Polycyclo Ring System Having The Additional Oxygen Hetero Ring As One Of The Cyclos Patents (Class 514/254.11)
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Patent number: 8673920Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: GrantFiled: April 27, 2010Date of Patent: March 18, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Alexander Pasternak, Aurash Shahripour, Haifeng Tang, Nardos H. Teumelsan, Lihu Yang, Yuping Zhu, Shawn P. Walsh
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Publication number: 20140073595Abstract: The present invention relates to an aromatic substituted pentadienoic acid amides and there use in combination of specific amounts of aromatic amides i.e. 4-alkyl-5-(substituted phenyl)-2(E),4(E)-pentadienoic acid amides, its geometrical isomers or their dihydro or tetrahydro derivatives and an anti-infective drug useful in potentiating the bioefficacy of antiinfective drug. The combination of the present invention is useful in the treatment of certain infections and disease at lower concentration of anti-infectives necessary to inhibit the growth of microbial strains and may also find applications in reducing the resistance in microorganisms.Type: ApplicationFiled: October 11, 2013Publication date: March 13, 2014Applicant: Council Of Scientific and Industrial ResearchInventors: Surrinder KOUL, Jawahir Lal KOUL, Subhash Chandra TANEJA, Pankaj GUPTA, Inshad Ali KHAN, Zahid Mehmood MIRZA, Ashwani KUMAR, Rakesh Kamal JOHRI, Monika PANDITA, Anita KHOSA, Ashok Kumar TIKOO, Subhash Chander Sharma, Vijeshwar VERMA, Ghulam Nabi QAZI
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Publication number: 20140066365Abstract: A product comprising at least one given antibiotic and a calixarene for use as medicament.Type: ApplicationFiled: April 11, 2012Publication date: March 6, 2014Inventors: Marion Grare, Raphaƫl, Emmanuel Duval
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Publication number: 20140051709Abstract: Disclosed is a compound for treatment of Myotonic Dystrophy type 1 having the formula: Wherein X is selected from the group consisting of O, N, C, or S, Y is a homo- or heteroatomic 5-membered ring comprising one or more atoms selected from the group consisting of N, O, S, and C, Z is an optionally substituted aryl group or optionally substituted heteroaryl, including but not limited to halogenated benzenes, pyridines, substituted benzene, substituted pyridine, R2=hydroxy, acyl, alkoxyl, esters, ethers, cyclic ethers, and lactones, R3=H, alkyl, an optionally substituted alkyl, aliphatic ether, ester, cyclic unsaturated and aromatic ring groups, and R1, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, alkyl, and alkoxyl or a pharmaceutically or cosmetically acceptable salt, solvate, or hydrate thereof.Type: ApplicationFiled: August 16, 2012Publication date: February 20, 2014Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Sita REDDY, Lucio Comai, Nouri Neamati
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Publication number: 20140045791Abstract: The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X and R are as defined herein. The compounds of formula (I) are useful as gyrase and/or topoisomerase IV inhibitors for treating bacterial infections. The compounds of formula (I) either possess a broad range of anti-bacterial activity and advantageous toxicological properties or are prodrugs of compounds having said activity.Type: ApplicationFiled: July 15, 2013Publication date: February 13, 2014Inventors: Christopher Phillip Locher, Youssef Laafiret Bennani, Ann-Laure Grillot, Hardwin O'Dowd, Emanuele Perola, Arnaud Le Tiran
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Patent number: 8648083Abstract: A method of treating diabetic hyperlipidemia or lipidemia with carbamoyloxy arylalkanoyl arylpiperazine compounds including:Type: GrantFiled: July 8, 2011Date of Patent: February 11, 2014Assignee: SK Biopharmaceuticals Co., Ltd.Inventors: Hong Sik Moon, Han Ju Yi, Eun Hee Chae, Sang Mi Chae, Hye Won Shin
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Publication number: 20140038921Abstract: A pharmaceutical composition for treating tuberculotic diseases with no side effect/low side effect is provided by the present invention, which pharmaceutically effective amount of one or more compounds chosen from isoniazid, rifampin, pyrazinamide and ethambutol, and pharmaceutically effective amount of substances which can reduce the side effect of the antituberculosis agents.Type: ApplicationFiled: April 20, 2011Publication date: February 6, 2014Applicant: NATIONAL DEFENSE EDUCATION AND RESEARCH FOUNDATIONInventors: Oliver Yaopu Hu, Tonho Young, Chenghuei Hsiong, Wenliang Chang, Tungyuan Shih, Hsintien Ho
