The Additional Hetero Ring Is Six-membered Consisting Of One Nitrogen And Five Carbons Patents (Class 514/263.22)
  • Patent number: 8404674
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1, R2 and R3 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and their use for preparing a pharmaceutical composition having the above-mentioned properties.
    Type: Grant
    Filed: March 4, 2008
    Date of Patent: March 26, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heinz Stadtmueller, Guido Boehmelt, Harald Engelhardt, Ulrich Hirt, Otmar Schaaf, Irene Waizenegger
  • Publication number: 20130072504
    Abstract: The present invention relates to new crystalline forms of a purine derivative which exhibits excellent anti-tumour activity. The invention also relates to a pharmaceutical composition containing said crystalline forms as an active ingredient, and use thereof in the prevention or treatment of disease. The invention further relates to a process for preparing the crystalline forms.
    Type: Application
    Filed: January 24, 2011
    Publication date: March 21, 2013
    Applicant: CYCLACEL LIMITED
    Inventors: Benjamin Mark Skead, Christopher Peter Worrall, Jonathan Charles Christian Atherton, Julian Scott Northen, Philippe Fernades
  • Publication number: 20130059869
    Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.
    Type: Application
    Filed: February 22, 2012
    Publication date: March 7, 2013
    Inventors: Howard Ng, Manfred Weigele, Magdalene Moran, Jayhong Chong, Christopher Fanger, Glenn R. Larsen, Donato Del Camino, Neil Hayward, Steven P. Adams, Amy Ripka
  • Publication number: 20130053406
    Abstract: The invention provides novel therapeutic compounds, pharmaceutical compositions comprising these compounds, and methods for using these compounds and compositions to treat diseases and disorders such as cancer.
    Type: Application
    Filed: August 23, 2010
    Publication date: February 28, 2013
    Applicant: Myrexis, Inc.
    Inventors: SE-HO KIM, Herbert L. Ley, III, Ashok Bajji
  • 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
  • Publication number: 20130035325
    Abstract: Methods of inhibiting kinases using kinase inhibitors having olefin moieties are disclosed.
    Type: Application
    Filed: November 16, 2010
    Publication date: February 7, 2013
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: John William Taunton, JR., Rebecca Maglathlin, Iana Serafimova, Michael S. Cohen, Rand Miller, Ville Paavilainen, Jesse McFarland, Shyam Krishnan
  • Publication number: 20130029982
    Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.
    Type: Application
    Filed: July 18, 2012
    Publication date: January 31, 2013
    Applicants: INTELLIKINE, LLC, INFINITY PHARMACEUTICALS, INC.
    Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
  • Publication number: 20130029944
    Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.
    Type: Application
    Filed: June 20, 2012
    Publication date: January 31, 2013
    Applicant: Portola Pharmaceuticals, Inc.
    Inventors: Yonghong Song, Qing Xu, Shawn M. Bauer, Zhaozhong J. Jia, Mukund Mehrotra, Anjali Pandey
  • Publication number: 20130012515
    Abstract: A series of fused bicyclic pyridine and pyrazine derivatives, substituted directly on the pyridine or pyrazine ring by a functional group attached via a sulphur-containing linkage, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
    Type: Application
    Filed: November 11, 2010
    Publication date: January 10, 2013
    Applicant: UCB PHARMA S.A.
    Inventors: Gilles Raphy, Roland Bürli, Alan Findlay Haughan
  • Publication number: 20130012526
    Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
    Type: Application
    Filed: April 18, 2011
    Publication date: January 10, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Philippe G. Nantermet, Zhi-Qiang Yang, Constantine Kreatsoulas, Abbas M. Walji, Hong Zhu
  • Publication number: 20130005748
    Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.
    Type: Application
    Filed: September 11, 2012
    Publication date: January 3, 2013
    Applicant: IRM LLC
    Inventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
  • Patent number: 8343961
    Abstract: The present invention relates to substituted heterocyclic compounds and substituted tetrahydroisoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzodiazepine compounds and substituted tetrahydroisoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.
