At Least Three Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/236)
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Publication number: 20130343992Abstract: Compounds of formula (I) are disclosed Compounds of formula (I) are useful in treating conditions and disorders prevented by or ameliorated by PDE10A ligands. Radiolabeled compounds of formula (I) are also useful as diagnostic tools as PDE10A positron emission tomography ligands. Also disclosed are pharmaceutical compositions comprising compound of formula (I), methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).Type: ApplicationFiled: December 21, 2012Publication date: December 26, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
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Publication number: 20130345424Abstract: Hydrazinopyridazines, fused hydrazinopyridazines, phenylethylhydrazines, or combinations thereof, compositions comprising hydrazinopyridazines, fused hydrazinopyridazines, phenylethylhydrazines, or combinations thereof, and methods for using them for the treatment of pain are described.Type: ApplicationFiled: March 2, 2012Publication date: December 26, 2013Applicant: PURDUE RESEARCH FOUNDATIONInventor: Riyi Shi
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Publication number: 20130338133Abstract: The present invention relates to substituted imidazopyridazine compounds of general formula (I), which are Mps-1 (Monopolar Spindle 1) Kinase inhibitors (also known as Tyrosine Threonine Kinase, TTK) in which R3, R5, and A are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: September 6, 2011Publication date: December 19, 2013Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventors: Ulrich Klar, Marcus Koppitz, Rolf Jautelat, Dirk Kosemund, Rolf Bohlmann, Philip Lienau, Gerhard Siemeister, Antje Margret Wengner
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Publication number: 20130331349Abstract: The present invention relates to compounds of Formula (I), a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesiod X receptors (FXR).Type: ApplicationFiled: November 30, 2011Publication date: December 12, 2013Inventors: David C. Tully, Paul Vincent Rucker, Phillip B. Alper, Daniel Mutnick, Donatella Chianelli
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Publication number: 20130331384Abstract: The disclosure provides for novel antimicrobial agents, methods of making, and methods of use thereof.Type: ApplicationFiled: February 14, 2012Publication date: December 12, 2013Applicant: The Regents of the University of CaliforniaInventors: Richard L. Gallo, Teruaki Nakatsuji
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Publication number: 20130324526Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).Type: ApplicationFiled: February 8, 2012Publication date: December 5, 2013Applicant: NOVARTIS AGInventors: Feng He, Haibing Deng, Xingnian Fu, Haibing Guo, Yuan Mi, Xiaoxia Yan, Hongping Yu, Ji Yue (Jeff) Zhang
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Patent number: 8598177Abstract: The invention relates to novel compounds of formula I where R1, R2, R3, R4, R5, R6, R7, R8, R9, Q1, Q2 and Q3 are each as defined below. The compounds of formula I have antithrombotic activity and inhibit especially protease-activated receptor 1 (PAR1). The invention further relates to a process for preparing the compound of formula I and to the use thereof as a medicament.Type: GrantFiled: August 5, 2010Date of Patent: December 3, 2013Assignee: SanofiInventors: Uwe Heinelt, Volkmar Wehner, Matthias Herrmann, Karl Schoenafinger, Henning Steinhagen
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Patent number: 8592425Abstract: The invention encompasses imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: January 12, 2010Date of Patent: November 26, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Michael D. Altman, Mark T. Bilodeau, Jongwon Lim, Alan Northrup, Matthew G. Stanton, Brandon M. Taoka
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Publication number: 20130309200Abstract: New imidazo[1,2-b]pyridazine and imidazo[4,5-b]pyridine derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).Type: ApplicationFiled: November 24, 2011Publication date: November 21, 2013Applicant: ALMIRALL, S.A.Inventors: Jacob Gonzalez Rodriguez, Bernat Vidal Juan, Laura Vidal Gispert, Jordi Bach Taña
