The Ring Nitrogens Are Bonded Directly To Each Other (e.g., Pyridazine, Etc.) Patents (Class 514/236.5)
-
Publication number: 20140080801Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: November 18, 2013Publication date: March 20, 2014Applicant: Genentech, Inc.Inventors: Alastair James Hodges, Mizio Matteucci, Andrew Sharpe, Minghua Sun, Xiaojing Wang, Vickie H. Tsui
-
Patent number: 8673911Abstract: This invention relates to compounds and methods for the inhibition of HDAC enzymatic activity. More particularly, the invention provides for compounds of formula (I), (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein L, M, n, R, W, X and Y are as defined in the specification.Type: GrantFiled: November 3, 2008Date of Patent: March 18, 2014Assignee: MethylGene Inc.Inventors: Tammy Mallais, Oscar Moradei, Alain Ajamian, Pierre Tessier, David Smil, Sylvie Frechette, Silvana Leit, Patrick Beaulieu, Robert Deziel, John Mancuso
-
Publication number: 20140073634Abstract: The present invention relates to compounds and methods which may be useful as inhibitors of HIF pathway activity for the treatment or prevention of cancer and other hypoxia-mediated diseases.Type: ApplicationFiled: August 23, 2013Publication date: March 13, 2014Applicant: Institute For Applied Cancer Science/The University of Texas MD Anderson Cancer CenterInventors: Philip Jones, Maria Emilia DiFrancesco, Alessia Petrocchi, Joe Marszalek, Gang Liu, Zhijun Kang, Chris Carroll, Timothy McAfoos, Barbara Czako
-
Publication number: 20140057915Abstract: There are provided compounds of formula I, wherein R, R1, Ra, Rb, Q, X and Y have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.Type: ApplicationFiled: August 16, 2013Publication date: February 27, 2014Applicants: TOPIVERT PHARMA LIMITED, RESPIVERT LIMITEDInventors: CLAIRE ANNE MARIE CARIOU, CATHERINE ELISABETH CHARRON, EUAN ALEXANDER FRASER FORDYCE, MATTHEW COLIN THOR FYFE, DANIEL HAMZA, KAZUHIRO ITO, JOHN KING-UNDERWOOD, PETER JOHN MURRAY, STUART THOMAS ONIONS, STEPHEN MALCOLM THOM, HAYLEY TEGAN ANGELA WATSON, JONATHAN GARETH WILLIAMS
-
Patent number: 8658643Abstract: Compounds selected from the group according to claim 1 are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: August 3, 2012Date of Patent: February 25, 2014Assignee: Merck Patent GmbHInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
-
Publication number: 20140051660Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein R1, R2, R3, Q, and G are defined herein.Type: ApplicationFiled: August 16, 2013Publication date: February 20, 2014Applicant: Janssen Pharmaceutica NVInventors: Michael WINTERS, Zhihua Sui, Christopher Flores
-
Publication number: 20140051672Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: August 7, 2013Publication date: February 20, 2014Inventors: Atwood Kim CHEUNG, Donovan Noel CHIN, Natalie DALES, Aleem FAZAL, Timothy Brian HURLEY, John KERRIGAN, Gary O'BRIEN, Lei SHU, Robert SUN, Moo Je SUNG
-
Publication number: 20140051677Abstract: Novel pyrrazolopyridines according to Formula I, able to inhibit JAK are disclosed, these compounds may be prepared as a pharmaceutical composition, and may be used for the prophylaxis and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, allergy, inflammatory conditions, autoimmune diseases, proliferative diseases, transplant rejection, diseases involving impairment of cartilage turnover, congenital cartilage malformations, and/or diseases associated with hypersecretion of IL6 or interferons.Type: ApplicationFiled: April 26, 2012Publication date: February 20, 2014Inventors: Christel Jeanne Marie Menet, Alastair James Hodges, Huw David Vater
-
Publication number: 20140045813Abstract: The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y 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: August 8, 2013Publication date: February 13, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Joerg Martin BENTZIEN, Angela Kay BERRY, Todd BOSANAC, Michael Jason BURKE, Darren Todd DISALVO, Joshua Courtney HORAN, Shuang LIANG, Can MAO, Wang MAO, Yue SHEN, Fariba SOLEYMANZADEH, Renee M. ZINDELL
-
Patent number: 8648072Abstract: The present invention provides novel pyrazolines that are useful as cannabinoid receptor blockers and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, inflammatory disorders, cardiometabolic disorders, hepatic disorders, and/or cancers.Type: GrantFiled: June 29, 2012Date of Patent: February 11, 2014Assignee: Jenrin Discovery, Inc.Inventors: John F. McElroy, Robert J. Chorvat
