Patents Issued in November 24, 2016
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Publication number: 20160340305Abstract: A method for the direct stereospecific conversion of structurally diverse mono-, di-, tri- and tetra-substituted olefins to N—H, N-alkyl, N-cycloalkyl, or N-aralkyl aziridines using a hydroxylamine amination agent with transition metal catalyst. The method is operationally simple (i.e., one-pot), scalable and fast at ambient temperature.Type: ApplicationFiled: January 3, 2015Publication date: November 24, 2016Inventors: Daniel Halsell ESS, John Russell FALCK, Jawahar Lal JAT, Laszlo URTI
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Publication number: 20160340306Abstract: Disclosed herein are compositions and methods of treating osteroporosis, bone fracture, bone loss, and increasing bone density by administration of compounds of formula (I) or compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier, wherein L1, L2, L4, R1, R4, R5, R6, and s are as defined in the specification.Type: ApplicationFiled: August 2, 2016Publication date: November 24, 2016Inventors: Stephen Douglas Barrett, Fred Lawrence Ciske, Joseph Michael Colombo, Gregory William Endres, Bradlee David Germain, Andriy Kornilov, James Bernard Kramer, Adam Uzieblo, Thomas Allen Owen, James Paul O'Malley
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Publication number: 20160340307Abstract: A method for the manufacture of a 2-hydrocarbyl-3,3-bis(hydroxyaryl)phthalimidine composition comprises: reacting a phthalimide of formula (2) with a phenol of formula (3) I (2) I (3) in the presence of a catalyst and optionally a solvent at an elevated temperature to form the 2-hydrocarbyl-3,3-bis(hydroxyaryl)phthalimidine composition, wherein the 2-hydrocarbyl-3,3-bis(hydroxyaryl)phthalimidine composition comprises a 2-hydrocarbyl-3,3-bis(hydroxyaryl)phthalimidine of formula (1) I (1) wherein in formulas (1), (2) and (3), R1 is hydrogen, C1-6 alkyl, C1-6 alkoxy, or phenyl optionally substituted with 1 to 5 C1-6 alkyls, each occurrence of R2 and R3 is independently a C1-6 alkyl, and p and q are independently 0 to 4.Type: ApplicationFiled: January 14, 2015Publication date: November 24, 2016Inventors: VENKATA RAMANARAYANAN GANAPATHY BHOTLA, BHASKAR REDDY ALURI, S SHUBASHREE
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Publication number: 20160340308Abstract: A compound represented by the general Formula (I) below, or a salt or solvate thereof, which is useful as an ALK inhibitor, and is useful for prophylaxis or treatment of a disease accompanied by abnormality in ALK, for example, cancer, cancer metastasis, depression or cognitive function disorder: (meanings of the symbols that are included in the formula are as given in the specification).Type: ApplicationFiled: July 28, 2016Publication date: November 24, 2016Applicant: Chugai Seiyaku Kabushiki KaishaInventors: Kazutomo Kinoshita, Kohsuke ASOH, Noriyuki FURUICHI, Toshiya ITO, Hatsuo KAWADA, Nobuya ISHll, Hiroshi SAKAMOTO, WooSang HONG, MinJeong PARK, Yoshiyuki ONO, Yasuharu KATO, Kenji MORIKAMI, Takashi EMURA, Nobuhiro OIKAWA
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Publication number: 20160340309Abstract: The invention provides compounds having activity as sodium channel (e.g., NaV1.7) inhibitors that are useful for treating sodium channel-mediated diseases or conditions, such as pain, as well as other diseases and conditions associated with the mediation of sodium channels, and compositions containing such compounds and methods for using such compounds and compositions.Type: ApplicationFiled: May 20, 2016Publication date: November 24, 2016Applicants: GENENTECH, INC., XENON PHARMACEUTICALS INC.Inventors: Sultan CHOWDHURY, Christoph Martin DEHNHARDT, Abid HASAN, Ivan William HEMEON, Qi JIA, Jun LI, Zhiguo LIU, Daniel F. ORTWINE, Brian SAFINA, Daniel SUTHERLIN, Shaoyi SUN, Andrew D. WHITE, Wei GONG, Alla Yurevna ZENOVA, Jiuxiang ZHU
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Publication number: 20160340310Abstract: The present application provides novel pyridine compounds and pharmaceutically acceptable salts or prodrugs thereof. Also provided are methods for preparing these compounds. These compounds are useful in inhibiting CYP17 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 CPY17 activity. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer, such as prostate cancer.Type: ApplicationFiled: November 13, 2013Publication date: November 24, 2016Inventors: Roger A. Smith, Nicholas James Laping, Aranapakam M. Venkatesan, Raghava Reddy Kethiri, Chandregowda Venkateshappa, Bheemashankar Kulkarni, Purushottam Dewang, Rajendra Kristam, Rajesh Devraj
