Patents Examined by N. Wright
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Patent number: 6310209Abstract: The present invention relates to a method for the synthesis of the dihydroindole C-ring found in CC-1065/duocarmycin analogs.Type: GrantFiled: July 10, 2000Date of Patent: October 30, 2001Assignee: The Scripps Research InstituteInventor: Dale L. Boger
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Patent number: 6306852Abstract: Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R1 and R2 are optional substituents and independently represent C1-6 alkyl, C2-6 alkenyl, optionally substituted by CO2H or CO2(C1-6 alkyl), C2-6 alkynyl, halogen, C1-3 perfluoroalkyl, (CH2)mAr1, (CH2)mHet1, (CH2)mCONR7R8, (CH2)mCO2R8, O(CH2)qCO2R8, (CH2)mCOR8, (CH2)mOR8, O(CH2)pOR8, (CH2)mNR7R8, CO2(CH2)qNR7R8, (CH2)mCN, S(O)nR8, SO2NR7R8, CONH(CH2)mAr1 or CONH(CH2)mHet1; R3 represents H, C1-6 alkyl, (CH2)pNR9R10, SO2R10, SO2NR9R10, (CH2)mCO2R10, C2-6 alkenyl, C2-6 alkynyl, (CH2)mCONR9R10, (CH2)mCO2R10, (CH2)pCN, (CH2)pR10 or (CH2)pOR10; R4 represents H or C1-6 alkyl; R5 represents H or OH; R6 represents phenyl optionally fused to a herterocyclic ring, the group as a whole being optionally substituted; R7-10 are fully defined herein and may independently represent Ar2 or Het2; Z represents CO2H, CONH(tetrazol-5-yl), CONHSO2O(C1-4 alkyl), CO2Ar3, CO2(C1-6 alkyl), tetrazol-5-yl, CONHSO2Ar3, CONHSO2(CH2)qAr3 oType: GrantFiled: April 24, 2000Date of Patent: October 23, 2001Assignee: Pfizer Inc.Inventors: David James Rawson, Kevin Neil Dack, Roger Peter Dickinson, Kim James
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Patent number: 6291685Abstract: The present invention is concerned with a novel process for the preparation of the hydroxybenzothiophene of formula I comprising cyclocarbonylation of a compound of formula II wherein Y is as defined in the specification, followed by saponification. The compound of Formula I is a building block of pharmaceutically active substances, e.g. 5-[4-[2-(5-methyl-2-phenyl-4-oxazolyl)ethoxy]-7-benzothiophenylmethyl]-2,4-thiazolidinedione and the corresponding sodium salt which are from agents useful in the treatment of diabetes.Type: GrantFiled: July 26, 2000Date of Patent: September 18, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Junghans, Michelangelo Scalone, Thomas Albert Zeibig
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Patent number: 6288238Abstract: A process for preparing 5-hydroxymethyl-2-oxazolidinone (1), preferably optically active, in one step from 3,4-boronic acid ester protected 3,4-dihydroxybutyramides (2) is described. The oxazolidinone is important in the pharmaceutical industry especially in the areas of antimicrobials and behavioral disorders.Type: GrantFiled: September 19, 2000Date of Patent: September 11, 2001Assignee: Board of Trustees operating Michigan State UniversityInventors: Rawle I. Hollingsworth, Guijun Wang
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Patent number: 6288061Abstract: The present invention relates to the imidazole derivative of the following formula (I) wherein R1 is hydrogen, optionally substituted alkyl and the like, R2 is hydrogen, optionally substituted alkyl and the like, R3is optionally substituted heteroaryl, R4 is optionally substituted cycloalkyl, optionally substituted phenyl and the like, provided that when R1 is hydrogen, and R2 and R4 are the same or different and each is phenyl or phenyl substituted by halogen atom, lower alkyl or lower alkoxy, R3 is benzothiazolyl or thiazolyl substituted by phenyl, the imidazole derivative of the following formula (XII) wherein R6 is optionally substituted phenyl or optionally substituted heteroaryl and R7 is substituted phenyl, and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 21, 2000Date of Patent: September 11, 2001Assignee: Welfide CorporationInventors: Hiroyuki Sueoka, Jouji Yasuoka, Akira Nishiyama, Masatoshi Kiuchi, Katsuya Yamamoto, Kunio Sugahara, Syuji Ehara, Kei Sakata