-
Publication number: 20140031331Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: September 19, 2013Publication date: January 30, 2014Inventors: Wilhelm Amberg, Michael Ochse, Udo Lange, Andreas Kling, Berthold Behl, Wilfried Hornberger, Mario Mezler, Charles W. Hutchins
-
Publication number: 20140031329Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: ApplicationFiled: February 18, 2013Publication date: January 30, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventor: BAYER INTELLECTUAL PROPERTY GmbH
-
Patent number: 8637508Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.Type: GrantFiled: January 11, 2012Date of Patent: January 28, 2014Assignee: Novartis AGInventors: Sangamesh Badiger, Murali Chebrolu, Konstanze Hurth, Sébastien Jacquier, Rainer Martin Lueoend, Rainer Machauer, Heinrich Rueeger, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
-
Patent number: 8629132Abstract: The present invention provides a new group of protein kinase inhibitors, pyrropyrimidine and pyrazolopyrimidine derivatives, and pharmaceutically acceptable salts and prodrugs thereof that are useful for treating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. The invention also provides useful intermediates generated during the syntheses of the pyrropyrimidine and pyrazolopyrimidine derivatives.Type: GrantFiled: November 12, 2010Date of Patent: January 14, 2014Assignees: Genosco, Oscotec, Inc.Inventors: Jaekyoo Lee, Ho-Juhn Song, Jong Sung Koh, Hee Kyu Lee, Youngsam Kim, Hong Woo Kim, Sunhwa Chang, Sun-Hee Lim, Jang-Sik Choi, Jung-Ho Kim, Se-Won Kim
-
Patent number: 8623866Abstract: The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.Type: GrantFiled: June 2, 2011Date of Patent: January 7, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Konrad Bleicher, Alexander Flohr, Katrin Groebke Zbinden, Felix Gruber, Matthias Koerner, Bernd Kuhn, Jens-Uwe Peters, Rosa Maria Rodriguez-Sarmiento
-
Publication number: 20130345120Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.Type: ApplicationFiled: March 9, 2012Publication date: December 26, 2013Applicant: Glaxosmithkline LLCInventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
-
Patent number: 8614214Abstract: Disclosed is a pyrazole amide compound having fungicidal activity, with a structure shown by the general formula (I): Each of the substituents of the compound being defined as in the description. The compound of the present invention has fungicidal activity, and excellent prevention and controlling effects on diseases, such as cucumber downy mildew, corn rust, wheat powdery mildew, rice blast, etc., and in particular, a better prevention and controlling effect on cucumber downy mildew and corn rust. Also disclosed is a process for preparing the compound, a fungicidal composition containing the compound of general formula (I) and the use thereof in preventing and controlling disease in crops.Type: GrantFiled: November 2, 2011Date of Patent: December 24, 2013Assignee: Sinochem CorporationInventors: Changling Liu, Lizeng Wang, Zhinian Li, Xufeng Sun, Jie Lan, Lanhui Ren, Qiang Wu, Huiwei Chi
-
Publication number: 20130331382Abstract: The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, J, and X3 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, diabetes, obesity, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula I.Type: ApplicationFiled: March 12, 2013Publication date: December 12, 2013Inventors: Robert D. HUBBARD, Le WANG, Chang H. PARK, Chaohong SUN, Keith F. McDANIEL, John K. PRATT, Todd N. SOLTWEDEL, Michael D. WENDT, John H. HOLMS, Dachun LIU, George S. SHEPPARD
-
Publication number: 20130330365Abstract: In one aspect, the invention relates to compounds having the formula X: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Adam D. Hughes, Melissa Fleury
-
Patent number: 8604016Abstract: The invention relates to novel heterocyclic compounds and pharmaceutical preparations thereof. The invention further relates to methods of treatment using the novel heterocyclic compounds of the invention.Type: GrantFiled: November 19, 2012Date of Patent: December 10, 2013Assignee: Calithera Biosciences Inc.Inventors: Jim Li, Lijing Chen, Bindu Goyal, Guy Laidig, Timothy Friend Stanton, Eric Brian Sjogren
