Oxygen Double Bonded And Acyclic Nitrogen Bonded Directly To The Same Carbon Patents (Class 544/168)
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Patent number: 11358975Abstract: Provided is an efficient and effective process for preparing certain organotin compounds having alkyl and alkylamino substituents. The process provides the organotin compounds in a highly pure crystalline form which are particularly useful as precursors in the deposition of high-purity tin oxide films in, for example, extreme ultraviolet light (EUV) lithography techniques used in the manufacture of certain microelectronic devices.Type: GrantFiled: July 2, 2021Date of Patent: June 14, 2022Assignee: ENTEGRIS, INC.Inventors: David M. Ermert, Thomas M. Cameron, David Kuiper, Thomas H. Baum
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Patent number: 10537545Abstract: The invention provides a compound of formula (I): (I) wherein R1-R4 have any of the values defined in the specification, as well as compositions comprising a compound of formula (I) and methods for treating diseases (e.g. cancer).Type: GrantFiled: July 19, 2016Date of Patent: January 21, 2020Assignee: Rutgers, The State University of New JerseyInventors: Richard Lutz, Eric Andrianasolo, Paul Falkowski, Eileen White, Liti Haramaty
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Patent number: 10100012Abstract: The present invention relates to novel compounds of formula (1): The present invention also discloses compounds of formula (1) along with other pharmaceutical acceptable excipients and use of the compounds as anti-tubercular agents.Type: GrantFiled: June 1, 2015Date of Patent: October 16, 2018Assignees: SPHAERA PHARMA PVT. LTD., DRUG DISCOVERY RESEARCH CENTREInventors: Sundeep Dugar, Dinesh Mahajan, Santosh Kumar Rai, Kanury Rao, Varshneya Singh
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Patent number: 9475854Abstract: A novel method of preventing or reducing ototoxicity in vertebrates undergoing treatment with therapeutically effective amounts of platinum-based chemotherapeutic agents such as cisplatin or aminoglycoside antibiotics is disclosed herein. The method(s) comprise administering an effective amount of an otoprotective agent comprising Dihexa prior to, concomitantly with, or subsequently to administration of the platinum-based chemotherapeutic agent or aminoglycoside antibiotic.Type: GrantFiled: May 22, 2015Date of Patent: October 25, 2016Assignee: Washington State UniversityInventors: Allison Coffin, Joseph Harding, Leen Kawas, Phillip Uribe
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Publication number: 20150051144Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation. The present invention is directed towards compounds which can be used to treat diseases such as hyperlipidemia and also have a beneficial effect on cholesterol.Type: ApplicationFiled: September 26, 2012Publication date: February 19, 2015Inventors: Harikishore Pingali, Vrajesh Pandya
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Publication number: 20150038493Abstract: The present invention relates to a series of molecules derived from 2,3-diaminopropionic acid (DAP), comprising or not comprising an 8-hydroxyquinoline (8-HQ) motif, and to the use of said molecules for trapping an alpha-oxoaldehyde resulting particularly from the degradation of the glucose or for trapping an alpha-beta-unsaturated aldehyde, resulting particularly from the oxidative degradation of fatty acids. These molecules can have a further application in the fields of cosmetics, food processing, and pharmaceuticals.Type: ApplicationFiled: October 5, 2012Publication date: February 5, 2015Inventors: Guy Potier, André Nobumichi Sasaki, Nicolas Audic
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Publication number: 20150031878Abstract: The invention provides derivatives of DEA which have increased potency and hydrolysis resistance as compared to DEA, and compositions thereof, as well as methods of using these derivatives to promote neurogenesis, neurite growth and/or length, and/or promote synaptogenesis.Type: ApplicationFiled: March 15, 2013Publication date: January 29, 2015Inventors: Hee-Yong Kim, Juan Jose Marugan, Erika E. Englund, Samarjit Patnaik
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Publication number: 20140378459Abstract: [Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.Type: ApplicationFiled: September 14, 2012Publication date: December 25, 2014Applicant: ASTELLAS PHARMA INC.Inventors: Jiro Fujiyasu, Kazuhiko Ohne, Susumu Yamaki, Tomoyoshi Imaizumi, Takeshi Hondo, Keisuke Matsuura, Tomohki Satou, Satoshi Sasamura
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Patent number: 8916556Abstract: Methods and compounds for treating neurodegenerative and other disorders. Included is the administering to a subject in need thereof an effective amount of a compound having binding specificity for a p75NTR receptor molecule. Enhanced survival of neural and other cells has been observed.Type: GrantFiled: April 19, 2010Date of Patent: December 23, 2014Assignees: The University of North Carolina at Chapel Hill, The Regents of The University of California, The United States of America represented by the Department of Vetran AffairsInventors: Frank M. Longo, Stephen M. Massa
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Patent number: 8901295Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: GrantFiled: February 21, 2014Date of Patent: December 2, 2014Assignees: Institut National de la Sante et de la Recherche Medicale (INSERM), Universite Montpellier 1, Universite Paris-EST Creteil val de Marne, Assistance Publique-Hopitaux de Paris, Centre National de la Recherche ScientifiqueInventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
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Publication number: 20140296240Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: June 17, 2014Publication date: October 2, 2014Inventors: Gary Mark COPPOLA, Yuki IWAKI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Gary Michael KSANDER, Muneto MOGI, Robert SUN
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Publication number: 20140256698Abstract: The present invention is directed to inhibitors of cathepsins and the methods for using and making such inhibitors.Type: ApplicationFiled: March 11, 2014Publication date: September 11, 2014Inventors: Robert Booth, Jeff Dener, Michael Green
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Patent number: 8802666Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: GrantFiled: December 21, 2010Date of Patent: August 12, 2014Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
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Publication number: 20140179687Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: ApplicationFiled: February 21, 2014Publication date: June 26, 2014Applicant: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michael Pawlotsky
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Publication number: 20140128335Abstract: The present invention relates to the use of polyaminoisoprenyl derivatives in antibiotic or antiseptic treatment of bacteria including those presenting multiple drug resistance (MDR), in particular as efflux pump inhibitors. It also relates to novel polyaminoisoprenyl derivatives, compositions comprising the same, process for preparing the same, and use thereof in antibiotic or antiseptic treatment.Type: ApplicationFiled: February 23, 2012Publication date: May 8, 2014Applicants: UNIVERSITE D'AIX-MARSEILLE, UNIVERSITE DE CORSE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Jean-Michel Bolla, Jean Michel Brunel, Joseph Pierre Felix Casanova, Vannina Lorenzi, Liliane Berti
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Publication number: 20140116293Abstract: The present invention relates to a cellulose acetate film for optical compensation and a retardation enhancer used therein, and relates to a cellulose acetate film which has a high retardation value in the thickness direction (Rth).Type: ApplicationFiled: June 20, 2012Publication date: May 1, 2014Applicant: SK INNOVATION CO., LTD.Inventors: Won Yeob Kim, Min Joung Im, Seung Eon Lee, Hyo Shin Kwak, Myoung Lae Kim, Yong Gyun Cho
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Publication number: 20140100224Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.Type: ApplicationFiled: June 26, 2013Publication date: April 10, 2014Applicants: The University of North Carolina at Chapel Hill, U.S. Government represented by the Department of Veterans Affairs, The Regents of the University of CaliforniaInventors: Frank M. Longo, Stephen M. Massa
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Patent number: 8686184Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, 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: GrantFiled: May 18, 2012Date of Patent: April 1, 2014Assignee: Theravance, Inc.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
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Publication number: 20140081017Abstract: The present invention relates to compositions and methods to selectively treat fungal infection. More particularly, the invention relates to compounds, compositions thereof, and methods for selectively enhancing fungal sensitivity to antifungal compounds.Type: ApplicationFiled: March 14, 2013Publication date: March 20, 2014Applicant: METHYLGENE INC.Inventor: METHYLGENE INC.
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Publication number: 20130345213Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors of Formula (I).Type: ApplicationFiled: March 9, 2012Publication date: December 26, 2013Applicant: LUPIN LIMITEDInventors: Manojkumar Ramprasad Shukla, Vinod Dinkar Chaudhari, Majid Bashir Sayyed, Ramesh Dattatraya Phadtare, Navnath Bajirao Walke, Sanjeev Anant Kulkarni, Venkata P. Palle, Rajender Kumar Kamboj
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Publication number: 20130310383Abstract: Compounds of the formula where the variables have the meaning defined in the specification have analgesic and/or immunostimulant effect in mammals.Type: ApplicationFiled: July 24, 2013Publication date: November 21, 2013Applicant: Allergan, Inc.Inventors: Bertrand Leblond, Eric Beusoleil, Thierry Taverne, John E. Donello
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Publication number: 20130289034Abstract: Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.Type: ApplicationFiled: June 21, 2013Publication date: October 31, 2013Inventors: Orion D. JANKOWSKI, Kieron E. WESSON, Paul MOLLARD, William D. SHRADER
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Publication number: 20130261041Abstract: The present invention relates to specific acylhydrazone compounds, their use as oxidation catalysts and to a process for removing stains and soil on textiles and hard surfaces. The compounds are substituted with a specific cyclic ammonium group adjacent to the acyl group. Further aspects of the invention are compositions or formulations comprising such compounds.Type: ApplicationFiled: December 8, 2011Publication date: October 3, 2013Applicants: HENKEL AG & CO. KGAA, BASF SEInventors: Hauke Rohwer, Barbara Wagner, Frederique Wendeborn, Katherina Misteli
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Patent number: 8450525Abstract: Novel compounds of the general formula (I), having histone deacetylase (HDAC) inhibiting enzymatic activity, their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. The present invention more particularly provides novel compounds of the general formula (I). Also included is a method for treatment of cancer, psoriasis, proliferative conditions and conditions mediated by HDAC, in a mammal comprising administering an effective amount of a novel compound of formula (I).Type: GrantFiled: October 21, 2008Date of Patent: May 28, 2013Assignee: Orchid Chemicals & Pharmaceuticals LimitedInventors: Sridharan Rajagopal, Virendra Kachhadia, Thanasekaran Ponpandian, Abdul Raheem Keeri, Karnambaram Anandhan, Sriram Rajagopal, Rajendran Praveen, Prabhu Daivasigamani
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Publication number: 20130109853Abstract: Disclosed is a synthesis method of a compound of formula 1,5-[[2(R)-[1(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxyl]-3(S)-4-fluorophenyl-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazole-3-one (i.e. aprepitant), which comprises cyclizing a compound of formula 4 in a solvent, wherein R is C1-C5 alkyl. The intermediate for preparing aprepitant is also disclosed. The present method is especially suitable for industrial production of aprepitant.Type: ApplicationFiled: May 20, 2011Publication date: May 2, 2013Inventors: Jianxin Ji, Qiang Zhang, Fengtian Du, Yi Jin, Tao Zhang, Na Guo, Xiaowei Yan, Yongrong Yang, Bogang Li
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Publication number: 20130096127Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 29, 2012Publication date: April 18, 2013Applicant: NOVARTIS AGInventor: NOVARTIS AG
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Publication number: 20130089624Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: wherein the variables are as defined herein. Additionally, the present invention also relates to novel processes for the production of various morpoholine based intermediates.Type: ApplicationFiled: September 28, 2012Publication date: April 11, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jean-Damien Charrier, Stephen Clinton Young, Christopher John Davis, John Studley
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Publication number: 20130079514Abstract: (R)-2-Arylpropionamide compounds of formula (I), pharmaceutical preparations of the compounds and a process for making the compounds are described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonuclear leukocytes and monocytes at inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use as inhibitors of chemotaxis of neutrophils and monocytes induced by the C5a fraction of complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of neutrophils and monocytes and the IL-8-induced chemotaxis of polymorphonuclear leukocytes.Type: ApplicationFiled: October 15, 2012Publication date: March 28, 2013Applicant: Dompé S.p.A.Inventor: Dompé S.p.A.
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Publication number: 20130018044Abstract: The present invention relates to a compound of formula (I): wherein: n is 0, 1 or 2; A is in particular CH or N; X is in particular CO, SO2, CS, and R1 is in particular H, R2 is a group of formula NR3R4 or OR5, R3 and R4 being in particular H, and R5 an alkyl group, R6 is in particular H or an alkyl group, and R7 is in particular an aryl group, for its use in the prevention and/or the treatment of viral pathologies or infections.Type: ApplicationFiled: December 21, 2010Publication date: January 17, 2013Inventors: Jean-Francois Guichou, Lionel Colliandre, Hakim Ahmed-Belkacem, Jean-Michel Pawlotsky
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Publication number: 20130005731Abstract: The present invention includes crystalline forms of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide and crystalline forms of salts and/or solvates of 2-amino-3-methyl-N-(2-morpholinoethyl)-pentanamide. Furthermore, the present invention provides compositions comprising the crystalline forms and therapeutic use of the crystalline forms.Type: ApplicationFiled: November 12, 2010Publication date: January 3, 2013Applicant: Pharmatrophix, Inc.Inventors: Rajgopal Munigeti, Frank M. Longo
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Patent number: 8343971Abstract: This application relates to pharmacologically-active vanilloid compounds which are useful for the treatment of various anti-inflammatory states characterized by inhibition of FAAH, such as, Alzheimer's dementia, Parkinson's disease, depression, pain, rheumatoid arthritis, pathophysiology of mood disorders, multiple sclerosis, and inflammation, or antagonism of TRPV1, such as, for example, Huntington's disease, hypertension, arthritis, allergic airway inflammation, Crohn's disease, ulcerative colitis, and neuropathic pain.Type: GrantFiled: September 15, 2010Date of Patent: January 1, 2013Assignees: Rutgers, The State University of New Jersey, The University of Medicine and Dentistry of New Jersey, Lehigh UniversityInventors: Jeffrey D. Laskin, Diane E. Heck, Carl Jeffrey Lacey, Erik Aponte, Mou-Tuan Huang, Ned D. Heindel
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Publication number: 20120322799Abstract: The present application is related to deuterated compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders involving degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such deuterated compounds.Type: ApplicationFiled: November 30, 2010Publication date: December 20, 2012Applicant: PHARMATROPHIX, INC.Inventor: Gopal Damodara
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Publication number: 20120308588Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, 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: 20120214785Abstract: The invention relates to new compounds of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: August 17, 2011Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Gerald Juergen ROTH, Martin FLECK, Niklas HEINE, Joerg KLEY, Thorsten LEHMANN-LINTZ, Heike NEUBAUER, Bernd NOSSE
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Patent number: 8242175Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.Type: GrantFiled: December 7, 2010Date of Patent: August 14, 2012Assignee: DAC S.R.L.Inventors: Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Pier Giuseppe Pelicci, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
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Publication number: 20120114633Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.Type: ApplicationFiled: April 6, 2010Publication date: May 10, 2012Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams
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Publication number: 20120095220Abstract: The invention relates to a continuous method for producing amides of aliphatic carboxylic acids by reacting at least one carbonic acid ester of formula (I) R3—COOR4 (I), wherein R3 represents hydrogen or an optionally substituted aliphatic hydrocarbon group with 1 to 100 carbon atoms and R4 represents a hydrocarbon group with 1 to 30 carbon atoms, or wherein R3 and R4 form an optionally substituted ring with 5, 6 or 7 ring members, with at least one amine of formula (II) HNR1R2 (II), wherein R1 and R2 independently represent hydrogen or a hydrocarbon group with 1 to 100 C atoms, in a reaction tube the longitudinal axis of which extends in the direction of propagation of the microwaves of a monomode microwave applicator, under microwave irradiation to form carboxamide.Type: ApplicationFiled: June 9, 2010Publication date: April 19, 2012Applicant: CLARIANT FINANCE (BVI) LIMITEDInventors: Matthias Krull, Roman Morschhaeuser
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Publication number: 20120059007Abstract: This application relates to pharmacologically-active vanilloid compounds which are useful for the treatment of various anti-inflammatory states characterized by inhibition of FAAH, such as, Alzheimer's dementia, Parkinson's disease, depression, pain, rheumatoid arthritis, pathophysiology of mood disorders, multiple sclerosis, and inflammation, or antagonism of TRPV1, such as, for example, Huntington's disease, hypertension, arthritis, allergic airway inflammation, Crohn's disease, ulcerative colitis, and neuropathic pain.Type: ApplicationFiled: September 15, 2010Publication date: March 8, 2012Inventors: Jeffrey D. Laskin, Diane E. Heck, Carl Jeffrey Lacey, Erik Aponte, Mou-Tuan Huang, Ned D. Heindel
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Publication number: 20110288094Abstract: Compounds of the formula where the variables have the meaning defined in the specification have analgesic and/or immunostimulant effect in mammals.Type: ApplicationFiled: August 2, 2011Publication date: November 24, 2011Applicant: ALLERGAN, INC.Inventors: Bertrand Leblond, Eric Beusoleil, Thierry Taverne, John E. Donello
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Publication number: 20110281872Abstract: The invention relates to compositions and methods for the treatment and prevention of cancer and other cell proliferative disorders.Type: ApplicationFiled: March 11, 2011Publication date: November 17, 2011Applicant: Kinex Pharmaceuticals, LLCInventors: David G. Hangauer, JR., Michael J. Ciesielski, Robert A. Fenstermaker
