Ring Nitrogen Is Shared By Two Of The Cyclos Patents (Class 514/294)
-
Patent number: 8748452Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level and the like. That is, the present invention relates to indolizine derivatives represented by the following formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, salts thereof or the like. In the formula, ring U represents aryl or heteroaryl; R1 represents halogen, a hydroxy group or the like; R2 represents halogen, a hydroxy group, alkyl, alkoxy, alkyl substituted by fluorine, alkoxy substituted by fluorine or the like; m represents a number from 0 to 2; n represents a number from 0 to 3; and R3 represents hydrogen, fluorine or the like.Type: GrantFiled: March 30, 2010Date of Patent: June 10, 2014Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Kazuo Shimizu, Masato Iizuka, Yasushi Takigawa
-
Publication number: 20140155369Abstract: An agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that activates a serotonin 5-HT2C receptor, an agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that stimulates an androgen binding site, and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence, which includes electrostimulating the abdominal muscles or a nerve controlling them of an animal to increase the abdominal pressure, and measuring the leak point pressure at that time.Type: ApplicationFiled: January 16, 2014Publication date: June 5, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Izumi KAMO, Tadatoshi HASHIMOTO
-
Patent number: 8722700Abstract: This invention provides CCI-779 cosolvent concentrates which are useful in preparing a parenteral formulation of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) following admixture with a diluent.Type: GrantFiled: May 13, 2013Date of Patent: May 13, 2014Assignee: Wyeth LLCInventors: Joseph T. Rubino, Victoria Siskavich, Maureen M. Harrison, Pooja Gandhi
-
Patent number: 8685960Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).Type: GrantFiled: May 5, 2009Date of Patent: April 1, 2014Assignee: Elexopharm GmbHInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
-
Publication number: 20140073623Abstract: The invention provides tricyclic sulfonamide compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.Type: ApplicationFiled: May 7, 2012Publication date: March 13, 2014Applicant: Zafgen, Inc.Inventors: Susan Mary Cramp, Hazel Joan Dyke, Thomas David Pallin, Robert Zahler
-
Publication number: 20140045870Abstract: The present invention relates to 7-(heteroaryl-amino)-6,7,8,9-tetrahydropyrido[1,2-a]indol acetic acid derivatives of the formula (I), wherein R1, R2, R3 and R4 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.Type: ApplicationFiled: April 13, 2012Publication date: February 13, 2014Applicant: Actelion Pharmaceuticals Ltd.Inventors: Hamed Aissaoui, Christoph Boss, Jerome Gabillet, Sylvia Richard-Bildstein, Romain Siegrist
-
Publication number: 20140030249Abstract: The present invention provides for a pharmaceutical composition that includes tetrabenazine and a release-retarding agent; and a method of treating a hyperkinetic movement disorder (e.g., Huntington's disease, chorea associated with Huntington's disease, hemiballismus, senile chorea, tic disorders, tardive dyskinesia, myoclonus, dystonia and/or Tourette's syndrome). The method includes administering an effective amount of the pharmaceutical composition, for a period of time effective to treat the hyperkinetic movement disorder.Type: ApplicationFiled: September 27, 2013Publication date: January 30, 2014Applicant: Valeant International BermudaInventors: Andrew John DUFFIELD, Graham Jackson, Steven E. Frisbee, Okponanabofa Eradiri, John CK Lai
-
Patent number: 8637671Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.Type: GrantFiled: September 17, 2009Date of Patent: January 28, 2014Assignee: Merck Canada Inc.Inventors: John Colucci, Michael Boyd, Mohamed Helmi Zaghdane, Michel Gallant
-
Patent number: 8637541Abstract: The compound (+) {7R-[[(4-fluorophenyl)sulfonyl] (methyl)ammo]-6,7,8,9-tetrahydropyrido[1,2-a]mdol-10-yl}acetic acid and pharmaceutically acceptable salts thereof are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-meidated diseases such as asthma.Type: GrantFiled: September 17, 2009Date of Patent: January 28, 2014Assignee: Merck Canada Inc.Inventor: Zhaoyin Wang
-