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Publication number: 20160340311Abstract: Methods for the recovery and/or reuse of palladium catalyst after a Suzuki coupling reaction in which two molecules are coupled are described.Type: ApplicationFiled: May 20, 2016Publication date: November 24, 2016Applicant: Dow AgroSciences LLCInventors: Sanjib Biswas, Reetam Chakrabarti, Lauren M. Huffman, Ronald B. Leng, Abraham D. Schuitman, Karin Spiers, Alan L. Stottlemyer, Jeffrey B. Epp
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Publication number: 20160340312Abstract: The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.Type: ApplicationFiled: August 4, 2016Publication date: November 24, 2016Inventors: Xicheng Sun, Jian Qiu, Adam Stout
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Publication number: 20160340313Abstract: Compounds, compositions and methods useful for treating infectious diseases are provided. In particular, 3-aryl quinoline compounds, their synthesis, pharmaceutical compositions thereof and methods of treating infectious diseases such as malaria, are disclosed.Type: ApplicationFiled: December 21, 2015Publication date: November 24, 2016Applicants: Oregon Health & Science University, The United States Government as Represented by the Department of Veterans AffairsInventors: Michael K. Riscoe, Rolf W. Winter, Sovitj Pou, David J. Hinrichs, Jane Xu Kelly, Yuexin Li, Aaron Nilsen
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Publication number: 20160340314Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.Type: ApplicationFiled: August 1, 2016Publication date: November 24, 2016Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
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Publication number: 20160340315Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.Type: ApplicationFiled: February 6, 2015Publication date: November 24, 2016Applicant: Merck Sharp & Dohme Corp.Inventors: Santhosh F. Neelamkavil, Scott D. Edmondson, Zhuyan Guo, Alan W. Hruza, Zahid Hussain, Remond Moningka, Nancy Jo Kevin
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Publication number: 20160340316Abstract: The application is directed to compounds of Formula (I) or (IA) and pharmaceutically acceptable salts and solvates thereof, wherein R1 R2, R3 and G are defined as set forth in the specification. The invention is also directed to use of compounds of Formula (I) or(IA), and the pharmaceutically acceptable salts and solvates thereof, to treat disorders responsive to the modulation of one or more opioid receptors, or as synthetic intermediates. Certain compounds of the present invention are especially useful for treating pain.Type: ApplicationFiled: December 19, 2014Publication date: November 24, 2016Inventors: Jeffrey Lockman, Laykea Tafesse
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Publication number: 20160340317Abstract: The present invention relates to compounds of Formula I, a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).Type: ApplicationFiled: November 4, 2014Publication date: November 24, 2016Applicant: NOVARTIS AGInventors: Donatella CHIANELLI, Xiaodong LIU, Valentina MOLTENI, John NELSON, Jason Thomas ROLAND, Paul Vicent RUCKER, David Charles TULLY
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Publication number: 20160340318Abstract: The present invention relates to 1-(2,5-dioxoimidazolidin-1-y)-3-substituted urea compounds, processes for preparing them, pharmaceutical compositions containing them, their use as pharmaceuticals as modulators of the FPR2 receptor, and to methods of treating inflammatory diseases or conditions in a subject in need thereof by administering the compound(s) or pharmaceutical composition to the subject.Type: ApplicationFiled: January 27, 2015Publication date: November 24, 2016Inventors: Richard L. Beard, Vidyasagar Vuligonda, Thong Huy Vu, Michael E. Garst
