Acyclic C-n=n-n Containing Patents (Class 514/151)
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Publication number: 20120148595Abstract: The present invention relates to GABA-linked anthracycline-lipid conjugates and to methods of using the conjugates to treat cancer. Methods for making the GABA-linked anthracycline lipid conjugates are also provided.Type: ApplicationFiled: March 11, 2010Publication date: June 14, 2012Applicant: Luitpold Pharmaceuticals, Inc.Inventors: Charles S. Swindell, Glenn G. Fegley, Hema M. Sundar, Richard Lawrence
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Patent number: 8198334Abstract: Methods for modulating macrophage proliferation in an individual afflicted with or at risk for an ocular disease such as ARMD are provided. The methods employ a polyamine analog, or salt or protected derivative thereof. Macrophage proliferation has been implicated in a number of serious disorders, including ARMD. The invention also provides methods for aiding diagnosis and monitoring therapy of an ocular disease such as ARMD.Type: GrantFiled: February 22, 2005Date of Patent: June 12, 2012Assignee: Pathologica LLCInventor: Michael McGrath
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Publication number: 20120134959Abstract: The invention relates to pyrimidine compounds of the Formula I: or a pharmaceutically acceptable salt thereof, wherein the constituent variables are as defined herein, compositions comprising the compounds, and methods for making and using the compounds.Type: ApplicationFiled: April 15, 2010Publication date: May 31, 2012Applicant: Wyeth LLCInventors: Kevin Joseph Curran, Joshua Aaron Kaplan, David James Richard, Jeroen Cunera Verheijen, Arie Zask
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Patent number: 8143237Abstract: Selenopheno triazene analogs, their compositions, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, and pharmaceutically acceptable salts and mixtures thereof are useful for the treatment of metastatic malignant melanoma and other cancers. The selenopheno triazene analogs have the general formulae (I) or (II): wherein the substituents R1, R2, R3, R6, and R7 are as described in the specification. Other cancers include which may be treated with these compounds include, but are not limited to, malignant melanoma, leukemia, lymphomas (Hodgkins and non-Hodgkins), sarcomas (Ewing's sarcoma), brain tumors, central nervous system (CNS) metastases, gliomas, carcinomas such as breast cancer, prostate cancer, lung cancer (small cell and non-small cell), colon cancer, pancreatic cancer, Head and Neck cancers and oropharyngeal squamous cell carcinoma.Type: GrantFiled: April 26, 2010Date of Patent: March 27, 2012Assignee: Kasina Laila Innova Pharmaceuticals Private LimitedInventors: Ganga Raju Gokaraju, Sudhakar Kasina, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Venkateswarlu Somepalli, Trimurtulu Golakoti, Kiran Bhupathiraju, Sengupta Krishanu, Venkata Krishna Raju Alluri
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Patent number: 8124650Abstract: Antitumor combinations comprising a taxane and at least one epidophllotoxin for treating neoplastic diseases are described.Type: GrantFiled: December 30, 2003Date of Patent: February 28, 2012Assignee: Aventis Pharma S.A.Inventor: Marie-Christine Bissery
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Publication number: 20120045519Abstract: Methods for treating melanoma in a subject in need thereof are disclosed. The method comprises administering to the subject a composition comprising a therapeutically effective amount of deoxyelephantopin or an analogue thereof; and a pharmaceutically acceptable carrier. Methods of inhibiting proliferation, migration and/or metastasis of melanoma cells in a subject in need thereof are also disclosed. Also disclosed are methods for reducing side effects of an anti-cancer agent in a subject in need thereof.Type: ApplicationFiled: August 19, 2011Publication date: February 23, 2012Applicant: Academia SinicaInventors: Lie-Fen SHYUR, Wen-Wan Chao, Ya-Wen Cheng
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Publication number: 20120028927Abstract: The present invention relates to novel triazene compounds, to a process for their preparation, to pharmaceutical compositions comprising them, and to the use thereof in the treatment of cancer diseases in humans. The novel triazene compounds are distinguished, as compared with the known triazene compounds, by improved activity while at the same time having reduced toxicity, that is to say by fewer side-effects.Type: ApplicationFiled: August 9, 2011Publication date: February 2, 2012Applicant: TRIN THERAPEUTICS GMBHInventors: Rudolf Reiter, Jochen Kalbe, Heinz Forster
