Tetracyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 548/420)
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Patent number: 7745473Abstract: There is provided a novel pyrrole-imidazole polyamide compound for alkylating the specific base sequence of DNA, the polyamide compound being capable of being synthesized through fewer reaction steps than known hybrid molecules and having a combination of a high reactivity in DNA alkylation and the ability to recognize a sequence. Furthermore, there is provided an alkylating agent and a molecule serving as a drug, the alkylating agent and the molecule containing the polyamide compound.Type: GrantFiled: March 10, 2005Date of Patent: June 29, 2010Assignee: Kyoto UniversityInventors: Hiroshi Sugiyama, Toshikazu Bando
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Publication number: 20100144821Abstract: The invention is directed to compounds and methods for treating protein folder disorders. In certain embodiments the invention provides compounds and methods for treating neurodegenerative diseases such as Alzheimer's disease, tauopathy, cerebral amyloid angiopathy, Lewy body disease, dementia, Huntington's disease and prion-based spongiform encelopathy. The invention further provides compounds, methods and pharmaceutical compositions for inhibiting tau protein, A? protein or ?-synuclein protein aggregation.Type: ApplicationFiled: November 19, 2007Publication date: June 10, 2010Applicant: Queen's University at KingstonInventors: Michael D. Carter, Donald F. Weaver, Sheila Marie H. Jacobo, Erhu Lu, Fuye Gao
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Publication number: 20100136491Abstract: Compounds of formula (I), (II), and (III), wherein R1, R2, R?2 and R??2 for example are C1-C20alkyl, provided that at least one of R1, R2, R?2 and R??2 carries a specified substituent; R3, R4, and R5 for example independently of one another are hydrogen or a defined substituent provided that at least one of R3, R4 or R5 is other than hydrogen or C1-C20alkyl; R6, R7, R8, R?7, RV, R?8, R?6, R?7, R??6 and R??7 for example independently of one another have one of the meanings as given for R3, R4, and R5; and R9 for example is C1-C20alkyl; exhibit an unexpectedly good performance in photopolymerization reactions.Type: ApplicationFiled: April 24, 2008Publication date: June 3, 2010Inventors: Akira Matsumoto, Junichi Tanabe, Hisatoshi Kura, Masaki Ohwa
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Patent number: 7696239Abstract: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.Type: GrantFiled: January 3, 2008Date of Patent: April 13, 2010Assignee: Janssen Pharmaceutica NVInventors: Zhihua Sui, Xuqing Zhang, Xiaojie Li
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Publication number: 20100019663Abstract: Provided is a fused aromatic compound suitable for an organic layer of an organic light emitting emitting diode (OLED).Type: ApplicationFiled: June 8, 2009Publication date: January 28, 2010Inventors: Dong-woo SHIN, Byoung-ki CHOI, Myeong-suk KIM, Tae-yong NOH, O-hyun KWON, Tae-woo LEE, Yu-jin KIM
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Publication number: 20090302752Abstract: The present invention relates to compounds of the formula (1) and to the use thereof in organic electroluminescent devices, in particular as matrix material in phosphorescent devices.Type: ApplicationFiled: December 10, 2007Publication date: December 10, 2009Applicant: Merck Patent GmbHInventors: Amir Hossain Parham, Jonas Kroeber, Arne Buesing, Horst Vestweber
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Publication number: 20090143457Abstract: Described herein are various compounds for treatment of ocular neurodegenerative diseases, including but not limited to glaucoma and diabetic retinopathy. The compounds described herein can act to attenuate and/or block calcium release from external neuronal environments as well as intracellular stores.Type: ApplicationFiled: December 4, 2008Publication date: June 4, 2009Applicant: NORTHEASTERN OHIO UNIVERSITIES COLLEGE OF MEDICINEInventors: Cornelis J. Van der Schyf, Randolph B. Schiffer, Paula Grammas, Masao Roy Wilson, Werner J. Geldenhuys, Lois-May Bezuidenhout
