Ring Sulfur Or Ring Oxygen In The Additional Hetero Ring Patents (Class 546/209)
-
Publication number: 20150024935Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols RA1, RA2, X, Y, L1, L2, RB1, RB2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).Type: ApplicationFiled: December 21, 2012Publication date: January 22, 2015Applicant: Bayer Intellectual Property GmbHInventors: Tomoki Tsuchiya, Pierre Wasnaire, Sebastian Hoffmann, Thomas Seitz, Stefan Hillebrand, Jürgen Benting, Jan Peter Schmidt, Pierre Cristau
-
Publication number: 20150018330Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: ApplicationFiled: July 30, 2014Publication date: January 15, 2015Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. MacDonald, Thomas Eric Ballard, JR.
-
Patent number: 8933075Abstract: Novel 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives that are effective for use in treating viral infections are described. Also described are pharmaceutical compositions comprising the 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives and methods for using the compounds or compositions.Type: GrantFiled: June 17, 2011Date of Patent: January 13, 2015Assignees: FUZIANS BIOMEDICALS, Inc., The UAB Research FoundationInventors: Guoxin Wang, Ming Luo, Zhen Yang
-
Patent number: 8933101Abstract: The present invention relates to [1-(benzyl)-piperidin-4-yl]-([1,3,4]thiadiazol-2-yl)-amine and [1-(benzyl)-piperidin-4-yl]-(thiazol-2-yl)-amine derivatives of formula (I) that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.Type: GrantFiled: April 18, 2008Date of Patent: January 13, 2015Assignee: Janssen Pharmaceutica NVInventors: Gregor James MacDonald, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool
-
Publication number: 20150011526Abstract: The present invention relates to 2-oxo-piperidinyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: October 10, 2012Publication date: January 8, 2015Inventors: Ali Ates, Florian Montel, Anne Valade, Olivier Lorthioir
-
Patent number: 8927551Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.Type: GrantFiled: May 18, 2010Date of Patent: January 6, 2015Assignee: Infinity Pharmaceuticals, Inc.Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
-
Patent number: 8921398Abstract: The present invention relates to compounds of general formula I, wherein R1, LP, HetAr, Ar, and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: GrantFiled: June 6, 2012Date of Patent: December 30, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Armin Heckel, Frank Himmelsbach, Elke Langkopf, Bernd Nosse, Neil J. Ashweek, Nicole Harriott
-
Patent number: 8921559Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: GrantFiled: November 30, 2011Date of Patent: December 30, 2014Assignee: Janssen Pharmaceutica NVInventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui, Xuqing Zhang
-
Patent number: 8921544Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: GrantFiled: June 3, 2014Date of Patent: December 30, 2014Assignee: Sareum LimitedInventors: John Charles Reader, John Mark Ellard, Helen Boffey, Susanne Taylor, Andrew David Carr, Michael Cherry, Michelle Wilson, Richard Boakye Owoare
-
Publication number: 20140377292Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: September 5, 2014Publication date: December 25, 2014Applicant: Incyte CorporationInventors: Andrew P. Combs, Eddy W. Yue
-
Publication number: 20140377219Abstract: Chemical compounds that inhibit retroviruses are presented herein. More particularly, this disclosure provides small molecule compounds that inhibit infection with, or treat infection caused by, human immunodeficiency viruses.Type: ApplicationFiled: September 6, 2012Publication date: December 25, 2014Applicant: New York Blood CEnter, Inc.Inventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
-
Publication number: 20140371238Abstract: The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:Type: ApplicationFiled: March 13, 2014Publication date: December 18, 2014Applicant: FLATLEY DISCOVERY LABInventors: Michael P. Zawistoski, Yevgen Barsukov, Bridget M. Cole, Richard A. Nugent
-
