1,2,4-triazoles (including Hydrogenated) Patents (Class 546/272.4)
  • Patent number: 7998984
    Abstract: The invention provides compounds of formula wherein R1, R3, R4, R5, R6, R14, X and W are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of human neutrophil elastase.
    Type: Grant
    Filed: May 7, 2007
    Date of Patent: August 16, 2011
    Assignee: AstraZeneca AB
    Inventors: Peter Hansen, Karolina Lawitz, Matti Lepistö, Hans Lönn, Asim Ray
  • Publication number: 20110196150
    Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Application
    Filed: February 10, 2011
    Publication date: August 11, 2011
    Inventors: Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
  • Publication number: 20110195930
    Abstract: To provide a novel pesticide. The present invention provides a pesticide which contains, as an active ingredient, novel pyridine derivative represented by the formula (I) or its salt: wherein R1 is alkyl, cycloalkyl, alkoxyalkyl or OR3; R2 is 1H-1,2,4-triazol-1-yl which may be substituted, 1H-imidazol-1-yl which may be substituted, 1H-1,2,3-triazol-1-yl which may be substituted, or 4H-1,2,4-triazol-4-yl which may be substituted; X is alkyl which may be substituted, cycloalkyl which may be substituted, halogen, nitro, etc.; R3 is alkyl which may be substituted, cycloalkyl which may be substituted, alkenyl which may be substituted, alkynyl which may be substituted, etc.; m is an integer of from 1 to 4.
    Type: Application
    Filed: November 6, 2009
    Publication date: August 11, 2011
    Applicant: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Takahiro Haga, Masayuki Morita, Kazuhisa Kiriyama, Kumiko Azuma
  • Patent number: 7989637
    Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted triazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.
    Type: Grant
    Filed: December 17, 2008
    Date of Patent: August 2, 2011
    Assignee: Roche Palo Alto LLC
    Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
  • Publication number: 20110183981
    Abstract: Disclosed are compounds of the Formula I and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R7, R8 and R9, W, X and Y are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer and inflammation, in mammals, and inflammatory conditions. Also disclosed are methods of using such compounds in the treatment of hyperproliferative diseases in mammals and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: March 30, 2011
    Publication date: July 28, 2011
    Applicant: ARRAY BIOPHARMA INC.
    Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
  • Publication number: 20110172276
    Abstract: A carboxamide compound represented by the formula (I): [wherein Q represents a nitrogen-containing 5-membered heterocyclic group optionally fused with a benzene ring, R1 represents a C1-C3 alkyl group or the like, R2 represents a hydrogen atom or the like, and R3 represents a hydrogen atom.] has an excellent plant disease controlling effect.
    Type: Application
    Filed: March 25, 2011
    Publication date: July 14, 2011
    Inventors: Sadayuki Arimori, Yoshiharu Kinoshita
  • Patent number: 7973033
    Abstract: The present invention provides a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Ar1 represents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, Ar2 represents a phenyl group that may be substituted with a C1-6 alkoxy group, or the like, X1 represents a double bond or the like, and Het represents an imidazolyl group that may be substituted with a C1-6 alkyl group, or the like, which is effective as a therapeutic or prophylactic agent for a disease caused by A?.
    Type: Grant
    Filed: January 12, 2011
    Date of Patent: July 5, 2011
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Teiji Kimura, Noritaka Kitazawa, Toshihiko Kaneko, Nobuaki Sato, Koki Kawano, Koichi Ito, Eriko Doi, Mamoru Takaishi, Takeo Sasaki, Takehiko Miyagawa, Hiroaki Hagiwara, Takashi Doko
  • Publication number: 20110152232
    Abstract: Compounds that modulate GHS-R are described, for examples compounds formula (I)
    Type: Application
    Filed: October 26, 2010
    Publication date: June 23, 2011
    Inventors: Jeffrey O. Saunders, Thomas Coulter, Paul Mortenson, Manuel A. Navia, Jean-Francois Pons
  • Patent number: 7960422
    Abstract: Compounds of formula (I) wherein R1 is as well as pharmaceutically acceptable salts, hydrates and/or enantiomers thereof are useful as compounds that exhibit activity at metabotropic glutamate receptors.
