Polycyclo Ring System Having The 1,2-diazole Ring As One Of The Cyclos Patents (Class 546/275.7)
  • Publication number: 20110271406
    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: Application
    Filed: August 21, 2008
    Publication date: November 3, 2011
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Olivier Loiseleur, Roger Graham Hall, Andre Denis Stoller, Gerald Wayne Craig, Andre Jeanguenat, Andrew Edmunds
  • Publication number: 20110263559
    Abstract: The present invention is directed to substituted indazole compounds, pharmaceutical compositions of these compounds and methods of use thereof. The compounds of the present invention are ketohexokinase (KHK) inhibitors, useful for treating or ameliorating a KHK mediated metabolic disorders and/or diseases such as obesity, Type II diabetes mellitus and Metabolic Syndrome X.
    Type: Application
    Filed: April 21, 2011
    Publication date: October 27, 2011
    Inventors: Xuqing ZHANG, Marta G. ABAD, Alan C. GIBBS, Gee-Hong KUO, Lawrence C. KUO, Fengbin SONG, Zhihua SUI
  • Publication number: 20110263588
    Abstract: The present invention relates to compounds that may be negative allosteric modulators of metabotropic receptors-subtype 5, and methods of making and using same.
    Type: Application
    Filed: October 23, 2009
    Publication date: October 27, 2011
    Applicant: GLAXO GROUP LIMITED
    Inventors: Peter Bertinato, Merav Fichman, Shomir Ghosh, Jian Lin, Dalia Segal, Zhaoda Zhang
  • Publication number: 20110237628
    Abstract: This invention relates to novel cyclopentyl- and cycloheptylpyrazole derivatives of the formula I wherein A and R1 to R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. The invention relates also to compositions including these compounds and methods of using the compounds.
    Type: Application
    Filed: March 17, 2011
    Publication date: September 29, 2011
    Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Bernd Kuhn, Hans Richter, Sven Taylor
  • Patent number: 8022059
    Abstract: A compound of the formula: wherein ring X is benzene or pyridine; R1 is substituted alkyl; R2 is optionally substituted aryl or optionally substituted heterocyclic group; R3 is hydrogen or alkyl; R4 is hydrogen, halogen or alkyl; R5 is hydrogen or alkyl; R6 and R7 are the same or different and each hydrogen or halogen, or a pharmaceutically acceptable salt thereof, which is useful as IKur blocker effective for preventing or treating cardiac arrhythmia such as atrial fibrillation.
    Type: Grant
    Filed: September 26, 2008
    Date of Patent: September 20, 2011
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Tetsuo Yamaguchi, Hiroyuki Kawanishi, Hideki Ushirogochi, Tatsuyuki Takahashi, Tohru Takebe
  • Publication number: 20110212961
    Abstract: The present invention provides compounds having the general structure I, or a pharmaceutically acceptable salt thereof: wherein X is a six-member ring selected from phenyl, pyridine, or pyrimidine; Y is H, an alkenyl, a substituted alkenyl, or alkynyl, and R is H or alkyl. Pharmaceutical compositions for treating various disorders such as cancers, the compositions including compound I are also provided.
    Type: Application
    Filed: May 9, 2011
    Publication date: September 1, 2011
    Inventors: Maurizio Pellecchia, Surya De, Elisa Barile
  • Patent number: 8008505
    Abstract: This invention relates to novel indazole or 4,5,6,7-tetrahydro-indazole derivatives of formula I wherein R1 to R8 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are FXR modulators and can be used as medicaments.
    Type: Grant
    Filed: September 21, 2009
    Date of Patent: August 30, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Gregory Martin Benson, Konrad Bleicher, Uwe Grether, Bernd Kuhn, Hans Richter, Sven Taylor
  • Patent number: 8008481
    Abstract: Novel compounds of Formula (I) or pharmaceutically acceptable salts, prodrugs and biologically active metabolites thereof of Formula (I) wherein the substituents are as defined herein, which are useful as therapeutic agents.