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Publication number: 20140038945Abstract: The invention includes a compound of formula I: wherein R1, X, Z, n, and m have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds ate inhibitors of PDE4function and are useful for improving cognitive function in animals.Type: ApplicationFiled: July 31, 2013Publication date: February 6, 2014Applicant: DART NEUROSCIENCE (CAYMAN) LTDInventors: Terence P. Keenan, Alan P. Kaplan
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Publication number: 20140038979Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: October 14, 2013Publication date: February 6, 2014Applicant: Janssen Pharmaceutica NVInventors: Kristof VAN EMELEN, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noelle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviene Van Heusden
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Publication number: 20140018342Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.Type: ApplicationFiled: April 4, 2012Publication date: January 16, 2014Inventors: Wen-Lian Wu, Duane A. Burnett, William J. Greenlee
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Publication number: 20140005135Abstract: Disclosed is a stable liquid formulation for parenteral injection comprising a biocompatible non-aqueous solvent and a small molecule drug, or a salt thereof, solubilized within the non-aqueous solvent, wherein the liquid formulation comprises less than 10% by weight residual water, and wherein the volume of the liquid formulation to be parenterally injected is from 0.1 ?l to 3 ml.Type: ApplicationFiled: March 14, 2013Publication date: January 2, 2014Applicant: XERIS PHARMACEUTICALS, INC.Inventors: Steven J. Prestrelski, Nancy Scott
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Publication number: 20130345196Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. The glucuronidase inhibitors include phenoxy thiophene sulfonamides, and other compounds such as pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls. These compounds include nialamide, isocarboxazid, phenelzine, amoxapine, loxapine and mefloquine. Also compositions including one or more of such compounds for use in inhibiting glucuronidase and methods of using one or more of such compounds for selective inhibition of bacterial ?-glucuronidase. These compounds may be used as a co-drug in combination with the anticancer drug CPT-11. Also a method for screening compounds to determine their usefulness in reducing diarrhea associated with irinotecan chemotherapy.Type: ApplicationFiled: May 24, 2012Publication date: December 26, 2013Inventors: Alfred L. WILLIAMS, John Scott, Li-An Yeh, Matthew Robert Redinbo
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Publication number: 20130345195Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: August 23, 2013Publication date: December 26, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, Michael J. BURKE, Thomas Martin KIRRANE, Matthew Russell NETHERTON, Anil Kumar PADYANA, Lana Louise SMITH KEENAN, Hidenori TAKAHASHI, Michael Robert TURNER, QIANG ZHANG, Qing ZHANG
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Publication number: 20130345235Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. Glucuronidase inhibitors described include phenoxy thiophene sulfonamides. Other compounds, for instance pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls, are also contemplated. Also contemplated are compositions including one or more of such compounds for use inhibiting glucuronidase and methods of using one or more of such compounds as a co-drug to be used in combination with the anticancer drug CPT-11.Type: ApplicationFiled: March 10, 2011Publication date: December 26, 2013Applicants: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, NORTH CAROLINA CENTRAL UNIVERSITYInventors: Alfred L. Williams, John Scott, Li-An Yeh, Matthew Robert Redinbo
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Publication number: 20130337078Abstract: Particulate constructs stabilized by amphiphilic copolymers and comprising at least one active coupled to a hydrophobic moiety provide sustained release of the active in both in vitro and in vivo environments.Type: ApplicationFiled: August 16, 2013Publication date: December 19, 2013Applicants: THE TRUSTEES OF PRINCETON UNIVERSITY, CELATOR PHARMACEUTICALS, INC.Inventors: Lawrence D. MAYER, Robert K. PRUD'HOMME, Christine J. ALLEN, Walid S. SAAD
