of General Formula (I) or General Formula (II) in which A is a leaving group; X is hydrogen, O, N or N3; X1 is hydrogen, —CH2O—, —CH2NH—, —CH3, —CH2N3 or —COO—; and B, C, D and E are protecting groups that can be cleaved orthogonally, and in which B, C, D and E are absent when X is hydrogen or N3, and E is absent when X1 is hydrogen, CH3 or N3.Type: GrantFiled: January 18, 2000Date of Patent: October 11, 2005Assignee: Alchemia Pty. Ltd.Inventors: Gyula Dekany, John Papagerogiou, Laurent Francois Bornaghi
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Patent number: 6939986Abstract: The invention provides a multistep process for preparing 1,2-diamino compounds and pharmaceutically acceptable addition salts thereof from 1,2-epoxides.Type: GrantFiled: February 22, 2002Date of Patent: September 6, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Martin Karpf, René Trussardi
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Patent number: 6852887Abstract: The present invention provides a new process for the preparation of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride, wherein this compound is prepared directly from the chloromethylalcohol. Importantly, the process of the present invention results in higher yields of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride without sacrificing its purity. The processes of the present invention can be used to prepare not only the 2S,3S-derivative, but also the 2R,3S-, 2S,2R- and the 2R,3R-derivatives.Type: GrantFiled: March 4, 2003Date of Patent: February 8, 2005Assignee: Aerojet Fine Chemicals LLCInventors: Aslam A. Malik, Hasan Palandoken, Joy A. Stringer, Roland P. Carlson, John Leach, Thomas G. Archibald, Robert G. Miotke
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Patent number: 6849626Abstract: The invention relates to semicarbazides of the general formula I where R1, R2, R3, R4 and I have the meaning indicated in claim 1. The compounds of the formula I can be employed as pharmaceutical active compounds in human and veterinary medicine, in particular for the control and prevention of thromboembolic disorders such as thrombosis, mycocardial infarct, arteriosclerosis, inflammation, apoplexy, angina pectoris, restenosis after angioplasty and intermittent claudication.Type: GrantFiled: August 21, 2001Date of Patent: February 1, 2005Assignee: Merck Patent GmbHInventors: Werner Mederski, Horst Juraszyk, Dieter Dorsch, Christos Tsaklakidis, Johannes Gleiltz, Christopher Barnes
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Patent number: 6831196Abstract: The invention relates to a highly active, highly specific urokinase inhibitor which is suitable for therapeutic applications and can be synthesized in an extremely simple manner. Surprisingly, it was found that amidino benzylamine derivatives, especially 4-amidino-benzylamine, with two bonded amino acids represent a new group of highly active and very selective uPA inhibitors. The urokinase inhibitors can be used in medical applications, e.g. in the treatment of malign tumors such as in cases of metastatic spread.Type: GrantFiled: December 9, 2002Date of Patent: December 14, 2004Assignee: Curacyte AGInventors: Jörg Stürzebecher, Torsten Steinmetzer, Andrea Schweinitz
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Patent number: 6831102Abstract: New thyroid receptor ligands are provided which have the general formula I: wherein R1 is halogen, trifluoromethyl, substituted or unsubstituted aryl, substituted or unsubstituted C1-6 alkyl, or substituted or unsubstituted C3-7 cycloalkyl; R2 and R3 are each independently hydrogen, halogen, substituted or unsubstituted C1-4 alkyl, or substituted or unsubstituted C3-6 cycloalkyl, wherein at least one of R2 and R3 is other than hydrogen; R4 is a carboxylic acid selected from the group consisting of (CH2)nCOOH, (CH)2COOH, NHCO(CH2)nCOOH, CONH(CH2)nCOOH and NH(CH2)mCOOH; n is an integer from 0 to 4; and m is an integer from 1 to 4. In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a T3 regulated gene, wherein a compound as described above is administered in a therapeutically effective amount.Type: GrantFiled: December 6, 2002Date of Patent: December 14, 2004Assignee: Bristol-Myers Squibb CompanyInventor: Jon J. Hangeland
