Acyclic Chalcogen Bonded Directly To The Hetero Ring Patents (Class 549/466)
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Publication number: 20110118486Abstract: The invention relates to the use of monoliths as particle filters for limiting the deactivation of catalysts during catalytic reactions in multi-tubular reactors. The invention is particularly well-suited for catalytic oxidation reactions in the gaseous phase. The invention also relates to multi-tubular reactors including monoliths as particle filters.Type: ApplicationFiled: July 23, 2008Publication date: May 19, 2011Inventor: Jean-Luc Dubois
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Patent number: 7902385Abstract: Novel ester compounds having formulae (1) to (4) wherein A1 is a polymerizable functional group having a carbon-carbon double bond, A2 is oxygen, methylene or ethylene, R1 is a monovalent hydrocarbon group, R2 is H or a monovalent hydrocarbon group, any pair of R1 and/or R2 may form an aliphatic hydrocarbon ring, R3 is a monovalent hydrocarbon group, and n is 0 to 6 are polymerizable into polymers. Resist compositions comprising the polymers as a base resin are thermally stable and sensitive to high-energy radiation, have excellent sensitivity and resolution, and lend themselves to micropatterning with electron beam or deep-UV.Type: GrantFiled: July 5, 2007Date of Patent: March 8, 2011Assignee: Shin-Etsu Chemical Co., Ltd.Inventors: Masaki Ohashi, Takeshi Kinsho, Takeru Watanabe
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Publication number: 20110053974Abstract: To find a therapeutic agent and/or a preventive agent for diabetes mellitus or the like having excellent activity and safety. A compound represented by the following general formula (I), or a pharmacologically acceptable salt thereof. In the formula, X represents ?C(R5)- or ?N—; Y represents —O— or —NH—; L represents a bond or a substitutable C1-C3 alkylene group; M represents a substitutable C3-C10 cycloalkyl group, a substitutable C6-C10 aryl group, or a substitutable heterocyclic group; R1 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C6 haloalkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group, a C1-C6 aliphatic acyl group, a C1-C6 alkoxy C1-C6 alkyl group, or a C6-C10 aryl group; and R2, R3, R4, and R5 may be the same or different and each represent a hydrogen atom, a halogen atom, a C1-C3 alkyl group, a C1-C3 haloalkyl group, a C1-C3 alkoxy group, or a nitro group.Type: ApplicationFiled: September 29, 2010Publication date: March 3, 2011Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Narihiro TODA, Masao YOSHIDA, Rieko TAKANO, Masahiro INOUE, Takeshi HONDA, Koji MATSUMOTO, Ryutaro NAKASHIMA
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Publication number: 20100331370Abstract: Isobenzofuran analogs of sclerophytin A are prepared in a highly concise fashion via an aldol-cycloaldol sequence. The analogs exhibit IC50's as low as 1 ?M in growth inhibitory studies against KB3 cells using an MTT assay. Preferred analogs have one of the following structural formulas, where R is hydrogen or a substituted or unsubstituted lower alkyl group and Ar is a substituted or unsubstituted aryl group.Type: ApplicationFiled: June 30, 2010Publication date: December 30, 2010Inventor: Matthias C. McIntosh
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Publication number: 20100297540Abstract: Compounds of the Formula (I), wherein L1, L?1, L?1, L2, L?2, L?2, L3, L?3, L?3, L4, L?4 and L?4 for example are hydrogen or COT; R, R? and R? for example are hydrogen, C6-C12aryl or C3-C20heteroaryl; X, X? and X? for example are O, S, single bond, NRa or NCORa, T is for example hydrogen, C1-C20alkyl, C3-C12cycloalkyl, C2-C20alkenyl, C5-C12cycloalkenyl, C7-C18cycloalkylenaryl, C5-C18cycloalkylenheteroaryl, C6-C14aryl, providedthat at least one of R, R? or R? is unsubstituted or substituted C3-C20heteroaryl; and Y is an inorganic or organic anion; are suitable as photolatent acid generators.Type: ApplicationFiled: September 22, 2008Publication date: November 25, 2010Applicant: BASF SEInventors: Pascal Hayoz, Hitoshi Yamato, Toshikage Asakura