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Publication number: 20090075996Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly diseases or disorders that involve thrombocytopenia.Type: ApplicationFiled: July 14, 2006Publication date: March 19, 2009Applicant: Irm LLCInventors: Phillip B. Alper, Thomas Marsilje, Arnab Chatterjee, Wenshuo Lu, Daniel Mutnick, Michael Roberts, Yun He
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Publication number: 20090069220Abstract: A conjugate of formula: V—(Y)a-Z-T??(I), T-X—B—(Y)a-Z-T???(II), V—(Y)a-Z-(Y?)a—V???(III), T-X—B—(Y)a-Z-(Y?)a—X?—B?-T???(IV), V—(Y)a-Z-(Y?)a—X—B-T??(V), V—(Y)a-Z-X—B-Z?-(Y?)a—(V?)b??(VI), or (W)a—(Y)b-[(Z)c-(Y?)d—(X—B)e—(Y?)f-(Z?)g]h-(Y??)i—(W?)j??(VII), in which W and W? are independently a DNA intercalator or terminal subunit, V and V? are independently a DNA intercalator, X and X? are independently a DNA alkylator, B and B? are the same or different and each is a heteroaromatic residue that is attached to the N-terminus of an alkylator subunit (X or X?), Y, Y?, Y? and Y?? are independently a linker, T and T? are independently terminal subunits, Z and Z? are independently a polyamide group that binds to the minor groove of DNA, a, b, c, d, f, g, i, and j are independently 0 to 5, and e and h are independently 1 to 5, a composition comprising a conjugate of any of formulae (I)-(VII) and a carrier, and a method for treating cancer in a mammal comprising administering an effective amount ofType: ApplicationFiled: September 16, 2008Publication date: March 12, 2009Applicant: GOVERNMENT OF THE UNITED STATES OF AMERICA, REPRESENTED BY THE SECRETARY, DEPAInventors: Zoltan Szekely, Humcha Krishnamurthy Hariprakasha, Marek W. Cholody, Christopher Michejda
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Publication number: 20080267981Abstract: Methods for treating a neoplastic disease with an antibody-cytotoxin conjugate molecule, methods of synthesizing an antibody-cytotoxin conjugate molecule are provided. Compounds that are useful as antibody-cytotoxin conjugate molecule or useful in the synthesis of these molecules are also provided.Type: ApplicationFiled: June 29, 2005Publication date: October 30, 2008Applicant: The Scripps Research InstituteInventors: Kim D. Janda, Peter Wirsching, Dale L. Boger
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Patent number: 7420065Abstract: Provided are novel hetero-polycyclic compounds having a specific structure, color-changing material compositions comprising (A) a fluorescent coloring matter comprising at least one of the hetero-polycyclic compounds described above and (B) a binder material, color-changing films comprising the above hetero-polycyclic compounds, coloring matters comprising the above hetero-polycyclic compounds, and pigments or dyes comprising the hetero-polycyclic compounds described above, and provided are color-changing material compositions which are not deteriorated in a color-changing performance even after used for long time and which are prevented from being unusable due to deposition of coloring matters during storage and color-changing films produced by using the same, and novel hetero-polycyclic compounds, coloring matters and pigments or dyes which actualize them.Type: GrantFiled: February 12, 2004Date of Patent: September 2, 2008Assignees: Idemitsu Kosan Co., Ltd., Techno Network Shikoku Co., Ltd.Inventors: Katsuhira Yoshida, Yousuke Ooyama, Satoshi Hachiya
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Patent number: 7408072Abstract: The present invention provides heteropolycyclic compounds represented by General Formulae (1) and (2): wherein R1 is a straight- or branched-chain C1-C10 alkyl group or the like; R2 and R3 are the same or different and are each a straight- or branched-chain C1-C10 alkyl group or the like; R4 and R5 are each a hydrogen atom; X is —OH or the like; X? is a straight- or branched-chain C1-C10 alkyl group or the like; and Z is —O— or the like. The heteropolycyclic compounds of the present invention have appropriate optical absorption wavelengths and fluorescence wavelengths and a high luminescence intensity, and can be advantageously used in various applications as colorants that have excellent performance in terms of heat resistance, light resistance, solubility, dispersibility in resist materials, solid luminescence, etc.Type: GrantFiled: February 10, 2005Date of Patent: August 5, 2008Assignee: Kochi UniversityInventors: Katsuhira Yoshida, Yousuke Ooyama
