Polycyclo Ring System Having The Additional 1,3-diazine Ring As One Of The Cyclos Patents (Class 514/252.16)
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Publication number: 20140206673Abstract: Provided are compounds of formula (I), wherein X, Y, Z, W, V, R2, R3 and m are defined as in the description. Their pharmaceutical compositions and their uses for treating cancers are also provided.Type: ApplicationFiled: June 18, 2012Publication date: July 24, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Sheldon Cao, Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey O. Saunders, Xuefei Tan, Jeremy Travins, Shunqi Yan, Zhixiong Ye
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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: 20140200207Abstract: Provided herein are Pyrrolopyrimidine Compounds having the following structure: wherein R1, R2, R3, and L are as defined herein, compositions comprising an effective amount of a Pyrrolopyrimidine Compound, and methods for treating or preventing breast cancer, more particularly triple negative breast cancer, comprising administering an effective amount of such Pyrrolopyrimidine Compounds to a subject in need thereof.Type: ApplicationFiled: January 15, 2014Publication date: July 17, 2014Applicant: Signal Pharmaceutical LLCInventors: Andrew Antony Calabrese, Brandon Jeffy, Dale Robinson, Dan Zhu, Dehua Huang, Jan Elsner, John Boylan, Lida Tehrani, Mark A. Nagy, Mehran Fallah Moghaddam, Raj Kumar Raheja, Paul Erdman, Rama K. Narla, Roy L. Harris, Tam Minh Tran, Jennifer Riggs, Yuhong Ning
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Publication number: 20140200206Abstract: Provided herein are Pyrrolopyrimidine Compounds having the following structure: wherein R1, R2, R3, and L are as defined herein, compositions comprising an effective amount of a Pyrrolopyrimidine Compound, and methods for treating or preventing breast cancer, more particularly triple negative breast cancer, comprising administering an effective amount of such Pyrrolopyrimidine Compounds to a subject in need thereof.Type: ApplicationFiled: January 15, 2014Publication date: July 17, 2014Applicant: Signal Pharmaceutical LLCInventors: Andrew Antony Calabrese, Brandon Jeffy, Dale Robinson, Dan Zhu, Dehua Huang, Jan Elsner, John Boylan, Lida Tehrani, Mark A. Nagy, Mehran Fallah Moghaddam, Raj Kumar Raheja, Paul Erdman, Rama K. Narla, Roy L. Harris, Tam Minh Tran, Jennifer Riggs, Yuhong Ning
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Publication number: 20140200219Abstract: The present methods and compositions are of use for treatment of conditions involving fibrosis, such as Peyronie's disease plaque, penile corporal fibrosis, penile veno-occlusive dysfunction, Dupuytren's disease nodules, vaginal fibrosis, clitoral fibrosis, female sexual arousal disorder, abnormal wound healing, keloid formation, general fibrosis of the kidney, bladder, prostate, skin, liver, lung, heart, intestines or any other localized or generalized fibrotic condition, vascular fibrosis, arterial intima hyperplasia, atherosclerosis, arteriosclerosis, restenosis, cardiac hypertrophy, hypertension or any condition characterized by excessive fibroblast or smooth muscle cell proliferation or deposition of collagen and extracellular matrix in the blood vessels and/or heart.Type: ApplicationFiled: March 17, 2014Publication date: July 17, 2014Applicant: Los Angeles Biomedical Research Institute at Harbor-UCLA Medical CenterInventors: Nestor F. Gonzalez-Cadavid, Jacob Rajfer
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Publication number: 20140194417Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: January 8, 2014Publication date: July 10, 2014Applicant: Nimbus Iris, Inc.Inventors: Jeremy Robert Greenwood, Geraldine C. Harriman, Rosana Kapeller-Libermann, Craig E. Masse, Shaughnessy Robinson, Donna L. Romero, Mee Shelley, Ronald T. Wester
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Publication number: 20140194418Abstract: Compounds of formula (I) or pharmaceutical acceptable salts are provided, wherein X1˜X5, R1˜R3, A, B, Z and n are defined in the description. And compositions containing said compounds, and the uses for inhibitors of kinases such as ALK, and the uses for treating cancer thereof are provided.Type: ApplicationFiled: January 20, 2012Publication date: July 10, 2014Applicant: ABBVIE INC.Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Fengchun Wu, Yan Shen, Cuihua Liu, Zhenguang Zou, Marina Pliushchev
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Publication number: 20140194403Abstract: Provided herein are methods for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal, which comprises administering to said mammal in need thereof a therapeutically effective amount of a compound of Formula I: in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification.Type: ApplicationFiled: July 16, 2013Publication date: July 10, 2014Applicant: Array BioPharma Inc.Inventors: Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
