Plural Ring Oxygens In The Tricyclo Ring System Patents (Class 546/90)
  • Patent number: 9328093
    Abstract: The present invention concerns the discovery of new selective inhibitors of ubiquitin specific proteases, their process of preparation and their therapeutic use.
    Type: Grant
    Filed: September 17, 2014
    Date of Patent: May 3, 2016
    Assignee: HYBRIGENICS SA
    Inventors: Roman Lopez, Frederic Colland
  • Patent number: 9175003
    Abstract: The present invention relates to substituted azoanthracene derivatives and intermediates for the preparation thereof. The substituted azoanthracene derivatives and associated intermediates may be useful for the preparation of pharmaceutical compositions for the treatment or prevention of diseases, disorders, and conditions wherein modulation of the human GLP-1 receptor is beneficial.
    Type: Grant
    Filed: January 23, 2015
    Date of Patent: November 3, 2015
    Assignee: vTv Therapeutics LLC
    Inventors: Adnan M. M. Mjalli, Christopher Behme, Daniel P. Christen, Devi Reddy Gohimukkula, Dharma Rao Polisetti, James C. Quada, Jr., Jennifer L. R. Freeman, Muralidhar Bondlela, Mustafa Guzel, Ravindra Reddy Yarragunta, Robert Carl Andrews, Santhosh Kalpathy, Stephen Thomas Davis, Thomas Scott Yokum
  • Publication number: 20150148538
    Abstract: The present invention relates to the use of new chemical substances, the levogyre and dextrogyre enantiomers of (AMINO-7 TRIETHOXY-4,5,6 OXO-1 DIHYDRO-1,3 ISOBENZOFURANNYL-3)-1 METHOXY-8 METHYL-2METHYLENEDIOXY-6,7 TETRAHYDRO-,2,3,4 ISOQUINOLEINE or tritoqualine, to treat acute myeloid or lymphoid leukemia, with the exception of type B leukemia.
    Type: Application
    Filed: November 28, 2014
    Publication date: May 28, 2015
    Inventor: Gaetan TERRASSE
  • Publication number: 20150148539
    Abstract: The present invention relates to substituted azoanthracene derivatives and intermediates for the preparation thereof. The substituted azoanthracene derivatives and associated intermediates may be useful for the preparation of pharmaceutical compositions for the treatment or prevention of diseases, disorders, and conditions wherein modulation of the human GLP-1 receptor is beneficial.
    Type: Application
    Filed: January 23, 2015
    Publication date: May 28, 2015
    Inventors: Adnan M.M. Mjalli, Christopher Behme, Daniel P. Christen, Devi Reddy Gohimukkula, Dharma Rao Polisetti, James C. Quada, JR., Jennifer L.R. Freeman, Muralidhar Bondlela, Mustafa Guzel, Ravindra Reddy Yarragunta, Robert Carl Andrews, Santhosh Kalpathy, Stephen Thomas Davis, Thomas Scott Yokum
  • Publication number: 20150133666
    Abstract: The present invention relates to the use of a histamine H4 agonist molecule, the enantiomers of the (AMINO-7 TRIETHOXY-4,5,6 OXO-1 DIHYDRO-1,3 ISOBENZOFURANNYL-3)-1METHOXY-8 METHYL-2 METHYLENEDIOXY-6,7 TETRAHYDRO-,2,3,4 ISOQUINOLINE or tritoqualine for the treatment of respiratory impairment caused by cystic fibrosis and the reduction and prevention of bronchial superinfections.
    Type: Application
    Filed: May 21, 2013
    Publication date: May 14, 2015
    Inventor: Gaetan Terrasse
  • Patent number: 8987295
    Abstract: The present invention is directed to substituted azoanthracene derivatives or pharmaceutically acceptable salts thereof that modulate the human GLP-1 receptor and that may be useful in the treatment of diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial, such as diabetes mellitus type 2. The invention is also directed to pharmaceutical compositions comprising these compounds and to the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: March 24, 2015
    Assignee: TransTech Pharma, LLC
    Inventors: Adnan M. M. Mjalli, Christopher Behme, Daniel P. Christen, Devi Reddy Gohimukkula, Dharma Rao Polisetti, James C. Quada, Jr., Jennifer L. R. Freeman, Kalpathy Santhosh, Muralidhar Bondlela, Mustafa Guzel, Ravindra Reddy Yarragunta, Robert Carl Andrews, Stephen Thomas Davis, Thomas Scott Yokum
  • Publication number: 20150051393
    Abstract: A pseudorotaxane, a rotaxane and a catenane are provided. The pseudorotaxane includes at least a macrocyclic host molecule, a guest molecule, and a metal ion. The host molecule contains at least a binding unit and an aromatic linking spacer. The guest molecule has at least a recognition unit. The metal ion is used to template the threading of the guest molecule through the macrocycle host molecule by coordinating to a binding pocket formed from the binding unit of the macrocycle and the recognition moiety of the guest molecule. Rotaxanes or catenanes can be synthesized from the pseudorotaxane complexes, with or without the metal template ion in their molecular structures.
