Ring Nitrogen Shared By Two Of The Cyclos Patents (Class 514/230.2)
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Publication number: 20140011762Abstract: Provided herein are methods and computer-implemented systems for using computer simulations to predict likelihood of a cell population associated with a pathophysiological condition acquiring resistance to a therapeutic agent, to screen for therapeutic agents effective to suppress acquisition of resistance within a cell population and to treat the pathophysiological conditions associated therewith. The computer simulation comprises at least an input/out system and a mathematical model, including operably linked equations, parameter values and constant values, of growth response over a period of time of a cell population in contact with an therapeutic agent. Also provide is a method for determining a best-fit mathematical model of adaptation of a microbial population to a therapeutic agent over time and using the model to simulate microbial population behavior to a therapeutic agent.Type: ApplicationFiled: May 22, 2013Publication date: January 9, 2014Inventors: Vincent H. Tam, Michael Nikolaou
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Publication number: 20140005184Abstract: Provided herein are spirocyclic aminoquinolones of formula I and compositions containing the compounds. The compounds and compositions provided herein are useful in the prevention, amelioration or treatment of GSK-3 inhibitors mediated diseases.Type: ApplicationFiled: May 24, 2013Publication date: January 2, 2014Applicant: KYORIN PHARMACEUTICALS CO., LTD.Inventors: Oana COCIORVA, Yasumichi FUKUDA, Yasushi KOHNO, Bei LI, Kyoko OKADA, Ayako NAKAMURA, Masahiro NOMURA, Shigeki SETO, Anna Katrin SZARDENINGS, Kazuhiro YUMOTO
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Publication number: 20140005185Abstract: The present invention provides an imidazooxazine compound represented by Formula (I) or a salt thereof, wherein A, B, C, and D are as defined in the specification.Type: ApplicationFiled: April 5, 2012Publication date: January 2, 2014Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Masayuki Nakamura, Kenji Niiyama, Kaori Kamijo, Mitsuru Ohkubo, Toshiyasu Shimomura
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Patent number: 8618094Abstract: A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.Type: GrantFiled: July 2, 2009Date of Patent: December 31, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Hisashi Takahashi, Satoshi Komoriya, Takahiro Kitamura, Takashi Odagiri, Hiroaki Inagaki, Toshifumi Tsuda, Kiyoshi Nakayama, Makoto Takemura, Kenichi Yoshida, Rie Miyauchi, Masatoshi Nagamochi
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Publication number: 20130331376Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, E1, E2, R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: August 14, 2013Publication date: December 12, 2013Applicant: Elan Corporation, Inc.Inventors: Robert A. Galemmo, Dean R. Artis, Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Publication number: 20130331374Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: April 4, 2013Publication date: December 12, 2013Inventor: Rigel Pharmaceuticals, Inc.
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Publication number: 20130316999Abstract: The invention relates to the field of blood coagulation. Novel oxazolidinone derivatives of the general formula (I) processes for their preparation and their use as medicinally active compounds for the prophylaxis and/or treatment of disorders are described.Type: ApplicationFiled: August 7, 2013Publication date: November 28, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Alexander STRAUB, Thomas LAMPE, Jens POHLMANN, Susanne RÔHRIG, Elisabeth PERZBORN, Karl-Heinz SCHLEMMER, Joseph PERNERSTOFER
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Publication number: 20130303473Abstract: The invention provides pharmaceutical compositions based on liquid vehicles whose density is substantially higher than that of aqueous physiological fluids. The compositions are useful as medicines in ophthalmology, in particular for the treatment of conditions affecting the posterior segment of an eye. They may be administered topically into the eye or in a minimally invasive manner by periocular injection. Preferred liquid carriers are selected from semifluorinated alkanes.Type: ApplicationFiled: November 10, 2011Publication date: November 14, 2013Applicant: NOVALIQ GmbHInventor: Clive G. Wilson
