The Nitrogen Is Attached Indirectly To A Benzene Ring By Acyclic Nonionic Bonding Patents (Class 558/422)
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Patent number: 11845710Abstract: The present application relates to a method for citalopram intermediate citalopram diol. The method comprises: first mixing two Grignard reagents required for a reaction; then mixing the mixed Grignard reagents with a raw material 5-cyanophthalide in a temperature-controllable micromixer to obtain a reaction solution; then subjecting the reaction solution to the reaction by means of a reactor to obtain a citalopram diol reaction solution; and then performing operations such as quenching, concentration, extraction, acidification, and crystallization to obtain a qualified product. The citalopram diol provided in the present invention has good selectivity, high yield, high safety, safety and reliability, and little sewage discharge, and is suitable for industrial production.Type: GrantFiled: December 2, 2019Date of Patent: December 19, 2023Assignees: ZHEJIANG HUAHAI PHARMACEUTICAL CO., LTD, SHANGHAI AOBO PHARMTECH, INC., LTD.Inventors: Chen Liu, Xing Li, Huaxiang Ye, Jicheng Zhang, Luning Huang, Anping Tao, Jianguo An, Hong Gu
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Patent number: 10253002Abstract: The invention provides compounds of Formula I, and methods of treating or preventing a bacterial infection in a subject using a compound of Formula I. The invention also provides the use of a compound of Formula I in the manufacture of a medicament for the treatment of a bacterial infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a bacterial infection in a subject and to a medical device comprising the composition of the invention.Type: GrantFiled: May 1, 2014Date of Patent: April 9, 2019Assignee: NEOCULI PTY LTDInventors: Stephen Page, Sanjay Garg, Martine Keenan, Adam McCluskey, Andrew Stevens
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Publication number: 20150065725Abstract: In OLEDs, improved efficiency is obtained by compounds which can form inter alia electron injection layers of the formula (I) wherein R1 is a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with one or more C1-C4 alkyl, alkoxy or cyano; R2 and R3 together form a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with C1-C4 alkyl, alkoxy or cyano; R4 is hydrogen, C1-C4 alkyl or aryl; and Ar is monocyclic, bicyclic or tricyclic aryl or heteroaryl which is optionally substituted with one or more C1-C4-alkyl or alkoxy groups, or an oligomer thereof.Type: ApplicationFiled: October 9, 2014Publication date: March 5, 2015Inventors: Poopathy KATHIRGAMANATHAN, Yun Fu CHAN
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Patent number: 8815870Abstract: The present teachings provide a compound of Formula (I-B): wherein R1-R10 are as described herein; a pharmaceutically acceptable salt of the compound, a geometric isomer of the compound, or a pharmaceutically acceptable salt of the geometric isomer. Also described are methods of preparing the same, as well as methods for preparing vilazodone using the same.Type: GrantFiled: July 1, 2013Date of Patent: August 26, 2014Inventors: Henning Böttcher, Timo Heinrich
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Publication number: 20140209872Abstract: A compound having an electron injection capability and/or electron transport capability represented by Formula 1, an organic light emitting device including the compound; and a flat display device including the organic light emitting device. The descriptions of substituents are referred to in the detailed description.Type: ApplicationFiled: July 26, 2013Publication date: July 31, 2014Inventors: Jun-Ha Park, Seok-Hwan Hwang, Young-Kook Kim, Hye-Jin Jung, Eun-Young Lee, Jin-O Lim, Sang-Hyun Han, Eun-Jae Jeong, Soo-Yon Kim, Jong-Hyuk Lee
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Publication number: 20140200239Abstract: The present invention provides new compounds of formula I, II or III, which have Src homology-2 containing protein tyrosine phosphatase-1 (SHP-1) agonist activity. Also provided are treatment methods using the compounds of formula I, II or III.Type: ApplicationFiled: August 3, 2012Publication date: July 17, 2014Applicant: National Taiwan UniversityInventors: Chung-Wai Shiau, Kuen-Feng Chen
