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1. WO2020198537 - MODULATORS OF MAS-RELATED G-PROTEIN RECEPTOR X4 AND RELATED PRODUCTS AND METHODS

Publication Number WO/2020/198537
Publication Date 01.10.2020
International Application No. PCT/US2020/025077
International Filing Date 26.03.2020
IPC
A61K 31/192 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
19Carboxylic acids, e.g. valproic acid
192having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid
A61K 45/06 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 17/04 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
04Antipruritics
A61P 29/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or antiinflammatory agents, e.g antirheumatic agents; Non-steroidal antiinflammatory drugs (NSAIDs)
A61P 37/02 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
C07C 15/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
15Cyclic hydrocarbons containing only six-membered aromatic rings as cyclic part
12Polycyclic non-condensed hydrocarbons
CPC
A61K 31/192
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic, hydroximic acids
19Carboxylic acids, e.g. valproic acid
192having aromatic groups, e.g. sulindac, 2-arylpropionic acids, ethacrynic acid
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 17/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
04Antipruritics
A61P 29/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
29Non-central analgesic, antipyretic or anti-inflammatory agents, e.g antirheumatic agents; Non-steroidal anti-inflammatory drugs (NSAIDs)
A61P 37/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
37Drugs for immunological or allergic disorders
02Immunomodulators
C07C 217/48
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
217Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
02having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
48the carbon skeleton being unsaturated and containing rings
Applicants
  • ESCIENT PHARMACEUTICALS, INC. [US]/[US]
Inventors
  • YEAGER, Adam
  • SELFRIDGE, Brandon
  • SAINZ, Marcos
  • MARTINBOROUGH, Esther
  • BOEHM, Marcus
  • HUANG, Liming
Agents
  • HERMANNS, Karl, R.
  • SUN, Eileen, S.
  • SOLTANI, Bobby, B.
  • HEFTER, Karl, A.
  • COOPER, Michael, P.
  • LI, Yiheng
  • CANTRELL, Tyler, C.
  • BAUNACH, Jeremiah, J.
  • OBEIDAT, Baha, A.
  • KUMABE, Blake, K.
  • ZENTZ, Bradley, J.
  • SARGEANT, Brooke
  • QUIST, Brooke, W.
  • ROTH, Carol, J.
  • EIDT, Chandra, E.
  • WITTKOPP, Cristina, J.
  • O'BRIEN, Daniel
  • CARLSON, David, V.
  • STARK, Duncan
  • TARLETON, E., Russell
  • HARWOOD, Eric, A.
  • GERTZ, Glenda, A.
  • HAN, Hai
  • TALBERT, Hayley, J.
  • BARRETT, Jared, M.
  • SAKOI, Jeffrey, M.
  • ZHANG, Jianping
  • MORGAN, John, A.
  • WAKELEY, John, J.
  • COE, Justin, E.
  • HENCKEL, Karen, M.
  • MORGAN, Kevan, L.
  • COSTANZA, Kevin, S.
  • LIN, Qing
  • HALLER, Rachel, A.
  • IANNUCCI, Robert
  • WEBB, Samuel, E.
  • LEEK, Shoko, I.
  • ROSENMAN, Stephen, J.
  • ABEDI, Syed
  • BOLLER, Timothy, L.
  • SHEWMAKE, Thomas, A.
  • CLAYTON, Kenneth W.
  • SAKOI, Zachary M.
  • MIXCO, Javier, M.
  • LIU, Shi
  • LAWRENZ, Steven, D.
  • CHEN, David W.
  • CONLEE, David C.
  • DANLEY, Jeffrey E.
  • BENDEMIRE, Paul D.
  • SEO, Jeong Hee
Priority Data
62/825,74128.03.2019US
62/849,09516.05.2019US
62/864,30620.06.2019US
62/938,27720.11.2019US
62/955,96731.12.2019US
62/959,79910.01.2020US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) MODULATORS OF MAS-RELATED G-PROTEIN RECEPTOR X4 AND RELATED PRODUCTS AND METHODS
(FR) MODULATEURS DU RÉCEPTEUR X4 DE LA PROTÉINE G ASSOCIÉE À MAS ET PRODUITS ET PROCÉDÉS ASSOCIÉS
Abstract
(EN)
Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I): (I) or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein n, x, A, Q1, Q2, Z, R, R1, R2, R3, R4 and R5 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.
(FR)
La présente invention concerne d'une manière générale des procédés de modulation de MRGPR X4 ou plus spécifiquement de traitement d'un état dépendant de MRGPR X4, en mettant en contact MRGPR X4 ou en administrant à un sujet qui le nécessite, respectivement, une quantité efficace d'un composé ayant la structure de formule (I) : (I) ou d'un isomère, d'un racémate, d'un hydrate, d'un solvate, d'un isotope pharmaceutiquement acceptable ou d'un de ses sels, n, x, A, Q1, Q2, Z, R, R1, R2, R3, R4 et R5 étant tels que définis dans la description. L'invention concerne également les compositions pharmaceutiques comprenant de tels composés ainsi que les composés proprement dits.
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