Asymmetrical (e.g., 1, 2, 4-triazines, Etc.) Patents (Class 544/182)
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Patent number: 12241094Abstract: Provided herein are phenazine degrading agents, methods and systems for interfering with viability of bacteria and related antimicrobial and compositions.Type: GrantFiled: September 21, 2020Date of Patent: March 4, 2025Assignee: CALIFORNIA INSTITUTE OF TECHNOLOGYInventors: Dianne K. Newman, Kyle C. Costa
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Patent number: 12180192Abstract: Disclosed herein are compounds of Formula I: TL-La-CE-HD??(I) or a pharmaceutically acceptable salt, prodrug, amide or ester thereof, where i) TL is a moiety of Formula IIa, IIb, IIIa, IIIb, IIIc, or IIId; ii) CE is a moiety of Formula IV; iii) HD is a moiety of Formula V or VI; where the substituents are as defined herein. Disclosed are also pharmaceutical compositions comprising the above compounds, and methods of treating disease by administering or contact a patient with one or more of the above compounds.Type: GrantFiled: May 25, 2021Date of Patent: December 31, 2024Assignee: Aligos Therapeutics, Inc.Inventors: Koen Vandyck, Pierre Jean-Marie Bernard Raboisson, David McGowan, Jerome Deval
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Patent number: 11884664Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: April 13, 2022Date of Patent: January 30, 2024Assignee: Array BioPharma Inc.Inventors: James Francis Blake, Mark Laurence Boys, Mark Joseph Chicarelli, Adam Wade Cook, Mohamed S. A. Elsayed, Jay Bradford Fell, John P. Fischer, Ronald Jay Hinklin, Yutong Jiang, Oren Teague McNulty, Macedonio J. Mejia, Martha E. Rodriguez, Christina Elizabeth Wong
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Patent number: 11874264Abstract: A computer-implemented method for reporting performance of an agricultural input for a plant involves: storing in a computer database a set of agricultural inputs, plants for which the agricultural inputs are used, performance attributes of the agricultural inputs, historical agricultural input performance values, and a relative significance of each of the agricultural inputs for the performance attribute. A computer processor is used to receive a plant selection; receive an attribute to be targeted for the plant selection; identify a plurality of agricultural inputs for affecting the targeted attribute for the plant using the historical agricultural input performance values; rank the plurality of agricultural inputs for affecting the targeted attribute for the selected plant using the relative significance associated therewith; and display the plurality of agricultural inputs and corresponding ranks for the received attribute associated with the selected plant.Type: GrantFiled: August 2, 2019Date of Patent: January 16, 2024Assignee: Heritage Landscape Supply Group, Inc.Inventor: Bruce A. Jump
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Patent number: 11634417Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: GrantFiled: March 31, 2020Date of Patent: April 25, 2023Assignee: Array BioPharma Inc.Inventors: James F. Blake, Mark Laurence Boys, Mark Joseph Chicarelli, Adam W. Cook, Mohamed S. A. Elsayed, Jay Bradford Fell, John P. Fischer, Ronald Jay Hinklin, Yutong Jiang, Oren T. McNulty, Macedonio J. Mejia, Martha E. Rodriguez, Christina E. Wong
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Patent number: 11203587Abstract: Provided herein are compounds, preferably thyroid hormone receptor beta (THR beta) agonist compounds, compositions thereof, methods of their preparation, and methods of agonizing THR beta and methods for treating disorders mediated by THR beta.Type: GrantFiled: October 10, 2019Date of Patent: December 21, 2021Assignee: TERNS, INC.Inventors: Thorsten A. Kirschberg, Randall Halcomb, Yingzi Xu, F. Anthony Romero
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Patent number: 11136615Abstract: Disclosed herein are compositions and methods for stabilizing a benzothiazole luciferin analog such as D-luciferin and 6-amino-D-luciferin. The compositions may include the benzothiazole luciferin analog, a thionucleobase compound of formula (I), and a liquid medium, in which the thionucleobase is present in an amount effective to stabilize the luminogenic composition against decomposition. The methods provided herein may stabilize the benzothiazole luciferin analog against decomposition by contacting the benzothiazole luciferin analog with an effective amount of the thionucleobase compound in the presence of a liquid medium. Also provided herein is a kit containing the composition.Type: GrantFiled: August 2, 2018Date of Patent: October 5, 2021Assignee: PROMEGA CORPORATIONInventors: Ce Shi, Mary P. Hall, Thomas A. Kirkland, Lance P. Encell, Poncho Meisenheimer, Wenhui Zhou
