Additional Hetero Ring Attached Directly Or Indirectly To The Purine Ring System By Nonionic Bonding Patents (Class 514/263.2)
  • Publication number: 20120022001
    Abstract: A method of parenterally administering a composition, the method including parenterally administering to a person a composition including at least one omega-3 fatty acid and at least one drug, wherein the at least one omega-3 fatty acid source and the at least one drug are administered simultaneously.
    Type: Application
    Filed: September 12, 2011
    Publication date: January 26, 2012
    Applicant: STABLE SOLUTIONS LLC
    Inventor: David F. Driscoll
  • Publication number: 20120014949
    Abstract: The present invention provides an improved method of diagnosing a subject having received an organ transplant with Acute Cellular Rejection (ACR). The method comprises obtaining a biological sample from the subject, detecting an amount of at least one protein indicative of ACR in the sample, and comparing the amount of the protein in the sample to a control, wherein a difference between the amount of the protein in the sample relative to the control indicates the subject has or is developing ACR. The difference can be an increase or a decrease. In one version the biological sample comprises a serum sample, and the transplanted organ is selected from a heart, kidney, liver, bone marrow, pancreas, eye, lung or skin. Methods of treating a subject having an organ transplant for ACR are also provided.
    Type: Application
    Filed: July 18, 2011
    Publication date: January 19, 2012
    Inventor: Michael R. Charlton
  • Publication number: 20120004212
    Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.
    Type: Application
    Filed: August 26, 2011
    Publication date: January 5, 2012
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
  • Publication number: 20120003329
    Abstract: This disclosure relates generally to treating patients having pulmonary hypertension, or symptoms associated therewith, by administering a therapeutically effective amount of an A2B receptor antagonist to the patient.
    Type: Application
    Filed: June 29, 2011
    Publication date: January 5, 2012
    Inventors: Luiz Belardinelli, Dewan Zeng, Hongyan Zhong
  • Publication number: 20120003228
    Abstract: The invention relates to means and methods for determining whether a subject is at high or low risk of autoimmune disease progression by determining the CD8 or CD4 cell subtype of the subject. Autoimmune diseases of particular interest include vasculitis, systemic lupus erythematosus (SLE), rheumatoid arthritis, multiple sclerosis, and inflammatory bowel disease. The invention also relates to means and methods for determining the CD8 or CD4 cell subtype of a subject, e.g. for predicting responses to infection, vaccination and/or transplantation.
    Type: Application
    Filed: January 20, 2010
    Publication date: January 5, 2012
    Applicant: Cambridge Enterprise Limited
    Inventors: Ken Smith, Paul Lyons, Eoin McKinney
  • Publication number: 20120003306
    Abstract: The invention discloses a pharmaceutical composition of bioactive nanoparticles composed of chitosan, poly-glutamic acid, and a bioactive agent for oral delivery. The chitosan-based nanoparticles are characterized with a positive surface charge and enhanced permeability for oral drug delivery.
    Type: Application
    Filed: September 8, 2011
    Publication date: January 5, 2012
    Inventors: Hsing-Wen Sung, Kiran Sonaje, Hosheng Tu
  • Publication number: 20120004247
    Abstract: A compound of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof, and their preparation and use as pharmaceuticals wherein R1, R2 and R3 are as defined herein.
    Type: Application
    Filed: August 26, 2011
    Publication date: January 5, 2012
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
  • Publication number: 20120004246
    Abstract: This invention relates to novel purinyl derivatives and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.
    Type: Application
    Filed: March 27, 2008
    Publication date: January 5, 2012
    Applicant: NeuroSearch A/S
    Inventors: Birgitte L. Eriksen, Ulrik Svane Sorensen, Charlotte Hougaard, Dan Peters, Palle Christophersen
  • Publication number: 20110319404
    Abstract: The present invention relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for treating non-Hodgkin's lymphoma, in a subject in need thereof.
