Phosphorus Is Part Of A Ring Patents (Class 514/110)
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Publication number: 20130217645Abstract: New uses for phenylketone carboxylate compounds and substituted aromatic compounds of Formula I, Formula I.1, Formula I.2, Formula IA, Formula IB, Formula IC and Formula II and their pharmaceutical acceptable salts for the treatment of cancer. The use of a combination of two of these compounds is described and the use of the combination of one of these compounds with an anticancer agent such as decarbazine, doxorubicin, daunorubicin, cyclophosphamide, busulfex, busulfan, vinblastine, vincristine, bleomycin, etoposide, topotecan, irinotecan, taxotere, taxol, 5-fluorouracil, methotrexate, gemcitabine, cisplatin, carboplatin and chlorambucil.Type: ApplicationFiled: October 26, 2011Publication date: August 22, 2013Applicant: PROMETIC BIOSCIENCES INC.Inventors: Lyne Gagnon, Brigitte Grouix, Lilianne Geerts, Pierre Laurin, Christopher Penney, Boulos Zacharie
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Publication number: 20130209446Abstract: Provided herein are methods of diagnosing and/or treating malignant or pre-malignant conditions in a subject. Overexpression of copy number variant-dependent genes, e.g., genes encoding a cell surface receptor, resulting from copy number changes compared to control is diagnostic of the condition, such as multiple myeloma or monoclonal gammopathy of undetermined significance. Also provided are methods for treating malignant conditions, such as multiple myeloma or a hyperdiploid subtype, with therapeutic agents, with or without other anti-cancer drugs, to downrregulate the overexpressed CNV genes and/or up-regulate the underexpressed genes. Furthermore, methods for lowering drug resistance in multiple myeloma cells via inhibition of platelet activation or thrombin release and for increasing survivability of a multiple myeloma subject via lithibition of PSMD4 gene to increase b-catenin protein expression are provided.Type: ApplicationFiled: July 20, 2011Publication date: August 15, 2013Applicant: Board of Trustees of the University of ArkansasInventors: John D. Shaughnessy, JR., Bart Barlogie, Erming Tian, Yiming Zhou
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Publication number: 20130212720Abstract: The present disclosure is generally related to pulmonary autoantigens. The disclosure provides methods and kits for assessing whether a subject has or is predisposed to interstitial lung disease. Additionally the present disclosure provides methods of treatment and animal models of interstitial lung disease.Type: ApplicationFiled: June 10, 2011Publication date: August 15, 2013Applicant: The Regents of the University of CaliforniaInventors: Mark S. Anderson, Anthony K. Shum
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Publication number: 20130195852Abstract: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.Type: ApplicationFiled: January 22, 2013Publication date: August 1, 2013Applicant: Pharmacyclics, Inc.Inventors: Joseph J. Buggy, Laurence Elias, Gwen Fyfe, Eric Hedrick, David J. Loury, Tarak D. Mody
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Publication number: 20130195848Abstract: The present invention relates to imidazopyrazine compounds of general Formula (I): in which X, R1, R2, R3a, R3b, R4a, R4b, R4C, and R4D are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.Type: ApplicationFiled: March 16, 2011Publication date: August 1, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Ulrich Klar, Marcus Koppitz, Dirk Kosemund, Rolf Bohlmann, Benjamin Bader, Philip Lienau, Gerhard Siemeister, Stefan Prechtl, Duy Nguyen, William Scott
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Publication number: 20130195840Abstract: Processes of diagnosing or treating an autoimmune abnormality are provided whereby the presence of IgA anti-neutrophil cytoplasmic antibodies (ANCA) in a subject are detected correlating with both presence and severity of disease such as Wegener's granulomatosis (WG). The FCAR genotype predicts whether IgA ANCA will be stimulatory or inhibitory of neutrophil activation such that in subjects with an inhibitory genotype, IgA ANCA will act as an inhibitor of disease severity, and in subjects with a proinflammatory genotype, IgA ANCA will increase disease severity as observed by increased prevalence of renal disease in WG. Thus, individualized medical treatment is possible based on determination of the presence of IgA ANCA and FCAR genotype.Type: ApplicationFiled: January 13, 2011Publication date: August 1, 2013Inventors: Robert P. Kimberly, Jeffrey C. Edberg, James M. Kelley
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Publication number: 20130183381Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: ApplicationFiled: January 14, 2013Publication date: July 18, 2013Applicant: Celgene CorporationInventor: JEROME B. ZELDIS
