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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Patent number: 8815888Abstract: The present invention relates to new rifaximin forms kappa, theta, rifaximin:piperazine cocrystal 1 and rifaximin:piperazine cocrystal 2, methods of making same and to their use in medicinal preparations and therapeutic methods.Type: GrantFiled: July 31, 2013Date of Patent: August 26, 2014Assignee: Salix Pharmaceuticals, Ltd.Inventors: Yiduo Wu, Stephan D. Parent, Nathan Carl Schultheiss, Melanie Janelle Bevill, Petinka Vlahova, Travis L. Houston
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Patent number: 8815872Abstract: 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: GrantFiled: September 3, 2009Date of Patent: August 26, 2014Assignee: Merck Patent GmbHInventors: Henry Yu, Lizbeth Celeste De Selm, Xuliang Jiang, Benny C. Askew, Jr., Srinivasa R. Karra, Andreas Goutopoulos
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Publication number: 20140235821Abstract: A substance contains a phosphatidylinositol-3-kinase (PI3K) inhibitor including a depsipeptide-class compound represented by formula (1), or a physiologically acceptable salt thereof that combines a PI3K inhibitory effect and an HDAC inhibitory effect to provide an anti-cancer pharmaceutical composition for the treatment of an intractable cancer.Type: ApplicationFiled: September 25, 2012Publication date: August 21, 2014Applicant: TOHOKU UNIVERSITYInventors: Ken Saijo, Chikashi Ishioka, Tadashi Katoh
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Publication number: 20140221338Abstract: The present invention provides compounds of Formula (Ia): 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: August 6, 2012Publication date: August 7, 2014Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Donald J. P. Pinto, James R. Corte, Paul J. Gilligan, Tianan Fang, Leon M. Smith, II, Yufeng Wang, Wu Yang, William R. Ewing
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Patent number: 8796300Abstract: The invention provides compounds of formula (I) wherein u, d, v, m, n, R1, W, X, Y, and Z have any values defined herein, as well as salts thereof. The compounds have activity as anti-proliferative agents.Type: GrantFiled: November 5, 2010Date of Patent: August 5, 2014Assignees: Rutgers, the State University of New Jersey, University of Medicine and Dentistry of New JerseyInventors: Edmond J. LaVoie, Joseph E. Rice, Suzanne G. Rzuczek, Daniel S. Pilch
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Patent number: 8790691Abstract: 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: GrantFiled: May 26, 2009Date of Patent: July 29, 2014Assignee: The University of British ColumbiaInventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
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Publication number: 20140205567Abstract: The present invention discloses a class of novel macro-heterocyclic compounds represented by the formula Ia or Ib, and their intermediates, preparation methods and the uses. The macro-heterocyclic compounds of the present invention have good inhibitory activities against hepatitis C virus (HCV), and can be used to treat HCV infection effectively by its excellent inhibition against HCV, low toxicity and side effects.Type: ApplicationFiled: June 14, 2012Publication date: July 24, 2014Applicant: AB Pharma Ltd.Inventor: Zheng-yun James Zhan
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Publication number: 20140206683Abstract: The present invention relates to novel macrocylic compounds and compositions containing said compounds acting as kinase inhibitors, in particular as inhibitors of LRRK2 (Leucine-Rich Repeat Kinase 2). Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine or diagnostic agent, in particular for the treatment and/or diagnosis of diseases characterized by LRRK2 kinase activity such as neurological disorders including Parkinson's disease and Alzheimer's disease.Type: ApplicationFiled: September 28, 2012Publication date: July 24, 2014Inventors: Jan Hoflack, Petra Blom
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Patent number: 8785487Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B—W??(I), 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: GrantFiled: January 25, 2011Date of Patent: July 22, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Hui Cao, Yat Sun Or
