Nitrogen Attached Directly At 2-position By Nonionic Bonding Patents (Class 544/320)
  • Patent number: 9296697
    Abstract: The invention relates to the hetaryl-substituted guanidine compounds of general formula (I), enantiomeres, diastereomeres and/or tautomeres thereof, in addition to the pharmaceutically acceptable salts thereof and the prodrugs of the known compounds. The invention also relates to the use of said hetaryl-substituted guanidine compounds as binding partners for 5-HT5-receptors for treating and/or for the prophylaxis of illnesses which are modulated by a 5-HT5-receptor activity, in particular, for treating and/or for the prophylaxis of neurodegenerative and neuropsychiatric disorders, and signs, symptoms and dysfunctions associated with said disorders.
    Type: Grant
    Filed: August 23, 2006
    Date of Patent: March 29, 2016
    Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KG
    Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Charles W. Hutchins, Francisco Javier Garcia-Ladona, Wolfgang Wernet, Alfred Hahn
  • Patent number: 9040699
    Abstract: The present invention relates to the preparation of cyclopropane derivatives, in particular 2-amino-9-[[(1S,2R)-1,2-bis(hydroxymethyl)cyclopropyl]methyl]-4,8-dihydro-1H-purin-6-one, especially via the [(1S,7R)-4-phenyl-3,5-dioxabicyclo[5.1.0]octan-1-yl]methanol intermediate.
    Type: Grant
    Filed: November 10, 2011
    Date of Patent: May 26, 2015
    Assignee: Aratana Therapeutics NV
    Inventors: Eleonora Kiss, Erwin Blomsma, Serge De Bruijn, E. J. N. Remy Litjens
  • Publication number: 20150141446
    Abstract: Pyrimidine compounds and their use in controlling pests such as insects and other invertebrates are provided. Further embodiments, forms, objects, features, advantages, aspects and benefits shall become apparent from the description.
    Type: Application
    Filed: November 19, 2014
    Publication date: May 21, 2015
    Inventors: Tony K. Trullinger, Timothy C. Johnson, Ricky Jim Hunter
  • Patent number: 9006433
    Abstract: The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: April 18, 2011
    Date of Patent: April 14, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Changyou Zhou, Wuxin Zou, Yuxia Hua, Qun Dang
  • Patent number: 8980904
    Abstract: The present invention pertains to the field of medical technology, and particularly relates to a heterocyclic substituted pyrimidine compound represented by General Formula (I) and its pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description, the present invention also relates to a preparation method of the compound, a pharmaceutical composition containing the compound, and a use of the compound and the pharmaceutical composition in preparation of a medicine for enhancing a cGMP signal transduction function or a medicine for treating or preventing sexual dysfunction and diseases with lower urinary tract symptoms.
    Type: Grant
    Filed: July 19, 2012
    Date of Patent: March 17, 2015
    Assignee: Xuanzhu Pharma Co., Ltd.
    Inventors: Yongqian Wu, Aichen Wang
  • Patent number: 8969510
    Abstract: Fluorinated supramolecular polymers containing at least 5% by weight of covalently bonded fluorine atoms, based on total weight of the polymers are disclosed. The polymers comprise a fluorinated polymer chain and a (self-)complementary unit capable of forming at least three hydrogen bonds being covalently bonded to the fluorinated polymer chain. Also disclosed are materials comprising (a) a fluorinated supramolecular polymer and (b) a non-fluorinated polymer and/or (c) a fluorinated compound, the non-fluorinated polymer being a polymer containing less than 5% by weight of covalently bonded fluorine atoms, based on the total weight of the non-fluorinated polymer, and the fluorinated compound being either a low molecular weight fluorinated compound comprising at least one fluorine atom and having a molecular weight of 34 to 600 amu, or a fluoropolymer containing at least 5% by weight of covalently bonded fluorine atoms and a Mn from about 600 to about 5000.
    Type: Grant
    Filed: November 22, 2011
    Date of Patent: March 3, 2015
    Assignee: SupraPolix B.V.
    Inventor: Anton Willem Bosman
  • Patent number: 8952025
    Abstract: The present disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof: compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.
