Asymmetrical (e.g., 1,2,4-triazine, Etc.) Patents (Class 514/242)
-
Patent number: 8101592Abstract: This invention is directed to a hexahydro-cyclooctyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: GrantFiled: May 24, 2010Date of Patent: January 24, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Mingde Xie, Fina Liotta, Huajun Lu, Meng Pan, Michael P. Wachter
-
Publication number: 20120010172Abstract: The present application discloses compounds of formula (I) wherein X is ?O, ?S, ?NH, ?NOH and ?NO-Me; A is —C(?O)—, —S(?O)2—, —C(?S)— and P(?O)(R5)—; B is, —O—, —(CH2)3-6—, and O—(CH2)2-5—; D is, —O—, —CR7R8— and —NR9; m is 0-12, n is 0-12, m+n is 1-20; p is 0-4; R1 is opt.sub. heteroaryl; and pharmaceutically acceptable salts thereof, and prodrugs thereof. The application also discloses the compound for use as a medicament for the treatment of a disease or a condition caused by an elevated level of nicotinamide phosphoribosyltransferase (NAMPRT), e.g. inflammatory and tissue repair disorders; dermatosis; autoimmune diseases, Alzheimers disease, stroke, athersclerosis, restenosis, diabetes, glomerulonephritis, cancer, cachexia, inflammation associated with infection and certain viral infections, including Acquired Immune Deficiency Syndrome (AIDS), adult respiratory distress syndrome, ataxia telengiectasia.Type: ApplicationFiled: August 31, 2009Publication date: January 12, 2012Applicant: McDERMOTT WILL & EMERY LLPInventors: Mette Knak Christensen, Fredrik Bjorkling
-
Publication number: 20110319389Abstract: The present invention relates to methods for the treatment or prevention of fatigue associated with disordered sleep, for example, in multiple sclerosis, fibromyalgia, Fabry's disease, Parkinson's disease, or traumatic brain injury, using cyclobenzaprine The present invention further relates to a biomarker for the therapeutic effects of a cyclobenzaprine treatment.Type: ApplicationFiled: June 9, 2011Publication date: December 29, 2011Applicant: TONIX PHARMACEUTICALS, INC.Inventors: Seth Lederman, Herb Harris
-
Patent number: 8076334Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as obesity, hyperlipidemia, hypercholesterolemia and diabetes and other related disorders and diseases, and may be useful for other diseases such as NASH, atherosclerosis, cardiovascular diseases, hypothyroidism, thyroid cancer and other disorders and diseases related thereto.Type: GrantFiled: September 2, 2008Date of Patent: December 13, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Nancy-Ellen Haynes, Nathan Scott, Jefferson Wright Tilley
-
Publication number: 20110301165Abstract: Compounds represented by the formula 1: wherein each R individually is H, an aliphatic acyl group or an aromatic acyl group; A is selected from the group consisting of wherein X is selected from the group consisting of hydrogen, halo, alkoxy, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, amino, monoalkylamino, dialkylamino, cyano and nitro; are used to treat or prevent arthritis including rheumatoid arthritis.Type: ApplicationFiled: August 15, 2011Publication date: December 8, 2011Applicant: Southern Research InstituteInventors: John A. Secrist, III, William R. Waud, Zhican Qu, Xaingmin Cui
-
Patent number: 8071651Abstract: Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is —CH2—; R is a mono- to tetra-substituted, mono- or bicyclic, unsaturated heterocyclic radical having 1 to 4 nitrogen atoms, R2 is C1-6alkyl or C3-6cycloalkyl; R3 is independently of one another H, C1-6alkyl, C1-6alkoxycarbonyl or C1-6alkanoyl; R4 is C2-6alkenyl, C1-6alkyl, unsubstituted or substituted aryl-C1-6alkyl or C3-8cycloalkyl; R5 is -Lm-R6; L is C1-6alkylene which is optionally substituted by 1-4 halogen, or a linker: formula (II) n=0, 1 or 2; m=0 or 1; R6 is a radical composed of 2 cyclic systems selected from bicyclo[x.y.z]alkyl, spiro[o.p]alkyl, mono- or bioxabicyclo[x.y.z]alkyl or mono- or bioxaspiro[o.Type: GrantFiled: September 14, 2006Date of Patent: December 6, 2011Assignee: Novartis AGInventors: Peter Herold, Robert Mah, Vincenzo Tschinke, Stefan Stutz, Aleksandar Stojanovic, Christiane Marti, Dirk Behnke, Stjepan Jelakovic
