Additional Hetero Ring Which Is Unsaturated Patents (Class 544/324)
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Patent number: 11542260Abstract: The present disclosure relates to compounds capable of emitting delayed fluorescence and uses of these compounds in organic light-emitting diodes.Type: GrantFiled: January 30, 2019Date of Patent: January 3, 2023Assignee: KYULUX, INC.Inventors: Shuo-Hsien Cheng, Yu Seok Yang, Yoshitake Suzuki, Hayato Kakizoe, Ayataka Endo, Jorge Aguilera-Iparraguirre, Timothy D. Hirzel
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Patent number: 11505539Abstract: The present application relates to compounds of Formula I (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB and/or by degrading BCL6, such as cancer.Type: GrantFiled: December 21, 2018Date of Patent: November 22, 2022Assignee: Ontario Institute for Cancer Research (OICR)Inventors: Methvin Isaac, Anh My Chau, Ahmed Mamai
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Patent number: 11427570Abstract: The present invention is relates to an improved process for the preparation of pazopanib or a pharmaceutically acceptable salts thereof. The present invention also relates to novel polymorphic Forms of pazopanib hydrochloride, and its intermediates thereof.Type: GrantFiled: February 26, 2020Date of Patent: August 30, 2022Assignee: Laurus Labs LimitedInventors: Satyanarayana Chava, Seeta Rama Anjaneyulu Gorantla, Venkata Sunil Kumar Indukuri, Sanjay Kumar Dehury, Nagaraju Mekala, Jahangeer Baba Shaik, Durga Prasad Kuchipudi
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Patent number: 11427571Abstract: The present disclosure relates to crystalline polymorph and amorphous forms of 2-methyl-2-(3-methyl-4-(4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-1H-pyrazol-1-yl)propanenitrile or solvates, tautomers, and pharmaceutically acceptable salts or cocrystals thereof, and processes for their preparation.Type: GrantFiled: November 27, 2020Date of Patent: August 30, 2022Inventors: Travis Remarchuk, Anantha Sudhakar
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Patent number: 11192880Abstract: The present application relates to compounds of Formula I or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB and/or by degrading BCL6, such as cancer.Type: GrantFiled: December 20, 2018Date of Patent: December 7, 2021Assignee: ONTARIO INSTITUTE FOR CANCER RESEARCH (OICR)Inventors: Methvin Isaac, Anh My Chau
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Patent number: 11155549Abstract: The invention provides compounds of formula (I): or pharmaceutically-acceptable salts thereof, that are inhibitors of Janus kinases and release an active metabolite in vivo. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat inflammatory skin diseases and other diseases.Type: GrantFiled: April 23, 2020Date of Patent: October 26, 2021Assignee: Theravance Biopharma R&D IP, LLCInventors: Philip A. Gerken, Jianhua Chao, Daniel D. Long
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Patent number: 10898474Abstract: Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.Type: GrantFiled: June 27, 2019Date of Patent: January 26, 2021Assignee: INTERMUNE, INC.Inventors: Brad Owen Buckman, John Beamond Nicholas, Johnnie Y. Ramphal, Kumaraswamy Emayan, Scott D. Seiwert
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Patent number: 10851088Abstract: The present disclosure relates to crystalline polymorph and amorphous forms of 2-methyl-2-(3-methyl-4-(4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-1H-pyrazol-1-yl)propanenitrile or solvates, tautomers, and pharmaceutically acceptable salts or cocrystals thereof, and processes for their preparation.Type: GrantFiled: June 20, 2019Date of Patent: December 1, 2020Assignee: Denali Therapeutics Inc.Inventors: Travis Remarchuk, Anantha Sudhakar
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Patent number: 10632119Abstract: The present invention provides a compound of formula (I) or a salt form thereof. The compound of formula (I) has ALK and FAK inhibitory activity, and may be used to treat proliferative disorders.Type: GrantFiled: October 26, 2018Date of Patent: April 28, 2020Assignee: CEPHALON, INC.Inventors: Shawn P. Allwein, Laurent Courvoisier, Martin J. Jacobs, Gregory R. Ott
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Patent number: 10626110Abstract: The present disclosure provides a crystalline form F of Pazopanib HCl, which is characterized by an X-ray diffraction (XRD) pattern having peaks at about 11.3, 14.6, 16.9, 19.5, 19.7, 23.5 and 25.9°±0.2° 2?. The present disclosure also provides a preparation process of a crystalline form F of Pazopanib HCl.Type: GrantFiled: August 7, 2018Date of Patent: April 21, 2020Assignee: FORMOSA LABORATORIES, INC.Inventor: Sheng-Kai Ko
