Additional Hetero Ring Attached Directly Or Indirectly To The Diazole Ring By Nonionic Bonding Patents (Class 548/364.1)
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Patent number: 8106075Abstract: Compounds of formula I wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: October 10, 2005Date of Patent: January 31, 2012Assignee: Syngenta Crop Protection, Inc.Inventors: Anthony Cornelius O'Sullivan, David John Hughes, André Jeanguenat, Michel Muehlebach, Olivier Loiseleur
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Publication number: 20120010235Abstract: Compounds of formula and enantiomers and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control, amelioration or prevention of cancer.Type: ApplicationFiled: June 30, 2011Publication date: January 12, 2012Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
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Patent number: 8084467Abstract: One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.Type: GrantFiled: June 24, 2005Date of Patent: December 27, 2011Assignee: University of ConnecticutInventors: Alexandros Makriyannis, Qian Liu, Rajesh Thotapally, Venkata Kiran Vemuri
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Patent number: 8080571Abstract: There is provided compounds of formula I, wherein A, X1, X2, X3, X4, Y1, Y2, Y3, Y4, Z1, Z2, R4 and R5 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as selective agonists of the AT2 receptor, and thus, in particular, in the treatment of inter alia gastrointestinal conditions, such as dyspepsia, IBS and MOF, and cardiovascular disorders.Type: GrantFiled: April 12, 2006Date of Patent: December 20, 2011Assignee: Vicore Pharma ABInventors: Mathias Alterman, Anders Hallberg, Xiongyu Wu
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Publication number: 20110301173Abstract: The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl group, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.Type: ApplicationFiled: June 8, 2011Publication date: December 8, 2011Applicant: Takeda Pharmaceutical Company LimitedInventors: Masahiro Kajino, Atsushi Hasuoka, Haruyuki Nishida
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Publication number: 20110301174Abstract: The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R1 is a nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle, the nitrogen-containing monocyclic heterocyclic group optionally condensed with a benzene ring or a heterocycle optionally has substituent(s), R2 is an optionally substituted C6-14 aryl group, an optionally substituted thienyl group or an optionally substituted pyridyl group, R3 and R4 are each a hydrogen atom, or one of R3 and R4 is a hydrogen atom and the other is an optionally substituted lower alkyl pup, an acyl group, a halogen atom, a cyano group or a nitro group, and R5 is an alkyl group or a salt thereof.Type: ApplicationFiled: June 8, 2011Publication date: December 8, 2011Applicant: Takeda Pharmaceutical Company LimitedInventors: Masahiro Kajino, Atsushi Hasuoka, Haruyuki Nishida
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Publication number: 20110294819Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such compounds, and methods for inhibiting the function of the NS5A protein.Type: ApplicationFiled: December 21, 2010Publication date: December 1, 2011Inventors: Omar D. Lopez, Denis R. St. Laurent, Jason Goodrich, Jeffrey Lee Romine, Michael Serrano-Wu, Fukang Yang, Ramesh Kakarla, Xuejie Yang, Yuping Qiu, Lawrence B. Snyder
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Patent number: 8067615Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.Type: GrantFiled: June 24, 2010Date of Patent: November 29, 2011Assignee: 4SC AGInventors: Thomas Maier, Thomas Beckers, Thomas Baer, Petra Gimmnich, Frank Dullweber, Matthias Vennemann
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Patent number: 8058452Abstract: The present invention relates to novel pyrazolyl-substituted heterocycles of the formula (I) in which X, Y, Z and Het are as defined in the disclosure, to processes for their preparation, and to their use as pesticides, microbicides and herbicides.Type: GrantFiled: November 12, 2009Date of Patent: November 15, 2011Assignee: Bayer CropScience AGInventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Axel Trautwein, Ralf Wischnat, Christoph Erdelen, Angelika Lubos-Erdelen, legal representative, Dieter Feucht, Mark Wilhelm Drewes
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Publication number: 20110275673Abstract: The invention relates to compounds of Formula (I). Compounds of the present invention are inhibitors of sphingosine kinase 3, and are useful in the treatment of various disorders and conditions, such as inflammatory disorders.Type: ApplicationFiled: September 17, 2009Publication date: November 10, 2011Inventors: Yibin Xiang, Bradford Hirth, John L. Kane, Junkai Liao, Kevin Noson, Christopher Yee
