Tetracyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/246)
  • Patent number: 9040519
    Abstract: This disclosure is directed to fused tetracyclic pyrido[4,3-b>]indole and pyrido[3,4-b]indole derivatives. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: February 18, 2011
    Date of Patent: May 26, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Sarvajit Chakravarty, Barry Patrick Hart, Rajendra Parasmal Jain
  • Publication number: 20150087755
    Abstract: The present invention relates to a composition, which comprises a) an organic material susceptible to oxidative, thermal or light-induced degradation, which is a polymer, an oligohydroxy compound, a wax, a fat or a mineral oil, with the proviso that the polymer is not a polypeptide, agar-agar or a component of agar-agar and the oligohydroxy compound is not glucose or a component of agar-agar; and b) a compound of formula (I) n is 1, 2, 3 or 4; when n is 1, R5 is H, C1-C30-alkyl, C3-C10-cycloalkyl, C6-C10-aryl, which is unsubstituted or substituted by C1-C8-alkyl, C1-C8-alkoxy, halogen or one phenyl, C7-C13-aralkyl, C2-C22-alkenyl, C3-C12-alkinyl, OH, C1-C30-alkyloxy, C3-C10-cycloalkyloxy, C6-C12-aryloxy, C7-C13-aralkyloxy, hydroxy-C1-C8-alkyl, carboxy-C1-C12-alkyl, C1-C12-alkoxycarbonyl-C1-C12-alkyl, C2-C30-alkyl, which is interrupted by one or more oxygen atoms, C2-C16-alkyl, which is interrupted by one sulfur atom, or NR?1R?2; when n is 2, R5 is C1-C12-alkane-diyl, C6-C14-arylene, C4-C8-cycloalkane-bis-(C1-
    Type: Application
    Filed: March 19, 2013
    Publication date: March 26, 2015
    Applicant: BASF SE
    Inventors: Werner Hoelzl, Bruno Rotzinger
  • Publication number: 20140349992
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Application
    Filed: June 9, 2014
    Publication date: November 27, 2014
    Applicant: Sunovion Pharmaceuticals Inc.
    Inventors: Larry Wendell Hardy, Michele L.R. Heffernan, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
  • Publication number: 20140332758
    Abstract: Donor-acceptor compounds with nitrogen containing polyaromatics as the acceptor with emission originated from the charge transfer (CT) state is disclosed. The donor-acceptor compound is provided that has the structure of Formula 1 shown below: wherein X1 to X12 is independently selected from the group consisting of C—R and N, wherein at least one of X1 to X12 is N, wherein each R is independently selected from the group consisting of hydrogen, deuterium, halide, alkyl, cycloalkyl, heteroalkyl, arylalkyl, alkoxy, aryloxy, amino, silyl, alkenyl, cycloalkenyl, heteroalkenyl, alkynyl, aryl, heteroaryl, acyl, carbonyl, carboxylic acids, ester, nitrile, isonitrile, sulfanyl, sulfinyl, sulfonyl, phosphino, and combinations thereof; and at least one of the R comprises a donor group with at least two electron-donating nitrogens.
    Type: Application
    Filed: May 9, 2013
    Publication date: November 13, 2014
    Applicant: UNIVERSAL DISPLAY CORPORATION
    Inventors: Raymond Kwong, Sui Tung Lam, Chi Hang Lee
  • Patent number: 8829008
    Abstract: 1- or 2-substituted (6aR,9aS)-3-(phenylamino)-5-6a,7,8,9,9a-hexahydro-5-methyl-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(1H or, 2H)-one compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: June 1, 2012
    Date of Patent: September 9, 2014
    Assignee: Takeda Pharmaceutical Company Limited
    Inventor: Peng Li
  • Patent number: 8772301
    Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: July 8, 2014
    Assignee: Sunovion Pharmaceuticals, Inc.
    Inventors: Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
  • Patent number: 8680107
    Abstract: The invention presents methods of identifying small molecule compounds that are activators of tumor suppressor protein p53 pathway, and its associated family members p63 and p73, function. The invention is further drawn to methods of killing tumor cells and treating cancers or other conditions requiring activation of the p53 family member pathways and DNA damage response pathways with the small molecules.
