Plural Ring Chalcogens In The Polycyclo Ring System Or The Piperazine Ring Bonded Directly To The Polycyclo Ring System Patents (Class 544/378)
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Publication number: 20140309418Abstract: 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: ApplicationFiled: September 28, 2012Publication date: October 16, 2014Inventors: 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
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Publication number: 20140242097Abstract: 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: ApplicationFiled: October 11, 2012Publication date: August 28, 2014Applicant: THE ROYAL VETERINARY COLLEGEInventors: Liam Good, Kantaraja Chindera, Valentina Gburcik
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Patent number: 8716329Abstract: 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 meType: GrantFiled: June 24, 2013Date of Patent: May 6, 2014Assignee: University of KentuckyInventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
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Patent number: 8698117Abstract: 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: GrantFiled: August 31, 2011Date of Patent: April 15, 2014Assignee: Transitions Optical, Inc.Inventors: Meng He, Anil Kumar, Darrin R. Dabideen
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Publication number: 20140018342Abstract: 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: ApplicationFiled: April 4, 2012Publication date: January 16, 2014Inventors: Wen-Lian Wu, Duane A. Burnett, William J. Greenlee
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Patent number: 8470875Abstract: The present invention provides compounds of the formula (I) or a pharmaceutically acceptable salt, ester or prodrug thereof.Type: GrantFiled: February 13, 2012Date of Patent: June 25, 2013Assignee: University of KentuckyInventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
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Publication number: 20130039904Abstract: 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: ApplicationFiled: August 2, 2010Publication date: February 14, 2013Applicant: Liaoning Lifeng Scientific & Technology Development Company Ltd.Inventor: Lifeng Xu
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Patent number: 8188089Abstract: 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: GrantFiled: December 20, 2006Date of Patent: May 29, 2012Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Linyi Wei, Kenneth F. Bastow, Arnold Brossi, Tian-Shung Wu
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Publication number: 20120126185Abstract: 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: ApplicationFiled: August 31, 2011Publication date: May 24, 2012Applicant: TRANSITIONS OPTICAL, INC.Inventors: Meng He, Anil Kumar, Darrin R. Dabideen
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Patent number: 8158623Abstract: 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: GrantFiled: May 29, 2007Date of Patent: April 17, 2012Assignee: Shanghai Institute of Materia Medica Chinese Academy of SciencesInventors: Jianhua Shen, Ying Leng, Hualiang Jiang, Junhua Chen
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Patent number: 8124652Abstract: 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 meType: GrantFiled: January 25, 2010Date of Patent: February 28, 2012Assignee: University of KentuckyInventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
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Publication number: 20110152289Abstract: 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: ApplicationFiled: July 29, 2009Publication date: June 23, 2011Applicants: PIERRE FABRE MEDICAMENT, UNIVERSITE PARIS-SUDInventors: Jean-Pierre Begue, Daniele Bonnet-Delpon, Benoit Crousse, Anais Fournial, Celine Mordant, Jacques Fahy
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Publication number: 20110144094Abstract: 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: ApplicationFiled: February 16, 2011Publication date: June 16, 2011Inventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez
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Publication number: 20110130363Abstract: 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: ApplicationFiled: January 31, 2011Publication date: June 2, 2011Applicant: 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
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TETRACYCLIC DIPYRANO-COUMARIN COMPOUNDS WITH ANTI-HIV AND ANTI-MYCOBACTERIUM TUBERCULOSIS ACTIVITIES
Publication number: 20100324067Abstract: 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: ApplicationFiled: November 5, 2007Publication date: December 23, 2010Inventors: Gang Liu, Hai Xue, Tao Ma, Ziwei Chen, Lin Wang -
Patent number: 7846926Abstract: 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: GrantFiled: April 14, 2005Date of Patent: December 7, 2010Assignee: Pierre Fabre MedicamentInventors: Thierry Imbert, Yves Guminski, Jean-Marc Barret, Anna Kruczynski
