The Nitrogens Are In The 1,4-positions Of The Hetero Ring Patents (Class 540/575)
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Publication number: 20140005168Abstract: 5-Azaindazole compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, 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: June 26, 2013Publication date: January 2, 2014Inventors: Steven Do, Huiyong Hu, Aleksandr Kolesnikov, Vickie H. Tsui, Xiaojing Wang
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Patent number: 8618283Abstract: The invention provides compounds of general formulae (I)-(IV) or pharmaceutically acceptable salts thereof: The invention also provides methods of preparing the compounds, pharmaceutical compositions comprising the compounds and use of the compounds for the preparation of medicaments intended to modulate the activity of one or more members of the G-protein coupled receptor (GPCR) class. Compounds of the invention may be used to create a compound library for use in screening for agents which modulate signalling through GPCRs.Type: GrantFiled: November 4, 2011Date of Patent: December 31, 2013Assignee: Cambridge Enterprise LimitedInventors: David J Grainger, David John Fox
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Publication number: 20130345197Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: June 3, 2013Publication date: December 26, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Luc Farmer, Randy Bethiel, Edmund Harrington, Jeremy Green, John Court, Jon Come, David Lauffer, Alex Aronov, Hayley Binch, Dean Boyall, Jean-Damien Charrier, Simon Everitt, Damien Fraysse, Michael Mortimore, Francoise Pierard, Daniel Robinson, Jian Wang, Joanne Pinder, Tiansheng Wang, Albert Pierce
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Publication number: 20130345195Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n 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: ApplicationFiled: August 23, 2013Publication date: December 26, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, Michael J. BURKE, Thomas Martin KIRRANE, Matthew Russell NETHERTON, Anil Kumar PADYANA, Lana Louise SMITH KEENAN, Hidenori TAKAHASHI, Michael Robert TURNER, QIANG ZHANG, Qing ZHANG
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Publication number: 20130345200Abstract: Herein are disclosed indoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: August 7, 2013Publication date: December 26, 2013Applicant: GlaxoSmithKline LLCInventors: James Brackley, III, Joelle Lorraine Burgess, Seth Grant, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma
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Publication number: 20130338139Abstract: Described herein are compounds of Formula I and Formula II, methods of their synthesis, compositions comprising the compounds, and use of the compounds and compositions in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.Type: ApplicationFiled: June 18, 2013Publication date: December 19, 2013Inventors: Amy Allan, Bryan Branstetter, James Breitenbucher, Brian Dyck, Tawfik Gharbaoui, Laurent Gomez, Andrew Richard Hudson, Tami Jo Marrone, Troy Vickers, Michael I. Weinhouse
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Publication number: 20130336920Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y, A, R1 and R2 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: ApplicationFiled: January 4, 2013Publication date: December 19, 2013Applicant: ARDELYX, INC.Inventor: Ardelyx, Inc.
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Publication number: 20130338066Abstract: The invention relates to the compounds of formula (I) and to the physiologically acceptable salts thereof. Said compounds are suitable e.g. for the treatment of hyperglycemia.Type: ApplicationFiled: March 7, 2012Publication date: December 19, 2013Applicant: SANOFIInventors: Thomas Boehme, Christian Engel, Stefan Guessregen, Torsten Haack, Kurt Ritter, Georg Tschank
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Publication number: 20130331379Abstract: The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof.Type: ApplicationFiled: February 27, 2012Publication date: December 12, 2013Inventors: Carl A. Baxter, Edward Cleator, Faye Sheen, Shane W. Krska, Gavin Stewart, Neil Strotman, Debra J. Wallace, Timothy Wright
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Publication number: 20130324516Abstract: The invention provides novel compounds having the general formula: wherein A, R1, R2 and R3 are as defined herein, compositions including the compounds and methods of using the compounds.Type: ApplicationFiled: May 31, 2013Publication date: December 5, 2013Inventors: Huifen Chen, Terry Crawford, Seth F. Harris, Steven R. Magnuson, Chudi Ndubaku, Lan Wang