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Patent number: 10501440Abstract: Disclosed are heteroarylcarboxamides of formula (I), and pharmaceutically acceptable salts thereof, wherein A, T, R1, R2 and R3 are as defined herein. Also disclosed are methods of using these compounds for the treatment of diseases which can be influenced by inhibition of plasma kallikrein.Type: GrantFiled: April 16, 2018Date of Patent: December 10, 2019Assignee: Boehringer Ingelheim International GmbHInventors: Sara Frattini, Iain Lingard, Dieter Wolfgang Hamprecht, Remko Alexander Bakker, Matthias Eckhardt, Andreas Gollner, Joerg P. Hehn, Elke Langkopf, Holger Wagner, Bernd Wellenzohn, Dieter Wiedenmayer
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Patent number: 10370361Abstract: The present disclosure relates to crystalline polymorph and amorphous forms of 2-methyl-2-(3-methyl-4-(4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-1H-pyrazol-1-yl)propanenitrile or solvates, tautomers, and pharmaceutically acceptable salts or cocrystals thereof, and processes for their preparation.Type: GrantFiled: November 20, 2018Date of Patent: August 6, 2019Assignee: Denali Therapeutics Inc.Inventors: Travis Remarchuk, Anantha Sudhakar
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Patent number: 10023562Abstract: Compounds having the following formula: or a stereoisomer or a pharmaceutically-acceptable salt thereof, wherein R2 is a monocyclic heteroaryl group, and R1, R3, R4, R5 and R6 are as defined herein, are useful as kinase modulators, including IRAK-4 inhibition.Type: GrantFiled: April 6, 2017Date of Patent: July 17, 2018Assignee: Bristol-Myers Squibb CompanyInventors: Rajeev S. Bhide, John V. Duncia, John Hynes, Satheesh K. Nair, William J. Pitts, Sreekantha R. Kumar, Daniel S. Gardner, Natesan Murugesan, Venkatram Reddy Paidi, Joseph B. Santella, Ramesh Sistla, Hong Wu
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Patent number: 9993491Abstract: The present invention includes novel compounds and pharmaceutically acceptable formulations of said compounds which exhibit antibiotic activity against microorganisms bearing a guanine riboswitch that controls the expression of the guaA gene, including organisms which are resistant to certain antibiotic families, and which are useful as antibacterial agents for treatment or prophylaxis of bacterial infections in animals or in humans, in particular but not limited to infections of the mammary gland, or their use as antiseptics, agents for sterilization or disinfection.Type: GrantFiled: February 6, 2015Date of Patent: June 12, 2018Assignee: SOCPRA—SCIENCES ET GÉNIE S.E.C.Inventors: Jerome Mulhbacher, Daniel Lafontaine, Francois Malouin, Marianne Allard, Eric Marsault
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Patent number: 9926298Abstract: Heterocyclic compounds of Formula (I) shown herein. Also disclosed are pharmaceutical compositions containing the heterocyclic compounds and methods of using the heterocyclic compounds to mobilize hematopoietic stem cells and endothelial progenitor cells into the peripheral circulation. Further provided are methods for treating tissue injury, cancer, inflammatory disease, and autoimmune disease with the heterocyclic compounds.Type: GrantFiled: September 22, 2017Date of Patent: March 27, 2018Assignee: National Health Research InstitutesInventors: Kak-Shan Shia, Jiing-Jyh Jan, Lun Kelvin Tsou, Chiung-Tong Chen, Yu-Sheng Chao
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Patent number: 9447095Abstract: The present invention relates to novel pyrimidine derivatives of formula (I) as inhibitors of the enzyme phosphodiesterase 10 (PDE-10), pharmaceutical compositions comprising an effective amount of these compounds and the use of the compounds for manufacturing a medicament for the treatment of pathological conditions or diseases that can improve by inhibition of the enzyme Phosphodiesterase 10 such as neurological, psychiatric, respiratory or metabolic diseases.Type: GrantFiled: January 24, 2014Date of Patent: September 20, 2016Assignee: PALOBIOFARMA S.L.Inventors: Juan Camacho Gómez, Julio Castro Palomino Laria
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Patent number: 9428492Abstract: The present invention is directed to secondary alcohol substituted triazole compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: November 11, 2013Date of Patent: August 30, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Christopher D. Cox, Vadim Y. Dudkin, Carol A. McVean, Thomas S. Reger, Justin T. Steen
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Patent number: 9359348Abstract: The present invention is directed to substituted cyclopropyl imidazopyridine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: November 11, 2013Date of Patent: June 7, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Douglas C. Beshore, Thomas S. Reger
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Patent number: 9284302Abstract: The present invention is directed to substituted cyclobutyl benzimidazole compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: November 11, 2013Date of Patent: March 15, 2016Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Casey C. McComas, Thomas S. Reger