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Publication number: 20140142304Abstract: There is provided a process for producing an aminopropyne or an enaminone comprising the step of reacting a metal acetylide, an amine and a carbonyl-containing compound in the presence of a transition metal catalyst. There is also provided a process for producing an aminopropyne comprising the step of reacting a metal acetylide, an amine and a halide-containing compound in the presence of a transition metal catalyst at a reaction temperature of 50° C. to 150° C. There are also provided processes to further synthesize the aminopropyne produced to obtain a butyneamine, another aminopropyne or a triazol.Type: ApplicationFiled: July 6, 2012Publication date: May 22, 2014Applicant: Agency for Science, Technology and ResearchInventors: Yugen Zhang, Dingyi Yu, Zhewang Lin
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Publication number: 20140005395Abstract: The present teachings provide a compound of Formula (I-B): wherein R1-R10 are as described herein; a pharmaceutically acceptable salt of the compound, a geometric isomer of the compound, or a pharmaceutically acceptable salt of the geometric isomer. Also described are methods of preparing the same, as well as methods for preparing vilazodone using the same.Type: ApplicationFiled: July 1, 2013Publication date: January 2, 2014Inventor: Matthew Ronsheim
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Patent number: 8431514Abstract: The present invention relates to bis-amide derivatives of formula (I), to processes and intermediates for preparing them, to methods of using them to control insect, acarine, nematode and mollusc pests, and to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them.Type: GrantFiled: April 14, 2010Date of Patent: April 30, 2013Assignee: Syngenta Crop Protection LLCInventors: Pierre Joseph Marcel Jung, Christopher Richard Ayles Godfrey, Ottmar Franz Hueter, Peter Maienfisch
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Patent number: 8314137Abstract: The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.Type: GrantFiled: July 22, 2009Date of Patent: November 20, 2012Assignee: Trustess of Dartmouth CollegeInventors: Tadashi Honda, Emilie David, Dale Mierke
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Publication number: 20120289595Abstract: The present invention relates to a novel biarylamide derivative and a pharmaceutical composition or a cosmetic composition comprising the same as an active ingredient. More particularly, the present invention relates to a novel biarylamide derivative, a pharmaceutical composition or a cosmetic composition for preventing or treating a pigmentation disorder caused by an abnormal excess of melanin or a disease caused by melanocyte hyperplasia comprising the same as an active ingredient. The biarylamide derivative of the present invention inhibits melanin production and thus inhibits melanocyte hyperplasia. Therefore, a cosmetic composition comprising the biarylamide is excellent in a whitening effect, and a pharmaceutical composition comprising the biarylamide is effective in the prevention or treatment of pigmentation disorders of skin such as lentigo, melasma, freckle, etc. and malignant melanoma.Type: ApplicationFiled: July 25, 2012Publication date: November 15, 2012Applicant: Catholic University Industry Academy Cooperation FoundationInventor: Dong Heon Shin
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Publication number: 20120282629Abstract: The present invention relates to compounds suitable for modulating huntingtin protein processing and useful for treating or preventing huntingtin-related disorders. The invention provides pharmaceutical compositions comprising said compounds and methods of syntheses thereof.Type: ApplicationFiled: August 19, 2010Publication date: November 8, 2012Applicant: MAX-DELBRUCK-CENTRUM FUR MOLEKULARE MEDIZINInventors: Erich Wanker, Thomas Wiglenda, Julius Tachu Babila, Annett Boddrich, Michael Schmidt, Sandra Neuendorf, Franziska Schiele
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Publication number: 20120205638Abstract: In OLEDs, improved efficiency is obtained by compounds which can form inter alia electron injection layers of the formula (I) wherein R1 is a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with one or more C1-C4 alkyl, alkoxy or cyano; R2 and R3 together form a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with C1-C4 alkyl, alkoxy or cyano; R4 is hydrogen, C1-C4 alkyl or aryl; and Ar is monocyclic, bicyclic or tricyclic aryl or heteroaryl which is optionally substituted with one or more C1-C4-alkyl or alkoxy groups, or an oligomer thereof.Type: ApplicationFiled: April 27, 2012Publication date: August 16, 2012Applicant: Merck Patent GmbHInventors: Poopathy Kathirgamanathan, Yun Fu Chan