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Publication number: 20040236119Abstract: The present invention relates to a process wherein a cyclic carbonate compound bearing an electrophilic group is reacted with a compound containing a nucleophilic group, especially an amine group. Such reactions permit to obtain urethane groups useful in polymer preparation, such as polyurethanes, or other urethane-containing polymers.Type: ApplicationFiled: April 12, 2004Publication date: November 25, 2004Inventor: Jurgen Van Holen
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Patent number: 6759511Abstract: The present invention relates to a carbonic acid ester compound of the following formula (1): in which X, Y, and Ar are defined in the specification, which can be easily combined with the amino group of an amino acid or removed therefrom under mild conditions, whereby the amino group can be effectively protected during peptide syntheses, process for preparing the same, and use of the same. Since the amino acid derivatives thus protected have high thermal and chemical stabilities and good solubility for organic solvents, peptides can be synthesized at a low cost with a high yield.Type: GrantFiled: October 31, 2002Date of Patent: July 6, 2004Assignee: Hanchem Co., Ltd.Inventors: Hogyu Han, Nakcheol Jeong, SangJo Lee, Jin Gab Oh, Hosung Yu
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Patent number: 6756511Abstract: Gamma-secretase inhibitors, useful in the treatment or prevention of Alzheimer's disease, are disclosed. The preferred compounds have, as the central portion of the molecule, the structure (a) and are di-astereoisomers of known protease inhibitors.Type: GrantFiled: July 18, 2002Date of Patent: June 29, 2004Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Timothy Harrison, Peter Alan Hunt, Alan John Nadin
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Publication number: 20040077690Abstract: Novel quaternary amidino-containing compounds of the general formulae (I), (II), (III), (IV), (V) and (VI): including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and the compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.Type: ApplicationFiled: October 16, 2003Publication date: April 22, 2004Inventors: Bing-Yan Zhu, Wenrong Huang, Penglie Zhang, Zhaozhong Jon Jia, Liang Bao, Yanhong Wu, Robert M. Scarborough
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Patent number: 6696487Abstract: The invention relates to compounds of formula (I), and also to salts thereof, which have fungicidal activities: in which the various radicals and substituents are as defined in the description, and also to the fungicidal compositions containing them and to methods for combating the phytopathogenic fungi of crops using these compounds and compositions.Type: GrantFiled: August 6, 2001Date of Patent: February 24, 2004Assignee: Bayer Cropscience S.A.Inventors: Vincent Gerusz, Darren James Mansfield, José Perez, David Tickle, Jean-Pierre Vors, Derek Baldwin, Thomas Lawley Hough, Dale Robert Mitchell
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Publication number: 20040023944Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-chalcogenmethylcarbonyl group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.Type: ApplicationFiled: May 21, 2003Publication date: February 5, 2004Applicant: Beacon Laboratories, Inc.Inventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman
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Patent number: 6686470Abstract: Compounds of the saframycin-ecteinascidin series with cytotoxic properties having the following general formula, their uses and synthesis, are disclosed: wherein R1 and R4 is H, a C1 to C4 alkyl group, or an acyl group; wherein R2 is an ether, ester, amide, or a phthalimide group; wherein R3 is ═O, OH, an ether group, an acyl group such as OC(O)Me, OC(O)Bn and OC(O)Et, or a sulfide group; wherein R5 is H, halogen, OH, an ether group, an acyl group, or an amide group; wherein R6 is ═O, OH, OCH3, CN, or an acyloxy group; wherein R7, is ═O, OH, halogen, an ether group, or an acyl group; wherein R8 and R9 are independently H, CH3, OCH3, OC2H5, CF3, halogen such as Br and F, or R8 and R9 are joined together as a methylenedioxy group, or other five or six membered ring; wherein R10 and R11 are independently CH3, OCH3, OC2H5, SCH3, or SC2H5; wherein R12 is H, a C1 to C4 alkyl group, or an acyl group; and wherein the chiral center marked * has the R or the S configuration.Type: GrantFiled: January 19, 2001Date of Patent: February 3, 2004Assignee: The Trustees of Columbia University in the City of New YorkInventors: Samuel J. Danishefsky, Bishan Zhou
