Oxy Bonded Directly To A Ring Patents (Class 568/33)
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Patent number: 7189880Abstract: A process for producing 2,4?-dihydroxydiphenylsulfone which comprises separating 4,4?-dihydroxydiphenylsulfone by crystallization from a mixture containing 4,4?-dihydroxydiphenylsulfone, 2,4?-dihydroxydiphenylsulfone, phenolsulfonic acid and phenol which is obtained by dehydration of phenol and sulfuric acid or phenolsulfonic acid to obtain a mixture having a content of 2,4?-dihydroxydiphenylsulfone greater than the content of 4,4?-dihydroxydiphenylsulfone, crystallizing 2,4?-dihydroxydiphenylsulfone by adjusting the composition of the solvent of the obtained mixture so that the ratio of the amounts by weight of phenol to water is 10:90 to 90:10, and separating 2,4?-dihydroxydiphenylsulfone by filtration; and a process as described above in which the filtrate obtained by the filtration is used as the raw material for the hydration.Type: GrantFiled: January 22, 2003Date of Patent: March 13, 2007Assignee: Nicca Chemical Co., Ltd.Inventors: Gou Yoshino, Yuichi Tomoda, Norihiro Taniguchi, Kazuaki Igarashi, Takeo Hasegawa
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Patent number: 7053123Abstract: (E)-Styryl benzylsulfones useful as antiproliferative agents, including, for example, anticancer agents, are provided according to formula I: wherein: R1 is selected from the group consisting of halogen, C1–C6 alkoxy, nitro, phosphonato, amino, sulfamyl, carboxy, acetoxy and dimethylamino (C2–C6 alkoxy); and R2 and R3 are independently selected from the group consisting of halogen, C1–C6 alkoxy, C1–C6 alkyl, nitro, cyano, hydroxyl, phosphonato, amino, sulfamyl, carboxy, acetoxy, and dimethylamino (C2–C6 alkoxy); provided: R1 may not be halogen when R2 and R3 are both halogen; R2 may not be 2-halogen when R3 is 4-halogen; or a pharmaceutically acceptable salt thereof; or formula II: wherein: R4 is selected from the group consisting of C1–C6 alkoxy, phosphonato, amino, sulfamyl, carboxy, acetoxy and dimethylamino (C2–C6 alkoxy); R6 is selected from the group consisting of nitro, hydrogen, phosphonato, amino, sulfamyl, carboxy, acetoxy and dimethylamino (C2–C6 alkoxy); and R7 is selected from the group consistinType: GrantFiled: October 5, 2001Date of Patent: May 30, 2006Assignee: Temple University-of the Commonwealth System of Higher EducationInventors: E. Premkumar Reddy, M. V. Ramana Reddy
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Patent number: 6974886Abstract: The present invention provides a process for producing dihydroxydiphenylsulfone wherein trihydroxytriphenylsulfone and coloring impurities are effectively removed without altering the isomeric composition of dihydroxydiphenylsulfone. In particular, the present invention provides a process for producing dihydroxydiphenylsulfone comprising the steps of dissolveing or suspending in an aqueous solvent crude dihydroxydiphenylsulfone containing trihydroxytriphenylsulfone, adjusting the pH to 5–7, optionally cooling, and separating the crystalline dihydroxydiphenylsulfone thus precipitated.Type: GrantFiled: April 24, 2003Date of Patent: December 13, 2005Assignee: Konishi Chemical Ind. Co., Ltd.Inventors: Fumio Oi, Norio Yanase, Takayuki Kitahara, Nobuyuki Nate
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Patent number: 6965054Abstract: The present invention provides a process for producing a mixture of dihydroxydiphenylsulfone isomers containing 2,4?-dihydroxydiphenylsulfone, the process comprising heating 4,4?-dihydroxydiphenylsulfone or a mixture of dihydroxydiphenylsulfone isomers containing at least 85 wt. % of 4,4?-dihydroxydiphenylsulfone in the presence of phenol and sulfuric or sulfonic acid.Type: GrantFiled: September 26, 2002Date of Patent: November 15, 2005Assignee: Konishi Chemical Ind. Co., Ltd.Inventors: Fumio Oi, Norio Yanase, Masamichi Yamamoto
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Patent number: 6914074Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10, are as defined in the specification, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: December 11, 2002Date of Patent: July 5, 2005Assignee: WyethInventors: Richard E. Mewshaw, Richard J. Edsall, Cuijian Yang, Heather A. Harris, James C. Keith, Jr., Leo M. Albert, Eric S. Manas
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Publication number: 20040261190Abstract: Hydrazono-malonitrile derivatives of the formula (I) in which R1, R2, R3, R3′ and R4 have the meanings given in claim 1 act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDS.Type: ApplicationFiled: May 4, 2004Publication date: December 30, 2004Inventors: Hans-Michael Eggenweiler, Michael Wolf, Norbert Beier, Pierre Schelling, Thomas Ehring
