Quinolines Which Are Unsubstituted Or Which Are Alkyl Or Alkenyl Substituted Only, Or Salt Thereof Patents (Class 546/181)
-
Patent number: 9688589Abstract: Disclosed is a process for preparation of n-propyl benzene. The process gives high selectivity and yield of n-propyl benzene by single step catalytic alkylation that involves contacting a mixture of aromatic hydrocarbon having an active hydrogen on a saturated ?-carbon, such as toluene, and an alkene, such as ethylene, in presence of a metal catalyst, a solid support, and an initiator. Following the alkylation, aqueous and organic phases are separated from a reaction mixture. The aqueous phase is separated for recovery of the catalyst, the solid support, and un-reacted aromatic hydrocarbon (e.g., toluene); and the organic phase is separated for obtaining n-propyl benzene and byproduct. Thus, the catalyst phase can be recovered and recycled in the next alkylation reaction. Also, the process facilitates recovery and recycling of the byproduct for the better selectivity.Type: GrantFiled: December 8, 2014Date of Patent: June 27, 2017Assignee: VINATI ORGANICS LIMITEDInventors: Prashant Purushottam Barve, Jayesh Ajitkumar Ashar
-
Patent number: 9499517Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.Type: GrantFiled: February 12, 2014Date of Patent: November 22, 2016Assignee: Eolas Therapeutics, Inc.Inventors: Theodore M. Kamenecka, Yuanjun He, William Nguyen, Rong Jiang, Xinyi Song, Robert Jason Herr, Qin Jiang
-
Publication number: 20150094468Abstract: The present invention relates to a novel diamine compound represented by the general formula (1), a ruthenium-diamine complex, an iridium-diamine complex, and a rhodium-diamine complex having the diamine compound as a ligand. Furthermore, the present invention relates to methods for selectively producing optically active compounds by using any of these complexes as a catalyst. wherein R1, R2, R3, X, Y, and Z are as defined in claim 1.Type: ApplicationFiled: September 26, 2014Publication date: April 2, 2015Applicant: TAKASAGO INTERNATIONAL CORPORATIONInventor: Taichiro TOUGE
-
Patent number: 8940499Abstract: The present disclosure provides a reagent for blood analysis which may include: (1) a compound having the general formula I as a fluorescent dye, wherein n, X, R1, R2, R3, R4, R5 and Y? are as defined in the specification; (2) a surfactant selected from cationic surfactants, zwitterionic surfactants and anionic surfactants. The present disclosure also provides a method to perform blood analysis including the following steps of: (a) mixing the blood sample with the reagent for blood analysis disclosed to form a cell suspension; (b) detecting the scattered light signals and fluorescence signals from the cells; and (c) differentiating and counting the cells in the blood in terms of the scattered light signals and fluorescence signals.Type: GrantFiled: October 16, 2009Date of Patent: January 27, 2015Assignee: Shenzhen Mindray Bio-Medical Electronics Co., Ltd.Inventors: Yuji Kuang, Baohua Zhang, Bing Xu, Jianhui Shao, Ting Lei, Li Zhang
-
Patent number: 8933231Abstract: Compounds of formula (I) wherein: n=0, 1, 2, 3, and R=C2-C6 linear and branched alkyl, alkenyl and cycloalkyl substituents are interesting flavor or fragrance ingredients having herbal-green aspects.Type: GrantFiled: June 22, 2011Date of Patent: January 13, 2015Inventors: Andreas Goeke, Li Jun Zhou
-
Publication number: 20140228572Abstract: Provided are a novel chiral iridium(III) complex; and a method for producing optically active 2-substituted-1,2,3,4-tetrahydroquinolines from 2-substituted-quinolines with the use of the chiral iridium(III) complex through a more economical and easy production process.Type: ApplicationFiled: July 13, 2012Publication date: August 14, 2014Applicant: HAMARI CHEMICALS, LTD.Inventors: Sadayuki Maeda, Tatsunori Sato, Yasuhiko Kawano, Toshio Miyawaki
