Patents Examined by Robert Shiao
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Patent number: 7199141Abstract: Nitro-oxyderivative compounds or salts thereof having the following general formula (I): A—(B)b0—(C)c0—NO2 wherein: c0 is an integer and is 0 or 1, b0 is an integer and is 0 or 1, A=R—T1—, wherein R is the radical of an analgesic drug for the chronic pain, in particular for the neuropathic pain; B is such that its precursor is selected from anminoacids, hydroxyacids, polyalcohols, compounds containing at least one acid function; C is a bivalent radical containing an aliphatic, heterocyclic or aromatic radical.Type: GrantFiled: May 10, 2002Date of Patent: April 3, 2007Assignee: Nicox S.A.Inventors: Piero Del Soldato, Ennio Ongini
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Patent number: 7199264Abstract: Provided is a separating method for an optical isomer mixture comprising the steps of mixing an amino acid derivative such as N-(tert-butoxycarbonyl)-DL-alanine in which optical isomers of a D type and an L type are present in a mixture with a hydrophilic compound such as ?-cyclodextrin having a different affinity to two kinds of the optical isomers described above and then bringing the resulting aqueous solution or aqueous suspension into contact with a hydrophobic substance such as a solid matter subjected on a surface thereof to hydrophobic treatment on the condition that the pH is 3.5 or lower or under the coexistence of ions including an atomic group having hydrophobicity which can be a counter ion for the amino acid derivative described above such as a triethylammonium ion to thereby separate the D type amino acid derivative from the L type amino acid derivative present in the above aqueous solution or aqueous suspension.Type: GrantFiled: October 25, 2001Date of Patent: April 3, 2007Assignee: Tokuyama CorporationInventors: Shin Watanabe, Mizue Kawahara
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Patent number: 7199250Abstract: The invention includes methods of processing an initial di-carbonyl compound by conversion to a cyclic compound. The cyclic compound is reacted with an alkylating agent to form a derivative having an alkylated ring nitrogen. The invention encompasses a method of producing an N-alkyl product. Ammonia content of a solution is adjusted to produce a ratio of ammonia to di-carboxylate compound of from about 1:1 to about 1.5:1. An alkylating agent is added and the initial compound is alkylated and cyclized. The invention includes methods of making N-methyl pyrrolidinone (NMP). Aqueous ammonia and succinate is introduced into a vessel and ammonia is adjusted to provide a ratio of ammonia to succinate of less than 2:1. A methylating agent is reacted with succinate at a temperature of from greater than 100° C. to about 400° C. to produce N-methyl succinimide which is purified and hydrogenated to form NMP.Type: GrantFiled: December 10, 2003Date of Patent: April 3, 2007Assignee: Battelle Memorial InstituteInventors: Todd A. Werpy, John G. Frye, Jr., James F. White, Johnathan E. Holladay, Alan H. Zacher
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Patent number: 7192982Abstract: Disclosed is a compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aromatic group. Q is a covalent bond, —CH2— or —CH2CH2—; W is a substituted or unsubstituted alkylene or a substituted or unsubstituted heteroalkylene linking group from two to ten atoms in length, preferably from two to seven atoms in length.Type: GrantFiled: May 30, 2002Date of Patent: March 20, 2007Assignees: Ligand Pharmaceuticals, Inc., Eli Lilly and CompanyInventors: Dawn Alisa Brooks, Alan M. Warshawsky, Chahrzad Montrose-Rafezadeh, Anne-Reifel Miller, Lourdes Prieto, Isabel Rojo, Jose Alfredo Martin, Maria Rosario Gonzales Garcia, Alicia Torrado, Rafael Ferritto Crespo, Carlos Lamas-Peteira, Robert J. Ardecky, Maria Martin-Ortega Finger
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Patent number: 7193090Abstract: A process for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, tert-butylester comprising: (a) reduction of 5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-oxo-1-pentanoic acid, (R)-2-hydroxy-1,2,2-triphenylethyl ester; (b) hydrolysis of (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (R)-2-hydroxy-1,2,2-triphenylethyl ester using an alkali base in a solvent to form the acid; (c) alkylation of the acid forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, tert-butylester.Type: GrantFiled: March 16, 2004Date of Patent: March 20, 2007Assignee: Apotex Pharmachem Inc.Inventors: Bhaskar Reddy Guntoori, Daqing Che, Fan Wang, Yajun Zhao, K. S. Keshava Murthy, Stephen E. Horne