    Type: Grant
    Filed: April 2, 2007
    Date of Patent: August 30, 2011
    Inventors: Anna M. Ericsson, Andrew Burchat, Kristine E. Frank, David J. Calderwood, Lily K. Abbott, Maria A. Argiriadi, David W. Borhani, Kevin P. Cusack, Richard W. Dixon, Thomas D. Gordon, Kelly D. Mullen, Robert V. Talanian, Xiaoyun Wu, Xiaolei Zhang, Lu Wang, Biqin Li, Claude E. Barberis, Neil Wishart
  • Publication number: 20110207750
    Abstract: This invention provides compounds of Formula I which are PAFR antagonists: I and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.
    Type: Application
    Filed: October 26, 2009
    Publication date: August 25, 2011
    Inventors: Lin Chu, Anthony Ogawa, Hyun O. Ok, Feroze Ujjainwalla
  • Publication number: 20110207731
    Abstract: This invention relates to novel 4-(indazolyl)-1,4-dihydropyridine og the following formula (I) derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.
    Type: Application
    Filed: May 29, 2009
    Publication date: August 25, 2011
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Nicole Teusch, Karen Engel
  • Publication number: 20110195110
    Abstract: Pyrazole urea compounds, pharmaceutical compositions which contain them and methods for treating cancer using them.
    Type: Application
    Filed: December 1, 2006
    Publication date: August 11, 2011
    Inventors: Roger Smith, Holia N. Hatoum-Mokdad, Louis David Cantin, Donald E. Bierer, Wenlang Fu, Dhanapalan Nagarathnam, Gaetan Ladouceur, Yamin Wang, Herbert Ogutu, Scot Wilhelm, Ian Taylor, Sanjeeva Reddy, Richard Gedrich, Christopher Carter, Aaron Schmitt, Xiaomei Zhang
  • Publication number: 20110196150
    Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
    Type: Application
    Filed: February 10, 2011
    Publication date: August 11, 2011
    Inventors: Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
  • Publication number: 20110195934
    Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable faints thereof according to wherein all of the variables are defined herein.
    Type: Application
    Filed: October 8, 2009
    Publication date: August 11, 2011
    Inventors: Pratik Devasthale, Wliiam N. Washburn, Wei Wang, Andres Hernandez, Saleem Ahmad, Guohua Zhao
  • Publication number: 20110190283
    Abstract: Compounds of the Formula (I) are disclosed which are Fab I inhibitors and are useful in the treatment of bacterial infections.
    Type: Application
    Filed: July 6, 2010
    Publication date: August 4, 2011
    Inventors: William H. Miller, Kenneth A. Newlander, Mark A. Seefeld, Irene N. Uzinskas, Walter E. DeWolf, JR., Dalia R. Jakas
  • Publication number: 20110190335
    Abstract: The purpose of the present invention is to provide a glucokinase activator which is useful as a pharmaceutical agent such as agents for the prophylaxis or treatment of diabetes, obesity and the like, and the like. The present invention is a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Application
    Filed: April 15, 2009
    Publication date: August 4, 2011
    Inventors: Tsuneo Yasuma, Osamu Ujikawa
  • Publication number: 20110183973
    Abstract: The invention is directed to certain novel compounds directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
    Type: Application
    Filed: June 3, 2009
    Publication date: July 28, 2011
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Paul Spencer Jones, Joelle Le, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst
  • Publication number: 20110183939
    Abstract: The present invention provides a novel P2X3 and/or P2X2/3 receptor antagonist. A compound represented by the formula (I); wherein Z1 is optionally protected hydroxy, etc.; Z2 is —C(?O)—, etc.; Z3a and Z3b are taken together ?O or ?S; t is an integer of 0 to 4; R4a and R4b are each independently, hydrogen or substituted or unsubstituted lower alkyl, etc.; m and n are each independently an integer of 0 to 2; k is an integer of 0 or 1; Ring A is an aromatic carbocyclic ring or a heterocyclic ring, etc.; B is aromatic carbocyclic ring-diyl or heterocyclic ring-diyl, etc.; R1a and R1b are each independently halogen, hydroxy, substituted or unsubstituted lower alkyl, etc.; R2 is substituted or unsubstituted alkyl, etc.; R3 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group, etc.; or its pharmaceutically acceptable salt, or a solvate thereof is provided.
