Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/461)
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Publication number: 20090062250Abstract: The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting 17-ammonium hydroquinone ansamycin analog.Type: ApplicationFiled: August 27, 2008Publication date: March 5, 2009Inventors: Julian Adams, Yun Gao, Asimina T. Georges Evangelinos, Louis Grenier, Roger H. Pak, James R. Porter, James L. Wright
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Publication number: 20090048253Abstract: The present invention provides a benzenoid ansamycin derivative represented by Formula (I) (wherein R1 and R2 each represent a hydrogen atom or are combined together to form a bond, R8 represents a bond or an oxygen atom, R11 represents hydroxy, substituted or unsubstituted lower alkoxy or substituted or unsubstituted lower alkanoyloxy, R15 represents a hydrogen atom or methoxy, R22 represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkanoyl or substituted or unsubstituted aroyl, R4 and R5 each represent a hydrogen atom or are combined together to form a bond, R18 represents a hydrogen atom, or the like, R21 represents hydroxy or the like, and R17 and R19 may be the same or different and each represents a hydrogen atom, or the like) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 29, 2006Publication date: February 19, 2009Applicant: Kyowa Hakko Kogyo Co., Ltd.Inventors: Shinpei Yamaguchi, Takayuki Nakashima, Yutaka Kanda
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Publication number: 20090042847Abstract: Polymorphs and pharmaceutical formulations of 17-allylamino-17-demethoxy-geldanamycin (17-AAG).Type: ApplicationFiled: May 29, 2008Publication date: February 12, 2009Applicant: Kosan Biosciences IncorporatedInventors: Peter J. Licari, Timothy Leaf, Ruchir P. Desai, Jorge L. Galazzo, Greg O. Buchanan, Stephen William Watt, Alexander Redvers Eberlin, Robert Arslanian
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Publication number: 20090022704Abstract: The present invention relates to a new method, and the process to manufacture a medicament, for treating gout or pseudogout, comprising administering an effective amount of inhibitors blocking IL-1 or its maturation by the NALP3 inflammasome.Type: ApplicationFiled: January 8, 2007Publication date: January 22, 2009Applicant: APOXIS SAInventors: Virginie Petrilli, Fabio Martinon, Jurg Tschopp, Thibault De Smedt
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Publication number: 20080312317Abstract: There provided a 12-membered-ring macrolactam derivative having antitumor activity: A compound represented by Formula (1) or a salt thereof. In this Formula, R1 is a hydrogen atom, a C1-6 alkyl group, a C1-6 alkylcarbonyl group or a C6-14 arylcarbonyl group; R2 is a hydrogen atom or a C1-6 alkyl group; R3 is a hydrogen atom or a hydroxyl group; R4 is a hydrogen atom or a hydroxyl group; R5 is a hydrogen atom or a C1-6 alkyl group; R6 is a hydrogen atom or a hydroxyl group; and R7 is an acetyl group or the like.Type: ApplicationFiled: April 10, 2008Publication date: December 18, 2008Applicant: Eisai R&D Management Co., Ltd.Inventors: Masayuki Miyano, Daisuke Ito, Norio Murai
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Publication number: 20080275018Abstract: The invention relates to antibacterial amide-macrocycles of formula (I), in which R26 represents hydrogen, halogen, amino or methyl, R7 represents a group of formula (II), (III), (IV) or (V), whereby R1 represents hydrogen or hydroxy and * is the linkage site to the carbon atom, R2 represents hydrogen or methyl and methods for their production, their use for the treatment and/or prophylaxis of diseases as well as their use for the production of medicaments for the treatment and/or prophylaxis of diseases, in particular of bacterial infections.Type: ApplicationFiled: September 28, 2007Publication date: November 6, 2008Applicant: AiCuris GmbH & Co. KGInventors: Rainer ENDERMANN, Kerstin EHLERT, Siegfried RADDATZ, Martin MICHELS, Yolanda CANCHO-GRANDE, Stefan WEIGAND, Karin FISCHER
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Publication number: 20080275039Abstract: The present invention relates to geldanamycin derivatives, benzoquinone ansamycin biosynthesized by gene manipulation of Streptomyces hygroscopicus subsp. duamyceticus and the method producing them, more particularly to a geldanamycin O-carbamoyl transferase gene(gel8)-inactive mutant, the method producing it and geldanamycin derivatives, 4,5-dihydro-7-O-descarbamoyl-7-hydroxy geldanamycin and 4,5-dihydro-7-O-descarbamoyl-7-hydroxy-17-O-demethyl geldanamycin. Since geldanamycin derivatives of the present invention suppress Hsp90 like geldanamycin, they can effectively be used for antibiotic, antifungal, antiviral, anti-inflammatory and antitumor agents and an immune suppressant.Type: ApplicationFiled: August 11, 2005Publication date: November 6, 2008Inventors: Jung Joon Lee, Young Soo Hong, Dongho Lee, Jeong-Hyung Lee, Kwang-Soo Sung