Publication number: 20140371239Abstract: The present invention relates generally to compounds that inhibit the binding of menin and MLL or MLL fusion proteins and methods of use thereof. In particular embodiments, the present invention provides compositions comprising piperidine-containing compounds and methods of use thereof to inhibit the interaction of menin with MLL oncoproteins (e.g., MLL1, MLL2, MLL-fusion oncoproteins), for example, for the treatment of leukemia, solid cancers, diabetes, and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, MLL-PTD and/or menin.Type: ApplicationFiled: June 11, 2014Publication date: December 18, 2014Inventors: Jolanta Grembecka, Tomasz Cierpicki, Sunil Kumar Upadhyay, Shaun R. Stauffer, Rocco D. Gogliotti, Timothy J. Senter
-
Publication number: 20140371176Abstract: This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.Type: ApplicationFiled: September 3, 2014Publication date: December 18, 2014Inventors: Neil W. Johnson, Jiri Kasparec, Meagan B. Rouse, Xinrong Tian
-
Publication number: 20140371269Abstract: The present invention provides compounds of Formula I or a pharmaceutical salt thereof, where the variables for R1, R2, and R3 are as described herein; methods of treating a condition such as hypertriglyceridemia; and processes for preparing the compounds.Type: ApplicationFiled: January 16, 2013Publication date: December 18, 2014Applicant: Eli Lilly and CompanyInventors: Maria Carmen Fernandez, Maria Rosario Gonzalez-Garcia, Bin Liu, Lance Allen Pfeifer
-
Publication number: 20140363454Abstract: Antibody-cytotoxin antibody-drug conjugates and related compounds, such as linker-cytotoxin conjugates and the linkers used to make them, tubulysin analogs, and intermediates in their synthesis; compositions; and methods, including methods of treating cancers.Type: ApplicationFiled: June 6, 2014Publication date: December 11, 2014Applicant: Igenica Biotherapeutics, Inc.Inventors: David Y. Jackson, Edward Ha, Gary D. Probst
-
Publication number: 20140364433Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.Type: ApplicationFiled: August 14, 2014Publication date: December 11, 2014Inventors: Theodore M. KAMENECKA, Yuanjun HE, Rong JIANG, William NGUYEN, Xinyi SONG
-
Publication number: 20140364432Abstract: The present invention is directed to compounds that modulate the bioactivity of an orexin receptor such as OX1 or OX2, or both; to pharmaceutical compositions and combinations comprising a compound of the invention; to methods of treatment of malconditions in patients wherein modulation of an orexin receptor is medically indicated; and to methods of preparation of compounds of the invention.Type: ApplicationFiled: February 12, 2014Publication date: December 11, 2014Inventors: Theodore M. KAMENECKA, Yuanjun HE, William NGUYEN, Rong Jiang, Xinyi Song
-
Patent number: 8907098Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, Y1, Y2, V, W, n, m and o have the meanings given herein, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.Type: GrantFiled: November 18, 2010Date of Patent: December 9, 2014Assignee: MERCK PATENT GmbHInventors: Frank Stieber, Dirk Wienke
-
Publication number: 20140356322Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins that are degraded and/or otherwise inhibited by bifunctional compounds of the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand that binds to the ubiquitin ligase and on the other end a moiety that binds a target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds of the present invention, consistent with the degradation/inhibition of targeted polypeptides.Type: ApplicationFiled: January 11, 2013Publication date: December 4, 2014Inventors: Craig M. Crews, Dennis Buckley, Alessio Ciulli, William Jorgensen, Peter C. Gareiss, Inge Van Molle, Jeffrey Gustafson, Hyun-Seop Tae, Julien Michel, Dentin Wade Hoyer, Anke G. Roth, John David Harling, Ian Edward David Smith, Afjal Hussain Miah, Sebastien Andre Campos, Joelle Le
-
Patent number: 8901307Abstract: The invention relates to chemical compounds of formula (I), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of PIM-1 and/or PIM-2, and/or PIM-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of PIM kinase related conditions and diseases, preferably cancer.Type: GrantFiled: July 2, 2009Date of Patent: December 2, 2014Assignee: AstraZeneca ABInventors: Leslie Dakin, James Edward Dowling, Michelle Lamb, Jon Read, Xiaolan Zheng
-