    Type: Application
    Filed: September 24, 2009
    Publication date: July 28, 2011
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Hiroyuki Kai, Yoshiyuki Taoda, Takeshi Endoh, Tohru Horiguchi, Kentaro Asahi, Hiroyuki Tobinaga
  • Publication number: 20110173726
    Abstract: The present invention relates to a method for controlling invertebrate pests which method comprises treating the pests, their food supply, their habitat or their breeding ground or a plant, seed, soil, area, material or environment in which the pests are growing or may grow, or the materials, plants, seeds, soils, surfaces or spaces to be protected from pest attack or infestation with a pesticidally effective amount of a pyrazole compound of formulae I or II or a salt or an N-oxide thereof, wherein A is a pyrazole radical of the formulae A1 or A2, wherein # denotes the binding; D is a 5- or 6-membered heterocyclic radical fused to the pyrazole moiety; Rp1, Rp2 and Rpx are H, halogen, CN, NO2, C1-C10-alkyl, C2-C10-alkenyl, C2-C10-alkynyl, etc.
    Type: Application
    Filed: September 23, 2009
    Publication date: July 14, 2011
    Applicant: BASF SE
    Inventors: Steffen Groß, Karsten Körber, Wolfgang Von Deyn, Florian Kaiser, Ronan Le Vezouet, Sebastian Sörgel, Matthias Pohlman, Prashant Deshmukh, Joachim Dickhaut, Douglas D. Anspaugh, Deborah L. Culbertson, Hassan Oloumi-Sadeghi
  • Publication number: 20110166343
    Abstract: To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: —CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)].
    Type: Application
    Filed: March 14, 2011
    Publication date: July 7, 2011
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi
  • Publication number: 20110160210
    Abstract: An ophthalmic pharmaceutical composition useful in the treatment of glaucoma and control of intraocular pressure comprising an effective amount of a selective modulator of ALK5 receptor activity is disclosed. Also disclosed is a method of treating glaucoma and controlling intraocular pressure comprising applying a therapeutically effective amount of a pharmaceutical composition comprising a selective modulator of ALK5 receptor activity to an affected eye of a patient.
    Type: Application
    Filed: March 8, 2011
    Publication date: June 30, 2011
    Applicant: ALCON, INC.
    Inventors: Debra L. Fleenor, Iok-Hou Pang, Allan R. Shapard, Mark R. Hellberg, Abbot F. Clark, Peter G. Klimko
  • Publication number: 20110144121
    Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.
    Type: Application
    Filed: June 16, 2010
    Publication date: June 16, 2011
    Applicant: CARA THERAPEUTICS, INC.
    Inventor: Robert Zhiyong Luo
  • Publication number: 20110129624
    Abstract: This invention provides an azomethine compound that can realize a good coupling reaction and, at the same time, can significantly reduce the production cost of the azomethine compound, the azomethine compound comprising a pyridine ring bonded through a nitrogen atom to a 1H-pyrazolo[1,5-b][1,2,4]triazole ring. The azomethine compound is represented by formula (M-I): wherein R1 represents a phenyl group or a naphthyl group optionally substituted by an alkyl group or a halogen; and R2 and R3 each independently represent a C2-4 (number of carbon atoms) alkyl group.
    Type: Application
    Filed: March 31, 2010
    Publication date: June 2, 2011
    Applicant: Dai Nippon Printing Co., Ltd.
    Inventors: Tomoyuki Sanada, Tsuaki Odaka, Hiroyuki Hasegawa, Hiroko Amano
  • Publication number: 20110118246
    Abstract: The invention is directed to to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.
    Type: Application
    Filed: June 3, 2009
    Publication date: May 19, 2011
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Juliet Kay Simpson, Christian Alan Paul Smethurst
  • Publication number: 20110118248
    Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.
    Type: Application
    Filed: January 13, 2009
    Publication date: May 19, 2011
    Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M. K. Pennell, John J. Wright, Antoni Krasinski, Qiang Wang
  • Publication number: 20110118236
    Abstract: An object of the present invention is to provide a novel AMPA receptor potentiator. A compound represented by the following formula (I) or a salt thereof: wherein in formula (I) R1 represents (1) a halogen atom, or (2) cyano group, or the like; Ra and Rb each independently represent a hydrogen atom or C1-4 alkyl; L represents a bond, or a spacer in which the number of atoms in the main chain is 1 to 8; Ring A represents (1) a non-aromatic carbon ring of 4-8 carbon atoms, or (2) a 4- to 8-membered non-aromatic heterocycle either of which is optionally substituted with 1 or more substituents selected from (a) halogen atoms, and (b) cyano group; and Ar represents a substituted phenyl group, or optionally substituted 5- or 6-membered aromatic heterocyclic group.
