Asymmetrical (e.g., 1, 2, 4-triazines, Etc.) Patents (Class 544/182)
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Publication number: 20140275077Abstract: The present application provides compounds of Formula I or salt forms thereof, wherein Ra, Rb, Rc, Rd, D, W, R1a, R1b, R1c, Y, R3, X, E and G are as defined herein, compositions, methods of treatment and uses thereof.Type: ApplicationFiled: May 13, 2014Publication date: September 18, 2014Applicant: Cephalon, Inc.Inventors: Reddeppa Reddy Dandu, Robert L. Hudkins, Kurt A. Josef, Catherine P. Prouty, Rabindranath Tripathy
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Patent number: 8822465Abstract: The present invention relates to a quinoline derivative represented by general formula (I) or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof, wherein Ar, R1, R2, R3, X, Y and n have the meanings given in the description. The present invention also relates to the comparatively strong effect of the compound represented by general formula (I) on inhibiting c-Met kinase. The present invention further relates to the use of this compound or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof in the manufacturing of a medicament for treating the disease caused by abnormally over-expressing c-Met kinase, in particular, for treating or preventing cancer.Type: GrantFiled: March 14, 2013Date of Patent: September 2, 2014Assignee: Wuhan Shengyun Biopharma Co., Ltd.Inventor: Hua Xu
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Publication number: 20140243343Abstract: The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The compounds are of formula I: in which R1 is a halo-alkyl group and A is an optionally substituted aromatic heterocyclic or carbocyclic ring system, or a pharmaceutically acceptable salt or solvate thereof.Type: ApplicationFiled: April 30, 2014Publication date: August 28, 2014Applicant: University of GreenwichInventors: Michael Leach, Karl Franzmann, Dieter Riddall, Laurence Harbige
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Patent number: 8816079Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, or a pharmacologically acceptable salt thereof.Type: GrantFiled: April 27, 2011Date of Patent: August 26, 2014Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Kazuhiro Maeda, Jun-ichi Endoh, Akiko Tarao, Kaoru Tashiro, Seigo Ishibuchi, Hidemasa Hikawa
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Patent number: 8809525Abstract: According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1-A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, whicType: GrantFiled: February 7, 2011Date of Patent: August 19, 2014Assignee: Heptares Therapeutics LimitedInventors: Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
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Publication number: 20140221362Abstract: 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: February 4, 2014Publication date: August 7, 2014Applicant: Bayer CropScience AGInventors: Thomas BRETSCHNEIDER, Martin Füßlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria FRANKEN, Arnd VOERSTE
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Publication number: 20140213590Abstract: Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.Type: ApplicationFiled: January 3, 2014Publication date: July 31, 2014Applicant: FOCHON PHARMA, INC.Inventors: WEIBO WANG, TONGSHUANG LI
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Patent number: 8779129Abstract: The present invention provides novel compounds of formula I wherein W1, W2, W3, W4, W5, B, X1, X2, X3, X4, X5, E and L are as defined herein; invention compounds are gamma amino butyrique acid receptor-subtype B (“GABAB”) positive allosteric modulators (enhancers), which are useful to provide methods of treating or preventing diseases or disorders, including treatment of anxiety, depression, epilepsy, schizophrenia, cognitive disorders, spasticity and skeletal muscle rigidity, spinal cord injury, multiple sclerosis, amyotrophic lateral sclerosis, cerebral palsy, neuropathic pain and craving associated with cocaine and nicotine, panic disorder, posttraumatic stress disorders, urge urinary incontinence, gastroesophageal reflux disease, transient lower oesophageal sphincter relaxations, functional gastrointestinal disorders and irritable bowel syndrome.Type: GrantFiled: December 14, 2012Date of Patent: July 15, 2014Assignee: Addex Pharma S.A.Inventors: Eric Riguet, Brice Campo, Antoine Gibelin, Karim Mhalla
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Patent number: 8772479Abstract: The invention relates to (among other things) oligomer-containing substituted aromatic triazine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.Type: GrantFiled: May 13, 2010Date of Patent: July 8, 2014Assignee: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
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Patent number: 8772291Abstract: This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders.Type: GrantFiled: December 8, 2009Date of Patent: July 8, 2014Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Joseph Barbosa, Li Dong, Cynthia Anne Fink, Jiancheng Wang, G. Gregory Zipp
