Pteridines (including Hydrogenated) Patents (Class 544/257)
  • Patent number: 10328078
    Abstract: The invention provides compounds effective as inhibitors of monocarboxylate transporters such as MCT1 and MCT4, which can be used for treatment of medical conditions wherein treatment of the condition with a compound having an inhibitor effect on MCT1, MCT4, or both is medically indicated. Compounds of the invention can have antitumor, antidiabetes, anti-inflammatory, or immunosuppressive pharmacological effects, and can be effective for treatment of cancer and of type II diabetes.
    Type: Grant
    Filed: January 22, 2016
    Date of Patent: June 25, 2019
    Assignee: The Scripps Research Institute
    Inventors: Thomas D. Bannister, Hui Wang, Chao Wang, John L. Cleveland
  • Patent number: 10272087
    Abstract: The invention relates to new pteridine derivative compounds, of formula (I), to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: July 6, 2016
    Date of Patent: April 30, 2019
    Assignee: ASTEX THERAPEUTICS LTD
    Inventors: Gordon Saxty, Christopher Charles Frederick Hamlett, Valerio Berdini, Christopher William Murray, Patrick René Angibaud, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet
  • Patent number: 9233175
    Abstract: The present disclosure relates to compounds that are useful as near-infrared fluorescence probes, wherein the compounds include i) a pteroyl ligand that binds to a target receptor protein, ii) a dye molecule, and iii) a linker molecule that comprises an amino acid or derivative thereof. The disclosure further describes methods of imaging of inflammatory diseases using the compounds.
    Type: Grant
    Filed: December 19, 2013
    Date of Patent: January 12, 2016
    Assignee: Purdue Research Foundation
    Inventors: Philip S. Low, Sumith A. Kularatne, Lindsay E. Kelderhouse, Sakkarapalayam M. Mahalingam
  • Patent number: 9126996
    Abstract: The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: September 8, 2015
    Assignee: JANUS BIOTHERAPEUTICS, INC.
    Inventors: Grayson B. Lipford, Charles M. Zepp
  • Publication number: 20150126502
    Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
    Type: Application
    Filed: January 14, 2015
    Publication date: May 7, 2015
    Inventors: Robert A. GALEMMO, Dean R. ARTIS, Xiaocong Michael YE, Danielle Aubele, Anh TRUONG, Simeon BOWERS, Roy K. Hom, Yong-Liang ZHU, R. Jeffrey NEITZ, Jennifer SEALY, Marc ADLER, Paul BEROZA, John P. ANDERSON
  • Publication number: 20150018349
    Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: March 27, 2014
    Publication date: January 15, 2015
    Applicant: University of Utah Research Foundation
    Inventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
  • Patent number: 8895735
    Abstract: A preparation process of (6R)-tetrahydrobiopterin hydrochloride is provided, which comprises hydrogenating L-biopterin in the presence of a catalyst of Pt group metal in the basic substrate containing solvent, potassium hydroxide and potassium dihydrogen phosphate to obtain (6R)-tetrahydrobiopterin hydrochloride, wherein the pH value of the basic substrate is controlled by potassium hydroxide and potassium dihydrogen phosphate in the range of about 10 to about 13.
    Type: Grant
    Filed: November 15, 2010
    Date of Patent: November 25, 2014
    Assignee: Innopharmax, Inc.
    Inventors: Zhen Wang, Dongbing Zhao, Weida Wang, Jingbo Lan, Jinsong You
  • Patent number: 8895568
    Abstract: The present disclosure relates to 1- or 2-(4-(aryloxy)-phenyl)ethylamino-oxy- or sulfanyl) pteridines and 1- or 2-(4 Jheteroaryloxy)-phenyl)ethylamino-, oxy- or sulfanyl)pteridines and their use as agrochemicals and animal health products. The disclosure provides compounds of Formula (I-A) and Formula (I-B).
    Type: Grant
    Filed: May 20, 2013
    Date of Patent: November 25, 2014
    Assignee: Dow AgroSciences, LLC.
    Inventors: William K. Brewster, David A. Demeter, W. Randal Erickson, Christian T. Lowe, Carla J. R. Klittich, Jaime S. Nugent, Brent J. Rieder, Thomas L. Siddall, Chenglin Yao, Carla N. Yerkes, Yuanming Zhu
  • Publication number: 20140303157
    Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.
    Type: Application
    Filed: August 27, 2012
    Publication date: October 9, 2014
    Inventors: William J. Hoekstra, Robert J. Schotzinger
  • Patent number: 8835451
    Abstract: The present invention provides organic compounds of the following structure; A-L1-B-C-D-L2-E that are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.