-
Patent number: 8741897Abstract: Compounds of Formula (IA), (IB), (IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.Type: GrantFiled: September 22, 2004Date of Patent: June 3, 2014Assignee: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Younes Bekkali, Rajashekhar Betageri, Michel J. Emmanuel, Abdelhakim Hammach, Christian Hanke Justus Joachim Harcken, Thomas Martin Kirrane, Jr., Daniel Kuzmich, Thomas Wai-Ho Lee, Pingrong Liu, Usha R. Patel, John Robert Proudfoot, Hossein Razavi, Doris Riether, Hidenori Takahashi, David S. Thomson, Ji Wang, Renee Zindell
-
Patent number: 8476443Abstract: The present invention provides dyes and labeled reagents that may be used in the detection or quantification of desirable target molecules, such as proteins, nucleic acids and cellular organelles. Dyes are provided that may be used free in solution where the binding of the dye to the target molecule provides signal generation. Dyes provided in this invention can comprise reactive groups that may be used to attach the dyes to probes that will bind to desirable target molecules. The novel dyes of the present invention have been substituted with specific groups to provide beneficial properties.Type: GrantFiled: January 3, 2013Date of Patent: July 2, 2013Assignee: Enzo Life Sciences, Inc.Inventors: Praveen Pande, Hilary J. Cox, Yuejun Xiang, Wayne Forrest Patton
-
Patent number: 8450491Abstract: A method for the preparation of montelukast acid sodium salt thereof in amorphous form has been described. The method comprises of following steps: (a) generating the dilithium dianion of 1-(mercaptomethyl)cyclopropane acetic acid, by reacting with alkyl lithium, (b) coupling the said dianion with wet mesylate to get montelukast acid in crude form, (c) obtaining DCHA salt in crude form by adding dicyclohexylamine (DCHA) to crude acid obtained in the above step (b), (d) purifying and converting the said DCHA salt in crude form, to montelukast acid in pure form, and (e) reacting the pure montelukast acid in a polar protic solvent with a source of sodium ion followed by evaporating the solvent and triturating of the residue with non-polar water immiscible solvent.Type: GrantFiled: June 6, 2003Date of Patent: May 28, 2013Assignee: Morepen Laboratories LimitedInventors: Sanjay Suri, Jujhar Singh, Gurdeep Singh Sarin, Madan Pal Tanwar, Manu Mahendru
-
Publication number: 20130129655Abstract: Compounds of formula (I) wherein: n=0, 1, 2, 3, and R=C2-C6 linear and branched alkyl, alkenyl and cycloalkyl substituents are interesting flavour or fragrance ingredients having herbal-green aspects.Type: ApplicationFiled: June 22, 2011Publication date: May 23, 2013Applicant: Givaudan SAInventors: Andreas Goeke, Li Jun Zhou
-
Patent number: 8445511Abstract: The present invention relates to compounds of Formula (I) below, to their pharmaceutically acceptable salts and to their isomers or mixtures of isomers: HetAr—X—CHR1R2 (I) in which: —HetAr represents a group chosen from: —X represents a linear, saturated or unsaturated, hydrocarbon-based chain comprising from 8 to 22 carbon atoms, optionally interrupted by an —NH— or —NH—CO— group, —R1 represents a hydrogen atom or an —OH, —O(C1-C6)alkyl, —OCO((C1-C6)alkyl), —OSO2((C1-C6)alkyl) or —OSO3H group, and —R2 represents a hydrogen atom or a (C2-C6)alkynyl, (C2-C6)alkenyl or (C3-C6)cycloalkyl group. The present invention also relates to a process for preparing the compounds of Formula (I), and also to the use thereof, especially in the treatment of neurodegenerative diseases.Type: GrantFiled: July 20, 2009Date of Patent: May 21, 2013Assignee: Centre National de la Recherche Scientifique (SNRS)Inventors: Fanny Schmidt, Bruno Figadere, Sylvia Rita Vozari, Pierre Champy, Xavier Franck
-