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Publication number: 20080249085Abstract: Ansamycin analogs, including maytansinoid analogs, and their use in treating cell proliferative diseases and conditions, and in particular, for use as antitumor agents.Type: ApplicationFiled: April 4, 2005Publication date: October 9, 2008Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: John M. Cassady, Heinz G. Floss
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Publication number: 20080234246Abstract: Analogs of geldanamycin (an ansamycin), pharmaceutical formulations comprising such analogs, and methods of use (e.g., treating tumors).Type: ApplicationFiled: November 15, 2007Publication date: September 25, 2008Applicant: Abraxis BioScience, Inc.Inventors: Chunlin Tao, Hongna Han, Xiaowen Sun, Neil Desai, Patrick Soon-Shiong
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Publication number: 20080221077Abstract: Provided herein, inter alia, are solid forms of geldanamycin analogs, pharmaceutical compositions comprising a geldanamycin analog and a crystallization inhibitor, methods of making and using such compositions. Additionally, provided are methods for the treatment of cancer, a neoplastic disease state and/or a hyperproliferative disorder, and methods of inhibiting Heat Shock Protein 90 (“Hsp90”).Type: ApplicationFiled: December 11, 2007Publication date: September 11, 2008Inventors: Brian C. Austad, Louis Grenier, Edward B. Holson, John J. Lee, Roger H. Pak, James R. Porter, James L. Wright
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Publication number: 20080206788Abstract: Immunoassay reagents, methods and test kits for the specific quantification of vancomycin in a test sample are disclosed. The reagent comprises antibodies prepared with immunogens of FIG. 6 wherein P is an immunogenic carrier material and X is a linking moiety. Also described is the synthesis of labeled reagents of FIG. 8 wherein Q is a detectable moiety, preferably fluorescein or a fluorescein derivative, and X is a linking moiety.Type: ApplicationFiled: October 9, 2007Publication date: August 28, 2008Inventors: Maciej Adamczyk, Elaine M. Brate, Mary M. Perkowitz, Sushil D. Rege
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Publication number: 20080188450Abstract: Macrolactams are made by feeding aromatic amino acids as replacement starter units to a mutant strain of the geldanamycin-producing microorganism Streptomyces hygroscopicus var. geldanus NRRL 3602, wherein the gene cluster encoding enzymes for the biosynthesis of the natural starter unit 3-amino-5-hydroxybenzoic acid has been deleted.Type: ApplicationFiled: January 23, 2008Publication date: August 7, 2008Inventors: Gary W. Ashley, Hugo Menzella, Janice Lau Wee, John R. Carney
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Publication number: 20080171865Abstract: The present invention discloses a method for targeting maytansinoids to a selected cell population, the method comprising contacting a cell population or tissue suspected of containing the selected cell population with a cell-binding agent maytansinoid conjugate, wherein one or more maytansinoids is covalently linked to the cell-binding agent via a non-cleavable linker and the cell-binding agent binds to cells of the selected cell population.Type: ApplicationFiled: October 29, 2007Publication date: July 17, 2008Applicant: IMMUNOGEN, INC.Inventors: Rita Steeves, Robert Lutz, Ravi Chari, Hongsheng Xie, Yelena Kovtun
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Publication number: 20080132485Abstract: The invention relates to conformationally constrained mimetics of Smac which function as inhibitors of Inhibitor of Apoptosis Proteins. The invention also relates to the use of these mimetics for inducing apoptotic cell death and for sensitizing cells to inducers of apoptosis.Type: ApplicationFiled: July 11, 2005Publication date: June 5, 2008Inventors: Shaomeng Wang, Haiying Sun, Zaneta Nikolovksa-Coleska, Chao-Yie Yang, Liang Xu, Naoyuki G. Saito, Jianyong Chen