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Publication number: 20130303528Abstract: Compositions for the treatment of neurodegenerative diseases are disclosed. Methods of treating and monitoring progression of a neurodegenerative disease are disclosed. According to the present invention, a selective CB2 receptor modulator may be administered to a mammal for the treatment of a neurodegenerative disease.Type: ApplicationFiled: March 29, 2013Publication date: November 14, 2013Inventors: Paul L. Prather, John P. Crow
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Publication number: 20130296275Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: July 2, 2013Publication date: November 7, 2013Inventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi
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Patent number: 8563546Abstract: The heterocyclic nitrogenous or oxygenous compounds of formula (A), (B), (C) or (D) formed from dialdehydes, their optical isomers, cis- and trans-isomers, or agrochemically acceptable salts, their preparation methods, agrochemical compositions comprising the compounds and the uses thereof are provided. The compounds and their derivatives have high insecticidal activities to several farming and forestry pests including homoptera and lepidoptera pests, such as aphis, fulgorid, whitefly, leafhopper, common thrips, cotton bollworm, cabbage caterpillar, cabbage moth, cotton leafworm, armyworm and so on.Type: GrantFiled: December 18, 2009Date of Patent: October 22, 2013Assignees: East China University of Science and Technology, Shanghai Shengnong Pesticide Co., Ltd.Inventors: Zhong Li, Xuhong Qian, Xusheng Shao, Xiaoyong Xu, Liming Tao, Gonghua Song
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Patent number: 8563547Abstract: (6,7-Dihydro-2-nitro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)amide compounds of formula (I), and their pharmaceutically acceptable salts, preparation methods and pharmaceutical compositions thereof are disclosed, wherein m and R are defined as in the description. The uses of the compounds in preparing medicaments for treating infectious diseases caused by Mycobacterium tuberculosis, especially infectious diseases caused by multi-drug resistance Mycobacterium tuberculosi are also disclosed.Type: GrantFiled: October 26, 2012Date of Patent: October 22, 2013Assignee: Shanghai Sun-Sail Pharmaceutical Science & Technology Co., Ltd.Inventors: Tiancai Wang, Ting Xin, Houxing Fan, Yilang Chen
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Publication number: 20130274239Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: May 8, 2013Publication date: October 17, 2013Inventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. A. Kiryanov
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Patent number: 8546383Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)— group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: May 25, 2012Date of Patent: October 1, 2013Assignee: 3M Innovative Properties CompanyInventors: George W. Griesgraber, Tushar A. Kshirsagar, Azim A. Celebi, Sarah J. Slania, Michael E. Danielson, Michael J. Rice, Joshua R. Wurst
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Publication number: 20130243828Abstract: The invention relates to respirable dry particles that contain one or more divalent metal cations, such as calcium, in an amount of less than 3% by weight, and to dry powders that contain the respirable particles. The dry particles can further contain an active agent, or can be used as carrier particles to deliver an active agent.Type: ApplicationFiled: September 29, 2011Publication date: September 19, 2013Applicant: PULMATRIX, INC.Inventors: Michael M. Lipp, Jean C. Sung
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Patent number: 8536167Abstract: The present invention relates to methods for treating an ophthalmic, otic, or nasal infection comprising treating the infected tissue with a composition comprising finafloxacin or a finafloxacin derivative. The present invention also relates to antimicrobial compositions comprising finafloxacin or a finafloxacin derivative. The compositions are suitable for the treatment of ophthalmic, otic, or nasal infections.Type: GrantFiled: July 2, 2010Date of Patent: September 17, 2013Assignee: Alcon Research, Ltd.Inventors: David W. Stroman, Masood A. Chowhan, Kenneth C. Appell
