Ring Carbons Shared By Each Of The Three Cyclos (e.g., 1,8-naphthalimides, Etc.) Patents (Class 514/296)
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Publication number: 20110192493Abstract: The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments.Type: ApplicationFiled: April 14, 2011Publication date: August 11, 2011Applicants: Helsinn Healthcare S.A., Roche Palo Alto LLCInventors: Giorgio Calderari, Daniele Bonadeo, Roberta Cannella, Enrico Braglia, Riccardo Braglia, Andrew Miksztal, Thomas Malefyt, Kathleen M. Lee
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Publication number: 20110178163Abstract: The present disclosure provides methods of determining the levels of BRCA1 in a cell, altering the levels of BRCA1 in a cell, determining the likelihood of developing cancer, and determining the prognosis of a patient with cancer using miR-182 and analogs thereof. Importantly, the invention also provides methods of determining whether a patient should be treated with PARP inhibitors, improving PARP therapy in cancer, as well as methods for selecting and improving genotoxic therapies. Also featured are methods of treating patients with cancers based on the expression levels of miR-182. The invention also features compositions comprising miR-182 and analogs thereof, antagomirs of mIR-182 and analogs thereof, in combination with PARP inhibitors and genotoxic agents.Type: ApplicationFiled: January 13, 2011Publication date: July 21, 2011Inventor: Dipanjan Chowdhury
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Publication number: 20110178118Abstract: Methods and compositions for reducing chemotherapy and radiotherapy induced emises with 5-HT3 receptor antagonists are disclosed, especially with palonosetron.Type: ApplicationFiled: March 31, 2011Publication date: July 21, 2011Inventors: Alberto Macciocchi, Sergio Cantoreggi, Enrico Braglia, Riccardo Branglia, Simone Macciocchi, Giulio Macciocchi
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Publication number: 20110160181Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: ApplicationFiled: February 28, 2011Publication date: June 30, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: ANTONI TORRENS, JORDI QUINTANA, HELMUT BUSCHMANN, ALBERT DORDAL, JOSEP MAS
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Patent number: 7947839Abstract: Bis 1,8 naphthalimide compounds including antibody drug conjugate (ADC) are described. Pharmaceutical compositions comprising an effective amount of a 1,8 bis-naphthalimide compound for treatment of hyperproliferative disorders and other disorders are described. Methods are described for killing or inhibiting the proliferation of tumor cells or cancer cells including administering to a patient an effective amount of a 1,8 bis-naphthalimide compound.Type: GrantFiled: January 30, 2006Date of Patent: May 24, 2011Assignee: Genentech, Inc.Inventors: Lewis J. Gazzard, Edward HyungSuk Ha, David Y. Jackson, Joann M. Um
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Publication number: 20110092447Abstract: Compounds can be used to act as inhibitors of enzymes having histone deacetylase activity for the medical therapy of conditions which predispose a person for the development of a disease, such as but not limited to cancer, inflammatory or metabolic diseases. Such conditions are linked to genetically inherited mutations of crucial genes which predispose a person with this condition to develop the disease phenotype. Thus, such compounds can be used for a suppressive therapeutic approach—the SUPPRESSION THERAPY—in order to inhibit or delay the onset or progression of the genetically predisposed disorder. Furthermore, a clinically used medicament can be manufactured for the SUPPRESSION THERAPY of such inherited predisposing conditions.Type: ApplicationFiled: December 22, 2010Publication date: April 21, 2011Inventors: Bernd Hentsch, Alexander B. Maurer, Sascha Hovelmann, Monika Raab, Elke Martin
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Patent number: 7897766Abstract: The invention relates to amine-substituted aza-adamantane derivatives, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. Radiolabelled compounds useful for evaluating the binding affinity to ?7 nicotinic acetylcholine receptors also are described.Type: GrantFiled: September 7, 2006Date of Patent: March 1, 2011Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Kevin B. Sippy, David J. Anderson, William H. Bunnelle, Diana L. Nersesian