Publication number: 20130116438Abstract: An object of the present invention is to provide a novel iridium complex, and to provide a novel catalyst having excellent performances in terms of enantioselectivity, catalytic activity, and the like. Provided is an iridium complex of the following general formula (1): IrHZ2(PP)(Q)m??(1) wherein Z represents a halogen atom, PP represents a bisphosphine, Q represents an amine, and m represents 1 or 2.Type: ApplicationFiled: August 30, 2011Publication date: May 9, 2013Applicant: TAKASAGO INTERNATIONAL CORPORATIONInventors: Hideo Shimizu, Hideki Nara
-
Patent number: 8383646Abstract: Disclosed herein is a compound of the formula (I) therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: May 21, 2008Date of Patent: February 26, 2013Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Todd M. Heidelbaugh, Ken Chow, Smita S. Bhat, Phong X. Nguyen, Michael E. Garst
-
Patent number: 8377573Abstract: Provided is a compound having a substituted pyridyl group and a pyridoindole ring structure linked through a phenylene group, having formula (1), and an organic EL device with a pair of electrodes and at least one organic layer interposed between the electrodes, wherein the at least one organic layer having the compound:Type: GrantFiled: January 30, 2009Date of Patent: February 19, 2013Assignee: Hodogaya Chemical Co., Ltd.Inventors: Norimasa Yokoyama, Shuichi Hayashi, Sawa Izumi, Shigeru Kusano
-
Patent number: 8257981Abstract: Novel chemical compounds, with application in fluorometric analytical methods, for qualitative and quantitative determination of biomolecules. The aim of the invention is to identify and prove the suitability of such compounds. Said aim is achieved with compounds of formula (1) where R1 is an antenna function, R2 is a chelate forming agent, containing a coordinated lanthanide(III)ion, X is —OH or a group with affinity for the biomolecule, bonded to a carboxylate group of the chelate forming agent by means of an amide bond and Y is —H or a group with affinity for the biomolecule, coupled to the antenna function.Type: GrantFiled: April 30, 2005Date of Patent: September 4, 2012Assignee: Sensient Imaging Technologies GmbHInventors: Jörg Marx, Frank Schumer, Regina Lischewski, Kornelia Zeckert, Hans-Joachim Böhme, Horst Hennig
-
Patent number: 8067602Abstract: Asymmetric cyanine fluorescent dyes are represented by general formula I. These kinds of dyes may be used as a staining agent for nucleic acids, with the spectra at 600-900 nm in the near-infrared region and without interference from background fluorescence. These kinds of dyes may be useful with small-type red semiconductor lasers as the light source (such as 633 nm). Compositions comprising these dyes and methods for staining biological samples using these dyes or compositions are also provided.Type: GrantFiled: December 12, 2008Date of Patent: November 29, 2011Assignee: Shenzhen Mindray Bio-Medical Electronics Co., Ltd.Inventor: Jianhui Shao
-
Publication number: 20110263849Abstract: Provided is a method whereby a heteroaromatic ring aryl can be very rapidly methylated at a high yield. In an N-alkyl-2-pyrrolidinone, a heteroaromatic ring aryltrialkylstannan is cross-coupled with methyl iodide in the presence of a palladium complex, a phosphine ligand, a cuprous halide, a carbonic acid salt and/or an alkali metal fluoride to thereby rapidly methylate the heteroaromatic ring aryl. (Formula shows a case wherein the heteroaromatic ring aryl is a pyridyl group.Type: ApplicationFiled: December 25, 2009Publication date: October 27, 2011Applicants: GIFU UNIVERSITY, RIKENInventors: Masaaki Suzuki, Hisashi Doi, Hiroko Koyama
-