    Type: Grant
    Filed: March 28, 2007
    Date of Patent: September 16, 2014
    Assignee: Novartis AG
    Inventors: Michael H. Serrano-Wu, Young-Shin Kwak, Wenming Liu
  • Publication number: 20140256922
    Abstract: The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.
    Type: Application
    Filed: May 16, 2014
    Publication date: September 11, 2014
    Inventors: Sunil David, Nikunj M. Shukla
  • 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
  • Patent number: 8722905
    Abstract: Disclosed is a dye, having a chemical formula: wherein each R1 is independently selected from hydrogen, —(CxH2x+1), —(CyH2y)—S—(CxH2x+1), or —(CyH2y)—N(CxH2x+1)2; Ar1 is wherein each R2 is independently selected from —(CxH2x+1), —(CxH2x)—S—(CxH2x+1), or (CxH2x)—N(CxH2x+1)2; Ar2 is wherein each R3 is independently selected from hydrogen, —(CxH2x+1), —(CyH2y)—S—(CxH2x+1), or —(CyH2y)—N(CxH2x+1)2; X is sulfur, oxygen, selenium, or N—R4, and R4 is —(CxH2x+1); m is in integer of 1 to 4; x is an integer of 1 to 20; and y is an integer of 0 to 20. The dye can be applied to a photoelectric conversion device.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: May 13, 2014
    Assignee: Industrial Technology Research Institute
    Inventors: Yao-Shan Wu, Yung-Liang Tung, Jen-An Chen, Chun-Guey Wu, Jheng-Ying Li
  • Patent number: 8658652
    Abstract: The present invention provides combinations of active agents, such combinations comprising one or more antifolate compounds. The particularly can include methotrexate and one or more further antifolate compounds. In specific embodiments, the combinations are useful for treating certain conditions, such as rheumatoid arthritis. The invention also provides articles useful to provide the combinations in desirable dosage forms and combinations. The combinations further may be useful in the treatment of further conditions, including abnormal cell proliferation, inflammatory diseases, asthma, and arthritis.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: February 25, 2014
    Assignee: Chelsea Therapeutics, Inc.
    Inventors: Michael J. Roberts, Gerry Rowse
  • Publication number: 20140031546
    Abstract: A hydrodeoxygenation catalyst comprises a metal catalyst, an acid promoter, and a support. The metal catalyst is selected from platinum, palladium, ruthenium, rhenium rhodium, osmium, iridium, nickel, cobalt, molybdenum, copper, tin, or mixtures thereof. The support is a promoted-zirconium material including texture promoters and acid promoters. The hydrodeoxygenation catalyst may be used for hydrodeoxygenation (HDO) of sugar or sugar alcohol in an aqueous solution. In one embodiment the HDO catalyst may be used for HDO of fatty acids such as fatty acid methyl esters (FAME), triglycerols (in plant oil and animal fat), pyrolysis oil, or lignin. The hydrodeoxygenation catalyst for fatty acid process does not require the use of an acid promoter, it is optional.
    Type: Application
    Filed: July 25, 2012
    Publication date: January 30, 2014
    Inventors: Wenqin Shen, Alguo Liu, Wayne Turbeville
  • Patent number: 8618106
    Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: December 31, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steve Durrant
  • Publication number: 20130331376
    Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, E1, E2, R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
    Type: Application
    Filed: August 14, 2013
    Publication date: December 12, 2013
    Applicant: Elan Corporation, Inc.
    Inventors: Robert A. Galemmo, Dean R. Artis, Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
  • Patent number: 8580800
    Abstract: The present invention relates to novel 1,4-diarylpyrimido[4,5-d]pyridazine-2,5-dione derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.
    Type: Grant
    Filed: April 24, 2009
    Date of Patent: November 12, 2013
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Franz Von Nussbaum, Dagmar Karthaus, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig
  • Patent number: 8501749
    Abstract: Disclosed are small molecule inhibitors of the formula (I), which are useful in treating various diseases and conditions involving chymase.
    Type: Grant
    Filed: January 26, 2010
    Date of Patent: August 6, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Xin Guo, Chuk Chui Man, Hidenori Takahashi
  • Publication number: 20130156826
    Abstract: The present invention relates to respiratory formulations comprising a compound of formula (I): and use of said compounds and compositions in treatment, for example in the treatment of an inflammatory disease or a respiratory disorder, in particular an inflammatory mediated and/or virally mediated respiratory disorder such as asthma and COPD or the treatment or prevention of viral infection, for example infection by influenza virus, rhinovirus or RSV. The invention also extends to certain novel compounds of formula (I).