    Type: Application
    Filed: March 25, 2009
    Publication date: May 19, 2011
    Inventors: Michiyo Mochizuki, Shotaro Miura
  • Publication number: 20110112299
    Abstract: Provided are a tetracyclic compound represented by the formula (I): [in the formula (I), the formula (A) represents a benzene ring or the like, X represents CH or a nitrogen atom, Q represents —O— or the like, R1, R2, and R3 may be the same or different and each represent a hydrogen atom or the like, l, m, and n each represent an integer from one to the maximum substitutable number of substituents, and R4 and R5 may be the same or different and each represent a hydrogen atom or the like], or a pharmaceutically acceptable salt thereof, and the like.
    Type: Application
    Filed: July 3, 2009
    Publication date: May 12, 2011
    Applicant: KYOWA HAKKO KIRIN CO., LTD.
    Inventors: Junichiro Yamamoto, Kiyotoshi Mori, Tomohiro Era, Yoshisuke Nakasato, Kenji Uchida
  • Publication number: 20110112147
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
    Type: Application
    Filed: October 5, 2010
    Publication date: May 12, 2011
    Inventors: David Robert Bolin, Stuart Hayden, Yimin Qian
  • Publication number: 20110112070
    Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of P13-kinase activity.
    Type: Application
    Filed: June 3, 2009
    Publication date: May 12, 2011
    Inventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Katherine Louise Jones, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, Christian Alan Paul Smethurst, Yoshiaki Washio
  • Publication number: 20110104110
    Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: August 27, 2008
    Publication date: May 5, 2011
    Inventors: Gopinadhan N. Anikumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
  • Publication number: 20110105440
    Abstract: The present invention is directed to hexahydrocyclopentylf]indazole carboxamides and derivatives thereof as selective glucocorticoid receptor ligands useful for treating a variety of autoimmune and inflammatory diseases or conditions. Pharmaceutical compositions and methods of use are also included.
    Type: Application
    Filed: February 24, 2009
    Publication date: May 5, 2011
    Inventors: William P. Dankulich, Mildred L. Kaufman, Danielle M. McMaster, Robert S. Meissner, Helen J. Mitchell
  • Patent number: 7932250
    Abstract: To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: —CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)].
    Type: Grant
    Filed: July 1, 2005
    Date of Patent: April 26, 2011
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Hidekazu Inoue, Hidenobu Murafuji, Yasuhiro Hayashi
  • Publication number: 20110082141
    Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to Formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.
    Type: Application
    Filed: March 5, 2009
    Publication date: April 7, 2011
    Applicant: AZIENDE CHIM. RIUN.ANG.FRANC. A.C.R.A.F. S.p.A.
    Inventors: Angelo Guglielmotti, Guido Furlotti, Giorgina Mangano, Nicola Cazzolla
  • Publication number: 20110071165
    Abstract: Aza- and polyazanthranyl amides and their use as medicaments in the treatment of diseases caused by persistent angiogenesis are described, as well as the intermediates used in the preparation of the aza- and polyazanthranyl amides.