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Publication number: 20100267768Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.Type: ApplicationFiled: March 19, 2010Publication date: October 21, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: John DeMattei, Adam R. Looker, Bobbianna Neubert-Langille, Martin Trudeau, Stefanie Roeper, Michael P. Ryan, Dahrika Milfred Lao Yap, Brian R. Krueger, Peter D.J. Grootenhuis, Fredrick F. van Goor, Martyn C. Botfield, Gregor Zlokarnik
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Publication number: 20100267822Abstract: The invention relates to aurones and extracts comprising them useful in the prophylactic and/or therapeutic treatment of an animal (including a human) with an estrogen receptor (ER) related disease or condition of the animal or human body, as well as methods, uses and other inventions related thereto.Type: ApplicationFiled: March 29, 2010Publication date: October 21, 2010Inventors: Annie George D/O V.K. George, Bärbel Köpcke, Ernst Roemer, Jens Bitzer, Joachim Hans, Joerg Gruenwald, Matthias Gehling, Philipp Wabnitz, Tengku Shahrir bin Tengku Adnan, Torsten Grothe
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Publication number: 20100267823Abstract: The invention relates to aurones and extracts comprising them useful in the prophylactic and/or therapeutic treatment of an animal (including a human) with a phosphodiesterase (PDE) dependent disease or condition of the central nervous system, as well as methods, uses and other inventions related thereto.Type: ApplicationFiled: March 29, 2010Publication date: October 21, 2010Inventors: Annie George D/O V.K. George, Bärbel Köpcke, Ernst Roemer, Jens Bitzer, Joerg Gruenwald, Matthias Gehling, Philipp Wabnitz, Tengku Shahrir bin Tengku Adnan, Torsten Grothe
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Publication number: 20100190831Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.Type: ApplicationFiled: December 17, 2009Publication date: July 29, 2010Inventors: Dong Fang Shi, Jiangao Song, Jingyuan Ma, Aaron Novack, Phuongly Pham, Imad Fayek Nashashibi, Christopher J. Rabbat, Xin Chen
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Publication number: 20100152416Abstract: Disclosed herein is a method for producing a purified 2-aryl-3,3-bis(4-hydroxyaryl) phthalimidine of formula (I) wherein R1 is hydrogen or a C1-25 hydrocarbyl group and R2 is a hydrogen, a C1-25 hydrocarbyl group, or a halogen, and wherein the method comprises dissolving a crude phthalimidine compound in an aqueous base solution; precipitating the dissolved, crude phthalimidine compound from the aqueous base solution by adding an acid in an amount effective to lower the pH of the solution to 9.0 to 12.0, to provide a semicrude phthalimidine compound; and isolating the semicrude phthalimidine compound from the aqueous base solution, to provide the purified 2-aryl-3,3-bis(4-hydroxyaryl)phthalimidine of formula (I), and having a phenolphthalein compound content of less than 2,500 ppm, based on the weight of the purified 2-aryl-3,3-bis(4-hydroxyaryl)phthalimidine.Type: ApplicationFiled: December 12, 2008Publication date: June 17, 2010Inventors: Venkata Rama Narayanan Ganapathy BHOTLA, Balakrishnan GANESAN, Kishan Gurram, Salkod Parameshwar MALLIKA, Kumar Arun Satyanarayana, Swaminathan SHUBASHREE
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Patent number: 7714146Abstract: The invention is related to novel azulene-oxindole compounds having formula (I) shown below, wherein one of R1, R2 and R3 represents a moiety of formula (II), each of A1 and A2 independently is nitrogen, oxygen or sulfur, each of the others of R1, R2, R3, R1, R5, R6, R7, R8, R9, R10, R11, R12, R13, and R14 is as recited in the specification. The novel compound potentially inhibits multiple kinases and thus can be used to treat some disease like cancer or inflammatory.Type: GrantFiled: October 31, 2007Date of Patent: May 11, 2010Assignee: Industrial Technology Research InstituteInventors: On Lee, Chrong-Shiong Hwang, Chih-Hung Chen, Yuan-Jang Tsai, Chih-Peng Liu, Ching-Huai Ko, Hsin-Hsin Shen, Ling-Mei Wang, Kuei-Tai Lai, Ying-Chu Shih, Ting-Shou Chen, Yen-Chun Chen, Lain-Tze Lee