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Publication number: 20040254400Abstract: The present invention provides a process for producing a mixture of dihydroxydiphenylsulfone isomers containing 2,4′-dihydroxydiphenylsulfone, the process comprising heating 4,4′-dihydroxydiphenylsulfone or a mixture of dihydroxydiphenylsulfone isomers containing at least 85 wt. % of 4,4′-dihydroxydiphenylsulfone in the presence of phenol and sulfuric or sulfonic acid.Type: ApplicationFiled: March 25, 2004Publication date: December 16, 2004Inventors: Fumio Oi, Norio Yanase, Masamichi Yamamoto
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Patent number: 6831201Abstract: The present invention is to provide methods for producing highly pure 4,4′-dihydroxydiphenyl sulfone monoethers advantageously in industrial production. In a process for producing a compound represented by Formula (1) (wherein, R1 and R2 are each independently halogen, alkyl having 1 to 8 carbons or alkenyl having 2 to 8 carbons; m and n are each independently 0 or an integer of 1 to 4; and R3 is alkyl having 1 to 8 carbons, alkenyl having 2 to 8 carbons, cycloalkyl having 3 to 8 carbons or optionally substituted aralkyl), (1) a pH adjustment is carried out twice or more in the purification process, (2) an excessive amount of alkyl halide used is removed, (3) a solvent, such as water, containing 0.05 ppm or less of iron components is used, (4) tanks with corrosion-resistant layers over the inner walls are used, (6) a chelating agent is added, and (7) a means of drying with mechanical stir is applied.Type: GrantFiled: September 20, 2002Date of Patent: December 14, 2004Assignee: Nippon Soda Co., Ltd.Inventors: Kiyoshi Katsuura, Tomoya Hidaka, Yutaka Takashina, Yasuo Ohnuki
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Publication number: 20040242935Abstract: The present invention provides a process for producing a mixture of 4,4′- and 2,4′-dihydroxydiphenylsulfones comprising heating trihydroxytriphenyldisulfone or a mixture of dihydroxydiphenylsulfone isomers containing trihydroxytriphenyldisulfone in the presence of phenol and an acid catalyst.Type: ApplicationFiled: March 25, 2004Publication date: December 2, 2004Inventors: Fumio Oi, Norio Yanase, Hiroyuki Yamamoto
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Publication number: 20040192971Abstract: Disclosed herein is a process for preparing 4-(2-sulfoethylcyclohexane)-1,2 diol, at ambient condition and in the presence of a buffer and an initiator, from vinylcyclohexane-1,2-diolType: ApplicationFiled: March 24, 2003Publication date: September 30, 2004Inventors: Yanhui Sun, Shaorong Chen
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Publication number: 20040092749Abstract: Polysubstituted indan-1-ol compounds, methods for their preparation; and methods for their use are disclosed herein.Type: ApplicationFiled: October 27, 2003Publication date: May 13, 2004Applicant: Aventis Pharma Deutschland GmBHInventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
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Patent number: 6700020Abstract: A semicontinuous process is provided for the preparation of 4,4′-dihydroxydiphenyl sulfone, comprising the following steps: (a) reaction of phenol with a sulfonating agent, (b) suspension of the resulting crude product in water heated to at least 40° C., which is free of inert organic solvents and can contain residual amounts of unreacted phenol, and filtration of the product, and (c) recycling of the resulting educt-containing and/or product-containing waste streams into the preparative process, wherein, in carrying out step (b), the crude product and water are used in a weight ratio of 85:15 to 55:45.Type: GrantFiled: October 10, 2002Date of Patent: March 2, 2004Assignee: BASF AktiengesellschaftInventors: Gunther Pabst, Jürgen Kast
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Publication number: 20040030191Abstract: A process for producing 4-isopropoxy-4′-hydroxydiphenyl sulfone useful as the developer for leuco dyes to be used in thermosensible papers, which is excellent in productivity, economical efficiency and safety and permits the production of the compounds from constantly available raw materials. This process is improved in productivity and economical efficiency as compared with those of the prior art both by shortening the production time by the use of an isopropyl iodide, which is more reactive than isopropyl bromide which have been used in the prior art.Type: ApplicationFiled: May 28, 2003Publication date: February 12, 2004Inventors: Syuichiro Sanpei, Masayuki Hanzawa, Yasuyuki Suzuki, Minoru Kaeriyama, Tomoya Hidaka, Toru Kawabe