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Patent number: 7388024Abstract: The present invention provides indeno[2,1a]indene and isoindolo[2,1-a]indole derivatives of the Formula I, its salts and its stereoisomers, wherein X, R1, R2, R3, R4, R6, R7, R8, R9, R11, R12, R13 and R14 are as described in the specification. The invention also provides a method to prepare the compound of formula I, pharmaceutical composition containing such compounds, and method to manufacture a medicament. These compounds are useful in the treatment of various CNS disorders, hematological disorders, eating disorders, diseases associated with pain, respiratory diseases, genito-urological disorders, cardio vascular diseases and cancer.Type: GrantFiled: June 29, 2006Date of Patent: June 17, 2008Assignee: Suven Life Sciences LimitedInventors: Jasti Venkateswarlu, Satya Nirogi Ramakrishna Venkata, Sastri Kambhampati Rama, Shreekrishna Shirsath Vikas, Kandikere Vishwottam Nagaraj
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Publication number: 20080122344Abstract: Provided are an organic light emitting compound represented by Formula 1 below, an organic light emitting device comprising the same, and a method of manufacturing the light emitting device: wherein CY1, CY2, Ar1, R1 and R2 are described in the detailed description of the invention. An organic light emitting device comprising the organic light emitting compound has low turn-on voltage, high efficiency, high color purity and high luminance.Type: ApplicationFiled: May 31, 2007Publication date: May 29, 2008Applicant: SAMSUNG ELECTRONICS CO., LTD.Inventors: Dong-woo SHIN, Eun-sil HAN, Woon-jung PAEK, Yi-yeol LYU, O-hyun KWON, Myeong-suk KIM, Byoung-ki CHOI, Jhun-mo SON, Young-mok SON
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Publication number: 20080124455Abstract: Provided are an organic light emitting compound represented by Formula 1 below, an organic light emitting device comprising the same, and a method of manufacturing the organic light emitting device: where CY1 and CY2 are each independently a fused C6-C50 aromatic ring, Ar1 is a substituted or unsubstituted C6-C50 arylene group, Ar2, Ar3, Ar4, and Ar5 are each independently a substituted or unsubstituted C6-C50 aryl group, m and n are independently 0-3, and R1 and R2 are substituent groups. An organic light emitting device comprising the organic light emitting compound has low turn-on voltage, high efficiency, high color purity and high luminance.Type: ApplicationFiled: June 22, 2007Publication date: May 29, 2008Applicant: SAMSUNG ELECTRONICS CO., LTD.Inventors: Dong-woo SHIN, Eun-sil HAN, Woon-jung PAEK, Yi-yeol LYU, O-hyun KWON, Myeong-suk KIM, Byoung-ki CHOI, Jhun-mo SON, Young-mok SON
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Patent number: 7354947Abstract: Isaothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof having the general formula: and pharmaceutically acceptable salts thereof, wherein R0 is —CH2—, —SO—, —O—, —SO2—, or —S—; compositions comprising the iazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof; and methods for treating or preventing a disorder alleviated by inhibiting Jun N-terminal kinase (JNK) by administering the isaothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof are described herein.Type: GrantFiled: June 22, 2005Date of Patent: April 8, 2008Assignee: Signal Pharmaceuticals, LLCInventors: Steven T. Sakata, Heather K. Raymon
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Patent number: 7348425Abstract: Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: GrantFiled: February 3, 2006Date of Patent: March 25, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Xiaofan Zheng, Feng He, Min Ding, Carl P. Bergstrom, Piyasena Hewawasam, Scott W. Martin, Robert G. Gentles