Patent number: 7960553Abstract: A newly synthesized compound designated lepidine ether 2-(4-Methoxybenzyloxy)-4-methylquinoline reacts with methyl triflate in the presence of alcohols to generate a neutral organic salt that transfers the para-methoxybenzyl (PMB) protecting group onto alcohols in high yield and under mild conditions.Type: GrantFiled: October 2, 2007Date of Patent: June 14, 2011Assignee: Florida State University Research Founation, Inc.Inventor: Gregory B. Dudley
-
Publication number: 20110136242Abstract: Novel chemical compounds, with application in fluorometric analytical methods, for qualitative and quantitative determination of biomolecules. The aim of the invention is to identify and prove the suitability of such compounds. Said aim is achieved with compounds of formula (1) where R? is an antenna function, R2 is a chelate forming agent, containing a coordinated lanthanide(III)ion, X is —OH or a group with affinity for the biomolecule, bonded to a carboxylate group of the chelate forming agent by means of an amide bond and Y is —H or a group with affinity for the biomolecule, coupled to the antenna function.Type: ApplicationFiled: April 30, 2005Publication date: June 9, 2011Applicant: SENSIENT IMAGING TECHNOLOGIES GMBHInventors: Jorg Marx, Frank Schumer, Regina Lischewski, Kornelia Zeckert, Hans-Joachim Bohme, Horst Hennig
-
Patent number: 7956196Abstract: Novel 1,3-dihydro-benzimidazol-2-ylidene amine derivatives of formula the addition salts and stereochemically isomeric forms wherein each Alk is C1-6alkanediyl; Q is hydrogen; C1-6alkyl substituted with one or two Ar2 radicals; C1-6alkyl substituted with quinolinyl, oxazolidinyl, thiazolidinyl, morpholinyl, thiomorpholinyl, or with pyrrolidinonyl; —CO—Ar2; or Q is a radical of formula wherein t is 1, 2 or 3; R4 is amino, mono-or di(C1-6alkyl)amino; R1 is Ar2, —CO—Ar2 or a monocyclic or bicyclic heterocycle which may optionally be substituted; R2 is as R1 and additionally can be hydrogen; where Q is other than hydrogen, R3 is hydrogen; and where Q is other than hydrogen, R3 is a radical: wherein R6 is hydrogen, C1-6alkyl, substituted C1-6alkyl; R7, R8, R9 are halo, cyano, C1-6alkyl, substituted C1-6alkyl, C2-6alkenyl, cyanoC2-6alkenyl, C2-6alkynyl, cyanoC2 6alkynyl, Ar1, R10a—0—, R10a—S—, —N(R5aR5b), R10a—O—C(?O)—, N(R5aR5b)—C(?O)—, R10a—C(?O)—NR5b—, R10b—C(?O)—O—; and R8 and/or R9 may also beType: GrantFiled: March 17, 2006Date of Patent: June 7, 2011Assignee: Tibotec Pharmaceuticals Ltd.Inventors: Jean-François Bonfanti, Jérôme Michel Claude Fortin, Ismet Dorange
-
Publication number: 20110095282Abstract: The invention relates to organic electroluminescent devices which comprise triazine derivatives as the electron transport material.Type: ApplicationFiled: November 26, 2009Publication date: April 28, 2011Applicant: Merck Patent GmbHInventors: Christof Pflumm, Simone Leu, Joachim Kaiser, Amir Hossain Parham, Frank Voges, Jonas Valentin Kroeber, Arne Buesing
-
Patent number: 7875215Abstract: The invention provides a near-infrared-absorbing material comprising at least one first compound selected from the group consisting of a singlet oxygen scavenger, a radical trapping agent and an antioxidant and at least one second compound represented by the following formula (II-1) or (II-2).Type: GrantFiled: September 21, 2007Date of Patent: January 25, 2011Assignee: FUJIFILM CorporationInventors: Keizo Kimura, Katsuyoshi Yamakawa, Osama Uchida
-
Publication number: 20110003992Abstract: A quaternary nitrogen-containing corrosion inhibitor of formula wherein is an aromatic, nitrogen-containing ring of 5 to 14 ring atoms, optionally containing an additional N, O or S ring atom and optionally substituted with one or more alkyl, alkenyl, aryl, arylalkyl, cycloalkyl, amino, aminoalkyl, alkoxy, hydroxylalkyl, or cyano groups, or a mixture thereof; Y is a group of formula —OC(O)R1 or —C(O)R1; L is C1-C10 alkyl, C2-C10 alkenyl or a group of formula —CH2CH(OR2)CH2—; R1 is C8-C20 alkyl or C8-C20 alkenyl; R2 is H or —C(O)R1; R3 and R4 are independently selected from H, alkyl, alkenyl, amino, alkoxy, hydroxylalkyl and cyano; and X is Br, Cl or I is particularly useful for inhibiting corrosion in oil and gas field applications.Type: ApplicationFiled: September 15, 2010Publication date: January 6, 2011Inventor: Laxmikant Tiwari