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Patent number: 7705044Abstract: The invention relates to compounds of the general formula and optionally the enantiomers thereof. These compounds have advantageous pesticidal properties. They are especially suitable for controlling parasites in warm-blooded animals.Type: GrantFiled: May 14, 2002Date of Patent: April 27, 2010Assignee: Novartis AGInventors: Pierre Ducray, Jacques Bouvier, Matthias Keller, Corina Bergamin
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Patent number: 7671055Abstract: Certain novel 3-(dihaloalkenyl)phenyl derivatives have unexpected insecticidal activity. These compounds are represented by formula (I), where R through R5, a, b, D, E, G and U are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: October 20, 2005Date of Patent: March 2, 2010Assignee: FMC CorporationInventors: Edward J. Barron, Y. Larry Zhang, Frank J. Zawacki, John W. Lyga, George Theodoridis
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Publication number: 20100003191Abstract: The present invention provides a composition for diagnosing amyloid-related diseases, comprising a compound represented by general formula (I): wherein X represents O or the like; R1, R3, R4, R5, R6, R8 and R9 represent a hydrogen atom or the like; R2 represents a halogen atom or the like; and R7 represents a dimethylamino group or the like; or the compound labeled with a radionuclide, or a pharmaceutically acceptable salt of the compound or the labeled compound. The compound represented by general formula (I) has all of the following properties: high binding specificity to amyloid ? protein, high permeability through the blood-brain barrier, and rapid clearance from sites without senile plaques in the brain.Type: ApplicationFiled: October 26, 2007Publication date: January 7, 2010Applicant: NAGASAKI UNIVERSITYInventor: Masahiro Ono
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Publication number: 20090306201Abstract: A pharmaceutical composition comprising a compound of formula I or II and a pharmaceutically acceptable carrier. Methods for treating a proliferative disorder mediated by a methyl transferase comprising administering an anti-proliferative effective amount of the compound of formula I or II are also presented.Type: ApplicationFiled: June 15, 2007Publication date: December 10, 2009Applicant: University of Medicine and Dentistry of New JerseyInventors: Danny Reinberg, Patrick Trojer, Gianluca Sbardella
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Patent number: 7585891Abstract: Certain novel (dihalopropenyl)phenylalkyl substituted benzodioxolane and benzodioxane derivatives have provided unexpected insecticidal activity. These compounds are represented by formula I: where R through R10, inclusively, x, A, B, y, D, E, G and M are fully described herein. Preferred compounds of the present invention are those wherein the benzofused ring moiety is attached to the remainder of the molecule at the positions designated as 1- or 2-. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: GrantFiled: April 28, 2004Date of Patent: September 8, 2009Assignee: FMC CorporationInventors: George Theodoridis, Edward J. Barron, Dominic P. Suarez, Y. Larry Zhang, Ping Ding, John W. Lyga, Matthew P. Whiteside, Frank J. Zawacki
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Publication number: 20090209532Abstract: Compounds of formula (I) exhibit COMT enzyme inhibiting activity and are thus useful as COMT inhibitors.Type: ApplicationFiled: July 17, 2006Publication date: August 20, 2009Inventors: Marko Ahlmark, Reijo Backstrom, Anne Luiro, Jarmo Pystynen, Eija Tiainen