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Publication number: 20130324517Abstract: The present invention relates to novel antagonists for CCR2 (CC chemokine receptor 2) and their use for providing medicaments for treating conditions and diseases, especially pulmonary diseases like asthma and COPD.Type: ApplicationFiled: July 24, 2013Publication date: December 5, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Heiner EBEL, Sara FRATTINI, Riccardo GIOVANNINI, Christoph HOENKE, Thomas TRIESELMANN, Patrick TIELMANN, Stefan SCHEUERER, Silke HOBBIE, Frank BUETTNER
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Patent number: 8598179Abstract: The present invention relates to compounds of the formula I, wherein R1; R2; Z; A; B; D; Q; J; V; G and M have the meanings indicated in the claims. The compounds of the formula I are valuable pharmacologically active compounds. They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable, e.g., for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: GrantFiled: June 17, 2010Date of Patent: December 3, 2013Assignee: SanofiInventors: Marc Nazaré, Gernot Zech, Jochen Goerlitzer, Melitta Just, Tilo Weiss, Gerhard Hessler, Werngard Czechtizky, Sven Ruf
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Patent number: 8598159Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and modulating GABAA, and use of the compound of formula I for the treatment of GABAA receptor associated disorders. The general structure of formula I is shown below and can exist in tautomeric forms: The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: GrantFiled: November 18, 2010Date of Patent: December 3, 2013Assignee: Dart Neuroscience (Cayman) Ltd.Inventors: Alan P. Kaplan, Varsha Gupta, Jan W. F. Wasley
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Patent number: 8598157Abstract: 5-alkynyl-pyridine of general formula (I) their use as inhibitors of the activity of PI3Kalpha, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R6 and n have the meanings given in the claims and in the specification.Type: GrantFiled: January 24, 2012Date of Patent: December 3, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Tobias Wunberg, Oliver Kraemer, Lars van der Veer
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Publication number: 20130310348Abstract: This disclosure provides a new class of compounds referred to as “reversed chloroquines” (RCQs), which are highly effective against CQR and CQS malaria parasites. RCQs are hybrid molecules, which include an antimalarial quinoline analog (such as chloroquine) moiety and a CQR reversal moiety. Exemplary RCQ chemical structures are provided. Also provided are pharmaceutical compositions including the disclosed RCQ compounds, and methods of using such compounds and compositions for the treatment of malaria and inhibition of CQR or CQS Plasmodium sp. (such as P. falciparum).Type: ApplicationFiled: July 25, 2013Publication date: November 21, 2013Applicants: State UniversityInventors: David H. Peyton, Steven Burgess
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Patent number: 8586576Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.Type: GrantFiled: February 23, 2007Date of Patent: November 19, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Marc Labroli, Kartik M. Keertikar
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Publication number: 20130302416Abstract: New substituted tricyclic compounds of formula (I) are described, wherein R1, R2, X, Y, Z are herein defined, having protein kinase inhibiting activity. The invention includes methods to prepare the compounds of formula (I), pharmaceutical compositions containing them, and their use in therapy, in particular for the treatment of diseases caused by and/or associated with dysregulated activity of protein kinase.Type: ApplicationFiled: January 19, 2012Publication date: November 14, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Marina Caldarelli, Francesco Casuscelli, Daniele Donati, Danilo Mirizzi, Francesca Quartieri, Marco Silvagni
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Patent number: 8580782Abstract: In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or compositions.Type: GrantFiled: April 20, 2007Date of Patent: November 12, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Timothy J. Guzi, Kamil Paruch, Michael P. Dwyer, Marc A. Labroli, Kartik M. Keertikar
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Publication number: 20130296307Abstract: Provided herein are compounds according to Formula I and pharmaceutically acceptable salts thereof, and compositions comprising the same, for use in various methods, including treating cancers such as colon, ovarian, pancreatic, breast, liver, prostate and hematologic cancers:Type: ApplicationFiled: July 10, 2013Publication date: November 7, 2013Inventors: John Hood, Sunil Kumar KC, David Mark Wallace
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Publication number: 20130289020Abstract: Disclosed are compounds that are antagonists of the CXCR4 receptor.Type: ApplicationFiled: October 13, 2011Publication date: October 31, 2013Applicant: Proximagen LimitedInventors: Edward Daniel Savory, Allson Stewart, Allison Cartey, Giles Brown, Iain Simpson, Kathryn Oliver, Lee Patient, Michael Higginbottom, Andrew Graham Cole
