Three Or More Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/117)
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Publication number: 20140155385Abstract: The present invention relates to 6-5 membered fused pyridine ring compounds according to formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to formula I in the treatment of Brutons Tyrosine Kinase (Btk) mediated disorders.Type: ApplicationFiled: July 11, 2012Publication date: June 5, 2014Inventors: Tjeerd A. Barf, Christian Gerardus Johannes Maria Jans, Petrus Antonius De Adrianus Man, Arthur A. Oubrie, Hans C.A. Raaijmakers, Johannes Bernardus Maria Rewinkel, Jan-Gerard Sterrenburg, Jacobus C.H.M. Wijkmans
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Publication number: 20140154240Abstract: The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof 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: May 30, 2013Publication date: June 5, 2014Inventors: Kerim Babaoglu, Constantine G. Boojamra, Eugene J. Eisenberg, Hon Chung Hui, Richard L. Mackman, Jay P. Parrish, Michael Sangi, Oliver L. Saunders, Dustin Siegel, David Sperandio, Hai Yang
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Patent number: 8735387Abstract: The present invention relates to oxazolopyrimidine compounds of the formula I in which A, R1, R2 and R3 are defined as indicated in the claims. The compounds of the formula I modulate the activity of the Edg-1 receptor and in particular are agonists of this receptor, and are useful for the treatment of diseases such as atherosclerosis, heart failure or peripheral arterial occlusive disease, for example. 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 compositions comprising them.Type: GrantFiled: July 2, 2009Date of Patent: May 27, 2014Assignee: SanofiInventors: Dieter Kadereit, Matthias Schaefer, Werngard Czechtizky
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Publication number: 20140135315Abstract: There is provided a compound of formula I: or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula 1, and the use of a compound of Formula 1 as a medicament and in the treatment of cancer.Type: ApplicationFiled: April 9, 2013Publication date: May 15, 2014Applicant: KuDOS Pharmaceuticals LimitedInventor: KuDOS Pharmaceuticals Limited
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Publication number: 20140128388Abstract: Drug candidates for inhibition of HIV-1 replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3-diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-1 viral replication in vitro.Type: ApplicationFiled: July 31, 2013Publication date: May 8, 2014Applicant: University of Pittsburgh - Of the Commonwealth System of Higher EducationInventors: Lori Emert-Sedlak, Toshiaki Kodama, Billy W. Day, Weixiang Dai, Ronald P. Trible, Thomas E. Smithgall
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Publication number: 20140128390Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and mutant c-kit protein kinases.Type: ApplicationFiled: September 5, 2013Publication date: May 8, 2014Inventors: JACK LIN, JOHN BUELL, KATRINA CHAN, TODD EWING, PRABHA IBRAHIM, MARIKA NESPI, PHUONGLY PHAM, SONGYUAN SHI, WAYNE SPEVAK, GUOXIAN WU, JIAZHONG ZHANG, YING ZHANG
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Patent number: 8716282Abstract: The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.Type: GrantFiled: April 28, 2011Date of Patent: May 6, 2014Assignee: Janssen Pharmaceutica NVInventors: Joaquin Pastor-Fernández, José Manuel Bartolomé-Nebreda, Gregor James Macdonald, Susana Conde-Ceide, Óscar Delgado-González, Greta Constantia Peter Vanhoof, Michiel Luc Maria Van Gool, María Luz Martín-Martín, Sergio-Alvar Alonso-de Diego, Kelly Ann Swinney, Carina Leys, Johan Erwin Edmond Weerts, Stijn Wuyts
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Publication number: 20140121200Abstract: Provided are pyridopyrazine compounds of formula (1), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, R4 and m are as defined in the specification.Type: ApplicationFiled: June 7, 2012Publication date: May 1, 2014Applicant: HUTCHISON MEDIPHARMA LIMITEDInventors: Wei-Guo Su, Wei Deng, Jianguo Ji
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Patent number: 8710219Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.Type: GrantFiled: March 30, 2012Date of Patent: April 29, 2014Assignee: Curis, Inc.Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Changgeng Qian, Rudi Bao
