Nitrogen Bonded Directly To The Bicyclo Ring System Patents (Class 549/404)
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Patent number: 12007369Abstract: A method for determining corrosion inhibitor residual concentration of a hydrocarbon sample is described. The hydrocarbon sample is mixed with a standard solution to form a first mixture. The standard solution includes a corrosion inhibitor in a known concentration. The first mixture is mixed with an aqueous saline solution to form a second mixture. The aqueous saline solution includes about 1% salt concentration or greater. The second mixture is agitated for about 1 hour or longer and at a temperature of about 50 degrees Celsius (° C.) or greater. After agitation, a hydrocarbon phase and an aqueous phase of the second mixture are allowed to separate. A portion of the aqueous phase is obtained. The portion of the aqueous phase is analyzed to determine a corrosion inhibitor residual concentration of the hydrocarbon sample.Type: GrantFiled: April 1, 2021Date of Patent: June 11, 2024Assignee: Saudi Arabian Oil CompanyInventors: Talal M. Al-Ghamdi, Muhaned M. Feghia, Faisal M. Mutahhar, Musab M. Talal
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Patent number: 11091455Abstract: ?9-THC carboxylic acid is extracted from cannabis flowers using a first organic solvent, then separated using a second aqueous solvent. ?9-THC carboxylic acid is converted to ?9-THC carboxylic salt before being extracted by a third organic solvent and converted back to ?9-THC carboxylic acid. Using a solvent swap, ?9-THC carboxylic acid is decarboxylated and extracted again with an organic solvent prior to purification to give ?9-THC.Type: GrantFiled: January 28, 2020Date of Patent: August 17, 2021Assignee: APIRx Pharmaceutical USA, LLCInventors: Lekhram Changoer, Cornelis Herman Michel Van Der Loo, Erik Keller
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Publication number: 20150119418Abstract: Provided is a pharmaceutical agent containing a compound represented by General Formula (1), a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein A represents a C1-C3 linear alkylene group, in which one methylene group is optionally substituted with O or S; n represents an integer of from 3 to 5; X1 and X2 each independently represent CH or N; W1 and W2 each independently represent a carboxyl group or a tetrazolyl group; V represents a C1-C8 linear or branched alkylene group, in which one methylene group is optionally substituted with O or S; and R represents a substituted phenyl group, for example.Type: ApplicationFiled: April 15, 2013Publication date: April 30, 2015Applicant: TOA EIYO LTD.Inventors: Kazuhiro Uemoto, Yoshimichi Sato, Naoki Okada, Emiko Iimori, Masayuki Kageyama
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Patent number: 8877741Abstract: The invention relates to new pyrrolidine derivatives of the formula to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: GrantFiled: January 22, 2014Date of Patent: November 4, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
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Patent number: 8853196Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.Type: GrantFiled: August 3, 2012Date of Patent: October 7, 2014Assignee: AbbVie Deutschland GmbH & Co. KGInventors: Wilhelm Amberg, Udo Lange, Frauke Pohlki
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Patent number: 8716497Abstract: A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.Type: GrantFiled: September 10, 2012Date of Patent: May 6, 2014Assignees: Children's Hospital Medical Center, Ausio Pharmaceuticals, Inc.Inventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
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Publication number: 20140045931Abstract: The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.Type: ApplicationFiled: October 18, 2013Publication date: February 13, 2014Applicant: THE HONG KONG POLYTECHNIC UNIVERSITYInventors: Q. PING DOU, TAK-HANG CHAN, DAVID M. SMITH