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Patent number: 7317035Abstract: The present invention relates to novel tetracyclic arylcarbonyl indoles, their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel tetracyclic arylcarbonyl indoles of the general formula (I), their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them.Type: GrantFiled: June 19, 2003Date of Patent: January 8, 2008Assignee: Suven Life Sciences LimitedInventors: Venkateswarlu Jasti, Venkata Satya Nirogi Ramakrishna, Rama Sastri Kambhampati, Srinivasa Reddy Battula, Venkata Satya Veerabhadra Vadlamudi Rao
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Patent number: 7309532Abstract: The present invention is related to a cyclopentaphenanthrene-based compound and an organic electroluminescence device using the same. In particular, the cyclopentaphenanthrene-based compound offers several advantages, including easy processibility, high solubility, superior color purity, color stability and thermal stability. Moreover, the cyclopentaphenanthrene-based compound may be used not only as a material for forming an organic layer of an organic electroluminescence device, particularly, a light-emitting layer, but also as a material of an organic pigment or nonlinear optical substance.Type: GrantFiled: October 1, 2004Date of Patent: December 18, 2007Assignee: Samsung SDI Co., Ltd.Inventors: Kyu-Sik Kim, Byung-Hee Sohn, Lyong-Sun Pu, Jhun-Mo Son, Sang-Hoon Park, Ji-Hoon Lee, Woon-Jung Paek
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Patent number: 7297711Abstract: The present invention relates to novel tetracyclic arylalkyl indoles, their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel tetracyclic arylalkyl of the general formula (I), their derivatives, their analogues, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates, novel intermediates described herein and pharmaceutically acceptable compositions containing them. This invention also relates to process/es for preparing such compound/s of general formula (I), composition/s containing effective amount/s of such a compound and the use of such a compound/composition in therapy.Type: GrantFiled: June 19, 2003Date of Patent: November 20, 2007Assignee: Suven Life Sciences LimitedInventors: Venkateswarlu Jasti, Venkata Satya Nirogi Ramakrishna, Rama Sastri Kambhampati, Srinivasa Reddy Battula, Venkata Satya Veerabhadra Vadlamudi Rao
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Patent number: 7253292Abstract: A process for preparing cyclopentadiene derivatives comprising the steps of: a) coupling a five membered heterocycle ring with a five or six membered heterocycle ring; b) reacting the obtained compound with a carbonilating system: c) reducing the obtained compound.Type: GrantFiled: May 8, 2002Date of Patent: August 7, 2007Assignee: Basell Polyolefine GmbHInventors: Ilya E. Nifant'ev, Igor A Kashulin, Pavel V. Ivchenko, Peter A. A. Klusener, Frans M. Kornorffer, Kees P. De Kloe, Jos J. H. Rijsemus
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Patent number: 7153848Abstract: Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.Type: GrantFiled: July 14, 2005Date of Patent: December 26, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Xiaofan Zheng, Feng He, Min Ding, Carl P. Bergstrom, Piyasena Hewawasam, Scott W. Martin, Robert G. Gentles
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Patent number: 7122679Abstract: The present invention is directed to novel multicyclic molecules that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of PARP, VEGFR2, and MLK3 enzymes, including, for example, neurodegenerative diseases, inflammation, ischemia, and cancer.Type: GrantFiled: May 8, 2001Date of Patent: October 17, 2006Assignee: Cephalon, Inc.Inventors: Mark A. Ator, Ron Bihovsky, Sankar Chatterjee, Derek Dunn, Robert L. Hudkins
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Patent number: 7094798Abstract: This invention relates to pyrrolocarbazole derivatives according formula I wherein R1, R2, R7, R8, R9, X and Y are as defined in the specification wherein said derivatives specifically inhibit one or both of the checkpoint kinases Wee1 and Chk1Type: GrantFiled: April 25, 2003Date of Patent: August 22, 2006Assignee: Pfizer IncInventors: Richard John Booth, Ellen Myra Dobrusin, Alan Kraker, Lorna Helen Mitchell, William Alexander Denny, Jeffrey Bruce Smaill, Andrew Mark Thompson, Florence Oliver Joseph McCarthy, Ho Huat Lee, Brian Desmond Palmer