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Publication number: 20160340319Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.Type: ApplicationFiled: August 5, 2016Publication date: November 24, 2016Inventors: Christian GNAMM, Thorsten OOST, Stefan PETERS, Holger HOESCH, Uwe Joerg RIES
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Publication number: 20160340320Abstract: The present invention relates to a family of S-substituted quinazoline derivatives that inhibitors of the enzyme phosphodiesterase 7 (PDE7), useful for the treatment or prevention of diseases mediated by said enzyme, especially inflammatory, neurodegenerative, neurological, psychiatric and/or autoimmune diseases.Type: ApplicationFiled: May 17, 2016Publication date: November 24, 2016Inventors: Ana Martinez Gil, Carmen Belen Gil Ayuso-Gontan, Daniel Ignacio Perez Fernandez, Ana Maria Garcia Fernandez
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Publication number: 20160340321Abstract: Compounds represented by Formula I: and/or a pharmaceutically acceptable salts, a prodrug, a solvate and a combination thereof, a pharmaceutical composition including the triazole derivative, and a method of treating a cancer disease in an individual are disclosed.Type: ApplicationFiled: May 18, 2015Publication date: November 24, 2016Inventors: Duen-Ren Hou, Sharada Prasanna Swain
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Publication number: 20160340322Abstract: Disclosed is a novel triazinone compound with an inhibitory activity on a T-type voltage-dependent calcium channel, and is specifically useful for prevention or treatment of pain, chronic kidney disease and atrial fibrillation. A novel triazinone compound of Formula (I), wherein each substituent in the formula is defined in detail in the description, R4 means a hydrogen atom, or a C1-6 alkoxy group, etc., L1 and L2 each independently mean a single bond, or NR2, etc., L3 means a C1-6 alkylene group, etc., A means a C6-14 aryl group or a 5 to 10-membered heteroaryl group which may be substituted, B means a C3-11 cycloalkylene group, etc., D means a C6-14 aryl amino group or a 5 to 10-membered heteroaryl group which may be substituted, etc., a tautomer of the compound, a pharmaceutically acceptable salt of the compound, or a solvate of the compound, the tautomer, or the pharmaceutically acceptable salt.Type: ApplicationFiled: December 17, 2014Publication date: November 24, 2016Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Michiaki ADACHI, Masataka MINAMI, Jun EGI, Yuichi HIRAI, Toshimasa IWAMOTO, Yusuke SHINTANI, Takuya OKADA, Daiki TAKAHASHI
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Publication number: 20160340323Abstract: Novel azaquinazoline carboxamide derivatives of formula (I) wherein W1, W2, W3, W4, R1, R2, R3 and m which are defined above, are p70S6K inhibitor, and can be employed, inter alia, for the treatment of hyperproliferative disorders.Type: ApplicationFiled: August 3, 2016Publication date: November 24, 2016Inventors: Bayard R. HUCK, Ruoxi LAN, Justin POTNICK, Lizbeth Celeste DESELM, Mark W. CRONIN, JR., Constantin NEAGU, Xiaoling CHEN, Roch BOIVIN, Theresa L. JOHNSON, Andreas GOUTOPOULOS
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Publication number: 20160340324Abstract: Embodiments provided herein relate to methods and compositions for treating cancer. Some embodiments relate to certain compounds having activity against retinoid X receptor-alpha (RXR?). Some embodiments included designing or identifying a compound that binds to human RXRa protein, such as the ligand binding domain (LBD) of human RXRa protein.Type: ApplicationFiled: December 22, 2014Publication date: November 24, 2016Inventors: Ying SU, Xiao-kun ZHANG
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Publication number: 20160340325Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.Type: ApplicationFiled: May 20, 2016Publication date: November 24, 2016Applicant: President and Fellows of Harvard CollegeInventors: Andrew G. Myers, Mark G. Charest, Christian D. Lerner, Jason D. Brubaker, Dionicio R. Siegel
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Publication number: 20160340326Abstract: The invention relates to a tizoxanide carbamate compound of Formula I and a pharmaceutically acceptable salt, a hydrate or a solvate thereof, and their pharmaceutical use.Type: ApplicationFiled: July 4, 2014Publication date: November 24, 2016Applicant: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. ChinaInventors: Song LI, Xingzhou LI, Wu ZHONG, Zhibing ZHENG, Junhai XIAO, Xinbo ZHOU, Yunde XIE, Xiaokui WANG, Lili WANG, Wei CHEN, Fei XIE