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Patent number: 8765943Abstract: A 1,2,4-triazine of formula (I): and its process of manufacture and use.Type: GrantFiled: October 8, 2010Date of Patent: July 1, 2014Assignees: Compagnie Generale des Etablissements Michelin, Michelin Recherche et Technique S.A.Inventors: Nicolas Seeboth, Sergey Ivanov, Sergey Molkov
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Publication number: 20140179691Abstract: Disclosed is a novel oxazolidinone derivative represented by Formula 1 above, in particular, a novel oxazolidinone compound having a cyclic amidoxime or cyclic amidrazone group. In Formula 1, R and Q are the same as defined in the detailed description. In addition, disclosed is a pharmaceutical composition for an antibiotic which includes the novel oxazolidinone derivative of Formula 1, a prodrug thereof, a hydrate thereof, a solvate thereof, an isomer thereof, or a pharmaceutically acceptable salt thereof as an active ingredient. The novel oxazolidinone derivative, the prodrug thereof, the hydrate thereof, the solvate thereof, the isomer thereof, and the pharmaceutically acceptable salt thereof have broad antibacterial spectrum against resistant bacteria, low toxicity and strong antibacterial effects against Gram-positive and Gram-negative bacteria and thus may be effectively used as antibiotics.Type: ApplicationFiled: March 29, 2012Publication date: June 26, 2014Applicant: LEGOCHEM BIOSCIENCES, INC.Inventors: Young Lag Cho, Sung Yoon Baek, Sang Eun Chae, Sun Young Kim, Hong Bum Lee, Hyang Sook Lee, Kyuman Oh, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim, Hye Jin Heo
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Patent number: 8754210Abstract: Disclosed are: a method for preparing a 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin-1-yl)phenyl]-1,3-oxazolidin-5-yl}-methyl)thiophene-2-carboxamide derivative, which is a inhibitor of blood coagulation factor Xa, in a high purity and yield; and a novel intermedicate used therein.Type: GrantFiled: July 7, 2010Date of Patent: June 17, 2014Assignees: Green Cross Corporation, Legochem Bioscience Ltd.Inventors: Young Lag Cho, Sang Eun Chae, Seong Jin Kim, Ho Young Song, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim, Jinhwa Lee, Suk Ho Lee
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Patent number: 8748599Abstract: The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The compounds are of formula (I): in which z is a single bond or an optionally substituted linking group, R1 is a halo-alkyl group; and A is an optionally substituted aromatic heterocyclic or carbocyclic ring system; or a salt thereof.Type: GrantFiled: July 8, 2010Date of Patent: June 10, 2014Assignee: University Of GreenwichInventors: Michael Leach, Karl Franzmann, Dieter Riddall, Laurence Harbige
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Patent number: 8748600Abstract: The present invention relates to triazine compounds having sodium channel blocking properties, and to use of the compounds for preparation of medicaments for treatment of associated disorders. The triazine compounds are of formula (I) wherein: R1 is hydrogen or a substituent group; R2 is amino or a substituent group; N* is amino when R1 is hydrogen or ?NH when R1 is a substituent group; R3 and R4 are both carbocyclic, heterocyclic or alkyl groups and may be same or different; and R5 is hydrogen, alkyl or a cyclic aryl group, with the proviso that: when R3 and R4 are both alkyl they are linked to form a cycloalkyl group, and R5 is a cyclic aromatic group; and when R3 and R4 are both carbocyclic or heterocyclic groups, R5 is hydrogen or an alkyl group; or a salt thereof.Type: GrantFiled: July 8, 2010Date of Patent: June 10, 2014Assignee: University of GreenwichInventors: Michael Leach, Karl Franzmann, Dieter Riddall, Laurence Harbige
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Publication number: 20140155403Abstract: A method of treating a disorder. The method includes administering to a subject in need thereof a compound of formula (I): Each of A, N*, X, Y, Z, R1, and R2 is defined herein. Also disclosed are compounds of the formula and a pharmaceutical composition containing such a compound.Type: ApplicationFiled: February 6, 2014Publication date: June 5, 2014Applicant: University of GreenwichInventors: Michael Leach, Laurence Harbige, Dieter Riddall, Karl Franzmann
