Benzene Ring In A Substituent E Patents (Class 564/218)
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Publication number: 20150045580Abstract: Selectively fluorinated molecules are important as materials, pharmaceuticals, and agrochemicals, but their synthesis by simple, mild, laboratory methods is challenging. We report a straightforward method for the cross-coupling of a difluoromethyl group with readily available reagents to form difluoromethylarenes. The reaction of electron-neutral, electronrich, and sterically hindered aryl and vinyl iodides with the combination of Cul, CsF and TMSCF2H leads to the formation of difluoromethylarenes in high yield with good functional group compatibility. This transformation is surprising, in part, because of the prior observation of the instability of CuCF2H.Type: ApplicationFiled: March 5, 2013Publication date: February 12, 2015Inventors: John Hartwig, Patrick Fier
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Publication number: 20150011749Abstract: Metal-accumulating plants for preparing compositions including a metal catalyst derived from the plants. The composition is substantially devoid of organic matter. Also, carrying out chemical reactions with the compositions prepared from metal-accumulating plants.Type: ApplicationFiled: March 5, 2013Publication date: January 8, 2015Applicants: UNIVERSITE MONTPELLIER 2 SCIENCES ET TECHNIQUES, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Claude Grison, Vincent Escande
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Publication number: 20140235565Abstract: The present invention provides N-alkylthio ?-lactams and disulfide compounds (e.g., alkyl-coenzyme A asymmetric disulfides or aryl-alkyl disulfides), compositions containing such compounds, and methods of their use as anti-bacterial agents.Type: ApplicationFiled: May 1, 2014Publication date: August 21, 2014Applicant: UNIVERSITY OF SOUTH FLORIDAInventors: EDWARD TUROS, KEVIN D. REVELL
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Patent number: 8722929Abstract: This invention provides compounds of formula A and formula B which are modulators of potassium ion channels and are useful for the treatment of seizure disorders.Type: GrantFiled: October 10, 2007Date of Patent: May 13, 2014Assignee: Valeant Pharmaceuticals InternationalInventors: Jean-Michel Vernier, Jianlan Song, Huanming Chen, Zhi Hong
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Patent number: 8680333Abstract: The invention relates to a process for the preparation of formamides by reacting aromatic amines with a formic acid ester in the presence of a catalyst, wherein the catalyst is a phosphorus-containing acid or a Lewis-acidic metal salt.Type: GrantFiled: December 1, 2010Date of Patent: March 25, 2014Assignee: BASF SEInventors: Axel Franzke, Torsten Mattke, Julia Leschinski, Radwan Abdallah, Michael Bock, Robert Baumann, Eckhard Stroefer
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Publication number: 20130303621Abstract: This invention provides a composition comprising Formula I, or salt thereof, wherein X is either chlorine or bromine, Y is either hydrogen or an alkyl group having a carbon chain length from 1 to 5 carbon atoms, and R is an alkyl group having a carbon chain length from 1 to 5 carbon atoms, except that X is not chlorine when Y is hydrogen and R is an ethyl group. A method of preventing bone erosion in a patient and a method of reducing inflammation in a patient using the compositions of Formula I are disclosed.Type: ApplicationFiled: April 17, 2013Publication date: November 14, 2013Inventor: John B. Barnett
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Publication number: 20130281664Abstract: The present invention relates to novel Ruthenium catalysts and related borohydride complexes, and the use of such catalysts, inter alia, for (1) hydrogenation of amides (including polyamides) to alcohols and amines; (2) preparing amides from alcohols with amines (including the preparation of polyamides (e.g., polypeptides) by reacting dialcohols and diamines and/or by polymerization of amino alcohols); (3) hydrogenation of esters to alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones) or polyesters); (4) hydrogenation of organic carbonates (including polycarbonates) to alcohols and hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (5) dehydrogenative coupling of alcohols to esters; (6) hydrogenation of secondary alcohols to ketones; (7) amidation of esters (i.e.Type: ApplicationFiled: October 11, 2011Publication date: October 24, 2013Inventors: David Milstein, Ekambaram Balaraman, Chidambaram Gunanathan, Boopathy Gnanaprakasam, Jing Zhang
