Chalcogen Bonded Directly To Ring Carbon Of The Purine Ring System Patents (Class 544/265)
  • Patent number: 10913742
    Abstract: The invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula (I) as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as respiratory disorders or pain.
    Type: Grant
    Filed: May 23, 2019
    Date of Patent: February 9, 2021
    Assignee: Genentech, Inc.
    Inventors: Huifen Chen, Daniel Shore, Elisia Villemure, Matthew Volgraf, Baihua Hu, Aijun Lu, Andrew Cridland, Stuart Ward, Francis Beaumier, Martin Dery, Robin Larouche-Gauthier
  • Patent number: 10711005
    Abstract: Compound I and a compound II as well as preparation methods therefor and use thereof are disclosed. A newly synthesized compound of formula I is capable of stimulating congenital immunity and cellular immunity for tumor resistance while greatly improving the antitumor effect of ethacrynic acid (EA), and thus an integrated synergistic anti-tumor dual-immunity drug design is explored. The immune response mechanism for resisting melanoma of the compound as shown in the formula I is demonstrated. A compound that is as shown in a formula II and is prepared from the compound of formula I and ROR1 by means of covalency markedly slows down the growth of subcutaneously transplanted mammary cancer tumor, such that the immune response mechanism, for treating the mammary cancer, of the compound as shown in the formula II is demonstrated.
    Type: Grant
    Filed: November 8, 2016
    Date of Patent: July 14, 2020
    Assignees: SHENZHEN UNIVERSITY, SHENZHEN KANGJUZHENG PHARMACEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Guangyi Jin, Zhulin Wang
  • Patent number: 10597397
    Abstract: The present specification relates to adenine conjugate compounds represented by the formula (1), wherein A, L1, L2, X1, R1, R2, R3, and m are as defined herein, or their pharmaceutically acceptable salts. Compounds of formula (1) have immunostimulating properties and may therefore be useful in therapy, for example as vaccine adjuvants. The present specification also relates to a process for preparing adenine conjugate compounds and pharmaceutically acceptable salts thereof, and to pharmaceutical compositions comprising adenine conjugate compounds and their pharmaceutically acceptable salts.
    Type: Grant
    Filed: September 28, 2016
    Date of Patent: March 24, 2020
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Hitoshi Ban, Yukihiro Nishio, Padma Malyala, Bilikallahalli K. Muralidhara, Marcus Wong
  • Publication number: 20150087643
    Abstract: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity; the compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.
    Type: Application
    Filed: October 10, 2014
    Publication date: March 26, 2015
    Applicant: Advinus Therapeutics Private Limited
    Inventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
  • Patent number: 8969361
    Abstract: Cyclopropanecarboxylate esters of purine analogues, method of making and using the same for treating herpes virus infections and tumors are disclosed.
    Type: Grant
    Filed: April 2, 2013
    Date of Patent: March 3, 2015
    Assignee: Annji Pharmaceutical Co., Ltd.
    Inventors: Ji-Wang Chern, Shin-Yu Lai, Pei-Teh Chang
  • Publication number: 20150045355
    Abstract: Provided are certain fused tricyclic compounds and salts thereof, compositions thereof, and methods of use therefor.
    Type: Application
    Filed: December 31, 2011
    Publication date: February 12, 2015
    Inventors: Changyou Zhou, Shaohui Wang, Guoliang Zhang
  • Patent number: 8946242
    Abstract: Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an effective amount of a spiro[2.4]heptane as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier, are provided. The spiro[2.4]heptane compounds either possess antiviral activity, or are metabolized to a compound that exhibits such activity.
    Type: Grant
    Filed: January 23, 2014
    Date of Patent: February 3, 2015
    Assignee: University of Georgia Research Foundation, Inc.
    Inventor: Chung K. Chu
  • Publication number: 20150011512
    Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.
    Type: Application
    Filed: September 12, 2014
    Publication date: January 8, 2015
    Inventors: Steven Albert Everett, Saraj Ulhaq
  • Patent number: 8921384
    Abstract: Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an effective amount of a spiro[2.4]heptane as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier, are provided. The spiro[2.4]heptane compounds either possess antiviral activity, or are metabolized to a compound that exhibits such activity.
    Type: Grant
    Filed: January 23, 2014
    Date of Patent: December 30, 2014
    Assignee: Unversity of Georgia Research Foundation, Inc.
