Nitrogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/311)
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Publication number: 20100222586Abstract: The present invention relates to a process for preparing sulfuric diamides of the general formula I R1R2N—S(O)2—NH2??(I) in which R1 and R2 are each independently a primary alkyl radical having from 1 to 8 carbon atoms, a secondary alkyl radical having from 3 to 8 carbon atoms or a cycloalkyl radical having from 5 to 8 carbon atoms, or, together with the nitrogen atom, form a 5- to 8-membered, saturated nitrogen heterocycle which, as well as the nitrogen atom, may have a further heteroatom selected from O and S as a ring member, where the nitrogen heterocycle is unsubstituted or may have 1, 2, 3 or 4 alkyl groups having in each case from 1 to 4 carbon atoms as substituents.Type: ApplicationFiled: October 10, 2008Publication date: September 2, 2010Inventors: Axel Pleschke, Thomas Schmidt, Joachim Gebhardt, Sandra Loehr, Michael Keil, Jan Hendrik Wevers
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Publication number: 20100222372Abstract: To provide a therapeutic agent for inflammatory bowel disease. The therapeutic agent for inflammatory bowel disease contains, as an active ingredient, a uracil derivative or a pharmaceutically acceptable salt thereof, represented by formula (1).Type: ApplicationFiled: October 10, 2008Publication date: September 2, 2010Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Kazuki Sakamoto, Fumio Nakagawa
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Publication number: 20100216813Abstract: The present invention relates to a compound represented by the following formula I or a pharmaceutically acceptable salt thereof; wherein R1, R2, and y are defined herein. The present invention further relates to compositions that include the compound of the present invention as well as a method of treating a patient from endometreosis or uterine fibroids.Type: ApplicationFiled: November 29, 2006Publication date: August 26, 2010Inventor: James S. Frazee
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Publication number: 20100204471Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with MEK that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.Type: ApplicationFiled: October 22, 2007Publication date: August 12, 2010Applicant: Takeda Pharmaceutical Company LimitedInventors: Qing Dong, Victoria Feher, Stephen W. Kaldor, Naoki Tomita
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Publication number: 20100204182Abstract: The present invention provides ectonucleotidase inhibitors represented by the following formula, including ecto-nucleotide triphosphate diphosphohydrolase (NTPDase) inhibitors and ecto-5?-nucleotidase (ecto-5?-NT) inhibitors, namely nucleotide mimetics as selective NTPDase or ecto-5?-NT inhibitors. It also provides methods for preparations of said compounds. Furthermore provided are pharmaceutical and diagnostic compositions comprising said compounds, and the use of said compounds in a medicament for treating diseases associated with ectonucleotidase activity and/or P1 or P2 receptors.Type: ApplicationFiled: May 24, 2007Publication date: August 12, 2010Applicant: RHEINISCHE FRIEDRICH-WILHELMS-UNIVERSITAT BONNInventors: Christa E. Müller, Andreas Brunschweiger, Jamshed Iqbal
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Publication number: 20100168019Abstract: The present invention relates to prodrug molecules comprising conjugates of an antiproliferative drug, a protease specific cleavable peptide, and, optionally, a targeting peptide, with the prodrugs being substantially inactive prior to degradation of the cleavable sequence by proteolytic enzymes abundant within or in close proximity to the target cancer cell. Also, pharmaceutical compositions of the conjugates and the use of these compositions for treatment of cancer are disclosed.Type: ApplicationFiled: November 23, 2009Publication date: July 1, 2010Inventor: Stela Gengrinovitch
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Publication number: 20100158860Abstract: Compounds having the formula I wherein A, R1, R2, R3, R4a, R4b, R4c, R5, R6, R7a, R7b, Ar1, Rc, Rd, Re, Rf, X, n and p are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: December 14, 2009Publication date: June 24, 2010Inventors: Sandra Steiner, Jim Li, Ryan Craig Schoenfeld, Francisco Xavier Talamas
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Patent number: 7741485Abstract: The invention relates to benzenesulphonamide derivatives of formula (I), methods and intermediate products for production thereof and use of said compounds, or means comprising said compounds for the control of undesired plants and for the desiccation/defoliation of plants.Type: GrantFiled: April 6, 2004Date of Patent: June 22, 2010Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Michael Puhl, Robert Reinhard, Werner Seitz, Cyrill Zagar, Matthias Witschel, Andreas Landes