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Patent number: 8487109Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R1; R2; R3; R4; R5; J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process for aryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional aryl-1-alkynes of the formula I.Type: GrantFiled: December 23, 2009Date of Patent: July 16, 2013Assignee: SanofiInventors: Omar Rkyek, Marc Nazare, Andreas Lindenschmidt, Matthias Urmann, Nis Halland, Jorge Alonso
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Publication number: 20130053417Abstract: The invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity, the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.Type: ApplicationFiled: March 21, 2012Publication date: February 28, 2013Applicant: JAPAN TOBACCO INC.Inventors: Hisashi Shinkai, Kimiya Maeda, Hiroshi Okamoto
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Patent number: 8378143Abstract: The present invention provides a process for the preparation of Efavirenz. A compound of Formula 1: may be prepared by a process comprising cyclizing, in the presence of a first base, a compound of Formula 5 with a haloformate of Formula 6. Other processes are also provided as well as novel compounds prepared by and used in such processes.Type: GrantFiled: December 19, 2011Date of Patent: February 19, 2013Assignee: Apotex Pharmachem Inc.Inventors: Bo Chen, Zhi-Xian Wang, Yutao Xue, Lihong Liu, Hao Chen
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Patent number: 8362024Abstract: This invention relates to novel purinyl derivatives of formula Ia or Ib Wherein the symbols are as defined in the Specification and of pharmaceutically acceptable salts thereof useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels, for the preparation of a medicament for such treatment and to pharmaceutical compositions containing such compounds.Type: GrantFiled: March 27, 2008Date of Patent: January 29, 2013Assignee: NeuroSearch A/SInventors: Birgitte L. Eriksen, Ulrik Svane Sørensen, Charlotte Hougaard, Dan Peters, Tina Holm Johansen, Palle Christophersen
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Publication number: 20120296090Abstract: Disclosed are systems biology-based methods for repositioning known pharmaceutical compounds to new indications, through the identification of network-based signatures. In particular, the invention provides new and useful methods for selecting drugs or combinations of drugs (and preferably previously-approved drugs) for use in new therapeutic indications. Also disclosed are methods for identifying anti-breast tumor initiating cell (TIC)-based therapeutics from within populations of target compounds. In illustrative embodiments, the invention provides methods and computer programs for the repositioning of FDA-approved pharmaceutical compounds to new indications using network-based signature analysis coupled with conventional in vitro and in vivo testing of identified drug candidates. The invention also allows identification of drugs or drug combinations for treating unmet medical needs including, for example, “orphan” diseases.Type: ApplicationFiled: April 4, 2012Publication date: November 22, 2012Applicant: The Methodist Hospital Research InstituteInventors: Stephen TC Wong, Hong Zhao, Guangxu Jin
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Publication number: 20120253072Abstract: The invention relates to a process for the preparation of formamides by reacting aromatic amines with a formic acid ester in the presence of a catalyst, wherein the catalyst is a phosphorus-containing acid or a Lewis-acidic metal salt.Type: ApplicationFiled: December 1, 2010Publication date: October 4, 2012Applicant: BASF SEInventors: Axel Franzke, Torsten Mattke, Julia Leschinski, Radwan Abdallah, Michael Bock, Robert Baumann, Eckhard Stroefer