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Publication number: 20130231335Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6, are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: April 17, 2013Publication date: September 5, 2013Applicant: Elan Pharmaceuticals, Inc.Inventors: Robert A. Galemmo, Dean R. Artis, Xiaocong Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Publication number: 20130225549Abstract: The present invention relates to dihydropteridinones, their use as modulators of ?-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with ?-secretase and/or its substrate and therefore modulate the formation of A? peptides.Type: ApplicationFiled: February 14, 2013Publication date: August 29, 2013Applicant: Boehringer Ingelheim International GmbHInventor: Boehringer Ingelheim International GmbH
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Publication number: 20130213398Abstract: The present invention is directed toward respirable dry particles for delivery of divalent metal cation salts and/or monovalent cation salts to the respiratory tract and methods for treating a subject having a respiratory disease and/or infection.Type: ApplicationFiled: August 26, 2011Publication date: August 22, 2013Inventors: Michael M. Lipp, Jean C. Sung, Robert W. Clarke, David L. Hava
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Publication number: 20130217673Abstract: Effective treatments of pain for extended periods of time are provided. Through the administration of an effective amount of mixed monoamine reuptake inhibitor locally at or near a target site, one can relieve pain caused by diverse sources, including but not limited to spinal disc herniation (i.e. sciatica), spondilothesis, stenosis, discogenic back pain and joint pain, as well as pain that is incidental to surgery. When appropriate formulations are provided within biodegradable polymers, this relief can be continued for at least thirty days. In some embodiments, the relief can be for at least at least fifty days, at least one hundred days, at least one hundred and twenty days, at least one hundred and thirty, at least one hundred fifty days or at least one hundred and eighty days.Type: ApplicationFiled: February 22, 2012Publication date: August 22, 2013Applicant: Warsaw Orthopedic, IncInventor: Jared T. Wilsey
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Publication number: 20130210806Abstract: The present invention is directed to tricyclic indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.Type: ApplicationFiled: February 14, 2013Publication date: August 15, 2013Applicant: Janssen Pharmaceutica, NVInventor: Janssen Pharmaceutica, NV
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Publication number: 20130210801Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds of formula (I).Type: ApplicationFiled: July 1, 2011Publication date: August 15, 2013Applicant: GILEAD SCIENCES, INC.Inventors: Kerim Babaoglu, Kyla Bjornson, Hongyan Guo, Randall L. Halcomb, John O. Link, Hongtao Liu, Michael L. Mitchell, Jianyu Sun, James Taylor, Randall W. Vivian, Lianhong Xu
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Patent number: 8507481Abstract: Novel benzoxazine oxazolidinone compounds, preparation methods and uses thereof are disclosed, which belong to the field of pharmacy. More specifically, novel benzoxazine oxazolidinone compounds represented by the following general formula (I), preparation methods and uses thereof in preparing medicament for treating infectious diseases, especially infectious diseases caused by multi-drug resistant bacteria, are disclosed.Type: GrantFiled: May 12, 2011Date of Patent: August 13, 2013Assignees: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Nanjing Changao Pharmaceutical Science & Technology Co., LimitedInventors: Yushe Yang, Qisheng Xin, Houxing Fan, Bin Guo, Xin Liu, Huili He, Wei Li, Zhan Li
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Publication number: 20130203747Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: November 21, 2012Publication date: August 8, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Publication number: 20130178468Abstract: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: September 7, 2012Publication date: July 11, 2013Inventors: Joseph P. Vacca, John S. Wai, Linda S. Payne, Richard C. A. Isaccs, Wei Han, Melissa Egbertson, Richard Pracitto
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Publication number: 20130165368Abstract: A composition for use in the prevention and/or treatment of microbial infection comprising essentially of one or more pure alkanol alkoxylates, diol alkoxylates and/or triol alkoxylates.Type: ApplicationFiled: February 1, 2011Publication date: June 27, 2013Inventors: Ian Steel, Paul Armstrong
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Publication number: 20130143875Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: February 6, 2013Publication date: June 6, 2013Applicant: RIGEL PHARMACEUTICALS, INC.Inventor: RIGEL PHARMACEUTICALS, INC.