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Publication number: 20110044899Abstract: A compound of formula (I): in which R1 represents a hydrogen atom, an optionally labelled halogen, a radionuclide or a Sn[(C1-C4)alkyl]3 group, Ar represents an aryl group or a heteroaryl group, R9 represents a hydrogen atom, a (C1-C4) alkyl group or forms together with the group R1—Ar a ring fused with the Ar group, A represents a group of formula (?) or (?): R3 and R4 independently represent a hydrogen atom, a (C1-C6)alkyl group, a (C1-C6) alkenyl group or a group of formula (y): wherein R11 represents an optionally labelled halogen, a radionuclide, an aryl or heteroaryl group optionally substituted by an optionally labelled halogen, a radionuclide, a —NO2 group, a —NR5R6 group, a N+R5R6R7X? group, or a —OSO2R12 group, and their addition salts with pharmaceutically acceptable acids.Type: ApplicationFiled: January 28, 2009Publication date: February 24, 2011Applicants: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), COMMISSARIAT A L'ENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES, UNIVERSITE D'AUVERGNE CLERMONT 1, LABORATOIRES CYCLOPHARMAInventors: Jean-Michel Chezal, Frederic Dolle, Jean-Claude Madelmont, Aurelie Maisonial, Elisabeth Miot-Noirault, Nicole Moins, Janine Papon, Bertrand Kuhnast, Bertrand Tavitian, Raphael Boisgard
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Publication number: 20110028420Abstract: A method is disclosed for treating and inducing the regression of established atherosclerotic plaques. A method is disclosed for treating asthma, including treatment of an ongoing asthma attack. In both cases, treatment with PARP inhibitors, such as the PARP inhibitor TIQ-A (Thieno[2,3-c]isoquinolin-5-one), can lead to regression of existing disease and symptoms.Type: ApplicationFiled: April 7, 2009Publication date: February 3, 2011Inventors: Hamid A. Boulares, Chetan P. Hans, Amarjit S. Naura
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Publication number: 20110003742Abstract: The present invention provides methods for dosing patients with naphthalimides, including amonafide, amonafide salts, and analogs thereof based on N-acetyl transferase genotyping. The invention also provides methods for dosing the amount of granulocyte colony stimulating factor (GCSF) used in combination with naphthalimide to prevent or modulate leukocytopenia.Type: ApplicationFiled: March 9, 2010Publication date: January 6, 2011Applicant: ChemGenex Pharmaceuticals, Inc.Inventor: Dennis M. Brown
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Publication number: 20100303719Abstract: The present invention relates to anti-cancer compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides analogs of the known anti-cancer compound amonafide, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with hyperproliferation.Type: ApplicationFiled: January 12, 2009Publication date: December 2, 2010Applicant: NORTHWESTERN UNIVERSITYInventors: Sui Huang, John Norton, Daniel Appella, Mark Witschi
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Publication number: 20100305152Abstract: The shikimate pathway links metabolism of carbohydrates to biosynthesis of aromatic compounds, which is an attractive target for the rational drug and herbicide design because it is essential in algae, higher plants, bacteria, and fungi, but absent from mammals. Thus, the present invention provides a method of inhibiting the growth of bacteria or fungi, especially Helicobacter pylori, through inhibiting enzymes in the shikimate pathway.Type: ApplicationFiled: May 27, 2009Publication date: December 2, 2010Applicant: NATIONAL TSING HUA UNIVERSITYInventors: WEN-CHING WANG, WEN-CHI CHENG, JINN-MOON YANG
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Publication number: 20100292267Abstract: The present invention provides novel palonosetron free base in an amorphous form and crystalline form-G and processes for their preparation. The present invention also provides a process for the preparation of palonosetron hydrochloride from the novel palonosetron free base in an amorphous form and/or in crystalline form-G.Type: ApplicationFiled: December 11, 2008Publication date: November 18, 2010Applicant: GLENMARK GENERICS LTDInventors: Mubeen Khan, Mahendra Patil Raghunath, Prashant Yadav Kundlik
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Publication number: 20100226857Abstract: The present invention provides new compositions and methods for treatment of intracellular parasites. The compositions comprise one or more hydroxamic acids in an amount sufficient to interfere with the activity of one or more histone deacetylases in the intracellular parasites. The compositions and methods can be used to treat members of the Apicomplexa group of intracellular parasites.Type: ApplicationFiled: March 28, 2007Publication date: September 9, 2010Inventors: Jeannine Strobl, David S. Lindsay