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Publication number: 20130281430Abstract: The invention relates to new amino-indole-substituted imidazolyl-pyrimidines of formula 1 wherein R1, R2, R3, R4 and R5 are defined as in claim 1 and pharmaceutically acceptable salts thereof and the use of these compounds for the preparation of a medicament for treating a disease selected from asthma, COPD, rheumatoid arthritis, specific lymphomas and specific diseases of the nervous system.Type: ApplicationFiled: April 17, 2013Publication date: October 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Georg DAHMANN, Horst DOLLINGER, Christian GNAMM, Dennis FIEGEN, Matthias HOFFMANN, Jasna KLICIC, David James LAMB, Andreas SCHNAPP
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Publication number: 20130281429Abstract: The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a pharmaceutical composition having the above-mentioned properties.Type: ApplicationFiled: March 26, 2013Publication date: October 24, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Stephan Karl ZAHN, Guido BOEHMELT, Andreas MANTOULIDIS, Ulrich REISER, Matthias TREU, Ulrich GUERTLER, Andreas SCHOOP, Flavio SOLCA, Ulrike TONTSCH-GRUNT, Ralph BRUECKNER, Charlotte REITHER, Lars HERFURTH, Oliver KRAEMER, Heinz STADTMUELLER, Harald ENGELHARDT
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Publication number: 20130281433Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Patent number: 8563576Abstract: The present invention relates to compounds of tricyclic pyrazolopyridine useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: GrantFiled: December 1, 2011Date of Patent: October 22, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy Brenchley, Dean Boyall, Damien Fraysse, Juan-Miguel Jimenez, Luca Settimo
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Patent number: 8563539Abstract: Disclosed are compounds, pharmaceutical compositions containing those compounds, and uses of the compounds and compositions as modulators of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway. Uses are also disclosed for the treatment or prevention of a range of therapeutic indications due at least in part to aberrant physiological activity of casein kinase 1 (e.g., CK1?), casein kinase 2 (CK2), Pim 1, Pim2, Pim3, the TGF? pathway, the Wnt pathway, the JAK/STAT pathway, and/or the mTOR pathway.Type: GrantFiled: December 23, 2010Date of Patent: October 22, 2013Assignee: Jasco Pharmaceuticals, LLCInventors: Carmen M. Baldino, Justin L. Caserta, Chee-Seng Lee, Robert B. Nicewonger, Yvonne L. Flanders, Stephane A. Dumas
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Publication number: 20130274244Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof in which R1, R2, R3, R4, R5 and R6 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of fibrosis, bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases, pain and burns in a mammal.Type: ApplicationFiled: December 13, 2011Publication date: October 17, 2013Inventors: Mark Laurence Boys, Robert Kirk Delisle, Erik James Hicken, April L. Kennedy, David A. Mareska, Fredrik P. Marmsater, Mark C. Munson, Brad Newhouse, Bryson Rast, James P. Rizzi, Martha E. Rodriguez, George T. Topalov, Qian Zhao
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Publication number: 20130274241Abstract: Compounds of Formula (I) are used for the treatment of inflammation and autoimmune disorders.Type: ApplicationFiled: December 16, 2011Publication date: October 17, 2013Applicant: MERCK SERONO S.A. - INTELLECTUAL PROPERTYInventors: Catherine Jorand-Lebrun, Stefano Crosignani, Jerome Dorbais, Tania Grippi-Vallotton, Adeline Pretre
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Patent number: 8551985Abstract: [Object] It is to provide a novel LXR? agonist useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate: (wherein, each V and W independently show N or C—R7; each X and Y independently show CH2, C?O, SO2, etc; Z shows CH or N; each R1, R2 and R7 independently show a hydrogen atom, C1-8 alkyl group, etc.; R3 shows C1-8 alkyl group; R4 shows an optionally substituted C6-10 aryl group or an optionally substituted 5- to 11-membered heterocyclic group; R5 and R6 show a hydrogen atom, etc.; L shows a C1-8 alkyl chain optionally substituted with an oxo group, etc.; and n shows any integer of 0 to 2.Type: GrantFiled: April 28, 2010Date of Patent: October 8, 2013Assignee: Kowa Company, Ltd.Inventors: Minoru Koura, Hisashi Sumida, Takayuki Matsuda, Yuichiro Watanabe, Takashi Enomoto, Kimiyuki Shibuya, Sumiko Kurobuchi
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Patent number: 8551982Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n 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: GrantFiled: March 13, 2012Date of Patent: October 8, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