    Type: Application
    Filed: October 28, 2014
    Publication date: February 19, 2015
    Inventors: Sheng-Hsien CHIU, You-Han LIN
  • Publication number: 20140371259
    Abstract: A method for treating a neoplasm in a subject, comprising co-administering to the subject a therapeutically effective amount of an anticancer agent and a substituted 6,7-methylenedioxy-4-amino-quinoline, or a pharmaceutically acceptable salt or ester thereof.
    Type: Application
    Filed: January 29, 2013
    Publication date: December 18, 2014
    Applicant: University of Pittsburgh - Of the Commonwealth System of Higher Education
    Inventors: Barry I. Gold, Xiangqun Xie, Ajay Srinivasan, LiRong Wang
  • Patent number: 8889705
    Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are noscapine analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers. While the antitussive plant alkaloid, noscapine, binds tubulin, displays anticancer activity, and has a safe pharmacological profile in humans, structure-function analyzes pointed to a proton at position 9 of the isoquinoline ring that can be modified without compromising tubulin binding activity. Noscapine analogs with various functional moieties at position 9 on the isoquinoline ring kill human cancer cells resistant to other anti-microtubule agents, such as vincas and taxanes.
    Type: Grant
    Filed: June 5, 2012
    Date of Patent: November 18, 2014
    Assignee: Emory University
    Inventors: Harish C. Joshi, Ritu Aneja, Surya N. Vangapandu
  • Publication number: 20140309253
    Abstract: The invention relates to compounds of the formula wherein R?, R1 through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
    Type: Application
    Filed: June 25, 2014
    Publication date: October 16, 2014
    Inventors: Bertrand Leblond, Cedric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Desire, Matthew P. Pando, John E. Donello, Rong Yang
  • Publication number: 20140275529
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.
    Type: Application
    Filed: June 2, 2014
    Publication date: September 18, 2014
    Inventors: Stephen F. Traynelis, Dennis C. Liotta, Rose M. Santangelo, Ethel C. Garnier
  • Publication number: 20140249312
    Abstract: The present invention relates generally to [1,3]dioxolo[4,5-g]quinoline-6(5H)thione and [1,3]dioxolo[4,5-g][1,2,4]triazolo[1,5-a]quinoline derivatives and/or compositions for use in inhibiting, preventing and/or treating cancer, e.g. hepatocellular carcionoma (HCC). In some embodiments, the invention relates to the use of small-molecule compounds to inhibit, prevent and/or treat expression of the transcription factor Late SV40 Factor (LSF) for treatment of HCC or other cancer types.
    Type: Application
    Filed: October 12, 2012
    Publication date: September 4, 2014
    Applicant: TRUSTEES OF BOSTON UNIVERSITY
    Inventors: Scott E. Schaus, Ulla Hansen, Joshua A. Bishop
  • Patent number: 8822462
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.
    Type: Grant
    Filed: January 28, 2010
    Date of Patent: September 2, 2014
    Assignee: Emory University
    Inventors: Stephen F. Traynelis, Dennis C. Liotta, Rose M. Santangelo, Ethel C. Garnier
  • Patent number: 8802444
    Abstract: A “real time” method for detecting chemical agents generally and particularly electrophilic and nucleophilic species by employing tunable, precursor sensor materials that mimic the physiological interaction of these agents to form highly florescent berberine-type alkaloids that can be easily and rapidly detected. These novel precursor sensor materials can be tuned for reaction with both electrophilic (chemical species, toxins) and nucleophilic (proteins and other biological molecules) species. By bonding or otherwise attaching these precursor molecules to a surface or substrate they can be used in numerous applications.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: August 12, 2014
    Assignee: Sandia Corporation
    Inventors: James R. McElhanon, Timothy J. Shepodd
  • Publication number: 20140221371
    Abstract: The invention relates to compounds of general formula (I), corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof and the prodrugs of said compounds. The invention also relates to the use of said compounds as binding partners for 5-HT5 receptors for treating diseases that are modulated by a 5-HT5 receptor activity, in particular, for treating neurodegenerative and neuropsychiatric disorders as well as signs, symptoms and dysfunctions.