    Type: Grant
    Filed: April 2, 2013
    Date of Patent: February 10, 2015
    Assignee: Arizona Board of Regents, A Body Corporate of the State of Arizona Acting for and on Behalf of Arizona State University
    Inventors: Sidney Hecht, Omar Khdour, Jun Lu, Pablo Arce
  • Publication number: 20150011574
    Abstract: The present invention provides a compound which enhances the production of erythropoietin. The present invention provides a compound represented by the formula (1) wherein R1: an aromatic hydrocarbon ring group or an aromatic heterocyclic group; R2: a hydrogen atom, an alkyl group, or a heterocycloalkyl group; R3: a hydrogen atom or an alkyl group; A: a hydrogen atom or a hydroxy group; L: —NHCO— or —OCH2—; and X: a nitrogen atom or ?CH—.
    Type: Application
    Filed: September 24, 2014
    Publication date: January 8, 2015
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Tatsuya NISHI, Naoki TANAKA, Ryoko KITAZAWA, Riki GOTO, Takashi ISHIYAMA
  • Patent number: 8916578
    Abstract: Pyrimidine compounds and their use in controlling pests such as insects and other invertebrates are provided. Further embodiments, forms, objects, features, advantages, aspects and benefits shall become apparent from the description.
    Type: Grant
    Filed: April 3, 2014
    Date of Patent: December 23, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: Tony K. Trullinger, Timothy C. Johnson, Ricky Jim Hunter
  • Patent number: 8906906
    Abstract: The present invention relates to a series of novel compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutical amount of such compounds, optionally combined with one or more other drugs having antiviral activity.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: December 9, 2014
    Assignee: Katholieke Universiteit Leuven
    Inventors: Patrick Chaltin, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Wim Smets, Arnout Voet, Frauke Christ
  • Publication number: 20140357616
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.
    Type: Application
    Filed: July 28, 2014
    Publication date: December 4, 2014
    Inventors: Thomas D. Penning, Keith W. Woods, Chunqiu Lai, Alan S. Florjancic, Yunsong Tong
  • Patent number: 8883812
    Abstract: The present invention relates to compounds of Formula (I) as described herein or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof and methods of treating, or manufacture of a medicament to treat, a disease, disorder, or condition of the central nervous system, including bipolar disorder, depressive disorders, anxiety disorders, cognitive disorders, pain disorders, urogentital disorder, and epilepsy, among the other diseases, disorders or conditions discussed herein as mono-therapy or in combination with another active pharmaceutical ingredient.
    Type: Grant
    Filed: June 20, 2011
    Date of Patent: November 11, 2014
    Assignee: Pfizer Inc.
    Inventors: Michelle Marie Claffey, Jennifer Elizabeth Davoren, John Adams Lowe, III, Robert Joseph Mather
  • Patent number: 8877766
    Abstract: The neuroprotective multifunctional antioxidants are compounds that contain a 2-diacetylamino-5-hydroxypyrimidine moiety, having the structural formula: wherein R1 is CH2 or C2H4; R2 is H or —OR4 where R4 is H or aryl; and R3a and R3b are independently selected from the group consisting of H and —O-alkyl. The antioxidants are orally bioavailable metal-attenuating multifunctional antioxidants that can independently attenuate transition metals, as well as scavenger free radicals. The multifunctional antioxidant compounds, by their ability to independently chelate metals, such as Fe, Cu or Zn, and scavenge free radicals generated from different sources, are neuroprotective and are beneficial for the treatment of various neurological disorders, such as Alzheimer's disease, Parkinson's disease, ALS, traumatic brain injury, ocular disorders, such as cataract, glaucoma, age-related macular degeneration and other retinal degeneration, as well as for reducing the progression of diabetic complications.