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Publication number: 20120027846Abstract: Methods of using azide-modified biomolecules, such as fatty acids, carbohydrates and lipids, to treat a plant, an insect or an animal infected with a virus or to inhibit infectivity of a virus, such as the human immunodeficiency virus, are provided. Also provided are methods of labeling a virus, such as human immunodeficiency virus, with an azide-modified biomolecule, such as a fatty acid, a carbohydrate, or an isoprenoid lipid. Also, provided are methods of tracking a virus in vivo, with an azide-modified biomolecule, such as a fatty acid, a carbohydrate, or an isoprenoid lipid. The azide-modified biomolecules may be combined with a pharmaceutically acceptable excipient to produce a pharmaceutical composition, optionally containing another anti-viral agent and/or a delivery agent, such as a liposome.Type: ApplicationFiled: July 28, 2011Publication date: February 2, 2012Applicant: LIFE TECHNOLOGIES CORPORATIONInventors: Brian AGNEW, David GRAHAM, Upinder SINGH, Scott GRECIAN
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Patent number: 8101652Abstract: Antitumor combinations comprising a taxane and at least one antimetabolite for treating neoplastic diseases are described.Type: GrantFiled: December 30, 2003Date of Patent: January 24, 2012Assignee: Aventis Pharma S.A.Inventor: Marie-Christine Bissery
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Publication number: 20110305632Abstract: The present invention relates to a method of making asymmetrical bis(thiosemicarbazones), compounds useful as synthetic intermediates in the method, new bis(thiosemicarbazones) that can be readily accessed by use of the method and methods of treatment and imaging utilising some of the new bis(thiosemicarbazones).Type: ApplicationFiled: December 11, 2009Publication date: December 15, 2011Applicant: THE UNIVERSITY OF MELBOURNEInventors: Paul Stephen Donnelly, Brett Michael Paterson
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RADIOISOTOPE-LABELED LYSINE AND ORNITHINE DERIVATIVES, THEIR USE AND PROCESSES FOR THEIR PREPARATION
Publication number: 20110250137Abstract: The invention relates to the compounds suitable for radiolabeling with a chelator free radioisotope and radiolabeled compounds of the general Formula I. Said compounds are ornithine or lysine derivatives.Type: ApplicationFiled: November 26, 2009Publication date: October 13, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLCHAFTInventors: Norman Koglin, Lutz Lehmann, Holger Siebeneicher, Andre Müller, Niels Böhnke -
Publication number: 20110217331Abstract: Azido-diarylpyrimidine (azido-DAPY) compounds, and compositions containing such compounds, are provided. In addition, methods of using azido-diarylpyrimidines to inactivate reverse transcriptases, prepare inactivated viruses, and treat or prevent viral infections are also provided.Type: ApplicationFiled: March 5, 2010Publication date: September 8, 2011Inventor: Adan Rios
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Publication number: 20110206739Abstract: The disclosure relates to compositions and methods of forming nanoemulsions, e.g., containing an active component, in combination with lipophilic components such as oils, hydrophilic components such as water, and one or more surfactants capable of causing a temperature-dependent phase inversion, such as a nonionic polyethoxylated surfactant. Nanoemulsions containing the active component can be produced having average oil droplet sizes of less than 100 nm, 50 nm, or 25 nm without the need for high energy emulsion forming methods (such as microfluidization) by combining the surfactant and the oil in specified weight ratios (e.g., at least 3:1) prior to forming the nanoemulsion.Type: ApplicationFiled: March 30, 2009Publication date: August 25, 2011Applicant: UNIVERSITY OF MASSACHUSETTSInventors: Robert J. Nicolosi, Fonghsu Kuo, SriKanth Kakumanu, Shawn Konecni, Carl W. Lawton
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Publication number: 20110189305Abstract: An immunomodulatory compound is administered to treat, prevent, inhibit, or reduce lung cancer in a subject.Type: ApplicationFiled: August 21, 2008Publication date: August 4, 2011Inventor: Cynthia W. Tuthill
