Chalcogen Bonded Directly To A Ring Carbon Of The Purine Ring System Patents (Class 514/263.3)
  • Patent number: 9828362
    Abstract: The present invention provides a 1,4-disubstituted imidazole derivative of formula (1?) wherein ring Q1 is optionally-substituted C6-10 aryl group, etc.; R1 and R2 are independently hydrogen atom, etc.; W1 is optionally-substituted C1-4 alkylene group; W2 is —NR3aC(O)— wherein R3a is hydrogen atom or C1-6 alkyl group, etc.; ring Q2 is 5- to 10-membered heteroaryl group, etc.; W3 is optionally-substituted C1-4 alkylene group, etc.; n is 1, 2, 3, 4, or 5; R4 is independently halogen atom, optionally-substituted C1-6 alkyl group, etc.; R5 is hydroxy group, etc.; and a pharmacologically acceptable salt thereof, which have a potent inhibitory effect on the sphere-forming capacity of cancer cells and are useful as an orally-available anti-tumor agent.
    Type: Grant
    Filed: February 27, 2017
    Date of Patent: November 28, 2017
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Hitoshi Ban, Manabu Kusagi, Shingo Tojo, Futoshi Hasegawa, Miki Hashizume
  • Publication number: 20150148307
    Abstract: The present invention is directed to methods of prognosing relapsed leukemia in a subject. These methods are based on the detection of one or more relapse-specific gene mutations in a patient sample. The present invention further relates to methods of preventing and treating relapse leukemia in a subject based on the determined prognosis of the subject.
    Type: Application
    Filed: May 7, 2013
    Publication date: May 28, 2015
    Applicant: NEW YORK UNIVERSITY
    Inventors: William L. Carroll, Julia A. Meyer
  • Patent number: 9029413
    Abstract: Alterations of certain metabolite concentrations and fluxes that occur in response to viral infection are described. Host cell enzymes in the involved metabolic pathways are selected as targets for intervention; i.e., to restore metabolic flux to disadvantage viral replication, or to further derange metabolic flux resulting in “suicide” of viral-infected cells (but not uninfected cells) to limit viral propagation. While any of the enzymes in the relevant metabolic pathway can be selected, pivotal enzymes at key control points in these metabolic pathways are preferred as candidate antiviral drug targets. Inhibitors of these enzymes are used to reverse, or redirect, the effects of the viral infection. Drug candidates are tested for antiviral activity using screening assays in vitro and host cells, and in animal models. Animal models are then used to test efficacy of candidate compounds in preventing and treating viral infections. Antiviral activity of enzyme inhibitors is demonstrated.
    Type: Grant
    Filed: April 3, 2012
    Date of Patent: May 12, 2015
    Assignee: The Trustees of Princeton University
    Inventors: Josh Munger, Bryson Bennett, Thomas Shenk, Joshua Rabinowitz
  • Publication number: 20150087643
    Abstract: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity; the compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.
    Type: Application
    Filed: October 10, 2014
    Publication date: March 26, 2015
    Applicant: Advinus Therapeutics Private Limited
    Inventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
  • Publication number: 20150079116
    Abstract: NK cell licensing predisposes patients to chronic inflammatory disease. Methods and kits to diagnose and treat chronic inflammatory disease based on genetic haplotype and cytokine profile are described herein.
    Type: Application
    Filed: April 11, 2013
    Publication date: March 19, 2015
    Inventors: Jonathan Braun, Lin Lin
  • Publication number: 20150065525
    Abstract: Provided are compositions and methods for improving diaphragm function in a patient by administering to the patient an effective amount of a skeletal muscle troponin activator or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 1, 2013
    Publication date: March 5, 2015
    Inventors: Jeffrey R. Jasper, Fady Malik, Darren T. Hwee
  • Patent number: 8969556
    Abstract: A pharmaceutical composition for inhibiting at least protein kinase in a cell of a subject includes a purine based triazole.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: March 3, 2015
    Assignee: Case Western Reserve University
    Inventors: Prakash V. Reddy, Nanditha G. Nair, Wataru Kudo, Gemma Casadesus
  • Publication number: 20150011512
    Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.
