Two Of The Cyclos Share At Least Three Ring Members Or A Ring Member Is Shared By Three Of The Cyclos (e.g., Bridged, Peri-fused, Etc.) Patents (Class 540/456)
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Publication number: 20120046234Abstract: The invention provides compounds of formula I, II, and III as defined herein, as well as salts thereof. The compounds may have activity as anti-proliferative agents.Type: ApplicationFiled: August 1, 2008Publication date: February 23, 2012Inventors: Edmond J. LaVoie, Joseph E. Rice
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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: 20120027852Abstract: A pharmaceutical formulation includes a Limus family immunosuppressive macrolide on a pharmaceutically acceptable excipient, which may be compounded as suitable for oral administration.Type: ApplicationFiled: March 31, 2010Publication date: February 2, 2012Applicant: ETHYPHARMInventors: Frantz Deschamps, Catherine Herry, Jennifer Jung, Fabrice Leboeuf
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Publication number: 20120028908Abstract: A process for preparing a crystalline rapamycin analog includes: combining the rapamycin analog with an organic medium to form a mixture; incubating the mixture until the rapamycin analog crystallizes; and recovering the crystalline rapamycin analog. The organic medium can be a solvent, and the process can include causing the rapamycin analog to dissolve into the solvent, and incubating the solvent until the rapamycin analog crystallizes. The following can also be performed: forming a slurry of crystalline rapamycin analog; stirring the rapamycin analog mixture until the rapamycin analog crystallizes; saturating the rapamycin analog solution; forming a supersaturated rapamycin analog solution; combining an antisolvent with the rapamycin analog and the solvent to form a biphasic mixture, and incubating the biphasic mixture to cause a liquid-liquid phase split.Type: ApplicationFiled: October 1, 2011Publication date: February 2, 2012Applicant: Abbott LaboratoriesInventors: Shekhar VISWANATH, Larry Bartelt, Robert Leanna, Michael Rasmussen, Madhup Dhaon, Rodger Henry, Thomas Borchardt, Shuang Chen, Geoff Zhang
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Publication number: 20110294801Abstract: Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.Type: ApplicationFiled: September 3, 2009Publication date: December 1, 2011Applicant: MERCK PATENT GMBHInventors: Henry Yu, Lizbeth Celeste De Selm, Xuliang Jiang, Benny C. Askew, Jr., Srinivasa R. Karra, Andreas Goutopoulos
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Patent number: 8067429Abstract: The present invention relates to Rifaximin polymorphic, salt, hydrate, and amorphous forms, to their use in medicinal preparations and to therapeutic methods using them.Type: GrantFiled: February 25, 2009Date of Patent: November 29, 2011Assignee: Salix Pharmaceuticals, Ltd.Inventors: Karen S. Gushurst, Donglai Yang, Melanie Roe, Nathan Schultheiss, Petinka Vlahova, Jeffrey S. Stults, Travis L. Houston
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Patent number: 8058426Abstract: This invention concerns a new family of phosphorus-containing compounds containing a moiety JQA- in which: A is absent or is —O—, —S— or —NR2—; Q is absent or (if A is —O—, —S— or —NR2—) Q may be —V—, —OV—, —SV—, or —NR2V—, where V is an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, such that J is linked to the cyclohexyl ring directly, through A or through VA, OVA, SVA or NR2VA; K is O or S; each occurrence of Y is independently —O—, —S—, —NR2—, or a bond linking a R5 moiety to P; each occurrence of R2 and R5 is independently an aliphatic, heteroaliphatic, aryl, or heteroaryl moiety, or H; and each occurrence of R6 is independently —PK(YR5)(YR5), —SO2(YR5) or —C(O)(YR5); so long as any R2, or R5 moiety linked directly to P is not H; wherein two R2, R5 and/or R6 moieties may be chemically linked to one another to form a ring; each occurrence of G is independently —O—, —S—, —NR2— or (M)x; each occurrence of M is independently a substituted or unsubstituted methylene moiety, and any M-M? moiType: GrantFiled: April 6, 2010Date of Patent: November 15, 2011Assignee: ARIAD Pharmaceuticals, Inc.Inventors: David L. Berstein, Leonard W. Rozamus, Yihan Wang, Chester A. Metcalf, III
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Patent number: 8039600Abstract: Monoclonal antibodies to rapamycin and to 40-O-alkylated derivatives of rapamycin are provided, together with novel haptens, immunogenic conjugates, and processes for making them and assay kits for using them.Type: GrantFiled: August 20, 2001Date of Patent: October 18, 2011Assignee: Novartis AGInventors: Richard Sedrani, Valerie Q Ryffel