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Publication number: 20120245388Abstract: There are provided a 4-(trichloromethylthio)aniline represented by the general formula (II): wherein R1 represents a hydrogen atom or an alkyl group having 1 to 3 carbon atoms, R2 each independently represents a halogen atom, an alkyl group having 1 to 3 carbon atoms, or a perfluoroalkyl group having 1 to 3 carbon atoms, R3 represents a formyl group, an acetyl group, or a trifluoroacetyl group, and m represents an integer of 0 to 4, a method for producing the same, and a method for producing a 4-(trifluoromethylthio)aniline derivative using the 4-(trichloromethylthio)aniline. It becomes possible to produce a 4-(trifluoromethylthio)aniline with a high yield by using raw materials that can easily be obtained industrially and using general purpose production facilities.Type: ApplicationFiled: June 8, 2012Publication date: September 27, 2012Inventors: Yoshitomo TOHYAMA, Kengo Kanematsu
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Patent number: 8268838Abstract: Provided are substituted purinyl-pyrazol derivatives of the following formula (I), or a pharmaceutically acceptable salt thereof, and their use as potassium channel modulating agents, as well as pharmaceutical compositions having such derivatives that are useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels: wherein R1 represents hydrogen or alkyl; one of R2, R3 and R4 represents alkyl, hydroxy-alkyl, alkoxy-alkyl, halo, trifluoromethyl, trifluoromethoxy, hydroxy or alkoxy; and the other two of R2, R3 and R4, independently of each other, represent hydrogen, alkyl, hydroxy-alkyl, alkoxy-alkyl, halo, trifluoromethyl, trifluoromethoxy, hydroxy or alkoxy; R5 represents phenyl optionally substituted with one or more substituents selected from the group consisting of alkyl, halo, trifluoromethyl, trifluoromethoxy, alkoxy and cyano; and R6 represents R?OC(?O)—, wherein R? represents alkyl, alkoxy, alkoxy-alkyl or adamantanyl.Type: GrantFiled: September 22, 2009Date of Patent: September 18, 2012Assignee: Neurosearch A/SInventors: Birgitte L. Eriksen, Charlotte Hougaard, Dan Peters, Palle Christophersen
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Patent number: 8163903Abstract: The present invention relates to a new process for the preparation of N-[5-(3-dimethylamino-acryloyl)-2-fluorophenyl]-N-methyl-acetamide (I) in a high yield and high purity, which is an intermediate in the synthesis of compounds with affinity for GABAA receptor. In this process, N-(5-acetyl-2-fluorophenyl)-N-methyl-acetamide (VI) is reacted with an excess of N,N-dimethylformamide dimethyl acetal (NNDMF-DMA). The present invention also provides a new process for the preparation of a compound with affinity for GABAA receptor, N-{2-fluoro-5-[3-(thiophene)-2-carbonyl-pyrazolo[1,5-a]pyrimidin-7-yl]phenyl}-N-methyl-acetamide (II), which comprises the following steps: a) methylation of N-(5-acetyl-2-fluorophenyl)-N-acetamide (IV) with a methyl sulfonate, b) reaction of the resulting compound (VI) with NNDMF-DMA, and c) reaction of the resulting compound (I) with (5-amino-1H-pirazol-4-yl)thiophen-2-yl-methanone (III) in glacial acetic acid. The present invention also relates to new intermediate (VI).Type: GrantFiled: January 11, 2010Date of Patent: April 24, 2012Assignee: Interquim, S.A.Inventors: Juan Sallares Rosell, Francisco Marquillas
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Publication number: 20120095249Abstract: The present invention provides a process for the preparation of Efavirenz. A compound of Formula 1: may be prepared by a process comprising cyclizing, in the presence of a first base, a compound of Formula 5 with a haloformate of Formula 6. Other processes are also provided as well as novel compounds prepared by and used in such processes.Type: ApplicationFiled: December 19, 2011Publication date: April 19, 2012Applicant: APOTEX PHARMACHEM INC.Inventors: Bo CHEN, Zhi-Xian WANG, Yutao XUE, Lihong LIU, Hao CHEN
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Publication number: 20110319636Abstract: The present invention relates to a method for preparation of carboxamides using alcohols and amines as starting materials in a dehydrogenative coupling reaction catalyzed by a ruthenium N-heterocyciic carbene (NHC) complex, which may be prepared in situ.Type: ApplicationFiled: November 23, 2009Publication date: December 29, 2011Inventors: Lars Ulrik Nordstrom, Henning Vogt, Robert Madsen, Johan Hygum Dam