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Patent number: 6277995Abstract: A process for preparing a compound represented by formula (I), wherein R1 represents straight-chain or branched C1-5 alkyl, C1-5 haloalkyl, or C3-6 cycloalkyl, and R2 represents C1-3 alkyl or C1-3 haloalkyl.Type: GrantFiled: May 10, 2000Date of Patent: August 21, 2001Assignee: LG Chemical Ltd.Inventors: Goon-Ho Joe, Ju-Young Lee, Sang-Who Lee, Jae-Hoon Jeon, Kun-Tai Kim, Hwan-Sung Cheon
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Patent number: 6277790Abstract: Tetrazolinonecarboxamides of formula I wherein Het is oxetan-3-yl, thietan-3-yl, tetrahydrofuran-3-yl, furan-3-yl, tetrahydrothiophen-3-yl, thiophen-3-yl, tetrahydro-2H-pyran-3-yl, tetrahydro-2H-thiopyran-3-yl, tetrahydro-2H-pyran-4-yl or tetrahydro-2H-thiopyran-4-yl, in each case with or without substitution; R1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, phenyl, or 3- to 7-membered heterocyclyl; R2 is hydrogen, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, or is optionally substituted cycloalkyl, cycloalkylalkyl, phenyl, phenylalkyl, 3- to 7-membered heterocyclyl, or 3- to 7-membered heterocyclylalkyl, their preparation and herbicidal compositions comprising them.Type: GrantFiled: February 1, 2000Date of Patent: August 21, 2001Assignee: BASF AktiengesellschaftInventors: Cyrill Zagar, Gerhard Hamprecht, Markus Menges, Olaf Menke, Robert Reinhard, Peter Schäfer, Karl-Otto Westphalen, Martina Otten, Helmut Walter
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Patent number: 6274742Abstract: The present invention describes a method of organic synthesis for N-homocysteine thiolactonyl retinamide, a compound that has anticancer and antiatherogenic properties.Type: GrantFiled: April 25, 2000Date of Patent: August 14, 2001Assignee: Baylor UniversityInventors: Michal Kazimir, F. Ray Wilson, II
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Patent number: 6271249Abstract: Novel compounds of Formula 1 are useful to treat disorders responsive to openers of the large conductance calcium-activated potassium channels: wherein “Het” is one of a select group of heterocyclic moieties; Z is independently for each occurrence selected from O or S; Ra, Rb and Rc each are independently selected from hydrogen, halogen, OH, CF3, NO2, or provided Rc is not hydrogen; and when Ra and Rb are hydrogen, Rc may be a heterocyclic moiety selected from the group consisting of imidazol-1-yl, morpholinomethyl, N-methylimidazol-2-yl, and pyridin-2-yl; Rd and Re each are independently selected from hydrogen, halogen, CF3, NO2 or imidazol-1-yl; m, n and p each are independently selected from an integer of 0 or 1; and Rf and Rg each are independently hydrogen; C1-4 alkyl; or Rf and Rg, taken together with the nitrogen atom to which they are attached, is a heterocyclic moiety selected from the group consisting of N-methylpiperazine, morpholine, thiomorpholine,Type: GrantFiled: March 29, 2000Date of Patent: August 7, 2001Assignee: Bristol-Myers Squibb CompanyInventors: Jeffrey L. Romine, Scott W. Martin, Piyasena Hewawasam, Nicholas A. Meanwell, Valentin K. Gribkoff, John E. Starrett, Jr.