-
Publication number: 20110293533Abstract: Disclosed are mixtures and compositions for controlling invertebrate pests relating to combinations comprising (a) 3-bromo-N-[4-chloro-2-methyl-6-[(methylamino)carbonyl]phenyl]-1-(3-chloro-2-pyridinyl)-1H-pyrazole-5-carboxamide, and its N-oxides, and suitable salts thereof and a component (b) wherein the component (b) is at least one compound or agent selected from neonicotinoids, cholinesterase inhibitors, sodium channel modulators, chitin synthesis inhibitors, ecdysone agonists, lipid biosynthesis inhibitors, macrocyclic lactones, GABA-regulated chloride channel blockers, juvenile hormone mimics, ryanodine receptor ligands, octopamine receptor ligands, mitochondrial electron transport inhibitors, nereistoxin analogs, pyridalyl, flonicamid, pymetrozine, dieldrin, metaflumizone, biological agents, and suitable salts of the foregoing.Type: ApplicationFiled: August 11, 2011Publication date: December 1, 2011Applicant: E.I. DU PONT NEMOURS AND COMPANYInventors: Isaac Billy Annan, John Lindsey Flexner, Hector Eduardo Portillo, George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
-
Publication number: 20110269763Abstract: Compounds of formula (I) are useful for the treatment of disease responsive to modulation of CRTH2 receptor activity, such as asthma, rhinitis, allergic airway syndrome, and allergic rhinobronchitis: wherein A represents a carboxyl group —COOH, or a carboxyl bioisostere; A1 is hydrogen or methyl; ring Ar1 is an optionally substituted phenyl ring or 5- or 6-membered monocyclic heteroaryl ring, in which AA1CHO— and L2 are linked to adjacent ring atoms; rings Ar2, Ar3 each independently represent a phenyl or 5- or 6-membered monocyclic heteroaryl ring, or a bicyclic ring system consisting of a 5- or 6-membered carbocyclic or heterocyclic ring which is benz-fused or fused to a 5- or 6-membered monocyclic heteroaryl ring, said ring or ring system being optionally substituted; t is 0 or 1; L2 and L3 are linker radicals as defined in the description.Type: ApplicationFiled: June 2, 2011Publication date: November 3, 2011Applicant: 7TM Pharma A/SInventors: Trond Ulven, Thomas Frimurer, Øystein Rist, Evi Kostenis, Thomas Högberg, Jean-Marie Receveur, Marie Grimstrup
-
Publication number: 20110269722Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.Type: ApplicationFiled: December 23, 2010Publication date: November 3, 2011Inventor: Apparao Satyam
-
Publication number: 20110269709Abstract: The invention provides the compounds of formula (I) or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutical compositions comprising one or more compounds of formula I or intermediates thereof and one more of pharmaceutically acceptable carriers, vehicles or diluents. The invention further provides methods of preparation and methods of use of prodrugs including NO-releasing prodrugs, double prodrugs and mutual prodrugs comprising the compounds of formula I.Type: ApplicationFiled: December 23, 2010Publication date: November 3, 2011Inventor: Apparao Satyam
-
Publication number: 20110269712Abstract: This invention is directed to compounds of Formula (1) including all geometric and stereoisomers, N oxides, and agriculturally suitable salts thereof, agricultural compositions containing them and their use as fungicides, (1) provided that the compound of Formula 1 is other than 2-[1-[(2-chlorophenyl)acetyl]-4-piperidinyl]-N-methyl-N-[(1R)-1-phenylethyl]-4-thiazolecarboxamide and R1 is other than 4-fluorophenyl; wherein R1, R2, A, G, Q, W1, W2, X and n are otherwise as defined in the disclosure, Also disclosed are compositions containing the a compound having a formula corresponding to Formula (1) where the provisos are both omitted; and methods for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound having a formula corresponding to Formula (1) where the provisos are both omitted.Type: ApplicationFiled: July 26, 2006Publication date: November 3, 2011Inventors: John Joseph Bisaha, Patrick Ryan Kovacs, Renne M. Lett, Jeffrey Keith Long, Robert James Pasteris, Boris Abramovich Klyashchitsky, Bruce Lawrence Finkelstein, Brenton Todd Smith