    Type: Grant
    Filed: October 17, 2008
    Date of Patent: June 14, 2011
    Assignee: AstraZeneca AB
    Inventors: Erwan Arzel, Louise Edwards, Methvin Isaac, Donald A. McLeod, Abdelmalik Slassi, Tao Xin
  • Patent number: 7947683
    Abstract: The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salt thereof: processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat drug dependency, as antipsychotic agents, to treat obsessive compulsive spectrum disorders, premature ejaculation or cognition impairment.
    Type: Grant
    Filed: April 12, 2006
    Date of Patent: May 24, 2011
    Assignee: Glaxo Group Limted
    Inventors: Giorgio Bonanomi, Anna Checchia, Elettra Fazzolari, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Silvia Terreni
  • Publication number: 20110105460
    Abstract: [Problem] A compound, which can be used for preventing or treating diseases, in which 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1) is concerned, in particular, diabetes, insulin resistance, dementia, schizophrenia and depression, is provided. [Means for Solution] It was found that a triazole derivative, in which one of the 3- and 5-positions of the triazole ring has (di)alkylmethyl or cycloalkyl, each of which is substituted with —O— (aryl or a heterocyclic group, each of which may be substituted, or lower alkylene-cycloalkyl), and the other thereof has aryl, a heterocyclic group or cycloalkyl, each of which may be substituted, or a pharmaceutically acceptable salt thereof exhibits potent 11?-HSD1 inhibitory action. From the above, the triazole derivative of the present invention can be used for preventing or treating diabetes, insulin resistance, dementia, schizophrenia and depression.
    Type: Application
    Filed: July 2, 2009
    Publication date: May 5, 2011
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Seiji Yoshimura, Noriyuki Kawano, Tomoaki Kawano, Daisuke Sasuga, Takanori Koike, Hideyuki Watanabe, Hiroki Fukudome, Nobuyuki Shiraishi, Ryosuke Munakata, Hiroaki Hoshii, Kayoko Mihara
  • Patent number: 7935815
    Abstract: A compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Ar1 represents an imidazolyl group or the like which may be substituted with a C1-6 alkyl group, Ar2 represents a phenyl group or the like which may be substituted with a C1-6 alkoxy group, X1 represents a double bond or the like and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, is effective as a therapeutic or prophylactic agent for a disease caused by A?.
    Type: Grant
    Filed: August 28, 2008
    Date of Patent: May 3, 2011
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Teiji Kimura, Noritaka Kitazawa, Toshihiko Kaneko, Nobuaki Sato, Koki Kawano, Koichi Ito, Mamoru Takaishi, Takeo Sasaki, Yu Yoshida, Toshiyuki Uemura, Takashi Doko, Daisuke Shinmyo, Daiju Hasegawa, Takehiko Miyagawa, Hiroaki Hagiwara
  • Publication number: 20110076230
    Abstract: The present invention relates to novel amyloid binding compounds and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted indole derivatives, compositions, and therapeutic uses and processes for making such compounds.
    Type: Application
    Filed: May 28, 2009
    Publication date: March 31, 2011
    Inventors: James C. Barrow, Scott Harrison, James Mulhearn, Scott Wolkenberg
  • Patent number: 7915295
    Abstract: Compounds of the formula Z: where; A is CH or N; R1 is a substituent to a carbon atom in the ring containing A selected from —S(?O)pRa, where Ra is —C1-C4 alkyl, —ORx, —NRxRx, —NHNRxRx, —NHNHC(?O)ORx, —NRxOH; —C(?O)—Rb, where Rb is —CT-C4-alkyl, ORx, —NRxRx, —NHNRxRx, —NHC1-C3-alkyl-C(?O)Orx —NRxRc, where Rc is H, C1-C4 alkyl, —NRxRx; —C(=0)Rd, —CN, S(?O)pRx, where Rd is Rd is C1-C4-alkyl, —ORx, —NRxRx C1-C3-alkyl-O—C1-C3-alkylC(?O)ORx, —C1-C3-alkyl-COORx; —C1-C3alkyl-OH or C1-C4 alkyl ethers or esters thereof (O—C1-C3alkyl)q-O—Rx a 5 or 6 membered aromatic ring having 1-3 hetero atoms p is 1 or 2; Rx is independently selected from H, C1-C4 alkyl or acetyl; or a pair of Rx can together with the adjacent N atom form a ring; L is -0-, —S(?O)—, or —CH2—, where r is 0, 1 or 2; R3-R7 are substituents as defined in the specification; X is —(CR8R8?)n-D-(CR8R8?)m-; D is a bond, —NR9—, -0-, —S—, —S(=0)- or —S(=0)2-; and pharmaceutically acceptable salts and prodrugs thereof, have utility as HIV antivirals.