Patent number: 8901152Abstract: The present invention relates to compounds of formula (I): wherein Q, G1, G2, and G3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.Type: GrantFiled: July 16, 2012Date of Patent: December 2, 2014Assignee: AbbVie Inc.Inventors: Andrew S. Judd, Mathew M. Mulhern, Rajesh R. Iyengar, Philip R. Kym, Andrew J. Souers
-
Patent number: 8895753Abstract: An object of the present invention is to provide a compound having a modulating activity at an S1P receptor which is useful for preventing and treating autoimmune diseases, allergic diseases, and the like. According to the present invention, a compound represented by formula (I) or a pharmaceutically acceptable salt thereof is provided.Type: GrantFiled: December 21, 2012Date of Patent: November 25, 2014Assignee: Meiji Seika Pharma Co., Ltd.Inventors: Satoshi Yoshida, Tomohisa Ninomiya
-
Patent number: 8895741Abstract: The present invention relates to processes for the preparation of biaryl oxazolidinones. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.Type: GrantFiled: September 14, 2012Date of Patent: November 25, 2014Assignee: Melinta Therapeutics, Inc.Inventors: Yusheng Wu, Shili Chen, Yi Chen, Roger Hanselmann, Rongliang Lou, Jiacheng Zhou
-
Patent number: 8895750Abstract: The present invention encompasses compounds of the formula (I) wherein the groups ring A and Cy are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.Type: GrantFiled: March 13, 2014Date of Patent: November 25, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Todd Bosanac, Michael J. Burke, Darren Disalvo, Wang Mao, John Westbrook
-
Publication number: 20140343017Abstract: Provided is a highly safe and effective compound represented by the following general formula (1) or a salt thereof which acts on tubulin and has an anticancer effect, wherein Ar represents an aryl group or a heteroaryl group; Z1, Z2, Z3, and Z4 each independently represent CH, a nitrogen atom, an oxygen atom, or a sulfur atom; R1 represents a hydrogen atom, a halogen atom, an alkyl group, or the like; R2 and R3 are the same or different and each represent a hydrogen atom, a halogen atom, a carboxyl group, or the like; n units of R4 are the same or different and each represent a hydrogen atom, an alkyl group, or the like; and n represents a number of 0 to 4.Type: ApplicationFiled: January 24, 2013Publication date: November 20, 2014Applicant: Kabushiki Kaisha Yakult HonshaInventors: Takashi Ikeda, Masahiro Ono, Satoshi Ueno, Ryuta Yamazaki, Takashi Yaegashi, Takeshi Matsuzaki
-
Patent number: 8889668Abstract: The invention relates to compounds of formula (I): wherein R1, R2, Ra, Rb, Rc and W, have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: GrantFiled: December 12, 2012Date of Patent: November 18, 2014Assignee: Merck Serono SAInventors: Cyril Montagne, Anna Quattropani, Wolfgang Sauer, Agnes Bombrun
-
Patent number: 8889670Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: February 16, 2010Date of Patent: November 18, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Alessandra Bartolozzi, Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell
-
Publication number: 20140336167Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.Type: ApplicationFiled: May 10, 2013Publication date: November 13, 2014Applicant: ABBVIE INC.Inventors: Ramzi F. Sweis, Michael L. Curtin, Marina A. Pliushchev, Todd M. Hansen, Kenton Longenecker
-
Publication number: 20140336388Abstract: The present invention provides nitrofurfuryl substituted phenyl linked piperidino-oxadiazolone compounds of general formula (A) as anti-tubercular agents; wherein G=formula (B); X?H, F; R?H, CH3, C2H5, Benzyl.Type: ApplicationFiled: December 18, 2012Publication date: November 13, 2014Inventors: Ahmed Kamal, Arutla Viswanath, Jayanti Naga Srirama Chandra Murty, Farheen Sulthana, Gadupudi Ramakrishna, Inshad Ali Khan, Nitin Pal Kalia
-
Patent number: 8884025Abstract: Processes and intermediates for the preparation of compounds of the Formula (1) and the pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, wherein R1, R2, and R3 have the definitions provided herein.Type: GrantFiled: August 2, 2005Date of Patent: November 11, 2014Inventors: David B. Damon, Brian P. Jones
-