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Publication number: 20110150831Abstract: The present invention relates to kinase modulators of the naphthyridine type and to the preparation and use thereof as medicaments for the modulation of misdirected cellular signal transduction processes, in particular for influencing the function of tyrosine and serine/threonine kinases and for the treatment of malignant or benign tumours and other disorders based on pathological cell proliferation, such as, for example, restenosis, psoriasis, arteriosclerosis and cirrhosis of the liver.Type: ApplicationFiled: November 24, 2010Publication date: June 23, 2011Applicant: AETERNA ZENTARIS GmbHInventors: Tilmann SCHUSTER, Matthias GERLACH, Irene SEIPELT, Emmanuel POLYMEROPOULOS, Gilbert MUELLER, Eckhard GUENTHER, Pascal MARCHAND, Julien DEFAUX
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Publication number: 20110091418Abstract: Methods for treating viral infections using polyamine analogs, including mitoguazone (MGBG), are provided. In these methods, polyamine analogs destroy macrophages that act as viral reservoirs, facilitating the destruction of the viruses that dwell within the macrophages. Examples of viral infections that may be treated with the present methods include, but are not limited to, infections from human immunodeficiency viruses. These methods differ from previous methods of treatment using polyamine analogs, wherein the polyamine analogs were administered only as anti-tumor agents.Type: ApplicationFiled: December 21, 2010Publication date: April 21, 2011Applicant: Pathlogica, LLCInventors: Michael S. McGrath, Kenneth G. Hadlock
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Publication number: 20110086113Abstract: The invention relates to the use of one or more cannabinoids, particularly THC and/or CBD in combination with a non-cannabinoid chemotherapeutic agent in the manufacture of a medicament for use in the treatment of cancer. In particular the cancer to be treated is a brain tumour, more particularly a glioma, more particularly still a glioblastoma multiforme (GBM). The non-cannabinoid chemotherapeutic agent may be a selective estrogen receptor modulator or an alkylating agent.Type: ApplicationFiled: June 4, 2009Publication date: April 14, 2011Inventors: Guillermo Velasco Diez, Manuel Guzman Pastor, Mar Lorente, Sofia Torres
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Publication number: 20110082116Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: December 14, 2010Publication date: April 7, 2011Applicant: ABBOTT LABORATORIESInventors: William A. Carroll, Michael J. Dart, Teodozyj Kolasa, Tongmei Li, Derek W. Nelson, Meena V. Patel, Sridhar Peddi, Arturo Perez-Medrano, Xueqing Wang
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Publication number: 20110052527Abstract: A compound of general Formula (I) having histone deacetylase (HDAC) and/or CDK inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: November 10, 2010Publication date: March 3, 2011Applicant: Gilead Sciences, Inc.Inventors: Lawrence S. Melvin, JR., Michael Graupe, Chandrasekar Venkataramani
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Publication number: 20100330009Abstract: The present invention relates to derivatives of the 1H-pyrano[4,3-b]benzofuran-1-one structure and their nitrogen analogues which possess powerful antioxidant properties combined with a highly effective UV absorbing functionality in one molecule. These compounds are especially useful in cosmetical and dermatological formulations.Type: ApplicationFiled: February 29, 2008Publication date: December 30, 2010Applicant: CIBA CORPORATIONInventors: Barbara Wagner, Sebastien Mongiat, Bernd Herzog, Werner Baschong, Andreas Buthe, Reinhold Ohrlein
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Publication number: 20100323993Abstract: Methods are provided herein for treatment of myotonic dystrophy and other toxic RNA diseases in a subject. In some examples, the method comprises administration of a compound that binds a nucleotide repeat expansion in a ribonucleic acid molecule, thereby treating the disease. In additional examples, the method comprises administration of a compound that disrupts binding of muscleblind-like proteins to an RNA nucleotide repeat expansion. Compounds for use in the disclosed method include pentamidine or heptamidine or derivatives thereof. Representative compounds are described herein.Type: ApplicationFiled: February 20, 2009Publication date: December 23, 2010Inventors: John Andrew Berglund, Bryan M. Warf, Catherine Matthys, Michael M. Haley, Cameron L. Hilton
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Publication number: 20100310500Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: June 7, 2010Publication date: December 9, 2010Applicant: Gilead Sciences, Inc.Inventors: Michael Graupe, Chandrasekar Venkataramani