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Publication number: 20150126504Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: January 12, 2015Publication date: May 7, 2015Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
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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: 20150111883Abstract: Compounds of Formula (I) and methods for inhibiting kinases, including spleen tyrosine kinases, are disclosed. Also disclosed are methods for treating a kinase-mediated disease or condition by administering to a subject a therapeutically effective amount of the compound of Formula (I).Type: ApplicationFiled: October 21, 2014Publication date: April 23, 2015Inventors: Jaekyoo Lee, Jang-Sik Choi, Hae-Jun Hwang, Ho-Juhn Song, Jung-Ho Kim, Se-Won Kim, Jong Sung Koh, Jaesang Lee, Tae-Im Lee, Yung-Geun Choi, Sung-Ho Park, In Yong Lee, Byung-Chul Suh, Paresh Devidas Salgaonkar, Dong-Sik Jung
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Patent number: 9006243Abstract: HIV replication inhibitors of formula R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2, R3, R6 and R7 are hydrogen; hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(?O)R9; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 and R5 are hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; formyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(?O)R9; cyano; —S(?O)rR9; —NH—S(?O)2R9; —NHC(?O)H; —C(?O)NHNH2; —NHC(?O)R9; Het; —Y-Het; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R5 is pyridyl, —C(?O)NR5aR5b; —CH(OR5c)R5d; —CH2—NR5eR5f; —CH?NOR5a; —CH2—O—C2-6alkenyl; —CH2—O—P(?O)(OR5g)2; —CH2—O—C(?O)—NH2; —C(?O)—R5d; X is —NR1—, —O—, —CH2—, —S—; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compouType: GrantFiled: December 28, 2007Date of Patent: April 14, 2015Assignee: Janssen R&D IrelandInventors: Jerôme Emile Georges Guillemont, Céline Isabelle Mordant
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Publication number: 20150099743Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disease pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.Type: ApplicationFiled: October 3, 2014Publication date: April 9, 2015Inventors: Hui LI, Seiji NUKUI, Stephanie Anne SCALES, Min TENG, Chunfeng YIN
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Publication number: 20150099875Abstract: The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions.Type: ApplicationFiled: October 6, 2014Publication date: April 9, 2015Inventors: Jean-Damien Charrier, Michael Edward O'Donnell
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Publication number: 20150099749Abstract: This invention concerns pyrimidine derivatives of formula having HIV (Human Immunodeficiency Virus) replication inhibiting properties, the preparation thereof and pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: December 10, 2014Publication date: April 9, 2015Inventors: Jerôme Emile Georges Guillemont, Mikaël Paugam, Bruno François Marie Delest
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Publication number: 20150099770Abstract: The present disclosure concerns at least one entity chosen from compounds of Formula (I) and pharmaceutically acceptable salts thereof: (I) wherein the variable groups X, R1, R2, R3 m, n and p are as defined herein. The present disclosure also relates to methods for the preparation of at least one such entity, and intermediates useful in the preparation thereof, to pharmaceutical compositions containing at least one such entity, to the use of at least one such entity in the preparation of medicaments, and to the use of at least one such entity in the treatment of conditions such as, for example, allergic diseases, autoimmune diseases, viral diseases, and cancer.Type: ApplicationFiled: May 17, 2013Publication date: April 9, 2015Inventors: Seiji Hori, Futoshi Hasegawa, Daisuke Urabe, Hirotaka Kurebayashi
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Publication number: 20150094298Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: December 5, 2014Publication date: April 2, 2015Inventors: Shawn M. Bauer, Zhaozhong J. Jia, Mukund Mehrotra, Yonghong Song, Qing Xu, Wolin Huang, Chandrasekar Venkataramani, Jack W. Rose, Anjali Pandey
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Publication number: 20150094296Abstract: The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: March 27, 2013Publication date: April 2, 2015Applicant: Takeda Pharmaceutical Company LimitedInventors: Tetsuya Tsukamoto, Yusuke Ohba, Takafumi Yukawa, Hiroyuki Nagamiya, Taku Kamei, Norihito Tokunaga, Morihisa Saitoh, Atsutoshi Okabe
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Publication number: 20150080368Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: November 24, 2014Publication date: March 19, 2015Applicant: VERASTEM, INC.Inventors: Michael Joseph Luzzio, Kevin Daniel Freeman-Cook, Samit Kumar Bhattacharya, Matthew Merrill Hayward, Catherine Angela Hulford, Christopher Lowell Autry, Xumiao Zhao, Jun Xiao, Kendra Louise Nelson