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Patent number: 7576224Abstract: Insecticidal (dihalopropenyl) phenylalkyl substituted dihydrobenzofuran and dihydrobenzopyran derivatives of Formula I are disclosed. These compounds provide unexpected insecticidal activity across a spectrum of insect pests combined with desirable physical properties including improved photostability. wherein x and y are integers independently selected from 0 or 1; and B is a bridging group *—(CR16R17)q—(CR18R19)r—(CR20R21)s-Lt-(CR22R23)u—(CR24R25)v—(CR26R27)w—, where the asterisk denotes attachment at A; and q, r, s, u, v and w are integers independently selected from 0, 1 and 2; and t is an integer selected from 0 and 1. A, D, E, G, M, R through R11, and R16 through R27, inclusively, are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I and methods of controlling insects by applying said compositions to a locus where insects are present or are expected to be present are also disclosed.Type: GrantFiled: December 1, 2005Date of Patent: August 18, 2009Assignee: FMC CorporationInventors: George Theodoridis, Edward J. Barron, Dominic P. Suarez, Y. Larry Zhang, Ping Ding, David M. Roush, Stephen F. Donovan, Frank J. Zawacki, Walter H. Yeager, John W. Lyga, Daniel H. Cohen
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Publication number: 20090192213Abstract: The present invention relates to benzo[b]furane and benzo[b]thiophene derivatives of the general formula IV as the free base or salts thereof and their use.Type: ApplicationFiled: February 20, 2009Publication date: July 30, 2009Applicant: H. Lundbeck A/SInventors: Jan Kehler, Karsten Juhl, Morten Bang Norgaard
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Publication number: 20090131688Abstract: The invention concerns a novel method for synthesis of 4-benzofuran-carboxylic acid or alkyl ester thereof. This method is characterized in that a reaction for aromatization of a compound of formula (II) is performed for the synthesis of the compound of formula (I), according to the scheme A2 below: wherein R independently represents hydrogen or a linear or branched C1-15 alkyl group. With the invention, it is possible to industrially synthesize 4-benzofuran-carboxylic acid or alkyl ester thereof with good yield and very good purity.Type: ApplicationFiled: February 25, 2008Publication date: May 21, 2009Applicant: ZACH SYSTEMInventors: Alain Burgos, Martine Maruani, Florence Perrin, Stephane Frein
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Patent number: 7521476Abstract: The invention relates to compounds of the general formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R8?, R9, W, a, b and n have the significances given in claim 1, and optionally the enantiomers thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling parasites on warm-blooded animals.Type: GrantFiled: June 18, 2003Date of Patent: April 21, 2009Assignee: Novartis AGInventors: Pierre Ducray, Thomas Goebel
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Publication number: 20090088469Abstract: Method for the preparation of citalopram comprising reaction of a compound of Formula (IV) wherein R is halogen, or CF3—(CF2)n—SO2—, n being 0 to 8, with a cyanide source in the presence of a palladium catalyst and a catalytic amount of Cu+ or Zn2+, or with Zn(CN)2 in the presence of a palladium catalyst.Type: ApplicationFiled: December 8, 2008Publication date: April 2, 2009Applicant: H. Lundbeck A/SInventors: Hans Petersen, Michael Harold Rock, Henrik Svane
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Publication number: 20090075989Abstract: The present invention relates to non-steroidal progesterone receptor modulators of the general formula 1, the use of the progesterone receptor modulators for the manufacture of medicaments, and pharmaceutical compositions which comprise these compounds. The compounds according to the invention are suitable for the therapy and prophylaxis of gynaecological disorders such as endometriosis, leiomyomas of the uterus, dysfunctional bleeding and dysmenorrhoea, and for the therapy and prophylaxis of hormone-dependent tumours and for use for female fertility control and for hormone replacement therapy.Type: ApplicationFiled: December 20, 2007Publication date: March 19, 2009Inventors: Wolfgang Schwede, Carsten Moeller, Anja Schmidt, Ulrike Fuhrmann, Andrea Rotgeri, Thomas Andrew Kirkland, Ralf Wyrwa