    Type: Application
    Filed: December 23, 2013
    Publication date: August 7, 2014
    Inventors: Wilhelm Amberg, Astrid Netz, Andreas Kling, Michael Ochse, Udo Lange, Charles W. Hutchins, Franciso Javier Garcia-Ladona, Wolfgang Wernet
  • Patent number: 8772316
    Abstract: The invention relates to compounds of the formula wherein R?, R1, through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
    Type: Grant
    Filed: February 17, 2012
    Date of Patent: July 8, 2014
    Assignees: Allergan, Inc., Exonhit Therapeutics SA
    Inventors: Bertrand Leblond, John E. Donello, Cédric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Désiré, Matthew P. Pando, Rong Yang
  • Publication number: 20140142134
    Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Psendomonas spp., Yersinia spp., en tero pathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.
    Type: Application
    Filed: July 13, 2012
    Publication date: May 22, 2014
    Applicant: MICROBIOTIX, INC.
    Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams, Matthew Torhan
  • Publication number: 20140121233
    Abstract: Compound of Formula (I) and use thereof as microtubule modulating agents in the treatment of cancer are described herein.
    Type: Application
    Filed: June 11, 2012
    Publication date: May 1, 2014
    Applicant: GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.
    Inventors: Ritu Aneja, Ram Chandra Mishra
  • Publication number: 20140121231
    Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt thereof wherein X, M, Y, R1 and R2 are as defined herein. The compounds have activity as anticancer agents.
    Type: Application
    Filed: June 19, 2013
    Publication date: May 1, 2014
    Inventors: David Robert Bolin, Javier de Vicente Fidalgo, Johannes Hermann, Parcharee Tivitmahaisoon, Lin Yi, Mark Zak
  • Publication number: 20140113928
    Abstract: Methods and compositions for enhancing fertility and/or inhibiting pregnancy failure, restoring glucose tolerance and/or preventing glucose intolerance and/or maintaining glucose homeostasis and/or inducing or enhancing weight loss, treating dyslipidemia, treating hypertestosteronism or hyperandrogenism, and/or treating type 2 diabetes in an individual in need thereof are provided. These involve compositions that inhibit expression of interferon-gamma (IFN-?) or a downstream IFN-?-stimulated gene, which is preferably a macrolide immunosuppressant compound.
    Type: Application
    Filed: May 31, 2012
    Publication date: April 24, 2014
    Applicant: QUEEN'S UNIVERSITY AT KINGSTON
    Inventors: Ahmad J.H. Albaghdadi, Frederick W.K. Kan
  • Publication number: 20140018384
    Abstract: There is provided compounds of formula I, wherein X1 to X4, R1 to R4, Y1, Y2 and L are as defined in the description, and pharmaceutically-acceptable salts thereof, which may be useful in the treatment and/or prophylaxis of autoimmune diseases, inflammatory (e.g. chronic inflammatory) diseases and/or other diseases that may benefit from production of ROS (reactive oxygen species) by a NADPH oxidase complex.
    Type: Application
    Filed: March 16, 2012
    Publication date: January 16, 2014
    Applicant: PRONOXIS AB
    Inventors: Karl Fredrik Wallner, Jan Peter Olofsson, Malin Kristin Hultqvist, Benjamin Harry Pelcman
  • Publication number: 20140011796
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: September 12, 2013
    Publication date: January 9, 2014
    Applicant: AMGEN INC.