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Publication number: 20040004207Abstract: The present invention provides a difluoromethyl ether derivative which shows various suitable physical properties as a liquid crystal compound, a liquid crystal composition comprising the compound and a liquid crystal display element containing the composition, and also provides a simple and efficient process for producing the difluoromethyl ether derivative.Type: ApplicationFiled: June 18, 2003Publication date: January 8, 2004Inventors: Tomoyuki Kondo, Kouki Sagou, Shuichi Matsui, Hiroyuki Takeuchi, Yasuhiro Kubo, Etsuo Nakagawa
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Patent number: 6667345Abstract: Derivatives of C2-substituted indan-1-ol compounds of the formula I: its physiologically acceptable salts, and its physiologically functional derivatives for the prophylaxis or treatment of obesity are disclosed herein. Compositions comprising the same, methods for preparing the instant compounds, and methods for reducing weight in mammals and for the prophylaxis or treatment of obesity are also described.Type: GrantFiled: August 29, 2002Date of Patent: December 23, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
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Patent number: 6657086Abstract: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives. Compounds of embodiments of the invention may include compounds of formula I in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds are suitable, for example, for use as anorectics.Type: GrantFiled: August 30, 2002Date of Patent: December 2, 2003Assignee: Aventis Pharma Deutschland GmbHInventors: Gerhard Jaehne, Volker Krone, Martin Bickel, Matthias Gossel
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Patent number: 6630509Abstract: The present invention relates to certain phenalkyloxy-phenyl derivatives of formula (I) and analogs, to a process for preparing such compounds, which compounds have utility in treating clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: June 3, 2002Date of Patent: October 7, 2003Assignee: AstraZeneca ABInventors: Jonas Fägerhag, Lanna Li, Eva-Lotte Lindstedt Alstermark
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Publication number: 20030149308Abstract: The invention relates to a semi-continuous method for producing 4,4-dihydroxydiphenylsulfone, comprising the following steps: (a) reacting phenol with a sulfonating agent; (b) suspending the resulting crude product in hot water which is at least 40° C. and which is free from inert organic solvents and can contain residual amounts of unreacted phenol, and filtering off the product; and (c) returning the resulting waste streams containing the educt and/or product to the production process. Step (b) is carried out using the crude product and water in a weight ratio of 85:15 to 55.45.Type: ApplicationFiled: October 10, 2002Publication date: August 7, 2003Inventors: Gunther Pabst, Jurgen Kast
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Patent number: 6590126Abstract: A process for producing compounds of general formula (II) useful as the developer for leuco dyes to be used in thermosensible papers, which is excellent in productivity, economical efficiency and safety and permits the production of the compounds from constantly available raw materials. This process is improved in productivity, economical efficiency and safety as compared with those of the prior art both by shortening the production time by the use of, e.g., an alkyl iodide, RI, which is more reactive than alkyl bromides which have been used in the prior art, and by attaining the complete recovery and reuse of iodine by incorporating into the process the iodine recovery step of recovering iodine from the manufacturing wastewater and reacting this iodine with an alcohol to thereby self-produce an alkyl iodide.Type: GrantFiled: September 21, 2001Date of Patent: July 8, 2003Assignee: Nippon Soda Co., Ltd.Inventors: Syuichiro Sanpei, Masayuki Hanzawa, Yasuyuki Suzuki, Minoru Kaeriyama, Tomoya Hidaka, Toru Kawabe