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Publication number: 20130172656Abstract: Novel Uses of an aromatic ester isolated from Armillaria mellea, particularly, armillaridin, are disclosed herein. The armillaridin is useful for manufacturing a medicament or a pharmaceutical composition for suppressing the growth of cancerous cells or for enhancing susceptibility of esophageal cancerous cells to a radiation treatment, in a subject.Type: ApplicationFiled: January 3, 2012Publication date: July 4, 2013Inventors: Yu-Jen Chen, Chien-Chih Chen
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Publication number: 20130171268Abstract: The present invention relates to compositions and methods for prophylactic and/or therapeutic treatment of conditions related to mitochondrial function. In various aspects, the present invention comprises administering one or more compounds selected from the group consisting of epicatechin, an epicatechin derivative, catechin, a catechin derivative, nicorandil, and a nicorandil derivative in an amount effective to ameliorate mitochondrial toxicity caused by administration of a chemical, food, or drug.Type: ApplicationFiled: June 5, 2012Publication date: July 4, 2013Inventors: Francisco Villarreal, Alan Maisel, George Schreiner, Guillermo M. Ceballos Reyes, Pam Taub
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Publication number: 20130172296Abstract: The present invention provides a method of hydroxylating or oxidizing a compound of interest in a subject (e.g., a cytotoxic oxazaphosphorine prodrug), by administering the compound of interest to the subject; and concurrently administering the subject a metalloporphyrin in an amount effective to hydroxylate or oxidize the compound of interest in the subject.Type: ApplicationFiled: February 8, 2013Publication date: July 4, 2013Inventor: Duke University
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Publication number: 20130156756Abstract: The present invention relates to substituted triazolopyridine compounds of general formula (I): in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease of uncontrolled cell growth, proliferation and/or survival as well as to the use of intermediate compounds for the preparation of said compounds.Type: ApplicationFiled: June 14, 2011Publication date: June 20, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Volker Schulze, Dirk Kosemund, Hartmut Schirok, Benjamin Bader, Philip Lienau, Antje Margret Wengner, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Marcus Koppitz, Detlef Stöckigt, Olaf Prien
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Publication number: 20130156727Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.Type: ApplicationFiled: November 21, 2012Publication date: June 20, 2013Applicant: Pharmacyclics, Inc.Inventor: Pharmacyclics, Inc.
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Publication number: 20130156790Abstract: The present invention relates to the fields of genetics, immunology and medicine. The present invention more specifically relates to in vitro or ex vivo methods for determining the susceptibility to a cancer treatment of a subject having a tumour. These methods comprise a step of determining the ability of the treatment, of the subject and/or of the tumour to induce an anticancer immune response, the inability of at least one of the treatment, the subject and the tumor to induce an anticancer immune response being indicative of a resistance of the subject to the therapeutic treatment of cancer. Inventors in particular identify genes specific of a human subject or of cancerous cells which can be used to predict or assess the sensitivity of a subject to a treatment of cancer. The invention also relates to particular compounds capable of activating or enhancing the immune system of a particular subject, when the subject is exposed to a therapeutic treatment of cancer or before such an exposition.Type: ApplicationFiled: February 21, 2013Publication date: June 20, 2013Applicant: INSTITUT GUSTAVE ROUSSYInventor: INSTITUT GUSTAVE ROUSSY
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Publication number: 20130142730Abstract: The present invention provides organic arsenicals. Many of these compounds have potent in vitro cytotoxic activity against numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia.Type: ApplicationFiled: November 14, 2012Publication date: June 6, 2013Applicant: ZIOPHARM ONCOLOGY, INC.Inventor: ZIOPHARM Oncology, Inc.
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Publication number: 20130142758Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: January 17, 2013Publication date: June 6, 2013Applicant: PHARMACYCLICS, INC.Inventor: PHARMACYCLICS, INC.