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Patent number: 7378407Abstract: Geldanamycin compounds having a structure according to formula I where Q1, L, L1, R5, R6, and R11 are as defined herein, are useful for treating a disease or disorder ameliorated by inhibiting the function of extracellular heat shock protein-90.Type: GrantFiled: July 6, 2007Date of Patent: May 27, 2008Assignee: Kosan Biosciences IncorporatedInventors: Daniel V. Santi, Zong-Qiang Tian, Yaoquan Liu, Zhan Wang
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Patent number: 7375217Abstract: The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting 17-ammonium hydroquinone ansamycin analog.Type: GrantFiled: April 14, 2005Date of Patent: May 20, 2008Assignee: Infinity Pharmaceuticals, Inc.Inventors: Julian Adams, Yun Gao, Asimina T. Georges Evangelinos, Louis Grenier, Roger H. Pak, James R. Porter, James L. Wright
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Publication number: 20080108694Abstract: The present invention relates to compounds having the structure (and pharmaceutically acceptable derivatives thereof) wherein Ro-R4, Z, X, A-B, D-E, G-J, and K-L are as defined herein, the synthesis thereof and the use of these compounds as therapeutic agents.Type: ApplicationFiled: December 17, 2004Publication date: May 8, 2008Inventors: Samuel J Danishefsky, Zhi-Qiang Yang, Xudong Geng, Ting-Chao Chou, Neal Rosen
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Patent number: 7361647Abstract: The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting 17-ammonium hydroquinone ansamycin analog.Type: GrantFiled: April 14, 2005Date of Patent: April 22, 2008Assignee: Infinity Pharmaceuticals, Inc.Inventors: Julian Adams, Yun Gao, Asimina T. Georges Evangelinos, Louis Grenier, Roger H. Pak, James R. Porter, James L. Wright
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Patent number: 7329746Abstract: The present invention is directed to compounds of formula I which are inhibitors of the beta-secretase enzyme and that are useful in the treatment or prevention of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease.Type: GrantFiled: August 10, 2004Date of Patent: February 12, 2008Assignee: Merck & Co., Inc.Inventors: Craig A. Coburn, Shawn J. Stachel, Joseph P. Vacca
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Patent number: 7282493Abstract: The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting 17-ammonium hydroquinone ansamycin analog.Type: GrantFiled: December 23, 2004Date of Patent: October 16, 2007Assignee: Infinity Pharmaceuticals, Inc.Inventors: Julian Adams, Yun Gao, Asimina T. Georges Evangelinos, Louis Grenier, Roger H. Pak, James R. Porter, James L. Wright
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Patent number: 7279573Abstract: Compounds of structural Formula (I) where A is a lipophilic group including an aliphatic bridging group, B is a lipophilic group, D is a group having at least one amino or substituted amino group and R is hydrogen, alkyl or cycloalkyl, and pharmaceutically acceptable salts and individual isomers thereof, which have growth hormone releasing activity in humans or animalsType: GrantFiled: February 23, 2006Date of Patent: October 9, 2007Assignees: Kaken Pharmaceutical Co., Ltd., Molecular Research InstituteInventors: Hidenori Funamizu, Nobuo Ishiyama, Satoru Ikegami, Tadashi Okuno, Kiyoshi Inoguchi, Ping Huang, Gilda Loew
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Patent number: 7271160Abstract: Bifunctional molecules comprising two hsp-binding moieties which bind to hsp90 in the pocket to which ansamycin antibiotics bind connected via a linker are effective for inducing the degradation and/or inhibition of HER-family tyrosine kinases. For example, a compound of two geldanamycin moities joined by a four-carbon linker provides selective degradation of HER-family tyrosine kinases, without substantially affecting other kinases. These compounds can be used for treatment of HER-positive cancers with reduced toxicity, since these compounds potently kill cancer cells but affect fewer proteins than geldanamycin.Type: GrantFiled: September 21, 2001Date of Patent: September 18, 2007Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Neal Rosen, Scott D. Kuduk, Samuel J. Danishefsky, Furzhong F. Zheng, Laura Sepp-Lorenzino, Ouatek Ouerfelli
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Patent number: 7259156Abstract: Geldanamycin compounds having a structure according to formula I where Q1, L, L1, R5, R6, and R11 are as defined herein, are useful for treating a disease or disorder ameliorated by inhibiting the function of extracellular heat shock protein-90.Type: GrantFiled: May 17, 2005Date of Patent: August 21, 2007Assignee: Kosan Biosciences IncorporatedInventors: Daniel V. Santi, Zong-Qiang Tian, Yaoquan Liu, Zhan Wang
