Polycyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 514/393)
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Publication number: 20100093733Abstract: Compounds of formula (I): or pharmaceutically acceptable salts and esters thereof, are useful for the treatment of obesity, type II diabetes and the metabolic syndrome.Type: ApplicationFiled: February 15, 2008Publication date: April 15, 2010Applicant: PROSIDION LIMITEDInventors: Oscar Barba, Graham Dawson, William Gattrell, Martin James Procter, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Philippe Wong-Kai-In
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Publication number: 20100087499Abstract: The present invention provides formulations, kits and methods useful for treating cell proliferative disorder. In particular, the formulations, kits and methods include temozolomide (TMZ) in combination with a multi-targeted kinase inhibitor.Type: ApplicationFiled: January 28, 2008Publication date: April 8, 2010Applicant: SCHERING CORPORATIONInventors: Yaolin Wang, Ming Liu, Walter Robert Bishop
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Patent number: 7691635Abstract: The present invention relates to a temperature-stable labeling reagent of formula (0): in which: R1 represents H or an alkyl, aryl or substituted aryl group, R2 represents a detectable marker or at least two detectable markers interlinked by at least one multimeric structure, L is a linker arm comprising a linear chain of at least two covalent bonds and n is an integer equal to 0 or 1, R3 and R4 represent, independently of one another: H, NO2, Cl, Br, F, I, R2-(L)n-Y—X—, OR, SR, NR2, R, NHCOR, CONHR, COOR, —CO—NH—(CH2)3—(O—CH2—CH2)3—CH2—NH—R2, —CO—NH—(CH2)3—(O—CH2—CH2)4—CH2—NH—R2 with R=alkyl or aryl, A is a linker arm comprising at least one covalent double bond enabling the conjugation of the diazo function with the aromatic ring and u is an integer between 0 and 2, preferably 0 or 1, —Y—X— represents —CONH—, —NHCO—, —CH2O—, —CH2S—, —Z— represents —NH—, —NHCO—, —CONH— or —O—, m is an integer between 1 and 10, preferably between 1 and 3, and p is an integer between 1 and 10, preferably between 1 and 3Type: GrantFiled: March 24, 2005Date of Patent: April 6, 2010Assignee: BiomerieuxInventors: Ali Laayoun, Eloy Bernal-Mendez
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Publication number: 20100068303Abstract: This invention relates to compositions and methods utilizing a chemotherapeutic drug and 6-bromoindirubin3?-oxime (BIO) for the treatment of cancer, including glioblastoma multiforme. The present invention demonstrates that BIO works synergistically with chemotherapeutic drugs to increase the cytotoxic effects of these drugs in glioma cells.Type: ApplicationFiled: February 25, 2008Publication date: March 18, 2010Applicant: CEDARS-SINAI MEDICAL CENTERInventor: John S. Yu
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Publication number: 20100063121Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt, solvate or ester thereof, wherein U, W, X, L, Y, M, Z, c, d, e, f, g, h, s, t, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.Type: ApplicationFiled: November 17, 2009Publication date: March 11, 2010Inventors: Ulrich Iserloh, Zhaoning Zhu, Andrew Stamford, Johannes H. Voigt
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Publication number: 20100062063Abstract: Provided is a preparation of ramosetron which is stable under irradiation with light. The solid pharmaceutical composition of the present invention can provide a stable preparation by blending a compound absorbing light having a specific wavelength with ramosetron which is unstable, usually under irradiation with light, or a pharmaceutically acceptable salt thereof. Particularly, this technique is useful because it is adaptable to a preparation containing ramosetron or a pharmaceutically acceptable salt thereof at a low content or an orally disintegrating tablet containing ramosetron or a pharmaceutically acceptable salt thereof. Also, the present invention relates to a method for stabilizing a solid pharmaceutical composition of ramosetron or a pharmaceutically acceptable salt thereof, which is characterized by blending a compound having characteristics of absorbing light having a specific wavelength.Type: ApplicationFiled: September 12, 2007Publication date: March 11, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Hiroyuki Umejima, Ippei Kurimoto, Atsushi Kanbayashi, Chieko Mori