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Publication number: 20130336915Abstract: Particulate constructs stabilized by amphiphilic copolymers and comprising at least one active coupled to a hydrophobic moiety provide sustained release of the active in both in vitro and in vivo environments.Type: ApplicationFiled: May 29, 2013Publication date: December 19, 2013Inventors: Lawrence D. MAYER, Robert K. PRUD'HOMME, Christine J. ALLEN, Walid S. SAAD
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Publication number: 20130338059Abstract: This disclosure relates to methods for differentiating between mammals having active and latent Tuberculosis disease, by determining the percentage of polyfunctional CD4+ T-cells expressing TNF-alpha, IFN-gamma, and IL-2, or by determining expression of IL-17.Type: ApplicationFiled: December 22, 2011Publication date: December 19, 2013Applicant: Centre Hospitalier Universitaire VaudoisInventors: Giuseppe Pantaleo, Alexandre Harari, Matthieu Perreau
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Publication number: 20130331396Abstract: Certain piperazinyl and piperidinyl urea compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: ApplicationFiled: August 13, 2013Publication date: December 12, 2013Applicant: Janssen Pharmaceutica NVInventors: Richard Apodaca, J. Guy Breitenbucher, Kanaka Pattabiraman, mark Seierstad, Wei Xiao
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Treatment of Motor and Movement Disorder Side Effects Associated with Parkinson's Disease Treatments
Publication number: 20130331399Abstract: This invention provides methods of treating motor disorder side effects associated with the administration of levodopa to a subject having Parkinson's disease, by administering a dose of eltoprazine or a pharmaceutically acceptable acid addition salt thereof. In particular, the invention provides methods for reducing dyskinesia associated with Parkinson's disease treatments, and effective doses of eltoprazine or a pharmaceutically acceptable acid addition salt thereof.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Emer Leahy, Bavani Shankar -
Publication number: 20130302402Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.Type: ApplicationFiled: April 19, 2013Publication date: November 14, 2013Applicant: LIXTE BIOTECHNOLOGY, INC.Inventors: John S. KOVACH, Francis JOHNSON
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Publication number: 20130302253Abstract: Disclosed is a carrier for the local, targeted administration of a hydrophobic drug. The hydrophobic drug is rendered in to a hydrophilic prodrug thereof, and is contained in the lumen of a thermosensitive liposome or polymersome. Upon administration of the carrier, heat can be applied at the locus where the drug is to be released. After release of the prodrug, it will be activated so as to turn into the active drug.Type: ApplicationFiled: January 25, 2012Publication date: November 14, 2013Applicant: KONINKLIJKE PHILIPS N.V.Inventors: Holger Gruell, Sander Langereis, Charles Sio
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Publication number: 20130303437Abstract: The disclosure provides a molecular genetic approach of targeted mutagenesis and heterologous expression, coupled with in vitro and in vivo models of bacterial pathogenesis, to demonstrate that the S. aureus pigment is a virulence factor and potential novel target for antimicrobial therapy.Type: ApplicationFiled: July 16, 2013Publication date: November 14, 2013Inventors: Victor NIZET, George Y. LIU
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Publication number: 20130303544Abstract: The present invention provides a kind of benzopyrone compounds having a structure of formula (I) and the pharmaceutically acceptable salts or prodrugs thereof, and the pharmaceutical compositions containing such compounds, which can be used to regulate the novel estrogen receptor ER-a36, and prevent and/or treat the related diseases mediated by the ER-a36 receptor, such as cancers, etc.Type: ApplicationFiled: December 21, 2011Publication date: November 14, 2013Applicant: BEIJING SHENOGEN PHARMA GROUP LTD.Inventors: Hongxia Ding, Kun Meng, Jin Li
