Additional Hetero Ring Attached Directly Or Indirectly To The Diazole Ring By Nonionic Bonding Patents (Class 548/364.1)
  • Patent number: 8106075
    Abstract: 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: Grant
    Filed: October 10, 2005
    Date of Patent: January 31, 2012
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Anthony Cornelius O'Sullivan, David John Hughes, André Jeanguenat, Michel Muehlebach, Olivier Loiseleur
  • Publication number: 20120010235
    Abstract: 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: Application
    Filed: June 30, 2011
    Publication date: January 12, 2012
    Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
  • Patent number: 8084467
    Abstract: 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: Grant
    Filed: June 24, 2005
    Date of Patent: December 27, 2011
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Qian Liu, Rajesh Thotapally, Venkata Kiran Vemuri
  • Patent number: 8080571
    Abstract: 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: Grant
    Filed: April 12, 2006
    Date of Patent: December 20, 2011
    Assignee: Vicore Pharma AB
    Inventors: Mathias Alterman, Anders Hallberg, Xiongyu Wu
  • Publication number: 20110301173
    Abstract: 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: Application
    Filed: June 8, 2011
    Publication date: December 8, 2011
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Haruyuki Nishida
  • Publication number: 20110301174
    Abstract: 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: Application
    Filed: June 8, 2011
    Publication date: December 8, 2011
    Applicant: Takeda Pharmaceutical Company Limited
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Haruyuki Nishida
  • Publication number: 20110294819
    Abstract: 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: Application
    Filed: December 21, 2010
    Publication date: December 1, 2011
    Inventors: 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
  • Patent number: 8067615
    Abstract: 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: Grant
    Filed: June 24, 2010
    Date of Patent: November 29, 2011
    Assignee: 4SC AG
    Inventors: Thomas Maier, Thomas Beckers, Thomas Baer, Petra Gimmnich, Frank Dullweber, Matthias Vennemann
  • Patent number: 8058452
    Abstract: 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: Grant
    Filed: November 12, 2009
    Date of Patent: November 15, 2011
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Astrid Ullmann, Thomas Bretschneider, Axel Trautwein, Ralf Wischnat, Christoph Erdelen, Angelika Lubos-Erdelen, legal representative, Dieter Feucht, Mark Wilhelm Drewes
  • Publication number: 20110275673
    Abstract: 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: Application
    Filed: September 17, 2009
    Publication date: November 10, 2011
    Inventors: Yibin Xiang, Bradford Hirth, John L. Kane, Junkai Liao, Kevin Noson, Christopher Yee
  • Patent number: 8048893
    Abstract: 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: Grant
    Filed: February 27, 2009
    Date of Patent: November 1, 2011
    Assignee: Aventis Pharma SA
    Inventors: 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
  • Patent number: 8039502
    Abstract: 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: Grant
    Filed: July 24, 2008
    Date of Patent: October 18, 2011
    Assignee: The Ohio State University Research Foundation
    Inventors: Ching-Shih Chen, Hao-Chieh Chiu, Dasheng Wang, John S. Gunn, Larry S. Schlesinger
  • Patent number: 8039467
    Abstract: 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: Grant
    Filed: October 20, 2009
    Date of Patent: October 18, 2011
    Assignee: Schering Corporation
    Inventor: Chaoyang Dai
  • Publication number: 20110224273
    Abstract: 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: Application
    Filed: September 9, 2010
    Publication date: September 15, 2011
    Applicant: AstraZeneca AB
    Inventors: Martin John Packer, James Stewart Scott, Andrew Stocker, Paul Robert Owen Whittamore
  • Patent number: 8017607
    Abstract: 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: Grant
    Filed: October 6, 2010
    Date of Patent: September 13, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
  • Publication number: 20110207781
    Abstract: Compounds of Formula (I), in which the substituents are as defined in claim 1, are suitable for use as microbiocides.
