Acyclic -c(=x)-, Wherein X Is Chalcogen, Attached Directly Or Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/473)
  • Patent number: 7914700
    Abstract: The invention relates to compounds of formula (I): wherein R1 and R2 are each independently selected from the group: H, F, Cl and CH3; n1 and n2 are each independently integers 3 to 20; q and r are each independently integers 0, 1 or 2, with the proviso that q+r is ?1; D is a divalent chiral radical selected from the group: wherein R3 is a C1 to C6 straight or branched chain alkyl group; and each B1 and B2 is a divalent radical independently selected from the group: R4-substituted-1,4-phenyl, wherein R4 is H, —CH3 or —OCH3; 2,6-naphthyl; and 4,4?-biphenyl; with the provisos that when q+r=3, at least one of B1 and B2 is R4-substituted-1,4-phenyl; and when q+r=4, at least two of B1 and B2 are R4-substituted-1,4-phenyl. The invention further relates to liquid crystal compositions comprising compounds of formula (I) and polymer networks derived from the polymerization of the liquid crystal compositions.
    Type: Grant
    Filed: March 30, 2007
    Date of Patent: March 29, 2011
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Marc B. Goldfinger, Jose Manuel Rodriguez-Parada, Lee A. Silverman, Kai Qi
  • Publication number: 20110040109
    Abstract: Method of producing C8-C15 hydrocarbons. comprising providing a ketone starting material; providing an aldol starting material comprising chloromethylfurfural; mixing the ketone starting material and the aldol starting material in a reaction in the presence of a proline-containing catalyst selected from the group consisting of Zn(Pro)2, Yb(Pro)3, and combinations thereof, or a catalyst having one of the structures (I), (II) or (III), and in the presence of a solvent, wherein the solvent comprises water and is substantially free of organic solvents, where (I), (II) and (III) respectively are where R1 is a C1-C6 alkyl moiety, X=(OH) and n=2. In (III), X may be CH2, sulfur or selenium, M may be Zn, Mg, or a lanthanide, and R1 and R2 each independently may be a methyl, ethyl, phenyl moiety.
    Type: Application
    Filed: August 17, 2009
    Publication date: February 17, 2011
    Applicant: LOS ALAMOS NATIONAL SECURITY, LLC
    Inventors: Louis A. Silks, John C. Gordon, Ruilan Wu, Susan Kloek Hanson
  • Publication number: 20110040110
    Abstract: Method of producing C8-C15 hydrocarbons comprising providing a ketone starting material; providing an aldol starting material comprising hydroxymethylfurfural; mixing the ketone starting material and the aldol starting material in a reaction in the presence of a proline-containing catalyst selected from the group consisting of Zn(Pro)2, Yb(Pro)2, and combinations thereof, or a catalyst having one of the structures (I), (H) or (III), and in the presence of a solvent, wherein the solvent comprises water and is substantially free of organic solvents, where (I), (II) and (III) respectively are: where R1 is a C1-C6 alkyl moiety, X?(OH) and n=2. In (III), X may be CH2, sulfur or selenium, M may be Zn, Mg, or a lanthanide, and R1 and R2 each independently may be a methyl, ethyl, phenyl moiety.
    Type: Application
    Filed: August 17, 2009
    Publication date: February 17, 2011
    Applicant: LOS ALAMOS NATIONAL SECURITY, LLC
    Inventors: Louis A. Silks, John C. Gordon, Ruilan WU, Susan Kloek Hanson
  • Patent number: 7884126
    Abstract: The invention relates to novel indazole derivatives as cited in claim 1, which are inhibitors of CHK1, CHK2 and SGK kinases and can be used to treat cancer and other diseases.
    Type: Grant
    Filed: January 10, 2007
    Date of Patent: February 8, 2011
    Assignee: Merck Patent GmbH
    Inventors: Markus Klein, Rolf Gericke, Werner Mederski, Norbert Beier, Florian Lang
  • Publication number: 20100317870
    Abstract: The invention generally relates to novel polymers (SMAMPs) and their syntheses and use. The polymers exhibit promising properties of AMPs. In particularly, for example, a ring-opening metathesis polymerization (ROMP) platform was developed that allows syntheses of SMAMPs that employ a minimum number of norbornene-based building blocks and/or enable easy and independent variation of hydrophobic and hydrophilic groups in the monomer units and/or along the polymeric backbone to finetune and select desirable properties of the polymers.
