C07C255/17

COMPOSITIONS AND METHODS RELATED TO MOLECULAR CONJUGATION

The invention relates to activated Michael acceptor (AMA) compounds that can undergo conjugation with biomolecules containing Michael donor moieties, thereby providing plasma-stable antibody-drug conjugates (ADCs). Pharmaceutical compositions of the ADCs are disclosed as well. Also provided herein are a number of applications (e.g., therapeutic applications) in which the compositions are useful.

Fluorine-containing ether compound, lubricant for magnetic recording medium, and magnetic recording medium

Provided is a fluorine-containing ether compound that can be suitably used as a material for a lubricant for a magnetic recording medium, capable of forming a lubricant layer having excellent chemical substance resistance and wear resistance even when the thickness is small. A fluorine-containing ether compound represented by the following formula (1):
R.sup.1—R.sup.2—CH.sub.2—R.sup.3—CH.sub.2—R.sup.4—R.sup.5  (1) In the formula (1), R.sup.3 is a perfluoropolyether chain. R.sup.2 and R.sup.4 are divalent linkage groups having a polar group, and may be the same or different. R.sup.1 and R.sup.5 are terminal groups bonded to R.sup.2 or R.sup.4, which may be the same or different, and at least one of R.sup.1 and R.sup.5 is an organic group having 1 to 8 carbon atoms wherein one or more hydrogen atoms of the organic group is substituted with a cyano group.

Fluorine-containing ether compound, lubricant for magnetic recording medium, and magnetic recording medium

Provided is a fluorine-containing ether compound that can be suitably used as a material for a lubricant for a magnetic recording medium, capable of forming a lubricant layer having excellent chemical substance resistance and wear resistance even when the thickness is small. A fluorine-containing ether compound represented by the following formula (1):
R.sup.1—R.sup.2—CH.sub.2—R.sup.3—CH.sub.2—R.sup.4—R.sup.5  (1) In the formula (1), R.sup.3 is a perfluoropolyether chain. R.sup.2 and R.sup.4 are divalent linkage groups having a polar group, and may be the same or different. R.sup.1 and R.sup.5 are terminal groups bonded to R.sup.2 or R.sup.4, which may be the same or different, and at least one of R.sup.1 and R.sup.5 is an organic group having 1 to 8 carbon atoms wherein one or more hydrogen atoms of the organic group is substituted with a cyano group.

Kinase inhibitors

There are provided compounds of formula I, ##STR00001##
wherein R.sup.1 to R.sup.5, X.sup.1, X.sup.2, Ar, L, E, A, A.sup.1, G and G.sup.1 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

Kinase inhibitors

There are provided compounds of formula I, ##STR00001##
wherein R.sup.1 to R.sup.5, X.sup.1, X.sup.2, Ar, L, E, A, A.sup.1, G and G.sup.1 have meanings given in the description, which compounds have antiinflammatory activity (e.g. through inhibition of one or more of members of: the family of p38 mitogen-activated protein kinase enzymes; Syk kinase; and members of the Src family of tyrosine kinases) and have use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, eye and intestines.

Pinene-derived diisocyanates

A pinene-derived diisocyanate compound, a process for forming a pinene-derived polyurethane, and an article of manufacture that includes the polyurethane are disclosed. The process for forming the polyurethane includes forming a pinene-derived diisocyanate compound, and reacting the pinene-derived diisocyanate compound with a polyol in a polymerization compound.

Pinene-derived diisocyanates

A pinene-derived diisocyanate compound, a process for forming a pinene-derived polyurethane, and an article of manufacture that includes the polyurethane are disclosed. The process for forming the polyurethane includes forming a pinene-derived diisocyanate compound, and reacting the pinene-derived diisocyanate compound with a polyol in a polymerization compound.

Efficient process for the preparation of sitagliptin

Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine. ##STR00001##

Efficient process for the preparation of sitagliptin

Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine. ##STR00001##

ARYL AND PYRIDYL AMIDE PESTICIDES AND COMPOSITIONS THEREOF

The subject matter described herein is directed to compounds, synergistic compositions, and methods for repelling arthropods, such as insects. The compositions comprise aryl and pyridyl-type compounds. The compounds demonstrate strong vapor and topical repellency when applied alone and in synergistic compositions.