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Publication number: 20150065533Abstract: The present application relates to novel benzyl-substituted carbamates, 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 preparing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.Type: ApplicationFiled: November 3, 2011Publication date: March 5, 2015Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Jens Ackerstaff, Nils Griebenow, Niels Lindner, Frank Wunder, Volkhart Min-Jian Li
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Patent number: 8962643Abstract: The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.Type: GrantFiled: February 23, 2007Date of Patent: February 24, 2015Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Ankush Argade, Kin Tso, Sambaiah Thota, David Carroll, Arvinder Sran, Robin Cooper, Rajinder Singh, Somasekhar Bhamidipati, Vanessa Taylor, Esteban Masuda
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Patent number: 8962622Abstract: Compounds of formula I modulate jnk and cdk: or a pharmaceutically acceptable salt thereof, where R, R1, R2, R3, and m are defined herein.Type: GrantFiled: September 7, 2007Date of Patent: February 24, 2015Assignee: Roche Palo Alto LLCInventors: David Michael Goldstein, Levi Gong, Christophe Michoud, Wylie Solang Palmer, Achyutharao Sidduri
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Publication number: 20150051201Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3 and A are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.Type: ApplicationFiled: November 3, 2014Publication date: February 19, 2015Applicant: Genentech, Inc.Inventors: Charles Baker-Glenn, Bryan K. Chan, Jennafer Dotson, Anthony Estrada, Timothy Heffron, Joseph Lyssikatos, Zachary Sweeney
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Publication number: 20150051238Abstract: Pyrazole compounds that are modulators of LRRK2, methods of making the compounds, and methods for using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.Type: ApplicationFiled: November 3, 2014Publication date: February 19, 2015Applicant: GENENTECH, INC.Inventors: Charles Baker-Glenn, Daniel Jon Burdick, Bryan K. Chan, Mark Chambers, Huifen Chen, Anthony Estrada, Zachary Kevin Sweeney
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Patent number: 8957068Abstract: The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.Type: GrantFiled: September 26, 2012Date of Patent: February 17, 2015Assignee: Novartis AGInventors: Thomas Raymond Caferro, Young Shin Cho, Abran Q. Costales, Huangshu Lei, Francois Lenoir, Julian Roy Levell, Gang Liu, Mark G. Palermo, Keith Bruce Pfister, Martin Sendzik, Cynthia Shafer, Michael David Shultz, Troy Smith, James Clifford Sutton, Bakary-Barry Toure, Fan Yang, Qian Zhao
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Patent number: 8957081Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.Type: GrantFiled: September 11, 2012Date of Patent: February 17, 2015Assignee: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, III, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
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Publication number: 20150045339Abstract: The object is to provide an Fms-like tyrosine kinase 3 (FLT3) inhibitor useful as a therapeutic agent for acute myeloid leukemia (AML). A novel nitrogen-containing heterocyclic compound represented by the general formula [1] or a salt thereof is provided. The compound or a salt thereof of the present invention can be used as an active ingredient of a pharmaceutical composition for a treatment of a disease or condition relating to FLT3, such as acute myeloid leukemia (AML) and acute promyelocytic leukemia (APL).Type: ApplicationFiled: October 16, 2014Publication date: February 12, 2015Applicant: FUJIFILM CORPORATIONInventors: Masaru TAKASAKI, Toshiaki TSUJINO, Shintarou TANABE, Megumi OOKUBO, Kimihiko SATO, Atsushi HIRAI, Daisuke TERADA, Shinsuke INUKI, Shinsuke MIZUMOTO
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Publication number: 20150038460Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: ApplicationFiled: October 16, 2014Publication date: February 5, 2015Applicant: Genentech, Inc.Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A.G.N. Montalbetti
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Publication number: 20150038481Abstract: Described are compounds of Formula I or Formula II: wherein: ring A is a 5- or 6-membered heteroaryl group; dashed lines are optional double bonds; X is N or O; Y is a carbon atom or an S or N heteroatom in ring A in any suitable location; and substituents are as given herein. Compositions containing the same and methods of using the same in treating cancers such as acute lymphoblastic leukemia are also described.Type: ApplicationFiled: May 21, 2013Publication date: February 5, 2015Inventors: Xiaodong Wang, Weihe Zhang, Dmitri Kireev, Dehui Zhang, Andrew Mclver
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Publication number: 20150025095Abstract: This disclosure relates to: (a) compounds and salts thereof that, inter alia, inhibit RSV infection and/or replication; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: ApplicationFiled: February 15, 2013Publication date: January 22, 2015Inventors: Tatyana Dekhtyar, Arthur Gomtsyan, M-Akhteruzzaman Molla, Anil Vasudevan, Teresa (lok Chan) Ng, Mikhail Shafeev