    Type: Application
    Filed: September 7, 2011
    Publication date: December 29, 2011
    Inventor: Kevin Foley
  • Publication number: 20110312979
    Abstract: The present invention provides fused pyrrole derivatives of Formula I: wherein V, W, X, Y, L, Q, Ar, Z, R1 and R6 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: Application
    Filed: June 21, 2011
    Publication date: December 22, 2011
    Inventors: Yun-Long Li, Andrew P. Combs
  • Publication number: 20110306610
    Abstract: The present invention provides an 8-oxoadenine compound having immunemodulating activities such as an interferon inducing activity and useful as an antiviral agent and antiallergic agent, which is represented by the following formula (1): [wherein the ring A represents a 6-10 membered aromatic carbocyclic ring and the like, R represents a halogen atom, an alkyl group and the like, n represents an integer of 0-2, Z1 represents alkylene, X2 represents oxygen atom, sulfur atom, SO2, NR5, CO, CONR5, NR5CO and the like, Y1, Y2 and Y3 represent independently a single bond or an alkylene group, X1 represents oxygen atom, sulfur atom, NR4 (R4 is hydrogen atom or an alkyl group) or a single bond, R2 represents a substituted or unsubstituted alkyl group, R1 represents hydrogen atom, hydroxy group, an alkoxy group, an alkoxycarbonyl group or a haloalkyl group] or its pharmaceutically acceptable salt.
    Type: Application
    Filed: July 20, 2011
    Publication date: December 15, 2011
    Applicants: AstraZeneca Aktiebolag, Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Ayumu KURIMOTO, Kazuki Hashimoto, Yoshiaki Isobe, Stephen Brough, Ian Millichip, Hiroki Wada, Roger Bonnert, Thomas Mcinally
  • Patent number: 8071565
    Abstract: Compounds of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof, wherein W, R1, R2 and R3 have the meanings as indicated in the specification, are useful for treating conditions mediated by activation of the adenosine A2A receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.
    Type: Grant
    Filed: July 11, 2007
    Date of Patent: December 6, 2011
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor
  • Patent number: 8071609
    Abstract: This invention relates to compounds of the general formula: in which Q is an ethynyl or ethenyl moiety; Ring A is an aryl, heteroaryl or heterocyclic ring or ring system; and the remaining variable groups are as defined herein, and to their preparation and use.
    Type: Grant
    Filed: August 11, 2006
    Date of Patent: December 6, 2011
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Yihan Wang, Wei-Sheng Huang, Rajeswari Sundaramoorthi, Xiaotian Zhu, R. Mathew Thomas, William C. Shakespeare, David C. Dalgarno, Tomi K. Sawyer
  • Publication number: 20110293610
    Abstract: The present invention relates to antibodies and related molecules that immunospecifically bind to B Lymphocyte Stimulator. The present invention also relates to methods and compositions for detecting or diagnosing a disease or disorder associated with aberrant B Lymphocyte Stimulator expression or inappropriate function of B Lymphocyte Stimulator comprising antibodies or fragments or variants thereof or related molecules that immunospecifically bind to B Lymphocyte Stimulator. The present invention further relates to methods and compositions for preventing, treating or ameliorating a disease or disorder associated with aberrant B Lymphocyte Stimulator expression or inappropriate B Lymphocyte Stimulator function comprising administering to an animal an effective amount of one or more antibodies or fragments or variants thereof or related molecules that immunospecifically bind to B Lymphocyte Stimulator.
    Type: Application
    Filed: August 12, 2011
    Publication date: December 1, 2011
    Applicant: HUMAN GENOME SCIENCES, INC.