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Publication number: 20120004262Abstract: The present invention relates to phenylcyclopropylamine derivatives. In particular, pharmaceutical compositions comprising phenylcyclopropylamine derivatives are provided. The compounds of this invention can, inter alia, be used for the treatment and the prevention of cancer as well as neurodegenerative diseases or disorders.Type: ApplicationFiled: January 21, 2010Publication date: January 5, 2012Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria
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Patent number: 8067640Abstract: The present invention relates to a novel method for the preparation of diol intermediates having the formula (II) and/or the opposite enantiomer of an acylated diol having the formula (IV) useful for the preparation of escitalopram involving selective enzymatic acylation or deacylation.Type: GrantFiled: May 17, 2010Date of Patent: November 29, 2011Assignee: H. Lundbeck A/SInventors: Naoki Taoka, Takahisa Kato, Shogo Yamamoto, Takashi Yoshida, Toshihiro Takeda, Yasuyoshi Ueda, Hans Petersen, Robert Dancer, Haleh Ahmadian, Lars O. Lyngso
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Publication number: 20110269834Abstract: Described herein are compounds and compositions, and methods for using the compounds and compositions, for treating respiratory diseases and illness, such as severe acute respiratory syndrome (SARS).Type: ApplicationFiled: August 21, 2009Publication date: November 3, 2011Applicants: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS, PURDUE RESEARCH FOUNDATIONInventors: Arun K. Ghosh, Jun Takayama, Andrew David Mesecar, Michael E. Johnson, Kiira M. Ratia, Rima Chaudhuri, Debbie C. Mulhearn
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Publication number: 20110230465Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: ApplicationFiled: September 16, 2010Publication date: September 22, 2011Applicant: BOEHRINGER INGLEHEIM INTERNATIONAL GMBHInventors: Timothy STAMMERS, Xavier BARBEAU, Pierre BEAULIEU, Megan BERTRAND-LAPERLE, Christian BROCHU, Paul J. EDWARDS, Pasquale FORGIONE, Cédrickx GODBOUT, Oliver HUCKE, Marc-André JOLY, Serge LANDRY, Olivier LEPAGE, Julie NAUD, Marc PESANT, Martin POIRIER, Maude POIRIER, Bounkham THAVONEKHAM
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Patent number: 8022232Abstract: This patent discloses a method for resolution of 4-[4-(dimethylamino)-1-(4?-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile as a racemic or non-racemic enantiomer mixture into its isolated enantiomers, said method comprising the step of fractionally crystallizing 4-[4-(dimethylamino)-1-(4?-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile as a salt with the (+)-(S,S)- or (?)-(R,R)-enantiomer of O,O?-di-p-toluoyl-tartaric acid in a solvent system comprising 1-propanol, ethanol or acetonitrile.Type: GrantFiled: September 2, 2008Date of Patent: September 20, 2011Assignee: H. Lundbeck A/SInventors: Carla De Faveri, Florian Anton Martin Huber, Robert Dancer
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Publication number: 20110196007Abstract: The present invention features monocyclic cyanoenone compositions and methods for using the same in the treatment of diseases such as cancer, inflammatory diseases and neurodegenerative diseases.Type: ApplicationFiled: July 22, 2009Publication date: August 11, 2011Inventors: Tadashi Honda, Emilie David, Dale Mierke
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Publication number: 20110118325Abstract: This invention provides REL inhibitors which interfere with the DNA binding capacity of a REL protein. Additionally this invention provides methods of treating, abrogating, or preventing diseases which respond with a positive clinical score to a REL inhibitor. Methods of identifying REL inhibitor based on a REL protein three dimensional model are described.Type: ApplicationFiled: January 7, 2009Publication date: May 19, 2011Inventors: Youhai H. Chen, Ramachandran Murali, Jing Sun
