Patent classifications
C07C247/16
INHIBITORS OF LYSINE GINGIPAIN
The present invention relates generally to therapeutics targeting the bacterium Porphyromonas gingivalis, including its protease Lysine gingipain (Kgp), and their use for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease. In certain embodiments, the invention provides compounds according to Formula I, as described herein, and pharmaceutically acceptable salts thereof.
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COMPOUND OR SALT THEREOF, AND ANTIBODY OBTAINED BY USING THE SAME
A desired antibody or antibody composition may be obtained by modifying a thiol group chemically introduced to an antibody to obtain an antibody composition comprising (A) an antibody intermediate or a salt thereof having a bioorthogonal functional group which may be protected, which is represented by the following formula (A):
AbS-L-R].sub.n(A) wherein Ab is a certain antibody, S is a sulfur atom, L is a divalent group, R is a bioorthogonal functional group which may be protected, and n is an integer from 1 to 8, and (B) a thiol group-introduced antibody or a salt thereof, which is represented by the following formula (B):
AbSH].sub.n(B) wherein Ab and n are the same as formulae (A), and SH is a thiol group; and the like.
COMPOUND OR SALT THEREOF, AND ANTIBODY OBTAINED BY USING THE SAME
A desired antibody or antibody composition may be obtained by modifying a thiol group chemically introduced to an antibody to obtain an antibody composition comprising (A) an antibody intermediate or a salt thereof having a bioorthogonal functional group which may be protected, which is represented by the following formula (A):
AbS-L-R].sub.n(A) wherein Ab is a certain antibody, S is a sulfur atom, L is a divalent group, R is a bioorthogonal functional group which may be protected, and n is an integer from 1 to 8, and (B) a thiol group-introduced antibody or a salt thereof, which is represented by the following formula (B):
AbSH].sub.n(B) wherein Ab and n are the same as formulae (A), and SH is a thiol group; and the like.
Method for synthesizing iodo- or astatoarenes using diaryliodonium salts
The present invention concerns a method of synthesizing a iodo- or astatoarene comprising the reaction of a diaryliodonium compound with a iodide or astatide salt, respectively. The invention also relates to said iodo- or astatoarene and diaryliodonium compound as such. The invention also concerns a method of synthesizing a iodo- or astatolabelled biomolecule and/or vector using said iodo- or astatoarene.
Method for synthesizing iodo- or astatoarenes using diaryliodonium salts
The present invention concerns a method of synthesizing a iodo- or astatoarene comprising the reaction of a diaryliodonium compound with a iodide or astatide salt, respectively. The invention also relates to said iodo- or astatoarene and diaryliodonium compound as such. The invention also concerns a method of synthesizing a iodo- or astatolabelled biomolecule and/or vector using said iodo- or astatoarene.
AN IMPROVED PROCESS FOR THE PREPARATION OF TRIFLOXYSTROBIN
The present invention relates to an improved process for the preparation of trifloxystrobin of formula (I), which is simple, economical, efficient, user and environment friendly, moreover commercially viable with higher yield and chemical purity.
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Ketone inhibitors of lysine gingipain
The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
Ketone inhibitors of lysine gingipain
The present invention provides compounds according to Formula I as described herein, and their use for inhibiting the lysine gingipain protease (Kgp) from the bacterium Porphyromonas gingivalis. Also described are gingipain activity probe compounds and methods for assaying gingipain activity are also described, as well as methods for the treatment of disorders associated with P. gingivalis infection, including brain disorders such as Alzheimer's disease.
METHOD FOR SYNTHESIZING IODO- OR ASTATOARENES USING DIARYLIODONIUM SALTS
The present invention concerns a method of synthesizing a iodo- or astatoarene comprising the reaction of a diaryliodonium compound with a iodide or astatide salt, respectively. The invention also relates to said iodo- or astatoarene and diaryliodonium compound as such. The invention also concerns a method of synthesizing a iodo- or astatolabelled biomolecule and/or vector using said iodo- or astatoarene.
METHOD FOR SYNTHESIZING IODO- OR ASTATOARENES USING DIARYLIODONIUM SALTS
The present invention concerns a method of synthesizing a iodo- or astatoarene comprising the reaction of a diaryliodonium compound with a iodide or astatide salt, respectively. The invention also relates to said iodo- or astatoarene and diaryliodonium compound as such. The invention also concerns a method of synthesizing a iodo- or astatolabelled biomolecule and/or vector using said iodo- or astatoarene.