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Patent number: 11091467Abstract: Disclosed herein are compounds of Formula I: TL-La-CE-HD??(I) or a pharmaceutically acceptable salt, prodrug, amide or ester thereof, where i) TL is a moiety of Formula IIa, IIb, IIIa, IIIb, IIIc, or IIId; ii) CE is a moiety of Formula IV; iii) HD is a moiety of Formula V or VI; where the substituents are as defined herein. Disclosed are also pharmaceutical compositions comprising the above compounds, and methods of treating disease by administering or contact a patient with one or more of the above compounds.Type: GrantFiled: May 7, 2020Date of Patent: August 17, 2021Assignee: Aligos Therapeutics, Inc.Inventors: Koen Vandyck, Pierre Jean-Marie Bernard Raboisson, David McGowan, Jerome Deval
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Patent number: 11084802Abstract: The present invention discloses a compound represented by the following Formula (I) and a pharmaceutically acceptable salt thereof. The compound improves the THR? selectivity while maintaining good THR? agonistic activity, thereby improving properties of the finished drug.Type: GrantFiled: December 12, 2019Date of Patent: August 10, 2021Assignee: TERNS, INC.Inventors: Shanghai Yu, Ben Li
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Patent number: 11034676Abstract: The present invention discloses a compound represented by the following Formula (I) and a pharmaceutically acceptable salt thereof. The compound improves the THR? selectivity while maintaining good THR? agonistic activity, thereby improving properties of the finished drug.Type: GrantFiled: September 4, 2020Date of Patent: June 15, 2021Assignee: TERNS, INC.Inventors: Shanghai Yu, Ben Li
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Patent number: 10988455Abstract: 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: October 16, 2018Date of Patent: April 27, 2021Assignee: Heptares Therapeutics LimitedInventors: Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
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Patent number: 10793529Abstract: Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: GrantFiled: October 15, 2018Date of Patent: October 6, 2020Assignee: ARENA PHARMACEUTICALS, INC.Inventors: Thuy-Anh Tran, Rena Hayashi, Jason B. Ibarra, Brett Ullman, Ning Zou
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Patent number: 10695346Abstract: The present invention provides novel compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, prodrugs, and compositions thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., lung cancer, breast cancer, leukemia, lymphoma, melanoma, multiple myeloma, Ewing's sarcoma, osteosarcoma, brain cancer, neuroblastoma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of a kinase (e.g. a protein kinase (e.g. a cyclin-dependent kinase (CDK) (e.g. CDK7, CDK12, or CDK13) or a lipid kinase such as a phosphatidylinositol-5-phosphate 4-kinase (PIP4K) (e.g.Type: GrantFiled: June 24, 2016Date of Patent: June 30, 2020Assignee: Dana-Farber Cancer Institute, Inc.Inventors: Nathanael S. Gray, Tinghu Zhang
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Patent number: 10562901Abstract: A temozolomide compound according to formula (I) is described, wherein R1, L1, and X are defined herein. The temozolomide compound can be used to prepare polymers comprising temozolomide. Additionally, the polymers comprising temozolomide can be particularly useful in the treatment of certain diseases.Type: GrantFiled: September 20, 2017Date of Patent: February 18, 2020Assignee: THE UNIVERSITY OF MASSACHUSETTSInventors: Todd Emrick, Matthew Skinner, Sarah M. Ward, Banishree Saha
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Patent number: 10376517Abstract: The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TR? mutation.Type: GrantFiled: April 10, 2018Date of Patent: August 13, 2019Assignees: Madrigal Pharmaceuticals, Inc., Hoffmann-La Roche Inc.Inventors: Rebecca Taub, Charles H. Reynolds, Lianhe Shu, Ping Wang, Duk Soon Choi