    Type: Application
    Filed: September 12, 2014
    Publication date: January 8, 2015
    Inventors: Steven Albert Everett, Saraj Ulhaq
  • Publication number: 20140370105
    Abstract: Methods of administering a delayed release 6-mercaptopurine pharmaceutical composition to patients suffering from inflammatory bowel disease which provide for release of the 6-mercaptopurine after passage of the pharmaceutical composition through the stomach are disclosed. The methods result in significant clinical improvement despite leading to very little systemic absorption of 6-mercaptopurine and also result in very few undesirable side effects.
    Type: Application
    Filed: July 10, 2014
    Publication date: December 18, 2014
    Inventors: Vered Rosenberger, Brenda Kolatch, Linda Susan Marshall, Anna Hotovely-Salomon
  • Publication number: 20140303112
    Abstract: The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity.
    Type: Application
    Filed: April 9, 2013
    Publication date: October 9, 2014
    Inventors: Han-Min CHEN, Cheng-Yi KUO, Chun-Fang HUANG, Jiun-Tsai LIN
  • Publication number: 20140301947
    Abstract: A method for aiding in selecting or adjusting a dose of TSPO imaging or therapeutic agent for use with a subject, the method comprising the step of determining the subject's genotype for TSPO rs6971. A TSPO imaging or therapeutic agent for use in TSPO imaging or therapy in a subject, wherein the subject is a subject whose genotype at TSPO polymorphism position rs6971 is determined. The subject's genotype for TSPO may be taken into account when assessing the results of the TSPO imaging, for example normalising the subject's determined measure of binding of the TSPO agent to take account of the subject's determined genotype. The subject's genotype for TSPO may be taken into account when choosing the TSPO agent and/or the dose of TSPO agent. The subject may be a subject who has been determined to have genotype CC or CT at TSPO polymorphism position rs6971, for example when using a TSPO agent that binds with higher affinity to Aia147TSPO than to Thr147TSPO.
    Type: Application
    Filed: May 31, 2012
    Publication date: October 9, 2014
    Applicant: IMPERIAL INNOVATIONS LIMITED
    Inventors: David Owen, Martin Wilkins
  • Publication number: 20140303192
    Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.
    Type: Application
    Filed: March 5, 2014
    Publication date: October 9, 2014
    Applicant: HYDRA BIOSCIENCES, INC.
    Inventor: Jayhong A. Chong
  • Publication number: 20140303193
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Application
    Filed: June 6, 2013
    Publication date: October 9, 2014
    Applicant: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Christopher F. Claiborne, Stephen Critchley, Courtney A. Cullis, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
  • Patent number: 8853222
    Abstract: Anti-herpetic material such as 2-aminopurine derivatives, e.g., the aminocyclopropylcarboxylate derivatives of acyclovir, penciclovir, and ganciclovir, are described to prevent or treat autoimmune disease or a disease originating from an abnormal functioning of the sympathetic chain in a human subject. Prolonged use of the anti-herpetic compounds reduces prodrome, vesicle formation and viral shedding. The anti-herpetic compounds may be administered alone or in combination with a compound that reduces the rate of renal excretion of the anti-herpetic compound. The anti-herpetic compounds are particularly useful when administered at a level equivalent in activity to at—least about 150 mg/kg famciclovir per day.
    Type: Grant
    Filed: March 6, 2009
    Date of Patent: October 7, 2014
    Inventor: Ray W. Exley
  • Publication number: 20140294972
    Abstract: A liquid pharmaceutical composition for use in the treatment of acute lymphoblastic leukaemia (ALL) comprising 6-mercaptopurine or a salt, hydrate or solvate thereof and a pharmaceutically-acceptable excipient, wherein the composition is a suspension for oral administration, a kit of parts for the accurate dosing and administration of the liquid pharmaceutical composition, and a method for the treatment of ALL in a human patient comprising administration of a therapeutically effective amount of the liquid pharmaceutical composition.
    Type: Application
    Filed: September 7, 2012
    Publication date: October 2, 2014
    Applicant: NOVA BIO-PHARMA TECHNOLOGIES LIMITED
    Inventor: Peter John Pitt White
  • Publication number: 20140243273
    Abstract: The present invention provides method of treating or lessening the severity of a disease selected from spondyloarthropathy, systemic lupus erythematosus, rheumatoid arthritis, or any combination thereof comprising the administration of a compound of Formula I and an optional co-therapy (e.g., chemotherapy agent, DMARD, or any combination thereof). The present invention also provides a pharmaceutical composition comprising a compound of Formula I, a method of manufacturing a pharmaceutical composition comprising a compound of Formula I, and a method of administering a pharmaceutical composition comprising a solid form of a compound of Formula I.
