Tricyclo Ring System Having 1,3-diazine As One Of The Cyclos Patents (Class 514/267)
-
Patent number: 9556187Abstract: This disclosure relates to novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities. A tricyclic heterocyclic compound represented by the formula (Ib), wherein the rings Ab and Bb, Xb, Yb, R1b, R2b, R3b, L1b, L2b, L3b and nb are as defined in the specification.Type: GrantFiled: October 2, 2015Date of Patent: January 31, 2017Assignee: NISSAN CHEMICAL INDUSTRIES, LTD.Inventors: Keishi Hayashi, Tsuneo Watanabe, Koji Toyama, Junji Kamon, Masataka Minami, Miyuki Uni, Mariko Nasu
-
Patent number: 9505756Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.Type: GrantFiled: February 6, 2015Date of Patent: November 29, 2016Assignee: HYDRA BIOSCIENCES, INC.Inventors: Xinyuan Wu, Spencer David Kimball, Ping Chen, Ding Zhou, Shaoping Peng
-
Patent number: 9504688Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).Type: GrantFiled: May 2, 2013Date of Patent: November 29, 2016Assignees: THE REGENTS OF THE UNIVERSITY OF MICHIGAN, THE CURATORS OF THE UNIVERSITY OF MISSOURIInventors: David Ginsburg, Scott D. Larsen, Bryan Yestrepsky, Hongmin Sun
-
Patent number: 9422297Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.Type: GrantFiled: September 25, 2014Date of Patent: August 23, 2016Assignee: Duquesne University of the Holy GhostInventor: Aleem Gangjee
-
Patent number: 9415005Abstract: This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics.Type: GrantFiled: March 13, 2013Date of Patent: August 16, 2016Assignee: VeroScience LLCInventor: Anthony H. Cincotta
-
Patent number: 9403778Abstract: The invention provides compounds of formula I: or a salt thereof as described herein. The invention also provides dermatological compositions comprising a compound of formula I or mixtures of one or more compounds of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods for protecting skin or DNA from photodamage or repairing photodamaged skin or DNA.Type: GrantFiled: January 11, 2013Date of Patent: August 2, 2016Assignee: Regents of the University of MinnesotaInventors: Robert Vince, Abbas Raza, Christine Dreis
-
Patent number: 9402830Abstract: The present disclosure describes compounds and pharmaceutically acceptable salts thereof and compositions and formulations comprising the same that are useful in methods of treating dyskinesia or related disorders, and methods for treating dyskinesia or related disorders.Type: GrantFiled: May 1, 2015Date of Patent: August 2, 2016Assignee: Melior Discovery, Inc.Inventors: John Ciallella, John Gruner, Andrew G. Reaume, Michael S. Saporito
-
Patent number: 9382287Abstract: Methods are provided for using methotrexate (MTX) active agents in which reduced host toxicity is observed. Aspects of the methods include administering to a subject an effective amount of an MTX active agent in conjunction with a MTX toxicity-reducing adjuvant, such as a 2,2?-anhydropyrimidine, a derivative thereof or a uridine phosphorylase inhibitor. Also provided are compositions and kits that find use in practicing embodiments of the invention. The methods and compositions find use in a variety of applications, including the treatment of a variety of different disease conditions.Type: GrantFiled: October 6, 2014Date of Patent: July 5, 2016Assignee: Tosk, Inc.Inventors: William A. Garland, Brian D. Frenzel, Travis Karg
-
Patent number: 9365575Abstract: The present invention relates to compounds of Formula I or a pharmaceutically acceptable salt thereof, wherein variables R, Ar, X, and Ar1 and n are as defined herein. The compounds are capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: GrantFiled: May 20, 2013Date of Patent: June 14, 2016Assignee: Allergan, Inc.Inventors: Thomas C. Malone, Julie A. Wurster, Clarence Eugene Hull, III
-