-
Patent number: 8048882Abstract: The invention relates to novel pharmaceutical combinations with improved sodium channel blocking effect. Further, the invention relates to the use of said pharmaceutical combinations in chronic pain, in disturbances of the motor system, in epilepsy, as well as in other therapeutic fields where the use of sodium channel blockers is acceptable.Type: GrantFiled: December 18, 2004Date of Patent: November 1, 2011Inventors: Pal Kocsis, Istvan Tarnawa, Marta Than, Karoly Tihanyi, Gyorgy Nemeth
-
MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Publication number: 20110245251Abstract: Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: ApplicationFiled: December 7, 2009Publication date: October 6, 2011Applicant: Arena Pharmaceuticals, Inc.Inventors: Thuy-Anh Tran, Rena Hayashi, Jason B. Ibarra, Brett Ullman, Ning Zou -
Publication number: 20110243911Abstract: The present invention is directed to the use of a compound capable of reducing the uric acid level in a mammal for the prevention and/or the treatment of IL-1? driven lung pathology, particularly to treat lung inflammation such as chronic fibrosis, COPD and interstitial fibrosis and other IL-1? driven lung pathologies including those of autoimmune origin. Preferred compounds capable of reducing the uric acid level are selected from the group consisting of xanthine oxidase inhibitors, such as allopurinol, recombinant enzyme uricase and uricosuric compound capable of enhancing uric acid excretion, such as probenecid. The invention further relates to a method for identifying in vitro whether a patient presents an IL-1? driven lung pathology or is at risk to develop an IL-1? driven lung pathology, or for the screening of a compound for treating an IL-1? driven lung pathology.Type: ApplicationFiled: September 18, 2009Publication date: October 6, 2011Inventors: Bernhard Ryffel, Isabelle Couillin
-
Publication number: 20110245235Abstract: The present inventions provide combination therapies, kits, and methods for providing relief and/or for improving one or more symptoms associated with an auditory system disorder in a subject diagnosed with the auditory system disorder, comprising an effective amount of at least one pharmaceutical agent and at least one auditory system disorder device, as well as methods for using at least one pharmaceutical agent and/or at least one auditory system disorder device in the manufacture of said kits.Type: ApplicationFiled: October 9, 2009Publication date: October 6, 2011Inventors: Peter J. Hanley, Robert H. Frater, Arjun Goyal, Paul B. Davis
-
Publication number: 20110245156Abstract: Compounds are disclosed. Compositions that include the compounds are disclosed. Methods of making and using the compounds are also disclosed.Type: ApplicationFiled: December 9, 2009Publication date: October 6, 2011Applicant: CYTOKINE PHARMASCIENCES, INC.Inventor: Thais M. Sielecki-Dzurdz
-
Patent number: 8022221Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.Type: GrantFiled: February 12, 2009Date of Patent: September 20, 2011Assignee: Amgen Inc.Inventors: Victor J. Cee, Holly L. Deak, Bingfan Du, Stephanie D. Geuns-Meyer, Brian L. Hodous, Hanh Nho Nguyen, Philip R. Olivieri, Vinod F. Patel, Karina Romero, Laurie Schenkel
-
Publication number: 20110212949Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests, including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: ApplicationFiled: July 4, 2009Publication date: September 1, 2011Inventors: Thomas Bretschneider, Eva-Maria Franken, Ulrich Görgens, Martin Füßlein, Achim Hense, Joachim Kluth, Hans-Georg Schwarz, Adeline Köhler, Olga Malsam, Arnd Voerste, Angela Becker
-