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Publication number: 20090030214Abstract: Peroxo-carbonates derived from molten alkali and/or Group II metal salts, particularly carbonate salts are used as catalysts in oxidation and epoxidation reactions, transition metal compounds may be included to improve the selectivity of the reactions.Type: ApplicationFiled: July 27, 2007Publication date: January 29, 2009Inventors: Helge Jaensch, Gary David Mohr
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Publication number: 20080268519Abstract: Disclosed herein are non-natural amino acids and polypeptides that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The non-natural amino acids, by themselves or as a part of a polypeptide, can include a wide range of possible functionalities, but typical have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid polypeptides that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such polypeptides. Typically, the modified non-natural amino acid polypeptides include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid polypeptides and modified non-natural amino acid polypeptides, including therapeutic, diagnostic, and other biotechnology uses.Type: ApplicationFiled: October 26, 2007Publication date: October 30, 2008Applicant: AMBRX, INC.Inventors: Zhenwei MIAO, Junjie LIU, Thea NORMAN, Russell DRIVER
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Patent number: 7420001Abstract: The present invention relates to biaryl sulfonamides and their use as, for example, metalloproteinase inhibitors.Type: GrantFiled: December 1, 2004Date of Patent: September 2, 2008Assignee: WyethInventors: Jeremy Ian Levin, Thomas Saltmarsh Rush, III, Frank Lovering, Yonghan Hu, Jianchang Li, Wei Li, Jun Jun Wu, Rajeev Hotchandani, Jason Shaoyun Xiang, Xuemei Du, Derek Cecil Cole, Steve Yikkai Tam
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Publication number: 20080206322Abstract: The present invention relates to a novel composition, e.g. of mycophenolic acid, a salt or a prodrug thereof, in a modified release form.Type: ApplicationFiled: August 29, 2005Publication date: August 28, 2008Applicant: NOVARTIS AGInventors: Dieter Becker, Jutta Beyer, Janez Kerc, Andrea Kramer, Nicoletta Loggia, Chirstian-Peter Luftensteiner, Jorg Ogorka
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Patent number: 7405310Abstract: This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.Type: GrantFiled: March 2, 2005Date of Patent: July 29, 2008Assignee: Medivir ABInventors: Stefan Lindstrom, Christer Sahlberg, Hans Wallberg, Genaidy Kalyanov, Lourdes Salvador Oden, Lotta Naeslund
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Publication number: 20080153873Abstract: The present invention is directed to dihydrobenzofuranyl derivatives of formula I: or a pharmaceutically acceptable salt thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behavioral disorder, cognitive disorder, diabetic neuropathy, pain, and other diseases or disorders.Type: ApplicationFiled: December 12, 2007Publication date: June 26, 2008Applicant: WyethInventors: Puwen Zhang, Joseph Peter Sabatucci, Eugene Anthony Terefenko, Eugene John Trybulski
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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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Patent number: 7273886Abstract: Compounds of Formula I are useful for inhibiting serine protease enzymes, such as TF/factor VIIa, factor Xa, thrombin and kallikrein and have improved pharmacokinetic properties. These compounds may be used in methods of preventing and/or treating clotting disorders.Type: GrantFiled: May 19, 2004Date of Patent: September 25, 2007Assignee: Genentech, Inc.Inventors: Alan G. Olivero, Daniel P. Sutherlin