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Publication number: 20160340327Abstract: The present invention provides a process for preparing amorphous Cabazitaxel from the solvate form of Cabazitaxel. The present invention also provides novel diisopropyl ether solvate form of Cabazitaxel (I), and process for preparation thereof. Said amorphous Cabazitaxel and crystalline diisopropyl ether solvate of Cabazitaxel of the present invention can be utilized in preparing the pharmaceutical composition/s useful in the treatment of cancer.Type: ApplicationFiled: June 18, 2016Publication date: November 24, 2016Applicant: SHILPA MEDICARE LIMITEDInventors: SRIRAM RAMPALLI, PRASHANT PUROHIT, PRADEEP POTHANA, ANAND KUMAR DUNGA, AKSHAY KANT CHATURVEDI
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Publication number: 20160340328Abstract: Disclosed are compounds having the formula: wherein R1, R2 and R3 are as defined herein, and methods of making and using the same, including use as inhibitors of BMP1, TLL1 and/or TLL2 and in treatment of diseases associated with BMP1, TLL1 and/or TLL2 activity.Type: ApplicationFiled: January 9, 2015Publication date: November 24, 2016Inventors: Sarah E. DOWDELL, Hilary Schenck EIDAM, Mark ELBAN, Ryan Michael FOX, Marlys HAMMOND, Mark A. HILFIKER, Tram H. HOANG, Lara KALLANDER, Brian Griffin LAWHORN, Sharada MANNS, Joanne PHILP, David G. WASHBURN, Guosen YE
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Publication number: 20160340329Abstract: The present invention relates broadly to anti-cancer agents. In particular, the present invention relates to selected benzopyran compounds, the preparation thereof, and their use in methods for treating cancer and reducing the incidence or risk of cancer recurrence.Type: ApplicationFiled: February 5, 2015Publication date: November 24, 2016Inventors: Andrew Heaton, David Brown, Graham Kelly
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Publication number: 20160340330Abstract: The present invention provides NO-releasing nitrooxy-alkylenyl-linked-chromene conjugates, having the structure of Formula (1) wherein R1, R2, R3, R4, X, and L are as defined in the detailed description; pharmaceutical compositions comprising at least one compound o Formula (I); and methods useful for healing wounds, preventing and treating cancer and treating actinic keratosis, cystic fibrosis, and acne, using a compound of Formula (1).Type: ApplicationFiled: January 14, 2015Publication date: November 24, 2016Inventors: JOHN J. TALLEY, EDUARDO J. MARTINEZ
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Publication number: 20160340331Abstract: A compound inhibiting Hsp90 and a pharmaceutical composition including the same as an active ingredient are described, which compound is represented by formula 2 and suppresses the expression of Hsp90, inhibits the accumulation of HIF-1?, the Hsp90 client protein, and efficiently inhibits the activation of VEGF. The compound displays low cytotoxicity and can be effectively used as an active ingredient of an anti-cancer agent, a diabetic retinopathy treating agent, and an anti-arthritic agent.Type: ApplicationFiled: July 22, 2016Publication date: November 24, 2016Applicant: SNU R&DB FOUNDATIONInventors: Young-Ger SUH, Hongchan AN, Seungbeom LEE, Kyu-Won KIM, Ho-Young LEE, Sang Geon KIM, Jeong Hun KIM
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Publication number: 20160340332Abstract: In one embodiment, the present application discloses mixtures comprising (a) water in an amount of at least 1% wt/wt of the mixture; (b) a transition metal catalyst; and (c) one or more solubilizing agents; and methods for using such mixtures for performing transition metal mediated bond formation reactions.Type: ApplicationFiled: May 27, 2016Publication date: November 24, 2016Inventor: Volker Berl
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Publication number: 20160340333Abstract: Provided is a novel process for the preparation of alogliptin.Type: ApplicationFiled: May 20, 2014Publication date: November 24, 2016Inventors: Navin Ganesh Bhatt, Samir Naik, Ajay Kumar Sharma, Mahendra Joma Choraghe, Shekhar Bhaskar Bhirud