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Publication number: 20140031388Abstract: Anticancer compounds according to formula I are described herein. wherein R1, R2, R3 and R4 are selected from H, CH3, OH, SH, OCH3, NHR?, halogen, CF3, N-linked pyrrolidine, and SO2NHR?, or any combination thereof; R5 is an alkyl, alkenyl, or alkaryl group including from 4 to 11 carbons, X is selected from CH2, CHOH, C?O, S?O, O?S?O, and an oxetane ring, Y is selected from CH2, O, and NH, and R? is a H, aryl, or a lower alkyl group, or pharmaceutically acceptable salts thereof. The compounds have been shown to facilitate site-specific dephosphorylation of Akt at Ser-473, thereby inactivating Akt and decreasing dysregulation of Akt signaling that can occur in cancer cells.Type: ApplicationFiled: July 26, 2013Publication date: January 30, 2014Inventors: Ching-Shih Chen, Dasheng Wang, Samuel K. Kulp
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Publication number: 20130345255Abstract: Disclosed herein are compounds of formula (I) or pharmaceutically acceptable salts, prodrugs, or combinations thereof, wherein X1, L, Rx, Ry, Rz, R1, R2, A, m, n, p, q, and r are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: June 20, 2013Publication date: December 26, 2013Inventors: Arthur Gomtsyan, Jerome Daanen, Michael E. Kort, Philip R. Kym, Eric A. Voight, Kevin R. Woller
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Publication number: 20130345420Abstract: The invention is the discovery of the use of the class of compounds represented by Formula I, as selective inhibitors of excitatory amino acid transporter (EAAT) subtype 1 (EAAT1) and its rodent ortholog L-glutamate/L-aspartate transporter (GLAST) for the study of function and distribution of EAAT1/GLAST in the central nervous system and studies of the physiological and pathological functions of the EAAT1/GLAST subtype in native tissues, cultured neurons, and/or animal models for CNS disorders.Type: ApplicationFiled: September 19, 2011Publication date: December 26, 2013Inventors: Lennart Bunch, Anders Asbjørn Jensen
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Patent number: 8609692Abstract: Disclosed herein are compounds of formula (I), or pharmaceutically acceptable salts, solvates, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and m are defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: GrantFiled: October 15, 2009Date of Patent: December 17, 2013Assignee: AbbVie Inc.Inventors: Arthur R. Gomtsyan, Erol K. Bayburt, Jun Chen, Stanley DiDomenico, Jerome F. Daanen, Michael E. Kort, Philip R. Kym, Heath A. McDonald, Richard J. Perner, Robert G. Schmidt, Eric A. Voight
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Publication number: 20130324525Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: August 6, 2013Publication date: December 5, 2013Applicant: Gilead Sciences, Inc.Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
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Publication number: 20130310254Abstract: The present application relates to novel alpha, beta-unsaturated imines, to processes for their preparation, to their use for controlling animal pests including arthropods and in particular insects and to their use in the control of vectors.Type: ApplicationFiled: November 24, 2011Publication date: November 21, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Stefan Werner, Ulrich Ebbinghaus-Kintscher, Sebastian Horstmann, Michael Maue, Hans-Georg Schwarz, Robert Velten, Arnd Voerste, Ulrich Görgens, Andreas Turberg
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Patent number: 8546571Abstract: A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral catalyst and a source of hydrogen, wherein: X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl, wherein: the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.Type: GrantFiled: December 12, 2007Date of Patent: October 1, 2013Assignee: BIAL—Portela & C.A., S.A.Inventors: David Alexander Learmonth, Antonio Zanotti-Gerosa, Gabriela Alexandra Grasa, Alexander Beliaev
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Patent number: 8530460Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.Type: GrantFiled: December 14, 2012Date of Patent: September 10, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Martin Fleck, Bernd Nosse, Niklas Heine, Gerald Juergen Roth
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Publication number: 20130158067Abstract: Disclosed herein are compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein X1, L, Rx, Ry, Rz, A, m, n, p, q, s, and positions a and b are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: December 17, 2012Publication date: June 20, 2013Applicant: ABBVIE INC.Inventor: AbbVie Inc.