    Inventor: Chung K. Chu
  • Patent number: 8907086
    Abstract: The present invention is directed to novel bicyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: March 1, 2012
    Date of Patent: December 9, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Chad E. Bennett, Duane A. Burnett, Hongmei Li, Yonggang Chen, Troy McCracken, Monica Vicarel
  • Patent number: 8901136
    Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.
    Type: Grant
    Filed: June 6, 2013
    Date of Patent: December 2, 2014
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Stephen Critchley, Courtney A. Cullis, Steven P. Langston, Hirotake Mitzutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
  • Patent number: 8901135
    Abstract: Substituted bicyclic heteroaryls having the following formula where the variables are as defined herein, 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-pro
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: December 2, 2014
    Assignee: 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: 8859566
    Abstract: The present invention discloses substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, solvates, pharmaceutically acceptable salts, or pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders that may be susceptible to improvement by antagonism of the adenosine receptor, such as asthma, chronic obstructive pulmonary disorder, angiogenesis, pulmonary fibrosis, emphysema, allergic diseases, inflammation, reperfusion injury, myocardial ischemia, atherosclerosis, hypertension, congestive heart failure, retinopathy, diabetes mellitus, obesity, inflammatory gastrointestinal tract disorders, and/or autoimmune diseases.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: October 14, 2014
    Assignee: Advinus Therapeutics Private Limited
    Inventors: Venkata Palle, Vidya Ramdas, Dinesh Barawkar, Sujay Basu, Summon Koul, Yogesh Waman, Meena Patel, Anil Panmand
  • Patent number: 8796290
    Abstract: The present invention provides substituted fused pyrimidine compounds of formula (I), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by adenosine receptor (AR) activity. The present invention also provides processes for preparation of compounds of formula (I).
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: August 5, 2014
    Assignee: Advinus Therapeutics Limited
    Inventors: Vidya Ramdas, Summon Koul, Sujay Basu, Yogesh Waman, Yogesh Shejul, Dinesh Barawkar, Venkata Poornapragnacharyulu Palle
  • Patent number: 8765757
    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: Grant
    Filed: November 13, 2008
    Date of Patent: July 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
  • Publication number: 20140154772
    Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.
    Type: Application
    Filed: November 27, 2013
    Publication date: June 5, 2014
    Applicant: ICOS CORPORATION
    Inventors: Chanchal SADHU, Ken DICK, Jennifer TREIBERG, C. Gregory SOWELL, Edward A. KESICKI, Amy OLIVER
  • Patent number: 8735406
    Abstract: The present invention provides a compound represented by the formula (1) or a pharmaceutically acceptable salt thereof (wherein W represents a hydrogen atom, a halogen atom, or the others; A represents an alkyl group optionally substituted by aryl group or the others, an aryl group, or the others; and one of X and Y represents a di-substituted alkylaminocarbonyl group, or the others, and the other represents a hydrogen atom, an alkyl group, an alkylcarbonyl group, or the others); a medicament or a pharmaceutical composition for treatment or prophylaxis of FAAH-related diseases such as depression, anxiety disorder or pains, comprising the compound or the like as an active ingredient; a use of the compound or the like; and a method for treatment or prophylaxis using the compound or the like.
    Type: Grant
    Filed: September 8, 2010
    Date of Patent: May 27, 2014
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventors: Keiji Adachi, Yoko Nakai, Tomoyuki Furuta, Yuki Fujii
  • Patent number: 8703754
    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: Grant
    Filed: February 8, 2011
    Date of Patent: April 22, 2014
    Assignee: GlaxoSmithKline LLC
    Inventors: Robert Hermann Gibbon, Amanda Lucas, Stephen Andrew Hermitage
  • Patent number: 8680108
    Abstract: The present invention provides fused aryl and heteroaryl derivatives of Formula I: wherein X, V, Y, U, W, Z, R1, R2, Cy, and Ar are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.
    Type: Grant
    Filed: December 17, 2010
    Date of Patent: March 25, 2014
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, Andrew P. Combs, Eddy W. Yue, Hui-Yin Li
  • Patent number: 8673926
    Abstract: Compounds, methods, and compositions for the treatment of infections in or exposure to humans and other host animals of Flaviviridae viruses, including HCV, that includes the administration of an effective amount of a spiro[2.4]heptane as described herein or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable carrier, are provided. The spiro[2.4]heptane compounds either possess antiviral activity, or are metabolized to a compound that exhibits such activity.
