Abstract: There is provided compounds of formula (I): wherein R1, R2 and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. PI3-K, particularly class I PI3K) is desired and/or required, and particularly in the treatment of cancer.
Type:
Grant
Filed:
April 1, 2010
Date of Patent:
August 26, 2014
Assignee:
Centro Nacional de Investigaciones Oncologicas (CNIO)
Inventors:
Joaquin Pastor Fernández, Guido Kurz, Sonia Martinez Gonzalez
Abstract: Compounds of the formula I, in which R1, R2, X and Y have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.
Abstract: The present invention relates to compounds of formula I wherein A, B, X, Y, Ar, R1, R2, R?, m and n are as defined herein and to pharmaceutical active acid addition salts thereof, which have a good affinity to the trace amine associated receptors TAAR1, so that they can be used for the treatment of depression, anxiety disorders and bipolar disorder.
Type:
Grant
Filed:
March 20, 2012
Date of Patent:
August 12, 2014
Assignee:
Hoffmann-La Roche Inc
Inventors:
Guido Galley, Roger David Norcross, Philippe Pflieger
Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.
Type:
Application
Filed:
February 4, 2014
Publication date:
August 7, 2014
Applicant:
Bayer CropScience AG
Inventors:
Thomas BRETSCHNEIDER, Martin Füßlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria FRANKEN, Arnd VOERSTE
Abstract: The present invention relates to compounds of formula I or a pharmaceutically acceptable salt thereof, wherein A1, A2, A3, L1, L2 and D are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the Compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.
Type:
Application
Filed:
July 17, 2012
Publication date:
August 7, 2014
Applicant:
BOEHRINGER INGELHEIM INTERNATIONAL GMBH
Inventors:
Alexander Heim-Riether, Anil Kumar Padyana, Shuang Liang, Steven John Taylor, Qiang Zhang
Abstract: A process is described for preparing aromatic and heteroaromatic amines of the general formula (I) Ar—NR1R2, in which an aromatic compound with the general formula (II) Ar—X is reacted in the presence of a catalyst with an amine of the general formula (III) H—NR1R2 and a base, wherein the catalyst is selected from transition metal complexes having one or more ligands with the general formula (IV).
Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
Abstract: The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as ROR?, ROR?, or ROR?. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.
Type:
Application
Filed:
May 16, 2012
Publication date:
July 3, 2014
Applicant:
The Scripps Research Institute
Inventors:
Theodore Mark Kamenecka, Patrick R. Griffin, Youseung Shin, Yuanjun He, Anne-Laure Blayo, Brent R. Lyda, Marcel Koenig, Naresh Kumar, Thomas Burris
Abstract: The invention relates to bicyclic compounds of formulas I and Ia, 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:
Application
Filed:
March 21, 2012
Publication date:
July 3, 2014
Applicant:
AMGEM INC.
Inventors:
Hui-Ling Wang, Victor J. Cee, Bradley J. Herberich, Claire L.M. Jackson, Brian Alan Lanman, Thomas Nixey, Liping H. Pettus, Anthony B. Reed, Bin Wu, Ryan Wurz, Andrew Tasker
Abstract: This invention relates to novel 1-hydroxyimino-3-phenyl-propanes of the formula wherein R1 to R10 are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds are GPBAR1 agonists and may be used as medicaments for the treatment of diseases such as type II diabetes.
Type:
Grant
Filed:
July 12, 2011
Date of Patent:
July 1, 2014
Assignee:
Hoffmann-La Roche Inc
Inventors:
Caterina Bissantz, Henrietta Dehmlow, Shawn David Erickson, Kyungjin Kim, Rainer E. Martin, Patrizio Mattei, Ulrike Obst Sander, Sherrie Lynn Pietranico-Cole, Hans Richter, Christoph Ullmer
Abstract: Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.
