Plural Ring Chalcogens In The Polycyclo Ring System Or The Piperazine Ring Bonded Directly To The Polycyclo Ring System Patents (Class 544/378)
  • Publication number: 20140309418
    Abstract: Gambogenic acid derivatives having a structure shown as Formula (I) or (II), salts, preparation method and application thereof in the treatment of tumor. Compared with gambogenic acid, the gambogenic acid derivatives exhibit more potent anti-tumor activities.
    Type: Application
    Filed: September 28, 2012
    Publication date: October 16, 2014
    Inventors: Wantao Chen, Xu Wang, Zhiyuan Zhang, Chenping Zhang, Li Mao, Ping Zhang, Qin Xu, Ming Yan, Jianjun Zhang, Jinsong Pan, Yan Lv, Rongxin Deng, Weiliu Qiu
  • Publication number: 20140242097
    Abstract: A method for promoting entry of an agent (introduced agent) into a cell, the method comprising the step of complexing the introduced agent in the presence of an entry-promoting agent and then exposing to cells, wherein the entry-promoting agent comprises a linear and/or branched or cyclic polymonoguanide/polyguanidine, polybiguanide, analogue or derivative thereof according to the following Formula 1a & b. The method also provides a means for formation of nanoparticles formed between the entry promoting agent and the introduced agent.
    Type: Application
    Filed: October 11, 2012
    Publication date: August 28, 2014
    Applicant: THE ROYAL VETERINARY COLLEGE
    Inventors: Liam Good, Kantaraja Chindera, Valentina Gburcik
  • Patent number: 8716329
    Abstract: The present invention provides compounds of the formula (I) wherein: X1, X2 and X3 are heteroatoms; R4, R5, R6, R7, R8, R9 and R10 are independently selected from H, halo, —OH, —NO2, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR1—, —C(O)NR1NR2—, —C(O)O—, —OC(O)—, —NR1CO2—, —O—, —NR1C(O)NR2—, —OC(O)NR1—, —NR1NR2—, —NR1C(O)—, —S—, —SO—, —SO2—, —NR1—, —SO2NR1—, —NR1R2, or —NR1SO2—, wherein R1 and R2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR1R2, R1 and R2 optionally together with the nitrogen atom form an optionally substituted 5-12 me
    Type: Grant
    Filed: June 24, 2013
    Date of Patent: May 6, 2014
    Assignee: University of Kentucky
    Inventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
  • Patent number: 8698117
    Abstract: The present invention relates to compounds represented by the following Formulas (I) and (II), Ring-A of Formulas I and II can be, for example, an aryl group, and Q? and Q?? can each be independently selected from groups, such as, halogen, —OH, —CN, amine groups, amide groups, carboxylic acid ester groups, carboxylic acid groups, alkenyl groups, alkynyl groups, carbonate groups, sulfide groups, and sulfonic acid ester groups. The present invention also relates to photochromic compositions and photochromic articles that include one or more photochromic compounds, such as represented by Formula II.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: April 15, 2014
    Assignee: Transitions Optical, Inc.
    Inventors: Meng He, Anil Kumar, Darrin R. Dabideen
  • Publication number: 20140018342
    Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
    Type: Application
    Filed: April 4, 2012
    Publication date: January 16, 2014
    Inventors: Wen-Lian Wu, Duane A. Burnett, William J. Greenlee
  • Patent number: 8470875
    Abstract: The present invention provides compounds of the formula (I) or a pharmaceutically acceptable salt, ester or prodrug thereof.
    Type: Grant
    Filed: February 13, 2012
    Date of Patent: June 25, 2013
    Assignee: University of Kentucky
    Inventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
  • Publication number: 20130039904
    Abstract: The present invention discloses a gamboge acid cyclization analogs, their preparation methods and applications by semi-synthesis with the following structural formula I-III: Where ring A, ring B or/and ring C is 4-10 membered saturated or/and unsaturated aliphatic ring aliphatic heterocycle or aryl heterocycle. R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 or/and R12 is, independently at each occurrence, optionally substituted substituent of glycosyl, multi-hydroxyl, amino acid, acyloxy, phosphoric acid oxy, sulfonyloxy, alkoxy, aryloxy, heterocyclic oxy, thiol, aliphatic or cyclic group containing oxygen, sulfur, nitrogen or phosphorus, one of the substituents or combinations thereof. The present invention has antitumor activity management, antiviral, antibacterial and antifungal activity management, as anti-tumor, anti-viral, immune, antibacterial and antifungal agents, with other known anti-tumor, anti-viral, immune, together with the application of antibacterial and antifungal.