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Patent number: 7241754Abstract: 2-Desmethyl ansamycins having a structure according to formula I, where R1, R2, R3, R4, R5 and R6 are as defined herein, and other 2-desmethyl ansamycins are useful as antiproliferative agentsType: GrantFiled: June 14, 2004Date of Patent: July 10, 2007Assignee: Kosan Biosciences, Inc.Inventors: Zong-Qiang Tian, Robert McDaniel, David C. Myles, Kedar Gautam Patel, Misty Piagentini, Zhan Wang
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Patent number: 7238682Abstract: Bifunctional molecules comprising two hsp-binding moieties which bind to hsp90 in the pocket to which ansamycin antibiotics bind connected via a linker are effective for inducing the degradation and/or inhibition of HER-family tyrosine kinases. For example, a compound of two geldanamycin moities joined by a four-carbon linker provides selective degradation of HER-family tyrosine kinases, without substantially affecting other kinases. These compounds can be used for treatment of HER-positive cancers with reduced toxicity, since these compounds potently kill cancer cells but affect fewer proteins than geldanamycin.Type: GrantFiled: April 7, 2000Date of Patent: July 3, 2007Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Neal Rosen, Scott D. Kuduk, Samuel J. Danishefsky, Furzhong F. Zheng, Laura Sepp-Lorenzino, Ouatek Ouerfelli
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Patent number: 7211572Abstract: The present invention relates to a nitrogen-containing fused ring compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof, and an anti-HIV agent containing such compound. The compound of the present invention has an HIV integrase inhibitory activity, and is useful as an agent for the prophylaxis or treatment of AIDS, or as an anti-HIV agent. In addition, by the combined use with other anti-HIV agents such as a protease inhibitor, a reverse transcriptase inhibitor and the like, it can be a more effective anti-HIV agent. Because it shows integrase-specific high inhibitory activity, the compound can be a pharmaceutical agent safe on human body, which causes only a fewer side effects.Type: GrantFiled: October 13, 2005Date of Patent: May 1, 2007Assignee: Japan Tobacco Inc.Inventors: Susumu Miyazaki, Susumu Katoh, Kaoru Adachi, Hirotaka Isoshima, Satoru Kobayashi, Yuji Matsuzaki, Wataru Watanabe, Kazunobu Yamataka, Shinichi Kiyonari, Shuichi Wamaki
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Patent number: 7176235Abstract: This invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3, R4, R5, W, X, Y, and Ar are as defined herein. Compounds of formula (I) are useful in the treatment of diseases or conditions characterized by cellular hyperproliferation. This invention also relates to means for the preparation of compounds of formula (I); formulations containing compounds of formula (I); and methods for the use of said compounds and formulations in the treatment of a disease or condition characterized by cellular hyperproliferation, including cancer.Type: GrantFiled: May 12, 2004Date of Patent: February 13, 2007Assignee: Kosan Biosciences, Inc.Inventors: Gary Ashley, John R. Carney, Brian Metcalf
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Patent number: 7166720Abstract: Hydroxy-imino derivatives of formula IIb are disclosed, in which R and R1 have the meanings given in the description.Type: GrantFiled: September 22, 2005Date of Patent: January 23, 2007Assignee: Merck Patent GesellschaftInventors: Thorsten Hartig, Steffen Enke
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Patent number: 7138395Abstract: The present invention relates to novel compounds, compositions comprising said compounds, and uses thereof, said compounds having the formula: X is —CH2—, —O— or —NR9—; R is a carbocyclic or heterocyclic ring; R1 is a cysteine trap; R2a, R2a?, R2b, and R2b? are each independently hydrogen, C1–C4 alkyl, C1–C4 alkoxy, and mixtures thereof; or R2a? and R2b? can taken together to form a double bond; R9 is hydrogen or a unit having the formula -L2-R10; L is the same as defined herein above; R10 is hydrogen; substituted or unsubstituted C1–C6 linear; branched, or cyclic hydrocarbyl; substituted or unsubstituted aryl; substituted or unsubstituted C1–C9 heterocyclic; and substituted or unsubstituted heteroaryl.Type: GrantFiled: June 9, 2003Date of Patent: November 21, 2006Assignee: The Procter & Gamble CompanyInventors: Steven Victor O'Neil, Michael Christopher Laufersweiler, Yili Wang, Kofi Abeka Oppong, David Lindsey Soper, John August Wos, Biswanath De, Thomas Prosser Demuth, Jr.