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Patent number: 8455482Abstract: A quinolone antibacterial compound, or a salt or hydrate of the compound, for the treatment of infectious diseases, which exhibit potent antibacterial activity and higher selective toxicity against Gram-positive and Gram-negative bacteria, which do not cause side effects (e.g.Type: GrantFiled: March 11, 2011Date of Patent: June 4, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Hisashi Takahashi, Junichi Kuroyanagi, Rie Miyauchi, Masatoshi Nagamochi, Makoto Takemura, Isao Hayakawa
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Publication number: 20130137675Abstract: The present invention aims to provide a compound having a PDE inhibitory action and useful as a medicament for the prophylaxis or treatment of schizophrenia and the like. A compound represented by the formula (1x): wherein each symbol is as described in the DESCRIPTION, or the formula (1): W1—W2??(1) wherein each symbol is as described in the DESCRIPTION, or a salt thereof.Type: ApplicationFiled: August 9, 2011Publication date: May 30, 2013Inventors: Takahiko Taniguchi, Shinkichi Suzuki, Masato Yoshikawa, Tomoaki Hasui, Makoto Fushimi, Jun Kunitomo
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Publication number: 20130137670Abstract: A formulation is provided that includes a volume of an aqueous multivalent physiological ion solution compatible with cerebrospinal fluid containing at least one divalent cation of magnesium or calcium, and at least one anion of carbonate or phosphate, and having a pH between 6.5 and 8.0. A zwitterionic therapeutic agent other than baclofen is dissolved the solution to achieve higher concentration or ease of solution and/or storage relative to therapeutic saline solutions of the same agent. A process of delivering a zwitterionic therapeutic agent into a subject is provided that includes dissolving a therapeutic amount of the zwitterionic therapeutic agent in a volume of artificial cerebrospinal fluid to form a stable formulation. The solution is then administered to the subject using an intrathecal pump.Type: ApplicationFiled: January 25, 2013Publication date: May 30, 2013Applicant: WAYNE STATE UNIVERSITY BOARD OF GOVERNORSInventor: Wayne State University Board of Governors
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Patent number: 8450311Abstract: Pharmaceutical compositions containing a fluoroquinolone antibiotic drug are disclosed. The compositions exhibit improved homogeneity, improved bioavailability, lower turbidity or a combination thereof. The composition can be use as otic or nasal compositions, but are particularly useful as ophthalmic compositions.Type: GrantFiled: May 29, 2009Date of Patent: May 28, 2013Assignee: Novartis AGInventors: Inmaculada Campins, Nuria Jiménez, Roman Vidal, Nuria Carreras, Carmen Martinez, Francisco Javier Galán
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Publication number: 20130123249Abstract: Novel benzoxazine oxazolidinone compounds, preparation methods and uses thereof are disclosed, which belong to the field of pharmacy. More specifically, novel benzoxazine oxazolidinone compounds represented by the following general formula (I), preparation methods and uses thereof in preparing medicament for treating infectious diseases, especially infectious diseases caused by multi-drug resistant bacteria, are disclosed.Type: ApplicationFiled: May 12, 2011Publication date: May 16, 2013Inventors: Yushe Yang, Qisheng Xin, Houxing Fan, Bin Guo, Xin Liu, Huili He, Wei Li, Zhan Li
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Publication number: 20130116243Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: December 23, 2010Publication date: May 9, 2013Applicant: ALMAC DISCOVERY LIMITEDInventors: Lixin Zhang, Graham Peter Trevitt, Hugues Miel, Frank Burkamp, Timothy Harrison, Andrew John Wilkinson, Charles-Henry Fabritius
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Publication number: 20130096109Abstract: An object of the present invention is to provide a novel integrase inhibitor. The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.Type: ApplicationFiled: April 11, 2011Publication date: April 18, 2013Applicant: SHIONOGI & CO., LTD.Inventors: Kazunari Hattori, Kenji Tomita
