Four Or More Ring Nitrogens In The Bicyclo Ring System Patents (Class 544/118)
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Publication number: 20140243523Abstract: A cellular model is described that targets dysregulation or inappropriate activation of the Sonic Hedgehog/Patched (SHH/PTCH) pathway. Also described, is a screening method using this cellular model to screen for pharmacological compounds that can treat or prevent skin cancer, in particular, Basal Cell Carcinoma (BCC) lesions.Type: ApplicationFiled: September 24, 2012Publication date: August 28, 2014Applicants: GALDERMA RESEARCH & DEVELOPMENT, CNRSInventors: Elodie Burty, Thierry Magnaldo, Yannick Gache, Jérôme Aubert
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Publication number: 20140235632Abstract: The present invention concerns a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, where R1-R3 and Y are defined in the description, and its use in the treatment of disorders in which pi3 kinase is implicated.Type: ApplicationFiled: April 25, 2014Publication date: August 21, 2014Applicant: NOVARTIS AGInventors: Graham Charles Bloomfield, Ian Bruce, Brian Cox, Lee Edwards, Judy Fox Hayler, Catherine Howsham
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Publication number: 20140234852Abstract: A cellular model is described for targeting dysregulation or inappropriate activation of the Sonic Hedgehog/Patched (SHH/PTCH) pathway. Also described, is a screening method using this cellular mod& to screen for pharmacological compounds that can treat or prevent skin cancer and, in particular, Basal Cell Carinoma (BCC) lesions.Type: ApplicationFiled: September 24, 2012Publication date: August 21, 2014Applicants: GALDERMA RESEARCH & DEVELOPMENT, CNRSInventors: Elodie Burty, Thierry Magnaldo, Yannick Gache
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Publication number: 20140235856Abstract: A cellular model is described that targets dysregulation or inappropriate activation of the Sonic Hedgehog/Patched (SHH/PTCH) pathway. Also described, is a screening method using this cellular model to screen for pharmacological compounds that can treat or prevent skin cancer, in particular, Basal Cell Carcinoma, (BCC) lesions.Type: ApplicationFiled: September 24, 2012Publication date: August 21, 2014Inventors: Elodie Burty, Thierry Magnaldo, Yannick Gache
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Publication number: 20140221646Abstract: The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.Type: ApplicationFiled: February 12, 2014Publication date: August 7, 2014Applicant: JANUS BIOTHERAPEUTICS, INC.Inventors: Grayson B. LIPFORD, Charles M. ZEPP
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Publication number: 20140213737Abstract: A method for enhancing, by at least 10 fold, the antibacterial activity of an antisense oligonucleotide composed of morpholino subunits linked by phosphorus-containing intersubunit linkages. The method includes one or both of: conjugating an arginine-rich carrier to a 3? or 5? end of the oligonucleotide and modifying the oligonucleotide to contain 20%-50% intersubunit linkages that are positively charged at physiological pH. Also disclosed is an antisense oligonucleotide having enhanced antibacterial activity by virtue of one or both modifications.Type: ApplicationFiled: August 9, 2013Publication date: July 31, 2014Applicant: Sarepta Therapeutics, Inc.Inventors: Dwight D. Weller, Bruce L. Geller, Patrick L. Iversen, Lucas D. Tilley, Jed N. Hassinger
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Publication number: 20140206685Abstract: The present invention provides heterocyclic compounds for use as kinase inhibitors and in other applications. Also provided are pharmaceutical compositions and methods of treatments of diseases and conditions associated with P13 kinase activity.Type: ApplicationFiled: March 21, 2014Publication date: July 24, 2014Applicant: INTELLIKINE LLCInventors: Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN, Troy Edward WILSON
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Publication number: 20140206684Abstract: Chemical entities that modulate PI3 kinase activity, and chemical entities, pharmaceutical compositions, and methods of treatments of diseases and conditions associated with P13 kinase activity are described herein.Type: ApplicationFiled: March 21, 2014Publication date: July 24, 2014Applicant: INTELLIKINE LLCInventors: Pingda REN, Yi LIU, Troy Edward WILSON, Katrina CHAN, Christian ROMMEL, Liansheng LI
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Publication number: 20140170110Abstract: Compounds 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: May 21, 2012Publication date: June 19, 2014Applicant: ALMIRALL, S.A.Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Elena Gomez Castillo, Jordi Bach Taña