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: March 25, 2014
    Assignee: The Johns Hopkins University
    Inventors: Marikki Laiho, Karita Peltonen
  • Patent number: 8557827
    Abstract: The present invention relates to novel pyrimidine derivatives and their use in perfume compositions.
    Type: Grant
    Filed: March 27, 2012
    Date of Patent: October 15, 2013
    Assignee: International Flavors & Fragrances Inc.
    Inventors: Robert P. Belko, Anthony T. Levorse, Jr., Anubhav P. S. Narula, Michael G. Monteleone
  • Publication number: 20120277325
    Abstract: The present invention relates to novel pyrimidine derivatives and their use in perfume compositions. The novel pyrimidine derivatives of the present invention are represented by the following formula: wherein m and n are integers that when m is 0, n is 1; when m is 1, n is 0 or 1; or when m is 2, n is 0; wherein (CH)m and (CH)n are each independently optionally substituted with a substituent selected from the group consisting of methyl and ethyl; wherein X is selected from the group consisting of N, O, and S; and wherein R1 and R2 each independently represent H or a hydrocarbon group, or R1 and R2 together represent a fused ring or a ring system, with the proviso that when R1 is H, R2 is not H.
    Type: Application
    Filed: July 3, 2012
    Publication date: November 1, 2012
    Inventors: Robert P. Belko, Paul D. Jones, Anthony T. Levorse, JR., Michael G. Monteleone, Anubhav P.S. Narula, Franc T. Schiet
  • Publication number: 20120244182
    Abstract: The invention provides immunostimulatory compositions and methods of administration thereof. Also provided are methods of administering a tryptanthrin compound in an effective amount to enhance the immune response of a subject to an antigen. Also provided are methods of administering an effective amount of a tryptanthrin to stimulate the immune response in a subject for the treatment of cancer. Further provided are methods of administering a tryptanthrin compounds as an immunotherapeutic in the treatment of infectious diseases.
    Type: Application
    Filed: June 4, 2012
    Publication date: September 27, 2012
    Applicant: NOVARTIS VACCINES AND DIAGNOSTICS, INC.
    Inventor: Nicholas M. VALIANTE
  • Patent number: 8273751
    Abstract: 1- or 2-substituted (6aR,9aS)-3-(phenylamino)-5-6a,7,8,9,9a-hexahydro-5-methyl-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(1H or, 2H)-one compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: December 6, 2008
    Date of Patent: September 25, 2012
    Assignee: Takeda Pharmaceutical Company Limited
    Inventor: Peng Li
  • Patent number: 8207172
    Abstract: The invention relates to novel heterocycles of formula (I) processes for their preparation and their use for preparing medicaments for the treatment or prophylaxis of disorders, especially of hyperproliferative disorders.
    Type: Grant
    Filed: August 19, 2005
    Date of Patent: June 26, 2012
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Chengzhi Zhang, Jacques Dumas, Qingming Zhu, Roger Smith, Qingjie Liu, Sharad Verma, Jason Duquette, Qian Zhao, Dongping Fan, Georgiy Bondar, Philip Coish
  • Patent number: 8058457
    Abstract: A star-shaped oligothiophene-arylene derivative in which an oligothiophene having p-type semiconductor characteristics is bonded to an arylene having n-type semiconductor characteristics positioned in the central moiety of the molecule and forms a star shape with the arylene, thereby simultaneously exhibiting both p-type and n-type semiconductor characteristics. Further, an organic thin film transistor using the oligothiophene-arylene derivative. The star-shaped oligothiophene-arylene derivative can be spin-coated at room temperature, leading to the fabrication of organic thin film transistors simultaneously satisfying the requirements of high charge carrier mobility and low off-state leakage current.