Patent number: 9359370Abstract: The invention relates to 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, its therapeutic usage for treatment of diseases mediated by EGFR kinase and its combinatory therapeutic usage together with other therapeutic agents. The invention also provides synthetic methods for preparation of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, and the relevant synthetic intermediates for synthesis of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride.Type: GrantFiled: July 31, 2014Date of Patent: June 7, 2016Assignee: Beta Pharma, Inc.Inventors: Yinxiang Wang, Guojian Xie, Lieming Ding, Fenlai Tan, Yunyan Hu, Wei He, Bin Han, Wei Long, Yong Liu, Haima Ai, Charles Davis, Don Zhang
-
Patent number: 9301958Abstract: Pharmaceutical compositions comprising tricyclic 3,4-propinoperhydropurines and uses thereof for the treatment of facial wrinkling are provided.Type: GrantFiled: June 4, 2012Date of Patent: April 5, 2016Assignee: Phytotox LimitedInventor: Nestor Antonio Lagos Wilson
-
Patent number: 9303035Abstract: The present invention provides a compound of formula I or a pharmaceutically acceptable salt thereof; and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: December 17, 2013Date of Patent: April 5, 2016Assignee: Novartis AGInventors: Mahbub Ahmed, Alexander Ashall-Kelly, Graham Charles Bloomfield, Louisa Gueritz, Jeffrey McKenna, Joseph McKenna, Simon Mutton, Rakesh Parmar, Jon Sheperd, Paul Wright
-
Patent number: 9284335Abstract: Described herein are compounds and chemical entities of Formula (I), methods of their synthesis, compositions comprising them, and their use in treating numerous diseases and disorders, including cognitive deficits associated with CNS diseases and disorders.Type: GrantFiled: June 18, 2013Date of Patent: March 15, 2016Assignee: Dart NeuroScience (Cayman) Ltd.Inventors: Amy Allan, Bryan Branstetter, Brian Dyck, Laurent Gomez, Tami Jo Marrone, Marco Peters, Michael I. Weinhouse
-
Patent number: 9284318Abstract: The present invention relates to novel kinase inhibitors. Compounds of this class have been found to be effective inhibitors of protein kinases, including members of PDGFR and VEGFR families.Type: GrantFiled: April 3, 2012Date of Patent: March 15, 2016Assignee: Pharmascience, Inc.Inventors: Alain Laurent, Yannick Rose, Stephen Morris, James Jaquith
-
Patent number: 9260452Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.Type: GrantFiled: June 8, 2012Date of Patent: February 16, 2016Assignee: Sunovion Pharmaceuticals Inc.Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
-
Patent number: 9227979Abstract: Disclosed are compounds of the formula (I) which are fluorescently labeled antagonists of the A3 adenosine receptor: wherein A, R1, R2, and Y are as described herein. Also disclosed are diagnostic compositions and a method of diagnosis of a patient for a possible treatment by an antagonist of the A3 adenosine receptor, involving the use of one or more of these compounds as diagnostic agents.Type: GrantFiled: January 24, 2013Date of Patent: January 5, 2016Assignees: The United States of America, as represented by The Secretary, Department of Health and Human Services, Universita Degli Studi Di Trieste, Universita Degli Studi Di PadovaInventors: Kenneth A. Jacobson, Santhosh Kumar Thatikonda, Eszter Erika Kozma, Giampiero Spalluto, Stefano Moro, Stephanie Federico
-
Patent number: 9181269Abstract: The present invention discloses novel enantiomeric antifungal compounds of Formula (1a) and Formula (1b) containing thieno-[2,3-d]Jpyrimidin-4(3H)-one moiety and pharmaceutically acceptable salts thereof, method of preparing these compounds, the use of these compounds in prevention and treatment of fungal infections, and pharmaceutical preparations containing these compounds.Type: GrantFiled: May 31, 2011Date of Patent: November 10, 2015Assignees: FDC Limited, Council for Scientific & Industrial ResearchInventors: Hanumant Bapurao Borate, Suleman Riyajsaheb Maujan, Sangmeshwer Prabhkara Sawargave, Subhash Prataprao Chavan, Mohan Anand Chandavarkar, Ramkrishnan Ramachandran Iyer, Vikas Vasant Nawathye, Gajanan Jalindar Chavan, Amit Chandrakant Tawte, Deepali Damodar Rao
-