Publication number: 20110212944Abstract: This invention relates to novel 2-oxo-1-pyrrolidines, their derivatives, and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a compound with the ability to act as a synaptic vesicle protein 2A (SV2A) ligand and/or a sodium channel blocker.Type: ApplicationFiled: June 30, 2009Publication date: September 1, 2011Inventors: Julie Liu, Rose Persichetti
-
Publication number: 20110212966Abstract: This invention relates to compounds of formula I their salts, and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions comprising these compounds and their use in the treatment of picornavirus infections in mammals, as well as novel intermediates useful in the preparation of the compounds of formula I.Type: ApplicationFiled: May 4, 2011Publication date: September 1, 2011Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTDInventors: Keith Watson, Guy Krippner, Pauline Stanislawski, Darryl McConnell
-
Patent number: 8003806Abstract: The invention relates to compounds of the Formula 1 and to pharmaceutically acceptable salts and solvates thereof, wherein A, X2, X4, X5 and X1 are as defined herein. The invention also relates to methods of treating abnormal cell growth in mammals by administering the compounds of Formula 1 and to pharmaceutical compositions for treating such disorders which contain the compounds of Formula 1.Type: GrantFiled: November 9, 2005Date of Patent: August 23, 2011Assignee: OSI Pharmaceuticals, LLCInventors: Jason Bloxham, Gary V. Borzillo, Eric William Collington, Shazia Sadiq, Colin Peter Sambrook Smith, Chris L. Waller, Graham M. Wynne
-
Publication number: 20110178087Abstract: The present invention provides novel compounds and pharmaceutical compositions thereof, as well as methods for using the compounds and pharmaceutical compositions for treating tumors. Examples of specific tumor types that the compounds may be used to treat include, but are not limited to sarcomas, melanomas, neuroblastomas, carcinomas (including but not limited to lung, renal cell, ovarian, liver, bladder, and pancreatic carcinomas), and mesotheliomas.Type: ApplicationFiled: March 30, 2011Publication date: July 21, 2011Applicant: Compass Pharmaceuticals LLC.Inventors: David Kanne, John Ward, Gary Look, X. Michael Wang, Diva Chan, Tina Lee, Donald R. James, Richard Gless, John Schullek, Charles Vacin
-
Publication number: 20110172171Abstract: The present invention relates to taurine or taurine-like substances for the prevention of brain oedema, particularly brain intramyelinic oedema and more particularly brain intramyelinic oedema induced by an anti-convulsive drug such as vigabatrin. The invention relates to a substance selected from the group consisting of taurine, a taurine precursor, a taurine metabolite, a taurine derivative, a taurine analog and a substance required for the taurine biosynthesis for the prevention of brain oedema.Type: ApplicationFiled: September 4, 2009Publication date: July 14, 2011Inventors: Serge Picaud, José-Alain Sahel, Firas Jammoul
-
Publication number: 20110166143Abstract: The present application relates to the use of heterocyclic compounds, some of which are known, for controlling animal pests including arthropods and in particular insects, furthermore to novel heterocyclic compounds and to processes for their preparation.Type: ApplicationFiled: October 12, 2010Publication date: July 7, 2011Applicant: Bayer CropScience AGInventors: Thomas BRETSCHNEIDER, Martin Füßlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria Franken, Arnd Voerste
-
Publication number: 20110166142Abstract: 2-Substituted isoflavonoid compounds and pharmaceutical compositions containing same are useful as anti-inflammatory agents and antioxidants and for the treatment of related diseases and conditions.Type: ApplicationFiled: June 30, 2008Publication date: July 7, 2011Inventors: Eleanor Eiffe, Andrew Heaton, Catherine Walker, Alan James Husband
-