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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: 8039454Abstract: The invention is drawn to novel macrolide compounds of formula I having antibiotic and antineoplastic activities, useful as medicaments and/or agrochemicals for microorganism infections, in particularly for infectious diseases involving drug-resistant Staphylococcus, and for treatment of human and animal cancers.Type: GrantFiled: November 28, 2006Date of Patent: October 18, 2011Assignee: Weihe Pharma{grave over (c)}euticals Co. Ltd.Inventors: Genhui Chen, Bin Li, John M. Webster, Kaiji Hu, Jianxiong Li
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Publication number: 20110251231Abstract: A modified release composition comprising tacrolimus releases less than 20% w/w of the active ingredient within 0.5 hours when subjected to an in vitro dissolution test using USP Paddle method and using 0.1 N HCl as dissolution medium and has increased bioavailability by effectively reducing or even avoiding the effects of CYP3A4 metabolism. The modified composition may be coated with an enteric coating; and/or may comprise a solid dispersion or a solid solution of tacrolimus in a hydrophilic or water-miscible vehicle and one or more modifying release agents; and/or may comprise a solid dispersion or a solid solution of tacrolimus in an amphiphilic or hydrophobic vehicle and optionally one or more modifying release agents.Type: ApplicationFiled: June 23, 2011Publication date: October 13, 2011Applicant: LifeCycle Pharma A/SInventors: Per HOLM, Tomas NORLING
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Patent number: 8034926Abstract: A process for preparing a crystalline rapamycin analog includes: combining the rapamycin analog with an organic medium to form a mixture; incubating the mixture until the rapamycin analog crystallizes; and recovering the crystalline rapamycin analog. The organic medium can be a solvent, and the process can include causing the rapamycin analog to dissolve into the solvent, and incubating the solvent until the rapamycin analog crystallizes. The following can also be performed: forming a slurry of crystalline rapamycin analog; stirring the rapamycin analog mixture until the rapamycin analog crystallizes; saturating the rapamycin analog solution; forming a supersaturated rapamycin analog solution; combining an antisolvent with the rapamycin analog and the solvent to form a biphasic mixture, and incubating the biphasic mixture to cause a liquid-liquid phase split.Type: GrantFiled: September 20, 2010Date of Patent: October 11, 2011Assignee: Abbott LaboratoriesInventors: Shekhar Viswanath, Larry Bartelt, Robert Leanna, Michael Rasmussen, Madhup Dhaon, Rodger Henry, Thomas Borchardt, Shuang Chen, Geoff Zhang
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Patent number: 8030325Abstract: A polyketide synthase complex composed of polyketide synthase with 15 total modules, a non-ribosomal peptide synthetase with 1 module, and a cytochrome P450 hydroxylase is described. Also provided are novel Streptomyces species and methods of modified Streptomyces species. Further described are novel compounds, 36-ketomeridamycin, C9-deoxomeridamycin, and C9-deoxoprolylmeridamcyin and uses thereof.Type: GrantFiled: July 25, 2008Date of Patent: October 4, 2011Assignee: Wyeth LLCInventors: Min He, John Hucul, Bradley Arnold Haltli, Melissa M. Wagenaar, Edmund Idris Graziani, Mia Summers, Kerry Kulowski, Kevin Pong, Xidong Feng
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Publication number: 20110230531Abstract: The invention provides compounds of formula (I) wherein A, B, R1, F, G, n, n? and the dotted line have any values defined herein, as well as salts thereof. The compounds have activity as anti-proliferative agents.Type: ApplicationFiled: August 1, 2008Publication date: September 22, 2011Inventors: Edmond J. LaVoie, Joseph E. Rice, Satyanarayana Mavurapu
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Publication number: 20110184167Abstract: Novel intermediates, process for their preparation and their use in the preparation of therapeutically effective antineoplastic agents, in particular Temsirolimus of formula (I).Type: ApplicationFiled: January 28, 2011Publication date: July 28, 2011Applicant: Fresenius Kabi Oncology LimitedInventors: Nitin Gupta, Vishal Handa, Abir Kumar Pal, Hemant Kumar Singh, Saswata Lahiri, Sushil Kumar Dubey
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Publication number: 20110178130Abstract: The invention relates to compounds of the formula (I) which are inhibitors of activated thrombin-activable fibrinolysis inhibitor. The compounds of the formula I are suitable for producing medicaments for prophylaxis, secondary prevention and treatment of one or more disorders associated with thromboses, embolisms, hypercoagulability or fibrotic changes.Type: ApplicationFiled: May 22, 2009Publication date: July 21, 2011Applicant: SANOFI-AVENTISInventors: Christopher Kallus, Mark Broenstrup, Andreas Evers, Anja Globisch, Herman Schreuder, Michael Wagner
