Polycyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/461)
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Patent number: 8173802Abstract: Provided is a method for producing a piperidin-4-one derivative useful as an intermediate for agricultural chemicals or pharmaceutical products. A piperidin-4-one derivative represented by formula (III-a) or formula (III-b) is produced by reacting a cyclic bis(aminol)ether compound represented by formula (I) and an acetone derivative represented by formula (II) in the presence of at least one substance selected from the group consisting of protonic acids, Lewis acids, acid halides and dialkyl sulfuric acids.Type: GrantFiled: October 10, 2007Date of Patent: May 8, 2012Assignee: Nippon Soda Co., Ltd.Inventors: Hirohito Oooka, Yasushi Shibata, Hiroki Inoue, Tsutomu Imagawa
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Publication number: 20120039848Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: August 11, 2011Publication date: February 16, 2012Inventors: Yao-Ling Qiu, Xiaowen Peng, Ce Wang, Yat Sun Or
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Publication number: 20120041190Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective Factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: February 10, 2011Publication date: February 16, 2012Inventors: James R. Corte, Tianan Fang, Carl P. Decicco, Donald J.P. Pinto, Karen A. Rossi, Zilun Hu, Yoon Jeon, Mimi L. Quan, Joanne M. Smallheer, Yufeng Wang, Wu Yang
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Publication number: 20120022011Abstract: The invention provides purified 19-substituted geldanamycin derivatives, pharmaceutically acceptable salts thereof and prodrugs thereof that are potent Hsp90 binding agents that are useful for the treatment and/or the amelioration of symptoms of cancer and other proliferative tissue disorders.Type: ApplicationFiled: August 22, 2008Publication date: January 26, 2012Applicant: The Regents of the University of ColoradoInventors: David Ross, David Siegel, Wenchang Guo, Christopher J. Moody, Christopher S.P. McErlean
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Publication number: 20110319362Abstract: Inhibitors of STAT3 are disclosed. Methods of using the STAT3 inhibitors in the treatment of diseases and conditions wherein inhibition of STAT3 provides a benefit, like cancers, also are disclosed.Type: ApplicationFiled: December 7, 2009Publication date: December 29, 2011Inventors: Shaomeng Wang, Jianyong Chen, Cindy Gomez, Longchuan Bai, Zaneta Nikolovska-Coleska, Yu-Jun Zhao
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Publication number: 20110281845Abstract: The present disclosure relates to XIAP inhibitor compounds of the formula I.Type: ApplicationFiled: June 15, 2011Publication date: November 17, 2011Applicant: NOVARTIS AGInventors: Zhuoliang CHEN, Mark G. PALERMO, Sushil K. SHARMA, Troy SMITH, Christopher S. STRAUB, Run-Ming D. WANG, Yaping WANG, Leigh ZAWEL
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Publication number: 20110268722Abstract: Described are mitochondria-targeted anti-tumor agents, death receptor agonists, autophagy inhibitors, and NF-?B signaling pathway inhibitors, and methods of making and using the same for the treatment of disorders associated with unwanted cell proliferation.Type: ApplicationFiled: April 22, 2011Publication date: November 3, 2011Inventors: Markus D. Siegelin, Dario C. Altieri
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Publication number: 20110262449Abstract: 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: July 1, 2011Publication date: October 27, 2011Applicant: TOPOTARGET SWITZERLAND SAInventors: Virginie PETRILLI, Fabio Martinon, Jurg Tschopp, Thibault De Smedt
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Patent number: 8039455Abstract: The invention relates to novel macrocyclic compounds of the formula in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: GrantFiled: December 28, 2006Date of Patent: October 18, 2011Assignee: Novartis AGInventors: Claudia Betschart, Manuel Koller, Kurt Laumen, Andreas Lerchner, Rainer Machauer, Clive McCarthy, Marina Tintelnot-Blomley, Siem Jacob Veenstra
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Patent number: 8034806Abstract: In one aspect, the invention relates to bicyclic MGluR5 positive allosteric modulators, for example 6-(phenylethynyl)-3,4-dihydroisoquinolin-1(2H)-one, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with glutamate dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: October 31, 2008Date of Patent: October 11, 2011Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Charles David Weaver, Alice L. Rodriguez, Colleen M. Niswender, Carrie K. Jones, Richard Williams