    Type: Grant
    Filed: December 30, 2004
    Date of Patent: March 29, 2011
    Assignee: Medivir AB
    Inventors: Christian Sund, Nathalie Roue, Stefan Lindstrom, Dmitry Antonov, Christer Sahlberg, Katarina Jansson
  • Publication number: 20110070297
    Abstract: Compounds, pharmaceutical compositions, kits and methods are provided for use with glucokinase that comprise a compound selected from the group consisting of: wherein the variables are as defined herein.
    Type: Application
    Filed: December 1, 2010
    Publication date: March 24, 2011
    Applicants: Takeda San Diego, Inc., Takeda Pharmaceutical Company Limited
    Inventors: Sheldon X. Cao, Jun Feng, Yasuhiro Imaeda, Stephen L. Gwaltney, David J. Hosfield, Nobuyuki Takakura, Mingnam Tang
  • Publication number: 20110071291
    Abstract: A hydrazide compound represented by the formula (1): (wherein R1, R2, R3, R4, A1, A2, J, Q and n are defined in the specification) has excellent pesticidal activity.
    Type: Application
    Filed: November 19, 2010
    Publication date: March 24, 2011
    Inventors: Hiroshi Ikegami, Markus Jachmann, Yoshihiko Nokura, Chiemi Iwata
  • Publication number: 20110065696
    Abstract: A compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Ar1 represents an imidazolyl group or the like which may be substituted with a C1-6 alkyl group, Ar2 represents a phenyl group or the like which may be substituted with a C1-6 alkoxy group, X1 represents a double bond or the like and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, is effective as a therapeutic or prophylactic agent for a disease caused by A?.
    Type: Application
    Filed: November 19, 2010
    Publication date: March 17, 2011
    Inventors: Teiji KIMURA, Noritaka Kitazawa, Toshihiko Kaneko, Nobuaki Sato, Koki Kawano, Koichi Ito, Mamoru Takaishi, Takeo Sasaki, Yu Yoshida, Toshiyuki Uemura, Takashi Doko, Daisuke Shinmyo, Daiju Hasegawa, Takehiko Miyagawa, Hiroaki Hagiwara
  • Publication number: 20110009410
    Abstract: The present invention relates to compounds of Formula (I): where in X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).
    Type: Application
    Filed: July 12, 2010
    Publication date: January 13, 2011
    Applicant: Gilead Sciences, Inc.
    Inventors: Britton Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, JR., Gregory Notte
  • Publication number: 20110003815
    Abstract: The present invention provides compounds of Formula I which are FLAP inhibitors useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Application
    Filed: October 6, 2008
    Publication date: January 6, 2011
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Bing Li, Lin Chu, Minal Patel, Helen M. Armstrong, Hyun O. Ok, Rosemary Sisco, Dwight MacDonald, John Hutchinson, Helene Perrier
  • Publication number: 20110003806
    Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: January 28, 2010
    Publication date: January 6, 2011
    Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company Limited
    Inventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil
  • Patent number: 7863299
    Abstract: The present invention relates to novel compounds of formula (IC) or a salt thereof: wherein: p is an integer ranging from 0 to 4; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl or SF5; or corresponds to a group R5; m1, m2, m3, and m4 are 0; m5, m6 and m7 are each independently 0, 1 or 2 wherein the sum of m5, m6 and m7 is 1 or 2; R6 is C1-6alkyl; R7 is halogen, C1-6alkyl or haloC1-6alkyl; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is S or —CH2—; R3 is C1-4alkyl; R4 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and C1-4alkanoyl; R5 is isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl or 2-pyrrolidinonyl, wherein eac
    Type: Grant
    Filed: August 18, 2006
    Date of Patent: January 4, 2011
    Assignee: Glaxo Group Limited
    Inventors: Anna Maria Capelli, Elettra Fazzolari, Fabrizio Micheli, Giovanna Tedesco, Silvia Terreni
  • Publication number: 20100330069
    Abstract: 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: Application
    Filed: January 8, 2010
    Publication date: December 30, 2010
    Applicant: TargeGen, Inc.
    Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
  • Publication number: 20100324053
    Abstract: The present invention relates to 1-aryl-3-aniline-5-alkyl-1,2,4-triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to potent positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulator having the capability to increase the efficacy of nicotinic receptor agonists.
    Type: Application
    Filed: March 18, 2009
    Publication date: December 23, 2010
    Inventors: Gregor James MacDonald, Johannes Wilhelmus John F. Thuring, Pauline Carol Stanislawski, Wei Zhuang, Yves Emiel Maria Van Roosbroeck, Frans Alfons Maria Van Den Keybus
  • Patent number: 7851701
    Abstract: A photoelectric conversion device using a semiconductor fine material such as a semiconductor fine particle sensitized with a dye carried thereon, characterized in that the dye is a methine type dye having a specific partial structure, for example, a methine type dye having a specific carboxyl-substituted hetero ring on one side of a methine group and an aromatic residue substituted with a dialkylamino group or an organic metal complex residue on the other side of the methine group, or a methine type dye having a carboxyl-substituted aromatic ring on one side of a methine group and a heteroaromatic ring having a dialkylamino group or an organic metal complex residue on the other side of the methine group; and a solar cell using the photoelectric conversion element. The photoelectric conversion element exhibits a conversion efficiency comparable or superior to that of a conventionally known photoelectric conversion element sensitized with a methine type dye.
    Type: Grant
    Filed: July 5, 2002
    Date of Patent: December 14, 2010
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Masaaki Ikeda, Koichiro Shigaki, Teruhisa Inoue
  • Publication number: 20100267725
    Abstract: The present invention relates to compounds, compositions and methods for treating a disease in an animal, which disease is responsive to inhibiting of functional cystic fibrosis transmembrane conductance regulator (CFTR) polypeptide by administering to a mammal in need thereof an effective amount of a compound defined herein (including those compounds set forth in Table 1 or 2 or encompassed by formula I) or compositions comprising these compounds, thereby treating the disease. The present invention particularly, relates to a method of treating diarrhea and polycystic kidney disease.
    Type: Application
    Filed: April 20, 2010
    Publication date: October 21, 2010
    Inventors: Michael Geoffrey Neil Russell, Kevin James Doyle
  • Publication number: 20100261699
    Abstract: The present invention relates to a compound represented by the formula: or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently a lower alkyl group, X is CH or the like, and X1 is an aminoalkoxy group or the like, which has a glucokinase-activating effect and thus is useful in the treatment of diabetes, obesity, and the like.
    Type: Application
    Filed: December 15, 2008
    Publication date: October 14, 2010
    Inventors: Noriaki Hashimoto, Teruyuki Nishimura, Yufu Sagara
  • Patent number: 7812251
    Abstract: A photosensitizing transition metal complex of the formula (Ia) MLY1, (Ib) MLX3 (Ic) MLY2X, (Id) MLY3X or (Ie) MLY4X in which M is a transition metal selected from ruthenium, osmium, iron, rhenium and technetium, preferably ruthenium or osmium. X is a co-ligand independently selected from NCS—, Cl—, Br—, I—, CN—, H2O; pyridine unsubstituted or substituted by at least one group selected from vinyl, primary, secondary or tertiary amine, OH and C1-30 alkyl, preferably NSC and CN—; L is a tridentate polypyridine ligand, carrying at least one carboxylic, phosphoric acid or a chelating group and one substituted or unsubstituted alkyl group having 1 to 50 carbon atoms, substituted or unsubstituted alkylamide group having 2 to 30 carbon atoms or substituted or unsubstituted aralkyl group having 7 to 50 carbon atoms.
    Type: Grant
    Filed: October 15, 2004
    Date of Patent: October 12, 2010
    Assignee: Sharp Kabushiki Kaisha
    Inventors: Ashraful Islam, Liyuan Han, Atsushi Fukui
  • Publication number: 20100256357
    Abstract: Sulfonamides and pharmaceutical compositions containing the compounds useful in controlling intraocular pressure are disclosed. Methods for controlling intraocular pressure through administration of the compositions are also disclosed.