Patent number: 9173846Abstract: This invention provides novel solid pharmaceutical compositions and processes for the bulk production of said compositions. This invention also provides methods of using the pharmaceutical compositions in the treatment of cancer.Type: GrantFiled: May 14, 2010Date of Patent: November 3, 2015Assignee: MILLENNIUM PHARMACEUTICALS, INC.Inventor: Bhavishya Mittal
-
Patent number: 9163022Abstract: The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-? or by PDE4, including but not limited to rheumatoid arthritis.Type: GrantFiled: September 4, 2014Date of Patent: October 20, 2015Assignee: vTv Therapeutics LLCInventors: Adnan M. M. Mjalli, Bapu Gaddam, Dharma Rao Polisetti, Matthew J. Kostura, Mustafa Guzel
-
Patent number: 9107925Abstract: The invention concerns a sodium channel blocker for the treatment of a reduction or loss of superficial sensitivity or sense of touch of a human being or another mammal.Type: GrantFiled: February 10, 2011Date of Patent: August 18, 2015Assignee: PHYTOTOX LIMITEDInventors: Max Rutman, Jean J. Pilorget, Constanza Sigala, Pablo Valenzuela
-
Patent number: 9085588Abstract: The present invention relates to the technical field of medicine, and specifically provides methods for preparing Icotinib, Icotinib hydrochloride, and intermediates thereof. These methods avoid the use of phosphorus oxychloride, thereby greatly reducing the emission of pollutants, which is of major benefits to the economy and environment.Type: GrantFiled: December 28, 2012Date of Patent: July 21, 2015Assignee: Betta Pharmaceuticals Co., Ltd.Inventors: Shaojing Hu, Wei Long, Fei Wang, Zongquan Li
-
Patent number: 9085586Abstract: The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same.Type: GrantFiled: July 11, 2013Date of Patent: July 21, 2015Assignee: Nimbus Iris, Inc.Inventors: Donna L. Romero, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
-
Patent number: 9073936Abstract: Provided are PDE1 inhibitors of Formula I, processes for their production, their use as pharmaceuticals, and pharmaceutical compositions comprising them.Type: GrantFiled: March 13, 2014Date of Patent: July 7, 2015Assignee: INTRA-CELLULAR THERAPIES, INC.Inventors: Peng Li, Hailin Zheng, Jun Zhao, Lawrence P. Wennogle
-
Patent number: 9045489Abstract: The present invention provides tricyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.Type: GrantFiled: October 9, 2012Date of Patent: June 2, 2015Assignee: Duquesne University of the Holy SpiritInventor: Aleem Gangjee
-
Publication number: 20150141408Abstract: The present invention relates to tricyclic pyrrolo derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: January 30, 2015Publication date: May 21, 2015Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Marina Caldarelli, Mauro Angiolini, Italo Beria, Maria Gabriella Brasca, Francesco Casuscelli, Roberto D'Alessio, Andrea Lombardi Borgia
-
Publication number: 20150141444Abstract: The present invention is directed to N-methyl tetrahydroquinoline compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: ApplicationFiled: May 11, 2012Publication date: May 21, 2015Inventors: Scott D. Kuduk, Christina Ng DiMarco, Thomas J. Greshock
-
Publication number: 20150141415Abstract: The present invention relates to methods for treating an infectious disease in a subject in need thereof via administration of a therapeutically effective amount of compounds described herein. The methods may utilize particular compounds, for example, a quinoline, a hydrazone, a quinone, or a pyrimidine derivatives thereof or a pharmaceutical salts thereof.Type: ApplicationFiled: November 7, 2014Publication date: May 21, 2015Inventors: Omonike Arike Olaleye, Sarah Finney John, Adaugo Chimzurum Isichei, Jun O Liu, Rosa Maldonado, Janice Endsley
-
Publication number: 20150141445Abstract: The present invention provides tricyclic compounds having cytostatic and cytotoxic activity in a single molecule having receptor tyrosine kinase(s), dihydrofolate reductase, thymidylate synthase and/or dihydroorotate dehydrogenase inhibitory activity, which are useful as anti-angiogenic and anti-tumor agents. Also provided are methods of utilizing these inhibitors to treat tumor cells and other proliferative diseases and disorders.Type: ApplicationFiled: September 25, 2014Publication date: May 21, 2015Inventor: Aleem Gangjee