    Type: Grant
    Filed: February 17, 2010
    Date of Patent: November 15, 2011
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Kook Min Han, Eun Jeong Jeong, Chang Ju Kim, Eun Kyung Lee
  • Patent number: 8053039
    Abstract: The present invention is directed towards polymerizable dichroic azo dyes comprising azo-chromophores having at least one standard mesogenic ring system attached to said chromophores and at least one polymerizable group leading to dyes having sufficient solubilty and a very high order parameter.
    Type: Grant
    Filed: March 23, 2004
    Date of Patent: November 8, 2011
    Assignee: Rolic AG
    Inventors: Thomas Peglow, Franco Moia, Zoubair Mohammed Cherkaoui, Mario Schwab
  • Patent number: 7902359
    Abstract: This invention relates to a compound of the following formula: wherein R1, R2, R3, G, and Z are defined herein. It also relates to is methods of treating autoimmune disease, cancer, and atherosclerosis with such a compound.
    Type: Grant
    Filed: December 11, 2007
    Date of Patent: March 8, 2011
    Assignee: Hutchison MediPharma Enterprises Limited
    Inventors: Tao Wang, Weihan Zhang, Xiaoqiang Yan, Weiguo Su, Jifeng Duan, Yu Cai
  • Patent number: 7692029
    Abstract: A star-shaped oligothiophene-arylene derivative in which an oligothiophene having p-type semiconductor characteristics is bonded to an arylene having n-type semiconductor characteristics positioned in the central moiety of the molecule and forms a star shape with the arylene, thereby simultaneously exhibiting both p-type and n-type semiconductor characteristics. Further, an organic thin film transistor using the oligothiophene-arylene derivative. The star-shaped oligothiophene-arylene derivative can be spin-coated at room temperature, leading to the fabrication of organic thin film transistors simultaneously satisfying the requirements of high charge carrier mobility and low off-state leakage current.
    Type: Grant
    Filed: April 28, 2005
    Date of Patent: April 6, 2010
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Kook Min Han, Eun Jeong Jeong, Chang Ju Kim, Eun Kyung Lee
  • Patent number: 7176310
    Abstract: This invention is directed to compound of the following formula (I): wherein R1, R2, R3 and R4 are as described herein. These compounds and pharmaceutical compositions containing the compounds are useful in treating inflammatory disorders in mammals.
    Type: Grant
    Filed: April 4, 2003
    Date of Patent: February 13, 2007
    Assignee: UCB SA
    Inventors: Theodore A. Baughman, Jim P. Boyce, Ihab S. Darwish, J. Jeffry Howbert, Nathan C. Ihle, Randy W. Jackson, Scott C. Jeffrey, Dean Maeda, Kraig M. Yager
  • Patent number: 7105506
    Abstract: Compounds of structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.
    Type: Grant
    Filed: May 2, 2002
    Date of Patent: September 12, 2006
    Assignee: Lilly Icos LLC
    Inventors: Mark W. Orme, Jason S. Sawyer, Lisa M. Schultze
  • Patent number: 6964960
    Abstract: The invention provides compounds of formula (I) wherein R is as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals, for use in the treatment of any state associated with high levels of activeted PARP.
    Type: Grant
    Filed: July 16, 2001
    Date of Patent: November 15, 2005
    Assignee: Novartis AG
    Inventors: Kaspar Zimmermann, Robert Portmann, Dean Franklin Rigel
  • Publication number: 20040138219
    Abstract: Piperidine derivatives of formula (I) and pharmaceutically derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.
    Type: Application
    Filed: January 26, 2004
    Publication date: July 15, 2004
    Inventors: David Thomas Davies, Graham Elgin Jones, Roger Edward Markwell, William Miller, Neil David Pearson
  • Patent number: 6680326
    Abstract: Novel polycyclic compounds of the formula [I], wherein R1, R2, R3, R4, R5, R6, R7, ring A, ring B, X, Y and Z are as defined herein and the pharmaceutically acceptable salts thereof. These compounds have antitumor activity and useful for the treatment of cancer.