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Patent number: 7179896Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.Type: GrantFiled: July 15, 2005Date of Patent: February 20, 2007Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
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Patent number: 7157590Abstract: The present invention provides a new and effective process for the synthesis of 17-phenyl-18,19,20-trinor-PGF2? and its derivatives, including the anti-glaucoma drugs Bimatoprost and Latanoprost. The benefit of the present invention rises inter alia from the fact that a major intermediate involved in the synthesis of the above compounds may be isolated from a mixture containing also an undesired isomer, by crystallization. In addition, the undesired isomer may be oxidized to give the starting compound, which is then recycled.Type: GrantFiled: May 3, 2002Date of Patent: January 2, 2007Assignee: Finetech Laboratories Ltd.Inventors: Arie Gutman, Gennady Nisnevich, Marina Etinger, Igor Zaltzman, Lev Yudovitch, Boris Pertsikov
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Patent number: 7126012Abstract: The invention concerns compounds of formula (I): R-A-R? wherein: A is as defined in the description; R represents a group (V), (VI), (VII) or (VIII), where E, Q, R1, R2, R3, v and R4 are as defined in the description; R? represents a —(CH2)t-R5 group wherein t and R5 are as defined in the descriptionType: GrantFiled: September 23, 2004Date of Patent: October 24, 2006Assignee: Les Laboratoires ServierInventors: Daniel Lesieur, Frederique Klupsch, Gerald Guillaumet, Marie-Claude Viaud, Michel Langlois, Caroline Bennejean, Pierre Renaud, Philippe Delagrange
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Patent number: 7041700Abstract: This invention relates to benzopyran derivatives of the formula (1) or the formula (2) wherein R1 and R2 represent independently of each other hydrogen atom or C1-6alkyl group, R3 represents hydroxyl group or C1-6 alkylcarbonyloxy group, R4 represents hydrogen atom or C1-6 alkyl group, R5 represents C1-6 alkyl group substituted with C6-14 aryl group or heteroaryl group, R6 represents C1-6 alkyl group, C1-6 alkoxy group, halogen atom, nitro group, C(O)NH2, C(O)NHR8 or C(O)NR8R9, or pharmaceutically acceptable salts thereof.Type: GrantFiled: June 17, 2002Date of Patent: May 9, 2006Assignee: Nissan Chemical Industries, Ltd.Inventors: Yoshio Ohara, Kazuhiko Ohrai, Kazufumi Yanagihara, Yukihiro Shigeta, Toru Tsukagoshi, Toru Yamashita
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Patent number: 7019024Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.Type: GrantFiled: January 9, 2001Date of Patent: March 28, 2006Assignee: Allelix Neuroscience Inc.Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
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Patent number: 6998407Abstract: Chemical compounds which are antagonists of Monocyte Chemoattractant Protein-1 (MCP-1) function, pharmaceutical compositions comprising these compounds, methods of treatment employing these compounds and compositions, and processes for preparing these compounds. The compounds are useful in the prevention or treatment of chronic or acute inflammatory or autoimmune diseases, especially those associated with aberrant lymphocyte or monocyte accumulation such as arthritis, asthma, atherosclerosis, diabetic nephropathy, inflammatory bowel disease, Crohn's disease, multiple sclerosis, nephritis, pancreatitis, pulmonary fibrosis, psoriasis, restenosis, and transplant rejection.Type: GrantFiled: November 18, 2003Date of Patent: February 14, 2006Assignees: Telik, Inc., Sanwa Kagaku Kenkyusho Co. Ltd.Inventors: Edgardo Laborde, Louise Robinson, Fanying Meng, Brian T. Peterson, Hugo O. Villar, Steven E. Anuskiewicz, Yoshiro Ishiwata, Shoji Yokochi, Yukiharu Matsumoto, Takuji Kakigami, Hideaki Inagaki, Takahito Jomori, Kouji Matsushima