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Patent number: 7727986Abstract: The present invention relates to 2,5-disubstituted-4-pyrimidinyl-substituted-phenyl-amidine derivatives of formula (I) in which the substituents are as in the description, notably to 2,5-dialkyl-4-pyrimidinyl-substituted-phenyl-amidine derivatives, their process of preparation, their use as fungicide or insecticide active agents, particularly in the form of fungicide or insecticide compositions, and methods for the control of phytopathogenic fungi or damaging insects, notably of plants, using these compounds or compositions.Type: GrantFiled: September 12, 2006Date of Patent: June 1, 2010Assignee: Bayer CropScience AGInventors: Klaus Kunz, Jörg Greul, Oliver Guth, Benoît Hartmann, Kerstin Ilg, Wahed Ahmed Moradi, Thomas Seitz, Jean-Pierre Vors, Peter Dahmen, Arnd Voerste, Ulrike Wachendorff-Neumann, Mark Drewes, Ralf Dunkel, Ronald Ebbert, Herbert Gayer, Peter Lösel, Eva-Maria Franken, Olga Malsam
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Publication number: 20100113413Abstract: Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(arylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acids, show below: wherein the variables are as defined herein, and pharmaceutical compositions thereof, are provided for use as inhibitors of with MEK kinase.Type: ApplicationFiled: January 5, 2010Publication date: May 6, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Qing Dong, Stephen W. Kaldor
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Patent number: 7696218Abstract: Compounds of the substituted 1,3-dialkyl-2,4-dioxo-6-(arylamino)-1,2,3,4-tetrahydropyrimidine-5-hydroxamic acids, show below: wherein the variables are as defined herein, and pharmaceutical compositions thereof, are provided for use as inhibitors of with MEK kinase.Type: GrantFiled: October 22, 2007Date of Patent: April 13, 2010Assignee: Takeda San Diego, Inc.Inventors: Qing Dong, Stephen W. Kaldor
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Patent number: 7687500Abstract: Oxetane-containing nucleosides, particularly non-reducing psiconucleoside oxetanes are described herein. Therapeutic application of these oxetane compounds toward the treatment of nucleoside analog related disorders such as disorders involving cellular proliferation and infection are also described.Type: GrantFiled: January 24, 2008Date of Patent: March 30, 2010Assignee: The University of ConnecticutInventors: Amy R. Howell, Rosa C. Taboada, Stewart K. Richardson
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Publication number: 20100063080Abstract: The present invention relates to compounds of formula (I) and the use of these compounds as pharmaceuticals, e.g. in preventing or treating a CXCR2 receptor mediated condition or disease.Type: ApplicationFiled: November 21, 2007Publication date: March 11, 2010Inventors: Neil John Press, Peter Hunt, David Porter, Diana Janus
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Publication number: 20100041684Abstract: Objects of the present invention are the compounds of formula (I), their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.Type: ApplicationFiled: December 19, 2007Publication date: February 18, 2010Inventors: Guy Georges, Matthias Koerner, Irene Kolm, Ulrike Reiff, Wolfgang Schaefer, Edgar Voss, Stefan Weigand
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Patent number: 7652051Abstract: Heterocyclic compounds derived from benzotriazine, triazines, triazoles and oxadiazoles are disclosed. The methods of synthesis and of use of such heterocyclic compounds are also provided.Type: GrantFiled: August 24, 2005Date of Patent: January 26, 2010Assignee: TargeGen, Inc.Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
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Publication number: 20100016252Abstract: Disclosed are Mannich base N-oxides of drugs containing acidic N—H groups. Pharmaceutical compositions comprising a therapeutically effective amount of Mannich base N-oxides, or a N-oxide rearrangement product, pharmaceutically acceptable salt or prodrug thereof, are also disclosed. Further, disclosed are methods of using the compounds, alone or in combination with one or more other active agents or treatments.Type: ApplicationFiled: September 21, 2009Publication date: January 21, 2010Applicant: State of Oregon Acting By and Through The Oregon State Board of Higher Education On Behalf of The UInventors: John F.W. Keana, Paul Westberg, John Curd, Alshad S. Lalani
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Publication number: 20100008874Abstract: The present invention discloses substituted pyrimidines, processes for their synthesis and their use as effective sun-protecting agents either alone or in combination with other known sun-protecting agents.Type: ApplicationFiled: April 11, 2007Publication date: January 14, 2010Applicant: YISSUM RESEARCH DEVELOPMENT COMPANYInventors: Enk David Claes, Morris Srebnik