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Publication number: 20110172413Abstract: The present invention relates to a method for separating and purifying a lactone compound with an unsaturated alkyl group from a lactone compound with a saturated alkyl group which is an analog thereof. More specifically, the present invention relates to a method for effectively separating a lactone compound with an unsaturated alkyl group such as FK506 at high purity by extraction with a silver ion (Ag+) solution without use of column chromatography.Type: ApplicationFiled: March 18, 2011Publication date: July 14, 2011Applicant: GENOTECH CO., LTDInventors: Jae Jong Kim, Si Kyu Lim, Mi Ok Lee, Sang Myoun Lim, Bo-mi Lee, Dong Hwan Kim, Keum Soon Lee, Jeoung Hyun Ryu
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Publication number: 20110166172Abstract: Rapalogs of formula I, pharmaceutically acceptable salts, pharmaceutical compositions, and preparation methods and uses thereof. The rapalogs have the structure of formula I and can be used as an anti-tumor medicament. Comparing with rapamycin, the rapalogs of the present invention exhibit enhanced water solubility, and improved pharmacological and pharmacokinetic properties by introducing a hydrophilic and polar group such as a hydroxyl.Type: ApplicationFiled: September 17, 2009Publication date: July 7, 2011Applicant: Shanghai institute of Materia Medica, chinese Academy of SciencesInventors: Fajun Nan, Jian Ding, Jianping Zuo, Linqian Yu, Linghua Meng, Yangming Zhang, Na Yang, Min Gu
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Publication number: 20110165225Abstract: Drag derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drag derivatized with a weak-base moiety that facilitates active loading of the drag through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drag to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drag derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drags.Type: ApplicationFiled: May 26, 2009Publication date: July 7, 2011Inventors: Peter Cullis, Marcel Bally
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Publication number: 20110144176Abstract: This invention relates, in part, to macrolide compounds, actinomycete strains for producing them, and pharmaceutical compositions containing them.Type: ApplicationFiled: December 15, 2010Publication date: June 16, 2011Applicant: Wyeth LLCInventors: Mia Haruna Yoshino SUMMERS, Edmund Idris Graziani, Margaret M. Leighton, Kevin Pong, Roger Alan Kele, David P. Labeda
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Patent number: 7960405Abstract: A prodrug compound of a rapamycin analog and methods for inhibiting, treating, and preventing mammalian diseases.Type: GrantFiled: November 30, 2006Date of Patent: June 14, 2011Assignee: Abbott LaboratoriesInventors: Karl W. Mollison, Angela M. LeCaptain, Sandra E. Burke, Keith R. Cromack, Peter J. Tarcha, Yen-Chih J. Chen, John L. Toner
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Publication number: 20110123644Abstract: The instant invention describes macrocyclic compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders, and HDAC mediated disorders.Type: ApplicationFiled: April 10, 2009Publication date: May 26, 2011Applicant: University of Florida Research FoundationInventor: Hendrik Luesch
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Publication number: 20110123496Abstract: The present invention discloses compounds of formula Ia or Ib 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 the compounds of the present invention.Type: ApplicationFiled: October 19, 2010Publication date: May 26, 2011Inventors: Yonghua Gai, Yat Sun Or, Guoqiang Wang
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Publication number: 20110118323Abstract: The instant invention describes macrocyclic compounds having therapeutic activity, and methods of treating disorders such as cancer, tumors and cell proliferation related disorders, or affect cell differentiation, dedifferentiation or transdifferentiation.Type: ApplicationFiled: September 9, 2008Publication date: May 19, 2011Applicant: University of Florida Research Foundation, Inc.Inventors: Hendrik Luesch, Taori Kanchan, Valerie J. Paul
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Publication number: 20110118343Abstract: Antitumoral compounds of general formula I: wherein R1-R14 and the lines take permitted meanings for use in the treatment of cancer.Type: ApplicationFiled: July 2, 2009Publication date: May 19, 2011Applicant: Pharma Mar, S. A.Inventors: José Fernando Reyes Benítez, Gloria Crespo Sueiro, Rogelio Fernández Rodríguez, Andrés Francesch Solloso, María del Carmen Cuevas Marchante