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Patent number: 8067648Abstract: A phenyl tin compound is synthesized by using a derivative having various functional groups and a bromo- or iodo-benzene ring as a labeling material of a radioactive ligand. On the other hand, a novel hydroxytosyl iodobenzene compound having an electron-donating group is obtained by oxidizing iodobenzene having one or more electron-donating groups and reacting it with tosylic acid. Then, a diphenyliodonium salt which is a labeling precursor is synthesized by reacting the resulting compound with various phenyl tin compounds. Finally, a 18F-labeled ligand having various functional groups and a [18F] fluorobenzene ring is synthesized by reacting the resulting diphenyliodonium salt with [18F]F?.Type: GrantFiled: November 29, 2006Date of Patent: November 29, 2011Assignee: National Institute of Radiological SciencesInventors: Kazutoshi Suzuki, Ming-Rong Zhang, Katsushi Kumata
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Publication number: 20110275809Abstract: The present invention relates to a new process for the preparation of N-[5-(3-dimethylamino-acryloyl)-2-fluorophenyl]-N-methyl-acetamide (I) in a high yield and high purity, which is an intermediate in the synthesis of compounds with affinity for GABAA receptor. In this process, N-(5-acetyl-2-fluorophenyl)-N-methyl-acetamide (VI) is reacted with an excess of N,N-dimethylformamide dimethyl acetal (NNDMF-DMA). The present invention also provides a new process for the preparation of a compound with affinity for GABAA receptor, N-{2-fluoro-5-[3-(thiophene)-2-carbonyl-pyrazolo[1,5-a]pyrimidin-7-yl]phenyl}-N-methyl-acetamide (II), which comprises the following steps: a) methylation of N-(5-acetyl-2-fluorophenyl)-N-acetamide (IV) with a methyl sulfonate, b) reaction of the resulting compound (VI) with NNDMF-DMA, and c) reaction of the resulting compound (I) with (5-amino-1H-pirazol-4-yl)thiophen-2-yl-methanone (III) in glacial acetic acid. The present invention also relates to new intermediate (VI).Type: ApplicationFiled: January 11, 2010Publication date: November 10, 2011Inventors: Juan Sallares Rosell, Francisco Marquillas
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Patent number: 8039669Abstract: The invention provides methods and reagents for the metathesis of secondary amides via a transacylation mechanism employing catalytic quantities of an imide initiator and a Brønsted base. Equilibrium-controlled exchange between various amide reactant pairs is demonstrated for substrates bearing a variety of N-alkyl and N-aryl substituents.Type: GrantFiled: December 1, 2008Date of Patent: October 18, 2011Assignee: Wisconsin Alumni Research FoundationInventors: Christen Bell Smith, Denis A. Kissounko, Samuel H. Gellman, Shannon S. Stahl
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Publication number: 20110200549Abstract: Disclosed are compounds having the ability to modulate, namely to improve, enhance and/or modify fragrance compositions due to their ability to inhibit cytochrome P450 enzymes, e.g. CYP2A, e.g. 2A13 and 2A6, and CYP2B6.Type: ApplicationFiled: September 29, 2009Publication date: August 18, 2011Inventors: Thierry Granier, Boris Schilling
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Publication number: 20110178199Abstract: Disclosed herein are a reaction method and a production method of an organic compound which are capable of achieving high reaction selectivity according to the purpose and a high production rate of a target substance. The methods include at least two fluids, wherein at least one kind of the fluids is a fluid containing at least one organic compound and at least one kind of the fluids other than the above fluid is a fluid containing at least one reactant in the form of a liquid or solution, and the respective fluids join together in a thin film fluid foamed between processing surfaces arranged to be opposite to each other so as to be able to approach to and separate from each other, at least one of which rotates relative to the other, whereby an organic reaction is performed in the thin film fluid.Type: ApplicationFiled: September 11, 2008Publication date: July 21, 2011Applicant: M. Technique Co., Ltd.Inventor: Masakazu Enomura
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Patent number: 7951602Abstract: Mass defect labeled peptides and methods of identifying peptides are provided. In particular, embodiments of the present disclosure include mass defect labels for polypeptides that include at least one cysteine and/or at least one tryptophan and methods of using the mass defect labels to identify polypeptides. One embodiment, among others, includes a mass defect labeled peptide including at least one cysteine residue labeled with 2,4-dibromo-acetanilide. Another embodiment, among others, includes a mass defect labeled peptide including at least one tryptophan residue labeled with 4,6-dibromo-2-trifluoromethylphenylsulfenyl chloride.Type: GrantFiled: August 28, 2007Date of Patent: May 31, 2011Assignee: University of Georgia Research Foundation, Inc.Inventors: I. Jonathan Amster, Robert S. Phillips