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Publication number: 20140194404Abstract: This invention relates to amidopyrazole compounds that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment of cellular proliferative diseases, for example, cancer, hyperplasia, restenosis, cardiac hypertrophy, immune disorders and inflammation.Type: ApplicationFiled: March 21, 2012Publication date: July 10, 2014Inventors: William T. McElroy, Guoqing Li, Ginny Dai Ho, Zheng Tan, Sunil Paliwal, William Michael Seganish, Deen Tulshian, John Lampe, Joey L. Methot, Hua Zhou, Michael D. Altman, Liang Zhu
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Publication number: 20140187562Abstract: The instant invention relates to crystalline forms of MK-1775, an inhibitor of Weel kinase. Specifically, the instant invention relates to hemihydrates of MK-1775.Type: ApplicationFiled: March 6, 2014Publication date: July 3, 2014Inventors: Rositza Petrova, Eric Sirota, Robert Wenslow
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Publication number: 20140179701Abstract: Disclosed is a composition effective in reducing skin wrinkles. The composition comprises or uses a phosphodiesterase 5 (PDE5) inhibitor as an active ingredient. Further disclosed is a method for reducing skin wrinkles using the composition.Type: ApplicationFiled: March 3, 2014Publication date: June 26, 2014Applicant: SK CHEMICALS CO., LTD.Inventors: Soo-Min LEE, Sooheun LEE, Keun-Ho RYU, Bong-Yong LEE, Jae-Sun KIM, Jung-Hoon OH, Ye-Ji JEON
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Publication number: 20140178473Abstract: There is provided a solid dosage form adapted for the release of a biologically active material in the oral cavity wherein the dosage form includes at least one biologically active material, and at least one matrix forming agent, wherein the dosage form substantially dissolves in the oral cavity. A method of producing the same and a kit including the same are also provided.Type: ApplicationFiled: October 11, 2013Publication date: June 26, 2014Applicant: IX BIOPHARMA PTE LTDInventors: Chin Beng Stephen LIM, Vivian Bruce SUNDERLAND, Yip Hang Eddy LEE
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Patent number: 8759326Abstract: Drug combinations which contain a PDE4-inhibitor and a non-steroidal anti-inflammatory drug (NSAID), processes for preparing them, and their use in treating in particular respiratory complaints such as COPD, chronic sinusitis, and asthma. The PDE4 inhibitors of the drug combinations include compounds of general formula 1 wherein X is SO or SO2, but preferably SO, R3 is an optionally substituted, mono- or bicyclic, unsaturated, partly saturated or saturated heterocyclic group or an optionally substituted, mono- or bicyclic heteroaryl, and R1 and R2 have the meanings given in claim 1.Type: GrantFiled: August 15, 2013Date of Patent: June 24, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Peter Nickolaus, Rolf Goeggel, Daniel Peter
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Publication number: 20140171414Abstract: Compounds of formula (I) defined herein exhibit human neutrophil elastase inhibitory properties and are useful for treating diseases and conditions in which HNE is implicated.Type: ApplicationFiled: December 17, 2013Publication date: June 19, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: Lilian ALCARAZ, Robert Andrew Heald, Jonathan Mark Sutton, Elisabetta Armani, Carmelida Capaldi
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Publication number: 20140171405Abstract: The present invention relates to fused pyrazole 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: December 18, 2013Publication date: June 19, 2014Applicant: Incyte CorporationInventors: Jincong Zhuo, Meizhong Xu, Ding-Quan Qian
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Publication number: 20140171431Abstract: The present invention relates to the field of pharmaceutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) and a preparation method thereof, a pharmaceutical composition with the compounds as active components, and a use of the azole compounds and the pharmaceutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as defined in the specification.Type: ApplicationFiled: May 15, 2012Publication date: June 19, 2014Inventors: Jianhua Shen, Yiping Wang, Kai Wang
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Publication number: 20140171429Abstract: The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, Formula (1) wherein R1, R2, R3, X, Y, Z, A, B, G1, m, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.Type: ApplicationFiled: January 20, 2012Publication date: June 19, 2014Applicant: ABBVIE INC.Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Zhongqiang Zhao, Dikun Chai, Leifu Yang, Yingxiang Gao, Marina Pliushchev