-
Publication number: 20150133426Abstract: The present invention relates to substituted pyrrolopyrimidine compounds general formula I: in which A, X, R1, R2, m and n are as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: May 17, 2013Publication date: May 14, 2015Inventors: Ulrich Klar, Georg Kettschau, Detlev Sülzle, Florian Puehler, Dirk Kosemund, Philip Lienau, Ulf Bömer, Lars Wortmann
-
Publication number: 20150133425Abstract: The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: May 17, 2013Publication date: May 14, 2015Inventors: Georg Kettschau, Florian Puehler, Knut Eis, Ulrich Klar, Dirk Kosemund, Detlev Sülzle, Philip Lienau, Andrea Hägebarth, Ulf Bömer, Lars Wortmann, Keith Graham, Antje Margret Wengner
-
Publication number: 20150132352Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).Type: ApplicationFiled: May 2, 2013Publication date: May 14, 2015Inventors: Hongmin Sun, Bryan Yestrepsky, David Ginsburg, Scott D. Larsen
-
Publication number: 20150126496Abstract: The invention relates to methods for diagnosis and treatment of autism spectrum disorders, particularly for autism spectrum disorders characterized by increased head size (circumference) and deficits in social behavior.Type: ApplicationFiled: October 10, 2014Publication date: May 7, 2015Applicant: Massachusetts Institute of TechnologyInventors: Damon Theron Page, Mriganka Sur
-
Publication number: 20150126449Abstract: The present application relates to novel substituted (aza)pyridopyrazolopyrimidinones and indazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired bleeding disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of menorrhagia, postpartum hemorrhage, hemorrhagic shock, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.Type: ApplicationFiled: November 5, 2014Publication date: May 7, 2015Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Jorma Haßfeld, Tom KINZEL, Johannes Köbberling, Yolanda CANCHO GRANDE, Kristin BEYER, Susanne Röhrig, Maria Köllnberger, Michael SPERZEL, Nils BURKHARDT, Karl-Heinz SCHLEMMER, Christian STEGMANN, Joachim SCHUHMACHER, Matthias WERNER, Manuel ELLERMANN
-
Patent number: 9018222Abstract: The present invention refers to the use of sodium channel blockers such as tetrodotoxin or saxitoxin, its analogues/derivatives as well as their acceptable salts, for the production of a medicament for the treatment of neuropathic pain resulting from chemotherapy.Type: GrantFiled: March 26, 2007Date of Patent: April 28, 2015Assignee: Wex Medical LimitedInventors: Helmut Heinrich Buschmann, Jose Miguel Vela Hernandez, Jose Manuel Baeyens
-
Patent number: 9012466Abstract: The present invention relates to substituted tricyclic pyrazolo-pyrimidine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted tricyclic pyrazolo-pyrimidine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: March 11, 2014Date of Patent: April 21, 2015Assignee: ArQule Inc.Inventors: Nivedita Namdev, Jianqiang Wang, Mark Ashwell, Audra Dalton, Jason Hill, Eugene Kelleher, Jeffrey Link, Rocio Palma, Sudharshan Eathiraj, Neil Westlund, Hui Wu, Rui-Yang Yang
-
Patent number: 9012465Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.Type: GrantFiled: August 9, 2013Date of Patent: April 21, 2015Assignee: Hydra Biosciences, Inc.Inventors: Xinyuan Wu, Spencer David Kimball, Ping Chen, Ding Zhou, Shaoping Peng
-
Publication number: 20150105327Abstract: This disclosure provides methods and compositions to inhibit or suppress tumor growth or to treat cancer by inhibiting VprBP kinase activity. Also provided are methods of determining the effectiveness of the methods and compositions to inhibit or suppress tumor growth or to treat cancer by inhibiting VprBP kinase activity, methods for detecting a cancer, and methods for screening potential agents that inhibit VprBP kinase activity.Type: ApplicationFiled: October 14, 2014Publication date: April 16, 2015Inventors: Woojin An, Nouri Neamati, Kyunghwan Kim