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Patent number: 8778921Abstract: Aspects of the present invention provide compositions comprising a sulfur containing compound and a compound of the formula (I); and also provide methods of their preparation and use.Type: GrantFiled: October 15, 2009Date of Patent: July 15, 2014Assignee: Infinity Pharmaceuticals, Inc.Inventors: James R. Porter, Sonali Puri
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Patent number: 8778920Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents NH; Y represents —C3-9alkyl-, —C1-5alkyl-NR12—C1-5alkyl-, —C1-6alkyl-NH—CO— or —CO—NH—C1-6alkyl-; X1 represents —O—; X2 represents a direct bond, —NR11—C1-2alkyl-, —NR11—CH2—, —C1-2alkyl-, —O—C1-2alkyl, —O— or —O—CH2—; R1 represents hydrogen or halo; R2 represents hydrogen, cyano, halo, hydroxycarbonyl-, C1-4alkyloxycarbonyl-, Het16-carbonyl- or Ar5; R3 represents hydrogen, hydroxy, C1-4alkyloxy-, Ar4—C1-4alkyloxy or R3 represents C1-4alkyloxy substituted with one or where possible two or more substituents selected from C1-4alkyloxy- or Het2-; R10 represents hydrogen; R11 represents hydrogen, C1-4alkyl- or C1-4alkyl-oxy-carbonyl-; R12 represents Het14-C1-4alkyl, in particular morpholinyl-C1-4alkyl; Het2 represents a heterocycle selected from morpholinyl or piperidinyl optionally substituted with C1-4alkyl-, preferabType: GrantFiled: November 24, 2009Date of Patent: July 15, 2014Assignee: Janssen Pharmaceutica NVInventors: Eddy Jean Edgard Freyne, Peter Jacobus Johannes Antonius Buijnsters, Kristof Van Emelem, Werner Constant Johan Embrechts, Timothy Pietro Suren Perera
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Patent number: 8759512Abstract: 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: GrantFiled: February 24, 2009Date of Patent: June 24, 2014Assignees: University of Florida Research Foundation, Inc., Duke UniversityInventors: Hendrik Luesch, Jiyong Hong
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Patent number: 8754207Abstract: The invention relates to processes for the preparation of compound of CCI-779 having the Formula (I), which is useful as an antineoplastic agent. The invention further relates to certain novel intermediates useful in the preparation of compound of CCI-779 and processes for their preparation. The invention also relates to pharmaceutical compositions that include the compound of CCI-779, prepared according to the processes disclosed herein.Type: GrantFiled: September 24, 2010Date of Patent: June 17, 2014Assignee: Cadila Healthcare LimitedInventors: Mayank Ghanshyambhai Dave, Bipin Pandey
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Patent number: 8754098Abstract: 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: August 23, 2012Date of Patent: June 17, 2014Assignee: Salix Pharmaceuticals, Ltd.Inventors: Karen S. Gushurst, Donglai Yang, Melanie Janelle Bevill, Nathan Carl Schultheiss, Petinka Vlahova, Jeffrey S. Stults, Travis L. Houston
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Publication number: 20140163002Abstract: The present invention provides compounds of Formula (Ia): or stereoisomers, tautomers, or pharmaceutically acceptable salts 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: August 6, 2012Publication date: June 12, 2014Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Patrick Y.S. Lam, Charles G. Clark, James R. Corte, William R. Ewing, Paul J. Gilligan, Yoon Jeon, Wu Yang, Leon M. Smith, II, Yufeng Wang
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Patent number: 8741904Abstract: Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin ? and rifaximin ? useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization process 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: July 25, 2013Date of Patent: June 3, 2014Assignee: Alfa Wassermann S.p.A.Inventors: Giuseppe Claudio Viscomi, Manuela Campana, Donatella Confortini, Maria Barbanti, Dario Braga
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Patent number: 8735419Abstract: Embodiments relate to Rifaximin polymorphic, salt, and hydrate forms, methods of producing polymorphic forms and to their use in medicinal preparations and to therapeutic methods using them.Type: GrantFiled: February 10, 2012Date of Patent: May 27, 2014Assignee: Salix Pharmaceuticals, Ltd.Inventors: Stephan D. Parent, Lisa L. McQueen, Patricia Andres, Paul Schields, Yiduo Wu, Fei Ding, Jared P. Smit