    Type: Grant
    Filed: March 31, 2010
    Date of Patent: January 1, 2013
    Assignee: ArQule, Inc.
    Inventors: Robert Nicewonger, Audra Dalton, Chris Brassard, Mark A. Ashwell, Rocio Palma
  • Publication number: 20120329776
    Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the isoquinolone entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.
    Type: Application
    Filed: November 4, 2011
    Publication date: December 27, 2012
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Troy Edward Wilson
  • Publication number: 20120329747
    Abstract: A patentable new class of hydrazone derivative compounds is described, as are methods for synthesizing such compounds. The hydrazones of the invention can be used, for example, as potent anti-cancer agents, including to inhibit the growth of cancer cells that exhibit multidrug resistance.
    Type: Application
    Filed: June 21, 2012
    Publication date: December 27, 2012
    Inventors: Hiremagular N. JAYARAM, Praveen KUSUMANCHI, Mario GRIFANTINI, Palmarisa FRANCHETTI, Loredana CAPPELLACCI, Riccardo PETRELLI
  • Publication number: 20120315291
    Abstract: The present invention relates to compounds of formula (I): wherein; R1 represents hydrogen or C1-3alkyl; n is an integer having a value of 1 to 5; X represents O or NH; Y represents C or N; or a pharmaceutically acceptable salt thereof, have been shown to be inducers of human interferon and may possess an improved profile with respect to known inducers of human interferon, for example enhanced potency. The compounds of the invention may therefore be useful in the treatment of various disorders, in particular the treatment of infectious diseases, cancer, allergic diseases and other inflammatory conditions, and their use as vaccine adjuvants.
    Type: Application
    Filed: February 8, 2011
    Publication date: December 13, 2012
    Applicant: GLAXOSMITHKLINE LLC
    Inventors: Helene Bazin-Lee, Diane Mary Coe, David A. Johnson, Charlotte Jane Mitchell
  • Publication number: 20120308609
    Abstract: The present invention relates to a compound which is 6-amino-2-{[(1S)-1-methylbutyl]oxy}-9-[5-(1-piperidinyl)pentyl]-7,9-dihydro-8H-purin-8-one: in the form of a maleate salt, 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: February 8, 2011
    Publication date: December 6, 2012
    Applicant: GlaxoSmithKline LLC
    Inventors: Robert Hermann Gibbon, Amanda Lucas, Stephen Andrew Hermitage
  • Publication number: 20120309774
    Abstract: The present invention provides compounds of formulae Ia and Ib: wherein R1-5, Q, X, Y, Z, p, q, and r are as defined herein. The compounds are potent and selective antagonists of A2A adenosine receptors (ARs). The invention further includes pharmaceutical compositions containing these compounds and methods of using the same.
    Type: Application
    Filed: August 16, 2012
    Publication date: December 6, 2012
    Inventors: Anthony BEAUGLEHOLE, Jayson M. RIEGER, Robert D. THOMPSON
  • Patent number: 8324224
    Abstract: Disclosed are novel compounds that are A2B adenosine receptor antagonists, useful for treating various disease states, including asthma and diarrhea.
    Type: Grant
    Filed: June 27, 2011
    Date of Patent: December 4, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
  • Patent number: 8318718
    Abstract: Pyridine and pyrimidine compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Grant
    Filed: November 16, 2009
    Date of Patent: November 27, 2012
    Assignee: Amgen Inc.
    Inventors: Jennifer R. Allen, Biswas Kaustav, Frank Chavez, Ning Chen, Frenel Fils De Morin, James R. Falsey, Michael J. Frohn, Paul E. Harrington, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Roxanne Kunz, Holger Monenschein, Thomas T. Nguyen, Alexander J. Pickrell, Andreas Reichelt, Shannon Rumfelt, Robert M. Rzasa, Kelvin Sham, Guomin Yao
  • Patent number: 8318750
    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: Grant
    Filed: August 26, 2011
    Date of Patent: November 27, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
  • Publication number: 20120289503
    Abstract: A liquid composition that is an aqueous solution of a compound of formula (I), wherein the aqueous solution has a pH from about 3.0 to about 5.0. The liquid composition may be used in the treatment of a disorder selected from hyperproliferative diseases, autoimmune diseases and heart diseases.