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Publication number: 20150023930Abstract: Described herein are aminoquinoline and aminoacridine based hybrids, pharmaceutical compositions and medicaments that include such aminoquinoline and aminoacridine based hybrids, and methods of using such compounds for diagnosing and/or treating infections, neurodegerative diseases or disorders, inflammation, inflammation associated diseases and disorders, and/or diseases or disorders that are treatable with dopamine agonists such as the restless leg syndrome.Type: ApplicationFiled: February 28, 2013Publication date: January 22, 2015Applicant: The McLean Hospital CorporationInventors: Diwan S. Rawat, Sunny Manohar, Ummadisetty Chinna Rajesh, Deepak Kumar, Anuj Thakur, Mohit Tripathi, Panyala Linga Reddy, Shamseer Kulangara Kandi, Satyapavan Vardhineni, Kwang-Soo Kim, Chun-Hyung Kim
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Patent number: 8927547Abstract: The invention provides novel pyrimidine derivatives of formula I, to methods of preparing such compounds, to pharmaceutical compositions containing such compounds, and to methods for using such compounds in treatment of diseases including cancer; wherein R1, R2, R3, R4, R5, L, A, D, E, Z, and Y are as defined in the specification.Type: GrantFiled: May 20, 2011Date of Patent: January 6, 2015Assignee: Noviga Research ABInventors: Marita Högberg, Tommy Johansson, Emma Dahlstedt, Olof Smitt
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Publication number: 20150005297Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: September 12, 2014Publication date: January 1, 2015Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
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Publication number: 20150005302Abstract: The present invention directs a compound represented by formula (I).Type: ApplicationFiled: December 21, 2012Publication date: January 1, 2015Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Feryan Ahmed, Joel R. Walker, Raymond Huntley
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Publication number: 20150005281Abstract: The present invention relates to compounds of formula (I) wherein X, R, Y0, T0A, T0B have the meaning as cited in the description and the claims. Said compounds are useful as JAK inhibitors for the treatment or prophylaxis of immunological, inflammatory, autoimmune, allergic disorders, and immunologically-mediated diseases. The invention also relates to pharmaceutical compositions including said compounds and their use as medicaments.Type: ApplicationFiled: December 20, 2012Publication date: January 1, 2015Inventors: Andrew Hobson, Glynn Addison, Nigel Ramsden, John Harrison
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Publication number: 20150005293Abstract: 5-Membered heterocyclic amides and related compounds are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.Type: ApplicationFiled: September 9, 2014Publication date: January 1, 2015Inventors: Hongbin Li, Jun Yuan, Rajagopal Bakthavatchalam, Kevin J. Hodgetts, Qin Guo, Scott M. Capitosti, Jianmin Mao, David J. Wustrow
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Publication number: 20140378488Abstract: Provided are derivatives substituted by urea associated with 4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine-2-amino of formula (I), wherein these compounds may selectively regulate or inhibit an information transmission process controlled by natural or variant tyrosine kinase. Also provided are preparation methods and uses of the compounds.Type: ApplicationFiled: September 5, 2011Publication date: December 25, 2014Applicant: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.Inventors: Yili Ding, Xuan Yang, Qingyan Yan, Hua Bai, Lifeng Cai, Kenneth Smith, Jian Chai
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Patent number: 8916554Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: July 22, 2013Date of Patent: December 23, 2014Assignee: Janssen Pharmaceutica, N.V.Inventors: Patrick René´ Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
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Publication number: 20140363588Abstract: Provided is a polymer film containing at least one of a compound represented by formula (1) of hydrates, solvates, or salts thereof. Y is a methine group or nitrogen atom. Qa, Qb, and Qc are a single bond or a divalent linking group. Ra, Rb, and Rc, are hydrogen atom, alkyl group, alkenyl group, alkynyl group, aryl group, cyano group, halogen group, or heterocyclic group. X2 is a single bond or a divalent linking group. X1 is a single bond or a predetermined divalent linking group.Type: ApplicationFiled: August 27, 2014Publication date: December 11, 2014Applicant: FUJIFILM CorporationInventors: Aiko YAMAMOTO, Satoshi TANAKA, Teruki NIORI, Masato NAGURA, Masaki NORO, Aiko YOSHIDA, Nobutaka FUKAGAWA, Yasukazu KUWAYAMA