-
Patent number: 7790894Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (I) and pharmaceutically acceptable addition salts thereof, wherein the variable moieties are as defined in the specification. The invention also relates to a method of treating of mycobacterial diseases through administration of the claimed compounds and a process for preparing the claimed compounds.Type: GrantFiled: June 5, 2006Date of Patent: September 7, 2010Assignee: Janssen Pharmaceutica NVInventors: Jérôme Emile Georges Guillemont, Elisabeth Therese Jeanne Pasquier, David Francis Alain Lancois
-
Patent number: 7696227Abstract: The present invention provides a method of inhibiting an androgen receptor by administering a compound of Formula I: or a compound of Formula II: wherein R1, R2, R3 and R8 are each independently hydrogen or C1-6 alkyl. R4 is absent or is hydrogen, C1-6 alkyl or C1-6 alkyl-OH. R5 is hydrogen, C1-6 alkyl or —NR6R7. R6 and R7 are each independently hydrogen or C1-6 alkyl, or are combined with the nitrogen to which they are attached to form a heterocycloalkyl having from 5 to 7 ring members. L is a linker of C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene or C3-6 cycloalkylene. The compounds of Formula I include the salts, hydrates and prodrugs thereof. Each R9 is H, C1-6 alkyl, —OH or —O—C1-6 alkyl. The compounds of Formulas I and II include the salts, hydrates and prodrugs thereof. By administering the compound of Formula I or II, the method inhibits the androgen receptor.Type: GrantFiled: April 11, 2008Date of Patent: April 13, 2010Assignee: Regents of the University of CaliforniaInventors: Marc Diamond, Jeremy Jones, Adam Renslo
-
Patent number: 7572816Abstract: The present invention is directed to compounds having the structure wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells.Type: GrantFiled: July 21, 2004Date of Patent: August 11, 2009Assignee: Auspex Pharmaceuticals, Inc.Inventors: Bruno Tse, Sepehr Sarshar
-
Publication number: 20080262233Abstract: The present invention relates to a process for synthesizing trans-N,N-diethyldecahydroquinolinium cation or a mixture of a cis-N,N-diethyldecahydroquinolinium cation and a trans-N,N-diethyldecahydroquinolinium cation.Type: ApplicationFiled: October 2, 2007Publication date: October 23, 2008Inventor: Allen W. Burton
-
Publication number: 20080169453Abstract: According to the present invention, there is provided a near infrared ray absorbing material comprising at least a first compound having a spectral absorption maximum wavelength of 470 nm or less in a range of 270 to 1600 nm in solution, and a second compound represented by the following formula (II-1) or (II-2). where in the formulas, R201, R202, R211, R212, R221, and R222 each represent, independently, a hydrogen atom, an aliphatic group, an aromatic group, or a heterocyclic group linked via a carbon atom; Z201 and Z202 represent a nonmetal atomic group necessary for forming a nitrogen-containing heterocycle; R213 to R216 and R223 to R226 represent a hydrogen atom or a substituent.Type: ApplicationFiled: August 16, 2007Publication date: July 17, 2008Applicant: FUJIFILM CORPORATIONInventors: Keizo Kimura, Katsuyoshi Yamakawa, Osamu Uchida
-
Patent number: 7312222Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: March 25, 2004Date of Patent: December 25, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, George V. Delucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
-