    Type: Application
    Filed: May 7, 2014
    Publication date: August 28, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: Irina Nikolaevna Kadiyala, Shahla Jamzad, Thomas Carl Hoock, Lori Kell Taylor, Kathryn Lea Sewell
  • Patent number: 8791081
    Abstract: A method of treating a neoplastic disease in a subject includes administering to neoplastic cells of the subject an MGMT inhibitor and at least one of an antimitotic agent or a DNA damaging agent.
    Type: Grant
    Filed: February 29, 2008
    Date of Patent: July 29, 2014
    Assignee: Case Western Reserve University
    Inventors: Lili Liu, Stanton Gerson
  • Patent number: 8778952
    Abstract: A method of treating osteoarthritis by reducing intraosseous hypertension in a patient in need thereof by administering to a patient an effective amount of a composition containing a bone edema medication, such as a vasoactive medication or phosphodiesterase inhibitor, including a PDE-5.
    Type: Grant
    Filed: January 11, 2010
    Date of Patent: July 15, 2014
    Inventor: Joseph Bernstein
  • Patent number: 8765712
    Abstract: The present invention concerns an agent for prevention and treatment of pityriasis. The agent according to the present invention comprises at least one transaminase inhibitor effectively inhibiting the transamination process which is of pathogenetic relevance for the disease, prevents a recurrence of the disease and which protects the human skin flora. Upon release into the environment, no resistances are induced in other fungi.
    Type: Grant
    Filed: January 14, 2010
    Date of Patent: July 1, 2014
    Assignee: Justus-Liebig-Universitaet Giessen
    Inventor: Peter Mayser
  • Publication number: 20140178354
    Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.
    Type: Application
    Filed: December 23, 2013
    Publication date: June 26, 2014
    Applicant: The Regents of the University of California
    Inventors: William Fenical, Paul Jensen, Tracy Mincer, Robert H.R. Feling
  • Patent number: 8759361
    Abstract: 2-Phenoxy pyrimidinone analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.
    Type: Grant
    Filed: August 22, 2011
    Date of Patent: June 24, 2014
    Assignee: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
  • Publication number: 20140161888
    Abstract: The present invention provides improved formulations of 6-mercaptopurine that exhibit better bioavailability and faster dissolution than previous formulations.
    Type: Application
    Filed: February 10, 2014
    Publication date: June 12, 2014
    Applicant: TEVA PHARMACEUTICAL INDUSTRIES LTD.
    Inventors: E. Itzhak Lerner, Moshe Flashner-Barak, Erwin v Achthoven, Hans Keegstra, Ruud Smit
  • Patent number: 8735406
    Abstract: The present invention provides a compound represented by the formula (1) or a pharmaceutically acceptable salt thereof (wherein W represents a hydrogen atom, a halogen atom, or the others; A represents an alkyl group optionally substituted by aryl group or the others, an aryl group, or the others; and one of X and Y represents a di-substituted alkylaminocarbonyl group, or the others, and the other represents a hydrogen atom, an alkyl group, an alkylcarbonyl group, or the others); a medicament or a pharmaceutical composition for treatment or prophylaxis of FAAH-related diseases such as depression, anxiety disorder or pains, comprising the compound or the like as an active ingredient; a use of the compound or the like; and a method for treatment or prophylaxis using the compound or the like.
    Type: Grant
    Filed: September 8, 2010
    Date of Patent: May 27, 2014
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Keiji Adachi, Yoko Nakai, Tomoyuki Furuta, Yuki Fujii
  • Patent number: 8716300
    Abstract: Embodiments of the present disclosure include a coordination complex, comprising a first biologically active moiety, a second biologically active moiety, and a metal, wherein the first biologically active moiety and second biologically active moiety are bound to the metal by covalent coordination bonds, and wherein the first biologically active moiety and second biologically active moiety are different. These complexes may enhance the pharmacodynamic properties of biologically active moieties.