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Patent number: 6583161Abstract: The invention provides compounds, compositions and methods relating to novel aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: December 12, 2000Date of Patent: June 24, 2003Assignee: Tularik Inc.Inventor: Julio C. Medina
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Patent number: 6583321Abstract: The present invention relates to a novel 4′-methanesulfonyl-biphenyl derivative having a structure of formula 1 and its pharmaceutically acceptable salts as a highly selective cyclooxygenase-2 inhibitor. <Formula 1> Wherein, R1 and R2 are defined in this specification respectively.Type: GrantFiled: October 3, 2002Date of Patent: June 24, 2003Assignee: Cheil Jedang CorporationInventors: Il Hwan Cho, Jee Woong Lim, Ji Young Noh, Jong Hoon Kim, Sang Wook Park, Hyung Chul Ryu, Je Hak Kim, Hyung Ok Chun, So Young Wang, Eun Young Lee
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Publication number: 20030105078Abstract: The invention relates to novel diphenyl derivatives, to processes for their preparation and to their use in medicaments.Type: ApplicationFiled: February 26, 2002Publication date: June 5, 2003Inventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Christiane Faeste, Hilmar Bischoff, Axel Kretschmer, Verena Vohringer, Peter Ellinghaus
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Publication number: 20030105095Abstract: The present invention relates to a novel 4′-methanesulfonyl-biphenyl derivative having a structure of formula 1 and its pharmaceutically acceptable salts as a highly selective cyclooxygenase-2 inhibitor.Type: ApplicationFiled: October 3, 2002Publication date: June 5, 2003Applicant: CHEIL JEDANG CorporationInventors: Il Hwan Cho, Jee Woong Lim, Ji Young Noh, Jong Hoon Kim, Sang Wook Park, Hyung Chul Ryu, Je Hak Kim, Hyung Ok Chun, So Young Wang, Eun Young Lee
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Patent number: 6545184Abstract: The present invention provides a convergent method for the synthesis of ubiquinones and ubiquinone analogues. Also provided are precursors of ubiquinones and their analogues that are useful in the methods of the invention.Type: GrantFiled: August 15, 2000Date of Patent: April 8, 2003Assignee: The Regents of the University of CaliforniaInventor: Bruce H. Lipshutz
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Publication number: 20030065229Abstract: Disclosed are an efficient, safe process for producing artepillin C and derivatives thereof by an organic synthesis. The process comprises a step of reacting a phenol derivative with an acrylate or acrylic acid.Type: ApplicationFiled: November 28, 2001Publication date: April 3, 2003Inventors: Hitoshi Hori, Yoshinori Nakagawa
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Patent number: 6486354Abstract: Embodiments of the present invention generally relate to carrying out organic chemistry on solid supports comprising derivatised functionalities, methods for synthesizing said supports, methods for synthesizing compounds comprising amine groups or N-containing heterocycles using said solid supports, intermediate compounds linked to said supports and uses thereof.Type: GrantFiled: April 17, 2000Date of Patent: November 26, 2002Assignee: Akzo Nobel N.V.Inventors: David Gani, Friedrich Erich Karl Kroll, Michael John Plater, John Richard Morphy, David Rees
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Patent number: 6399833Abstract: A process for producing a purified aryl vinyl sulfone solution, characterized in that an aryl vinyl sulfone is crystallized from an organic solvent solution of a crude aryl vinyl sulfone to give a crystallization mixture, and a wet cake of the aryl vinyl sulfone obtained by the separation of the solution from the said mixture is dissolved in a solution-forming solvent selected from ethers of 4 to 8 carbon atoms, aromatic hydrocarbons of 6 to 10 carbon atoms, halogenated hydrocarbons of 1 to 6 carbon atoms, ketones of 3 to 8 carbon atoms, esters of 3 to 6 carbon atoms, and nitrites of 2 to 6 carbon atoms.Type: GrantFiled: July 31, 2000Date of Patent: June 4, 2002Assignee: Sumitomo Chemical Company, LimitedInventors: Akio Kurihara, Isao Kurimoto, Naoyuki Takano