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Publication number: 20160340334Abstract: Described herein are methods to purify alkaloids and amino acids. Also described are compositions and methods to treat or prevent a disease using the purified amino acids and alkaloids. The composition can be, for example, formulated into a beverage, a supplement, or formulated for use in e-cigarettes. Also described are methods of treating a disease such as Parkinson's Disease, Alzheimer's Disease, ADHD, ADD, vascular disorders, cancer, heart disorders, migraine headaches, cluster headaches, plaque reduction or aging using one or more of the purified alkaloids or amino acids.Type: ApplicationFiled: June 28, 2016Publication date: November 24, 2016Inventor: Joseph Robert Knight
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Publication number: 20160340335Abstract: Provided are methods for using bis-quaternary ammonium compounds to treat inflammatory pain, neuropathic pain and nociceptive pain.Type: ApplicationFiled: September 6, 2013Publication date: November 24, 2016Applicants: University of Utah, University of Kentucky Research FoundationInventors: Joseph R. HOLTMAN, Peter Anthony CROOKS, Linda P. DWOSKIN, J. Michael MCINTOSH, Elzbieta Pogonowska WALA
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Publication number: 20160340336Abstract: Compounds of Formula I and Formula II, pharmaceutically acceptable salt thereof, stereoisomers of any of the foregoing, or mixtures thereof are agonists of the APJ Receptor and have use in treating cardiovascular and other conditions. Compounds of Formula I and Formula II have the following structures: where the definitions of the variables are provided herein.Type: ApplicationFiled: May 18, 2016Publication date: November 24, 2016Inventors: Ning Chen, Xiaoqi Chen, Yinhong Chen, Alan C. Cheng, Richard V. Connors, Jeffrey Deignan, Paul John Dransfield, Xiaohui Du, Zice Fu, Julie Anne Heath, Daniel B. Horne, Jonathan Houze, Matthew R. Kaller, Aarif Yusuf Khakoo, David John Kopecky, Su-Jen Lai, Zhihua Ma, Lawrence R. McGee, Julio C. Medina, Jeffrey T. Mihalic, Nobuko Nishimura, Steven H. Olson, Vatee Pattaropong, Gayathri Swaminath, Xiaodong Wang, Kevin Yang, Wen-Chen Yeh, Mikkel V. Debenedetto, Robert P. Farrell, Simon J. Hedley, Ted C. Judd, Frank Kayser
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Publication number: 20160340337Abstract: Benzoimidazol-2-yl pyrimidines, purification methods for the same, and pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritus.Type: ApplicationFiled: August 3, 2016Publication date: November 24, 2016Inventors: Matteo Conza, Magali B. Hickey, Stefan Horns, Susanne Lochner
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Publication number: 20160340338Abstract: The meglumine salt of 1-(5,6-dichloro-1H-benzo[d]imidazol-2-yl)-1H-pyrazole-4-carboxylic acid (compound (1)) and pharmaceutically acceptable formulations thereof are described. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by prolyl hydroxylase activity.Type: ApplicationFiled: January 18, 2016Publication date: November 24, 2016Inventors: Kia Sepassi, Michele C. Rizzolio
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Publication number: 20160340339Abstract: The present invention encompasses compounds of the formula (I) wherein the groups R1, Cy, and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.Type: ApplicationFiled: January 23, 2015Publication date: November 24, 2016Inventors: Joerg BENTZIEN, Angela Kay BERRY, Todd BOSANAC, Michael Jason BURKE, Darren Todd DISALVO, Can MAO, Wang MAO, Yue SHEN
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Publication number: 20160340340Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein each Y1, Y2, Y3, Y4, Z, R2, m and R3 are as defined in the disclosure. Also disclosed are compositions containing a compound of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: December 9, 2014Publication date: November 24, 2016Inventors: Paula Louise Sharpe, Thomas Martin Stevenson, Nicholas Ryan Deprez, Ravisekhara P. Reddy, Srinivas Chittaboina
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Publication number: 20160340341Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: April 20, 2016Publication date: November 24, 2016Applicant: Vertex Pharmaceuticals IncorporatedInventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steve M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux, Jinwang Xu, Kevin Michael Cottrell, Mark A. Morris, Nathan D. Waal, John J. Court, Wenxin Gu, Hongbo Deng