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Publication number: 20140113882Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R7, R8, R9, G, and X are as defined herein. This application further describes compositions comprising the same. Compounds of formula (I) and their salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.Type: ApplicationFiled: September 27, 2013Publication date: April 24, 2014Applicants: Cancer Research Technology Limited, Cephalon, Inc.Inventors: Henry J. Breslin, Bruce D. Dorsey, Benjamin J. Dugan, Katherine M. Fowler, Robert L. Hudkins, Eugen F. Mesaros, Nathaniel J.T. Monck, Emma L. Morris, Ikeoluwa Olowoye, Gregory R. Ott, Gregoire A. Pave, Jonathan R. Roffey, Christelle N. Soudy, Ming Tao, Craig A. Zificsak, Allison L. Zulli
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Publication number: 20140107099Abstract: The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.Type: ApplicationFiled: December 19, 2013Publication date: April 17, 2014Applicant: Genentech, Inc.Inventors: Jeffrey Blaney, Paul A. Gibbons, Emily Hanan, Joseph P. Lyssikatos, Steven R. Magnuson, Richard Pastor, Thomas E. Rawson, Aihe Zhou, Bing-Yan Zhu
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Publication number: 20140107098Abstract: Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: ApplicationFiled: December 19, 2013Publication date: April 17, 2014Applicant: Janssen Pharmaceutica NVInventors: Bryan James Branstetter, J. Guy Breitenbucher, Alec D. Lebsack, Jing Liu, Jason C. Rech, Wei Xiao
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Publication number: 20140107118Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.Type: ApplicationFiled: December 20, 2013Publication date: April 17, 2014Applicant: NOVARTIS AGInventors: Sangamesh BADIGER, Murali CHEBROLU, Konstanze HURTH, Sebastien JACQUIER, Rainer Martin LUEOEND, Rainer MACHAUER, Heinrich RUEEGER, Marina TINTELNOT-BLOMLEY, Siem Jacob VEENSTRA, Markus VOEGTLE
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Publication number: 20140100366Abstract: Process methods for making the dual mTOR/PI3K inhibitor GDC-0980, named as (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one, having the structure: and stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: October 9, 2013Publication date: April 10, 2014Applicant: Genentech, Inc.Inventors: Srinivasan Babu, Zhigang Cheng, Francis Gosselin, Pirmin Hidber, Ursula Hoffmann, Theresa Humphries, Reinhard Reents, Qingping Tian, Herbert Yajima
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Publication number: 20140088096Abstract: Disclosed are chemical entities that inhibit ubiquitin-activating enzyme (UAE), each of which is a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Y is and W, Z, XY, RY1, RY2 and RY3 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers.Type: ApplicationFiled: February 14, 2013Publication date: March 27, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Roushan Afroze, Indu T. Bharathan, Jeffrey P. Ciavarri, Paul E. Fleming, Jeffrey L. Gaulin, Mario Girard, Steven P. Langston, Francois Soucy, Tzu-Tshin Wong, Yingchun Ye
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Patent number: 8680099Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.Type: GrantFiled: June 10, 2011Date of Patent: March 25, 2014Assignee: Afraxis Holdings, Inc.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
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Patent number: 8673905Abstract: Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of AML.Type: GrantFiled: March 9, 2012Date of Patent: March 18, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Kin-Chun Luk, Michael Soth
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Publication number: 20140073640Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: ApplicationFiled: August 12, 2013Publication date: March 13, 2014Inventors: Andrew S. Judd, Andrew J. Souers, Zhi-Fu Tao
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Publication number: 20140073626Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, JAK3, TEC, Btk, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as cancer and inflammatory diseases such as arthritis, and the like. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts and processes for preparing such compounds and pharmaceutically acceptable salts.Type: ApplicationFiled: May 16, 2012Publication date: March 13, 2014Applicant: Principia BiopharmaInventors: David Michael Goldstein, Kenneth Albert Brameld, Erik Verner
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Publication number: 20140073782Abstract: The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.Type: ApplicationFiled: November 11, 2013Publication date: March 13, 2014Applicant: Endo Pharmaceuticals Inc.Inventors: Roger A. Smith, Scott Kevin Thompson, Subramanya Hosahalli, Mallesham Bejugam, Srinivas Nanduri, Sunil Kumar Panigrahi, Natarajan Mahalingam
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Publication number: 20140065136Abstract: Dioxino- and oxazin-[2,3-d]pyrimidine PI3K inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions.Type: ApplicationFiled: August 29, 2013Publication date: March 6, 2014Applicant: Genentech, Inc.Inventors: Robert Andrew Heald, Neville James McLean