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Patent number: 6384273Abstract: The invention concerns a method for orthometalation of a carbocyclic aromatic derivative bearing at least an electron donor group, characterised in that it consists in reacting said carbocyclic aromatic derivative with an efficient amount of at least one alkaline metal in the presence of a compound of formula (I): RX, wherein: R represents a hydrocarbon radical having 1 to 20 carbon atoms which can be a saturated or unsaturated, linear or branched, acyclic aliphatic radical; a saturated or unsaturated, monocyclic or polycyclic cycloaliphatic radical; a saturated or unsaturated, linear or branched aliphatic radical bearing a cyclic substituent; and X represents a bromine or chlorine atom.Type: GrantFiled: January 24, 2001Date of Patent: May 7, 2002Assignee: Rhodia ChimieInventors: Virginie Pevere, Jean Roger Desmurs, Charles Mioskowski, Alain Wagner, Arnaud Gissot
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Method for making unsymmetrically substituted fluorenyl compounds for nonlinear optical applications
Patent number: 6379590Abstract: A new method for producing unsymmetrically substituted fluorenyl compounds, one step of which is the preparation of 2,7-disubstituted fluoren-9-one derivatives via the nucleophilic substitution of a compound of the formula D wherein A′ is selected from the group consisting of —Br, —Cl, —F, —NO2, and —CN; A is selected from the group consisting of —NO2, —CN, —CO2R, —C(O)R, —SO2R, —SO2RF, —C(CN)═C(CN)2 and —CH═C(CN)2; RF is —CpF2p+1, p=from about 0 to about 10; R is an straight, branched or cyclic aliphatic alkyl group having about 1 to 10 carbon atoms, or an aromatic group such as phenyl or naphthyl; and is a carbonyl or a protected carbonyl such as a ketal or thio-ketal such as wherein R′ is —CrH2r+1; R″ is —(CH2)r—; and r is independently 2 or 3, with a nucleophilic reagent in the presence of an aprotic solventType: GrantFiled: December 2, 1994Date of Patent: April 30, 2002Assignee: AlliedSignal Inc.Inventors: Chengjiu Wu, Jianhui Shan -
Patent number: 6326369Abstract: A compound of the formula: wherein R1 and R2 each represents a lower alkyl, or R1 and R2 may be bonded together to form a ring; X represents a spacer of which the number of atoms constituting the principal chain is 1 to 15; Y represents an acyl, or a hydroxy, an amino or an aromatic group, each of which may be substituted; and ring A represents a 5- to 8-membered ring which may be further substituted apart from —X—Y, or a salt thereof is useful as a pharmaceutical composition for preventing or treating disease related to mitochondrial dysfunction.Type: GrantFiled: July 6, 1999Date of Patent: December 4, 2001Assignee: Takeda Chemicals Industries, Ltd.Inventors: Kaneyoshi Kato, Taiichi Ohra, Masaomi Miyamoto
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Patent number: 6303562Abstract: The present invention relates to certain alkylated 2-(2-hydroxyphenyl) benzenesulfinic acid and 2-(2-hydroxyphenyl)benzenesulfonic acid compounds and compositions which consist essentially of 2-(2-hydroxyphenyl) benzenesulfinic acid, 2-(2-hydroxyphenyl)benzenesulfonic acid and/or substituted derivatives thereof. The compositions of the invention are useful as hydrotropes and are also of use as, or as starting materials for, surfactants, and as starting materials for the synthesis of other useful chemicals such as, polymers and resins, solvents, adhesives and biocides.Type: GrantFiled: June 20, 2000Date of Patent: October 16, 2001Assignee: Enchira Biotechnology CorporationInventors: Elaine A. Lange, Qun Lin
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Patent number: 6303630Abstract: In accordance with the present invention, there is now provided novel anti-HIV compounds of the formulae selected from the group consisting of: wherein R1 is hydrogen or C1-C4 alkyl; R2 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy or halogen; R3 is hydrogen, hydroxy, C1-C4 alkyl, C1-C4 alkoxy or halogen; R4 is hydrogen or halogen, R5 is hydrogen; C1-C4 alkoxy, nitro, halogen or haloalkyl; R6 is hydrogen or nitro; R7 is hydrogen or C1-C4 alkyl, C1-C4 alkoxy, nitro or halogen; R8 is hydrogen, hydroxy, C1-C4 alkyl, C1-C4 alkoxy or halogen; R9 is hydrogen or nitro; R10 is hydrogen or halogen; R11 is hydrogen, C1-C4 amine; R12 is hydrogen, C1-C4 alkyl or halogen; R13 is hydrogen, C1-C4 amine; R14 is hydrogen or halogen; R15 is hydrogen, C1-C4 alkoxy, C1-C4 haloalkyl, nitro, or halogen; R16 is hydrogen or nitro; R17 is hydrogen, C1-C4 alkyl, C1-C4 alkoxy, nitro or halogen; R18 is hydrogen, C1-C4 alkoxy, hydroxy, or halogen; R19 is hydrogen or nitro; and R20 is hydrogen or halogen, or a phaType: GrantFiled: April 11, 2000Date of Patent: October 16, 2001Assignee: University of the Sciences in PhiladelphiaInventor: Murray Zanger