-
Publication number: 20150105381Abstract: The present invention relates to the pyrazoloquinazolinone and pyrroloquinazolinone derivatives of the general formula (I), as well as pharmaceutical compositions containing them, and their use in the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals, in particular their use in the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders.Type: ApplicationFiled: May 21, 2013Publication date: April 16, 2015Inventors: Stanislas Mayer, Stephan Schann
-
Patent number: 9006258Abstract: The present invention relates to a new use for compounds that inhibit phosphodiesterase 1 (PDE1), e.g., that inhibit PDE1-mediated suppression of the dopamine D1 receptor and/or progesterone signaling pathways, including, e.g., methods of treatment or prophylaxis for conditions which may be ameliorated by enhancing the progesterone signaling response, particularly female sexual dysfunction.Type: GrantFiled: December 5, 2007Date of Patent: April 14, 2015Assignee: Intra-Cellular Therapies, Inc.Inventors: Allen A. Fienberg, Sharon Mates, Lawrence P. Wennogle
-
Patent number: 9000001Abstract: The invention provides novel 7,8-dihydro-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4-one compounds and 7,8,9-trihydro-[1H or 2H]-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds, substituted at the 1 or 2 position with C2-9 alkyl, C3-9 cycloalkyl, heteroarylalkyl, or substituted arylalkyl, in free, salt or prodrug form, processes for their production, their use as pharmaceuticals, particularly as PDE1 inhibitors, and pharmaceutical compositions comprising them.Type: GrantFiled: July 18, 2012Date of Patent: April 7, 2015Assignee: Intra-Cellular Therapies, Inc.Inventors: Peng Li, Haiyan Wu
-
Publication number: 20150086637Abstract: The present invention relates to a novel pharmaceutical composition free of gastric coating comprising anagrelide hydrochloride in combination with a non-pH dependent polymer and a pharmaceutically acceptable watersoluble acid and its use for the treatment of essential thrombocythemia.Type: ApplicationFiled: November 26, 2014Publication date: March 26, 2015Inventors: Rudolf WIDMANN, Georg STRIEDER
-
Patent number: 8987286Abstract: Compounds of Formula (I), which are effective inhibitors of the Pi3K/Akt pathway, processes for their production and their use as pharmaceuticals. The compounds of formula (I) a: useful for the treatment of cancer.Type: GrantFiled: December 13, 2011Date of Patent: March 24, 2015Assignee: Bayer Intellectual Property GmbHInventors: Hartmut Rehwinkel, Andrea Hägebarth, Oliver Politz, Roland Neuhaus, Ulf Bömer
-
Publication number: 20150079159Abstract: A dosing regimen for formulations that contain a therapeutic dosage of a site 1 sodium channel blocker, where the dosing regimen provides a prolonged nerve block and is in an effective amount to delay the onset of neuropathic pain, such as hyperalgesia and/or allodynia, for at least one week, and preferably longer at the site, and preferably the region (e.g. entire limb), where the nerve block was applied. The site 1 sodium channel blocker is preferably saxitoxin (STX), preferably in combination with a corticosteroid, preferably dexamethasone. In a preferred embodiment, liposomes are included in the formulation as a controlled release system, producing prolonged duration of block without systemic toxicity. As demonstrated by the examples, encapsulating STX in a controlled release system, such as liposomes, preferably also including a corticosteroid, and administering in suitable dosing regimen to achieve a prolonged nerve block without systemic toxicity, delays the onset of hyperalgesia.Type: ApplicationFiled: April 23, 2013Publication date: March 19, 2015Inventors: Sahadev Aramanethalgur Shankarappa, Daniel S. Kohane
-
