1,2,4-triazoles (including Hydrogenated) Patents (Class 546/272.4)
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Patent number: 7998984Abstract: 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: GrantFiled: May 7, 2007Date of Patent: August 16, 2011Assignee: AstraZeneca ABInventors: Peter Hansen, Karolina Lawitz, Matti Lepistö, Hans Lönn, Asim Ray
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Publication number: 20110196150Abstract: 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: ApplicationFiled: February 10, 2011Publication date: August 11, 2011Inventors: Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
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Publication number: 20110195930Abstract: 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: ApplicationFiled: November 6, 2009Publication date: August 11, 2011Applicant: Ishihara Sangyo Kaisha, Ltd.Inventors: Takahiro Haga, Masayuki Morita, Kazuhisa Kiriyama, Kumiko Azuma
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Patent number: 7989637Abstract: 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: GrantFiled: December 17, 2008Date of Patent: August 2, 2011Assignee: Roche Palo Alto LLCInventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
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Publication number: 20110183981Abstract: 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: ApplicationFiled: March 30, 2011Publication date: July 28, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Allison L. Marlow, Eli Wallace, Jeongbeob Seo, Joseph P. Lyssikatos, Hong Woon Yang, James Blake
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Publication number: 20110172276Abstract: 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: ApplicationFiled: March 25, 2011Publication date: July 14, 2011Inventors: Sadayuki Arimori, Yoshiharu Kinoshita
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Patent number: 7973033Abstract: 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: GrantFiled: January 12, 2011Date of Patent: July 5, 2011Assignee: 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
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Publication number: 20110152232Abstract: Compounds that modulate GHS-R are described, for examples compounds formula (I)Type: ApplicationFiled: October 26, 2010Publication date: June 23, 2011Inventors: Jeffrey O. Saunders, Thomas Coulter, Paul Mortenson, Manuel A. Navia, Jean-Francois Pons
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Patent number: 7960422Abstract: 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: GrantFiled: October 17, 2008Date of Patent: June 14, 2011Assignee: AstraZeneca ABInventors: Erwan Arzel, Louise Edwards, Methvin Isaac, Donald A. McLeod, Abdelmalik Slassi, Tao Xin
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Patent number: 7947683Abstract: 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: GrantFiled: April 12, 2006Date of Patent: May 24, 2011Assignee: Glaxo Group LimtedInventors: Giorgio Bonanomi, Anna Checchia, Elettra Fazzolari, Dieter Hamprecht, Fabrizio Micheli, Luca Tarsi, Silvia Terreni
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Publication number: 20110105460Abstract: [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: ApplicationFiled: July 2, 2009Publication date: May 5, 2011Applicant: 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
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Patent number: 7935815Abstract: 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: GrantFiled: August 28, 2008Date of Patent: May 3, 2011Assignee: 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
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Publication number: 20110076230Abstract: 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: ApplicationFiled: May 28, 2009Publication date: March 31, 2011Inventors: James C. Barrow, Scott Harrison, James Mulhearn, Scott Wolkenberg
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Patent number: 7915295Abstract: 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: GrantFiled: December 30, 2004Date of Patent: March 29, 2011Assignee: Medivir ABInventors: Christian Sund, Nathalie Roue, Stefan Lindstrom, Dmitry Antonov, Christer Sahlberg, Katarina Jansson
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Publication number: 20110070297Abstract: 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: ApplicationFiled: December 1, 2010Publication date: March 24, 2011Applicants: Takeda San Diego, Inc., Takeda Pharmaceutical Company LimitedInventors: Sheldon X. Cao, Jun Feng, Yasuhiro Imaeda, Stephen L. Gwaltney, David J. Hosfield, Nobuyuki Takakura, Mingnam Tang
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Publication number: 20110071291Abstract: 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: ApplicationFiled: November 19, 2010Publication date: March 24, 2011Inventors: Hiroshi Ikegami, Markus Jachmann, Yoshihiko Nokura, Chiemi Iwata
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Publication number: 20110065696Abstract: 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: ApplicationFiled: November 19, 2010Publication date: March 17, 2011Inventors: 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