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Publication number: 20140135339Abstract: The invention relates to compounds of formula (?) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.Type: ApplicationFiled: January 15, 2014Publication date: May 15, 2014Applicant: PFIZER INC.Inventors: Simon Bailey, Benjamin Joseph Burke, Michael Raymond Collins, Jingrong Jean Cui, Judith Gail Deal, Robert Louis Hoffman, Qinhua Huang, Ted William Johnson, Robert Steven Kania, John Charles Kath, Phuong Thi Quy Le, Michele Ann McTigue, Cynthia Louise Palmer, Paul Francis Richardson, Neal William Sach
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Patent number: 8722880Abstract: A method for preparing 42-(dimethylphosphinate) Rapamycin (Ridaforolimus) (I) is provided, which has advantages of high conversion rate and no 31,42-bis(dimethyl phosphinate) Rapamycin (III) generated. In the method of the present invention, Rapamycin (II) is firstly reacted with triethyl chlorosilane in a base condition to form 31,42-bis(triethylsilylether) Rapamycin (IV-b), followed by a selective deprotection process to obtain 31-triethylsilylether Rapamycin (V-b). Next, a phosphorylation reaction is performed by using dimethylphosphinic chloride under a base solution to obtain a crude product. Finally, a deprotection reaction is performed in a diluted sulfuric acid solution to obtain a crude product of Ridaforolimus (I). Since the conversion rate of each step of the method of the present invention is higher than 98%, it indicates that the method of the present invention is suitable for industrial production.Type: GrantFiled: August 15, 2013Date of Patent: May 13, 2014Assignee: Chunghwa Chemical Synthesis & Biotech Co., Ltd.Inventors: Kwang-Chung Lee, Yen-Shih Tung, Tzu-Ai Lee, Yu-Hsuan Shih
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Publication number: 20140107101Abstract: 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: March 15, 2013Publication date: April 17, 2014Applicant: JANSSEN R&D IRELANDInventor: Janssen R&D Ireland
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Patent number: 8697704Abstract: 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: GrantFiled: August 11, 2011Date of Patent: April 15, 2014Assignee: Enanta Pharmaceuticals, Inc.Inventors: Yao-Ling Qiu, Xiaowen Peng, Ce Wang, Yat Sun Or
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Patent number: 8697706Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: September 27, 2012Date of Patent: April 15, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Li-Qiang Sun, Qian Zhao, Paul Michael Scola
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Publication number: 20140100193Abstract: Diazonamide analogs having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders, and related pharmaceutical compositions are provided.Type: ApplicationFiled: November 25, 2013Publication date: April 10, 2014Applicant: Joyant Pharmaceuticals, Inc.Inventors: Qi Wei, Ming Zhou, Xiaoming Xu, Charles Caldwell, Susan Harran, Lai Wang
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Publication number: 20140100364Abstract: Compounds useful for making HCV protease inhibitors are described. Methods of using these compounds to make HCV protease inhibitors are also provided.Type: ApplicationFiled: October 7, 2013Publication date: April 10, 2014Inventors: Kenneth M. Engstrom, Yanqun Zhao
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Patent number: 8691811Abstract: The present invention provides a compound of general formulae 5a-r, 9a-i to 13a-i and 17a-i to 22a-i, useful as potential antitumour agents against human cancer cell lines. The present invention further provides a process for the preparation of pyrrolo[2,1-c][1,4]benzodiazepine hybrids of general formulae 5a-r, 9a-i to 13a-i and 17a-i to 22a-i.Type: GrantFiled: July 13, 2009Date of Patent: April 8, 2014Assignee: Council of Scientific & Industrial ResearchInventors: Kamal Ahmed, Earla V. Bharathi, Dudekula Dastagiri, Jonnala S. Reddy, Arutla Viswanath
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Publication number: 20140081016Abstract: The invention refers to the selective acylation of Rapamycin at the 42-position (I) with an acylating agent of the formula (II) wherein R4 and R5 are the same or different, individually the rest of an acetal, especially tetrahydropyran, or of a carbonate or the rest of a silyl ether or taken together are the rest of a boronate, an acetal or ketal.Type: ApplicationFiled: March 30, 2012Publication date: March 20, 2014Applicant: SANDOZ AGInventors: Wolfgang Felzmann, Niklas Schone
