C07D207/40

Prodrugs of fumarates and their use in treating various diseases

The present invention provides compounds of formula (I), ##STR00001##
wherein: R.sub.1 is unsubstituted C.sub.1-C.sub.6 alkyl; L.sub.a is substituted or unsubstituted C.sub.1-C.sub.6 alkyl linker, substituted or unsubstituted C.sub.3-C.sub.10 carbocycle, substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S, or substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S; and R.sub.2 and R.sub.3 are each, independently, H, substituted or unsubstituted C.sub.1-C.sub.6 alkyl, or substituted or unsubstituted C.sub.6-C.sub.10 aryl; or alternatively, R.sub.2 and R.sub.3, together with the nitrogen atom to which they are attached, form a substituted or unsubstituted heteroaryl comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S or a substituted or unsubstituted heterocycle comprising one or two 5- or 6-member rings and 1-4 heteroatoms selected from N, O and S. The invention also provides pharmaceutical compositions and methods for treating neurological diseases, such as multiple sclerosis.

NITRATION
20220009875 · 2022-01-13 · ·

A process for preparing a nitrated compound, including the step of reacting a compound (A) including at least one substituted or unsubstituted aromatic or heteroaromatic ring, wherein the heteroaromatic ring includes at least one heteroatom selected from the group consisting of oxygen, sulfur, phosphor, selenium and nitrogen, with a compound of formula (I)

##STR00001##

wherein Y is selected from the group consisting of hydrogen and nitro.

Method for identifying drug-discovery target protein for development of antibody drug, and method for producing antibody against target protein

Finding a protein of a minute amount present on a cell membrane to provide a method for producing an antibody against the protein. Producing an antibody using a protein identified by an identification method including: a labeling step of using a labeling agent comprising at least one selected from bis-iminobiotin compounds and bis-biotin compounds to obtain cells having a labeled protein; a degradation step of preparing a degradation product for an immobilization treatment, the degradation product containing the labeled protein; an immobilization step of immobilizing the labeled protein contained in the degradation product for an immobilization treatment on a stationary phase via a streptavidin mutant; a cleavage step of releasing an analysis sample from the stationary phase on which the labeled protein is immobilized; and an analysis step of analyzing the analysis sample to identify the labeled protein.

Compositions for the treatment of pulmonary fibrosis
11401245 · 2022-08-02 · ·

The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.

Compositions for the treatment of pulmonary fibrosis
11401245 · 2022-08-02 · ·

The present invention relates to compounds and their use in the prophylactic and/or therapeutic treatment of pulmonary fibrosis and/or related conditions.

PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.

##STR00001##

PRODRUGS OF FUMARATES AND THEIR USE IN TREATING VARIOUS DISEASES

The present invention provides compounds of formula (I), and pharmaceutical compositions thereof.

##STR00001##

(2,5-DIOXOPYRROLIDIN-1-YL)(PHENYL)-ACETAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISEASES

The first object of the invention is the compound of general formula (I) or pharmaceutically acceptable salts thereof. A second object of the invention is the use of compounds described by general formula (I) as active ingredient in pharmaceutical compositions for the treatment of epileptic seizures or neuropathic pain or migraine.

##STR00001##

(2,5-DIOXOPYRROLIDIN-1-YL)(PHENYL)-ACETAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF NEUROLOGICAL DISEASES

The first object of the invention is the compound of general formula (I) or pharmaceutically acceptable salts thereof. A second object of the invention is the use of compounds described by general formula (I) as active ingredient in pharmaceutical compositions for the treatment of epileptic seizures or neuropathic pain or migraine.

##STR00001##

Conjugates of cell binding molecules with cytotoxic agents

A conjugate of a potent cytotoxic agent with a cell-surface receptor binding molecule having a Formula (I), wherein T, L, m, n, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.1, R.sup.12, and R.sup.13 are defined herein, can be used for targeted treatment of cancer, autoimmune disease, and infectious disease.