    Type: Grant
    Filed: February 15, 2013
    Date of Patent: November 4, 2014
    Inventor: Peter F. Kador
  • Patent number: 8865898
    Abstract: A nucleoside analog and a salt thereof represented by any of the general formulae (1) to (10) below: wherein R1, R2, and R3 are the same or different groups, and each of the R1, R2 and R3 is selected from a hydrogen atom, a protecting group for a functional group in nucleic acid synthesis, a phosphate group, a phosphate group protected by a protecting group in nucleic acid synthesis, and an activated phosphate group for solid phase synthesis; and Ar is one of an aromatic hydrocarbon group and a polyaromatic hydrocarbon group.
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: October 21, 2014
    Assignee: Japan Science and Technology Agency
    Inventor: Yoshihito Ueno
  • Publication number: 20140275085
    Abstract: Described are compounds of Formula I which find utility in the treatment of cancer, autoimmune diseases and metabolic bone disorders through inhibition of c-FMS (CSF-1R), c-KIT, and/or PDGFR kinases. These compounds also find utility in the treatment of other mammalian diseases mediated by c-FMS, c-KIT, or PDGFR kinases.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Deciphera Pharmaceuticals, LLC
    Inventors: Michael D. Kaufman, Daniel L. Flynn, YuMi Ahn, Lakshminarayana Vogeti, Timothy Malcolm Caldwell
  • Publication number: 20140256756
    Abstract: Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X1, X2, X3, L, R3, R4, R5, R7 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.
    Type: Application
    Filed: October 30, 2012
    Publication date: September 11, 2014
    Inventors: Thomas Daniel Aicher, Josef Roland Benscik, Steven Armen Boyd, Kevin Ronald Condroski, Jay Bradford Fell, John Peter Fischer, Ronald Jay Hinklin, Scott Pratt, Ajay Singh, Timothy M. Turner
  • Patent number: 8822446
    Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1a, R1b, R1c, X, and Y are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as Cdc7 and methods of treating diseases such as cancer.
    Type: Grant
    Filed: April 14, 2011
    Date of Patent: September 2, 2014
    Assignee: AbbVie Inc.
    Inventors: Thomas D. Penning, Keith W. Woods, Chunqiu Lai, Yunsong Tong, Alan S. Florjancic
  • Patent number: 8815882
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: August 26, 2014
    Assignee: Genentech, Inc.
    Inventors: Charles Baker-Glenn, Daniel Jon Burdick, Mark Chambers, Bryan K. Chan, Huifen Chen, Anthony Estrada, Zachary Kevin Sweeney
  • Publication number: 20140235858
    Abstract: The neuroprotective multifunctional antioxidants are compounds that contain a 2-diacetylamino-5-hydroxypyrimidine moiety, having the structural formula: wherein R1 is CH2 or C2H4; R2 is H or —OR4 where R4 is H or aryl; and R3a and R3b are independently selected from the group consisting of H and —O-alkyl. The antioxidants are orally bioavailable metal-attenuating multifunctional antioxidants that can independently attenuate transition metals, as well as scavenger free radicals. The multifunctional antioxidant compounds, by their ability to independently chelate metals, such as Fe, Cu or Zn, and scavenge free radicals generated from different sources, are neuroprotective and are beneficial for the treatment of various neurological disorders, such as Alzheimer's disease, Parkinson's disease, ALS, traumatic brain injury, ocular disorders, such as cataract, glaucoma, age-related macular degeneration and other retinal degeneration, as well as for reducing the progression of diabetic complications.
    Type: Application
    Filed: February 15, 2013
    Publication date: August 21, 2014
    Inventor: PETER F. KADOR
  • Publication number: 20140228368
    Abstract: The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Application
    Filed: August 20, 2012
    Publication date: August 14, 2014
    Inventors: Christopher D. Cox, Vadim Y. Dudkin, Jeffrey Kern, Mark E. Layton, Izzat T. Raheem
  • Publication number: 20140221408
    Abstract: Pyrimidine compounds and their use in controlling pests such as insects and other invertebrates are provided. Further embodiments, forms, objects, features, advantages, aspects and benefits shall become apparent from the description.