-
Patent number: 8604022Abstract: There is provided a compound of formula (I): or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: GrantFiled: January 26, 2012Date of Patent: December 10, 2013Assignee: AstraZeneca ABInventors: Kevin Michael Foote, Maria-Elena Theoclitou, Andrew Peter Thomas, David Buttar
-
Publication number: 20130324536Abstract: The invention provides pyrazolyl guanidine compounds that inhibit F1Fo-ATPase, and methods of using pyrazolyl guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.Type: ApplicationFiled: December 8, 2011Publication date: December 5, 2013Applicant: Lycera CorporationInventors: Gary D. Glick, Alexander R. Hurd, Clarke B. Taylor, Chad A. Van Huis
-
Publication number: 20130324535Abstract: The invention refers to the use of a sigma ligand, particularly a sigma ligand of formula (I) to prevent and/or treat pain associated to bone cancer.Type: ApplicationFiled: December 2, 2011Publication date: December 5, 2013Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Daniel Zamanillo-Castanedo, José Miguel Vela-Hernández, Carlos Plata-Salaman
-
Publication number: 20130310361Abstract: The invention provides novel pyrimidine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of insulin-like growth factor (IGF-1R) or analplastic lymphoma kinase (ALK).Type: ApplicationFiled: July 23, 2013Publication date: November 21, 2013Inventors: Thomas H. Marsilje, Wenshuo Lu, Bei Chen, Xiaohui He, Christian Cho-Hua Lee, Songchun Jiang, Kunyong Yang
-
Publication number: 20130303540Abstract: The invention relates to pyrazole derivatives of formula I having pharmacological activity and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and/or prophylaxis of pain.Type: ApplicationFiled: December 2, 2011Publication date: November 14, 2013Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Antoni Torrens Jover, María Rosa Cuberes-Altisen
-
Publication number: 20130303492Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: March 14, 2013Publication date: November 14, 2013Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
-
Patent number: 8580781Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4? have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: April 29, 2008Date of Patent: November 12, 2013Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat
-
Publication number: 20130296321Abstract: The present invention relates to processes for preparing phenyl-pyrazoles of Formula (I) and salts and pharmaceutical compositions thereof, useful as modulators of 5-HT2A serotonin receptor activity. The present invention also relates to intermediates used in the processes, and their preparation. The present invention also relates to crystalline forms of 5-HT2A serotonin receptor modulators, compositions thereof and methods of using the same.Type: ApplicationFiled: July 3, 2013Publication date: November 7, 2013Inventors: Tawfik Gharbaoui, Dipanjan Sengupta, Ashwin M. Krishnan, Nainesh Shah, Ryan M. Hart, Mark Macias, Edward A. Lally, Jonathan Duffield
-
Publication number: 20130289025Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted pyrazolyl, and R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: ApplicationFiled: March 20, 2013Publication date: October 31, 2013Inventors: Li Chen, Michael Patrick Dillon, Lichun Feng, Ronald Charles Hawley, Minmin Yang
-
Publication number: 20130291227Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.Type: ApplicationFiled: March 7, 2013Publication date: October 31, 2013Applicant: DOW AGROSCIENCES LLCInventors: Ann M. Buysse, Noormohamed M. Niyaz, Yu Zhang, Martin J. Walsh, Asako Kubota, Ricky Hunter, Tony K. Trullinger, Christian T. Lowe, Daniel Knueppel, David A. Demeter, Akshay Patny, Negar Garizi, Paul Renee LePlae, JR., Frank Wessels
-
Patent number: 8569376Abstract: Provided are methods of reducing body fat in a subject, comprising locally (e.g., topically) administering one or more compounds of the Formula (I) and/or (V): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein X is —OR1, —SR2, or —NR3R4, and R1, R2, R3, R4, R5, R6, R7, R7?, Z, Y, n, y, and x, are as defined herein.Type: GrantFiled: March 1, 2013Date of Patent: October 29, 2013Assignee: Topokine Therapeutics, Inc.Inventors: Murat V. Kalayoglu, Michael S. Singer
-