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Publication number: 20140171440Abstract: The present invention is directed to methods of enhancing liver repair after injury, resection or transplantation using antagonists of the bone morphogenetic protein (BMP) signaling pathway in the liver.Type: ApplicationFiled: September 3, 2013Publication date: June 19, 2014Applicant: Beth Israel Deaconess Medical Center, Inc.Inventors: Seth J. Karp, Martin Dib, Nhue Do
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Patent number: 8754079Abstract: The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.Type: GrantFiled: February 25, 2011Date of Patent: June 17, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Thorsten Lehmann-Lintz, Armin Heckel, Joerg Kley, Elke Langkopf, Norbert Redemann, Achim Sauer, Leo Thomas, Dieter Wiedenmayer, Matthias Austen, John Danilewicz, Martin Schneider, Kay Schreiter, Phillip Black, Wesley Blackaby, Ian Linney
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Publication number: 20140163000Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as defined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.Type: ApplicationFiled: December 6, 2013Publication date: June 12, 2014Inventors: Nadia Ahmad, Dean Boyall, Jean-Damien Charrier, Chris Davis, Rebecca Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Donald Middleton, Michael O'Donnell, Maninder Panesar, Francoise Pierard, Joanne Pinder, David Shaw, Pierre-Henri Storck, John Studley, Heather Twin
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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: 20140163026Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders or neurofibromatosis. Also described herein are methods of utilizing PAK inhibitors for the treatment of cancer.Type: ApplicationFiled: April 9, 2012Publication date: June 12, 2014Applicant: Afraxis Holdings, Inc.Inventors: David Campbell, Sergio G. Duron
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Publication number: 20140163005Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140163007Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140163004Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140163003Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140163006Abstract: The present invention provides derivatives of pyrido[2,3-d]pyrimidin-7-one. These compounds are kinase inhibitors, including compounds that show anti-proliferative activity, including against tumor cells, and are useful in the treatment of diseases including cancer.Type: ApplicationFiled: July 24, 2013Publication date: June 12, 2014Applicant: Forma Therapeutics, Inc.Inventors: KRISHNA MURTHI, REBECCA CASAUBON, ARTHUR F. KLUGE, CHASE SMITH, JOACHIM VOGT
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Publication number: 20140155397Abstract: EMT signatures and markers useful for characterizing the status of epithelial cancers and for predicting drug responses in patients having non-small cell lung cancer are provided together with methods of using the same.Type: ApplicationFiled: April 2, 2012Publication date: June 5, 2014Applicant: Board of RegentsInventors: John V Heymach, Jing Wang, Lauren Averett Byers, Kevin R. Coombes, John D. Minna, Luc Girard
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Publication number: 20140155372Abstract: The invention provides combinations comprising a) compound of formula I: (formula I), or a pharmaceutically acceptable salt thereof; and another agent selected from GDC-0973, PD-0325901, or a pharmaceutically acceptable salt thereof. The combinations are particularly useful for treating hyperproliferative disorders, such as cancer.Type: ApplicationFiled: March 30, 2012Publication date: June 5, 2014Applicant: GENENTECH, INC.Inventors: Brian Lee, Kui Lin, Michelle Nannini, Elizabeth Punnoose, Deepak Sampath
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Publication number: 20140155389Abstract: The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, wherein R1, X, Y, Z, A, B, G1, and n are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as ALK and methods of treating diseases such as cancer.Type: ApplicationFiled: January 20, 2012Publication date: June 5, 2014Applicant: ABBVIE INC.Inventors: Anil Vasudevan, Thomas Dale Penning, Huanming Chen, Bo Liang, Shaohui Wang, Zhongqiang Zhao, Dikun Chai, Leifu Yang, Yingxiang Gao, Marina Pliushchev
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BRIDGED BICYCLIC ARYL AND BRIDGED BICYCLIC HETEROARYL SUBSTITUTED TRIAZOLES USEFUL AS AXL INHIBITORS
Publication number: 20140155386Abstract: Bridged bicyclic aryl or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: December 2, 2013Publication date: June 5, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Jiaxin Yu, Pingyu Ding, Joane Litvak -