    Type: Application
    Filed: June 9, 2009
    Publication date: August 25, 2011
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Daniel Stierli, Harald Walter, Sebastian Wendeborn, Antoine Daina
  • Patent number: 7994200
    Abstract: 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: Grant
    Filed: July 17, 2006
    Date of Patent: August 9, 2011
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Antonio Torrens Jover, Susana Yenes Minguez
  • Patent number: 7989485
    Abstract: 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: Grant
    Filed: March 5, 2007
    Date of Patent: August 2, 2011
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Rosa Cuberes-Altisent, Joerg Holenz
  • Publication number: 20110172207
    Abstract: 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: Application
    Filed: September 16, 2010
    Publication date: July 14, 2011
    Applicant: AiCuris Gmbh & Co. KG
    Inventors: Rudolf SCHOHE-LOOP, Reinhold Welker, Arnold Paessens, Marcus Bauser, Friederike Stoll, Frank Dittmer, Kerstin Henninger, Daniela Paulsen, Dieter Lang
  • Patent number: 7968573
    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: Grant
    Filed: November 19, 2010
    Date of Patent: June 28, 2011
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hiroshi Ikegami, Markus Jachmann, Yoshihiko Nokura, Chiemi Iwata
  • Publication number: 20110152236
    Abstract: 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: Application
    Filed: August 13, 2009
    Publication date: June 23, 2011
    Applicant: SANOFI-AVENTIS
    Inventors: Patrick Bernardelli, Jean-Francois Sabuco, Corinne Terrier
  • Publication number: 20110152241
    Abstract: 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: Application
    Filed: November 22, 2010
    Publication date: June 23, 2011
    Applicant: ALLERGAN, INC.
    Inventors: Phong X. NGUYEN, Todd M. HEIDELBAUGH
  • Publication number: 20110144080
    Abstract: 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: Application
    Filed: December 23, 2004
    Publication date: June 16, 2011
    Applicants: ASTEX THERAPEUTICS LIMITED, THE INSTITUTE OF CANCER RESEARCH ROYAL CANCER HOSPITAL
    Inventors: 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
  • Publication number: 20110136875
    Abstract: 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: Application
    Filed: August 14, 2009
    Publication date: June 9, 2011
    Applicant: N30 PHARMACEUTICALS, LLC
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Publication number: 20110129455
    Abstract: 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: Application
    Filed: June 24, 2009
    Publication date: June 2, 2011
    Inventors: Hong Lin, Meagan B. Rouse, Mark A. Seefeld, Dennis S. Yamashita, Ren Xie
  • Patent number: 7943652
    Abstract: 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: Grant
    Filed: March 26, 2009
    Date of Patent: May 17, 2011
    Assignee: Novartis AG
    Inventors: Michael D. Shultz, Christine Hiu-Tung Chen, Young Shin Cho, Lei Jiang, Jianmei Fan, Gang Liu, Dyuti Majumdar, Jianke Li
  • Publication number: 20110112088
    Abstract: This invention relates to compounds of the formula: to compositions containing these compounds, and to methods of treatment employing the compounds and compositions.
    Type: Application
    Filed: January 13, 2011
    Publication date: May 12, 2011
    Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
  • Publication number: 20110105456
    Abstract: 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: Application
    Filed: December 22, 2010
    Publication date: May 5, 2011
    Inventors: 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
  • Publication number: 20110105568
    Abstract: 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: Application
    Filed: March 11, 2009
    Publication date: May 5, 2011
    Applicant: 4SC AG
    Inventors: Matthias Muller, Bernd Muller, Thomas Maier
  • Publication number: 20110086897
    Abstract: 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: Application
    Filed: March 11, 2009
    Publication date: April 14, 2011
    Applicant: 4SC AG
    Inventors: Jürgen Volz, Martin Feth, Rolf-Peter Hummel, Matthias Muller, Thomas Maier, Bernd Muller
  • Publication number: 20110086854
    Abstract: 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: Application
    Filed: October 6, 2010
    Publication date: April 14, 2011
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
  • Publication number: 20110082165
    Abstract: 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: Application
    Filed: October 5, 2010
    Publication date: April 7, 2011
    Inventors: Bruce A. Ellsworth, William R. Ewing, Elizabeth Jurica
  • Publication number: 20110071289
    Abstract: 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: Application
    Filed: August 6, 2008
    Publication date: March 24, 2011
    Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.