Publication number: 20110158935Abstract: Disclosed are drug delivery systems for the delivery of small molecule and macromolecular drugs. More particularly, disclosed are substituted analogs of 3,6-di(alkyl-4 aminobutyl)-2,5-diketopiperazine (which may also be referred to DKP), their use in the formulation of both small molecule and macromolecular drugs including therapeutic, prophylactic and diagnostic agents, stabilizing agents and systems for their delivery.Type: ApplicationFiled: December 29, 2009Publication date: June 30, 2011Inventor: Kelly Sullivan Kraft
-
Publication number: 20110160212Abstract: Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.Type: ApplicationFiled: December 28, 2010Publication date: June 30, 2011Inventors: Weibo Wang, Tongshuang Li
-
Publication number: 20110130403Abstract: The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4/PDE type 7 inhibitors.Type: ApplicationFiled: March 13, 2008Publication date: June 2, 2011Applicant: RANBAXY LABORATORIES LIMITEDInventors: Sonali Rudra, Nidhi Gupta, Lalit Kumar Baregama, Ritu Agarwal, Mandadapu Raghuramaiah, Vinayak Vasantrao Khairnar, Venkata P. Palle, Sarala Balachandran, Abhijit Ray, Sunada G. Dastidar, Lalitha Vijaykrishnan
-
Publication number: 20110123489Abstract: Compounds having the formula I wherein wherein R1, R2 and R3 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors with improved bioavailability. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: November 19, 2010Publication date: May 26, 2011Applicant: Roche Palo Alto LLCInventor: Joshua Paul Gergely Taygerly
-
Publication number: 20110123618Abstract: Rapidly disintegrating multiparticulate controlled release formulations of lamotrigine having an improved pharmacokinetic profile and improved patient compliance, and process of preparing the formulations. It provides better control of blood plasma levels than conventional tablet formulations that is administered once or more times a day.Type: ApplicationFiled: January 26, 2011Publication date: May 26, 2011Inventor: Sunil Sadanand Nadkarni
-
Publication number: 20110124588Abstract: The novel active compound combinations comprising compounds of the formulae (I) and (II) have very good insecticidal and acaricidal properties.Type: ApplicationFiled: April 28, 2009Publication date: May 26, 2011Applicant: Bayer Cropscience AGInventors: Peter Jeschke, Reiner Fischer, Wolfram Andersch, Heike Hungenberg
-
Publication number: 20110118266Abstract: The present invention relates to derivatives of general formula I wherein: —W represents nitrogen, —R1 represents: •a hydrogen or a linear or branched C1-C5 alkyl radical or, •a C1-C3 alkyl radical substituted with groups such as trifluoromethyl, nitrile, hydroxy, C1-C3 alcoxy, C3-C6 alkoxyalkoxy, indolyl, thiophenyl, oxothiophenyl, C1-C3 N-alkylcarbamoyl groups or, •a phenyl or pyridyl or naphthyl, or thiophenyl group optionally substituted with one or more groups such as halogen atoms, nitro, nitrile, trifluoromethyl, vinyl, methylsulfanyl, linear branched C1-C4 alkyl, linear or branched C1-C3 alkoxy groups, •a C6 2-oxocycloalkyl radical—R2 represents a methyl or heptyl, —m, n are equal to 1, —V represents CH2, —X—Y represents —N— (C?O)—, —CH—O—, —Z represents a phenyl group substituted with one or more trifluoromethyl groups, halogen atoms or linear C1-C4 alkyl groups.Type: ApplicationFiled: July 7, 2009Publication date: May 19, 2011Applicant: PIERRE FABRE MEDICAMENTInventors: Isabelle Leroy, Elisabeth Dupont-Passelaigue, Karine Valeille, Yves Rival, Didier Junquero
-
Patent number: 7943614Abstract: A carboxamide compound represented by the formula (I): [wherein Q represents a nitrogen-containing 6-membered aromatic heterocyclic group optionally fused with a benzene ring, two or more ring constitutional atoms of the heterocyclic group are a nitrogen atom, and the heterocyclic group may be substituted with at least one group selected from the group consisting of a C1-C3 alkyl group etc.], and a plant disease controlling agent comprising this as an active ingredient.Type: GrantFiled: July 12, 2006Date of Patent: May 17, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Sadayuki Arimori, Yoshiharu Kinoshita