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Publication number: 20130261106Abstract: The present invention relates to compounds of formula (I): wherein R6 is —CONH2 or a —C(R?)(R?)(OH) group; R is a substituted phenyl or heteroaryl group; R7 is an optionally substituted aryl or heteroaryl group. Process for the preparation thereof and therapeutic use thereof.Type: ApplicationFiled: April 2, 2013Publication date: October 3, 2013Applicant: SANOFIInventors: Jean-Christophe CARRY, Fabienne CHATREAUX, Stephanie DEPRETS, Olivier DUCLOS, Vincent LEROY, Sergio MALLART, Dominique MELON-MANGUER, Maria MENDEZ-PEREZ, Fabrice VERGNE
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Publication number: 20130253186Abstract: Heteroaryloxyheterocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: May 10, 2013Publication date: September 26, 2013Applicant: Amgen Inc.Inventors: Jennifer R. Allen, Daniel B. Horne, Essa Hu Harrington, Matthew R. Kaller, Holger Monenschein, Thomas T. Nguyen, Andreas Reichelt, Robert M. Rzasa
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Publication number: 20130252939Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: April 30, 2013Publication date: September 26, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, John Studley, Ronald Knegtel, Luca Settimo, Christopher John Davis, Damien Fraysse, Philip N. Collier, Guy Brenchley, Dean Boyall, Andrew Miller, Heather Twin, Stephen Young
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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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Patent number: 8541402Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: GrantFiled: May 3, 2012Date of Patent: September 24, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Joly, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
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Publication number: 20130245002Abstract: 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: September 13, 2012Publication date: September 19, 2013Applicant: NOVARTIS AGInventors: Chao CHEN, Haibing DENG, Haibing GUO, Feng HE, Lei JIANG, Fang LIANG, Yuan MI, Huixin WAN, Yao-Chang XU, Hongping YU, Ji Yue ZHANG
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Publication number: 20130244995Abstract: Compounds of general 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: ApplicationFiled: November 21, 2011Publication date: September 19, 2013Applicant: LEO PHARMA A/SInventors: Per Vedsø, Lars Kristian Albert Blæhr
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Publication number: 20130244996Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n 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: ApplicationFiled: March 5, 2013Publication date: September 19, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, Steven Richard BRUNETTE, Michael J. BURKE, Suresh R. KAPADIA, Thomas Martin KIRRANE, Matthew Russell NETHERTON, Hossein RAZAVI, Sonia RODRIGUEZ, Anjan SAHA, Robert SIBLEY, Lana Louise SMITH-KEENAN, Hidenori TAKAHASHI, Michael Robert TURNER, Jiang-Ping WU, Erick Richard Roush YOUNG, Qiang ZHANG, Qing ZHANG, Renee M. ZINDELL
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Publication number: 20130244999Abstract: The present invention relates to substituted heterocyclic compounds of Formula I: or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors/antagonists useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.Type: ApplicationFiled: May 6, 2013Publication date: September 19, 2013Applicant: Incyte CorporationInventors: Colin Zhang, Ding-quan Qian, Jincong Zhuo, Wenqing Yao
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Patent number: 8536168Abstract: The present disclosure relates to compounds relating to the diagnosis and treatment of pathologies relating to the Hedgehog pathway, including but not limited to tumor formation, cancer, neoplasia, and non-malignant hyperproliferative disorders; specifically relating to compounds of formula I:Type: GrantFiled: March 13, 2008Date of Patent: September 17, 2013Assignee: Novartis AGInventors: Miao Dai, Feng He, Rishi Kumar Jain, Rajesh Karki, Joseph Kelleher, III, John Lei, Luis Llamas, Michael A. Mcewan, Karen Miller-Moslin, Lawrence Bias Perez, Stefan Peukert, Naeem Yusuff
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Publication number: 20130231332Abstract: The present invention relates to compositions and methods for the treatment of infection by enveloped viruses, such as Ebola and Lassa fever viruses.Type: ApplicationFiled: September 1, 2011Publication date: September 5, 2013Inventors: James Cunningham, Kyungae Lee, Tao Ren, Kartik Chandran
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TRANSAMINATION OF NITROGEN-CONTAINING COMPOUNDS TO MAKE CYCLIC AND CYCLIC/ACYCLIC POLYAMINE MIXTURES
Publication number: 20130231476Abstract: A transamination process is described to prepare polyamine product mixtures from reactants comprising mixed nitrogen-containing compounds with binary carbon spacing between nitrogen-containing groups (a binary component). A second nitrogen-containing component with a second carbon atom spacing between nitrogen-containing groups may also be employed. The molar ratio between the binary and second components can be adjusted to customize the product composition for desired end uses.Type: ApplicationFiled: October 20, 2011Publication date: September 5, 2013Applicant: Dow Global Technologies LLCInventor: Stephen W. King -