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Patent number: 8030307Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.Type: GrantFiled: November 26, 2008Date of Patent: October 4, 2011Assignee: Enanta Pharmaceuticals, Inc.Inventors: Joel D. Moore, Yat Sun Or, Zhe Wang
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Publication number: 20110207147Abstract: Provided are modified cycloalkyne compounds; and methods of use of such compounds in modifying biomolecules. Embodiments include a cycloaddition reaction that can be carried out under physiological conditions. The cycloaddition reaction involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo and in vitro.Type: ApplicationFiled: February 10, 2011Publication date: August 25, 2011Inventors: JOHN C. JEWETT, Carolyn Ruth Bertozzi, Ellen May Sletten, Chelsea Gloria Gordon
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Publication number: 20110183986Abstract: Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.Type: ApplicationFiled: April 1, 2011Publication date: July 28, 2011Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Dane Goff, Jiaxin Yu, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak, Jing Zhang
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Publication number: 20110160175Abstract: The present invention relates to macbecin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pre-treatment for cancer. The present invention also provides methods for the production of these compounds involving incorporation of non-natural starter units and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies.Type: ApplicationFiled: November 9, 2007Publication date: June 30, 2011Inventors: Christine Martin, Ming Zhang, Nigel Coates, William Vousden, Steven Moss, Sabine Gaisser
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Publication number: 20110091452Abstract: The present invention relates to 4,5-dihydromacbecin analogues to the formula (IA) or (IB), or a pharmaceutically acceptable salt there of: wherein: R1 represents H or CONH2 that are useful, e.g. in the treatment of cancer, B-cell malignancies malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies.Type: ApplicationFiled: March 30, 2007Publication date: April 21, 2011Inventors: Christine Martin, Ming Zhang, Sabine Gaisser, Nigel Coates, Barrie Wilkinson
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Publication number: 20110052528Abstract: Embodiments of this invention provide novel peptidomimetics that contain a macrocycle. Such compounds are neuroprotective and have utility as therapeutic agents for treatment of diseases, injuries and other conditions characterised by neuronal degeneration and/or death. Compounds are also useful for manufacture of medicaments useful for treatment of such conditions.Type: ApplicationFiled: December 14, 2007Publication date: March 3, 2011Applicant: Neuren Pharmaceuticals LimitedInventors: Paul William Richard Harris, Margaret Anne Brimble
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Publication number: 20110046189Abstract: The invention relates to heteroaryl-substituted bicyclic 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: April 13, 2009Publication date: February 24, 2011Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Haiying Sun, Zaneta Nikolovska-Coleska
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Publication number: 20110034686Abstract: The present invention is successful in providing a suitable process for the isolation and purification of geldanamycin. The process provided in the instant invention is easy to scale-up, industrially safe and will give high yield and productivity.Type: ApplicationFiled: June 6, 2008Publication date: February 10, 2011Inventors: Nitin Sopanrao Patil, Rakesh Bhaiyyaram Mendhe, Anantrao Phatale Amit, Prakash Khedkar Anand
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Publication number: 20110028450Abstract: The invention relates to ring-annulated dihydropyrrolo[2,1-a]isoquinoline compounds according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: ApplicationFiled: July 27, 2010Publication date: February 3, 2011Applicant: N.V. OrganonInventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen, Herman Thijs Stock
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Publication number: 20110021481Abstract: The present invention relates to ansamycin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases or a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine.Type: ApplicationFiled: November 9, 2007Publication date: January 27, 2011Inventor: Christine Martin