    Inventors: Michael David BARTBERGER, Ana Gonzalez Buenrostro, Hilary Plake Beck, Xiaoqi Chen, Richard Victor Connors, Jeffrey Deignan, Jason Duquette, John Eksterwicz, Benjamin Fisher, Brian Matthew Fox, Jiasheng Fu, Zice Fu, Felix Gonzalez Lopez De Turiso, Michael William Gribble, Dann James Gustin, Julie Anne Heath, Xin Huang, Xianyun Jiao, Michael Johnson, Frank Kayser, David John Kopecky, Sujen Lai, Yihong Li, Zhihong Li, Jiwen Liu, Jonathan Dante Low, Brian Stuart Lucas, Zhihua Ma, Lawrence R. McGee, Joel McIntosh, Dustin McMinn, Julio Cesar Medina, Jeffrey Thomas Mihalic, Steven Howard Olson, Yosup Rew, Philip Marley Roveto, Daqing Sun, Xiaodong Wang, Yingcai Wang, Xuelei Yan, Ming Yu, Jiang Zhu
  • Publication number: 20130324570
    Abstract: The present invention is directed to methods, compositions and kits for treatment of cancer, e.g. heptacellular carcinoma. In some embodiments, the present invention discloses the use of a small-molecule compound of formulas (I)-(XXVI) as disclosed herein to inhibit transcription factor Late SV40 Factor (LSF) for treatment of cancer, e.g., HCC.
    Type: Application
    Filed: September 30, 2011
    Publication date: December 5, 2013
    Applicant: TRUSTEES OF BOSTON UNIVERSITY
    Inventors: Ulla Hansen, Scott Schaus, Trevor Grant, Joshua Bishop, John Kavouris, Lisa M. Christadore
  • Publication number: 20130296572
    Abstract: A method for preparing temsirolimus, the method including: using a substituted aromatic aldehyde to protect 2,2-dimethylol propionic acid to produce intermediate II; carrying out reaction between the intermediate II and 2,4,6-trichlorobenzoyl chloride; carrying out condensation reaction between a resulting product and rapamycin to produce intermediate III; and finally using sulfuric acid to remove a protecting group from the intermediate III to yield temsirolimus.
    Type: Application
    Filed: July 3, 2013
    Publication date: November 7, 2013
    Inventors: Honghai SONG, Long TANG, Wei CHEN, Zheng LI, Jinzhou LI, Zhicun SUN, Jiajin FENG
  • Publication number: 20130274280
    Abstract: This invention provides an oral pharmaceutical composition comprising a physiologically tolerable gelled oil-in-water emulsion containing a drug of abuse.
    Type: Application
    Filed: April 11, 2011
    Publication date: October 17, 2013
    Applicant: AYANDA GROUP AS
    Inventors: Kurt Ingar Draget, Ingvild Johanne Haug, Steinar Johan Engelsen, Tore Seternes, Magnus N. Hattrem
  • Patent number: 8552194
    Abstract: Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of quinoline-3-carboxamide derivatives such as laquinimod, or a pharmaceutically acceptable salt thereof, in high yield and purity.
    Type: Grant
    Filed: April 27, 2009
    Date of Patent: October 8, 2013
    Assignee: Actavis Group PTC EHF
    Inventors: Girish Dixit, Krishnadatt Sharma, Kundan Singh Shekhawat, Nitin Sharadchandra Pradhan, Jon Valgeirsson
  • Publication number: 20130252999
    Abstract: 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120(Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and N,N-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.
    Type: Application
    Filed: May 13, 2013
    Publication date: September 26, 2013
    Applicant: China Medical University
    Inventors: Sheng-Chu KUO, Che-Ming Teng, Kuo-Hsiung Lee, Li-Jiau Huang, Li-Chen Chou, Chih-Shiang Chang, Chung-Ming Sun, Tian-Shung Wu, Shiow-Lin Pan, Tzong-Der Way, Jang-Chang Lee, Jing-Gung Chung, Jai-Sing Yang, Chien-Ting Chen, Ching-Che Huang, Shih-Ming Huang
  • Publication number: 20130230559
    Abstract: The present invention relates to novel tacrolimus analogues, a composition for the prevention or treatment of neurological diseases or immune hypersensitivity disorders comprising the same, a method for preventing or treating neurological diseases or immune hypersensitivity disorders comprising administering the analogues to a subject, a method for preparing the analogues using an isolated modified Streptomyces sp. strain wherein the activity of one or more enzymes selected from the group consisting of TcsA, TcsB, TcsC and TcsD is reduced; and the isolated modified Streptomyces sp. strain for prepare the analogues.