Patent number: 8617598Abstract: A pharmaceutical composition comprising a macrolide solid dispersion, a disintegrant and colloidal silicon dioxide, wherein the composition comprises 1 to 5% colloidal silicon dioxide by weight.Type: GrantFiled: June 5, 2012Date of Patent: December 31, 2013Assignee: Novartis AGInventors: Barbara Haeberlin, Andrea Kramer, Silvia Heuerding
-
Publication number: 20130338092Abstract: This invention relates to high-throughput, semi-automated methods for identifying compounds that are effective in targeting leukemia stem cells, as well as compounds identified by those methods and uses thereof for treating leukemia.Type: ApplicationFiled: August 16, 2013Publication date: December 19, 2013Inventors: Kimberly Hartwell, Malcolm A.S. Moore, David T. Scadden, Stuart L. Schreiber, Todd R. Golub, Benito Munoz, Benjamin L. Ebert, Andrew M. Stern, Peter G. Miller, D. Gary Gilliland, Anne Van Dyk Carpenter, David J. Logan, Joseph Negri, Nicola Tolliday, Alykhan Shamji, Siddhartha Mukherjee, Alison Stewart
-
Patent number: 8609685Abstract: The present invention relates to compounds conformationally constrained mimetics of Smac with function as inhibitors of Inhibitor of Apoptosis Proteins (IAPs), the invention also relates to the use of these compounds in therapy, wherein the induction of apoptotic cell death is beneficial, especially in the treatment of cancer, alone or in combination with other active ingredients.Type: GrantFiled: November 5, 2008Date of Patent: December 17, 2013Assignee: CISI SCRLInventors: Carlo Scolastico, Leonardo Pierpaolo Manzoni, Pierfausto Seneci, Laura Belvisi, Domenico Delia, Martino Bolognesi, Eloise Mastrangelo, Mario De Mayo De Mari Milani, Ilaria Motto, Carmelo Drago
-
Publication number: 20130317056Abstract: This application is directed to a-neuronal nicotinic receptor agonists selective for ?7-subtype that are useful for improving cognition impairment in patients having schizophrenia, a schizophreniform disorder or a related schizophrenia spectrum psychotic disorder. Compounds and compositions containing such compounds, and methods of using such compound and compositions are described herein.Type: ApplicationFiled: March 14, 2013Publication date: November 28, 2013Applicant: AbbVie Inc.Inventors: George M. Haig, Jeffrey F. Waring, Chih-Hung Lee, Deli Wang
-
Publication number: 20130317054Abstract: An embodiment relates to a selective agonist of neuronal nicotinic acetylcholine receptor ?7 subtype, a pharmaceutically suitable salt, prodrug, or a metabolite thereof, for the prevention and treatment of diseases and conditions that are mediated by nicotinic acetylcholine receptors, and methods of use thereof. Another embodiment is a method of administering a pharmaceutically effective amount of a selective agonist of neuronal nicotinic acetylcholine receptor ?7 subtype, or a pharmaceutically suitable salt, prodrug, or a metabolite thereof, to a mammal in need thereof.Type: ApplicationFiled: March 13, 2013Publication date: November 28, 2013Applicant: ABBVIE INC.Inventors: George M. HAIG, Jeffrey D. BAKER, Weining Z. Robieson
-
Publication number: 20130317055Abstract: An embodiment relates to a selective agonist of neuronal nicotinic acetylcholine receptor ?7 subtype, a pharmaceutically suitable salt, prodrug, or a metabolite thereof, for the prevention and treatment of diseases and conditions that are mediated by nicotinic acetylcholine receptors, and methods of use thereof. Another embodiment is a method of administering a pharmaceutically effective amount of a selective agonist of neuronal nicotinic acetylcholine receptor ?7 subtype, a pharmaceutically suitable salt, prodrug, or a metabolite thereof, to a mammal in need thereof.Type: ApplicationFiled: March 13, 2013Publication date: November 28, 2013Applicant: ABBVIE INC.Inventors: George M. HAIG, Jeffrey D. BAKER
-
Publication number: 20130303446Abstract: The invention relates to a pharmaceutical combination comprising the compound of formula I or pharmaceutically acceptable salts thereof in combination with at least one second therapeutic agent 2. The pharmaceutical combination of the invention is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.Type: ApplicationFiled: May 7, 2013Publication date: November 14, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Bradford S. HAMILTON, Thomas RAUCH, Manami TSUTSUMI