    Type: Application
    Filed: June 17, 2011
    Publication date: June 20, 2013
    Applicant: Respivert Limited
    Inventors: Peter John Murray, Stuart Thomas Onions, Jonathan Gareth Williams, Kevin Joly
  • Patent number: 8461164
    Abstract: The present disclosure relates to 1- or 2-(4-(aryloxy)-phenyl)ethylamino-, oxy- or sulfanyl)pteridines and 1- or 2-(4-(heteroaryloxy)-phenyl)ethylamino-, oxy- or sulfanyl)pteridines and their use as agrochemicals and animal health products. More specifically, the invention provides new compounds of the formula (I-A): wherein: R is H, CH3, phenyl, or a heterocycle comprising a 5 or 6 membered single ring or a fused ring system comprising at least one 5 or 6 membered heterocycle optionally substituted with H, halo, lower alkyl, lower alkoxy, benzyloxy, lower alkenyl, lower alkynyl, haloalkyl, haloalkoxy, NO2, CN, lower alkoxycarbonyl, lower alkylcarbonyl, lower alkyl-SOq, and aldoximes and lower alkyloximes, optionally substituted on oxygen by lower alkyl.
    Type: Grant
    Filed: August 31, 2009
    Date of Patent: June 11, 2013
    Assignee: Dow AgroSciences, LLC.
    Inventors: William K. Brewster, David A. Demeter, W. Randal Erickson, Christian T. Lowe, Carla J. R. Klittich, Jaime S. Nugent, Brent J. Rieder, Thomas L. Siddall, Chenglin Yao, Carla N. Yerkes, Yuanming Zhu
  • Publication number: 20130131050
    Abstract: The present invention provides a compound useful for the prophylaxis or treatment of eicosanoid-associated diseases such as atherosclerosis, atherothrombosis, diabetes, obesity, asthma, fever, pain, cancer, rheumatism, osteoarthritis, atopic dermatitis and the like, and having superior pharmacological action, physicochemical properties and the like. The present invention relates to a compound represented by the following formula: wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: July 22, 2011
    Publication date: May 23, 2013
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Nobuyuki Matsunaga, Hideo Suzuki, Kouhei Asano, Hidekazu Tokuhara, Takeshi Yamamoto, Rei Okamoto
  • Patent number: 8445675
    Abstract: Disclosed are storage stable aqueous infusible or injectable solutions containing an active substance of general formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and in the specification, and an amount of a physiologically acceptable acid or mixture of acids sufficient to dissolve the active substance and act as a stabilizer, optionally together with other formulating excipients suitable for parenteral administration, and a process for preparing the infusible or injectable solutions according to the invention.
    Type: Grant
    Filed: February 6, 2009
    Date of Patent: May 21, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Detlef Mohr, Claus Veit, Fridtjof Traulsen
  • Patent number: 8436002
    Abstract: The present invention provides AKT inhibitors of the formula: Formula I The present invention also provides pharmaceutical compositions comprising compounds of Formula I, uses of compounds of Formula I and method of using compounds of Formula I.
    Type: Grant
    Filed: October 20, 2010
    Date of Patent: May 7, 2013
    Assignee: Eli Lilly and Company
    Inventors: Douglas Wade Beight, Timothy Paul Burkholder, Joshua Ryan Clayton, MariJean Eggen, Kenneth James Henry, Jr., Deidre Michelle Johns, Saravanan Parthasarathy, Huaxing Pei, Mark Edward Rempala, Jason Scott Sawyer
  • Patent number: 8334316
    Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.
    Type: Grant
    Filed: February 9, 2009
    Date of Patent: December 18, 2012
    Assignee: ACEA Biosciences, Inc.
    Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
  • Patent number: 8293899
    Abstract: The present invention relates to a process for preparing stereoisomerically enriched 3-heteroaryl-3-hydroxycarboxylic esters by reducing 3-heteroaryl-3-oxocarboxylic esters in the presence of ruthenium-containing catalysts.
    Type: Grant
    Filed: February 27, 2003
    Date of Patent: October 23, 2012
    Assignee: Lanxess Deutschland GmbH
    Inventors: Boris Bosch, Markus Eckert, Hans-Christian Militzer, Claus Dreisbach
  • Patent number: 8278297
    Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.