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Patent number: 8048893Abstract: The present invention relates to the novel derivatives of formula (I) in which A is, if it is present, a (C1-C6) alkyl, a (C3-C6) alkenyl, a (C3-C6) alkynyl, a (C3-C7) cycloalkyl or a (C5-C7) cycloalkenyl, R1 is an NR6R7, (C4-C7) azacycloalkyl, (C5-C7) azacycloalkenyl, (C5-C9) azabicycloalkyl or (C5-C9) azabicycloalkenyl group; A-R1 is such that the nitrogen of R1 and the nitrogen in the 1-position of the pyrazole are necessarily separated by at least two carbon atoms, R3 is an H, halogen, OH, SH, NH2, ORc, SRc, SORa, SO2Ra, NHCHO, NRaRb, NHC(O)Ra, NHC(S)Ra or NHSO2Ra, R4 is an aryl or heteroaryl; and R5 is an H, halogen, CF3, CHF2, CH2F, linear or branched (C1-C6) alkyl or (C3-C7) cycloalkyl, to their racemates, enantiomers and diastereoisomers and to their mixtures, their tautomers and to their pharmaceutically acceptable salts.Type: GrantFiled: February 27, 2009Date of Patent: November 1, 2011Assignee: Aventis Pharma SAInventors: Arielle Genevois-Borella, Jean-Luc Malleron, Jean Bouquerel, Gilles Doerflinger, Andrees Bohme, Gaetan Touyer, Jean-Francois Sabuco, Corrine Terrier, Serge Mignani, Michel Evers, Youssef El-Ahmad
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Patent number: 8039502Abstract: A new class of phosphoinositide-dependent kinase-1 (PDK-1) inhibitors of Formula I: wherein X wherein X is —CF3, Ar is selected from and R is selected from where R? is L-Lys, D-Lys, ?-Ala, L-Lue, L-Ile, Phe, SO2CH2CH2NH2, SO2NH2, Asn, Glu or Gyl, and R? is methyl, ethyl, allyl, CH2CH2OH, CH2CN, CH2CH2CN, CH2CONH2,Type: GrantFiled: July 24, 2008Date of Patent: October 18, 2011Assignee: The Ohio State University Research FoundationInventors: Ching-Shih Chen, Hao-Chieh Chiu, Dasheng Wang, John S. Gunn, Larry S. Schlesinger
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Patent number: 8039467Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-? or combinations thereof.Type: GrantFiled: October 20, 2009Date of Patent: October 18, 2011Assignee: Schering CorporationInventor: Chaoyang Dai
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Publication number: 20110224273Abstract: A compound of formula (I): and pharmaceutically-acceptable salts thereof wherein the variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described.Type: ApplicationFiled: September 9, 2010Publication date: September 15, 2011Applicant: AstraZeneca ABInventors: Martin John Packer, James Stewart Scott, Andrew Stocker, Paul Robert Owen Whittamore
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Patent number: 8017607Abstract: There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, and R5 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.Type: GrantFiled: October 6, 2010Date of Patent: September 13, 2011Assignee: Hoffmann-La Roche Inc.Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
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Publication number: 20110207781Abstract: Compounds of Formula (I), in which the substituents are as defined in claim 1, are suitable for use as microbiocides.Type: ApplicationFiled: June 9, 2009Publication date: August 25, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Daniel Stierli, Harald Walter, Sebastian Wendeborn, Antoine Daina
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Patent number: 7994200Abstract: The present invention relates to Cycloalkane-substituted substituted pyrazoline compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: GrantFiled: July 17, 2006Date of Patent: August 9, 2011Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Antonio Torrens Jover, Susana Yenes Minguez
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Patent number: 7989485Abstract: The present invention relates to compounds of formula (I), methods for their preparation, medicaments comprising these compounds as well their use in the manufacture of a medicament for the treatment of humans and animals.Type: GrantFiled: March 5, 2007Date of Patent: August 2, 2011Assignee: Laboratorios del Dr. Esteve, S.A.Inventors: Rosa Cuberes-Altisent, Joerg Holenz
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Publication number: 20110172207Abstract: The present invention relates to novel substituted pyrazolamides, methods for their preparation, their use for the treatment and/or prophylaxis of diseases, as well as their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of retroviral diseases, in humans and/or animals.Type: ApplicationFiled: September 16, 2010Publication date: July 14, 2011Applicant: AiCuris Gmbh & Co. KGInventors: Rudolf SCHOHE-LOOP, Reinhold Welker, Arnold Paessens, Marcus Bauser, Friederike Stoll, Frank Dittmer, Kerstin Henninger, Daniela Paulsen, Dieter Lang
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Patent number: 7968573Abstract: 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: GrantFiled: November 19, 2010Date of Patent: June 28, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Hiroshi Ikegami, Markus Jachmann, Yoshihiko Nokura, Chiemi Iwata