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Patent number: 10329263Abstract: This invention provides a novel disubstituted 1,2,4-triazine compound or a pharmaceutically acceptable salt thereof, which has an aldosterone synthetase inhibitory activity and is useful for preventing and/or treating various diseases or conditions associated with aldosterone; a method for preparing it; use of it; as well as a pharmaceutical composition comprising it as an active ingredient. A compound of the general formula [I]: wherein RA is, for example, a group of the following formula (A-1): wherein ring A1 is, for example, a cycloalkyl group which may be substituted, and RB is, for example, a monocyclic cycloalkyl group, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: June 22, 2018Date of Patent: June 25, 2019Assignee: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Hideki Ushirogochi, Wataru Sasaki, Yuichi Onda, Ryo Sakakibara, Fumihiko Akahoshi
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Patent number: 10189859Abstract: The instant disclosure relates to (among other things) compounds that are derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine. The compounds provided possess unique effects and differences over other phenyltriazines known in the art.Type: GrantFiled: December 19, 2014Date of Patent: January 29, 2019Assignee: Nektar TherapeuticsInventors: Pankaj Sharma, Vijay Kumar Khatri, Xuyuan Gu, Yuan Song, Michael Lixin Shen, Jennifer Riggs-Sauthier, Neel K. Anand, Antoni Kozlowski, Aleksandrs Odinecs, Timothy A. Riley, Zhongxu Ren, YongQi Mu, Xiaoming Shen, Xuejun Yuan, Natalia Aurrecoechea, Donogh John Roger O'Mahony, Bo-Liang Deng
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Patent number: 10112923Abstract: 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 carbocylic 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, whichType: GrantFiled: November 4, 2016Date of Patent: October 30, 2018Assignee: Heptares Therapeutics LimitedInventors: Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
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Patent number: 9988372Abstract: The present invention relates to a novel crystalline form of 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 methanesulfonate and a pharmaceutical composition containing the same. The novel crystalline form of a compound according to the present invention exhibits excellent stability even in high-temperature and humidity environments, and thus can be favorably used to prevent or treat diseases, such as thrombosis, myocardial infarction, atherosclerosis, inflammation, stroke, angina pectoris, restenosis after angioplasty, and thromboembolism.Type: GrantFiled: July 18, 2014Date of Patent: June 5, 2018Assignees: GREEN CROSS CORPORATION, LEGOCHEM BIOSCIENCES, INC.Inventors: Soongyu Choi, Jungsub Choi, So-Hyun Yoon, Yoo Hoon Kim, Jae Yeon Kim, Suk Ho Lee, Young Lag Cho, Ho Young Song, Dae Yon Lee, Sung Yoon Baek, Sang Eun Chae, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
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Patent number: 9617228Abstract: The invention relates to (among other things) methods for treatment comprising administering 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: January 15, 2016Date of Patent: April 11, 2017Assignee: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
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Patent number: 9573908Abstract: Using a whole-cell high-throughput screen, eleven molecules were identified that activate V. cholerae quorum sensing (QS). Eight molecules are receptor agonists and three molecules are antagonists of LuxO, the central NtrC-type response regulator that controls the global V. cholerae QS cascade. Pro-QS molecules are used for the development of novel anti-infectives.Type: GrantFiled: February 20, 2013Date of Patent: February 21, 2017Assignee: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Bonnie L. Bassler, Wai-Leung Ng, Lark J. Perez, Jianping Cong, Martin F. Semmelhack
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Patent number: 9505753Abstract: D-amino acid oxidase (DAAO) inhibitors and methods of their use, either alone or in combination with D-serine or D-alanine, to facilitate allosteric activation of NMDA receptor-mediated neurotransmission and methods of their use as therapeutic agents for treating a subject afflicted with one or more cognitive-disorders, such as schizophrenia, including subjects suffering from negative symptoms and cognitive impairments, post-traumatic stress disorder (PTSD), or pain, are disclosed.Type: GrantFiled: August 8, 2013Date of Patent: November 29, 2016Assignee: THE JOHNS HOPKINS UNIVERSITYInventors: Takashi Tsukamoto, Barbara Stauch Slusher, Dana V. Ferraris, Camilo Rojas, Niyada Hin, Bridget Duvall