Publication number: 20140329857Abstract: The invention provides compounds of the formula: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a, Z and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.Type: ApplicationFiled: July 18, 2014Publication date: November 6, 2014Applicant: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Craig Husfeld, YuHua Ji, Rick Lee, Li Li, YongQi Mu, Cameron Smith, Johnny Uy
-
Publication number: 20140330011Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 6, 2014Publication date: November 6, 2014Applicant: CYTOKINETICS, INCInventors: Luke W. Ashcraft, Gustave Bergnes, Chihyuan Chuang, Scott Collibee, Pu-Ping Lu, Bradley Morgan, Alex Muci, Xiangping Qian, Jeffrey Warrington, Zhe Yang
-
Patent number: 8865744Abstract: Disclosed are (cyano-dimethyl-methyl)-isoxazoles and -[1,3,4]thiadiazoles and their use as CB2 cannabinoid receptor agonists, pharmaceutical compositions containing the same, and their use for the treatment of CB2 receptor mediated disorders or conditions.Type: GrantFiled: May 15, 2014Date of Patent: October 21, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Doris Riether, Florian Paul Christian Binder, Henri Doods, Stephan Georg Mueller, Janet Rachel Nicholson, Achim Sauer
-
Publication number: 20140309226Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, in which X1, X2, R3, R4, R5, Rx, R7, R9, R10 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.Type: ApplicationFiled: November 14, 2012Publication date: October 16, 2014Inventors: Jay Bradford Fell, John P. Fischer, Ronald J. Hinklin
-
Publication number: 20140309238Abstract: The present invention relates to compounds of Formula (I), wherein R1 is chosen among the following radicals: (II); (III); (IV), (V), (VI) (VII) and n=1 or 2 and m=1 or 2 with the proviso that m=2 when R1 is (VIII). The present invention also relates to the use thereof as drugs, more particularly in the treatment of mycobacterial infections and more particularly in the treatment of tuberculosis.Type: ApplicationFiled: October 24, 2012Publication date: October 16, 2014Applicants: Universite de Droit et de la Sante de Lille 2, INSERM (Institut National de la Sante et de la Recherche Medicale), Institut Pasteur de LilleInventors: Benoit Deprez, Nicolas Willand, Marion Flipo, Matthieu Desroses, Alain Baulard, Florence Leroux
-
Publication number: 20140303210Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols are each as defined in the description, and agrochemically active salts thereof, and use thereof for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).Type: ApplicationFiled: May 29, 2014Publication date: October 9, 2014Applicant: BAYER CROPSCIENCE AGInventors: Sebastian HOFFMANN, Pierre WASNAIRE, Tomoki TSUCHIYA, Pierre CRISTAU, Thomas SEITZ, Joachim KLUTH, Jurgen BENTING, Ulrike WACHENDORFF-NEUMANN
-
Patent number: 8853219Abstract: Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.Type: GrantFiled: January 11, 2011Date of Patent: October 7, 2014Assignee: NeuroSolis, Inc.Inventors: Michael L. Hendrickson, Jeffrey C. Ockuly, Trevor M. Twose, Melinda L. Verdone, Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson
-
Publication number: 20140296202Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.Type: ApplicationFiled: October 18, 2012Publication date: October 2, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
-
Publication number: 20140296196Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.Type: ApplicationFiled: June 13, 2014Publication date: October 2, 2014Inventors: Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Sapna S. Shah, Neng-Yang Shih
-
Publication number: 20140296289Abstract: Thiazolyl oxime ethers and hydrazones of the formula (I), in which the symbols A, L1, L2, Y, W, X, R1, R2, R3, R4, R5, R6 and R7 have the meanings given in the description, and also agrochemically active salts thereof, and their use for controlling phytopathogenic harmful fungi, and also methods for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).Type: ApplicationFiled: February 28, 2014Publication date: October 2, 2014Applicant: Bayer CropScience AGInventors: Pierre CRISTAU, Nicola Rahn, Tomoki Tsuchiya, Ulrike Wachendorff-Neumann, Arnd Voerste, Jürgen Benting
-
Patent number: 8846675Abstract: Compounds and methods are provided for the treatment of, inter alia, Type II diabetes and other diseases associated with poor glycemic control.Type: GrantFiled: May 3, 2012Date of Patent: September 30, 2014Assignee: Cymabay Therapeutics, Inc.Inventors: Jingyuan Ma, Christopher J. Rabbat, Jiangao Song, Xin Chen, Imad Nashashibi, Zuchun Zhao, Aaron Novack, Dong Fang Shi, Peng Cheng, Yan Zhu, Alison Murphy