    Type: Grant
    Filed: September 25, 2002
    Date of Patent: January 20, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Tsunehisa Aoyama, Kenichi Kawasaki, Miyako Masubuchi, Tatsuo Ohtsuka, Kiyoaki Sakata
  • Publication number: 20030199502
    Abstract: The invention provides compounds of formula (I) wherein R is as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals, for use in the treatment of any state associated with high levels of activeted PARP.
    Type: Application
    Filed: May 16, 2003
    Publication date: October 23, 2003
    Inventors: Kaspar Zimmermann, Robert Portmann, Dean Franklin Rigel
  • Publication number: 20030149264
    Abstract: The invention relates to chiral ionic liquids of the general formula
    Type: Application
    Filed: December 27, 2002
    Publication date: August 7, 2003
    Inventors: Peter Wasserscheid, Wilhelm Keim, Carsten Bolm, Andreas Bosmann
  • Patent number: 6599908
    Abstract: Fused polycyclic 2-aminopyrimidines of formula (1): wherein Ar is an optionally substituted aromatic or heteroaromatic group; X is a carbon or nitrogen atom; Y is a carbon or nitrogen atom; Z is a linker group; A together with X and Y forms an optionally substituted monocyclic or bicyclic aromatic or heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof are described. The compounds are potent and selective inhibitors of the protein tyrosine kinases p56lck and p59fyn and are of use in the prophylaxis and treatment of immune diseases, hyperproliferative disorders and other diseases in which inappropriate p56lck and/or p59fyn activity is believed to have a role.
    Type: Grant
    Filed: March 2, 2000
    Date of Patent: July 29, 2003
    Assignee: Celltech R & D Limited
    Inventors: Jeremy Martin Davis, Peter David Davis, David Festus Charles Moffat, Mark James Batchelor
  • Patent number: 6426416
    Abstract: The process for chemically modifying metal-free, colored anthraquinone or condensed anthraquinone compounds or the compounds prepared by said process for improving one or more properties thereof such as water dispersibility, compatibility with other organics, or increased chemical reactivity, wherein the process includes providing material with from 1-6 sulfonylhalide groups or sulfonate ester groups or mixtures thereof, and contacting the material under sulfonamido forming conditions with one or more reactants containing one or more poly(oxyalkylene) moieties, each of the reactants having from 1 to 4 functional amino groups, and each of the poly(oxyalkylene) moieties being comprised of from about 4 to about 200 epoxide reactant residues at least about 50 mole percent of which residues contain 2-4 carbons and wherein the total of said epoxide reactant residues is from about 4 to about 600.
    Type: Grant
    Filed: January 6, 2000
    Date of Patent: July 30, 2002
    Assignee: Millikan & Companay
    Inventors: Max Allen Weaver, Edward William Kluger, David Jesse Moody
  • Publication number: 20010034350
    Abstract: Compounds, compositions and methods are provided for treating malaria parasites in vitro and in vivo by administering indolo[2,1-b]quinazoline-6,12-dione compounds of Formula I.
    Type: Application
    Filed: May 8, 2001
    Publication date: October 25, 2001
    Inventors: Kevin K. Pitzer, John P. Scovill, Dennis E. Kyle, Lucia Gerena
  • Patent number: 6306865
    Abstract: Compounds of formula (I) or salts thereof, wherein the dotted line represents a single or double bond, R1 is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R2, R3, R4 and R5 are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O)nR8 wherein n is the integer 0, 1 or 2 and R8 is halo or alkyl or a group NR9R10 wherein R9 and R10 are both hydrogen, a group NR11R12 wherein R11 and R12 are the same or different and each is hydrogen or alkyl, a group OR13 wherein R13 is hydrogen or C1-4 of alkyl optionally substituted by halo; a C1-4 aliphatic group optionally substituted by a group OR14 or NR14R15 wherein R14 and R15 are the same or different and each is hydrogen or alkyl; or two of R2 to R5 are linked together to form a benzo group, or one of R2 to R5 is a group X—Y—R16 wherein X is CH2, NR17, CO or S(O)m and Y is CH2, NR17, O or S(O)m, or X—Y is O, NR17, —CH═CH— or N═N—, are disclosed as pharmacologic
    Type: Grant
    Filed: June 6, 2000
    Date of Patent: October 23, 2001
    Assignee: Glaxo Wellcome Inc.