Type:
Application
Filed:
December 20, 2013
Publication date:
June 5, 2014
Applicant:
Ligand Pharmaceuticals Incorporated
Inventors:
Koc-Kan Ho, David Diller, Jeffrey J. Letourneau, Brian F. McGuinness, Andrew G. Cole, David Rosen, Cornelis A. van Oeveren, Jason C. Pickens, Lin Zhi, Yixing Shen, Bijan Pedram
Abstract: The present invention relates to novel substituted 2,4?- and 3,4?-bipyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.
Type:
Application
Filed:
February 7, 2014
Publication date:
June 5, 2014
Applicant:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Peter NELL, Walter Hübsch, Barbara ALBRECHT-KÜPPER, Jörg KELDENICH, Andreas KNORR
Abstract: Compounds of formula (I) described herein are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and are useful for the prevention and/or treatment of an allergic disease state or a disease of the respiratory tract characterized by airway obstruction.
Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
Type:
Application
Filed:
November 8, 2013
Publication date:
May 15, 2014
Applicant:
Jacobus Pharmaceutical Company, Inc.
Inventors:
Gavin David Heffernan, David Penman Jacobus, Kurt William Saionz, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R2 to R4, A, X and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.
Abstract: Compounds of the formula Ia and Ib, in which R1, R1?, R2, R3, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.
Abstract: The present application relates to novel substituted 4-amino-3,5-dicyano-2-thiopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.
Type:
Grant
Filed:
November 17, 2007
Date of Patent:
April 22, 2014
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Peter Nell, Nicole Diedrichs, Barbara Albrecht-Küpper, Alexandros Vakalopoulos, Frank Süβmeier, Joerg Keldenich
Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.
Abstract: Thienylpyri(mi)dinylazole of the formula (I) in which R1 to R8 and X1 have the meanings given in the description, and agrochemically active salts, to their use and to methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants and for reducing mycotoxins in plants and parts of the plants, to processes for preparing such compounds and compositions and treated seed and also to their use for controlling phytopathogenic harmful fungi in agriculture, horticulture, forestry, in animal husbandry, in the protection of materials, in the domestic and hygiene field and for the reduction of mycotoxins in plants and parts of the plants.
Type:
Grant
Filed:
December 21, 2010
Date of Patent:
April 1, 2014
Assignee:
Bayer CropScience AG
Inventors:
Alexander Sudau, Mazen Es-Sayed, Julia Neumann, Catherine Sirven, Jürgen Benting, Christoph Andreas Braun, Ruth Meissner, Anne-Sophie Rebstock, Samir Bennabi, Philippe Desbordes, Arounarith Tuch, Philippe Rinolfi, Stephane Brunet, Hiroyuki Hadano, Marie-Claire Grosjean-Cournoyer
Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.
Type:
Grant
Filed:
October 12, 2010
Date of Patent:
April 1, 2014
Assignee:
Bayer CropScience AG
Inventors:
Thomas Bretschneider, Martin Füβlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria Franken, Arnd Voerste
Abstract: Compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.
Type:
Application
Filed:
November 13, 2013
Publication date:
March 20, 2014
Applicant:
MANNKIND CORPORATION
Inventors:
John Bruce PATTERSON, David Gregory LONERGAN, Gary A. FLYNN, Qingping ZENG, Peter V. PALLAI
Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are as set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. The compounds of formula I are useful for treating a variety of disorders including autoimmune diseases such as rheumatoid arthritis, multiple sclerosis and psoriasis.
Type:
Grant
Filed:
April 18, 2007
Date of Patent:
March 18, 2014
Assignee:
Janssen Pharmaceutica, N.V.
Inventors:
Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJariais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
Abstract: Compounds of structural formula I 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:
Grant
Filed:
May 12, 2011
Date of Patent:
March 11, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Dong-Ming Shen, John S. Debenham, Thomas H. Graham, Matthew J. Clements, Yong Zhang
Abstract: The present invention relates to small molecule potentiators of metabotropic receptors, in particular of the mGlu2 receptor. The present invention also relates to the use of these compounds for the prevention or treatment of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The present invention thus provides compounds of formula I and variables defined herein.