    Type: Application
    Filed: July 30, 2007
    Publication date: October 7, 2010
    Inventors: Wesley Kwan Mung Chong, Andrew M. Haidle, Martha Alicia Ornelas, Lin Li, Seiji Nukui, Eugene Yuanjin Rui, Min Teng, William Francois Vernier, Joe Zhongxiang Zhou
  • Publication number: 20100256172
    Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, CY, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.
    Type: Application
    Filed: January 28, 2010
    Publication date: October 7, 2010
    Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company Limited
    Inventors: Zhan Shi, Irache Visiers, Tricia J. Vos, Stepan Vyskocil
  • Publication number: 20100252820
    Abstract: Electroneutral metal complexes of the formula L Cu A, wherein L stands for an, especially bidentate, neutral ligand and A stands for an, especially bidentate, monoanionic ligand binding to Cu by at least one heteroatom selected from N, P, S; or wherein the ligands L and A with the above features are interconnected by at least one chemical bond to form one common tetradentate ligand; or protonated or alkylated forms or salts thereof show good light emitting efficiency in electroluminescent applications.
    Type: Application
    Filed: June 13, 2008
    Publication date: October 7, 2010
    Applicant: CIBA CORPORATION
    Inventors: Luisa De Cola, Yinghui Sun, Franz Schwarzenbach, Roger Pretot
  • Patent number: 7807690
    Abstract: A compound represented by the following general formula (1), or a salt thereof has serine protease inhibiting activity, and particularly excellent inhibiting activity against clotting factor VIIa. This compound or a salt thereof is useful as therapeutic and/or prophylactic agents for diseases associated with thrombus formation. [wherein R1 represents hydrogen, R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc.].
    Type: Grant
    Filed: September 19, 2008
    Date of Patent: October 5, 2010
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Richard Clark, Atsushi Takemura, Nobuhisa Watanabe, Osamu Asano, Tadashi Nagakura, Kimiyo Tabata
  • Patent number: 7807698
    Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein G is selected from a group consisting of: phenyl, pyridyl, benzothiazolyl, indazolyl; p is an integer ranging from 0 to 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; or corresponds to a group R5; R2 is hydrogen or C1-4alkyl; R3 is C1-4alkyl; R4 is C1-4 alkyl or C1-6 cycloalkyl optionally substituted by 1 or 2 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; R5 is a moiety selected from the group consisting of: isoxazolyl, —CH2—N-pyrrolyl, 1,1-dioxido-2-isothiazolidinyl, thienyl, thiazolyl, pyridyl, 2-pyrrolidinonyl, and such a group is optionally substituted by one or two substituents selected from: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl; processes for their preparation, int
    Type: Grant
    Filed: June 13, 2006
    Date of Patent: October 5, 2010
    Assignee: Glaxo Group Limited
    Inventors: Luca Arista, Giorgio Bonanomi, Dieter Hamprecht, Fabrizio Micheli
  • Patent number: 7803820
    Abstract: The present invention relates to novel compounds of formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is hydrogen or C1-4alkyl; R2 is C1-4alkyl; R3 is hydrogen, or a phenyl group, a heterocyclyl group, a 5- or 6-membered heteroaromatic group, or a 8- to 11-membered bicyclic group, any of which groups is optionally substituted by 1, 2, 3 or 4 substituents selected from the group consisting of: halogen, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, C1-4alkanoyl and SF5; p is 0, 1, 2, 3 or 4; and R4 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy and C1-4alkanoyl; n is 0 or 1; wherein when R4 is chlorine and p is 1, such R4 is not present in the ortho position with respect to the linking bond to the rest of the molecule; and wherein, if n is 0, R3 comprises at least one SF5 group as a substituent; processes for their preparation, intermediates used in these processes, pharmaceutical compositions conta
    Type: Grant
    Filed: April 12, 2006
    Date of Patent: September 28, 2010
    Assignee: Glaxo Group Limited
    Inventors: Daniele Andreotti, Anna Checchia, Dieter Hamprecht, Fabrizio Micheli
  • Publication number: 20100240707
    Abstract: The present invention relates to 2-[3-(2,2-Difluoro-benzo[1,3]dioxol-5-ylamino)-5-(2,6-dimethyl-pyridin-4-yl)-[1,2,4]triazol-1-yl]-N-ethyl-acetamide and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to a potent positive allosteric modulator of nicotinic acetylcholine receptors which have the capability of increasing the efficacy of nicotinic receptor agonists.
