公开(公告)号：US20250154143A1

公开(公告)日：2025-05-15

申请号：US18683412

申请日：2022-08-18

Applicant: UCL BUSINESS LTD

Inventor： Mark Brian PEPYS ,  Melanie Susanne GLOSSOP ,  Christopher SWAIN ,  Graham Walter TAYLOR ,  Stephen Paul WOOD

IPC: C07D453/02

Abstract: An agent for use in medicine, wherein the agent comprises a compound of Formula (I): wherein: Ar is an aryl linker group, and R1 and R2 are independently selected from groups of formula —OH; —OR3; —O(CO)R3; —NR3R3′; wherein: R3 and R3′ are independently selected from H, C1-C12 alkyl, C1-C12 alkylene, C3-C8 (hetero)cycloalkyl, or C5-C12 (hetero)aryl, or R3 and R3′ together form a C3-C8 heterocyclic ring with the nitrogen, each optionally substituted with one, two or three groups selected from halogen, —CF3, —OR6, —NR6R6, —COR6, and —CO2R6, C3-C8 (hetero)cycloalkyl, or C5-C12 (hetero)aryl; R4 and R5 are independently selected from H or C1-C6 alkyl; and R6 and R6 are independently C1-C6 alkyl, or together form a C3-C8 heterocyclic ring with the nitrogen, provided that R1 and R2 are not both —OH, including individual pharmaceutically acceptable salts, solvates, or derivatives thereof.

公开(公告)号：US20230101069A1

公开(公告)日：2023-03-30

申请号：US17904393

申请日：2021-02-18

Applicant: UCL BUSINESS LTD

Inventor： Mark Brian PEPYS ,  Christopher SWAIN ,  Graham Walter TAYLOR ,  Stephen Paul WOOD ,  Melanie Susanne GLOSSOP ,  Charlotte Alice Louise LANE

IPC: A61K31/439 ,  A61K45/06

Abstract: An agent for use in medicine, wherein the agent comprises a compound of Formula (I): wherein Ar is an aryl linker group, for example a 1,4-phenyl group, including individual pharmaceutically acceptable salts, solvates, prodrugs or derivatives thereof. The compounds of Formula (I) are inhibitors of human C-reactive protein (CRP) and may be used for the treatment of medical conditions mediated by CRP. Also provided are methods of making the compounds of Formula (I) and chemical intermediates thereof.

公开(公告)号：US20230357134A1

公开(公告)日：2023-11-09

申请号：US18245235

申请日：2021-09-16

Applicant: UCL BUSINESS LTD

Inventor： Vittorio BELLOTTI ,  Alessandra CORAZZA ,  Palma Patrizia MANGIONE ,  Mark Brian PEPYS ,  Christopher SWAIN ,  Graham Walter TAYLOR

IPC: C07C229/58 ,  C07D237/24 ,  C07D213/80 ,  C07D263/57 ,  C07D231/12 ,  C07D263/34 ,  A61P43/00

CPC classification number: C07C229/58 ,  C07D237/24 ,  C07D213/80 ,  C07D263/57 ,  C07D231/12 ,  C07D263/34 ,  A61P43/00

Abstract: The present invention relates to compounds for stabilising the native tetrameric form of transthyretin and protecting it from proteolytic cleavage; compounds for use in the prevention and treatment of transthyretin amyloidosis; and agents and medicaments comprising such compounds. The compounds are based on a general structure A-L-B, wherein A is a group of formula (II) or of formula (III): or of formula (IV) or of formula (V) B is a group of formula (III), (IV), or (V), or a group of formula (VI) or a group of formula —R10Z, wherein: Z is selected from —CO2R′, —CONR′R″, —SO2R′ wherein R′ and R″ are independently H or C1-C4 alkyl; and R10 is a C1-C4 alkylene or alkenylene group; and L represents a linker group which is a saturated or unsaturated chain of 5 to 13 carbon atoms.

公开(公告)号：US20230118142A1

公开(公告)日：2023-04-20

申请号：US17904388

申请日：2021-02-18

Applicant: UCL BUSINESS LTD

Inventor： Mark Brian PEPYS ,  Christopher SWAIN ,  Graham Walter TAYLOR ,  Stephen Paul WOOD ,  Melanie Susanne GLOSSOP ,  Charlotte Alice Louise LANE

IPC: A61K31/439 ,  A61K31/662 ,  A61K31/4025

Abstract: The invention comprises an agent for use in medicine, wherein the agent comprises a compound of Formula (I): B-L-B′ wherein: B and B′ are independently selected from groups of formula (B-I) wherein: Z is selected from —COOH, —CH2COOH, —PO(OH)(OR1), or —CH2PO(OH) (OR1), wherein R1 is H or a phosphate protecting group; W is an alicyclic amine group having from 5 to 12 carbon atoms and at least one amine nitrogen atom; W′ is H, or W′ is linked to W to form said alicyclic amine group; and Y is selected from —NH—, —N(CH3)—, —CH2—, —NHCO—, —CH2CONH—, —CONH—, CH2NHCO—, or —NHCH2—; and L is a linker group.