    Type: Application
    Filed: November 24, 2010
    Publication date: March 24, 2011
    Applicant: NOVARTIS AG
    Inventors: Dieter SEIDELMANN, Martin KRÜGER, Orlin PETROV, Andreas HUTH, Karl-Heinz THIERAUCH, Andreas MENRAD, Martin HABEREY
  • Publication number: 20110071194
    Abstract: Compounds of formula (I): The present invention relates to novel indazolyl ester or amide derivatives, to pharmaceutical compositions comprising such derivatives, to processes for preparing such novel derivatives and to the use of such derivatives as medicaments
    Type: Application
    Filed: December 2, 2010
    Publication date: March 24, 2011
    Inventors: Markus Berger, Jan Dahmén, Karl Edman, Anders Eriksson, Balint Gabos, Thomas Hansson, Martin Hemmerling, Krister Henriksson, Svetlana Ivanova, Matti Lepistö, Darren McKerrecher, Magnus Munck af Rosenschöld, Stinabritt Nilsson, Hartmut Rehwinkel, Camilla Taflin
  • Publication number: 20110065702
    Abstract: The present invention is directed to a compound is represented by Structural Formula (A):or a pharmaceutically acceptable salt therof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 19, 2008
    Publication date: March 17, 2011
    Inventors: Heinz W. Pauls, Bryan T. Forrest, Radoslaw Laufer, Miklos Feher, Peter Brent Sampson, Guohua Pan, Sze-Wan Li, Yong Liu
  • Patent number: 7902229
    Abstract: The invention relates to novel anthranilamide pyridinureas as VEGF receptor kinase inhibitors, their production and use as pharmaceutical agents for preventing or treating diseases that are triggered by persistent angiogenesis.
    Type: Grant
    Filed: November 3, 2005
    Date of Patent: March 8, 2011
    Assignee: Bayer Schering Pharma AG
    Inventors: Rolf Bohlmann, Martin Haberey, Andreas Huth, Stuart Ince, Martin Krueger, Karl-Heinz Thierauch, Holger Hess-Stumpp, Andreas Reichel
  • Patent number: 7893049
    Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R6 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: April 5, 2007
    Date of Patent: February 22, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Darryl McConnell, Bodo Betzemeier, Thomas Gerstberger, Maria Impagnatiello, Steffen Steurer, Lars van der Veen, Ulrike Weyer-Czernilofsky
  • Publication number: 20110034512
    Abstract: Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Application
    Filed: April 23, 2009
    Publication date: February 10, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Darren Disalvo, Daniel Kuzmich, Can Mao, Hossein Razavi, Christopher Sarko, Alan David Swinamer, David Smith Thomson, Qiang Zhang
  • Publication number: 20110028447
    Abstract: This invention relates to compounds, pharmaceutical compositions and methods for the treatment of a condition mediated by CB1 receptor activity in a mammalian subject including a human, which comprises administering to a mammal in need of such treatment a therapeutically effective amount of the compound of formula (I) wherein R1, R2 and R3 are as defined in this specification.
    Type: Application
    Filed: February 26, 2009
    Publication date: February 3, 2011
    Inventors: Ingrid Price Buchler, Michael Joseph Hayes, Shridhar Gajanan Hegde, Susan Landis Hockerman, Darin Eugene Jones, Steven Wade Kortum, Joseph Gerace Rico, Ruth Elizabeth TenBrink, Kun Ken Wu
  • Publication number: 20110028451
    Abstract: The invention relates to benzoindazole derivatives according to general Formula I or a pharmaceutically acceptable salt thereof. The compounds can be used for the treatment of infertility.
    Type: Application
    Filed: July 29, 2010
    Publication date: February 3, 2011
    Applicant: N.V. Organon
    Inventors: Cornelis Marius Timmers, Hubert Jan Jozef Loozen
  • Publication number: 20110015234
    Abstract: The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used in the prevention or treatment of diseases which are modulated by L-CPT1 inhibitors.
    Type: Application
    Filed: September 8, 2010
    Publication date: January 20, 2011
    Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
  • Patent number: 7863454
    Abstract: 3-substituted-6-aryl pyridines of Formula I are provided: wherein R1, R2, R3, R8, R9, A and Ar are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. The present invention also relates to pharmaceutical compositions comprising such compounds, and to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. In addition, the present invention provides labeled 3-substituted-6-aryl pyridines, which are useful as probes for the localization of C5a receptors.
    Type: Grant
    Filed: March 3, 2008
    Date of Patent: January 4, 2011
    Assignee: Novartis International Pharmaceutical Ltd.
    Inventors: Alan J. Hutchison, Jun Yuan, Kyungae Lee, George D. Maynard, Bertrand L. Chenard, Nian Liu, Qin Guo, Zihong Guo, Peter Hrnciar
  • Patent number: 7858645
    Abstract: The invention is concerned with novel indazole derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used in the prevention or treatment of diseases which are modulated by L-CPT1 inhibitors.