Patent number: 7265115Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.Type: GrantFiled: April 11, 2003Date of Patent: September 4, 2007Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Daniela Barlocco Cristina, Jerome F. Daanen, Michael J. Dart, Michael D. Meyer, Keith B. Ryther, Michael R. Schrimpf, Kevin B. Sippy, Richard B. Toupence
-
Patent number: 7102008Abstract: The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein the variables A, R1, R2, R3, R4, Z, U, X, Y, Za, and n are defined are as defined herein, which are useful as inhibitors of matrix metalloproteinases (MMP) and/or TNF-? converting enzyme (TACE), or a combination thereof.Type: GrantFiled: July 31, 2003Date of Patent: September 5, 2006Assignee: Bristol-Myers Squibb CompanyInventor: Thomas P. Maduskuie
-
Patent number: 6887996Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.Type: GrantFiled: November 30, 2001Date of Patent: May 3, 2005Assignee: Guilford Pharmaceuticals Inc.Inventors: Dana V. Ferraris, Jia-He Li, Vincent J. Kalish, Jie Zhang
-
Patent number: 6635641Abstract: Amide compounds represented by the formula: wherein: R1 is a moiety represented by the formula where X is selected from the group consisting of CH2, O, S, and NH; and Y is selected from the group consisting of CH2, O, and S, provided that at least one of X and Y is CH2, or X and Y together with the bond there-between form a cyclopropyl; are described. These compounds and pharmaceutical compositions containing them modulate and/or inhibit the activity of certain protein kinases and are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation.Type: GrantFiled: January 19, 2001Date of Patent: October 21, 2003Assignee: Agouron Pharmaceuticals, Inc.Inventors: Steven Lee Bender, Dilip Bhumralkar, Michael Raymond Collins, Stephen James Cripps, Judith Gail Deal, Lei Jia, Mitchell David Nambu, Cynthia Louise Palmer, Zhengwei Peng, Michael David Varney
-
Patent number: 6566372Abstract: The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.Type: GrantFiled: August 24, 2000Date of Patent: May 20, 2003Assignee: Ligand Pharmaceuticals IncorporatedInventors: Lin Zhi, Christopher Tegley, Barbara Pio, Cornelis Arjan Van Oeveren, Mehrnouch Motamedi, Esther Martinborough, Sarah West
-
Patent number: 6399821Abstract: The invention concerns a method of sulphonation characterised in that it consists in contacting a nucleophile whose nucleophilic atom is a nitrogen atom with a reagent comprising by successive or simultaneous addition: a heavy sulphonyl halide (i.e. whose atomic number is not less than that of chlorine), advantageously suphonyl chloride; and an organic base both not capable of alkylation and lipid soluble; and the organic part of said sulphonyl is perfluorinated on the carbon carried by the sulphur. The invention is applicable to organic synthesis.Type: GrantFiled: August 7, 2001Date of Patent: June 4, 2002Assignee: Rhodia ChimieInventors: Virginie Pevere, Emmanuel Marx, Laurent Gilbert
-
Patent number: 6399820Abstract: The present invention relates to a process and a reagent useful for the synthesis of sulphanilide which is perhalogenated on the carbon borne by the sulphur atom of the sulphanilide function. This persulphonylation process is characterized in that it comprises a step of placing a nucleophile, whose nucleophilic atom is a nitrogen, in contact with a reagent comprising, for successive or simultaneous addition, a heavy halide of sulphonyl, advantageously sulphonyl chloride, and an organic base comprising a trivalent atom from column V whose lone pair is conjugated directly or indirectly to a bond, and in that the organic part of the said sulphonyl is perhalogenated, advantageously perfluorinated, on the carbon borne by the sulphur. Application to the synthesis of intermediates for organic chemistry.Type: GrantFiled: May 15, 2001Date of Patent: June 4, 2002Assignee: Rhodia ChimieInventors: Jean-Roger Desmurs, Andr{dot over (e)} Millet, Virginie Pevere