Publication number: 20150080374Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: November 25, 2014Publication date: March 19, 2015Inventors: William Scott, Ningshu LIU, Manfred MÖWES, Andrea HÄGEBARTH, Ursula MÖNNING, Ulf BÖMER
-
Patent number: 8980903Abstract: Compounds, pharmaceutical compositions and methods are provided that are useful in the treatment of CDK4-mediated disorders, such as cancer. The subject compounds are fused pyridine, pyrimide and triazine derivatives.Type: GrantFiled: August 7, 2014Date of Patent: March 17, 2015Assignee: Amgen Inc.Inventors: Richard V. Connors, Kang Dai, John Eksterowicz, Pingchen Fan, Benjamin Fisher, Jiasheng Fu, Kexue Li, Zhihong Li, Lawrence R. McGee, Rajiv Sharma, Xiaodong Wang, Dustin L. McMinn, Jeffrey T. Mihalic, Jeffrey Deignan
-
Patent number: 8980902Abstract: Compounds of the following formula are provided for use with PARP: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits, and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds.Type: GrantFiled: September 18, 2013Date of Patent: March 17, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Jason W. Brown, Anthony R. Gangloff, Andre K. Kiryanov
-
Patent number: 8975268Abstract: Since each of the site I sodium channel blockers have a unique activity and cannot be used to extrapolate the same effective dosage for another site I sodium channel blocker, studies were conducted to identify dosages of neosaxitoxin (“NeoSTX”) and bupivacaine, alone or in combination with epinephrine, to provide two to three days of pain relief in humans. Bupivacaine-NeoSTX combinations produce more reliable blockade and longer duration blockade compared to NeoSTX alone. The three-way combination of NeoSTX-bupivacaine-epinephrine produces more prolonged local anesthesia than the two-way combination of NeoSTX-bupivacaine. Addition of epinephrine to this NeoSTX-bupivacaine combination dramatically prolongs the duration of complete blockade to a mechanical stimulus. These results led to development of specific combination dosage formulations.Type: GrantFiled: July 15, 2014Date of Patent: March 10, 2015Assignee: The Children's Medical Center CorporationInventors: Charles Berde, Daniel S. Kohane
-
Patent number: 8975269Abstract: The present invention provides a catalyst complex or ligand, and compositions thereof, for use in a variety of organic reactions having high reactivity and enantioselectivity. The catalyst is a N-heterocyclic carbene having three fused rings with first and second rings being six-membered rings and the third being a five-membered ring. The first ring is fused to the second and has four substituents. The second ring has two nitrogens flanking a carbene atom with one nitrogen bound to a substituent. The carbene atom may optionally be bonded to a metal. The third ring is fused to the second ring and contains two nitrogens. The third ring of the catalyst has a double bond and two substituents on adjacent non-fused carbons. A non-fused nitrogen of the third ring is partially bonded to another substituent. Methods for the synthesis and use of the catalyst embodiments of the present invention are also provided.Type: GrantFiled: July 29, 2014Date of Patent: March 10, 2015Assignee: Florida State University Research FoundationInventors: D. Tyler McQuade, Jin Kyoon Park, Matthew D. Rexford, Hershel H. Lackey
-
Patent number: 8975267Abstract: The present invention relates to tricyclic pyrrolo derivatives of Formula (I), which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.Type: GrantFiled: January 19, 2012Date of Patent: March 10, 2015Assignee: Nerviano Medical Sciences S.r.l.Inventors: Marina Caldarelli, Mauro Angiolini, Italo Beria, Maria Gabriella Brasca, Francesco Casuscelli, Roberto D'Alessio, Andrea Lombardi Borgia
-
Publication number: 20150065528Abstract: The invention concerns a paralytic shellfish poison for the treatment of itching in a human being or another mammal.Type: ApplicationFiled: March 15, 2013Publication date: March 5, 2015Applicant: ALGENIS SPAInventors: Max Rutman, Jean-Jacques Pilorget, Jimmy Stehberg, Wolfgang Vanscheidt, Constanza Sigala