Type:
Grant
Filed:
March 25, 2011
Date of Patent:
March 4, 2014
Assignee:
AbbVie Deutschland GmbH & Co. KG
Inventors:
Wilfried Braje, Katja Jantos, Hervé Geneste, Mario Mezler, Margaretha Henrica Maria Bakker, Jayne Froggett
Abstract: The present invention relates to novel ?4?2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them. The present invention relates to novel ?4?2 neuronal nicotinic acetylcholine receptor ligand compounds of the formula (I), and their derivatives, stereoisomers, pharmaceutically acceptable salts and compositions containing them.
Abstract: The present invention relates to substituted hydrazonamide compounds. The invention further relates to methods of inhibiting the activity of Hs?90 in a subject in need thereof and methods for treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a substituted hydrazonamide compound of the invention, or a pharmaceutical composition comprising such a compound.
Type:
Grant
Filed:
June 26, 2009
Date of Patent:
February 11, 2014
Assignee:
Synta Pharmaceuticals Corp.
Inventors:
Joseph Burlison, Dinesh U. Chimmanamada, Weiwen Ying, Shijie Zhang, David James
Abstract: The instant invention pertains to novel bi- or tricyclic sterically hindered alkoxyamines, their precursors, a process for their preparation and their use as light stabilizers for polymers or coatings, as flame retardants, as peroxide substitutes (rheology modifiers) or carbon radical scavengers.
Type:
Application
Filed:
October 4, 2013
Publication date:
February 6, 2014
Applicant:
BASF SE
Inventors:
Stefan Hauck, Walter Fischer, Kai-Uwe Schoening
Abstract: This invention relates to novel annellated 4-(indazolyl)-1,4-dihydropyridine 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:
Grant
Filed:
May 29, 2009
Date of Patent:
February 4, 2014
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Nicole Teusch, Karen Engel
Abstract: Compounds corresponding to formula I: which act as vanilloid receptor ligands, pharmaceutical compositions containing such compounds, a method for producing the compounds, and the use of such compounds to treat pain and various other conditions.
Type:
Grant
Filed:
July 25, 2012
Date of Patent:
February 4, 2014
Assignee:
Gruenenthal GmbH
Inventors:
Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Jeewoo Lee
Abstract: The present invention relates to compounds of general formula I, wherein the groups R1, R2 and m are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
Type:
Grant
Filed:
March 14, 2013
Date of Patent:
February 4, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Matthias Eckhardt, Sara Frattini, Dieter Hamprecht, Frank Himmelsbach, Elke Langkopf, Iain Lingard, Stefan Peters, Holger Wagner
Abstract: A method for producing starting materials or additives for cosmetics, pharmaceuticals and/or hydrocarbon-based fuels, especially for heating systems or internal combustion engines, takes organic residues or waste materials and decontaminates or sterilizes them with a hydrogenation process. In particular, the materials classified as K1, K2 or K3 according to EU Directive 1774/2002 are used for generating or producing the cited starting materials or additives, whereby an adequate decontamination of the residues or waste materials that are classified as being hazardous to health is ensured.
Abstract: The present invention provides a compound of formula (I): and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof. Also provided are pharmaceutical compositions containing these compounds and methods of treating a disease or condition mediated by CDK9 using these compounds and compositions.
Type:
Application
Filed:
November 17, 2011
Publication date:
December 5, 2013
Inventors:
William R. Antonios-McCrea, Paul A. Barsanti, Cheng Hu, Xianming Jin, Eric J. Martin, Yue Pan, Keith B. Pfister, Martin Sendzik, James Sutton, Lifeng Wan
Abstract: The present invention provides a compound of formula (II): where R1 is a substituted alkyl, heterocyclic, or cycloalkyl, group, and pharmaceutically acceptable salts, enantiomers, stereoisomers, rotamers, tautomers, diastereomers, or racemates thereof, and pharmaceutical compositions comprising these compounds. Also provided are methods of using these compounds to treat a disease or condition mediated by CDK9, such as cancers and other conditions described herein.