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Publication number: 20100215728Abstract: Disclosed are compositions and methods for skincare, e.g., reducing skin wrinkles and for treating skin disorders.Type: ApplicationFiled: February 5, 2010Publication date: August 26, 2010Applicant: Asan Laboratories Company (Cayman), LimitedInventors: Yih-Lin Chung, Nam-Mew Pui, Wei-Wei Chang
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Publication number: 20100204263Abstract: A method of treating multidrug resistant cancers in a patient, comprising administering to said patient a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof. The values and preferred values for variables R1 and R2 are defined herein.Type: ApplicationFiled: January 9, 2008Publication date: August 12, 2010Inventors: Alfred M. Ajami, Robert L. Capizzi
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Publication number: 20100178331Abstract: Disclosed is a preparation for transnasal application, which has improved fluidability. Specifically disclosed is a preparation for transnasal application, which comprises at least a complex comprising: a fluidability-improving component comprising a first crystalline cellulose (A) having specified powder properties, tricalcium phosphate (B) having specified powder properties, and a second crystalline cellulose (C) having specified powder properties or a starch (D) having specified powder properties; and a physiologically active substance.Type: ApplicationFiled: December 25, 2007Publication date: July 15, 2010Inventors: Ryoichi Nagata, Shunji Haruta
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Publication number: 20100166781Abstract: The invention provides processes and compositions for enhancing the immunogenicity of TAP-1 expression-deficient cells by increasing the presentation of MHC Class I surface molecules for detection by cytotoxic T-lymphocyte cells through increased TAP-1 expression, which comprises administering to the TAP-1 expression-deficient cells a TAP-1 expression increasing amount of a bio-acceptable substance that promotes transcription of TAP-1 gene in the cells to cause enhanced MHC Class I surface expression of the cells. The bio-acceptable substance may be a histone H3 deacetylase inhibitor, such as trichostatin A, a transcriptional co-activator having intrinsic histone acetyl transferase activity or a histone acetyl transferase comprising at least one member of the CBP/p300 protein family. The process and compositions increase the immunogenicity of the target cells to enhance their destruction by cytotoxic lymphocytes.Type: ApplicationFiled: July 17, 2009Publication date: July 1, 2010Applicant: Tapimmune, Inc.Inventors: Alvernia F. Setiadi, Muriel David, Robyn P. Seipp, Jennifer Hartikainen, Rayshad Gopaul, Wilfred Arthur Jefferies
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Publication number: 20100168093Abstract: The present invention relates to substituted pyrrolidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal.Type: ApplicationFiled: April 30, 2007Publication date: July 1, 2010Inventors: Miguel Angel Pericas-Brondo, Antoni Torrens-Jover, Susana Yenes-Minguez, Félix Cuevas Cordobés, Carmen Garcia Granda
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Publication number: 20100158798Abstract: The present invention embraces compounds selected for interacting with the Fingers-Palm pocket of telomerase and use thereof for modulating the activity of telomerase and preventing or treating diseases or conditions associated with telomerase.Type: ApplicationFiled: February 8, 2010Publication date: June 24, 2010Inventor: Emmanuel Skordalakes
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Publication number: 20100143461Abstract: The present invention provides solid oral formulations of palonosetron or salts thereof.Type: ApplicationFiled: December 8, 2009Publication date: June 10, 2010Inventors: Ben-Zion Solomon, Zvika Doani
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Publication number: 20100144754Abstract: This invention provides methods and pharmaceutical compositions for preventing or treating physical dependence and/or withdrawal associated with narcotic use, in particular by modulating a 5-HT3 receptor. Using a computational genetic approach in mice, a gene conserved between mice and humans was identified as candidate as a modulator of physical dependence to morphine. Administration of compounds that modulate 5-HT3 receptors was found to control withdrawal from morphine in mice and humans.Type: ApplicationFiled: December 4, 2009Publication date: June 10, 2010Applicant: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Gary PELTZ, David CLARK, Lawrence CHU