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Publication number: 20130303529Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: June 13, 2013Publication date: November 14, 2013Inventors: Brian K. ALBRECHT, David Bauer, Steven Bellon, Christiane M. Bode, Shon Booker, Alessandro Boezio, Deborah Choquette, Derin D'Amico, Jean-Christophe Harmange, Satoko Hirai, Randall W. Hungate, Tae-Seong Kim, Richard T. Lewis, Longbin Liu, Julia W. Lohman, Mark H. Norman, Michele Potashman, Aaron C. Siegmund, Stephanie K. Springer, Markian Stec, Ning Xi, Kevin Yang, Karina Romero, Katrina Woodin Copeland, Emily A. Peterson
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Publication number: 20130296557Abstract: The present invention relates to novel diarylacetylene hydrazide compounds of formula (I) or pharmaceutically acceptable salt thereof, as tyrosine kinase inhibitors, the process for their preparation, and to the use of the compounds of formula (I) in the preparation of pharmaceutical compositions for the therapeutic treatment of disorders related to tyrosine kinases, in warm-blooded animalsType: ApplicationFiled: January 23, 2012Publication date: November 7, 2013Applicant: SUN PHARMA ADVANCED RESEARCH COMPANY LTD.Inventors: Prabal Sengupta, Hemant Ashvinbhai Chokshi, Chetan Surjitsingh Puri, Sabbirhusen Yusufbhai Chimanwala, Varun Anilkumar Mehta, Dipali Manubhai Desai, Trinadha Rao Chitturi, Rajamannar Thennati
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Publication number: 20130296298Abstract: The present invention provides novel LRRK2 kinase inhibitors and methods of treating disease states using these inhibitors.Type: ApplicationFiled: May 2, 2013Publication date: November 7, 2013Applicants: THE UAB RESEARCH FOUNDATION, Southern Research InstituteInventors: Robert A. Galemmo, JR., Andrew B. West, Joseph A. Maddry, Subramaniam Ananthan, Ashish Kumar Pathak, Jacob Valiyaveettil
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Patent number: 8575337Abstract: The present invention provides a novel antimicrobial drug comprising an oxazolidinone derivative of the formula (I): or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: June 23, 2009Date of Patent: November 5, 2013Assignee: Research Foundation Itsuu LaboratoryInventors: Issei Katoh, Toshiaki Aoki, Hideyuki Suzuki, Iwao Utsunomiya, Norikazu Kuroda, Tsutomu Iwaki
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Publication number: 20130289013Abstract: Imidazo[1,2-a]pyridines are disclosed. Compounds of the invention are useful therapeutic agents and their inclusion in pharmaceutical formulations and use in methods of treatment are disclosed.Type: ApplicationFiled: June 24, 2013Publication date: October 31, 2013Inventors: Qun Kevin FANG, Frank Xinhe Wu, Paul T. Grover, Seth C. Hopkins, Una Campbell, Milan Chytil, Kerry L. Spear
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Publication number: 20130289037Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.Type: ApplicationFiled: March 14, 2013Publication date: October 31, 2013Inventor: MILLENNIUM PHARMACEUTICALS, INC
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Publication number: 20130273037Abstract: Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.Type: ApplicationFiled: April 17, 2013Publication date: October 17, 2013Inventors: Dustin Siegel, David Sperandio, Hai Yang, Michael Sangi, Jay P. Parrish, Hon Chung Hui
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Publication number: 20130267521Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: March 15, 2013Publication date: October 10, 2013Applicants: Intellikine LLC, Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. CASTRO, Katrina CHAN, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Liansheng LI, Tao LIU, Yi LIU, Pingda REN, Daniel A. SNYDER, Martin R. TREMBLAY
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Patent number: 8546393Abstract: The disclosure relates to compounds of formula (I): wherein , A, W, X, and Ra are as defined in the disclosure, and salts thereof, and to pharmaceutical compositions comprising said compounds, to processes for preparing them, and to their use as medicaments, in particular as MET inhibitors.Type: GrantFiled: January 26, 2010Date of Patent: October 1, 2013Assignee: SanofiInventors: Eva Albert, Eric Bacque, Conception Nemecek, Antonio Ugolini, Sylvie Wentzler