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Patent number: 6297402Abstract: There is provided a ketosulfone derivative represented by the formula (I): wherein Ar represents an aryl group which may be substituted, and R1′ and R2′ represent a hydrogen atom or a protective group of a hydroxyl group and processes for producing the same.Type: GrantFiled: August 22, 2000Date of Patent: October 2, 2001Assignee: Sumitomo Chemical Company, LimitedInventors: Toshiya Takahashi, Shinzo Seko
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Patent number: 6232503Abstract: The present invention provides compounds having the formula wherein R1, R2, R3, R4, and R5 are independently hydrogen, chlorine, bromine, fluorine, iodine, substituted or unsubstituted linear or branched C1-C3 alkoxy, substituted or unsubstituted linear or branched C1-C3 thioalkoxy, substituted or unsubstituted linear or branched C1-C8, alkyl, hydroxyl, thiol, —CN, —CF3, —OCF3, —NO2, acetyl, or —NR6R7; R6 and R7 are independently hydrogen, methyl, or ethyl; and X is iodine or bromine. Another embodiment of the invention includes specific ethynyl benzene sulfone derivatives. The alkynyl aryl sulfones of the present invention are useful as biocides, including, but not limited to, bactericides, fungicides, and preservatives. Also, a method of preparing the halogenated alkynyl aryl sulfones of formula I is provided.Type: GrantFiled: September 21, 1999Date of Patent: May 15, 2001Assignee: Lonza Inc.Inventor: Peter C. Nirchio
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Patent number: 6197993Abstract: The naphthyloxyacetic acid derivatives of the formula (I) wherein A is H, -(alkylene)COOR1, -(alkylene)CONR2R3, -(alkylene)OH, -(alkylene)tetrazole, -(alkylene)CN; E is single bond or alkylene; G is —S—, —SO—, —SO2—, —O— or —NR4—; L is alkylene, —(CH2)m—CH═CH—(CH2)n— or —(CH2)x—CH(OH)— (CH2)y—; M is phenyl, phenyl(thio, oxy, amino), diphenylmethyl, diphenylmethyl(thio, oxy, amino), and pharmaceutical composition comprising them as an active ingradient. The compounds of the formula (I) can combine PGE2 receptor and exhibit the activity to antagonize or agonize for PGE2 receptor. Therefore, they are useful as anti-hyperlipemia, for the prevention of abortion, for analgesics, as antidiarrheals, sleep inducer, diuretic, anti-diabetes, abortient, cathartics, antiulcer, anti-gastritis or antihypertensive etc.Type: GrantFiled: November 16, 1999Date of Patent: March 6, 2001Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Yuuki Nagao, Kazuhiko Torisu, Nobuyuki Hamanaka
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Patent number: 6162445Abstract: Novel pharmaceutically/cosmetically-active polyaromatic propynyl compounds have the structural formula (I): in which X is one of the radicals: ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.Type: GrantFiled: October 6, 1997Date of Patent: December 19, 2000Assignee: Centre International de Recherches Dermatologiques GaldermaInventor: Jean-Michel Bernardon
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Patent number: 6130334Abstract: The invention encompasses a process for making compounds of Formula I useful in the treatment of cyclooxygenase-2 mediated diseases.Type: GrantFiled: April 15, 1998Date of Patent: October 10, 2000Assignee: Merck & Co., Inc.Inventors: Philip J. Pye, Ashok Maliakal, Kai Rossen, Ralph P. Volante, Jess Sager
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Patent number: 6118016Abstract: A process for preparing phenoxyphenylsulfonyl halides, which are useful intermediates for the preparation of matrix metalloproteinase inhibitors.Type: GrantFiled: April 7, 1999Date of Patent: September 12, 2000Assignee: Pfizer Inc.Inventor: Joel M. Hawkins
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Patent number: 6114282Abstract: A heat-sensitive recording material in which a heat-sensitive color-developing layer comprising, as the main components, a usually colorless or light-colored color former and a developer capable of developing the color former upon heating on a support, characterized by comprising, as the developer, crystals of 3,3'-diallyl-4,4'-dihydroxy-diphenyl sulfone which have DSC (Te) of at least 149.degree. C. and which are of a crystal form characterized by an X-ray diffraction pattern having peaks at least at diffraction angles (2.theta.) [.degree.] of 7.2 and 22.0, obtained by an X-ray powder diffractometry using Cu--K.alpha. rays. This heat-sensitive recording material is high in sensitivity, little in Discoloration of the ground in heat and moisture and excellent in image durability.Type: GrantFiled: January 11, 1999Date of Patent: September 5, 2000Assignee: Nippon Kayaku Kabushiki KaishaInventors: Masao Onishi, Masaaki Saito, Hirofumi Iwamoto