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Patent number: 7189751Abstract: The present invention provides medicinal compositions characterized by comprising as the active ingredient either a compound represented by a formula [I] or a pharmaceutically acceptable composite thereof; [wherein X represents oxygen or sulfur; R1 represents e.g., C1-4 alkyl, phenyl optionally substituted, etc.; Q1 represents spacer consisted of 0 to 3 carbon atoms; R2 represents, e.g., phenyl optionally substituted; R3 represents, e.g., hydrogen, C1-4 alkyl, or a group represented by the following formulae; —CONH—R6; R4 and R5 represent e.g., nitro, cyano, C1-4 alkylcarbonyl, respectively]; in particular, medicine which is useful as therapeutic and/or protective drugs for inflammatory diseases and/or allergic diseases by improving sick conditions accompanied with the stimulated phospholipase A(2) activity.Type: GrantFiled: June 25, 2002Date of Patent: March 13, 2007Assignee: Nippon Soda Co., Ltd.Inventors: Masae Takagi, Tadayuki Nishibe, Keiichi Ishimitsu
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Patent number: 7186704Abstract: Novel synthetic forms of etherified oxidized phospholipids and methods of utilizing same for preventing and treating atherosclerosis and other related disorders, as well as inflammatory disorders, immune mediated diseases, autoimmune diseases and proliferative disorders, are provided. In addition, methods of synthesizing etherified and esterified oxidized phospholipids and of using same for preventing and treating atherosclerosis and other related disorders are also provided.Type: GrantFiled: November 24, 2003Date of Patent: March 6, 2007Assignee: Vascular Biogenics Ltd.Inventors: Dror Harats, Jacob George, Gideon Halperin
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Patent number: 7183417Abstract: A simple and effective stereocontrolled synthesis of salinosporamide A(1) has been developed which follows the pathway outlined in the FIGURE. The process, the first total synthesis of salinosporamide A, is capable of providing the compound in substantial quantities for further biological studies. In addition to the method of Scheme I, the present invention also includes several novel synthetic intermediate compounds, several intermediate steps of the preferred synthetic process; and the uses of these compounds in the preparation of synthetic derivatives of the compound Salinosporamide A. Salinosporamide A is of special interest as a synthetic target because of its protein in vitro cytotoxic activity against many tumor cell lines (IC50 values of 10 nM or less).Type: GrantFiled: April 9, 2004Date of Patent: February 27, 2007Assignee: President and Fellows of Harvard CollegeInventor: Elias J. Corey
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Patent number: 7183307Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: wherein B, R1, n, R3, Q and R4 are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.Type: GrantFiled: May 3, 2004Date of Patent: February 27, 2007Assignee: Vertex Pharmaceuticals IncroporatedInventors: Michael Robin Hale, James Walter Janetka, Francois Maltais, Qing Tang
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Patent number: 7179925Abstract: The present invention relates to a process for the reduction of aliphatic, aromatic or heterocyclic organic compounds by means of hydrides and/or derivatives thereof.Type: GrantFiled: March 1, 2001Date of Patent: February 20, 2007Assignee: Merck Patent GmbHInventors: Hanns Wurziger, Guido Pieper, Norbert Schwesinger
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Patent number: 7179927Abstract: There is disclosed a method for treating a source of azadirachtin: (a) dissolving said sample in an organic polar solvent; (b) combining the solution of step (a) with an organic non-polar solvent to form a single phase containing the said solvents and dissolved sample; (c) treating said single phase of step (b) with an aqueous salt solution to form an aqueous phase and a phase containing the organic non-polar solvent; and (d) recovering one or other or both of the aqueous phase and the phase containing the organic polar solvent.Type: GrantFiled: October 15, 2001Date of Patent: February 20, 2007Inventors: David Michael Williams, Chandra Mohen Pant
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Patent number: 7176231Abstract: The present invention relates to aryl-containing 5-acylindolinones of general formula wherein R1 to R3 are defined herein, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on protein kinases, particularly an inhibiting effect on the activity of glycogen synthase kinase (GSK-3).Type: GrantFiled: March 10, 2005Date of Patent: February 13, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Armin Heckel, Gerald Juergen Roth, Joerg Kley, Stefan Hoerer, Ingo Uphues
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Patent number: 7173018Abstract: Disclosed are compounds having non-steroidal anti-inflammatory drugs (NSAIDS) covalently linked to a phospholipid moiety via a bridging group. Also disclosed are a process for the synthesis of the compounds, pharmaceutical compositions comprising the compounds and the use thereof for the treatment of diseases and disorders related to inflammatory conditions, such as the treatment of ischemia.Type: GrantFiled: January 14, 2004Date of Patent: February 6, 2007Assignee: D-Pharm, Ltd.Inventors: Alexander Kozak, Israel Shapiro