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Patent number: 7834001Abstract: 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: GrantFiled: November 8, 2005Date of Patent: November 16, 2010Assignee: Piramal Life Sciences LimitedInventors: Bansi Lal, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More
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Publication number: 20100266570Abstract: 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: ApplicationFiled: December 22, 2008Publication date: October 21, 2010Applicants: Pierre Fabre Medicament, Centre National De La Recherche Scientifique, Universite Paris-Sud 11Inventors: Jean-Pierre Begue, Danièle Bonnet-Delpon, Benoît Crousse, Fabienne Grellepois, Constance Chollet, Jacques Fahy, Céline Mordant
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Publication number: 20100173905Abstract: 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: ApplicationFiled: May 29, 2007Publication date: July 8, 2010Inventors: Jianhua Shen, Ying Leng, Hualiang Jiang, Junhua Chen
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Publication number: 20100120760Abstract: 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: ApplicationFiled: March 25, 2008Publication date: May 13, 2010Applicant: ISTITUTO DI RICERCHE DI BIOLOGIA MOLECOLARE P. ANGInventors: Uwe Koch, Angela Claire Mackay, Frank Narjes, Ian Stansfield
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Patent number: 7700584Abstract: 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: GrantFiled: May 26, 2005Date of Patent: April 20, 2010Assignee: Hangzhou Minsheng Pharmaceuticals Co., Ltd.Inventors: Shulong Wang, Dianwu Guo, Zhaoke Meng
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Patent number: 7678904Abstract: 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 meType: GrantFiled: January 7, 2005Date of Patent: March 16, 2010Assignee: University of KentuckyInventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
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Publication number: 20100004234Abstract: 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: ApplicationFiled: August 6, 2009Publication date: January 7, 2010Inventors: Daniel V. Santi, Ralph C. Reid, C. Richard Hutchinson, Kurt F. Sundermann, Janice Lau
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Publication number: 20090176801Abstract: 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: ApplicationFiled: October 16, 2008Publication date: July 9, 2009Applicant: ArQule, Inc.Inventors: Mark Ashwell, Manish Tandon, Jean-Marc Lapierre, Syed Ali, Yanbin Liu, Chiang J. Li
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Publication number: 20090170843Abstract: 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: ApplicationFiled: April 14, 2005Publication date: July 2, 2009Inventors: Thierry Imbert, Yves Guminski, Jean-Marc Barret, Anna Kruczynski
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Publication number: 20080287433Abstract: 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: ApplicationFiled: July 9, 2008Publication date: November 20, 2008Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Jean-Pierre Begue, Daniele Bonnet-Delpon, Benoit Crousse, Michele Ourevitch, Fatima Chorki, Fabienne Grellepois, Guillaume Magueur
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Patent number: 7439238Abstract: 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: GrantFiled: January 9, 2006Date of Patent: October 21, 2008Assignee: The Hong Kong University of Science and TechnologyInventors: Richard K. Haynes, William Wai-Lun Lam, Ho-Wai Chan, Hing-Wo Tsang, Man-Ki Cheung, Gisela Greif, Gabriele Schmuck, Arnd Voerste
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Publication number: 20080125411Abstract: 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: ApplicationFiled: October 31, 2007Publication date: May 29, 2008Applicant: MEDICINES FOR MALARIA VENTURE MMVInventors: 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
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Patent number: 7312242Abstract: Compounds of the formula having anti-tumor activity, wherein R1 and R2 are as described hereinType: GrantFiled: July 9, 2004Date of Patent: December 25, 2007Assignee: University of KentuckyInventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
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Patent number: 7244730Abstract: 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: GrantFiled: April 19, 2002Date of Patent: July 17, 2007Assignee: Eisai Co., LtdInventors: 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
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Patent number: 6984640Abstract: 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: GrantFiled: July 14, 1999Date of Patent: January 10, 2006Assignee: Bayer AktiengesellschaftInventors: Richard K. Haynes, William Wai-Lun Lam, Ho-Wai Chan, Hing-Wo Tsang, Man-Ki Cheung, Gisela Greif, Gabriele Schmuck, Arnd Voerste
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Publication number: 20040077631Abstract: 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: ApplicationFiled: August 15, 2003Publication date: April 22, 2004Inventors: Marcel P.M. van Aar, Stefanus J. Schouten, Jan Zorgdrager, Michiel C. Heslinga