Patent number: 8569299Abstract: Compounds of structural formulas I-1 and I-2 are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.Type: GrantFiled: June 3, 2011Date of Patent: October 29, 2013Assignee: Merck Sharp & Dohme CorpInventors: Thomas H. Graham, Wensheng Liu, Iyassu K. Sebhat, Dong-Ming Shen, Zhi-Cai Shi
-
Patent number: 8569298Abstract: The present invention relates to compounds that inhibit of focal adhesion kinase function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm-blooded animals such as humans of diseases such as cancer.Type: GrantFiled: June 15, 2009Date of Patent: October 29, 2013Assignee: Astrazeneca ABInventors: Bernard Christophe Barlaam, Patrick Ple, Kevin Michael Foote, Clifford David Jones
-
Publication number: 20130281455Abstract: Phenylpyri(mi)dinylazoles of the formula [I-a] and [I-b], wherein the symbols have the meanings stated in the description, and agrochemically active salts thereof and the use thereof for the control of undesired microorganisms in the protection of plants and materials and for the reduction of mycotoxins in plants and plant parts and methods for the production of compounds of the formula [I-a] and [I-b].Type: ApplicationFiled: March 15, 2013Publication date: October 24, 2013Inventors: Alexander SUDAU, Mazen ES-SAYED, Christoph Andreas BRAUN, Ruth MEISSNER, Catherine SIRVEN, Jürgen BENTING, Peter DAHMEN, Daniela PORTZ, Ulrike WACHENDORFF-NEUMANN, Philippe DESBORDES, Samir BENNABI, Christophe CATHERIN, Anne-Sophie REBSTOCK, Marie-Claire GROSJEAN-COURNOYER, Hiroyuki HADANO, Thomas KNOBLOCH, Philippe RINOLFI
-
Publication number: 20130281449Abstract: The invention relates to novel heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification, in free form or in pharmaceutically acceptable salt form, to their preparation, to their medical use and to medicaments comprising them.Type: ApplicationFiled: January 11, 2012Publication date: October 24, 2013Applicant: NOVARTIS AGInventors: Konstanze Hurth, Rainer Martin Lueoend, Rainer Machauer, Ulf Neumann, Heinrich Rueeger, Michael Schaefer, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
-
Publication number: 20130281426Abstract: The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.Type: ApplicationFiled: June 18, 2013Publication date: October 24, 2013Inventors: Youhong HU, Liguang Lou, Shijun Lin, Hongbing Zhao, Zhende Liu, Yongping Xu, Bo Chao
-
Patent number: 8563552Abstract: The present invention provides a compound having an excellent inhibitory action on melanin production and being useful as a whitening agent, and a skin external preparation containing the compound. The whitening agent of the present invention comprises, as an active ingredient, a compound represented by formula (1) or a pharmacologically acceptable salt thereof: wherein X1, X2, and X3 are each CR2 or N; R1, R2, and R3 are each H, C1-6 alkyl, C1-6 alkoxy, SH, OH, or NRbRc, wherein Rb and Rc are each H, C1-6 alkyl, or hydroxy-C1-6 alkyl, or NRbRc forms a saturated or unsaturated 5- or 6-membered hetero ring; and B is a substituted or unsubstituted pyrazole, imidazole, pyridine, or piperidine; with the proviso that at least one of R1, R3, R4, and R6 is a group other than C1-3 alkyl in the case where X1?X2?Y1?N and X3?CR2.Type: GrantFiled: February 6, 2009Date of Patent: October 22, 2013Assignee: Shiseido Company Ltd.Inventors: Naoto Hanyu, Tomoko Saito, Takako Shibata, Kiyoshi Sato, Kimihiro Ogino
-
Publication number: 20130274227Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.Type: ApplicationFiled: March 14, 2013Publication date: October 17, 2013Applicant: Axikin Pharmaceuticals, Inc.Inventors: Erik Dean RAAUM, Garrett Thomas Potter, Tai Wei Ly
-
Patent number: 8557813Abstract: Compounds of the formula I in which R1, R2, R3, R4? have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: November 25, 2008Date of Patent: October 15, 2013Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
-
Publication number: 20130267519Abstract: This invention relates to novel 1,2-pyridazines, 1,6-pyridazines or pyrimidines of the formula wherein B1 to B3 and R1 to R7 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may therefore be useful as medicaments for the treatment of diseases such as type II diabetes.Type: ApplicationFiled: April 3, 2013Publication date: October 10, 2013Applicant: Hoffmann-La Roche Inc.Inventors: Henrietta Dehmlow, Shawn David Erickson, Patrizio Mattei, Hans Richter
-