    Type: Grant
    Filed: December 23, 2010
    Date of Patent: October 2, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven Durrant
  • Patent number: 8252787
    Abstract: In one aspect, the invention provides compounds of Formula I or pharmaceutically acceptable salts thereof. In another aspect, the invention provides methods for treatment of diseases or disorders mediated by a protein kinase, comprising administering a therapeutically effective amount of a compound of this invention.
    Type: Grant
    Filed: December 23, 2010
    Date of Patent: August 28, 2012
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jean-Damien Charrier, Steven Durrant
  • Publication number: 20120202690
    Abstract: The present invention relates to substituted heterobicyclic carboxylic acid derivatives, as well as N-oxides and agriculturally acceptable salts thereof, and their use in controlling plant growth, particularly undesirable plant growth, in crops of useful plants. The invention extends to herbicidal compositions comprising such compounds, N-oxides and/or salts as well as mixtures of the same with one or more further active ingredients and/or a safener.
    Type: Application
    Filed: October 8, 2010
    Publication date: August 9, 2012
    Applicant: SYNGENTA LIMITED
    Inventors: William Guy Whittingham, Caroline Louise Winn, Julie Evelyne Blanc, Shuji Hachisu, Matthew Brian Hotson, Harry Glithro
  • Patent number: 8183247
    Abstract: The present invention relates to novel boron comprising compounds, to pharmaceutical compositions comprising said compounds, to the therapeutic use of said compounds, and to a process for preparation of said compounds. The compounds are useful in boron neutron capture therapy (BNCT).
    Type: Grant
    Filed: August 17, 2006
    Date of Patent: May 22, 2012
    Assignee: Hammercap AB
    Inventors: Lars-Inge Olsson, Erwan Arzel, Arne Eek
  • Publication number: 20120108597
    Abstract: Disclosed are small molecule inhibitors of the formula (I), which are useful in treating various diseases and conditions involving chymase.
    Type: Application
    Filed: January 26, 2010
    Publication date: May 3, 2012
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Xin Guo, Chuk Chui Man, Hidenori Takahashi
  • Patent number: 8039617
    Abstract: A method for selectively producing stable alpha form crystals of sapropterin hydrochloride is provided. In this method, the alpha form crystal of sapropterin hydrochloride is produced by dissolving sapropterin hydrochloride with hydrochloric acid at a concentration of not less than 4 mol/L at not less than 70 degrees C.; adding heated ethanol to the solution; and cooling the solution at a cooling rate of not faster than 3 degrees C./min to a temperature of 40 to 55 degrees C. to precipitate the crystals.
    Type: Grant
    Filed: April 13, 2006
    Date of Patent: October 18, 2011
    Assignees: Shiratori Pharmaceutical Co., Ltd., Daiichi Sankyo Company, Limited
    Inventors: Katsumi Hotoda, Hiroomi Kiyono, Shinnosuke Tazawa
  • Publication number: 20110212942
    Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
    Type: Application
    Filed: December 21, 2010
    Publication date: September 1, 2011
    Inventors: Robert A. Galemmo, Dean R. Artis, Xiaocong Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
  • Publication number: 20110207716
    Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, E1, E2, R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.
    Type: Application
    Filed: December 21, 2010
    Publication date: August 25, 2011
    Inventors: Robert A. Galemmo, Dean R. Artis, Xiaocong Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
  • Publication number: 20110165118
    Abstract: The present invention relates to 3-Heterocyclic Substituted Indole Derivatives, compositions comprising at least one 3-Heterocyclic Substituted Indole Derivative, and methods of using the 3-Heterocyclic Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: November 13, 2008
    Publication date: July 7, 2011
    Inventors: Tin-Yau Chan, Jose S. Duca, Liwu Hong, Charles A. Lesburg, Brian A. McKittrick, Haiyan Pu, Li Wang, Henry M. Vaccaro
  • Patent number: 7968556
    Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1, R3, R4, L, X, Y, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.