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Publication number: 20110092719Abstract: The present patent application relates to an improved process for the preparation of escitalopram, its salts and intermediates. It also relates to a novel crystalline form S of citalopram diol intermediate, process for preparation and its use in the preparation of citalopram, escitalopram and their salts.Type: ApplicationFiled: May 28, 2009Publication date: April 21, 2011Applicant: SHODHANA LABORATORIES LIMITEDInventors: Thota Giridhar, Gudipati Srinivasulu, Kotaru Srinivasa Rao
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Publication number: 20110009648Abstract: This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.Type: ApplicationFiled: January 22, 2007Publication date: January 13, 2011Applicant: Sandoz AGInventors: Martin Albert, Hubert Sturm, Andreas Berger, Peter Kremminger
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Publication number: 20100298330Abstract: The present invention is related to the preparation and pharmaceutical In use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification:(I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases.Type: ApplicationFiled: November 19, 2008Publication date: November 25, 2010Applicant: PHARMAXIS LTD.Inventors: Ian A. McDonald, Craig Ivan Turner, Mandar Deodhar, Jonathan Stuart Foot
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Publication number: 20100179216Abstract: Provided is a novel amine compound represented by the following formula (I) having a superior peripheral blood lymphocyte decreasing action and superior in the immunosuppressive action, rejection suppressive action and the like, which shows decreased side effects of, for example, bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof. wherein each symbol is as defined in the specification.Type: ApplicationFiled: June 13, 2008Publication date: July 15, 2010Inventors: Masatoshi Kiuchi, Kaoru Tashiro, Maiko Hamada, Kunio Sugahara
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Publication number: 20100174090Abstract: The present application relates to novel methods for the preparation of primary, secondary and tertiary carbinamine compounds, particularly the preparation of compounds of formulae I, IV and VI, from a carbonyl compound of formula II in the presence of ammonia or an ammonium equivalent of the formula NH4+X?, by way of allylation, crotylation, arylation, reductive amination and catalytic hydrogenation.Type: ApplicationFiled: March 28, 2008Publication date: July 8, 2010Inventors: Avinash N. Thadani, Bhartesh Dhudshia
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Patent number: 7585982Abstract: The present invention relates to a method for producing an isoindole derivative (compound (II)) with the following general formula (II): (wherein R1 and R2 each independently represents a C1-6 alkyl group) or a salt thereof, comprising the step of cyclizing, in a solvent, compound (I) with the following general formula (I): (wherein R1 and R2 have the same meanings as R1 and R2 in formula (II) above) or a salt thereof, or their hydrate or solvate in the presence of a base (Step 1).Type: GrantFiled: July 27, 2005Date of Patent: September 8, 2009Assignee: Eisai R&D Management Co., Ltd.Inventors: Kazuhiro Yoshizawa, Taiju Nakamura, Shigeto Negi
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Patent number: 7582780Abstract: The invention relates to a method of separating and isolating an acylated derivative of 4-[(S)-4-dimethylamino-1-(4-fluorophenyl)-1-hydroxybutyl]-3-hydroxymethylbenzonitrile by reaction of a mixture of the 4-[(S)-4-dimethylamino-1-(4-fluorophenyl)-1-hydroxy-butyl]-3-hydroxymethylbenzonitrile and an acylated derivative thereof with a compound which form a derivative of the 4-[(S)-4-dimethylamino-1-(4-fluorophenyl)-1-hydroxy-butyl]-3-hydroxymethylbenzonitrile containing a carboxylic acid group. The acylated derivative containing a carboxylic acid group precipitates once it is formed and may easily be separated from the reaction mixture.Type: GrantFiled: February 2, 2005Date of Patent: September 1, 2009Assignee: H. Lundbeck A/SInventor: Lars Ole Lyngso
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Publication number: 20090137800Abstract: A compound represented by the following general formula (I), wherein ring A and ring B each independently represent a benzene, naphthalene, or heterocyclic ring which may be substituted; R1 and R2 each independently represent an alkyl group having 1 to 8 carbon atoms which may be substituted; R1 and R2 may be linked together to form a ring; a methylene group of the alkyl group having 1 to 8 carbon atoms may be replaced by —O— or —CH?CH—; Anq- represents a q-valent anion, where q is 1 or 2; p represents a coefficient to keep the charge neutral.Type: ApplicationFiled: March 5, 2007Publication date: May 28, 2009Inventor: Satoshi Yanagisawa