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Patent number: 6992100Abstract: A novel class of tetracyclic compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.Type: GrantFiled: December 6, 2001Date of Patent: January 31, 2006Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Michael Dean Kinnick, Ho-Shen Lin, John Michael Morin, Jr., Michael Enrico Richett, Daniel Jon Sall, Jason Scott Sawyer, John David Jandzinski
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Patent number: 6872743Abstract: A novel class of tetracyclic compounds represented by the formula I wherein R1, R2, R3, R4, R5, R6, R7, A, B, C, D, E, and n are as defined is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.Type: GrantFiled: December 6, 2001Date of Patent: March 29, 2005Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Michael Dean Kinnick, Ho-Shen Lin, John Michael Morin, Jr., Michael Enrico Richett, Daniel Jon Sall, Jason Scott Sawyer
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Patent number: 6844445Abstract: Compound of formula (I): wherein: R represents hydrogen or a group selected from alkenyl and optionally substituted alkyl, each of R1 to R8, which may be identical or different, represents hydrogen or a group selected from alkyl, alkenyl, hydroxy, alkoxy, alkenyloxy, arylalkyl, arylalkoxy, carboxy, acyloxy and arylcarbonyloxy, or one of R1 to R8 forms with an adjacent one R1 to R8 an alkylenedioxy group, its optical isomers when they exist, and addition salts thereof with a pharmaceutically acceptable acid or base, with the proviso that: when R does not represent hydrogen, then at least one of R1 to R8 represents hydroxy or acyloxy, and the compounds of formula (I) are other than indeno[1,2-b]indol-10(5H)-one and medicinal products containing the same which are useful for treatment of disorders of the melatoninergic system.Type: GrantFiled: March 19, 2002Date of Patent: January 18, 2005Assignee: Les Laboratoires ServierInventors: Michel Wierzbicki, Marie-Françoise Boussard, Anne Rousseau, Jean Albert Boutin, Philippe Delagrange
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Publication number: 20040265628Abstract: The invention provides organic compounds of the general structure (1) 1Type: ApplicationFiled: April 16, 2004Publication date: December 30, 2004Inventors: Suning Wang, Ruiyao Wang
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Publication number: 20040092543Abstract: A novel class of tetracyclic compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.Type: ApplicationFiled: June 16, 2003Publication date: May 13, 2004Inventors: Douglas Wade Beight, Michael Dean Kinnick, Ho-Shen Lin, John Michael Morin Jr, Michael Enrico Richett, Daniel Jon Sall, Jason Scott Sawyer, John David Jandzinski
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Publication number: 20040063941Abstract: A novel class of tetracyclic compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shockType: ApplicationFiled: June 16, 2003Publication date: April 1, 2004Inventors: Douglas Wade Beight, Michael Dean Kinnick, Ho-Shen Lin, John Michael Morin, Michael Enrico Richett, Daniel Jon Sall, Jason Scott Sawyer
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Publication number: 20030208076Abstract: A method for the preparation of a compound of general Formula: 1Type: ApplicationFiled: December 4, 2002Publication date: November 6, 2003Inventors: Martin Gerhardt Banwell, Bernard Luke Flynn
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Publication number: 20030186077Abstract: Compounds according to Formula I 1Type: ApplicationFiled: December 31, 2001Publication date: October 2, 2003Inventor: Jian P. Chen