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Patent number: 8546395Abstract: The invention relates to 6-cycloamino-3-(1H-pyrrolo[2,3-b]pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives corresponding to the general formula (I) in which R2 represents an aryl group optionally substituted with one or more halogen atoms or C1-6-alkyl, C1-6-alkyloxy, C1-6-alkylthio, C1-6-fluoroalkyl, C1-6-fluoroalkyloxy and —CN groups or R2 represents a group chosen from C1-6-alkyl, C1-6-fluoroalkyl, C3-7-cycloalkyl or C3-7-cycloalkyl-C1-6-alkyl groups; A represents a C1-7-alkylene group; B represents a C1-7-alkylene group; L represents either a nitrogen atom optionally substituted with an Rc or Rd group, or a carbon atom substituted with an Re1 group and an Rd group or two Re2 groups; the carbon atoms of A and of B being optionally substituted with one or more Rf groups, which may be identical to or different from one another. Preparation process and therapeutic use.Type: GrantFiled: November 30, 2009Date of Patent: October 1, 2013Assignee: SanofiInventors: Christophe Pacaud, Frederic Puech
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Publication number: 20130252936Abstract: Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein.Type: ApplicationFiled: March 8, 2013Publication date: September 26, 2013Applicant: Usher III InitiativeInventors: Roland Werner BÜRLI, William Rameshchandra Krishna Esmieu, Christopher James Lock, Karine Fabienne Malagu, Andrew Pate Owens, William E. Harte
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Publication number: 20130245022Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: May 3, 2013Publication date: September 19, 2013Applicant: Janssen Pharmaceutica NVInventors: J. GUY BREITENBUCHER, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Sierestad
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Publication number: 20130245021Abstract: Imidazo[1,2-b]pyridazine-based compounds of the formula: are disclosed, wherein R1, R2 and R3 are defined herein. Compositions comprising the compounds and methods of their use to treat, manage and/or prevent diseases and disorders mediated by mediated by adaptor associated kinase 1 activity are also disclosed.Type: ApplicationFiled: March 5, 2013Publication date: September 19, 2013Inventors: Yingzhi BI, Kenneth Gordon CARSON, Giovanni CIANCHETTA, Michael Alan GREEN, Godwin KUMI, Zhi LIANG, Ying Jade LIU, Alan MAIN, Yulian ZHANG, Gregory Glenn ZIPP
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Patent number: 8530387Abstract: The present invention relates to new dithiinopyridazinedione derivatives, to processes for preparing them, to their use for controlling unwanted microorganisms, more particularly phytopathogenic fungi, in crop protection, in the household and hygiene sector and in the protection of materials, and also to crop protection compositions comprising these dithiinopyridazinedione derivatives.Type: GrantFiled: April 14, 2011Date of Patent: September 10, 2013Assignee: Bayer CropScience AGInventors: Thomas Seitz, Ulrike Wachendorff-Neumann, Jürgen Benting
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Patent number: 8530650Abstract: The present invention relates to pyridopyrimidine derivatives according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: GrantFiled: November 3, 2009Date of Patent: September 10, 2013Assignee: MERCK PATENT GmbHInventors: Kai Schiemann, Melanie Schultz, Wolfgang Staehle, Ingo Kober, Dirk Wienke, Mireille Krier
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Publication number: 20130231337Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 13, 2013Publication date: September 5, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventors: Dong Zou, Wei-Sheng Huang, R. Mathew Thomas, Jan Antoinette C. Romero, Jiwei Qi, Yihan Wang, Xiaotian Zhu, William C. Shakespeare, Rajeswari Sundaramoorthi, Chester A. Metcalf, III, David C. Dalgarno, Tomi K. Sawyer
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Patent number: 8524900Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: December 1, 2011Date of Patent: September 3, 2013Assignee: Amgen Inc.Inventors: Brian K. Albrecht, David Bauer, Christiane M. Bode, Shon Booker, Alessandro Boezio, Deborah Choquette, Derin D'Amico, Jean-Christophe Harmange, Satoko Hirai, Richard T. Lewis, Longbin Liu, Julia Lohman, Mark H. Norman, Michele Potashman, Aaron C. Siegmund, Stephanie K. Springer, Markian Stec, Ning Xi, Kevin Yang