    Type: Application
    Filed: June 8, 2010
    Publication date: December 16, 2010
    Inventors: Gregory Tew, Ahmad E. Madkour, Karen Lienkamp, Ashlan Marie Musante
  • Publication number: 20100297541
    Abstract: Compounds of the formula (I), wherein X is a single bond, CRaRbO, S, NRc or NCORc; Z is formula (II) or C3-C20heteroaryl; L, L1, L2, L3, L4, L5, L6, L7 and L8 for example independently of one another are hydrogen or an organic substituent; Ra, Rb and Rc independently of one another are hydrogen or an organic substituent; R is for example is C5-C20heteroaryl or C6-C14 aryl; and Y is an inorganic or organic anion; are suitable as photolatent acid generators.
    Type: Application
    Filed: September 29, 2008
    Publication date: November 25, 2010
    Applicant: BASF SE
    Inventors: Pascal Hayoz, Hitoshi Yamato, Toshikage Asakura
  • Publication number: 20100292190
    Abstract: The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.
    Type: Application
    Filed: February 14, 2006
    Publication date: November 18, 2010
    Applicant: Bionomics Limited
    Inventors: Jason Hugh Chaplin, Gurmit Singh Gill, Damian Wojciech Grobelny, Bernard Luke Flynn
  • Publication number: 20100280186
    Abstract: Aromatic polyamines are derivatized with polycarboxylic acids or their derivatives to form polyamine amides) containing pendant amine groups; the derivatives have enhanced curative properties when used as curatives for polyureas, hybrid epoxy-urethanes, hybrid urea-urethanes, chain extenders for polyurethane and polyurea elastomers, and also for reaction injection molding (RIM) products.
    Type: Application
    Filed: August 28, 2009
    Publication date: November 4, 2010
    Inventors: Herman P. Benecke, Alex W. Kawczak, Daniel B. Garbark
  • Patent number: 7674909
    Abstract: The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are H, Me; R3 is (2-6C)heterocycloalkyl(1-4C)alkyl, (2-5C)heteroaryl(1-4C)alkyl, (6C)aryl (1-4C)alkyl, (1-4C)(di)alkylaminocarbonylamino(2-4C)alkyl, (2-6C) heterocycloalkylcarbonylamino(2-4C)alkyl, R5-(2-4C)alkyl or R5-carbonyl(1-4C)alkyl; R4 is (2-5C)heteroaryl, (6C)aryl, (3-8C)cycloalkyl, (2-6C)heterocycloalkyl or (1-6C) alkyl and R5 is (di)(1-4C)alkylamino, (1-4C)alkoxy, amino, hydroxy, (6C)arylamino, (di)(3-4C)alkenylamino, (2-5C)heteroaryl(1-4C)alkylamino, (6C)aryl(1-4C) alkylamino, (di)[(1-4C)alkoxy(2-4C)alkyl]amino, (di)[(1-4C)alkylamino(2-4C) alkyl]amino, (di)[amino(2-4C)alkyl]amino or (di)[hydroxy(2-4C)alkyl]amino. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to regulate fertility.
    Type: Grant
    Filed: December 16, 2003
    Date of Patent: March 9, 2010
    Assignee: N.V. Organon
    Inventors: Cornelis Marius Timmers, Willem Frederik Karstens
  • Patent number: 7670991
    Abstract: The invention relates to novel substituted benzoylcyclohexenones of the formula (I) in which Q, R1, R2, R3, R4, R5, Y and Z have one of the meanings given in the disclosure, to processes for their preparation, and to their use.
    Type: Grant
    Filed: May 3, 2002
    Date of Patent: March 2, 2010
    Assignee: Bayer CropScience AG
    Inventors: Hans-Georg Schwarz, Klaus-Helmut Muller, Stefan Herrmann, Dorothee Hoischen, Kristian Kather, Stefan Lehr, Otto Schallner, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen, Shinichi Narabu, Akihiko Yanagi, Shinichi Shirakura, Toshio Goto, Yoshihiro Yamaguchi
  • Publication number: 20100029752
    Abstract: A pharmaceutical composition containing a pharmaceutical diluent and a compound of formula II: wherein: R8?H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, —C(O)R4, where R4 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms, or —OH, —OR7 or —NR7, where R7 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, optionally containing halogen atoms; R9=—OR5, —NR5, —NH—NH—R5 where R5 is H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, allyl, or alkylaryl, optionally containing halogen atoms; R10?H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, or alkylaryl, or —CH2C(O)R6, where R6 is OR7 and NR7, where R7?H, C1-C20 alkyl, cycloalkyl, alkenyl, aryl, arylalkyl, allyl, or alkylaryl and can optionally contain halogen atoms. Also included in the invention are methods of using the pharmaceutical compositions and the chemical compounds used in the compositions.