Publication number: 20140148431Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.Type: ApplicationFiled: August 24, 2012Publication date: May 29, 2014Inventors: Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Satish Bhawsar, Sachin Bhagwat, Mohammed Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Sanjeev Joshi
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Publication number: 20140148436Abstract: The present invention provides compounds, including resolved enantiomers, diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula: A-L-CR where CR is a cyclical core group, L is a linking group and A is as defined herein. Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.Type: ApplicationFiled: January 31, 2014Publication date: May 29, 2014Applicant: Array BioPharma, Inc.Inventors: Ian S. Mitchell, Keith L. Spencer, Peter Stengel, Yongxin Han, Nicolas C. Kallan, Mark Munson, Guy P.A. Vigers, James Blake, Anthony Piscopio, John Josey, Scott Miller, Dengming Xiao, Rui Xu, Chang Rao, Bing Wang, April L. Bernacki
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Publication number: 20140148438Abstract: There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.Type: ApplicationFiled: September 22, 2011Publication date: May 29, 2014Inventor: Michael Farber
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Publication number: 20140148460Abstract: The invention relates to a product containing the compound of formula (I) below (I) or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having PDE5-inhibitory properties, or a pharmaceutically acceptable salt thereof, for therapeutic use, simultaneously, separately or over a period of time, in the treatment of a disease wherein vasoconstriction is involved.Type: ApplicationFiled: January 23, 2014Publication date: May 29, 2014Applicant: ACTELION PHARMACEUTICALS LTD.Inventor: Martine CLOZEL
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Publication number: 20140148465Abstract: The invention describes methods and compositions for alleviating medical afflictions for which anxiety may cause or exacerbate the affliction. A subject suffering from the affliction is treated with a combination of a pharmaceutical compound that enhances learning, and a second pharmaceutical recognized to be useful for treatment of the affliction, wherein D-cycloserine is the pharmaceutical compound that enhances learning. Representative afflictions include pain, mood disorders, anxiety disorders including performance anxiety, insomnia, female sexual dysfunction, chronic fatigue, autism spectrum disorders, fibromyalgia, and attention deficit-hyperactivity disorder.Type: ApplicationFiled: January 31, 2014Publication date: May 29, 2014Inventors: Jason P. McDevitt, Michael Davis
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Patent number: 8735386Abstract: Compounds of general formula (I) wherein the groups R1 to R3 and X 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: GrantFiled: July 20, 2011Date of Patent: May 27, 2014Assignee: Boehringer Ingelheim International GmbHInventor: Matthias Treu
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Publication number: 20140142113Abstract: A method of treating inflammatory diseases with Adenosine 2B receptor antagonists in particular with xanthine derived inhibitors. The method involves supplying a therapeutically active amount of the compounds of FIG. 1 and in particular compound 1.Type: ApplicationFiled: November 11, 2013Publication date: May 22, 2014Inventors: Michael W. Burnet, Thomas Stohr, Martin Donsbach
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Publication number: 20140135312Abstract: The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein.Type: ApplicationFiled: January 17, 2014Publication date: May 15, 2014Applicants: Astex Therapeutics Ltd., Novartis AGInventors: Gilbert BESONG, Christopher Thomas Brain, Clinton A. Brooks, Miles Stuart Congreve, Claudio Dagostin, Guo He, Ying Huo, Steven Howard, Yue Ll, Yipin Lu, Paul Mortenston, Troy Smith, Moo Je Sung, Steven Woodhead, Wojciech Wrona, Bharat Lagu
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Publication number: 20140127295Abstract: The present disclosure describes a composition and a kit having a plurality of compounds for use in the treatment of inflammatory joint diseases and chronic inflammatory connective tissue diseases, such as Rheumatoid Arthritis (RA). The disclosure also relates to a process of obtaining the composition and the method of treating diseases by administration of the compositions.Type: ApplicationFiled: March 7, 2012Publication date: May 8, 2014Applicants: Cellworks Group, Inc, Cellworks Research India Private LimitedInventors: Shireen Vali, Robinson Vidva, Prashant Ramachandran Nair, Pradeep Fernandes, Taher Abbasi, Saumya Radhakrishnan