    Inventors: Steven M. RUBEN, Steven C. BARASH, Gil H. CHOI, Tristan VAUGHAN, David HILBERT
  • Patent number: 8067413
    Abstract: The present invention provides compounds of formula (I) wherein R1, Y1, X1, L and R2 are as defined in the specification, and pharmaceutically acceptable salts thereof, as well as processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: November 29, 2011
    Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Roger Victor Bonnert, Thomas McInally, Stephen Thom
  • Patent number: 8067411
    Abstract: The present invention provides compounds of formula wherein R1, Y1, X1, Z1, X2, Y2, A, n and R2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: November 29, 2011
    Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Roger Victor Bonnert, Thomas McInally, Tobias Mochel, Stephen Thom
  • Patent number: 8063051
    Abstract: The present invention provides compounds of formula where n, R1, R2, A, X1, Y1, Z1, X2 and Y2 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: November 22, 2011
    Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Roger Victor Bonnert, Thomas McInally, Stephen Thom
  • Publication number: 20110281859
    Abstract: Compounds of the formula I, in which D, X, Y, Z, R and R1 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
    Type: Application
    Filed: December 22, 2009
    Publication date: November 17, 2011
    Applicant: Merck Patent Gesellschaft MIT Beschrankter Haftung
    Inventors: Timo Heinrich, Frank Zenke, Mireille Krier, Kai Schiemann
  • Patent number: 8058281
    Abstract: The present invention is directed to a method of treating systemic lupus erythematosus comprising administering a compound of formula (I) wherein R1 is selected from the group consisting of CF3, a C1-C5 alkyl, and (CH2)nR4, wherein n is between 0 and 4; R2 is selected from the group consisting of (CH2)mR4 and (CH2)mAr, wherein m is between 0 and 5; R3 is selected from the group consisting of hydrogen and methyl; R4 is selected from the group consisting of phenyl, OH, a C1-C3 alkoxy, a C1-C3 dialkylamino, piperidino, and N-methylpiperazino; Ar represents ?wherein X is selected from the group consisting of F, C1, a C1-C3 alkoxy, and CF3. The compounds can be used in combination with a second compound used in the treatment of systemic lupus erythematosus.
    Type: Grant
    Filed: March 6, 2007
    Date of Patent: November 15, 2011
    Assignee: Centre National de la Recherche Scientifique (CNRS)
    Inventors: Claire Renée Jeanne Lugnier, Sylviane Paule Ghislaine Muller, Fanny Sylvie Michèle Monneaux, Jean-Jaques Bourguignon
  • Publication number: 20110269780
    Abstract: Disclosed are small molecule inhibitors of the formula (I): and the pharmaceutical compositions thereof and processes of making the same. The compounds are useful in treating various diseases and conditions involving chymase.
    Type: Application
    Filed: August 25, 2009
    Publication date: November 3, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Michel Jose Emmanuel, Xin Guo, Jin Mi Kim, Ho Yin Lo, Peter Allen Nemoto, Kevin Chungeng Qian
  • Publication number: 20110263561
    Abstract: Compounds of the formula (I), in which R, X, Y, Z, R3 and R4 have the meanings indicated in claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
    Type: Application
    Filed: May 13, 2009
    Publication date: October 27, 2011
    Applicant: Merck Patent GmbH
    Inventors: Timo Heinrich, Mireille Krier, Thorsten Knoechel, Alfred Jonczyk, Frank Zenke, Holger Enderle
  • Publication number: 20110262398
    Abstract: Disclosed herein are reagents and methods for detecting and treating age-related diastolic dysfunction in an animal or a human.
    Type: Application
    Filed: April 21, 2011
    Publication date: October 27, 2011
    Applicant: UNIVERSITY OF ILLINOIS
    Inventors: Samuel C. Dudley, Roy L. Sutliff
  • Publication number: 20110263493
    Abstract: The present invention relates to the finding that certain DPP-4 inhibitors are particularly suitable for treating and/or preventing metabolic diseases, particularly diabetes, in patients for whom metformin therapy is inappropriate due to intolerability or contraindication against metformin.