    Type: Application
    Filed: August 2, 2010
    Publication date: February 14, 2013
    Applicant: Liaoning Lifeng Scientific & Technology Development Company Ltd.
    Inventor: Lifeng Xu
  • Patent number: 8188089
    Abstract: Compounds of Formula I are described: preferably subject to the proviso that either (a) R2 and R3 together form —O—CH(R10)—O—, or (b) R5 and R6 together form —O—CH(R10)—O—, wherein R10 is H, halo, or loweralkyl. Pharmaceutical salts, formulations, and methods of using the same in the treatment of cancer are also described.
    Type: Grant
    Filed: December 20, 2006
    Date of Patent: May 29, 2012
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Kuo-Hsiung Lee, Linyi Wei, Kenneth F. Bastow, Arnold Brossi, Tian-Shung Wu
  • Publication number: 20120126185
    Abstract: The present invention relates to compounds represented by the following Formulas (I) and (II), Ring-A of Formulas I and II can be, for example, an aryl group, and Q? and Q?? can each be independently selected from groups, such as, halogen, —OH, —CN, amine groups, amide groups, carboxylic acid ester groups, carboxylic acid groups, alkenyl groups, alkynyl groups, carbonate groups, sulfide groups, and sulfonic acid ester groups. The present invention also relates to photochromic compositions and photochromic articles that include one or more photochromic compounds, such as represented by Formula II.
    Type: Application
    Filed: August 31, 2011
    Publication date: May 24, 2012
    Applicant: TRANSITIONS OPTICAL, INC.
    Inventors: Meng He, Anil Kumar, Darrin R. Dabideen
  • Patent number: 8158623
    Abstract: The invention discloses a new use of a class of heptacyclic compounds in the preparation of formulations for the prevention and treatment of diabetes and metabolic syndromes; the present invention also discloses a new class of heptacyclic compounds; the present invention also discloses a process for preparing the heptacyclic compounds and a composition containing the same. The heptacyclic compounds of the present invention can be used to effectively preventing or treating diseases such as diabetes and metabolic syndromes.
    Type: Grant
    Filed: May 29, 2007
    Date of Patent: April 17, 2012
    Assignee: Shanghai Institute of Materia Medica Chinese Academy of Sciences
    Inventors: Jianhua Shen, Ying Leng, Hualiang Jiang, Junhua Chen
  • Patent number: 8124652
    Abstract: The present invention provides compounds of the formula (I) wherein: X1, X2 and X3 are heteroatoms; R4, R5, R6, R7, R8, R9 and R10 are independently selected from H, halo, —OH, —NO2, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR1—, —C(O)NR1NR2—, —C(O)O—, —OC(O)—, —NR1CO2—, —O—, —NR1C(O)NR2—, —OC(O)NR1—, —NR1NR2—, —NR1C(O)—, —S—, —SO—, —SO2—, —NR1—, —SO2NR1—, —NR1R2, or —NR1SO2—, wherein R1 and R2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR1R2, R1 and R2 optionally together with the nitrogen atom form an optionally substituted 5-12 me
    Type: Grant
    Filed: January 25, 2010
    Date of Patent: February 28, 2012
    Assignee: University of Kentucky
    Inventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
  • Publication number: 20110152289
    Abstract: The present invention relates to dimeric derivatives of 10-trifluoromethylated artemisinin of formula (I) below: Formula (I) and the pharmaceutically acceptable salts thereof, and also to the preparation method thereof and to the uses thereof, especially in the treatment of cancer.