-
Publication number: 20110112083Abstract: The present invention relates to novel oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group, pharmaceutically acceptable salts thereof, methods for preparing the same and pharmaceutical compositions comprising the same. The oxazolidinone derivatives with cyclic amidoxime or cyclic amidrazone group or the pharmaceutically acceptable salts thereof can be effectively used for the treatment of thromboembolism and tumor as an anticoagulant based on the inhibition of factor Xa.Type: ApplicationFiled: June 5, 2009Publication date: May 12, 2011Applicant: LEGOCHEM BIOSCIENCE LTD.Inventors: Ho Young Song, Young Lag Cho, Dae Yon Lee, Hee Sock Park, Sung Yoon Baek, Sang Eun Chae, Sang Hui Jo, Yeon Ok Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
-
Publication number: 20110098303Abstract: The present invention provides methods and compositions for increasing the rate of nail growth in mammals, especially humans, using thyromimetic compounds.Type: ApplicationFiled: November 18, 2003Publication date: April 28, 2011Inventors: Niall S. Doherty, Tanya Parkinson
-
Publication number: 20110086856Abstract: The present invention relates to compounds useful of inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: December 14, 2010Publication date: April 14, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Hayley Binch, Jean-Damien Charrier, Simon Everitt, Juliam M.C. Golec, David Kay, Ronald Knegtel, Andrew Miller, Francoise Pierard
-
Publication number: 20110086818Abstract: The invention features methods, compositions, and kits for selective inhibition of pain-and itch sensing neurons (nociceptors and pruriceptors) by drug molecules of small molecule weight, while minimizing effects on non-pain-sensing neurons or other types of cells.Type: ApplicationFiled: March 11, 2009Publication date: April 14, 2011Applicants: Presidents and Fellows of Harvard College, The General Hospital CorporationInventors: Bruce P. Bean, Clifford J. Woolf
-
Patent number: 7923554Abstract: The present invention relates to HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R1 represents hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyloxycarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxyC1-6alkylcarbonyl substituted with C1-6alkyloxycarbonyl; R2 or R4 represents hydrogen; hydroxy; halo; optionally substituted C1-6alkyl; optionally substituted C2-6alkenyl; optionally substituted C2-6alkynyl; C3-7cycloalkyl; C1-6alkyloxy; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; carboxyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-4alkyl; polyhaloC1-4alkyloxy; polyhaloC1-4alkylthio; —S(?O)pR6; —NH—S(?O)pR6; —C(?O)R6; —NHC(?O)H; —C(?O)NHNH2; NHC(?O)R6; C(?NH)R6; or R7; R2a or R3 represents cyano; aminocarbonyl; amino; halo; NHR13; NR13R14; —C(?O)—NHR13; —C(?O)—NR13R1Type: GrantFiled: August 10, 2005Date of Patent: April 12, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Georges Joseph Cornelius Hoornaert, Amuri Kilonda, Jan Heeres, Paulus Joannes Lewi, Marc René de Jonge, Frederik Frans Desiré Daeyaert, Hendrik Maarten Vinkers, Lucien Maria Henricus Koymans, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative
-
Publication number: 20110059974Abstract: Retinoic acid metabolism blocking agents (RAMBAs). The RAMBAs may be used for treatment of cancer, including breast and prostate cancers. Methods for preparing novel retinamide RAMBAs. The methods include reacting RAMBAs with terminal polar carboxylic acid group with a variety of amines in the presence of suitable coupling reagents. The retinamide RAMBAs are potent inhibitors of the growth of prostate and breast cancer cells and may be useful for the treatment of these diseases in humans.Type: ApplicationFiled: May 7, 2009Publication date: March 10, 2011Applicant: UNIVERSITY OF MARYLAND, BALTIMOREInventors: Vincent C. O. Njar, Lalji K. Gediya, Aakanksha Khandelwal
