Nitrogen Bonded Directly To The Bicyclo Ring System Patents (Class 549/404)
  • Patent number: 11091455
    Abstract: ?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: Grant
    Filed: January 28, 2020
    Date of Patent: August 17, 2021
    Assignee: APIRx Pharmaceutical USA, LLC
    Inventors: Lekhram Changoer, Cornelis Herman Michel Van Der Loo, Erik Keller
  • Publication number: 20150119418
    Abstract: 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: Application
    Filed: April 15, 2013
    Publication date: April 30, 2015
    Applicant: TOA EIYO LTD.
    Inventors: Kazuhiro Uemoto, Yoshimichi Sato, Naoki Okada, Emiko Iimori, Masayuki Kageyama
  • Patent number: 8877741
    Abstract: 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: Grant
    Filed: January 22, 2014
    Date of Patent: November 4, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Niklas Heine, Bernd Nosse, Gerald Juergen Roth
  • Patent number: 8853196
    Abstract: 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: Grant
    Filed: August 3, 2012
    Date of Patent: October 7, 2014
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Wilhelm Amberg, Udo Lange, Frauke Pohlki
  • Patent number: 8716497
    Abstract: 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: Grant
    Filed: September 10, 2012
    Date of Patent: May 6, 2014
    Assignees: Children's Hospital Medical Center, Ausio Pharmaceuticals, Inc.
    Inventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
  • Publication number: 20140045931
    Abstract: 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: Application
    Filed: October 18, 2013
    Publication date: February 13, 2014
    Applicant: THE HONG KONG POLYTECHNIC UNIVERSITY
    Inventors: Q. PING DOU, TAK-HANG CHAN, DAVID M. SMITH
  • Publication number: 20140031388
    Abstract: 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: Application
    Filed: July 26, 2013
    Publication date: January 30, 2014
    Inventors: Ching-Shih Chen, Dasheng Wang, Samuel K. Kulp
  • Publication number: 20130345255
    Abstract: 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: Application
    Filed: June 20, 2013
    Publication date: December 26, 2013
    Inventors: Arthur Gomtsyan, Jerome Daanen, Michael E. Kort, Philip R. Kym, Eric A. Voight, Kevin R. Woller
  • Publication number: 20130345420
    Abstract: 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: Application
    Filed: September 19, 2011
    Publication date: December 26, 2013
    Inventors: Lennart Bunch, Anders Asbjørn Jensen
  • Patent number: 8609692
    Abstract: 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: Grant
    Filed: October 15, 2009
    Date of Patent: December 17, 2013
    Assignee: 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
  • Publication number: 20130324525
    Abstract: 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: Application
    Filed: August 6, 2013
    Publication date: December 5, 2013
    Applicant: Gilead Sciences, Inc.
    Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
  • Publication number: 20130310254
    Abstract: 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: Application
    Filed: November 24, 2011
    Publication date: November 21, 2013
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Stefan Werner, Ulrich Ebbinghaus-Kintscher, Sebastian Horstmann, Michael Maue, Hans-Georg Schwarz, Robert Velten, Arnd Voerste, Ulrich Görgens, Andreas Turberg
  • Patent number: 8546571
    Abstract: 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: Grant
    Filed: December 12, 2007
    Date of Patent: October 1, 2013
    Assignee: BIAL—Portela & C.A., S.A.
    Inventors: David Alexander Learmonth, Antonio Zanotti-Gerosa, Gabriela Alexandra Grasa, Alexander Beliaev
  • Patent number: 8530460
    Abstract: Azetidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.
    Type: Grant
    Filed: December 14, 2012
    Date of Patent: September 10, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Martin Fleck, Bernd Nosse, Niklas Heine, Gerald Juergen Roth
  • Publication number: 20130158067
    Abstract: 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: Application
    Filed: December 17, 2012
    Publication date: June 20, 2013
    Applicant: ABBVIE INC.
    Inventor: AbbVie Inc.
  • Publication number: 20130079524
    Abstract: 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: Application
    Filed: November 21, 2012
    Publication date: March 28, 2013
    Inventors: Philippe Desbordes, Stephanie Gary, Marie-Clarie Grosjean-Cournoyer, Benoit Hartmann, Hadano Hiroyuki, Philippe Rinolfi, Jean-Pierre Vors
  • Patent number: 8394794
    Abstract: 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: Grant
    Filed: March 21, 2008
    Date of Patent: March 12, 2013
    Assignee: Regents of The University of Minnesota
    Inventors: Chengguo Xing, Jignesh Doshi
  • Patent number: 8383843
    Abstract: 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: Grant
    Filed: October 11, 2010
    Date of Patent: February 26, 2013
    Assignee: Kaohsiung Medical University
    Inventors: Eng-Chi Wang, Jui-Chi Tsai, Sie-Rong Li, Po-Yuan Chen
  • Publication number: 20130035382
    Abstract: 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: Application
    Filed: April 20, 2011
    Publication date: February 7, 2013
    Applicant: KINETA, INC.