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Publication number: 20140080137Abstract: Methods of reversibly inducing proximity of first and second target molecules in a sample are provided. Aspects of the methods include contacting the sample with a modifiable chemical inducer of proximity (MCIP) that reversibly induces proximity of the first and second target molecules, upon application of a stimulus that modifies the MCIP. Aspects of the invention further include methods for regulating a biological process in a cell. Aspects of the invention further include compositions, e.g., compounds and kits, etc., that find use in methods of the invention.Type: ApplicationFiled: September 10, 2013Publication date: March 20, 2014Inventors: Eric Espinosa, Andrew Farmer
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Patent number: 8669360Abstract: A method for converting an amorphous drug, such as everolimus, or other macrolide immunosuppressive drug, into a crystalline form. The method utilizes a slurry of the drug in organic liquid phase and ages the slurry to achieve the conversion.Type: GrantFiled: September 23, 2011Date of Patent: March 11, 2014Assignee: Boston Scientific Scimed, Inc.Inventors: Maggie Zeng, Yen-Lane Chen, Maura Romanshek, Erin Meyer
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Publication number: 20140066473Abstract: A modified release composition comprising tacrolimus which is useful for the treatment or prevention of rejection reactions by transplantation of organs or tissues.Type: ApplicationFiled: November 13, 2013Publication date: March 6, 2014Applicant: Veloxis Pharmaceuticals A/SInventors: Per HOLM, Tomas NORLING
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Publication number: 20140058081Abstract: A method for preparing 42-(dimethylphosphinate) Rapamycin (Ridaforolimus) (I) is provided, which has advantages of high conversion rate and no 31,42-bis(dimethyl phosphinate) Rapamycin (III) generated. In the method of the present invention, Rapamycin (II) is firstly reacted with triethyl chlorosilane in a base condition to form 31,42-bis(triethylsilylether) Rapamycin (IV-b), followed by a selective deprotection process to obtain 31-triethylsilylether Rapamycin (V-b). Next, a phosphorylation reaction is performed by using dimethylphosphinic chloride under a base solution to obtain a crude product. Finally, a deprotection reaction is performed in a diluted sulfuric acid solution to obtain a crude product of Ridaforolimus (I). Since the conversion rate of each step of the method of the present invention is higher than 98%, it indicates that the method of the present invention is suitable for industrial production.Type: ApplicationFiled: August 15, 2013Publication date: February 27, 2014Applicant: Chunghwa Chemical Synthesis & Biotech Co., Ltd.Inventors: Kwang-Chung LEE, Yen-Shih TUNG, Tzu-Ai LEE, Yu-Hsuan SHIH
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Publication number: 20140057844Abstract: The present invention describes the use of translation inhibitors for the treatment of cancer and other disorders. Described herein are translation-inhibiting compounds, and methods of using those compounds for the treatment of cancer and other disorders. In some aspects the compounds inhibit translation elongation at the ribosome. In some aspects the compounds are used alone or in combination with known therapies.Type: ApplicationFiled: December 2, 2011Publication date: February 27, 2014Inventors: Tin Tin Su, Gan Zhang
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Publication number: 20140038885Abstract: There is provided inter alia compounds of formula (I): for use in treatment of viral infection or as an immunosuppressant.Type: ApplicationFiled: March 29, 2012Publication date: February 6, 2014Applicant: NEUROVIVE PHARMACEUTICAL ABInventors: Steven James Moss, Matthew Alan Gregory, Barrie Wilkinson
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Publication number: 20140039011Abstract: 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: October 8, 2013Publication date: February 6, 2014Applicant: SANOFIInventors: Christopher Kallus, Mark Broenstrup, Andreas Evers, Anja Globisch, Herman Schreuder, Michael Wagner
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Publication number: 20140031400Abstract: 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: January 22, 2013Publication date: January 30, 2014Applicant: University of Florida Research Foundation, Inc.Inventor: University of Florida Research Foundation, Inc.