-
Patent number: 8580764Abstract: The present invention provides methods of treating a cell proliferative disorder, such as lung cancer and breast cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or a pyrroloquinolinyl-pyrrolidine-2,5-dione compound, such as (?)-trans-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)pyrrolidine-2,5-dione, in combination with a therapeutically effective amount of a second anti-proliferative agent, such as gemcitabine.Type: GrantFiled: July 1, 2011Date of Patent: November 12, 2013Assignee: ArQule, Inc.Inventors: Giovanni Abbadessa, Dennis S. France, Chang-Rung Chen, Thomas C. K. Chan
-
Publication number: 20130296360Abstract: The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: July 3, 2013Publication date: November 7, 2013Inventors: Thomas G. Gant, Manouchehr Shahbaz
-
Patent number: 8575191Abstract: The present invention provides methods of treating non-small cell lung cancer by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound in combination with a therapeutically effective amount of an epidermal growth factor tyrosine kinase inhibitor.Type: GrantFiled: August 31, 2011Date of Patent: November 5, 2013Assignee: ArQule, Inc.Inventors: Yinpu Chen, Edward G. Garmey, Brian Schwartz
-
Patent number: 8568782Abstract: The object of the invention consists of pharmaceutical formulations containing rifaximin in the shape of microgranules made gastroresistant by an insoluble polymer at pH values between 1.5 and 4.0 and soluble at pH values between 5.0 and 7.5, by their preparation and by their use in the manufacture of medicinal preparations useful in the treatment of inflammatory bowel diseases (IBD) and mainly Crohn's disease.Type: GrantFiled: March 6, 2006Date of Patent: October 29, 2013Assignee: Alfa Wassermann S.p.A.Inventors: Giuseppe Claudio Viscomi, Ernesto Palazzini, Villiam Zamboni, Maria Rosaria Pantaleo
-
Patent number: 8563567Abstract: The present invention relates to substituted heterocyclic compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted heterocyclic compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: December 29, 2010Date of Patent: October 22, 2013Assignee: ArQule, Inc.Inventors: Syed M. Ali, Mark A. Ashwell, Yanbin Liu, Magdi Moussa, Jianqiang Wang, Hui Wu
-
Publication number: 20130267552Abstract: This invention relates to novel pharmaceutical compositions comprising a therapeutically effective combination of a dopaminergic stabilizer known as Pridopidine, and an inhibitor of the vesicular monoamine transporter type 2 (VMAT) known as Tetrabenazine. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for improving the symptomatic therapeutic effects, and for reducing the adverse effects, of Tetrabenazine in the treatment of movement disorders, and in particular movement disorders associated with Huntington's disease, Gilles de la Tourette's syndrome, or tardive dyskinesia.Type: ApplicationFiled: April 3, 2013Publication date: October 10, 2013Applicant: IVAX INTERNATIONAL GMBHInventors: Ross Nicholas Waters, Eva Susanna Holm Waters
-
Publication number: 20130267553Abstract: The present invention relates to shelf-stable liquid formulations of palonosetron for reducing chemotherapy and radiotherapy induced emesis with palonosetron. The formulations are particularly useful in the preparation of intravenous and oral liquid medicaments.Type: ApplicationFiled: May 23, 2013Publication date: October 10, 2013Inventors: Giorgio Calderari, Daniele Bonadeo, Roberta Cannella, Alberto Macciocchi, Andrew Miksztal, Thomas Malefyt, Kathleen M. Lee
-
Patent number: 8551522Abstract: A sustained-release formulation is provided comprising a solid dispersion composition comprising a tricyclic compound or a pharmaceutically acceptable salt thereof in a mixture comprising a water-soluble polymer and a water-insoluble polymer, and an excipient.Type: GrantFiled: November 5, 2008Date of Patent: October 8, 2013Assignee: Astellas Pharma Inc.Inventors: Kazunari Yamashita, Eiji Hashimoto, Yukihiro Nomura, Fumio Shimojo, Shigeki Tamura, Takeo Hirose, Satoshi Ueda, Takashi Saitoh, Rinta Ibuki, Toshio Ideno
-