    Type: Application
    Filed: July 29, 2009
    Publication date: June 23, 2011
    Applicants: PIERRE FABRE MEDICAMENT, UNIVERSITE PARIS-SUD
    Inventors: Jean-Pierre Begue, Daniele Bonnet-Delpon, Benoit Crousse, Anais Fournial, Celine Mordant, Jacques Fahy
  • Publication number: 20110144094
    Abstract: This invention concerns novel substituted heterocyclic tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Application
    Filed: February 16, 2011
    Publication date: June 16, 2011
    Inventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
  • Publication number: 20110130363
    Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: January 31, 2011
    Publication date: June 2, 2011
    Applicant: Genentech, Inc.
    Inventors: Steven Do, Richard Goldsmith, Tim Heffron, Aleksandr Kolesnikov, Steven Staben, Alan G. Olivero, Michael Siu, Daniel P. Sutherlin, Bing-Yan Zhu, Paul Goldsmith, Tracy Bayliss, Adrian Folkes, Neil Pegg
  • Publication number: 20100324067
    Abstract: The present invention relates to tetracyclodipyrano-coumarin compounds of general formula (I), wherein the substituents are defined herein. These compounds exihibit dual biological activities of anti human immunodeficiency virus type 1 (HIV-1) infection and anti-Mycobacterium Tuberculosis (TB) infection.
    Type: Application
    Filed: November 5, 2007
    Publication date: December 23, 2010
    Inventors: Gang Liu, Hai Xue, Tao Ma, Ziwei Chen, Lin Wang
  • Patent number: 7846926
    Abstract: The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.
    Type: Grant
    Filed: April 14, 2005
    Date of Patent: December 7, 2010
    Assignee: Pierre Fabre Medicament
    Inventors: Thierry Imbert, Yves Guminski, Jean-Marc Barret, Anna Kruczynski
  • Patent number: 7834001
    Abstract: Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.
    Type: Grant
    Filed: November 8, 2005
    Date of Patent: November 16, 2010
    Assignee: Piramal Life Sciences Limited
    Inventors: Bansi Lal, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More
  • Publication number: 20100266570
    Abstract: The present invention relates to dimeric derivatives of 10-trifluoromethylated artemisinin of formula (I): or a pharmaceutically acceptable salt thereof with B1 and B2 selected from C?O, CHOH and CH2, as well as to their use in treating cancer and to their preparation method.
    Type: Application
    Filed: December 22, 2008
    Publication date: October 21, 2010
    Applicants: Pierre Fabre Medicament, Centre National De La Recherche Scientifique, Universite Paris-Sud 11
    Inventors: Jean-Pierre Begue, Danièle Bonnet-Delpon, Benoît Crousse, Fabienne Grellepois, Constance Chollet, Jacques Fahy, Céline Mordant
  • Publication number: 20100173905
    Abstract: The invention discloses a new use of a class of heptacyclic compounds in the preparation of formulations for the prevention and treatment of diabetes and metabolic syndromes; the present invention also discloses a new class of heptacyclic compounds; the present invention also discloses a process for preparing the heptacyclic compounds and a composition containing the same. The heptacyclic compounds of the present invention can be used to effectively preventing or treating diseases such as diabetes and metabolic syndromes.
    Type: Application
    Filed: May 29, 2007
    Publication date: July 8, 2010
    Inventors: Jianhua Shen, Ying Leng, Hualiang Jiang, Junhua Chen
  • Publication number: 20100120760
    Abstract: A compound of the formula (I): as defined herein, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing a compound of the formula (I) for use in inhibiting hepatitis C virus polymerase and/or of treating or preventing an illness due to hepatitis C virus,
    Type: Application
    Filed: March 25, 2008
    Publication date: May 13, 2010
    Applicant: ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANG
    Inventors: Uwe Koch, Angela Claire Mackay, Frank Narjes, Ian Stansfield
  • Patent number: 7700584
    Abstract: The present invention provides curcumol derivatives of the following formula (I) or pharmaceutical acceptable salts thereof: wherein, Y is selected from the group consisting of ?CHR2, —CH2R2, ?O, ?—OH or —OR1;R1 is selected from H, R, RCO or HO3S; and R is selected from the group consisting of H; saturated or unsaturated linear C1-10 hydrocarbon group and the like; R2 is selected from the group consisting of F; Cl; Br; I; H; —OH; —OR; —HSO3 and the like; with the proviso that both R1 and R2 are not H. The present invention also provides anti-tumor or antiviral pharmaceutical compositions comprising said derivatives or pharmaceutical acceptable salts thereof. The present invention further provides the use of said derivatives or pharmaceutical acceptable salts thereof in the preparation of a medicament for prophylaxis and/or treatment tumor or an antiviral medicament.