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Publication number: 20140030221Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.Type: ApplicationFiled: June 7, 2013Publication date: January 30, 2014Inventors: Caroline Aciro, Victoria Alexandra Steadman, Simon Neil Pettit, Karine G. Poullennec, Linos Lazarides, David Kenneth Dean, Neil Andrew Dunbar, Adrian John Highton, Andrew John Keats, Dustin Scott Siegel, Kapil Kumar karki, Adam James Schrier, Petr Jansa, Richard Mackman
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Patent number: 8633234Abstract: Amorphous rifaximin, methods of making it, and pharmaceutical compositions containing it. Also described are methods of converting amorphous rifaximin to crystalline rifaximin and vice versa.Type: GrantFiled: September 24, 2007Date of Patent: January 21, 2014Assignee: Cipla LimitedInventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Manjinder Singh Phull, Maruti Ghagare
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Publication number: 20140017198Abstract: Compounds of Formula I are disclosed As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.Type: ApplicationFiled: July 2, 2013Publication date: January 16, 2014Inventors: Kyla Bjornson, Eda Canales, Jeromy J. Cottell, Kapil Kumar Karki, Ashley Anne Katana, Darryl Kato, Tetsuya Kobayashi, John O. Link, Ruben Martinez, Barton W. Phillips, Hyung-Jung Pyun, Michael Sangi, Adam James Schrier, Dustin Siegel, James G. Taylor, Chinh Viet Tran, Teresa Alejandra Trejo Martin, Randall W. Vivian, Zheng-Yu Yang, Jeff Zablocki, Sheila Zipfel
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Patent number: 8629150Abstract: The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: September 24, 2012Date of Patent: January 14, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Tao Wang, Li-Qiang Sun, Paul Michael Scola, Zhongxing Zhang, Qian Zhao
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Patent number: 8628922Abstract: The present invention relates to a method for increasing the chronological lifespan of a cell comprising disrupting the function of at least one of the SAGA1 SLIK and/or SALSA complexes in said cell.Type: GrantFiled: July 8, 2010Date of Patent: January 14, 2014Assignee: Chronos Therapeutics LimitedInventors: Elizabeth Jane Mellor, Michael Youdell, Anitha Nair, Alexandre Akoulitchev
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Publication number: 20130323284Abstract: A method for treating a mammal having an infection with an organism that persists intracellularly in a mammalian cell by inducing an autophagy defect includes administering to the mammal an effective dose of a bioavailable agent that restores autophagy function, by inhibition of the mTOR pathway.Type: ApplicationFiled: June 5, 2012Publication date: December 5, 2013Applicant: JAZZYA INVESTMENTSInventor: Jose A. Bengoechea Alonso
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Publication number: 20130317053Abstract: An external medicine of the present invention includes a gel composition or an ointment composition, each of which contains sirolimus and/or a derivative thereof. Accordingly, provided is an external medicine which enables sirolimus, in an amount sufficient to treat a skin disease, to be absorbed into an affected part without causing a side effect.Type: ApplicationFiled: January 30, 2012Publication date: November 28, 2013Applicant: OSAKA UNIVERSITYInventors: Mari Kaneda, Ichiro Katayama
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Patent number: 8580777Abstract: 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: GrantFiled: May 22, 2009Date of Patent: November 12, 2013Assignee: SanofiInventors: Christopher Kallus, Mark Broenstrup, Andreas Evers, Anja Globisch, Herman Schreuder, Michael Wagner