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Patent number: 8658794Abstract: The present invention provides 8-methyl-1-phenyl-imidazo[1,5-a]pyrazine derivatives according to formula I or pharmaceutically acceptable salts thereof. The compounds of the current invention show inhibitory activity against Lck and can be used for the treatment of Lck-mediated diseases or Lck-mediated conditions such as inflammatory disorders.Type: GrantFiled: February 3, 2011Date of Patent: February 25, 2014Assignee: Merck Sharp & Dohme B.V.Inventors: Adrianus Petrus Antonius de Man, Johannes Bernardus Maria Rewinkel, Christiaan Gerardus Johannes Maria Jans, Hans Cornelis Andreas Raaijmakers, Jacobus Cornelis Henricus Maria Wijkmans
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Patent number: 8658646Abstract: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: August 31, 2012Date of Patent: February 25, 2014Assignee: Hoffmann-LaRoche Inc.Inventors: Shaoqing Chen, Javier de Vicente Fidalgo, Matthew Michael Hamilton, Johannes Cornelius Hermann, Joshua Kennedy-Smith, Hongju Li, Allen John Lovey, Matthew C. Lucas, Kin-Chun Thomas Luk, Stephen M. Lynch, Counde O'yang, Fernando Padilla, Ryan Craig Schoenfeld, Achyutharao Sidduri, Michael Soth, Ce Wang, Peter Michael Wovkulich, Xiaohu Zhang
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Publication number: 20140051699Abstract: Novel PI3K, especially PI3K delta isoform, selective inhibitors are disclosed. The compounds are useful in treating disorders related to abnormal PI3K or PI3K? activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.Type: ApplicationFiled: October 28, 2013Publication date: February 20, 2014Applicant: Xcovery Holding Company, LLCInventor: Congxin Liang
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Publication number: 20140045814Abstract: The present invention relates to pyrazine derivatives, and pharmaceutical compositions including the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.Type: ApplicationFiled: August 9, 2013Publication date: February 13, 2014Applicant: Incyte CorporationInventors: Liang Lu, Chunhong He, Wenqing Yao
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Patent number: 8648067Abstract: The present invention provides compounds of formula I: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.Type: GrantFiled: December 22, 2011Date of Patent: February 11, 2014Assignees: Cephalon, Inc., Teva SanteInventors: Edward R. Bacon, Thomas R. Bailey, Sankar Chatterjee, Derek D. Dunn, Greg A. Hostetler, Robert L. Hudkins, Brigitte Lesur, Babu G. Sundar, Allison L. Zulli, Christophe Yue
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Patent number: 8648074Abstract: The present application relates to: (a) compounds of Formula (I): and salts thereof, wherein Z?, Z?, L2, G2, R1, and R2 are as defined in the specification; (b) compositions comprising such compounds and salts; and (c) methods of use of such compounds, salts, and compositions, particularly use as calcium channel blockers.Type: GrantFiled: September 26, 2012Date of Patent: February 11, 2014Assignee: AbbVie Inc.Inventors: Tao Li, Sachin V. Patel, Richard J. Perner, John T. Randolph, Michael R. Schrimpf, Kevin R. Woller, Zhiren Xia, Qingwei Zhang
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Publication number: 20140038957Abstract: This invention relates to pyrrolopyrimidine derivatives of formula (I): where R1, X, p, R4, R2 and R3 are as defined herein, and their use as pharmaceuticals.Type: ApplicationFiled: December 15, 2011Publication date: February 6, 2014Inventors: David R. Witty, David Norton, Jason Paul Tierney, Ghislaine Lorthioir, Mairi Sime, Karen Louise Philpott
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Publication number: 20140038952Abstract: The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts, prodrugs, and solvates thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.Type: ApplicationFiled: August 2, 2013Publication date: February 6, 2014Applicant: Endo Pharmaceuticals Inc.Inventors: Roger Astbury Smith, Aranapakam Venkatesan, Mallesham Bejugam, Subramanya Hoshalli, Srinivas Nanduri