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Patent number: 8703939Abstract: Provided are a method for preparing (R)-3-(3-fluoro-4-(1-methyl-5, 6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl) oxazolidin-2-one derivatives, which are oxazolidinone antibiotic compounds having a cyclic amidrazone group, represented by Chemical Formula 1, and intermediates thereof, and uses 3,4-difluoro-4-nitrobenzen as a starting material. According to the preparation method of the present invention, (R)-3-(3-fluoro-4-(1-methyl-5, 6-dihydro-1,2,4-triazin-4(1H)-yl)phenyl)-5-(substituted methyl) oxazolidin-2-one derivatives, which are useful as oxazolidinone antibiotics, can be prepared in high purity and high yield in a simpler manner than conventional methods.Type: GrantFiled: March 8, 2011Date of Patent: April 22, 2014Assignee: Legochem Biosciences, Inc.Inventors: Young Lag Cho, Sung Yoon Baek, Sang Eun Chae, Hong Bum Lee, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
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Publication number: 20140107125Abstract: Pharmaceutical compositions and compounds are provided. The compounds of the invention demonstrate anti-proliferative activity, and may promote apoptosis in cells lacking normal regulation of cell cycle and death. In one embodiment of the invention, pharmaceutical compositions of the compounds in combination with a physiologically acceptable carrier are provided. The pharmaceutical compositions are useful in the treatment of hyperproliferative disorders, which disorders include tumor growth, lymphoproliferative diseases, angiogenesis. The compounds of the invention are substituted pyrazoles and pyrazolines.Type: ApplicationFiled: April 29, 2013Publication date: April 17, 2014Applicant: Dermira (Canada), Inc.Inventor: Dermira (Canada), Inc.
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Publication number: 20140106968Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein A is a radical selected from the group consisting of and A, R1, R2, m, p, and q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: October 15, 2013Publication date: April 17, 2014Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: ANDREW EDMUND TAGGI, Andrew Duncan Satterfield
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Patent number: 8697698Abstract: This invention describes novel pyrazole compounds of formula III: wherein Z1, Z2, and Z3 are as described in the specification; Q is —S—, —O—, —N(R4)—, or —CH(R6)—; R1 is T-Ring D, wherein Ring D is a 5-7 membered monocyclic ring or 8-10 membered bicyclic ring selected from aryl, heteroaryl, heterocyclyl or carbocyclyl; and R2 and R2?are as described in the specification. The compounds are useful as protein kinase inhibitors, especially as inhibitors of Aurora-2 and GSK-3, for treating diseases such as cancer, diabetes and Alzheimer's disease.Type: GrantFiled: September 28, 2012Date of Patent: April 15, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: David Bebbington, Jean-Damien Charrier, Julian Golec, Francoise Pierard
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Publication number: 20140100323Abstract: A rubber composition for manufacturing tyres is based on one or more diene elastomers, one or more reinforcing fillers, and a vulcanization system. The vulcanization system includes one or more 1,2,4-triazine compounds chosen from compounds of formula I and compounds of formula II: Certain specific 1,2,4-triazine derivatives are described.Type: ApplicationFiled: April 16, 2012Publication date: April 10, 2014Applicants: MICHELIN RECHERCHE ET TECHNIQUE S.A., COMPAGNIE GENERALE DES ETABLISSEMENTS MICHELINInventors: Anne Veyland, Nicolas Seeboth
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Patent number: 8691818Abstract: 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: GrantFiled: January 16, 2009Date of Patent: April 8, 2014Assignee: University Of GreenwichInventors: Michael Leach, Laurence Harbige, Dieter Riddall, Karl Franzmann
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Patent number: 8685964Abstract: 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: GrantFiled: October 12, 2010Date of Patent: April 1, 2014Assignee: Bayer CropScience AGInventors: Thomas Bretschneider, Martin Füβlein, Adeline Köhler, Friedrich August Mühlthau, Eva-Maria Franken, Arnd Voerste
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Publication number: 20140080828Abstract: This disclosure relates to antiviral compounds disclosed herein and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising 2-((benzo[d]imidazol-2-yl)thio)-N-phenylpropanamide derivatives, N-phenyl-2-((1-phenyl-benzo[d]imidazol-2-yl)thio)propanamide derivatives, or 2-((benzo[d]imidazol-2-yl)thio)-N-(2-chloro-4-methylphenyl)propanamide derivatives. The derivatives may be substituted with one or more substituents. Typically, the pharmaceutical composition comprises a compound of Formula (I), or salt, prodrug, or ester thereof wherein X, Y, and R1 to R7 are described herein.Type: ApplicationFiled: March 28, 2012Publication date: March 20, 2014Applicants: CHILDREN'S HEATLHCARE OF ATLANTA, INC., EMORY UNIVERSITYInventors: Richard K. Plemper, James P. Snyder, Aiming Sun, John M. Ndungu, Jeong-Joong Yoon
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Publication number: 20140066406Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 15, 2013Publication date: March 6, 2014Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: ARIAD PHARMACEUTICALS, INC.