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Publication number: 20130115192Abstract: This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly(ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization from” approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling to” that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonal” chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.Type: ApplicationFiled: November 2, 2012Publication date: May 9, 2013Applicant: BIND BIOSCIENCES, INCInventor: BIND BIOSCIENCES, INC
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Publication number: 20130108583Abstract: The invention provides methods for treating various conditions using derivatives of cyclopamine having the following formula:Type: ApplicationFiled: May 18, 2012Publication date: May 2, 2013Inventors: Alfredo C. Castro, Michael J. Grogan, William Matsui, Karen J. McGovern, Martin R. Tremblay
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Publication number: 20130109630Abstract: This document features method related to variants in the Inverted Formin 2 (INF2) gene that are susceptibility to focal segmental glomerulosclerosis (FSGS). For example, methods of using such variants for risk assessment and for diagnosing and optimizing treatment of FSGS are provided.Type: ApplicationFiled: December 7, 2010Publication date: May 2, 2013Applicant: THE BRIGHAM AND WOMEN'S HOSPITAL, INC.Inventors: Martin Pollak, Elizabeth J. Brown, Johannes Schlondorff
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Publication number: 20130101680Abstract: The present invention relates to a method of treating pancreatic cancer in a subject in need thereof by administering an effective amount of a composition containing (A) tegafur and (B) gimeracil in conjunction with radiotherapy.Type: ApplicationFiled: December 17, 2012Publication date: April 25, 2013Inventor: Masakazu FUKUSHIMA
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Publication number: 20130095170Abstract: Methods and systems for identifying and treating a patient suspected of having a tumor susceptible to growth inhibition by anti-progestins are provided. The degree of focal distribution of the progesterone receptor can be used to identify tumors susceptible to treatment with anti-progestin therapy.Type: ApplicationFiled: October 4, 2012Publication date: April 18, 2013Inventor: Erard Gilles
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Publication number: 20130078319Abstract: Among other things, the present disclosure provides a method including the steps of: obtaining a uterine sample; and detecting and/or characterizing in the uterine sample an ovarian cancer biomarker (e.g., CA125).Type: ApplicationFiled: September 22, 2012Publication date: March 28, 2013Applicant: Memorial Sloan-Kettering Cancer CenterInventor: Memorial Sloan-Kettering Cancer Center
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Publication number: 20130071323Abstract: The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administering a compound of formula A, wherein R is H, halo, or C1-C6 alkyl; R? is C1-C6 alkyl; or a pharmaceutically acceptable salt thereof; and optionally a pharmaceutically acceptable excipient; and administering at least one additional therapeutic agent.Type: ApplicationFiled: March 9, 2012Publication date: March 21, 2013Applicant: Gilead Calistoga LLCInventors: W. Michael Gallatin, Roger G. Ulrich, Neill A. Giese, Brian Lannutti, Langdon Miller, Thomas M. Jahn
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Publication number: 20130045179Abstract: The present invention provides therapy and methods for the treatment and prevention of diseases of cell proliferation such as cancer, benign tumors, and viral diseases such as HIV-AIDS, hepatitis B, hepatitis C and cirrhosis. The methods of this invention consist of the administration to a patient of a combination of effective amounts of agents capable of eradicating the neoplastic cells, while sparing the non-neoplastic cells from cytotoxic side-effects. The agents co-administered in therapeutically effective amounts are: chemotherapeutic agents, apoptotic agents, anti-angiogenic agents, cell differentiation agents, immunomodulating agents, antioxidants, vitamins, microelements, enzymes and natural extracts.Type: ApplicationFiled: August 15, 2011Publication date: February 21, 2013Inventors: Mihai Ciustea, Ghiorghe Ciustea
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Publication number: 20130039904Abstract: The present invention discloses a gamboge acid cyclization analogs, their preparation methods and applications by semi-synthesis with the following structural formula I-III: Where ring A, ring B or/and ring C is 4-10 membered saturated or/and unsaturated aliphatic ring aliphatic heterocycle or aryl heterocycle. R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11 or/and R12 is, independently at each occurrence, optionally substituted substituent of glycosyl, multi-hydroxyl, amino acid, acyloxy, phosphoric acid oxy, sulfonyloxy, alkoxy, aryloxy, heterocyclic oxy, thiol, aliphatic or cyclic group containing oxygen, sulfur, nitrogen or phosphorus, one of the substituents or combinations thereof. The present invention has antitumor activity management, antiviral, antibacterial and antifungal activity management, as anti-tumor, anti-viral, immune, antibacterial and antifungal agents, with other known anti-tumor, anti-viral, immune, together with the application of antibacterial and antifungal.Type: ApplicationFiled: August 2, 2010Publication date: February 14, 2013Applicant: Liaoning Lifeng Scientific & Technology Development Company Ltd.Inventor: Lifeng Xu