Type:
Application
Filed:
January 20, 2012
Publication date:
November 14, 2013
Applicant:
Novartis AG
Inventors:
William R. Antonios-McCrea, Paul A. Barsanti, Cheng Hu, Xianming Jin, Eric Martin, Yue Pan, Xiaodong Lin, Keith B. Pfister, Paul A. Renhowe, Martin Sendzik, James Sutton, Lifeng Wan
Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, Qa, Qb, QH, L and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
Type:
Grant
Filed:
April 19, 2011
Date of Patent:
November 5, 2013
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Harald Engelhardt, Christiane Kofink, Darryl McConnell
Abstract: Embodiments of the invention provide methods and materials for chemical cross-coupling reactions that utilize aryl alcohol derivatives as cross-coupling partners. Embodiments of the invention include methods for the amination of aryl sulfamates and carbamates, which are attractive cross-coupling partners, particularly for use in multistep synthesis. Illustrative embodiments include versatile means to use simple derivatives of phenol as precursors to polysubstituted aryl amines, as exemplified by a concise synthesis of the antibacterial drug linezolid.
Type:
Application
Filed:
January 6, 2012
Publication date:
October 31, 2013
Applicant:
The Regents of the University of California
Inventors:
Neil K. Garg, Stephen D. Ramgren, Amanda L. Silberstein, Kyle W. Quasdorf
Abstract: 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:
Application
Filed:
January 11, 2012
Publication date:
October 24, 2013
Applicant:
NOVARTIS AG
Inventors:
Konstanze Hurth, Rainer Martin Lueoend, Rainer Machauer, Ulf Neumann, Heinrich Rueeger, Michael Schaefer, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.
Type:
Application
Filed:
June 12, 2013
Publication date:
October 24, 2013
Inventors:
Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
Abstract: The invention provides inhibitors of focal adhesion kinase, an enzyme involved in the attachment of the cytoskeleton of a cell to an extracellular matrix, which has been implicated in processes such as cell migration, cell proliferation, and cell survival. The inhibitors are derivatives of a 5-substituted 2,4-diaminopyridine wherein the substituents are as defined herein. The invention also provides a method of using the inhibitors in treatment of cancer, and methods of preparation of the inhibitors by use of coupling reactions.
Type:
Application
Filed:
June 19, 2013
Publication date:
October 24, 2013
Applicant:
THE SCRIPPS RESEARCH INSTITUTE
Inventors:
Congxin Liang, Marcel Koenig, Yuanjun He, Par Holmberg
Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
Type:
Grant
Filed:
October 19, 2009
Date of Patent:
October 22, 2013
Assignees:
Merck Sharp & Dohme Corp, Metabasis Therapeutics, Inc.
Inventors:
Qun Dang, De Michael Chung, Tony S. Gibson, Hongjian Jiang, Daniel K. Cashion, Jianming Bao, Ping Lan, Huagang Lu, Gergely M. Makara, F. Anthony Romero, Iyassu Sebhat, Dariusz Wodka
Abstract: The present invention relates to a compound of formula (I): or hydrates, solvates, prodrugs, or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Y, ring A, R3 and R4 are as defined in the detailed description and claims. The compound of formula (I) are receptor tyrosine kinase (RTK) inhibitors and have efficacy for the treatment, prevention, or amelioration of RTK-related diseases.
Abstract: 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:
Application
Filed:
March 14, 2013
Publication date:
October 17, 2013
Applicant:
Axikin Pharmaceuticals, Inc.
Inventors:
Erik Dean RAAUM, Garrett Thomas Potter, Tai Wei Ly
Abstract: The invention, relates to compounds of formula I (or pharmaceutically acceptable salts thereof) as defined herein, pharmaceutical compositions thereof, and their use in manufactures and methods for modulating biological processes including inhibition of kinase activity such as P1-3 kinase.