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Patent number: 7169933Abstract: Compounds having two reactive functional groups are described that can be used to provide a connector group between a substrate and an amine-containing material. The first reactive functional group can be used to provide attachment to a surface of a substrate. The second reactive functional group is a N-sulfonylaminocarbonyl group that can be reacted with an amine-containing material, particularly a primary aliphatic amine, to form a carbonylimino-containing connector group. The invention also provides articles and methods for immobilizing amine-containing materials to a substrate.Type: GrantFiled: November 14, 2003Date of Patent: January 30, 2007Assignee: 3M Innovative Properties CompanyInventors: Karl E. Benson, Moses M. David, Cary A. Kipke, Brinda B. Lakshmi, Charles M. Leir, George G. Moore, Rahul Shah
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Patent number: 7166736Abstract: Neopentyl glycol bis(diphenyl phosphate) liquid compositions are described that comprise from about 75% to about 90%, by weight, of neopentyl glycol bis(diphenyl phosphate), less than about 5% by weight of cyclic product, less than about 8% by weight of triphenyl phosphate, and with a P3 content of no less than about 1%, by weight. These compositions are made by continuously adding neopentyl glycol to a diaryl chlorophosphate mixture at elevated temperature, under vacuum, and in the presence of a catalyst.Type: GrantFiled: May 6, 2003Date of Patent: January 23, 2007Assignee: Supresta LLCInventors: Danielle Angrand Bright, Ronald L. Pirrelli, Anantha Narayanan Desikan
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Patent number: 7166628Abstract: Disclosed are compounds of formula (I) Where Ar1, X, R3, R4, R5 and R6 are defined herein. The compounds of the invention inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: November 20, 2003Date of Patent: January 23, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Derek A. Cogan, Ming-Hong Hao, Kevin Chungeng Qian, Alan David Swinamer
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Patent number: 7164031Abstract: A process for continuously preparing 2-pyrrolidone by reacting gamma-butyrolactone with ammonia in the liquid phase in the presence of water, wherein the reaction is carried out at a temperature of from 275 to 300° C. and an absolute pressure of from 140 to 180 bar.Type: GrantFiled: August 30, 2002Date of Patent: January 16, 2007Assignee: BASF AktiengesellschaftInventors: Martin Rudloff, Peter Stops, Erhard Henkes, Helmut Schmidtke, Rolf-Hartmuth Fischer, Manfred Julius, Rolf Lebkücher, Karl-Heinz Ross
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Patent number: 7160908Abstract: A series of dynamic platinum compounds for cancer treatment are described. The compounds may become active and inactive reversibly.Type: GrantFiled: March 4, 2004Date of Patent: January 9, 2007Assignee: Unitech Pharmaceuticals, Inc.Inventor: Jiajiu Shaw
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Patent number: 7160877Abstract: The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula [I]: wherein A represents —CH2— or —S—, R1 represents hydrogen atom, a lower alkyl group, a hydroxy lower alkyl group or a lower-alkoxy lower alkyl group, X represents —N(R3)—, —O— or —CO—, where R3 represents hydrogen atom or a lower alkyl group, and R2 represents (1) a cyclic group which may be substituted, or (2) an amino group which may be substituted, or a pharmaceutically acceptable salt thereof, a method for preparing the above-mentioned compound and a pharmaceutical composition comprising the above-mentioned compound as an effective ingredient.Type: GrantFiled: June 22, 2004Date of Patent: January 9, 2007Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Kosuke Yasuda, Hiroshi Morimoto, Saburo Kawanami, Masataka Hikota, Takeshi Matsumoto, Kenji Arakawa
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Patent number: 7157498Abstract: The invention concerns diamines of general formula (I), wherein: A represents a group A1 or A2 of general formula (II); B represents a group B1 or B2 of general formula (III); X represents a SO2, CH2, C?O or COO; YZ represents a group of formula CH(R25)—CH(R26) or CH(R27)?(R28), and R1 to R28, identical or different, represent independently of one another, a hydrogen or halogen atom or an alkyl, cycloalkyl, CN, NO2, hydroxy, aryl, aralkyl, alkoxy, aryloxy, amino, alkylamino, dialkylamino, cycloalkylamino, arylamino, arylalkylamino, diarylamino diarylalkylamino, trihalogenoalkyl or trihalogenoalkoxy group, provided that in the group A1, at least one of the radicals R1, R2, R3, R4 or R5 represents the hydrogen atom when the other four do not represent the hydrogen atom and in the group B1, at least one of the radicals R13, R14, R15, R16 or R17 represents the hydrogen atom when the other four do not represent the hydrogen atom, and their salts with a pharmaceutically acceptable acid, in the form of racemic mixtuType: GrantFiled: August 7, 2001Date of Patent: January 2, 2007Assignee: Centre National de la Recherche Scientifique (CNRS)Inventors: Philippe Marcel Dauban, Robert Hugh Dodd, Helene Veronique Faure, Martial Ruat, Pierre Jean-Paul Potier, Albane Kessler