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Patent number: 6683200Abstract: N-Substituted-N′-substituted urea derivatives represented by the following formula, analogs thereof or pharmaceutically acceptable salts thereof are herein provided. These compounds show a TNF-&agr; production inhibitory activity.Type: GrantFiled: October 4, 2001Date of Patent: January 27, 2004Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Shiro Mita, Masato Horiuchi, Masakazu Ban, Hiroshi Suhara
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Patent number: 6667413Abstract: The present invention relates to an uracil compound of the formula [I]: wherein W represents oxygen, sulfur, imino or C1 to C3 alkylimino; Y represents oxygen, sulfur, imino or C1 to C3 alkylimino; R1 represents C1 to C3 alkyl or C1 to C3 haloalkyl; R2 represents C1 to C3 alkyl; R4 represents hydrogen or methyl; R5 represents C1 to C6 alkyl, C1 to C6 haloalkyl, or the like; X1 represents halogen, cyano or nitro; X2 represents hydrogen or halogen; and each of X3 and X4 independently represents hydrogen, halogen, C1 to C6 alkyl, or the like. The present compound has an excellent herbicidal activity.Type: GrantFiled: July 12, 2002Date of Patent: December 23, 2003Assignee: Sumitomo Chemical Company, LimitedInventors: Yoshitomo Tohyama, Yuzuru Sanemitsu, Tomohiko Gotou
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Patent number: 6653501Abstract: A method is provided for processing a solution having optical isomers to obtain a (2R,3S) target isomer: wherein P1 is H or a hydroxyl protecting group, R1 is H, an alkyl group, an olefinic group or an aromatic group, and R2 is H or R3CO, where R3 is an alkyl group, an olefinic group, an aromatic group, an O-alkyl group, an O-olefinic group or an O-aromatic group, provided that R1 is not H when R3 is Ph and P1 is H. The method includes passing the solution through a chromatographic stationary phase, such as S,S Whelk-O, that has a greater affinity for one of the target isomer and an optical isomer thereof. A portion of the solution with the target isomer is then collected. The solution may be a racemic mixture of (±)-N-CBZ-3-phenylisoserine ethyl ester.Type: GrantFiled: June 27, 2001Date of Patent: November 25, 2003Assignee: NaPro BioTherapeutics, Inc.Inventors: James D. McChesney, Herbert R. Brinkman, Siead Zegar, David Baehr
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Patent number: 6649639Abstract: Picornaviral 3C protease inhibitors, obtainable by chemical synthesis, inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.Type: GrantFiled: September 7, 2001Date of Patent: November 18, 2003Inventors: Peter S. Dragovich, Thomas J. Prins, Ru Zhou
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Patent number: 6646150Abstract: The present invention provides a process for industrially producing (aminomethyl)trifluoromethylcarbinol derivatives, in particularly, optically active compounds thereof, which are useful as starting compounds for drugs such as protease inhibitors, etc.Type: GrantFiled: June 13, 2002Date of Patent: November 11, 2003Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Fuminori Sato, Tomoki Omodani, Ryotaro Shiratake, Yasunao Inoue, Takashi Deguchi
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Patent number: 6620961Abstract: Biarylalkylenecarbamic acid derivative represented by general formula (I): [wherein Q is a phenyl group which may be substituted or the like, X is a halogen atom, a (C1-C6) alkyl group or the like, n is 0 or an integer of from 1 to 4, R1 is a (C1-C6) alkyl group or the like, R2 is a hydrogen atom, a (C1-C6) alkyl group or the like, A is a (C1-C7) alkylene group which may be branched, and G is an oxygen atom, a sulfur atom or a group —NR— (wherein R3 is a hydrogen atom or a (C1-C4) alkyl group)] and agricultural and horticultural fungicides. The agricultural and horticultural fungicides of the present invention are useful as agricultural and horticultural fungicides because they have high preventive effects on cucumber downy mildew, apple scab, wheat powdery mildew, rice blast, cucumber gray mold and rice sheath blight without damaging crops, and are excellent in residual effectiveness and rain-resistance.Type: GrantFiled: February 25, 2000Date of Patent: September 16, 2003Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co. Ltd.Inventors: Kazuhiro Ikegaya, Masami Ozaki, Takahiro Kawashima, Ichiro Miura, Norimichi Muramatsu