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Publication number: 20110112090Abstract: A Compound of structure (IX) or (X) or a pharmaceutically acceptable salt thereof, wherein: X is —C(?O)N(R10)— or —CH(OPr3)—; R7, R9 and R10 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid; Pr1 and Pr2 are the same or different and represent hydrogen or a thiol protecting group; Pr3 is hydrogen or an alcohol protecting group; R1, R2, R5 and R6 are the same or different and represent hydrogen or an amino acid side chain moiety from either a natural or an unnatural amino acid, or R1 and R2 and/or R5 and R6, taken together with the carbon atom to which they are attached, form a spirocyclic moiety, with the proviso that: each of R1 and R2 is not hydrogen, or each of R5 and R6 is not hydrogen.Type: ApplicationFiled: May 22, 2009Publication date: May 12, 2011Inventors: Stephen Joseph Shuttleworth, Franck Alexandre Silva, Cyrille Davy Tomassi, Alexander Richard Liam Cecil, Thomas James Hill
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Publication number: 20110105473Abstract: Inhibitors of HCV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R1, R2, R4, R5, R6 and R7 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.Type: ApplicationFiled: July 8, 2009Publication date: May 5, 2011Applicant: TIBOTEC PHARMACEUTICALSInventors: Sandrine Marie Hélène Vendeville, Pierre Jean-Marie Bernard Raboisson, Tse-l Lin, Abdellah Tahri, Katie Ingrid Eduard Amssoms
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Publication number: 20110098241Abstract: Analogs and derivatives of rapamycin are provided, wherein the analogs and derivatives can bind to FK-506 binding protein (FKBP), or inhibit the mTOR function of an FKBP, or both. The analogs and derivatives are rapamycin include the rapamycin skeleton substituted at the 42-hydroxyl group with certain specified chemically feasible groups. Methods of using the rapamycin analogs and derivatives in treatment of malconditions such as cancer, and methods of synthesizing the rapamycin analogs and derivatives, are provided.Type: ApplicationFiled: April 13, 2009Publication date: April 28, 2011Inventors: Connie L. Sun, Xiaoyuan Li
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Patent number: 7932261Abstract: The present invention is directed to macrocycle derivatives, pharmaceutical compositions containing them and their use in the treatment of Alzheimer's disease (AD) and related disorders. The compounds of the invention are inhibitors of ?-secretase, also known as ?-site cleaving enzyme and BACE, BACE1, Asp2 and memapsin2.Type: GrantFiled: February 6, 2007Date of Patent: April 26, 2011Assignee: Janssen Pharmaceutica NVInventors: Ellen W. Baxter, François P. Bischoff, Hans De Winter, Chih Yung Ho, Yifang Huang, Michael H. Parker, Allen B. Reitz, Charles H. Reynolds, Eric D. Strobel
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Publication number: 20110092697Abstract: The instant invention describes methods for producing macrocyclic compounds having antiproliferation activity, and useful in methods of treating disorders such as cancer, tumors and cell proliferation related disorders.Type: ApplicationFiled: February 24, 2009Publication date: April 21, 2011Applicant: UNIVERSITY OF FLORIDA RESEARCH FOUNDATIONInventors: Hendrik Luesch, Jiyong Hong
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Patent number: 7923553Abstract: Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin ? and rifaximin ?, and a poorly crystalline form named rifaximin ?, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.Type: GrantFiled: May 13, 2008Date of Patent: April 12, 2011Assignee: Alfa Wassermann, S.p.A.Inventors: Giuseppe Claudio Viscomi, Manuela Campana, Dario Braga, Donatella Confortini, Vincenzo Cannata, Paolo Righi, Goffredo Rosini
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Patent number: 7923230Abstract: Methods and compositions are provided for reducing aggregation of neurodegenerative proteins associated with neurotoxicity or other proteins. The compounds comprise a first domain or targeting element for binding to the target proteins linked to a second domain or recruiting element that binds to an aggregation inhibiting protein, e.g. a prolyl isomerase. By associating the aggregating forming proteins or neuronal cells under conditions where aggregating proteins are produced with the compound and the aggregation inhibiting protein, aggregation is reduced. The subject agents can be used in assays, investigating the etiology of the neuronal diseases and for prophylaxis and therapy.Type: GrantFiled: March 17, 2008Date of Patent: April 12, 2011Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Isabella A. Graef, Gerald R. Crabtree, Jason E. Gestwicki