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Patent number: 6046363Abstract: The present invention provides a method of making 4-hydroxy-4'-benzyloxydiphenyl sulfone. The manufacturing method of the present invention is characterized in that an aqueous solvent containing an appropriate amount of a lower alcohol is used as a reaction solvent between 4,4'-dihydroxyphenyl sulfone and a benzyl halide.Type: GrantFiled: May 20, 1998Date of Patent: April 4, 2000Assignee: Nicca Chemical Co., Ltd.Inventor: Yuichi Tomoda
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Patent number: 6040470Abstract: There is provided a developer composition including at least one of sulfonyl compounds represented by formula (1) and at least one of sulfonyl compounds represented by formula 2: ##STR1## wherein X is H or lower alkyl, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 which may be the same or different, present H, halogen or lower alkyl and Y represents alkyl, benzenesulfonyl, benzoyl et al, A thermalsensitive recording medium having the above developer is of high sensitivity, less surface-blushing with lapse of time and is excellent in storage stability of a recorded image, particularly in heat resistance, humidity resistance and anti-plasticizer.Type: GrantFiled: September 10, 1998Date of Patent: March 21, 2000Assignee: Sanko Kaihatsu Kagaku KenkyushoInventors: Shigeru Oda, Eiji Kawabata
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Patent number: 6037308Abstract: Diphenyl sulfone crosslinking type compounds of general formula (1) and a recording material containing at least one of them. This recording material is excellent in the storage stability of colored images.Type: GrantFiled: April 30, 1998Date of Patent: March 14, 2000Assignee: Nippon Soda Co., Ltd.Inventors: Takehiro Sato, Hiroshi Fujii, Shinichi Sato, Izuo Aoki
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Patent number: 5993700Abstract: This invention provides an aggregate of a compound capable of forming helical structures such that the aggregate is capable of achieving a specific rotation of at least 100,000.degree. for plane polarized light having a wavelength of 589 nm.Type: GrantFiled: July 18, 1997Date of Patent: November 30, 1999Assignee: The Trustees of Columbia University in the City of New YorkInventors: Thomas J. Katz, Colin P. Nuckolls
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Patent number: 5990105Abstract: The present invention relates to novel compounds of the general formula ##STR1## wherein R.sup.1 is hydrogen;R.sup.2 is hydrogen, trifluoromethyl or lower alkyl;R.sup.3 is hydrogen or amino; orR.sup.1 and R.sup.2 or R.sup.3 and R.sup.2 taken together are --CH.dbd.CH--CH.dbd.CH--;Z is pyrimidin-4-yl, pyridin-4-yl, pyridin-2-yl or phenyl;R.sup.4, R.sup.5 are each independently hydrogen, lower alkyl, trifluoromethyl, halogen, lower alkoxy, nitrilo, amino, lower alkyl-amino, di-lower alkyl-amino, piperazinyl, morpholinyl, pyrrolidinyl, vinyl, C.sub.3 -C.sub.6 cycloalkyl, C.sub.3 -C.sub.6 cycloalkenyl, t-buthylethinyl, hydroxyalkylethinyl, phenylethinyl, naphthyl, thiophenyl, or phenyl, which may be substituted by halogen, lower alkoxy, lower alkyl, trifluoromethyl or nitro, or a group --NH(CH.sub.2).sub.n NR.sup.6 R.sup.7, --N(CH.sub.3)(CH.sub.2).sub.n NR.sup.6 R.sup.7, --NH(CH.sub.2).sub.n -morpholin-4-yl or --NH(CH.sub.2).sub.n OH;n is 2-4R.sup.6 and R.sup.Type: GrantFiled: January 15, 1999Date of Patent: November 23, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bos, Walter Hunkeler, Claus Riemer
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Patent number: 5958983Abstract: The present invention relates to polyaromatic compounds having useful antiviral activity against viruses of the herpes family, to a composition containing them, and to a method of using them for the treatment of herpes viruses infections.Type: GrantFiled: April 1, 1998Date of Patent: September 28, 1999Assignee: Pharmacia & Upjohn CompanyInventors: Michael R. Barbachyn, Fred L. Homa, Antonio Monge, Esteban Santiago, Juan J. Martinez-Irujo, Maria Font