Patent number: 8546423Abstract: Disclosed herein are formulations of fluoroquinolones suitable for aerosolization and use of such formulations for aerosol administration of fluoroquinolone antimicrobials for the treatment of pulmonary bacterial infections. In particular, inhaled levofloxacin specifically formulated and delivered for bacterial infections of the lungs is described. Methods include inhalation protocols and manufacturing procedures for production and use of the compositions described.Type: GrantFiled: October 22, 2009Date of Patent: October 1, 2013Assignee: MPEX Pharmaceuticals, Inc.Inventors: Mark W. Surber, Keith A. Bostian, Michael N. Dudley, Olga Lomovskaya, David C. Griffith
-
Publication number: 20130251647Abstract: The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.Type: ApplicationFiled: September 20, 2012Publication date: September 26, 2013Applicant: BASF SEInventors: Thomas Subkowski, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel, Ralf Pelzer
-
Patent number: 8541404Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and a method of treating of hyperaldosteronism and/or disorders or diseases that are mediated by 11?-hydroxylase (CYP11B1) with these compounds.Type: GrantFiled: November 3, 2010Date of Patent: September 24, 2013Assignee: ElexoPharm GmbHInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
-
Patent number: 8536193Abstract: The instant invention provides for substituted [1,2,4]triazolo[4,3-a]-1,5-naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity, especially Akt1 by administering the compound to a patient in need of treatment of cancer.Type: GrantFiled: May 27, 2009Date of Patent: September 17, 2013Assignees: Merck Sharp & Dohme Corp., MSD K.K.Inventors: Hidetomo Furuyama, Yasuhiro Goto, Nobuhiko Kawanishi, Mark E. Layton, Takashi Mita, Yoshio Ogino, Yu Onozaki, Michael A. Rossi, Toshihiro Sakamoto, Philip E. Sanderson, Jiabing Wang
-
Publication number: 20130231311Abstract: Systems and methods are described for treating un-met medical needs in migraine and related conditions such as cluster headache. Included are treatments that are both rapid onset and long acting, which include sustained release formulations, and combination products. Also included are treatments for multiple symptoms of migraine, especially headache and nausea and vomiting. Systems that are self contained, portable, prefilled, and simple to self administer at the onset of a migraine attack are disclosed, and preferably include a needle-free injector and a high viscosity formulation, to eliminate such issues as fear of self administration with needles, and needle stick and cross contamination.Type: ApplicationFiled: April 16, 2013Publication date: September 5, 2013Inventors: Stephen J. FARR, John TURANIN, Roger HAWLEY, Jeffrey A. SCHUSTER
-
Patent number: 8524735Abstract: Disclosed herein are formulations of fluoroquinolones suitable for aerosolization and use of such formulations for aerosol administration of fluoroquinolone antimicrobials for the treatment of pulmonary bacterial infections. In particular, inhaled levofloxacin specifically formulated and delivered for bacterial infections of the lungs is described. Methods include inhalation protocols and manufacturing procedures for production and use of the compositions described.Type: GrantFiled: October 22, 2009Date of Patent: September 3, 2013Assignee: MPEX Pharmaceuticals, Inc.Inventors: Mark W. Surber, Keith A. Bostian, Michael N. Dudley, Olga Lomovskaya, David C. Griffith
-
Patent number: 8524734Abstract: Disclosed herein are formulations of fluoroquinolones suitable for aerosolization and use of such formulations for aerosol administration of fluoroquinolone antimicrobials for the treatment of pulmonary bacterial infections. In particular, inhaled levofloxacin specifically formulated and delivered for bacterial infections of the lungs is described. Methods include inhalation protocols and manufacturing procedures for production and use of the compositions described.Type: GrantFiled: October 22, 2009Date of Patent: September 3, 2013Assignee: MPEX Pharmaceuticals, Inc.Inventors: Mark W. Surber, Keith A. Bostian, Michael N. Dudley, Olga Lomovskaya, David C. Griffith
-
Patent number: 8524733Abstract: The present invention relates to new benzoquinoline inhibitors of vesicular monoamine transporter 2 (VMAT2), pharmaceutical compositions thereof, and methods of use thereof.Type: GrantFiled: September 18, 2009Date of Patent: September 3, 2013Assignee: Auspex PharmaceuticalsInventors: Thomas G. Gant, Manoucherhr M. Shahbaz
