Provided are an FGFR4 inhibitor having the structure of formula (I), and a preparation method therefor and the use thereof. The compound has a very strong inhibitory effect on FGFR4 kinase activity and has a very high selectivity, and can be widely used in the preparation of a drug for treating cancers, especially prostate cancer, liver cancer, pancreatic cancer, esophageal carcinomas, gastric cancer, lung cancer, breast cancer, ovarian carcinomas, colon cancer, skin cancer, glioblastomas or rhabdomyosarcomas, and is expected to be developed into a new generation of FGFR4 inhibitor drugs. ##STR00001##

Provided are an FGFR4 inhibitor having the structure of formula (I), and a preparation method therefor and the use thereof. The compound has a very strong inhibitory effect on FGFR4 kinase activity and has a very high selectivity, and can be widely used in the preparation of a drug for treating cancers, especially prostate cancer, liver cancer, pancreatic cancer, esophageal carcinomas, gastric cancer, lung cancer, breast cancer, ovarian carcinomas, colon cancer, skin cancer, glioblastomas or rhabdomyosarcomas, and is expected to be developed into a new generation of FGFR4 inhibitor drugs. ##STR00001##

The present invention relates to a composition capable of preventing or inhibiting axonal degeneration and effectively preventing, improving, or treating various neurological diseases caused by the axonal degeneration.

A compound having a structure of formula (I): ##STR00001##
Wherein each of R.sub.1A, R.sub.1B, R.sub.1C, R.sub.1D, R.sub.1E and R.sub.1F is independently selected from the group consisting of a hydrogen atom, a hydroxide group, and a substituted or unsubstituted C.sub.1-C.sub.8 alkoxy group, R.sub.2 is selected from the group consisting of a hydrogen atom and a hydroxide group, R.sub.3 is hydrogen atom, R.sub.4 is selected from the group consisting of a hydrogen atom, a C.sub.1-C.sub.3 alkyl group, and a C.sub.1-C.sub.3 fluoroalkyl group, R.sub.5 is selected from the group consisting of a hydrogen atom, a C.sub.1-C.sub.6 alkyl, and a C.sub.1-C.sub.6 fluoroalkyl, n is 1 or 2, and X is a negatively charged anion. Removal of the substituted nitroimidazole affords a phenanthroindolizidine or phenanthroquinolizidine alkaloid derivative. The compound is used in a pharmaceutical composition and a method of treating a proliferative disease.

Described herein are kits, compositions, and combination therapies comprising sulindac for use in the treatment of fragile X syndrome (FXS).

Described herein are kits, compositions, and combination therapies comprising sulindac for use in the treatment of fragile X syndrome (FXS).

The invention relates to modulators of Embryonic Ectoderm Development (EED) and/or Polycomb Repressive Complex 2 (PRC2) useful in the treatment of disorders and diseases associated with EEC and PRC2, being macrocyclic azolopyridine derivatives and compositions thereof of Formula I: ##STR00001##
or a pharmaceutically acceptable salt, prodrug, solvate, hydrate, enantiomer, isomer, or tautomer thereof, wherein X.sub.1, X.sub.2, X.sub.3, A.sub.1, A.sub.2, Y, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as described herein.

The invention relates to modulators of Embryonic Ectoderm Development (EED) and/or Polycomb Repressive Complex 2 (PRC2) useful in the treatment of disorders and diseases associated with EEC and PRC2, being macrocyclic azolopyridine derivatives and compositions thereof of Formula I: ##STR00001##
or a pharmaceutically acceptable salt, prodrug, solvate, hydrate, enantiomer, isomer, or tautomer thereof, wherein X.sub.1, X.sub.2, X.sub.3, A.sub.1, A.sub.2, Y, R.sub.1, R.sub.2, R.sub.3, and R.sub.4 are as described herein.

The invention provides a p38 MAPK inhibitor of Formula I, or a pharmaceutically acceptable salt or solvate thereof: Formula I for use in the treatment or prevention of hypercytokinemia in a human patient; wherein R is C.sub.1-3alkyl, optionally substituted by one or more halo, NR.sup.1R.sup.2 or hydroxy, and R.sup.1 and R.sup.2 are independently H, halo or C.sub.1-3alkyl, optionally substituted by one or more F. Also provided are compositions for use in the treatment or prevention of hypercytokinemia comprising the p38 MAPK inhibitor of Formula I; and methods for treating or preventing hypercytokinemia in a human patient in need thereof comprising administering to the patient a therapeutically or prophylactically effective amount of a p38 MAPK inhibitor of Formula I. The invention also provides a p38 MAPK inhibitor and an antimicrobial agent, such as an antiviral agent, for use in the treatment or prevention of hypercytokinemia. ##STR00001##

The invention provides a p38 MAPK inhibitor of Formula I, or a pharmaceutically acceptable salt or solvate thereof: Formula I for use in the treatment or prevention of hypercytokinemia in a human patient; wherein R is C.sub.1-3alkyl, optionally substituted by one or more halo, NR.sup.1R.sup.2 or hydroxy, and R.sup.1 and R.sup.2 are independently H, halo or C.sub.1-3alkyl, optionally substituted by one or more F. Also provided are compositions for use in the treatment or prevention of hypercytokinemia comprising the p38 MAPK inhibitor of Formula I; and methods for treating or preventing hypercytokinemia in a human patient in need thereof comprising administering to the patient a therapeutically or prophylactically effective amount of a p38 MAPK inhibitor of Formula I. The invention also provides a p38 MAPK inhibitor and an antimicrobial agent, such as an antiviral agent, for use in the treatment or prevention of hypercytokinemia. ##STR00001##