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Publication number: 20130039906Abstract: Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: August 10, 2012Publication date: February 14, 2013Inventors: Steven Do, Huiyong Hu, Aleksandr Kolesnikov, Wendy Lee, Vickie H. Tsui, Xiaojing Wang, Zhaoyang Wen
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Publication number: 20130028989Abstract: Targeting uncontrolled cell proliferation and resistance to DNA damaging chemotherapeutics with at least one reagent has significant potential in cancer treatment. Replication Protein A, the eukaryotic single-strand (ss) DNA binding protein, is essential for genomic maintenance and stability via roles in both DNA replication and repair. Reported herein are small molecules that inhibits the in vitro, in vivo, and cellular ssDNA binding activity of RPA, thereby disrupting the eukaryotic cell cycle, inducing cytotoxicity and increasing the efficacy of chemotherapeutic agents damage DNA, and/or disrupt its replication and/or function. These results provide new insights into the mechanism of RPA-ssDNA interactions in chromosome maintenance and stability. This represents a molecularly targeted eukaryotic DNA binding inhibitor and demonstrates the utility of targeting a protein-DNA interaction as a means of studying the cell cycle and providing a therapeutic strategy for cancer treatment.Type: ApplicationFiled: February 5, 2011Publication date: January 31, 2013Applicant: INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATIONInventors: John J. Turchi, Sarah Shuck
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Publication number: 20130017196Abstract: The present invention relates to new substituted imidazole compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds.Type: ApplicationFiled: September 13, 2012Publication date: January 17, 2013Inventors: Weibo Wang, Paul A. Barsanti, Yia Xia, Rustum Boyce, Sabina Pecchi, Nathan Brammeier, Megan C. Phillips, Kris Mendenhall, Kelly Wayman, Liana Marie Lagnition, Ryan Constantine, Hong Yang, Elizabeth Mieuli, Savithri Ramurthy, Elisa Jazan, Anu Sharma, Rama Jain, Sharadha Subramanian, Paul A. Renhowe, Kenneth W. Bair, David Duhl, Annette Walter, Tinya Abrams, Kay Huh, Eric Martin, Mark Knapp, Vincent P. Le
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Publication number: 20130011496Abstract: A cancer testis antigen biomarker useful to determine whether a non- small cell lung cancer tumor is likely to respond to neoadjuvant chemotherapy is provided. Methods of using the biomarker in the diagnosis, treatment and prognosis of non-small cell lung cancer also are provided.Type: ApplicationFiled: November 23, 2010Publication date: January 10, 2013Applicant: Ludwig Institute for Cancer Research Ltd.Inventors: Jonathan S. Cebon, Arun Azad, Sid Deb
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Publication number: 20130011365Abstract: The present invention relates to tetraaza phenalen-3-one compounds which inhibit poly (ADP-ribose) polymerase (PARP) and are useful in the chemosensitization of cancer therapeutics. The induction of peripheral neuropathy is a common side-effect of many of the conventional and newer chemotherapies. The present invention further provides means to reliably prevent or cure chemotherapy-induced neuropathy. The invention also relates to the use of the disclosed PARP inhibitor compounds in enhancing the efficacy of chemotherapeutic agents such as temozolomide. The invention also relates to the use of the disclosed PARP inhibitor compounds to radio sensitize tumor cells to ionizing radiation. The invention also relates to the use of the disclosed PARP inhibitor compounds for treatment of cancers with DNA repair defects.Type: ApplicationFiled: June 19, 2012Publication date: January 10, 2013Applicant: EISAI INC.Inventors: Weizheng XU, Greg Delahanty, Ling Wei, Jie Zhang
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Publication number: 20130012465Abstract: The present invention relates to a method of treating patients suffering from triple negative breast cancer comprising administration of an effective amount of the irreversible EGFR/HER1 and HER2 inhibitor BIBW 2992 (1) to a person in need of such treatment, optionally in combination with the administration of a further chemotherapeutic agent (2), in combination with radiotherapy, radio-immunotherapy and/or tumour resection by surgery.Type: ApplicationFiled: December 6, 2010Publication date: January 10, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Christian Haslinger, Flavio Solca, Martina Uttenreuther-Fischer