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Patent number: 8754080Abstract: The present invention relates to a purine compound useful as a kinase inhibitor. The compound has the structure (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 3, 2009Date of Patent: June 17, 2014Assignee: Verastem, Inc.Inventors: DiZhong Chen, Meredith Williams
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Publication number: 20140163027Abstract: Described herein are irreversible kinase inhibitor compounds, methods for synthesizing such irreversible inhibitors, and methods for using such irreversible inhibitors in the treatment of diseases. Further described herein are methods, assays and systems for determining an appropriate irreversible inhibitor of a protein, including a kinase.Type: ApplicationFiled: February 12, 2014Publication date: June 12, 2014Applicant: Pharmacyclics, Inc.Inventors: Erik Verner, Wei Chen
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Publication number: 20140163010Abstract: New pyrazolo[3,4-d]pyrimidine compounds having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for preparing these compounds, to compositions comprising them and to their use as medicaments.Type: ApplicationFiled: July 13, 2012Publication date: June 12, 2014Applicant: LABORATORIOS DEL DR. ESTEVE, S.A.Inventors: Maria Rosa Cuberes-Altisent, Jordi Corbera-Arjona, Jose Luis Diaz-Fernanadez, Carmen Almansa-Rosales
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Publication number: 20140155394Abstract: The present invention relates to compounds of Formula (I): and to their pharmaceutical compositions, and to their methods of use. These compounds provide a treatment for myeloproliferative disorders and cancer.Type: ApplicationFiled: June 21, 2013Publication date: June 5, 2014Applicant: Astrazeneca ABInventors: Audrey DAVIES, Stephanos IOANNIDIS, Michelle LAMB, Mei SU, Tao WANG, Hai-Jun ZHANG
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Publication number: 20140155593Abstract: Provided herein are methods to prepare Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein. The Heteroaryl compounds are useful for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions.Type: ApplicationFiled: February 7, 2014Publication date: June 5, 2014Applicant: SIGNAL PHARMACEUTICALS, LLCInventors: Roy L. Harris, John Sapienza, Graziella Shevlin, Patrick Papa, Branden Gingsee Lee, Garrick Packard, Jingjing Zhao, Patrick Anthony Jokiel, Deborah Mortensen, Jennifer Riggs, Juan Antonio Gamboa, Marie Georges Beauchamps, Matthew Michael Kreilein, Mohit Atul Kothare, Sophie Perrin-Ninkovic, Philip Pye, William Wei-Hwa Leong, Jan Elsner, Anusuya Choudhury
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Publication number: 20140154772Abstract: Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K? plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.Type: ApplicationFiled: November 27, 2013Publication date: June 5, 2014Applicant: ICOS CORPORATIONInventors: Chanchal SADHU, Ken DICK, Jennifer TREIBERG, C. Gregory SOWELL, Edward A. KESICKI, Amy OLIVER
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Patent number: 8741896Abstract: Compounds of the formula (I), in which X, R1 and R2 have the meanings indicated in claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumors.Type: GrantFiled: September 24, 2010Date of Patent: June 3, 2014Assignee: Merck Patent GmbHInventors: Hans Peter Buchstaller, Ulrich Emde, Markus Klein, Christina Esdar, Joerg Bomke
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Publication number: 20140142099Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, TEC, BTK, and TXK and are therefore useful for the treatment of diseases treatable by inhibition of tyrosine kinases such as autoimmune diseases, cancer and inflammatory diseases. Also provided are pharmaceutical compositions containing such compounds and pharmaceutically acceptable salts thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: November 19, 2013Publication date: May 22, 2014Applicant: Principia Biopharma Inc.Inventor: Timothy D. Owens
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Publication number: 20140142098Abstract: Disclosed are compounds of the formula (I) wherein the groups R1 to R3 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.Type: ApplicationFiled: November 11, 2013Publication date: May 22, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Harald ENGELHARDT, Davide GIANNI, Christian SMETHURST
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Patent number: 8729079Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.Type: GrantFiled: August 23, 2012Date of Patent: May 20, 2014Assignee: Endo Pharmaceuticals Inc.Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