    Type: Application
    Filed: July 26, 2006
    Publication date: February 4, 2010
    Inventors: Francis P. Kuhajda, Craig A. Townsend, Susan M. Medghalchi, Jill M. McFadden
  • Publication number: 20090227790
    Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).
    Type: Application
    Filed: April 7, 2009
    Publication date: September 10, 2009
    Inventor: Leu-Fen H. Lin
  • Publication number: 20090143602
    Abstract: Disclosed are compositions and methods for the production of mono-esters and di-esters from the reaction of HMF and a reactant selected from a diacid or a diacid derivative; typical reactants are PAN, phthaloyl dichloride, dimethyl phthalate, maleic acid, and maleic anhydride or mono-esters that can be prepared from HMF and MAN.
    Type: Application
    Filed: February 7, 2007
    Publication date: June 4, 2009
    Inventors: Herman P. Benecke, Jerry L. King, II, Alex Walter Kawczak, Donald W. Zehnder, II, Erica E. Hirschl
  • Patent number: 7514452
    Abstract: The present invention provides 2-furancarboxylic acid hydrazide compounds represented by General Formula (I) below, and prodrugs, physiologically acceptable salts, hydrates, solvates thereof: wherein A is a group represented by Formula (a) or the like: (wherein either R4 or R5 represents cyano, nitro or the like, and the other represents a hydrogen atom or the like); either R1 or R2 represents a group: -D-(X)m-R6 or the like, and the other represents a group: -E-(Y)n-R7, hydrogen atom, aryl or the like; R3 is a hydrogen atom or the like; D and E independently represent aryl; X and Y independently represent O or the like; R6 and R7 independently represent alkyl, aryl, arylalkyl or the like; and m and n are independently 0 or 1, provided that the aryl is optionally substituted.
    Type: Grant
    Filed: January 30, 2003
    Date of Patent: April 7, 2009
    Assignee: Dainippon Pharmaceutical Co., Ltd
    Inventors: Akihito Fujii, Toshiyuki Negoro, Chiaki Migihashi, Makoto Murata, Keiji Nakamura, Takashi Nukuda, Takafumi Matsumoto, Kiyomi Imano
  • Publication number: 20090018167
    Abstract: The present invention relates to chalcone and chalcone derivatives and analogs which are useful as angiogenesis inhibitors. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good activity as angiogenesis inhibitors. The present invention also relates to the use of chalcone and its analogs as antitumor/anticancer agents and to treat a number of conditions or disease states in which angiogenesis is a factor, including angiogenic skin diseases such as psoriasis, acne, rosacea, warts, eczema, hemangiomas, lymphangiogenesis, among numerous others, as well as chronic inflammatory disease such as arthritis.
    Type: Application
    Filed: August 22, 2008
    Publication date: January 15, 2009
    Applicants: J. Phillip Bowen, Emory University
    Inventors: J. Phillip Bowen, Thomas Philip Robinson, Tedman Ehlers, David Goldsmith, Jack Arbiser
  • Publication number: 20080249252
    Abstract: The invention relates to novel compounds of the formula I, II; III or IV wherein the general symbols are as defined in claim 1. These compounds are useful as surface modifiers for polymers in order to improve resistance to fog formation or water and oil repellency.
    Type: Application
    Filed: June 5, 2008
    Publication date: October 9, 2008
    Inventors: Piero Piccinelli, Manuele Vitali, Andrea Landuzzi, Giovanni Da Roit, Primo Carrozza, Markus Grob, Nicola Lelli
  • Patent number: 7423058
    Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
    Type: Grant
    Filed: December 21, 2006
    Date of Patent: September 9, 2008
    Assignee: Schering Corporation
    Inventors: Stephane L. Bogen, Weidong Pan, Sumei Ruan, Kevin X. Chen, Ashok Arasappan, Srikanth Venkatraman, Latha G. Nair, Mousumi Sannigrahi, Frank Bennett, Anil K. Saksena, F. George Njoroge, Viyyoor M. Girijavallabhan
  • Publication number: 20080161391
    Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.