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Publication number: 20100291025Abstract: The present invention relates to new indazole inhibitors of tyrosine kinase activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: April 13, 2010Publication date: November 18, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Tadimeti Rao, Chengzhi Zhang
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Publication number: 20100292192Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is selected from the group consisting of and 2) —C(R1H)OC(O)X((CR12R13)—(CHR10)m—(CH2)n—Zp—(CH2)q—(CHR11)r—(CR16R17))—R5; Z is —O— or —(CR14R15)_; m, n, p, q, and r are independently selected from the group consisting of 0 and 1; X is —O— or —(CR18R19)—; R1 is selected from the group consisting of hydrogen, C1-4 alkyl, aryl and C1-4 alkylaryl; R5 is —O—N?N(O)—NR3R4; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: ApplicationFiled: January 8, 2009Publication date: November 18, 2010Inventors: Amjad Ali, Michael Man-Chu Lo, Christopher Franklin, Brent R. Whitehead
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Publication number: 20100272678Abstract: Selenopheno triazene analogs, their compositions, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, and pharmaceutically acceptable salts and mixtures thereof are useful for the treatment of metastatic malignant melanoma and other cancers. The selenopheno triazene analogs have the general formulae (I) or (II): wherein the substituents R1, R2, R3, R6, and R7 are as described in the specification. Other cancers include which may be treated with these compounds include, but are not limited to, malignant melanoma, leukemia, lymphomas (Hodgkins and non-Hodgkins), sarcomas (Ewing's sarcoma), brain tumors, central nervous system (CNS) metastases, gliomas, carcinomas such as breast cancer, prostate cancer, lung cancer (small cell and non-small cell), colon cancer, pancreatic cancer, Head and Neck cancers and oropharyngeal squamous cell carcinoma.Type: ApplicationFiled: April 26, 2010Publication date: October 28, 2010Applicant: KASINA LAILA INNOVA PHARMACEUTICALS PRIVATE LIMITEInventors: Ganga Raju GOKARAJU, Sudhakar Kasina, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Venkateswarlu Somepalli, Trimurtulu Golakoti, Kiran Bhupathiraju, Sengupta Krishanu, Venkata Krishna Raju Alluri
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Publication number: 20100266540Abstract: Compositions, methods, and combination therapies for the treatment of cancers, including lymphomas, leukemias, melanomas, lung cancer, and metastatic disease, are provided. Specifically, compositions comprising ligands to Pgrmc1 are disclosed for use in treating and inhibiting tumor growth and progression and inhibition of metastases. The compositions and methods using these ligands can be used alone or in combination with other reagents and cancer treatment modalities.Type: ApplicationFiled: April 20, 2010Publication date: October 21, 2010Applicant: University of Kentucky Research FoundationInventor: Rolf Joseph CRAVEN
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Publication number: 20100266674Abstract: The main drawback in the use of most nucleoside anticancer agents originates from their hydrophilic nature, of which property requires a high and frequent dosage for an intravenous administration. Unlike other nucleoside anti-tumor agents, troxacitabine appears to predominantly enter tumor cells by passive diffusion rather then by using nucleoside transporters, although this may be model dependent. Accordingly, in the present work, a small library of twenty troxacitabine prodrugs has been synthesized using a parallel approach in order to evaluate the relationship between the lipophilicity of the prodrugs and their antitumor activity. Biological evaluation of the prodrugs on two non-small cell lung cancer cell lines (A549 and SW1573) and in pancreatic cell lines clearly showed better antitumor activity than that of troxacitabine, with IC50 values in the nanomolar range.Type: ApplicationFiled: August 30, 2007Publication date: October 21, 2010Applicant: UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.Inventor: David C.K. Chu
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Patent number: 7812058Abstract: The present invention provides a method for treating cancer in a mammal comprising contacting the cancer cells with a compound which is a apogossypol, derivative.Type: GrantFiled: June 25, 2004Date of Patent: October 12, 2010Assignee: The Burnham InstituteInventors: John C. Reed, Maurizio Pellecchia