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Publication number: 20130004482Abstract: The application describes methods for screening subjects with breast cancer to determine if the breast cancer will be responsive to a breast cancer therapy including an anthracycline. The application also describes methods for treating subjects with breast cancer by screening them for the likelihood of the effectiveness of treating the cancer with a therapy including anthracycline and administering the therapy in subjects when it is found that anthracycline is likely to be effective.Type: ApplicationFiled: March 15, 2012Publication date: January 3, 2013Applicants: The University of North Carolina at Chapel Hill, British Columbia Cancer Agency Branch, University of Utah Research Foundation, Washington UniversityInventors: Charles M. Perou, Matthew J. Ellis, Philip S. Bernard, Torsten O. Nielsen
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Publication number: 20120328611Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors: Formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis proliferative of diseases, as well as to intermediate compounds useful in the preparation of said compounds.Type: ApplicationFiled: November 17, 2010Publication date: December 27, 2012Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Volker Schulze, Marcus Koppitz, Dirk Kosemund, Benjamin Bader, Philip Lienau, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Antje Margret Wengner
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Publication number: 20120328610Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors: Formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis proliferative of diseases, as well as to intermediate compounds useful in the preparation of said compounds.Type: ApplicationFiled: November 17, 2010Publication date: December 27, 2012Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Volker Schulze, Marcus Koppitz, Dirk Kosemund, Hartmut Schirok, Benjamin Bader, Philip Lienau, Antje Margret Wengner, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Ulf Bömer
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Publication number: 20120322768Abstract: Provided are compounds, compositions and methods for treating protozoan infections.Type: ApplicationFiled: November 24, 2010Publication date: December 20, 2012Applicants: QUEEN MARY & WESTFIELD COLLEGE, RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Longqin Hu, Shane R. Wilkinson, Xinghua Wu, Belinda S. Hall
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Publication number: 20120315247Abstract: The present invention provides novel compounds useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: August 17, 2012Publication date: December 13, 2012Applicants: SUNSHINE LAKE PHARMA CO., LTD.Inventor: Ning Xi
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Publication number: 20120316139Abstract: Compounds of the general formula are disclosed with activity towards treating diseases related to inflammation, such as cancer, neurodegenerative and cardiovascular diseases. Pharmaceutical compositions and methods of use are also disclosed.Type: ApplicationFiled: July 27, 2012Publication date: December 13, 2012Inventor: Basil RIGAS
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Publication number: 20120294957Abstract: Disclosed are methods of treating lung cancer by administering to a human in need thereof effective amounts of FTS, or various analogs thereof, or a pharmaceutically acceptable salt thereof, optionally, in combination with a chemotherapeutic agent. Chemotherapeutic agents, and combinations thereof, for use with FTS, its analogs, or its salts are also disclosed.Type: ApplicationFiled: July 27, 2012Publication date: November 22, 2012Applicant: RAMOT AT TEL-AVIV UNIVERSITY LTD.Inventors: Yoel Kloog, Adi Zundelevich, Roni Haklai
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Publication number: 20120288501Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: July 24, 2012Publication date: November 15, 2012Applicant: Novartis Vaccines and Diagnostics, Inc. formerly known as Chiron CorporationInventors: Payman Amiri, Wendy Fantl, Barry Haskell Levine, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Sharadha Subramanian, Leonard Sung
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Publication number: 20120288554Abstract: Provided herein are methods for treating multiple myeloma by administering canfosfamide or a pharmaceutically acceptable salt thereof as a monotherapy, and also by administering canfosfamide or a pharmaceutically acceptable salt thereof as part of novel combination therapies further comprising one or more of bortezomib, lenalidomide, vorinostat, carfilzomib, pomalidomide, and elotuzumab.Type: ApplicationFiled: May 12, 2011Publication date: November 15, 2012Inventor: Gail L. Brown
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Patent number: 8309537Abstract: Disclosed herein are compositions and methods for treating colitis and other inflammatory bowel diseases, inter alia, indeterminate colitis, Crohn's disease, irritable bowel syndrome and ischemic colitis.Type: GrantFiled: November 5, 2010Date of Patent: November 13, 2012Assignee: Aerpio Therapeutics Inc.Inventors: Joseph H. Gardner, Robert Shalwitz