    Type: Application
    Filed: February 13, 2008
    Publication date: July 3, 2008
    Applicants: The University of North Carolina, The University of Rochester Medical Center, Androscience Corporation
    Inventors: Kuo-Hsiung Lee, Li Lin, Charles C-Y Shih, Ching-Yuan Su, Junko Ishida, Hironori Ohtsu, Hui-Kang Wang, Hideji Itokawa, Chawnshang Chang
  • Publication number: 20080146660
    Abstract: The present invention relates to compounds capable of acting as androgen receptor antagonists, pharmaceutical formulations containing the same, and methods of use thereof. Such uses include, but are not limited to, use as antitumor agents, particularly for the treatment of cancers such as colon, skin and prostate cancer and to induce androgen receptor antagonist activity in a subject afflicted with an androgen-related affliction. Examples of androgen-related afflictions include, but are not limited to, baldness, hirsutism, behavioral disorders, acne, and uninhibited spermatogenesis wherein inhibition of spermatogenesis is so desired.
    Type: Application
    Filed: February 13, 2008
    Publication date: June 19, 2008
    Applicants: The University of North Carolina at Chapel Hill, The University of Rochester Medical Center, Androscience Corporation
    Inventors: Kuo-Hsiung Lee, Li Lin, Charles C-Y Shih, Ching-Yuan Su, Junko Ishida, Hironori Ohtsu, Hui-Kang Wang, Hideji Itokawa, Chawnshang Chang
  • Patent number: 7342041
    Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
    Type: Grant
    Filed: February 24, 2005
    Date of Patent: March 11, 2008
    Assignee: Schering Corporation
    Inventors: F. George Njoroge, Srikanth Venkatraman, Ashok Arasappan, Francisco Velazquez, Viyyoor M. Girijavallabhan
  • Patent number: 7314885
    Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds, processes for making the compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: March 22, 2006
    Date of Patent: January 1, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Alex Aronov, Upul K. Bandarage, David J. Lauffer, Pan Li, Ronald C. Tomlinson
  • Patent number: 7205330
    Abstract: The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
    Type: Grant
    Filed: February 24, 2005
    Date of Patent: April 17, 2007
    Assignee: Schering Corporation
    Inventors: Stephane L. Bogen, Weidong Pan, Sumei Ruan, Kevin X. Chen, Ashok Arasappan, Srikanth Venkatraman, Latha G. Nair, Mousumi Sannigrahi, Frank Bennett, Anil K. Saksena, F. George Njoroge, Viyyoor M. Girijavallabhan
  • Patent number: 7186849
    Abstract: Taxanes having an ester substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: June 25, 2003
    Date of Patent: March 6, 2007
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 7183300
    Abstract: Substituted aryl aminomethyl thiazole ureas and analogues thereof that act as inhibitors of viral capsid formation, including HIV capsid formation, are provided here. Generally the virus capsid formation inhibitors described herein are compounds of Formula I wherein the variables A, R1, R2, R3, R4, X, Y, Z, A5, A6, A7, R8, R9, R12, and R13 are defined herein. Pharmaceutical compositions comprising such compounds and methods of treating animals infected with a virus having a capsid protein are provided herein. Methods of using such compounds to treat human patients infected with an HIV virus and reducing the mortality of AIDS are also provided herein.
    Type: Grant
    Filed: November 10, 2005
    Date of Patent: February 27, 2007
    Inventors: Michael F. Summers, Atul Agarwal, Xi Chen, Milind Deshpande
  • Patent number: 7145025
    Abstract: A method for inhibiting and/or ameliorating the occurrence of diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals in a subject whereby a subject is administered a carotenoid structural analog, either alone or in combination with another carotenoid analog, or co-antioxidant formulation. The analog or analog combination is administered such that the subject's risk of experiencing diseases associated with reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals may be thereby reduced. The analog or analog combination may be administered to a subject for the inhibition and/or amelioration of ischemia-reperfusion injury, liver disease, cancer, cardiac arrhythmia and/or sudden cardiac death, and/or any disease that involves production of reactive oxygen species, reactive nitrogen species, radicals and/or non-radicals. In one embodiment, a water-soluble and/or water-dispersible astaxanthin analog is particularly effective.