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Patent number: 5925788Abstract: 2-Trifluoromethoxy-benzenesulphonamide, of the formula (I), ##STR1## which can be used as intermediate for the preparation of certain herbicidally active compounds is obtained in very high yield and high purity by a process in which halogenated trifluoromethoxy-benzenesulphonamides of the general formula (II) ##STR2## in which X.sup.1 represents halogen and X.sup.2 represents hydrogen or halogenare reacted with hydrogen in the presence of a catalyst and in the presence of a diluent and, if appropriate, in the presence of an acid acceptor at temperatures between 0.degree. C. and 200.degree. C. ("dehalogenated"), the resulting compound of the formula (I) is isolated in the customary manner in the event that "X.sup.2 =halogen" and converted into a pure, crystalline product by treating it with a protic polar organic liquid and isolated by removing the liquid component by means of filtration with suction in the event that "X.sup.2 =H".Type: GrantFiled: May 14, 1998Date of Patent: July 20, 1999Assignee: Bayer AktiengesellschaftInventors: Reinhard Lantzsch, Albrecht Marhold, Ernst Kysela
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Patent number: 5843999Abstract: A series of new azulene derivatives are disclosed, which are represented by the following formula; ##STR1## wherein: R.sub.1 is hydrogen atom, lower alkoxycarbonyl group, carboxy group, halogen atom, lower alkyl group, phenyl group or lower alkanoyl group; R.sub.2, R.sub.3 and R.sub.4 are hydrogen atom, lower alkyl group, lower alkoxy group or halogen atom; X is lower alkyl group or amino group.The compounds of the present invention are useful for treatment of inflammation.Type: GrantFiled: December 2, 1997Date of Patent: December 1, 1998Assignee: Kotobuki Seiyaku Co., Ltd.Inventors: Tsuyoshi Tomiyama, Akira Tomiyama, Masayuki Yokota, Satoko Uchibori
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Patent number: 5807899Abstract: This invention describes the new triphenylethylenes of general formula I ##STR1## in which n means an integer from 1 to 10,R' means a sulfur-containing organic radical,R" means a hydrogen atom, an iodine atom or a hydroxy groups,E means a hydrogen atom,G means a hydrogen atom orE and G together mean a methylene bridge.The new compounds have strong antiestrogenic properties and are suitable for the production of pharmaceutical agents, for example for treating breast cancer.Type: GrantFiled: July 5, 1996Date of Patent: September 15, 1998Assignee: Schering AktiengesellschaftInventors: Rolf Bohlmann, Joseph Heindl, Hermann Kunzer, Yukishige Nishino, Karsten Parczyk, Martin Schneider
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Patent number: 5801288Abstract: The present invention is directed to recording materials characterized in that the recording materials comprise at least one of diphenyl sulfone derivatives represented by the following general formula (I); ##STR1## wherein Y represents a linear or branched (un)-saturated C.sub.1 -C.sub.12 hydrocarbon group, a C.sub.1 -C.sub.8 hydrocarbon group having an ether linkage, or a group represented by a general formula; ##STR2## wherein R represents methylene or ethylene; R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent each independently lower alkyl or lower alkenyl; m represents 0 or an integer of 1 or 2,; and n, p, q and r represent each independently 0 or an integer of 1 to 4, provided when n, p, q and r are each 2 or above, the substituents represented by R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be each different from one another.Type: GrantFiled: November 26, 1996Date of Patent: September 1, 1998Assignee: Nippon Soda Co., Ltd.Inventors: Hiroshi Fujii, Ryuichi Kaneko, Shinichi Satoh
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Patent number: 5767318Abstract: A process for producing a high purity 2,4'-dihydroxydiphenylsulfone (2,4'-isomer) comprising separating 2,4'-isomer from 4,4'-dihydroxydiphenylsulfone (4,4'-isomer) by adding a hydroxide of an alkali metal in an amount which is the total of an amount by mol 1.6 to 2.2 times as great as the amount by mol of 2,4'-isomer and an amount by mol 0.8 to 1.2 times as great as the amount by mol of 4,4'-isomer to a solution of a mixture of 2,4'-isomer and 4,4'-isomer containing 15% by weight or more of 2,4'-isomer in water, to allow 2,4'-isomer to remain dissolved in water in the form of a dialkali metal salt thereof and 4,4'-isomer to be precipitated from the solution in the form of a monoalkali metal salt thereof. A carbonate of an alkali metal may also be used. In order to accelerate the operation, an excess amount of the alkali may be added, which is subsequently neutralized. A high purity 2,4'-isomer having a purity of 95 to 99.Type: GrantFiled: January 17, 1996Date of Patent: June 16, 1998Assignee: Nicca Chemical Co., Ltd.Inventors: Masaaki Hosoda, Masahiro Makino