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Publication number: 20130303489Abstract: The present invention provides compounds, pharmaceutical compositions and methods for the treatment of specific cancers. Such compositions may generally comprise a compound of formula (I): wherein R1-R3 are as defined herein, or pharmaceutically acceptable salts or esters thereof; and a pharmaceutically acceptable carrier.Type: ApplicationFiled: March 11, 2013Publication date: November 14, 2013Applicant: Eisai R&D Management Co., Ltd.Inventors: Sergei Agoulnik, Bruce Decosta, Hong Du, Yimin Jiang, Xiang-Yi Li, Kenichi Nomoto, John (Yuan) Wang, Huiming Zhang
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Publication number: 20130296306Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (āABCā) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (āCFTRā). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: June 27, 2013Publication date: November 7, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
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Publication number: 20130296316Abstract: Disclosed is the use of mammalian target of rapamycin (mTOR) and/or phosphoinositide-3-kinase (PI3K) inhibitors as antiparasitic drugs, particularly in those parasitic infections caused by trypanosomatid parasites {Trypanosoma sp. and Leishmania sp.). These inhibitors are useful as trypanocides.Type: ApplicationFiled: July 11, 2011Publication date: November 7, 2013Inventors: Michael P. Pollastri, Miguel Navarro, Stephen Beverley, Ana Rodriguez
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Patent number: 8575161Abstract: The present invention relates to compounds of formula (I) wherein the substituents are as defined in the claims, including pharmaceutical compositions thereof and for their use in the treatment and/or prevention and/or amelioration of one or more symptoms of disease or disorders related to the activity of FXR. The invention is also directed to intermediates and to a method of preparation of compounds of formula (I).Type: GrantFiled: March 30, 2009Date of Patent: November 5, 2013Assignee: Merck Patent GmbHInventors: Didier Roche, GisĆØle Mautino, Ingo Kober, Francis Contard, Serge Christmann-Franck, Saumitra Sengupta, Ramesh Sistla, Gummadi Venkateshwar Rao
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Publication number: 20130288951Abstract: Infection-inhibiting compositions suitable for coating surfaces of implantable medical implants, including compositions and devices for coating medical devices in the operating room prior to implantation in a patient. Methods for inhibiting infection at the site of implantation of an orthopedic device in a human or animal subject, comprise rubbing a surface of the device, prior to implantation, with an infection-inhibiting composition having a waxy matrix comprising an infection-inhibiting material selected from the group consisting of a lipid, an antimicrobial agent, and mixtures thereof, wherein a thin layer of the infection-inhibiting material is deposited on the surface of the device. Medical implants which may be treated in the methods of this technology include orthopedic implants. Lipids include long-chain diacylglycerides or triacylglycerides, which may be saturated or unsaturated, such as lecithin or a purified form of phosphatidylcholine.Type: ApplicationFiled: April 26, 2013Publication date: October 31, 2013Applicant: BIOMET MANUFACTURING CORP.Inventors: Karen S. TROXEL, Michael PONTICIELLO, Troy W. HERSHBERGER
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Publication number: 20130280210Abstract: Disclosed herein are methods of inhibiting proliferation of a cancer cell or inducing apoptosis of a cancer cell, which does not overexpress NāCoR. Also disclosed herein are methods of inhibiting proliferation or inducing apoptosis of a cancer cell that overexpresses TCTP and methods for determining whether a compound is effective in inducing cell death.Type: ApplicationFiled: April 25, 2013Publication date: October 24, 2013Inventor: John S. Kovach
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Patent number: 8563582Abstract: The present invention is directed to compounds of Formula I: which are modulators of chemokine receptors. The compounds of the invention, and compositions thereof, are useful in the treatment of diseases related to chemokine receptor expression and/or activity.Type: GrantFiled: April 29, 2009Date of Patent: October 22, 2013Assignee: Incyte CorporationInventors: Chu-Biao Xue, Changsheng Zheng, Hao Feng, Michael Xia, Joseph Glenn, Ganfeng Cao, Brian W. Metcalf
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Publication number: 20130274212Abstract: The present invention relates to sesterterpene compounds, to the precursors thereof that are hydrolysable in a living body, or to the pharmaceutically acceptable salts thereof, and also relates to the prevention and treatment efficacy of the sesterterpene compounds with respect to non-insulin dependent diabetes mellitus, diabetic complications (renal failure and foot ulcers caused by diabetes), alcoholic, non-alcoholic, and viral fatty liver diseases, obesity, hyperlipidemia, atherosclerosis, cardiovascular diseases such as atherosclerotic stroke, and cerebropathies (Parkinsonism, schizophrenia and Alzheimer's disease). In addition, the present invention relates to compositions for functional foods, functional beverages, functional cosmetics, and functional feed.Type: ApplicationFiled: September 7, 2011Publication date: October 17, 2013Applicant: SNU R&DB FOUNDATIONInventors: Heon Joong Kang, Dong Hwan Won, In Ho Yang, Eun Oh Kim, Jung Ah Kim, Awadut Gajendra Giri, Venkat Reddy Mallepally
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Patent number: 8557808Abstract: Compounds, compositions and methods are provided that comprise selective ?-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ?-glucuronidases and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ?-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds.Type: GrantFiled: December 9, 2010Date of Patent: October 15, 2013Assignees: North Carolina Central University, The University of North Carolina at Chapel Hill, Albert Einstein College of Medicine of Yeshiva UniversityInventors: Matthew R. Redinbo, Sridhar Mani, Alfred Williams, John Scott, Li-An Yeh, Bret David Wallace, Kimberly Terry Lane
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Publication number: 20130267538Abstract: The invention relates the method of treatment or amelioration of mitochondrial disorders such as Alzheimer's disease, Parkinson's disease, Friedreich's ataxia (FRDA), cerebellar ataxias, Leber's hereditary optic neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, stroke (MELAS), Myoclonic Epilepsy with Ragged Red Fibers (MERFF), amyotrophic lateral sclerosis (ALS), motor neuron diseases, Huntington's disease, macular degeneration, and epilepsy, with chroman derivatives of Formula I or Formula II as described herein.Type: ApplicationFiled: April 24, 2013Publication date: October 10, 2013Inventors: Gail WALKINSHAW, Sekhar BODDUPALLI, Bing WANG, Guy M. MILLER
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Patent number: 8546402Abstract: The present invention relates to chromone derivatives, their preparation, their pharmaceutical compositions and their application as D3 dopaminergic ligands as a medicament for disorders of the central nervous system.Type: GrantFiled: August 31, 2010Date of Patent: October 1, 2013Inventors: Pierre Sokoloff, Thierry Imbert, Ludovic Leriche, Jean-FranƧois Patoiseau, Jean-Pierre Rieu
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Patent number: 8546376Abstract: 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: GrantFiled: September 17, 2010Date of Patent: October 1, 2013Assignee: Almac Discovery LimitedInventors: Mark Peter Bell, Timothy Harrison, Sumita Bhattacharyya, James Samuel Shane Rountree, Frank Burkamp, Stephen Price, Calum MacLeod, Richard Leonard Elliott, Phillip Smith, Toby Jonathan Blench, Colin Roderick O'Dowd, Lixin Zhang, Graham Peter Trevitt, Hazel Joan Dyke
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Patent number: 8541409Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.Type: GrantFiled: April 30, 2008Date of Patent: September 24, 2013Assignee: SK Biopharmaceuticals Co., Ltd.Inventors: Byong Sung Kwak, Hong Sik Moon, Han Ju Yi, Young Soon Kang, Dae Joong Im, Eun Hee Chae, Sang Mi Chae, Ki Ho Lee
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Publication number: 20130244996Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: March 5, 2013Publication date: September 19, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, Steven Richard BRUNETTE, Michael J. BURKE, Suresh R. KAPADIA, Thomas Martin KIRRANE, Matthew Russell NETHERTON, Hossein RAZAVI, Sonia RODRIGUEZ, Anjan SAHA, Robert SIBLEY, Lana Louise SMITH-KEENAN, Hidenori TAKAHASHI, Michael Robert TURNER, Jiang-Ping WU, Erick Richard Roush YOUNG, Qiang ZHANG, Qing ZHANG, Renee M. ZINDELL
