A new application about 2,2-Dimethylsuccinicanhydride

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Heterocyclically Substituted Anilinopyrimides

Heterocyclically substituted anilinopyrimidines of the formula (I) in which R1 to R10 and L1, L2, E1, E2, E3, Y and Z have the meanings given in the description, and agrochemically active salts thereof, their use and also methods and compositions for controlling phytopathogenic harmful fungi in and/or on plants or in and/or on seed of plants, processes for preparing such compositions and treated seed and also their use for controlling phytopathogenic harmful fungi in agriculture, horticulture and forestry, in the protection of materials and in the domestic and hygiene field. The present invention furthermore relates to a process for preparing heterocyclically substituted anilinopyrimidinenes of the formula (I).

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Tetrahydrofuran – Wikipedia,
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Synthesis and VEGF inhibitory activity of 16,17-pyrazo-annulated steroids

Eight 16,17-pyrazo-annulated steroidal derivatives were synthesized and evaluated in vitro vascular endothelial growth factor (VEGF) inhibitory activity with 2-methoxyestradiol (2-ME) as the reference compound. Most of the compounds showed potent VEGF inhibitory activity with EC50 values of micromolar or submicromolar range. Among them, the compounds 3 and 8 exhibited similar EC50 values and obviously better TI values compared with 2-ME.

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Conjugates of 3alpha-methoxyserrat-14-en-21beta-ol (PJ-1) and 3beta-methoxyserrat-14-en-21beta-ol (PJ-2) as cancer chemopreventive agents

3alpha-Methoxyserrat-14-en-21beta-ol (PJ-1) and 3beta-methoxyserrat- 14-en-21beta-ol (PJ-2) were conjugated with well-known phenolic compounds, narigenin, hesperetin, genistein, and daidzein (1-8). Other conjugates of PJ-2-3,5-dihydroxy-4-methoxybenzoic acid (9), PJ-2-pyrogallol (10), and derivatives of PJ-1, PJ-2-3,3-dimethyl-succinates (11, 12), PJ-1, PJ-2-succinates (13, 14), PJ-2-glycine (15), PJ-2-piperidine acetic acid (16), and PJ-1 epoxy-3,3-dimethyl-succinate (17) were tested for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol-13-acetate (TPA). The inhibitory effects of 11 (IC50 = 251), 12 (IC50 = 248), and 17 (IC50 = 230 mol ratio/32 pmol/TPA), were 2-fold stronger than those of the other compounds such as oleanolic acid (IC50 = 449). Compounds 10, 11, and 17 inhibited mouse skin tumor promotion in an in vivo two-stage carcinogenesis model. The in vivo two-stage mouse-skin carcinogenesis test employed 7,12-dimethylbenz[a]anthracene (DMBA) as an initiator and TPA as a promoter.

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Helix 12 directed non-steroidal antiandrogens

Compounds having the structure (or their salts):

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Click chemistry-assisted synthesis of novel C-2 triazole-linked betulinic acid conjugates with azidothymidine as potential anti-HIV agents

A new synthetic approach to C-2 triazole-linked bioconjugates of lupane triterpenoids with 3?-azido-3?- deoxythymidine (AZT) based on CuI-catalyzed 1,3-cycloaddition between alkynes and azides is described. The proposed strategy towards AZT-betulinic acid hybrid molecules as potential anti-HIV agents makes it possible to vary the C-3 and C-28 pharmacophores in triterpene moieties. The C-2 propargyl-substituted betulinic acid and its mono- or bi-functional derivatives with side chain at C-3 and/or C-28 positions were successfully synthesized by employing the click reaction.

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Tetrahydrofuran – Wikipedia,
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AMIDE COMPOUND

The present invention relates to compound (I) or a salt thereof which has a RORgammat inhibitory action. In the formula (I), each symbol is as defined in the specification.

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Tetrahydrofuran – Wikipedia,
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MODULATORS OF G-PROTEIN COUPLED RECEPTORS

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt and/or hydrate and/or prodrug of the compound) that modulate (e.g., agonize or partially agonize or antagonize) glucagon?like peptide?1 receptor (“GLP?1R”) and/or the gastric inhibitory polypeptide receptor (“GIPR”). The chemical entities are useful, e.g., for treating a subject (e.g., a human) having a disease, disorder, or condition in which modulation (e.g., agonism, partial agonism or antagonism) of GLP?1R and/or GIPR activities is benficial for the treatment or prevention of the underlying pathology and/or symptoms and/or progression of the disease, disorder, or condition. In some embodiments, the modulation results in an enhancment of (e.g., an increase in) existing levels (e.g., normal or below normal levels) of GLP?1R and/or GIPR activity (e.g., signaling). In some embodiments, the chemical entities described herein further modulate (e.g., attenuate, uncouple) -arrestin signaling relative to what is observed with the native ligand. This disclosure also features compositions as well as other methods of using and making the said chemical entities.

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Meta-anilide and meta-anilide urea herbicidal compounds and methods of use

A compound having the structural formula STR1 wherein R is selected from the group consisting of C1 -C5 alkyl, preferably methyl; C1 -C3 haloalkyl, preferably C2 -haloalkyl and most preferably trifluoromethyl; aryl, preferably phenyl, C2 -C8 alkoxyalkyl, preferably ethoxyethyl and ethoxyethoxyethyl; R’ is selected from the group consisting of C2 -C8 alkyl, preferably C2 -C3 alkyl; C1 -C3 alkoxy, preferably methoxy; cyclopropyl; methacryl; C1 -C3 alkylmercapto, preferably methylmercapto; methylamino; ethylamino; C2 -C4 dialkylamino, preferably dimethylamino; C2 -C4 alkylalkoxyamino, preferably methylmethoxyamino; and n equals the integer 0 or 1.

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Tetrahydrofuran – Wikipedia,
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PROPENOATE DERIVATIVES OF BETULIN

The present invention relates to a compound characterized by Formula (I); or a pharmaceutically acceptable salt thereof, wherein X, Y, and Z are as described herein. Compounds of the present invention are useful for the treatment of HIV.

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Tetrahydrofuran – Wikipedia,
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Enhanced selectivity profile of pyrazole-urea based DFG-out p38alpha inhibitors

By targeting an extended region of the conventional ‘DFG-out’ pocket of p38alpha, while minimizing interactions with the specificity pocket and eliminating interactions with the adenine binding site, we are able to design and synthesize a number of pyrazole-urea based DFG-out p38alpha inhibitors with good potencies, and excellent selectivity.

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Tetrahydrofuran – Wikipedia,
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