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Patent number: 6699858Abstract: 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: GrantFiled: November 12, 2002Date of Patent: March 2, 2004Inventors: José Ignacio Andrés-Gil, Francisco Javier Fernández-Gadea, Pilar Gil-Lopetegui
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Patent number: 6677353Abstract: 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: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: 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
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Publication number: 20030050306Abstract: A heteroaryl derivative having the formula (I) 1Type: ApplicationFiled: June 25, 2002Publication date: March 13, 2003Applicant: H. Lundbeck A/SInventors: Thomas Ruhland, Christian Krog-Jensen, Ivan Mikkelsen, Mario Rottlander, Gitte Mikkelsen, Ejner Knud Moltzen, Kim Andersen
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Patent number: 6514967Abstract: 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: GrantFiled: December 16, 1999Date of Patent: February 4, 2003Assignee: Centre National de la Recherche ScientifiqueInventors: Jean-Marc Kamenka, Isoline Caubere, Gerard Barbanel
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Publication number: 20020156084Abstract: 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: ApplicationFiled: April 1, 2002Publication date: October 24, 2002Inventor: Bryant G. Valent
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Patent number: 6462041Abstract: 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: GrantFiled: February 1, 2000Date of Patent: October 8, 2002Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Han-Zhong Zhang, Yan Wang, Ben Tseng, Shailaja Kasibhatla, John A. Drewe
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Patent number: 6458803Abstract: 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: GrantFiled: November 23, 2001Date of Patent: October 1, 2002Assignee: 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
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Patent number: 6455520Abstract: 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: GrantFiled: March 23, 2001Date of Patent: September 24, 2002Assignee: Astra Zeneca ABInventors: Dearg S Brown, George R Brown
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Patent number: 6340704Abstract: 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: GrantFiled: July 19, 1999Date of Patent: January 22, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Shogo Marui, Masatoshi Hazama, Kohei Notoya, Koki Kato
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Patent number: 6323206Abstract: 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: GrantFiled: January 21, 1998Date of Patent: November 27, 2001Assignee: Millennium Pharmaceuticals, Inc.Inventors: Charles F. Schwender, Charles R. Mackay, Julia C. Pinto, Walter Newman
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Patent number: 6153611Abstract: 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: GrantFiled: June 25, 1993Date of Patent: November 28, 2000Assignee: Bristol-Myers Squibb CompanyInventors: Ronald J. Mattson, John D. Catt
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Patent number: 6113812Abstract: 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: GrantFiled: August 4, 1997Date of Patent: September 5, 2000Assignee: Vision-Ease Lens, Inc.Inventor: Frank J. Hughes
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Patent number: 6100265Abstract: 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: GrantFiled: July 15, 1999Date of Patent: August 8, 2000Assignee: Suntory LimitedInventors: Akira Mizuno, Makoto Shibata, Tomoe Iwamori, Norio Inomata
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Patent number: 5869520Abstract: 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: GrantFiled: January 8, 1997Date of Patent: February 9, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley
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Patent number: 5869490Abstract: 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: GrantFiled: October 9, 1997Date of Patent: February 9, 1999Assignee: American Home Products CorporationInventor: Gary Paul Stack
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Patent number: 5869662Abstract: 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: GrantFiled: July 17, 1997Date of Patent: February 9, 1999Assignee: Vision-Ease Lens, Inc.Inventor: Frank J. Hughes
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Patent number: 5847168Abstract: 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: GrantFiled: December 1, 1997Date of Patent: December 8, 1998Assignee: Vision-Ease Lens, Inc.Inventor: Frank J. Hughes
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Patent number: 5847167Abstract: 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: GrantFiled: June 30, 1997Date of Patent: December 8, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: Raymond W. Kosley, Jr., Robert Joseph Cherill, Gerard O'Malley