    Type: Application
    Filed: January 21, 2011
    Publication date: November 15, 2012
    Applicant: APREA AB
    Inventors: Styrbjorn Bystrom, Charlotta Liljebris, Ninus Caram-Lelham
  • Patent number: 8309555
    Abstract: The present invention provides 2,6-disubstituted purine compounds, compositions and methods for dedifferentiating lineage committed mammalian cells into stem cells. The present invention also provides methods of inducing dedifferentiation of lineage committed mammalian cells into stem cells, which can be further differentiated into various lineage committed cells. Methods of identifying additional 2,6-disubstituted purine compounds useful for inducing dedifferentiation of lineage committed cells into stem cells are also provided.
    Type: Grant
    Filed: September 21, 2009
    Date of Patent: November 13, 2012
    Assignee: The Scripps Research Institute
    Inventors: Shuibing Chen, Sheng Ding, Peter G. Schultz
  • Publication number: 20120277206
    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: Application
    Filed: May 11, 2012
    Publication date: November 1, 2012
    Applicant: Andrea Boesciences, Inc.
    Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
  • Publication number: 20120277257
    Abstract: Disclosed herein are methods of treating diseases and disorders responsive to inhibition of Hsp90, pharmaceutical compositions, pharmaceutical dosage forms and medicaments useful for the treatment of diseases responsive to inhibition of Hsp90, and methods of making the pharmaceutical compositions, pharmaceutical dosage forms and medicaments.
    Type: Application
    Filed: May 14, 2012
    Publication date: November 1, 2012
    Applicant: MYREXIS, INC.
    Inventors: Margaret YU, Daniel A. WETTSTEIN, Vijay R. BAICHWAL, Damon I. PAPAC, Gaylen M. ZENTNER, Mark S. WILLIAMS
  • Patent number: 8288397
    Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
    Type: Grant
    Filed: December 16, 2008
    Date of Patent: October 16, 2012
    Assignee: Janssen Pharmaceutica NV
    Inventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C Rech, Wei Xiao
  • Publication number: 20120258974
    Abstract: Provided are methods of improving the cardiac condition of post-myocardial infarction (MI) patients and reducing cardiovascular death and hospitalization due to heart failure or arrhythmias, by administering a therapeutically effective amount of an A2B adenosine receptor antagonist.
    Type: Application
    Filed: April 5, 2012
    Publication date: October 11, 2012
    Inventors: Luiz Belardinelli, Hongyan Zhong, Dewan Zeng
  • Publication number: 20120252782
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are defined as in claim 1, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: June 15, 2012
    Publication date: October 4, 2012
    Applicant: BOEHRINGER INGELHEIM PHARMA GMBH AND CO. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf R.H. LOTZ
  • Publication number: 20120252783
    Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R4 are as defined herein, the tautomers and the stereoisomers thereof, mixtures thereof, the prodrugs and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Application
    Filed: June 15, 2012
    Publication date: October 4, 2012
    Applicant: BOEHRINGER INGELHEIM PHARMA & CO. KG
    Inventors: Frank HIMMELSBACH, Michael MARK, Matthias ECKHARDT, Elke LANGKOPF, Roland MAIER, Ralf LOTZ
  • Publication number: 20120244121
    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 7, 2012
    Publication date: September 27, 2012
    Applicant: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Randall L. Halcomb
  • Publication number: 20120245169
    Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.
    Type: Application
    Filed: January 13, 2012
    Publication date: September 27, 2012
    Inventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
  • Publication number: 20120245140
    Abstract: N-containing heteroaryl derivatives of formula I or II, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as JAK, particularly JAK3, kinase inhibitors.