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Patent number: 7674831Abstract: The present invention is directed to the use of a compound of Formula I and physiologically acceptable salts thereof wherein G1, G2, G3, R1, R2, R7, R3, R4, and R5 are defined herein. Compounds according to Formula I can be used to enhance a sweet taste produced by a tastant. The invention is also directed to compositions comprising a compound according to the above formula. Other aspects of the invention provide methods, compounds, and compositions for improved food products wherein the food product comprises a compound according to Formula I and a reduced amount of a sweet tastant.Type: GrantFiled: August 22, 2007Date of Patent: March 9, 2010Assignee: Redpoint Bio CorporationInventors: Karnail S. Atwal, Anita B. Atwal, legal representative, Robert W. Bryant, Ivona Bakaj, Roy Kyle Palmer, Rok Cerne
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Publication number: 20100056592Abstract: A prodrug that has a prodrug moiety that degrades into a compound having the general Formula I with R3 being an alcoholic moiety can be useful in therapies for neurodegenerative diseases as well as cancer. Accordingly, the prodrug compounds can have a structure of Formula I, analogs thereof, derivatives thereof, or salts thereof, wherein: A and B are sulfur or oxygen; R1 and R2, in para, meta, or ortho position, are independently halogen, alkyl, alkoxy, haloalkyl, where R1 and R2 independently are straight chain, branched, substituted or unsubstituted; and R3 is a prodrug moiety. As examples, the prodrug can have a structure of any of Formulas I-V, which as shown in the specification.Type: ApplicationFiled: August 10, 2009Publication date: March 4, 2010Inventors: Roger A. Rajewski, Mehmet Tanol, Ingrid Gunda Georg, Michelle P. McIntosh
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Publication number: 20100048657Abstract: Methods and related compositions are disclosed for treating an array of myeloproliferative disorders and hematological malignancies. In particular, treatment methods and compositions for treating chronic myelogenous leukemia are disclosed. The methods and compositions utilize certain casein kinases, and specifically CK2? agents.Type: ApplicationFiled: September 11, 2007Publication date: February 25, 2010Applicant: CLEVELAND STATE UNIVERSITYInventor: Michael Kalafatis
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Patent number: 7662785Abstract: This invention provides novel polydentate selective high affinity ligands (SHALs) that can be used in a variety of applications in a manner analogous to the use of antibodies. SHALs typically comprise a multiplicity of ligands that each bind different region son the target molecule. The ligands are joined directly or through a linker thereby forming a polydentate moiety that typically binds the target molecule with high selectivity and avidity.Type: GrantFiled: February 9, 2005Date of Patent: February 16, 2010Assignees: The Regents of California, Lawrence Livermore National Security, LLCInventors: Sally DeNardo, Gerald DeNardo, Rodney Balhorn
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Publication number: 20100028469Abstract: The present disclosure relates in part to extracts of cranberry (Vaccinium macrocarpon) comprising an enriched amount of certain compounds having anti-infective activity, e.g. antibacterial and/or antifungal activity, e.g. activity against C. albicans. Another aspect of the disclosure relates to combined cranberry and cinnamon extracts. In certain embodiments, these combined extracts have been optimized to control urinary tract infections caused by E. coli, S. aureus and C. albicans. Certain embodiments of the extract are enriched in bioactive compounds that have been shown to inhibit C. albicans adhesion and/or biofilm formation and its growth in vitro. In another aspect of the disclosure, the extracts are enriched in bioactives derived from cranberry and cinnamon that have been shown to inhibit the attachment and the growth of common urinary tract pathogens like E. coli, S. aureus and C. albicans.Type: ApplicationFiled: June 4, 2009Publication date: February 4, 2010Applicant: HerbalScience Group, LLCInventors: Randall S. Alberte, William P. Roschek, JR., Dan Li
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Patent number: 7655672Abstract: Pharmaceutical formulations and methods including an immune response modifier (IRM) compound and an oleic acid component are provided where stability is improved by using oleic acid have low polar impurities such as peroxides.Type: GrantFiled: December 12, 2008Date of Patent: February 2, 2010Assignee: 3M Innovative Properties CompanyInventors: Alexis S. Statham, Robert J. Nelson