    Type: Application
    Filed: February 22, 2013
    Publication date: September 5, 2013
    Applicant: EWHA University - Industry Collaboration Foundatio
    Inventors: Yeo Joon YOON, Jae Jong KIM, Si Kyu LIM
  • Patent number: 8524740
    Abstract: A compound of Formula I is disclosed as follows: or a pharmaceutically acceptable salt, prodrug, solvate, or metabolite thereof, wherein R is hydrogen, P(?O)(OH)2, P(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, P(?O)(OH)(OM), P(?O)(OM)2, P?O(O2M), S(?O)(OH)2, S(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, S(?O)(OH)(OM), S(?O)(OM)2; M is a monovalent or divalent metal ion, or alkylammonium ion; W is (C6-C20)aryl, (C6-C20)heteroaryl, (C1-C18)alkyl(C6-C20)aryl, (C1-C18)alkyl(C6-C20)heteroaryl, hydroxy(C6-C20)aryl, hydroxy(C6-C20)heteroaryl, (C1-C18)alkoxy(C6-C20)aryl, (C1-C18)alkoxy(C6-C20)heteroaryl, (C1-C18)alkylenedioxy(C6-C20)aryl, (C1-C18)alkylenedioxy(C6-C20)heteroaryl, halo(C6-C20)aryl, halo(C6-C20)heteroaryl, (C1-C18)alkylamino(C6-C20)aryl, (C1-C18)alkylamino(C6-C20)heteroaryl, (C1-C18)cycloalkylamino(C6-C20)aryl, or (C1-C18)cycloalkylamino(C6-C20)heteroaryl, and their OR8 substutes; R5 is (C1-C18alkoxy, hydrogen, hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or OR8, or R5 and R6 are (C1-C18)dioxy provided that R7 i
    Type: Grant
    Filed: July 13, 2011
    Date of Patent: September 3, 2013
    Assignee: Tairx, Inc.
    Inventors: Sheng-Chu Kuo, Kuo-Hsiung Lee, Li-Jiau Huang, Li-Chen Chou, Tian-Shung Wu, Tzong-Der Way, Jing-Gung Chung, Jai-Sing Yang, Chi-Hung Huang, Meng-Tung Tsai
  • Publication number: 20130184305
    Abstract: The invention discloses novel 42-0-(heteroalkoxyalkyl) rapamycin compounds of formula (1) and process for preparation thereof. These compounds are useful in the treatment of hyperproliferative vascular diseases such as restenosis and atherosclerosis Wherein, R denotes 3, 4 and 5 membered 3-hydroxy heteroalkoxyalkyl compounds selected from Tetrahydrofuran-3-ol, Oxetan-3-ol, Tetrahydropyran-3-ol, Tetrahydro-4- methyl furan-3-ol, Tetrahydro-2,5,5-trimethyl furan-3-ol, Tetrahydro-2,5-diethyl-2-methyl furan-3-ol, Tetrahydro-6-methoxy-2-methyl 2H-Pyran-3-ol and Tetrahydro-2,2-dimethyl-6-phenyl 2H-Pyran-3-ol.
    Type: Application
    Filed: August 2, 2011
    Publication date: July 18, 2013
    Inventors: Dhananjay Sharad Rane, Rajnikant Gandalal Vyas, Pramod Kumar Minocha
  • Publication number: 20130178494
    Abstract: The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy.
    Type: Application
    Filed: June 29, 2012
    Publication date: July 11, 2013
    Applicant: Academia Sinica
    Inventors: Tsann-Long SU, Ting-Chao Chou, Te-Chuang Lee
  • Publication number: 20130123286
    Abstract: Certain novel fused quinazoline derivatives of formula (I) as c-Met inhibitors, their synthesis and their uses for treating a c-Met mediated disorder. Methods for treating a c-Met-mediated disorder are also disclosed in the invention.
    Type: Application
    Filed: July 14, 2011
    Publication date: May 16, 2013
    Inventors: Shaojing Hu, Fei Wang, Wei Long, Xiaoyan Shen, Fenlai Tan, Yinxiang Wang
  • Publication number: 20130109713
    Abstract: The invention provides a compound of formula I:or a salt thereof, wherein R3-R8 and X and Y have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful as antibacterial agents.