    Type: Application
    Filed: April 3, 2014
    Publication date: August 7, 2014
    Applicant: Dow AgroSciences, LLC
    Inventors: Tony K. Trullinger, Timothy C. Johnson, Ricky Jim Hunter
  • Publication number: 20140221637
    Abstract: A nucleoside analog and a salt thereof represented by any of the general formulae (1) to (10) below: wherein R1, R2, and R3 are the same or different groups, and each of the R1, R2 and R3 is selected from a hydrogen atom, a protecting group for a functional group in nucleic acid synthesis, a phosphate group, a phosphate group protected by a protecting group in nucleic acid synthesis, and an activated phosphate group for solid phase synthesis; and Ar is one of an aromatic hydrocarbon group and a polyaromatic hydrocarbon group.
    Type: Application
    Filed: November 30, 2011
    Publication date: August 7, 2014
    Inventor: Yoshihito Ueno
  • Publication number: 20140221362
    Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.
    Type: Application
    Filed: February 4, 2014
    Publication date: August 7, 2014
    Applicant: Bayer CropScience AG
    Inventors: Thomas BRETSCHNEIDER, Martin Füßlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria FRANKEN, Arnd VOERSTE
  • Patent number: 8791049
    Abstract: Provided are improved agricultural processes for the improved cultivation of rice wherein the crops are treated to control undesired vegetative growth using a plant treatment composition comprising both halosulfuron and thifensulfuron to provide improved herbicidal efficacy against Heteranthera limosa, commonly referred to as “duck salad”. Also provided are compositions useful in the improved agricultural processes, as well as herbicidal treatment regimens. Unexpectedly high rates of efficacy against Heteranthera limosa, amongst rice plant in rice crops are disclosed.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: July 29, 2014
    Assignee: Gowan Co.
    Inventors: Eric Paige Webster, Dominic Frank Alonso, Sergio Comparini, Wallace Keith Majure, Sandra Alcaraz, Charles Paul Grasso, Eric James McEwen, Tak Wai Cheung
  • Patent number: 8785465
    Abstract: Pyrimidine compounds and their use in controlling pests such as insects and other invertebrates are provided. Further embodiments, forms, objects, features, advantages, aspects and benefits shall become apparent from the description.
    Type: Grant
    Filed: October 25, 2013
    Date of Patent: July 22, 2014
    Assignee: Dow AgroSciences, L.L.C.
    Inventors: Tony K. Trullinger, Timothy C. Johnson, Ricky Hunter
  • Patent number: 8785464
    Abstract: The present invention includes compounds of general formula (1) wherein A, X, R1 and R2 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 medicament having the above-mentioned properties.
    Type: Grant
    Filed: October 9, 2013
    Date of Patent: July 22, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heinz Stadtmueller, Bodo Betzemeier, Ioannis Sapountzis
  • Patent number: 8772482
    Abstract: Compounds of formula I are disclosed, as well as compositions comprising them and methods of their use to treat, prevent and/or manage diseases and disorders:
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: July 8, 2014
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Arokiasamy Devasagayaraj, Haihong Jin, Zhi-Cai Shi, Ashok Tunoori, Ying Wang, Chengmin Zhang
  • Patent number: 8772483
    Abstract: Solid forms of (S)-2-amino-3-(4-(2-amino-6-((R)-1-(4-chloro-2-(3-methyl-1H-pyrazol-1-yl)phenyl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)phenyl)propanoic acid and salts thereof are disclosed. Pharmaceutical dosage forms and methods of their use are also disclosed.
    Type: Grant
    Filed: November 3, 2011
    Date of Patent: July 8, 2014
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Qun Li, Weifeng Hu, Xiaogen Yang, Jiangqiong Zhao, Matthew Mangzhu Zhao
  • Patent number: 8772302
    Abstract: The present invention relates to novel GPR 119 agonists of the general Formula (I), their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, stereoisomers, and polymorphs. The invention also relates to processes for the preparation of the compounds of the invention, pharmaceutical compositions containing the compounds and to methods for treating one or both of diabetes and obesity using the compounds of the invention. The present invention is directed to G-protein coupled receptor (GPCR) agonists that are useful for the treatment of obesity, diabetes and related metabolic disorders.