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Publication number: 20110009410Abstract: 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: ApplicationFiled: July 12, 2010Publication date: January 13, 2011Applicant: Gilead Sciences, Inc.Inventors: Britton Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, JR., Gregory Notte
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Publication number: 20110003815Abstract: 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: ApplicationFiled: October 6, 2008Publication date: January 6, 2011Inventors: Anthony Ogawa, Feroze Ujjainwalla, Bing Li, Lin Chu, Minal Patel, Helen M. Armstrong, Hyun O. Ok, Rosemary Sisco, Dwight MacDonald, John Hutchinson, Helene Perrier
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Publication number: 20110003806Abstract: 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: ApplicationFiled: January 28, 2010Publication date: January 6, 2011Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company LimitedInventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil
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Patent number: 7863299Abstract: 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 eacType: GrantFiled: August 18, 2006Date of Patent: January 4, 2011Assignee: Glaxo Group LimitedInventors: Anna Maria Capelli, Elettra Fazzolari, Fabrizio Micheli, Giovanna Tedesco, Silvia Terreni
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Publication number: 20100330069Abstract: 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: ApplicationFiled: January 8, 2010Publication date: December 30, 2010Applicant: TargeGen, Inc.Inventors: Wolfgang Wrasidlo, Elena Dneprovskaia
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Publication number: 20100324053Abstract: 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: ApplicationFiled: March 18, 2009Publication date: December 23, 2010Inventors: Gregor James MacDonald, Johannes Wilhelmus John F. Thuring, Pauline Carol Stanislawski, Wei Zhuang, Yves Emiel Maria Van Roosbroeck, Frans Alfons Maria Van Den Keybus
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Patent number: 7851701Abstract: 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: GrantFiled: July 5, 2002Date of Patent: December 14, 2010Assignee: Nippon Kayaku Kabushiki KaishaInventors: Masaaki Ikeda, Koichiro Shigaki, Teruhisa Inoue
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Publication number: 20100267725Abstract: 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: ApplicationFiled: April 20, 2010Publication date: October 21, 2010Inventors: Michael Geoffrey Neil Russell, Kevin James Doyle
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Publication number: 20100261699Abstract: 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: ApplicationFiled: December 15, 2008Publication date: October 14, 2010Inventors: Noriaki Hashimoto, Teruyuki Nishimura, Yufu Sagara
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Patent number: 7812251Abstract: 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: GrantFiled: October 15, 2004Date of Patent: October 12, 2010Assignee: Sharp Kabushiki KaishaInventors: Ashraful Islam, Liyuan Han, Atsushi Fukui
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Publication number: 20100256357Abstract: 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: ApplicationFiled: July 30, 2007Publication date: October 7, 2010Inventors: 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
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Publication number: 20100256172Abstract: 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: ApplicationFiled: January 28, 2010Publication date: October 7, 2010Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company LimitedInventors: Zhan Shi, Irache Visiers, Tricia J. Vos, Stepan Vyskocil
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Publication number: 20100252820Abstract: 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: ApplicationFiled: June 13, 2008Publication date: October 7, 2010Applicant: CIBA CORPORATIONInventors: Luisa De Cola, Yinghui Sun, Franz Schwarzenbach, Roger Pretot
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Patent number: 7807690Abstract: 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: GrantFiled: September 19, 2008Date of Patent: October 5, 2010Assignee: Eisai R&D Management Co., Ltd.Inventors: Richard Clark, Atsushi Takemura, Nobuhisa Watanabe, Osamu Asano, Tadashi Nagakura, Kimiyo Tabata
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Patent number: 7807698Abstract: 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, intType: GrantFiled: June 13, 2006Date of Patent: October 5, 2010Assignee: Glaxo Group LimitedInventors: Luca Arista, Giorgio Bonanomi, Dieter Hamprecht, Fabrizio Micheli
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Patent number: 7803820Abstract: 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 contaType: GrantFiled: April 12, 2006Date of Patent: September 28, 2010Assignee: Glaxo Group LimitedInventors: Daniele Andreotti, Anna Checchia, Dieter Hamprecht, Fabrizio Micheli