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Patent number: 6610715Abstract: The present invention provides novel cathecol hydrazone derivatives of formula (I) or pharmaceutically acceptable salts thereof, wherein R1 is C1-7 alkyl or C3-7 cycloalkyl; R2 is hydrogen, hydroxy, C1-5 alkyl or —CH2CH2C(═O)NH2; R3 and R4 are independently hydrogen, C1-7 alkyl, —C(═X)—R5, or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one or two selected from a group consisting of halogen, C1-6 alkoxy, nitro, trifluoromethyl, C1-6 alkyl and carboxyl, or R3 and R4 are directly bonded by C3-4 containing oxygen, sulfur or nitrogen to form a heterocyclic ring, X is oxygen, sulfur or NH and R5 is C1-7 alkyl, —NHR6, CONH2 or 2-, 3- or 4-pyridyl, prymidyl or phenyl substituted with one selected from a group consisting of halogen, C1-6 alkoxy, nitrile, trifluoromethyl, C1-6 alkyl and carboxyl, and R6 is hydrogen, hydroxy, NH2, C1-5 alkoxy, C1-5 alkyl, pyridyl or phenyl.Type: GrantFiled: November 13, 2001Date of Patent: August 26, 2003Assignee: Cheil Jedang CorporationInventors: Yong Sik Youn, Myung Xik Xiang, Byoung Chol Suh, Jong Hoon Kim, Kwang Hyuk Lee, Eui Kyung Kim, Jae Kyu Shin, Chung Keun Rhee
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Publication number: 20030139470Abstract: The invention relates to 3,4-dihydroxybenzyl-substituted carbonic acid derivatives, to their production, and to their use as antioxidants or free-radical scavengers, especially in cosmetic and pharmaceutical preparations and in foodstuffs and stimulants, to protect cells and tissues from the harmful effects of radicals and reactive oxygen compounds that accelerate aging. The invention further relates to cosmetic and pharmaceutical preparations and to foodstuffs and stimulants that comprises the inventive 3,4-dihydroxybenzyl-substituted carbonic acid derivatives.Type: ApplicationFiled: December 19, 2002Publication date: July 24, 2003Inventors: Jakob Peter Ley, William Johncock, Roland Langner
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Patent number: 6573399Abstract: The present invention provides a commercially profitable process for producing a &bgr;-amino acid ester derivative which comprises reacting an &agr;-amino acid ester derivative with a base and a dihalomethane, reacting the same with a lithium amide and an alkyllithium in succession, and treating the reaction product with an acid in an alcohol.Type: GrantFiled: February 21, 2001Date of Patent: June 3, 2003Assignee: Kaneka CorporationInventors: Akira Nishiyama, Kenji Inoue
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Patent number: 6570034Abstract: The present invention relates to a novel blocked phenylenediamine developer useful, in reactive association, for enabling, on development, a non-magenta color, for example a cyan color, from a dye-forming coupler. In one embodiment, the developer has the property that the dye color formed with the coupler is distinctly different from the color formed by the same coupler with an oxidized form of the conventional developer 4-(N-ethyl-N-2-hydroxyethyl)-2-methylphenylenediamine. The invention is also directed to a light-sensitive silver-halide color photographic element comprising the blocked developing agent according to the present invention.Type: GrantFiled: May 31, 2001Date of Patent: May 27, 2003Assignee: Eastman Kodak CompanyInventors: Richard P. Szajewski, Lyn M. Irving
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Patent number: 6548706Abstract: The present invention provides a new process for the preparation of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride, wherein this compound is prepared directly from the chloromethylalcohol. Importantly, the process of the present invention results in higher yields of 2S,3S-N-isobutyl-N-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamide hydrochloride without sacrificing its purity. The processes of the present inventin can be used to prepare not only the 2S,3S-derivative, but also the 2R,3S-, 2S,2R- and the 2R,3R-derivatives.Type: GrantFiled: December 22, 2000Date of Patent: April 15, 2003Assignee: Aerojet Fine Chemicals LLCInventors: Aslam A. Malik, Hasan Palandoken, Joy A. Stringer, Roland P. Carlson, John Leach, Thomas G. Archibald, Robert G. Miotke