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Patent number: 7655683Abstract: The present invention is directed to novel imidazolopyrazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: February 1, 2007Date of Patent: February 2, 2010Assignee: Janssen Pharmaceutica NVInventors: Xuqing Zhang, Zhihua Sui
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Publication number: 20100022547Abstract: One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5?-monophosphate-dehydrogenase over human inosine-5?-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.Type: ApplicationFiled: June 1, 2007Publication date: January 28, 2010Applicants: BRANDEIS UNIVERSITY, UNIVERSITY OF GEORFIA RESEARCH FOUNDATIONInventors: Lizbeth K. Hedstrom, Boris Striepen
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Publication number: 20100021471Abstract: The present invention includes a conjugates comprising a carbon nanotube with at least one covalently attached recognition module, and at least one covalently attached pharmaceutical compound or a precursor of the pharmaceutical compound, wherein the pharmaceutical compound, or precursor of the pharmaceutical compound, is attached to the carbon nanotube by a linker moiety.Type: ApplicationFiled: July 25, 2008Publication date: January 28, 2010Applicant: Brookhaven Science Associates, LLCInventors: Jingyi Chen, Stanislaus S. Wong, Iwao Ojima
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Publication number: 20100022609Abstract: Disclosed are novel crystalline forms of Temozolomide, methods of preparation thereof, medicaments including the novel crystalline forms of Temozolomide, and uses thereof in the treatment of medical conditions.Type: ApplicationFiled: August 12, 2009Publication date: January 28, 2010Applicant: CHEMAGIS LTD.Inventors: Itai Adin, Carmen Iustain
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Publication number: 20100010015Abstract: The patent application relates to new heterocyclic compounds of the general formula (I) in which A, R, R1, R2, U, V, W, X, Y, Z, n and p have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these compounds as medicaments, particularly as aldosterone synthase inhibitors.Type: ApplicationFiled: May 30, 2006Publication date: January 14, 2010Inventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Aleksandar Stojanovic, Christiane Marti, Nathalie Jotterand, Christoph Schumacher, Michael Quirmbach
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Patent number: 7645784Abstract: Compounds of formula I, wherein R1, m, R2, R3, p, n, R5 and R9 are as defined as in the specification, salts, solvates or solvated salts thereof, processes for their preparation, intermediates used in the preparation thereof, pharmaceutical formulations containing said compounds and the use of said compounds in therapy.Type: GrantFiled: May 13, 2004Date of Patent: January 12, 2010Assignee: AstraZeneca ABInventors: Yevgeni Besidski, Inger Kers, Martin Nylöf, Didier Rotticci, Andis Slaitas, Mats Svensson
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Patent number: 7642258Abstract: Disclosed are pharmaceutical compositions comprising brimondine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.Type: GrantFiled: August 24, 2007Date of Patent: January 5, 2010Assignee: Allergan, Inc.Inventors: Chin-Ming Chang, Gary J. Beck, Cynthia C. Pratt, Amy L. Batoosingh
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Publication number: 20090326028Abstract: A process for the preparation of compounds of formula IA, where R?CH3 (i.e. temozolomide): comprising diazotizing a compound of the formula IIA: where in R is as defined above in the presence of at least one metal halide, an acid and a source of nitrous acid, followed by conversion of acidic solution containing temozolomide. The conversion can be carried out by a liquid-liquid extraction technique in a water immiscible solvent. The temozolomide may be further purified in an acetone-water mixture.Type: ApplicationFiled: September 28, 2007Publication date: December 31, 2009Applicant: CIPLA LIMITEDInventors: Srinivas Laxminarayan Pathi, Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan
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Publication number: 20090318520Abstract: The present invention generally relates to the use of drugs for the treatment of neurobehavioral disorders or symptoms of a neurobehavioral disorder associated with dysfunction of the trimonoamine modulating system (TMMS). More specifically, the invention describes methods for the treatment of a neurobehavioral disorder and/or treatment or prevention of symptoms of a neurobehavioral disorder by administering suitable Isoindole derivatives alone or in combination with other agents so as to provide relatively equal inhibitory effect on serotonin, dopamine and norepinephrine transporters.Type: ApplicationFiled: June 3, 2009Publication date: December 24, 2009Applicant: Afecta Pharmaceuticals DriveInventors: Bruce Kovacs, Laura A. Pinegar
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Publication number: 20090311235Abstract: Methods of enabling or improving the ability of a hydrogel to swell in the stomach of an animal and/or increasing the amount of time said hydrogel remains swollen in the stomach are described herein. In one embodiment, a polymer is administered in combination with one or more pH modifying agents which raise and maintain the pH of the micro environment of the polymer and/or the stomach in order inducing swelling in the polymer. The polymer can be a homopolymer, a copolymer, or a polymer blend or composite. In one embodiment, the polymer is a superabsorbent polymer (“SAP”). The polymers can also be administered with one or more active agents, such as appetite suppressants. The pH modifying agent and/or the active agent can be administered simultaneously with the polymer in the same dosage form, simultaneously with the polymer in separate dosage forms, or sequentially. The compositions are formulated for oral administration.Type: ApplicationFiled: March 13, 2009Publication date: December 17, 2009Inventors: Eric Elenko, Eyal S. Ron, Yishai Zohar
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Patent number: 7625922Abstract: The present invention pertains to certain imidazo[4,5-b]pyridin-2-one and oxazolo[4,5-b]pyridin-2-one compounds and analogs thereof, which, inter alia, inhibit RAF (e.g., B-RAF) activity, inhibit cell proliferation, treat cancer, etc.Type: GrantFiled: October 21, 2005Date of Patent: December 1, 2009Assignees: Cancer Research Technology Limited, The Institute of Cancer Research: Royal Cancer Hospital, Astex Therapeutics LimitedInventors: Dan Niculescu-Duvaz, Caroline Joy Springer, Adrian Liam Gill, Richard David Taylor, Richard Malcol Marais, Harmen Dijkstra, Catherine Gaulon, Delphine Menard, Esteban Roman Vela
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Publication number: 20090291948Abstract: Acyl sulfonamide, peri-substituted, fused bicyclic ring compounds useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed.Type: ApplicationFiled: August 3, 2009Publication date: November 26, 2009Applicant: DECODE GENETICS EHFInventors: Jasbir Singh, Mark E. Gurney, Georgeta Hategan, Peng Yu, David Zembower, Nian Zhou
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Patent number: 7622482Abstract: This invention relates to novel compounds having the formula (I): and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment for cancer.Type: GrantFiled: February 15, 2006Date of Patent: November 24, 2009Assignee: AstraZenecaInventors: Yongxin Han, Michelle Lamb, Peter Mohr, Bin Wang, Tao Wang, Dingwei Yu
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Patent number: 7622497Abstract: The present invention is directed to novel derivatives of gambogic acid and analogs thereof. The present invention also relates to the discovery that novel derivatives of gambogic acid are activators of caspases and inducers of apoptosis. Therefore, the activators of caspases and inducers of apoptosis of this invention can be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.Type: GrantFiled: December 17, 2004Date of Patent: November 24, 2009Assignee: Cytovia, Inc.Inventors: Sui Xiong Cai, Songchun Jiang, Han-Zhong Zhang