-
Patent number: 6388081Abstract: The present invention relates to novel 4-substituted quinoline compounds of the following formula, libraries containing such compounds, and to the generation of such combinatorial libraries composed of such compounds: wherein R1, R2, R3, R4, R5, R6, R7, R9, and Y, have the meanings provided.Type: GrantFiled: August 16, 1999Date of Patent: May 14, 2002Assignee: Lion bioscience AGInventors: Thomas K. Hayes, Behrouz Forood, John S. Kiely
-
Patent number: 6380213Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.Type: GrantFiled: November 17, 2000Date of Patent: April 30, 2002Assignee: Eli Lilly and CompanyInventors: Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, III, David Lee Varie
-
Patent number: 6365738Abstract: Described are preferred processes for preparing heterocycles having one or more nitrogen and/or oxygen heteroatoms, utilizing a 1,3-dihalopropene as an effective 3-carbon fragment. Preferred processes yield pyridines, quinolines, oxazoles, pyrimidines and pyrazoles, depending upon the other reactant or reactants utilized with the 1,3-dihalopropene.Type: GrantFiled: June 29, 1999Date of Patent: April 2, 2002Assignee: Reilly Industries, Inc.Inventors: Ramiah Murugan, Eric F. V. Scriven
-
Patent number: 6323366Abstract: The present invention provides a method for the preparation of a wide range of primary arylamines. The arylamines are prepared in two efficient, straightforward transformations: 1) an activated aryl group and an imine group are combined, in the presence of a transition metal catalyst, under conditions wherein the transition metal catalyst catalyzes the formation of a carbon-nitrogen bond between the activated carbon of the arene and the imine nitrogen; and 2) the resulting N-aryl imine is transformed, via any of a number of standard protocols, to the primary arylamine. The method of the invention may also be exploited in the preparation of vinylamines.Type: GrantFiled: July 24, 1998Date of Patent: November 27, 2001Assignee: Massachusetts Institute of TechnologyInventors: John P. Wolfe, Jens Ahman, Joseph P. Sadighi, Robert A. Singer, Stephen L. Buchwald
-
Patent number: 6303627Abstract: This invention provides compounds and a method for the inhibition of serotonin reuptake in mammals.Type: GrantFiled: June 3, 1999Date of Patent: October 16, 2001Assignee: Eli Lilly and CompanyInventors: Daniel James Koch, Vincent Patrick Rocco
-
Patent number: 6156748Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.Type: GrantFiled: October 6, 1997Date of Patent: December 5, 2000Assignee: Eli Lilly and CompanyInventors: Jill Ann Panetta, John Kevin Shadle, Lawrence Joseph Heinz, Michael LeRoy Phillips, John Robert Rizzo, Benjamin Alan Anderson, John Allan Rieck, III, David Lee Varie
-
Patent number: 6114350Abstract: A cyanine dye having the formula ##STR1## wherein R.sub.1 -R.sub.8 are each independently selected from a group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl group, and C.sub.0 -C.sub.4 alkyl group having a hydrophilic substituent thereon. R.sub.11 and R.sub.12 are chosen to include a free or protected thiol, amine or hydroxyl substituent capable of reacting with a target molecule through a nucleophilic displacement mechanism. The dye is useful in labeling a variety of target molecules. Processes are described for synthesizing suitable heterocyclic and indole derivatives as precursors for the aforementioned cyanine dyes.Type: GrantFiled: April 19, 1999Date of Patent: September 5, 2000Assignee: NEN Life Science Products, Inc.Inventors: Malcolm Harry Randall, Philip Richard Buzby, Thomas Joseph Erickson, Joseph David Trometer, Joseph John Miller, Jr., David George Ahern, Mark Norman Bobrow
-