    Type: Grant
    Filed: May 26, 2005
    Date of Patent: April 20, 2010
    Assignee: Hangzhou Minsheng Pharmaceuticals Co., Ltd.
    Inventors: Shulong Wang, Dianwu Guo, Zhaoke Meng
  • Patent number: 7678904
    Abstract: The present invention provides compounds of the formula (I) wherein: X1, X2 and X3 are heteroatoms; R4, R5, R6, R7, R8, R9 and R10 are independently selected from H, halo, —OH, —NO2, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR1—, —C(O)NR1NR2—, —C(O)O—, —OC(O)—, —NR1CO2—, —O—, —NR1C(O)NR2—, —OC(O)NR1—, —NR1NR2—, —NR1C(O)—, —S—, —SO—, —SO2—, —NR1—, —SO2NR1—, —NR1R2, or —NR1SO2—, wherein R1 and R2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR1R2, R1 and R2 optionally together with the nitrogen atom form an optionally substituted 5-12 me
    Type: Grant
    Filed: January 7, 2005
    Date of Patent: March 16, 2010
    Assignee: University of Kentucky
    Inventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
  • Publication number: 20100004234
    Abstract: Resorcylic acid lactones having a C5-C6 cis double bond and a ketone at C7 and other compounds capable of Michael adduct formation are potent and stable inhibitors of a subset of protein kinases having a specific cysteine residue in the ATP binding site.
    Type: Application
    Filed: August 6, 2009
    Publication date: January 7, 2010
    Inventors: Daniel V. Santi, Ralph C. Reid, C. Richard Hutchinson, Kurt F. Sundermann, Janice Lau
  • Publication number: 20090176801
    Abstract: The invention provides lapachone analogs and derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment or prevention of cancer or precancerous conditions.
    Type: Application
    Filed: October 16, 2008
    Publication date: July 9, 2009
    Applicant: ArQule, Inc.
    Inventors: Mark Ashwell, Manish Tandon, Jean-Marc Lapierre, Syed Ali, Yanbin Liu, Chiang J. Li
  • Publication number: 20090170843
    Abstract: The present invention relates to novel podophyllotoxin derivatives substituted in the 4-position by a substituted (poly)aminoalkylaminoacetamide chain, to their process of preparation and to their use as medicament as anticancer agents.
    Type: Application
    Filed: April 14, 2005
    Publication date: July 2, 2009
    Inventors: Thierry Imbert, Yves Guminski, Jean-Marc Barret, Anna Kruczynski
  • Publication number: 20080287433
    Abstract: A new artemisinin derivatives, of following general formula (I): In which: a and b are a single or a double bond, n1 and n2 are 0 or 1, R1 is a fluoroalkyl group or a fluoroaryl group, R2 is a hydrogen atom, or a halogen atom, or a group, if appropriate ionisable, making it possible to render said compounds of formula (I) water-soluble, R3 is a group, if appropriate ionisable, making it possible to render said compounds of formula (I) water-soluble, R4 is H or OH. The invention also relates to the process by which they are obtained, and their uses in pharmaceutical compositions intended for the treatment of malaria.
    Type: Application
    Filed: July 9, 2008
    Publication date: November 20, 2008
    Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Jean-Pierre Begue, Daniele Bonnet-Delpon, Benoit Crousse, Michele Ourevitch, Fatima Chorki, Fabienne Grellepois, Guillaume Magueur
  • Patent number: 7439238
    Abstract: This invention relates to the use of certain C-10 substituted derivatives of artemisinin of general formula (I) in the treatment and/or prophylaxis of diseases caused by infection with a parasite, certain novel C-10 substitued derivatives of artemisinin, processes for their preparation and pharmaceutical compositions containing such C-10 substituted derivatives. The compounds are particularly effective in the treatment of malaria, neosporosis and coccidiosis.