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Patent number: 7618992Abstract: The present invention relates to a method of treating cancer by co-administration of an effective amount of 1-(2-methoxyethyl)-2-methyl-4,9-dioxo-3-(pyrazin-2-ylmethyl)-4,9-dihydro-1H-naphtho[2,3-d]imidazol-3-ium bromide and an effective amount of one or more anticancer agents selected from the group consisting of carboplatin, cisplatin, paclitaxel, vinorelbine, gemcitabine, irinotecan, docetaxel, doxorubicin, dacarbazine and rituximab, or a retuximab-containing combination therapy selected from R-ICE and R-DHAP. The treatment method of the present invention is useful for the treatment for all solid tumors and lymphomas, preferably skin cancer, bladder cancer, breast cancer, uterine cancer, ovary cancer, prostate cancer, lung cancer, colon cancer, pancreas cancer, renal cancer, gastric cancer and the like. Particularly, they are expected as therapeutic agents for tumor types which show resistance against existing anticancer agents.Type: GrantFiled: December 27, 2007Date of Patent: November 17, 2009Assignee: Astellas Pharma Inc.Inventors: Takahito Nakahara, Kentaro Yamanaka, Aya Kita, Hiroshi Koutoku
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Patent number: 7618993Abstract: The present invention relates to new compounds or salts, solvates or solvated salts thereof, processes for their preparation and to new intermediates used in the preparation thereof, pharmaceutical compositions containing said compounds and to the use of said compounds in therapy.Type: GrantFiled: December 21, 2006Date of Patent: November 17, 2009Assignee: AstraZeneca ABInventors: Yevgeni Besidski, Martin Nylöf, Inger Kers, Karin Skogholm, Shawn Johnstone, Paul Jones, Denis Labrecque, Andrew Griffin
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Publication number: 20090270473Abstract: The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: April 28, 2009Publication date: October 29, 2009Inventors: Paul Allegretti, Seok-Ki Choi, Roland Gendron, Paul R. Fatheree, Robert Murray McKinnell
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Publication number: 20090270467Abstract: The present invention is directed to novel substituted aminocyclohexanes of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.Type: ApplicationFiled: January 19, 2007Publication date: October 29, 2009Applicant: MERCK & CO., INC.Inventors: Tesfaye Biftu, Jason Cox, Danqing Feng, Anthony Mastracchio, Xiaoxia Qian, Ann E. Weber
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Publication number: 20090270397Abstract: A method of potentiating the efficacy of an antineoplastic agent such as temozolomide, comprises the administration of an antifolate agent as defined herein. Also disclosed are compositions, including pharmaceutical compositions, comprising the antineoplastic agent and an antifolate agent, and the use of such compounds and compositions thereof to treat a variety of cancers, such as melanoma. Unit dosage forms and kits are also contemplated and disclosed.Type: ApplicationFiled: April 8, 2009Publication date: October 29, 2009Inventors: Seth J. Orlow, Ming Chen
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Patent number: 7605145Abstract: Formulations for minimizing damage to at least one of cells, organs and systems within the body of a subject afflicted with Diabetes Mellitus. The invention additionally encompasses methods for minimizing said damage which comprise administering to subjects in need thereof a therapeutic amount of a formulation(s) according to the invention.Type: GrantFiled: November 20, 2007Date of Patent: October 20, 2009Assignee: Premier Micronutrient CorporationInventors: Kedar N. Prasad, William C. Cole, Gerald M. Haase
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Publication number: 20090247598Abstract: There are disclosed methods for treating cancer in a patient in need of such treating comprising administering temozolomide according to improved dosing regimen and/or schedules based on the patient's MGMT level. Additional improved methods for treating patients with temozolomide are also disclosed.Type: ApplicationFiled: February 25, 2009Publication date: October 1, 2009Inventors: CHEN ZONG, Benjamin Winograd
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Publication number: 20090247599Abstract: There are disclosed methods and kits for treating cancer in a patient in need of such treating comprising administering temozolomide according to improved dosing schedules.Type: ApplicationFiled: April 8, 2009Publication date: October 1, 2009Inventors: Walter Robert Bishop, Paul Kirschmeier, Ming Liu