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Patent number: 9416114Abstract: This invention relates to 1,2,4-triazine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.Type: GrantFiled: October 1, 2013Date of Patent: August 16, 2016Assignees: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE DE ROUEN, INSTITUT NATIONAL DES SCIENCES APPLIQUEES DE ROUEN (INSA)Inventors: Vincent Gembus, Philippe Jubault, Christophe Hoarau, Vincent Levacher, Jean-Francois Bonfanti, David Graig McGowan, Jerome Emile Georges Guillemont
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Patent number: 9290481Abstract: The present invention relates to monocyclic heteroaryl cycloalkyldiamine derivatives of formula (I), to processes for their production, to their use as pharmaceuticals and to pharmaceutical compositions comprising them.Type: GrantFiled: May 15, 2013Date of Patent: March 22, 2016Assignee: NOVARTIS AGInventors: Alexander Baxter Smith, Gebhard Thoma, Maurice Van Eis
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Patent number: 9266861Abstract: The disclosure describes methods of synthesis of pyridazinone compounds as thyroid hormone analogs and their prodrugs. Preferred methods according to the disclosure allow for large-scale preparation of pyridazinone compounds having high purity. In some embodiments, preferred methods according to the disclosure also allow for the preparation of pyridazinone compounds in better yield than previously used methods for preparing such compounds. Also disclosed are morphic forms of a pyridazinone compound. Further disclosed is a method for treating resistance to thyroid hormone in a subject having at least one TR? mutation.Type: GrantFiled: March 17, 2015Date of Patent: February 23, 2016Assignees: Madrigal Pharmaceuticals, Inc., Hoffmann-La Roche Inc.Inventors: D. Keith Hester, II, Robert J. Duguid, Martha J. Kelly, Anna Chasnoff, Gang Dong, Edwin L. Crow, Duk Soon Choi, Lianhe Shu, Ping Wang
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Patent number: 9266845Abstract: The invention relates to (among other things) methods for treatment comprising administering 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: October 30, 2014Date of Patent: February 23, 2016Assignee: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
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Patent number: 9249130Abstract: 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: July 2, 2014Date of Patent: February 2, 2016Assignee: Heptares Therapeutics LimitedInventors: Miles Stuart Congreve, Stephen Philippe Andrews, Jonathan Stephen Mason, Christine Mary Richardson, Giles Albert Brown
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Patent number: 9232801Abstract: 1,2,4-Triazine-3,5-dione-6-carboxamides of the general formula (I) are described as herbicides. In this formula (I), R1 and R2 are radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. Q is a tetrazolyl, triazolyl or oxadiazolyl radical. Z and Y are each oxygen or sulfur.Type: GrantFiled: October 1, 2013Date of Patent: January 12, 2016Assignee: BAYER CROPSCIENCE AGInventors: Ralf Braun, Christian Waldraff, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler
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Patent number: 9040618Abstract: 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: GrantFiled: April 16, 2012Date of Patent: May 26, 2015Assignees: COMPAGNIE GENERALE DES ETABLISSEMENTS MICHELIN, MICHELIN RECHERCHE ET TECHNIQUE S.A.Inventors: Anne Veyland, Nicolas Seeboth
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Patent number: 9040530Abstract: 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: GrantFiled: March 15, 2013Date of Patent: May 26, 2015Assignee: PORTOLA PHARMACEUTICALS, INC.Inventors: Zhaozhong J. Jia, Brian Kane, Jack Rose, Shawn M. Bauer, Yonghong Song, Qing Xu, Anjali Pandey
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Patent number: 9034850Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.Type: GrantFiled: November 19, 2010Date of Patent: May 19, 2015Assignee: SK Chemicals Co., Ltd.Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