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Publication number: 20130079524Abstract: The present invention relates N-cycloalkyl-N-bicyclic-carboxamide, thiocarboxamide or N-substituted carboximidamide derivatives of formula (I) wherein A represents a carbo-linked, 5-membered heterocyclyl group; T represents O, S, N-Ra, N—ORa, N—NRaRb or N—CN; Z1 represents a C3-C7-cycloalkyl group; X represents N or a CZ7 and Z2; Z3; L1 and L2 represent various substituents; their process of preparation; preparation intermediate compounds; their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: November 21, 2012Publication date: March 28, 2013Inventors: Philippe Desbordes, Stephanie Gary, Marie-Clarie Grosjean-Cournoyer, Benoit Hartmann, Hadano Hiroyuki, Philippe Rinolfi, Jean-Pierre Vors
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Patent number: 8394794Abstract: The invention provides compounds of Formula (I) and (IV): as described herein, as well as salts thereof. The compounds have anti-cancer properties and/or chemosensitization properties.Type: GrantFiled: March 21, 2008Date of Patent: March 12, 2013Assignee: Regents of The University of MinnesotaInventors: Chengguo Xing, Jignesh Doshi
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Patent number: 8383843Abstract: Disclosed herein is a method for preparing a coumarin compound of formula (F), in which R1, R2, and R3 are independently H, C1˜C7 alkoxy, C1˜C7 alkyl, phenoxy, benzyloxy, or a halogen atom; R4 is an alkyl group; and Ar is an optionally substituted aryl group, the method including: treating a chromene compound having the following formula (E) with an acid in the presence of water. A chromene compound of formula (E) and a method for preparing the chromene compound of formula (E) are also disclosed.Type: GrantFiled: October 11, 2010Date of Patent: February 26, 2013Assignee: Kaohsiung Medical UniversityInventors: Eng-Chi Wang, Jui-Chi Tsai, Sie-Rong Li, Po-Yuan Chen
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Publication number: 20130035323Abstract: The present invention relates to aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives, and the use of such aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives for therapeutic purposes. The aminochromane, aminothiochromane and amino-1,2,3,4-tetrahydroquinoline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: August 3, 2012Publication date: February 7, 2013Applicant: Abbott GmbH & Co. KGInventors: Wilhelm AMBERG, Udo LANGE, Frauke POHLKI
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Publication number: 20130035382Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.Type: ApplicationFiled: April 20, 2011Publication date: February 7, 2013Applicant: KINETA, INC.Inventors: Shawn P. Iadonato, Kristin Bedard
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Patent number: 8263790Abstract: A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.Type: GrantFiled: June 1, 2011Date of Patent: September 11, 2012Assignees: Children's Hospital Medical Center, Girindus America, Inc.Inventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
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Publication number: 20120129818Abstract: Ortho methoxy phenolic compounds are provided that include methylenedioxyphenyl ferulate and ferulylproline and derivatives thereof. Pharmaceutical compositions comprising the compounds and methods of using the compounds for treating cardiovascular diseases, including hypertension, atherosclerosis, coronary heart disease, angina, stroke, and myocardial infarction, are further provided. The compounds are also useful in reducing low-density lipoprotein oxidation, improving or increasing vasodilation, and reducing plaque destabilization in a subject.Type: ApplicationFiled: April 23, 2010Publication date: May 24, 2012Inventor: Desikan Rajagopal
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Publication number: 20120101287Abstract: The invention related to an optically active compound of formula (I) or a salt thereof: wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use as herbicides or plant growth regulators. The invention also relates to novel intermediates of formula (III), (V) and (XIII) as defined in the description.Type: ApplicationFiled: December 28, 2011Publication date: April 26, 2012Applicant: Bayer CropScience AGInventors: Hartmut Ahrens, Hansjöerg Dietrich, Klemens Minn, Thomas Auler, Hermann Bieringer, Martin Hills, Heinz Kehne, Hubert Menne
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Publication number: 20120088923Abstract: Disclosed herein is a method for preparing a coumarin compound of formula (F), in which R1, R2, and R3 are independently H, C1˜C7 alkoxy, C1˜C7 alkyl, phenoxy, benzyloxy, or a halogen atom; R4 is an alkyl group; and Ar is an optionally substituted aryl group, the method including: treating a chromene compound having the following formula (E) with an acid in the presence of water. A chromene compound of formula (E) and a method for preparing the chromene compound of formula (E) are also disclosed.Type: ApplicationFiled: October 11, 2010Publication date: April 12, 2012Applicant: KAOHSIUNG MEDICAL UNIVERSITYInventors: Eng-Chi Wang, Jui-Chi Tsai, Sie-Rong Li, Po-Yuan Chen
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Publication number: 20120035361Abstract: The invention is the discovery of the use of the class of compounds represented by Formula I, as selective inhibitors of excitatory amino acid transporter (EAAT) subtype 1 (EAAT1) and its rodent ortholog L-glutamate/L-aspartate transporter (GLAST) for the study of function and distribution of EAAT1/GLAST in the central nervous system and studies of the physiological and pathological functions of the EAAT1/GLAST subtype in native tissues, cultured neurons, and/or animal models for CNS disorders.Type: ApplicationFiled: September 19, 2011Publication date: February 9, 2012Inventors: Lennart Bunch, Anders Asbjørn Jensen
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Publication number: 20120029067Abstract: The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.Type: ApplicationFiled: October 11, 2011Publication date: February 2, 2012Applicants: UNIVERSITY OF SOUTH FLORIDA, THE HONG KONG POLYTECHNIC UNIVERSITY, MCGILL UNIVERSITYInventors: Q. Ping DOU, Tak-Hang CHAN, David M. SMITH
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Publication number: 20120022103Abstract: The present application is directed to compounds that are TRPV1 antagonists and have formula (I) wherein variables Ar1, L1, R1, R2, R3, R4, R5, Y1, Y2, and Y3, are as defined in the description, which are useful for treating disorders caused by or exacerbated by vanilloid receptor activity.Type: ApplicationFiled: September 29, 2011Publication date: January 26, 2012Applicant: ABBOTT LABORATORIESInventors: Erol K. Bayburt, Jerome F. Daanen, Arthur R. Gomtsyan, Steven P. Latshaw, Chih-hung Lee, Robert G. Schmidt, JR.