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Patent number: 6627650Abstract: A compound of formula (I): wherein: R represents hydrogen, optionally substituted alkyl or alkenyl, R1 to R8, which may be identical or different, each represents hydrogen, optionally substituted alkyl, hydroxy, acyloxy, optionally substituted amino, carboxy, optionally substituted alkoxy, or alkenyloxy, or one of R1 to R8 forms, with another of R1 to R8 that is adjacent, an alkylenedioxy group, X represents oxygen or NR16 wherein R16 represents hydrogen, alkyl, aryl or arylalkyl, R9 represents hydrogen, aryl, heteroaryl, or optionally substituted, saturated or unsaturated alkyl, an isomer thereof, or an addition salt thereof with a pharmaceutically acceptable acid or base. Medicinal products containing the same which are useful as anti-cancer agents.Type: GrantFiled: June 13, 2002Date of Patent: September 30, 2003Assignee: Les Laboratoires ServierInventors: Michel Wierzbicki, Marie-Françoise Boussard, Anne Rousseau, Ghanem Atassi, John Hickman, Alain Pierre, Stéphane Leonce, Nicolas Guilbaut, Laurence Kraus-Berthier
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Publication number: 20030176454Abstract: A compound of the formula (I): wherein A is a hydrogen atom, an optionally substituted, unsaturated, N-containing heterocyclic group or a group of the formula (a): wherein R is an optionally substituted aryl group or an optionally substituted heterocyclic group; M is —(CH2)n-, —(CH2)n-O—(CH2)m-or —(CH2)n-NH—(CH2)m-, wherein n and m are independently 0, 1 or 2; Q is an optionally substituted cycloalkylene group, an optionally substituted arylene group or an optionally substituted divalent heterocyclic group; and the moiety of the formula (b): is an optionally substituted, unsaturated, mono-, di-, tri- or tetra-cyclic, N-containing heterocyclic group which may contain additional hetero atom(s) selected from the group consisting of nitrogen, oxygen and sulfur atoms as the ring member(s), its prodrug or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: November 1, 2002Publication date: September 18, 2003Inventors: Akira Yamada, Glen Spears, Hisashi Hayashida, Masaki Tomishima, Kiyotaka Ito, Masashi Imanishi
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Publication number: 20030125369Abstract: Compound of formula (I): 1Type: ApplicationFiled: June 13, 2002Publication date: July 3, 2003Inventors: Michel Wierzbicki, Marie-Francoise Boussard, Anne Rousseau, Ghanem Atassi, John Hickman, Alain Pierre, Stephane Leonce, Nicolas Guilbaud, Laurence Kraus-Berthier
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Patent number: 6576780Abstract: The current invention discloses hydroxyamidino derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: October 13, 2000Date of Patent: June 10, 2003Assignee: GD Searle & CompanyInventors: Rolando E. Gapud, Timothy J. Hagen, E. Ann Hallinan, Donald W. Hansen, Jr., Barnett S. Pitzele, Suzanne S. Metz, R. Keith Webber, Foe S. Tjoeng, Robert E. Manning, Mihaly V. Toth
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Publication number: 20030073732Abstract: Isothiazoloanthrones, isooxazoloanthrones, isoindolanthrones, and derivatives thereof having the general formula: 1Type: ApplicationFiled: February 7, 2002Publication date: April 17, 2003Applicant: Signal Pharmaceuticals, Inc.Inventors: Steven T. Sakata, Heather K. Raymon
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Patent number: 6548530Abstract: Analogs of the antitumor antibiotics CC-1065 and the duocarmycins incorporate the 1,2,9,9a-tetrahydrocyclopropa[c]benz[e]indol-4-one (CBI) alkylation subunit. The CBI-based analogs have potent cytotoxic activity and are useful as efficacious antitumor compounds. A direct relationship between functional stability and in vitro cytotoxic potency is disclosed. The CBI-based analogs are easily synthesized and are 4× more stable and 4× more potent than the corresponding analogs containing the authentic CPI alkylation subunit of CC-1065 and comparable in potency to agents containing the authentic alkylation subunit of duocarmycin SA. Similarly, the CBI-based agents alkylate DNA with an unaltered sequence selectivity at an enhanced rate and with a greater efficiency than the corresponding CPI analog and were comparable to the corresponding analog incorporating the duocarmycin SA alkylation subunit.Type: GrantFiled: October 2, 1998Date of Patent: April 15, 2003Assignee: The Scripps Research InstituteInventor: Dale L. Boger