    Inventors: William Pendergast, Scott Howard Dickerson, Julius Vass Johnson, Robert Ferone
  • Patent number: 6090941
    Abstract: Compounds of the formula (I) or salts thereof, ##STR1## wherein the dotted line represents a single or double bond, R.sup.1 is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group: R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O).sub.n R.sup.8 wherein n is the integer 0, 1 or 2 and R.sup.8 is halo or alkyl or a group NR.sup.9 R.sup.10 are both hydrogen, a group NR.sup.11 R.sup.12 wherein R.sup.11 and R.sup.12 are the same or different and each is hydrogen or alkyl, a group OR.sup.13 wherein R.sup.13 is hydrogen or C.sub.1-4 alkyl substituted by halo; a C.sub.1-4 aliphatic group optionally substituted by a group OR.sup.14 or NR.sup.14 R.sup.15 wherein R.sup.14 and R.sup.15 are the same or different and each is hydrogen or alkyl; ot two of R.sup.2 to R.sup.5 are linked together to form a benzp group, one of R.sup.2 to R.sup.3 is a group X--Y--R.sup.16 wherein X is CH.sub.2, NR.sup.17, CO, or S(O).sub.
    Type: Grant
    Filed: January 13, 1993
    Date of Patent: July 18, 2000
    Assignee: Glaxo Wellcome Inc.
    Inventors: William Pendergast, Scott Howard Dickerson, Julius Vass Johnson, Robert Ferone
  • Patent number: 5994544
    Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors and the method of preparing these compounds are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
    Type: Grant
    Filed: October 8, 1997
    Date of Patent: November 30, 1999
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, Christopher M. Tegley, Lin Zhi, James P. Edwards
  • Patent number: 5817810
    Abstract: The present invention provides a novel tryptanthrine derivative represented by a general formula: ##STR1## wherein R.sup.1 is an oxygen atom, or group represented by a formula: ##STR2## wherein R.sup.2A and R.sup.2B are the same or different and indicate a hydrogen atom, a cyano group, an acyl group, an alkoxycarbonyl group or an alkyl group, provided that R.sup.2A and R.sup.2B are not hydrogen atoms simultaneously; andR.sup.3A, R.sup.3B, R.sup.3C, R.sup.3D, R.sup.4A, R.sup.4B, R.sup.4C and R.sup.4D are the same or different and indicate a hydrogen atom or an alkyl group which may have a substituent, provided that when R.sup.1 is an oxygen atom, any one of R.sup.3A through R.sup.4D is a cyano group.Such a tryptanthrine derivative has an excellent electron transport capability to be suitably used for the electrophotosensitive material.
    Type: Grant
    Filed: July 24, 1996
    Date of Patent: October 6, 1998
    Assignee: Mita Industrial Co., Ltd.
    Inventors: Fumio Sugai, Syunichi Matsumoto, Nobuko Akiba, Yukimasa Watanabe, Hirofumi Kawaguchi, Sakae Saitoh
  • Patent number: 5786361
    Abstract: Compounds of the formula (I): ##STR1## are prepared by reaction of the phenylacetic acid derivatives substituted by the appropriate heterocycles, optionally in an activated form, with phenylglycinols. The compounds are suitable as active compounds in medicaments, in particular in medicaments having antiatherosclerotic activity.
    Type: Grant
    Filed: April 11, 1997
    Date of Patent: July 28, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Muller, Peter Eckenberg, Rudi Grutzmann, Hilmar Bischoff, Dirk Denzer, Ulrich Nielsch
  • Patent number: 5773613
    Abstract: The present invention provides a tryptoanthrinimine derivative represented by the general formula (Y): ##STR1## wherein R.sup.A to R.sup.M are as defined. Such a derivative of the general formula (Y) is superior in electron transferring capability. Accordingly, an electrophotosensitive material comprising a photosensitive layer containing this derivative (Y) is superior in sensitivity.