    Type: Grant
    Filed: February 14, 2013
    Date of Patent: March 18, 2014
    Assignee: University of Georgia Research Foundation, Inc.
    Inventor: Chung K. Chu
  • Patent number: 8642607
    Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
    Type: Grant
    Filed: November 9, 2011
    Date of Patent: February 4, 2014
    Assignee: Rhizen Pharmaceuticals SA
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V.S. Vakkalanka
  • Publication number: 20140031539
    Abstract: The present invention relates to certain purines, which act as topoisomerase II catalytic inhibitors. These compounds are useful in combination with topoisomerase II poisons, such as anthracyclines and epipodophyllotoxins, in the treatment of proliferative conditions (e.g., cancer). These compounds are useful in the treatment of tissue damage associated with extravasation of a topoisomerase II poison, such as an anthracycline or an epipodophyllotoxin.
    Type: Application
    Filed: July 3, 2013
    Publication date: January 30, 2014
    Applicant: Biocodex, Inc
    Inventors: Lars Hollund JENSEN, Maxwell SEHESTED
  • Patent number: 8609860
    Abstract: The present invention relates to a compound comprising an imine bond as an acid-labile trigger group, the use of such an imine bond as an acid-labile trigger group, a process of cleaving the imine bond in said compound, and a pharmaceutical composition comprising said compound.
    Type: Grant
    Filed: June 21, 2010
    Date of Patent: December 17, 2013
    Assignee: KTB Tumorforschungsgesellschaft mbH
    Inventors: André Warnecke, Ivonne Müller
  • Publication number: 20130306955
    Abstract: A specific nitrogen-containing heterocyclic compound having a urea structure, an electron transporting material containing the nitrogen-containing heterocyclic compound, and an organic electroluminescence device including a light emitting layer and an electron transporting layer between a cathode and an anode in which the electron transporting layer includes the electron transporting material or the nitrogen-containing heterocyclic derivative. An organic EL device exhibiting high emission efficiency even at low voltage and a material for organic EL devices are described.
    Type: Application
    Filed: February 1, 2012
    Publication date: November 21, 2013
    Applicant: IDEMITSU KOSAN CO., LTD.
    Inventors: Sayaka Mizutani, Takayasu Sado, Hiroki Ishida
  • Patent number: 8586739
    Abstract: Substituted bicyclic heteroaryls having the general structure: 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.
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: November 19, 2013
    Assignee: Amgen Inc.
    Inventors: Yi Chen, Timothy D. Cushing, Jason A. Duquette, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Brian S. Lucas, Lawrence R. McGee, Andreas Reichelt, Robert M. Rzasa, Jennifer L. Seganish, Youngsook Shin, Dawei Zhang
  • Patent number: 8552011
    Abstract: The present application relates to anti-viral selenopurine compounds of formula (I): wherein R1 is C2-6alkyl, and pharmaceutically acceptable salts, solvates, and prodrugs thereof. These 6-(C2-6alkylseleno)purine compounds find use in the treatment of neural measles virus infection and associated diseases (namely, multiple sclerosis or neural measles). A particularly preferred compound is ethylselenopurine or ESP.
    Type: Grant
    Filed: June 4, 2009
    Date of Patent: October 8, 2013
    Inventor: William G. Tucker
  • Patent number: 8518885
    Abstract: A novel class of peptide ?-ketoamides useful for selectively inhibiting calpains, selectively inhibiting cysteine proteases, and generally inhibiting all cysteine proteases, having the formula M-AA2-AA1-CO—NH—(CH2)n—R3. Processes for the synthesis of peptidyl ?-ketoamide derivatives. Compositions and methods for inhibiting cysteine proteases, inhibiting calpains, and treating disease caused by cysteine proteases and calpains are provided.
    Type: Grant
    Filed: July 16, 2008
    Date of Patent: August 27, 2013
    Assignees: Georgia Tech Research Corporation, Emory University
    Inventors: James C. Powers, Jonathan D. Glass, Asli Ovat, Zhaozhao Li
  • Patent number: 8501724
    Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.
    Type: Grant
    Filed: April 30, 2012
    Date of Patent: August 6, 2013
    Assignee: Pharmacyclics, Inc.