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Patent number: 7642303Abstract: Thermoplastic composition and articles containing UV absorbers that protect the articles contents from harmful UV radiation are disclosed as well as methods for making the thermoplastic articles and methods for using the articles to contain and protect materials sensitive to UV radiation. The UV absorbers contain oxazolone and/or azine functional groups that absorb UV radiation and prevent its transmission into the article. Many of the compounds are novel compositions of matter. The generally clear thermoplastic articles of this disclosure are particularly useful for containing a variety of UV sensitive consumer products that would otherwise have to be packaged in opaque containers.Type: GrantFiled: October 13, 2005Date of Patent: January 5, 2010Inventors: Thomas L. Shakely, James John Krutak
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Patent number: 7638520Abstract: Pyrimidone compounds of formula (I): are inhibitors of the enzyme Lp-PLA2 and are of use in treating atheroscelerosis.Type: GrantFiled: November 21, 2006Date of Patent: December 29, 2009Assignee: SmithKline Beecham, plcInventors: Deirdre Mary Bernadette Hickey, Robert John Ife, Colin Andrew Leach, Ivan Leo Pinto, Stephen Allan Smith, Steven James Stanway
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Publication number: 20090306022Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.Type: ApplicationFiled: June 9, 2009Publication date: December 10, 2009Applicants: Trustees of Tufts College, Paratek Pharmaceuticals, Inc.Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Mohamed Ismail, Todd Bowser, Beena Bhatia, David Messersmith, Laura McIntyre, Darrell Koza, Glen Rennie, Paul Sheahan, Paul Hawkins, Atul Verma, Tadeusz Warchol, Upul Bandarage
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Publication number: 20090286755Abstract: To provide a radiation therapy potentiator, which, when employed in combination with cancer radiation therapy, can reduce radiation dose and can mitigate adverse effects. The invention provides a radiation therapy potentiator containing, as an effective ingredient, a uracil derivative represented by formula (1) (wherein R1 represents a halogen atom or a cyano group; and R2 represents a 4- to 8-membered heterocyclic group having 1 to 3 nitrogen atoms and optionally having as a substituent a lower alkyl group, an imino group, a hydroxyl group, a hydroxymethyl group, a methanesulfonyloxy group, or an amino group; an amidinothio group in which a hydrogen atom attached to a nitrogen atom may be substituted by a lower alkyl group; a guanidino group in which a hydrogen atom attached to a nitrogen atom may be substituted by a lower alkyl group or a cyano group; a lower alkylamidino group; or a 1-pyrrolidinylmethyl group) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 28, 2007Publication date: November 19, 2009Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventor: Masakazu Fukushima
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Patent number: 7598379Abstract: The present invention provides processes for making pyridyl-linked-xanthines of formula VII, from 5,6-diamino-1H-pyrimidine-2,4-diones of formula II and acylating agents of formula VI. The xanthines are expected to be are selective antagonists of A2B adenosine receptors (ARs).Type: GrantFiled: February 27, 2006Date of Patent: October 6, 2009Assignee: PGx Health, LLCInventors: Guoquan Wang, Jayson M. Rieger, Robert D. Thompson
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Patent number: 7569575Abstract: The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as ?-L-oxy-LNA, amino-LNA, ?-L-amino-LNA, thio-LNA, ?-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilizing intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.Type: GrantFiled: May 8, 2003Date of Patent: August 4, 2009Assignee: Santaris Pharma A/SInventors: Mads Detlef Sørensen, Jesper Wengel, Troels Koch, Signe M. Christensen, Christoph Rosenbohm, Daniel Sejer Pedersen
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Publication number: 20090176812Abstract: A compound represented by the formula (I): wherein R1 is an oxo group, ?N—R or the like; a group represented by the formula: is a group represented by the formula: R2 is a group represented by the formula: R3 and R4 are each H, or C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, C1-C6 alkylamino, di(C1-C6)alkylamino or C1-C6 alkylthio, each of which is optionally substituted; and R5 is H, or C1-C6 alkyl, C2-C6 alkenyl, cyclic group, each of which is optionally substituted, —CO—R8 or —O—R8?, or a salt thereof. The compound of the present invention is useful as a drug for the prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases.Type: ApplicationFiled: May 2, 2008Publication date: July 9, 2009Inventors: Takanobu Kuroita, Hiroki Sakamoto, Hideyuki Igawa, Minoru Sasaki, Kouhei Asano, Tsuyoshi Maekawa, Koji Fuji