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Publication number: 20110319267Abstract: Prodrug compounds which metabolize into 5-ASA or analogs thereof, and taurine or analogs thereof, in the colon site are disclosed. Pharmaceutical compositions including the compounds, and methods of treatment using the compounds, are also disclosed. Such compounds have utility for treating or preventing gastrointestinal disorders, including colon cancer, ulcerative colitis and Crohn's disease.Type: ApplicationFiled: September 10, 2009Publication date: December 29, 2011Applicant: Numed International, Inc.Inventor: Nnochiri Ekwuribe
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Patent number: 8084490Abstract: The present invention is directed to novel sulfamide and sulfamate derivatives, pharmaceutical compositions containing them and their use in the treatment of epilepsy and related disorders.Type: GrantFiled: June 16, 2005Date of Patent: December 27, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: David F. McComsey, Michael H. Parker, Allen B. Reitz, Bruce E. Maryanoff
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Patent number: 8080664Abstract: Use of the general formula compound (I), or any salt thereof, for preparation of a pharmaceutical compound for the treatment of infections illnesses, in particular for the treatment of Helicobacter. Y is NO2, COOH or SO3H; Z is O, N or S; X1 and X2 are halogen atoms which may be the same or different; and m and n take values from 0 to 3 and may be equal or different.Type: GrantFiled: February 20, 2008Date of Patent: December 20, 2011Assignee: Universidad De ZaragozaInventors: Javier Sancho Sanz, Adrián Velazquez Campoy, Nunilo Cremades Casasin
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Patent number: 8048912Abstract: The present invention relates to a novel benzopyran derivative having goodantagonistic activity on TGF-? receptor which can be effectively used as a prophylactic and therapeutic agent for liver disease as well as several fibroplasiadiseases such as hepatic fibrosis, liver cirrhosis, pulmonary fibrosis, dermatosclerosis, glomerular fibrosis and the like; and a pharmaceutical use thereof.Type: GrantFiled: June 15, 2005Date of Patent: November 1, 2011Assignees: SK Chemicals Co., Ltd., Korea Research Institute of Chemical TechnologyInventors: Young-Dae Gong, Jin-Soo Seo, Moon-Kook Jeon, Wie-Jong Kwak, Yong-Baik Cho, Nam Kyu Lee, Eun Ju Lee, Jung Bum Lee, Jun Won Lee, Sukho Lee, Mi-Sook Dong, Jeong-Ran Kim
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Publication number: 20110251388Abstract: The present invention provides a 1-heterodiene derivative represented by formula (2) or salt thereof: (in formula (2), W represents hydrogen atom or the like, A represents oxygen atom or the like, R1 represents an optionally substituted C1-6 alkyl group or the like, m represents an integer of 0 to 10, n represents an integer of 1 to 4, X1 represents oxygen atom or the like, p represents an integer of 0 to 5, R3 represents an optionally substituted C1-6 alkyl group or the like, r presents an integer of 0 to 5, the 1-heterodiene derivative exists in E-form, Z-form or a mixture thereof according to the carbon-carbon undefined double stereo bond in formula (2)).Type: ApplicationFiled: December 17, 2009Publication date: October 13, 2011Applicant: Nippon Soda Co., Ltd.Inventors: Koichi Kutose, Jyun Takahashi, Isami Hamamoto, Makio Yano, Jyunko Morohoshi, Jyun Kanazawa
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Publication number: 20110237803Abstract: A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral catalyst and a source of hydrogen, wherein X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl, wherein the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means a phenyl or naphthyl group, optionally substituted by alkyloxy, halogen or nitro group; and the term halogen means fluorine, chlorine, bromine or iodine.Type: ApplicationFiled: May 6, 2009Publication date: September 29, 2011Applicant: Bial - Portela & CA, S.A.Inventors: Alexander Beliaev, David Alexander Learmonth
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Publication number: 20110166142Abstract: 2-Substituted isoflavonoid compounds and pharmaceutical compositions containing same are useful as anti-inflammatory agents and antioxidants and for the treatment of related diseases and conditions.Type: ApplicationFiled: June 30, 2008Publication date: July 7, 2011Inventors: Eleanor Eiffe, Andrew Heaton, Catherine Walker, Alan James Husband