    Type: Grant
    Filed: June 17, 2010
    Date of Patent: July 8, 2014
    Assignee: Cadila Healthcare Limited
    Inventors: Harikishore Pingali, Pandurang Zaware, Mukul Jain
  • Publication number: 20140187772
    Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2? are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.
    Type: Application
    Filed: December 24, 2013
    Publication date: July 3, 2014
    Inventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
  • Patent number: 8754213
    Abstract: The present invention relates to a supramolecular compound comprising a low molecular weight, apolar compound, said low molecular weight, apolar compound having a melting point of below 45° C., a molecular weight of about 80 to about 1500 amu and a HLB-value of lower than 8, said low molecular weight, apolar compound bearing a single 4H-unit per molecule. The supramolecular compound according to the present invention may be used in coating, ink, toner, resin, lacquer, adhesive or glue compositions.
    Type: Grant
    Filed: July 6, 2009
    Date of Patent: June 17, 2014
    Assignee: SupraPolix B.V.
    Inventors: Gaby Maria Leonarda Hoorne-van Gemert, Sandrine Chodorowski-Kimmès, Henricus Marie Janssen, Egbert Willem Meijer, Anton Willem Bosman
  • Publication number: 20140134271
    Abstract: Pyrimidine compounds and their use in controlling pests such as insects and other invertebrates are provided. Further embodiments, forms, objects, features, advantages, aspects and benefits shall become apparent from the description.
    Type: Application
    Filed: October 25, 2013
    Publication date: May 15, 2014
    Applicant: Dow AgroSciences LLC
    Inventors: Tony K. Trullinger, Timothy C. Johnson, Ricky Hunter
  • Patent number: 8722883
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: May 13, 2014
    Assignee: AstraZeneca AB
    Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Cherylin Francis Preston, Jeffrey Paul Stonehouse, Neal Michael Smith
  • Patent number: 8703785
    Abstract: The present invention provides a compound which has an effect of inhibiting amyloid-? production and is useful as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-? proteins. The present invention relates to a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein A is optionally substituted carbocyclic diyl or optionally substituted heterocyclic diyl; B is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is a group such as optionally substituted lower alkyl; R2 is a group such as hydrogen; and R3a and R3b are each independently a group such as hydrogen, provided that the following compound is excluded.
    Type: Grant
    Filed: October 22, 2009
    Date of Patent: April 22, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Shuji Yonezawa, Yuuji Kooriyama, Gaku Sakaguchi
  • Patent number: 8686155
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
    Type: Grant
    Filed: June 28, 2011
    Date of Patent: April 1, 2014
    Assignee: Amgen Inc.
    Inventors: Victor J. Cee, Philip R. Olivieri, Laurie Schenkel
  • Patent number: 8658657
    Abstract: The present invention provides a compound which has an effect of inhibiting amyloid-? production and is useful as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-? proteins. The present invention relates to a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein A is optionally substituted carbocyclic diyl or optionally substituted heterocyclic diyl; B is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is a group such as optionally substituted lower alkyl; R2 is a group such as hydrogen; and R3a and R3b are each independently a group such as hydrogen, provided that the following compound is excluded.
    Type: Grant
    Filed: October 22, 2009
    Date of Patent: February 25, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Shuji Yonezawa, Yuuji Kooriyama, Gaku Sakaguchi
  • Patent number: 8633313
    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: Grant
    Filed: December 17, 2010
    Date of Patent: January 21, 2014
    Assignee: Amgen Inc.
    Inventors: Timothy David Cushing, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Youngsook Shin
  • Patent number: 8604033
    Abstract: The present invention relates to novel compounds of Formula (I), wherein M, P, X, A and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
    Type: Grant
    Filed: January 14, 2011
    Date of Patent: December 10, 2013
    Assignee: Addex Pharma S.A.
    Inventor: Christelle Boléa
  • Patent number: 8575338
    Abstract: A compound of formula (A); wherein ring A is an aromatic ring or a heteroaromatic ring; R1 is independently halogen, cyano, etc., each of X1, X2 and X3 is CR2 or nitrogen, R2 is independently hydrogens, etc., n is 0, 1, 2, 3 or 4; -D-Y is —O—CH2COOH, etc, and G is a substituted amino, a substituted heterocyclic group, etc, or a pharmaceutical acceptable salt thereof, has activities of opening BK channels.