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Patent number: 7932416Abstract: Pentafluorosulfanyl-benzenes according to Formula (I): a process for their preparation and their use as valuable synthetic intermediates for preparing, for example, medicaments, diagnostic aids, liquid crystals, polymers, pesticides, herbicides, fungicides, nematicides, parasiticides, insecticides, acaricides and arthropodicides.Type: GrantFiled: December 13, 2007Date of Patent: April 26, 2011Assignee: Sanofi-Aventis Deutschland GmbHInventors: Heinz-Werner Kleemann, Remo Weck
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Publication number: 20110003959Abstract: The invention relates to a coordination complex system comprising a ligand having the formula: R1—SO2—NH—P (XR2)2 (1a); or R1—SO2—N?PH (XR2)2 (1b); or R1—SO(OH)?N—P(XR2)2 (1c); wherein X is independently O, S, NH, or a bond; R1 and R2 are independently selected from hydrogen and substituted or unsubstituted alkyl or aryl; wherein at least one equivalent of the ligand is complexed to an equivalent of a metal selected from a transition metal and lanthanide. The invention also relates to the use of said coordination complexes as catalysts in the hydroformylation, hydrogenation, transfer hydrogenation, hydrocyanation, polymerization, isomerization, carbonylation, cross-coupling, metathesis, CH activation, allylic substitution, aldol condensation, or Michael addition.Type: ApplicationFiled: November 19, 2008Publication date: January 6, 2011Inventors: Joost Nikolaas Hendrik Reek, Frederic William Patureau, Mark Kuil, Albertus Jacobus Sandee, Jurjen Meeuwissen
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Publication number: 20100331566Abstract: The invention provides synthetic methods that utilize bromo or chloro substituents as blocking groups during the functionalization of aromatic rings, as well as compounds that are prepared from such methods.Type: ApplicationFiled: June 25, 2010Publication date: December 30, 2010Inventors: Leslie S. Jimenez, Ahalya Ramanathan
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Patent number: 7858784Abstract: Ligands for transition metals are disclosed herein, which may be used in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The disclosed methods provide improvements in many features of the transition-metal-catalyzed reactions, including the range of suitable substrates, number of catalyst turnovers, reaction conditions, and efficiency. For example, improvements have been realized in transition-metal-catalyzed cross-coupling reactions.Type: GrantFiled: December 12, 2008Date of Patent: December 28, 2010Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Brett P. Fors, David S. Surry
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Publication number: 20100286106Abstract: Treating and/or preventing prostate problems and/or metastases, by selectively occluding various groin vessels and tools for selective occluding of various groin veins, including, for example, the deferential vein. Optionally providing anti-androgen treatment after such occluding.Type: ApplicationFiled: July 13, 2008Publication date: November 11, 2010Inventors: Yigal Gat, Menachem Goren
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Publication number: 20100261910Abstract: The present invention relates to a process for the regioselective synthesis of compounds of the formula (I), wherein R1; R2; R3; R4; R5; J and W have the meanings indicated in the claims. The present invention provides an efficient and general palladium-catalyzed coupling process for aryl tosylates with terminal alkynes to a wide variety of substituted, multifunctional aryl-1-alkynes of the formula I.Type: ApplicationFiled: December 23, 2009Publication date: October 14, 2010Applicant: sanofi-aventisInventors: Omar RKYEK, Marc NAZARE, Andreas LINDENSCHMIDT, Matthias URMANN, Nis HALLAND, Jorge ALONSO
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Publication number: 20100234472Abstract: The present invention particularly relates to novel nitrate esters of paracetamol. The nitrate esters of paracetamol are prepared by reacting the paracetamol with dihaloalkyl compound and followed by reaction with silver nitrate to obtain the corresponding nitrate ester derivatives. The nitrate esters of paracetamol are useful as analgesic, anti-inflammatory agents.Type: ApplicationFiled: February 17, 2010Publication date: September 16, 2010Inventors: Tilak Raj BHARDWAJ, Manoj Kumar, Neeraj Mehta, Neelima Dhingra