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Publication number: 20130079306Abstract: A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p27Kip1 is provided. The compound or the salt thereof is represented by the following formula (1): wherein A represents an alkyl group, a cycloalkyl group, an aryl group or a heterocyclic group, the group A may have a substituent; the ring B represents a 5- to 8-membered monocyclic heterocyclic ring or a condensed ring containing the monocyclic heterocyclic ring, the ring B may have a substituent; the ring C represents an aromatic ring, the ring C may have a substituent; L represents a linker comprising a main chain having 3 to 5 atoms selected from the group consisting of a carbon atom, a nitrogen atom, an oxygen atom and a sulfur atom, wherein at least one atom in the main chain is a hetero atom selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom, the linker L may have a substituent; and n is 0 or 1.Type: ApplicationFiled: July 1, 2011Publication date: March 28, 2013Inventors: Hiroshi Uchida, Akira Asagarasu, Teruaki Matsui
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Publication number: 20130065881Abstract: There is provided compounds of formula (I), wherein R1, R2, R3 and R4 have meanings given in the description (and which compounds are optionally substituted as indicated in the description), and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PIM family kinase, such as PIM-1, PIM-2 and/or PIM-3) is desired and/or required, and particularly in the treatment of cancer or a proliferative disease. There is also provided combinations comprising the compounds of formula (I).Type: ApplicationFiled: December 31, 2010Publication date: March 14, 2013Applicant: CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICASInventors: Joaquin Pastor Fernandez, Francisco Javier Ramos Lima, Ana Isabel Hernandez Higueras, Sonia Martinez Gonzalez, Jose Ignacio Martin Hernando, Carl-Gustave Pierre Saluste, Esther Gonzalez Cantalapiedra, Carmen Blanco Aparicio, Antonio Rodriguez Hergueta, Ana Maria Garcia Collazo, Antonio Salgado Serrano, Beatriz Noya Marino
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Publication number: 20130065866Abstract: The present invention is a dentinal drug delivery composition composed of cationic and/or neutral porous particles containing an effective amount of a therapeutic agent, a method for using the dentinal drug delivery to provide a dental treatment, and a method for identifying anti-inflammatory agents capable of diffusing through dentin.Type: ApplicationFiled: November 7, 2012Publication date: March 14, 2013Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventor: University of Medicine and Dentistry of New Jersey
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Patent number: 8394951Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: GrantFiled: January 13, 2010Date of Patent: March 12, 2013Assignee: Rigel Pharmaceuticals Inc.Inventors: Haoran Zhao, Rao Kolluri, Carlos Valdez, Kin Tso, Rajinder Singh, John Ramphal
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Patent number: 8389514Abstract: Provided herein are aminoquinolones and pharmaceutically acceptable derivatives thereof. In certain embodiments, provided herein are compounds, compositions and methods for treating, preventing or ameliorating GSK-3 mediated diseases.Type: GrantFiled: September 11, 2008Date of Patent: March 5, 2013Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Bei Li, Anna Katrin Szardenings
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Publication number: 20130045971Abstract: Sudden cardiac arrest is treated by reducing blood temperature from about 37° C. to 33° C., following resuscitation, by injecting hypothermia inducing drugs such as a cannabinoid type into the patient's body, preferably in combination with physical surface body cooling.Type: ApplicationFiled: August 18, 2011Publication date: February 21, 2013Inventors: Wanchun Tang, Shijie Sun
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Publication number: 20130040943Abstract: This disclosure relates to compounds of formula I: wherein R1, R2, R3, R4, X and Y have the meanings denoted in the disclosure. The compounds of formula I have antithrombotic activity and in particular inhibit the protease-activated receptor 1 (PAR1). The disclosure further relates to a method for producing the compound of formula I and to the use thereof as a pharmaceutical product.Type: ApplicationFiled: October 16, 2012Publication date: February 14, 2013Applicant: SANOFIInventor: SANOFI
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Publication number: 20130029977Abstract: A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.Type: ApplicationFiled: July 2, 2009Publication date: January 31, 2013Inventors: Hisashi Takahashi, Satoshi Komoriya, Takahiro Kitamura, Takashi Odagiri, Hiroaki Inagaki, Toshifumi Tsuda, Kiyoshi Nakayama, Makoto Takemura, Kenichi Yoshida, Rie Miyauchi, Masatoshi Nagamochi