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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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Patent number: 7589070Abstract: A therapeutic delivery system efficiently introduces biologically active molecules to mammalian cells without the use of synthetic polymers or biopolymer coatings. Surface modification of a metal support, such as a medical device, results in a single molecular layer that can fasten various molecules, thereby minimizing any cellular inflammatory response while enhancing biocompatibility.Type: GrantFiled: June 14, 2002Date of Patent: September 15, 2009Assignee: The Children's Hospital of PhiladelphiaInventors: Robert J. Levy, Ivan Alferiev, Cunxian Song, Ilia Fishbein
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Patent number: 7582770Abstract: An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof, as an inhibitor of HCV NS5B polymerase.Type: GrantFiled: February 18, 2005Date of Patent: September 1, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Youla S. Tsantrizos, Catherine Chabot, Pierre Beaulieu, Christian Brochu, Timothy A. Stammers, Bounkham Thavonekham, Jean Rancourt
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Publication number: 20090208422Abstract: Method and composition suitable for administering by direct convective interstitial infusion are disclosed. The method comprises: placing at least one direct convective interstitial infusion catheter in contact with the tissue, and pressuring the composition through the catheter. The composition is in a liquefied form having a viscosity above a predetermined value. The predetermined value is selected so as to improve infusion of the compositions into interstitial volumes of the tissue, while minimizing backflow of the compositions along an outer wall of the catheter or leakage into low resistance paths. It is demonstrated that high viscosity results in higher treatment efficiency.Type: ApplicationFiled: September 29, 2005Publication date: August 20, 2009Applicants: Medical Research Fund of Tel Aviv, Tel HaShomer Medical research Infrastructure and Service LtdInventors: Yael Mardor, Zvi Ram
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Publication number: 20090197909Abstract: The patent application relates to new heterocyclic compounds of the general formula (I) in which R, R1, R2, R3, R4 and n have the definitions elucidated in more detail in the description, to a process for preparing them and to the use of these C compounds as medicaments, particularly as aldosterone synthase inhibitors.Type: ApplicationFiled: December 8, 2006Publication date: August 6, 2009Inventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Michael Quirmbach, Christiane Marti, Aleksandar Stojanovic, Stefan Stutz
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Publication number: 20090186877Abstract: The present invention relates to 1H-benzimidazole-4-carboxamides of formula (I), their preparation, and their use as inhibitors of the enzyme poly(ADP-ribose)polymerase for the preparation of drugs.Type: ApplicationFiled: March 30, 2009Publication date: July 23, 2009Applicant: Abbott LaboratoriesInventors: Vincent L. Giranda, Thomas D. Penning, Virajkumar B. Gandhi, Sheela A. Thomas, Gui-Dong Zhu, Jianchun Gong
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Publication number: 20090176852Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.Type: ApplicationFiled: March 12, 2009Publication date: July 9, 2009Inventors: Sydney Ugwu, Vinay Radhakrishnan, Peter M. Ihnat, Leonore C. Witchey-Lakshmanan
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Publication number: 20090170880Abstract: Provided are Breast Cancer Resistance Protein (BCRP) inhibitors, P-glycoprotein (P-gp) inhibitors and chemotherapeutic agents for use in the treatment of cancer by combination therapy of the BCRP inhibitor and/or P-gp inhibitor with the chemotherapeutic agent. The chemotherapeutic agent is an imidazotetrazine, e.g. temozolomide.Type: ApplicationFiled: August 7, 2008Publication date: July 2, 2009Inventor: Olaf Van Tellingen
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Patent number: 7550602Abstract: Compounds of the general formula: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, and X are as defined. Further provided are methods for treatment of sexual dysfunction, including erectile dysfunction and female sexual dysfunction, and combination drugs and method of use thereof, including a compound of the invention and one or more second sexual dysfunction pharmaceutical agents.Type: GrantFiled: January 14, 2005Date of Patent: June 23, 2009Assignee: Palatin Technologies, Inc.Inventor: Shubh D. Sharma