-
Publication number: 20130210806Abstract: The present invention is directed to tricyclic indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.Type: ApplicationFiled: February 14, 2013Publication date: August 15, 2013Applicant: Janssen Pharmaceutica, NVInventor: Janssen Pharmaceutica, NV
-
Patent number: 8507519Abstract: The present invention relates to optically pure S-(?)-benzoquinolizine carboxylic acid, lysine salt and to pharmaceutical compositions comprising the S(?)-benzoquinolizine carboxylic acid, lysine salt.Type: GrantFiled: May 21, 2007Date of Patent: August 13, 2013Assignee: Wockhardt LimitedInventors: Mahesh Vithalbhai Patel, Shivkumar Agarwal, Sreenivas Kandepu
-
Publication number: 20130197026Abstract: The disclosure provides methods of treating glioblastoma, methods of screening for compounds that treat glioblastoma, and pharmaceutical compositions useful the treatment of glioblastoma.Type: ApplicationFiled: August 22, 2011Publication date: August 1, 2013Applicant: Unversity of Washington Through its Center for CommercializationInventors: Nephi Stella, Toni Kline
-
Publication number: 20130184307Abstract: The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.Type: ApplicationFiled: March 6, 2013Publication date: July 18, 2013Applicant: Arena Pharmaceuticals, Inc.Inventor: Arena Pharmaceuticals, Inc.
-
Patent number: 8486993Abstract: A pharmaceutical composition comprising tacrolimus (FK-506) dissolved and/or dispersed in a hydrophilic or water-miscible vehicle to form a solid dispersion or solid solution at ambient temperature have improved bioavailability.Type: GrantFiled: July 7, 2011Date of Patent: July 16, 2013Assignee: Veloxis Pharmaceuticals A/SInventor: Per Holm
-
Publication number: 20130165434Abstract: A harmful arthropod control composition comprising flonicamid, one or more Delphacidae control compounds selected from Group (A), and one or more rice blast disease control compounds selected from Group (B): Group (A): a group consisting of clothianidin, imidacloprid, dinotefuran, thiamethoxam, fipronil and pymetrozine. Group (B): a group consisting of isotianil, probenazole, tiadinil, tricyclazole, pyroquilone, thiophanate-methyl, orysastrobin and azoxystrobin.Type: ApplicationFiled: August 3, 2011Publication date: June 27, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Norihisa Sakamoto, Emiko Sakamoto
-
Patent number: 8470786Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing pyrroloquinolinyl-pyrrolidine-2,5-dione compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: December 23, 2011Date of Patent: June 25, 2013Assignee: ArQule, Inc.Inventors: Mark A. Ashwell, Darin Kizer, Takahiro Murai, Daisuke Nakai, Takanori Yasukochi
-
Publication number: 20130157990Abstract: A method of detoxifying a patient addicted to at least one drug comprises the step of administering a first-medication component to the patient for mitigating drug withdrawal symptoms of the patient. The method further comprises the step of administering an anesthetic component to the patient for putting the patient in a sedated state. The method further comprises the step of administering a detoxification component to the patient for detoxifying the patient of the drug(s) while the patient is in the sedated state. The detoxification component can comprise naloxone. The method further comprises the step of administering a second-medication component to the patient for further mitigating drug withdrawal symptoms of the patient while the patient is in the sedated state. The second-medication component can comprise naltrexone. The method further comprises the step of terminating administration of the anesthetic component to the patient for reviving the patient from the sedated state.Type: ApplicationFiled: February 20, 2013Publication date: June 20, 2013Applicant: EAGLE ADVANCEMENT INSTITUTE LLCInventor: EAGLE ADVANCEMENT INSTITUTE LLC
-
Publication number: 20130150398Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.Type: ApplicationFiled: February 7, 2013Publication date: June 13, 2013Inventors: Carl Berthelette, Michael Boyd, John Colucci, Karine Villeneuve, Joey L. Methot
-
Publication number: 20130150310Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.Type: ApplicationFiled: February 7, 2013Publication date: June 13, 2013Applicant: ARQULE, INC.Inventor: ARQULE, INC.