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Publication number: 20110166360Abstract: A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral transition metal catalyst and a source of hydrogen, wherein: X is CH2, oxygen or sulphur; R1, R2 and R3 are the same or different and signify hydrogen, halogen, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl, the transition metal catalyst comprising a chiral ligand having the formula wherein each R and R? independently represents alkyl, aryl, aralkyl, alkenyl, alkynyl, alkoxy, aryloxy, alkylthio, arylthio, unsubstituted or substituted cyclic moiety selected from a group consisting of monocyclic or polycyclic saturated or partially saturated carbocyclic or heterocyclic, aromatic or heteroaromatic rings said rings comprising from 4 to 8 atoms and comprising from 0 to 3 heteroatoms, wherein: the term alkyl means hydrocarbon chains, straight or branched, conType: ApplicationFiled: March 13, 2009Publication date: July 7, 2011Applicant: BIAL - PORTELA & CA, S.A.Inventors: Alexander Beliaev, David Alexander Learmonth, Juan José Almena Perea, Gerhard Geib, Patrick Hitzel, Renat Kadyrov, David Voigtlaender
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Patent number: 7968595Abstract: The present invention is directed to a substituted 4H-chromene represented by the Formula 1R, substantially free from the corresponding (S)-stereoisomer: The present invention also relates to the discovery that compound 1R, substantially free from the corresponding (S)-stereoisomer, is an activator of caspases and inducer of apoptosis, as well as an antivascular agent. Therefore, compound 1R, substantially free from the corresponding (S)-stereoisomer, can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs. Compound 1R, substantially free from the corresponding (S)-stereoisomer, also can be used for the treatment of diseases due to overgrowth of vasculature, such as solid tumors and ocular neovascularization.Type: GrantFiled: July 6, 2007Date of Patent: June 28, 2011Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, John A. Drewe, Shailaja Kasibhatla, William D. Kemnitzer, Ben Y. Tseng, Charles Blais, Denis Labrecque, Henriette Gourdeau
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Patent number: 7960573Abstract: A method for preparing an enantiomeric chromane, by asymmetrically hydrogenating a chromene compound in the presence of an Ir catalyst having a chiral ligand. The method includes the enantioselective preparation of enantiomeric equol. A preferred Ir catalyst has a chiral phosphineoxazoline ligand. Enantiomeric chromanes of high stereoselective purity can be obtained.Type: GrantFiled: May 4, 2009Date of Patent: June 14, 2011Assignees: Children's Hospital Medical Center, Girindus America, Inc.Inventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
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Patent number: 7951838Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein R1, R2, R3, R4, R5, A1, A2, A3, A4, X and Z are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits and impairment, schizophrenia and other similar central nervous system conditions. The invention also comprises further embodiments of Formula II, intermediates and processes useful for the preparation of compounds of Formulas I and II.Type: GrantFiled: August 20, 2010Date of Patent: May 31, 2011Assignee: Amgen Inc.Inventors: Daniel La, Patricia Lopez, Vinod F. Patel, Wenge Zhong
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Publication number: 20110123929Abstract: Provided are an oxime compound represented by General Formula (1), a photosensitive composition containing the oxime compound as a photopolymerization initiator, a production method for a color filter using the photosensitive composition, and a color filter obtained by the production method: in General Formula (1), R1 represents a hydrogen atom, an acyl group, an alkoxycarbonyl group or an aryloxylcarbonyl group, each of which may have a substituent; R2 represents or R2s each represent a halogen atom, an alkyl group, an aryl group, an alkyloxy group, an aryloxy group, an alkylthio group, an arylthio group or an amino group; m is an integer of 0 to 4; when m is an integer of 2 or more, R2s may be linked together to form a ring; and A represents a 4-, 5-, 6- or 7-membered ring.Type: ApplicationFiled: August 1, 2007Publication date: May 26, 2011Applicant: FUJIFILM CorporationInventors: Akinori Fujita, Takashi Tamura, Kimi Ikeda, Daisuke Kashiwagi
