A61K31/551

CROSSLINKED OPTICALLY ACTIVE SECONDARY AMINE DERIVATIVE

The present invention relates to the compound of formula (1a) wherein p is 1 or 2, R.sup.1-R.sup.4 are hydrogen atom or the like, Ring A is cycloalkylene or the like, L is single bond or the like, and R is methyl or the like, or a pharmaceutically acceptable salt thereof, which has an anticancer effect by inhibiting the binding between a MLL fusion protein that is fused with AF4, AF9, or the like, which is a representative fusion partner gene causing MLL leukemia, and menin.

##STR00001##

BET DEGRADER

The present invention provides a BET (protein) degrader, specifically a BET degrader containing a compound represented by formula (I) or a pharmaceutically acceptable salt thereof:

##STR00001##

wherein L1 and L2 are the same or different and each represents a small molecular ligand for BET protein, and S represents a group represented by a formula selected from the group consisting of formulas (S1) to (S18).

Anti-tumor effect potentiator using novel biphenyl compound
11510915 · 2022-11-29 · ·

An antitumor formulation comprising a biphenyl compound having LSD1 inhibitory activity or a salt thereof and one or more other antitumor agents that are administered in combination, the compound being represented by Formula (I): ##STR00001##
wherein ring A, ring B, R1 to R6, l, m, and n are as defined in the specification.

Anti-tumor effect potentiator using novel biphenyl compound
11510915 · 2022-11-29 · ·

An antitumor formulation comprising a biphenyl compound having LSD1 inhibitory activity or a salt thereof and one or more other antitumor agents that are administered in combination, the compound being represented by Formula (I): ##STR00001##
wherein ring A, ring B, R1 to R6, l, m, and n are as defined in the specification.

VENETOCLAX DOSING REGIMENS FOR USE IN TREATING MYELODYSPLASTIC SYNDROMES IN COMBINATION WITH A CYP3A INHIBITOR AND AZACITIDINE
20220370481 · 2022-11-24 · ·

The invention described herein relates to therapeutic dosing regimens comprising administering venetoclax in combination with azacitidine and a CYP3A inhibitor for treating myelodysplastic syndromes (MDS).

VENETOCLAX DOSING REGIMENS FOR USE IN TREATING MYELODYSPLASTIC SYNDROMES IN COMBINATION WITH A CYP3A INHIBITOR AND AZACITIDINE
20220370481 · 2022-11-24 · ·

The invention described herein relates to therapeutic dosing regimens comprising administering venetoclax in combination with azacitidine and a CYP3A inhibitor for treating myelodysplastic syndromes (MDS).

Bicyclic and tricyclic compounds

Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.

Bicyclic and tricyclic compounds

Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof.

PROPHYLACTIC OR THERAPEUTIC AGENT FOR NEUROPATHIC PAIN ASSOCIATED WITH GUILLAIN-BARRE SYNDROME
20230059381 · 2023-02-23 ·

A P2X.sub.4 receptor antagonist such as paroxetine, a diazepinedione derivative having the following formula (IX) is used as an agent for preventing or treating neuropathic pain associated with Guillain-Barré syndrome:

##STR00001##

wherein R.sup.1 is hydrogen, a C.sub.1-8 alkyl group, or the like; each R.sup.2 and R.sup.3 is hydrogen, a C.sub.1-8 alkyl group, or the like; each of R.sup.4 and R.sup.5 is hydrogen or the like; and W is a five-membered or six-membered heterocyclic ring optionally having one or more substituents and comprising one to four nitrogen atoms as the members of the ring.

PROPHYLACTIC OR THERAPEUTIC AGENT FOR NEUROPATHIC PAIN ASSOCIATED WITH GUILLAIN-BARRE SYNDROME
20230059381 · 2023-02-23 ·

A P2X.sub.4 receptor antagonist such as paroxetine, a diazepinedione derivative having the following formula (IX) is used as an agent for preventing or treating neuropathic pain associated with Guillain-Barré syndrome:

##STR00001##

wherein R.sup.1 is hydrogen, a C.sub.1-8 alkyl group, or the like; each R.sup.2 and R.sup.3 is hydrogen, a C.sub.1-8 alkyl group, or the like; each of R.sup.4 and R.sup.5 is hydrogen or the like; and W is a five-membered or six-membered heterocyclic ring optionally having one or more substituents and comprising one to four nitrogen atoms as the members of the ring.