    Type: Application
    Filed: August 5, 2009
    Publication date: October 27, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Klaus Dugi, Eva Ulrike Graefe-Mody, Ruth Harper, Hans-Juergen Woerle
  • Patent number: 8044061
    Abstract: Disclosed are novel compounds of the general formula (Ia), and pharmaceutically acceptable salts, isomers, diastereomers or enantiomers thereof and their use as medicines, for example in the treatment of dopamine-related movement disorders.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: October 25, 2011
    Assignee: UCB Pharma GmbH
    Inventors: Christa E. Müller, Jörg Hockemeyer, Nikolay T. Tzvetkov, Joachim C. Burbiel
  • Patent number: 8044056
    Abstract: A novel adenine compound represented by the formula (1): [wherein R1 is substituted or unsubstituted alkyl, etc., X is oxygen, etc., A1 is 4- to 8-membered substituted or unsubstituted saturated nitrogen-containing heterocycle containing 1 to 2 hetero atom(s) selected from 1 to 2 nitrogen(s), 0 to 1 oxygen and 0 to 1 sulfur, etc., A2 is substituted or unsubstituted 6- to 10-membered aryl, etc., L1 and L2 are independently a straight chain or branched chain alkylene, etc.], or a pharmaceutically acceptable salt thereof, which is useful as a medicament.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: October 25, 2011
    Assignees: Dainippon Sumitomo Pharma Co., Ltd., AstraZeneca Aktiebolag
    Inventors: Yoshiaki Isobe, Tomoaki Nakamura
  • Publication number: 20110257127
    Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
    Type: Application
    Filed: June 27, 2011
    Publication date: October 20, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
  • Publication number: 20110257167
    Abstract: Provided herein are methods for treating and/or preventing a cancer or a tumor syndrome in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having cancer or a tumor syndrome, characterized by a LKB1 and/or AMPK gene or protein loss or mutation.
    Type: Application
    Filed: February 3, 2011
    Publication date: October 20, 2011
    Inventors: Rajesh Chopra, Yuhong Ning, Sabita Sankar, Shuichan Xu, Weiming Xu
  • Publication number: 20110257205
    Abstract: The present invention relates to compounds which are xanthine derivatives, processes for the manufacture of said derivatives, pharmaceutical formulations containing these compounds and the use of the compounds in therapy, for example, in the treatment of diseases where under-activation of the HM74A receptor contributes to the disease or where activation of the receptor will be beneficial.
    Type: Application
    Filed: April 18, 2011
    Publication date: October 20, 2011
    Inventors: Richard Jonathan Daniel HATLEY, Andrew McMurtrie Mason, Ivan Leo Pinto
  • Publication number: 20110251217
    Abstract: This invention relates to novel substituted purinyl-pyrazol derivatives of formula (I) and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.
    Type: Application
    Filed: September 22, 2009
    Publication date: October 13, 2011
    Applicant: NEUROSEARCH A/S
    Inventors: Birgitte L. Eriksen, Charlotte Hougaard, Dan Peters, Palle Christophersen
  • Publication number: 20110250279
    Abstract: This invention relates to a controlled-release composition for producing a sustained-release preparation containing udenafil, including (A) udenafil and a pharmaceutically acceptable salt, (B) a solubility modulator, (C) an adsorbent, and (D) a hydrophilic polymer. This controlled-release composition for producing a sustained-release preparation containing udenafil releases drugs constantly regardless of the pH level in the gastrointestinal tract, and thus freely controls the drug release time within the range of 3˜24 hours, and reduces the variability in the effect of drugs among individuals. Also, this composition can be produced into a sustained-release preparation which has an optimum condition for expressing the effect of drugs in the treatment of diseases including pulmonary arterial hypertension, hepatic portal vein hypertension, benign prostatic hyperplasia, and the like, which can be treated by udenafil and which requires the long-term drug administration.
    Type: Application
    Filed: December 10, 2009
    Publication date: October 13, 2011
    Applicant: Dong-A Pharm. Co., Ltd.
    Inventors: Moo-Hi Yoo, Bong-Jin Cha, Jeong-Hoon Kim, Sun-Woo Jang, Sang-Dug Han
  • Publication number: 20110245265
    Abstract: Methods to treat or prevent acute kidney injury and chronic kidney injury in subjects using CXCR4 antagonists are disclosed.