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Publication number: 20130225592Abstract: The present invention relates to novel compounds and pharmaceutical compositions thereof, and methods for promoting healthy aging of skin, the treatment of skin disorders, the treatment of cardiovascular disorders, the treatment of renal disorders, the treatment of angiogenesis disorders, such as cancer, treatment of tissue damage, such as non-cardiac tissue damage, the treatment of evolving myocardial infarction, and the treatment of various other disorders, such as complications arising from diabetes with the compounds and compositions of the invention. Other disorders can include, but are not limited to, atherosclerosis, coronary artery disease, diabetic nephropathy, diabetic neuropathy, diabetic retinopathy, infections of the skin, peripheral vascular disease, stroke, and the like.Type: ApplicationFiled: January 16, 2013Publication date: August 29, 2013Inventors: Andrew WASMUTH, Donald W. LANDRY, Shi Xian DENG, Ravichandran RAMASAMY, Ann Marie SCHMIDT, Banavara L. MYLARI
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Publication number: 20130224114Abstract: The present invention relates to compounds and methods for imaging translocator protein (18 kDa) (TSPO) expression in a subject. This invention also relates to compounds and methods for the treatment of neurodegenerative disorders, inflammation or anxiety in a subject.Type: ApplicationFiled: March 25, 2013Publication date: August 29, 2013Applicant: The University of SydneyInventor: The University of Sydney
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Publication number: 20130225590Abstract: This invention relates to novel substituted triazolo-pyridazines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an ?1-GABA-A receptor antagonist and/or a ?2, ?3 and ?5 GABA-A receptor agonist.Type: ApplicationFiled: March 18, 2013Publication date: August 29, 2013Applicant: CONCERT PHARMACEUTICALS, INC.Inventor: Concert Pharmaceuticals, Inc.
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Patent number: 8518943Abstract: The present invention concerns 2-oxo-1-pyrrolidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: April 6, 2012Date of Patent: August 27, 2013Assignee: UCB Pharma, S.A.Inventors: Benoit Kenda, Yannick Quesnel, Ali Ates, Philippe Michel, Laurent Turet, Joel Mercier
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Publication number: 20130217662Abstract: Methods for treating a disease or disorder selected from pain, cancer, inflammation, neurodegenerative disease, Typanosoma cruzi infection and osteolytic disease in a mammal, which comprise administering to said mammal a therapeutically effective amount of a compound of Formula I in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification.Type: ApplicationFiled: September 13, 2012Publication date: August 22, 2013Inventors: Steven W. Andrews, Julia Haas, Yutong Jiang, Gan Zhang
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Publication number: 20130217693Abstract: The invention relates to a compound of Formulae I and/or II: and/or a pharmaceutically-acceptable salt, hydrate, solvate, tautomer, optical isomer, E-isomer, Z-isomer, or combination thereof; X is selected from Se, N—OH, NH, NO2, CN, N—CN, N?O, O or S, and the remaining substituents are described herein; and a composition thereof. The invention also relates to a method of administration thereof; and use thereof to treat HIV.Type: ApplicationFiled: April 1, 2011Publication date: August 22, 2013Inventors: Wayne Danter, Clinton Threlfall, Sylvain Guizzetti, Julien Marin
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Publication number: 20130210825Abstract: The invention relates to imidazo[1,2-b]pyridazines of general formula (I) a process for their manufacuture and their use for the treatment of benign and malignant neoplasia.Type: ApplicationFiled: July 27, 2011Publication date: August 15, 2013Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventors: Hartmut Rehwinkel, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer
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Patent number: 8507488Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Ros, KDR, FMS, C-FMS, FLT3, c-Kit, JAK2, JAK3, Aurora, PDGFR, Lck, TrkA, TrkB, TrkC, IGF-IR, ALK4, ALK5 and ALK or combinations thereof.Type: GrantFiled: May 7, 2009Date of Patent: August 13, 2013Assignee: IRM LLCInventors: Pamela A. Albaugh, Ha-Soon Choi, Gregory Chopiuk, Yi Fan, Paul Vincent Rucker, Zhicheng Wang