    Type: Grant
    Filed: January 9, 2006
    Date of Patent: October 21, 2008
    Assignee: The Hong Kong University of Science and Technology
    Inventors: Richard K. Haynes, William Wai-Lun Lam, Ho-Wai Chan, Hing-Wo Tsang, Man-Ki Cheung, Gisela Greif, Gabriele Schmuck, Arnd Voerste
  • Publication number: 20080125411
    Abstract: A means and method for treating malaria, schistosomiasis, and cancer using a spiro or dispiro 1,2,4-trioxolane is described. The preferred 1,2,4-trioxolanes include a spiroadamantane group on one side of the trioxolane group, and a spirocyclohexyl on the other side of the trioxolane group. In comparison to artemisinin semisynthetic derivatives, the compounds of this invention are structurally simple, easy to synthesize, non-toxic, and potent against malarial parasites. The compounds of the invention unexpectedly provide a single-dose cure for malaria, as well as prophylactic activity against the same. The compounds are also active against schistosomiasis and cancer.
    Type: Application
    Filed: October 31, 2007
    Publication date: May 29, 2008
    Applicant: MEDICINES FOR MALARIA VENTURE MMV
    Inventors: JONATHAN L. VENNERSTROM, YUXIANG DONG, SUSAN A. CHARMAN, SERGIO WITTLIN, JACQUES CHOLLET, DARREN J. CREEK, XIAOFANG WANG, KAMARAJ SRIRAGHAVAN, LIN ZHOU, HUGUES MATILE, WILLIAM N. CHARMAN
  • Patent number: 7312242
    Abstract: Compounds of the formula having anti-tumor activity, wherein R1 and R2 are as described herein
    Type: Grant
    Filed: July 9, 2004
    Date of Patent: December 25, 2007
    Assignee: University of Kentucky
    Inventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
  • Patent number: 7244730
    Abstract: A 2-iminopyrrolidine derivative represented by the formula: {wherein ring B represents a benzene ring, pyridine ring, etc.; R101–R103 represent hydrogen, halogen, C1-6 alkyl, etc.; R5 represents hydrogen, C1-6 alkyl, C1-6 alkoxy-C1-6 alkyl, etc.; R6 represents hydrogen, C1-6 alkyl, C1-6 alkyloxycarbonyl, etc.; Y1 represents a single bond, —CH2—, etc.; Y2 represents a single bond, —CO—, etc.; and Ar represents hydrogen, a group represented by the formula: [wherein R10—R14 represent hydrogen, C1-6 alkyl, hydroxyl, C1-6 alkoxy, etc.; and R11 and R12 or R12 and R13 may bond together to form a 5- to 8-membered heterocyclic ring], etc.}, or a salt thereof.
    Type: Grant
    Filed: April 19, 2002
    Date of Patent: July 17, 2007
    Assignee: Eisai Co., Ltd
    Inventors: Shuichi Suzuki, Makoto Kotake, Mitsuaki Miyamoto, Tetsuya Kawahara, Akiharu Kajiwara, Ieharu Hishinuma, Kazuo Okano, Syuhei Miyazawa, Richard Clark, Fumihiro Ozaki, Nobuaki Sato, Masanobu Shinoda, Atsushi Kamada, Itaru Tsukada, Fumiyoshi Matsuura, Yoshimitsu Naoe, Taro Terauchi, Yoshiaki Oohashi, Osamu Ito, Hiroshi Tanaka, Takashi Musya, Motoji Kogushi, Tsutomu Kawada, Toshiyuki Matsuoka, Hiroko Kobayashi, Ken-ichi Chiba, Akifumi Kimura, Naoto Ono
  • Patent number: 6984640
    Abstract: This invention relates to the use of certain C-10 substituted derivatives of artemisinin of general formula (I) in the treatment and/or prophylaxis of diseases caused by infection with a parasite, certain novel C-10 substituted deriviatives of artemisinin, processes for their preparation and pharmaceutical compositions containing such C-10 substituted derivatives. The compounds are particularly effective in the treatment of malaria, neosporosis and coccidiosis.