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Patent number: 8362011Abstract: The present invention relates to new tricyclic triazolic compounds having a high affinity for sigma-1 receptor as well as to the process for the preparation thereof, to composition comprising them and to their use as medicaments according to compounds of formula (I), Wherein R1 and R2 are as defined in the description.Type: GrantFiled: December 5, 2008Date of Patent: January 29, 2013Assignee: Laboratories del Dr. Esteve, S.A.Inventors: Miguel Angel Pericas-Brondo, Antoni Torrens-Jover, Félix Cuevas-Cordobes, Susana Yenes-Minguez
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Patent number: 8343964Abstract: The invention relates to the use of at least one compound of the formula (I), in which R and R3 are particularly a hydrogen atom, R1 is particularly a hydrogen atom or a methyl, ethyl or isobutyl mi group, R4, R5, R6 and R7 are independently a hydrogen atony, an alkoxyl group with 1 to 7 carbon atoms or a halogen atom, R2 is a hydrogen atom, an O? group or an OH group, B is an N-GP1 or NRc, group, GP1 being a Boc or Cbz group, and Rc is a hydrogen atom or a methyl or t-butyl group, for preparing a drug for treating conditions associated with bacterial infections, in particular for treating bacterial diseases.Type: GrantFiled: January 31, 2008Date of Patent: January 1, 2013Assignees: Universite Joseph Fourier, Centre National de la Recherche ScientifiqueInventors: Jean-Noel Marie Leon Denis, Xavier Jean Georges Marie Guinchard, Nicole Jeanne Moreau born Laffont, Luc Neuville, Yannick Vallee
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Publication number: 20120329773Abstract: This invention relates to bicyclic ring system substituted amide functionalized phenols of general formula 1, their use as inhibitors of CXCR2 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin, or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: ApplicationFiled: December 13, 2011Publication date: December 27, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Riccardo GIOVANNINI, Dieter HAMPRECHT, Barbara KISTLER, Iain LINGARD
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Publication number: 20120329790Abstract: The present invention is a dentinal drug delivery composition composed of cationic and/or neutral porous particles containing an effective amount of a therapeutic agent and a method for using the same to provide a dental treatment.Type: ApplicationFiled: November 23, 2010Publication date: December 27, 2012Applicant: University of Medicine and Dentistry of New JerseyInventor: Kenneth Markowitz
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Publication number: 20120322766Abstract: The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of anthrax and other infections.Type: ApplicationFiled: August 28, 2012Publication date: December 20, 2012Applicant: Morphochem Aktiengesellschaft fuer Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Hans Locher, Christine Schmitt
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Publication number: 20120316158Abstract: Instillation of a 1.5% (w/v) levofloxacin ophthalmic solution three times a day, which is the dosage or dose regimen of the present invention, has features to cure bacterial conjunctivitis in a shorter time than instillation of a 0.5% (w/v) ophthalmic solution three times a day, which is the conventional dosage or dose regimen, and not to increase the rate of occurrence of side effects. Curing the ocular infection in a short time leads to shortening of the duration of exposure of the ocular-infection-causing bacterium to levofloxacin. Therefore, the levofloxacin ophthalmic solution in the dosage or dose regimen of the present invention is eventually expected to suppress emergence of the resistant bacterium resulting from the long-term use of the levofloxacin ophthalmic solution in the conventional dosage or dose regimen.Type: ApplicationFiled: December 16, 2010Publication date: December 13, 2012Applicants: DAIICHI SANKYO COMPANY, LIMITED, SANTEN PHARMACEUTICAL CO., LTD.Inventors: Takashi Nagano, Koji Sakanaka, Masatsugu Nakamura, Kouichi Kawazu, Hajime Ibuki, Kayoko Sakamoto
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Publication number: 20120309724Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, X, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: May 18, 2012Publication date: December 6, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
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Publication number: 20120295899Abstract: The present application describes modulators of MCP-1 or CCR-2 of formula or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, n, W, X, R1 and R6, are defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using modulators of formula (I) are disclosed.Type: ApplicationFiled: February 8, 2011Publication date: November 22, 2012Inventors: Ian K. Mangion, Percy H. Carter, Jingwu Duan, Andrew J. Tebben