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Patent number: 8642594Abstract: Compounds of formula (1) are inhibitors of HSP90 activity in vitro or in vivo, and of use in the treatment of inter alia, cancer: wherein R2 is a group of formula —(Ar1)m-(Alk1)P-(Z)r-(Alk2)S-Q wherein Ar1 is an optionally substituted aryl or heteroaryl radical, Alk? and Alk 2 are optionally substituted divalent C1-C3 alkylene or C2-C3 alkenylene radicals, m, p, r and s are independently 0 or 1, Z is —O—, —S—, —(C?O)—, —(C?S)—, —SO2—, —C(?O)O—, —C(?O)NRA—, —C(?S)NRA—, —SO2NRA—, —NRAC(?O)—, —NRASO2— or —NRA— wherein RA is hydrogen or C1-C6 alkyl, and Q is hydrogen or an optionally substituted carbocyclic or heterocyclic radical; R3 is hydrogen, an optional substituent, or an optionally substituted (C1-C6)alkyl, aryl or heteroaryl radical; and R4 is a carboxylic ester, carboxamide or sulfonamide group.Type: GrantFiled: January 21, 2010Date of Patent: February 4, 2014Assignees: Vernalis (R&D) Limited, Cancer Research Technology Ltd., The Institute of Cancer ResearchInventors: Brian William Dymock, Martin James Drysdale, Christofe Fromont, Allan Jordan, Xavier Barril-Alonso
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Publication number: 20140018361Abstract: The present invention provides furano- and pyrrolo-pyrimidine and pyridine compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: July 11, 2013Publication date: January 16, 2014Inventors: Geraldine C. Harriman, Donna L. Romero, Craig E. Masse, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
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Publication number: 20140005183Abstract: The present invention provides novel 4,5-disubstituted-7H-pyrrolo[2,3-d]pyrimidine derivatives of Formula I, and the pharmaceutically acceptable salts thereof wherein R1, R2, R3, R4 and R5 are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.Type: ApplicationFiled: June 27, 2013Publication date: January 2, 2014Inventors: Paul Galatsis, Matthew Merrill Hayward, Bethany Lyn Kormos, Travis T. Wager, Lei Zhang, Antonia Friederike Stepan, Jaclyn Louise Henderson, Ravi G. Kurumbail, Patrick Robert Verhoest
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Publication number: 20140005166Abstract: The present invention provides piperidinylcyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I, as defined herein, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: May 17, 2013Publication date: January 2, 2014Applicant: Incyte CorporationInventors: JAMES D. RODGERS, Stacey Shepard, Wenyu Zhu, Lixin Shao, Joseph Glenn
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Publication number: 20140005188Abstract: A compound of formula (I): or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, and autoimmune conditions.Type: ApplicationFiled: March 8, 2012Publication date: January 2, 2014Applicant: GLAXO GROUP LIMITEDInventors: Francis Louis Atkinson, Stephen John Atkinson, Michael David Barker, Clement Douault, Neil Stuart Garton, John Liddle, Vipulkumar Kantibhai Patel, Alexander G. Preston, Tracy Jane Shipley, David Matthew Wilson, Robert J. Watson
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Patent number: 8618103Abstract: The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R?, X, X?, Y, Z1, Z2, and Z3 are defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.Type: GrantFiled: September 9, 2010Date of Patent: December 31, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Javier de Vicente Fidalgo, Johannes Cornelius Hermann, Remy Lemoine, Hongju Li, Allen John Lovey, Eric Brian Sjogren, Michael Soth
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Patent number: 8614208Abstract: The present invention provides a fused heterocycle derivative having a strong Smo inhibitory activity, and use thereof. Specially, the present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or salt thereof, and a medicament containing the compound or a prodrug thereof, which is an Smo inhibitor or an agent for the prophylaxis or treatment of cancer.Type: GrantFiled: August 25, 2010Date of Patent: December 24, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Hiroshi Banno, Toshio Tanaka, Satoshi Sasaki
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Publication number: 20130338153Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.Type: ApplicationFiled: June 10, 2011Publication date: December 19, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
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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: 20130338137Abstract: The present application relates to novel substituted annellated pyrimidines, methods for production thereof, use thereof alone or in combinations for treating and/or preventing diseases and use thereof for the production of medicinal products for treating and/or preventing diseases, in particular for treating and/or preventing cardiovascular diseases.Type: ApplicationFiled: August 30, 2012Publication date: December 19, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus FOLLMANN, Johannes-Peter STASCH, Gorden REDLICH, Nils GRIEBENOW, Dieter LANG, Frank WUNDER, Walter HÜBSCH, Niels LINDNER, Alexandros VAKALOPOULOS, Adrian TERSTEEGEN