    Type: Grant
    Filed: October 18, 2007
    Date of Patent: June 28, 2011
    Assignee: Signal Pharmaceuticals, LLC
    Inventors: Deborah Sue Mortensen, Maria Mercedes Delgado Mederos, John Joseph Sapienza, Ronald J. Albers, Steven Spencer Clareen, Kimberly Lyn Schwarz, Jason Simon Parnes, Jennifer R. Riggs, Patrick William Papa, Sayee Gajanan Hegde, Jeffrey Mark McKenna
  • Patent number: 7960394
    Abstract: This invention provides a compound or its pharmaceutically-acceptable salt of formula (I) wherein R1 represents a lower alkyl group et al; R2 and R3 are same and different and represents hydrogen atm et al; R4 represents the substituent of the formula (II) et al; X1 represents NH, O or S; Y represents N or C; Ar is a divalent substituent derived from aryl et al, by removing two hydrogen atoms therefrom; the ring A represents a 5- or 6-membered heteroaryl group; this compounds has a histamine-H3 receptor antagonistic effect or a histamine-H3 receptor inverse-agonistic effect and is useful for preventive or remedy of metabolic system diseases, circulatory system diseases or nervous system diseases.
    Type: Grant
    Filed: May 30, 2005
    Date of Patent: June 14, 2011
    Assignee: Banyu Pharmaceutical Co., Ltd.
    Inventors: Takashi Mizutani, Tsuyoshi Nagase, Nagaaki Sato, Akio Kanatani, Shigeru Tokita
  • Publication number: 20110059976
    Abstract: The present invention provides compounds having the formula: wherein A-B together represent one of the following structures: and n, R1, R2, R3, R4, L1, L2, Y and Z are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as inhibitors of protein kinase (e.g., RAF), and thus are useful, for example, for the treatment of RAF mediated diseases.
    Type: Application
    Filed: July 26, 2010
    Publication date: March 10, 2011
    Inventors: Johan D. Oslob, Jiang Zhu, Kenneth Barr, Jennifer Cossrow, Brian Raimundo, Hiroko Tanaka
  • Patent number: 7888359
    Abstract: The invention relates to antibiotic cyclohexyl or piperidinyl carboximide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl; one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRX, RX being a halogen atom; either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH?CH or CH2CH2; each of R3, R4, R5, R6, R7, and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9—COOH is naturally occurring amino acid or dimethylaminoglycine; and to salts of such compounds of formula (I).
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: February 15, 2011
    Assignee: Actelion Pharmaceutical Ltd.
    Inventors: Christian Hubschwerlen, Rueedi Georg, Jean-Philippe Surivet, Cornelia Zumbrunn Acklin
  • Patent number: 7875716
    Abstract: The invention relates to compounds of the formula I, or pharmaceutically acceptable salts thereof: wherein: Z=O or S; n=1-3; R3=—CO2R8, —C(O)SR8, —C(O)NHR8, —C(S)OR8, —C(S)SR8, —C(S)NHR8, —C(NH)SR8 or —C(NH)NHR8, wherein R8 is —H or alkyl; R4=—H, —CH2R5 or —CH2CH2R5, wherein R5 independently has one of the meanings of R3; B=—NR2—, —CH2NR2—, —CH2CH2NR2—, —CH2CHR7— or —CH2O—, wherein R2 is H or a C1-3 alkyl, alkenyl or alkynyl group, and R7 is H or a C1-3 alkyl or alkoxy group; wherein R1=—NH2 or —OH, and C and D are each, independently, a 5- or 6-membered, substituted or unsubstituted, aromatic or non-aromatic ring which may also contain one or more heteroatoms, and C is connected to group B in any available position.
    Type: Grant
    Filed: April 7, 2008
    Date of Patent: January 25, 2011
    Inventor: Dan Stoicescu
  • Patent number: 7875612
    Abstract: A cell population expressing folate receptors is selectively targeted with a non-peptide folic acid analogue. The non-peptide folic acid analogue is conjugated to a diagnostic or therapeutic agent to enable selective delivery of the agent to the targeted cell population.
    Type: Grant
    Filed: April 24, 2002
    Date of Patent: January 25, 2011
    Assignees: Purdue Research Foundation, Endocyte, Inc.
    Inventors: Mark A. Green, Chun-Yen Ke, Christopher P. Leamon
  • Publication number: 20100228026
    Abstract: The invention provides a sulfonyl malonamide derivative, or a pharmacologically acceptable salt thereof or a solvate thereof, that has therapeutic and/or preventive effect(s) on various diseases due to its agonist action at AT2 receptor, and is useful as a pharmaceutical agent for the treatment and/or prevention of diseases involving the renin-angiotensin-aldosterone system (RAAS).