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Publication number: 20140068820Abstract: 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: November 6, 2013Publication date: March 6, 2014Applicant: BASF SEInventors: Steffen GROSS, Delphine BREUNINGER, Henricus Maria Martinus BASTIAANS, Wolfgang von DEYN, Michael PUHL, Karsten KOERBER, Douglas D. ANSPAUGH, Deborah L. CULBERSTON, Hassan OLOUMI-SADEGHI
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Publication number: 20140045830Abstract: The disclosure relates to Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein R1, R2, Qa, Y1, Z, A, B, Qx, E, G, J, M, U, W, and a are as defined herein, compositions comprising an effective amount of a Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Cyclic Urea- or Lactam-Substituted Quinoxaline-Type Piperidine Compound.Type: ApplicationFiled: July 26, 2013Publication date: February 13, 2014Applicants: Shionogi & Co., Ltd., Purdue Pharma L.P.Inventors: Naoki TSUNO, Tatsuhiko Ueno, Xiaoming Zhou
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Patent number: 8648073Abstract: Provided are certain dipeptidyl peptidase inhibitors, pharmaceutical compositions thereof, and methods of use therefor.Type: GrantFiled: December 28, 2010Date of Patent: February 11, 2014Assignee: Fochon Pharma, Inc.Inventors: Weibo Wang, Tongshuang Li
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Publication number: 20140005197Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.Type: ApplicationFiled: June 14, 2013Publication date: January 2, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Paul S. Charifson, Michael P. Clark, Ioana Davies, Huai Gao, Joseph M. Kennedy, Mark W. Ledeboer, Francois Maltais, Emanuele Perola
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Patent number: 8618287Abstract: 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: GrantFiled: July 7, 2009Date of Patent: December 31, 2013Assignee: Pierre Fabre MedicamentInventors: Isabelle Leroy, Elisabeth Dupont-Passelaigue, Karine Valeille, Yves Rival, Didier Junquero
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Publication number: 20130345191Abstract: Provided are triazine compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.Type: ApplicationFiled: March 15, 2013Publication date: December 26, 2013Applicant: Portola Pharmaceuticals, Inc.Inventors: Zhaozhong J. Jia, Brian Kane, Jack Rose, Shawn M. Bauer, Yonghong Song, Qing Xu, Anjali Pandey
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Publication number: 20130345218Abstract: Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, wherein the values of Structural Formula (I) are as described herein. A pharmaceutical composition comprises an effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle.Type: ApplicationFiled: June 14, 2013Publication date: December 26, 2013Inventors: Paul S. Charifson, Michael P. Clark, Upul K. Bandarage, Hongbo Deng, Ioana Davies, John P. Duffy, Luc J. Farmer, Huai Gao, Wenxin Gu, Joseph M. Kennedy, Mark W. Ledeboer, Brian Ledford, Francois Maltais, Emanuele Perola, Marion W. Wannamaker, Tiansheng Wang, Francesco G. Salituro
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Publication number: 20130345219Abstract: The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound.Type: ApplicationFiled: August 28, 2013Publication date: December 26, 2013Applicant: Synta Pharmaceuticals Corp.Inventors: Chi-Wan Lee, Teresa Prezewloka, Weiwen Ying, Minghu Song, Zhenjian Du, Kevin Foley, Dan Zhou, Shuzhen Qin
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Publication number: 20130310387Abstract: The present invention relates to monocyclic heteroaryl cycloalkyldiamine derivatives, to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: ApplicationFiled: May 13, 2013Publication date: November 21, 2013Applicant: NOVARTIS AGInventors: Gebhard Thoma, Alexander Baxter Smith, Maurice van Eis
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Publication number: 20130274263Abstract: Compounds of general formula (I), (II), (III) and (V) are described for use in modulating microtubule polymerisation and in the treatment of associated disease states. Use of compounds (I), (III) and (V) in the treatment of kinase-associated disease states is also described. Further described are novel compounds of formula (II), (III) and (V).Type: ApplicationFiled: March 12, 2013Publication date: October 17, 2013Inventors: Christopher John Burns, Andrew Frederick Wilks, Michael Francis Harte, Harrison Sikanyika, Emmanuelle Fantino