    Type: Grant
    Filed: July 5, 2012
    Date of Patent: May 6, 2014
    Assignee: Synthonics, Inc.
    Inventors: Thomas Piccariello, Scott B. Palmer, John D. Price, Robert Oberlender, Mary C. Spencer, Michaela E. Mulhare
  • Publication number: 20140093505
    Abstract: The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.
    Type: Application
    Filed: June 4, 2012
    Publication date: April 3, 2014
    Applicant: Xuanzhu Pharma Co., Ltd.
    Inventors: Frank Wu, Yan Zhang
  • Patent number: 8680108
    Abstract: The present invention provides fused aryl and heteroaryl derivatives of Formula I: wherein X, V, Y, U, W, Z, R1, R2, Cy, and Ar are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: March 25, 2014
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, Andrew P. Combs, Eddy W. Yue, Hui-Yin Li
  • Patent number: 8653060
    Abstract: The present invention provides improved formulations of 6-mercaptopurine that exhibit better bioavailability and faster dissolution than previous formulations.
    Type: Grant
    Filed: April 25, 2012
    Date of Patent: February 18, 2014
    Assignee: Teva Pharmaceutical Industries Ltd.
    Inventors: E. Itzhak Lerner, Moshe Flashner-Barak, Erwin v Achthoven, Hans Keegstra, Ruud Smit
  • Publication number: 20130345242
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Application
    Filed: June 6, 2013
    Publication date: December 26, 2013
    Applicant: MILLENNIUM PHARMACEUTICALS, INC.
    Inventors: Christopher F. Claiborne, Stephen Critchley, Courtney A. Cullis, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
  • Publication number: 20130330322
    Abstract: A method of reducing the appearance of skin aging comprising the step of applying a topical composition to the skin of a human exhibiting one or more signs of skin aging selected from fine lines, wrinkles, decreased skin elasticity, decreased light reflection, uneven pigmentation (dyschromia), coarse texture, dryness, solar lentigos, seborrheic keratoses, decreased dermal thickness, and/or increased sebum production, wherein the composition consists essentially of a dermatologically acceptable carrier and a targeted immune response modifier selected the group consisting of: (i) a 5-amino thiazolo[4,5-d]pyrimidin-one compound; (ii) an 8-hydroxyadenine compound; (iii) an imidazo-1,5-napthyridine compound; (iv) a 2-substituted-8-oxodeazapurine; (v) methyl 2-(3-{[6-amino-2-butoxy-8-oxo-7H-purin-9(8H)-yl]methyl}phenyl)acetate; (vi) 2-(3-{[6-amino-2-butoxy-8-oxo-7H-purin-9(8H)-yl]methyl}phenyl)acetic acid; and (iii) methyl 2-(3-(((3-(6-amino-2-butoxy-8-oxo-7H-purin-9(8H)-yl)propyl)(3-(dimethylamino)propyl)amino) ph
    Type: Application
    Filed: August 14, 2013
    Publication date: December 12, 2013
    Applicant: Metabeauty, Inc.
    Inventor: Leslie Baumann
  • Publication number: 20130331403
    Abstract: Crystalline polymorph forms of 2-(5-bromo-4-(4-cyclopropyl naphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid are described. Pharmaceutical compositions and the uses of such compounds, compound forms, and compositions for the treatment of a variety of diseases and conditions are also presented.
    Type: Application
    Filed: August 14, 2013
    Publication date: December 12, 2013
    Applicant: Ardea Biosciences, Inc.
    Inventors: Laszlo R. TREIBER, Irina ZAMANSKY, Jean-Luc GIRARDET
  • Patent number: 8592433
    Abstract: The invention provides a novel class of compounds having the structure of Formula I, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, Bcr-Abl, Aurora-A, Axl, BMX, CHK2, c-RAF, cSRC, Fes, FGFR3, Flt3, IKK?, IR, JNK2?2, Lck, Met, MKK6, MST2, p70S6K, PDGFR?, PKA, PKD2, ROCK-II, Ros, Rsk1, SAPK2?, SAPK2?, SAPK3, SAPK4, Syk, Tie2 and TrkB kinases:
    Type: Grant
    Filed: October 20, 2006
    Date of Patent: November 26, 2013
    Inventors: Advait Nagle, Nathanael S. Gray
  • Publication number: 20130280328
    Abstract: Methods of administering a delayed release 6-mercaptopurine pharmaceutical composition to patients suffering from inflammatory bowel disease which provide for release of the 6-mercaptopurine after passage of the pharmaceutical composition through the stomach are disclosed. The methods result in significant clinical improvement despite leading to very little systemic absorption of 6-mercaptopurine and also result in very few undesirable side effects.