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Publication number: 20110082091Abstract: The invention teaches a method for testing a prospective or known immunomodulatory drug for T-cell activation, comprising the step of contacting in-vitro a peripheral blood mononuclear cell (PBMC) culture with a predetermined amount of the prospective or known immunomodulatory drug and observing the PBMC culture for T-cell activation using a readout system, upon contact with the prospective or known immunomodulatory drug, wherein the cell density of a PBMC preculture is adjusted such that cell-cell contact of the PBMC is enabled and wherein the PBMC preculture is cultured for at least 12 h.Type: ApplicationFiled: September 28, 2010Publication date: April 7, 2011Applicant: TheraMAB GmbHInventor: Thomas Hünig
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Publication number: 20110060021Abstract: Provided herein is a compound of Formula I: wherein R1 and R2 are as disclosed herein, and including reduced forms and dehydration products, and salts thereof. Also provided are compositions, including pharmaceutical compositions, methods of inhibiting histone deacetylase, methods of increasing histone deacetylase-controlled gene expression in a cell, methods of treating a disease associated with increased histone deacetylase activity, methods of inhibiting growth of a cancer cell, and methods of treating cancer in a subject that comprise a compound of Formula I.Type: ApplicationFiled: August 19, 2010Publication date: March 10, 2011Inventors: Yiqiang Cheng, Cheng Wang
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Patent number: 7902206Abstract: Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin ? and rifaximin ?, and a poorly crystalline form named rifaximin ?, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.Type: GrantFiled: May 13, 2008Date of Patent: March 8, 2011Assignee: Alfa Wassermann, S.p.A.Inventors: Giuseppe Claudio Viscomi, Manuela Campana, Dario Braga, Donatella Confortini, Vincenzo Cannata, Paolo Righi, Goffredo Rosini
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Patent number: 7897608Abstract: The present invention relates to novel 39-desmethoxy-39-methylrapamycin derivatives, methods for their production, and uses thereof. In a further aspect the present invention provides for the use of these 39-desmethoxy-39 -methylrapamycin derivatives in the treatment of cancer and/or B-cell malignancies, the induction or maintenance of immunosuppression, the treatment of transplantation rejection, graft vs. host disease, autoimmune disorders, diseases of inflammation, vascular disease and fibrotic diseases, the stimulation of neuronal regeneration or the treatment of fungal infections.Type: GrantFiled: November 19, 2008Date of Patent: March 1, 2011Assignee: Biotica Technology LimitedInventors: Barrie Wilkinson, Mingqiang Zhang, Rose Mary Sheridan
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Publication number: 20110046367Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.Type: ApplicationFiled: November 1, 2010Publication date: February 24, 2011Applicant: President and Fellows of Harvard CollegeInventors: José A. Halperin, Amarnath Natarajan, Huseyin Aktas, Yun-Hua Fan, Han Chen
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Publication number: 20110028494Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.Type: ApplicationFiled: July 28, 2006Publication date: February 3, 2011Inventors: M. Katharine Holloway, Nigel J. Liverton, John A. McCauley, Michael T. Rudd, Joseph P. Vacca, Steven W. Ludmerer, David B. Olsen
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Patent number: 7872122Abstract: A process for making Biolimus A9 comprises reacting sirolimus (or rapamycin) with alkyl benzene sulfonate under the catalyzing of organic base and in the presence of organic solvent to undergo a nucleophilic substitution reaction to obtain the Biolimus A9 with high yield, not only for small-scale laboratory experiment, but also for rendering reproducibility of high yield even after process amplification.Type: GrantFiled: May 8, 2009Date of Patent: January 18, 2011Assignee: Chunghwa Chemical Synthesis & Biotech Co., Ltd.Inventors: Kwang-Chung Lee, Ping-Shu Chen, Shu-Chuan Lin, Tzu-Ai Lee
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Publication number: 20110009618Abstract: A process for preparing a crystalline rapamycin analog includes: combining the rapamycin analog with an organic medium to form a mixture; incubating the mixture until the rapamycin analog crystallizes; and recovering the crystalline rapamycin analog. The organic medium can be a solvent, and the process can include causing the rapamycin analog to dissolve into the solvent, and incubating the solvent until the rapamycin analog crystallizes. The following can also be performed: forming a slurry of crystalline rapamycin analog; stirring the rapamycin analog mixture until the rapamycin analog crystallizes; saturating the rapamycin analog solution; forming a supersaturated rapamycin analog solution; combining an antisolvent with the rapamycin analog and the solvent to form a biphasic mixture, and incubating the biphasic mixture to cause a liquid-liquid phase split.Type: ApplicationFiled: September 20, 2010Publication date: January 13, 2011Applicant: Abbott LaboratoriesInventors: Shekhar Viswanath, Larry Bartelt, Robert Leanna, Michael Rasmussen, Madhup Dhaon, Rodger Henry, Thomas Borchardt, Shuang Chen, Geoff Zhang