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Patent number: 7754920Abstract: This invention relates to an improved method for crystallizing 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (“Compound A”), an intermediate in the industrial preparation of non-ionic X-ray contrast agents. In particular, the present invention provides an industrial process for crystallization of Compound A by evaporating methanol and water from the mother liquor after an initial crystallization of Compound A following the acetylation reaction. Specifically, the mother liquor is maintained at more than about 75% (v/v) of water and less than about 25% (v/v) of alcoholic solvent.Type: GrantFiled: November 18, 2009Date of Patent: July 13, 2010Assignee: GE HealthCare ASInventors: Lars Terje Holmaas, Kristin Rypestol
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Publication number: 20100160683Abstract: There is provided a novel process for production of a 2-(substituted phenyl)-3,3,3-trifluoropropene. Disclosed is a process for production of a 2-(substituted phenyl)-3,3,3-trifluoropropene compound represented by the formula (7) or a salt thereof The process comprises reacting a compound represented by the formula (1) (X is an alkyl group, etc.) with a compound represented by the formula (2) (Y is a halogen atom, etc.Type: ApplicationFiled: February 13, 2007Publication date: June 24, 2010Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Kazutaka Matoba, Takashi Mizukoshi, Yuji Moriyama
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Publication number: 20100063044Abstract: The present invention relates to aniline derivatives of formula I: wherein R1, R2, R3, R4, Z and q are as defined herein; or salts thereof and their use.Type: ApplicationFiled: August 17, 2009Publication date: March 11, 2010Applicant: H. Lundbeck A/SInventors: Christian Wenzel Tornoe, Mario Rottlãnder, Daniel Rodriguez Greve, Nikolay Khanzhin, Andreas Ritzén, William Patrick Watson
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Patent number: 7601869Abstract: The present invention relates to a method for the preparation of Florfenicol from Fluoroamine compound, namely (1R,2S)-1-[4-(methylsulfonyl)phenyl]-2-amino-3-fluoro-1-propanol (II), by reaction with dihaloacetic acid ester in an organic solvent in presence of an inorganic base.Type: GrantFiled: June 12, 2006Date of Patent: October 13, 2009Assignee: Aurobindo Pharma Ltd.Inventors: Mallikarjuna Reddy Karuru, Arun Kumar Gupta, Sivakumaran Meenakshisunderam
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Publication number: 20090221820Abstract: Ligands for transition metals are disclosed herein, which may be used in various transition-metal-catalyzed carbon-heteroatom and carbon-carbon bond-forming reactions. The disclosed methods provide improvements in many features of the transition-metal-catalyzed reactions, including the range of suitable substrates, number of catalyst turnovers, reaction conditions, and efficiency. For example, improvements have been realized in transition-metal-catalyzed cross-coupling reactions.Type: ApplicationFiled: December 12, 2008Publication date: September 3, 2009Applicant: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Brett P. Fors, David S. Surry
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Publication number: 20090216046Abstract: This invention is directed to a method of selectively acylating a compound of formula (II): (II), wherein: R1 is NO2, —N+R33, trihalomethyl, —CN, —SO3H, —CO2H, —CO2 R3, —CHO and —COR3, wherein R3 is C1-C6 alkyl, C1-C6 haloalkyl, C3-C12 cycloalkyl, C6-C12 aryl, C2-C9 heteroaryl, or C1-C9 heterocycloalkyl; comprising the step of reacting the compound of formula (II) with an acylating reagent to form a compound of formula (I): (I), wherein R2 is selected from C1-C12 alkyl, C1-C12 haloalkyl, C2-C7 alkenyl, C2-C7 alkynyl, C3-C12 cycloalkyl, C6-C12 aryl, C1-C9 heterocycloalkyl, C2-C9 heteroaryl, C1-C12 alkoxy, C1-C12 haloalkoxy, C3-C12 cycloalkoxy, C1-C9 heterocycloalkoxy, C6-C12 aryloxy, and C2-C9 heteroaryloxy; or salts thereof.Type: ApplicationFiled: October 12, 2006Publication date: August 27, 2009Applicant: WYETHInventor: Ronald Stanley Michalak