    Type: Application
    Filed: August 28, 2009
    Publication date: October 6, 2011
    Applicant: GENZYME CORPORATION
    Inventors: Anna Zuk, Steven Ledbetter, Nibedita Chattopadhyay
  • Publication number: 20110245257
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lympho
    Type: Application
    Filed: April 1, 2011
    Publication date: October 6, 2011
    Applicant: AMGEN INC.
    Inventors: Timothy D. Cushing, Jason A. Duquette, Xiao He, Julia Lohman, Youngsook Shin
  • Patent number: 8030495
    Abstract: The present invention is directed to cyclopropyl proline bis-amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.
    Type: Grant
    Filed: May 19, 2008
    Date of Patent: October 4, 2011
    Inventors: Paul J. Coleman, Swati P. Mercer, Anthony J. Roecker
  • Publication number: 20110237607
    Abstract: This invention relates to novel substituted purinyl-pyrazol derivatives (I) and their use as potassium channel modulating agents. Moreover the invention is directed to pharmaceutical compositions useful for the treatment or alleviation of diseases or disorders associated with the activity of potassium channels.
    Type: Application
    Filed: September 22, 2009
    Publication date: September 29, 2011
    Applicant: NEUROSEARCH A/S
    Inventors: Birgitte L. Eriksen, Charlotte Hougaard, Dan Peters, Palle Christophersen
  • Publication number: 20110236348
    Abstract: The present invention includes therapeutic methods that include the administration of a compound of Formula I or II: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, to a subject in need of such, and therapeutic methods that include the administration of such compounds with at least one additional active agent.
    Type: Application
    Filed: June 3, 2011
    Publication date: September 29, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Randall L. Halcomb
  • Patent number: 8026244
    Abstract: There are disclosed novel compounds of Formula (I) wherein L, R1, X and Y are as defined in the specification, and pharmaceutically acceptable salts thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of neuroinflammatory disorders, cardio- and cerebrovascular atherosclerotic disorders and peripheral artery disease and respiratory disorders.
    Type: Grant
    Filed: April 12, 2007
    Date of Patent: September 27, 2011
    Assignee: AstraZeneca AB
    Inventors: Anna-Karin Tiden, Jenny Viklund
  • Publication number: 20110229500
    Abstract: The present invention relates to compounds of formula (I): wherein R1 is C1-6alkylamino, C1-6alkoxy, or C3-7cycloalkyloxy; m is an integer having a value of 3 to 6; n is an integer having a value of 0 to 4; and salts thereof are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions for example allergic rhinitis and asthma, the treatment of infectious diseases and cancer, and may also be useful as vaccine adjuvants.
    Type: Application
    Filed: August 7, 2009
    Publication date: September 22, 2011
    Applicant: GLAXOSMITHKLINE LLC
    Inventors: Keith Biggadike, Diane Mary Coe, Xiao Qing Lewell, Charlotte Jane Mitchell, Stephen Allan Smith, Naimisha Trivedi
  • Publication number: 20110224217
    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: Application
    Filed: May 23, 2011
    Publication date: September 15, 2011
    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
  • Publication number: 20110218197
    Abstract: The present invention is directed to substituted aza-bicyclic imidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by TRP M8, including for example, inflammatory pain, inflammatory hyperalgesia, inflammatory hypersensitivity condition, neuropathic pain, neuropathic cold allodynia, inflammatory somatic hyperalgesia, inflammatory visceral hyperalgesia, cardiovascular disease aggravated by cold and pulmonary disease aggravated by cold.
    Type: Application
    Filed: February 25, 2011
    Publication date: September 8, 2011
    Inventors: Mark R. PLAYER, Raul Calvo, Jinsheng Chen, Sanath Meegalla, Daniel Parks, William Parsons, Scott Ballentine, Shawn Branum
  • Publication number: 20110217295
    Abstract: This invention provides a method of treating a subject afflicted with active lupus arthritis comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This invention also provides laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with active lupus arthritis. This invention further provides a pharmaceutical composition comprising an amount of laquinimod or pharmaceutically acceptable salt thereof for use in treating a subject afflicted with lupus arthritis.