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Publication number: 20110002884Abstract: A class of macrocyclic compounds of formula (I), wherein R1, R3, R4, Ra, Rb, A, B, Z, M, W and n are defined herein, that are useful as inhibitors of viral proteases, particularly the hepatitis C virus (HCV) NS3 protease, are provided. Also provided are processes for the synthesis and use of such macrocyclic compounds for treating or preventing HCV infection.Type: ApplicationFiled: February 12, 2009Publication date: January 6, 2011Inventors: John A. McCauley, Nigel J. Liverton, Steven Harper, Charles J. McIntyre, Michael T. Rudd
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Patent number: 7851620Abstract: This invention relates to novel macrocyclic lactams intermediates useful for the preparation of diazonamide analogs. This invention also relates to a novel electrochemical oxidative cyclization for the preparation of such macrocyclic lactams, and their further elucidation to provide diazonamide analogs.Type: GrantFiled: June 6, 2008Date of Patent: December 14, 2010Assignees: Board of Regents, The University of Texas System, Joyant Pharmaceuticals, Inc.Inventors: Gunnar Hanson, Charles Caldwell, Patrick G. Harran, Susan Harran, Qi Wei, Ming Zhou
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Publication number: 20100311757Abstract: Salarines and Tulearins isolated from Fascaplysinopsis sp. sponge and synthetic derivatives thereof are provided.Type: ApplicationFiled: September 25, 2008Publication date: December 9, 2010Applicants: RAMOT AT TEL-AVIV UNIVERSITY LTD., Université De La RéunionInventors: Yoel Kashman, Maurice Aknin, Amira Rudi, Ashgan Bishara, Drorit Neumann, Nathalie Ben Califa
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Publication number: 20100298248Abstract: The present invention provides a compound of the formula (I) or (II, wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(?O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(?O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent.Type: ApplicationFiled: August 6, 2010Publication date: November 25, 2010Applicant: The U.S.A., as represented by the secretary, Department of Health and Human ServicesInventors: Michael R. Boyd, Kirk R. Gustafson, Charles L. Cantrell
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Patent number: 7838519Abstract: Ansamycin analogs, including maytansinoid analogs, and their use in treating cell proliferative diseases and conditions, and in particular, for use as antitumor agents.Type: GrantFiled: April 4, 2005Date of Patent: November 23, 2010Assignee: The Ohio State University Research FoundationInventors: John M. Cassady, Heinz G. Floss
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Patent number: 7833997Abstract: 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: November 16, 2010Assignee: 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: 20100286185Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.Type: ApplicationFiled: October 23, 2007Publication date: November 11, 2010Inventors: Nigel J Liverton, Joseph P. Vacca, John A. McCauley, Joseph J. Romano, Michael T. Rudo
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Publication number: 20100280238Abstract: The Huisgen 1,3-dipolar cycloaddition is a ‘click’ reaction that results from the ligation of azides and alkynes to give a triazole moiety. This reaction has been shown to be effective in the formation of a variety of macrocyclic rings. A key point of interest is the regioselectivity and specificity of the cycloaddition. Disclosed herein are specific, selective, and high-yielding methods of azide-alkyne macrocyclization to form 1,4- and 1,5-triazoles and libraries thereof.Type: ApplicationFiled: April 29, 2010Publication date: November 4, 2010Inventors: Lisa A. Marcaurelle, Ann R. Kelly, Sarathy Kesavan, Jingqiang Wei, Damian W. Young
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Publication number: 20100279364Abstract: A method of generating synthetic metabolites of CCI-779 is provided. Five novel CCI-779 derivatives are described, as are methods of using these derivatives for detecting CCI-779 metabolites in samples.Type: ApplicationFiled: December 11, 2007Publication date: November 4, 2010Applicant: WyethInventors: Ping Cai, Mark Ruppen, Russ Tsao
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Publication number: 20100273792Abstract: The present invention relates to inhibitors of HCV replication of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein R1; R3; and R4 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.Type: ApplicationFiled: December 23, 2008Publication date: October 28, 2010Inventor: Pierre Jean-Marie Bernard RABOISSON