    Type: Application
    Filed: October 29, 2010
    Publication date: September 27, 2012
    Inventors: Carmen Almansa Rosales, Jorge Salas Solana, Robert Soliva Soliva, Sergio Rodríguez Escrich, Maria Cristina Sicre Gonzåles
  • Publication number: 20120237508
    Abstract: The present invention relates to HSP90 inhibitors containing fused amino pyridine core that are useful as inhibitors of HSP90 and their use in the treatment of HSP90 related diseases and disorders such as cancer, an autoimmune disease, or a neurodegenerative disease.
    Type: Application
    Filed: March 20, 2012
    Publication date: September 20, 2012
    Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
  • Patent number: 8258142
    Abstract: The present invention provides substituted 8-[6-amino-3-pyridyl]xanthines such as the following: and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: September 4, 2012
    Assignee: Dogwood Pharmaceuticals, Inc.
    Inventors: Guoquan Wang, Robert D. Thompson, Jayson M. Rieger
  • Patent number: 8258141
    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: Grant
    Filed: April 19, 2007
    Date of Patent: September 4, 2012
    Assignee: Novartis AG
    Inventors: Robin Alec Fairhurst, Roger John Taylor, Brian Cox
  • Publication number: 20120220585
    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: May 10, 2012
    Publication date: August 30, 2012
    Applicant: Amgen Inc.
    Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
  • Publication number: 20120220586
    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: May 10, 2012
    Publication date: August 30, 2012
    Applicant: Amgen Inc.
    Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer Seganish, Youngsook Shin, Dawei Zhang
  • Patent number: 8252791
    Abstract: The present invention relates to purine-based cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, inflammatory disorders, hepatic disorders, and a combination thereof.
    Type: Grant
    Filed: August 13, 2009
    Date of Patent: August 28, 2012
    Assignee: Jenrin Discovery, Inc.
    Inventors: John F. McElroy, Robert J. Chorvat
  • Patent number: 8252797
    Abstract: Compounds of the present disclosure are fused pyrimidine compounds of formula (I), its tautomers, polymorphs, stereoisomers, prodrugs, solvate or a pharmaceutically acceptable salts thereof, as Adenosine receptor antagonists. Processes of their preparation are also described in the disclosure.
    Type: Grant
    Filed: March 26, 2009
    Date of Patent: August 28, 2012
    Assignee: Advinus Therapeutics Pvt. Ltd.
    Inventors: Venkata Palle, Sujay Basu, Yogesh Waman, Vidya Ramdas, Dinesh Barawkar, Meena Patel, Anil Panmand
  • Publication number: 20120208829
    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: Application
    Filed: August 22, 2011
    Publication date: August 16, 2012
    Applicant: Neurogen Corporation
    Inventors: Rajagopal Bakthavatchalam, Scott M. Capitosti, Jianjun Xu, Bertrand L. Chenard, Manuka Ghosh, Charles A. Blum
  • Publication number: 20120202785
    Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Application
    Filed: February 8, 2012
    Publication date: August 9, 2012
    Inventors: Robert Heald, Stephen Price, Brian Safina, Pascal Pierre Alexandre Savy, Eileen Mary Seward, Daniel P. Sutherlin, Bohdan Waszkowycz
  • Publication number: 20120196845
    Abstract: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: October 1, 2010
    Publication date: August 2, 2012
    Inventors: Douglas C. Beshore, Scott D. Kuduk, Robert M. Dipardo
  • Patent number: 8232281
    Abstract: The specification describes the use of selected DPP IV inhibitors for the treatment of physiological functional disorders and for reducing the risk of the occurrence of such functional disorders in at-risk patient groups. In addition, the use of the above-mentioned DPP IV inhibitors in conjunction with other active substances is described, by means of which improved treatment outcomes can be achieved. These applications may be used to prepare corresponding medicaments.