    Type: Application
    Filed: March 2, 2011
    Publication date: September 8, 2011
    Inventors: Asi Haviv, Nora Tarcic
  • Publication number: 20110190319
    Abstract: The present invention provides fused derivatives of Formula I: 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: Application
    Filed: December 17, 2010
    Publication date: August 4, 2011
    Inventors: Andrew P. Combs, Yun-Long Li, Eddy W. Yue, Richard B. Sparks
  • Publication number: 20110189125
    Abstract: Compositions and methods for modulating HSP70 function, particularly for the targeted killing of cancer cells, are disclosed.
    Type: Application
    Filed: March 18, 2011
    Publication date: August 4, 2011
    Applicants: Trustees of the University of Pennsylvania, Fox Chase Cancer Center
    Inventors: Donna L. George, Julia I-Ju Leu, Maureen Murphy
  • Patent number: 7989459
    Abstract: A chemical genus of purinones and 1H-imidazopyridinones, which are useful as PKC?. inhibitors, and their methods of use are disclosed. The genus is represented by the formula I: wherein R1 is chosen from nitrogen-attached heterocyclyl, nitrogen-attached substituted heterocyclyl wherein the point of attachment is a nitrogen heteroatom, and R2 is chosen from aryl, substituted aryl, arylalkyl, substituted arylalkyl, heteroaryl, substituted heteroaryl, hetroarylalkyl, and substituted heteroarylalkyl.
    Type: Grant
    Filed: February 2, 2007
    Date of Patent: August 2, 2011
    Assignee: Pharmacopeia, LLC
    Inventors: Andrew Roughton, Yajing Rong, Koc Kan Ho, Michael Ohlmeyer, David Diller
  • Publication number: 20110184002
    Abstract: The invention is related to methods of preventing and treating hepatic fibrosis using A2B adenosine receptor antagonists and utility in the treatment and prevention of liver damage caused by alcohol abuse, surgical intervention, viral hepatitis, the ingestion of hepatotoxic drugs, or other hepatic diseases. The invention also relates to pharmaceutical compositions for use in the method.
    Type: Application
    Filed: August 10, 2010
    Publication date: July 28, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Luiz Belardinelli, Dewan Zeng, Hongyan Zhong
  • Publication number: 20110183985
    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: Application
    Filed: December 17, 2010
    Publication date: July 28, 2011
    Inventors: Yun-Long Li, Andrew P. Combs, Eddy W. Yue, Hui-Yin Li
  • Publication number: 20110183992
    Abstract: Provided are therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity or a pharmaceutically acceptable salt thereof; therapeutic and/or preventive agents for migraine which comprise, as an active ingredient, a compound having a selective adenosine A2A receptor antagonistic activity, which has an affinity for the adenosine A2A receptor 10 times or higher than that for the adenosine A1 receptor, or a pharmaceutically acceptable salt thereof; and the like.
    Type: Application
    Filed: July 23, 2009
    Publication date: July 28, 2011
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Junichi Ikeda, Shunji Ichikawa, Masako Kurokawa, Tomoyuki Kanda
  • Publication number: 20110165118
    Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: November 13, 2008
    Publication date: July 7, 2011
    Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
  • Publication number: 20110160162
    Abstract: Disclosed are prodrugs of A2B adenosine receptor antagonists, and their use in treating mammals for various disease states.
    Type: Application
    Filed: January 21, 2011
    Publication date: June 30, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Rao Kalla, Dmitry Koltun, Jeff Zablocki, Elfatih Elzein
  • Patent number: 7968556
    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: October 18, 2007
    Date of Patent: June 28, 2011
    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: 7968544
    Abstract: The present application includes a compound of Formula I or II: or a pharmaceutically acceptable-salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.
    Type: Grant
    Filed: June 26, 2008
    Date of Patent: June 28, 2011
    Assignee: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Randall L. Halcomb