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Patent number: 7807683Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: March 31, 2006Date of Patent: October 5, 2010Assignee: Schering CorporationInventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Alan Mallams, Carmen S. Alvarez, Kartik M. Keertikar, Jocelyn Rivera, Tin Yau Chan, Vincent Madison, Thierry O. Fischmann, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park, Vidyadhar M. Paradkar, Douglas Walsh Hobbs
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Publication number: 20100247433Abstract: The invention provides methods, reagents and systems to preferentially mark fast-proliferating cells/tissues (such as cancer), by incorporating non-natural amino acids into proteins, preferably in vivo, using the endogenous protein synthesis machinery of an organism. The incorporated non-natural amino acids contain reactive groups for further chemical reagents, which may serve as a “handle” to for a number of uses, such as imaging of cancer cells, targeting drugs to preferentially kill cancer cells, and proteomic analysis in the context of large scale or high throughput screening for candidate drug leads that affects the proliferation of a target cell, etc.Type: ApplicationFiled: October 16, 2006Publication date: September 30, 2010Applicant: California Institute of TechnologyInventors: David Tirrell, Daniela C. Dieterich, Aaron J. Link, Erin Schuman
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Publication number: 20100249075Abstract: The present invention relates to novel tetralin ER-? agonist compounds, pharmaceutical compositions thereof, and use of these compounds to treat a ER-? mediated disease such as nocturia, obstructive uropathy, benign prostatic hypertrophy, obesity, dementia, hypertension, incontinence, colon cancer, prostate cancer, infertility, depression, leukemia, inflammatory bowel disease, and arthritis.Type: ApplicationFiled: February 10, 2006Publication date: September 30, 2010Applicant: ELI LILLY AND COMPANYInventors: Venkatesh Krishnan, Julian Stanley Kroin, Bryan Hurst Norman, Elizabeth Marie Thomas
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Publication number: 20100215748Abstract: A bioadherent substrate includes a medical gel or medical gel precursor having a plurality of reactive members of a specific binding pair attached on or adapted to be attached to a surface of the medical gel, said reactive members being capable of forming covalent bonds with a plurality of complementary reactive members of the specific binding pair via a reaction selected from a Huisgen cycloaddition reaction, a Diels-Alder reaction and a thiol-ene reaction.Type: ApplicationFiled: February 19, 2010Publication date: August 26, 2010Inventors: Sebastien Ladet, Philippe Gravagna
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Publication number: 20100217287Abstract: A method for in situ formation of a medical device on biological tissue includes attaching a plurality of reactive members of a primary specific binding pair to a surface of the biological tissue, and providing a plurality of fibers having attached thereto a plurality of complementary reactive members of the primary specific binding pair, wherein upon contact of the reactive members on the surface of the biological tissue with the complimentary reactive members on the fibers, covalent bonds are formed between the reactive members and the complementary reactive members, thus adhering the fibers to the tissue. The fibers can incorporate functionalities which may cause them to bind to one another.Type: ApplicationFiled: February 19, 2010Publication date: August 26, 2010Inventors: Sebastien Ladet, Philippe Gravagna
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Publication number: 20100216748Abstract: The invention relates to a series of substituted pyrrole derivatives, compositions comprising the same, and methods of treating conditions and disorders using such compounds and compositions.Type: ApplicationFiled: May 7, 2010Publication date: August 26, 2010Applicant: ABBOTT LABORATORIESInventors: Ramin Faghih, Gregory A. Gfesser, Christopher L. Lynch, Murali Gopalakrishnan, Sujatha Gopalakrishnan, John Malysz, Earl J. Gubbins, Rachid El Kouhen, Jinhe Li
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Publication number: 20100203110Abstract: The present invention relates to methods of treating a cancerous tumor in a subject comprising administering to the subject an effective amount of 3-bromopyruvate. The 3-bromopyruvate may be administered intraarterially directly to a tumor as a continuous intraarterial infusion. The present invention also relates to methods for identifying agents that inhibit type II hexokinase activity.Type: ApplicationFiled: December 17, 2007Publication date: August 12, 2010Applicant: The Johns Hopkins UniversityInventors: Jean-Francois Geschwind, Mustafa Vali