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Patent number: 7919490Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 4, 2007Date of Patent: April 5, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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Patent number: 7915268Abstract: The present invention provides novel purines useful for the prevention and treatment of autoimmune diseases, inflammatory diseases, mast cell mediated disease and transplant rejection.Type: GrantFiled: October 4, 2007Date of Patent: March 29, 2011Assignee: Wyeth LLCInventors: Yingchun Lu, Celia Kingsbury, Adolph Bohnstedt, Michael Ohlmeyer, Vidyadhar Paradkar
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Patent number: 7902187Abstract: The present invention provides novel purinones and purines useful for the prevention and treatment of autoimmune diseases, inflammatory disease, mast cell mediated disease and transplant rejection.Type: GrantFiled: August 22, 2008Date of Patent: March 8, 2011Assignee: Wyeth LLCInventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
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Patent number: 7880042Abstract: The invention relates to multiply substituted tetrahydronaphthalene derivatives of the formula (Ia) to processes for preparing them and to their use as antiinflammatory agents.Type: GrantFiled: March 14, 2007Date of Patent: February 1, 2011Assignee: Bayer Schering Pharma AGInventors: Markus Berger, Hartmut Rehwinkel, Heike Schäcke, Stefan Bäurle, Norbert Schmees
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Publication number: 20100317862Abstract: Use of the general formula compound (I), or any salt thereof, for preparation of a pharmaceutical compound for the treatment of infections illnesses, in particular for the treatment of Helicobacter. Y is NO2, COOH or SO3H; Z is O, N or S; X1 and X2 are halogen atoms which may be the same or different; and m and n take values from 0 to 3 and may be equal or different.Type: ApplicationFiled: February 20, 2008Publication date: December 16, 2010Inventors: Javier Sancho Sanz, Adrián Velazquez Campoy, Nunilo Cremades Casasin
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Publication number: 20100311778Abstract: The present invention provides transient receptor potential vanilloid (TRPV) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.Type: ApplicationFiled: December 16, 2008Publication date: December 9, 2010Inventors: V S Prasadarao Lingam, Abraham Thomas, Laxmikant Atmaram Gharat, Deepak Vitthal Ukirde, Shantaram Kashinath Phatangare, Ajit Shankar Mindhe, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Publication number: 20100298580Abstract: Compounds of formula I, V, VI and II, and processes for their preparation, wherein R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino or dialkylamino group; and R4 is alkyl or aryl. There is also provided a process for preparing a compound of formula B from the compounds of formula V and I.Type: ApplicationFiled: November 13, 2008Publication date: November 25, 2010Applicant: BIAL - PORTELA & CA, S.A.Inventors: Brian Broadbelt, Alexander Beliaev, David Alexander Learmonth
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Patent number: 7838553Abstract: The present invention is directed to novel benzopyran derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders related to potassium channel.Type: GrantFiled: August 30, 2006Date of Patent: November 23, 2010Assignee: Janssen Pharmaceutica NVInventors: Xuqing Zhang, Xiaojie Li, Zhihua Sui
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Patent number: 7812019Abstract: Compounds that are antagonists of the VR1 receptor, having formula (I) or a pharmaceutically acceptable salt, prodrug, or salt of a prodrug thereof, wherein A1, A2, A3, A4, R7, R8, R9, X, Y, Z, L, n, and m, are as defined herein, and are useful in disorders prevented or ameliorated by inhibiting the VR1 receptor.Type: GrantFiled: November 22, 2005Date of Patent: October 12, 2010Assignee: Abbott LaboratoriesInventors: Arthur Gomtsyan, Erol K. Bayburt, Robert G. Schmidt, Jr., Chih-Hung Lee, Brian S. Brown, Tammie K. Jinkerson, John R. Koenig, Jerome F. Daanen, Steven P. Latshaw
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Publication number: 20100217009Abstract: A process for preparing a compound of formula (22), comprising reducing a compound of formula (21), to produce a compound of formula (23), followed by the hydrogenolysis of the compound of formula 23 in a solvent comprising a C1 to C6 alkyl sulfonic acid and optionally a chlorinated solvent.Type: ApplicationFiled: May 21, 2008Publication date: August 26, 2010Applicant: BIAL - PORTELA & CA, S.A.Inventors: David Alexander Learmonth, Alexander Beliaev