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Publication number: 20100113405Abstract: The present invention relates to new methylindazole modulators of 5-HT3 receptor activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: November 4, 2009Publication date: May 6, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Publication number: 20100093611Abstract: Methods of treating, ameliorating, preventing, or reducing the risk of developing an auto-immune disease and/or an inflammatory condition, such as systemic lupus erythematosus, in a patient, such as a human being, using a therapeutically effective amount of an agent(s) that inhibits the activity of one or more of histone deacetylase (HDAC), IKB kinase (IKK-2), nuclear factor kB (NF-kB), ubiquitin/proteasome and Janus kinase (JAK) are disclosed. Compounds useful in such methods are also presented.Type: ApplicationFiled: May 16, 2008Publication date: April 15, 2010Inventors: Stephen K. Horrigan, Qin Zong, Daniel Soppet, Juana Castaneda, Bo Chen, Ricardo Cibotti, Laurent P. Audoly, Anthony Coyle, Peter Kiener
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Publication number: 20100048607Abstract: Pharmaceutical compositions comprising palonosetron and its pharmaceutically acceptable salts, in the form of a ready-to-use solution or a lyophilized form. Specific embodiments of the invention relate to stable pharmaceutical formulations of palonosetron and its pharmaceutically acceptable salts, wherein the formulation does not comprise a chelating agent or an antioxidant.Type: ApplicationFiled: August 24, 2009Publication date: February 25, 2010Inventors: Chandrashekhar Kocherlakota, Sreedhar Bandari, Nagaraju Banda, Kranthi Kumar Hinge, Ramachandra Reddy Yeluri
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Publication number: 20100048608Abstract: Ophthalmic compositions containing HDAC inhibitors and their use for treating ocular neovascular or edematous diseases and disorders are disclosed.Type: ApplicationFiled: October 30, 2009Publication date: February 25, 2010Applicant: ALCON, INC.Inventors: Peter G. Klimko, David P. Bingaman
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Publication number: 20090312363Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.Type: ApplicationFiled: February 14, 2007Publication date: December 17, 2009Inventors: James Elliot Bradner, Ralph Mazitschek, Tang Weiping, Stuart S. Schreiber
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Publication number: 20090285877Abstract: There is provided a percutaneous absorption preparation that has a simple laminated structure and a long shelf life, while maintaining excellent percutaneous absorption for palonosetron. The percutaneous absorption preparation comprises a support and a drug-containing pressure-sensitive adhesive layer formed on at least one side of the support, wherein the drug-containing pressure-sensitive adhesive layer comprises, as essential constituent components, an adhesive base, palonosetron or a pharmaceutically acceptable acid addition salt thereof, and at least one type of fatty alcohol selected from the group consisting of C6-12 straight-chain saturated alcohols, C10-22 straight-chain unsaturated alcohols, C10-22 branched alcohols and C10-15 cyclic alcohols, and the constituent components other than palonosetron or its pharmaceutically acceptable acid addition salt are carboxyl group-free components.Type: ApplicationFiled: May 14, 2009Publication date: November 19, 2009Applicant: HISAMITSU PHARMACEUTICAL CO., INC.,Inventors: Takashi Yasukochi, Yukihisa Naka, Tsuyoshi Endo, Hirotoshi Adachi
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Publication number: 20090264458Abstract: The invention relates to compounds having pharmacological activity towards the 5-receptor, and more particularly to some 2,2a,4,5-tetrahydro-1H-3-aza-acenaphthylen substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders.Type: ApplicationFiled: May 22, 2009Publication date: October 22, 2009Inventors: Antoni Torrens Jover, Susana Yenes Minguez, Josep Mas Prio, Luz Romero Alonso, Alberto Dordal Zueras, Helmut Henrich Buschmann
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Publication number: 20090232907Abstract: Novel ureyl-substituted naphthalimide derivatives, pharmaceutically acceptable salts thereof and solvates thereof, are useful for making pharmaceutical compositions for the treatment of cell proliferative diseases such as cancer. The invention also provides methods of treating specific types of cancer such as prostate, esophageal, glioblastoma, gliosarcoma, NSCLC, head and neck, and breast with the compounds described herein alone and in combination with antineoplastic agents.Type: ApplicationFiled: November 17, 2008Publication date: September 17, 2009Applicant: Unibioscreen S.A.Inventors: Eric Van Quaquebeke, Gentiane Simon, Mohamed El Yazidi, Jerome Tuti, Laurent Van Den Hove, Francis Darro, Robert Kiss