    Type: Application
    Filed: June 24, 2011
    Publication date: May 2, 2013
    Inventors: Edmond J. Lavoie, Ajit Parhi, Daniel S. Pilch
  • Patent number: 8399449
    Abstract: The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention provides a compound represented by the formula (I) wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR1 (R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s)); R2 is carbamoyl optionally having substituent(s); and R3 is hydroxy optionally having substituent(s), or a salt thereof.
    Type: Grant
    Filed: February 25, 2009
    Date of Patent: March 19, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Nobuhiro Fujii, Yuya Oguro, Satoshi Sasaki, Shigeru Kondo
  • Patent number: 8394957
    Abstract: 9-aminonoscapine, prodrugs thereof, and pharmaceutically acceptable salts thereof, are disclosed. Pharmaceutical compositions including 9-aminonoscapine, and methods of preparation and use thereof are disclosed. 9-aminonoscapine is a noscapine analog that can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, by binding tubulin and inducing apoptosis selectively in tumor cells (ovarian and T-cell lymphoma) resistant to paclitaxel, vinblastine and teniposide. 9-aminonoscapine can perturb the progression of cell cycle by mitotic arrest, followed by apoptotic cell death associated with increased caspase-3 activation and appearance of TUNEL-positive cells. Thus, 9-aminonoscapine is a novel therapeutic agents for a variety of cancers, including ovarian and T-cell lymphoma cancers, even those that have become drug-resistant to currently available chemotherapeutic drugs.
    Type: Grant
    Filed: September 4, 2009
    Date of Patent: March 12, 2013
    Assignee: Emory University
    Inventors: Harish C. Joshi, Ritu Aneja, Surya N. Vangapandu
  • Patent number: 8383644
    Abstract: The present invention is directed to substituted azoanthracene derivatives or pharmaceutically acceptable salts thereof that modulate the human GLP-1 receptor and that may be useful in the treatment of diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial, such as diabetes mellitus type 2. The invention is also directed to pharmaceutical compositions comprising these compounds and to the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation of the human GLP-1 receptor is beneficial.
    Type: Grant
    Filed: June 29, 2010
    Date of Patent: February 26, 2013
    Assignee: TransTech Pharma, Inc.
    Inventors: Adnan M. M. Mjalli, Christopher Behme, Daniel P. Christen, Devi Reddy Gohimukkula, Dharma Rao Polisetti, James Quada, Jennifer L. R. Freeman, Kalpathy Santhosh, Muralidhar Bondlela, Mustafa Guzel, Ravindra Reddy Yarragunta, Robert Carl Andrews, Stephen Thomas Davis, Thomas Scott Yokum
  • Publication number: 20120289471
    Abstract: The present invention is directed to novel therapeutic compounds comprised of an amino acid bonded to a medicament or drug having a hydroxy, amino, carboxy or acylating derivative thereon. These high therapeutic index derivatives have the same utility as the drug from which they are made, and they have enhanced pharmacological and pharmaceutical properties. In fact, the novel drug derivatives of the present invention enhance at least one therapeutic quality, as defined herein. The present invention is also directed to pharmaceutical compositions containing same.
    Type: Application
    Filed: April 18, 2012
    Publication date: November 15, 2012
    Applicant: SIGNATURE R&D HOLDINGS, LLC
    Inventor: V. Ravi Chandran
  • Publication number: 20120252834
    Abstract: Rapamycin is used for prevention and treatment of toxic shock. The toxic shock is induced, for example, by a toxin, such as Staphylococcal enterotoxin A (SEA), Staphylococcal enterotoxin B (SEB), toxic shock syndrome toxin 1 (TSST-I), streptococcal pyrogenic exotoxin A (SPEA), and streptococcal pyrogenic exotoxin C (SPEC).
    Type: Application
    Filed: August 4, 2010
    Publication date: October 4, 2012
    Inventors: Teresa Krakauer, Marilyn Buckley
  • Patent number: 8258299
    Abstract: The present invention provides two synthetic routes for the preparation of Temsirolimus (compound 1b and analog of Temsirolimus 1a). The first route includes the synthesis of CCI-779 by directly reacting rapamycin (4b) or Prolyl-rapamycin (4a) with substituent-2,2-bis(methoxy) propionic acid anhydride(11) in the presence of an organic base, followed by deprotection to give CCI-779 or Proline CCI-779. The second route includes a process involving a reaction of rapamycin-OH-31-sily ether (4d) or Prolyl-rapamycin-OH-31-sily ether (4c) with substituent-2,2-bis(methoxy) propionic acid anhydride(11) in the presence of an organic base and followed by subsequent hydrolysis step to obtain the desired CCI-779 or Proline CCI-779. Compound 11, as described in this invention, is stable at room temperature, cost effective and ease of processing.