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Publication number: 20140135492Abstract: The present application includes a compound of Formula I or II: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods that include the administration of such compounds with at least one additional active agent.Type: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Inventors: Michael Graupe, Randall L. Halcomb
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Publication number: 20140128389Abstract: The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: October 15, 2010Publication date: May 8, 2014Applicant: GILEAD SCIENCES, INC.Inventors: Randall L. Halcomb, Paul A. Roethle
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Publication number: 20140128599Abstract: The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications.Type: ApplicationFiled: May 13, 2013Publication date: May 8, 2014Applicant: Intellikine LLCInventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson
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Publication number: 20140121205Abstract: 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: May 1, 2014Applicant: 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: 8703767Abstract: In one aspect, the invention relates to substituted N-(3-(pyrimidin-4-yl)phenyl)acrylamide analogs, derivatives thereof, and related compounds, which are useful as inhibitors of the BTK kinase; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds and compositions to treat disorders associated with dysfunction of the BTK kinase. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: April 1, 2012Date of Patent: April 22, 2014Assignee: University of Utah Research FoundationInventors: David J. Bearss, Hariprasad Vankayalapati, Venkataswamy Sorna, Steven L. Warner, Sunil Sharma
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Publication number: 20140107115Abstract: The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.Type: ApplicationFiled: June 1, 2012Publication date: April 17, 2014Applicant: Janus Biotherapeutics, Inc.Inventors: Grayson B. Lipford, Charles M. Zepp
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Publication number: 20140100224Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.Type: ApplicationFiled: June 26, 2013Publication date: April 10, 2014Applicants: The University of North Carolina at Chapel Hill, U.S. Government represented by the Department of Veterans Affairs, The Regents of the University of CaliforniaInventors: Frank M. Longo, Stephen M. Massa
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Publication number: 20140094459Abstract: The present disclosure provides compounds and pharmaceutically acceptable salts thereof that are tyrosine kinase inhibitors, in particular BLK, BMX, EGFR, HER2, HER4, ITK, 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 thereof and processes for preparing such compounds and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: May 16, 2012Publication date: April 3, 2014Applicant: Princpia Biopharma Inc.Inventors: David Michael Goldstein, Kenneth Albert Brameld
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Patent number: 8686135Abstract: Provided herein are methods to prepare Heteroaryl Compounds having the following structure: wherein R1-R4 are as defined herein. The Heteroaryl compounds are useful for treating or preventing cancer, inflammatory conditions, immunological conditions, neurodegenerative diseases, diabetes, obesity, neurological disorders, age-related diseases, or cardiovascular conditions.Type: GrantFiled: April 30, 2013Date of Patent: April 1, 2014Assignee: Signal Pharmaceuticals, LLCInventors: Patrick Anthony Jokiel, Juan Antonio Gamboa, Philip Pye, William Wei-Hwa Leong, Anusuya Choudhury
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Publication number: 20140086984Abstract: The present invention provides a new use of 2-(4-morpholinoaniline)-6-cyclohexyl aminopurine and pharmaceutically acceptable salt or derivative thereof. The 2-(4-morpholinoaniline)-6-cyclohexyl aminopurine can inhibit the activated hepatic stellate cells from synthesizing and expressing collagens and other extracellular matrix proteins including MMPs and TIMPs, and so it can inhibit liver fibrosis. In the liver, it can inhibit collagen synthesis and expression, and therefore reverse and treat hepatitis and liver cirrhosis effectively. Also discloses is a method for preparing drugs for treating or preventing infective hepatitis, non-infectious hepatitis, liver injury, liver cirrhosis, liver cancer and liver fibrosis, and protecting and improving the liver function, in which the compound is used alone or in combination with a target molecule or carrier comprising a vitamin A-coupled liposome.Type: ApplicationFiled: December 2, 2013Publication date: March 27, 2014Applicant: ZHANGZHOU PIEN TZE HUANG PHARMACEUTICAL CO., LTD.Inventors: Jiahao Li, Ruohan Chen, Zhibo Hou, Quanwei Pan