    Type: Grant
    Filed: July 14, 1999
    Date of Patent: January 10, 2006
    Assignee: Bayer Aktiengesellschaft
    Inventors: Richard K. Haynes, William Wai-Lun Lam, Ho-Wai Chan, Hing-Wo Tsang, Man-Ki Cheung, Gisela Greif, Gabriele Schmuck, Arnd Voerste
  • Publication number: 20040077631
    Abstract: The invention relates to the mesylates of a group of piperazine derivatives and to a process for the preparation of these mesylates in an economic way in the high yield and of high purity. According to the process of the invention the synthesis of the piperazine ring and the mesylate formation are combined in a single reaction step. The invention relates to the mesylate of compounds of the formula (I) wherein X is a bicyclic heterocyclic phenyl group and Y is methyl, ethyl (optionally substituted with fluorine), cycloalkyl (3-7C) methyl, benzyl or m-phenyl benzyl.
    Type: Application
    Filed: August 15, 2003
    Publication date: April 22, 2004
    Inventors: Marcel P.M. van Aar, Stefanus J. Schouten, Jan Zorgdrager, Michiel C. Heslinga
  • Patent number: 6699858
    Abstract: This invention concerns the compounds of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is zero, 1, 2, 3, 4, 5 or 6; X is CH2 or O; R1 and R2 each independently are hydrogen, C1-6alkyl, C1-6alkylcarbonyl, halomethylcarbonyl or C1-6alkyl substituted with hydroxy, C1-6alkyloxy, carboxyl, C1-6alkylcarbonyloxy, C1-6alkyloxycarbonyl or aryl; or R1 and R2 taken together with the nitrogen atom to which they are attached may form a morpholinyl ring or an optionally substituted heterocycle; R3 and R4 are both halogen; or R3 is halogen and R4 is hydrogen; or R3 is hydrogen and R4 is halogen; and aryl is phenyl or phenyl substituted with 1, 2 or 3 substituents selected from halo, hydroxy, C1-6alkyl and halomethyl. The compounds of formula (I) may be used as therapeutic agents.
    Type: Grant
    Filed: November 12, 2002
    Date of Patent: March 2, 2004
    Inventors: José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Pilar Gil-Lopetegui
  • Patent number: 6677353
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: January 13, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Publication number: 20030050306
    Abstract: A heteroaryl derivative having the formula (I) 1
    Type: Application
    Filed: June 25, 2002
    Publication date: March 13, 2003
    Applicant: H. Lundbeck A/S
    Inventors: Thomas Ruhland, Christian Krog-Jensen, Ivan Mikkelsen, Mario Rottlander, Gitte Mikkelsen, Ejner Knud Moltzen, Kim Andersen
  • Patent number: 6514967
    Abstract: The invention relates to compounds of the following general formula (I): in which: R1 and R2 represent a hydrogen atom, or form a ring, especially a benzene ring, R3 represents a hydrogen atom or an alkyl group, especially a methyl group, X and Y, independently of one another, represent a carbon atom, or a heteroatom such as a sulphur atom S, or a group with the formula (a) in which R4 and R5 represent a hydrogen atom or a methyl group, or R4 and R5 form a heterocycle, and their use for the preparation of a drug intended for the treatment of pathologies associated with abnormally high concentrations of extracellular glutamate.
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: February 4, 2003
    Assignee: Centre National de la Recherche Scientifique
    Inventors: Jean-Marc Kamenka, Isoline Caubere, Gerard Barbanel
  • Publication number: 20020156084
    Abstract: A chemical composition, namely n-benzyl piperazine and derivatives, for use as a weight control product and or a quality of life enhancer. The unobviousness lies in the fact that the aforementioned compounds work without the unwanted side effects of many weight control products, due to their “harmonious” balancing of the norepinephrine and serotonin receptors in the brain.