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Publication number: 20080214834Abstract: The present invention relates to a method for producing an isoindole derivative (compound (II)) with the following general formula (II): (wherein R1 and R2 each independently represents a C1-6 alkyl group) or a salt thereof, comprising the step of cyclizing, in a solvent, compound (I) with the following general formula (I): (wherein R1 and R2 have the same meanings as R1 and R2 in formula (II) above) or a salt thereof, or their hydrate or solvate in the presence of a base (Step 1).Type: ApplicationFiled: July 27, 2005Publication date: September 4, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Kazuhiro Yoshizawa, Taiju Nakamura, Shigeto Negi
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Patent number: 7256312Abstract: The invention relates to a process for preparing 4-[aminoalkoxy]benzylamines of the general formula (I) by catalytically hydrogenating 4-[aminoalkoxy]benzonitriles of the general formula (II) where, in the compounds of the general formulae I and II, R1 is C1-C8-alkylene, R2 and R3 are each independently C1-C8-alkyl or are joined to give a ring which may additionally contain a heteroatom, which comprises carrying out the hydrogenation at elevated pressure and elevated temperatures. The invention further relates to a process for preparing the intermediate (II).Type: GrantFiled: July 18, 2003Date of Patent: August 14, 2007Assignee: BASF AktiengesellschaftInventors: Oliver Löber, Christoph Benisch, Klaus Ebel, Johann-Peter Melder
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Patent number: 7241625Abstract: A carbonyl compound scavenger comprising a mineral acid salt of a benzylhydroxyamine-based compound of the formula (1) and at least one adsorbent selected from the group consisting of silica gel, alumina, cellulose and activated carbon: [wherein, R represents an alkyl group having 1 to 8 carbon atoms, haloalkyl group having 1 to 4 carbon atoms, alkoxy group having 1 to 4 carbon atoms, haloalkoxy group having 1 to 4 carbon atoms, nitro group or cyano group, and R1 and R2 represent each independently a hydrogen atom or alkyl group having 1 to 8 carbon atoms, and a hydrogen atom on a benzene ring to which a cyano group and R are connected may be substituted with an alkyl group having 1 to 8 carbon atoms, haloalkyl group having 1 to 4 carbon atoms, alkoxy group having 1 to 4 carbon atoms, haloalkoxy group having 1 to 4 carbon atoms, aryl group having 6 to 10 carbon atoms, nitro group or cyano group.].Type: GrantFiled: June 2, 2005Date of Patent: July 10, 2007Assignee: Sumika Chemical Analysis Service, LimitedInventors: Kazuya Kitasaka, Hatsumi Shimajiri, Koichi Sugihara
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Patent number: 7223794Abstract: There are provided novel compounds of formula (I), wherein R1, R2, R3, T, U, X, Y, V and W are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy.Type: GrantFiled: July 26, 2002Date of Patent: May 29, 2007Assignee: AstraZeneca ABInventors: David Cheshire, Stephen Connolly, Antonio Mete
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Patent number: 6953797Abstract: There is disclosed the use of a compound of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of nitric oxide synthase activity is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed; together with processes for their preparation, compositions containing them and their use in therapy.Type: GrantFiled: February 20, 2001Date of Patent: October 11, 2005Assignee: AstraZeneca ABInventors: David Cheshire, Stephen Connolly, David Cox, Ian Millichip
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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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Patent number: 6900243Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.Type: GrantFiled: February 20, 2001Date of Patent: May 31, 2005Assignee: AstraZeneca ABInventors: David Cheshire, Stephen Connolly, David Cox, Antonio Mete