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Patent number: 6271388Abstract: An industrial process for preparing an oxazolidin-2-one derivative represented by the following general formula (3) wherein R1, R2, R3 and R4 are hydrogen atom, straight, branched or cyclic alkyl group, straight or branched alkyl group substituted by alkoxy, substituted amino or alkylthio, substituted or unsubstituted aralkyl group, or substituted or unsubstituted aryl group, and R5 is are hydrogen atom, straight, branched or cyclic alkyl group, substituted or unsubstituted aralkyl group, or substituted or unsubstituted aromatic ring, which is characterized in reacting a 1,3-dioxolan-2-one derivative and a carbamate derivative or an urea derivative in the presence of a fluoride salt.Type: GrantFiled: September 8, 2000Date of Patent: August 7, 2001Assignee: Daiso Co., Ltd.Inventors: Keisuke Yaegashi, Yoshiro Furukawa, Hiroshi Yoshimoto
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Patent number: 6271382Abstract: An organic compound having a nitroxide free radial of the formula (2) is prepared by reacting a cyclic secondary amine having a steric hindrance of the formula (1) with a peroxide in the presence of at least 1 part by weight of an organic compound having a cyano group per 1 part by weight of the cyclic secondary amine having the steric hindrance. In the formulae (1) and (2), T is a methylene group, an ethylene group, an oxygen atom or a methyleneoxy group; R is an alkyl group, an aralkyl group, an aryl group, a cycloalkyl group, an alkoxy group, an acyl group an acyloxy group, an amino group, a hydroxyl group or a heterocyclic group; R1, R2, R3 and R4 are the same or different and each an alkyl group or an aryl group, or R1 and R2 and/or R3 and R4 together form a tetramethylene group or a pentamethylene group; and n is an integer of 0 to 6.Type: GrantFiled: August 28, 2000Date of Patent: August 7, 2001Assignee: Koei Chemical Co., Ltd.Inventor: Katsuhiro Iwazaki
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Patent number: 6268515Abstract: A process for preparing a 3-hydroxy-&ggr;-butyrolactone derivative represented by the following formula (1): wherein R is C1-C6 alkyl, 3 to 6-membered cycloalkyl, aralkyl, 2-alkenyl, acyl, &agr;-hydroxyalkyl, alkoxycarbonylalkyl or alkoxycarbonyl, which is characterized in treating 3-hydroxy-&ggr;-butyrolactone with a metal salt of hexamethyldisilazane and then, reacting it with an electrophilic reagent, optionally in the presence of a reaction promoter.Type: GrantFiled: June 23, 2000Date of Patent: July 31, 2001Assignee: Daiso Co., Ltd.Inventors: Kazumasa Hinoue, Yoshiro Furukawa, Shigeo Katsumura, Yoshikazu Takehira
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Patent number: 6265589Abstract: Described is a process for preparing mixtures of mixed-alkylated methylolated 4,5-dihydroxyimidazolidin-2-ones by reaction of methylolated 4,5-dihydroxyimidazolidin-2-one (DMDHEU) with a monohydric C1-5 alcohol and a polyol selected from the group consisting of ethylene glycol, diethylene glycol, 1,2-propylene glycol, 1,3-propylene glycol, 1,2-butylene glycol, 1,3-butylene glycol, 1,4-butylene glycol, glycerol and polyethylene glycols of the formula HO(CH2CH2O)nH where 3≦n≦20, the monohydric C1-5 alcohol and the polyol each being used in an amount of from 0.1 to 2.0 mol equivalents, based on DMDHEU, and the reaction being carried out at temperatures from 20° C. to 70° C. and at a pH of from 1 to 2.5, and the pH being set to a value of from 4 to 8 after the reaction.Type: GrantFiled: June 30, 1999Date of Patent: July 24, 2001Assignee: BASF AktiengesellschaftInventors: Pia Hois, Ferdinand Lippert, Jürgen Reichert
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Patent number: 6258954Abstract: The present invention relates to compounds of formula I provided that R1 and R2 not simultaneously stand for phenyl, the use thereof in, for example, electroluminescent devices and as void detection compounds.Type: GrantFiled: August 22, 2000Date of Patent: July 10, 2001Assignee: Ciba Specialty Chemicals Corp.Inventors: Kazuhiko Kunimoto, Junji Otani, Kunihiko Kodama, Hiroshi Yamamoto, Patrick Verhoustraeten, Sonia Megert, Adalbert Braig