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Publication number: 20030022930Abstract: This invention provides compounds of the formula: 1Type: ApplicationFiled: June 27, 2002Publication date: January 30, 2003Applicant: WyethInventors: Gary Paul Stack, John Dunlop, Alexander Alexei Greenfield, Jonathan Laird Gross
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Patent number: 6486326Abstract: A series of bioactive analogs of (+)-CC-1065 (1) and the duocarmycins 2 and 3 are synthesized. The bioactive analogs include either iso-CI or iso-CBI (6 and 7) as a DNA alkylation subunit. Conjugated to the DNA alkylating subunits are a variety of DNA binding subunits. The bioactive analogs maintain their DNA selectivity and display enhance reactivity.Type: GrantFiled: July 17, 2001Date of Patent: November 26, 2002Assignee: The Scripps Research InstituteInventor: Dale L. Boger
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Publication number: 20020173531Abstract: Compound of formula (I): 1Type: ApplicationFiled: March 19, 2002Publication date: November 21, 2002Inventors: Michel Wierzbicki, Marie-Francoise Boussard, Anne Rousseau, Jean Albert Boutin, Philippe Delagrange
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Patent number: 6482567Abstract: New photoacid generator compounds (“PAGs”) are provided and photoresist compositions that comprise such compounds. In particular, non-ionic PAGs are provided that contain an oxime sulfonate group, and/or an N-oxyimidosulfonate group. PAGs of the invention are particularly useful as photoactive components of photoresists imaged at short wavelengths such as 248 nm, 193 nm and 157 nm.Type: GrantFiled: August 25, 2000Date of Patent: November 19, 2002Assignee: Shipley Company, L.L.C.Inventors: James F. Cameron, Gerhard Pohlers
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Patent number: 6465660Abstract: Compound of formula (I): wherein: R1, R2, R3, R4, R5, R6 and R8, which may be identical or different, each represents hydrogen, alkyl, arylalkyl, hydroxy, alkoxy, arylalkoxy, acyloxy, arylcarbonyloxy, carboxyalkyl or carboxy, R7 represents hydrogen, hydroxy, alkoxy, arylalkoxy, acyloxy or arylcarbonyloxy group, or one of R1 to R8, together with another of R1 to R8 adjacent to it, forms an alkylenedioxy, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid or base.Type: GrantFiled: February 26, 2002Date of Patent: October 15, 2002Assignee: Les Laboratoires ServierInventors: Michel Wierzbicki, Marie-Françoise Boussard, Anne Rousseau, Jean Albert Boutin, Philippe Delagrange
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Patent number: 6440889Abstract: An amine-elimination process for making single-site catalysts is disclosed. First, an indenoindole or its synthetic equivalent reacts with a tetrakis(dialkylamino) Group 4 metal compound to give a tris(dialkyl-amino) compound. This versatile intermediate can be halogenated, alkylated, or reacted directly with cyclopentadienyl precursors to provide valuable indenoindolyl-Group 4 metal complexes. The process selectively provides mono-indenoindolyl complexes. In addition, it enables the economical preparation of desirable Cp- or Cp-like derivatives and allows the use of an inexpensive Group 4 transition metal source.Type: GrantFiled: August 15, 2001Date of Patent: August 27, 2002Assignee: Equistar Chemicals, LPInventor: Barbara M. Tsuie
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Publication number: 20020049335Abstract: A series of bioactive analogs of (+)-CC-1065 (1) and the duocarmycins 2 and 3 are synthesized. The bioactive analogs include either iso-CI or iso-CBI (6 and 7) as a DNA alkylation subunit. Conjugated to the DNA alkylating subunits are a variety of DNA binding subunits. The bioactive analogs maintain their DNA selectivity and display enhance reactivity.Type: ApplicationFiled: July 17, 2001Publication date: April 25, 2002Applicant: The Scripps Research InstituteInventor: Dale L. Boger