    Type: Application
    Filed: June 19, 2008
    Publication date: September 9, 2010
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Tomohiro Yoshida, Hiroshi Sakashita, Atsushi Numata, Saori Tahara, Hisashi Kawasumi
  • Patent number: 7767687
    Abstract: The present invention provides compounds having the formula: wherein A-B together represent one of the following structures: n, R1, R2, R3, R4, L1, L2, Y and Z are as defined in classes and subclasses herein, and pharmaceutical compositions thereof, as described generally and in subclasses herein, which compounds are useful as inhibitors of protein kinase (e.g., RAF), and thus are useful, for example, for the treatment of RAF mediated diseases.
    Type: Grant
    Filed: December 12, 2005
    Date of Patent: August 3, 2010
    Assignees: Biogen Idec MA Inc., Sunesis Pharmaceuticals, Inc.
    Inventors: Johan D. Oslob, Jiang Zhu, Kenneth Barr, Jennifer Cossrow, Brian Raimundo, Hiroko Tanaka
  • Patent number: 7750009
    Abstract: The invention relates to new pteridines which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.
    Type: Grant
    Filed: November 18, 2005
    Date of Patent: July 6, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Horst Dollinger, Juergen Mack, Domnic Martyres, Birgit Jung, Peter Nickolaus
  • Patent number: 7750152
    Abstract: Disclosed are dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the pharmaceutical compositions, isomers, intermediates thereof and processes for preparing these dihydropteridinones. The compounds are useful the treatment and/or prevention of cancer, infections, inflammatory and autoimmune diseases.
    Type: Grant
    Filed: November 16, 2007
    Date of Patent: July 6, 2010
    Assignee: Boehringer Ingelheim Pharma GmbH & Co. KG
    Inventors: Matthias Hoffman, Matthias Grauert, Trixi Brandl, Steffen Breitfelder, Christian Eickmeier, Martin Steegmaier, Gisela Schnapp, Anke Baum, Jens Jurgen Quant, Flavio Solca, Florian Colbatzky
  • Patent number: 7718660
    Abstract: The invention relates to compounds of the formula I, or pharmaceutically acceptable salts thereof: wherein: Z=O or S; n=1?3; R3?—CO2R8, —C(O)SR8, —C(O)NHR8, —C(S)OR8, —C(S)SR8, —C(S)NHR8, —C(NH)SR8 or —C(NH)NHR8, wherein R8 is —H or alkyl; R4?.H, —CH2R5 or —CH2CH2R5, wherein R5 independently has one of the meanings of R3; B?—NR2—, —CH2NR2—, —CH2CH2NR2, —CH2CHR7— or —CH2O—, wherein R2 is H or a C1-3 alkyl, alkenyl or alkynyl group, and R7 is H or a C13 alkyl or alkoxy group; A= wherein R1?—NH2 or —OH, and C and D are each, independently, a 5- or 6-membered, substituted or unsubstituted, aromatic or non-aromatic ring which may also contain one or more heteroatoms, and C is connected to group B in any available position.
    Type: Grant
    Filed: August 16, 2006
    Date of Patent: May 18, 2010
    Inventor: Dan Stoicescu
  • Patent number: 7662820
    Abstract: Provided herein is dipterinyl calcium pentahydrate (DCP) and therapeutic methods based thereon. Also provided herein is the compound dipterinyl calcium pentahydrate (DCP) or an analog or polymorph thereof.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: February 16, 2010
    Assignee: SanRX Pharmaceuticals, Inc.
    Inventors: Phillip Moheno, Wolfgang Pfleiderer
  • Publication number: 20090298840
    Abstract: Disclosed are hydrates and polymorphs of 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, processes for preparing them and their use as pharmaceutical compositions.
    Type: Application
    Filed: June 4, 2009
    Publication date: December 3, 2009
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Guenter LINZ, Peter SIEGER, Gerd F. KRAEMER, Rolf HERTER, Matthias HOFFMANN, Werner RALL, Rolf SCHMID
  • Patent number: 7626019
    Abstract: Disclosed are processes for the preparation of fused piperazin-2-one derivatives of general formula (I) wherein the groups R1 to R5, A1 and A2 have the meanings given in the claims and in the description, particularly the preparation of 7,8-dihydro-5H-pteridin-6-one derivatives and intermediates thereof.
    Type: Grant
    Filed: May 16, 2007
    Date of Patent: December 1, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Adil Duran, Guenter Linz
  • Patent number: RE43115
    Abstract: Disclosed are processes for the preparation of fused piperazin-2-one derivatives of general formula (I) wherein the groups R1 to R5, A1 and A2 have the meanings given in the claims and in the description, particularly the preparation of 7,8-dihydro-5H-pteridin-6-one derivatives and intermediates thereof.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: January 17, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Adil Duran, Guenter Linz