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Patent number: 8507489Abstract: The present disclosure provides bicyclic triazole protein kinase modulators and methods of using these compounds to treat diseases mediated by kinase activity.Type: GrantFiled: October 18, 2007Date of Patent: August 13, 2013Assignee: SGX Pharmaceuticals, Inc.Inventors: Pierre-Yves Bounaud, Christopher Ronald Smith, Elizabeth Anne Jefferson
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Patent number: 8507469Abstract: The present invention relates to compounds of formula (I) wherein A is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-halo-alkenyl, C3-C6-cycloalkyl, aryl-C1-C4-alkyl, aryl-C2-C4-alkenyl, aryl or hetaryl; is a single or double bond; X1 and X2 are N, CRx1, NRx2 or CRx3Rx4; Rx1, Rx3 and Rx4 are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, etc. or two geminal radicals Rx3 and Rx4 together with the carbon atom to which they are bound may form a carbonyl group or a 3- to 6-membered carbocyclic or heterocyclic spiro-annulated ring; Rx2 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; or two vicinal radicals Rx1, Rx2, Rx3 or Rx4 together with X1 and X2 form a five- or six-membered carbocyclic or heterocyclic fused ring; Y1, Y2 and Y3 are N or CRy; Ry is H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.Type: GrantFiled: March 20, 2008Date of Patent: August 13, 2013Assignee: Abbott GmbH & Co. KGInventors: Thomas Schultz, Wilfried Braje, Sean Colm Turner, Andreas Haupt, Udo Lange, Karla Drescher, Karsten Wicke, Liliane Unger, Mario Mezler, Matthias Mayrer
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Publication number: 20130203714Abstract: The invention concerns bicyclic compounds of Formula I wherein R1, R2, L1, L2, J, Y, k, n, p and r are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen-receptor associated conditions, particularly prostate cancer.Type: ApplicationFiled: August 1, 2012Publication date: August 8, 2013Applicant: ASTRAZENECA R&DInventors: Robert Hugh Bradbury, Gregory Richard Carr, Alfred Arthur Rabow, Srinivasa Rao Korupoju, Harikrishna Tumma
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Patent number: 8501738Abstract: This invention relates to novel substituted triazolo-pyridazines and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an ?1-GABAA receptor antagonist or an ?2- and/or an ?3-GABAA receptor partial agonist.Type: GrantFiled: June 22, 2010Date of Patent: August 6, 2013Assignee: Concert Pharmaceuticals, Inc.Inventors: Scott L. Harbeson, Julie F. Liu
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Publication number: 20130196979Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 13, 2013Publication date: August 1, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: ARIAD Pharmaceuticals, Inc.
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Patent number: 8497266Abstract: Compounds of the formula (I), in which R1, R2, R3, R3?, R4 have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: May 25, 2009Date of Patent: July 30, 2013Assignee: Merck Patent GmbHInventors: Dieter Dorsch, Oliver Schadt, Frank Stieber, Andree Blaukat
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Patent number: 8497368Abstract: The invention relates to compounds of formula (I) and salts thereof: wherein the substituents are as defined in the specification; a compound of formula (I) for use in the treatment of the human or animal body, in particular with regard to c-Met tyrosine kinase mediated diseases or conditions; the use of a compound of formula (I) for manufacturing a medicament for the treatment of such diseases; pharmaceutical compositions comprising a compound of the formula (I), optionally in the presence of a combination partner, and processes for the preparation of a compound of formula (I).Type: GrantFiled: August 10, 2010Date of Patent: July 30, 2013Assignee: Novartis AGInventors: Feng He, Miao Dai, Xingnian Fu, Yue Li, Lei Liu, Yuan Mi, Yao-chang Xu, Guoliang Xun, Zhengtian Yu, Ji Yue Zhang
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Patent number: 8497269Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A4, L, R1, R2, R3, R5 and m are as defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of p38 map kinase mediated diseases including rheumatoid arthritis, psoriasis, chronic obstructive pulmonary disease, ankylosing spondylitis, pain and other inflammatory disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: GrantFiled: October 7, 2009Date of Patent: July 30, 2013Assignee: Amgen Inc.Inventors: Andrew Tasker, James R. Falsey, Robert M. Rzasa, Bradley J. Herberich, Dawei Zhang