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Patent number: 6498004Abstract: This invention provides a photographic element comprising at least one silver halide emulsion layer in which the silver halide is sensitized with a compound of the formula (a): &Dgr;−(t)m−XY′ (a) XY′−(t)m−&Dgr; (b) &Dgr;−(t)m−XY′−(t)m−&Dgr; (c) wherein &Dgr; is protective group that is eliminated during development of the photographic element, t is a timing group, m is an integer from 0 to 3, and XY′ is a fragmentable electron donor moiety in which X is an electron donor group and Y′ is a leaving proton H or a leaving group Y, with the proviso that if Y′ is a proton, a base, &bgr;−, is present in the emulsion or is covalently linked directly or indirectly to X, and wherein: 1) X—Y′ has an oxidation potential between 0 and about 1.Type: GrantFiled: December 28, 2000Date of Patent: December 24, 2002Assignee: Eastman Kodak CompanyInventors: Jerome R. Lenhard, Annabel A. Muenter, Stephen A. Godleski, Paul A. Zielinski, Deepak Shukla, Donald R. Diehl
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Publication number: 20020188020Abstract: This invention is directed to compounds of the following formula: 1Type: ApplicationFiled: August 31, 2001Publication date: December 12, 2002Applicant: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Michael Chorev, Tamar Goren, Yacov Herzig, Jeffrey Sterling, Marta Weinstock-Rosin, Moussa B.H. Youdim
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Patent number: 6492515Abstract: The present invention relates to benzoxazinones of formula I: or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as an assay standard or reagent, and intermediates and processes for making the same.Type: GrantFiled: July 31, 2001Date of Patent: December 10, 2002Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Joseph Marian Fortunak, Mona Patel
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Patent number: 6486350Abstract: Disclosed are biological reagents which comprise compounds that inhibit &bgr;-amyloid peptide release and/or its synthesis, and, accordingly, have utility in determining the cellular mechanism involved in the generation of &bgr;-amyloid peptide.Type: GrantFiled: September 29, 1999Date of Patent: November 26, 2002Assignees: Elan Pharmaceuticals Inc., Eli Lilly & CompanyInventors: James E. Audia, Paul A. Hyslop, Jeffrey S. Nissen, Richard C. Thompson, Jay S. Tung, Laura I. Tanner
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Patent number: 6486341Abstract: Compounds of formula (I) wherein R1 is C1-C4-alkyl or cyclopropyl; R2 is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkinyl; or C1-C6-alkyl substituted by 1 to 5 fluorine atoms; R3 is C1-C6-alkyl, C1-C6-alkoxy, C3-C6-cycloalkyl, C3-C6-cycloalkoxy, C2-C6-alkenyl, C2-C6-alkenyloxy, C2-C6-alkinyl, C2-C6-alkinyloxy, C1-C6-alkoxycarbonyl, CN, or aryl, heteroaryl, heterocyclyl, aryloxy, heteroaryloxy or heterocyclyloxy, whereby the above-mentioned groups may be substituted by identical of different substituents, R5 signifies hydrogen or methyl; R6 and R7 are C1-C4-alkyl; have microbicidal, insecticidal and acaricidal activity and may be used for the control of pests and plant-pathogenic fungi in agriculture, horticulture and in the field of hygiene.Type: GrantFiled: July 10, 2001Date of Patent: November 26, 2002Assignee: Bayer AktiengesellschaftInventor: Hugo Ziegler
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Patent number: 6465678Abstract: Methyl carbazate which is particularly pure and has a particularly low tendency toward discoloration is obtained from hydrazine and dimethyl carbonate if the two reactants are metered simultaneously into an initially introduced first solvent at from −20 to +30° C., the solvent and low-boiling components are then distilled off under reduced pressure, and then either a second solvent is added to the crude methyl carbazate present and this solvent is distilled off under reduced pressure or an inert gas is passed through the crude methyl carbazate present.Type: GrantFiled: July 20, 2001Date of Patent: October 15, 2002Assignee: Bayer AktiengesellschaftInventors: Lars Rodefeld, Horst Behre, Alexander Klausener, Robert Söllner
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Publication number: 20020137961Abstract: The present invention relates to certain resorcinol derivatives and their use as skin lightening agents.Type: ApplicationFiled: September 17, 2001Publication date: September 26, 2002Inventors: Stuart E. Bradley, Eric W. Collington, Matthew C. Fyfe, William T. Gattrell, Joanna V. Geden, Peter J. Murray, Martin J. Procter, Robert J. Rowley, Jonathan G. Williams