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Publication number: 20090171084Abstract: Aminopyrimidine compounds represented by formula (3) may be efficiently prepared by reacting an azlactone compound represented by formula (1) with an amidine compound represented by formula (2) or a salt thereof: wherein R1, R2 and M are as defined in the specification.Type: ApplicationFiled: December 18, 2008Publication date: July 2, 2009Applicant: Ajinomoto Co., Inc.Inventors: Daisuke Takahashi, Kunisuke Izawa
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Publication number: 20090163457Abstract: The invention relates to codrugs having improved properties, methods for preparing and administering them, and methods of formulating and administering the codrugs as pharmaceutical preparations. In certain embodiments, the codrugs can be locally administered to deliver the constituent biologically active compound in a sustained-release fashion, reducing systemic concentrations of the biologically active compound.Type: ApplicationFiled: November 26, 2008Publication date: June 25, 2009Applicant: pSivida, Inc.Inventors: Paul Ashton, Jianbing Chen, Hong Guo, Grazyna Cynkowska, Tadeusz Cynkowski
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Publication number: 20090163712Abstract: Compounds of Formula (I): can be prepared by a multi-step process from compounds of Formula (II): wherein G is Cl, Br or I.Type: ApplicationFiled: December 17, 2008Publication date: June 25, 2009Applicants: Gilead Sciences, Inc., Korea Research Institute of Chemical TechnologyInventors: Hongyan Guo, Stacey Heumann, Ill Young Lee, Michael L. Mitchell, Steven Pfeiffer, Jong Chan Son
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Publication number: 20090155917Abstract: A method is herein presented for analyzing nucleobases on a single molecular basis (a single molecule detection), which comprises scanning a molecular tip chemically modified with the complementary nucleobase on the nucleobases, and measuring the tunneling currents between the scanned nucleobases and the molecular tips with scanning tunneling microscopy.Type: ApplicationFiled: December 28, 2005Publication date: June 18, 2009Inventors: Yoshio Umezawa, Takahito Ohshiro
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Publication number: 20090137803Abstract: The present invention provides a production method of 5-aminopyrimidine compound represented by the formula (5) by reacting a glycine compound represented by the formula (1) with t-butoxybisdimethylaminomethane, dimethylformamidedimethylacetal or dimethylformamidediethylacetal to produce a dialkylaminomethylene compound represented by the formula (2), reacting the compound of formula (2) in the presence of an acid to produce a hydroxymethylene compound represented by the formula (3), and reacting the compound of formula (3) with an amidine compound represented by the formula (4) or a salt thereof.Type: ApplicationFiled: January 29, 2009Publication date: May 28, 2009Applicant: Ajinomoto Co., Inc.Inventors: Daisuke TAKAHASHI, Kunisuke IZAWA
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Publication number: 20090137457Abstract: This invention relates to novel compounds that are pyrimidinedione derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrimidinedione derivatives that are derivatives of alogliptin. This invention also provides compositions comprising one or more compounds of this invention and a carrier, and the use of the disclosed compound and compositions in methods of treating diseases and conditions that are beneficially treated by administering a dipeptidyl peptidase IV (DPP4) inhibitor.Type: ApplicationFiled: October 2, 2008Publication date: May 28, 2009Applicant: CoNCERT Pharmaceuticals, Inc.Inventor: Scott L. Harbeson
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Publication number: 20090124796Abstract: Provided is a simple and efficient production process of a nucleobase having a perfluoroalkyl group. A nucleobase (for example, uracils, cytosines, adenines, guanines, hypoxanthines, xanthines, or the like) is reacted with a perfluoroalkyl halide in the presence of a sulfoxide, a peroxide and an iron compound to produce a perfluoroalkyl-substituted nucleobase, which is useful as an intermediate for medical drugs, economically.Type: ApplicationFiled: November 6, 2006Publication date: May 14, 2009Inventors: Tetsu Yamakawa, Kyoko Yamamoto, Daisuke Uraguchi, Kenji Tokuhisa
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Patent number: 7521396Abstract: The invention relates to compounds of the formula (I) in which Q, R1, R2, R3, R4, R5, R6, R7 are as defined in the disclosure, to processes for their preparation, and to their use as herbicides.Type: GrantFiled: April 22, 2003Date of Patent: April 21, 2009Assignee: Bayer CropScience AGInventors: Hans-Georg Schwarz, Roland Andree, Dorothee Hoischen, Joachim Kluth, Karl-Heinz Linker, Anton Vidal-Ferran, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
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Publication number: 20090075939Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: June 26, 2008Publication date: March 19, 2009Inventors: Gong-Xin He, Choung U. Kim, Michael L. Mitchell, Lianhong Xu