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Publication number: 20110152236Abstract: The invention relates to compounds of the formula (I) where: R is a (C1-C6)alkyl group, a halo(C1-C6)alkyl group; R1 is a hydrogen atom; R2 is a heteroaromatic group or a heteroaromatic(C1-C4)alkyl group, said groups being optionally substituted; R3 and R4 represent independently from each other an optionally substituted phenyl group; Y is a hydrogen atom, a halogen, a cyano, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, a (C1-C6)alkoxy group, a halo(C1-C6)alkoxy group or a (C1-C6)alkylS(O)p group; and p is 0 to 2. Said compounds can be in the form— of a base or a salt for addition to an acid. The invention also relates to a method for preparing same and to the therapeutic application thereof.Type: ApplicationFiled: August 13, 2009Publication date: June 23, 2011Applicant: SANOFI-AVENTISInventors: Patrick Bernardelli, Jean-Francois Sabuco, Corinne Terrier
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Publication number: 20110152241Abstract: The present invention relates to novel cyclic amine and cycloalkyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: ApplicationFiled: November 22, 2010Publication date: June 23, 2011Applicant: ALLERGAN, INC.Inventors: Phong X. NGUYEN, Todd M. HEIDELBAUGH
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Publication number: 20110144080Abstract: The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR2R3 and a maximum chain length of 4 atoms extending between E and NR2R3, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR2R3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR2R3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R1 is an aryl or heteroaryl group; and R2, R3, R4 and R5 are as defined in the claims.Type: ApplicationFiled: December 23, 2004Publication date: June 16, 2011Applicants: ASTEX THERAPEUTICS LIMITED, THE INSTITUTE OF CANCER RESEARCH ROYAL CANCER HOSPITALInventors: Valerio Berdini, Gordon Saxty, Marinus Leendert Verdonk, Steven John Woodhead, Paul Graham Wyatt, Robert George Boyle, Hanna Fiona Sore, David Winter Walker, Ian Collins, Robert Downham, Robin Arthur Ellis Carr
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Publication number: 20110136875Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.Type: ApplicationFiled: August 14, 2009Publication date: June 9, 2011Applicant: N30 PHARMACEUTICALS, LLCInventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
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Publication number: 20110129455Abstract: Invented are novel pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.Type: ApplicationFiled: June 24, 2009Publication date: June 2, 2011Inventors: Hong Lin, Meagan B. Rouse, Mark A. Seefeld, Dennis S. Yamashita, Ren Xie
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Patent number: 7943652Abstract: The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, Y, Z, and are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of using compounds of Formula I in treating, inhibiting, or preventing pathologic conditions or disorders mediated wholly or in part by deacetylases.Type: GrantFiled: March 26, 2009Date of Patent: May 17, 2011Assignee: Novartis AGInventors: Michael D. Shultz, Christine Hiu-Tung Chen, Young Shin Cho, Lei Jiang, Jianmei Fan, Gang Liu, Dyuti Majumdar, Jianke Li
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Publication number: 20110112088Abstract: This invention relates to compounds of the formula: to compositions containing these compounds, and to methods of treatment employing the compounds and compositions.Type: ApplicationFiled: January 13, 2011Publication date: May 12, 2011Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
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Publication number: 20110105456Abstract: The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: December 22, 2010Publication date: May 5, 2011Inventors: Bradley Teegarden, Yifeng Xiong, Sonja Strah-Pleynet, Honnappa Jayakumar, Peter I. Dosa, Konrad Feichtinger, Matin Casper, Juerg Lehmann, Robert M. Jones, David J. Unett, Jin Sun Karoline Choi
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Publication number: 20110105568Abstract: Process for the preparation of a compound of formula (I) wherein R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification, comprising the step of reacting an acrylic acid chloride compound of formula (II?): wherein R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification, with aqueous hydroxylamine and optionally converting the resulting compound into an acid addition salt thereof.Type: ApplicationFiled: March 11, 2009Publication date: May 5, 2011Applicant: 4SC AGInventors: Matthias Muller, Bernd Muller, Thomas Maier