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Publication number: 20090221628Abstract: Novel ureyl-substituted naphthalimide derivatives, pharmaceutically acceptable salts thereof and solvates thereof, are useful for making pharmaceutical compositions for the treatment of cell proliferative diseases such as cancer. The invention also provides methods of treating specific types of cancer such as prostate, esophageal, glioblastoma, gliosarcoma, NSCLC, head and neck, and breast with the compounds described herein alone and in combination with antineoplastic agents.Type: ApplicationFiled: November 17, 2008Publication date: September 3, 2009Applicant: Unibioscreen S.A.Inventors: Eric Van Quaquebeke, Gentiane Simon, Mohamed El Yazidi, Jerome Tuti, Laurent Van Den Hove, Francis Darro, Robert Kiss
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Publication number: 20090215815Abstract: A pharmaceutical composition comprising a compound of Formula I wherein R1 is selected from, inter alia, alkyl, aryl-loweralkyl, heterocycle-loweralkyl, loweralkyl-carbonate; optionally substituted amino; benimidaz-2-yl; optionally substituted phenyl; loweralkyl-(R5)(R6) wherein one of R5 and R6 is selected from H and the other is selected from carboxy, carboxy-loweralkyl and loweralkoxycarbonyl; NHCH2CH2OX wherein X represents an in vivo hydrolyzable ester; and R2 and R3 are independently selected from H, NO2, halo, di(loweralkyl)amino, cyano, C(O)OH, phenyl-S—, loweralkyl, and Z(O)OR7 wherein Z is selected from C and S and R7 is selected from H, loweralkylamino and arylamino; or pharmaceutically acceptable salts or certain in vivo hydrolyzable esters or amides thereof, in an amount effective to inhibit neurotrophin-mediated activity, and a suitable carrier, is described.Type: ApplicationFiled: April 28, 2009Publication date: August 27, 2009Inventors: Ashok Tehim, Xiannong Chen
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Publication number: 20090215814Abstract: The present invention relates to compositions which inhibit the binding of nerve growth factor to the p75NTR common neurotrophin receptor and methods of use thereof. In one embodiment, the compound which inhibits binding of nerve growth factor to p75NTR comprises, particularly when bound to nerve growth factor, at least two of the following: (1) a first electronegative atom or functional group positioned to interact with Lys34 of nerve growth factor; (2) a second electronegative atom or functional group positioned to interact with Lys95 of nerve growth factor; (3) a third electronegative atom or functional group positioned to interact with Lys88 of nerve growth factor; (4) a fourth electronegative atom or functional group positioned to interact with Lys32 of nerve growth factor; and (5) a hydrophobic moiety which interacts with the hydrophobic region formed by Ile31, Phe101 and Phe86 of nerve growth factor.Type: ApplicationFiled: April 28, 2009Publication date: August 27, 2009Inventors: Gregory M. Ross, Igor L. Shamovsky, Sandra Marone, Donald F. Weaver, Richard J. Riopelle
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Publication number: 20090203728Abstract: The invention relates to compounds for use in medicine.Type: ApplicationFiled: March 31, 2005Publication date: August 13, 2009Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCHInventors: Surana Uttam, Vaidehi Krishnan, Anthony Ting, Hong Hwa Lim
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Compositions and methods for treatment of glioblastoma, gliosarcoma, NSCLC, and head and neck cancer
Publication number: 20090186915Abstract: Novel ureyl-substituted naphthalimide derivatives, pharmaceutically acceptable salts thereof and solvates thereof, are useful for making pharmaceutical compositions for the treatment of cell proliferative diseases such as cancer. The invention also provides methods of treating specific types of cancer such as prostate, esophageal, glioblastoma, gliosarcoma, NSCLC, head and neck, and breast with the compounds described herein alone and in combination with antineoplastic agents.Type: ApplicationFiled: November 17, 2008Publication date: July 23, 2009Applicant: Unibioscreen S. A.Inventors: Eric Van Quaquebeke, Gentiane Simon, Mohamed El Yazidi, Jerome Tuti, Laurent Van Den Hove, Francis Darro, Robert Kiss -