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Publication number: 20140080827Abstract: The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.Type: ApplicationFiled: November 26, 2013Publication date: March 20, 2014Applicant: Rhizen Pharmaceuticals SAInventors: Meyyappan MUTHUPPALANIAPPAN, Srikant Viswanadha, Govindarajulu Babu, Swaroop Kumar V.S. Vakkalanka
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Publication number: 20140079724Abstract: The present invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.Type: ApplicationFiled: June 1, 2012Publication date: March 20, 2014Applicant: Janus Biotherapeutics, Inc.Inventors: Grayson B. Lipford, Charles M. Zepp
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Patent number: 8673907Abstract: The present invention concerns hydrochloric acid, hydrobromic acid and maleic acid salts of methyl (3-{[[3-(6-amino-2-butoxy-8-oxo-7,8-dihydro-9H-purin-9-yl)propyl](3-morpholin-4-ylpropyl)amino]methyl}phenyl)acetate, compositions comprising them and their use in therapy.Type: GrantFiled: December 16, 2008Date of Patent: March 18, 2014Assignees: AstraZeneca AB, Dainippon Sumitomo Pharma Co., Ltd.Inventors: Thomas McInally, Håkan Schulz
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Publication number: 20140073638Abstract: The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.Type: ApplicationFiled: October 16, 2013Publication date: March 13, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Publication number: 20140066620Abstract: 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 tumours and cancers as well as other disorders or conditions related to or associated with PI3 and/or mTOR kinases.Type: ApplicationFiled: November 11, 2013Publication date: March 6, 2014Applicant: VERASTEM, INC.Inventors: Harish K. Mysore, Meredith Williams
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Publication number: 20140051698Abstract: The present invention concerns a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, where R1-R3 and Y are defined in the description, and its use in the treatment of disorders in which pi3 kinase is implicated.Type: ApplicationFiled: October 9, 2013Publication date: February 20, 2014Applicant: NOVARTIS AGInventors: Ian Bruce, Judy Fox Hayler, Graham Charles Bloomfield, Lee Edwards, Brian Cox, Catherine Howsham
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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: 20140046056Abstract: Provided is a novel compound represented by the following formula wherein each symbol is as defined in the specification, or a salt thereof, which has an angiotensin II receptor antagonistic activity and a peroxisome proliferator-activated receptor ? agonistic activity, and is useful as an agent for the prophylaxis or treatment of circulatory diseases such as hypertension and the like and/or metabolic diseases such as diabetes and the like, and the like.Type: ApplicationFiled: October 22, 2013Publication date: February 13, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Tsuyoshi Maekawa, Hideyuki Igawa
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Patent number: 8648085Abstract: The invention relates to novel substituted pyrazolopyrimidines. Chemically, the compounds are characterized by general Formula (I): with R1 being phenyl or pyridyl, any of which is substituted with 1 to 4, preferably 1 to 3 substituents X; X independently of each other being selected from C2-C6-alky1 or Ci-C6-alkoxy, where C2-C6-alkyl and C1-C6-alkoxy are at least dihalogenated up to perhalogenated. preferably with 2 to 6 halogen substituents, and the halogen atoms being selected from the group of fluoro, chloro and bromo, preferably fluoro; R2 being phenyl or heteroaryl, where phenyl is substituted by 1 to 3 radicals and heteroaryl is optionally substituted by 1 to 3 radicals in each case independently of one another selected from the group of C1-C6-alkyl, C1-C6-alkoxy, hydroxycarbonyl, cyano, trifluoromethyl, amino, nitro, hydroxy, C1-C6-alkylamino, halogen, C6-C10-arylcarbonylamino, C1-C6-alkylcarbonylamino, C1-C6-alkylaminocarbonyl. C1-C6-alkoxycarbonyl, C6-C10-arylaminocarbonyl, heteroarylaminocarbonyl.Type: GrantFiled: November 27, 2008Date of Patent: February 11, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Christian Eickmeier, Cornelia Dorner-Ciossek, Dennis Fiegen, Thomas Fox, Klaus Fuchs, Riccardo Giovannini, Niklas Heine, Martin Hendrix, Holger Rosenbrock, Gerhard Schaenzle