    Type: Grant
    Filed: April 8, 2009
    Date of Patent: November 5, 2013
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Yasuyuki Tsuzuki, Miki Hirai
  • Patent number: 8569294
    Abstract: A compound represented by the formula (I), an optically active isomer thereof, or a pharmaceutical acceptable salt thereof: wherein R2 represents a hydrogen or the like; R3 represents methyl group or the like; R20 represents a halogen atom or the like; q represents an integer of 0 to 3; Z represent nitrogen atom, CH, or the like; R4 represents hydrogen or the like; R5 represents hydrogen or the like; R6 represents a substituted alkyloxy and the like; p represents an integer of 0 to 3; X represents bond, CH2, oxygen atom, NH, or the like; any one or more of R5 and R6, R5 and R4, R6 and R4, X and R5, X and R4, X and R6, and R6 and R6 may combine to each other to form a ring, which is used for preventive and/or therapeutic treatment of a disease caused by tau protein kinase 1 hyperactivity such as a neurodegenerative diseases (e.g. Alzheimer disease).
    Type: Grant
    Filed: March 14, 2007
    Date of Patent: October 29, 2013
    Assignees: Mitsubishi Tanabe Pharma Corporation, Sanofi
    Inventors: Kenji Fukunaga, Toshiyuki Kohara, Kazutoshi Watanabe, Yoshihiro Usui, Fumiaki Uehara, Satoshi Yokoshima, Daiki Sakai, Shin-ichi Kusaka, Kazuki Nakayama
  • Publication number: 20130267546
    Abstract: The present disclosure provides biologically active compounds of formula (I): and pharmaceutically acceptable salts thereof: compositions comprising these compounds, and methods of using these compounds in a variety of applications, such as treatment or suppression of diseases associated with decreased mitochondrial function resulting in diminished ATP production and/or oxidative stress and/or lipid peroxidation.
    Type: Application
    Filed: April 2, 2013
    Publication date: October 10, 2013
    Applicant: Arizona Board of Regents, a body corporate of the State of Arizona acting for and on behalf of Ari
    Inventors: Sidney HECHT, Omar KHDOUR, Jun LU, Pablo ARCE
  • Publication number: 20130253186
    Abstract: Heteroaryloxyheterocyclyl 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, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.
    Type: Application
    Filed: May 10, 2013
    Publication date: September 26, 2013
    Applicant: Amgen Inc.
    Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
  • Patent number: 8518937
    Abstract: Disclosed embodiments provide pyrimidinediamine compounds useful for inhibiting kinase activity, including the activity of polo-like kinase 1 (PLK1). Also disclosed are pharmaceutical compositions comprising these compounds and methods of treating diseases associated with kinase activity, in particular enhanced PLK1 catalytic activity, such as diseases associated with abnormal cell proliferation, including neoplastic disorders.
    Type: Grant
    Filed: September 11, 2012
    Date of Patent: August 27, 2013
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Andy Atuegbu, John Ramphal, Hui Li, Marina Gelman, Jeffrey Clough, Carlos Valdez, Somasekhar Bhamidipati, Sambaiah Thota, Darren McMurtrie
  • Publication number: 20130210807
    Abstract: The present invention describes and claims compounds of the Structural Formula I, Structural Formula II, or Structural Formula III: wherein R1, R2, R3 and R3? are —H or methyl, or R3 and R3 taken together form a double bond, or R3? is —H and R2 and R3 taken together form a spiro-cyclopropyl substituent, R4 is —H or —F, and R5 is —H, methyl, —CI or —Br, Formula II wherein R1 is —H, ethyl-, isopropyl-, cyclopropyl-, methyl- or methoxy-, R4 is —H or —F, and “Y” is: (a) —CH2—; (b) —CR6H-0-CR7R8—, wherein R6, R7, and R8 are independently —H or methyl; (c) —CR6H—N(R9)—CR7R8—, wherein R6, R7, and R8 are independently —H or methyl; (d) —CH2—C(R9)(R10)—C(R7)(R8)—, wherein R7, R8, R9 and R10 are independently —H or -methyl, or both R7 and R8 are —F, R9 and R10 are independently —H or -methyl, or both R9 and R10 are —F, or R9 and R10 taken together are (0=), which together with the carbon to which they are attached forms a carbonyl group.