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Patent number: 7560591Abstract: Compounds which can be represented by the general formula (I) indicated below: and in which: A is selected independently from the carboxamide group, the thiocarboxamide group, and the carbonyl group, R1 is selected from an alkyl group having from 1 to 3 carbon atoms and the amino group, unsubstituted or substituted with the nitro group or the methyl group, R2 is selected independently from hydrogen, an alkyl group having from 1 to 4 carbon atoms, the methoxy, ethoxy, propoxy group, a mono-, bi- or tricyclic cycloalkane residue having from 5 to 12 carbon atoms, the adamantyl group, an aryl, naphthyl or heterocyclic group, unsubstituted or substituted with methyl, methoxy, hydroxy, amino or halogen groups, R3 and R4 are selected independently from hydrogen and an alkyl group having from 1 to 3 carbon atoms, R5 represents one or two substituents independently selected from hydrogen and the methyl, methoxyl and hydroxyl groups, n is a whole number from 0 to 6, and the amidine group is in the para or meta pType: GrantFiled: April 30, 2008Date of Patent: July 14, 2009Assignee: Rotta Research Laboratorium S.p.A.Inventors: Francesco Makovec, Simona Zanzola, Roberto Artusi, Lucio Claudio Rovati
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Patent number: 7553993Abstract: Process for the preparation of a compound of general formula (I): in which X represents a halogen atom, by reaction of para-trifluoromethylaniline of formula (II): with a dihalogen X2, the two compounds being introduced simultaneously into a polar aprotic solvent in a dihalogen/compound (II) molar ratio ranging from 1.9 to 2.5 and at a temperature ranging from 100 to 300° C.Type: GrantFiled: October 24, 2003Date of Patent: June 30, 2009Assignees: BASF Agro B.V., Wadenswil/AUInventors: Bernard Buathier, Pierre Le Roy
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Patent number: 7452995Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: April 7, 2005Date of Patent: November 18, 2008Assignee: Theravance, Inc.Inventors: Edmund J. Moran, John R. Jacobsen, James Aggen
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Patent number: 7411091Abstract: This invention is related to compounds and use of N-Acyl-N?-benzyl-alkylendiamino derivatives of the following general formula (I), wherein A is a straight or branched C2-C8 alkyl chain; X is a methylene, oxygen, sulphur or a NR7 group; R1 is a straight or branched C1-C8 alkyl or C3-C8 alkenylene or C3-C8 alkynylene chain, optionally substituted with CF3, phenyl, phenoxy or naphthyl, the aromatic rings optionally substituted by one or more C1-C4 alkyl, halogens, trifluoromethyl, hydroxy or C1-C4 alkoxy groups; R2, R3 are independently hydrogen, a C1-C3 alkyl chain, halogen, trifluoromethyl, hydroxy or C1-C4 alkoxy groups; R4, R5 are independently hydrogen or C1-C6 alkyl; R6 is a hydrogen or a straight or branched C1-C8 alkyl or linked to R5 can form a five to seven membered lactam; R7 is hydrogen or C1-C6 alkyl; and the pharmaceutically acceptable salts thereof that are active as sodium and/or calcium channel modulators and therefore useful in preventing, alleviating and curing a wide range of pathologies, inType: GrantFiled: November 12, 2004Date of Patent: August 12, 2008Assignee: Newron Pharmaceuticals S.p.A.Inventors: Florian Thaler, Cibele Maria Sabido David, Laura Faravelli, Stefania Gagliardi, Elena Colombo, Patricia Salvati
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Publication number: 20080064884Abstract: The present invention relates to a novel process for the preparation of compounds of formula (I) wherein X, Q, R1 and R2 are as defined in the specification, the compounds being useful in the preparation of therapeutic agents. The invention further relates to novel intermediates useful in the preparation of the therapeutic agents.Type: ApplicationFiled: May 3, 2007Publication date: March 13, 2008Applicant: AstraZeneca ABInventors: Debra Ainge, Philip Cornwall, Duncan Michael Gill, Vinod Kumar, Luis Manuel Vaz, Philip O'Keefe, Rhona Sinclair, Edward Laurence Way
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Patent number: 7268252Abstract: Disclosed herein are novel binaphthol derivatives and methods for the optical resolution of amino acids or amino alcohols and for the optical transformation of D, L-forms of amino acids using the same.Type: GrantFiled: January 30, 2006Date of Patent: September 11, 2007Assignee: Green of Life Co., Ltd.Inventors: Kwan Mook Kim, Won Woo Nam, Hyun Jung Park, Jik Chin