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Publication number: 20090076045Abstract: Compounds of formula I, wherein R1, X1, X2 and A, are as defined herein or pharmaceutically acceptable salts thereof, inhibit HIV-1 reverse transcriptase and afford a method for prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC. The present invention also relates to compositions containing compounds of formula I useful for the prevention and treatment of HIV-1 infections and the treatment of AIDS and/or ARC.Type: ApplicationFiled: May 30, 2008Publication date: March 19, 2009Inventors: Joshua Kennedy-Smith, Zachary Kevin Sweeney, Jeffrey Wu
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Publication number: 20080318907Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.Type: ApplicationFiled: March 12, 2007Publication date: December 25, 2008Applicant: The Trustees of California State UniversityInventors: Yong Ba, Errol V. Mathias
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Publication number: 20080312183Abstract: Deoxyuridine derivatives of the formula (I) where R1 is H or various substituents; D is —NHCO—, —CONH—, -0-, —C(?O)—, —CH?CH, —C?C—, —NR5—; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl or a stable monocyclic, bicyclic or tricyclic ring system; G is —O—, —S—, —CHR10—, —C(?O)—; J is —CH2—, or when G is CHR10 may also be —O— or —NH—; R10 is H, F, —CH3, —CH2NH2, —CH2OH; —OHR11 is H, F, —CH3, —CH2NH2, —CH2OH, —CH(OH)CH3, CH(NH3)CH3; or R10 and R11 together define an olefinic bond, or together form a —CH2-group, thereby defining a cis or trans cyclopropyl group; have utility in the prophylaxis or treatment of protozoal diseases such as malaria.Type: ApplicationFiled: January 6, 2005Publication date: December 18, 2008Inventors: Ian Gilbert, Corinne Nguyen, Gian Filippo Ruda, Alessandro Schipani, Ganasan Kasinathan, Nils-Gunnar Johansson, Dolores Gonzalez Pacanowska
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Patent number: 7462625Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs 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 for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: September 11, 2006Date of Patent: December 9, 2008Assignee: Neurocrine Biosciences, Inc.Inventors: Yun-Fei Zhu, Chen Chen, Fabio C. Tucci, Zhiqiang Guo, Timothy D. Gross, Martin Rowbottom, R. Scott Struthers
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Publication number: 20080262005Abstract: Compounds having utility as GnRH receptor antagonists and for treatment of a variety of sex-hormone related conditions in both men and women. Such compounds have the following structure (I): (I) wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6, R7, n and X are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of structure (I) in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: ApplicationFiled: May 13, 2005Publication date: October 23, 2008Applicant: NEUROCRINE BIOSCIENCES, INC.Inventors: Yun-Fei Zhu, Zhiqiang Gou, Mi Chen, Liren Zhao
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Patent number: 7419983Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs 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 for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: January 25, 2007Date of Patent: September 2, 2008Assignee: Neurocrine Biosciences, Inc.Inventors: Zhiqiang Guo, Yongsheng Chen, Dongpei Wu, Chen Chen, Warren Wade, Wesley J. Dwight, Charles Q. Huang, Fabio C. Tucci
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Publication number: 20080188501Abstract: Compounds, pharmaceuticals, kits and methods are provided for use with DPP-IV and other S9 proteases that comprise a compound comprising: wherein M is N or CR4; Q1 and Q2 are each independently selected from the group consisting of CO, SO, SO2, and C?NR9; and each L, X, R1, R2, and R3 are as defined herein.Type: ApplicationFiled: October 30, 2007Publication date: August 7, 2008Inventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Bruce J. Elder, Paul K. Isbester, Grant J. Palmer, Jonathon S. Salsbury, Luckner G. Ulysse
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Patent number: 7358239Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 7329669Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R2a, R2b, R3, R4, R5, R6, R7 and X are as defined herein, including stereoisomers, prodrugs 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 for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: June 2, 2006Date of Patent: February 12, 2008Assignee: Neurocrine Biosciences, Inc.Inventors: Yun-Fei Zhu, Collin Regan, Jaimie K Rueter, Zhiqiang Guo, Yongsheng Chen, Charles Q Huang
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Patent number: 7304070Abstract: Disclosed are novel A2B adenosine receptor antagonists having the structure of Formula I or Formula II: The compounds are particularly useful for treating asthma, inflammatory gastrointestinal tract disorders, cardiovascular diseases, neurological disorders, and diseases related to undesirable angiogenesis.Type: GrantFiled: September 16, 2004Date of Patent: December 4, 2007Assignee: CV Therapeutics, Inc.Inventors: Rao Kalla, Thao Perry, Elfatih Elzein, Vaibhav Varkhedkar, Xiaofen Li, Prabha Ibrahim, Venkata Palle, Dengming Xiao, Jeff Zablocki