    Type: Application
    Filed: October 15, 2008
    Publication date: September 23, 2010
    Inventors: Johannes Wilhelmus John F. Thuring, Theodorus Dinklo, Anne Simone Josephine Lesage
  • Patent number: 7786125
    Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).
    Type: Grant
    Filed: April 7, 2009
    Date of Patent: August 31, 2010
    Inventor: Leu-Fen H. Lin
  • Publication number: 20100216846
    Abstract: The present invention relates to substituted 1-(alkyl)-3-aniline-5-aryl triazole derivatives and analogues or pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, according to Formula (I). The invention particularly relates to potent positive allosteric modulators of nicotinic acetylcholine receptors which have the capability of increasing the efficacy of nicotinic receptor agonists.
    Type: Application
    Filed: October 15, 2008
    Publication date: August 26, 2010
    Inventors: Johannes Wilhelmus John F. Thuring, Theodorus Dinklo, Anne Simone Josephine Lesage, Marcel Frans Leopold De Bruyn, Wei Zhuang
  • Publication number: 20100190761
    Abstract: The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors: formula (I). Compounds of Formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Application
    Filed: June 16, 2008
    Publication date: July 29, 2010
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Ellen K. Vande Bunte, Lin Chu, Debra Ondeyka, Ihor E. Kopka, Bing Li, Hyun O. Ok, Minal Patel, Rosemary Sisco
  • Publication number: 20100184981
    Abstract: A compound represented by the following general formula (1), or a salt thereof, has serine protease inhibiting activity, and particularly excellent inhibiting activity against clotting factor VIIa. This compound or a salt thereof is useful as therapeutic and/or prophylactic agents for diseases associated with thrombus formation. wherein R1 represents hydrogen, R2 represents optionally substituted phenyl, etc., R3 represents optionally substituted C6-10 aryl, etc.
    Type: Application
    Filed: January 15, 2010
    Publication date: July 22, 2010
    Inventors: Richard Clark, Atsushi Takemura, Nobuhisa Watanabe, Osamu Asano, Tadashi Nagakura, Kimiyo Tabata
  • Publication number: 20100152186
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.
    Type: Application
    Filed: February 19, 2010
    Publication date: June 17, 2010
    Applicant: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Cheng Hu, Jeff Jin, Yandong Li, Anita Melikian, Andrew M.K. Pennell, Sreenivas Punna, Solomon Ungashe, Yibin Zeng
  • Publication number: 20100137277
    Abstract: The present invention relates to certain new pyridin analogues of Formula (I) to processes for preparing such compounds, to their utility as P2Y12 inhibitors and as anti-trombotic agents etc, their use as medicaments in cardiovascular diseases as well as pharmaceutical compositions containing them.
    Type: Application
    Filed: January 11, 2008
    Publication date: June 3, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Thomas Antonsson, Peter Bach, David Brown, Ruth Bylund, Fabrizio Giordanetto, Johan Johansson
  • Publication number: 20100120714
    Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein W is O or S; V is a direct bond or NR3; Q is or CR6aR6b, O, NR7, C?N—O—R7 or C(?O); Y is —C(R5)?N—O—(CR8aR8b)p—X—(CR9aR9b)q—SiR10aR10bR10c; or a phenyl ring substituted as defined in the disclosure; or Z; and R1, R2, R3, R4, R5, R6a, R7, R8a, R8b, R9b, R10a, R10b, R10c, Z, p and q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.
    Type: Application
    Filed: April 4, 2008
    Publication date: May 13, 2010
    Applicant: E.I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Bruce Lawrence Finkelstein, Andrew Edmund Taggi, Jefrey Keith Long, Paula Louise Sharpe, Chi-ping Tseng, Stephen Frederick Mccann, Amy X. Ding, Steven Lewis Swann, JR.
