- Histone histone deacetylase inhibitor and application thereof
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The invention provides a histone histone deacetylase inhibitor and application thereof. Specifically, the invention provides a compound of formula (I) as shown in the specification, and a pharmaceutically acceptable salt of the compound, and in the formula, the groups are defined as shown in the specification. The invention further provides a preparation method of the compound. The compound of formula (I), which is provided by the invention, can be adopted to treat a series of diseases mediated by histone histone deacetylases by inhibiting histone histone deacetylases (HDACs), particularly type-I histone histone deacetylases (subtypes such as HDAC1 and HDAC3), particularly including tumor diseases such as solid tumor and leukemia, neurodegenerative diseases, and the like.
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Paragraph 0184; 0187
(2018/04/26)
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- Pesticidal compositions and processes related thereto
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This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
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Page/Page column 93
(2016/01/09)
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- PROTOZOAN PARASITE GROWTH INHIBITORS
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Compounds and methods for inhibiting growth of a protozoan parasite. Methods of treating a protozoan parasite infection in a subject by administering a therapeutically effective amount of a compound as disclosed herein. The compounds and methods can be us
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Paragraph 0201
(2015/11/10)
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- Protozoan Parasite Growth Inhibitors Discovered by Cross-Screening Yield Potent Scaffolds for Lead Discovery
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Tropical protozoal infections are a significant cause of morbidity and mortality worldwide; four in particular (human African trypanosomiasis (HAT), Chagas disease, cutaneous leishmaniasis, and malaria) have an estimated combined burden of over 87 million disability-adjusted life years. New drugs are needed for each of these diseases. Building on the previous identification of NEU-617 (1) as a potent and nontoxic inhibitor of proliferation for the HAT pathogen (Trypanosoma brucei), we have now tested this class of analogs against other protozoal species: T. cruzi (Chagas disease), Leishmania major (cutaneous leishmaniasis), and Plasmodium falciparum (malaria). Based on hits identified in this screening campaign, we describe the preparation of several replacements for the quinazoline scaffold and report these inhibitors' biological activities against these parasites. In doing this, we have identified several potent proliferation inhibitors for each pathogen, such as 4-((3-chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)-6-(4-((4-methyl-1,4-diazepan-1-yl)sulfonyl)phenyl)quinoline-3-carbonitrile (NEU-924, 83) for T. cruzi and N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-7-(4-((4-methyl-1,4-diazepan-1-yl)sulfonyl)phenyl)cinnolin-4-amine (NEU-1017, 68) for L. major and P. falciparum.
- Devine, William,Woodring, Jennifer L.,Swaminathan, Uma,Amata, Emanuele,Patel, Gautam,Erath, Jessey,Roncal, Norma E.,Lee, Patricia J.,Leed, Susan E.,Rodriguez, Ana,Mensa-Wilmot, Kojo,Sciotti, Richard J.,Pollastri, Michael P.
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p. 5522 - 5537
(2015/08/03)
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- PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
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This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
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Page/Page column
(2014/06/25)
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- PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
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This document discloses molecules having the following formula ("Formula One"): and processes associated therewith.
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Page/Page column 92
(2014/07/08)
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- PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
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This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
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Paragraph 0439
(2014/06/25)
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- PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
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This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
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Paragraph 0605
(2014/06/25)
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- PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
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This document discloses molecules having the following formula ("Formula One") and processes associated therewith.
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Page/Page column 93
(2014/07/08)
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- PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO
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This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.
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Page/Page column 49
(2013/02/28)
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- PHTHALAZINE DERIVATIVES
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The present invention relates to novel phthalazine derivatives and, more particularly, to phthalazine derivatives that are useful as protein kinase inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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Page/Page column 55
(2008/12/05)
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- PHTHALAZINE, AZA- AND DIAZA-PHTHALAZINE COMPOUNDS AND METHODS OF USE
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The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2/su
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Page/Page column 47
(2008/06/13)
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- Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants
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The present invention provides novel phenylglycinamide derivatives of Formula (I) or (IV): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables W, W1, Y, Z, R7, R8, R9, and R11 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
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Page/Page column 105
(2010/11/25)
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- A thienopyridazinone-based melanin-concentrating hormone receptor 1 antagonist with potent in vivo anorectic properties
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Melanin-concentrating hormone receptor antagonists containing thieno- and a benzopyridazinone cores were designed and tested as potential anorectic agents. These ligands showed high affinity for the receptor, potent functional activity in vitro, and good oral bioavailability in rats. The thiophene analogue exhibited low iv clearance, long half-life, and high brain penetration. In obese rats, the thienopyridazinone demonstrated a dose-dependent reduction in feeding and body weight with doses between 1 and 10 mg kg-1.
- Dyck, Brian,Markison, Stacy,Zhao, Liren,Tamiya, Junko,Grey, Jonathan,Rowbottom, Martin W.,Zhang, Mingzhu,Vickers, Troy,Sorensen, Katie,Norton, Christi,Wen, Jenny,Heise, Christopher E.,Saunders, John,Conlon, Paul,Madan, Ajay,Schwarz, David,Goodfellow, Val S.
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p. 3753 - 3756
(2007/10/03)
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- Phthalazine, aza- and diaza-phthalazine compounds and methods of use
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The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.
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Page/Page column 22; 23
(2008/06/13)
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- 1(2H)-Phthalazinones as cytoprotective agents
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1(2H)-Phthalazinones such as trans-6-[2-(4-methoxy-phenyl)ethenyl]-2-(3-aminopropyl)phthalazin-1(2H)-one hydrobromide, trans-6-[2-(4-methoxyphenyl)ethenyl]-2-[3--(dimethylamino)propyl]phthalazin-1(2H)-one hydrobromide, and trans-6-[2-(4-hydroxphenyl)ethenyl]-2-[3-(dimethyl-amino)propyl]phthalazin-1(2H)-one hydrochloride are useful as cytoprotective agents in mammals.
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- Anti-allergy 1(2H)-phthalazinones
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Novel 1 2(H)-phthalazones are disclosed along with a method of treating either allergic rihinitis or bronchial asthma by the administration to a mammal an effective amount of a compound of the formula: STR1 wherein R1 is hydrogen, hydroxyl, C1 -C4 alkoxy, or C1 -C4 alkylthio, R2 is STR2 or 1-pyrrolidinyl, R3 and R4 are independently hydrogen or C1 -C4 alkyl, X is CH2, O or NR5, Y is ethylene or ethenylene, R5 is hydrogen or C1 -C4 alkyl, n is 2, 3 or 4, and all stereoisomeric forms and pharmaceutical acceptable addition salts thereof.
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