    Type: Application
    Filed: April 1, 2002
    Publication date: October 24, 2002
    Inventor: Bryant G. Valent
  • Patent number: 6462041
    Abstract: The present invention is directed to gambogic acid, analogs and derivatives thereof, represented by the general Formulae I-III: wherein R1-R5 are defined herein. The present invention also relates to the discovery that compounds having Formula I-III are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled cell growth and spread of abnormal cells occurs.
    Type: Grant
    Filed: February 1, 2000
    Date of Patent: October 8, 2002
    Assignee: Cytovia, Inc.
    Inventors: Sui Xiong Cai, Han-Zhong Zhang, Yan Wang, Ben Tseng, Shailaja Kasibhatla, John A. Drewe
  • Patent number: 6458803
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.
    Type: Grant
    Filed: November 23, 2001
    Date of Patent: October 1, 2002
    Assignee: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6455520
    Abstract: The invention concerns amide derivatives of formula (I) wherein R3 is (1-6C)alkyl or halogeno; m is 0-3, p is 0-2 and q is 0-4; each of R1 and R2 is a group such as hydroxy, halogeno, trifluoromethyl and cyano; R4 is a basic group such as amino, (1-6C)alkylamino, di-[(1-6C)alkyl]amino, di-[(1-6C)alkyl]amino-(1-6C)alkyl, di-[(1-6C)alkyl]amino-(2-6C)alkoxy, heteroaryl, heteroaryloxy, heteroaryl-(1-6C)alkoxy, heterocyclyl, heterocyclyloxy and heterocyclyl-(1-6C)alkoxy; and Q2 is a group such as heteroaryl, heteroaryloxy or heteroaryl-(1-6C)alkoxy which is optionally substituted; or pharmaceutically-acceptable salts or in-vivo-cleavable esters thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical conditions mediated by cytokines.
    Type: Grant
    Filed: March 23, 2001
    Date of Patent: September 24, 2002
    Assignee: Astra Zeneca AB
    Inventors: Dearg S Brown, George R Brown
  • Patent number: 6340704
    Abstract: The present invention provides a compound represented by the formula: wherein R1 is an amino group which may be substituted; R2 is a hydrogen atom or a lower alkyl group which may be substituted; X is a methyne group which may be substituted or N(O)m (m is 0 or 1); a ring A is a homo- or hetero-cycle which is substituted by a halogen atom, lower alkyl, lower alkoxy or lower alkylenedioxy; and a ring B is a homo- or hetero-cycle which may be substituted; or a salt thereof, which exhibits excellent cell differentiation-inducing action and cell differentiation-inducing factor action-enhancing action, and is useful in the treatment and prevention of various nerve diseases or bone/joint diseases.
    Type: Grant
    Filed: July 19, 1999
    Date of Patent: January 22, 2002
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Koki Kato
  • Patent number: 6323206
    Abstract: Disclosed is a method of treating a subject with a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to the subject a therapeutically effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.
    Type: Grant
    Filed: January 21, 1998
    Date of Patent: November 27, 2001
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Charles F. Schwender, Charles R. Mackay, Julia C. Pinto, Walter Newman
  • Patent number: 6153611
    Abstract: Novel non-dopaminergic antiischemic compounds have Formula I: ##STR1## wherein R=R.sub.1 and is independently H, C.sub.1-4 alky C.sub.1-4 alkoxy, C.sub.1-4 trihaloalkyl or halogen, or R and R.sub.1 may be taken together to form an --O(CH.sub.2).sub.m O-- (m=1 or 2);X=a 3-indolyl, phenyl, naphthalenyl or 2-benzothiazolyl residue;n=0, 1, 2 or 3; ##STR2## R.sub.2 =R.sub.3 and is independently H or C.sub.1-4 alkyl; and R.sub.4 =phenyl, 2-thienyl, 2-quinolinyl, 4-pyridinyl or substituted phenyl.