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Patent number: 6326391Abstract: The present invention relates generally to the fields of bacteriology and mycology. More particularly, the present invention provides novel inhibitors of multidrug transport proteins that may be used in combination with existing antibacterial agent and/or antifungal agents to increase the toxic effects of the antimicrobial agents. More specifically the present invention provides methods and compositions for enhancing the antibacterial action of fluoroquinolones by administering fluoroquinolones in combination with an inhibitor of multidrug transporters and of enhancing the antifungal action of azole antifungal agents by administering an azole antifungal agent in combination with an inhibitor of multidrug transporters. Compositions comprising indole, urea, quinoline or aromatic amide based inhibitors also are disclosed.Type: GrantFiled: December 2, 1999Date of Patent: December 4, 2001Assignee: Influx, Inc.Inventors: Penelope N. Markham, Debbie C. Mulhearn, Alexander A. Neyfakh, David Crich, Mohamad-Rami Jaber, Michael E. Johnson
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Patent number: 6281355Abstract: A nitrogen-containing tetracyclic compound represented by the formula: wherein Y1—Y2—Y3 is N—C═N or a group represented by the formula: C═C—NR3 (wherein R3 is a hydrogen atom, a C1-5 alkyl group or a nitrogen-containing C2-10 alkyl group), Y4 is S, SO, SO2, CH2 or a group represented by the formula: NR4 (wherein R4 is a C1-5 alkanoyl group or a C1-5 alkyl group), R1 and R2 are the same or different, and are each a hydrogen atom, a C1-10 alkyl group, a C3-15 alkoxyalkyl group or a C3-15 alkylaminoalkyl group, or R1 and R2 taken together with the nitrogen atom to which they are attached form a cyclic amino group, X1 and X2 are the same or different, and are each a hydrogen atom, a C1-5 alkyl group, a C1-5 alkoxy group or a halogen atom, and n is 0, 1 or 2; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 1, 2000Date of Patent: August 28, 2001Assignees: Taisho Pharmaceutical Co., Ltd., Nihon Nohyaku Co., Ltd.Inventors: Atsuro Nakazato, Taketoshi Okubo, Toshihito Kumagai, Shigeyuki Chaki, Kazuyuki Tomisawa, Masashi Nagamine, Makoto Gotoh, Kuniaki Kondoh, Masanori Yoshida
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Patent number: 6262271Abstract: A series of bioactive analogs of (+)-CC-1065 (1) and the duocarmycins 2 and 3 are synthesized. The bioactive analogs include either iso-CI or iso-CBI (6 and 7) as a DNA alkylation subunit. Conjugated to the DNA alkylating subunits are a variety of DNA binding subunits. The bioactive analogs maintain their DNA selectivity and display enhanced reactivity.Type: GrantFiled: April 12, 2000Date of Patent: July 17, 2001Assignee: The Scripps Research InstituteInventor: Dale L. Boger
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Patent number: 6147105Abstract: Novel 2-phenyl indoles are disclosed of general formula (I), wherein: R.sup.1 represents one of the rests --(CH.sub.2).sub.n --S(O).sub.m --R.sup.4, --(CH.sub.2).sub.n --NR.sup.6 --SO.sub.2 --R.sup.4, (a), and n' being integers between 4 and 12 and m and m' are 0, 1 or 2; X represents a methylene group, an imino group .dbd.NR.sup.6, or an oxygen or sulphur atom; R.sup.2 and R.sup.3 independently of one another represent a hydrogen atom, a C.sub.1 -C.sub.10 alkyl group, a benzyl, alkanoyl or alkanoyloxy, or carbarnoyl rest of formula --C(O)R.sup.5 or --C(O)NR.sup.6 R.sup.7 or a tetrahydropyranyl group; R.sup.4 represents a hydrogen atom, a C.sub.1 -C.sub.10 alkyl, a completely or partially fluorinated alkyl group --(CH.sub.2).sub.o --(CF.sub.2).sub.p CF.sub.3, o and p being independently of one another integers between 0 and 6, an (alkyl)amino or (alkyl)carbamoyl group of formula (CH.sub.2).sub.q --Y--NR.sup.8 R.sup.Type: GrantFiled: May 14, 1997Date of Patent: November 14, 2000Assignee: Schering AktiengesellschaftInventors: Erwin Von Angerer, Christian Biberger, Martin Schneider
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Patent number: 6069153Abstract: The present invention relates to new substituted benzo[a]carbozoles and indenoindoles which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, having the general structures below.Type: GrantFiled: May 6, 1999Date of Patent: May 30, 2000Assignee: American Home Products CorporationInventors: Chris P. Miller, Michael D. Collini, Bach D. Tran