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Publication number: 20130296550Abstract: A method for synthesizing temsirolimus, the method including: using a substituted boric acid to protect 2,2-dimethylol propionic acid to produce intermediate II; carrying out a reaction between the intermediate II and 2,4,6-trichlorobenzoyl chloride; carrying out condensation reaction between a resulting product and rapamycin to produce intermediate III; and finally using a diol to remove a protecting group from the intermediate III to yield temsirolimus.Type: ApplicationFiled: July 1, 2013Publication date: November 7, 2013Inventors: Honghai SONG, Long TANG, Wei CHEN, Zheng LI, Jinzhou LI, Zhicun SUN, Jiajin FENG
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Patent number: 8569333Abstract: A prodrug compound of a rapamycin analog and methods for inhibiting, treating, and preventing mammalian diseases.Type: GrantFiled: May 27, 2011Date of Patent: October 29, 2013Assignee: 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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Patent number: 8569326Abstract: The present invention relates to Rifaximin polymorphic forms, to their use in medicinal preparations and to therapeutic methods using them.Type: GrantFiled: August 16, 2012Date of Patent: October 29, 2013Assignee: Salix Pharmaceuticals, Ltd.Inventors: Karen S. Gushurst, Donglai Yang, Petinka Vlahova, Jeffrey S. Stults
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Publication number: 20130274463Abstract: The present invention relates to macrolactam compounds, intermediates useful in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing and modifying macrolactams. One use of the compounds and methods described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. An example of an HCV inhibitory compound that can be synthesized using the procedures described herein is Compound A and derivative thereof.Type: ApplicationFiled: December 13, 2011Publication date: October 17, 2013Inventors: Cheng Chen, Jongrock Kong, Guy Humphrey, Sarah Dolman, Hongmei Li, Matthew T. Tudge, Kelvin Yong, Bangping Xiang, Michael Zacuto
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Publication number: 20130267511Abstract: 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: June 3, 2013Publication date: October 10, 2013Inventors: Pierre Jean-Marie Bernard Raboisson, Lili Hu, Sandrine Vendeville, Origene Nyanguile
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Publication number: 20130252961Abstract: The invention relates to compounds of formula (?) as further defined herein and to the pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising such compounds and salts, and to the uses thereof. The compounds and salts of the present invention inhibit anaplastic lymphoma kinase (ALK) and/or EML4-ALK and are useful for treating or ameliorating abnormal cell proliferative disorders, such as cancer.Type: ApplicationFiled: March 5, 2013Publication date: September 26, 2013Applicant: PFIZER INC.Inventors: Simon BAILEY, Benjamin Joseph Burke, Michael Raymond Collins, Jingrong Jean Cui, Judith Gail Deal, Robert Louis Hoffman, Qinhua Huang, Ted William Johnson, Robert Steven Kania, John Charles Kath, Phuong Thi Quy Le, Michele Ann McTigue, Cynthia Louise Palmer, Paul Francis Richardson, Neal William Sach
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Patent number: 8524893Abstract: Novel intermediates, process for their preparation and their use in the preparation of therapeutically effective antineoplastic agents, in particular Temsirolimus of formula (I).Type: GrantFiled: January 28, 2011Date of Patent: September 3, 2013Assignee: Fresenius Kabi Oncology LimitedInventors: Nitin Gupta, Vishal Handa, Abir Kumar Pal, Hemant Kumar Singh, Saswata Lahiri, Sushil Kumar Dubey
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Patent number: 8518949Abstract: Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin ? and rifaximin ? useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization process 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: June 4, 2012Date of Patent: August 27, 2013Assignee: ALFA Wassermann S.p.A.Inventors: Giuseppe Claudio Viscomi, Manuela Campana, Donatella Confortini, Maria Miriam Barbanti, Dario Braga