    Type: Grant
    Filed: November 28, 1995
    Date of Patent: June 30, 1998
    Assignee: Mita Industrial Co., Ltd.
    Inventors: Hirofumi Kawaguchi, Nobuko Akiba, Yukimasa Watanabe, Hiroaki Iwasaki, Yasuyuki Hanatani, Yasufumi Mizuta, Fumio Sugai, Sakae Saito, Syunichi Matsumoto, Toshiyuki Fukami, Ichiro Yamazato, Hisakazu Uegaito, Yuji Tanaka
  • Patent number: 5773644
    Abstract: The present invention relates to a class of compounds represented by the Formula I ##STR1## or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the .alpha..sub.v .beta..sub.3 integrin.
    Type: Grant
    Filed: March 27, 1997
    Date of Patent: June 30, 1998
    Assignee: G. D. Searle & Co.
    Inventors: Barbara B. Chen, Helen Y. Chen, Michael Clare, Shashidhar N. Rao, Mark A. Russell
  • Patent number: 5696130
    Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: December 9, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, David T. Winn, Mark E. Goldman, Lawrence G. Hamann, Lin Zhi, Luc J. Farmer, Robert L. Davis
  • Patent number: 5696127
    Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: December 9, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, Lin Zhi, James P. Edwards, Christopher M. Tegley, Sarah J. West
  • Patent number: 5693647
    Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: December 2, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, Lin Zhi, Christopher M. Tegley, David T. Winn, Lawrence G. Hamann, James P. Edwards, Sarah J. West
  • Patent number: 5693646
    Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: December 2, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, Christopher M. Tegley, Lin Zhi, James P. Edwards, Sarah J. West
  • Patent number: 5688810
    Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: November 18, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, Mark E. Goldman, Charlotte L.F. Pooley, David T. Winn, James P. Edwards, Sarah J. West, Christopher M. Tegley, Lin Zhi
  • Patent number: 5688808
    Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: November 18, 1997
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventors: Todd K. Jones, David T. Winn, Lin Zhi, Lawrence G. Hamann, Christopher M. Tegley, Charlotte L. F. Pooley
  • Patent number: 5616441
    Abstract: According to the present invention, there is provided a novel tryptoanthorine derivative represented by the formula: ##STR1## wherein R.sup.1a, R.sup.1b, R.sup.1c, R.sup.1d, R.sup.2a, R.sup.2b, R.sup.2c, and R.sup.2d are the same or different and indicate a hydrogen atom, an alkyl group or a halogenated alkyl group; provided that R.sup.1a, R.sup.1b, R.sub.1c and R.sup.1d do not indicate a hydrogen atom, simultaneously. Tryptoanthorine and a derivative thereof are suitably used for an electrophotosensitive material because of their excellent electron transferring capability.
    Type: Grant
    Filed: September 13, 1995
    Date of Patent: April 1, 1997
    Assignee: Mita Industrial Co., Ltd.
    Inventors: Hirofumi Kawaguchi, Yasufumi Mizuta, Syunichi Matsumoto, Nobuko Akiba, Toshiyuki Fukami, Ichiro Yamazato, Hisakazu Uegaito, Yuji Tanaka
  • Patent number: 5486512
    Abstract: A method of treating cognitive deficiencies is described by administering a quinazoline derivative of the general formula ##STR1## wherein A represents ##STR2## in which n is 1-10, P is a bond or (CH.sub.2).sub.m in which m is 0-10, and M is .dbd.O, .dbd.S, .dbd.NR, .dbd.CRR', ##STR3## novel compounds of the above are also described as well as methods of manufacture and pharmaceutical compositions.