-
Publication number: 20130143866Abstract: Compositions of matter including ?-tocotrienol and SU11274 are disclosed herein. A variety of Met kinase inhibitors may be used in conjunction with tocotrienols in the treatment or prevention of cancer. Combinations of ?-tocotrienol and SU11274 inhibit the cell growth of +SA mammary tumor cells.Type: ApplicationFiled: December 2, 2012Publication date: June 6, 2013Inventor: Paul W. Sylvester
-
Patent number: 8455539Abstract: This invention provides CCI-779 cosolvent concentrates which are useful in preparing a parenteral formulation of rapamycin 42-ester with 3-hydroxy-2-(hydroxymethyl)-2-methylpropionic acid (CCI-779) following admixture with a diluent.Type: GrantFiled: October 15, 2012Date of Patent: June 4, 2013Assignee: Wyeth LLCInventors: Joseph T. Rubino, Victoria Siskavich, Maureen M. Harrison, Pooja Gandhi
-
Patent number: 8431702Abstract: Disclosed herein are compounds represented by the structural formula: therapeutic methods, compositions, and medicaments related thereto are also disclosed.Type: GrantFiled: August 8, 2012Date of Patent: April 30, 2013Assignee: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, Richard L. Beard, John E. Donello, Michael E. Garst
-
Publication number: 20130102626Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.Type: ApplicationFiled: September 14, 2012Publication date: April 25, 2013Inventors: Peter Wipf, Marie Celine Frantz
-
Patent number: 8415484Abstract: The present invention relates to certain substituted tricyclic acid derivatives of Formula (I) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, myocardial ischemia-reperfusion injury, hypertensive nephropathy, glomerulosclerosis, gastritis, polymyositis, thyroiditis, vitiligo, hepatitis, biliary cirrhosis, microbial infections and associated diseases, viral infections and associated diseases, diseases and disorders mediated by lymphocytes, auto immune diseases, inflammatory diseases, and cancer.Type: GrantFiled: August 26, 2009Date of Patent: April 9, 2013Assignee: Arena Pharmaceuticals, Inc.Inventors: Robert M. Jones, Daniel J. Buzard, Andrew M. Kawasaki, Sun Hee Kim, Lars Thoresen, Juerg Lehmann, Xiuwen Zhu
-
Patent number: 8394789Abstract: The invention relates to 5,6-dihydropyrrolo[2,1-?]isoquinoline and pyrrolo[2,1-?]isoquinoline derivatives according to general formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.Type: GrantFiled: February 6, 2009Date of Patent: March 12, 2013Assignee: MSD Oss B.V.Inventors: Rachel Deborah van Rijn, Hubert Jan Josef Loozen, Cornelis Marius Timmers, Lars Anders van der Veen, Willem Frederik Johan Karstens
-
Patent number: 8394819Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.Type: GrantFiled: February 19, 2010Date of Patent: March 12, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Carl Berthelette, Michael Boyd, John Colucci, Karine Villeneuve, Joey Methot
-
Publication number: 20130023494Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an SGLT2 inhibitor, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto.Type: ApplicationFiled: April 5, 2011Publication date: January 24, 2013Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Robert M. Jones, Sangdon Han, Daniel J. Buzard, Juerg Lehmann, Sanju Narayanan, Dawei Yue