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Patent number: 6987194Abstract: Insecticidal (dihalopropenyl) phenylalkyl substituted dihydrobenzofuran and dihydrobenzopyran derivatives of Formula I are disclosed. These compounds provide unexpected insecticidal activity across a spectrum of insect pests combined with desirable physical properties including improved photostability. wherein x and y are integers independently selected from 0 or 1; and B is a bridging group *—(CR16R17)q—(CR18R19)r—(CR20R21)s—Lt—(CR22R23)u—(CR24R25)v—(CR26R27)w—, where the asterisk denotes attachment at A; and q, r, s, u, v and w are integers independently selected from 0, 1 and 2; and t is an integer selected from 0 and 1. A, D, E, G, M, R through R11, and R16 through R27, inclusively, are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I and methods of controlling insects by applying said compositions to a locus where insects are present or are expected to be present are also disclosed.Type: GrantFiled: April 27, 2004Date of Patent: January 17, 2006Assignee: FMC CorporationInventors: George Theodoridis, Edward J. Barron, Dominic P. Suarez, Y. Larry Zhang, Ping Ding, David M. Roush, Stephen F. Donovan, Frank J. Zawacki, Walter H. Yeager, John W. Lyga, Daniel H. Cohen
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Patent number: 6984741Abstract: The present invention relates to 5-nitrobenzofurans, to a process for preparing 5-nitrobenzofurans, and to 5-nitro-2,3-dihydrobenzofuran-3-ols, to a process for the preparation thereof and to intermediates.Type: GrantFiled: August 18, 2003Date of Patent: January 10, 2006Assignee: Bayer AktiengesellschaftInventor: Wolfgang Mägerlein
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Patent number: 6969766Abstract: This application relates to monomers of the general formula (I) for the preparation of PNA (peptide nucleic acid) oligomers and provides method for the synthesis of both predefined sequence PNA oligomers and random sequence PNA oligomers: wherein E is nitrogen or C—R?; J is sulfur or oxygen; R?, R1, R2, R3, R4 is independently H, halogen, alkyl, nitro, nitrile, alkoxy, halogenated alkyl, halogenated alkoxy, phenyl or halogenated phenyl, R5 is H or protected or unprotected side chain of natural or unnatural ?-amino acid; and B is a natural or unnatural nucleobase, wherein when said nucleobase has an exocyclic amino function, said function is protected by protecting group which is labile to acids but stable to weak to medium bases in the presence of thiol.Type: GrantFiled: April 25, 2003Date of Patent: November 29, 2005Assignee: Panagene, Inc.Inventors: Sung Kee Kim, Hyunil Lee, Jong Chan Lim, Hoon Choi, Jae Hoon Jeon, Sang Youl Ahn, Sung Hee Lee, Won Jun Yoon
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Patent number: 6958358Abstract: Compounds of general formula (I): wherein R1, Y, (X)o, (W)n, (V)m, Z and U are as defined in the specification, are inhibitors of cruzipain and other cysteine protease inhibitors and are useful as therapeutic agents, for example in Chagas' disease, or for validating therapeutic target compounds.Type: GrantFiled: January 17, 2002Date of Patent: October 25, 2005Assignee: Amura Therapeutics LimitedInventors: Martin Quibell, Manoj Kumar Ramjee
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Patent number: 6951870Abstract: Compounds of formula I? wherein the two —OH substituents in the phenyl moiety are in a position ortho to one another and R1 in a position ortho to one of the hydroxy groups; and X, R1 to R6 are as defined in disclosure. The compounds exhibit COMT enzyme inhibiting activity, so are useful as COMT inhibitors.Type: GrantFiled: June 28, 2001Date of Patent: October 4, 2005Assignee: Orion CorporationInventors: Jarmo Pystynen, Martti Ovaska, Jukka Vidgren, Timo Lotta, Marjo Yliperttula-Ikonen
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Patent number: 6943182Abstract: The invention relates to cyclopentabenzofuran derivatives, process for their preparation, the use of cyclopentabenzofuran derivatives for the production of a medicament for the therapy of NF-?B-dependent diseases and medicaments which contain the cyclopentabenzofuran derivatives.Type: GrantFiled: May 30, 2002Date of Patent: September 13, 2005Assignee: Bayer AktiengesellschaftInventors: Walter Guarnieri, Thomas Jaetsch, Andreas Schoop, Jörg Baumgarten, Axel Kretschmer, Horst-Peter Antonicek