    Type: Grant
    Filed: March 17, 1994
    Date of Patent: January 23, 1996
    Assignee: Warner-Lambert Company
    Inventor: Vlad E. Gregor
  • Patent number: 5441955
    Abstract: Methods, compounds and compositions are provided form inhibiting the growth of pathogenic mycobacteria in vitro and of treatment of pathogenic mycobacterial infections in vivo using indolo[2,1-b]quinazoline-6,12-dione compounds of the formula (I): ##STR1## wherein A, B, C, D, E, F, G and H are independently selected from carbon and nitrogen, or A and B or C and D can be taken together to be nitrogen or sulfur, and the pharmaceutically acceptable salts thereof. The methods, compounds and compositons are particularly useful for inhibiting the growth of Mycobacterium tuberculosis, and may be used alone, or in combination with other anti-Mycobacterium tuberculosis agents, such as isoniazid, rifampin, pyrazinamide, rifabutin, streptomycin and ciprofloxacin, to provide new agents for the treatment of tuberculosis, including multidrug-resistant tuberculosis (MDRTB).
    Type: Grant
    Filed: November 19, 1993
    Date of Patent: August 15, 1995
    Assignee: PathoGenesis Corporation
    Inventors: William R. Baker, Lester A. Mitscher
  • Patent number: 5439916
    Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treating allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.
    Type: Grant
    Filed: August 31, 1990
    Date of Patent: August 8, 1995
    Assignee: Schering Corporation
    Inventors: Ashit K. Ganguly, Richard J. Friary, John H. Schwerdt, Marvin I. Siegel, Sidney R. Smith, Edmund J. Sybertz
  • Patent number: 5420259
    Abstract: Tryptanthrine derivative of the formula ##STR1## where the rings A and B may be benzofused and/or substituted and X is a radical which is derived from a CH-acidic heterocyclic structure which may have a further tryptanthrine radical or from a hydrazinoanthraquinone or, if one or both of the rings A and B are benzofused and/or substituted by phthaloyl, is furthermore oxygen, are used as colorants.
    Type: Grant
    Filed: September 23, 1994
    Date of Patent: May 30, 1995
    Assignee: BASF Aktiengesellschaft
    Inventors: Andreas Guentner, Guenther Seybold, Gerhard Wagenblast
  • Patent number: 5329006
    Abstract: Chromogenic lactam compounds of the formula ##STR1## in which the ring A is an aromatic or heteroaromatic radical which has 6 ring atoms and may contain a fused aromatic ring, it being possible for both the ring A and the fused ring to be substituted;the ring B is an unsubstituted or substituted benzene ring;Z is ##STR2## R is hydrogen; unsubstituted or substituted C.sub.1 -C.sub.12 alkyl, cycloalkyl having 5 to 10 carbon atoms; unsubstituted or substituted aryl or aralkyl; C.sub.1 -C.sub.12 acyl; N-(lower alkyl)carbamoyl; or N-arylcarbamoyl which is unsubstituted or substituted on the ring;Q is C.sub.1 -C.sub.12 alkylene, aryl-C.sub.1 -C.sub.4 alkylene, 1,2-cycloalkylene, 1,2- or 1,8-arylene or aralkylene; andX.sub.1 and X.sub.2, independently of one another, are each hydrogen; unsubstituted or substituted alkyl having a maximum of 12 carbon atoms; acyl having 1 to 8 carbon atoms; cycloalkyl having 5 to 10 carbon atoms; or unsubstituted or ring-substituted aralkyl or aryl; or (X.sub.1 and X.sub.
    Type: Grant
    Filed: September 6, 1991
    Date of Patent: July 12, 1994
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans Baumann, Ian J. Fletcher
  • Patent number: 5284563
    Abstract: An electrocatalyst for use in electrolytic reduction of carbon dioxide gas in an aqueous solution. The electrocatalyst is formed of nickel alkyl cyclam which is expressed by the general formula: ##STR1## where each of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 is selected from the group consisting of hydrogen atom and aliphatic saturated hydrocarbon group expressed by the formula of C.sub.n H.sub.2n+1 ; wherein at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 is the aliphatic saturated hydrocarbon group in which n is a number ranging from 1 to 22. The nickel alkyl cyclam as the electrocatalyst is excellent in stability and energy consumption improving effect while exhibiting a high carbon dioxide gas reduction effect, as compared with conventional nickel cyclam.