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Publication number: 20140128370Abstract: The invention relates to substituted tetrahydro-pyrido-pyrimidine derivatives of the formula (I), wherein Y, R1, R2 and m are as defined in the description. Such compounds are suitable for the treatment of a disorder or disease which is mediated by the activity of the PI3K enzymes.Type: ApplicationFiled: January 9, 2014Publication date: May 8, 2014Applicant: NOVARTIS AGInventors: Nigel Graham COOKE, Frédéric ZECRI, Nicolas SOLDERMANN, Romain WOLF, Christina HEBACH, Klemens HOEGENAUER, Gregory John HOLLINGWORTH, Anette VON MATT, Ross Sinclair STRANG, Alexander Baxter SMITH, Paulo FERNANDES GOMES DOS SANTOS, Nadege GRAVELEAU, Frank STOWASSER, Nicola TUFILLI
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Publication number: 20140127311Abstract: The present invention provides biocompatible nano-polymer particles which are composed of a biocompatible polymer, a stabilizer and an active agent for the treatment of pulmonary hypertension or erectile dysfunction and which can be used to produce a pharmaceutical preparation for the treatment of pulmonary hypertension or erectile dysfunction. Biocompatible nano-polymer particles of this invention have a diameter ranging from 10 nm to 10 ?m auf, a stabilizing layer thickness between 0 and 50 nm, contain between 0 and 50% of an active agent for the treatment of pulmonary hypertension or erectile dysfunction, are nebulizable and continuously release the active agent over a period of up to 48 hours. Biocompatible nano-polymer particles of this invention can be synthesized for example using the emulsion technique known to the expert with subsequent solvent evaporation or via spray drying.Type: ApplicationFiled: May 23, 2012Publication date: May 8, 2014Applicant: JUSTUS-LIEBIG-UNIVERSITAET GIESSENInventors: Moritz Beck-Broichsitter, Thomas Schmehl, Tobias Gessler, Thomas Kissel
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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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Publication number: 20140128405Abstract: Compositions and methods for enhancing the aesthetic appearance of the lip or lips of a human achieved by applying to the surface of the lip a composition containing a phosphodiesterase inhibitor, preferably a pyrazolopyrimidinone such as sildenafil or its citrate salt.Type: ApplicationFiled: January 15, 2014Publication date: May 8, 2014Inventor: Alex Chervinsky
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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: 20140128399Abstract: Methods and compositions are provided for treating a urinary tract infection (UTI). The methods involve administering to a subject in need thereof a cAMP elevator or agent that mimics cAMP, particularly a labdane diterpene such as forskolin or a derivative or analog thereof in a therapeutically effective amount to treat a UTI. The methods may further include administration of at least one cAMP elevator in combination with one or more additional active compounds from other classes of therapeutic agents, such as antimicrobial agents or cholesterol lowering drugs. Compositions of the invention include pharmaceutical compositions and kits for treating a UTI in a subject in need thereof that include therapeutically effective amounts of at least two cAMP elevators, particularly where one of the cAMP elevators is a labdane diterpene such as forskolin or a derivative or analog thereof.Type: ApplicationFiled: December 6, 2013Publication date: May 8, 2014Applicant: DUKE UNIVERSITYInventors: Soman N. Abraham, Brian L. Bishop, Matthew J. Duncan, K. Ranga Rama Krishnan, Jeongmin Song, Guojie Li, David W. Zaas
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Patent number: 8710061Abstract: The present disclosure provides a series of compounds of the formula (I) which modulate ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: GrantFiled: January 26, 2012Date of Patent: April 29, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Kenneth M. Boy, Jason M. Guernon, John E. Macor, Richard E. Olson, Jianliang Shi, Lorin A. Thompson, III, Yong-Jin Wu, Li Xu, Yunhui Zhang, Dmitry S. Zuev
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Publication number: 20140113909Abstract: A combination of a CDK4/6 inhibitor and an FGFR kinase inhibitor for the treatment of cancer.Type: ApplicationFiled: June 28, 2012Publication date: April 24, 2014Applicant: Novartis AGInventors: Sunkyu Kim, Shivang Doshi, Kristy Hans, Steven Kovats
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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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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