Patent number: 6103904Abstract: The present invention relates to an improved Skraup reaction process wherein pressure is applied during the reaction and the number of equivalents of sulfuric acid utilized is reduced.Type: GrantFiled: July 17, 1997Date of Patent: August 15, 2000Assignee: BASF CorporationInventor: Ronald R. Eva
-
Patent number: 6093825Abstract: Methods for conversion of anilines to 1,2-dihydroquinolines. 1,2-dihydroquinoliiies are generated from combining an aniline, a silylating agent, and further condensing with a ketone in the presence of a catalyst. In one aspect, the silylation of the aniline may be performed in a one-step synthesis by adding the silylating, agent to the same reaction vessel as the ketone, aniline, and catalyst. In a second aspect, the 1,2-dihydroquinoline is generated in a two-step synthesis where an N-silyl aniline is formed prior to the addition of the ketone and catalyst.Type: GrantFiled: May 27, 1998Date of Patent: July 25, 2000Assignees: American Home Products, Ligand Pharmaceuticals IncorporatedInventors: Reinhold H. W. Bender, James P. Edwards, Todd K. Jones
-
Patent number: 6063784Abstract: A compound selected from the group consisting of a compound of the formula ##STR1## wherein the substituents are defined as in the application and its non-toxic, pharmaceutically acceptable acid addition salts which are useful for treating hypertension.Type: GrantFiled: March 10, 1999Date of Patent: May 16, 2000Assignee: Societe de Conseils de Recherches et D'Applications Scientifiques (S.C.R.A.S. )Inventors: Dennis Bigg, Marie-Odile Galcera
-
Patent number: 6020494Abstract: In a method of purifying quinaldine prepared from coal tar, a phenol, cresol and xylenol-type mononuclear aromatic compound is added to the quinaldine fraction, said aromatic compound is crystallized out forming an adduct with quinaldine and the quinaldine/mononuclear aromatic adduct is then separated, whereby, before the mononuclear aromatic compound is added, 5% to 20% by weight of a mixture of aromatic compounds or toluene, in relation to the mass of the quinaldine fraction, is added to the quinaldine fraction.Type: GrantFiled: June 25, 1998Date of Patent: February 1, 2000Assignee: Rutgers VFT AGInventors: Jorg Talbiersky, Edgar Fuhrmann, Heinz-Gunter Janneck
-
Patent number: 5939268Abstract: This invention features methods of synthesizing combinatorial libraries of chemical compounds, and combinatorial libraries of chemical compounds formed by the methods of this invention. Specifically, Diels-Alder chemistry is utilized to generate libraries of diverse molecules which are easily differentially functionalized with various chemical moities and in one aspect are configured to act as non-hydrolyzable peptidomimetics.Type: GrantFiled: July 26, 1994Date of Patent: August 17, 1999Assignee: The Scripps Research InstituteInventor: Dale L. Boger
-
Patent number: 5780634Abstract: Quinolin-2-yl benzoic acid compounds which are useful as intermediates of quinoline compounds having angiotensin II antagonist activity prepared by decarboxylating 2-(carboxyphenyl)-4-quinolinecarboxylic acid compounds in which a carboxyl group bonded to a phenyl group may be esterified, while a carboxyl group bonded to a quinoline ring is not esterified, and both rings may have one or more substituents inert to the decarboxylation reaction.Type: GrantFiled: October 27, 1995Date of Patent: July 14, 1998Assignees: The Green Cross Corporation, Asahi Glass Co., Ltd.Inventors: Yoshihisa Inoue, Hajime Ebisu, Naomichi Ishida, Norifumi Nakamura, Jun Sasaki, Takashi Okazoe, Yoshitomi Morizawa, Arata Yasuda, Shuzhong Wang, Tomoko Ito
-
Patent number: RE41150Abstract: This invention relates to compounds, pharmaceutical compositions, and methods of using the disclosed compounds for inhibiting PARP.Type: GrantFiled: January 10, 2008Date of Patent: February 23, 2010Assignee: Eisai Corporation of North AmericaInventors: Dana V. Ferraris, Jia-He Li