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Patent number: 6444849Abstract: A compound represented by the following general formula (1); wherein X represents R1(R2)(R3)C— where R1 represents a C3-C8 cycloalkyl group, an optionally substituted C6-C14 aryl group, an optionally substituted heterocyclic residue, an optionally substituted C6-C14 aryloxy group, or an optionally substituted C7-C15 arylmethyl group; R2 and R3 independently represent hydrogen atom or a C1-C5 alkyl group, or R2 and R3 may combine to represent a C2-C7 alkylene group; or X represents R7—A— wherein R7 represents (i) a C1-C10 alkyl group which may optionally be substituted with an optionally substituted C6-C14 aryl group, an optionally substituted fluorenyl group or an optionally substituted heterocyclic group, (ii) an optionally substituted C6-C14 aryl group or (iii) an optionally substituted heterocyclic group, and A represents an oxygen atom or —N—R8 where R8 represents hydrogen atom or a C1-C5 alkyl group, Y represents an oxygen atom or a sulfur atom, R4 and RType: GrantFiled: December 22, 1999Date of Patent: September 3, 2002Assignee: Mitsubishi Chemical CorporationInventors: Ryoichi Ando, Makoto Kawamura, Noriko Chiba, Kazutoshi Watanabe
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Patent number: 6437169Abstract: 1. A 1-naphthol compound represented by formula (I) below: wherein A represents the moiety of a compound having an acidic proton the pKa of a corresponding protonated form (AH) of which is 0 to 14, R1 represents an aliphatic group, aryl group, or heterocyclic group, R2 represents a substituent, n represents an integer of 0 to 5, X represents a hydrogen atom, halogen atom, R11—, R11O—, R11S—, R11OCOO—, R12COO—, R12(R13)NCOO—, R12CON(R13)—, —NO, —NO2, or —N═N—R11, wherein R11 represents an aliphatic group, aryl group, or heterocyclic group, and each of R12 and R13 independently represents a hydrogen atom, aliphatic group, aryl group, or heterocyclic group, and Y represents an oxygen atom or sulfur atom.Type: GrantFiled: June 19, 2000Date of Patent: August 20, 2002Assignee: Fuji Photo Film Co., Ltd.Inventors: Takayuki Ito, Koji Takaku
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Patent number: 6423854Abstract: Use of at least one aminophenol derivative of formula (I) below: in which: R represents a hydrogen atom or a radical —COR2, wherein R2 represents a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon or alkoxy radical; R1 is a radical of formula (a), (b) or (c) below: (a) —CO—NR3R4 (b) —CO—O—R5 (c) —SO2—R5 wherein R3 represents a hydrogen atom or a linear or branched, saturated or unsaturated, optionally hydroxylated, C1 to C6 hydrocarbon radical, R4 represents a hydrogen atom or a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon radical, and R5 represents a saturated or unsaturated, linear, cyclic or branched, optionally hydroxylated, C1 to C30 hydrocarbon radical, in a depigmenting and/or bleaching cosmetic composition for human skin, body hairs or head hair; compositions comprising the derivatives of formula (I) and a process forType: GrantFiled: June 21, 1999Date of Patent: July 23, 2002Assignee: L'OrealInventors: Michel Philippe, Remy Tuloup, Christian Blaise
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Patent number: 6410749Abstract: Process for preparing optically active &bgr;-amino alcohols represented by a general formula (2): Ra—C*H(OH)—C*H(Rb)—Rc wherein Ra and Rc are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, Rb is one member selected from among groups represented by the following general formulae; (3) R1CO(R2)N—, and (4) R1CO(R1′CO)N—, and C* is an asymmetric carbon atom, characterized by reacting a racemic &agr;-aminocarbonyl compound represented by the general formula (1): Ra—CO—CH(Rb)—Rc, with hydrogen in the presence of an optically active transition metal compound represented by a general formula (7): MaXY(Px)m(Nx)n wherein Ma represents a metal atom belonging to VIII-group of the periodic law, X and Y represent each independently hydrogen, halogeno, Px represents a phosphine ligand, Nx represents an amine ligand, at least one of Px and Nx is optically active, and m and n each independently represent 0 or an integer of 1 thType: GrantFiled: July 17, 2001Date of Patent: June 25, 2002Assignee: Nippon Soda Co., Ltd.Inventors: Eiji Katayama, Daisuke Sato, Hirohito Ooka, Tsutomu Inoue