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Patent number: 7855192Abstract: 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: GrantFiled: January 23, 2008Date of Patent: December 21, 2010Assignee: Kosan Biosciences, Inc.Inventors: Gary W. Ashley, Hugo Menzella, Janice Lau Wee, John R. Carney
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Publication number: 20100311694Abstract: A set of geldanamycin derivatives and their preparation methods. Pharmaceutical compositions comprising the said compounds as an active ingredient which are used as antivirus and antitumor agents. The said derivatives are used in the manufacture of heat shock protein 90 (Hsp 90) inhibiting agents which have the utility as antivirus and antitumor agents.Type: ApplicationFiled: January 19, 2009Publication date: December 9, 2010Applicant: Institute of Medicinal Biotechnology, Chinese Academy of Medical SciencesInventors: Zhuorong Li, Zonggen Peng, Yanping Li, Jianhua Zhu, Peizhen Tao, Bo Fan, Yuping Wang, Guangzhi Shan, Shuqin Wang, Tian Zhang, Jiandong Jiang
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Publication number: 20100279995Abstract: There are provided inter alia derivatives of a benzenoid ansamycin which contain a 1,4-dihydroxyphenyl moiety bearing at position 6 an amino carboxy substituent, in which position 2 and the carboxy substituent at position 6 are connected by an aliphatic chain of varying length characterised in that one or both of the 1-hydroxy and the 4-hydroxy position(s) of the phenyl ring are independently derivatised by an aminoalkyleneaminocarbonyl group, which alkylene group, which may optionally be substituted by alkyl groups, has a chain length of 2 or 3 carbons and which derivatising group(s) increase the water solubility and/or the bioavailability of the parent molecule but which are capable of being removed in-vivo. Such compounds are described for the treatment of cancer or B-cell malignancies.Type: ApplicationFiled: September 1, 2006Publication date: November 4, 2010Inventors: Alexander R. Guiblin, Barrie Wilkinson, Steven J. Moss, Ming-Qiang Zhang, Alison D. McElhinney, Christine J. Martin
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Patent number: 7816346Abstract: Analogs of geldanamycin (an ansamycin), pharmaceutical formulations comprising such analogs, and methods of use (e.g., treating tumors).Type: GrantFiled: November 15, 2007Date of Patent: October 19, 2010Assignee: Abraxis BioScience, LLCInventors: Chunlin Tao, Hongna Han, Xiaowen Sun, Neil Desai, Patrick Soon-Shiong
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Publication number: 20100210597Abstract: According to the invention there are provided derivatives of a C21-deoxy ansamycin or salt thereof which contain a 1-hydroxyphenyl moiety bearing at position 3 an aminocarboxy substituent, in which position 5 and the aminocarboxy substituent at position 3 are connected by an aliphatic chain of varying length characterised in that the 1-hydroxy position of the phenyl ring is derivatised by an aminoalkyleneaminocarbonyl group, which alkylene group (which may optionally be substituted by alkyl groups) has a chain length of 2 or 3 carbon atoms, a phosphoric acid, or a phosphoric acid ester (such as an alkyl ester) group, or a salt thereof, and which derivatising group increases the water solubility and/or the bioavailability of the parent molecule. Such compounds are useful in therapy eg in the treatment of cancer and B-cell malignancies.Type: ApplicationFiled: March 3, 2008Publication date: August 19, 2010Inventors: Steven Moss, Christine Martin, Ming Zhang
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Patent number: 7776849Abstract: 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: GrantFiled: June 29, 2006Date of Patent: August 17, 2010Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Shinpei Yamaguchi, Takayuki Nakashima, Yutaka Kanda
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Patent number: 7700587Abstract: Haloperidol analogs that conforms to the structural formulae: wherein: R is H, or —(CH2)n—OH, n is an integer from 0 to 2, and A is a heterocyclic bridging group, consisting essentially of carbon and at least one nitrogen atom, which effectively maintains the distance between the moieties connected thereby such that the compound (1) is incapable of metabolizing to BCPP+ like species, (2) has an affinity for the D2 receptor subtype of 15<D2<250 and (3) functions as a dopamine receptor antagonist, or the structural formulae: wherein: R1 is H, or —(CH2)n—OH, n is an integer from 0 to 2, B is an aza- or diaza-bicyclo group, which effectively maintains the distance between the moieties connected thereby such that the compound is incapable of metabolizing to BCPP+ like species; and Z is —CH— or N; and pharmaceutically acceptable salts, esters, derivatives, metal complexes, conjugates and prodrugs thereof.Type: GrantFiled: September 7, 2004Date of Patent: April 20, 2010Assignee: Florida A&M UniversityInventors: Seth Y. Ablordeppey, Donald M. N. Sikazwe