-
Publication number: 20140275041Abstract: The invention provides a compound which is an amide of the formula (1), or a salt, solvate, N-oxide or tautomer thereof; wherein: a is 0 or 1; b is 0 or 1: provided that the sum of a and b is 0 or 1; T is O or NH Ar1 is a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S, and being optionally substituted by one or more substituents R1; Ar2 Js a monocyclic or bicyclic 5- to 10-membered aryl or heteroaryl group containing up to 4 heteroatoms selected from O, N and S and being optionally substituted by one or more substituents R2; and R1 and R2 are as defined in the claims. The compounds are inhibitors of kinases and in particular FLT3, FLT4 and Aurora kinases.Type: ApplicationFiled: June 3, 2014Publication date: September 18, 2014Applicant: Sareum LimitedInventors: John Charles READER, John Mark ELLARD, Helen BOFFEY, Susanne TAYLOR, Andrew David CARR, Michael CHERRY, Michelle WILSON, Richard Boakye OWOARE
-
Publication number: 20140275032Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, n, p, q, r, A, X1, X2, X3, X4, X5, X6, Y, Z, G, R1a, R2a, R1b, R2b, R3, R4, R5 and R6 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Applicant: Genentech, Inc.Inventors: Benjamin Fauber, Olivier Rene, Monique Bodil van Niel, Stuart Ward
-
Publication number: 20140275012Abstract: The present invention encompasses compounds of the formula (I) wherein the groups ring A and Cy are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Todd BOSANAC, Michael J. BURKE, Darren DISALVO, Wang MAO, John WESTBROOK
-
Patent number: 8835437Abstract: The invention further relates to a DGAT inhibitor of formula (I), including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —S(?O)p—; C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —O—C(?O)—; —C(?O)—C(?O)—; R1 represents a 5-membered monocyclic heterocycle containing at least 2 heteroatoms; a 6-membered aromatic monocyclic heterocycle; or a 5-membered heterocycle containing at least 2 heteroatoms fused with phenyl, cyclohexyl or a 5-or 6-membered heterocycle; wherein each of said heterocycles may optionally be substituted; R2 represents R3; R3 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxlyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzo-dioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or 6-mType: GrantFiled: June 5, 2008Date of Patent: September 16, 2014Assignee: Janssen Pharmaceutica N.V.Inventors: Jean-Pierre André Marc Bongartz, Lieven Meerpoel, Gustaaf Maria Boeckx, Guy Rosalia Eugeen Van Lommen, Christophe Francis Robert Nestor Buyck, Daniel Obrecht, Philipp Ermert, Anatol Luther
-
Publication number: 20140256756Abstract: Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X1, X2, X3, L, R3, R4, R5, R7 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.Type: ApplicationFiled: October 30, 2012Publication date: September 11, 2014Inventors: Thomas Daniel Aicher, Josef Roland Benscik, Steven Armen Boyd, Kevin Ronald Condroski, Jay Bradford Fell, John Peter Fischer, Ronald Jay Hinklin, Scott Pratt, Ajay Singh, Timothy M. Turner
-
Publication number: 20140249315Abstract: Processes for preparing tubulysins and derivatives thereof are described. In addition, processes for preparing unnatural tubulysins are described.Type: ApplicationFiled: March 15, 2013Publication date: September 4, 2014Inventor: Endocyte, Inc.
-
Patent number: 8822466Abstract: The invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.Type: GrantFiled: March 9, 2012Date of Patent: September 2, 2014Assignee: Novartis AGInventors: Noëlle Gauvry, Steve Nanchen
-
Patent number: RE45183Abstract: This invention relates to compounds of formula (I) which are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.Type: GrantFiled: July 12, 2013Date of Patent: October 7, 2014Assignee: Novo Nordisk A/SInventors: Anthony Murray, Jesper Lau, Lone Jeppesen, Per Vedsoe, Michael Ankersen, Jane Marie Lundbeck, Marit Kristiansen, Maria Carmen Valcarce Lopez, Dharma Rao Polisetti, Govindan Subramanian, Robert Carl Andrews, Daniel P. Christen, Jeremy T. Cooper, Kalpathy Chidambareswaran Santhosh