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Patent number: 7041696Abstract: The present invention relates to interleukin-1? converting enzyme inhibitors having the formula: R is a carbocyclic or heterocyclic ring; R1 is a cysteine trap; R2a, R2a?, R2b, and R2b? are each independently hydrogen, C1–C4 alkyl, C1–C4 alkoxy, and mixtures thereof; or R2a? and R2b? can taken together to form a double bond; L and L1 are linking groups having the formula: T is selected from the group consisting of: i) —NR6—; ii) —O—; iii) —NR6S(O)2—; iv) —S(O)2NR6—; and v) mixtures thereof; R6 is hydrogen, substituted or unsubstituted C1–C20 linear, branched, or cyclic alkyl, C6–C20 aryl, C7–C20 alkylenearyl, and mixtures thereof; the indices w, w1, and w2 are each independently 0 or 1; i) hydrogen; ii) C1–C4 linear, branched, and cyclic alkyl; iii) R3a and R3b or R4a, and R4b can be taken together to form a carbonyl unit; iv) two R3a or two R3b units from adjacent carbon atoms or two R4a or two R4b units from adjacent carbon atoms can be taken together to form a double bond; and v) mixtures thereof;Type: GrantFiled: June 9, 2003Date of Patent: May 9, 2006Assignee: The Procter & Gamble CompanyInventors: John August Wos, David Lindsey Soper, Steven Victor O'Neil, Yili Wang, Kofi Abeka Oppong, Michael Christopher Laufersweiler, Jian Chen, Biswanath De, Thomas Prosser Demuth, Jr.
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Patent number: 7038042Abstract: A process suitable for safely mass-producing, through a short step, cyclic compounds useful in medicines, agricultural chemicals, foods, cosmetics, and chemical products or as intermediates therefor. The process, which is for producing a compound represented by the formula: {wherein Z represents an electron-attracting group; W represents optionally substituted ethylene or optionally substituted vinylene; R3 represents hydrogen or an optionally substituted hydrocarbon group; and X represents a divalent group [provided that when W represents optionally substituted vinylene, then —X—CH2-Z is not —X1—X2—CH2, -Z (wherein X1 represents sulfur or optionally substituted nitrogen and X2 represents optionally substituted ethylene)]} or a salt thereof, is characterized by subjecting a compound represented by the formula (II) or a salt thereof: (wherein the symbols have the same meanings as the above) to a ring closure reaction in a solvent containing a carbonic diester.Type: GrantFiled: December 10, 2004Date of Patent: May 2, 2006Assignee: Takeda Pharmaceutical Company LimitedInventors: Tomomi Ikemoto, Tatsuya Ito, Kiminori Tomimatsu
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Patent number: 7026350Abstract: The present invention relates to water-soluble drugs, compositions containing same, and, in particular, a water-soluble analogue of geldanamycin. This invention also relates to a method of producing water-soluble analogues of water-insoluble drugs through derivatization and conjugation with a polar moiety via a thiol ether bond with a heterobifunctional linking molecule.Type: GrantFiled: May 3, 2004Date of Patent: April 11, 2006Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: David K. Ho, Raya Mandler, Ada Belinda Alvarado-Lindner, Kaye B. Dillah Upadhyay, David J. Newman
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Patent number: 6890917Abstract: A geldanamycin derivative exhibiting significant preliminary in vivo activity, particularly significant oral in vivo activity, and a method of treating or preventing cancer in a host comprising administering a geldanamycin derivative to a host in an amount sufficient to treat or prevent cancer.Type: GrantFiled: March 28, 2002Date of Patent: May 10, 2005Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth M. Snader, B. Rao Vishnuvajjala, Melinda G. Hollingshead, Edward A. Sausville
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Patent number: 6887993Abstract: Compounds having a structure according to formula I wherein the groups R1 and R4 are as defined in the specification, are useful as anti-proliferative agents.Type: GrantFiled: April 16, 2004Date of Patent: May 3, 2005Assignee: Kosan Biosciences, Inc.Inventors: Zong-Qiang Tian, Yaoquan Liu, David C. Myles, Zhan Wang
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Patent number: 6875863Abstract: Compounds having a structure according to formula I wherein the groups R1 and R4 are as defined in the specification, are useful as anti-proliferative agents.Type: GrantFiled: April 16, 2004Date of Patent: April 5, 2005Assignee: Kosan Biosciences, Inc.Inventors: Zong-Qiang Tian, Yaoquan Liu, David C. Myles, Zhan Wang