Patent number: 8536165Abstract: The present disclosure relates to new azabiphenylaminobenzoic acid derivatives of formula (I); as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).Type: GrantFiled: August 8, 2008Date of Patent: September 17, 2013Assignee: Almirall, S.A.Inventors: Julio Cesar Castro Palomino Laria, Emma Terricabras Belart, Montserrat Erra Sola, Eloisa Navarro Romero, Silvia Fonquerna Pou, Aranzazu Cardus Figueras, Maria Estrella Lozoya Toribio
-
Publication number: 20130237541Abstract: The present invention relates to certain pyrazole derivatives of Formula (I) 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 prophylaxis or 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 and the like.Type: ApplicationFiled: September 14, 2012Publication date: September 12, 2013Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Bradley Teegarden, Honnappa Jayakumar, Hongmei Li, Sonja Strah-Pleynet, Peter Ian Dosa
-
Publication number: 20130237515Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2, L1, L2, U and B are as defined in the application, which have valuable pharmacological properties, and in particular modulate the activity of the MCH receptor.Type: ApplicationFiled: February 28, 2013Publication date: September 12, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Thorsten OOST, Ralf LOTZ, Dirk STENKAMP
-
Publication number: 20130237540Abstract: The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: September 14, 2012Publication date: September 12, 2013Inventors: BRADLEY TEEGARDEN, YIFENG XIONG, SONJA STRAH-PLEYNET, HONNAPPA JAYAKUMAR, PETER I. DOSA, KONRAD FEICHTINGER, MARTIN CASPER, JUERG LEHMANN, ROBERT M. JONES, DAVID J. UNETT, JIN SUN KAROLINE CHOI
-
Publication number: 20130225585Abstract: Disclosed is a pyrazole amide compound having fungicidal activity, with a structure shown by the general formula (I): Each of the substituents of the compound being defined as in the description. The compound of the present invention has fungicidal activity, and excellent prevention and controlling effects on diseases, such as cucumber downy mildew, corn rust, wheat powdery mildew, rice blast, etc., and in particular, a better prevention and controlling effect on cucumber downy mildew and corn rust. Also disclosed is a process for preparing the compound, a fungicidal composition containing the compound of general formula (I) and the use thereof in preventing and controlling disease in crops.Type: ApplicationFiled: November 2, 2011Publication date: August 29, 2013Applicants: SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY CO., LTD., SINOCHEM CORPORATIONInventors: Changling Liu, Lizeng Wang, Zhinian Li, Xufeng Sun, Jie Lan, Lanhui Ren, Qiang Wu, Huiwei Chi
-
Publication number: 20130225584Abstract: The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by LRRK2 kinase activity, for example Parkinson's disease or Alzheimer's disease.Type: ApplicationFiled: August 31, 2011Publication date: August 29, 2013Inventors: Daniele Andreotti, Xuedong Dai, Andrew John Eatherton, Karamjit Singh Jandu, Qian Liu, Oliver James Philps
-
Publication number: 20130217689Abstract: This invention provides compounds of formula I: wherein R1, R2, CY, Y1, Y2, X1, X2, and X3 are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: April 1, 2013Publication date: August 22, 2013Applicant: Millennium Pharmaceuticals, Inc.Inventor: Millennium Pharmaceuticals, Inc.
-
Patent number: 8513244Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, R4, and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: May 18, 2012Date of Patent: August 20, 2013Assignee: Theravance, Inc.Inventors: Roland Gendron, Adam D. Hughes
-
Publication number: 20130210809Abstract: The present invention relates to novel compounds of Formula (1), wherein M, A and B are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors-subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: July 12, 2011Publication date: August 15, 2013Inventors: Christelle Boléa, Sylvain Celanire, Cédric Boudou, Lam Tang, Jean-Philippe Rocher, Nigel John Liverton
-
Patent number: 8501731Abstract: The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.Type: GrantFiled: March 18, 2009Date of Patent: August 6, 2013Assignee: Shanghai Institute of Materia Medica, Chinese Academy of SciencesInventors: Youhong Hu, Liguang Lou, Shijun Lin, Hongbing Zhao, Zhende Liu, Yongping Xu, Bo Chao