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Publication number: 20100183743Abstract: Inhibitors of poly(ADP-ribose)polymerase having a structure of Formula (I), ways to make them and methods of treating patients using them are disclosed.Type: ApplicationFiled: January 19, 2010Publication date: July 22, 2010Applicant: ABBOTT LABORATORIESInventors: Magdalena K. Przytulinska, Thomas D. Penning, Yunsong Tong
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Publication number: 20100183726Abstract: A uniform microfluidized nanoemulsion is disclosed containing an anti-cancer agent, such as dacarbazine. The microfluidized nanoemulsion improves the combination's cell membrane permeability by at least four-fold over conventional nanoemulsion compositions, which significantly increases the intracellular concentration of anti-cancer agents. As a nanoemulsion, dacarbazine has a greater anti-cancer efficacy than when applied as a free solution.Type: ApplicationFiled: August 2, 2007Publication date: July 22, 2010Inventors: Robert Nicolosi, Jean-Bosco Tagne
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Publication number: 20100179111Abstract: The invention provides compounds of formula I and compositions thereof. The invention further provides methods of using the compounds and compositions. The compounds of the invention can provide high affinity binding to sigma-1 receptors in a mammal. The compounds can exhibit selectivity for the sigma-1 receptor over the sigma-2 receptor. The compounds and compositions of the invention can also be used to treat conditions that involve the sigma-1 receptor, such as addiction, cardiovascular conditions, and cancer, for example, cancer of the breast, lung, prostate, ovarian, colorectal, or the CNS.Type: ApplicationFiled: November 18, 2009Publication date: July 15, 2010Applicant: WARF - Wisconsin Alumni Research FoundationInventors: Arnold E. Ruoho, Abdol R. Hajipour, Uyen B. Chu, Dominique A. Fontanilla
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Publication number: 20100143296Abstract: The present invention relates to new podophyllotoxin inhibitors of topoisomerase II, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: December 10, 2009Publication date: June 10, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventor: Thomas G. Gant
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Publication number: 20100129470Abstract: Disclosed is (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride effective as a cytotoxic agent. (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride is useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and in particular to its use in treating brain cancer.Type: ApplicationFiled: October 8, 2009Publication date: May 27, 2010Applicant: Myriad Pharmaceuticals, IncorporatedInventor: MARK LAUGHLIN
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Patent number: 7723389Abstract: The invention provides pharmaceutical compositions for the treatment or prevention of the toxic effects of therapeutic agents and methods of treating or preventing such toxicity using a toxicity reducing amount of N-acetylcysteine either alone or in combination with a therapeutically effective amount or, to achieve its therapeutic advantages, an amount larger than what is customarily given as a therapeutically effective amount, of a therapeutic agent.Type: GrantFiled: November 4, 2002Date of Patent: May 25, 2010Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Leonard A. Herzenberg, Leonore A. Herzenberg, Stephen C. De Rosa, James Andrus
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Publication number: 20100086518Abstract: Methods of treating melanoma include administering a compound of Structure I, a tautomer of the compound, a pharmaceutically acceptable salt of the compound, a pharmaceutically acceptable salt or the tautomer, or a mixture thereof to a subject. The compound, tautomer, salt of the compound, salt of the tautomer, or mixture thereof may be used to prepare medicaments for treating metastatic cancer. The variable A has the values defined herein.Type: ApplicationFiled: March 7, 2008Publication date: April 8, 2010Applicant: NOVARTIS AGInventors: Carla C. Heise, Paul Hollenbach, Daniel Menezes, Nancy Pryer, Katherine Rendahl, Marion Wiesmann