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Patent number: 6890955Abstract: The invention concerns aryloxypropanolamine derivatives having at least an anti-diabetic and anti-fat activity and their methods of preparation and applications, particularly as human and veterinary medicine and animal food additive.Type: GrantFiled: January 3, 2003Date of Patent: May 10, 2005Assignee: Virbac SAInventors: Ahmed El Hadri, Philippe Archimbault, Gérard Leclerc, Arthur Donny Strosberg, France Pietri-Rouxel
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Patent number: 6861561Abstract: The invention relates to substituted aromatic polycyclic tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.Type: GrantFiled: September 26, 2002Date of Patent: March 1, 2005Assignee: G. D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Mark A. Massa, Jane L. Wang, Deborah A. Mischke, Barry L. Parnas, Melvin L. Rueppel
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Patent number: 6743939Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.Type: GrantFiled: August 22, 2002Date of Patent: June 1, 2004Assignee: AstraZeneca ABInventors: Tim Birkinshaw, David Cheshire, Antonio Mete
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Patent number: 6710080Abstract: Substituted 2-dialkylaminoalkylbiphenyl derivatives, processes for their preparation, pharmaceutical compositions comprising these compounds and methods using these compounds for the preparation of medicaments and for the treatment of diseases.Type: GrantFiled: February 11, 2002Date of Patent: March 23, 2004Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Babette-Yvonne Koegel, Helmut Buschmann
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Publication number: 20040039033Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, 1Type: ApplicationFiled: December 10, 2002Publication date: February 26, 2004Inventors: Karnail S. Atwal, Gary J. Grover, Charles Z. Ding, Philip D. Stein, John Lloyd, Saleem Ahmad, Lawrence G. Hamann, David Green, Francis N. Ferrara
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Patent number: 6576596Abstract: The invention relates to 2-benzoylcyclohexane-1,3-diones of the formula I where R1, R2 are each hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxyalkyl, alkenyl, alkynyl, —OR5, —OCOR6, —OSO2R6, —SH, —S(O)nR7, —SO2OR5, —SO2NR5R8, —NR8SO2R6 or —NR8COR6; R3 is hydrogen, cyano, alkyl, haloalkyl, —OR7, —SR7 or —NR7R10; R4 is hydrogen, substituted or unsubstituted alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, —COR9, —CO2R9, —COSR9 or —CONR8R9; X is oxygen or NR8; n is 0, 1 or 2; R5 is hydrogen, alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R6 is alkyl or haloalkyl; R7 is alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R8 is hydrogen or alkyl; R9 is alkyl, alkenyl, alkynyl, phenyl or benzyl; R10 is alkyl, haloalkyl, alkenyl or alkynyl; Q is a cyclohexane-1,3-dione ring with or without substitution attached in position 2; and agriculturally useful salts thereoType: GrantFiled: June 23, 1999Date of Patent: June 10, 2003Assignee: BASF AktiengesellschaftInventors: Regina Luise Hill, Uwe Kardorff, Michael Rack, Ernst Baumann, Wolfgang von Deyn, Stefan Engel, Guido Mayer, Martina Otten, Joachim Rheinheimer, Matthias Witschel, Ulf Misslitz, Helmut Walter, Karl-Otto Westphalen
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Patent number: 6541670Abstract: A compound of the general formula I wherein R1 represents a substituent selected from the group consisting of halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, and nitro; R2 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, —CONH2, phenyl, and nitro; R3 represents one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, cyano, carboxy, carbamoyl, (C1-C10)alkyl, (C2-C10)olefinic group, (C3-C8)monocyclic hydrocarbon group, (C1-C10)alkoxy, (C1-C10)alkylthio, (C1-C10)alkoxycarbonyl, and phenyl; R4 represents hydrogen, (C1-C6)alkyl, (C2-C6)olefinicType: GrantFiled: March 20, 2001Date of Patent: April 1, 2003Assignee: Leo Pharmaceutical Products Ltd. A/SInventor: Erik Rytter Ottosen
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Patent number: 6521667Abstract: The present invention features calcilytic compounds. “Calcilytic compounds” refer to compounds able to inhibit calcium receptor activity. Also described are the use of calcilytic compounds to inhibit calcium receptor activity and/or achieve a beneficial effect in a patient; and techniques which can be used to obtain additional calcilytic compounds.Type: GrantFiled: August 11, 1998Date of Patent: February 18, 2003Assignees: NPS Pharmaceuticals, Inc., SmithKline Beecham, PLC, SmithKline Beecham, Corp.Inventors: Eric G. Del Mar, Robert M. Barmore, Derek Sheehan, Bradford C. Van Wagenen, James F. Callahan, Richard M. Keenan, Nikesh R. Kotecha, Maria Amparo Lago, Linda Sue Southall, Mervyn Thompson