    Type: Grant
    Filed: March 29, 2010
    Date of Patent: September 4, 2012
    Assignee: Chungwa Chemical Synthesis & Biotech Co., Ltd.
    Inventors: Kwang-Chung Lee, Ting-Huei Lee, Yen-Shih Tung, Chia-Chen Kao, Tzu-Ai Lee
  • Publication number: 20120214837
    Abstract: The invention relates to compounds of the formula wherein R?, R1, through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
    Type: Application
    Filed: February 17, 2012
    Publication date: August 23, 2012
    Applicants: ExonHit Therapeutics SA, ALLERGAN, INC.
    Inventors: Bertrand Leblond, Cédric Chauvignac, Thierry Taverne, Eric Beausoleil, Anne-Sophie Casagrande, Laurent Désiré, Matthew P. Pando, John E. Donello, Rong Yang
  • Patent number: 8247554
    Abstract: A “real time” method for detecting chemical agents generally and particularly electrophilic and nucleophilic species by employing tunable, precursor sensor materials that mimic the physiological interaction of these agents to form highly florescent berberine-type alkaloids that can be easily and rapidly detected. These novel precursor sensor materials can be tuned for reaction with both electrophilic (chemical species, toxins) and nucleophilic (proteins and other biological molecules) species. By bonding or otherwise attaching these precursor molecules to a surface or substrate they can be used in numerous applications.
    Type: Grant
    Filed: November 9, 2007
    Date of Patent: August 21, 2012
    Assignee: Sandia Corporation
    Inventors: James R. McElhanon, Timothy J. Shepodd
  • Patent number: 8207188
    Abstract: The invention provides a method for the treatment of H4R modulated diseases and/or conditions comprising administering to the subject an effective amount of a H4R agonist. The invention also provides a method for treating COPD comprising administering to the subject an effective amount of a H4R agonist, a H1R antagonist and an anticholinergic drug. Further, the invention provides a pharmaceutical formulation comprising a H4R agonist, a second active agent and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: June 17, 2009
    Date of Patent: June 26, 2012
    Inventors: Michalis Nicolaou, Emile Loria, Gaetan Terrasse, Yves Trehin
  • Publication number: 20120108581
    Abstract: The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R7, a sulfur atom or an oxygen atom, R1, R2, R2?, R3 and R3? independently represent a hydrogen atom, C1-6 alkyl group or C3-6 cycloalkyl group, and R4, R5 and R6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.
    Type: Application
    Filed: March 25, 2010
    Publication date: May 3, 2012
    Applicant: Kowa Company, Ltd
    Inventors: Masanori Ashikawa, Toshiharu Morimoto, Hajime Yamada, Shunji Takemura, Tatsuaki Nishiyama, Takeshi Doi, Hiroyuki Ishiwata
  • Publication number: 20120101120
    Abstract: The invention provides an isolated stereoisomer of tritoqualine having the structure of FIG. 2 and FIG. 3.
    Type: Application
    Filed: August 24, 2011
    Publication date: April 26, 2012
    Inventors: Michalis Nicolaou, Emile Loria, Gaetan Terrasse, Yves Trehin
  • Publication number: 20120095075
    Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells.
    Type: Application
    Filed: August 16, 2011
    Publication date: April 19, 2012
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah MANOHARAN, Kallanthottathil G. Rajeev, David Butler, Narayanannair K. Jayaprakash, Muthusamy Jayaraman, Laxman Eltepu
  • Patent number: 8138344
    Abstract: Processes for the production of a 32-deoxorapamycin from a 32-iodo- or 32-hydroxyrapamycin, wherein the hydroxy group is substituted by the residue of an arylthionocarbonate or an arylthiocarbamate, in the presence of tris(trimethylsilyl)-silan and ?,??-azo-isobutyronitril in organic solvent; and 32-deoxorapamycin in the form of a crystalline solvate.
    Type: Grant
    Filed: January 22, 2007
    Date of Patent: March 20, 2012
    Assignee: Novartis AG
    Inventors: Murat Acemoglu, Sabine Pfeffer
  • Publication number: 20120041019
    Abstract: Compounds useful as protease inhibitors are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In one embodiment, the compounds are useful for inhibiting HIV protease enzymes, and are therefore useful in slowing the proliferation of HIV.