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Publication number: 20130245010Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (āABCā) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (āCFTCā). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: April 26, 2013Publication date: September 19, 2013Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Publication number: 20130236534Abstract: Drug derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drug derivatized with a weak-base moiety that facilitates active loading of the drug through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drug to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drug derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drugs.Type: ApplicationFiled: April 19, 2013Publication date: September 12, 2013Inventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
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Patent number: 8529935Abstract: The present invention relates to hydrogels endowed with antibacterial properties, to be used for injection in damaged bones or in the production of antibacterial coatings of prostheses for implant in the human or animal body, obtained by loading with antibacterial agents hydrogels formed by derivatives of hyaluronic acid; the invention also relates to a kit of parts for producing the antibacterial hydrogels.Type: GrantFiled: January 29, 2010Date of Patent: September 10, 2013Assignees: Mero S.R.L., Novagenit S.R.L.Inventors: Gaetano Giammona, Giovanna Pitarresi, Fabio Palumbo, Carlo Luca Romano, Enzo Meani, Edgardo Cremascoli
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Publication number: 20130230582Abstract: Drug derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drug derivatized with a weak-base moiety that facilitates active loading of the drug through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drug to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drug derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drugs.Type: ApplicationFiled: April 19, 2013Publication date: September 5, 2013Inventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
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Publication number: 20130230583Abstract: Drug derivatives are provided herein which are suitable for loading into liposomal nanoparticle carriers. In some preferred aspects, the derivatives comprise a poorly water-soluble drug derivatized with a weak-base moiety that facilitates active loading of the drug through a LN transmembrane pH or ion gradient into the aqueous interior of the LN. The weak-base moiety can optionally comprise a lipophilic domain that facilitates active loading of the drug to the inner monolayer of the liposomal membrane. Advantageously, LN formulations of the drug derivatives exhibit improved solubility, reduced toxicity, enhanced efficacy, and/or other benefits relative to the corresponding free drugs.Type: ApplicationFiled: April 19, 2013Publication date: September 5, 2013Inventors: Pieter Cullis, Marcel Bally, Marco Ciufolini, Norbert Maurer, Igor Jigaltsev
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Publication number: 20130225561Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.Type: ApplicationFiled: October 21, 2011Publication date: August 29, 2013Inventors: Haifeng Tang, Alexander Pasternak, Lihu Yang, Shawn P. Walsh, Barbara Pio, Aurash Shahripour, Nardos Teumelsan
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Patent number: 8518949Abstract: Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin ? and rifaximin ? useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.Type: GrantFiled: June 4, 2012Date of Patent: August 27, 2013Assignee: ALFA Wassermann S.p.A.Inventors: Giuseppe Claudio Viscomi, Manuela Campana, Donatella Confortini, Maria Miriam Barbanti, Dario Braga
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Patent number: 8518450Abstract: The invention provides a process for the production of nanoparticle carriers for drug delivery, said nanoparticles being produced by preparing a double emulsion of water-oil-water including one or more polymer which forms the basis of the nanoparticle carrier, blending the drug to be delivered into one of the emulsion phases, doping either the oil-phase or the outer-water phase with a carbohydrate, and spray drying the emulsion to form nanoparticles of a narrow particle size distribution of 100 nm to 1000 nm, which nanoparticles are substantially spherical.Type: GrantFiled: August 17, 2010Date of Patent: August 27, 2013Assignee: CSIRInventor: Lonji Kalombo