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Patent number: 6872715Abstract: The invention relates to benzoquinone ansamycin analogs useful for the treatment of cancer and other diseases or conditions characterized by undesired cellular proliferation or hyperproliferation. Therapies involving the administration of such benzoquinone ansamycin analogs, optionally in combination with an inhibitor of an HSP90 client protein, are useful to treat cancer and non-cancerous disease conditions.Type: GrantFiled: August 5, 2002Date of Patent: March 29, 2005Assignee: Kosan Biosciences, Inc.Inventors: Daniel Santi, David C. Myles, Zong-Qiang Tian, C. Richard Hutchinson, Robert Johnson, Yi-Qing Zhou, Li Feng
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Patent number: 6870049Abstract: Compounds having a structure according to formula I wherein the groups R1 and R4 are as defined in the specification, are useful as anti-proliferative agents.Type: GrantFiled: April 16, 2004Date of Patent: March 22, 2005Assignee: Kosan Biosciences, Inc.Inventors: Zong-Qiang Tian, Yaoquan Liu, David C. Myles, Zhan Wang
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Patent number: 6855705Abstract: Compounds having a structure according to formula I wherein the groups R1 and R4 are as defined in the specification, are useful as anti-proliferative agents.Type: GrantFiled: April 16, 2004Date of Patent: February 15, 2005Assignee: Kosan Biosciences, Inc.Inventors: Zong-Qiang Tian, Yaoquan Liu, David C. Myles, Zhan Wang
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Patent number: 6846814Abstract: Compounds having the general formula wherein R1a, R1b, R1c, R2, R3, R4, R5, R6, R7, R8, X1, X2, Y, Z and n are as defined in the specification, methods of using such compounds for the treatment of diseases and pharmaceutical composition comprising such compounds.Type: GrantFiled: April 5, 2001Date of Patent: January 25, 2005Assignee: Astra Zeneca ABInventors: Jeffrey Scott Albert, Peter Bernstein, Cyrus Ohnmacht, Jr., Keith Russell, Ashokkumar Bhikkappa Shenvi
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Patent number: 6759387Abstract: This invention provides compositions and methods for enhancing delivery of drugs and other agents across epithelial tissues, including the skin, gastrointestinal tract, pulmonary epithelium, and the like. The compositions and methods are also useful for delivery across endothelial tissues, including the blood brain barrier. The compositions and methods employ a delivery enhancing transporter that has sufficient guanidino or amidino sidechain moieties to enhance delivery of a compound conjugated to the reagent across one or more layers of the tissue, compared to the non-conjugated compound. The delivery-enhancing polymers include, for example, poly-arginine molecules that are preferably between about 6 and 25 residues in length (SEQ ID NO:50).Type: GrantFiled: July 30, 2002Date of Patent: July 6, 2004Assignee: Cellgate, Inc.Inventors: Jonathan B. Rothbard, Paul A. Wender, P. Leo McGrane, Lalitha V. S. Sista, Thorsten A. Kirschberg
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Patent number: 6747055Abstract: The present invention provides water-soluble drugs, in particular, water-soluble analogues of geldanamycin, and compositions comprising the same. This invention also provides a method of rendering water-soluble drugs soluble in water through derivatization with a bifunctional linking molecule and subsequent conjugation to a polar moiety through a thio ether. The present invention ether provides a method of treating cancer in a mammal.Type: GrantFiled: April 18, 2001Date of Patent: June 8, 2004Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: David K. Ho, Raya Mandler, Ada Belinda Alvarado-Lindner, Kaye B. Dillah Upadhyay, David J. Newman
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Publication number: 20040053909Abstract: A geldanamycin derivative exhibiting significant preliminary in vivo activity, particularly significant oral in vivo activity, and a method of treating or preventing cancer in a host comprising administrering a geldanamycin derivative to a host in an amount sufficient to treat or prevent cancer.Type: ApplicationFiled: September 16, 2003Publication date: March 18, 2004Inventors: Kenneth M. Snader, B. Rao Vishnuvajjala, Melinda G. Hollingshead, Edward A. Sausville