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Patent number: 8552183Abstract: The present invention relates to a process for linking two molecules by means of a Diels Alder reaction with inverse electron requirement (DARinv), comprising the following steps: reaction of a (a) triazine or tetrazine with one or more electron-attracting substituents on the ring as a diene component, the electron-attracting substituents being selected from: COOR C(O)NR2 CX3 (X=halogen) halogen CN SO2—R or SO3—R PR2 wherein R?H, alkyl, aryl, heterocycle, which in turn may be substituted, where appropriate, with alkyl, OH, SH, halogen, aryl, heterocycle, nitro, carboxyamido or amine group.Type: GrantFiled: June 18, 2007Date of Patent: October 8, 2013Assignee: Deutsches Krebsforschungszentrum Stiftung des Offentlichen RechtsInventors: Manfred Wiessler, Eduard Müller, Peter Lorenz, Christian Kliem, Heinz Fleischhacker
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Publication number: 20130252958Abstract: The present invention relates to a quinoline deravative represented by general formula (I) or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof, wherein Ar, R1, R2, R3, X, Y and n have the meanings given in the description. The present invention also relates to the comparatively strong effect of the compound represented by general formula (I) on inhibiting c-Met kinase. The present invention further relates to the use of this compound or a pharmaceutically acceptable salt, hydrate, solvate or prodrug thereof in the manufacturing of a medicament for treating the disease caused by abnormally over-expressing c-Met kinase, in particular, for treating or preventing cancer.Type: ApplicationFiled: March 14, 2013Publication date: September 26, 2013Inventor: Hua XU
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Publication number: 20130231342Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).Type: ApplicationFiled: July 27, 2011Publication date: September 5, 2013Applicant: Oryzon Fenomics S.A.Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Iñigo Tirapu Fernandez de la Cuesta, Maria de los Ángeles Estirate-Martinez
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Publication number: 20130231479Abstract: The present invention provides a pest control agent, acaricide or fungicide that contains, as the active ingredient thereof, at least one type of compound selected from the aryloxyurea compounds represented by formula (V) (wherein R1 to R5 each independently represents an alkyl group or the like, X is a halogen atom or the like, n is an integer of 0 to 5, and Z is an oxygen atom or sulfur atom) or salts thereof.Type: ApplicationFiled: October 6, 2011Publication date: September 5, 2013Inventors: Hironori Furukawa, Takehiko Nakamura, Tetsuo Tamai, Daisuke Hanai
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Patent number: 8524712Abstract: The present invention relates to compounds according to formulae (IA) to (ID) and compositions that inhibit the activity of Hsp90. The invention further relates to methods of inhibiting the activity of Hsp90 in a subject in need thereof and methods for preventing or treating hyperproliferative disorders, such as cancer, in a subject in need thereof comprising administering to the subject a compound of the invention, or a composition comprising such a compound.Type: GrantFiled: March 24, 2008Date of Patent: September 3, 2013Assignee: Synta Pharmaceuticals Corp.Inventors: Chi-Wan Lee, Teresa Przewloka, Weiwen Ying, Minghu Song, Zhenjian Du, Kevin Foley, Dan Zhou, Shuzhen Qin
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Publication number: 20130225527Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 15, 2013Publication date: August 29, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: ARIAD PHARMACEUTICALS, INC.
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Publication number: 20130225528Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 15, 2013Publication date: August 29, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: ARIAD Pharmaceuticals, Inc.