    Type: Application
    Filed: June 19, 2013
    Publication date: October 24, 2013
    Inventors: Vered Rosenberger, Brenda Kolatch, Linda Susan Marshall, Anna Hotovely-Salomon
  • Patent number: 8557831
    Abstract: Disclosed herein are methods of delaying the onset or treating diabetes that comprises administering a uric acid lowering agent. The inventors have made the remarkable discovery that elevated uric acid levels are not a corollary to insulin resistance, but rather a primary mediator of insulin resistance. Specifically exemplified are methods that involve administering to a patient susceptible to development of diabetes a composition comprising a uric acid lowering agent in a regimen that maintains serum uric acid levels below at least 5.2 to 5.5 mg/dl.
    Type: Grant
    Filed: July 21, 2005
    Date of Patent: October 15, 2013
    Assignee: University of Florida Research Foundation, Inc.
    Inventors: Richard J. Johnson, Takahiko Nakagawa
  • Patent number: 8552011
    Abstract: The present application relates to anti-viral selenopurine compounds of formula (I): wherein R1 is C2-6alkyl, and pharmaceutically acceptable salts, solvates, and prodrugs thereof. These 6-(C2-6alkylseleno)purine compounds find use in the treatment of neural measles virus infection and associated diseases (namely, multiple sclerosis or neural measles). A particularly preferred compound is ethylselenopurine or ESP.
    Type: Grant
    Filed: June 4, 2009
    Date of Patent: October 8, 2013
    Inventor: William G. Tucker
  • Patent number: 8530484
    Abstract: The method includes the steps of cleansing of the scalp sufficiently to remove material which would otherwise block antiviral medication from reaching hair follicles, heating the scalp to increase the absorption of the antiviral medication and applying the antiviral medication to the scalp in effective amount to suppress viral replication or viral activation present in the nerves leading to the scalp.
    Type: Grant
    Filed: November 4, 2009
    Date of Patent: September 10, 2013
    Assignee: Loreal SA
    Inventor: Robert E Akridge
  • Patent number: 8501724
    Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: August 6, 2013
    Assignee: Pharmacyclics, Inc.
    Inventors: Wei Chen, David J. Loury
  • Publication number: 20130184240
    Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like; m is an integer of 0 to 3; R2 is hydrogen, or substituted or unsubstituted alkyl; X is —O—; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
    Type: Application
    Filed: September 8, 2011
    Publication date: July 18, 2013
    Applicant: Shionogi & Co., Ltd.
    Inventors: Keisuke Tonogaki, Akira Ino, Eiichi Kojima, Manabu Katou, Masafumi Iwatsu, Nobuyuki Tanaka, Masahiko Fujioka
  • Publication number: 20130121986
    Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.
    Type: Application
    Filed: December 26, 2012
    Publication date: May 16, 2013
    Inventors: Frederic MARION, Jean-Philippe ANNEREAU, Jacques FAHY
  • Publication number: 20130101615
    Abstract: This invention is a method for immunizing, preventing or treating a Mycobacterium avium subspecies paratuberculosis-associated disease or condition by screening subjects for markers indicative of predisposition or susceptibility to a Mycobacterium avium subspecies paratuberculosis-associated disease or condition and administering a Mycobacterium avium subspecies paratuberculosis vaccine or prophylactic or therapeutic agent.
    Type: Application
    Filed: December 14, 2012
    Publication date: April 25, 2013
    Inventor: Robert J. Greenstein
  • Publication number: 20130101514
    Abstract: Activated fatty acids, pharmaceutical composition compositions including activated fatty acids, methods for using activated fatty acids to treat nephropathy, and methods for preparing activated fatty acids are provided herein.
    Type: Application
    Filed: October 10, 2012
    Publication date: April 25, 2013
    Applicant: Complexa, Inc.