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Patent number: 6248908Abstract: A process for the synthesis of a C-4 methyl carbonate paclitaxel analog from 10-deacetylbaccatin III by the selective reduction of the acetate at the C-4 position of 10-deacetylbaccatin using Red-Al.Type: GrantFiled: August 10, 2000Date of Patent: June 19, 2001Assignee: Bristol-Myers Squibb CompanyInventor: Joydeep Kant
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Patent number: 6248897Abstract: The present invention relates to a novel method for producing a compound of the formula [11] wherein R is an optionally substituted aromatic hydrocarbon group, an optionally substituted alicyclic hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted condensed heterocyclic group, which is useful as a therapeutic agent for diabetes. The method of the present invention is an industrially utilizable method that enables efficient production of the objective compound [11] from &bgr;-methyl L-aspartate via an important intermediate compound [6] wherein R is as defined above, at high yield.Type: GrantFiled: November 29, 1999Date of Patent: June 19, 2001Assignee: Japan Tobacco Inc.Inventors: Koji Ando, Masanobu Suzuki
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Patent number: 6245790Abstract: Azole compounds of the formula: wherein R1 is lower alkyl substituted with carboxy, etc., R2 is hydrogen or lower alkyl, R3 is aryl, etc. R4 is aryl, etc. Q is etc., and X is O, NH or S, and its salt, which are useful as medicament.Type: GrantFiled: March 8, 2000Date of Patent: June 12, 2001Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kouji Hattori, Osamu Okitsu, Naoaki Fujii, Akira Tanaka, Kiyoshi Taniguchi, Satoshi Koyama, Mie Nishio
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Patent number: 6239287Abstract: A process for the preparation of the phosphonium compound of formula (1), which comprises reacting N-phenylpyrrolidinone (II), with pyridinium bromide perbromide, in the presence of a tertiary organic base and a suitable lewis acid and then treating the resultant bromo derivative (III) with the phosphine (IV, R1R2R1P) and the use of compound (I) when so prepared for the preparation of the glycine antagonist.Type: GrantFiled: September 7, 1999Date of Patent: May 29, 2001Assignee: Glaxo Wellcome SpAInventors: Simon Charles Dolan, Paolo Maragni, Alcide Perboni
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Patent number: 6235763Abstract: The invention relates to polycyclc 2-aminodihydrothiazole systems and their physiologically tolerated salts and physiologically functional derivatives. Compounds of the formula I, in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.Type: GrantFiled: February 8, 2000Date of Patent: May 22, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Gerhard Jaehne, Karl Geisen, Hans-Jochen Lang, Martin Bickel
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Patent number: 6235736Abstract: A 3-anilino-2-cycloalkenone derivative of the formula (I): wherein, R1 represents a C1 to C8 alkyl group, which may have a substituent, except for a methyl group, a C3 to C7 cycloalkyl group, a 3-tetrahydrofuryl group, an 2-indanyl group, etc., R2 represents a C1 to C4 alkyl group, R3 represents a hydrogen atom, a C3 to C7 alkyl group, which may have a substituent, a C3 to C7 cycloalkyl group, etc., R4 represents a hydrogen atom, a C1 to C5 alkyl group, which may have a substituent, a halogen atom, etc., R5, R6, R7, and R8 independently represent a hydrogen atom, a C1 to C5 alkyl group, which may have a substituent, etc., X represents —(CR11R12)n—, wherein n is 0 to 2, R11 and R12 independently represent a hydrogen atom, a C1 to C5 alkyl group, which may have a substituent, etc.Type: GrantFiled: March 20, 2000Date of Patent: May 22, 2001Assignee: Nikken Chemicals Co., Ltd.Inventors: Shinji Ina, Kenjirou Yamana, Kyoji Noda, Akane Takahama, Toshihiko Akiyama