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Publication number: 20160340342Abstract: The invention relates to compounds of formula (I), or a pharmaceutically acceptable salt thereof: which possess inhibitory activity against activating mutant forms of EGFR, and are accordingly useful for their anti-cancer activity and in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of the compounds, or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.Type: ApplicationFiled: May 24, 2016Publication date: November 24, 2016Applicant: AstraZeneca ABInventors: David Yunzhi LI, Jiabing WANG, Zhenfan YANG, Qingbei ZENG, Xiaolin ZHANG
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Publication number: 20160340343Abstract: There are provided compounds of formula I, wherein R1 to R5, X1, X2, Ar, L, E, A, A1, G and G1 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.Type: ApplicationFiled: August 1, 2016Publication date: November 24, 2016Inventors: Matthew Colin Thor FYFE, Premji MEGHANI, Matthew Alexander Henry STENT, Stephen Malcolm THOM, Claire Anne WALSHE
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Publication number: 20160340344Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, solvates thereof, wherein R and R? are, each independently, —CR1R2R3, aryl, heteroaryl or heteroC4-6cycloalkyl, whereby aryl and heteroaryl may optionally be substituted with 1 or 2 substituents selected from halo and methyl. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.Type: ApplicationFiled: August 4, 2016Publication date: November 24, 2016Inventors: Koen Vandyck, Stefaan Julien Last, Ioannis Nicolaos Houpis, Pierre Jean-Marie Bernard Raboisson
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Publication number: 20160340345Abstract: The present disclosure provides processes for the preparation of a compound of formula I: which is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula I.Type: ApplicationFiled: August 4, 2016Publication date: November 24, 2016Inventors: Robert William Scott, Justin Philip Vitale, Kenneth Stanley Matthews, Martin Gerald Teresk, Alexandra Formella, Jared Wayne Evans
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Publication number: 20160340346Abstract: Disclosed herein are analogues of itraconazole that are both angiogenesis and hedgehog signaling pathway inhibitors. The compounds are expected to be useful in the treatment of cancer, particularly cancers that are dependent upon the hedgehog signaling pathway such as basal cell carcinoma and medulloblastoma.Type: ApplicationFiled: August 1, 2016Publication date: November 24, 2016Inventors: MATTHEW KYLE HADDEN, UPASANA BANERJEE
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Publication number: 20160340347Abstract: This invention provides well defined 6-alkyl or hydroxyalkyl-1-naphthamide or quinoline compounds for treating glaucoma or ocular hypertension.Type: ApplicationFiled: December 20, 2013Publication date: November 24, 2016Applicant: Allergan, Inc.Inventor: David W. Old
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Publication number: 20160340348Abstract: The invention relates generally to muscarinic agonists, which are useful for stimulating muscarine receptors, and treating cognitive disorders. Included among the muscarinic agonists disclosed herein are oxadiazole derivatives, compositions, and preparations thereof. Methods of synthesizing oxadiazole compounds also are provided. This disclosure also relates in part to compositions for enhancing cognitive function in subjects such as humans, the compositions comprising a muscarinic agonist or a pharmaceutically suitable form thereof. This disclosure relates in part to methods of treating animals such as humans by administering such compositions.Type: ApplicationFiled: July 29, 2016Publication date: November 24, 2016Inventors: Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson, Michael L. Hendrickson, Jeffrey C. Ockuly, Trevor M. Twose, Melinda L. Verdone