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Publication number: 20100068178Abstract: The present invention discloses triazene analogs of the general formula (I) and formula (II), their tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, and pharmaceutically acceptable salts thereof for the metastatic malignant melanoma and other cancers including but not limited to lymphomas, sarcomas, carcinomas, and gliomas. The invention further discloses a process for the preparation of the above said triazene analogs of formula (I) and formula (II), and their pharmaceutically acceptable compositions.Type: ApplicationFiled: September 15, 2009Publication date: March 18, 2010Applicant: LAILA NUTRACEUTICALSInventors: Ganga Raju Gokaraju, Sudhakar Kasina, Rama Raju Gokaraju, Trimurtulu Golakoti, Venkateswarlu Somepalli, Sengupta Krishanu, Kiran Bhupathiraju
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Patent number: 7625884Abstract: A method of increasing the bioavailability of balsalazide by administration of an oral dosage form with food is provided, as well as an article of manufacture comprising an oral dosage form of balsalazide in a suitable container and associated with printed labeling which describes the increased bioavailability of the medication in the container when taken with food.Type: GrantFiled: October 23, 2007Date of Patent: December 1, 2009Assignee: Salix Pharmaceuticals, LtdInventor: Lorin Johnson
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Patent number: 7585856Abstract: The present invention is generally drawn to novel isolated therapeutic agents, termed resolvins, generated from the interaction between a dietary omega-3 polyunsaturated fatty acid (PUFA) such as eicosapentaenoic acid (EPA) or docosahexaenoic acid (DHA), cyclooxygenase-II (COX-2) and an analgesic, such as aspirin (ASA). Surprisingly, careful isolation of compounds generated from the combination of components in an appropriate environment provide di- and tri-hydroxy EPA or DHA compounds having unique structural and physiological properties. The present invention therefore provides for many new useful therapeutic di- or tri-hydroxy derivatives of EPA or DHA (resolvins) that diminish, prevent, or eliminate inflammation or PMN migration, for example. The present invention also provides methods of use, methods of preparation, and packaged pharmaceuticals for use as medicaments for the compounds disclosed throughout the specification.Type: GrantFiled: August 12, 2003Date of Patent: September 8, 2009Assignee: The Brigham and Women's Hospital, Inc.Inventor: Charles N. Serhan
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Patent number: 7576072Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X, Y and Z are as defined in the specification. Such compounds are MEK inhibitors and are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.Type: GrantFiled: November 18, 2004Date of Patent: August 18, 2009Assignee: Array BioPharma Inc.Inventors: Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, T. Brian Hurley, Allison L. Marlow, James Blake
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Publication number: 20090143340Abstract: Pyrocatechin derivatives of formula I wherein R illustrates a group of formulae Ia, Ib, Ic or Id R1 is 4-halogen-but-2-enyl, R2 is lower alkyl or cycloalkyl, R3 is lower alkoxy and R4 is lower alkoxy lower alkoxy, or, where R is a group of formula (Ia), it is hydroxy, hydroxy lower alkoxy or a group of formula Ie R5 is reactive esterified hydroxy, R6 is azido and R7 is lower alkyl, lower alkenyl, cycloalkyl or aryl lower alkyl, and their salts, are valuable intermediates in the production of active ingredients for medicaments.Type: ApplicationFiled: July 10, 2006Publication date: June 4, 2009Inventors: Gottfried Sedelmeier, Kurt Nebel, Siem Jacob Veenstra, Janos Zergenyi
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Patent number: 7514442Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: March 31, 2006Date of Patent: April 7, 2009Assignees: Schering Corporation, Pharmacopeia, Inc.Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Carmen S. Alvarez, Tin Yau Chan, Chad Knutson, Vincent Madison, Thierry O. Fischmann, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park
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Patent number: 7494984Abstract: The invention encompasses a series of bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: August 29, 2006Date of Patent: February 24, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Jacques Banville, Roger Remillard, Serge Plamondon
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Patent number: 7470695Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: March 31, 2006Date of Patent: December 30, 2008Assignee: Schering CorporationInventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Ronald J. Doll, Viyyoor M. Girijavallabhan, Lawrence W. Dillard, Vinh D. Tran, Zhen Min He, Ray Anthony James, Haengsoon Park