-
Publication number: 20110059973Abstract: The present invention relates to novel pyrazole compounds of the formulae I and II, to their salts and their N-oxides which can be used for combating or controlling invertebrate pests, in particular arthropod pests. The invention also relates to a method for controlling invertebrate pests by using these compounds. The present invention also relates to seed and to an agricultural and veterinary composition comprising said compounds. wherein A is a pyrazole radical of the formulae A1, A2 or A3 # denotes the binding site to the remainder of formulae I or II; X1 is S, O or NR1a; X2 is OR2a, NR2bR2c, S(O)mR2d; X3 is a lone pair or oxygen; R1, R2 and R3 are, inter alia, hydrogen, and wherein R41, R42, R43, R51, R52, R53, R61, R62, R63, are as defined in claim 1.Type: ApplicationFiled: August 26, 2008Publication date: March 10, 2011Applicant: BASF SEInventors: Steffen Gross, Delphine Breuninger, Henricus Maria Martinus Bastiaans, Wolfgang von Deyn, Michael Puhl, Karsten Koerber, Douglas D. Anspaugh, Deborah L. Culbertson, Hassan Oloumi-Sadeghi
-
Publication number: 20110052686Abstract: The present invention relates to uncoated modified-release tablets of lamotrigine and the process for preparation thereof, wherein the tablets comprise a portion of lamotrigine in an admixture with a pH-dependent polymer.Type: ApplicationFiled: September 2, 2010Publication date: March 3, 2011Applicant: RANBAXY LABORATORIES LIMITEDInventors: Murali Krishna Bhavarisetti, Rajan K. Verma, Romi Barat Singh
-
Publication number: 20110053914Abstract: A pharmaceutical combination comprising: (a) at least one 6-dimethylaminomethyl-1-(3-methoxy-phenyl)-cyclohexane-1,3-diol component and/or at least one 6-dimethylaminomethyl-1-(3-hydroxy-phenyl)-cyclohexane-1,3-diol component, and (b) at least one antiepileptic; a pharmaceutical composition comprising said combination, a medicament comprising such a combination, a kit containing the ingredients of such a combination, and a method of treating pain in which components (a) and (b) are administered simultaneously or sequentially, whereby component (a) may be administered before or after component (b), and in which components (a) and (b) are administered either via the same or a different pathway of administration.Type: ApplicationFiled: August 27, 2010Publication date: March 3, 2011Applicant: Gruenenthal GmbHInventors: Klaus SCHIENE, Petra Bloms-Funke
-
Publication number: 20110053919Abstract: The novel active compound combinations comprising a compound of the formula (I) or (II) and the active compounds (1) to (6) listed in the description have very good insecticidal and acaricidal properties.Type: ApplicationFiled: July 6, 2007Publication date: March 3, 2011Applicant: BAYER CROPSCIENE AGInventors: Reiner Fischer, Wolfram Andersch, Thomas König, Anton Kraus, Emmanuel Salmon, Heike Hungenberg
-
Publication number: 20110045974Abstract: The present invention relates to triazinylmethyl sulfonamides of formula I wherein T, R1, R2, R3, A, Y and D are as defined in the claims and to the N-oxides, and salts thereof and their use for combating harmful fungi, and also to compositions and seed comprising at least one such compound. The invention also relates to processes and intermediates for preparing these compounds.Type: ApplicationFiled: March 11, 2009Publication date: February 24, 2011Applicant: BASF SEInventors: Jochen Dietz, Thomas Grote, Wassilios Grammenos, Bernd Mueller, Jan Klaas Lohmann, Jens Renner, Sarah Ulmschneider, Marianna Vrettou, Alice Glaettli
-
Patent number: 7888356Abstract: The structure and preparation of antibiotics incorporating borinic acid complexes are disclosed, especially hydroxyquinoline, imidazole and picolinic acid derivatives, along with compositions of these antibiotics and methods of using the antibiotics and compositions as bactericidal and fungicidal agents as well as therapeutic agents for the treatment of diseases caused by bacteria and fungi.Type: GrantFiled: January 9, 2008Date of Patent: February 15, 2011Assignee: Anacor Pharmaceuticals, Inc.Inventors: Ving Lee, Stephen J. Benkovic, Stephen J. Baker, Kirk R. Maples, Tsutomu Akama, Yong-Kang Zhang, Rajesjwar Singh, Vittorio A. Sauro, Chetan Pandit, Zhuoyi Su, Zhixiang Yang