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Patent number: 7696192Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R5c, m and n are defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: September 6, 2005Date of Patent: April 13, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Steven N. Gallicchio, Craig A. Stump, Cory R. Theberge, Joseph P. Vacca, C. Blair Zartman, Xufang Zhang
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Publication number: 20100068203Abstract: The present invention relates to 17-oxymacbecin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies.Type: ApplicationFiled: May 9, 2007Publication date: March 18, 2010Inventors: Christine Martin, Ming Zhang, Sabine Gaisser, Nigel Coates
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Patent number: 7662809Abstract: The present invention relates to tetracyclic indole compounds of formula (I); wherein R1, R2, R14, R15, A, Ar, Y and Z are defined herein, and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising them, and their use for the treatment or prevention of infection by hepatitis C virus.Type: GrantFiled: October 25, 2005Date of Patent: February 16, 2010Assignee: Istituto di Richerche di Biologia Molecolare P Angeletti SpAInventors: Caterina Ercolani, Joerg Habermann, Frank Narjes, Simona Ponzi, Michael Rowley, Ian Stansfield
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Publication number: 20090298804Abstract: The present invention relates to 15-desmethoxymacbecin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies.Type: ApplicationFiled: March 30, 2007Publication date: December 3, 2009Inventors: Sabine Gaisser, Christine Martin, Ming Zhang, Barrie Wilkinson, Nigel Coates, Mohammed Nur-E-Alam, Nikolaos Galtatzis
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Publication number: 20090291941Abstract: The present invention relates to pyrido[3,2-c]benzazocinone derivatives and related compounds, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: ApplicationFiled: October 18, 2006Publication date: November 26, 2009Inventors: Christopher J. Dinsmore, Jongwon Lim, Alan B. Northrup
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Publication number: 20090291996Abstract: The present invention provides Caspofungin and salts thereof substantially free of Caspofungin C0 and salts thereof. The present invention also provides processes for the preparation of said Caspofungin and salts thereof and processes for the determination of the amount of Caspofungin C0 and salts thereof present in Caspofungin and salts thereof. The present invention further provides pharmaceutical compositions comprising said Caspofungin and salts thereof.Type: ApplicationFiled: May 21, 2009Publication date: November 26, 2009Inventors: Ferenc Korodi, Piroska Kovacs, Andrea Csorvasi, Gabor Nagy
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Publication number: 20090285773Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: ApplicationFiled: May 13, 2009Publication date: November 19, 2009Inventors: Li-Qiang Sun, Paul Michael Scola
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Patent number: 7608613Abstract: 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: August 27, 2008Date of Patent: October 27, 2009Assignee: 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: 20090253653Abstract: 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: October 8, 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: 20090253667Abstract: The present invention relates to 18,21-didesoxymacbecin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pre-treatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies.Type: ApplicationFiled: May 9, 2007Publication date: October 8, 2009Inventors: Christine Martin, Ming Zhang, Nigel Coates, William Vousden, Steven Moss, Sabine Gaisser
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Publication number: 20090209494Abstract: The present invention relates to 21-deoxymacbecin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and or prophylaxis of cancer or B-cell malignancies.Type: ApplicationFiled: December 22, 2006Publication date: August 20, 2009Inventors: Christine Janet Martin, Barrie Wilkinson, Sabine Gaisser, Ming-Oiang Zhang, Rose Mary Sheridan, Lesley Sarah Sheehan, Rachel Edith Lill, Mohammed Nur-E-Alam, William Alexander Vousden