    Type: Grant
    Filed: April 24, 1991
    Date of Patent: February 8, 1994
    Assignees: Nissan Motor Co., Ltd., Masamichi Fujihira
    Inventors: Masamichi Fujihira, Yoshiki Hirata, Kosaku Suga, Uichi Akiba, Yasuo Nakamura
  • Patent number: 5244595
    Abstract: 1. A mesomorphic compound represented by the following formula 8 I]: ##STR1## wherein R.sub.1 and R.sub.2 respectively denote a straight chain or branch chain allyl group having 1-18 carbon atoms, wherein --CH.sub.2 -- in the alkyl group may be substituted by ##STR2## on condition that hetero atoms are not adjacent each other, R.sup.2 may be hydrogen atom, halogen atom, cyano group and trifluoromethyl group; n is 0 or 1, with the proviso that A.sup.1 denotes a single bond, ##STR3## when n is 0, A.sup.1 denotes a single bond when n is 1; A.sup.2 denotes any one of ##STR4## and X.sup.1, X.sup.2, Z.sup.1 and Z.sup.2 denote independently any one of hydrogen atom, halogen atom, cyano group and trifluoromethyl group, with proviso that X.sup.1, X.sup.2, Z.sup.1 and Z.sup.2 may not be all hydrogen atoms; Y denotes any one of ##STR5## a single bond.
    Type: Grant
    Filed: July 15, 1991
    Date of Patent: September 14, 1993
    Assignee: Canon Kabushiki Kaisha
    Inventors: Yoko Yamada, Takao Takiguchi, Takashi Iwaki, Takeshi Togano, Shinichi Nakamura
  • Patent number: 5202433
    Abstract: A polysaccharide derivative prepared by replacing a part or the whole of hydrogen atoms of hydroxyl and/or amino groups of a polysaccharide with one or more atomic groups represented by the following formula (1), (2) or (3) is new and useful for the separation of optical isomers: ##STR1## wherein the number of carbon atoms constituting R is 1 to 30 and R is a group having at least one asymmetric center.
    Type: Grant
    Filed: January 18, 1991
    Date of Patent: April 13, 1993
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Yoshio Okamoto, Koichi Hatada
  • Patent number: 5196431
    Abstract: The present invention is novel compounds which are 2-substituted amino-4,6-di-tertiarybutyl-5-hydroxy-1,3-pyrimidines and pharmaceutically acceptable acid addition or base salts thereof, pharmaceutical compositions and methods of use therefor. The invention compounds are described as having activity as inhibitors of 5-lipoxygenase and/or cyclooxygenase providing treatment of conditions advantageously affected by such inhibition including inflammation, arthritis, pain, fever and the like. Thus, the present invention is also a pharmaceutical composition or method of manufacturing a pharmaceutical composition for the use of treating the noted conditions.
    Type: Grant
    Filed: February 24, 1992
    Date of Patent: March 23, 1993
    Assignee: Warner-Lambert Company
    Inventors: Thomas R. Belliotti, David T. Connor, Catherine R. Kostlan
  • Patent number: 5180735
    Abstract: The present invention relates to a compound of the formula: ##STR1## wherein A is halogen, N(O)mR.sup.1 R.sup.2, N.sup..sym. R.sup.1 R.sup.2 R.sup.3 .multidot.X.sup..crclbar., S(O)nR.sup.1 or S.sup..sym. (O)mR.sup.1 R.sup.2 .multidot.X.sup..crclbar. where R.sup.1, R.sup.2 and R.sup.3 are each optionally substituted hydrocarbon or heterocyclic group, X.sup..crclbar. is a counter anion; m is an integer of 0 or 1; n is an integer of 0 to 2; R.sup.1 and R.sup.2 may form a nitrogen-containing or a sulfur-containing heterocyclic ring, which may further form a condensed ring, with the adjacent nitrogen atom or sulfur atom, and these nitrogen-containing or sulfur-containing heterocyclic rings may have substituents, Z is O or NR.sup.4 where R.sup.
    Type: Grant
    Filed: August 29, 1990
    Date of Patent: January 19, 1993
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shoji Kishimoto, Shogo Marui, Takeshi Fujita