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Patent number: 7232926Abstract: The present invention relates to a process for preparing sulfamoyl halides of primary or secondary amines, comprising the following steps: i) reacting a primary or secondary amine A1 with at least equimolar amounts of SO3 or an SO3 source in the presence of at least equimolar amounts of a tertiary amine A2, based in each case on the amine A1, and ii) reacting the reaction mixture obtained in step i) with at least the amount of a phosphorus halide required by the stoichiometry; The invention further relates to a process for preparing sulfonic diamides, comprising the preparation of sulfamoyl halides by means of carrying out steps i) and ii) and subsequently reacting the sulfamoyl halide obtained with ammonia. The invention further relates to the use of this process for preparing active herbicidal ingredients having a sulfuric diamide structure. The invention further relates to novel sulfamoyl chlorides.Type: GrantFiled: May 15, 2003Date of Patent: June 19, 2007Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Michael Puhl, Robert Reinhard, Ingo Sagasser, Thomas Schmidt, Norbert Götz, Thomas Zierke
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Patent number: 7229995Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein n, R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs 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 for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: November 1, 2005Date of Patent: June 12, 2007Assignee: Neurocrine Biosciences, Inc.Inventors: Charles Q. Huang, Chen Chen, Yongsheng Chen, Zhiqiang Guo, Warren Wade, Martin Rowbottom, Jaimie K. Rueter
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Patent number: 7202252Abstract: Compounds of the general formula (I) are described: wherein A is a 5- or 6-membered aromatic or heteroaromatic ring. Compositions comprising such compounds and methods of use thereof are also described.Type: GrantFiled: February 17, 2004Date of Patent: April 10, 2007Assignee: Endacea, Inc.Inventors: Constance Neely Wilson, John J. Partridge
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Patent number: 7179815Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein A, Q, R1, R2, R3a, R3b, R4, R5, R6 and n are as defined herein, including stereoisomers, prodrugs 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 for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: December 17, 2004Date of Patent: February 20, 2007Assignee: Neurocrine Biosciences, Inc.Inventors: Yun-Fei Zhu, Chen Chen, Fabio C. Tucci, Zhiqiang Guo, Timothy D. Gross, Martin Rowbottom, R. Scott Struthers
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Patent number: 7176211Abstract: GnRH receptor antagonists are disclosed that have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R2a, R2b, R3, R4, R5, R6 and X are as defined herein, including stereoisomers, prodrugs 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 for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: October 14, 2005Date of Patent: February 13, 2007Assignee: Neurocrine Biosciences, Inc.Inventors: Zhiqiang Guo, Yongsheng Chen, Dongpei Wu, Chen Chen, Warren Wade, Wesley J. Dwight, Charles Q. Huang, Fabio C. Tucci
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Patent number: 7148229Abstract: The present invention is a sulfonamide substituted xanthine derivative of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 is lower alkyl, lower alkyl substituted by phenyl, or lower alkyl substituted by halogen substituted phenyl; R2 is lower alkyl or lower alkyl substituted by lower cycloalkyl; and R3 is: Compounds of formula I and pharmaceutically acceptable salts or prodrugs thereof show activity as modulators of gluconeogenesis.Type: GrantFiled: February 11, 2004Date of Patent: December 12, 2006Assignee: Hoffman-La Roche Inc.Inventors: Peter W. Dunten, Louise H. Foley, Nicholas J. S. Huby, Sherrie L. Pietranico-Cole, Weiya Yun
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Patent number: RE39590Abstract: Novel herbicidal and defoliant substituted aniline derived compounds represented by general structure (I) are described. W, X, Y, Z, and Q are as defined in the disclosure. Also described are the processes for the manufacture of these compounds and agriculturally suitable compositions containing these as active ingredients which are useful as herbicides for general or selective pre-emergent or post-emergent control of undesired plant species and defoliants at very low concentrations of these biologically active compounds.Type: GrantFiled: April 27, 2000Date of Patent: April 24, 2007Assignee: ISK Americas IncorporatedInventors: Sandeep Gupta, Shao-Yong Wu, Masamitsu Tsukamoto, David A. Pulman, Bai-Ping Ying