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Publication number: 20100240707Abstract: 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: ApplicationFiled: October 15, 2008Publication date: September 23, 2010Inventors: Johannes Wilhelmus John F. Thuring, Theodorus Dinklo, Anne Simone Josephine Lesage
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Patent number: 7786125Abstract: 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: GrantFiled: April 7, 2009Date of Patent: August 31, 2010Inventor: Leu-Fen H. Lin
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Publication number: 20100216846Abstract: 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: ApplicationFiled: October 15, 2008Publication date: August 26, 2010Inventors: Johannes Wilhelmus John F. Thuring, Theodorus Dinklo, Anne Simone Josephine Lesage, Marcel Frans Leopold De Bruyn, Wei Zhuang
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Publication number: 20100190761Abstract: 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: ApplicationFiled: June 16, 2008Publication date: July 29, 2010Inventors: Anthony Ogawa, Feroze Ujjainwalla, Ellen K. Vande Bunte, Lin Chu, Debra Ondeyka, Ihor E. Kopka, Bing Li, Hyun O. Ok, Minal Patel, Rosemary Sisco
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Publication number: 20100184981Abstract: 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: ApplicationFiled: January 15, 2010Publication date: July 22, 2010Inventors: Richard Clark, Atsushi Takemura, Nobuhisa Watanabe, Osamu Asano, Tadashi Nagakura, Kimiyo Tabata
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Publication number: 20100152186Abstract: 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: ApplicationFiled: February 19, 2010Publication date: June 17, 2010Applicant: ChemoCentryx, Inc.Inventors: Trevor T. Charvat, Cheng Hu, Jeff Jin, Yandong Li, Anita Melikian, Andrew M.K. Pennell, Sreenivas Punna, Solomon Ungashe, Yibin Zeng
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Publication number: 20100137277Abstract: 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: ApplicationFiled: January 11, 2008Publication date: June 3, 2010Applicant: ASTRAZENECA ABInventors: Thomas Antonsson, Peter Bach, David Brown, Ruth Bylund, Fabrizio Giordanetto, Johan Johansson
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Publication number: 20100120714Abstract: 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: ApplicationFiled: April 4, 2008Publication date: May 13, 2010Applicant: E.I. DU PONT DE NEMOURS AND COMPANYInventors: 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.
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Publication number: 20100113532Abstract: 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: ApplicationFiled: December 4, 2009Publication date: May 6, 2010Inventors: T.G. Murali Dhar, Hai-Yun Xiao, Bingwei Yang
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Patent number: 7709469Abstract: 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: GrantFiled: November 6, 2006Date of Patent: May 4, 2010Assignee: Abbott LaboratoriesInventors: William A. Carroll, Alan S. Florjancic, Arturo Perez-Medrano, Sridhar Peddi
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Publication number: 20100099718Abstract: 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: ApplicationFiled: September 20, 2007Publication date: April 22, 2010Inventors: Masayuki Matsukura, Satoshi Inoue, Keigo Tanaka, Norio Murai, Shuji Shirotori
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Publication number: 20100093694Abstract: 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: ApplicationFiled: September 4, 2009Publication date: April 15, 2010Inventors: 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
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Patent number: 7696352Abstract: 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: GrantFiled: January 5, 2007Date of Patent: April 13, 2010Assignee: 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
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Publication number: 20100087464Abstract: 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: ApplicationFiled: August 27, 2007Publication date: April 8, 2010Applicant: IRM LLCInventors: Yuan Mi, Pamela A. Albaugh
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Publication number: 20100079066Abstract: 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: ApplicationFiled: August 31, 2009Publication date: April 1, 2010Inventors: Hiroko Nomura, Sachiko Kawakami, Nobuharu Ohsawa, Satoshi Seo
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Patent number: 7683176Abstract: 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: GrantFiled: July 10, 2007Date of Patent: March 23, 2010Assignee: ChemoCentryx, Inc.Inventors: Trevor T. Charvat, Cheng Hu, Jeff Jin, Yandong Li, Anita Melikian, Andrew M. K. Pennell, Sreenivas Punna, Solomon Ungashe, Yibin Zeng
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Patent number: 7678796Abstract: 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: GrantFiled: April 25, 2007Date of Patent: March 16, 2010Assignee: AstraZeneca ABInventors: Andreas Wallberg, Karolina Nilsson, Björn Holm, Mats Nagard, Kenneth Granberg, Abdelmalik Slassi, Louise Edwards, Methvin Isaac, Tao Xin, Tomislav Stefanac