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Publication number: 20090142332Abstract: The present invention relates to methods of determining colorectal cancer status in a subject. The invention further relates to kits for determining colorectal cancer status in a subject. The invention further related to methods of identifying biomarker for determining colorectal cancer status in a subject.Type: ApplicationFiled: March 22, 2006Publication date: June 4, 2009Applicant: Government of the US, as represented by the Secretary, DHHSInventors: Thomas Ried, Jens Habermann
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Publication number: 20090136593Abstract: The present invention relates to the field of human health, and more particularly to the treatment of attention deficit/hyperactivity disorder (ADHD) with mazindol. The latter can be administered as monotherapy or in combination with one or more compounds, including psychostimulants, for the indication of ADHD and associated or co-morbid symptoms.Type: ApplicationFiled: April 11, 2007Publication date: May 28, 2009Inventor: Eric Konofal
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Publication number: 20090131407Abstract: The invention provides novel kinase inhibitors that are useful as therapeutic agents for example in the treatment malignancies where the compounds have the general formula (I): I wherein X, Y, Z, R1, R2, R3, Ra, Rb, and n are as described herein.Type: ApplicationFiled: December 14, 2006Publication date: May 21, 2009Inventors: Brian Safina, Thomas E. Rawson, Ignacio Aliagas-Martin, Bing-Yan Zhu
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Publication number: 20090118342Abstract: The present invention relates to the synthesis and characterisation of biotinylated analogue of N-arachidonoylethanolamine (AEA) and its use as a tool to study AEA transport and trafficking through biochemical and morphological techniques. In particular biotinylated AEA (b-AEA, for which we propose the common name MM22) is suitable to design highly sensitive and simple methods for the non-radioactive detection and quantitation of AEA from complex samples, which would offer a useful alternative approach to the routinely used radiometric assays. The invention also relates to the use of b-AEA as a potential therapeutic and diagnostic agent.Type: ApplicationFiled: May 2, 2006Publication date: May 7, 2009Applicants: UNIVERSITA' DEGLI STUDI DI ROMA "TOR VERGATA", UNIVERSITA' DEGLI STUDI DI TERAMOInventors: Mauro Maccarrone, Sergio Oddi, Filomena Fezza, Alessandro Finazzi Agro
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Publication number: 20090099024Abstract: The present invention deals with an alternative interfacial polymerization process of microencapsulation, microcapsule's produced thereof, microencapsulated agrochemicals, pharmaceuticals, catalysts and phase transfer materials, and formulations thereof, by means of microcapsules and starting materials with much lower toxicological profile than customary microencapsulation materials, and with the participation of acetylene carbamide derivatives in the final structure of the microcapsules' wall.Type: ApplicationFiled: March 28, 2007Publication date: April 16, 2009Inventors: Victor Casana Giner, Miguel Gimeno Sierra, Barbara Gimeno Sierra
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Patent number: 7517897Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-sulfonic acid which exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: GrantFiled: May 12, 2006Date of Patent: April 14, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Magnus Carl Arne Eriksson, Rene Marc Lemieux
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Publication number: 20090081119Abstract: The invention provides anticancer methods. In one embodiment, the inventive method involves the co-administration to cancerous cells of (a) a chemotherapeutic agent, radiation, or a combination of a chemotherapeutic agent and radiation and (b) an inhibitor of DNA polymerase beta. In another embodiment, the invention provides anticancer methods involving the co-administration to cancerous cells of (a) a chemotherapeutic agent, radiation, or a combination of a chemotherapeutic agent and radiation and (b) an siRNA or shRNA in an amount sufficient to attenuate base excision repair within the cell. Another aspect of the invention relates to pharmaceutical compositions comprising an siRNA or shRNA that attenuates base excision repair.Type: ApplicationFiled: May 19, 2006Publication date: March 26, 2009Applicant: University of Pittsburgh-Of the Commonwealth System of Higher EducationInventor: Robert W. Sobol