    Type: Grant
    Filed: May 4, 2007
    Date of Patent: July 31, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Klaus Dugi, Frank Himmelsbach, Michael Mark
  • Publication number: 20120190697
    Abstract: HIV replication inhibitors of formula wherein -a1=a2-a3=a4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; -b1=b2-b3=b4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; n and m is 0-4, R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; polyhalomethyl; polyhalomethylthio; —S(?O)pR6; C(?NH)R6; R2a is CN; amino; substituted amino; C1-6alkyl; halo; C1-6alkyloxy; carbonyl; —CH?N—NH—C(?O)—R16; C1-6alkyloxyC1-6alkyl; C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X—R7; R3 is CN; amino; C1-6alkyl; halo; C1-6alkyloxy; substituted carbonyl; —CH?N—NH—C(?O)—R16; substituted C1-6alkyl; C1-6alkyloxyC1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7; —X—R7; R4 is halo; OH; C1-6alkyl, C2-6alkenyl or C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; CN; nitro; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; substituted
    Type: Application
    Filed: March 2, 2012
    Publication date: July 26, 2012
    Inventors: Jerôme Emile Georges GUILLEMONT, Mikaël Paugam, Bruno Francois Marie Delest, Jan Heeres, Paulus Joannes Lewi, Frank Xavier Jozef Herwig Arts
  • Publication number: 20120190679
    Abstract: The invention relates to a novel group of compounds of Formula (I) or salts thereof: wherein Y, Z1, Z2, R1, R4, R5 and n are as described in the specification, which may be useful in the treatment or prevention of a disease or medical condition mediated through protein kinase B (PKB) such as cancer. The invention also relates to pharmaceutical compositions comprising said compounds, methods of treatment of diseases mediated by PKB using said compounds and methods for preparing compounds of Formula (I).
    Type: Application
    Filed: December 13, 2011
    Publication date: July 26, 2012
    Applicant: ASTRAZENECA AB
    Inventors: Paul David Johnson, Andrew Leach, Richard William Arthur Luke, Zbigniew Stanley Matusiak, Jeffrey James Morris
  • Patent number: 8227601
    Abstract: This application concerns certain 2-phenylamino-6-aryl amino-, 6-aryloxy-, and 6-arylthio-purines, -azapurines and -deazapurines. These compounds are non-nucleoside reverse transcriptase inhibitors and have potential as anti-HIV treatment.
    Type: Grant
    Filed: May 5, 2006
    Date of Patent: July 24, 2012
    Assignee: Ardea Biosciences, Inc.
    Inventors: Jean-Luc Girardet, Yung-Hyo Koh, Stephanie Shaw, Hong Woo Kim, Zhi Hong
  • Publication number: 20120184569
    Abstract: Disclosed are (N)-methanocarba adenine nucleosides of formulas (I)-(V), for example, of formula (V): as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides exhibit similar selectivities as agonists of the A3 versus the A1 receptor for both human and mouse adenosine receptors, and are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias.
    Type: Application
    Filed: February 10, 2012
    Publication date: July 19, 2012
    Applicant: The United States of America, as represented by the Secretary, Dept. of Health and Human Services
    Inventors: Kenneth A. Jacobson, Dilip K. Tosh
  • Publication number: 20120184568
    Abstract: Polymorphs of chemical compounds that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. Also provided herein are processes for preparing compounds, polymorphs thereof, and pharmaceutical compositions thereof.
    Type: Application
    Filed: January 10, 2012
    Publication date: July 19, 2012
    Inventors: Pingda Ren, Michael Martin, Paul Isbester, Benjamin S. Lane, Jason Kropp
  • Publication number: 20120178716
    Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: December 5, 2011
    Publication date: July 12, 2012
    Applicant: 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: 20120172347
    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: Application
    Filed: September 8, 2010
    Publication date: July 5, 2012
    Applicant: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Keiji Aachi, Yoko Nakai, Tomoyuki Furuta, Yuki Fujii