    Type: Grant
    Filed: July 29, 2003
    Date of Patent: December 5, 2006
    Assignee: Hawaii Biotech, Inc.
    Inventors: Samuel Fournier Lockwood, Sean O'Malley, David G. Watumull, Laura M. Hix, Henry Jackson, Geoff Nadolski
  • Patent number: 7019024
    Abstract: The invention provides a pharmaceutical for treatment of neurological and neuropsychiatric disorders comprising a compound of the formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: March 28, 2006
    Assignee: Allelix Neuroscience Inc.
    Inventors: Vassil Iliya Ognyanov, Laurence A. Borden, Stanley Charles Bell, Jing Zhang
  • Patent number: 6972343
    Abstract: The invention concerns drug precursors with antimalarial effect, characterised in that it consists in quaternary bis-ammonium salts of general formula (I) wherein A and A?, identical or different, are respectively either a group A1 and A?1 of formula (1) wherein n=2 to 4; R?1 is hydrogen, C1-C5 alkyl, optionally substituted by an aryl, a hydroxy, an alkoxy, wherein the alkyl comprises 1 to 5 C, or aryloxy and W is halogen or a nucleofuge group; or a group A2 which represents formyl-CHO, or acetyl-COCH3.
    Type: Grant
    Filed: July 21, 2000
    Date of Patent: December 6, 2005
    Assignee: CNRS
    Inventors: Henri Vial, Marie-Laure Ancelin, Valerie Vidal, Michele Calas, Jean-Jacques Bourguignon, Eric Rubi
  • Patent number: 6872837
    Abstract: Taxanes having a heterosubstituted acetate substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: June 27, 2003
    Date of Patent: March 29, 2005
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 6861446
    Abstract: Taxanes having a heterosubstituted acetate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: November 24, 2003
    Date of Patent: March 1, 2005
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 6858740
    Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives and a process for preparing them and their uses. The invention also concerns a process for preparing ?-ethyl-2-oxo-1-pyrrolidine acetamide derivatives from unsaturated 2-oxo-1-pyrrolidine derivatives. Particularly the invention concerns novel intermediates and their use in methods for the preparation of S-?-ethyl-2-oxo-1-pyrrolidine acetamide.
    Type: Grant
    Filed: July 1, 2003
    Date of Patent: February 22, 2005
    Assignee: UCB Farchim S.A.
    Inventors: John Surtees, Violeta Marmon, Edmond Differding, Vincent Zimmermann
  • Patent number: 6841571
    Abstract: Disclosed are cathepsin S, K, F, L and B reversible inhibitory compounds of the formulas (Ia) and (Ib) where R2, R3, R4, R6, R8 and Y are defined herein. The compounds are useful for treating autoimmune and other diseases.
    Type: Grant
    Filed: October 24, 2002
    Date of Patent: January 11, 2005
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Younes Bekkali, Denice Mary Spero, Sanxing Sun, Yancey David Ward
  • Patent number: 6797712
    Abstract: Compounds of formula I, or a pharmaceutically acceptable salt thereof, The compounds of the present invention are suitable for the treatment of pain and migraine. Also disclosed are method for preparing the compounds, and pharmaceutical composition comprising the compounds as well as methods for treating pain and migraine using the pharmaceutical compositions.