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Patent number: 6391904Abstract: A compound of the formula where the substituents are defined in the specification and its pharmaceutically acceptable salts and prodrugs thereof useful as antagonists of vitronectin receptors.Type: GrantFiled: June 29, 2001Date of Patent: May 21, 2002Assignees: Aventis Pharma S.A., Genentech, Inc.Inventors: Denis Carniato, Jean-Francois Gourvest, Jean-Marie Ruxer, Jochen Knolle, Anurschirwan Peyman, Sarah C. Bodary, Thomas R. Gadek
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Patent number: 6388134Abstract: The present invention refers to new derivatives of the 6-(4-phenylbutoxy)hexylamine of the general formula (I): wherein: R1 is CHO or CHOR3OR4, where R3 and R4 independently are C1-C6 alkyl, aralkyl, or they form 5 or 6 membered cyclic acetals; and R2 is H, benzyl or an alkyloxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl or acyl group; and to a process for its obtention. The invention also refers to a new process for obtaining Salmeterol or its pharmaceutically acceptable salts, characterized in that reaction of an organometallic compound of the general formula (13) is carried out in an inert solvent at low temperature with a synthetic intermediate of the general formula (I), wherein R1 is CHO, and R2 is an alkyloxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl or acyl group.Type: GrantFiled: March 28, 2001Date of Patent: May 14, 2002Inventors: Jordi Bessa Bellmunt, Pere Dalmases Barjoan, Francisco Marquillas Olondriz
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Patent number: 6369270Abstract: Compound of the formula are useful as intermediates to new 4-benzoylisoxazoles.Type: GrantFiled: October 19, 1999Date of Patent: April 9, 2002Assignee: Rhone Poulenc Agriculture LimitedInventors: Angela Jacqueline Bailey, Michael Gingell, David William Hawkins
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Publication number: 20020026068Abstract: Composition containing at least one aminophenol derivative and a solubilizing compound which is not in the form of vesicles, chosen from: (a) oxyalkylenated fatty acid esters of sorbitan, (b) oxyalkylenated hydrogenated castor oils, and/or (c) oxyalkylenated fatty alcohols. The invention also relates to a process for dissolving at least one aminophenol derivative by mixing it with a solubilizing agent as defined above.Type: ApplicationFiled: December 20, 2000Publication date: February 28, 2002Applicant: L'OREALInventors: Veronique Chevalier, Melanie Quest
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Patent number: RE38796Abstract: Compounds formed by reacting a protected amino acid with an alkali metal enolate of an alkyl acetate are reacted with a halogenating agent for halogenation of the 2-position, or a protected amino acid is reacted with an alkali metal enolate of an alkyl halogenoacetate, to form a 4-amino-3-oxo-2-halogenobutanoic acid ester derivative, and hydrolysis and decarboxylation are conducted to produce a 3-amino-2-oxo-1-halogenopropane derivative or its salt. The present method is a useful process for producing a 3-amino-2-oxo-1-halogenopropane derivatives which can easily be converted to a 3-amino-1,2-epoxypropane.Type: GrantFiled: June 16, 2000Date of Patent: September 13, 2005Assignee: Ajinomoto Co.,Inc.Inventors: Yutaka Honda, Satoshi Katayama, Kunisuke Izawa, Masakazu Nakazawa, Takayuki Suzuki, Naoko Kanno
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Patent number: RE39616Abstract: This invention is directed to compounds of the following formula: wherein when a is 0, b is 1 or 2; when a is 1, b is 1, m is from 0-3, X is O or S, Y is halogeno, R1 is hydrogen C1-4 alkyl, R2 is hydrogen, C1-4 alkyl, or optionally substituted propargyl and R3 and R4 are each independently hydrogen, C1-6 alkyl, C6-12 aryl, C6-12 aralkyl each optionally substituted. This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADD), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome, Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia. This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: March 25, 2005Date of Patent: May 8, 2007Assignees: Teva Pharmaceutical Industries, Ltd., Yissum Research Development Company of the Hebrew University of Jerusalem, Technion Research and Development Foundation, Ltd.Inventors: Michael Chorev, Tamar Goren, Yacov Herzig, Jeffrey Sterling, Marta Weinstock-Rosin, Moussa B. H. Youdim