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Publication number: 20130338142Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of an imidazopyrazine compound effective to reduce signs or symptoms of the disease or disorder are provided.Type: ApplicationFiled: June 14, 2013Publication date: December 19, 2013Inventors: Peter A. BLOMGREN, Kevin S. CURRIE, Randall HALCOMB, Jeffrey E. KROPF, Seung H. LEE, Jiayao LI, Jennifer R. LO, Scott A. MITCHELL, Aaron SCHMITT, Qiaoyin WU, Jin-Min XIONG, Jianjun XU, Zhongdong ZHAO, Jayaraman CHANDRASEKHAR, Eric LANSDON
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Patent number: 8609838Abstract: The present invention relates to purine compounds that are useful as kinase inhibitors. More particularly, the present invention relates to purine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative conditions or disorders. These compounds may be useful as medicaments for the treatment of a number of proliferative conditions or disorders including tumors and cancers as well as other disorders or conditions related to or associated with PI3 and/or mTOR kinases.Type: GrantFiled: July 20, 2012Date of Patent: December 17, 2013Assignee: Verastem, Inc.Inventors: Harish K. Nagaraj, Meredith Williams
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Publication number: 20130331375Abstract: There are provided compounds of the formula (I) wherein Q, R1 and R2 are defined herein. The compounds have activity as anticancer agents.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Nancy-Ellen Haynes, Johannes Hermann, Kyungjin Kim, Nathan Robert Scott, Lin Yi, Mark Zak
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Publication number: 20130324527Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof: compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.Type: ApplicationFiled: December 16, 2011Publication date: December 5, 2013Applicant: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdella Tahri, Steven Maurice Paula Van Hoof, Sandrine Marie Helene Vendeville
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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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Patent number: 8598156Abstract: The invention is directed to substituted indoline derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1, R2, and R3 are defined herein. The compounds of the invention are inhibitors of PERK and can be useful in the treatment of cancer, ocular diseases, and diseases associated with activated unfolded protein response pathways, such as Alzheimer's disease, stroke, Type 1 diabetes Parkinson disease, Huntington's disease, amyotrophic lateral sclerosis, myocardial infarction, cardiovascular disease, atherosclerosis, and arrhythmias, and more specifically cancers of the breast, colon, pancreatic, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PERK activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: GrantFiled: March 23, 2011Date of Patent: December 3, 2013Assignee: GlaxoSmithKline LLCInventors: Jeffrey Michael Axten, Seth Wilson Grant, Dirk A. Heerding, Jesus Rual Medina, Stuart Paul Romeril, Jun Tang
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Patent number: 8586580Abstract: Disclosed are a 2,7-substituted thieno[3,2-d]pyrimidine compound having a protein kinase inhibition activity, a pharmaceutically acceptable salt, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth comprising the compound as an effective ingredient. Since the novel 2,7-substituted thieno[3,2-d]pyrimidine compound exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating diseases caused by abnormal cell growth.Type: GrantFiled: October 15, 2010Date of Patent: November 19, 2013Assignee: Korea Institute of Science and TechnologyInventors: Tae Bo Sim, Hwan Geun Choi, Jung Mi Hah, Young Jin Ham, Eun Jin Jun, Jung Hun Lee, Hwan Kim
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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: 20130303533Abstract: Provided herein are azolopyridine and azolopyrimidine compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 31, 2011Publication date: November 14, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventors: Qi Chao, Michael J. Hadd, Mark W. Holladay, Martin Rowbottom
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Publication number: 20130303532Abstract: The present invention relates to substituted imidazopyrazine compounds of general formula (I): in which R1, R2, R3, R4 and R5 are as defined in the claims, to methods of and intermediates for 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: December 13, 2011Publication date: November 14, 2013Applicant: BAYER INTELLECTUAL PROPERTY GmbHInventors: Marcus Koppitz, Ulrich Klar, Rolf Jautelat, Dirk Kosemund, Rolf Bohlmann, Benjamin Bader, Philip Lienau, Gerhard Siemeister
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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