Type:
Grant
Filed:
January 23, 2009
Date of Patent:
October 15, 2013
Assignee:
Signal Rx Pharmaceuticals, Inc.
Inventors:
Guillermo A. Morales, Kevin T. Weber, Jessica M. Newblom, Xiaodong Peng, Jingdong Su, Joseph R. Garlich
Abstract: Compounds of general formula I, (formula [I)], their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.
Type:
Application
Filed:
November 21, 2011
Publication date:
October 10, 2013
Applicant:
LEO PHARMA A/S
Inventors:
Kristoffer Månsson, Lars Kristian Albert Blæhr
Abstract: The present application relates to novel 6-alkylamino-substituted dicyanopyridines, to their amino acid ester prodrugs, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders.
Type:
Application
Filed:
March 13, 2013
Publication date:
October 10, 2013
Applicant:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Alexandros VAKALOPOULOS, Daniel MEIBOM, Barbara ALBRECHT-KÜPPER, Katja ZIMMERMANN, Jörg KELDENICH, Hans-Georg LERCHEN, Peter NELL, Frank SÜßMEIER, Ursula KRENZ
Abstract: This invention relates to novel 4-(indazolyl)-1,4-dihydropyridine of 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:
Grant
Filed:
May 29, 2009
Date of Patent:
October 8, 2013
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Nicole Teusch, Karen Engel
Abstract: A compound having Formula (I) or Formula (II) is disclosed as an P2X7 antagonist, wherein A, B, C, Y, Y, Z, m, v, R1, R2, R3, R4, and R5, are as defined in the description. Methods and compositions for treating disease or condition modulated by P2X7 are also disclosed.
Type:
Grant
Filed:
July 9, 2012
Date of Patent:
October 1, 2013
Assignee:
Abbvie Inc.
Inventors:
William A. Carroll, Arturo Perez-Medrano, Alan S. Florjancic, Derek W. Nelson, Sridhar Peddi, Tongmei Li, Eric M. Bunnelle, Gavin Hirst, Biquin C. Li
Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1).
Type:
Application
Filed:
October 24, 2011
Publication date:
September 12, 2013
Inventors:
Sobhana Babu Boga, Joseph M. Kelly, Hugh Y. Zhu, Abdul-Basit Alhassan, Xin Yao, Xiaolei Gao, James J-S Wang, Jagdish A. Desai, Subrahmanyam Gudipati, Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Yongqi Deng, Gerald W. Shipps, JR.
Abstract: The invention provides a combination comprising an Hsp90 inhibitor compound of the formula (VII): or tautomer or salt thereof and one or more therapeutic agents selected from topoisomerase I inhibitors; antimetabolites; tubulin targeting agents; DNA binder and topoisomerase II inhibitors; alkylating agents; monoclonal antibodies; anti-hormones; signal transduction inhibitors; proteasome inhibitors; DNA methyl transferases; cytokines; retinoids and HDAC or HAT modulators.
Type:
Grant
Filed:
October 12, 2011
Date of Patent:
September 10, 2013
Assignee:
Astex Therapeutics Ltd.
Inventors:
Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford, Maria Grazia Carr, Robert Downham, Michael Alistair O'Brien, Theresa Rachel Phillips, Andrew James Woodhead
Abstract: This invention relates to a method of preparing a benzoimidazole derivative at high purity and high yield so as to enable the production of the benzoimidazole derivative compound as an antagonist against a vanilloid reactor-1, and particularly to a method of preparing a benzoimidazole derivative at high purity and high yield, wherein the benzoimidazole derivative is synthesized using a novel intermediate, namely, benzaldehyde, and thereby the preparation process is simple so that it can be applied to production.
Type:
Application
Filed:
September 27, 2011
Publication date:
September 5, 2013
Applicant:
DAEWOONG PHARMACEUTICAL CO., LTD.
Inventors:
In Woo Kim, Ji Duck Kim, Hong Chul Yoon, Hee Kyoon Yoon, Byung Goo Lee, Joon Hwan Lee, Young Mook Lim, Soo Jin Choi