    Inventors: Yoshihiro Horiuchi, Noriko Nunami, Hiroto Tatamidani, Eiko Ohata
  • Publication number: 20110065667
    Abstract: 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: Application
    Filed: November 22, 2010
    Publication date: March 17, 2011
    Applicant: 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
  • Publication number: 20110060009
    Abstract: 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: Application
    Filed: August 27, 2010
    Publication date: March 10, 2011
    Inventors: Clinton A. BROOKS, Christine Hiu-Tung CHEN, Young Shin CHO, Lei JIANG, Gang LIU, Michael SHULTZ
  • Publication number: 20110053980
    Abstract: 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: Application
    Filed: July 4, 2008
    Publication date: March 3, 2011
    Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.
    Inventors: Monica Garcia-Lopez, Antonio Torrens-Jover
  • Patent number: 7897589
    Abstract: 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: Grant
    Filed: July 14, 2006
    Date of Patent: March 1, 2011
    Assignee: Laboratorios Del Dr. Esteve, S.A.
    Inventors: Antoni Torrens, Jordi Quintana, Helmut Buschmann, Albert Dordal, Josep Mas
  • Patent number: 7897634
    Abstract: 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: Grant
    Filed: January 30, 2007
    Date of Patent: March 1, 2011
    Assignee: Athersys, Inc.
    Inventors: Youssef L. Bennani, Michael G. Campbell, David Dastrup, Emile Porter Huck
  • Publication number: 20110039821
    Abstract: 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: Application
    Filed: October 27, 2010
    Publication date: February 17, 2011
    Inventors: 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
  • Patent number: 7888354
    Abstract: 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: Grant
    Filed: November 13, 2008
    Date of Patent: February 15, 2011
    Assignee: 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
  • Publication number: 20110034432
    Abstract: 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: Application
    Filed: March 12, 2010
    Publication date: February 10, 2011
    Applicant: AstraZeneca AB
    Inventors: Craig JOHNSTONE, Darren MCKERRECHER, Kurt Gordon PIKE
  • Publication number: 20110028485
    Abstract: 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: Application
    Filed: September 16, 2010
    Publication date: February 3, 2011
    Inventors: Hans-Michael EGGENWEILER, Michael Wolf, Hans-Peter Buchstaller, Christian Sirrenberg
  • Publication number: 20110028476
    Abstract: 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: Application
    Filed: September 1, 2010
    Publication date: February 3, 2011
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
  • Publication number: 20110021775
    Abstract: 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: Application
    Filed: January 9, 2009
    Publication date: January 27, 2011
    Inventors: Guy Bertrand, Vincent Lavallo, Adam C. Dyker
  • Patent number: 7875647
    Abstract: 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: Grant
    Filed: September 28, 2007
    Date of Patent: January 25, 2011
    Assignee: Green Cross Corporation
    Inventors: 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
  • Patent number: 7872006
    Abstract: 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: Grant
    Filed: October 20, 2006
    Date of Patent: January 18, 2011
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Yasunori Moritani, Ritsuo Imashiro, Atsushi Sato
  • Publication number: 20110009622
    Abstract: [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: Application
    Filed: April 17, 2009
    Publication date: January 13, 2011
    Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
  • Publication number: 20110003799
    Abstract: 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: Application
    Filed: September 8, 2010
    Publication date: January 6, 2011
    Applicant: 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
  • Publication number: 20110003690
    Abstract: 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: Application
    Filed: January 29, 2009
    Publication date: January 6, 2011
    Applicant: BAY CROPSCIENCE AG
    Inventors: Ulrich Goergens, Yasushi Yoneta, Tetsuya Murata, Jun Mihara, Kei Domon, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara
  • Publication number: 20100331381
    Abstract: 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: Application
    Filed: May 6, 2010
    Publication date: December 30, 2010
    Applicant: Gruenenthal GmbH
    Inventors: 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