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Patent number: 6670348Abstract: Compounds having an ansamycin anitibiotic, or other moiety which binds to hsp90, coupled to a targeting moiety which binds specifically to a protein, receptor or marker can provide effective targeted delivery of the ansamycin antibiotic leading to the degradation of proteins and death of the targeted cells. These compositions may have different specificity than the ansamycin alone, allowing for a more specific targeting of the therapy, and can be effective in instances where the ansamycin alone has no effect. Thus, these compounds provide an entirely new class of targeted chemotherapy agents with application, depending on the nature of the targeting moiety, to treatment of a variety of different forms of cancer. Such agents can further be used to promote selective degradation of proteins associated with the pathogenesis of others diseases, including antigens associated with autoimmune disorders and pathogenic proteins associated with Alzheimer's disease.Type: GrantFiled: October 20, 1999Date of Patent: December 30, 2003Assignee: Sloan-Kettering Institute for Cancer ResearchInventors: Neal Rosen, Samuel Danishefsky, Ouathek Ouerfelli, Scott D. Kuduk, Laura Sepp-Lorenzino
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Publication number: 20030236296Abstract: The present invention relates to interleukin-1&bgr; converting enzyme inhibitors having the formula: 1Type: ApplicationFiled: June 9, 2003Publication date: December 25, 2003Applicant: The Procter & Gamble CompanyInventors: John August Wos, David Lindsey Soper, Steven Victor O'Neil, Yili Wang, Kofi Abeka Oppong, Michael Christopher Laufersweiler, Jian Chen, Biswanath De, Thomas Prosser Demuth
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Publication number: 20030087888Abstract: The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives, and intermediates therefor.Type: ApplicationFiled: May 14, 2002Publication date: May 8, 2003Inventors: Alicia Regueiro-Ren, Robert M. Borzilleri, Gregory D. Vite, Soong-Hoon Kim
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Patent number: 6534650Abstract: This invention relates to compounds of Formula V H—Y—G—R V and Formula VI (wherein f, X, Y, G and R have the values defined in the description) which are useful as intermediates for the preparation of compounds, or pharmaceutically acceptable salts thereof, which are useful as thrombin inhibitors, coagulation inhibitors and agents for the treatment of thromboembolic disorders.Type: GrantFiled: March 9, 2001Date of Patent: March 18, 2003Assignee: Eli Lilly and CompanyInventors: Valentine J Klimkowski, Aaron L Schacht, Michael R Wiley
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Publication number: 20030023082Abstract: The present invention relates to bicyclic compounds wherein one of the cyclic moieties is a 16-membered macrocycle and to methods for making and using these compounds.Type: ApplicationFiled: May 13, 2002Publication date: January 30, 2003Inventors: Gary Ashley, Brian Metcalf
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Publication number: 20030004338Abstract: The present invention relates to a process for the preparation of epothilone analogs by initially forming novel ring-opened epothilones and carrying out a macrolactamization reaction thereon. The subject process is amenable to being carried out in a single reaction vessel without isolation of the intermediate compound and provides at least about a three-fold increase in yield over prior processes for preparing the desired epothilone analogs.Type: ApplicationFiled: September 5, 2001Publication date: January 2, 2003Inventors: Wen Sen Li, John E. Thornton, Zhenrong Guo, Shankar Swaminathan
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Publication number: 20020193361Abstract: The present invention relates to 16-membered macrocyclic compounds.Type: ApplicationFiled: April 3, 2001Publication date: December 19, 2002Inventors: Gary Ashley, Brian Metcalf
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Patent number: 6489315Abstract: Novel compounds of the following general formula or salts thereof. wherein Ring M is a heterocyclic ring having —N═C<, —CO—N< or —CS—N< as the partial structure —X{overscore (— — — — — — — — —)} Y<; Ra and Rb are bonded to each other to form Ring A, or they are the same or different and represent, independently, a hydrogen atom or a substituent on the Ring M; Ring A and Ring B represent, independently, an optionally substituted homocyclic or heterocyclic ring, and at least one of them is optionally substituted heterocyclic ring; Rng C is optionally substituted homocyclic or heterocyclic ring; Rng Z is an optionally substituted ring; and n represents an integer of from 1 to 6, or a salt thereof, which has an excellent tachykinin receptor antagonistic effect, and their production, and pharmaceutical compositions.Type: GrantFiled: August 23, 2000Date of Patent: December 3, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Hideaki Natsugari, Takenori Ishimaru, Takayuki Doi, Yoshinori Ikeura, Chiharu Kimura