    Type: Grant
    Filed: May 30, 2003
    Date of Patent: September 28, 2004
    Assignee: Gruenenthal GmbH
    Inventors: Corinna Maul, Werner Englberger, Michael Przewosny
  • Patent number: 6750245
    Abstract: Taxanes having a carbamoyloxy substituent at C(7), a hydroxy substituent at C(10, and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: February 6, 2002
    Date of Patent: June 15, 2004
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 6747154
    Abstract: A process for preparing a compound of formula 1 from a compound of formula 2 the process comprising reacting in one step the compound of formula 2 with a compound of formula 3 wherein: X− is chlorine, bromine, iodine, methanesulfonate, or trifluoromethanesulfonate; R1 is hydroxy, C1-C4-alkyl, C1-C4-alkoxy, CF3, or fluorine; Ar is phenyl, naphthyl, thienyl, and furyl, each optionally mono- or disubstituted with one or two groups selected from C1-C4-alkyl, C1-C4-alkoxy, hydroxy, fluorine, chlorine, bromine, or CF3; Y− is chlorine, bromine, iodine, methanesulfonate, or trifluoromethanesulfonate; and R is hydroxy, methoxy, ethoxy, O—N-succinimide, O—N-phthalimide, phenyloxy, nitrophenyloxy, fluorophenyloxy, pentafluorophenyloxy, vinyloxy, 2-allyloxy, —S-methyl, —S-ethyl, or —S-phenyl.
    Type: Grant
    Filed: January 9, 2003
    Date of Patent: June 8, 2004
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Joerg Brandenburg, Waldemar Franz-Augustin Pfrengle, Werner Rall
  • Patent number: 6673833
    Abstract: Taxanes having a heterosubstituted acetate substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: February 2, 2001
    Date of Patent: January 6, 2004
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 6667318
    Abstract: The invention relates to novel compounds having formula (I) wherein Cy, X, Y, L and R1-6 are as defined herein. The compounds bind CD11/CD18 adhesion receptors such as Lymphocyte Function-associated Antigen-1 (LFA-1) and are therefore useful for treating disorders mediated by LFA-1 such as inflammation and autoimmune diseases.
    Type: Grant
    Filed: November 26, 2001
    Date of Patent: December 23, 2003
    Assignee: Genentech, Inc.
    Inventors: Daniel J. Burdick, Mark S. Stanley, David Oare, Mark E. Reynolds, Thomas R. Gadek, James C. Marsters
  • Patent number: 6649632
    Abstract: Taxanes having an ester substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: February 2, 2001
    Date of Patent: November 18, 2003
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 6620804
    Abstract: Novel selenophene compounds useful as anti-tumor agents are described. Preferred compounds include compounds of formula I: wherein R1 and R2 are independently selected from the group consisting of; H, CHO, CH2OH and CH2NH2; and X and Y are independently selected from the group consisting of Se, S, O, NCH3 and NH. Pharmaceutical compositions and a method for treating patients having tumors utilizing the disclosed selenophene compounds are also described.
    Type: Grant
    Filed: February 1, 2002
    Date of Patent: September 16, 2003
    Assignee: Purdue Research Foundation
    Inventors: Ching-jer Chang, Curtis L. Ashendel, Darrick Kim
  • Patent number: 6610860
    Abstract: Taxanes having an ester substituent at C(7), a hydroxy substituent at C(10), and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Grant
    Filed: February 2, 2001
    Date of Patent: August 26, 2003
    Assignee: FSU Research Foundation, Inc.
    Inventor: Robert A. Holton
  • Patent number: 6583175
    Abstract: This invention relates to novel alkylxanthates of formulae 1 to 3 and use of alkylxanthates of formulae 1 to 6 in the integrated pest management, more specifically alkyl xanthates are used as insect growth regulators for pest management in agricultural fields no or less environmental impact.
    Type: Grant
    Filed: March 30, 2001
    Date of Patent: June 24, 2003
    Assignee: Council of Scientific & Industrial Research
    Inventors: Janapala Venkateswara Rao, Yenamandra Venkateswarlu, Kondapuram Vijaya Raghavan
  • Patent number: 6552205
    Abstract: Taxane derivatives having alternative C10 substituents.
    Type: Grant
    Filed: October 27, 1999
    Date of Patent: April 22, 2003
    Assignee: Florida State University
    Inventors: Robert A. Holton, Ki-byung Chai
  • Publication number: 20030060638
    Abstract: Taxanes having a carbamoyloxy substituent at C(7), a hydroxy substituent at C(10, and a range of C(2), C(9), C(14), and side chain substituents.
    Type: Application
    Filed: February 6, 2002
    Publication date: March 27, 2003
    Applicant: Florida State University Research Foundation Inc.
    Inventor: Robert A. Holton
  • Patent number: 6521660
    Abstract: Taxane derivatives having an alkyl substituted C13 side chain.