  • Publication number: 20100113532
    Abstract: A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the structure of formula (I) or (II): including a stereoisomer thereof, a tautomer thereof, a prodrug thereof, or a pharmaceutically acceptable salt thereof, where Q is selected from N, O, and S; Y is aryl or heteroaryl; Z is H, C2-6alkyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, halo, or alkoxy; and A, B, R, Ra, Rb, Rc and Rd are defined herein. Also provided are pharmaceutical compositions and methods of treating obesity, diabetes and inflammatory or immune associated diseases comprising said compounds.
    Type: Application
    Filed: December 4, 2009
    Publication date: May 6, 2010
    Inventors: T.G. Murali Dhar, Hai-Yun Xiao, Bingwei Yang
  • Patent number: 7709469
    Abstract: The invention is directed to compounds that are P2X7 antagonist and have the formula (I) or (II) or a pharmaceutically acceptable salt, prodrug, salt of a prodrug or a combination thereof, wherein R1, R2, and R3 are defined in the specification. The invention is also directed to a method of selectively inhibiting P2X7 activity comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound of formula (III), (IV) or (V) wherein R6, R7, R8, R9, R10, and R11 are defined in the specification.
    Type: Grant
    Filed: November 6, 2006
    Date of Patent: May 4, 2010
    Assignee: Abbott Laboratories
    Inventors: William A. Carroll, Alan S. Florjancic, Arturo Perez-Medrano, Sridhar Peddi
  • Publication number: 20100099718
    Abstract: The present invention provides an antifungal agent that has excellent antifungal action, and is also excellent in terms of its properties, safety, and metabolic stability.
    Type: Application
    Filed: September 20, 2007
    Publication date: April 22, 2010
    Inventors: Masayuki Matsukura, Satoshi Inoue, Keigo Tanaka, Norio Murai, Shuji Shirotori
  • Publication number: 20100093694
    Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.
    Type: Application
    Filed: September 4, 2009
    Publication date: April 15, 2010
    Inventors: Kap-Sun Yeung, Kyle E. Parcella, John A. Bender, Brett R. Beno, Katharine A. Grant-Young, Ying Han, Piyasena Hewawasam, John F. Kadow, Andrew Nickel
  • Patent number: 7696352
    Abstract: The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.
    Type: Grant
    Filed: January 5, 2007
    Date of Patent: April 13, 2010
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Yonghong Song, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough, Carroll Anna Crew Scarborough, legal representative
  • Publication number: 20100087464
    Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of TrkA, TrkB, TrkC, Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC?, Raf, ROCK-II, Rsk1, and SGK kinases, or a combination thereof.
    Type: Application
    Filed: August 27, 2007
    Publication date: April 8, 2010
    Applicant: IRM LLC
    Inventors: Yuan Mi, Pamela A. Albaugh
  • Publication number: 20100079066
    Abstract: A novel triazole derivative which has a large energy gap and can be used for electron-transporting layer of a light-emitting element or as a host material. In addition, a light-emitting element which has higher emission efficiency by using the novel triazole derivative. Furthermore, a low power consumption light-emitting device and electronic device. A triazole derivative having a structure represented by the general formula (G1). In the formula, Py represents a pyridyl group. R11 and R12 each represent any of hydrogen, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, or a phenyl group.
    Type: Application
    Filed: August 31, 2009
    Publication date: April 1, 2010
    Inventors: Hiroko Nomura, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
  • Patent number: 7683176
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 or CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2 and CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, CCR9-mediated diseases, as controls in assays for the identification of CCR2 antagonists and as controls in assays for the identification of CCR9 antagonists.
    Type: Grant
    Filed: July 10, 2007
    Date of Patent: March 23, 2010
    Assignee: ChemoCentryx, Inc.
    Inventors: Trevor T. Charvat, Cheng Hu, Jeff Jin, Yandong Li, Anita Melikian, Andrew M. K. Pennell, Sreenivas Punna, Solomon Ungashe, Yibin Zeng
  • Patent number: 7678796
    Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.
    Type: Grant
    Filed: April 25, 2007
    Date of Patent: March 16, 2010
    Assignee: AstraZeneca AB
    Inventors: Andreas Wallberg, Karolina Nilsson, Björn Holm, Mats Nagard, Kenneth Granberg, Abdelmalik Slassi, Louise Edwards, Methvin Isaac, Tao Xin, Tomislav Stefanac