Publication number: 20130231331Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.Type: ApplicationFiled: March 1, 2013Publication date: September 5, 2013Inventors: Annapurna Pendri, David R. Langley, Samuel Gerritz, Guo Li, Weixu Zhai, Stanley D'Andrea, Manoj Patel, B. Narasimhulu Naidu, Kevin Peese, Zhongyu Wang
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Patent number: 8524705Abstract: The invention provides compounds of formula (I), and pharmaceutically and agriculturally acceptable salts thereof: wherein: R1, R2, R3, R4, R5, R6, R7, R8, A1, L1 and n are as defined herein. These compounds and their pharmaceutically acceptable salts are useful in the manufacture of medicaments for use in the prevention or treatment of a fungal disease. Compounds of formula (I), and agriculturally acceptable salts thereof, may also be used as agricultural fungicides.Type: GrantFiled: May 21, 2008Date of Patent: September 3, 2013Assignee: F2G Limited British Body CorporateInventors: Lloyd James Payne, Robert Downham, Graham Edward Morris Sibley, Philip Edwards, Gareth Morse Davies
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Publication number: 20130225562Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R0 to R3 and L 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: ApplicationFiled: March 25, 2011Publication date: August 29, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Peter Ettmayer, Steffen Steurer
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Publication number: 20130224195Abstract: New substituted benzazole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: April 3, 2013Publication date: August 29, 2013Inventors: Abran Costales, Teresa Hansen, Barry H. Levine, Christopher McBride, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Cynthia M. Shafer, Sharadha Subramanian, Joelle Verhagen
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Publication number: 20130225564Abstract: Provided herein are Aminopurine Compounds having the following structure: wherein R1, R2 and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.Type: ApplicationFiled: March 18, 2013Publication date: August 29, 2013Applicant: Signal Pharmaceuticals, LLCInventor: Signal Pharmaceuticals, LLC
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Publication number: 20130224107Abstract: Disclosed are heterocyclic derivatives, methods for making them, compositions containing the same and uses thereof. Particularly, their pharmaceutical use as inhibitors of PARP is disclosed.Type: ApplicationFiled: December 2, 2010Publication date: August 29, 2013Applicant: SHANGHAI DE NOVO PHARMATECH CO LTD.Inventor: Daxin Gao
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Publication number: 20130225548Abstract: A main object of the present invention is to provide a novel pyridine derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof. In formula [1], R represents an aryl group or a heteroaryl group, which may be substituted by an optionally substituted alkyl group, a hydroxy group, a halogen atom or a group represented by general formula [2]. In formula [2], -L1-L2-L3-RA ??[2] L1 and L3 independently represent a single bond, an alkylene group or a cycloalkylene group; L2 represents a single bond, O, or NRB; RB represents H or an optionally substituted alkyl group; and RA represents B, an amino group, a cyano group, a hydroxy group, an alkoxy group, an aryl group, a monoalkylamino group, a dialkylamino group, a carbamoyl group, an alkyloxycarbonyl group, a monoalkylaminocarbonyl group, a dialkylaminocarbonyl group, an alkylcarbonylamino group, and a saturated heterocyclic group, among other groups.Type: ApplicationFiled: October 27, 2011Publication date: August 29, 2013Applicant: NIPPON SHINYAKU CO., LTD.Inventors: Hidetaka Fujihara, Hiroyuki Sugiyama, Takashi Tsuji, Takara Ino, Yoshinari Haruta
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Patent number: 8518936Abstract: Monohydrochloride acid addition salts of a polyacidic basic compound, or a water adduct having basic site(s) stronger than pyridine. These monohydrochlorides can be produced by reacting a polyacidic basic compound with an acid salt of pyridine.Type: GrantFiled: April 16, 2010Date of Patent: August 27, 2013Assignee: Kowa Co., Ltd.Inventors: Kimiyuki Shibuya, Tadaaki Ohgiya, Takayuki Matsuda
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Publication number: 20130217661Abstract: Quinazoline derivatives of the following formula: wherein R1, R2, R3, R4, R5, X, Y, and Z are defined herein. It also discloses a method of treating cancer with one of these compounds.Type: ApplicationFiled: March 18, 2013Publication date: August 22, 2013Applicant: HUTCHISON MEDIPHARMA ENTERPRISES LIMITEDInventor: Hutchison Medipharma Enterprises Limited