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Publication number: 20130190314Abstract: The invention relates to derivatives of 6-cycloamino-2-thienyl-3-(pyridin-4-yl)imidazo[1,2-b]-pyridazine and 6-cycloamino-2-furanyl-3-(pyridin-4-yl)imidazo[1,2-b]-pyridazine with general formula (I). The invention also relates to a method for the preparation and therapeutic application thereof, in the treatment or prevention of illnesses involving casein kinase 1 epsilon and/or casein kinase 1 delta.Type: ApplicationFiled: December 17, 2009Publication date: July 25, 2013Inventors: Yulin Chiang, Cecile Enguehard-Gueiffier, Pascal George, Alaim Gueiffier, Frederic Puech, Mireille Sevrin, Qiuxia Zhao
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Publication number: 20130190172Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: October 5, 2011Publication date: July 25, 2013Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: George Philip Lahm, Thomas Francis Pahutski, JR.
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Publication number: 20130184240Abstract: Disclosed is a compound which is useful as an AMPK activator. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein a group represented by the formula: is a group represented by the formula: R1 is each independently halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like; m is an integer of 0 to 3; R2 is hydrogen, or substituted or unsubstituted alkyl; X is —O—; and Y is substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl.Type: ApplicationFiled: September 8, 2011Publication date: July 18, 2013Applicant: Shionogi & Co., Ltd.Inventors: Keisuke Tonogaki, Akira Ino, Eiichi Kojima, Manabu Katou, Masafumi Iwatsu, Nobuyuki Tanaka, Masahiko Fujioka
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Patent number: 8486945Abstract: The invention relates to novel heterocyclic compounds and to the use thereof, to pharmaceutical compositions containing said chemical compounds as an active ingredient and to the use thereof for producing medicinal preparations for the human being and warm-blood animals for treating diseases caused by the aberrant activity of an Hedgehog (Hh)-signal system, in particular oncological diseases. The invention also relates to the use of the above-mentioned compounds in the form of ‘molecular pharmacological tools’ for examining (in vitro and in vivo) the biochemical features of the Hh-signal system, in particular, the interaction of Hh protein and transmembrane proteins, namely, suppressor Patched (Ptc) and protooncogenic proteins.Type: GrantFiled: December 12, 2008Date of Patent: July 16, 2013Inventors: Andrey Ivashchenko, Yan Lavrovsky, Sergey Malyarchuk, Ilya Okun, Nikolay Savchuk, Sergey Tkachenko, Alexander Khvat, Alexander Ivashchenko
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Publication number: 20130178460Abstract: The present invention relates to the use of novel compounds of Formula I: wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.Type: ApplicationFiled: January 10, 2013Publication date: July 11, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130178622Abstract: The invention features methods, kits, and pharmaceutical compositions for treating cancer using 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)-methyl)-3-(trifluoromethyl)phenyl)benzamide.Type: ApplicationFiled: March 13, 2013Publication date: July 11, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: ARIAD Pharmaceuticals, Inc.
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Patent number: 8481538Abstract: The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders.Type: GrantFiled: September 18, 2007Date of Patent: July 9, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alexander Aronov, Jon Come, John Court, David Deininger, David Lauffer, Pan Li, Kira McGinty, Suganthini Nanthakumar, Dean Stamos, Kirk Tanner
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Publication number: 20130171102Abstract: The invention is related to anti-viral compounds of formula (A) as defined in the claims, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: May 20, 2011Publication date: July 4, 2013Applicant: Gilead Sciences, Inc.Inventors: Kyla Bjornson, Steven S. Bondy, You-chul Choi, Chien-Hung Chou, Ruchika Mishra, James D. Trenkle, Winston C. Tse, Randall W. Vivian, James G. Taylor