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Publication number: 20110086897Abstract: A salt of (E)-N-{2-amino-phenyl)-3-{1-[4-(1-methyl-1H-pyrazol-4-yl)-be?zenesulfonyl]-1H-pyrrol-3-yl)-acrylamide selected from the group consisting of the hydrobromide, methansulfonate, hemi ethane-1,2-disulfonate, benzenesulfonate, toiuenesulfonate and 2-naphthalenesulfonate.Type: ApplicationFiled: March 11, 2009Publication date: April 14, 2011Applicant: 4SC AGInventors: Jürgen Volz, Martin Feth, Rolf-Peter Hummel, Matthias Muller, Thomas Maier, Bernd Muller
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Publication number: 20110086854Abstract: There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, and R5 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.Type: ApplicationFiled: October 6, 2010Publication date: April 14, 2011Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
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Publication number: 20110082165Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are GPR40 G protein-coupled receptor modulators which may be used as medicaments.Type: ApplicationFiled: October 5, 2010Publication date: April 7, 2011Inventors: Bruce A. Ellsworth, William R. Ewing, Elizabeth Jurica
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Publication number: 20110071289Abstract: Disclosed is a compound represented by the formula (1) below or a pharmaceutically acceptable salt thereof, which is useful as an agent for prevention and/or treatment of diabetes and the like. (In the formula, RA and RB independently represent an optionally substituted alkyl group or the like; RC represents an optionally substituted alkyl group or the like; RD represents a hydrogen atom or the like; RE represents a hydrogen atom or the like; and RF represents a group selected from those represented by the formulae (G1) below: wherein one hydrogen atom serves as a bonding hand, or the like.Type: ApplicationFiled: August 6, 2008Publication date: March 24, 2011Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Yoshihiro Horiuchi, Noriko Nunami, Hiroto Tatamidani, Eiko Ohata
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Publication number: 20110065667Abstract: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases. A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.Type: ApplicationFiled: November 22, 2010Publication date: March 17, 2011Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Toshio NAKAMURA, Makoto Tatsuzuki, Dai Nozawa, Tomoko Tamita, Seiji Masuda, Hiroshi Ohta, Shuhei Kashiwa, Aya Fujino, Shigeyuki Chaki, Toshiharu Shimazaki
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Publication number: 20110060009Abstract: The present teachings relate to compounds of Formula I: and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R1, R2, R3, R4, R5, ring A, and Z are as defined herein. The present teachings also provide methods of preparing compounds of Formula I and methods of use compounds of Formula I in treating pathologic conditions or disorders mediated wholly or in part by deacetylases.Type: ApplicationFiled: August 27, 2010Publication date: March 10, 2011Inventors: Clinton A. BROOKS, Christine Hiu-Tung CHEN, Young Shin CHO, Lei JIANG, Gang LIU, Michael SHULTZ
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Publication number: 20110053980Abstract: The present invention relates to indane-amine compounds of general formula (I) and compositions thereof, methods for their preparation, and the use of said compounds for the preparation of a medicament for the treatment of humans or animals.Type: ApplicationFiled: July 4, 2008Publication date: March 3, 2011Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Monica Garcia-Lopez, Antonio Torrens-Jover
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Patent number: 7897589Abstract: The present invention relates to substituted pyrazoline compounds, methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animals.Type: GrantFiled: July 14, 2006Date of Patent: March 1, 2011Assignee: Laboratorios Del Dr. Esteve, S.A.Inventors: Antoni Torrens, Jordi Quintana, Helmut Buschmann, Albert Dordal, Josep Mas
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Patent number: 7897634Abstract: This invention relates to compounds of the formulas (1), (2) and (3) having pharmacological activity, to compositions containing these compounds, and to methods of treatment employing the compounds and compositions.Type: GrantFiled: January 30, 2007Date of Patent: March 1, 2011Assignee: Athersys, Inc.Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
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Publication number: 20110039821Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: October 27, 2010Publication date: February 17, 2011Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukui, Ru Zhou