    Inventor: Complexa, Inc.
  • Publication number: 20130064789
    Abstract: The present invention relates to hairy cell leukemia biomarkers and methods of utilizing these biomarkers to diagnose and/or treat hairy cell leukemia.
    Type: Application
    Filed: May 10, 2012
    Publication date: March 14, 2013
    Inventors: Brunangelo Falini, Raul Rabadan, Enrico Tiacci
  • Patent number: 8383634
    Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1, R3, R4, L, X, Y, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
    Type: Grant
    Filed: May 23, 2011
    Date of Patent: February 26, 2013
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Deborah Sue Mortensen, Maria Mercedes Delgado Mederos, John Joseph Sapienza, Ronald J. Albers, Steven Spencer Clareen, Kimberly Lyn Schwarz, Jason Simon Parnes, Jennifer R. Riggs, Patrick William Papa, Sayee Gajanan Hegde, Jeffrey Mark McKenna
  • Patent number: 8372852
    Abstract: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: February 12, 2013
    Assignee: Ardea Biosciences, Inc.
    Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
  • Patent number: 8372807
    Abstract: Described herein are compounds useful in the reduction of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, a compound disclosed herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: February 12, 2013
    Assignee: Ardea Biosciences, Inc.
    Inventors: Martha De La Rosa, Jean-Luc Girardet, Karen Watson
  • Patent number: 8318728
    Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.
    Type: Grant
    Filed: May 14, 2009
    Date of Patent: November 27, 2012
    Assignee: Hydra Biosciences, Inc.
    Inventor: Jayhong A. Chong
  • Publication number: 20120282172
    Abstract: The present invention provides a system presenting site-specific accumulation through a ligand that specifically targets a receptor overexpressed on the surface of specific cells within a target organ, like, for example, tumor cells and/or vascular cells of tumor blood vessels. Moreover, this invention provides a method where, upon internalization of the previous-mentioned system by the target cells, triggered release at a high rate of the associated agent takes place, permitting efficient intracellular delivery and, thus, increased concentration of the transported cargo at the target site. Overall, this invention provides a method for the diagnosis, prevention and treatment of human diseases and disorders.
    Type: Application
    Filed: May 9, 2012
    Publication date: November 8, 2012
    Applicants: Centro de Neurociencias e Biologia Celular, Universidade de Coimbra
    Inventors: João Nuno Sereno de Almeida Moreira, Vera Lúcia Dantas Nunes Caldeira de Moura, Sérgio Paulo de Magalhães Simões, Maria da Conceição Monteiro Pedroso de Lima
  • Publication number: 20120283267
    Abstract: Methods of treating exposure to Giardia lamblia and/or giardiasis and methods of antagonizing Giardia lamblia attachment to the intestinal wall of a subject are described herein.
    Type: Application
    Filed: December 2, 2010
    Publication date: November 8, 2012
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Heidi G. Elmendorf, Colleen D. Walls, Christian Wolf
  • Publication number: 20120277256
    Abstract: Embodiments of the present disclosure include a coordination complex, comprising a first biologically active moiety, a second biologically active moiety, and a metal, wherein the first biologically active moiety and second biologically active moiety are bound to the metal by covalent coordination bonds, and wherein the first biologically active moiety and second biologically active moiety are different. These complexes may enhance the pharmacodynamic properties of biologically active moieties.
    Type: Application
    Filed: July 5, 2012
    Publication date: November 1, 2012
    Applicant: Synthonics, Inc.
    Inventors: Thomas Piccariello, Scott B. Palmer, John D. Price, Robert Oberlender, Mary C. Spencer, Michaela E. Mulhare
  • Publication number: 20120230972
    Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.
    Type: Application
    Filed: May 22, 2012
    Publication date: September 13, 2012
    Inventors: William Fenical, Paul Jensen, Tracy Mincer, Robert H.R. Feling
  • Publication number: 20120225869
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).
    Type: Application
    Filed: March 8, 2012
    Publication date: September 6, 2012
    Applicant: IRM LLC
    Inventors: Hong Liu, Xiaohui He, Ha-Soon Choi, Kunyong Yang, David H. Woodmansee, Zhicheng Wang, David Archer Ellis, Boagen Wu, Yun He, Truc Ngoc Nguyen