Publication number: 20090181927Abstract: Naphthalimide compounds are used in tissue bonding and protein cross-linking applications. When activated by an activating agent, such as light in the 400-500 nm absorption range, the naphthalimide compounds form chemically-reactive species that cross-link proteins, bond connective tissues together, and bond tissues and other biomaterials together. A naphthalimide-labeled biomolecule, such as a naphthalimide-labeled chitosan, is also capable of bonding tissues without subsequent direct illumination of the contacted tissue area. The naphthalimide compounds may be used in tissue or arterial repair, stabilization of an expanded arterial wall after angioplasty, tethering pharmaceutical agents to tissue surfaces to provide local drug delivery, and for chemically bonding skin care products, sunscreens, and cosmetics to the skin.Type: ApplicationFiled: March 19, 2009Publication date: July 16, 2009Applicant: PhotoBioMed CorporationInventors: Ronald E. Utech, Kaia L. Kloster, Millard M. Judy, Kevin J. Vaska, James L. Matthews
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Publication number: 20090181971Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: ApplicationFiled: August 13, 2007Publication date: July 16, 2009Inventors: Daniel Delorme, Soon Hyung Woo, Arkadii Vaisburg
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Patent number: 7557120Abstract: The present invention is directed to compounds of formulae (I and II)(wherein A, D, E, X, l, m, n and R1 through R18 are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.Type: GrantFiled: February 23, 2004Date of Patent: July 7, 2009Assignee: Merck & Co., Inc.Inventors: Stephen D. Goble, Alexander Pasternak, Cheng Tang, Changyou Zhou, Lihu Yang
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Publication number: 20090170840Abstract: The present invention generally relates to compounds to treat viral infections and methods of their use. In particular, compounds of the present invention inhibit the activity of NS1 protein, thereby mitigating viral infection and, in particular, influenza virus infection. Accordingly, NS1 protein inhibitors and methods of treatment that employ such inhibitors are contemplated by the present invention.Type: ApplicationFiled: December 8, 2008Publication date: July 2, 2009Inventors: Michael Roth, Beatriz Fontoura, Shuguang Wei, Neal Satterly
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Patent number: 7553965Abstract: The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some 2,2a,4,5-tetrahydro-1H-3-aza-acenaphthylen substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders.Type: GrantFiled: December 27, 2005Date of Patent: June 30, 2009Assignee: Laboratories Del Dr. Esteve, S.A.Inventors: Antoni Torrens Jover, Susana Yenes Mínguez, Josep Mas Prió, Luz Romero Alonso, Alberto Dordal Zueras, Helmut Henrich Buschmann
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Publication number: 20090163451Abstract: The invention features methods of treating visceral pain in humans by administering an effective amount of a 5HT1B or 5HT1D receptor agonist, (e.g., a triptan). These methods can be used, for example, to treat a human suffering from visceral pain secondary to an underlying disease of a visceral organ, such as pancreatitis. Visceral pain treatable by the methods of the invention may also be secondary to a disease of the liver, kidney, ovary, uterus, bladder, bowel, stomach, esophagus, duodenum, intestine, colon, spleen, pancreas, appendix, heart, or peritoneum.Type: ApplicationFiled: November 17, 2008Publication date: June 25, 2009Inventors: Frank Porreca, Louis P. Vera-Portocarrero
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Publication number: 20090118321Abstract: Novel ureyl-substituted naphthalimide derivatives, pharmaceutically acceptable salts thereof and solvates thereof, are useful for making pharmaceutical compositions for the treatment of cell proliferative diseases such as cancer. The invention also provides methods for making such derivatives through hydrolysis of known compounds.Type: ApplicationFiled: May 7, 2007Publication date: May 7, 2009Applicant: Unibioscreen S.A.Inventors: Eric Van Quaquebeke, Gentiane Simon, Mohamed El Yazidi, Jerome Tuti, Laurent Van den Hove, Francis Darro, Robert Kiss
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Publication number: 20090076021Abstract: A therapeutic combination, useful in a co-therapy method for improving cardiovascular performance and/or treating cardiovascular diseases, is provided comprising a first agent and a second agent, wherein the first agent comprises a histone deacetylase inhibiting agent and the second agent comprises at least one nuclear hormone receptor ligand.Type: ApplicationFiled: August 26, 2008Publication date: March 19, 2009Inventor: Craig F. Plato