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Patent number: 7888354Abstract: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases. A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.Type: GrantFiled: November 13, 2008Date of Patent: February 15, 2011Assignee: Taisho Pharmaceutical Co., LtdInventors: Toshio Nakamura, Makoto Tatsuzuki, Dai Nozawa, Tomoko Tamita, Seiji Masuda, Hiroshi Ohta, Shuhei Kashiwa, Aya Fujino, Shigeyuki Chaki, Toshiharu Shimazaki
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Publication number: 20110034432Abstract: Compounds of Formula (I): wherein: R1 is methoxymethyl; R2 is selected from —C(O)NR4R5, —SO2NR4R5, —S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro-drug or solvate thereof, are described.Type: ApplicationFiled: March 12, 2010Publication date: February 10, 2011Applicant: AstraZeneca ABInventors: Craig JOHNSTONE, Darren MCKERRECHER, Kurt Gordon PIKE
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Publication number: 20110028485Abstract: Novel 1,5-diphenylpyrazole derivatives of the formula (I) in which R1-R6 have the meanings indicated in claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.Type: ApplicationFiled: September 16, 2010Publication date: February 3, 2011Inventors: Hans-Michael EGGENWEILER, Michael Wolf, Hans-Peter Buchstaller, Christian Sirrenberg
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Publication number: 20110028476Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof.Type: ApplicationFiled: September 1, 2010Publication date: February 3, 2011Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
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Publication number: 20110021775Abstract: Stable, bent allenes, organometallic complexes of bent allenes are provided along with methods of conducting chemical processes such as olefin metathesis, comprising contacting an olefin substrate with an organometallic complex as described herein, under suitable conditions.Type: ApplicationFiled: January 9, 2009Publication date: January 27, 2011Inventors: Guy Bertrand, Vincent Lavallo, Adam C. Dyker
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Patent number: 7875647Abstract: A heteroaryl-pyrazole compound of formula (I) or a pharmaceutically acceptable salt thereof is effective as a cannabinoid CB1 receptor inverse agonist or antagonist, which is useful for preventing or treating obesity and obesity-related metabolic disorders. The present invention also provides a method for preparing the inventive heteroaryl-pyrasole compounds or a pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating obesity and obesity-related metabolic disorders.Type: GrantFiled: September 28, 2007Date of Patent: January 25, 2011Assignee: Green Cross CorporationInventors: Jinhwa Lee, Jeong Min Kim, Chong-Hwan Jonathan Chang, Suk Ho Lee, Hee Jeong Seo, Suk Youn Kang, Kwang-Seop Song, Jong Yup Kim, Min-ah Kim, Sung-han Lee, Kwang-Woo Ahn, Myung Eun Jung, Ji-Hyun Park
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Patent number: 7872006Abstract: The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula: —N(R7)—, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula: —N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: —N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc., or a pharmaceutically acceptable salt thereof.Type: GrantFiled: October 20, 2006Date of Patent: January 18, 2011Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Yasunori Moritani, Ritsuo Imashiro, Atsushi Sato
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Publication number: 20110009622Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].Type: ApplicationFiled: April 17, 2009Publication date: January 13, 2011Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
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Publication number: 20110003799Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.Type: ApplicationFiled: September 8, 2010Publication date: January 6, 2011Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Adrian Liam GILL, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
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Publication number: 20110003690Abstract: The invention relates to novel arylpyrroline compounds of formula (I) which having excellent insecticidal activity and which can thus be used as an insecticide is provided.Type: ApplicationFiled: January 29, 2009Publication date: January 6, 2011Applicant: BAY CROPSCIENCE AGInventors: Ulrich Goergens, Yasushi Yoneta, Tetsuya Murata, Jun Mihara, Kei Domon, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara
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Publication number: 20100331381Abstract: The invention relates to substituted phenylureas and phenylamides, to processes for the preparation thereof, to pharmaceutical compositions containing these compounds and also to the use of these compounds for preparing pharmaceutical compositions.Type: ApplicationFiled: May 6, 2010Publication date: December 30, 2010Applicant: Gruenenthal GmbHInventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Nils Damann, Sven Frormann, Bernhard Lesch, Jeewoo Lee, Yong-Soo Kim, Myeong-Seop Kim