    Type: Grant
    Filed: April 29, 2002
    Date of Patent: February 18, 2003
    Assignee: Florida State University
    Inventors: Robert A. Holton, Ki-Byung Chai, Hamid Idmoumaz, Hossain Nadizadeh, Yukio Suzuki
  • Patent number: 6500958
    Abstract: The present invention relates to compounds which are useful for efficient synthesis of 2-amino-4-oxobicyclo[3.1.0]hexane-2,6-dicarboxylic acids. The compounds according to the present invention comprise 2-oxobicyclo[3.1.
    Type: Grant
    Filed: June 24, 2002
    Date of Patent: December 31, 2002
    Assignee: Taisho Pharmaceutical Co., Ltd.
    Inventors: Atsuro Nakazato, Toshihito Kumagai, Kazunari Sakagami, Kazuyuki Tomisawa
  • Publication number: 20020198382
    Abstract: The invention relates to novel arylalkyl- or aryloxyalkyl-substituted oxiranecarboxyclic acids of the general formula I 1
    Type: Application
    Filed: June 18, 2002
    Publication date: December 26, 2002
    Inventor: Horst P.O. Wolf
  • Patent number: 6468444
    Abstract: Chiral dopants of the formula I Z1—Y1—(A1)m—Y2—M—Y3—X—Y4—(A2)n—Y5—Z2  I in which the variables have, independently of one another, the following meanings: A1 and A2 a spacer with a chain length of 1 to 30 carbon atoms; Y1 to Y5 a chemical bond, —O—, —S—, —C(═O)—, —C(═O)—O—, —O—C(═O)—, —CH═CH—C(═O)—O—, —O—C(═O)—O—, —C(═O)—N(R)— or —(R)N—C(═O)—, —CH2—O—, —O—CH2—, —CH═N—, —N═CH— or —N═N—; M a mesogenic group; R hydrogen, C1-C4-alkyl; Z1 and Z2 hydrogen, C1-C4-alkyl, a polymerizable group or a radical having a polymerizable group; x a dianhydrohexitol residue selected from the group consisting of dianhydrosorbitol, dianhydromannitol and dianhydroiditol;
    Type: Grant
    Filed: March 20, 2000
    Date of Patent: October 22, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Frank Meyer, Peter Schuhmacher, Frank Prechtl
  • Patent number: 6462208
    Abstract: Taxane derivatives having alternative C7 substituents.
    Type: Grant
    Filed: October 25, 1999
    Date of Patent: October 8, 2002
    Assignee: Florida State University
    Inventors: Robert A. Holton, Ki-Byung Chai
  • Publication number: 20020115870
    Abstract: A method of preparing a compound of formula I is described.
    Type: Application
    Filed: November 21, 2001
    Publication date: August 22, 2002
    Inventors: Jiann T?apos;suen Lin, Iuan-Yuan Wu, Yu-Tai Tao, E. Balasubramaniam
  • Patent number: 6410754
    Abstract: Novel spiropyran compounds, particularly with photochromic properties, are disclosed, as well as photochromic compositions and ophthalmic articles containing said compounds. The photochromes have been designed so as to have a high colorability, a high sensitivity to activating radiation breaking the pyran ring, to be entirely or practically free from coloration in a non activated non exposed state, to have an intense coloration following activation and a high coverage of the visible spectrum in combination with at least one other photochrome, and to have high rates of coloration/decoloration. The spiropyrans are easily produced and photochemically stable, and are, e.g., of formula (i), wherein L=(a); (b).
    Type: Grant
    Filed: November 14, 1997
    Date of Patent: June 25, 2002
    Assignee: Flamel Technologies
    Inventors: Gérard Soula, You-Ping Chan
  • Patent number: 6407268
    Abstract: 4-Benzoylpyrazoles of the formula I where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C2-C6-alkenyl, C2-C6-alkynyl, —OR10, —OCOR10, —OSO2R10, —S(O)nR10, —SO2OR10, —SO2NR3R10, —NR10SO2R10 or —NR10COR; Q is a pyrazole of the formula II,  which is attached in position 4 and, Substituted 4-benzoylpyralozoles.
    Type: Grant
    Filed: June 6, 2000
    Date of Patent: June 18, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Stefan Engel, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Guido Mayer, Martina Otten, Joachim Rheinheimer, Oliver Wagner, Matthias Witschel, Ulf Misslitz, Helmut Walter