-
Publication number: 20110034450Abstract: The present application relates to novel carboxylic acid derivatives having an oxo-substituted azaheterocyclic partial structure, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: April 6, 2009Publication date: February 10, 2011Applicant: BAYER SCHERING PHARMA AKTIEGESELLSCHAFTInventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Friederike Stoll, Stefan Heitmeier, Klaus Münter, Nils Griebenow, Thomas Lampe, Sherif El Sheikh, Volkhart Min-Jian Li
-
Patent number: 7880000Abstract: The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other poliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.Type: GrantFiled: May 9, 2005Date of Patent: February 1, 2011Assignee: Amgen Inc.Inventors: Stephanie D. Geuns-Meyer, Brian L. Hodous, Stuart C. Chaffee, Paul A. Tempest, Philip R. Olivieri, Rebecca E. Johnson, Brian K. Albrecht, Vinod F. Patel, Victor J. Cee, Joseph L. Kim, Steven Bellon, Xiaotian Zhu, Yuan Cheng, Ning Xi, Karina Romero, Hanh Nho Nguyen, Holly L. Deak
-
Publication number: 20110015076Abstract: The invention relates to a pesticidal composition comprising as active ingredient a mixture consisting of one compound (A) as defined in the patent claims and at least one compound (B) as defined in the patent claims, to a process for the preparation of and to the use of such a composition, to a method of controlling pests using such a composition and to plant propagation material treated with such a composition.Type: ApplicationFiled: September 10, 2010Publication date: January 20, 2011Applicant: Syngenta Crop Protection, Inc.Inventors: Max Angst, Ana Cristina Dutton
-
Publication number: 20110014304Abstract: The disclosure relates to pharmacotherapy of a psychiatric disorder which is schizophrenia and/or anxiety, wherein schizophrenia includes schizophrenia related disorders such as brief psychotic disorders, delusional disorders, schizoaffective disorders, and schizophreniform disorders, and anxiety includes panic disorders, obsessive-compulsive disorders (OCD), post-traumatic stress disorders (PTSD), social phobia or social anxiety disorders, specific phobia, and generalized anxiety disorders (GAD). The compounds of the disclosure are useful for the treatment of the above psychiatric disorders alone or in combination with other therapeutical agents effective in the treatment of schizophrenia and/or anxiety disorders.Type: ApplicationFiled: June 15, 2010Publication date: January 20, 2011Applicant: Newron Pharmaceuticals S.p.A.Inventors: Emanuela Izzo, Laura Faravelli, Elena Barbanti, Patricia Salvati
-
Publication number: 20110009413Abstract: Compounds of general structure in which X and Y are each N or C with at least one of X and Y being N; Z is a single bond or an optionally substituted linking group R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when RI is hydrogen or ?NH when R1 is a substituent group; or N* is a group NRaRb where Ra and Rb are independently H or an alkyl group; or N* is an optionally substituted piperazinyl ring; and A is an optionally substituted heterocyclic or carbocyclic ring system which may be linked to the triazo/diazo ring through R2 to form a fused multicyclic ring; are indicated as suitable for treatment of disorders in mammals that are susceptible to sodium channel blockers and antifolates, and particularly disorders such epilepsy, multiple sclerosis, glaucoma and uevitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motorneurone disease, Alzheimer's disease, Parkinson's disease, chronic inflType: ApplicationFiled: January 16, 2009Publication date: January 13, 2011Applicant: UNIVERSITY OF GREENWICHInventors: Michael Leach, Laurence Harbige, Dieter Riddall, Karl Franzmann