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Publication number: 20130210809Abstract: The present invention relates to novel compounds of Formula (1), wherein M, A and B are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors-subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: July 12, 2011Publication date: August 15, 2013Inventors: Christelle Boléa, Sylvain Celanire, Cédric Boudou, Lam Tang, Jean-Philippe Rocher, Nigel John Liverton
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Patent number: 8492540Abstract: The invention relates to compounds of the formula I: wherein A is a saturated or unsaturated hydrocarbon chain having a chain length of 4 to 6 carbon atoms, the hydrocarbon chain being unsubstituted or substituted by 1, 2 or 3 methyl groups; R1 is selected from the group consisting of hydrogen, C1-C3 alkyl and fluorinated C1-C3 alkyl; R2 is hydrogen, halogen, cyano, C1-C3 alkyl, C1-C3 alkoxy, fluorinated C1-C3 alkyl or fluorinated C1-C3 alkoxy; R3 is selected from the group consisting of branched C4-C6 alkyl and C3-C6 cycloalkyl, and R4 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C3-alkyl and fluorinated C3-C6 cycloalkyl. and the physiologically tolerated salts of these compounds and the N-oxides thereof.Type: GrantFiled: October 31, 2008Date of Patent: July 23, 2013Assignee: Abbott GmbH & Co. KGInventors: Wilfried Braje, Sean Colm Turner, Andreas Haupt, Udo Lange, Hervé Geneste, Karla Drescher, Liliane Unger, Ana Lucia Relo, Anton Bespalov
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Patent number: 8486927Abstract: The invention is directed to novel crystalline forms of lamotrigine. These novel crystalline forms of lamotrigine have improved dissolution and in-vivo absorption profile, as compared to pure lamotrigine. These novel crystalline forms of lamotrigine provide a substantial increase in the blood concentration of lamotrigine, as compared to pure lamotrigine when administered to a subject. These novel crystalline forms of lamotrigine also provide a slower, steady build up of lamotrigine blood concentration suitable for sustained release of lamotrigine in-vivo, as compared to pure lamotrigine.Type: GrantFiled: November 10, 2008Date of Patent: July 16, 2013Assignee: Thar PharmaceuticalsInventors: Mazen Hanna, Ning Shan, Miranda L. Cheney
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Publication number: 20130172323Abstract: The present invention relates to pyridazinone derivatives of general formula I, wherein the groups A, G and R1 are as defined in the application, the tautomers thereof, stereoisomers thereof, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: May 6, 2011Publication date: July 4, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias Grauert, Remko Bakker, Steffen Breitfelder, Frank Buettner, Peter Eickelmann, Thomas Fox, Marc Grundl, Thorsten Lehmann-Lintz, Wolfgang Rist
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Publication number: 20130156699Abstract: The present invention relates to Radiolabeled Compounds labeled with fluorine, bromine, iodine, carbon, or tritium isotopes and methods of use thereof for treating or preventing a psychiatric disorder in a subject, for stabilizing the mood of a subject having a mood disorder, or as imaging agents for a serotonin receptor. Compositions comprising an imaging-effective amount of a Radiolabeled Compound are also disclosed.Type: ApplicationFiled: November 5, 2012Publication date: June 20, 2013Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Joseph John MANN, J.S. Dileep KUMAR
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Publication number: 20130150368Abstract: Provided are compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein R2, R4, R5, R6, R7, R8, R9, X, Z1, Z2, Z3, Z4 and m are as defined herein. Also provided is a pharmaceutically acceptable composition comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof. Also provided are methods of using a compound of Formula I, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 22, 2011Publication date: June 13, 2013Applicant: CYTOKINETICS, INC.Inventors: Luke W. Ashcraft, Gustave Bergnes, Scott Collibee, Chihyuan Chuang, Jeff Gardina, Bradley P. Morgan, Alex R. Muci, Xiangping Qian, Antonio Romero, Jeffrey Warrington, Zhe Yang
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Patent number: RE44338Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.Type: GrantFiled: July 17, 2012Date of Patent: July 2, 2013Assignee: The Trustees Of The University Of PennsylvaniaInventors: Hank F. Kung, Mei-Ping Kung, Zhi-Ping Zhuang, Virginia M. Y. Lee, John Q. Trojanowski, Daniel M. Skovronsky
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Patent number: RE44354Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form-amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.Type: GrantFiled: July 17, 2012Date of Patent: July 9, 2013Assignee: The Trustees Of The University Of PennsylvaniaInventors: Hank F. Kung, Mei-Ping Kung, Zhi-Ping Zhuang, Virginia M. Y. Lee, John Q. Trojanowski, Daniel M. Skovronsky