    Type: Grant
    Filed: June 25, 1993
    Date of Patent: November 28, 2000
    Assignee: Bristol-Myers Squibb Company
    Inventors: Ronald J. Mattson, John D. Catt
  • Patent number: 6113812
    Abstract: A photochromic article that includes a host material and a photochromic amount of a benzopyran compound, the benzopyran compound represented by one of the formulas: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are selected from hydrogen, a stable organic radical, a heterocyclic group, halogen, a nitrogen-substituted group, and a nitrogen-substituted ring compound.
    Type: Grant
    Filed: August 4, 1997
    Date of Patent: September 5, 2000
    Assignee: Vision-Ease Lens, Inc.
    Inventor: Frank J. Hughes
  • Patent number: 6100265
    Abstract: A thiopyran derivative represented by the following formula (I) or (I'), or the salt thereof. ##STR1## wherein A is S or --CH.dbd.CH--; the dotted line indicates that the bond may be either present or absent; Z and Z' are typically ##STR2## L is an ethylene or trimethylene group; Y is CH or N; n is 2; B is a carbonyl group; m is 0 or 1; D is a phenyl group; and E.sub.1 and E.sub.2 are hydrogen atoms. These compounds exhibit a strong serotonin-2 blocking action and highly safe. Some compounds also exhibit an .alpha..sub.1 -blocking action and therefore are useful as an antihypertensive agent with less side effects. Thus, the thiopyran derivatives are useful as drugs for the treatment of circulatory diseases in general such as hypertension, ischemic heart disease, cerebrovascular disturbance, and peripheral circulatory disturbance.
    Type: Grant
    Filed: July 15, 1999
    Date of Patent: August 8, 2000
    Assignee: Suntory Limited
    Inventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Norio Inomata
  • Patent number: 5869520
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: January 8, 1997
    Date of Patent: February 9, 1999
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
  • Patent number: 5869662
    Abstract: Benzopyran compounds represented by the formulas: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, and R.sub.10 are selected from hydrogen, a stable organic radical, a heterocyclic group, halogen, a nitrogen-substituted group, and a nitrogen-substituted ring compound.
    Type: Grant
    Filed: July 17, 1997
    Date of Patent: February 9, 1999
    Assignee: Vision-Ease Lens, Inc.
    Inventor: Frank J. Hughes
  • Patent number: 5869490
    Abstract: The compounds of formula I: ##STR1## wherein X is H.sub.2 or O;R.sup.1 is hydrogen, hydroxy, halo, trifluoromethyl, trifluoromethoxy, alkyl, alkoxy, aralkoxy, alkanoyloxy, amino, mono- or di-alkylamino, alkanamido or alkanesulfonamido;Z is defined by ##STR2## wherein R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as defined in the specification; or a pharmaceutically acceptable salt thereof, are useful for the treatment of brain dopamine dysregulation.
    Type: Grant
    Filed: October 9, 1997
    Date of Patent: February 9, 1999
    Assignee: American Home Products Corporation
    Inventor: Gary Paul Stack
  • Patent number: 5847168
    Abstract: A photochromic article that includes a host material and a photochromic amount of a naphthopyran compound, the naphthopyran compound represented by the formula: ##STR1## wherein R.sub.1 ', R.sub.2 ', R.sub.3 ', R.sub.4 ', R.sub.5 ', R.sub.6 ', R.sub.7 ', R.sub.8 ', R.sub.9 ', R.sub.10 ', R.sub.1 ", R.sub.2 ", R.sub.3 ", R.sub.4 ", R.sub.5 ", R.sub.6 ", R.sub.7 ", R.sub.8 ", R.sub.9 ", and R.sub.10 " are each selected from the following group: a stable organic radical, a heterocyclic group, halogen, a nitrogen-substituted group, and a nitrogen-substituted ring compound.
    Type: Grant
    Filed: December 1, 1997
    Date of Patent: December 8, 1998
    Assignee: Vision-Ease Lens, Inc.
    Inventor: Frank J. Hughes
  • Patent number: 5847167
    Abstract: Novel carbamoyloxylabdanes, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure and treating cardiac failure utilizing compounds and compositions thereof are disclosed.
    Type: Grant
    Filed: June 30, 1997
    Date of Patent: December 8, 1998
    Assignee: Hoechst Marion Roussel, Inc.
    Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley