Nitrogen Containing Patents (Class 514/471)
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Publication number: 20110065710Abstract: Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re, Rf, Rg, Rh, R5, d, e, U, V, X, WR6 and R7 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: December 2, 2004Publication date: March 17, 2011Inventors: David M. Roush, John F. Chiarello, Jianming Yu, Benjamin J. Dugan, George Theodoridis, Manorama M. Patel, Walter H. Yeager, Steven W. Szczepanski
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Patent number: 7906535Abstract: A topical insecticide preparation is provided which can be safe to use and avoids many common deleterious side effects of conventional topical insecticides. The topical insecticide contains a combination of a first pyrethroid insecticide effective for killing fleas, a second pyrethroid insecticide effective for killing ticks, and an insect growth regulator (IGR). The topical insecticide preparation can be packaged together or packaged so that the first and second pyrethroid insecticides are stored separately prior to administration of the insecticide preparation to the animal. The combination of the first and second pyrethroid insecticides with an insect growth regulator results in an insecticide preparation formulated to have enhanced insecticidal activity against fleas and ticks compared to the effectiveness of the first and second insecticides used alone.Type: GrantFiled: April 27, 2007Date of Patent: March 15, 2011Assignee: Summit VetPharm, LLCInventors: Ian Cottrell, Albert Ahn, Linda Dorneval
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Publication number: 20110053939Abstract: Pharmaceutical compositions comprising at least one compound of e.g. the formulas (Ie) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols and substituents have the following meaning—X— is e.g. and Y is e.g. or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds can be applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.Type: ApplicationFiled: November 8, 2010Publication date: March 3, 2011Applicant: REVOTAR BIOPHARMACEUTICALS AGInventors: Ewald M. AYDT, Remo Kranich
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Publication number: 20110054017Abstract: The present application relates to novel substituted furan derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular diseases.Type: ApplicationFiled: January 29, 2009Publication date: March 3, 2011Inventors: Thomas Lampe, Raimund Kast, Friederike Stoll, Joachim Schuhmacher
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Publication number: 20110046195Abstract: Compounds which modulate quorum sensing in quorum sensing bacteria. Compounds of the invention inhibit quorum sensing and/or activate quorum sensing in various bacteria. Compounds that inhibit quorum sensing are particularly useful for inhibition of detrimental bacterial biofilm formation. Compounds that activate quorum sensing are particularly useful for promoting growth and biofilm formation of beneficial bacterial.Type: ApplicationFiled: June 24, 2010Publication date: February 24, 2011Inventors: Helen E. BLACKWELL, Christine E. McInnis
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Publication number: 20110046129Abstract: 2-Phenylethylamino substituted carboxamide derivatives and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies are presented.Type: ApplicationFiled: September 9, 2010Publication date: February 24, 2011Applicant: Newron Pharmaceuticals S.p.A.Inventors: Florian Thaler, Mauro Napoletano, Cibele Sabido-David, Ermanno Moriggi, Carla Caccia, Laura Faravelli, Alessandra Restivo, Patricia Salvati
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Patent number: 7893084Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein: A is O, S, NR1, or CR1, wherein R1 is defined herein; represents either a single or a double bond; R2 is selected from: H, halogen, R21, OR21, SR21, COOR21, SO2N(R22)2, N(R22)2, CON(R22)2, NR22C(O)R22 or NR22C(O)NR22 wherein R21 and each R22 is defined herein; B is NR3 or CR3, with the proviso that one of A or B is either CR1 or CR3, wherein R3 is defined herein; K is N or CR4, wherein R4 is defined herein; L is N or CR5, wherein R5 has the same definition as R4; M is N or CR7, wherein R7 has the same definition as R4; Y1 is O or S; Z is N(R6a)R6 or OR6, wherein R6a is H or alkyl or NR61R62 wherein R61 and R62 are defined herein; and R6 is H, alkyl, cycloalkyl, alkenyl, Het, alkyl-aryl, alkyl-Het; or R6 is wherein R7 and R8 and Q are as defined herein; Y2 is O or S; R9 is H, (C1-6 alkyl), (C3-7)cycloalkyl or (C1-6)alkyl-(C3-7)cycloalkyl, aryl, Het, (C1-6)alkyl-aryl or (C1-6)alkyl-Het, all of whichType: GrantFiled: November 26, 2008Date of Patent: February 22, 2011Assignee: Boehringer Ingelheim Canada Ltd.Inventors: Pierre Louis Beaulieu, Gulrez Fazal, Sylvie Goulet, George Kukolj, Martin Poirier, Youla S. Tsantrizos, Eric Jolicoeur, James Gillard, Marc-André Poupart, Jean Rancourt
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Publication number: 20110034528Abstract: The present invention describes Elansolids, a new class of novel anti-bacterial compounds of formula (I).Type: ApplicationFiled: February 19, 2009Publication date: February 10, 2011Inventors: Klaus Gerth, Heinrich Steinmetz, Gerhard Höfle
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Publication number: 20110034513Abstract: Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's disease and Down's syndrome are described.Type: ApplicationFiled: October 19, 2010Publication date: February 10, 2011Applicants: Wyeth LLC, ArQule, Inc.Inventors: Anthony F. Kreft, Derek C. Cole, Kevin R. Woller, Joseph R. Stock, George Diamantidis, Dennis M. Kubrak, Kristina M. Kutterer, William J. Moore, David S. Casebier
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Publication number: 20110028509Abstract: The invention relates to compounds of formula I wherein R1, R2, R4, Ra, Rb, Rc, Re, A*, W1, W2 and W3 are as defined in claim 16, for the treatment of CXCR3 related diseases.Type: ApplicationFiled: April 8, 2009Publication date: February 3, 2011Applicant: MERCK SERONO SAInventors: Stefano Crosignani, Christophe Cleva, Christos Tsaklakidis, Lars Burgdorf
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Publication number: 20110021624Abstract: Disclosed are a series of ?-amino-N-substituted amide compounds having a structure of the following formula, the pharmaceutically acceptable salts thereof, and the pharmaceutical composition comprising the same. The ?-amino-N-substituted amide compounds or the pharmaceutically acceptable salts thereof according to the present invention have anti-tumor and/or anti-cancer activities in vivo and in vitro, can effectively depress the growth of various tumor cells and/or cancer cells, and thus can be used in preparing drugs for treating tumors and/or cancers.Type: ApplicationFiled: December 11, 2008Publication date: January 27, 2011Inventors: Fajun Nan, Jia Li, Jian Ding, Gang Liu, Chuanming Xie, Zehong Miao, Wanyi Tai
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Publication number: 20110021571Abstract: The disclosures herein relate generally to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, pharmaceutical compositions thereof, methods of making prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, methods of using prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof, and pharmaceutical compositions thereof for treating or preventing common diseases and/or disorders such as spasticity and/or acid reflux disease. The disclosures herein also relate to acyloxyalkyl carbamate prodrugs of (±)-4-amino-3-(4-chlorophenyl)butanoic acid and analogs thereof which are suitable for oral administration and to sustained release oral dosage forms thereof.Type: ApplicationFiled: September 16, 2010Publication date: January 27, 2011Applicant: XenoPort, Inc.Inventors: Mark A. Gallop, Fenmei Yao, Maria J. Ludwikow, Thu Phan, Ge Peng
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Publication number: 20110014127Abstract: Described herein are methods for effectively and accurately measuring a patient response upon administration of one or more drugs to the patient. The methods are more sensitive than current methodologies. Also described herein are compositions comprising an analgesic and a sufficient amount of an antihistamine to enhance the analgesic properties of the analgesic. With respect to these compositions, the methods described herein are useful for evaluating qualities of pain, definite improvement, and one or more bodily functions of a subject afflicted with pain. The compositions described herein are useful in improving the quality of pain in a subject or a bodily function of a subject afflicted with pain or definite improvement of a subject afflicted with pain.Type: ApplicationFiled: January 5, 2009Publication date: January 20, 2011Inventor: Bernard P. Schachtel
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Publication number: 20110009463Abstract: The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same.Type: ApplicationFiled: October 17, 2008Publication date: January 13, 2011Inventors: Yuri Karl Petersson, Xiang Simon Wang, Patrick John Casey, Alexander Tropsha
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Publication number: 20110009457Abstract: The invention relates to a composition comprising at least one aminobenzamide compound or a salt thereof for controlling animal parasites, veterinary pharmaceutical compositions comprising at least one aminobenzamide of formula (I) for preventing infection with diseases transmitted through parasites, its use for the preparation of a veterinary pharmaceutical for controlling animal parasites, and a method for preventing infection with diseases transmitted through parasites.Type: ApplicationFiled: December 9, 2008Publication date: January 13, 2011Applicant: BAYER CROPSCIENCE AGInventors: Ulrich Görgens, Katsuaki Wada, Yukiyoshi Watanabe, Jun Mihara, Koichi Araki
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Publication number: 20110009482Abstract: Disclosed is a method of treating chronic obstructive disease, said method comprising administering an effective amount of a CXCR2 antagonist and administering an effective amount of at least one drug selected from the group consisting of: angiotensin-converting enzyme inhibitors, Angiotensin II receptor antagonists, cardioselective beta blockers, and lipid regulating drugs. Examples of the CXCR2 antagonist include: (formula 1.0A and 1.0B).Type: ApplicationFiled: December 3, 2008Publication date: January 13, 2011Applicant: Schering CorporationInventors: Irina V. Khanskaya, Jonathan Sadeh, Heribeth Staudinger
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Publication number: 20110003827Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: ApplicationFiled: December 10, 2004Publication date: January 6, 2011Inventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
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Publication number: 20100331234Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.Type: ApplicationFiled: March 3, 2010Publication date: December 30, 2010Applicant: Massachusetts Institute of TechnologyInventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher Gerard Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel G. Anderson
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Publication number: 20100331329Abstract: The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by histone deacetylase.Type: ApplicationFiled: September 10, 2010Publication date: December 30, 2010Applicant: ASTRAZENECA ABInventors: Elaine Sophie Elizabeth Stokes, Craig Anthony Roberts, Michael James Waring
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Patent number: 7858644Abstract: Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(?O), S(?O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(?O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): or (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted alkyl; (iv) tetrazol-5-yl.Type: GrantFiled: January 28, 2009Date of Patent: December 28, 2010Assignee: Asterand UK LimitedInventors: Alexander W. Oxford, Richard J. Davis, Robert A. Coleman, Kenneth L. Clark, David E. Clark, Neil V. Harris, Garry Fenton, George Hynd, Keith A. J. Stuttle, Jonathan M. Sutton, Christopher G. Newton
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Publication number: 20100324046Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: June 24, 2008Publication date: December 23, 2010Inventors: Paul Harrington, Richard W. Heidebrecht, JR., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Paul Tempest, Kevin J. Wilson, David J. Witter
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Publication number: 20100322881Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R3, R4 have the meaning cited in the claims, to methods for the production thereof, agents containing said compounds and to their use for the functionalisation of matrices, in particular their use as skin and/or hair-binding UV filters.Type: ApplicationFiled: January 15, 2009Publication date: December 23, 2010Applicant: MERCK PATENT GESELLSCHAFTInventors: Thomas Rudolph, Philipp Buehle
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Publication number: 20100323993Abstract: Methods are provided herein for treatment of myotonic dystrophy and other toxic RNA diseases in a subject. In some examples, the method comprises administration of a compound that binds a nucleotide repeat expansion in a ribonucleic acid molecule, thereby treating the disease. In additional examples, the method comprises administration of a compound that disrupts binding of muscleblind-like proteins to an RNA nucleotide repeat expansion. Compounds for use in the disclosed method include pentamidine or heptamidine or derivatives thereof. Representative compounds are described herein.Type: ApplicationFiled: February 20, 2009Publication date: December 23, 2010Inventors: John Andrew Berglund, Bryan M. Warf, Catherine Matthys, Michael M. Haley, Cameron L. Hilton
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Patent number: 7855231Abstract: A topical insecticide is provided which can be safe to use and avoids many common deleterious side effects of conventional topical insecticides. The insecticide contains an insecticide and an insect growth regulator effective for killing fleas, flea larvae and flea eggs. The insecticide is formulated by dissolving an insecticidal (tetrahydro-3-furanyl) methylamine derivative and an insect growth regulator (IGR) in a solvent containing N-octyl pyrrolidone and/or N-methyl pyrrolidone to increase the solvency of the IGR component, thereby providing an insecticide having high insecticidal activity.Type: GrantFiled: April 27, 2007Date of Patent: December 21, 2010Assignee: Summit VetPharm, LLCInventors: Ian W. Cottrell, Albert Ahn, Linda Dorneval
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Patent number: 7855232Abstract: A compound containing an alkylene selenocyanate or an alkylene isoselenocyanate moiety effective to prevent the occurrence or progression of cancer or a precancerous condition. The compound can be provided and administered in the form of a pharmaceutical composition, a cosmetic, a food additive, supplement, or the like. Methods for synthesis and use of the chemopreventive compound of the invention are also provided.Type: GrantFiled: October 31, 2007Date of Patent: December 21, 2010Assignee: LKT Laboratories, Inc.Inventors: Luke K. T. Lam, Nayaz Ahmed
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Publication number: 20100311727Abstract: Therapeutic amine-arylsulfonamide conjugate compounds, of the general formula: wherein R? is [D-W-], hydroxyl, or alkoxyl; R? is independently [D-W?-], hydrogen, alkoxy, alkyl, cycloalkyl, alkenyl, alkynyl or aryl, or R? and R? together with the nitrogen atom to which they are attached form a 4-, 5-, 6-, 7- or 8-membered ring optionally containing one or two further heteroatoms independently selected from nitrogen, oxygen and sulfur; D is independently a therapeutic amine radical comprising at least one nitrogen atom and optionally at least one oxygen atom coupled to W or W? by a nitrogen or oxygen atom; W and W? are a chemical bond or linker; wherein either R? is [D-W-] or at least one R? is [D-W?-], and pharmaceutically acceptable esters, amides, salts or solvates thereof, pharmaceutical compositions containing same, methods for their preparation, and their use in treating psychiatric, neurologic and metabolic disorders are disclosed.Type: ApplicationFiled: June 8, 2010Publication date: December 9, 2010Applicant: ALGEBRA, INC.Inventors: Philip F. MORGAN, James L. KELLEY
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Publication number: 20100311582Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6, independently of each other, are for example, selected from the group consisting of H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C6-alkoxy, C3-C8-cycloalkyl, R7C(?O), and a ring system; provided that at least one of R1 and R6 is a —C2-C6-alkenylthio-C1-C6-alkyl, —C1-C6-alkoxy-C(?O)NRx-C1-C6-alkyl, —partially or fully unsaturated ring system containing in at least one ring in the ring system at least one hetero atom selected from N, O and S, which ring system is bound (i.e. through the N bonded to R1 and R6 in formula I) either directly or via a a C1-C6-alkylene group to the remainder of the compound, —partially or fully unsaturated ring system containing a ring that is bound to the remainder of the compound (i.e.Type: ApplicationFiled: January 23, 2009Publication date: December 9, 2010Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Thomas Pitterna, Peter Renold, Ottmar Franz Hueter, Peter Maienfisch, Werner Zambach
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Publication number: 20100298138Abstract: The present invention relates to the use of aminoazoline and urea derivatives for com-bating animal pests. The invention also relates to a method for controlling animal pests by using these compounds, to seed and to an agricultural and veterinary composition comprising said compounds and to specific azoline and urea derivatives.Type: ApplicationFiled: May 23, 2008Publication date: November 25, 2010Applicant: BASF SEInventors: Christopher Koradin, Markus Kordes, Ernst Baumann, Ronan Le Vezouet, Deborah L. Culbertson
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Patent number: 7838551Abstract: This invention describes a process for the production of ANHYDROUS active pharmaceutical ingredients (APIs); a process for the preparation of HYDRATED active pharmaceutical ingredients, a process for the preparation of sterile and stable injectable solutions, and their use, more specifically, APIs which are taxane derivatives, especially (2R,3S) 4-acetoxy-2-?-benzoyloxy-5?-20-epoxy-1,7-?-10-?-tri-hydroxy-9-oxo-tax-11-en-13?-il 3-tert-butoxy carbonylamino-2-hydroxy-3-phenylpropionate (I); 4-acetoxy-2-?-benzoyloxy-5-?-20-epoxy-1,7?-10-?-tri-hidroxy-9-oxo-tax-11-en-13?-il (2R,3S) 3-benzoylamino-2-hydroxy-3-phenylpropionate (II), and particularly 4-acetoxy-2-?-benzoyloxy-5?-20-epoxy-1, 7-?-10-?-tri-hidroxy-9-oxo-tax-11-en-13?-il (2R,3S) 3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate tri-hydrate (III).Type: GrantFiled: December 10, 2004Date of Patent: November 23, 2010Assignees: Quiral Quimica do Basil S.A., Biorganica LTDA.Inventors: Marco Antônio Santini, Antônio Machado, Aurélio Maranduba, Eneida Guimarães, Marcio Santiago Junior, Maria Silva
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Patent number: 7838513Abstract: The present invention relates to the treatment of a mammal with a pharmaceutical composition comprising an H2-blocker, at least one anti-inflammatory agent, a cytotoxic agent and, optionally, levamisole, a retinoid, an NFkB inhibitor, a redox quinone, an agent that enhances the intracellular accumulation of NADH+H+, a poly-alcohol, an inhibitor of pro-angiogenic growth factor(s) and an MMP inhibitor, such pharmaceutical composition allowing for the enhanced therapy and/or prevention of neoplastic diseases and disorders.Type: GrantFiled: July 4, 2007Date of Patent: November 23, 2010Assignee: Tiltan Pharma Ltd.Inventor: Shmuel A. Ben-Sasson
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Publication number: 20100286103Abstract: The invention relates to compounds that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: ApplicationFiled: July 31, 2008Publication date: November 11, 2010Inventor: Shoujun Chen
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Publication number: 20100284944Abstract: Disclosed are Compounds that block off-notes in consumables and methods of blocking off-notes in consumables including off-notes provided by artificial sweeteners including aspartame, Saccharin, acesulfame K (Acesulfame potassium), sucralose and cyclamate; and including stevioside, swingle extract, glyccerhizin, perillartine, naringin dihydrochalcone, neohesperidine dihydrochalcone, mogroside V, rubusoside, rubus extract, and rebaudioside A.Type: ApplicationFiled: March 27, 2008Publication date: November 11, 2010Inventors: Ioana Maria Ungureanu, Nicole Erna Irene Brune, Jay Patrick Slack, Kimberley Gray, Christopher Todd Simons, Jenny Ellen Evans Pennimpede
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Publication number: 20100280081Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, for the use as a medicament.Type: ApplicationFiled: May 3, 2010Publication date: November 4, 2010Applicant: 4SC AGInventors: Daniel VITT, Manfred GROEPPEL, Roland BAUMGARTNER, Johann LEBAN
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Publication number: 20100280075Abstract: Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C?Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—. R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group. R7 and Rg are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and Rg is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group. Z is ?O or ?S.Type: ApplicationFiled: January 25, 2010Publication date: November 4, 2010Inventors: Keizo Koya, Lijun Sun, Shoujun Chen, Noriaki Tatsuta, Yaming Wu, Mitsunori Ono
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Publication number: 20100272808Abstract: Drugs are formulated as oral dosage forms for controlled release in which the release rate limiting portion is a shell surrounding the drug-containing core. The shell releases drug from the core by permitting diffusion of the drug from the core. The shell also motes gastric retention of the dosage form by swelling upon imbibition of gastric fluid to size that is retained in the stomach during the postprandial or fed mode.Type: ApplicationFiled: April 29, 2010Publication date: October 28, 2010Inventors: Bret Berner, Jenny Louie-Helm, Gloria Gusler, John N. Shell
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Publication number: 20100273835Abstract: The invention provides compounds of general formula (I) or a pharmaceutically acceptable salt, polymorph or solvate thereof, including all tautomers and stereoisomers thereof, wherein K, W, X; Y and Z are described throughout the description and claims. The compounds of the present invention are useful as inhibitors of prolyl endopeptidase (PEP, EC 3.4.21.26) and/or IL-6.Type: ApplicationFiled: July 10, 2008Publication date: October 28, 2010Applicant: PROBIODRUG AGInventors: Ulrich Heiser, Andre J. Niestroj, Ingo Schulz
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Publication number: 20100272781Abstract: This invention relates to chewable tablets containing medicants such as gastrointestinal drugs. More particularly, the invention relates to chewable tablets of medicaments that are sugar free and have reduced calories. Accordingly, the tablets of the invention are suitable for both diabetic and non-diabetic patients.Type: ApplicationFiled: March 29, 2010Publication date: October 28, 2010Inventors: Veerappan Subramanian, Muthusamy Shanmugan, Yuh-Herng Eric Lin, Kanni Paranjothy, Kranthikumar Gorlamari
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Publication number: 20100267676Abstract: Gamma-amino-butyric acid derivatives that are GABAB receptor ligands, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives and pharmaceutical compositions thereof for treating diseases are disclosed.Type: ApplicationFiled: April 16, 2010Publication date: October 21, 2010Inventors: Feng Xu, Mark A. Gallop, Ge Peng, Thu Phan, Usha Dilip, David J. Wustrow
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Publication number: 20100267690Abstract: Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.Type: ApplicationFiled: June 30, 2010Publication date: October 21, 2010Applicant: Piramal Life Sciences LimitedInventors: Bansi LAL, Swati Bal-Tembe, Usha Ghosh, Arun Kumar Jain, Tulsidas More, Anil Ghate, Jacqueline Trivedi, Sapna Parikh
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Patent number: 7816389Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-6)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.Type: GrantFiled: January 11, 2007Date of Patent: October 19, 2010Assignee: Nabriva Therapeutics Forschungs GmbHInventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
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Publication number: 20100261757Abstract: Certain novel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, b, c, T, W, Y R, Rf, Rg, Rh, Ri, Rj, Rk, Rm, Rn, and R are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: January 15, 2007Publication date: October 14, 2010Inventors: John F. Chiarello, Harvey R. Wendt, Najing Zhang, George Theodoridis
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Publication number: 20100261760Abstract: The disclosure provides EP2 receptor agonist compounds and methods for using the compounds for treating conditions which can be alleviated by agonism of an EP2 receptor.Type: ApplicationFiled: June 22, 2010Publication date: October 14, 2010Applicant: Asterand UK LimitedInventors: Alexander William Oxford, Richard John Davis, Robert Alexander Coleman, Kenneth Lyle Clark, David Edward Clark, Neil Victor Harris, Garry Fenton, George Hynd, Keith Alfred James Stuttle, Jonathan Mark Sutton, Mark Richard Ashton, Edward Andrew Boyd, Shirley Ann Brunton
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Publication number: 20100256156Abstract: The present invention provides a heterocyclic compound represented by the following formula (I), which has a glucagon antagonistic action and is useful for the prophylaxis or treatment of diabetes and the like, a compound represented by wherein ring A is an optionally substituted benzene ring and the like; Y is a nitrogen atom and the like; X is —O— and the like; R4 is a hydrogen atom and the like; R5 and R6 are each independently a hydrogen atom and the like; R1 is an optionally substituted hydrocarbon group and the like; R2 is a hydrogen atom and the like; and R3 is —(CH2)3—COOH and the like, or a salt thereof.Type: ApplicationFiled: October 31, 2008Publication date: October 7, 2010Inventors: Yoshihiro Banno, Ryoma Hara, Ryosuke Tokunoh
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Publication number: 20100256201Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.Type: ApplicationFiled: March 11, 2010Publication date: October 7, 2010Applicant: Bayer Schering Pharma AktiengesellschaftInventors: Tsuneji Suzuki, Tomoyuki Ando, Katsutoshi Tsuchiya, Osamu Nakanishi, Akiko Saito, Takashi Yamashita, Yoshinori Shiraishi, Eishi Tanaka
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Publication number: 20100249197Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: —NR1C(?O)— and —C(?O)NR1—; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g.Type: ApplicationFiled: June 3, 2009Publication date: September 30, 2010Inventors: Clare J. Watkins, Maria Rosario Romero-Martin, Kathryn G. Moore, James Ritchie, Paul W. Finn, Ivars Kalvinsh, Einars Loza, Igor Starchenkov, Klara Dikovska, Rasma Bokaldere, Vija Gailite, Maxim Vorona, Victor Andrianov, Daina Lolya, Valentina Semenikhina, Andris Amolins, C. John Harris, James E.S. Duffy
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Publication number: 20100249165Abstract: This invention relates to compounds useful as PDZ domain modulators, in particular the PDZ domain of PICK1. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions.Type: ApplicationFiled: June 3, 2008Publication date: September 30, 2010Applicants: University of Copenhagen, NeuroSearch A/SInventors: Ulrik Gether, Kenneth Madsen, Thor Seneca Thorsen, Dan Peters, Tino Dyhring, Lars Christian Rønn
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Patent number: 7803800Abstract: 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: September 30, 2005Date of Patent: September 28, 2010Assignee: DAC S.R.L.Inventors: Saverio Minucci, Pier Giuseppe Pelicci, Antonello Mai, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
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Publication number: 20100239666Abstract: The invention relates to a process for producing mouldings by injection moulding the steps in the process being a) melting and mixing of a (meth)acrylate copolymer composed of from 85 to 98% by weight of C1-C4-alkyl (meth)acrylates capable of free-radical polymerization and from 15 to 2% by weight of (meth)acrylate monomers having a quaternary ammonium group in the alkyl radical, with from 10 to 25% by weight of a plasticizer, and also from 10 to 50% by weight of a dryers [sic] and/or from 0.1 to 3% by weight of a release agent, and, where appropriate, with other conventional pharmaceutical additives or auxiliaries and/or with an active pharmaceutical ingredient, b) devolatilizing the mixture at temperatures of at least 120° C., thus reducing the content of the low-boiling constituents with a vapour pressure of at least 1.9 bar at 120° C. to not more than 0.5% by weight, and c) injecting the devolatilized mixture at a temperature of from 80 to 160° C.Type: ApplicationFiled: June 3, 2010Publication date: September 23, 2010Inventors: Hans-Ulrich Petereit, Thomas Beckert, Manfred Assmus, Wemer Hoess, Wolfgang Fuchs, Hartmut Schikowsky
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Publication number: 20100234455Abstract: Hormone refractory metastatic disease can be treated with an oxyamide-containing compound through the inhibition of HDAC1 or HDAC2.Type: ApplicationFiled: October 6, 2009Publication date: September 16, 2010Inventors: Norbert L. Wiech, Hsuan-Yin Lan-Hargest
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Publication number: 20100233086Abstract: This invention relates to novel compounds suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).Type: ApplicationFiled: October 14, 2008Publication date: September 16, 2010Inventors: Lutz Lehmann, Andrea Thiele, Tobias Heinrich, Thomas Brumby, Christer Halldin, Balazs Gulyas, Sangram Nag