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Patent number: 8058273Abstract: New inhibitors of histone deacetylases having antitumor activity, and the process of preparation thereof are herein described. These compounds belong to the structural formula (I) where R1 is a linear or branched chain containing at least two conjugated double bonds, A is an optionally substituted phenyl or pyridyl ring, Ar is an aryl or heteroaryl group, and R3 is hydrogen or alkoxyalkyl. The application also describes the use of said compounds in the treatment of diseases associated to the deregulation of histone deacetylases activity, such as tumors, as well as the relevant pharmaceutical compositions for administration to patients requiring said treatment.Type: GrantFiled: June 1, 2010Date of Patent: November 15, 2011Assignee: DAC S.R.L.Inventors: Saverio Minucci, Pier Giuseppe Pelicci, Antonello Mai, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
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Publication number: 20110251196Abstract: The present disclosure is generally directed to compounds which can modulate G-protein coupled receptor 88, compositions comprising such compounds, and methods for modulating G-protein coupled receptor 88.Type: ApplicationFiled: October 5, 2010Publication date: October 13, 2011Inventors: Carolyn Diane Dzierba, Richard A. Hartz, Yingzhi Bi, Vijay T. Ahuja, Joanne J. Bronson, Kenneth Carson, Giovanni Cianchetta, Michael Green, David Kimball, S. Roy Kimura, Soojin Kwon, John E. Macor, Yulian Zhang, Greg Zipp
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Publication number: 20110245243Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of Cathepsin S.Type: ApplicationFiled: June 16, 2011Publication date: October 6, 2011Inventors: Hong LIU, David C. TULLY, Arnab CHATTERJEE, Phillip B. ALPER, David H. WOODMANSEE, Daniel MUTNICK
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Publication number: 20110230428Abstract: Certain chemical entities are provided herein. Pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: ApplicationFiled: July 22, 2009Publication date: September 22, 2011Inventors: John Wityak, Leticia M. Toledo-sherman, Celia Dominguez, Stephen Martin Courtney, Christopher John Yarnold, Paula C. De Aguiar Pena, Andreas Scheel, Dirk Winkler
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Publication number: 20110230479Abstract: The present application is related to compounds which are novel neurotrophin mimetics. The application also discloses the treatment of disorders associated with p75 expression, such as degradation or dysfunction of cells expressing p75 in a mammal by administering an effective amount of such compounds.Type: ApplicationFiled: October 22, 2010Publication date: September 22, 2011Inventors: Frank M. Longo, Stephen M. Massa
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Publication number: 20110224213Abstract: The invention relates to the use of glutaric acid derivatives of general formula (I), which are disclosed in the invention description, as anti-arrhythmic agents.Type: ApplicationFiled: March 18, 2009Publication date: September 15, 2011Inventors: Vladimir Evgenievich Nebolsin, Dmitry Sergeevich Blinov, Vladimir Pavlovich Balashov, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina
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Publication number: 20110178088Abstract: This invention relates to tetrahydro-naphthalene derivatives and salts thereof which are useful as an active ingredient of pharmaceutical preparations. The tetrahydro-naphthalene derivatives of the present invention have excellent activity as VR1 antagonist and useful for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urinary incontinence, overactive bladder, urge urinary incontinence, chronic pain, neuropathic pain, post-operative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, inflammatory disorders, asthma and COPD.Type: ApplicationFiled: March 21, 2011Publication date: July 21, 2011Applicant: XENTION LIMITEDInventors: Masaomi Tajimi, Toshio Kokubo, Masahiro Shiroo, Yasuhiro Tsukimi, Takeshi Yura, Klaus Urbahns, Noriyuki Yamamoto, Muneto Mogi, Hiroshi Fujishima, Tsutomu Masuda, Nagahiro Yoshida, Toshiya Moriwaki
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Publication number: 20110166141Abstract: Cathepsin S inhibitors having formula (I), (II), (III) or (IV) as shown in the specification. These inhibitors can be used to treat cancer and autoimmune/inflammatory diseases.Type: ApplicationFiled: December 6, 2010Publication date: July 7, 2011Applicants: DCB-USA, LLC, National Tsing Hua University, National Health Research InstitutesInventors: Chun-Cheng Lin, Wun-Shaing Wayne Chang, Biing-Jiun Uang, Jang-Yang Chang, Jo-Chun Chen, Hsing-Pang Hsieh
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Publication number: 20110082109Abstract: The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na+/H+ exchanger type 3) and effectively improves diseases or conditions of organs in which NHE3 is expressed.Type: ApplicationFiled: October 1, 2010Publication date: April 7, 2011Applicant: AJINOMOTO CO., INC.Inventors: Wataru MIYANAGA, Yoichiro Shima, Misato Noguchi, Akiko Oonuki, Yayoi Kawato, Hiroshi Iwata, Eri Harada, Ryuta Takashita, Hirokazu Ueno, Tadakiyo Nakagawa
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Publication number: 20110077247Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.Type: ApplicationFiled: December 7, 2010Publication date: March 31, 2011Applicant: DAC S.r.I.Inventors: Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Pier Giuseppe Pelicci, Marco Ballarini, Gaetano Gargiulo, Silvio Massa