    Inventors: Wei Chen, David J. Loury
  • Patent number: 8501735
    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: Grant
    Filed: October 29, 2010
    Date of Patent: August 6, 2013
    Assignee: Palau Pharma, S.A.
    Inventors: Carmen Almansa Rosales, Jorge Salas Solana, Robert Soliva Soliva, Sergio Rodriguez Escrich, Maria Cristina Sicre González
  • Publication number: 20130184240
    Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like; m is an integer of 0 to 3; R2 is hydrogen, or substituted or unsubstituted alkyl; X is —O—; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.
    Type: Application
    Filed: September 8, 2011
    Publication date: July 18, 2013
    Applicant: Shionogi & Co., Ltd.
    Inventors: Keisuke Tonogaki, Akira Ino, Eiichi Kojima, Manabu Katou, Masafumi Iwatsu, Nobuyuki Tanaka, Masahiko Fujioka
  • Patent number: 8486902
    Abstract: The present invention provides hydroxyl, keto, and glucuronide derivatives of 3-(4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-3-cyclopentylpropanenitrile.
    Type: Grant
    Filed: October 8, 2010
    Date of Patent: July 16, 2013
    Assignee: Incyte Corporation
    Inventors: James D. Rodgers, Adam Shilling, Argyrios G. Arvanitis, Stacey Shepard, Laurine G. Galya, Mei Li, Frank M. Nedza
  • Publication number: 20130079323
    Abstract: Novel gyrase inhibitors and related compositions and methods are useful for impeding bacterial growth.
    Type: Application
    Filed: September 10, 2010
    Publication date: March 28, 2013
    Applicant: TRIUS THERAPEUTICS, INC.
    Inventors: Christopher J. Creighton, Leslie William Tari, Zhiyong Chen, Mark Hilgers, Thanh To Lam, Xiaoming Li, Michael Trzoss, Junhu Zhang, John Finn, Daniel Bensen
  • Patent number: 8378044
    Abstract: Provided is a low-cost, environmentally friendly living radical polymerization catalyst having high activity. The catalyst is used for a living radical polymerization method, and contains a central element consisting of oxygen and at least one halogen atom bound to the central element. Furthermore, an alcohol compound can be used as a catalyst precursor. By polymerizing a monomer in the presence of the catalyst, a polymer having narrow molecular weight distribution can be obtained, and the cost of the living radical polymerization can be remarkably reduced. The present invention is significantly more environmentally friendly and economically excellent than conventional living radical polymerization methods, due to advantages of the catalyst such as low toxicity of the catalyst, low amount of the catalyst necessary, high solubility of the catalyst, mild reaction conditions, and no coloration/no odor (which do not require a post-treatment for a molded article), and the like.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: February 19, 2013
    Assignee: Kyoto University
    Inventors: Atsushi Goto, Takeshi Fukuda, Yoshinobu Tsujii
  • Patent number: 8372852
    Abstract: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: February 12, 2013
    Assignee: Ardea Biosciences, Inc.
    Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton
  • Patent number: 8362244
    Abstract: The present invention relates to a method for producing a nucleoside derivative represented by formula (2), comprising the step of reducing a nucleoside of formula (1) in the presence of a noble metal catalyst comprising a carrier and a noble metal supported thereby, selected from the group consisting of (A) a homogeneously supported catalyst where the specific surface area of the noble metal is 95.0 m2/g or more and the particle size of the noble metal is 4.3 nm or less, and (B) a surface-loaded catalyst where the specific surface area of the noble metal is 56.0 m2/g or more and the particle size of the noble metal is 8.0 nm or less, wherein R1 is hydrogen or a protective group, R2 is NH2 or OH, R3 is an acyl group, and X is a chlorine or bromine atom. According to the present invention, the yield can be made equal even when the amount of catalyst is smaller than that used for the conventional products.
    Type: Grant
    Filed: July 25, 2007
    Date of Patent: January 29, 2013
    Assignee: Ajinomoto Co., Inc.
    Inventors: Satoji Takahashi, Mitsuhiko Kojima, Shouichi Kondou, Tatsuya Ishikawa, Yoshinori Ogawa
  • Patent number: 8329926
    Abstract: The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: July 27, 2005
    Date of Patent: December 11, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Constantine G. Boojamra, Kuei-Ying Lin, Richard L. Mackman, David Y. Markevitch, Oleg V. Petrakovsky, Adrian S. Ray, Lijun Zhang
  • Publication number: 20120302748
    Abstract: The disclosure relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. Also provided are pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. Provided are methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1B1 and allelic variants thereof. Finally, provided is a method for determining the efficacy of a compound as described herein in treating cancer.