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Publication number: 20090209507Abstract: The present invention relates to 15-O-desmethylmacbecin analogues according to the formula (IA) or (IB) herein, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 either both represent H or together they represent a bond (i.e. C4 to C5 is a double bond); and R3 represents H or CONH2 that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies.Type: ApplicationFiled: March 30, 2007Publication date: August 20, 2009Inventors: Sabine Gaisser, Christine Martin, Ming Zhang, Barrie Wilkinson, Nigel Coates, Mohammed Nur-E-Alam, William Vousden
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Publication number: 20090180984Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.Type: ApplicationFiled: December 12, 2008Publication date: July 16, 2009Inventors: Ying Sun, Yonghua Gai, Yat Sun Or, Zhe Wang
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Publication number: 20090180983Abstract: The present invention relates to compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising a compound of the present invention.Type: ApplicationFiled: November 26, 2008Publication date: July 16, 2009Inventors: Joel D. Moore, Yat Sun Or, Zhe Wang
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Publication number: 20090170878Abstract: The invention relates to novel macrocyclic compounds of the formula in which all of the variables are as defined in the specification, in free base form or in acid addition salt form, to their preparation, to their use as medicaments and to medicaments comprising them.Type: ApplicationFiled: July 19, 2007Publication date: July 2, 2009Inventor: Rainer Machauer
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Publication number: 20090123480Abstract: The invention relates to bivalent 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: November 13, 2008Publication date: May 14, 2009Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Shaomeng Wang, Haiying Sun, Dongguang Qin, Zaneta Nikolovska-Coleska, Jianfeng Lu, Su Qiu, Yuefeng Peng, Qian Cai
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Publication number: 20090117127Abstract: The present invention relates to 11-O-desmethylmacbecin analogues that are useful, e.g. in the treatment of cancer, B-cell malignancies, malaria, fungal infection, diseases of the central nervous system and neurodegenerative diseases, diseases dependent on angiogenesis, autoimmune diseases and/or as a prophylactic pretreatment for cancer. The present invention also provides methods for the production of these compounds and their use in medicine, in particular in the treatment and/or prophylaxis of cancer or B-cell malignancies.Type: ApplicationFiled: March 30, 2007Publication date: May 7, 2009Inventors: Sabine Gaisser, Christine Martin, Ming Zhang, Barrie Wilkinson, Lesley Sheehan, Nigel Coates, Mohammed Nur-E-Alam, William Vousden, Nikolaos Gaitatzis
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Publication number: 20090111816Abstract: Polycyclic aryl and polycyclic heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl catalytic activity are also disclosed.Type: ApplicationFiled: December 29, 2007Publication date: April 30, 2009Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Dane Goff, Jiaxin Yu, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Joane Litvak, Jing Zhang
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Publication number: 20090105471Abstract: The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.Type: ApplicationFiled: December 22, 2008Publication date: April 23, 2009Inventors: Lawrence M. Blatt, Steven W. Andrews, Kevin R. Condroski, George A. Doherty, Yutong Jiang, John A. Josey, April L. Kennedy, Machender R. Madduru, Peter J. Stengel, Steven M. Wenglowsky, Benjamin T. Woodard, Laura Woodard
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Publication number: 20090099080Abstract: Described are mitochondria-targeted anti-tumor agents, and methods of making and using the same for the treatment of disorders associated with unwanted cell proliferation.Type: ApplicationFiled: September 10, 2008Publication date: April 16, 2009Inventors: Dario C. Altieri, Byoung Heon Kang
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Publication number: 20090088414Abstract: 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: April 2, 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: 20090069281Abstract: 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: August 20, 2008Publication date: March 12, 2009Inventors: 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: 20090062528Abstract: 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: August 20, 2008Publication date: March 5, 2009Inventors: Brian C. Austad, Louis Grenier, Edward B. Holson, John J. Lee, Roger H. Pak, James R. Porter, James L. Wright