Disclosed are general and “substantially pure” branched discrete polyethylene glycol constructs useful in attaching to a variety of biologically active groups, for example, preferential locators, as well as biologics like enzymes, for use in diagnostics, e.g. imaging, therapeutics, theranostics, and moieties specific for other applications. In its simplest intermediate state, a branched discrete polyethylene glycol construct is terminated at one end by a chemically reactive moiety, “A”, a group that is reactive with a biologic material that creates “A”, which is a biologically reactive group, connected through to a branched core (BC) which has attached at least two dPEG-containing chains, indicated by the solid line, , having terminal groups, which can be charged, non-reactive or reactable moieties and containing between about 2 and 64 dPEG residues.

This invention describes processes for the convergent synthesis of calicheamicin derivatives, and similar analogs using bifunctional and trifunctional linker intermediates.

This invention describes processes for the convergent synthesis of calicheamicin derivatives, and similar analogs using bifunctional and trifunctional linker intermediates.

The present invention provides a diarylamine-based compound represented by General Formula (1): ##STR00001##
(where A.sup.1 and A.sup.2 each independently represent a C.sub.6 to C.sub.18 arylene group which may have a substituent, and A.sup.3 and A.sup.4 each independently represent an organic group having a cyclic imide structure which may have a substituent).

A crystal form A of 2-(2, 5-dioxopyrrolidin-1yl)ethyl methyl fumarate has a good light irradiation stability, high-temperature stability and high-humidity stability.

A crystal form A of 2-(2, 5-dioxopyrrolidin-1yl)ethyl methyl fumarate has a good light irradiation stability, high-temperature stability and high-humidity stability.

The invention relates to compounds of formula (IW-1) and to their use in treating or preventing an inflammatory disease or a disease associated with an undesirable immune response: wherein R.sup.A, R.sup.B, R.sup.C and R.sup.D are as defined herein.

##STR00001##

A method for producing a nitrogen-containing fluorine-containing compound includes a step in which a compound represented by formula (5) is fluorinated to obtain a compound represented by formula (6). R.sup.3 is a single bond or a C1-20 divalent organic group. R.sup.4 and R.sup.5 are each independently a monovalent organic group having an electron-withdrawing group, a C1-20 monovalent hydrocarbon group, or a C2-20 monovalent hydrocarbon group which contains an etheric oxygen atom between carbon atoms. At least one of R.sup.4 and R.sup.5 is a monovalent organic group having an electron-withdrawing group. R.sup.3, R.sup.4, and R.sup.5 may be bonded to each other to form a divalent organic group or a trivalent organic group. R.sup.6 is a C1-20 monovalent organic group. E.sup.3 is a divalent organic group. R.sup.3F, R.sup.4F, R.sup.5F, R.sup.6F, and E.sup.3F are groups formed by fluorinating some or all of hydrogen atoms of R.sup.3, R.sup.4, R.sup.5, R.sup.6, and E.sup.3.

##STR00001##

2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2-oxopyrrolidin-1-yl)propanamide derivatives with R-configuration at the stereogenic center are disclosed, showing broad-spectrum protective activity in animal models of epileptic seizures, pain, depression and anxiety that are simultaneously devoid of undesirable sedative effects. Additionally, the disclosed derivatives have neuroprotective effects in the in vitro and in vivo studies.

##STR00001##

2-(2,5-dioxopyrrolidin-1-yl)propanamide and 2-(2-oxopyrrolidin-1-yl)propanamide derivatives with R-configuration at the stereogenic center are disclosed, showing broad-spectrum protective activity in animal models of epileptic seizures, pain, depression and anxiety that are simultaneously devoid of undesirable sedative effects. Additionally, the disclosed derivatives have neuroprotective effects in the in vitro and in vivo studies.

##STR00001##