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Publication number: 20160340349Abstract: General formula (I): The present invention pertains to: a pyridone derivate or a salt thereof represented by general formula (I); or a medicine containing the pyridone derivative or salt thereof as an active ingredient. [In the formula, ring A, R1, R2, R3 and R4 are specific groups.Type: ApplicationFiled: August 9, 2016Publication date: November 24, 2016Applicant: KAKEN PHARMACEUTICAL CO., LTD.Inventors: Noriyuki KAMEI, Yoshitake SUMIKAWA, Daigo KAMIMURA, Shingo TODO, Takuya YAMADA, Shota TOKUOKA
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Publication number: 20160340350Abstract: The present invention provides a method for physically separating the active pharmaceutical ingredient (API) from the excipients in a pharmaceutical formulation before the API is fully characterized by standard techniques. The presently disclosed method is based on making use of the difference in density of the API and that of the excipients. In the method, the API is not dissolved, nor is the crystal form of the API changed.Type: ApplicationFiled: April 25, 2016Publication date: November 24, 2016Applicant: The Curators of the University of MissouriInventor: Jerry L. Atwood
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Publication number: 20160340351Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring B, and the subscript r are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk).Type: ApplicationFiled: December 18, 2014Publication date: November 24, 2016Inventors: Brian M. Andresen, Kenneth L. Arrington, Ryan D. Otte, John Michael Ellis, John W. Butcher, Alan B. Northrup, Joel S. Robichaud, Jacques Yves Gauthier, Jean-Francois Fournier
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Publication number: 20160340352Abstract: Provided are a compound represented by formula (I) or (II), a salt thereof, or solvates of the compound and salt, having an analgesic effect and high metabolic stability. Further provided are the following: an analgesic obtained from the compound, a salt thereof, or solvates of the compound and salt; a pharmaceutical composition containing the compound, a salt thereof, or solvates of the compound and salt; an analgesic treatment method using the compound, a salt thereof, or solvates of the compound and salt; and a use of the compound, a salt thereof, or solvates of the compound and salt, in the production of an analgesic composition.Type: ApplicationFiled: October 28, 2014Publication date: November 24, 2016Inventor: Hiromitsu TAKAYAMA
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Publication number: 20160340353Abstract: Provided is a novel compound having a selective JAK3-inhibitory effect and also having excellent oral absorbability. Also provided is a pharmaceutical agent, which is based on a JAK3-inhibitory effect and is useful for preventing and/or treating a disease involving the JAK3, and in particular, rheumatoid arthritis or multiple sclerosis. An azaindole derivative having a cycloalkenyl group, which is represented by the following formula (I), or a salt thereof, and a pharmaceutical composition containing the same: where R1 to R4, m and n have the same meanings as those defined in the description.Type: ApplicationFiled: February 4, 2015Publication date: November 24, 2016Applicant: TAIHO PHARMARCEUTICAL CO., LTD.Inventors: Masayuki NAKAMURA, Hiroyoshi YAMANAKA, Kazuaki SHIBATA, Morihiro MITSUYA, Takafumi HARADA
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Publication number: 20160340354Abstract: Compounds that selectively inhibit pathological production of human vascular endothelial growth factor (VEGF) and compositions comprising such Compounds are described. Compounds that inhibit viral replication or the production of viral RNA or DNA or viral protein and compositions comprising such Compounds are described. Also described are methods of reducing VEGF using such Compounds and methods for treating cancer and non-neoplastic conditions involving the administration of such Compounds. Further described are methods of inhibiting viral replication or the production of viral RNA or DNA or viral protein using such Compounds and methods for treating viral infections involving the administration of such Compounds. The Compounds may be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatments.Type: ApplicationFiled: April 20, 2016Publication date: November 24, 2016Inventors: THOMAS W. DAVIS, MARLA L. WEETALL