    Type: Application
    Filed: December 17, 2009
    Publication date: February 16, 2012
    Inventors: Mitchell W. Mutz, Kenneth J. Barr, Jason Gestwicki
  • Publication number: 20120028977
    Abstract: Provided are compounds, pharmaceutical compositions and methods of treating or preventing disorders associated with NMDA receptor activity, including schizophrenia, Parkinson's disease, cognitive disorders, depression, neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds of the general Formulas A-J, and pharmaceutically acceptable salts, esters, prodrugs or derivatives thereof are disclosed.
    Type: Application
    Filed: January 28, 2010
    Publication date: February 2, 2012
    Applicant: EMORY UNIVERSITY
    Inventors: Stephen F. Traynelis, Dennis C. Liotta, Rose M. Santangelo, Ethel C. Garnier
  • Publication number: 20120015908
    Abstract: A compound of Formula I is disclosed as follows: or a pharmaceutically acceptable salt, prodrug, solvate, or metabolite thereof, wherein R is hydrogen, P(?O)(OH)2, P(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, P(?O)(OH)(OM), P(?O)(OM)2, P?O(O2M), S(?O)(OH)2, S(?O)(O(C1-C18)alkylene(C6-C20)aryl)2, S(?O)(OH)(OM), S(?O)(OM)2; M is a monovalent or divalent metal ion, or alkylammonium ion; W is (C6-C20)aryl, (C6-C20)heteroaryl, (C1-C18)alkyl(C6-C20)aryl, (C1-C18)alkyl(C6-C20)heteroaryl, hydroxy(C6-C20)aryl, hydroxy(C6-C20)heteroaryl, (C1-C18)alkoxy(C6-C20)aryl, (C1-C18)alkoxy(C6-C20)heteroaryl, (C1-C18)alkylenedioxy(C6-C20)aryl, (C1-C18)alkylenedioxy(C6-C20)heteroaryl, halo(C6-C20)aryl, halo(C6-C20)heteroaryl, (C1-C18)alkylamino(C6-C20)aryl, (C1-C18)alkylamino(C6-C20)heteroaryl, (C1-C18)cycloalkylamino(C6-C20)aryl, or (C1-C18)cycloalkylamino(C6-C20)heteroaryl, and their OR8 substutes; R5 is (C1-C18alkoxy, hydrogen, hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or OR8, or R5 and R6 are (C1-C18)dioxy provided that R7 i
    Type: Application
    Filed: July 13, 2011
    Publication date: January 19, 2012
    Applicant: Efficient Pharma Management Corporate
    Inventors: Sheng-Chu Kuo, Kuo-Hsiung Lee, Li-Jiau Huang, Li-Chen Chou, Tian-Shung Wu, Tzong-Der Way, Jing-Gung Chung, Jai-Sing Yang, Chi-Hung Huang, Meng-Tung Tsai
  • Publication number: 20110319378
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: June 3, 2011
    Publication date: December 29, 2011
    Applicant: AMGEN INC.
    Inventors: Michael David BARTBERGER, Ana GONZALEZ BUENROSTRO, Hilary Plake BECK, Xiaoqi CHEN, Richard Victor CONNORS, Jeffrey DEIGNAN, Jason DUQUETTE, John EKSTEROWICZ, Benjamin FISHER, Brian Matthew FOX, Jiasheng FU, Zice FU, Felix GONZALEZ LOPEZ DE TURISO, Michael GRIBBLE, JR., Darin James GUSTIN, Julie Anne HEATH, Xin HUANG, Xianyun JIAO, Michael G. JOHNSON, Frank KAYSER, David John KOPECKY, Sujen LAI, Yihong LI, Zhihong LI, Jiwen LIU, Jonathan Dante LOW, Brian Stuart LUCAS, Zhihua MA, Lawrence McGEE, Joel McINTOSH, Dustin McMINN, Julio Cesar MEDINA, Jeffrey Thomas MIHALIC, Steven Howard Olson, Yosup REW, Philip Marley ROVETO, Daqing SUN, Xiaodong WANG, Yingcai WANG, Xuelei YAN, Ming YU, Jiang ZHU