    Type: Grant
    Filed: October 19, 2007
    Date of Patent: December 28, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei
  • Patent number: 7855203
    Abstract: The present invention is directed to novel indazolyl-substituted pyrroline compounds of Formula (I): useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: December 21, 2010
    Assignee: Ortho-McNeil-Janssen Pharmaceuticals, Inc.
    Inventors: Han-Cheng Zhang, Bruce Maryanoff, Kimberly White, Hong Ye, Leonard R. Hecker, David F. McComsey
  • Publication number: 20100317618
    Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of novel 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1 and CX3CR1, and to their use in a method for treating or preventing diseases based on the expression of MCP-1 and CX3CR1.
    Type: Application
    Filed: March 6, 2009
    Publication date: December 16, 2010
    Applicant: AZIENDE CHIM. RIUN. ANGEL. FRA. A.C.R.A.F. S.p.A.
    Inventors: Angelo Guglielmotti, Guido Furlotti, Giorgina Mangano, Nicola Cazzolla
  • Publication number: 20100311744
    Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.
    Type: Application
    Filed: March 5, 2009
    Publication date: December 9, 2010
    Applicant: AZIENDE CHIM. RIUN. ANG. FRANC. A.C.R.A.F. S.p.A.
    Inventors: Angelo Guglielmotti, Guido Furlotti, Giorgina Mangano, Nicola Cazzolla, Barbara Garofalo
  • Publication number: 20100280016
    Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.
    Type: Application
    Filed: July 12, 2010
    Publication date: November 4, 2010
    Inventors: Marvin J. Meyers, Graciela B. Arhancet, XiangYang Chen, Susan Hockerman, Scott A. Long, Matthew W. Mahoney, David B. Reitz, Joseph G. Rico
  • Publication number: 20100273830
    Abstract: An insecticidal compound of formula (I) in which G1, G2, and G3 together with the two carbon atoms to which G1 and G3 are attached, form a non-aromatic 4- or 5-membered ring system; wherein G1 is sulfur, SO, SO2, oxygen, a direct bond, NRa or CR5aR5b; G2 is sulfur, SO, SO2, oxygen, a direct bond, NRb or CR5cR5d; G3 is sulfur, SO, SO2, oxygen, a direct bond, NRc or CR5eR5f; with the provisos that a) not more than 1 group G can be a direct bond, b) not more than 2 G groups can be oxygen, sulfur, SO or SO2 and c) when 2 G groups are oxygen, SO, SO2 and/or sulfur the two groups are separated by a carbon atom; each of Z1 and Z2, which may be the same or different, represents oxygen or sulfur; D is phenyl or a 5- or 6-membered heteroaromatic ring and R1a, R1b, R5a, R5b, R5c, R5d, R5e, R5f, Ra, Rb Rc, R2, R3 and R20 are specified organic groups and agronomically acceptable salts/isomers/enantiomers/tautomers/N-oxides of those compounds.
    Type: Application
    Filed: July 14, 2008
    Publication date: October 28, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Roger Graham Hall, Olivier Loiseleur, Jagadish Pabba, Sitaram Pal, Andre Jeanguenat, Andrew Edmunds, Andre Stoller
  • Publication number: 20100261724
    Abstract: The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which T-type calcium channels are involved.
    Type: Application
    Filed: October 23, 2008
    Publication date: October 14, 2010
    Inventors: James C. Barrow, Paul J. Coleman, Thomas S. Reger, Kelly-Ann S. Schlegel, Youheng Shu, Zhi-Qiang Yang
  • Publication number: 20100256108
    Abstract: A compound of the formula: wherein ring X is benzene or pyridine; R1 is substituted alkyl; R2 is optionally substituted aryl or optionally substituted heterocyclic group; R3 is hydrogen or alkyl; R4 is hydrogen, halogen or alkyl; R5 is hydrogen or alkyl; R6 and R7 are the same or different and each hydrogen or halogen, or a pharmaceutically acceptable salt thereof, which is useful as IKur blocker effective for preventing or treating cardiac arrhythmia such as atrial fibrillation.
    Type: Application
    Filed: September 26, 2008
    Publication date: October 7, 2010
    Inventors: Tetsuo Yamaguchi, Hiroyuki Kawanishi, Hideki Ushirogochi, Tatsuyuki Takahashi, Tohru Takebe