    Inventors: Shawn P. Iadonato, Kristin Bedard
  • Publication number: 20130035323
    Abstract: 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: Application
    Filed: August 3, 2012
    Publication date: February 7, 2013
    Applicant: Abbott GmbH & Co. KG
    Inventors: Wilhelm AMBERG, Udo LANGE, Frauke POHLKI
  • Patent number: 8263790
    Abstract: 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: Grant
    Filed: June 1, 2011
    Date of Patent: September 11, 2012
    Assignees: Children's Hospital Medical Center, Girindus America, Inc.
    Inventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
  • Publication number: 20120129818
    Abstract: 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: Application
    Filed: April 23, 2010
    Publication date: May 24, 2012
    Inventor: Desikan Rajagopal
  • Publication number: 20120101287
    Abstract: 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: Application
    Filed: December 28, 2011
    Publication date: April 26, 2012
    Applicant: Bayer CropScience AG
    Inventors: Hartmut Ahrens, Hansjöerg Dietrich, Klemens Minn, Thomas Auler, Hermann Bieringer, Martin Hills, Heinz Kehne, Hubert Menne
  • Publication number: 20120088923
    Abstract: 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: Application
    Filed: October 11, 2010
    Publication date: April 12, 2012
    Applicant: KAOHSIUNG MEDICAL UNIVERSITY
    Inventors: Eng-Chi Wang, Jui-Chi Tsai, Sie-Rong Li, Po-Yuan Chen
  • Publication number: 20120035361
    Abstract: 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: Application
    Filed: September 19, 2011
    Publication date: February 9, 2012
    Inventors: Lennart Bunch, Anders Asbjørn Jensen
  • Publication number: 20120029067
    Abstract: 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: Application
    Filed: October 11, 2011
    Publication date: February 2, 2012
    Applicants: UNIVERSITY OF SOUTH FLORIDA, THE HONG KONG POLYTECHNIC UNIVERSITY, MCGILL UNIVERSITY
    Inventors: Q. Ping DOU, Tak-Hang CHAN, David M. SMITH
  • Publication number: 20120022103
    Abstract: 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: Application
    Filed: September 29, 2011
    Publication date: January 26, 2012
    Applicant: ABBOTT LABORATORIES
    Inventors: Erol K. Bayburt, Jerome F. Daanen, Arthur R. Gomtsyan, Steven P. Latshaw, Chih-hung Lee, Robert G. Schmidt, JR.
  • Publication number: 20110319267
    Abstract: 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: Application
    Filed: September 10, 2009
    Publication date: December 29, 2011
    Applicant: Numed International, Inc.
    Inventor: Nnochiri Ekwuribe
  • Patent number: 8084490
    Abstract: 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: Grant
    Filed: June 16, 2005
    Date of Patent: December 27, 2011
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: David F. McComsey, Michael H. Parker, Allen B. Reitz, Bruce E. Maryanoff
  • Patent number: 8080664
    Abstract: 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: Grant
    Filed: February 20, 2008
    Date of Patent: December 20, 2011
    Assignee: Universidad De Zaragoza
    Inventors: Javier Sancho Sanz, Adrián Velazquez Campoy, Nunilo Cremades Casasin
  • Patent number: 8048912
    Abstract: 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: Grant
    Filed: June 15, 2005
    Date of Patent: November 1, 2011
    Assignees: SK Chemicals Co., Ltd., Korea Research Institute of Chemical Technology
    Inventors: 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
  • Publication number: 20110251388
    Abstract: 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: Application
    Filed: December 17, 2009
    Publication date: October 13, 2011
    Applicant: Nippon Soda Co., Ltd.
    Inventors: Koichi Kutose, Jyun Takahashi, Isami Hamamoto, Makio Yano, Jyunko Morohoshi, Jyun Kanazawa
  • Publication number: 20110237803
    Abstract: 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: Application
    Filed: May 6, 2009
    Publication date: September 29, 2011
    Applicant: Bial - Portela & CA, S.A.
    Inventors: Alexander Beliaev, David Alexander Learmonth
  • Publication number: 20110166360
    Abstract: 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, con
    Type: Application
    Filed: March 13, 2009
    Publication date: July 7, 2011
    Applicant: BIAL - PORTELA & CA, S.A.
    Inventors: Alexander Beliaev, David Alexander Learmonth, Juan José Almena Perea, Gerhard Geib, Patrick Hitzel, Renat Kadyrov, David Voigtlaender
  • Publication number: 20110166142
    Abstract: 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: Application
    Filed: June 30, 2008
    Publication date: July 7, 2011
    Inventors: Eleanor Eiffe, Andrew Heaton, Catherine Walker, Alan James Husband
  • Patent number: 7968595
    Abstract: 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: Grant
    Filed: July 6, 2007
    Date of Patent: June 28, 2011
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, John A. Drewe, Shailaja Kasibhatla, William D. Kemnitzer, Ben Y. Tseng, Charles Blais, Denis Labrecque, Henriette Gourdeau
  • Patent number: 7960573
    Abstract: 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: Grant
    Filed: May 4, 2009
    Date of Patent: June 14, 2011
    Assignees: Children's Hospital Medical Center, Girindus America, Inc.