    Type: Application
    Filed: July 9, 2011
    Publication date: August 15, 2013
    Inventors: Nigel J Liverton, Christelle Boléa, Sylvain Celanire, Yunfu Luo
  • Patent number: 8497064
    Abstract: Nucleic acid labeling compounds are disclosed. The compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.
    Type: Grant
    Filed: November 1, 2011
    Date of Patent: July 30, 2013
    Assignee: Affymetrix, Inc.
    Inventors: Glenn H. McGall, Anthony D. Barone
  • Patent number: 8481731
    Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein X1, X2, X3, X4, Y1, Y2, A, R1, R2, R3, R4, m, n, p, and q are as defined herein, including stereoisomers, esters, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof in a patient in need thereof.
    Type: Grant
    Filed: June 23, 2010
    Date of Patent: July 9, 2013
    Assignees: Boehringer Ingelheim International GmbH, Neurocrine Biosciences, Inc.
    Inventors: Joe A. Tran, Chen Chen
  • Patent number: 8476434
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other proliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.
    Type: Grant
    Filed: November 22, 2010
    Date of Patent: July 2, 2013
    Assignee: Amgen Inc.
    Inventors: Stephanie D. Geuns-Meyer, Brian L. Hodous, Stuart C. Chaffee, Paul Tempest, Ning Xi, Phillip R. Olivieri, Joseph L. Kim, Steven Bellon, Xiaotian Zhu, Yuan Cheng, Brian K. Albrecht, Vinod F. Patel, Victor J. Cee, Karina Romero, Hanh Nho Nguyen, Holly L. Deak, Rebecca E. Johnson
  • Publication number: 20130158021
    Abstract: Described herein are compounds and compositions characterized, in certain embodiments, by conjugation of various groups, such as lipophilic groups, to an amino or amide group of an amino acid, a linear or cyclic peptide, a linear or cyclic polypeptide, or structural isomer thereof, to provide compounds of the present invention, collectively referred to herein as “APPLs”. Such APPLs are deemed useful for a variety of applications, such as, for example, improved nucleotide delivery. Exemplary APPLs include, but are not limited to, compounds of Formula (I), (II), (III), (IV), (V), and (VI), and salts thereof, as described herein: wherein m, n, p, R?, R1, R2, R3, R4, R5, R8, Z, W, Y, and Z are as defined herein.
    Type: Application
    Filed: October 26, 2012
    Publication date: June 20, 2013
    Applicant: Massachusetts Institute of Technology
    Inventor: Massachusetts Institute of Technology
  • Patent number: 8466155
    Abstract: The present invention encompasses compounds of general formulae (1a) and (1b) wherein the groups R1 to R5, A, Q, m, n, p and q are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use as medicaments.
    Type: Grant
    Filed: September 29, 2010
    Date of Patent: June 18, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Heinz Stadtmueller, Ioannis Sapountzis
  • Publication number: 20130150391
    Abstract: The present invention relates to compounds of Formula (I) as described herein or a pharmaceutically acceptable salt thereof, pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof and methods of treating, or manufacture of a medicament to treat, a disease, disorder, or condition of the central nervous system, including bipolar disorder, depressive disorders, anxiety disorders, cognitive disorders, pain disorders, urogentital disorder, and epilepsy, among the other diseases, disorders or conditions discussed herein as mono-therapy or in combination with another active pharmaceutical ingredient.
    Type: Application
    Filed: June 20, 2011
    Publication date: June 13, 2013
    Applicant: PFIZER INC.
    Inventors: Michelle Marie Claffey, Jennifer Elizabeth Davoren, John Adams Lowe, III, Robert Joseph Mather