The present invention relates to a process for labeling compounds comprising thiol moieties with 3-arylpropiolonitrile compounds, to 3-arylpropiolonitrile compounds substituted with tag moieties and to specific 3-arylpropiolonitrile linkers.

The present invention relates to a process for labeling compounds comprising thiol moieties with 3-arylpropiolonitrile compounds, to 3-arylpropiolonitrile compounds substituted with tag moieties and to specific 3-arylpropiolonitrile linkers.

The present invention aims to provided a novel production method of an enzalutamide crystal form in which wet crystals of enzalutamide are obtained in a step of crystallizing in the production process of the enzalutamide crystal form, and then 2-propanol which is solvated with enzalutamide and the B-type crystals are reduced. The present invention relates to a production method of an enzalutamide crystal form, which comprises a step of crystallizing for obtaining wet crystals of enzalutamide, and a step of drying the wet crystals, and comprises a step of washing using a mixed solvent of a good solvent and a poor solvent after the step of crystallizing.

The present invention aims to provided a novel production method of an enzalutamide crystal form in which wet crystals of enzalutamide are obtained in a step of crystallizing in the production process of the enzalutamide crystal form, and then 2-propanol which is solvated with enzalutamide and the B-type crystals are reduced. The present invention relates to a production method of an enzalutamide crystal form, which comprises a step of crystallizing for obtaining wet crystals of enzalutamide, and a step of drying the wet crystals, and comprises a step of washing using a mixed solvent of a good solvent and a poor solvent after the step of crystallizing.

Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof,

##STR00001##

wherein R.sup.1 is F, Cl or Br; R.sup.2 is H or F; and R.sup.3 is Cl or Br; and
(b) at least one fungicidal compound selected from (b1) through (b13) as disclosed herein. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an N-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed are process intermediate compounds useful for preparing compounds of Formula 1.

Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof,

##STR00001##

wherein R.sup.1 is F, Cl or Br; R.sup.2 is H or F; and R.sup.3 is Cl or Br; and
(b) at least one fungicidal compound selected from (b1) through (b13) as disclosed herein. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an N-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed are process intermediate compounds useful for preparing compounds of Formula 1.

New chelators such as H.sub.3L1, H.sub.3L2, H.sub.3L3, H.sub.3L26 and derivatives were synthesized for the complexation of {Al.sup.18F}.sup.2+. These new chelators are able to complex {AI.sup.18F}.sup.2+ with good radiochemical yields using a labeling temperature of 37 C. The stability of the new Al.sup.18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum. AI.sup.18F-L3 and AI.sup.18F-L26 showed a stability comparable to that of the previously reported Al.sup.18F-NODA. Moreover, the biodistribution of Al.sup.18F-L3 and Al.sup.18F-L26 showed absence of in vivo demetallation since only very limited bone uptake was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestine due to hepatobiliary clearance of the radiolabeled ligand. The chelators H.sub.3L3 and Al.sup.18F-L26 demonstrated to be a good lead candidates for the labeling of heat sensitive biomolecules with .sup.18F-fluorine and derivatives have been synthesized. We have explored the complexation of {AI.sup.18F}.sup.2+ with new chelators and obtained very favourable radiochemical yields (>85%) using a labeling temperature of 37 C. The stability of the new Al.sup.18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum at 37 C., where AI.sup.18F-L3 and AI.sup.18F-L26 showed a stability comparable to that of the previously reported Al.sup.18F-NODA. Moreover, the biodistribution of Al.sup.18F-L3 and Al.sup.18F-L26 showed high stability, since only very limited bone uptakewhich would be an indication of release of fluorine-18 in the form of fluoridewas observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestines due to hepatobiliary clearance of the radiolabeled ligand. The chelators H.sub.3L3 and H.sub.3L26 demonstrated to be good lead candidates for the labeling of heat sensitive biomolecules with .sup.18F-fluorine and several derivatives have been synthesized.

New chelators such as H.sub.3L1, H.sub.3L2, H.sub.3L3, H.sub.3L26 and derivatives were synthesized for the complexation of {Al.sup.18F}.sup.2+. These new chelators are able to complex {AI.sup.18F}.sup.2+ with good radiochemical yields using a labeling temperature of 37 C. The stability of the new Al.sup.18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum. AI.sup.18F-L3 and AI.sup.18F-L26 showed a stability comparable to that of the previously reported Al.sup.18F-NODA. Moreover, the biodistribution of Al.sup.18F-L3 and Al.sup.18F-L26 showed absence of in vivo demetallation since only very limited bone uptake was observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestine due to hepatobiliary clearance of the radiolabeled ligand. The chelators H.sub.3L3 and Al.sup.18F-L26 demonstrated to be a good lead candidates for the labeling of heat sensitive biomolecules with .sup.18F-fluorine and derivatives have been synthesized. We have explored the complexation of {AI.sup.18F}.sup.2+ with new chelators and obtained very favourable radiochemical yields (>85%) using a labeling temperature of 37 C. The stability of the new Al.sup.18F-complexes was tested in phosphate buffered saline (PBS) at pH 7 and in rat serum at 37 C., where AI.sup.18F-L3 and AI.sup.18F-L26 showed a stability comparable to that of the previously reported Al.sup.18F-NODA. Moreover, the biodistribution of Al.sup.18F-L3 and Al.sup.18F-L26 showed high stability, since only very limited bone uptakewhich would be an indication of release of fluorine-18 in the form of fluoridewas observed, whereas the major fraction of activity 60 min p.i. was observed in liver and intestines due to hepatobiliary clearance of the radiolabeled ligand. The chelators H.sub.3L3 and H.sub.3L26 demonstrated to be good lead candidates for the labeling of heat sensitive biomolecules with .sup.18F-fluorine and several derivatives have been synthesized.

Disclosed are small molecule inhibitors of deubiquitinating enzymes (DUBs), and methods of using them. Certain compounds are selective for particular ubiquitin-specific proteases (USPs).

Disclosed are small molecule inhibitors of deubiquitinating enzymes (DUBs), and methods of using them. Certain compounds are selective for particular ubiquitin-specific proteases (USPs).