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Publication number: 20140031539Abstract: The present invention relates to certain purines, which act as topoisomerase II catalytic inhibitors. These compounds are useful in combination with topoisomerase II poisons, such as anthracyclines and epipodophyllotoxins, in the treatment of proliferative conditions (e.g., cancer). These compounds are useful in the treatment of tissue damage associated with extravasation of a topoisomerase II poison, such as an anthracycline or an epipodophyllotoxin.Type: ApplicationFiled: July 3, 2013Publication date: January 30, 2014Applicant: Biocodex, IncInventors: Lars Hollund JENSEN, Maxwell SEHESTED
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Publication number: 20140018344Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating immunological disorders, cardiovascular disease, cancer, and other diseases, disorders or conditions associated with PI3K?.Type: ApplicationFiled: July 8, 2013Publication date: January 16, 2014Inventors: Edcon Chang, Wolfgang Reinhard Ludwig Notz, Michael B. Wallace
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Publication number: 20130345215Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt thereof, wherein Q, R1 and R2 are as defined herein. The compounds of formula I are useful in the treatment of cancer.Type: ApplicationFiled: June 6, 2013Publication date: December 26, 2013Inventors: Jianwen Feng, Nancy-Ellen Haynes, Johannes Cornelius Hermann, Kyungjin Kim, Jin-Jun Liu, Nathan Robert Scott, Lin Yi, Mark Edward Zak, Guiling Zhao
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Publication number: 20130345216Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: ApplicationFiled: August 20, 2013Publication date: December 26, 2013Applicant: INTELLIKINE LLCInventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
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Publication number: 20130331376Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, E1, E2, R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: August 14, 2013Publication date: December 12, 2013Applicant: Elan Corporation, Inc.Inventors: Robert A. Galemmo, Dean R. Artis, Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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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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Publication number: 20130324525Abstract: The present invention relates to novel heterocyclic compounds and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I): wherein Q1, Q2, R2, R3, R4, R5, and R6 are as described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: August 6, 2013Publication date: December 5, 2013Applicant: Gilead Sciences, Inc.Inventors: Matthew Abelman, Robert H. Jiang, Jeff Zablocki
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Publication number: 20130317023Abstract: A novel purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative, a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutical composition with an inhibitory activity against Raf kinase, containing the same as an active ingredient are provided. The purinylpyridinylamino-2,4-difluorophenyl sulfonamide derivative of the present invention effectively regulates the activity of B-Raf kinase, and thus may be useful for preventing or treating cancers induced by the over-activation of Raf kinase, especially various melanoma, colorectal cancer, prostate cancer, thyroid cancer, ovarian cancer and the like.Type: ApplicationFiled: November 25, 2011Publication date: November 28, 2013Applicant: YOUAI CO., LTD.Inventors: Eun Kyong Shim, Nam Doo Kim, Tae Bo Shim, Seung Yong Kim
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Patent number: 8592432Abstract: The invention provides novel pyrimidine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, c-ros oncogene (ROS), insulin-like growth factor (IGF-1R), and/or insulin receptor (InsR) or a combination thereof.Type: GrantFiled: April 3, 2009Date of Patent: November 26, 2013Inventors: Bei Chen, Tao Jiang, Thomas H. Marsilje, Pierre-Yves Michellys, Truc Ngoc Nguyen, Wei Pei, Baogen Wu, Zhaobo Gao, Yonghui Ge, Chen Huang, Yuncheng Li, Xuefeng Zhu
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Patent number: 8586581Abstract: The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5) and they are therefore useful for the treatment of diseases related to this receptor.Type: GrantFiled: December 10, 2010Date of Patent: November 19, 2013Assignee: Hoffmann-La Roche IncInventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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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: 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