    Type: Application
    Filed: February 28, 2012
    Publication date: November 29, 2012
    Applicant: THE UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEE
    Inventors: Steven Albert Everett, Saraj Ulhaq
  • Patent number: 8318701
    Abstract: The invention is related to phosphorus substituted anti-viral inhibitory compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: July 26, 2005
    Date of Patent: November 27, 2012
    Assignee: Gilead Sciences, Inc.
    Inventors: Constantine G. Boojamra, Kuei-Ying Lin, Richard L. Mackman, David Y. Markevitch, Oleg V. Petrakovsky, Adrian S. Ray, Lijun Zhang
  • Publication number: 20120277256
    Abstract: Embodiments of the present disclosure include a coordination complex, comprising a first biologically active moiety, a second biologically active moiety, and a metal, wherein the first biologically active moiety and second biologically active moiety are bound to the metal by covalent coordination bonds, and wherein the first biologically active moiety and second biologically active moiety are different. These complexes may enhance the pharmacodynamic properties of biologically active moieties.
    Type: Application
    Filed: July 5, 2012
    Publication date: November 1, 2012
    Applicant: Synthonics, Inc.
    Inventors: Thomas Piccariello, Scott B. Palmer, John D. Price, Robert Oberlender, Mary C. Spencer, Michaela E. Mulhare
  • Patent number: 8288526
    Abstract: The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: October 16, 2012
    Assignee: Ajinomoto Co., Inc.
    Inventors: Takayoshi Torii, Kunisuke Izawa, Doo Ok Jang, Dae Hyan Cho
  • Publication number: 20120225869
    Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cannabinoid Receptor 1 (CB1).
    Type: Application
    Filed: March 8, 2012
    Publication date: September 6, 2012
    Applicant: IRM LLC
    Inventors: Hong Liu, Xiaohui He, Ha-Soon Choi, Kunyong Yang, David H. Woodmansee, Zhicheng Wang, David Archer Ellis, Boagen Wu, Yun He, Truc Ngoc Nguyen
  • 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
  • Patent number: 8252920
    Abstract: The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).
    Type: Grant
    Filed: July 30, 2010
    Date of Patent: August 28, 2012
    Assignee: Ajinomoto Co., Inc.
    Inventors: Takayoshi Torii, Kunisuke Izawa, Doo Ok Jang, Dae Hyan Cho
  • Publication number: 20120190639
    Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.
    Type: Application
    Filed: April 30, 2010
    Publication date: July 26, 2012
    Applicant: UNIVERSITY COURT OF THE UNIVERSITY OF DUNDEE
    Inventors: Steven Albert Everett, Saraj Ulhaq
  • 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
  • Patent number: 8222257
    Abstract: Compounds and compositions are provided for treatment, prevention, or amelioration of a variety of medical disorders associated with viral infections and/or cell proliferation. The compounds provided herein are 5-phosphono-pent-2-en-1-yl nucleosides and esters thereof.
    Type: Grant
    Filed: March 30, 2006
    Date of Patent: July 17, 2012
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Hyunah Choo
  • Patent number: 8217050
    Abstract: The invention provides a compound which is (a) an amino acid derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate or solvate thereof: wherein R1, R2, L1, Het, A, x, y and W are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.
    Type: Grant
    Filed: November 5, 2007
    Date of Patent: July 10, 2012
    Assignee: Chroma Therapeutics Limited
    Inventors: David Festus Charles Moffat, Simon Christopher Hirst, Stuart Thomas Onions
  • 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
  • Publication number: 20120172591
    Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.
    Type: Application
    Filed: February 17, 2012
    Publication date: July 5, 2012
    Applicant: ICOS CORPORATION
    Inventors: Chanchal Sadhu, Ken Dick, Jennifer Treiberg, C. Gregory Sowell, Edward A. Kesicki, Amy Oliver
  • Patent number: 8207178
    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: December 12, 2008
    Date of Patent: June 26, 2012
    Assignee: Ardea Biosciences, Inc.
    Inventors: Alex Shaginian, Samedy Ouk, Jean-Michel Vernier, Anthony B. Pinkerton