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Publication number: 20130209522Abstract: In some embodiments, the invention provides an implant comprising a uniform mixture of degradable polymer, bone, and a drug. In some embodiments, the drug comprises an antibiotic. In some embodiments, diffusion of the drug from the implant at a therapeutic level is maintained for an amount of time longer than an amount of time that a pathogen is senescent. In some embodiments, diffusion of the drug from the implant at a therapeutic level is maintained for at least eight weeks, or at least ten weeks, or at least twelve weeks post-implantation. In some embodiments, the therapeutic level is maintained at an implantation site of the implant. In some embodiments, the implant is a solid, a paste, or a liquid. In some embodiments, the solid implant is carved or molded for insertion into a site of implantation in a vertebrate host prior to implantation. In some embodiments, the paste implant hardens following implantation. In some embodiments, the liquid implant is used to coat a prosthesis (e.g.Type: ApplicationFiled: February 5, 2013Publication date: August 15, 2013Applicant: UNIVERSITY OF UTAH RESEARCH FOUNDATIONInventor: UNIVERSITY OF UTAH RESEARCH FOUNDATION
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Publication number: 20130202663Abstract: It is intended to provide a remedy for diseases caused by macrophages with dysfunction or mediated by macrophages. Namely, a remedy which activates the phagocytic capacity of macrophages and thus is efficiently incorporated into the macrophages due to the vigorous phagocytosis. As a result, the macrophages with dysfunction are normalized, macrophages infected with a pathogen are exterminated or a pathogen in the infected macrophages is exterminated.Type: ApplicationFiled: March 14, 2013Publication date: August 8, 2013Inventor: Hiroshi Terada
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Patent number: 8501744Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein one of R1 and R2 is H, and the other is selected from C1-8-alkyl, C3-6-cycloalkyl and C1-8-alkyl-C5-10-aryl; R3 is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl, cyclohexyl and 1-methylcyclopentyl; R9 is selected from the following: wherein: R4 is selected from C1-8-alkyl and C3-8-cycloalkyl; G is selected from: CH, CMe and N; E is selected from: O, S, SO2, NH, NMe and N-oxide (N?O); J and R are independently selected from: CH, N and N-oxide (N?O); and R41 is selected from amino, methylamino, dimethylamino, isopropylamino, isopropyl(methyl)amino, cyclopropylamino, cyclopropyl(methyl)amino, cyclopentylamino, morpholino, piperidin-1-yl, piperidin-1-ylmethyl, morpholinomethyl, 4-methylpiperazin-1-yl, 4-(2-methoxyethyl)piperazin-1-yl, 1-morpholinoethyl, 1-(dimethylamino)ethyl, 1-(methylamino)ethyl, 4-fluoro-1-methylpyrrolidin-2-yl, 4,4-difluoropiperidin-1Type: GrantFiled: June 25, 2010Date of Patent: August 6, 2013Assignee: Amura Therapeutics, LimitedInventors: Martin Quibell, John Paul Watts
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Publication number: 20130196987Abstract: The present invention provides compounds, methods for the synthesis thereof and methods for the use thereof in the treatment of various disorders including inflammatory or autoimmune disorders, and disorders involving malignancy or increased angiogenesis.Type: ApplicationFiled: October 30, 2012Publication date: August 1, 2013Applicant: EISAI CO., LTD.Inventors: Roch Boivin, Kenichi Chiba, Jesse Chow, Hong Du, Yoshihito Eguchi, Masanori Fujita, Masaki Goto, Fabian Gusovsky, Jean-Christophe Harmange, Atsushi Inoue, Yimin Jiang, Megumi Kawada, Takatoshi Kawai, Yoshiyuki Kawakami, Akifumi Kimura, Makoto Kotake, Yoshikazu Kuboi, Charles-Andre Lemelin, Xiang-Yi Li, Tomohiro Matsushima, Yoshiharu Mizui, Kenzo Muramoto, Hideki Sakurai, Yong-Chun Shen, Hiroshi Shirota, Mark Spyvee, Isao Tanaka, John (Yuan) Wang, Satoshi Yamamoto, Naoki Yoneda
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Publication number: 20130183236Abstract: The present invention provides targeted delivery compositions and methods of using the compositions for treating and diagnosing a disease state in a subject.Type: ApplicationFiled: November 29, 2012Publication date: July 18, 2013Applicant: Mallinckrodt Inc.Inventor: Mallinckrodt Inc.