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Publication number: 20150126474Abstract: Using a whole-cell high-throughput screen, eleven molecules were identified that activate V. cholerae quorum sensing (QS). Eight molecules are receptor agonists and three molecules are antagonists of LuxO, the central NtrC-type response regulator that controls the global V. cholerae QS cascade. Pro-QS molecules are used for the development of novel anti-infectives.Type: ApplicationFiled: February 20, 2013Publication date: May 7, 2015Applicant: THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Bonnie L. Bassler, Wai-Leung Ng, Lark J. Perez, Jianping Cong, Martin F. Semmelhack
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Patent number: 9024019Abstract: Compounds of the formula (I) or (I?), wherein the substituents are as defined in claim 1, are useful as pesticides.Type: GrantFiled: November 20, 2012Date of Patent: May 5, 2015Assignee: Syngenta Participations AGInventors: Sebastian Rendler, Jurgen Harry Schaetzer, Shuji Hachisu, Peter Maienfisch, Thomas Pitterna, Olivier Jacob, Jerome Yves Cassayre
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Patent number: 9018224Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: November 9, 2012Date of Patent: April 28, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Scott Edmondson, Zhiyong Hu, Ping Liu, Gregori J. Morriello, Jason W. Szewczyk, Bowei Wang, Liping Wang, Harold B. Wood, Cheng Zhu, Yuping Zhu, Zhiqiang Guo
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Publication number: 20150111857Abstract: Compounds and compositions useful for treating disorders related to KIT and PDFGR are described herein.Type: ApplicationFiled: October 17, 2014Publication date: April 23, 2015Applicant: BLUEPRINT MEDICINES CORPORATIONInventors: Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu, Douglas Wilson, Yulian Zhang
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Publication number: 20150105385Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: ApplicationFiled: December 17, 2014Publication date: April 16, 2015Inventors: Alfredo C. CASTRO, Katrina CHAN, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Liansheng LI, Tao LIU, Yi LIU, Pingda REN, Daniel A. SNYDER, Martin R. TREMBLAY
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Patent number: 9000155Abstract: 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: GrantFiled: April 30, 2014Date of Patent: April 7, 2015Assignee: University Of GreenwichInventors: Michael Leach, Karl Franzmann, Dieter Riddall, Laurence Harbige
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Publication number: 20150094308Abstract: The present application relates to novel substituted fused pyrimidines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: January 8, 2013Publication date: April 2, 2015Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Nils Griebenow, Frank Wunder, Dieter Lang
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Patent number: 8987256Abstract: 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: GrantFiled: April 6, 2009Date of Patent: March 24, 2015Assignee: Bayer Intellectual Property GmbHInventors: 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
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Publication number: 20150072986Abstract: The present invention provides novel compounds of any one of Formulae (I)-(III), and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I)-(III) and pharmaceutical compositions thereof that are mucus penetrating. The invention also provides methods and kits for using the inventive compounds, and pharmaceutical compositions thereof, for treating and/or preventing diseases associated with abnormal or pathological angiogenesis and/or aberrant signaling of a growth factor (e.g., vascular endothelial growth factor (VEGF)), such as proliferative diseases (e.g., cancers, benign neoplasms, inflammatory diseases, autoimmune diseases) and ocular diseases (e.g., macular degeneration, glaucoma, diabetic retinopathy, retinoblastoma, edema, uveitis, dry eye, blepharitis, and post-surgical inflammation) in a subject in need thereof.Type: ApplicationFiled: June 11, 2014Publication date: March 12, 2015Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, John Thomas Feutrill, Jinsoo Kim, Minh Ngoc Nguyen, Elizabeth Enlow
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Publication number: 20150065706Abstract: The invention relates to (among other things) methods for treatment comprising administering 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: ApplicationFiled: October 30, 2014Publication date: March 5, 2015Inventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