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Patent number: 7268255Abstract: N-Aryl or N-heteroarylformamides are prepared by hydrogenating a corresponding nitroarene or nitroheteroarene with formic acid and/or ammonium formate as hydrogen donor and formylating agent in the presence of at least one noble metal-based hydrogenation catalyst and a vanadium or molybdenum compound as co-catalyst.Type: GrantFiled: February 19, 2004Date of Patent: September 11, 2007Assignee: Lonza AGInventors: Ulrich Kampfen, Dario Veghini, Dominique Roberge, Jared Randall
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Patent number: 7041852Abstract: The present invention relates to a process for preparing perfluoroalkylanilines and to their use for preparing active ingredients, in particular for agrochemicals.Type: GrantFiled: November 6, 2003Date of Patent: May 9, 2006Assignee: Bayer Chemicals AGInventors: Albrecht Marhold, Axel Pleschke
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Patent number: 6946462Abstract: New compounds represented by the formula or pharmaceutically acceptable salts or prodrugs thereof, wherein X1 and X2 are each independently selected from a CH group or a nitrogen atom; and R is an optionally substituted five or six membered nonaromatic carbocyclic ring or a nonaromatic or aromatic heterocyclic ring, whereby the ring is optionally condensed with a 6-membered, optionally substituted carbocyclic aromatic ring.Type: GrantFiled: April 13, 2004Date of Patent: September 20, 2005Assignee: Hoffmann-La Roche Inc.Inventors: Rainer Haag, Ulrike Leser-Reiff, Anja Limberg, Michael Weidner, Gerd Zimmermann
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Patent number: 6870069Abstract: A phenyloxyaniline derivative useful as a ligand for peripheral benzodiazepine receptor having a strong affinity and a high selectivity, which is represented by formula (1): wherein X1 and X2 are same or different and each is hydrogen atom or halogen atom; R1 and R2 are same or different and each is hydrogen atom, an alkyl group having 1 to 10 carbon(s) or a halogen-substituted alkyl group having 1 to 10 carbon(s); and R3 is a halogen-substituted alkyl group having 1 to 5 carbon(s), or a radioisotope thereof.Type: GrantFiled: November 4, 2003Date of Patent: March 22, 2005Assignees: National Institute of Radiological Sciences, Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co., Ltd.Inventors: Kazutoshi Suzuki, Ming-Rong Zhang, Tetsuya Suhara, Atsuro Nakazato, Makoto Goto
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Patent number: 6869953Abstract: New compounds represented by the formula or pharmaceutically acceptable salts or prodrugs thereof, wherein X1 and X2 are each independently selected from a CH group or a nitrogen atom; and R is an optionally substituted five or six membered nonaromatic carbocyclic ring or a nonaromatic or aromatic heterocyclic ring, whereby the ring is optionally condensed with a 6-membered, optionally substituted carbocyclic aromatic ring.Type: GrantFiled: August 6, 2002Date of Patent: March 22, 2005Assignee: Hoffman-La Roche Inc.Inventors: Rainer Haag, Ulrike Leser-Reiff, Anja Limberg, Michael Weidner, Gerd Zimmermann
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Patent number: 6864246Abstract: The invention concerns more particularly dodecylthio-phenylacetanilide derivative complexes such as (S)-2?,3?,5?-trimethyl-4?-hydroxy-?-dodecylthio-phenylacetanilide or related derivatives thereof and cyclodextrins.Type: GrantFiled: April 9, 2002Date of Patent: March 8, 2005Assignee: Pierre Fabre MedicamentInventors: Joël Bougáret, Elie Leverd, Marie-Dominique Ibarra, Alexandre Gil
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Patent number: 6855847Abstract: A novel process for producing an optically active amide excellent in chemical selectivity and enantioselectivity by asymmetric hydrogenation of an ?,?-unsaturated amide and also allowing the reaction to proceed efficiently even when a trace amount of a catalyst is used relative to the substrate as compared with the amount in a conventional process. An optically active amide is produced by asymmetric hydrogenation of an ?,?-unsaturated amide derivative in the presence of a transition metal complex containing a specific phosphine-phosphorane compound.Type: GrantFiled: July 22, 2002Date of Patent: February 15, 2005Assignee: Takasago International CorporationInventors: Kazuhiko Matsumura, Takao Saito