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Publication number: 20120282172Abstract: The present invention provides a system presenting site-specific accumulation through a ligand that specifically targets a receptor overexpressed on the surface of specific cells within a target organ, like, for example, tumor cells and/or vascular cells of tumor blood vessels. Moreover, this invention provides a method where, upon internalization of the previous-mentioned system by the target cells, triggered release at a high rate of the associated agent takes place, permitting efficient intracellular delivery and, thus, increased concentration of the transported cargo at the target site. Overall, this invention provides a method for the diagnosis, prevention and treatment of human diseases and disorders.Type: ApplicationFiled: May 9, 2012Publication date: November 8, 2012Applicants: Centro de Neurociencias e Biologia Celular, Universidade de CoimbraInventors: João Nuno Sereno de Almeida Moreira, Vera Lúcia Dantas Nunes Caldeira de Moura, Sérgio Paulo de Magalhães Simões, Maria da Conceição Monteiro Pedroso de Lima
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Publication number: 20120270842Abstract: The invention pertains to use of DGAT-1 inhibitors to treat and/or prevent overweight, obesity and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease. Compounds and compositions suitable for use in the disclosed methods are also provided.Type: ApplicationFiled: April 27, 2012Publication date: October 25, 2012Applicant: Metabasis Therapeutics, Inc.Inventors: K. RAJA REDDY, Jeff Stebbins, Serge H. Boyer, Mark D. Erion, Scott J. Hecker, Nicholas Brian Raffaele, Brett C. Bookser, Venkat Reddy Mali
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Publication number: 20120264698Abstract: Dopamine reuptake inhibitors, and their analogs, are disclosed for treating and delaying the progression of autoimmune diseases.Type: ApplicationFiled: October 5, 2011Publication date: October 18, 2012Inventors: Hao Chen, Alexel Miagkov, Lisa Leary, Ming Liu, Qi Su
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Publication number: 20120263708Abstract: The present invention relates to substituted aminoquinoxaline compounds of general formula (I) in which (II), R2, R3, R4, R6, R7, n and m are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.Type: ApplicationFiled: August 24, 2010Publication date: October 18, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Benjamin Bader, Ulf Bömer, Stuart Ince, Marcus Koppitz, Philip Lienau, Tobias Marquardt, Duy Nguyen, Stefan Prechtl, Gerhard Siemeister, Christof Wegscheid-Gerlach
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Publication number: 20120258080Abstract: The present invention provides new pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.Type: ApplicationFiled: April 4, 2012Publication date: October 11, 2012Applicant: AETERNA ZENTARIS GmbHInventors: Matthias GERLACH, Irene SEIPELT, Lars BLUMENSTEIN, Gilbert MUELLER, Eckhard GUENTHER, Tilmann SCHUSTER, Michael TEIFEL
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Publication number: 20120259151Abstract: The present invention provides new pyridopyrazine compounds which are suitable for the treatment or prevention of physiological and/or pathophysiological states mediated and/or modulated by signal transduction pathways and/or enzymes in mammals and in particular in humans.Type: ApplicationFiled: April 4, 2012Publication date: October 11, 2012Applicant: AETERNA ZENTARIS GmbHInventors: Matthias GERLACH, Irene Seipelt, Lars Blumenstein, Gilbert Mueller, Eckhard Guenther, Tilmann Schuster, Michael Teifel
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Publication number: 20120252740Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.Type: ApplicationFiled: July 2, 2010Publication date: October 4, 2012Inventors: Alan Kozikowski, Kyle V. Butler, Jay H. Kalin
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Publication number: 20120251496Abstract: Ezatiostat is useful for inhibiting multiple myeloma cell proliferation and treating multiple myeloma, alone or when added together with another anti-myeloma drug.Type: ApplicationFiled: March 20, 2012Publication date: October 4, 2012Inventor: Michael M. Wick
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Publication number: 20120244214Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: ApplicationFiled: June 5, 2012Publication date: September 27, 2012Inventor: Jerome B. Zeldis
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Publication number: 20120244110Abstract: Compounds of Formula I are useful inhibitors of CDK 4, CDK6, and FLT3. Such compounds are useful in treating cancer and various other disease conditions. Compounds of Formula I have the following structure: where R1 is a group of Formula IA, Formula IB, Formula IC, or Formula ID and the definitions of the other variables are provided herein.Type: ApplicationFiled: March 21, 2012Publication date: September 27, 2012Applicant: Amgen Inc.Inventors: Xiaoqi Chen, Kang Dai, Jason Duquette, Michael W. Gribble, JR., Justin N. Huard, Kathleen S. Keegan, Zhihong Li, Sarah E. Lively, Lawrence R. McGee, Mark L. Ragains, Xianghong Wang, Margaret F. Weidner, Jian Zhang