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Patent number: 8969554Abstract: Disclosed are compounds exhibiting sufficient herbicidal activity at low application dosage when they are applied to soils and foliage, and an agrochemical composition using the same, in particular herbicides. The compounds are triazine derivatives represented by following Formula 1 or salts thereof, and the herbicides containing them: [Chem. 28] wherein in the formula, R1 represents a hydrogen atom; a C1-C12 alkyl group; a C2-C6 alkenyl group, etc., R2 represents a C1-C12 alkyl group, etc., Y and Z represent an oxygen atom or a sulfur atom, and A represents a 5- or 6-membered cyclic group which may contain a nitrogen atom, an oxygen atom, or a sulfur atom.Type: GrantFiled: May 26, 2011Date of Patent: March 3, 2015Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Atsushi Shibayama, Ryu Kajiki, Masami Kobayashi, Takashi Mitsunari, Atsushi Nagamatsu
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Modulators of the prostacyclin (PGI2) receptor useful for the treatment of disorders related thereto
Patent number: 8940891Abstract: Cyclohexane derivatives of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: GrantFiled: December 7, 2009Date of Patent: January 27, 2015Assignee: Arena Pharmaceuticals, Inc.Inventors: Thuy-Anh Tran, Rena Hayashi, Jason B. Ibarra, Brett Ullman, Ning Zou -
Publication number: 20140378432Abstract: Heteroaryl pyridone and aza-pyridone compounds are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: September 8, 2014Publication date: December 25, 2014Inventors: James John Crawford, Daniel Fred Ortwine, BinQing Wei, Wendy B. Young
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Publication number: 20140371223Abstract: 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: ApplicationFiled: June 16, 2014Publication date: December 18, 2014Applicant: Addex Pharma S.A.Inventors: Eric Riguet, Brice Campo, Antoine Gibelin, Karim Mhalla
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Publication number: 20140357599Abstract: 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 18, 2014Publication date: December 4, 2014Inventors: Mette Knak CHRISTENSEN, Fredrik BJORKLING
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Patent number: 8895553Abstract: The invention relates to (among other things) methods for treatment comprising administering 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 20, 2014Date of Patent: November 25, 2014Assignee: Nektar TherapeuticsInventors: Jennifer Riggs-Sauthier, Bo-Liang Deng
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Publication number: 20140343038Abstract: The present invention provides a compound represented by the following general formula (I) or a salt thereof which has a Syk inhibitory effect (in the formula R1 represents a hydrogen atom or an optionally substituted C1-C6 alkyl group; A represents a hydrogen atom, an optionally substituted C1-C8 alkyl group, an optionally substituted C2-C6 alkenyl group, an optionally substituted C2-C6 alkynyl group, an optionally substituted C3-C10 cycloalkyl group, an optionally substituted C6-C14 aromatic hydrocarbon group, an optionally substituted 4- to 10-membered unsaturated heterocyclic group, or an optionally substituted 4- to 10-membered saturated heterocyclic group, or optionally forms a 4- to 10-membered unsaturated heterocyclic ring or a 4- to 10-membered saturated heterocyclic ring together with R1 and the nitrogen atom bonded thereto; R2 represents a hydrogen atom or an optionally substituted C1-C6 alkyl group; and B represents an optionally substituted unsaturated heterocyclic group).Type: ApplicationFiled: September 28, 2012Publication date: November 20, 2014Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Toshihiro Sakamoto, Takashi Mita, Kazuaki Shibata, Yoshio Ogino, Hideya Komatani
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Publication number: 20140336186Abstract: 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 9, 2014Publication date: November 13, 2014Inventors: Thomas BRETSCHNEIDER, Eva-Maria FRANKEN, Ulrich GÖRGENS, Martin FÜSSLEIN, Achim HENSE, Joachim KLUTH, Hans-Georg SCHWARZ, Adeline KÖHLER, Olga MALSAM, Arnd VOERSTE, Angela BECKER
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Publication number: 20140329819Abstract: Compounds of the formula (I) or (I?), wherein the substituents are as defined in claim 1, are useful as pesticides.Type: ApplicationFiled: November 20, 2012Publication date: November 6, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Sebastian Rendler, Jurgen Harry Schaetzer, Shuji Hachisu, Peter Maienfisch, Thomas Pitterna, Olivier Jacob, Jerome Yves Cassayre