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Publication number: 20090062329Abstract: The bisnaphthalimidopropyl derivatives with anti-parasitic and anti-cancer activity. Bisnaphthalimidopropyl derivatives (A) BNIPPut, BNIPDapen, BNIPDhex, BNIPDahep, BNIPDaoct, BNIPDanon, BNTPDadec, BNIPDadod, BNPDpta, BNIPDeta were synthesized in yields ranging from 50-70 and their cytotoxicity against colon cancer cells (CaCo-2) and the parasite Leishmania infantum determined using the MTT assay and by luciferase activity present in parasite, respectively. Cytotoxicity within CaCo-2 cells was manifested with IC50 values between 0.3 and 22 m M after 48 h of compounds incubation. Against Leishmania infantum, IC50 values were encompassed within a narrower concentration range of 0.39-2.09 m M, for pro-mastigote form, and between 5.24 and 17.42 m M, for axenic amastigote and between 2.43 and 9.52 m M, for intracellular amastigote forms.Type: ApplicationFiled: June 15, 2007Publication date: March 5, 2009Inventors: Anabela Cordeiro Da Silva, Joana Alexandra Pinto Da Costa Tavares, Paul Kong Thoo Lin
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Publication number: 20090036480Abstract: The invention relates to compounds having pharmacological activity towards the 5-HT7 receptor, and more particularly to some 2,2a,4,5-tetrahydro-1H-3-aza-acenaphthylen substituted sulfonamide compounds, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which 5-HT is involved, such as CNS disorders.Type: ApplicationFiled: December 27, 2005Publication date: February 5, 2009Inventors: Antoni Torrens Jover, Susana Yenes Minguez, Josep Mas Prio, Luz Romero Alonso, Alberto Dordal Zueras, Helmut Henrich Buschmann
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Publication number: 20080287484Abstract: A pharmaceutical composition comprising a compound of Formula I wherein R1 is selected from, inter alia, alkyl, aryl-loweralkyl, heterocycle-loweralkyl, loweralkyl-carbonate; optionally substituted amino; benzimidaz-2-yl; optionally substituted phenyl; loweralkyl-(R5)(R6) wherein one of R5 and R6 is selected from H and the other is selected from carboxy, carboxy-loweralkyl and loweralkoxycarbonyl; NHCH2CH2OX wherein X represents an in vivo hydrolyzable ester; and R2 and R3 are independently selected from H, NO2, halo, di(loweralkyl)amino, cyano, C(O)OH, phenyl-S—, loweralkyl, and Z(O)OR7 wherein Z is selected from C and S and R7 is selected from H, loweralkylamino and arylamino; or pharmaceutically acceptable salts or certain in vivo hydrolyzable esters or amides thereof, in an amount effective to inhibit neurotrophin-mediated activity, and a suitable carrier, is described.Type: ApplicationFiled: September 28, 2007Publication date: November 20, 2008Inventors: Ashok Tehim, Xiannong Chen
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Publication number: 20080279821Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt, ester, or prodrug, 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: April 24, 2008Publication date: November 13, 2008Inventors: Deqiang Niu, Yat Sun Or, Zhe Wang
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Publication number: 20080221147Abstract: The present invention relates to compositions which inhibit the binding of nerve growth factor to the p75NTR common neurotrophin receptor and methods of use thereof. In one embodiment, the compound which inhibits binding of nerve growth factor to p75NTR comprises, particularly when bound to nerve growth factor, at least two of the following: (1) a first electronegative atom or functional group positioned to interact with Lys34 of nerve growth factor; (2) a second electronegative atom or functional group positioned to interact with Lys95 of nerve growth factor; (3) a third electronegative atom or functional group positioned to interact with Lys88 of nerve growth factor; (4) a fourth electronegative atom or functional group positioned to interact with Lys32 of nerve growth factor; and (5) a hydrophobic moiety which interacts with the hydrophobic region formed by Ile31, Phe101 and Phe86 of nerve growth factor.Type: ApplicationFiled: April 8, 2008Publication date: September 11, 2008Inventors: Gregory M. Ross, Igor L. Shamovsky, Sandra Marone, Donald F. Weaver, Richard J. Riopelle
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Publication number: 20080152704Abstract: Provided are solid oral dosage forms of palonosetron hydrochloride, methods of using the dosage forms to treat emesis, and methods of making the dosage forms. The dosage forms have improved stability and bioavailability, and are preferably in the form of liquid filled capsules.Type: ApplicationFiled: October 24, 2007Publication date: June 26, 2008Inventors: Daniele Bonadeo, Giorgio Calderari, Enrico Braglia, Riccardo Braglia
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Publication number: 20080058367Abstract: The present application relates to a process for purification of palonosetron or its salt substantially free of its R-isomer and structure related impurities.Type: ApplicationFiled: August 28, 2007Publication date: March 6, 2008Inventors: Raghavendracharyulu Venkata Palle, Madhavrao Marathe Anant, Nageshwar Gunda