    Inventors: Kenneth David Reginald Setchell, Victor Dmitrievich Sorokin
  • Patent number: 7951838
    Abstract: 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: Grant
    Filed: August 20, 2010
    Date of Patent: May 31, 2011
    Assignee: Amgen Inc.
    Inventors: Daniel La, Patricia Lopez, Vinod F. Patel, Wenge Zhong
  • Publication number: 20110123929
    Abstract: 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: Application
    Filed: August 1, 2007
    Publication date: May 26, 2011
    Applicant: FUJIFILM Corporation
    Inventors: Akinori Fujita, Takashi Tamura, Kimi Ikeda, Daisuke Kashiwagi
  • Patent number: 7919490
    Abstract: 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: Grant
    Filed: October 4, 2007
    Date of Patent: April 5, 2011
    Assignee: Wyeth LLC
    Inventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
  • Patent number: 7915268
    Abstract: 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: Grant
    Filed: October 4, 2007
    Date of Patent: March 29, 2011
    Assignee: Wyeth LLC
    Inventors: Yingchun Lu, Celia Kingsbury, Adolph Bohnstedt, Michael Ohlmeyer, Vidyadhar Paradkar
  • Patent number: 7902187
    Abstract: 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: Grant
    Filed: August 22, 2008
    Date of Patent: March 8, 2011
    Assignee: Wyeth LLC
    Inventors: Irina Neagu, David Diller, Celia Kingsbury, Adolph C. Bohnstedt, Michael J. Ohlmeyer, Vidyadhar Paradkar, Nasrin Ansari
  • Patent number: 7880042
    Abstract: 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: Grant
    Filed: March 14, 2007
    Date of Patent: February 1, 2011
    Assignee: Bayer Schering Pharma AG
    Inventors: Markus Berger, Hartmut Rehwinkel, Heike Schäcke, Stefan Bäurle, Norbert Schmees
  • Publication number: 20100317862
    Abstract: 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: Application
    Filed: February 20, 2008
    Publication date: December 16, 2010
    Inventors: Javier Sancho Sanz, Adrián Velazquez Campoy, Nunilo Cremades Casasin
  • Publication number: 20100311778
    Abstract: 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: Application
    Filed: December 16, 2008
    Publication date: December 9, 2010
    Inventors: V S Prasadarao Lingam, Abraham Thomas, Laxmikant Atmaram Gharat, Deepak Vitthal Ukirde, Shantaram Kashinath Phatangare, Ajit Shankar Mindhe, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
  • Publication number: 20100298580
    Abstract: 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: Application
    Filed: November 13, 2008
    Publication date: November 25, 2010
    Applicant: BIAL - PORTELA & CA, S.A.
    Inventors: Brian Broadbelt, Alexander Beliaev, David Alexander Learmonth
  • Patent number: 7838553
    Abstract: 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: Grant
    Filed: August 30, 2006
    Date of Patent: November 23, 2010
    Assignee: Janssen Pharmaceutica NV
    Inventors: Xuqing Zhang, Xiaojie Li, Zhihua Sui
  • Patent number: 7812019
    Abstract: 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: Grant
    Filed: November 22, 2005
    Date of Patent: October 12, 2010
    Assignee: Abbott Laboratories
    Inventors: 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
  • Publication number: 20100217009
    Abstract: 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: Application
    Filed: May 21, 2008
    Publication date: August 26, 2010
    Applicant: BIAL - PORTELA & CA, S.A.
    Inventors: David Alexander Learmonth, Alexander Beliaev
  • Patent number: 7781483
    Abstract: This invention relates to benzopyran compounds of formula (I) wherein X is NR6, Y is a bond, SO or SO2, Z is C1-4alkyl group or phenyl group, W is hydrogen atom, hydroxy group, C1-6 alkoxy group, a halogen atom, C1-4alkyl group or C1-6alkylsulfonylamino group, R1 and R2 are independently of each other C1-3alkyl group, R3 is hydrogen atom, hydroxy group or methoxy group, m is an integer of 0 to 4, n is an integer of 0 to 4, V is a single bond, CR7R8, NR9, O, S, SO or SO2, R4 is hydrogen atom or C1-6alkyl group, R5 is hydrogen atom, C1-6alkyl group, C3-8cycloalkyl group, C3-8cycloalkenyl group, C6-14aryl group or C2-9heteroaryl group. These compounds are useful as an anti-arrhythmic agent.
    Type: Grant
    Filed: February 25, 2005
    Date of Patent: August 24, 2010
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Toru Tsukagoshi, Takayuki Nagatsuka, Tomoyuki Matsuda, Norio Hashimoto