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Patent number: 6927300Abstract: Disclosed is a process for the preparation of the anti-glaucoma drug Latanoprost, in good yield, in large amounts and with desired purity. Also disclosed are novel intermediates for the above process.Type: GrantFiled: January 26, 2001Date of Patent: August 9, 2005Assignee: FineTech Laboratories LTDInventors: Arie Gutman, Gennadiy Nisnevich, Marina Etinger, Igor Zaltzman, Lev Judovich, Boris Pertsikov
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Patent number: 6903134Abstract: The invention relates to a cosmetic or pharmaceutical formulation comprising at least one compound of formula (I). The cosmetics or pharmaceutical products are particularly suitable for the care of the skin in protecting against oxidative stress and ageing phenomena.Type: GrantFiled: January 22, 2001Date of Patent: June 7, 2005Assignee: Merck Patent GmbHInventors: Frank Pflücker, Herwig Buchholz, Ralf Rosskopf, Joachim Bünger
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Patent number: 6864379Abstract: Methods for manufacture of citalopram through stepwise alkylation of 5-substituted 1-(4-fluorophenyl)-1,3-dihydroisobenzofurans are disclosed.Type: GrantFiled: September 10, 2002Date of Patent: March 8, 2005Assignee: H. Lundbeck A/SInventors: Hans Petersen, Haleh Ahmadian
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Patent number: 6861444Abstract: Compounds of the general formula (I): or a salt thereof, wherein R1 is hydrogen, hydroxyl or halogen; R2 is NHSO2CH3, SO2NHCH3 or the like; R5 and R6 each independently is hydrogen, C1-6 alkyl, optionally substituted phenyl or optionally substituted benzyl; X is NH, sulfur, oxygen or methylene; Y is oxygen, NR7, sulfur, methylene or a bond; and * represents an asymmetric carbon atom. The compounds are useful as a medicine for treating or preventing diabetes, obesity, hyperlipidemia, digestive diseases, depression or urinary disturbances.Type: GrantFiled: April 25, 2001Date of Patent: March 1, 2005Assignee: Asahi Kasei Pharma CorporationInventors: Shunichi Ikuta, Shiro Miyoshi, Kohei Ogawa
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Patent number: 6855822Abstract: Benzo[b]furan dimers and processes for their preparation are provided. The invention provides a synthetic process for the preparation of benzo[b]furan dimer using mild reaction conditions, which provides a high substituent tolerance and is appropriate for use in solid phase syntheses for producing a library of benzo[b]furan dimers for biological screening.Type: GrantFiled: June 23, 2003Date of Patent: February 15, 2005Assignee: VivoQuest, Inc.Inventors: Yun Liao, Reza Fathi, Zhen Yang
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Patent number: 6849203Abstract: The invention relates to photoisomerizable compounds of formula I wherein A, Z, L, R, R1, k, m and r are defined herein.Type: GrantFiled: April 5, 2002Date of Patent: February 1, 2005Assignee: Merck Patent Gesellschaft Mit Beschraenkter HaftungInventors: Louise Diane Farrand, Christopher Worrall, Owain Llyr Parri
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Patent number: 6828341Abstract: Described are cyclohexylamine derivatives of Formula I and pharmaceutically acceptable salts thereof, wherein R1, g, *, R, V, B, E, Y, G, H, X1, and d are as defined in the description. The compounds of Formulas I, VI, and VIa are antagonists of NMDA receptor channel complexes useful for treating cerebral vascular disorders such as, for example, stroke, cerebral ischemia, trauma, hypoglycemia, anxiety, migraine headache, convulsions, Parkinson's disease, aminoglycoside antibiotics-induced hearing loss, psychosis, glaucoma, CMV retinitis, opioid tolerance or withdrawal, chronic pain, or urinary incontinence.Type: GrantFiled: March 27, 2002Date of Patent: December 7, 2004Assignee: Warner-Lambert CompanyInventors: Russell Joseph DeOrazio, Sham Shridhar Nikam, Ian Leslie Scott, Brian Alan Sherer