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Patent number: 6479550Abstract: &agr;-Sulfenimino acid derivatives of formula I including the optical isomers thereof and mixtures of such isomers, wherein A is cycloalkyl, cycloalkenyl, aryl or heteroaryl, each optionally substituted, B is a direct bond or optionally substituted alkylene, E is hydrogen or optionally substituted aryl, R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, each optionally substituted, and T is NH or oxygen, have been found to be useful for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi. The invention relates the novel compounds and also to the preparation thereof and to the use of the compounds for plant protection, and to compositions suitable for applying the novel compounds in agricultural techniques.Type: GrantFiled: July 16, 2001Date of Patent: November 12, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: André Jeanguenat, Martin Zeller, Hugo Ziegler
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Patent number: 6448293Abstract: A compound of general formula (I), or pharmaceutically acceptable salts, solvates or polymorphs thereof; wherein; R1 and R2, which may be the same or different, are hydrogen, C1-C6alkyl, (CH2)m (C3-C6cycloalkyl) wherein m =0, 1, 2 or 3, or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; each R3 is independently CF3, OCF3, C1-4alkylthio or C1-C4alkoxy; n is 1, 2 or 3; and R4 and R5, which may be the same or different, are: A—X, wherein A =—CH=CH— or —(CH2)p— where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7, SO2NR6R7, SO2NHC(=O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; R6, R7, R8 and R10 which may be the same or different, are hydrogen or C1-6alkyl optionally substituted independently by one or more R12; R9 is C1-6 alkyl optionally substituted independently by one or more R12; R11 is hydrogen, C1-6 alkyl optionally substituted independently by one or more R12, C(OType: GrantFiled: March 16, 2001Date of Patent: September 10, 2002Assignee: Pfizer Inc.Inventors: Mark David Andrews, David Hepworth, Donald Stuart Middleton, Alan Stobie
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Patent number: 6437153Abstract: The present invention relates to a novel process for preparing 3-(1-hydroxyphenyl-1-alkoximinomethyl)dioxazines which are known as intermediates for preparing compounds having fungicidal properties (WO 95-04728). Furthermore, the invention relates to novel 3-(1-hydroxyphenyl-1-alkoximinomethyl)dioxazines, to novel intermediates for their preparation and to a plurality of processes for preparing the novel intermediates.Type: GrantFiled: September 26, 2001Date of Patent: August 20, 2002Assignee: Bayer AktiengesellschaftInventors: Bernd Gallenkamp, Lothar Rohe, Herbert Gayer, Peter Gerdes
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Patent number: 6417215Abstract: Novel calcilytic compounds are provided.Type: GrantFiled: July 26, 2001Date of Patent: July 9, 2002Assignee: SmithKline Beecham CorporationInventor: Amparo Maria Lago
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Patent number: 6392083Abstract: A process for producing a salt of a cyanobenzylamine comprising reacting a cyanobenzylamine with an acid. A salt of a cyanobenzylamine can industrially easily be produced and the resulting salt of a cyanobenzylamine has a high bulk density.Type: GrantFiled: June 7, 2001Date of Patent: May 21, 2002Assignee: Showa Denko K.K.Inventors: Isao Yamagami, Hiroshi Yasuda, Masatoshi Murakami, Toru Yoshida
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Publication number: 20020040003Abstract: Disclosed are compounds of the Formula I 1Type: ApplicationFiled: July 5, 2001Publication date: April 4, 2002Inventors: Laurence E. Burgess, John J. Gaudino, Robert D. Groneberg, Mark H. Norman, Martha E. Rodriguez, Xicheng Sun, Eli M. Wallace
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Publication number: 20020038045Abstract: Novel hydroxamic acid compounds, e.g.Type: ApplicationFiled: October 9, 2001Publication date: March 28, 2002Inventors: Georg Kottirsch, Ulf Neumann